Akakura K, Furuya Y, Ito H
Department of Urology, Chiba University School of Medicine.
Nihon Rinsho. 1998 Aug;56(8):2124-8.
Antiandrogens are defined as substances which prevent androgens from expressing their activity at target sites. Based on their chemical structures, antiandrogens are divided into steroidal and nonsteroidal antiandrogens. In addition to antiandrogenic action, steroidal antiandrogens simulate the negative feedback inhibition of the hypothalamus, resulting in lowering the concentration of plasma testosterone. On the other hand, in nonsteroidal antiandrogens, the androgenic actions are blocked in both hypothalamus and target tissues. Therefore, negative feedback signals are inhibited and production of testosterone is increased in the testis. For the endocrine therapy of prostate cancer, chlormadinone acetate, flutamide and bicalutamide are or will be available in Japan. Antiandrogen is generally used by the combination with surgical or medical castration, namely as total androgen blockade.
抗雄激素被定义为阻止雄激素在靶位点发挥其活性的物质。根据其化学结构，抗雄激素可分为甾体类抗雄激素和非甾体类抗雄激素。除了抗雄激素作用外，甾体类抗雄激素还模拟下丘脑的负反馈抑制，导致血浆睾酮浓度降低。另一方面，在非甾体类抗雄激素中，下丘脑和靶组织中的雄激素作用均被阻断。因此，负反馈信号受到抑制，睾丸中睾酮的产生增加。对于前列腺癌的内分泌治疗，醋酸氯地孕酮、氟他胺和比卡鲁胺在日本已经或即将上市。抗雄激素通常与手术去势或药物去势联合使用，即作为全雄激素阻断。
