Studies in cattle on the disposition of the anti-trypanosomal drug diminazene diaceturate (Berenil).
After intramuscular injection of ca. 3.5 mg kg-1 diminazene diaceturate-(bis-phenyl-U-14C) to two healthy male calves weighing 185 and 180 kg, levels of radioactivity were determined in blood, plasma, urine, faeces, and in edible tissues. The maximal blood level of 4.6 micrograms and 4.7 micrograms equivalents of diminazene diaceturate ml-1 (calculated from total radioactivity) occurred 15 min (calf C1) and 45 min (calf C2) after administration. The decrease in concentration followed a biphasic process with half lives of 2 and 188 hours. Seven days after treatment 47.1% of the dose had been excreted in the urine and 7.1% in the faeces. The respective values were 72.2% and 10.3% after 20 days. The half lives were similar to those in blood. The main product in urine was unchanged diminazene. Distribution studies showed concentrations which were low in general in edible tissues, i.e. in skeletal musculature and fat (below 1 microgram equivalent g-1), but higher in organs with excretory functions. There were 75.5 micrograms equivalents g-1, corresponding to 22% of the dose, in the liver 7 days after injection. This had decreased to 24.4 micrograms equivalents g-1, corresponding to 15% of the dose, at day 20. Only unchanged deminazene was detected in the liver extracts by thin-layer chromatography. Relay-bioavailability studies showed that the total liver residues were only partially available (mean = 23% of the dose) when fed to rats.
D000578:Amidines / Q000378:metabolism*; D000818:Animals; D001345:Autoradiography; D001682:Biological Availability; D002250:Carbon Radioisotopes; D002417:Cattle / Q000378:metabolism*; D004133:Diminazene / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000097:blood / Q000378:metabolism* / Q000652:urine; D005243:Feces / Q000032:analysis; D006207:Half-Life; D007273:Injections, Intramuscular / Q000662:veterinary; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013997:Time Factors; D014018:Tissue Distribution; D014344:Trypanocidal Agents / Q000097:blood / Q000378:metabolism* / Q000652:urine
D000578:Amidines; D002250:Carbon Radioisotopes; D014344:Trypanocidal Agents; C003915:diminazene aceturate; D004133:Diminazene