摘要
美西律属于类IB抗心律失常的药物,它仍然被认为是一种药物的首选治疗肌强直。但是有些病人使用美西律没有明显药效作用或有明显的副作用限制了其使用。因此应该设计这种药物的替代品。美西律在人类通过第一阶段和第二阶段的反应被大量代谢。只有一小部分(大约10%)剂量的美西律以原型从尿液排泄。尽管在过去的几十年美西律缺乏生物活性代谢物被报道,最近的研究似乎又否认这种说法。实际上,类似于美西律,一些羟化代谢产物显示了药理作用,从而导致其临床研究。本文的目的是总结所有关于美西律代谢物、构效关系以及合成策略从提出到现在的研究。生物学和分析方法研究也将阐述。
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。
Current Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/0929867322666150227145412 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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