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1080 Reassessment Application October 2006<br />

Appendix C<br />

<strong>Source</strong>: <strong>Landcare</strong> <strong>Research</strong><br />

(<strong>1964</strong>). <strong>Control</strong> <strong>of</strong> <strong>poisons</strong>. <strong>Royal</strong> Society <strong>of</strong> Health Journal 84, 52-53.<br />

Keywords: <strong>poisons</strong>/non-target species/fluoroacetamide/livestock<br />

Occupational Health Bulletin: Sodium Fluoroacetate Compound 1080. New Series No 1 (revision <strong>of</strong> Vol.6<br />

No 11, July 1962). 1967. Wellington, Department <strong>of</strong> Health.<br />

Ref Type: Pamphlet<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080<br />

(1969). Fluoroacetate. In 'Clinical toxicology <strong>of</strong> commercial products'. (M. Gleason, R. Gosselin, H.<br />

Hodge, and R. SmithEds. ) pp. 116-117. (The Williams & Wilkins: Baltimore.)<br />

Keywords: fluoroacetate/sodium fluoroacetate/diagnosis/treatment/acute toxicity<br />

Poisonings. 20. 1976. Surveillance 1976 No.4.<br />

Ref Type: Report<br />

Keywords: poisoning/1080/analysis/muscle/liver/livestock/witholding period<br />

Abstract: 1080 poisoning was in the public eye in Canterbury when sheep died after they were returned to a<br />

block pronounced "safe" after poisoning operations. About 160 ewes died out <strong>of</strong> 800, and 1080 poisoning<br />

was confirmed. It is reported that errors were made in the analysis <strong>of</strong> bait tested to determine if it was safe<br />

to stock. Recently a workshop on 1080 analysis was held at Invermay AHL. These are the<br />

recommendations for sampling: 1) Take the samples from the animals which are first to die in the outbreak<br />

even though they may be more autolysed. 2) The best specimens in order <strong>of</strong> preference are muscle, stomach<br />

contents then liver<br />

1080 poisoning. 26. 1976. Surveillance 1976 No. 4.<br />

Ref Type: Report<br />

Keywords: 1080/poisoning/birds/persistence in animals/non-target species/secondary poisoning/humans<br />

Abstract: Recently, Canada geese around Lake Benmore were poisoned by oats impregnated with 1080<br />

Diagnosis <strong>of</strong> 1080 poisoning in dogs. 4. 1978. Surveillance 1978 No.1.<br />

Ref Type: Report<br />

Keywords: 1080/poisoning/dogs/diagnosis<br />

Abstract: A dog may die <strong>of</strong> 1080 poisoning but have tissue 1080 levels too low to detect.<br />

(1986). Rodenticides, Fungicides, Herbicides, Fumigants and Repellents. In 'Poisoning. Toxicology,<br />

Symptoms, Treatments'. (J. M. Arena and R. H. DrewEds. ) pp. 226-227. (Charles C. Thomas: Springfield,<br />

Illinois, U.S.A.)<br />

Keywords: diagnosis/sodium fluoroacetate/treatment/poisoning<br />

(1988). Submission to the Animal Welfare Advisory Committee on the use <strong>of</strong> 1080 for pest animal control<br />

in Victoria. (Department <strong>of</strong> Conservation Forests and Lands: [Melbourne].)<br />

Keywords: field efficacy/ground control/welfare/1080<br />

(1991). Toxic Agents. In 'Casarett and Doull's Toxicology. The basic science <strong>of</strong> <strong>poisons</strong>.'. (M. O. Amdur,<br />

J. Doull, and C. D. KlaassenEds. ) p. 612. (Pergamon Press: New York, Oxford, Bejing, Frankfurt, Sao<br />

Paulo, Sydney, Tokyo, Toronto.)<br />

Keywords: fluoroacetate/poisoning/treatment/<strong>poisons</strong><br />

(1991). Sodium fluoroacetate. In 'Documentation <strong>of</strong> the threshold limit values and biological exposure<br />

indices : 6th ed'. pp. 1411-1415. (American Conference <strong>of</strong> Governmental Industrial Hygienists: Cincinnati.)<br />

Keywords: occupational exposure/regulatory toxicology/metabolism/sodium<br />

fluoroacetate/fluoroacetate/humans/developmental toxicity/reproductive effects<br />

1


1080 Reassessment Application October 2006<br />

Appendix C<br />

(1992). Sodium fluoroacetate. Federal register 57, 26275-26276.<br />

Keywords: occupational exposure/regulatory toxicology/sodium fluoroacetate/fluoroacetate/humans<br />

Water quality monitoring <strong>of</strong> Stage 1 <strong>of</strong> the Department <strong>of</strong> Conservation/ Taranaki Regional Council<br />

possum control operation on Mount Taranaki/Egmont 1993. 93-27, -20. 1993. Stratford, New Zealand,<br />

Taranaki Regional Council. Technical Report.<br />

Ref Type: Report<br />

Keywords: persistence in water/possums/aerial control/1080/fluoride/poisoning/persistence in invertebrates<br />

Abstract: Public concerns about stage 1 <strong>of</strong> the joint Department <strong>of</strong> Conservation/Taranaki Regional Council<br />

possum control operation on Mount Taranaki/Egmont included issues relating to potential effects <strong>of</strong> the use<br />

<strong>of</strong> 1080 poison on water quality and water usage, in particular domestic water supplies from catchments<br />

drainign areas within the aerial poison application zone. Taranaki Regional Council undertook a<br />

comprehensive water quality moniotring programme in recognition <strong>of</strong> these concerns, despite the existence<br />

<strong>of</strong> documented water quality monitoring information for two earlier aerila control operations (Waipoua<br />

Forest and Rangitoto Island) which indicated that no contamination <strong>of</strong> natural water by 1080 resulted from<br />

these large scale operations. This programme included natural surface waters within and outside (controls)<br />

the operational zone, major water supplies (raw and treated) and groundwaters. Monitoring concentrated on<br />

1080 and fluoride (the principal breakdown product) concentrations in the waters. Sampling commenced in<br />

advance <strong>of</strong> the first aerial application <strong>of</strong> 1080 and extended througout the operational period with one site<br />

smapled more intensively to monitor any immeduate impacts <strong>of</strong> the department <strong>of</strong> Conservation's initial<br />

three-day aerial poison drop within the National Park. In addition to the physicochemical monitoring, the<br />

programme was augmented with biological monitoring <strong>of</strong> three representative catchment sites draining the<br />

opertaional area and two catchment sites (controls) immediately beyond the boundaries. The results<br />

consistently showed no measurable impact <strong>of</strong> the possum control operation on the physicochemical<br />

parameters (1080 and fluoride concentrations) or biological indicators (benthic macroinvertebrate fauna)<br />

measured in any <strong>of</strong> the natural waters draining botht he National Park and the buffer zones within the<br />

operational poisoning area. No impacts attributable to the possum control operation were measured on<br />

these physicochemical parameters in teh raw and traeted domestic water supplies, or groundwaters<br />

monitored. The resutls <strong>of</strong> this relatively intensive monitoringprogram may provide guidelines for the<br />

assessment and estbalishment <strong>of</strong> appropriate monitoring <strong>of</strong> any future possum control operations <strong>of</strong> this<br />

nature.<br />

Water quality monitoring <strong>of</strong> Stages 2&3 <strong>of</strong> the Department <strong>of</strong> Conservation/ Taranaki Regional Council<br />

possum control operation on Mount Taranaki/Egmont 1994. 94-7, -20. 1994. Stratford, New Zealand,<br />

Taranaki Regional Council. Technical Report.<br />

Ref Type: Report<br />

Keywords: 1080/persistence in water/aerial control/possums/fluoride/poisoning/persistence in invertebrates<br />

Abstract: Public concerns relating to the joint Department <strong>of</strong> Conservation/Taranaki Regional Council<br />

possum control operation on Mount Taranaki/Egmont included issues relating to potential effects <strong>of</strong> the use<br />

<strong>of</strong> 1080 poison on water quality and water usage, in particular domestic water supplies from catchments<br />

draining areas within the aerial poison application zone. Taranaki Regional Council, in 1993, undertook a<br />

comprehensive water quality monitoring <strong>of</strong> stage 1 <strong>of</strong> the control programme in recognition <strong>of</strong> these<br />

concerns, despite the existence <strong>of</strong> documented water quality monitoring information for two earlier aerila<br />

control operations (Waipoua Forest and Rangitoto Island) which indicated that no contamination <strong>of</strong> natural<br />

water by 1080 resulted from these large scale operations. Taranaki Regional Council results consistently<br />

showed no measurable impact <strong>of</strong> the possum control operation on the physicochemical parameters (1080<br />

and fluoride concentrations) or biological indicators (benthic macroinvertebrate fauna) measured in any <strong>of</strong><br />

the natural waters draining both the National Park and the buffer zones within the operational poisoning<br />

area. No impacts attributable to the possum control operation were measured on these physicochemical<br />

parameters in the raw and treated domestic water supplies, or groundwaters monitored. The results <strong>of</strong> this<br />

relatively intensive monitoring programme provided guidelines for the performance <strong>of</strong> an appropraite<br />

monitoring programme in association with the remaining stages (2&3) <strong>of</strong> the Mount Taranaki/Egmont<br />

possum control operations. The programme concentrated on the physicochemical moniotring <strong>of</strong> seven<br />

treated local authority water supplies abstracted from catchments draining the operational area, and was<br />

complemented with intensive monitoring <strong>of</strong> one raw surface water supply catchment, and biological<br />

monitoring <strong>of</strong> representative surface waters in close porximity to the National Park operational area.<br />

2


1080 Reassessment Application October 2006<br />

Appendix C<br />

Sampling commenced in advance <strong>of</strong> the aerial operation <strong>of</strong> 1080 and extended throughout the operational<br />

period with one site sampled more intensively to monitor any immediate impacts <strong>of</strong> the aerial poisoning<br />

application within the National Park and adjacent bush. The monitoring confirmed 1993 results, with no<br />

detectable concentrations <strong>of</strong> 1080 measured, in natural or treated water supplies, before, during or within<br />

one month following the possum control operation. No measurable impacts <strong>of</strong> this operation were found<br />

from the monitoring <strong>of</strong> fluoride concentrations and longer term biological indicators (benthic<br />

macroinvertebrate fauna) in the representative ctahcments draining the operational area. The results <strong>of</strong> both<br />

water quality programmes (all three stages <strong>of</strong> the Mount Taranaki/Egmont possum control operation) hvae<br />

combined to provide the most intensive moniotring <strong>of</strong> a 1080 poisoning operation to date in New Zealand,<br />

and may contribute to the estbalishment <strong>of</strong> appropriate monitoring <strong>of</strong> future possum control operations <strong>of</strong><br />

this nature.<br />

(1995). Pesticide poisoning. (U.K. Department <strong>of</strong> Health:<br />

Keywords: poisoning/acute toxicity/treatment<br />

The use <strong>of</strong> genetically modified rumen bacteria to protect livestock from fluoroacetate poisoning. [29<br />

March 2000], 1-24. 2000. Murdoch University, Western Australia.<br />

Ref Type: Conference Proceeding<br />

Keywords: bacteria/livestock/fluoroacetate/poisoning/GMO<br />

Abstract: The workshop consisted <strong>of</strong> oral presentations and discussion among attendees who are involved<br />

in various aspects <strong>of</strong> the Fluoroacetate Detoxification Project and those who have raised concerns on the<br />

possible environmental and conservation outcomes <strong>of</strong> the use <strong>of</strong> GMOs to protect ruminant livestock from<br />

fluoroacetate poisoning. The aim <strong>of</strong> the workshop was to establish the precautions required for safe testing<br />

<strong>of</strong> the GMOs and to define those factors that should be established before general use <strong>of</strong> the GMOs can be<br />

considered.<br />

Factors discussed included the producer-driven origins <strong>of</strong> the project, the technology employed, and the<br />

outcome <strong>of</strong> animal toxicity tests to prove the efficacy <strong>of</strong> the GMOs. This was balanced by discussion <strong>of</strong><br />

potential risks to pest control with Compound 1080, and environmental effects <strong>of</strong> the GMOs through<br />

possible alterations to browsing behaviour <strong>of</strong> domestic and feral ruminants and native animals with<br />

prefermentative digestive systems.<br />

Aggarwal, A., Kaur, G., and Mehrotra, R. S. (1986). Effect <strong>of</strong> certain metabolic inhibitors on growth and<br />

respiration <strong>of</strong> Phytophtora colocasiae Racib. Indian Bot.Reptr. 5, 119-122.<br />

Keywords: fungus/sodium fluoroacetate/fluoroacetate/poisoning/aconitase/enzyme/inhibition/fluoride<br />

Abstract: In the present investigation all the six metabolic inhibitors tested showed the inhibitory effects on<br />

respiration and mycelial growth. Sodium fluoroacetate which is known to inhibit TCA cycle by poisoning<br />

aconitase enzyme activity also showed inhibition. Sodium fluoride which also showed inhibition and is<br />

known to inactive enolase enzyme <strong>of</strong> EM pathway.<br />

Agricultural Compounds and Veterinary Medicines Group. <strong>Control</strong>led pesticides. Sodium fluoroacetate<br />

(1080) in pest control. VPC - 1080 03/00, -5. 2000.<br />

Ref Type: Report<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080<br />

Agricultural Pests Destruction Council. Use <strong>of</strong> 1080 poison for agricultural pest control. 1977. Wellington,<br />

Agricultural Pests Destruction Council.<br />

Ref Type: Pamphlet<br />

Keywords: 1080/poison/rabbits/possums<br />

Agriculture Protection Board <strong>of</strong> Western Australia. The proposed use <strong>of</strong> 1080 to control feral goats in<br />

Western Australia. 752. 1993. Perth, Agricultural Protection Board <strong>of</strong> Western Australia. Public<br />

Environmental Review.<br />

Ref Type: Report<br />

Keywords: 1080/goats<br />

3


1080 Reassessment Application October 2006<br />

Appendix C<br />

Akao, S. and Kubota, S. (1978). Biosynthesis <strong>of</strong> organic acids in satsuma fruits. 3. Changes in 14C-labelled<br />

organic acids (citrate-1, 5-14C, malate-14C (U), succinate-2, 3-14C and pyruvate-3-14C) in juice vesicles.<br />

Bulletin <strong>of</strong> the Shikoku Agricultural Experiment Station No. 32, 43-48.<br />

Keywords: biosynthesis/citrate/fluoroacetate<br />

Abstract: When malate -14C was added to juice vesicles, labelled citrate and succinate were detected after<br />

3 hours; when succinate-14C was added citrate, malate and fumarate were detected; when pyruvate-14C<br />

was added citrate, malate, fumarate and succinate were detected. Fluoroacetate and malonate had inhibitory<br />

effects. These findings indicate that the TCA cycle operates in juice vesicles. [For parts 1 and 2 see HcA<br />

44, 5088 and 5089.]<br />

al Juburi, A. Z., Clarkson, T. W., and Cockett, A. T. (1989). Vasocystostomy: a model for studying male<br />

reproductive toxicity in the rat. ReproductiveToxicology 3, 181-186.<br />

Keywords: toxicity/testes/reproductive effects/rats/pathology/target organ<br />

Alabaster, J. S. (1969). Survival <strong>of</strong> fish in 164 herbicides, insecticides, fungicides, wetting agents and<br />

miscellaneous substances. International Pest <strong>Control</strong> 11, 29-35.<br />

Keywords: fluoroacetamide/fish/aquatic species/toxicity/lethal concentration<br />

Alekseev, A. N. and Turov, I. S. (1967). A study <strong>of</strong> fluoracetamide as a poison to systemic activity.<br />

Zhurnal Mukrobiologii 44, 98-103.<br />

Keywords: fluoroacetamide/invertebrates/rats/systemic toxicity/poison/lethal dose<br />

Abstract: Fluoracetamide (CH2F CON H2) was studied in the capacity <strong>of</strong> a poison with systemic effect. This preparation proved to be toxic for<br />

Xenopsylla cheopis Rotsch. and for Ceratophyllus consimilis Wagn. in feeding them through a biomembrane with the nutritional solution containing this poison.<br />

Toxemia in albino rats lasted for not less than 19 hours following fluoracetamide administration (the agent was intorduced by feeding fleas <strong>of</strong> the mentioned species<br />

on rats). Almost all the fleas (fed on albino rats gievn the preparation in doses 1.5-2 times lower than the minimal lethal dose) gradually perished - on the 6th -10th<br />

day. An opinion is put forward on the expediency <strong>of</strong> field trial <strong>of</strong> fluroacetamide not only as a rat poison, but also as a preparation with systemic effect.<br />

Alekseev, A. N., Avdeeva, E. V., Turov, I. S., and Tokareva, T. G. (1971). The chemosterilising effect <strong>of</strong><br />

fluoroorganic compounds on larvae and adults <strong>of</strong> fleas ectoparasitic on rodentsRussian Incomplete.<br />

Abstract: It was established in laboratory experiments that organic fluorine compounds, fluoroacetamide<br />

and sodium fluoroacetate at dosages sublethal for rodents and their ectoparasites inhibit reproduction in<br />

males and females <strong>of</strong> Nosopsyllus (Ceratophyllus) consimilis (Wagn.) and Xenopsylla cheopis (Roths.) if<br />

the compounds are imbibed, and also have some effect on adults developing from larvae that had eaten<br />

faeces <strong>of</strong> fleas that contained poisoned blood. This effect was more evident in N. consimilis than in X.<br />

cheopis, which is less sensitive to fluorine poisoning<br />

Algar, D. and Kinnear, J. E. (1996). Secondary poisoning <strong>of</strong> foxes following a routine 1080 rabbit-baiting<br />

campaign in the Western Australian wheatbelt. CALMScience 2, 149-151.<br />

Abstract: There is circumstantial evidence that foxes (Vulpes vulpes) feeding on rabbits (Oryctolagus<br />

cuniculus) poisoned with sodium mon<strong>of</strong>luoroacetate (1080 poison) die from secondary poisoning. A rabbitpoisoning<br />

campaign that occurred during a fox research study provided direct evidence to support the<br />

above view<br />

Allcr<strong>of</strong>t, R., Peters, R. A., and Shorthouse, M. (1969). Fluoroacetamide poisoning : part II. Toxicity in<br />

dairy cattle : confirmation <strong>of</strong> diagnosis. Veterinary record 84, 403-409.<br />

Keywords: acute toxicity/diagnosis/non-target species/persistence in animals/persistence in<br />

plants/persistence in water/fluoroacetamide/poisoning<br />

Allcr<strong>of</strong>t, R. and Jones, J. S. L. (1969). Fluoroacetamide poisoning : part I. Toxicity in dairy cattle : clinical<br />

history and preliminary investigations. Veterinary record 84, 399-402.<br />

Keywords: acute toxicity/diagnosis/non-target species/fluoroacetamide/poisoning<br />

Allender, W. J. (1990). Determination <strong>of</strong> sodium fluoroacetate (Compound 1080) in biological tissues.<br />

Journal <strong>of</strong> Analytical Toxicology 14, 45-49.<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080/sodium mon<strong>of</strong>luoroacetate/baits/analysis<br />

Abstract: A sensitive gas chromatographic method was developed for the determination <strong>of</strong> sodium<br />

4


1080 Reassessment Application October 2006<br />

Appendix C<br />

mon<strong>of</strong>luoroacetate (Compound 1080 and 1080 poison) in baits and avian tissues. The procedure involves<br />

extraction <strong>of</strong> 1080 with acetone/water (8:1) followed by derivation with pentafluorobenzyl bromide.<br />

Cleanup <strong>of</strong> the esterified extracts was carried out using minicolumns containing Florisil and the eluates<br />

were subsequently analyzed by electron capture gas chromatography. Bait samples were initially screened<br />

by thin-layer chromatography and identity <strong>of</strong> derivatized extracts was confirmed by gas chromatography/<br />

mass spectrometry.<br />

Allender, W. J. (1990). Determination <strong>of</strong> sodium fluoracetate (compound 1080) in biological tissues.<br />

Journal <strong>of</strong> Analytical Toxicology 14, 45-49.<br />

Keywords: 1080/sodium fluoroacetate/fluoroacetate/baits/analysis<br />

Abstract: A sensitive gas chromatographic method is described for the determination <strong>of</strong> sodium<br />

fluoroacetate in baits and avian tissues. Acetone/water extracts <strong>of</strong> tissues and bait were screened by thin<br />

layer chromatography before postcolumn derivization with pentafluorobenzyl bromide. Cleanup <strong>of</strong> the<br />

extracts was carried out using minicolumns containing Florisil. Eluates were analysed by electron capture<br />

gas chromatography. The method was applied to tissues from a magpie (Gymnorhina tibicen) that had<br />

ingested bait containing compound 1080<br />

Allender, W. J. (1990). The determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound 1080) in formulation<br />

and technical samples by high pressure liquid chromatography. Journal <strong>of</strong> Liquid Chromatography 13,<br />

3465-3472.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/liquid chromatography/analysis<br />

Abstract: A high pressure liquid chromatographic (HPLC) procedure was developed for the determination<br />

<strong>of</strong> sodium mon<strong>of</strong>luoroacetate (Compound 1080). The procedure utilized an amine (NH-2) bonded column<br />

for the reverse phase determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate in formulation and technical samples<br />

Alterio, N. (2000). <strong>Control</strong>ling small mammal predators using sodium mon<strong>of</strong>luoroacetate (1080) in bait<br />

stations along forestry roads in a New Zealand beech forest. New Zealand journal <strong>of</strong> ecology 24, 3-9.<br />

Keywords: secondary poisoning/ground<br />

control/1080/cats/possums/brodifacoum/poisoning/gut/predators/rats/efficacy/carnivores/poison/wildlife<br />

Abstract: A single five night pulse <strong>of</strong> sodium mon<strong>of</strong>luroacetate (0.15% 1080) applied in bait stations at two<br />

different spacing intervals, 100 and 200 m, along forestry roads in New Zealand beech forest, killed all four<br />

<strong>of</strong> the resident radio-tagged stoats (Mustela erminea) and all three <strong>of</strong> the resident radio-tagged wild house<br />

cats (Felis catus) by secondary poisoning. Gut contents <strong>of</strong> predators indicated that house mice (Mus<br />

musculus), ship rats (Rattus rattus) and bushtail possums (Trichosurus vulpecula) were important sources <strong>of</strong><br />

the toxin. High kills <strong>of</strong> predators, possums and rats at both 100 and 200 m spacing regimes suggest that<br />

greater efficacy <strong>of</strong> controlling these pests would be achieved with the latter method. Evidence suggests that<br />

routine management <strong>of</strong> possums and rats using 1080 and brodifacoum has resulted in widespread control <strong>of</strong><br />

small mammalian carnivores by secondary poisoning in New Zealand forests. However, aerial application<br />

<strong>of</strong> poison can kill large numbers <strong>of</strong> tomtits (Petroica macrocephala) and robins (Petroica australis) and few<br />

other native bird species have been adequately monitored through such operations. Reducing risks to native<br />

wildlife is responsible ecological management. Use <strong>of</strong> bait stations along forestry roads or tracks may be<br />

fundamental in mounting cost-effective :Large-scale ground-based protection <strong>of</strong> native wildlife through<br />

safer predator controls.<br />

Andersen, I. Ban on bacterium that makes poison plants safe. New scientist 4 February 1995, 5. 1995.<br />

Ref Type: Magazine Article<br />

Keywords: bacteria/degradation/fluoroacetate<br />

Ando, J. (1966). A selective blockade <strong>of</strong> the cardiac inotropic effect <strong>of</strong> adrenaline by sodium<br />

mon<strong>of</strong>luoroacetate. Bulletin <strong>of</strong> Osaka Medical School 12, 1-4.<br />

Keywords: cardiac/sodium mon<strong>of</strong>luoroacetate/heart/rabbits/mode <strong>of</strong> action<br />

Abstract: In a few cases <strong>of</strong> the experiments with isolated, perfused rabbit heart preparations having received<br />

sodium mon<strong>of</strong>luoroacetate, adrenalin produced only a positive chronotropic effect without any concomitant<br />

positive intropic one in the course <strong>of</strong> development <strong>of</strong> heart failure induced by the metabolic inhibitor.<br />

5


1080 Reassessment Application October 2006<br />

Appendix C<br />

Annison, E. F., Hill, K. J., Lindsay, D. B., and Peters, R A. (1960). Fluoroacetate poisoning in sheep.<br />

Journal <strong>of</strong> comparative pathology 70, 145-155.<br />

Keywords: non-target species/mammals/pathology/heart/sublethal<br />

effects/fluoroacetate/poisoning/livestock/poison/toxicity/antidote/acetate/blood<br />

Abstract: Poisoning <strong>of</strong> livestock by the ingestion <strong>of</strong> the South African Plant Dichapetalum cymosum has<br />

long been recognised. The toxic principle <strong>of</strong> this plant is fluoroacetate (Marais, 1944). More recently the<br />

introduction <strong>of</strong> sodium fluoracetate as a rat and rabbit poison has provided another source <strong>of</strong> this toxic<br />

substance which may be potentially dangerous to the grazing animal. These facts justify a close study <strong>of</strong><br />

fluoroacetate poisoning in ruminants since, despite a considerable literature on the biochemical nature <strong>of</strong><br />

fluoroacetate poisoning in laboratory animals (Peters, 1952), there is little reliable information on its action<br />

and toxicity in the larger domestic animals. The most urgent problem however is to obtain an antidote. In<br />

some animals, acetate is a major product <strong>of</strong> fermentation in the rumen, and the concentration <strong>of</strong> acetate in<br />

the blood <strong>of</strong> these animals is usually 3 to 10 times that <strong>of</strong> nonruminants. It was not, therefore, anticipated<br />

that acetate would prove to be an effective antidote in sheep, but some protective action <strong>of</strong> acetate has been<br />

demonstrated in preliminary experiments which are described in this paper. Data on the toxic dose <strong>of</strong><br />

fluoroacetate in sheep and some <strong>of</strong> its biochemical effect are also reported.<br />

Annison, E. F. and Bryden, W. L. (1998). Perspectives on ruminant nutrition and metabolism I. Metabolism<br />

in the rumen. Nutrition research reviews 11, 173-198.<br />

Keywords: metabolism/non-target species/pathology<br />

Abstract: Advances in knowledge <strong>of</strong> ruminant nutrition and metabolism during the second half <strong>of</strong> the<br />

twentieth century have been reviewed. Part I is concerned with metabolism in the rumen: Part II discusses<br />

utilization <strong>of</strong> nutrients absorbed from the rumen and lower tract to support growth and reproduction. The<br />

time frame was prompted by the crucial advances in ruminant physiology which arose from the work <strong>of</strong> Sir<br />

Jospeh Barcr<strong>of</strong>t and his colleagues at Cambridge in the 1940s and 50s, and by the brilliant studies <strong>of</strong> Robert<br />

Hungate on rumen microbiology at much the same time. In reviewing the growth <strong>of</strong> knowledge <strong>of</strong> the role<br />

<strong>of</strong> bacteria, protozoa, fungi and bacteriophages in the rumen, outstanding developments have included the<br />

identification and characterization <strong>of</strong> fungi and the recognition that the utilization <strong>of</strong> polysaccharides in the<br />

rumen is accomplished by the sequential activities <strong>of</strong> consortia <strong>of</strong> rumen microorganisms. The role <strong>of</strong><br />

protozoa is discussed in relation to the long standing debate on whether or not the removal <strong>of</strong> protozoa<br />

(defaunation) improves the efficiency <strong>of</strong> ruminant production. In relation to nitrogen (N) metabolism, the<br />

predation <strong>of</strong> bacteria by protozoa increases protein turnover in the rumen and reduces the efficiency <strong>of</strong><br />

microbial protein production. This may account for the beneficial effects <strong>of</strong> defaunation where dietary N<br />

intakes are low and possibly rate limiting for growth and production. Current approaches to the<br />

measurement <strong>of</strong> rates <strong>of</strong> production <strong>of</strong> short chain fatty acids (SCFA) in the rumen based on the<br />

mathematical modelling <strong>of</strong> isotope dilution data are outlined. The absorption <strong>of</strong> SCFA from the rumen and<br />

hindgut is primarily a passive permeation process. The role <strong>of</strong> microorganisms in N metabolism in the<br />

rumen has been discussed in relation to ammonia and urea interrelationships and to current inadequacies in<br />

the measurement <strong>of</strong> both protein degradation in the rumen and microbial protein synthesis. The growth <strong>of</strong><br />

knowledge <strong>of</strong> digestion and absorption <strong>of</strong> dietary lipids has been reviewed with emphasis on the<br />

antimicrobial activity <strong>of</strong> lipids and the biohydrogenation <strong>of</strong> unsaturated fatty acids. The protection <strong>of</strong><br />

unsaturated dietary fats from ruminal biohydrogenation is an approach to the manipulation <strong>of</strong> the fatty acid<br />

composition <strong>of</strong> meat and dairy products. Discussion <strong>of</strong> the production <strong>of</strong> toxins in the rumen and the role <strong>of</strong><br />

microorganisms in detoxification has focused on the metabolism <strong>of</strong> oxalate, nitrate, mycotoxins, saponins<br />

and the amino acid mimosine. Mimosine occurs in the tropical shrub leucaena, which is toxic to cattle in<br />

Australia but not in Hawaii. Tolerance to leucaena stems from the presence <strong>of</strong> a bacterium found in the<br />

rumen <strong>of</strong> Hawaiian cattle, which when transferred to Australian cattle survives and confers protection from<br />

mimosine. The genetic modification <strong>of</strong> rumen microorganisms to improve their capacity to ultilize nutrients<br />

or to detoxify antinutritive factors is an attractive strategy which has been pursued with outstanding success<br />

in the case <strong>of</strong> fluoroacetate. A common rumen bacterium has been genetically modified to express the<br />

enzyme fluoroacetate dehalogenase. The modified organism has been shown to survive in the rumen at<br />

metabolically significant levels and to confer substantial protection from fluoroacetate poisoning.<br />

Anon (1900). West Australian poison plants. Official report. Journal <strong>of</strong> the Department <strong>of</strong> Agriculture <strong>of</strong><br />

Western Australia 2, 418-423.<br />

Keywords: poison/occurrence in nature<br />

6


1080 Reassessment Application October 2006<br />

Appendix C<br />

Anonymous. Animal <strong>Research</strong>: bait development and toxicology. Forest <strong>Research</strong> Institute Report 1979,<br />

67-70. 1979. Rotorua, New Zealand.<br />

Ref Type: Report<br />

Keywords: acute toxicity/toxicity/1080/poison/lethal dose<br />

Abstract: Studies <strong>of</strong> the acute toxicity <strong>of</strong> compound 1080 to psosums have made considerable progress. In a<br />

2-year programme involving eight separate dosing trials <strong>of</strong> captive animals from North and South Island<br />

sources, the estimated LD50 (ie. the dose estimated to kill 50% <strong>of</strong> a sample population) ranged between 1.3<br />

and 2.1 mg/kg. These are higher doses than the 0.8 mg/kg which has been accepted on the evidence <strong>of</strong><br />

previous experimenters. It is becoming clear that the estimate may be affected by factors such as the type <strong>of</strong><br />

possum, its age and sex and perhaps physical condition, the weather, degree <strong>of</strong> acclimatisation <strong>of</strong> the<br />

animals to captivity, season, time <strong>of</strong> day and the technique <strong>of</strong> administering the poison.<br />

Aplin, T. E. H. (1967). Poison plants <strong>of</strong> Western Australia. The toxic species <strong>of</strong> the genera Gastrolobium<br />

and Oxylobium 1. Characteristics <strong>of</strong> the group. Journal <strong>of</strong> Agriculture <strong>of</strong> Western Australia 8, 42-52.<br />

Keywords: poison/occurrence in nature<br />

Aplin, T. E. H. (1967). Poison plants <strong>of</strong> Western Australia. The toxic species <strong>of</strong> the genera Gastrolobium<br />

and Oxylobium. York Road Poison and Box Poison. Journal <strong>of</strong> Agriculture <strong>of</strong> Western Australia 8, 200-<br />

206.<br />

Keywords: poison/occurrence in nature<br />

Aplin, T. E. H. (1971). Poison plants <strong>of</strong> Western Australia. The toxic species <strong>of</strong> the genera Gastrolobium<br />

and Oxylobium. Wodjil poison (Gastrolobium floribundum S. Moore), breelya or kite-leaf poison<br />

(Gastrolobium laytonii J. White), Roe's poison (Oxylobium spectabile Endl) and granite poison<br />

(Oxylobium graniticum S. Moore). Journal <strong>of</strong> Agriculture <strong>of</strong> Western Australia 12, 154-159.<br />

Keywords: fluoroacetate/poison/occurrence in nature<br />

Aplin, T. E. H. (1971). Poison plants <strong>of</strong> Western Australia: Gastrolobium and Oxylobium. Western<br />

Australian Department <strong>of</strong> Agriculture Bulletin No. 3772, 1-64.<br />

Keywords: poison/livestock/fluoroacetate/occurrence in nature<br />

Abstract: Toxic species <strong>of</strong> the genera Gastrolobium and Oxylobium, which cause considerable numbers <strong>of</strong><br />

livestock deaths in Western Australia as a result <strong>of</strong> their fluoroacetate content, are described<br />

Arellano, M., Malet-Martino, M., and Martino, R. (1995). First experiments demonstrating the<br />

metabolization <strong>of</strong> 5-fluorouracil into highly toxic fluoroacetate. Proceedings <strong>of</strong> the American Association<br />

for Cancer <strong>Research</strong> 36, 405.<br />

Keywords: 5-fluorouracil/fluoroacetate/NMR/metabolism<br />

Abstract: Over the last decade, the number <strong>of</strong> reports <strong>of</strong> cardiotoxicity and neurotoxicity attributed to 5fluorouracil<br />

(FU) has rapidly increased. Several authors postulated but never experimentally demonstrated<br />

that FU might be transformed into fluoroacetate (FAC), a highly cardiotoxic and neurotoxic poison. Using<br />

19 F NMR, we demonstrated for the first time, in the isolated perfused rat liver (IPRL) model and in rats,<br />

that the last catabolite <strong>of</strong> FU is not α-fluoro-β-alanine. The metabolism continues and leads to two new<br />

catabolites, FAC and 2-fluoro-3-hydrooxypropionic acid. IPRL were treated with 15 or 45 mg FU/kg b.w..<br />

Rats were injected intraperitoneally with 180 mg FU/kg b.w.. FU used in these experiments was pure, i.e.<br />

free from degradation compounds that can be precursors <strong>of</strong> FAC. The levels <strong>of</strong> FAC found in perfusates or<br />

in rat urine were low: 0.14% and 0.05% <strong>of</strong> injected FU for 15 and 45 mg FU/kg respectively in perfusates<br />

and 0.006% in rat urine. However, FAC cumulation can occur and might be responsible for the cardiotoxic<br />

and/or neurotoxic symptoms.<br />

Arellano, M., Malet-Martino, M., Martino, R., and Spector, T. (1997). 5-Ethynyluracil (GW776) : effects<br />

on the formation <strong>of</strong> the toxic catabolites <strong>of</strong> 5-fluorouracil, fluoroacetate and fluorohydroxypropionic acid in<br />

the isolated perfused rat liver model. British journal <strong>of</strong> cancer 76, 1170-1180.<br />

Keywords: mode <strong>of</strong> action/pathology/metabolism<br />

7


1080 Reassessment Application October 2006<br />

Appendix C<br />

Arellano, M., Malet-Martino, M., Martino, R., and Gires, P. (1998). The anti-cancer drug 5-fluorouracil is<br />

metabolized by the isolated perfused rat liver and in rats into highly toxic fluoroacetate. British journal <strong>of</strong><br />

cancer 77, 79-86.<br />

Keywords: mode <strong>of</strong> action/NMR/metabolism/humans/5fluorouracil/fluoroacetate/liver/rats/analysis/urine/poison/degradation<br />

Abstract: We report the first demonstration <strong>of</strong> the biotransformation <strong>of</strong> the anti-cancer drug 5-fluorouracil<br />

(FU) into two new metabolites, alpha-fluoro-beta-hydroxypropionic acid (FHPA) and fluoroacetate (FAG),<br />

in the isolated perfused rat liver (IPRL) and in the rat in vivo. IPRL was perfused with solutions <strong>of</strong> pure FU<br />

at two doses, 15 or 45 mg kg(-1) body weight, and rats were injected i.p. with 180 mg <strong>of</strong> FU kg(-1) body<br />

weight. Fluorine-19 NMR analysis <strong>of</strong> perfusates from IPRL and rat urine showed the presence <strong>of</strong> the<br />

normal metabolites <strong>of</strong> FU and low amounts <strong>of</strong> FHPA (0.4% or 0.1% <strong>of</strong> injected FU in perfusates from<br />

IPRL treated with 15 or 45 mg <strong>of</strong> FU kg(-1) body weight, respectively; 0.08% <strong>of</strong> the injected FU in rat<br />

urine) and FAC (0.1% or 0.03% <strong>of</strong> injected FU in perfusates from IPRL treated with 15 or 45 mg <strong>of</strong> FU<br />

kg(-1) body weight, respectively; 0.003% <strong>of</strong> the injected FU in rat urine). IPRL was also perfused with a<br />

solution <strong>of</strong> alpha-fluoro-beta-alanine (FBAL) hydrochloride at 16.6 mg kg(-1) body weight dose equivalent<br />

to 15 mg <strong>of</strong> FU kg(-1) body weight. Low amounts <strong>of</strong> FHPA (0.2% <strong>of</strong> injected FBAL) and FAC (0.07%)<br />

were detected in perfusates, thus demonstrating that FHPA and FAC arise from FBAL catabolism. As FAC<br />

is a well-known cardiotoxic poison, and FHPA is also cardiotoxic at high doses, the cardiotoxicity <strong>of</strong> FU<br />

might stem from at least two sources. The first one, established in previous papers (Lemaire et al, 1992,<br />

1994), is the presence in commercial solutions <strong>of</strong> FU <strong>of</strong> degradation products <strong>of</strong> FU that are metabolized<br />

into FHPA and FAG; these are formed over time in the basic medium necessary to dissolve the drug. The<br />

second, demonstrated in the present study, is the metabolism <strong>of</strong> FU itself into the same compounds.<br />

Arrovaye, C. Pers. comm. 2004.<br />

Ref Type: Personal Communication<br />

Keywords: humans/poisoning/treatment<br />

Abstract: Thank you for your information.<br />

I want to say to you that compound 1080 is the 3rd cause <strong>of</strong> intoxication in<br />

Antioquia, Colombia, after the medicaments and organophosphates. We treat<br />

this intoxication with etanol with good results but we have problems with<br />

the determination in laboratory because is difficult, that is the reason for<br />

what we haven`t published it. Last year we had 20 patiens with this<br />

intoxication in an Universitary Hospital.<br />

We can be in contact.<br />

Mi address is: Cra.94 No.38-275 Apto204 Medellín, Colombia.<br />

Thank you very much.<br />

Artyushkova, V. A. and Timeyko, V. N. (1982). [Effect <strong>of</strong> sodium fluoroacetate on oxygen consumption in<br />

liver and skeletal muscles <strong>of</strong> rats and cats]. Vopr.Med.Khim. 28, 77-81.<br />

Keywords: sodium fluoroacetate/fluoroacetate/liver/muscle/rats<br />

Abstract: Endogenous respiration in cat liver tissue homgenates decreased 5 hrs after intraperitoneal<br />

administration <strong>of</strong> sodium fluoroacetate at a dose <strong>of</strong> 0.35 mg/kg. In rats the endogenous liver tissue<br />

respiration was unaltered even after the intraperitoneal administration <strong>of</strong> the compound at a dose <strong>of</strong> 5<br />

mg/kg. At the same time, the endogenous respiration was inhibited in rat skeletal muscle homogenates<br />

within 5 hrs after the intoxication but it was not altered in the cat skeletal muscles. In vitro sodium<br />

fluoroacetate inhibited respiration in the homogentaes <strong>of</strong> cat and rat skeletal muscles and <strong>of</strong> cat liver tissue<br />

and did not affect the respiration in rat liver homogenates. Pyruvate protected completely the cat and rat<br />

skeletal muscle preparations and partially cat liver tissue against the fluoroacetate effect in vivo.<br />

Ashok, A., Gurinderjit, K., Mehrotra, R. S., Aggarwal, A., and Kaur, G. (1986). Effect <strong>of</strong> certain metabolic<br />

inhibitors on growth and respiration <strong>of</strong> Phytophthora colocasiae Racib. Indian Botanical Reporter 5, 119-<br />

122.<br />

8


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: sodium fluoroacetate/fluoroacetate/fluoride<br />

Abstract: In lab. tests sodium azide, mercuric chloride, sodium fluoroacetate, sodium malonate, methylene<br />

blue and sodium fluoride inhibited respiration and mycelial growth <strong>of</strong> P. colocasiae on Colocasia esculenta<br />

Aspin, P., Stringer, I., and Potter, M. Invertebrate abundance in pitfall traps before and after aerial sowing<br />

and bait station presentations <strong>of</strong> 1080. Ecological consequences <strong>of</strong> <strong>poisons</strong> used for mammalian pest<br />

control, meeting Christchurch 9-10 July 1998 , -17. 1999.<br />

Ref Type: Abstract<br />

Keywords: 1080/invertebrates/non-target species/ground control/aerial control<br />

Ataria, J. M., Eason, C. T., Norris, B., Temple, W., Hope, A., and Smith, N. A. (1995). Evaluation <strong>of</strong> 1080<br />

antidotes. (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Lincoln.)<br />

Keywords: treatment/1080<br />

Abstract: Objectives : To identify potential antidotes for 1080 poisoning from the literature on the<br />

pharmacology <strong>of</strong> 1080 and its metabolites; to provide a synopsis <strong>of</strong> a survey <strong>of</strong> current veterinary practices<br />

for the treatment <strong>of</strong> animals suffering from 1080 poisoning; to confirm citrate and calcium concentrtaions<br />

and aconitrtae hydratase activity as biochemical markers <strong>of</strong> 1080 poisoning; to evaluate potentail antidotes.<br />

Conclusions : Citrate concentration is a reliable biomarker <strong>of</strong> 1080 poisoning; ionised calcium is not;<br />

acetamide shows prophylactic properties at the clinical level; in contrast, glyceraol monoacetate does not<br />

reduce 1080-induced biochemical changes in citrate;<br />

Ataria, J. M., Wickstrom, M. L., Arthur, D., and Eason, C. T. (2000). Biochemical and histopathological<br />

changes induced by sodium mon<strong>of</strong>luoroacetate (1080) in mallard ducks. Proceedings <strong>of</strong> the New Zealand<br />

Plant Protection Conference 53, 293-298.<br />

Keywords: non-target species/birds/pathology/persistence in<br />

animals/1080/poisoning/blood/cardiac/serum/citrate/inhibition/Krebs cycle/enzyme/muscle/sublethal<br />

effects<br />

Abstract: Public concern over inadvertent kills <strong>of</strong> native birds following largescale aerial poisoning<br />

operations for possum has highlighted deficiencies in information concerning the effects <strong>of</strong> 1080 on<br />

nontarget species. In this study biochemical and histopathological changes were measured in adult male<br />

mallard ducks (Anas playtrynchos) dosed orally with 1080. The toxin was quickly absorbed into the blood<br />

and distributed to the cardiac tissue. The time taken to reach maximum 1080 concentrations in these tissues<br />

corresponded closely with the onset <strong>of</strong> clinical signs <strong>of</strong> toxicosis. Tissue and serum citrate accumulation is<br />

a direct result <strong>of</strong> 1080 induced inhibition <strong>of</strong> the Krebs Cycle enzyme aconitate hydratase.<br />

Histopathological lesions indicated that skeletal muscle was a target organ for 1080 induced damage in<br />

birds. Dose dependent increases in serum ceratinine kinase (CK) and aspartate aminotransferase (AST)<br />

were consistent with extensive muscle necrosis. Skeletal muscle may be a unique avian specific target<br />

organ for 1080.<br />

Atzert, S. P. (1971). A review <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound 1080) : its properties, toxicology,<br />

and use in predator and rodent control. (United States Department <strong>of</strong> the Interior.Bureau <strong>of</strong> Sport Fisheries<br />

and Wildlife: Washington,DC.)<br />

Keywords: product chemistry/acute toxicity/field efficacy/metabolism/mode <strong>of</strong><br />

action/diagnosis/treatment/persistence in plants/persistence in soil/secondary poisoning/non-target<br />

species/pathology/1080/pigs<br />

Abstract: The purpose <strong>of</strong> this monograph is to summarize current information on sodium<br />

mon<strong>of</strong>luoroacetate, to review use patterns, and to provide a base for further studies.<br />

Au, K. G. and Walsh, C. T (1984). Stereochemical studies on a plasmid-encoded fluoroacetate<br />

halidohyrolase. Bioorganic Chemistry 12, 197-205.<br />

Keywords: fluoroacetate/analysis/NMR/bacteria/degradation/enzyme<br />

Abstract: The stereochemical course <strong>of</strong> action <strong>of</strong> haloacetate halidohydrolase H-1 from Pseudomonas sp.,<br />

strain A, which catalyses the dehalogenation <strong>of</strong> fluoroacetate to glycolate, has been determined by<br />

enzymatic analysis <strong>of</strong> products from incubations with both enantiomers and 2-fluoroproprionate and by 1H<br />

NMR analysis <strong>of</strong> the ester <strong>of</strong> (-)-alpha-methoxy-alpha(trifluoromethyl)phenylacetic acid with phenacyl<br />

glycolate derived from the product <strong>of</strong> incubation with the (s)-monodeuter<strong>of</strong>luoroacetate.<br />

9


1080 Reassessment Application October 2006<br />

Appendix C<br />

Aulerich, R. J., Ringer, R. K., and Safron<strong>of</strong>f, J. (1987). Primary and secondary toxicity <strong>of</strong> warfarin, sodium<br />

mon<strong>of</strong>luoroacetate. and methyl parathion in mink. Archives <strong>of</strong> environmental contamination and toxicology<br />

16, 357-366.<br />

Keywords: acute toxicity/secondary poisoning/mammals/non-target species/sodium mon<strong>of</strong>luoroacetate<br />

Abstract: The primary and secondary toxicity <strong>of</strong> warfarin, sodium mon<strong>of</strong>luoroacetate (Compound 1080),<br />

and methyl parathion were assessed in the mink, a representative surrogate mammalian wildlife carnivore.<br />

In a 28-day test, a LC50 value for mink fed warfarin per se (primary toxicity) was calculated to be 11.7<br />

ppm (mg/kg) with a 95% confidence interval <strong>of</strong> 9.2 to 15.0 ppm (mg/kg) and a slope <strong>of</strong> 2.03. Feeding mink<br />

warfarin-contaminated rabbit (minus digestive tract contents) incorporated into diets to provide warfarin<br />

residue levels equivalent to the warfarin concentrations fed in the LC50 primary toxicity test did not<br />

produce secondary toxicity, suggesting that warfarin may be readily bound and/or metabolized into non-, or<br />

less toxic metabolites by the primary consumer. Toxic residues <strong>of</strong> 1080 for mink (as in secondary toxicity)<br />

were not produced in rabbits fed a lethal dose <strong>of</strong> this compound when the gastrointestinal tract contents<br />

were removed from the rabbit carcasses. These results suggested that reports <strong>of</strong> secondary toxicity from<br />

1080 may be primarily due to consumption <strong>of</strong> the unmetabolized compound from the gut <strong>of</strong> the prey<br />

species.<br />

Bachelard, H. (1998). Landmarks in the application <strong>of</strong> C 13 magnetic resonance spectroscopy to studies <strong>of</strong><br />

neuronal/glial relationships. Developmental neuroscience 20, 277-288.<br />

Keywords: mode <strong>of</strong> action/NMR/metabolism<br />

Backholer, J. R. Reference Information on the toxicity <strong>of</strong> Sodium Mon<strong>of</strong>luoroacetate (Compound 1080).<br />

1980. Victoria, Vermin and Noxoius Weeds Destruction Board, Department <strong>of</strong> Crown Lands and Survey.<br />

Ref Type: Pamphlet<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080<br />

Bacq, Z. M., Fischer, P., Herve, A., Liebecq, C., and Liebecq-Hutter, S. (1958). Sodium fluoroacetate as a<br />

protecting agent against irradation. Nature 182, 175-176.<br />

Keywords: sodium fluoroacetate/fluoroacetate/mode <strong>of</strong> action<br />

Bacq, Z. M. and Liebecq-Hutter, S. (1960). Protection against irradiation afforded by sodium fluoroacetate.<br />

Radiation <strong>Research</strong> 13, 286-297.<br />

Keywords: sodium fluoroacetate/fluoroacetate/citric acid/metabolism/liver/rats/citrate/rodents<br />

Abstract: Sodium fluoroacetate injected into mice at a dose <strong>of</strong> 4 to 5 mg/kg, 5 hours before irradiation,<br />

reduced the mortality produced by 650 to 675 r <strong>of</strong> whole-body X-irradiation. The high levels <strong>of</strong> citric acid<br />

in the tissues <strong>of</strong> the poisoned animals returned to normal within 24 hours if 675 r <strong>of</strong> X-rays were given 5<br />

hours after 5 mg/kg <strong>of</strong> sodium fluoroacetate, whereas 48 hours were required in the case on non-irradiated<br />

control mice. Thus, X-rays interfered with the metabolism <strong>of</strong> citric acid in the tissues <strong>of</strong> the mouse as in the<br />

tissues <strong>of</strong> the rat. The liver <strong>of</strong> the mouse, however, did not behave like the liver <strong>of</strong> the rat. In contrast to<br />

rats, male mice injected with sodium fluoroacetate accumulated citrate in their livers, whereas females did<br />

not; whole-body irradiation reduced the level <strong>of</strong> accumulated citrate in the liver as it did in tissues <strong>of</strong> the<br />

mouse. The injection <strong>of</strong> sodium fluoroacetate produced a prolonged hypothermia. It is suggested that the<br />

fluoroacetate-induced accumualtion <strong>of</strong> citrate protects the animals by complexing magnesium ions<br />

necessary for DNase activity.<br />

Balcomb, R., Bowen, C. A., and Williamson, H. O. (1983). Acute and sublethal effects <strong>of</strong> 1080 on<br />

starlings. Bulletin <strong>of</strong> environmental contamination and toxicology 31, 692-698.<br />

Keywords: 1080/sodium mon<strong>of</strong>luoroacetate/birds/reproductive effects/testes/sublethal effects<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (Compound 1080) is highly toxic to mammals and has been used<br />

widely for control <strong>of</strong> rodents and mammalian predators. In 1972 many uses <strong>of</strong> 1080 were cancelled, due, in<br />

part to mortalities that were reported among non-target animals. Though 1080 baits and dead poisoned<br />

animals may be available to birds during avain breeding periods we are unaware <strong>of</strong> any investigation <strong>of</strong><br />

long-term exposure in birds or possible effects on avian reproduction. Such studies are <strong>of</strong> particular interest<br />

as testing with rats has shown testicular lesions and atrophy resulting from sublethal 1080 exposure. Our<br />

study was undertaken to investigate the short-term acute and long-term sublethal effects <strong>of</strong> 1080 on<br />

European starlings (Sturnus vulgaris) with emphasis on testicular morphology. Starlings fed 1080 showed<br />

10


1080 Reassessment Application October 2006<br />

Appendix C<br />

roughly 14% less testis weight development than controls but the difference was not statistically<br />

significant. This result suggests a substantial difference in the sensitivity between birds and mammals as<br />

testing with rats at a lower dosage for a shorter period resulted in significant reductions in testes weights<br />

and pronounced morphological lesions.<br />

Ballard, C. L. and Hyde, P. M (1967). Effect <strong>of</strong> insulin on blood glucose and corticosteroid levels in<br />

sodium fluoroacetate induced diabetes. Proceedings <strong>of</strong> the Society for Experimental Biology and Medicine<br />

124, 317-320.<br />

Keywords: blood/sodium fluoroacetate/fluoroacetate/metabolism<br />

Abstract: Sodium fluoroacetate (SFA) has been shown to produce hyperglycemia and ketonemia in the rat.<br />

Although this SFA-induced diabetes has been described as being partially insensitive to insulin by Engel et<br />

al., a significant insulin effect has been demonstrated. Karam and Grodskey reported that greater than<br />

normal amounts <strong>of</strong> insulin were present in the pancreatic tissue <strong>of</strong> the SFA-treated animal. The present<br />

study was designed to investigate the effect <strong>of</strong> exogenous insulin in reducing blood glucose levels in<br />

control and SFA-induced hyperglycemic rats. In addition, the effects <strong>of</strong> SFA and insulin on the levels <strong>of</strong><br />

circulating corticosteroid were determined. The hyperglycemia produced by SFA can be significantly<br />

reduced by small amounts <strong>of</strong> insulin. The very levels <strong>of</strong> plasma corticosteroid found to occur following<br />

treatment with SFA can be transiently increased by the administration <strong>of</strong> insulin. These high levels are<br />

thought to be due to a SFA induced decrease in the hepatic inactivation <strong>of</strong> the adrenal hormone.<br />

Bamford, J. (1970). Evaluating opossum poisoning operations by interference with non-toxic bait.<br />

Proceedings <strong>of</strong> the New Zealand Ecological Society 17, 118-125.<br />

Keywords: poisoning<br />

Abstract: From eight trials made during 1967-69 a technique was developed for estimating the reduction,<br />

by poisoning, <strong>of</strong> opossums (Trichosurus vulpecula) from the extent <strong>of</strong> interference with non-toxic flourpaste<br />

baits. The model assumes that opossums do not, through experience and learning, search for other<br />

baits close by.<br />

The trial data showed that contagion, an increase in levels <strong>of</strong> bait interference from night to night and very<br />

high acceptance levels were a consequence <strong>of</strong> baits having been preferentially placed on open ridges and<br />

spaced too closely.<br />

Manipulation <strong>of</strong> baits on randomly-located lines showed that if baits were spaced 40 yards apart and lines<br />

were at least 200 yards apart there was little evidence <strong>of</strong> contagion.<br />

Procedures are given for using interference levels from poisoned areas and untreated control areas to<br />

estimate kills.<br />

Banat, I. M., Lindstrom, E. B., Nedwell, D. B., and Balba, M. T. (1981). Evidence for coexistence <strong>of</strong> two<br />

distinct functional groups <strong>of</strong> sulfate-reducing bacteria in salt marsh sediment. Applied and environmental<br />

microbiology 42, 985-992.<br />

Keywords: bacteria/acetate/fluoroacetate/metabolism/inhibition/toxicity<br />

Abstract: Oxidation <strong>of</strong> acetate in salt marsh sediment was inhibited by the addition <strong>of</strong> fluoroacetate, and<br />

also by the addition <strong>of</strong> molybdate, an inhibitor <strong>of</strong> sulfate-reducing bacteria. Molybdate had no effect upon<br />

the metabolism <strong>of</strong> acetate in a freshwater sediment in the absence <strong>of</strong> sulfate. The inhibitory effect <strong>of</strong><br />

molybdate on acetate turnover in the marine sediment was attributed to inhibition <strong>of</strong> sulfate-reducing<br />

bacteria which oxidized acetate to carbon dioxide. Sulfide was not recovered from sediment in the presence<br />

<strong>of</strong> molybdate, but sulfide was recovered quantitatively even in the presence <strong>of</strong> molybdate by the addition <strong>of</strong><br />

the strong reducing agent titanium chloride before acidification <strong>of</strong> the sediment. Reduction <strong>of</strong> sulfate to<br />

sulfide by the sulfate-reducing bacteria in the sediment was only partially inhibited by fluoroacetate, but<br />

was completely inhibited by molybdate addition. This was interpreted as showing the presence <strong>of</strong> two<br />

functional groups <strong>of</strong> sulfate-reducing bacteria - one group oxidizing acetate, and another group probably<br />

oxidizing hydrogen<br />

Barasa, A., Godina, G., Buffa, P., and Pasquali-Rochetti, I. (1973). Biochemical lesions <strong>of</strong> respiratory<br />

enzymes and configurational changes <strong>of</strong> mitochondria in vivo. I. The effect <strong>of</strong> fluoroacetate: a study by<br />

phase-contrast microscopy and time-lapse cinemicrography. Zeitschrift fuer Zellforschung und<br />

Mikroskopische Anatomie 138, 187-210.<br />

Keywords: mode <strong>of</strong> action/pathology/biochemistry/heart/fluoroacetate/inhibition<br />

11


1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Chick embro heart fragments in primary hangingdrop culture were treated with sodium<br />

fluroacetate to induce inhibition <strong>of</strong> aconitate hydratase, a mitochondrial enzyme <strong>of</strong> the tricarboxylic acid<br />

cycle. The mitochondria were analyzed in the living myoblasts by phasecontrast timelapse<br />

cinemicrography. The results were recorded in 1 16 mm film. After 2030 minutes contact <strong>of</strong> the cells with<br />

the inhibitor some mitochondrion became thickened and swollen. The swelling was polymorphous,<br />

asynchronous and reversible; the name mitochondrion could swell and shrink many times. Some<br />

mitochondria seemed not to respond to fluroacetate and remained rodlike. Mitochondria appeared the only<br />

cell components to be morphologically affected by fluroacetate and the changes were specifically caused by<br />

the inhibitor. The type <strong>of</strong> mitochondrial swelling differed from the largeamplitude inspirationdependent<br />

swelling <strong>of</strong> the isolated mitochondria in vitro and from the configurational changes <strong>of</strong> isolated<br />

mitochondria associated with the respiratory states. The evidence pointed to specific connection between<br />

the biochemical lesion caused by fluroacetate and the configurational changes <strong>of</strong> the mitochondria. The<br />

mitochondrial swelling as to a large extent revered by washing the cultures with Tyrode physiological<br />

saline solution and the reversal was further accentuated by incubation <strong>of</strong> the cultures in fresh nutrient<br />

medium.<br />

Barnett, M. L. J., Batcheler, C. L., and Lambert, R. E. Investigations into the use <strong>of</strong> natural baits and<br />

compound 1080 for poisoning deer. 75, 1-12. 1970. Rangiora, Forest & Range Experiment Station.<br />

Protection Forestry Branch Report No. 75.<br />

Ref Type: Report<br />

Keywords: baits/1080/poisoning/deer<br />

Abstract: Poisoning <strong>of</strong> natural baits with 1080 powder dissolved in an adhesive is effective for killing deer<br />

in an area <strong>of</strong> high rainfall and dense vegetation, where conventional methods <strong>of</strong> control have met with<br />

limited success in in recent years. Experiments showed that natural baits treated with the adhesive were<br />

fairly readily accepted by deer.<br />

Barnett, S. A. and Spencer, M. M. (1949). Sodium fluoroacetate (1080) as a rat poison. The Journal <strong>of</strong><br />

Hygiene 47, 426-430.<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080/poisoning/rats/birds/<strong>poisons</strong>/efficacy<br />

Abstract: Sodium fluoroacetate (1080) has been tested in the field as a poison for Rattus norvegicus and R.<br />

rattus. Direct poisoning (without prebaiting) was used in thirteen tests on R. norvegicus. In eight <strong>of</strong> these<br />

tests censuses showed kills <strong>of</strong> at least 89%; in three tests the poison failed, and in two the results were<br />

equivocal. Of three similar tests against R. rattus two were successful and one was a failure. Six tests <strong>of</strong><br />

1080 after prebaiting gave five successes (including one against R. rattus) and one in which the estimated<br />

kill was about 82%. In five out <strong>of</strong> six tests populations <strong>of</strong> R. norvegicus which had survived baiting with<br />

1080 showed shyness (refusal) <strong>of</strong> the poison when it was given in a new bait base. The LD50 <strong>of</strong> 1080 for a<br />

strain <strong>of</strong> white rats was found to be 3.8 mg/kg (approx. range 2.8-5.2). A number <strong>of</strong> wild birds and some<br />

domestic aniamls were accidentally killed during the tests despite stringent precautions taken in laying the<br />

bait and in warning occupiers. It is concluded that (a) although 1080 is probably more effective in direct<br />

poisoning than other <strong>poisons</strong> used in the past, it does not give as consistent results as the standard <strong>poisons</strong><br />

do after prebaiting; (b) 1080 is too dangerous for general use.<br />

Baron, M. L., Bothroyd, C. M., Rogers, G. I., Staffa, A., and Rae, I. D. (1987). Detection and measurement<br />

<strong>of</strong> fluoroacetate in plant extracts by 19 F NMR. Phytochemistry 26, 2293-2295.<br />

Keywords: NMR<br />

Abstract: Examination <strong>of</strong> extracts from seeds and foliage <strong>of</strong> several species known to contain fluoroacetate,<br />

using 19FNMR spectroscopu, has shown the presence <strong>of</strong> the characteristic FCH2-signal in most <strong>of</strong> them<br />

and enabled quantitative determiniation <strong>of</strong> their fluoroacetate contect. No other fluorine-containing plant<br />

metabolites were detected; fluoroacetate was not detected in the extracts <strong>of</strong> several non-toxic species. The<br />

limit <strong>of</strong> detection is estimated to be ca 4 Fg/g.<br />

Barry, T. N., Blaney, B. J., Hacker, J. B., and Ternouth, J. H. (1987). Secondary compounds <strong>of</strong> forages.<br />

(Academic Press; London; UK:<br />

Keywords: chemistry/cyanide/fluoroacetate/occurrence in nature<br />

Abstract: This review is divided into sections each dealing with representatives <strong>of</strong> a separate group <strong>of</strong><br />

compounds. Within each section, sub-sections describe the chemistry <strong>of</strong> the compound(s), factors affecting<br />

12


1080 Reassessment Application October 2006<br />

Appendix C<br />

their concentration in plants, and the effect <strong>of</strong> the secondary compound(s) upon animals and upon forage<br />

nutritive value. Secondary compounds may be either toxic to animals (e.g. cyanide, nitrate and<br />

fluoroacetate), cause sub-clinical losses in productivity, (e.g. some mycotoxins and high concentrations <strong>of</strong><br />

condensed tannins), increase nutritive value (e.g. low concentrations <strong>of</strong> condensed tannins), reduce mineral<br />

availability (e.g. oxalate) or improve plant persistency (e.g. peramine). The important groups <strong>of</strong> secondary<br />

compounds are listed in a table, together with appropriate references<br />

Bartlett, G. R. and Barron, E. S. G. (1947). The effect <strong>of</strong> fluoroacetate on enzymes and on tissue<br />

metabolism. Journal <strong>of</strong> biological chemistry 170, 67.<br />

Keywords: fluoroacetate/enzyme/metabolism<br />

Baselt, R. C. (2000). Fluoroacetate. In 'Disposition <strong>of</strong> toxic drugs and chemicals in man. 5th ed'. (Ed. R. C.<br />

Baselt.) pp. 365-367. (Chemical Toxicology Institute: Foster City.)<br />

Keywords: metabolism/acute toxicity/mode <strong>of</strong> action/liquid chromatography/fluoroacetate<br />

Basson, P. A., Norval, A. G., H<strong>of</strong>meyr, J. M., Ebedes, H., and Schultz, R. A. (1982). Antelope and<br />

poisonous plants: 1. Gifblaar Dichapetalum cymosum containing mon<strong>of</strong>luoroacetate. Madoqua 13, 59-70.<br />

Keywords: mon<strong>of</strong>luoroacetate/goats/stomach/poisoning/liver/lethal dose/pathology/heart<br />

Abstract: Ten tame eland (Taurotragus oryx), 4 kudu (Tragelaphus strepsiceros), 2 gemsbok (Oryx gazella),<br />

6 springbok (Antidorcas marsupialis) and 33 domestic goats were drenched by stomach tube with extracts<br />

<strong>of</strong> the poisonous plant gifblaar (Dichapetalum cymosum) (Hooker) Engler and Prantl (= D. venenatum<br />

Engler and Gilg). Semi-quantitative analyses <strong>of</strong> the mon<strong>of</strong>luoroacetate (MFA) content <strong>of</strong> the leaves were<br />

conducted at regular intervals and the proven lethal (about LD-100) caprine dose was found to be<br />

equivalent to 1.01-1.60 mg/kg MFA. Eland and kudu only succumbed at high dosage levels <strong>of</strong> 6-8 mg/kg<br />

MFA and proved to be much less susceptible to gifblaar poisoning than goats. Springbok and gemsbok<br />

were as susceptible as goats, although confirmation is needed in gemsbok to eliminate possible interaction<br />

between the immobilizing drugs used and MFA. During separate voluntary intake trials, eland ate limited<br />

<strong>of</strong>ferings <strong>of</strong> both low and highly toxic stages <strong>of</strong> gifblaar. At these dosages they showed no ill effects. Kudu<br />

on the other hand were more cautious and intake was minimal. The lesions caused by gifblaar are<br />

described. A few macroscopic lesions observed in some <strong>of</strong> the animals have not been recorded previously.<br />

These include: edema and hemorrhages <strong>of</strong> the gall bladder with occasional blood-stained bile; edema <strong>of</strong> the<br />

abomasum, periportal area <strong>of</strong> the liver, pancreas and pulmonary valves; adrenal hemorrhages and petechiae<br />

in the urinary bladder. Histopathological changes were described in various organs such as the myocardium<br />

where replacement fibrosis became evident in animals which survived for 2 or more days<br />

Batcheler, C. L. Compound 1080, its properties, effectiveness, dangers, and use. Forest <strong>Research</strong> Institute.<br />

14-17. 1978. Wellington, New Zealand Forest Service.<br />

Ref Type: Report<br />

Keywords: 1080/aquatic species/fish<br />

Batcheler, C. L. (1982). Quantifying "bait quality" from number <strong>of</strong> random encounters required to kill a<br />

pest. New Zealand journal <strong>of</strong> ecology 5, 129-139.<br />

Keywords: possums/field efficacy/baits/carrot<br />

Batcheler, C. L. and Challies, C. N. (1988). Loss <strong>of</strong> compound 1080 (sodium mon<strong>of</strong>luoroacetate) from<br />

Carbopol gel smeared on foliage to poison deer. New Zealand journal <strong>of</strong> forestry science 18, 109-115.<br />

Keywords: 1080/bait degradation/baits/deer/mon<strong>of</strong>luoroacetate/poison/sodium mon<strong>of</strong>luoroacetate<br />

Abstract: Compound 1080 (sodium mon<strong>of</strong>luoroacetate) in a gel carrier was applied to the leaves <strong>of</strong><br />

broadleaf (Griselinia littoralis Raoul) baits (cuttings) to poison deer. In two trials on Stewart Island, (New<br />

Zealand) assays for F- showed that the poison disappeared during rain, 90% being lost in 207 mm <strong>of</strong> rain<br />

and 81 mm <strong>of</strong> rain in the respective trials. In one trial significant losses <strong>of</strong> Compound 1080 also resulted<br />

from biodegradation in storage. Baits set to kill deer were sampled after 0, 15, 30, and 45 days <strong>of</strong><br />

weathering. Only 10% <strong>of</strong> the treated leaves retained toxic gel after 45 days. About 1.4% <strong>of</strong> the Compound<br />

1080 was lost from the leaves per millimetre <strong>of</strong> rainfall. This rate was similar to loss rates for Compound<br />

1080 from other baits commonly used in animal control operations.<br />

13


1080 Reassessment Application October 2006<br />

Appendix C<br />

Bauermeister, A., Thompson, C. J., and Nimmo, I. A. (1977). The susceptibility <strong>of</strong> rainbow trout to<br />

fluoroacetate. Biochemical Society transactions 5, 304-306.<br />

Keywords: aquatic species/non-target species<br />

Abstract: Certain poikilothermic animals are resistant to fluoroacetate. Since no-one seems to know how<br />

they tolerate fluoroacetate, we have examined some <strong>of</strong> its effects on the Rainbow trout, and for comparsion,<br />

on the albino rat. Comparison <strong>of</strong> the LD50 values for fluoroacetate with the concentrations <strong>of</strong> it which<br />

inhibit hepatic respiration suggests that in neither species is the liver the critical organ. Nevertheless, it is<br />

tempting to speculate that trout are relatively immune to fluoroacetate, partly because their aconitrate<br />

hydratase is only poorly inhibited by fluorocitate, and partly because their low body temperature further<br />

diminishes the potency <strong>of</strong> this inhibitor.<br />

Beard, C. E., Hefford, M. A., Forster, R. J., Sontakke, S., Teather, R. M., and Gregg, K. (1995). A stable<br />

and efficient transformation system for Butyrivibrio fibrisolvens OB156. Current Microbiology 30, 105-<br />

109.<br />

Keywords: resistance<br />

Abstract: A 9.5-kb shuttle vector capable <strong>of</strong> replication and selection in both Esherichia coli and<br />

Butyrivibrio fibrisolvens was constructed. Plasmid pUC118 provided replication functions and ampicillin<br />

resistance selection in E. coli. In B. fibrisolvens, replication was controlled by the native plasmid pRJF1<br />

from strain OB156, and selectability was provided by a 3.5-kb fragment <strong>of</strong> plasmid pAMβ1 containing the<br />

erythromycin gene. Optimum conditions for transformation were 15 kV/cm, 2 hr recovery, and plating in<br />

an agar overlay on medium containing 10 µg erythromycin/ml. Maximum efficiency was 1.1 x 10 5<br />

transformants per µg plasmid DNA (average 3 x 10 4 ), and restriction mechanisms reduced efficiency by a<br />

factor <strong>of</strong> 2 x 10 2 . Nonselective growth for 200 generations gave no measurable loss <strong>of</strong> plasmid.<br />

Beasley, M. (1996). 1080 - overview <strong>of</strong> toxicology issues. In 'Improving conventional control <strong>of</strong> possums :<br />

proceedings <strong>of</strong> a workshop organised by the Possum and Bovine Tuberculosis <strong>Control</strong> National Science<br />

Strategy Committee, 25-26 October 1995, Wellington'. pp. 15-17. (<strong>Royal</strong> Society <strong>of</strong> New Zealand:<br />

Wellington.)<br />

Keywords: occupational exposure/1080/possums<br />

Abstract: This paper reviews the health issues concerning the continued use <strong>of</strong> 1080<br />

Beasley, V. R., Dorman, D. C., Fikes, J. D., Diana, S. G., and Woshner, V. (1997). Fluoroacetate - 1080. In<br />

'A systems affected approach to veterinary toxicology : reference notes for Toxicology VB 320'. pp. 98-<br />

102. (University <strong>of</strong> Illinois, Dept. <strong>of</strong> Veterinary Biosciences: Urbana.)<br />

Keywords: metabolism/acute toxicity/diagnosis/treatment/1080/pathology<br />

Abstract: Brief notes on the sources, mechanism, toxicity, signs, clinical pathology, lesions, diagnosis and<br />

treatment.<br />

Beggs, J. R., T<strong>of</strong>t, R. J., Malham, J. P., Rees, J. S., Tilley, J. A. V., Moller, H., and Alspach, P. (1998). The<br />

difficulty <strong>of</strong> reducing introduced wasp (Vespula vulgaris) populations for conservation gains. New Zealand<br />

journal <strong>of</strong> ecology 22, 55-63.<br />

Keywords: birds/invertebrates/wasps/<strong>poisons</strong>/poison/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/poisoning<br />

Abstract: Vespula vulgaris are widespread, abundant pests in New Zealand. They compete for food with<br />

native birds and feed on native invertebrates. The authors poisoned wasps annually over 4 years (1991-95)<br />

to see if it was possible to reduce their abundance in two 30-ha beech (Noth<strong>of</strong>agus) forest sites near Lake<br />

Rotoroa. Two different <strong>poisons</strong> (sodium mon<strong>of</strong>luoroacetate [sodium fluoroacetate] and sulfluramid) were<br />

used, mixed with sardine cat food. There was no evidence that one poison was more effective than the<br />

other. Between 82 and 100% <strong>of</strong> the colonies were killed in the poisoned sites, but reinvasion by foraging<br />

workers meant that cumulative wasp biomass (measured using Malaise traps) was reduced by only 55-70%.<br />

Individual wasps were about 16% heavier in the poisoned sites at the peak <strong>of</strong> the wasp season (March) than<br />

in the non-poisoned sites, although this had a minimal effect on cumulative biomass over the entire season.<br />

Conservation gains need to be quantified in order to assess whether the expense <strong>of</strong> such poisoning<br />

operations is warranted<br />

14


1080 Reassessment Application October 2006<br />

Appendix C<br />

Belcher, C. A. (1998). Susceptibility <strong>of</strong> the tiger quoll, Dasyurus maculatus, and the eastern quoll, D.<br />

viverrinus, to 1080-poisoned baits in control programmes for vertebrate pests in eastern Australia. Wildlife<br />

research 25, 33-40.<br />

Keywords: baits/marsupials/non-target species<br />

Bell, A. T., Newton, L. G., Everist, S. L., and Legg, J. (1955). Acacia georginae poisoning <strong>of</strong> cattle and<br />

sheep. The Australian Veterinary Journal 249-257.<br />

Keywords: poisoning/occurrence in nature/livestock<br />

Bell, J. (1972). The acute toxicity <strong>of</strong> four common <strong>poisons</strong> to the opossum Trichosurus vulpecula. New<br />

Zealand veterinary journal 20, 213-214.<br />

Keywords: acute toxicity/strychnine/rabbits/secondary poisoning/cyanide/arsenic<br />

Abstract: Although a number <strong>of</strong> <strong>poisons</strong> are used for the destruction <strong>of</strong> opossums, Trichosurus vulpecula<br />

(Kerr), very little information on their acute toxic effects is available. A study <strong>of</strong> the toxicity <strong>of</strong> four<br />

<strong>poisons</strong> was therefore undertaken. Two <strong>of</strong> these compounds, sodium mon<strong>of</strong>luoroacetate and sodium<br />

cyanide, are used as toxins against opossums in New Zealand, and others, arsenic trioxide and strychnine<br />

alkaloid, are used for the destruction <strong>of</strong> rabbits. Arsenic trioxide and strychnine were suggested as<br />

replacements for sodium mon<strong>of</strong>luoroacetate and sodium mon<strong>of</strong>luoroacetate and sodium cyanide by the<br />

Rabbit Destruction Council (pers. comm.). They suggested strychnine as a substitute for cyanide to<br />

overcome poison shyness and arsenic as a substitute for sodium mon<strong>of</strong>luoroacetate to circumvent the<br />

danger <strong>of</strong> secondary poisoning to farmers dogs.<br />

The investigation determined the oral toxicity <strong>of</strong> these <strong>poisons</strong> and comments on the suitability <strong>of</strong> arsenic<br />

trioxide and strychnine as substitutes.<br />

Benitez, D., Pscheidt, G. R., and Stone, W. E. (1954). Formation <strong>of</strong> ammonium ion in the cerebrum in<br />

fluoroacetate poisoning. American journal <strong>of</strong> physiology 176, 488-492.<br />

Keywords: mode <strong>of</strong> action/pathology<br />

Abstract: A study was made <strong>of</strong> the ammonium ion and glutamine in the cerbrum during the course <strong>of</strong><br />

fluoracetate poisoning in dogs.<br />

Bennett, L. W., Miller, G. W., Yu, M. H., and Lynn, R. I. (1983). Production <strong>of</strong> fluoroacetate by callus<br />

tissue from leaves <strong>of</strong> Acacia georginae. Fluoride 16, 111-117.<br />

Keywords: fluoroacetate/fluoride/inhibition/occurrence in nature/persistence in plants<br />

Abstract: Callus cultures <strong>of</strong> A. georginae were initiated from leaf discs from young leaves. Growth <strong>of</strong> callus<br />

was slow but predictable with tissue volume up to 2.2 cm-3 being formed. Fluoride concentrations up to 80<br />

ppm in the medium produced no adverse effect on callus growth. Reversible growth inhibition occurred at<br />

160 ppm; apparent death occurred at higher concentrations. Fluoroacetate was detected by gas<br />

chroamtography in the callus treated with 40, 80 and 160 ppm fluoride<br />

Bentley, E. W., Alabaster, J. S., and Taylor, E. J. (1958). The use <strong>of</strong> sodium fluoroacetate against rats living<br />

in sewers discharging into natural waters. Sanitarian London 1966.<br />

Keywords: aquatic species/fish/toxicity/1080<br />

Bentley, E. W., Hammond, L. E., Bathard, A. H., and Greaves, J. H. (1961). Sodium fluoroacetate and<br />

fluoroacetamide as 'direct' <strong>poisons</strong> for the control <strong>of</strong> rats in sewers. Journal <strong>of</strong> Hygiene, Cambridge 59,<br />

413-417.<br />

Keywords: sodium fluoroacetate/fluoroacetate/fluoroacetamide/<strong>poisons</strong>/rats/zinc<br />

phosphide/poisoning/efficacy/treatment<br />

Abstract: Field trials suggest that 3-monthly operations against rats in sewers using either 0.25% sodium<br />

fluoroacetate or 2% fluroacetamide as a direct poison are more effective than 6-monthly treatments with<br />

2.5% zinc phosphide or 10% arsenious oxide using the pre-baiting method. In six paired trials 2%<br />

fluoroacetamide gave better results (an apparent 100% clearance in 5 instances) than 0.25% sodium<br />

fluoroacetate. There is no evidence, at present, that direct poisoning treatments with 2% fluoroacetamide or<br />

0.25% sodium fluoroacetate are improved by the addition <strong>of</strong> mould inhibiting substances to the bait.<br />

15


1080 Reassessment Application October 2006<br />

Appendix C<br />

Berends, A. G., Keetelaar-Jansen, W. A. J., and Van Dijk, N. R. M. A comparison <strong>of</strong> the toxicity <strong>of</strong> sodium<br />

trifluoroacetate, sodium mon<strong>of</strong>luoroacetate and sodium fluoride to the alga Scenedesmus subspicatus .<br />

56835/61/94. 1994. Washington DC USA, AFEAS. Alternative Fluorocarbons Environmental<br />

Acceptability Study Final Report.<br />

Ref Type: Report<br />

Keywords: algae/toxicity/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/fluoride<br />

Berends, A. G., Boutonnet, J. C., de Rooij, C. G., and Thompson, R. S. (1999). Toxicity <strong>of</strong> trifluoroacetate<br />

to aquatic organisms. Environmental toxicology and chemistry 18, 1053-1059.<br />

Keywords: mode <strong>of</strong> action/metabolism/aquatic species/acute toxicity/algae<br />

Berg-Johnsen, J, Paulsen, R. E., Fonnum, F., and Langmoen, L. A. (1993). Changes in evoked potentials<br />

and amino acid content during fluorocitrate action studied in rat hippocampal cortex. Experimental brain<br />

research 96, 241-246.<br />

Keywords: mode <strong>of</strong> action<br />

Abstract: Fluorocitrate inhibits the glial tricarboxylic acid cycle and thereby the synthesis <strong>of</strong> glutamine,<br />

which is the main precursor for transmitter glutamate. We investigated the possibility that there is a<br />

functional correlate to fluorocitrate action by recording evoked field potentials in rat hippocampal slices.<br />

The excitatory postsynaptic potential (field-EPSP) was markedly depressed after 7-8 h <strong>of</strong> fluorocitrate<br />

action. The population spike was also reduced, but a major part <strong>of</strong> the reduction may be the result <strong>of</strong><br />

weaker synaptic activation rather than reduced excitability <strong>of</strong> the postsynaptic cells. The activity <strong>of</strong> thin<br />

unmyelinated fibres was only slightly affected. Preceding the changes in the field-EPSP there was a<br />

decrease in the glutamine content in the fluorocitrate treated slices relative to controls. Only a small<br />

decrease in tissue glutamate was seen concomitantly with the synaptic failure, probably because the<br />

transmitter pool <strong>of</strong> glutamate in those fibres stimulated makes little contribution to the total tissue<br />

glutamate.<br />

Bergmann, F. and Shimoni, A. (1953). The enzymic hydrolysis <strong>of</strong> alkyl fluoroacetates and related<br />

compounds. Biochemical journal 55, 50-57.<br />

Keywords: product chemistry<br />

Bester, M. N., Bloomer, J. P., Bartlett, P. A., Muller, D. D., van Rooyen, M., and Buchner, H. (2000). Final<br />

eradication <strong>of</strong> feral cats from sub-Antarctic Marion Island, southern Indian Ocean. South African Journal <strong>of</strong><br />

Wildlife <strong>Research</strong> 30, 53-57.<br />

Keywords: cats/poisoning/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/field efficacy<br />

Abstract: The last stages <strong>of</strong> the eradication <strong>of</strong> feral domestic cats Felis catus from sub-Antarctic Marion<br />

Island are described. After four seasons <strong>of</strong> hunting, intensive gin-trapping from 1990 and poisoning with<br />

sodium mon<strong>of</strong>luoroacetate from 1991 were incorporated into the eradication campaign. Hunting became<br />

totally ineffective at low densities, while trapping became more effective. Poisoning was added to rid the<br />

island <strong>of</strong> any remaining cats. The last live cat was sighted and shot in January 1991, while the last cat<br />

trapped in July 1991. No sign <strong>of</strong> cats has been seen on the island in the subsequent eight years, and it is<br />

stated with complete confidence that feral house cats have finally been eradicated from Marion Island.<br />

Beveridge, A. E., Smale, M. C., and Holzapfel, A. S. Ecology and management <strong>of</strong> Pureora Forest Park.<br />

Conservation Science Advisory Notes 282. 2000. Wellington, Department <strong>of</strong> Conservation.<br />

Ref Type: Report<br />

Bieleski, R. (2002). The 1080 Plant. New Zealand Garden Journal 5, 2-3.<br />

Keywords: 1080/occurrence in nature<br />

Abstract: At the moment, there is a lot <strong>of</strong> interest and a fiery debate about the use <strong>of</strong> 1080 in controlling<br />

possums. Interestingly, there are environmentalists on both sides <strong>of</strong> the debate. The 'antis' argue that 1080<br />

<strong>poisons</strong> our environment, while the 'pros' argue that its use greatly reduces possum damage, and allows<br />

recovery <strong>of</strong> our native vegetation from the drastic effects <strong>of</strong> introduced animals. Unfortunately, the debate<br />

is being muddled by claims that are not based on any concrete evidence or even contradicted by wellestablished<br />

knowledge. Perhaps the biggest confusion relates to the nature and use <strong>of</strong> the bait (the stuff the<br />

poison is carried in) versus the nature <strong>of</strong> the poison itself. Many <strong>of</strong> the concerns about use <strong>of</strong> 1080 are<br />

16


1080 Reassessment Application October 2006<br />

Appendix C<br />

essentially about the form <strong>of</strong> the bait and the way that the bait is distributed, so that other <strong>poisons</strong> used in<br />

the same ways would present the same problems. Largely neglected in the public debate is the nature <strong>of</strong> the<br />

poison itself, particularly in relation to its status as a natural plant product, rather than being some unnatural<br />

creation <strong>of</strong> unethical chemists.<br />

Blake, P. G. and Tomlinson, A. D. (1971). Thermal decomposition <strong>of</strong> fluoroacetic acid. Journal <strong>of</strong> the<br />

Chemical Society (B) 1596-1597.<br />

Keywords: bait degradation/chemistry/temperature<br />

Abstract: Thermal decomposition <strong>of</strong> gaseous fluoroacetic acid in silica at 295 - 283° C gives carbon<br />

monoxide, formaldehyde carbon dioxide, silicon tetrafluoride and fluoroacetyl fluoride as main products.<br />

Elimination <strong>of</strong> hydrogen fluoride appears to be the initial step in decomposition, followed mainly by<br />

formation <strong>of</strong> formaldehyde and carbon monoxide.<br />

Blok, J. (1975). Methods for measurement <strong>of</strong> biodegradability <strong>of</strong> chemical compounds. Int.Biodetn.Bull.<br />

11, 78-84.<br />

Abstract: This survey aims at promoting the standardization <strong>of</strong> methods for determing biodegradability.<br />

The most important problems met in biodegradation research concern adaptation, toxicity, non-biotic<br />

eliminations and analytical restrictions. Consequent rules and recommendations can be devided into two<br />

groups, viz one group aiming at adaptation and another group at obtaining reliable measurements. From a<br />

classification <strong>of</strong> frequently used methods it appears that there are only two clearly different groups <strong>of</strong><br />

methods which show a great many small differences. Adjustment <strong>of</strong> well known methods to the proposed<br />

rules and recommendations calls for an adaption procedure followed by a procedure for measurements.<br />

Blomquist, G. J., Halarnkar, P. P., and Dwyer, L. A. (1985). Proprionate and methyl malonate metabolism<br />

in insects. In 'Bioregulators for pest control'. (Ed. P. A. Hedin.) pp. 245-253. (American Chemical Society:<br />

Washington DC USA.)<br />

Keywords: metabolism/invertebrates/fluoroacetate/biosynthesis<br />

Abstract: <strong>Source</strong>s <strong>of</strong> propionate and methylmalonate and their use as substrates for juvenile hormone and<br />

methyl branched hydrocarbon biosynthesis in insects are reviewed. An unusual pathway for propionate<br />

metabolism has been shown to occur in insects and it may be related to the absence or low levels <strong>of</strong> vitamin<br />

B12 found in many species. This pathway suggested the possibility that 2-fluoropropionate might be<br />

selectively metabolized in insects to the toxic 2-fluoroacetate. However, 2-fluoropropionate was not toxic<br />

to Musca domestica or Periplaneta americana, presumably because it was not metabolized to 2fluoroacetate<br />

rapidly enough. Nevertheless, it is suggested that exloitation <strong>of</strong> unique metabolic pathways in<br />

insects <strong>of</strong>fers the potential for novel control techniques.<br />

Boink, A. B. T. J., Wemer, J., Meulenbelt, J., Vaessen, H. A. M. G., and de Wildt, D. J. (1994). The<br />

mechanism <strong>of</strong> fluoride-induced hypocalcaemia. Human & Experimental Toxicology 13, 149-155.<br />

Keywords: fluoride/toxicity/humans/cardiac<br />

Abstract: 1. Fluoride intoxication leads to sudden cardiac death which has been assumed to result from the<br />

accompanying severe hypocalcaemia. The aim <strong>of</strong> this study has been to investigate the suggestion that<br />

fluorapatite formation rather than CaF2 precipitation is responsible for this low calcium.<br />

2. Measurements <strong>of</strong> free Ca 2+ and F - ion concentrations in HEPES buffered solutions containing F - , Ca 2+ ,<br />

and phosphate ions at different concentrations in the absence and presence <strong>of</strong> hydroxyapatite showed that<br />

the presence <strong>of</strong> hydroxyapatite enhanced the decrease <strong>of</strong> Ca 2+ and F - concentration.<br />

3. The ratio <strong>of</strong> Ca 2+ :F - clearance was 5:1 which is consistent with formation <strong>of</strong> fluorapatite. These results<br />

support the hypothesis that hydroxyapatite acts as a nucleation catalyst for fluorapatite formation and this<br />

process is responsible for the hypocalcaemia induced by fluoride intoxication.<br />

4. The proposed mechanism explains also the metabolic acidosis which is frequently seen in cases <strong>of</strong><br />

fluoride intoxication.<br />

Bong, C. L., Cole, A. L. J., Walker, J. R. L., and Peters, J. A. (1979). Effect <strong>of</strong> sodium fluoroacetate<br />

("Compound 1080") on the soil micr<strong>of</strong>lora. Soil biology and biochemistry 11, 13-18.<br />

Keywords: persistence in soil/sodium fluoroacetate/fluoroacetate/soil/aquatic species/algae/persistence in<br />

plants/fungus<br />

Abstract: A range <strong>of</strong> New Zealand soils, many contaminated by sodium fluoroacetate ("Compound 1080"<br />

17


1080 Reassessment Application October 2006<br />

Appendix C<br />

or NaFA) were examined for micro-organisms capable <strong>of</strong> defluorinating this animal poison. Species <strong>of</strong><br />

Pseudomonas and Fusarium capable <strong>of</strong> growth on NaFA were isolated whilst many other soil bacteria and<br />

fungi exhibited defluorinating activity when grown on an alternative organic C source. It was concluded<br />

that NaFA has a short biological half-life in the soils investigated.<br />

Some NaFA-contaminated soils also contained species <strong>of</strong> the algae Chlorella and Chlamydomonas which<br />

were unaffected by NaFA but growth <strong>of</strong> a duck weed, Spirodela oligorrhiza, was inhibited 73% in the<br />

presence <strong>of</strong> 5 µΜ−NaFA.<br />

Bong, C. L., Walker, J. R. L., and Peters, J. A. (1980). The effect <strong>of</strong> fluoroacetate ("Compound 1080") and<br />

fluoride upon duckweeds. New Zealand journal <strong>of</strong> science 23, 179-183.<br />

Keywords: persistence in plants/aquatic species/persistence in water/bioassay/fluoroacetate/fluoride<br />

Abstract: The toxic effects <strong>of</strong> fluoroacetate (Nafa) and fluoride (NaF) upon three different species <strong>of</strong><br />

duckweed have been compared. Duckweeds proved far more sensitive to Nafa than to NaF; the frond<br />

multiplication rate being halved by 0.5mM Nafa compared to 10mM NaF. The frond multiplication rate<br />

was proportional to the logarithm <strong>of</strong> the Nafa concentration, whereas it was linearly related to NaF<br />

concentration. Our results suggest that duckweeds could beused as a sensitive bioassay system, and their<br />

potential as an indicator <strong>of</strong> pollution <strong>of</strong> ponds and streams by Nafa is being investigated.<br />

Booth, L. H., Ogilvie, S. C., Wright, G. R., and Eason, C. T. (1997). Water quality monitoring after 1080<br />

pest control operations. Water and wastes in NZ 96, 22.<br />

Keywords: persistence in water/1080<br />

Abstract: The results suggested that significant or prolonged contamination after using 1080 for pest control<br />

is highly unlikely, if care is taken to avoid watercourses when aerially sowing 1080 bait.<br />

Booth, L. H., Ogilvie, S. C., Wright, G. R., and Eason, C. T. (1999). Degradation <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) and fluorocitrate in water. Bulletin <strong>of</strong> environmental contamination and<br />

toxicology 62, 34-39.<br />

Keywords: metabolism/persistence in water/1080/fluorocitrate<br />

Abstract: Using a method developed for the analysis <strong>of</strong> fluorocitrate in water, it is shown that fluorocitrate<br />

is product <strong>of</strong> 1080 degradation, but is rapidly degraded and due to its lower oral toxicity compared with<br />

1080, it is more important to monitor 1080 residues than fluorocitrate after a possum control operation<br />

using 1080 bait.<br />

Booth, L. H., Ogilvie, S. C., and Eason, C. T. (1999). Persistence <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080),<br />

pindone, cholecalciferol, and brodifacoum in possum baits under simulated rainfall. New Zealand journal<br />

<strong>of</strong> agricultural research 42, 107-112.<br />

Keywords: bait degradation/1080/brodifacoum/possums<br />

Booth, L. H. and Wickstrom, M. L. (1999). The toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) to Huberia<br />

striata, a New Zealand native ant. New Zealand journal <strong>of</strong> ecology 23, 161-165.<br />

Keywords: non-target species/invertebrates/persistence in animals/1080/secondary poisoning/birds<br />

Booth, L. H., Wright, G. R. G., Brown, L. E., Radford, C. D., and Eason, C. Dust and 1080 residue<br />

contamination after aerial sowing <strong>of</strong> 1080 baits for possum control. New Zealand Plant Protection 53, 446.<br />

2000.<br />

Ref Type: Abstract<br />

Keywords: 1080/baits<br />

Bosakowski, T. and Levin, T. T. (1986). Serum citrate as a peripheral indicator <strong>of</strong> fluoroacetate and<br />

fluorocitrate toxicity in rats and dogs. Toxicology and applied phamacology 85, 428-436.<br />

Keywords: non-target species/mammals/metabolism/lethal<br />

dose/fluoroacetate/fluorocitrate/citrate/heart/acute toxicity/blood<br />

Abstract: The utility <strong>of</strong> serum citrate as a peripheral indicator <strong>of</strong> toxicity was tested as a possible<br />

investigational probe for compounds which inhibit citrate metabolism. Fluoroacetate (FA) and its putative<br />

toxic metabolite, fluorocitrate (FC), were given to rats and dogs in a series <strong>of</strong> studies. In rats 3mg/kg FA<br />

18


1080 Reassessment Application October 2006<br />

Appendix C<br />

(po) caused a 46% depletion in heart ATP concentrations and a 15fold increase in heart citrate<br />

concentrations. Both <strong>of</strong> these changes were significantly correlated with a fivefold elevation in serum<br />

citrate elevations corresponded with the appearance <strong>of</strong> serious clinical signs and death. In range finding<br />

studies with rats or dogs, serum citrate elevations were always observed in a doserelated pattern according<br />

to the does <strong>of</strong> FA or FC administered. In contrast to FA toxic doses <strong>of</strong> FC did not reduce heart ATP in<br />

either rats <strong>of</strong> dogs and high correlations were established between serum glucose and serum citrate in both<br />

species. Serum total calcium was reduced (18%) in dogs treated with FC (8mg/kg, iv) and a strong inverse<br />

correlation to serum citrate was shown. This correlation is biologically meaningful in light <strong>of</strong> the known<br />

chelating effect <strong>of</strong> citrate on calcium. Clinical manifestations <strong>of</strong> tremors, tetany, and convulsions in FC<br />

treated dogs were consistent with know symptoms <strong>of</strong> hypocalcemia. No decrease in total calcium was<br />

observed in rats treated with either FA or FC. Despite certain species differences in response to the two<br />

inhibitors, serum citrate levels were always reflective <strong>of</strong> nontoxic, toxic or lethal doses.<br />

Bosakowski, T. and Levin, A. A. (1987). Comparative acute toxicity <strong>of</strong> chlorocitrate and fluorocitrate in<br />

dogs. Toxicology and Applied Pharmacology 89, 97-104.<br />

Keywords: non-target species/mammals/metabolism/acute toxicity/fluorocitrate/dogs<br />

Bourke, E., Frindt, G., Schreiner, G. E., and Preuss, H. G. (1979). Effects <strong>of</strong> fluorocitrate on renal<br />

ammoniagenesis and glutamine metabolism in the intact dog kidney. Kidney International 15, 255-263.<br />

Keywords: fluorocitrate/metabolism/kidney<br />

Abstract: Renal glutamine metabolism was studied in vivo following infusions <strong>of</strong> fluorocitrate into<br />

chronically acidotic and alkalotic dogs. Coincident with a dramatic rise in renal cortical citrate<br />

concentrations, there was a significant fall in tissue glutamate in both acid-base states. This was<br />

accompanied by a significnat increase in total renal ammonia production. Glutamine metabolism and<br />

ammoniagenesis in alkalotic dogs receiving fluorocitrate simulated that achieved in acidotic dogs. The<br />

simultaneous administration <strong>of</strong> α-ketoglutarate and fluorocitrate significantly diminished the fall in tissue<br />

glutamate and the rise in ammoniagenesis induced by fluorocitrate alone. These results are compatable<br />

with the hypothesis that ammonia production from glutamine is enhanced secondary to increased glutamate<br />

deamination. We postulate that this chain <strong>of</strong> events may be the consequence <strong>of</strong> impared α-ketoglutarate<br />

production from citrate.<br />

Bovis, R., Kasten, F. H., and Okigaki, T. (1966). Electron microscopic study <strong>of</strong> the toxic effect <strong>of</strong> the toxic<br />

effect <strong>of</strong> sodium fluoroacetate on rat myocardial cultures. Experimental cell research 43, 611-621.<br />

Keywords: pathology/mode <strong>of</strong> action/sodium fluoroacetate/fluoroacetate<br />

Bowen, L. H., Morgan, D. R., and Eason, C. T. (1995). Persistence <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) in<br />

baits under simulated rainfall. New Zealand journal <strong>of</strong> agricultural research 38, 529-531.<br />

Keywords: bait degradation/1080/persistence in water<br />

Abstract: The rate <strong>of</strong> leaching <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) by simulated rainfall was determined<br />

for carrot and possum pellet baits containing 0.08 and 0.15% 1080. Carrot baits were highly water-resistant<br />

and showed no decline in 1080 concn after 200 mm <strong>of</strong> rain. It is concluded that it is inadvisable to use<br />

carrot bait in arid areas when rapid restocking <strong>of</strong> land is required after a control operation, but they may be<br />

particularly suitable for forest habitats. Of the two types <strong>of</strong> pellet (Wanganui No. 7 and RS5) tested, RS5<br />

pellets were the less water-resistant and started to disintegrate after only 5 mm <strong>of</strong> rain. The 1080 concn also<br />

declined more rapidly in these pellets. So that toxicity is retained for the maximum length <strong>of</strong> time, RS5<br />

pellets should be used in arid areas and Wanganui No. 7 pellets in wetter environments, when pellets are<br />

the bait <strong>of</strong> choice. RS5 pellets should be used if rapid return to stock to the land is required.<br />

Bowen, L. H., Morgan, D. R., and Eason, C. T. Persistence <strong>of</strong> 1080 in baits under simulated rainfall.<br />

[LC9495/107], -8. 1995. Christchurch, Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract<br />

report.<br />

Ref Type: Report<br />

Keywords: bait degradation/1080<br />

Abstract: Objective: To determine the rate <strong>of</strong> leaching <strong>of</strong> 1080 by simulated rainfall from commercial 1080<br />

pellets and carrot baits.<br />

Conclusions / recommendations : Carrot baits are highly water-resistant, and it is inadvisable to use them<br />

19


1080 Reassessment Application October 2006<br />

Appendix C<br />

where rapid destocking <strong>of</strong> land is required; in order to retain toxicity for the maximum length <strong>of</strong> time, RS5<br />

pellets should be used in arid areas and the more water-resistant Wanganui no 7 pellets in wetter<br />

environments. If rapid return <strong>of</strong> stock to land is required, RS5 pellets should be used; bait type is a more<br />

important determinant <strong>of</strong> 1080 persistence than initial concentration.<br />

Bowman, R. G. (1999). Fate <strong>of</strong> sodium mon<strong>of</strong>luroacetate (1080) following disposal <strong>of</strong> pest bait to a<br />

landfill. New Zealand journal <strong>of</strong> ecology 23, 193-197.<br />

Keywords: persistence in water/persistence in soil/1080/baits<br />

Abstract: The results <strong>of</strong> a programme to monitor the containment and natural breakdown <strong>of</strong> approximately<br />

12 000 kg <strong>of</strong> toxic vertebrate pest bait, containing compound 1080 (sodium mon<strong>of</strong>luroacetate), in a landfill<br />

site are reported. The baits were buried in a purpose-dug pit in a managed solid waste disposal site at<br />

Winton in central Southland, New Zealand, in August 1996. Compound 1080 is used extensively in a bait<br />

form to control a range <strong>of</strong> introduced vertebrate pests, (e.g., European rabbit, Australian brush tailed<br />

possum), which cause considerable economic and environmental damage in New Zealand. Two shallow<br />

monitor bores, sited 5 and 13 m from the disposal pit, were sampled weekly for five weeks and thereafter<br />

monthly for 13 months. Analyses detected 1080 in 5 <strong>of</strong> the 28 groundwater/leachate samples. The 1080<br />

concentrations in those samples, except for one result, were low. These were either below or close to the<br />

Ministry <strong>of</strong> Health provisional maximum acceptable value standards (PMAV) for drinking water, currently<br />

0.005 mu g ml(-1). The concentrations <strong>of</strong> 1080 in groundwater in the more distant bore (13 m) were<br />

markedly lower than those in the nearer bore (5 m). 1080 was first detected in the near bore after 5 weeks<br />

and the more distant bore after 16 weeks. The level and frequency <strong>of</strong> incidence <strong>of</strong> 1080 in both holes<br />

decreased over the sampling period until none was detected after 10 months. In situ sampling <strong>of</strong> the<br />

residual waste material indicated the 1080 concentration in the disposal pit decreased to less than 10% <strong>of</strong> its<br />

original level in 12 months. The active anaerobic bacterial processes operating in the organic refuse pile<br />

appear to provide an ideal environment for the rapid natural breakdown <strong>of</strong> 1080. The findings will assist<br />

with the setting <strong>of</strong> conditions for resource consents concerning the disposal <strong>of</strong> materials containing 1080 in<br />

landfill sites.<br />

Bowman, R. H. (<strong>1964</strong>). Inhibition <strong>of</strong> citrate metabolism by sodium fluoroacetate in the perfused rat heart<br />

and the effect on phosph<strong>of</strong>ructokinase activity and glucose utilisation. Biochemical journal 93, 13c-15c.<br />

Keywords: inhibition/citrate/metabolism/sodium fluoroacetate/fluoroacetate/heart<br />

Abstract: The results do show that the concentration <strong>of</strong> ATP was considerably decreased in hearts from<br />

animals treated with fluoroacetate, but it is not known whether these depressed ATP concentrations are<br />

below that required for adequate hexokinase activity in the heart.<br />

Brady, R. O. (1955). Fluoroacetyl coenzyme A. Journal <strong>of</strong> biological chemistry 217, 213-224.<br />

Keywords: fluoroacetate/poison/fluorocitrate<br />

Abstract: The increasing biochemical importance <strong>of</strong> reactions mediated by thiol esters <strong>of</strong> coenzyme A 1<br />

leads to an interest in the possible metabolic activity <strong>of</strong> substituted derivatives <strong>of</strong> CoASH. Of particular<br />

interest is mon<strong>of</strong>luoroacetyl coenzyme A, since fluoroacetate is a potent lethal poison. A partial<br />

explanation <strong>of</strong> the toxicity <strong>of</strong> fluoroacetate has come from the work <strong>of</strong> Liébecq and Peters (3) and Martius<br />

(4). Peters and collaborators (5) have elegantly demonstrated the formation <strong>of</strong> fluorocitrate which is a<br />

potent inhibitor <strong>of</strong> the tricarboxylic acid cycle by virtue <strong>of</strong> its competitive inhibition <strong>of</strong> the enzyme<br />

aconitase (6). The formation <strong>of</strong> fluorocitrate is presumed to be due to the activation <strong>of</strong> fluoroacetate to Facetyl<br />

SCoA, which is subsequently condensed with oxalacetate in the presence <strong>of</strong> the condensing enzyme<br />

described by Ochoa, Stern, and Schneider (7).<br />

The preparation and properties <strong>of</strong> F-acetyl SCoA and its reactivity in various enzyme systems are<br />

described. Evidence for a fluoroacetate activating system different from that for acetate is reported.<br />

Brand, M. D., Evans, S. M., Mendes-Mourão, J., and happell, J. B. (1973). Fluorocitrate inhibition <strong>of</strong><br />

Aconitate hydratase and the tricarboxylate carrier <strong>of</strong> rat liver mitochondria. Biochemical journal 134, 217-<br />

224.<br />

Keywords: fluorocitrate/inhibition/liver<br />

Abstract: 1. The effect <strong>of</strong> biologically synthesized and purified fluorocitrate on the metabolism <strong>of</strong><br />

tricarboxylate anions by isolated rat liver mitochondria was investigated, in relation to the claim by Eanes<br />

et al. (1972) that this fluoro compound inhibits the tricarboxylate carrier at concentrations at which it has<br />

20


1080 Reassessment Application October 2006<br />

Appendix C<br />

little effect on the aconitate hydratase activity. 2. That the inhibitory action <strong>of</strong> fluorocitrate is at the level <strong>of</strong><br />

the aconitate hydratase and not at the level <strong>of</strong> the tricarboxylate carrier is indicated by the following<br />

findings. Although the oxidation <strong>of</strong> citrate and cis-aconitate, but not that <strong>of</strong> isocitrate, was inhibited by<br />

fluorocitrate, the exchange <strong>of</strong> internal citrate for external citrate or L-malate was not. Had the<br />

tricarboxylate carrier been affected, these latter exchange reactions would have been inhibited. 3. By using<br />

aconitate hydratase solubilized from mitochondria it was found that with citrate as substrate the inhibition<br />

by fluorocitrate was partially competitive (Ki = 3.4x10 -8 M), whereas with cis-aconitate as substrate the<br />

inhibition was partially non-competitive (Ki = 3.0x10 -8 M).<br />

Bremer, J. and Davis, J. (1973). Fluoroacetylcarnitine: metabolism and metabolic effects in mitochondria.<br />

Biochimica et biophysica acta 326, 262-271.<br />

Keywords: metabolism/citrate/heart/muscle/biochemistry/fluorocitrate/liver/pathology<br />

Abstract: The metabolism and metabolic effects <strong>of</strong> fluoroacetylcarnitine have been investigated. 1,<br />

Carnitineacetyltransferase (EC 2.3.1.7) transfers the fluoro-acetyl group <strong>of</strong> fluoroacetylcarnitine nearly as<br />

rapidly to CoA as the acetyl group <strong>of</strong> acetylcarnitine. 2. Fluorocitrate is then formed by citrate synthase<br />

(EC 4.1.3.7) but htis second reaction is relatively slow. 3. The fluorocitarte formed intramitochondrially<br />

inhibits the metabolism <strong>of</strong> citrate. 4. In heart and skeletal muscle mitochondria the accumulated citarte<br />

inhibits citrate synthesis and the beta-oxidation <strong>of</strong> fatty acids. Free acetate is formed, presumably because<br />

accumulated acetyl-CoA is hydrolyzed. 5. In liver mitochondria the accumulation <strong>of</strong> citrate leads to a<br />

relatively increased rate <strong>of</strong> ketogenesis. Increased ketogensis is obatined also upon the addition <strong>of</strong> citrate to<br />

the reaction mixture.<br />

Bremer, J. and Davis, E. J. (1974). Citrate as a regulator <strong>of</strong> acetyl-CoA metabolism in liver mitochondria.<br />

Biochimica et biophysica acta 370, 564-572.<br />

Keywords: citrate/metabolism/liver/mode <strong>of</strong> action/enzyme/fluorocitrate<br />

Abstract: The reversibility <strong>of</strong> citrate synthesis and the effects <strong>of</strong> fluorocitrate on citrate synthesis in whole<br />

mitochondria have been investigated. Cleavage <strong>of</strong> citrate to oxaloacetate (trapped as malate) and acetyl-<br />

CoA (trapped as acetycarnitine) in whole liver mitochondria can be demonstrated. The maximum rate <strong>of</strong><br />

the reversed reaction is at most 1/40 <strong>of</strong> the maximum rate <strong>of</strong> citrate synthesis. Citrate and fluorocitrate are<br />

competitive inhibitors with respect to oxaloacetate <strong>of</strong> purified pig heart synthase. The K1 for both<br />

compounds was found to be approx. 1.5 mM. Both citrate and fluorocitrate inhibit citrate synthesis and<br />

increase ketone genesis in whole liver mitochondria. The probably act as competitive inhibitors with<br />

respect to oxaloacetate, since malate counteracts this inhibition. For kinetic reasons it is concluded that the<br />

citrate synthesis recation probably never approaches equilibrium in the intact tissue. The improtance<strong>of</strong><br />

citrate in the regulation <strong>of</strong> citrate and ketone body fomration in the liver is discussed.<br />

Brezis, M., Shanley, P., Silva, P., Spokes, K., Lear, S., Epstein, F., and Rosen, S. (1985). Disparate<br />

mechanisms for hypoxic cell injury in different nephron segments. Journal <strong>of</strong> Clinical Investigation 76,<br />

1796-1806.<br />

Keywords: kidney/inhibition/metabolism/mon<strong>of</strong>luoroacetate<br />

Abstract: Hypoxic injury was evaluated morphologically in the proximal tubule and in the medullary thick<br />

ascending limb <strong>of</strong> isolated rat kidneys perfused for 90 min with or without O2 or with various metabolic<br />

inhibitors. Inhibition <strong>of</strong> mitochondrial respiration (with rotenone, antimycin, oligomycin) or <strong>of</strong><br />

intermediary metabolism (with mon<strong>of</strong>luoroacetate, malonate, 2-deoxyglucose) caused reduction in renal<br />

oxygen consumption, renal function and ATP content comparable with those elicited by oxygen<br />

deprivation.<br />

Brezis, M., Rosen, S., Spokes, K., Silva, P., and Epstein, F. (1986). Substrates induce hypoxic injury to<br />

medullary thick limbs <strong>of</strong> isolated rat kidneys. American journal <strong>of</strong> physiology 251, F710-F717.<br />

Keywords: kidney/metabolism/inhibition/mon<strong>of</strong>luoroacetate<br />

Abstract: Under certain conditions, excess <strong>of</strong> substrates may be detrimental to the kidney. In isolated rat<br />

kidneys perfused with cell-free medium, oxidative metabolism to support reabsorptive transport in the<br />

presence <strong>of</strong> a limited oxygen supply results in hypoxic injury to medullary thick ascending limbs (mTAL).<br />

Since inhibitors <strong>of</strong> mitochondrial respiration markedly reduced this injury, we evaluated the effects <strong>of</strong><br />

altering the availability <strong>of</strong> substrate for oxidative metabolism in the mTAL. Inhibition <strong>of</strong> glucose utilization<br />

with 2-deoxyglucose (50 mM) and simultaneous inhibition <strong>of</strong> long-chain fatty acid metabolism with 2-<br />

21


1080 Reassessment Application October 2006<br />

Appendix C<br />

tatredecyglycidic acod (10 -4 mM) in the absence <strong>of</strong> exogenous substrates consistently reduced hypoxic cell<br />

injury to mTAL. Similarly the direct inhibition <strong>of</strong> substrate oxidation by the citric acid cycle with<br />

mon<strong>of</strong>luoroacetate (5 mM) also reduced the extent <strong>of</strong> damage to this nephron segment.<br />

Bringmann, G. and Kuhn, R. (1976). Vergleichende Befunde der Schadwirkung wassergefahrender St<strong>of</strong>fe<br />

gegen Backterien (Psuedomonas putida) und Blaualgen (Microcystis aeruginosa). GWF-wasser/abwasser<br />

117, 410-413.<br />

Keywords: bacteria/algae/toxicity/sodium fluoroacetate<br />

Brock, E. M. (1965). Toxicological feeding trials to evaluate the hazard <strong>of</strong> secondary poisoning to gopher<br />

snakes, Pituophis catenifer. Copeia 2, 244-245.<br />

Keywords: poisoning/reptiles/secondary poisoning/non-target species<br />

Abstract: No observable reaction was shown by snakes which accpeted mice that had consumed lethal<br />

quantities <strong>of</strong> either thallium sulphate or <strong>of</strong> warfarin, diphacin, or prolin. Snakes fed rodents poisoned with<br />

sodium fluoroacetate, endrin, arsenic trioxide or zinc phosphide baits <strong>of</strong>ten regurgitated the mice but<br />

exhibited no other response. In fourteen snake feeding trials, the Microtus used had accepted baits soaked<br />

in a high concentration <strong>of</strong> sodium fluoroacetate. Twelve <strong>of</strong> these mice were regurgitated. Snakes fed mice<br />

which had eaten baits treated with strychine alkaloid became irritable and reacted with tremors. Five <strong>of</strong><br />

these snakes died <strong>of</strong> secondary poisoning.<br />

Brockmann, J. L., McDowell, A. V., and Leeds, W. G. (1955). Fatal poisoning with sodium fluoroacetate :<br />

report <strong>of</strong> a case. Journal <strong>of</strong> the American Medical Association 159, 1529-1532.<br />

Keywords: diagnosis/treatment/pathology/sodium fluoroacetate/humans<br />

Abstract: Certain drugs can be used with benefit in a case <strong>of</strong> sodium fluoroacetate poisoning. These are (1)<br />

procainamide (Pronestyl) hydrochloride for cardiac arrythmias, (2) intravenously used alcohol for central<br />

nervous system irritability, and (3) vasodepressor drugs such as mephentermine (Wyamine) sulfate to<br />

maintain blood pressure. In the future these drugs, which we feel prolonged the life <strong>of</strong> our patient, should<br />

be tried in cases <strong>of</strong> sodium fluoroacetate poisoning, as they may save the lives <strong>of</strong> patients who have<br />

ingested smaller amounts <strong>of</strong> the poison.<br />

Brothers, N. P. (1982). Feral cat control on Tasman Island. Australian Ranger Bulletin 2, 9.<br />

Brown, C. J. (1993). Test <strong>of</strong> compound 1080 from a poison collar on a captive vulture. Vulture News 29,<br />

19-26.<br />

Keywords: 1080/poison/birds/toxicity/USA/predators/lethal dose/<strong>poisons</strong><br />

Abstract: The poison collar was developed in the USA in the late 1970s. It was designed to be an<br />

effective and highly selective means <strong>of</strong> killing Coyotes Canis latrans that preyed on domestic stock,<br />

without harming non-target individuals and species (Connolly et al. 1978; Saverie & Sterner 1979). The<br />

collar has been exported to other parts <strong>of</strong> the world, where it is used against mainly medium-sized<br />

mammalian predators.<br />

The poison collar consists <strong>of</strong> two rubber pouches containing poison under low pressure, and two straps<br />

with velco attachments. The collar is fitted around the neck <strong>of</strong> a sheep or goat and the pouches are<br />

positioned around the throat, which is the site <strong>of</strong> attack by most mammalian predators. The exact position<br />

<strong>of</strong> the pouches depends on the expected predator. A number <strong>of</strong> young domestic animals (usually at least<br />

20) are fitted with collars and released with a larger flock <strong>of</strong> adult animals into the camp where losses are<br />

being experienced. The predator usually atacks one <strong>of</strong> the smaller animals. On biting into one <strong>of</strong> the<br />

poison pouches, a lethal dose <strong>of</strong> poison squirts into the predator's mouth and is ingested.<br />

In the USA a wide spectrum <strong>of</strong> <strong>poisons</strong> were tested for use in the collar (e.g. Connelly et al. 1978);<br />

Saverie & Sterner 1979; Sterner 1979). Compound 1080 (sodium mon<strong>of</strong>luoroacete) was found to be the<br />

most suitable toxin and was registered for this purpose (Scrivner 1983; Howard & Schmidt 1984). The use<br />

<strong>of</strong> the poison collar and compound 1080 were vigorously opposed and intensively monitored by a number<br />

<strong>of</strong> environmental pressure groups in the USA (e.g. Anon. 1982; Doherty 1982; Sibbison 1984). The issue<br />

was eventually settled in court. The verdict was in favour <strong>of</strong> the use <strong>of</strong> the collar and compound 1080<br />

because, after extensive testing by impartial organisations, no secondary poisoning was found and no nontarget<br />

animals were killed (Connolly 1983; Eastland & Beasom 1986). Recent investigations <strong>of</strong> secondary<br />

poisoning concluded that consuming carcasses <strong>of</strong> Coyotes killed by 1080 poison from a collar poses little,<br />

22


1080 Reassessment Application October 2006<br />

Appendix C<br />

if any, hazard to Striped Skunks Mephitis mephitis and Golden Eagles Aquila chrysaetos (Burns et al.<br />

1991).<br />

Results:<br />

The vulture's first meal was at about 18h00 on day one. About 0.5 kg <strong>of</strong> food was taken. Within 30 min<br />

the bird regurgitated its entire crop contents. The bird fed again at midday on day two, taking about 0.3 kg,<br />

which it kept down. It fed again at about 17h00 on day two, from the carcass (about 0.5 kg) and from the<br />

meat ergurgitated on day one (about 0.2 kg). Within about 20 min it regurgitated about 0.3 kg but kept the<br />

remainder down until nightfall. On arrival at the cage at 07h30 on day three it was apparent that the vulture<br />

had regurgitated about 0.2 kg <strong>of</strong> food during the night, and that it had been pulling at the carcass, but not<br />

feeding much, as its crop was empty.<br />

In addition to feeding from the incisions, and gaining access through them to meat between the skin and<br />

skeleton, the bird had tugged and torn the contaminated skin. At no stage did the vulture show any<br />

symptoms <strong>of</strong> 1080 poisoning other than regurgitation. Common symptoms are depression, unsteady gait<br />

and loss <strong>of</strong> balance, closed eyes, hunched posture and raised or fluffed feathers (McIlroy 1984). After<br />

returning the bird to the large aviary, it fed on clean meat on the afternoon <strong>of</strong> day three and showed no<br />

signs <strong>of</strong> having been poisoned.<br />

Brown, F. G. (1972). Heart-leaf, poisonous to livestock. Unknown.<br />

Abstract: The distribution in Queensland, clinical symptoms and control <strong>of</strong> heart-leaf poison bush<br />

(Gastrolobium grandiflorum), which is toxic to livestock at all stages <strong>of</strong> growth, are described. The toxin is<br />

a fluoroacetate. 2,4,5-T diluted with dieselene and applied to the main stem at ground level gave effective<br />

control<br />

Brown, T. D., Jones-Mortimer, M. C., and Kornberg, H. L. (1977). The enzymic interconversion <strong>of</strong> acetate<br />

and acetyl coenzyme A in Escherichia-coli. J Gen Microbiol 102, 327-336.<br />

Abstract: Mutants <strong>of</strong> Escherichia coli K12 have been isolated that grow on media containing pyruvate or<br />

proline as sole carbon sources despite the presence <strong>of</strong> 10 or 50 µm-sodium fluoroaetate. Such mutants lack<br />

either acetate kinase [ATP: acetate phosphotransferase; EC2.7.2.I] or phosphotransacetylase [acetyl-<br />

CoA:orthophosphate acetyltransferase; EC2.3.I.8] activity. Unlike wild-type E coli, phosphotransacetylase<br />

mutants do not excrete acetate when growing aerobically or anearobically on glucose; their anaerobic<br />

growth on this sugar is slow. The genes that specify acetate kinase (ack) and phosphotransacetylase (pta)<br />

activities are cotransducible with each other and with purF and are thus located at about min 50 on the E<br />

coli linkage map. Although Pta- and Ack- mutants are greatly impared in their growth on acetate, they<br />

incorporate [2- 14 C]acetate added to cultures growing on glycerol, but not on glucose. An inducible acetyl-<br />

CoA synthetase [acetate: CoA ligase (AMP-forming); EC6.2.I.I] effects this uptake.<br />

Browne, J. L., Sanford, P. A., and Smyth, D. H. (1977). Transport and metabolic processes in the small<br />

intestine. Proceedings <strong>of</strong> the <strong>Royal</strong> Society <strong>of</strong> London, B 195, 307-321.<br />

Keywords: citrate/fluoride/fluoroacetate/citric acid/inhibition/gut<br />

Abstract: The transfer <strong>of</strong> alpha -methylglucoside and citrate was studied in experiments with everted sacs<br />

<strong>of</strong> rat and hamster small intestine. The transfer <strong>of</strong> alpha -methylglucoside was stimulated in the hamster<br />

tissue by metabolizable hexoses and by citrate, succinate and pyruvate. In the rat jejunum metabolizable<br />

hexoses only were effective. Fluoride (10 mmol/litre) inhibited endogenous transfer in the hamster and<br />

glucose-dependent transfer in both rat and hamster. Fluoroacetate (10 mmol/litre) inhibited endogenous<br />

transfer in tissue <strong>of</strong> both animals, but inhibited glucose-dependent transfer only in the hamster. This<br />

indicated that in the hamster the citric acid cycle is the major source <strong>of</strong> energy both for endogenous<br />

substrate and for added glucose. In the rat, added glucose supplies energy mainly through the glycolytic<br />

pathway, although endogenous energy is derived from the citric acid cycle. In the rat, glucose abolished<br />

completely the inhibition <strong>of</strong> alpha -methylglucoside transfer produced by L-proline, although the inhibitory<br />

effects <strong>of</strong> galactose could be only partially overcome. In the hamster, L-proline caused an inhibition which<br />

was not completely abolished by the additional energy. The results indicate that in the rat sugars and amino<br />

acids compete for energy rather than interact at the carrier level. In the hamster it is possible that sugars and<br />

amino acids interact at carrier level in addition to competing for energy. Citrate is more rapidly transferred<br />

and metabolized by hamster than by rat intestine. Citrate and unidentified radioactive metabolites<br />

accumulated in the serosal fluid, thus establishing the existence <strong>of</strong> a specific mechanism for citrate transfer<br />

23


1080 Reassessment Application October 2006<br />

Appendix C<br />

Brownsey, R. W., Bridges, B. J., and Denton, R. M. (1977). Effects <strong>of</strong> fluoroacetate and (-)-hydroxycitrate<br />

on fatty acid synthesis in rat epididymal adipose tissue. Biochemical Society transactions 5, 1286-1288.<br />

Keywords: fluoroacetate/citrate/metabolism/testes<br />

Abstract: Regualtion <strong>of</strong> the conversion <strong>of</strong> pyruvate (derived from glucose) into fatty acids in rat adipose<br />

tissue appears to be largely brought about by parallel changes in the proportions <strong>of</strong> pyruvate dehydrogenase<br />

and acetyl-CoA carboxylase in their respective active forms. We conclude form this study as we have<br />

previously on other evidence that the concentration <strong>of</strong> citrate is probably not <strong>of</strong> great importance in the<br />

regulation <strong>of</strong> fatty acid synthesis.<br />

Buckley, N. A., Whyte, I. M., O'Connell, D. L., and Dawson, A. H. (1999). Activated charcoal reduces the<br />

need for N-Acetylcysteine treatment after Acetaminophen (Paracetamol) overdose. Clinical Toxicology 37,<br />

753-757.<br />

Keywords: antidote/treatment/poisoning/humans<br />

Abstract: Background: The evidence for efficacy <strong>of</strong> gastric lavage and activated charcoal for<br />

gastrointestinal decontamination in poisoning has relied entirely on volunteer studies and/or<br />

pharmacokinetic studies and evidence for any clinical benefits or resource savings is lacking. Aim <strong>of</strong> study:<br />

To investigate the value <strong>of</strong> gastrointestinal decontamination using gastric lavage and/or activated charcoal<br />

in acetaminophen (paracetamol) poisoning. Patients and Methods: We analyzed a series <strong>of</strong> 981 consecutive<br />

acetaminophen poisonings. These patients were treated with gastric lavage and activated charcoal, activated<br />

charcoal alone, or no gastrointestinal decontamination. The decision as to which treatment was received<br />

was determined by patient cooperation, the treating physician, coingested drugs, and time to presentation<br />

after overdose. Results: Ot 981 patients admitted over 10 years, 10% (100) had serum concentrations <strong>of</strong><br />

acetaminophen that indicated a probable or high risk <strong>of</strong> hepatotoxicity. The risk <strong>of</strong> toxic concentrations for<br />

patients ingesting less than 10g <strong>of</strong> acetaminophen was very low. In patients presenting within 24 hours,<br />

who had ingested 10g or more, those who had been given activated charcoal were significantly less likely<br />

to have probable or high tisk concentrations (Odds ratio 0.36, 95% CI 0.23-0.58, p < 0.0001). Gastric<br />

lavage, in addition to activated charcoal, did not further decrease the risk (Odds ratio 1.12, 95% CI 0.57-<br />

2.20, p = 0.86). Conclusions: Toxic concentrations <strong>of</strong> serum acetaminophen (paracetamol) are uncommon<br />

in patients ingesting less than 10 g. In those ingesting more, activated charcoal appears to reduce the<br />

number <strong>of</strong> patients who achieve toxic acetaminophen concentrations and thus may reduce the need for<br />

treatmernt and hospital stay.<br />

Buffa, P. and Peters, R. A. (1950). The in vivo formation <strong>of</strong> citrate induced by fluoroacetate and its<br />

significance. Journal <strong>of</strong> physiology 110, 488-500.<br />

Keywords: metabolism/mode <strong>of</strong> action/persistence in<br />

animals/citrate/fluoroacetate/enzyme/biochemistry/aconitase<br />

Buffa, P., Guarriero-Bobyleva, V, and Pasquali-Rochetti, I. (1971). Biochemical effects <strong>of</strong> fluoroacetate<br />

poisoning in rat liver. CIBA Foundation Symposia 2, 303-326.<br />

Keywords: fluoroacetate/poisoning/liver/metabolism/mode <strong>of</strong> action/lethal dose/citrate/fluorocitrate/rats<br />

Abstract: The mode <strong>of</strong> action <strong>of</strong> fluoroacetate in the liver <strong>of</strong> the rat has been studied. The response <strong>of</strong> liver<br />

tissue to fluoroacetate posioning depends in a decisive manner on the nutritional state <strong>of</strong> the animal. In the<br />

fed rat a lethal dose <strong>of</strong> fluoroacetate causes marked accumulation <strong>of</strong> citrate, rapid fall in the amount <strong>of</strong><br />

glycogen and decrease <strong>of</strong> tissue ATP. In the rat starved for 24 hours, the concentration <strong>of</strong> liver glycogen is<br />

very low, the amount <strong>of</strong> ATP is reduced by about 40% and fluoroacetate poisoning causes only a slight<br />

increase in liver citrate. In teh fed rat the tricarboxylic acid cycle runs mostly on pyruvate, and<br />

fluoroacetate is converted to fluorocitrate; when the tricarboxylic acid cycle runs mostly on fatty acids, as is<br />

the case in the starved rat, very little fluoroacetate is converted to fluorocitrate in the liver. In the liver<br />

slices obtained for fluoroacetate-poisoned fed rats the endogenous respiration is not inhibited and the citrate<br />

previously accumulated is metabolized. The mirochondria isolated from the poisoned liver are inhibited in<br />

their ability to oxidize added citrate (by over 50%), cis-aconitate (by about 15%) and oxaloacetate (by<br />

about 30%), whereas they oxidize other intermediates <strong>of</strong> the cycle and pyruvate and glutamate at normal<br />

rates. Oxidative phosphorylation is not affected. Extramitochondrial aconitate hydratase is virtually<br />

unaffected in the liver cell poisoned with fluoroacetate and in conjunction with extramitochondrial NADPlinked<br />

isocitrate dehydrogenase, it provides an alternative metabolic pathway for the citrate which has<br />

diffused out <strong>of</strong> the mitochondria into the cytosol.<br />

24


1080 Reassessment Application October 2006<br />

Appendix C<br />

Buffa, P., Guarriero-Bobyleva, V, and Costa-Tiozzo, R. (1973). Metabolic effects <strong>of</strong> fluoracetate poisoning<br />

in mammals. Fluoride 6, 224-245.<br />

Keywords: metabolism/poisoning/mammals/symptoms/Krebs cycle/pathology<br />

Abstract: Fluoroacetate poisoning causes a variety <strong>of</strong> metabolic effects in animals: block in the<br />

tricarboxylic acid cycle at the citrate stage; accumulation <strong>of</strong> citrate and lowering <strong>of</strong> adenosine triphosphate<br />

in tissues; increased production <strong>of</strong> ketone bodies; rapid hydrolysis <strong>of</strong> glycogen in liver, skeletal muscle and<br />

heart tissues and a parallel in blood glucose and lactate.<br />

Injected fluoroacetate is rapidly distributed in all the tissues <strong>of</strong> the rat and 3% <strong>of</strong> it is transformed into<br />

fluorocitrate. The synthesis <strong>of</strong> fluorocitrate occurs in the mitochondria, in the complex formed by the inner<br />

membrane and the matrix. In isolated rat liver mitochondria fluorocitrate is formed from pyruvate plus<br />

fumarate or from acetate plus fumarate but not from fatty acids plus fumarate. Endogenous fluorocitrate<br />

inhibits specifically the mitochondrial-bound aconitate hydratase and not the enzyme present in the soluble<br />

cytoplasm. The primary biochemical lesion is soon followed by secondary inhibitions at various sites in<br />

the tricarboxylic acid cycle and ultrastructural changes in the mitochondria.<br />

The increased production <strong>of</strong> ketone bodies is likely to be induced by inhibition <strong>of</strong> citrated synthase caused<br />

by fluoroacetyl-SCoA and the accumulated citrate.<br />

Glycogen depletion in all probability is due to adrenalin release or intense sympathetic stimulation as a<br />

result <strong>of</strong> the biochemical changes caused by fluoroacetate. The parallel hyperglycemia and increased<br />

lactate formation can be explained by the rapid glycogenolysis.<br />

The metabolic changes caused by fluoroacetate poisoning are discussed in light <strong>of</strong> the present knowledge<br />

on cell biochemistry.<br />

Buffa, P., Pasquali-Rochetti, I., Barasa, A., and Godina, G. (1977). Biochemical lesions <strong>of</strong> respiratory<br />

enzymes and configurational changes <strong>of</strong> mitochondria in vivo II. Early ultrastructural modifications<br />

correlated to the biochemical lesion induced by fluoroacetate. Cell and tissue research 183, 1-23.<br />

Keywords: mode <strong>of</strong> action/pathology/treatment/developmental toxicity/biochemistry/aconitase<br />

Abstract: Correlative biochemical and electron microscopic alterations were observed in chick embryo<br />

myoblasts in vitro after treatment with fluoroacetate. Fluoroacetate poisoning caused an increase <strong>of</strong> citrate<br />

and a decrease <strong>of</strong> ATP in the cultures. Cell respiration was only slightly impaired by fluoroacetate in the<br />

first 10 min but was inhibited to 30% one hour after exposure to the poison. Fluoroacetate did not affect<br />

oxidative phosphorylation. The evidence suggests that fluoroacetate was transformed in myoblasts into<br />

fluorocitrate which inhibited the mitochondrialbound aconitate hydratase as in adult tissues. Ultrastructural<br />

changes in the majority <strong>of</strong> the fluoroacetatetreated cells were observed. Very few myoblasts appeared<br />

unaffected by the poison. Mitochondria were specifically altered. The early changes occurred in the<br />

mitochondrial matrix where the inhibited enzyme is known to be located and were followed by<br />

modifications in the configuration and structure <strong>of</strong> cristae. Exogenous fluorocitrate caused ultrastructural<br />

changes in the mitochondria similar to that provoked by fluoroacetate. The localization <strong>of</strong> the early change<br />

in the mitochondrial matrix and the evaluation <strong>of</strong> the structural modifications suggest a correlation between<br />

the biochemical lesion, i.e. the inhibition <strong>of</strong> aconitate hydratase, and the change revealed in the<br />

mitochondrial structure containing the inhibited enzyme.<br />

Buffa, P., Costa Tiozzo, R., and Gualtieri Fruggeri, M. (1979). The synthesis <strong>of</strong> fluorocitrate from<br />

fluoroacetate in isolated rat mitochondria. Fluoride 12, 114-124.<br />

Keywords:<br />

fluorocitrate/fluoroacetate/citrate/liver/brain/kidney/heart/acetate/inhibition/enzyme/aconitate/metabolism<br />

Abstract: The lethal effects <strong>of</strong> fluoroacetate have always been found to be associated with an increase <strong>of</strong><br />

citrate in the tissues. For this reason, accumulation <strong>of</strong> citrate is considered an indicator for fluorocitrate<br />

formation. The synthesis <strong>of</strong> fluorocitrate was studied in isolated rat liver, brain, kidney and heart<br />

mitochondria. Evidence for fluorocitrate formation was found in liver, brain and kidney mitochondria but<br />

not in heart mitochondria. Fluoroacetate was activated and transformed into fluorocitrate in mitochondria<br />

metabolizing either pyruvate and fumarate, or acetate and fumarate, or octanoate and fumarate; the<br />

fluorocitrate synthesis was demonstrated by citrate accumulation in the system following the inhibition <strong>of</strong><br />

the enzyme aconitate hydratase. Synthesis <strong>of</strong> fluorocitrate did not appear to require mitochondrial structural<br />

integrity; it occurred in osmotically altered mitochondria and in mitochondria deprived <strong>of</strong> the outer<br />

membrane. When the substrates were pyruvate and fumarate in liver mitochondria, uncoupling <strong>of</strong> oxidative<br />

phosphorylation enhanced citrate formation and did not inhibit fluorocitrate synthesis. With acetate and<br />

25


1080 Reassessment Application October 2006<br />

Appendix C<br />

fumarate as substrates uncoupling <strong>of</strong> oxidative phosphorylation inhibited the both citrate and fluorocitrate<br />

synthesis. In liver mitochondria fluoroacetate was activated through 2 separate pathways, one associated<br />

with pyruvate metabolism and not dependent on oxidative phosphorylation energy, the other associated<br />

with acetate metabolism and ATP dependent<br />

Burande, M. D., Goyal, R. K., and Verma, S. C. (1983). Studies on the mechanism <strong>of</strong> cardiotonic effects <strong>of</strong><br />

sodium fluoroacetate and dobutamine. Indian journal <strong>of</strong> experimental biology 21, 150-152.<br />

Keywords: pathology/metabolism/fluoroacetate<br />

Abstract: Sodium fluoroacetate (20 to 320 µg) and dobutamine (0.5 to 0.8 µg) produced dose dependent<br />

positive inotropic effect in isolated frog heart preparation, without affecting the heart rate. The dose<br />

dependent increase in cardiac contractility to sodium fluoroacetate was not affected by propranolol (1 x 10 -6<br />

M), whereas the reponses to dobutamine were inhibited competitively by propranolol (1 x 10 -6 M).<br />

Phentolamine (1 x 10 -6 M), had no significant effect and phenomenon <strong>of</strong> tachyphylaxis was not observed<br />

with either sodium fluoroacetate or dobutamine. Responses to sodium fluoroacetate were not affected<br />

either by caffeine (2 mM), or by imidazole (100 µM). However, dose dependent responses to dobutamine<br />

were potentiated by caffeine and inhibited by imidazole. The decrease in sodium chloride concentration<br />

(from 110 to 165 mM) in frog Ringer solution, inhibited the responses to sodium fluoroacetate while<br />

increasing it (from 110 to 165 mM) the responses were potentiated. But the responses to dobutamine were<br />

unchanged when sodium chloride concentration in perfusion fluid were altered. It is suggestive from the<br />

data that sodium fluoroacetate induced positive inotrophic effects are probably due to sodium extrusion<br />

mechanism while dobutamine is acting directly through beta adrenoceptors and indirectly involving<br />

adenylate CAMP system for the positive inotrophic action.<br />

Burande, M. D., Goyal, R. K., and Verma, S. C. (1983). Influence <strong>of</strong> extracellular ions on the positive<br />

inotropic effects <strong>of</strong> sodium fluoroacetate and dobutamine. Indian Journal <strong>of</strong> Pharmacology 15, 111-118.<br />

Keywords: sodium fluoroacetate/fluoroacetate/heart/mode <strong>of</strong> action/amphibian<br />

Abstract: Sodium fluoroacetate (Na FAC, 20 ug to 320 ug) and dobutamine (0.5 ug to 8 ug) produced dose<br />

dependent positive inotropic effect in isolated frog heart preparation, without affecting the heart rate. The<br />

responses to NaFAC and dobutamine were inhibited when calcium chlroide (CaCl2) concentration was<br />

increased from 1.58 mM to 317 mM in frog Ringer solution. When CaCl2 concentration was reduced the<br />

responses to both NaFAC and dobutamine were potentiated. By reducing the potasium chloride (KCl)<br />

concentration in the perfusion fluid the response to NaFAC were potentiated, while increasing the<br />

concentration the responses were inhibited. However, the responses to dobutamine were unchanged by<br />

changing the KCl concentration in the perfusion fluid. The decrease in sodium chloride (NaCl)<br />

concentration potentiated the responses to NaFAC. However the responses to dobutamine were unchanged<br />

when NaCl concentration in the perfusion fluid were altered. It is suggested from the data that NaFAC<br />

induced positive inotropic effects probably due to sodium extrusion mechanism leading to facilitation <strong>of</strong><br />

calcium uptake.<br />

Burke, D. G., Lew, D. K., and Cominos, X. (1989). Determination <strong>of</strong> fluoroacetate in biological matrixes as<br />

the dodecyl ester. The Journal <strong>of</strong> the Association <strong>of</strong> Official Analytical Chemists 72, 503-507.<br />

Keywords: fluoroacetate/chemistry/analysis<br />

Burns, R. J., Connolly, G., and Okuno, I. Secondary toxicity <strong>of</strong> coyotes killed by 1080 single-dose baits.<br />

Salmon, T. P. 324-329. 1986. University <strong>of</strong> California, Davis. Proceedings Twelfth Vertebrate Pest<br />

Conference.<br />

Ref Type: Conference Proceeding<br />

Keywords: 1080/baits/persistence in animals/predators/USA/secondary poisoning<br />

Abstract: Carcasses and viscera <strong>of</strong> coyotes poisoned by Compound 1080 in single dose tallow baits (SDBs)<br />

were fed to 3 coyotes, 3 domestic dogs, 4 striped skunks, and 15 black-billed magpies to determine if these<br />

species would be poisoned secondarily. Test subjects received no food other than tissues from poisoned<br />

coyotes for periods <strong>of</strong> 14 to 35 days. Total amounts <strong>of</strong> contaminated coyote tissues consumed by dogs,<br />

coyotes, skunks, and magpies, respectively, averaged 67, 152, 117, and 371% <strong>of</strong> body weight. Except for<br />

one skunk that refused to eat, no mortalities occurred and no evidence <strong>of</strong> poisoning was seen.<br />

The average 1080 residue in tissues fed to nontarget animals from coyotes poisoned by one to three SDBs<br />

(5 to 15 mg 1080 per coyote) was 0.29, 0.30, and 0.31 repectively. Highest residue levels observed were<br />

26


1080 Reassessment Application October 2006<br />

Appendix C<br />

0.66 ppm in muscle, 0.79 ppm in small intestine, and 0.76 ppm in stomach tissue. These concentrations<br />

were apparently too low to cause secondary poisoning in the species tested.<br />

Burns, R. J., Tietjen, H., and Connolly, G. E. (1991). Secondary hazard <strong>of</strong> livestock protection collars to<br />

skunks and eagles. Journal <strong>of</strong> wildlife management 55, 701-704.<br />

Keywords: non-target species/mammals/birds/secondary poisoning/persistence in<br />

animals/livestock/livestock protection collar<br />

Burns, R. J. and Connolly, G. E. (1992). Toxicity <strong>of</strong> compound 1080 to magpies and the relationship <strong>of</strong><br />

dose rates to residues recovered. Proceedings <strong>of</strong> the Vertebrate Pest Conference 15, 403-408.<br />

Keywords: acute toxicity/birds/persistence in animals/1080/temperature/lethal dose/muscle/gut<br />

Burns, R. J. and Connolly, G. E. (1995). Toxicity <strong>of</strong> compound 1080 livestock protection collars to sheep.<br />

Archives <strong>of</strong> environmental contamination and toxicology 28, 141-144.<br />

Keywords: acute toxicity/mammals/non-target species/1080/sodium fluoroacetate/fluoroacetate/treatment<br />

Burns, R. J. and Connolly, G. E. (1995). Assessment <strong>of</strong> potential toxicity <strong>of</strong> compound 1080 from livestock<br />

protection collars to canines and scavenging birds. International Biodeterioration and Biodegradation 36,<br />

161-167.<br />

Keywords: secondary poisoning/birds/mammals/persistence in animals/1080/livestock/livestock protection<br />

collar/scavenger/dogs/muscle<br />

Burns, R. J., Zemlicka, D. E., and Savarie, P. J. (1996). Effectiveness <strong>of</strong> large livestock protection collars<br />

against depredating coyotes. Wildlife Society bulletin 24, 123-127.<br />

Keywords: livestock/livestock protection collar/1080/predators/symptoms/time to death/efficacy<br />

Abstract: We investigated the effectiveness <strong>of</strong> large livestock protection collars (LLPCs) to kill coyotes<br />

(Canis latrans) that attacked sheep. The LLPC, designed for sheep and goats >22.7 kg, contained the same<br />

formulation <strong>of</strong> Compound 1080 as the smaller collar (LPC) registered by the Environmental Protection<br />

Agency in 1985. In 32 tests involving 19 sheep wearing LLPCs, 12 coyotes made 14 neck or throat attacks.<br />

In 10 <strong>of</strong> the 14 attacks (71%) LLPCs were punctured and all 10 coyotes died. Coyotes that punctured<br />

collars showed signs <strong>of</strong> intoxication in an avergae <strong>of</strong> 203 minutes and died an average <strong>of</strong> 93 minutes later.<br />

Time to death did not differ among coyotes that punctured 1 collar comaprtment versus 2 compartments.<br />

The LLPC was more effective in deterring coyote predation on large sheep than the previously registered<br />

small LPC.<br />

Busana, F., Gigliotti, F., and Marks, C. A. (1998). Modified M-44 cyanide ejector for the baiting <strong>of</strong> red<br />

foxes (Vulpes vulpes). Wildlife research 25, 209-215.<br />

Keywords: cyanide/foxes/analysis/efficacy/mode <strong>of</strong> action/baits<br />

Abstract: Fox carcasses are seldom recovered after a 1080-baiting program, making analysis <strong>of</strong> efficacy<br />

difficult. Sodium cyanide was selected as an alternative toxin due to its rapid mode <strong>of</strong> action. A number <strong>of</strong><br />

bait techniques were trialled in order to develop an appropriate cyanide delivery system that could be used<br />

as a buried bait. Techniques investigated included treated wax and gelatine capsules, a wooden capsule<br />

holder and a modified M-44 cyanide ejector. Subsequent trials showed that the modified M-44 ejector had<br />

greater efficacy in recovering fox carcasses at bait stations when compared with the other techniques<br />

trialled. This paper describes the range <strong>of</strong> baits trialled and the modifications that allow the M-44 to be used<br />

as a buried bait. A protocol for deployment <strong>of</strong> the M-44 in the field, together with a brief assessment <strong>of</strong><br />

efficacy for each technique is also provided<br />

Busch, H. and Potter, V. R. (1952). Multiple effects <strong>of</strong> fluoroacetate on pyruvate metabolism in vitro.<br />

Proceedings <strong>of</strong> the Society for Experimental Biology and Medicine 80, 701-704.<br />

Keywords: fluoroacetate/metabolism/citrate/kidney/liver<br />

Abstract: Citrate formation is increased and the oxidation is diminished by the addition <strong>of</strong> fluoroacetate to<br />

kidney homogenates; under the same conditions, citrate formation is decreased and acetoacetate fromation<br />

is increased while oxidation is unchanged in liver homogenates. At higher concentrations <strong>of</strong> fluoroacetate,<br />

acetoacetate formation is also inhibited in liver homogenates.<br />

27


1080 Reassessment Application October 2006<br />

Appendix C<br />

Butcher, A. D. The effect on fauna <strong>of</strong> <strong>poisons</strong> used in vermin control. Wildlife Contribution No 5. <strong>1964</strong>.<br />

Victoria, Fisheries and Wildlife Department.<br />

Ref Type: Conference Proceeding<br />

Keywords: <strong>poisons</strong>/poison<br />

Byrd, G. V., McClellan, G. T., and Fuller, J. P. To determine the efficacy <strong>of</strong> and environmental hazards <strong>of</strong><br />

compound 1080 (sodium fluoroacetate) as a control agent for Arctic fox (Alopex lagopus) on Kiska Island,<br />

Aleutian islands unit. Alaska Maritime National Wildlife Refuge. Unpublished final progress report by<br />

AIU-AMNWR, 22pp. 1988.<br />

Ref Type: Unpublished Work<br />

Keywords: efficacy/1080/sodium fluoroacetate/fluoroacetate/foxes/lethal dose/baits/non-target<br />

species/birds<br />

Abstract: A single experimental application <strong>of</strong> Compound 1080 was used to assess the efficacy and hazards<br />

associated with efforts to eradicate introduced Arctic fox (Alopex lagopus) on Kiska Island, Alaska.<br />

Results from feeding trials showed that 4 mg <strong>of</strong> 1080 in beef tallow and bees wax pellets was an adequate<br />

lethal dose for Arctic foxes. In March and June <strong>of</strong> 1986, nearly 50,000 single-dose baits were distributed<br />

along the coastal areas <strong>of</strong> Kiska Island. Most foxes on Kiska were killed following the first application in<br />

March 1986, but at least one remained until June 1988. There was no evidence <strong>of</strong> mortality to non-target<br />

species like Bald eagles (Haliaeetus leucocephalus) or Common ravens (Corvus corax); however at least<br />

two Glaucous-winged gulls (Larus glaucescens) were killed, probably by directly ingesting bait. It appears<br />

the use <strong>of</strong> Compound 1080 to remove introduced Artic foxes on Kiska Island has been successful. Several<br />

species <strong>of</strong> island nesting birds appear to exhibit signs (by 1988) <strong>of</strong> population increase associated with fox<br />

eradication. With the eradication <strong>of</strong> Artic foxes on Kiska Island, the potential for this insular ecosystem to<br />

sustain former numbers <strong>of</strong> ground nesting birds has been restored.<br />

Cai, J., Luo, H., Guo, C., Cai, J. S., Luo, H. M., and Guo, C. K. (1997). Study on the clinical features <strong>of</strong><br />

fluoroacetamide and sodium fluoroacetate poisoning cases. Zhongguo Meijieshengwuxue ji Kongzhi Zazhi<br />

= Chinese Journal <strong>of</strong> Vector Biology and <strong>Control</strong> 8 , 251-254.<br />

Keywords: fluoroacetamide/sodium<br />

fluoroacetate/fluoroacetate/poisoning/symptoms/birds/mammals/humans<br />

Abstract: The symptoms <strong>of</strong> cases <strong>of</strong> fluoroacetamide and sodium fluoroacetate poisoning, which happened<br />

in Jinli town, Gaoyao City, Guangdong, China between June and November 1995 are described. The onset<br />

<strong>of</strong> poisoning in wild birds and mammals was rapid. Symptoms included vomiting and neurological<br />

symptoms. Mortality was high. Symptoms in poisoned humans included dizziness, headache, nausea,<br />

vomiting and tics<br />

Cai, X. L., Zhang, D. M., Ju, H. X., Wu, G. P., and Liu, X. P. (2004). Fast detection <strong>of</strong> fluoroacetamide in<br />

body fluid using gas chromatography-mass spectrometry after solid-phase microextraction. Journal <strong>of</strong><br />

Chromagraphy B: Analytical Technologies in the Biomedical and Life Sciences 802, 239-245.<br />

Keywords: fluoroacetamide/fluorine/blood/urine/analysis<br />

Abstract: A novel method for fast determination <strong>of</strong> fluoroacetamide, a kind <strong>of</strong> organic fluorine pesticide, in<br />

blood and urine samples was developed with acetamide as an internal standard using gas<br />

chromatography/mass spectrometry (GC/MS) after solid-phase microextraction (SPME) technique. The<br />

SPME was performed by immersing a PDMS fiber <strong>of</strong> 100 mum coating thickness in a sample solution for<br />

25 min at 70degreesC with (CH3CH2)(4)NBr to improve the extraction efficiency. After a GC sample<br />

injection, the extracted fluoroacetamide was desorbed from the fiber for 4 min to perform the GC/MS<br />

detection with a HP-PLOT Q capillary column. The analytical conditions were optimized by examining<br />

systematically, the effects <strong>of</strong> experimental parameters on the ratio <strong>of</strong> characteristic ion peak areas <strong>of</strong><br />

fluoroacetamide to acetamide. Under optimal conditions, the ratio was proportional to the concentration <strong>of</strong><br />

fluoroacetamide ranging from 5.0 to 90 mug/ml with a detection limit <strong>of</strong> 1.0 mug/ml. The average recovery<br />

<strong>of</strong> fluoroacetamide in blood sample was 92.2%. The established method could be used for the fast and<br />

convenient measurement <strong>of</strong> fluoroacetamide in poisoned sample.<br />

Caithness, T. A. and Williams, G. R. (1971). Protecting birds from poisoned baits. New Zealand journal <strong>of</strong><br />

agriculture 122(6), 38-43.<br />

28


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: non-target species/birds<br />

Abstract: Techniques to protect birds from poisoning include the consideration <strong>of</strong> bait size and use <strong>of</strong> dyes.<br />

Calder, B. and Deuss, F. The effect <strong>of</strong> 1080 poisoning on bird populations in Motere, Pureora Forest Park,<br />

winter 1984. 1985.<br />

Ref Type: Unpublished Work<br />

Keywords: 1080/poisoning/birds/non-target species<br />

Calver, M. C. and King, D. (1986). <strong>Control</strong>ling vertebrate pests with fluoroacetate: lessons in wildlife<br />

management, bio-ethics and co-evolution. Journal <strong>of</strong> Biological Education 20, 257-262.<br />

Keywords: fluoroacetate/humans/livestock/predators<br />

Abstract: Pest management is one the most important aspects <strong>of</strong> applied ecology included in the school<br />

biology curricula. This reflects the need to regulate pest numbers to maximise agriculturla production,<br />

reduce damage to buildings, check the risk <strong>of</strong> spread <strong>of</strong> serious diseases <strong>of</strong> humans and domestic animals,<br />

and minimise the nuisance to people and livestock caused by some pests. Additionally, conservation<br />

policies sometimes involve culling predators or competitors <strong>of</strong> threatened species using pest control<br />

techniques. However, the discussions <strong>of</strong> pest control in biology textbooks are biased heavily towards the<br />

control <strong>of</strong> invertebrate and plant pests, while vertebrate pests are neglected. While no doubt motivated by<br />

the relative economic importance <strong>of</strong> vertebrate and invertebrate pests, this attitude prevents a<br />

comprehensive coverage <strong>of</strong> pest control issues. Compound 1080 (sodium mon<strong>of</strong>luoroacetate) was used as a<br />

vertebrate pesticide in the USA from the 1940s until its ban for use on Federal land in 1972, and it is still<br />

used widely on private lands. In Australia, it has been in increasing use since its introduction in the early<br />

1950s. This paper compares and contrasts the use <strong>of</strong> 1080 in both countries focusing on the aims and<br />

methods involved, the biological peculiarities <strong>of</strong> each system and the role <strong>of</strong> public opinion and pressure in<br />

determining the nature <strong>of</strong> 1080 use.<br />

Calver, M. C., McIlroy, J. C., King, D. R., Bradley, J. S., and Gardner, J. L. (1989). Assessment <strong>of</strong> an<br />

approximate lethal dose technique for determining the relative susceptibility on non-target species to 1080<br />

toxin. Australian wildlife research 16, 33-40.<br />

Keywords: acute toxicity/non-target species/approximate lethal dose/lethal dose/1080<br />

Calver, M. C., King, D. R., Bradley, J. L., Gardner, J. L., and Martin, G. (1989). An assessment <strong>of</strong> the<br />

potential target specificity <strong>of</strong> 1080 predator baiting in Western Australia. Aust.Wildl.Res. 16, 625-638.<br />

Keywords: 1080/baits/non-target species/mammals<br />

Abstract: The potential hazard <strong>of</strong> 1080 baiting for predators to 14 species <strong>of</strong> non-target mammals in the<br />

pastoral areas <strong>of</strong> Western Australia and a further six from Western Australia's Fitzgerald River National<br />

Park, was assessed by comparing projected doses <strong>of</strong> 1080 (based on consumption <strong>of</strong> non-toxic bait by<br />

captive animals in the absence <strong>of</strong> alternative food) with the approximate lethal dose <strong>of</strong> 1080 for each<br />

species. These figures suggested that individuals from 12 species were potentially at risk from crackle baits,<br />

while only individuals from Dasyurus hallucatus, Ningaui spp., Sminthopsis crassicaudata, Planigale<br />

maculata, one population <strong>of</strong> Leggadina forresti and one population <strong>of</strong> Sminthopsis ooldea were potentially<br />

endangered by meat baits.<br />

Tests using the native mammals Zyzomys argurus and Pseudomys hermannsbergensis and laboratory mice<br />

(Mus musculus) and laboratory rats (Rattus norvegicus) showed that individuals <strong>of</strong> all species reduced their<br />

consumption <strong>of</strong> toxic bait relative to non-toxic bait, although this did not prevent three <strong>of</strong> five rats and one<br />

<strong>of</strong> three P. hermannsbergensis from being killed.<br />

Cappenberg, T. E. (1974). Interrealtions between sulfate-reducing and methane-producing bacteria in<br />

bottom deposits <strong>of</strong> a fresh-water lake. II. Inhibition experiments. Antonie van Leeuwenhoek 40, 297-306.<br />

Keywords: bacteria/inhibition/fluoroacetate/toxicity<br />

Abstract: A possible substrate interrelationship between methane-producing and sulphtae-reducing bacteria<br />

has been studied in the bottom deposits <strong>of</strong> Lake Vechten. Inhibition <strong>of</strong> methnogenesis in mud samples by<br />

chlorine-containing analogues <strong>of</strong> methane resulted in accumulation <strong>of</strong> acetate. Fluoroacetate reduced the<br />

concentration <strong>of</strong> methane by about 75%.<br />

29


1080 Reassessment Application October 2006<br />

Appendix C<br />

Cappenberg, T. E. and Prins, R. A. (1974). Interrelations between sulfate-reducing and methane-producing<br />

bacteria in bottom deposits <strong>of</strong> a fresh-water lake. III. experiments with 14 -C labelled substrates. Antonie van<br />

Leeuwenhoek 40, 457-469.<br />

Keywords: bacteria/fluoroacetate/inhibition/toxicity<br />

Abstract: An ecological substrate relationship between sulfate-reducing and methane-producing bacteria in<br />

14-C labeled acetate and lactate as substrates. Fluoroacetate strongly<br />

mud <strong>of</strong> Lake Vechten has been studied in experiments using<br />

inhibited the formation <strong>of</strong> 14CO2 from [U-14C]-acetate and β-fluorolactate gave an inhibition <strong>of</strong> similar magnitude <strong>of</strong> the breakdown <strong>of</strong> [U-14C]-L-lactate to 14CO2<br />

thus confirming earlier results on the specific action <strong>of</strong> these inhibitors.<br />

Carrell, H. L., Glusker, J. P., Villafranca, J. J., Mildvan, A. S., Dummel, R. J., and Kun, E. (1970).<br />

Fluorocitrate inhibition <strong>of</strong> aconitase : relative configuration <strong>of</strong> inhibitory isomer by X-ray crystallography.<br />

Science 170, 1412-1414.<br />

Keywords: product chemistry/mode <strong>of</strong> action<br />

Abstract: The fluorocitrate isomer that is a strong inhibitor and inactivator <strong>of</strong> aconitase has been shown by<br />

x-ray crystallographic studies on the rubidium ammonium salt to have the configurations (1R:2R) or<br />

(1S:2S) 1-fluoro-2-hydroxy-1,2,3-propanetricarboxylic acid. A possible mechanism for the action <strong>of</strong><br />

fluorocitrate is proposed which involves the 1R:2R isomer suggested from biochemical data.<br />

Casper, H. H., McMahon, T. L., and Paulson, G. D. (1984). Sodium fluoroacetate levels in canine tissues.<br />

Proceedings <strong>of</strong> the Annual Meeting <strong>of</strong> the American Association <strong>of</strong> Veterinary Laboratory Diagnosticians<br />

26 (1983 Meeting), 155-160.<br />

Keywords: acute toxicity/non-target species/persistence in animals/sodium<br />

fluoroacetate/fluoroacetate/1080/poisoning/dogs/liver/kidney/secondary poisoning/analysis<br />

Abstract: Sodium fluoroacetate (1080) poisoning in dogs is a continuing problem. A recently developed<br />

assay for 1080 in tissue was applied to tissues from field cases <strong>of</strong> suspected 1080 toxicosis in dogs. The<br />

assay utilizes C14-1080 internal standards and capillary gas chromatography / mass spectrometry to give<br />

clear identification <strong>of</strong> 1080 levels down to 10 ppb tissue equivalent. The 1080 levels in tissues from field<br />

cases <strong>of</strong> 1080 toxicosis ranged from 45 to 5451 ppb for liver (n=11) and 55 to 297 ppb for kidney (n=5).<br />

There were no clear differences in liver 1080 levels for primary poisoning cases vs levels in suspected<br />

secondary poisoning cases. For routine diagnostic use a 1080 analysis must be reliable at the 20 ppb tissue<br />

level.<br />

Casper, H. H., McMahon, T. L., and Paulson, G. D. (1985). Capillary gas chromatographic-mass<br />

spectrometric determination <strong>of</strong> fluoroacetate residues in animal tissues. Journal <strong>of</strong> the Association <strong>of</strong><br />

Official Analytical Chemists 68, 722-725.<br />

Keywords: fluoroacetate/acetate/analysis<br />

Abstract: A method for the quantitative determination <strong>of</strong> fluoroacetate (FAC) (a rodenticide) residues in<br />

animal tissues is described. The procedure involves tungstic acid extraction, partitioning into ethyl acetate,<br />

evaporation <strong>of</strong> ethyl acetate, derivation with pentafluorobenzyl bromide (PFB), and analysis <strong>of</strong> the resulting<br />

derivative (PFB-FAC) by capillary gas chromatography-mass spectrometry (CGC-MS) with specific ion<br />

monitoring (SIM). The tungstic acid system extracted 96.8 +- 4.2% <strong>of</strong> the endogenous 14C-1080 residues<br />

in rat tissues. Recovery <strong>of</strong> FAC during the extraction, purification, and derivatization procedures is<br />

established by use <strong>of</strong> a 14C-FAC spike. 1,2-Dibromobenzene is used as an internal standard for the CGC-<br />

MS analysis. PFB-FAC is identified on the basis <strong>of</strong> comparative retention times and the relative intensities<br />

<strong>of</strong> m/z 257.9 and 181.0. PFB-FAC is quantitated by comparing the response at m/z 257.9 to a PFB-FAC<br />

standard curve. Routine sensitivity <strong>of</strong> the method allows determination <strong>of</strong> 10 ppb fluoroacetate in tissue<br />

Casper, H. H., Mount, M. E., Marsh, R. E., and Schmidt, R. H. (1986). Fluoroacetate residues in ground<br />

squirrel and coyote tissues due to primary or secondary 1080 poisoning. Journal <strong>of</strong> the Association <strong>of</strong><br />

Official Analytical Chemists 69, 441-442.<br />

Keywords: acute toxicity/secondary poisoning/mammals/persistence in animals/1080<br />

Abstract: Fluoroacetate residues in various tissues <strong>of</strong> 1080 poisoned ground squirrels and coyotes are listed.<br />

The tissues (excluding the stomach) <strong>of</strong> squirrels poisoned with an average <strong>of</strong> 0.8mg 1080/kg (low dose)<br />

contained from 182 to 1309 ppb Fluoroacetate. In squirrels poisoned with an average <strong>of</strong> 4.8 mg 1080/kg<br />

(high dose), the tissue residues ranged from 535 to 9754 ppb Fluoroacetate. Tissues from coyotes which<br />

died after consuming 1080 poisoned ground squirrels were also analyzed for fluoroacetate residues.<br />

30


1080 Reassessment Application October 2006<br />

Appendix C<br />

Residues in these coyote kidneys and livers ranged from less than 10 ppb to 95 ppb fluoroacetate. The<br />

residue findings in this research indicate that a diagnostic assay for 1080 in tissues must be reliable at 10<br />

ppb (or less) fluoroacetate.<br />

Casselton, L. A. and Casselton, P. J. (1974). Functional aspects <strong>of</strong> fluoroacetate resistance in Coprinus with<br />

special reference to acetyl-CoA synthetase deficiency. Molecular gen genetics 132, 255-264.<br />

Keywords: fluoroacetate/resistance/fungus<br />

Abstract: Mutants <strong>of</strong> Coprinus lagopus unable to utilise acetate were selected on a glucose medium<br />

containing the toxic analogue fluoroacetic acid. Tests for interallelic complementation between twenty-five<br />

differently isolated acu-1 mutants proved negative, indicating that the acetyl-CoA synthetase activity is<br />

carried on a single polypeptide.<br />

Cater, D. B. and Peters, R. A. (1961). The occurrence <strong>of</strong> renal changes resembling nephrosis in rats<br />

poisoned with fluorocitrate. British journal <strong>of</strong> experimental pathology 42, 278-289.<br />

Keywords: kidney/pathology/rats/poisoning/fluorocitrate/citric acid/aconitase/<strong>poisons</strong>/poison<br />

Abstract: The kidneys <strong>of</strong> rats dying 2 hr after 60 or 80 mg/kg fluorocitrate ip showed degeneration <strong>of</strong> the<br />

mitochondria in the cells <strong>of</strong> the proximal convoluted tubules with blockages <strong>of</strong> tehe tubules and distension<br />

<strong>of</strong> the Bowman's capsule with fluid. In rats killed, or dying, after 2 or more daily or alternative day doses,<br />

marked fatty change was observed in the cells <strong>of</strong> the proximal convoluted tubules, together with<br />

degeneration and loss <strong>of</strong> tubular cells. Rats dying in this group showed fatty degeneration in the walls <strong>of</strong><br />

the arcuate, interlobular and glomerular arteries. The histological picture resembled that found in the<br />

kidneys <strong>of</strong> patients dying with lipoid nephrosis. Similar changes were found in hepatoma-bearing rats<br />

treated with fluorocitrate, but not in the kidneys <strong>of</strong> heptoma-bearing rats injected with saline, fluoro-oleic<br />

acid or 1-deoxy-1-fluoroglycerol. Fluorocitrate produces a specific block in teh citric acid cycle at the<br />

aconitase stage. The various known causes <strong>of</strong> nephrosis in rats are discussed in relation to their action as<br />

mitochondrial <strong>poisons</strong><br />

Cerutti, V. F. and Peters, R A. (1969). Observations upon the effect <strong>of</strong> fluoroacetate and pyruvate upon the<br />

isolated atria from rat heart. Biochemical Pharmacology 18, 2264-2267.<br />

Keywords: fluoroacetate/heart/fluorocitrate/citrate<br />

Abstract: In these experiments with atria there was no support for the attractive idea that pyruvate reverses<br />

the action <strong>of</strong> fluorocitrate in causing accumulation <strong>of</strong> citrate; but it should be stressed that their<br />

observations were upon the whole heart. The failure to reverse is, however, consistent with earlier<br />

experiments. It appears, however, as if there can be some recovery by washing after a low dose <strong>of</strong><br />

fluoroacetate, which is enough to restore a return <strong>of</strong> the beat and improved inotropism. This may be due to<br />

washing out citrate. Nevertheless the general toxicity <strong>of</strong> fluoroacetate could account in part for the asthenic<br />

state observed by Peters and Morselli. regarding the interesting results with noradrenalin, these may be due<br />

to reactivation <strong>of</strong> phosphokinase on the lines described by Murad et al.<br />

Chandler, G. T., Bayer, R. J., and Crisp, M. D (2001). A molecular phylogeny <strong>of</strong> the endemic Australian<br />

genus Gastrolobium (Fabaceae: Mirbelieae) and allied genera using chloroplast and nuclear markers.<br />

American Journal <strong>of</strong> Botany 88, 1675-1687.<br />

Keywords: occurrence in nature<br />

Abstract: Gastrolobium is an endemic Australian genus that produces toxic sodium mon<strong>of</strong>luoroacetate. Past<br />

key morphological characters, such as fluoroacetate content and characters associated with pollination<br />

syndrome, are shown to be polyphletic, with fluoroacetate possibly a pleisomorphic condition lost in more<br />

derived species.<br />

Chandler, G. T., Crisp, M. D, Cayzer, L. W., and Bayer, R. J. (2002). Monograph <strong>of</strong> Gastrolobium<br />

(Fabaceae : Mirbelieae). Australian Systemic Botany 15, 619-739.<br />

Keywords: occurrence in nature/fluoroacetate<br />

Chapman, E. A. and Graham, D. (1974). The effect <strong>of</strong> light on the tricarboxylic acid cycle in green leaves.<br />

1. Relative rates <strong>of</strong> the cycle in the dark and the light. Plant Physiology 53, 879-885.<br />

Keywords: inhibition/fluoroacetate/persistence in plants<br />

Abstract: In excised leaves <strong>of</strong> mung bean (Phaseolus aureus [= Vigna radiata]), illumination with 0.043<br />

31


1080 Reassessment Application October 2006<br />

Appendix C<br />

gcal/cm min <strong>of</strong> white light gave a rate <strong>of</strong> respiration 11-fold greater than in darkness. Feeding 14CO2 or<br />

14C-labelled acids <strong>of</strong> the tricarboxylic acid cycle in darkness for 2 h labelled the mitochondrial pools <strong>of</strong><br />

cycle intermediates. 82% inhibition <strong>of</strong> apparent photosynthesis with 0.1mM 3-(3,4-dichlorophenyl)-1,1dimethyl-urea<br />

largely prevented internally derived 14CO2 fixation and under these conditions 14CO2<br />

evolution continued in the light at a similar rate to that in darkness, showing that light-induced nonphotosynthetic<br />

processes have no significant effect on endogenous dark respiration. The effect <strong>of</strong> malonate<br />

and fluoroacetate as inhibitors <strong>of</strong> the tricarboxylic acid cycle suggested that the cycle functions in the light<br />

at a rate similar to that in darkness except for a short initial inhibition<br />

Chaurasia, S. C. (1981). Efficacy <strong>of</strong> certain metabolic inhibitors against Phytophthora parastica var.<br />

piperina causing foot-rot and leaf-rot diseases <strong>of</strong> pan. Indian Journal <strong>of</strong> Mycology and Plant Pathology 11,<br />

155-156.<br />

Keywords: inhibition/fungus/sodium fluoroacetate/fluoroacetate/fluoride<br />

Abstract: Sodium fluoroacetate was comparatively less toxic to the growth <strong>of</strong> the pathogen than other<br />

fluoride compounds tested.<br />

Cheng, S.-C., Kumar, S., and Casella, G. A. (1972). Effects <strong>of</strong> fluoroacetate and fluorocitrate on the<br />

metabolic compartmentation <strong>of</strong> tricarboxylic acid cycle in rat brain slices. Brain research 42, 117-128.<br />

Keywords: mode <strong>of</strong> action/metabolism/Krebs cycle/brain<br />

Abstract: (1) The effects <strong>of</strong> fluoroacetate and fluorocitrate in striatum slices <strong>of</strong> the rat brain were studied<br />

after metabolizing 3 different labeled substrates in the presence <strong>of</strong> glucose. The concentration <strong>of</strong> citrate<br />

increased under the influence <strong>of</strong> these inhibitors; those <strong>of</strong> glutamine decreased and those <strong>of</strong> (-aminobutyrate<br />

increased only in the presence <strong>of</strong> fluorocitrate. These inhibitors did not affect acetylcholine synthesis.<br />

(2) The effect <strong>of</strong> these fluoroinhibitors on the labeling <strong>of</strong> intermediates was rather complicated. The<br />

specific radioactivity <strong>of</strong> various metabolites changed differently according to both the labeled substrate and<br />

the inhibitor. The effects <strong>of</strong> these fluoroinhibitors on the specific radioactivity ratios or<br />

citrate/acetylcholine, glutamine/glutamate, (-aminobutyrate/glutamine, and aspartate/glutamate were also<br />

discussed in the text. These changes in specific radioactivities and their rations were explained using a<br />

model with 3 metabolic compartments. The compartments were characterized by labeled substrate<br />

utilization and glutamate-glutamine pool sizes. Pyruvate entered primarily the large compartment with a<br />

large glutamate pool, and acetate and citrate each entered primarily a different small compartment with<br />

small glutamate pools. In addition, these changes suggested that fluoroacetate and fluorocitrate did not<br />

have completely similar effects.<br />

Chengxin, W. and Zhi, D. Rodent control in China. Dubock, A. C. 521-531. 1984. England, ICI Plant<br />

Protection Division, Fernhurst, Haslemere Surrey England. Proceedings <strong>of</strong> a Conference on the<br />

Organisation and Practice <strong>of</strong> Vertebrate Pest <strong>Control</strong>. 30 August- 3 September 1982. Elvetham Hall<br />

Hampshire England. 30-8-0082.<br />

Ref Type: Conference Proceeding<br />

Keywords: zinc phosphide/diphacinone/difenacoum/brodifacoum/lethal dose/sodium<br />

fluoroacetate/1080/fluoroacetamide/strychnine/chlorophacinone<br />

Chenoweth, M. B. and Gilman, A. (1946). Studies on the pharmacology <strong>of</strong> fluoroacetate I. Species<br />

response to fluoroacetate. Journal <strong>of</strong> pharmacology and experimental therapeutics 87, 90-103.<br />

Keywords: mode <strong>of</strong> action/metabolism/mammals/fluoroacetate/acute toxicity/symptoms<br />

Chenoweth, M. B. and Gilman, A. (1946). Pharmacology <strong>of</strong> fluoroacetate. Federation proceedings 5, 171.<br />

Keywords: acute toxicity/fluoroacetate<br />

Chenoweth, M. B. and St.John, E. F. (1947). Studies on the pharmacology <strong>of</strong> fluoroacetate III. Effects on<br />

the central nervous systems <strong>of</strong> dogs and rabbits. Journal <strong>of</strong> pharmacology and experimental therapeutics<br />

90, 76-82.<br />

Keywords: fluoroacetate/dogs/rabbits/welfare/symptoms/brain<br />

Abstract: Spike and dome waves <strong>of</strong> high voltage occurring at a 3 per second rate have been produced in the<br />

EEG <strong>of</strong> curarized dogs by the administartion <strong>of</strong> fluoroacetic acid. Six <strong>of</strong> 8 dogs receving intravenous<br />

injection <strong>of</strong> 0.05 to 1.0 mg/kg <strong>of</strong> fluroacetate (sodium salt or methyl ester) developed cerebral dysrythmias<br />

32


1080 Reassessment Application October 2006<br />

Appendix C<br />

strongly resembling clinical grand mal and petit mal seizures. Fourteen <strong>of</strong> 16 dogs receving intracranial<br />

injections <strong>of</strong> fluroacetate (sodium salt or methyl ester) <strong>of</strong> 41 to 250 per cent <strong>of</strong> the LD50 developed similar<br />

dysrythmias. No definite relation was found between the use or dosage <strong>of</strong> water or lipoid soluble fluoroacetates, the sex, age or size <strong>of</strong> the dog and the occurrence <strong>of</strong><br />

the petit mal type dysrythmias. The grand mal seizures were produced more frequently with larger doses. Rabbits, a species which can not be convulsed by the<br />

intravenous injection <strong>of</strong> fluoroacetate in any dosage, convulse when very small doses (40 and 80 per cent <strong>of</strong> the intravenous LD50) are injected intracranially.<br />

Chenoweth, M. B. and Gilman, A. (1947). Studies on the pharmacology <strong>of</strong> fluoroacetate II. Action on the<br />

heart. Bulletin <strong>of</strong> the U.S.Army Medical Department 7, 687-706.<br />

Keywords: fluoroacetate/heart/lethal dose/muscle/rabbits/herbivores/carnivores/mode <strong>of</strong> action<br />

Abstract: The circulatory changes produced in rabbit, pig, goat, horse and rhesus and spider monkeys by<br />

lethal doses <strong>of</strong> fluoroacetate were examined, and it is concluded that they result from the action <strong>of</strong> the drug<br />

on the heart. The actions <strong>of</strong> fluoroacetate on the heart are tw<strong>of</strong>old; (1) depression <strong>of</strong> the excitation and<br />

conduction systems and the development <strong>of</strong> myocardial foci <strong>of</strong> excitation and (2) the depression <strong>of</strong> the<br />

muscular system. The characteristic response to these actions varies between species. The most significant<br />

differences among species were (1) the absence <strong>of</strong> any effect upon auricular activity or auricoloventricular<br />

conduction and a tendency towards various forms <strong>of</strong> alternation which characterized the rabbit and the<br />

monkey (2) the minimum <strong>of</strong> ectopic rhythyms and alternation which characterized the cat (3) the absence<br />

<strong>of</strong> acute changes and the delayed development <strong>of</strong> idioventricular bradycardia which characterized the rat.<br />

Ventricular fibrillation is the cause <strong>of</strong> death in these species and is preceeded by numerous<br />

electrocardiographic changes, such as heterotopic rhythyms, S-T changes resembling coronary disease, AV<br />

and intraventricular conduction blocks and unrelated degrees <strong>of</strong> electrical and mechanical pulsus alternans.<br />

The action <strong>of</strong> fluoroacetate is considered to be on a specific metabolic system unevenly distributed<br />

throughout these species and on which the hearts <strong>of</strong> these species are dependent to a varying degree, or<br />

which is varyingly sensitive to fluoroacetate.<br />

Chenoweth, M. B. (1949). Mon<strong>of</strong>luoroacetic acid and related compounds. Pharmacological reviews 1, 383-<br />

424.<br />

Keywords: mode <strong>of</strong> action/acute toxicity/metabolism<br />

Abstract: Conversion <strong>of</strong> a metabolic intermediate into a very highly toxic compound by the introduction <strong>of</strong><br />

a single fluorine atom in a strategic position in the molecule has been described for a number <strong>of</strong><br />

compounds. It appears to be a useful method for producing agents with which the metabolic pathways can<br />

be differentiated in a large number <strong>of</strong> species with a minimum <strong>of</strong> effort, for it is evident that these agents<br />

act by virtue <strong>of</strong> their close resemblance to natural metabolites. As an example, the variation among species<br />

in response to mon<strong>of</strong>luoroacetic acid has ben related to certain definite differences in metabolism in the<br />

species studied.<br />

Chenoweth, M. B., Kandel, A., Johnson, L. B., and Bennett, D. R. (1951). Factors influencing fluoroacetate<br />

poisoning : practical treatment with glycerol monoacetate. Journal <strong>of</strong> pharmacology and experimental<br />

therapeutics 102, 31-49.<br />

Keywords: diagnosis/treatment/acute toxicity/pathology/sodium fluoroacetate/rabbits<br />

Abstract: 1. The ability <strong>of</strong> various chemical substances to prevent or reverse the toxic effects <strong>of</strong> sodium<br />

fluoroacetate has been studied in mice, rats, rabbits, dogs and rhesus monkeys (Macacca mulatta).<br />

2. Commercially available monoacetin containing about 60 per cent glycerol monoacetate has been found<br />

to be superior to any other substance yet tested for general use against fluoroacetate poisoning. Certain<br />

characteristics <strong>of</strong> its action have been described.<br />

3. Various factors such as water and electrolyte imbalance have been assigned distinct, but minor roles in<br />

the development <strong>of</strong> the phenomena <strong>of</strong> fluoroacetate poisoining.<br />

4. The ability <strong>of</strong> fluoroacetate to potentiate the depressant action <strong>of</strong> barbiturates has been observed and the<br />

autoprotective effect in rats has been further clarified.<br />

5. An outline has been presented, based upon experiments with monkeys, which may be helpful for the<br />

guidance <strong>of</strong> those treating human fluoroacetate poisoning.<br />

Chenoweth, M. B. Fluoroacetate: still a portal to comparative toxicology. Unknown , 1074. 1970.<br />

Ref Type: Abstract<br />

Keywords: fluoroacetate<br />

33


1080 Reassessment Application October 2006<br />

Appendix C<br />

Chi, C.-H., Chen, K.-W., Chan, S.-H., Wu, M.-H., and Huang, J.-J. (1996). Clinical presentation and<br />

prognostic factors in sodium mon<strong>of</strong>luoroacetate intoxication. Journal <strong>of</strong> toxicology : clinical toxicology<br />

34, 707-712.<br />

Keywords: diagnosis/treatment/acute toxicity/humans/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/poisoning/analysis/serum<br />

Abstract: Background: The diagnosis <strong>of</strong> sodium mon<strong>of</strong>luoroacetate intoxication in humans is usually based<br />

on a history <strong>of</strong> ingestion and clinical findings. Although several previous reports have described the clinical<br />

course and outcome <strong>of</strong> patients who ingested this drug, prognostic indicators <strong>of</strong> short-term survival are not<br />

available. Methods: A retrospective study <strong>of</strong> 38 consecutive cases <strong>of</strong> sodium mon<strong>of</strong>luoroacetate poisoning<br />

at the National Cheng Kung University Hospital, 1988-1993, to analyze the clinical findings and to predict<br />

mortality. Results: Seven <strong>of</strong> 38 patients (18%) died. The most common symptom was nausea or vomiting<br />

(74%). The most frequent ECG finding was nonspecific ST-T and T wave abnormalities (72%).<br />

Hypocalcemia (42%) and hypokalemia (65%) were the common electrolyte abnormalities. The clinical and<br />

laboratory characteristics were compared for the survival and mortality groups. Significant differences in<br />

hypotension, respiratory rate, pulse rate, creatinine, potassium, elevated alanine aminotransferase, pH,<br />

PCO2, APACHE II score, and subjective respiratory distress were noted. Discriminant analysis identified<br />

hypotension, increased serum creatinine, and decreased pH as the most important predictors <strong>of</strong> mortality,<br />

with sensitivity <strong>of</strong> 86% and specificity <strong>of</strong> 96%. Conclusions: Hypotension and the early onset <strong>of</strong> metabolic<br />

acidosis and increased serum creatinine are associated with poor short-term survival. These prognostic<br />

variables can be useful in the care <strong>of</strong> patients with suspected sodium mon<strong>of</strong>luoroacetate intoxication. It is<br />

suggested that all such patients should be observed intensively for at least 48 h.<br />

Chi, C.-H., Lin, T.-K., and Chen, K.-W. (1999). Hemodynamic abnormalities in sodium mon<strong>of</strong>luoroacetate<br />

intoxication. Human and experimental toxicology 18, 351-353.<br />

Keywords: diagnosis/treatment/mode <strong>of</strong> action/acute toxicity/humans/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/resistance/cardiac<br />

Abstract: Hypotension is one <strong>of</strong> the most important predictors <strong>of</strong> mortality in sodium mon<strong>of</strong>luoroacetate<br />

(SMFA) intoxication. This paper reports the hemodynamic response in one fatal and another survival case<br />

<strong>of</strong> SMFA intoxication. Despite correction <strong>of</strong> hypovolemia and with inotropic support, the patients remained<br />

in shock. Hemodynamic observations have provided evidence that shock after SMFA intoxication is due to<br />

diminished systemic vascular resistance and increased cardiac output. This is the first report in which such<br />

an invasive hemodynamic investigation has been recorded in a clinical case <strong>of</strong> SMFA intoxication.<br />

Chidthiasong, A. and Conrad, R. (2000). Specificity <strong>of</strong> chlor<strong>of</strong>orm, 2-bromoethanesulfonate and<br />

fluoroacetate to inhibit methanogenesis and other anaerobic processes in anoxic rice field soil. Soil biology<br />

and biochemistry 32, 977-988.<br />

Keywords: fluoroacetate/soil/acetate/bacteria/degradation<br />

Abstract: Chlor<strong>of</strong>orm (CHCl3), 2-bromoethanesulfonate (BES) and fluoroacetate have frequently been used<br />

as methanogenic inhibitors in rice field soil and in other environments, but their effects on other microbial<br />

processes have not received sufficient attention. Therefore, we comparatively determined the effects <strong>of</strong><br />

CHCl3, BES and fluoroacetate on different microbial processes in rice field soil slurry upon incubation<br />

under anoxic conditions: on the reduction <strong>of</strong> the electron acceptors nitrate, ferric iron, sulfate; on the<br />

production <strong>of</strong> CH4 and CO2; on the temporal change <strong>of</strong> the electron donors H2, acetate and propionate; and<br />

on the turnover <strong>of</strong> [2- 14 C]acetate during the early reduction phase (day 7), and during the later<br />

methanogenic phase (day 30). The results demonstrate: (1) fluoroacetate inhibited acetate consumption by<br />

all microorganisms, (2) BES generally inhibited CH4 production, and (3) CHCl3 not only inhibited<br />

methanogenesis, but partially also acetate-dependent sulfate reduction, and perhaps H2-dependent<br />

homoacetogenesis. The specificity <strong>of</strong> the different inhibitors resulted in characteristic patterns <strong>of</strong> the<br />

temporal change <strong>of</strong> electron donors and acceptors and <strong>of</strong> CH4. The pattern <strong>of</strong> propionate change was<br />

consistent with production by fermenting bacteria and consumption by sulfate reducers either using sulfate<br />

or methanogens as electron acceptor. Sulfate reducers were also found to be important for acetate<br />

consumption during the early phase <strong>of</strong> soil anoxia. Later on, however, methanogenic acetate consumption<br />

was much more pronounced. The application <strong>of</strong> inhibitors with different specificity was helpful for<br />

elucidating the flow <strong>of</strong> carbon and electrons during degradation <strong>of</strong> organic matter in anoxic rice field soil.<br />

34


1080 Reassessment Application October 2006<br />

Appendix C<br />

Chumakova, I. V., Taran, I. F., and Dyatlov, A. I. Cytological studies <strong>of</strong> female fleas treated with<br />

chemosterilants and systemic <strong>poisons</strong>. g, 198-199. 1974. 14-5-1974.<br />

Ref Type: Conference Proceeding<br />

Keywords: <strong>poisons</strong>/poison/fluoroacetate/invertebrates/toxicity<br />

Abstract: Female fleas were treated by contact with 0.25, 0.5, 0.75 and 1% aqueous solutions <strong>of</strong> thiotepa<br />

(tiotef), and orally by feeding on white mice to which fenitrothion (Sumithion) or barium fluoroacetate had<br />

been given at 1.5, 3.0 or 9.0 mg/kg body weight. Resulting changes in the genital system were followed<br />

from the first to the fourteenth day <strong>of</strong> adult life. In females treated with 0.25% thiotepa, slight degenerative<br />

changes in the gonads were seen for 3-4 days, but thereafter the ovaries reverted to their normal form and<br />

functions. In those treated with 0.5% and 0.75% thiotepa, changes were noted on the second day.<br />

Development <strong>of</strong> the ovaries was delayed, and in 70-75% <strong>of</strong> females they showed resorption in different<br />

degrees. These changes were more evident in females that had been treated with a 1% solution. Fleas that<br />

had taken up systemic <strong>poisons</strong> from mice treated at 1.5-3.0 mg/kg showed no apparent changes in the<br />

gonads but laid a greater proportion <strong>of</strong> non-viable eggs than untreated females. Those that fed on mice that<br />

had been treated at 9.0 mg/kg showed delay in the development <strong>of</strong> the ovaries, complete resorption <strong>of</strong> the<br />

egg-cells or irreversible degenerative changes in the gonads<br />

Chung, H. M. (1984). Acute renal failure caused by acute mon<strong>of</strong>luoroacetate poisoning. Veterinary and<br />

human toxicology 26 Supplement 2, 29-32.<br />

Keywords: mode <strong>of</strong> action/diagnosis<br />

Abstract: NaFA produces toxic effects by metabolic conversion to fluorocitrate, inhibits Krebs' cycle and<br />

the formation <strong>of</strong> ATP, reduces energy supply to cells, and thus causes cellular dysfunction or degeneration.<br />

All body cells are potentially affected, although with different sensitivity. Acute renal failure was found in<br />

three out <strong>of</strong> our five cases, and two were in frank uremia. The ARF was reversible and may be either<br />

oliguric or non-oliguric. The causes <strong>of</strong> ARF were not apparent, but direct nephropathy or some other<br />

factors might be involved in the pathogenesis <strong>of</strong> ARF<br />

Cifarelli, A., Pepe, G., Paradisi, F., and Piccolo, D. (1979). The influence <strong>of</strong> some metabolic inhibitors on<br />

phagocytic activity <strong>of</strong> mouse macrophages in-vitro. Res.Exp.Med. 174, 197-204.<br />

Keywords: fluoride/sodium fluoroacetate/fluoroacetate/temperature/Krebs cycle/plasma/mode <strong>of</strong> action<br />

Abstract: The action <strong>of</strong> different metabolic inhibitors on phagocytosis by macrophages from mouse<br />

peritoneal exudate cultured in vitro was studied. The following metabolic inhibitors were tested: sodium<br />

iodacetate, sodium fluoride, sodium fluoroacetate, sodium melonate, 2-4-dinitrophenol, sodium azide,<br />

ouabain and cycloheximide, all at the concentration <strong>of</strong> 10-3 M. Iodoacetate caused a strong inhibitory<br />

effect on phagocytosis,confirming that glycolycis is the main source <strong>of</strong> energy for the phagocytic process.<br />

Fluoride, although it is an effective inhibitor <strong>of</strong> glycolysis, did not exert any effect. Sodium fluoride blocks<br />

anaerobic glycolysis only in vitro at an unphysiological temperature (0. degree. C). Fluoroacetate and<br />

malonate, 2 compounds which interfere with the Krebs cycle, did not inhibit phagocytosis; but the Krebs<br />

cycle activity is poorly developed in the macrophagic cells. Sodium azide and 2-4-dinitrophenol, 2<br />

inhibitors <strong>of</strong> oxidative phosphorylation, showed an effect on phagocytosis only after 3 h <strong>of</strong> contact with the<br />

cell cultures. Quabain blocked Na + and K + transport across the plasma membrane and it probably inhibited<br />

phagocytosis by interfering with the movements <strong>of</strong> the cell membrane. The mode <strong>of</strong> action <strong>of</strong><br />

cycloheximide on phagocytosis is uncertain. This compound inhibits the protein synthesis and it can<br />

perhaps act by preventing the renewal <strong>of</strong> the cell membrane.<br />

Clarke, D. D. and Nicklas, W. J. (1970). Tricarboxylic acid cycle metabolism in the brain. Effect <strong>of</strong><br />

fluoroacetate and fluorocitrate on the labelling <strong>of</strong> glutamate, aspartate, glutamine and y-aminobutyrate.<br />

Biochemistry Journal 120, 345-351.<br />

Keywords: metabolism/brain/Krebs cycle/biochemistry/fluoroacetate/fluorocitrate<br />

Abstract: The effect <strong>of</strong> fluoroacetate and fluorocitrate on the compartmentation <strong>of</strong> the glutamate-glutamine<br />

system was studied in brain slices with L-[U-14C]glutamate, L-[U-14C]aspartate, [1-14C]acetate and yamino[1-14C]butyrate<br />

as precursors and in homogenates <strong>of</strong> brain tissue with [1-14C]acetate. The effect <strong>of</strong><br />

fluoroacetate was also studied in vivo in mouse brain with [1-14C]acetate as a precursor. Fluoroacetate and<br />

fluorocitrate inhibit the labelling <strong>of</strong> glutamine from all precursors but affect the labelling <strong>of</strong> glutamate to a<br />

much lesser extent. This effect is not due to inhibition <strong>of</strong> glutamine synthetase. It is interpreted as being due<br />

to selective inhibition <strong>of</strong> the metabolism <strong>of</strong> a small pool <strong>of</strong> glutamate that preferentially labels glutamine.<br />

35


1080 Reassessment Application October 2006<br />

Appendix C<br />

Clarke, D. D. (1991). Fluoroacetate and fluorocitrate: mechanism <strong>of</strong> action. Neurochemical research 16,<br />

1055-1058.<br />

Keywords: metabolism/mode <strong>of</strong> action/fluoroacetate/fluorocitrate/aconitase<br />

Abstract: The concept <strong>of</strong> lethal synthesis as suggested by Peters is reviewed in the light <strong>of</strong> the more recent<br />

work in this area. It is suggested that fluorocitrate is a "suicide" substrate for aconitase rather than a<br />

competitive inhibitor as originally suggested. The use <strong>of</strong> these substances to study glial-neuronal<br />

relationships is considered<br />

Clear, M. Reports from New Zealand Food Safety Authority - red meat residue and species verification<br />

monitoring. Surveillance 30[2], 18-19. 2003.<br />

Ref Type: Magazine Article<br />

Keywords: residues/liver/pigs/possums/brodifacoum/1080<br />

Cohen, E. and Levinson, H. Z. (1974). The effect <strong>of</strong> fatty acids and their alpha-fluoro analogs on the<br />

feeding response and development <strong>of</strong> the hidebeetle Dermestes maculatus Deg. Zeitschrift fur Angewandte<br />

Entomologie 76, 98-105.<br />

Keywords: sodium fluoroacetate/fluoroacetate/inhibition/invertebrates<br />

Abstract: Studies in Israel showed that larvae and adults <strong>of</strong> Dermestes maculatus Deg. were attracted by<br />

palmitic and stearic acids and were repelled by caprylic acid, a lower homologue. Lauric acid, which<br />

strongly deterred the larvae from feeding, stimulated the adults to feed. Palmitic and stearic acids enhanced<br />

larval growth and metamorphosis, but caprylic and lauric acids inhibited them. The larvae and adults<br />

differed in their response to alpha -fluoro fatty acids. The former were invariably repelled by the fluoro<br />

analogues, but the latter fed readily on a diet containing alpha -fluorolaurate and alpha -fluorostearate. It<br />

appeared that the adults were incapable <strong>of</strong> distinguishing between fatty acids and their respective fluoro<br />

derivatives. Sodium fluoroacetate was very toxic to the larvae but alpha -fluoro fatty acids were relatively<br />

non-toxic, inhibiting growth only at a dietary level <strong>of</strong> 1%. This moderate effect was ascribed to inhibition<br />

<strong>of</strong> beta -oxidation, whereby the lethal fluorocaetate was not released<br />

Cohen, P. (1996). Protecting sheep puts birds at risk. New scientist 149, 5.<br />

Keywords: secondary poisoning/persistence in animals/birds<br />

Cole, B. T., Engel, F. L., and Fredericks, J. (1955). Sodium fluoroacetate diabetes: correlations between<br />

glycemia, ketonemia and tissue citrate levels. Endocrinology 56, 675-683.<br />

Keywords: sodium<br />

fluoroacetate/fluoroacetate/citrate/rats/heart/liver/spleen/kidney/muscle/poisoning/Krebs cycle/persistence<br />

in animals<br />

Abstract: Sodium fluoroacetate was administered intraperitoneally to fasted and fed rats. Hyperglycemia<br />

and ketosis developed within four hours. Ketosis persisted between 24-40 hours and hyperglycemia from<br />

40-64 hours in both groups. A single SFA poisoned rat exhibited a prolonged survival, dying on the 14th<br />

day <strong>of</strong> fasting with marked hyperglycemia and ketosis. The citrate content <strong>of</strong> the heart, liver, spleen,<br />

kidney, pancreas and gastrocnemius muscle was estimated in SFA posioned rats and found to correlate<br />

reasonably well with the hyperglycemia and ketosis. With the exception <strong>of</strong> spleen, citrate levels were all<br />

back to normal by 64 hours. Pretreatment with cortisone acetate prevented the ketosis <strong>of</strong> SFA poisoning<br />

and increased the hyperglycemia but did not modify the tissue citrate concentrations. These data are<br />

interpreted to indicate that the Krebs cycle blockade in the tissues in general plays a primary role in the<br />

etiology <strong>of</strong> SFA diabetes. The single observation <strong>of</strong> persistent diabetes, however leaves open the possibility<br />

<strong>of</strong> specific damage to insulin producing cells as a factor in the diabetes.<br />

Coleman, J. D., Montague, T. L., Eason, C. T., and Statham, H. L. The management <strong>of</strong> problem browsing<br />

and grazing mammals in Tasmania. LC9596/106, 1-74. 1997. Tasmania, Department <strong>of</strong> Primary Industry<br />

and Fisheries.<br />

Ref Type: Report<br />

Keywords: mammals/deer/rabbits/possums/goats<br />

Coleman, J. D., Morgan, D. R., and Sweetapple, P. J. Seasonal constraints on the use <strong>of</strong> aerially-sown baits<br />

loaded with 1080 to control possum populations. [LC9899/123], -21. 1999. Lincoln, Manaaki Whenua -<br />

36


1080 Reassessment Application October 2006<br />

Appendix C<br />

<strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract report.<br />

Ref Type: Report<br />

Keywords: aerial control/possums/field efficacy/1080<br />

Abstract: Objectives : To determine the probability <strong>of</strong> success <strong>of</strong> aerial possum control operations<br />

conducted over the early spring - autumn period in forest adjacent to pasture and representative <strong>of</strong> that<br />

present in Tb Vector Risk Areas.<br />

Conclusions : Bait acceptance by possums living near forest margins at Waitaha is poorer than that<br />

recorded from possums living deep in the forest; condition <strong>of</strong> possums over the period <strong>of</strong> the study<br />

appeared to be a poor predictor <strong>of</strong> bait acceptance; bait acceptance could not be predicted from the<br />

availability or use by possums <strong>of</strong> favoured natural foods; there is no strong evidence that baiting outside <strong>of</strong><br />

winter at Waitaha would result in an operational failure.<br />

Collier, D. N., Spence, C., Cox, M. J., and Phibbs, P. V. (2001). Isolation and phenotypic characterization<br />

<strong>of</strong> Pseudomonas aeruginosa pseudorevertants containing supressors <strong>of</strong> the catabolite repression controldefective<br />

crc-10 allele. FEMS Microbiology Letters 196, 87-92.<br />

Keywords: bacteria/enzyme/metabolism/fluoroacetate/fluoroacetamide<br />

Abstract: The amiE gene encodes an aliphatic amidase capable <strong>of</strong> converting fluoroacetamide to the toxic<br />

compound fluoroacetate and is one <strong>of</strong> many genes whose expression is subject to catabolite repression<br />

control in Pseudomonas aeruginosa. The protein product <strong>of</strong> the crc gene, Crc, is required for repression <strong>of</strong><br />

amiE and most other genes subject to catabolite repression control in this bacterium. When grown in a<br />

carbon source such as succinate, wild-type P. aeruginosa is insensitive to fluoroacetamide (due to the<br />

repression <strong>of</strong> amiE expression). In contrast, mutants harbouring the crc-10 null allele cannot grow in the<br />

presence <strong>of</strong> fluoroacetamide (due to lack <strong>of</strong> repression <strong>of</strong> amiE). Selection for succinate-dependent,<br />

fluoroacetamide-resistant derivatives <strong>of</strong> the crc-10 mutant yielded three independent pseudorevertants<br />

containing suppressors that restored a degree <strong>of</strong> catabolite repression control. Synthesis <strong>of</strong> Crc protein was<br />

not reestablished in these pseudorevertants. All three suppressors <strong>of</strong> crc-10 were extragenic, and all three<br />

also suppressed a δcrc: :tetA allele. In each <strong>of</strong> the three pseudorevertants, catabolite repression control <strong>of</strong><br />

amidase expression was restored. Catabolite repression control <strong>of</strong> mannitol dehydrogenase production was<br />

also restored in two <strong>of</strong> the three isolates. None <strong>of</strong> the suppressors restored repression <strong>of</strong> glucose-6phosphate<br />

dehydrogenase or pyocyanin production.<br />

Collins, D. (1983). Evaluation <strong>of</strong> a routine method for determining sodium fluoroacetate (compound 1080)<br />

residues in poison baits. New Zealand journal <strong>of</strong> science 26, 283-286.<br />

Keywords: high-performance liquid chromatography/bait degradation/1080/sodium fluoroacetate<br />

Abstract: A total fluorine method routinely used for measuring sodium fluoroacetate (compound 1080 or<br />

1080) in poison baits was evaluated by using a more specific high performance liquid chromatographic<br />

(HPLC) technique. The rountine method accurately measures 1080 in unweathered baits and adequately<br />

estimates the level in baits during the early stages <strong>of</strong> weathering. In well weathered baits with levels <strong>of</strong><br />

1080 below 100 mg/kg the rountine method always overestimates the amount <strong>of</strong> 1080 present. Further<br />

investigation showed that most <strong>of</strong> the overestimation could be attributed to thepresence <strong>of</strong> inorganic<br />

fluoride which is not distinguished from 1080 by the rountine method. Production <strong>of</strong> fluoride from 1080<br />

within a poison bait has not previously been suggested as a contributing factor in bait detoxification<br />

Collins, D. M., Fawcett, J. P., and Rammell, C. G. (1981). Determination <strong>of</strong> sodium fluoroacetate<br />

(Compound 1080) in poison baits by HPLC. Bulletin <strong>of</strong> environmental contamination and toxicology 26,<br />

669-673.<br />

Keywords: high-performance liquid chromatography/sodium fluoroacetate/1080/liquid chromatography<br />

Abstract: Sodium fluoroacetate, also known as compound 1080, has been widely used as a poison for<br />

controlling various vertebrate pests. The field use <strong>of</strong> such a highly toxic compound necessitates the<br />

analysis <strong>of</strong> baits and tissues to monitor to exposure <strong>of</strong> operators, agricultural stock and protected wildlife<br />

species (RAMMELL and FLEMING 1978) Two general analytical methods are currently used, one based<br />

on a final fluorine estimation and the other on gas liquid chromatography (GLC). In the fluorine methods<br />

the sample extract is ashed and the fluorine determined either colorimetrically (AOAC 1980) or with a<br />

fluorideselective electrode (Peters and Baxter 1974). The fluorine methods, although sufficiently sensitive<br />

for most purposes, are necessarily nonspecific. The GLC methods which have been described are<br />

cumbersome and generally semi quantitative (Stahr et al. 1974, Peterson 1975, Stevens et al. 1976). An<br />

37


1080 Reassessment Application October 2006<br />

Appendix C<br />

improved GLC method using pentafluorobenzyl derivatisation and electroncapture detection was proposed<br />

recently (Okuno and Meeker 1980) but the presence <strong>of</strong> interfering peaks and low, variable recovering were<br />

a problem.<br />

The preparation <strong>of</strong> fluorescent derivatives <strong>of</strong> monocarboxylic acids using<br />

4bromomethyl7methoxycoumarin (BrMmc) and their separation by high performance liquid<br />

chromatography (HPLC) has recently been reported (Lam and Grushka 1978). We have adapted this<br />

method to the analysis <strong>of</strong> sodium fluoroacetate. A simple but efficient method for recovering this<br />

compound from baits is also described.<br />

Colvin, B. A., Hegdal, P. L., and Jackson, W. B. (1988). Review <strong>of</strong> non-target hazards associated with<br />

rodenticide use in the USA. Bulletin OEPP 18, 301-308.<br />

Keywords: non-target species/birds/mammals/secondary poisoning/USA/predators/raptors<br />

Connolly, G. and Burns, R. J. (1990). Efficacy <strong>of</strong> compound 1080 livestock protection collars for killing<br />

coyotes that attack sheep. Proceedings <strong>of</strong> the Vertebrate Pest Conference 14, 269-276.<br />

Keywords: ground control/efficacy/1080/livestock/livestock protection collar/USA/predators<br />

Connolly, G. (1993). Livestock protection collars in the United States, 1988-1993. In 'Eleventh Great Plains<br />

Wildlife Damage <strong>Control</strong> Workshop proceedings, April 26-29, 1993, Kansas City, Missouri'. pp. 25-33.<br />

(U.S. Dept. <strong>of</strong> Agriculture, Forest Service, Rocky Mountain Forest and Range Experiment Station: Fort<br />

Collins.)<br />

Keywords: ground control/target species/livestock/livestock protection collar/predators/USA/field efficacy<br />

Connolly, G. Development and use <strong>of</strong> compound 1080 in coyote control, 1944-1972. Proceedings <strong>of</strong> the<br />

21st Vertebrate Pest Conference, Visalia, California, March 2004, X. 2004.<br />

Ref Type: Conference Proceeding<br />

Keywords: 1080/fluoroacetate/toxicity/sodium<br />

fluoroacetate/rodents/rodent/baits/livestock/fish/wildlife/humans/occurrence in nature<br />

Abstract: Compound 1080 ® is a man-made sodium salt <strong>of</strong> fluoroacetic acid or fluoroacetate, which occurs<br />

in nature as the toxin in many species <strong>of</strong> poisonous plants. The toxicity <strong>of</strong> such plants had long been<br />

recognized, but the toxic agent was not identified as fluoroacetate until 1944. By that time, the pesticidal<br />

potential <strong>of</strong> synthesized sodium fluoroacetate (code number 1080-44) was being explored in the United<br />

States in a war time, crash program aimed at finding new rodenticides. Compound 1080, the main product<br />

<strong>of</strong> that program, proved to be the best rodenticide known up to that time. It was found to be even more<br />

toxic to canids than to rodents, so was used experimentally for coyote control beginning in November 1944.<br />

Compound 1080 was authorized for operational use in governmental predator control in 1946. Large meat<br />

baits, or bait stations, injected with 1080 solution and placed on livestock ranges in winter quickly became<br />

a preferred method for reducing coyote populations that preyed on sheep and cattle. The use <strong>of</strong> 1080 bait<br />

stations peaked in Fiscal Year (FY) 1963, when over 16,000 stations were placed by the U. S. Fish and<br />

Wildlife Service (FWS) Predator and Rodent <strong>Control</strong> (PARC) program. After 1963, numbers <strong>of</strong> 1080<br />

stations declined year by year to 1972 when the use <strong>of</strong> 1080 and other predacides on Federal lands and in<br />

Federal programs was stopped by President Nixon's Executive Order 11643, followed by Environmental<br />

Protection Agency (EPA) suspension and cancellation <strong>of</strong> registrations for 1080 and other predacides. The<br />

1080 cancellation was based partly on high potential hazard to humans, even though no human had ever<br />

been killed or seriously injured in connection with the use <strong>of</strong> this toxicant in coyote control.<br />

Paradoxically, most <strong>of</strong> the political agitation over Compound 1080 focused its use in predator control even<br />

though much greater amounts were used for rodent control. The total amount <strong>of</strong> 1080 sold in the U. S.<br />

during 1968-72, the last five years in which 1080 bait stations were used, was approximately 10,003 lb.<br />

Only 1.3 percent (129 lb) <strong>of</strong> that amount was used for predator control. The largest amount <strong>of</strong> 1080 used<br />

for coyote control in the United States in any one year was about 42.4 lb, in FY 1963.<br />

Cook, C. J. (1998). Serotonergic and cholecystokinin antagonists change patterns <strong>of</strong> response in rats (Rattus<br />

norvegicus) to oral sodium mon<strong>of</strong>luoroacetate. New Zealand veterinary journal 46, 76-78.<br />

Keywords: mode <strong>of</strong> action/welfare/rats/sodium mon<strong>of</strong>luoroacetate<br />

38


1080 Reassessment Application October 2006<br />

Appendix C<br />

Cook, C. J., Eason, C. T., Wickstrom, M., and Devine, C. D. (2001). Development <strong>of</strong> antidotes for sodium<br />

mon<strong>of</strong>luoroacetate (1080). Biomarkers 6, 72-76.<br />

Keywords: treatment/1080/pathology/antidote/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/dogs/CNS/cardiac/muscle/rats/blood/brain<br />

Cooke, J. A. (1976). The uptake <strong>of</strong> sodium mon<strong>of</strong>luoroacetate by plants and its physiological effects.<br />

Fluoride 9, 204-212.<br />

Keywords: persistence in plants/metabolism/fluoroacetate/fluoride/sodium fluoroacetate<br />

Abstract: The uptake and physiological effects <strong>of</strong> sodium fluoroacetate and sodium fluoride on a number <strong>of</strong><br />

plant species are compared. Both ionized fluoride and fluoroacetate were taken up by Helianthus annuus<br />

although the patterns <strong>of</strong> distribution differed. Fluoride accumulated mainly in the root but a small<br />

percentage was translocated to the shoot causing premature senescence <strong>of</strong> the leaves. Fluoroacetate,<br />

however, was translocated to the shoot with little accumulation in the root. On a µgF/ml basis, the<br />

fluoroacetate solutions were more toxic reducing dry weight and producing leaf necrosis. However,<br />

fluoroacetate did not have the the rapid effect on the water balance <strong>of</strong> the plants shown by fluoride. The<br />

significance <strong>of</strong> the metabolism <strong>of</strong> fluoroacetate is discussed in relation to these physiological studies.<br />

Corr, P. V. and Martire, P. (1971). Leaching by rain <strong>of</strong> sodium fluoroacetate ("1080") from baits used for<br />

rabbit control. Australian journal <strong>of</strong> experimental agriculture and animal husbandry 11, 278-281.<br />

Keywords: bait degradation/sodium fluoroacetate/1080<br />

Abstract: This paper reports experiments concerned with the loss <strong>of</strong> 1080 from a new type <strong>of</strong> pellet bait<br />

made from a mixture <strong>of</strong> pollard, bran, and molasses (PBM) and compared this with carrot and oat baits.<br />

The effect <strong>of</strong> different amounts <strong>of</strong> poison applied to baits in different ways was also studied. The<br />

experiments were done at Frankston (25 miles south east <strong>of</strong> Melbourne), Victoria in 1965 and 1966. The<br />

results for pellets at Frankston are compared with those for pellets retrieved from the field during poisoning<br />

experiments.<br />

Corr, P. V. (1971). The acceptability and effectiveness <strong>of</strong> pellet bait for poisoning rabbits. Australian<br />

journal <strong>of</strong> experimental agriculture and animal husbandry 11, 407-414.<br />

Keywords: poisoning/rabbits/carrot/baits/field efficacy/1080<br />

Abstract: It is concluded that the specially prepared pellet baits are as effective for poisoning rabbits as<br />

carrot baits, better than oat baits, and generally satisfactory.<br />

Corsi, A. and Granata, A. L. (1967). Differential toxicity <strong>of</strong> fluoroacetate to heart, kidney and brain<br />

mitochondria <strong>of</strong> the living rat. Biochemical Pharmacology 16, 1083-1089.<br />

Keywords: mode <strong>of</strong> action/metabolism/pathology/fluoroacetate/heart/brain/kidney<br />

Abstract: Mitochondria were prepared from the heart, kidney and brain <strong>of</strong> rats intoxicated with<br />

fluoroacetate. Incubation with several substrates showed dpression <strong>of</strong> respiration <strong>of</strong> heart mitochondria<br />

with pyruvate and succinate, and depression <strong>of</strong> kidney mitochondria with pyruvate, succinate, citrate, βoxobutyrate<br />

and L-glutamate; no inhibition<strong>of</strong> respiration was detected in brain mitochondria.<br />

Phosphorylative capacity, as expressed by the P:O ratios, was not affected in any <strong>of</strong> the tissues. However, a<br />

reduction in respiratory control was observed in all cases.<br />

Cottral, G. E., Dibble, G. D., and Winton, B. (1947). The effect <strong>of</strong> sodium fluoroacetate ("1080"<br />

rodenticide) on white leghorn chickens. Poultry Science 26, 610-613.<br />

Keywords: fluoroacetate/birds/symptoms/sodium fluoroacetate/poisoning/1080/acute toxicity/lethal<br />

dose/mammals<br />

Abstract: The symptoms <strong>of</strong> sodium fluoroacetate ("1080") poisoning in chickens are cyanosis <strong>of</strong> the comb<br />

and wattles, depression, weakness, disinclination to eat or move about, distention <strong>of</strong> the crop with fluid and<br />

gas, edema <strong>of</strong> the wattles, dyspnea and moist rales. The necropsy findings on sodium fluoroacetate<br />

poisoning in chickens are hemorrage and edema <strong>of</strong> the lungs, petechial hemorrages in the pericardial and<br />

mesenteric fat, enteritis, congestion <strong>of</strong> the internal organs and ovarian hemorrage in laying birds. The most<br />

pronounced effect <strong>of</strong> "1080" is on the lungs, where it causes hemorrage and edema. All birds that died <strong>of</strong><br />

"1080" poisoning showed hemorrage and edema <strong>of</strong> the lungs therefore these lesions are considered<br />

diagnostic. The results obtained after the administration <strong>of</strong> 1080 to 28 birds <strong>of</strong> two age groups indicated the<br />

following dose levels: Maximum tolerant dose between 4.0 and 5.0 mg/kg, LD50 between 7.0 and 8.0<br />

39


1080 Reassessment Application October 2006<br />

Appendix C<br />

mg/kg and LD100 between 15.0 and 18.0 mg/kg. Laying hens appeared to be more susceptible to 1080<br />

poisoning than hens that were not laying. Chickens are considerably more resistant to 1080 poisoning than<br />

are many <strong>of</strong> the small mammals.<br />

Cox, R. B. and Zatman, L. J (1972). The effect <strong>of</strong> fluoroacetate on the growth <strong>of</strong> the facultative<br />

methylotrophs bacerium 5H2, Pseudomonas AMI and bacterium 5B1. Society for General Microbiology:<br />

Proceedings 6.<br />

Keywords: bacteria/fluoroacetate/inhibition/toxicity<br />

Crawford, M. A. (1963). The effects <strong>of</strong> fluoroacetate, malonate and acid-based balance on the renal<br />

disposal <strong>of</strong> citrate. Biochemical journal 88, 115-120.<br />

Keywords: metabolism/fluoroacetate/citrate/excretion/urine/biochemistry<br />

Curry, D. Model permit conditions for the use <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080). 1995. Wellington,<br />

Ministry <strong>of</strong> Health.<br />

Ref Type: Pamphlet<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080<br />

Dalrymple, B. P. and McSweeney, C. S. (1998). Manipulation <strong>of</strong> rumen function by the inoculation <strong>of</strong><br />

novel microorganisms. Outlook on Agriculture 27, 107-113.<br />

Keywords: toxicity/<strong>poisons</strong>/poison/fluoroacetate/bacteria/GMO<br />

Abstract: Some recent developments in the area <strong>of</strong> utilizing ruminal microorganisms for the modification<br />

and improvement <strong>of</strong> productivity in ruminants are described. The inoculants, designed for establishment in<br />

the new domestic ruminant host, have specific, superior or modified activities, but currently have a<br />

restricted geographical or species distribution. Current work has focused on three novel or augmented<br />

activities, namely: reducing the toxicity <strong>of</strong> particular plant <strong>poisons</strong>, increasing the utilization <strong>of</strong> plant fibre<br />

and the modification <strong>of</strong> protein supply. The most successful projects so far have tackled the detoxification<br />

<strong>of</strong> the plant <strong>poisons</strong>, mimosine and fluoroacetate, but projects aimed at increasing the utilization <strong>of</strong> plant<br />

fibre are now well advanced. Molecular techniques have significantly assisted in the identification,<br />

differentiation and tracking <strong>of</strong> organisms and are essential for the construction <strong>of</strong> modified organisms<br />

Daniel, M. J. (1962). <strong>Control</strong> <strong>of</strong> introduced deer in New Zealand. Nature 194, 527-528.<br />

Keywords: deer/1080/persistence in animals/efficacy/field efficacy<br />

Daniel, M. J. Early trials with sodium mon<strong>of</strong>luoroacetate (Compound 1080) for the control <strong>of</strong> introduced<br />

deer in New Zealand. Technical Paper No. 51, O.D.C. 414.11, -27. 1966. Wellington, Forest <strong>Research</strong><br />

Institute, New Zealand Forest Service.<br />

Ref Type: Report<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/deer/lethal dose/birds/non-target<br />

species/symptoms/welfare<br />

Abstract: More than 100 baiting and poison trials using sodium mon<strong>of</strong>luoroacetate (compound 1080)<br />

carried out by the New Zealand Forest Service from 1957 to 1961 on fallow, red and sika deer, are<br />

described in some detail. Toxicity ratings varied from 1/4 lb to 1 lb (0.11 - 0.45 kg) <strong>of</strong> 1080 per 1,000 lb<br />

(454 kg) <strong>of</strong> chopped carrot bait, apparently the bait most favoured by these species <strong>of</strong> deer. If the LD50 for<br />

deer is similar to that for sheep (0.45 mg per 1 kg <strong>of</strong> body weight) a lethal dose for a 11lb (50 kg) deer<br />

would be contained in some 1.5 oz (40 g) <strong>of</strong> toxic carrot at the toxicity levels used. Some deer in the trials<br />

consumed more than 4 lb (1.8 kg) <strong>of</strong> toxic carrot, which would have contained well over 30 lethal doses.<br />

More than 500 deer were poisoned on grassy river flats and at least 40 in Noth<strong>of</strong>agus forest edges. The<br />

danger to native and exotic birds does not appear to be nearly as great as was anticipated. These trials<br />

indicate that large concentrations <strong>of</strong> deer on open clearings and in forest edges can be effectively reduced<br />

by the use <strong>of</strong> 1080 in carrot bait. It appears unlikely at this stage, however, that this technqiue will<br />

supersede hunting as an econmic method <strong>of</strong> deer control in most <strong>of</strong> New Zealand's 14,000,000ac<br />

(5,700,000 ha) <strong>of</strong> indigenous watershed-protection and production forests, or in the 1,000,000 ac (405, 000<br />

ha) <strong>of</strong> exotic production forests.<br />

40


1080 Reassessment Application October 2006<br />

Appendix C<br />

David, W. A. L. (1950). Sodium fluoroacetate as a systemic and contact insecticide. Nature 165, 493-494.<br />

Keywords: acute toxicity/persistence in plants/invertebrates/sodium fluoroacetate/fluoroacetate<br />

David, W. A. L. and Gardiner, B. O. C. (1951). Investigations on the systemic insecticidal action <strong>of</strong> sodium<br />

fluoroacetate and <strong>of</strong> three phosphorus compounds on Aphis fabae Scop. Annals <strong>of</strong> applied biology 91-110.<br />

Keywords: acute toxicity/invertebrates/persistence in plants/sodium fluoroacetate/fluoroacetate/systemic<br />

toxicity/persistence in soil<br />

Abstract: The general insecticidal properties <strong>of</strong> bis (bis-dimethylamino phosphonus) anhydride, bis<br />

(dimethylamino) fluorophosphine oxide, diethyl paranitro-phenyl phospahte (E600) and sodium<br />

fluoroacetate are described. All are toxic to aphids when infested planst are dipped in solutions. Although<br />

this is thought to be a contact action the possibility that the materials are first absorbed by the leaves and<br />

that the aphids are killed by imbibing toxic sap is not excluded. At the lowest concentrations giving a<br />

complete kill <strong>of</strong> aphids, the anhydride is the most persistently effective <strong>of</strong> the four compounds. E600 is the<br />

most phytotoxic compound. When applied to the roots the order <strong>of</strong> decreasing toxicity <strong>of</strong><br />

acetate>oxide>anhydride>E600 in sand and soil, and acetate>oxide>anhydride=E600 in culture solution.<br />

The anhydride and acetate are more persistent in the plants than the oxide and E600. The amrgin <strong>of</strong> safety<br />

between insecticidal dosage and phyocidal dosage is appreciably larger with the acetate than with the other<br />

three compounds. When equal dosages are administered to plants by the cut tap root technique the order <strong>of</strong><br />

decreasing toxicity to aphids is seen to be acetate>oxide>E600>anhydride. All compounds, except possibly<br />

E600 appear to be absorbed by the intact roots <strong>of</strong> the plants. Systemic insecticidal action following<br />

application made to leaves <strong>of</strong> the broad bean is easy to demonstrate with the acetate, demionstrable with<br />

difficulty with the anhydride and not at all with E600 and the oxide. Sodium fluoroacetate is an extremely<br />

effective systemic insecticide whether applied to the leaves or the roots <strong>of</strong> the broad bean. It is apparently<br />

not phytotoxic at several times the concentration necessary for insecticidal action but may prove to be too<br />

generally toxic or persistent for practical use.<br />

David, W. A. L. and Gardiner, B. O. C. (1953). The systemic insecticidal action <strong>of</strong> sodium fluoroacetate<br />

and <strong>of</strong> three phosphorus compounds on the eggs and larvae <strong>of</strong> Pieris brassicae L. Annals <strong>of</strong> applied biology<br />

40, 403-417.<br />

Keywords: acute toxicity/invertebrates/persistence in plants/sodium fluoroacetate/fluoroacetate/systemic<br />

toxicity<br />

David, W. A. L. and Gardiner, B. O. C. (1954). The systemic insecticidal action <strong>of</strong> certain compounds <strong>of</strong><br />

fluorine and <strong>of</strong> phosphorus on Phaedon cochleariae Fab. Annals <strong>of</strong> applied biology 41, 261-270.<br />

Keywords: acute toxicity/invertebrates/persistence in plants/fluorine/systemic toxicity<br />

David, W. A. L. and Gardiner, B. O. C. (1958). Fluoroacetamide as a systemic insectide. Nature 181 ,<br />

1810.<br />

Keywords: fluoroacetamide/efficacy/invertebrates/systemic toxicity<br />

David, W. A. L. and Gardiner, B. O. C. (1966). Persistence <strong>of</strong> fluoroacetate and fluoroacetamide in soil.<br />

Nature 209, 1367-1368.<br />

Keywords: persistence in soil/fluoroacetate/fluoroacetamide/soil<br />

De Meyer, R. and De Plaen, J. (<strong>1964</strong>). An approach to the biochemical study <strong>of</strong> teratogenic substances on<br />

isolated rat embryo. Life sciences 3, 709-713.<br />

Keywords: regulatory toxicology/mammals/rodents/teratogenicity/sodium fluoroacetate/developmental<br />

toxicity/reproductive effects<br />

Abstract: The genesis <strong>of</strong> congenital malformations, especially those induced by drugs, has long been a<br />

clinical enigma. In the rat, we have been able to demonstrate the teratogenic activity <strong>of</strong> three substances, all<br />

<strong>of</strong> which can specifically affect carbohydrate metabolism. Carbutamide, administered by stomach tube at a<br />

dose <strong>of</strong> 500 mg/day on the 9th and 10th days <strong>of</strong> pregnancy, induces cleft palate and microphthalmia or<br />

anophthalmia in nearly 100% <strong>of</strong> the embryos. The intramuscular injection <strong>of</strong> 2-deoxyglucose at a dose <strong>of</strong><br />

120 mg/day during the 9th and 10th day <strong>of</strong> pregnancy produces resorption in 17 out <strong>of</strong> 54 foetuses and<br />

foetal anomalies, such as cleft palate or forelimb anomalies in 17 out <strong>of</strong> those surviving. Sodium<br />

41


1080 Reassessment Application October 2006<br />

Appendix C<br />

fluoroacetate, 600 micrograms given intraperitoneally on the 9th day, causes eye anomalies, syndactylia<br />

and evisceration.<br />

De Moraes-Moreau, R. L., Haraguchi, M., Morita, H., and Palermo-Neto, J. (1995). Chemical and<br />

biological demonstration <strong>of</strong> the presence <strong>of</strong> mon<strong>of</strong>luoroacetate in the leaves <strong>of</strong> Palicourea marcgravii St<br />

Hil. Brazilian journal <strong>of</strong> medical and biological research 28, 685-692.<br />

Keywords: mode <strong>of</strong> action/occurrence in nature/product chemistry/acute toxicity/NMR/mon<strong>of</strong>luoroacetic<br />

acid/symptoms/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/rats<br />

Abstract: Cattle losses in Brazil have been attributed to Palicourea marcgravii St. Hil., a toxic plant for<br />

cattle. The crude extract from the leaves <strong>of</strong> P. marcgravii was successively fractionated using solvents with<br />

different polarities to determine whether mon<strong>of</strong>luoroacetic acid and/or some other substance present in the<br />

leaves maybe responsible for the acute symptoms caused by the plant. Authentic sodium mon<strong>of</strong>luoroacetate<br />

(SMFA) was used for comparison. The only P. marcgravii fraction which induced seizures and death in<br />

intoxicated rats was water soluble. The signs and symptoms induced in the animals by the crude extract and<br />

water-soluble fraction were the same as induced by SMFA and included tonic seizures and other actions on<br />

the CNS. The close-lethality and dose-latency to the 1st seizure curves constructed for the water-soluble<br />

fraction <strong>of</strong> the leaf extract (30-100 mg/kg) and SMFA (0.6-3.0 mg/kg) were parallel. Five animals per dose<br />

were used. The potency ratio <strong>of</strong> SMFA in relation to the water-soluble fraction <strong>of</strong> the leaf extract was 53.8<br />

(dose-lethality curve) and 64.1 (dose-latency to the 1st seizure curve). The water-soluble fraction contained<br />

a substance with hRf = 20 which was the same as that <strong>of</strong> authentic SMFA. The F-19 NMR spectra <strong>of</strong><br />

authentic SMFA and the P. marcgravii water-soluble fraction were identical. These data demonstrate the<br />

presence <strong>of</strong> SMFA in the water-soluble fraction <strong>of</strong> P. marcgravii leaves and show that mon<strong>of</strong>luoroacetate is<br />

the active principle responsible for the signs and symptoms <strong>of</strong> acute intoxication.<br />

de Oliveira, M. M. (1963). Chromatographic isolation <strong>of</strong> mon<strong>of</strong>luoroacetic acid from Palicourea<br />

marcgravii St.Hill. Experientia 29, 586-587.<br />

Keywords: occurrence in nature/analysis/mon<strong>of</strong>luoroacetic acid<br />

Abstract: 'Erva de rato' (rat weed) Palicourea marcgravii (Rubiaceae) whose natural habitat is in moist<br />

woodlands is a shrub found in several Brazilian states. It has long been known as one <strong>of</strong> the most toxic<br />

plants <strong>of</strong> our pastures, although its active principle had not previously been identified. The present note<br />

deals with the isolation <strong>of</strong> the substance mainly by chromatographic methods, and its identification as<br />

mon<strong>of</strong>luoroacetic acid.<br />

Demarchi, A. C., Menezes M.L., Mercadante A., and Vassillief I. (2001). Determination <strong>of</strong> the sodium<br />

mon<strong>of</strong>luoroacetate in serum by gas chromatography. Chromatographia 54, 402-404.<br />

Keywords: serum/sodium mon<strong>of</strong>luoroacetate/humans/poisoning/analysis<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (NAFAc) has been widely used for vertebrate pest control, such as<br />

rabbits in Australia. However NAFAc is extremely toxic to all vertebrates and its use is restricted. Although<br />

this compound is stringently restricted, the occurrence <strong>of</strong> accidental and homicidal poisoning is no everpresent<br />

possibility. The method developed in this work shows the applicability <strong>of</strong> SPE with alumina<br />

cartridges for the extraction <strong>of</strong> NAFAc from serum samples. The method is efficient with recoveries <strong>of</strong> at<br />

least 96.8% from spiked serum. The samples were subsequently derivatized with dicyclohexylcabodiimide<br />

(DCC), using 2,4-dichloroaniline (DCA), to make the product volatile for GC analysis.<br />

Deonier, C. C., Jones, H. A., and Incho, H. H. (1946). Organic compounds effective against larvae <strong>of</strong><br />

Anopheles quadrimaculatus : laboratory tests. Journal <strong>of</strong> economic entomology 39, 459-462.<br />

Keywords: aquatic species/non-target species/invertebrates<br />

Abstract: Of the 6000 organic compounds tested to determine their toxicity to fourth-instar larvae <strong>of</strong><br />

Anopheles quadrimaculatus Say only 175 gave mortalities <strong>of</strong> over 50 per cent in 58 hours at 1 p.p.m.<br />

Twenty-two compounds, in addition to DDT and related compounds, showed toxicity at 0.1 p.p.m. Acetic<br />

acid 1-trichloromethyl -2,2,-methylene bis (4,6-dichlorophenyl) diester; benzene hexachloride; and<br />

Synthetic 3956 were superior to the other compounds in their toxicity to anopheline larvae.<br />

Desmoulin, F., Gilard, V., Malet-Martino, M., and Martino, R. (2002). Metabolism <strong>of</strong> capecitabine, an oral<br />

fluorouracil prodrug: F-19 NMR studies in animal models and human urine. Drug metabolism and<br />

disposition 30, 1221-1229.<br />

42


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: 5-fluorouracil/fluoride/fluoroacetate/humans/kidney/liver/metabolism/NMR/plasma/rats/urine<br />

Abstract: Capecitabine (Xeloda; CAP) is a recently developed oral antineoplastic prodrug <strong>of</strong> 5-fluorouracil<br />

(5-FU) with enhanced tumor selectivity. Previous studies have shown that CAP activation follows a<br />

pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine (5'-<br />

DFCR) and 5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-FU preferentially in tumor tissues. In the<br />

present work, we investigated all fluorinated compounds present in liver, bile, and perfusate medium <strong>of</strong><br />

isolated perfused rat liver (IPRL) and in liver, plasma, kidneys, bile, and urine <strong>of</strong> healthy rats. Moreover,<br />

data obtained from rat urine were compared with those from mice and human urine. According to a low<br />

cytidine deaminase (3.5.4.5) activity in rats, 5'-DFCR was by far the main product in perfusate medium<br />

from IPRL and plasma and urine from rats. Liver and circulating 5'-DFCR in perfusate and plasma<br />

equilibrated at the same concentration value in the range 25 to 400 muM, which supports the involvement<br />

<strong>of</strong> es-type nucleoside transporter in the liver. 5'-DFUR and alpha-fluoro-beta-ureidopropionic acid (FUPA)<br />

+ alpha-fluoro-beta-alanine (FBAL) were the main products in urine <strong>of</strong> mice, making up 23 to 30% <strong>of</strong> the<br />

administered dose versus 3 to 4% in rat. In human urine, FUPA + FBAL represented 50% <strong>of</strong> the<br />

administered dose, 5'-DFCR 10%, and 5'-DFUR 7%. Since fluorine-19 nuclear magnetic resonance<br />

spectroscopy gives an overview <strong>of</strong> all the fluorinated compounds present in a sample, we observed the<br />

following unreported metabolites <strong>of</strong> CAP: 1) 5-fluorocytosine and its hydroxylated metabolite, 5-fluoro-6hydroxycytosine,<br />

2) fluoride ion, 3) 2-fluoro-3-hydroxypropionic acid and fluoroacetate, and 4) a<br />

glucuroconjugate <strong>of</strong> 5'-DFCR.<br />

Devine, C. D. and Cook, C. J. (1998). Bait shyness and its prevention in the rabbit Oryctolagus cuniculus L.<br />

New Zealand journal <strong>of</strong> zoology 25, 223-229.<br />

Keywords: bait shyness/rabbits/aversion/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/poisoning<br />

Abstract: Caged New Zealand white rabbits were examined for the development, and prevention, <strong>of</strong> a<br />

learned aversion to toxic feed. Two familiar feeds were <strong>of</strong>fered. One feed, a paste, contained sublethal<br />

amounts <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080); the other feed, cereal-based pellets, was unpoisoned. On<br />

initial poisoning, consumption <strong>of</strong> both feeds decreased, but more markedly for the 1080-dosed pastes.<br />

Suppressed feed consumption was observed for several days and may have been illness induced. A second<br />

poisoning elicited a significant depression <strong>of</strong> consumption <strong>of</strong> pastes but not pellets. The addition <strong>of</strong> a<br />

mixture <strong>of</strong> certain drugs (neurotransmitter antagonists) to the poisoned paste appeared to prevent the<br />

characteristic depression <strong>of</strong> this paste intake. We speculate that the drugs disrupted the associative process<br />

linking 1080 to recognisable attributes <strong>of</strong> the toxin or bait itself. The implications <strong>of</strong> these results on<br />

aversion formation in rabbits and pest control are discussed. [References: 29]<br />

Dieke, S. and Richter, C. P. (1946). Comparative assay <strong>of</strong> rodenticides on wild Norway rats. I. Public<br />

Health Rep. 61, 672-679.<br />

Keywords: assay/rats/zinc phosphide/Lethal Dose 50/acute toxicity<br />

Abstract: Eight rodenticides were bioassayed, using 406 recently trapped adult wild Norway rats.<br />

Unanaesthetised rats were given the various <strong>poisons</strong> suspended (or dissolved) in 10% acacia solution,<br />

through a metahl stomach tube. No significant seasonal variation was observed nor was there any sex<br />

variation (except in the case <strong>of</strong> red squill). The median lethal doses and their standard errors were found to<br />

be as follows, in mg/kg:<br />

1080 was 0.22 ± 0.01, strychnine sulphate was 4.8 ± 0.4, ANTU was 6.9 ± 0.5, thallium sulphate was 15.8<br />

± 0.9, zinc phosphide was 40.5 ± 2.9, arsenic trioxide was 138 ± 13, fortified red squill in females was 133<br />

± 10, fortified red squill in males was 276 ± 29 and barium carbonate was 1480 ± 340.<br />

Dietrich, L. S. and Shapiro, D. M. (1956). Fluoroacetate and fluorocitrate antagonism <strong>of</strong> tumor growth.<br />

Effect <strong>of</strong> these compounds on citrate metabolism in normal and neoplastic tissue. Cancer <strong>Research</strong> 16,<br />

585-588.<br />

Keywords: fluoroacetate/fluorocitrate/citrate/citric acid/brain/heart/kidney/aconitase/mode <strong>of</strong><br />

action/metabolism/mon<strong>of</strong>luoroacetate<br />

Abstract: Mon<strong>of</strong>luoroacetate and mon<strong>of</strong>luorocitrate both show carcinostatic activity against the<br />

adenocarcinoma 755 growth in C57BL mice. The administration <strong>of</strong> mon<strong>of</strong>luoroacetate markedly increased<br />

the citric acid levels in the 755 tumor and normal brain, heart and kidney tissue. Mon<strong>of</strong>luorocitrate<br />

administration raised the citrate concentration in the tumor and kidney tissue but had no effect on the citric<br />

acid levels in mouse brain or heart. In vitro studies on seven different experimental mouse neoplasms<br />

43


1080 Reassessment Application October 2006<br />

Appendix C<br />

indirectly indicate that all these tumor tissue possess aconitase activity. However, <strong>of</strong> all the neoplasms<br />

studied, adenocarcinoma 755 can efficiently convert fluoroacetate to fluorocitrate as measured by citric<br />

acid accumulation in the fluoroacetate poisoned tumor homogenates.<br />

Dilks, P. and Lawrence, B. (2000). The use <strong>of</strong> poison eggs for the control <strong>of</strong> stoats. New Zealand journal <strong>of</strong><br />

zoology 27.<br />

Keywords: poison/stoats/1080/lethal dose/field efficacy<br />

Abstract: Stoats (Mustela erminea) are an important predator <strong>of</strong> many forest bird species in New Zealand,<br />

and more effective methods for their control are being sought. Stoat control using Fenn traps has been<br />

shown to prevent predation on mohua (Mohoua ochrocephala), but this technique is labour-intensive and<br />

costly to use for protection <strong>of</strong> large areas <strong>of</strong> habitat. We evaluated 1080 delivered in eggs as a poison for<br />

control <strong>of</strong> stoats. The lethal dose has been determined by captive and field trials, but attempts to implement<br />

a large-scale control operation have given inconclusive results. To clarify the effectiveness <strong>of</strong> 1080 eggs as<br />

a control technique, we carried out further field trials with radio-tagged stoats in the Makarora Valley.<br />

Twenty animals were monitored by radio tracking, and data loggers and video cameras recorded their visits<br />

to bait stations. The precise time an individual stoat ate a poison egg could be determined from data logger<br />

and video information, and its fate was followed. Sixteen <strong>of</strong> twenty stoats were killed by 1080 eggs, three<br />

died <strong>of</strong> other causes and one remained alive at the end <strong>of</strong> the trials.<br />

Dobereiner, J. and Tokarnia, C. H. (1959). Poisoning <strong>of</strong> cattle by "erva de rato" (Palicourea marcgravii St.<br />

Hil.) in the Itapicuru Valley, Maranhao. Arq Institut Biol Anim 2, 83-91.<br />

Keywords: poisoning/livestock/occurrence in nature<br />

Douglas, G. W., Woodfield, B. R. G, and Tighe, F. G (1959). 1080 poison. A major weapon in rabbit<br />

control. The Journal <strong>of</strong> Agriculture (Victoria) 279-327.<br />

Keywords: 1080/poison<br />

Abstract: In the past four years poisoning with 1080 (sodium fluoroacetate) has become well established as<br />

a major method <strong>of</strong> rabbit destruction in Victoria.<br />

Early in 1953, successful trials with 1080, using apple as bait, were carried out in the Jack River and<br />

Yarram districts <strong>of</strong> Victoria. Kills were estimated to be between 90 and 99 per cent, <strong>of</strong> the rabbits in the<br />

areas where the poisoning was effected, and further trials in the Yarram district confirmed these estimates.<br />

Douglas, M. H. (1967). <strong>Control</strong> <strong>of</strong> thar (Hemitragus jemlahicus): evaluation <strong>of</strong> a poisoning technique. New<br />

Zealand journal <strong>of</strong> science 10, 511-526.<br />

Keywords: poisoning/1080/carrot/poison/secondary poisoning<br />

Abstract: An attempt was made to evaluate a poisoning technique utilizing compound 1080 and carrots for<br />

the control <strong>of</strong> thar. Pre-poisoning and post-poisoning counts were undertaken in three Zonesto define the<br />

effectiveness <strong>of</strong> the poison and pre-feeding. Zone I with no pre-feeds had an estimated kill <strong>of</strong> 11%, Zone II<br />

with one pre-feed an estimated kill <strong>of</strong> 30%, Zone III with two pre-feeds an estimated kill <strong>of</strong> 51%.<br />

Supplementary results were collected on secondary poisoning, identification <strong>of</strong> 1080 death, whether<br />

poisoning took a biased sample <strong>of</strong> the population, and biological data.<br />

DuBois, K. P. (1948). New rodenticidal compounds. Journal <strong>of</strong> the American Pharmaceutical Association<br />

37, 307-310.<br />

Keywords: sodium fluoroacetate/fluoroacetate/efficacy/antidote/poisoning/lethal dose/rodents<br />

Abstract: The toxicological and some <strong>of</strong> the pharmacological properties <strong>of</strong> Castrix, α-napthylthiourea, and<br />

sodium fluoroacetate are reviewed. Information relating to the toxicity and rodenticidal efficacy <strong>of</strong> 2chloro-4-dimethylamino-6-methylpyrimidine<br />

is reported. Sodium pentabarbital has been found to be<br />

effective as an antidote for Castrix poisoning.<br />

Dummel, R. J. and Kun, E. (1969). Studies with specific enzyme inhibitors. The Journal <strong>of</strong> Biological<br />

Chemistry 244, 2956-2969.<br />

Keywords: chemistry/enzyme/mode <strong>of</strong> action/analysis/fluorocitrate<br />

Abstract: Isolation <strong>of</strong> D and L isomers <strong>of</strong> erythro-fluorocitric acid was accomplished by first separation <strong>of</strong><br />

diastereomeric racemates as cyclohexamine salts <strong>of</strong> diethyl fluorocitrate. This was followed by resolution<br />

44


1080 Reassessment Application October 2006<br />

Appendix C<br />

<strong>of</strong> the erythro-diastereoisomer into optical isomers by fractional crystallization as (+) and (-)dioxyephidrine<br />

salts. Partial hydrolysis to the monoethyl ester <strong>of</strong> resolved fluorocitrate was acheived by<br />

guanidine carbonate and complete hydrolysis to the free acid in NaOH. Purification tothe final stage <strong>of</strong><br />

optically resolved free acids was carried out by fractionation as barium and cyclohexamine salts. Only the<br />

L isomer inhibited aconitase activity <strong>of</strong> rat kidney mitochondria.<br />

Dunn, D. and Berman, D. A. (1966). Oxidation <strong>of</strong> glucose-1-14C, glucose-6-14C and acetate-1-14C by rat<br />

ventricle strips during the inotropic action <strong>of</strong> fluoroacetate. Life sciences 5, 1881-1886.<br />

Keywords: fluoroacetate/heart/rodents/mode <strong>of</strong> action/metabolism/inhibition/muscle<br />

Abstract: The alterations in metabolism that occur in hearts poisoned with fluoroacetate have been studied<br />

by Williamson et al. They found that the depression <strong>of</strong> contractility appeared to correlate well with the<br />

metabolic inhibition. Under certain experimental conditions, however, fluoroacetate stimulates the force <strong>of</strong><br />

contraction <strong>of</strong> the heart. Katzung et al. demonstrated that fluoroactate stimulates contractility at low<br />

frequencies <strong>of</strong> stimulation and depresses contractility at high frequencies. Pasner demonstrated that<br />

fluoroacetate exerts a greater positive inotropic effect when the heart muscle is suspended in a medium<br />

containing a low calcium concentration than in high calcium.<br />

The present investigation was undertaken to study the effects <strong>of</strong> fluoroacetate on the metabolism <strong>of</strong><br />

electrically stimulated rat ventricle strips under conditions in which fluoroacetate stimulates contractility;<br />

i.e. the tissue was suspended in a medium containing a low calcium concentration and was electrically<br />

stimulated at a low frequency.<br />

Eanes, R. Z., Skilleter, D. N., and Kun, E. (1972). Inactivation <strong>of</strong> the tricarboxylate carrier <strong>of</strong> liver<br />

mitochondria by (-)-erythr<strong>of</strong>luorocitrate. Biochemical and biophysical research communications 46, 1618-<br />

1622.<br />

Keywords: metabolism/liver/fluorocitrate/inhibition/citrate/aconitase<br />

Eanes, R. Z. and Kun, E. (1974). Inhibition <strong>of</strong> liver aconitase isozymes by (-)-erythro-fluorocitrate.<br />

Molecular Pharmacology 10, 130-139.<br />

Keywords: metabolism/inhibition/liver/aconitase/biochemistry/enzyme/fluorocitrate/citrate<br />

Eason, C., Batcheler, D., and Wright, G. Environmental impact assessments on 1080 associated with<br />

possum control in the Waipoua Forest Sanctuary, Northland. FWE 91/8, -9. 1991.<br />

Ref Type: Report<br />

Keywords: 1080/non-target species/aerial control/possums/witholding<br />

period/mammals/invertebrates/analysis/persistence in water/persistence in animals<br />

Abstract: High concentrations <strong>of</strong> 1080 in mice suggested significant rodent mortality after possum control<br />

operations. Although some 1080 was present in insects, at the maximum concentration detected a 50-g bird<br />

would have to eat approximately 300-g <strong>of</strong> insect material at one session to be affected. Kauri snails were<br />

not contaminated. These analyses were undertaken on a small sample and should be treated accordingly.<br />

The sowing techniques did not affect bait size and integrity. The risk to non-target forest species, humans<br />

and stock was low after 28 days. However, baits from one area contained a significant amount <strong>of</strong> 1080 for 6<br />

weeks. The streams and rivers <strong>of</strong> the Waipoua Forest Snactuary were not comtaminated after the sowing <strong>of</strong><br />

1080 possum baits.<br />

Eason, C. and Gooneratne, R. An evaluation <strong>of</strong> the risk to man <strong>of</strong> secondary poisoning with sodium<br />

mon<strong>of</strong>luoroacetate (1080). New Zealand medical journal 106[949], 41. 1993.<br />

Ref Type: Abstract<br />

Keywords: secondary poisoning/poisoning/sodium<br />

mon<strong>of</strong>luoroacetate/1080/humans/possums/livestock/rabbits/witholding period<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) was introduced in 1954 for vertebrate pest control in New<br />

Zealand. It remains an essential tool for the containment <strong>of</strong> tuberculosis spread by possums and to reduce<br />

possum damage to crops and forests. Whilst stock should be removed from areas where this toxin is being<br />

used, there have been concerns that livestock may become contaiminated with 1080 after ingestion <strong>of</strong> a<br />

sublethal dose <strong>of</strong> toxin by eating a bait intended for a rabbit or a possum. To quantitate the risk <strong>of</strong> such an<br />

event, rabbits, sheep and goats have been orally dosed witj 0.1 mg/kg 1080 (approximately one quarter <strong>of</strong><br />

the LD50) and plasma pharmacokinetics and tissue concentrations <strong>of</strong> 1080 have been measured. The<br />

45


1080 Reassessment Application October 2006<br />

Appendix C<br />

plasma elimination t1/2 in rabbits, goats and sheep was 1, 5 and 11 hour respectively and tissue<br />

concentrations were consistently lower than plasma concentrations. All traces <strong>of</strong> 1080 were eliminated in<br />

one week. The rapid elimination <strong>of</strong> 1080 couples with destocking practices, suggests that the likelihood <strong>of</strong><br />

1080 residues occurring in meat for human consumption or export is extremely remote.<br />

Eason, C., Temple, W., Reeve, J. E., Waters, J. D, Fagerstone, K. A., and Savarie, P. J. An evaluation <strong>of</strong> the<br />

need for regulatory toxicology studies on sodium mon<strong>of</strong>luoroacetate (1080). <strong>Landcare</strong> <strong>Research</strong> Contract<br />

Report LC9596/06, -27. 1995.<br />

Ref Type: Report<br />

Keywords: regulatory toxicology/sodium mon<strong>of</strong>luoroacetate/1080<br />

Eason, C., Wickstrom, M., Milne, L., Warburton, B., and Gregory, N. (1998). Implications <strong>of</strong> animal<br />

welfare considerations for pest control research : the possum as a case study. In 'Ethical approaches to<br />

animal-based science ; proceedings <strong>of</strong> the Joint ANZCCART/NAEAC conference held in Auckland, New<br />

Zealand 19-20 September 1997'. pp. 125-130. (ANZCCART: Auckland.)<br />

Keywords: welfare/possums<br />

Abstract: Increasingly animal welfare considerations have influenced the focus <strong>of</strong> pest control research and<br />

the manner in which it is conducted. In this case study we review the trends and influences on research<br />

related to the Australian brushtail possum, considered the most damaging animal pest in New Zealand. The<br />

limited public acceptance for killing <strong>of</strong> animal pests such as rats and possums, carries the caveat that it<br />

must be done with minimal pain and distress. Finding control methods that are cost effective, target<br />

specific, and humane remains a major ethical and animal welfare issue. There is increasing emphasis on<br />

establishing the relative merits <strong>of</strong> different trap types and <strong>poisons</strong> (from a welfare perspective) and the<br />

development <strong>of</strong> non-lethal methods and biocontrol. We have initiated new research which will lead to an<br />

animal welfare audit <strong>of</strong> the existing six toxicants commonly used for possum control. The merits <strong>of</strong> this and<br />

all other pest control research will be judged increasingly from a welfare perspective, and research must<br />

initiate the use <strong>of</strong> animal management techniques which minimise pain or distress.<br />

Eason, C., Warburton, B., and Henderson, R. (2000). Toxicants used for possum control. In 'The brushtail<br />

possum : biology, impact and management <strong>of</strong> an introduced marsupial'. (Ed. T. L. Montague.) pp. 154-163.<br />

(Manaaki Whenua: Lincoln.)<br />

Keywords: acute toxicity/possums/welfare/non-target species/secondary poisoning/1080/brodifacoum<br />

Abstract: In New Zealand there are six toxicants currently registered for possum control: 1080 (sodium<br />

mon<strong>of</strong>luoroacetate), cyanide, cholecalciferol (Vitamin D), phosphorus, brodifacoum, and pindone. Their<br />

use for killing possums raises a variety <strong>of</strong> concerns including risks and persistence, which are <strong>of</strong>ten<br />

different for each toxicant because <strong>of</strong> the differences in their physical and chemical properties and their<br />

toxicological modes in action.<br />

The ideal toxicant for possum control should be inexpensive, usable by farmers, and humane. It should<br />

have an antidote and be degradable in soil and water. As far as possible it should be species-specific. It<br />

should not leave persistent residues in livestock and should have a low risk <strong>of</strong> primary or secondary<br />

poisoning in non-target species. It should be supported by a comprehensive database <strong>of</strong> efficacy,<br />

toxicology, and risk assessment studies that satisfy local concerns as well as national and international<br />

regulatory agencies. Such and ideal pesticide has not yet been identified and may never be. The<br />

advantages and disadvantages <strong>of</strong> the six toxicants currently used for possum control are summaried below<br />

ans some <strong>of</strong> the research questions being addressed regarding their safety and efficacy are outlined.<br />

Currently the range <strong>of</strong> toxicants and baits available allows those involved in possum control to select the<br />

most appropriate combination for sustained control <strong>of</strong> possums, provided they are familiar witht eh<br />

advantages and disadvantages <strong>of</strong> the different toxicants and baits.<br />

Eason, C. (2000). Persistence <strong>of</strong> 1080. Surveillance 20, 7.<br />

Keywords: 1080/persistence in animals/persistence in invertebrates/persistence in water<br />

Eason, C. and Wright, G. Water monitoring for contamination after aerial 1080 pest control operations - an<br />

update. He Korero Paihama - Possum <strong>Research</strong> News 16[December 2001], 10-11. 2001. <strong>Landcare</strong><br />

<strong>Research</strong>.<br />

46


1080 Reassessment Application October 2006<br />

Appendix C<br />

Ref Type: Magazine Article<br />

Keywords: 1080/persistence in water/aerial control<br />

Eason, C. and Wickstrom, M. Vertebrate Pesticide Toxicology Manual (Poisons). Department <strong>of</strong><br />

Conservation Technical Series 23, -122. 2001. Department <strong>of</strong> Conservation, PO Box 10-420, Wellington,<br />

New Zealand.<br />

Ref Type: Report<br />

Keywords: <strong>poisons</strong><br />

Eason, C. and O'Halloran, K. (2002). Biomarkers in toxicology versus ecological risk assessment.<br />

Toxicology in press.<br />

Keywords: humans/regulatory toxicology/toxicity/wildlife<br />

Abstract: Toxicity testing <strong>of</strong> drugs, pesticides, and hazardous compounds has substantially evolved into a<br />

battery <strong>of</strong> standardized tests conducted in a range <strong>of</strong> surrogate test organisms. The toxicity <strong>of</strong> these<br />

xenobiotics in terms <strong>of</strong> their LD50, LC50, ED50, EC50, MATC, LOEL, LOEC, NOEL or NOEC is extrapolated to humans and wildlife. Historical<br />

failures in the risk assessment process have been largely due to over reliance on regulatory toxicology and an "assembly line" mentality to toxicology. The<br />

importance <strong>of</strong> toxicokinetics, receptor studies and biomarkers are reviewed, firstly, with reference to toxicological incidences in drug development programmes, and<br />

secondly, with reference to improved environmental risk assessment <strong>of</strong> pesticides and other contaminants. Ecological risk assessments also require multidisciplinary<br />

skills to study the entry, distribution, and biological effect and fate <strong>of</strong> chemicals to fully characterise and understand the potential adverse implications <strong>of</strong><br />

contamination. Optimum integration <strong>of</strong> chemical measurements and biomarker responses is a challenge that will lead to an improved understanding <strong>of</strong> adverse<br />

effects and their significance in both human and ecological risk assessment.<br />

Eason, C. (2002). Sodium mon<strong>of</strong>luoroacetate (1080) risk assessment and risk communication. Toxicology<br />

181-182, 523-530.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080<br />

Abstract: Sodium mon<strong>of</strong>luroacetate (1080) is a vertebrate pesticide widely used for possum control in New<br />

Zealand. Fluoracetate is also a toxic component <strong>of</strong> poisonous plants found in Australia, South Africa,<br />

South America, and India. Because <strong>of</strong> its importance and effectiveness in pest control and the highly toxic<br />

nature <strong>of</strong> this compound, its acute sub-lethal and target organ toxicity have been extensively studied. In<br />

relation to its use as a pesticide its environmental fate, persistence, non-target impacts and general<br />

toxicology have been and continue to be extensively studied. Toxic baits must be prepared and used with<br />

extreme care, otherwise humans, livestock, and non-target wildlife will be put at risk. The high risk <strong>of</strong><br />

secondary poisoning <strong>of</strong> dogs is a cause for concern. 1080 acts by interfering with cellular energy<br />

production. Possums die from heart failure, usually within 6-18 h <strong>of</strong> eating baits. Long-term exposure to<br />

sub-lethal doses can have harmful effects and strict safety precautions are enforced to protect contractors<br />

and workers in the bait manufacturing industry. Considerable care is taken when using 1080 to ensure that<br />

the risks <strong>of</strong> using it are outweighed by the ecological benefits achieved from its use. When its use is<br />

controversial, risk communicators must take care not to trivialise the toxicity <strong>of</strong> the compound. The<br />

benefits <strong>of</strong> 1080 use in conservation, pest control, and disease control should be weighed up alongside the<br />

risks <strong>of</strong> using 1080 and other techniques for pest control.<br />

Eason, C. T. and Frampton, C. M. (1991). Acute toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) baits to feral<br />

cats. Wildlife research 445-449.<br />

Keywords: acute toxicity/cats/field efficacy/welfare/1080<br />

Abstract: Feral cat populations have had a devastating effect <strong>of</strong> many native wildlife species. As part <strong>of</strong> a<br />

program to evaluate improved predator control, feral cants were observed after they had ingested a polymer<br />

bait loaded with 0.4-1.6mg sodium mon<strong>of</strong>luoroacetate (1080) per 1-g bait, equivalent <strong>of</strong> doses <strong>of</strong> 0.1-1.3<br />

mg per kg body weight. Deaths occurred with 0.6 mg per bait and all higher doses. With the highest dose<br />

all animals died within 24 h. An approximate oral LD50 <strong>of</strong> 0.28 mg per kg (0.07-0.49) and LD90 <strong>of</strong> 0.35<br />

mg per kg (0.14-0.56) were calculated (with 95% confidence limits). Main symptoms were disorientation<br />

and lethargy, followed by death. A dose <strong>of</strong> 2 mg 1080 per bait is recommended as a humane and lethal<br />

poison for feral cats.<br />

Eason, C. T. (1991). Cholecalciferol as an alternative to sodium mon<strong>of</strong>luoroacetate (1080) for poisoning<br />

possums. Proceedings <strong>of</strong> the New Zealand Weed and Pest <strong>Control</strong> Conference 44, 35-37.<br />

Keywords: possums/non-target species/1080/acute toxicity<br />

47


1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Large-scale possums control in New Zealand is dependent on the use <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080). Although 1080 is highly effective, its use is restricted and there is public<br />

pressure to find alternatives. An acute toxicity programme has been set up to identify safer, humane, and<br />

more target-specific toxins. Possums ere dosed with a new rodenticide, cholecalciferol (Vitamin D3).<br />

Interim results indicated that cholecalciferol has and LD90 <strong>of</strong> approx. 20-50mg/kg in the possum.<br />

Eason, C. T., Wright, G. R., and Fitzgerald, H. (1992). Sodium mon<strong>of</strong>luoroacetate (1080) water-residue<br />

analysis after large-scale possum control. New Zealand journal <strong>of</strong> ecology 16, 47-49.<br />

Keywords: persistence in water/1080/possums/aquifer<br />

Abstract: Two major control operations were conducted in New Zealand in 1990 using aerially sown baits<br />

containing the poison sodium mon<strong>of</strong>luoroacetate (1080) [sodium fluoroacetate] against (1) brushtail<br />

possums (Trichosurus vulpecula) in kauri (Agathis australis) mixed hardwood forests <strong>of</strong> Waipoua Forest<br />

Sanctuary, and (2) against brushtail possums and rock wallabies (Petrogale penicillata) in the pohutukawa<br />

(Metrosideros excelsa) forests on the volcanic cone <strong>of</strong> Rangitoto Island. This note briefly reports the results<br />

<strong>of</strong> water-residue analyses carried out to determine the fate <strong>of</strong> 1080 in waterways. In Waipoua, streams and<br />

rivers were monitored for 4 months after 100 t <strong>of</strong> 1080 possum baits were sown over 17 000 ha <strong>of</strong> forest. At<br />

Rangitoto Island, surface and ground water samples were analysed for 6 months after 20 t <strong>of</strong> 1080 possum<br />

baits were sown over the 2300 ha island. No 1080 was detected in the streams and rivers <strong>of</strong> the Waipoua<br />

forest or the surface or ground water <strong>of</strong> Rangitoto Island.<br />

Eason, C. T. (1992). The evaluation <strong>of</strong> alternative toxins to sodium mon<strong>of</strong>luoroacetate (1080) for possum<br />

control. Proceedings <strong>of</strong> the Vertebrate Pest Conference 15, 348-350.<br />

Keywords: possums/acute toxicity/1080/lethal dose/field efficacy/bait shyness<br />

Abstract: Possum control in New Zealand is dependent on the use <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) and<br />

cyanide. Although 1080 is highly effective, its uses is restricted to government staff. Cyanide is available<br />

for a wide group <strong>of</strong> licensed operators but cyanide "shyness" reduces its effectiveness. An acute toxicity<br />

programme has been set up to identify non anticoagulant toxins, that could be used safely by farmers. Dose<br />

ranging studies showed that possums are susceptible to cholecalciferol, calciferol, gliftor, alpha-chloralose,<br />

and nicotine, but not to bromethalin. As lethal doses for these toxins have been ascertained, which <strong>of</strong> them<br />

are likely to be cost-effective and safe alternatives to 1080 now needs to be established. Bait palatability<br />

and field studies will then be undertaken with the most promising candidates.<br />

Eason, C. T., Morgan, D. R., and Clapperton, B. K. Toxic bait and baiting strategies for feral cats. 371-<br />

376. 1992. University <strong>of</strong> California, Davis. Proceedings <strong>of</strong> the 15th Vertebrate Pest Conference. Borrecco,<br />

J. E. and Marsh, R. E.<br />

Ref Type: Conference Proceeding<br />

Keywords: cats/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/baits/acute<br />

toxicity/plasma/warfarin/field efficacy/iophenoxic acid<br />

Abstract: To improve feral cat control we developed a dry pelleted toxic bait and evaluated the potential <strong>of</strong><br />

lures. A ploymer fish meal bait was preferred by cats from a range <strong>of</strong> bait types tested. L-alanine furtehr<br />

increased bait acceptance by cat in pens trials and catnip may have the potential to increase field acceptance<br />

and target specificity. An oral LD90 <strong>of</strong> 0.38 mg/kg was established for sodium mon<strong>of</strong>luoroacetate (1080) in<br />

feral cats voluntarily eating surface-loaded baits. Acute toxicity to cats <strong>of</strong> warfarin, cholecalciferol and<br />

gliftor was tested. However, because the cat proved highly sensitive to 1080, we recommended its use at a<br />

dose <strong>of</strong> 2 mg per cat bait. In preliminary field trials <strong>of</strong> bait acceptance using non-toxic ploymer bait<br />

(without flavour or attractants) marked with the plasma marler iophenoxic acid, 50% <strong>of</strong> 39 cats caught<br />

within 3 weeks <strong>of</strong> laying the baits were marked. Subsequently polymer bait, surface coated with 1080 was<br />

used in the successful eradication <strong>of</strong> feral cats from Matakohe Island (37 ha) Whangerei Harbour, New<br />

Zealand.<br />

Eason, C. T. Old pesticide - new data. New Zealand Science Monthly [March 1992], 15-16. 1992.<br />

Ref Type: Magazine Article<br />

Eason, C. T. and Hickling, G. J. (1992). Evaluation <strong>of</strong> a bio-dynamic technique for possum pest control.<br />

New Zealand journal <strong>of</strong> ecology 16, 141-144.<br />

Keywords: pest/possums<br />

48


1080 Reassessment Application October 2006<br />

Appendix C<br />

Eason, C. T., Gooneratne, R., Wright, G. R., Pierce, R., and Frampton, C. M. (1993). The fate <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) in water, mammals, and invertebrates. Proceedings <strong>of</strong> the New Zealand Plant<br />

Protection Conference 46, 297-301.<br />

Keywords: persistence in animals/persistence in water/invertebrates/mammals/metabolism/non-target<br />

species/1080/possums/birds<br />

Abstract: New data on the fate <strong>of</strong> sodium monoacetate (1080) [SMA] in water and its persistence in<br />

mammals and invertebrates is summarized. Studies revealed that 1080 was readily degraded in water,<br />

mammals and invertebrates. It was found that significant water contamination after the aerial distribution <strong>of</strong><br />

1080 bait for the control <strong>of</strong> possums was very unlikely. The rapid elimination <strong>of</strong> 1080 from animal tissue<br />

confirms that 1080 residues are most unlikely in meat. Analyses <strong>of</strong> residues in invertebrates indicated there<br />

was no long-term contamination <strong>of</strong> invertebrates and little risk <strong>of</strong> significant amounts <strong>of</strong> 1080 passing<br />

through the food chain to birds.<br />

Eason, C. T., Frampton, C. M., Henderson, R., Thomas, M. D., and Morgan, D. R. (1993). Sodium<br />

mon<strong>of</strong>luoroacetate and alternative toxins for possum control. New Zealand journal <strong>of</strong> zoology 20, 329-334.<br />

Keywords: possums/acute toxicity/1080<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) is still an essential tool for possum control. We gave<br />

reassessed the fate <strong>of</strong> this compound in the environment and found no evidence <strong>of</strong> water contamination<br />

after largescale possum control operations. The toxin is biodegradable in all living systems and will not<br />

accumulate in the food chain. Nevertheless, over reliance on a single toxin for a particular pest, such as<br />

1080 for possum control, is unwise, and we are evaluating alternatives. Possums are susceptible to some<br />

nonanticoagulant toxins, including gliftor, cholecalciferol, calciferol, and alphachloralose. Of the<br />

anticoagulant toxins, broadifacoum is more effective than pindone. Integrated pen and field trials will<br />

determine the most cost effective alternatives to 1080 for use in bait stations and for aerial application.<br />

Any alternative toxin will need to be subjected to the same scrutiny as 1080 for its environmental fate and<br />

impact on nontarget species.<br />

Eason, C. T., Frampton, C. M., Henderson, R. J., and Thomas, M. D. (1993). Alternatives to 1080 for<br />

possums. (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Christchurch.)<br />

Keywords: possums/acute toxicity/1080/brodifacoum<br />

Abstract: Objectives: To generate data on the safety and effectiveness <strong>of</strong> new toxins to support their<br />

registration for possum control: to determine the effectiveness <strong>of</strong> anticoagulant toxins for possum control;<br />

to conduct limited research on back-up compounds, such as alpha-chloralose.<br />

Conclusions: Cholecalciferol and gliftor show considerable promise as alternatives to 1080; brodifacoum<br />

is approximately 800 times more toxic to possums than pindone, is effective for maintenance control, and<br />

can significantly reduce possum populations.<br />

Eason, C. T. (1993). Persistence <strong>of</strong> 1080. Surveillance 20(2), 7-8.<br />

Keywords: persistence in animals/persistence in water/1080<br />

Eason, C. T. (1993). How safe is 1080? Surveillance 20(4), 23-24.<br />

Keywords: persistence in animals/persistence in water/1080<br />

Eason, C. T., Henderson, R., Thomas, M. D., and Frampton, C. M. (1994). The advantages and<br />

disadvantages <strong>of</strong> sodium mon<strong>of</strong>luoroacetate and alternative toxins for possum control. In 'Proceedings <strong>of</strong><br />

the Science Workshop on 1080, 12-14 December 1993, Christchurch, New Zealand'. (A. A. Seawright and<br />

C. T. EasonEds. ) pp. 159-165. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: possums/acute toxicity/1080/non-target species/brodifacoum<br />

Abstract: Over-reliance on a single toxin, such as sodium mon<strong>of</strong>luoroacetate (1080) is unwise. Current<br />

possum control strategies should integrate use <strong>of</strong> cyanide and trapping with 1080-use where appropriate<br />

and for the future new alternative toxins are needed. Ideally, an alternative toxin for possum control should<br />

be inexpensive and usable by farmers and it should have an antidote. It should be degradable in soil and<br />

water. It should be humane and, as far as possible, species specific. It should not persist in livestock and<br />

should have low risk <strong>of</strong> primary or secondary poisoning in non-target species. Such and ideal toxin will be<br />

difficult to identify. We have been testing alternative toxins in pen and field trials, and have re-evaluated<br />

the susceptibility <strong>of</strong> the possum to anticoagulants. Brodifacoum is more potent than pindone, but is<br />

49


1080 Reassessment Application October 2006<br />

Appendix C<br />

persistent in livestock receiving a sub-lethal dose. Cholecalciferol and gliftor are effective and have a<br />

number <strong>of</strong> positive attributes. any alternative toxin will need to be subjected to the same scrutiny that 1080<br />

has received for its environmental fate and impact on non-target species. In the future, greater effort will<br />

need to be expended in discussing the risk versus benefit <strong>of</strong> possum control using 1080 or alternative<br />

technologies with a wide range <strong>of</strong> interest groups, as well as with those directly involved with or affected<br />

by pest control.<br />

Eason, C. T., Gooneratne, R., Fitzgerald, H., Wright, G., and Frampton, C. (1994). Persistence <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate in livestock animals and risk to humans. Human and experimental toxicology 13, 119-<br />

122.<br />

Keywords: persistence in animals/non-target species/occupational exposure/metabolism/1080/secondary<br />

poisoning/sodium mon<strong>of</strong>luoroacetate/kidney/livestock/humans/goats/poisoning/blood/muscle/liver/plasma<br />

Abstract: 1 Sodium mon<strong>of</strong>luoroacetate (1080), a vertebrate pesticide widely used in New Zealand, was<br />

administered orally to sheep and goats at a dose level <strong>of</strong> 0.1 mg kg(-1) body weight to assess risk to<br />

humans <strong>of</strong> secondary poisoning from meat. Blood, muscle, liver, and kidney were analysed for 1080<br />

residues. 2 The plasma elimination half-life was 10.8 h in sheep and 5.4 h in goats, Concentrations <strong>of</strong> 1080<br />

in muscle (0.042 mu g g(-1)), kidney (0.057 mu g g(-1)), and liver (0.021 mu g g(-1)) were substantially<br />

lower than those in plasma (0.098 mu g ml(-1)) at 2.5 h after dosing. 3 Only traces <strong>of</strong> 1080 (


1080 Reassessment Application October 2006<br />

Appendix C<br />

Public concern about contamination <strong>of</strong> the waterways has focused our research on the persistence <strong>of</strong> 1080<br />

in aquatic ecosystems. This paper concludes that significant contamination <strong>of</strong> waterways with 1080 or<br />

fluoride after possum or rabbit control is unlikely, nevertheless further monitoring <strong>of</strong> water and labotatory<br />

studies are planned. We will continue to address concerns regarding 1080 and potential risk to humans<br />

from contaminated water.<br />

Eason, C. T., Henderson, R. J., Frampton, C. M., and Thomas, M. D. (1994). Alternatives to 1080 for<br />

possums (September 1993 to July 1994). (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Christchurch.)<br />

Keywords: possums/acute toxicity/1080/brodifacoum<br />

Abstract: Objectives: To generate data on new toxins to support their registration and use by farmers for<br />

possum control: to determine the effectiveness <strong>of</strong> gliftor, cholecalciferol, brodifacoum and pindone; to<br />

conduct limited research on back-up compounds.<br />

Conclusions: Cholecalciferol and gliftor continue to show promise as alternatives to 1080; brodifacoum<br />

and pindone can significantly reduce possum populations, but relatively large amounts <strong>of</strong> bait are needed;<br />

cholecalciferol combined with an anticoagulant such as broadifacoum in a cereal bait may improve cost<br />

effectiveness.<br />

Eason, C. T. (1995). Sodium mon<strong>of</strong>luoroacetate (1080) : an update on recent environmental toxicology data<br />

and community concerns. In 'Proceedings <strong>of</strong> the 10th Australian Vertebrate Pest <strong>Control</strong> conference,<br />

Hobart, Tasmania - May 1995'. pp. 39-43. (Department <strong>of</strong> Primary Industry and Fisheries: Kings<br />

Meadows,Tasmania.)<br />

Keywords: field efficacy/non-target species/persistence in animals/persistence in plants/persistence in<br />

soil/persistence in water/occupational exposure/1080/possums<br />

Abstract: Effective and publicly acceptable pest control requires the fulfilment <strong>of</strong> three essential<br />

prerequisites:<br />

i) data on effectiveness<br />

ii)data on environmental toxicology and non-target impacts<br />

iii)community involvement or acceptance<br />

This paper explores the extent to which current use <strong>of</strong> sodium mono fluoroacetate (1080) in New Zealand<br />

meets these prerequisites and suggests where we need to focus more effort in the future.<br />

Sodium mon<strong>of</strong>luoroacetate (1080) was patented as a rodenticide in the USA in the late 1930s and has been<br />

used in New Zealand since 1954 to control introduced animal pests. particularly possums (Trichosurus<br />

vulpecula). Possums cause damage to native and exotic forests and spread bovine tuberculosis (Tb) to<br />

cattle (Cowan 1991). Over the last 20 years, an extensive database on the effectiveness <strong>of</strong> killing possums<br />

has been collected and some data on environmental toxicology and non-target impacts have been gathered<br />

(Seawright and Eason 1994). Despite assurances from the scientific community that the benefits <strong>of</strong> 1080<br />

use far outweigh the risks, the level <strong>of</strong> public antagonism to 1080 has become more widespread. This<br />

suggests that the scientific community and wildlife managers are not adequately meeting the three essential<br />

prerequisites.<br />

Eason, C. T., Warburton, B., and Gregory, N. (1995). Assessment <strong>of</strong> the humaneness <strong>of</strong> toxins used for<br />

possum control in New Zealand. (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Lincoln.)<br />

Keywords: welfare/possums/acute toxicity/brodifacoum<br />

Abstract: Objectives: To review the need for toxins in possum control: to determine the effectiveness <strong>of</strong><br />

gliftor, cholecalciferol, brodifacoum and pindone; to review the humaneness <strong>of</strong> the toxins currently used for<br />

possum control in New Zealand. Conclusions: Although the mode <strong>of</strong> action <strong>of</strong> these toxins is well<br />

understood and the clinical signs in a range <strong>of</strong> species have been recorded, good comparative data on the<br />

relative humaneness <strong>of</strong> existing toxins are not available for the possum.<br />

Eason, C. T., Wright, G. R., Meikle, L., and Elder, P. (1996). The persistence and secondary poisoning<br />

risks <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080), brodifacoum, and cholecalciferol in possums. Proceedings <strong>of</strong><br />

the Vertebrate Pest Conference 17, 54-58.<br />

Keywords: secondary poisoning/non-target species/persistence in<br />

animals/metabolism/1080/brodifacoum/possums/cats<br />

Abstract: To determine the risk <strong>of</strong> secondary poisoning for animals preying on sub-lethally poisoned<br />

brushtail possums, captive possums were treated with near-lethal doses <strong>of</strong> sodium mon<strong>of</strong>luoroacetate<br />

51


1080 Reassessment Application October 2006<br />

Appendix C<br />

(1080) or brodifacoum, and toxicant concentrations in blood and tissue were monitored over time. Sodium<br />

mon<strong>of</strong>luoroacetate was rapidly eliminated from the blood (within three days). Brodifacoum was retained in<br />

the liver and, to a lesser extent, the muscle <strong>of</strong> possums for eight months after dosing. To determine the<br />

potential risk for animals scavenging on the carcasses <strong>of</strong> possums poisoned with cholecalciferol, cats were<br />

fed poisoned carcasses for six days. No changes in behavior, appetite, or body weight were observed.<br />

Serum calcium concentrations increased slightly, but remained within the normal range for cats.<br />

Eason, C. T., Warburton, B., and Gregory, N. (1996). Future directions for toxicology and welfare in<br />

possum control. In 'Improving conventional control <strong>of</strong> possums : proceedings <strong>of</strong> a workshop organised by<br />

the Possum and Bovine Tuberculosis <strong>Control</strong> National Science Strategy Committee, 25-26 October 1995,<br />

Wellington'. pp. 24-28. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: welfare/possums/regulatory toxicology/acute toxicity<br />

Abstract: Non-tariff trade barriers will be imposed on New Zealand if our pest control techniques are<br />

deemed unacceptable in overseas markets. Finding control methods for possums that are economic,<br />

effective, and humane is a major ethical and animal welfare issue. The increasing international focus on<br />

animal welfare issues makes the development <strong>of</strong> humane trapping and poisoning techniques a high priority.<br />

The current Animal Protection Act (1960) exempts possum control from the requirements <strong>of</strong> the Act except<br />

for one specific section relating to trapping. The pending Animal Welfare Act, however, requires that all<br />

wild animals must not be subjected to unnecessary or unreasonable pain, suffering, or distress. This, in<br />

essence, means that any method used to kill possums must be humane in its action and effect. This<br />

legislation brings New Zealand in line with its major overseas trading partners. For example, the UK<br />

<strong>Control</strong> <strong>of</strong> Pesticides Regulations (1986) requires that pests should be controlled by methods that are<br />

humane, and a more recent European Union Directive (91/414/EEC) requires that vertebrate pesticides do<br />

not cause undue suffering. While some data exist for traps, no published quantitative data exsit for toxic<br />

agents to be able to conform to this legislation and certainly not to the extent that questions relating to their<br />

humaneness could be thoroughly answered. Furthermore, literature accounts <strong>of</strong> the humaneness <strong>of</strong><br />

different toxicants are inconsistent, and species difference in response to different xenobiotics need to be<br />

taken into account. The background to The present situation relating to possum control and The need for a<br />

welfare scoring system for selection acceptable toxicants and traps are discussed in this paper.<br />

Eason, C. T. (1997). Sodium mon<strong>of</strong>luoroacetate toxicology in relation to its use in New Zealand.<br />

Australasian journal <strong>of</strong> ecotoxicology 3, 57-64.<br />

Keywords: possums/bait degradation/persistence in animals/persistence in plants/persistence in<br />

soil/persistence in water/non-target species/mode <strong>of</strong> action/metabolism/pathology/1080<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) is a highly toxic vertebrate pesticide widely used for possum<br />

control in New Zealand. Fluoroacetate is also a toxic component <strong>of</strong> poisonous plants found in Australia,<br />

South Africa, South America, and India. Because <strong>of</strong> the highly toxic nature <strong>of</strong> this compound, its<br />

environmental fate, persistence, and non-target impacts have been extensively studied. Current evidence<br />

suggests that the risks <strong>of</strong> using 1080 are outweighed by the benefits achieved from sustained large-scale<br />

pest control. However, it toxic baits are not prepared and used with extreme care, humans, livestock, and<br />

non-target wildlife will be put at risk. The risk to dogs from poisoned carcasses must not be<br />

underestimated.<br />

Eason, C. T., Wickstrom, M., and Gregory, N. (1997). Product stewardship, animal welfare and regulatory<br />

toxicology constraints on vertebrate pesticides. Proceedings <strong>of</strong> the New Zealand Plant Protection<br />

Conference 50, 206-213.<br />

Keywords: product chemistry/welfare/regulatory toxicology/teratogenicity<br />

Abstract: Increasing regulatory and product safety standards along with the enhaanced expectations <strong>of</strong><br />

todays consumers have influenced the manner in which new pesticides and older compounds subject to<br />

reevaluation, face everrising standards in product efficacy, toxicology and environmental risk assessment.<br />

Vertebrate pesticides are no exception to this worldiwide phenomenon and in this paper we review, using<br />

possum control in New Zealand as a casestudy, some <strong>of</strong> the factors that are likely to influence the future<br />

use ot toxicants in this field.<br />

Eason, C. T., Wickstrom, M., and Spurr, E. B. (1998). Review <strong>of</strong> impacts <strong>of</strong> large-scale sodium<br />

mon<strong>of</strong>luoroacetate (1080) use in New Zealand. In '11th Australian Vertebrate Pest Conference, Bunbury,<br />

52


1080 Reassessment Application October 2006<br />

Appendix C<br />

Western Australia, 3-8 May 1998 : programme and proceedings.'. pp. 105-110. (Agriculture Western<br />

Australia: Forrestfield.)<br />

Keywords: non-target species/persistence in plants/persistence in soil/persistence in<br />

water/1080/mammals/birds/possums/rabbits/secondary poisoning/metabolism/invertebrates<br />

Abstract: New Zealand had no indigenous terrestrial mammals except 2 species <strong>of</strong> bats prior to human<br />

settlement. Introduced mammals have had serve impacts on native flora and fauna, including extinctions <strong>of</strong><br />

birds and the near collapse <strong>of</strong> indigenous rainforests. <strong>Control</strong> strategies currently rely on the large-scale<br />

use <strong>of</strong> vertebrate pesticides, including aerial distribution <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) baits to<br />

control possums (Trichosurus vulpecula) and rabbits (Oryctolagus cuniculus). Studies <strong>of</strong> the implications<br />

<strong>of</strong> widespread use <strong>of</strong> 1080 include risks <strong>of</strong> primary or secondary poisoning to non-target species,<br />

accumulation in soil, uptake into vegetation, and persistence in surface water. Results indicate that 1080 is<br />

not environmentally persistent under most conditions. It is water-soluble, readily leaches from baits, and<br />

does not bind to soil constituents. However, detoxification by soil microorganisms varies with soil<br />

conditions, and may be prolonged by drought and cold. Surface water monitoring following aerial 1080<br />

applications revealed no significant contamination. Toxin breakdown in aquaria studies was temperaturedependent,<br />

but occurred within 1-2 weeks even at 11°C. Uptake and persistence in plants varied with<br />

different species, with peak concentration ranging from 0.06 to 0.08 ppm, and elimination occurring with 1-<br />

5 weeks. metabolism and excretion was rapid in sub-lethally dosed mammals (75<br />

days, increasing the risks <strong>of</strong> secondary poisoning to scavengers. Some losses <strong>of</strong> individual native birds<br />

have been observed, especially with the use <strong>of</strong> 1080 bait containing excessive small fragments, but no long<br />

term population-level effect have been reported. Native invertebrates have been observed feeding on toxic<br />

baits, but adverse effects on invertebrate populations or secondary poisoning <strong>of</strong> insectivorous birds or bats<br />

have not been documented to date.<br />

Eason, C. T., Wickstrom, M. L., and Turck, P. A. Assessment <strong>of</strong> the developmental toxicity <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroactetate (1080) in rats. 11th Australian Vertebrate Pest Conference, Bunbury, Western<br />

Australia, 3-8 May 1998 : programme and proceedings. 159-164. 1998. Forrestfield, Agriculture Western<br />

Australia.<br />

Ref Type: Conference Proceeding<br />

Keywords: regulatory toxicology/pathology/1080/teratogenicity/reproductive effects/developmental<br />

toxicity<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) has been used in New Zealand to control vertebrate pests since<br />

1954, and although a large historical database exists, little is known about the development toxicity <strong>of</strong> this<br />

pesticide. This investigation was intended to evaluate the development toxicity and teratogenic potential <strong>of</strong><br />

1080 in SpragueDawley rats following oral intubation. A pilot study was performed to help select doses for<br />

the subsequent study an consisted <strong>of</strong> groups <strong>of</strong> 5 time mated females. Animals received 1080 at<br />

concentrations ranging from 0.1 to 1.0mg/kg.day from days 617 <strong>of</strong> gestation. A 60%mortality rate and<br />

reductions in maternal body weight and body weight gain as well as decreased litter size and increased<br />

resorption were observed at 1.0 mg/kg/day. Consequently, the doses selected for the main study were 0.1,<br />

0.33, and 0.75 mg/kg/day. Groups <strong>of</strong> 26 timemated females received 1080 from days 617 <strong>of</strong> gestation. On<br />

day 20 <strong>of</strong> gestation, litters were delivered via laparohysterectomy. Significant reductions in maternal body<br />

weight, body weight gain, and food consumption were noted at 0.75 mg/kg/day. No changes in litter size<br />

or resorption were observed, but foetal body weight was significantly reduced at 0.75 mg/kg/day. No<br />

external or visceral foetal abnormalities were noted. There were treatmentrelated effects on skeletal<br />

development at 0.33 mg/kg/day and higher. Forelimb malformations occurred at 0.75 mg/kg/day, but were<br />

not observed in controls. An increased incidence <strong>of</strong> bent/way ribs was observed at 0.33 and 0.75<br />

mg/kg/day when compared with controls. Available data indicate that 1080 is maternally toxic at 0.75<br />

mg/kg/day and higher. Embryolethality was noted at 1.0 mg/kg/day, but not at 0.75 mg/kg/day.<br />

Development toxicity was observed at 0.33 mg/kg/day and higher. Sodium mon<strong>of</strong>luoroacetate was<br />

considered to be teratogenic at 0.75 mg/kg/day. Reductions in foetal body weight at 0.75 mg/kg/day are<br />

likely linked to maternal toxicity rather than a direct effect on the foetus.<br />

Eason, C. T., Wickstrom, M., Turck, P., and Wright, G. R. G. (1999). A review <strong>of</strong> recent regulatory and<br />

environmental toxicology studies on 1080: results and implications. New Zealand journal <strong>of</strong> ecology 23,<br />

129-137.<br />

53


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: regulatory toxicology/occupational exposure/pathology/persistence in water/developmental<br />

toxicity/reproductive effects/teratogenicity/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/rats/humans/baits<br />

Eason, C. T., Turck, P., and Fountain, J. S. A 90-day oral (gavage) study <strong>of</strong> compound 1080 (sodium<br />

mon<strong>of</strong>luoroacetate) with a 56-day recovery period in rats, and its implications for human health. <strong>Landcare</strong><br />

<strong>Research</strong> Contract Report: LC0001/39, -17. 2000. Manaaki Whenua <strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Report<br />

Keywords: 1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/rats/testes/heart/sublethal effects/regulatory<br />

toxicology/treatment/pathology/blood/urine<br />

Abstract: This study was conducted to determine the sub-lethal effects <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080)<br />

exposure in rats, and the No-Observable-Effect-Level (NOEL) for chronic exposure. The objectives <strong>of</strong><br />

conducting toxicology studies <strong>of</strong> this type are principally: (i) to establish an up-to-date regulatory<br />

toxicology database on 1080, (ii) to set Acceptable Daily Intakes (ADIs) for human exposure, and (iii) to<br />

provide data to improve risk assessment for workers involved in the pest control industry.<br />

Three groups <strong>of</strong> 10 male and 10 female Sprague-Dawley rats received 1080 dissolved in water at doses <strong>of</strong><br />

0.025, 0.075, and 0.25mg/kg/day by oral gavage once daily for 90days. A group <strong>of</strong> 10 male and 10 female<br />

rats served as the control group, and were administered water. The control and 0.25 mg/kg/day groups<br />

included 10 additional rats <strong>of</strong> each sex that were treated for 90 days, then maintained without treatment for<br />

a further 56-day recovery period.<br />

No 1080-related changes in body weight or food consumption were noted when compared with the control<br />

group during the treatment or recovery periods. Erythrocyte counts decreased slightly in males at<br />

0.25mg/kg/day when compared with controls. No other changes in clinical pathology parameters derived<br />

from blood samples were detected. The only 1080-related findings at necropsy were small testes and<br />

epididymis in males at 0.25mg/kg/day, and these observations were corroborated by a reduction in the<br />

weight <strong>of</strong> the testes. 1080-related increases in heart weight were noted in both males and females at 0.25<br />

mg/kg/day when compared with controls. No effects were noted in the lower-dose groups. Microscopic<br />

changes in the testes and the heart were seen only in males at 0.25mg/kg/day when compared with controls<br />

and included severe hypospermia in the epididymis, severe degeneration <strong>of</strong> the seminiferous tubules <strong>of</strong> the<br />

testes, and cardiomyopathy. The testicular and epididymal effects were also evident from the sperm<br />

evaluation, which indicated severe decreases in all three sperm parameters evaluated, concentration, %<br />

motile, and % abnormal, at 0.25 mg/kg/day. There were no microscopic changes or effects on sperm<br />

parameters at 0.025 and 0.075 mg/kg/day when compared with controls. The effects in males at 0.25<br />

mg/kg/day were evident following both the treatment and recovery periods. No recovery in sperm<br />

evaluation parameters was noted, although there appeared to be a slight improvement in the microscopic<br />

changes, and effects were slightly less severe after the 56-day recovery period. This suggested a slight<br />

reversal in both the hypospermia and seminiferous tubule degeneration at 0.25 mg/kg/day in the males<br />

following 56 days with no treatment.<br />

Based on the results <strong>of</strong> this study, the NOEL for rats administered 1080 via oral gavage for 90 days was<br />

0.075 mg/kg/day. Since this study is similar to that derived from an earlier developmental study (0.1<br />

mg/kg/day) there is no reason to adjust, on the basis <strong>of</strong> these data, the Ministry <strong>of</strong> Health guidelines for<br />

acceptable levels <strong>of</strong> 1080 in water. Concentrations <strong>of</strong> 1080 in rats dosed with 0.25 mg/kg/day were<br />

0.28g/mL one hour after dosing and 0.075 g/mL 12 hours after dosing. Rat urine collected from the same<br />

animals contained 0.06 g/mL. These 1080 concentrations can be cross-correlated with 1080 concentrations<br />

determined in blood and urine samples from workers in the pest control industry to enhance the power <strong>of</strong><br />

human risk assessment estimates and assist in defining acceptable and unacceptable levels <strong>of</strong> exposure.<br />

Eason, C. T. (2002). Vertebrate pesticides, old and new. What will influence their future development and<br />

use. The <strong>Royal</strong> Society <strong>of</strong> New Zealand 46-50.<br />

Keywords: possums<br />

Abstract: Vertebrate pesticides for wild animal control and pesticides in general are coming under steadily<br />

increasing scrutiny both nationally and internationally. Further research will need to be undertaken if these<br />

pesticides are to be continued to be used in New Zealand. For example, wildlife management agencies in<br />

54


1080 Reassessment Application October 2006<br />

Appendix C<br />

the United States (US) have spent many millions <strong>of</strong> dollars on upgrading the toxicology databases on old<br />

toxicants such as cyanide, 1080, and diphacenone to meet current US EPA data requirements. In New<br />

Zealand we can anticipate that the six toxicants currently registered for possum control will remain under<br />

similar scrutiny by the community, scientists, and pest managers. Issues such as safety, how they are used,<br />

humaneness, and how they are perceived in New Zealand and internationally by regulatory authorites and<br />

overseas markets, will determine their future. The advantages and disadvantages <strong>of</strong> existing toxicants are<br />

summarised, and research questions relating to their use are identified.<br />

Eason, C. T. and Turck, P. (2002). A 90-day toxicological evaluation <strong>of</strong> compound 1080 (sodium<br />

mon<strong>of</strong>luoroacetate) in Sprague-Dawley rats. Toxicological Sciences 69, 439-447.<br />

Keywords: 1080/heart/mon<strong>of</strong>luoroacetate/plasma/rats/regulatory toxicology/reproductive effects/sodium<br />

mon<strong>of</strong>luoroacetate/testes/treatment/urine/brain<br />

Abstract: Groups <strong>of</strong> Sprague-Dawley rats received sodium mon<strong>of</strong>luoroacetate (Compound 1080) at 0.025,<br />

0.075, and 0.25 mg/kg by oral gavage once daily for 90 days and were then euthanased. The control and<br />

0.25 mg/kg/day groups included additional rats <strong>of</strong> each sex that were treated for 90 days, then maintained<br />

without treatment for a further 56-day recovery period. Microscopic changes were restricted to the testes<br />

and the heart, and were seen only in males dosed with 1080 at 0.25 mg/kg/day and included severe<br />

hypospermia in the epididymides, severe degeneration <strong>of</strong> the seminiferous tubules <strong>of</strong> the testes, and<br />

cardiomyopathy. Sperm evaluation indicated severe decreases in all three sperm parameters evaluated<br />

(concentration, % motile, and % abnormal) at 0.25 mg/kg/day. There were no microscopic changes or<br />

1080-related effects on sperm parameters at 0.025 and 0.075 mg/kg/day. The no observable effects level<br />

(NOEL) for rats administered 1080 via oral gavage for 90 days was 0.075 mg/kg/day. The lowest<br />

observable effects level (LOEL) dose was 0.25 mg/kg/day. After dosing with the LOEL dose <strong>of</strong> 0.25<br />

mg/kg/day, mean concentrations <strong>of</strong> 1080 in rat plasma were 0.26 g/ml at 1 h and 0.076 g/ml at 12 h. Rat<br />

urine collected from the same animals contained 0.059 g/ml.<br />

Eastland, W. G. and Beasom, S. L. (1986). Effects <strong>of</strong> ambient temperature on the 1080-LD50 <strong>of</strong> raccoons.<br />

Wildlife Society bulletin 14, 234-235.<br />

Keywords: acute toxicity/mammals<br />

Eastland, W. G. and Beasom, S. L. (1986). Potential secondary hazards <strong>of</strong> compound 1080 to three<br />

mammalian scavengers. Wildlife Society bulletin 14, 232-233.<br />

Keywords: non-target species/secondary poisoning/mammals/1080/scavenger/predators<br />

Eastland, W. G. and Beasom, S. L. (1987). Acute toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate to the striped<br />

skunk. Bulletin <strong>of</strong> environmental contamination and toxicology 38, 934-936.<br />

Keywords: acute toxicity/mammals/non-target species/sodium mon<strong>of</strong>luoroacetate<br />

Egekeze, J. O. and Oehme, F. W. (1979). Sodium mon<strong>of</strong>luoroacetate (SMFA, compound 1080) : a<br />

literature review. Veterinary and human toxicology 21, 411-416.<br />

Keywords: product chemistry/acute toxicity/field efficacy/metabolism/mode <strong>of</strong><br />

action/diagnosis/treatment/secondary poisoning/non-target species/pathology/1080<br />

Abstract: The literature (from 1945 to 1977) relating to 1080 is reviewed.<br />

Egekeze, J. O. and Oehme, F. W. (1979). Inorganic and organic fluoride concentrations in tissues after the<br />

oral administration <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound 1080) to rats. Toxicology 15, 43-53.<br />

Keywords: metabolism/persistence in animals/sodium<br />

mon<strong>of</strong>luoroacetate/1080/rats/defluorination/blood/liver/kidney/gut/fluoride/mon<strong>of</strong>luoroacetate/plasma/stom<br />

ach/convulsions/symptoms<br />

Abstract: Male rats were used to study the inorganic (ionic) and organic fluoride concentrations in plasma,<br />

liver, kidneys and stomach content after oral doses <strong>of</strong> 0, 2.2, 3.5, 4.0, 5.0 and 7.0 mg sodium<br />

mon<strong>of</strong>luoroacetate (SMFA, Compound 1080)/ kg bodyweight. Tissue and plasma ionic fluoride<br />

concentrations were observed to be higher in all rats given SMFA as compared to rats in the control group.<br />

The observation suggests the in vivo defluorination <strong>of</strong> SMFA. Homogentaes <strong>of</strong> liver obtained from SMFApoisoned<br />

rats showed significant increases in ionic fluoride concentration during a 6-day storage period at 4<br />

degrees C, with the total fluoride concentration (organic and inorganic) remaining constant. The average<br />

55


1080 Reassessment Application October 2006<br />

Appendix C<br />

percentages <strong>of</strong> distribution <strong>of</strong> SMFA (organic fluoride) in plasma, liver and kidneys were 7.05, 5.07 and<br />

1.68 respectively. Plasma and tissue SMFA concentrations were generally lower than the corresponding<br />

stomach fluid SMFA concentrations for all dosage groups. Lethal concentration <strong>of</strong> SMFA in the liquid<br />

stomach content was in the range 84.9 - 189 ug/mL corresponding to the total (ionic and organic) fluoride<br />

concentrations in the range <strong>of</strong> 16.1 - 36 ug/mL.<br />

Egekeze, J. O. and Oehme, F. W. (1979). Determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound 1080) in<br />

biological tissues using oxygen combustion and a fluoride selective membrane electrode. Toxicology letters<br />

4, 461-468.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/fluoride/plasma/liver/analysis<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (rodenticide) (SMFA) was quantitated in plasma and liver<br />

homogenates after total fluoride analysis using an O2 combustion method and fluoride selective electrode.<br />

The organic content <strong>of</strong> the samples were estimated by difference between total fluoride and inorganic<br />

fluoride. Recoveries (%+-SD) <strong>of</strong> SMFA in aqueous samples (dog and rat), plasma and (bovine and rat)<br />

liver homogenates were 99.1+- 2.3, 95.2+-3.3 and 95.3+-2.9, respectively. The within-run coefficient <strong>of</strong><br />

variation in the 10.0-0.072 mg/ml (or mg/g) range for all samples was 4.7% or less. The method is suitable<br />

for quantitation <strong>of</strong> SMFA in biological materials and as a laboratory diagnostic aid in cases <strong>of</strong> acute SMFA<br />

intoxication<br />

Egyed, M. N. (1971). Experimental acute fluoroacetamide poisoning in sheep. III. Therapy. Refuah<br />

veterinarith 28, 70-73.<br />

Keywords: fluoroacetamide/poisoning/monoacetin/lethal dose/toxicity/treatment<br />

Abstract: Acetamide at 200 mg/kg given orally one hour after the administration <strong>of</strong> 20 mg/kg <strong>of</strong><br />

fluoroacetic acid (FAA), failed to save a sheep. Another sheep given the two substances simultaneously<br />

also died. Repeated doses <strong>of</strong> 0.4 ml/kg <strong>of</strong> monoacetin were similarly unable to save a sheep from a lethal<br />

dose <strong>of</strong> FAA. Both acetamide and monacetin did nothing to reverse the occurrence <strong>of</strong> hyperglycaemia, a<br />

common finding in FAA poisoning. In toxicity trials 200 mg/kg <strong>of</strong> acetamide had no ill effect on one sheep,<br />

while in another sheep monoacetin caused depression and pain at the site <strong>of</strong> injection <strong>of</strong> the drug<br />

Egyed, M. N. (1971). Some aspects <strong>of</strong> fluoroacetate research. Refuah veterinarith 28, 175-177.<br />

Keywords: fluoroacetate<br />

Egyed, M. N. (1973). Clinical, pathological, diagnostic and therapeutic aspects <strong>of</strong> fluoroacetate research in<br />

animals. Fluoride 6, 215-224.<br />

Keywords: diagnosis/pathology/treatment/fluoroacetate<br />

Egyed, M. N. and Shlosberg, A. (1973). Diagnosis <strong>of</strong> field cases <strong>of</strong> sodium fluoroacetate and<br />

fluoroacetamide poisoning in animals. Refuah veterinarith 30, 112-115.<br />

Keywords: diagnosis/sodium fluoroacetate/fluoroacetate/fluoroacetamide/poisoning/non-target species<br />

Abstract: Of the 143 cases investigated, guinea-pig kidney citrate levels were normal (less than 50 µg/g) in<br />

63 cases. In the remaining 80 cases the citrate levels were elevated, ranging from 70 -1200 µg/g. The<br />

highest values were obtained after the injection <strong>of</strong> suspect baits.<br />

Egyed, M. N., Nobel, T. A., Klopfer, U., and Shlosberg, A. (1977). The differential diagnosis <strong>of</strong> sodium<br />

fluoroacetate and strychnine poisoning in dogs. Refuah veterinarith 34, 125-130.<br />

Keywords: diagnosis/pathology/mammals/sodium fluoroacetate/fluoroacetate/strychnine/poisoning/dogs<br />

Egyed, M. N. (1978). Mass poisoning in dogs associated with feeding meat contaminated with<br />

organ<strong>of</strong>luoride (sodium fluoroacetate or fluoroacetamide). Refuah veterinarith 35, 8-11.<br />

Keywords: poisoning/dogs/sodium fluoroacetate/fluoroacetate/fluoroacetamide/strychnine<br />

Abstract: The results <strong>of</strong> laboratory investigations are reported in a case <strong>of</strong> mass poisoning in which about<br />

70 dogs died shortly after consuming purchased poultry meat. Clinical and pathological findings indicated<br />

either strychnine or sodium fluoroacetate (FAC) or fluoroacetamide (FAA) poisoning. Toxicological<br />

examination revealed poisoning by FAC or FAA. The toxicological and public health implications <strong>of</strong> the<br />

case are discussed<br />

56


1080 Reassessment Application October 2006<br />

Appendix C<br />

Egyed, M. N. (1979). Mass poisoning in dogs due to meat contaminated by sodium fluoroacetate or<br />

fluoroacetamide (special reference to the differential diagnosis). Fluoride 12, 76-84.<br />

Keywords: non-target species/secondary poisoning/mammals/diagnosis/pathology/poisoning/dogs/sodium<br />

fluoroacetate/fluoroacetate/fluoroacetamide<br />

Egyed, M. N. and Shlosberg, A. (1979). Trends in poisoning <strong>of</strong> domestic animals in Israel. Israel journal <strong>of</strong><br />

veterinary medicine 36, 153-162.<br />

Keywords: poisoning<br />

Egyed, M. N., Nobel, T. A., Klopfer, U., and Shlossberg, A. Sodium fluoroacetate and strychnine poisoning<br />

in dogs as a major toxicological problem in Israel. 45-47. 1980. Tel-Aviv, Association for Buiatrics; Israel.<br />

20-10-1980.<br />

Ref Type: Conference Proceeding<br />

Keywords: sodium fluoroacetate/fluoroacetate/strychnine/poisoning/dogs/rodents/<strong>poisons</strong>/poison/diagnosis<br />

Abstract: Sodium fluoroacetate and strychnine are by far the most common source <strong>of</strong> poisoning in Israel.<br />

The former is used as a rodenticide and the latter is used for destroying stray dogs as possible vectors <strong>of</strong><br />

rabies. Dogs may be victims <strong>of</strong> poisoning either by eating the bait or poisoned rodents. Both <strong>poisons</strong> affect<br />

the central nervous system and at a certain stage <strong>of</strong> poisoning the clinical signs can be similar. The<br />

pathological lesions may be absent, or not characteristic or even identical (haemorrhages in the pancreas<br />

and thymus) and therefore in some cases the diagnosis without chemical-toxicological examinations can be<br />

difficult. Differential diagnostic methods and toxicological evaluation <strong>of</strong> these two poisonings are<br />

discussed<br />

Eichhold, T. H., Hookfin, E. B., Taiwo, Y. O., De, B., and Wehmeyer, K. R. (1997). Isolation and<br />

quantification <strong>of</strong> fluoroacetate in rat tissues, following dosing <strong>of</strong> Z-Phe-Ala-CH2-F, a peptidyl fluoromethyl<br />

ketone protease inhibitor. Journal <strong>of</strong> pharmaceutical and biomedical analysis 16, 459-467.<br />

Keywords: mode <strong>of</strong> action<br />

Eisler, R. (1995). Sodium mon<strong>of</strong>luoroacetate (1080) hazards to fish, wildlife, and invertebrates : a synoptic<br />

review. (Fish and Wildlife Service, U.S. Dept. <strong>of</strong> the Interior: Washington,D.C.)<br />

Keywords: non-target species/aquatic<br />

species/mammals/invertebrates/diagnosis/pathology/metabolism/mode <strong>of</strong> action/product<br />

chemistry/treatment/acute toxicity/target species/welfare/birds/secondary poisoning/bait<br />

degradation/persistence in animals/persistence in plants/persistence in soil/persistence in water/occurrence<br />

in nature/1080/rabbits/possums/deer/cats/lethal dose<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (CH2FCOONa), also known as 1080 first used in the United States to<br />

control gophers (Geomys spp) squirrels (Sciurus spp., Spermophilus spp), prairie dogs (Cynomys spp), other<br />

rodents (Rodentia) and coyotes (Canis latrans); domestic use is currently restricted to livestockprotection<br />

collars on sheep and goats to selectively kill depredating coyotes. However, Australia, New Zealand, and<br />

some other nations continue to use 1080 to control rabbits, possums, deer, foxes, feral pigs and cats, wild<br />

dogs, wallabies, rodents and other mammals. The chemical is readily absorbed by ingestion or inhalation.<br />

At lethal doses, metabolic conversion <strong>of</strong> fluoroacetate to fluorocitrate results in the accumulation <strong>of</strong> citrate<br />

in the tissues and death within 24 hr from ventricular fibrillation <strong>of</strong> from respiratory failure; no antidote is<br />

available. At sublethal doses, the toxic effects <strong>of</strong> 1080 are reversible. Primary and secondary poisoning <strong>of</strong><br />

nontarget vertebrates may accompany the use <strong>of</strong> 1080. Sensitive mammals including representative species<br />

<strong>of</strong> livestock, marsupials, felids, rodents, and canids died after a single dose <strong>of</strong> 13 mg/kg BW. High residues<br />

were measured in some poisoned target mammals, and this contributed to secondary poisoning <strong>of</strong><br />

carnivores that ingested poisoned prey. Sublethal effects occurred in sensitive mammals at greater than 2.2<br />

mg 1080/L in drinking water or at 0.8 1.1 mg 1080/kg in the diet. Sensitive species <strong>of</strong> birds died after a<br />

single 1080 dose <strong>of</strong> 0.62.5 mg/kg BW, after daily doses <strong>of</strong> 0.5 mg/kg BW for 30 days after 47 mg/kg in<br />

diets for 5 days, or after 18 mg/L in drinking water for 5 days. Adverse effects occurred in birds at dietary<br />

loadings as low as 1013 mg 1080/kg ration. Amphibians and reptiles were more resistant to 1080 than<br />

birds and mammals. LD50 values were greater than 44 mg/kg BW in tested amphibians and greater than<br />

54 mg/kg BW in tested reptiles, resistance 10 1080 was attributed to their reduced ability to convert<br />

fluoroacetate to fluorocitrate and their increased ability to detoxify fluoroacetate by defluorination.<br />

Mosquito larvae reportedly died at 0.0250.05 mg 1080/L, but fishes seemed unaffected at 13 mg/L;<br />

57


1080 Reassessment Application October 2006<br />

Appendix C<br />

however, data on 1080 in aquatic ecosystems are incomplete. Acute LD50 values in terrestrial insects<br />

ranged from 1.13.9 mg/kg BW to 130.0 mg/kg BW in larvae feeding on fluoroacetatebearing vegetation.<br />

Residues <strong>of</strong> 1080 in exposed insects were usually low (>4mg 1080/kg fresh weight) or negligible and were<br />

usually eliminated completely within 6 days, suggesting low risk to insectivorous birds. Loss <strong>of</strong> 1080 from<br />

baits occurs primarily from microbial defluorination and secondarily from leaching by rainfall and<br />

consumption by insect larvae, leachates from 1080 baits are probably held in the upper soil layers. The use<br />

<strong>of</strong> 1080 seems warranted in the absence <strong>of</strong> suitable alternative control methods.<br />

Eldridge, S. R., Berman, D. M., and Walsh, B. (2000). Field evaluation <strong>of</strong> four 1080 baits for dingo control.<br />

Wildlife research 27, 495-500.<br />

Keywords: field efficacy/ground control/1080<br />

Elgie, H. J. (1961). Wallaby eradication by aerial poisoning. New Zealand journal <strong>of</strong> agriculture 102, 26-<br />

31.<br />

Keywords: poisoning/field efficacy<br />

Ellenhorn, M. J. and Barceloux, D. G. (1988). Sodium Mon<strong>of</strong>luoroacetate ("1080"). In 'Medical<br />

Toxicology. Diagnosis and treatment <strong>of</strong> human poisoning'. (Elsevier: New York/Amsterdam/London.)<br />

Keywords: humans/sodium fluoroacetate/treatment/analysis/diagnosis/poisoning<br />

Ellis, D. A., Martin, J. W., Muir, D. C. G., and Mabury, S. A. (2000). Development <strong>of</strong> an 19F NMR<br />

Method for the Analysis <strong>of</strong> Fluorinated Acids in Environmental Water Samples. Anal.Chem. 72, 726-731.<br />

Keywords: NMR/analysis<br />

Abstract: This investigation was carried out to evaluate 19F NMR as an anal. tool for the measurement <strong>of</strong><br />

trifluoroacetic acid (TFA) and other fluorinated acids in the aquatic environment. A method based upon<br />

strong anionic exchange (SAX) chromatog. was also optimized for the concn. <strong>of</strong> the fluoro acids prior to<br />

NMR anal. Extn. <strong>of</strong> the analyte from the SAX column was carried out directly in the NMR solvent in the<br />

presence <strong>of</strong> the strong org. base, DBU. The method allowed the anal. <strong>of</strong> the acid without any prior cleanup<br />

steps being involved. Optimal NMR sensitivity based upon T1 relaxation times was investigated for seven<br />

fluorinated compds. in four different NMR solvents. The use <strong>of</strong> the relaxation agent chromium<br />

acetylacetonate, Cr(acac)3, within these solvent systems was also evaluated. Results show that the optimal<br />

NMR solvent differs for each fluorinated analyte. Cr(acac)3 was shown to have pronounced effects on the<br />

limits <strong>of</strong> detection <strong>of</strong> the analyte. Generally, the optimal sensitivity condition appears to be methanold4/2M<br />

DBU in the presence <strong>of</strong> 4 mg/mL <strong>of</strong> Cr(acac)3. The method was validated through spike and<br />

recovery for five fluoro acids from environmentally relevant waters. Results are presented for the anal. <strong>of</strong><br />

TFA in Toronto rainwater, which ranged from


1080 Reassessment Application October 2006<br />

Appendix C<br />

either citrate synthetase or acetate thiokinase from D. cymosum had different affinities for the fluoronated<br />

derivative and the 'normal' metabolite. The addition <strong>of</strong> fluoropyruvate to leaf discs caused a decrease in<br />

oxygen uptake and no change in the citrate concentration. From this it was deduced that fluoropyruvate<br />

inhibited pyruvate oxidase in both plants. It was concluded that the tolerance <strong>of</strong> D. cymosum to such high<br />

concentrations <strong>of</strong> fluoroacetate may be ascribed to the fact that the 'lethal synthesis' <strong>of</strong> fluorocitrate does<br />

not take place in the plant most probably because citrate synthetase has different affinities for<br />

fluoroacytlycoenzyme A and acetylconenzyme A.<br />

El<strong>of</strong>f, J. N. (1972). Evidence for the occurance <strong>of</strong> a Krebs Cycle in the fluoroacetate containing plant<br />

Dichapetalum cymosum (Gifbaar). Zeitschrift für Pflanzenphysiologie 67, 207-211.<br />

Keywords: Krebs cycle/fluoroacetate<br />

Abstract: The evidence obtained by respiration studies in the presence <strong>of</strong> malonate and by tracer<br />

experiments indicates that Dichapetalum cymosum has an active Krebs cycle. The label pattern found<br />

among the amino acids after feeding pyruvate-1- 14 C, pyruvate-2- 14 C, pyruvate-3- 14 C, citrate 1,5- 14 C and<br />

acetate-2- 14 C indicates that the plant does contain an active Krebs cycle. The results indicate that the<br />

Krebs cycle may play a more important role in young leaves than in old leaves.<br />

El<strong>of</strong>f, J. N. and Grobbelaar, N. (1972). A preliminary evaluation <strong>of</strong> the metabolic fate <strong>of</strong> fluoroacetate and<br />

acetate in Dichapetalum cymosum and Parinari capensis. Joernaal van die Suid-Afrikaanse Chemiese<br />

Instituut 25, 109-114.<br />

Keywords: fluoroacetate<br />

Abstract: Fluoroacetate-2- 14 C and acetate-2- 14 C were fed to intact leaves <strong>of</strong> D. cymosum and P. capensis.<br />

In comparison wih acetate, fluoroacetate was found to be relatively inactive metabolically, both in regard to<br />

the rate at which it was metabolized and the diversity <strong>of</strong> labelled compounds that originated from it. The<br />

results indicate that fluoroacetate is not initially primarily defluorinated to acetate since the labelled<br />

products arising from fluoroacetate differed qualitatively in important respects from those which arose from<br />

acetate. The present results are in line with the hypothesis that the relative insensitivity <strong>of</strong> D. cymosum to<br />

fluoroacetate should be ascribed to the fact that this plant does not readily convert fluoroacetate to<br />

fluorocitrate.<br />

Elsden, S. R. and Ormerod, J. G (1956). The effect <strong>of</strong> mon<strong>of</strong>luoroacetate on the metabolism <strong>of</strong><br />

Rhodospirillum rubrum. The Biochemical Journal 63, 691-701.<br />

Keywords: metabolism/bacteria/fluoroacetate/toxicity<br />

Emlen, J. T. and Stokes, A. W. (1947). Effectiveness <strong>of</strong> various rodenticides on populations <strong>of</strong> brown rats<br />

in Baltimore, Maryland. American Journal <strong>of</strong> Hygiene 45, 254-257.<br />

Keywords: rats/1080/efficacy<br />

Abstract: Five <strong>poisons</strong> (ANTU, thallium sulfate, 1080, zinc phosphide and arsenic trioxide) gave good or<br />

moderately good kills when presented in standard corn bait to groups <strong>of</strong> wild brown rats in a large indoor<br />

pen; two (strychine sulfate and fortified red squill) gave poor kills. Of 3 poison selected as reasonably safe<br />

for field work in residential communities and exposed in various bait preparations to free-living populations<br />

in city-block test units, only one (ANTU) gave good kills.<br />

Emlen, J. T. and Strecker, R. L. (1951). The effect <strong>of</strong> laboratory confinement on survival <strong>of</strong> poisoned house<br />

mice. Ecology 32, 331-332.<br />

Keywords: mice<br />

Emptage, M. Mechanistic studies <strong>of</strong> a fluoroacetate dehalogenase. Enzyme Mechanisms Conference III ,<br />

A1197-Abstract 839. 1973.<br />

Ref Type: Conference Proceeding<br />

Keywords: fluoroacetate/bacteria/enzyme/degradation<br />

Abstract: We have isolated from activated sewage sludge a psuedomonad which has the ability to grow on<br />

the toxic fluoroacetate as its sole carbon and energy source. From this organism we have purifed to<br />

homogeneity a haloacid dehalogenase that converts fluoroacetate to glycolate. The enzyme has a monomer<br />

molecular weight <strong>of</strong> about 35 000 and contains no detectable metals or c<strong>of</strong>actors. The thermodynamically<br />

difficult reaction <strong>of</strong> breaking a methyl carbon-fluorine bond is catalyzed at reasonable rates (kcat= 20 sec-1,<br />

59


1080 Reassessment Application October 2006<br />

Appendix C<br />

Km=1 mM). The pH pr<strong>of</strong>iles <strong>of</strong> kcat and kcat/Km suggest a single catalytic base (pKa=7), presumably<br />

involved in deprotonating water. The enzymic reaction occurs via an SN2 mechanism as evidenced by 1)<br />

conversion <strong>of</strong> (S)-2-chloroproprionate to (R)-lactate, 2) conversion <strong>of</strong> only the (S)-isomer <strong>of</strong> racemic αfluorophenylacetate<br />

to (R)-mandelate, and 3) slow tight-binding inhibition by vanadate. Vanadate is known<br />

to form pentacoordinate structures which apparently mimic the the SN2 transition site.<br />

Emptage, M., Tabinowski, J., and Odom, J. M. (1997). Effect <strong>of</strong> fluoroacetates on methanogenesis in<br />

samples from selected methanogenic environments. Environ Sci Technol 31, 732-734.<br />

Keywords: fluoroacetate/degradation/bacteria/persistence in soil/inhibition/toxicity<br />

Abstract: Trifluoroacetic acid (TFA) is an atmospheric decomposition product <strong>of</strong> a new generation <strong>of</strong><br />

refrigerants that will replace current ozone-depleting CFCs. The effect <strong>of</strong> TFA on microbial<br />

methanogenesis was assessed using environmental samples from four distinct methanogenic systems; the<br />

anaerobic digestor, the rumen, freshwater sediments and marine sediments. TFA exhibited no toxicity, as<br />

evidenced by the rate <strong>of</strong> methanogenesis, at concentrations up to 10 mM. [1-14C]TFA was used to test for<br />

biodegradation (release <strong>of</strong> 14CO2) in methanogenic marine sediments. No significant release <strong>of</strong> 14CO2<br />

was observed. As a control, the toxic mon<strong>of</strong>luoroacetate (MFA) which is not an atmospheric degradation<br />

product <strong>of</strong> CFC replacements, was found to inhibit methanogenesis in freshwater and anaerobic digestor<br />

samples at or above concentrations <strong>of</strong> 0.1 mM. We conclude that TFA is inert in these methanogenic<br />

systems and there is no evident toxicity to either the methanogenic or fermentative populations.<br />

Emsley, J. Plants that can do what chemists can't. New scientist 29 November, 15. 1992.<br />

Ref Type: Magazine Article<br />

Keywords: occurrence in nature/biosynthesis/fluoroacetate<br />

Environmental Health Service. Code <strong>of</strong> Practice on the safe use and management <strong>of</strong> 1080. July 2000. 2000.<br />

Shenton Park, West Australia, Environmental Health Service.<br />

Ref Type: Pamphlet<br />

Keywords: 1080<br />

Environmental Risk Management Authority. User guide to the HSNO Thresholds and Classifications.<br />

2001. Wellington, New Zealand, Environmental Risk Management Authority.<br />

Ref Type: Report<br />

Keywords: regulatory toxicology/lethal concentration/legislation/1080<br />

Erlichman, J. S., Li, A., and Nattie, E. E. (1998). Ventilatory effects <strong>of</strong> glial dysfunction in a rat brain stem<br />

chemoreceptor region. Journal <strong>of</strong> applied physiology 85, 1599-1604.<br />

Keywords: mode <strong>of</strong> action/pathology/treatment/brain/fluorocitrate/analysis<br />

Abstract: Glia are thought to be important in brain extracellular fluid ion and pH regulation, but their role in<br />

brain stem sites that sense pH and stimulate breathing is unknown. Using a diffusion pipette, we<br />

administered the glial toxin, fluorocitrate (FC; 1 mM) into one such brain stem region, the retrotrapezoid<br />

nucleus (RTN) for 45-60 min. This dose and time period were chosen so that the effects <strong>of</strong> FC would be<br />

largely reversible. Within minutes, tissue pH decreased, and respiratory output increased. Both recovered<br />

almost completely after cessation <strong>of</strong> FC administration. The response to systemic CO2 stimulation was<br />

unaffected by FC treatment compared with that following control diffusion. Anatomic analysis showed, at<br />

the center <strong>of</strong> FC administration, some small (mean diameter = 5.1 mu m) cells that stained for DEAD Red,<br />

a marker for altered cell membrane permeability, and some fragmented glia (glial fibrillary acidic protein<br />

immunohistochemistry). The average RTN tissue volume that contained such DEAD Red-positive cells<br />

was 271 nl, similar to 23% <strong>of</strong> the volume <strong>of</strong> one RTN region. Reversible disruption <strong>of</strong> glia in the RTN, a<br />

region known to contain central chemoreception, results in an acidic local pH and in stimulation <strong>of</strong><br />

respiratory output.<br />

Evans, B. and Soulsby, R. (1993). The impact <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) rabbit poisoning<br />

operations on California quail populations. (Otago Fish and Game Council: Dunedin.)<br />

Keywords: non-target species/rabbits/birds/1080/poisoning<br />

60


1080 Reassessment Application October 2006<br />

Appendix C<br />

Everard, C. O. R. and Everard, J. D. (1992). Mongoose rabies in the Caribbean. Annals <strong>of</strong> the New York<br />

Academy <strong>of</strong> Sciences 653, 356-366.<br />

Keywords: strychnine/sodium fluoroacetate/fluoroacetate/1080/baits/poisoning/serum<br />

Abstract: Mongooses (Herpestes auropunctatus) have been introduced into most <strong>of</strong> the larger Caribbean<br />

islands, some notable exceptions being Dominica, Tobago and Montserrat. Rabies in Caribbean mongooses<br />

is present in Puerto Rico, Cuba, the Dominican Republic (and presumably Haiti), and Grenada. Bat rabies<br />

is known on Cuba, Grenada and Trinidad, although mongooses found on Trinidad are free <strong>of</strong> the disease.<br />

None <strong>of</strong> the other islands is known to have rabies, although it could be present in sequestered bat<br />

populations. All reported case numbers <strong>of</strong> mongoose rabies in the Caribbean are underestimates, and<br />

available information is at best incomplete and at times fragmentary. Nevertheless, data are presented from<br />

the 4 affected islands. Mongoose reduction campaigns have been undertaken on Cuba and Grenada. In<br />

Cuba strychnine sulfate inoculated into labelled eggs is used, whereas in Grenada sodium fluoroacetate<br />

(1080) has been used in boiled cowhide baits. Mongoose poisoning is unsatisfactory and ineffective in the<br />

long-term. Because many mongooses naturally exposed to rabies virus develop serum neutralizing<br />

antibodies and are considered to be immunized possibly for life, vaccination in the wild has been under<br />

consideration since the mid-1970s. Early attempts to produce a pill coated with ERA vaccine for enteric<br />

absorption in mongooses were not very successful, but new modified vaccines and recombinant techniques<br />

hold considerable promise<br />

Fagerstone, K. A., Savarie, P. J., Elias, D. J., and Schaffer Jr., E. W. (1994). Recent regulatory<br />

requirements for pesticide registration and the status <strong>of</strong> Compound 1080 studies conducted to meet EPA<br />

requirements. In 'Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14 December 1993, Christchurch, New<br />

Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 33-38. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: 1080/acute toxicity/aquatic species/dermal/non-target species/product chemistry/regulatory<br />

toxicology<br />

Abstract: In the U.S., pesticides are registered by the Environmental Protection Agency (EPA) under the<br />

Federal Insecticide, Fungicide, adn Rodenticide Act (FiFRA). This act was ammended in 1998 to require<br />

that each pesticide registered before 1984 be regiseted within a 9 year period. The registration process has<br />

increased data requirements and costs and has caused cancellation <strong>of</strong> many mior use pesticides that do not<br />

genrate sufficient pr<strong>of</strong>it to justify data generation costs.<br />

In 1998, the U.S. Environmental Protection Agency (EPA) notified registrants <strong>of</strong> its intent to cancel the<br />

registration for the only Compound 1080 technical product (held by Tull Chemical Co) and all Compound<br />

1080 rodenticide use registrations. These notifications occurred because the registrants had not submitted<br />

required data to maintain the registrations. All rodenticide uses were subsequently cancelled in 1990. This<br />

resulted in the loss <strong>of</strong> a chemical critical to managing vertebrate pests. However, EPA allowed the Animal<br />

and Plant Health Inspection Service (APHIS) to maintain a technical Compound 1080 registration for use<br />

only in the APHIS Livestock Protection Collar (LPC). APHIS is currently providing data to reregister the<br />

COMPOUND 1080 technical product. Prior to 1992, six product chemistry and three toxicology studies<br />

(acute dermal rabbit, eye irritation rabbit, and skin irritation rabbit) were submitted to the EPA, along with<br />

some non-target hazard studies. In a Data Call-In issued on September 30, 1992, EPA required only a<br />

minimal amount <strong>of</strong> additional data for the APHIS technical product. To date, APHIS has supplied 11<br />

studies to the EPA under the 1993 Data Call-In: eight product chemistry studies, bluegill sunfish and<br />

rainbow trout toxicity studies, and an aquatic invertebrate toxicity study. Avian dietary toxicity studies on<br />

bobwhite quail and mallard duck are scheduled to be completed in April 1994.<br />

Fairhurst, A. S., Smith, R. E., and Gal, E. M. (1958). The effects <strong>of</strong> fluorocompounds on oxidative<br />

phosphorylation II. Effects on the breakdown <strong>of</strong> nucleotides by liver mitochondria. Biochemical<br />

Pharmacology 1, 280-287.<br />

Keywords: liver/inhibition/biochemistry/fluorocitrate<br />

Abstract: The fluorocompounds generally increased the dephosphorylation <strong>of</strong> adenine and pyridine<br />

nucleotides. A definite quantitative and qualitative difference, however, existed with respect to the pattern<br />

<strong>of</strong> breakdown produced by the fluorocompounds from those resulting throught he action <strong>of</strong> DNP.<br />

Fairhurst, A. S., Smith, R. E., and Gal, E. M. (1958). The effects <strong>of</strong> fluorocompounds on oxidative<br />

phosphorylation I. Effects on P/O ratios with fumarate and with reduced diphosphopyridine nucleotide.<br />

Biochemical Pharmacology 1, 273-279.<br />

61


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: liver/inhibition/biochemistry/fluoroacetate/fluorocitrate<br />

Abstract: The effect <strong>of</strong> fluoroinhibitors on the oxidative phosphorylation <strong>of</strong> rat liver mitochondria has been<br />

studied. Fluoroacetate per se had no effect, while synthetic fluorocitrate and fluoropyruvate directly<br />

interfered with phosphorylation.<br />

Fall, M. W. and Jackson, W. B. (1998). A new era <strong>of</strong> vertebrate pest control? An introduction.<br />

International Biodeterioration and Biodegradation 42, 85-91.<br />

Keywords: regulatory toxicology<br />

Abstract: Vertebrate pest control has made substantial progress, worldwide, in the past century - moving<br />

from what were uncoordinated private efforts to trap, shoot, or poison animal pests to organized IPM<br />

approaches employing a variety pf pest control tactics. Some <strong>of</strong> the tools <strong>of</strong> the past are still critically<br />

important in these programs, but as new pest problems and new constraints arise, these tools are <strong>of</strong>ten<br />

found wanting. This paper briefly examines developments in vertebrate pest control in the past 100 years<br />

and summarizes some <strong>of</strong> the current lines <strong>of</strong> research that will carry us into the future.<br />

Fanshier, D. W., Gottwald, L. K., and Kun, E. (1962). Enzymatic synthesis <strong>of</strong> mon<strong>of</strong>luorocitrate from bfluoro-oxaloacetate.<br />

The Journal <strong>of</strong> Biological Chemistry 237, 3588-3596.<br />

Keywords: biochemistry/enzyme/fluorocitrate<br />

Fanshier, D. W., Gottwald, L. K., and Kun, E. (<strong>1964</strong>). Studies on specific enzyme inhibitors. VI.<br />

Characterization and mechanism <strong>of</strong> action <strong>of</strong> the enzyme-inhibitory isomer <strong>of</strong> mon<strong>of</strong>luorocitrate. The<br />

Journal <strong>of</strong> Biological Chemistry 239, 425-434.<br />

Keywords: enzyme/fluorocitrate/inhibition/mode <strong>of</strong> action<br />

Abstract: As an approach to the study <strong>of</strong> controlling mechanisms <strong>of</strong> enzyme activity in complex systems,<br />

we are in the process <strong>of</strong> determining the influence <strong>of</strong> relatively minor chemical alterations (e.g. exchange <strong>of</strong><br />

one or more hydrogen by fluorine atoms) in well known enzyme substrate molecules on their reactivity<br />

with purified enzymes. The immediate purpose <strong>of</strong> these experiments is to obtain specific inhibitors for<br />

certain key enzymes, which then are further studied in complex biochemical systems with the aid <strong>of</strong> these<br />

specific inhibitors (1-5). In the course <strong>of</strong> this work an unexpected observation was made: the enzymatic<br />

condensation <strong>of</strong> acetyl coenzyme A with B-mon<strong>of</strong>luoro-oxaloacetate yielded in isomer <strong>of</strong> monfluorocitrate<br />

which did not inhibit aconitase (4). It seemed likely that this enzymatic reaction produced only <strong>of</strong> the four<br />

isomers <strong>of</strong> mon<strong>of</strong>luorocitrate. The elucidation <strong>of</strong> stereochemical and enzyme inhibitory relationships <strong>of</strong> the<br />

remaining three isomers to this enzymatically synthesized fluorocitrate has been the subject <strong>of</strong> further<br />

experiments. It will be shown in this paper that the aconitase-inhibitory effect <strong>of</strong> synthetic<br />

mon<strong>of</strong>luorocitrate is actually due to one isomer, synthesized enzymatically from fluoroacetyl coenzyme A<br />

and oxaloacetate. The separation <strong>of</strong> diastereoisomers <strong>of</strong> synthetic mon<strong>of</strong>luorocitrate acid and the<br />

comparison <strong>of</strong> chemical and enzyme-inhibitory properties <strong>of</strong> these with enzymatically formed isomers<br />

considerably diminished uncertainties regarding the true structure and mode <strong>of</strong> action <strong>of</strong> the inhibitory<br />

species <strong>of</strong> mon<strong>of</strong>luorocitric acid.<br />

Fawcett, J., Blakeley, T., and Woodward, A. A scoping study regarding the health <strong>of</strong> workers in the pest<br />

control industry - report to the Animal Health Board. R-80567- report sourced electronically via P.<br />

Fairbrother, AHB, -32. 2002.<br />

Ref Type: Report<br />

Keywords: 1080/toxicity/humans/poisoning/occupational exposure/heart<br />

Abstract: The safety <strong>of</strong> 1080 (sodium mon<strong>of</strong>louroacetate) is an important issue in New Zealand because the<br />

chemical is biologically active in a wide range <strong>of</strong> animal species, and is widely used as a pest control agent.<br />

Each year the amount <strong>of</strong> 1080 applied in New Zealand is estimated to exceed its total use in all other<br />

countries combined. To date, knowledge <strong>of</strong> 1080 toxicity in humans largely relies on case reports from<br />

acute poisonings and extrapolation from animal experiments. If humans in New Zealand are exposed to<br />

1080, this is most likely to occur amongst workers who are manufacturing and distributing 1080 products,<br />

and health effects will should also be first evident in this group.<br />

This report examines the availability, completeness, access to and quality <strong>of</strong> information needed to conduct<br />

a study <strong>of</strong> chemical exposures and the health <strong>of</strong> workers in the pest control industry.<br />

62


1080 Reassessment Application October 2006<br />

Appendix C<br />

We have found that the population at risk <strong>of</strong> occupational exposure to 1080 can be readily defined from<br />

lists <strong>of</strong> licence-holders. A full historical cohort based on all 1080 licensees would have enough power to<br />

detect an increased risk <strong>of</strong> heart disease, provided a high level <strong>of</strong> follow-up was achieved. However, we<br />

advise against attempting to carry out such a study. In our view, the historical data are not adequate to<br />

develop a robust measure <strong>of</strong> personal exposures to 1080. Moreover, there is insufficient information in the<br />

historical employment records to confidently link license holders with records <strong>of</strong> subsequent hospitalisation<br />

and mortality. Employment records since 1989 are likely to be more complete but the fragmentation <strong>of</strong> the<br />

workforce in recent years would increase the complexity <strong>of</strong> any study and add a degree <strong>of</strong> variability to any<br />

measures based on employment histories.<br />

A cross-sectional study <strong>of</strong> the current workforce would be achievable provided all (or most) contractors<br />

could be identified and agreed to participate. However the demographic pr<strong>of</strong>ile <strong>of</strong> this occupational group<br />

suggests that recruitment to and retention in such a study would be challenging. Follow-up <strong>of</strong> a crosssectional<br />

study <strong>of</strong> the current workforce could be achieved. Such a study would provide the most robust<br />

exposure measurements and enable assessment <strong>of</strong> potential confounders. A cross-sectional survey would<br />

also provide a sampling frame for further more intensive health assessment studies with greater sensitivity<br />

to detect impaired function. Finally, a cross-sectional study <strong>of</strong> the current workforce, or the could form the<br />

baseline data for a prospective cohort study.<br />

We recommend that the Animal Health Board:<br />

• Does not carry out a retrospective cohort study<br />

• But does investigate further the possibility <strong>of</strong> conducting a cross-sectional survey.<br />

If a cross-sectional study is carried out, we recommend it is implemented in such a way that<br />

• it can be converted to a prospective cohort study at a later date<br />

• it may be used as a sampling frame for more intensive health studies <strong>of</strong> workers with different<br />

exposure pr<strong>of</strong>iles<br />

Feldwick, M. G., Mead, R. J., and Kostyniak, P. J. (1993). Biochemical effects <strong>of</strong> fluoroacetate and related<br />

pesticides: The potential <strong>of</strong> 4-methylpyrazole as an antidote. Proceedings <strong>of</strong> the science workshop on 1080,<br />

<strong>Royal</strong> Soc.<strong>of</strong> NZ Miscellaneous series 28. 28 , 1-10.<br />

Keywords: fluoroacetate/antidote/sodium<br />

fluoroacetate/citrate/metabolism/enzyme/treatment/aconitase/fluorocitrate/1,3-difluoro-2-propanol/4methylpyrazole<br />

Abstract: Administration to rats <strong>of</strong> sodium fluoroacetate (1.5 mg kg-1 body wt) resulted in a three fold<br />

increase in kidney citrate levels within 1 h <strong>of</strong> dosing. Administration to rats <strong>of</strong> 1,3-difluoro-2-propanol<br />

(DFP) (100 mg kg-1 body wt), the major ingredient <strong>of</strong> the pesticide gliftor, also resulted in citrate<br />

accumulation in the kidney but only after a 2 h lag phase. Inhibition <strong>of</strong> aconitate hydratase activity and<br />

elevation <strong>of</strong> kidney citrate levels in the DFP-treated animals was a consequence <strong>of</strong> the metabolism <strong>of</strong> DFP<br />

to (-)erythr<strong>of</strong>luorocitrate. A standard curve relating aconitate hydratase inhibition to concentration <strong>of</strong><br />

fluorocitrate was employed to determine the pattern <strong>of</strong> kidney fluorocitrate accumulation for each<br />

treatment. Kidney fluorocitrate accumulation patterns for both sodium fluoroacetate and DFP-treated<br />

animals were found to correspond closely with their respective citrate accumulation pr<strong>of</strong>iles. Intraperitoneal<br />

injection <strong>of</strong> 4-methylpyrazole (90 mg kg-1 body wt), 2 h prior to sodium fluoroacetate administration had<br />

no effect on the accumulation <strong>of</strong> either kidney citrate or fluorocitrate. In contrast, kidney citrate<br />

accumulation was significantly reduced when 4-methylpyrazole was administered to rats 2 h prior to DFP.<br />

Kidney fluorocitrate levels were also found to be significantly reduced in these animals and they displayed<br />

no signs <strong>of</strong> intoxication. The antidotal effects <strong>of</strong> 4-methylpyrazole were found to be due to its inhibition <strong>of</strong><br />

an NAD+ - dependent alcohol dehydrogenase involved in the conversion <strong>of</strong> DFP to difluoroacetone, an<br />

intermediate in the pathway <strong>of</strong> (-)erythr<strong>of</strong>luorocitrate synthesis.<br />

Feldwick, M. G., Noakes, P. S., Prause, U., Mead, R. J., and Kostyniak, P. J. (1998). The biochemical<br />

toxicology <strong>of</strong> 1,3-difluoro-2-propanol, the major ingredient <strong>of</strong> the pesticide gliftor: the potential <strong>of</strong> 4methylpyrazole<br />

as an antidote. Journal <strong>of</strong> Biochemical and Molecular Toxicology 12, 41-52.<br />

Keywords: 1,3-difluoro-2-propanol/4methylpyrazole/antidote/rats/citrate/kidney/aconitate/fluoride/defluorination/poisoning/fluoroacetate/1080/f<br />

63


1080 Reassessment Application October 2006<br />

Appendix C<br />

luoroacetamide<br />

Abstract: Administration to rats <strong>of</strong> 1,3-difluoro-2-propanol (100 mg kg-1 body weight), the major<br />

ingredient <strong>of</strong> the pesticide gliftor, resulted in accumulation <strong>of</strong> citrate in the kidney after a 3 hour lag phase.<br />

1,3-Difluoro-2-propanol was found to be metabolized to 1,3-difluoroacetone and ultimately to the aconitate<br />

hydratase inhibitor (-) erythr<strong>of</strong>luorocitrate and free fluoride. The conversion <strong>of</strong> 1,3-difluoro-2-propanol to<br />

1,3-difluoroacetone was found to be catalyzed by an NAD(+)-dependent alcohol dehydrogenase, while the<br />

defluorination was attributed to microsomal monooxygenase activity induced by phenobarbitone and<br />

inhibited by piperonyl butoxide. 4-Methylpyrazole was found to inhibit both <strong>of</strong> these processes in vitro and<br />

when administered (90 mg kg-1 body weight) to rats, 2 hours prior to 1,3-difluoro-2-propanol, eliminated<br />

signs <strong>of</strong> poisoning, prevented (-) erythr<strong>of</strong>luorocitrate synthesis, and markedly decreased citrate and fluoride<br />

accumulation in vivo. 4-Methylpyrazole also appeared to diminish (-) erythr<strong>of</strong>luorocitrate synthesis from<br />

fluoroacetate in vivo, and this was attributed to its capacity to inhibit malate dehydrogenase activity. The<br />

antidotal potential <strong>of</strong> 4-methylpyrazole and the potential for 1,3-difluoro-2-propanol to replace<br />

fluoroacetate (compound 1080) as a vertebrate pesticide is discussed<br />

Filip, J., Novak, L., Sikulova, J., and Kolacny, I (1970). Body temperature during fluoroacetate poisoning<br />

in rats. Physiologia bohemoslovaca 19, 123-127.<br />

Keywords: acute toxicity/fluoroacetate/poisoning/rats/rodents/temperature/lethal dose<br />

Findley, G. M. Use <strong>of</strong> 1080 poison for agricultural pest control. 1-36. 1980. Wellington, Agricultural Pests<br />

Destruction Council.<br />

Ref Type: Report<br />

Keywords: 1080/dogs/poison/<strong>poisons</strong>/rabbits/strychnine<br />

Abstract: Opossum control for animal health reasons cannot be effectively carried out without the use <strong>of</strong><br />

1080. It is an impossible task to cover effectively with other <strong>poisons</strong> large tracts <strong>of</strong> indigenous forest, gorse<br />

and scrub, which are usually ideal opossum habitat, to obtain the level required for animal health purposes.<br />

Furthermore, the topography is such that manpower alone cannot cover the ground successfully and<br />

thoroughly. Even where possible the cost <strong>of</strong> using manpower alone with the less efficient methods would<br />

at least double or treble the cost with a lot lower percentage kill which in the long-term would force<br />

continuing operations.<br />

Rabbit control without 1080, particularly in the high country <strong>of</strong> both islands, would force the use <strong>of</strong> less<br />

effective <strong>poisons</strong> and methods. It is impossible to control rabbits in the rough inaccessible areas without<br />

the use <strong>of</strong> an efficient poison.<br />

If the agricultural pests destruction movement was forced once again to resort to the use <strong>of</strong> arsenic and<br />

strychnine the cost would increase.<br />

Rabbit control without poison would be impossible in rough areas. While it could be possible to control<br />

some areas <strong>of</strong> New Zealand with the less effective methods (e.g. dogs, traps, night shooting) the cost would<br />

double or treble what it is today. This would be brought about by the immediate need for large increases in<br />

staff and equipment.<br />

1080 is the most efficient poison for the control <strong>of</strong> animal pests that affect agricultural production.<br />

Unless a suitable replacement is made available before the use <strong>of</strong> 1080 is curtailed, the pest destruction<br />

movement cannot guarantee the protection it now <strong>of</strong>fers.<br />

Fine, A. (1989). The effects <strong>of</strong> fluorocitrate on renal glutamine, lactate, alanine, and oxygen metabolism in<br />

the dog. Can.J.Physiol.Pharmacol. 67, 641-644.<br />

Keywords: fluorocitrate/metabolism/dogs/citrate/inhibition/kidney<br />

Abstract: Acid-base status is considered the major factor controlling renal NH4 + production from glutamine,<br />

with maximal values found in chronic acidosis. However, metabolic inhibitors have been shown to<br />

increase NH4 + production without acid-base change; the mechanism for this increase is unclear.<br />

Fluorocitrate was administered to dogs with chronic metabolic alkalosis. Following fluorocitrate total renal<br />

NH4 + production rose from 32 + 5 to 104 + 15 µmol/(min . 100 mL glomerular filtration rate (GFR))<br />

(p


1080 Reassessment Application October 2006<br />

Appendix C<br />

remained unchanged following fluorocitrate, 584 + 29 vs. 549 + 29 µmol/(min . 100 mL GFR). These<br />

results demonstrate that in the presence <strong>of</strong> metabolic inhibition in the kidney, ATP production remains<br />

constant. This is achieved by increased utilization <strong>of</strong> one substrate, glutamine, when the ATP production<br />

from other substrates is reduced. Thus the necessity to maintain constant ATP production appears to<br />

modulate renal NH4 + production.<br />

Fisher, P., O'Connor, C. E., and Eason, C. T. Monitoring workers in the pest control industry against a<br />

Biological Exposure Index (BEI) for 1080. LCR0102/087, -10. 2002. <strong>Landcare</strong> <strong>Research</strong> Lincoln.<br />

Ref Type: Report<br />

Keywords: 1080/baits/carrot/humans/occupational exposure<br />

Abstract: • The workers involved in the two aerial cereal bait operations and one ground paste bait<br />

operation that were monitored appeared protected from above-BEI exposure to 1080.<br />

• Some workers monitored during the manufacture <strong>of</strong> 1080 baits, and during three aerial carrot bait<br />

operations, had instances <strong>of</strong> above-BEI exposure to 1080.<br />

• The exact source(s) or route(s) <strong>of</strong> exposure to 1080 during the factory manufacture <strong>of</strong> 1080 baits<br />

or carrot 1080 bait distribution processes cannot be identified from these results.<br />

• Continuation <strong>of</strong> worker monitoring against the BEI provides a means to ensure that 1080 handling<br />

practices and protective equipment minimise worker exposure to acceptable levels.<br />

Fisher, P., O'Connor, C. E., and Eason, C. T. Monitoring pest control factory workers against a biological<br />

exposure index (BEI) for 1080. LCR0102/135, -15. 2002. <strong>Landcare</strong> <strong>Research</strong> Lincoln.<br />

Ref Type: Report<br />

Keywords: 1080/analysis/baits/brodifacoum/cyanide/humans/occupational exposure/urine<br />

Abstract: • Present procedures appear adequate to protect most workers from exposure to 1080<br />

exceeding the BEI, on most occasions. However, ACP should confirm the identity <strong>of</strong> the workers against<br />

the numbered samples submitted to <strong>Landcare</strong> <strong>Research</strong> for analysis from April 2002, as some <strong>of</strong> these were<br />

above the BEI.<br />

• Two factory workers have had exposure to 1080 over the limit set by the BEI, which occurred<br />

during successive monitoring occasions, and in successive urine samples taken over a number <strong>of</strong> days each<br />

time. Protective procedures and equipment used by these individuals in 1080-handling tasks should be<br />

reviewed.<br />

• The comparatively high concentrations measured in samples from one worker in 2001 and 2002<br />

appear to be the result <strong>of</strong> contamination during sampling. Follow-up monitoring <strong>of</strong> this individual is<br />

recommended.<br />

• The exact point(s) or route(s) <strong>of</strong> exposure to 1080 during the factory manufacture <strong>of</strong> 1080 baits<br />

cannot be identified from these results.<br />

• No conclusions can be made regarding effects on the health <strong>of</strong> workers who had exposure levels<br />

over the BEI, from these results. The BEI is a measure <strong>of</strong> acceptable exposure to 1080 only.<br />

Recommendations<br />

• Monitoring <strong>of</strong> urine for concentrations <strong>of</strong> 1080 indicative <strong>of</strong> exposure should be continued in the<br />

long term for ACP factory workers. Especial emphasis should be given to the two workers who have been<br />

exposed to 1080, i.e. more frequent monitoring until they return samples consistently below the BEI<br />

following all procedures involving the handling <strong>of</strong> 1080.<br />

• ACP should consult Occupational Safety and Health (OSH) for advice regarding the<br />

implementation <strong>of</strong> an appropriate schedule for routine monitoring <strong>of</strong> workers for exposure to 1080, and<br />

appropriate responses when individual workers return samples that exceed the BEI.<br />

• All sample collection carried out on-site at the factories must adhere to strict clean-up protocols to<br />

avoid the risk <strong>of</strong> sample contamination. This should include removal <strong>of</strong> all protective clothing and<br />

showering before providing a sample into an appropriate clean container. Samples should be given in an<br />

area well away from the areas <strong>of</strong> the factory where 1080 is stored and handled.<br />

• Sample collection in future should be carried out within a 2-hour 'end <strong>of</strong> shift' period to enable a<br />

65


1080 Reassessment Application October 2006<br />

Appendix C<br />

strict comparison with the BEI.<br />

• Based on these results, consideration should be given to monitoring <strong>of</strong> pest control industry<br />

workers involved in production and/or use <strong>of</strong> other vertebrate pesticides, e.g. brodifacoum and cyanide.<br />

Fisher, P., Wright, G., and Eason, C. Water monitoring for contamination after aerial 1080 pest control<br />

operations. Water and wastes in NZ September 2003[20], 21. 2003.<br />

Ref Type: Magazine Article<br />

Keywords: persistence in water/residues/aerial control/analysis<br />

Abstract: Debate about the risks and benefits <strong>of</strong> using the vertebrate pesticide 1080 to control possums in<br />

New Zealand continues. In particular, the potential <strong>of</strong> aerially applied 1080 carrot or cereal pellet baits to<br />

contaminate water is a concern, especially the risk <strong>of</strong> 1080 contaminating water catchments used for human<br />

drinking supplies. The Pest <strong>Control</strong> and Wildlife Toxicology team at <strong>Landcare</strong> <strong>Research</strong> analyses water<br />

samples collected after aerial 1080 operations to check for any contamination by the pesticide. The<br />

<strong>Landcare</strong> <strong>Research</strong> Toxicology Laboratory maintains a database <strong>of</strong> water samples they have analysed,<br />

which includes the results from over 1550 water samples collected from streams on days immediately<br />

following 1080 baiting operations in an area. So far, water samples taken following 210 possum control<br />

operations, conducted in different areas throughout New Zealand during 1990 to 2003, have been analysed<br />

for 1080 concentrations. It is important to note that these samples have been taken predominantly from<br />

within or adjacent to baited areas, where there would be the greatest chance <strong>of</strong> detecting contamination<br />

were it to occur.<br />

Residues <strong>of</strong> 1080 can be detected in water at concentrations as low as 0.1 part per billion (ppb), which is<br />

equivalent to 0.1 microgram <strong>of</strong> 1080 per litre <strong>of</strong> water. Of the samples analysed to date, most (96.3%)<br />

contained no detectable residues <strong>of</strong> 1080. Residues were found in 3.7% (58) <strong>of</strong> all samples, but in most <strong>of</strong><br />

these (51) the 1080 measured was less than 1 ppb (Figure). Where positive results were found in water<br />

samples, these have been mostly in small streams and associated with the observation <strong>of</strong> bait in the water.<br />

Of the 1550 samples, 107 were taken from reticulated town water supplies (drinking water), but none <strong>of</strong><br />

these contained detectable 1080 residues.<br />

In the Drinking-Water Standards for New Zealand, issued in 2000 by the Ministry <strong>of</strong> Health, the<br />

Provisional Maximum Acceptable Value (PMAV) for 1080 in water is 3.5 ppb. The PMAV value is one<br />

that, on the basis <strong>of</strong> present knowledge, is not considered to cause any significant risk to the health <strong>of</strong> the<br />

consumer over a lifetime <strong>of</strong> consumption <strong>of</strong> the water. However, the Ministry <strong>of</strong> Health also recommends<br />

that water taken from catchments sown with 1080 baits should not be used for human supply until tests<br />

show that the concentration <strong>of</strong> 1080 is below 2 ppb. The figure <strong>of</strong> 2 ppb is an approximation <strong>of</strong> 50% <strong>of</strong> the<br />

PMAV value, and is applied to testing water for 1080 as a conservative measure.<br />

In the few instances where the 1080 concentration in water samples exceeded the 2 ppb threshold, this was<br />

limited to a single sample taken at a particular site. For example, a water sample collected 2 hours after an<br />

aerial operation at Te Kopia Scenic Reserve, Rotorua, in 1999 was 4 ppb, and a further sample taken from<br />

the same location 24 hours later was 1 ppb. These individual samples did not represent any hazard to<br />

human drinking water supplies.<br />

These ongoing results suggest that significant or prolonged contamination <strong>of</strong> waterways after 1080 baiting<br />

operations is unlikely if due care is taken by pest control operators in planning and running 1080 baiting<br />

operations. Regulations stipulate that poison baits must not be laid in any catchment that provides water for<br />

human consumption, except where approved by local authorities such as the Medical Officer <strong>of</strong> Health.<br />

Continued water sampling and testing following 1080 baiting operations are prudent actions to ensure<br />

minimal risk to the public <strong>of</strong> contaminated water, and more information about testing water for 1080 can be<br />

found at http://www.landcareresearch.co.nz/services/laboratories/toxlab/protocol_water.asp.<br />

Fisher, P., O'Connor, C., Radford, C., and Beasley, M. Occupational exposure <strong>of</strong> pest control industry<br />

workers to 1080: continued monitoring against a biological exposure index. <strong>Landcare</strong> <strong>Research</strong> Contract<br />

Report LC03/04/008, -14. 2003. Lincoln, <strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Report<br />

Keywords: occupational exposure/1080/carrot/baits/dermal/urine/humans/aerial control<br />

Abstract: Conclusions<br />

66


1080 Reassessment Application October 2006<br />

Appendix C<br />

• As indicated by previous monitoring efforts, workers with duties preparing toxic carrot baits in the<br />

field appear to be those with the highest potential for unacceptable exposure to 1080.<br />

• Review and modification <strong>of</strong> personal protective equipment used by workers in aerial carrot-baiting<br />

operations appeared to reduce the incidence <strong>of</strong> unacceptable (above-BEI) exposure, however individual<br />

worker practice is likely to have contributed to continuing detectable exposure to 1080.<br />

• A formal industry standard operating procedure for carrot baiting operations, including<br />

specifications for protective equipment and compliance monitoring would provide a consistent standard<br />

from which to determine whether the exposure <strong>of</strong> workers is being minimised in future.<br />

Recommendations<br />

• Establishment <strong>of</strong> an industry standard operating procedure for aerial carrot baiting operations<br />

should be considered in conjunction with worker training in the use <strong>of</strong> personal protective equipment,<br />

including correct procedures for selection, fit testing, cleaning/maintenance and storage.<br />

• Workers handling 1080 cereal pellet baits should further minimise their risk <strong>of</strong> dermal exposure by<br />

wearing gloves and washing frequently with clean water.<br />

• Worker compliance in the use <strong>of</strong> protective equipment when preparing or handling toxic baits or<br />

solutions should be obligatory during future operations. This includes proper use <strong>of</strong> face shields, masks and<br />

gloves at all times, and regular washing-<strong>of</strong>f <strong>of</strong> dye stains from bare skin using clean water.<br />

• In conjunction with this, regular worker monitoring during aerial carrot-baiting operations should<br />

continue, in order to ensure that 1080 handling practices and protective equipment continue to minimise<br />

worker exposure risk.<br />

• Where individual workers show detectable concentrations <strong>of</strong> 1080 in urine samples at the end <strong>of</strong><br />

an operation, clearance should be confirmed by monitoring for up to five days afterwards.<br />

• When interpreting the results <strong>of</strong> worker monitoring against the BEI, employers should consult<br />

Occupational Safety and Health, New Zealand, for advice on appropriate actions to minimise worker<br />

exposure.<br />

Fisher, P. and Eason, C. AHB Project No. R-10544 Review <strong>of</strong> the Regulatory Toxicology <strong>of</strong> Sodium<br />

Fluoroacetate (1080). <strong>Landcare</strong> <strong>Research</strong> Contract Report: LC0203/086, -11. 2003. Lincoln. New Zealand,<br />

<strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Report<br />

Keywords: regulatory toxicology/sodium fluoroacetate/fluoroacetate/1080/risk assessment/acute<br />

toxicity/toxicity/inhalation/testes/target organ/degradation/fish/invertebrates/algae<br />

Abstract: • There has been ongoing research to address concerns about the potential risks <strong>of</strong> using<br />

1080, resulting in a considerable literature and knowledge base about the compound. In particular, the last<br />

decade has seen an increasing focus on regulatory toxicology <strong>of</strong> 1080 and on field-based studies<br />

investigating the long-term effects <strong>of</strong> 1080 on non-target populations in New Zealand.<br />

• 1080 has high acute toxicity through the oral and inhalation routes.<br />

• 1080 is mildly irritating to the skin, and irritating to the eye.<br />

• 1080 is not mutagenic and is therefore not anticipated to be a carcinogen.<br />

• 1080 is a developmental toxicant, and can have teratogenic effects, effects on growth, and effects<br />

on reproductive tissue (testes) at particular doses and frequencies <strong>of</strong> exposure.<br />

• Heart and testes are especially recognised as target organs <strong>of</strong> 1080, although effects on other<br />

organs have been described.<br />

• 1080 is degraded in natural aquatic environments, due to both dilution and/or dispersion and biotic<br />

degradation. Acute toxicity to fish and aquatic invertebrates appears to be relatively low, although some<br />

algae and aquatic plants are sensitive to 1080.<br />

Fleming, P. J. S. and Parker, R. W. (1991). Temporal decline <strong>of</strong> 1080 within meat baits used for control <strong>of</strong><br />

wild dogs in New South Wales. Wildlife research 18, 729-740.<br />

Keywords: bait degradation/1080/dogs<br />

67


1080 Reassessment Application October 2006<br />

Appendix C<br />

Fleming, P. J. S., Thompson, J. A., and Nicol, H. I. (1996). Indices for measuring the efficacy <strong>of</strong> aerial<br />

baiting for wild dog control in north-eastern New South Wales. Wildlife research 23, 665-674.<br />

Keywords: efficacy/1080/poison/sodium fluoroacetate/fluoroacetate/dogs/treatment<br />

Abstract: The efficacy <strong>of</strong> aerial baiting with 1080 poison (sodium fluoroacetate) for the control <strong>of</strong> wild<br />

dogs (Canis familiaris familiaris and C. familiaris dingo) in the temperate rangelands <strong>of</strong> north-eastern New<br />

South Wales was studied. In each year from 1991 to 1993, 2 indices <strong>of</strong> the abundance <strong>of</strong> dogs, one a raw<br />

count <strong>of</strong> sets <strong>of</strong> footprints per km <strong>of</strong> transect (SF) and the other an ln-transformed frequency corrected for<br />

sightability <strong>of</strong> signs (CI), were used to quantify the changes in abundance caused by aerial baiting.<br />

Abundance <strong>of</strong> dogs at a nil-treatment site was estimated concurrently. The SF index found the 1991 baiting<br />

to be efficacious. Both measures <strong>of</strong> abundance showed baiting to be efficacious in 1992 and 1993.<br />

Reductions <strong>of</strong> 66.3-84.5% in the abundance <strong>of</strong> dogs at the treatment site were found for the CI measure.<br />

The SF measure displayed abundance changes <strong>of</strong> 76.1-91.1%. The indices <strong>of</strong> abundance measured prior to<br />

the annual baiting in 1992 and 1993 were similar, indicating that populations returned to their initial<br />

abundance within 1 year<br />

Forsberg, C. W., Egbosimba, E. E., and Maclellan, S. (1999). Recent advances in biotechnology <strong>of</strong> rumen<br />

bacteria: Review. Asian Australasian Journal <strong>of</strong> Animal Sciences 12, 93-103.<br />

Keywords: fluoroacetate/bacteria/enzyme/GMO<br />

Abstract: Recent advances in the biotechnology <strong>of</strong> ruminal bacteria have been made in the characterization<br />

<strong>of</strong> enzymes involved in plant cell wall digestion, the exploration <strong>of</strong> mechanisms <strong>of</strong> gene transfer in ruminal<br />

bacteria, and the development <strong>of</strong> vectors. These studies have culminated in the introduction and expression<br />

<strong>of</strong> heterologous glucanase and xylanase genes and a fluoroacetate dehalogenase gene in ruminal bacteria.<br />

These recent studies show the strategy <strong>of</strong> gene and vector construction necessary for the production <strong>of</strong><br />

genetically engineered bacteria for introduction into ruminants. Molecular research on proteolytic turnover<br />

<strong>of</strong> protein in the rumen is in its infancy, but a novel protein high in essential amino acids designed for<br />

intracellular expression in nominal organisms provides an interesting approach for improving the amino<br />

acid pr<strong>of</strong>ile <strong>of</strong> ruminal organisms<br />

Foss, G. L. (1948). The toxicology and pharmacology <strong>of</strong> methylfluoroacetate (MFA) in animals, with some<br />

notes on experimental therapy. Brit.J.Pharmacol. 3, 118-127.<br />

Keywords: treatment/mode <strong>of</strong> action/acute toxicity/pathology/humans<br />

Fowles, C. R. and Williams, J. R. (1997). Water quality monitoring in relation to a possum control<br />

operation on Mount Taranaki/Egmont. New Zealand Natural Sciences 23, 93-99.<br />

Keywords: persistence in water/1080/possums/fluoride<br />

Abstract: Public concerns about a possum control operation on Mount Taranaki/Egmont in 1993 and 1994<br />

included issues realting to potential effects <strong>of</strong> the use <strong>of</strong> 1080 poison on water quality and water usage; in<br />

particular domestic water supplies from catchment draining areas within the aerial poison application<br />

zones. A comprehensive water monitoring program was undertaken in response to these concerns. Natural<br />

surface waters within and outside the operational zones, major water supplies (raw and treated) and<br />

groundwaters were sampled and analyses for residues <strong>of</strong> 1080 and fluoride were performed. Sampling<br />

commenced in advance <strong>of</strong> the first aerial operation <strong>of</strong> 1080 and extended throughout the operational<br />

periods with two sites sampled more intensively to monitor any immediate impacts <strong>of</strong> the initial aerial<br />

poisoning operations within the National Park. The result showed no measurable impact <strong>of</strong> the possum<br />

control operation on 1080 and fluoride concentrations measured in any <strong>of</strong> the natural waters draining both<br />

the National Park and the buffer zones within the operational poisoning area or in the raw and treated<br />

doemstic supplies, or groundwaters monitored. The results <strong>of</strong> this intensive monitoring may provide<br />

guidelines for the assessment and establishment <strong>of</strong> appropriate moniotring <strong>of</strong> any future possum control<br />

operations <strong>of</strong> this nature.<br />

Frampton, C. M., Warburton, B., Henderson, R., and Morgan, D. R. (1999). Optimising bait size and 1080<br />

concentration (sodium mon<strong>of</strong>luoroacetate) for the control <strong>of</strong> brushtail possums (Trichosurus vulpecula).<br />

Wildlife research 26, 53-59.<br />

Keywords: field efficacy/possums/ground control/1080/lethal dose<br />

Abstract: A method is presented for quantitatively assessing the likely effectiveness <strong>of</strong> specific bait size and<br />

1080 concentration for controlling brushtail possums with a known weight distribution. Data from aerial<br />

68


1080 Reassessment Application October 2006<br />

Appendix C<br />

1080 operations for the control <strong>of</strong> brushtail possums in New Zealand show that estimates <strong>of</strong> the bait size<br />

and toxic concentration required derived fi om the mean parameters [pest weight, bait size, and lethal dose<br />

(LD95)] will not be accurate. This inaccuracy is most likely to lead to an underestimate <strong>of</strong> the amount <strong>of</strong><br />

toxin presented to each animal, so that many operations currently run the risk <strong>of</strong> sub-lethally dosing<br />

possums and thereby possibly inducing some degree <strong>of</strong> poison shyness. On the basis <strong>of</strong> more accurate<br />

quantitative assessments <strong>of</strong> bait effectiveness we recommend that the 1080 concentration be increased to<br />

0.15% and that baits less than 5 g be excluded to ensure that when mean possum weights are less than 3 kg<br />

more than 95% <strong>of</strong> possums are lethally dosed by a single bait.<br />

Fraser, K. W., Spurr, E., and Eason, C. Non target kills <strong>of</strong> deer and other animals from aerial 1080<br />

operations. Rod and Rifle 16[5], 20-22. 1995.<br />

Ref Type: Magazine Article<br />

Keywords: deer/1080/non-target species<br />

Abstract: Editorials and letters in recent issues <strong>of</strong> hunting magazines express concerns about the effects <strong>of</strong><br />

aerial 1080 (sodium mon<strong>of</strong>luoroacetate) poisoning operations for possum control on deer populations, other<br />

non target species and the environment. This article summarises the most recent available information on<br />

non-target kills and environmental effects <strong>of</strong> 1080. It is not usual in this magazine to cite references, but we<br />

have provided these details here for those readers who wish to examine the evidence more closely.<br />

Fraser, K. W. and Sweetapple, P. J. A comparison <strong>of</strong> the effectiveness <strong>of</strong> two toxic loadings (0.08% and<br />

0.15%) for control <strong>of</strong> deer during aerial 1080 poisoning using carrot baits. [LC9900/084], -22. 2000.<br />

Lincoln, Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract report.<br />

Ref Type: Report<br />

Keywords: field efficacy/aerial control/deer/1080/treatment/possums<br />

Abstract: Objectives: To determine whether higher deer kills can be achieved by using a toxic loading <strong>of</strong><br />

0.15% 1080 rather than 0.08% 1080 in a routine aerial poisoning operation using carrot baits, by comparing<br />

the reductions in red deer density achieved with the two treatments on Mt Titiraupenga in winter 1997.<br />

Conclusions: the reductions in red deer densities in our two treatment blocks (92.8% and 91.6%) were<br />

considerable higher than those recorded in similar studies (between c.30% and c.65%). We have been<br />

unable to demonstrate whether the higher toxic loading (0.15% 1080) was more effective in killing deer.<br />

Several other factors including the variation in pre-control densities <strong>of</strong> both red deer and possums between<br />

the two treatment blocks, the overall considerably lower possum densities throughout the study area, and<br />

the difference in predominant aspect (and possibly other habitat-related variables) are likely to have<br />

affected our comparison. Our post-control pellet-group density estimates suggest that residual red deer<br />

densities are greater than or equal to 0.3 deer/km 2 in each <strong>of</strong> the blocks. In the absence <strong>of</strong> recreational<br />

hunting and immigration from adjacent (controlled) areas, red deer numbers will take about 10 years to<br />

recover to their pre-control levels in each <strong>of</strong> the treatment blocks. Despite the considerable differences in<br />

pre-control possum densities and the present kills between two treatment blocks, residual possum numbers<br />

are now very low throughout the control area. It appears that the higher toxic loading did not adversely<br />

affect the possum kill in the 0.15% 1080 treatment block, although this result should be tested further under<br />

conditions where both treatment blocks used for the comparison are more similar in terms <strong>of</strong> possum<br />

densities, aspect, and other potential variables than was the case in the present study. Possum populations<br />

could take up to 10-13 years to recover to pre-control levels in the 0.15% 1080 block but are likely to<br />

recover quicker in the 0.08% block because <strong>of</strong> higher post-control densities.<br />

Fraser, W. Introduced Wildlife in New Zealand: A Survey <strong>of</strong> General Public Views. Bezar, C. 23, 1-45.<br />

2001. Manaaki Whenua Press, <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> Science Series.<br />

Ref Type: Report<br />

Keywords: legislation/wildlife<br />

Abstract: Issues involving introduced wildlife and their management are <strong>of</strong>ten controversial subjects,<br />

reflecting the diverse range <strong>of</strong> views held, particularly on environmental issues. Previously there has been<br />

little original research on public perceptions in relation to introduced wild animals and their management in<br />

New Zealand. Since public attitudes ultimately play some part in determining <strong>of</strong>ficial policy and can affect<br />

the success <strong>of</strong> some conservation and management programmes, there is a need for better understanding <strong>of</strong><br />

how people perceive introduced wildlife and related issues. Indeed, recent changes in environmental<br />

legislation make specific provision for some public consultation in areas such as national and regional pest<br />

69


1080 Reassessment Application October 2006<br />

Appendix C<br />

management strategies and the application <strong>of</strong> pesticides.<br />

One <strong>of</strong> the challenges facing the agencies responsible both for the conservation <strong>of</strong> New Zealand's native<br />

flora and fauna and for the control <strong>of</strong> introduced wild animals (either for conservation or economic reasons)<br />

is to reflect public sentiments in their policies and practices. I surveyed public attitudes on introduced<br />

wildlife and related issues in 1994 to document the range <strong>of</strong> views held, quantify the levels <strong>of</strong> support for<br />

various issues, and to provide a baseline for more detailed research. The results presented here illustrate<br />

the divergence <strong>of</strong> views that exist within contemporary New Zealand society.<br />

Freeman, A. B., Hickling, G. J., and Bannock, C. A. (1996). Response <strong>of</strong> the skink Oligosoma maccanni<br />

(Reptilia:Lacertilia) to two vertebrate pest control baits. Wildlife research 23, 511-516.<br />

Keywords: baits/lethal dose/reptiles/pindone<br />

Abstract: The attractiveness <strong>of</strong> two vertebrate pest-control baits (non-toxic RS5 and pindone-impregnated<br />

AgTech) to captive skinks (Oligosoma maccannii) was assessed with timelapse video and feeding trials in<br />

New Zealand. O. maccannii were attracted to both bait types. When dry, pindone baits were more palatable<br />

than RS5 baits. However, when wet the palatability <strong>of</strong> both baits increased and was similar. Bait size had<br />

no signficant effect on palatability. Lizards ate an average <strong>of</strong> 0.01 g <strong>of</strong> RS5 baits or 0.02 g <strong>of</strong> AgTech<br />

Pindone bait, over two days. On the basis <strong>of</strong> published susceptibility data, it is unlikely that this level <strong>of</strong><br />

consumption would expose skinks to lethal doses <strong>of</strong> these vertebrate pest toxins. Potential sublethal effects<br />

<strong>of</strong> such doses require further study.<br />

Frick, E. J. and Boebel, F. W. (1946). Clinical observation <strong>of</strong> "1080" poisoning. Veterinary medicine 41,<br />

196-198.<br />

Keywords: diagnosis/welfare/secondary<br />

poisoning/poisoning/1080/livestock/dogs/heart/mammals/symptoms/time to death<br />

Abstract: From this experiment one may say that "1080" poisoning; 1. seems to exert its action primarliy on<br />

teh heart 2. it is a slow-acting poison as far as solipeds are concerned 3. it is a very toxic chemical as<br />

indicated by the small amount that proved lethal - the lethal dose was 5 mg per kilogram bodyweight. 4.<br />

heart muscle from poisoned animals transmits the poison to other animals that may consume it. Apparently<br />

the poison has an affinity for cardiac tissue 5. there was rpactically no struggling or violence showed by<br />

any <strong>of</strong> the animals used in the test<br />

Frost, R. L., Parker, R. W., and Hanna, J. V. (1989). Detection <strong>of</strong> the pesticide Compound 1080 (sodium<br />

mon<strong>of</strong>luoroacetate) using fluorine-19 nuclear magnetic resonance spectroscopy. Analyst 114, 1245-1248.<br />

Keywords: NMR/1080<br />

Abstract: Fluorine-19 nuclear magnetic resonance (19F NMR) spectroscopic measurement were used to<br />

determine the chemical nature and amounts <strong>of</strong> organ<strong>of</strong>luorine in dosed meat baits. Earlier work implied that<br />

sodium mon<strong>of</strong>luoroacetate (compound 1080) in meat baits was broken down into other organ<strong>of</strong>luorine<br />

compounds such as fluorocitrate. No chemical evidence was found for such compounds. Only<br />

mon<strong>of</strong>luoroacetate was detected in the prepared 1080 bait samples. Once the baits have aged, aqueous<br />

extraction fails to recover all the added 1080. Analysis using 19F NMR confirmed that the 1080 present in<br />

the aqueous extracts <strong>of</strong> the bait is recovered by Kramer's liquid chromatography method. It was shown here<br />

that the aqueous extracts do not recover all the 1080 in the meat bait.<br />

Fry, D. M., Santolo, G., and Grau, C. R. Final report for interagency agreement: effects <strong>of</strong> compound 1080<br />

poison on turkey vultures. Department <strong>of</strong> Avian Sciences, University <strong>of</strong> California, davis, 44 pp. 1986.<br />

Ref Type: Unpublished Work<br />

Keywords: birds/1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/lethal<br />

dose/poisoning/temperature/sublethal effects/mammals/symptoms/resistance/secondary poisoning/rodents<br />

Abstract: A study <strong>of</strong> the effects <strong>of</strong> Compound 1080, sodium mon<strong>of</strong>luoroacetate (SMFA) was conducted<br />

with captive Turkey Vultures (Cathartes aura). Fifteen birds were dosed individually with SMFA in meat<br />

baits at levels <strong>of</strong> 20-100mg/kg body wt. The behavioural responses <strong>of</strong> dosed birds were monitored with<br />

video recordings and dose responses to sublethal and lethal doses were obtained. The sensitivity <strong>of</strong> Turkey<br />

Vultures to SMFA poisoning was temperature dependent over the range <strong>of</strong> 7.6-28.6 o C. Severe sublethal<br />

effects including ataxia (inability to perform voluntary muscular movements) and intention tremors <strong>of</strong> the<br />

head were observed at 75% <strong>of</strong> the lethal dose at both high and low temperatures. The debilitating effects <strong>of</strong><br />

high sublethal doses would probably result in death <strong>of</strong> dosed birds in the wild. The lethal dose at 8-9 o C<br />

70


1080 Reassessment Application October 2006<br />

Appendix C<br />

was 100mg/kg. The high lethal dose levels indicate that Turkey Vultures are more resistant to the effects <strong>of</strong><br />

SMFA than most species <strong>of</strong> mammals and birds. Emesis (vomiting) within 2-5 hr <strong>of</strong> exposure was a<br />

characteristic symptom <strong>of</strong> poisoned vultures, but the amount <strong>of</strong> SMFA regurgitated by dosed birds was not<br />

determined. Increasing clinical symptoms were observed with increasing doses <strong>of</strong> SMFA at each<br />

temperature studied. Clinical symptoms at 50% <strong>of</strong> the lethal dose included lethargy, wing and head droop,<br />

and difficulty <strong>of</strong> arousal from sleep. The onset <strong>of</strong> intention tremors occured 40-65 hr after a sublethal dose<br />

and tremors persisted 3 days at low doses and persisted undiminished for 11 days (until euthanasia) in<br />

severe cases. The high resistance <strong>of</strong> Turkey Vultures to SMFA indicates that birds are probably at low risk<br />

<strong>of</strong> lethal doses from secondary poisoning after consuming poisoned rodents, but the extent <strong>of</strong> permanence<br />

<strong>of</strong> the nervous system damage exemplified by intention tremors following sublethal doses is unknown.<br />

Fukuhara, R. and Nishikawa, Y. (1973). Effect <strong>of</strong> metabolic inhibitors on respiration, glycolysis and<br />

motility <strong>of</strong> goat spermatozoa under aerobic conditions. Unknown.<br />

Abstract: It was found that fluoride, mono-iodoacetate and fluoroacetate inhibited sperm motility, while<br />

2,4-dinitrophenol and arsenite stimulated initial vigorous motility which was not, however, maintained.<br />

With 10-4 and 10-3M cyanide, initial motility was good and well maintained<br />

Gajdusek, D. C. and Luther, G. (1960). Fluoroacetate poisoning : a review and report <strong>of</strong> a case. American<br />

Journal <strong>of</strong> Diseases <strong>of</strong> Children 79, 310-320.<br />

Keywords: diagnosis/treatment/mammals/non-target species/sodium fluoroacetate<br />

Abstract: Sodium fluoroacetate, commonly called "1080" has obtained wide-spread use since the war as a<br />

potent rodenticide. Because <strong>of</strong> its varied pharamacologic properties and biochemical interest, it has<br />

become increasinly important in laboratory studies. Experimentaol poisoning in laboratory animals was<br />

studied during and since the war by many workers, but no previous report <strong>of</strong> a case <strong>of</strong> human poisioning is<br />

know to us.<br />

A case <strong>of</strong> poisoining with what was probably relatively pure sodium fluorocetate in a 2 year old Negor<br />

cheild is reported. Cardic and central nervous system symptoms perdominates, as in experimental animals,<br />

but the chold recovered completely without sequelae.<br />

This clinical picture presented by this case is briefly compared with that seen in experimental poisoning ,<br />

and the literature on fluoroacetate poisoning is briefly reviewed.<br />

Gal, E. M., Peters, R A., and Wakelin, R. W. (1956). Some effects <strong>of</strong> synthetic fluoro compounds in the<br />

metabolism <strong>of</strong> acetate and citrate. Biochemistry 64, 161-168.<br />

Keywords: metabolism/citrate/biochemistry/fluoroacetate/rats<br />

Abstract: Injections into rats <strong>of</strong> some fluorocompounds followed by [2- 14 C]acetate led to reduction in the<br />

14 CO2 expired as follows; fluoroacetate 40%, fluorocitrate 30% and fluoropyruvate 50%. The carcasses <strong>of</strong><br />

the poisoned animals contained more radioactivity than the other tissues examined. In male rats, whereas<br />

generally flurooacetate induced no rise in citric acid content <strong>of</strong> the liver, fluorocitrate injections caused an<br />

immediate rise in the citric acid level.<br />

Gal, E. M. and Smith, R. E. (1960). Conditions affecting inhibition <strong>of</strong> the tricarboxylic acid cycle by<br />

fluoroacetate in rat liver mitochondria. P.S.E.B.M. 103, 401-404.<br />

Keywords: inhibition/fluoroacetate/liver/citrate/poisoning/fluorocitrate/rats/metabolism<br />

Abstract: In presence <strong>of</strong> fumarate, rat liver mitochondria responds with citrate acumulation to fluoroacetate<br />

poisoning. This response is not sex-dependent. There is a time lag to inhibitory effect <strong>of</strong> fluorocompounds<br />

on respiration. Rates <strong>of</strong> respiration <strong>of</strong> fluoroacetate and control system <strong>of</strong> starved and fed animals were in<br />

close agreement. Testosterone did not abolish the effect <strong>of</strong> fluoroacetate on fluorocitrate accumulation,<br />

wherease progesterone significantly reversed it only on liver mitochondria <strong>of</strong> male rats. Progesterone, like<br />

DNP, when in combination with fluoroacetate, inhibited respiration. In normal nutritional states, irradiation<br />

does not significantly increase citrate accumulation in the liver mitochondria <strong>of</strong> male rats.<br />

Gal, E. M., Drewes, P. A., and Taylor, N. F. (1961). Metabolism <strong>of</strong> fluoroacetic acid-2-C 14 in the intact rat.<br />

Archives <strong>of</strong> biochemistry and biophysics 93, 1-14.<br />

Keywords: metabolism/persistence in<br />

animals/fluoroacetate/excretion/kidney/liver/fluorocitrate/heart/brain/urine<br />

Abstract: Syntheses and purification <strong>of</strong> fluoroacetate 2-c14 is described. During a 4 day period following<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

injection <strong>of</strong> fluoroacetate into intact rats, 3% <strong>of</strong> the label appeared in the respiratory CO2 and 32% was<br />

excreted in the urine. Radioautography <strong>of</strong> the urinary ether extracts revealed at least seven radioactive<br />

components. The appearance <strong>of</strong> urinary fluoroacetate sharply decreased by 48 hr. While that <strong>of</strong> the<br />

fluorocitrate reached maximum in 24 hr. Fluorocitrate in the urine represented only 3% <strong>of</strong> the total<br />

radioactivity administered. The major radioactive component was not inhibitory to aconitase.<br />

Concentration <strong>of</strong> the label was very high in heart, kidneys, liver and brain. Percentage <strong>of</strong> radioactivity <strong>of</strong><br />

the homogenates <strong>of</strong> liver and kidney distributed equally within the subcellular fractions, but the<br />

concentration <strong>of</strong> activity was about four times greater in the mitochrondrial fraction <strong>of</strong> the kidney than in<br />

the liver. Fifteen times as much labeled fluorocitrate was found in the kidney as in the liver. Analysis <strong>of</strong><br />

liver constituents revealed incorporation <strong>of</strong> activity into fatty acids and small amounts <strong>of</strong> label in<br />

cholesterol. The results indicate the existence <strong>of</strong> several pathways <strong>of</strong> fluoroacetate metabolism hitherto not<br />

extensively investigated.<br />

Gal, E. M. (1972). Effect <strong>of</strong> fluoro compounds on metabolic control in brain mitochondria. In 'Carbon-<br />

Fluorine Compounds. Chemistry, Biochemistry & Biological Activities.'. pp. 77-93. (Associated Scientific<br />

Publishers: Amsterdam.)<br />

Keywords: brain/chemistry/biochemistry/liver/fluoroacetate/metabolism/enzyme/inhibition<br />

Abstract: Since the discovery <strong>of</strong> 'lethal synthesis' by Peters great effort has been expended on understanding<br />

the details <strong>of</strong> this mechanism and the total effect <strong>of</strong> the fluoroinhibitors in biological systems. Here we<br />

present data from our in vivo and in vitro experiments with radio-active fluoroinhibitors. Major points<br />

discussed are 1) comparison <strong>of</strong> the subcellular distribution <strong>of</strong> fluoroinhibitors in the rat liver and barin at<br />

convulsive and non-convulsive doses 2) recovery <strong>of</strong> fluoroinhibitors from brain mitochondria by densitygradient<br />

sedimentation 3) effect <strong>of</strong> DL-erythro-fluorocitarte on the ability <strong>of</strong> brain mitochondria to<br />

accumulate calcium in vitro and changes in the respiration-dependent mitochondrial calcium after<br />

administration <strong>of</strong> fluoroacetate 4) penetration <strong>of</strong> fluoro compounds into cerebral mitochondria and 5)<br />

changes in the metabolism and membrane transport <strong>of</strong> cerebral mitochondria as a function <strong>of</strong> enzyme<br />

inhibition by fluoro compounds<br />

Gallon, J. R., Ul-Haque, M. I., and Chaplin, A. E. (1978). Fluoroacetate metabolism in Gloeocapsa sp.<br />

LB795 and its relationship to acetylene reduction (nitrogen fixation). Journal <strong>of</strong> general microbiology 106,<br />

329-336.<br />

Keywords: metabolism/persistence in plants/fluoroacetate/algae<br />

Abstract: Sodium fluoroacetate (1mM) caused an accumulation <strong>of</strong> citrate and altered the lipid composition<br />

in cells <strong>of</strong> Gloeocapsa sp. LB795. It also inhibited acetylene reduction (nitrogen fixation) by the alga -<br />

markedly under aerobic conditions, but much less so in the absence <strong>of</strong> oxygen. This inhibition is largely<br />

the result <strong>of</strong> the conversion <strong>of</strong> fluoroacetate to fluorocitrate which, by inhibiting aconitate hydratase<br />

(EC4.2.1.3.), interrupts the synthesis <strong>of</strong> the 2-oxoglutarate required for the assimulation <strong>of</strong> NH4 + . The<br />

consequent accumulation <strong>of</strong> NH4 + within the cells <strong>of</strong> Gloeocapsa sp. inhibits nitrogenase synthesis and,<br />

since oxygen rapidly inactivates pre-existing nitrogenase, nitrogen fixation by Gloeocapsa sp. decreases<br />

under aerobic conditions.<br />

Gammie, J. (1980). Sodium fluoroacetate poisoning in a cat. Canadian Veterinary Journal 21, 64.<br />

Keywords: sodium fluoroacetate/fluoroacetate/poisoning/symptoms/treatment/1080<br />

Abstract: Clinical symptoms and treatment are described for a domestic cat which had consumed, and then<br />

vomited up within 1 hour, a dead chipmunk killed after eating 1080 treated bran laid for rodent control.<br />

Survival <strong>of</strong> the cat considered largely due to it having initially vomited up most <strong>of</strong> the dead chipmunk<br />

Gardner, P. R., Nguyen, D-D. H., and White, C. W. (1994). Aconitase is a sensitive and critical target <strong>of</strong><br />

oxygen poisoning in cultured mammalian cells and in rat lungs. Proceedings <strong>of</strong> the National Academy <strong>of</strong><br />

Sciences <strong>of</strong> the United States <strong>of</strong> America 91, 12248-12252.<br />

Keywords: aconitase/poisoning/enzyme/inhibition/fluoroacetate/fluorocitrate/poison/rats/citric acid<br />

Abstract: The effect <strong>of</strong> hyperoxia on activity <strong>of</strong> the superoxide-sensitive citric acid cycle enzyme aconitase<br />

was measured in cultured human epithelial-like A549 cells and in rat lungs. Rapid and progressive loss <strong>of</strong><br />

>80% <strong>of</strong> the aconitase activity in A549 cells was seen during a 24-hr exposure to a PO2 <strong>of</strong> 600 mmHg (1<br />

mmHg = 133 Pa). Inhibition <strong>of</strong> mitochondrial respiratory capacity correlated with loss <strong>of</strong> aconitase activity<br />

in A549 cells exposed to hyperoxia, and this effect could be mimicked by fluoroacetate (or fluorocitrate), a<br />

72


1080 Reassessment Application October 2006<br />

Appendix C<br />

metabolic poison <strong>of</strong> aconitase. Exposure <strong>of</strong> rats to an atmospheric PO2 <strong>of</strong> 760 mmHg or 635 mmHg for 24<br />

hr caused respective 73% and 61% decreases in total lung aconitase activity. We propose that early<br />

inactivation <strong>of</strong> aconitase and inhibition <strong>of</strong> the energy-producing and biosynthetic reactions <strong>of</strong> the citric acid<br />

cycle contribute to the sequelae <strong>of</strong> lung damage and edema seen during exposure to hyperoxia.<br />

Garre, V. and Torres Martinez, S. (1996). Mutants <strong>of</strong> Phycomyces blakesleeanus defective in acetyl-CoA<br />

synthetase. Fungal Genetics and Biology 20, 70-73.<br />

Keywords: resistance/fluoroacetate/acetate/analysis/bacteria<br />

Abstract: Mutants (9) <strong>of</strong> P. blakesleeanus were isolated based on their resistance to fluoroacetate. None <strong>of</strong><br />

the isolates used acetate as their sole carbon source. Genetic complementation experiments revealed that all<br />

the mutants belonged to the same complementation group. Biochemical analysis indicated that acetateinduced<br />

acetyl-CoA synthetase activity was abolished in all mutants. This suggested that they were affected<br />

in the gene coding for acetyl-CoA synthetase (facA)<br />

Gillies, C. A. and Pierce, R. J. (1999). Secondary poisoning <strong>of</strong> mammalian predators during possum and<br />

rodent control operations at Trounson Kauri Park, Northland, New Zealand. New Zealand journal <strong>of</strong><br />

ecology 23, 183-192.<br />

Keywords: field efficacy/secondary poisoning/non-target species/target<br />

species/possums/poisoning/predators/1080/brodifacoum/rodents/mammals/cats/carnivores/analysis<br />

Gillies, C. A. Managing Rodents on the New Zealand mainland--what options are currently available?<br />

Summary <strong>of</strong> a workshop session at the Department <strong>of</strong> Conservation 'mainland island' hui, Omapere, 20-23<br />

August 2001. Department <strong>of</strong> Conservation Internal Science Series No. 47, -20. 2002. Wellington,<br />

Department <strong>of</strong> Conservation.<br />

Ref Type: Report<br />

Keywords: brodifacoum/warfarin/pindone/cholecalciferol/1080/field efficacy/rodent/rats/mice<br />

Abstract: Since late 1998, staff at most Department <strong>of</strong> Conservation 'mainlan island' sites have been<br />

investigating alternatives to brodifacoum-laced baits laid in bait stations for controlling rodents. A<br />

workshop session was held as part <strong>of</strong> the 2001 annual 'mainland island' hui (meeting) to discuss and review<br />

the different rodent control techniques tried by managers on the New Zealand mainland since 1998, and to<br />

make recommendations regarding the issues surrounding the different techniques. The consensus was that<br />

currently there are two main options (other than brodifacoum) available for rodent control on the New<br />

Zealand mainland: kill-trapping and a range <strong>of</strong> other toxins (1080, cholecalciferol, warfarin and pindone).<br />

The main reported advantage <strong>of</strong> trapping was that the technique has a much greater public acceptance than<br />

toxins. Toxins, however, were reported to be less labour-intensive than trapping and can be used over<br />

relatively large areas. The most commonly expressed concern was that very little is understood about the<br />

impacts <strong>of</strong> mice and what techniques are available to control them.<br />

Gitter, S (1956). The influence <strong>of</strong> acetimide on citrate accumulation after fluoroacetate poisoning.<br />

Unknown 63, 182-187.<br />

Keywords: fluoroacetate/treatment/citrate/mode <strong>of</strong> action/poisoning<br />

Glusker, J. P. (1968). Mechanism <strong>of</strong> aconitase action deduced from crystallographic studies <strong>of</strong> its<br />

substrates. Journal <strong>of</strong> Molecular Biology 38, 149-162.<br />

Keywords: aconitase/biochemistry/citrate/enzyme<br />

Abstract: A mechanism for the interconversion <strong>of</strong> citrate, isocitrate and cis-aconitate ions by the enzyme<br />

aconitase is suggested.<br />

Glusker, J. P. (1992). Structural aspects <strong>of</strong> citrate biochemistry. Current Topics in Cellular Regulation 33,<br />

169-184.<br />

Keywords: citrate/biochemistry/enzyme<br />

Abstract: Analogs <strong>of</strong> citrate provide excellent probes <strong>of</strong> mechanism in citrate-utilizing enzymes. The basic<br />

principles listed here must hold, but now that the detailed structures <strong>of</strong> large proteins with bound substrate<br />

can be determined by X-ray diffraction techniques, the stereochemical significance <strong>of</strong> citrate can be furtehr<br />

investigated.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Godoy, H. M. and Villarruel, M. C. (1974). Myocardial adenine nucleotides, hexose phosphates and<br />

inorganic phosphate, and the regulation <strong>of</strong> phosph<strong>of</strong>ructokinase activity during fluoroacetate poisoning in<br />

the rat. Biochemical Pharmacology 23, 3179-3189.<br />

Keywords: mode <strong>of</strong> action/fluoroacetate/biochemistry/heart/rodents/poisoning/serum/citrate/citric<br />

acid/inhibition<br />

Abstract: Myocardial levels <strong>of</strong> adenine nucleotides, inorganic phopshate (Pi) and hexose phosphates were<br />

measured as a function <strong>of</strong> the time after fluoroacetate (FAc) administration (6 mg/kg ip) to the rat. ATP<br />

content was progressively depleted, reaching at 6 hr 60% and at 18 hr, 45% <strong>of</strong> the control values. AMP and<br />

ADP levels increased during the initial 2 hr and later declined. Intracellular Pi accumulated in great<br />

amounts, with a maximum at 4 hr, while serum Pi increased continusously throughout the experiment.<br />

Citrate levels reached a maximum at 6 hr and remained nearly constant thereafter. These results suggest<br />

that the energy reserves <strong>of</strong> the tissues are progressively exhausted during the intoxication and the the<br />

reactivation <strong>of</strong> the citric acid cycle by the accumulated citrate, postulated by previous authors, does not<br />

occur under the present conditions. Fructose diphopshate (FDP) levels were unlatered during the<br />

intoxication, while fructose-6-phosphate (F6P) and glucose-6-phopshate only showed transient initial<br />

increases. The FDP/F6P ration, which is indicative <strong>of</strong> intracellular phosph<strong>of</strong>ructokinase (PFK) activity, was<br />

not significanlty altered, in spite <strong>of</strong> the striking changes produced in the levels <strong>of</strong> PFK effectors. This<br />

suggests that the PFK activation usually occurred with a depletion if high-energy phosphates and Pi<br />

accumulation is blocked in the poisoned tissue. In vitro experiments were perdormed in which PFK activity<br />

was evaluated in the presence <strong>of</strong> concentrations <strong>of</strong> substrates and metabolites simulating those found in<br />

vivo. It was observed that in the physiological pH range (6.9 -7.1), PFK is stikingly activated in the assays<br />

corresponding to intoxicated hearts, regardless <strong>of</strong> the high citrate levels. The suggests that the activation<br />

assocaited with the fall <strong>of</strong> ATP is quantitatively more important than the citrate inhibition. However, at<br />

lower pH values this activation is not produced, irrespective <strong>of</strong> the levels <strong>of</strong> ATP, AMP, Pi or citrate. It is<br />

suggested that intracellular acidification, possibly assocaited with the accumulation <strong>of</strong> citric acid, might be<br />

the main factor responsible for the blockade <strong>of</strong> PFK activation observed in intoxicated hearts in vivo.<br />

Goldman, P. (1965). The enzymatic cleavage <strong>of</strong> the carbon-fluorine bond in fluoroacetate. Journal <strong>of</strong><br />

biological chemistry 240, 3434-3438.<br />

Keywords: product chemistry/fluorine/chemistry/analysis/fluoroacetate/soil/bacteria/enzyme/biochemistry<br />

Goldman, P. and Milne, G. W. (1966). Carbon-fluorine bond cleavage II. Studies on the mechanism <strong>of</strong> the<br />

defluorination <strong>of</strong> fluoroacetate. The Journal <strong>of</strong> Biological Chemistry 23, 5557-5559.<br />

Keywords: defluorination/fluoroacetate/chemistry/enzyme/biochemistry<br />

Abstract: Studies on the mechanism <strong>of</strong> the reaction XCH2COO<br />

- + OH- >> X- + HOCH2COO- (where X= F, Cl and I) catalyzed by<br />

the enzyme haloacetate halidohydrolase indicate that the hydroxyl group <strong>of</strong> glycolate is derived from water. No evidence can be obtained for the reversibility <strong>of</strong> the<br />

dehalogenation. In addition the exchanges between glycolate and H218O and between chloroacetate and 36Cl- are not catalyzed by the enzyme.<br />

Goldman, P. Enzymology <strong>of</strong> carbon-halogen bonds. 147-165. 12-6-1971. Degradation <strong>of</strong> synthetic orgnaic<br />

molecules in the biosphere : natural pesticidal and various other man-made compounds. Proceedings <strong>of</strong> a<br />

conference held in San Francisco, June 12-13 1971.<br />

Ref Type: Conference Proceeding<br />

Keywords: degradation/chemistry/fluorine/enzyme<br />

Goodwin, R. M. and Ten Houten, A. (1991). Poisoning <strong>of</strong> honey bees (Apis mellifera) by sodium<br />

fluoroacetate (1080) in baits. New Zealand journal <strong>of</strong> zoology 18, 45-51.<br />

Keywords: non-target species/invertebrates/possums/poisoning/sodium<br />

fluoroacetate/fluoroacetate/1080/baits/bees/honey/humans<br />

Gooneratne, R., Dickson, C., Wallace, D., Eason, C. T., Fitzgerald, H., and Wright, G. (1994). Plasma and<br />

tissue 1080 in rabbits after lethal and sub-lethal doses. In 'Proceedings <strong>of</strong> the Science Workshop on 1080,<br />

12-14 December 1993, Christchurch, New Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 67-73.<br />

(<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: metabolism/rabbits/persistence in animals/1080/non-target species/lethal dose<br />

Abstract: The persistence <strong>of</strong> 1080 in plasma, liver, kidney, and muscle was studied in rabbits administered<br />

sodium mon<strong>of</strong>luoroacetate (1080) at two dose levels (sub-lethal and lethal) with a view to assessing risk<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

from consumption <strong>of</strong> meat from lethally or sub-lethally poisoned rabbits by non-target species. The plasma<br />

elimination half-life in rabbits receiving a sub-lethal dose was 1.1 h. The tissue retention <strong>of</strong> 1080 was<br />

greater in rabbits dosed with lethal dose than those which received a sub-lethal dose. Irrespective <strong>of</strong> dose<br />

<strong>of</strong> 1080 given, the concentration <strong>of</strong> 1080 in muscles, kidney and liver was substantially lower than in<br />

plasma.<br />

The plasma fluoride (F) concentration in sub-lethally poisoned animals increased initially but returned to<br />

normal within 3 h. Elevation <strong>of</strong> plasma F in lethally dosed animals was higher (at least x3) and was the<br />

highest in animals which died early. In contrast the tissue F concentration in these animal was variable. In<br />

sub-lethally poisoned animals only muscle citrate was elevated. In contract, the tissue citrate<br />

concentrations in lethally dosed animals were variable but the plasma citrate levels were elevated in<br />

animals which died later. Abnormal electrocardiographs were recorded from 13% <strong>of</strong> rabbits given the sublethal<br />

dose.<br />

Gooneratne, S. R., Eason, C. T., Dickson, C. J., Fitzgerald, H., and Wright, G. (1995). Persistence <strong>of</strong><br />

sodium mon<strong>of</strong>luoroacetate in rabbits and risk to non-target species. Human and experimental toxicology<br />

14, 212-216.<br />

Keywords: persistence in animals/non-target species/rabbits/1080/lethal<br />

dose/birds/blood/liver/kidney/muscle/secondary poisoning<br />

Gordon, E. E. (1961). The metabolism <strong>of</strong> citrate-C 14 in normal and in fluoroinhibitor-poisoned rats.<br />

J.Clin.Invest. 40, 1719-1726.<br />

Keywords: metabolism/rats/blood/citrate/kidney/liver/fluoroacetate/fluorocitrate/excretion<br />

Abstract: The turnover <strong>of</strong> the blood citrate is extremely rapid as measured by the conversion <strong>of</strong><br />

intravenously administered citrate-C14 to respiratory C14O2. Approximately 85% <strong>of</strong> the radioactive carbon<br />

<strong>of</strong> the labeled citrate that is retained in the rat is converted to C14O2 in 3 hours. Approximately 1% <strong>of</strong> the<br />

administered radioactivity was recovered in protein and lipid in the kidneys and liver. The incorporation <strong>of</strong><br />

C14 into the kidney tissue fractions was greater than that into the corresponding liver fractions. In vivo and<br />

in vitro experiments demonstrated a divergent action <strong>of</strong> fluoroacetate and fluorocitrate as inhibitors <strong>of</strong><br />

metabolism. In the intact animal fluoroacetate treatment inhibited the urinary excretion <strong>of</strong> administered<br />

citrate-C14 and enhanced its conversion to respiratory C14O2, fluorocitrate treatment resulted in an<br />

augmentation <strong>of</strong> the urinary excreation <strong>of</strong> the citrate-C14 and depressed its conversion to respiratory<br />

C14O2. Studies <strong>of</strong> the metabolism <strong>of</strong> liver and the kidney slices in the presence <strong>of</strong> fluoroacetate and<br />

fluorocitrate indicated a difference in the mechanism <strong>of</strong> action <strong>of</strong> these inhibitors. Although the distribution<br />

<strong>of</strong> citrate in the subcellular fractions <strong>of</strong> liver differed from that found in kidney after fluoroinhibitor<br />

administration, the localization in each <strong>of</strong> the tissues was the same, regardless <strong>of</strong> whether the rat received<br />

fluoroacetate or fluorocitrate.<br />

Gorniak, S. L., Palermo-Neto, J, and Spinosa, H. S. (1994). Effects <strong>of</strong> acetamide on experimentally-induced<br />

Palcourea marcgravii (St Hill) poisoning in rats. Veterinary and human toxicology 36, 101-102.<br />

Keywords: poisoning/rats/antidote/convulsions/treatment/occurrence in nature<br />

Abstract: High indices <strong>of</strong> mortality in cattle have been reported in Brazil as a consequence <strong>of</strong> Palicourea<br />

marcgravii (Pm) acute intoxications. It has been established that Pm leaves contain mon<strong>of</strong>luoroacetic acid<br />

(MFA), the active toxic principle <strong>of</strong> the plant. Rational therapy for MFA poisoning involves the use <strong>of</strong> a<br />

substance that might prevent fluorocitric acid formation. The present work was undertaken to verify if<br />

acetamide, a MFA antidote and an acetate donor, protects rats against both Pm and MFA intoxications. It<br />

was verified that acetamide protected rats from both convulsions and death. Future experiments should be<br />

carried out on cattle to examine the efficacy <strong>of</strong> acetamide, and particularly under field conditions.<br />

Grant, W. E., Fraser, S. O., and Isakson, K. G. (1984). Effect <strong>of</strong> vertebrate pesticides on nontarget wildlife<br />

populations: Evaluation through modelling. Ecological Modelling 21, 85-108.<br />

Keywords: wildlife/1080<br />

Abstract: A general modeling methodology to evaluate the potential effects <strong>of</strong> pesticides on non-target<br />

wildlife populations is described, and its use within a resource management framework is demonstrated.<br />

Attention is focused on interfacing relatively simple numerical and analytical procedures with available<br />

data to specify initial baseline population parameters, representing density-dependent relationships<br />

affecting non-target natality and survival rates, and interpreting simulated non-target population responses<br />

75


1080 Reassessment Application October 2006<br />

Appendix C<br />

to different pesticide-use schemes within a management framework. The methodology involves use <strong>of</strong> a<br />

Leslie matrix model with variable age-specific natality and survival rates. Natality and survival rates can<br />

vary as a function <strong>of</strong> non-target population density, the density <strong>of</strong> competitor, predator, and/or prey<br />

populations, and/or abiotic environmental factors. Required model input includes estimates <strong>of</strong> initial<br />

density <strong>of</strong> the non-target population, age-specific natality rates, the relative magnitudes <strong>of</strong> age-specific<br />

survival rates, the relationship <strong>of</strong> natality and survival rates to the appropriate population densities and/or<br />

abiotic environmental factors, and the magnitude <strong>of</strong> pesticide-induced mortality. Model output includes<br />

estimates <strong>of</strong> the density <strong>of</strong> the non-target population over time, the mean lowest density reached, the mean<br />

recovery time, and the probability <strong>of</strong> extinction resulting from a specified scheme <strong>of</strong> pesticide use. Use <strong>of</strong><br />

the model within a management framework is demonstrated by evaluating the effects <strong>of</strong> 4 hypothetical<br />

coyote control schemes, using Compound 1080, on great horned owl populations in the United States<br />

Green, W. (2004). The use <strong>of</strong> 1080 for pest control - a discussion document. (Animal Health Board and the<br />

Department <strong>of</strong> Conservation: Wellington, New Zealand.)<br />

Greene, T. G. The effect <strong>of</strong> compound 1080 on populations <strong>of</strong> specific non-target species, Waihaha<br />

Ecological Area, Pureora Forest Park, winter 1994. 1995. Department <strong>of</strong> Conservation.<br />

Ref Type: Report<br />

Keywords: 1080/non-target species/birds<br />

Greentree, C., Saunders, G., McLeod, L., and Hone, J. (2000). Lamb predation and fox control in southeastern<br />

Australia. Journal <strong>of</strong> applied ecology 37, 935-943.<br />

Keywords: ground control/1080/treatment<br />

Gregg, K., Cooper, C. L., Schafer, D. J., Sharpe, H., Beard, C. E., Allen, G., and Xu, J. (1994).<br />

Detoxification <strong>of</strong> the plant toxin fluoroacetate by a genetically modified rumen bacterium. Bio/technology<br />

12, 1361-1365.<br />

Keywords: fluoroacetate/bacteria/degradation/GMO/occurrence in nature<br />

Abstract: The construction <strong>of</strong> rumen bacteria that are able to detoxify an important natural poison supports<br />

the feasibility <strong>of</strong> using genetically modified rumen bacteria to aid animal production.<br />

Gregg, K. (1995). Engineering gut flora <strong>of</strong> ruminant livestock to reduce forage toxicity: progress and<br />

problems. Tibtech 13, 418-421.<br />

Keywords: gut/livestock/bacteria/degradation/fluoroacetate/poisoning<br />

Abstract: The rumen bacterium Butyvibrio fibriosolvens has been genetically modified to detoxify<br />

fluoroacetate (a poisonous component <strong>of</strong> trees and shrubs in Australia, Africa and Central America) and has<br />

been shown to persist when it is returned to the rumen. Such bacteria may save animals from poisoning,<br />

thereby reducing economic losses for livestock industries in those countries. The ability to make genetic<br />

changes to rumen bacteria raises important questions about their practicality, and about the environmental<br />

factors that must be considered befire releasing modified strains. The fluoroacetate-detoxifying bacterium<br />

provides an important model by which these issues can be examined.<br />

Gregg, K., Hamdorf, B., Henderson, K., Kopecny, J., and Wong, C. (1998). Genetically modified ruminal<br />

bacteria protect sheep from fluoroacetate poisoning. Applied and environmental microbiology 64, 3496-<br />

3498.<br />

Keywords: metabolism/pathology/fluoroacetate/symptoms/poisoning<br />

Abstract: Four strains <strong>of</strong> Butyrivibrio fibrisolvens, transformed with a gene encoding fluoroacetate<br />

dehalogenase, maintained a combined population <strong>of</strong> 10(6) to 10(7) cells ml(-1) in the rumens <strong>of</strong> test sheep.<br />

Five inoculated sheep showed markedly reduced toxicological symptoms after fluoroacetate poisoning<br />

when behavioral, physiological, and histological effects were compared with those <strong>of</strong> five uninoculated<br />

control sheep.<br />

Gregory, G. Perception <strong>of</strong> pain associated with 1080 poisoning. 300-302. 1991. Adelaide.<br />

Ref Type: Conference Proceeding<br />

Keywords: 1080/poisoning/welfare/symptoms<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Greksak, M., Lopes-Cardozo, M., and van den Bergh, S. G. (1982). Citrate synthesis in intact rat-liver<br />

mitochondria is irreversible. European Journal <strong>of</strong> Biochemistry 122, 423-427.<br />

Keywords: citrate<br />

Abstract: Rat-liver mitochondria were incubated with [1,5- 14 C]citrate in the presence <strong>of</strong> fluorocitrate to<br />

block oxidation in the Krebs cycle. The reaction products were analysed enzymatically and by anionexchange<br />

chromatography. Incorporation <strong>of</strong> 14 C into acetyl-L-carnitine or ketone bodies via a backward<br />

action <strong>of</strong> citrate synthase was not observed. The optimal rate <strong>of</strong> citrate synthesis from pyruvate and malate<br />

in the presence <strong>of</strong> fluorocitrate was 15 nmol . mg -1 . min -1 . In the absence <strong>of</strong> fluorocitrate, but in the<br />

presence <strong>of</strong> malonate, citrate was oxidized to succinate at a rate <strong>of</strong> 4 nmol . mg -1 . min -1 .<br />

We conclude that the synthesis <strong>of</strong> citrate by intact rat liver mitochondria is an irreversible process. The<br />

possible mechanism underlying this phenomenon and the consequence for metabolic regulation are<br />

discussed<br />

Gribble, G. W. (1973). Fluoroacetate toxicity. Journal <strong>of</strong> chemical education 50, 460-462.<br />

Keywords: mode <strong>of</strong> action/acute toxicity/fluoroacetate<br />

Gribble, G. W. (2002). Naturally occurring organ<strong>of</strong>luorines. Organ<strong>of</strong>luorines 3, 121-136.<br />

Keywords: occurrence in nature<br />

Griffiths, M. E. (1959). The effect <strong>of</strong> weathering on the toxicity <strong>of</strong> baits treated with sodium fluoroacetate.<br />

CSIRO wildlife research 4, 93-95.<br />

Keywords: bait degradation/sodium fluoroacetate/fluoroacetate<br />

Grobbelaar, N. and Meyer, J. J. M. (1990). Fluoroacetate production by Dichapetalum cymosum. Journal <strong>of</strong><br />

plant physiology 135, 550-553.<br />

Keywords: fluoroacetate/occurrence in nature/biosynthesis/bacteria/fluoride<br />

Abstract: Field-grown Dichapetalum cymosum plants which appeared normal were invariably found to be<br />

infested with bacteria. It has not yet been ascertained whether the bacteria can synthesise fluoroacetate but<br />

seedlings <strong>of</strong> D. cymosum, when grown from surface sterilised seed in an aseptic environment, appear to<br />

synthesise fluoroacetate. A callus culture <strong>of</strong> D. cymosum was established which appears to be internally<br />

devoid <strong>of</strong> microorganisms. The culture grows well in the absence <strong>of</strong> fluoride and then does not contain<br />

fluoroacetate. Fluoride (0.78 to 6.24 mM) does not affect the growth <strong>of</strong> the callus but results in the<br />

production <strong>of</strong> up to 1227 mg fluoroacetate per kg fresh callus.<br />

Groenvald, A. H. C. and Berends, A. G. A comparison <strong>of</strong> the toxicity <strong>of</strong> sodium trifluoroacetate,<br />

difluoroacetic acid salt, sodium mon<strong>of</strong>luoroacetate and sodium fluoride to the alga Selenastrum<br />

capricornatum . 56835/44/94. 1994. Washington DC USA, AFAES. Alternative Fluorocarbons<br />

Environmental Acceptability Study Final Report.<br />

Ref Type: Report<br />

Keywords: algae/toxicity/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/fluoride<br />

Guan, F., Wu, H., and Luo, Y. (1996). Sensitive and selective method for the determination <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate by capillary zone electrophoresis. Journal <strong>of</strong> chromatography A 719, 421-426.<br />

Keywords: bait degradation<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (SMFA) is a highly toxic substance and its determination is needed in<br />

several areas. Its chromatographic (GC or HPLC) determination is difficult because <strong>of</strong> its ionic and<br />

hydrophilic properties. A simple, sensitive and selective capillary zone electrophoretic method is described<br />

for the determination <strong>of</strong> SMFA. It is well separated from structurally related compounds (formate, acetate,<br />

chloroacetate, bromoacetate, etc) in an acidic electrolyte buffer containing 5 mmol/1 phthalate (pH 4.61)<br />

and 0.3 mmol/1 cetyltrimethylammonium bromide (CTAB) or in a basic electrolyte solution containing 5<br />

mmol/14hydroxy benzoate 0.3 mmol/1 CTAB and 10 mmol/1 ammonium (pH 9.49). Good resolution was<br />

achieved at relatively low electric field (200250) kV/cm) and CTAB concentration (0.3 mmol/1). The<br />

separation selectivity was improved in acidic phthalate buffer. Using bromoacetate as internal standard, the<br />

calibration graph for SMFA was linear over the concentration range 110 jug/ml. The detection limit was<br />

0.4 jg/ml. The method was applied to the determination <strong>of</strong> SMFA in rodenticide baits<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Guan, F. Y., Miao, Z. C., and Luo, Y. (1994). A new method for detection and identification <strong>of</strong> sodium<br />

fluoroacetate and fluoroacetamide by NMR spectroscopy. Chinese science bulletin 39, 154-157.<br />

Keywords: NMR/sodium fluoroacetate/fluoroacetamide/fluoroacetate/analysis<br />

Guarriera-Bobyleva, V and Buffa, P. Changes in rat liver glycolytic reactions during fluoroacetate<br />

poisoning. Ananchenko, S. N. Frontiers <strong>of</strong> bioorganic chemistry and molecular biology : proeecings <strong>of</strong> the<br />

International Symposium, Moscow and Tashkent, USSR, 25 September - 2 October 1978. 185-191. 1980.<br />

Oxford, New York, Pergamon Press.<br />

Ref Type: Conference Proceeding<br />

Keywords: liver/fluoroacetate/poisoning/metabolism/chemistry<br />

Guarriera-Bobyleva, V., Hughes, P. E., and Lardy, H. A. (1984). Effect <strong>of</strong> fluoroacetate on hepatic<br />

gluconeogenesis. Fluoride 17, 94-104.<br />

Keywords: fluoroacetate/liver/birds<br />

Abstract: Studies on the effect <strong>of</strong> fluoroacetate on chicken liver gluconeogenesis revealed that fluoroacetate<br />

intoxication blocked the tricarboxylic acid cycle in fed or fasted birds; this decreased the generation <strong>of</strong> ATP<br />

required for gluconeogenesis A decrease <strong>of</strong> glucose synthesis with reduced substrates. Lactate was<br />

especially observed in isolated hepatocytes incubated with fluoroacetate which was explained by decreased<br />

amount <strong>of</strong> available energy for glucose synthesis, decreased activity <strong>of</strong> the malate shuttle and decreased<br />

activity <strong>of</strong> lactate dehydrogenase<br />

Guarriero-Bobyleva, V and Buffa, P. (1969). The inhibition <strong>of</strong> fluorocitrate <strong>of</strong> rat liver mitochondrial and<br />

extramitochondrial aconitate hydratase. Biochemistry Journal 113, 853-860.<br />

Keywords: inhibition/fluorocitrate/liver/enzyme/aconitase/biochemistry<br />

Abstract: The effects <strong>of</strong> synthetic fluorocitrate were studied on a) the oxidation <strong>of</strong> citrate and cis-aconitate<br />

by rat liver mitochondria b) the activity <strong>of</strong> the aconitate hydratse found in the liver cell sap c) the activity <strong>of</strong><br />

the aconitate hydratase solubilized from liver mitochondria. Fluorocitrate was found to be a potent inhibitor<br />

<strong>of</strong> oxidation <strong>of</strong> citrate but only a weak inhibitor <strong>of</strong> oxidation <strong>of</strong> cis-aconitate: 6-7 uM-fluorocitrate<br />

(conatinign 4% <strong>of</strong> the inhibitory isomer) caused 94% inhibition <strong>of</strong> the oxidation <strong>of</strong> citrate (2mM) whereas<br />

1mM-fluorocitrate was necessary to provoke the same inhibition when cis-aconitate (2mM) was the<br />

substrate. The degree <strong>of</strong> inhibition varied in relation to the respiratory state <strong>of</strong> mitochondria when<br />

fluorocitrate was added. The inhibition could be partially reversed by cis-aconitate. The aconitate hydratase<br />

extracted from the mitochondria was much less inhibited by fluorocitrate than was the mitochondria-bound<br />

enzyme, and the aconitate hydratase found in the cell sap was even less sensitive. 0.3 mM fluorocitrate was<br />

required to cause 50% inhibition <strong>of</strong> the reaction citrate > cis-aconitate, catalysed by the aconitate hydratase<br />

extracted from the mitochondria, and 1.2 M-fluorocitrate for the extramitochondrial enzyme. For both<br />

enzymes the reaction citrate > cis-aconitate was 2-3 times more sensitive to fluorocitrate than was the<br />

reaction isocitrate > cis-aconitate. The inhibition was <strong>of</strong> the competitive type for both reactions.<br />

Gulati, P., Singh, V., Gupta, M. K., Vaidya, V., Dass, S., and Prakash, S. (1993). Studies on the leaching <strong>of</strong><br />

fluoride in tea infusions. The Science <strong>of</strong> the Total Environment 138 , 213-222.<br />

Keywords: fluoride/persistence in plants<br />

Abstract: In order to assess the levels <strong>of</strong> fluoride ingestion through intake <strong>of</strong> tea, studies were conducted<br />

with four different brands <strong>of</strong> tea leaves commonly available in the Indian market. Four most prevalent<br />

methods for the preparation <strong>of</strong> tea with various contact times (2,4,6,8 and 10 min) <strong>of</strong> tea leaves with water<br />

show that: (a) leaching <strong>of</strong> fluoride is least in case <strong>of</strong> leaf tea as compared to powdered tea (F levels<br />

increasing with decreasing grain size); (b) leaching <strong>of</strong> fluoride reached a maximum after a contact <strong>of</strong> about<br />

6 min; (c) there is no difference between levels <strong>of</strong> fluoride with or without addition <strong>of</strong> milk in the English<br />

style where tea leaves are not boiled, while for the Indian style, addition <strong>of</strong> milk and subsequent boiling<br />

resulted in reduction <strong>of</strong> fluoride levels and (d) ingestion <strong>of</strong> fluoride per cup <strong>of</strong> tea ranged from 1.55 mg/l to<br />

3.21 mg/l amounting to an intake per day per person <strong>of</strong> fluoride between 0.3 to 1.9 mg.<br />

Gwag, B. J., Kemmerer, K., Robin, V., Lehmann, J., Sessler, F. M., and Springer, J. E. (1993).<br />

Fluorocitrate, a metabolic inhibitor <strong>of</strong> glial function, induces NGF and BDNF mRNA in the rat<br />

hippocampal formation. Society for Neuroscience Abstracts 19, 257.<br />

Keywords: fluorocitrate/metabolism/inhibition/brain<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Several studies have supported the involvement <strong>of</strong> glutamatergic-mediated neuronal events in<br />

regulating neurotrophin mRNA expression in the central nervous system. The effects <strong>of</strong> glutamate are<br />

mediated through ionotrophic or metabotrophic glutamate receptors. Glutamate levels at the synaptic cleft<br />

are regulated by an equilibrium between calcium-dependent glutamate release into the synaptic cleft and<br />

glutamate uptake primarily into glial cells. In the present study, we used in vivo microdialysis and in situ<br />

hybridization to investigate whether blockade <strong>of</strong> glial cell metabolism will influence glutamate levels in the<br />

extracellular space and mRNA levels <strong>of</strong> two neurotrophins, nerve growth factor (NGF) and brain-derived<br />

neurotrophic factor (BDNF) in the hippocampal formation. Female Long Evans rats were anesthetized<br />

with pentobarbital and placed into a stereotaxic apparatus. A total <strong>of</strong> 1-2nmoles <strong>of</strong> fluorocitrate, an<br />

inhibitor <strong>of</strong> glial cell metabolism, was injected into the hippocampal formation. Over a 4 hour time period,<br />

fluorocitrate treatment resulted in a significant increase (3-5 fold) in glutamate levels over time, while<br />

glutamine levels significantly decreased. These data support the decreased metabolic activity <strong>of</strong> glial cells<br />

as assessed by the selective effect <strong>of</strong> fluorocitrate on glutamate and glutamine levels. In situ hybridization<br />

histochemistry revealed that fluorocitrate injections into the hippocampal formation increases the<br />

expression <strong>of</strong> NGF and BDNF mRNA in dentate granule cells. The fluorocitrate-induced increase in NGF<br />

and BDNF mRNA was blocked by pretreatment with the N-methyl-D-aspartate (NMDA) receptor<br />

antagonist, AP5. The present results provide evidence that mRNA expression <strong>of</strong> neurotrophins in the<br />

hippocampal formation can be modified by glial activity, as well as neuronal activity regulating levels <strong>of</strong><br />

synaptically-released glutamate through NMDA receptors.<br />

Hagan, E. C., Ramsey, L. L., and Woodard, G. (1950). Absorption, distribution, and excretion <strong>of</strong> sodium<br />

fluoroacetate (1080) in rats. Journal <strong>of</strong> pharmacology and experimental therapeutics 99, 432-434.<br />

Keywords: metabolism/persistence in animals/1080/excretion/rodents/analysis<br />

Abstract: Data are presented which indicate that the rat possesses the capacity for metabolizing sodium<br />

mon<strong>of</strong>luoroacetate (1080). Distribution <strong>of</strong> the 1080 is rather uniform throughout the animal with the<br />

exception <strong>of</strong> a lower liver content usually found.<br />

Hagan, E. C., Ramsey, L. L., and Angel, R. (1950). unknown. Journal <strong>of</strong> pharmacology and experimental<br />

therapeutics 98, 234.<br />

Keywords: liver/fluoroacetate/citrate<br />

Hall, R. J. and Cain, R. B. (1972). Organic fluorine in tropical soils. New Phytologist 71, 839-853.<br />

Keywords: fluorine/soil/occurrence in nature/persistence in soil/fluoroacetate<br />

Abstract: A number <strong>of</strong> tropical soils growing toxic plant species which contain organically combined<br />

fluorine have been studied with a view to establishing the relationship between plant and soil in terms <strong>of</strong><br />

fluorine. The analyses <strong>of</strong> the soils for total fluorine and water-soluble fluoride showed that there was no<br />

correlation with the levels <strong>of</strong> total and organically-combined fluorine in the leaves <strong>of</strong> the plant species.<br />

Some <strong>of</strong> the most toxic plants grew in soils having low levels <strong>of</strong> mineral fluorine. Examination by<br />

electrodialysis, gas-liquid chromatography and infa-red spectroscopy, supported by chemical analysis, has<br />

revealed the presence in significant amounts <strong>of</strong> what appears to be fluoroacetate in several <strong>of</strong> the soils<br />

supporting species known to contain toxic fluorinated fatty acids. The origin <strong>of</strong> the naturally-occurring<br />

fluoroacetate in these soils is discussed.<br />

Hall, R. J. (1972). The distribution <strong>of</strong> organic fluorine in some toxic tropical plants. New Phytologist 71,<br />

855-871.<br />

Keywords: fluorine/fluoroacetate/soil/occurrence in nature<br />

Abstract: 1. The tissues <strong>of</strong> a number <strong>of</strong> toxic plants, including Acacia georginae, from Africa, Australia and<br />

South America, were analysed for the presence <strong>of</strong> organic and inorganic F. The presence <strong>of</strong> organically<br />

combined F was established in most <strong>of</strong> the species but the concentration <strong>of</strong> such F was very variable. A<br />

waxy exudate on the surface <strong>of</strong> the toxic leaves <strong>of</strong> A. georginae contained significant quantities <strong>of</strong> F and is<br />

believed to be part <strong>of</strong> an excretory mechanism. Only a small proportion <strong>of</strong> the exudate was identified as<br />

fluoroacetate, and other fluorinated organic compounds appear to be present. 2. Tissues <strong>of</strong> 15 toxic species<br />

from Africa, Australia and South America were analysed for organic and inorganic F. Organicallycombined<br />

F was found in most <strong>of</strong> the species, but varied in concentration. In African Dichapetalaceae the F<br />

content was generally higher in stems and roots than in leaves; in Australian Gastrolobium and Oxylobium<br />

spp. and Brazilian Palicourea marcgravii the reverse situation was found. Large amounts <strong>of</strong> organic F were<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

found in most seeds but not in those <strong>of</strong> Acacia georginae. None <strong>of</strong> the toxic species examined grew in high-<br />

F soils, but some grew in soils with very low F content. A waxy exudate on the outside <strong>of</strong> the toxic leaves<br />

<strong>of</strong> A. georginae contained significant amounts <strong>of</strong> organic F and appeared to be part <strong>of</strong> an excretory<br />

mechanism. Only a small proportion <strong>of</strong> the exudate was fluoroacetate and other fluorinated organic<br />

compounds seemed to be present. Crystals which appeared to be a complex mixture containing calcium<br />

oxalate, chloride, F, Mn and Si were found on the outer surface <strong>of</strong> roots and stems <strong>of</strong> Dichapetalaceae, and<br />

were also thought to be associated with a detoxication process<br />

Hall, R. J. (1974). The metabolism <strong>of</strong> ammonium fluoride and sodium mon<strong>of</strong>luoroacetate by experimental<br />

Acacia georginae. Environ.Pollut. 6, 267-280.<br />

Keywords: metabolism/fluoride/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate<br />

Abstract: Plants <strong>of</strong> Acacia georginae (one <strong>of</strong> numerous toxic tropical species now known to contain<br />

mon<strong>of</strong>luoroacetate) were cultivated in nutrient-washed quartz, and in soil. Attempts were made to induce<br />

the formation <strong>of</strong> organic fluorine by treatment <strong>of</strong> the roots with a solution <strong>of</strong> ammonium fluoride. Only<br />

small amounts <strong>of</strong> carbon-fluorine material were measured in the leaves and roots, and examinations by<br />

physico-chemical methods failed to detect any evidence <strong>of</strong> the presence <strong>of</strong> mon<strong>of</strong>luoroacetate in any <strong>of</strong> the<br />

plants. Similar plants were treated with sodium mon<strong>of</strong>luoroacetate which underwent considerable<br />

degradation to an acid-labile form <strong>of</strong> fluorine (probably inorganic fluoride). The results <strong>of</strong> the analysis <strong>of</strong><br />

the roots and leaves for fluorine revealed that the difference between acid-labile (diffusible) fluoride and<br />

total fluorine cannot be taken as a measure <strong>of</strong> the organic fluorine.<br />

Hamilton, D. J. and Eason, C. T. (1994). Monitoring for 1080 residues in waterways after a rabbitpoisoning<br />

operation in Central Otago. New Zealand journal <strong>of</strong> agricultural research 37, 195-198.<br />

Keywords: persistence in water/1080/rabbits<br />

Hamilton, D. J., Murphy, C. D., Amin, M. R., O'Hagan, D., and Harper, D. B. (1998). Exploring the<br />

biosynthetic origin <strong>of</strong> fluoroacetate and 4-fluorothreonine in Streptomyces cattleya. Journal <strong>of</strong> the<br />

Chemical Society.Perkin Transaction 1, 759-767.<br />

Keywords: fluoroacetate/bacteria/biosynthesis/enzyme<br />

Abstract: The striking similarity between the labelling patterns within the two fluorometabolites recorded in<br />

every experiment demonstrates that there is a single fluorination enzyme in S. cattleya.<br />

Hamilton, J. T. G., Amin, M. R., Harper, D. B., and O'Hagan, D. (1997). Biosynthesis <strong>of</strong> fluoroacetate and<br />

4-fluorothreonine by Streptomyces cattleya. Glycine and pyruvate as precursors. Chemical<br />

Communications 797-798.<br />

Keywords: biosynthesis/fluoroacetate<br />

Abstract: Using 19 F NMR spectroscopy, 13 C-labelled glycines and pyruvates are shown to be incorporated<br />

at high levels into fluoroacetate and 4-fluorothreonine by resting cells <strong>of</strong> Streptomyces cattleya; the<br />

labelling patterns illustrate a coversion <strong>of</strong> glycine via serine to pyruvate, where the C-2 and C-3 carbon<br />

atoms <strong>of</strong> pyruvate contribute both carbon atoms <strong>of</strong> fluoroacetate and C-3 and C-4 <strong>of</strong> 4-fluorothreonine<br />

respectively.<br />

Hamilton, J. T. G. Biosynthesis <strong>of</strong> organ<strong>of</strong>luorine compounds in plants and bacteria. 1997. Queen's<br />

University <strong>of</strong> Belfast (Northern Ireland)Editor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: biosynthesis/bacteria/fluorine/fluoroacetate/NMR/metabolism/enzyme<br />

Abstract: Organ<strong>of</strong>luorine compounds are relatively rare in nature compared with other organohalogens.<br />

Notwithstanding the obvious biochemical interest and potential biotechnological significance, the<br />

mechanism by which fluorine is inserted into these compounds has yet to be elucidated. This investigation<br />

re-examined the organ<strong>of</strong>luorine compounds in the seeds <strong>of</strong> the West African plant Dichapetalum<br />

toxicarium and further probed the biochemical processes involved in fluoroacetate and 4-fluorothreonine<br />

formation in the actinomycete Streptomyces cattleya. An unidentified fluorinated natural product<br />

previously isolated from seed oils <strong>of</strong> D. toxicarium was identified as threo-18-fluoro-9,10-dihydroxystearic<br />

acid. Using GC/MS the presence <strong>of</strong> $omega$-fluoro-palmitoleic, -stearic, -linoleic, -arachidic and -<br />

eicosenoic acids was established from this source. To facilitate studies with S. cattleya GC/MS and HPLC<br />

procedures for the quantitative determination <strong>of</strong> fluoroacetate and 4-fluorothreonine in culture supernatant<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

were developed, and GC/MS and $sp{19}$F NMR methodologies established for the measurement <strong>of</strong><br />

stable isotope label in both fluorometabolites. Using these techniques glycine has been shown to be a<br />

highly effective precursor <strong>of</strong> both fluorometabolites. The $alpha$-carbon atom <strong>of</strong> glycine is incorporated<br />

efficiently into both C-1 and C-2 <strong>of</strong> fluoroacetate and also C-3 and C-4 <strong>of</strong> 4-fluorothreonine but the<br />

carboxyl carbon <strong>of</strong> the precursor is not retained in either metabolite. This pattern <strong>of</strong> labelling is consistent<br />

with the metabolism <strong>of</strong> glycine via serine to pyruvate and the utilisation <strong>of</strong> pyruvate or a closely related<br />

metabolite as the substrate for the fluorinating enzyme. Studies with $sp{13}$C-labelled pyruvates provide<br />

strong support <strong>of</strong> the postulated pathway. The extent to which labelling in C-1 and C-2 <strong>of</strong> fluoroacetate<br />

parallels that in C-3 and C-4 <strong>of</strong> 4-fluorothreonine in experiments using $sp{13}$C-labelled precursors<br />

suggests that both fluorometabolites arise from a common intermediate, a conclusion implying that a single<br />

fluorinating enzyme exists in S. cattleya. 4-Fluorothreonine biosynthesis does not appear to proceed via a<br />

direct condensation <strong>of</strong> glycine and fluoroacetaldehyde as originally postulated, but instead may involve<br />

fluoroacetaldehyde and 2-aminomalonate<br />

Hansford, D. 1080: The Facts. New Zealand Wilderness [September], 36-38. 2002.<br />

Ref Type: Magazine Article<br />

Keywords: 1080/persistence in animals<br />

Abstract: What is 1080?<br />

It's a tasteless, odourless white powder named sodium mon<strong>of</strong>luoracete, or C2H2FNaO. It's been used for<br />

possum and rabbit control in New Zealand since the 1950s.<br />

Fluoroacetate (the active ingredient <strong>of</strong> 1080) is a natural compound found in plants from South America,<br />

South Africa and Australia. The most toxic species is found in South Africa, which can carry 8mg/g <strong>of</strong><br />

fluoracetate in its seeds. You'll also find very low amounts <strong>of</strong> fluoroacetate in tea and in guar gum, a<br />

common ingredient in foodstuffs.<br />

The toxin prevents animals from browsing on the plant's leaves. Scientists can replicate this natural<br />

compound in the lab, and it's this that is used in 1080 baits.<br />

There is very little actual poison in a 1080 pellet. Only 0.15% <strong>of</strong> a bait, at most, is fluoroacetate. The rest<br />

is a matrix <strong>of</strong> cereal or carrot, which acts as a lure. Carrot baits are fiddly, expensive and degrade quickly<br />

in wet weather, and are used less nowadays, particularly in aerial drops.<br />

Harper, D. B., O'Hagan, D., and Murphy, C. D. (2003). Fluorinated natural products: Occurrence and<br />

biosynthesis. Natural Production <strong>of</strong> Organohalogen Compounds 3, 141-169.<br />

Keywords: occurrence in nature/biosynthesis<br />

Harris, R. J. and Rees, J. S. Aerial poisoning <strong>of</strong> wasps. 162, 1-50. 2000. Wellington, Department <strong>of</strong><br />

Conservation. Science for Conservation.<br />

Ref Type: Report<br />

Keywords: poisoning/wasps/baits/non-target species/1080/efficacy<br />

Abstract: The feasability <strong>of</strong> the aerial application <strong>of</strong> bait to kill wasps was investigated as a technique for<br />

large-scale poisoning <strong>of</strong> wasps in areas <strong>of</strong> 1000-5000 ha. Methods <strong>of</strong> bait dehydration and pelletisation<br />

into a form suitable for aerial delivery were tested. Bait attractiveness to wasps was determined and<br />

interest in baits by non-target species recorded. A simulated aerial application was used to test the efficacy<br />

<strong>of</strong> a toxic freeze-dried formulation for wasp control. Baits were produced that were sufficiently robust for<br />

aerial application, but processing reduced attractiveness to wasps. Aerial baiting <strong>of</strong> wasps is technically<br />

feasible, but reduced attractiveness <strong>of</strong> pelletised baits, non-target issues, and successes with current groundbased<br />

operations mean further improvements are needed before it would be worth adopting.<br />

Harris, W. (<strong>1964</strong>). Sodium fluoroacetate poisoning in dogs. Journal <strong>of</strong> the American Veterinary Medical<br />

Association 145, 1001.<br />

Keywords: sodium fluoroacetate/fluoroacetate/poisoning/dogs/convulsions/cats/cardiac/treatment<br />

Abstract: Clinical signs usually occur between 15 minutes and 2 hours after ingestion and may involve<br />

either the cardiovascular system or the nervous system or both. Dogs ordinarily have convulsions whereas<br />

in cats there may be a combination <strong>of</strong> convulsions and cardiac disorder.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Harris, W. F. (1975). Clinical toxicities <strong>of</strong> dogs. The Veterinary Clinics <strong>of</strong> North America 5, 605-622.<br />

Keywords: dogs/symptoms/poisoning<br />

Harrison, B. L., Bransford, A. V., and McNamara, B. P. (1951). Deterioration <strong>of</strong> sodium mon<strong>of</strong>luoroacetate<br />

in water and saline solutions. Federation proceedings 10, 306-307.<br />

Keywords: persistence in water/sodium mon<strong>of</strong>luoroacetate<br />

Harrison, H. C. and Harrison, H. E. (1959). Cortisol and citrate metabolism. American journal <strong>of</strong><br />

physiology 196, 943-945.<br />

Keywords: citrate/metabolism/serum/rodents/gut/kidney/blood<br />

Abstract: Determinations <strong>of</strong> citrate concentrations in serum and tissues were made in fluoroacetate-injected<br />

rats given cortisol. The increment <strong>of</strong> serum citrate is less in the cortiosl treated rats than in the controls<br />

injected with fluoroacetate, but the accumulation <strong>of</strong> citrate in the heart and small intestine following<br />

fluoroacetate is equally great in both groups. Lower concentrations <strong>of</strong> citrate in the kidneys <strong>of</strong> cortisoltreated<br />

rats are probably due to difference in citrate <strong>of</strong> tubular urine. In the adrenalectomized rat<br />

fluoroacetate causes a greater rise <strong>of</strong> serum citrate than in the intact rat but there is no greater increase <strong>of</strong><br />

tissue citrate. Calculation <strong>of</strong> citrate distribution ratios i.e. the ration <strong>of</strong> the concentration <strong>of</strong> citrate in<br />

intracellular water to that <strong>of</strong> extracellular fluid, indicates that the distribution ratio following fluoroacetate<br />

is increased by cortisol and decreased by adrenalectomy. Cortisol does not apparently influence the<br />

intracellular accumulation <strong>of</strong> citrate but alters the distribution <strong>of</strong> citrate between cells and extracellular<br />

fluid, possibly due to an effect upon the efflux <strong>of</strong> citrate from cells.<br />

Harrison, J. W. E., Ambrus, J. L., Ambrus, C. M., Rees, E. W., Peters, R. H., and Reese, L. C. (1952).<br />

Acute poisoning with sodium fluoroacetate (compound 1080). Journal <strong>of</strong> the American Medical<br />

Association Aug 23, 1520-1522.<br />

Keywords: acute toxicity/sodium fluoroacetate/1080/humans<br />

Abstract: 1. A case history <strong>of</strong> fluoroacetate poisoning has been described together with postmortem<br />

examination and chemical analysis <strong>of</strong> the fluoroacetate content <strong>of</strong> organs and body fluids.<br />

2. It appears that there is no important difference between postmortem findings <strong>of</strong> sodium fluoroacetate and<br />

sodium fluoride poisoning. The additional biochemical effects <strong>of</strong> sodium fluoroacetate thus seem to have<br />

no pathological manifestation <strong>of</strong> diagnostic significance.<br />

3. Because <strong>of</strong> indications <strong>of</strong> gastrointestinal excretion and reabsorption <strong>of</strong> fluoride compounds, repeated<br />

gastric lavages seem to be advisable<br />

4. Other therapeutic aspects are briefly discussed.<br />

Harrison, M. (1978). 1080. Wildlife : a review 9, 48-53.<br />

Keywords: non-target species/birds/1080<br />

Abstract: Application <strong>of</strong> principles involving bait size and type should much reduce the incidence <strong>of</strong> bird<br />

poisoning in the course <strong>of</strong> 1080 campaigns against forest and pasture pests.<br />

Harrisson, J. W. E., Ambrus, J. L., and Ambrus, C. M. (1952). Fluoroacetate (1080) poisoning. Industrial<br />

medicine and surgery 21, 440-442.<br />

Keywords: acute toxicity/fluoroacetate/1080/poisoning<br />

Hashimoto, Y., Makita, T., Miyata, H., Noguchi, T., and Ohta, G. (1968). Acute and subchronic toxicity <strong>of</strong><br />

a new fluorine pesticide, N-Methyl-N-(I-Naphthyl) Fluoroacetamide. Toxicology and Applied<br />

Pharmacology 12, 536-547.<br />

Keywords: acute toxicity/fluoroacetamide/1081/fluorine<br />

Hashimoto, Y., Makita, T., Mori, T, Nishibe, T., and Noguchi, T (1970). Toxicologic and pharmacologic<br />

studies on acetamide, as an antidote against mon<strong>of</strong>luoroacetamide poisoning; Studies on the selective<br />

toxicity. XVII. Pharmacometrics 4, 451-462.<br />

Keywords: poisoning/antidote/treatment/rabbits/acute toxicity<br />

Abstract: Acetimide, an antidote to mon<strong>of</strong>luoroacetamide derivatives, has received toxicologic and<br />

pharmacologic investigations. The acute toxicity <strong>of</strong> acetamide for several species by different routes <strong>of</strong><br />

administration was very slight, there being an about 10g/kg in mice or rats by the intravenous injection <strong>of</strong><br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

acetamide. By subacute toxicity studies in rats and rabbits, there was neither marked effect on body weight<br />

gain, nor any gross signs <strong>of</strong> toxicity. During the studies <strong>of</strong> repeated application in rats and rabbits, clinical<br />

observations, hematologic data, organ function values, urinalysis, and terminal gross and microscopic<br />

examinations <strong>of</strong> tissues were obtained. No evidence <strong>of</strong> drug effect was observed in rats or rabbits that<br />

received daily injection <strong>of</strong> 1,000 mg/kg or less for 90 consecutive days.<br />

Acetamide did not exhibit significant activity in any <strong>of</strong> the pharmacologic tests such as its actions on the<br />

central nervous system, cardiovascular and respiratory systems, peripheral systems, and blood.<br />

Hassan, S. S., Amer, M. M., Abdelfatah, S. A., and Elkosasy, A. M. (1998). Membrane sensors for the<br />

selective determination <strong>of</strong> fluorouracil. Analytica chimica acta 363, 81-87.<br />

Keywords: mode <strong>of</strong> action<br />

Hassel, B., Paulsen, R. E., Johnsen, A., and Fonnum, F. (1992). Selective inhibition <strong>of</strong> glial cell metabolism<br />

in vivo by fluorocitrate. Brain research 576, 120-124.<br />

Keywords: inhibition/metabolism/fluorocitrate<br />

Abstract: The effect <strong>of</strong> fluorocitrate on glial and neuronal amino acid metabolism was studied. One nmol<br />

<strong>of</strong> fluorocitrate administered intrastriatally in the rat caused a 95% reduction in glutamine formation from<br />

[ 14 C]acetate, a substrate which enters the glial cells selectively. The metabolism <strong>of</strong> [ 14 C]glucose which<br />

enters neurons, was unaffected by fluorocitrate treatment except for the glutamine formation. This is<br />

evidence that fluorocitrate is a selective inhibitor <strong>of</strong> the glial Krebs' cycle. [ 14 C]Citrate and 2-oxoglutarate<br />

labelled amino acids in a manner similar to [ 14 C]acetate, which shows that these substrates are taken up and<br />

metabolized by glial cells. Differences in the labelling <strong>of</strong> y-aminobutyric acid (GABA) from [ 14 C]acetate<br />

and citrate suggest that astrocytes associated with GABAergic and glutamatergic nerve terminals may<br />

differ in their preference for amino acid precursors.<br />

Hassel, B., Sonnewald, U., Unsgard, G., and Fonnum, F. (1994). NMR spectroscopy <strong>of</strong> cultured astrocytes<br />

- effects <strong>of</strong> glutamine and the gliotoxin fluorocitrate. Journal <strong>of</strong> neurochemistry 62, 2187-2194.<br />

Keywords: mode <strong>of</strong> action/NMR<br />

Hassel, B., Westergaard, N., Schousboe, A., and Fonnum, F. (1995). Metabolic differences between<br />

primary cultures <strong>of</strong> astrocytes and neurons from cerebellum and cerebral cortex. Effects <strong>of</strong> fluorocitrate.<br />

Neuroscience research 20, 413-420.<br />

Keywords: mode <strong>of</strong> action<br />

Hassel, B., Bachelard, H., Jones, P., Fonnum, F., and Sonnewald, U. (1997). Trafficking <strong>of</strong> amino acids<br />

between neurons and glia in vivo : effects <strong>of</strong> inhibition <strong>of</strong> glial metabolism by fluoroacetate. Journal <strong>of</strong><br />

cerebral blood flow and metabolism 17, 1230-1238.<br />

Keywords: mode <strong>of</strong> action/metabolism/brain/fluoroacetate/citrate<br />

Abstract: Glial-neuronal interchange <strong>of</strong> amino acids was studied by C-13 nuclear magnetic resonance<br />

spectroscopy <strong>of</strong> brain extracts from fluoroacetate-treated mice that received [1,2-C-13]acetate and [1-C-<br />

13]glucose simultaneously. [C-13]Acetate was found to be a specific marker for glial metabolism even with<br />

the large doses necessary for nuclear magnetic resonance spectroscopy. Fluoroacetate, 100 mg/kg, blocked<br />

the glial, but not the neuronal tricarboxylic acid cycles as seen from the C-13 labeling <strong>of</strong> glutamine,<br />

glutamate, and gamma-aminobutyric acid. Glutamine, but not citrate, was the only glial metabolite that<br />

could account for the transfer <strong>of</strong> C-13 from glia to neurons. Massive glial uptake <strong>of</strong> transmitter glutamate<br />

was indicated by the labeling <strong>of</strong> glutamine from [1-C-13]glucose in fluoroacetate-treated mice. The C-3/C-<br />

4 enrichment ratio, which indicates the degree <strong>of</strong> cycling <strong>of</strong> label, was higher in glutamine than in<br />

glutamate in the presence <strong>of</strong> fluoroacetate, suggesting that transmitter glutamate (which was converted to<br />

glutamine after release) is associated with a tricarboxylic acid cycle that turns more rapidly than the overall<br />

cerebral tricarboxylic acid cycle. [References: 47]<br />

Hattori, Y. and Hino, S. (1981). Inactivation by oxygen and stabilization by fluorocitrate <strong>of</strong> aconitase from<br />

Escherichia coli. J.Gen.Appl.Microbiol. 27, 33-41.<br />

Keywords: fluorocitrate/aconitase/treatment/enzyme<br />

Abstract: More than 50% <strong>of</strong> the total aconitase activity in Escherichia coli was lost when cell-free extracts<br />

were prepared under air by a French press, by osmotic rupture <strong>of</strong> spheroplasts or by sonic treatment, as<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

shown by the fact that the enzyme activity <strong>of</strong> the extracts prepared by sonic treatment under N2 was more<br />

than twice that <strong>of</strong> the extracts prepared by the other methods. When the extracts prepared by sonic<br />

treatment under N2 were gently shaken under air at 25º, about 70 to 80% <strong>of</strong> the original activity was lost<br />

over 30 min, but a constant level <strong>of</strong> the enzyme activity remained even after prolonged incubation. The<br />

remaining aconitase activity after a long aerobic incubation was the same whether the extracts were<br />

prepared by sonic treatment under air or N2. Aconitase was stable when cell-free extracts were incubated<br />

under anaerobic conditions or when fluorocitrate, in concentration less than 1µM, was added during aerobic<br />

incubation. Citrate was less effective than fluorocitrate in preventing enzyme inactivation. Aconitase in<br />

the extracts, which had been incubated under air with fluorocitrate, was stable against oxygen inactivation<br />

and showed different Vmax and Km values from those <strong>of</strong> the aconitase in the extracts that had been<br />

incubated under air without the addition <strong>of</strong> fluorocitrate.<br />

Hayes, F. D., Short, R. D., and Gibson, J. E. (1973). Differential toxicity <strong>of</strong> monochloroacetate,<br />

mon<strong>of</strong>luoroacetate and monoiodoacetate in rats. Toxicology and Applied Pharmacology 26, 93-102.<br />

Keywords: acute toxicity/mammals/mode <strong>of</strong> action/rats<br />

Hegdal, P. L., Gatz, T. A., and Fite, E. C. (1981). Secondary effects <strong>of</strong> rodenticides on mammalian<br />

predators. In 'Worldwide Furbearer Conference proceedings, August 3-11, 1980, Frostburg, Maryland<br />

USA'. (J. A. Chapman and D. PursleyEds. ) pp. 1781-1793. ([The Conference]: [Frostburg].)<br />

Keywords: secondary poisoning/mammals/non-target species/predators/USA<br />

Hegdal, P. L., Fagerstone, K. A., Gatz, T. A., Glahn, J. F., and Matschke, G. H. (1986). Hazards to wildlife<br />

associated with 1080 baiting for California ground squirrels. Wildlife Society bulletin 14, 11-21.<br />

Keywords: mammals/birds/non-target species/secondary poisoning/1080/strychnine/rabbits<br />

Abstract: Mon<strong>of</strong>luoroacetic acid was first prepared in Belgium in 1896 (Atzert 1971), but was not seriously<br />

investigated as a pesticide in the United States until World War II eliminated major sources <strong>of</strong> raw<br />

materials for red squill, thallium, and strychnine. Studies by the U.S. Fish and Wildlife Service showed<br />

that sodium mon<strong>of</strong>luoroacetate (1080) was an effective rodenticide, predacide, and insecticide, and resulted<br />

in it widespread use from the late 1940s through the 1960s.<br />

Although laboratory studies have repeatedly shown that 1080 theoretically poses hazards to nontarget<br />

wildlife through both primary poisoning (the toxic bait is ingested directly) and secondary poisoning (the<br />

result <strong>of</strong> consuming and animal killed by primary poisoning), few field data are available to assess the<br />

effect <strong>of</strong> 1080 on nontarget populations. The objective <strong>of</strong> this study was to evaluate the primary and<br />

secondary effects on nontarget wildlife <strong>of</strong> an operational program using 1080 treated gain bait to control<br />

ground squirrels. Specific objectives were to determine efficacy <strong>of</strong> 1080 for control <strong>of</strong> California ground<br />

squirrels (Spermophilus beecheyi); primary hazards to other rodents, rabbits, and seed eating birds; and<br />

secondary hazards to raptors and mammalian predators.<br />

Henderson, R. J., Frampton, C. M., Morgan, D. R., and Hickling, G. J. (1999). The efficacy <strong>of</strong> baits<br />

containing 1080 for control <strong>of</strong> brushtail possums. Journal <strong>of</strong> wildlife management 63, 1138-1151.<br />

Keywords: field efficacy/possums/1080/acute toxicity<br />

Abstract: A significant proportion <strong>of</strong> brushtail possums (Trichosurus vulpecula) in New Zealand survive<br />

pest control operations using sodium mon<strong>of</strong>luoroacetate (1080) baits. To be effective, bait needs to contain<br />

an appropriate concentration <strong>of</strong> 1080 and be eaten in amounts lethal to all possums, In our trials, the acute<br />

toxicity <strong>of</strong> 1080 to captive possums was estimated when the toxicant was included in different bait types,<br />

and results compared with published data for 1080 administered in aqueous solutions by oral gavage, The<br />

effectiveness <strong>of</strong> baits containing different 1080 concentrations, and <strong>of</strong> different palatabilities, was also<br />

assessed. Captive possums that fed on baits in this trial were less susceptible to 1080 (LD50 = 1.5 mg/kg)<br />

than in previously reported trials where the toxicant was administered to caged possums by oral gavage<br />

(LD50 = 0.8 mg/kg; P < 0.001). The differences in the acute toxicity <strong>of</strong> 1080 in water and in baits are<br />

attributed mainly to the reduced bioavailability <strong>of</strong> 1080 in baits. Also in our trial, captive animals feeding<br />

voluntarily on baits more closely approximated the status <strong>of</strong> animals in the wild than when acute toxicity<br />

was estimated by anaesthetizing possums and intubating solutions by oral gavage. Genetic polymorphisms<br />

caused some animals to be much more susceptible to 1080 toxicosis than others. Body mass differences<br />

cause females and young possums to ingest a higher toxic dose (mg/kg) than adult males, and the<br />

concentrations <strong>of</strong> toxicant affected the amounts <strong>of</strong> bait eaten and the resultant mortality. For the range <strong>of</strong><br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

baits tested, the palatability <strong>of</strong> bait was a more important determinant <strong>of</strong> amounts eaten, and the percentage<br />

<strong>of</strong> possums sublethally poisoned, than was toxicant concentration. Possums that ate baits <strong>of</strong> low palatability<br />

and inappropriate 1080 concentration ingested small doses <strong>of</strong> 1080 and either endured a protracted time to<br />

death or survived. The size and quality <strong>of</strong> bait have implications for the management <strong>of</strong> wild populations <strong>of</strong><br />

possums in different climatic areas where aerial and land-based methods <strong>of</strong> control are used.<br />

Henry, S. J. Biodegradation <strong>of</strong> sodium mon<strong>of</strong>luoroacetate ("Compound 1080"). -45. 1984. Botany Dept,<br />

University <strong>of</strong> Canterbury, New Zealand.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/sodium<br />

fluoroacetate/fluoroacetate/soil/degradation/enzyme/analysis/bacteria<br />

Abstract: A species <strong>of</strong> Penicillium capable <strong>of</strong> degrading "Compound 1080" (sodium fluoroacetate, SFA)<br />

was isolated from leaves <strong>of</strong> Griselinia littoralis. The growth <strong>of</strong> Penicillium sp on a "1080" gel infers that<br />

the SFA component <strong>of</strong> this gel, when applied to leaves, may be degraded before being leached into the soil.<br />

The optimal conditions for growth and SFA degradation by this Penicillium sp were investigated, and<br />

subsequent attempts were made to induce vigorous SFA degrading ability for a crude enzyme extract. This<br />

enzyme was studies for qualitative analysis <strong>of</strong> SFA residues by enzymic assay. The constitutive nature <strong>of</strong><br />

this enzyme was observed as SFA could be broken down by enzyme extracts not previously adapted to<br />

SFA.<br />

Herrmann, D. B. J., Herz, R., and Fröhlich, J. (1985). Role <strong>of</strong> gastrointestinal tract and liver in acetate<br />

metabolism in rat and man. European Journal <strong>of</strong> Clinical Investigation 15, 221-226.<br />

Keywords: liver/metabolism/acetate<br />

Abstract: Nte acetate uptake/release by various tissues was studied in vivo in fed, starved and<br />

Paromomycin-treated rats and in patients with cirrhosis <strong>of</strong> the liver. In humans the portal vein, hepatic vein<br />

and hepatic arterial blood flow rates were determined simultaneously. In rats acetate is only intestinally<br />

produced and released into the portal vein. Intestinal production is decreased by 33% in starved and<br />

Paromomycin-treated rats compared to fed animals. Portal vein-hepatic vein acetate differences are<br />

linearly related to the portal vein acetate concentration (r = 0.92). Acetate uptake from the portal vein by<br />

the liver was found when the portal venous concentration exceeded 180 µmol 1 -1 . In humans the hepatic<br />

net acetate uptake from the portal vein/net acetate release into the hepatic vein, measured as µmol min -1 , is<br />

linearly related to the portal vein acetate concentration (r = 0.97). Furthermore, portal vein-hepatic vein<br />

differences are correlated to the arterial concentration (r = 0.96). The data indicate that the liver may<br />

homeostatically regulate the systemic acetate concentration in rat and man.<br />

Heyward, R. P. and Norbury, G. L. (1999). Secondary poisoning <strong>of</strong> ferrets and cats after 1080 rabbit<br />

poisoning. Wildlife research 26, 75-80.<br />

Keywords: secondary poisoning/non-target species/mammals/cats/1080/treatment/rabbits/persistence in<br />

animals<br />

Abstract: The incidence <strong>of</strong> secondary poisoning was determined by using radio-telemetry to assess the<br />

survival <strong>of</strong> 68 ferrets and 21 cats on two treatment sites and one control site in the dry tussock grasslands <strong>of</strong><br />

New Zealand. The treatment sites were aerially poisoned with 1080-coated carrot baits (0.02% wt/wt) to<br />

control rabbits. The control site was not poisoned. Ferrets and cats were monitored at two-weekly intervals<br />

for at least 1 month before, and 2 months after the poison operations. Muscle samples from ferrets and cats<br />

that died within 50 days <strong>of</strong> poisoning on the treatment sites were assayed for 1080. In all, 7-11% (n = 28) <strong>of</strong><br />

ferrets on one site and 8-15% (n = 26) <strong>of</strong> ferrets at the other site apparently died <strong>of</strong> secondary 1080<br />

poisoning. Natural mortality rates <strong>of</strong> ferrets were 46-81% per annum. While we have evidence that<br />

secondary poisoning <strong>of</strong> cats does occur, we monitored insufficient numbers <strong>of</strong> cats to reliably estimate<br />

mortality rates. Declines in predator numbers are commonly observed after rabbit poisoning. This study<br />

indicates that secondary poisoning contributes to these declines.<br />

Hickling, G. J. (1994). Behavioural resistance by vertebrate pests to 1080 toxin: implications for<br />

sustainable pest management in New Zealand. In 'Proceedings <strong>of</strong> the science workshop on 1080.'. (A. A.<br />

Seawright and C. EasonEds. ) pp. 151-158. (The <strong>Royal</strong> Society <strong>of</strong> New Zealand:<br />

Keywords: resistance/1080/bait shyness/possums<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Hickling, G. J., Henderson, R. J., and Thomas, M. C. C. (1999). Poisoning mammalian pests can have<br />

unintended consequences for future control: Two case studies. New Zealand journal <strong>of</strong> ecology 23, 267-<br />

273.<br />

Keywords: poisoning/baits/non-target<br />

species/behaviour/aversion/possums/rabbits/cyanide/efficacy/1080/cholecalciferol<br />

Abstract: Vertebrate pest control operations using toxic baits can have unintended consequences for nontarget<br />

species, some <strong>of</strong> which may themselves be pests. Learned avoidance behaviour (termed 'aversion')<br />

can be induced by sublethal dosing, which can arise when species with high and low susceptibilities to a<br />

toxin co-exist in the same area. In such cases the less-susceptible species (e.g., possums Trichosurus<br />

vulpecula) may be sublethally poisoned by control work targeting the more-susceptible species (e.g.,<br />

rabbits Oryctolagus cuniculus). A case study <strong>of</strong> rabbit control on North Canterbury farmland is presented to<br />

demonstrate this effect. When control is being repeated at frequent intervals, it is prudent to vary the<br />

control methods used. Nevertheless, aversion induced by the use <strong>of</strong> one toxic bait (e.g., cyanide paste) can<br />

in some situations 'generalise' so that the efficacy <strong>of</strong> control using other toxins (e.g., 1080 and<br />

cholecalciferol in cereal baits) is also compromised. A case study <strong>of</strong> initial and follow-up possum control in<br />

four discrete areas <strong>of</strong> Canterbury forest provides an example <strong>of</strong> this problem. The implications <strong>of</strong> these<br />

findings for future pest management in New Zealand are discussed<br />

Hicks, S. P. (1952). Some effects <strong>of</strong> ionizing radiation and metabolic inhibition on the developing<br />

mammalian nervous system. Journal <strong>of</strong> Pediatrics 40, 489-513.<br />

Keywords: fluoroacetate/developmental toxicity/regulatory toxicology/brain/inhibition/heart/reproductive<br />

effects/metabolism/rats/teratogenicity<br />

Abstract: The developing nervous system in vivo, specifically its neuroblasts, has been found to be<br />

unusually susceptible to acute metabolic injury by ionising radiation, certain sulfhydryl reagents, other<br />

inhibitors and antimetabolites. It has been foudn to be relatively insensitive to acute interference with<br />

glucose and oxygen metabolism except late in development. In the first third <strong>of</strong> gestation the neural tube is<br />

resistant to radiation and possibly other agents but this period is in need <strong>of</strong> more investigation. Injuries in<br />

the latter two thirds <strong>of</strong> gestation cause the development <strong>of</strong> progressive malformations <strong>of</strong> the nervious<br />

system during growth that carry over into adult life. The most important mechanisms that determine the<br />

form <strong>of</strong> the malformation are the actula destruction <strong>of</strong> building blocks (neurobalsts) and the time during<br />

gestation (critical period) at which the injury occurs. These experiments carried out on experimental<br />

animals, chiefly rats and mice invite attention to the possibility that a variety <strong>of</strong> agents mat act during<br />

nervous system development to produce malformations.<br />

Hill, E. F., Heath, R. G., Spann, J. W., and Williams, J. D. Lethal dietary toxicities <strong>of</strong> environmental<br />

pollutants to birds. 191, 1-8. 1975. Washington, D.C., U.S. Fish and Wildlife Service. Special Scientific<br />

Report - Wildlife No. 191.<br />

Ref Type: Report<br />

Keywords: lethal dose/acute toxicity/birds<br />

Abstract: This report is a compilation and analysis <strong>of</strong> the results <strong>of</strong> nearly 10 years <strong>of</strong> testing the lethal<br />

dietary toxicities <strong>of</strong> pesticidal and industrial chemicals to young bobwhites (Colinus virginianus), Japanese<br />

quail (Coturnix c. japonica), ring-necked pheasants (Phasianus colchicus), and mallards (Anas<br />

platyrhynchos).<br />

A total <strong>of</strong> 131 compounds were tested. Toxicities are expressed as median lethal dietary concentrations<br />

(LC50) and are based on 5 days <strong>of</strong> dietary exposure to the test compound followed by 3 days <strong>of</strong> untreated<br />

feed. From these data statistical comparisons between toxicities are possible for a given species.<br />

Certain classes <strong>of</strong> pesticides - organochlorine compounds, organophosphates and organometallic<br />

compounds - contained most <strong>of</strong> the compounds judged "highly toxic". The most frequent order <strong>of</strong> species<br />

response was bobwhite > Japanese quail > ring-necked pheasant > mallard. This order correlates with their<br />

body sizes at the ages tested.<br />

Hilton, H. W., Yuen, Q. H., and Nomura, N. S. (1969). Absorption <strong>of</strong> mon<strong>of</strong>luoroacetate-2- 14 C ion and its<br />

translocation in sugarcane. Journal <strong>of</strong> agricultural and food chemistry 17, 131-134.<br />

Keywords: persistence in plants/cellulose<br />

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Appendix C<br />

Hone, J. and Mulligan, H. (1982). Vertebrate pesticides. (Department <strong>of</strong> Agriculture, New South Wales:<br />

Sydney.)<br />

Keywords: acute toxicity/mode <strong>of</strong> action/lethal dose<br />

Abstract: The literature is reviewed on 38 pesticides used against vertebrate pests. Each pesticide is dealt<br />

with separately and information given on physical and chemical properties, mode <strong>of</strong> action, known<br />

antidote, current usage and legal status. Chronic and acute toxicity information is listed according to<br />

species, sex, lethal dose and mode <strong>of</strong> administration. A glossary <strong>of</strong> relevant terms and abbreviations and an<br />

index <strong>of</strong> common, alternative and trade names is also included.<br />

Hone, J. and Kleba, R. (1984). The toxicity and acceptability <strong>of</strong> warfarin and 1080 poison to penned feral<br />

pigs. Australian wildlife research 11, 103-111.<br />

Keywords: 1080/pigs/acute toxicity/efficacy<br />

Abstract: Experiments were conducted which examined the toxicity and acceptability <strong>of</strong> warfarin and 1080<br />

poison to penned feral pigs. Warfarin was very toxic and highly acceptable. Maximum mortality was 11 <strong>of</strong><br />

12 at 0.08% concentration for 2 or 3 days, or 0.1% concentration for 2 days. 1080 toxicity was 2 <strong>of</strong> 19 at<br />

0.05% for 1 day. Bait intake declined significantly when bait was poisoned with 1080.<br />

Hoogenboom, J. J. L. (1987). Determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound 1080) in tissues and<br />

baits as its benzyl ester by reaction-capillary gas chromatography. Journal <strong>of</strong> Analytical Toxicology 11,<br />

140-143.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/1080/baits/mon<strong>of</strong>luoroacetate/analysis<br />

Abstract: A reaction-capillary gas chromatographic procedure using photo-ionization (PID) or flameionization<br />

(FID) detcetion was developed for the determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound<br />

1080), a pesticide, in tissues and baits. Fluoroacetic acid from tissue (1 g) and bait (10 g) extracts was first<br />

partitioned into ethyl acetate and then into 0.5 M benzyldimethylphenylammonium hydroxide. Benzylation<br />

was acheived by pyrolysis <strong>of</strong> the quaternary ammonium salt in the injection port. Chloroacetic acid was<br />

used as the internal standard. A linear relationship (r= 0.999) was observed between the peak area ratio <strong>of</strong><br />

the substrate/internal standard and the fluoroacetic acid concentration. The detection limit for compound<br />

1080 using the described analytical procedure was 15 µg/kg with PID and 100 µg/kg with FID.<br />

Hopper, S. Poison peas: Deadly protectors. Landscope Winter 1991, 45-50. 1991.<br />

Ref Type: Magazine Article<br />

Keywords: poison<br />

Abstract: Poison plants were a major deterrent to ealy settlers in parts <strong>of</strong> Western Aust.- and thereby helped<br />

to preserve some areas <strong>of</strong> high conservation value. Now, ironically, plants that were for more than a<br />

century thought <strong>of</strong> as pests are endangered. In this companion piece to King and Kinnear's '1080: The<br />

Toxic Paradox' in the present issue <strong>of</strong> Landscope, CALM research scientist Steve Hopper tells the story <strong>of</strong><br />

some <strong>of</strong> Western Australia's killer fauna.<br />

Horiuchi, N. (1961). The C-F bond rupture <strong>of</strong> mon<strong>of</strong>luoroacetate by soil microbes I. Isolation <strong>of</strong> bacteria<br />

and ability <strong>of</strong> their rupture. Nippon Nogeikagaka Kaishi 35, 870-873.<br />

Keywords: mon<strong>of</strong>luoroacetate/soil/bacteria/metabolism<br />

Abstract: Chem Abstr 60: 9630d <strong>1964</strong><br />

Horiuchi, N. (1962). Breakage <strong>of</strong> the C-F bond in mon<strong>of</strong>luoroacetate by soil microbes. Seikagagu<br />

(Biochemistry) 34, 92-98.<br />

Keywords: mon<strong>of</strong>luoroacetate/soil/fluoroacetate/enzyme/bacteria/temperature/resistance/degradation<br />

Abstract: Mon<strong>of</strong>luoroacetate is currently in extensive use as an agricultural insecticide and rodenticide.<br />

However, thsi fluoroacetate compound differs from other halo-carboxylic acids in having an extremely<br />

strong C-F bond which, for example, does not break even on on distillation with concentrated sulphuric<br />

acid at 170 degrees celcius and is only 50% broken after 20 hours <strong>of</strong> boiling with 20% caustic potash. For<br />

this reason there is a doubt as to whether fluoroacetates decompose when released into the environment. In<br />

South Africa a toxic plant known locally as Gifblaar has been found to be a fluoroacetate, and the<br />

concentration <strong>of</strong> the toxic compound is known to fluctuate on a seasonal basis. The problem <strong>of</strong> the enzymes<br />

associated with the formation and decomposition <strong>of</strong> these compounds in nature has therefore arisen, after<br />

being hitherto unknown. The author has previously determined the levels <strong>of</strong> mon<strong>of</strong>luoroacetamide residues<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

dispersed in various plants, and discovered that soil contains a bacterium which breaks the C-F bond in<br />

mon<strong>of</strong>luoroacetamide. This paper reports on the bacterium, which has been isolated and provisionally<br />

termed the C-F bacterium, and gives the results <strong>of</strong> research into the properties on the C-F bacterium and the<br />

enzymes which break the C-F bond. The properties <strong>of</strong> the C-F bacterium isolated from soil, which has the<br />

ability to break the C-F bond in mon<strong>of</strong>luoroacetate, were studied, and some reaesrch was done into the<br />

character <strong>of</strong> the C-F bond-breaking enzyme extracted from that bacterium;<br />

1. The bacterium is a gram-negative bacillus with polar flagella, and measures 0.3-0.7 by 0.5 to 2µ.<br />

2. The bacterium can be cultured at a pH ranging from 5.0 to 9.0, at an optimum temperature <strong>of</strong> 25-30<br />

degrees<br />

3. Its temperature resistance is low, the bacterium being killed by one minute at 60 degrees<br />

4. Study <strong>of</strong> its physiological properties showed that this bacterium strongly resembles Psuedomonas<br />

indoloxidans, but it is regarded as a separate species lacking the ability to oxidise indole.<br />

5. This bacterium breaks the C-F bond in mon<strong>of</strong>luoroacetate, but has no effect on difluoroacetate<br />

6. The enzyme which breaks the C-F bond occurs only inside the bacterium and is not excreted from it<br />

7. The enzyme extract solution was comparatively stable at low temperatures but unstable at high<br />

temperatures, and was found to be completely deactivated after 2 days at 35 degrees Celcius or 3 minutes at<br />

100 degrees Celcius<br />

8. The optimum temperature <strong>of</strong> the enzyme was 28 degrees celcius after testing for 3 hours, and 24 degrees<br />

after 4 hours<br />

9. The ezyme showed little dependence on pH, but the optimum pH range was from 7.5 to 8.0<br />

10. Salting out the ezymes with ammonium sulphate gave almost complete precipitation at an Osbourne<br />

saturation <strong>of</strong> 0.395<br />

11. The enzyme had an effect only on the FCH2CO- radical in the experiment<br />

12. The enzyme is believed to participate in the following reaction:<br />

FCH2COONa + H2O = HOCH2COONa + HF<br />

Horn, C. and Kilvington, M. Mäori and 1080. <strong>Landcare</strong> <strong>Research</strong> website . 2002.<br />

Ref Type: Internet Communication<br />

Keywords: humans/1080/poison<br />

Abstract: The toxin 1080 is used in New Zealand for the control <strong>of</strong> the introduced marsupial the brushtailed<br />

possum (Trichosurus vulpecula) for conservation purposes and for controlling the effects <strong>of</strong> Bovine<br />

Tuberculosis. The use <strong>of</strong> this poison is controversial. This report outlines a research project aimed at<br />

understanding how the quality <strong>of</strong> consultation processes affects the way that Mäori communities deal with<br />

the use <strong>of</strong> 1080 in their local areas.<br />

Mäori differ little to Päkehä in their range <strong>of</strong> views on the use <strong>of</strong> toxins in their local environments. On the<br />

whole, few people whether Mäori or Päkehä, are comfortable when toxins such as 1080 are aerially<br />

dropped in their local area, particularly when they take water from that area. For the community groups<br />

involved, it appears the issue is not purely about the use <strong>of</strong> 1080. Rather it is about the level <strong>of</strong> control local<br />

people feel they have over their own local environment.<br />

Authorities or people representing them must involve iwi and try to increase their sense <strong>of</strong> control. This<br />

means that they must work on their relationships with iwi and see these interactions as part <strong>of</strong> an ongoing<br />

process. Public controversy is less likely to constrain pest control operations if agencies manage pests in<br />

partnership with the appropriate iwi group. In a true partnership situation, agency representatives must<br />

respond honestly to the requests <strong>of</strong> the community and the community need to feel that the agency hears<br />

and responds to their concerns. Overall, it appears many agency representatives may need assistance with<br />

the communication processes involved in developing partnerships with iwi (or indeed any other community<br />

group). In particular it is important that representatives distinguish between informing groups and working<br />

with them in a partnership situation.<br />

Hornfeldt, C. S. and Larson, A. A. (1990). Seizures induced by fluoroacetic acid and fluorocitric acid may<br />

involve chelation<strong>of</strong> divalent ions in the spinal cord. European Journal <strong>of</strong> Pharmacology 179, 307-313.<br />

Keywords: brain/fluorocitrate/fluoroacetate/citrate/poisoning/citric acid/strychnine/convulsions<br />

Abstract: Fluoroacetic and fluorocitric acid toxicity is <strong>of</strong>ten characterised by seizures, however the<br />

mechanism <strong>of</strong> this activity is unknown. Intrathecal (i.t.) injection <strong>of</strong> fluorocitrate in mice resutled in<br />

seizures after an average latency <strong>of</strong> 15 seconds, while intracerebroventricular (i.c.v) injection produced<br />

seizures after 36.5 minutes and required higher dosages to acheive this effect. This indicates that the<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

probably site <strong>of</strong> fluoroacetate and fluorocitrate neurotoxicity is the spinal cord. To mimic citrate<br />

accumulation characteristic <strong>of</strong> fluoroacetate and fluorocitrate poisoning, citric acid was injected i.t. and also<br />

found to produce seizures. The structurally unrelated compounds EDTA, EGTA, glutamic acid and lactic<br />

acid also produced seizures identical to fluorocitrate. The ability <strong>of</strong> these compounds to chelate Ca2+<br />

correlates well with their ability to cause seizures when adminsitered i.t. and coadministration <strong>of</strong> calcium<br />

greatly attenuated the neurotoxicity <strong>of</strong> these compounds as well as fluoroacetate and fluorocitrate. In<br />

contrast, Ca2+ was unable to inhibit seizures elicited by strychnine, suggesting calcium's ability to inhibit<br />

chelators <strong>of</strong> divalent cations is not due to a general anticonvulsant effect. These results suggest that changes<br />

in Ca2+ concentration in the spinal cord may be responsible for some forms <strong>of</strong> seizure activity.<br />

Hornshaw, T. C. Development <strong>of</strong> dietary LC(,50) and reproduction test protocols using mink and ferrets as<br />

representative mammalian carnivores. 228. 1984. Michigan State UniversityEditor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: ferrets/carnivores/wildlife/reproductive effects/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/acute toxicity/toxicity<br />

Abstract: Representative mammalian wildlife species have not been designated as toxicological models for<br />

testing substances <strong>of</strong> environmental concern. The mink (Mustela vison) and the European ferret (M.<br />

putorius furo) have been suggested as representative mammalian species since they are among the most<br />

sensitive mammalian species to the toxic and reproductive effects <strong>of</strong> several substances. Also, as<br />

carnivores, these species are subject to the effects <strong>of</strong> bioaccumulation <strong>of</strong> lipophilic compounds. Therefore,<br />

dietary LC(,50) and reproduction tests were initiated with these species, using sodium mon<strong>of</strong>luoroacetate<br />

(Compound 1080), o-cresol, tetramethylthiuram disulfide (thiram), and a polychlorinated biphenyl (Aroclor<br />

1254) as test substances to develop protocols for these tests. The results <strong>of</strong> the various tests demonstrate<br />

that mink and ferrets may be used in subacute and reproduction tests with a wide range <strong>of</strong> test substances,<br />

since the test substances used represented a wide range <strong>of</strong> solubilities, volatilities, acute toxicities, modes <strong>of</strong><br />

action, and chemical classes. Since the tests were conducted indoors under controlled conditions, it is<br />

expected that the results should be reproducible in similarly equipped laboratories. Factors demonstrated in<br />

these tests that may affect the determination <strong>of</strong> toxicity <strong>of</strong> a substance include the age <strong>of</strong> the animal at the<br />

beginning <strong>of</strong> a test and the carrier used to introduce the substance into the diet, while the diet's composition<br />

(as long as it meets the nutrient requirements <strong>of</strong> the test species) and the season <strong>of</strong> the year may have little<br />

or no effect on the results <strong>of</strong> the test. Dietary LC(,50) tests may be conducted with as few as 32 animals (3<br />

test concentrations plus control, 8 animals per concentration) if an accurate acute oral LD(,50) is available,<br />

while reproduction tests may require 64 animals (3 test concentrations plus control, 16 animals per<br />

concentration) if unproven breeders are used<br />

Hornshaw, T. C., Ringer, R. K., Aulerich, R. J., and Casper, H. H. (1986). Toxicity <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (Compound 1080) to mink and European ferrets. Environmental toxicology and<br />

chemistry 5, 213-223.<br />

Keywords: acute toxicity/non-target species/pathology/1080/ferrets/blood/testes/reproductive effects<br />

Abstract: The toxicity <strong>of</strong> sodium monolfluoroacetate (Compound 1080) to mink (Mustela vison) and<br />

European ferrets (Mustela putorius furo) was evaluated through LC50 and reproduction tests. Subacute<br />

dietary exposure to Compound 10890 resulted in dose dependent decreases in body weights and feed<br />

consumption in both species. The mink were more sensitive to Compound 1080 than were the ferrets. The<br />

28d dietary LC50 for mink and for ferrets was calculated to be 3.2 and 9.4ppm respectively. Dietary<br />

exposure to 0.80 ppm Compound 1080 for 2 months prior to breeding severely impaired reproduction in the<br />

mink, which was presumed to be due to oligoor aspermia. In young, rapidly growing ferrets, red and white<br />

blood cell counts were adversely affected by dietary concentrations <strong>of</strong> Compound 1080 as low as 1.08 ppm.<br />

The 28d LC50 test, however, revealed that young, rapidly growing animals may be unsuitable for tests <strong>of</strong><br />

this duration unless precautions are taken to assure that they do not "outgrow" potentially lethal<br />

concentrations <strong>of</strong> the test chemical.<br />

Hosek, B., Novak, L., and Misustova, J. (1970). Mathematical evaluation <strong>of</strong> the course <strong>of</strong> body temperature<br />

in mice after the administration <strong>of</strong> sodium fluoroacetate. Physiol.Bohemoslov. 19, 129-133.<br />

Keywords: temperature/sodium fluoroacetate/fluoroacetate<br />

Abstract: The authors carried out a theoretical evaulation <strong>of</strong> body temperature changes in mice after the<br />

administration <strong>of</strong> 5 mg FAc/kg at environmental temperatures <strong>of</strong> 30º, 23º and 17ºC. A differential equation<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

for the course <strong>of</strong> the body temperature, based on the recipricoal relationship <strong>of</strong> hear production and hear<br />

output, was formed and an analogue computer study was done. Changes in effective heat conductivity<br />

during several hours' exposure to FAc did not signficantly influence the course <strong>of</strong> the body temperature.<br />

The effectiveness <strong>of</strong> their influence and the significance <strong>of</strong> the environmental temperature for adjustment <strong>of</strong><br />

the body temperature in the presence <strong>of</strong> limited heat production is discussed.<br />

Howard, W. E. (1965). <strong>Control</strong> <strong>of</strong> introduced mammals in New Zealand. New Zealand Department <strong>of</strong><br />

Scientific and Industrial <strong>Research</strong> Information Series 45, 1-96.<br />

Keywords: deer/goats/mammals/pigs/predators/rabbits/resistance/soil<br />

Abstract: New Zealand has a multiplicity <strong>of</strong> important ecologically challenging, animal control<br />

problems that must be seen to be believed. They are the consequence <strong>of</strong> intentionally introducing a number<br />

<strong>of</strong> mammals for sport, food, fur, or mistakenly, as predators <strong>of</strong> the introduced rabbits. These introduced<br />

mammals have upset the natural stability <strong>of</strong> the habitats over large areas by destroying vegetation, thus also<br />

causing extensive erosion. The principal reasons for the destructiveness <strong>of</strong> the exotic big game animals, fur<br />

bearers, and wild pigs and goats to certain habitats in New Zealand are (1) some <strong>of</strong> the soils are highly<br />

susceptible to erosion, (2) the mountainous country <strong>of</strong>ten gets high intensity rainfall, and (3) many <strong>of</strong> the<br />

endemic plants have little innate resistance to heavy, selective, grazing or browsing. As a result <strong>of</strong> these<br />

introductions, an irreversible change in the composition <strong>of</strong> the vegetation has occurred throughout many <strong>of</strong><br />

the mountain ranges. However, where enough soil has remained, and where browse-resistant and<br />

unpalatable plants have replaced adequately those destroyed by the browsing mammals, a new and stable<br />

equilibrium <strong>of</strong> the animal-vegetation-soil complex has developed. But on some mountains both the A and<br />

B soil horizons have been lost.<br />

It appears that the problem species <strong>of</strong> introduced mammals cannot be eradicated from New Zealand.<br />

Consequently, it would seem to be more prudent from a long term viewpoint to accept the concomitant<br />

vegetational changes, especially where they do not adversely affect watershed conservation. Therefore, a<br />

logical long-term objective toward the noxious animal problem is to strive for habitat stability, whether by<br />

reseeding, shooting by private hunters, or, wherever the exotic animals have upset seriously the soilvegetation<br />

stability <strong>of</strong> the original communities, by intensive animal control by government personnel.<br />

Better means <strong>of</strong> either repelling troublesome mammals or <strong>of</strong> achieving more effective reduction <strong>of</strong> their<br />

numbers with chemicals and other means are urgently required now to protect critical areas and localised<br />

sites where the introduced mammals are still depleting the land or are maintaining it in an unstable<br />

condition. In the future we must learn to tolerate deer in some areas while at the same time controlling<br />

them more effectively in other.<br />

Howard, W. E., Marsh, R. E., and Palmateer, S. D. (1973). Selective breeding <strong>of</strong> rats for resistance to<br />

sodium mon<strong>of</strong>luoroacetate. Journal <strong>of</strong> applied ecology 10, 731-736.<br />

Keywords: acute toxicity/rats/resistance/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/lethal dose<br />

Abstract: There is little evidence in the literature indicating that pest vertebrates have developed genetic<br />

resistance to rodenticides. This study ahs confirmed that Long-Evans rats, thus rpesumably also wild rats,<br />

have the propensity <strong>of</strong> developing considerable genetic resistance to the rodenticide sodium<br />

mon<strong>of</strong>luoroacetate (commonly called compound 1080). After five generations <strong>of</strong> nonintensive selective<br />

breeding, the approximate LD50 changed from 2 mg/kg <strong>of</strong> 1080 for the parents to 3.5 mg/kg for the F4<br />

generation. The percentage survival <strong>of</strong> F4 rats stomach-tubed with 5 mg/kg <strong>of</strong> 1080 was 3.75 times as great<br />

as occurred with the parental stock and 4.75 at 6 mg/kg.<br />

Howard, W. E., Marsh, R. E., and Cole, R. E. (1977). Duration <strong>of</strong> associative memory to toxic bait in deer<br />

mice. Journal <strong>of</strong> wildlife management 41, 484-486.<br />

Keywords: fluoroacetate/metabolism/bait shyness/baits/rodents/behaviour/mice<br />

Abstract: Deer mice (Peromyscus maniculatus) conditioned by sublethal doses to avoid eating oat kernels<br />

dipped in sodium fluoracetate (1080) were held for 1,2,4 and 8 months without access to any oats. When<br />

tested for aversion, no mouse tested directly with poisoned oats, at all 4 kernels <strong>of</strong>fered each day, although<br />

9% ate fatal amounts. Of 32 mice prebaited with clean oats for 2 days, only 72% consumed lethal amounts.<br />

Deer mouse control should not employ the same poison at intervals shorter than 8 months.<br />

Huang, T. Y. (1980). The toxicity <strong>of</strong> fluoroacetic acid derivatives as antischistosomal agents in rabbits.<br />

National Medical Journal <strong>of</strong> China 60, 340.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: toxicity/rabbits/antidote/metabolism/citric acid<br />

Abstract: All rabbits given fluoroacetyl glycine (1.5 mg/kg body-weight) without antidote died from<br />

ventricular fibrillation within 2 to 6 h. More than half <strong>of</strong> those given reserpine and oxytocin as antidote<br />

survived and all <strong>of</strong> those given acetamide before and together with fluoroacetyl glycine survived. None <strong>of</strong><br />

those given acetamide 1.5 h after fluoroacetyl glycine survived. It is suggested that fluoroacetic acid<br />

derivatives may cause a blockage <strong>of</strong> the metabolism <strong>of</strong> citric acid in rabbits<br />

Huang, T. Y. (1980). The energy metabolism <strong>of</strong> Schistosoma japonicum. International Journal <strong>of</strong><br />

Biochemistry 12, 457-464.<br />

Keywords: metabolism/fluoroacetate/fluoroacetamide/invertebrates<br />

Abstract: Work carried out by the author since 1959 on the energy metabolism <strong>of</strong> Schistosoma japonicum is<br />

summarized under the headings: influence <strong>of</strong> the composition <strong>of</strong> the medium on respiration and glycolysis;<br />

identification <strong>of</strong> a functional tricarboxylic acid cycle; effects <strong>of</strong> fluoroacetate and its derivatives on the<br />

tricarboxylic acid cycle; effects <strong>of</strong> fluoroacetamide on glycolysis. Findings are compared with those <strong>of</strong><br />

other workers, particularly with regard to S. mansoni<br />

Hudick, J. P. (1972). Studies on the toxic isomer <strong>of</strong> fluorocitrate. Biochemistry 2931-B-2932-B.<br />

Keywords: fluorocitrate/fluoroacetate<br />

Abstract: Preliminary enzymatic studies with R and S tritated fluoroacetate have been performed, and the<br />

amount <strong>of</strong> enzymatically synthesized T2O and tritated fluorocitrate has been quantitated after<br />

chromatagraphic resolution. The results show a dilution <strong>of</strong> counts in fluorocitrate (as compared to T2O)<br />

with time.<br />

These studies are presently being investigated in depth as a possible means <strong>of</strong> determining the absolute<br />

configuration <strong>of</strong> the inhibitory isomer <strong>of</strong> fluorocitrate.<br />

Hudson, R. H., Tucker, R. K., and Haegele, M. A. (1972). Effect <strong>of</strong> age on sensitivity: acute oral toxicity <strong>of</strong><br />

14 pesticides to mallard ducks <strong>of</strong> several ages. Toxicology and applied phamacology 22, 556-561.<br />

Keywords: lethal dose/birds<br />

Abstract: Acute po LD50 values for 14 common pesticides (4 central nervous system stimulants and 10<br />

anticholinesterases) were determined on mallard ducks (Anas platyrhynchos) aged 36 hr, 7 days, 30 days<br />

and 6 mo. The youngest mallards were more sensitive than the oldest to 6 compounds and less sensitive to<br />

8. the extremes in susceptability to a compound between age groups were generally less than 3-fold. The 4<br />

central nervous system stimulants produced LD50 values that decreased from 36 hr to 7 or 30 day old<br />

animals, and increased from animals aged 7 or 30 day old animals, and decreased from animals aged 7 or<br />

30 days to 6 mo. the results indicate that young animals are not always more susceptible to pesticides than<br />

adults <strong>of</strong> a species. It is recommended that age-susceptability factors be considered in the development <strong>of</strong><br />

standardized toxicological protocols.<br />

Hudson, R. H., Tucker, R. K., and Haegele, M. A. (1984). Sodium Mon<strong>of</strong>luoroacetate. In 'Handbook <strong>of</strong><br />

Toxicity <strong>of</strong> Pesticides to Wildlife'. pp. 73-74. (United States Department <strong>of</strong> the Interior: Washington, D.C.)<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/wildlife/birds/ferrets/deer<br />

Abstract: LD50's for birds and ferrets and mule deer.<br />

Hugghins, E. J., Casper, H. H., and Ward, C. D. (1988). Tissue fluoroacetate residues in prairie dogs dosed<br />

with low-level sodium mon<strong>of</strong>luoroacetate. Journal <strong>of</strong> the Association <strong>of</strong> Official Analytical Chemists 71,<br />

579-581.<br />

Keywords: secondary poisoning/fluoroacetate/sodium mon<strong>of</strong>luoroacetate/ferrets/mammals/persistence in<br />

animals<br />

Hughes, G. M. K. and Saunders, B. C. (1954). Enzymatic rupture <strong>of</strong> a C-F bond. Chemistry in Britain<br />

[1954], 1265.<br />

Keywords: product chemistry<br />

Hulsmann, S., Oku, Y., Zhang, W. Q., and Richter, D. W. (2000). Metabotropic glutamate receptors and<br />

blockade <strong>of</strong> glial Krebs cycle depress glycinergic synaptic currents <strong>of</strong> mouse hypoglossal motoneurons.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

European journal <strong>of</strong> neuroscience 12, 239-246.<br />

Keywords: mode <strong>of</strong> action<br />

Hulsmann, S., Oku, Y., Zhang, W. Q., and Richter, D. W. (2000). Metabolic coupling between glia and<br />

neurons is necessary for maintaining respiratory activity in transverse medullary slices <strong>of</strong> neonatal mouse.<br />

European journal <strong>of</strong> neuroscience 12, 856-862.<br />

Keywords: mode <strong>of</strong> action<br />

Hutchens, J. O., Wagner, H., Podolsky, B, and McMahon, T. M. (1949). The effect <strong>of</strong> ethanol and various<br />

metabolites on fluoroacetate poisoning. J.Pharmacology & Exp.Therapy 95, 62-70.<br />

Keywords: sodium fluoroacetate/treatment/mode <strong>of</strong> action/rabbits/dogs/fluoroacetate/poisoning<br />

Hutcheson, J. A. Impact <strong>of</strong> 1080 on weta populations. Forest <strong>Research</strong> Institute Unpublished Report, -6.<br />

27-4-1990.<br />

Ref Type: Report<br />

Keywords: 1080/baits/poisoning/invertebrates/sublethal effects<br />

Abstract: Caged weta (Hemideina thoracica) were <strong>of</strong>fered 1080 poison impregnated grain based pellets in<br />

the laboratory. 50% <strong>of</strong> the weta <strong>of</strong>fered the toxic baits died, while the other 50% suffered sublethal<br />

poisoning which altered their behavioural patterns. This did not occur with the control group <strong>of</strong> those<br />

<strong>of</strong>fered non-toxic baits.<br />

Igamberdiev, A. U., Popov, V. N., and Falaleeva, M. I. (1995). Succinate metabolization in fat-storing<br />

tissues <strong>of</strong> germinating cereal seeds. Russian Journal <strong>of</strong> Plant Physiology 42, 100-105.<br />

Keywords: metabolism/treatment/fluoroacetate/fluorocitrate/aconitase/biosynthesis/persistence in plants<br />

Abstract: Succinate metabolism was investigated in scutella <strong>of</strong> germinating wheat cv. Severdonskaya and<br />

maize cv. Voronezhskaya 76 seeds, Ricinus communis endosperm, and sunflower cv. Trudovik and<br />

soyabean cv. Amurskaya cotyledons. In scutella, succinate oxidation via the conventional mitochondrial<br />

succinate dehydrogenase coexisted with a tenoyltrifluoroacetone- and malonate-insensitive succinate<br />

oxidase system, which was strictly confined to the glyoxysomal membranes. Malate and H2O2 were<br />

identified as products <strong>of</strong> this glyoxysomal succinate oxidase complex. The complex was most active during<br />

enhanced operation <strong>of</strong> the glyoxylate cycle, with a pH optimum at 7.5-8 and an apparent Km value for<br />

succinate <strong>of</strong> 18 ± 4 mM, which is much higher than that known for succinate dehydrogenase. Neither<br />

sunflower or soyabean cotyledons, nor R. communis endosperm demonstrated glyoxysomal succinate<br />

oxidase activity. Treatment <strong>of</strong> [1.4-14C]-succinate-fed maize scutella with tenoyltrifluoroacetone, an<br />

inhibitor <strong>of</strong> succinate dehydrogenase, dramatically reduced label incorporation into the sugar fraction,<br />

increased 14CO2 evolution, and did not significantly affect the amino acid labelling pattern. Fluoroacetate,<br />

which is known to convert to fluorocitrate, an inhibitor <strong>of</strong> aconitase, suppressed both the tricarboxylic acid<br />

and the glyoxylate cycles, decreased the label incorporation from succinate to organic acids and potentiated<br />

the biosynthesis <strong>of</strong> labelled amino acids, notably alanine, glutamic acid, aspartic acid, serine, valine, and<br />

lysine. Thus, succinate oxidation by the glyoxysomal succinate oxidase complex was associated with its<br />

conversion to amino acids, organic acids, and CO2. It was concluded that succinate oxidation in cereal<br />

scutellum glyoxysomes, which bypassed a control pressure from the tricarboxylic acid cycle and respiratory<br />

chain, enables rapid succinate mobilization during large-scale synthesis through the glyoxylate cycle<br />

Imesch, E. and Rous, S. (1984). Partial purification <strong>of</strong> rat liver cytoplasmic acetyl-CoA synthetase;<br />

characterization <strong>of</strong> some properties. Int.J.Biochem. 16, 875-881.<br />

Keywords: liver<br />

Abstract: 1. Rat liver cytoplasmic acetyl-CoA synthetase was partially purified (purification factor = 23,<br />

yield = 30%).<br />

2. The apparent Kms for acetate, coenzyme A, ATP and MgCl2 were determined and found to be 52.5 µM,<br />

50.5 µM, 570 µM and 1.5 mM, respectively.<br />

3. The partially-purified enzyme showed a low affinity for short-chain carbon substrates other than acetate.<br />

4. The properties <strong>of</strong> the partially-purified enzyme were compared with those <strong>of</strong> enzymes from other<br />

sources.<br />

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Innes, J., Warburton, B., Williams, D., Speed, H., and Bradfield, P. (1995). Large-scale poisoning <strong>of</strong> ship<br />

rats (Rattus rattus) in indigenous forests <strong>of</strong> the North Island, New Zealand. New Zealand journal <strong>of</strong> ecology<br />

19, 5-17.<br />

Keywords: poisoning/rats/1080/brodifacoum/birds/baits/field efficacy<br />

Abstract: This paper describedthe impact <strong>of</strong> nine poison operations on ship rats in four areas (35 ha to 3200<br />

ha) <strong>of</strong> North Island forest. Poisoning with 1080, brodifacoum, or pindone killed 87-100% <strong>of</strong> rats, based on<br />

trapping and tracking-tunnel indices. Rat populatiosn took 4-5 months to recover. Operations to protect<br />

nesting birds should therefore coincide with the onset <strong>of</strong> nesting and be repeated each year, although not<br />

necessarily with the same methods. Population reduction declined each year at Mapara, King Country<br />

during three annual 1080 operations which used the same lures and baits, but remained high at Kaharoa,<br />

Bay <strong>of</strong> Plenty, where poison toxicity was higher, non-toxic bait was pre-fed, and poisoning methods varied<br />

each year. Mouse tracking rates increased in poisoned forests 3-6 months fater poisoning if the initial kill <strong>of</strong><br />

rats exceeded 90%, peaked 7-9 months after poisoning then declined to pre-poison levels.<br />

Innes, J. and Barker, G. (1999). Ecological consequences <strong>of</strong> toxin use for mammalian pest control in New<br />

Zealand : an overview. New Zealand journal <strong>of</strong> ecology 23, 111-127.<br />

Keywords: field efficacy/target species/non-target species/persistence in animals/persistence in<br />

plants/persistence in soil/persistence in water/1080/brodifacoum/mammals<br />

Abstract: Toxins, especially sodium mon<strong>of</strong>luoroacetate (1080) and brodifacoum, are widely used<br />

throughout New Zealand for control <strong>of</strong> introduced mammals that are considered pests. This level <strong>of</strong> toxin<br />

use (not necessarily with these toxins) is unlikely to decline for at least 5-10 years. Ecological<br />

consequences derive both from mammal population reduction or eradication, and from using toxins as the<br />

control method. Scientists have not examined the net ecological outcomes <strong>of</strong> these consequences at the<br />

community level due to their daunting complexity, although managers usually manipulate whole<br />

communities and key conservation legislation demands that they do so. A food web could be a useful<br />

conceptual framework to generate hypotheses about toxin movement through communities, and to explore<br />

net outcomes <strong>of</strong> pest control at the community level. It could also sharpen objectives for ecosystem<br />

restoration on the New Zealand mainland, and help to find common ground between different participants<br />

in ecosystem management. We interpret present evidence to suggest that the ecological costs <strong>of</strong> using<br />

toxins are much less than the damage costs if they are not used, due to the magnitude <strong>of</strong> known impacts <strong>of</strong><br />

introduced pest mammals. This suggestion deserves exploration; it may not be true when persistent toxins<br />

such as brodifacoum are used repeatedly. <strong>Research</strong> on toxin use should continue on its present broad front,<br />

but we suggest that priorities are to measure net ecological outcomes at the community level, to reduce<br />

toxin use, and to improve pest control strategies and techniques in the maintenance phase <strong>of</strong> control<br />

operations. Finally, we suggest that an annual ecosystem management conference in New Zealand, which<br />

explicitly brings together managers, policymakers, landowners, and scientists from the many disciplines<br />

now relevant to the complex field <strong>of</strong> pest mammal control, would enhance progress and co-operation.<br />

Janero, D. R. and Hreniuk, D. (1996). Suppression <strong>of</strong> TCA cycle activity in the cardiac muscle cell by<br />

hydroperoxide-induced oxidant stress. American journal <strong>of</strong> physiology 270, C1735-C1742.<br />

Keywords: cardiac/muscle<br />

Abstract: Excess H2O2 contributes to myocardial reperfusion injury. We detail the effect <strong>of</strong> H2O2-induced<br />

oxidant stress on the tricarboxylic acid (TCA) cycle in isolated heart muscle cells. Cardiomyocyte<br />

exposure to bolus H2O2 (>50 µM) acutely suppressed TCA cycle activity. Loss <strong>of</strong> cardiomyocyte TCA<br />

cycle function on cellular H2O2 exposure was supported by the rapid in situ inactivation <strong>of</strong> aconitase along<br />

with cardiomyocyte membrane peroxidation. Without peroxidation, the loss <strong>of</strong> aconitase catalysis was<br />

itself sufficient to jeopardize TCA cycle activity. Only H2O2 dismutation completely preserved both<br />

cardiomyocyte aconitase activity and TCA cycle flux during H2O2 overload. Restoration <strong>of</strong> aconitase<br />

catalsis after alleviation <strong>of</strong> the oxidant insult was prohibited by cell-permeable metal chelators, and TCA<br />

cycle flux could not be reestablished in peroxidized cells, even if aconitase activity had recovered. The<br />

characteristics <strong>of</strong> aconitase inactivation-reactivation observed are consistent with adverse redox changes to<br />

the enzyme's (Fe-S) cluster. These data demonstrate that specific aspects <strong>of</strong> the TCA cycle in heart muscle<br />

are sensitive to H2O2-induced oxidative stress and identify a peroxidative component <strong>of</strong> the injury process.<br />

Jarrett, I. G. and Packham, A. (1956). Response <strong>of</strong> sheep to sublethal doses <strong>of</strong> fluoroacetate. Nature 4508,<br />

580-581.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: fluoroacetate/citrate/blood/convulsions/mammals/symptoms<br />

Abstract: The effect <strong>of</strong> continued administration <strong>of</strong> sublethal doses <strong>of</strong> fluoroacetate to sheep was<br />

investigated.<br />

Jensen, R., Tobiska, J. W., and Ward, J. C. (1948). Sodium fluoroacetate (Compound 1080) poisoning in<br />

sheep. American Journal <strong>of</strong> Veterinary <strong>Research</strong> 9, 370-372.<br />

Keywords: sodium<br />

fluoroacetate/fluoroacetate/1080/poisoning/symptoms/convulsions/heart/livestock/mammals/lethal dose<br />

Abstract: Under conditions <strong>of</strong> the experiment, the m.l.d. <strong>of</strong> sodium fluoroacetate for sheep was between<br />

0.25 and 0.50 mg per kilogram <strong>of</strong> body weight. The m.l.d. was also the minimal dose producing symptoms.<br />

The time interval between administration and manifestation <strong>of</strong> symptoms varied inversely with the size <strong>of</strong><br />

the dose. Symptoms <strong>of</strong> poisoning were motor irritation, excitation, rapid pulse becoming weak, general<br />

weakness, convulsions and death; heart action ceased before respiration. All animals showing symptoms<br />

died. The 2 survivors received the lowest dosage and appeared normal at all times. A modified field rodent<br />

bait prepared with steam rolled oats, containg 1 mg sodium fluoroacetate per gram <strong>of</strong> gram was used in this<br />

experiment.<br />

Jeong, J. M., Lee, D. S., Chung, J. K., Lee, M. C., Koh, C. S., and Kang, S. S. (1997). Synthesis <strong>of</strong> nocarrier-added<br />

[ 18 F] fluoroacetate. Journal <strong>of</strong> labelled compounds and radiopharmaceuticals 39, 395-399.<br />

Keywords: product chemistry<br />

Johannsen, F. R. and Knowles, C. O. (1972). Citrate accumulation in twospotted spider mites, house flies,<br />

and mice following treatment with the acaricide 2-fluoro-N-methyl-N-(1-naphthyl) acetamide. Journal <strong>of</strong><br />

economic entomology 65, 1754-1756.<br />

Keywords: citrate/treatment/mammals/fluoroacetate/fluorocitrate/aconitase/Krebs cycle/mode <strong>of</strong><br />

action/citric acid/liver/brain/symptoms/poisoning/inhibition/invertebrates<br />

Abstract: Nissol (2-fluoro-N-methyl-N-1-naphthylacetamide), which is selectively toxic to several species<br />

<strong>of</strong> insects and mites but not very toxic to mammals, is hydrolysed to the substituted naphthylamine and<br />

fluoroacetate in all three types <strong>of</strong> organism. Such hydrolysis is common to the N-containing derivatives <strong>of</strong><br />

fluoroacetic acid, all <strong>of</strong> which cause accumulation <strong>of</strong> citrate in treated organisms through (it is thought)<br />

conversion <strong>of</strong> the fluoroacetate to fluorocitrate, a known inhibitor <strong>of</strong> the activity <strong>of</strong> aconitase on citrate in<br />

the Krebs cycle. To find whether this is the likely mode <strong>of</strong> action <strong>of</strong> Nissol, the amounts <strong>of</strong> citric acid in<br />

mice, house-flies (Musca domestica L.) and two-spotted spider mites (Tetranychus urticae Koch) were<br />

determined before and up to 12 h after they had been treated with half the respective LD50's and LC50 <strong>of</strong><br />

the compound. Preliminary tests, in which mortalities were recorded 24 h after treatment, showed the LD50<br />

for mice to be 200 mg/kg body weight by intraperitoneal injection, those for house-flies to be 14 mg/kg by<br />

injection and 525 mg/kg by topical application, and the LC50 for mites to be 250 p.p.m. [cf. RAE/A 61,<br />

274] by the slide-dip technique [cf. 52, p.103]. In the main tests, the amounts <strong>of</strong> citric acid found 12 h after<br />

treatment with Nissol were in mg/g, 0.30 in mice (as compared with 0.13 in untreated examples), 0.68 in<br />

house-flies (0.48) and 0.60 in mites (0.36). The amounts in mouse tissues varied from 81.1 mg/kg in liver<br />

to 512.5 mg/kg in brain, compared with 41.0 and 166.0 in untreated examples. These rises, together with<br />

the fact that typical symptoms <strong>of</strong> organ<strong>of</strong>luorine poisoning were observed, suggest that Nissol acts by<br />

inhibition <strong>of</strong> aconitase in all three test species<br />

Jones, L. M. (1948). 1080 poisoning in dogs. N.Amer.Vet 29, 725-726.<br />

Keywords: 1080/poisoning/dogs<br />

Kailis, S. G. and Morgan, E. H. (1977). Iron uptake by immature erythroid cells. Mechanism <strong>of</strong> dependence<br />

on metabolic energy. Biochem.Biophys.Acta. 464, 389-398.<br />

Keywords: metabolism/bone/sodium fluoroacetate/fluoroacetate/blood<br />

Abstract: The mechanism by which the utilization <strong>of</strong> transferrin-bound iron is linked with cellular<br />

metabolism was investigated using rabbit reticulocytes and bone marrow cells. The rate <strong>of</strong> metabolism was<br />

altered by the use <strong>of</strong> inhibitors which act at different sites in the metabolic pathway (NaF, sodium<br />

fluoroacetate, rotenone, 2,4-dinitrophenol, NaCN) and by the addition <strong>of</strong> metabolic substrates (inosine,<br />

sodium pyruvate, sodium lactate). Measurements were made <strong>of</strong> the rates <strong>of</strong> iron and transferrin uptake and,<br />

in many <strong>of</strong> the experiments <strong>of</strong> cellular ATP and NADH concentrations. The results showed that there was a<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

significant correlation between the rate <strong>of</strong> iron uptake and the ATP concentration <strong>of</strong> the cells, but no<br />

correlation was found with the NADH concentration. The rate <strong>of</strong> transferrin uptake was inhibited to a lesser<br />

degree than that <strong>of</strong> iron uptake, and only when the ATP concentration had fallen below that necessary to<br />

inhibit iron uptake. It is concluded that the rate <strong>of</strong> uptake <strong>of</strong> transferrin-bound iron by immature erythroid<br />

cells is dependent on the intracellular concentration <strong>of</strong> ATP but is independent <strong>of</strong> the NADH concentration<br />

Kalinowski, S. A. and deCalesta, D. S. (1981). Baiting regimes for reducing ground squirrel damage to<br />

alfalfa. Wildlife Society bulletin 9, 268-272.<br />

Keywords: efficacy/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/USA/field efficacy<br />

Abstract: Damage by Belding's ground squirrels (Spermophilus beldingi) to alfalfa and the efficacies <strong>of</strong> 3<br />

baiting regimes to reduce damage were evaluated in southcentral Oregon during March-July 1977. Regimes<br />

examined were number <strong>of</strong> applications (1 or 2) and inclusion <strong>of</strong> a baited border around baited fields. Bait<br />

was sodium mon<strong>of</strong>luoroacetate (1080) on oat groats.<br />

Kalmbach, E. R. (1945). "Ten-eighty" : a war-produced rodenticide. Science 102, 232-233.<br />

Keywords: field efficacy<br />

Abstract: The manufacture <strong>of</strong> "1080" is still on a limited scale and for the experimental work still under<br />

way. Indications are that, because <strong>of</strong> its high toxicity, the material will become, under volume production, a<br />

relatively cheap poison. At the present time, the many unknowns regarding it and the restricted basis on<br />

which it is being produced preclude the use <strong>of</strong> "1080" by the public or even by rodent control operators<br />

generally. It is reasonably ceratin that the discovery <strong>of</strong> "1080" assures this nation <strong>of</strong> a highly effective<br />

economic poison which can not be denied this country through any future interruptions <strong>of</strong> world trade.<br />

Kalnitsky, G. (1948). The effect <strong>of</strong> BaCl2, MgCl2 and fluoroacetate on the formation and utilization <strong>of</strong><br />

citrate. Arch.Biochem. 403-411.<br />

Keywords: fluoroacetate/citrate/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate<br />

Abstract: BaCl2, MgCl2 and sodium mon<strong>of</strong>luoroacetate increase the formation <strong>of</strong> citrate from oxaloacetate<br />

by a rabbit kidney cortex homogenate. Mg ++ is twice as effective as Ba ++ . Ba ++ seems to have more than<br />

one concentration optimum, and inhibits at higher concentrations.<br />

MgCl2 and sodium fluoroacetate are equally effective, over a wide range <strong>of</strong> concentrations. The other<br />

halogen acetates do not increase citrate formation from oxoacetate.<br />

The effects <strong>of</strong> BaCl2 and MgCl2 in increasing citrate formation can be accounted for by the inhibition <strong>of</strong><br />

citrate utilization by the tissue, Mg ++ being somewhat superior to Ba ++ in this respect.<br />

The slight inhibition <strong>of</strong> citrate utilization at higher concentrations <strong>of</strong> fluoroacetate can only account for<br />

about 60% <strong>of</strong> the increased citrate formation from oxaloacetate, in the presence <strong>of</strong> fluoroacetate.<br />

The possible mechanisms <strong>of</strong> action <strong>of</strong> Ba ++, Mg ++ , and fluoroacetate, in this system, are discussed.<br />

Kamau, J. A., Gachuhi, D. M., Gyrd Hansen, N., and Gathuma, J. M. (1978). A study <strong>of</strong> the toxicity <strong>of</strong><br />

Dichapetalum ruhlandii (Ludi). Indian Veterinary Journal 55, 626-630.<br />

Keywords: toxicity/rats/liver/kidney/occurrence in nature/pathology/heart<br />

Abstract: Toxicity <strong>of</strong> the shrub was demonstrated in guinea-pigs, rats and calves, fed on extract <strong>of</strong> ground<br />

material from the leaves or branches. Calves developed hydropericardium with haemorrhages on the epi-<br />

and endocardium. The peritoneal cavities contained 1.5-2 litres <strong>of</strong> fluid. Haemorrhages also occurred on the<br />

lungs and there was some haemorrhagic enteritis. Histologically, there were degenerative changes <strong>of</strong> the<br />

myocardium and extensive congestion <strong>of</strong> the liver and kidneys. Congestion was also observed in the lungs,<br />

meninges and intestinal mucosa. Clinical and PM findings were similar to those in calves poisoned by D.<br />

cymosum in which the toxic principle is fluoracetic acid. The acidic component <strong>of</strong> D. ruhlandii was shown<br />

to be toxic to guinea-pigs. This extract was not identified but some properties indicate the presence <strong>of</strong><br />

fluoroacetic acid in the crude acidic extract<br />

Kandel, A. and Chenoweth, M. B. (1952). Tolerance to fluoroacetate and fluorobutyrate in rats.<br />

J.Pharmacology & Exp.Therapy 104, 248-252.<br />

Keywords: tolerance/fluoroacetate/rats/citrate/brain/resistance<br />

Abstract: The citrate content <strong>of</strong> rat brain appears to have no relation to the tolerance to fluoroacetate which<br />

has been observed. The citrate which accumulates in rat brain as the result <strong>of</strong> a small dose <strong>of</strong> fluoroacetate<br />

does not prevent the further formation <strong>of</strong> citrate when larger doses <strong>of</strong> fluoroacetate are given. Small doses<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

<strong>of</strong> fluoroacetate increase the resistance in rats to challenging doses <strong>of</strong> <strong>of</strong> fluoroacetate or 4-fluorobutyrate.<br />

Resistance to fluoroacetate <strong>of</strong> 4-fluorobutyrate could not be evoked when rats were intiailly treated with<br />

small doses <strong>of</strong> 4-fluorobuyrate.<br />

Karam, J., Harrison, M., Hartog, M., and Fraser, R. (1961). Renal citrate and urinary calcium excretion -<br />

the effects <strong>of</strong> growth hormone contrasted with those <strong>of</strong> sodium fluoroacetate. Clinical Science 21, 265-272.<br />

Keywords: citrate/excretion/sodium fluoroacetate/fluoroacetate/rats/plasma/urine<br />

Abstract: In rats, administration <strong>of</strong> bovine growth hormone led to an increase in urinary calcium excretion<br />

associated with a fall in renal concentration <strong>of</strong> citrate. Plasma citrate was uncahnged, while urinary citrate<br />

either increased or remained constant.<br />

Kato, T., Shimamoto, Y., Uchida, J., Ohshimo, H, Abe, M., Shirasaka, T., and Fukushima, M. (2001).<br />

Possible regulation <strong>of</strong> 5-fluorouracil-induced neuro- and oral toxicities by two biochemical modulators<br />

consisting <strong>of</strong> S-1, a new oral formulation <strong>of</strong> 5-fluorouracil. Anticancer <strong>Research</strong> 21, 1705-1712.<br />

Keywords: 5-fluorouracil/biochemistry/fluoroacetate/treatment/convulsions<br />

Abstract: S-1 is a new oral formulation <strong>of</strong> 5-fluorouracil (5-FU) containing 1M tegafur and 0.4M 5-chloro-<br />

2,4-dihydroxypyridine (CDHP) and 1M potassium oxonate (Oxo). It has been reported to have a high<br />

antitumour activity and low gastrointestinal toxicity in rats bearing murine and human tumors. We furtehr<br />

studied the possible inhibition <strong>of</strong> the toxicites caused by the products <strong>of</strong> 5-FU metabolism with the use <strong>of</strong><br />

CDHP, a new inhibitor <strong>of</strong> 5-FU degradation and Oxo, an inhibitor <strong>of</strong> 5-FU phosphorylation. In a model <strong>of</strong><br />

pentylenetetrazole-induced convulsions in mice, intravenous injection <strong>of</strong> fluoroacetate ( 3 mg/kg), 2-fluorob-alanine<br />

(30 mg/kg) and 5-FU (over 300 mg/kg) significantly augmented the occurrence <strong>of</strong> convulsion.<br />

However coadministration <strong>of</strong> an equivalent dose <strong>of</strong> CDHP with 5-FU almost completely suppressed the 5-<br />

FU-augmented convulsions, suggesting that inhibition <strong>of</strong> 5-FU catabolism by CDHP may lead to a<br />

decreased risk <strong>of</strong> development <strong>of</strong> 5-FU neurotoxicity.<br />

Kazmi, S. M., Soni, N. K., and Trivedi, V. B. (1980). Effect <strong>of</strong> some antibiotics, fungicides and metabolic<br />

inhibitors on oxidative metabolism <strong>of</strong> Rhizopus stolonifer. Trans.Mycol.Soc.Jpn. 21, 259-262.<br />

Keywords: metabolism/inhibition/fluoride/sodium fluoroacetate/fluoroacetate/fungus<br />

Abstract: Oxidative metabolism <strong>of</strong> R. stolonifer (Ehrenberg ex Fr.) Lind. [s<strong>of</strong>t root pathogen <strong>of</strong> Pyrus<br />

communis] was studied manometrically using a Warburg constant volume respirometer. The respiratory<br />

rates were directly dependent on the phase <strong>of</strong> fungal growth. Maximum QO2 [µl <strong>of</strong> O2 consumed/h . mg -1<br />

dry weight <strong>of</strong> fungal mycelium] values (26.0) were obtained at 120 h <strong>of</strong> culture age. Inhibition caused by<br />

sodium fluoride and sodium fluoroacetate suggests the occurence <strong>of</strong> an EM pathway and TCA<br />

[tricarboxylic acid] cycle in the oxidative metabolism. Sodium malonate could not produce suppression.<br />

All the tested antibiotics produced respiratory inhibition. A highly significant inhibitory effect was<br />

produced by ampicillin (calculated value <strong>of</strong> t = 11.54 significant at 0.001 probability). QO2 values were<br />

considerably suppressed by the fungicides such as sultaf, cosan, brassicol, thiram and captan.<br />

Keefe, D. L., Roistacher, N., and Pierri, M. K. (1993). Clinical cardiotoxicity <strong>of</strong> 5-fluorouracil.<br />

J.Clin.Pharmacol. 33, 1060-1070.<br />

Keywords: 5-fluorouracil/mode <strong>of</strong> action/acute toxicity/cardiac/chemistry<br />

Abstract: 5-Fluorouracil is widely known to be toxic to the hematopoietic and gastrointestinal systems. It<br />

also has cardiac toxicity, but this is perceived to be rare. During a 16-month period from January 1990<br />

through April 1991, approximately 910 patients were treated with 5-fluorouracil. Five <strong>of</strong> these developed<br />

life-threatening toxicity consistent with coronary artery spasm for an incidence <strong>of</strong> .55%. The acute events<br />

occurred on the third or fourth day <strong>of</strong> the 5-day infusion and after the fourth intravenous bolus in the patient<br />

on bolus therapy. Each <strong>of</strong> the patients had ST elevation and ventricular arrhythmias, four had acute<br />

myocardial infarction, and two had cardiac arrests. In these cases and those previously reported, cardiac<br />

toxicity is consistent with drug- or metabolite-mediated increases in coronary vasomotor tone and spasm,<br />

leading to the full spectrum <strong>of</strong> signs and symptoms <strong>of</strong> myocardial ischemia in susceptible individuals.<br />

Keller, D. A., Roe, D. C., and Lieder, P. H. (1996). Fluoroacetate-mediated toxicity <strong>of</strong> fluorinated ethanes.<br />

Fundamental and applied toxicology 30, 213-219.<br />

Keywords: mode <strong>of</strong><br />

action/NMR/metabolism/inhalation/fluoroacetate/urine/serum/citrate/heart/toxicity/rats/acute<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

toxicity/convulsions/analysis/fluorocitrate/kidney/fluoride/humans<br />

Abstract: A series <strong>of</strong> 1-(di)halo-2-fluoroethanes reported in the literature to be nontoxic or <strong>of</strong> low toxicity<br />

were found to be highly toxic by the inhalation route. Experiments were performed that showed the<br />

compounds, 1,2-difluoroethane, 1-chloro-2-fluoroethane, 1-chloro-1,2-difluoroethane, and 1-bromo-2fluoroethane<br />

to be highly toxic to rats upon inhalation for 4 hr. All four compounds had 4-hr approximate<br />

lethal concentrations <strong>of</strong> less than or equal to 100 ppm in rats. In contrast, 1,1-difluoroethane (commonly<br />

referred to as HFC-152a) has very low acute toxicity with a 4-hr LC50 <strong>of</strong> >400,000 ppm in rats. Rats<br />

exposed to the selected toxic fluoroethanes showed clinical signs <strong>of</strong> fluoroacetate toxicity (lethargy,<br />

hunched posture, convulsions). 1,2-Diffuoroethane, 1-chloro-2-fluoroethane, 1-chloro-1,2-difluoroethane,<br />

and 1-bromo-2-fluoroethane were shown to increase concentrations <strong>of</strong> citrate in serum and heart tissue, a<br />

hallmark <strong>of</strong> fluoroacetate intoxication. F-19 NMR analysis confirmed that fluoroacetate was present in the<br />

urine <strong>of</strong> rats exposed to each toxic compound. Fluorocitrate, a condensation product <strong>of</strong> fluoroacetate and<br />

oxaloacetate, was identified in the kidney <strong>of</strong> rats exposed to 1,2-difluoroethane. There was a concentrationrelated<br />

elevation <strong>of</strong> serum and heart citrate in rats exposed to 0-1000 ppm 1,2-difluoroethane. Serum citrate<br />

was increased up to 5-fold and heart citrate was increased up to Ii-fold over control citrate levels,<br />

Metabolism <strong>of</strong> 1,2-diffuoroethane by cytochrome P450 (most likely CYP2E1) is suspected because<br />

pretreatment <strong>of</strong> rats or mice with SKF-525A, disulfiram, or dimethyl sulfoxide prevented or delayed the<br />

toxicity observed in rats not pretreated. Experimental evidence indicates that the metabolism <strong>of</strong> the toxic<br />

fluoroethanes is initiated at the carbon-hydrogen bond, with metabolism to fluoroacetate via an aldehyde or<br />

an acyl fluoride. The results <strong>of</strong> these studies show that 1-(di)halo-2-fluoroethanes are highly toxic to rats<br />

and should be considered a hazard to humans unless demonstrated otherwise.<br />

Kelly, M. (1965). Isolation <strong>of</strong> bacteria able to metabolize fluoroacetate or fluoroacetamide. Nature 208,<br />

809-810.<br />

Keywords: fluoroacetate/fluoroacetamide/defluorination/metabolism/bacteria/aconitase<br />

Abstract: Fluoroacetate or fluoracetamide, after conversion to fluoroacitrate, inhibit aconitase and therefore<br />

block the tricarboxylic acid cycle; consequently these chemicals are toxic to animals and are used as<br />

pesticides. There have been at least two occasions when accidental contamination <strong>of</strong> soil and water by<br />

fluoracetamide has occurred. This communication reports the isolation <strong>of</strong> bacteria able to use these<br />

compounds for growth.<br />

Kemmerling, W. (1996). Toxicity <strong>of</strong> Palicourea marcgravii: Combined effects <strong>of</strong> fluoroacetate, Nmethyltyramine<br />

and 2-methyltetrahydro-B-carboline. Zeitschrift fur Naturforschung 51, 59-64.<br />

Keywords: occurrence in nature/mammals<br />

Abstract: Feeding experiments carried out with cattle and horses could prove the toxic effects <strong>of</strong><br />

P.marcgravii (Rubiaceae) in all cases. The typical symptoms <strong>of</strong> "sudden death", however, are observed in<br />

ruminants only. This difference could not be explained so far.<br />

Apart from fluoroacetate, two more substances also have influence the toxic effects and have been isolated<br />

from P.marcgravii for the first time: N-methyltyramine and 2-methyltetra-hydro-Beta-carboline (2-Me<br />

THBC). Structure elucidation <strong>of</strong> these compounds is mainly accomplished by H-NMR, C-NMR and MS<br />

techniques.<br />

Due to the small quantity <strong>of</strong> fluoroacetate (5.4 mug/g plant), the main toxic effect obviously lies in the two<br />

discovered substances. In contrast to the slow death <strong>of</strong> horses (monogastriers), the "sudden death<br />

syndrome" <strong>of</strong> cattle (ruminants) can be explained as a result <strong>of</strong> the higher resorbility <strong>of</strong> these two<br />

substances in the gastro-intestinal system.<br />

Given orally, both substances influence the monoamine oxidase type A (MAO-A): N-methyltyramine acts<br />

as a competitive substrate, and 2-Me THBC is one <strong>of</strong> the most effective MAO-A-inhibitors.<br />

Thus, the decomposition <strong>of</strong> the specific MAO-A-substrates noradrenaline and adrenaline as well as <strong>of</strong> Nmethyltyramine<br />

itself is inhibited. The alpha and beta receptors <strong>of</strong> the sympathetic system are stimulated<br />

more strongly, which leads to a drastic rise in blood pressure and thereby to a more rapid distribution <strong>of</strong><br />

fluoroacetate in the body. This results in a reinforced input <strong>of</strong> fluoroacetate in the cells <strong>of</strong> especially active<br />

organs <strong>of</strong> the body (heart etc.). Thus even smaller quantities <strong>of</strong> fluoroacetate are lethal.<br />

Khan, A. A., Ahmad, M., Ahmad, S, and Rizvi, S. W. (1992). Evaluation <strong>of</strong> the comparative efficacy <strong>of</strong><br />

fumigants and acute poison baits against Indian crested porcupine, Hystrix indica. Forest Ecology and<br />

Management 48, 295-303.<br />

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Appendix C<br />

Keywords: efficacy/baits/<strong>poisons</strong>/cyanide/strychnine/sodium<br />

fluoroacetate/fluoroacetate/1080/fumigant/ground control/rodents/field efficacy<br />

Abstract: Filed trials were conducted to determine the efficacy <strong>of</strong> three fumigants and two acute <strong>poisons</strong><br />

against the crested porcupine Hystrix indica, in forest plantations and croplands. the highest mortality was<br />

obtained with the use <strong>of</strong> a two ingredient gas cartridge, followed by sodium cyanide and aluminium<br />

phosphide. Strychnine baits were less effective than baits prepared from sodium fluoroacetate (1080).<br />

Further large-scale opertaional research studies are needed to develop the use <strong>of</strong> a two-ingredient gas<br />

cartridge as a single management tool against H. indica and other burrowing porcupines.<br />

Kimball, B. A. and Mishalanie, E. A. (1993). Gas chromatographic determination <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate as the free acid in an aqueous solvent. Journal <strong>of</strong> chromatography 634, 289-296.<br />

Abstract: A procedure was developed for the determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate as the free acid<br />

by capillary gas chromatography with massselective detection. Commercially available polyethylene<br />

glycol capillary columns were compatible with injections <strong>of</strong> highly acidic aqueous solutions which were<br />

required for this relatively strong acid. Using monochloroacetic acid as an internal standard, a coefficient<br />

<strong>of</strong> variation <strong>of</strong> less than 2% was routinely obtained from replicate injections <strong>of</strong> a 100 jg/ml solution <strong>of</strong><br />

sodium mon<strong>of</strong>luoroacetate in 1 M HC1. The mon<strong>of</strong>luoroacetic acid/monochloroacetic acid detector<br />

response ratio was a linear function <strong>of</strong> sodium mon<strong>of</strong>luoroacetic acid is obtained, the method <strong>of</strong>fers<br />

advantages over previously described chromatographic methods for the determination <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate. The average analyte recovery from 30 to 40 g biological samples fortified with<br />

between 2.5 and 100 mg <strong>of</strong> sodium mon<strong>of</strong>luoroacetate was 81% with relative standard deviation typically<br />

less than 7%. The instrument limit <strong>of</strong> detection was 200 pg sodium mon<strong>of</strong>luoroacetate when the detector<br />

was operated in the selected ion monitoring mode.<br />

King, D. (1982). How toxic 1080 selects its targets. Australian Natural History 20, 329-333.<br />

Keywords: 1080/mode <strong>of</strong> action/occurrence in nature/tolerance<br />

King, D. R., Oliver, A. J., and Mead, R. J. (1978). The adaptation <strong>of</strong> some Western Australian mammals to<br />

food plants containing fluoroacetate. Aust.J.Zool. 26, 699-712.<br />

Keywords: mammals/fluoroacetate/tolerance/occurrence in nature/marsupials/rodents<br />

Abstract: The tolerance to fluoroacetate <strong>of</strong> Macropus fuliginosus, Trichosurus vulpecula and Rattus<br />

fuscipes from the south-west <strong>of</strong> Western Australia is unusually high. T.vulpecula and R. fuscipes from<br />

eastern Australia are much more susceptible than conspecifics from Western Australia. This tolerance<br />

appears to be an adaptation to the presence <strong>of</strong> mon<strong>of</strong>luoroacetic acid in many species <strong>of</strong> the plant genera<br />

Gastrolobium and Oxylobium, which occur within the range <strong>of</strong> these mammals in Western Australia. The<br />

co-evolution <strong>of</strong> this defence mechanism in plants and the development <strong>of</strong> tolerance to fluoroacetate by<br />

herbivores is discussed.<br />

King, D. R., Oliver, A. J., and Mead, R. J. (1981). Bettongia and fluoroacetate: a role for 1080 in fauna<br />

management. Aust.Wildl.Res. 8, 529-536.<br />

Keywords: fluoroacetate/1080/tolerance/occurrence in nature/marsupials/mammals<br />

Abstract: The tolerance <strong>of</strong> the three species <strong>of</strong> Bettongia to fluoroacetate has been determined. B.gaimardi<br />

is comparable with most species <strong>of</strong> herbivorous mammals, B.lesueur is highly tolerant and B.penicillata<br />

has an exceptionally high tolerance. These differences reflect the past distribution <strong>of</strong> these species in<br />

relation to plants containing fluoroacetate. The relevance <strong>of</strong> these tolerance levels in the management <strong>of</strong><br />

Bettongia populations (by the control <strong>of</strong> introduced predators) is discussed. A more general role for 1080 in<br />

the conservation <strong>of</strong> threatened fauna in Western Australia is suggested.<br />

King, D. R., Twigg, L. E., and Gardner, J. L. (1989). Tolerance to sodium mon<strong>of</strong>luoroacetate in dasyurids<br />

from Western Australia. Aust.Wildl.Res. 16, 131-140.<br />

Keywords: tolerance/fluoroacetate/marsupials/1080/sodium mon<strong>of</strong>luoroacetate/acute toxicity/lethal dose<br />

Abstract: The tolerances to sodium fluoroacetate (1080) were estimated for Dasyurus ge<strong>of</strong>froii (LD 50, ca.<br />

7.5 mg 1080 kg-1), D.hallucatus (ca. 7.5 mg kg-1), Antechinus flavipes (ca. 11.0 mg kg-1) and Phascogale<br />

calura (ca. 17.5 ,g kg-1) from western Australia and comparisons were made with D.viverrinus (ca. 1.5 mg<br />

kg-1) and A.flavipes (ca. 3.5 mg kg-1) from south-eastern Australia. The species from western Australia<br />

have had evolutionary exposure to naturally occurring fluoroacetate and were more tolerant to the toxin<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

than dasyurids from south-eastern Australia. Presumably, they have acquired this tolerance through feeding<br />

on prey which had fed on plants containing fluoroacetate.<br />

King, D. R. (1989). An assessment <strong>of</strong> the hazard posed to northern quolls (Dasyurus hallucatus) by aerial<br />

baiting with 1080 to control dingoes. Australian wildlife research 16, 569-574.<br />

Keywords: aerial control/non-target species/1080/marsupials<br />

King, D. R. and Kinnear, J. E. 1080: The toxic paradox. Landscope Winter 1991, 10-14. 1991.<br />

Ref Type: Magazine Article<br />

Keywords: 1080/acute toxicity/non-target species/tolerance<br />

Abstract: Ecology is about relationships - how different things affect populations <strong>of</strong> animals, plants and<br />

otehr microorganisms, and how populations affect each other. Many thousnads <strong>of</strong> years ago, a genus <strong>of</strong><br />

leuminous plants in Western Australia learned how to make a poison commonly known as 1080 to deter<br />

seed-eating and browsing animals. In doing so, these plants have pr<strong>of</strong>undly affected the ecology <strong>of</strong> the<br />

State. Dennis King and Jack Kinnear describe how scientists' increased knowledge <strong>of</strong> the ecology <strong>of</strong> 1080<br />

can provide a means <strong>of</strong> controlling introduced species, primarily foxes, which threaten the survival <strong>of</strong> many<br />

species <strong>of</strong> our wildlife.<br />

King, D. R., Kirkpatrick, W. E., Wong, D. H., and Kinnear, J. E. (1994). Degradation <strong>of</strong> 1080 in Australian<br />

soils. In 'Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14 December 1993, Christchurch, New<br />

Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 45-49. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: persistence in soil/1080<br />

Abstract: Soils from temperature regions <strong>of</strong> Western Australia contain a diverse assemblage <strong>of</strong> bacteria and<br />

fungi which can defluorinate 1080. Rates <strong>of</strong> defluorination differed markedly with different species <strong>of</strong><br />

microorganisms, ranging from 289%. No thermophilic defluorinating microorganisms were found in soil<br />

from semiarid or arid regions. Optimal defluorination by soil baceteria occurred at netural to alkaline pH<br />

while defluorination by fungi was greatest at Ph5. Defluorination rates in soil were greatest at temperatures<br />

which fluctuated between 11 0 and 28 o C with moisture levels <strong>of</strong> 815%. Defluorination rate in soil did not<br />

seem to be closely related to inoculum size, unless 1080 was the only source <strong>of</strong> carbon.<br />

King, D. R. (1994). The sensitivity <strong>of</strong> Rattus villosissimus to 1080. Australian mammology 17, 123-124.<br />

Keywords: acute toxicity/mammals/1080<br />

King, D. R., Kirkpatrick, W. E., and McGrath, M. (1996). The tolerance <strong>of</strong> Malleefowl Leipoa ocellata to<br />

1080. EMU 96, 198-202.<br />

Keywords: tolerance/1080/birds<br />

King, J. E. and Penfound, W. T. (1946). Effects <strong>of</strong> new herbicides on fish. Science 103, 487.<br />

Keywords: aquatic species/1080/toxicity<br />

Abstract: During the course <strong>of</strong> some experiments to determine the effects <strong>of</strong> certain <strong>of</strong> the new herbicides<br />

<strong>of</strong> fish, we set up some tests, largely out <strong>of</strong> curiosity, using the new rodenticide 1080. In view <strong>of</strong> the<br />

extreme toxicity <strong>of</strong> this substance, as reported by ER Kalmach (Science 1945, 102,232) we were certainly<br />

surprised to find that fingerling bream and bass would survive in concentrations <strong>of</strong> 1080 as great as 370<br />

ppm for an indefinite period and with no apparent discomfort.<br />

Kingery, A. F. and Allen, H. E. (1994). Ion chromatographic separation and quantitative analysis <strong>of</strong><br />

fluoroacetic acid and formic acid in soil. Journal <strong>of</strong> chromatography A 671, 231-237.<br />

Keywords: ion chromatography<br />

Kirk, K. and Goldman, P. (1970). Fluorocitric acid: selective microbial degradation <strong>of</strong> the inhibitory<br />

isomer. Biochemistry Journal 117, 409-410.<br />

Keywords: fluorocitrate/mode <strong>of</strong> action/bacteria/degradation<br />

Kirms, M. A. and Kirms, L. M. (2002). The identification <strong>of</strong> sodium fluoroacetate (Compound 1080)<br />

employing NMR Spectroscopy. Journal <strong>of</strong> Forensic Sciences 47, 573-577.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: fluoroacetate/1080/NMR/sodium fluoroacetate/analysis<br />

Abstract: Nuclear magnetic resonance (NMR) spectroscopy was employed for the purpose <strong>of</strong> identifying<br />

samples <strong>of</strong> materials suspected <strong>of</strong> containing sodium fluoroacetate (Compound 1080). Acquisition <strong>of</strong><br />

routine proton (H-1) and carbon (C-13) NMR spectra provided a straight-forward means for determining<br />

the presence <strong>of</strong> Compound 1080 in the samples and thus afforded a simple method for analysis and<br />

identification <strong>of</strong> this compound<br />

Kirsten, E., Sharma, M. L., and Kun, E. (1977). Molecular toxicology <strong>of</strong> (--)-erythro-fluorocitrate: selective<br />

inhibition <strong>of</strong> citrate transport in mitochondria and the binding <strong>of</strong> fluorocitrate to mitochondrial proteins.<br />

Molecular Pharmacology 14, 172-184.<br />

Keywords: citrate/fluorocitrate/biochemistry/enzyme/metabolism/liver/kidney/heart/brain<br />

Abstract: It was concluded that (--)-erythro-fluorocitrate specifically inhibited citrate transport by its<br />

covalent binding to two proteins fractions associated with the mitoplast <strong>of</strong> liver, kidney, heart and brain<br />

tissue.<br />

Kirzon, M. V. and Artyushkova, V. A. (1967). On the relationship between the central nervous and<br />

peripheral factors in poisoning white rats with sodium fluoroacetate. Moscow University Bulletin (Vestnik<br />

Moskovskogo Universiteta) 22, 35-40.<br />

Keywords: poisoning/sodium fluoroacetate/fluoroacetate/muscle/brain/rodents/mode <strong>of</strong> action/symptoms<br />

Abstract: (Conclusions section from Russian article). 1. The character <strong>of</strong> variation <strong>of</strong> the total electricity <strong>of</strong><br />

the skeletal muscles <strong>of</strong> a rat poisoned with FA (fluoroacetate) (5 mg/kg, intraperitoneally introduced) allow<br />

subdivision <strong>of</strong> the process <strong>of</strong> poisoning into three stages: Stage 1, characterised by decrease <strong>of</strong> electrical<br />

activity (EA) to 15% <strong>of</strong> the original level; Stage 2, characterised by an increase <strong>of</strong> EA <strong>of</strong> approximately<br />

50% above the original level, and Stage 3, characterised by an irreversible decraese <strong>of</strong> EA to 5-10% <strong>of</strong> the<br />

orginal level. 2. An argument in favour <strong>of</strong> Stage 2 (characterised by a considerable increase in EA)<br />

representing a compensating, mainly heat-regulating, stimulation <strong>of</strong> brain structures due to a powerful<br />

afferentation caused by hypothermia is discussed. 3. Stage 2 coincides with the period when the loss <strong>of</strong><br />

body heat and a decrease in total oxygen intake proceed at a lower rate. A similar pattern was observed<br />

previously in rodents poisoned with FA and FA-related compounds. The authours believe that this is a<br />

consequence <strong>of</strong> compensatory stimulation <strong>of</strong> the central nervous system. 4. It is suggested that the final<br />

stage <strong>of</strong> an almost complete cessation <strong>of</strong> EA reflects a weakening <strong>of</strong> activity <strong>of</strong> the central nervous system<br />

and consequently a cessation <strong>of</strong> neurotrophical effects on the periphery.<br />

Kirzon, M. V., Timeyko, V. N., and Artyushkova, V. A. (1970). Citric acid content in various rat organs<br />

after fluoroacetate poisoning. Voprosy meditsinskoi khimii 16, 543-549.<br />

Keywords: persistence in animals/metabolism/fluoroacetate/citric<br />

acid/blood/liver/heart/muscle/brain/biochemistry/poisoning/rats/inhibition<br />

Abstract: Citric acid content in blood and organs at various time intervals after ip fluoroacetate<br />

administration was determined in albino rats. The content <strong>of</strong> citric acid in blood, heart, skeletal muscles and<br />

brain reached the maximum 0.5, 1 and 2 h (for two latter organs). In liver the increased amount <strong>of</strong> citric<br />

acid was determined to the end <strong>of</strong> the second hour only. In all organs studies except the liver the citric acid<br />

content diminished 2-3 hours after the poisoning. It was concluded that in the blood citric acid accumulates<br />

as a result <strong>of</strong> its release from organs. The liver not damaged by the gift is able to increased utilisation <strong>of</strong><br />

citric acid and then accumulates it as a result <strong>of</strong> detoxification inhibition. Two hours after poisoning the<br />

initial fall in endogenous breathing <strong>of</strong> skeletal muscles is substituted by its temporal increase. This increase<br />

coincides in time with the increased citric acid formation in muscles. It is suggested that the course <strong>of</strong> both<br />

processes may be explained by the utilization <strong>of</strong> fatty acids the mobilization <strong>of</strong> which constitutes the part <strong>of</strong><br />

compensatory processes forming in central nervous system<br />

Klingensmith, C. W. (1945). A note on the natural occurrence <strong>of</strong> fluoroacetic acid, the acid <strong>of</strong> the new<br />

rodenticide "1080". Science 102, 622-623.<br />

Keywords: occurrence in nature/fluoroacetate<br />

Kochansky, J. P., Robbins, W. E., L<strong>of</strong>gren, C. S., and Williams, D. F. (1979). Design <strong>of</strong> some delayedaction<br />

toxicants for baits to control red imported fire ants (Solenopsis invicta). Journal <strong>of</strong> economic<br />

entomology 72, 655-658.<br />

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Appendix C<br />

Keywords: baits/metabolism/toxicity/fluoroacetate/invertebrates<br />

Abstract: New candidate insecticides for Solenopsis invicta Buren were prepared which should require<br />

metabolism to the known toxicants fluoroacetic acid and trichlorfon before appreciable toxicity could be<br />

expressed. Cholesteryl fluoroacetate, sitosteryl fluoroacetate, N-dodecyl 2-fluoroacetamide and to a lesser<br />

extent, several fatty acid esters <strong>of</strong> trichlorfon gave delayed kill <strong>of</strong> imported fire ant workers. In certain<br />

cases, these compounds gave delayed kill over an increased range <strong>of</strong> concentrations compared to the<br />

underivatized toxicants<br />

Koenig, H. (1969). Acute axonal dystrophy caused by fluorocitrate: the role <strong>of</strong> mitochondrial swellingq.<br />

Science 164, 310-312.<br />

Keywords: fluorocitrate/Krebs cycle/mode <strong>of</strong> action/pathology<br />

Abstract: Fluorocitrate, a Krebs cycle inhibitor, induces neurons to rapidly expel multitudinous lysosomes,<br />

mitochondria and other cytoplasmic constituents into their axons. After convulsive seizures commence,<br />

spectacular axonal balloons develop owing to obstruction <strong>of</strong> axonal flow by "log jams' <strong>of</strong> extruded<br />

organelles. A swelling <strong>of</strong> neuronal mitochondria is apparently responsible for the disgorgement <strong>of</strong><br />

cytoplasmic material into axons.<br />

Koenig, W. D. and Reynolds, M. D. (1987). Potential poisoning <strong>of</strong> yellow-billed magpies by compound<br />

1080. Wildlife Society bulletin 15, 274-276.<br />

Keywords: poisoning/1080/baits/birds/persistence in animals/non-target species<br />

Abstract: The use <strong>of</strong> 1080 baits for rodent control can apparently lead to mortality <strong>of</strong> yellow-billed<br />

magpies. Birds die in the nest making recovery <strong>of</strong> the bodies unlikely.<br />

Kohn, G. D. (1956). Compound 1080 - Its use as a rabbit poison in Victoria. The Journal <strong>of</strong> Agriculture<br />

(Victoria) 279-283.<br />

Keywords: 1080/poison<br />

Kononen, D. W., Hochstein, J. R., and Ringer, R. K. (1991). Mallard and northern bobwhite exposure to<br />

compound 1080 : acute toxicity and food avoidance behavior. Chemosphere 22, 655-663.<br />

Keywords: acute toxicity/birds/non-target species/1080/toxicity/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/lethal concentration<br />

Abstract: Standard 8-day toxicity experiments were conducted with mallards (Anas platyrhynchos) and<br />

northern bobwhite (Colinus virginianus) exposed to a range <strong>of</strong> dietet sodium mon<strong>of</strong>luoroacetate<br />

(Compound 1080) concentrations. Food LC50 estimates for mallards and northern bobwhite were 527 and<br />

385 ppm respectively. Food avoidance tests in which birds were given free choice between equal amounts<br />

<strong>of</strong> clean and contaminated food inidcated that mallards and northern bobwhite avoided consumption <strong>of</strong><br />

1080-treated food at levels equal to or greater than 236 ppm and 95 ppm respectively. Although water<br />

LC50 estimates for both species were approximately an order <strong>of</strong> magnitude less than those estimated from<br />

the food LC50 experiments, these differences could be largely attributed to the fact than, on a w/w basis,<br />

both species utilize from 5 to 10 times as much water as food. Water avoidance tests showed that mallards<br />

avoided consumption <strong>of</strong> 1080-contaminted water at concentrations between 13 and 24 ppm. Bobwhite<br />

avoided consumption <strong>of</strong> 1080-contaminated water at concentrations greater than 9 ppm.<br />

Korn, T. J. and Livanos, G. (1986). The effect <strong>of</strong> dosing technique on the 1080 content <strong>of</strong> meat baits.<br />

Australian wildlife research 13, 455-459.<br />

Keywords: ground control/bait degradation/field efficacy/1080/baits/predators/dogs<br />

Korn, T. J. and O'Brien, P. H. A review <strong>of</strong> vertebrate pest control using 1080 in Australia. Bureau <strong>of</strong> Rural<br />

Resources, Department <strong>of</strong> Primary Industries and Energy. 1-76. 1989.<br />

Ref Type: Report<br />

Keywords: 1080<br />

Korth, M., Weger, N., and Reiter, M. (1978). The positive inotropic effect <strong>of</strong> sodium fluoroacetate on<br />

guniea-pig ventricular myocardium. Nauynn-Schmeideberg's Arch Pharmacol 303 , 7-14.<br />

Keywords: sodium fluoroacetate/fluoroacetate/heart/mammals/muscle/mode <strong>of</strong> action<br />

Abstract: In the isolated papillary muscle <strong>of</strong> the guinea-pig sodium fluoroacetate (Fac) produced, after an<br />

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Appendix C<br />

initial decrease in the force <strong>of</strong> concentration, a transient positive inotropic effect which was due to an<br />

increase in the rate <strong>of</strong> force development. Time to peak force was shortened and relaxation time was<br />

prolonged whereas total contraction time was barely affected. Threshold and maximally effective<br />

concentration for the positive intropic effect were 1 x 10 -5 and 5 x 10 -3 M, respectively<br />

Kostyniak, P. J., Bosmann, H. B., and Smith, F. A. (1978). Defluorination <strong>of</strong> fluoroacetate in vitro by rat<br />

liver subcellular fractions. Toxicology and Applied Pharmacology 44, 89-97.<br />

Keywords: metabolism/defluorination/fluoroacetate/liver/fluoride/bone/rats<br />

Abstract: An earlier report showing enhanced accumulation <strong>of</strong> ionic fluoride in bones <strong>of</strong> rats given<br />

fluoroacetate (FAc) suggested an in vivo defluorination <strong>of</strong> fluoroacetate. Rat liver an organ which shows<br />

minimal pathological and biochemical effects in FAc intoxication was found to possess defluorination<br />

activityin vitro. Subcellular fractionation <strong>of</strong> livers from male Sprague-Dawley rats was performed in 0.25<br />

M sucrose and yielded the following fractions: whole homogenate, nuclear, mitochondrial, microsomal and<br />

105,000 g supernatant. Defluorination activity was measured by incubating subcellular fractions and their<br />

boiled controls with FAc (1 hr. 37ºC. pH 7.4, in 0.1 M tris-HCl or 0.1% Triton X-100) and comparing the<br />

difference in ionic fluoride content at the end <strong>of</strong> the incubation. Defluorination activity based on protein<br />

content was consistently the highest in the 105,000 g supernatant fraction, the only fraction showing an<br />

activity increase over the original homogenate. The microsomal fraction had minimal activity.<br />

Defluorination activity in the 105,000 g supernatant as a function <strong>of</strong> time after fraction isolation at 4ºC<br />

revealed a time-dependent reduction in activity. After 24 hr at 4ºC, activity was almost completely lost.<br />

The time-dependent loss <strong>of</strong> activity at 4ºC could be regained when glutathione (GSH) was added to this<br />

fraction at a final concentration <strong>of</strong> 5 mM. Furthermore, GSH significantly increased the defluorination<br />

activity in all subcellular fractions. A study <strong>of</strong> the optimum pH for defluorination activity in the 105,000 g<br />

supernatant fraction was performed in 0.1 M Tris-maleate buffer. Surprisingly, a complete loss <strong>of</strong> activity<br />

with this buffer resulted throughout the pH range studied (pH 5.6-8.0). Furthermore, defluorination activity<br />

<strong>of</strong> all subcellular rat liver fractions was completely inhibited by maleate and stimulated by glutathione.<br />

These results are consistent with the involvement <strong>of</strong> a sulfhydryl group in the defluorination <strong>of</strong> FAc in rat<br />

liver.<br />

Kostyniak, P. J. (1979). Defluorination : a possible mechanism <strong>of</strong> detoxification in rats exposed to<br />

fluoroacetate. Toxicology letters 3, 225-228.<br />

Keywords: metabolism/persistence in animals/defluorination/rats/fluoroacetate<br />

Kostyniak, P. J. and Soiefer, A. I. (1984). The role <strong>of</strong> fluoroacetate-specific deholgenase and glutathione<br />

transferase in the metabolsim <strong>of</strong> fluoroacetamide and 2,4-dinitr<strong>of</strong>luorobenzene. Toxicology letters 22, 217-<br />

222.<br />

Keywords: fluoroacetamide/fluoroacetate/enzyme/biochemistry<br />

Abstract: 2,4-dinitr<strong>of</strong>luorobenzene (DNFB) reacts with glutathione to form a stable product similar to that<br />

formed with the model glutathione-S-transferase (GST) substrate, 1-chloro-2,4-dinitrobenzene (CDNB).<br />

DNFB is approx. 40 times as reactive as CDNB in this chemical reaction. The enzymatic defluorination <strong>of</strong><br />

DNFB also proceeds at a more rapid rate that that <strong>of</strong> CDNB in the GST assay. Fluoroacetamide (FAM) like<br />

fluoroacetate (FAC) undergoes no discernable chemical defluorination. Its enzymatic defluorination is<br />

approx. 10% <strong>of</strong> that observed for FAC and only 0.2% <strong>of</strong> the rate for DFNB. An antibody raised tot he the<br />

fluoroacetate specific dehalogenase (FSD) precipitated both FAC and FAM defluorinating activity but had<br />

no effect on either CDNB or DFNB activity. The data are consistent with the hypothesis that DNFB is<br />

metabolised by the GST while FAM is metabolised by the FSD.<br />

Kozlov, M. P., Savel' ev, V. N., Chumakova, I. V., Taran, I. F., and Dyatlov, A. I. The outlook for the<br />

development <strong>of</strong> biological methods <strong>of</strong> control for fleas <strong>of</strong> rodents. g, 150-152. 1974.<br />

Ref Type: Conference Proceeding<br />

Keywords: rodents/<strong>poisons</strong>/poison/fluoroacetate/rats/mammals/invertebrates<br />

Abstract: In view <strong>of</strong> the ecological disadvantages <strong>of</strong> using wide-spectrum insecticides such as DDT, there is<br />

need for a method <strong>of</strong> biological control. The prospects for developing a system along these lines are<br />

discussed. It has been found in the laboratory that Entobakterin (a proprietary preparation <strong>of</strong> Bacillus<br />

thuringiensis) can cause high mortality in fleas in 7-9 days, depending on the dosage used, and is also<br />

pathogenic to the larvae. The outlook for the use <strong>of</strong> sterilisants such as thiotepa (tiotef) is considered. Some<br />

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rat <strong>poisons</strong> (fenitrothion (Sumithion) and barium fluoroacetate) at dosages <strong>of</strong> 0.12-0.45 mg/kg body weight<br />

can sterilise fleas on the rats. At the same time, it has been shown that carbaryl (Sevin) similarly used in<br />

doses sublethal to rodents stimulates reproduction in fleas on the rodents. The intensification <strong>of</strong> the<br />

pathogenic effect <strong>of</strong> B. thuringiensis on Coleoptera by its use in combination with trichlorphon (chlor<strong>of</strong>os),<br />

DDT, gamma -BHC and other insecticides suggests the possibility <strong>of</strong> elaborating an integrated method <strong>of</strong><br />

control for fleas using B. thuringiensis together with insecticides at dosages too low to be harmful to<br />

mammals<br />

Kramer, H. L. (1984). Liquid chromatographic determination <strong>of</strong> sodium fluoroacetate (Compound 1080) in<br />

meat baits and formulations. Journal <strong>of</strong> the Association <strong>of</strong> Official Analytical Chemists 67, 1058-1061.<br />

Keywords: liquid chromatography/sodium fluoroacetate/1080<br />

Abstract: A liquid chromatographic (LC) method is described for the determination <strong>of</strong> sodium fluoroacetate<br />

in meat baits and formulations. Baits were extracted with water, ultrafiltered, partitioned into butanone,<br />

back-partitioned into dilute base, and diluted with acetonitrile. Aqueous formulations <strong>of</strong> 1080 were diluted<br />

with acetonitrile. The solutions were esterfied with p-bromophenacyl bromide, using crown either<br />

catalysis, and chromatographed on a 10 p.m reverse phase column. Ultraviolet absorbance was monitored<br />

at 260 nm. Samples spiked to contain 1 mg and 10 mg 1080/100 g meat gave recoveries <strong>of</strong> 84.0 - 103.4%<br />

Kramer, H. L., Merrell, P. W., and Burren, B. J. (1987). Use <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound<br />

1080) in the control <strong>of</strong> dingoes I. Meat bait preparation techniques. Australian wildlife research 14, 65-68.<br />

Keywords: ground control/bait degradation/field efficacy/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/predators/dogs<br />

Krebs, H. A. (1970). The history <strong>of</strong> the tricarboxylic acid cycle. Perspectives in Blood and Medicine 14,<br />

154-170.<br />

Keywords: metabolism/enzyme/biochemistry<br />

Krebs, H. C., Kemmerling, W., and Habermehl, G. (1994). Qualitative and quantitative determination <strong>of</strong><br />

fluoroacetic acid in Arrabidea bilabiata and Palicourea marcgravii by 19F-NMR spectroscopy. Toxicon<br />

Oxford 32, 909-913.<br />

Keywords: analysis/fluoroacetate/occurrence in nature<br />

Abstract: A. bilabiata [Arrabidaea bilabiata] and P. marcgravii are poisonous plants (endemic to the<br />

Amazonian area) which cause 'sudden death' in grazing animals. A new method involving 19F-NMR<br />

spectroscopy, which can detect amounts <strong>of</strong> fluoroacetic acid (a toxic principle from P. marcgravii) at<br />

contents below 4 µg/g, is described. Fluoroacetic acid was quantified in the leaves <strong>of</strong> A. bilabiata and P.<br />

marcgravii (3.0 and 5.4 µg/g, respectively), and in the seeds <strong>of</strong> A. bilabiata (64.1 µg/g)<br />

Krenzelok, E. and Vale, A. (1997). Position statements: gut decontamination. Clinical Toxicology 35, 695-<br />

697.<br />

Keywords: poisoning/treatment<br />

Kun, E. (1982). Mon<strong>of</strong>luoroacetic acid (compound 1080), its pharmacology and toxicology. Proceedings <strong>of</strong><br />

the Vertebrate Pest Conference 10, 34-40.<br />

Keywords: mode <strong>of</strong> action/metabolism/1080<br />

Kurihara, T., Esaki, N., and Soda, K. (2000). Bacterial 2-haloacid dehalogenases: structures and reaction<br />

mechanisms. Journal <strong>of</strong> molecular catalysis B - Enzymatic 10, 57-65.<br />

Keywords: metabolism<br />

Kurihara, T., Yamauchi, T., Ichiyama, S., Takahata, H., and Esaki, N. (2003). Purification, characterization,<br />

and gene cloning <strong>of</strong> a novel fluoroacetate dehalogenase from Burkholderia sp FA1. Journal <strong>of</strong> Moleclar<br />

Catalysis B-Enzymatic 23, 347-355.<br />

Keywords: fluoroacetate/defluorination/enzyme/residues/bacteria<br />

Abstract: Fluoroacetate dehalogenase catalyzes the hydrolytic defluorination <strong>of</strong> fluoroacetate to produce<br />

glycolate. The enzyme is unique in that it catalyzes the cleavage <strong>of</strong> the highly stable carbon-fluorine bond<br />

in an aliphatic compound. The bacterial isolate FA1, which was identified as Burkholderia, grew on<br />

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Appendix C<br />

fluoroacetate as the sole carbon source to produce fluoroacetate dehalogenase (FAc-DEX FA1). The<br />

enzyme was purified to homogeneity and characterized. The molecular weights were estimated to be<br />

79,000 and 34,000 by gel filtration and SDS-polyacrylamide gel electrophoresis (PAGE), respectively,<br />

suggesting that the enzyme is a dimer. The purified enzyme was specific to haloacetates, and fluoroacetate<br />

was the best substrate. The activities toward chloroacetate and bromoacetate were less than 5% <strong>of</strong> the<br />

activity toward fluoroacetate. The K-m and V-max values for the hydrolysis <strong>of</strong> fluoroacetate were 5.1 mM<br />

and 11 mumol per minute milligram, respectively. The gene coding for the enzyme was isolated, and the<br />

nucleotide sequence was determined. The open reading frame consisted <strong>of</strong> 912 nucleotides, corresponding<br />

to 304 amino acid residues. Although FAc-DEX FA1 showed high sequence similarity to fluoroacetate<br />

dehalogenase from Moraxella sp. B (FAc-DEX H1) (61% identity), the substrate specificity <strong>of</strong> FAc-DEX<br />

FA1 was significantly different from that <strong>of</strong> FAc-DEX H1: FAc-DEX FA1 was more specific to<br />

fluoroacetate than FAc-DEX H1.<br />

LaGoy, P. K., Bohrer, R. L., and Halvorsen, F. H. (1992). The development <strong>of</strong> cleanup criteria for an<br />

acutely toxic pesticide at a contaminated industrial facility. American Industrial Hygiene Association<br />

journal 53, 298-302.<br />

Keywords: occupational exposure/dermal/inhalation/humans/regulatory toxicology/reproductive<br />

effects/sodium fluoroacetate/fluoroacetate/rats/soil/analysis<br />

Abstract: Sodium fluoroacetate, a restricted-use rodenticide, was improperly applied to kill rats in a South<br />

American steel mill. As a result <strong>of</strong> this application, several workers were seriously injured. During plant<br />

decontamination, cleanup levels were developed to prevent significant exposure <strong>of</strong> workers, who could<br />

inhale contaminate dust, contact dust or soil dust in outdoor areas or on plant floors and who could contact<br />

contaminated surfaces. On the basis <strong>of</strong> a health risk analysis, the following cleanup levels for sodium<br />

fluoroacetate were developed - air cleanup levels 0.05 mg/m3, soil/dust cleanup levels 100 mg/kg and wipe<br />

sample cleanup levels 0.2 mg/100 cm3. These risk-based cleanup levels were ultimately used to assist the<br />

regulatory agencies in reaching a decision to reopen the plant.<br />

Lahiri, S. and Quastel, J. H. (1963). Fluoroacetate and the metabolism <strong>of</strong> ammonia in the brain.<br />

Biochemical journal 89, 157-163.<br />

Keywords: fluoroacetate/metabolism/brain/sodium fluoroacetate<br />

Abstract: 1. Sodium fluoroacetate, at concentartions <strong>of</strong> 1 mM or less, which have no effect on the<br />

respiration <strong>of</strong> rat-brain-cortex slices incubated in Krebs-Ringer phosphate medium containing glucose,<br />

suppresses the formation <strong>of</strong> 14 C-labelled glutamine from [ 14 C6]glucose, the effect being greater in a medium<br />

containing 105 m-eqiv. <strong>of</strong> K + ions/l. than in one containing 5 m-eqiv. <strong>of</strong> K + ions/l. There is a concomitant<br />

increase in the amount <strong>of</strong> 14 C-labelled glutamate formed. 2. Sodium fluoroacetate (1 mM) suppresses the<br />

accelerating action <strong>of</strong> NH4 + ions on the rates <strong>of</strong> oxygen consumption and <strong>of</strong> the formation <strong>of</strong> 14 C-labelled<br />

glutamine from [ 14 C6]glucose by the brain cortex slices.3. Sodium fluoroacetate (1 mM) increases the<br />

amount <strong>of</strong> free ammonia in the barin-cortex slices after incubation in the presence <strong>of</strong> glucose for 1 hr at 37<br />

degrees.4. The yields <strong>of</strong> 14C-labelled glutamine and 14C-labelled aspartate derived from [14C5]glutamate<br />

by rat-brain-cortex slices, incubated in Krebs-Ringer phosphate medium containing glucose, are diminished<br />

in the presence <strong>of</strong> sodium fluoroacetate (1 mM). 5. The addition <strong>of</strong> Amytal (0.5 mM) diminishes the<br />

enhanced rate <strong>of</strong> formation <strong>of</strong> 14C-labelled glutamate from 14C6glucose due to 1 mM sodium fluoroacetate<br />

6. The results are consistent with the conclusion that sodium fluoroacetate, at 1 mM or less, inhibits the<br />

utilization <strong>of</strong> NH4+ ions by rat-brain-cortex slices.<br />

Laine, K., Kivisto, K. T., and Neuvonen, P. J. (1992). Failure <strong>of</strong> oral activated charcoal to accelerate the<br />

elimination <strong>of</strong> amiodarone and chloroquine. Human & Experimental Toxicology 11, 491-494.<br />

Keywords: poisoning/treatment/antidote/rats<br />

Abstract: 1. The effect <strong>of</strong> activated charcoal on the elimination <strong>of</strong> amiodarone and chloroquine was studied<br />

in the rat.<br />

2. The study consisted <strong>of</strong> two separate experiments. Amiodarone and chloroquine were injected<br />

subcutaneously at doses <strong>of</strong> 200 mg kg-1 and 100 mg kg-1, respectively. Six rats in both experiments were<br />

put on a charcoal-containing diet 48hr after drug administraion, while the control groups remained on a<br />

normal diet.<br />

3. Treatment with repeated oral activated charcoal had no effect on the true elimination <strong>of</strong> amiodarone and<br />

chloroquine.<br />

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4. These results suggest that, after the distribution <strong>of</strong> amiodarone and chloroquine into peripheral<br />

compartments, their rate <strong>of</strong> elimination cannot be significantly accelerated with multiple oral doses <strong>of</strong><br />

activated charcoal.<br />

Largo, C., Cuevas, P., Somjen, G. G., Martin del Rio, R., and Herreras, O. (1996). The effect <strong>of</strong> depressing<br />

glial function in rat brain in situ on ion homeostasis, synaptic transmission, and neuron survival. The<br />

Journal <strong>of</strong> Neuroscience 16, 1219-1229.<br />

Keywords: brain<br />

Largo, C., Ibarz, J. M., and Herreras, O. (1997). Effects <strong>of</strong> the gliotoxin fluorocitrate on spreading<br />

depression and glial membrane potential in rat brain in situ. Journal <strong>of</strong> neurophysiology 78, 295-307.<br />

Keywords: mode <strong>of</strong> action/treatment<br />

Largo, C., Tombaugh, G. C., Aitken, P. G., Herreras, O., and Somjen, G. G. (1997). Heptanol but not<br />

fluoroacetate prevents the propagation <strong>of</strong> spreading depression in rat hippocampal slices. Journal <strong>of</strong><br />

neurophysiology 77, 9-16.<br />

Keywords: mode <strong>of</strong> action/metabolism<br />

Larner, J. (1950). Toxicological and metabolic effects <strong>of</strong> fluorine-containing compounds. Industrial<br />

medicine and surgery 19, 535-539.<br />

Keywords: fluorine/fluoride/metabolism/acute toxicity/chronic poisoning/mode <strong>of</strong> action<br />

Abstract: The various aspects <strong>of</strong> the problem <strong>of</strong> fluoride toxicity have been discussed. The ubiquitous<br />

distribution <strong>of</strong> this element has been pointed out. The acute and chronic toxicity and the important<br />

mechanisms <strong>of</strong> this toxicity are reviewed. Since it is even yet incomplete, more investigation will have to<br />

be carried out in order to complete the picture <strong>of</strong> this important present-day problem.<br />

Latge, J. P. (1980). Sporulation <strong>of</strong> Entomophthora obscura Hall & Dunn in liquid culture. Canadian<br />

Journal <strong>of</strong> Microbiology 26, 1038-1048.<br />

Keywords: fungus/sodium fluoroacetate/fluoroacetate<br />

Abstract: In connection with the possible development <strong>of</strong> the fungus for the biological control <strong>of</strong> aphids,<br />

growth and production <strong>of</strong> azygospores <strong>of</strong> Entomophthora obscura were studied through batch cultures in<br />

media containing glucose, or vegetable oil, and yeast extract in the laboratory in Paris. In media containing<br />

3% glucose and 1% yeast extract, an 8-h lag phase occurred and sporulation began only at the 40th hour <strong>of</strong><br />

culture; spore maturation lasted 4 days on average. Young mycelial stages were characterised by high<br />

nucleic acid and protein but low lipid concentrations. During sporogenesis, the quantity <strong>of</strong> lipids and chitin<br />

increased and the concentration <strong>of</strong> the total polyosides (chitin excluded) was lower in comparison with the<br />

mycelial stages. Sporulation was induced by means <strong>of</strong> medium starvation in carbon and/or nitrogen. The<br />

only sporulation inhibitor that allowed considerable growth was sodium fluoroacetate<br />

Lauble, H., Kennedy, M. C., Emptage, M. H., Beinert, H., and Stout, C. D. (1996). The reaction <strong>of</strong><br />

fluorocitrate with aconitase and the crystal structure <strong>of</strong> the enzyme-inhibitor complex. Proceedings <strong>of</strong> the<br />

National Academy <strong>of</strong> Sciences <strong>of</strong> the United States <strong>of</strong> America 93, 13699-13703.<br />

Keywords: mode <strong>of</strong> action<br />

Lazarus, M. (1956). The toxicity and relative acceptability <strong>of</strong> some <strong>poisons</strong> to the wild rabbit, Oryctolagus<br />

cuniculus (L.). CSIRO wildlife research 1, 96-100.<br />

Keywords: <strong>poisons</strong>/poisoning/rabbits/fluoroacetate/1080/strychnine/field efficacy/target species<br />

Abstract: Laboratory tests <strong>of</strong> nine substances already in use or considered suitable for poisoning wild<br />

rabbits, Oryctolagus cuniculus, showed that only sodium fluoroacetate (1080) seems to have any<br />

considerable advantage over strychnine and phosphorus.<br />

Le Couteur, D. G., McLean, A. J., Taylor, M. C., Woodham, B. L., and Board, P. G. (1999). Pesticides and<br />

Parkinson's disease. Biomedicine and Pharmacotherapy 53, 122-130.<br />

Keywords: metabolism/1080/sublethal effects/brain/mode <strong>of</strong> action/humans<br />

Abstract: Epidemiological studies and case reports provide evidence for an association between Parkinson's<br />

disease and past exposure to pesticides. Susceptibility to the effects <strong>of</strong> pesticides and other putative<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

neurotoxins depends on variability in xenobiotic metabolism possibly generated by genetic polymorphisms,<br />

aging and variation in exposure to environmental agents including pesticides. The simplest mechanistic<br />

hypothesis for the association <strong>of</strong> pesticides with Parkinson's disease is that pesticides or their metabolites<br />

are directly toxic to mitochondria, although modulation <strong>of</strong> xenobiotic metabolism by pesticides provides an<br />

adjunct or alternative hypothesis.<br />

le Mar, K. and McArthur, C. (2000). Relocating radio-collared targeted marsupials after a 1080 poisoning<br />

operation. Tasforests 12, 155-160.<br />

Keywords: marsupials/1080/poisoning/possums/efficacy<br />

Abstract: The fate <strong>of</strong> 26 radiocollared individuals from three targeted marsupial species were followed<br />

during a 1080 poisoning operation on a eucalypt plantation, to investigate where animals die in relation to<br />

the bait-line. Fifteen <strong>of</strong> the 26 animals died during the poisoning operation; eight <strong>of</strong> ten Tasmanian<br />

pademelons (Thylogale billardierii ), one <strong>of</strong> seven Bennett's wallabies (Macropus rufogriseus rufogriseus)<br />

and six <strong>of</strong> nine brushtail possums (Trichosurus vulpecula). The proportions <strong>of</strong> radio-collared animals that<br />

died within each species did not reflect kill rates calculated from more reliable absolute density data.<br />

Radio-collared carcasses were found between 8 m and 83 m from the bait-line (mean distance 31 m).<br />

Seventy-five per cent <strong>of</strong> carcasses were found inside shelters (i.e. inside windrows, hollow logs, dens or<br />

under fallen vegetation). Twelve <strong>of</strong> the 15 poisoned radio-collared carcasses were found intact. Three<br />

carcasses were not found but recovered collars showed carnivore's teeth marks, suggesting that Tasmanian<br />

devils (Sarcophilus harrisii) or spotted-tailed quolls (Dasyurus maculatus) had moved and/or consumed<br />

them.<br />

le Mar, K. and McArthur, C. (2001). Changes in marsupial herbivore densities in relation to a forestry<br />

1080-poisoning operation. Australian Forestry 64, 175-180.<br />

Keywords: poisoning/non-target species<br />

Abstract: Line transect surveys were used to monitor species densities before and after poisoning.<br />

Targetted species: red-bellied pademelon (Thylogale billardierii); the red-necked wallaby (Macropus<br />

rufogriseus subspecies M. r. rufogriseus), the common brushtail possum (Trichosurus vulpecula) and<br />

European rabbit (Oryctolagus cuniculus). One non-target species, the common wombat (Vombatus<br />

ursinus), was also monitored. Good kill <strong>of</strong> pademelon but speculates red-necks come into vacated habitat.<br />

No sig. effects detected with wombats, possums and rabbits.<br />

Lechat, P. (1978). Metabolic changes which modify the biological effects <strong>of</strong> nutrients and toxins. World<br />

Review <strong>of</strong> Nutrition and Dietetics 29Transformations metaboliques qui conditionnent les effets<br />

biologiques des nutriments et des toxiques. Using Smart <strong>Source</strong> Parsing 21 ref, 77-95.<br />

Keywords: metabolism/fluoroacetate/biochemistry<br />

Abstract: Chemical or biological changes occurring in the body, which transform foreign substances to<br />

metabolites with nutritional, pharmacological or toxic effects are discussed. Examples include the<br />

conversion <strong>of</strong> beta -carotene to vitamin A and <strong>of</strong> organ<strong>of</strong>luorides to the toxic fluoroacetic acid. Organisms<br />

may transform the different stereoisomers <strong>of</strong> a substance in different ways<br />

Lemaire, L., Malet-Martino, M., Martino, R., de Forni, M., and Lasserre, B. (1994). The Tris formulation<br />

<strong>of</strong> fluorouracil is more cardiotoxic than the sodium salt formulations. Oncology Reports 1, 173-174.<br />

Keywords: metabolism/fluoroacetate/humans/excretion<br />

Abstract: The cardiotoxicity <strong>of</strong> 5-fluorouracil (FU) was attributed to degradation compounds present in the<br />

injected vials, fluoroacetaldehyde (Facet) and fluoromalonaldehydic acid (FMald). FU-NaOH vials were<br />

much less cardiotoxic than FU-Tris vials on the isolated perfused rabbit heart model since Facet and FMald<br />

are stored in stable depot forms in FU-Tris vials whereas, in FU-NaOH vials, they are extensively<br />

transformed. Cardiotoxic fluoroacetate (FAC), coming from Facet metabolization, was found in urine <strong>of</strong><br />

patients, who with a ratio FAC/FU catabolites 10-30 fold lower in patients treated with FU-NaOH than in<br />

those than in those treated with FU-Tris.<br />

Lemaire, L., Arellano, M., Malet-Martino, M., and Martino, R. (1996). 1225. A novel metabolite <strong>of</strong> 5fluorouracil<br />

in humans: 2-fluoro-3-hydroxypropionic acid. Proceedings <strong>of</strong> the American Association for<br />

Cancer <strong>Research</strong> 37, 179.<br />

Keywords: 5-fluorouracil/humans/metabolism/fluoroacetate<br />

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Abstract: We previously demonstrated that pure 5-fluorouracil (FU) was metabolized, via its major<br />

catabolite α-fluoro-β-alanine, into highly cardiotoxic compounds, 2-fluoro-3-hydroxypropionic acid<br />

(FHPA) and fluoroacetate (FAC), in rats (Proc AACR 36: A2415, 1995). Does this metabolic pathway<br />

occur in humans? Fluorine-19 nuclear magnetic resonance analysis <strong>of</strong> urine samples from two patients (Y,<br />

Z) treated with continuous IV infusion <strong>of</strong> FU (1 g/m 2 /d over 4 days) revealed the presence <strong>of</strong> FHPA and<br />

FAC. However, these compounds could also arise from respective metabolism <strong>of</strong> fluoromalonic acid semialdehyde<br />

(FMASA1d) and fluoroacetalaldehyde (Facet) which are degradation compounds <strong>of</strong> FU present in<br />

the solutions injected to patients. Since 10.5 (Y) and 4.9 (Z) µmoles <strong>of</strong> Facet were injected with FU, the<br />

amounts <strong>of</strong> FAC detected in urine over 5 days (2.8 (Y) and 1.3 (Z) µmoles) did not permit to conclude to a<br />

metabolism <strong>of</strong> FU itself into FAC. On the other hand, the large amounts <strong>of</strong> FHPA in urine (810 (Y) and<br />

340 (Z) µmoles over 5 days) comparatively to those <strong>of</strong> FMASA1d injected to patients (9.9 (Y) and 7.4 (Z)<br />

µmoles) suggests that FU itself is metabolized to FHPA in humans. This study constitutes an indirect pro<strong>of</strong><br />

<strong>of</strong> this metabolic pathway. The direct pro<strong>of</strong> will only be obtained when solutions <strong>of</strong> FU free <strong>of</strong> degredation<br />

compounds (a lyophilisate form for example) will be commercially available.<br />

Lemieux, G., Baverel, G., Vinay, P, and Gougoux, A. (1979). Effect <strong>of</strong> fluoroacetate on the inhibitory<br />

action <strong>of</strong> ketone bodies and fatty acids on renal ammoniagenesis. American journal <strong>of</strong> physiology 237, F7-<br />

F13.<br />

Keywords: fluoroacetate/enzyme/aconitase/citrate/Krebs cycle<br />

Abstract: The present studies demonstrate that ketone bodies and fatty acids inhibit renal ammoniagenesis<br />

and gluconeogensis in vitro through their oxidation in the mitochondria. They also suggest that direct<br />

transamination <strong>of</strong> glutamine into alanine may be significant when oxidation <strong>of</strong> pyruvate is inhibited by<br />

fluoroacetate.<br />

Liang, C. S. (1977). Metabolic control <strong>of</strong> circulation. Effects <strong>of</strong> iodoacetate and fluoroacetate. J.Clin.Invest.<br />

60, 61-69.<br />

Keywords: fluoroacetate/inhibition/dogs/blood/resistance/cardiac<br />

Abstract: The circulatory effects <strong>of</strong> selective metabolic inhibition <strong>of</strong> glycolysis and <strong>of</strong> the tricarboxylic acid<br />

cycle by iodoacetate and fluoroacetate were studied in intact chloralose-anesthetized dogs. Pulmonary<br />

arterial blood pressure and vascular resistance increased after administration <strong>of</strong> both inhibitors, but neither<br />

systemic hemodynamics nor myocardial contractility changed significantly. Coronary blood flow did not<br />

change after iodoacetate administration but increased four- to five-fold after fluoroacetate. Administration<br />

<strong>of</strong> normal saline had no effect on any <strong>of</strong> the parameters. The changes in pulmonary arterial blood pressure<br />

and coronary blood flow after fluoroacetate were not mediated via the autonomic nerves or adrenergic<br />

neurohumors because they still occurred after autonomic nervous system inhibition. Neither myocardial<br />

oxygen consumption nor left ventricular work changed. A selective increase in myocardial blood flow also<br />

occurred in conscious dogs after fluoroacetate administration; hepatic artery flow was reduced, but other<br />

organ flows did not change significantly. These results indicate that pulmonary pressor and coronary dilator<br />

effects may be produced in intact dogs by selective metabolic blockade, in the absence <strong>of</strong> reduced oxygen<br />

supply or impairment in the electron transport system. These results also suggest that the increases in<br />

pulmonary arterial blood pressure, coronary blood flow, and cardiac output that occur during hypoxia<br />

probably are related to separate metabolic events in the tissue<br />

Liebecq, C. (1989). Commentary on 'The Toxicity <strong>of</strong> Fluoroacetate and the Tricarboxylic Acid Cycle'.<br />

Biochim Biophys Acta 1000, 251-253.<br />

Keywords: toxicity/fluoroacetate<br />

Liebecq, C. and Peters, R. A. (1989). The toxicity <strong>of</strong> fluoroacetate and the tricarboxylic acid cycle. Biochim<br />

Biophys Acta 1000, 254-269.<br />

Keywords: toxicity/fluoroacetate<br />

Lindenbaum, A., White, M. A., and Schubert, J. (1951). Citrate formation in vivo induced by non-lethal<br />

doses <strong>of</strong> fluoroacetate. Journal <strong>of</strong> biological chemistry 190, 585-593.<br />

Keywords: mode <strong>of</strong> action/citrate/fluoroacetate<br />

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Lisella, F. S., Long, K. R., and Scott, H. G. (1970). Toxicology <strong>of</strong> rodenticides and their relation to human<br />

health. J.E.H. 33, 231-237.<br />

Keywords: poisoning/1080/residues/poison/humans<br />

Abstract: (from text) In man the action on the central nervous system produces epilepti-form convulsive<br />

seizures followed by severe depression. Twenty-two cases <strong>of</strong> poisoning by this material, with 12 deaths<br />

have been reported. In another instance, 4 men died from the consumption <strong>of</strong> 1080 which had been stored<br />

in s<strong>of</strong>t drink or whiskey bottles. Also, four suicides have occurred as the result <strong>of</strong> drinking 1080. Five<br />

confirmed deaths and three possible deaths <strong>of</strong> small children have been traced to the consumption <strong>of</strong> 1080<br />

solutions from souffle cups and from chewing on empty cups containing dried residues <strong>of</strong> the poison.<br />

Littin, K., Mellor, D. J., Warburton, B., and Eason, C. T. (2004). Animal welfare and ethical issues relevant<br />

to the humane control <strong>of</strong> vertebrate pests. New Zealand veterinary journal 52, 1-10.<br />

Keywords: welfare/pest<br />

Liu, J. Q., Kurihara, T., Ichiyama, S., Miyagi, M., Tsunasawa, S., Kawasaki, H., Soda, K., and Esaki, N.<br />

(1998). Reaction mechanism <strong>of</strong> fluoroacetate dehalogenase from Moraxella sp. B. Journal <strong>of</strong> biological<br />

chemistry 273, 30897-30902.<br />

Keywords: metabolism/persistence in soil<br />

Livanos, G. and Milham, P. J. (1984). Fluoride ion-selective electrode determination <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate in meat baits and formulations. Journal <strong>of</strong> the Association <strong>of</strong> Official Analytical<br />

Chemists 67, 10-12.<br />

Keywords: fluoride/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/1080/analysis<br />

Abstract: Hot aqueous alkaline conditions were used to defluorinate sodium mon<strong>of</strong>luoroacetate (Compound<br />

1080) with a mean efficacy <strong>of</strong> 98% and a coefficient <strong>of</strong> variation <strong>of</strong> 2%. The liberated fluoride was<br />

determined by ion-selective electrode.<br />

Livingstone, P. G. (1994). Implications <strong>of</strong> 1080 for control <strong>of</strong> animal pests. In 'Proceedings <strong>of</strong> the Science<br />

Workshop on 1080. 12-14 December 1993, Christchurch, New Zealand.'. (A. A. Seawright and C. T.<br />

EasonEds. ) pp. 1-9. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: 1080/possums/rabbits/Tb<br />

Abstract: New Zealand's environment evolved without herbivorous mammals. Humans introduced and<br />

actively assisted in the colonisation <strong>of</strong> a range <strong>of</strong> mammals throughout New Zealand. Introduced mammals<br />

have affected agricultural production, changed the local composition <strong>of</strong> native flora and fauna and<br />

contributed to the ecological degradation <strong>of</strong> the environment. In defined areas, possums are the major<br />

vector <strong>of</strong> tuberculosis for cattle.<br />

Aerial and ground deployment <strong>of</strong> 1080 bait provides a cost-effective means <strong>of</strong> reducing rabbit, wallaby,<br />

possum, feral goat and deer populations in areas where they were negatively impacting on agricultural or<br />

conservation values. Because <strong>of</strong> their continuing impacts, an estimated $30 million will be spent<br />

controlling these animals in 1993/94, largely using 1080 bait.<br />

Use <strong>of</strong> 1080 poison through has caused problems and provoked controversy. It can kill some nontarget<br />

species. It has induced local "shyness" problems in target species and its increased use has given rise to<br />

concerns over its fate in the environment.<br />

Introduced herbivores will continue to place New Zealand's environment and agricultural production at<br />

risk, requiring their control. Until an acceptable form <strong>of</strong> biological control is available, environmental<br />

research and management data indicates that 1080 is the toxin <strong>of</strong> choice for large scale feral/wild animal<br />

control. Rejection <strong>of</strong> the use <strong>of</strong> 1080 by stakeholders would have major implications for New Zealand's<br />

ability to preserve its unique ecological heritage and maintain acceptance <strong>of</strong> exported primary produce.<br />

Livingstone, P. G. and Nelson, P. C. Possum <strong>Control</strong> and the Use <strong>of</strong> 1080 in New Zealand. 1-16. 1994.<br />

DoC, AHB, MAF.<br />

Ref Type: Report<br />

Keywords: 1080/possums/birds/Tb/deer<br />

Abstract: The possum problem<br />

Australian brushtail possums (Trichosurus vulpecula) are a major pest in New Zealand. They browse<br />

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native vegetation and prey on native birds and insects. Possums have been linked to persistent problems <strong>of</strong><br />

bovine tuberculosis (Tb) in cattle and deer herds, threatening an export trade currently valued at $5 billion.<br />

Llewellyn, M. C. Assessment <strong>of</strong> wallaby populations poisoned with 1080-inpregnated baits. Lake Okataina<br />

and Makatit Dome. Contract report prepared for Department <strong>of</strong> Conservation, 7p. 1988.<br />

Ref Type: Unpublished Work<br />

Keywords: baits/poisoning/1080<br />

Lloyd-Jones, G., Aislabie, J, and Hunter, D. W. F. Biodegradation <strong>of</strong> mon<strong>of</strong>luoroacetate (1080).<br />

LC9495/11, 1-6. 1994. <strong>Landcare</strong> <strong>Research</strong> Contract Report.<br />

Ref Type: Report<br />

Keywords: mon<strong>of</strong>luoroacetate/1080<br />

Abstract: Looking for microorganisms that degrade 1080 in 8 soil and 8 water samples. Three soils and two<br />

water samples did contain the required bacteria<br />

Lloyd, B. and McQueen, S. (1998). Evaluating the impact <strong>of</strong> 1080 pest control operations on short-tailed<br />

bats. In 'Proceedings <strong>of</strong> the Second New Zealand Bat Conference, Ohakune, New Zealand, 28-29 March<br />

1998'. (Ed. B. Lloyd.) p. 16. (Department <strong>of</strong> Conservation: Wellington.)<br />

Keywords: non-target species/mammals/1080/invertebrates<br />

Abstract: The impact <strong>of</strong> an aerial 1080 operation on a population <strong>of</strong> short-tailed bats Mystacina tuberculata<br />

inhabiting Rangataua Forest was evaluated using several methods. Bats caught and held for 48 hours<br />

displayed no symptoms <strong>of</strong> 1080 intoxication, although this technique's sensitivity has not been resolved.<br />

Invertebrates were collected and assayed for 1080 content, and results indicated that short-tailed bats, and<br />

other vertebrate insectivores, are vulnerable to secondary poisoning after aerial 1080 operations.<br />

Lloyd, B. D. Evaluating the potential hazard <strong>of</strong> aerial 1080 poison operations to short-tailed bat<br />

populations. Conservation Advisory Notes No. 108, -12. 1994. Wellington, New Zealand, Department <strong>of</strong><br />

Conservation.<br />

Ref Type: Report<br />

Keywords: 1080/invertebrates/non-target species/aerial control/mammals/bats/poison<br />

Abstract: Available relevant information was reviewed to assess the potential hazard <strong>of</strong> aerial 1080 poison<br />

operations to short-tailed bat populations. Although there is insufficient information available to provide a<br />

reliable evaluation <strong>of</strong> the hazards, the information that is available indicates that short-tailed bat<br />

populations are unlikely to suffer from direct poisoning caused by bats consuming arthropods that have fed<br />

on 1080 baits. Because <strong>of</strong> their low fecundity bat populations may take a long time to recover from<br />

relatively minor mortality episodes.<br />

Lloyd, B. D. (1997). Evaluating the impact <strong>of</strong> 1080 on invertebrate food sources for bats. In 'Report from<br />

the possum and bovine tuberculosis control National Science Strategy Committee, october 1997'. (Ed. D. E.<br />

Wright.) p. -35. Wellington, New Zealand.)<br />

Keywords: 1080/invertebrates/non-target species/secondary poisoning/bats/mammals<br />

Lloyd, B. D. and McQueen, S. M. (2000). An assessment <strong>of</strong> the probability <strong>of</strong> secondary poisoning <strong>of</strong><br />

forest insectivores following an aerial 1080 possum control operation. New Zealand journal <strong>of</strong> ecology 24,<br />

47-56.<br />

Keywords: secondary poisoning/non-target species/birds/1080/lethal dose/invertebrates<br />

Lloyd, B. D. and McQueen, S. M. (2002). Measuring mortality in short-tailed bats (Mystacina tuberculata)<br />

as they return from foraging after an aerial 1080 possum control operation. New Zealand journal <strong>of</strong> ecology<br />

26, 53-59.<br />

Keywords: bats/1080/baits/secondary poisoning/poisoning/possums/symptoms/analysis/behaviour<br />

Abstract: Lesser short-tailed bats (Mystacina tuberculata) feed on arthropod taxa known to consume 1080<br />

baits. Thus, they may be vulnerable to secondary poisoning after control operations for brushtail possums<br />

(Trichosurus vulpecula) using aerially broadcast 1080 baits. Short-tailed bat mortality was monitored<br />

during 11 days after 1080 baits were broadcast over their winter foraging area. Monitoring involved<br />

catching a sample <strong>of</strong> 269 bats as they arrived at a roost after foraging, then holding them in captivity for 48<br />

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hours. None <strong>of</strong> the captured bats displayed any symptoms <strong>of</strong> 1080 poisoning. Power analysis indicates<br />

that there was a > 0.95 probability <strong>of</strong> detecting mortality when the actual mortality rate was above 11.1<br />

deaths per thousand foraging flights. Uncertainties in assumptions about the bats' behaviour meanthat the<br />

overall population mortality corresponding to this minimum detectable mortality rate may range from 5.4 to<br />

28.4%, with the best estimate <strong>of</strong> 14.4%. Although it can be concluded that this 1080 operation probably<br />

did not cause major mortality <strong>of</strong> the short-tailed bats, several replicate trials are required before a<br />

generalised conclusion can be drawn about the fate <strong>of</strong> short-tailed bats following aerial 1080 operations.<br />

More information about short-tailed bat population demography is required to assess the impact <strong>of</strong> 1080<br />

operations on population viability.<br />

Lloyd, W. E. (1983). Sodium fluoroacetate (compound 1080) poisoning. In 'Current veterinary therapy<br />

VIII. Small animal practice'. (Ed. R. W. Kirk.) pp. 112-114. (W.B.Saunders: Philadelphia.)<br />

Keywords: diagnosis/treatment/mode <strong>of</strong> action/sodium fluoroacetate/1080/cats<br />

Abstract: Sodium fluoroacetate (compound 1080) is a potent rodenticide that has been restricyted to use by<br />

pr<strong>of</strong>essional exterminators. Owing to its high toxicity in dogs and cats, it has been responsible for the<br />

deaths <strong>of</strong> these animals after they have ingested rodents killed by the compound. Fortunatley, the use <strong>of</strong><br />

compound 1080, and therefore, the poisoning <strong>of</strong> pets have diminished during recent years. However, the<br />

practitioner should not rule out compound 1080 poisoning in carnivorous pet animals, even though there is<br />

no specific satisfactory treatment. Diagnosis and prognosis are discussed.<br />

Loracher, C. and Lux, H. D. (1974). Impaired hyperpolarising inhibition during insulin hypoglycaemia and<br />

fluoroactetate poisoning. Brain research 69, 164-169.<br />

Keywords: cats/mode <strong>of</strong> action/pathology/welfare/inhibition/poisoning/CNS/brain/fluoroacetate/symptoms<br />

Lotspiech, W. D., Peters, R A., and Wilson, T. H. (1952). The inhibition <strong>of</strong> aconitase by 'inhibitor fractions'<br />

isolated from tissues poisoned with fluoroacetate. Unknown 51, 20-25.<br />

Keywords: inhibition/aconitase/fluoroacetate/enzyme/citrate/poisoning/biochemistry<br />

Abstract: The fluorotricarboxylic acid fractions isolated from tissues poisoned with fluoroacetate have been<br />

shown to inhibit the following reactions <strong>of</strong> the enzyme aconitase: citrate to isocitrate, isocitrate to citrate,<br />

cis-aconitase to citrate, cis-aconitate to isocitrate. The reaction citrate to isocitrate is inhibited to the same<br />

degree as the reverse reaction; the two reactions starting with cis-aconitate are less sensitive to the inhibitor.<br />

It is considered that this inhibitor <strong>of</strong> aconitase has a direct relation tot eh accumulation <strong>of</strong> citrate in<br />

fluoroacetate poisoning.<br />

Lovelace, J., Miller, G. W., and Welkie, G. W. (1968). The accumulation <strong>of</strong> fluoroacetate and fluorocitrate<br />

in forage crops collected near a phosphate plant. Atmospheric Environment 2, 187-190.<br />

Keywords: fluoroacetate/fluorocitrate/persistence in plants/fluoride/aconitase/analysis/secondary<br />

poisoning/biosynthesis<br />

Abstract: Plants were collected from an are high in atmospheric fluoride. Animals grazing on this are<br />

showed severe fluoride injury. Analyses <strong>of</strong> plants indicated accumulation <strong>of</strong> fluorocitrate and fluoroacetate<br />

concentrations <strong>of</strong> 896 ug and 179 ug/g leaf dry weight. The presence <strong>of</strong> these compounds was established<br />

by chromatogrpahic techniques, inhibition <strong>of</strong> aconitase and i.r. spectral analysis.<br />

Lowe, M. 1080 in honey from possum baits, Rahotu - Taranaki. -17. 1994.<br />

Ref Type: Report<br />

Keywords: 1080/baits/humans/secondary poisoning/persistence in animals/honey<br />

Abstract: Honey was sampled from beehives within the flight zone <strong>of</strong> a possum poisoning operation using<br />

1080 with "jam" bait which is an attractive forage for bees. The methodology required some determination<br />

<strong>of</strong> bee activity and estimation <strong>of</strong> sample age so as to establish the link between samples and the poisoning<br />

operation. The highest concentration <strong>of</strong> 1080 detected in the honey was 15 ppb and subsequent tests<br />

showed a gradual decay down to 3 ppb after 59 days. The honey source that the samples were taken form<br />

would have eventually gone on sale after 16 weeks, hence there would not have been any detectable level<br />

<strong>of</strong> 1080 in teh sale product, although under different circumstances this time could be considerably shorter.<br />

There is no risk <strong>of</strong> acute poisoning from such low levels <strong>of</strong> 1080 and with regard to sublethal effects, there<br />

has been little research done. Aspects <strong>of</strong> risk management for Medical Officer <strong>of</strong> helath approvals, that<br />

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include such factors for consideration as toxicity, decay, public perception and oracticla options for<br />

reducing levels <strong>of</strong> contamination are discussed.<br />

Lynch, G. D. and Nass, R. D. (1981). Sodium mon<strong>of</strong>luoroacetate (1080): relation <strong>of</strong> its use to predation on<br />

livestock in western national forests, 1960-78. Journal <strong>of</strong> Range Management 34, 421-423.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/livestock/field efficacy/predators<br />

Abstract: Concern over certain animal damage control methods used by the US Fish and Wildlife Service,<br />

primarily the predacide Compound 1080, prompted a Presidential Order in 1972 banning the use <strong>of</strong><br />

toxicants ion public lands. This continuing ban <strong>of</strong> 1080 use has been reinforced by the recent policy address<br />

issued by the Secretary <strong>of</strong> the Interior. Following the initial ban, greater emphasis was placed on aerial<br />

hunting <strong>of</strong> coyotes for prevention and correction <strong>of</strong> damage to sheep and goats. Aerial hunting is expensive,<br />

however, and has only limited application in timbered, mountainous areas <strong>of</strong> many national forests. Inthe<br />

period since toxicants were banned, numbers <strong>of</strong> grazing livestock reported as lost to predationon western<br />

national forests has increased. Numbers <strong>of</strong> toxic bait stations (1080) used throughout the West, from 1960<br />

tot he 1972 ban, showed a strong inverse relationship with numbers <strong>of</strong> livestock reported lost to predation<br />

on national forests during these same years.<br />

Lyver, P. O'B., Ataria, J. M., and Trought, K. R-10604 Residues in Long-fin Eels (Anguilla dieffenbachii)<br />

following Exposure to 1080 in Water and Food. <strong>Landcare</strong> <strong>Research</strong> Contract Report: LC0304/140, -22.<br />

2004.<br />

Ref Type: Report<br />

Keywords: residues/1080/baits/dermal/muscle/gut/possums/treatment/acute<br />

toxicity/toxicity/poisoning/metabolism/excretion/mammals/birds/degradation<br />

Abstract: Objectives<br />

• To determine the effect <strong>of</strong> exposing captive long-fin eels to 1080 from RS5 cereal pellet baits<br />

deployed in the water column (primary exposure) via: (a) ingestion and dermal absorption and; (b) via<br />

dermal absorption only.<br />

• To determine the effect <strong>of</strong> exposing captive long-fin eels to 1080 through the ingestion <strong>of</strong> possum<br />

muscle and gut tissue that contained 1080 (secondary exposure).<br />

• To measure the concentration <strong>of</strong> 1080 in eel muscle tissue following primary and secondary<br />

exposure.<br />

• To report findings and engage Ngâi Tahu tangata whenua and relevant stakeholders in a dialogue<br />

process regarding the use <strong>of</strong> 1080 in possum control and potential effects on longfin eels.<br />

Methods<br />

• Wild-sourced eels were acclimatised for 21 days in a wet-laboratory before being exposed to 1080<br />

in scenarios representative <strong>of</strong> primary or secondary exposure.<br />

• In Trial 1, to simulate direct access to baits in waterways, 16 eels were exposed to 1080 from RS5<br />

cereal baits (0.16%) wrapped in plastic mesh (Mesh) and 16 eels had free access to RS5 cereal 1080 bait<br />

(Free) placed directly into the water column.<br />

• In Trial 2, to simulate secondary exposure where eels scavenge the carcasses <strong>of</strong> possums poisoned<br />

by 1080, 24 eels were presented with three boluses <strong>of</strong> either muscle tissue (8.3 µg/g) from possums<br />

poisoned by 1080, or gut tissue (1.4 µg/g) from the same possums. As a control 24 eels were presented<br />

with either non-poisoned possum muscle or gut tissue.<br />

• In each trial eels were monitored daily for mortality and clinical signs <strong>of</strong> toxicosis.<br />

• In Trial 1, water samples were were collected and analysed for 1080 residue at 0, 5, and 48 h after<br />

bait deployment, and eel tissue 4 d after bait deployment.<br />

• In Trial 2 eel tissue was sampled and analysed for 1080 residue 12 d after beginning the 1080poisoned-tissue<br />

feeding regime.<br />

Results<br />

• No 1080 was detected in water samples from the control treatments in Trial 1 or 2.<br />

• In Trial 1, 1080 concentrations in water samples from the free- and meshed-pellet treatments were<br />

0.057 µg/ml and 0.025 µg/ml respectively 5 h after baits were placed in the tanks. These concentrations<br />

declined to


1080 Reassessment Application October 2006<br />

Appendix C<br />

samples from the pellet-free or pellet-mesh treatments.<br />

• In Trial 2, no 1080 was detected in water samples. There were detectable concentrations <strong>of</strong> 1080<br />

in the muscle <strong>of</strong> eels (mean = 0.011 µg/g) that had consumed possum muscle containing residues <strong>of</strong> 1080.<br />

Also, there were detectable concentrations <strong>of</strong> 1080 in the muscle <strong>of</strong> eels (mean = 0.010 µg/g) that had<br />

consumed possum gut containing residues <strong>of</strong> 1080. No significant difference in 1080 residue was detected<br />

in eels that had consumed contaminated possum muscle (mean = 0.012 µg/g) or gut (mean = 0.038 µg/g)<br />

tissue in the last 3 days <strong>of</strong> the trial (t = 2.17; d.f. = 7; P = 0.067).<br />

Conclusions<br />

• 1080 leached from cereal pellet baits is unlikely to kill eels.<br />

• Eels did not eat cereal 1080 baits in this study, suggesting that the risk <strong>of</strong> acute toxicity in eels<br />

from the consumption <strong>of</strong> baits in the field is low.<br />

• Risk to eels <strong>of</strong> acute 1080 poisoning following the consumption <strong>of</strong> possum tissue containing<br />

concentrations <strong>of</strong> 1080 up to 8.3 µg/g over 12 d also appears to be low.<br />

• Residues <strong>of</strong> 1080 will occur in eel muscle after eels consume tissue from 1080-poisoned possums,<br />

indicating the potential for secondary contamination <strong>of</strong> eels that scavenge possum carcasses in field<br />

conditions.<br />

• The detection <strong>of</strong> 1080 in the muscle tissue <strong>of</strong> an eel 9 d after it last consumed possum gut tissue<br />

containing residual 1080 suggests that the metabolism and excretion <strong>of</strong> sublethal doses <strong>of</strong> 1080 in long-fin<br />

eels may be slower than in mammals and birds.<br />

Recommendations<br />

• To reduce response variation in the endpoints measured, all experiments were carried out in the<br />

laboratory under controlled conditions (e.g. environmental parameters and feeding regime). Although field<br />

conditions can increase variation in the response <strong>of</strong> biological endpoints, these may be balanced against a<br />

reduction in eel stress and benefits from increased environmental realism associated with field trials. Field<br />

trials could include eels and possum carcasses in natural waterways, monitoring <strong>of</strong> the presence and<br />

degradation <strong>of</strong> possum carcasses in and around (within 2 m) waterways after an aerial operation, and<br />

monitoring <strong>of</strong> wild eel stocks for 1080 residues before and after aerial baiting operations.<br />

• Proactive measures should be taken to address likely concerns regarding potential 1080<br />

contamination <strong>of</strong> eels for human consumption. To minimise negative impacts to the commercial fishing<br />

sector an in-depth study should be undertaken to evaluate the toxicokinetics <strong>of</strong> 1080 in eels so that an<br />

adequate withholding period can be established for eel harvest following baiting operations.<br />

• Given the apparent potential for eels to carry 1080 residues as the result <strong>of</strong> scavenging possum<br />

carcasses, initial evaluations <strong>of</strong> other scavenging aquatic fauna such as kanakana or piharau (Geotria<br />

australis; freshwater lamprey), which are also gathered for human consumption, should be considered.<br />

• As an additional risk-minimisation measure, the timing <strong>of</strong> aerial 1080 control operations with the<br />

hibernation period for eels and outside commercial fishing seasons should be implemented in appropriate<br />

areas.<br />

Lyver, P. O'B., Hayes, L., and Horn, C. A process for enhancing dialogue on security issues. <strong>Landcare</strong><br />

<strong>Research</strong> Contract Report LCR0304/132, -33. 2004. <strong>Landcare</strong> <strong>Research</strong>, Lincoln.<br />

Ref Type: Report<br />

Keywords: pest/1080/New Zealand<br />

Abstract: The objective <strong>of</strong> this research was to find a better way for scientists to have meaningful dialogue<br />

with the wider community about contentious scientific issues. We tested a dialogue process that combined<br />

principles from Franklin Covey's "The 7 Habits <strong>of</strong> Highly Effective People" programme with aspects <strong>of</strong><br />

tikanga Mâori (Mâori custom) on two pest control issues: the use <strong>of</strong> 1080 to control mammalian pest<br />

species and the introduction <strong>of</strong> biological control agents for weeds. We invited stakeholders with a history<br />

<strong>of</strong> involvement in these issues, as well as groups that traditionally have played a lesser role (e.g. women,<br />

youth, and the elderly), to participate in discussions or debate on these topics. The dialogue occurred at<br />

four 2-day hui around New Zealand: two in the North Island and two in the South Island.<br />

This report outlines the background <strong>of</strong> this work, the processes and activities used during each hui, and our<br />

overall reflections on this project.<br />

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Important lessons learned were:<br />

1. The process proved to be a successful formula for engaging stakeholders in dialogue. It helped<br />

people discover common ground, learn more about the standpoints <strong>of</strong> others, and build trust and<br />

understanding.<br />

2. Much time has to be spent building relationships with stakeholders prior to the dialogue event.<br />

The event itself is just the tip <strong>of</strong> the iceberg.<br />

3. While it seems a good idea to cast the net widely when looking for participants, they need to see<br />

that they will benefit from attending.<br />

4. Taking 2 days out to attend a hui was a problem for some groups and prevented them from<br />

attending. By contrast many <strong>of</strong> those who did attend said they would have liked it to be longer.<br />

5. Providing support through information and guidance was an important part <strong>of</strong> helping people to<br />

deal with a culturally unfamiliar environment.<br />

6. Getting women to present formally to the group was difficult, but they were very good at working<br />

within the group and interacting less formally.<br />

7. Participants need to be present at the hui for the entire time because the dialogue process builds<br />

upon itself.<br />

8. Much <strong>of</strong> the success <strong>of</strong> the process came from finding common ground, which then allowed<br />

people to discuss the science and work through the problem.<br />

9. Complex problems require the negative aspects <strong>of</strong> a solution to be balanced against other<br />

alternatives. The strength <strong>of</strong> dialogue in this situation was that it allowed each participant to weigh up the<br />

positive and negative points for themselves in an environment where those in authority were not able to<br />

move into persuasion mode.<br />

10. People need time and a reason to consider issues and to develop their own understanding and<br />

solutions. Most experts have had years to consider the issues, other people need more than just a public<br />

meeting for this. "Taking people with us" therefore means providing a reason and opportunities for them to<br />

participate in piecing together an understanding <strong>of</strong> the issues rather than trying to persuade them.<br />

11. People are taught to speak, but are not taught to listen. To exchange knowledge we need to<br />

develop our listening skills. It takes training, effort, work, and self-aware reflection to build good listening<br />

skills.<br />

12. Effective facilitation is essential for good dialogue.<br />

13. Removing participants from familiar surroundings assisted with breaking down barriers between<br />

groups. Being placed in a "new" environment helped participants to become more open to "new" ideas or<br />

alternative perspective.<br />

Macchiavello, A. (1946). Plague control with DDT and "1080" : results achieved in a plague epidemic at<br />

Tumbes, Peru, 1945. American journal <strong>of</strong> public health 36, 842-854.<br />

Keywords: target species<br />

Mackintosh, G. R. (1950). Destruction <strong>of</strong> wild pigs by poisoned baits. New Zealand journal <strong>of</strong> agriculture<br />

80, 259-262.<br />

Keywords: pigs/baits/field efficacy<br />

Marais, J. S. C. (1944). Mon<strong>of</strong>luoroacetic acid, the toxic principle <strong>of</strong> "Gifblaar" Dichapetalum cymosum<br />

(Hook) Engl. Onderstepoort journal <strong>of</strong> veterinary science and animal industry 20, 67-73.<br />

Keywords: product chemistry/occurrence in nature<br />

Marks, C. A., Busana, F., and Gigliotti, F. (1999). Assessment <strong>of</strong> the M-44 ejector for the delivery <strong>of</strong> 1080<br />

for red fox (Vulpes vulpes) control. Wildlife research 26, 101-109.<br />

Keywords: 1080/foxes/lethal dose/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/non-target species<br />

Abstract: The M-44 ejector delivered a reliable lethal dose <strong>of</strong> 1080 (sodium mon<strong>of</strong>luoroacetate) to captive<br />

foxes, with a capsule dose <strong>of</strong> 2.0 mg <strong>of</strong> 1080, if a 'collar' modification was used. Behavioural observations<br />

indicated that the collar influenced the orientation <strong>of</strong> the fox's mouth to the M-44 bait upon activation,<br />

resulting in a much greater amount <strong>of</strong> 1080 entering its mouth. This dose is below the 3 mg currently used<br />

in fox baits in Victoria and may increase the margin <strong>of</strong> safety for non-target species during 1080 baiting<br />

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Appendix C<br />

programs. The authors discuss some <strong>of</strong> the potential advantages <strong>of</strong> the ejector over the use <strong>of</strong> meat baits,<br />

such as the elimination <strong>of</strong> bait caching and improved target specificity. The potential for the M-44 to<br />

deliver an even lower lethal dose <strong>of</strong> 1080, which is closer to the reported theoretical bait LD100 <strong>of</strong> 1.25 mg<br />

for this species, may further reduce the risk <strong>of</strong> 1080 baiting to non-target species such as tiger quolls.<br />

[References: 25] 25<br />

Marks, C. A., Hackman, C., Busana, F., and Gigliotti, F. (2000). Assuring that 1080 toxicosis in the red fox<br />

(Vulpes vulpes) is humane: fluoroacetic acid (1080) and drug combinations. Wildlife research 27, 483-494.<br />

Keywords: acute toxicity/welfare/mammals/1080/treatment<br />

Marrazzi, M. A. and Holliday, J. F. (1981). Comparison <strong>of</strong> insulin hypoglycemia-induced and<br />

fluoroacetate-induced convulsions in gold thioglucose lesioned mice. Biochemical Pharmacology 30, 3231-<br />

3237.<br />

Keywords: convulsions/brain/fluoroacetate/citrate<br />

Abstract: In addition to its well known effect in producing hyperphagia, resulting in obesity, and<br />

histological damage focused relatively selectively in the ventromedial hypothalamic area, systemically<br />

administered gold thioglucose (GTG) also increased the sensitivity to insulin hypoglycemic convulsions.<br />

The change was in the convulsive response to equal hypoglycemia, rather than in the degree <strong>of</strong><br />

hypoglycemia in response to insulin. The effect suggests that a relatively discreet control center is involved<br />

in adjusting brain functions to metabolic alterations, in this case hypoglycemia. These results compare the<br />

effects <strong>of</strong> GTG lesions on insulin hypoglycemic and fluoroacetate-induced convulsions. GTG lesions did<br />

not alter the sensitivity to another metabolic convulsant, fluoroacetate, which blocks the Krebs cycle by<br />

blocking the conversion <strong>of</strong> citrate to isocitrate. Thus, although related in both cases to a shortage <strong>of</strong><br />

available cellular fuel, the metabolic convulsions induced by insulin hypoglycemia and fluoroacetate must<br />

be qualitatively different.<br />

Marsh, R. E., Schmidt, R. H., and Howard, W. E. (1987). Secondary hazards to coyotes <strong>of</strong> ground squirrels<br />

poisoned with 1080 or strychnine. Wildlife Society bulletin 15, 380-385.<br />

Keywords: 1080/strychnine/baits/lethal dose/secondary poisoning/predators/persistence in animals<br />

Abstract: Separate groups <strong>of</strong> California ground squirrels were laboratory fed either strychnine or 1080treated<br />

baits in amounts representative <strong>of</strong> low or high consumption rates expected to occur in a control<br />

program. Acute and chronic secondary toxicity was subsequently evaluated with captive groups <strong>of</strong> 4-7<br />

coyotes. In these acute tests, a single feeding <strong>of</strong> 2 squirrels, which had consumed either a low (0.5 mg) or<br />

high (3.0 mg) lethal dose <strong>of</strong> 1080, was fed to each coyote <strong>of</strong> the test groups. No mortality occurred in the<br />

coyotes given 2 low-dose squirrels, but 5 <strong>of</strong> 6 coyotes that were given 2 squirrels receiving the high 1080<br />

dose (ie 6 times the low dose) died. In teh chronic 1080 test, 1 <strong>of</strong> 7 (14.2%) coyotes that consumed a lowdose<br />

squirrel for 5 consecutive days died. This suggests little secondary hazard for 5 low (0.5 mg) multiple<br />

doses.<br />

Martin, G. R. and Twigg, L. E. (2001). Sensitivity to sodium fluoroacetate (1080) <strong>of</strong> native animals from<br />

north-western Australia. Wildlife research in press, in press.<br />

Keywords: acute toxicity/non-target species/secondary poisoning/birds/citrate/approximate lethal dose<br />

Abstract: The sensitivity to sodium fluoroacetate (1080) <strong>of</strong> 9 species <strong>of</strong> native animals from north Western<br />

Australia was assessed using the increasing dose procedure to determine the Approximate Lethal Dose<br />

(ALD) for each species. Increases in plasma citrate concentration was also determined for some species.<br />

Granivorous birds from this region (e.g. ducks, corellas) were generally more sensitive to 1080 than their<br />

counterparts from southern Australia, and theoretically be at risk from primary poisoning during 1080<br />

grain-based baiting programs. However, the tolerance to 1080 <strong>of</strong> birds <strong>of</strong> prey from these areas is sufficient<br />

that these species face little risk <strong>of</strong> secondary poisoning during pest control programs aimed at rodents or<br />

rabbits. The risk <strong>of</strong> primary posioning to raptors from meat baits conatinign 6 mg 1080 per bait or less<br />

appears to be low. The coexistence <strong>of</strong> brown falcons and barn owls with fluoroacetate-bearing vegetation<br />

over parts fo their range has probably contributed to their development <strong>of</strong> tolerance to fluoroacetate.<br />

Martin, G. R., Twigg, L. E., Marlow, N. J., Kirkpatrick, W. E., and Gaikhorst, G. (2002). The acceptability<br />

<strong>of</strong> three types <strong>of</strong> predator baits to captive non-target animals. Wildlife research 29, 489-502.<br />

Keywords: baits/non-target species/poisoning/1080/tolerance/rodents/predators<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: The acceptability <strong>of</strong> three types <strong>of</strong> non-toxic predator baits to a variety <strong>of</strong> indigenous non-target<br />

species was determined in the laboratory. The bait-types tested were: Dried Meat Bait (DMB), Probait and<br />

two sizes <strong>of</strong> FoxOff(TM) baits (30 g and 60 g). The potential poisoning risk, if the baits had been toxic,<br />

was calculated for each species from their consumption <strong>of</strong> non-toxic bait and their sensitivity to 1080.<br />

Three species consistently sampled baits; Dasyurus ge<strong>of</strong>froii, Trichosurus vulpecula and Rattus fuscipes.<br />

Where species have had exposure to fluoroacetate-bearing vegetation, their consumption <strong>of</strong> bait and their<br />

level <strong>of</strong> tolerance to 1080 was such that only 2 <strong>of</strong> 15, 4 <strong>of</strong> 15, and 3 <strong>of</strong> 6 species were considered to be<br />

potentially at some risk from toxic DMBs, Probait, and FoxOff(TM) baits, respectively. In contrast, and<br />

mainly because <strong>of</strong> their lower tolerance to 1080, the theoretical risk for those species without evolutionary<br />

exposure to fluoroacetate-bearing vegetation was such that 6 <strong>of</strong> 12, 8 <strong>of</strong> 12, and 8 <strong>of</strong> 9 species theoretically<br />

face a high or moderate risk from 3-mg DMBs, Probait, and FoxOff(TM) baits, respectively. We<br />

emphasise, however, that theoretical risk does not necessarily equate to a practical risk, and these results<br />

are best used to determine which non-target species should be monitored at the population level during<br />

predator-control operations. Factors affecting the potential risk to non-target indigenous animals, and some<br />

cautions when extrapolating data from laboratory-based studies to the field situation, are discussed.<br />

Martinez, R. R. (1979). Diagnosis and frequency <strong>of</strong> the most commonly identified intoxications <strong>of</strong> dogs in<br />

the Mexico City area. Veterinaria, Mexico 10, 45-49.<br />

Keywords: diagnosis/dogs/strychnine/zinc phosphide/warfarin/fluoroacetate<br />

Abstract: Among 49 dogs diagnosed clinically as poisoned, strychnine was demonstrated in 21, zinc<br />

phosphide in 2, lead in 3, dieldrin in 1, warfarin in 3, thalium in 1, an organic phosphorus insecticide in 1<br />

and probably fluoroacetate in 2; the cause was not determined in 15. Death was usually sudden<br />

Matsubara, I., Kamiya, J., and Imai, S. (1980). Cardiotoxic effects <strong>of</strong> 5-fluorouracil in the Guinea Pig.<br />

Japan J.Pharmacol. 30, 871-879.<br />

Keywords: chemistry/heart/mode <strong>of</strong> action/5-fluorouracil/citrate/Krebs cycle<br />

Abstract: In order to search into the underlying mechanisms <strong>of</strong> ECG changes suggestive <strong>of</strong> ischemia<br />

observed in humans and in rabbits after administration <strong>of</strong> 5-fluorouracil (5-FU), experiments were<br />

performed in anesthetized open-chest guinea pigs. The substance produced similar ECG changes in this<br />

species as well, after a rather long latent period <strong>of</strong> around 3 hours intravenous administration. The<br />

incidence <strong>of</strong> ECG abnormality in animals given 60 mg/kg was 7/7, while that in animals given 30 mg/kg<br />

was 4/9. With 10-20 mg/kg, ECG changes were not observed during an experimental period as long as 5<br />

hours. Associated with these ECG changes, a depletion <strong>of</strong> the high-energy phosphate compounds <strong>of</strong> the<br />

ventricular myocardium was observed. Analysis <strong>of</strong> tricarboxylic acid cycle (TCA cycle) intermediates<br />

revealed an accumulation <strong>of</strong> citrate within the myocardium, suggesting a malfunction <strong>of</strong> TCA cycle<br />

resulting from an inhibition <strong>of</strong> aconitase by fluorocitrate, as a cause <strong>of</strong> depletion <strong>of</strong> the high-energy<br />

phosphates. It is probable that the accumulation <strong>of</strong> citrate was due to the formation <strong>of</strong> fluoroacetate, an<br />

inhibitor <strong>of</strong> aconitase, from 5_FU via alpha-fluoro-beta-alanine, a major degradation product <strong>of</strong> 5-FU, for it<br />

is known that beta-alanine is usually converted to acetate.<br />

Matsumura, F. and O'Brien, R. D. (1963). A comparative study <strong>of</strong> the modes <strong>of</strong> action <strong>of</strong> fluoroacetamide<br />

and fluoroacetate in the mouse and American cockroach. Biochemical Pharmacology 12, 1201-1205.<br />

Keywords: fluoroacetamide/fluoroacetate/poisoning/citrate/fluorocitrate/muscle/invertebrates/metabolism<br />

Abstract: In the American cockroach and mouse, both fluoroacetate and fluoroacetamide poisoning led to<br />

large large citrate concentrations in the body. In the cockroach poisoned with fluoroacetamide,<br />

fluoroacatate and fluorocitrate were found in muscle. It thus seems probable that the first step in<br />

fluoroacetamide poisoning is hydrolysis to fluoroacetate. This hydrolysis was more rapid in cockroach<br />

homogenates than in mouse homogenates, which may account for the selective toxicity <strong>of</strong> fluoroacetamide<br />

to the cockroach.<br />

Mazzanti, L., Lopez, M., and Berti, M. G. (<strong>1964</strong>). Selective destruction in testes induced by<br />

fluoroacetamide. Experientia 20, 492-493.<br />

Keywords: testes/fluoroacetamide/reproductive effects<br />

Mazzanti, L. (1965). Atrophy <strong>of</strong> the testis produced by sodium mon<strong>of</strong>luoroacetate in albino rats.<br />

Experientia 21, 446-447.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/rats/mon<strong>of</strong>luoroacetate/fluoroacetamide/testes/reproductive effects<br />

Abstract: The lesions caused by sodium mon<strong>of</strong>luoroacetate on the testis <strong>of</strong> the albino rat are described.<br />

They consist <strong>of</strong> regressive modifications <strong>of</strong> the seminiferous tubules which initially cause damage tot he<br />

intermediate stages and only later to the spermatogonia. The action <strong>of</strong> sodium mon<strong>of</strong>luoroacetate is similar<br />

to that <strong>of</strong> fluoroacetamide.<br />

Mazzanti, L., Lopez, M., and Del Tacca, M. (1968). Regeneration <strong>of</strong> testes atrophied by fluoroacetamide.<br />

Experientia 24, 258-259.<br />

Keywords: testes/fluoroacetamide/reproductive effects/rats/treatment/sublethal effects<br />

Abstract: Morphological changes <strong>of</strong> atrophic testis, obtained by treating normal rats with fluoroacetamide,<br />

are studied at various times after treatment. The data show that the testicular germinal epithelium is fully<br />

regenerated 165 days after treatment.<br />

McCombie, H. and Saunders, B. C. (1946). Fluoroacetates and allied compounds. Nature 158, 382-385.<br />

Keywords: product chemistry/fluoroacetate<br />

McDougall, W. A. (1949). The rat <strong>poisons</strong>, sodium fluoroacetate and "Castrix". Queensland Journal <strong>of</strong><br />

Agricultural Science 6, 54-60.<br />

Keywords: <strong>poisons</strong>/sodium fluoroacetate/fluoroacetate/1080/efficacy/baits/lethal dose/rodents<br />

Abstract: The rat <strong>poisons</strong> sodium fluoroacetate ("1080") and "Castrix" were tested against Rattus conatus<br />

and Melomys littoralis in cages, and against R. conatus in settled field populations. Feeding tests show that<br />

the LD50 for R. conatus and M. littoralis respectively are : sodium fluoroacetate, 1.42 mg/kg, 2.23 mg/kg,<br />

Castrix, 4.46 mg/kg, 5.62 mg/kg. An I.T.F. <strong>of</strong> 3.5 is obtained at a poison strength <strong>of</strong> 1:1000 with 1080 and<br />

at 1:250 with Castrix. Both these white powders which can be used with grain are technically good rat<br />

<strong>poisons</strong>. There are strong indications that the general use <strong>of</strong> Castrix would be more dangerous than that <strong>of</strong><br />

1080. The latter (which is water soluble) at a strength <strong>of</strong> 1:1000 could replace, without any loss <strong>of</strong> efficacy,<br />

the expensive thallous sulphate in food baits for use in Queensland canefields. Though highly toxic, neither<br />

<strong>of</strong> these two new rat <strong>poisons</strong> can replace yellow phosphorus un bread snap baits.<br />

McDowell, E. M. (1973). Light and electron microscope studies <strong>of</strong> rat kidney after administration <strong>of</strong><br />

inhibitors <strong>of</strong> the citric acid cycle in vivo. Virchows Arch.Abt.B Zellpath. 13, 321-340.<br />

Keywords: kidney/citric acid/Krebs cycle/fluorocitrate/rodents/pathology<br />

Abstract: The morphological changes that occurred in the pars recta tubules <strong>of</strong> rat kidney after single<br />

intraperitoneal injections <strong>of</strong> sodium fluorocitrate, a competitive inhibitor <strong>of</strong> aconitase, at 15 or 60 mg per kg<br />

body weight are described. A gamut <strong>of</strong> pathological changes occurred along the length <strong>of</strong> renal proximal<br />

tubules during fluorocitrate poisoning. These changes must be related in part to the physiological,<br />

functional and metabolic capacities <strong>of</strong> different segments <strong>of</strong> the proximal tubules.<br />

McEwan, T. (<strong>1964</strong>). Isolation and identification <strong>of</strong> the toxic principle <strong>of</strong> Gastrolobium grandiflorum.<br />

Queensland Journal <strong>of</strong> Agricultural Science 21Copy <strong>of</strong> paper on file., 1-14.<br />

Keywords: fluoroacetate/occurrence in nature<br />

McEwan, T. (1978). Organo-fluorine compounds in plants. In 'Effects <strong>of</strong> Poisonous Plants on Livestock'.<br />

(R. F. Keeler, K. R. Van Kampen, and L. F. JamesEds. ) pp. 147-158. (Academic Press:<br />

Keywords: livestock/toxicity/fluoroacetate/poisoning/occurrence in nature<br />

Abstract: A brief review is presented <strong>of</strong> the occurrence <strong>of</strong> organ<strong>of</strong>luroine compounds in plants and <strong>of</strong> the<br />

effects <strong>of</strong> feeding plants with F. The compounds are found in Dichapetalum cymosum, Acacia georginae,<br />

Palicourea marcgravii, Gastrolobium spp. and Oxylobium spp. The influence <strong>of</strong> F location in a molecule on<br />

toxicity is discussed and the toxicities <strong>of</strong> a range <strong>of</strong> organ<strong>of</strong>luorine compounds, both naturally occurring<br />

and synthetic, are summarized. Distribution <strong>of</strong> fluoroacetate in Acacia georginae is considered and the<br />

various findings are related to the incidence <strong>of</strong> poisoning <strong>of</strong> sheep and cattle in the field. Difficulties in<br />

detection <strong>of</strong> organ<strong>of</strong>luorine compounds are emphasized and possible areas <strong>of</strong> further investigation are<br />

indicated<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

McGary, E. and Meloan, C. E. (1981). A rapid qualitative method for the detection <strong>of</strong> mon<strong>of</strong>luoroacetic<br />

acid (1080) in liquid baits. Analytical letters 14, 1653-1657.<br />

Keywords: product chemistry<br />

McGirr, J. L. and Papworth, D. S. (1955). The toxicity <strong>of</strong> rodenticides I. Sodium fluoroacetate, Antu and<br />

warfarin. The Veterinary Record February 12, 124-131.<br />

Keywords: sodium fluoroacetate/fluoroacetate/warfarin<br />

McIlroy, J. C. (1981). The sensitivity <strong>of</strong> Australian animals to 1080 poison II. Marsupial and Eutherian<br />

Carnivores. Aust.Wildl.Res. 8, 385-399.<br />

Keywords: 1080/fluoroacetate/mammals/marsupials/secondary poisoning/carnivores/non-target species<br />

Abstract: Eutherian carnivores were more sensitive to 1080 poison than marsupial carnivores. Both groups<br />

<strong>of</strong> animals displayed similar symptoms but there was wide intra- and interspecific variation in the time to<br />

onset, the sequence <strong>of</strong> occurrence and duration <strong>of</strong> the symptoms. The risks that individual carnivores face<br />

from primary and secondary poisoning have been assessed. Theoretically, dingoes probably face the<br />

greatest risk amongst the species studied, followed by members <strong>of</strong> the smaller dasyurids and feral cats.<br />

Members <strong>of</strong> the dasyurids and long-nosed bandicoots probably face the least risk. Factors likely to<br />

influence the actual effect <strong>of</strong> 1080-poisoning campaigns on carnivore populations are discussed.<br />

McIlroy, J. C. (1981). The sensitivity <strong>of</strong> Australian animals to 1080 poison I. Intraspecific variation and<br />

factors affecting acute toxicity. Wildlife research 9, 369-383.<br />

Keywords: 1080/poison/acute toxicity<br />

McIlroy, J. C. (1982). The sensitivity <strong>of</strong> Australian carnivorous mammals to 1080 poison. In 'Carnivorous<br />

marsupials'. (Ed. M. Archer.) pp. 267-271. (<strong>Royal</strong> Zoological Society <strong>of</strong> New South Wales: Mosman,<br />

NSW.)<br />

Keywords: acute toxicity/non-target species/mammals/1080/marsupials<br />

McIlroy, J. C. (1982). The sensitivity <strong>of</strong> Australian animals to 1080 poison IV. Native and introduced<br />

rodents. Aust.Wildl.Res. 9, 505-517.<br />

Keywords: 1080/tolerance/fluoroacetate/mammals/rodents/acute toxicity/diagnosis/baits/time to death<br />

Abstract: Most rodent species that have been tested in Australia and elswhere are highly sensitive to 1080<br />

poison. A few native species, particularly members <strong>of</strong> the 'pseudo-mouse group' (Conilurini), part <strong>of</strong> whose<br />

range is in Western Australia, are much more tolerant. These species may have developed this tolerance<br />

from being exposed to indigenous plants that contain fluoroacetate. The most common signs <strong>of</strong> poisoning<br />

amongst rodents are depression, hypersensitivity to stimuli, respiratory distress and convulsions. Signs <strong>of</strong><br />

poisoning first appeared amongst the species tested in this study 0.4 - 38.1 h after dosing. Deaths occurred<br />

0.7 - 205.8 h after dosing. The susceptibility to 1080-poisoning <strong>of</strong> the 14 species <strong>of</strong> rodents tested in<br />

Australia depends on both sensitivity and body size, and is discussed in relation to typical baits and<br />

concentrations <strong>of</strong> 1080 used against vertebrate pests. Individuals <strong>of</strong> most species <strong>of</strong> rodents would appear to<br />

face a considerable risk if pest-poisoning campaigns are carried out within their range, but the crucial factor<br />

governing the actual effect on populaions will be how many individuals find and eat the baits.<br />

McIlroy, J. C. (1982). The sensitivity <strong>of</strong> Australian animals to 1080 poison III. Marsupial and eutherian<br />

herbivores. Wildlife research 9, 487-503.<br />

Keywords: 1080/poison/carnivores/lethal dose/time to death/symptoms<br />

McIlroy, J. C. (1983). The sensitivity <strong>of</strong> Australian animals to 1080 poison VI. Bandicoots. Australian<br />

wildlife research 10, 507-512.<br />

Keywords: non-target species/acute toxicity/1080<br />

McIlroy, J. C. (1983). The sensitivity <strong>of</strong> Australian animals to 1080 poison V. The sensitivity <strong>of</strong> feral pigs,<br />

Sus scr<strong>of</strong>a, to 1080 and its implications for poisoning campaigns. Aust.Wildl.Res. 10, 139-148.<br />

Keywords: 1080/pigs/poisoning/lethal dose/analysis/mammals/<strong>poisons</strong>/baits/birds/non-target species/field<br />

efficacy<br />

Abstract: Acute oral LD50s (median lethal doses) and 95% confidence limits <strong>of</strong> 1080 poison for feral pigs,<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Sus scr<strong>of</strong>a, obtained by moving average and probit analysis methods are 1.04 (0.84 - 1.27) mg/kg and and<br />

1.00 (0.72 - 1.28) mg/kg respectively. These values are slightly higher than LD50s obtained for pigs by<br />

intraperitoneal dosing but similar to those obtained by oral dosing for other eutherian mammals. Signs <strong>of</strong><br />

poisoning, either vomiting or increasing lethergy and laboured respiration, appeared from 1.97 to 47.3 h<br />

(median 6.2 h) after dosing, and deaths from 2.8 to 80 h (median 16.1 h) after dosing. Although 1080 is one<br />

<strong>of</strong> the most toxic <strong>poisons</strong> for pigs it has disadvantages, including the relatively large amounts that must be<br />

distributed in baits to kill pigs, and the comparatively greater susceptibility to it <strong>of</strong> many non-target birds<br />

and mammals. For example, 36 species out <strong>of</strong> a selection <strong>of</strong> 40 non-target species likely to feed on<br />

poisoned baits are more suscpetible to 1080 than pigs. In practice many other factors such as bait<br />

acceptance will govern what proportions <strong>of</strong> target and non-target populations will be poisoned. Attention to<br />

methods <strong>of</strong> posioning or baiting techniques could minimise the risk non-target animals face from pigpoisoning<br />

campaigns.<br />

McIlroy, J. C. (1983). The sensitivity <strong>of</strong> the brushtail possum (Trichosurus vulpecula) to 1080 poison. New<br />

Zealand journal <strong>of</strong> ecology 6, 125-131.<br />

Keywords: 1080/possums/baits/aversion/lethal dose/field efficacy<br />

Abstract: A knwoledge <strong>of</strong> the sensitivity <strong>of</strong> the brushtail possum (Trichosurus vulpecula) to 1080 poison is<br />

important as a basis for planning effective control campaigns. This study assesses the effects that<br />

experimental procedure may have on determining the LD50 <strong>of</strong> 1080 for brushtail possums and reports on<br />

the variation in sensitivity within an between different populations <strong>of</strong> the species in Australia, where it is<br />

indigenous. LD50s obtained ranged from 0.39 -0.92 mg/kg with 95% confidence limits <strong>of</strong> from 0.29 -1.20<br />

mg/kg. These figures are similar to those obtained by Ministry <strong>of</strong> Agriculture and Fisheries researchers in<br />

New Zealand but are less than those obtained by the New Zealand Forest Service and bring into question<br />

which figures are valid for free roaming possums in the bush. This is important in regard to the toxic<br />

loading <strong>of</strong> baits, particularly given the reported aversion by some possums to baits containing the recently<br />

increased concentrations <strong>of</strong> 1080 recommended for possum control in New Zealand forest areas.<br />

McIlroy, J. C. (1984). The sensitivity <strong>of</strong> Australian animals to 1080 poison VII. Native and introduced<br />

birds. Australian wildlife research 11, 373-385.<br />

Keywords: non-target species/birds/acute toxicity/1080/lethal dose/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/tolerance/fluoroacetate/poisoning/convulsions/baits<br />

Abstract: Birds in Australia vary greatly in their sensitivity to 1080 poison (sodium mon<strong>of</strong>luoroacetate).<br />

Median lethal doses (LD50s) range from 0.63 mg kg-1 for red-browed firetails, Emblema temporalis, to<br />

approximately 278 mg kg-1 for the emu, Dromaius novaehollandiae. Significant differences occur<br />

between the sensitivity <strong>of</strong> different groups <strong>of</strong> birds and may be related to differences in their metabolic<br />

rates. A few species may also have developed a tolerance to 1080 from being exposed to indigenous plants<br />

that contain fluoroacetate, or to insects and other animals which have fed on such plants. The most<br />

common signs <strong>of</strong> 1080 poisoning among birds are depression, fluffed feathers, a reluctance to move and<br />

convulsions. Signs <strong>of</strong> poisoning first appeared among the species tested at 1-60 h after dosing, and deaths<br />

follow between 1 h to almost 11 days after dosing. The susceptibility <strong>of</strong> 48 species <strong>of</strong> birds in Australia to<br />

1080 poisoning is discussed in relation to typical baits and poison concentrations used against vertebrate<br />

pests. Theoretically, fewer types <strong>of</strong> birds are likely to be at risk from dingo-poisoning than pig-poisoning<br />

campaigns that also use meat baits but higher concentration <strong>of</strong> 1080. Individuals <strong>of</strong> 39 out <strong>of</strong> the 48 species<br />

could be at risk from rabbit and other pig-poisoning campaigns. The impact on the bird population will<br />

depend, among other factors, on the amount <strong>of</strong> bait individuals eat and on the poisoning methods<br />

employed.<br />

McIlroy, J. C. (1984). The sensitivity <strong>of</strong> Australian animals to 1080 poison I. Intraspecific variation and<br />

factors affecting acute toxicity. Australian wildlife research 8, 369-383.<br />

Keywords: acute toxicity/mode <strong>of</strong> action/rabbits/possums/birds/mammals/non-target species/1080<br />

McIlroy, J. C., King, D. R., and Oliver, A. J. (1985). The sensitivity <strong>of</strong> Australian animals to 1080 poison<br />

VIII. Amphibians and reptiles. Australian wildlife research 12, 113-118.<br />

Keywords: non-target species/acute toxicity/1080/reptiles<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

McIlroy, J. C. (1986). The sensitivity <strong>of</strong> Australian animals to 1080 poison IX. Comparisons between the<br />

major groups <strong>of</strong> animals, and the potential danger non-target species face from 1080-poisoning campaigns.<br />

Australian wildlife research 13, 39-48.<br />

Keywords: non-target species/mammals/acute toxicity/1080<br />

Abstract: The sensitivity <strong>of</strong> a species to 1080 poison is difficult to predict from toxicity data for other,<br />

closely related species. LD50s <strong>of</strong> practical use for evaluating the risk species might face from 1080poisoning<br />

campaigns can be obtained for untested members <strong>of</strong> some groups by the use <strong>of</strong> either values fro<br />

similar species, regression equations involving body weight, or the lower 95% confidence limits <strong>of</strong> the<br />

distribution <strong>of</strong> LD50s <strong>of</strong> members in each group.<br />

Among the 171 species for which there are data there was considerable variability in the time until signs <strong>of</strong><br />

poisoning became apparent (0.1 h ->7 days), the time to death (0.1 h-> 21days) and the time until animals<br />

began to show signs <strong>of</strong> recovery (2h-18 days). Marsupial carnivores generally showed signs earlier and<br />

died or recovered quicker than eutherian carnivores, eutherian herbivores and the marsupial herbivores <strong>of</strong><br />

eastern Australia, even though the last three groups have lower LD50s. Reptiles and amphibians generally<br />

were the slowest to show signs <strong>of</strong> poisoning, to die or to recover, and the highest LD50s.<br />

All species in Australia for which toxicity data are available were ranked according to the percentage <strong>of</strong><br />

their body weight they would have to eat <strong>of</strong> various poison baits to receive and LD50. Many non-target<br />

species require lower percentages than the target animals consumption <strong>of</strong> lethal bait may be affected by<br />

various factors. Finally, an evaluation is given <strong>of</strong> the major groups <strong>of</strong> animals potentially most at risk in<br />

1080-poisoning campaigns in Australia, based on their susceptibility to 1080.<br />

McIlroy, J. C., Gifford, E. J., and Cooper, R. J. (1986). Effects on non-target animal populations <strong>of</strong> wild<br />

dog trail-baiting campaigns with 1080 poison. Australian wildlife research 13, 447-453.<br />

Keywords: non-target species/birds/mammals/1080<br />

McIlroy, J. C., Gifford, E. J., and Carpenter, S. M. (1988). The effect <strong>of</strong> rainfall and blowfly larvae on the<br />

toxicity <strong>of</strong> '1080'-treated meat baits used in poisoning campaigns against wild dogs. Australian wildlife<br />

research 15, 473-483.<br />

Keywords: bait degradation/poisoning/dogs<br />

McIlroy, J. C. and King, D. (1990). Appropriate amounts <strong>of</strong> 1080 poison in baits to control foxes, Vulpes<br />

vulpes. Aust.Wildl.Res. 17, 11-13.<br />

Keywords: 1080/baits/foxes/lethal dose/field efficacy<br />

Abstract: Data are presented on the sensitivity <strong>of</strong> foxes to 1080 poison, which, although not meeting the<br />

requirements for the calculation <strong>of</strong> a precise LD50, provide a bsis for determining the appropriate amount<br />

<strong>of</strong> 1080 to use in baits to control foxes. Amounts <strong>of</strong> 2.5 mg per bait appear ample, based on the lethal dose<br />

<strong>of</strong> c. 0.15 mg/kg for foxes, but further trials may be necessary to confirm whether this provides sufficient<br />

allowance for possible reduced bioavailability and reductions in 1080 concentration in meat baits under<br />

different environmental conditions.<br />

McIlroy, J. C. and Gifford, E. J. (1991). Effect on non-target animal popualtions <strong>of</strong> a rabbit trail-baiting<br />

campaign with 1080 poison. Wildlife research 18, 315-325.<br />

Keywords: 1080/birds/mammals/rabbits/foxes/non-target species/field efficacy<br />

Abstract: Populations <strong>of</strong> non-target birds and mammals on a semi-cleared grazing property near<br />

Braidwood, New South Wales, did not appear to be affected by a trail-baiting campaign against rabbits,<br />

Oryctolagus cuniculus, using pellet bait and 1080 poison. Rabbit numbers were reduced by about 90% and<br />

those <strong>of</strong> the fox, Vulpes vulpes, another exotic pest, by about 75%. Populations <strong>of</strong> both pest species began<br />

recovering soon after the campaign, indicating the need for continued control measures.<br />

McIlroy, J. C. and Gifford, E. J. (1992). Secondary poisoning hazards associated with 1080-treated carrotbaiting<br />

campaigns against rabbits, Oryctolagus cuniculus. Wildlife research 19, 629-641.<br />

Keywords: secondary poisoning/non-target species/rabbits/acute toxicity/1080/cats/dogs/poisoning<br />

Abstract: The potential hazards that rabbits, Oryctolagus cuniculus, and other animals that may be poisoned<br />

during rabbit-control campaigns present to different carrion-eating animals were evaluated by comparing<br />

the amounts <strong>of</strong> 1080 that carrion-eaters could ingest from feeding on poisoned corpses with their measure<br />

sensitivity to the poison, Foxes, Vulpes vulpes, dingoes, Canis familiaris dingo, dogs, Canis f. familiaris,<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

and cats, Felis catus, probably face greater risk <strong>of</strong> secondary poisoning than other animals from feeding on<br />

rabbits poisoned with 1080-treated carrots. The extent to which other carrion-eating animals, particularly<br />

what and how much <strong>of</strong> the different tissues and organs <strong>of</strong> poisoned animals they eat, whether they vomit or<br />

regurgitate partly digested food, and whether they quickly develop and aversion to the taste or smell <strong>of</strong><br />

1080. Secondary poisoning hazards during rabbit-control campaigns can be minimised by using the<br />

minimum effective concentration <strong>of</strong> 1080 in baits for rabbits, by using the minimum effective number <strong>of</strong><br />

'free foods' <strong>of</strong> bait, and by removing all dead animals that can be found from the treated area.<br />

McIlroy, J. C. (1994). Susceptibility <strong>of</strong> target and non-target animals to 1080. In 'Proceedings <strong>of</strong> the<br />

Science Workshop on 1080. 12-14 December 1993, Christchurch, New Zealand.'. (A. A. Seawright and C.<br />

T. EasonEds. ) pp. 90-96. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: 1080/poison/tolerance/fluoroacetate/birds/rabbits/possums/baits/poisoning<br />

Abstract: The likelihood <strong>of</strong> an animal being killed by pest-control programs with 1080 depends on many<br />

factors. The animal's sensitivity to the poison is a key factor, but this may vary according to the animal's<br />

age or breeding condition, or whether its ancestors developed a tolerance to 1080 through feeding on plants<br />

that naturally contain fluoroacetate. Measurements <strong>of</strong> sensitivity to 1080 can vary according to differences<br />

in the experimental procedure used to obtain them, and may not necessarily indicate sensitivity under field<br />

conditions.<br />

Body size is also important in influencing what amounts <strong>of</strong> 1080 may prove lethal to different animals;<br />

small animals, such as passerine birds, are <strong>of</strong>ten more tolerant to 1080 than pests such as rabbits,<br />

Oryctolagus cuniculus, and brushtail possums, Trichosurus vulpecula, but can be killed by eating much<br />

smaller total amounts <strong>of</strong> 1080. Their fate during a baiting program depends on many factors, but<br />

principally on how many baits or poisoned animals they encounter and how much 1080 they ingest.<br />

The susceptibility <strong>of</strong> animal populations to 1080-poisoning can be gauged also by assessing their ability<br />

(in terms <strong>of</strong> reproductive an dispersal capacities) to recover from reductions in numbers caused by<br />

poisoning programs. Predictions <strong>of</strong> potential susceptibility should be compared with measurements <strong>of</strong> the<br />

actual impact <strong>of</strong> poisoning programs on populations. Results from field studies indicate that such<br />

predictions are likely to overemphasise the risk that non-target animals face, but more studies are required<br />

on rare and endangered species.<br />

McIntosh, I. G. (1958). 1080 poison. Outstanding animal pest destroyer. New Zealand journal <strong>of</strong><br />

agriculture 97, 361-366.<br />

Keywords: 1080/poison<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) has been proved during the last 15 years to be an extremely<br />

effective poison against warm-blooded animal pests in America. In Australia and New Zealand it is being<br />

used sucessfully against the rabbit. Its properties are such as to commend it for the control <strong>of</strong> all<br />

mammalian pests and as it is likely to be used more widely in this country in the future, it is desirable that<br />

farmers, hunters, and others should be informed about its nature and properties<br />

McIntosh, I. G. and Staples, E. L. J. (1959). The toxicity <strong>of</strong> muscle, liver, and heart <strong>of</strong> deer poisoned with<br />

sodium mon<strong>of</strong>luoroacetate (1080). New Zealand journal <strong>of</strong> science 2, 371-378.<br />

Keywords: secondary poisoning/mammals/persistence in animals/deer/heart/sodium<br />

mon<strong>of</strong>luoroacetate/1080/muscle/liver/humans<br />

McIntosh, I. G. (1963). 1080 Poison Baits for Animal Pests. Wallaceville shows that proper use will not<br />

bees or affect honey. New Zealand journal <strong>of</strong> agriculture 141-143.<br />

Keywords: 1080/poison/baits/honey<br />

Abstract: Trials by Wallaceville Animal <strong>Research</strong> Centre have shown that: Bees are attracted to jam baits in<br />

which 1080 is used as a poison, but the baits can be laid only by, or under the supervision <strong>of</strong>, approved<br />

operators. They are instructed not to lay baits within 1/4 mile <strong>of</strong> apiaries. Close watch on 1080 poisoning<br />

operations in the past six years has produced no evidence <strong>of</strong> mass mortalities <strong>of</strong> bees.<br />

McIntosh, I. G., Bell, J., Poole, W. S. H., and Staples, E. L. J. (1966). The toxicity <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) to the North Island weka (Gallirallus australis greyi). New Zealand journal <strong>of</strong><br />

science 9, 125-128.<br />

Keywords: acute toxicity/birds/non-target species/persistence in animals/secondary poisoning/1080<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

McIntosh, I. G. (1976). "Ten-Eighty" poison for animal pests. New Zealand journal <strong>of</strong> agriculture<br />

September 1976, 65-69.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/humans/non-target species<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) is an extremely effective poison against warm-blooded animal<br />

pests; it's properties are such as to commend it for the control <strong>of</strong> all animal pests. As it is used extensively<br />

used, in New Zealand and overseas, it is desirable that farmers, hunters and others should be informed<br />

about its nature and properties. This article examines its poisonous properties, the precautions to be take by<br />

users and the risks to humans, domestics animals and wildlife.<br />

McNaughton, A. and Greene, B. The effect <strong>of</strong> 1080 on the Hochstetter's frog (Leiopelma hochstetteri)<br />

population in the Hunua Ranges. ARC Parks Technical publication series, No 7. 1994. Auckland Regional<br />

Council.<br />

Ref Type: Report<br />

Keywords: 1080/non-target species/amphibian<br />

McTaggart, D. R. (1970). Poisoning due to sodium fluoroacetate ("1080"). The Medical Journal <strong>of</strong><br />

Australia 2, 641-642.<br />

Keywords: diagnosis/sodium fluoroacetate<br />

Abstract: A boy, aged eight years, was admitted to hospital in status epilepticus following the ingestion <strong>of</strong><br />

sodium fluoroacetate ("1080"). Subsequently, he was resuscitated from cardiac arrest, but was left with<br />

severe neurological impairment. This widely-used agricultural poison is cardiotoxic and neurotoxic, and<br />

stringent precautions exist to control its use.<br />

Mead, R. J. and Segal, W. (1972). Fluoroacetic acid biosynthesis : a proposed mechanism. Australian<br />

journal <strong>of</strong> biological sciences 25, 327-333.<br />

Keywords: occurrence in nature/product chemistry/biosynthesis<br />

Mead, R. J., Oliver, A. J., and King, D. R. (1979). Metabolism and defluorination <strong>of</strong> fluoroacetate in the<br />

brush-tailed possum (Trichosurus vulpecula). Australian journal <strong>of</strong> biological sciences 32, 15-26.<br />

Keywords: metabolism/defluorination/fluoroacetate<br />

Abstract: The brush-tailed possum from Western Australia was found to be nearly 150 times more resistant<br />

to fluoroacetate intoxication in vivo than the same species from South Australia. Acetone powder<br />

preparations from the liver <strong>of</strong> animals from both populations showed similar abilities to convert<br />

fluoroacetate into fluorocitrate. Aconitate hydratase activity in liver preparations from both Western<br />

Australian and South Australian animals was similarly and competitively inhibited by fluorocitrate. Both<br />

animals were capable <strong>of</strong> defluorinating fluoroacetate at similar rates by a glutathione-dependent enzymatic<br />

mechanism resulting in the formation <strong>of</strong> free fluoride ion and S-carboxymethylcysteine. Glutathione was<br />

also capable <strong>of</strong> partial protection against the toxic effects <strong>of</strong> fluoroacetate in vitro by a further unelucidated<br />

mechanism.<br />

Mead, R. J. The biochemistry and coevolutionary role <strong>of</strong> mon<strong>of</strong>luoroacetic acid in plant animal interaction<br />

in Australia. 1980. University <strong>of</strong> Western AustraliaEditor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: biochemistry/mon<strong>of</strong>luoroacetic acid/occurrence in nature/tolerance<br />

Mead, R. J., Moulden, D. L., and Twigg, L. E. (1985). Significance <strong>of</strong> sulfhydryl compounds in the<br />

manifestation <strong>of</strong> fluoroacetate toxicity to the rat, brush-tailed possum, woylie and estern grey kangaroo.<br />

Australian journal <strong>of</strong> biological sciences 38, 139-149.<br />

Keywords: mammals/mode <strong>of</strong><br />

action/metabolism/fluoroacetate/citrate/rodents/marsupials/possums/kidney/liver/defluorination/toxicity/rat<br />

s/1080/sodium fluoroacetate/plasma/fluorocitrate/inhibition/tolerance<br />

Abstract: Levels <strong>of</strong> citrate in kidneys and livers <strong>of</strong> rats with normal glutathione levels increased 6.8 and<br />

1.7-fold respectively after dosing with 1.5 mg <strong>of</strong> compound 1080 (=95% sodium fluoroacetate) per<br />

kilogram bodyweight. In animals with liver glutathione levels 15% <strong>of</strong> normal increases in plasma and liver<br />

citrate levels after dosing with fluoroacetate were significantly greater than those <strong>of</strong> control animals.<br />

Cysteamine and N-acetylcysteine, like glutathione, partially prtoected aconitat hydratase from fluorocitrate<br />

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Appendix C<br />

inhibition in rat liver preparations but were unable to replace glutathione as a substrate for the<br />

defluorination <strong>of</strong> fluoroacetate in vivo. _______ The in vivo defluorination patterns <strong>of</strong> four mammal species<br />

with differing sensitivities to fluoroacetate did not indicate a direct relationship between tolerance and rate<br />

<strong>of</strong> defluorination and it as also suggested that a high level <strong>of</strong> activity <strong>of</strong> glutathione-S-transferase<br />

responsible for the defluorination <strong>of</strong> fluoroacetate is not the major mechanism for circumventing<br />

fluoroacetate toxicity in resistant mammals.<br />

Mead, R. J., Oliver, A. J., King, D. R., and Hubach, P. H. (1985). The co-evolutionary role <strong>of</strong> fluoroacetate<br />

in plant-animal interactions in Australia. Oikos 44, 55-60.<br />

Keywords: fluoroacetate/1080/occurrence in nature/tolerance/mammals/marsupials<br />

Abstract: Fluoroacetate-bearing species <strong>of</strong> Gastrolobium and Oxylobium occur in SW but not SE Australia.<br />

Populations <strong>of</strong> grey kangaroos (Macropus fuliginosus), bush rats (Rattus fuscipes) and rat kangaroos<br />

(Bettongia penicillata) whose ranges include these plants are highly resistant to fluoroacetate, while an<br />

island population <strong>of</strong> B. lesueur, separated from contact with fluoroacetate-bearing vegetation for at least<br />

7000 yr is moderately tolerant. The grey kangaroo includes these plants in its diet and it appears that the<br />

production <strong>of</strong> fluoroacetate as a protection against herbivore grazing pressure and the development <strong>of</strong><br />

genetic resistance to the toxin is a co-evolutionary event which has occurred in Western Australia. SE<br />

Australian populations <strong>of</strong> B. gaimardi and R. fuscipes are highly susceptible to fluoroacetate and it is<br />

suggested that R. fuscipes and Bettongia radiated from the east into Western Australia, the western<br />

populations evolving a degree <strong>of</strong> resistance dependent upon the extent <strong>of</strong> exposure to fluoroacetate-bearing<br />

vegetation. Eastern populations <strong>of</strong> M. fuliginosus are as resistant as western populations and it is suggested<br />

that the grey kangaroo evolved in Western Australia and spread eastward, retaining tolerance to<br />

fluoroacetate in the absence <strong>of</strong> specific selection pressure.<br />

Mead, R. J., Twigg, L. E., King, D. R., and Oliver, A. J. (1985). The tolerance to fluoroacetate <strong>of</strong><br />

geographically separated populations <strong>of</strong> the Quokka (Setonix brachyurus). Aust.Zool. 21, 503-511.<br />

Keywords: tolerance/fluoroacetate/occurrence in nature/marsupials/citrate<br />

Abstract: The tolerance to fluoroacetate <strong>of</strong> three geographically separated populations <strong>of</strong> the macropodid<br />

marsupial, the quokka (Setonix brachyurus) in southwestern Australia is compared in terms <strong>of</strong> elevation <strong>of</strong><br />

plasma citrate levels in response to dosing with 1080.<br />

The populations from mainland Western Australia and from Bald Island <strong>of</strong>f the south coast <strong>of</strong> W.A. are<br />

currently in contact with fluoroacetate-bearing plants. These populations have a much higher tolerance to<br />

fluoroacetate and are more genetically homogenous for the resistance than the population on Rottnest<br />

Island <strong>of</strong>f the west coast <strong>of</strong> Western Australia. The latter population has been isolated from contact with<br />

fluoroacetate-bearing vegetation from some 5,000-7,000 years, but is much more tolerant than are<br />

macropodids in southeastern Australia where fluoroacetate-containing plants are not known to occur.<br />

Mead, R. J., Feldwick, M. G., and Bunn, J. T. (1991). 1,3-difluoro-2-propanol: a potential replacement for<br />

1080 in fauna management programs in Australia. Wildlife research 18, 27-37.<br />

Keywords: 1,3-difluoro-2-propanol/1080/mode <strong>of</strong> action/rodents/treatment/antidote<br />

Abstract: Administration to rats <strong>of</strong> 100 mg per kilogram <strong>of</strong> 1,3-difluoro-2-propanol (DFP), the major<br />

ingredient <strong>of</strong> the pesticide Gliftor, resulted in citrate accumulation on the kidley after a 3-h lag pahse.<br />

Inhibition <strong>of</strong> aconitate hydratase in the kidney and symptoms typical <strong>of</strong> sodium fluoroacetate poisoning in<br />

DFP-intoxicated rats suggested metabolism <strong>of</strong> DFP to (-)erythr<strong>of</strong>luorocitrate. The conversion <strong>of</strong> DFP to the<br />

toxic metabolite was found to involve defluorination by a microsomal mixed-function oxidase in the liver,<br />

induced by phenobarbitone and inhibited by piperonyl butoxide. Administration to rats <strong>of</strong> pyrazole (90 mg<br />

per kg body weight) decreased the activity <strong>of</strong> the mixed-function oxidase-dependent defluorination <strong>of</strong> DFP.<br />

When administered to rats either 2 h before or 2 h after DFP (100 mg per kg body weight) it eliminated<br />

symptoms <strong>of</strong> poisoning, prevented citrate and fluoride accumulation, and decreased aconitate hydratase<br />

inhibition in the kidney. The antidotal properties <strong>of</strong> pyrazole, the mode <strong>of</strong> toxic action <strong>of</strong> (-<br />

)erythr<strong>of</strong>luorocitrate and the potential for DFP to replace 1080 in fauna management programs in Australia<br />

is discussed.<br />

Meads, M. Effect <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) in non-target invertebrates <strong>of</strong> Whitecliffs<br />

Conservation Area, Taranaki. <strong>Landcare</strong> <strong>Research</strong> Contract report LC9495, -15. 1994.<br />

Ref Type: Report<br />

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Appendix C<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/1080/invertebrates/non-target species/temperature/persistence in<br />

plants<br />

Abstract: Results show that insects are most affected and molluscs the least. In descending order the taxa<br />

most severly repressed were; Coleoptera, Collembola, Diptera, Hymenoptera, Orthoptera, Opiliones and<br />

earthworms. Mollusca, Amphipoda, Acarina and Araneida showed no change. The significant drop in<br />

insect numbers after heavy rain suggests stongly that the control plots had become contaminated with 1080.<br />

1080 adsorbs to cellulosic leaf litter, and persists in the litter for at least three months. Results show that the<br />

insects associated witht he breakdown <strong>of</strong> leaf-litter are the most severly affected by 1080. Breakdown <strong>of</strong><br />

1080 can take more than 120 days at a temperature <strong>of</strong> 5 degrees celcius. Tests showed that after 113 days at<br />

5 degrees, 1080 still contained a concentration <strong>of</strong> 1.5 mMol/L. In the forest the average tempertaure fot he<br />

leaf litter in winter was at 5 degrees. Comparison <strong>of</strong> the Whitecliffs data with that <strong>of</strong> other lowland<br />

podocarp/broadleaf forests over one year, shows that 1080 has a severe impact on many other invertebrates.<br />

At Whitecliffs, insect larvae, comprising coleoptera, hymenoptera, diptera and lepidoptera dropped<br />

dramatically from July through to October, then stabilised for the remainder <strong>of</strong> the year at the crash level.<br />

Insect larvae in other forests followed the normal pattern <strong>of</strong> continual rise form July until the onset <strong>of</strong> the<br />

following winter.<br />

Meenken, D and Johnson, B. Effects on water quality <strong>of</strong> 1080 possum poisoning operation by manual bait<br />

application. 00/1, 1-23. 2000.<br />

Ref Type: Report<br />

Keywords: 1080/poisoning<br />

Meenken, D, Johnson, B., and Eason, C. T. Effect <strong>of</strong> 1080 Hand-baiting on Water Quality. 00/1, 1-23.<br />

2000. Wellington, Wellington Regional Council.<br />

Ref Type: Report<br />

Keywords: 1080/persistence in water/baits/ground control/poisoning<br />

Abstract: Executive Summary<br />

A substantial database exists on water quality after aerial 1080 possum and rabbit poisoning operations<br />

in New Zealand (see Appendix 1.). However, no water quality investigations have been undertaken to<br />

assess the effect <strong>of</strong> a ground-based 1080 poisoning operation. This is due to the perception that manual<br />

application <strong>of</strong> toxic bait is less likely to result in significant quantities <strong>of</strong> bait entering watercourses<br />

compared to aerial application.<br />

A meeting with Dr Gillian Durham, the then Director <strong>of</strong> Public Health, at the Ministry <strong>of</strong> Health on 19<br />

February 1999, discussed model permit conditions, in particular the requirements for drinking water<br />

supplies and monitoring. At the meeting it was agreed that the perceived risk from ground applications <strong>of</strong><br />

1080 was much lower than from aerial applications and that was why statutory requirements were much<br />

less involved for the former. It was agreed that the Wellington Regional Council (WRC) would monitor a<br />

ground 1080 operation and report on water quality effects, so that Ministry could promulgate national<br />

advice on the appropriate approach to ground application <strong>of</strong> 1080.<br />

The WRC subsequently designed a study to investigate a "worst case" scenario. A 14-ha catchment in<br />

the Wairarapa was poisoned with 1080 cereal baits (0.15% 1080 w/w) on 26 November 1999. Baits were<br />

hand-broadcast at approximately 10 kg/ha.<br />

Duplicate water samples were collected during and after bait application, and during subsequent rainfall<br />

events. Sample collection was automated using a Manning Sampler, with sampling intervals set for 15 or<br />

30 minutes.<br />

A total <strong>of</strong> 52 samples were analysed for 1080 by the <strong>Landcare</strong> <strong>Research</strong> laboratory at Lincoln. None<br />

contained detectable concentrations <strong>of</strong> 1080.<br />

This study provides support for the assertion that ground-based 1080 possum poisoning operations do<br />

not have a measurable effect on water quality.<br />

Meenken, D. and Eason, C. T. (1995). Effects on water quality <strong>of</strong> a possum (Trichosurus vulpecula)<br />

poisoning operation using toxin 1080 (sodium mon<strong>of</strong>luoroacetate). New Zealand journal <strong>of</strong> marine and<br />

freshwater research 29, 25-28.<br />

Keywords: persistence in water/1080<br />

Abstract: A possum (Trichosurus vulpecula) control operation using aerially sown baits containing sodium<br />

mon<strong>of</strong>luoroacetate (1080) was conducted in June 1993 in and adjoining Tararua Forest Park, New Zealand.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

In total, 66 water samples from eight sites collected over a period <strong>of</strong> 4 months were analysed for residual<br />

1080 potentially resulting from the control operation. No 1080 was detected in any <strong>of</strong> the samples<br />

(quantifiable level 0.0003 mg l/sup -1 ).<br />

Meenken, D. and Booth, L. H. (1997). The risk to dogs <strong>of</strong> poisoning from sodium mon<strong>of</strong>luoroacetate<br />

(1080) residues in possum (Trichosurus vulpecula). New Zealand journal <strong>of</strong> agricultural research 40, 573-<br />

576.<br />

Keywords: secondary poisoning/mammals/non-target species/persistence in<br />

animals/1080/stomach/dogs/scavenger<br />

Mehlman, M. A. (1968). Inhibition <strong>of</strong> pyruvate carboxylation by fluorocitrate in rat kidney mitochondria.<br />

The Journal <strong>of</strong> Biological Chemistry 243, 1919-1925.<br />

Keywords: inhibition/fluorocitrate/kidney/biochemistry/rodents<br />

Abstract: Rat kidney mitochondria, in the presence <strong>of</strong> ATP, Pi and magnesium ions, converted pyruvate<br />

and bicarbonate to malate, fumarate and citrate, and, in the presence <strong>of</strong> glutamate, also to aspartate. The<br />

addition <strong>of</strong> fluorocitrate strongly inhibited pyruvate utilisation and 14CO2 incorporation into organic acids.<br />

The inhibition <strong>of</strong> 14CO2 incorporation into organic acids in the presence <strong>of</strong> fluorocitrate appeared to be<br />

caused by malonyl coenzyme A produced by fluorocitrate stimulation <strong>of</strong> acetyl-CoA carboxylase.<br />

Meikle, L., Eason, C. T., Gooneratne, S. R., and Arthur, D. (1996). The short and long-term effects <strong>of</strong> a<br />

single exposure <strong>of</strong> 1080 in sheep September 1994 to September 1995 : 1 year report. (Manaaki Whenua -<br />

<strong>Landcare</strong> <strong>Research</strong>: Lincoln.)<br />

Keywords: acute toxicity/non-target species/mammals/pathology/diagnosis/1080/lethal dose/heart<br />

Abstract: Objectives: To establish whether the diagnosis <strong>of</strong> acute and long-term poisoning with 1080 in<br />

sheep can be improved; to determine any long term effects <strong>of</strong> acute 1080 poisoning on the health,<br />

productivity and survival <strong>of</strong> sheep.<br />

Conclusions: Phase 1 - Acute and Sub-acute effects <strong>of</strong> 1080 All the sheep that died <strong>of</strong> 1080 poisoning died<br />

within 4 days <strong>of</strong> exposure. There were no reliable bioindicators <strong>of</strong> 1080 exposure in sheep that survived<br />

the first 4 days after exposure. Gross and microscopic pathology <strong>of</strong> the lungs provides a good indicator in<br />

sheep dying from 1080 poisoning. Lungs were wet and heavy with clear fluid draining from the cut<br />

surface. The trachea was usually filled with frothy liquid. Pulmonary congestion and oedema was diffuse,<br />

affecting all lobes equally in all sheep that died. Cardiac damage was typified by necrosis and<br />

mineralisation within the mycoardium <strong>of</strong> the left ventricle in half <strong>of</strong> the sheep that died <strong>of</strong> 1080. there were<br />

no abnormalities in the heart or lungs <strong>of</strong> sheep that were killed 14 days after exposure. Residues <strong>of</strong> 1080 in<br />

blood, stomach, or muscle, and elevated serum citrate concentrations in the blood can be used as short-term<br />

indicators <strong>of</strong> 1080 exposure. Changes in electrocardiogram characteristics can be detected for 36 h after<br />

1080 exposure. An increase in heart rate can be measured for 48 h after exposure. Phase 2 - Long-term<br />

effects <strong>of</strong> a near lethal dose <strong>of</strong> 1080 If death does not occur within the first four days <strong>of</strong> exposure to a<br />

single dose <strong>of</strong> 1080, subsequent adverse effects on the health <strong>of</strong> sheep are unlikely.<br />

Meldrum, G. K. and Bignell, J. T. (1957). The use <strong>of</strong> sodium fluoroacetate (1080) for the control <strong>of</strong> the<br />

rabbit in Tasmania. The Australian Veterinary Journal 33, 186-196.<br />

Keywords: fluoroacetate/1080/rabbits/field efficacy/mode <strong>of</strong> action<br />

Mendz, G. L., Lim, T. N., and Hazell, S. L. (1993). Fluorinated probes to measure carboxylesterase<br />

activities using 19 F NMR spectroscopy: Application to erythrocytes and Helicobacter pylori. Archives <strong>of</strong><br />

biochemistry and biophysics 305, 252-260.<br />

Keywords: NMR<br />

Abstract: Eight fluorinated compounds were tested as putative probes to measure carboxylesterase activity<br />

employing 19 F nuclear magnetic resonance spectroscopy. The method takes advantage <strong>of</strong> the sensitivity <strong>of</strong><br />

fluorine resonances to the changes in the chemical bonding in the covalent structures where they are<br />

located. Determination <strong>of</strong> the kinetic parameters <strong>of</strong> ethyl fluoroacetate and diethyl fluoromalonate in<br />

hemolysates showed that these probes were well suited to study carboxylesterase activities in complex<br />

systems. The potential <strong>of</strong> these probes for noninvasive applications was demonstrated in measurements <strong>of</strong><br />

carboxylesterase kinetic parameters in intact erythrocytes. The presence <strong>of</strong> carboxylesterases was<br />

established in several strains <strong>of</strong> the bacterium Helicobacter pylori employing 19 F nuclear magnetic<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

resonance spectroscopy, and the kinetic parameters <strong>of</strong> these enzymes for ethyl fluoroacetate and diethyl<br />

fluoromalonate were measured.<br />

Menn, J. J. and Still, G. G. (1977). Metabolism <strong>of</strong> Insecticides and Herbicides in Higher Plants. CRC<br />

Critical Reviews in Toxicology 5, 1-21.<br />

Keywords: metabolism<br />

Menon, K. I., Feldwick, M. G., Noakes, P. S., and Mead, R. J. (2001). The mode <strong>of</strong> toxic action <strong>of</strong> the<br />

pesticide gliftor: the metabolism <strong>of</strong> 1,3-difluoroacetone to (-)-erythro-fluorocitrate. Journal <strong>of</strong> Biochemical<br />

and Molecular Toxicology 15, 47-54.<br />

Keywords: metabolism/mode <strong>of</strong> action/1,3-difluoro-2-propanol/kidney/rats/fluoride/citrate/4methylpyrazole/aconitase/enzyme<br />

Abstract: The biochemical toxicology <strong>of</strong> 1,3-difluoroacetone, a known metabolite <strong>of</strong> the major ingredient<br />

<strong>of</strong> the pesticide Gliftor (1,3-difluoro-2-propanol), was investigated in vivo and in vitro. Rat kidney<br />

homogenates supplemented with coenzyme A, ATP, oxaloacetate, and Mg2+ converted 1,3-difluoroacetone<br />

to (-)-erythro-fluorocitrate in vitro. Administration <strong>of</strong> 1,3-difluoroacetone (100 mg kg(-1) body weight) to<br />

rats in vivo resulted in (-)-erythro-fluorocitrate synthesis in the kidney, which was preceded by an elevation<br />

in fluoride levels and followed by citrate accumulation. Animals dosed with 1,3-difluoroacetone did not<br />

display the 2-3 hour lag phase in either (-)-erythro-fluorocitrate synthesis or in citrate and fluoride<br />

accumulation characteristic <strong>of</strong> animals dosed with 1,3-difluoro-2-propanol. We demonstrate that the<br />

conversion <strong>of</strong> 1,3-difluoro-2-propanol to 1,3-difluoroacetone by an NAD+-dependent oxidation is the ratelimiting<br />

step in the synthesis <strong>of</strong> the toxic product, (-)-erythro-fluorocitrate from 1,3-difluoro-2-propanol.<br />

Prior administration <strong>of</strong> 4-methylpyrazole (90 mg kg(-1) body weight) was shown to prevent the conversion<br />

<strong>of</strong> 1,3-difluoro-2-propanol (100 mg kg(-1) body weight) to (-)-erythro-fluorocitrate in vivo and to eliminate<br />

the fluoride and citrate elevations seen in 1,3-difluoro-2-propanol-intoxicated animals. However,<br />

administration <strong>of</strong> 4-methylpyrazole (90 mg kg(-1) body weight) to rats 2 hours prior to 1,3-difluoroacetone<br />

(100 mg kg(-1) body weight) was ineffective in preventing (-)-erythro-fluorocitrate synthesis and did not<br />

diminish fluoride or citrate accumulation in vivo. We conclude that the prophylactic and antidotal<br />

properties <strong>of</strong> 4-methylpyrazole seen in animals treated with 1,3-difluoro-2-propanol derive from its<br />

capacity to inhibit the NAD+-dependent oxidation responsible for converting 1,3-difluoro-2-propanol to<br />

1,3-difluoroacetone in the committed step <strong>of</strong> the toxic pathway<br />

Merks, P. F. and Calver, M. C. (1989). The effect <strong>of</strong> ant activity on meat baits impregnated with sodium<br />

mon<strong>of</strong>luoroacetate (compound 1080) used for the control <strong>of</strong> dingoes and wild dogs. Australian Rangeland<br />

Journal 11, 83-87.<br />

Keywords: baits/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/dogs/bait degradation/invertebrates<br />

Abstract: Wild dog and dingo baits impregnated with the toxin 1080 and exposed at two different sites in<br />

the field suffered signficant reduction in weight compared with controls as a result <strong>of</strong> ant activity. In one<br />

case a bait was completely destroyed in five days, while others were reduced in weight by over 70% during<br />

the same period. Sun-drying <strong>of</strong> baits for 48h before laying did not significantly reduce damage by ants. Ant<br />

activity may detoxify baits before they are taken by wild dogs.<br />

Meyer, J. J. M. and Grobbelaar, N. (1990). The determination, uptake and transport <strong>of</strong> fluoroacetate in<br />

Dichapetalum cymosum. Journal <strong>of</strong> plant physiology 135, 546-549.<br />

Keywords: occurrence in nature/high-performance liquid chromatography/fluoroacetate<br />

Meyer, J. J. M., Grobbelaar, N., and Steyn, P. L. (1990). Fluoroacetate-metabolizing pseudomonad isolated<br />

from Dichapetalum cymosum. Applied and environmental microbiology 56, 2152-2155.<br />

Keywords: metabolism/occurrence in nature<br />

Meyer, J. J. M. and Grobbelaar, N. (1991). Fluoroacetate degradation by Dichapetalum cymosum. Journal<br />

<strong>of</strong> plant physiology 138, 122-124.<br />

Keywords: fluoroacetate/degradation/persistence in plants/occurrence in nature/bacteria<br />

Abstract: The fluoroacetate-containg plant, Dichapetalum cymosum, is capable <strong>of</strong> releasing CO2 from<br />

fluoroacetate. Fluoroacetate is more readily degraded by the old than the young leaves <strong>of</strong> the plant. An<br />

aseptic callus culture <strong>of</strong> D. cymosum is also capable <strong>of</strong> degrading fluoroacetate albeit at a much lower rate<br />

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Appendix C<br />

than the leaves <strong>of</strong> the plant. Inoculation fo the cells with Psuedomonas cepacia isolated from the plant<br />

increased the rate <strong>of</strong> CO2 release from fluoroacetate about five-fold.<br />

Meyer, J. J. M. and O'Hagan, D. (1992). Conversion <strong>of</strong> fluoropyruvate to fluoroacetate by Dichapetalum<br />

cymosum. Phytochemistry 31, 499-501.<br />

Keywords: fluoroacetate/fluoride/occurrence in nature/biosynthesis<br />

Abstract: Studies utilising 19F NMR spectroscopy have demonstrated that callus culture <strong>of</strong> Dichapetalum<br />

cymosum can efficiently convert fluoropyruvate to fluoroacetate, fluorolactate and fluoride. The conversion<br />

<strong>of</strong> fluoropyruvate to fluoroacetate is unusual in a biological system and the possibel role <strong>of</strong> fluoropyruvate<br />

in the biosynthesis <strong>of</strong> fluoroacetate is discussed.<br />

Meyer, J. J. M., Grobbelaar, N., Vleggaar, R., and Louw, A. I. (1992). Fluoracetyl-coenzyme A hydrolaselike<br />

activity in Dichapetalum cymosum. Journal <strong>of</strong> plant physiology 139, 369-372.<br />

Keywords: occurrence in nature/biosynthesis/enzyme<br />

Abstract: The presence <strong>of</strong> this enzyme in D. cymosum probably explains why this plant is not poisoned by<br />

its production <strong>of</strong> fluoroacetate.<br />

Meyer, J. J. M. and O'Hagan, D. (1992). Conversion <strong>of</strong> 3-fluoropyruvate to fluoroacetate by cell-free<br />

extracts <strong>of</strong> Dichapetalum cymosum. Phytochemistry 31 , 2699-2701.<br />

Keywords: fluoroacetate/biosynthesis/persistence in plants/occurrence in nature<br />

Abstract: A cell-free extract derived from callus tissue <strong>of</strong> Dichapetalum cymosum was able to oxidatively<br />

decarboxylate fluoropyruvate to give fluoroacetate. By employing sodium monomethyl acetylphosphate, an<br />

inhibitor <strong>of</strong> the pyruvate dehydrogenase complex (PDC) fluoroacetate production was increased and it was<br />

demonstrated unambiguously that PDC is not responsible for this transformation in D. cymosum.<br />

Meyer, J. J. M. Fluoroacetate metabolism <strong>of</strong> Dichapetalum cymosum. 1992. University <strong>of</strong> Pretoria (South<br />

Africa)Editor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: fluoroacetate/metabolism/high-performance liquid chromatography/liquid<br />

chromatography/bacteria/enzyme/occurrence in nature<br />

Abstract: A fast and sensitive method was developed for the determination <strong>of</strong> fluoroacetate in<br />

Dichapetalum cymosum using high-performance liquid chromatography. The highest concentrations <strong>of</strong><br />

fluoroacetate were found in the immature seeds, flowers and young leaves <strong>of</strong> the plant. The young leaves<br />

are more toxic than the older leaves. Foliarly applied fluoroacetate is also more readily accumulated by the<br />

young than by the older leaves <strong>of</strong> D. cymosum. Fluoroacetate can be taken up by the roots <strong>of</strong> D. cymosum<br />

and be transported to the leaves. It was, however, demonstrated in this study that aseptically grown D.<br />

cymosum seedlings, as well as an aseptic callus culture <strong>of</strong> the plant, is capable <strong>of</strong> producing fluoroacetate.<br />

A pseudomonad was isolated from D. cymosum and identified as Pseudomonas cepacia. It was established<br />

that an isolate <strong>of</strong> this bacterium could grow in fluoroacetate enriched solutions without any reduction in<br />

growth rate. This bacterium is capable <strong>of</strong> defluorinating fluoroacetate and also <strong>of</strong> liberating CO2 from<br />

fluoro-acetate. It seems as though the synthesis <strong>of</strong> N-methyl alanine and the occurrence <strong>of</strong> N- methyl serine<br />

in D. cymosum, is a result <strong>of</strong> the symbiosis between the plant and its endophyte. An aseptic callus culture<br />

<strong>of</strong> D. cymosum is capable <strong>of</strong> degrading fluoroacetate albeit at a much lower rate than the leaves <strong>of</strong> the<br />

plant. By contaminating the callus with P. cepacia, isolated from the plant, the rate <strong>of</strong> CO2 release from<br />

fluoroacetate was increased about five fold. A D. cymosum crude mitochondrial enzyme extract can release<br />

CoASH from fluoroacetyl-CoA at a rate <strong>of</strong> 29.5 nmoles/min/mg protein, indicating the presence in the<br />

extract <strong>of</strong> an enzyme which is probably fluoroacetyl-CoA hydrolase. This enzyme could not use acetyl-<br />

CoA as a substrate. The presence <strong>of</strong> the fluoroacetyl-CoA hydrolase-like enzyme in D. cymosum together<br />

with the ability <strong>of</strong> the plant and its endophyte to degrade the fluoroacetate, helps to explain why D.<br />

cymosum is not poisoned by the high fluoroacetate concentrations which occur in the plant at times<br />

Meyer, J. J. M. (1994). Fluoroacetate metabolism <strong>of</strong> Pseudomonas cepacia. In 'Proceedings <strong>of</strong> the Science<br />

Workshop on 1080, 12-14 December 1993, Christchurch, New Zealand'. (A. A. Seawright and C. T.<br />

EasonEds. ) pp. 54-58. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: metabolism/occurrence in nature/NMR/1080<br />

Abstract: Pseudomonas cepacia was isolated from the stems and seeds <strong>of</strong> the fluoroacetate accumulating<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

plants Dichapetalum braunii and D. cymosum. The fluoroacetate concentration in the seeds <strong>of</strong> D. braunii<br />

was 8000 ppm. this is probably this highest concentration <strong>of</strong> fluoroacetate yet found in a living organism P.<br />

cepacia isolated from these extremely toxic seed can break down fluoroacetate and is able to grow in<br />

fluoroacetate concentrations up to 10mM. It metabolises fluoroacetate to several other fluorinated<br />

compounds, including fluorociatrate and fluoroglutamate. It is proposed to fluoroacetate enters the citric<br />

acid cycle as fluotoacetyl-CoA and is then converted to fluorocitrate, fluoroaconitate, 4-fluoro-isocitrate<br />

and 4 fluoro-2-ketoglutarate. The keto acid then undergoes a transamination reaction to form 4fluoroglutamate.<br />

P.cepacia isolated from the stems <strong>of</strong> D. cymosum only defluorinated fluoroacetate and did not metabolise it<br />

further, as was the case with the D.braunii isolate. The deflourination rate <strong>of</strong> the D.cymosum isolate was<br />

about five times faster than that <strong>of</strong> the D.braunii isolate.<br />

Meyer, J. J. M. and van Rooyen, S. W. (1994). Fluoroacetate metabolism <strong>of</strong> a bacterium from<br />

Dichapetalum braunii. In 'Plant-associated toxins : agricultural, phytochemical and ecological aspects'. (S.<br />

M. Colegate and P. R. DorlingEds. ) pp. 457-461. (CAB International, Wallingford:<br />

Keywords: fluoroacetate/bacteria/metabolism/occurrence in nature/defluorination<br />

Meyer, J. J. M. and van Rooyen, S. W. (1996). Genetically transformed Bacillus subtilis with<br />

defluorinating ability. South African journal <strong>of</strong> botany 62, 65-66.<br />

Keywords: metabolism/occurrence in nature/NMR/bacteria/defluorination/biosynthesis<br />

Abstract: A 16-18 kb pairs plasmid was isolated from the fluoroacetate-metabolizing bacterium,<br />

Pseudomonas cepacia. This strain <strong>of</strong> P. cepacia is a natural symbiont <strong>of</strong> the fluoroacetate-producing plant,<br />

Dichapetalum cymosum (Hook.) Engl. After transformation <strong>of</strong> B. subtilis with this plasmid, the<br />

transformed bacterium was also able to defluorinate fluoroacetate when cultured in a fluoroacetate-enriched<br />

medium. The extent <strong>of</strong> defluorination was measured by a fluorine-specific electrode as well as by 19 Fnuclear<br />

magnetic resonance spectroscopy.<br />

Meyer, M. and O'Hagan, D. (1992). Rare fluorinated natural products. Chemistry in Britain 28, 785-788.<br />

Keywords: metabolism/occurrence in nature/fluoroacetate/invertebrates<br />

Abstract: In nature organ<strong>of</strong>luorine metabolites are few and far between. Fluoroacetate is found in some<br />

plants and in one bacterial source. However, the remaining metabolites are normally unique to one<br />

particular organism.<br />

Meyer, S. G. E. (1978). Effects <strong>of</strong> heat, cold, anaerobiosis and inhibitors on metabolite concentrations in<br />

larvae <strong>of</strong> Callitroga macellaria. Insect Biochemistry 8, 471-477.<br />

Keywords: metabolism/inhibition/cyanide/citric acid/aconitase/invertebrates<br />

Abstract: Changes in different metabolite concentrations in non-feeding larvae <strong>of</strong> Cochliomyia macellaria<br />

(F.) (Callitroga macellaria) were investigated in their dependence on heat, cold, anaerobiosis and<br />

inhibitors. With the exception <strong>of</strong> dinitrophenol, all factors inhibited the oxidative metabolism to some<br />

extent. This was seen by the increased production <strong>of</strong> lactate, pyruvate and alanine. Polyolformation was<br />

correlated with the inhibition <strong>of</strong> the electron transport system whilst polyolphosphate formation depended<br />

on additional factors. Tests with 14Cl and 14C 6 -glucose showed the greater importance <strong>of</strong> the hexose-monophosphate shunt during anaerobiosis,<br />

cyanide and fluoroacetic acid blocked metabolism. After the application <strong>of</strong> fluoroacetic acid the concentrations <strong>of</strong> malate, asparagine, aspartate and citric acid were<br />

determined, and it was possible to suggest a diagram <strong>of</strong> metabolism during fluoroacetic acid action which shows a bypass <strong>of</strong> the aconitase step and the possibility <strong>of</strong><br />

an oxidative ATP-production at a low rate<br />

Middendorf, P. J. and Dusenbery, D. B. (1993). Fluoroacetic acid is a potent and specific inhibitor <strong>of</strong><br />

reproduction in the nematode Caenorhabditis elegans. Journal <strong>of</strong> nematology 25, 573-577.<br />

Keywords: mode <strong>of</strong> action/invertebrates/reproductive effects/aconitase/fluorocitrate<br />

Miller, C. J. and Anderson, S. (1992). Impacts <strong>of</strong> aerial 1080 poisoning on the birds <strong>of</strong> Rangitoto Island,<br />

Hauraki Gulf, New Zealand. New Zealand journal <strong>of</strong> ecology 16, 103-107.<br />

Keywords: non-target species/birds/aerial control/1080/poisoning/poison/possums/wallaby/mammals<br />

Abstract: Bird popualtions were monitored for one year (October 1990-October 1991) to determine whether<br />

the 1080 poison used to eradicate possums and wallabies on Rangitoto Island had had any detrimental<br />

effects on them. There was no significant decline in bird numbers recorded immediately after poisoning,<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

with four species increasing in abundance (P


1080 Reassessment Application October 2006<br />

Appendix C<br />

Milne, L., Fisher, P., O'Connor, C. E., Wright, G. R. G., and Eason, C. T. Potential human exposure to<br />

vertebrate pesticides through contaminated meat or milk. LCR0203/010, -18. 2002. <strong>Landcare</strong> <strong>Research</strong><br />

Lincoln.<br />

Ref Type: Report<br />

Keywords: 1080/blood/brodifacoum/cholecalciferol/cyanide/humans/liver/muscle/persistence in<br />

animals/secondary poisoning<br />

Abstract: • Brodifacoum was detected in the blood <strong>of</strong> high-dose ewes at 2 days and 4 days after<br />

dosing, but not from 8 days onwards. Five <strong>of</strong> eight high-dose ewes had detectable concentrations <strong>of</strong><br />

brodifacoum in their milk 2 days after dosing. There was no brodifacoum detected in any ewe's milk from 4<br />

days after dosing.<br />

• At 4 hours after dosing, the concentration <strong>of</strong> 1080 in ewes' blood was approximately 30 times<br />

higher than in milk. No ewes had detectable 1080 in their milk at 72 hours after dosing.<br />

• At 10 days after dosing, concentrations (mean SE) <strong>of</strong> brodifacoum in possum muscle and liver<br />

were 0.06 0.02 g/g and 0.60 0.12 g/g respectively. Brodifacoum concentrations in both possum muscle<br />

and liver were not significantly affected by cooking.• At 8 hours after dosing, concentrations (mean SE) <strong>of</strong><br />

1080 residue in possum muscle and liver were 0.64 0.14 g/g and 0.40 0.05 g/g respectively. 1080<br />

concentrations in both possum muscle and liver were not significantly affected by cooking.<br />

• At 5 minutes after dosing, concentrations (mean SE) <strong>of</strong> cyanide in possum muscle and liver were<br />

0.50 0.47 g/g and 1.60 0.56 g/g respectively. This was suggestive <strong>of</strong> a cooking effect, however the<br />

reduction <strong>of</strong> cyanide concentrations in possum liver and muscle were not statistically significant.<br />

• At 2 days after dosing, concentrations (mean SE) <strong>of</strong> cholecalciferol in possum muscle and liver<br />

were 0.04 0.01 g/g and 1.30 0.42 g/g respectively. Cholecalciferol concentrations in possum liver were<br />

reduced by cooking.<br />

• Brodifacoum and 1080 can be transferred to milk and are likely to detectable for 4 and 6 days,<br />

respectively.<br />

• Brodifacoum, 1080, cyanide and cholecalciferol can be transferred to liver and muscle tissue.<br />

• Risk to human consumers from 1080, brodifacoum or cyanide in muscle or liver is not likely to<br />

significantly reduced by cooking.<br />

• Risk to human consumers from cholecalciferol in liver is likely to be reduced by cooking.<br />

Minnaar, P. P., McCrindle, R. I., Botha, C. J., and Naudé, T. W. (2000). Investigation <strong>of</strong> biological samples<br />

for mon<strong>of</strong>luoroacetate and Dichapetalum cymosom poisoning in southern Africa. Onderstepoort journal <strong>of</strong><br />

veterinary research 67, 27-30.<br />

Keywords: diagnosis<br />

Minnaar, P. P., Swan, G. E., McCrindle, R. I., de Beer, W. H. J., and Naudé, T. W. (2000). A highperformance<br />

liquid chromatographic method for the determination <strong>of</strong> mon<strong>of</strong>luoroacetate. Journal <strong>of</strong><br />

chromatographic science 38, 16-20.<br />

Keywords: high-performance liquid chromatography<br />

Abstract: A simple isocratic high-performance liquid chromatographic (HPLC) method for the quantitative<br />

analysis <strong>of</strong> mon<strong>of</strong>luoroacetic acid (MFA), the toxic substance <strong>of</strong> Dichapetalum cymosum, in plant material,<br />

rumen contents (gastric contents), and liver samples is described. A suitable HPLC column that gives<br />

optimum sensitivity, accuracy, precision, and separation <strong>of</strong> MFA is identified. A C-610 organic acid<br />

analysis column at ambient temperature with 0.02M H3P)4 as an eluent and ultraviolet detection at 210 nm<br />

is utilised to quantitate MFA. Using the method, the average percentage recovery in plant material, bovine<br />

liver, and rumen samples is 94.8%, and a detection limit <strong>of</strong> 12 ug/L is achievable.<br />

Minnaar, P. P., McCrindle, R. I., Naude, T. W., and Botha, C. J. (2000). Investigation <strong>of</strong> biological samples<br />

for mon<strong>of</strong>luoroacetate and Dichapetalum cymosum poisoning in southern Africa. Onderstepoort journal <strong>of</strong><br />

veterinary research 67, 27-30.<br />

Keywords: mon<strong>of</strong>luoroacetate/poisoning/liquid chromatography/stomach/temperature/occurrence in nature<br />

Abstract: A new high performance liquid chromatography method was developed for measuring<br />

mon<strong>of</strong>luoroacetate (MFA) for a variety <strong>of</strong> biological samples. The method was used in the laboratory over<br />

24 months to investigate suspected MFA poisoning in 50 samples including stomach contents <strong>of</strong> cheetah<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

(1), bird (1), horse (1), man (2), sheep (2), cat (7), dog (13) and cattle (17), and in bait (5) and water (1).<br />

MFA was detected in 66% <strong>of</strong> samples from cases <strong>of</strong> suspected poisoning, reflecting the extent <strong>of</strong> the<br />

problem. Stability <strong>of</strong> MFA in samples was also determined so as to have a time-bound baseline for the<br />

acceptance <strong>of</strong> samples submitted. Level <strong>of</strong> MFA decreased with time so that, after 14 days at room<br />

temperature, only 50% <strong>of</strong> the spiked dose could be identified. It is suggested that samples be examined<br />

within 7 days <strong>of</strong> death if they cannot be kept frozen<br />

Misustova, J., Novak, L., and Hosek, B. (1969). Influence <strong>of</strong> lowered environmental temperature on<br />

metabolic and lethal effects <strong>of</strong> sodium fluoroacetate in mice. Physiologia bohemoslovaca 18, 319-324.<br />

Keywords: temperature/sodium fluoroacetate/fluoroacetate/mode <strong>of</strong> action<br />

Abstract: The effect <strong>of</strong> a lowered environmental temperature on the manifestations <strong>of</strong> the effect <strong>of</strong> sodium<br />

fluoroacetate (FAc) was studied in male strain H mice aged 9-12 weeks. It was found that only a small<br />

decrease in the environmental tempertaure (from 23 degrees Celcius to 17 degrees) during FAc intoxication<br />

(5 mg/kg bodyweight) induced further depression <strong>of</strong> the already lowered level <strong>of</strong> respiratory excahnge and<br />

body temperature. Simultaneously it enhanced the toxic effect <strong>of</strong> the given dose <strong>of</strong> FAc. Mortality after 5<br />

mg FAc/kg rose from 3% (at 23 degrees C) to 47% (at 17 degrees C) while LD50/3 days fell on expsoure to<br />

cold from 12.1 mg/kg to 5.16 mg/kg. These results cna be used when studying the radioproective effect <strong>of</strong><br />

FAc, to fix a suitable environmental temperature for the experiments.<br />

Misustova, J. and Novak, L. (1970). The importance <strong>of</strong> hypothermy in the mechanism <strong>of</strong> the protective<br />

action <strong>of</strong> sodium fluoroacetate. In 'Radiation protection and sensitization : Proceedings, Instituto Superiore<br />

di Sanita, Rome, 6-8 May 1969'. (H. Moroson and M. QuintilianiEds. ) pp. 344-347. (Taylor & Francis:<br />

London.)<br />

Keywords: metabolism/sodium fluoroacetate/fluoroacetate/temperature<br />

Abstract: The role <strong>of</strong> temperature in the mechanism <strong>of</strong> protective action <strong>of</strong> sodium fluoroacetate (FAc), was<br />

studied on H-strain males, mice, aged 9-12 weeks. After FAc application (5 mg/kg body weight) animals<br />

were kept at temperatures 17º, 23º, and 30ºC and irradiated at these temperatures with 800 R. Change in<br />

the ambient temperature in the course <strong>of</strong> intoxication by FAc significantly influences the body temperature<br />

<strong>of</strong> experimental animals, but does not affect the degree <strong>of</strong> protection or its time course. These results<br />

correspond with the opinion that the degree <strong>of</strong> protection by FAc is determined by the consequences <strong>of</strong><br />

blocking <strong>of</strong> aconitase, which is proportional to FAc dose, rather than hypothermy.<br />

Misustova, J., Hosek, B., and Kautska, J. (1980). Characterization <strong>of</strong> the protective effect <strong>of</strong> radioprotective<br />

substances by means <strong>of</strong> long-term changes in oxygen consumption. Strahlentherapie 156, 790-794.<br />

Abstract: A comparison <strong>of</strong> long-term hypothermic effects <strong>of</strong> radioprotective substances and their protective<br />

effectiveness was carried out in mice after acute and prolonged irradiation. As radioprotective substances<br />

were used AET, cystamine, serotonine, 5-methoxytryptamine, cysteamine-S-phosphate, sodium<br />

fluoroacetate and some double combinations <strong>of</strong> the substances. The irradiation was carried out with dose<br />

rates 38.3 and 612.5 mGy/min, the hypothermic reaction was evaluated according to total oxygen<br />

consumption, measured during 5 hours after the drug administration. The results demonstrated the<br />

existence <strong>of</strong> a correlation between the suppression <strong>of</strong> metabolic processes and both short-term and longterm<br />

protective effectiveness <strong>of</strong> radioprotective substances. The protective effectiveness <strong>of</strong> a drug is the<br />

higher, the greater decrease <strong>of</strong> oxygen consumption is induced by this substance in the investigated time<br />

interval. An analogous dependence was also demonstrated between the duration <strong>of</strong> hypothermic and<br />

radioprotective effects. The found correlation is valid for both acute and prolonged irradiation (correlation<br />

coefficient 0.79-0.87; p


1080 Reassessment Application October 2006<br />

Appendix C<br />

decrease the immediate predation pressure on native wildlife and rabbits (Oryctolagus cuniculus).<br />

Observed decreases in bovine tuberculosis reactor rates in deer and cattle herds after some poisoning<br />

operations may therefore result from killing <strong>of</strong> non-target mammals, especially ferrets, rather than possums.<br />

Moller, H., Clapperton, B. K., and Fletcher, D. J. (1997). Density <strong>of</strong> rabbits (Oryctolagus cuniculus L.) in<br />

the Mackenzie Basin, South Island, New Zealand. New Zealand journal <strong>of</strong> ecology 21, 161-167.<br />

Keywords: rabbits/1080/baits/poisoning/efficacy/predators/secondary poisoning<br />

Abstract: The density <strong>of</strong> rabbits (Oryctolagus cuniculus) in the modified tussock grasslands <strong>of</strong> the<br />

Mackenzie Basin, South Island, New Zealand, in August-September 1991 was determined within 26 one-ha<br />

quadrats spread over 1000 ha. The area was poisoned with 1080 [sodium fluoroacetate]-carrot baits and<br />

dead and live rabbits counted. The overall kill rate was 93%. Wide variability in rabbit densities amongst<br />

the quadrats was correlated with burrow density, but vegetation was not a significant predictor <strong>of</strong> rabbit<br />

numbers. High density quadrats were not all spatially clumped together. Variation amongst quadrats <strong>of</strong> 0-<br />

43% <strong>of</strong> rabbits dying underground shows that searching burrows as well as the surface will provide the<br />

most accurate rabbit densities. Poisoning efficacy was _90% in 77% <strong>of</strong> the quadrats, but two low-density<br />

quadrats recorded kill rates


1080 Reassessment Application October 2006<br />

Appendix C<br />

extract was 53.8 (dose-lethality curve) and 64.1 (dose-latency to the 1st seizure curve). The water-soluble<br />

fraction contained a substance with hRf = 20 which was the same as that <strong>of</strong> authentic SMFA. The 19F<br />

NMR spectra <strong>of</strong> authentic SMFA and the P. marcgravii water-soluble fraction were identical. These data<br />

demonstrate the presence <strong>of</strong> SMFA in the water-soluble fraction <strong>of</strong> P. marcgravii leaves and show that<br />

mon<strong>of</strong>luoroacetate is the active principle responsible for the signs and symptoms <strong>of</strong> acute intoxication<br />

Moran, S., S<strong>of</strong>er, S., and Cohen, M. (1987). <strong>Control</strong> <strong>of</strong> rock hyrax, Procavia capensis, in fruit orchards by<br />

fluoroacetamide baits. Crop Protection 6, 265-270.<br />

Keywords: fluoroacetamide/baits/field efficacy<br />

Abstract: Populations <strong>of</strong> the rock hyrax, Procavia capensis, live in man-made rock terraces bordering fruit<br />

plots. They destroy fruit trees by browsing and breaking branches. In an experiment to control these<br />

animals using fluoroacetamide-treated fruit baits, rock hyrax damage was completely prevented in all<br />

treated plots.<br />

Moran, S. (1991). Toxicity <strong>of</strong> sodium fluoroacetate and zinc phosphide wheat grain baits to Microtus<br />

guentheri and Meriones tristrami. Bulletin OEPP 21, 73-80.<br />

Keywords: acute toxicity/ground control/sodium fluoroacetate/fluoroacetate/zinc phosphide<br />

Moran, S. and Keidar, H. Assessment <strong>of</strong> toxic bait efficacy in field trials by counts <strong>of</strong> burrow openings.<br />

168-174. 1994. University <strong>of</strong> California, Davis. Proceedings <strong>of</strong> the 16th Vertebrate Pest Conference.<br />

Halverson, W. S. and Crabb, A. C.<br />

Ref Type: Conference Proceeding<br />

Keywords: efficacy/sodium fluoroacetate/brodifacoum/zinc phosphide/rodents<br />

Moran, S. (1995). Reducing sodium fluoroacetate and fluoroacetamide concentrations in field rodent baits.<br />

Phytoparasitica 23, 195-203.<br />

Keywords: sodium fluoroacetate/fluoroacetate/fluoroacetamide/baits/1080/1081/efficacy/rodents<br />

Abstract: Laboratory trials were carried out in order to estbalish the minimum active ingredient<br />

concentration <strong>of</strong> sodium fluoroacetate (1080) and <strong>of</strong> fluoroacetamide (1081) in wheat baits employed<br />

against Microtus guentheri, the Levant vole, and Meriones tristrami, Tristram's jird, without interfering<br />

with the toxicants' efficacy. Using a mixture <strong>of</strong> treated and untraeted grain enabled a greater reduction in<br />

the a.i. concentration compared with that which could be acheived when all the grains <strong>of</strong>fered conatined a<br />

lower a.i. concentration <strong>of</strong> the toxicants. For M. tristrami, the lowest efficient final a.i. concentration in the<br />

bait was 0.0125% for 1080 mixed bait (1:10 mixture <strong>of</strong> 0.05% poison grains mixed with filler grains) and<br />

0.01% for 1081 mixed bait (1:10 mixture <strong>of</strong> 0.1% poison grains with filler grains); and for M. guentheri, -<br />

0.005% mixed bait <strong>of</strong> 1080 or 1081 (1:10 mixture <strong>of</strong> 0.05% poison grains with filler grains). This leads to a<br />

reduction <strong>of</strong> the hazards involved in the use <strong>of</strong> prepared baits <strong>of</strong> these toxicants in the field.<br />

Moran, S. (1999). Rejection <strong>of</strong> dyed field rodent baits by feral pigeons and chukar partridges.<br />

Phytoparasitica 27, 9-17.<br />

Keywords: fluoroacetate/baits/sodium fluoroacetate/rodents/birds<br />

Abstract: Whole wheat grain bait, treated with sodium fluoroacetate, is used to control field rodents in<br />

Israel. However, this bait constitutes a potential primary non-target hazard to seed-eating birds. In the<br />

present study black-, red-, green- and yellow-dyed whole wheat and sorghum grains, as well as undyed<br />

ones, were <strong>of</strong>fered to feral pigeons, Columba livia, and to chukar partridges, Alectoris chukar, in the<br />

laboratory during 4 days. Grains were <strong>of</strong>fered either piled on trays, or scattered. Consumption levels varied<br />

significantly (P0.05) was observed in the<br />

consumption <strong>of</strong> the differently dyed grains<br />

Morgan, D. R. (1982). Field acceptance <strong>of</strong> non-toxic and toxic baits by populations <strong>of</strong> the brushtail possum<br />

(Trichosurus vulpecula Kerr). New Zealand journal <strong>of</strong> ecology 5, 36-43.<br />

Keywords: possums/field efficacy/baits/bait shyness<br />

132


1080 Reassessment Application October 2006<br />

Appendix C<br />

Morgan, D. R., Batcheler, C. L., and Peters, J. A. Why do possums survive aerial poisoning operations?<br />

Salmon, T. P. 210-214. 1986. University <strong>of</strong> Davis, California. Proceedings <strong>of</strong> Twelfth Vertebrate Pest<br />

Conference.<br />

Ref Type: Conference Proceeding<br />

Keywords: possums/poisoning/baits/aversion/1080/field efficacy/aerial control<br />

Abstract: Major causes <strong>of</strong> failure <strong>of</strong> aerial poisoning operations against possums identified were; subletahl<br />

toxic loading, unsersize sublethal baits, nonlearned behavioural aversion to 1080, and failure to encounter<br />

bait. Dislike <strong>of</strong> bait was not a major cause <strong>of</strong> failure. Progress has been made towards solving these<br />

problems, but failure to encounter bait remains a likely major reason for possums surviving aerial<br />

poisoning. Improvements in the aerial sowing <strong>of</strong> bait are essential if the full benefit <strong>of</strong> this progress is to be<br />

realised.<br />

Morgan, D. R. and Warburton, B. Comparison <strong>of</strong> the effectiveness <strong>of</strong> hunting and aerial 1080 poisoning for<br />

reducing a possum population. Forest <strong>Research</strong> Institute. 1-17. 1987. Christchurch, Forest <strong>Research</strong><br />

Institute.<br />

Ref Type: Report<br />

Keywords: 1080/poisoning<br />

Abstract: Both achieved kills <strong>of</strong> 80%; Patchy distribution with the aerial drop; hunters made pr<strong>of</strong>it for half<br />

the total kill by averaging 8.2 possum skins /hr (selling skins)<br />

Morgan, D. R. (1990). Behavioural response <strong>of</strong> brushtail possums, Trichosurus vulpecula, to baits used in<br />

pest control. Australian wildlife research 17 , 601-613.<br />

Keywords: field efficacy/possums/1080<br />

Abstract: The behaviourial responses <strong>of</strong> captive possums (Trichosurus vulpecula) was observed during first<br />

encounters with non-toxic and toxic carrot and pellet baits used in pest control programmes. Possum<br />

confronted with new baits first used smell in a highly discriminating way, and then taste, which sometimes<br />

changed their initial response. Toxic carrot baits were rejected by 27.5% <strong>of</strong> possums, equally by smell and<br />

taste aversion, and toxic baits. Such non-learned aversion mechanisms therefore have an important role in<br />

the feeding behaviour <strong>of</strong> possums. A range <strong>of</strong> flavours tested, using barely as a food base, showed that<br />

only orange-flavoured barley was significantly preferred to non-flavoured barley: 19 flavours had no<br />

significant effect, and 19 others significantly reduced barley consumption. Orange and cinnamon, which<br />

was ranked fourth and repels some bird species , were tested as masks for 1080 baits. Both flavours<br />

effectively masked the aversive smell and taste <strong>of</strong> 1080. The levels <strong>of</strong> toxic flavoured bait rejection were<br />

low and did not differ from those <strong>of</strong> non-toxic (flavoured or non-flavoured) baits. Very few possums were<br />

observed vomiting, a behaviour in other species that may assist survival.<br />

Morgan, D. R. (1994). Improving aerial control <strong>of</strong> possums by precision bait delivery. Proceedings <strong>of</strong> the<br />

Vertebrate Pest Conference 16, 287-292.<br />

Keywords: field efficacy/aerial control/possums/1080<br />

Abstract: Aerial delivery <strong>of</strong> 1080 (sodium mon<strong>of</strong>luoroacetate) baits is the main technique for reducing<br />

populations <strong>of</strong> New Zealand's foremost vertebrate pest, the Australian brushtail possum, in large areas <strong>of</strong><br />

inaccesible country. Surveys after pilot-controlled aerial sowing <strong>of</strong> baits in seven operations in forests<br />

showed that inaccurate navigation along the swaths left up to half the target zone untreated. Kill was<br />

estimated to average 75%. Inadequate coverage with baits was therefore believed to be a major factor in<br />

the survival <strong>of</strong> possums during aerial control operations. This was confirmed in field trials using<br />

rhodamine B as a biomarker to reveal acceptance <strong>of</strong> non-toxic baits. More possums were unmarked in<br />

partially treated blocks than in completely treated blocks. After a large scale aerial control operation,<br />

proportionally more possums survived in untreated gaps than it treated areas.<br />

Six operations that used navigation guidance systems (Decca Flying Flagman and GPS) yielded complete<br />

coverage and high levels <strong>of</strong> kill (mean <strong>of</strong> 92%) in five. Precision sowing <strong>of</strong> possum baits prevents survival<br />

<strong>of</strong> possums by failure to encounter baits, and enables lower rates <strong>of</strong> bait application. This will give large<br />

cost savings and improved environmental safety. A small proportion <strong>of</strong> a population may still not be<br />

targeted because <strong>of</strong> individual dislike <strong>of</strong> bait or failure to encounter baits because animals stayed in the<br />

forest canopy during operations. Development <strong>of</strong> more palatable and longer lived baits may facilitate local<br />

extermination <strong>of</strong> possums.<br />

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Appendix C<br />

Morgan, D. R. (1994). Improving the efficiency <strong>of</strong> aerial sowing <strong>of</strong> baits for possum control. New Zealand<br />

journal <strong>of</strong> agricultural research 37, 199-206.<br />

Keywords: field efficacy/aerial control/treatment/possums<br />

Abstract: Four aerial sowing treatments <strong>of</strong> non-toxic possum bait were compared in a pine plantation <strong>of</strong> flat<br />

terrain. Baits were dyed with Rhodamine B and treatment were assessed by the proportion <strong>of</strong> dy-marked<br />

possums captured. Sowing was least accurate where flight paths were not marked, but the resulting baitfree<br />

patches did not prevent possums from finding and eating bait. Where larger gaps were deliberately<br />

created in bait dispersion acceptance <strong>of</strong> bait by possums was slower and overall, less than where coverage<br />

was assisted by flight line marking. Sowing bait at a rate <strong>of</strong> 3 kg/ha was as effective as 10kg/ha. These<br />

results have two main implications for routine aerial control. First, because incomplete coverage <strong>of</strong> a target<br />

are will yield poorer kills, navigation aids should be used in systematic sowing and sowing equipment<br />

improved. Second a cost-saving can be achieved by reducing sowing rate to 3kg/ha and possibly lower.<br />

Trials are required in other habitat types to test the general applicability <strong>of</strong> this result.<br />

Morgan, D. R. and Goodwin, M. Field trials <strong>of</strong> 1080 paste treated with a bee repellent. [LC9394/101], -15.<br />

1994. Christchurch, Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract report.<br />

Ref Type: Report<br />

Keywords: non-target species/invertebrates/ground control/1080/possums<br />

Abstract: Objectives: To extend the initial field testing <strong>of</strong> the efficacy <strong>of</strong> IVA (isovaleric acid) as a bee<br />

repellent in 1080 apple paste; to extend the initial field testing <strong>of</strong> the efficacy <strong>of</strong> IVA-treated 1080 paste in<br />

killing possums. Conclusions: IVA reduces the likelihood <strong>of</strong> bees being poisoned or hives being<br />

contaminated. However, we have not established the level <strong>of</strong> hazard remaining. The likelihood <strong>of</strong> bees<br />

feeding on 1080 paste varies seasonally, and IVA itself may also vary seasonally in repellancy to bees.<br />

IVA can be included in possum paste without reducing the effectiveness <strong>of</strong> control operations.<br />

Morgan, D. R. (1994). Improved cost-effectiveness and safety <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) possum<br />

control operations. In 'Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14 December 1993, Christchurch,<br />

New Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 144-150. (<strong>Royal</strong> Society <strong>of</strong> New Zealand:<br />

Wellington.)<br />

Keywords: field efficacy/ground control/aerial control/1080/possums/birds/non-target species<br />

Abstract: Maintenance <strong>of</strong> many <strong>of</strong> New Zealand's fragile ecosystems and a large proportion <strong>of</strong> its<br />

agricultural production are presently dependent on the use <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) poison for<br />

controlling possums. The growing demand for possum control by land managers has highlighted the need<br />

<strong>of</strong> maximum efficiency in operational methods and minimum environmental impact. Several major<br />

improvements in control techniques have been made in the last five years. Specifications for bait<br />

production have reduced the possibility <strong>of</strong> possums being sublethally poisoned, costly waste, and the risk <strong>of</strong><br />

birds and other non-target species eating small toxic fragments. Aerial distribution <strong>of</strong> baits has become<br />

more accurate through the use <strong>of</strong> navigation guidance systems. This has led to high kills being attained<br />

using reduced application rates <strong>of</strong> toxic bait and to a consequent further reduction in environmental risks.<br />

Hand-laid bait "feeders" have been developed as restricted sources <strong>of</strong> toxic bait for use in some areas where<br />

wide-spread aerial poisoning may be inadvisable. Bait formulations are also being improved by using<br />

water or inexpensive materials, repellents that deter non-target animals not possums, and polymer coatings<br />

that improved bait-life. Such improvements will help sustain the use <strong>of</strong> 1080 until superior alternative<br />

control techniques are developed.<br />

Morgan, D. R. and Goodwin, M. Identification <strong>of</strong> 1080 paste suitable for use in the presence <strong>of</strong> bees.<br />

[LC9596/003], -20. 1995. Lincoln, Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract<br />

report.<br />

Ref Type: Report<br />

Keywords: non-target species/invertebrates/ground control/1080/possums/birds<br />

Abstract: Objectives: To test new formulations <strong>of</strong> low-sugar pastes against bees and possums; to assess the<br />

safety <strong>of</strong> promising pastes to fruit- and nectar-eating birds and bats; to assess the shelf- and field-life <strong>of</strong><br />

promising pastes.<br />

Conclusions: Two pastes, BB3 and BB16, are suitable as possum baits and are more target-specific than<br />

BB13. They can also be used as prefeed paste, but this may reduce efficacy, perhaps because <strong>of</strong> the more<br />

obvious change in taste when 1080 is added compared with the sugar-rich BB13. It is unlikely that bees<br />

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Appendix C<br />

will feed on the pastes and contamination <strong>of</strong> hives and honey from using these bait types is therefore also<br />

unlikely. The two new pastes were less attractive than BB13 to most captive and wild birds. The runny<br />

texture <strong>of</strong> BB3 and the development <strong>of</strong> fluid on the surface <strong>of</strong> BB16 present a hazard as leakage from both<br />

applicator guns and containers may occur. Furthermore, 1080 is rapidly lost from baits in the field by<br />

drainage <strong>of</strong> fluid.<br />

Morgan, D. R., Morriss, G., and Hickling, G. J. (1996). Induced 1080 bait-shyness in captive brushtail<br />

possums and implications for management. Wildlife research 23, 207-211.<br />

Keywords: field efficacy/1080/possums/brodifacoum<br />

Abstract: The probable cause <strong>of</strong> possums (Trichosurus vulpecula) becoming 'shy' towards 1080 [sodium<br />

fluoroacetate] bait, a growing problem in the control <strong>of</strong> this pest, was determined. Possums captured from<br />

North Canterbury, New Zealand, (n = 131) were <strong>of</strong>fered sublethal baits (1 or 2.5 g) followed by lethal (6 g)<br />

baits 2 days later. Most possums became bait shy and the proportion becoming shy appeared to be related<br />

to the size <strong>of</strong> the initial sublethal dose. Most <strong>of</strong> a group <strong>of</strong> survivors retested after 3 months with toxic<br />

pellets were still shy. Shyness was not overcome by changing to a different mask (orange flavour, as<br />

opposed to cinnamon flavour) or toxin (brodifacoum), but changing to both a different bait base (carrot)<br />

and mask (orange) resulted in most shy possums eating a lethal quantity <strong>of</strong> bait. Possums therefore<br />

appeared to learn to recognise the bait base as the cue for avoiding poisoning. More shy possums than naive<br />

possums rejected non-dyed, non-masked, non-toxic pellets, confirming that shy possums recognised the<br />

bait base. Green dye appears to act as a secondary cue for avoiding pellets as a higher percentage <strong>of</strong> 'shy'<br />

possums than naive possums rejected dyed baits.<br />

Morgan, D. R., Thomas, M. D., Meenken, D., and Nelson, P. C. (1997). Less 1080 bait usage in aerial<br />

operations to control possums. Proceedings <strong>of</strong> the New Zealand Plant Protection Conference 50, 391-396.<br />

Keywords: field efficacy/aerial control/1080/possums<br />

Abstract: Field trials showed that high application rates (20-35 kg/ha) <strong>of</strong> 1080 pellet and carrot baits for<br />

possum control were unnecessary, wasteful, and environmentally unsound. Reducing the standard<br />

operation rate to 5-10 kg/ha has saved conservatively, $8.9 million/year. In our most recent trials, kills<br />

averaging 95% were gained with 2 kg/ha indicating further potential savings <strong>of</strong> $3 million/year or more. A<br />

new helicopter bait-application bucket has been developed to overcome the common problem <strong>of</strong> buckets<br />

becoming blocked below rates <strong>of</strong> 3-4 kg/ha. The new bucket can apply baits uniformly at rates as low as<br />

0.5 kg/ha, promising not only great efficiency but enhanced environmental safety.<br />

Morgan, D. R. (1999). Risks to non-target species from use <strong>of</strong> a gel bait for possum control. New Zealand<br />

journal <strong>of</strong> ecology 23, 281-287.<br />

Keywords: non-target species/field efficacy/ground control/1080/baits<br />

Abstract: The risks to non-target species <strong>of</strong> a newly developed bait containing either 0.15% 1080 or 0.6%<br />

cholecalciferol in a gel matrix were assessed. Very few <strong>of</strong> them ate gel bait. The safety <strong>of</strong> the gel bait is<br />

further enhanced by its placement in the purpose-designed bait station from which little spillage occurs, and<br />

which can be placed so that it is out <strong>of</strong> reach <strong>of</strong> most non-target animals. Comparative data show that<br />

nontarget species are considerably less susceptible to cholecalciferol than to sodium mon<strong>of</strong>luoroacetate<br />

(1080). Risks to non-target species could be further reduced by use <strong>of</strong> the cholecalciferol form <strong>of</strong> the bait.<br />

Morgan, D. R. Assessment <strong>of</strong> 1080 pastes for possum control. [LC9900/117], -24. 2000. Lincoln, Manaaki<br />

Whenua - <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract report.<br />

Ref Type: Report<br />

Keywords: field efficacy/bait degradation/non-target species/invertebrates/ground control/1080<br />

Abstract: Objectives: To test three possum pastes (BB3, BB16 and CP (I.e. cyanide prefeed) against AHB<br />

specificatons for attractiveness to bees; dehydration; toxicity; bait shape; field stability, including wind<br />

resistance, detoxication, and rain resistance; palatability; and efficacy. Following renegotiation with AHB,<br />

to assess two further variations on BB3 coded as SB(i) and SB3(ii), against selected specifications.<br />

Results: The performance <strong>of</strong> paste baits against the nine specifications is summarised. CP and SB(ii) were<br />

the best performing pastes. BB3, although superceded by the SB3 pastes, is regarded as potentially useful,<br />

while BB16 and SB3(i) performed poorly.<br />

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Appendix C<br />

Morgan, D. R. and Eason, C. T. 1080: A review <strong>of</strong> its properties, usage, lethal and sublethal effects,<br />

environmental fate, and non-target poisoning risks in New Zealand. 2002. Advances in Vertebrate Pest<br />

Management III.<br />

Ref Type: Conference Proceeding<br />

Keywords: 1080/poisoning/mon<strong>of</strong>luoroacetate/sodium mon<strong>of</strong>luoroacetate/mammals/USA/Krebs<br />

cycle/heart/brain/non-target species/livestock/blood/liver/brodifacoum/regulatory<br />

toxicology/rats/soil/invertebrates/baits/dogs<br />

Abstract: Mon<strong>of</strong>luoroacetate, the active component <strong>of</strong> 1080, occurs naturally in toxic plants in Australia,<br />

South Africa, and South America. Manufactured 1080 (sodium mon<strong>of</strong>luoroacetate) is used to control<br />

introduced mammals in New Zealand, Australia, Israel, Mexico and the USA. It is a broad-spectrum poison<br />

that acts by interfering with the energy-producing Krebs cycle in cell mitochondria, particularly in the<br />

heart, lungs and brain. Used correctly, it is a highly cost-effective vertebrate pesticide. Because 1080 is<br />

used more widely in New Zealand than elsewhere, its fate in water and its effect on non-target species,<br />

especially livestock and native fauna, have been comprehensively assessed. Sub-lethal doses <strong>of</strong> 1080<br />

consumed by livestock do not cause persistent toxic residues in meat, blood, the liver, or fat. This is in<br />

marked contrast to the prolonged persistence <strong>of</strong> the anticoagulant toxicant brodifacoum. Nevertheless, if<br />

livestock become exposed to 1080 bait, a minimum withholding period <strong>of</strong> 5–10 days is advised to permit<br />

elimination. Regulatory toxicology studies, conducted to assess human health hazards, indicate that<br />

prolonged exposure <strong>of</strong> rats to sub-lethal doses <strong>of</strong> 1080 may lead to malformations in developing embryos,<br />

but no evidence <strong>of</strong> mutagenic effects was detected. Environmental studies show that operational use <strong>of</strong><br />

1080 causes minimal long-term water and soil contamination, and current evidence suggests that<br />

populations <strong>of</strong> common bird species and invertebrates are not adversely affected, but further monitoring <strong>of</strong><br />

rarer species after aerial application <strong>of</strong> baits is continuing. In cold or dry conditions, 1080 may persist in<br />

baits or in possum carcasses for several weeks or months, posing a hazard to dogs, which are particularly<br />

susceptible to the poison. The greatest potential risks from 1080 are therefore to scavenging dogs, and to<br />

bait manufacturing workers with a high degree <strong>of</strong> exposure to 1080. Constant vigilance is required to<br />

minimise these risks.<br />

Morgan, D. R. (2004). Enhancing maintenance control <strong>of</strong> possum populations using long-life baits. New<br />

Zealand journal <strong>of</strong> zoology in press.<br />

Keywords:<br />

baits/Tb/possums/analysis/toxicity/efficacy/cholecalciferol/livestock/1080/brodifacoum/degradation/bait<br />

degradation<br />

Abstract: Possum populations must be maintained at very low density if the aims <strong>of</strong> Tb eradication and<br />

conservation <strong>of</strong> particularly vulnerable native species are to be met. The present tactic <strong>of</strong> initial<br />

'knockdown' followed by annual maintenance control allows for reinfestation in between annual operations.<br />

Development <strong>of</strong> toxic baiting methods for 'continuous' control <strong>of</strong> possum populations is therefore desirable.<br />

Six baittype/ presentation-methods designed for prolonged field life were exposed to field conditions at a<br />

forest-edge site in Westland. Samples <strong>of</strong> baits were collected at 2-monthly intervals for up to 26 months,<br />

and assessed for palatability to possums and toxicant concentration. Regression analysis was used to predict<br />

the time at which reductions in palatability and toxicity would lead to inadequate bait efficacy. Field life<br />

varied between 2 and >26 months, the most durable option tested being a solid gel bait containing<br />

cholecalciferol. This bait type was selected for assessment in 'continuous' control <strong>of</strong> possums in forest-edge<br />

habitat in Westland. Baits were placed up trees beyond the reach <strong>of</strong> livestock and left in place for 10<br />

months. Trap-catch monitoring showed baits were effective in reducing the number <strong>of</strong> possums, but this<br />

was achieved only after improving the visibility, attractiveness, and accessibility <strong>of</strong> bait stations. As the<br />

study predicted that cholecalciferol gel bait should remain effective for longer than 2 years in the field,<br />

there appears to be considerable potential for improving the efficiency (and probably environmental safety)<br />

<strong>of</strong> long-term control using this new tool.<br />

Mori, M., Nakajima, H., and Seto, Y. (1996). Determination <strong>of</strong> fluoroacetate in aqueous samples by<br />

headspace gas chromatography. Journal <strong>of</strong> chromatography A 736, 229-234.<br />

Morohashi, Y. and Shimokoriyama, M. (1972). Physiological studies on germination <strong>of</strong> Phaseolus mungo<br />

seeds. 1. Development <strong>of</strong> respiration and changes in the contents <strong>of</strong> constituents in the early stages <strong>of</strong><br />

germination. Journal <strong>of</strong> Experimental Botany 23, 45-53.<br />

136


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: fluoroacetate/citric acid/persistence in plants<br />

Abstract: In laboratory experiments, O2 uptake by P. mungo seeds germinated at 30 deg C, (a) rose sharply<br />

for 4-5 h, then (b) remained constant for 1-2 h and (c) again increased. Iodoacetate and fluoroacetate<br />

inhibited the inrease in (c), but did not affect (a) or (b). Aspartic-acid content decreased from 16.2 to 7.7<br />

moles/100 seeds in 9 h. Citric acid and malic acid were the main organic-acid constituents. Citric-acid<br />

content decreased while that <strong>of</strong> malic acid was unchanged, although it was leached freely into the medium,<br />

especially in the first 6 h<br />

Morris, M. C. and Weaver, S. A. (2003). Minimizing harm in possum control operations and experiments<br />

in New Zealand. Journal <strong>of</strong> Agricultural & Environmental Ethics 16, 367-385.<br />

Keywords: welfare/poisoning/possums/degradation<br />

Abstract: Pest control operations and experimentation on sentient animals such as the brushtail possum can<br />

cause unnecessary and avoidable suffering in the animal subjects. Minimizing animal suffering is an animal<br />

welfare goal and can be used as a guide in the design and execution <strong>of</strong> animal experimentation and pest<br />

control operations. The public has little sympathy for the possum, which can cause widespread<br />

environmental damage, but does believe that control should be as painless as possible. Trapping and<br />

poisoning provide only short-term solutions to the possum problem and <strong>of</strong>ten involve methods that cause<br />

suffering. Intrusive experiments connected with these methods <strong>of</strong> control and published in the last 6 years<br />

are reviewed. Many <strong>of</strong> the experiments do not attain the welfare standards required by members <strong>of</strong> the<br />

public. Possums also act as vectors for bovine tuberculosis. While this is not as important in the minds <strong>of</strong><br />

the public as environmental degradation, as long as people wish to continue raising cattle, this disease<br />

needs to be controlled. Immunocontraception is a humane means <strong>of</strong> controlling possums with wide public<br />

acceptance. The use <strong>of</strong> vaccines for cows and/or possums would also cause far less suffering than present<br />

eradication operations. <strong>Research</strong> into these methods does require some intrusive experimentation. This can<br />

be reduced if live animals are not used for secondary antibody harvesting, if adequate analgesia is provided,<br />

and if potential vaccines or contraceptives are tested under conditions that would be experienced in the<br />

field.<br />

Morrison, J. F. (1954). The purifaction <strong>of</strong> aconitase. Biochemistry Journal 56, 99-105.<br />

Keywords: aconitase/biochemistry<br />

Morrison, J. F. and Peters, R. A. (1954). Biochemistry <strong>of</strong> fluoroacetate poisoning : the effect <strong>of</strong><br />

fluorocitrate on purified aconitase. Biochemical journal 58, 473-479.<br />

Keywords: metabolism/biochemistry/fluoroacetate/poisoning/fluorocitrate/aconitase/mode <strong>of</strong><br />

action/enzyme/inhibition<br />

Abstract: 1. The competitive inhibition <strong>of</strong> aconitase by natural fluorocitrate has been established.<br />

2. On the other hand, synthetic fluorocitrate has been shown to inhibit aconitase in both a competitive and<br />

an apparent irreversible fashion.<br />

3. The dissociation constants <strong>of</strong> the aconitase-fluorocitrate complexes for both the natural and synthetic<br />

fluorocitrates have been measured. The affinity <strong>of</strong> aconitase for the synthetic compound is much greater<br />

than for the natural compound.<br />

4. The possible reasons have been discussed for the difference between the two preparations <strong>of</strong> fluorocitrate<br />

in inhibiting the isolated aconitase and also for the difference between the action <strong>of</strong> these compounds on the<br />

isolated aconitase system as compared to their action in vivo and on the kidney-particle system.<br />

Morselli, P. L., Garattini, S., Marcucci, F., Mussini, E., Rewersky, W., Valzelli, L., and Peters, R. A.<br />

(1968). The effect <strong>of</strong> injections <strong>of</strong> fluorocitrate into the brains <strong>of</strong> rats. Biochemical Pharmacology 17, 195-<br />

202.<br />

Keywords: mode <strong>of</strong> action/acute toxicity/fluorocitrate/brain/rats/fluoroacetate/target organ/symptoms<br />

Moss, S. J., Murphy, C. D., Hamilton, D. J., McRoberts, W. C., O'Hagan, D., Schaffrath, C., and Harper, D.<br />

B. (2000). Fluoroacetaldehyde: a precursor <strong>of</strong> both fluoroacetate and 4-fluorothreonine in Streptomyces<br />

cattleya. Chem Comm 2281-2282.<br />

Keywords: fluoroacetate/bacteria/biosynthesis<br />

Abstract: Fluoroacetaldehyde is converted to fluoroacetate and 4-fluorothreonine in Streptomyces cattleya<br />

indicating that it is the biosynthetic precursor <strong>of</strong> both <strong>of</strong> these secondary metabolites<br />

137


1080 Reassessment Application October 2006<br />

Appendix C<br />

Moss, Z. N., O' Connor, C. E., and Hickling, G. J. (1998). Implications <strong>of</strong> prefeeding for the development<br />

<strong>of</strong> bait aversions in brushtail possums (Trichosurus vulpecula).<br />

Abstract: Development <strong>of</strong> aversions, or learned 'bait-shyness', in frequently poisoned possum (Trichosurus<br />

vulpecula) populations is becoming increasingly detrimental to the efficacy <strong>of</strong> pest-control operations in<br />

New Zealand. This experiment aimed to identify the effects <strong>of</strong> prefeeding, a common management<br />

procedure, on the subsequent development <strong>of</strong> aversions in possums. Wild possums (n = 96) were captured<br />

and acclimatised, then allocated to one <strong>of</strong> three treatments groups that for seven days received either (i) no<br />

prefeed, (ii) plain RS5 cereal baits, or (iii) green-dyed and cinnamon-lured RS5 cereal baits. The possums<br />

were then <strong>of</strong>fered a standard green-dyed and cinnamon-lured RS5 bait that contained a sublethal dose (0.4<br />

mg kg-1) <strong>of</strong> the toxin sodium mon<strong>of</strong>luoroacetate (1080). The possums were tested for development <strong>of</strong> an<br />

aversion towards a toxic RS5 1080 bait, a prefeed bait, and a prefeed bait containing an alternative toxin,<br />

brodifacoum. Most (96%) <strong>of</strong> the non-prefed possums became averse to the 1080 bait after two exposures,<br />

compared with only 55% and 9% <strong>of</strong> the two prefed groups. Similarly, 90% and 92% <strong>of</strong> the non-prefed<br />

possums were averse to prefeed and brodifacoum baits, respectively, compared with 8% and 14% <strong>of</strong> the<br />

prefed possums. This suggests that pest managers can reduce the risk <strong>of</strong> 'bait shyness' by prefeeding. A<br />

further advantage <strong>of</strong> prefeeding is that if poison shyness develops, use <strong>of</strong> an alternative toxin such as<br />

brodifacoum in the original bait base may still be successful<br />

Mount, M. E. and Feldman, B. F. (1984). Practical toxicologic diagnosis. A guide to improving the<br />

diagnosis <strong>of</strong> chemical toxicosis in veterinary practice. Unknown.<br />

Abstract: Diagnosis <strong>of</strong> poisoning with strychnine, fluoroacetate, rodenticides, insecticides, ethylene glycol,<br />

urea, monensin, salt, lead, arsenic, copper and poisonous plants is summarized. The samples required for<br />

chemical analysis are also tabulated<br />

Munday, B. L. (1978). Marsupial disease. In 'Proceedings No. 36 <strong>of</strong> a course for Veterinarians (the J.P.<br />

Stewart course for 1978)'. (Sydney University Post Graduate Committee in Veterinary Science:<br />

Keywords: lethal dose/1080<br />

Murphy, C. D. Biological fluorination and defluorination in Streptomyces cattleya. 185. 1998. Queen's<br />

University <strong>of</strong> Belfast (Northern Ireland)Editor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: defluorination/fluoroacetate/NMR/metabolism/acetate/fluorine/enzyme<br />

Abstract: Little is understood about the mechanism by which fluorinated compounds are biologically<br />

formed, although the existence <strong>of</strong> such natural products was established over 50 years ago. This<br />

investigation concerns the biochemical pathways involved in fluoroacetate and -fluorothreonine production<br />

by the actinomycete Streptomyces cattleya and the enzymatic defluorination <strong>of</strong> 4-fluoroglutamate by the<br />

same organism. By employing GC/MS and $sp{19}$F NMR methodologies it was possible to determine<br />

the incorporation <strong>of</strong> isotopic label into the fluorometabolites after various $sp{13}$C and $sp2$H-labelled<br />

precursors were incubated with resting cell suspensions. The incorporation <strong>of</strong> isotopic label from (3-<br />

$sp{13}$3C) -serine was consistent with the metabolism <strong>of</strong> glycine via serine and pyruvate to the<br />

fluorometabolites, as previously suggested and investigations with (2-$sp{13}$C) -acetate indicated that<br />

pyruvate does not enter the TCA cycle before yielding the carbon substrate for flurination. Observations<br />

from resting cell studies with (R)- and (S)-(1,1-$rmsp2Hsb2$) -glycerol suggested that (a) the carbon<br />

substrate for fluorination is closely related to an intermediate <strong>of</strong> the glycolytic pathway linking glycerol and<br />

pyruvate and (b) the mechanism <strong>of</strong> fluorination probably involves the replacement <strong>of</strong> phosphate with<br />

fluorine. It was tentatively concluded from isotopic dilution experiments and studies with various stable<br />

isotope labelled glucoses that either dihydroxyacetone phosphate or glyceraldehyde-3-phosphate (or a close<br />

derivative) is the carbon substrate for fluonnation. When fluoroacetaldehyde was incubated with resting cell<br />

suspensions, it was largely oxidized to fluoroacetate and, more importantly, significant amounts <strong>of</strong> 4fluorothreonine<br />

were formed, consistent with the hypothesis that fluoroacetaldehyde is the immediate<br />

fluorinated precursor <strong>of</strong> both fluorometabolites. Cell-free extracts <strong>of</strong> S. cattleya were found to defluorinate<br />

4-fluoroglutamate, a compound that may be formed inside the cell via TCA cycle metabolism <strong>of</strong><br />

fluoroacetyl CoA and which may act as an analogue <strong>of</strong> L-glutamate. The defluorinating system does not<br />

appear to require a c<strong>of</strong>actor and partial purification <strong>of</strong> the cell free extract by anion-exchange<br />

chromatography demonstrated that the defluorinating activity could be separated from deaminating activity.<br />

Passage <strong>of</strong> the enzyme through a gel filtration column indicated a molecular weight <strong>of</strong> $sim$80,000<br />

138


1080 Reassessment Application October 2006<br />

Appendix C<br />

Murphy, C. D., Moss, S. J., and O'Hagan, D. (2001). Isolation <strong>of</strong> an aldehyde dehydrogenase involved in<br />

the oxidation <strong>of</strong> fluoroacetylaldehyde to fluoroacetate in Streptomyces cattleya. Applied and environmental<br />

microbiology 67, 4919-4921.<br />

Keywords: fluoroacetate/biosynthesis/metabolism/bacteria/enzyme/occurrence in nature<br />

Abstract: Streptomyces cattleya is unusual in that it produces fluoroacetate and 4-fluorothreonine as<br />

secondary metabolites. We now report that the isolation <strong>of</strong> an NAD+-dependent fluoroacetaldehyde<br />

dehydrogenase from S.cattleya that mediates the oxidation <strong>of</strong> fluoroacetaldehyde to fluoroacetate. This is<br />

the first enzyme to be identified that is directly involved in fluorometabolite biosynthesis. Production <strong>of</strong> the<br />

enzyme begins in late exponential growth and continues into the stationary phase. Measurement <strong>of</strong> kinetic<br />

parameters shows that the enzyme has a high affinity for fluoroacetaldehyde and glycoaldehyde, but not<br />

acetaldehyde.<br />

Murphy, C. D., Schaffrath, C., and O'Hagan, D. (2003). Fluorinated natural products: the biosynthesis <strong>of</strong><br />

fluoroacetate and 4-fluorothreonine in Streptomyces cattleya. Chemosphere 52, 455-461.<br />

Keywords: biosynthesis/fluoroacetate/bacteria/enzyme<br />

Abstract: Organ<strong>of</strong>luorine compounds are rare in Nature, with only a handful known to be produced by<br />

some species <strong>of</strong> plant and two microorganisms. Consequently, the mechanism <strong>of</strong> enzymatic carbon-fluorine<br />

bond formation is poorly understood. The bacterium Streptomyces cattleya biosynthesises fluoroacetate and<br />

4-fluorothreonine as secondary metabolites and is a convenient system to study the biosynthesis and<br />

enzymology <strong>of</strong> fluorometabolite production. Using stable-isotope labelled precursors it has been shown that<br />

there is a common intermediate in the biosynthesis <strong>of</strong> the fluorometabolites, which has recently been<br />

identified as fluoroacetaldehyde. Studies with cell-free extracts <strong>of</strong> S. cattleya have identified two enzymes,<br />

an aldehyde dehydrogenase and a threonine transaldolase, that are involved in the biotransformation <strong>of</strong><br />

fluoroacetaldehyde to fluoroacetate and 4-fluorothreonine.<br />

Murphy, E. C., Clapperton, K., Bradfield, P., and Speed, H. (1998). Effects <strong>of</strong> rat-poisoning operations on<br />

abundance and diet <strong>of</strong> mustelids in New Zealand podocarp forests. New Zealand journal <strong>of</strong> zoology 25,<br />

315-328.<br />

Keywords: ferrets/1080/brodifacoum/pindone/secondary<br />

poisoning/poisoning/stomach/rats/birds/invertebrates/possums/field efficacy<br />

Abstract: This study aimed to quantify the changes in numbers and diet <strong>of</strong> stoats, weasels and ferrets<br />

following rat and possum poison operations in two podocarp-hardwood forests between 1989 and 1995.<br />

Poison operations were classified according to their success in reducing rat numbers, and if they used an<br />

acute toxin (1080) or an anticoagulant (brodifacoum or pindone). Stoat catch rates followed the same<br />

seasonal patterns as rat footprint tracking rates, and stoat catch rates were positively correlated with rat<br />

catch rates. Rat numbers in spring had no significant relationship with the number <strong>of</strong> juvenile stoats caught<br />

in summer. Stoat catch rates did not vary significantly with poison-operation type over a six month period,<br />

but all three successful anticoagulant operations resulted in lower stoat catch rates than did unsuccessful<br />

operations. Brodifacoum in bait stations may have lowered stoat numbers by secondary poisoning for the<br />

first 2-3 months, but there after there was no apparent effect. The sex ratio <strong>of</strong> stoats caught varied<br />

significantly amongst the poison operations. The fewest females were caught following anticoagulant<br />

operations. Stoat stomachs and intestines contained mostly rats, and some birds and mice. Weasels ate<br />

mostly mice, while ferrets predominantly ate lagomorphs and invertebrates. Male and female stoats ate<br />

similar proportions <strong>of</strong> rats, but females ate more mice. Both sexes, but particularly females, ate fewer birds<br />

in autumn and winter than in spring and summer. Stoats shifted between eating rats and birds, depending on<br />

the abundance <strong>of</strong> rats. Thuis successful rat-poisoning operations resulted in higher bird consumption than<br />

unsuccessful ones. Combining the numerical and functional responses <strong>of</strong> stoats into a 'bird predation index'<br />

showed that stoats are likely to have the greatest effect on birds after successful 1080 operations. Diet shifts<br />

could not be demonstrated in weasels or ferrets because sample sizes were too small for quantitative<br />

assessments. The risk <strong>of</strong> increased predation pressure on birds from diet-shifting by stoats must be balanced<br />

against the predation pressure on birds and other ecological impacts <strong>of</strong> rats and possums from different<br />

poison operations.<br />

Murphy, E. C., Robbins, L., Young, J. B., and Dowding, J. E. (1999). Secondary poisoning <strong>of</strong> stoats after<br />

an aerial 1080 poison operation in Pureora forest, New Zealand. New Zealand journal <strong>of</strong> ecology 23, 175-<br />

182.<br />

139


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: secondary poisoning/mammals/1080/birds<br />

Abstract: Stoats were monitored by three methods through an aerial 1080 poisoning operation at<br />

Waimanoa, Pureora Forest in August 1997. Tracking rates and number <strong>of</strong> live captures were used as indices<br />

<strong>of</strong> abundance, and radio-transmitters were used to follow individual animals. All 13 stoats with radiotransmitters<br />

within the poisoned area died between 2-18 days after the operation. No mustelids were<br />

tracked or live-trapped after the operation for three months. Of the radio-tracked stoats that died, rat<br />

remains occurred in 67%, passerine birds in 17%, cave weta in 17% and possum in 8%. Residues <strong>of</strong> 1080<br />

were found in 12 <strong>of</strong> the 13 dead stoats. Our findings have important implications for the management <strong>of</strong><br />

threatened species. Stoats are known to be a major factor in the continuing decline <strong>of</strong> some native birds.<br />

Previously, the potential <strong>of</strong> secondary poisoning to control stoats land other predators) in New Zealand had<br />

focused on the use <strong>of</strong> anticoagulants, as these compounds persist and can accumulate in predators over a<br />

longer period. However, our results suggest that secondary poisoning with an acute toxin can also be highly<br />

efficient. This may also have greater public acceptability.<br />

Murray, L. R. and Woolley, D. R. (1968). The uptake <strong>of</strong> fluoride by Acacia georginae E.M. Bailey.<br />

Australian Journal <strong>of</strong> Soil <strong>Research</strong> 6, 203-210.<br />

Keywords: fluoride/persistence in plants/fluorine<br />

Abstract: Chemical and physical measurements were made on soil samples and leaft material from Acacia<br />

georginae in order to investigate a number <strong>of</strong> factors which were considered to be possibly influencing the<br />

uptake <strong>of</strong> fluoride by the plant in the field. No correlation was found between leaf fluorine levels and any<br />

<strong>of</strong> the factros measured. The available evidence suggests that the 100-fold variation in leaf fluorine levels<br />

found is not due to variation in soil composition; this conclusion was supported by pot trials using soil from<br />

trees with high and low leaf fluorine levels. High leaf fluorine levels (> 10 ppm or air dry material) were<br />

found in the filed only where the trees grow over carbonate bedrock (limestone or dolomite); however only<br />

a small percentage <strong>of</strong> teh trees in such areas have elevated leaf fluorine levels.<br />

Nachman, M. and Hartley, P. L. (1975). Role <strong>of</strong> illness in producing learned taste aversions in rats: a<br />

comparison <strong>of</strong> several rodenticides. J.Comp.Physiol.Psychol. 89, 1010-1018.<br />

Keywords: bait shy/aversion/rats/lethal dose/sodium<br />

fluoroacetate/fluoroacetate/warfarin/cyanide/strychnine/symptoms<br />

Abstract: Several toxic agents were compared in order to test the effect <strong>of</strong> various types <strong>of</strong> illness in<br />

producing learned taste aversions. After a 10-min sucrose drinking trial, groups <strong>of</strong> rats were injected<br />

intraperitoneally with lithium chloride or with a strong, near lethal dose <strong>of</strong> a rodenticide. Strong sucrose<br />

aversions were acquired by groups injected with lithium chloride, copper sulfate, sodium fluoroacetate, or<br />

red squill, and very weak or no aversions were learned by groups injected with thallium, warfarin cyanide,<br />

or strychnine. The results were discussed in terms <strong>of</strong> onset <strong>of</strong> symptoms, duration <strong>of</strong> symptoms, and kinds<br />

<strong>of</strong> physiological effects necessary to produce aversions. It was concluded that the effects <strong>of</strong> different drugs<br />

may be mediated by different physiological systems learned taste aversions<br />

Nadler, J. V., Horwitch, P., and Cooper, J. R. (1972). Effects <strong>of</strong> sodium fluoroacetate on the metabolism <strong>of</strong><br />

N-acetylaspartate and aspartate in mouse brain. Journal <strong>of</strong> neurochemistry 19, 2107-2118.<br />

Keywords: mode <strong>of</strong> action/sodium fluoroacetate/fluoroacetate/metabolism/brain/Krebs cycle<br />

Abstract: ......We consider the results to be consistent with a selective inhibition both by sodium<br />

fluoroacetate and by exogenous aspartic acid <strong>of</strong> the tricarboxylic acid cycle in the brain associated with the<br />

biosynthesis <strong>of</strong> glutamine. We suggest that the activity <strong>of</strong> this pathway may regulate the metabolism <strong>of</strong> Nacetylaspartate<br />

and aspartate.<br />

Negherbon, W. O. (1959). Sodium fluoroacetate. In 'Handbook <strong>of</strong> Toxicology Volume III Insecticides'.<br />

(Ed. W. O. Negherbon.) pp. 694-695.<br />

Keywords: sodium fluoroacetate/fluoroacetate/invertebrates<br />

New Zealand Veterinary Association. 1080 necessary. Vets@Work [June 2004], -2. 2004. Wellington,<br />

New Zealand, New Zealand Veterinary Association.<br />

Ref Type: Magazine Article<br />

Keywords: 1080/pest/New Zealand<br />

140


1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Until a better way <strong>of</strong> killing noxious pest animals comes along, New Zealand had no alternative<br />

but to continue with the widespread use ot 1080, according to the New Zealand Veterinary Association.<br />

Nichols, H. C., Thomas, E. F., Brawner, W. R., and Lewis, R. Y. (1949). Report <strong>of</strong> poisoning two dogs<br />

with 1080 rat poison. Journal <strong>of</strong> the American Veterinary Medical Association 115, 355-356.<br />

Keywords: poisoning/dogs/1080/symptoms/convulsions/welfare/treatment/diagnosis<br />

Abstract: From these observations and the cases brought to our clinic, we consider the following symptoms<br />

to be characteristic <strong>of</strong> 1080 poisoning; extreme pain manifested by running and barking, convulsions <strong>of</strong> the<br />

tetanic type with ophisthotonos. Death follows first symptoms in thirteen to thirty minutes. We have had<br />

two cases to recover from 1080 poisoning, which in our opinion received only a very small amount <strong>of</strong> the<br />

poison. The health department has discontinued the use <strong>of</strong> 1080 in our county.<br />

Nieschalk, J., Hamilton, J. T. G., Murphy, C. D., Harper, D. B., and O'Hagan, D. (1997). Biosynthesis <strong>of</strong><br />

fluoroacetate and 4-fluorothreonine by Streptomyces cattleya. The stereochemical processing <strong>of</strong> glycerol.<br />

Chemical Communications 799-800.<br />

Keywords: biosynthesis/fluoroacetate<br />

Abstract: When both (2R)-[1- 2 H2]- and (2S)-[1- 2 H 2]-glycerol are incubated with resting cell suspensions <strong>of</strong><br />

S. cattleya, only the 2R-enantiomer labels the fluoromethyl groups <strong>of</strong> fluoroacetate and 4-fluorothreonine,<br />

with retention <strong>of</strong> both deuterium atoms, placing metabolic and mechanistic limitations on the process <strong>of</strong><br />

biological fluorination.<br />

Nigrovic, V. and Cafruny, E. J. (1974). Renal concentration <strong>of</strong> citrate as a negative modulator <strong>of</strong> diuretic<br />

response to mercurials. Nature 247, 381-383.<br />

Keywords: citrate/metabolism/excretion/kidney/dogs/persistence in animals<br />

Noguchi, T, Ohnuki, Y., and Okigaki, T. (1966). Effect <strong>of</strong> sodium fluoroacetate on myocardial cells in<br />

vitro. Nature 209, 1197-1198.<br />

Keywords: sodium fluoroacetate/fluoroacetate/heart/mode <strong>of</strong> action/cardiac/Krebs<br />

cycle/metabolism/poisoning<br />

Abstract: It is not known whether the response <strong>of</strong> the cardiac tissue is mediated through an interruption <strong>of</strong><br />

the vagus control or through its own dependence on Krebs cycle metabolism. Myocardial cells in vitro were<br />

utilised to examine this question. It is interesting to note that cardiac fibrillation observed in cases <strong>of</strong><br />

sodium fluoroacetate poisoning in man and animals is also recorded in isolated myocardial cells treated in<br />

tissue culture. The absence <strong>of</strong> nerve tissue in this in vitro preparation indicates that fibrillation results from<br />

a direct effect on the myocardial cells.<br />

Noguchi, T, Hashimoto, Y., and Miyata, H. (1968). Studies <strong>of</strong> the biochemical lesions caused by a new<br />

fluorine pesticide, N-ethyl-N-(I-napthyl)mon<strong>of</strong>luoroacetamide. Toxicology and applied phamacology 13,<br />

189-198.<br />

Keywords: fluorine/fluoroacetamide/mammals/testes/mon<strong>of</strong>luoroacetic<br />

acid/citrate/heart/kidney/rats/liver/metabolism/acute toxicity/enzyme<br />

Abstract: N-ethyl-N-(I-napthyl)mon<strong>of</strong>luoroacetamide (MNFA), a derivative <strong>of</strong> mon<strong>of</strong>luoroacetic acid, is an<br />

effective pesticide with low toxicity for most mammals. The biochemical effect <strong>of</strong> this compound was<br />

investigated. After a single dose the citrate levels rose in the heart <strong>of</strong> the rat and monkey and in the kidney<br />

<strong>of</strong> the guinea-pig. A chronic toxicity experiment showed that there was an increase in the citrate level only<br />

in the testis <strong>of</strong> rats receiving 10 mg/kg/day <strong>of</strong> MNFA for 180 days and a decrease in the level in the liver<br />

and kidney as compared with animals receiving a single dose. The lack <strong>of</strong> toxicity associated with chronic<br />

administration may be due to accelerated detoxication (sic) in the liver and kidney as a consequence <strong>of</strong><br />

metabolism in the animal body. The hydrolysis on MNFA by liver homogenates was closely related to the<br />

acute toxicity. The enzyme activity in the guinea-pig was about 35 times that <strong>of</strong> the rat or mouse. The<br />

product <strong>of</strong> the hydrolysis <strong>of</strong> MNFA by liver homogenates <strong>of</strong> guinea-pigs, rats and mice was N-methyl-1napthylamine.<br />

The LD50 <strong>of</strong> MNFA, a N-CH3 compound <strong>of</strong> NFA, was 3.1 times that <strong>of</strong> NFA, and the<br />

amount hydrolysed after 30 minutes incubation was about one-fifth.<br />

Norbury, G. L. The use <strong>of</strong> 1080 to control feral goats in Western Australia. Agriculture Protection Board <strong>of</strong><br />

Western Australia. 1992.<br />

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Ref Type: Report<br />

Keywords: 1080/goats<br />

Abstract: The minimum conc. <strong>of</strong> 1080 to kill 100% <strong>of</strong> goats was estimated from yard trials to be 7 mg <strong>of</strong><br />

1080 per litre <strong>of</strong> water. This equates to a dose <strong>of</strong> 1.4 mg/kg. There appeared to be minimal suffering from<br />

poisoning.<br />

If precautions are not taken to prevent non-target species from drinking, Zebra Finches, Budgerigars and<br />

some Galahs will be at risk <strong>of</strong> poisoning. Other bird species are resistant to 1080 at the poisoning rates<br />

required to kill goats. When inverted sheet metal guttering was applied to the edges <strong>of</strong> poisoned troughs,<br />

birds could not perch safely when attempting to drink. Provided an alternative watering trough was<br />

available, birds rarely drank from the poisoned troughs. Some kangaroos will also be at risk from<br />

poisoning unless poison is removed at the recommended time <strong>of</strong> 1200 hr.<br />

It is technically feasible to selectively poison feral goats with 1080 provided the appropriate safeguards are<br />

adopted to protect non-target species. Six guidelines are recommended for goat poisoning campaigns.<br />

Norris, R. The federal animal damage control program. Audubon Wildlife Report 1987, 223-238. 1987.<br />

Ref Type: Report<br />

Keywords: 1080/ground control/regulatory toxicology/livestock protection collar/legislation/USA<br />

Norris, W. R., Temple, W. A., Eason, C. T., Wright, G. R., Ataria, J., and Wickstrom, M. L. (2000).<br />

Sorption <strong>of</strong> fluoroacetate (compound 1080) by colestipol, activated charcoal and anion-exchange resins in<br />

vitro and gastrointestinal decontamination in rats. Veterinary and human toxicology 42, 269-275.<br />

Keywords: treatment/1080/sodium fluoroacetate/antidote<br />

Notman, P. (1989). A review <strong>of</strong> invertebrate poisoning by compound 1080. New Zealand entomologist 12,<br />

67-71.<br />

Keywords: non-target species/invertebrates/1080/birds/mammals/secondary poisoning<br />

Abstract: Compound 1080 is widely used in New Zealand for the control <strong>of</strong> wild animals. The tendency <strong>of</strong><br />

1080 to poison non-target birds and mammals is recognised, but its effects on invertebrates have gone<br />

mostly unnoticed. At least 9 invertebrate orders are prone to 1080 poisoning. Invertebrates have been<br />

observed eating baits, and their habitats are contaminated by residues leaching from baits, and from animal<br />

by-products and carcasses. Poisoned insects leaching from baits, and from animal by-products and<br />

carcasses. Poisoned insects provide a means <strong>of</strong> secondary poisoning for insectivores . Therefore 1080<br />

should not be used where susceptible invertebrate species or rare insectivores are found.<br />

Novak, L., Misustova, J., and Hosek, B. (1968). The effects <strong>of</strong> sodium fluoroacetate on the respiratory<br />

exchange in mice and rats. Physiologia bohemoslovaca 17, 97-103.<br />

Keywords: fluoroacetate/rats/sodium fluoroacetate/temperature/citric acid/mode <strong>of</strong> action<br />

Abstract: It was found in mice and rats that an intraperitoneal injection <strong>of</strong> sodium fluoroacetate in sublethal<br />

doses <strong>of</strong> 2.5 to 7.5 mg/kg produces a sharp decrease in the resting vales <strong>of</strong> carbon dioxide output and<br />

oxygen consumption within 60 to 90 minutes after application. In mice, the values <strong>of</strong> respiratory echange<br />

decrease within 2 to 5 hours following the injection <strong>of</strong> sodium fluoroacetate to a mere 15 to 20 per cent <strong>of</strong><br />

the initial values. The decrease <strong>of</strong> respiatory exchange coincides with the decrease <strong>of</strong> rectal temperature and<br />

falls into the period when citric acid accumulates in the body tissues and when the sensitivity <strong>of</strong> the<br />

organism to irradiation occurs. The results are interpreted in favour <strong>of</strong> the hypothesis on the importance <strong>of</strong><br />

the level <strong>of</strong> metabolic processes in the organism for its sensitivity to irradiation.<br />

Novak, L., Sikulova, J., Hosek, B., and Misustova, J. (1969). Radioprotective effect <strong>of</strong> sodium<br />

fluoroacetate in mice. Radiation <strong>Research</strong> 40, 430-439.<br />

Keywords: fluoroacetate/metabolism/mode <strong>of</strong> action<br />

Abstract: A quantitative study <strong>of</strong> the radioprotective effect <strong>of</strong> sodium fluoroacetate (FAc) in white mice <strong>of</strong><br />

H-strain, 9-12 weeks old was made. The results <strong>of</strong> the experiment showed that FAc administered<br />

intraperitoneally 3 hours before irradiation in the amount <strong>of</strong> 7.5 mg/kg increases the average LD 50(30)<br />

values from 648 R (controls) to 998 R (protected). A comparison <strong>of</strong> the obtained results with data on the<br />

radioprotective effect <strong>of</strong> cysteine, cysteamine, AET, serotonin and hypoxia indicates that the<br />

radioprotective effect <strong>of</strong> FAc is not statistically different from the effect <strong>of</strong> these compounds. The<br />

protective effect <strong>of</strong> FAc , however, requires much smaller doses (50-75 u moles/kg). At the same time, the<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

duration <strong>of</strong> protection after FAc administration is much longer, lasting roughly from 30 minutes to 7 hours<br />

after the application <strong>of</strong> the substance, with maximum protection between the first and second hour.<br />

Novak, L., Misustova, J., and Hosek, B. (1972). Course <strong>of</strong> respiratory exchange and body temperature in<br />

mice after repeated administration <strong>of</strong> fluoroacetate: an indicator <strong>of</strong> aconitase activity in vivo. Physiol<br />

Bohemoslov 21, 53-61.<br />

Keywords: temperature/fluoroacetate/aconitase/fluorocitrate/enzyme/Krebs cycle<br />

Abstract: Fluorocitrate formed by lethal synthesis from injected fluoroacetate blocks the enzyme aconitase<br />

and hence the course <strong>of</strong> Krebs cycle reactions. This is manifested in a temporary decrease in respiatory<br />

exchange and body temperature. In male strain H mice given doses <strong>of</strong> 2.5 and 5 mg/kg, respiratory<br />

exchange recovered and returned to the initial level 24-72 hours after the injection. On administering a<br />

second FAc injection at different intervals after the first, a further and greater decrease in respiratory<br />

exchange and body temperature was found. Actinomycin D and cycloheximide prolonged the recovery<br />

period. This means that the observed recovery <strong>of</strong> respiratory exchange and body temperature are an<br />

expression <strong>of</strong> renewed aconitse activity and that the block <strong>of</strong> the enzyme is followed not by an adequate<br />

compensatory by-pass reaction, but by the induction <strong>of</strong> new aconitase molecules.<br />

Novak, L., Kolacny, I, Sikulova, J., and Vlkova, G. (1974). Resistance <strong>of</strong> the fluorocitrate-aconitase<br />

complex to natural inactivation and heat denaturation in vivo. Physiologia bohemoslovaca 23, 555-565.<br />

Keywords: fluorocitrate/aconitase/biochemistry/temperature/heart/kidney/liver/enzyme/sodium<br />

fluoroacetate/fluoroacetate<br />

Abstract: In experiments with heart, kidney and liver homogenates from male strain H mice (aged nine<br />

weeks), it was found that the addition <strong>of</strong> synthetic sodium fluorocitrate to organ homogenates in vitro<br />

raised the in vitro resistance <strong>of</strong> aconitase to inactivation during storage <strong>of</strong> crude extract <strong>of</strong> the enzyme at<br />

low temperatures, in the same way as fluorocitrate formed in the organs in vivo by Peter's lethal synthesis<br />

from injected sodium fluoroacetate (FAc). Raised resistance <strong>of</strong> aconitase to heat denaturation at 50, 55, 60<br />

and 65 degrees celcius was likewise demonstrated in homogneates or organs removed at 2 hours after the<br />

i.p. injection <strong>of</strong> a radioprotective dose <strong>of</strong> FAc (50 u mol/kg). The results support the authors hypothesis that<br />

the presence <strong>of</strong> the FCTR molecule, bound to the aconitase molecule "protects" the enzyme against natural<br />

inactivation during storage at low temperatures and raises its resistance to heat denaturation.<br />

Nugent, G., Fraser, K. W., Asher, G. W., and Tustin, K. G. (2001). Advances in New Zealand mammalogy<br />

1999-2000: deer. Journal <strong>of</strong> the <strong>Royal</strong> Society <strong>of</strong> New Zealand 31, 263-298.<br />

Keywords: deer/non-target species/1080/aerial control<br />

Nugent, G. and Yockney, I. Fallow deer deaths during aerial poisoning <strong>of</strong> possums in the Blue Mountains,<br />

Otago. <strong>Landcare</strong> <strong>Research</strong> Contract Report LC0102/044, -27. 2001.<br />

Ref Type: Report<br />

Keywords: deer/aerial control<br />

Nugent, G. and Yockney, I (2004). Fallow deer deaths during aerial-1080 poisoning <strong>of</strong> possums in the Blue<br />

Mountains, Otago, New Zealand. New Zealand journal <strong>of</strong> zoology 31, 185-192.<br />

Keywords: deer/poisoning/possums/New Zealand/brushtail possum/baits/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/Tb<br />

Abstract: Incidental kills <strong>of</strong> deer during aerial-1080 poisoning <strong>of</strong> brushtail possums (Trichosurus vulpecula)<br />

using baits containing sodium mon<strong>of</strong>luoroacetate (1080) causes widespread hunter opposition to this<br />

control method. We document the deaths <strong>of</strong> a large number <strong>of</strong> fallow deer (Dama dama) after aerial-1080<br />

poisoning in the Blue Mountains, Otago. Three deer fitted with radio collars all died during the poisoning.<br />

Eight randomly located "search cells" (25-57 ha) were each searched twice. One pig (Sus scr<strong>of</strong>a), 53 deer,<br />

58 possum, and 20 bird (three native) carcasses were found. Deer-carcass density varied widely between<br />

cells (2.2-38.6/km 2 ), reflecting differences in deer density but apparently also the amount <strong>of</strong> ground cover.<br />

The total number <strong>of</strong> deer killed was estimated using Lincoln indices. More fawns were killed than larger<br />

adult deer. Comparison with historical harvest data suggested that between two-thirds and three-quarters <strong>of</strong><br />

the deer present had been killed. This unintended by-kill will have reduced deer impacts on native plants<br />

and the risk <strong>of</strong> Tb spread or persistence in deer. However, such incidental benefits may not <strong>of</strong>fset the<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

increased indirect "social" costs likely to arise from increased hunter opposition to use <strong>of</strong> aerial-1080<br />

poisoning.<br />

Nwude, N. and Parsons, L. E. (1977). Nigerian plants that may cause poisoning in livestock. Veterinary<br />

Bulletin 47, 811-817.<br />

Keywords: poisoning/livestock/cardiac/fluoroacetate/occurrence in nature<br />

Abstract: This review covers 60 spp. <strong>of</strong> plants which are potential sources <strong>of</strong> poisoning to livestock in<br />

Nigeria. The plants are listed, with a little information on each, under the toxic constituents, as follows:<br />

cyanogenetic glycosides, cardiac glycosides, alkaloids, fluoroacetate, oxalates, saponins, miscellaneous and<br />

unknown toxic constituents. Also included are some spp. which cause mechanical injury, through sharp<br />

awns, burrs, spines or thorns, or cause ulcers or hair balls in the digestive tract<br />

Nwude, N., Parsons, L. E., and Adaudi, A. O. (1977). Acute toxicity <strong>of</strong> the leaves and extracts <strong>of</strong><br />

Dichapetalum barteri (Engl.) in mice, rabbits and goats. Toxicology 7, 23-29.<br />

Keywords: acute<br />

toxicity/toxicity/rabbits/goats/convulsions/liver/kidney/spleen/heart/mon<strong>of</strong>luoroacetate/occurrence in<br />

nature<br />

Abstract: Acute toxicity <strong>of</strong> the leaves and extracts <strong>of</strong> Dichapetalum barteri for mice, rabbits and goats was<br />

investigated. Consumption <strong>of</strong> 0.5 g/kg and 2.2 g/kg body weight <strong>of</strong> dried leaves was lethal to rabbits and<br />

goats, respectively, within 4 h. Plants collected in the dry season were more toxic than those collected<br />

during the wet season. Clinical signs observed were initial depression followed by restlessness,<br />

convulsions, and death. The main lesions observed were acute vasculitis and congestion <strong>of</strong> the liver, lung,<br />

kidney, spleen as well as extensive oedema and congestion <strong>of</strong> the myocardium. The water extract <strong>of</strong> the<br />

leaves was lethal to mice at 2.0 g/kg, to rabbits at 0.1 g/kg and toxic to isolated rabbit heart at 2 mg/ml <strong>of</strong><br />

Locke's solution. Mon<strong>of</strong>luoroacetate was detected in the plant material and is probably the toxic principle<br />

<strong>of</strong> D. barteri<br />

O' Connor, C. E., Airey, A. T., and Littin, K. E. Relative humaneness assessment <strong>of</strong> possum <strong>poisons</strong>.<br />

LC0203/158, -20. 2003. Lincoln, New Zealand, <strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Report<br />

Keywords: <strong>poisons</strong>/poison/brodifacoum/cyanide/possums/1080/welfare/poisoning/cholecalciferol<br />

Abstract: (outcomes) In summary, cyanide caused mild abnormal breathing in 52% <strong>of</strong> the poisoned<br />

possums and convulsion occurred in all animals after they had become unconscious. For 1080 there is<br />

potential welfare compromise for 9.5 hours following poisoning. A small percentage <strong>of</strong> possums posioned<br />

with 1080 had mild to moderate retching , most became uncoordinated and then all had mild to moderate<br />

tremors or spasms. The main welfare concern with phosphorus is the congestion is the congestion <strong>of</strong> the<br />

gastric mucosa, which was linked to the adoption <strong>of</strong> a crouching posture. This was probably assocaited with<br />

some mild pain and lasted for 10 h until possums became prostrate. Cholecalciferol caused mineralisation<br />

in the organs <strong>of</strong> 67% <strong>of</strong> possums and lung damage in 59% <strong>of</strong> the animals. Seventy-one percent <strong>of</strong> possums<br />

had abnormal breathing for 1.5 days before death. They did not eat for 7 days, on average, and 21% lost<br />

more than 30% <strong>of</strong> their bodyweight. Finally, brodifacoum caused widespread haemorrhages <strong>of</strong> varying<br />

severity in all animals. The welafre consequences depended on the site and severity <strong>of</strong> the haemorrhages,<br />

which makes it difficult to generalise the welfare impact <strong>of</strong> this poison. Nevertheless, all animals had at<br />

least one severe haemorrhage in an area that would cause or contribute to pain, distress or weakness. In<br />

addition, in order to describe a refined humane end-point for effeicayc testing, we determined that the<br />

behaviour shown by most possums across all <strong>poisons</strong> was a prolonged period <strong>of</strong> prostration or lying, on the<br />

side, back or belly. We have defined prolonged in this case as a continuous 2 hours or more. If this refined<br />

end-point (prolonged period <strong>of</strong> prostration), had been used there would have been a significant reduction,<br />

<strong>of</strong> several hours, in the period <strong>of</strong> suffering for many animals tested.<br />

O'Brien, P. and Korn, T. (1995). 1080 - for pest control in New South Wales. Agfacts Department <strong>of</strong><br />

Agriculture, New South Wales No. A9.0.18, 1-4.<br />

Keywords: 1080/mode <strong>of</strong> action/humans/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate<br />

Abstract: Details are given <strong>of</strong> the characteristics, mode <strong>of</strong> action, persistence in the environment, suitability,<br />

usage in New South Wales and risk to humans <strong>of</strong> sodium mon<strong>of</strong>luoroacetate [sodium fluoroacetate]<br />

(known as 1080), which is used widely to control vertebrate pests in Australia<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

O'Brien, P. H., Kleba, R., Beck, J. A., and Baker, P. J. (1986). Vomiting by feral pigs after 1080<br />

intoxication: nontarget hazard and influence <strong>of</strong> anti-emetics. Wildlife Society bulletin 14, 425-432.<br />

Keywords: pigs/1080/symptoms/non-target species/efficacy<br />

Abstract: We examined vomiting by feral pigs after 1080 intoxication and tested the effectiveness <strong>of</strong><br />

metoclopramide in suppressing emesis. Most pigs vomited repeatedly after 1080 intoxication. At the doses<br />

tested (1,4 and 16 mg/kg) metoclopramide did not reduce the frequency <strong>of</strong> vomiting, but decreased the<br />

proportion <strong>of</strong> a pig's 1080 dose that was ejected by decreasing the amount <strong>of</strong> vomitus produced. Becuase <strong>of</strong><br />

wide individual variability in response, and the small sample size, there was no signficant effect <strong>of</strong><br />

metoclopramide on mortality. Overall mortality was lower than expected. Vomitus varied widely in mass,<br />

1080 concentration and 1080 content. Typical levels <strong>of</strong> 1080 in vomitus would be hazardous to a number <strong>of</strong><br />

nontarget species and peak levels hazardous to most. Other feral pigs are unlikely to be poisoned by<br />

consuming vomitus.<br />

O'Brien, P. H., Beck, J. A., and Lukins, B. Residual tissue levels <strong>of</strong> warfarin and 1080 in in poisoned feral<br />

pigs. 1987. Australian Vertebrate Pest <strong>Control</strong> Conference, Coolangatta, Queensland.<br />

Ref Type: Conference Proceeding<br />

Keywords: residues/pigs/warfarin/1080/distribution/liver<br />

Abstract: We measured the distribution and persistence <strong>of</strong> warfarin and 1080 in the tissues <strong>of</strong> captive feral<br />

pigs <strong>of</strong>fered toxins in wheat in a choice experiment. Compound 1080 was found in low levels in all tissues<br />

tested except fat. Warfarin was concentrated in the liver <strong>of</strong> poisoned animals. Liver levels <strong>of</strong> warfarin were<br />

well correlated with levels in other tissues. Liver may be a useful tissue for asaay for diagnostic purposes.<br />

Both toxins declined to very low levels over time, with no evidence <strong>of</strong> persistence. Samples obtained from<br />

pigs in the field had extermely high warfarin levels, indicating cumulation with repeated dosing.<br />

O'Brien, P. H., Lukins, B. S., and Beck, J. A. (1988). Bait type influences the toxicity <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (Compound 1080) to feral pigs. Australian wildlife research 15, 451-457.<br />

Keywords: high-performance liquid chromatography/acute toxicity/mammals/1080/sodium<br />

mon<strong>of</strong>luoroacetate/pigs<br />

Abstract: The toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) to captive feral pigs was compared in wheat<br />

and pellet bait. Morality following 4-34 mg 1080 kg-1 was significantly higher among pigs receiving 1080<br />

in wheat bait (60%, 24/40) than in pellet bait (28% 11/40, x2 = 7.31, 1 d.f., P< ,0.05). There were no<br />

significant differences between pigs receiving each bait type in terms <strong>of</strong> time until vomiting began,<br />

frequency, mass <strong>of</strong> vomitus produced. or in time until death. The amount and concentration <strong>of</strong> 1080 in<br />

vomitus and the proportion <strong>of</strong> 1080 dose ejected were unrelated to bait type. Surviving pigs produced<br />

vomitus with a greater 1080 concentration but smaller mass than those that died. Bait type is an important<br />

determinant <strong>of</strong> the toxicity <strong>of</strong> 1080 to captive feral pigs and should be closely evaluated before speicifc bait<br />

types are used in the field.<br />

O'Brien, P. H. (1988). The toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (compound 1080) to captive feral pigs,<br />

Sus scr<strong>of</strong>a. Australian wildlife research 15, 163-170.<br />

Keywords: acute toxicity/mon<strong>of</strong>luoroacetate/1080/pigs/symptoms<br />

Abstract: The toxicity <strong>of</strong> sodium fluoroacetate (1080) to captiveferal pigs was assessed over a range <strong>of</strong><br />

doses (1.50 - 21.3 mg/kg) administered orally in wheat bait to 80 animals. Calculated LD50 dose was 4.11<br />

mg/kg (95% fiducial limits 3.02 - 5.34 mg/kg) and LD90 was 11.25 mg/kg (8.05 - 21.69 mg/kg). The<br />

incidence (985) and frequency <strong>of</strong> vomiting were high. Frequency <strong>of</strong> vomiting was unrelated to log10 dose,<br />

although time until vomiting began and time until death had a significant neagtive association with log10<br />

dose. Medina latency was 49 mintes and median timeuntil death was 244 minutes.Sex and bodyweight had<br />

no effect on frequency <strong>of</strong> vomiting, time until death or prognosis. Feral pigs were much less sensitive to<br />

1080 under these test conditions than those in earlier studies.<br />

O'Brien, P. H. and Lukins, B. S. (1988). Factors influencing the intake <strong>of</strong> sodium mon<strong>of</strong>luoroacetate<br />

(Compound 1080) by free-ranging feral pigs. Australian wildlife research 15 , 285-291.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/pigs/stomach/baits<br />

Abstract: Post-mortem investigations <strong>of</strong> 207 feral pigs poisoned in the field were conducted to assess the<br />

influence on 1080 dose <strong>of</strong> bait type, site, sex, bodyweight and distance from bait stations. The stomachs <strong>of</strong><br />

most (126/207) pigs contained only bait material. Bait type significantly affected intake and 1080 dose,<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

with pellet intake greater than cereal baits. Sex and bodyweight also influenced intake: females ingested<br />

significantly larger 1080 doses than males; and larger pigs tended to consume more bait in absolute terms<br />

but lower doses <strong>of</strong> 1080 (mg kg-1). Average intake <strong>of</strong> 1080 varied widely at different locations. Pigs that<br />

died close to bait stations had higher 1080 doses but smaller proportions <strong>of</strong> bait in their stomach contents<br />

than those that died away from bait stations<br />

O'Connor, C. E., Milne, L. M., Arthur, D. G., Ruscoe, W. A., and Wickstrom, M. (1999). Toxicity effects<br />

<strong>of</strong> 1080 on pregnant ewes. Proceedings <strong>of</strong> the New Zealand Society <strong>of</strong> Animal Production 59, 250-253.<br />

Keywords: acute toxicity/non-target<br />

species/mammals/pathology/1080/treatment/livestock/baits/poisoning/reproductive effects/developmental<br />

toxicity<br />

Abstract: There are no data on the potential for 1080 used for pest control to cause delayed deaths or<br />

impaired productivity in livestock following multiple, sub-lethal doses. Recent losses <strong>of</strong> late-gestation<br />

ewes exposed to weathered 1080 baits has also led to speculation that pregnant ewes may be unusually<br />

sensitive to the toxin. TO address these data gaps, groups <strong>of</strong> 20 Perendale ewes, non-pregnant or pregnant<br />

with twins, were administered either a single (0.25 mg/kg) or multiple oral doses (0.05 mg/kg over 3<br />

consecutive days) <strong>of</strong> a 1080 cereal pellet. The highest mortality occurred in the single does groups<br />

(pregnant 45%, non-pregnant 21%) compared to the multiple doses groups (pregnant 35%, non-pregnant<br />

0%). There was no mortality in the control group <strong>of</strong> pregnant ewes. Log-linear modelling showed highly<br />

significant treatment effects (P+0.0003) and differences (P=0.045) in acute mortality rates between<br />

pregnant (40%) and non-pregnant ewes (10%), which was linked to increase bioavailability. There were no<br />

differences in the incidence <strong>of</strong> metabolic diseases, lambing percentages, lamb survival, or growth rates<br />

between dosed and undosed pregnant ewes. This study demonstrated that extra care should be taken to<br />

avoid exposure to pregnant ewes to even small bait fragments, but also provides further evidence that there<br />

are no long term health effects in animal that survive accidental 1080 poisoning.<br />

O'Connor, C. E., Morgan, D. R., and Wickstrom, M. (1999). The development <strong>of</strong> alternatives to 1080 for<br />

possum control. (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Lincoln.)<br />

Keywords: possums/acute toxicity/1080/zinc phosphide/lethal dose<br />

Abstract: Objectives: To develop alternative <strong>poisons</strong> to 1080 for the effective and humane control <strong>of</strong><br />

possums, by determining the palatability and efficacy <strong>of</strong> a zinc phosphide cereal bait to possums;<br />

determining the palatability and efficacy <strong>of</strong> a cholecalciferol gel bait to possums; determining the efficacy<br />

and cost effectiveness <strong>of</strong> these new zinc phosphide and cholecalciferol baits for possums control, in field<br />

trials. Conclusions: Zinc phosphide cereal bait Zinc phosphide is an effective toxicant in cereal baits for<br />

possums. It is uniformly lethal to animals ingesting only 3 g <strong>of</strong> bait containing 2% active ingredient. Many<br />

possums apparently detect the odour and / or taste <strong>of</strong> zinc phosphide, and reject the bait in spite <strong>of</strong> efforts to<br />

mask the toxicant. About 40% <strong>of</strong> captive ani9mals <strong>of</strong>fered the best cereal bait formulation in two-choice<br />

trials did not ingest a lethal dose. Zinc phosphide-coated grain bits developed for rodent control are not<br />

appropriate for possums. Cholecalciferol gel bait The cholecalciferol gel bait is palatable and effective in<br />

pen trials with captive possums. There is no difference in efficacy <strong>of</strong> formulations containing from 0.66%<br />

and 1.0% cholecalciferol. The LD50 for possums for cholecalciferol in the gel matrix is < 12mg/kg, which<br />

is similar to LD50 values obtained with current formulations <strong>of</strong> Campaign cholecalciferol cereal bait.<br />

Cholecalciferol gel was at least as effective as prefed 1080 pellets in replicated field trials. The most likely<br />

cause was the poor kills in these trials was the abundance <strong>of</strong> natural foods in the summer and possums'<br />

consequent disinterest in artificial baits.<br />

O'Connor, C. E. and Matthews, L. R. (1999). 1080-induced bait aversions in wild possums: influence <strong>of</strong><br />

bait characteristics and prevalence. Wildlife research 26, 375-381.<br />

Keywords: possums/1080/baits/efficacy/aversion/bait shyness<br />

Abstract: The current experiment aimed to determine the proportion <strong>of</strong> wild-caught from previously<br />

poisoned and non-poisoned populations that developed aversions to 1080 baits. In addition, we aimed to<br />

identify the bait characteristics mediating the ongoing aversions. In an initial test, animals from areas<br />

previously exposed to a 1080 control-operation avoided 1080 baits (60-80%), whereas few naive animals<br />

(0-20%) avoided these baits. The baits comprised a green-dyed, cinnamon-lured cereal loaded with 0.08%<br />

1080. As a result <strong>of</strong> the exposure to the toxic baits, over 80% <strong>of</strong> the naive animals subsequently developed<br />

aversions to those baits. Sixty-nine <strong>of</strong> these averse animals were allocated to on <strong>of</strong> 16 bait-treatment groups<br />

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in a factorail design balanced for population, age,sex and bodyweight. Each bait was characterised by one<br />

<strong>of</strong> four factors a) presence or absence <strong>of</strong> 1080 b) presence or absence <strong>of</strong> green dye c) lure type (cinnamon<br />

or orange) and d) bait type (No.7 or carrot). The presence or absence <strong>of</strong> 1080 or green dye did not influence<br />

the degree <strong>of</strong> bait avoidance. Lure type had a signficant effect on consumption, with 53% <strong>of</strong> possums<br />

avoiding an orange bait compared with 73% for cinnamon baits. Bait type also has a significant effect on<br />

avoidance rates, with carrot baits being avoided by 42% <strong>of</strong> possums compared with 83% for No. 7 baits.<br />

Changing the bait type would appear to hold the greatest promise for overcoming aversiosn by possums to<br />

cereal baits.<br />

O'Connor, C. E., Eason, C., and Fountain, J. S. Assessing exposure risks to 1080 workers in New Zealand.<br />

LC9900/98, 1-19. 2000. <strong>Landcare</strong> <strong>Research</strong> Contract Report.<br />

Ref Type: Report<br />

Keywords: 1080/blood/urine/carrot/humans/analysis/occupational exposure<br />

Abstract: In those areas where either the Workplace Exposure Standard has been exceeded, or a<br />

Level 3 exposure has been found, standard procedures need to be reviewed and more rigorously enforced.<br />

We recommend further immediate monitoring, at the factories and aerial carrot operation sites, to<br />

ensure that improvements in procedures do reduce the 1080 exposure risk.<br />

$ The exposure level <strong>of</strong> workers involved in laying 1080 paste bait needs to be determined (i.e.<br />

determine if detectable levels <strong>of</strong> 1080 are present in urine samples).<br />

$ A goal should be no measurable biological exposure (Level 1), which can be achieved by<br />

encouraging the use <strong>of</strong> work practices (e.g. foot pedal taps, face masks, clean gloves) that can be shown to<br />

minimise risk <strong>of</strong> worker exposure to 1080.<br />

$ A representative sample <strong>of</strong> staff working with 1080 should be monitored at least annually to<br />

ensure continual minimal risk <strong>of</strong> exposure.<br />

$ The risk to worker health needs to be assessed by comparing measured daily exposures with<br />

acceptable maximum doses for chronic exposure derived from ongoing animal dietary exposure studies.<br />

$ The health <strong>of</strong> highly exposed 1080 workers should be monitored through occupational physicians<br />

or an epidemiological investigation.<br />

$ A human health risk assessment should be undertaken that includes hazard identification, doseB<br />

response relationship and risk characterisation (acute and chronic).<br />

$ These unique data should be published in a peer-reviewed clinical toxicology journal to<br />

demonstrate the recognition <strong>of</strong> these risks by our pest control industry.<br />

O'Connor, C. E., Littin, K., and Eason, C. Assessing the humaneness <strong>of</strong> <strong>poisons</strong> used for possum control. -<br />

53. 2000. Lincoln New Zealand, <strong>Landcare</strong> <strong>Research</strong> New Zealand. Australasian Wildlife Management<br />

Society 13th Annual Conference, 28 Nov-1 Dec 2000, Queenstown New Zealand.<br />

Ref Type: Conference Proceeding<br />

Keywords:<br />

<strong>poisons</strong>/wildlife/possums/poisoning/cyanide/1080/cholecalciferol/brodifacoum/behaviour/poison/welfare/ti<br />

me to death<br />

Abstract: Wildlife managers have the responsibility to use the most humane methods available for pest<br />

control. However, data have not been available to identify practices that meet these expectations. We have<br />

assessed the behavioural, biochemical and pathological chnages in caged possums following poisoning<br />

with cyanide, 1080, phosphorus, cholecalciferol or brodifacoum. The eman time until death, mean duration<br />

<strong>of</strong> illness, and the type and prevalence <strong>of</strong> changes in behaviour differed between <strong>poisons</strong>. On average death<br />

occurred 18 minutes after cyanide, 11.5 hours after 1080, 18 hours after phosphorus, 9 days after<br />

cholecalciferol and 20 days after brodifacoum poisoning. Main behavioural changes included:<br />

incoordination and unconsciousness within 7 minutes after cyanide poisoning; retching during an 8-hour<br />

illness period after 1080; restlessness and a crouching posture for 16 hours after phosphorus; inappetance<br />

and listlessness for 47 before death after cholecalciferol; and listlessness and abnormal postures for 6 days<br />

before death after brodifacoum poisoning. Cyanide is therefore the most preferred posion from a welfare<br />

perspective. Phosphorus and brodifacoum appear less humane than 1080, cholecalciferol, or cyanide.<br />

O'Connor, C. E., Milne, L., Wright, G., and Eason, C. Poison residues in our meat and milk. He Korero<br />

Paihama - Possum <strong>Research</strong> News 15, 10. 2001. <strong>Landcare</strong> <strong>Research</strong>, PO Box 69, Lincoln, New Zealand.<br />

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Ref Type: Magazine Article<br />

Keywords: 1080/humans/secondary poisoning/persistence in animals<br />

O'Connor, C. E., Fountain, J. S., and Eason, C. Worker exposure to 1080. LC0001/56, 1-9. 2001. <strong>Landcare</strong><br />

<strong>Research</strong> Contract Report.<br />

Ref Type: Report<br />

Keywords: 1080/carrot/humans/analysis/urine/blood/occupational exposure<br />

Abstract: • 'False' positives through contamination need to be conclusively eliminated, by increased<br />

diligence during sampling (e.g., monitored washing before all sampling) in the future.<br />

• The source <strong>of</strong> worker exposure needs to be identified and then isolated through (i) engineering<br />

controls (e.g., splash guards) and (ii) more rigorous use <strong>of</strong> Personal Protective Equipment (e.g., glove<br />

liners, or to continually wear a clean face mask).<br />

• The three exposure levels used to describe the results in this study must not be considered as<br />

classified hazard levels. A Biological Exposure Index for future routine monitoring will be developed by<br />

the Occupational Safety and Health Service.<br />

• Work practices that can be shown, by biological monitoring, to adequately protect workers need to<br />

be determined.<br />

• Further immediate biological monitoring at more aerial carrot operation sites is required to ensure<br />

that changes in procedures and practices do reduce the 1080 exposure risk to acceptable levels.<br />

• Once these levels are achieved, annual or biannual biomonitoring <strong>of</strong> a representative sample <strong>of</strong> all<br />

1080 workers to ensure continual good practice and minimal risks <strong>of</strong> exposure should be enforced.<br />

O'Hagan, D., Perry, R., Lock, J. M., Meyer, M., Dasaradhi, L., Hamilton, D. J., and Harper, D. B. (1993).<br />

High levels <strong>of</strong> mon<strong>of</strong>luoroacetate in Dichapetalum braunii. Phytochemistry 33, 1043-1045.<br />

Keywords: occurrence in nature/fluoride/fluoroacetate<br />

Abstract: Mon<strong>of</strong>luoroacetate occurs in young leaves and seed <strong>of</strong> Dichapetalum braunii Engl. & K. Krause<br />

from southeat Tanzania at concentrations <strong>of</strong> 7200 and 8000 ppm, respectively, on a dry weight basis. This<br />

is the highest level so far reported from a plant source. The fluoride and mon<strong>of</strong>luoroacetate (MFA)<br />

concentrations in this species are comapred with those <strong>of</strong> six other Dichapetalum spp. collected from the<br />

same locality in Tanzania. The seeds <strong>of</strong> D. braunii, unlike D. toxicarium, so not contain any w-fluorinated<br />

fatty acids.<br />

O'Hagan, D. and Harper, D. B. (1999). Fluorine-containing natural products. Journal <strong>of</strong> fluorine chemistry<br />

100, 127-133.<br />

Keywords: metabolism/occurrence in nature<br />

Abstract: It is now more than 50 years since the first fluorinated natural product was identified. In that time<br />

only about a dozen fluorinated natural products have been isolated, the last one over a decade ago. Very<br />

little is known about the mechanism <strong>of</strong> biological fluorination although significant progress has been made<br />

in elucidating the pathway by which biosynthesis <strong>of</strong> fluoroacetate and 4-fluorothreonine occurs in the<br />

bacterium Streptomyces cattleya. In this article we review the fluorinated natural products and the current<br />

status <strong>of</strong> our understanding <strong>of</strong> fluorometabolite biosynthesis.<br />

O'Hagan, D., Goss, R. J. M., Meddour, A., and Cortieu, J. (2003). Assay for the enantiomeric analysis <strong>of</strong> [H-<br />

2(1)]-fluoroacetic acid: Insight into the stereochemical course <strong>of</strong> fluorination during fluorometabolite<br />

biosynthesis in Streptomyces cattleya . Journal <strong>of</strong> the American Chemical Society 125, 379-387.<br />

Keywords: analysis/biosynthesis/fluoroacetate/bacteria/enzyme/fluoride<br />

Abstract: A sensitive method for the configurational analysis <strong>of</strong> (R)- and (S)-[H-2(1)]-fluoroacetate has been<br />

developed using H-2{H-1}-NMR in a chiral liquid crystalline solvent. This has enabled biosynthetic<br />

experiments to be conducted which reveal stereochemical details on biological fluorination occurring during<br />

the biosynthesis <strong>of</strong> fluoroacetate and 4-fluorothreonine in the bacterium Streptomyces cattleya. In particular,<br />

feeding experiments to S. cattleya with isotopically labeled (1R, 2R)- and (1S, 2R)-[1-H-2(1)]-glycerol 3d and 3e<br />

and [2,3-H-2(4)]-Succinate 4a gave rise to samples <strong>of</strong> enantiomerically enriched [2-H-2(1)]-fluoroacetates 1a.<br />

The predominant enantiomer resulting from each experiment suggests that the stereochemical course <strong>of</strong><br />

biological fluorination takes place with an overall retention <strong>of</strong> configuration between a glycolytic intermediate<br />

and fluoroacetate 1. Consequently, this outcome suggests that the stereochemical course <strong>of</strong> the recently<br />

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identified fluorinase enzyme which mediates a reaction between fluoride ion and S-adenosyl-L-methionine<br />

(SAM), occurs with an inversion <strong>of</strong> configuration.<br />

O'Halloran, K., Jones, D., and Fisher, P. Project number: R-10581. Ecotoxicity <strong>of</strong> 1080 to Soil<br />

Microorganisms and Plants. <strong>Landcare</strong> <strong>Research</strong> Contract Report: LC00304/057, -23. 2003. <strong>Landcare</strong><br />

<strong>Research</strong>, Lincoln.<br />

Ref Type: Report<br />

Keywords: 1080/soil/inhibition/urine/possums/lethal dose<br />

Abstract: The lowest-observed-effect concentration (LOEC) <strong>of</strong> 1080 on lettuce seedlings was 7<br />

mg/kg dry weight soil, at which the time to emergence significantly increased. A significant decrease in<br />

seedling shoot growth also occurred. A median effective concentration (EC50) value <strong>of</strong> 10 mg 1080/kg dry<br />

weight soil was derived for lettuce shoot growth. Lettuce seedlings appeared to be relatively more sensitive<br />

to 1080 soil concentrations than oat seedlings, for which LOEC and EC50 values were 22 and 42 mg/kg dry<br />

soil weight, respectively.<br />

No 1080-related inhibition <strong>of</strong> soil nitrate production was found.<br />

The addition <strong>of</strong> possum urine to soils enhanced basal nitrate production, probably by supplying<br />

soil microbes with an easily convertible source <strong>of</strong> nitrogen (N) as nitrate (NH). The urine from possums<br />

that had received a lethal dose <strong>of</strong> 1080 caused a 15% reduction in substrate-induced nitrate production<br />

compared with that in soils spiked with control urine. However, in terms <strong>of</strong> ecotoxicological hazard, this<br />

reduction was considered neither statistically nor biologically significant.<br />

O'Halloran, K., Jones, D., and Booth, L. H. Project number: R-10608, Reproductive Ecotoxicity <strong>of</strong> 1080 to<br />

Earthworms. LCR0304/046, -17. 2003. <strong>Landcare</strong> <strong>Research</strong>, Lincoln.<br />

Ref Type: Report<br />

Keywords: 1080/soil/residues/invertebrates/toxicity<br />

Abstract: •• No mortality or growth changes were observed in earthworms after a 28-day exposure to<br />

any <strong>of</strong> the soil concentrations <strong>of</strong> 1080 tested.<br />

• The NOEC, LOEC and EC50 for Eisenia fetida exposed to 1080 in a chronic test were 50, 100 and<br />

160 mg/kg, respectively, for juvenile production, and 50, 100 and 90 mg/kg, respectively, for cocoon<br />

production.<br />

• Residues <strong>of</strong> 1080 in soil were reduced after 28 days to


1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) is a toxin used throughout New Zealand for the control <strong>of</strong><br />

possums Trichosurus vulpecula. Its rate <strong>of</strong> degradation was measured in stream water in aquaria in the<br />

presence and absence <strong>of</strong> the endemic aquatic plant Myriophyllum triphyllum together has a significant<br />

effect on 1080 degradation rate, with concentrations decreasing below detectable levels in 1 day at 23°C<br />

and 3 days at 7°C. M.triphyllum is therefore capable <strong>of</strong> playing a significant role in 1080 degradation,<br />

bu1080 introduced into the environment at colder times <strong>of</strong> the year is likely to take longer to degrade than<br />

if introduced in warmer temperatures.<br />

Ogilvie, S. C., Hetzel, F., and Eason, C. T. (1996). Effect <strong>of</strong> temperature on the biodegradation <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) in water and in Elodea canadensis. Bulletin <strong>of</strong> environmental contamination and<br />

toxicology 56, 942-947.<br />

Keywords: persistence in water/1080/sodium fluoroacetate/temperature/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/degradation/fluoroacetate<br />

Abstract: The influence <strong>of</strong> temperatures <strong>of</strong> 21 and 11øC on the biodegradation <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate [sodium fluoroacetate] in water and in Elodea canadensis was studied in the laboratory,<br />

using stream water and plant material collected from the field in New Zealand. Concn <strong>of</strong> the rodenticide<br />

remained relatively constant in deionised water at both temperatures but decreased with time in stream<br />

water. Degradation was more rapid in the stream water at 21 than at 11øC. Elodea canadensis was<br />

considered to play a mediating role in the degradation <strong>of</strong> sodium fluoroacetate.<br />

Ogilvie, S. C., Thomas, M. D., Fitzgerald, H., and Morgan, D. R. Sodium mon<strong>of</strong>luoroacetate (1080) baitshyness<br />

in a wild brushtail possum (Trichosurus vulpecula) population. 143-146. 1996. Proceedings <strong>of</strong><br />

49th NZ Plant Protection Conference.<br />

Ref Type: Conference Proceeding<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/bait shyness/possums/carrot/poisoning/field<br />

efficacy<br />

Abstract: Bait-shyness was investigated in wild possums by comparing the consumption <strong>of</strong> diced carrot<br />

with the consumption <strong>of</strong> non-toxic cereal bait before and after the population had been poisoned with the<br />

same cereal bait containing 0.04% sodium mon<strong>of</strong>luoroacetate (1080). Before poisoning, 64% <strong>of</strong> the total<br />

bait consumed was cereal, whereas after the poisoning cereal bait consumption declined to 3-4%. To<br />

determine whether any individual component <strong>of</strong> the cereal bait cues possum aviodance, the consumption <strong>of</strong><br />

plain cereal bait, cereal bait with green dye and cereal bait with cinnamon lure were also measured.<br />

Possums remained shy <strong>of</strong> the cereal bait even when the dye and lure were absent. Ways to overcome bait<br />

shyness are discussed in light <strong>of</strong> these new findings.<br />

Ogilvie, S. C., Booth, L. H., and Eason, C. T. (1998). Uptake and persistence <strong>of</strong> sodium mon<strong>of</strong>luoroacetate<br />

(1080) in plants. Bulletin <strong>of</strong> environmental contamination and toxicology 60, 745-749.<br />

Keywords: persistence in plants/1080/rabbits/secondary poisoning<br />

Abstract: In New Zealand, large-scale control <strong>of</strong> introduced possums (Trichosurus vulpecula) and rabbits<br />

(Oryctolagus cuniculus) is based on aerial application <strong>of</strong> baits containing the toxin sodium<br />

mon<strong>of</strong>luoroacetate (1080). The high solubility <strong>of</strong> 1080 has caused concerns about the environment effects<br />

<strong>of</strong> 1080 leaching from baits to soil and waterways (Livingstone 1994).<br />

Sodium mon<strong>of</strong>luoroacetate which has leached into soil may be absorbed by plants (Atzert 1971; Rammel<br />

and Fleming 1978). Cabbage (Brassica oleracea capitata) has been shown to systemically accumulate<br />

1080 through its roots, and subsequently become toxic to aphids (Negherborn 1959). Herbivores may be at<br />

risk <strong>of</strong> secondary poisoning if they consume plants which have taken up 1080 that has leached from bait.<br />

Depending on the period <strong>of</strong> time 1080 persists within plant tissues, plants could remain toxic to herbivores<br />

after the risk <strong>of</strong> primary poisoning had gone, i.e., after baits had degraded and become non-toxic.<br />

We have investigated the potential risks <strong>of</strong> 1080 poisoning to herbivorous species by determining the<br />

uptake and persistence <strong>of</strong> 1080 in two plant species, the native New Zealand broadleaf (Griselinia<br />

littoralis), a dicotyledon, and perennial ryegrass (Lolium perenne), a monocotyledon.<br />

Ogilvie, S. C., Thomas, M. D., Morriss, G. A., Morgan, D. R., and Eason, C. T. (2000). Investigation <strong>of</strong><br />

sodium mon<strong>of</strong>luoroacetate (1080) bait shyness in wild brushtail possum (Trichosurus vulpecula)<br />

populations. International journal <strong>of</strong> pest management 46, 77-80.<br />

Keywords: field efficacy/1080/bait shyness/mon<strong>of</strong>luoroacetate/poisoning<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Bait shyness is a significant threat to the sustainable control <strong>of</strong> vertebrate pests. New Zealand's<br />

foremost vertebrate pest is the introduced brushtail possum (Trichosurus vulpecula). Bait shyness was<br />

identified in two wild possum populations by comparing the consumption <strong>of</strong> two non-toxic bait types<br />

before and after each population was presented with one <strong>of</strong> the bait types containing the toxin sodium<br />

mon<strong>of</strong>luoroacetate (1080). Before poisoning, approximately 60% <strong>of</strong> total bait consumption was <strong>of</strong> the type<br />

which 1080 was later presented in, whereas after poisoning this bait type made up only 2-4% <strong>of</strong> total<br />

consumption. This shyness persisted for at least 11 weeks in one <strong>of</strong> the populations. No individual<br />

component (bait base, cinnamon lure or green dye) <strong>of</strong> the toxic bait could be isolated as the primary cue<br />

eliciting bait shyness as the response. Possible means <strong>of</strong> overcoming bait shyness are discussed in light <strong>of</strong><br />

these findings.<br />

Ogilvie, S. C., Ataria, J. M., Waiwai, J., Doherty, J., Lambert, N., and Lambert, M. Uptake and persistence<br />

<strong>of</strong> 1080 in plants <strong>of</strong> cultural importance. Lincoln University Contract Report ?, -16. 2004.<br />

Ref Type: Report<br />

Keywords: 1080/baits/humans/aerial control/poisoning/pest/Tb/persistence in plants<br />

Abstract: (Conclusions) 1080 can move out <strong>of</strong> Wanganui No. 7 baits when the baits are applied in the field.<br />

There is no evidence that either pikopiko or karamuramu contain endogenous 1080. There was no evidence<br />

<strong>of</strong> pikopiko plants taking up 1080 that has elached out <strong>of</strong> baits. Karamuramu plants will take up 1080,<br />

however based on this experiment only a very small proportion (0.0004%) <strong>of</strong> the original 1080 present in<br />

baits is likely to be seen in the leaves and the shoots. The highest 1080 concentration measured in the<br />

karamuramu was 5 ppb, in leaf material 7 days after bait placement. 1080 did not persist, plants containing<br />

1080 reduced levels to zero after 25 days. At the highest measured concentration <strong>of</strong> 5 ppb, a person would<br />

need to consume 28 tonnes <strong>of</strong> this material to receive an LD50. There is negligible risk <strong>of</strong> humans being<br />

poisoned by consuming plants that have taken up 1080 from baits during an aerial control operation.<br />

(Recommendations) The poisoning <strong>of</strong> humans by consuming pikopiko or karamuramu plants after aerial<br />

application <strong>of</strong> 1080 should not be considered as a significant risk. Consideration should be made for Maori<br />

groups to adopt a withholding period <strong>of</strong> 30 days after the aerial application <strong>of</strong> 1080, during which plants<br />

from within the 1080 application area are not used for rongoa (medicinal) purposes. Support should be<br />

given to further collaborative research projects involving Maori groups, as this allows these groups to play<br />

an informed role in considering the acceptability <strong>of</strong> 1080 as a vertebrate pest control technique, thus<br />

potentially strengthening efforts to reduce Tb vector numbers.<br />

Okuno, I, Connolly, G. E., Savarie, P. J., and Breidenstein, C. P. (1984). Gas chromatographic analysis <strong>of</strong><br />

coyote and magpie tissues for residues <strong>of</strong> compound 1080 (sodium fluoroacetate). Journal <strong>of</strong> the<br />

Association <strong>of</strong> Official Analytical Chemists 67, 549-553.<br />

Keywords: persistence in animals/birds/mammals/analysis/1080/sodium<br />

fluoroacetate/fluoroacetate/muscle/heart/kidney/liver/gut/temperature<br />

Oliver, A. J., King, D. R., and Mead, R. J. (1977). The evolution <strong>of</strong> resistance to fluoroacetate intoxication<br />

in mammals. Search 8, 130-132.<br />

Keywords: fluoroacetate/mammals/tolerance/occurrence in nature/marsupials<br />

Oliver, A. J., King, D. R., and Mead, R. J. (1979). Fluoroacetate tolerance, a genetic marker in some<br />

Australian mammals. Aust.J.Zool. 27, 363-372.<br />

Keywords: fluoroacetate/tolerance/mammals/marsupials<br />

Abstract: The toxin fluoroacetate occurs naturally in many south-western Australia species <strong>of</strong> the legume<br />

genera Gastrolobium and Oxylobium. No fluoroacetate-bearing species are known from south-eastern<br />

Australia. Herbivores have evolved a high level <strong>of</strong> genetic tolerance to this toxin; this has persisted in some<br />

mammalian herbivores whose range now extends beyond the range <strong>of</strong> the toxic plants. Other species <strong>of</strong><br />

mammals have acquired tolerance since extending their range into south-western Australia. This tolerance<br />

can be used as a genetic marker to identify the geographic origin and trace the subsequent spread <strong>of</strong><br />

herbivorous mammals in southern Australia. In this paper, this marker has been used to clarify the recent<br />

evolutionary history <strong>of</strong> the western grey kangaroo, the tammer wallaby and the bush rat.<br />

Oliver, A. J., Wheeler, S. H., and Gooding, C. D. (1982). Field evaluation <strong>of</strong> 1080 and pindone oat bait, and<br />

the possible decline <strong>of</strong> effectiveness <strong>of</strong> poison baiting for the control <strong>of</strong> the rabbit, Oryctolagus cuniculus.<br />

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Australian wildlife research 9, 125-134.<br />

Keywords: field efficacy/target species/bait degradation/1080/pindone/rabbits<br />

Oliver, A. J. and King, D. R. (1983). The influence <strong>of</strong> ambient temperatures on the susceptibility <strong>of</strong> mice,<br />

guinea pigs and possums to compound 1080. Australian wildlife research 10, 297-301.<br />

Keywords: acute toxicity/mammals/possums/1080/non-target species/lethal dose<br />

Abstract: The susceptibilities <strong>of</strong> mice Mus musculus, guinea-pigs Cavia porcellus and brushtail possums<br />

Trichosurus vulpecula to sodium mon<strong>of</strong>luoroacetate (compound 1080) were determined at various ambient<br />

temperatures in the range 4-33EC. Toxicity was greater at both ends <strong>of</strong> the range than in the middle. In<br />

mice the LD50 at 24EC was five times that at 12.2EC, in guinea-pigs the LD50 at 17EC was twice that at<br />

4EC, in possums the LD50 at 23.5EC was two and a half times that at 10.5EC. It is important to consider<br />

these differences when assessing the efficacy <strong>of</strong> 1080 for pest control, and potential hazards to non-target<br />

species in situations where such temperature ranges may be commonly expected.<br />

Omara.F. and Sisodia, C. S. (1990). Evaluation <strong>of</strong> potential antidotes for sodium fluoroacetate in mice.<br />

Veterinary and human toxicology 32, 427-431.<br />

Keywords: treatment/sodium fluoroacetate/lethal dose<br />

Abstract: Pathogenesis in fluoroacetate poisoning is multifactorial. Biochemically it is characterized by<br />

lethal synthesis <strong>of</strong> fluorocitrate, causing hypocalcemia, and energy deficiency through blockade <strong>of</strong> the TCA<br />

cycle. Calcium gluconate (CaG) was chosen to antagonize hypocalcemia, while sodium alpha kelogluterate<br />

(NaKG) and sodium succinate (NaSuc) were selected as potential antidotes to revive the TCA cycle.<br />

Effectiveness <strong>of</strong> each <strong>of</strong> these antidotes individually and in certain combinations was tested in mice<br />

exposed to lethal doses (15 mg/kg ip) <strong>of</strong> sodium fluoroacetate (NaFAC). Antidotal treatments were<br />

administered at 15 min, 4 h, 10 h, 24 h, and 36 h after NaFAC. All 3 <strong>of</strong> the antidotes alone, as well as a<br />

combination <strong>of</strong> CaG with NaKG, were ineffective in reducing morality in mice after NaFAC. On the other<br />

hand, a combination <strong>of</strong> CaG (130 mg/kg) with NaSuc (240 mg/kg) was effective if the 2 solutions were<br />

either injected at separate sites or mixed in the same syringe just prior to injections. Similar solutions, if<br />

mixed for 24 h or longer before administrations, were ineffective. Increasing the dose <strong>of</strong> NaSuc to 360 or<br />

480 mg/kg with CaG (130 mg/kg) was unrewarding. These results indicate that CaG in combination with<br />

240 mg NaSuc/kg <strong>of</strong>fer a promising therapy modality in NaFAC intoxication. Additional studies involving<br />

biochemical parameters and other species are needed to confirm the efficacy and mechanism(s) <strong>of</strong> action <strong>of</strong><br />

this combination.<br />

Orr, M. and Bentley, G. (1994). Accidental 1080 poisonings in livestock and companion animals.<br />

Surveillance 21(1), 27-28.<br />

Keywords: non-target species/mammals/1080/poisoning/livestock/witholding period/target<br />

species/carrot/welfare<br />

Abstract: It appears that compound 1080 is relatively humane and efficient and its use by approved<br />

operators ensures that it is relatively target species specific. The operators usually advise that livestock and<br />

pet animals should be withheld from the poisoned areas for at least 8 weeks and preferably until at least 10<br />

cm <strong>of</strong> rain has fallen. In low rainfall areas, it may be appropriate to extend the withholding time until<br />

laboratory testing <strong>of</strong> weathered bait indicates that it is safe to restock. Extra precautions should be taken<br />

before livestock are allowed to graze airstrips from which 1080 carrot has been flown.<br />

Owen, N. E., Chaure, P. T., and Connerton, I. F. (1992). Isolation and characterization <strong>of</strong> new fluoroacetate<br />

resistant/acetate non-utilizing mutants <strong>of</strong> Neurospora crassa. Journal <strong>of</strong> general microbiology 138, 2599-<br />

2608.<br />

Keywords: fluoroacetate/fungus/resistance/acetate/analysis/enzyme<br />

Abstract: Sixty-two mutants <strong>of</strong> the filamentous fungus Neurospora crassa were isolated on the basis <strong>of</strong><br />

resistance to the antimetabolite fluoroacetate. Of these, 14 were unable to use acetate as sole carbon source<br />

(acetate non-utilizers, acu) and were the subject <strong>of</strong> further genetic and biochemical analysis. These mutants<br />

fell into four complementation groups, three <strong>of</strong> which did not complement any known acu mutants.<br />

Mutants <strong>of</strong> complementation group 3 failed to complement acu-8, demonstrated similar phenotypic<br />

properties and provided to be closely linked (less than 2% recombination) but not allelic. Representatives <strong>of</strong><br />

groups 2 and 4 were mapped to independent loci; the single representative <strong>of</strong> group 1 could not be mapped.<br />

The four complementation groups were therefore designated as genes acu-10 to acu-13, respectively. All<br />

152


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Appendix C<br />

the mutants demonstrated normal acetate-induced expression <strong>of</strong> acetyl-CoA synthetase and the unique<br />

enzymes <strong>of</strong> the glyoxylate cycle and gluconeogenesis. The nature <strong>of</strong> these mutations is therefore quite<br />

different to those reported for other fungal species. Mutant acu-11 was unable to fix labelled acetate,<br />

indicating the loss <strong>of</strong> an initial transport function; partial enzyme lesions were observed for acu-12 (acetyl-<br />

CoA hydrolase) and acu-13 (acetate-inducible NAD+-specific malate dehydrogenase)<br />

Ozawa, H. and Tsukioka, T. (1987). Gas chromatographic determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate in<br />

water by derivatization with dicyclohexylcarbodiimide. Analytical Chemistry 59 , 2914-2917.<br />

Keywords: persistence in water<br />

Abstract: A method is described for the determination <strong>of</strong> trace amounts <strong>of</strong> sodium mon<strong>of</strong>luoroacetate<br />

(MFA-Na) in water. MFA-Na was converted to the dichloroanilide derivative in a water sample acidfled<br />

with hydrochloric acid by using N,N' -dl- cyclohexylcarbodiimide (DCC) and 2,4-dichloroanilide (DCA)<br />

and the derivative was extracted from the sample water and cleaned up by the silica gel column<br />

chromatography. The derivative was quantified by gas chromatography with electron capture detection<br />

(GC-ECD). The limit <strong>of</strong> detection was 0.0006 ug/mL, with a 50-mL water sample. The recoveries from<br />

environmental waters spiked at concentrations <strong>of</strong> 0.005-0.01 ug/mL were 93-97% with less than 4%<br />

relative standard deviation.<br />

Ozawa, H. and Tsukioka, T. (1989). Determination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate in soil and biological<br />

samples as the dichloroanilide derivative. Journal <strong>of</strong> chromatography 473, 251-259.<br />

Keywords: persistence in soil/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/soil<br />

Abstract: A method is described for the determination <strong>of</strong> trace amounts <strong>of</strong> sodium mon<strong>of</strong>luoroacetate<br />

(MFA-Na) in soil and biological samples. Soil samples were sonicated with distilled water in the presence<br />

<strong>of</strong> basic magnesium carbonate. Biological samples were extracted with distilled water by sonication and<br />

the extracts were coagulated by addition <strong>of</strong> equal volumes <strong>of</strong> alcohol and centrifuged. MFA-Na in each<br />

sample solution was absorbed on Dowex 1-X8 anion-exchanged resin and eluted with 2% (w/v) sodium<br />

chloride. The eluate was acidified with hydrochloric acid and treated with 2,4-dichloroaniline and N,N'dicyclohexylcarbodiimide.<br />

The dichloroanilide derivative <strong>of</strong> MFA-Na was extracted with ethyl acetate and<br />

quantified by gas chromatography with electron-capture detection and gas chromatography-mass<br />

spectrometry. The detection limits were 0.0015 and 0.003 ug/g in 20 g <strong>of</strong> soil and 10 g <strong>of</strong> biological<br />

sample, respectively.<br />

Palmer-Jones, T. (1958). Laboratory methods for measuring the toxicity <strong>of</strong> pesticides to honey bees. New<br />

Zealand journal <strong>of</strong> agricultural research 1, 290-300.<br />

Keywords: honey/invertebrates/lethal dose/stomach/<strong>poisons</strong>/1080<br />

Abstract: A description is given <strong>of</strong> laboratory tests designed to study the effect upon honey bees <strong>of</strong><br />

pesticides acting as stomach and dry contact <strong>poisons</strong>. Methods are also given for measuring direct spray<br />

and fumigant action. Compound 1080 is highly toxic to bees as a stomach poison.<br />

Parfitt, R. L., Eason, C. T., Morgan, A. J., Wright, G. R., and Burke, C. M. (1994). The fate <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) in soil and water. In 'Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14<br />

December 1993, Christchurch, New Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 59-66. (<strong>Royal</strong><br />

Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: persistence in soil/persistence in water/1080<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) was added to streamwater at a rate <strong>of</strong> 0.1 mg 1-1 in an<br />

aquarium, and 3-8 mg (representing typical baits) was added to small cores <strong>of</strong> soil in the laboratory, and the<br />

concentration <strong>of</strong> 1080 in solution measured with time. For the streamwater at 21EC, biodegradation was<br />

complete within 2-6 days; in the soils biodegradation took longer, and increased with temperature and<br />

moisture content. In laboratory experiments 1080 was found to be leached through soils bu at three field<br />

sites no 1080 was detected in groundwater after aerial application <strong>of</strong> baits. Surface waters as well as<br />

groundwaters were monitored after four possum-control operations and one rabbit-control operation<br />

between 1990 and 1993. No 1080 was detected in the water after three <strong>of</strong> the possum-control operations.<br />

Extremely small, but variable, traces (


1080 Reassessment Application October 2006<br />

Appendix C<br />

both taken with 24 hours <strong>of</strong> the application, probably as a result <strong>of</strong> baits falling into streams. The amount<br />

<strong>of</strong> 1080 used per has is extremely low (less than 15 g) and if any 1080 is not degraded because <strong>of</strong> low<br />

biological activity (e.g., at low temperature) it will be diluted by soil water and streamwater to very low<br />

concentrations.<br />

Parfitt, R. L., Eason, C. T., H<strong>of</strong>f, H., and Heng, L. K. (1995). Sodium mon<strong>of</strong>luoroacetate (1080) leaching<br />

through soils. Bulletin <strong>of</strong> environmental contamination and toxicology 55, 162-169.<br />

Keywords: persistence in soil/1080/non-target species<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (Compound 1080) is used in New Zealand for the control <strong>of</strong> animals<br />

such as rabbit and the brush-tail possum. Since more than one tonne <strong>of</strong> this pesticide is applied annually in<br />

New Zealand a clear understanding <strong>of</strong> possible risks to the environment is essential. <strong>Research</strong> has been<br />

conducted on the toxicity <strong>of</strong> 1080 to a number <strong>of</strong> target and non-target species (Atzert 1971; Rammel and<br />

Flemming 1978; Eason et al. 1993). Work on biodegradation <strong>of</strong> 1080 has shown that it is defluorinated<br />

both by organisms which have been isolated from soil (Walker and Bong 1981; Wong et al. 1991) and<br />

within soils themselves (David and Gardiner 1966; Parfitt et al. 1994). In Australia where fluoroacetate<br />

occurs naturally in 41 plant species from two genera <strong>of</strong> Leguminosae at concentrations <strong>of</strong> from


1080 Reassessment Application October 2006<br />

Appendix C<br />

Parkin, P. J., McGiven, A. R., and Bailey, R. R. (1977). Chronic sodium mon<strong>of</strong>luoroacetate (compound<br />

1080) intoxication in a rabbiter. New Zealand medical journal 85, 93-96.<br />

Keywords: diagnosis/treatment/pathology/1080/humans/kidney<br />

Abstract: A rabbiter who was repeatedly exposed to sodium mon<strong>of</strong>luoroacetate (compound 1080)<br />

developed renal failure and evidence <strong>of</strong> other organ damage. This is believed to be the first report <strong>of</strong><br />

chronic sodium mon<strong>of</strong>luoroacetate intoxication occurring in man.<br />

Parton, K., Bruere, A. N., and Chambers, J. P. (2001). Veterinary Clinical Toxicology. (Foundation for<br />

Continuing Education <strong>of</strong> the N.Z. Veterinary Association: Massey University, Palmerston North, New<br />

Zealand.)<br />

Keywords: symptoms/poisoning/treatment/mode <strong>of</strong> action/1080<br />

Parton, K. Toxicology Update: Sodium mon<strong>of</strong>luoroacetate (1080) poisoning. Vetscript New Zealand<br />

September 2002, -1. 2002.<br />

Ref Type: Magazine Article<br />

Keywords: treatment/antidote/1080/poisoning/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/dogs/convulsions/poison<br />

Abstract: Until an effective antidote is licensed for use in domestic animals, veterinarians must use their<br />

pr<strong>of</strong>essional judgement and skills in the treatment <strong>of</strong> animals poisoned by 1080. IN the past, glycerol<br />

monoacetate (GMA) was used to treat people and animals but GMA had a short shelf life and is no longer<br />

available. Alternatively, acetamide treatment appears to be effective in the treatment <strong>of</strong> dogs as reported by<br />

john McLaren in Vetscript March 1999. Because many practices do not have a ready supply <strong>of</strong> acetamide<br />

available for poisonings, symptomatic treatment <strong>of</strong> convulsions and metabolic acidosis arising from 1080<br />

ingestion may require anaesthesia and fluids containing sodium bicarbonate. Of importance in all cases <strong>of</strong><br />

poisoning, the use <strong>of</strong> decontamination to prevent absorption and eliminate the poison is <strong>of</strong>ten the key to<br />

success. An emetic may be indicated before clinical signs appear to reduce the amount <strong>of</strong> poison available<br />

for absorption. The use <strong>of</strong> activated charcoal with sorbitol binds to, and aids, the elimination <strong>of</strong> 1080 in the<br />

intestinal tract.<br />

Patel, A. and Koenig, H. (1968). The neurochemical effects <strong>of</strong> fluorocitrate. Neurology 18, 296.<br />

Keywords: fluorocitrate/Krebs cycle/symptoms/brain<br />

Abstract: Fluorocitrate (FC) an inhibitor <strong>of</strong> the Krebs cycle that acts by blocking aconitase, the enzyme<br />

which catalyzes the conversion <strong>of</strong> citrate to isocitrate, exerts potent neurobiological effects. Injected<br />

intracerebrally in rat, FC (5 - 10 ug) causes lethargy followed by convulsive seizures and death. When<br />

injected intrathetcally in cat, FC (10 - 30 ug) produces a spinal status epilepticus featuring clonic-tonic<br />

seizures <strong>of</strong> hindlimbs and trunk after a latent period <strong>of</strong> 1-2 hour.<br />

Patel, A. and Koenig, H. (1971). Some neurochemical aspects <strong>of</strong> fluorocitrate intoxication. Journal <strong>of</strong><br />

neurochemistry 18, 621-628.<br />

Keywords: metabolism/cats/fluorocitrate<br />

Paulsen, R. E., Contestabile, A., Villani, L., and Fonnum, F. (1988). The effect <strong>of</strong> fluorocitrate on<br />

transmitter amino acid release from rat striatal slices. Neurochemical research 13, 637-641.<br />

Keywords: fluorocitrate/treatment/brain/metabolism/inhibition<br />

Abstract: In order to study the role <strong>of</strong> glutamine from glial cells for the synthesis <strong>of</strong> transmitter amino<br />

acids, the effect <strong>of</strong> the gliotoxic substance fluorocitrate on amino acid release from slices was investigated.<br />

In vivo treatment with 1 nmol fluorocitrate reduced the Ca 2+ dependent K + evoked release <strong>of</strong> endogenous<br />

glutamate and GABA from the slices, whereas the glutamine efflux decreased and alanine efflux increased.<br />

The K + evoked release <strong>of</strong> [ 3 H]D-aspartate increased during fluorocitrate treatment. The latter is consistent<br />

with an inhibited uptake <strong>of</strong> D-aspartate into glial cells. Incubation <strong>of</strong> striatal slices with fluorocitrate (0.1<br />

mM) decreased the glutamine efflux and increased the alanine efflux. Similar to the in vivo condition,<br />

fluorocitrate increased the K + evoked [ 3 H]D-aspartate release, but the K + evoked release <strong>of</strong> endogenous<br />

glutamate and GABA increased rather than decreased. The ratio between the K + evoked release <strong>of</strong><br />

exogenous D-aspartate to endogenous glutamate increased in both cases. The results suggest an important<br />

role <strong>of</strong> glial cells in the synthesis and inactivation <strong>of</strong> transmitter amino acids.<br />

155


1080 Reassessment Application October 2006<br />

Appendix C<br />

Payne, W. J., Wiebe, W. J., and Christian, R. R (1970). Assays for biodegradability essential to unrestricted<br />

usage <strong>of</strong> organic compounds. BioScience 20, 862-865.<br />

Keywords: enzyme/soil/resistance/analysis<br />

Abstract: Most organic compounds are degraded in nature either by chemical interactions or by the<br />

enzymes <strong>of</strong> microoganisms distributed widely in soils and waters; but some are not. Alexander (1965) has<br />

used the term "recalcitrant" to characterize the compounds that can resist inactivation and biodegradation,<br />

and accumulate in nature as a consequence. Within the past decade, certain <strong>of</strong> the components <strong>of</strong><br />

commercial detergents were found to be recalcitrant in this sense and were replaced by the manufacturers in<br />

the formulation <strong>of</strong> products sold in the United States. Synthetic surfactants largely susceptible to microbial<br />

attack are now used, and this problem has been eased without diminishing the quality <strong>of</strong> the product.<br />

Today, organic herbicides and insecticides are the most troublesome <strong>of</strong> the persistent organic compounds<br />

routinely broadcast in nature.<br />

It is tempting to speak <strong>of</strong> these lingering substances as unqualified nuisances, but attitudes toward<br />

pesticides must necessarily be ambivalent. It is certain, for example, that employment <strong>of</strong> DDT and other<br />

pesticides has resulted in more effective disease control and greatly increased agricultural productivity.<br />

The resistance <strong>of</strong> these compounds to biodegradation and their adverse effects on the environment have<br />

typically come to light only after some years <strong>of</strong> just such extensive and effective use. The unintentional,<br />

and originally unexpected, persistence <strong>of</strong> many <strong>of</strong> these agents and their progressive concentration in<br />

organisms in successive trophic levels must now be cause for growing alarm. Once perceived, hazards as<br />

clear as these should be regarded as danger signals that place us on guard against future <strong>of</strong>fenses.<br />

Pekelharing, C. J. (1979). Fluctuation in opossum populations along the north bank <strong>of</strong> the Taramakau<br />

catchment, New Zealand, and its effect on the forest canopy. New Zealand journal <strong>of</strong> forestry science 9,<br />

212-224.<br />

Keywords: 1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/carrot/aerial control/possums<br />

Abstract: Fluctuations in density patterns <strong>of</strong> opossum populations were studied by fecal pellet counts, along<br />

the North Bank <strong>of</strong> the Taramakau catchment from 1970-1977. The study area contained 2 major vegetation<br />

associations, rata(Podocarpus hallii)/kamahi forest and red beech (Noth<strong>of</strong>agus fusca) forest. Variations in<br />

density patterns over the years indicated that peak population numbers in the beech forests were<br />

approximately half those in the rata/kamahi forests. The upper transitional forests above both major forest<br />

types reached similar peak densities. Canopy defoliation was studied by aerial photography in 1960 and in<br />

1973. Within 13 yr over 40% <strong>of</strong> the canopy in these protection forests was defoliated. This large-scale<br />

defoliation coincided with a build-up and peaking <strong>of</strong> the opossum population. In the winter <strong>of</strong> 1974 the<br />

whole area was poisoned by air with 1080 (sodium mon<strong>of</strong>luoroacetate) impregnated carrot. Approximately<br />

85% <strong>of</strong> the opossum population was removed by this operation. The greatest decline in pellet densities was<br />

recorded in the lower and mid-forest strata<br />

Pekelharing, C. J. and Batcheler, C. L. (1990). The effect <strong>of</strong> control <strong>of</strong> brushtail possums (Trichosurus<br />

vulpecula) on condition <strong>of</strong> a southern rata/kamahi (Metorsideros umbellata / Weinmannia racemosa) forest<br />

canopy in Westland, New Zealand. New Zealand journal <strong>of</strong> ecology 13, 73-82.<br />

Keywords: possums/poisoning/field efficacy/aerial control<br />

Abstract: Brushtail possums began colonising a rata/kamahi forest in the Taramakau catchment, Westland<br />

about 1950 and by 1973 had caused widespread conspicuous forest canopy defoliation. They were<br />

poisoning in one block <strong>of</strong> this forest in 1970, at about the time they reached peak denisyt, and again in<br />

1974. In an adjacent block they were poisoning in 1974 only. A survey <strong>of</strong> forest canopy condition in 1985<br />

showed that, in the block poisoned at peak density, 21% <strong>of</strong> the basal area <strong>of</strong> palatable trees had died,<br />

compared with 47% in the block where poisoning was deferred for 4 years. This suggested that control at or<br />

before populations attain peak denisty is critically important for limiting canopy mortality. After the 1974<br />

poisoning, possum numbers in both blocks recoverd to within 20% <strong>of</strong> their pre-control levels in 10 years,<br />

indicating that control should be carried out at about decade intervals. Defoliation indices and species<br />

condition patterns showed that canopy dieback was least evident on relatively unpalatable trees. Of the<br />

palatable trees, kamahi was in best overall condition with least canopy dieback, followed by cedar, southern<br />

rata and Hall's totara.<br />

156


1080 Reassessment Application October 2006<br />

Appendix C<br />

Pelfrene, A. F. (1991). Synthetic organic rodenticides : 19.2 Fluoroacetic acid and its derivatives. In<br />

'Handbook <strong>of</strong> pesticide toxicology. Volume 3. Classes <strong>of</strong> pesticides'. (W. J. Hayes and E. R. LawsEds. ) pp.<br />

1272-1283. (Academic Press: San Diego.)<br />

Keywords: acute toxicity/mode <strong>of</strong> action/treatment/pathology/metabolism<br />

Perez, G. O. and Frindt, G. (1976). The effect <strong>of</strong> fluorocitrate on urinary calcium and citrate excretion.<br />

Experientia 33, 741-742.<br />

Keywords: fluorocitrate/citrate/metabolism/dogs/biochemistry/excretion/persistence in animals<br />

Abstract: The renal handling <strong>of</strong> calcium and citrate was studied in dogs after the administration <strong>of</strong><br />

fluorocitrate. The drug produced a significant increase in urinary calcium and citrate excretion. Net renal<br />

secretion <strong>of</strong> citrate occurred during the infusion <strong>of</strong> fluorocitrate since citrate clearances exceeded the<br />

glomerular filtration rate.<br />

Perfect, J. Aspects <strong>of</strong> the ecology <strong>of</strong> the native frogs Leiopelma archeyi and l. hochstetteri, and the impacts<br />

<strong>of</strong> compound 1080. 1996. Victoria University <strong>of</strong> Wellington.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: 1080/non-target species/amphibian<br />

Peters, J. A. Some Toxicological Aspects <strong>of</strong> Protection Forestry: A Treatise. 93, 1-58. 1970. Rangiora,<br />

Forest <strong>Research</strong> Institute.<br />

Ref Type: Report<br />

Keywords: 1080/systemic toxicity<br />

Peters, J. A. Chemical control <strong>of</strong> vertebrate pests. Report on overseas tour <strong>of</strong> study. 117, 1-32. 1973.<br />

Rangiora, Forest <strong>Research</strong> Insitute, New Zealand Forest Service.<br />

Ref Type: Report<br />

Abstract: On the basis <strong>of</strong> an overseas tour <strong>of</strong> study an insight is conveyed into the complexity <strong>of</strong> regulating<br />

vertebrate wildlife populations by lethal chemical control alone. In the United States, the pendulum <strong>of</strong><br />

public opinion has swung away entirely from this type <strong>of</strong> control. This has led to a drastic revision <strong>of</strong><br />

research-into-control priorities. The use <strong>of</strong> acutely lethal compounds has been severely restricted. In<br />

Europe and Japan, this situation has long been established fact.<br />

Abroad major changes are in the <strong>of</strong>fing in which the trend <strong>of</strong> research-into-control is toward integrated<br />

manipulation <strong>of</strong> pest populations by bio-chemical means. This trend takes into account the influence <strong>of</strong><br />

biological attractants and deterrents (pheromones), and the decrease <strong>of</strong> birth rates by means <strong>of</strong> reprodution<br />

inhibitors (chemosterilants).<br />

With respect to research-into-control in the New Zealand situation, fruitful contact has been made with<br />

Japan to augment Compound 1080 with other organo-fluorine derivatives. It is envisaged that these<br />

derivatives will impose secondary hazards <strong>of</strong> lesser consequence than hitherto possible.<br />

Peters, J. A. and Baxter, K. J. (1974). Analytical determination <strong>of</strong> compound 1080 (sodium fluoroacetate)<br />

residues in biological materials. Bulletin <strong>of</strong> environmental contamination and toxicology 11, 177-183.<br />

Keywords: product chemistry/ion chromatography/fluorine/analysis<br />

Abstract: A rapid and accurate method is described to determine toxic organ<strong>of</strong>luorine residues in biological<br />

materials. Sample preparation is minimal. The sample is degraded by oxygen combustion and the liberated<br />

inorganic fluorine determined by ion-specific electrode.<br />

Peters, J. A. (1974). Chemical control <strong>of</strong> vertebrate pests : a perspective. New Zealand journal <strong>of</strong> forestry<br />

19, 233-245.<br />

Keywords: persistence in animals/non-target species/legislation/cost-benefit<br />

Abstract: With growing emphasis on environmental impacts, the control <strong>of</strong> vertebrate pest populations by<br />

lethal chemicals is examined in the light <strong>of</strong> some overseas and local situations. The current philosophy<br />

embodied in legislation and policy <strong>of</strong> developed countries abroad is that a compound should be proven<br />

safe, rather than be found by use and experience not to be harmful. Such a level <strong>of</strong> scientific certainty is so<br />

unreasonable that, functionally, it may never be achieved. Such a concept <strong>of</strong> safety ignores dosage/response<br />

relationships and takes no account <strong>of</strong> the need or benefits. Given the multiple values <strong>of</strong> a situation and the<br />

ultimate problem <strong>of</strong> not having all the answers (and sometimes not even being aware <strong>of</strong> the appropriate<br />

157


1080 Reassessment Application October 2006<br />

Appendix C<br />

questions), it is not surprising that issues spill over from one problem to anaother. In such a situation the<br />

charge <strong>of</strong> bias as active prejudice must be clearly distinguished from bias inferring a certain set <strong>of</strong><br />

presuppositions. New chemicals will undergo much more intensive scrutiny than those already approved, as<br />

criteria previously ignored, not identified, or not considered significant are developed and applied. The<br />

ramifications <strong>of</strong> environmental policies and attitudes overseas are discussed particularly in relation to future<br />

developments <strong>of</strong> chemical tools in the New Zealand situation. It may be that, by the time all the options<br />

have been thoroughly assessed, some will have quietly slipped away<br />

Peters, J. A. (1975). Contamination <strong>of</strong> forest ecosystems by sodium fluoroacetate (compound 1080).<br />

Proceedings <strong>of</strong> the New Zealand Ecological Society 22, 34-41.<br />

Keywords: persistence in soil/persistence in water/sodium fluoroacetate/1080<br />

Abstract: Predictive and conceptual models are used to examine the contamination, toxicology, and<br />

residues <strong>of</strong> sodium fluoroacetate (Compound 1080) in relation to its application in vertebrate pest control<br />

programmes on forest and pastoral lands.<br />

As a pesticide, the toxin appears to be neither mobile nor persistent. Exceedingly slender opportunities<br />

exist therefore for significant contamination <strong>of</strong> susceptible components <strong>of</strong> the environment.<br />

Peters, J. A. (1977). 1080 poisoning. New Zealand medical journal 85, 295-296.<br />

Keywords: 1080/poisoning/analysis/humans<br />

Abstract: Letter to the editor in response to article by Parkin, McGiven and Bailey in 9 February 1977 issue<br />

<strong>of</strong> New Zealand Medical Journal.<br />

Peters, J. A. and Fredric, B. J. Susceptibility <strong>of</strong> the brushtail possum (Trichosurus vulpecula) to sodium<br />

fluoroacetate (Compound 1080 or SFA). 1983.<br />

Ref Type: Unpublished Work<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080/aversion/carrot/lethal dose/possums<br />

Abstract: The susceptibilities to sodium fluoroacetate <strong>of</strong> 10 regional possum populations in captivity are<br />

determined by acute and chronic dose experiments. Circadian rhythyms and desynchronisation (capture<br />

stress) have major influences on susceptibility. The relationships between susceptibility and bait acceptance<br />

are examined. Toxic anorexia (loss <strong>of</strong> appetite) induced by sub-lethal doses inhibits further bait-seeking,<br />

and smell and taste aversion diminishes bait-eating when the toxic load in bait is high. Susceptibility<br />

determined under experimental conditions in captivity is not significantly from susceptibility measured in a<br />

wild population. The varying suscpetibilities in regional populstions are considered in the light <strong>of</strong> field<br />

control operations, A general toxic load <strong>of</strong> 6 mg SFA/ carrot bait is recommended, but specific toxic loads<br />

determined for individual regional populations may <strong>of</strong>ten be more effective.<br />

Peters, J. A. Susceptibility determinations to Compound 1080 in captive wallabies. Forest <strong>Research</strong><br />

Institute Report, 5p. 1984.<br />

Ref Type: Unpublished Work<br />

Keywords: 1080/lethal dose/efficacy<br />

Peters, R A., Wakelin, R. W., Buffa, P., and Thomas, L. C. (1953). Biochemistry <strong>of</strong> fluoroacetate poisoning<br />

: the isolation and some properties <strong>of</strong> the fluorotricarboxylic acid inhibitor <strong>of</strong> citrate metabolism.<br />

Proceedings <strong>of</strong> the <strong>Royal</strong> Society <strong>of</strong> London.Series B 140, 497-507.<br />

Keywords: mode <strong>of</strong> action/acute toxicity/metabolism<br />

Abstract: It has been suggested that the toxicity <strong>of</strong> fluoroacetate is due to the enzyme synthesis <strong>of</strong> a<br />

fluorotricarboxylic acid, which 'jams' the tricarboxylic acid cycle at the citrate stage. This communication<br />

presents the pro<strong>of</strong> <strong>of</strong> this hypothesis. The inhibitory substance for citrate metabolism synthesized by<br />

enzymie action from fluoroacetate has been isolated as a compound in crystalline form <strong>of</strong> great potency.<br />

Under The conditions <strong>of</strong> test it inhibits The disappearance <strong>of</strong> approximately 300 times its weight <strong>of</strong> citric<br />

acid in 30 min. The final isolation involved a separation from citric acid by The use <strong>of</strong> ion-exchange resin.<br />

and fractional extraction with ether. It is a mon<strong>of</strong>luorotricarboxylic acid, as shown by its migration on a<br />

paper chromatogram, by its fluorine content (estimated spectrochemically), and by its titration curve. It<br />

does not give the colour reaction with sodium sulphide for penta-bromacetone produced from citric acid by<br />

The usual methods. It gives an infra-red band which may be expected from a C-F bond. By a process <strong>of</strong><br />

exclusion, it is considered to be a fluorocitric acid; a final decision must await synthesis.<br />

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Appendix C<br />

Peters, R A., Wakelin, R. W., Rivett, D. E. A., and Thomas, L. C. (1953). Fluoroacetate poisoning:<br />

comparison <strong>of</strong> synthetic fluorocitric acid with the enzymically synthesized fluorotricarboxylic acid. Nature<br />

171, 1111-1112.<br />

Keywords: fluoroacetate/poisoning/chemistry/fluorocitrate<br />

Abstract: As the spectra <strong>of</strong> the enzymically synthesized compound show no bands which cannot be<br />

accounted for by the bands seen with the synthetic fluorocitric acid together with bands expected from<br />

traces <strong>of</strong> barium salts, the compound made enzymically must be actually mon<strong>of</strong>luorocitric acid; it has<br />

approximately twice the activity <strong>of</strong> the synthetic specimen.<br />

Peters, R A., Hall, R. J., Ward, P. F., and Sheppard, N. (1960). The chemical nature <strong>of</strong> the toxic compounds<br />

containign fluorine in the seeds <strong>of</strong> Dichapetalum toxicarium. Biochemical journal 77, 17-23.<br />

Keywords: fluorine/occurrence in nature<br />

Peters, R A. (1961). Further experiments on the inhibition <strong>of</strong> aconitase by enzymatically prepared<br />

fluorocitric acid. Biochemistry Journal 79, 261-268.<br />

Keywords: inhibition/aconitase/fluorocitrate/enzyme<br />

Abstract: A new method has been worked out for testing the activity <strong>of</strong> fluorocitrate on soluble aconitase.<br />

In this a cruder enzyme preparation is used taken to an intermediate stage <strong>of</strong> fractionation which does not<br />

require reactivation with ferrous salts and cysteine.<br />

Peters, R A. and Shorthouse, M. (<strong>1964</strong>). Fluoride metabolism in plants. Nature 202, 21-22.<br />

Keywords: fluoride/metabolism/persistence in plants<br />

Abstract: Grass seedlings exposed to inorganic fluoride solutions do not take up appreciable amounts <strong>of</strong><br />

fluoride until concentrations <strong>of</strong> more than 1.0 mM (19 ppm) are used. No formation <strong>of</strong> organic fluoride has<br />

been found even with exposure to 15.75 mM fluoride, indicating that there is no formation <strong>of</strong> fluoroacetate<br />

or similar compounds.<br />

Peters, R A. and Shorthouse, M. (1966). Note upon the behaviour <strong>of</strong> rat brain tissue treated with<br />

fluoroacetate in vitro. Biochemical Pharmacology 15, 2130-2131.<br />

Keywords: brain/fluoroacetate/fluorocitrate<br />

Abstract: We could not therefor demonstarte an effect <strong>of</strong> fluoroacetate in vitro, and conclude that any<br />

synthesis <strong>of</strong> fluorocitrate must be very slight if it occurs at all.<br />

Peters, R A. and Shorthouse, M. (1967). Observations <strong>of</strong> the metabolism <strong>of</strong> fluoride in Acacia georginae<br />

and some other plants. Nature 216, 80-81.<br />

Keywords: metabolism/occurrence in nature<br />

Abstract: When working with homogenates <strong>of</strong> Acacia georginae in an attempt to trace the pathway <strong>of</strong><br />

fluoroacetate synthesis, we found that there was a loss <strong>of</strong> fluoride, and we extended our experiments to<br />

some other plants to study this effect. This communication describes experiments which have led us to<br />

believe that plants can convert fluoride, possibly in part, to a volatile form.<br />

Peters, R A. (1967). Experiments upon the biochemistry <strong>of</strong> the synthesis <strong>of</strong> fluoroacetate in the Australian<br />

Georginae and their significance. Revue roumaine de Biochimie 4, 79-91.<br />

Keywords: biochemistry/fluoroacetate<br />

Peters, R A. and Shorthouse, M. (1969). An organically combined fluorine compound in bone. The<br />

Biochemical Journal 113, 9P.<br />

Keywords: fluorine/bone/fluoride/aconitase/liquid chromatography/fluorocitrate<br />

Abstract: We have now found that some extracts <strong>of</strong> fluorosed bones from cattle contained small amounts <strong>of</strong><br />

fluorocitric acid, which have been identified by their capacity for inhibiting aconitase and by gas liquid<br />

chromatography.<br />

Peters, R A. and Shorthouse, M. (1970). Aconitate hydratase. Some new observations with especial relation<br />

to its use as a test system for fluorocitrate, together with studies on the electrophoretic separation <strong>of</strong><br />

components <strong>of</strong> the crude enzyme. Biochimica et biophysica acta 220, 569-579.<br />

Keywords: fluorocitrate/enzyme/aconitase/analysis/biochemistry<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Preparations <strong>of</strong> aconitate hydratase from pig heart, purified to the first ethanol stage have been<br />

studied, and evidence supporting the existence <strong>of</strong> two centres has been confirmed; wide variations in the<br />

ratio <strong>of</strong> the isocitrate hydro-lase to that <strong>of</strong> the citrate hydro-lase have been found. Additive effects occur on<br />

the enzymatic action when on <strong>of</strong> the substrates is added to the other, both additions being at vmax.<br />

Fluorocitrate never inhibits these mixed enzymes completely.<br />

Peters, R A. and Shorthouse, M. (1972). Fluorocitrate in plants and food stuffs. Phytochemistry 11 , 1337-<br />

1338.<br />

Keywords: metabolism/persistence in plants/occurrence in nature/biosynthesis/defluorination<br />

Abstract: Mon<strong>of</strong>luorocarbon acids can be formed from inorganic fluoride by single cell cultures <strong>of</strong> Acacia<br />

georginae and tea. Fluorocitrate is also present in small amounts in commercial specimens <strong>of</strong> tea and<br />

oatmeal. The significance <strong>of</strong> these observations is discussed, especially in relation to the toxic plants.<br />

Peters, R A. and Shorthouse, M. (1972). Formation <strong>of</strong> mon<strong>of</strong>luorocarbon compounds by singel cell cultures<br />

<strong>of</strong> Glycine max growing on inorganic fluoride. Phytochemistry 11, 1339.<br />

Keywords: fluoride/biosynthesis/persistence in plants<br />

Peters, R. (1952). Lethal synthesis. Proceedings <strong>of</strong> the <strong>Royal</strong> Society <strong>of</strong> London 139, 142-170.<br />

Peters, R. (1954). Biochemical light upon an ancient poison : a lethal synthesis. Endeavour 13, 137-154.<br />

Keywords: occurrence in nature/metabolism/mode <strong>of</strong> action<br />

Peters, R., Shorthouse, M., Ward, P. F. V., and McDowell, E. M. (1972). Observations upon the<br />

metabolism <strong>of</strong> fluorocitrate in rats. Proceedings <strong>of</strong> the.<strong>Royal</strong>.Society.<strong>of</strong> London.Series.B. 182, 1-8.<br />

Keywords: metabolism/acute toxicity/fluorocitrate/rats<br />

Peters, R. A. (1952). The puzzle for therapy in fluoroacetate poisoning. British medical journal 1165-1170.<br />

Keywords: fluoroacetate/poisoning/treatment/sodium fluoroacetate/metabolism/enzyme<br />

Peters, R. A. (1957). Mechanism <strong>of</strong> the toxicity <strong>of</strong> the active constituent <strong>of</strong> Dichapetalum cymosum and<br />

related compounds. Advances in enzymology and related subjects <strong>of</strong> biochemistry 18, 113-159.<br />

Keywords: mode <strong>of</strong> action/occurrence in nature/metabolism/biochemistry<br />

Peters, R. A. and Morselli, P. L. (1965). Observations on the use and action <strong>of</strong> monoacetin in fluoroacetate<br />

poisoning. Biochemical Pharmacology 14, 1891-1893.<br />

Keywords: fluoroacetate/poisoning/fluorocitrate/monoacetin<br />

Peters, R. A. and Shorthouse, M. (1971). Oral toxicity <strong>of</strong> fluoroacetate and fluorocitrate in rats. Journal <strong>of</strong><br />

physiology 216, 40-41.<br />

Keywords: acute toxicity/mammals/fluoroacetate/fluorocitrate/rats<br />

Peters, R. A. (1972). Some metabolic aspects <strong>of</strong> fluoroacetate especially related to fluorocitrate. In 'Carbonfluorine<br />

compounds : chemistry, biochemistry and biological activities : a Ciba Foundation symposium'. pp.<br />

55-76. (Associated Scientific Publishers: Amsterdam; London; New York.)<br />

Keywords: product chemistry/mode <strong>of</strong> action/occurrence in<br />

nature/fluoroacetate/fluorocitrate/chemistry/biochemistry<br />

Peters, R. A., Spencer, H., and Bidstrup, P. L. (1981). Subacute fluoroacetate poisoning. Journal <strong>of</strong><br />

occupational medicine 23, 112-113.<br />

Keywords: diagnosis/occupational exposure/fluoroacetate/poisoning<br />

Peterson, D. R. and [team leader] (1994). Possum management in New Zealand. (Parliamentary<br />

Commissioner for the Environment: Wellington.)<br />

Keywords: acute toxicity/aerial control/aquatic species/bait degradation/birds/cats/deer/field<br />

efficacy/ground control/invertebrates/mammals/non-target species/occurrence in nature/persistence in<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

animals/persistence in plants/persistence in soil/persistence in water/possums/rabbits/secondary<br />

poisoning/target species/welfare<br />

Abstract: This investigation has confirmed the magnitude <strong>of</strong> the threat posed by possums, which should not<br />

be underestimated. New Zealand's native biota and natural values are at risk from the damaging effects <strong>of</strong><br />

possums and, although the incidence <strong>of</strong> bovine Tb may not have serious financial effects on individual<br />

farmers, it could significantly affect the New Zealand economy. Ongoing possum control over more than a<br />

third <strong>of</strong> New Zealand, using current techniques, will be essential until there is a breakthrough in the search<br />

for new methods <strong>of</strong> control.<br />

Peterson, J. E. (1975). A gas chromatographic method for sodium fluoroacetate (Compound 1080) in<br />

biological materials. Bulletin <strong>of</strong> environmental contamination and toxicology 13, 751-757.<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080<br />

Abstract: Title says it all<br />

Phillips, A. H. and Langdon, R. G. (1955). Incorporation <strong>of</strong> mon<strong>of</strong>luoroacetic acid into the nonsaponifiable<br />

lipids <strong>of</strong> the rat liver. Archives <strong>of</strong> biochemistry and biophysics 58, 247-249.<br />

Keywords: metabolism/fluoroacetate/liver<br />

Abstract: Mon<strong>of</strong>luoroacetic acid is found to be efficiently utilized as a substrate for the biosynthesis <strong>of</strong><br />

fluorine-containing nonsaponifiable lipids by a cell-free preparation <strong>of</strong> rat liver.<br />

Phillips, M. A. and Worden, A. N. (1957). The mammalian oral toxicity <strong>of</strong> fluoroacetamide. Journal <strong>of</strong> the<br />

science <strong>of</strong> food and agriculture 8, 653-657.<br />

Keywords: mammals/acute toxicity/treatment/fluoroacetamide<br />

Phillips, M. A. (1960). Fluoroacetamide and some derivatives as pesticides. Agricultural and Veterinary<br />

Chemicals 1, 151-153.<br />

Keywords: fluoroacetamide<br />

Pierce, R. J. and Montgomery, P. J. The fate <strong>of</strong> birds and selected invertebrates during a 1080 operation.<br />

[121], -17. 1992. Wellington, Department <strong>of</strong> Conservation. Science and research internal report.<br />

Ref Type: Report<br />

Keywords: non-target species/birds/invertebrates/1080/possums<br />

Abstract: An aerial 1080 poison operation for possums at Waipoua Forest in spring 1990 applied cereal<br />

pellets lured with cinnamon. Numbers <strong>of</strong> brown kiwi, moreporks, fernbirds, kokako and common diurnal<br />

birds were monitored before, during and after the operation, while small numbers <strong>of</strong> insects and kauri snails<br />

were tested for 1080 uptake. Of the birds only blackbird and tomtit showed possible declines after the<br />

poisoning. Although some kiwi had consumed non-toxic baits, no 1080 related deaths were detected<br />

following the poison operation. Low concentrations <strong>of</strong> 1080 were found in the insects, but none <strong>of</strong> the<br />

kauri snails had detectable levels <strong>of</strong> 1080.<br />

Polter, C. (1967). Influence <strong>of</strong> mon<strong>of</strong>luoroacetic acid on oxygen uptake <strong>of</strong> pea roots after cultivation under<br />

different conditions. Biologisches Zentralblatt 86, 567-581.<br />

Keywords: mon<strong>of</strong>luoroacetic acid/citrate/citric acid/metabolism/mode <strong>of</strong> action/persistence in plants<br />

Abstract: After sufficiently long influence <strong>of</strong> 10mM/l mon<strong>of</strong>luoroacetic acid (MFA) (pH 4.5), the oxygen<br />

consumption in segments <strong>of</strong> seedling roots is nearly completely blocked. By addition <strong>of</strong> citrate and citric<br />

acid measurements it was found that MFA probably exerts the sime effect on pea roots as known for animal<br />

tissues. 1 mMol MFA has no effect. If no substrate is <strong>of</strong>fered during the MFA action, oxygen consumption<br />

is less hampered than at presence <strong>of</strong> sucrose. Roots cultivated in vitro behave similar to seedling roots; their<br />

O2 consumption is not as much suppressed by MFA. Addition <strong>of</strong> 2.10-8 molar 2,4-dichlorophenoxycetic<br />

acid (2,4-D) to the nutrient solution does not induce considerable changes in the sensitivity <strong>of</strong> O2<br />

consumption <strong>of</strong> roots against MFA. After 6 hours <strong>of</strong> MFA action all segments contained less dry matter<br />

than the controls. They were the smaller the stronger O2 uptake had been blocked, which fact is explained<br />

to be the result <strong>of</strong> suppressed uptake <strong>of</strong> substrate. From the experiment it is concluded that in 3 days old<br />

seedling roots most <strong>of</strong> the O2 consumption is combined with dehydration in acid-metabolism and that there<br />

is no difference in dehydration-type between the root segments <strong>of</strong> meristems. elongation and differentiation<br />

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Appendix C<br />

zones. When substrate is lacking even small amounts <strong>of</strong> substances not being decomposed via isocitrcic<br />

acid, probably proteins are oxidised.<br />

Poole, W. E. (1963). Field enclosure experiments on the technique <strong>of</strong> poisoning the rabbit, Oryctolagus<br />

cuniculus (L.) : V. A study <strong>of</strong> concentrations <strong>of</strong> "1080" in bait material. CSIRO wildlife research 8, 154-<br />

165.<br />

Keywords: field efficacy/ground control/rabbits/poisoning<br />

Abstract: Four 4-acre enclosures were kept stocked with rabbits and used to compare, under different<br />

seasonal conditions, the effectiveness <strong>of</strong> bait, cheifly carrot poisoned at concentrations <strong>of</strong> 0.01%, 0.02% or<br />

the usual field strength <strong>of</strong> 0.04% <strong>of</strong> sodium fluoroacetate.<br />

Poole, W. E., Carpenter, M., and Simms, N. G. (1990). Subspecific separation in the Western Grey<br />

Kangaroo, Macropus fuliginosus: a morphometric study. Aust.Wildl.Res. 17, 159-168.<br />

Keywords: fluoroacetate/tolerance/marsupials<br />

Abstract: Morphometric analyses <strong>of</strong> cranial and body measurements from western grey kangaroos were<br />

undertaken as a possible means <strong>of</strong> determining the taxonomic status <strong>of</strong> the described forms. The kangaroos<br />

were assigned arbitrarily to one <strong>of</strong> four geographic groups, those from Kangaroo Island (Macropus<br />

fuliginosus fuliginosus) and three from the mainland, comprising animals taken from the western<br />

(Macropus fuliginosus ocydromus) and eastern Macropus fuliginosus melanops) extremities <strong>of</strong> their<br />

distribution together with an intermediate geographic group. Four types <strong>of</strong> analysis - analysis <strong>of</strong> variance,<br />

canonical variate analysis, principal component analysis and discriminant function analysis - were utilised<br />

and their outcome assessed. Earlier findings based on diverse criteria such as aspects <strong>of</strong> reproductive<br />

cycles, distribution <strong>of</strong> red-cell lactate dehydrogenase types, and responses to ingestion <strong>of</strong> fluoroacetate,<br />

revealed that M.f.fuliginosus was quite distinct from M.f.melanops on the adjacent mainland and to a lesser<br />

extent from M.f.ocydromus in Western Australia. The present results confirm these levels <strong>of</strong> affinity and<br />

suggest that western grey kangaroos comprise at least two principal subspecific forms, a uniform group,<br />

M.f.fuliginosus, from Kangaroo Island and a composite group on the mainland that intergrades clinally in<br />

its morphological traits along a longitudinal (west-east) gradient. M.f.melanops Gould is the senior name<br />

for the mainland complex.<br />

Popa, D. (1978). <strong>Research</strong> concerning the action <strong>of</strong> sodium mon<strong>of</strong>luoroacetate on the protoplasmic<br />

streaming in barley Hordeum-vulgare root hairs, part 2. Stud Univ Babes-Bolyai Biol 1, 9-15.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/mode <strong>of</strong> action/persistence in plants<br />

Abstract: The author has studied the evolution <strong>of</strong> protoplasmic streaming in barley root hairs treated with<br />

sodium mon<strong>of</strong>luoroacetate (MFA), in three experimental variants.<br />

In the first variant, the treatment with a 10- 2 M solution <strong>of</strong> MFA for 60 minutes was followed by a 30<br />

minute washing with buffer solution and by treatment with a 10- 4 M solution <strong>of</strong> ATP for 30 minutes. The<br />

results obtained indicate that the exogenous ATP added after the removal <strong>of</strong> the MFA has increased the<br />

speed <strong>of</strong> protoplasmic streaming.<br />

In the second variant the root hairs were treated simultaneously with MFA (10 -2 M) and ATP (10 -4 M) for<br />

120 minutes. The combined treatment resulted in strong inhibition <strong>of</strong> protoplasmic streaming. In the third<br />

variant, administration <strong>of</strong> MFA in 10 -2 M concentration for 60 minutes was followed by washing with buffer<br />

solution for 30 minutes andby addition <strong>of</strong> LiCl (10 -2 M) for 30 minutes. The results show that LiCl was not<br />

able to remove completely the modification caused by MFA in the protoplasmic structure.<br />

The author has drawn the conclusion based on the experimental data that MFA decreases the speed od<br />

protoplasmic streaming by inhibiting respiration and by increasing the vicosity <strong>of</strong> protoplasm.<br />

Posner, C. J. and Berman, D. A. (1967). A mathematical analysis <strong>of</strong> the interval-strength relationship in the<br />

rat ventricle strip and its modification by fluoroacetate. Journal <strong>of</strong> pharmacology and experimental<br />

therapeutics 156, 166-177.<br />

Keywords: pathology/analysis/fluoroacetate<br />

Potter, V. R. and Busch, H. (1950). Citric acid content <strong>of</strong> normal and tumor tissues in vivo following<br />

injection <strong>of</strong> fluoroacetate. Cancer <strong>Research</strong> 10, 353-356.<br />

Keywords: citric acid/fluoroacetate/citrate/Krebs cycle/metabolism<br />

Abstract: Previous investigations have indicated that tumor tissues are deficient in enzymes which oxidise<br />

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Appendix C<br />

pyruvate via the Krebs citric acid cycle. The work <strong>of</strong> Buffa and Peters <strong>of</strong>fered a means for testing the<br />

ability <strong>of</strong> tumor to produce citrate in vivo, since oxidation <strong>of</strong> citric acid is rpevented and the compound<br />

accumulates following injections <strong>of</strong> sodium fluoroacetate.<br />

Powlesland, R. G., Knegtmans, J. W., and Marshall, I. S. J. Evaluating the impacts <strong>of</strong> 1080 possum control<br />

operations on North Island robins, North Island tomtits and moreporks at Pureora- preliminary results.<br />

Science for Conservation 74, -22. 1998. Department <strong>of</strong> Conservation New Zealand.<br />

Ref Type: Report<br />

Keywords: 1080/non-target species/poison/carrot/baits/possums/birds/poisoning<br />

Abstract: This report describes results from the first two years <strong>of</strong> a three-year programme to determine<br />

whether the costs and benefits <strong>of</strong> aerial 1080 possum control operations to North Island robins (Petroica<br />

australis longipes), North Island tomtits (Petroica macrocephala toitoi) and moreporks (Ninox<br />

novaeseelandiae) in Pureora Forest Park. Prior to this study, the five-minute count technique had been used<br />

to quantify mortality <strong>of</strong> forest passerines during aerial possum control operations. During this study robins<br />

were individually colour-banded, and moreporks radio tagged at both treatment and non-treatment study<br />

areas. The poison operation took place in mid-September 1996 (carrot baits, 15 kg/ha, 1080 0.08% ww).<br />

An audit after the operation indicated that only 9.9% wastage (chaff) by weight was produced, rather than<br />

the expected c. 20%. This suggests that the other 50% <strong>of</strong> teh expected chaff was not screened out and so<br />

was made toxic and distributed with the baits. No possums were trapped in the treatment area during<br />

October and December 1996. Rodent population indices from foot-print tracking tunnels indicated the rat<br />

population (known to be mainly Rattus rattus) had declined markedly in the treatment area (95% in June<br />

1996 to 5% in October 1996) following the poison operation, and indices remained low (5-10%) during the<br />

robin nesting season (October - February).Twelve (54.5%) <strong>of</strong> the 22 banded robins in the treatment area<br />

disappeared during the fortnight immediately following the poison operation, but none <strong>of</strong> 24 in the nontreatment<br />

area. If the mortality is considered with regard to the number <strong>of</strong> banded and unbanded ronins in a<br />

defined area, 12 (42.8%) <strong>of</strong> 28 robins disappeared from the treatment area, but none in the non-treatment<br />

area. All three robins found dead following the operation tested positive for 1080. In the treatment area,<br />

nesting success (72%, n=18 nests) was much greater than in the non-treatment area (11%, n=35 nests; 0.4,<br />

n=14 pairs). The high nesting success in the treatment area resulted in the number <strong>of</strong> robins present just<br />

before the start <strong>of</strong> the next nesting season (August 1997) being 36, a 28.6% increase in the number present<br />

prior to the posion operation. In contrast, teh numbers present in the non-treatment area remained much the<br />

same., 32 in September 1996 as compared with 33 in August 1997. All five tomtits, including two banded<br />

birds, that were regularly fed in the treatment area disappeared immediately after the poisoning operation.<br />

No tomtits were monitored in the non-treatment area. One <strong>of</strong> six radio-tagged moreporks (16.7%) in the<br />

treatment area was found dead during the poison operation and tested positive for 1080. The single radiotagged<br />

mroepork in teh non-treatment area was alive several months afterwards.<br />

Powlesland, R. G., Knegtmans, J. W., and Marshall, I. S. J. (1999). Costs and benefits <strong>of</strong> aerial 1080<br />

possum control operations using carrot baits to North Island robins (Petroica australis longipes), Pureora<br />

Forest Park. New Zealand journal <strong>of</strong> ecology 23, 149-159.<br />

Keywords: field efficacy/non-target species/birds/1080/treatment/possums<br />

Powlesland, R. G., Knegtmans, J. W., and Styche, A. Impacts <strong>of</strong> Aerial 1080 possum control operations on<br />

North Island robins and moreporks at Pureora in 1997 and 1998. Science for Conservation 133. 1999.<br />

Department <strong>of</strong> Conservation, New Zealand.<br />

Ref Type: Report<br />

Keywords: 1080<br />

Powlesland, R. G., Knegtmans, J. W., and Styche, A. (2000). Mortality <strong>of</strong> North Island tomtits (Petroica<br />

macrocephala toitoi) caused by aerial 1080 possum control operations, 1997-98, Pureora Forest Park. New<br />

Zealand journal <strong>of</strong> ecology 24, 161-168.<br />

Keywords: non-target species/birds/1080/treatment/possums/poisoning/carrot/baits/rodents<br />

Powlesland, R. G., Wills, D. E., August, A. C. L., and August, C. K. (2003). Effects <strong>of</strong> a 1080 operation on<br />

kaka and kereru survival and nesting success, Whirinaki Forest Park. New Zealand journal <strong>of</strong> ecology 27,<br />

125-137.<br />

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Appendix C<br />

Keywords: 1080/birds/treatment/poison/carrot/baits/possums/rats/predators/non-target species<br />

Abstract: To measure the costs and benefits <strong>of</strong> an aerial 1080 possum control operation to kereru and kaka<br />

in Whirinaki Forest Park, individuals <strong>of</strong> both species were radio-tagged from October 1998 to June 2002.<br />

We monitored birds in one treatment and one non-treatment study area to compare toxin-related mortality,<br />

nesting success and survival. The poison operation involved the spreading <strong>of</strong> non-toxic carrot baits on 1<br />

May 2000, and the toxic baits on 17/18 May 2000. Possums and rats were moderately abundant in both<br />

study areas prior to the poison operation, but afterwards few possums and rats remained in the treatment<br />

area. All radio-tagged kaka and kereru in the treatment area survived the poison operation. No radio-tagged<br />

kereru and too few radio-tagged kaka bred in either study area during the 2000/01 nesting season to show<br />

whether reduced possum and rat populations would enable the birds to nest more successfully. A reduction<br />

in possum and rat densities in the non-treatment area (and an increase in densities in the treatment area)<br />

during 2001/02 meant that during the second nesting season after the poison operation, possum and rat<br />

densities were similar in the two study areas. The nesting effort and success <strong>of</strong> kaka and kereru is described<br />

for each <strong>of</strong> four nesting seasons, with the main cause <strong>of</strong> nesting failure for both species being predation.<br />

While no radio-tagged adult male kaka died during the study, 6 females did, giving them a mean life<br />

expectancy <strong>of</strong> 9.5 years. In contrast, radio-tagged adult kereru suffered high mortality, resulting in a mean<br />

life expectancy <strong>of</strong> just 1.5 years. Predation by introduced mammalian predators was the main cause <strong>of</strong><br />

mortality <strong>of</strong> kaka eggs, chicks, fledglings and adult females, and <strong>of</strong> kereru eggs, chicks, fledglings and<br />

adults. Effective control <strong>of</strong> introduced mammalian predators, including control by aerial 1080 operations,<br />

just before mast fruiting events that invariably promote prolific kaka and kereru breeding, should benefit<br />

these bird populations.<br />

Prestwich, G. D., Gayen, A. K., Phirwa, S., and Kline, T. B. (1983). 29-Flurophytosterols: novel proinsecticides<br />

which cause death by dealkylation. Biotechnology 1, 62-65.<br />

Keywords: invertebrates/USA/poison/fluoroacetate/fluorocitrate<br />

Abstract: Unlike invertebrates, phytophagous insects lack the capacity for de novo synthesis <strong>of</strong> the steroid<br />

nucleus and rely on C28 and C29 phytosterols as sources for C26 cholesterol. The authors report on recent<br />

work in the USA to exploit the phytosterol dealkylation pathway to release, in vivo, the latent poison<br />

fluoroacetate, which undergoes 'lethal synthesis' to fluorocitrate. Four 29-fluorophytosterols were prepared<br />

in diastereometrically pure form by total synthesis from stigmasterol, and 1 was prepared from 24oxocholesterol.<br />

The recrystallised 29-fluorosterols were dissolved in dichloromethane and applied as a<br />

coating to wheat germ in the artifical diet <strong>of</strong> larvae <strong>of</strong> Manduca sexta (Joh.). <strong>Control</strong> larvae received either<br />

50 p.p.m. stigmasterol or no additional sterols. First-instar larvae were kept on the diet from the 7th day<br />

(test day 0) after egg collection at 26 deg C, RH 65% and LD 17:7. All 5 29-fluorophytosterols<br />

significantly impaired larval growth and development. The doses affording 50% reduction in maximum<br />

larval weight, survival to test day 21 and pupation were 110, 300 and 150 p.p.m., respectively for 29fluorositosterol,<br />


1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: fluorine/fluorocitrate/fluoroacetate/inhibition/acetate/fluoride/invertebrates<br />

Abstract: Substitution <strong>of</strong> fluorine for hydrogen in essential sterols, juvenile hormones and pheromones can<br />

lead to materials that interfere with insect growth, development or communication, in novel and potentially<br />

useful ways. In this paper, examples drawn from work in these areas are used to illustrate fluorocitrate<br />

generation via dealkylation <strong>of</strong> 29-fluorophytosterols; fluoroacetate release by beta-oxidation <strong>of</strong> fatty<br />

alcohols and acids; inhibition <strong>of</strong> juvenile hormone esterase by trifluoromethyl ketones; inhibition <strong>of</strong><br />

antennal esterases that hydrolyse acetate pheromones; and sensory disruption by acyl fluorides that mimic<br />

aldehyde pheromones<br />

Preuss, P. W. The metabolism <strong>of</strong> fluoroacetic acid in plants. Chemistry 28[12], 4910. 1967.<br />

Ref Type: Abstract<br />

Keywords: metabolism/fluoride/fluorine/persistence in plants/fluoroacetate<br />

Abstract: Acacia georginae, a plant native to Australia, is known to contain mon<strong>of</strong>luoroacetic acid. We<br />

have shown that this compound is synthesised when seedlings <strong>of</strong> Acacia georginae are grown axenically<br />

and supplied with sodium fluoride. The metabolsim <strong>of</strong> mon<strong>of</strong>luoroacetic acid was studied in Acacia<br />

georginae, peanut (Arachis hypogaea L.), castor bean (Ricinus communis L.), and Pinto bean (Phaseolus<br />

vulgaris). When 2- 14 C-fluoroacetate was supplied to seedlings <strong>of</strong> the above four plants, it was demonstrated<br />

that the radioactive carbon is evolved as 14 CO2 and incorporated into various water-soluble and lipid<br />

fractions. Evolution <strong>of</strong> 14 CO2 from germinated seeds <strong>of</strong> the four plants was studied on a time-course basis.<br />

Incorporation <strong>of</strong> radioactivity and fluorine into lipids was studied by means <strong>of</strong> thin-layer chromatography,<br />

gas chromatography and mass spectrometry. Results idnicate that Acacia and otehr plants can metabolise<br />

mon<strong>of</strong>luoroacetic acid and cleave the carbon-fluorine bond. The data obtained are not consistent with the<br />

generally accepted scheme <strong>of</strong> fluoroacetate utilisation and toxicity in animals and a hypothesis is presented<br />

to explain the metabolism <strong>of</strong> fluoroacetate in plants. The synthesis <strong>of</strong> several fluoroorganic compounds is<br />

suggested and the metabolic reactions leading to such syntheses are discussed<br />

Preuss, P. W., Lemmens, A. G., and Weinstein, L. H. (1968). Studies on fluoro-organic compounds in<br />

plants. I. Metabolism <strong>of</strong> 2- 14 C-fluoroacetate. Contributions from Boyce Thompson Institute 23, 25-31.<br />

Keywords: metabolism/fluoroacetate/enzyme/persistence in plants/defluorination<br />

Abstract: The metabolism <strong>of</strong> 2- 14 C-sodium fluoroacetate was studied in Acacia georginae, peanut, castor<br />

bean and 'Pinto' bean. When this compound was supplied to sterile seedlings <strong>of</strong> the four plants, 14 CO2 was<br />

evolved and 14 C was incorporated into water-soluble fractions and lipids. Results indicate that the plants<br />

studied contained an enzyme system capable <strong>of</strong> cleaving the carbon-fluorine bond.<br />

Preuss, P. W. and Weinstein, L. H. (1969). Studies on fluoro-organic compounds in plants II.<br />

Defluorination <strong>of</strong> fluoroacetate. Contributions from Boyce Thompson Institute 24, 151-155.<br />

Keywords: persistence in plants/metabolism/sodium fluoroacetate<br />

Abstract: Experiments were carried out to 1) confirm the germinating peanut seeds contain enzymes which<br />

split the carbon-fluorine bond <strong>of</strong> fluoroacetic acid and 20 determine if fluoroacetic acid can by metabolized<br />

to fluor<strong>of</strong>atty acids in Acacia georginae. About 15 per cent <strong>of</strong> the fluorine supplied to germinating peanut<br />

seeds as sodium fluoroacetate was found in the inorganic form in the seedlings or in the incubation medium<br />

after 48 hours. Only 2 to 5 per cent was detected aft incubation <strong>of</strong> boiled seeds. The gas chromatographic<br />

patter <strong>of</strong> fatty acids control <strong>of</strong> fluoroacetate-treated Acacia seeds was the same and analysis <strong>of</strong> each peak by<br />

mass spectrometry provided no evidence for the presence <strong>of</strong> a fluorine atom attached to the fatty acids.<br />

Pridmore, S. A. (1978). Fluoroacetate poisoning: nine years later [letter]. Medical Journal <strong>of</strong> Australia 2,<br />

269-270.<br />

Keywords: fluoroacetate/poisoning/humans<br />

Pronk, A. Isolation and characterisation <strong>of</strong> 1080-degrading bacteria from New Zealand soils. -17. 2001.<br />

Ref Type: Report<br />

Keywords: bacteria/soil/degradation<br />

Abstract: A range <strong>of</strong> soil bacteria is capable <strong>of</strong> using 1080 as their sole carbon source. Both soils and<br />

isolation techniques raised a number <strong>of</strong> different isolates. The descriptions and ID-kit results indicate that<br />

the isolates belong to a range <strong>of</strong> species. Some <strong>of</strong> the isolates with simialr results might belong to the same<br />

species. For the true identification <strong>of</strong> the isolates the amplified 16S gene should be sequenced. Due to the<br />

165


1080 Reassessment Application October 2006<br />

Appendix C<br />

inability <strong>of</strong> the majority <strong>of</strong> natural microorgansims to grow under artificial conditions the obtained<br />

collection <strong>of</strong> isolates is not a good representation <strong>of</strong> all 1080 degrading bacteria in soil. With the primers<br />

used in this study it could not be shown that any <strong>of</strong> the isolates contained a gene similar to dehH1 in<br />

Moraxella. Results from PCRs with the 16S and dehalogenase primers indicate that inhibitory substances<br />

were present in both soil samples as well as in the enrichment culture <strong>of</strong> soil B (Manawatu).<br />

Quin, J. I. and Clark, R. (1947). Studies on the action <strong>of</strong> potassium mon<strong>of</strong>luoroacetate (CH2FCOOK)<br />

[Dichapetalum cymosum (Hook) Engl.] toxin on animals. Onderstepoort journal <strong>of</strong> veterinary science and<br />

animal industry 22, 77-82.<br />

Keywords: mon<strong>of</strong>luoroacetate/heart/rabbits/cardiac/mammals/acute toxicity/bacteria/poison/sublethal<br />

effects/chronic poisoning<br />

Abstract: Considerable variation in susceptibility to potassium mon<strong>of</strong>luoroacetate has been found to exist<br />

among various species <strong>of</strong> laboratory animals. The compound is not affected by actively fermenting ruminal<br />

flora nor does its presence affect such fermentation. Direct observations on the heart <strong>of</strong> rabbits and sheep<br />

injected with this compound have proved it to be a heart poison probably affecting the cardiac conducting<br />

mechanism thus leading to partial or complete heart block.<br />

Ramirez, M. (1986). Inebriation with pyridoxine and fluoroacetate: a case report. Veterinary and human<br />

toxicology 28, 154.<br />

Keywords: poisoning/fluoroacetate/humans<br />

Rammell, C. G., Fleming, P. A., and O'Hara, P. J. (1977). 1080 poisoning. New Zealand medical journal<br />

85, 295-296.<br />

Keywords: 1080/poisoning/fluorine/urine/humans<br />

Abstract: Letter to the editor in response to article by Parkin, McGiven and Bailey in 9 February 1977 issue<br />

<strong>of</strong> New Zealand Medical Journal.<br />

Rammell, C. G. and Fleming, P. A. (1978). Compound 1080 : properties and uses <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate in New Zealand. (Animal Health Division, Ministry <strong>of</strong> Agriculture and Fisheries:<br />

Wellington.)<br />

Keywords: acute toxicity/aerial control/aquatic species/bait degradation/birds/cats/deer/diagnosis/field<br />

efficacy/ground control/invertebrates/mammals/metabolism/mode <strong>of</strong> action/non-target species/occurrence<br />

in nature/pathology/persistence in animals/persistence in plants/persistence in soil/persistence in<br />

water/possums/product chemistry/rabbits/secondary poisoning/target species/treatment/welfare/1080<br />

Abstract: Preparation <strong>of</strong> this book grew out <strong>of</strong> the need to provide a ready reference source for the answers<br />

to many <strong>of</strong> the questions that were being asked about the use <strong>of</strong> 1080 in New Zeland. Much <strong>of</strong> the<br />

information on 1080 was scattered throughout a variety <strong>of</strong> publications and unpublished reports. This book<br />

is an attempt to present, in a readily digestible form, the available information as it applies to the New<br />

Zealand situation.<br />

Rammell, C. G., Hoogenboom, J. J. L., Julian, A. F., and Livingstone, P. G. (1985). Treatment <strong>of</strong> 1080<br />

poisoning in dogs with glycerol monoacetate. New Zealand veterinary journal 33, 149-150.<br />

Keywords: diagnosis/treatment/1080<br />

Abstract: Therapy using glycerol monoacetate, as is used for humans, has been applied to dogs.<br />

Observation <strong>of</strong> circulating acetate levels indicated that GMA doses <strong>of</strong> more that 100mg/kg are required.<br />

Rammell, C. G. (1993). Persistence <strong>of</strong> compound 1080 in sheep muscle and liver. Surveillance 20(1), 20-<br />

21.<br />

Keywords: metabolism/non-target species/persistence in animals/1080/lethal dose<br />

Abstract: Forty sheep were dosed orally with compound 1080 (sodium mon<strong>of</strong>luoroacetate) at or near the<br />

lethal dose rate and then sacrificed 2 to 32 hours after dosing to determine the 1080 residues in the muscle<br />

and liver. Compound 1080 concentrations in the muscle from sheep dosed at 200 u g/kg reached a<br />

maximum <strong>of</strong> about 110 ppb in 4 hours and decayed exponentially thereafter with a half-life <strong>of</strong> about 12<br />

hours. In liver, the maximum concentration <strong>of</strong> about 40 ppb was found at 2 hours with an exponential<br />

decay thereafter and half-life <strong>of</strong> about 3 hours. The data imply that 1080 should be undetectable (less than<br />

3 ppb) in meat from any sheep which inadvertently consumed 1080 more than 5 days pre-slaughter.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Ramsay, J. (1977). 1080 poisoning. New Zealand medical journal 85, 295.<br />

Keywords: humans/1080/poisoning/kidney<br />

Ramsey, L. L. and Patterson, W. I. (1951). A new qualitative test for mon<strong>of</strong>luoroacetic acid. Journal <strong>of</strong> the<br />

Association <strong>of</strong> Official Analytical Chemists 34, 827-831.<br />

Keywords: product chemistry<br />

Ramsey, L. L. (1954). Report on sodium fluoroacetate (1080). Journal <strong>of</strong> the Association <strong>of</strong> Official<br />

Analytical Chemists 37, 581-586.<br />

Keywords: product chemistry<br />

Randerson, J. (2002). Resistant rabbits are fighting back. New scientist 17th August, 13.<br />

Keywords: 1080/lethal dose/rabbits/resistance/tolerance<br />

Abstract: Rabbits in Australia are developing resistance to a widely used poison, raising fears that the<br />

authorities are losing their battle to control the invaders. It's the first time a small mammal other than mice<br />

has become resitant to the pesticide, and serves as a warning to countries such as New Zealand that use<br />

huge quantities <strong>of</strong> it.<br />

In some areas <strong>of</strong> the outback there are as many as 3000 rabbits per square kilometre, giving<br />

conservationists and farmers alike a major headache. Attempts to wipe out the animals using lethal viruses<br />

have proved only partially successful. Last week, New Scientist revealed that researchers are now<br />

developing a virus they hope will make the pests sterile.<br />

But the most widely used control measure remains the poison sodium fluoracetate - better known as 1080.<br />

The chemical is deployed against mammal pests in various countries, but New Zealand accounts for 90 per<br />

cent <strong>of</strong> its use, mainly to control pssums introduced from Australia.<br />

The poison is particularly useful in Australia because fluoracetate is produced as a natural defence by<br />

several Australian plant species. So while rabbits are vulnerable to it, it does little damage to native planteating<br />

mammals, which are up to 100 times less likely to succumb.<br />

But Laurie Twigg at the Department <strong>of</strong> Agriculture for Western Australian in Perth and his team have<br />

found that three rabbit populations repeatedly exposed to 1080 are becoming resistant to it. By comparing<br />

results from a similar study in 1979, they found that more than double to amount <strong>of</strong> poison is now needed<br />

to kill the same number <strong>of</strong> animals (Journal <strong>of</strong> Applied Ecology, vol 39, p 549).<br />

"I was surprised that we would find resistance in 25 years, " Twigg says. "We would advocate alternating<br />

the use <strong>of</strong> 1080 with other control measures," he says. James Randerson<br />

Rathore, A. K. (1985). Use <strong>of</strong> metoclopramide to prevent 1080-induced emesis in wild pigs. Journal <strong>of</strong><br />

wildlife management 49, 55-56.<br />

Keywords: pigs/1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/rabbits/stomach/secondary<br />

poisoning/poisoning/lethal dose/field efficacy<br />

Abstract: Wild pigs (Sus scr<strong>of</strong>a) in Australia annually casue damage worth 73.3 million dollars (Australian)<br />

to the agricultural and pastoral industry. Since 1971, Compound 1080 (sodium mon<strong>of</strong>luoroacetate) has<br />

been sued in New South Wales to control wild pigs. The recorded LD50 for pigs is


1080 Reassessment Application October 2006<br />

Appendix C<br />

Analytical Chemists 64, 19-24.<br />

Keywords: liquid chromatography/diagnosis/sodium fluoroacetate/1080<br />

Abstract: A sensitive high pressure liquid chromatographic method was developed for the determination <strong>of</strong><br />

sodium fluoroacetate (compound 1080) in canine gastric content. The procedure involves extraction <strong>of</strong><br />

1080 with water, methyl, ethyl ketone, and dilute base, followed by sample cleanup using octadecylsilane<br />

bonded phase cartridges and derivatization in ethyl acetate solution with O-p-nitrobenzyl-N-N'-diisopropylisouera<br />

(PNBDI). The compound was chromatographed on a 10 um silica column, and ultraviolet<br />

absorbance at 254 and 280 nm was measured. Recovery was greater than 95% for standard 1080 and in the<br />

70 - 90% range for spike samples (1-50 ppm).<br />

Reenilä, I., Tuomainen, P., Soinila, S., and Männistö, P. T. (1997). Increase <strong>of</strong> catechol-Omethyltransferase<br />

activity in rat brain microglia after intrastriatal infusion <strong>of</strong> fluorocitrate, a glial toxin.<br />

Neuroscience letters 230, 155-158.<br />

Keywords: brain/fluorocitrate<br />

Abstract: Striatal catechol-O-methyltransferase (COMT), monoamine oxidase B (MAO-B; an astroglial<br />

enzyme), alkaline phosphodiesterase I (PDE; a microglia/macrophage marker) and tyrosine hydroxylase<br />

(TH; catecholaminergic neuron marker) activities were analysed biochemically 1-3 days after infusion <strong>of</strong><br />

fluorocitrate, an astrocyte damaging agent. Astrocytes, microglia and neurons were stained<br />

immunohistochemically with specific antibodies (against glial fibrillary acidic protein, OX-42 and TH,<br />

respectively) and with COMT antiserum. Three days after fluorocitrate infusion the activity <strong>of</strong> MAO-B<br />

was reduced, whereas COMT and PDE activities were increased. The elevation <strong>of</strong> COMT<br />

immunoreactively co-localized to microglial cells, but not to astrocytes. In conclusion, this is the first<br />

report indicating that microglia contains COMT activity which may be increased in pathological conditions.<br />

Reetz, M. T. and Ruggeberg, C. J. (2002). A screening system for enantioselective enzymes based on<br />

differential cell growth. Chemical Communications 13, 1428-1429.<br />

Keywords: enzyme/fluoroacetate/inhibition/metabolism<br />

Abstract: The esterase-catalyzed enantioselective hydrolysis <strong>of</strong> the fluoroacetate <strong>of</strong> pantolactone leads to<br />

fluoroacetic acid, a toxic compound which inhibits the growth <strong>of</strong> esterase-producing yeast; this forms the<br />

basis <strong>of</strong> an ee-assay.<br />

Reid, K. A. Biochemical studies <strong>of</strong> fluoroacetate and 4-fluorothreonine biosynthesis in Streptomyces<br />

cattleya. 201. 1994. Queen's University <strong>of</strong> Belfast (Northern Ireland)Editor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: fluoroacetate/biosynthesis/fluoride/NMR/metabolism/bacteria<br />

Abstract: The production <strong>of</strong> fluoroacetic acid and 4-fluorothreonine in batch culture by the actinomycete<br />

Streptomyces cattleya NRRL 8057 was examined on a chemically defined medium containing 2 mM<br />

fluoride using GC-MS and $sp{19}$F NMR spectroscopy techniques. Fluoride uptake by cells did not<br />

begin until growth had ceased and closely reflected fluorometabolite levels found in culture supernatants.<br />

4-Fluorothreonine was detected prior to fluoroacetate and was present at higher concentrations throughout<br />

incubation, although levels <strong>of</strong> both compounds stabilised at about 0.75 mM after approximately three<br />

weeks. 4-Fluorothreonine was purified from batch cultures <strong>of</strong> S. cattleya by column chromatography.<br />

Another amino acid, 3-ethynylserine, copurified with the fluorocompound, and was also isolated. Several<br />

hypotheses for the biosynthesis <strong>of</strong> fluoroacetate and 4-fluorothreonine were investigated by feeding<br />

possible precursors and biosynthetic intermediates to resting cells. Only D- homoserine had a significant<br />

effect on the amounts and relative proportions <strong>of</strong> the metabolites formed, stimulating 4-fluorothreonine<br />

production by over 20%. Such studies also indicated that neither <strong>of</strong> the fluorometabolites produced is<br />

derived by metabolism <strong>of</strong> the other. The incorporation <strong>of</strong> $sp{14}$C-label into fluoroacetate from L-(U-<br />

$sp{14}$C) threonine by resting cells was in the range 1-3% and compared favourably with those from<br />

both (U-$sp{14}$C) glycerol and D-(U-$sp{14}$C) glucose. However, the highest incorporation from all<br />

the radiolabelled possible precursors examined was from (1,2-$sp{14}$C) glycolate, in the range 2-5%. It<br />

is concluded that the fluorinated secondary metabolites elaborated by S. cattleya are derived either by two<br />

entirely separate biosynthetic pathways, or from a common fluorinated intermediate. The most plausible<br />

hypothesis from present data involves 4-fluorothreonine formation from the phosphate ester <strong>of</strong> homoserine<br />

or threonine, mediated by pyridoxal phosphate. Twenty five other Streptomyces spp. were examined for<br />

their ability to incorporate inorganic fluoride into fluorometabolites. In over half the species examined, a<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

significant uptake <strong>of</strong> fluoride (0.2-0.3 mM) was observed, but no fluorometabolites were detected in culture<br />

supernatants by $sp{19}$F NMR spectroscopy<br />

Reid, K. A., Hamilton, J. T. G., Bwoden, R. D., O'Hagan, D., Dasaradhi, L., Amin, M. R., and Harper, D.<br />

B. (1995). Biosynthesis <strong>of</strong> fluorinated secondary metabolites by Streptomyces cattleya. Microbiology 141,<br />

1385-1393.<br />

Keywords: biosynthesis/bacteria/fluoroacetate/NMR/fluoride<br />

Abstract: The biosynthesis <strong>of</strong> organ<strong>of</strong>luorine compounds by Streptomyces cattleya NRRL 8057 was<br />

examined using 19 F NMR spectroscopy. The organsim produced 1.2 mM fluoroacetate and 0.5 mM 4fluorothreonine<br />

as secondary metabolites when cultured for 28 days on a chemically defined medium<br />

containing 2 mM fluoride.<br />

Reid, K. A., Bowden, R. D., and Harper, D. B. (1995). Biosynthesis <strong>of</strong> fluoroacetate and 4-fluorothreonine<br />

by Streptomyces cattleya. In 'Naturally-Produced Organohalogens: Selected and Edited Proceedings <strong>of</strong> the<br />

First Conference on Naturally-Produced Organohalogens'. (A. Grimvall and E. W. B. de LeerEds. ) pp.<br />

269-279. (Kluwer Academic:<br />

Keywords: biosynthesis/fluoroacetate/bacteria<br />

Reigart, J. R., Brueggerman, J. L., and Keil, J. E. (1975). Sodium fluoroacetate poisoning. American<br />

Journal <strong>of</strong> Diseases <strong>of</strong> Children 129, 1224-1226.<br />

Keywords: diagnosis/treatment/sodium fluoroacetate/humans<br />

Abstract: We observed a case <strong>of</strong> poisoning with sodium fluoroacetate, and extremely lethal rodenticide that<br />

has had relatively strict controls placed on its use. The case was unusual in the very long time the<br />

rodenticide had been present in the home, the mild nature <strong>of</strong> the poisoning, and the remarkably delayed<br />

onset <strong>of</strong> serious central nervous system symptoms. It demonstrates the need for even stronger control on<br />

the use <strong>of</strong> sodium fluoroacetate.<br />

Renschen, F. H., Klein, D., and Scholl, A. (1995). Trace analysis <strong>of</strong> airborne haloacetates. Journal <strong>of</strong> High<br />

Resolution Chromatography 18, 83-88.<br />

Keywords: analysis/mon<strong>of</strong>luoroacetate<br />

Abstract: Haloacetates in various environmental compartments can be determined by gas chromatographynegative-ion<br />

chemical-ionization mass spectrometry after derivatization with l-pentafluorophenyl<br />

diazoethane. Detection limits in absolute amounts per injection are between 0.01 fg (chlorodifluoroacetate)<br />

and 80 fg (mon<strong>of</strong>luoroacetate). Sampling <strong>of</strong> haloacetates in urban air was performed by means <strong>of</strong><br />

cylindrical denuders coated with alkalized glycerol. The haloacetates detected are trifluoro-, monochloro-,<br />

dichloro-, trichloro-, monobromo-, and dibromoacetate. The concentrations in ambient air fluctuate<br />

strongly, e.g. between 20 and 3000 pg/m(3) for TFA. Haloacetates are also found in river waters and tree<br />

foliage. A major problem is interference from contamination with trifluoro- and trichloroacetate<br />

Rick, R. (1989). Metabolic control <strong>of</strong> intracellular ion concentration in frog skin epithelium. Miner<br />

Electrolyte Metabolism 15, 150-154.<br />

Keywords: inhibition/metabolism/amphibian/fluoroacetate<br />

Abstract: The effects <strong>of</strong> the metabolic inhibitors 2-deoxy-d-glucose and mon<strong>of</strong>luoroacetate on intracellular<br />

ion concentrations and Na transport were investigated in the isolated frog skin epithelium <strong>of</strong> Rana pipiens.<br />

Ion concentrations were determined in thin freeze-dried cryosections using energy dispersive X-ray<br />

microanalysis. Metabolic inhibition was compared to direct inhibition <strong>of</strong> the Na pump by ouabain. At<br />

similar rates <strong>of</strong> transepithelial transport, inhibition <strong>of</strong> the Na pump always resutled in much more<br />

pronounced Na concentration increase than metabolic inhibition. The result suggests that the apical Na<br />

influx is under effective metabolic control. Downregulation <strong>of</strong> the Na influx during impaired cellular<br />

energy metabolism may eb a means by which transporting epithelial cells avoid potentially damaging<br />

derangements <strong>of</strong> intracellular ion compositon.<br />

Riess, C. M. and Flores, S. (1971). Pocket gopher pest species in Mexico cane areas. Proceedings <strong>of</strong> the<br />

International Society <strong>of</strong> Sugar Cane Technologists, 14th CongressUsing Smart <strong>Source</strong> Parsing 1972, 581<br />

583; 2 ref.<br />

Keywords: fumigant/sodium fluoroacetate/fluoroacetate/field efficacy/mammals<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Pocket gophers (<strong>of</strong> several genera), which live underground and construct extensive galleries in<br />

cane fields, damage more than 60,000 acres/year in the major cane producing regions <strong>of</strong> Mexico. Primitive<br />

control methods include trapping, shooting, extermination with CO2 and flooding <strong>of</strong> galleries. Commercial<br />

fumigants that have been or are currently in use include Cyanogas, methyl bromide and aluminium<br />

phosphide. The best and most economical control is obtained with pieces <strong>of</strong> cane soaked with sodium<br />

fluoroacetate and placed at gallery entrances<br />

Risbey, D. A., Calver, M., and Short, J. (1997). <strong>Control</strong> <strong>of</strong> feral cats for nature conservation. I. Field tests<br />

<strong>of</strong> four baiting methods. Wildlife research 24, 319-326.<br />

Keywords: cats/field efficacy<br />

Rist, R. J., Romero, I. A., and Abbott, N. J. (1995). Actions <strong>of</strong> fluorocitrate and 1,3-dinitrobenzene on brain<br />

endothelial cytoskeleton and permeability. Neurotoxicology 16, 558.<br />

Keywords: fluorocitrate/brain/metabolism/treatment<br />

Abstract: Experimental energy-deprivation syndromes are known to have toxic effects on brain astrocytes<br />

in vivo (Cavanagh, Toxicology, 49, 131-136, 1988). Some <strong>of</strong> these toxins are proposed to act on astrocytes<br />

alone (fluorocitrate) whilst others are associated with changes in the permeability <strong>of</strong> the BBB (1,3dinitrobenzene).<br />

Fluorocitrate has been shown to alter metabolism in glial cells and this is proposed to be<br />

its main site <strong>of</strong> action (Hassel et al., J Neurochem 62, 2187-2194, 1994). In contrast, 1,3-dinitrobenzene<br />

has been shown to alter BBB permeability in vivo (Romero et al., Neuropath Appl Neurobiol, 17, 495-508,<br />

1991). The RBE4 cell line (Durieu-Trautmann et al., J Cell Physiol, 155, 104-111, 1993) has proved to be<br />

a useful in vitro model <strong>of</strong> the BBB. It has been reported that a marginal F-actin distribution is required to<br />

maintain the tightness <strong>of</strong> the tight junctions in brain endothelial cells (Rubin et al., J Cell Biol, 115, 1725-<br />

1735, 1991). In this study, the effects <strong>of</strong> fluorocitrate and 1,3-dinitrobenzene on permeability <strong>of</strong> RBE4 cell<br />

monolayers grown on filters was measured and correlated with changes in the metabolism,and F-actin<br />

cytoskeleton in the cells. Treatment <strong>of</strong> RBE4 cells with fluorocitrate and 1,3-dinitrobenzene leads to a<br />

decrease in F-actin distribution at the cell margin and a reduction in the F-actin content <strong>of</strong> the cells at<br />

concentrations >0.5 mM. Fluorocitrate significantly reduced and 1,3-dinitrobenzene significantly increased<br />

the glucose consumption and lactate production <strong>of</strong> the RBE4 cells. Fluorocitrate (0.1 to 1 mM) had no<br />

significant effect on RBE4 cell monolayer permeability measured by FITC-dextran or 14C-sucrose.<br />

However, 1,3-dinitrobenzene (0.5 mM) significantly increased the permeability <strong>of</strong> RBE4 cell monolayers.<br />

These results show that whilst both fluorocitrate and 1,3-dinitrobenzene have significant effects on the<br />

RBE4 cell F-actin cytoskeleton and cellular metabolism, only 1,3-dinitrobenzene treatment produces<br />

increases in endothelial cell monolayer permeability. These data demonstrate that pr<strong>of</strong>ound toxic effects on<br />

endothelial cell structure and metabolism do not necessarily indicate changes in monolayer permeability.<br />

Robertson, H. A., Colbourne, R. M., Graham, P., Miller, P. J., and Pierce, R. J. (1999). Survival <strong>of</strong> brown<br />

kiwi exposed to 1080 poison used for control <strong>of</strong> brushtail possums in Northland, New Zealand. Wildlife<br />

research 26, 209-214.<br />

Keywords: non-target species/birds/1080/possums/secondary poisoning/invertebrates/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/carrot/poisoning<br />

Robinson, J. B., Inman, L., Sumegi, B., and Srere, P. A. (1987). Further characterization <strong>of</strong> the Krebs<br />

tricarboxylic acid cycle metabolon. The Journal <strong>of</strong> Biological Chemistry 262, 1786-1790.<br />

Keywords: metabolism/biochemistry/enzyme/inhibition<br />

Abstract: A preparation <strong>of</strong> gently disrupted rat liver mitochondria which shows exposed and easily<br />

sedimented Krebs tricarboxylic acid cycle enzyme activites has been characterised further. Results indicate<br />

that the Krebs tricarboxylic acid cycle exists as a sequential complex <strong>of</strong> enzymes, a metabolon, in situ.<br />

Robinson, M. H. and Wheeler, S. H. (1983). A radiotracking study <strong>of</strong> four poisoning techniques for control<br />

<strong>of</strong> the European rabbit, Oryctolagus cuniculus (L.). Aust.Wildl.Res. 10, 513-520.<br />

Keywords: poisoning/rabbits<br />

Abstract: Telemetry was used to determine the patterns <strong>of</strong> mortality <strong>of</strong> rabbits, Oryctolagus cuniculus (L.),<br />

day by day following laying <strong>of</strong> poisoned bait in the field. Four poisoning methods were studied:<br />

'conventional' 1080 (sodium mon<strong>of</strong>luoroacetate) in oat bait, 'conventional' 1080 in carrot bait, pindone (2-<br />

170


1080 Reassessment Application October 2006<br />

Appendix C<br />

pivalyl-1,3-indandione) in oat bait, and 'one-shot' 1080 (0.25%, 1%, and 4%) were compared. The relative<br />

merits <strong>of</strong> the various poisoning techniques are discussed.<br />

Robinson, R. F., Griffith, J. R., Wolowich, W. R., and Nahata, M. C. (2002). Intoxication with sodium<br />

mon<strong>of</strong>luoroacetate (compound 1080). Veterinary and human toxicology 44, 93-95.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/toxicity/humans<br />

Abstract: The highly toxic sodium mon<strong>of</strong>luoroacetate (SMFA) was banned as a rodenticide in the U.S. in<br />

1972. We report the first case <strong>of</strong> intentional ingestion in this country in over 15 y. A 47-y-old male was<br />

brought to the emergency room status post tonic clonic seizure. At 34 h post ingestion, he responded only<br />

to noxious stimuli and at 48 h, he was unresponsive to painful stimuli, was intubated and placed on a<br />

ventilator. Over the following 3 d, he was became minimally responsive to external stimuli with bouts <strong>of</strong><br />

agitation and hypertension. Two days later he was discharged with no evidence <strong>of</strong> neurologic sequelae. We<br />

report this patient to increase awareness <strong>of</strong> SMFA toxicity, and its ability to cause anion gap metabolic<br />

acidosis<br />

Robinson, W. B. (1953). Population trends <strong>of</strong> predators and fur animals in 1080 station areas. Journal <strong>of</strong><br />

Mammalogy 34, 220-227.<br />

Keywords: predators/1080/mammals/field efficacy/USA<br />

Abstract: Coyote populations have been greatly reduced during the past several years in many <strong>of</strong> the<br />

western states. Trapping data from seven localities in the plains and deserts <strong>of</strong> Wyoming, Colorado and<br />

New mexico suggest that in these areas where control has been vigorously conducted coyotes are now<br />

about one-fourth as numerous as they were a decade ago. predator control work by the Fish and Wildlife<br />

Service, particularly the employment <strong>of</strong> 1080 stations, has been largely responsible fort his reduction.<br />

During the same period, and in teh same areas, populations <strong>of</strong> bobcats, skunks, badgers and raccoons have<br />

greatly increased. This may be due, at least in part, to less commercial trapping. Some <strong>of</strong> these mammals<br />

have been accidentally poisoned or otherwise killed in control operations, but not in sufficent numbers to<br />

prevent sizable population increases.<br />

Robison, W. H. (1970). Acute toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate to cattle. Journal <strong>of</strong> wildlife<br />

management 34, 647-648.<br />

Keywords: acute toxicity/1080/livestock<br />

Abstract: The LD50's and 95 percent confidence limits for sodium mon<strong>of</strong>luoroacetate (1080) were 0.393<br />

(0.247-0.625) mg/kg for Hereford cows 0.221 (0.149-0.327) mg/kg for Hereford steer and heifer calves.<br />

This high susceptibility demonstrates the importance <strong>of</strong> using safe techniques when applying 1080 grain<br />

baits for rodent control.<br />

Rogers, G. Organ<strong>of</strong>luorine Compounds in Australian Native Plants and the Synthesis <strong>of</strong> Intermediate<br />

Fluorinated Metabolites. 1984. MonashEditor.<br />

Ref Type: Thesis/Dissertation<br />

Keywords: occurrence in nature<br />

Rogers, S. H. (1976). Schistosomatium douthitti: carbohydrate metabolism in the adults. Experimental<br />

Parasitology 40, 397-405.<br />

Keywords: metabolism/sodium fluoroacetate/fluoroacetate/cyanide/inhibition/citric acid/invertebrates<br />

Abstract: Investigation <strong>of</strong> pathways <strong>of</strong> carbohydrate metabolism showed that adult Schistosomatium<br />

douthitti appear to depend on glycolysis to a marked degree. The worms were also capable <strong>of</strong> aerobic<br />

metabolism. Histochemical studies demonstrated the existence <strong>of</strong> the TCA cycle and a cytochrome system.<br />

The presence or absence <strong>of</strong> glucose in the incubation medium had no effect on O2 consumption. Reduction<br />

<strong>of</strong> O2 tension had a severe effect on motility. Oxygen uptake was completely inhibited by tartar emetic and<br />

partially inhibited by sodium fluoroacetate and sodium cyanide. Inhibition by sodium fluoroacetate was<br />

partially counteracted by citric acid in the medium. Adults showed an oxygen debt following anaerobic<br />

incubation. A maximum <strong>of</strong> 52% <strong>of</strong> the glucose consumed under aerobic conditions was excreted as lactic<br />

acid. Under anaerobic conditions the amount <strong>of</strong> lactic acid increased. Acids other than lactic acid were also<br />

released. It is indicated that although glycolysis is the major pathway, 2 additional aerobic pathways also<br />

exist, one which is cyanide sensitive and the other cyanide insensitive<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Rognstad, R. (1986). Metabolic effects <strong>of</strong> mon<strong>of</strong>luoroacetate and difluoroacetate in rat hepatocytes.<br />

Biochemical archives 2, 121-126.<br />

Keywords: mon<strong>of</strong>luoroacetate/fluoroacetate/fluorocitrate/inhibition/aconitase/rodents/metabolism<br />

Abstract: At concentrations up to 2mM, fluoracetate stimulates gluconeogenesis from L-lactate, possibly by<br />

activating pyruvate dehydrogenase. At high concentrations, fluoroacetate becomes weakly inhibitory,<br />

probably because <strong>of</strong> fluorocitrate inhibition <strong>of</strong> mitochondrial aconitase. This inhibition becomes<br />

considerably more pronounced when NH-3 is present together with lactate. Difluoroacetate stimulates<br />

gluconeogenesis from lactate and increases pyruvate dehydrogenase flux<br />

Rokita, S. E., Srere, P. A., and Walsh, C. T. (1982). 3-fluoro-3-deoxycitrate: a probe for mechanistic study<br />

<strong>of</strong> citrate-utilizing enzymes. Biochemistry 21, 3765-3774.<br />

Keywords: enzyme/biochemistry/citrate<br />

Abstract: The interaction <strong>of</strong> a novel fluorinated analogue <strong>of</strong> citrate, 3-fluoro-3-deoxycitrate (3-fluorocitrate)<br />

with the four known citrate-processing enzymes is described in thsi report. Three <strong>of</strong> the citrate-processing<br />

enzymes, citrate syntahse, ATP citrate lyase and citrate lyase, catalyze reversible aldol-type condensations.<br />

The fate <strong>of</strong> 3-fluorcitrate with each enzyme is uniquely related to their mechanisms <strong>of</strong> action. For citrate<br />

synthase, 3-fluorocitrate is a competitive inhibitor. 3-fluorocitrate is a substrate for the carboxylate<br />

activation half-reaction catalyzed by ATP citrate lyase and induces a net ATPase action during conversion<br />

to 3-fluorocitryl-S-coenzyme A. Because <strong>of</strong> the unusual mechanism <strong>of</strong> citrate cleavage catalysed by<br />

bacterial citrate layse, 3-fluorocitrate is a mechanism-based inhibitor, acting at two points during turnover<br />

<strong>of</strong> the acetyl enzyme. The fourth citrate-processingenzyme, aconitase, does turn over 3-fluorocitrate<br />

catalytically. This enzyme, catalyzing a dehydration and rehydration <strong>of</strong> citrate, also catalyzes the<br />

elimination <strong>of</strong> HF from 3-fluorocitrate, yielding cis-aconitate and fluoride.<br />

Rokita, S. E. and Walsh, C. T. (1983). Turnover and inactivation <strong>of</strong> bacterial citrate lyase with 2fluorocitrate<br />

and 2-hydroxycitrate stereoiosmers. Biochemistry 22, 2821-2828.<br />

Keywords: citrate/biochemistry/enzyme/fluorocitrate<br />

Abstract: Bacterial citrate lyase catclytically cleaves the carbon skeleton <strong>of</strong> the naturally occurring<br />

fluorocvitrate isomer (-)-erythro-2-fluorocitrate (2R, 3R) with the same regiospecificty as with citrate<br />

cleavage.<br />

Ross, J. G., Hickling, G. J., and Morgan, D. R. Use <strong>of</strong> subacute and chronic toxicants to control sodium<br />

mon<strong>of</strong>luoroacetate (1080) bait shy possums. 397-400. 1997. Proceedings <strong>of</strong> 50th NZ Plant Protection<br />

Conference.<br />

Ref Type: Conference Proceeding<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/possums/field efficacy/bait shyness<br />

Ross, J. G., Hickling, G. J., Morgan, D. R., and Eason, C. T. (2000). The role <strong>of</strong> non-toxic prefeed and<br />

postfeed in the development and maintenance <strong>of</strong> 1080 bait shyness in captive brushtail possums. Wildlife<br />

research 27, 69-74.<br />

Keywords: field efficacy/possums/1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/aversion/bait<br />

shyness/efficacy<br />

Abstract: Shyness to sodium mon<strong>of</strong>luoroacetate (1080) in cereal bait can persist in sub-lethally poisoned<br />

possum (Trichosurus vulpecula) populations for at least 2 years. We investigated the use <strong>of</strong> non-toxic cereal<br />

'prefeed' and 'postfeed' as ways <strong>of</strong> inhibiting and overcoming such shyness. The postfeed result was also<br />

compared with changing to a non-cereal, gel-based 1080 bait. Prefeeding had a significant effect on the<br />

number <strong>of</strong> possums that became 'bait shy' following an approximate LD20 1080 dose, with 97% <strong>of</strong> nonprefed<br />

possums developing an aversion to 1080 cereal bait compared with only 22% <strong>of</strong> prefed possums. In<br />

contrast, postfeeding with cereal was relatively ineffective in reducing the number <strong>of</strong> 1080 bait-shy<br />

possums, with mortality <strong>of</strong> these possums being 30% compared with 0% <strong>of</strong> non-postfed possums. In<br />

contrast, the gel 1080 bait killed 64% <strong>of</strong> 1080 cereal bait-shy possums. These results suggest that 1080 bait<br />

shyness can be markedly reduced by prefeeding non-toxic bait to possums prior to each control operation.<br />

However, this may not be the most cost-effective control option, given the observed efficacy <strong>of</strong> follow-up<br />

baiting with 1080 gel.<br />

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Appendix C<br />

Ross, J. G. and Henderson, R. J. (2003). An improved 1080 paste for the control <strong>of</strong> possums. New Zealand<br />

Plant Protection 56, 66-70.<br />

Keywords: 1080/possums/bees/efficacy/treatment/New Zealand<br />

Abstract: A new 1080 paste (PTP) was developed by Pest-Tech Ltd. and then<br />

evaluated in a series <strong>of</strong> comparative trials with Pest<strong>of</strong>f possum paste (POP).<br />

The research indicated that PTP was significantly more palatable to captive<br />

possums than POP following 57 h <strong>of</strong> exposure to 'hot' conditions (hot<br />

conditions were 30°C for 6 h followed by 18 h at 13°C on a 24 h cycle).<br />

Acceptance by bees was low with significantly less PTP than POP removed<br />

by forager bees over a 30 h period. In the field, the control efficacy <strong>of</strong><br />

both pastes was high (89%-94% kill), with no significant differences<br />

between treatments. Based on these results, it is recommend that PTP is<br />

registered for possum control in New Zealand.<br />

Ross, W. D., Bell, J., and Robson, D. L. Preference and acceptability <strong>of</strong> commercially prepared cereal<br />

pellets and the effectiveness <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) on caged possums. MAF Qual <strong>Research</strong><br />

Project, 1-25. 1987. Lincoln, MAF Tech.<br />

Ref Type: Report<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/possums<br />

Abstract: RS5 most preferred bait; manipulating prefeeding and cinnamon conc.<br />

Ross, W. D. Vertebrate pest control using 1080: warnings for the future. 295-299. 1991. Adelaide.<br />

Ref Type: Conference Proceeding<br />

Keywords: 1080<br />

Roukas, T. and Kotzekidou, P. (1987). Influence <strong>of</strong> some trace metals and stimulants on citric acid<br />

production from brewery wastes by Aspergillus niger. Enzyme Microb.Technol. 9, 291-294.<br />

Keywords: citric acid/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate<br />

Abstract: The addition <strong>of</strong> increasing levels <strong>of</strong> Mn 2+ , Fe 3+ , Zn 2+ , Co 2+ , Cu 2+ , Ca 2+ , sodium mon<strong>of</strong>luoroacetate<br />

and methanol during citric acid surface fermentation <strong>of</strong> spent grain liquor by Aspergillus niger (ATCC<br />

9142) was investigated. For spent grain liquor the addition <strong>of</strong> 51 ppb Mn 2+ , 5 ppb Fe 3+ , 75 ppb Zn 2+ and<br />

4% (v/v) methanol caused a 4.9, 1.9, 10.9 and 16.8% increase in citric acid yield respectively. In all other<br />

fermentations the yield <strong>of</strong> citric acid was decreased whereas the biomass production in some cases was<br />

increased.<br />

Rowley, I (1958). Behaviour <strong>of</strong> a natural rabbit population poisoned with "1080". CSIRO wildlife research<br />

3, 32-39.<br />

Keywords: field efficacy/ground control/target species/rabbits<br />

Rowley, I (1960). The effect <strong>of</strong> concentration on the ingestion <strong>of</strong> "1080" poisoned baits by the rabbit.<br />

CSIRO wildlife research 5, 126-133.<br />

Keywords: field efficacy/target species/rabbits/baits<br />

Rowley, I (1963). Field enclosure experiments on the technique <strong>of</strong> poisoning the rabbit, Oryctolagus<br />

cuniculus (L.) : IV. A study <strong>of</strong> shyness in wild rabbits subjected to "1080" poisoning. CSIRO wildlife<br />

research 8, 142-153.<br />

Keywords: rabbits/field efficacy/ground control/poisoning/baits/bait shyness<br />

Rowley, I. (1963). The effect on rabbits <strong>of</strong> repeated sublethal doses <strong>of</strong> sodium fluoroacetate. CSIRO<br />

wildlife research 8, 52-55.<br />

Keywords: metabolism/mode <strong>of</strong> action/rabbits/sodium fluoroacetate<br />

Abstract: Caged wild rabbits Oryctolagus cuniculus (L), were fed sublethal doses <strong>of</strong> sodium fluoroacetate<br />

("1080") at different levels and at different intervals. Results show that in some circumstances "1080" can<br />

accumulate and cause death and that its elimination from the rabbit is a slow process.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Roy (Shapira), A., Taitelman, U., and Bursztein, S. (1980). Evaluation <strong>of</strong> the role <strong>of</strong> ionized calcium in<br />

sodium fluoroacetate (1080) poisoning. Toxicology and Applied Pharmacology 56, 216-220.<br />

Keywords: sodium<br />

fluoroacetate/fluoroacetate/1080/poisoning/pathology/treatment/metabolism/cats/fluorocitrate/enzyme/citra<br />

te<br />

Abstract: Fluoroacetate, which is an inhibitor <strong>of</strong> the tricarboxilic acid cycle, is widely used as a rodenticide.<br />

Fluoroacetate is converted in the body to fluorocitrate, which is an inhibitor <strong>of</strong> the enzyme aconitate<br />

hydrase. As a result, energy production goes down, and citrate accumulates. As citrate is a potent chelator<br />

<strong>of</strong> calcium ion, we postulate that ionized calcium concentration in the blood would drop. Fluoroacetate,<br />

0.03 mmol/kg, was injected iv into anesthetized cats. Ionized calcium concentration in anaerobically drawn<br />

arterial blood samples was measured with an ion-exchange electrode. Samples were taken immediately<br />

before and 40 min after poisoning, after which the animals were either used as controls (six cats) or treated<br />

with an infusion <strong>of</strong> iv CaCl2 (another 6 cats), so as to restore ionized calcium levels to normal values. Forty<br />

minutes after fluoroacetate injection, the ionized calcium levels fell by an average <strong>of</strong> 27.2%, from 1.09 + -<br />

0.07 to 0.79 + - 0.14 mM. There was a corresponding prolongation <strong>of</strong> the QTc interval <strong>of</strong> the ECG (r =<br />

0.82). Treatment with CaCl2 significantly prolonged the life <strong>of</strong> the treated animals as compared to the<br />

control animals (p


1080 Reassessment Application October 2006<br />

Appendix C<br />

the rate <strong>of</strong> 2kg/ha to prevent the forest from rat-injuries, it was investigated in the course <strong>of</strong> 5 months if the<br />

river water near the forest is contaminated by the rodenticide. Sodium fluoroacetate, however, was not<br />

detected at all in the river in this investigation.<br />

Saito, T. (1990). Glucose-supported oxidative metabolism and evoked potentials are sensitive to<br />

fluoroacetate, an inhibitor <strong>of</strong> glial tricarboxylic acid cycle in the olfactory cortex slice. Brain research 535,<br />

205-213.<br />

Keywords: fluoroacetate/metabolism/brain<br />

Abstract: When the slice <strong>of</strong> rat brain was perfused with a solution containing fluoroacetate (1 or 10 mM), a<br />

selective inhibitor <strong>of</strong> glial metabolism, cytochromes shifted to oxidized levels. The amplitude <strong>of</strong> evoked<br />

potentials tended to decline by a low dose (1 mM) and signficantly decreased by a high dose (10 mM) <strong>of</strong><br />

fluoroacetate. Oxygen consumption <strong>of</strong> the slice was dose-relatedly lowered by fluoroacetate.<br />

Saitou, E. (1984). Studies <strong>of</strong> the effects <strong>of</strong> fluoroacetate on ameloblasts in rat incisor. Bulletin <strong>of</strong> Tokyo<br />

Medical and Dental University 31, 33-50.<br />

Keywords: fluoroacetate/citrate/metabolism/plasma/blood/bone/pathology<br />

Abstract: The effects <strong>of</strong> fluoroacetate on ameloblasts were studied in the rat incisor. Fluoroacetate is an<br />

inhibitor <strong>of</strong> tricarboxylic acid cycle and accumulation <strong>of</strong> citrate occurred in the animal tissue due to<br />

fluoroacetate administration. Fluoroacetate injection caused severe morphologic changes in the<br />

ameloblasts. The most prominent change was observed in the mitochondria. Reduction <strong>of</strong> the mitochondrial<br />

matrix density was the earliest change followed by varying degrees <strong>of</strong> matrix swelling. Loss <strong>of</strong> the matrix<br />

granules and disintegration <strong>of</strong> the cristae were also observed. The difference in the mitochondrial activities<br />

in regard to the citrate metabolism was found between the matrix formation stage and the maturation stage<br />

in the ameloblasts. Extensive dilatation <strong>of</strong> the rough-surfaced endoplasmic reticulum and grossly enlarged<br />

vacuoles were found mainly in the early maturation stage at 12 and 24 h after fluoroacetate administration.<br />

These abnormally large vacuoles seemed to be caused by the water stored within the endoplasmic reticulum<br />

cisternae. Accumulation <strong>of</strong> plasma citrate and decrease <strong>of</strong> ionized Ca concentration in the whole blood<br />

were observed in the fluoroacetate treated group. Fluoroacetate may have caused the lowering <strong>of</strong> the<br />

function <strong>of</strong> the ameloblasts through the suppression <strong>of</strong> cell energy production. The secretion <strong>of</strong> the matrix<br />

and calcification <strong>of</strong> the enamel may have been inhibited<br />

Sample, B. E., Opresko, D. M., and Suter II, G. W. Toxicological Benchmarks for Wildlife: 1996 Revision.<br />

1996.<br />

Ref Type: Report<br />

Keywords: dermal/inhalation/risk assessment/soil/wildlife/regulatory toxicology<br />

Abstract: Executive Summary:<br />

The process <strong>of</strong> evaluating ecological risks <strong>of</strong> environmental contaminants comprises two tiers. The first<br />

tier is a screening assessment where concentrations <strong>of</strong> contaminants in the environment are compared to no<br />

observed adverse effects level (NOAEL)-based toxicological benchmarks that represent concentrations <strong>of</strong><br />

chemicals in environmental media (water, sediment, soil, food, etc.); these concentrations are presumed to<br />

be nonhazardous to the surrounding biota. The second tier is a baseline cosmological risk assessment<br />

where toxicological benchmarks are one <strong>of</strong> several lines <strong>of</strong> evidence used to support or refute the presence<br />

<strong>of</strong> ecological effects.<br />

This report presents NOAEL- and lowest observed adverse effects level (LOAEL)-based toxicological<br />

benchmarks for assessment <strong>of</strong> effects <strong>of</strong> 85 chemicals on 9 representative mammalian wildlife species or 11<br />

avian wildlife species. The chemicals are some <strong>of</strong> those that occur at U.S. Department <strong>of</strong> Energy waste<br />

sites; the wildlife species were chosen because they are widely distributed and provide a representative<br />

range <strong>of</strong> body sizes and diets. Further descriptions <strong>of</strong> the chosen wildlife species and chemicals are also<br />

provided in this report. The NOAEL-based benchmarks represent values believed to be nonhazardous for<br />

the listed wildlife species; LOAEL-based benchmarks represent threshold levels at which adverse effects<br />

are likely to become evident. These benchmarks consider contaminant exposure through oral ingestion <strong>of</strong><br />

contaminated media; however, exposure through inhalation and/or direct dermal exposure are not<br />

considered in this report.<br />

Sanada, M., Miyano, T., Iwadare, S., Williamson, J. M., Arison, B. H., Smith, J. L., Douglas, A. W.,<br />

Liesch, J. M., and Inamine, E. (1986). Biosynthesis <strong>of</strong> fluorothreonine and fluoroacetic acid by the<br />

175


1080 Reassessment Application October 2006<br />

Appendix C<br />

thienamycin producer, Streptomyces cattleya. Journal <strong>of</strong> Antibiotics (Tokyo) 39, 259-265.<br />

Keywords: biosynthesis/fluoride/NMR/fluoroacetate/bacteria<br />

Abstract: An antimetabolite, THX, was isolated from fermentation broths <strong>of</strong> the thienamycin producer,<br />

Streptomyces cattleya, when the organism was grown in the presence <strong>of</strong> a fluorine-containing substrate.<br />

THX was subsequently identified as one <strong>of</strong> the four possible stereoisomers <strong>of</strong> 4-fluorothreonine. Inorganic<br />

fluoride or any one <strong>of</strong> a number <strong>of</strong> organ<strong>of</strong>luorine compounds can be used as precursors <strong>of</strong> 4fluorothreonine.<br />

In addition, 19F NMR has provided evidence that the organism synthesizes fluoroacetate<br />

under the same fermentation conditions. The in vitro antibacterial spectrum <strong>of</strong> 4-fluorothreonine is also<br />

presented<br />

Saunders, B. C. (1947). Toxic properties <strong>of</strong> fluor-carboxylic acids and derivatives. Nature 4058, 179-181.<br />

Keywords: acute toxicity/product chemistry/fluoroacetate<br />

Saunders, G., Coman, B., Kinnear, J., and Braysher, M. (1995). Managing vertebrate pests: foxes.<br />

(Australian Government Publishing Service: Canberra, ACT; Australia.)<br />

Keywords: foxes/predators/sodium fluoroacetate/fluoroacetate/poisoning/rabbits/goats/pigs/rodents<br />

Abstract: The red fox (Vulpes vulpes) was introduced into Victoria in 1871, and subsequently spread to all<br />

parts <strong>of</strong> Australia except the tropical north and Tasmania. As predators, they are a threat to native species,<br />

such as rock wallabies, bettongs and numbats. Their biology is reviewed and strategic management <strong>of</strong> foxes<br />

at local and regional levels is discussed. Sodium fluoroacetate has been for poisoning foxes in Australia.<br />

For den fumigation, hydrogen phosphide is prefered to chloropicrin. Sensitive habitats have been protected<br />

by fox-pro<strong>of</strong> fencing. Recreational fox hunting, as practised in Australia, has had little effect on fox<br />

populations. Detailed information on the extent <strong>of</strong> predation by foxes, and the need for controlling them in<br />

specific areas is needed. Other publications in the "Managing vertebrate pests" series have dealt with feral<br />

horses, rabbits, feral goats, feral pigs and rodents<br />

Saunders, G., McLeod, S., and Kay, B. (2000). Degradation <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) in buried<br />

fox baits. Wildlife research 27, 129-135.<br />

Keywords: bait degradation/1080/treatment<br />

Savarie, P. J. (1984). Toxic characteristics <strong>of</strong> fluorocitrate, the toxic metabolite <strong>of</strong> compound 1080.<br />

Proceedings <strong>of</strong> the Vertebrate Pest Conference 11, 132-137.<br />

Keywords: non-target species/metabolism/mode <strong>of</strong> action/1080/fluorocitrate<br />

Abstract: This paper reviews toxicological research involving fluorocitrate, the toxic metabolite <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (fluorocetate), which is the active ingredient in the pesticide Compound 1080. Many<br />

toxicological studies have been done with fluoroacetate and the results obtained are actually due to the<br />

fluorocitrate because it has been definitely proved that, from a biochemical perspective, fluoroacetate is not<br />

toxic but fluorocitrate is. The classical explanation <strong>of</strong> the toxic action <strong>of</strong> fluorocitrate is that it inhibits the<br />

enzyme aconitase in the tricarboxylic acid cycle. Deactivation <strong>of</strong> aconitase results in decreased energy<br />

production by cells and ultimately death <strong>of</strong> the organism. However, the more recent explanation <strong>of</strong><br />

fluorocitrate's mode <strong>of</strong> action is that it binds with mito-chondrial protein with prevents transport <strong>of</strong> citrate<br />

and its utilization by cells for energy production. metabolism studies indicate that only small amounts,<br />

perhaps less than 3% <strong>of</strong> fluorocitrate is formed from fluoroacetate. From the limited number <strong>of</strong> acute and<br />

chronic studies conducted with fluorocitrate it does not appear to be as potent as fluoroacetate by either the<br />

oral or parenteral routes <strong>of</strong> administration. This decreased level <strong>of</strong> toxicity is though to be due to the larger<br />

molecular weight <strong>of</strong> fluorocitrate which would not be as readily absorbed by tissues. Central nervous<br />

system toxic manifestations (i.e., tremors, convulsions) are characteristic in animals poisoned with<br />

fluoroacetate. Fluorocitrate administered directly into the brain was found to be 100 times more toxic than<br />

fluoroacetate. The accumulation <strong>of</strong> citrate in organs is characteristic <strong>of</strong> fluorocitrate poisoning; from a<br />

quantitative point <strong>of</strong> view the liver is less affected than the brain, heart, kidney, or spleen. Fluorocitrate<br />

causes extensive kidney damage, but the tests are most sensitive to sublethal doses. Testicular damage may<br />

be either reversible or irreversible, depending upon the dose. Several plants have the ability to metabolize<br />

both fluoroacetate and fluorocitrate from either inorganic or atmospheric fluoride.<br />

Savarie, P. J. and Schafer, Jr. Biodeterioration <strong>of</strong> warfarin, sodium mon<strong>of</strong>luoroacetate (1080), 4aminopyridine<br />

and 3-chloro-4-methylbenzenamine in terrestrial vertebrate pests. Barry, S. and Houghton,<br />

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Appendix C<br />

D. R. Biodeterioration 6. Papers presented at the 6th International Biodeterioration Symposium,<br />

Washington, DC, August 1984. 66-73. 1986. Slough, CAB International.<br />

Ref Type: Conference Proceeding<br />

Keywords: persistence in animals/secondary poisoning/metabolism/sodium<br />

mon<strong>of</strong>luoroacetate/1080/warfarin/predators/fluorocitrate<br />

Abstract: Warfarin, an antocoagulant rodenticide, is a racemic mixture <strong>of</strong> two isomers, R-warfarin and Swarfarin.<br />

Metabolites <strong>of</strong> warfarin are 6-, 7-, 8- and 4'-hydroxywarfarin. The major metabolic product <strong>of</strong> Rwarfarin<br />

os 7-hydroxywarfarin and the major metabolic products <strong>of</strong> S-warfarin are 7- and 4'hydroxywarfarin.<br />

The latter possesses one-fourth the anticoagulant activity <strong>of</strong> warfarin but the other<br />

metabolites are inactive. Scavenging mammalian predators can be poisoned by consuming animals killed<br />

by warfarin. Tissue residues <strong>of</strong> 1080, an acute rodenticide and predacide, can also poison mammalian<br />

predators although less than 3% <strong>of</strong> 1080 is converted to the toxic metabolite, fluorocitrate. The major<br />

unidentified metabolite <strong>of</strong> 1080 is nontoxic. 1080 is also metabolised into amino acids, fatty acids and<br />

cholesterol.<br />

Savarie, P. J., Matschke, G. H., Engeman, R. M., and Fagerstone, K. A. Susceptibility <strong>of</strong> prarie dogs to<br />

Compound 1080 (sodium mon<strong>of</strong>luoroacetate) baits and secondary poisoning effects in European ferrets<br />

under laboratory conditions. Seawright, A. A. and Eason, C. T. 28, 134-143. 1994. Christchurch, New<br />

Zealand, <strong>Royal</strong> Society Of New Zealand Miscellaneous Series. Proceedings <strong>of</strong> the Science Workshop on<br />

1080. 12-12-1993.<br />

Ref Type: Conference Proceeding<br />

Keywords: dogs/1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/secondary<br />

poisoning/poisoning/ferrets<br />

Saxty, B. A., Novelli, R., Dolle, R. E., Kruse, L. I, Reid, D. G., Camilleri, P., and Wells, T. N. (1992).<br />

Synthesis and evaluation <strong>of</strong> (+) and (-)-2,2-difluorocitrate as inhibitors <strong>of</strong> rat liver ATP-citrate lyase and<br />

porcine heart aconitase. European Journal <strong>of</strong> Biochemistry 202, 889-896.<br />

Keywords: liver/heart/aconitase/biochemistry/fluorocitrate<br />

Sayama, K. and Brunetti, O. (1952). The effects <strong>of</strong> sodium fluoroacetate (1080) on California quail.<br />

California Fish and Game 38, 295-300.<br />

Keywords: fluoroacetate/1080/sodium fluoroacetate/birds/lethal<br />

dose/heart/liver/poisoning/brain/kidney/pathology/diagnosis/symptoms<br />

Abstract: Sodium fluoroacetate is extremely toxic to California quail. Although insufficient birds were<br />

available to make an accurate determination <strong>of</strong> the minimum lethal dose, it was found to lie between 1 and<br />

5 mg/kg <strong>of</strong> body weight. Death due to a minimal lethal dose <strong>of</strong> sodium fluoroacetate occurs in about three<br />

hours in California quail. The birds first become inactive, standing stationary with fluffed wings and finally<br />

assuming a prone position in a comatose state. Death is preceded by a convulsive fluttering <strong>of</strong> the tail<br />

feathers <strong>of</strong> several seconds' duration. Upon autopsy, the only obvious gross pathological changes are<br />

hyperemia <strong>of</strong> the heart and liver, with extreme fragility <strong>of</strong> the liver. The general histopathological picture <strong>of</strong><br />

sodium fluoroacetate poisoning in quail is hyperemia <strong>of</strong> the brain, liver, lungs, heart and kidney. The heart<br />

is further characterised by fatty infiltration and focal areas <strong>of</strong> interstitial hemorrhages and the liver by<br />

sinusoidal engorgement and severe diffuse fatty degeneration. Although pathological changes were<br />

produced in quail by sodium fluoroacetate, the lack <strong>of</strong> specificity precludes pathology as a means <strong>of</strong><br />

diagnosis for 1080 poisoning.<br />

Schaefer, H. and Machleidt, H. (1971). Conversion <strong>of</strong> fluoroacetic acid to amino acids in the mammal.<br />

Biochimica et biophysica acta 252, 83-91.<br />

Keywords: metabolism/mammals/mode <strong>of</strong> action/rabbits/fluorocitrate/fluoroacetate/persistence in<br />

animals/rodents/pigs<br />

Abstract: When living mice were poisoned with (2-14C) fluoroacetic acid, no detectable amounts <strong>of</strong><br />

fluorocitric acid were found in the organism. Similarly, no fluorocitric acid was found in homogenates <strong>of</strong><br />

organs <strong>of</strong> rats, guinea pigs, rabbits and pigs after incubation, with radioactive fluoroacetic acid. However,<br />

several amino acids were formed, as can be shown by electrophoresis followed by identification reactions.<br />

Two <strong>of</strong> these are acidic amino acids and behave similarly to fluorocitric acid in paper chromatography.<br />

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Appendix C<br />

When pig liver in incubated with unlabelled fluorocitric acid, the information <strong>of</strong> an amino acid can be<br />

demonstrated by a single electrophoresis. I mg <strong>of</strong> this amino acid was purified and contained 9.3% fluorine.<br />

Schardein, J. L. (1993). Miscellaneous Pesticides. In 'Chemically induced birth defects'. pp. 704-709.<br />

(Marcel Dekker, Inc.: New York.)<br />

Keywords: teratogenicity/1080<br />

Schitoskey, F. Jr. (1975). Primary and secondary hazards <strong>of</strong> three rodenticides to kit fox. Journal <strong>of</strong> wildlife<br />

management 39, 416-418.<br />

Keywords: foxes/secondary poisoning/persistence in animals/USA/1080/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/strychnine/zinc phosphide/rats/predators<br />

Abstract: Acute oral LD50s to the kit fox (Vulpes macrotis) were determined to be 0.22 mg/kg for<br />

compound 1080 (sodium mon<strong>of</strong>luoroacetate), 0.75 mg/kg for strychnine alkaloid and 93 mg/kg for zinc<br />

phosphide. One fox died within hours when fed a kangaroo rat (Dipodomys spp.) killed by 0.74 mg <strong>of</strong> 1080<br />

or 12.8 mg <strong>of</strong> strychnine, amounts one rat might consume in field baiting programs. However, foxes<br />

survived repreated feedings <strong>of</strong> kangaroo rats each killed by 480 mg <strong>of</strong> zinc phosphide, equivalent to 3 times<br />

the LD50 for a fox and some 29 times the amount one rat might consume in bait.<br />

Schnautz, J. O. (1949). Sodium fluoroacetate (Compound 1080) poisoning in cattle. Journal <strong>of</strong> the<br />

American Veterinary Medical Association 114, 435.<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080/poisoning/symptoms/herbivores/convulsions/livestock<br />

Abstract: This is a report <strong>of</strong> losses apparently due to a new product, about which little information is<br />

available concerning it's toxicity to farm animals. The following observations in cattle are similar to those<br />

reported in sheep.<br />

Schultz, R. A., Coetzer, J. A. W., Kellerman, T. S., and Naudé, T. W. (1982). Observations on the clinical,<br />

cardiac and histopathological effects <strong>of</strong> fluoroacetate in sheep. Onderstepoort journal <strong>of</strong> veterinary<br />

research 49, 237-245.<br />

Keywords: acute toxicity/heart/mammals/non-target species/pathology<br />

Abstract: Fluoroacetate was dosed per stomach tube to 17 Merino sheep at the rate <strong>of</strong> 0,05 - 1,0 mg/kg/day.<br />

The clinical signs, haemodynamic changes, chemical pathology and pathology <strong>of</strong> acute, subacute and<br />

chronically intoxicated cases are described.<br />

Tetanic convulsions were seen in acutely intoxicated animals and in them respiratory failure, occurring<br />

concomitantly with cardic failure, may have been the cause <strong>of</strong> death. Subacute intoxication resulted in less<br />

conspicuous clinical signs when the sheep were at rest, but they developed apparent nervous signs <strong>of</strong> being<br />

handled, and later tended to lie down. Chronically intoxicated animals were only mildly affected.<br />

At levels <strong>of</strong> intoxication changes in the chemical pathological parameters were wither absent or were mild<br />

and transient.<br />

The microscopic lesions in the hearts <strong>of</strong> acutely intoxicated sheep included degeneration as well as necrosis<br />

<strong>of</strong> individual or small groups <strong>of</strong> myocardial fibers. In the subacutely and chronically intoxicated animals<br />

the multifocal myocardial lesions were more widespread and in various stages <strong>of</strong> development or<br />

resolution.<br />

Schulz, S. and Conrad, R. (1996). Influence <strong>of</strong> temperature on pathways to methane production in the<br />

permanently cold pr<strong>of</strong>undal sediment <strong>of</strong> Lake Constance. FEMS Microbiology Ecology 20, 1-14.<br />

Keywords: temperature/bacteria/fluoroacetate/inhibition<br />

Abstract: The in situ temperature <strong>of</strong> the pr<strong>of</strong>undal sediment <strong>of</strong> Lake Constance is constant at 4 o C.<br />

Methanogenic bacteria could not be detected at 6 o C by the most probable number technique using acetate<br />

and H2/CO2 as methanogenic substrates. Instead homoacetogenic bacteria were detected on H2/CO2. At a<br />

higher temperature <strong>of</strong> 20 o C however methanogenic bacteria were found. However CH4 production was<br />

observed at both 4 o C and 20 o C. production <strong>of</strong> CH4 was inhibited by chlor<strong>of</strong>orm and fluoroacetate and the<br />

accumulation <strong>of</strong> intermediary metabolites was measured.<br />

Schwarte, L. H. (1947). The toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) for swine and chickens. Journal<br />

<strong>of</strong> the American Veterinary Medical Association October 1947, 301-303.<br />

Keywords: mon<strong>of</strong>luoroacetate/1080/pigs/birds/acute toxicity/symptoms/poisoning/lethal dose/chronic<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

poisoning<br />

Abstract: The toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate has been determined for swine and chickens. The<br />

characteritic symptoms and lesions have been described for both species. Swine are particularly susceptible<br />

to poisoning by this agent. The minimum lethal dose is much less than that reported for the common<br />

Norway rat or the horse. Chickens can tolerate slightly larger doses than swine and are slightly more<br />

resistant to this type <strong>of</strong> poisoning than the common rat or the horse. Repeated sublethal doses to chickens<br />

show its cumulative effects.<br />

Seawright, A. A., Eason, C. T., and eds. (1994). Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14<br />

December 1993, Christchurch, New Zealand. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: acute toxicity/aerial control/aquatic species/bait degradation/birds/cats/deer/diagnosis/field<br />

efficacy/ground control/invertebrates/mammals/metabolism/mode <strong>of</strong> action/non-target species/occurrence<br />

in nature/pathology/persistence in animals/persistence in plants/persistence in soil/persistence in<br />

water/possums/product chemistry/rabbits/regulatory toxicology/secondary poisoning/target<br />

species/treatment/welfare/1080<br />

Abstract: This workshop was convened by the <strong>Royal</strong> Society <strong>of</strong> New Zealand in conjunction with Manaaki<br />

Whenua - <strong>Landcare</strong> <strong>Research</strong>. It brought together 70 scientists and other delegates from wildlife<br />

management, animal welfare, and conservation backgrounds from Australia, south Africa, the United<br />

States, and New Zealand. The purpose <strong>of</strong> the workshop was to review and discuss historical and recent<br />

research findings, and to identify gaps in our present knowledge. The need for substantial scientific data to<br />

provide the foundation for resolving conflicts beteween 1080 use for environmental protection, and<br />

terrestrial wildlife and human resource values was recognised as the principal issue <strong>of</strong> the meeting.<br />

[Note : Many <strong>of</strong> the papers from the workshop are indexed separately.]<br />

Seawright, A. A. (1994). The environmental toxicology <strong>of</strong> 1080 - key points revisited. In 'Proceedings <strong>of</strong><br />

the Science Workshop on 1080. 12-14 December 1993. Christchurch, New Zealand.'. (A. A. Seawright<br />

and C. T. EasonEds. ) pp. 166-167. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: 1080/birds/deer/degradation/goats/mammals/possums/soil<br />

Abstract: As frequently happened with European colonisation <strong>of</strong> so-called "new lands", the introduction<br />

<strong>of</strong> both domestic and wild mammals into New Zealand in the recent century left a legacy <strong>of</strong> problems for<br />

the attention <strong>of</strong> the contemporary human population.<br />

We have seen in the foregoing papers in these proceedings that the problems referred to have their<br />

genesis in the burgeoning populations <strong>of</strong> mainly the Australian brushtail possum and the European rabbit.<br />

A principal effect <strong>of</strong> the possums is extensive degradation <strong>of</strong> the natural forests in which they have become<br />

established. This has resulted specifically in loss <strong>of</strong> habitat for native animals and birds, and possums<br />

along with other introduced mammals such as goats and deer will have contributed to land slips on steep<br />

slopes and soil erosion. In addition, the possums have caused damage to pasture crops, pine plantations,<br />

and vegetation established to prevent soil erosion. To varying degrees an estimated 92% <strong>of</strong> the land mass<br />

<strong>of</strong> New Zealand is being affected by possums on one way or another.<br />

An issue <strong>of</strong> equal if not greater concern is the high level <strong>of</strong> infection <strong>of</strong> the possums in some areas with<br />

bovine tuberculosis. apart from its obvious significance as an animal health problem on farms bordering on<br />

the affected forest areas, the concern about bovine tuberculosis infection in the possum is that the<br />

discharges due to the disease contain large numbers <strong>of</strong> the micro-organisms. This maximises the<br />

opportunity for infection <strong>of</strong> in-contact, susceptible animals and poses a significant public health problem.<br />

Seigler, D. S. (2003). Phytochemistry <strong>of</strong> Acacia - sensu lato. Biochemical Systematics and Ecology 31,<br />

845-873.<br />

Keywords: occurrence in nature/chemistry/fluoroacetate<br />

Abstract: Little is known about the chemistry <strong>of</strong> most species <strong>of</strong> the genus Acacia, although the genus is<br />

quite large and widespread in the warm subarid and and portions <strong>of</strong> the world. As presently defined, Acacia<br />

is a cosmopolitan genus containing in excess <strong>of</strong> 1350 species. Taxonomic relationships and identification <strong>of</strong><br />

Acacia species are difficult; new studies <strong>of</strong> the genus confirm that Acacia is an agglomeration <strong>of</strong> at least<br />

five discrete groups. The major elements <strong>of</strong> this 'genus' are the groups now recognized as the subgenus<br />

Acacia, the genus Faidherbia, the subgenus 'Aculeiferum', relatives <strong>of</strong> Acacia coulteri, Bentham's series<br />

Filicinae, the subgenus Phyllodineae, and possibly others, each with somewhat distinct chemistry. A<br />

number <strong>of</strong> secondary metabolites have been reported from various Acacia species including amines and<br />

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Appendix C<br />

alkaloids, cyanogenic glycosides, cyclitols, fatty acids and seed oils, fluoroacetate, gums, nonprotein amino<br />

acids, terpenes (including essential oils, diterpenes, phytosterol and triterpene genins and saponins),<br />

hydrolyzable tannins, flavonoids and condensed tannins. The most evident and best known are<br />

polysaccharides (gums) and complex phenolic substances (condensed tannins).<br />

Shapira, A. R., Taitelman, U., and Bursztein, S. (1980). Evaluation <strong>of</strong> the role <strong>of</strong> ionized calcium in sodium<br />

fluoroacetate ("1080") poisoning. Toxicology and Applied Pharmacology 56, 216-220.<br />

Keywords: sodium<br />

fluoroacetate/fluoroacetate/poisoning/fluorocitrate/aconitate/citrate/blood/cats/treatment/biochemistry<br />

Abstract: Fluoroacetate, which is an inhibitor <strong>of</strong> the tricarboxylic acid cycle, is widely used as a<br />

rodenticide. In the body fluoroacetate is converted to fluorocitrate, which is an inhibitor <strong>of</strong> aconitate<br />

hydrase. Energy production decreases and citrate accumulates. As citrate is a potent chelator <strong>of</strong> Ca-2+ the<br />

drop in Ca-2+ concentration in the blood was studied. Fluoroacetate, 0.03 mmol/kg, was injected i.v. into<br />

anesthetized cats. Ca-2+ concentration in anaerobically drawn arterial blood samples was measured with an<br />

ion-exchange electrode. Samples were taken immediately before and 40 min after poisoning. The animals<br />

were then used as controls (6) or treated with an infusion <strong>of</strong> i.v. CaCl-2 (6) to restore Ca-2+ levels to<br />

normal values. After fluoroacetate injection (40 min), Ca-2+ levels fell by an average <strong>of</strong> 27.2%, from 1.09<br />

+- 0.07 to 0.79 +- 0.14 mM. There was a corresponding prolongation <strong>of</strong> QTc interval <strong>of</strong> the ECG (r = 0.82).<br />

Treatment with CaCl-2 significantly prolonged life <strong>of</strong> treated animals compared to control animals (P lt<br />

0.0016 by the Mann-Whitney rank sum test). Reduced levels <strong>of</strong> Ca-2+ apparently play an important role in<br />

the pathogenesis <strong>of</strong> fluoroacetate poisoning. Reduced levels <strong>of</strong> Ca-2+ explain the toxic effects <strong>of</strong><br />

fluoroacetate and may be the missing link between biochemistry <strong>of</strong> poisoning and clinical manifestations<br />

Sherley, G., Wakelin, M., and McCartney, J. (1999). Forest invertebrates found on baits used in pest<br />

mammal control and the impact <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) on their numbers at Ohakune, North<br />

Island, New Zealand. New Zealand journal <strong>of</strong> zoology 26, 279-302.<br />

Keywords: non-target species/invertebrates/1080/mammals<br />

Sherley, M. (2004). The traditional categories <strong>of</strong> fluoroacetate poisoning signs and symptoms belie<br />

substantial underlying similarities. Toxicology letters 151, 399-406.<br />

Keywords: fluoroacetate/poisoning/symptoms/sodium<br />

mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/pest/lethal dose/cardiac<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (Compound 1080) has been widely used around the world as a<br />

vertebrate pest control agent. Following ingestion <strong>of</strong> 1080 there is a latent period, during which the<br />

compound is metabolised into a toxic form, before the onset <strong>of</strong> symptoms. The timing <strong>of</strong> this period varies<br />

significantly between species as does the median lethal dose. Traditionally different species have also been<br />

classified into groups depending on the primary organ system involved in 1080 toxicosis (cardiac, nervous,<br />

or mixed signs/symptoms). However, general acceptance <strong>of</strong> this method <strong>of</strong> classification has obscured the<br />

fact that several signs <strong>of</strong> fluoroacetate poisoning are common to most vertebrate species. This paper<br />

reviews five decades <strong>of</strong> literature on the signs/symptoms <strong>of</strong> fluoroacetate poisoning in vertebrates and<br />

concludes that there is little justification for the division <strong>of</strong> animals poisoned by fluoroacetate into<br />

symptomatic groups.<br />

Shinoda, K., Mitsumori, K., Uneyama, C., and Uehara, M. (2000). Induction and inhibition <strong>of</strong> testicular<br />

germ cell apoptosis by fluoroacetate in rats. Archives <strong>of</strong> toxicology 74, 33-39.<br />

Keywords: pathology/fluoroacetate/aconitase/rats/reproductive effects/testes<br />

Abstract: Fluoroacetate (FA), an inhibitor <strong>of</strong> aconitase, is known to lower the intracellular level <strong>of</strong><br />

adenosine triphosphate (ATP), which recently has been suggested to be a possible determinant <strong>of</strong> the form<br />

<strong>of</strong> cell death, apoptosis or necrosis. To investigate which form <strong>of</strong> germ cell death occurs in FR-induced<br />

testicular toxicity, adult Sprague Dawley rats were given a single oral dose <strong>of</strong> FA (0.5 or 1.0 mg/kg) and<br />

euthanized at 3, 6, 12, 24, 48, and 72 h thereafter. Germ cell degeneration was histologically first found in<br />

early round spermatids at stage I and in spermatogonia at stages II-IV <strong>of</strong> seminiferous tubules 6 and 12 h,<br />

respectively, after dosing. Degenerating spermatogonia exhibited characteristic features <strong>of</strong> apoptosis as<br />

demonstrated by both electron microscopy and in situ terminal deoxynucleotidyl transferase-mediated<br />

dUTP nick end labeling (TUNEL), whereas spermatids did trot. At the 24 and 48 h time points,<br />

degenerating spermatids were continually present and subsequently formed multinucleated giant cells,<br />

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Appendix C<br />

while the number <strong>of</strong> degenerating spermatogonia and TUNEL-labeled spermatogonia was drastically<br />

and/or significantly decreased compared to those from the control group, indicating that spontaneous male<br />

germ cell apoptosis is inhibited. Coincident with these morphological changes, DNA laddering on gel<br />

electrophoresis was apparent only 12 h after dosing. The results demonstrate that FA induces either<br />

apoptosis or necrosis <strong>of</strong> male germ cells in the early stage after dosing and subsequently inhibits<br />

spontaneous apoptosis.<br />

Shlosberg, A. and Egyed, M. N. (1975). Fluoroacetamide (1081) poisoning in wild birds. Journal <strong>of</strong><br />

Wildlife Diseases 11, 534-536.<br />

Keywords: fluoroacetamide/1081/poisoning/birds<br />

Abstract: An outbreak <strong>of</strong> poisoning in four greylag geese (Anser anser) and 35-45 teal (Anas crecca ) is<br />

described. Laboratory findings led to the conclusion that a wheat bait containing the rodenticide<br />

fluoroacetamide (1081) caused the poisoning. Circumstantial evidence incriminated fluoroacetamide as the<br />

cause <strong>of</strong> death in white-fronted geese (Anser albifrons), mallards (Amas platyrhynchos), and chukars<br />

(Alectoris chukar).<br />

Shlosberg, A. and Booth, L. H. Veterinary and Clinical Treatment <strong>of</strong> Vertebrate Pesticide Poisoning - a<br />

Technical Review. -101. 2004. <strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Report<br />

Keywords: treatment/poisoning/<strong>poisons</strong>/poison/mammals/pest/New<br />

Zealand/1080/baits/brodifacoum/rodent/non-target species<br />

Abstract: The focus <strong>of</strong> this review is on the treatment <strong>of</strong> toxicoses caused by <strong>poisons</strong> used for the control <strong>of</strong><br />

introduced mammals that are considered pests in New Zealand (NZ). Intensive measures have been<br />

devised, and implemented widely in NZ, to control a variety <strong>of</strong> introduced mammalian pests. These<br />

include, for example, aerial application <strong>of</strong> 1080 bait for possum control on mainland NZ, and also <strong>of</strong> baits<br />

containing brodifacoum for rodent eradication on <strong>of</strong>fshore islands. Such necessary measures are amongst<br />

the most comprehensive and aggressive taken worldwide to control introduced mammals, and the<br />

subsequent results have proved their worth. The risk to non-target species will be determined by the<br />

intrinsic susceptibility <strong>of</strong> the various species, the properties <strong>of</strong> the toxicants used (such as their<br />

toxicokinetics), the bait formulation, and the way in which toxic baits are used in the field, which may<br />

preclude, limit or increase the exposure <strong>of</strong> non-target species. This technical manual documents in detail<br />

the properties <strong>of</strong> the various <strong>poisons</strong> relevant to risk <strong>of</strong> accidental poisoning. All toxicants have advantages<br />

and disadvantages, which make them more or less effective or appropriate for different use patterns. A<br />

large database <strong>of</strong> global literature has been compiled on these compounds, which has been complemented<br />

by NZ-based research. Much <strong>of</strong> the information (and the basis <strong>of</strong> this work) was detailed (with full<br />

references) in the Department <strong>of</strong> Conservation Technical Series guide "Vertebrate Pesticide Toxicology<br />

Manual (Poisons)" (2001).<br />

Short, J., Turner, B., Risbey, D. A., and Carnamah, R. (1997). <strong>Control</strong> <strong>of</strong> feral cats for nature conservation.<br />

II Population reduction by poisoning. Wildlife research 24, 703-714.<br />

Keywords: cats/poisoning/mammals/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/baits/field<br />

efficacy<br />

Abstract: A feral cat popualtion was substantially reduced by poisoning at a semi-arid site in Western<br />

Australia. The control programme was designed to protect twos pecies <strong>of</strong> endangered native mammals that<br />

had recently been reintroduced to the site. Feral cats were poisoned with the carcasses <strong>of</strong> laboratory mice,<br />

each impregnated with with 4.5 mg <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080). Baits were placed at 100-m<br />

intervals along the track system each night for four nights. Kill rates were assessed by monitoring survival<br />

<strong>of</strong> radio-collared cats and by spotlight counts <strong>of</strong> cats before and after baiting. All radio-collared cats were<br />

killed and there was a 74% reduction in spotlight counts <strong>of</strong> cats after baiting. Bait removal varied with the<br />

abundance <strong>of</strong> rabbits, the primary prey item for cats in this area. Effectiveness <strong>of</strong> control operations against<br />

feral cats is maximised by baiting at times <strong>of</strong> low prey abundance. Monitoring the changing abundance <strong>of</strong><br />

the primary prey species provide important information for timing contraol operations against feral cats.<br />

Sibbison, S. EPA and the politics <strong>of</strong> poison: the 1080 story. Defenders 59, 4-15. 1984.<br />

Ref Type: Magazine Article<br />

Keywords: 1080/USA<br />

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Appendix C<br />

Sikorski, M., Dmochowski, A., and Safian, E. (1992). [Accidental fatal poisoning with ethyl fluoroacetate].<br />

Pol.Tyg.Lek. 47, 317-319.<br />

Keywords:<br />

poisoning/fluoroacetate/diagnosis/symptoms/metabolism/citrate/CNS/monoacetin/inhalation/humans<br />

Abstract: Fluoroacetic salts belong to the most toxic chemicals. They are used for various purposes, and<br />

form stable compounds in some plants. A case <strong>of</strong> poisoning with ethyl fluoroacetate is presented in detail.<br />

Diagnostic problems and therapy which failed due to the late diagnosis and dramatic progress in the<br />

symptoms <strong>of</strong> poisoning are also discussed. Fluoroacetic ion alone is non-toxic but in vivo forms<br />

fluorotricarboxylic acid, which blocks cellular metabolism at the citrate stage. Symptoms occur with a<br />

delay but lethal synthesis <strong>of</strong> fluorotricarboxylic acid leads to the irreversible cellular dysfunction, especially<br />

in CNS and circulatory system. Poisoning may be treated with monoacetin and acetamide. An emphasis is<br />

on health hazards resulting from the exposure to fluoroacetate and necessity to observe strictly safety<br />

regulations<br />

Sikulova, J. and Novak, L. (1970). Body temperature as an indicator <strong>of</strong> the radioprotective effect <strong>of</strong> sodium<br />

fluoroacetate in mice. International journal <strong>of</strong> radiation biology 17, 587-590.<br />

Keywords: metabolism/sodium fluoroacetate/fluoroacetate<br />

Simpson, D. P. (1983). Citrate excretion: a window on renal metabolism. American journal <strong>of</strong> physiology<br />

244, F223-F234.<br />

Keywords: citrate/metabolism/citric acid/inhibition/fluorocitrate/biochemistry<br />

Abstract: The rate <strong>of</strong> intracellular metabolism <strong>of</strong> citrate plays a major role in determining the amount <strong>of</strong><br />

citrate excreted in the urine.Fractional excretion <strong>of</strong> citrate can be increased eitehr by increasing intracellular<br />

citrate synthesis from precursors or by inhibiting mitochondrial citrate metabolism. Increased excrteion<br />

secondary to incraesed synthesis <strong>of</strong> citrate occurs when citric acid cycle precursors such as malate or<br />

succinate are infused. Increased excretion resulting form inhibition <strong>of</strong> citrate metabolism occurs when<br />

malonate, maleate or fluorocitrate is administered. Systemic acid-base changes cause striking changes in<br />

citrate clearance and metabolism.<br />

Sinclair, R. G. and Bird, P. L. (1984). The reaction <strong>of</strong> Sminthopsis crassicaudata to meat baits containing<br />

1080 : implications for assessing risk to non-target species. Australian wildlife research 11, 501-507.<br />

Keywords: non-target species/mammals/baits/1080/marsupials/predators<br />

Singh, M., Vijayaraghavan, R., Pant, S. C., Sugendran, K., Kumar, P., Singh, R., and Purnanand (2000).<br />

Acute inhalation toxicity study <strong>of</strong> 2-fluoroacetamide in rats. Biomedical and Environmental<br />

Sciences.[print] June 13, 90-96.<br />

Keywords: inhalation/toxicity/rats/convulsions/liver/kidney<br />

Abstract: One <strong>of</strong> the most potent rodenticides is 2-fluoroacetamide (2-FA). Toxicity <strong>of</strong> this chemical is well<br />

documented. However, its inhalation toxicity data is not available in the literature. Hence, acute inhalation<br />

toxicity study was carried out by exposing male and female rats to aerosols <strong>of</strong> 2-FA at different<br />

concentrations for 4 h in a dynamically operated whole body inhalation exposure chamber. During and after<br />

the inhalation exposure the rats were less active, and showed mild tremors and convulsions. At higher<br />

concentrations the rats died after 2-3 days. The estimated 4-h LC50 for male and female rats was 136.6 and<br />

144.5 mgcntdotm-3 respectively. Exposure to 0.7 LC50 for 4 h duration showed an increase in the liver<br />

weight <strong>of</strong> male and female rats 7 days after exposure. Various haematological and biochemical variables<br />

determined were within the normal limits. However, histological findings showed injured lung as indicated<br />

by desquamation and necrosis <strong>of</strong> the epithelium <strong>of</strong> the respiratory tract. Marked hypertrophy <strong>of</strong> hepatocytes<br />

displaying strong acidophilic granulated cytoplasm was observed. Focal dilatation <strong>of</strong> renal proximal tubules<br />

in kidney with cytoplasmic vacuolation, and irregularly placed pyknotic nuclei were seen. The present<br />

study shows that 2-FA is a highly toxic chemical through the inhalation route based on the LC50 value.<br />

Consequently necessary precautions should be taken during its handling<br />

Smith, F. A., Gardner, D. E., Yuile, C. L., de Lopez, O. H., and Hall, L. L. (1977). Defluorination <strong>of</strong><br />

fluoroacetate in the rat. Life sciences 20, 1131-1138.<br />

Keywords: treatment/metabolism/pathology/1080/defluorination/fluoride/urine/kidney/reproductive<br />

effects/bone/fluoroacetate/rats/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/excretion/inhibition/Krebs<br />

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Appendix C<br />

cycle/citrate/testes<br />

Abstract: Rats given 5 ppm F as FAc (equivalent to 26 ppm <strong>of</strong> NaFAc) in drinking water for approximately<br />

4 months deposited as much fluoride in the skeletal system as did rats receiving 5 ppm F as NaF in the<br />

water. Little evidence could be found for the presence <strong>of</strong> organically cound fluide in bone after ingesteding<br />

FAc, though an aprpeciable proportion <strong>of</strong> skeletal fluoride deposited when NaF was ingested was shown<br />

not to respond to the fluoride ion electrode. The daily urinary excretion <strong>of</strong> total fluoride after FAc was<br />

somewhat greater than after NaF; about two thirds <strong>of</strong> this fluoride responded to the electrode, whereas more<br />

than 90% <strong>of</strong> the total fluoride after NaF ws ionic in nature. The data are interpreted as showing that the rat<br />

is capable <strong>of</strong> splitting the C-F bond in FAc and/or in its fluoride-containing metbolites, with subsequent<br />

skeletal storage and renal excretion <strong>of</strong> the released fluoride ion. The chronic administration <strong>of</strong> this low level<br />

<strong>of</strong> FAc caused an early but temporary retardation <strong>of</strong> growth. The Krebs cycle was interfered with, as<br />

evidence by increased concentrations <strong>of</strong> citrate in kidney and urine. At termination <strong>of</strong> the experiment,<br />

histological examination <strong>of</strong> the testes showed that FAc had induced severe damage characterised by<br />

massive disorganisation <strong>of</strong> the tubules, nearly total loss <strong>of</strong> functional cells, absence <strong>of</strong> sperm and damage to<br />

the Sertoli cells.<br />

Smith, G. J. and Grosch, D. S. (1976). Fluoroacetate-induced changes in the fecundity and fertility <strong>of</strong><br />

Bracon hebetor females. Journal <strong>of</strong> economic entomology 69, 521-522.<br />

Keywords: invertebrates/pathology/fluoroacetate/developmental toxicity<br />

Smith, M. R. and Lequerica, J. L. (1985). Methanosarcina mutant unable to produce methane or assimilate<br />

carbon from acetate. Journal <strong>of</strong> bacteriology 164 , 618-625.<br />

Keywords: fluoroacetate/mon<strong>of</strong>luoroacetate/bacteria/resistance/metabolism<br />

Abstract: Mutants <strong>of</strong> methanosarcina barkeri 227 resistant to fluoroacetate were isolated from<br />

mon<strong>of</strong>luoroacetate-treated cultures. Mutant strain FAr9 was 100 times more resistant to mon<strong>of</strong>luoroacetate<br />

than the wild-type strain and was deficient in carbon uptake and CH4 and CO2 prodcution from methyllabeled<br />

acetate. Methanol was assimilated at increased levels.<br />

Soiefer, A. I. and Kostyniak, P. J. (1983). The enzymatic defluorination <strong>of</strong> fluoroacetate in mouse liver<br />

cytosol : the separation <strong>of</strong> defluorination activity from several glutathione S-transferases <strong>of</strong> mouse liver.<br />

Archives <strong>of</strong> biochemistry and biophysics 225, 928-935.<br />

Keywords: metabolism/defluorination/enzyme/liver/temperature<br />

Abstract: The liberation <strong>of</strong> free fluoride ion from fluoroacetate (FAc) proceeds as an enzyme-catalyzed<br />

dehalogenation reaction in the soluble fractions <strong>of</strong> several organs <strong>of</strong> the CFW Swiss mouse. Liver<br />

contained the highest FAc defluorinating activity. The enzyme activity in other organs decreased in the<br />

order kidney > lung > heart > testes. No activity was detected in the brain. Experiments were designed to<br />

characterize and identify the enzyme species responsible for FAc metabolism in liver. Enzyme activity was<br />

dependent on the concentration <strong>of</strong> glutathione (GSH) in the assay mixture, with maximal activity occurring<br />

above 5mM. The dehalogenation <strong>of</strong> FAc had an apparent Km <strong>of</strong> 7.0 mM when measured in the presence <strong>of</strong><br />

a saturating concentration <strong>of</strong> GSH. An increase in the pH <strong>of</strong> the assay mixture enhanced fluoride release in<br />

both phosphate and borate buffer. The defluorination activity was reduced to negligible levels when stored<br />

for 24 h at 4EC. The addition <strong>of</strong> either GSH, dithiothreitol, or 2-mercaptoethanol increased stability, with<br />

the latter providing protection for greater than 150 h at a concentration <strong>of</strong> 15mM. DEAE anion-exchange<br />

chromatography separated the defluorinating activity from 90% <strong>of</strong> the soluble GSH S-transferase activity<br />

measure with 1-chloro-2,4-dinitrobenzene. FAc deluorination activity did not bind to a GSH affinity<br />

column which selectively separates it from a group <strong>of</strong> anionic GSH S-transferases. The GSH-dependent<br />

enzyme which dehalogenates FAc has unique properties and can be separated from the liver GSH Stransferases<br />

previously described in the literature.<br />

Soiefer, A. I. and Kostyniak, P. J. (1984). Purification <strong>of</strong> a fluoroacetate-specific defluorinase from mouse<br />

liver cytosol. The Journal <strong>of</strong> Biological Chemistry 259, 10787-10792.<br />

Keywords: liver/enzyme/defluorination/rodents/fluoride/metabolism<br />

Abstract: Fluoroacetate-specific defluorinase, an enzyme which catalyzes the release <strong>of</strong> fluoride ion from<br />

the rodenticide fluoroacetate, has been purified 347-fold from mouse liver cytosol and shown to be distinct<br />

from multiple cationic and anionic glutathione S-transferase isozymes.The evidence presented suggests<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

that fluoroacetate-specific defluorinase and glutathione S-tranferase activities are catclyzed by separate<br />

proteins present in the cytosol <strong>of</strong> mouse liver<br />

Soiefer, A. I. The biochemical and immunological characterization <strong>of</strong> the fluoroacetate-specific<br />

defluorinase from mouse liver cytosol. Pharmacology Dissertation Abstracts International 4[03], 845-B.<br />

1984.<br />

Ref Type: Abstract<br />

Keywords: liver/fluoroacetate/enzyme/biochemistry/metabolism<br />

Abstract: An hepatic defluorinase which specifically catalyses the liberation <strong>of</strong> fluoride ion from the<br />

rodenticide fluoroacetate has been isolated and characterised by biochemical and immunological<br />

techniques.<br />

Somers, J. M., Sweet, G. D., and Kay, W. W. (1981). Fluorocitrate resistant tricarboxylate transport<br />

mutants <strong>of</strong> Salmonella typhimurium. ? Gen.Genet. 181 , 338-345.<br />

Keywords: fluorocitrate/citrate/bacteria/metabolism/Krebs cycle/aconitate<br />

Abstract: Spontaneous and Tn10 induced fluorocitrate resistant mutants were isolated and characterized.<br />

These mutants were unable to grow on either cis-aconitate or DL-isocitrate but were still able to grow<br />

slowly on sodium citrate and normally on potassium or potassium-plus-sodium citrate. These mutants were<br />

defective in both citrate transport and citrate binding to periplasmic proteins. Tn10 insertion mutants were<br />

unable to produce immunologically detectable amounts <strong>of</strong> the citrate inducible periplasmic C protein<br />

previously shown to bind tricarboxylates.<br />

Using a series <strong>of</strong> tct: :Tn10 directed Hfrs the tct locus was accurately positioned at 59 units between srlA<br />

and pheA, but was not cotransducible with either gene. In the absence <strong>of</strong> P22 mediated cotransduction with<br />

16 adjacent chromosomal markers the srlA and tct loci were bridged by using a series <strong>of</strong> tct flanking Tn10<br />

insertions, and by newly isolated and characterized nalB mutants. In addition the hyd and recA loci were<br />

located establishing the gene order in this region <strong>of</strong> the chromosome as: pheA tct nalB recA srlA hyd cys.<br />

Nitrosoguanidine derived tricarboxylate mutations (Imai 1975) were also mapped within the tct locus.<br />

Soni, N. K., Kazmi, S. M., and Trivedi, V. B. (1980). Respiratory responses <strong>of</strong> Rhizoctonia solani and<br />

Colletotrichum capsici induced by some carbohydrates, amino acids and metabolic inhibitors. Transactions<br />

<strong>of</strong> the Mycological Society <strong>of</strong> Japan 21, 131-135.<br />

Keywords: inhibition/sodium fluoroacetate/fluoroacetate/fungus<br />

Abstract: Respiration was stimulated by galactose, arabinose and fructose in R. solani and by lactose,<br />

xylose and glucose in C. capsici. Most <strong>of</strong> the amino acids tested stimulated respiration but L-tyrosine and<br />

DL-threonine in C. capsici and beta -alanine in R. solani were inhibitory. Metabolic inhibitors showed<br />

adverse effects on fungal respiration with the exception <strong>of</strong> methylene blue and Na malonate in R. solani.<br />

Inhibitory effects were less pronounced in R. solani than in C. capsici. Respiratory inhibition by sodium<br />

fluoroacetate suggests the presence <strong>of</strong> a functional TCA cycle in both pathogens<br />

Spencer, A. F. and Lowenstein, J. M. (1967). Citrate content <strong>of</strong> liver and kidney <strong>of</strong> rat in various metabolic<br />

states and in fluoroacetate poisoning. Biochemical journal 103, 342-348.<br />

Keywords: metabolism/persistence in animals/mode <strong>of</strong> action/citrate/liver/kidney/fluoroacetate/poisoning<br />

Abstract: The citrate content <strong>of</strong> rat liver changes little when normal rats are starved, when starved rats are<br />

re-fed with various diets and when normal animals are made diabetic with alloxan. The citrate content <strong>of</strong> rat<br />

kidney changes little on starvation, but it doubles on induction <strong>of</strong> diabetes. Fluoroacetate poisoning has<br />

relatively little effect on the citrate content <strong>of</strong> liver under a variety <strong>of</strong> conditions except that normal female<br />

rats show a 2.4-fold increase. Fluoroacetate poisoning leads to increases in the citrate content <strong>of</strong> kidney<br />

under all conditions. The relevance <strong>of</strong> these observations to the regulation <strong>of</strong> fatty acid synthesis is<br />

discussed. The acteic anhydride-pyridine method and the pentobromoacetone method for the estimation <strong>of</strong><br />

citrate are compared.<br />

Spielmann, H., Meyer-Wendecker, R., and Spielmann, F. (1973). Influence <strong>of</strong> 2-deoxy-D-glucose and<br />

sodium fluoroacetate on respiratory metabolism <strong>of</strong> rat embryos during organogenesis. Teratology 7, 127-<br />

134.<br />

Keywords: metabolism/pathology/sodium fluoroacetate/treatment/reproductive effects/developmental<br />

toxicity/teratogenicity<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: The effect <strong>of</strong> various concentration <strong>of</strong> 2 deoxy-d-glucose (2DG) and sodium fluoroacetate (SFA)<br />

on the Q02 <strong>of</strong> day-11 and 12 rat embryos was studied in vitro. The dose-response curves - % inhibition<br />

versus log concentration - were linear for 2DG between 500 uM and 50 mM; day 11 rat embryos showed a<br />

higher rate <strong>of</strong> inhibition than day-12 embryos and adult kidney tissue. The inhibitory effect <strong>of</strong> SFA on the<br />

embryonic Q02 in vitro was significantly lower than on adult kidney tissue slices. These is vitro effects are<br />

in agreement with recent investigations on the energy metabolism <strong>of</strong> rat embryos that revealed a change<br />

from glycolysis to an oxidative, respiratory metabolism during organogenesis. The administration <strong>of</strong> a<br />

single dose <strong>of</strong> 2DG and SFA to pregnant rats at day 9 or 10 <strong>of</strong> pregnancy significantly reduced the Q02 and<br />

dry weight <strong>of</strong> the embryos at day 11, where as both parameters were unchanged at day 12. The same<br />

treatment was nonteratogenic, which is in contrast to the findings <strong>of</strong> other investigators.<br />

Sporkert, F., Pragst, F., Hubner, S., and Mills, G. (2002). Headspace solid-phase microextraction with 1pyrenyldiazomethane<br />

on-fibre derivatisation for analysis <strong>of</strong> fluoroacetic acid in biological samples. Journal<br />

<strong>of</strong> chromatography 772, 45-51.<br />

Keywords: analysis/serum/blood/urine/stomach/kidney<br />

Abstract: A new and in part automated headspace solid-phase microextraction method for quantitative<br />

determination <strong>of</strong> the highly toxic rodenticide fluoroacetic acid (FAA) in serum and other biological samples<br />

has been developed. FAA and deuterated acetic acid (internal standard) were extracted from acidified<br />

samples by a StableFlex divinylbenzene-Carboxen on polydimethylsiloxane fibre. The acids were<br />

derivatised on the fibre in-situ with 1-pyrenyldiazomethane and detected using gas chromatography-mass<br />

spectrometry with electron impact ionisation and selected ion monitoring. The calibration curve for FAA in<br />

serum was linear over the range from 0.02 to 5 mug/ml, with limits <strong>of</strong> detection and quantification <strong>of</strong> 0.02<br />

and 0.07 mug/ml, respectively. The method was also tested with spiked whole blood, urine, stomach<br />

contents and kidney samples. It was sufficiently reliable, reproducible and sensitive for use in routine<br />

forensic toxicology applications.<br />

Spurr, E. (2000). Impacts <strong>of</strong> possum control on non-target species. In 'The brushtail possum : biology,<br />

impact and management <strong>of</strong> an introduced marsupial'. (Ed. T. L. Montague.) pp. 175-186. (Manaaki<br />

Whenua: Lincoln.)<br />

Keywords: non-target species/possums/aerial control/ground control<br />

Spurr, E., Berben, P. H., McGregor, P. G., and Arnold, G. Impacts <strong>of</strong> simulated aerial application <strong>of</strong> 1080poisoned<br />

baits on ground-dwelling invertebrate populations. LCR to be specified, -40. 2002. <strong>Landcare</strong><br />

<strong>Research</strong> Contract Report.<br />

Ref Type: Report<br />

Keywords: baits/persistence in invertebrates/invertebrates/aerial control<br />

Spurr, E. B. (1979). A theoretical assessment <strong>of</strong> the ability <strong>of</strong> bird species to recover from an imposed<br />

reduction in numbers, with particular reference to 1080 poisoning. New Zealand journal <strong>of</strong> ecology 2, 46-<br />

63.<br />

Keywords: non-target species/birds/1080/poisoning<br />

Spurr, E. B. (1991). Effects <strong>of</strong> brushtail possum control operations on non-target bird populations. In<br />

'Proceedings <strong>of</strong> the 20th International Ornithological Congress'. (B. D. Bell and et al.Eds. ) pp. 2534-2545.<br />

(Ornithological Congress Trust Board: [Christchurch].)<br />

Keywords: non-target species/birds/1080<br />

Abstract: The brushtail Possum Trichosurus vulpecula, a herbivorous Australian marsupial, is a serious pest<br />

<strong>of</strong> forest and farmland in New Zealand. Possum numbers are periodically controlled, mainly by aerial<br />

distribution <strong>of</strong> baits containing Compound 1080, ground based trapping, or cyanide poisoning. Poisoning<br />

with 1080 kills more non-target birds per hectare than commercial trapping or cyanide poisoning, but is<br />

also potentially more beneficial to bird populations because it causes a greater reduction in Possum<br />

populations, and hence a greater improvement in the condition <strong>of</strong> the habitat. There is no evidence that<br />

Possum control operations have any detrimental effects on populations survival <strong>of</strong> the more common bird<br />

species present in Possum areas.<br />

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Appendix C<br />

Spurr, E. B. (1991). Reduction <strong>of</strong> wasp (Hymenoptera: Vespidae) populations by poison-baiting :<br />

experimental use <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) in canned sardine. New Zealand journal <strong>of</strong> zoology<br />

18, 215-222.<br />

Keywords: field efficacy/invertebrates/mon<strong>of</strong>luoroacetate/1080/wasps<br />

Spurr, E. B. (1991). Wasp control by poison baiting : experimental use <strong>of</strong> hydramethylnon in canned<br />

sardine bait. Proceedings <strong>of</strong> the New Zealand Weed and Pest <strong>Control</strong> Conference 44, 42-46.<br />

Keywords: ground control/field efficacy/invertebrates/wasps<br />

Spurr, E. B. (1991). Fighting the wasp problem. What's New in Forest <strong>Research</strong>.<br />

Keywords: baits/honey/poison/1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate<br />

Abstract: Baits typically consist <strong>of</strong> fresh fish or meat. Sugar-based baits are unsuitable because they are<br />

attractive to honey bees. Until recently, a slow-acting organochlorine poison called mirex was mixed with<br />

baits. This has now been withdrawn from the market but a replacement has not yet been found. At the<br />

request <strong>of</strong> the former New Zealand Forest Service and Department <strong>of</strong> Conservation, the Forest <strong>Research</strong><br />

Institute has tested the effectiveness <strong>of</strong> compound 1080 (sodium mon<strong>of</strong>luoroacetate) as an alternative<br />

poison for the control <strong>of</strong> wasps in areas <strong>of</strong> high public use.<br />

Spurr, E. B. (1993). Feeding by captive rare birds on baits used in poisoning operations for control <strong>of</strong><br />

brushtail possums. New Zealand journal <strong>of</strong> ecology 17, 13-18.<br />

Keywords: non-target species/birds/possums/baits<br />

Abstract: Baits may be made less acceptable to birds by increasing the strength or slowing the release <strong>of</strong><br />

cinnamon, or by using a more repellent flavour. Because baits may always be acceptable to some birds,<br />

wildlife managers need to know the chances <strong>of</strong> wild rare birds feeding on baits before approving poisoning<br />

operations in areas where they occur.<br />

Spurr, E. B. (1994). Review <strong>of</strong> the impacts on non-target species <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) in<br />

baits used for brushtail possum control in New Zealand. In 'Proceedings <strong>of</strong> the Science Workshop on 1080,<br />

12-14 December 1993, Christchurch, New Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 124-133.<br />

(<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: non-target species/invertebrates/birds/1080<br />

Abstract: The impacts on non-target species <strong>of</strong> 70 aerial 1080-poisoning operation or trials for brushtail<br />

possum control in New Zealand between 1978 and 1993 are reviewed> Dead birds were reported from 15<br />

operations on trials; 34 blackbirds were reported from 15 operations or trials; 34 blackbirds, 15 tomtits, 14<br />

chaffinches, nine whiteheads, four moreporks, three fantails, one grey warbler, on robin, one tui and one<br />

magpie. Significantly more birds were found dead after operations using carrot baits than after operations<br />

using cereal-based baits. Selected bird populations <strong>of</strong> common, adequately monitored bird species.<br />

However, less common bird species (e.g. kiwi, kaka, kakariki, and kokako) have been inadequately<br />

monitored , at least for some bait types. Bats, lizards and frogs have not been monitored in any 1080<br />

poisoning operations, and none have been reported killed by 1080. Selected invertebrate populations were<br />

monitored in five 1080 poisoning operations. No impact was detected on populations <strong>of</strong> weta in Waipoua<br />

Forest, a range <strong>of</strong> invertebrate species on Rongitoto Island, predatory insects in Mapara Reserve, or grounddwelling<br />

invertebrates in Puketi Forest and Titirangi Reserve.<br />

Spurr, E. B. (1994). Impacts on non-target invertebrate populations <strong>of</strong> aerial application <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) for brushtail possum control. In 'Proceedings <strong>of</strong> the Science Workshop on 1080,<br />

12-14 December 1993, Christchurch, New Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 116-123.<br />

(<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: non-target species/invertebrates/1080<br />

Abstract: Impacts on non-target ground-dwelling invertebrate populations <strong>of</strong> two aerial 1080-poisonings<br />

operations using cereal-based baits for brushtail possum control were monitored in Puketi Forest and<br />

Titirangi Scenic Reserve. Invertebrates were collected in 100 pitfall traps in paired poison and non-poison<br />

areas. Bait density within 2m <strong>of</strong> traps in poison areas was measured on the day <strong>of</strong> poisoning. The traps<br />

were open continuously an were emptied monthly twice before poisoning at Puketi, four times before<br />

poisoning at Titirangi, and 12 time after poisoning at both sites. Trapped invertebrates were sorted into<br />

orders and/or families. Preliminary analysis <strong>of</strong> counts from five traps in Puketi, 10 traps in Titirangi, and<br />

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Appendix C<br />

10 traps in each non-poison area did not reveal any impact <strong>of</strong> the 1080 poisoning operations on populations<br />

<strong>of</strong> Acari, Amphipoda, Araneae, three families <strong>of</strong> Coleoptera, other Coleoptera, Collembola, Diplopoda,<br />

Formicidae. Pulmonata and Rhaphidophoridae.<br />

Spurr, E. B. and Powlesland, R. G. Impacts <strong>of</strong> aerial application <strong>of</strong> 1080 on non-target native fauna : review<br />

and priorities for conservation. [62], -31. 1997. Wellington, Department <strong>of</strong> Conservation. Science for<br />

conservation.<br />

Ref Type: Report<br />

Keywords: non-target species/invertebrates/birds/1080/possums<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) is used by the Department <strong>of</strong> Conservation (in cereal-based<br />

baits) and by Regional Councils (in carrot and cereal-based baits) during aerial poisoning operation for<br />

control <strong>of</strong> possums (Trichosurus vulpecula) in New Zealand. The impacts <strong>of</strong> these operations on non-target<br />

species <strong>of</strong> birds, bats, lizards, frogs and invertebrates are reviewed, and priorities for further research are<br />

recommended. A <strong>Research</strong> Co-ordinating Group should be established to implement these<br />

recommendations.<br />

Spurr, E. B. and Porter, R. E. R. (1998). Cinnamamide as a bird repellent for baits used in mammalian pest<br />

control. In '11th Australian Vertebrate Pest Conference, Bunbury, Western Australia, 3-8 May 1998 :<br />

programme and proceedings.'. pp. 295-299. (Agriculture Western Australia: Forrestfield.)<br />

Keywords: non-target species/birds/possums<br />

Abstract: An effective bird repellent is required to prevent bird species in New Zealand from eating baits<br />

used for the control on introduced mammalian pests, such as brushtail possums and Norway rats. In a doseresponse<br />

study, cinnamamide mixed into cereal based baits at concentrations <strong>of</strong> 0.1% and 0.25% (wt/wt)<br />

did not significantly reduce bait consumption by captive weka, but 0.5% cinnamamide reduced bait<br />

consumption by 83%. Addition <strong>of</strong> 0.5% cinnamamide to the surface <strong>of</strong> carrot baits reduced bait<br />

consumption by captive kea by 89%, and eastern rosellas by 80% in one trial and 85% in a subsequent trial.<br />

Birds exhibited both direct taste repellency and learned taste aversion to cinnamamide. A surface coating<br />

<strong>of</strong> 0.5% cinnamamide on carrot baits did not significantly reduce bait consumption by captive possums, but<br />

as little as 0.25% cinnamamide mixed into cereal-based baits reduced bait consumption by captive Norway<br />

rates by 53%. These results indicate that 0.5% cinnamamide added to baits could greatly reduce the risks to<br />

birds during rodent control operations.<br />

Spurr, E. B. and Drew, K. W. (1999). Invertebrates feeding on baits used for vertebrate pest control in New<br />

Zealand. New Zealand journal <strong>of</strong> ecology 23, 167-173.<br />

Keywords: non-target species/invertebrates/possums<br />

Abstract: This study was initiated in response to concerns that vertebrate pest control operations in New<br />

Zealand may be having deleterious impacts on invertebrate populations and, secondarily, on insectivorous<br />

non-target vertebrate populations. Invertebrates feeding on non-toxic baits <strong>of</strong> the types used for vertebrate<br />

pest control were collected and identified. The bait types were diced carrots and three types <strong>of</strong> cereal-based<br />

baits (No.7, RS5, and AgTech). The study was conducted in two rata/kamahi dominated forests (Bell Hill<br />

Scenic Reserve and Kopara Forest, West Coast), in July and September 1996. The most common species<br />

found on baits was the ant Huberia brouni (Hymenoptera: Formicidae). Other common taxa were<br />

Orthoptera (at least eight species <strong>of</strong> weta including Zealandosandrus aff. gracilis, Gymnoplectron sp., and<br />

Pleioplectron sp.). Coleoptera (at least nine species <strong>of</strong> beetles including Saphobius nitidulus, Nestrius sp.,<br />

and Phrynixus sp.), Dermaptera (at least one species <strong>of</strong> the earwig Parisolabis sp.), Opiliones (at least three<br />

species <strong>of</strong> harvestmen), and Acarina (at least three species <strong>of</strong> mites). The ants and weta were found<br />

predominately on cereal-based baits, and the beetles, earwigs, harvestmen, and mites predominantly on<br />

carrot baits. More invertebrates were found on carrot and RS5 cereal-based baits than on the other two bait<br />

types, and more on baits at night than during the day. Fewer invertebrates were found on cinnamonflavoured<br />

baits (used for 1080-poisoning <strong>of</strong> possums) than on plain baits (used for brodifacoum-poisoning<br />

<strong>of</strong> rodents). The number <strong>of</strong> species and number <strong>of</strong> individual invertebrates found on baits were a small<br />

proportion <strong>of</strong> the number likely to be present in the forest litter. We predict that vertebrate pest control<br />

operations are unlikely to have any long term deleterious impacts on invertebrate populations. This<br />

prediction should be tested by monitoring populations <strong>of</strong> invertebrate species, found to eat baits, during<br />

vertebrate pest control operations.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Spurr, E. B. Are insectivorous birds killed by primary or secondary 1080 poisoning? [LC9899/057], -16.<br />

1999. Lincoln, Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>. <strong>Landcare</strong> <strong>Research</strong> contract report.<br />

Ref Type: Report<br />

Keywords: non-target species/invertebrates/birds/secondary poisoning/1080/lethal dose<br />

Abstract: Objective : To determine whether insectivorous birds could die as a result <strong>of</strong> secondary 1080poisoning,<br />

based on the amount <strong>of</strong> toxin ingested by invertebrates and the number <strong>of</strong> invertebrates that an<br />

insectivorous bird would need to ingest to receive a lethal dose <strong>of</strong> 1080.<br />

Conclusion : The risk <strong>of</strong> secondary 1080-poisoning to insectivorous birds is related to the amount <strong>of</strong> 1080<br />

required to kill the birds and the amount <strong>of</strong> 1080 that the birds ingest from invertebrates that have eaten<br />

bait; Based on published LD50s and the amounts <strong>of</strong> 1080 measured in invertebrates after 1080-poisoning<br />

operations, secondary 1080-poisoning <strong>of</strong> insectivorous birds is theoretically possible; However, the<br />

circumstantial evidence available suggests that direct poisoning <strong>of</strong> insectivorous birds from eating baits is<br />

more likely than secondary poisoning from eating invertebrates that have eaten baits.<br />

Spurr, E. B. (2000). Hen eggs poisoned with sodium mon<strong>of</strong>luoroacetate (1080) for control <strong>of</strong> stoats<br />

(Mustela erminea) in New Zealand. New Zealand journal <strong>of</strong> zoology 27, 165-172.<br />

Keywords: field efficacy/ground control/predators/1080<br />

Spurr, E. B. and Berben, P. H. Are weta populations affected by 1080? Kararehe Kino [1], 10-11. 2002.<br />

Lincoln, Manaaki Whenua <strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Magazine Article<br />

Keywords: 1080/poisoning/baits/poison/invertebrates<br />

Abstract: Weta are potentially at risk from 1080 poisoning for possum control as several species have<br />

been observed eating toxic baits. Also some weta collected alive after 1080-poisoning operations have<br />

contained residues <strong>of</strong> 1080. To date, weta populations that have been monitored in poison baited areas<br />

have not been affected by the toxin. These results are open to challenge, however, because the methods<br />

used to monitor impacts have not included individually marked weta. For example, one study recorded<br />

weta calls heard at night and another the number <strong>of</strong> weta caught in pitfall traps.<br />

To confirm the risk to weta (or not), Eric Spurr and Peter Berben monitored individually marked weta<br />

occupying artificial refuges before and after simulated aerial 1080-poisoning (i.e. baits spread by hand). To<br />

do this, they set up 10 randomly located artificial refuges (Fig. 1) in each <strong>of</strong> 20 plots spaced at least 50m<br />

apart on a north-facing ridge in Tararua Forest Park in August 1999. From October onwards, the refuges<br />

were checked monthly for occupancy by weta and other invertebrates, and any tree weta present were<br />

individually marked with coloured paint. In August 2000, 10 <strong>of</strong> the plots, chosen at random, were sown by<br />

hand with 1080 bait at 5 kg/ha. The bait was green-dyed, cinnamon-lured, Wanganui No.7 cereal-based<br />

bait containing 1500 ppm (0.15%) 1080. The remaining 10 plots were not baited. The artificial refuges<br />

were checked for occupancy by weta and other invertebrates a week after bait application, and then again at<br />

monthly intervals for the next 4 months.<br />

Spurr, E. B. (2002). Bird control chemicals. (Marcel Dekker: New York.)<br />

Keywords: birds/1080/strychnine/alphachloralose/fenthion/DRC-1339<br />

Abstract: Chemicals used to control bird populations when they cause damage to crops, stock-food,<br />

buildings and other structures, and when they are ahzards at places suchas airports, public parks, golf<br />

courses and rubbish dumps. They include lethal toxicants (avidcides) and stressing agents, and nonlethal<br />

immobilizing agents, repellents and reproductive inhibitors. Lethal methods <strong>of</strong> control attempt tor educe<br />

bird numbers, whereas nonlethal control methods generally attempt to modify bird behaviour without<br />

causing mortality as a means <strong>of</strong> reducing damage.<br />

Spurr, E. B. and Berben, P. H. (2004). Assessment <strong>of</strong> non-target impact <strong>of</strong> 1080-poisoning for vertebrate<br />

pest control on weta (Orthoptera: Anostostomatidae and Rhaphidophoridae) and other invertebrates in<br />

artificial refuges. New Zealand journal <strong>of</strong> ecology 28, 63-72.<br />

Keywords: pest/invertebrates/baits/1080/New Zealand/lethal dose/poisoning/residues/non-target species<br />

Abstract: Artificial refuges and mark-recapture techniques were used to monitor the non-target impacts <strong>of</strong><br />

hand-broadcast applications (simulating aerial application) <strong>of</strong> Wanganui No. 7 cereal-based baits<br />

containing 0.15% (1500 ug/g) 1080 on populations <strong>of</strong> weta and other invertebrates in Tararua Forest Park,<br />

North Island, New Zealand. Wellington tree weta (Hemideina crassidens) and a cave weta (Isoplectron sp.)<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

were the only species <strong>of</strong> weta that occupied the refuges. Flatworms, slugs, spiders, harvestmen, amphipods,<br />

millipedes, centipedes, cockroaches and beetles also occupied the refuges. Invertebrate numbers in the<br />

refuges were monitored for 12 months before and 4 months after bait application on 22 August 2000. Bait<br />

application had no significant impact on the numbers <strong>of</strong> either species <strong>of</strong> weta, or on slugs, spiders and<br />

cockroaches, the most numerous other invertebrates occupying the refuges. Bait application also had not<br />

effect on the number <strong>of</strong> individually marked tree weta resighted in the refuges. Few weta or other<br />

invertebrates were observed on baits at night. The concentration <strong>of</strong> 1080 in a cave weta collected alive from<br />

a bait, and a tree weta collected alive from outside an artificial refuge was less than 10% <strong>of</strong> the average<br />

lethal dose. The results indicate that 1080 poisoning for vertebrate pest control is unlikely to have any<br />

negative impact on populations <strong>of</strong> weta or the other invertebrates monitored.<br />

Srere, P. A. (1965). The molecular physiology <strong>of</strong> citrate. Nature 205, 766-770.<br />

Keywords: citrate/metabolism/enzyme<br />

Abstract: Citrate has always occupied an important position in metabolism and several recent observations<br />

have added new dimensions to its role in living processes. A significant observation was that <strong>of</strong> Brady and<br />

Gurin who found that the rate <strong>of</strong> fatty acid synthesis by a crude soluble enzyme system was greatly<br />

stimulated by citrate. This observation eventually led to the recognition <strong>of</strong> three metabolic functions for<br />

citrate in addition to its role in the Krebs cycle and ATP production: a source <strong>of</strong> reducing power, a source<br />

<strong>of</strong> acetyl groups for biosynthetic pathways and a controlling (activating or inhibiting) substance for a<br />

number <strong>of</strong> enzymes.<br />

Stahr, H. M., Clardy, D. O., and Buck, W. B. (1971). Screening test for fluoroacetate in baits and biological<br />

samples. Journal <strong>of</strong> the Association <strong>of</strong> Official Analytical Chemists 54, 1235-1237.<br />

Keywords: fluoroacetate/baits/fluoride/analysis<br />

Abstract: A simple screening test, based on the reaction <strong>of</strong> the fluoride ion with the ion-selective fluoride<br />

electrode, has been developed for fluoroacetate in baits and biologicla samples. Positive results have been<br />

obtained in diagnostic cases. The method is not specific for fluoroacetate, but other fluoride-containing<br />

compounds are not likely to be present in the extract. Positive responses to the test should be confirmed as<br />

fluoroacetate by another method, such as the <strong>of</strong>ficial AOAC method or by gas chromatography-mass<br />

spectrometry.<br />

Stahr, H. M. (1977). Quantitative gas-liquid chromatographic method for sodium fluoroacetate. Journal <strong>of</strong><br />

the Association <strong>of</strong> Official Analytical Chemists 60, 1434-1535.<br />

Keywords: product chemistry<br />

Stallings, W. C., Monti, C. T., Belvedere, J. F., Preston, R. K., and Glusker, J. P. (1980). Absolute<br />

configuration <strong>of</strong> the isomer <strong>of</strong> fluorocitrate that inhibits aconitase. Archives <strong>of</strong> biochemistry and biophysics<br />

203, 65-72.<br />

Keywords: mode <strong>of</strong> action/product chemistry/fluorocitrate/aconitase<br />

Staples, E. L. J. (1968). The reduction <strong>of</strong> the sodium mon<strong>of</strong>luoroacetate ("1080") content <strong>of</strong> carrot baits <strong>of</strong><br />

various thicknesses by weathering. New Zealand journal <strong>of</strong> agricultural research 11, 319-329.<br />

Keywords: bait degradation/rabbits/deer/possums/sodium mon<strong>of</strong>luoroacetate/zinc phosphide/witholding<br />

period<br />

Abstract: The rate <strong>of</strong> removal <strong>of</strong> sodium fluoroacetate (1080) from chopped carrot treated witht he poison<br />

at a rate <strong>of</strong> 1/2 lb or 1 lb per ton and then exposed to weather has been studied. The rainfall pattern is an<br />

important factor in the weathering <strong>of</strong> poisoned rabbit baits but it is not possible to lay down specific rules<br />

about the time that domestic stock should be kept <strong>of</strong>f recently-poisoned areas. The trials showed that the<br />

baits became harmless to stockmore quickly when that carrot was cut thin and when the amount <strong>of</strong> 1080<br />

receommended for rabbits ie. 1/2 lb per ton <strong>of</strong> carrot, was not exceeded. When opossums or deer are to be<br />

poisoned in areas that are not to be restocked with domestic animals larger pieces <strong>of</strong> carrot and high levels<br />

<strong>of</strong> 1080 ie. 2 lb per ton are indicated. in order that baits should remain toxic for as long as possible.<br />

Staples, E. L. J. (1969). Absorption <strong>of</strong> sodium mon<strong>of</strong>luoroacetate ("1080") solution by carrot baits. New<br />

Zealand journal <strong>of</strong> agricultural research 12, 783-788.<br />

Keywords: bait degradation/field efficacy/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/baits/carrot<br />

189


1080 Reassessment Application October 2006<br />

Appendix C<br />

Statham, M. Vertebrate Pest Manual Tasmania. Tasmanian Institute <strong>of</strong> Agricultural <strong>Research</strong>. 1988.<br />

Ref Type: Report<br />

Keywords: 1080<br />

Steinberger, E. and Sud, B. N. (1970). Specific effect <strong>of</strong> fluoroacetamide on spermatogenesis. Biol.Reprod.<br />

2, 369-375.<br />

Keywords: fluoroacetamide/testes/reproductive effects<br />

Stewart, D. J, Manley, T. R, White, D. A., Harrison, D. L., and Stringer, E. A. (1974). Natural fluorine<br />

levels in the Bluff area, New Zealand. 1. Concentrations in wildlife and domestic animals. New Zealand<br />

journal <strong>of</strong> science 17, 105-113.<br />

Keywords: fluorine<br />

Abstract: Natural fluorine concentrations are reported in the skeletons <strong>of</strong> birds, fish, small mammals, cattle<br />

and sheep, sampled in the Bluff area <strong>of</strong> New Zealand. Expressed on a bone-ash basis the values obtained<br />

were: 142-8050 ppm for nine species <strong>of</strong> birds; 100-4554 ppm for six species <strong>of</strong> fish; 13-357 ppm for six<br />

species <strong>of</strong> shellfish; 184-278 ppm for opossums and rabbit; and 19-1469 ppm for cattle and sheep.<br />

Comparisons with published data indicate that the natural levels <strong>of</strong> fluorine in the fauna <strong>of</strong> the Bluff area<br />

are, in general, similar to levels found elsewhere in the world.<br />

Stewart, G. G., Abbs, E. T., and Roberts, D. J. (1969). Biochemical effects <strong>of</strong> fluoroacetate administration<br />

in rat brain, heart and blood. Biochemical Pharmacology 19, 1861-1866.<br />

Keywords: mode <strong>of</strong> action/persistence in<br />

animals/fluoroacetate/brain/heart/blood/rodents/symptoms/citrate/Krebs cycle<br />

Abstract: Treatment <strong>of</strong> rats with fluoroacetate resulted in two phases <strong>of</strong> behaviour (i) a sedated phase<br />

followed by (ii) a tonic extensor convulsive phase. The levels <strong>of</strong> various labile metabolites such as citric<br />

acid, lactic acid, ammonia, free glucose and glycogen, were measures at these two phases in heart, brain<br />

and blood. In heart the citric acid level rose in both <strong>of</strong> the phases, however in the brain the level <strong>of</strong> this<br />

metabolite fell at the convulsion following an initial rise during the sedative phase. This alteration in the<br />

citrate content <strong>of</strong> brain could have pr<strong>of</strong>ound effects on the tricarboxylic acid cycle as a whole and also on<br />

the level <strong>of</strong> compounds, such as GABA, related to the cycle. The implications <strong>of</strong> such alterations on the<br />

overall behavioural patterns are discussed.<br />

Stewart, H., Jenkin, B., McCarthy, R., and Flinn, D. (1994). Public versus user perceptions <strong>of</strong> risks and<br />

benefits <strong>of</strong> plantation forestry in Victoria, Australia. In 'Proceedings <strong>of</strong> the Science Workshop on 1080. 12-<br />

14 December 1993, Christchurch, New Zealand.'. (A. A. Seawright and C. T. EasonEds. ) pp. 10-19. (<strong>Royal</strong><br />

Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: 1080/wallaby<br />

Abstract: In the past two decades there had been considerable conflict concerning social, economic and<br />

environmental aspects <strong>of</strong> plantations in Victoria. The issues have included: the change <strong>of</strong> land use from<br />

agriculture to forestry; the use <strong>of</strong> 1080 to control browsing animals and vermin; aerial application <strong>of</strong><br />

herbicides; perceived human health hazard from plantation disease such as Pine Needle Blight; and<br />

recently, the implications <strong>of</strong> genetic engineering in plantation forestry. These concerns have been fought as<br />

single issues in some cases and collectively in others in a wide range <strong>of</strong> forums. In some instances strident<br />

opposition has resulted in direct action to halt plantation works. Conflict about use <strong>of</strong> 1080 in plantation<br />

development in Gippsland (in southern Victoria) provides a useful case study <strong>of</strong> the way in which a single<br />

issue can impact on the public perception <strong>of</strong> plantations and influence plantation management practices.<br />

Initial responses to these concerns included 'do nothing', communication to the relevant groups rationale<br />

for the plantation program, and the use <strong>of</strong> scientific facts to dispel arguments about specific environmental<br />

impacts. This approach met with limited success. In 1986, public participation was engaged seriously in<br />

the broad debate on plantations for the first time by way <strong>of</strong> a Plantation Impact Study initiated by<br />

government. This and subsequent forestry inquiries have failed, however, to deliver universal support for<br />

plantation forestry. Such a goal is probably unrealistic given that the basis for conflict is continually<br />

changing in response to changes in socio-economic factors and scientific knowledge. Lessons have been<br />

learned, however, by all parties involved in the debate on these issues and a number <strong>of</strong> principles are<br />

generally agreed as a means <strong>of</strong> moving forward: identify and understand issues early; research issues and<br />

make relevant knowledge available; adopt the concept <strong>of</strong> informed consent; develop a framework for<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

genuine public participation; and make a sincere commitment to participate with the public in resolving<br />

questions about the risks and benefits <strong>of</strong> plantation forestry.<br />

Steyn, D. G. (1934). Plant poisoning in stock and the development <strong>of</strong> tolerance. Onderstepoort journal <strong>of</strong><br />

veterinary science 3, 119-123.<br />

Keywords: poisoning/tolerance/livestock/occurrence in nature/rabbits/heart<br />

Abstract: From the results <strong>of</strong> experiments conducted upon thirty-two rabbits it appears (a) that the<br />

continuous ingestion <strong>of</strong> leaves or underground stems <strong>of</strong> gifblaar does not induce the development <strong>of</strong><br />

tolerance to this plant; and (b) that the active principle <strong>of</strong> gifblaar has cumulative effects, that is, it is<br />

inactivated in the body or excreted at a very slow rate. It is also possible that repeated small doses <strong>of</strong> the<br />

plant may cause progressive damage to organs <strong>of</strong> vital importance (heart) and that the sum total <strong>of</strong> these<br />

consecutive and progressive lesions is sufficient to cause death in spite <strong>of</strong> the fact that the active principle<br />

has been partly or completely excreted.<br />

There also was a certain amount <strong>of</strong> evidence that some animals became sensitized to the effects <strong>of</strong> the<br />

plant, unless we accept that these animals possessed and idiosyncrasy to gifblaar.<br />

Stoner, H. B. (1969). Studies on the mechanism <strong>of</strong> shock : the effect <strong>of</strong> trauma on the toxicity <strong>of</strong> 3,5<br />

dinitro-o-cresol and sodium fluoroacetate. British journal <strong>of</strong> experimental pathology 50, 277-284.<br />

Keywords: acute toxicity/mode <strong>of</strong> action/sodium fluoroacetate/fluoroacetate<br />

Sullivan, J. L., Smith, F. A., Wilkenfield, R. M., Garman, R. H., and Kostyniak, P. J. (1978).<br />

Mon<strong>of</strong>luoroacetate and trifluoroethanol as testicular <strong>poisons</strong> in the rat. Toxicology and applied<br />

phamacology 45, 291-292.<br />

Keywords: citrate/fluoroacetate/inhalation/mon<strong>of</strong>luoroacetate/poison/<strong>poisons</strong>/rats/reproductive<br />

effects/teratogenicity/testes/treatment/liver<br />

Abstract: During the course <strong>of</strong> investigations into the toxicology <strong>of</strong> aliphatic fluorocompounds, it was noted<br />

that trifluoroethanol (TFE) produced testicular damage in the rat. Fluoroacetate (FAc) is already recognised<br />

as a testicular poison, and it seemed worthwhile to compare effects <strong>of</strong> this nature produced by each<br />

compound. Previous work in our laboratory showed that 20 ppm <strong>of</strong> FAc in drinking water decreased the<br />

testis weight, elevated citrate concentration in the testis and produced early signs <strong>of</strong> seminiferous epithelial<br />

damage and involved both spermatocytes and spermatids. Early signs <strong>of</strong> regeneration were evident by 7<br />

days post-treatment, but this was not complete at 21 days. New information from a breeding experiment<br />

extend these morphological observations through a 10 week post treatment period. Also, reproductive<br />

performance was impaired after 1 week post treatment, completely inhibited 3 to 6 weeks post treatment<br />

and improved thereafter, being near normal when the experiment was terminated after 12 weeks. No<br />

unusual incidence <strong>of</strong> gross abnormalities was seen in the fetus taken 11 days post-conception. The 2-hour<br />

LC50 for male rats inhalating TFE was 4850 ppm (deaths were recorded at 24 hours post exposure).<br />

Damage to spermatocytes, spermatagonia and Sertoli cells were observed at 400 ppm for 2 hour, the lowest<br />

concentration used in the LC50 determination and persisted for at leat 86 hours post exposure. Single doses<br />

<strong>of</strong> 50 mg TFE/kg <strong>of</strong> injected ip induced similar testicular damage through 7 days postinjection. TFE was<br />

not defluorinated in vitro by a rat liver fraction capable <strong>of</strong> defluorinating FAc. TFE appears to differ<br />

somewhat from FAc in that a former compound affects spermatogonia whereas FAc does not.<br />

Sullivan, J. L., Smith, F. A., and Garman, R. H. (1979). Effects <strong>of</strong> fluoroacetate on the testis <strong>of</strong> the rat.<br />

Journal <strong>of</strong> reproduction and fertility 56, 201-207.<br />

Keywords: acute toxicity/mode <strong>of</strong> action/pathology/sodium<br />

fluoroacetate/treatment/metabolism/reproductive effects/Krebs cycle/rodents/sublethal effects<br />

Abstract: Rats receiving 20, 6.6 or 2.2 p.p.m. sodium fluoroacetate in the drinking water were killed daily<br />

during the 7 day treatment and at more widely spaced intervals in the succeeding 21 days. Testicular<br />

weight and ATP concentrations decreased in rats receiving 20 or 6 p.p.m fluoroacetate, while citrate<br />

concentrations were elevated and morphological dama was seen in the tests <strong>of</strong> all the treated rats. Initial<br />

cellular changes common to the three treatment groups included altered appearance and decreased numbers<br />

<strong>of</strong> spermatids, and formation <strong>of</strong> spermatid and spermatocyte giant cells. At the two higher concentrations,<br />

damage progressed to marked seminiferous tubule atrophy. Regeneration <strong>of</strong> the seminiferous tubules was<br />

complete by 7 days after treatment, in the rats given 2 p.p.m but regeneration was not complete by Day 21<br />

after treatment in those receiving the higher doses. Spermatogenesis was abnormal in some instances<br />

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during the regeneration period in these groups. The findings are consistent with impaired energy<br />

production via blockage <strong>of</strong> the Krebs cycle, and subsequent impairment <strong>of</strong> carbohydrate metabolism<br />

through the Embden-Meyerh<strong>of</strong> pathway.<br />

Suren, A. and Lambert, P. Monitoring <strong>of</strong> streams in the Haupiri forests after aerial 1080 drops. NIWA<br />

Client Report CHCO2/38, Project No. WCR02502, -17. 2002.<br />

Ref Type: Report<br />

Keywords: 1080/persistence in water/invertebrates/aquatic species/aerial control<br />

Abstract: Streams, sediment and aquatic invertebrate samples were monitored in following an aerial drop in<br />

Haupiri State Forest. No 1080 was detected in any <strong>of</strong> the water samples collected. No major changes to the<br />

invertebrate communities was observed, except for a decrease in the total number <strong>of</strong> taxa collected in some<br />

streams five days after the 1080 drop. There was also a slight decline in the number <strong>of</strong> EPT taxa collected 5<br />

days after the drop. Such decreases were not evident in the control site. However, both taxonomic richness<br />

and the number <strong>of</strong> EPT taxa found in streams 14 days after the drop were generally higher than those<br />

observed before the drop. It is thought that these changes most likely reflect effects <strong>of</strong> a small-scale flood<br />

event that occurred prior to the 1080 drop.<br />

Suren, A. and Bonnett, M. The effects <strong>of</strong> pollard baits containing sodium mon<strong>of</strong>luoroacetate (1080) on new<br />

Zealand freshwater crayfish (Paranephrops planifrons). NIWA Client Report: CHC2004-054<br />

May 2004<br />

NIWA Project: AHB04501, -22. 2004. National Institute <strong>of</strong> Water & Atmospheric <strong>Research</strong> Ltd<br />

10 Kyle Street, Riccarton, Christchurch<br />

P O Box 8602, Christchurch, New Zealand<br />

Phone +64-3-348 8987, Fax +64-3-348 5548<br />

www.niwa.co.nz.<br />

Ref Type: Report<br />

Keywords: baits/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/New<br />

Zealand/invertebrates/muscle/gut/analysis/tolerance/predators/secondary poisoning/poisoning/humans<br />

Abstract: The effects <strong>of</strong> pollard baits containing sodium mon<strong>of</strong>luoroacetate (1080) on New Zealand<br />

freshwater crayfish (Paranephrops planifrons) i<br />

This study assessed whether native crayfish (Paranephrops planifrons) consumed 1080 baits<br />

in preference to their natural food source <strong>of</strong> decomposing leaf litter and invertebrates, and<br />

determined whether ingestion <strong>of</strong> such pollard baits resulted in crayfish mortality. It also<br />

assessed whether residual 1080 remained in crayfish muscle and gut viscera after exposure <strong>of</strong><br />

these animals to 1080 baits.<br />

2. The experiment was conducted on the NIWA campus in Christchurch in a "stream simulator",<br />

consisting <strong>of</strong> a 5 m x 1 m long riffle section and 3.5 m long x 3.0 m wide pool (1 m deep)<br />

through which clean groundwater water flowed at a rate <strong>of</strong> 5 l s-1. Water was discharged to the<br />

reticulated sewer system to avoid accumulation <strong>of</strong> 1080 in the simulator. This simulator was<br />

divided into an upstream riffle section, and a downstream pool section. Twenty-five cages (15<br />

cm x 50 cm: mesh size 15 mm) were placed in each <strong>of</strong> these habitat types. Small plastic PVC<br />

pipes and large cobbles were also placed in each cage to give the crayfish shelter.<br />

3. Crayfish were collected from streams on the West Coast, and transported to Christchurch.<br />

Single crayfish were placed into each cage and left for 1 week to acclimate, after which time a<br />

single 1080 bait (mean weight = 6.4 g) containing c. 0.15% 1080 (i.e., 9.6 mg) was added to<br />

20 <strong>of</strong> the cages. Non-toxic baits were also added to 5 control cages within each habitat. A<br />

further 5 crayfish were kept in separate aquaria for the duration <strong>of</strong> the experiment to act as a<br />

double control. Replicate crayfish were collected at random from both the riffle and pool<br />

habitats after 1, 2, 4 and 8 days and frozen pending analysis <strong>of</strong> residual 1080 in their viscera or<br />

tail muscle. The crayfish fed the non-toxic baits, and those placed in the aquaria were also<br />

collected after 8 days, frozen and analysed for presence <strong>of</strong> 1080. Water samples were also<br />

collected at regular intervals for analysis <strong>of</strong> dissolved 1080.<br />

4. Observations <strong>of</strong> the crayfish over time showed that some had moved the pollard baits into or<br />

near their PVC pipes, while others had consumed some baits. The fact that detritus was also<br />

present in the cages suggested that pollard baits may represent a more favourable food item to<br />

crayfish than detritus. Despite the direct consumption <strong>of</strong> 1080 baits by crayfish, no mortality<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

was observed during the study, even after 8 days when the experiment was terminated.<br />

5, Analysis <strong>of</strong> crayfish viscera and tail muscle confirmed that crayfish had consumed baits. The<br />

highest 1080 concentration found in the viscera was 3.3 mg kg-1 <strong>of</strong> body tissue, while up to 5<br />

mg kg-1 <strong>of</strong> 1080 was found in the tail muscle. There was no significant difference in<br />

concentrations <strong>of</strong> 1080 in animals placed in either pools or riffles, and 1080 concentrations<br />

decreased over time. The highest total concentration <strong>of</strong> 1080 found within a particular crayfish<br />

(7.7 mg kg-1) suggested that c. 80% <strong>of</strong> a pollard bait had been consumed by this individual,<br />

assuming that each bait contained 9.6 mg <strong>of</strong> 1080.<br />

6. The amount <strong>of</strong> 1080 found in the tail muscle was significantly related to the amount found<br />

within the viscera, suggesting that what each animal consumed was being transferred to<br />

muscle tissue. The 1080 body burden <strong>of</strong> animals collected 2 and 4 days after being exposed to<br />

the 1080 baits was related to their body size, suggesting that larger animals consumed more <strong>of</strong><br />

the baits. The significant decline in 1080 concentration in the muscle tissue between days 4<br />

and 8 suggests that crayfish that consumed sub-lethal doses <strong>of</strong> 1080 were able to successfully<br />

metabolise this compound.<br />

7. Water samples collected from the outlet <strong>of</strong> the stream simulator for 1080 analysis showed that<br />

the highest concentration <strong>of</strong> 1080 (1.1 µg l-1) occurred after 2 days. No residual 1080 was<br />

detected in the water after 8 days.<br />

8. Crayfish that were fed control (non-toxic) baits had no residual 1080 in their viscera or tail<br />

muscle, despite being exposed to the very low concentrations <strong>of</strong> 1080 in the water within the<br />

stream simulator. Lack <strong>of</strong> detectable 1080 in control animals suggests that contaminant<br />

loadings in the animals exposed to the toxic baits reflected direct consumption <strong>of</strong> 1080 pollard<br />

baits, and not exposure to water containing traces <strong>of</strong> 1080.<br />

9. Lack <strong>of</strong> crayfish mortality may reflect their naturally high tolerance to 1080, or the fact that<br />

they were exposed to only 1 pollard bait. It is, however, theoretically possible that crayfish in<br />

natural streams could encounter more than 1 pollard bait within their territory, and consume<br />

them. Whether consumption <strong>of</strong> more than 1 bait by an individual is enough to cause mortality<br />

is unknown.<br />

10. The main ecological implication <strong>of</strong> crayfish consuming 1080 baits is the potential for<br />

predators becoming susceptible to secondary poisoning. The main predators <strong>of</strong> crayfish are<br />

eels, trout and humans. A theoretical risk may exist to humans if they consume crayfish<br />

caught from within operational areas and which still contain a significant body-burden <strong>of</strong><br />

residual 1080.<br />

11. Such risks could be minimised by changes to operational practices. In operational areas where<br />

crayfish are likely to occur, aerial flight plans could be varied to minimise the chances <strong>of</strong><br />

overflying streams in the latter part <strong>of</strong> the day, as crayfish are mostly nocturnal feeders. 1080<br />

leaches rapidly from pollard baits, so baits that land in streams in the early part <strong>of</strong> the day<br />

would have little residual 1080 left in them after sunset. The risk <strong>of</strong> crayfish accumulating<br />

1080 from such baits is greatly reduced. Consideration should also be taken to warn the public<br />

against harvesting crayfish from streams within any operational areas for a period <strong>of</strong> time after<br />

the cessation <strong>of</strong> the aerial drop.<br />

Suzuki, T., Akiyama, S., Yamazaki, O., Nara, K., Nakao, Y., and Fukuda, H. (1975). Induction and<br />

stabilization <strong>of</strong> yeast aconitase activity by fluorocitrate. Agricultural and Biological Chemistry 39, 97-103.<br />

Keywords: metabolism/mode <strong>of</strong> action/aconitase/fluorocitrate/bacteria/inhibition/fluoroacetate<br />

Abstract: Both fluorocitrate and fluoroacetate acted on yeast aconitase as an inducer and a stabilizer <strong>of</strong> the<br />

enzyme. Fluoroacetate appeared to function after conversion to fluorocitrate in the cells. Inhibitors <strong>of</strong><br />

protein synthesis and terminal respiratory system showed a strong inhibitory effect on the inductive<br />

formulation <strong>of</strong> aconitase. In addition, these fluorocompounds were also found to induce various microbial<br />

aconitases.<br />

Swanson, R. A. and Graham, S. H. (1994). Fluorocitrate and fluoroacetate effects on astrocyte metabolism<br />

in vitro. Brain research 664, 94-100.<br />

Keywords: mode <strong>of</strong> action/metabolism/Krebs cycle/fluorocitrate/fluoroacetate/brain<br />

Abstract: The Krebs cycle inhibitor fluorocitrate (FC) and its precursor fluoroacetate (FA) are taken up in<br />

brain preferentially by glia. These compounds are used experimentally to inhibit glial metabolism in situ.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

The actions <strong>of</strong> these agents have been attributed to both the disruption <strong>of</strong> carbon flux through the Krebs<br />

cycle and to impairment <strong>of</strong> ATP production. We used primary astrocyte cultures to evaluate these two<br />

possible modes <strong>of</strong> action. Astrocyte ATP levels exhibited little or no reduction during incubation with 0.5<br />

mM FC or 25 mM FA. Correspondingly, FC and FA caused less than 30% reductions in glutamate uptake<br />

(P > 0.05), an important energy-dependent astrocyte function. Carbon flux through the Krebs cycle was<br />

assessed by measuring astrocyte glutamine production in the absence <strong>of</strong> exogenous glutamate or aspartate.<br />

Under these conditions, glutamine production was reduced 65 +/- 5% by 0.5 mM FC and 61 +/- 3% by 25<br />

mM FA (P < 0.01). In contrast, FC and FA had no effect on glutamine production when 50 mu M<br />

glutamate was provided in the media. These findings suggest that the metabolic effects <strong>of</strong> FC and FA on<br />

astrocytes in vivo result from impairment <strong>of</strong> carbon flux through the Krebs cycle, and not from impairment<br />

<strong>of</strong> oxidative ATP production.<br />

Sweetapple, P. J. (1995). Effectiveness <strong>of</strong> foliage bait poisoning for deer : development <strong>of</strong> a plasma marker<br />

for deer and a toxic field trial. (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Lincoln.)<br />

Keywords: field efficacy/deer/1080<br />

Abstract: Objectives : To determine whether orally administered iophenoxic acid provides an effective<br />

plasma marker for red deer and identify the quantities needed per bait for use in non-toxic bait-acceptance<br />

field trials; To determine the percentage <strong>of</strong> a low-density forest-dwelling deer population killed using toxic<br />

foliage baits and the cost <strong>of</strong> achieving that level <strong>of</strong> control.<br />

Conclusion : Iophenoxic acid is an effective plasma marker for use in red deer bait acceptance trials, with<br />

only 0.3 mg/kg required to mark red deer for at least 40 days, and 3-6 mg/kg probably marking red deer for<br />

at least 6 months. The plasma marker can be used to determine the number <strong>of</strong> marked baits eaten by red<br />

deer; The cost <strong>of</strong> baiting forest with 2 baits/ha is likely to be about $6.00/ha, compared with about $20/ha<br />

for aerial poisoning. Actual cost will depend on wage rates, accessibility and topography <strong>of</strong> the poison<br />

area, and availability <strong>of</strong> broadleaf material; At least some deer accept foliage baits even when deer densities<br />

are low. Deer did not appear to selectively avoid baited leaves. Because shade-grown broadleaf foliage<br />

retains toxic leafs longer than other foliage types and is <strong>of</strong> similar palatability, it is the best broadleaf<br />

foliage type for 1080 foliage baits; The trial did not reduce deer densities in the poison area, but this failure<br />

may simply reflect the low concentration <strong>of</strong> 1080 in the gel. The large number <strong>of</strong> baits browsed indicate<br />

that it is likely that some deer would have been killed had the toxic gel contained 10% 1080.<br />

Sykes, T. R. (1986). Synthesis and murine tissue uptake <strong>of</strong> sodium [18F] fluoroacetate. Int J Rad Appl<br />

Instrum [B] 13, 497-500.<br />

Keywords: fluoroacetate/metabolism/excretion<br />

Sykes, T. R., Quastel, J. H., Adam, M. J., Ruth, T. J., and Noujaim, A. A. (1987). The disposition and<br />

metabolism <strong>of</strong> [ 18 F]-fluoroacetate in mice. Biochemical archives 3, 317-323.<br />

Keywords: metabolism/persistence in animals/defluorination/rodents/excretion<br />

Abstract: Very little is known about the in vivo behavior <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (FAc). We have<br />

studied the disposition, excretion and metabolism <strong>of</strong> this compound up to four hours after the intravenous<br />

injection <strong>of</strong> the (18F)-labelled material <strong>of</strong> mice. There was no tissue specific accumulation <strong>of</strong> the<br />

compound itself, however bone accumulation <strong>of</strong> (18F) activity was significant. Comparison to (18F)-NaF<br />

data and the demonstration <strong>of</strong> (18F)-fluoride in the blood supported the concept <strong>of</strong> metabolic defluorination<br />

<strong>of</strong> FAc.<br />

Szerb, J. C. and Issekutz, B. (1987). Increase in the stimulation-induced overflow <strong>of</strong> glutamate by<br />

fluoroacetate, a selective inhibitor <strong>of</strong> the glial tricarboxylic cycle. Brain research 410, 116-120.<br />

Keywords: mode <strong>of</strong> action/brain/Krebs cycle/fluoroacetate<br />

Abstract: Fluoroacetate is known to be taken up selectively by glia, where after forming fluorocitrate, it<br />

inhibits the tricarboxylic acid cycle. Since uptake into glia has a major role in the inactivation <strong>of</strong><br />

synaptically released glutamate, the effect <strong>of</strong> fluoroacetate on the overflow <strong>of</strong> glutamate evoked by<br />

electrical field stimulation in slices <strong>of</strong> rat hippocampus was investigated. In agreement with previous<br />

reports, 1 mM fluoroacetate reduced the release and content <strong>of</strong> glutamine, but increased only slightly the<br />

overflow <strong>of</strong> glutamate induced by stimulation. If, however, 0.5 mM glutamine was added to the superfusion<br />

fluid, fluoroacetate nearly tripled the overflow <strong>of</strong> glutamate evoked by electrical field stimulation. The<br />

large glutamate overflow due to field stimulation in the presence <strong>of</strong> fluoroacetate was fully Ca2+ -<br />

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1080 Reassessment Application October 2006<br />

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dependent. Results confirm the major role <strong>of</strong> glia in the inactivation <strong>of</strong> glutamate. The absence <strong>of</strong> such an<br />

uptake may contribute to the in vivo convulsive effect <strong>of</strong> fluoroacetate.<br />

Szerb, J. C. and O'Regan, P. A. (1988). Increase in the stimulation-induced overflow <strong>of</strong> excitatory amino<br />

acids from hippocampal slices : interaction between low glucose concentration and fluoroacetate.<br />

Neuroscience letters 86, 207-212.<br />

Keywords: mode <strong>of</strong> action/fluoroacetate/brain<br />

Tahori, A. S. (1963). Selection for a fluoroacetate resistant strain <strong>of</strong> house flies and investigation <strong>of</strong> its<br />

resistance pattern. Journal <strong>of</strong> economic entomology 56, 67-69.<br />

Keywords: fluoroacetate/resistance/invertebrates<br />

Tahori, A. S. (1966). Changes in the resistance pattern <strong>of</strong> a fluoroacetate-resistant fly strain. J Econ<br />

Entomol 59, 462-464.<br />

Keywords: resistance/invertebrates/fluoroacetate<br />

Abstract: Selection <strong>of</strong> an insecticide-susceptible house fly, Musca domestica L., strain with fluoroacetate<br />

produced moderate resistance t<strong>of</strong>luoroacetate during the first 65 genertions <strong>of</strong> selection. After the 75th<br />

generation, resistance increased sharply, reaching 500 µg <strong>of</strong> fluoroacetate per fly at the 81st generation <strong>of</strong><br />

selection.<br />

Selection with fluoroacetate for 57 generations caused a 200-fold increase in DDT-resistance. After<br />

further selection, this high level dropped gradually to 8-fold only. An 8000-fold increase in resistance to<br />

dieldrin was observed after 25 generations <strong>of</strong> selection with fluoroacetate. During the nex 20 generations<br />

this high level <strong>of</strong> dieldrin resistance declined considerably.<br />

When selection with fluoroacetate was discontinued after the 17th generation, the levels <strong>of</strong> DDT and<br />

dieldrin resistance were maintained for another 40 generations. Later on they declined, while always<br />

remaining above those <strong>of</strong> the corresponding strain, selected continuously with fluoroacetate.<br />

No resistance developed to the organophosphorus insecticides parathion, malathion, and trichlorfon.<br />

Taitelman, U., Roy, A., Raikhlin-Eisenkraft, B., and H<strong>of</strong>fer, E. (1983). The effect <strong>of</strong> monoacetin and<br />

calcium chloride on acid-base balance and survival in experimental sodium fluoroacetate poisoning.<br />

Archives <strong>of</strong> toxicology Supplement 6, 222-227.<br />

Keywords: treatment/metabolism/cats/monoacetin/sodium fluoroacetate/fluoroacetate/poisoning<br />

Taitelman, U., Roy (Shapira), A., and H<strong>of</strong>fer, E. (1983). Fluoroacetamide poisoning in man: the role <strong>of</strong><br />

ionized calcium. Archives <strong>of</strong> toxicology Suppl. 6, 228-231.<br />

Keywords: fluoroacetamide/poisoning/humans/treatment/cardiac/heart<br />

Abstract: Two cases are reported <strong>of</strong> severe acute fluoroacetamide poisoning in man, with successful<br />

treatment <strong>of</strong> the life-threatening cardiac arrythmias by the administration <strong>of</strong> calcium chloride. The<br />

arrythmias were preceded by prolongation <strong>of</strong> the QT interval in the ECG. Calcium chloride therapy<br />

restored to normal the markedly prolonged QT interval.<br />

Takeuchi, Y., Ogura, H., Ishii, Y., and Koizumi, T. (1990). Chemistry <strong>of</strong> novel compounds with<br />

multifunctional carbon structure: VI. Synthetic studies and fluorine-19 NMR investigation <strong>of</strong> novel<br />

alpha,alpha-disubstituted fluoroacetates. Chemical and Pharmaceutical Bulletin (Tokyo) 38, 2404-2408.<br />

Keywords: chemistry/NMR/fluoroacetate<br />

Abstract: As a part <strong>of</strong> our work on synthetic studies <strong>of</strong> chiral mon<strong>of</strong>luoro compounds and molecular design<br />

<strong>of</strong> efficient reagents for optical purity determination, we focused on novel alpha,alpha-disubstituted alphafluoroacetic<br />

acids (8a-d) (R-1 = Me, Ph; R-2 = C tbd CPh, Me, Bu). The ethyl esters (13a-d) were prepared<br />

by introduction <strong>of</strong> alkyl groups into the appropriate alpha-keto acids (9a,b) followed by fluorination <strong>of</strong> the<br />

corresponding hydroxy-esters (12a-d) with diethylaminosulfur trifluoride (DAST). For comparison with<br />

Mosher's reagent (2-methoxy-2-trifluoromethylphenylacetic acid, (MTPA)), the ethyl esters (13a-d) were<br />

converted into three representative diastereoisomers, (14a-d), (15a-d), and (16a-d), and 19F-nuclear<br />

magnetic resonance (19F-NMR) chemical shift differences between pairs <strong>of</strong> diastereoisomers (DELTAdelta)<br />

were obtained. These alpha,alpha-disubstituted alpha-fluoroacetate derivatives have much larger<br />

DELTA-delta values than the corresponding derivatives <strong>of</strong> MTPA, which strongly indicates that the acids<br />

(8a-d) can potentially be better reagents for ee determination than MTPA. The influence on the DELTA-<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

delta values <strong>of</strong> the steric effects which arise upon introduction <strong>of</strong> the two substituents (R-1 and R-2) on the<br />

fluorine-bearing chiral center is also discussed<br />

Tamura, T., Wada, M., Esaki, N., and Soda, K. (1995). Synthesis <strong>of</strong> fluoroacetate from fluoride, glycerol,<br />

and β-hydroxypyruvate by Streptomyces cattleya. Journal <strong>of</strong> bacteriology 177, 2265-2269.<br />

Keywords: occurrence in nature/NMR/product chemistry/fluoroacetate/fluoride/bacteria/biosynthesis<br />

Abstract: Streptomyces cattleya produces fluoroacetate and 4-fluorothreonine from inorganic fluoride<br />

added to the culture broth. We have shown by F-19 nuclear magnetic resonance (NMR) spectrometry that<br />

fluoroacetate is accumulated first in the culture broth and that accumulation <strong>of</strong> 4-fluorothreonine is next. To<br />

show precursors <strong>of</strong> the carbon skeleton <strong>of</strong> fluoroacetate, we carried out tracer experiments with various C-<br />

14- and C-13-labeled compounds. Radioactivity <strong>of</strong> [U-C-14]glucose, [U-C-14]glycerol, [U-C-14]serine,<br />

and [U-C-14]beta-hydroxypyruvate was incorporated into fluoroacetate to an extent <strong>of</strong> 0.2 to 0.4%,<br />

whereas [3-C-14]pyruvate, [2,3-C-14]succinate, and [U-C-14]aspartate were less efficiently incorporated<br />

(0.04 to 0.08%). The addition <strong>of</strong> [2-C-13]glycerol to the mycelium suspension <strong>of</strong> Streptomyces cattleya<br />

caused exclusive enrichment <strong>of</strong> the carboxyl carbon <strong>of</strong> fluoroacetate with C-13; about 40% <strong>of</strong> carboxyl<br />

carbon <strong>of</strong> fluoroacetate was labeled with C-13. We studied the radioactivity incorporation <strong>of</strong> [3-C-14]-, [U-<br />

C-14]-, and [1-C-14]beta-hydroxypyruvates to show that C-2 and C-3 <strong>of</strong> beta-hydroxypyruvate are<br />

exclusively converted to the carbon skeleton <strong>of</strong> fluoroacetate. These results suggest that the carbon skeleton<br />

<strong>of</strong> fluoroacetate derives from C-1 and C-2 <strong>of</strong> glycerol through beta-hydroxypyruvate, whose hydroxyl<br />

group is eventually replaced by fluoride<br />

Tamura, T., Sawamoto, Y., Kuriyama, T., Oba, K., Tanaka, H., and Inagaki, K. (2003). Cosynthesis <strong>of</strong><br />

mon<strong>of</strong>luoroacetate and 4-fluorothreonine by resting cells <strong>of</strong> blocked mutants <strong>of</strong> Streptomyces cattleya<br />

NRRL8057. Journal <strong>of</strong> Moleclar Catalysis B-Enzymatic 23, 257-263.<br />

Keywords: mon<strong>of</strong>luoroacetate/fluoride/assay/enzyme/bacteria/biosynthesis<br />

Abstract: Streptomyces cattleya NRRL 8057 produces mon<strong>of</strong>luoroacetate and 4-fluorothreonine from<br />

inorganic fluoride. Mutants blocked in fluorometabolite production were prepared by chemical<br />

mutagenesis, and cosynthesis experiments with these blocked mutants were carried out by suspending cells<br />

<strong>of</strong> one blocked mutant in the supernatant broth <strong>of</strong> another blocked mutant. The harvest age <strong>of</strong> the cells, pH<br />

<strong>of</strong> the buffer, potassium fluoride concentration and glycerol supplementation were optimized for the<br />

mon<strong>of</strong>luoroacetate production by a resting-cell suspension <strong>of</strong> S. cattleya. Successful cosynthesis with pairs<br />

<strong>of</strong> the mutants characterized four distinctive blocked sites in the order N-82, N-44, N-43 and N-47.<br />

Additional preparation <strong>of</strong> blocked mutants by UV irradiation and their cosynthesis assay confirmed that U-<br />

303, U-304, U-400 and U-500 were blocked in later steps than N-47. O'Hagan et al. recently proposed that<br />

fluoroacetaldehyde, the hypothetical precursor <strong>of</strong> mon<strong>of</strong>luoroacetate and 4-fluorothreonine, derives from<br />

5'-fluoro-5-deoxyadenosine, the first fluorinated metabolite synthesized from S-adenoSyl-L-methionine and<br />

inorganic fluoride by the novel enzyme 'fluorinase'. We were able to detect fluorinase activity in crude<br />

extracts <strong>of</strong> wild type and N-47 mutant strains, but not in the other mutant strains whose blocked steps<br />

flanked that <strong>of</strong> N-47.<br />

Tanada, M, Miyoshi, T., Nakamura, T., and Tanada, S. (1991). Adsorption removal <strong>of</strong> benzalkonium<br />

chloride by granular activated carbon for medical waste water treatment. Asia Pac.Public Health 5, 27-31.<br />

Keywords: treatment/poisoning/antidote<br />

Abstract: The adsorption removal <strong>of</strong> benzalkonium chloride disinfectant by granular activated carbon is<br />

discussed. The adsorption isotherm <strong>of</strong> benzalkonium chloride was expressed by the Freundlich equation. A<br />

significant correlation was found between the amount <strong>of</strong> benzalkonium chloride adsorbed in less than 1000<br />

ppm <strong>of</strong> equilibrium concentration and the micropore volume <strong>of</strong> activated carbon. As for the adsorption rate,<br />

a change in intraparticle diffusiveness was found with increasing adsorption ratio. No significant<br />

correlation between the value <strong>of</strong> intraparticle diffusiveness and the properties <strong>of</strong> activated carbon was<br />

found. It was concluded that the micropore volume <strong>of</strong> activated carbon was the dominant factor in the<br />

adsorption removal <strong>of</strong> benzalkonium chloride by granular activated carbon.<br />

Tani, Y., Sakai, Y, and Chou, S.-G (1990). Production <strong>of</strong> citric acid from methanol by a fluoroacetateresistant<br />

mutant <strong>of</strong> Candida sp. Y-1. Appl.Microbiol.Biotechnol. 34, 5-9.<br />

Keywords: citric acid<br />

Abstract: Fermentative production <strong>of</strong> citric acid from methanol by an isolated yeast, Candida sp. Y-1, was<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

investigated using a medium containing fluoroacetate, a potential inhibitor <strong>of</strong> aconitase. Culture conditions<br />

were optimized, and the results showed that efficient production <strong>of</strong> citric acid required several factors; (1)<br />

the optimum concentration <strong>of</strong> fluoroacetate, (2) an addition <strong>of</strong> yeast extract with corn steep liquor, (3) a low<br />

nitrogen source concentration, and (4) strictly aerobic conditions. We then isolated a fluoroacetate-resistant<br />

mutant strain MA92 with threefold higher citric acid productivity than the wild strain. This mutant strain<br />

had lower aconitase activity than the wild strain and produced 4.6 g/l citric acid from methanol after 4 days<br />

<strong>of</strong> culture.<br />

Taylor, R. Possums and poison: it's time to ban 1080. Organic NZ May/June 2002, 12-13. 2002.<br />

Ref Type: Magazine Article<br />

Keywords: possums/poison/1080/anti-1080<br />

Taylor, W. M., D'Costa, M., Angel, A, and Halperin, M. L. (1977). Insulin-like effects <strong>of</strong> fluoroacetate on<br />

lipolysis and lipogensis in adipose tissue. Canadian Journal <strong>of</strong> Biochemistry 55, 982-987.<br />

Keywords: fluoroacetate/mode <strong>of</strong> action/inhibition/aconitase/metabolism<br />

Abstract: In summary, there is a parallel between the observed effects <strong>of</strong> fluoroacetate reported in this<br />

paper and the metabolic actions <strong>of</strong> insulin. Both agents lower cAMP, decrease lipolysis and lipolytic<br />

production, accelarte glucose transport , activate pyruvate dehydrogenase, and increase lipogenesis.<br />

However, there are ceratin quantitative differences observed between the effects <strong>of</strong> these agents such as the<br />

fluoroacetate-induced inhibition <strong>of</strong> aconitase and pyruvate dehydrogenase kinase and the insulin-induced<br />

activation <strong>of</strong> a low Km phosphodiesterase. However, where the actions are similar, it is tempting to<br />

speculate that a primary event such as the reduction in cAMP could be responsible for the analbolic pattern<br />

<strong>of</strong> glucose metabolism observed.<br />

Tecle, B. and Casida, J. E. (1989). Enzymatic defluorination and metabolism <strong>of</strong> fluoroacetate,<br />

fluoroacetamide, fluoroethanol, and (-)-erythro-fluorocitrate in rats and mice examined by 19 F and 13 C<br />

NMR. Chemical research in toxicology 2, 429-435.<br />

Keywords:<br />

metabolism/fluoroacetamide/NMR/treatment/fluoroacetate/kidney/excretion/fluoride/fluorocitrate/mode <strong>of</strong><br />

action<br />

Abstract: Fluoroacetate administered intraperitoneally (ip) to rats and mice is defluorinated to give fluoride<br />

ion evident in urine and kidney by 19F NMR. The use <strong>of</strong> (2-13C)-,(1,2-13C)- and (1,2-14C) fluoroacetate,<br />

prepared from isotopically labeled glycine, combined with 13C NMR as TLC radioactography,<br />

respectively, reveals a complex mixture <strong>of</strong> urinary metabolites including S-(carboxymethyl) conjugate<br />

complex in rats and mice and sulfoxidation products there<strong>of</strong> in rats. Direct 13C NMR examination <strong>of</strong> the<br />

bile following treatment with (2-13C) fluoroacetate shows the presence <strong>of</strong> S-(carboxymethyl) glutathoine<br />

or a related conjugate and an O-conjugate <strong>of</strong> fluoroacetate. Incubation <strong>of</strong> (13C) fluoroacetate with rat and<br />

mouse liver cytosol involves formation <strong>of</strong> S- ((13C) carboxymethyl)g glutathione and fluoride ion.<br />

Fluorocitrate is also detected by 19 F NMR examination <strong>of</strong> fluoroacetate incubations with mouse liver<br />

cytosol. Fluoroacetamide administered ip to rats and mice yields urinary fluoride ion formed via<br />

fluoroacetate which is liberated on hydrolysis by and organophosphate-sensitive amidase. 19F NMR<br />

chemical shifts <strong>of</strong> other metabolites <strong>of</strong> Fluoroacetamide are consistent with fluoroacetohydroxamic acid in<br />

the liver <strong>of</strong> mice and Fluorocitrate in the urine <strong>of</strong> rats. Fluoroethanol gives urinary fluoroacetate and<br />

fluoride ion in rats and mice and is converted to fluoroacetaldehyde by mouse and rat liver microsomes (-)<br />

and (+)-erythro-fluorocitrates administered ip rats yield mostly the parent compounds in urine at 6 h with<br />

increasing amounts <strong>of</strong> fluoride ion thereafter 19F NMR establishes that rat and mouse liver cytosol<br />

defluorinate (-) but not (+)-erythro-Fluorocitrate and pig heart aconitase also defluorinates (-) eryht<strong>of</strong>luorocitrate.<br />

Metabolic defluorination <strong>of</strong> fluoroacetate and its progenitors, fluoroacetamide and<br />

fluoroethanol, is therefore attributable to both conjugation <strong>of</strong> fluoroacetate with glutathione and conversion<br />

to (-) erythro-fluorocitrate which is both an inhibitor <strong>of</strong> and a substrate for aconitase. 13C NMR spectra <strong>of</strong><br />

urine <strong>of</strong> rats and mice poisoned with fluoroacetate or (-) erythro fluorocitrate show elevated citrate and<br />

glucose and diminished urea consistent with disruption in the tricarboxylic acid cycle and ammonia<br />

metabolism.<br />

Temple, W. A. and Edwards, I. R. (1985). Toxic ducks : 1080 residues in game birds : an exercise in<br />

applied toxicology. Veterinary and human toxicology 27, 20-21.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: non-target species/birds/1080/poisoning/humans/secondary poisoning/residues<br />

Abstract: Conclusions from this study are that it is unlikely that anyone would suffer adversely from<br />

consuming a normal cooked portion <strong>of</strong> SMFA-killed duckmeat. More information about the kinetics <strong>of</strong><br />

SMFA in man would be needed to determine levels <strong>of</strong> this substance when poisonings occur to achieve a<br />

better understanding and management <strong>of</strong> human toxicity.<br />

Teplova, V. V., Evtodienko, Y. V., Kholmukhamedov, E. L., Sergejenko, N. G., and Goncharov, N. V.<br />

(1992). Effect <strong>of</strong> fluorocitrate on substrate oxidation and Ca 2+ transporting systems <strong>of</strong> rat liver<br />

mitochondria. Tsitologiia 34, 71-75.<br />

Keywords: fluorocitrate/liver/inhibition<br />

Abstract: The effect <strong>of</strong> fluorocitrate on oxidative reactions and energy production systems <strong>of</strong> rat liver<br />

mitochondria has been studied. It was shown that oxidation <strong>of</strong> endogeneous substrates and malate with<br />

pyruvate as well as the phosphorylation <strong>of</strong> the added ADP were inhibited by fluorocitrate. Inhibition <strong>of</strong><br />

oxygen consumption by fluorocitrate induced the efflux <strong>of</strong> Ca 2+ ions from mitochondria and a decrease in<br />

the Ca 2+ -accumulating capacity. The effect <strong>of</strong> fluorocitrate on Ca 2+ transport in mitochondria is due to<br />

activation <strong>of</strong> the Ca-efflux pathway in those sensitive to Ruthenium red.<br />

Tepperman, H. M. and Tepperman, J. (1955). unknown. American journal <strong>of</strong> physiology 180, 511.<br />

Keywords: liver/citrate/fluoroacetate<br />

Terada, H., Miyoshi, T., Imaki, M., Nakamura, T., and Tanada, S. (1994). Studies on in vitro paraquat and<br />

diquat removal by activated carbon. Tokushima J.Exp.Med. 41, 31-40.<br />

Keywords: poisoning/treatment/antidote<br />

Abstract: The adsorption characteristics <strong>of</strong> paraquat and diquat onto activated carbon in vitro were<br />

discussed for the primary treatment <strong>of</strong> acute poisoning by accidental, suicidal or homicidal ingestion <strong>of</strong><br />

paraquat containing herbicides. Paraquat was adsorbed onto activated carbon more abundantly and more<br />

rapidly in physiological saline solution than that in artificial gastric juice and distilled water. Most suitable<br />

solvent for paraquat removal by activated carbon was physiological saline solution (0.9% sodium chloride<br />

solution). No significant correlation was observed between the ability <strong>of</strong> paraquat removal and the<br />

properties <strong>of</strong> adsorbent. Paraquat was preferentially adsorbed onto activated carbon in the mixed solution.<br />

The adsorption abilities by activated carbon (the removal ratio, the amount adsorbed and the adsorption<br />

rate) for paraquat were larger than those for diquat, and it was enhanced by added sodium chloride and<br />

added magnesium sulfate. Enhancing effect for adsorption removal was proportional to the saline<br />

concentration. As addition <strong>of</strong> salts into carbon suspension enhanced the adsorption ability, it will contribute<br />

to the effective treatment <strong>of</strong> acute poisoning.<br />

Teran Mogro, G. (1988). Morbidity due to chemical pesticides. Revista Cubana de Higiene y<br />

Epidemiologia 26, 107-122.<br />

Thomas, M. D. (1994). Possum control in native forest using sodium mon<strong>of</strong>luoroacetate (1080) in bait<br />

stations. Proceedings <strong>of</strong> the New Zealand Plant Protection Conference 47, 107-111.<br />

Keywords: field efficacy/possums/1080/sodium fluoroacetate/treatment<br />

Abstract: <strong>Control</strong> <strong>of</strong> brushtail possums (Trichosurus vulpecula) using baits containing sodium fluoroacetate<br />

was investigated in New Zealand during April 1992, December 1993 and February 1994. Populations were<br />

reduced to similiar levels to those achieved with aerial application, provided the possums were fed nontoxic<br />

cereal baits before treatment. Compared with aerial treatment, the amount <strong>of</strong> pesticide used was<br />

reduced by more than 90%.<br />

Thomas, M. D. (1998). Optimising the use <strong>of</strong> bait stations to control possums in New Zealand native<br />

forests. In '11th Australian Vertebrate Pest Conference, Bunbury, Western Australia, 3-8 May 1998 :<br />

programme and proceedings.'. pp. 337-340. (Agriculture Western Australia: Forrestfield.)<br />

Keywords: field efficacy/possums/1080<br />

Abstract: Possum control in native forest is essential to reduce damage to native flora and fauna, so the<br />

development <strong>of</strong> more efficient control methods is a high priority. We investigated methods to improve<br />

control efficiency using toxic baits to fed from bait stations. Results showed that by using the<br />

recommended bait station spacing grid <strong>of</strong> 150-m, and baits containing 0.15% 1080, a mean possum kill <strong>of</strong><br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

83% could be achieved after 3 weeks <strong>of</strong> prefeeding with non-toxic baits. With no prefeeding a mean kill <strong>of</strong><br />

68% was achieved. Prefeeding gave 70% increase in the amount <strong>of</strong> 1080 baits taken from the bait stations.<br />

Prefeeding also resulted in 95% <strong>of</strong> the 1080 baits being taken from the bait stations on the first night <strong>of</strong><br />

baiting. With no prefeeding 1080 baits were taken gradually over a 50 day baiting period with increased<br />

the likelihood <strong>of</strong> baits decaying and becoming less palatabel. When Talon followed 1080 baiting, there was<br />

no further reduction in possum numbers but rat numbers were reduced a further 23%. More research needs<br />

to be conducted to improve cost-efficiency and to monitor non-target and environmental effects when feed<br />

toxic baits from bait stations.<br />

Thompson, C. C. (1959). Determination <strong>of</strong> fluoroacetic acid and fluoroacetamide in plant material.<br />

J.Sci.Food Agr. 10, 388-394.<br />

Keywords: fluoroacetamide/fluoride/analysis<br />

Abstract: FCH2CO2H and FCH2CONH2 residues are extd. from the plant material and the ext. is subjected<br />

to chromatography on a silica gel column, which removes fluorides and fluosilicates. The acids are detd. as<br />

F, which is released by fusion with CaO. To det. FCH2CONH2 in plant exts., the ext. is treated with the<br />

anion exchange resin De-acidite FF to remove inorg. and org. F-contg. plant constituents, and<br />

FCH2CONH2 is detd. as F. With a 100-g. sample, 1 p.p.m. can be assayed with an accuracy <strong>of</strong> 13% and<br />

0.1p.p.m. with an accuracy <strong>of</strong> 50%<br />

Thompson, J., Toms, B, Akers, D, Bell, R., Te Kloot, J., Cross, J., and Wingrave, S. Review <strong>of</strong> 1080 use in<br />

Queensland. 1-65. 1995. Queensland, Land Protection Branch, Department <strong>of</strong> Lands.<br />

Ref Type: Report<br />

Keywords: 1080/pigs/dogs/foxes<br />

Tietjen, H., Deines, F., and Stephensen, W. (1988). Sodium mon<strong>of</strong>luoroacetate (1080) : a study <strong>of</strong> residues<br />

in arctic fox muscle tissues. Bulletin <strong>of</strong> environmental contamination and toxicology 40, 707-710.<br />

Keywords: persistence in animals/mammals/1080/treatment<br />

Abstract: This study provides data on the efficacy <strong>of</strong> 1080 against arctic fox, the impacts <strong>of</strong> treatment on<br />

non-target raptors and scavengers, and investigates the posttreatment recovery <strong>of</strong> specific prey species.<br />

Tisdale, M. J. and Brennan, R. A. (1985). Role <strong>of</strong> fluoroacetate in the toxicity <strong>of</strong> 2-fluoroethylnitrosoureas.<br />

Biochemical Pharmacology 34, 3323-3327.<br />

Keywords: fluoroacetate/treatment/citrate/heart/kidney/liver/metabolism<br />

Abstract: The possible role <strong>of</strong> fluoroacetate in the toxicity and antitumour activity <strong>of</strong> the<br />

fluoroethylnitrosoureas, BFNU and FCNU has been studied in CBA mice bearing the TLX5 lymphoma<br />

eitehr sensitive (TLXS) or resistant (TLXRT) to nitrosoureas. Treatment <strong>of</strong> mice bearing either TLXS or<br />

TLXRT tumours with either BFNU or FCNU caused an elevation in the citrate levels <strong>of</strong> the heart, kidney<br />

and tumour, but not the liver, 24 hr after drug administration. Heart citrate levels were maximally elevated<br />

10-fold, while the levels in kidney and tumour were increased 3- to 6-fold. Tissue levels <strong>of</strong> fluorocitrate<br />

were determined by glc after conversion to the ethyl ester. This showed maximum levels <strong>of</strong> fluoroacetate<br />

production in the heart, with lower levels in kidney, tumour and liver. Treatment <strong>of</strong> K562 human<br />

erythroleukamia cells in vitro with BFNU caused an inhibition in the production <strong>of</strong> 14 CO2 from 14 C<br />

palmitate and [U- 14 C] glucose. These results suggest that some <strong>of</strong> the effects <strong>of</strong> the fluoroethylnitrosoureas<br />

may be related to fluoroacetate production and the consequent blocking effect on aconitase. This effect is<br />

probably related more to the generalised toxicity <strong>of</strong> these agents than to their therapeutic efficacy.<br />

Titmarsh, J. and O'Day, J. (1983). Ten-eighty poisoning in dogs. <strong>Control</strong> & Therapy 1637.<br />

Keywords: poisoning/dogs/treatment<br />

Tomkins, B. A. (1994). Screening procedure for sodium fluoroacetate (Compound 1080) at submicrogram/gram<br />

concentrations in soils. Analytical letters 27, 2703-2718.<br />

Keywords: fluoroacetate/1080/soil/sodium fluoroacetate/analysis<br />

Abstract: Sodium fluoroacetate (Compound 1080) is readily quantitated at sub-microgram per gram<br />

concentrations in small (ca. 1 g) soil samples. Samples are ultrasonically extracted with water, which is<br />

then partitioned with hexane, and acidified prior to re-extraction with ethyl acetate. The latter is taken to<br />

dryness in the presence <strong>of</strong> triethanolamine "keeper" and the resulting acid is derivatised with<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

pentafluorobenzyl bromide. Quantitation is performed using a gas chromatograph equipped with an<br />

electron-capture detector. A standardised statistical protocol is used to validate a screening level 0.2 µg<br />

compound 1080/g soil. Difluoroacetic, trifluoroacetic and naturally-occurring formic acids do not interfere<br />

with the determination. The rocvery for compound 1080 was 40% from soil fortified to 0.2 µg/g soil.<br />

Tonomura, K., Futai, F., Tanabe, O., and Yamaoka, T. (1965). Defluorination <strong>of</strong> mon<strong>of</strong>luoroacetate by<br />

bacteria. Part I. Isolation <strong>of</strong> bacteria and their activity <strong>of</strong> defluorination. Agricultural and Biological<br />

Chemistry 29, 124-128.<br />

Keywords: persistence in soil/defluorination/bacteria<br />

Abstract: Mon<strong>of</strong>luoroacetate (FA) is well known as a toxic substance and has been used as an insecticide:<br />

C-F linkage <strong>of</strong> which is very stable. Bacteria, capable <strong>of</strong> being grown in a defined salt medium containing<br />

FA as a sole source <strong>of</strong> carbon, have been isolated from soil. It has been found that the defluorination <strong>of</strong> FA<br />

involved an enzyme which catalyzes the conversion <strong>of</strong> FA to glycolate and fluoride ions and that the<br />

enzyme was induced when bacteria were grown in a defined salt medium containing FA as a sole source <strong>of</strong><br />

carbon. The activity <strong>of</strong> defluorination was fairly stable and strong in this organism.<br />

Tourtellotte, W. W. and Coon, J. M. (1950). Treatment <strong>of</strong> fluoroacetate poisoning in mice and dogs.<br />

Journal <strong>of</strong> pharmacology and experimental therapeutics 101, 82-91.<br />

Keywords: treatment/1080<br />

Abstract: 1.Sodium acetate and ethanol acted synergistically to anatgonize 1080 poisoning in mice. The<br />

LD50 <strong>of</strong> 1080 for mice (17.0 mgm/kgm. subcutaneously) was raised 4.6 times by immediate treatment with<br />

soium acetate, 3.1 times by ethanol, and 12.7 times by a combination <strong>of</strong> these substances.<br />

2. The beneficial effect <strong>of</strong> the acetate-ethanol treatment decreased rapidly with increasing time after the<br />

administration <strong>of</strong> 1080 in mice.<br />

3. The oral LD50 <strong>of</strong> 1080 in dogs was 0.066 mgm./kgm. and the LD100 was 0.08 to 0.12 mgm/kgm.<br />

4. In treating 1080 poisoned dogs, ethanol and acetate had some antidotal effect when administered<br />

immediatley after the 1080 but these agents were <strong>of</strong> no value as adjuncts to treatment with barbiturates<br />

when this treatment was started 30 minutes after poisoning.<br />

5. By the use <strong>of</strong> barbiturate therapy and by starting treatment 0.5 or 3 hours after poisoning, 100 per cent <strong>of</strong><br />

dogs poisoned with approximately 2 x LD50 <strong>of</strong> 1080 were saved. When treatment was started 0.5 or 3<br />

hours after oral poisoning with approximately 4 x LD50, 80 or 17 per cent <strong>of</strong> dogs, respectivley, were<br />

saved. No dogs survived when barbiturate treatment was instituted 0.5 hour after oral poisoning with<br />

approximately 6 x LD50.<br />

Trabes, J., Rason, N., and Avrahami, E. (1983). Computed tomography demonstration <strong>of</strong> brain damage due<br />

to acute sodium mon<strong>of</strong>luoroacetate poisoning. Journal <strong>of</strong> toxicology : clinical toxicology 20, 85-92.<br />

Keywords: diagnosis/mode <strong>of</strong> action/pathology/metabolism/brain/humans/treatment/welfare/symptoms<br />

Abstract: A previously healthy 15 year old female attempted suicide by SMFA-ingestion. The case reported<br />

developed an acute brain syndrome, including cerebellar signs, shortly after the ingestion <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate. After insiduous improvement <strong>of</strong> the clinical symptoms, the patient remained with an<br />

"end-stage" cerebellar ataxia for 18 months following the acute intoxication. The development <strong>of</strong> brain<br />

atrophy, proven by computed tomography, is considered to represent a direct influence <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate on the brain and to reflect the unique disturbances in cellular metabolism <strong>of</strong> glucose.<br />

Treasure, E. T., Drummond, B. K., Buchan, H. A., Beasley, M. G., Henaghan, R. M., and Nicholas, B. R.<br />

Fluoridation <strong>of</strong> water supplies. 1-34. 1993. Wellington, Public Health Commission.<br />

Ref Type: Report<br />

Keywords: persistence in water/fluoride/degradation<br />

Tremblay, L. A., Fisher, P., and Leusch, F. D. L. Evaluation <strong>of</strong> the Potential <strong>of</strong> Sodium Mon<strong>of</strong>luoroacetate<br />

(1080) and Fluorocitrate to Bind to a Mammalian Oestrogen Receptor. LCR0203/044, -16. 2002. Lincoln,<br />

<strong>Landcare</strong> <strong>Research</strong>.<br />

Ref Type: Report<br />

Keywords: 1080/fluoroacetate/fluorocitrate/mammals/mon<strong>of</strong>luoroacetate/reproductive effects/sodium<br />

fluoroacetate/sodium mon<strong>of</strong>luoroacetate<br />

Abstract: Sodium fluoroacetate (1080) and its active metabolite fluorocitrate were tested to determine<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

whether they can mimic the sex steroid 17β-oestradiol (E2) by binding to the oestrogen receptor (ER). This work was carried out by<br />

<strong>Landcare</strong> <strong>Research</strong>/ CENTOX, Lincoln for the Animal Health Board in September and October 2002. ER preparations were isolated from sheep uterine tissue and<br />

used in a competitive receptor-binding assay to determine the relative affinity <strong>of</strong> a variety <strong>of</strong> compounds for the ER. The assay is based on the ability <strong>of</strong> competitor<br />

molecules to displace radiolabelled E2 from the ER. The assay was validated by generating displacement curves for the natural oestrogen E2, nonylphenol (a known<br />

environmental oestrogen), tamoxifen (an anti-oestrogen drug), o,p'-DDT (an oestrogenic pesticide), and the androgen testosterone. The results showed that the ER<br />

preparations used met the requirements for validation. The known oestrogenic pesticide o,p'-DDT showed significant displacement <strong>of</strong> E2 while neither 1080 (sodium<br />

mon<strong>of</strong>luoroacetate) nor its active metabolite (fluorocitrate) had any effect on ER binding. Neither 1080 nor fluorocitrate are likely to promote oestrogenic or antioestrogenic<br />

effects by binding to a mammalian ER, therefore both compounds are unlikely to act as EDCs through this specific mechanism.<br />

Tremblay, L. A., Fisher, P., and Leusch, F. Evaluation <strong>of</strong> the potential <strong>of</strong> 1080 to bind to the mammalian<br />

oestrogen receptor. Proceedings <strong>of</strong> the Third International Wildlife Management Congress, New Zealand ,<br />

398. 2003.<br />

Ref Type: Abstract<br />

Abstract: Concerns were raised over the possibility that sodium fluoroacetate (1080) and its active<br />

metabolite fluorocitrate could cause endocrine disruption. Both compounds were tested to determine<br />

whether they could interfere with the sex steroid 17β-oestradiol (E2) by binding to the oestrogen receptor<br />

(ER), which is one <strong>of</strong> the most studied endocrine disruption mechanism. ER preparations were isolated<br />

from sheep uterine tissue and used in a competitive receptor-binding assay to determine the relative affinity<br />

<strong>of</strong> a variety <strong>of</strong> compounds for the ER. The assay is based on the ability <strong>of</strong> competitor molecules to displace<br />

radiolabelled E2 from the ER. The assay was validated by generating displacement curves for the natural<br />

oestrogen E2, nonylphenol (a known environmental oestrogen), tamoxifen (an anti-oestrogen drug), o,p'-<br />

DDT (an oestrogenic pesticide), and the androgen testosterone. The results showed that the ER preparations<br />

used met the requirements for a validated assay. The known oestrogenic pesticide o,p'-DDT showed<br />

significant displacement <strong>of</strong> E2 while neither 1080 nor its active metabolite fluorocitrate had any effect on<br />

ER binding. The data strongly suggest that neither 1080 nor fluorocitrate are likely to promote oestrogenic<br />

or anti-oestrogenic effects by directly binding to a mammalian ER. Therefore it is highly improbable that<br />

both compounds can act as EDCs through this specific mechanism. However, in order to provide a more<br />

complete evaluation, further screening tests based on higher levels <strong>of</strong> cellular organisation are required.<br />

Tremblay, L. A., Fisher, P., and Leusch, F. (2004). Potential <strong>of</strong> Sodium Mon<strong>of</strong>luoroacetate (1080) and<br />

Fluorocitrate to Bind to estrogen Receptor. Australasian journal <strong>of</strong> ecotoxicology 10.<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/fluorocitrate/assay/reproductive effects<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080), a vertebrate pesticide used in New Zealand, and its metabolite<br />

fluorocitrate were tested to determine whether the pesticide could promote an estrogenic response by<br />

binding to a mammalian estrogen receptor (ER). ER preparations were isolated from sheep uterine tissue<br />

and used in a competitive binding assay. The assay was validated by generating displacement curves for the<br />

natural estrogen (E2) and known environmental estrogens like o,p'-DDT and 4-nonylphenol. The known<br />

estrogenic pesticide o,p'-DDT showed significant displacement <strong>of</strong> E2 while neither 1080 nor its active<br />

metabolite fluorocitrate had any effect on ER binding. Sodium mon<strong>of</strong>luoroacetate and fluorocitrate are<br />

unlikely to promote estrogenic or anti-estrogenic effects by binding to the ER.<br />

Tremblay, L. A., Fisher, P., Leusch, F. D. L., van den Heuvel, M., Nicolas, J-C., and Balaguer, P. Potential<br />

<strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) and fluorocitrate to interact with androgen and oestrogen receptors.<br />

LC0405/019, -17. 2004. <strong>Landcare</strong> <strong>Research</strong>, Lincoln.<br />

Ref Type: Report<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/fluorocitrate/New Zealand/fish/brain/assay<br />

Abstract: Objectives<br />

• To determine, using an in vitro test system established in New Zealand, whether 1080 and<br />

fluorocitrate bind to fish brain androgen receptors.<br />

To determine, using an in vitro test system (Inserm, Montpellier, France), whether 1080 and<br />

fluorocitrate bind or block the actions <strong>of</strong> natural hormones at human androgen receptors.<br />

Methods<br />

• The androgenicity <strong>of</strong> 1080 and fluorocitrate was tested using a fish AR binding assay. Additional<br />

assays were conducted using a mammalian-based system.<br />

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1080 Reassessment Application October 2006<br />

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• A reporter gene assay system incorporating the human AR was used to determine whether 1080<br />

and fluorocitrate bind to the AR or block the actions <strong>of</strong> testosterone.<br />

Results<br />

• Neither 1080 nor fluorocitrate showed androgenic activity in the rainbow trout AR competitive<br />

binding assay. In reporter gene assays using the human AR, neither 1080 nor fluorocitrate showed<br />

androgenic or anti-androgenic activity.<br />

• In reporter gene assays using the human oestrogen receptor α (ERα), neither 1080 nor fluorocitrate<br />

showed oestrogenic or anti-oestrogenic activity.<br />

Conclusions<br />

Neither 1080 nor fluorocitrate are likely to promote androgenic or anti-androgenic effects by<br />

binding to a fish or the human AR. Therefore, both compounds are unlikely to act as endocrine-disrupting<br />

chemicals through these specific mechanisms.<br />

Both compounds did not interact with the human ERα, supporting the results <strong>of</strong> earlier work with<br />

a sheep ER assay.<br />

Recommendations<br />

These results should be considered by the Environmental Risk Management Authority (ERMA<br />

New Zealand) as part <strong>of</strong> the formal reassessment <strong>of</strong> 1080.<br />

Triggs, S. and Green, W. O. (1989). Geographic patterns <strong>of</strong> genetic variation in brushtail possums<br />

(Trichosurus vulpecula) and implications for pest control. New Zealand journal <strong>of</strong> ecology 12, 1-10.<br />

Keywords: brushtail possum/morphology/pest/1080/New Zealand/Australia/resistance<br />

Abstract: Two morphological types <strong>of</strong> brushtail possum were introduced to new Zealand: smaller, grey<br />

possums from mainland southeastern Australia and larger, black possums from Tasmania. Analysis <strong>of</strong><br />

patterns <strong>of</strong> allozyme variation and allele frequencies <strong>of</strong> rpesent-day possum populations in New Zealand<br />

and southeastern Austrlia indicates that populations comprised predominantly <strong>of</strong> balck possums remain<br />

genetically similar to possums in Tasmania, whereas predominantly grey populations are genetically closer<br />

to Victorian and New South Wales possums. The distribution <strong>of</strong> possums in New Zealand can be accounted<br />

for at least partly by selection <strong>of</strong> stock types with respect to climate. genetic differences between<br />

populations may have important implications for the control <strong>of</strong> possums, because Tasmanian possums have<br />

a greater resistance than mainland southeastern Australian possums to 1080 poison (sodium<br />

mon<strong>of</strong>luoroacetate), which is commonly used to control possums in New Zealand.<br />

Trujillo, M. H., Guerrero, J., Fragachan, C., and Fernandez, M. A. (1998). Pharmacologic antidotes in<br />

critical care medicine: A practical guide for drug administration. Crit.Care Med. 26, 377-391.<br />

Keywords: treatment/poisoning/antidote<br />

Tsuchiya, T. and Levy, G. (1972). Relationship between effect <strong>of</strong> activated charcoal on drug absorption in<br />

man and its drug adsorption characteristics In Vitro. Journal <strong>of</strong> Pharmaceutical Sciences 61, 586-589.<br />

Keywords: poisoning/treatment/antidote/humans<br />

Abstract: Parallel in vivo and in vitro determinations <strong>of</strong> the adsorption characteristics <strong>of</strong> activated charcoal<br />

were carried out with three drugs having a different pKa: aspirin, salicylamide, and phenylpropanolamine.<br />

In vitro adsorption isotherms at pH1 and 8.2 and the effect <strong>of</strong> increasing pH on drug desorption<br />

characteristics suggested that, as these drugs pass from stomach to intestine, the in vivo adsorption <strong>of</strong> : (a)<br />

aspirin will be reversed significantly due to change in pH, (b) salicylamide will be decreased only slightly<br />

except for possible competitive effects <strong>of</strong> normal intestinal contents,and (c) phenylpropanolamine may be<br />

increased slightly unless intestinal content exerts a displacing effect. Absorption studies in human<br />

volunteers yielded results that are consistent with these predictions and that demonstrate the effect <strong>of</strong> dose<br />

and mode <strong>of</strong> charcoal administration on the efficacy <strong>of</strong> this adsorbent. These studies suggest that it may be<br />

possible to make reasonable predictions concerning the relative antidotal effectiveness <strong>of</strong> activated charcoal<br />

in man on the basis <strong>of</strong> appropriate in vitro adsorption studies.<br />

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Appendix C<br />

Tu, L., Bolton, R. M., Wright, P. F. A., and Ahokas, J. T. The subcellular distribution <strong>of</strong> defluorination<br />

activity in three mammalian species. International Congress <strong>of</strong> Toxicology ICT VIII, 5-10 July 1998, Paris.<br />

1998.<br />

Ref Type: Conference Proceeding<br />

Keywords: defluorination<br />

Abstract: Fluoroacetate is highly toxic to a wide range <strong>of</strong> animals, including non-target species. The species<br />

difference in sensitivity to fluoroacetate remains without an explanation. In mammals, detoxification <strong>of</strong><br />

fluoroacetate by defluoriantion occurs mainly in the liver by fluoroacetate-specific defluorinase. This<br />

enzyme is thought to be a unique glutithine-S-transferase, but the mechanism <strong>of</strong> this glutathione dependent<br />

reaction is still unclear. To understand the species differences in sensitivity to fluoroacetate, subcellualr<br />

fractionation <strong>of</strong> livers from Wistar Rats, Bal b/c mice and brushtail possums was performed. Defluorination<br />

was measured by fluoride ion determination in vitor based on fluoride release after incubation, using<br />

sodium fluoroacetate as the substrate. The result showed; 1) defluorination activity based on protein content<br />

was the highest in the cytosolic fraction <strong>of</strong> all species. The mitochondrial and microsomal fractions both<br />

had minimal activity. 2) The subcellualr distribution <strong>of</strong> defluorinationactivity in the liver <strong>of</strong> male rats<br />

showed the nuclear, mitochondria, microsomes and cytosol presented 33.2%, 0.6%, 1.3% and 50.8%<br />

respectively <strong>of</strong> the defluorination activity in the homogenate. 3) The comparison between male and female<br />

<strong>of</strong> rats and mice suggested that there was increasing defluorination activity in females. However, only the<br />

cytosolic fraction <strong>of</strong> female rats had significantly higher activity than male rats. 4) Comparison <strong>of</strong><br />

defluorination activity in the three species showed that rats and possums had a relatively lower activity in<br />

cytosol, but higher activity in mitochondria and microsomes compared with mice. The rank order <strong>of</strong><br />

defluorination activity in the mitochondrial fraction in the three species is possum> rat>mouse. This study<br />

suggested that the defluorination <strong>of</strong> fluoroacetate is mainly localised in cytosolic fraction <strong>of</strong> the liver.<br />

Female animals presented a higher defluorination activity tendency. The role <strong>of</strong> mitochondria in<br />

defluorination <strong>of</strong> fluoroacetate requires further investigation.<br />

Tucker, R. K. and Crabtree, D. G. Handbook <strong>of</strong> toxicity <strong>of</strong> pesticides to wildlife. Resource Publication No.<br />

84, -131 pp. 1970. Bureau <strong>of</strong> Sport Fisheries and Wildlife, Denver Wildlife <strong>Research</strong> Centre.<br />

Ref Type: Report<br />

Keywords: lethal dose/ferrets/1080<br />

Tucker, R. K. and Haegele, M. A. (1971). Comparative acute oral toxicity <strong>of</strong> pesticides to six species <strong>of</strong><br />

birds. Toxicology and Applied Pharmacology 20, 57-65.<br />

Keywords: acute toxicity/birds/non-target species<br />

Turck, P. A., Eason, C. T., and Wickstrom, M. (1998). Assessment <strong>of</strong> the developmental toxicity <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) in rats. Toxicologist 42, 259.<br />

Keywords: developmental toxicity/toxicity/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/rats<br />

Twigg, L. E., Majer, J. D., and Kotula, R. The influence <strong>of</strong> fluoroacetate producing plants upon seed<br />

selection by seed harvesting ants. 75-80. 1983. Western Australia. Annual Report Mulga <strong>Research</strong> Centre<br />

1982.<br />

Ref Type: Report<br />

Keywords: fluoroacetate/invertebrates/occurrence in nature<br />

Abstract: Little is known about the influence <strong>of</strong> fluoroacetate-bearing seed upon the selection <strong>of</strong> seed by<br />

harvesting ants. The response <strong>of</strong> ants to seed containing fluoroacetate, which were placed out in artificial<br />

depots in a Eucalyptus wandoo open woodland, suggested that the presence <strong>of</strong> this substance had very little<br />

effect upon the seed selection <strong>of</strong> harvesting ants. Of the total seed <strong>of</strong>fered, 44.3 % was removed in 24<br />

hours. The principal ant species observed taking seed were Camponotus sp. J.D.M.183, Melophorus sp.<br />

J.D.M. 117, Meranoplus sp. J.D.M. 400, Monomorium sp. 1 (ANIC) and Rhytidoponera sp. J.D.M. 121.<br />

Small numbers <strong>of</strong> Gastrolobium microcarpum (fluoroacetate producing) seed were recovered form two <strong>of</strong><br />

five extracted ant nests.<br />

Twigg, L. E., Mead, R. J., and King, D. R. (1986). Metabolism <strong>of</strong> fluoroacetate in the skink (Tiliqua<br />

rugosa) and the rat (Rattus norvegicus). Australian journal <strong>of</strong> biological sciences 39, 1-15.<br />

Keywords: metabolism/sodium fluoroacetate/1080/persistence in animals/defluorination/liver<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Abstract: Administration <strong>of</strong> 100 mg sodium fluoroacetate (compound 1080) per kilogram body weight to T.<br />

rugosa resulted in a 3.4-fold increase in plasma citrate levels 48h. after dosing while administration <strong>of</strong> 3 mg<br />

sodium fluoroacetate per kilogram body weight to R. norvegicus produced a fivefold increase in plasma<br />

citrate levels within 4 h. Administration <strong>of</strong> 300 mg sodium fluoroacetate per kilogram body weight reduced<br />

the oxygen consumption <strong>of</strong> the skink by between 2.5 and 11% while in the rat, 2 mg sodium fluoroacetate<br />

per kilogram body weight reduced oxygen consumption by between 28 and 57%. Aconitate hydratase<br />

activity in extracts <strong>of</strong> liver acetone powders from T. rugosa was less inhibited by (-)erythr<strong>of</strong>luorocitrate<br />

(Ki: 0.065 mM) than that in extracts derived from R. norvegicus (Ki: 0.026 mM).The rate <strong>of</strong> defluorination<br />

<strong>of</strong> fluoroacetate in erythrocytes and in extracts <strong>of</strong> liver acetone powders <strong>of</strong> T. rugosa was 8- and 4.5-fold<br />

greater, respectively, than that found in similar preparations from R. norvegicus. A rapid rate <strong>of</strong><br />

defluorination together with a low reliance on aerobic respiration favoured detoxification <strong>of</strong> fluoroacetate<br />

in T. rugosa rather than its conversion into fluorocitrate. Though defluorination in this species helped to<br />

minimize the immediate effects <strong>of</strong> fluoroacetate on aerobic respiration, it resulted in rapid depletion <strong>of</strong> liver<br />

glutathione levels.<br />

Twigg, L. E., King, D. R., and Bradley, A. J. (1988). The effect <strong>of</strong> sodium mon<strong>of</strong>luoroacetate on plasma<br />

testosterone concentration in Tiliqua rugosa (Gray). Comparative biochemistry and physiology 91C, 343-<br />

347.<br />

Keywords: acute toxicity/non-target species/mode <strong>of</strong> action/pathology/sodium<br />

fluoroacetate/1080/reptiles/reproductive effects/plasma/blood/chronic poisoning/fluoroacetate<br />

Abstract: 1. Administration <strong>of</strong> multiple or single doses <strong>of</strong> sodium fluoroacetate (1080) to male Tiliqua<br />

rugosa caused a decrease in plasma testosterone concentration.<br />

2. A single dose <strong>of</strong> 100 or 250 mg 1080kg -1 body weight decreased plasma testosterone by 52%.<br />

However, 25mg kg-1 had little apparent effect on testosterone levels. When lizards were given the multiple<br />

dose equivalent <strong>of</strong> these doses over 12 days at 3 day intervals, the effect was much less dramatic with<br />

plasma testosterone concentration steadily declining over 15 days for the two higher doses.<br />

3. There was a suggestion <strong>of</strong> degeneration <strong>of</strong> seminiferous tubules in some individuals.<br />

Twigg, L. E., King, D. R., Davis, H. M., Saunders, G., and Mead, R. J. (1988). Tolerance to, and<br />

metabolism <strong>of</strong>, fluoroacetate in the emu. Australian wildlife research 15, 239-247.<br />

Keywords: non-target species/birds/metabolism/persistence in animals/1080<br />

Abstract: Compared with most other birds, the emu, Dromaius novaehollandiae Vieillot, has unusually high<br />

tolerance to fluoroacetate (1080). The LD50 for emus with evolutionary exposure to fluoroacetate bearing<br />

vegetation in the southwest <strong>of</strong> Western Australia was 102 mg <strong>of</strong> 1080 per kilogram. This tolerance appears<br />

to result from: the substantial capacity <strong>of</strong> emus to detoxify fluoroacetate by defluorination; the limited<br />

conversion <strong>of</strong> fluoroacetate into fluoroacetate by emus; and/or their possession <strong>of</strong> an aconitate hydratase<br />

which is relatively insensitive to fluorocitrate.<br />

Twigg, L. E. and King, D. R. (1989). Tolerance to sodium fluoroacetate in some Australian birds.<br />

Aust.Wildl.Res. 16, 49-62.<br />

Keywords: tolerance/fluoroacetate/birds/occurrence in nature/citrate<br />

Abstract: Increases in plasma citrate concentration in response to dosing with sodium fluoroacetate were<br />

shown to reflect the sensitivity to fluoroacetate intoxication <strong>of</strong> birds with similar metabolic rates and<br />

phylogenetic affinities. Platycercus icterotis and Purpureicephalus spurius are indigenous to the south-west<br />

<strong>of</strong> Western Australia where fluoroacetate-bearing vegetaion is abundant and they were more tolerant to<br />

fluoroacetate than Barnardius zonarius, Polytelis anthopeplus and Cacatua roseicapilla whose<br />

distributions include areas outside the range <strong>of</strong> the toxic plants. Streptopelia senegalensis and the Barbary<br />

dove (Streptopelia sp.) have had little or no exposure to naturally occurring fluoroacetate and were much<br />

more sensitive to fluoroacetate poisoning than were Phaps chalcoptera and Ocyphaps lophotes, regardless<br />

to the extent <strong>of</strong> exposure <strong>of</strong> the latter species to the toxic plants. Phaps chalcoptera, Ocyphaps lophotes,<br />

Anas superciliosa and Chenonetta jubata in eastern Australia are not exposed to fluoroacetate-bearing<br />

vegetation, but had tolerances similar to that <strong>of</strong> their conspecifics in the south-west <strong>of</strong> Western Australia.<br />

The level <strong>of</strong> tolerance to fluoroacetate appears dependent upon the length <strong>of</strong> evolutionary exposure to the<br />

toxic plants, and the degree <strong>of</strong> mobility in each species.<br />

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Appendix C<br />

Twigg, L. E. and Mead, R. J. (1990). Comparative metabolism <strong>of</strong>, and sensitivity to fluoroacetate in<br />

geographically separated populations <strong>of</strong> Tiliqua rugosa (Gray) (Scincidae). Australian Journal <strong>of</strong> Zoology<br />

37, 617-626.<br />

Keywords: metabolism/fluoroacetate/liver/defluorination/fluorocitrate/tolerance<br />

Abstract: Populations <strong>of</strong> Tiliqua rugosa which coexist with fluoroacetate bearing vegetation were much<br />

less sensitive to fluoroacetate intoxication than were conspecifics not exposed to the toxic plants. However,<br />

the biochemical mechanisms responsible for this toxicity differential were not ascertained. Liver acetone<br />

powder preparations from both conspecifics were similar in their abilities to detoxify fluoroacetate by<br />

defluorination, and to convert fluoroacetate to fluorocitrate. The aconitate hydratase in these preparations<br />

was also similarly inhibited by (-)erythro-fluorocitrate. These findings, and other possibilites which could<br />

be responsible for the toxicity differential are discussed.<br />

Twigg, L. E. (1990). The sensitivity <strong>of</strong> some Western Australian caterpillars to fluoroacetate. Mulga<br />

<strong>Research</strong> Centre Journal 10, 14-18.<br />

Keywords: fluoroacetate/invertebrates/lethal dose/1080<br />

Abstract: The sensitivity <strong>of</strong> fluoroacetate (1080) <strong>of</strong> three species <strong>of</strong> lepidopteran and one species <strong>of</strong><br />

hymenopteran larvae, which coexist with fluoroacetate-bearing vegetation in Western Australia, was<br />

determined. Larvae <strong>of</strong> Perga dorsalis (hymenopteran) and Mnesamplea privata feed mainly on eucalypts<br />

and were very sensitive to the toxin with LD50 values <strong>of</strong> 1.05 and 3.88 mg 1080 kg -1 respectively.<br />

Spilosoma sp. has a cosmopolitan diet and was moderately tolerant to fluoroacetate (LD50 42.73 mg 1080<br />

kg -1 ). However, larvae <strong>of</strong> Ochrogaster lunifer, which when collected were feeding on fluoroacetate-bearing<br />

Gastrolobium microcarpum, were extremely tolerant to the toxin (LD50 c. 150 mg 1080 kg -1 ). This suggests<br />

that co-evolution has occurred between tolerant insects and the toxic plants.<br />

Twigg, L. E., King, D. R., and Mead, R. J. (1990). Tolerance to fluoroacetate <strong>of</strong> populations <strong>of</strong> Isoodon<br />

spp. and Macrotis lagotis and its implications for fauna management. In 'Bandicoots and Bilbies'. (J. H.<br />

Seebeck, P. R. Brown, R. L. Wallis, and C. M. KemperEds. ) pp. 185-192. (Surrey Beatty and Sons:<br />

Sydney.)<br />

Keywords: tolerance/fluoroacetate<br />

Twigg, L. E. and King, D. R. (1991). The impact <strong>of</strong> fluoroacetate-bearing vegetation on native Australian<br />

fauna: a review. Oikos 61, 412-430.<br />

Keywords: fluoroacetate/occurrence in nature/tolerance/mammals/non-target species<br />

Abstract: Fluoroacetate is a highly toxic compound which is produced by three genera <strong>of</strong> plants in parts <strong>of</strong><br />

south western and northern Australia, particularly the south west corner <strong>of</strong> Western Australia. Native<br />

animals in these regions have coexisted with this toxic vegetation for at least several thousand years, and<br />

many species have developed a marked tolerance to fluoroacetate. Factors influencing their level <strong>of</strong><br />

tolerance, the possible causal mechanisms, and the implications to fauna management are discussed.<br />

Twigg, L. E. (1994). Occurrence <strong>of</strong> fluoroacetate in Australian plants and tolerance to 1080 in indigenous<br />

Australian animals. In 'Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14 December 1993,<br />

Christchurch, New Zealand'. (A. A. Seawright and C. T. EasonEds. ) pp. 97-115. (<strong>Royal</strong> Society <strong>of</strong> New<br />

Zealand: Wellington.)<br />

Keywords: metabolism/acute toxicity/occurrence in nature/1080/mammals/birds<br />

Abstract: In parts <strong>of</strong> Australia, plant species <strong>of</strong> the genus Gastrolobium, can produce considerable<br />

quantities <strong>of</strong> fluoroacetate (.2,000 mg kg-1 in leaves) as a chemically mediated defence strategy against<br />

herbivory. The concentration <strong>of</strong> fluoroacetate in these plants varies between species, region, soil type, and<br />

season. By necessity, animal populations have coexisted with this fluoroacetate bearing vegetation for at<br />

least several thousand years. Consequently, they have developed varying degrees <strong>of</strong> tolerance to this potent<br />

toxin which depends upon their dietary and habitat specialisation, the size <strong>of</strong> their home range, the degree<br />

<strong>of</strong> mobility exhibited by each species, and the length <strong>of</strong> evolutionary exposure to the toxic vegetation.<br />

Dietary studies indicate that animals are able to discriminate between the highly toxic and less toxic plant<br />

species. Fluoroacetate-tolerance has developed in insects, reptiles, mammals, and birds with herbivores ><br />

omnivores > carnivores. It is also retained by animal populations even when they become isolate from the<br />

toxic vegetation for 7,000 to 10,000 y.<br />

Development <strong>of</strong> tolerance to fluoroacetate by animals has evolved on at least three continents where<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

indigenous plants are known to produce fluoroacetate. However, the biochemical mechanisms responsible<br />

for the tolerance are poorly understood. As fluoroacetate can cause a reduction in animal fertility, and in<br />

levels <strong>of</strong> reduced glutathione in the liver necessary for detoxification, it is argued that both the acute and<br />

chronic effects <strong>of</strong> fluoroacetate poisoning are equally important selection pressures for the development <strong>of</strong><br />

tolerance to fluoroacetate.<br />

Tolerance to fluoroacetate (1080) in native Australian animals enhances the target specificity <strong>of</strong> 1080<br />

poison during control programs directed at introduced vertebrate pests. Baiting with 1080 also plays an<br />

important role in protecting native Australian flora and fauna from the effect <strong>of</strong> predation and competition<br />

generated by introduced predators and herbivores.<br />

Twigg, L. E. (1995). Fluoroacetate-bearing vegetation and Australian animals: a biological arms race.<br />

Toxicology and Ecotoxicology News 2, 44-49.<br />

Keywords: occurrence in nature/tolerance/fluoroacetate/mammals/marsupials<br />

Abstract: In south-western Australia, 39 species <strong>of</strong> indigenous plants from the genus Gastrolobium produce<br />

fluoroacetate (1080 posion - a highly toxic vertebrate pesticide) as a chemically-mediated defence against<br />

being eaten. Many species <strong>of</strong> native animals have therefore co-existed with this toxic vegetation for several<br />

thousand years and, as a consequence, have developed varying degrees <strong>of</strong> tolerance to fluoroacetate. This<br />

article summarises our current understanding <strong>of</strong> this natural biological 'arms race'.<br />

Twigg, L. E., King, D. R., Bowen, L. H., Wright, G. R., and Eason, C. T. (1996). Fluoroacetate found in<br />

Nemcia spathulata. Australian journal <strong>of</strong> botany 44, 411-412.<br />

Keywords: occurrence in nature<br />

Abstract: A note suggesting that the concentrations <strong>of</strong> fluoroacetate found in plants which naturally produce<br />

fluoroacetate will vary according to time <strong>of</strong> year, particular plant part tested, species examined, and ability<br />

<strong>of</strong> the species to rpoduce fluoroacetate. The presence or absence <strong>of</strong> fluoroacetate should therefore not be<br />

taken as a reliable indicator <strong>of</strong> the genetic relationship <strong>of</strong> these plants, at least not until all the potential<br />

candidates, which are likely to contain fluoroacetate, have been adequately assessed.<br />

Twigg, L. E., King, D. R., Bowen, L. H., Wright, G. R., and Eason, C. T. (1996). Fluoroacetate content <strong>of</strong><br />

some species <strong>of</strong> toxic Australian plant genus, Gastrolobium, and its environmental persistence. Natural<br />

toxins 4, 122-127.<br />

Keywords: metabolism/persistence in plants/occurrence in nature<br />

Abstract: Gas chromatography confirmed the relatively high concentrations <strong>of</strong> fluoroacetate found in toxic<br />

Gastrolobiums, a genus <strong>of</strong> indigenous Australia plants. Fluoroacetate concentration in these plants ranged<br />

from 0.1 to 3875 ug/g (ppm) dry weight, with young leaves and flowers containing the highest<br />

concentrations. However, there as considerable intrastand variation between individual plants <strong>of</strong> at least<br />

two species with coefficients <strong>of</strong> variation ranging from 94% to 129%. Despite the high concentrations <strong>of</strong><br />

fluoroacetate in many species, only one <strong>of</strong> nine soil samples collected from beneath these plants contained<br />

fluoroacetate. None <strong>of</strong> the 16 water samples collected from nearby streams catchments dams contained<br />

fluoroacetate. This suggest that fluoroacetate does not persist in this environment. Fluoroacetate was also<br />

found in the genus Nemcia, and very low levels <strong>of</strong> fluoroacetate (ng/g) were detected in the foodstuffs, tea<br />

and guar gum. The latter indicates that other plant species my produce biologically insignificant amounts<br />

<strong>of</strong> fluoroacetate.<br />

Twigg, L. E. and Socha, L. V. (1996). Physical versus chemical defence mechanisms in toxic<br />

Gastrolobium. Oecologia 108, 21-28.<br />

Keywords: occurrence in nature/fluoroacetate<br />

Abstract: The degree to which physical defence mechanisms are present in toxic species <strong>of</strong> Gastrolobium<br />

was compared with the known fluoroacetate (the toxic principle) concentrations <strong>of</strong> these plants using both<br />

histological leaf sections prepared from fresh leaves (4 species), and a variety <strong>of</strong> visual external traits<br />

measured from herbarium specimens (28 species). There was a strong negative correlation between the<br />

presence <strong>of</strong> physical deterrents (e.g. area <strong>of</strong> fibres, number and length <strong>of</strong> spines) and the fluoroacetate<br />

concentration <strong>of</strong> each species. This suggests that, with respect to their leaves, individual species have<br />

established a compromise between producing physical grazing deterrents and the adoption <strong>of</strong> chemically<br />

mediated antiherbivore strategies.<br />

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Appendix C<br />

Twigg, L. E., Wright, G. R., and Potts, M. D. (1999). Fluoroacetate content <strong>of</strong> Gastrolobium brevipes in<br />

central Australia. Australian journal <strong>of</strong> botany 47, 877-880.<br />

Keywords: occurrence in nature<br />

Abstract: Fluoroacetate was found in Gastrolobium brevipes and some other Australian species. Its<br />

presence suggests that some native animals in central Australia are likely to have developed a degree <strong>of</strong><br />

tolerance to the toxin.<br />

Twigg, L. E., Eldridge, S. R., Edwards, G. P., Shakeshaft, B. J., dePreu, N. D., and Adams, N. (2000). The<br />

longevity and efficacy <strong>of</strong> 1080 meat baits used for dingo control in central Australia. Wildlife research 27,<br />

473-481.<br />

Keywords: bait degradation/1080/cats/non-target species<br />

Twigg, L. E. and King, D. (2000). Artificially enhanced tolerance to fluoroacetate and its implications for<br />

wildlife conservation. Pacific Conservation Biology 6, 9-13.<br />

Keywords: tolerance/fluoroacetate/bacteria/1080/livestock/poisoning/GMO/occurrence in nature<br />

Abstract: It is with some concern that we have been following a research programme aimed atdeveloping<br />

non-specific geneticlaly modified ruminant bacteria capable <strong>of</strong> detoxifying fluoroacetate (Compound 1080)<br />

to protect domestic livestock from fluoroacetate poisoning. The main thrust <strong>of</strong> this research programme is<br />

the prevention <strong>of</strong> cattle losses in the Georgina Basin in the Northern Territory and Queensland where the<br />

toxic plant Gidgee Acacia georginae occurs. Although rarely mentioned in formal reports <strong>of</strong> this work,<br />

1080 is an important vertebrate pesticide that is widely used throughout Australia and New Zealand. It is<br />

the first defence against a number <strong>of</strong> pest species that impact on agricultural production and conservation<br />

efforts in both countries. The main concerns about this work relate to the potential lack <strong>of</strong> target specifity <strong>of</strong><br />

these modified microorganisms, and also, if released, their potential impact on conservation biology. We<br />

raise these questions now because the Genetic Manipulation Advisory Council has been approached for<br />

approval to conduct field trials in Western Australia using the modified bacteria. We believe the perceived<br />

advantages and disadvantages <strong>of</strong> these modified organisms need informed debate before such approval, or<br />

any general release <strong>of</strong> these modified rumen bacteria could be considered.<br />

Twigg, L. E. and Socha, L. V. (2001). Defluorination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate by soil microorganisms<br />

from central Australia. Soil biology and biochemistry 33, 227-234.<br />

Keywords: metabolism/persistence in soil/1080<br />

Twigg, L. E., Kok, N. E., Kirkpatrick, W. E., and Burrow, G. (2001). The longevity <strong>of</strong> 1080 egg-baits in a<br />

regularly baited nature reserve in south-western Australia. Wildlife research 28, 607-618.<br />

Keywords: 1080/foxes/baits/bait degradation/birds/non-target species/reptiles<br />

Abstract: The longevity <strong>of</strong> 1080 in egg-baits (4.5 mg 1080 per egg) used for fox control was monitored at<br />

the Corackerup Nature Reserve, Western Australia. Irrespective <strong>of</strong> season, most egg baits (94%) were<br />

found to retain sufficient 1080 to be theoretically lethal to all foxes for at least 42 days, and 75% <strong>of</strong> baits<br />

contained an LD50 <strong>of</strong> 1080 at Day 63. Exponential decay curves also predicted that these baits would<br />

remain toxic to most foxes for up to 32 weeks, depending upon environmental conditions. Sealing the<br />

injection hole with wax, or using sterile techniques to prepare some egg-baits, appeared to have little effect<br />

on the longevity <strong>of</strong> 1080 in these baits compared with that <strong>of</strong> unsealed eggs. Bait take, and identification <strong>of</strong><br />

those species taking baits were monitored over 12 days at 216 permanent bait stations in the reserve. Track<br />

plots were present for 3-6 days on 83 <strong>of</strong> these stations in spring and summer but not in winter. In spring and<br />

summer, <strong>of</strong> those species likely to take bait, goannas were the most frequent visitors to the track plots and<br />

they were also responsible for most <strong>of</strong> the baits taken at this time (59% and 90% <strong>of</strong> baits taken). Foxes<br />

accounted for 27% (spring), 8% (summer) and 75% (winter) <strong>of</strong> the egg-baits taken. No egg-baist were<br />

taken by goannas in winter, but the overall bait take was also low at this time (28 <strong>of</strong> 211 baits laid, 13%).<br />

Overall bait take after 12 days in spring and summer was 64% (135 <strong>of</strong> 211) and68% (145 <strong>of</strong> 212) <strong>of</strong> baits<br />

laid. Except for goannas, birds and other non-target species (eg bob-tail skink) took relatively few baits in<br />

any season.<br />

Twigg, L. E., Gray, G. S., Massam, M. C., Lowe, T. J., Kirkpatrick, W., Bendotti, G., and Chester, D. R.<br />

(2001). Evaluation <strong>of</strong> bait stations for control <strong>of</strong> urban rabbits. Wildlife research 28, 299-310.<br />

Keywords: rabbits/field efficacy/efficacy/1080/pindone/non-target species/birds/resistance<br />

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Abstract: The acceptability <strong>of</strong> four different bait station designs (drum, slab, tyre, corrugated iron) to<br />

rabbits was tested in the field using unpoisoned oat bait. The drum (200 L, cut longitudinally) and the<br />

raised concrete slab (60 X 60 cm) designs were the most acceptable to rabbits. The raised tyre design was<br />

unacceptable, and this was supported by later field efficacy trials that compared the drum and tyre designs<br />

using 1080 One-shot oats. The efficacy <strong>of</strong> three <strong>of</strong> these designs (drum, slab, tyre) against 'urban' rabbits<br />

was assessed more fully using pindone oat bait. The tyre stations were again found to have little impact on<br />

rabbit numbers. With the exception <strong>of</strong> one drum site where pindone bait stations were totally ineffective,<br />

the proportional reductions in rabbit numbers for the remaining sites were similar between the drum (69%,<br />

n = 3) and slab (70%, n = 5) designs. However, the slab design provided much easier access to bait by nontarget<br />

species (particularly birds), and we therefore recommend that the drum design would be the best bait<br />

station for controlling rabbits. The overall proportional reduction in rabbit numbers achieved with pindone<br />

bait stations was 48% (range 0-80%, n = 13), which is less than that usually achieved during broadacare<br />

control programs with pindone (60-90+%). In addition, these kills took 30-60 days to achieve, and as rabbit<br />

damage sstill occurred over this period, the use <strong>of</strong> pindone bait stations did not always result in damage<br />

mitigation or, ultimately, an economic benefit. Some potential problems associated with the use <strong>of</strong> pindone<br />

bait stations, such as the possibility <strong>of</strong> the development <strong>of</strong> 'resistance' to pindone bait and the risk to nontarget<br />

species, are also discussed. The combined use <strong>of</strong> track counts and a 'digs' index proved a reliable<br />

indicator <strong>of</strong> changes in rabbit abundance<br />

Twigg, L. E., Martin, G. R., and Lowe, T. J. (2002). Evidence <strong>of</strong> pesticide resistance in medium-sized<br />

mammalian pests: a case study with 1080 poison and Australian rabbits. Journal <strong>of</strong> applied ecology 39,<br />

549-560.<br />

Keywords: 1080/efficacy/lethal dose/poison/rabbits/resistance/rodents/toxicity/wildlife<br />

Abstract: Toxicant-resistance is a potential, or very real, problem with many pest-control programmes<br />

world-wide. However, apart from rodents, pesticide-resistance has not been well documented in<br />

vertebrates. We assessed the potential impact <strong>of</strong> developing resistance to 1080 in rabbit populations with<br />

differing levels <strong>of</strong> historical exposure to 1080-baiting programmes in south-western Australia. The<br />

sensitivity to 1080 <strong>of</strong> three out <strong>of</strong> the four populations <strong>of</strong> rabbits examined had decreased signficantly since<br />

Australian rabbits were last tested over 25 years ago. The lethal dose values (LD50) for these populations,<br />

as determined from formal toxicity trials, ranegd from 0.744 to 1.019 mg pure 1080/kg, and were<br />

significantly greater (P0.05). The lethal dose<br />

values (LD99) fort eh four rabbit populations tested ranged from 1.181 to 1.666 mg pure 1080/kg, and<br />

suggested that, theoretically, all rabbits should be killed during routine baiting compaigns provided that<br />

there is no loss <strong>of</strong> active ingredient from the bait. In reality, the efficacy <strong>of</strong> 1080 poison bait laid in trails for<br />

controlling free-ranging rabbits was reduced in those populations where rabbits had decreased sensitivity to<br />

1080. Mean reductions in rabbit numbers 7-9 days after trail baiting <strong>of</strong> resistant and sensitive populations<br />

ranged from 51.2% to 65.2%, and from 76.4% and 76.5% respectively. These findings suggest that genetic<br />

resistance to 1080 is developing in at least some populations <strong>of</strong> Australian rabbits. This has world-wide<br />

implications for agricultural protection and wildlife conservation programmes that rely on a 1080-baiting<br />

strategy for reducing the impact <strong>of</strong> vertebrate pests.<br />

Twigg, L. E., Martin, G. R., Eastman, A. F., King, D. R., and Kirkpatrick, W. E. (2003). Sensitivity <strong>of</strong><br />

some Australian animals to sodium fluoroacetate (1080): additional species and populations, and some<br />

ecological considerations. Australian Journal <strong>of</strong> Zoology 51, 515-531.<br />

Keywords: sodium fluoroacetate/fluoroacetate/1080/rodents/rodent/tolerance/lethal dose<br />

Abstract: The sensitivity to fluoroacetate ( 1080) <strong>of</strong> a number <strong>of</strong> species <strong>of</strong> rodents and dasyurids with and<br />

without evolutionary exposure to fluoroacetate-bearing vegetation was determined. Rattus fuscipes, and<br />

species <strong>of</strong> Pseudomys from populations with exposure to this vegetation, were particularly tolerant to<br />

fluoroacetate. However, the level <strong>of</strong> tolerance varied among the different populations <strong>of</strong> each species,<br />

depending on the degree to which the toxic plants were present in their microhabitat. The tolerance <strong>of</strong> the<br />

F1 <strong>of</strong>fspring <strong>of</strong> sensitive R. fuscipes ( South Australia) crossed with tolerant conspecifics from Western<br />

Australia was mid-range between those <strong>of</strong> the parental populations. The sensitivity <strong>of</strong> introduced R. rattus<br />

and Mus domesticus from areas with fluoroacetate-producing plants in Western Australia was similar to<br />

that reported elsewhere for these rodents. This suggests that their relatively short coexistence with the toxic<br />

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Appendix C<br />

plants has had little obvious impact on their level <strong>of</strong> sensitivity to fluoroacetate. The dibbler, Parantechinus<br />

apicalis, which coexists with the toxic vegetation, was exceptionally tolerant for a native<br />

carnivore/insectivore (LD50 similar to35 mg 1080 kg(-1)). In contrast, however, Phascogale tapoatafa from<br />

southern Western Australia was more sensitive to 1080 than was expected, with an estimated LD50 <strong>of</strong> 7 mg<br />

1080 kg(-1). Although the level <strong>of</strong> tolerance to fluoroacetate was seen to vary depending on the level <strong>of</strong><br />

exposure <strong>of</strong> each species/ population to fluoroacetate-bearing vegetation, our findings provide further<br />

evidence <strong>of</strong> the evolutionary impact that fluoroacetate-producing plants appear to have had on the genetic<br />

composition <strong>of</strong> indigenous Australian fauna.<br />

Twyford, K. L., Humphrey, P. G., Nunn, R. P., and Willoughby, L. (2000). Eradication <strong>of</strong> feral cats (Felis<br />

catus) from Gabo Island, south-east Victoria. Ecological Management & Restoration 1, 42-49.<br />

Keywords: cats<br />

Ueno, Y. (1983). Effect <strong>of</strong> fluoroacetate on the physiological distal drift <strong>of</strong> rat molar. Bulletin <strong>of</strong> the Tokyo<br />

Medical & Dental University 30, 119-127.<br />

Keywords: fluoroacetate/inhibition/bone<br />

Abstract: The effect <strong>of</strong> fluoroacetate (FA) on the physiological distal drift <strong>of</strong> the rat molar was investigated<br />

in this study. FA produced a dose-dependent inhibition <strong>of</strong> the bone formation ratio on the modeling side.<br />

The total number <strong>of</strong> osteoclast population on the remodeling side decreased with the increase <strong>of</strong> the dose <strong>of</strong><br />

FA, but not dose-dependently. Therefore, the physiological distal drift seemed to be inhibited by the FA<br />

injections and the rate <strong>of</strong> the distal drift seemed to be not proportional to the total number <strong>of</strong> osteoclasts on<br />

the remodeling side. Among the osteoclast population, the number <strong>of</strong> multinucleated cells in contact with<br />

the bone surface (on-bone multinucleated osteoclasts) decreased considerably when the physiological distal<br />

drift was inhibited by the FA injections. The availability <strong>of</strong> the change in the number <strong>of</strong> the on-bone<br />

multinucleated osteoclasts as a marker <strong>of</strong> the degree <strong>of</strong> bone resorption was also discussed<br />

Vagelos, P. R., Alberts, A. W., and Martin, D. B. (1963). Studies on the mechanism <strong>of</strong> activation <strong>of</strong> acetyl<br />

coenzyme A carboxylase by citrate. Journal <strong>of</strong> biological chemistry 238 , 533-540.<br />

Keywords: citrate/enzyme/fluorocitrate/behaviour/Krebs cycle/biochemistry<br />

Abstract: The mechanism <strong>of</strong> citrate activation <strong>of</strong> acetyl coenzyme A carboxylase has been investigated.<br />

Several chelating agents cannot substitute for citrate in the activation <strong>of</strong> this enzyme. The activation <strong>of</strong> the<br />

enzyme by citrate is not blocked by either trans-aconitate or fluorocitrate. Fluorocitrate activates the<br />

enzyme to the same extent as citrate.<br />

Sucrose gradient centrifugation studies indicate that the enzyme has a sedimentation coefficient (s20,w) <strong>of</strong><br />

approximately 18.8 S. When the enzyme is incubated with citrate under the conditions that activate the<br />

enzyme, and then centrifuged in medium containing citrate, it sediments much faster. The approximate<br />

s20,w value <strong>of</strong> the citrate-treated carboxylase is 43 S. Centrifugation <strong>of</strong> control carboxylase in the presence<br />

<strong>of</strong> citrate did not give rise to the new, rapidly sedimenting peak. Centrifugation <strong>of</strong> citrate-treated<br />

carboxylase in the absence <strong>of</strong> citrate gave rise to a series <strong>of</strong> peaks, none <strong>of</strong> which was in the usual location<br />

<strong>of</strong> the citrate-treated enzyme. The change in sedimentation behaviour is quite specific as to the Krebs cycle<br />

compounds that can cause it to occur. Nonspecific protein does not sediment with the citrate-treated<br />

carboxylase.<br />

Further studies on the activation process have shown that activation by citrate does not occur at 0º, that the<br />

rate <strong>of</strong> activation at 30º is dependent upon the concentration <strong>of</strong> the enzyme, and that activation is rapidly<br />

reversible upon dilution <strong>of</strong> citrate.<br />

Valette, G. and Leclair, M. F. (1976). Influence <strong>of</strong> metabolic inhibitors on the mechanical responses<br />

observed on Rat isolated duodenum following variations <strong>of</strong> the amount <strong>of</strong> calcium in the bathing medium. J<br />

Pharmacol (Paris) 7, 549-562.<br />

Keywords: sodium fluoroacetate/fluoroacetate/cyanide<br />

Abstract: 1. Using isolated Rat duodenum previously decalcified, the authors had compared the effect <strong>of</strong><br />

various metabolic inhibitors on the increase <strong>of</strong> tonus brought about by addition <strong>of</strong> calcium ions.<br />

Conversely, the same inhibitors had been assayed on the fall <strong>of</strong> tonus following the decalcification <strong>of</strong> the<br />

same organ.<br />

4. Sodium fluoroacetate (2,0 µmol/l) and 2,4-DNP (0,27 µmol/l) induced sensitization <strong>of</strong> the organ only in<br />

case <strong>of</strong> high doses <strong>of</strong> Ca 2+ (0,45 mmol/l).<br />

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5. Sodium cyanide, sodium malonate and sodium fluoroacetate hindered the fall <strong>of</strong> tonus following the<br />

decalcification <strong>of</strong> the organ.<br />

van den Berg, M. A. and Steensma, H. Y. (1997). Expression cassettes for formaldehyde and fluoroacetate<br />

resistance, two dominant markers in Saccharomyces cerevisiae. Yeast 13, 551-559.<br />

Keywords: fluoroacetate/resistance<br />

Abstract: We employed two genes in constructing yeast expression cassettes for dominant, selectable<br />

markers. The Saccharomyces cerevisiae gene SFA1, encoding formaldehyde degydrogenase, was placed<br />

under the control <strong>of</strong> the GPD1 promoter and CYC1 terminator. The Moraxella sp. strain B gene dehH1,<br />

encoding fluoroacetate dehalogenase, was placed under the control <strong>of</strong> both the GPD1 and CYC1 promoters.<br />

With these constructs it was possible to select directly for yeast strains resistant to either formaldehyde or<br />

fluoroacetate. Both selective agents are completely metabolized and inexpensive, making them very useful<br />

in the pursuit <strong>of</strong> yeast gene functions and for industrial applications. An additional advantage <strong>of</strong> the<br />

formaldehyde dehydrogenase marker is that it is an S. cerevisiae gene, thus allowing 'all yeast' constructs.<br />

Van Dijk, C., Vickery, B., and Vickery, M. L. (1972). Poisoning <strong>of</strong> livestock by Dichapetalum toxicarium.<br />

Nigerian Journal <strong>of</strong> Science 6, 135-138.<br />

Keywords: poisoning/livestock/poison/fluoroacetate/fluorocitrate/Krebs<br />

cycle/heart/rabbits/antidote/occurrence in nature<br />

Abstract: In Njala, Sierra Leone, N'Dama cattle died or became ill. In the dry season when grass was<br />

scarce, they had eaten the palatable young leaves <strong>of</strong> Dichapetalum toxicarum. The plant is used as rat<br />

poison and has fluoro-fatty acids that are oxidised in the body to fluoroacetate and converted enzymically<br />

to fluorocitrate, which upsets the Krebs cycle in heart cells. Clinical and postmortem signs are described;<br />

similar signs were found in calves and rabbits given the leaves. Antidotes are being studied<br />

Vartiainen, T. and Kauranen, P. (1984). The determination <strong>of</strong> traces <strong>of</strong> fluoroacetic acid by extractive<br />

alkylation, pentafluorobenzylation and capillary gas chromatography-mass spectrometry. Analytica chimica<br />

acta 157, 91-97.<br />

Keywords: occurrence in nature/analysis<br />

Abstract: A method is described for the extraction and determination <strong>of</strong> nanogram amounts <strong>of</strong> the highly<br />

toxic fluoroacetic acid in plant samples. The acid is extracted by ammonia solution and purified by<br />

repeated other extractions. The fluoroacetate is then transferred to dichloromethane by using<br />

tetrahexylammonium as counter-ion, and finally derivatized by pentafluorobenzyl bromide. The<br />

determination is completed by capillary gas chromatography and single-ion monitoring mass spectrometry.<br />

Small amounts <strong>of</strong> fluoroacetate were found in many plan samples, including tea. The limit <strong>of</strong> detection was<br />

about 0.005 Fg g-1, The reproducibility about ±9% and The recovery <strong>of</strong> added fluoroacetate 89 ± 6%.<br />

Vartiainen, T. and Gynther, J. (1984). Fluoroacetic acid in guar gum. Food and chemical toxicology 22,<br />

307-308.<br />

Keywords: occurrence in nature/fluoroacetate<br />

Abstract: The toxicity <strong>of</strong> guar gum, derived from the Indian leguminous plant Cyamopsis<br />

tetragonolobus, is thought to be due to a globulin which can be denaturated and made non-toxic. Another<br />

very toxic compound, fluoroacetic acid, has been detected at a low level in raw samples <strong>of</strong> guar gum (0.07-<br />

1.42 microgram fluoroacetic acid/g). A sample <strong>of</strong> a guar-gum pharmaceutical formulation contained only<br />

0.08 ppm fluoroacetate. One exceptionally high value <strong>of</strong> 9.5 micrograms/g was found in a guar-gum<br />

powder. The low concentrations <strong>of</strong> fluoroacetate found in guar gum dispel any considerations about<br />

possible health risks associated with fluoroacetate during the prolonged use <strong>of</strong> guar gum at the<br />

recommended doses.<br />

Vartiainen, T., Takala, K., and Kauranen, P. (1995). Occurrence <strong>of</strong> fluoroacetate, a naturally-produced<br />

organohalogen, in plants. In 'Naturally-Produced Organohalogens: Selected and Edited Proceedings <strong>of</strong> the<br />

First Conference on Naturally-Produced Organohalogens'. (A. Grimvall and E. W. B. de LeerEds. ) pp.<br />

245-250. (Kluwer Academic:<br />

Keywords: fluoroacetate/occurrence in nature<br />

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Appendix C<br />

Veltman, C. J. and Pinder, D. N. (2001). Brushtail possum mortality and ambient temperatures following<br />

aerial poisoning using 1080. Journal <strong>of</strong> wildlife management 65, 476-481.<br />

Keywords: temperature/poisoning/1080/baits/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/treatment/field<br />

efficacy<br />

Abstract: Kill rates estimated after aerial broadcast <strong>of</strong> cereal baits containing sodium mon<strong>of</strong>luoroacetate<br />

(1080) to control brushtail possum (Trichosurus vulpecula) populations in New Zealand varied from 61-<br />

100% in 48 operations between 1994 and 1999. Possum mortality was not related to size <strong>of</strong> treated area,<br />

toxin concentration, bait sowing rate or year <strong>of</strong> operation. We tested the hypothesis that ambient<br />

temperature influenced operational outcome using temperature measurements from meteorological<br />

recording stations (local scale) and latitude (regional scale) nearest to application sites. Field temperatures<br />

ranged from 3.0 - 17.4 o C, and both temperature and latitude contributed significantly to a regression model<br />

for predicting possum kill rates. Highest estimated kill rates were observed during winter and at southern<br />

latitudes, consistent with previous laboratory studies <strong>of</strong> 1080 toxicity at warm and cool temperatures.<br />

Modeling showed populations that were reduced by more than 90% returned to 95% <strong>of</strong> initial density after<br />

14.5 years, while sites with a kill rate <strong>of</strong> 70% needed only 9 years to reach 95% <strong>of</strong> initial density. During 9<br />

years following an operation, simulated average possum densities were over 2 times greater in forests that<br />

experienced a 70% kill. Shorter intervals between control operations led to lower averge densities for given<br />

kill rates in simulated populations. Therefore, we recommend that managers limit their operations to<br />

months with the coldest average temperatures and consider varying treatment intervals to remedy the<br />

ecological effects <strong>of</strong> low possum mortality after some operations.<br />

Vickery, B. and Vickery, M. L. (1972). Fluoride metabolism in Dichapetalum toxicarium. Phytochemistry<br />

11, 1905-1909.<br />

Keywords: fluoride/metabolism/mon<strong>of</strong>luoroacetic acid/mon<strong>of</strong>luoroacetate/livestock/occurrence in nature<br />

Abstract: Samples <strong>of</strong> the toxic plant D. toxicarium were collected from a 20-km2 area at Njala, and<br />

analysed. No free mon<strong>of</strong>luoroacetic acid was detected in the leaves, but the mon<strong>of</strong>luoroacetate ion (MFA)<br />

was present. MFA concentration was highest in leaves adnate to the flowers (1100 ppm on a fresh tissue<br />

basis), young leaves (450) and young stems (270), was lowest in the wet season and highest in the hot, dry<br />

season. D. toxicarium, however, was toxic to livestock throughout the year. The fluoride ion was an<br />

intermediate in the synthesis <strong>of</strong> MFA and it was concluded that D. toxicarium had an unusual ability to<br />

withdraw fluoride from a low fluoride environment<br />

Vickery, B. and Vickery, M. L. (1973). Toxicity for livestock <strong>of</strong> organ<strong>of</strong>luorine compounds present in<br />

Dichapetalum plant species. The Veterinary Bulletin 43, 537-542.<br />

Keywords: livestock/goats/dogs/rabbits/occurrence in nature/mode <strong>of</strong> action/symptoms/antidote<br />

Abstract: When the Voortrekkers crossed the Transvaal in the 1830s they found that their cattle died after<br />

eating the leaves <strong>of</strong> a particular, small, green-leaved plant. This plant was given the Afrikaans name<br />

gifblaar- poison leaf. Its botanical name is Dichapetalum cymosum. Since that time many cattle have been<br />

poisoned by this plant, which is alos highly toxic to goats, sheep, horses, donkeys, dogs, rabbits and guineapigs.<br />

Apart from D. cymosum, there are at least twelve other poisonous species <strong>of</strong> the genus Dichapetalum.<br />

These are found in West, South-West, East and South Africa. The genus is , however, wodespread<br />

throughout the tropics, more than 200 species being known. The toxicity or otherwise <strong>of</strong> most <strong>of</strong> these<br />

species has not yet been determined.<br />

Vickery, B. and Vickery, M. L. (1975). The synthesis and defluorination <strong>of</strong> mon<strong>of</strong>luoroacetate in some<br />

Dichapetalum species. Phytochemistry 14, 423-427.<br />

Keywords: defluorination/mon<strong>of</strong>luoroacetate/occurrence in nature/biosynthesis/persistence in plants<br />

Villafranca, J. J. and Platus, E. (1973). Fluorocitrate inhibition <strong>of</strong> aconitase. Reversibility <strong>of</strong> the<br />

Inactivation. Biochemical and biophysical research communications 55, 1197-1207.<br />

Keywords: fluorocitrate/inhibition/aconitase/fluoride/metabolism<br />

Abstract: Fluoride ion is released nearly stoichiometrically when (-)-erythro-fluorocitrate is incubated with<br />

aconitase. The release <strong>of</strong> F - parallels the loss in activity and could arise from direct displacement <strong>of</strong> F - by a<br />

base on the enzyme or from dehydration to fluoro-cis-aconitate and attack <strong>of</strong> an enzymic base to release F - .<br />

Aconitase inactivated by 14 C-fluorocitrate does not retain radioactivity when passed through G-50<br />

Sephadex or precipitated by ammonium sulfate. Full enzymic activity can be regained after either <strong>of</strong> these<br />

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Appendix C<br />

treatments by activation by cysteine or ferrous salts. These data are consistent with the report <strong>of</strong><br />

fluorocitrate being a competitive (and non-competitive) inhibitor <strong>of</strong> acontase (Villafranca,J.J. 1972 Intra-<br />

Science Chem. Rept. 6 (4), 1-11) which rapidly inactivates the enzyme. This inactivated enzyme may be a<br />

very labile covalent complex, a very tight complex between enzyme and fluoro-cis-aconitate or a tight<br />

complex between a defluorinated derivative <strong>of</strong> fluorocitrate.<br />

Virgili, M., Paulsen, R., Villani, L., Contestabile, A., and Fonnum, F. (1991). Temporary impairment <strong>of</strong><br />

Müller cell metabolism in the rat retina by intravitreal injection <strong>of</strong> fluorocitrate. Experimental eye research<br />

53, 115-122.<br />

Keywords: mode <strong>of</strong> action/pathology/metabolism<br />

Abstract: Fluorocitrate was injected in the vitreum <strong>of</strong> rats in order to define the experimental conditions for<br />

a temporary impairment <strong>of</strong> Muller cell metabolism in the retina. Injection <strong>of</strong> 16 nmol <strong>of</strong> fluorocitrate<br />

appeared to fulfil this requirement since this dose resulted in a large decrease in retinal endogenous<br />

glutamine and a smaller decrease in glutamate within 6 hr <strong>of</strong> administration. The reversible nature <strong>of</strong> the<br />

effect was attested by a substantial recovery <strong>of</strong> the retinal levels <strong>of</strong> the two amino acids within 24 hr <strong>of</strong><br />

injection. In vitro experiments <strong>of</strong> carbon incorporation from different substrates, carried out with retinas<br />

dissected from eyes previously injected with fluorocitrate, were consistent with a metabolic impairment <strong>of</strong><br />

glial cells, since carbon incorporation from [14C]acetate into glutamine was almost completely abolished in<br />

the fluorocitrate-treated retinas. Electron microscopic examination in fluorocitrate-poisoned retinas<br />

demonstrated essentially selective ultrastructural alterations <strong>of</strong> Muller cells at times corresponding to their<br />

maximal metabolic impairment. Since Muller cells are by far the largest glial population <strong>of</strong> the rat retina,<br />

common astrocytes being only scattered in the nerve fibre layer, the present experimental model may be<br />

used to study the role <strong>of</strong> Muller cells in the metabolism <strong>of</strong> retinal neurotransmitters.<br />

Viriyanondha, P. and Baxter, R. M. (1970). Incorporation <strong>of</strong> fluoroacetate into uridine nucleotides <strong>of</strong><br />

Staphylococcus aureus. Biochim.Biophys.Acta. 201, 495-496.<br />

Keywords: fluoroacetate/bacteria<br />

Visscher, P. T., Culbertson, C. W., and Oremland, R. S. (1994). Degradation <strong>of</strong> trifluoroacetate in oxic and<br />

anoxic sediments. Nature 369, 729-731.<br />

Keywords: degradation/soil/mon<strong>of</strong>luoroacetate/bacteria/chemistry<br />

Abstract: The deleterious effect <strong>of</strong> chlor<strong>of</strong>luorocarbons on stratospheric ozone has led to international<br />

cooperation to end their use.The search for acceptable alternatives has focused on hydr<strong>of</strong>luorocarbons<br />

(HFCs) or hydrochlor<strong>of</strong>luorocarbons (HCFCs) which are attractive because they have relatively short<br />

atmospheric residence times. HFCs and HCFCs are attacked by tropospheric hydroxyl radicals, leading to<br />

the formation <strong>of</strong> trifluoroacetate (TFA). Most <strong>of</strong> the atmospheric TFA is deposited at the Earths surface,<br />

where it is thought to be highly resistant to bacterial attack. Therefore, use <strong>of</strong> HFCs and HCFCs may lead<br />

to an accumulation <strong>of</strong> TFA in soils, where it could prove to be toxic or inhibitory to plants and soil<br />

microbial communities. Although little is known about the toxicity <strong>of</strong> TFA, mon<strong>of</strong>luoroacetate, which<br />

occurs at low levels in some plants and which is susceptible to slow attack by aerobic soil microbes, is<br />

known to be acutely toxic. Here we report that TFA can be rapidly degraded microbially under anoxic and<br />

oxic conditions. These results imply that signficant microbial sinks exist in nature for the elimination <strong>of</strong><br />

TFA from the environment. We also show that oxic degradation <strong>of</strong> TFA leads to the formation <strong>of</strong><br />

fluor<strong>of</strong>orm, a potential ozone-depleting compound with a much longer atmospheric lifetime than the parent<br />

compounds.<br />

Wade, D. A. Standard guideline for the use and development <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (Compound<br />

1080) as a predacide (ASTM Designation E 590-76). Jackson, W. B. and Marsh, R. E. ASTM Special<br />

Technical Publication 625, 157. 1976. University <strong>of</strong> California, Davis. 8-3-1976.<br />

Ref Type: Conference Proceeding<br />

Keywords: sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080<br />

Abstract: This is a "state <strong>of</strong> the art" document prepared by the Predator Task Group, American Society for<br />

Testing and Materials (ASTM) Subcommittee E35.17, as a consensus guideline for the use <strong>of</strong> Compound<br />

1080 in wild canid control. Toxicology, storage, handling, bait formulations and preparation <strong>of</strong> baits are<br />

discussed. Bait placement, exposure period, disposal, human safety factors and environmental impact are<br />

also treated. Toxicity data and a reference list also are included.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Wainwright, M. and Supharungsun, S. (1984). Release by fungi <strong>of</strong> F- from insoluble fluorides. J.????<br />

Br.mycol.Soc. 82, 289-292.<br />

Keywords: fluoride<br />

Abstract: A number <strong>of</strong> fungi capable <strong>of</strong> releasing F - from insoluble fluorides in vitro, were isolated from F -<br />

polluted soils. All isolates were capable <strong>of</strong> releasing F - from cryolite (Na3AlF6) and fluorspar (CaF2) in<br />

vitro, a process which was associated with an increase in medium pH. Fusarium culmorum and a<br />

Penicillium sp. also released F - from MgF2, in vitro, and the Penicillium sp. was able to release the ion from<br />

AlF3. Neither species grew in the presence <strong>of</strong> LiF3, or MnF2. Culture variables influencing the release <strong>of</strong> F -<br />

by fungi are reported. The Penicillium sp. was also able to release F - from cryolite when growing in<br />

autoclaved soils, but like Fusarium merismoides, it was incapable <strong>of</strong> releasing F - from fluorspar under these<br />

conditions. Implications <strong>of</strong> release <strong>of</strong> F - from insoluble fluorides on the toxicology <strong>of</strong> the element in soils,<br />

and the possibility <strong>of</strong> using fungi to remove F - from industrial raw materials are commented upon.<br />

Waldbot, G. L. (1963). Acute Fluoride Intoxication. Acta Medica Scandinavica 400, 1-44.<br />

Keywords: blood/convulsions/fluoride/humans/poison/stomach<br />

Abstract: 1. Acute intoxication with fluoride compounds through accidental exposure, homicides and<br />

suicides, is not uncommon. Epidemics <strong>of</strong> rather serious proportions have been caused by mistaking<br />

fluoride compounds for baking soda, flour, sugar, etc.<br />

2. There are wide variations in response to fluoride intake, depending on such factors as the particular<br />

fluoride compound involved, the animal species and on various biological conditions in humans. Inorganic<br />

fluorides, especially NaF and Na2SiF6, are more frequently involved in acute intoxication than organic compounds. HF, H2SiF6 and particulate<br />

NaF are mostly responsible for acute intoxication from air contamination.<br />

3. Three autopsied cases <strong>of</strong> intoxication with NaF are reported, namely two homicides and one accidental case.<br />

4. Clinical, autopsy and laboratory findings <strong>of</strong> acute fluoride intoxication are sparse and inconsistent. Hemorrhagic gastritis, tetaniform convulsions, hypoglycemia<br />

and hyperfluoruria are the principal clinical findings. There are no pathognomonic changes at autopsy. Corrosive lesions in the upper intestinal tract, congestion and<br />

hyperemia in other vital organs are usually encountered. Changes suggestive <strong>of</strong> corrosion have been reported in the respiratory tract in intoxication from airborne<br />

fluoride.<br />

5. Therapy should be directed toward removal <strong>of</strong> the poison from the stomach and intestinal tract; toward retarding its absorption into the blood stream; toward<br />

countering calcium deprivation in the blood.<br />

6. A description <strong>of</strong> the topical effect <strong>of</strong> fluoride and <strong>of</strong> allergic reactions is presented.<br />

Walker, B. (2001). New hazardous substances regime starting up. Law talk 568, 27.<br />

Keywords: regulatory toxicology/legislation/1080<br />

Walker, J. R. L. and Bong, C. L. (1981). Metabolism <strong>of</strong> fluoroacetate by a soil Pseudomonas sp. and<br />

Fusarium solani. Soil biology and biochemistry 13, 231-235.<br />

Keywords: persistence in<br />

soil/metabolism/fluoroacetamide/biochemistry/bacteria/defluorination/enzyme/temperature<br />

Abstract: Enzymes (haloacetate halidohyrolases) capable <strong>of</strong> cleaving the C-F bond <strong>of</strong> fluoroacetate and<br />

some other organ<strong>of</strong>luorine compounds have been isolated and partially purified from a soil pseudo-monad<br />

and from the common soil fungus Fusarium Solami. Both enzymes readily released F-from<br />

mon<strong>of</strong>luoroacetate and fluoroacetamide but were without effect on a wide range <strong>of</strong> other organic fcompounds.<br />

The enzymes also cleaved the C-CI and C-Br bonds in mono-chloroacetate and monobromoacetate.<br />

Inorganic F- acted as a competitive inhibitor <strong>of</strong> the enzymes. The molecular weighs both<br />

enzymes were about 62,000. This the properties <strong>of</strong> the halidohyrolases from both organisms were similar<br />

in many respects by the bacterial enzyme was more stable at 55EC and exhibited an unusual difference in<br />

temperature coefficient (q10 value) over its higher (30-55EC) and lower (15-30EC) temperature ranges.<br />

Walker, J. R. L. (1994). Degradation <strong>of</strong> sodium mon<strong>of</strong>luoroacetate by soil micro-organisms. In<br />

'Proceedings <strong>of</strong> the Science Workshop on 1080, 12-14 December 1993, Christchurch, New Zealand'. (A. A.<br />

Seawright and C. T. EasonEds. ) pp. 50-53. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: persistence in soil/1080<br />

Abstract: Using simple enrichment culture techniques micro-organisms capable <strong>of</strong> detoxifying<br />

mon<strong>of</strong>luoroacetate by removal <strong>of</strong> F-have been found in many and diverse samples <strong>of</strong> local soils. Species <strong>of</strong><br />

Pseudomonas and fusarium were found to be capable <strong>of</strong> growth on fluoroacetate as sole source <strong>of</strong> carbon<br />

whilst several other organisms display defluorinating activity if supplied with a supplementary carbon<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

source for growth. It was concluded that fluoroacetate had a relatively short biological half life in most NZ<br />

soils.<br />

Wang, F., Dicinoski, G. W., Zhu, Y., and Haddad, P. R. (2004). Simultaneous determination <strong>of</strong><br />

mon<strong>of</strong>luoroacetate, difluoroacetate and trifluoroacetate in environmental samples by ion chromatography.<br />

Journal <strong>of</strong> chromatography A 1032, 31-35.<br />

Keywords: mon<strong>of</strong>luoroacetate/ion chromatography/fluoroacetate/analysis/carrot/baits<br />

Abstract: A method is reported for the sensitive, simultaneous determination <strong>of</strong> mono- (MFA), di- (DFA),<br />

and trifluoroacetates (TFA) by ion chromatography (IC). These species were separated using a Dionex<br />

AS17 anion-exchange column employed with a potassium hydroxide gradient (via a Dionex EG40 eluent<br />

generator) and suppressed conductivity detection. The fluoroacetates were successfully separated from a<br />

range <strong>of</strong> inorganic and organic species likely to be present in environmental samples, in a total analysis<br />

time <strong>of</strong> 35 min (including re-equilibration <strong>of</strong> the column). Detection limits for mono-, di- and<br />

trifluoroacetate were 21, 38 and 36 mug/l, respectively, determined using a signal-to-noise ratio <strong>of</strong> 3, and<br />

were obtained using a sample injection volume <strong>of</strong> 50 mul. Precision was less than 0.83% relative standard<br />

deviation (RSD) for replicate injections performed over a period <strong>of</strong> 30 days. The method was applied to the<br />

determination <strong>of</strong> *mon<strong>of</strong>luoroacetate* in river water samples and also in carrot baits.<br />

Wang, S. L., Rice, S. A., Serra, M. T., and Gross, B. (1986). Purification and identification <strong>of</strong> rat hepatic<br />

cytosolic enzymes responsible for defluorination <strong>of</strong> methoxyflurane and fluoroacetate. Drug metabolism<br />

and disposition 14, 392-398.<br />

Keywords: metabolism/enzyme/defluorination/fluoroacetate/rats/liver/biochemistry<br />

Abstract: Enzymes responsible for the defluorination <strong>of</strong> methoxyflurane (MOF) and fluoroacetate (FAc)<br />

were separated and purified from rat liver cytosol. Both hepatic cytosolic enzymes with defluorination<br />

activity were labile and addition <strong>of</strong> 2-mercaptoethanol had little effect on the stability <strong>of</strong> these enzymes.<br />

Glutathione S-transferase (GT) activity <strong>of</strong> the same cytosolic fractions was stable for at least 11 days.<br />

Separation <strong>of</strong> defluorination and GT ezymatic activities on DEAE-Sephadex A-50 and reduced glutathioneaffinity<br />

columns revealed that the defluorination <strong>of</strong> MOF and FAc were primarily catalyzed by anionic<br />

proteins which also exhibited GT activity. Further identification by two-dimensional sodium dodecyl<br />

sulfate-polyacrylamide gel electrophoresis showed protein bands with pl values <strong>of</strong> approximately 6.5 and<br />

6.9 and molecular weights <strong>of</strong> approximately 20,000. However, other proteins that exhibited no GT activity<br />

also defluorinated MOF and FAc, but accounted for only 10% <strong>of</strong> the total defluorination activity present in<br />

anionic proteins. Results from a separate purification experiment using a CM-cellulose column also<br />

indicated that the enzymes responsible for defluorination coeluted with cationic GTs. Collectively, these<br />

cationic enzymes were responsible for about 20% <strong>of</strong> the recovered cytosolic defluorination activities. The<br />

results suggest that the cytosolic defluorinations <strong>of</strong> both MOF and FAc are primarily the result <strong>of</strong> a<br />

dehalogenation reaction catalyzed by one or more species <strong>of</strong> rat liver cytosolic GTs.<br />

Warburton, B. (1990). <strong>Control</strong> <strong>of</strong> Bennett's and Tammar wallabies in New Zealand using compound 1080<br />

gel on foliage baits. Australian wildlife research 17, 541-546.<br />

Keywords: ground control/field efficacy/target species/1080/baits/marsupials<br />

Ward, A. A. (1947). Convulsive activity induced by fluoroacetate. Journal <strong>of</strong> neurophysiology 10, 105-111.<br />

Keywords: fluoroacetate/symptoms/convulsions/brain/cats/carnivores<br />

Abstract: Intravenous injection <strong>of</strong> sodium fluoroacetate causes local, rythymic, seizure discharges in<br />

subcortical structures. These occur at a time when the animal is exhibiting repeated tonic seizures. There is<br />

no clear correlation between the electricla activity <strong>of</strong> the cortex and the paroxysmal activity occurring in the<br />

thalamus, hypothalamus or reticular formation <strong>of</strong> the pons. Dome and spike activity has been recorded from<br />

the cortex synchronously with rapid seizure discharges in subcortical structures.<br />

Ward, J. C. (1946). Rodent control with 1080, ANTU and other war-developed toxic agents. American<br />

journal <strong>of</strong> public health 36, 1427-1431.<br />

Keywords: 1080/field efficacy/rodents<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Ward, J. C. and Spencer, D. A. (1947). Notes on the pharmacology <strong>of</strong> sodium fluoroacetate - compound<br />

1080. Journal <strong>of</strong> the American Pharmaceutical Association 36, 59-62.<br />

Keywords: acute toxicity/mammals/birds/sodium fluoroacetate/fluoroacetate/1080<br />

Ward, P. F. (1970). Studies on an alternative pathway for the metabolism <strong>of</strong> fluoroacetate. WAAP / IBP<br />

symposium 187-189.<br />

Keywords: metabolism/fluoroacetate/persistence in plants<br />

Ward, P. F. and Huskisson, N. S. (1978). The energy metabolism <strong>of</strong> adult Haemonchus contortus, in vitro.<br />

Parasitology 77, 255-271.<br />

Keywords: metabolism/persistence in invertebrates/invertebrates/fluorocitrate/fluoroacetate/citrate<br />

Abstract: A comparison was made <strong>of</strong> the major excretory products when adult Haemonchus contortus<br />

worms were incubated with D-[U-14C] glucose under aerobic and anaerobic conditions. Catabolites<br />

measured were propan-1-ol, acetate, n-proprionate and CO2 and the only major difference was that nearly<br />

twice as much CO2 both in terms <strong>of</strong> quantity and radioactivity was excreted under aerobic than anaerobic<br />

conditions. The worms were also much more physically active under aerobic conditions. When worms were<br />

incubated under aerobic conditions with increasing amounts <strong>of</strong> fluoroacetate their CO2 production was<br />

progressively reduced to the anaerobic level. Their movement and their ability to clump together was also<br />

progressively reduced. After aerobic incubation with fluoroacetate and D-[U- 14 C] glucose the quantity and<br />

radioactivity <strong>of</strong> citrate within worms increased greatly. When worms were similarly incubated<br />

anaerobically no increase in citrate occurred and the worms appeared physically unaffected. When worms<br />

were incubated aerobically with fluoro[1-14C] they produced radioactive fluorocitrate.<br />

Ward, P. F. V. and Huskisson, N. S. (1969). The metabolism <strong>of</strong> fluoroacetate by plants : in Proceedings <strong>of</strong><br />

the Biochemical Society short note on. Biochemical journal 113(2) [appendix], 9.<br />

Keywords: metabolism/persistence in plants<br />

Abstract: A short note on investigation <strong>of</strong> the metabolism <strong>of</strong> fluoroacetate in lettuce plants - results reported<br />

in later paperby same authors.<br />

Ward, P. F. V. and Huskisson, N. S. (1972). The metabolism <strong>of</strong> fluoroacetate in lettuce. Biochemical<br />

journal 130, 575-587.<br />

Keywords: metabolism/persistence in plants<br />

Abstract: 1. Whole lettuce plants were incubated with (1) (1-14C) acetate (2) fluoroacetate followed by (1-<br />

14C) acetate, (3) fluoro(1-14C)acetate, (4) fluoro(2-14)acetate or (5) s-carboxy(14C)methylgulathione. 2.<br />

Fluoroacetate did not affect the expiration <strong>of</strong> 14CO2 from (1-14C)acetate and only a small amount <strong>of</strong><br />

14Co2 was produced from either fluoro (1-14C)-acetate or fluoro (2-14C)acetate in 43 h. 3. Fluoroacetate<br />

at 50 mg/kg wet wt. doubled the plant citrate concentration after 43h incubation, and depending on the age<br />

and size <strong>of</strong> the plant 50-100% <strong>of</strong> the compound was metabolized. 4. With both fluoro (1-14C)acetate and<br />

fluoro (2-14C)acetate all the radioactivity except that in the CO2 was found in the water-soluble acid<br />

fraction. About 2% was in fluorocitrate and the remainder, apart from unchanged fluoroacetate was in a<br />

number <strong>of</strong> compounds devoid <strong>of</strong> fluorine but containing nitrogen and sulphur. These were peptide-like and<br />

could be separated by chromatography on an amino acid analyser. 5. Identical compounds were obtained<br />

form the spontaneous reaction between iodo (2-14C)acetate and glutathione, the major product being Scarboxy-methylglutathione.<br />

6. S-Carboxymethylcysteine was also isolated and its mass spectrum compared<br />

with a commercial sample. 7. Reaction rates <strong>of</strong> all the monohaloacetates with glutathione were studied at<br />

pH7 at 25EC. No reaction was observed with fluoroacetate. 8. The metabolism <strong>of</strong> fluoroacetate by lettuce<br />

is discussed in relation to that <strong>of</strong> aliphatic and aromatic halogen compounds, including fluoroacetate, by<br />

mammalian liver and to the metabolism <strong>of</strong> fluoroacetate by different plant reported by other workers.<br />

Ward, P. F. V. and Huskisson, N. S. (1972). Defluorination <strong>of</strong> fluoroacetate by lettuce. The Biochemical<br />

Journal 127, 89P-90P.<br />

Keywords: defluorination/fluoroacetate/metabolism<br />

Abstract: It appears that lettuce can remove fluorine from fluoroacetate in much the same way that animals<br />

remove halogens from some halogenated aliphatic compounds (Thomson et al.,1963). Unlike<br />

fluoropyruvate, fluoroacetate does not react directly with cysteine or glutathione; a catalyst such as an<br />

enzyme is required.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Watts, M. Parkinson's disease, pesticides and derris dust. Soil & Health, Pesticide Report , 16-18. 2001.<br />

Ref Type: Report<br />

Keywords: 1080/humans/sublethal effects<br />

Abstract: In September last year we reported on the medical finding <strong>of</strong> Parkinson's disease as a result <strong>of</strong><br />

exposure to 2,4-D in Northland. In November, the mainstream media published the results <strong>of</strong> a laboratory<br />

study linking the disease to rotenone, more commonly known as Derris Dust. There is a gathering body <strong>of</strong><br />

evidence and worldwide concern that exposure to pesticides might be an important triggering factor in the<br />

development <strong>of</strong> this devastating and irreversible condition <strong>of</strong> the nervous sytem. We take a closer look at<br />

the problem.<br />

Weaver, S. A. (2003). Policy implications <strong>of</strong> 1080 toxicology in New Zealand. Journal <strong>of</strong> Rural and<br />

Remote Environmental Health 2, 46-58.<br />

Keywords: 1080/New Zealand/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/pest/poison/temperature<br />

Abstract: Sodium mon<strong>of</strong>luoroacetate (1080) is used for large-scale pest control operations in New Zealand<br />

to control the introduced marsupial brush tailed possum. Wide-scale opposition to the use <strong>of</strong> 1080 had<br />

grown in recent years with the development <strong>of</strong> a substantial "anti 1080" lobby. Concerns for public health<br />

and effects on non-target animals among critics <strong>of</strong> 1080 have prompted the Environmental Risk<br />

Management Authority to undertake an <strong>of</strong>ficial review <strong>of</strong> this pesticide. In anticipation <strong>of</strong> this regulatory<br />

review an evaluation <strong>of</strong> the peer-reviewed scientific literature was conducted on the risks associated with<br />

the use <strong>of</strong> 1080, in order to ascertain the dgreee to which regulations <strong>of</strong> 1080 reflect current scientific<br />

knowledge <strong>of</strong> the toxicology <strong>of</strong> this poison. Key areas <strong>of</strong> concern revealed in the literature incldue evidence<br />

that 1080 could have endocrine disrupting capabilities and that it is relatively slow to break down to low<br />

temperature when microbial activity is low. These two issues are yet to be fully resolved through further<br />

research and represent significant gaps in current knowledge. If regulations are to take full account <strong>of</strong><br />

current science on 1080 they will need to acknowledge and reflect what is known, the gaps in thie<br />

knowledge, and the risks asscoaited with this uncertainty. Recommendations include further targeted<br />

research to fill gaps in current knowledge, regulatory precaution intil such research is completed, and<br />

explorations <strong>of</strong> alternative methods to be used euther in conjunction with, or instead <strong>of</strong> this toxin.<br />

Weis, K. Forests flourish after possum control. New Zealand Geographic 57[May-June], 10-11. 2002.<br />

Ref Type: Magazine Article<br />

Abstract: Refers to monitoring <strong>of</strong> forest after possum control in Taranaki and Wanganui.<br />

Westbrooke, I. M., Etheridge, N. D., and Powlesland, R. G. (2003). Comparing methods for assessing<br />

mortality impacts <strong>of</strong> an aerial 1080 pest control operation on tomtits (Petroica macrocephala toitoi) in<br />

Tongariro Forest. New Zealand journal <strong>of</strong> ecology 27, 115-123.<br />

Keywords: 1080/poisoning/baits/poison/non-target species/birds<br />

Abstract: This study aimed to estimate the level <strong>of</strong> mortality <strong>of</strong> North Island tomtits (Petroica macrocephala<br />

toitoi) during an aerial 1080 possum poisoning operation in Tongariro Forest, New Zealand, and to evaluate<br />

transect-based alternatives to banding for monitoring tomtit populations. The operation used 12 g toxic<br />

(1080 at 0.15% weight/weight) cereal baits sown at 3 kg/ha. Transects were established at three<br />

neighbouring sites; two within the 1080 poison area, and one outside. The re-sighting <strong>of</strong> 14 out <strong>of</strong> 15<br />

banded male tomtits at one site within the 1080 operation indicated that mortality was low. This was<br />

backed up by results from a before-after-control-impact (BACI) design to analyse density estimates from<br />

distance sampling along transects. We analysed the change in counts <strong>of</strong> territorial males before and after<br />

the operation based on the same transect surveys. This also showed little impact <strong>of</strong> poisoning on tomtits,<br />

and indicated that loss rates greater than 8.4% due to 1080 were incompatible with the data (95% one-sided<br />

confidence bound). Counts <strong>of</strong> territorial males gave a much tighter confidence bound than the banding or<br />

distance sampling results. Of the techniques applied, the counting <strong>of</strong> territorial males appears to have the<br />

most promise for providing high-precision estimates <strong>of</strong> short-term impacts, by taking full advantage <strong>of</strong> the<br />

territorial habits <strong>of</strong> male tomtits in spring. However, distance sampling shows potential for providing the<br />

basis for longer-term monitoring <strong>of</strong> tomtit populations. The transect-based approaches involved<br />

substantially fewer resources than banding for estimating short-term impacts, and <strong>of</strong>fer a considerably lessintensive<br />

means <strong>of</strong> longer-term monitoring <strong>of</strong> tomtits.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Western Australian Department <strong>of</strong> Agriculture (1973). Poison plants <strong>of</strong> Western Australia. The toxic<br />

species <strong>of</strong> the genera Gastrolobium and Oxylobium. Western Australian Department <strong>of</strong> Agriculture Bulletin<br />

3772, -66.<br />

Keywords: occurrence in nature<br />

Wheeler, S. H. and Oliver, A. J. (1978). The effect <strong>of</strong> rainfall and moisture on the 1080 and pindone<br />

content <strong>of</strong> vacuum-impregnated oats used for control <strong>of</strong> rabbits, Oryctolagus cuniculus. Australian wildlife<br />

research 5, 143-149.<br />

Keywords: bait degradation/1080/rabbits<br />

Abstract: The effect <strong>of</strong> rainfall, dew and soil moisture on the losses <strong>of</strong> pindone (2-pivalyl-1,3 indandione)<br />

and 1080 (sodium mon<strong>of</strong>luoroacetate) from vacuum-impregnated oat grains used for rabbit control are<br />

described. 1080 is lost much faster than pindone. The practical significance <strong>of</strong> these results is discussed.<br />

Wheeler, S. H. and Hart, D. S. (1979). The toxicity <strong>of</strong> sodium mon<strong>of</strong>luoroacetate to wild rabbits,<br />

Oryctolagus cuniculus (L.), from three sites in Western Australia. Australian wildlife research 6, 57-62.<br />

Keywords: acute toxicity/mammals/rabbits<br />

Whittem, J. H. and Murray, L. R. (1963). The chemistry and pathology <strong>of</strong> Georgina River poisoning.<br />

Australian veterinary journal 39, 168-173.<br />

Keywords: acute toxicity/mode <strong>of</strong> action/mammals/occurrence in<br />

nature/pathology/poisoning/fluoroacetate/heart/sublethal effects<br />

Abstract: A fatal disease <strong>of</strong> cattle and sheep which has come to be known as Georgina River poisoning or<br />

gidyea poisoning has been know to occur in the region <strong>of</strong> the Georgina River basin in the eastern Northern<br />

Territory and western Queensland since the early days <strong>of</strong> settlement. Bell et al (1955) have described the<br />

history and distribution <strong>of</strong> the disease in Queensland and established that it is due to the ingestion <strong>of</strong> the<br />

pods and leaves <strong>of</strong> the gidyea tree Acacia georgina. Barnes (1958) described the disease in the Northern<br />

Territory and confirmed that is can be produced by experimental feeding <strong>of</strong> the leaves and pods <strong>of</strong> the<br />

gidyea tree. Neither author described in detail the pathology and histopathology.<br />

Subsequent investigations in the Northern Territory and Queensland have revealed that the toxic principle<br />

<strong>of</strong> the gidyea tree is the fluoroacetate ion (Murray, McConnell and Whittem 1961; Oelrichs and McEwan<br />

1961).<br />

This paper presents details <strong>of</strong> the phyto-chemical investigation carried out in the Northern territory and an<br />

account <strong>of</strong> the histopathology <strong>of</strong> Georgina River poisoning as established by the study <strong>of</strong> a considerable<br />

number <strong>of</strong> natural and experimental cases in cattle and sheep. The lesions <strong>of</strong> experimental fluoroacetate<br />

poisoning in sheep and guinea pigs are also described.<br />

Wickstrom, M. and Eason, C. T. (1997). Sample collection for the diagnosis <strong>of</strong> 1080 poisoning in livestock.<br />

Vetscript New Zealand 10(7), 30.<br />

Keywords: acute toxicity/diagnosis/1080<br />

Abstract: Numerous cases <strong>of</strong> susepect accidental poisoning <strong>of</strong> livestock with sodium mon<strong>of</strong>luoroacetate<br />

(1080) occur in New Zealand every year. Veterinarians are <strong>of</strong>ten called upon to perform postmortem<br />

examinations and collect samples to confirm the cause <strong>of</strong> death. Inadequate or inappropriate sample<br />

collection, handling or analysis significantly weakens the livestock owner's ability to prove liability and<br />

obtain compensation for loses from the Regional Council or other authority involved in the pest control<br />

operation. This article outlines the correct procedures for sample collection and handling to establish a<br />

diagnosis <strong>of</strong> 1080 toxicosis in livestock.<br />

Wickstrom, M., Milne, L., Eason, C. T., and Arthur, D. The short- and long-term effects <strong>of</strong> a single<br />

exposure <strong>of</strong> 1080 in sheep. <strong>Landcare</strong> <strong>Research</strong> Contract Report: LC9798/40 , -9. 1997.<br />

Ref Type: Report<br />

Keywords: 1080/brain/heart/mammals/sublethal effects/developmental toxicity/gut/livestock<br />

Abstract: Ewes that survived a single exposure to 1080 did not experience any adverse long-term effects.<br />

Over 2 years, including two lambing cycles, 1080-exposed (n=21) and control ewes did not differ in the<br />

following indices <strong>of</strong> health and productivity; incidence <strong>of</strong> infectious <strong>of</strong> metabolic disease, chronic organ<br />

damage, mortality, general condition / live weight, fleece weight, lambing percentage, lamb birth weight,<br />

lamb survival and growth rate. Contrary to preliminary findings that indicated no evidence <strong>of</strong> 1080-induced<br />

217


1080 Reassessment Application October 2006<br />

Appendix C<br />

lesions 14 days after exposure (Miekle et al 1996), detailed histopathological examination <strong>of</strong> heart sections<br />

using special stains revealed scattered foci <strong>of</strong> fibrous tissue in cardiac muscle more than 2 years after the<br />

single 1080 dose. These lesions may represent scarring resulting from toxin-induced damage to heart tissue.<br />

The clinical significance <strong>of</strong> these lesions in uncertain, but is likely to be minor given the lack <strong>of</strong> evidence<br />

for any adverse effects over a 2-year period. From a diagnostic perspective, this type <strong>of</strong> lesion is rather nonspecific<br />

and could result from other toxic or non-toxic insults causing damage to heart muscle. Finding<br />

similar lesions in animals suspected <strong>of</strong> exposure to 1080 would strengthen the case for toxicosis, but their<br />

presence or absence could not be considered definitive pro<strong>of</strong>.<br />

Wickstrom, M. L., Cook, C. J., and Eason, C. T. (1998). Development <strong>of</strong> antidotes and improved treatment<br />

<strong>of</strong> 1080 toxicosis. (Manaaki Whenua - <strong>Landcare</strong> <strong>Research</strong>: Lincoln.)<br />

Keywords: treatment/1080<br />

Abstract: Objectives : To improve veterinary treatment <strong>of</strong> non-target animals exposed to 1080 by:<br />

Determining the efficacy <strong>of</strong> anion exchange resins and other potential 1080 absorbents to decrease toxin<br />

uptake and reduce mortality in orally dosed rats; Determining the efficacy <strong>of</strong> specific glutamate<br />

antagonists, GABA (gamma amino butyric acid) agonists, and other neurotransmitter modulators to reduce<br />

the severity <strong>of</strong> seizures and increase the survival <strong>of</strong> rats exposed to 1080; Determining the efficacy <strong>of</strong> the<br />

best binding agent to reduce 1080 uptake, and the effectiveness <strong>of</strong> peritoneal dialysis to enhance<br />

elimination <strong>of</strong> the toxin in anaesthetised dogs dosed with 1080.<br />

Conclusions : Although both Carbosorb and colestipol were effective at binding 1080 in vitro, and<br />

colestipol reduced 1080 serum concentration by 50% during the first 4 h after exposure in a previous study<br />

(Wickstorm et al. 1998, unpub;.), neither compound appears able to reduce absorption sufficiently to affect<br />

survival in rats given a high dose <strong>of</strong> 1080, even when a large amount <strong>of</strong> absorbent is given immediately<br />

after dosing; Oral administration <strong>of</strong> a mixture <strong>of</strong> centrally acting, neurotransmitter modulating agents<br />

appears to provide significant protection from the lethal effects <strong>of</strong> 1080 in rats given an LD80 dose <strong>of</strong> the<br />

toxin. The margin <strong>of</strong> safety with this mixture <strong>of</strong> potent compounds is rather small, since treatment at 2-4<br />

times the therapeutic dose actually contributed to mortality in 1080-exposed rats, by excessive depression<br />

<strong>of</strong> the central nervous system or reduction/disruption <strong>of</strong> baseline transmission levels required to maintain<br />

homeostasis; Unlike the results seen in rats in a previous study (Wikerstorm et al. 1998, unpubl.),<br />

administration <strong>of</strong> colestipol to anaesthetised dogs immediately after oral 1080 dosing does not appear to<br />

significantly inhibit toxin absorption from the gastrointestinal tract; Peritoneal dialysis is not effective at<br />

reducing 1080 blood concentrations in orally dosed dogs, even though substantial amounts <strong>of</strong> toxin can be<br />

removed from circulation in the dialysate.<br />

Wiedemann, P., Szinicz, L., and Weger, N. (1983). Biochemical aspects <strong>of</strong> fluoroacetate poisoning in<br />

isolated rat kidney tubules: reversibility <strong>of</strong> inhibition <strong>of</strong> gluconeogenesis by α−ketoglutarate. Toxicology in<br />

the use, misuse and abuse <strong>of</strong> food, drugs and chemicals, Arch.Toxicol., Suppl.6 232-237.<br />

Keywords: fluoroacetate/poisoning/kidney/inhibition/citrate<br />

Abstract: The effects <strong>of</strong> fluoroacetate (FAC) on suspensions <strong>of</strong> isolated rat kidney tubules were<br />

investigated. FAC inhibited gluconeogenesis from lactate, pyruvate, fructose, dihydroxyacetone,<br />

α−ketoglutarate and succinate. The gluconeogenesis from pyruvate, ketoglutarate and lactate was less<br />

sensitive to FAC than that from other substrates. FAC also caused a decrease in oxygen consumption,<br />

hydroxybutyrate to acetoacetate ratio, α−ketoglutarate, ATP and total adenine nucleotide content; the<br />

citrate content was increased. Addition <strong>of</strong> α−ketoglutarate, 5 mmol/l, caused a reversal <strong>of</strong> gluconeogenesis<br />

inhibition, an increase in ATP content and a delay in citrate accumulation in isolated rat kidney tubules<br />

incubated with FAC.<br />

Wienhaus, H. (1973). The responses <strong>of</strong> different grapevine organs to the application <strong>of</strong> metabolic inhibitors<br />

and uncouplers during the ripening stage. Vitis 12, 105-118.<br />

Keywords: sodium fluoroacetate/fluoroacetate/fluoride/treatment/cyanide<br />

Abstract: Six respiratory inhibitors were applied to the berries and other plant parts. Sodium fluoroacetate<br />

decreased berry weight, reducing sugar and K contents, but increased titratable acidity and Ca content; it<br />

also caused stalk necrosis. Malonic acid promoted fruit sugar accumulation, lowered acidity, and did not<br />

affect weight. Sodium fluoride induced fruit skin discoloration and curtailed the rise in berry weight and<br />

sugar accumulation. After treatment with CCP (carbonyl cyanide m-chlorophenylhydrazone) berry weight,<br />

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Appendix C<br />

reducing sugars, titratable acidity, K and Ca all increased. Sodium azide and dl-glyceraldehyde had no<br />

effect<br />

Wildlife Advisory Committee. An Investigation into the use <strong>of</strong> the Poison 1080 in Tasmania. 1-32. 1990.<br />

Ref Type: Report<br />

Keywords: poison/1080<br />

Williams, A. T. (1948). Sodium fluoroacetate poisoning. Hospital Corps Quarterly 21, 16-18.<br />

Keywords: sodium<br />

fluoroacetate/fluoroacetate/poisoning/humans/symptoms/welfare/treatment/1080/inhalation<br />

Abstract: During the weighing [<strong>of</strong> 1080 powder], a small quantity <strong>of</strong> poison was blown into the writer's<br />

face and some <strong>of</strong> it was inhaled. A tart, sourish taste was shortly thereafter noted, followed almost<br />

immediately by a tingling sensation around the corners <strong>of</strong> the mouth and in the nasal passages. Becoming<br />

alarmed, medical assistance was sought. Soon the entire face had become numb, and the tingling sensation<br />

was rapidly entering the arms and legs. This was followed by spasmodic contractions <strong>of</strong> the voluntary<br />

muscles, gradual loss <strong>of</strong> speech, and within 2 and 1/2 hours after inhaling the powder as noted above,<br />

unconsciousness. No actual pain was noted during the entire onset.<br />

Williams, C. K. and Moore, R. J. (1995). Effectiveness and Cost-Efficiency <strong>of</strong> <strong>Control</strong> <strong>of</strong> the Wild Rabbit,<br />

Oryctolagus Cuniculus (L), By Combinations <strong>of</strong> Poisoning, Ripping, Fumigation and Maintenance<br />

Fumigation. Wildlife research 22, 253-269.<br />

Keywords: poisoning/treatment/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/1080/rabbits<br />

Abstract: An experiment compared effectiveness, cost and cost-efficiency <strong>of</strong> factorial combinations <strong>of</strong> the<br />

four commonly used methods <strong>of</strong> rabbit control on grazing properties in the Southern Tablelands <strong>of</strong> eastern<br />

Australia. Sixteen different treatment combinations were applied to 32 sites. The treatments comprised<br />

initial control, applied over four months, followed by repeated maintenance control on half the replicates,<br />

applied after intervals <strong>of</strong> 2, 6 and 12 months. Initial control comprised no treatment, or poisoning (P) with<br />

sodium mon<strong>of</strong>luoroacetate (1080), or warren-ripping (R), or chloropicrin pressure fumigation (F), or<br />

combinations <strong>of</strong> these (P+R, P+F, R+F, P+R+F). Maintenance control consisted <strong>of</strong> phosphine-diffusion<br />

fumigation (M). Indices <strong>of</strong> rabbit abundance were compared one month before treatments were<br />

implemented. Treatment effects were assessed one month after completion <strong>of</strong> the initial control, and one<br />

and 5-6 months after the three maintenance controls, and additionally nine months after the second<br />

maintenance control. <strong>Control</strong> combinations that were highly effective and cost-efficient included both<br />

warren-ripping and maintenance treatment. poisoning prior to warren-ripping, or fumigating subsequently,<br />

or both, improved effectiveness and cost-efficiency. Warren-ripping interacted positively with one or more<br />

subsequent fumigations, improving effectiveness and cost-efficiency non-additively. <strong>Control</strong> combinations<br />

that excluded warren-ripping were ineffective and cost-inefficient, and one combination interacted<br />

negatively. Single treatments <strong>of</strong> poisoning or fumigation were cost-inefficient, allowing rabbits to<br />

recolonise rapidly to densities higher than original. Only multiple combination treatments or repeated<br />

applications were highly effective and cost-efficient; single applications <strong>of</strong> any method were inefficient and<br />

costly. The most effective and cost-efficient combination comprised the maximum six applications<br />

including ripping and maintenance treatment, namely P+R+F+M. The high effort and expenditure on the<br />

initial control resulted in high effectiveness and cost-efficiency, which maintenance control sustained at<br />

low cost. Maintenance treatments sustained or achieved effective control <strong>of</strong> rabbits; the cost <strong>of</strong> maintenance<br />

treatments halved on each repetition. [References: 28]<br />

Williams, D. Animal welfare aspects <strong>of</strong> the use <strong>of</strong> sodium fluoroacetate to poison wild rabbits. Fisher, P.<br />

and Marks, C. A. Humaneness and vertebrate pest control : proceedings <strong>of</strong> the seminar held on March 27th<br />

1996. 37-41. 1996. [Melbourne], Agriculture Victoria, Dept. <strong>of</strong> Natural Resources and Environment.<br />

Report series / Victorian Institute <strong>of</strong> Animal Science. Vertebrate Pest <strong>Research</strong> Unit.<br />

Ref Type: Conference Proceeding<br />

Keywords: welfare/rabbits/sodium fluoroacetate/fluoroacetate/poisoning/poison/1080/lethal<br />

dose/convulsions/cardiac<br />

Abstract: The effect <strong>of</strong> 1080 on a rabbit is dose dependent. A lethal dose results in a period <strong>of</strong> weakness,<br />

not attended by evidence <strong>of</strong> pain, which precedes unconsciousness. Convulsions occur only after the rabbit<br />

loses consciousness and is insensible to pain. The convulsions are due to barin anoxia resulting from acute<br />

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cardiac failure and circulatory collapse. Poisoning with sublethal doses <strong>of</strong>ten results in anorexia but rabbits<br />

recover fully within 24-48 hours. Killing rabbits with 1080 does not contravene the spirit <strong>of</strong> the Prevention<br />

to Cruelty to Animals Act 1986 because there is no evidence that its use causes pain.<br />

Williams, J. M. (1994). Food and fibre markets and societal trends: implications for pest management. In<br />

'Proceedings <strong>of</strong> the Science Workshop on 1080. 12-14 December 1993, Christchurch, New Zealand.'. (A.<br />

A. Seawright and C. T. EasonEds. ) pp. 20-32. (<strong>Royal</strong> Society <strong>of</strong> New Zealand: Wellington.)<br />

Keywords: 1080/possums/rabbits<br />

Abstract: In global markets New Zealand is in the business <strong>of</strong> pampering the palates <strong>of</strong> the prosperous.<br />

Our sophisticated markets, in east and west, are demanding ever-higher quality in foods and fibres, both in<br />

the product and in the environment in which they are produced. The market scene <strong>of</strong> the 1990s will be<br />

influenced more strongly by concerns for personal health, the environment in general and concerns for<br />

nature in terms <strong>of</strong> animal welfare.<br />

For New Zealand, these factors mean that our clean, green image must be substantive. Perceptions <strong>of</strong><br />

"quality" will be governed as much by the way we manage, and are seen to manage, our natural and manmade<br />

environments, as by scientific evidence <strong>of</strong> safety <strong>of</strong> inputs or product quality.<br />

Parallel to these trends is a growing disenchantment in influential sectors <strong>of</strong> western society, with what<br />

science and modern medicine has provided, there is a rising level <strong>of</strong> environmental awareness. These<br />

trends are expressed in many ways: debates on the benefits <strong>of</strong> bio-technology; the increase in medical<br />

ethics committees; and "phobic" responses to perceived chemical risks, e.g. Alar on apples. These societal<br />

trends are having an impact on public perceptions <strong>of</strong> the seriousness <strong>of</strong> pests and the risks associated with<br />

various control methods. One <strong>of</strong> the few studies <strong>of</strong> perceptions <strong>of</strong> pest risks in New Zealand revealed that<br />

rabbits and possums were considered "serious" or "very serious" pests by 93% and 90%, respectively, <strong>of</strong><br />

1,000 respondents. However, only 44-45% considered 1080 a suitable or very suitable control method.<br />

Biological control, via disease, was slightly more acceptable (46-49%), while shooting was favoured by 68-<br />

69%. This highlights one <strong>of</strong> the great needs <strong>of</strong> pest research: study <strong>of</strong> the societal values threatened by<br />

pests or the control methods. For too long, pest researchers and controllers have focused on pest damage<br />

(impacts) and control efficacy and safety. The future use <strong>of</strong> 1080 in New Zealand is now critically<br />

dependent on establishing consensus on:<br />

(a) What values possums and rabbits threaten;<br />

(b) What are the ways (including 1080) <strong>of</strong> protecting or enhancing these values;<br />

(c) What are the risks associated with each <strong>of</strong> the "ways".<br />

This will require a significant increase in risk perception and societal values research. On-going refinement<br />

<strong>of</strong> the understanding <strong>of</strong> 1080 chemistry and bio-impacts will do little to allay societal concerns. Future<br />

emphasis must be on understanding the values bases from which such concerns arise and on developing<br />

strategies to address the concerns, while reducing pest and market risks.<br />

Williamson, J. R., Jones, E. A., and Azzone, G. F. (<strong>1964</strong>). Metabolic control in perfused rat heart during<br />

fluoroacetate poisoning. Biochemical and biophysical research communications 17, 696-702.<br />

Keywords: heart/fluoroacetate/poisoning/fluorocitrate/inhibition/citrate/aconitase/metabolism/mode <strong>of</strong><br />

action<br />

Abstract: These results suggest that although the initial effect <strong>of</strong> fluoroacetate is to give rise to fluorocitrate,<br />

the secondary inhibition <strong>of</strong> phosph<strong>of</strong>ructokinase by the accumulated citrate is actually lethal since it<br />

deprives the cell <strong>of</strong> pyruvate which would eventually overcome the inhibition <strong>of</strong> aconitase.<br />

Williamson, J. R. (1967). Glycolytic control mechanisms III. effects <strong>of</strong> iodoacetamide and fluoroacetate on<br />

glucose metabolism in the perfused rat heart. Journal <strong>of</strong> biological chemistry 242, 4476-4485.<br />

Keywords: mode <strong>of</strong> action/fluoroacetate/metabolism/heart/citrate/enzyme<br />

Williamson, J. R. and Corkey, B. E. (1979). [23] Assay <strong>of</strong> citric acid cycle intermediates and related<br />

compounds - update with tissue metabolite levels and intracellular distribution. In 'Methods in<br />

Enzymology, Volume LV. Biomembranes: Part F: Bioenergetics-Oxidative Phosphorylation'. (S. Fleischer<br />

and L. PackerEds. ) pp. 200-222. (Academic Press: New York, San Francisco, London.)<br />

Keywords: citric acid/metabolism/citrate<br />

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Appendix C<br />

Wilson, C. and Cannon, J. (2004). Community consultation processes for aerial 1080 applications. Science<br />

for Conservation 247, -52.<br />

Keywords: 1080/New Zealand/baits/poison<br />

Abstract: <strong>Research</strong> is reported on case studies in six localities throughout New Zealand where the<br />

Department <strong>of</strong> Conservation (DOC) and communities have engaged in consultation processes on possum<br />

control and aerial spreading <strong>of</strong> 1080-poisoned baits. Information from DOC staff and community groups<br />

and individuals was obtained by interviews and focus group discussions. The report provides an overview<br />

<strong>of</strong> the consultation and information-sharing process used in each case study. Key factors discussed that can<br />

influence community consultation processes (aside from the methods and tools adopted) included: differing<br />

perceptions <strong>of</strong> what 'consultation' meant; the approach and attitude <strong>of</strong> DOC staff; risk perceptions <strong>of</strong> aerial<br />

spreading <strong>of</strong> 1080 poison; community impressions <strong>of</strong> different organisations and contractors involved;<br />

differing structures and social contexts <strong>of</strong> communities; and media involvement. The various processes and<br />

methods used by staff when undertaking community consultation and information sharing over aerial 1080<br />

are assessed. The report also highlights key considerations for staff who are involved in community<br />

consultation processes. Consultation should be part <strong>of</strong> a wider relationship-building process with<br />

communities, but the need to clearly define what DOC is consulting on in any operation is emphasised.<br />

Winfrey, M. R. and Zeikus, J. G. (1979). Anaerobic metabolism <strong>of</strong> immediate methane precursors in Lake<br />

Mendota. Applied and environmental microbiology 37, 244-253.<br />

Keywords: metabolism/fluoroacetate/bacteria/persistence in water/inhibition<br />

Abstract: Lake Mendota sediments and the immediate overlying water column were studied to better<br />

understand the metabolism <strong>of</strong> methanogenic precursors H2/CO2 and acetate in nature. Air and nitrate<br />

addition inhibited CH4 formation and stimulated CO2 production, whereas fluoroacetate addition totally<br />

inhibted acetate metabolism.<br />

Wolfe, G. W. Subchronic toxicity study in rats with sodium fluoroacetate. HLA Study No. 2399-118, -505.<br />

7-12-1998.<br />

Ref Type: Report<br />

Keywords: rats/sodium fluoroacetate/fluoroacetate/heart/testes/reproductive<br />

effects/chemistry/fluorocitrate/spleen/pathology/brain<br />

Abstract: The test material, sodium fluoroacetate (RN62-74-8) was administered by oral gavage to<br />

Sprague-Dawley rats (20 animals/sex/group), to evaluate its subchronic toxicity. The rats received 0.05,<br />

0.20 and 0.50 mg/kg/day sodium fluoroacetate (Groups 2 to 4 respectively) in deionized water for 13<br />

weeks. The controls (Group 1) received deionized water only. Criteria evaluated included mortality, clinical<br />

signs, body weights, total food consumption, opthalmologic examinations, hematology, clinical chemistry,<br />

organ weights, organ-to-body weight ratios, gross- and histopathology. No treatment-related findings were<br />

noted in survival, clinical observations, mean body weights, body weight gains, total food consumption,<br />

opthalmological examinations, or hematology and clinical chemistry findings, except for fluorocitrate<br />

results. Fluorocitrate levels were significantly increased at Week 4 in group 4 males and Groups 3 and 4<br />

females and at Week 13 in Groups 3 and 4 <strong>of</strong> both sexes. Treatment-related findings were noted in absolute<br />

and/or relative organ weights <strong>of</strong> the heart, testes/epididymides, and spleen. Absolute and relative heart<br />

weights were signficantly increased in Group 4 males and Group 3 and 4 females. Absolute spleen weights<br />

were significantly decreased in Group 4 males. Significant decreases in absolute and relative<br />

testes/epididymides weights in Groups 3 and 4 males were accompanied by corresponding findings in gross<br />

and microscopic pathology. At necropsy, testes/epididymides were noted as small. Microscopic examintion<br />

<strong>of</strong> the tissues revealed compound-related findings in the testes and epididymides and the mid and high-dose<br />

(Groups 3 and 4) rats. Testicular changes consisted <strong>of</strong> bilateral hypospermatogensis with fusion bodies in<br />

the seminiferous tubules. Changes in the epididymides consisted <strong>of</strong> immature/abnormal sperm forms and<br />

hypospermatogenesis with reduced numbers <strong>of</strong> sperm forms in the epididymal ducts. Testes and<br />

epididymides from low-dose rats showed no evidence <strong>of</strong> compound-related effects. No treatment-related<br />

effects were observed in the other tissues <strong>of</strong> the males or in any <strong>of</strong> the tissues <strong>of</strong> the females. The findings<br />

<strong>of</strong> this study indicated that the no-observed-effect-level (NOEL) for sodium fluoroacetate, when given<br />

orally to Sprague-Dawley rats for 13 weeks, was 0.05 mg/kg/day.<br />

Wong, D. Outfoxing the fox: Microbial degradation <strong>of</strong> compound 1080. Curtin Gazette 3[3], 22-24. 1988.<br />

Ref Type: Magazine Article<br />

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Appendix C<br />

Keywords: 1080/bait degradation/persistence in soil/non-target species/foxes/soil/degradation<br />

Abstract: Over the last few years there has been an increasing awareness <strong>of</strong> the need for fox control in<br />

Australia to protect native species <strong>of</strong> fauna from excessive levels <strong>of</strong> predation and possible extinction.<br />

Compound 1080, a poiosn impregnated into various types <strong>of</strong> baits has been used to control foxes by the<br />

department <strong>of</strong> Conservation and Land Management and the Agriculture Protection Board in Western<br />

Australia. Studies on the degradation <strong>of</strong> compound 1080 in bait materials and Western Australian soils,<br />

conducted by Dr. Dee Wong, Lecturer in the School <strong>of</strong> Medical Technology at the University, have<br />

provided vital information on long term environmental hazards.<br />

Wong, D. H., Kinnear, J. E., Runham, C. F., and DenHollander, L. C. (1991). A preliminary report on a<br />

bacteriological assay for compound 1080 (sodium mon<strong>of</strong>luoroacetate). Letters in applied microbiology 12,<br />

161-163.<br />

Keywords: product chemistry/bioassay<br />

Wong, D. H., Kirkpatrick, W. E., Kinnear, J. E., and King, D. R. (1991). Defluorination <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) by microorganisms found in bait materials. Wildlife research 18, 539-544.<br />

Keywords: bait degradation/defluorination/sodium mon<strong>of</strong>luoroacetate/1080<br />

Wong, D. H., Kirkpatrick, W. E., King, D. R., and Kinnear, J. E. (1992). Defluorination <strong>of</strong> sodium<br />

mon<strong>of</strong>luoroacetate (1080) by microorganisms isolated from Western Australian soils. Soil biology and<br />

biochemistry 24, 833-838.<br />

Keywords: persistence in soil/1080<br />

Abstract: Soils from four sites, two with and two without previous exposure to sodium mon<strong>of</strong>luoracetate<br />

(1080), in Western Australia were investigated to determine whether they contained microorganisms<br />

capable <strong>of</strong> defluorinating 1080. Most samples from these four sites showed microbial defluorination<br />

activity. A number <strong>of</strong> species <strong>of</strong> bacteria and fungi were isolated: Aspergillus fumigatus, Fusarium<br />

oxysporum, Pseudomonas acidovorans, Pseudomonas fluorescens 1, an unidentified Pseudomonas sp.,<br />

Penicillium purpurescens and Penicillium restrictum. These seven microorganisms could defluorinate 1080<br />

when grown in a 1080 solution, which was the sole carbon source, and also in autoclaved soil. The amount<br />

<strong>of</strong> defluorination varied with different species <strong>of</strong> microorganisms, ranging from 2 to 85% in soil and from 2<br />

to 89% in 1080 solutions. A time-course experiment showed that some indigenous soil micr<strong>of</strong>lora were<br />

able to defluorinate over 50% and up to 87% <strong>of</strong> the 1080 within 5-9 days in soil with a moisture content <strong>of</strong><br />

about 10% when kept at 28°C (day) and 15°C (night). Soils from four other arid or semiarid sites were also<br />

investigated for the presence <strong>of</strong> thermophilic microorganisms with 1080 defluorinating ability; no<br />

thermophilic microorganisms were isolated<br />

Wong, D. H., Kirkpatrick, W. E., King, D. R., and Kinnear, J. E. (1992). Environmental factors and<br />

microbial inoculum size, and their effect on biodefluorination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080). Soil<br />

biology and biochemistry 24, 839-843.<br />

Keywords: persistence in soil/1080<br />

Abstract: The effects <strong>of</strong> inoculum size and the environmental factors <strong>of</strong> pH, temperature and soil moisture<br />

on the biodefluorination <strong>of</strong> sodium mon<strong>of</strong>luoroacetate (1080) by seven microorganisms (four bacterial<br />

species and three fungi) were studied. In the presence <strong>of</strong> 1080 as the sole carbon source, the effect <strong>of</strong> pH on<br />

1080 defluorination varied among the organisms. Optimum 1080 defluorination by soil bacteria<br />

(Pseudomonas acidovorans and P. fluorescens 1) was at neutral to alkaline pH and the maximum<br />

defluorination by fungi (Fusarium oxysporum and Penicillium restrictum) was at pH 5. Most organisms<br />

grew on nutrient agar at a pH range <strong>of</strong> 5-8. The optimal temperature for 1080 defluorination varied with<br />

different microorganisms and with different organic carbon sources. On agar, all seven isolates grew best in<br />

the temperature range <strong>of</strong> 28-30°C. The highest rate <strong>of</strong> 1080 defluorinatiion in soil for all isolates occurred<br />

with fluctuating temperatures (minimum = 11°C, maximum = 24°C) and at soil moisture contents <strong>of</strong> 8-<br />

15%, while the lowest rates occurred at a soil moisture content <strong>of</strong> 30%. The defluorination rate <strong>of</strong> 1080<br />

when it was present at the sole carbon source decreased as the inoculum size decreased. In soil the rate <strong>of</strong><br />

reduction in 1080 defluorination was not directly proportional to the microbial inoculum size and the rate<br />

varied with different microorganisms. Some microorganisms had their highest rate <strong>of</strong> defluorination<br />

activity at a low inoculum density (105 cells/ml in 1080 solution and 107 cells/ml in soil)<br />

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Appendix C<br />

Wong, D. H., Kinnear, J. E., and Runham, C. F. (1995). A simple rapid bioassay for compound 1080<br />

(sodium fluoroacetate) in bait materials and soil - its technique and applications. Wildlife research 22, 561-<br />

568.<br />

Keywords: bioassay/bait degradation/1080/sodium fluoroacetate<br />

Woodfield, B. R. G. A Manual for the use <strong>of</strong> 1080 in Rabbit <strong>Control</strong>. 1976. Frankston, Victoria, The Keith<br />

Turnbull <strong>Research</strong> Institute.<br />

Ref Type: Pamphlet<br />

Keywords: 1080<br />

World Health Organisation. Sodium fluoroacetate. Data Sheets on Pesticides No. 16, VBC/DS/75.16, -11.<br />

1975.<br />

Ref Type: Report<br />

Keywords: sodium fluoroacetate/fluoroacetate<br />

Wright, G., Brown, L. E., and Eason, C. 1080 binding to cellulose: a pilot study. LC0102/022, -13. 2001.<br />

<strong>Landcare</strong> <strong>Research</strong> Lincoln. <strong>Landcare</strong> <strong>Research</strong> Contract Report.<br />

Ref Type: Report<br />

Keywords: 1080/persistence in plants/persistence in water/degradation<br />

Abstract: 1080 in the presence <strong>of</strong> aquatic weed reduced in concentration depending on the amount <strong>of</strong> weed<br />

present. There was no observed reduction <strong>of</strong> 1080 in the presence <strong>of</strong> shredded carrot. Neither cellulose nor<br />

glass fibre filter material showed any effect on 1080 concentration in water.<br />

Wright, G. R., Booth, L. H., Morriss, G. A., Potts, M. D., Brown, L., and Eason, C. T. (2002). Assessing<br />

potential environmental contamination from compound 1080 (sodium mon<strong>of</strong>luoroacetate) in bait dust<br />

during possum control operations. New Zealand journal <strong>of</strong> agricultural research 45, 57-65.<br />

Keywords: 1080/sodium mon<strong>of</strong>luoroacetate/mon<strong>of</strong>luoroacetate/poisoning/invertebrates/baits/soil/nontarget<br />

species/persistence in plants/persistence in soil<br />

Abstract: The risk <strong>of</strong> environmental contamination by 1080 from bait dust during possum control<br />

operations was assessed after three such operations. This research was prompted by the lack <strong>of</strong> data on the<br />

potential risk <strong>of</strong> poisoning invertebrates in leaf litter by 1080 from bait dust. Cereal baits containing 0.15%<br />

1080 were aerially applied and samples <strong>of</strong> bait dust (from application <strong>of</strong> bait), plants, leaf litter, soil, and<br />

water (from within and up to 1000 m outside the treatment areas) were collected prior to and up to 30 days<br />

after bait application. A maximum concentration <strong>of</strong> 25.2 µg 1080 m –2 was detected in bait dust (from dust<br />

collectors) within the control zone immediately after aerial application <strong>of</strong> 1080 baits. Lower concentrations<br />

<strong>of</strong> 1080 were found outside the treatment areas indicating relatively little drift <strong>of</strong> bait dust. There were<br />

detectable short-term 1080 residues in water, plant, leaf litter, and soil samples after two <strong>of</strong> the three baiting<br />

operations. However, the residues were very low indicating only minor contamination by 1080. Using the<br />

maximum concentration <strong>of</strong> 1080 found in leaf litter, and literature LD50 values for invertebrates, these<br />

results indicate that 1080 derived from bait fragments and bait dust does not pose a significant risk <strong>of</strong><br />

poisoning to resident leaf litter invertebrates. However, the presence <strong>of</strong> 1080 baits on the ground may still<br />

pose a risk to those invertebrates in close proximity to these baits.<br />

Wright, G. R. G. Trends in vertebrate pesticide contamination <strong>of</strong> wildlife. -68. 2000. University <strong>of</strong><br />

Waikato New Zealand. New Zealand Ecological Society Conference, 19-23 Nov 2000 Hamilton.<br />

Ref Type: Conference Proceeding<br />

Wright, G. R. G. Protocol for environmental water sampling and testing associated with 1080 pest control<br />

operations. 1-6. 2003.<br />

Ref Type: Pamphlet<br />

Keywords: 1080/livestock/poison/poisoning/rats/treatment/persistence in water<br />

Abstract: Water quality is to be monitored during 1080 poisoning operations to determine whether or not<br />

1080 is present at undesirable concentrations in the natural waters <strong>of</strong> the poison treatment area. This is <strong>of</strong><br />

particular concern where drinking water for domestic purposes or for livestock is drawn from catchments in<br />

or adjacent to these areas. As a result <strong>of</strong> recent research findings on the teratogenicity (effects on unborn<br />

<strong>of</strong>fspring) <strong>of</strong> 1080 in rats (Eason et al. unpublished contract report 1998), the Ministry <strong>of</strong> Health has issued<br />

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Appendix C<br />

guidelines recommending that water should not be used for drinking until tests show that the concentration<br />

<strong>of</strong> 1080 is below 2 parts per billion. This value was taken from the Ministry's approach to priority<br />

determinands in drinking water. The Drinking Water Standards for New Zealand require that, whenever a<br />

determinand is present at more than 50 percent <strong>of</strong> the maximum acceptable value (MAV), additional<br />

sampling is carried out until it has been established that its concentration does not exceed the MAV. The<br />

figure <strong>of</strong> 2ppb is an approximation to 50 percent <strong>of</strong> the provisional MAV <strong>of</strong> 5ppb.<br />

An intensive water-monitoring programme after a poisoning operation enables any water contamination<br />

to be detected and public concerns answered, provided due attention is given to site selection, timing, and<br />

the care and handling <strong>of</strong> samples.<br />

This sampling protocol has been prepared for Department <strong>of</strong> Conservation, regional council and district<br />

council pest control managers who need to undertake water monitoring, or Medical Officer <strong>of</strong> Health<br />

(MOH) who is involved in assessing the need for sampling. It provides information on water sampling,<br />

handling, transport, contact names, and the costs involved. Samples are received and analysed by the<br />

Toxicology Laboratory <strong>of</strong> <strong>Landcare</strong> <strong>Research</strong>, Lincoln. Advice on the establishment <strong>of</strong> a sampling strategy<br />

may be obtained from Environmental science and <strong>Research</strong> Ltd (ESR).<br />

Wright, G. R. G., Manning, L. M., and Fisher, P. M. Effects <strong>of</strong> aquatic plants on the concentration <strong>of</strong> 1080<br />

in water. <strong>Landcare</strong> <strong>Research</strong> Contract Report LC0203/177, -16. 2003.<br />

Ref Type: Report<br />

Keywords: 1080/metabolism/secondary poisoning/poisoning/humans/persistence in plants/persistence in<br />

water<br />

Abstract: The half-life <strong>of</strong> 1080 in solutions contaiing E.canadensis concentrations <strong>of</strong> 0.33 to 133 mg/mL<br />

ranged from 18.8 to 2.5 h respectively. The presence or absence <strong>of</strong> artificial light did not appear to affect<br />

the rate <strong>of</strong> elimination <strong>of</strong> 1080 from solutions containing plant material. E. canadensis absorbed 1080 from<br />

the solution to reach a maximum <strong>of</strong> 2.5 µg/kg after 2h. This concentration slowly decreased to below the<br />

method detection limit (2 µg/kg) after 24h.<br />

The elimination rate <strong>of</strong> 1080 from low-concentration solutions is influenced by the amount <strong>of</strong> living aquatic<br />

plant material present.The metabolism <strong>of</strong> 1080 by plant material is not affected by the presence or absence<br />

<strong>of</strong> artificial light. The rate <strong>of</strong> loss <strong>of</strong> 1080 from solution due to plant material is relatively slow below 15ºC,<br />

but becomes more rapid above 20ºC. There is a very low theoretical risk <strong>of</strong> acute secondary poisoning <strong>of</strong><br />

humans and animals consuming aquatic plants contaminated with 1080 through exposure to low<br />

concentrations in water.<br />

Wright, J. A. (1975). Altered aconitase activity in Hamster cells selected for resistance to fluoroacetate.<br />

Biochemical and biophysical research communications 66, 578-585.<br />

Keywords: aconitase/resistance/fluoroacetate/fluorocitrate/citrate/temperature<br />

Abstract: Two independent Chinese hamster ovary cell lines have been isolated in cell culture which<br />

exhibit resistance to the cytotoxic effects <strong>of</strong> fluorocitrate. Although the oxidation <strong>of</strong>citrate by wild type cell<br />

suspensions was markedly inhibited by 1 mM fluorocitrate drug-resistant cells oxidized citrate at<br />

approximately normal rates in the presence <strong>of</strong> the drug. The aconitase activity from the resistant cells was<br />

less sensitive to the inhibitory action <strong>of</strong> fluorocitrate in vitro and showed altered heat stability properties<br />

when tested in heat inactivation experiments at 3 different temperatures. These results are consistent with<br />

the view that the resistant cell lines contain a structural gene mutation.<br />

Wurster, D. E., Burke, G. M., Berg, M. J., Veng-Pedersen, P., and Schottelius.D.D. (1988). Phenobarbital<br />

adsorption from simulated intestinal fluid U.S.P., and simulated gastric fluid, U.S.P., by two activated<br />

charcoals. Pharmaceutical <strong>Research</strong> 5, 183-186.<br />

Keywords: antidote/poisoning/treatment<br />

Abstract: Adsorption <strong>of</strong> phenabarbital from simulated intestinal and gastric fluids by two activated<br />

charcoals was studied. Adsorption isotherm data were analyzed by the linearized Langmuir equation and by<br />

nonlinear least-squares regression employing both Langmuir and Freundlich models. These analyses<br />

indicated differences in the capacities <strong>of</strong> the two charcoals for phenobarbital which could not be completely<br />

explained by surface-area considerations.<br />

Wurster, D. E., Kolling, W. M., and Knosp, B. M. (1994). Computer modeling <strong>of</strong> adsorption on an<br />

activated charcoal surface. Journal <strong>of</strong> Pharmaceutical Sciences 83, 1717-1722.<br />

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1080 Reassessment Application October 2006<br />

Appendix C<br />

Keywords: antidote/poisoning/treatment<br />

Abstract: The molecular modeling program SYBYL was used to simulate the adsorption <strong>of</strong> various<br />

barbiturates by an activated charcoal surface. The compounds barbituric acid (BA), barbital (B),<br />

phenobarbital (PB), mephobarbital (M), and primidone (Pr) were modeled, and their structures were<br />

energetically minimized. These structures agreed with literature reports for the conformations <strong>of</strong> these<br />

molecules in dimethyl sulfoxide-d6, methanol-d4, and chlor<strong>of</strong>orm-d. The activated charcoal surface was<br />

modeled using graphitic crystallites which had either no oxygen-containing functional group, a C-OH<br />

functional group, or a C=O functional group. The presence <strong>of</strong> the C-O (presumably C-OH) and C=O<br />

functional states on activated charcoal surfaces had been previously determined by X-ray photoelectron<br />

spectroscopy. It was assumed that the crystallite was locally flat. Upon docking, conformational changes<br />

were observed for barbital, phenobarbital, mephobarbital, and primidone. Estimates for the heat <strong>of</strong><br />

adsorption ranged from -62.3 kJ/mol for barbituric acid to -91.1 kJ/mol for mephobarbital on the<br />

hydroxylated surface. Allowance for the heat <strong>of</strong> desorption <strong>of</strong> the required number <strong>of</strong> water molecules from<br />

the surface, also determined by SYBYL, gave heat <strong>of</strong> displacement values <strong>of</strong> -19.4 kJ/mol for barbituric<br />

acid and -32.6 kJ/mol for mephobarbital. These values compared well to the heat <strong>of</strong> displacement values<br />

obtained by isoperibol calorimetry, which were -20.3 kJ/mol for barbituric acid and -31.6 kJ/mol for<br />

mephobarbital. Previous laboratory studies had demonstrated the greater importance <strong>of</strong> the C-O functional<br />

state for barbiturate adsorption compared to the C=O functional state. The computer-modeled system<br />

predicted the same result.<br />

Yoshioka, K., Nisimaru, N., Yanai, S., Shimoda, H., and Yamada, K. (2000). Characteristics <strong>of</strong><br />

monocarboxylates as energy substrates other than glucose in rat brain slices and the effect <strong>of</strong> selective glial<br />

poisoning - a P-31 NMR study. Neuroscience research 36, 215-226.<br />

Keywords: mode <strong>of</strong> action/NMR/metabolism<br />

Zahavi, M., Tahori, A. S., and Mager, J. (1968). Studies on the biochemical basis <strong>of</strong> susceptibility and<br />

resistance <strong>of</strong> the housefly to fluoroacetate. Biochimica et biophysica acta 153, 787-798.<br />

Keywords: resistance/fluoroacetate/persistence in invertebrates/citrate/inhibition/fluorocitrate<br />

Abstract: 1) Administration <strong>of</strong> fluoroacetate to sensitive houseflies in amounts close to the LD50 range (0.25<br />

- 0.3 ug per fly) brought about a prompt elevation <strong>of</strong> the citrate content. With about 10-fold higher doses <strong>of</strong><br />

fluoroacetate a concurrent increase <strong>of</strong> both citrate and pyruvate levels took place in the fly tissues. 2)<br />

Incubation <strong>of</strong> sarcosomes <strong>of</strong> the sensitive housefly strain in the presence <strong>of</strong> oxidizable substrates and<br />

fluoroacetate resulted in accumulation <strong>of</strong> citrate , inhibition <strong>of</strong> respiration and uncoupling <strong>of</strong> oxidative<br />

phosphorylation. The magnitude <strong>of</strong> the effects varied considerably with the different substrates used, being<br />

particularly pronounced with pyruvate and malate and inappreciable with succinate and alphaglycerophosphate<br />

3) The respiratory inhibition induced by a brief exposure in teh cold <strong>of</strong> housefly<br />

sarcosomes to fluoroacetate, persisted after the sarcosomes had been washed free from fluoroacetate. The<br />

toxic effect <strong>of</strong> fluoroacetate on the respiratory chain could be prevented by an excess <strong>of</strong> simultaneously<br />

added acetate. 4)The susceptibility <strong>of</strong> the respiratory function <strong>of</strong> the sarcosomes to fluoroacetate inhibition<br />

was abolished by sonication. The unresponsiveness <strong>of</strong> the sonicated sarcosomes to fluoroacetate was<br />

attended by a loss <strong>of</strong> their respiratory chain phosphorylation activity 5) Sarcosomes derived from a partially<br />

resistant housefly strain, when incubated in the presence <strong>of</strong> fluoroacetate, failed to accumulate citrate, but<br />

displayed the characteristic respiratory-inhibition response. Sarcosome from a highly resistant strain<br />

showed no impairment fo their functional capacity by fluoroacetate. Howevre, all the different housefly<br />

strains tested proved to be equally sensitive to the deleterious effect <strong>of</strong> fluorocitrate in sarcosomal<br />

respiration. 6) The possible biochemical mechanisms underlying the toxicity <strong>of</strong> fluoroacetate in the<br />

housefly are considered with particular reference to the altered response <strong>of</strong> the target systems exhibited by<br />

the fluoroacetate-resistant strains.<br />

Zhou, J., Kaufmann, F. C., Ballow, C. H., and Thurman, R. G (1984). Inhibition <strong>of</strong> mixed-function<br />

oxidation in perfused rat liver by fluoroacetate treatment. Biochemical Pharmacology 33, 319-323.<br />

Keywords: inhibition/liver/fluoroacetate/treatment/citric acid/rats/sodium fluoroacetate/citrate/fluorocitrate<br />

Abstract: The effect <strong>of</strong> fluoroacetate, an inhibitor <strong>of</strong> the citric acid cycle, on the mixed-function oxidation<br />

<strong>of</strong> p-nitoranisole in isolated perfused livers from fed rats was studied. The citric acid cycle was inhibited by<br />

injection <strong>of</strong> 5 mg/kg sodium fluoroacetate into rats 3 hr prior to liver perfusion experiments. Inhibition <strong>of</strong><br />

the citric acid cycle was marked by accumulation <strong>of</strong> citrate (5-fold) and decreases in rates <strong>of</strong> glycolysis and<br />

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Appendix C<br />

glycogenolysis by 50-90%. Fluoroacetate treatment inhibited mixed function oxidation in the perfused liver<br />

by about 50% without affecting p-nitroanisole O-demethylation by isolated microsomes. Fluorocitrate at<br />

concentrations up to 50 uM did not inhibit microsomal p-nitroanisole O-demethylation in vitro. These data<br />

support the hypothesis that mixed-function oxidation in intact hepatocytes is dependent upon reducing<br />

equivalents generated via the citric acid cycle.<br />

226

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