Pharmacokinetics of triclabendazole in rabbits.
1. Pharmacokinetic profiles of triclabendazole (TCBZ) following intravenous (i.v.) and oral administration of the drug in rabbits were carried out. 2. In normal rabbits, TCBZ was metabolized rapidly to its sulphoxide (TCBZ-SO) and sulphone (TCBZ-SO2) derivatives following administration, with undetectable concentrations of unchanged TCBZ in the plasma of the treated animals at any time (detection limit, 10 ng/ml). 3. The disposition kinetics of this drug in rabbits can be described by a two-compartment open model. 4. Mean peak concentrations in plasma of TCBZ-SO and TCBZ-SO2 of 12.41 micrograms/ml and 9.5 micrograms/ml occurred 7.5 and 9.5 hr after oral administration, respectively. 5. Both metabolites were eliminated slowly from plasma with elimination half-lives of 16.86 hr for the sulphoxide and 13 hr for the sulphone. 6. The area under the plasma concentration versus time curve (AUC) was 240 mg hr/l for the sulphoxide, higher than that found for the sulphone, 185 g hr/l.
Alvarez-Bujidos
M L
ML
Departamento de Fisiología, Farmacología y Toxicología, Facultad de Veterinaria, Universidad de León, Spain.
Ortiz
A I
AI
Negro
A
A
Cubría
J C
JC
Ordóñez
D
D
D000284:Administration, Oral; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001562:Benzimidazoles / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001711:Biotransformation; D006207:Half-Life; D007202:Indicators and Reagents; D007275:Injections, Intravenous; D008297:Male; D008954:Models, Biological; D011817:Rabbits; D013450:Sulfones / Q000378:metabolism; D013454:Sulfoxides / Q000378:metabolism; D000077682:Triclabendazole
D000871:Anthelmintics; D001562:Benzimidazoles; D007202:Indicators and Reagents; D013450:Sulfones; D013454:Sulfoxides; D000077682:Triclabendazole