CA1320132C - Dehydroepiandrosterone therapy - Google Patents
Dehydroepiandrosterone therapyInfo
- Publication number
- CA1320132C CA1320132C CA000565605A CA565605A CA1320132C CA 1320132 C CA1320132 C CA 1320132C CA 000565605 A CA000565605 A CA 000565605A CA 565605 A CA565605 A CA 565605A CA 1320132 C CA1320132 C CA 1320132C
- Authority
- CA
- Canada
- Prior art keywords
- symptoms
- dhea
- composition
- testosterone
- dehydroepiandrosterone
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
Abstract
ABSTRACT
Dehydroepiandrosterone and acceptable salts thereof are utilized for sexual disfunction therapy.
Dehydroepiandrosterone and acceptable salts thereof are utilized for sexual disfunction therapy.
Description
~ 1 132~3~
This invention relates to the administration of dehydroepiandrosterone (DHEA) and its therapeutically acceptable salts, including the sulfate (DHEA-S) to ameliorate the symptoms of prostatic hypertrophy, certain symptoms of menopause, particularly those related to nervous system dysfunction, and of psychosexual dysfunction symptoms such as inhibited sexual desire, inhibited sexual excitement and inhibited orgasm. These benefits may result from modification by DHEA or DHEA-S
of the testosterone-estrogen ratio in human subjects.
In accordance of with an a~pect of the present invention, the process which comprises administering an effective amount of dehydroepiandrosterone or a therapeutically acceptable salt thereof to modify the testosterone to estrogen ratio in a human.
In accordance with a further aspect of the present invention, a process for ameliorating symptoms selected from the group consisting of prostate hypertrophy symptoms, sexual dysfunction symptoms and menopausal s~mptomæ related to nervous system dysfunction which consists of administering an effective amount of dehydroepiandrosterone or a therapeutically effective salt thereof to a human manifesting such symptoms.
In accordance with another aspect of the present invention, a composition useful in modifying the testosterone to estrogen ratio in a human comprises a therapeutically effective amount of an active compound selected from the group consisting of dehydro-epiandrosterone and therapeutically acceptable excipients.
The enlargement of the prostate that takes place in later years in adult males is generally coincident with decreases with age in the levels of DHEA and DHEA-S in the blood. Normal prostatic function appears to depend on the capability of testicular and prostatic tissue to provids an appropriate ratio of testosterone to estrogens. DHEA and ~HEA-S are percursors of androgens, including testosterone which, in turn, are precursors for estrogens. See generally, Roberts, E., Treatment A
This invention relates to the administration of dehydroepiandrosterone (DHEA) and its therapeutically acceptable salts, including the sulfate (DHEA-S) to ameliorate the symptoms of prostatic hypertrophy, certain symptoms of menopause, particularly those related to nervous system dysfunction, and of psychosexual dysfunction symptoms such as inhibited sexual desire, inhibited sexual excitement and inhibited orgasm. These benefits may result from modification by DHEA or DHEA-S
of the testosterone-estrogen ratio in human subjects.
In accordance of with an a~pect of the present invention, the process which comprises administering an effective amount of dehydroepiandrosterone or a therapeutically acceptable salt thereof to modify the testosterone to estrogen ratio in a human.
In accordance with a further aspect of the present invention, a process for ameliorating symptoms selected from the group consisting of prostate hypertrophy symptoms, sexual dysfunction symptoms and menopausal s~mptomæ related to nervous system dysfunction which consists of administering an effective amount of dehydroepiandrosterone or a therapeutically effective salt thereof to a human manifesting such symptoms.
In accordance with another aspect of the present invention, a composition useful in modifying the testosterone to estrogen ratio in a human comprises a therapeutically effective amount of an active compound selected from the group consisting of dehydro-epiandrosterone and therapeutically acceptable excipients.
The enlargement of the prostate that takes place in later years in adult males is generally coincident with decreases with age in the levels of DHEA and DHEA-S in the blood. Normal prostatic function appears to depend on the capability of testicular and prostatic tissue to provids an appropriate ratio of testosterone to estrogens. DHEA and ~HEA-S are percursors of androgens, including testosterone which, in turn, are precursors for estrogens. See generally, Roberts, E., Treatment A
2 1~0132 Development Strate~ies for_Alzheimer's Disease, Mark Pauley Associatesl Inc., pp. 188, et seq (1986).
As a result of the decrease with age of DHEA and DHEA-S serum levels, the capability of pxostatic and testicular tissues to make testosterone is impaired.
While acceptable levels of the male hormone may be maintained, the subsequent synthesis of estrogen from testosterone is decreased. I'he result is the presence of testosterone without the counterbalancing effects of appropriate amounts of estrogen.
It is a postulate of this invention that the abnormality observed in prostatic hypertrophy is consequent from this imbalance in testosterone estrogen ratio. Pursuant to one aspect of the invention, DHEA or a therapeutically acceptable salt thereof is administered to human males with decreased serum levels of DHEA or DHEA-S to preclude the occurrence of prostatic hypertrophy or prevent it from progressing once it has begun.
~0 A number of menopausal symptoms, particularly those related to nervous system dysfunction, also may be attributable to an imbalance in the appropriate testosterone to estrogen ratio. It is known that DHEA
and DHEA-S decrease in the blood at the same time that estrogens decrease in menopause. Pursuant to this invention, DHEA or a therapeutically acceptable salt thereof is administered to human females to correct the hormone imbalan~e, and thus ameliorate the emotional and neural problems of menopause.
~ Human sexual dysfunction refers to sexual drive (libido), sexual excitement and orgasm. Common organic causes of sexual dysfunction include disruption of genital sensory or motor nerves, hormonal imbalances, vascular disease, drug side effects and diabetes.
Psychosexual dysfunctions have no apparent organic basis.
Treatment is primarily a matter of behaviour modification and counsalling.
.
~ .
As a result of the decrease with age of DHEA and DHEA-S serum levels, the capability of pxostatic and testicular tissues to make testosterone is impaired.
While acceptable levels of the male hormone may be maintained, the subsequent synthesis of estrogen from testosterone is decreased. I'he result is the presence of testosterone without the counterbalancing effects of appropriate amounts of estrogen.
It is a postulate of this invention that the abnormality observed in prostatic hypertrophy is consequent from this imbalance in testosterone estrogen ratio. Pursuant to one aspect of the invention, DHEA or a therapeutically acceptable salt thereof is administered to human males with decreased serum levels of DHEA or DHEA-S to preclude the occurrence of prostatic hypertrophy or prevent it from progressing once it has begun.
~0 A number of menopausal symptoms, particularly those related to nervous system dysfunction, also may be attributable to an imbalance in the appropriate testosterone to estrogen ratio. It is known that DHEA
and DHEA-S decrease in the blood at the same time that estrogens decrease in menopause. Pursuant to this invention, DHEA or a therapeutically acceptable salt thereof is administered to human females to correct the hormone imbalan~e, and thus ameliorate the emotional and neural problems of menopause.
~ Human sexual dysfunction refers to sexual drive (libido), sexual excitement and orgasm. Common organic causes of sexual dysfunction include disruption of genital sensory or motor nerves, hormonal imbalances, vascular disease, drug side effects and diabetes.
Psychosexual dysfunctions have no apparent organic basis.
Treatment is primarily a matter of behaviour modification and counsalling.
.
~ .
3 13 ~0132 The sole presently known prior art pertaining specifically to the pharmacologic treatment of psychological aspects of sexual dysfunction is a report of the administration of bupropion hydrochloride in a controlled Glinical trial involving some sixty (60) test subjects which resulted in increased sexual desire and heightened libido. See Time, May 4, 1987, p. 6. (The drug Wellbutrin referenced in the Time article is understood to be bupropion hydrochloride.) Administration of bupropion is reported to result in an increase in serum DHEA-S.
It is a further postulate of the invention that the administration of DHEA or a therapeutically acceptable salt thereof ameliorates sexual dysfunction by modification of neurochemical, specifically androgen (testosterone), estrogen balance or by correction of neurochemical imbalance in human subjects. Specifically, another aspect of this invention entails the administration of DHEA or a therapeutically acceptable salt thereof, e.g., DHEA-S to enhance sexual desire and performance and to ameliorate sexual dysfunction in human male and female subjeats.
For all purposes of this invention, dosage of DHEA
or a salt thereof to establish and maintain appropriate serum levels is within the skill of the art. For example, 90 to 300 mg per day administered in three 30 to 100 mg aliquots is appropriate. A 350 to 400 mg serum level is preferably established and maintained by periodic, e.g., daily, administration, for such time as may be indicated by patient response to the therapy.
Administration may be accomplished in any desired manner, e.g., orally, transdermally, by time lapse capsule, or intranasally.
DHEA or an acceptable salt thereof can be formulated into capsules, tablets, elixirsj or the like together with suitable excipients in a manner conventional in the art.
., .~, ~, ,, .
.
It is a further postulate of the invention that the administration of DHEA or a therapeutically acceptable salt thereof ameliorates sexual dysfunction by modification of neurochemical, specifically androgen (testosterone), estrogen balance or by correction of neurochemical imbalance in human subjects. Specifically, another aspect of this invention entails the administration of DHEA or a therapeutically acceptable salt thereof, e.g., DHEA-S to enhance sexual desire and performance and to ameliorate sexual dysfunction in human male and female subjeats.
For all purposes of this invention, dosage of DHEA
or a salt thereof to establish and maintain appropriate serum levels is within the skill of the art. For example, 90 to 300 mg per day administered in three 30 to 100 mg aliquots is appropriate. A 350 to 400 mg serum level is preferably established and maintained by periodic, e.g., daily, administration, for such time as may be indicated by patient response to the therapy.
Administration may be accomplished in any desired manner, e.g., orally, transdermally, by time lapse capsule, or intranasally.
DHEA or an acceptable salt thereof can be formulated into capsules, tablets, elixirsj or the like together with suitable excipients in a manner conventional in the art.
., .~, ~, ,, .
.
Claims (6)
1. A composition useful in modifying the testosterone to estrogen ratio in a human comprises a therapeutically effective amount of an active compound selected from the group consisting of dehydro-epiandrosterone and therapeutically acceptable excipients.
2. A composition of claim 1 wherein said selected active compound is dehydroepiandrosterone.
3. A composition of claim 1 wherein said selected active compound is dehydroepiandrosterone sulfate.
4. The use of a composition of claim 1 in modifying the testosterone to estrogen ration in a human.
5. The use of a composition of claim 1 in ameliorating symptoms selected from the group consisting of prostate hypertrophy symptoms, sexual dysfunction symptoms and menopausal symptoms.
6. The use of claim 5 wherein said sexual dysfunction symptoms are selected from the group consisting of inhibited sexual excitement, inhibited libido and inhibited orgasms.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US046,579 | 1987-05-06 | ||
| US07/046,579 US4835147A (en) | 1987-05-06 | 1987-05-06 | Dehydroepiandrosterone therapy for ameleoration of prostate hypertrophy and sexual dysfunction |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1320132C true CA1320132C (en) | 1993-07-13 |
Family
ID=21944198
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000565605A Expired - Fee Related CA1320132C (en) | 1987-05-06 | 1988-04-29 | Dehydroepiandrosterone therapy |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US4835147A (en) |
| AU (1) | AU1563288A (en) |
| CA (1) | CA1320132C (en) |
| GB (1) | GB2204490B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009021323A1 (en) * | 2007-08-10 | 2009-02-19 | Endorecherche, Inc. | Dhea compositions for treating menopause |
| US8835413B2 (en) | 2004-10-20 | 2014-09-16 | Endorecherche, Inc. | Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5925774A (en) * | 1991-01-07 | 1999-07-20 | Pherin Corporation | Estrenes for inducing hypothalamic effects |
| US5969168A (en) * | 1991-01-07 | 1999-10-19 | Pherin Corporation | Androstanes for inducing hypothalamic effects |
| US5883087A (en) * | 1991-01-07 | 1999-03-16 | Pherin Corporation | Androstane steroids as neurochemical initiators of change in human hypothalamic function and related pharmaceutical compositions and methods |
| AU686120B2 (en) * | 1993-01-19 | 1998-02-05 | Endorecherche Inc. | Therapeutic methods & delivery systems utilizing sex steroid precursors and novel steroidal derivatives and pharmaceutical compositions thereof |
| US5776923A (en) * | 1993-01-19 | 1998-07-07 | Endorecherche, Inc. | Method of treating or preventing osteoporosis by adminstering dehydropiandrosterone |
| US5407927A (en) * | 1993-04-16 | 1995-04-18 | The Regents Of The University Of California | Treatment of mild depression and restoration of IGF-I levels in aging by dehydroepiandrosterone |
| US5609617A (en) * | 1995-02-21 | 1997-03-11 | C. Norman Shealy | Method for enhancement of dehydroepiandrosterone |
| DE19610645A1 (en) * | 1996-03-06 | 1997-09-11 | Schering Ag | Combination of dehydroepiandrosterone and aromatase inhibitors and use of this combination for the manufacture of a medicament for the treatment of a relative and absolute androgen deficiency in men |
| US5753696A (en) * | 1996-12-12 | 1998-05-19 | Cluster Technology Corp. | Compositions and methods for enhancement of dehydroepiandrosterone |
| US6025368A (en) * | 1997-02-25 | 2000-02-15 | Celtrix Pharmaceuticals, Inc. | Method for treating the symptoms of chronic stress-related disorders using IGF |
| US6015786A (en) | 1997-02-25 | 2000-01-18 | Celtrix Pharmaceuticals, Inc. | Method for increasing sex steroid levels using IGF or IGF/IGFBP-3 |
| US6514937B1 (en) | 1997-02-25 | 2003-02-04 | Celtrix Pharmaceuticals, Inc. | Method of treating psychological and metabolic disorders using IGF or IGF/IGFBP-3 |
| US5912240A (en) | 1997-04-10 | 1999-06-15 | Loria; Roger M. | 5-androstene 3β, 17α diol as an inhibitor of tumor growth |
| US7098206B2 (en) * | 1998-01-21 | 2006-08-29 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6998400B2 (en) * | 1998-01-22 | 2006-02-14 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| AU2483599A (en) * | 1998-01-29 | 1999-08-16 | Sepracor, Inc. | Pharmaceutical uses of optically pure (-)-bupropion |
| AU2349999A (en) | 1998-01-29 | 1999-08-16 | Sepracor, Inc. | Pharmacological uses of pure (+) -bupropion |
| US6734213B2 (en) | 1999-01-20 | 2004-05-11 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6855820B2 (en) | 1999-01-20 | 2005-02-15 | Smithkline Beecham Corporation | Pharmaceutically active morpholinol |
| US6337328B1 (en) | 1999-03-01 | 2002-01-08 | Sepracor, Inc. | Bupropion metabolites and methods of use |
| US6342496B1 (en) | 1999-03-01 | 2002-01-29 | Sepracor Inc. | Bupropion metabolites and methods of use |
| US6548087B1 (en) * | 1999-07-12 | 2003-04-15 | Frances B. Kent | Nutritional supplement |
| US20040137081A1 (en) * | 2003-01-13 | 2004-07-15 | Peter Rohdewald | Attaining sexual wellness and health of the sexual vascular system with proanthocyanidins |
| CA2431566A1 (en) * | 2000-12-11 | 2002-07-18 | Testocreme, Llc | Topical testosterone formulations and associated methods |
| US20050181057A1 (en) * | 2004-02-13 | 2005-08-18 | Rosenberg Paul K. | Vaginal lubricant |
| US20060276442A1 (en) * | 2004-09-08 | 2006-12-07 | Woodward John R | Methods of female sexual enhancement |
| US9446049B2 (en) * | 2006-03-09 | 2016-09-20 | Jonathan V. Wright | Hormone replacement formulation |
| US8124598B2 (en) * | 2006-09-14 | 2012-02-28 | Sharon Sageman | 7-keto DHEA for psychiatric use |
| AU2012204083C1 (en) * | 2007-08-10 | 2015-02-05 | Myriel Pharmaceuticals, Llc | DHEA compositions for treating menopause |
| US20100160274A1 (en) * | 2007-09-07 | 2010-06-24 | Sharon Sageman | 7-KETO DHEA for Psychiatric Use |
| US20090092687A1 (en) * | 2007-10-03 | 2009-04-09 | Stein Daniel S | Prhormone composition and method of use thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK122125B (en) * | 1967-10-04 | 1972-01-24 | Schering Ag | Analogous process for the preparation of therapeutically active carboxylic acid esters of 3β-hydroxy-5-androstan-17-one (dehydroepiandrosterone) having 7-11 carbon atoms in the ester residue. |
| US4005200A (en) * | 1975-07-17 | 1977-01-25 | Kanebo, Ltd. | Method for improving the maturity of the parturient canal and the sensitivity to oxytocin |
| JPS58101691A (en) * | 1981-11-10 | 1983-06-16 | Kirin Brewery Co Ltd | Preparation of cellulase |
| US4496556A (en) * | 1982-08-16 | 1985-01-29 | Norman Orentreich | Topical applications for preventing dry skin |
| US4542129A (en) * | 1982-08-16 | 1985-09-17 | Norman Orentreich | DHEA Formulations and methods for treating dry skin |
| US4518595A (en) * | 1983-07-19 | 1985-05-21 | The Jackson Laboratory | Method for treating diabetes using DHEA compounds |
-
1987
- 1987-05-06 US US07/046,579 patent/US4835147A/en not_active Expired - Lifetime
-
1988
- 1988-04-29 CA CA000565605A patent/CA1320132C/en not_active Expired - Fee Related
- 1988-05-05 AU AU15632/88A patent/AU1563288A/en not_active Abandoned
- 1988-05-06 GB GB8810834A patent/GB2204490B/en not_active Expired - Fee Related
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8835413B2 (en) | 2004-10-20 | 2014-09-16 | Endorecherche, Inc. | Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women |
| US10076525B2 (en) | 2004-10-20 | 2018-09-18 | Endorecherche, Inc. | Sex steroid precursors alone or in combination with selective estrogen receptor modulators for the prevention and treatment of dyspareunia in postmenopausal women |
| US10478443B2 (en) | 2004-10-20 | 2019-11-19 | Endorecherche, Inc. | Sex steroid precursors alone or in combination with selective estrogen receptor modulators for the prevention and treatment of sexual dysfunction in postmenopausal women |
| WO2009021323A1 (en) * | 2007-08-10 | 2009-02-19 | Endorecherche, Inc. | Dhea compositions for treating menopause |
| US8268806B2 (en) | 2007-08-10 | 2012-09-18 | Endorecherche, Inc. | Pharmaceutical compositions |
| US8629129B2 (en) | 2007-08-10 | 2014-01-14 | Endorecherche, Inc. | Pharmaceutical compositions |
| EA020683B1 (en) * | 2007-08-10 | 2015-01-30 | Эндорешерш, Инк. | Method for treating or reducing acquiring symptoms or diseases in postmenopausal women, intravaginal composition and suppository used therein |
| US8957054B2 (en) | 2007-08-10 | 2015-02-17 | Endorecherche, Inc. | Pharmaceutical compositions |
| US10881650B2 (en) | 2007-08-10 | 2021-01-05 | Endorecherche, Inc. | Pharmaceutical compositions |
Also Published As
| Publication number | Publication date |
|---|---|
| AU1563288A (en) | 1988-11-10 |
| GB2204490B (en) | 1991-03-27 |
| US4835147A (en) | 1989-05-30 |
| GB2204490A (en) | 1988-11-16 |
| GB8810834D0 (en) | 1988-06-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKLA | Lapsed |