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.
Keywords: Antiarrhythmic agents, antimyotonic agents, chiral switch, mexiletine, sodium channel blockers.
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