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Home / Equine Research Bank / J Vet Pharmacol Ther / Pharmacokinetics, metabolism and excretion of celecoxib, a s...
Journal of veterinary pharmacology and therapeutics2019; 42(5); 518-524; doi: 10.1111/jvp.12757

Pharmacokinetics, metabolism and excretion of celecoxib, a selective cyclooxygenase-2 inhibitor, in horses.

Abstract: Celecoxib, a nonsteroidal anti-inflammatory drug, is frequently used to treat arthritis in humans with minimal gastrointestinal side effect compared to traditional NSAIDs. The primary aim of this study was to determine the pharmacokinetic profile of celecoxib-a selective cyclooxygenase-2 (COX-2) inhibitor in horses. Six horses were administered a single oral dose of celecoxib at 2 mg/kg (body weight). After oral dosing, the drug reached a maximum concentration (mean ± SD) in blood of 1,088 ± 324 ng/ml in 4.58 hr. The elimination half-life was 13.60 ± 3.18 hr, and the area under the curve was 24,142 ± 1,096 ng hr ml . The metabolism of celecoxib in horses was via a single oxidative pathway in which the methyl group of celecoxib is oxidized to a hydroxymethyl metabolite and is further oxidized to form a carboxylic acid metabolite. Celecoxib is eliminated mainly through faeces as unchanged drug and as metabolites in urine. Therefore, instructions for a detection time following therapeutic dosing of celecoxib can be set by the racing practitioner and veterinarians to control illegal use in horse racing based on the results of this study.
© 2019 John Wiley & Sons Ltd.
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Publication Date: 2019-03-19 PubMed ID: 30888074DOI: 10.1111/jvp.12757Google Scholar: Lookup
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  • Clinical Trial
  • Veterinary
  • Journal Article

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

The research study focuses on understanding how the drug celecoxib, commonly used for treating arthritis in humans, is absorbed, metabolized, and excreted in horses.

Objective and Approach of the Study

  • The primary objective of this research was to determine the pharmacokinetics, or the movement, of celecoxib in horses. This includes how the drug is absorbed, distributed, metabolized, and eliminated from the horse’s body.
  • A pharmacokinetic analysis provides precise information about how the drug impacts an organism over a particular period.
  • The researchers administered a single oral dose of celecoxib to six horses and observed and analyzed the concentration over time.

Key Findings

  • The drug reached its maximum blood concentration approximately 4.58 hours after the dosage. The average blood concentration was 1088 ng/ml.
  • The pharmacokinetic profile analysis revealed that celecoxib has an elimination half-life of approximately 13.60 hours.
  • The area under the curve (a measure indicating the overall drug exposure over the time) was around 24,142 ng hr ml.

Metabolism and Excretion Processes

  • The study discovered that horses metabolize celecoxib in a single oxidative pathway. Specifically, the methyl group of celecoxib is oxidized to a hydroxymethyl metabolite, which is further oxidized to create a carboxylic acid metabolite.
  • Excretion occurs primarily through faeces as unchanged drug and metabolites in urine.

Implications for Horse Racing

  • Knowing the pharmacokinetics of celecoxib helps racing practitioners and veterinarians establish the detection time for therapeutic usage of the drug, serving as a measure against its illegal use in horse racing.

Cite This Article

APA
Subhahar MB, Singh J, Albert PH, Kadry AM. (2019). Pharmacokinetics, metabolism and excretion of celecoxib, a selective cyclooxygenase-2 inhibitor, in horses. J Vet Pharmacol Ther, 42(5), 518-524. https://doi.org/10.1111/jvp.12757

Publication

Journal of veterinary pharmacology and therapeutics
ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 42
Issue: 5
Pages: 518-524

Researcher Affiliations

Subhahar, Michael Benedict
  • Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, UAE.
Singh, Jaipaul
  • School of Forensic and Investigative Science, University of Central Lancashire, Preston, UK.
Albert, Peter Henry
  • Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, UAE.
Kadry, Ahmed Mahmoud
  • Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, UAE.

MeSH Terms

  • Animals
  • Area Under Curve
  • Celecoxib / administration & dosage
  • Celecoxib / blood
  • Celecoxib / pharmacokinetics
  • Celecoxib / urine
  • Cyclooxygenase 2 Inhibitors / blood
  • Cyclooxygenase 2 Inhibitors / pharmacokinetics
  • Cyclooxygenase 2 Inhibitors / urine
  • Female
  • Half-Life
  • Horses / blood
  • Horses / urine
  • Male

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Citations

This article has been cited 3 times.
  1. Flood J, Stewart AJ. Non-Steroidal Anti-Inflammatory Drugs and Associated Toxicities in Horses.. Animals (Basel) 2022 Oct 26;12(21).
    doi: 10.3390/ani12212939pubmed: 36359062google scholar: lookup
  2. Jacobs CC, Schnabel LV, McIlwraith CW, Blikslager AT. Non-steroidal anti-inflammatory drugs in equine orthopaedics.. Equine Vet J 2022 Jan 25;54(4):636-48.
    doi: 10.1111/evj.13561pubmed: 35076950google scholar: lookup
  3. Solà J, Menargues À, Homedes J, Salichs M, Serafini MT, Encina G. Comparative In vitro Metabolism of Enflicoxib in Dogs, Rats, and Humans: Main Metabolites and Proposed Metabolic Pathways.. Drug Metab Lett 2021;14(3):206-218.
    doi: 10.2174/1872312814666211209161933pubmed: 34886785google scholar: lookup
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