Pharmacokinetics of diminazene in sheep

Publisher Website
Google Scholar
Abstract
The pharmacokinetic behavior of diminazene in plasma after administration of 2 mg/kg i.v. and 3.5 mg/kg i.m. was studied in four healthy Dala × Ryggja rams. Following i.v. injection, the data were satisfactorily described by a triexponential equation; the apparent volume of distribution at the steady-state was 0.56±0.04 L/Kg (X±sd; n=4); total body clearance averaged 1.1±0.09 ml/kg/min and elimination half-life was 9.30±1.40 hr. After intramuscular administration peak plasma levels of 6.30–7.57 μg/ml were reached in 20 to 45 min and the mean absorption time averaged 5.83±1.61 hr. Systemic availability relative to the intravenous dose was 95.10±23.21% and mean residence time averaged 14.16±1.55hr. The partition of diminazene between erythrocytes and plasma averaged 0.64±0.10; plasma protein binding was high (65–85%) and concentration-dependent. Based on the experimental data obtained, an initial i.m. dose of 2.5 mg/kg followed by 2 mg/kg 24 hr later should be safe and effective in cases of babesiosis and trypanosomiasis sensitive to diminazene. A preslaughter withdrawal period of 14–26 days was estimated.