Inhibition of skin 5 alpha-reductase by oral contraceptive progestins in vitro

T. Rabe, A Kowald, Axel Kowald, J. Ortmann, S. Rehberger-Schneider
Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology · 2000 · vol. 14(4) , pp. 223–230 · doi:10.3109/09513590009167685 · PMID:11075290 · W2014123062
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In vitro assays demonstrate that oral contraceptive progestins norgestimate and dienogest inhibit skin 5α-reductase activity while exhibiting minimal androgenic potential, suggesting their utility in treating clinical hyperandrogeny.

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Abstract

Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5 alpha-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androgen disorders of the skin. The mechanisms of action by which oral contraceptives correct skin androgen levels may include inhibition of 5 alpha-reductase and androgen receptor activity. We investigated the inhibitory effect of oral contraceptive progestins and ethinyl estradiol on skin 5 alpha-reductase and their influence on androgen receptor activity and affinity, using three different in vitro assay systems. It was shown that norgestimate blocked 5 alpha-reductase activity with an IC50 value of 10 microM, followed by levonorgestrel (IC50 52 microM), dienogest (IC50 55 microM), cyproterone acetate (IC50 87 microM) and gestodene (IC50 98 microM). To determine the full androgenic potential of the progestins, androgen receptor binding affinities and activation potentials were determined. The progestins norgestimate and dienogest in particular combined 5 alpha-reductase inhibition with minimal androgenic potential. These data demonstrate that the progestins norgestimate and dienogest might help in the treatment of clinical hyperandrogeny in women.

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MeSH descriptors

3-Oxo-5-alpha-Steroid 4-Dehydrogenase Contraceptives, Oral Nandrolone Norgestrel Progestins Receptors, Androgen Skin 3-Oxo-5-alpha-Steroid 4-Dehydrogenase Adolescent Adult Contraceptives, Oral Dose-Response Relationship, Drug Female Humans Hyperandrogenism Hyperandrogenism Nandrolone Nandrolone Norgestrel Norgestrel

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