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Pharmacokinetics of Toltrazuril and Its Metabolites, Toltrazuril Sulfoxide and Toltrazuril Sulfone, After a Single Oral Administration to Pigs

Pharmacokinetics of Toltrazuril and Its Metabolites, Toltrazuril Sulfoxide and Toltrazuril Sulfone, After a Single Oral Administration to Pigs

Jong-Hwan Lim, Myoung-Seok Kim, Youn-Hwan Hwang, In-Bae Song, Byung-Kwon Park, Hyo-In Yun

J Vet Med Sci. 2010 Aug;72(8):1085-7.

PMID: 20332592

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 microg/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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP69004155	Toltrazuril sulfoxide		69004-15-5	Price

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