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American journal of veterinary research2000; 61(6); 706-709; doi: 10.2460/ajvr.2000.61.706

Pharmacokinetics of enrofloxacin administered intravenously and orally to foals.

Abstract: To determine the pharmacokinetics of enrofloxacin administered IV and orally to foals. Methods: 5 clinically normal foals. Methods: A 2-dose cross-over trial with IV and oral administration was performed. Enrofloxacin was administered once IV (5 mg/kg of body weight) to 1-week-old foals, followed by 1 oral administration (10 mg/kg) after a 7-day washout period. Blood samples were collected for 48 hours after the single dose IV and oral administrations and analyzed for plasma enrofloxacin and ciprofloxacin concentrations by use of high-performance liquid chromatography. Results: For IV administration, mean +/- SD total area under the curve (AUC0-infinity) was 48.54 +/- 10.46 microg x h/ml, clearance was 103.72 +/- 0.06 ml/kg/h, half-life (t1/2beta) was 17.10 +/- 0.09 hours, and apparent volume of distribution was 2.49 +/- 0.43 L/kg. For oral administration, AUC0-infinity was 58.47 +/- 16.37 microg x h/ml, t1/2beta was 18.39 +/- 0.06 hours, maximum concentration (Cmax) was 2.12 +/- 00.51 microg/ml, time to Cmax was 2.20 +/- 2.17 hours, mean absorption time was 2.09 +/- 0.51 hours, and bioavailability was 42 +/- 0.42%. Conclusions: Compared with adult horses given 5 mg of enrofloxacin/kg IV, foals have higher AUC0-infinity, longer t1/2beta, and lower clearance. Concentration of ciprofloxacin was negligible. Using a target Cmax to minimum inhibitory concentration ratio of 1:8 to 1:10, computer modeling suggests that 2.5 to 10 mg of enrofloxacin/kg administered every 24 hours would be effective in foals, depending on minimum inhibitory concentration of the pathogen.
Publication Date: 2000-06-13 PubMed ID: 10850849DOI: 10.2460/ajvr.2000.61.706Google Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research article investigates how foals’ bodies absorb and eliminate the drug enrofloxacin, an antibiotic, when given intravenously or orally. The study found that this process is more efficient in foals compared to adult horses and certain dosage recommendations are suggested based on computer modeling.

Research Methods

  • Five clinically normal foals were involved in this study. Enrofloxacin was administered in two ways in a cross-over experiment: first intravenously at 5 mg/kg of body weight, then orally at 10 mg/kg after a 7-day washout period – time allowed for the drug to completely leave the foal’s system.
  • Blood samples were collected over 48 hours after both methods of administration. The plasma samples were then analyzed using high-performance liquid chromatography, a technique used to identify amounts of specific substances, to determine presence and quantities of enrofloxacin and its derivative compound, ciprofloxacin.

Findings

  • Several pharmacokinetic parameters were calculated from the collected data. For IV administration, overall exposure to the drug (measured as mean AUC – area under the curve) was approximately 48.54 microg x h/ml, clearance rate was 103.72 ml/kg/h, half-life around 17.10 hours, and volume of distribution was about 2.49 L/kg.
  • For oral administration, these figures altered; AUC was around 58.47 microg x h/ml, half-life approximately 18.39 hours, peak concentration (Cmax) was about 2.12 microg/ml, time taken to reach this peak (time to Cmax) was 2.20 hours, and the average absorption time was 2.09 hours. The bioavailability (amount of enrofloxacin that entered the systemic circulation) was estimated at 42%.
  • The levels of ciprofloxacin, a derivative compound of enrofloxacin, were negligible indicating that the foals’ bodies did not break down substantial amounts of the administered enrofloxacin into this compound.

Implications and Conclusion

  • Comparatively, it was found that foals have higher total drug exposure (higher AUC), longer drug half-life, and slower drug clearance than adult horses administered with the identical dosage of 5 mg/kg enrofloxacin intravenously.
  • These findings suggest that the biological system of foals processes enrofloxacin differently as compared to adult horses.
  • Based on these pharmacokinetic data and computer modelling, the study proposes that administering between 2.5 to 10 mg of enrofloxacin/kg every 24 hours would effectively treat bacterial infections in foals, depending on the particular pathogen’s minimum inhibitory concentration – the lowest concentration of the drug which can prevent bacterial growth.

Cite This Article

APA
Bermingham EC, Papich MG, Vivrette SL. (2000). Pharmacokinetics of enrofloxacin administered intravenously and orally to foals. Am J Vet Res, 61(6), 706-709. https://doi.org/10.2460/ajvr.2000.61.706

Publication

ISSN: 0002-9645
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 61
Issue: 6
Pages: 706-709

Researcher Affiliations

Bermingham, E C
  • Department of Anatomy, College of Veterinary Medicine, North Carolina State University, Raleigh 27606, USA.
Papich, M G
    Vivrette, S L

      MeSH Terms

      • Administration, Oral
      • Animals
      • Animals, Newborn / metabolism
      • Anti-Infective Agents / administration & dosage
      • Anti-Infective Agents / blood
      • Anti-Infective Agents / metabolism
      • Anti-Infective Agents / pharmacokinetics
      • Area Under Curve
      • Chromatography, High Pressure Liquid / veterinary
      • Ciprofloxacin / blood
      • Computer Simulation
      • Cross-Over Studies
      • Enrofloxacin
      • Fluoroquinolones
      • Half-Life
      • Horses / metabolism
      • Injections, Intravenous / veterinary
      • Quinolones / administration & dosage
      • Quinolones / blood
      • Quinolones / metabolism
      • Quinolones / pharmacokinetics
      • Regression Analysis

      Citations

      This article has been cited 6 times.
      1. Liu X, Yang Q, Fan Y, Du Y, Lei L, Wang D, Liu Y. Pharmacokinetics and pharmacodynamics of enrofloxacin treatment of Escherichia coli in a murine thigh infection modeling. BMC Vet Res 2021 Jun 9;17(1):212.
        doi: 10.1186/s12917-021-02908-8pubmed: 34107961google scholar: lookup
      2. Endo Y, Tsuchiya T, Omura T, Nakai K, Korosue K, Ishimaru M, Ishikawa Y, Hobo S. Effects of pre-shipping marbofloxacin administration on fever and blood properties in healthy Thoroughbreds transported a long distance. J Vet Med Sci 2015 Jan;77(1):75-9.
        doi: 10.1292/jvms.14-0336pubmed: 25720808google scholar: lookup
      3. Howard AM, Papich MG, Felt SA, Long CT, McKeon GP, Bond ES, Torreilles SL, Luong RH, Green SL. The pharmacokinetics of enrofloxacin in adult African clawed frogs (Xenopus laevis). J Am Assoc Lab Anim Sci 2010 Nov;49(6):800-4.
        pubmed: 21205443
      4. 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.
        doi: 10.1023/a:1016242812772pubmed: 12212727google scholar: lookup
      5. 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.
        pubmed: 11480524
      6. Yang B, Liu S, Cheng J, Qu H, Guo Y, Ji C, Wang Y, Zhao S, Huang S, Zhao L, Ma Q. Pharmacokinetics of Enrofloxacin in Plasma, Urine, and Feces of Donkey (Equus asinus) after a Single Intragastric Administration. Antibiotics (Basel) 2024 Apr 12;13(4).
        doi: 10.3390/antibiotics13040355pubmed: 38667031google scholar: lookup