The metabolism of cilostamide in the rat in vitro and in vivo.
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.
D000818:Animals; D002250:Carbon Radioisotopes; D005243:Feces / Q000032:analysis; D006900:Hydroxylation; D066298:In Vitro Techniques; D008099:Liver / Q000378:metabolism; D008297:Male; D011804:Quinolines / Q000378:metabolism*; D015363:Quinolones; D051381:Rats; D011919:Rats, Inbred Strains
D002250:Carbon Radioisotopes; D011804:Quinolines; D015363:Quinolones; C021294:cilostamide