新的孕激素:回顾在准更年期和绝经后妇女的影响。
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Sitruk-Ware R
新的孕激素:回顾在准更年期和绝经后妇女的影响。
衰老药物。2004;21 (13):865 - 83。
- PubMed ID
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15493951 (在PubMed]
- 文摘
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黄体酮有不同的药理特性取决于父分子,通常睾丸激素和孕激素,它们是派生的。非常小的结构性变化在父分子可能在导数的活动产生相当大的差异。与一个完整的绝经后妇女子宫,黄体酮与雌激素结合使用激素替代疗法(HRT)。开发新一代又一代的黄体酮与改善选择性配置文件是一个巨大的挑战。甾体和非甾体类孕激素受体(PR)受体激动剂已被合成,尽管后者仍在开发的早期阶段。一些新的孕酮,合成在过去2年,可能被认为是第四代黄体酮。屈,这些包括dienogest Nestorone(人口理事会,纽约,纽约,美国),醋酸nomegestrol trimegestone。第四代黄体酮设计没有雄性或雌激素行动和活动的生理激素孕酮。其不同于经典的黄体酮是来自spirolactone。它本质上是一个antimineralocorticoid类固醇但部分antiandrogenic效果没有雄激素的影响。 The antiovulatory potency of the different progestins varies. Trimegestone and Nestorone are the most potent progestins synthesised to date, followed by two of the older progestins, 3-keto-desogestrel and levonorgestrel. The new molecules trimegestone, drospirenone and dienogest also have antiandrogenic activity. Following the publication of the results of the Women's Health Initiative study, the role of progestins in HRT became controversial. Unfortunately, this concern has been directed towards progestins as a class, although striking differences exist among the progestins. Natural progesterone and some of its derivatives, such as the 19-norprogesterone molecules, and the new molecules drospirenone and dienogest are not androgenic and, therefore, have no negative effect on the lipid profile. The effects of progestins on breast tissue remain controversial as well. However, depending on the progestin and the duration of application, breast cell differentiation and apoptosis may predominate over proliferation. It is still unclear if the currently available progestins are able to bind specifically to the PR isoforms PR-A or PR-B and whether this is of clinical relevance to breast cell proliferation is also unclear. Although it is likely that the new progestins may have neutral effects on the risk of coronary heart disease or breast cancer in younger postmenopausal women, this hypothesis must be confirmed in large randomised, well controlled clinical trials.