FenbendazoleanimalAnimal model2000

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)Unclearother
    not_reportedeffect: 1.36 L/h/kg
  • Volume of distribution at steady state (IV)Unclearother
    not_reportedeffect: 3.35 L/kg
  • Mean residence time (IV)Unclearother
    not_reportedeffect: 2.63 hours
  • Peak plasma concentration of fenbendazole (oral)Unclearother
    not_reportedeffect: 0.07 microg/ml
  • Time to peak plasma concentration (oral)Unclearother
    not_reportedeffect: 3.75 hours
  • Mean residence time (oral)Unclearother
    not_reportedeffect: 15.15 hours
  • Bioavailability of fenbendazoleUnclearother
    not_reportedeffect: 27.1%
  • Oxfendazole proportion of total AUCUnclearother
    not_reportedeffect: two-thirds of total AUC
  • Fenbendazole proportion of total AUC (IV)Unclearother
    not_reportedeffect: 8.4%
  • Fenbendazole proportion of total AUC (oral)Unclearother
    not_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.

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