Pharmacology and Toxicology, University of California, Davis, Suite 3016, Sacramento, CA 95817, USA.
Expert Opin Drug Metab Toxicol. 2010 Jun;6(6):773-9. doi: 10.1517/17425255.2010.487483.
Millions of women worldwide suffer from vulvovaginal atrophy (VVA) associated with menopause, and many women report that this adversely affects their quality of life. Ospemifene is a non-hormonal estrogen receptor agonist/antagonist effective in the treatment of VVA. Although similar in structure to other estrogen receptor agonists/antagonists that have antagonistic effects on the vagina, ospemifene has an estrogen-like effect on vaginal epithelium. This review focuses on ospemifene including its pharmacologic properties, clinical efficacy and safety.
The paper provides information on the phamacodynamic and pharmacokinetic properties of ospemifene. It also contains an overview of its preclinical and clinical efficacy as well as its clinical safety.
From this paper, the reader will gain an appreciation for a new non-hormonal estrogen receptor agonist/antagonist, ospemifene.
The pharmacologic properties of ospemifene make it a logical candidate for the treatment of women with moderate to severe symptoms of VVA associated with menopause. Clinical trials have confirmed that daily doses are well-tolerated and that it is effective in normalizing vaginal maturation index and pH as well as improving the symptoms associated with VVA including dyspareunia.
全世界数以百万计的妇女患有与绝经相关的外阴阴道萎缩(VVA),许多妇女报告说这对她们的生活质量有不利影响。奥昔布芬是一种非激素雌激素受体激动剂/拮抗剂,可有效治疗 VVA。尽管奥昔布芬在结构上与其他对阴道具有拮抗作用的雌激素受体激动剂/拮抗剂相似,但它对阴道上皮具有雌激素样作用。本综述重点介绍奥昔布芬,包括其药理学特性、临床疗效和安全性。
本文提供了奥昔布芬的药效学和药代动力学特性信息。它还概述了其在临床前和临床中的疗效以及临床安全性。
读者将从本文中了解到一种新的非激素雌激素受体激动剂/拮抗剂,奥昔布芬。
奥昔布芬的药理学特性使其成为治疗与绝经相关的中度至重度 VVA 症状的合理候选药物。临床试验证实,每日剂量可耐受良好,并且有效使阴道成熟指数和 pH 值正常化,改善与 VVA 相关的症状,包括性交困难。