Progestogens with Antiandrogenic Properties

@article{Raudrant2012ProgestogensWA,
  title={Progestogens with Antiandrogenic Properties},
  author={Daniel Raudrant and Thomas Rabe},
  journal={Drugs},
  year={2012},
  volume={63},
  pages={463-492}
}
Chlormadinone acetate, cyproterone acetate and dienogest are potent, orally active progestogens, which have antiandrogenic instead of partial androgenic activity. They act mainly by blocking androgen receptors in target organs, but also reduce the activity of skin 5α-reductase, the enzyme responsible for converting testosterone to the more potent androgen, 5α-dihydrotestosterone, in sebaceous glands and hair follicles. Chlormadinone acetate and cyproterone acetate also suppress gonadotropin… 

Use of oral contraceptives in the management of acne

Assessment of the cause of acne and appropriate management can be undertaken using oral contraceptives containing low daily doses of ethinyl estradiol associated with a progestin compound, such as cyproterone acetate, drospirenone, or chlormadinone acetates, the antiandrogenic activity of which has been demonstrated by many studies in animals and in humans.

Evaluation of different antiandrogenic progestins on clinical and biochemical variables in polycystic ovary syndrome

DNG exerted an important stimulatory effect on sex hormone-binding globulin (SHBG) and biochemical markers of hyperandrogenism as well as dehydroepiandrosterone sulphate and total testosterone in women with polycystic ovary syndrome.

Ethinylestradio-Chlormadinone Acetate Combination for the Treatment of Hirsutism and Hormonal Alterations of Normal-Weight Women With Polycystic Ovary Syndrome: Evaluation of the Metabolic Impact

The EE-CMA combination ameliorates clinical and hormonal features of PCOS women, with no detrimental effects on glucose, insulin, and lipid metabolism.
...

References

SHOWING 1-10 OF 185 REFERENCES

[Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations].

The results exclude the possibility that the very distinct antiandrogenic effect of dienogest on a cellular level is neutralised or reduced by an increased systemic supply of androgen.

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

Data demonstrate that the progestins norgestimate and dienogest in particular combined 5α-reductase inhibition with minimal androgenic potential and might help in the treatment of clinical hyperandrogeny in women.

Antifertility effects of low dose progestin.

Culdoscopic visualization of the ovaries showing recent corpora lutea indicates that contraception is not dependent on ovulation suppression, and sustained release of drugs from silastic capsule implants has been demonstrated but this method has not yet been developed as an acceptable and useful means of human contraception.

Comparative Pharmacology of Newer Progestogens

SummaryThe newer progestogens desogestrel, norgestimate, gestodene, dienogest and nomegestrol share the common property of having weak or no androgenic effects, but there is great variation between

Effects on acne of two oral contraceptives containing desogestrel and cyproterone acetate.

Both Marvelon and Diane are effective in the treatment of acne in Oriental women who also need reliable contraception, without marked differences between the preparations.

Can oral contraceptive steroids influence the elimination of nifedipine and its primary pryidine metabolite in humans?

The investigation presented demonstrates the importance of metabolite measurement when in vivo studies are undertaken to investigate different influences on drug metabolizing ability.

Androgens and Therapeutic Aspects of Antiandrogens in Women

Antiandrogens provide a logical and clinically effective pharmacotherapy of hyperandrogenic disorders and both steriodal and nonsteroidal antiandrogens may cause significant side effects, largely because of their interactions not only with androgen receptors, but also with other receptors and various enzymatic activities.

Contraceptive and therapeutic effectiveness of two low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsute patients.

  • S. VenturoliB. Ravaioli C. Flamigni
  • Medicine, Biology
    The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception
  • 1998
Both treatments greatly improve hirsutism, reduce clinical problems and side-effects, guarantee both anovulation and contraceptive effectiveness and afford an optimal control of the menstrual cycle.

RU 58841, a new specific topical antiandrogen: A candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism

...