The disposition of the local anaesthetic, pentacaine, in rats and mice

Abstract

The pharmacokinetics of pentacaine, a new local anaesthetic agent from the group of carbanilates, was investigated in the rat at a dose of 2 mg kg-1 i.v. and per os. A three-compartment open model gave the best fit to the data. The model parameters are: t1/2 99.0 +/- 14.1 min, Vss 7411.1 ml kg-1, Cl 77.9 ml min-1 kg-1; after oral administration t1/2ab 4.9 +/- 1.9 min, bioavailability 59.1 per cent, and extent of absorption 79.3 per cent. Pentacaine is eliminated almost entirely by metabolism. The metabolites are excreted equally in the urine and faeces at a relatively slow rate. The pharmacokinetics of pentacaine was linear in the dose range 0.008-4 mg kg-1. The whole-body autoradiography in mice showed rapid transfer of 3H radioactivity from the vessels to tissues and a markedly heterogeneous disposition pattern in organs.