Studies in rabbits on the disposition and trypanocidal activity of the anti-trypanosomal drug, diminazene aceturate (Berenil).
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 micrograms g-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.
D000578:Amidines / Q000378:metabolism*; D000818:Animals; D004133:Diminazene / Q000031:analogs & derivatives / Q000378:metabolism* / Q000627:therapeutic use; D007700:Kinetics; D011817:Rabbits; D014018:Tissue Distribution; D014353:Trypanosomiasis, African / Q000188:drug therapy
D000578:Amidines; C003915:diminazene aceturate; D004133:Diminazene