Pharmacokinetics of fenbendazole following intravenous and oral administration to pigs.
American journal of veterinary research
confidence
Key findings
Fenbendazole rapidly eliminated and absorbed in pigs but with low oral bioavailability (27.1%); oxfendazole was the major plasma metabolite (two-thirds of AUC).
View source on PubMed (PMID 10803655) ↗
- Sample size
- 4 pigs
- Population
- Mixed-breed female pigs weighing 32 to 45 kg
- Dosing
- 1 mg/kg IV; 5 mg/kg oral
- Duration
- Blood samples collected up to 72 hours; oral dosing 1 week after IV
- Route
- intravenous and oral
- Blinding
- not_reported
- Controls
- none
- Drug class
- veterinary antiparasitic
Measured endpoints
- Body clearance of fenbendazole (IV)Unclearothernot_reportedeffect: 1.36 L/h/kg
- Volume of distribution at steady state (IV)Unclearothernot_reportedeffect: 3.35 L/kg
- Mean residence time (IV)Unclearothernot_reportedeffect: 2.63 hours
- Peak plasma concentration of fenbendazole (oral)Unclearothernot_reportedeffect: 0.07 microg/ml
- Time to peak plasma concentration (oral)Unclearothernot_reportedeffect: 3.75 hours
- Mean residence time (oral)Unclearothernot_reportedeffect: 15.15 hours
- Bioavailability of fenbendazoleUnclearothernot_reportedeffect: 27.1%
- Oxfendazole proportion of total AUCUnclearothernot_reportedeffect: two-thirds of total AUC
- Fenbendazole proportion of total AUC (IV)Unclearothernot_reportedeffect: 8.4%
- Fenbendazole proportion of total AUC (oral)Unclearothernot_reportedeffect: 4.5%
Full abstract
To determine pharmacokinetics and metabolic patterns of fenbendazole after IV and oral administration to pigs. 4 mixed-breed female pigs weighing 32 to 45 kg. Fenbendazole was administered IV at a dose of 1 mg/kg. One week later, it was administered orally at a dose of 5 mg/kg. Blood samples were collected for up to 72 hours after administration, and plasma concentrations of fenbendazole, oxfendazole, and fenbendazole sulfone were determined by use of high-pressure liquid chromatography. Plasma pharmacokinetics were determined by use of noncompartmental methods. Body clearance of fenbendazole after IV administration was 1.36 L/h/kg, volume of distribution at steady state was 3.35 L/kg, and mean residence time was 2.63 hours. After oral administration, peak plasma concentration of fenbendazole was 0.07 microg/ml, time to peak plasma concentration was 3.75 hours, and mean residence time was 15.15 hours. Bioavailability of fenbendazole was 27.1%. Oxfendazole was the major plasma metabolite, accounting for two-thirds of the total area under the plasma concentration versus time curve after IV and oral administration. Fenbendazole accounted for 8.4% of the total AUC after IV administration and 4.5% after oral administration. Results indicate that fenbendazole was rapidly eliminated from plasma of pigs. The drug was rapidly absorbed after oral administration, but systemic bioavailability was low.