健康受试者中普鲁卡因胺（PA）和N-乙酰普鲁卡因胺（NAPA）的药代动力学研究。

Pharmacokinetic studies of procainamide (PA) and N-acetylprocainamide (NAPA) in healthy subjects.

作者信息

Wierzchowiecki M, Michałowska D, Lowicki Z, Ochotny R, Grześkowiak A, Tomaszkiewicz T

出版信息

Int J Clin Pharmacol Ther Toxicol. 1980 Jun;18(6):272-6.

Abstract

Pharmacokinetic studies after a single oral dose of 750 mg of PA in 10 normal subjects were performed. In 6 of them, pharmacokinetics of NAPA were also determined after a single oral dose of 900 mg of NAPA. Substantial differences in pharmacokinetic parameters of PA depending on acetylation phenotype were found. In fast acetylators (sulphadimidine phenotyping), half-life was shorter (2.4 +/- 0.7 hr) and 24 hr urine NAPA excretion was larger (22.5 +/- 5.8% of dose) than in slow acetylators (3.6 +/- 1.0 hr and 8.8 +/- 5.4% respectively). NAPA was characterized by different pharmacokinetic parameters (t 1/2 7.0 +/- 1.0 hr, 24 hr urine elimination - 58.5% of dose). Clinical implications of these findings are discussed.

摘要

对10名正常受试者单次口服750毫克对氨基水杨酸（PA）后进行了药代动力学研究。其中6人在单次口服900毫克烟酰对氨基水杨酸（NAPA）后也测定了其药代动力学。发现PA的药代动力学参数因乙酰化表型不同而存在显著差异。在快速乙酰化者（通过磺胺二甲嘧啶表型分析）中，半衰期较短（2.4±0.7小时），24小时尿中NAPA排泄量较大（占剂量的22.5±5.8%），而在慢速乙酰化者中半衰期分别为3.6±1.0小时，24小时尿中NAPA排泄量为8.8±5.4%）。NAPA具有不同药代动力学参数（t1/2为7.0±1.0小时，24小时尿排泄量为剂量的58.5%）。讨论了这些发现的临床意义。