Kakade Aniket S, Kulkarni Yashwant S
J Indian Med Assoc. 2014 Jan;112(1):36-40.
The first clinically available antiprogestin, mifepristone has generated immense interest in the research community since its' discovery in 1980. Mifepristone is a synthetic orally active steroid with potent antiglucocorticoid, antiprogestogen and a weak anti-androgen activity, used primarily for termination of pregnancy. It acts as a competitive receptor antagonist at the progesterone receptor in the presence of progesterone, and acts as a partial agonist in the absence of progesterone. Extensive research has been carried out regarding its' antiprogestogen activity for use in medical abortion. Lately other medical uses of mifepristone are being explored like for induction of labour in late preg- nancy, as oestrogen free oral contraceptive and for treatment of endometriosis, uterine fibroids, ovarian cancer, prostate cancer, meningiomas, Cushing's syndrome and major psychotic depression.
米非司酮是首个可供临床使用的抗孕激素药物,自1980年被发现以来,它在研究界引起了极大的关注。米非司酮是一种合成的口服活性甾体,具有强大的抗糖皮质激素、抗孕激素和微弱的抗雄激素活性,主要用于终止妊娠。在有孕酮存在时,它作为孕酮受体的竞争性拮抗剂起作用,而在无孕酮时则作为部分激动剂起作用。关于其在药物流产中的抗孕激素活性已进行了广泛研究。最近,米非司酮的其他医学用途也在探索中,如用于晚期妊娠引产、作为无雌激素口服避孕药以及用于治疗子宫内膜异位症、子宫肌瘤、卵巢癌、前列腺癌、脑膜瘤、库欣综合征和重度精神病性抑郁症。