Inhibition of skin 5α-reductase by oral contraceptive progestinsin vitro
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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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Cited by (4)
- Progestogens with Antiandrogenic Properties 2003
- New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia®) for contraception and for treatment of heavy menstrual bleeding: patient considerations 2012
- Early onset vulvar Lichen Sclerosus in premenopausal women and oral contraceptives 2007
- Use of oral contraceptives for management of acne vulgaris and hirsutism in women of reproductive and late reproductive age 2018
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Cited by (4)
- Use of oral contraceptives for management of acne vulgaris and hirsutism in women of reproductive and late reproductive age 2018
- New developments in oral contraception: clinical utility of estradiol valerate/dienogest (Natazia®) for contraception and for treatment of heavy menstrual bleeding: patient considerations 2012
- Early onset vulvar Lichen Sclerosus in premenopausal women and oral contraceptives 2007
- Progestogens with Antiandrogenic Properties 2003
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