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Disposition and excretion of flunixin meglumine in horses.

Abstract: The disposition of flunixin meglumine administered IV at a dosage of 1.1 mg/kg was described by a 2-compartment model; the alpha and beta half-lives (t1/2) were 0.61 and 1.5 hours, respectively. When administered IV at a rate of 2.2 mg/kg, the disposition was best described by a 3-compartment model, and the alpha, beta, and lambda t1/2 were 0.16, 1.52, and 6.00 hours, respectively. The zero-time plasma concentrations after flunixin meglumine was administered at 1.1 and 2.2 mg/kg were 9.3 +/- 0.76 and 21.5 +/- 7.4 mg/L, respectively. The bioavailability after oral administration of 1.1 mg/kg was 85.8%. The absorption t1/2 was 0.57 hours, with a peak concentration of 2.50 +/- 1.25 mg/L. The cumulative urinary recoveries for IV and oral administrations were 61.0% and 63.3%, respectively, of the dose for the 12-hour collection period. The final asymptotic points of urine excretion after IV and oral administrations were 406.4 +/- 65.5 and 357.7 +/- 53.5 mg, respectively, which represented 75.5 and 77.5% of the drug accounted for between 30 and 35 hours after administration. Flunixin meglumine was rapidly excreted in urine over a 2- to 4-hour period after drug administration and was highly bound to protein in plasma.
Publication Date: 1988-11-01 PubMed ID: 3247913
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research article discusses the disposition and excretion of the drug flunixin meglumine in horses. It explores how varying doses of the drug administered intravenously and orally are absorbed, distributed, and eliminated from the body, and how long it takes for the drug to reach its maximum concentration after administration.

Setting and Methodology

  • The study investigated the pharmacokinetics of flunixin meglumine, a nonsteroidal anti-inflammatory drug (NSAID) often used in horses to treat pain and inflammation.
  • The drug was administered to horses either intravenously (IV) at two different dosages, 1.1 mg/kg and 2.2 mg/kg, or orally at a dosage of 1.1 mg/kg.
  • The researchers used both a two-compartment and three-compartment model to describe the disposition of the drug when administered IV, where the compartments likely represent various parts of the body interacting with the drug (such as the blood, tissue, and organs).
  • The study also evaluated how much of the drug was eliminated through the urine by measuring urinary recoveries after administration.

Findings

  • The IV administration of flunixin meglumine at 1.1 mg/kg could be described by a two-compartment model with half-lives of 0.61 and 1.5 hours.
  • When the dosage was increased to 2.2 mg/kg IV, a three-compartment model was deemed more appropriate, with half-lives of 0.16, 1.52, and 6.00 hours.
  • A significant proportion of the drug was bound to protein in plasma, suggesting a potential high level of distribution within the body.
  • The bioavailability of the drug – how much of it enters the circulation when introduced orally – was found to be 85.8%.
  • The drug was excreted quite rapidly, reaching its peak concentration in urine 2 to 4 hours after administration. Cumulative urinary recoveries for IV and oral administrations were 61.0% and 63.3% respectively.

Implications

  • The study provides important information about how flunixin meglumine is handled by the body of horses, which can help in determining appropriate dosage and frequency of administration.
  • The findings show that flunixin meglumine is rapidly eliminated from the body, and most of the dose is excreted through the urine, which could be taken into account when using the drug in practice.
  • The higher bioavailability after oral administration suggests that this route of administration is nearly as effective as IV administration.

Cite This Article

APA
Soma LR, Behrend E, Rudy J, Sweeney RW. (1988). Disposition and excretion of flunixin meglumine in horses. Am J Vet Res, 49(11), 1894-1898.

Publication

ISSN: 0002-9645
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 49
Issue: 11
Pages: 1894-1898

Researcher Affiliations

Soma, L R
  • School of Veterinary Medicine, New Bolton Center, University of Pennsylvania, Kennett Square 19348-1692.
Behrend, E
    Rudy, J
      Sweeney, R W

        MeSH Terms

        • Administration, Oral
        • Animals
        • Biological Availability
        • Clonixin / administration & dosage
        • Clonixin / analogs & derivatives
        • Clonixin / pharmacokinetics
        • Clonixin / urine
        • Female
        • Glomerular Filtration Rate
        • Horses / metabolism
        • Injections, Intravenous / veterinary
        • Nicotinic Acids / pharmacokinetics
        • Protein Binding
        • Regression Analysis

        Citations

        This article has been cited 4 times.
        1. Knych HK, Katzman S, McKemie DS, Arthur RM, Blea J. Pharmacokinetics and metabolism of lidocaine HCl 2% with epinephrine in horses following a palmar digital nerve block. BMC Vet Res 2023 Oct 30;19(1):225.
          doi: 10.1186/s12917-023-03787-xpubmed: 37904169google scholar: lookup
        2. Kuroda T, Minamijima Y, Nomura M, Yamashita S, Yamada M, Nagata S, Mita H, Tamura N, Fukuda K, Kuwano A, Kusano K, Toutain PL, Sato F. Medication control of flunixin in racing horses: Possible detection times using Monte Carlo simulations. Equine Vet J 2022 Sep;54(5):979-988.
          doi: 10.1111/evj.13532pubmed: 34719043google scholar: lookup
        3. Nixon E, Mays TP, Routh PA, Yeatts JL, Fajt VR, Hairgrove T, Baynes RE. Plasma, urine and tissue concentrations of Flunixin and Meloxicam in Pigs. BMC Vet Res 2020 Sep 16;16(1):340.
          doi: 10.1186/s12917-020-02556-4pubmed: 32938437google scholar: lookup
        4. Pairis-Garcia MD, Karriker LA, Johnson AK, Kukanich B, Wulf L, Sander S, Millman ST, Stalder KJ, Coetzee JF. Pharmacokinetics of flunixin meglumine in mature swine after intravenous, intramuscular and oral administration. BMC Vet Res 2013 Aug 13;9:165.
          doi: 10.1186/1746-6148-9-165pubmed: 23941181google scholar: lookup