Clinical efficacy and pharmacokinetics of a new orally effective antiarrhythmic, tocainide.

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Abstract
Tocainide, a new oral antiarrhythmic agent, was studied in man in a short-term protocol designed to evaluate the efficacy, kinetics and toxicity of this compound. Premature ventricular contractions (PVC) were suppressed by > 70% in 11 of 15 patients compared with pre-drug placebo controls. For these 11 responders, there was an average PVC reduction of 91% .+-. 10 (range 70-100%) at tocainide doses not associated with side effects. Mild transient CNS toxicity was observed in some patients near the time of peak concentrations during the highest dose administered. The drug had linear kinetics over the dose range studied and a plasma half-life of 13.5 .+-. 2 h. Plasma concentration-response curves indicate antiarrhythmic activity over all plasma concentrations, with 70% PVC reduction above 6.0 .mu.g/ml. Tocainide is a safe and effective antiarrhythmic agent during short-term administration and is worthy of further clinical trials.