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当月药物。一种含戊酸雌二醇和地诺孕素的新型复方口服避孕药(炔雌醇环丙孕酮片)

[Medication of the month. A new combined oral contraceptive containing estradiol valerate and dienogest (Qlaira)].

作者信息

Gaspard U, Pintiaux A, Kridelka F

机构信息

Service universitaire de Gynécologie Obstétrique CHR Citadelle, Liège, Belgique.

出版信息

Rev Med Liege. 2010 Dec;65(12):706-13.

PMID:21287768
Abstract

In combined oral contraception (OC), a drastic reduction of both ethinylestradiol and androgenic progestins mostly derived from 19 NOR testosterone, allowed to moderately reduce the adverse impact of classical combined pills on metabolism and circulation (both arterial and venous). However, the marked hepatic action of ethinylestradiol, even in small dosages, lessens the expected risk reduction. For the first time, an OC has been developed, which contains estradiol valerate (with reduced hepatic action because of lack of a 17alpha ethinyl group) with dienogest, a 19 NOR testosterone-derived nonandrogenic progestin, which powerfully inhibits endometrial proliferation. Thanks to a dynamic modulation of estrogen and progestin doses (26 active days + 2 placebo days), an adequate contraceptive effectiveness, a good cycle control and drug tolerance are achieved, similar to those obtained with a classical low-dose OC. Recent data indicate that this new combination reduces the usually observed metabolic impact. An adequate cycle control (with 20% amenorrhea) is achieved for the first time with estradiol valerate + progestin,, in opposition with prior catastrophic results with other formulations containing 17beta-estradiol. A second combination containing estradiol + nomegestrol acetate (monophasic, 24 active days + 4 placebo days) is under study and seems also to yield promising results. Of course, in-depth study of metabolic and vascular effects of these new combinations is mandatory - and ongoing.

摘要

在复方口服避孕药(OC)中,乙炔雌二醇和大多源自19-去甲睾酮的雄激素类孕激素的大幅减少,使得传统复方避孕药对代谢和循环(动脉和静脉)的不良影响得到适度降低。然而,乙炔雌二醇即使小剂量也具有明显的肝脏作用,这削弱了预期的风险降低效果。首次研发出一种OC,它含有戊酸雌二醇(由于缺乏17α-乙炔基,肝脏作用减弱)和地诺孕素,地诺孕素是一种源自19-去甲睾酮的非雄激素类孕激素,能有效抑制子宫内膜增殖。由于雌激素和孕激素剂量的动态调节(26个活性日 + 2个安慰剂日),实现了足够的避孕效果、良好的周期控制和药物耐受性,与传统低剂量OC的效果相似。近期数据表明,这种新组合降低了通常观察到的代谢影响。戊酸雌二醇 + 孕激素首次实现了足够的周期控制(闭经率为20%),这与其他含17β-雌二醇制剂先前灾难性的结果相反。第二种组合,即雌二醇 + 醋酸诺美孕酮(单相,24个活性日 + 4个安慰剂日)正在研究中,似乎也产生了有前景的结果。当然,对这些新组合的代谢和血管效应进行深入研究是必不可少的,并且正在进行中。

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Rev Med Liege. 2010 Dec;65(12):706-13.
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