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运动可改变咪达唑仑的药代动力学。

Exercise alters the pharmacokinetics of midazolam.

作者信息

Strömberg C, Vanakoski J, Olkkola K T, Lindqvist A, Seppälä T, Laitinen L A

机构信息

Department of Pharmacology, University of Helsinki, Finland.

出版信息

Clin Pharmacol Ther. 1992 May;51(5):527-32. doi: 10.1038/clpt.1992.58.

DOI:10.1038/clpt.1992.58
PMID:1587067
Abstract

Six healthy volunteers received 15 mg midazolam, 50 mg ephedrine, or placebo orally before a 50-minute aerobic treadmill exercise and in a control session. Plasma drug concentrations for pharmacokinetic calculations were estimated from samples drawn up to 24 hours after drug intake. Heart rate, blood pressure, critical flicker fusion test, Maddox wing test, and visual analog scales relating to mood and feelings of tiredness were included in the sessions as pharmacodynamic measures. These tests were made at 35, 55, and 75 minutes and at 2, 2 1/2, 3 1/2, and 5 hours after drug intake. Exercise impaired the absorption of midazolam and counteracted the midazolam-induced decrement in flicker fusion threshold. Whether the effect on flicker fusion was caused mainly by the pharmacokinetic changes or by a general alerting effect of exercise cannot be verified by this experiment. The kinetics of ephedrine was not affected by exercise, but exercise enhanced the tachycardic response to ephedrine and abolished its pressor effect.

摘要

六名健康志愿者在进行50分钟的有氧跑步机运动前以及在对照时段口服15毫克咪达唑仑、50毫克麻黄碱或安慰剂。根据服药后长达24小时采集的样本估算用于药代动力学计算的血浆药物浓度。作为药效学指标,各时段纳入了心率、血压、临界闪烁融合试验、马多克斯翼试验以及与情绪和疲劳感相关的视觉模拟量表。这些测试在服药后35、55和75分钟以及2、2.5、3.5和5小时进行。运动损害了咪达唑仑的吸收,并抵消了咪达唑仑引起的闪烁融合阈值降低。本实验无法证实对闪烁融合的影响主要是由药代动力学变化还是运动的一般警觉作用所致。麻黄碱的动力学不受运动影响,但运动增强了对麻黄碱的心动过速反应并消除了其升压作用。

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Exercise alters the pharmacokinetics of midazolam.运动可改变咪达唑仑的药代动力学。
Clin Pharmacol Ther. 1992 May;51(5):527-32. doi: 10.1038/clpt.1992.58.
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