The pharmacokinetics of quinidine and quinine following intravenous administration (10 mg/kg) with and without concurrent treatment with oral activated charcoal was studied in the rabbit. Marked differences were observed in the pharmacokinetic parameters. Compared to quinidine, quinine was characterized by larger volume of distribution (Vd), systemic clearance (Cl) and elimination rate constant (Kel), and smaller half-life of elimination (t1/2), mean residence time (MRT) and area under the curve (AUC). Activated charcoal administered orally (15 g) significantly decreased the serum concentrations of quinidine but not quinine. Furthermore, charcoal treatment significantly enhanced the systemic elimination of quinidine as indicated by the significant increase in Cl and decrease in t1/2, MRT and AUC. By contrast, activated charcoal had no significant effect on the pharmacokinetic parameters of quinine. Differences between quinidine and quinine in respect to the effect of activated charcoal on the systemic elimination of these drugs seem at least, in part, dependent on dispositional factors. The high Cl and Vd of quinine in the rabbit are probably factors that mask the effect of charcoal on the elimination of this drug.