Tocainide

Tocainide is an antiarrhythmic agent and a derivative of the local anesthetic lidocaine.¹ It inhibits voltage-gated sodium channel 1.4 (Na_v1.4) in HEK293 cells expressing the human channel (IC₅₀s = 699 and 182 µM at 0.1 and 10 Hz, respectively).² Tocainide reduces the action potential duration at 50% repolarization in isolated dog Purkinje fibers in a concentration-dependent manner.¹ In vivo, tocainide reduces ventricular heart rate and the percent of ectopic beats in a dog model of ventricular tachycardia induced by the cardiac glycoside ouabain (Item No. 14319).¹ Tocainide (50 mg/kg) decreases mechanical hyperalgesia in the nerve-injured paw in a rat model of neuropathic pain induced by chronic constriction injury of the sciatic nerve.² Formulations containing tocainide have previously been used in the treatment of ventricular arrhythmias.

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1. Moore, E.N., Spear, J.F., Horowitz, L.N., et al. Electrophysiologic properties of a new antiarrhythmic drug — tocainide. Am. J. Cardiol. 41(4), 703-709 (1978).

2. Ghelardini, C., J.-F., D., Muraglia, M., et al. Effects of a new potent analog of tocainide on hNav1.7 sodium channels and in vivo neuropathic pain models. Neuroscience 169(2), 863-873 (2010).