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

✍ Scribed by Š. Bezek; V. Ščasnár; T. Trnovec; M. Ďurišová; V. Faberová; L. Beneš

• Publisher: John Wiley and Sons
• Year: 1986
• Tongue: English
• Weight: 542 KB
• Volume: 7
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510070205

✦ Synopsis

The pharmacokinetics of pentacaine, a new local anaesthetic agent from the group of carbanilates, was investigated in the rat at a dose of 2mg kg-I i.v. and per 0s. A three-compartment open model gave the best fit to the data. The model parameters are: flI2 99.0 k 14.lmin, V,, 7411.1ml kg-I, C1 77.9ml min-' kg-I: after oral administration f1/2ah 4.9 k 1.9min, 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 0.0084mg kg-'. The whole-body autoradiography in mice showed rapid transfer of 3H radioactivity from the vessels to tissues and a markedly heterogenous disposition pattern in organs.