Antiandrogens in the treatment of acne and hirsutism.

The review discusses (1) the relationship between the endocrine actions of antiandrogens and their therapeutic efficacy and (2) recent chemical and pharmacokinetic data on cyproterone acetate (CPA). It also provides (3) a comparison of CPA and spironolactone regarding the tentative benefits and risks and offers (4) general rules for the drug treatment of androgenized women. Clinical results indicate that those agents are most effective which not only competitively inhibit androgen binding at the receptor level but also suppress androgen secretion and/or production. The combined mode of action is observed with CPA as well as spironolactone. Pharmacokinetic studies underline the necessity to restrict CPA administration in huge doses to the first half of a treatment cycle in order to avoid bleeding disturbances. Also it appears that individual differences in CPA bioavailability do not satisfactorily explain the lack of therapeutic response in about 30% of the cases. Data are presented hinting that the 15 beta-hydroxy-, metabolite of CPA may actually be the biologically active agent. In addition preliminary results are given indicating that intramuscular CPA is therapeutically more effective than oral CPA.