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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• Animal Behavior & Ethology (AREA)
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• Chemical Kinetics & Catalysis (AREA)
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• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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• 1999
  • 1999-07-09 AU AU49579/99A patent/AU4957999A/en not_active Abandoned
  • 1999-07-09 WO PCT/US1999/014129 patent/WO2000003678A2/en not_active Application Discontinuation
  • 1999-07-09 JP JP2000559813A patent/JP2002520346A/ja active Pending
  • 1999-07-09 EP EP99933540A patent/EP1098653A2/de not_active Withdrawn

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