title: 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.
authors.affiliation: Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, GA 30602-2352, USA.
authors.forename: I A
authors.initials: IA
authors.lastname: Aljuffali
authors.forename: B M
authors.initials: BM
authors.lastname: Brainard
authors.forename: J N
authors.initials: JN
authors.lastname: Moore
authors.forename: S
authors.initials: S
authors.lastname: Kwon
authors.forename: D
authors.initials: D
authors.lastname: Allen
authors.forename: T P
authors.initials: TP
authors.lastname: Robertson
authors.forename: R D
authors.initials: RD
authors.lastname: Arnold
mesh_terms: D000818:Animals; D019540:Area Under Curve; D005260:Female; D006207:Half-Life; D006736:Horses / Q000097:blood* / Q000378:metabolism; D007650:Ketanserin / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D015394:Molecular Structure; D010975:Platelet Aggregation Inhibitors / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D010975:Platelet Aggregation Inhibitors; D007650:Ketanserin