Metabolism of Simeconazole in rats

The excretion, tissue distribution and metabolic fate of simeconazole [(RS)-2-(4-fluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-trimethylsilyl propane-2-ol] in rats were studied by administering 14C-labeled simeconazole orally to male and female rats at 5 mg/kg b.w. (low dose) and 70 mg/kg b.w. (high dose). The simeconazole was readily absorbed and most of the radioactivity was excreted in the urine and feces within three days. The blood radioactivity level reached a maximum at 4–8 hr and 1–2 hr post-dosing in male and female rats, respectively. The radioactivity in the tissues and organs rapidly decreased with time. Simeconazole was initially metabolized to M1, the hydroxymethyl metabolite. M1 was further metabolized to glucuronide, sulfate, silanols and various dessiloxane compounds. © Pesticide Science Society of Japan