Isolation and identification of metabolites of ofloxacin in rats, dogs and monkeys.
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.
Sudo
K
K
Okazaki
O
O
Tsumura
M
M
Tachizawa
H
H
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
D005965:Glucuronates; D010078:Oxazines; D010087:Oxides; D015242:Ofloxacin