Pharmacokinetics of enrofloxacin in adult horses and concentration of the drug in serum, body fluids, and endometrial tissues after repeated intragastrically administered doses.
Abstract: To investigate the pharmacokinetics of enrofloxacin in adult horses. Methods: 2-dose oral and i.v. cross-over trial followed by multiple oral doses. Methods: 8 clinically normal adult horses. Methods: 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 i.v. 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 i.v. 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 bioavailability 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 micrograms/ml for the low dose and 5.97 +/- 1.56 micrograms/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 i.v. 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.
Publication Date: 1996-07-01 PubMed ID: 8807015
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- Journal Article
Summary
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The research article is about a study that assessed the behaviour of the drug enrofloxacin in adult horses, which involved observing how the drug moves within the body and its concentration levels in different body fluids and tissues after repeated administration.
Objective of the Study
The primary objective of this research was to explore the pharmacokinetics (how a body absorbs, distributes, metabolizes, and excretes a drug) of enrofloxacin in adult horses. Researchers administered the drug in different doses and ways and measured its concentration in various body fluids and tissues over time.
Methodology of the Study
- Eight clinically normal adult horses were used in the research.
- The team used a 2-dose oral and intravenous (i.v.) cross-over trial (where groups of subjects receive different sequences of treatments) followed by multiple oral doses.
- Enrofloxacin was administered to half the horses at 2.5 mg/kg of body weight and to the other half at 5.0 mg/kg, via both intragastric and i.v. routes.
- After the first intragastric dosage, an additional five doses were administered at 12-hour intervals.
- Enrofloxacin concentrations were then measured in serum, synovial fluid, peritoneal fluid, urine, cerebrospinal fluid (CSF), and endometrial tissues.
Results of the Study
- The distribution of enrofloxacin after intravenous administration conformed to a two-compartment model with an elimination half-life of around six hours for both dosages.
- After the first intragastric administration, time to peak concentration was around 1 to 1.25 hours, with the bioavailability (the proportion of the drug that enters the circulation when introduced into the body) being between 57.39% and 62.52% for the low and high doses, respectively.
- After multiple intragastric doses, enrofloxacin concentrations in the synovial fluid, urine, and endometrial tissue exceeded serum concentrations. In contrast, the concentration in peritoneal fluid and CSF was lower than in serum.
Conclusion of the Study
Based on the pharmacokinetic data, the study suggests that a single daily i.v. administered dose of 5.5 mg/kg, or an orally administered dose of 7.5 mg/kg every 24 hours or 4.0 mg/kg every 12 hours, would be effective in horses. However, additional research is recommended to confirm the efficacy and safety of these doses in a clinical, practical setting.
Cite This Article
APA
Giguère S, Sweeney RW, Bélanger M.
(1996).
Pharmacokinetics of enrofloxacin in adult horses and concentration of the drug in serum, body fluids, and endometrial tissues after repeated intragastrically administered doses.
Am J Vet Res, 57(7), 1025-1030.
Publication
Researcher Affiliations
- New Bolton Center, Department of Clinical Studies, School of Veterinary Medicine, University of Pennsylvania, Kennett Square 19348, USA.
MeSH Terms
- Administration, Oral
- Animals
- Anti-Infective Agents / administration & dosage
- Anti-Infective Agents / blood
- Anti-Infective Agents / pharmacokinetics
- Cross-Over Studies
- Dose-Response Relationship, Drug
- Drug Administration Schedule
- Endometrium / metabolism
- Enrofloxacin
- Female
- Fluoroquinolones
- Horses
- Injections, Intravenous
- Male
- Quinolones / administration & dosage
- Quinolones / blood
- Quinolones / pharmacokinetics
- Software
- Synovial Fluid / metabolism
- Tissue Distribution
Citations
This article has been cited 16 times.- Atef M, El-Banna HA, Elzorba HY, Soliman AM. Pharmacokinetics and tissue residue of enrofloxacin in healthy, Eimeria-infected broiler chickens and those pre-treated with amprolium and toltrazuril.. Int J Vet Sci Med 2020 Jun 1;8(1):31-38.
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- Kang J, Hossain MA, Park HC, Kim Y, Lee KJ, Park SW. Pharmacokinetic and pharmacodynamic integration of enrofloxacin against Salmonella Enteritidis after administering to broiler chicken by per-oral and intravenous routes.. J Vet Sci 2019 Mar;20(2):e15.
- Xiao X, Jiang L, Lan W, Jiang Y, Wang Z. In vivo pharmacokinetic/Pharmacodynamic modeling of Enrofloxacin against Escherichia coli in broiler chickens.. BMC Vet Res 2018 Nov 29;14(1):374.
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- Lei Z, Liu Q, Yang B, Xiong J, Li K, Ahmed S, Hong L, Chen P, He Q, Cao J. Clinical Efficacy and Residue Depletion of 10% Enrofloxacin Enteric-Coated Granules in Pigs.. Front Pharmacol 2017;8:294.
- Sang K, Hao H, Huang L, Wang X, Yuan Z. Pharmacokinetic-Pharmacodynamic Modeling of Enrofloxacin Against Escherichia coli in Broilers.. Front Vet Sci 2015;2:80.
- Ruennarong N, Wongpanit K, Sakulthaew C, Giorgi M, Kumagai S, Poapolathep A, Poapolathep S. Dispositions of enrofloxacin and its major metabolite ciprofloxacin in Thai swamp buffaloes.. J Vet Med Sci 2016 Mar;78(3):397-403.
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- Adams AR, Haines GR, Brown MP, Gronwall R, Merritt K. Pharmacokinetics of difloxacin and its concentration in body fluids and endometrial tissues of mares after repeated intragastric administration.. Can J Vet Res 2005 Jul;69(3):229-35.
- Ramesh S, Rao GS, Malik JK. Pharmacokinetic disposition of subcutaneously administered enrofloxacin in goats.. Vet Res Commun 2002 Oct;26(7):563-9.
- Fumuso E, Checura C, Losinno L, Soto P, Sánchez S. Endometrial tissue concentrations of enrofloxacin after intrauterine administration to mares.. Vet Res Commun 2002 Jul;26(5):371-80.
- Haines GR, Brown MP, Gronwall RR, Merritt KA, Baltzley LK. Pharmacokinetics of orbifloxacin and its concentration in body fluids and in endometrial tissues of mares.. Can J Vet Res 2001 Jul;65(3):181-7.
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