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孕酮拮抗剂及新型选择性孕酮受体调节剂在生殖健康中的作用

Role of progesterone antagonists and new selective progesterone receptor modulators in reproductive health.

作者信息

Olive David L

机构信息

Department of Obstetrics and Gynecology, Division of Reproductive Endocrinology and Infertility, University of Wisconsin-Madison Medical School, 53792, USA.

出版信息

Obstet Gynecol Surv. 2002 Nov;57(11 Suppl 4):S55-63. doi: 10.1097/00006254-200211004-00001.

Abstract

UNLABELLED

Given the importance of progesterone in female reproductive health, it was inevitable that analogues of this molecule would be developed to treat a variety of gynecologic maladies. Such medications, termed progesterone antagonists, act to counteract the effect of progesterone. A newer class of molecules, the selective progesterone receptor modulators (SPRMs), have both agonist and antagonist activities depending upon the site of action. These compounds have been studied for their effect on endometrial growth, endometrial vascular development, the hypothalmic-pituitary-ovarian axis and cervical integrity. Such research has led to a number of potential clinical applications. Progesterone antagonists are well established in their use for termination of pregnancy, although SPRMs seem to have a diminished capacity for induction of abortion. Similarly, antagonists work well to soften and dilate the cervix before surgery, but such efficacy by SPRMs is unlikely. Other applications for progesterone antagonists include induction of labor, the treatment of endometriosis, fibroids and contraception; SPRMs also may prove useful in the treatment of endometriosis and fibroids, as well as for postmenopausal hormone replacement therapy and the treatment of dysfunctional uterine bleeding. Finally, these compounds may aid investigators in unraveling many of the nuances of the role of progesterone in reproductive function.

TARGET AUDIENCE

Obstetricians & Gynecologists, Family Physicians Learning Objectives: After completion of this article, the reader will be able to describe the receptor action and selective modulation of progesterone, explain the effects of progesterone receptor modulators, and list the potential clinical applications of progesterone antagonists and selective progesterone receptor modulators.

摘要

未标注

鉴于孕酮在女性生殖健康中的重要性,开发该分子的类似物以治疗各种妇科疾病是不可避免的。这类药物被称为孕酮拮抗剂,其作用是抵消孕酮的作用。一类较新的分子,即选择性孕酮受体调节剂(SPRMs),根据作用部位具有激动剂和拮抗剂两种活性。已经研究了这些化合物对子宫内膜生长、子宫内膜血管发育、下丘脑 - 垂体 - 卵巢轴和宫颈完整性的影响。此类研究已带来一些潜在的临床应用。孕酮拮抗剂在用于终止妊娠方面已得到充分确立,尽管SPRMs诱导流产的能力似乎有所减弱。同样,拮抗剂在手术前软化和扩张宫颈方面效果良好,但SPRMs不太可能有此功效。孕酮拮抗剂的其他应用包括引产、治疗子宫内膜异位症、子宫肌瘤和避孕;SPRMs在治疗子宫内膜异位症和子宫肌瘤以及绝经后激素替代疗法和功能失调性子宫出血方面也可能证明是有用的。最后,这些化合物可能有助于研究人员阐明孕酮在生殖功能中的许多细微作用。

目标受众

妇产科医生、家庭医生

学习目标

读完本文后,读者将能够描述孕酮的受体作用和选择性调节,解释孕酮受体调节剂的作用,并列出孕酮拮抗剂和选择性孕酮受体调节剂的潜在临床应用。

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