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Journal of veterinary pharmacology and therapeutics2011; 35(5); 472-477; doi: 10.1111/j.1365-2885.2011.01346.x

Pharmacokinetic assessment of ketanserin in the horse.

Abstract: The purpose of this study was to determine the pharmacokinetics (PK) of the 5-HT(2A) receptor antagonist ketanserin in healthy adult horses, and to develop a computational model that could be used to optimize dosing. Plasma concentrations of ketanserin were determined using liquid chromatography with mass spectrometry after single and multiple intravenous administration in the horse. A two-compartment linear pharmacokinetic model described the plasma concentration-time profile of ketanserin after single and multiple doses in healthy horses; the terminal half-life was 11.5 h; steady-state volume of distribution was 10.5 L/kg; AUC was 115 ng · h/mL; and clearance was 0.87 L/h/kg. Model simulations followed by the examination in three healthy horses suggest 0.3 mg/kg q.8 h exhibited linear PK and produced consistent systemic blood concentrations of ketanserin above 3 ng/mL.
Publication Date: 2011-11-18 PubMed ID: 22091605DOI: 10.1111/j.1365-2885.2011.01346.xGoogle Scholar: Lookup
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  • Clinical Trial
  • Journal Article
  • Research Support
  • Non-U.S. Gov't

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 research studies the movement and effects of the drug ketanserin in horses, with the researchers using a computer model to optimize dosage. The conclusions were reached using both single and multiple doses.

Study Objective

  • The primary objective of this study involved understanding the pharmacokinetics, that is, the movement of the drug ketanserin, within the body of a healthy horse. The scientists aimed to create a mathematical model that would aid in determining optimal dosage.

Methods Used

  • The researchers measured plasma concentrations of ketanserin in the horses’ blood, utilizing liquid chromatography coupled with mass spectrometry. This approach was applied following both single and multiple intravenous applications.

Findings

  • Upon reviewing the concentration-time profile for plasma levels of ketanserin, a two-compartment linear pharmacokinetic model was found to best represent the data, following single and consecutive doses in healthy horses.
  • Various pharmacokinetic parameters were identified, including an 11.5-hour terminal half-life for ketanserin, a steady-state volume of distribution at 10.5L/kg, and clearance at a rate of 0.87 L/h/kg.
  • The study also identified the Area Under the Curve (AUC – a metric representing total drug exposure over time) as 115 ng·h/mL – a value that stands out when assessing the drug’s overall exposure.

Simulations and Validation

  • An examination of three healthy horses suggested a dose of 0.3 mg/kg given every 8 hours was apt. This was established based on linear pharmacokinetics in the horses sampled and offered a stable systemic blood concentration of the drug over 3 ng/mL. Thus, a predictive model was created for vet practitioners to employ this drug effectively.

It’s important to note, however, that these findings are based on a small sample size, and more extensive studies are necessary for better substantiation.

Cite This Article

APA
Aljuffali IA, Brainard BM, Moore JN, Kwon S, Allen D, Robertson TP, Arnold RD. (2011). Pharmacokinetic assessment of ketanserin in the horse. J Vet Pharmacol Ther, 35(5), 472-477. https://doi.org/10.1111/j.1365-2885.2011.01346.x

Publication

ISSN: 1365-2885
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 35
Issue: 5
Pages: 472-477

Researcher Affiliations

Aljuffali, I A
  • Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, GA 30602-2352, USA.
Brainard, B M
    Moore, J N
      Kwon, S
        Allen, D
          Robertson, T P
            Arnold, R D

              MeSH Terms

              • Animals
              • Area Under Curve
              • Female
              • Half-Life
              • Horses / blood
              • Horses / metabolism
              • Ketanserin / blood
              • Ketanserin / chemistry
              • Ketanserin / pharmacokinetics
              • Molecular Structure
              • Platelet Aggregation Inhibitors / blood
              • Platelet Aggregation Inhibitors / chemistry
              • Platelet Aggregation Inhibitors / pharmacokinetics

              Citations

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