What is Which of the following is anti-androgenic drug? and explain in detail?
Ans. a (Bicalutamide). (Ref. Bailey and Love 25th/108)BICALUTAMIDE# is an anti-androgenic drug used in prostatic cancer therapy for medical castration.# The addition of actual antagonists of androgens acting at the androgen receptor, including flutamide or bicalutamide, is of uncertain additional benefit in extending overall response duration, but it clearly prevents the activation of androgen receptors by adrenal androgens, and the combined use of orchiectomy or leuprolide plus flutamide is referred to as "total androgen blockade."# Other hormones that may be active include estrogens, progestins, ketoconazole, and glucocorticoids.TamoxifenBlocks oestrogen receptorsBreast cancerAnastrazoleAn aromatase inhibitor that blocks post-menopausal (non- ovarian) oestrogen productionBreast cancerExemestaneAn aromatase inhibitor that blocks post-menopausal (non- ovarian) oestrogen productionBreast cancerLetrozoleAn aromatase inhibitor that blocks post-menopausal (non- ovarian) oestrogen productionBreast cancerLeuprolideAnalogue of gonadotrophin-releasing hormone; continued use produces downregulation of the anterior pituitary with a consequent fall in testosterone levelsProstate cancerGoserilinAnalogue of gonadotrophin-releasing hormone; continued use produces downregulation of the anterior pituitary with a consequent fall in testosterone levelsProstate cancerBuserelinAnalogue of gonadotrophin-releasing hormone; continued use produces downregulation of the anterior pituitary with a consequent fall in testosterone levelsProstate cancerCabergolineBlocks prolactin release, a long-acting dopamine agonistProlactin-secreting pituitary tumorBromocriptineDopamine agonist, blocks stimulation of the anterior pituitaryPituitary tumoursCyproterone acetateBlocks the effect of androgensProstate cancerFlutamideBlocks the effect of androgensProstate cancerNilutamideBlocks the effect of androgensProstate cancerBicalutamideBlocks the effect of androgensProstate cancerEducational Points:# Prostate cancer is classically treated by diethylstilbesterol (DES) acting as an estrogen at the level of the hypothalamus to down-regulate hypothalamic LH production, resulting in decreased elaboration of testosterone by the testicle. For this reason, orchiectomy is equally as effective as moderate-dose DES.# In the event that orchiectomy is not accepted by the patient, testicular androgen suppression can also be effected by luteinizing hormone-releasing hormone (LHRH) agonists such as leuprolide and goserelin.# Primary hormonal manipulation in prostate cancer one can choose orchiectomy or leuprolide, not both.