Baird D T
University of Edinburgh, Department of Obstetrics and Gynaecology, UK.
Br Med Bull. 1993 Jan;49(1):73-87. doi: 10.1093/oxfordjournals.bmb.a072607.
Antigestogens are compounds which inhibit the synthesis of progesterone or antagonise its biological action. The progesterone antagonist mifepristone (RU 486) binds with high affinity to progesterone receptors throughout the body, blocking the action of endogenous progesterone. In the last 10 years it has been demonstrated that mifepristone, in combination with a suitable prostaglandin, is a safe, effective alternative to vacuum aspiration for termination of pregnancy in the first two months. Preliminary trials suggest that antigestogens may be useful true contraceptives by inhibiting ovulation or by preventing implantation as once a month pills and postcoital agents. In late pregnancy, by sensitising the uterus to prostaglandins and by promoting cervical dilatation, they may induce labour and facilitate lactation. In non-pregnant women mifepristone may have application in the treatment of hormone-dependent conditions such as endometriosis, fibromyomata, meningioma and breast cancer. The availability of hormone antagonists to oestrogens, androgens and progesterone offers the possibility of new methods of regulating reproductive function in health and disease.
抗孕激素是抑制孕酮合成或拮抗其生物学作用的化合物。孕酮拮抗剂米非司酮（RU 486）与全身的孕酮受体具有高亲和力结合，阻断内源性孕酮的作用。在过去10年中，已证明米非司酮与合适的前列腺素联合使用，对于头两个月终止妊娠而言，是一种安全、有效的替代真空抽吸的方法。初步试验表明，抗孕激素通过抑制排卵或作为每月一次的药丸及性交后用药来防止着床，可能成为有效的真正避孕药。在妊娠晚期，通过使子宫对前列腺素敏感并促进宫颈扩张，它们可能诱发分娩并促进泌乳。在未怀孕的女性中，米非司酮可能应用于治疗诸如子宫内膜异位症、纤维瘤、脑膜瘤和乳腺癌等激素依赖性疾病。雌激素、雄激素和孕酮的激素拮抗剂的可得性为在健康和疾病中调节生殖功能的新方法提供了可能性。
