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硝苯地平和维拉帕米对氧化代谢的选择性抑制作用:对茶碱的影响。

Selective inhibitory effects of nifedipine and verapamil on oxidative metabolism: effects on theophylline.

作者信息

Robson R A, Miners J O, Birkett D J

机构信息

Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, South Australia.

出版信息

Br J Clin Pharmacol. 1988 Mar;25(3):397-400. doi: 10.1111/j.1365-2125.1988.tb03319.x.

Abstract

Nine healthy male volunteers were studied to assess the possibility of an interaction between theophylline and nifedipine or verapamil using a randomised, crossover design. Subjects received theophylline 125 mg 8 hourly with and without nifedipine 20 mg 12 hourly and verapamil 80 mg 8 hourly. Nifedipine treatment reduced mean total theophylline clearance by 9%, due to decreased clearances via 1- and 3-demethylation. Verapamil treatment reduced mean total theophylline clearance by 14%, due to decreased clearances via 1- and 3-demethylation and 8-hydroxylation. Verapamil and nifedipine at usual clinical doses are unlikely to cause clinically significant changes in theophylline disposition.

摘要

九名健康男性志愿者参与了一项研究,采用随机交叉设计来评估茶碱与硝苯地平或维拉帕米之间相互作用的可能性。受试者每8小时服用125毫克茶碱,同时分别在服用和不服用每12小时20毫克硝苯地平以及每8小时80毫克维拉帕米的情况下进行观察。硝苯地平治疗使茶碱的平均总清除率降低了9%,这是由于1-脱甲基化和3-脱甲基化途径的清除率下降所致。维拉帕米治疗使茶碱的平均总清除率降低了14%,这是由于1-脱甲基化、3-脱甲基化和8-羟化途径的清除率下降所致。常规临床剂量的维拉帕米和硝苯地平不太可能引起茶碱处置方面具有临床意义的变化。

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