Disposition of enrofloxacin in plasma, pulmonary epithelial lining fluid, peritoneal fluid, and cerebrospinal fluid of healthy mares.

OBJECTIVE

To investigate the disposition of enrofloxacin and its active metabolite, ciprofloxacin, in plasma, pulmonary epithelial lining fluid (PELF), peritoneal fluid, and CSF in horses following IV administration of enrofloxacin at doses of 5 mg/kg and 7.5 mg/kg of body weight.

METHODS

6 healthy, mature mares were randomly assigned to receive a single dose of enrofloxacin at either 5 mg/kg or 7.5 mg/kg in a crossover design with a washout period of 10 days. Concentrations of enrofloxacin and ciprofloxacin were determined in plasma, PELF, peritoneal fluid, and CSF.

RESULTS

Both doses of enrofloxacin were generally well tolerated. One horse developed focal, self-limiting limb edema. The median maximum concentration extrapolated to time 0 and area under the plasma concentration-versus-time curve from time 0 to the last quantifiable time point (24 hours) for enrofloxacin in plasma were significantly greater when horses were given enrofloxacin at 7.5 mg/kg. Similarly, the median elimination rate constant, half-life of the terminal phase, peak serum concentration (Cmax), area under the plasma concentration-versus-time curve from time 0 to the last quantifiable time point (24 hours), area under the plasma concentration-versus-time curve extrapolated to infinity, and mean residence time for ciprofloxacin in plasma were significantly greater following administration of enrofloxacin at 7.5 mg/kg. There were no significant differences between doses in any of the measured pharmacokinetic variables in PELF.

CONCLUSIONS

There was no apparent pharmacokinetic advantage of enrofloxacin at the 7.5-mg/kg dose for susceptible isolates; however, this dose achieved higher concentrations and prolonged persistence in fluid matrices. Further studies are required to evaluate repeated administration at this dose for tolerability and clinical efficacy.

CLINICAL RELEVANCE

Despite the wide use of enrofloxacin in horses, pharmacokinetic data is limited. This study provides pharmacokinetic data that can be used in a clinical setting.