Androgen Receptor Inhibitors
- Spironolactone (Aldactone)
Spironolactone, brand name Aldactone, is in a class of drugs called potassium-sparing diuretics (often called water pills). Spironolactone is typically used to reduce fluid in your body without causing the loss of potassium. It is also used to treat potassium deficiency, high blood pressure (hypertension), swelling (edema), and a hormonal disorder called hyperaldosteronism.
Spironolactone acts as an anti-androgen in two ways. First, it slows down the production of androgens in the adrenal glands and ovaries. Second, it blocks the action of androgens in part by preventing dihydrotestosterone (DHT) from binding to its androgenetic receptor.
- Cimetidine (Tagamet)
Cimetidine, brand name Tagamet, belongs to a class of histamine blockers used mainly to treat gastrointestinal ulcers. The histamine-blocking action prevents the stomach from producing excess acid, allowing the body to heal the ulcer. Cimetidine also has a fairly powerful anti-androgenic effect and has been shown to block dihydrotestosterone from binding the follicle receptor sites.
Cimetidine has been used to treat excess facial hair growth (hirsutism) in women and has shown promising results in studies of women with androgenic alopecia. High doses are needed to achieve results, so men should not take cimetidine to treat their hair loss due to possible feminizing effects, including adverse sexual side effects.
- Cyproterone Acetate
Cyproterone acetate is used to reduce excessive sex drive in men and to treat pronounced sexual aggression. It is also prescribed for severe hirsutism in woman of childbearing age and for androgenetic alopecia in women. Cyproterone acetate exerts its effects by blocking the binding of dihydrotestosterone (DHT) to its receptors.
Cyproterone acetate is not available in the U.S. Doctors consider it one of the last resorts for treating female pattern hair loss because of its possible toxicity and long-term side effects. As with any drug, side effects other than those listed on the package may occur. Contact your doctor if you notice a side effect that is unusual or particularly bothersome.
Estrogen and Progesterone
Estrogen and progesterone pills and creams may be an effective treatment for women with androgenetic alopecia who are going through menopause or whose estrogen and/or progesterone are lacking for other reasons.