Objectives: We reviewed the mechanisms of androgen actions and the established and experimental uses of antiandrogens in women.

Methods: Relevant studies were identified through a computerized bibliographic search (MEDLINE) and through manual review of bibliographies in relevant publications.

Results: Androgens exert major effects on the functions of gonads, sex organs, and various "nonreproductive" organs and systems, including muscles, liver, skin, nervous system, and the immune system. Most, but not all, of the actions of androgens may be explained by their binding with specific androgen receptors. Antiandrogens prevent androgens from expressing their activity at target cells. They act primarily by binding to androgen receptors and thus preventing activation of receptors by androgens. Steroidal antiandrogens may also exert a wide range of other hormonal and antihormonal effects by interacting with receptors for progesterone, glucocorticoids, and mineralocorticoids. Furthermore, some antiandrogens may decrease the production of androgens by acting at the hypothalamic-pituitary unit and modifying the release of LH, or by directly inhibiting individual enzymes involved in steroidogenesis. Antiandrogens are widely used in the treatment of women with various hyperandrogenic conditions, including polycystic ovary syndrome, idiopathic hirsutism, acne, seborrhea, and hair loss.

Conclusions: Antiandrogens provide a logical and clinically effective pharmacotherapy of hyperandrogenic disorders. However, both steroidal 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. Difficulties in designing the optimal antiandrogen largely result from the complexities of androgen metabolism and action in various tissues.