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Mexiletine is a new antiarrhythmic agent which resembles to lidocaine electrophysiologically and is available for oral use. We investigated pharmacokinetic parameters and clinical effects on ventricular premature contractions (VPCs) of a single dose of mexiletine in 27 patients with frequent VPCs. The maximum concentration (Cmax) and the area under the time-concentration curve (AUC) increased dose-dependently, and the time to the maximum concentration after oral administration was 3.0 hours. There were significant correlations between dosage (mg/kg) and Cmax (r=0.87, p