Pharmacokinetics of lidocaine and its active metabolites in dogs

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Abstract
The pharmacokinetics of lidocaine [an antiarrhythmic] in dogs were investigated following i.v. and i.m. administration of single doses of lidocaine hydrochloride. The mean elimination rate constant and the mean specific clearance determined for the i.v. portion of the study were 0.786 h-1 and 2.40 l/kg per h, respectively. Following i.m. administration the mean absorption rate constant was 7.74 h-1. Absorption was nearly complete as the percentage of an i.m. dose absorbed averaged 91.9%. Concentrations of 2 N-deethylated metabolites, determined following the administration of lidocaine suggest that monoethylglycinexylidide is eliminated rapidly while glycinexylidide is more slowly eliminated. The relative contribution of these metabolites to the therapeutic and toxic effects of lidocaine and the potential for glycinexylidide accumulation during lidocaine administration remain to be investigated.