Phototoxic potential of the new quinolone antibacterial agent levofloxacin in mice.
The phototoxic potential of (-)-(S)-9-fluoro-2,3-dihydro-3-methyl-10-(4- methyl-1-piperazyl)-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6- carboxylic acid hemihydrate (levofloxacin, DR-3355, CAS 100986-85-4) was evaluated by the mice ear swelling reaction. Results were compared with those for enoxacin (ENX). Mice were orally administered DR-3355 or ENX and immediately exposed to ultraviolet-A for 4 h. Phototoxicity was determined by measuring ear thickness developing 24 h after irradiation. DR-3355 provided no changes in the ear at 200 mg/kg, but caused ear swelling at 800 mg/kg. ENX caused severe phototoxicity in a dose dependent manner from 50 mg/kg. These data suggest that DR-3355 has minor phototoxic potential, but is approximately 4-fold less toxic than ENX in these experimental conditions.
Wagai
N
N
Drug Safety Research Center, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Yoshida
M
M
Takayama
S
S
D000818:Animals; D000890:Anti-Infective Agents / Q000633:toxicity*; D015365:Enoxacin / Q000633:toxicity; D005260:Female; D064704:Levofloxacin; D008027:Light; D051379:Mice; D008807:Mice, Inbred BALB C; D015242:Ofloxacin / Q000633:toxicity*; D010787:Photosensitivity Disorders / Q000139:chemically induced* / Q000473:pathology
D000890:Anti-Infective Agents; D015365:Enoxacin; D064704:Levofloxacin; D015242:Ofloxacin