Abstract
The pharmacokinetics of diminazene aceturate following intramuscular (i.m.) administration at 4.2 mg/kg was evaluated in 8 healthy German Shepherd dogs. Blood samples were collected at 19 intervals over a period of 21 days. Diminazene plasma concentrations were measured using a validated HPLC method with UV detection and a sensitivity of 25 ng/ml. The in vitro and in vivo binding of diminazene to blood elements was additionally determined. Diminazene pharmacokinetics showed a large inter-individual variation after i.m. administration. It had a short absorption half-life (K01-HL of 0.11 +/- 0.18 h), resulting in a C(max) of 1849 +/- 268.7 ng/ml at T(max) of 0.37 h and a mean overall elimination half-life (T1/2beta) of 5.31 +/- 3.89 h. A terminal half-life of 27.5 +/- 25.0 h was measured. At 1 h after i.m. injection, 75% of the diminazene in whole blood was in the plasma fraction. The results of this study indicate that diminazene is rapidly distributed and sequestered into the liver, followed by a slower terminal phase during which diminazene is both redistributed to the peripheral tissues and/or renally excreted. It is recommended that diminazene administered i.m. at 4.2 mg/kg should not be repeated within a 21-day period.
Highlights
Diminazene is the antibabesial drug of choice for the treatment of canine babesiosis in South Africa[5]
Diminazene is most likely first sequestered in the liver, is slowly released back into the central compartment and redistributed into less well perfused peripheral tissues before being eliminated
The slower redistribution to and from these peripheral tissues is likely to be mainly responsible for the longer elimination half-life of diminazene as measured by non-compartmental analysis
Summary
Diminazene is the antibabesial drug of choice for the treatment of canine babesiosis in South Africa[5]. Differences in the dosage described for diminazene and the occurrence of mortality at doses equal to or close to the recommended therapeutic dose for the treatment of canine babesiosis have been described[14,17,18,22,25]. The diminazene products used to treat babesiosis in South Africa contain a combination of diminazene aceturate and antipyrine, mostly in a concentration of 45 % m/m and 55 % m/m, respectively. Babesia canis is a tick-transmitted intraerythrocytic protozoan parasite responsible for high morbidity and mortality among dogs in South Africa[23]. In 1955, Fussgänger aDepartment of Companion Animal Studies and bDepartment of Paraclinical Sciences, Faculty of Veterinary Science, University of Pretoria, Private Bag X04, Onderstepoort, 0110 South Africa
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