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Pharmacokinetic assessment of ketanserin in the horse

Authors

  • I. A. ALJUFFALI,

    1. Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, GA, USA
    2. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
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  • B. M. BRAINARD,

    1. Departments of Small Animal, Medicine and Surgery, University of Georgia, Athens, GA, USA
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  • J. N. MOORE,

    1. Large Animal Medicine, University of Georgia, Athens, GA, USA
    2. Physiology and Pharmacology, College of Veterinary Medicine, University of Georgia, Athens, GA, USA
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  • S. KWON,

    1. Large Animal Medicine, University of Georgia, Athens, GA, USA
    2. Physiology and Pharmacology, College of Veterinary Medicine, University of Georgia, Athens, GA, USA
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  • D. ALLEN,

    1. Large Animal Medicine, University of Georgia, Athens, GA, USA
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  • T. P. ROBERTSON,

    1. Large Animal Medicine, University of Georgia, Athens, GA, USA
    2. Physiology and Pharmacology, College of Veterinary Medicine, University of Georgia, Athens, GA, USA
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  • R. D. ARNOLD

    1. Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, GA, USA
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Robert D. Arnold, Department of Pharmaceutical and Biomedical Sciences, University of Georgia, 250 W. Green Street, Room 220, Athens, GA 30602-2352, USA. E-mail: rarnold@rx.uga.edu

Abstract

Aljuffali, I. A., Brainard, B. M., Moore, J. N., Kwon, S., Allen, D., Robertson, T. P., Arnold, R. D. Pharmacokinetic assessment of ketanserin in the horse. J. vet. Pharmacol. Therap35, 472–477.

The purpose of this study was to determine the pharmacokinetics (PK) of the 5-HT2A 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.

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