title: Isolation and identification of metabolites of ofloxacin in rats, dogs and monkeys.
abstract: Metabolites of (+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H -pyrido [1,2,3-de][1,4]benzoxazine-6-carboxylic acid (ofloxacin) in excreta of rats, dogs and monkeys after oral administration of 14C-ofloxacin (20 mg/kg) were isolated and identified. Three metabolites of ofloxacin were detected in the excreta of all three species, and identified by t.l.c., u.v., n.m.r. and mass spectrometry as follows: M-1, ester glucuronide of ofloxacin; M-2, unchanged ofloxacin; M-3, (+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(1-piperazinyl)-7-oxo-7H-pyrido [1,2,3-de][1,4]benzoxazine-6-carboxylic acid (desmethyl ofloxacin); M-4, (+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H -pyrido [1,2,3-de][1,4]-benzoxazine-6-carboxylic acid piperazine-4-oxide (ofloxacin N-oxide). It is concluded that ofloxacin is metabolized by O-acyl glucuronidation, N-demethylation and N-oxidation.
authors.forename: K
authors.initials: K
authors.lastname: Sudo
authors.forename: O
authors.initials: O
authors.lastname: Okazaki
authors.forename: M
authors.initials: M
authors.lastname: Tsumura
authors.forename: H
authors.initials: H
authors.lastname: Tachizawa
mesh_terms: D000818:Animals; D001646:Bile / Q000378:metabolism; D001711:Biotransformation; D004285:Dogs; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D005965:Glucuronates / Q000378:metabolism; D008252:Macaca fascicularis; D008297:Male; D015242:Ofloxacin; D010078:Oxazines / Q000378:metabolism*; D010087:Oxides; D051381:Rats
chemical_list: D005965:Glucuronates; D010078:Oxazines; D010087:Oxides; D015242:Ofloxacin