抗心律失常药物AN - 132和奎尼丁对大鼠血浆地高辛浓度的影响。

Effects of AN-132 and quinidine, antiarrhythmic agents, on plasma digoxin concentrations in rats.

作者信息

Sakai K, Yamazaki T, Hinohara Y

机构信息

Department of Pharmacology, Chugai Pharmaceutical Co., Ltd., Japan.

出版信息

J Pharm Pharmacol. 1988 Jan;40(1):68-9. doi: 10.1111/j.2042-7158.1988.tb05157.x.

DOI:10.1111/j.2042-7158.1988.tb05157.x

PMID:2896782

Abstract

The effects of AN-132, 3-(diisopropylaminoethyl-amino)-2',6'-dimethylpropionanilide.2H 3PO4, on chloroform-induced arrhythmias and plasma digoxin concentrations have been compared with those of quinidine in rats. AN-132 (0.01-3 mg kg-1) administered orally significantly inhibited the incidence of cardiac arrhythmias in a dose-related fashion. A single dose of digoxin (1 mg kg-1) given orally for 7 consecutive days was followed, on day 8, orally by digoxin alone, or together with AN-132 (50, 100 and 200 mg kg-1) or quinidine (25 and 50 mg kg-1). The AUC0-24 and Cmax of plasma digoxin were enhanced significantly by co-administration of quinidine, but not by AN-132.

摘要

已将3-(二异丙基氨基乙基-氨基)-2',6'-二甲基丙酰苯胺.2H₃PO₄（AN-132）对氯仿诱导的心律失常和血浆地高辛浓度的影响与奎尼丁在大鼠中的影响进行了比较。口服给予AN-132（0.01 - 3 mg/kg）以剂量相关方式显著抑制心律失常的发生率。连续7天每天口服单剂量地高辛（1 mg/kg），在第8天，单独口服地高辛，或与AN-132（50、100和200 mg/kg）或奎尼丁（25和50 mg/kg）一起口服。同时给予奎尼丁可显著提高血浆地高辛的AUC₀₋₂₄和Cmax，但AN-132则无此作用。