Disposition kinetics and urinary excretion of pefloxacin after intravenous injection in crossbred calves

Abstract

The disposition kinetics and urinary excretion of pefloxacin after a single intravenous administration of 5 mg/kg were investigated in crossbred calves and an appropriate dosage regimen was calculated. At 1 min after injection, the concentration of pefloxacin in the plasma was 18.95 +/- 0.892 microg/ml, which declined to 0.13 +/- 0.02 microg/ml at 10 h. The pefloxacin was rapidly distributed from the blood to the tissue compartment as shown by the high values for the initial distribution coefficient, alpha (12.1 +/- 1.21 h-1) and the constant for the rate of transfer of drug from the central to the peripheral compartment, K12 (8.49 +/- 0.99 h ). The elimination half-life and volume of distribution were 2.21+/- 0.111 h and 1.44 +/- 0.084 L/kg, respectively. The total body clearance (ClB) and the ratio of the drug present in the peripheral to that in the central compartment (P/C ratio) were 0.454 +/- 0.026 L/kg h) and 5.52 +/- 0.519, respectively. On the basis of the pharmacokinetic parameters obtained in the present study, an appropriate intravenous dosage regimen for pefloxacin in cattle for most of the bacteria sensitive to it would be 6.4 mg/kg repeated at 12 h intervals.