ABSTRACT
This chapter presents classification & mode of action, indications & dermatological uses, formulations/presentation, dosages & suggested regimens, baseline investigations, considerations & monitoring, contraindications, cautions, important drug interactions, adverse effects & their management, use in special situations, and essential patient information of Antiandrogens. Antiandrogens are a group of drugs that block the action of androgens by two broad mechanisms: competitive inhibition of binding of androgens, and inhibition of the enzyme 5α-reductase that converts testosterone to dihydrotestosterone (DHT). Bicalutamide is a newer and potent antiandrogen with similar mechanism of action. Cyproterone acetate was the first antiandrogen in clinical use and was introduced 1964. Cimetidine has weak antiandrogenic effects due to competitive inhibition of DHT at peripheral androgen receptors. All antiandrogens are contraindicated in pregnancy. Antiandrogens are contraindicated during pregnancy due to the risk of feminization of the male fetus. Antiandrogens are contraindicated during breastfeeding.
