Benagiano Giuseppe, Bastianelli Carlo, Farris Manuela, Brosens Ivo
University of Rome, 'Sapienza', Department of Gynaecology, Obstetrics and Urology , C/O AIED Via Toscana 30, 00187 Rome , Italy
Expert Opin Pharmacother. 2014 Jul;15(10):1403-15. doi: 10.1517/14656566.2014.914494. Epub 2014 Apr 30.
Several selective progesterone receptor modulators (SPRMs) show promise in several areas of medicine and this work has been summarized by us in 2008.
Since the publication of our reviews, several developments have taken place in the field of reproductive medicine. The first is emergency contraception (EC). Two SPRMs are clinically utilized today: mifepristone (MFP) and ulipristal acetate (UPA). MFP is available for EC in up to 120 h following unprotected intercourse. A dose of 10 mg is significantly more effective than levonorgestrel (LNG). In a metanalysis of the use of UPA versus LNG up to 72 h after unprotected intercourse, failure rates of 1.4 versus 2.2% were reported. The second is contraception. A daily dose of 2 mg MFP can block ovulation and several MFP regimens are being tested, including a vaginal ring releasing MFP. The third is the preoperative administration in women harboring leiomyomas, where clinical testing of several SPRM has shown that they can decrease uterine leiomyomas' size and substantially reduce uterine bleeding. SPRM can induce unusual, specific endometrial appearances. Many believe that these changes should not cause concern, but the issue remains controversial.
SPRMs are very effective in EC and for the preoperative treatment of uterine leiomyomas.
几种选择性孕激素受体调节剂（SPRM）在多个医学领域显示出前景，我们已在2008年对这项工作进行了总结。
自我们的综述发表以来，生殖医学领域发生了多项进展。首先是紧急避孕（EC）。如今有两种SPRM在临床上得到应用：米非司酮（MFP）和醋酸乌利司他（UPA）。MFP可在无保护性交后长达120小时用于紧急避孕。10毫克剂量的MFP比左炔诺孕酮（LNG）显著更有效。在一项对无保护性交后长达72小时使用UPA与LNG的荟萃分析中，报告的失败率分别为1.4%和2.2%。其次是避孕。每日2毫克剂量的MFP可抑制排卵，并且正在测试几种MFP给药方案，包括释放MFP的阴道环。第三是对患有平滑肌瘤的女性进行术前给药，多项SPRM的临床试验表明它们可减小子宫平滑肌瘤的大小并大幅减少子宫出血。SPRM可诱发不寻常的、特定的子宫内膜表现。许多人认为这些变化无需担忧，但该问题仍存在争议。
SPRM在紧急避孕和子宫平滑肌瘤的术前治疗中非常有效。
