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. Therap. 35, 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.