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The metabolism of N-cyclohexyl'N-methyl-4-(1,2-dihydro-2-oxo-6-quinolyloxy)butyramide (cilostamide) was studied in vitro and in vivo after oral administration to rats. Recovery of orally administered 14C-cilostamide (3 mg/kg) and its metabolites in 48 h was 50.5% dose in urine and 47.6% dose in faeces. The drug was extensively metabolized. The metabolites of cilostamide in rats wee identified by t.l.c., g.l.c.-mass spectrometry and n.m.r. The major route of metabolism is hydroxylation at the cyclohexyl ring.
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