ANDROGENS AND THERAPEUTIC ASPECTS OF ANTIANDROGENS IN WOMEN

OBJECTIVES: We reviewed the mechanisms of androgen actions and the est ablished and experimental uses of antiandrogens in women. METHODS: Rel evant studies were identified through a computerized bibliographic sea rch (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 syst ems, including muscles, liver, shin, nervous system, and the immune sy stem. Most, but not all, of the actions of androgens may be explained by their binding with specific androgen receptors. Antiandrogens preve nt androgens from expressing their activity at target cells. They act primarily by binding to androgen receptors and thus preventing activat ion 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 mineralocortico ids. Furthermore, some antiandrogens may decrease the production of an drogens by acting at the hypothalamic-pituitary unit and modifying the release of LH, or by directly inhibiting individual enzymes involved in steroidogenesis. Antiandrogens ave widely used in the treatment of women with various hyperandrogenic conditions, including polycystic ov ary syndrome, idiopathic hirsutism, acne, seborrhea, and hair loss. CO NCLUSIONS: Antiandrogens provide a logical and clinically effective ph armacotherapy of hyperandrogenic disorders. However, both steroidal an d nonsteroidal antiandrogens may cause significant side effects, large ly because of their interactions not only with androgen receptors, but also with other receptors and various enzymatic activities. Difficult ies in designing the optimal antiandrogen largely result from the comp lexities of androgen metabolism and action in various tissues.