GB2310600A - Pharmaceutical composition containing gestrinone and use thereof - Google Patents
Pharmaceutical composition containing gestrinone and use thereof Download PDFInfo
- Publication number
- GB2310600A GB2310600A GB9703862A GB9703862A GB2310600A GB 2310600 A GB2310600 A GB 2310600A GB 9703862 A GB9703862 A GB 9703862A GB 9703862 A GB9703862 A GB 9703862A GB 2310600 A GB2310600 A GB 2310600A
- Authority
- GB
- United Kingdom
- Prior art keywords
- gestrinone
- pharmaceutical composition
- emergency
- contraceptive
- conception
- 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.)
- Withdrawn
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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
- A61K31/568—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/569—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
-
- 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
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A pharmaceutical composition for use as an emergency contraceptive comprises a unit dosage form of gestrinone (13 B ethyl-17 B hydroxy - 18, 19-di-nor-17 pregna-4,9, 11-trien-20-yn-3-one) of between 5 and 10 mg, and at least one physiologically acceptable carrier or adjuvant. Gestrinone is also used in the manufacture of a medicament to be used as an emergency contraceptive, and for preventing conception in a female by administration thereof to a female following unprotected intercourse.
Description
PHARMACEUTICAL COMPOSITION CONTAINING GESTRINONE
AND USE THEREOF
This invention relates to a new use of the known medicinal compound gestrinone (13 B ethyl-17 B hydroxy -18, 19-di-nor-17 pregnant,9, 11 -trien-20-yn-3-one) and to pharmaceutical compositions containing it.
Emergency contraception is required in today's society as an alternative to traditional contraception for women who do not use other methods of contraception and who are occasionally exposed to the fear of unwanted pregnancy. Emergency contraception is also required by those women whose chosen method of contraception fails during coitus, for example owing to breakage of a contraceptive sheath.
Known methods of emergency contraception are mechanical or medicinal. Mechanical methods include intra-uterine devices (IUD) which can be inserted up to 7 days following intercourse to prevent pregnancy. Medicinal methods of emergency contraception have been in use for many years. The most widely used and promoted method is the so called Yuzpe regimen which consists of the administration of a combination of 100 micrograms of ethinyl estradiol and 250 micrograms of levonorgestrel. A low-dose combination pill of ethinyl estradiol and levonorgestrel is marketed as a regular oral contraceptive, but may be used as an emergency contraceptive in the required effective doses of the Yuzpe regimen. For use as an emergency contraceptive, a number of the lower dose pills must be ingested within the 12 hours interval required for the treatment, which must be commenced no later than 72 hours following unprotected intercourse.
The doctor should be sure that the woman for whom emergency contraception is prescribed is not pregnant from another occurrence of unprotected intercourse occurring prior to the 72 hour time limit. Side-effects of the Yuzpe regimen include nausea and vomiting, which may affect 20% of users, headaches, abdominal cramps and dizziness.
The second most widely recommended emergency contraceptive is levonorgestrel, a synthetic progestine, given in two doses of 0.75mg each, 12 hours apart with the initial dose being taken within 48 hours of unprotected intercourse. This levonorgestrel regimen is presently marketed in some countries in Eastern Europe. In common with the combination pill of the Yuzpe regimen, levonorgestrel is also marketed as a regular oral contraceptive. It may therefore be used as an emergency contraceptive by administration of two doses of ten pills each of the available oral contraceptive containing 0.075mg of levonorgestrel.
Other compounds being tested as emergency contraceptives include high-dose estrogens, mifepristone, which is an anti-progesterone used as an abortifacient in Europe, and Danazol which is an anti-gonadotropin.
Danazol is administered in two doses of 400mg each taken 12 hours apart.
High-dose estrogens cause intolerable nausea and vomiting and the effectiveness of Danazol, even at the high doses recommended, remains to be shown. Also, it is generally undesirable to require patients to take a number of pills spaced over a period of time, since the regimen can be overlooked or otherwise not followed.
Accordingly, there is a recognised need in the art for a method of emergency contraception with reduced side-effects, which is effective in preventing unwanted pregnancy following unprotected intercourse, and which can be administered in a single effective dose.
I have now found that emergency contraception can be provided by administration of gestrinone.
According to one aspect of the present invention, there is provided the use of gestrinone in the manufacture of a medicament to be used as an emergency contraceptive.
The invention further includes the use of gestrinone to prevent conception after unprotected intercourse.
Gestrinone (13 B ethyl-17 B hydroxy - 18, 19-di-nor-17 pregna4,9, 1 1-trien-20-yn-3-one) is a trienic steroid with combined anti-estrogen and antiprogesterone properties which is used in the treatment of endometriosis, and is marketed for this medical condition in over 20 countries. It has been proposed for the treatment of fibro-cystic disease of the breast and uterine fibromas which appear to shrink under the anti-progesterone/anti-estrogen effects of the drug, but not for use as an emergency contraceptive. Additionally, gestrinone acts to inhibit gonadotropin production. Once absorbed it is metabolised by the liver relatively slowly and is therefore long-acting. For these reasons, treatment with gestrinone does not require daily administration.
I have found that gestrinone, administered as an emergency contraceptive in doses preferably of between about 5 and about 10mg within 72 hours of unprotected intercourse, is effective in preventing conception.
According to a further aspect of the present invention, there is provided a pharmaceutical composition to be used as an emergency contraceptive, comprising a unit dosage form of gestrinone and at least one physiologically acceptable carrier or adjuvant, wherein the unit dosage form contains from 5 mg to 10 mg of gestrinone.
The gestrinone for use as an emergency contraceptive is administered either orally or vaginally in tablet form. Tablets of gestrinone will contain the usual excipients such as, for example, lactose, starch, polyvinylpyrrolidone and magnesium estearate etc. as will be clear to those skilled in the art.
I prefer the administration of a single physiologically effective dose, in order to overcome the difficulties that a patient may not comply with a regime requiring e.g. more than one tablet of a lower dose to be taken. However, if desired, the gestrinone can be administered in two or more dosage units, as will be clear to those skilled in the art.
In a further aspect, the invention includes a method of preventing conception, which method comprises administering a pharmaceutical composition according to the invention to a female following unprotected intercourse, but before conception has occurred. Whilst this method may be practised privately, it may also be offered commercially in clinics and hospitals for example.
In order that the present invention may be more fully understood the following Example is provided, by way of illustration only.
Example
Sixty-nine female patients complaining of the risk of an unwanted pregnancy were each administered a single unit dose of 10 mg of gestrinone within seventy-two hours of unprotected sexual intercourse. Of the sixty-five female patients who reported back to the clinic, only one of them went on to become pregnant.
Claims (7)
1. A pharmaceutical composition to be used as an emergency contraceptive, comprising a unit dosage form of gestrinone and at least one physiologically acceptable carrier or adjuvant, wherein the unit dosage form contains from 5 mg to 10 mg of gestrinone.
2. A composition according to claim 1 which is in tablet form.
3. The use of gestrinone in the manufacture of a medicament to be used as an emergency contraceptive.
4. The use of gestrinone to prevent conception after unprotected intercourse.
5. A method of preventing conception which method comprises administering a pharmaceutical composition according to claim 1 or 2, to a female following unprotected intercourse, but before conception has occurred.
6. A method according to claim 6, wherein the pharmaceutical composition is administered within 72 hours of unprotected intercourse.
7. A method according to claim 6 or 7, wherein the pharmaceutical composition is administered orally or vaginally.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9703862A GB2310600A (en) | 1996-03-01 | 1997-02-25 | Pharmaceutical composition containing gestrinone and use thereof |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9604426.8A GB9604426D0 (en) | 1996-03-01 | 1996-03-01 | Pharmaceutical composition and use thereof |
| GB9703862A GB2310600A (en) | 1996-03-01 | 1997-02-25 | Pharmaceutical composition containing gestrinone and use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB9703862D0 GB9703862D0 (en) | 1997-04-16 |
| GB2310600A true GB2310600A (en) | 1997-09-03 |
Family
ID=26308840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB9703862A Withdrawn GB2310600A (en) | 1996-03-01 | 1997-02-25 | Pharmaceutical composition containing gestrinone and use thereof |
Country Status (1)
| Country | Link |
|---|---|
| GB (1) | GB2310600A (en) |
-
1997
- 1997-02-25 GB GB9703862A patent/GB2310600A/en not_active Withdrawn
Non-Patent Citations (5)
| Title |
|---|
| Contracept. Fertil.Sex. (France), 1985, 13/1 Suppl., 359-364Serfaty, D. * |
| Fertil. Steril. (United States), 1983, 39(3), p.267-9 Adashi, E. Y. * |
| Fertil. Steril. , 1978, 30(3), p.289-92, Spellacy, W.N.et al * |
| Fertil. Steril. , 1981, 35(3), p.284-8, Mahmood, A.N. et al * |
| Martindale, The Extra Pharmacopoeia, 29th Edition, 1989, seeGestrinone * |
Also Published As
| Publication number | Publication date |
|---|---|
| GB9703862D0 (en) | 1997-04-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| WAP | Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1) |