WO1992022296A1 - Use of atipamezole for the treatment of male sexual impotence - Google Patents
Use of atipamezole for the treatment of male sexual impotence Download PDFInfo
- Publication number
- WO1992022296A1 WO1992022296A1 PCT/FI1992/000191 FI9200191W WO9222296A1 WO 1992022296 A1 WO1992022296 A1 WO 1992022296A1 FI 9200191 W FI9200191 W FI 9200191W WO 9222296 A1 WO9222296 A1 WO 9222296A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- atipamezole
- treatment
- male
- male sexual
- sexual impotence
- Prior art date
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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Definitions
- This invention relates to a novel therapeutic treatment of male sexual impotence by the administration of atipamezole which is the INN-approved generic name for 4-(2-ethyl-2,3-dihydro-1 H-inden-2-yl)-1 H-imidazole or a pharmaceutically acceptable acid addition salt thereof.
- Atipamezole is a selective and potent a2*-adrenoceptor antagonist which is currently marketed for the reversal of sedative-analgesic veterinary drugs.
- Atipamezole has been disclosed e.g. in the European Patent EP 183492 as useful for the reversal of detomidine.
- Yohimbine Another a2-adrenoreceptor antagonist, yohimbine, is currently used for the treatment of male impotence. Yohimbine increases noradrenergic neurotransmission and has been reported to facilitate the sexual capacity of male animals, although the results of different studies are conflicting.
- Atipamezole is, however clearly advantageous over yohimbine for this use because of its excellent selectivity.
- selectivity ratio of atipamezole is
- Atipamezole doses varied from 0.01 to 0.3 mg/kg (dissolved in saline to get a volume of about 0.2 ml). Each dose was tested 5-15 times in each monkey. Taking into account the saline days, the testing of one dose in one monkey took from 10 days to one month. The order of testing each dose was varied between 5 the monkeys to counterbalance possible serial effects.
- the difference in the number of ejaculations obtained at a given atipamezole dose and the corresponding saline control days was used as an index of the effect of atipamezole on sexual behaviour. This is how the possible variation in the baseline sexual activity (represented by ejaculations during saline days) could o be minimized.
- the incidence of ejaculations (the percentage of saline days with one or more ejaculations) during saline days was used as an index of baseline sexual activity of each male.
- ANOVA analysis of variance
- Student's t-test were used in statistical evaluation of the data. P ⁇ 0.05 was considered to represent a significant difference.
- Atipamezole increased the number of ejaculations in a dose-dependent way in all three male monkeys (for each individual; p ⁇ 0.05, ANOVA; Figure 1 A- 5 C).
- the lowest effective dose of atipamezole varied from 0.01 to 0.08 mg/kg depending on the individual; the younger the male, the lower the lowest effective dose.
- the average atipamezole-induced increase of ejaculations over the three males also was dose-dependent and significant (p ⁇ 0.05, ANOVA; Figure 1 D). No other behavioral effects produced by atipamezole were o observed except increased alertness.
- the drug is preferably administrated perorally, transmucosally, intravenously, intramuscularly or transdermally.
- the preferable daily dose range is about 0.01 to 1 mg/kg, preferably 0.05 to 0.3 mg/kg for i.v., i.m., tr ansmucosai or transdermal administration and 0.3 to 10 mg/kg for peroral administration.
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Orthopedics, Nursing, And Contraception (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Abstract
Description
Claims
Priority Applications (10)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1019930703555A KR100324447B1 (en) | 1991-06-18 | 1992-06-18 | Pharmaceutical composition for treating male sexual dysfunction containing atipamezole |
DE69214647T DE69214647T2 (en) | 1991-06-18 | 1992-06-18 | USE OF ATIPAMEZOL FOR TREATING MALE SEXUAL IMPOTENCE |
HU9303636A HU220068B (en) | 1991-06-18 | 1992-06-18 | Process for producing pharmaceutical preparations containing atipamezole for treatment impotence |
EP92911915A EP0589957B1 (en) | 1991-06-18 | 1992-06-18 | Use of atipamezole for the treatment of male sexual impotence |
CA002102187A CA2102187C (en) | 1991-06-18 | 1992-06-18 | Use of atipamezole for the treatment of male sexual impotence |
CS932487A CZ284409B6 (en) | 1991-06-18 | 1992-06-18 | Use of atipamezol or a pharmaceutically acceptable acid addition salt thereof for the preparation of a medicament |
AU19724/92A AU661698B2 (en) | 1991-06-18 | 1992-06-18 | Use of atipamezole for the treatment of male sexual impotence |
JP51106392A JP3151217B2 (en) | 1991-06-18 | 1992-06-18 | Uses of Atipamezole for the treatment of male or male impotence |
NO934690A NO304011B1 (en) | 1991-06-18 | 1993-12-17 | Use of atipamezole in the manufacture of a medicament for the treatment of men's impotence |
GR960403051T GR3021677T3 (en) | 1991-06-18 | 1996-11-15 | Use of atipamezole for the treatment of male sexual impotence |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB9113077.3 | 1991-06-18 | ||
GB919113077A GB9113077D0 (en) | 1991-06-18 | 1991-06-18 | Use of atipamezole |
Publications (1)
Publication Number | Publication Date |
---|---|
WO1992022296A1 true WO1992022296A1 (en) | 1992-12-23 |
Family
ID=10696833
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/FI1992/000191 WO1992022296A1 (en) | 1991-06-18 | 1992-06-18 | Use of atipamezole for the treatment of male sexual impotence |
Country Status (21)
Country | Link |
---|---|
EP (1) | EP0589957B1 (en) |
JP (1) | JP3151217B2 (en) |
KR (1) | KR100324447B1 (en) |
AT (1) | ATE144141T1 (en) |
AU (1) | AU661698B2 (en) |
CA (1) | CA2102187C (en) |
CZ (1) | CZ284409B6 (en) |
DE (1) | DE69214647T2 (en) |
DK (1) | DK0589957T3 (en) |
ES (1) | ES2092685T3 (en) |
GB (1) | GB9113077D0 (en) |
GR (1) | GR3021677T3 (en) |
HU (1) | HU220068B (en) |
IE (1) | IE921735A1 (en) |
IL (1) | IL101961A (en) |
MX (1) | MX9202948A (en) |
NO (1) | NO304011B1 (en) |
NZ (1) | NZ242863A (en) |
RU (1) | RU2111749C1 (en) |
WO (1) | WO1992022296A1 (en) |
ZA (1) | ZA923961B (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FI20002756A0 (en) * | 2000-12-15 | 2000-12-15 | Orion Yhtymae Oyj | New treatment procedure |
-
1991
- 1991-06-18 GB GB919113077A patent/GB9113077D0/en active Pending
-
1992
- 1992-05-21 IL IL10196192A patent/IL101961A/en not_active IP Right Cessation
- 1992-05-22 NZ NZ242863A patent/NZ242863A/en not_active IP Right Cessation
- 1992-05-29 ZA ZA923961A patent/ZA923961B/en unknown
- 1992-06-17 MX MX9202948A patent/MX9202948A/en not_active IP Right Cessation
- 1992-06-18 KR KR1019930703555A patent/KR100324447B1/en not_active IP Right Cessation
- 1992-06-18 WO PCT/FI1992/000191 patent/WO1992022296A1/en active IP Right Grant
- 1992-06-18 CA CA002102187A patent/CA2102187C/en not_active Expired - Fee Related
- 1992-06-18 ES ES92911915T patent/ES2092685T3/en not_active Expired - Lifetime
- 1992-06-18 RU RU93058537A patent/RU2111749C1/en not_active IP Right Cessation
- 1992-06-18 DE DE69214647T patent/DE69214647T2/en not_active Expired - Fee Related
- 1992-06-18 AU AU19724/92A patent/AU661698B2/en not_active Ceased
- 1992-06-18 CZ CS932487A patent/CZ284409B6/en not_active IP Right Cessation
- 1992-06-18 EP EP92911915A patent/EP0589957B1/en not_active Expired - Lifetime
- 1992-06-18 AT AT92911915T patent/ATE144141T1/en not_active IP Right Cessation
- 1992-06-18 JP JP51106392A patent/JP3151217B2/en not_active Expired - Fee Related
- 1992-06-18 DK DK92911915.4T patent/DK0589957T3/en active
- 1992-06-18 HU HU9303636A patent/HU220068B/en not_active IP Right Cessation
- 1992-07-01 IE IE173592A patent/IE921735A1/en not_active IP Right Cessation
-
1993
- 1993-12-17 NO NO934690A patent/NO304011B1/en not_active IP Right Cessation
-
1996
- 1996-11-15 GR GR960403051T patent/GR3021677T3/en unknown
Non-Patent Citations (3)
Title |
---|
Annals of Clinical Research, vol. 20, 1988; E. MacDONALD et al.: "Therapeutic applications of drugs acting on alpha-adrenoceptors", pages 298-310, see abstract; pages 300,302 * |
Drugs Future, vol. 15, no. 5, 1990, "Atipamezole", pages 448-452, see page 449 * |
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, vol. 42, 1992, Pergamon Press Ltd, (US), I. LINNANKOSKI et al.: "Increased sexual behavior in male Macaca arctoides monkeys produced by atipamezole, a selective alpha2-adrenoceptor antagonist", pages 197-200, see whole document * |
Also Published As
Publication number | Publication date |
---|---|
NO934690D0 (en) | 1993-12-17 |
DE69214647T2 (en) | 1997-02-20 |
GR3021677T3 (en) | 1997-02-28 |
CA2102187C (en) | 2003-03-11 |
AU1972492A (en) | 1993-01-12 |
CZ248793A3 (en) | 1994-04-13 |
KR100324447B1 (en) | 2002-06-20 |
HUT65817A (en) | 1994-07-28 |
AU661698B2 (en) | 1995-08-03 |
CZ284409B6 (en) | 1998-11-11 |
NO934690L (en) | 1993-12-17 |
JP3151217B2 (en) | 2001-04-03 |
RU2111749C1 (en) | 1998-05-27 |
ATE144141T1 (en) | 1996-11-15 |
DE69214647D1 (en) | 1996-11-21 |
IE921735A1 (en) | 1992-12-30 |
IL101961A0 (en) | 1992-12-30 |
MX9202948A (en) | 1993-04-01 |
NZ242863A (en) | 1997-06-24 |
GB9113077D0 (en) | 1991-08-07 |
EP0589957A1 (en) | 1994-04-06 |
ZA923961B (en) | 1993-02-24 |
JPH06508350A (en) | 1994-09-22 |
EP0589957B1 (en) | 1996-10-16 |
HU220068B (en) | 2001-10-28 |
NO304011B1 (en) | 1998-10-12 |
ES2092685T3 (en) | 1996-12-01 |
IL101961A (en) | 1995-12-31 |
DK0589957T3 (en) | 1996-11-18 |
CA2102187A1 (en) | 1992-12-19 |
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