Department of Pharmacotherapy & Translational Research, College of Pharmacy, University of Florida, Gainesville, FL, USA.
Ann Pharmacother. 2011 Oct;45(10):1256-61. doi: 10.1345/aph.1Q216. Epub 2011 Sep 13.
To review the pharmacology, pharmacokinetics, efficacy, and safety of the new oral contraceptive estradiol valerate/dienogest.
Searches of PubMed (1966-July 2011) and International Pharmaceutical Abstracts (1970-July 2011) were conducted using the key words estradiol valerate, dienogest, Natazia, and Qlaira. Bibliographies of retrieved articles were reviewed to identify additional references.
All identified studies published in English and involving efficacy and safety of estradiol valerate/dienogest as an oral contraceptive were reviewed.
Estradiol valerate/dienogest is a 4-phasic oral contraceptive approved for the prevention of pregnancy. The 4-phasic design allows for acceptable cycle control with this hormonal combination. In efficacy trials of estradiol valerate/dienogest in women aged 18-35 years, the Pearl Index ranged from 0.40 to 1.64, a range comparable to that of other combination oral contraceptives. The safety profile was also similar to that of other oral contraceptives, with headache, metrorrhagia, breast tenderness, nausea or vomiting, acne, and weight gain reported as the most common adverse effects. Menstrual bleeding patterns and cycle control with estradiol valerate/dienogest were comparable to those of a monophasic oral contraceptive containing ethinyl estradiol/levonorgestrel. Estradiol valerate/dienogest differs from other oral contraceptives in that it necessitates more stringent dosing guidelines for maximum contraceptive efficacy. New starts should be on the first day of menses only, and a back-up method of contraception is required for the first 9 days, as compared to 7 days with other oral contraceptives. Back-up contraception is usually required for any pill taken more than 12 hours later than scheduled.
Estradiol valerate/dienogest is an effective oral contraceptive. Because it has more stringent start times and requires a longer duration of backup contraception and stricter adherence, estradiol valerate/dienogest should be reserved for patients who are intolerant of other combination oral contraceptives.
综述新型口服避孕药雌二醇戊酸酯/地诺孕素的药理学、药代动力学、疗效和安全性。
检索 PubMed（1966 年-2011 年 7 月）和国际药学文摘（1970 年-2011 年 7 月），使用关键词雌二醇戊酸酯、地诺孕素、Natazia 和 Qlaira。检索文章的参考文献也进行了回顾，以确定其他参考文献。
所有以英文发表并涉及雌二醇戊酸酯/地诺孕素作为口服避孕药的疗效和安全性的已识别研究均进行了回顾。
雌二醇戊酸酯/地诺孕素是一种 4 相口服避孕药，用于预防妊娠。这种 4 相设计允许这种激素组合具有可接受的周期控制。在 18-35 岁女性中进行的雌二醇戊酸酯/地诺孕素疗效试验中，珍珠指数范围为 0.40 至 1.64，与其他复方口服避孕药的范围相当。安全性概况也与其他口服避孕药相似，报告的最常见不良反应包括头痛、突破性出血、乳房触痛、恶心或呕吐、痤疮和体重增加。雌二醇戊酸酯/地诺孕素的月经出血模式和周期控制与含有炔雌醇/左炔诺孕酮的单相口服避孕药相似。雌二醇戊酸酯/地诺孕素与其他口服避孕药的不同之处在于，为了达到最大避孕效果，需要更严格的剂量指南。新开始只能在月经的第一天，并且在前 9 天需要备用避孕方法，而其他口服避孕药只需 7 天。与其他口服避孕药相比，任何超过计划时间 12 小时以上的药物都需要备用避孕方法。
雌二醇戊酸酯/地诺孕素是一种有效的口服避孕药。由于其起始时间更严格，需要更长时间的备用避孕方法和更严格的坚持，因此雌二醇戊酸酯/地诺孕素应保留给不能耐受其他复方口服避孕药的患者。
