SINGLE-DOSE QUINIDINE TREATMENT INHIBITS MEXILETINE OXIDATION IN EXTENSIVE METABOLIZERS OF DEBRISOQUINE

被引：12

作者：

BROLY, F ^{[1
]}

VANDAMME, N ^{[1
]}

CARON, J ^{[1
]}

LIBERSA, C ^{[1
]}

LHERMITTE, M ^{[1
]}

机构：

[1] HOP CALMETTE,DEPT BIOCHIM,TOXICOL LAB,F-59045 LILLE,FRANCE

来源：

LIFE SCIENCES | 1991年 / 48卷 / 26期

关键词：

D O I：

10.1016/0024-3205(91)90618-L

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Urinary elimination of unchanged mexiletine, p-hydroxymexiletine (PHM), hydroxymethylmexiletine (HMM) and mexiletine N-glucuronide conjugate (MGC) was investigated before and after treatment with quinidine. All subjects were phenotyped as extensive metabolizers for debrisoquine oxidation. The total recovery of mexiletine and metabolites was significantly reduced after quinidine pretreatment. It is concluded that pretreatment with a very low dose of quinidine inhibits markedly the elimination of both major mexiletine metabolites (PHM and HMM) and likely decreases the overall elimination of mexiletine. That should lead to changes in mexiletine disposition and have clinical consequences during combination therapy with both drugs.

引用

页码：PL123 / PL128

页数：6

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