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Journal of veterinary pharmacology and therapeutics1997; 20(3); 204-208; doi: 10.1111/j.1365-2885.1997.tb00096.x

Pharmacokinetic study of dipyrone metabolite 4-MAA in the horse and possible implications for doping control.

Abstract: The pharmacokinetic behaviour of dipyrone metabolite 4-MAA in serum was determined in seven horses of different breeds after a single intravenous dose administration. A biexponential formula was fitted to the serum concentration vs. time data. The median half-life of the elimination phase (t1/2 beta) was 4.85 h (range 5.04 h), the median volume of distribution (Vd(area)) was 1.85 L/kg (range 3.2 L/kg) and median of total clearance was 4.0 mL/min/kg (range 2.3 mL/min/kg).
Publication Date: 1997-06-01 PubMed ID: 9185086DOI: 10.1111/j.1365-2885.1997.tb00096.xGoogle Scholar: Lookup
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  • Journal Article

Summary

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The research explores the pharmacokinetic behaviour of the metabolite 4-MAA, a byproduct of dipyrone, in horses after a single dose. It also discusses its implications for doping control.

Overview of Research

  • This study was conducted to determine the pharmacokinetic behavior of 4-MAA, a metabolite of dipyrone, in horses.
  • The research was focused on seven horses of various breeds that were given a single intravenous dose of the substance.
  • The serum concentration vs. time data was then analyzed using a biexponential formula to draw conclusions.

Results of the Study

  • The analysis showed that the median half-life of the elimination phase (t1/2 beta) was 4.85 hours, with a range of 5.04 hours. The half-life of a drug is the time it takes for the concentration of the drug in the body to be reduced by half. This suggests that the drug is eliminated relatively quickly from the horse’s system.
  • The median volume of distribution (Vd(area)) was 1.85 L/kg, with a range of 3.2 L/kg. The volume of distribution refers to how widely a drug disperses in the body tissues. A higher volume of distribution shows that drug spreads widely through the body’s tissues.
  • The median of total clearance was 4.0 mL/min/kg, with a range of 2.3 mL/min/kg. Clearance refers to the body’s efficiency in eliminating the drug. Higher values would indicate a higher efficiency in drug elimination.

Implications for Doping Control

  • The pharmacokinetic data of 4-MAA in horses is important because it can be used to establish accurate and effective doping control strategies.
  • The data about the half-life, volume of distribution, and clearance can help in determining how long the dipyrone metabolite remains detectable in the horse’s body. This can assist in developing strategies to ensure fair competition in horse racing.

Cite This Article

APA
Klaus AM, Schlingloff Y, Kleinitz U, Böttcher M, Hapke HJ. (1997). Pharmacokinetic study of dipyrone metabolite 4-MAA in the horse and possible implications for doping control. J Vet Pharmacol Ther, 20(3), 204-208. https://doi.org/10.1111/j.1365-2885.1997.tb00096.x

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 20
Issue: 3
Pages: 204-208

Researcher Affiliations

Klaus, A M
  • Institut für Pharmakologie, Toxikologie und Pharmazie, Tierärztliche Hochschule Hannover, Germany.
Schlingloff, Y
    Kleinitz, U
      Böttcher, M
        Hapke, H J

          MeSH Terms

          • Animals
          • Anti-Inflammatory Agents, Non-Steroidal / metabolism
          • Area Under Curve
          • Dipyrone / analogs & derivatives
          • Dipyrone / blood
          • Dipyrone / metabolism
          • Dipyrone / pharmacokinetics
          • Doping in Sports
          • Female
          • Gas Chromatography-Mass Spectrometry
          • Half-Life
          • Horses / blood
          • Horses / metabolism
          • Male
          • Metabolic Clearance Rate
          • Pyrazolones

          Citations

          This article has been cited 2 times.
          1. Mercer MA, Davis JL, McKenzie HC. The Clinical Pharmacology and Therapeutic Evaluation of Non-Steroidal Anti-Inflammatory Drugs in Adult Horses.. Animals (Basel) 2023 May 10;13(10).
            doi: 10.3390/ani13101597pubmed: 37238029google scholar: lookup
          2. Trindade PHE, Taffarel MO, Luna SPL. Spontaneous Behaviors of Post-Orchiectomy Pain in Horses Regardless of the Effects of Time of Day, Anesthesia, and Analgesia.. Animals (Basel) 2021 May 31;11(6).
            doi: 10.3390/ani11061629pubmed: 34072875google scholar: lookup