Göretzlehner G, Köhler G
Klinik und Poliklinik für Gynäkologie und Geburtshilfe, Bereichs Medizin der Ernst-Moritz-Arndt-Universität Greifswald.
Zentralbl Gynakol. 1988;110(12):766-71.
In a survey it is reported on the antiprogestins mifepristone (RU 486) and gestrinone (R 2323). Thanks to its high reversible affinity for progesterone receptor mifepristone stops progesterone activity at its target organs. Mifepristone also inhibits ovarian progesterone synthesis. This antiprogesterone was tested clinically with different results for following indications: postcoital contraception, luteolysis, early abortion, ectopic pregnancy, missed abortion, cervix priming, and breast cancer. Gestrinone has antiestrogenic, antiprogesterone, and weak androgenic properties. These effects are related to the affinity for estrogene-, progesterone- and androgene receptor. A suppressory action on gonadotropins has been observed in therapeutic dosages. On the basis of its properties gestrinone is used for treatment of endometriosis, leiomyomas, benign breast diseases and also for contraception.
一项调查报道了抗孕激素米非司酮（RU 486）和孕三烯酮（R 2323）。由于米非司酮对孕激素受体具有高度可逆亲和力，它能在靶器官阻断孕激素活性。米非司酮还能抑制卵巢孕激素的合成。这种抗孕激素针对以下适应症进行了临床测试，结果各异：性交后避孕、黄体溶解、早期流产、异位妊娠、稽留流产、宫颈准备和乳腺癌。孕三烯酮具有抗雌激素、抗孕激素和弱雄激素特性。这些作用与对雌激素、孕激素和雄激素受体的亲和力有关。在治疗剂量下已观察到对促性腺激素的抑制作用。基于其特性，孕三烯酮用于治疗子宫内膜异位症、平滑肌瘤、良性乳腺疾病以及避孕。
