Acute oral toxicity of the new quinolone antibacterial agent levofloxacin in mice, rats and monkeys.
Acute oral toxicity of (-)-(S)-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 hemihydrate (levofloxacin, DR-3355, CAS 100986-85-4), a new quinolone antibacterial agent, was studied in ddy mice, SD rats and cynomolgus monkeys. LD50 values were 1,881 mg/kg for males and 1,803 mg/kg for females in mice, 1,478 mg/kg for males and 1,507 mg/kg for females in rats and more than 250 mg/kg in females monkeys. Toxic signs included the decrease in locomotor activity, ptosis, tremor, tonic convulsion and respiratory depressed in rodents and soft feces or vomiting in monkeys. At necropsy, no treatment-related changes were observed in any species except for the enlargement of the cecum in rats.
Kato
M
M
Drug Safety Research Center, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Furuhama
K
K
Yoshida
M
M
Akahane
K
K
Takayama
S
S
D000818:Animals; D000890:Anti-Infective Agents / Q000633:toxicity*; D001522:Behavior, Animal / Q000187:drug effects; D005260:Female; D007928:Lethal Dose 50; D064704:Levofloxacin; D008252:Macaca fascicularis; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015242:Ofloxacin / Q000633:toxicity*; D051381:Rats; D011919:Rats, Inbred Strains
D000890:Anti-Infective Agents; D064704:Levofloxacin; D015242:Ofloxacin