WO2000003678A2 - Subcutaneous medroxyprogesterone acetate for contraception - Google Patents
Subcutaneous medroxyprogesterone acetate for contraception Download PDFInfo
- Publication number
- WO2000003678A2 WO2000003678A2 PCT/US1999/014129 US9914129W WO0003678A2 WO 2000003678 A2 WO2000003678 A2 WO 2000003678A2 US 9914129 W US9914129 W US 9914129W WO 0003678 A2 WO0003678 A2 WO 0003678A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- female
- medroxyprogesterone acetate
- progestogen
- effective amount
- contraceptively effective
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- 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
- A61P15/18—Feminine contraceptives
Definitions
- the present invention is a subcutaneous method for adrninistering medroxyprogesterone acetate for female contraceptive use.
- Contraception, 56, 353-359 also discloses a clinical study of medroxyprogesterone acetate (25 mg) and estradiol cypionate (5 mg) by monthly IM injection for female contraception.
- IM and IM injections should be administered not by the patient but by an appropriately trained health care professional.
- the method of the present invention does not rely on IM adrninistration but rather subcutaneous adrninistration which can be done by the patient.
- SUMMARY OF INVENTION Disclosed is a method of human female contraception which comprises subcutaneous administration of a contraceptively effective amount of a contraceptive agent selected from the group consisting of a progestogen and a progestogen plus an estrogen.
- DETAILED DESCRIPTION OF THE INVENTION The present invention is a method of human female contraception which comprises subcutaneous adnvinistration of a contraceptively effective amount of a contraceptive agent selected from the group consisting of a progestogen and a progestogen plus an estrogen.
- the method of the present invention can be practiced by the female patient self administering the subcutaneous injection herself.
- the patient should be taught by a trained health care professional how to administer the subcutaneous injection of progestogen or progestogen plus estrogen.
- the patient then injects subcutaneously a contraceptively effective amount as she was directed either approximately once a month or approximately every three months or approximately every six months.
- the word "approximately” is used because some months have 30 days while others have 31 days.
- the method of the present invention can be practiced by the administration of a combination of a progestogen plus an estrogen once a month.
- this method is utilized the female will have a menstrual period every month. At the end of each month time period, normal fertility returns unless the patient uses another injection or some other form of fertility control.
- US Patent 4,038,389 discloses a 200-600 mg/ml parenteral formulation of medroxyprogesterone acetate.
- the parenteral formulation can be administered once every month or every 13 weeks (3 months) or every 26 weeks (6 months). Following the contraceptive period, the female has a menstrual period unless she has another IM injection prior to her period.
- the female may have a series of IM injections of medroxyprogesterone acetate to provide contraception on a continuous basis.
- the /. Reprod. Fertil., 15, 209-14 (1968) discloses a formulation of medroxyprogesterone acetate (25 mg) and estradiol cypionate (5 mg) which was used in a clinical study by monthly IM injection for female contraception. See also
- the progestogen be selected from the group consisting of medroxyprogesterone acetate, progesterone, norethindrone, desogestrel and levo- norgestrelit is more preferred that the progestogen be medroxyprogesterone acetate.
- the estrogen be selected from the group consisting of ethinyl estradiol, estradiol cypionate and estradiol valerate; it is more preferred that the estrogen be estradiol cypionate.
- the contraceptive agent be medroxyprogesterone acetate or medroxyprogesterone acetate plus estradiol cypionate.
- the contraceptive method of the present invention is practiced by using a progestogen alone, it is preferred that the progestogen be in a depot form as is well known to those skilled in the art. It is preferred that the contraceptively effective amount for one month be for medroxyprogesterone acetate from about 10 mg to about 50 mg/female, for progesterone from about 25 mg to about 200 mg/female, for northindrone from about 5 mg to about 50 mg/female, for desogestrel from about 1 mg to about 4 mg/female, for levo-norgrestrel from about 0.5 mg to about 2 mg/female; for three months be for medroxyprogesterone acetate from about 100 mg to about 200 mg/female, for progesterone from about 25 mg to about 200 mg/female, for northindrone from about 5 mg to about 50 mg/female, for desogestrel from about 1 mg to about 4 mg/female, for levo-n
- the dose for one, three and six monthes be from about 20 mg to about 30 mg/female, from about 125 mg to about 175 mg/female and from about 250 mg to about 300 mg/female.
- the contraceptive method of the present invention is practice by using a progestogen plus an estrogen once a month, the progestogen and estrogen should be in an aqueous suspension. It is preferred that the contraceptively effective amount be: for medroxyprogesterone acetate from about 10 mg to about 50 mg/female, for progesterone from about 25 mg to about 200 mg/female, for northindrone from about 5 mg to about 50 mg/female, for desogestrel from about 1 mg to about 4 mg/female, for levo-norgrestrel from about 0.5 mg to about 2 mg/female.
- estradiol cypionate from about 2.5 mg to about 20 mg/female, ethinyl estradiol from about 0.5 mg to about 3 mg/female, estradiol valerate from about 2.5 mg to about 20 mg/female. It is preferred the contraceptively effective amount of medroxyprogesterone acetate is from about 20 mg to about 30 mg/female and the contraceptively effective amount of estradiol cypionate is from about 3 to about 10 mg female.
- the exact dosage and frequency of administration depends on the age, weight, general physical condition of the particular patient, other medication the individual may be taking as is well known to those skilled in the art and can be more accurately determined by measuring the blood level or concentration of the progestogen or progestogen and estrogen in the patient's blood and/or the patient's response to the particular condition being treated.
- Medroxyprogesterone acetate refers to 17I-hydroxy-6I-methylpregn-4-ene- 3,20-dione 17-acetate.
- a 78 kg 37 year old female who desires to have sexual intercourse on a regular basis is shown how to give a subcutaneous injection by her physician's nurse. She injects 1.0 ml of a 150 mg/ml of an aqueous suspension of medroxyprogesterone acetate subcutaneous as instructed on the second day of her menstrual period. She has sexual intercourse three times a week with a fertile male and does not become pregnant.
- a 67 kg 21 year old female who desires to have sexual intercourse on a regular basis is shown how to give a subcutaneous injection by her gynecologist. She injects 2.0 ml of a 150 mg/ml of an aqueous suspension of medroxyprogesterone acetate subcutaneous as instructed on the third day of her menstrual period. She has sexual intercourse for six months with an average of three and a half times a week with a fertile male and does not become pregnant.
- EXAMPLE 4 40 Year Old Female - Progestogen Plus Estrogen A 71 kg 40 year old female who desires to have sexual intercourse on a regular basis is shown how to give a subcutaneous injection by her physician's nurse.
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Gynecology & Obstetrics (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
Description
Claims
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU49579/99A AU4957999A (en) | 1998-07-17 | 1999-07-09 | Subcutaneous medroxyprogesterone acetate for contraception |
EP99933540A EP1098653A2 (en) | 1998-07-17 | 1999-07-09 | Subcutaneous medroxyprogesterone acetate for contraception |
JP2000559813A JP2002520346A (en) | 1998-07-17 | 1999-07-09 | Subcutaneous medroxyprogesterone acetate for contraception |
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9317198P | 1998-07-17 | 1998-07-17 | |
US10369998P | 1998-10-09 | 1998-10-09 | |
US60/103,699 | 1998-10-09 | ||
US12682499P | 1999-03-30 | 1999-03-30 | |
US60/093,171 | 1999-03-30 | ||
US60/126,824 | 1999-03-30 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2000003678A2 true WO2000003678A2 (en) | 2000-01-27 |
WO2000003678A3 WO2000003678A3 (en) | 2000-11-09 |
Family
ID=27377447
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US1999/014129 WO2000003678A2 (en) | 1998-07-17 | 1999-07-09 | Subcutaneous medroxyprogesterone acetate for contraception |
Country Status (4)
Country | Link |
---|---|
EP (1) | EP1098653A2 (en) |
JP (1) | JP2002520346A (en) |
AU (1) | AU4957999A (en) |
WO (1) | WO2000003678A2 (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002521452A (en) * | 1998-07-28 | 2002-07-16 | イエナファーム ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディートゲゼルシャフト | Use of biogenic estrogen sulfamate for hormone replacement therapy |
EP2399566A1 (en) * | 2010-06-28 | 2011-12-28 | Laboratoire HRA Pharma | Once-a-month method of contraception |
EP2419108A1 (en) | 2009-04-14 | 2012-02-22 | Laboratoire HRA Pharma | Method for on-demand contraception |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0129947A2 (en) * | 1983-05-19 | 1985-01-02 | World Health Organisation | Contraceptive compositions based on esters of levo-norgestrel |
EP0303306A1 (en) * | 1987-08-08 | 1989-02-15 | Akzo N.V. | Contraceptive implant |
US4826831A (en) * | 1983-08-05 | 1989-05-02 | Pre Jay Holdings Limited | Method of hormonal treatment for menopausal or post-menopausal disorders involving continuous administration of progestogens and estrogens |
WO1993000070A1 (en) * | 1991-06-28 | 1993-01-07 | Endorecherche Inc. | Controlled release systems and low dose androgens |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SU724127A1 (en) * | 1977-02-10 | 1980-03-30 | Всесоюзный Научно-Исследовательский Институт Акушерства И Гинекологии | Ovary function determining method |
SU686736A1 (en) * | 1977-02-10 | 1979-09-25 | Всесоюзный Научно-Исследовательский Институт Акушерства И Гинекологии | Method of treating endocrine gynecologic diseases |
-
1999
- 1999-07-09 WO PCT/US1999/014129 patent/WO2000003678A2/en not_active Application Discontinuation
- 1999-07-09 AU AU49579/99A patent/AU4957999A/en not_active Abandoned
- 1999-07-09 EP EP99933540A patent/EP1098653A2/en not_active Withdrawn
- 1999-07-09 JP JP2000559813A patent/JP2002520346A/en active Pending
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0129947A2 (en) * | 1983-05-19 | 1985-01-02 | World Health Organisation | Contraceptive compositions based on esters of levo-norgestrel |
US4826831A (en) * | 1983-08-05 | 1989-05-02 | Pre Jay Holdings Limited | Method of hormonal treatment for menopausal or post-menopausal disorders involving continuous administration of progestogens and estrogens |
EP0303306A1 (en) * | 1987-08-08 | 1989-02-15 | Akzo N.V. | Contraceptive implant |
WO1993000070A1 (en) * | 1991-06-28 | 1993-01-07 | Endorecherche Inc. | Controlled release systems and low dose androgens |
Non-Patent Citations (6)
Title |
---|
COUTINHO E M ET AL: "Conception control by monthly injections of medroxyprogesterone suspension and long-acting oestrogen." JOURNAL OF REPRODUCTION AND FERTILITY, (1968 MAR) 15 (2) 209-14., XP000904773 cited in the application * |
DATABASE WPI Derwent Publications Ltd., London, GB; AN 1980-36031c XP002136710 "Endocrine gynaecological disorder treatment- by- injecting oestrogen and progesterone subcutaneously in amounts depending on skin sensitivity." & SU 686 736 A (OBSTETRICS RESEARCH INSTITUTE), 28 September 1977 (1977-09-28) * |
DATABASE WPI Derwent Publications Ltd., London, GB; AN 1980-80228c XP002136709 "Investigating functioning of ovaries - by subcutaneous injections of oestradiol, oestriol, oestrone and progesterone and evaluating skin reaction." & SU 724 127 A (OBSTETRICS GYNAECOL), 30 March 1980 (1980-03-30) * |
HALL P ET AL: "Introductory study of the once-a-month, injectable contraceptive Cyclofem in Brazil, Chile, Colombia, and Peru." CONTRACEPTION, (1997 DEC) 56 (6) 353-9., XP000904758 cited in the application * |
JEF REYNOLDS: "Martindale, The Extra PHarmacopea" , THE ROYAL PHARMACEUTICAL SOCIETY , LONDON, UK XP002136038 page 1495, column 2 -page 1496, column 2 * |
SARKAR N.N. ET AL: "Bioavailability of norethindrone in women and rabbits after administration of norethindrone acetate through the subcutaneous route." EXPERIENTIA, (1982) 38/11 (1345-1346). CODEN: EXPEAM, XP000891845 * |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2002521452A (en) * | 1998-07-28 | 2002-07-16 | イエナファーム ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディートゲゼルシャフト | Use of biogenic estrogen sulfamate for hormone replacement therapy |
JP4891479B2 (en) * | 1998-07-28 | 2012-03-07 | ステリクス リミテッド | Use of biologically derived estrogen sulfamate for hormone replacement therapy |
EP2419108A1 (en) | 2009-04-14 | 2012-02-22 | Laboratoire HRA Pharma | Method for on-demand contraception |
US9283233B2 (en) | 2009-04-14 | 2016-03-15 | Laboratoire Hra-Pharma | Method for on-demand contraception |
EP3106167A1 (en) * | 2009-04-14 | 2016-12-21 | Laboratoire HRA Pharma | Method for on-demand contraception |
US10159681B2 (en) | 2009-04-14 | 2018-12-25 | Laboratoire Hra-Pharma | Method for on-demand contraception |
EP2399566A1 (en) * | 2010-06-28 | 2011-12-28 | Laboratoire HRA Pharma | Once-a-month method of contraception |
WO2012000909A1 (en) * | 2010-06-28 | 2012-01-05 | Laboratoire Hra-Pharma | Once-a-month method of contraception |
US20130090318A1 (en) * | 2010-06-28 | 2013-04-11 | Laboratoire Hra-Pharma | Once-a-month method of contraception |
Also Published As
Publication number | Publication date |
---|---|
AU4957999A (en) | 2000-02-07 |
EP1098653A2 (en) | 2001-05-16 |
WO2000003678A3 (en) | 2000-11-09 |
JP2002520346A (en) | 2002-07-09 |
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