Sprouse J S, Schneck D W, Hayes A H
J Pharmacol Exp Ther. 1978 Dec;207(3):698-704.
The effects of isoniazid (INH), hydralazine, salicylazosulfapyridine, and sulfapyridine on the quantitative disposition of procainamide (PA) in the intact rat were examined. A dose-dependent inhibition of PA acetylation was observed after coadministration of PA with INH via nasogastric intubation. The 24-hr urinary excretion of N-acetylprocainamide was noted to decline in the presence of INH whereas that of the unchanged drug exhibited a coincident rise. A reduction in the systemic clearance of PA and a prolongation in its half-life of elimination was also observed. INH increased PA hepatic levels and decreased N-acetylprocainamide hepatic content. In contrast hydralazine affects not only PA acetylation but also its absorption rate and transformation by other metabolic pathways. Salicylazosulfapyridine did not affect PA acetylation whereas high doses of sulfaphridine did.
研究了异烟肼（INH）、肼屈嗪、柳氮磺胺吡啶和磺胺吡啶对完整大鼠体内普鲁卡因胺（PA）定量处置的影响。经鼻胃管同时给予PA和INH后，观察到PA乙酰化受到剂量依赖性抑制。在INH存在的情况下，N - 乙酰普鲁卡因胺的24小时尿排泄量下降，而未变化药物的尿排泄量则同时升高。还观察到PA的全身清除率降低，消除半衰期延长。INH增加了PA的肝脏水平，降低了N - 乙酰普鲁卡因胺的肝脏含量。相比之下，肼屈嗪不仅影响PA的乙酰化，还影响其吸收速率和通过其他代谢途径的转化。柳氮磺胺吡啶不影响PA的乙酰化，而高剂量的磺胺吡啶则有影响。
