Tocainide is an antiarrhythmic agent belonging to class IB that was primarily used for suppression
of symptomatic ventricular arrhythmias. Tocainide was also reported to relieve pain such as tic
douloureux, trigemina neuralgia in humans and tinnitus. Significant antinociception, as assayed on the
hot-plate test, was observed after intraperitoneal injection of tocainide, too. By the mid-1980s tocainide
was emerging as a more consistently effective treatment for myotonic disorders. Numerous reports of
serious adverse reactions led to the use of tocainide being discontinued, even though research on tocainide
and its analogues, endowed with a better pharmacological profile, is still in progress for their
potential usefulness in the treatment of myotonias. This review is focused on the description of the different
synthetic routes to racemic and optically active tocainide developed in the last decades, as well
as analytical studies regarding enantioseparation methods. Finally, some analogues of tocainide reported
in the literature, most of which with pharmacological studies, have been mentioned.
Keywords: Antiarrhythmic agents, antimyotonic agents, sodium channel blockers, tocainide, hNav1.4, myotonias.
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