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American journal of veterinary research2015; 76(2); 155-160; doi: 10.2460/ajvr.76.2.155

Pharmacokinetics of pergolide after intravenous administration to horses.

Abstract: To determine the pharmacokinetics of pergolide after IV administration to horses. Methods: 8 healthy adult horses. Methods: Pergolide mesylate was administered IV at a dose of 20 μg/kg (equivalent to 15.2 μg of pergolide/kg) to each horse, and blood samples were collected over 48 hours. Pergolide concentrations in plasma were determined by means of high-performance liquid chromatography-tandem mass spectrometry, and pharmacokinetic parameters were determined on the basis of noncompartmental methods. Results: After IV administration of pergolide, mean ± SD clearance, elimination half-life, and initial volume of distribution were 959 ± 492 mL/h/kg, 5.64 ± 2.36 hours, and 0.79 ± 0.32 L/kg, respectively. Conclusions: With an elimination half-life of approximately 6 hours, twice-daily dosing may be more appropriate than once-daily dosing to reduce peak-trough fluctuation in pergolide concentrations. Further pharmacodynamic and pharmacokinetic studies of pergolide and its metabolites will be necessary to determine plasma concentrations that correlate with clinical effectiveness to determine the therapeutic range for the treatment of pituitary pars intermedia dysfunction.
Publication Date: 2015-01-30 PubMed ID: 25629913DOI: 10.2460/ajvr.76.2.155Google Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research article investigates how the drug pergolide, once administered intravenously, behaves within the body of a horse. The study monitors the drug’s clearance rate, elimination half-life, and distribution volume, ultimately suggesting a twice-daily dosing schedule for more consistent pergolide concentrations.

Methodology and Samples

  • In this study, eight healthy adult horses were chosen as subjects.
  • The researchers administered an intravenous dose of pergolide mesylate, equivalent to 20 μg/kg (or 15.2 μg of pergolide/kg) to each horse.
  • Following administration, blood samples were gathered at regular time intervals over a span of 48 hours.
  • The plasma concentration of pergolide was then assessed using a high-performance liquid chromatography-tandem mass spectrometry technique.
  • Pharmacokinetic parameters were ascertained using non-compartmental methods.

Summary of Results

  • After the horses were given an intravenous (IV) dose of pergolide, the mean clearance, elimination half-life, and initial volume of distribution were monitored.
  • The study found that the clearance rate of pergolide was 959 ± 492 mL/h/kg on average.
  • The elimination half-life, the time it takes for the body to clear half of the drug, was approximately 5.64 ± 2.36 hours.
  • The initial volume of distribution, a measure of how the drug spreads throughout the body, was roughly 0.79 ± 0.32 L/kg.

Conclusions and Recommendations

  • Given pergolide’s elimination half-life of approximately 6 hours, it is recommended to administer the drug twice daily rather than once to reduce peak-trough fluctuations in the drug’s concentration.
  • However, more extensive pharmacodynamic and pharmacokinetic studies on pergolide and its metabolites are required in order to ascertain the plasma concentrations that correlate with the drug’s clinical effectiveness.
  • These further studies would contribute towards discerning the therapeutic range of pergolide for treating pituitary pars intermedia dysfunction, a common endocrine disorder in horses.

Cite This Article

APA
Rendle DI, Hughes KJ, Doran GS, Edwards SH. (2015). Pharmacokinetics of pergolide after intravenous administration to horses. Am J Vet Res, 76(2), 155-160. https://doi.org/10.2460/ajvr.76.2.155

Publication

ISSN: 1943-5681
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 76
Issue: 2
Pages: 155-160

Researcher Affiliations

Rendle, David I
  • School of Animal and Veterinary Sciences, Charles Sturt University, Wagga Wagga, NSW 2650, Australia.
Hughes, Kris J
    Doran, Gregory S
      Edwards, Scott H

        MeSH Terms

        • Administration, Intravenous
        • Animals
        • Chromatography, Liquid / veterinary
        • Dopamine Agonists / administration & dosage
        • Dopamine Agonists / blood
        • Dopamine Agonists / pharmacokinetics
        • Horses / metabolism
        • Male
        • Pergolide / administration & dosage
        • Pergolide / blood
        • Pergolide / pharmacokinetics
        • Tandem Mass Spectrometry / veterinary

        Citations

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