Caring For Women Wellness Center, Davis, CA 95616, USA.
J Womens Health (Larchmt). 2012 Feb;21(2):161-9. doi: 10.1089/jwh.2011.2839. Epub 2011 Oct 19.
To compare oral and transdermal delivery systems in domains of lipid effects; cardiovascular, inflammatory, and thrombotic effects; effect on insulin-like growth factor, insulin resistance, and metabolic syndrome; sexual effects; metabolic effects including weight; and effects on target organs bone, breast, and uterus.
Review of the literature 1990-2010. Studies selected on basis of applicability, quality of data, and relationship to topic.
Data applicable to the comparisons of oral versus transdermal delivery systems for postmenopausal estrogen therapy were utilized to perform a review and formulate conclusions.
Significant differences appear to exist between oral and transdermal estrogens in terms of hormonal bioavailability and metabolism, with implications for clinical efficacy, potential side effects, and risk profile of different hormone therapy options, but neither results nor study designs are uniform. Bypassing hepatic metabolism appears to result in more stable serum estradiol levels without supraphysiologic concentrations in the liver. By avoiding first-pass metabolism, transdermal hormone therapy may have less pronounced effects on hepatic protein synthesis, such as inflammatory markers, markers of coagulation and fibrinolysis, and steroid binding proteins, while oral hormone therapy has more pronounced hyper-coagulant effects and increases synthesis of C-reactive protein and fibrinolytic markers. Both oral and transdermal delivery systems have beneficial effects on high-density lipoprotein cholesterol to low-density lipoprotein cholesterol ratios (oral>transdermal), while the transdermal system has more favorable effects on triglycerides. Incidence of metabolic syndrome and weight gain appears to be slightly lower with a transdermal delivery system. Oral estrogen's significant increase in hepatic sex hormone binding globulin production lowers testosterone availability compared with transdermal delivery, with clinically relevant effects on sexual vigor.
比较口服和透皮给药系统在脂质作用、心血管、炎症和血栓形成作用、对胰岛素样生长因子、胰岛素抵抗和代谢综合征的影响、性作用、包括体重的代谢作用以及对目标器官骨骼、乳房和子宫的影响等方面。
对 1990 年至 2010 年的文献进行综述。根据适用性、数据质量和与主题的关系选择研究。
利用适用于绝经后雌激素治疗的口服与透皮给药系统比较的数据，进行了综述并得出结论。
口服和透皮雌激素在激素生物利用度和代谢方面似乎存在显著差异，这对临床疗效、潜在副作用和不同激素治疗选择的风险状况有影响，但结果和研究设计并不统一。绕过肝脏代谢似乎会导致更稳定的血清雌二醇水平，而肝脏中没有超生理浓度。通过避免首过代谢，透皮激素治疗可能对肝脏蛋白合成（如炎症标志物、凝血和纤维蛋白溶解标志物以及甾体结合蛋白）的影响较小，而口服激素治疗的促凝作用更明显，并增加 C 反应蛋白和纤维蛋白溶解标志物的合成。口服和透皮给药系统都对高密度脂蛋白胆固醇与低密度脂蛋白胆固醇的比值有有益影响（口服>透皮），而透皮系统对甘油三酯的影响更有利。与口服给药系统相比，透皮给药系统的代谢综合征和体重增加的发生率似乎略低。口服雌激素显著增加肝脏性激素结合球蛋白的产生，降低了与透皮给药相比的睾酮可用性，对性活力有临床相关影响。
