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Androgens and Therapeutic Aspects of Antiandrogens in Women

1st Department of Internal Medicine, University of Athens, Laiko Hospital, 34 Aroes Street, P. Faliro, Athens, 175-62, Greece

George Tolis, MD

Antoni J. Duleba, MD

1st Department of Internal Medicine, University of Athens, Laiko Hospital, Athens, Greece; Department of Endocrinology, Hippokration Hospital, University of Athens, Athens, Greece; Department of Obstetrics and Gynecology, Yale University School of Medicine, New Haven, Connecticut

Objectives: We reviewed the mechanism 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 gonals, sex organs, and various "monreproductive" 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 interacing with receptors for progesterone, glucocorticoids, and mineralocorticoids. Furthermore, some antiandrogens may decrease the production of dangrogens by acting at the hypothalamic-pituitary unit and modifying the release of LH, or by directly inhibiting individual enzymes involvedin steriodogenesis. 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 steriodal 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.

Key Words: Androgens • antiandrogens • spironolactone

Journal of the Society for Gynecologic Investigation, Vol. 2, No. 4, 577-592 (1995)
DOI: 10.1177/107155769500200401


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