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Equine veterinary journal. Supplement1992; (11); 69-72; doi: 10.1111/j.2042-3306.1992.tb04778.x

Pharmacokinetics of tolfenamic acid in the horse.

Abstract: The pharmacokinetics of tolfenamic acid were studied in five ponies after an intravenous (iv) administration (2 mg/kg bodyweight [bwt]) and in four horses after an oral administration (30 mg/kg bwt) of tolfenamic acid. The plasma levels were determined by high pressure liquid chromatography (HPLC) and gas chromatography-mass spectrometry (GC-MS). For the iv administration, a three-compartment model was used to represent the plasma concentration-time curve of the drug. The elimination half-life of the compound was 6.1 +/- 1.5 h, the total body clearance was 72.4 +/- 16.7 ml/kg bwt/h and the steady-state volume of distribution 0.32 +/- 0.11 litres/kg bwt. For the oral administration, absorbtion was delayed with a mean lag-time to absorption of 32 +/- 28 mins. The peak plasma concentration 11.1 +/- 0.69 micrograms/ml was observed after a highly variable delay ranging from 1.9 to 6.5 h post administration. The terminal half-life (4.2 +/- 0.48 h) was very similar to that obtained after iv administration. Tolfenamic acid could not be detected in equine plasma with the described analytical methods more than 48 h after drug administration.
Publication Date: 1992-02-01 PubMed ID: 9109966DOI: 10.1111/j.2042-3306.1992.tb04778.xGoogle Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research investigated how horses absorb, distribute, metabolize and eliminate a drug called tolfenamic acid. The study found that the drug was quickly absorbed regardless of being delivered via intravenous or oral administration, but its complete elimination from the horse’s body took upwards of 48 hours.

Introduction

  • The study focuses on understanding the pharmacokinetics of tolfenamic acid in ponies and horses. Pharmacokinetics is the branch of pharmacology focused on the movement of drugs within the body, which includes absorption, distribution, metabolism, and excretion.
  • Tolfenamic acid is an anti-inflammatory medication commonly used in veterinary medicine for its analgesic and antipyretic properties.

Methodology

  • The study was performed on five ponies intravenously administered tolfenamic acid (2 mg/kg bodyweight), and on four horses orally administered the same drug (30 mg/kg bodyweight).
  • The researchers measured the plasma (the clear, non-cellular part of blood) levels of the drug using two methods: high pressure liquid chromatography (HPLC) and gas chromatography-mass spectrometry (GC-MS).
  • For the intravenously administered ponies, the researchers used a three-compartment model, a mathematical model commonly used in pharmacokinetics, to describe the drug’s concentration-time curve in the plasma.

Results

  • The study found that the elimination half-life of the tolfenamic acid, which is the time it takes for the body to reduce the amount of drug in the plasma by half, averaged 6.1 hours (with a variation of 1.5 hours).
  • The total body clearance, a measure of the body’s efficiency in eliminating the drug, was calculated to be 72.4 ml/kg bodyweight/hour.
  • The steady-state volume of distribution, an indicator of how widely the drug is distributed throughout the body, was 0.32 liters/kg bodyweight.
  • For the orally administered horses, the drug was absorbed at a slower rate, with a mean time to absorption of 32 minutes. The elapsed time from drug administration to achieving the highest concentration in the plasma was variable, ranging from 1.9 to 6.5 hours after administration.
  • The terminal half-life after oral administration was similar to that of intravenous administration, averaging around 4.2 hours.
  • Using the described analytical methods, tolfenamic acid could not be detected in equine plasma more than 48 hours post-administration, indicating it had been fully metabolized and eliminated from the body.

Implications

  • The findings of this study provide valuable insights into the pharmacokinetics of tolfenamic acid in horses, which can guide optimal dosing strategies for veterinary use.
  • The observed similarities in the half-life of the drug with both delivery methods also suggest that repeated dosing may not be necessary for maintaining effective therapeutic levels in the body.

Cite This Article

APA
Jaussaud P, Guieu D, Bellon C, Barbier B, Lhopital MC, Sechet R, Courtot D, Toutain PL. (1992). Pharmacokinetics of tolfenamic acid in the horse. Equine Vet J Suppl(11), 69-72. https://doi.org/10.1111/j.2042-3306.1992.tb04778.x

Publication

NlmUniqueID: 9614088
Country: United States
Language: English
Issue: 11
Pages: 69-72

Researcher Affiliations

Jaussaud, P
  • INRA-ENVL Research Laboratory for Equine Sport, National School of Veterinary Medicine, Marcy I'Etoile, France.
Guieu, D
    Bellon, C
      Barbier, B
        Lhopital, M C
          Sechet, R
            Courtot, D
              Toutain, P L

                MeSH Terms

                • Animals
                • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
                • Anti-Inflammatory Agents, Non-Steroidal / blood
                • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
                • Blood Specimen Collection / veterinary
                • Chromatography, High Pressure Liquid
                • Dose-Response Relationship, Drug
                • Female
                • Half-Life
                • Horses / metabolism
                • Injections, Intravenous
                • Male
                • Reproducibility of Results
                • ortho-Aminobenzoates / administration & dosage
                • ortho-Aminobenzoates / blood
                • ortho-Aminobenzoates / pharmacokinetics

                Citations

                This article has been cited 1 times.
                1. Fadel C, Giorgi M. Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses.. Vet Anim Sci 2023 Mar;19:100286.
                  doi: 10.1016/j.vas.2023.100286pubmed: 36684818google scholar: lookup