Journal of Veterinary Medical Science
Online ISSN : 1347-7439
Print ISSN : 0916-7250
Pharmacology
Pharmacokinetics of Toltrazuril and Its Metabolites, Toltrazuril Sulfoxide and Toltrazuril Sulfone, after a Single Oral Administration to Pigs
Jong-Hwan LIMMyoung-Seok KIMYoun-Hwan HWANGIn-Bae SONGByung-Kwon PARKHyo-In YUN
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2010 Volume 72 Issue 8 Pages 1085-1087

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Abstract

Toltrazuril (TZR) is a triazine-based antiprotozoal agent. Following a single oral administration of TZR at 10 and 20 mg/kg to male pigs, the mean TZR concentration in plasma peaked at 4.24 and 8.18 μg/ml at 15.0 and 12.0 hr post-dose, respectively. TZR absorbed was rapidly converted to the short-lived intermediary metabolite toltrazuril sulfoxide (TZR-SO), and then metabolized to the reactive toltrazuril sulfone (TZR-SO2). TZR-SO2 was actually more slowly eliminated, with average half-lives of 231 and 245 hr, compared with TZR (48.7 and 68.9 hr) or TZR-SO (51.9 and 53.2 hr) in the 10 and 20 mg/kg groups, respectively. This study demonstrates that TZR metabolizes to TZR-SO2 having a long-terminal half-life, enabling the persistent clinical efficacy in the treatment of I. suis infection. In contrast, special consideration should be given to the residual of TZR-SO2.

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