FENTANYL AND PETHIDINE ARE ANTAGONISTS ON MUSCARINIC RECEPTORS IN GUINEA-PIG ILEUM

被引:13
作者
HUSTVEIT, O
SETEKLEIV, J
机构
[1] Department of Pharmacology, University of Oslo
关键词
CENTRAL ANTICHOLINERGIC SYNDROME; FENTANYL; GUINEA-PIG ILEUM; MUSCARINIC RECEPTORS; PETHIDINE;
D O I
10.1111/j.1399-6576.1993.tb03761.x
中图分类号
R614 [麻醉学];
学科分类号
100217 ;
摘要
In order to evaluate the anticholinergic effect of fentanyl and pethidine, the influence of these drugs on the cumulative dose-response curves of carbacholine on the guinea-pig ileum has been investigated. Fentanyl and pethidine displaced the dose-response curve for carbacholine to the right in a parallel fashion, indicating competitive antagonism. Dissociation constants determined by an agonist EC versus antagonist plot were 0.22 mumol/l for fentanyl and 1.4 mumol/l for pethidine. It is concluded that during high-dose fentanyl anaesthesia, fentanyl may bind to muscarinic receptors and thereby produce a central anticholinergic syndrome. An additional finding was that the maximal response to carbacholine increased significantly when combined with pethidine.
引用
收藏
页码:541 / 544
页数:4
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