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 r...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.展开更多
文摘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.
