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硝苯地平对肝脏药物氧化的影响。

Effects of nifedipine on hepatic drug oxidation.

作者信息

Dickinson T H, Egan J M, Abernethy D R

机构信息

Division of Clinical Pharmacology, Brown University, Providence, R.I.

出版信息

Pharmacology. 1988;36(6):405-10. doi: 10.1159/000138329.

Abstract

To determine whether inhibition of drug oxidation is a general property of all calcium antagonist drugs or just of a few, we measured effects of therapeutic doses of nifedipine on antipyrine biotransformation. Antipyrine was administered in random order to 10 subjects while drug-free and while taking nifedipine 30 mg 3 times daily. Total antipyrine clearance (means +/- SE, 43.1 +/- 4.8 control vs. 50.4 +/- 6.5 ml/min; NS) tended to increase but not significantly. Elimination half-life decreased slightly (13.7 +/- 1.0 control vs. 11.7 +/- 0.9; p less than 0.05). Antipyrine metabolite excretion, measured to evaluate selective oxidative pathways, was unaffected by concurrent nifedipine administration. Nifedipine in therapeutic doses had no effect on antipyrine oxidation, unlike verapamil and diltiazem, both of which inhibit hepatic drug oxidation. Inhibition of drug oxidation appears not to be a general property of calcium antagonist drugs.

摘要

为了确定抑制药物氧化是所有钙拮抗剂药物的普遍特性还是仅为少数药物的特性,我们测量了治疗剂量的硝苯地平对安替比林生物转化的影响。在10名受试者未服用药物以及每天3次服用30 mg硝苯地平的情况下,随机给予安替比林。安替比林的总清除率(均值±标准误,未服用药物时为43.1±4.8,服用硝苯地平时为50.4±6.5 ml/min;无显著性差异)有升高趋势,但不显著。消除半衰期略有下降(未服用药物时为13.7±1.0,服用硝苯地平时为11.7±0.9;p<0.05)。为评估选择性氧化途径而测量的安替比林代谢物排泄不受同时服用硝苯地平的影响。与维拉帕米和地尔硫䓬不同,治疗剂量的硝苯地平对安替比林氧化没有影响,维拉帕米和地尔硫䓬均抑制肝脏药物氧化。抑制药物氧化似乎不是钙拮抗剂药物的普遍特性。

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