Bioavailability, pharmacokinetics, and tissue distribution of 14C homidium after parenteral administration to Boran cattle.
The absorption, distribution and elimination characteristics of 14C homidium have been described in non-infected and Trypanosoma congolense-infected cattle treated with 14C homidium chloride by either intramuscular (i.m.) or intravenous (i.v.) injection at a dose level of 1 mg/kg body weight. Results show that the mean (+/-SD) elimination of the drug from plasma followed a biexponential process, with half-lives of 0.084 +/- 0.006 h and 97.66 +/- 16.28 h for the distribution and elimination phases after intravenous injection, respectively. Bioavailability of the intramuscular dose was 62.5% and 57.8% in non-infected and trypanosome-infected cattle, respectively. Absorption was rapid, with a tmax of 15 min and a mean Cmax (+/-SD) of 268.4 +/- 4.09 ng/mL following the intramuscular dose in non-infected cattle. The major route of excretion was via faeces. Approximately 90% of the total dose given to non-infected i.m.-treated cattle was excreted within 14 days. Following intramuscular administration of the drug, residues remained high in the major excretory organs, with the liver having concentrations of 1411 and 1199 ng/g after 14 and 28 days, respectively. Over the same period, the values in the kidneys were 649 and 448 ng/g. Concentrations in the liver 14 and 21 days following i.v. treatment were 2195 and 2454 ng/g, respectively. These results show that there was no significant difference in liver drug residues between 14 and 21 days, or 28 days depending on the treatment given, suggesting that once the drug is in this organ, it is released back into the circulation at an extremely slow rate.
Murilla
G A
GA
Radioisotope Laboratory, Kenya Trypanosomiasis Research Institute, Kikuyu, Kenya.
Mdachi
R E
RE
Ismail
A A
AA
Karanja
W M
WM
D000042:Absorption; D000818:Animals; D001682:Biological Availability; D002250:Carbon Radioisotopes; D002417:Cattle / Q000378:metabolism*; D004996:Ethidium / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006207:Half-Life; D007273:Injections, Intramuscular / Q000662:veterinary; D007275:Injections, Intravenous / Q000662:veterinary; D007553:Isotope Labeling; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008297:Male; D012044:Regression Analysis; D014018:Tissue Distribution; D014344:Trypanocidal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D014348:Trypanosoma congolense; D014353:Trypanosomiasis, African / Q000188:drug therapy / Q000378:metabolism / Q000662:veterinary; D014354:Trypanosomiasis, Bovine / Q000188:drug therapy* / Q000378:metabolism
D002250:Carbon Radioisotopes; D014344:Trypanocidal Agents; D004996:Ethidium