Pharmacokinetics of levofloxacin after single intravenous and oral administration, and its interaction with sucralfate in mixed-breed dogs

Urzua, Natalia
Messina, Maria Jimena
Caverzan, Matias
Prieto, Guillermo
Lüders Post, Carlos
Errecalde, Carlos
Datos de publicación:
The study aims to establish the plasma pharmacokinetic parameters of levofloxacin in mixed-breed dogs, at a single dose of 5 mg/kg, intravenously, orally only and orally with sucralfate pre-treatment (1 g per animal), to evaluate its influence on antimicrobial absorption. Concentrations of levofloxacin in plasma were determined using high-performance liquid chromatography (HPLC) with fluorescence detection. After iv of levofloxacin, the mean (+/- SD) of AUC(0-24), Vz,t1/2 lambda z and MRT, was 19.05 +/- 6.4 mu g-h/ml, 2.43 +/- 0.5 L/kg, 7.93 +/- 1.41 hours and 8.7 +/- 1.5 hours, respectively. After oral administration, theC(max),t1/2 lambda z and bioavailability were 1.95 +/- 0.7 mu g/ml, 7.65 +/- 1.38 hours and 71.93 +/- 9.75%, respectively. In animals given an oral dose of levofloxacin with sucralfate pre-treatment, there was a significant decrease (p < 0.05) inC(max)(0.57 +/- 0.23 mu g/ml), AUC (5.73 +/- 2.26 mu g-h/ml) and bioavailability (31.92 +/- 14.19%). In the dogs studied, it is suggested that the dose 5 mg/kg of levofloxacin for both routes is inadequate to meet PK-PD targets for susceptible bacteria using breakpoints established by the Institute of Clinical and Laboratory Standards (CLSI).