IngentaConnect Pharmacokinetics of azithromycin after i.v. and i.m. administrati...

Authors: CÁRCELES, C. M.; FONT, A.; ESCUDERO, E.; ESPUNY, A.; MARÍN, P.; FERNÁNDEZ-VARÓN, E.

Source: Journal of Veterinary Pharmacology & Therapeutics, Volume 28, Number 5, October 2005 , pp. 475-479(5)

Abstract:

Cárceles, C. M., Font, A., Escudero, E., Espuny, A., Marín, P., Fernández-Varón, E. Pharmacokinetics of azithromycin after i.v. and i.m. administration to sheep. J. vet. Pharmacol. Therap.28, 475–479.

The pharmacokinetics (PK) of azithromycin after i.v. and i.m. injection at a single dosage of 20 mg/kg bodyweight was studied in sheep. Blood samples were collected from the jugular vein until 120 h after dosing for both routes. Plasma concentrations of azithromycin were determined by bioassay. The plasma concentration–time data of azithromycin best fitted a three-compartment model after i.v. administration and a two-compartment model with first-order absorption after i.m. administration. The elimination half-life (t_1/2z) was 47.70 ± 7.49 h after i.v. administration and 61.29 ± 13.86 h after i.m. administration. Clearance value after i.v. dosing was 0.52 ± 0.08 L/kg·h. After i.m. administration a peak azithromycin concentration (C_max) of 1.26 ± 0.19 mg/L was achieved at 1.24 ± 0.31 h (t_max). Area under the curve (AUC) were 38.85 ± 5.83 mg·h/L and 36.03 ± 1.52 mg·h/L after i.v. and i.m. administration respectively. Bioavailability obtained after i.m. administration was 94.08 ± 11.56%. The high tolerability of this i.m. preparation and the favourable PK behaviour such as the long half-life and high bioavailability make azithromycin likely to be effective in sheep.

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