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Antigestagene

Neue Einsatzmöglichkeiten in der Gynäkologie

Antiprogestins

New therapeutic options in gynaecology

  • Leitthema
  • Published:
Gynäkologische Endokrinologie Aims and scope

Zusammenfassung

Progesteron spielt für den Eintritt und den Erhalt einer Schwangerschaft eine entscheidende Rolle. Da Antigestagene die Effekte von Progesteron antagonisieren können, stellen sie eine Gruppe hochinteressanter Substanzen dar, die nicht nur zum Schwangerschaftsabbruch bzw. zur Abortinduktion, sondern auch zur Familienplanung eingesetzt werden könnten. Im Hinblick auf die Anwendung im Rahmen der Kontrazeption ist die Therapie mit Mifepriston zur Notfallkontrazeption das heute am weitesten entwickelte Konzept. Eine Vielzahl von Studien belegt hier die effektive Wirksamkeit. Um ein neues, östrogenfreies orales Kontrazeptivum zu entwickeln, sind viele verschiedene Therapieregime untersucht worden, wobei die kontinuierliche Anwendung von 5 mg Mifepriston/Tag das erfolgversprechendste Verfahren zu sein scheint. Allerdings ist Mifepriston bisher nur zur Abortinduktion zugelassen. Andere klinisch interessante Forschungsgebiete beinhalten die Anwendung von Antigestagenen bei Myomen, Endometriose, zur Behandlung und Prävention hormonabhängiger Tumoren wie Mammakarzinomen und Meningeomen, aber auch die Anwendung bei kortikoidabhängigen Erkrankungen.

Abstract

Progesterone plays a crucial role for the establishment and maintenance of pregnancy. Since antiprogestins counteract the effects of progesterone, they are a very promising group of compounds that could be used not only for pregnancy termination and abortion induction, but also for family planning. Currently the most promising contraceptive approach appears to be the use of mifepriston for post-coital emergency contraception, the efficacy of which has been proven in a number of clinical trials. Various regimes have been tested to develop a new estrogen-free oral contraceptive pill. Studies suggest that the continuous use of 5 mg mifepriston/day is a very promising regimen. However, mifepriston has currently only been approved for abortion induction. Other areas of further research include the treatment of uterine fibromyomas, endometriosis, and the treatment and prevention of hormone-dependent tumours such as breast cancer and meningiomas. Another potential clinical indication is the use of mifepriston for corticoid-related disorders.

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Literatur

  1. Baird DT, Brown A, Critchley HO et al. (2003) Effect of long-term treatment with low-dose mifepristone on the endometrium. Hum Reprod 18: 61–68

    Article  PubMed  CAS  Google Scholar 

  2. Brenner RM, Slayden OD, Critchley HO (2002) Anti-proliferative effects of progesterone antagonists in the primate endometrium: a potential role for the androgen receptor. Reproduction 124: 167–172

    Article  PubMed  CAS  Google Scholar 

  3. Brown A, Cheng L, Lin S, Baird DT (2002) Daily low-dose mifepristone has contraceptive potential by suppressing ovulation and menstruation: a double-blind randomized control trial of 2 and 5 mg per day for 120 days. J Clin Endocrinol Metab 87: 63–70

    Article  PubMed  CAS  Google Scholar 

  4. Cheng L, Gülmezoglu AM, Piaggio G et al. (2008) Interventions for emergency contraception. Cochrane Database Syst Rev Issue 2. Art. No.: CD001324. DOI: 10.1002/14651858.CD001324.pub3

  5. Cheng L, Zhu H, Wang A et al. (2000) Once a month administration of mifepristone improves bleeding patterns in women using subdermal contraceptive implants releasing levonorgestrel. Hum Reprod 15: 1969–1972

    Article  PubMed  CAS  Google Scholar 

  6. Croxatto HB, Salvatierra AM, Fuentealba B, Massai R (1998) Contraceptive potential of a mifepristone-nomegestrol acetate sequential regimen in women. Hum Reprod 13: 3297–3302

    Article  PubMed  CAS  Google Scholar 

  7. Danielsson KG, Swahn ML, Westlund P et al. (1997) Effect of low daily doses of mifepristone on ovarian function and endometrial development. Hum Reprod 12: 124–131

    Article  PubMed  CAS  Google Scholar 

  8. Eisinger SH, Bonfiglio T, Fiscella K et al. (2005) Twelve-month safety and efficacy of low-dose mifepristone for uterine myomas. J Minim Invasive Gynecol 12: 227–233

    Article  PubMed  Google Scholar 

  9. Eisinger SH, Meldrum S, Fiscella K et al. (2003) Low-dose mifepristone for uterine leiomyomata. Obstet Gynecol 101: 243–250

    Article  PubMed  CAS  Google Scholar 

  10. Engman M, Skoog L, Söderqvist G, Gemzell-Danielsson K (2008) The effect of mifepristone on breast cell proliferation in premenopausal women evaluated through fine needle aspiration cytology. Hum Reprod Jun 24 (Epub ahead of print)

  11. Fiscella K, Eisinger SH, Meldrum S et al. (2006) Effect of mifepristone for symptomatic leiomyomata on quality of life and uterine size: a randomized controlled trial. Obstet Gynecol 108: 1381–1387

    PubMed  CAS  Google Scholar 

  12. Grow DR, Williams RF, Hsiu JG, Hodgen GD (1996) Antiprogestin and/or gonadotropin-releasing hormone agonist for endometriosis treatment and bone maintenance: a 1-year primate study. J Clin Endocrinol Metab 81: 1933–1939

    Article  PubMed  CAS  Google Scholar 

  13. Grunberg SM, Weiss MH, Russell CA et al. (2006) Long-term administration of mifepristone RU486: clinical tolerance during extended treatment of meningioma. Cancer Invest 24: 727–733

    Article  PubMed  CAS  Google Scholar 

  14. Herrmann W, Wyss R, Riondel A et al. (1982) The effects of an antiprogesterone steroid in women: interruption of the menstrual cycle and of early pregnancy. C R Seances Acad Sci III 294: 933–938

    PubMed  CAS  Google Scholar 

  15. Kulier R, Gülmezoglu AM, Hofmeyr GJ et al. (2004) Medical methods for first trimester abortion. Cochrane Database Syst Rev Issue 1. Art. No.: CD002855. DOI: 10.1002/14651858.CD002855.pub3

  16. Lakha F, Ho PC, Van der Spuy ZM et al. (2007) A novel estrogen-free oral contraceptive pill for women: multicenter, double-blind, randomized controlled trial of mifepristone and progestogen-only pill (levonorgestrel). Hum Reprod 22: 2428–2436

    Article  PubMed  CAS  Google Scholar 

  17. Ledger WL, Sweeting VM, Hillier H, Baird DT (1992) Inhibition of ovulation by low-dose mifepristone (RU 486). Hum Reprod 7: 945–950

    PubMed  CAS  Google Scholar 

  18. Lohr PA, Hayes JL, Gemzell-Danielsson K (2008) Surgical versus medical methods for second trimester induced abortion. Cochrane Database Syst Rev Issue 1. Art. No.: CD006714. DOI: 10.1002/14651858.CD006714.pub2

  19. Luukkainen T, Heikinheimo O, Haukkamaa M, Lähteenmäki P (1988) Inhibition of folliculogenesis and ovulation by the antiprogesterone RU 486. Fertil Steril 49: 961–963

    PubMed  CAS  Google Scholar 

  20. Massai MR, Pavez M, Fuentealba B et al. (2004) Effect of intermittent treatment with mifepristone on bleeding patterns in Norplant implant users. Contraception 70: 47–54

    Article  PubMed  CAS  Google Scholar 

  21. Milgrom E, Atger M, Baulieu EE (1970) Progesterone in uterus and plasma. IV: Progesterone receptor(s) in guinea pig uterus cytosol. Steroids 16: 741–754

    Article  PubMed  CAS  Google Scholar 

  22. Narvekar N, Glasier A, Dada K et al. (2006) Toward developing a once-a-month pill: a double-blind, randomized, controlled trial of the effect of three single doses of mifepristone given at midcycle on the pattern of menstrual bleeding. Fertil Steril 86: 819–824

    Article  PubMed  CAS  Google Scholar 

  23. Nayak NR, Slayden OD, Mah K et al. (2007) Antiprogestin-releasing intrauterine devices: a novel approach to endometrial contraception. Contraception 75 (6 Suppl): S104–111

    Article  PubMed  CAS  Google Scholar 

  24. Newfield RS, Spitz IM, Isacson C, New MI (2001) Long-term mifepristone (RU486) therapy resulting in massive benign endometrial hyperplasia. Clin Endocrinol (Oxf) 54: 399–404

    Google Scholar 

  25. O’Malley BW, McGuire WL, Kohler PO, Korenman SG (1969) Studies on the mechanism of steroid hormone regulation of synthesis of specific proteins. Recent Prog Horm Res 25: 105–160

    Google Scholar 

  26. Philibert D, Deraedt R, Teutsch G (1981) RU 38486: a potent antiglucocorticoid in vivo. Paper presented at the VII International Congress of Pharmacology, 1981, Tokyo, Japan

  27. Piaggio G, Heng Z, von Hertzen H et al. (2003) Combined estimates of effectiveness of mifepristone 10 mg in emergency contraception. Contraception 68: 439–446

    Article  PubMed  CAS  Google Scholar 

  28. Slayden OD, Nayak NR, Burton KA et al. (2001) Progesterone antagonists increase androgen receptor expression in the rhesus macaque and human endometrium. J Clin Endocrinol Metab 86: 2668–2679

    Article  PubMed  CAS  Google Scholar 

  29. Spitz IM, Grunberg SM, Chabbert-Buffet N et al. (2005) Management of patients receiving long-term treatment with mifepristone. Fertil Steril 84: 1719–1726

    Article  PubMed  CAS  Google Scholar 

  30. van der Stege JG, Pahl-van Beest EH, Beerthuizen RJ et al. (2006) Effects of a preovulatory single low dose of mifepristone on ovarian function. Eur J Contracept Reprod Health Care 11: 104–108

    Article  Google Scholar 

  31. Verbost PM, Hanssen RG, Korver GH, Mulders TM (2005) TM ORG 33628 and ORG 31710 to control vaginal bleeding in progestin-only contraceptive regimens. Semin Reprod Med 23: 101–111

    Article  PubMed  CAS  Google Scholar 

  32. von Hertzen H, Van Look PF (2005) Antiprogestins for contraception? Semin Reprod Med 23: 92–100

    Article  Google Scholar 

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Authors and Affiliations

  1. Praxis für gynäkologische Endokrinologe und Reproduktionsmedizin, Gynaekologicum Hamburg, Altonaerstraße 59, 20357, Hamburg, Deutschland

    A. Schwenkhagen & K. Schaudig

  2. Klinik für Gynäkologie und Geburtshilfe, Universität Schleswig-Holstein, Campus Lübeck, Lübeck, Deutschland

    A. Schwenkhagen & K. Schaudig

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  1. A. Schwenkhagen
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  2. K. Schaudig
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Correspondence to A. Schwenkhagen.

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Schwenkhagen, A., Schaudig, K. Antigestagene. Gynäkologische Endokrinologie 6, 216–220 (2008). https://doi.org/10.1007/s10304-008-0268-3

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  • DOI: https://doi.org/10.1007/s10304-008-0268-3

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