Pharmacological basis for clinical use of antiandrogens

The first antiandrogen which was also of clinical interest--cyproterone acetate (CPA)--was discovered at the beginning of the 60th. CPA acts in all target organs for androgens and in principle affects all functions which are governed or influenced by androgens under physiological or pathophysiological conditions.

Accessory sexual gland function and spermatogenesis are inhibited, there is a loss of libido in most species, the onset of puberty and bone maturation is delayed, sebaceous gland function and lipogenesis is inhibited, androgen mediated steps in male sexual differentiation do not occur. CPA is also a highly effective progestrogen and it inhibits gonadotrophine secretion. The progestational partial effect is especially important for the use of this drug in women in the treatment of certain dermatological disorders. CPA has certain glucocorticoid-like properties in animals. In humans these effects were only seen under high-dose therapy of children with precocious puberty (greater than 80 to 100 mg/m3 body area) but never in adults. Proven indications for CPA: Prostatic carcinoma, precocious puberty, hypersexuality and sexual deviations, androgenization in women (hirsutism, acne, seborrhoea oleosa, alopecia androgentica).