The disposition of the local anaesthetic, pentacaine, in rats and mice.
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.
Bezek
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S
Scasnár
V
V
Trnovec
T
T
Durisová
M
M
Faberová
V
V
Benes
L
L
D000284:Administration, Oral; D000779:Anesthetics, Local / Q000378:metabolism*; D000818:Animals; D001345:Autoradiography; D002219:Carbamates / Q000008:administration & dosage / Q000378:metabolism*; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity; D014018:Tissue Distribution; D014316:Tritium
D000779:Anesthetics, Local; D002219:Carbamates; D014316:Tritium; C010618:pentacaine