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Home / Equine Research Bank / Equine Vet J / Pharmacokinetic properties of pergolide mesylate following s...
Equine veterinary journal2022; doi: 10.1111/evj.13917

Pharmacokinetic properties of pergolide mesylate following single and multiple-dose administration in donkeys (Equus asinus).

Abstract: Donkeys with clinical signs of pituitary pars intermedia dysfunction are treated with oral pergolide mesylate despite the lack of species-specific pharmacokinetic data. Objective: To evaluate the pharmacokinetics of intragastric and oral pergolide mesylate in healthy donkeys (Equus asinus). Methods: Pharmacokinetic study. Methods: Six healthy donkeys were administered pergolide mesylate (Prascend®) at 2 μg/kg bodyweight (bwt) intragastrically once, then once daily per os (PO) for 5 days. Blood samples were collected at 0, 10, 20, 30 and 45 min and 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 and 48 h after the single intragastric dose, once daily immediately before the PO dose, and then again at the above times after Day 5 of once daily oral dosing. Plasma pergolide concentration was quantified via ultra-performance liquid chromatography-tandem mass spectrometry. Pergolide concentration versus time data after the first and last doses were analysed based on noncompartmental pharmacokinetics using commercial software. Paired t-tests were used to compare single and multiple doses (p < 0.05). In a follow-up study, a single oral dose was then administered to two donkeys followed by concurrent blood sampling from the jugular and cephalic veins to evaluate the effect of route of administration on pergolide pharmacokinetics. Results: C , T AUC, and t differed significantly (p ≤ 0.03) after single and multiple doses, with significantly lower C (0.16 ± 0.16 ng/ml) and t (9.74 ± 1.35 h) after intragastric dosing on Day 1 than after 5 days of oral dosing (3.74 ± 2.26 ng/ml and 16.35 ± 5.21 h, respectively). Pergolide plasma concentrations were higher in jugular vein samples compared to cephalic vein samples after a single oral dose. Conclusions: Small sample size; varied administration routes. Conclusions: Pergolide mesylate (dosed at 2 μg/kg bwt) is bioavailable in donkeys after intragastric and PO administration. Differences in pharmacokinetics were noted after multiple doses, related to different routes of administration and sublingual absorption of pergolide.
© 2022 The Authors. Equine Veterinary Journal published by John Wiley & Sons Ltd on behalf of EVJ Ltd.
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Publication Date: 2022-12-26 PubMed ID: 36572900DOI: 10.1111/evj.13917Google Scholar: Lookup
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  • 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 researchers investigated how pergolide mesylate, a drug used to treat certain disorders in donkeys, is metabolized and absorbed in the species. After administering single and multiple doses through different methods, they found that the drug is indeed bioavailable in donkeys, and that its pharmacokinetics vary depending on the route of administration and repeated exposure.

Objective and Methodology

  • The main goal was to understand how pergolide mesylate, specifically Prascend® brand, is absorbed, metabolized, and excreted in healthy donkeys. This drug is often given to donkeys showing signs of pituitary pars intermedia dysfunction, but no pharmacokinetic data specific to donkeys are currently available.
  • The research was done with six healthy donkeys administered with 2 μg/kg bodyweight pergolide mesylate once through intragastric injection and daily through oral ingestion for five days.
  • Blood samples were taken at specified intervals before, during, and after treatment to measure the concentration of the drug in the plasma. The concentration was measured through ultra-performance liquid chromatography-tandem mass spectrometry.

Results and Conclusions

  • Pharmacokinetic values such as maximum concentration, time to reach maximum concentration, area under the concentration-time curve, and half-life showed significant differences after single and multiple doses. The differences show how the route of administration and the number of dosages can affect the drug’s pharmacokinetics.
  • After the initial intragastric injection, plasma pergolide concentration and half-life were found to be lower than after five days of oral administration. The observed increase after multiple oral doses suggests that the drug might accumulate in the body over time.
  • There was a noted difference between plasma concentrations in the jugular vein and the cephalic vein after oral administration, indicating that the drug’s absorption and distribution might also depend on the sampling site.
  • In conclusion, the research confirmed that pergolide mesylate is bioavailable in donkeys both when given intragastrically and orally. Moreover, multiple doses and the drug administration route were found to have a significant impact on pergolide mesylate’s pharmacokinetics in donkeys.

Cite This Article

APA
Xue C, Davis J, Berghaus LJ, Hanafi A, Vaughn SA, Hart KA. (2022). Pharmacokinetic properties of pergolide mesylate following single and multiple-dose administration in donkeys (Equus asinus). Equine Vet J. https://doi.org/10.1111/evj.13917

Publication

Equine veterinary journal
ISSN: 2042-3306
NlmUniqueID: 0173320
Country: United States
Language: English

Researcher Affiliations

Xue, Cynthia
  • Department of Large Animal Medicine, University of Georgia College of Veterinary Medicine, Athens, Georgia, USA.
Davis, Jennifer
  • Department of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Blacksburg, Virginia, USA.
Berghaus, Londa J
  • Department of Large Animal Medicine, University of Georgia College of Veterinary Medicine, Athens, Georgia, USA.
Hanafi, Amanda
  • Department of Large Animal Medicine, University of Georgia College of Veterinary Medicine, Athens, Georgia, USA.
Vaughn, Sarah A
  • Department of Large Animal Medicine, University of Georgia College of Veterinary Medicine, Athens, Georgia, USA.
Hart, Kelsey A
  • Department of Large Animal Medicine, University of Georgia College of Veterinary Medicine, Athens, Georgia, USA.

Grant Funding

  • College of Veterinary Medicine, University of Georgia

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