Pharmacokinetics of toremifene

M. Anttila, R. Valavaara , S. Kivinen , J. Mäenpää
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引用次数: 57

Abstract

The pharmacokinetics of toremifene has been investigated in man after single and multiple oral doses. Toremifene was completely absorbed without first-pass metabolism. Peak concentration in serum was achieved in 4 h. Mean half-lives of distribution and elimination were 4 h and 5 days, respectively. Kinetics was linear in the studied dose-range of 10–680 mg. Toremifene was over 99% bound to plasma proteins and extensively metabolized. The main metabolites in serum were demethyl- and deaminohydroxytoremifene. In patients receiving multiple dosing of 60 mg/day serum steady-state level of toremifene was 0.8 μg/ml on average. The level of demethyl metabolite was twice and that of deaminohydroxy metabolite was one tenth of toremifene.

托瑞米芬的药代动力学
研究了托瑞米芬单次和多次口服后在人体中的药代动力学。托瑞米芬完全被吸收,没有第一次代谢。血清浓度在4 h内达到峰值,分布和消除的平均半衰期分别为4 h和5 d。动力学在10-680 mg的研究剂量范围内呈线性。托瑞米芬99%以上与血浆蛋白结合并被广泛代谢。血清主要代谢物为去甲基和去胺羟基托瑞米芬。在多次给药60mg /d的患者中,托瑞米芬的血清稳态水平平均为0.8 μg/ml。去甲基代谢物是托瑞米芬的两倍,脱胺羟基代谢物是托瑞米芬的十分之一。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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