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EP0814811A1 - Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause - Google Patents

Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause

Info

Publication number
EP0814811A1
EP0814811A1 EP96907506A EP96907506A EP0814811A1 EP 0814811 A1 EP0814811 A1 EP 0814811A1 EP 96907506 A EP96907506 A EP 96907506A EP 96907506 A EP96907506 A EP 96907506A EP 0814811 A1 EP0814811 A1 EP 0814811A1
Authority
EP
European Patent Office
Prior art keywords
month
estradiol
replacement therapy
injectable
once
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Withdrawn
Application number
EP96907506A
Other languages
German (de)
English (en)
Inventor
Ursula Lachnit-Fixson
Semiramis Aydinlik
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Schering AG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Schering AG filed Critical Schering AG
Publication of EP0814811A1 publication Critical patent/EP0814811A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens

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)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne l'utilisation d'une injection mensuelle qui contient des composants oestrogènes et gestagènes comme principes actifs pour préparer un médicament contraceptif utile en même temps en hormonothérapie substitutive pour femmes dans la périménopause et dans la préménopause. On obtient avec ce médicament un effet contraceptif fiable avec un oestrogène "naturel" (sans éthinyloestradiol), ainsi qu'une thérapie efficace des premiers symptômes d'insuffisance d'oestrogène, ainsi qu'une prophylaxie de l'ostéoporose.
EP96907506A 1995-03-16 1996-03-15 Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause Withdrawn EP0814811A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19510861 1995-03-16
DE19510861A DE19510861A1 (de) 1995-03-16 1995-03-16 Einmonatsspritze als Depot-Kontrazeptivum und für die Hormonersatztherapie für peri- und praemenopausale Frauen
PCT/EP1996/001201 WO1996028165A1 (fr) 1995-03-16 1996-03-15 Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause

Publications (1)

Publication Number Publication Date
EP0814811A1 true EP0814811A1 (fr) 1998-01-07

Family

ID=7757668

Family Applications (1)

Application Number Title Priority Date Filing Date
EP96907506A Withdrawn EP0814811A1 (fr) 1995-03-16 1996-03-15 Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause

Country Status (17)

Country Link
EP (1) EP0814811A1 (fr)
JP (1) JPH11501649A (fr)
KR (1) KR19980703058A (fr)
AR (1) AR002283A1 (fr)
AU (1) AU713258B2 (fr)
CA (1) CA2215382A1 (fr)
CZ (1) CZ289697A3 (fr)
DE (1) DE19510861A1 (fr)
HU (1) HUP9801691A3 (fr)
IL (1) IL117516A (fr)
MX (1) MX9707009A (fr)
NO (1) NO974255L (fr)
NZ (1) NZ304027A (fr)
PL (1) PL322202A1 (fr)
SK (1) SK123997A3 (fr)
WO (1) WO1996028165A1 (fr)
ZA (1) ZA962177B (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0000313D0 (en) * 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9628165A1 *

Also Published As

Publication number Publication date
PL322202A1 (en) 1998-01-19
NZ304027A (en) 2000-05-26
AU713258B2 (en) 1999-11-25
WO1996028165A1 (fr) 1996-09-19
AU5110896A (en) 1996-10-02
ZA962177B (en) 1996-07-29
CA2215382A1 (fr) 1996-09-19
NO974255L (no) 1997-11-14
AR002283A1 (es) 1998-03-11
KR19980703058A (ko) 1998-09-05
HUP9801691A2 (hu) 1998-11-30
SK123997A3 (en) 1998-02-04
MX9707009A (es) 1997-11-29
IL117516A0 (en) 1996-07-23
NO974255D0 (no) 1997-09-15
HUP9801691A3 (en) 1999-03-01
DE19510861A1 (de) 1996-09-19
CZ289697A3 (en) 1997-12-17
IL117516A (en) 2000-07-26
JPH11501649A (ja) 1999-02-09

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