Pharmacokinetics and sedative effects of intramuscular medetomidine in domestic sheep

Intramuscular (i.m.) administration of medetomidine (MED) may avoid the severe pressor effects caused by peripheral actions of MED associated with intravenous (i.v.) dosing. The purpose of this study was to determine the pharmacokinetics, the time course of sedation and occurence of hypoxaemia after i.m. administration of MED in domestic sheep. The MED was injected i.m. at a dose of 30 micro g/kg in nine domestic sheep. Blood was sampled at 0, 5, 10, 20, 30, 40, 60, 120, 180, 240, 360 and 600 min after MED. Sedation was assessed and arterial blood samples were taken before and 35 min after MED application. Mean (SD) pharmacokinetic parameters of i.m. MED were: absorption half-life: 13.2 (7.5) min; terminal half-life: 32.7 (14.9) min; time to peak concentration: 29.2 (8.9) min; peak concentration: 4.98 (1.89) ng/mL; volume of distribution: 3.9 (2.4) l/kg; total body clearance: 81.0 (21.5) mL/(min kg). Peak sedation occurred between 30 and 40 min after injection of MED. The degree of sedation correlated with individual plasma concentrations (rS: 0.926). One animal became hypoxaemic (PaO2 = 54.1 mmHg).