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
• • 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
  • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P19/00—Drugs for skeletal disorders
  • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
  • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P5/00—Drugs for disorders of the endocrine system
  • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
  • A61P5/30—Oestrogens

Definitions

• the present invention relates to the use of a one-month injection (once-a-month injectable composition) containing an estrogenic and gestagenic component as active ingredients for the manufacture of a medicament for contraception and simultaneous hormone replacement therapy for peri- and premenopausal women.
• a monthly injection in the sense of the present invention means a hormone preparation which is injected once a month for women of childbearing age for contraception.
• This hormone preparation contains a gestagenic and an estrogenic component as active substances, each with a long enough effect to achieve a contraceptive effect for a period of one month.
• progestogen-only injectables are also available, which ensure long-term contraceptive protection, albeit with poor cycle control.
• US Pat. No. 4,826,831 already discloses a method for the hormonal treatment of menopausal, including perimenopausal and postmenopausal disorders (disorders), which relates in particular to treatment using a progestogen in conjunction with an estrogen.
• the estrogen can also be continuous or cyclical, i.e. H. with breaks.
• estrogens and progestogens are mentioned which are suitable for the purposes of this invention, including norethisterone acetate and medroxyprogesterone acetate as progestogens and estradiol valerate.
• norethisterone acetate and medroxyprogesterone acetate as progestogens and estradiol valerate.
• it should be possible to use all estrogens and progestogens that are also in oral contraceptives are conceivable. Adequate contraceptive protection is provided by the described
• Norethisterone acetate / estradiol valerate is also disclosed as a possible combination.
• progestogen and estrogen used are low: progestogen in a daily amount equivalent to 0.025 mg to 0.075 mg levonorgestrel and estrogen in a daily amount corresponding to 0.5 to 2.0 mg estradiol .
• the amount to be administered daily is the amount to be administered daily.
• estradiol valerate 20 mg to 100 mg estradiol valerate are given.
• Gestagen depot formulation for 3 months should be 50 to 500 mg medroxyprogesterone acetate or 20 to
• This patent also relates to pharmaceutical compositions for performing them
• Premenopause begins, onset of ailments, such as hot flushes, dryness of the
• US Pat. No. 4,826,831 expressly states that oral administration is not a method of contraception.
• peri- and premenopause should have their conventional meaning as described in "The Controversial Cli acteric", P.A. van Keep et al., Ed., MTP Press (1981) on page 9 can be understood.
• a one-month injection in the sense of the present invention should be understood to mean both the products already mentioned at the beginning and all other possible combinations of a natural estrogen with a progestogen.
• the two active components must be present in a depot formulation, the depot effect being achieved either through the special type of pharmaceutical formulation (for example microcrystalline suspension) or rather through the chemical structure of the progestogen and / or estrogen (for example through the esterification of free hydroxyl groups).
• the main estrogens here are 17 ⁇ -estradiol, estradiol-3-benzoate, estradiol-17-valerate, cypionate, undecylate, enanthate and or other estradiol esters (US Pat. No. 2,611,773, US Pat
• the gestagen component is preferably selected from the group of compounds
• Norethisterone acetate, norethisterone acetate, medroxyprogesterone acetate and cyproterone acetate Norethisterone acetate, norethisterone acetate, medroxyprogesterone acetate and cyproterone acetate.
• Tables LA and 2A list selected estrogens or gestagens to be used according to the present invention, with an indication of the preferred amount range.
• Tables 1B and 2B show the particularly preferred amounts of the respective estrogen or progestogen which are to be contained in a one-month syringe according to the present invention.
• the combination of medroxyprogesterone acetate and estradiol cypionate is preferred for producing a one-month syringe for peri- and premenopausal contraception; the combination of norethisterone enanthate / estradiol valerate is particularly preferred.
• the particularly preferred embodiment based on the progestogen / estrogen combination norethisterone enanthate / estradiol valerate not only offers a prophylactic effect with regard to osteoporosis, but in addition to the bone depletion-inhibiting effect of estrogen, a bone building effect caused by the norethis-terone enanthate is observed in this combination.

Landscapes

• Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Medicinal Chemistry (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Epidemiology (AREA)
• Physical Education & Sports Medicine (AREA)
• Endocrinology (AREA)
• Rheumatology (AREA)
• Reproductive Health (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Diabetes (AREA)
• Gynecology & Obstetrics (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Steroid Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Medicinal Preparation (AREA)

Applications Claiming Priority (3)

Publications (1)

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ID=7757668

Family Applications (1)

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• 1995
  • 1995-03-16 DE DE19510861A patent/DE19510861A1/de not_active Withdrawn
• 1996
  • 1996-03-15 CZ CZ972896A patent/CZ289697A3/cs unknown
  • 1996-03-15 PL PL96322202A patent/PL322202A1/xx unknown
  • 1996-03-15 HU HU9801691A patent/HUP9801691A3/hu unknown
  • 1996-03-15 KR KR1019970706467A patent/KR19980703058A/ko not_active Application Discontinuation
  • 1996-03-15 EP EP96907506A patent/EP0814811A1/de not_active Withdrawn
  • 1996-03-15 WO PCT/EP1996/001201 patent/WO1996028165A1/de not_active Application Discontinuation
  • 1996-03-15 AR ARP960101766A patent/AR002283A1/es unknown
  • 1996-03-15 SK SK1239-97A patent/SK123997A3/sk unknown
  • 1996-03-15 CA CA002215382A patent/CA2215382A1/en not_active Abandoned
  • 1996-03-15 AU AU51108/96A patent/AU713258B2/en not_active Ceased
  • 1996-03-15 MX MX9707009A patent/MX9707009A/es not_active IP Right Cessation
  • 1996-03-15 JP JP8527295A patent/JPH11501649A/ja not_active Ceased
  • 1996-03-15 NZ NZ304027A patent/NZ304027A/xx not_active IP Right Cessation
  • 1996-03-17 IL IL11751696A patent/IL117516A/xx not_active IP Right Cessation
  • 1996-03-18 ZA ZA962177A patent/ZA962177B/xx unknown
• 1997
  • 1997-09-15 NO NO974255A patent/NO974255L/no not_active Application Discontinuation

Non-Patent Citations (1)

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