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Equine veterinary journal1999; 31(5); 411-416; doi: 10.1111/j.2042-3306.1999.tb03841.x

Disposition and tolerance of suxibuzone in horses.

Abstract: Suxibuzone (SBZ), a nonsteroidal anti-inflammatory drug, was administered to 6 horses at a dose rate of 7.5 mg/kg bwt by intravenous (i.v.) route. Plasma and synovial fluid concentrations of suxibuzone and its main active metabolites, phenylbutazone (PBZ) and oxyphenbutazone (OPBZ), were measured simultaneously by a sensitive and specific high-performance liquid chromatographic method. The pharmacokinetic parameters were determined by noncompartmental analysis. Plasma SBZ concentrations rapidly decreased and were not detectable beyond 20 min after treatment. The parent drug was not detected in any synovial fluid samples. Average maximum plasma concentrations of PBZ (16.43 microg/ml) and OPBZ (2.37 microg/ml) were attained at 0.76 and 7.17 h, respectively. The mean residence time (MRT) of PBZ was 6.96 h in plasma. Oxyphenbutazone plasma concentrations were below those reached by phenylbutazone during the first 12 h after suxibuzone administration, even though its values were detectable for at least 24 h (MRT = 10.65 h). Plasma concentrations of PBZ and OPBZ exceeding EC50 and IC50 of TXB2 and PGE2 were reached by at least 12 h. Synovial fluid concentrations of PBZ and OPBZ were 2.87+/-0.37 microg/ml and 0.97+/-0.08 microg/ml at 9 h after suxibuzone administration and exceeded IC50 of PGE2 for at least this time. In the present study, suxibuzone was well tolerated following i.v. injection.
Publication Date: 1999-10-03 PubMed ID: 10505957DOI: 10.1111/j.2042-3306.1999.tb03841.xGoogle Scholar: Lookup
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Summary

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This study examined the effects of the drug Suxibuzone (SBZ), a non-steroidal anti-inflammatory drug, in horses. The research found that the drug was quickly metabolized and distributed in horses, and was well tolerated even when administered intravenously.

Introduction

In this research study, the scientists were focusing on the nonsteroidal anti-inflammatory drug Suxibuzone (SBZ). This drug was administered to six horses and then the scientists measured the levels of SBZ and its metabolites in the horses’ plasma and synovial fluid.

Methodology

  • The researchers selected six horses and administered the drug Suxibuzone intravenously at a dose rate of 7.5 mg/kg of the horse’s body weight.
  • They then utilized a specialized method known as high-performance liquid chromatography to measure the concentration of SBZ and its metabolites (phenylbutazone or PBZ, and oxyphenbutazone or OPBZ) in both plasma and synovial fluid samples from the horses.
  • A noncompartmental analysis was used to determine the pharmacokinetic parameters or the movement of drugs within the body.

Results

  • The researchers found that after the treatment, the plasma concentrations of SBZ rapidly decreased and were undetectable beyond 20 minutes.
  • The main drug was not detected in any synovial fluid samples – only its metabolites PBZ and OPBZ were found.
  • The average maximum plasma concentrations of PBZ and OPBZ were reached at 0.76 hour and 7.17 hours, respectively. This signifies how fast the SBZ was converted into its active forms inside the horse’s body.
  • The mean residence time, which is the average time a drug stays in the body, was also calculated. PBZ had a mean residence time in plasma of approximately 6.96 hours while OPBZ was detectable for at least 24 hours with a mean residence time of about 10.65 hours.
  • The researchers also observed that plasma concentrations of PBZ and OPBZ exceeded the levels necessary for anti-inflammatory effects (as indicated by EC50 and IC50) at least 12 hours after administering suxibuzone.
  • Additionally, the synovial fluid concentrations of PBZ and OPBZ exceeded the levels necessary for PGE2 inhibition (another marker of anti-inflammatory action) at least 9 hours after administering suxibuzone.
  • Finally, the horses showed no adverse effects or intolerance to the intravenous injection of suxibuzone.

Conclusion

This study concluded that suxibuzone was rapidly metabolized and well tolerated when administered intravenously in horses. This suggests that it could be a safe and effective anti-inflammatory medication for use in this species.

Cite This Article

APA
Jaraiz MV, Rodriguez C, San Andres MD, Gonzalez F, San Andres MI. (1999). Disposition and tolerance of suxibuzone in horses. Equine Vet J, 31(5), 411-416. https://doi.org/10.1111/j.2042-3306.1999.tb03841.x

Publication

ISSN: 0425-1644
NlmUniqueID: 0173320
Country: United States
Language: English
Volume: 31
Issue: 5
Pages: 411-416

Researcher Affiliations

Jaraiz, M V
  • Cátedra de Farmacología, Facultad de Veterinaria, Universidad Complutense de Madrid, Spain.
Rodriguez, C
    San Andres, M D
      Gonzalez, F
        San Andres, M I

          MeSH Terms

          • Animals
          • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
          • Anti-Inflammatory Agents, Non-Steroidal / adverse effects
          • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
          • Area Under Curve
          • Blood Cell Count / veterinary
          • Chromatography, High Pressure Liquid / veterinary
          • Hematocrit / veterinary
          • Horses / metabolism
          • Horses / physiology
          • Indomethacin / blood
          • Indomethacin / pharmacokinetics
          • Injections, Intravenous / veterinary
          • Male
          • Oxyphenbutazone / blood
          • Oxyphenbutazone / pharmacokinetics
          • Phenylbutazone / administration & dosage
          • Phenylbutazone / adverse effects
          • Phenylbutazone / analogs & derivatives
          • Phenylbutazone / blood
          • Phenylbutazone / pharmacokinetics
          • Synovial Fluid / metabolism

          Citations

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