Selection of an aminoglycoside antibiotic for administration to horses.
The serum concentrations of the aminoglycosides neomycin, kanamycin and streptomycin were determined after intravenous (iv) and intramuscular (im) administration. These values were then related to the minimum inhibitory concentrations (MIC) of a number of equine pathogenic bacteria to determine the duration of therapeutic serum concentrations of the aminoglycosides in the horse. Pharmacokinetic analysis of the data using neomycin as the example revealed a mean (+/- sd) peak serum concentration of 23.2 +/- 10.2 micrograms/ml present at 30 mins, and at 8 h the serum concentration was 2.8 +/- 0.8 micrograms/ml. From the pharmacological analysis of concentration-time data it was shown that neomycin was very rapidly absorbed from the im injection site, with an absorption half-time of 0.16 +/- 0.05 and was well absorbed (systemic availability was 73.7 +/- 26.9 per cent). A peak tissue level, which represented 40 per cent of the amount of drug in the body, was obtained at 32 mins after injection of the drug. At 8 h, the fractions of the dose in the central and peripheral compartments of the model were 1.5 per cent and 2.5 per cent respectively, and 96 per cent was the cumulative amount eliminated up to that time. Based on the MIC values of the majority of isolates of Corynebacterium equi, and only a few isolates of Klebsiella pneumoniae, Escherichia coli, Salmonella typhimurium and Streptococcus equi, one would expect a serum concentration of more than 2 micrograms neomycin/ml up to 8 h following im dosage (10 mg/kg) to be therapeutically effective.
D000617:Aminoglycosides / Q000008:administration & dosage / Q000097:blood; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000097:blood; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D006736:Horses / Q000097:blood*; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D013997:Time Factors
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents