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The Veterinary Record, Vol 138, Issue 8, 181-183
Copyright © 1996 by British Veterinary Association

Disposition of antimony after the administration of N-methylglucamine antimoniate to dogs

J. E. Valladares DVM1, J. Alberola PhD1, M. Arboix PhD1, and M. Esteban PhD2

1 Divisió de Farmacologia, Facultat de Veterinària, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain
2 Department de Química Analítica, Facultat de Químiques, Universitat de Barcelona, 08028 Barcelona, Spain

A study was carried out in dogs to define the pharmacokinetic profile of antimony and to define a better therapeutic protocol for the treatment of canine leishmaniasis. Six healthy beagle dogs received 100 mg/kg of N-methylglucamine antimoniate containing 27·2 per cent of antimony intravenously, intramuscularly and subcutaneously. After intravenous administration the plasma concentration of antimony decreased rapidly and after 240 minutes it was lower than the ED50 values suggested for Leishmania donovani. The pharmacokinetic parameters and bioavailability of antimony were calculated after each route of administration in each dog. The curves of plasma concentrations vs time were best described by a triexponential open model with a mean (sd) half life tfrac12agr of 9·4 (4·4) min, a tfrac12beta of 45·3 (4·5) min and a tfrac12ggr of 618·0 (93·5) min. The mean volume of distribution at steady state was 0·25 (0·03) litres/kg and the total body clearance was 0·25 (0·04) litres/h/kg. The peak plasma concentration (Cmax) after intramuscular administration was 27·2 (3·1) µg/ml, and after subcutaneous administration it was 25·5 (4·5) µg/ml; they were reached after 73·6 (11·9) min and 85·6 (11·3) min, respectively. The bioavailabilities after intramuscular and subcutaneous administration were 91·7 (7·1) and 92·2 (7·1) per cent, respectively. More than 80 per cent of the antimony was excreted in the urine in the first nine hours.




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Copyright © 1996 British Veterinary Association