综述：美西律代谢

Title:Mexiletine Metabolites: A Review

Volume: 22 Issue: 11

Author(s): Alessia Catalano, Alessia Carocci and Maria Stefania Sinicropi

Affiliation:

关键词: 抗心律失常药，抗肌肉强直剂、手性转换、美西律、钠通道阻滞剂。

摘要: Mexiletine belongs to class IB antiarrhythmic drugs and it is still considered a drug of choice for treating myotonias. However some patients do not respond to mexiletine or have significant side effects limiting its use; thus, alternatives to this drug should be envisaged. Mexiletine is extensive metabolized in humans via phase I and phase II reactions. Only a small fraction (about 10%) of the dose of mexiletine administered is recovered without modifications in urine. Although in the past decades Mex metabolites were reported to be devoid of biological activity, recent studies seem to deny this assertion. Actually, several hydroxylated metabolites showed pharmacological activity similar to that of Mex, thus contributing to its clinical profile. Purpose of this review is to summarize all the studies proposed till now about mexiletine metabolites, regarding structureactivity relationship studies as well as synthetic strategies. Biological and analytical studies will be also reported.

Cite this article as:

Alessia Catalano, Alessia Carocci and Maria Stefania Sinicropi , Mexiletine Metabolites: A Review, Current Medicinal Chemistry 2015; 22 (11) . https://dx.doi.org/10.2174/0929867322666150227145412