Dienogest

In: Drugs · 1998 · vol. 56(5) , pp. 825–833 · doi:10.2165/00003495-199856050-00007 · PMID:9829156 · W3190789610
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Dienogest selectively binds the progesterone receptor, inhibiting ovulation, affecting the endometrium, and possessing antiandrogenic and antiproliferative properties.

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This paper reviews dienogest, a highly progesterone-receptor selective progestogen with high progestational and antiandrogenic activity but only moderate antigonadotrophic effects, summarizing its pharmacodynamics and pharmacokinetics. It reports that dienogest inhibits ovulation, induces secretory transformation of the endometrium, and has antiproliferative effects; in combination with ethinylestradiol (2 mg dienogest/30 μg ethinylestradiol), it provides effective contraception with good cycle stability and irregular bleeding in 6% after 12 months, while androgenic symptoms improve and metabolic/lipid/haemostatic parameters change little. The major caveat is that the presented contraceptive data are tied to specific fixed-dose combination use, whereas the document is largely a summary/review of different experimental and clinical studies rather than a single new trial. Relevance to endometriosis: it is directly discussed as “The therapy of endometriosis with dienogest” and includes reported studies on lipid/carbohydrate metabolism and routine liver function testing during dienogest treatment for endometriosis, though the overall paper focus is a broader drug profile and review rather than a primary endometriosis outcomes study.

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Abstract

- ▴ 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 μg/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. Similar content being viewed by others

References

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Contraception 1997 Aug; 56: 67–75 Author information Authors and Affiliations Corresponding author Rights and permissions About this article Cite this article Foster, R.H., Wilde, M.I. Dienogest. Drugs 56, 825–833 (1998). https://doi.org/10.2165/00003495-199856050-00007 Published: Issue date: DOI: https://doi.org/10.2165/00003495-199856050-00007

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