Dienogest.
The progestogen dienogest exhibits highly selective binding to the progesterone receptor. It has high progestational and significant antiandrogenic activity, but only moderate antigonadotrophic activity. Dienogest inhibits ovulation, produces secretory transformation of the endometrium and has antiproliferative effects. Oral dienogest 2 mg/day plus ethinylestradiol 30 micrograms/day provides effective contraception (Pearl Index approximately 0.2). Cycle stability is good during long term use of this combination; irregular vaginal bleeding was evident in 6% of women after 12 months' use. Androgenic symptoms (including hirsutism, seborrhoea, alopecia, acne vulgaris and hair and skin greasiness) improved in women treated with dienogest plus ethinylestradiol. The adverse events associated with dienogest are typical of those expected of a progestogen. The drug does not produce androgenic adverse effects and has little clinically significant effect on metabolic, lipid and haemostatic parameters.
Foster
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Adis International Limited, Auckland, New Zealand. demail@adis.co.nz
Wilde
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D000726:Androgen Antagonists / Q000494:pharmacology; D000818:Animals; D002986:Clinical Trials as Topic; D003276:Contraceptives, Oral / Q000494:pharmacology*; D004997:Ethinyl Estradiol / Q000494:pharmacology; D005260:Female; D006801:Humans; D009277:Nandrolone / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology; D011372:Progestins / Q000494:pharmacology
D000726:Androgen Antagonists; D003276:Contraceptives, Oral; D011372:Progestins; D004997:Ethinyl Estradiol; C023635:dienogest; D009277:Nandrolone