经皮激素避孕研究进展:以炔雌醇/去甲孕酮避孕贴片为重点。

Alessandra Graziottin
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引用次数: 13

摘要

使用不完善的避孕方法明显增加了怀孕的可能性。提高激素避孕依从性的一种方法是尽量减少给药计划。目前有两种形式的激素避孕达到了这个目的:透皮贴片和阴道环。第一个也是唯一一个获得全球监管机构批准的透皮避孕贴片(炔雌醇/去甲孕酮)是一种方便的避孕方法,具有与口服避孕药(OCs)相似的功效,但每周给药一次的好处。此外,经皮给药避孕激素消除了胃肠道吸收的变异性,避免了肝脏第一次代谢,并防止了OCs所见的血清浓度的波峰和波谷。去甲孕酮,即贴片中所含的黄体酮,是去甲睾酮的活性代谢物,在结构上与去甲睾酮19相关。去甲孕酮和去甲孕酮模拟孕激素对孕激素受体的生理作用;然而,去甲孕酮的直接或间接雄激素活性可忽略不计,这表明它可能适用于与雄激素过量相关的疾病(如多毛症、痤疮和脂质紊乱)的女性。避孕效果通常是一种避孕药具的功效与对其给药方案的依从性的函数。避孕贴片的有效性在三个III期试验中得到了明确的证明,其中两个是与OC随机比较的。这些避孕方法之间的怀孕可能性相似;然而,贴片的依从性明显更好,特别是在年轻女性中。该贴片的安全性和耐受性与OC相似。一项成本效益分析表明,避孕贴片比普通避孕贴片更具成本效益,因为与意外怀孕相关的成本降低了。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch.

Imperfect use of contraceptive methods notably increases the likelihood of pregnancy. One means of improving user adherence with hormonal contraception is to minimize the dosing schedule. Two forms of hormonal contraceptive have currently achieved this goal: the transdermal patch and the vaginal ring. The first and only transdermal contraceptive patch to receive worldwide regulatory approval (ethinylestradiol/norelgestromin) is a convenient approach to contraception that has a similar efficacy to oral contraceptives (OCs), but with the benefit of once-weekly administration. In addition, transdermal delivery of contraceptive hormones eliminates variability in gastrointestinal absorption, avoids hepatic first-pass metabolism, and prevents the peaks and troughs in serum concentrations that are seen with OCs. Norelgestromin, the progestin contained in the patch, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor; however, norelgestromin has negligible direct or indirect androgenic activity, suggesting that it may be suitable for women with disorders related to androgen excess (such as hirsutism, acne, and lipid disorders).Contraceptive effectiveness is usually a function of the efficacy of a contraceptive in combination with compliance with its dosing regimen. The efficacy of the contraceptive patch has been clearly demonstrated in three phase III trials, two of which were randomized comparisons with an OC. The likelihood of pregnancy was similar between these contraceptive methods; however, compliance with the patch was notably better, particularly in younger women. The safety and tolerability profile of the patch was similar to that of the OC. A cost-effectiveness analysis has suggested that the contraceptive patch is more cost effective than the OC, due to decreased costs related to unwanted pregnancy.

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