Studies in rabbits on the disposition and trypanocidal activity of the antitrypanosomal drug, diminazene aceturate (Berenil)

Abstract

After intramuscular injection of 3.5 mg kg−1 to rabbits, diminazene aceturate shows biphasic pharmacokinetics with maximum blood and interstitial fluid concentrations occurring after 15 min and 3 h respectively. Seven days after treatment, 40–50% of the dose had been excreted in the urine and 8–20% in faeces. Highest diminazene residues were determined in liver: 7 days after dosage, residues of 40.53 ± 4.00 μg−1 were present, corresponding to 35–50% of the dose. The recommended dose of 3.5 mg kg−1 was not curative for Trypanosoma congolense infections of rabbit but did cause the parasitaemia to become subpatent. A limited prophylactic effect was observed. 1983 British Pharmacological Society