Pharmacokinetics of enrofloxacin in adult horses and concentration of the drug in serum, body fluids, and endometrial tissues after repeated intragastrically administered doses

Steeve Giguère From the New Bolton Center, Department of Clinical Studies, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, PA 19348.

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Raymond W. Sweeney From the New Bolton Center, Department of Clinical Studies, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, PA 19348.

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Myriam Bélanger From the New Bolton Center, Department of Clinical Studies, School of Veterinary Medicine, University of Pennsylvania, Kennett Square, PA 19348.

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Abstract

Objective

To investigate the pharmacokinetics of enrofloxacin in adult horses.

Design

2-dose oral and IV cross-over trial followed by multiple oral doses.

Animals

8 clinically normal adult horses.

Procedure

Enrofloxacin was administered at dosages of 2.5 mg/kg of body weight to 4 horses and 5.0 mg/kg to 4 other horses. Each dose was given by the intragastric and IV routes, using a cross-over design. After the first intragastric dose, 5 additional doses were administered at 12-hour intervals. Enrofloxacin concentrations were measured in serum, synovial fluid, peritoneal fluid, urine, CSF, and endometrial tissues.

Results

Disposition of enrofloxacin after IV administration conformed to a 2-compartment model with an elimination half-life of 5.95 and 6.09 hours for the low and high dose, respectively. After the first intragastric administration, time to peak concentration was 1.0 ± 0.35 and 1.25 ± 0.43 hours, and the bioavailabihty was 57.39 ± 8.45 and 62.52 ± 19.65% for the low and high dose, respectively. After multiple intragastric administration, peak serum concentration (at 72 to 96 hours) was 2.62 ± 0.61 μg/ml for the low dose and 5.97 ± 1.56 μg/ml for the high dose. After multiple intragastric doses, synovial fluid, urine, and endometrial tissue concentrations exceeded serum concentrations. Peritoneal fluid and CSF concentrations were lower than serum concentrations.

Conclusions

Computer modeling of the pharmacokinetic variables suggested that a single daily IV administered dose of 5.5 mg/kg, or orally administered doses of 7.5 mg/kg every 24 hours or 4.0 mg/kg every 12 hours, would be effective in horses. Additional studies are necessary to confirm the efficacy and safety of these dosages in a clinical setting. (Am J Vet Res 1996;57:1025–1030)

Abstract

Objective

To investigate the pharmacokinetics of enrofloxacin in adult horses.

Design

2-dose oral and IV cross-over trial followed by multiple oral doses.

Animals

8 clinically normal adult horses.

Procedure

Enrofloxacin was administered at dosages of 2.5 mg/kg of body weight to 4 horses and 5.0 mg/kg to 4 other horses. Each dose was given by the intragastric and IV routes, using a cross-over design. After the first intragastric dose, 5 additional doses were administered at 12-hour intervals. Enrofloxacin concentrations were measured in serum, synovial fluid, peritoneal fluid, urine, CSF, and endometrial tissues.

Results

Disposition of enrofloxacin after IV administration conformed to a 2-compartment model with an elimination half-life of 5.95 and 6.09 hours for the low and high dose, respectively. After the first intragastric administration, time to peak concentration was 1.0 ± 0.35 and 1.25 ± 0.43 hours, and the bioavailabihty was 57.39 ± 8.45 and 62.52 ± 19.65% for the low and high dose, respectively. After multiple intragastric administration, peak serum concentration (at 72 to 96 hours) was 2.62 ± 0.61 μg/ml for the low dose and 5.97 ± 1.56 μg/ml for the high dose. After multiple intragastric doses, synovial fluid, urine, and endometrial tissue concentrations exceeded serum concentrations. Peritoneal fluid and CSF concentrations were lower than serum concentrations.

Conclusions

Computer modeling of the pharmacokinetic variables suggested that a single daily IV administered dose of 5.5 mg/kg, or orally administered doses of 7.5 mg/kg every 24 hours or 4.0 mg/kg every 12 hours, would be effective in horses. Additional studies are necessary to confirm the efficacy and safety of these dosages in a clinical setting. (Am J Vet Res 1996;57:1025–1030)

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