The oxidative metabolism of aldicarb in pigs: in vivo-in vitro comparison.

Aldicarb was administered (1 mg/kg b.w.) to four female pigs and the kinetics of its major oxidized metabolites (sulfoxide and sulfone) was followed for 6 hours. The in vitro transformations of the carbamate pesticide into these two still active metabolites were also investigated in hepatocytes and in microsomes from pig livers. In all cases, aldicarb was quickly oxidized to the sulfoxide (major metabolite) and only a minor quantity of sulfone was produced. The in vivo toxic symptomatology was related to the peak serum concentration of sulfoxide, suggesting that this metabolite is principally responsible for the aldicarb toxicity. Selective in vitro inhibition of flavin-containing and cytochrome P-450 monooxygenases confirmed that the former enzymes catalyze mainly sulfoxide production whereas the latter that of sulfone.