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Assessment of the main metabolism pathways for the flukicidal compound triclabendazole in sheep

Article

Authorship
VIRKEL, GUILLERMO LEON ; LIFSCHITZ, ADRIAN LUIS ; Sallovitz, Juan Manuel ; Pis, Alejandra ; LANUSSE, CARLOS EDMUNDO
Date
2006
Publishing House and Editing Place
Wiley Blackwell Publishing, Inc
Magazine
JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS, vol. 29 (pp. 213-223) Wiley Blackwell Publishing, Inc
Summary Information provided by the agent in SIGEVA
Triclabendazole (TCBZ) is an halogenated benzimidazole (BZD) compound worldwide used to control immature and adult stages of the liver fluke Fasciola hepatica. The purpose of this investigation was to characterize in vitro the patterns of hepatic and ruminal biotransformation of TCBZ and its metabolites in sheep. TCBZ parent drug was metabolized into its sulphoxide (TCBZSO), sulphone (TCBZSO2) and hydroxy derivatives by sheep liver microsomes. The same microsomal fraction was also able to oxidi... Triclabendazole (TCBZ) is an halogenated benzimidazole (BZD) compound worldwide used to control immature and adult stages of the liver fluke Fasciola hepatica. The purpose of this investigation was to characterize in vitro the patterns of hepatic and ruminal biotransformation of TCBZ and its metabolites in sheep. TCBZ parent drug was metabolized into its sulphoxide (TCBZSO), sulphone (TCBZSO2) and hydroxy derivatives by sheep liver microsomes. The same microsomal fraction was also able to oxidize TCBZSO into TCBZSO2 and hydroxy?TCBZSO (HO?TCBZSO). TCBZ sulphoxidation was significantly (P?
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