Pharmacokinetics of pefloxacin in goats after intravenous or oral administration.

The plasma concentrations and pharmacokinetics of the fluoroquinolone antimicrobial agent pefloxacin, following the administration of a single intravenous (10 mg/kg) or oral (20 mg/kg) dose, were investigated in healthy female goats. The antimicrobial activity in plasma was measured at predetermined times after drug administration by an agar well diffusion microbiological assay, using Escherichia coli (ATCC 25922) as the test organism. Concentrations of the drug > or = 0.25 microg/ml were maintained in plasma for up to 6 and 10 h after intravenous (i.v.) or oral administration of pefloxacin, respectively. The concentration time data for pefloxacin in plasma after i.v. or oral administration conformed to two- and one-compartment open models, respectively. Plasma pefloxacin concentrations decreased rapidly during the initial phase after i.v. injection, with a distribution half-life (t(1/2alpha)) of 0.10 +/- 0.01 h. The terminal phase had a half-life (t(1/2beta)) of 1.12 +/- 0.21 h. The volume of distribution at steady state (Vdss), mean residence time (MRT) and total systemic clearance (ClB) of pefloxacin were 1.08 +/- 0.09 L/kg, 1.39 +/- 0.23 h and 821 +/- 88 (ml/h)/kg, respectively. Following oral administration of pefloxacin, the maximum concentration in the plasma (Cmax) was 2.22 +/- 0.48 microg/ml and the interval from administration until maximum concentration (tmax) was 2.3 +/- 0.7 h. The absorption half-life (t(1/2ka)) mean absorption time (MAT) and elimination half-life of pefloxacin were 0.82 +/- 0.40, 4.2 +/- 1.0 and 2.91 +/- 0.50 h, respectively. The oral bioavailability of pefloxacin was 42% +/- 5.8%. On the basis of the pharmacokinetic data, a dosage regimen of 20 mg/kg, i.v. at 8 h intervals or orally twice daily, is suggested for treating infections caused by drug-sensitive pathogens in goats.