Trémollieres F
Centre de ménopause, hôpital Paule de Viguier, 330, avenue de Grande-Bretagne, TSA 70034, 31059 Toulouse cedex 9, France.
Gynecol Obstet Fertil. 2012 Feb;40(2):109-15. doi: 10.1016/j.gyobfe.2011.10.009. Epub 2012 Jan 12.
Estradiol 17-β, which is the natural estrogen in women, offers an alternative to ethinyl-estradiol to be used in combined oral contraceptives. Thanks to its biochemical structure, estradiol has a far lesser impact on the synthesis of hepatic proteins than ethinyl-estradiol, which is likely to result in a better metabolic and vascular profile. However and until lately, the different clinical trials that had investigated estradiol-containing oral contraceptives were limited by bleeding disturbances, with breakthrough and irregular bleeding and higher rates of discontinuation. Development of anti-gonadotropic progestins with a potent endometrial activity is likely to make possible their combination with estradiol in oral contraceptives. The objective of this current review is to provide an overview of the development of combined oral contraceptives containing natural estrogen from the respective biochemical and pharmacological characteristics of ethinyl-estradiol and estradiol.
17-β-雌二醇是女性体内的天然雌激素，可作为乙炔雌二醇的替代品用于复方口服避孕药。由于其生化结构，与乙炔雌二醇相比，雌二醇对肝脏蛋白质合成的影响要小得多，这可能会带来更好的代谢和血管状况。然而，直到最近，研究含雌二醇口服避孕药的不同临床试验都受到出血紊乱的限制，出现突破性出血和不规则出血，停药率也较高。具有强效子宫内膜活性的抗促性腺孕激素的开发可能会使其与雌二醇联合用于口服避孕药成为可能。本综述的目的是从乙炔雌二醇和雌二醇各自的生化和药理学特性出发，概述含天然雌激素复方口服避孕药的发展情况。
