Which medications in the drug class Antiandrogens are used in the treatment of Androgen Excess?

Updated: Mar 14, 2018
  • Author: Mohamed Yahya Abdel-Rahman, MD, MSc; Chief Editor: Richard Scott Lucidi, MD, FACOG  more...
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Antiandrogens are another group of agents used as a first-line therapy for hirsutism. However, the teratogenic potential of these drugs means that they should be used in conjunction with adequate contraception in women of reproductive age. Spironolactone, an aldosterone antagonist, competes with testosterone and dihydrotestosterone at the androgen receptor. Although its primary indication is as a diuretic, a dose of 50-200 mg/d will reduce facial hair growth in most patients after 6 cycles of treatment. [87] Concurrent use of spironolactone with OC pills has been shown to significantly improve hirsutism and reduce serum androgen levels. [88] For patients with hirsutism that is refractory to OCs after 6 months, adding spironolactone may be effective.

Flutamide is an antiandrogen used for the treatment of prostate cancer. It is more effective in treating hirsutism than spironolactone. [89] However, a recent study concluded that although flutamide is very effective in treating hirsutism, it is associated with frequent side effects and low long-term compliance. [90] Hepatic cell damage, the major complication of flutamide, may be fatal. [91] Consequently, flutamide is not approved by the FDA for treatment of hirsutism. [92]

Cyproterone acetate is an antiandrogen as well as a progestin. In one systematic review, cyproterone acetate (2 mg) was more effective than placebo, but not better than any other antiandrogen in the treatment of hirsutism. [90] It is also available in an OC pill as cyproterone acetate (2 mg) with 35 u ethinyl estradiol, which has been shown to be well tolerated. This drug is not currently available in the United States.

Finasteride, another antiandrogen, inhibits only the type 2 isoenzyme of 5 α-reductase. It is anticipated that the effect of finasteride may be partial. Whether it is equally effective or less effective than spironolactone is controversial. [93, 94] The FDA has not approved finasteride for treatment of hirsutism.

Spironolactone (Aldactone)

Used most effectively in combination with an OC. First choice because of few adverse effects, cost, and clinical experience.

Flutamide (Eulexin)

Nonsteroidal antiandrogen that inhibits androgen uptake or binding of androgen to target tissues.

Cyproterone acetate

Powerful antiandrogen usually administered with estrogens to maintain regular menstruation and to prevent conception. Not available in United States.

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