Departments of Obstetrics and Gynecology and Preventive Medicine, University of Southern California Keck School of Medicine, Los Angeles, CA 90033, USA.
Contraception. 2013 Jun;87(6):706-27. doi: 10.1016/j.contraception.2012.12.011. Epub 2013 Jan 8.
The need to seek improved combined oral contraceptive (COC) efficacy, with fewer health risks and better acceptability, has been ongoing since the introduction of COCs more than 50 years ago. New progestin formulations combined with lower doses of ethinyl estradiol (EE), the predominant estrogenic component of COCs, have reduced the incidence of venous thromboembolism and other negative outcomes of COC treatment. Previous attempts to use endogenous 17β-estradiol (E₂) instead of EE were limited primarily by poor cycle control. The recent introduction of E₂-based formulations has renewed interest to determine if there are potential benefits of using E₂ in COCs. These formulations have been shown to have similar efficacy and cycle control as EE-based COCs. This review provides a brief summary of the pharmacology of EE and E₂, including metabolism, pharmacokinetics and pharmacodynamics, as well as adverse effects of these estrogens.
自 50 多年前口服避孕药问世以来，人们一直需要寻求具有更好疗效、更少健康风险和更好接受度的新型复方口服避孕药。新型孕激素与低剂量的炔雌醇（COC 中主要的雌激素成分）结合使用，降低了静脉血栓栓塞和其他 COC 治疗不良结局的发生率。以前尝试使用内源性 17β-雌二醇（E₂）替代 EE 主要受到较差的周期控制的限制。最近 E₂ 为基础的制剂的引入重新激发了人们的兴趣，以确定在 COC 中使用 E₂ 是否具有潜在的益处。这些制剂已被证明与 EE 为基础的 COC 具有相似的疗效和周期控制。本文简要综述了 EE 和 E₂ 的药理学特性，包括代谢、药代动力学和药效学，以及这些雌激素的不良反应。
