PATTERN OF TRICLABENDAZOLE ACCUMULATION IN LIVER FLUKES (FASCIOLA HEPATICA) COLLECTED FROM TREATED SHEEP

CEBALLOS, L; MORENO, L.; ALVAREZ, L; LANUSSE, C

Tandil. Argentina

Congreso; XL Reunion Anual de la Asociación Argentina de Farmacología Experimantal; 2008

The fluckicidal compound triclabendazole (TCBZ) has a complex metabolic pattern that includes the systemic presence of active metabolites. The aim of this work was to evaluate the relative importance of oral ingestion or transtegumental diffusion in TCBZ/metabolites accumulation into Fasciola hepatica. Sheep infected with F. hepatica (n= 12) were treated with TCBZ (10 mg/kg) by the i.r. route. At 3, 24, 48 and 60 h post-treatment, animal was killed (n= 3) and plasma, bile and F. hepatica samples were obtained. TCBZ/metabolites concentrations were measured by HPLC. TCBZ sulphoxide (TCBZSO) and sulphone (TCBZSO2) the only molecules found in plasma. These metabolites were also the main analytes recovered in F. hepatica, with low TCBZ concentrations detected at 24 h post-tretment. However, TCBZ, TCBZSO, TCBZSO2 and hydroxi-TCBZ were found in bile of treated sheep at all sampling times. Plasma samples were collected (PK study) and analysed by HPLC. The similar concentration pattern observed for TCBZSO and TCBZSO2 in plasma and F. hepatica may indicate that the oral ingestion is an important route of drug entry into the trematode when the assessment is done under in vivo conditions.