Interaction of Fasciola hepatica with albendazole and its metabolites

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Abstract
Adult F. hepatica recovered from sheep 12 and 24 h after a single oral dose of albendazole (20 mg/kg) contained significant amounts of 2 oxidized metabolites of albendazole (ABZ), a sulfoxide (SX) and a sulfone (SO), but not ABZ. Flukes incubated in vitro with 10 .mu.M SX or SO contained these metabolites at a level 2-3 times the level observed in flukes recovered from sheep 24 h after a curative oral dose of ABZ. The concentration of ABZ in flukes was 10-fold greater than either SX or SO after a 24 h in vitro incubation in 10 .mu.M of the respective drug. Flukes exposed to ABZ in vitro contained 2 fold higher SX levels than SX-treated flukes due to a combination of spontaneous oxidation in media and fluke-mediated oxidation of ABZ. Measurement of end-products of glucose metabolism following 24 h incubation in 10 .mu.M of either ABZ, SX or SO did not show a significant difference between treated and untreated flukes.