Spironolactone is an anti-mineralocorticoid agent that also acts as an anti-androgen. It is a potassium sparing diuretic that in high doses (100-200 mg/ day) demonstrates significant anti-androgenic properties. Spironolactone interferes with testosterone biosynthesis by reducing 17-hydroxylase activity and thus lowers plasma testosterone. It also inhibits dihydrotestosterone's binding to the androgen receptor. It is not FDA-approved for treatment of androgenic symptoms but in many studies has been shown to be an effective agent in this regard. It is often combined with oral contraceptives to reduce testosterone action and production.
Menstrual cycle irregularity can be seen with the use of spironolactone alone. Typically it is combined with oral contraceptives, thereby reducing this concern. Additionally it is a pregnancy category C drug so should be used with contraception to avoid pregnancy while taking it.
Flutamine and finasteride can improve androgenic symptoms in PCOS. In general potential serious side-effects have limited their use in the United States. Flutamide
is a nonsteroidal, nonhormonal antiandrogenic drug, which has been demonstrated to block the action of dihydrotestosterone (DHT) on androgen receptors. It has been associated with hepatocellular dysfunction. Finasteride is a 4-aza analog of testosterone and is a competitive inhibitor of both tissue and hepatic 5-alpha reductase. This results in inhibition of the conversion of testosterone to dihydrotestosterone. In small mostly uncontrolled studies it has been shown to be effective in the treatment of hirsutism. It does not seem to treat androgenic alopecia in women however, unlike the effect seen in male pattern baldness in men.
Eflornithine hydrochloride is an inhibitor of ornithine decarboxylase in skin. It is available as a topical cream that can slow the rate of hair growth and has been shown to have some effect in the treatment of facial hirsutism.
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