Departments of Clinical Pharmacology and Internal Medicine (Division of Cardiology), University of Linköping, Linköping, Sweden.
Br J Clin Pharmacol. 1974 Dec;1(6):467-75. doi: 10.1111/j.1365-2125.1974.tb01696.x.
1 A specific gas-chromatographic method was developed for determination of N-acetylprocaine amide in plasma and urine, using 4-amino-N-(2-piperidinoethyl)benzamide as an internal standard. The investigation was performed in 50 cardiac patients who had reached steady-state plasma concentrations of procaine amide. 2 The plasma concentrations of the acetylated metabolite varied between 1.0 and 15.0 μg/ml and were thus of the same order of magnitude as those of the parent drug. Especially high plasma levels of the metabolite were seen in patients with poor kidney function. 3 The urinary excretion of the metabolite varied markedly between individuals and ranged between 6 and 52% of the administered daily dose. There was a clear tendency towards higher rates of acetylation of procaine amide in patients with short plasma half-lives of isoniazid, i.e. the phenotype rapid acetylators. Because of coexisting therapy with other drugs and impaired renal function in some patients studies are required in healthy human volunteers to ascertain whether the acetylation of procaine amide and isoniazid are mediated by the same enzyme system.
1 建立了一种特异的气相色谱分析法，可用于测定人血浆和尿中的 N-乙酰普鲁卡因酰胺，以 4-氨基-N-(2-哌啶基乙基)苯甲酰胺作为内标。本研究在 50 例已达普鲁卡因酰胺稳态血浓度的心脏病患者中进行。2 酰化代谢产物的血浆浓度在 1.0 和 15.0μg/ml 之间，与母体药物的浓度处于同一数量级。肾功能不良的患者其代谢产物的血浆浓度特别高。3 代谢产物的尿排泄在个体之间差异很大，范围在给予的日剂量的 6～52%之间。异烟肼血浆半衰期短（即快乙酰化表型）的患者，普鲁卡因酰胺的乙酰化率明显较高，有这种倾向。由于一些患者同时进行其它药物治疗和肾功能受损，需要在健康志愿者中进行研究，以确定普鲁卡因酰胺和异烟肼的乙酰化是否由相同的酶系统介导。
