Pharmacokinetics and preliminary safety evaluation of azithromycin in adult horses

• Published in: Journal of veterinary pharmacology and therapeutics Vol. 35; no. 6; pp. 541 - 549
• Main Authors: LECLERE, M, MAGDESIAN, K. G, COLE, C. A, SZABO, N. J, RUBY, R. E, RHODES, D. M, EDMAN, J, VALE, A, WILSON, W. D, TELL, L. A
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.12.2012
• Subjects: Administration, Oral; adults; Animals; Anti-Bacterial Agents - adverse effects; Anti-Bacterial Agents - blood; Anti-Bacterial Agents - pharmacokinetics; appetite; Area Under Curve; azithromycin; Azithromycin - adverse effects; Azithromycin - blood; Azithromycin - pharmacokinetics; bioavailability; Biological Availability; Bronchoalveolar Lavage Fluid - cytology; Cross-Over Studies; Female; foals; Half-Life; Horses - blood; Injections, Intravenous; intragastric administration; Macrophages; mares; neutrophils; oral administration; pharmacokinetics; potassium; safety assessment
• ISSN: 0140-7783; 1365-2885
• DOI: 10.1111/j.1365-2885.2011.01351.x

Leclere, M., Magdesian, K. G., Cole, C. A., Szabo, N. J., Ruby, R. E., Rhodes, D. M., Edman, J., Vale, A., Wilson, W. D., Tell, L. A. Pharmacokinetics and preliminary safety evaluation of azithromycin in adult horses. J. vet. Pharmacol. Therap. 35, 541–549. Azithromycin is widely used in foals but has not been studied in adult horses. The goals of this study were to determine the pharmacokinetic profile and to make a preliminary assessment of the safety of azithromycin in adult horses. Azithromycin was administered intravenously (5 mg/kg) and intragastrically (10 mg/kg) to six healthy mares in a crossover design. Serial plasma samples, blood neutrophils, and pulmonary macrophages were collected for the measurement of azithromycin concentrations. Azithromycin was also administered orally (10 mg/kg) once a day for 5 days to five healthy mares for preliminary evaluation of safety in adult horses. The bioavailability of azithromycin following intragastric administration was 45 ± 12%. Concentrations within peripheral neutrophils and bronchoalveolar macrophages were several fold higher than that of plasma. Mild decreases in appetite (n = 3) and alterations in fecal consistency (n = 3) were noted following repeated oral administration. The pharmacokinetic profiles of azithromycin in adult horses, especially the slow elimination rate and intraneutrophil and intrapulmonary macrophage accumulation, demonstrate that it is conducive to use in this age group. Because of the gastrointestinal alterations noted, further studies are warranted before azithromycin can be recommended for use in adult horses.