乙醇导致人体中普鲁卡因酰胺乙酰化增加。
Ethanol-induced increase in procainamide acetylation in man.
作者信息
Olsen H, Mørland J
出版信息
Br J Clin Pharmacol. 1982 Feb;13(2):203-8. doi: 10.1111/j.1365-2125.1982.tb01357.x.
Abstract
1 The effect of ethanol on procainamide pharmacokinetics was studied in humans by two different experimental designs. In one, ethanol was given 1.5 h after taking the drug followed by hourly drinks, while in the other ethanol was given 2 h before and subsequently after taking the drug. 2 In both studies, ethanol caused a significant reduction of T1/2 and a significant increase in total clearance of procainamide, while the apparent volume of distribution of procainamide, as well as the renal clearance of both procainamide and N-acetylprocainamide were unaffected by ethanol treatment. 3 Ethanol treatment increased the percentage of N-acetylprocainamide measured in blood and urine and the ratio of AUCNAPA/AUCPA significantly. 4 The T1/2 and total clearance of procainamide was significantly different in slow and rapid acetylators.
摘要
1 通过两种不同的实验设计，研究了乙醇对人体普鲁卡因胺药代动力学的影响。在一种设计中，服药1.5小时后给予乙醇，随后每小时饮用一次；而在另一种设计中，服药前2小时及服药后给予乙醇。2 在两项研究中，乙醇均导致普鲁卡因胺的半衰期显著缩短，总清除率显著增加，而普鲁卡因胺的表观分布容积以及普鲁卡因胺和N - 乙酰普鲁卡因胺的肾清除率均不受乙醇治疗的影响。3 乙醇治疗显著增加了血液和尿液中测得的N - 乙酰普鲁卡因胺的百分比以及AUCNAPA/AUCPA的比值。4 慢乙酰化者和快乙酰化者的普鲁卡因胺半衰期和总清除率存在显著差异。
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