健康的绝经前女性志愿者中单剂量或多剂量阿那司唑的药物代谢动力学、药效学及安全性的I期研究  

A phase I study of the pharmacokinetics, pharmacodynamics, and safety of single-and multiple-dose anastrozole in healthy, premenopausal female volunteers

作　　者：Tredway D.R Buraglio M Hemsey G Denton G. 王雅楠 

出　　处：《世界核心医学期刊文摘（妇产科学分册）》2005年第5期32-32,共1页Core Journal in Obstetrics/Gynecology

摘　　要：To evaluate the pharmacokinetic, pharmacodynamic, and safety profiles of the a romatase inhibitor anastrozole in healthy, premenopausal women. Phase I, single -center study. Infertility clinic. Twenty-six women with regular ovulatory cyc les: 20 received either a single dose of 5 mg, 10 mg, 15 mg, or 20 mg anastrozol e, or remained untreated; 6 received five daily doses of 10 mg or 15 mg anastroz ole. Anastrozole was administered on cycle day 2 for the single-dose groups and on days 26 for the multiple-dose groups. Ultrasound follicular development and endometrial biopsies were performed. Safety was determined from adverse event r eports and laboratory parameters. Pharmacokinetics, pharmacodynamics, and safety . The pharmacokinetics of anastrozole were linear, predictable, and consistent w ith previously published data in healthy volunteers. In the single-dose groups, E2 levels reached their nadir 36 hours after administration, decreasing by an a verage of 39%from baseline. Follicle-stimulating hormone levels rose by 13%, 52%, 49%, and 75%in the 5-mg, 10-mg, 15-mg, and 20-mg groups, respectivel y, at approximately 24 hours after dosing. Most subjects recruited just one matu re follicle, with no apparent effect on endometrial maturation. No safety concer ns were noted. Anastrozole was well tolerated and suppressed E2 levels, with a r esultant increase in FSH.To evaluate the pharmacokinetic, pharmacodynamic, and safety profiles of the a romatase inhibitor anastrozole in healthy, premenopausal women. Phase I, single -center study. Infertility clinic. Twenty-six women with regular ovulatory cyc les: 20 received either a single dose of 5 mg, 10 mg, 15 mg, or 20 mg anastrozol e, or remained untreated; 6 received five daily doses of 10 mg or 15 mg anastroz ole. Anastrozole was administered on cycle day 2 for the single-dose groups and on days 26 for the multiple-dose groups. Ultrasound follicular development and endometrial biopsies were performed. Safety was determined from adverse event r eports and laboratory parameters. Pharmacokinetics, pharmacodynamics, and safety . The pharmacokinetics of anastrozole were linear, predictable, and consistent w ith previously published data in healthy volunteers. In the single-dose groups, E2 levels reached their nadir 36 hours after administration, decreasing by an a verage of 39%from baseline. Follicle-stimulating hormone levels rose by 13%, 52%, 49%, and 75%in the 5-mg, 10-mg, 15-mg, and 20-mg groups, respectivel y, at approximately 24 hours after dosing. Most subjects recruited just one matu re follicle, with no apparent effect on endometrial maturation. No safety concer ns were noted. Anastrozole was well tolerated and suppressed E2 levels, with a r esultant increase in FSH.

关 键 词：绝经前女性 药效学 药物代谢动力学 排卵周期 子宫内膜活检 不孕门诊 超声检测 卵泡发育情况 成熟卵泡 参数评价 

分 类 号：R96[医药卫生—药理学]