Developmental toxicity studies of the quinolone antibacterial agent irloxacin in rats and rabbits.

Embryotoxicity studies on irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1,4-dihydro-4-oxo-quinolone-3-carboxylic acid, CAS-91524-15-1), a new fluoroquinolone antibacterial agent, were performed in rats and rabbits. Oral administration of irloxacin during the fetal period of organogenesis to pregnant rats and rabbits at dose levels of up to 1000 and 350 mg/kg/d, respectively, elicited no evidence of teratogenicity. During the first days of treatment, transient stasis in body weight increase was observed in rat dams receiving doses of 350 or 1000 mg/kg/d, and reduced food consumption was observed in those receiving 1000 mg/kg/d.

Four-week oral toxicity studies of the new quinolone antibacterial agent cetefloxacin tosylate in rats and marmoset monkeys.

Four-week oral toxicity studies with cetefloxacin tosylate ((-)-7[3-(R)-amino-2-(S)-methyl-1-azetidinyl]-1-(2,4- difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-3-quinolinecarboxylic acid tosylate, CAS 141725-88-4 (base), E-4868.Ts) a new quinolone antibacterial agent, were performed in Sprague-Dawley rats and marmoset monkeys at doses of 100, 450, 2000 mg/kg/d and 25, 50, 125, 300 mg/kg/d, respectively. In rats, due to its toxicity the high dose was decreased to 1000 mg/kg/d after 3 days of treatment.

Subchronic toxicity of the new quinolone antibacterial agent irloxacin in beagle dogs.

The subchronic oral toxicity of the new quinolone antibacterial agent irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1,4-dihydro-4-oxo-quinolone- 3-carboxylic acid, CAS 91524-15-1) in Beagle dogs was investigated in studies of 4 and 29 weeks of duration. In both studies animals received dosages of 10, 120 and 1400 mg/kg/d. Pale coloured faeces were seen on animals receiving 1400 mg/kg/d.

Acute and subchronic toxicity studies of the new quinolone antibacterial agent irloxacin in rodents.

Irloxacin (6-fluorine-7-(pyrrol-1-yl)-1-ethyl-1, 4-dihydro-4-oxo-quinolone-3-carboxylic acid, CAS 91524-15-1), a new quinolone antibacterial agent, was administered as a single dose to rats and mice both by oral and intraperitoneal route in oder to study its acute toxicity. Its oral subchronic toxicity was also assessed by treating rats for 4 and 13 weeks. The results obtained showed that irloxacin was well tolerated after single administration in mice and rats, with LD50 values above 2000 and 5000 mg/kg for intraperitoneal and oral administration, respectively.

A study of reference parameters in the CFY (remote Sprague-Dawley) rat.

The reference parameters for 10- and 19-week old CFY (remote Sprague-Dawley) rats fed powdered feed have been studied: growth curves, food consumption, ophthalmoscopy, results of urinalyses and hematological and biochemical assays, and absolute and relative organ weights. Detailed information is given of instrumentation and methods employed, of the animals, strain and environment, and of blood-sampling technique. In general, the results obtained were similar to those previously reported in literature.

Acute, subacute and subchronic toxicity of besulpamide.

The acute oral and intraperitoneal toxicity of besulpamide has been studied in the rat and mouse, together with the subacute and subchronic oral toxicity in the rat at doses of 0, 125, 500 and 2000 mg/kg/day. The LD50 is in excess of 12,800 mg/kg by the oral route and in excess of 5,000 mg/kg intraperitoneally. Toxic signs were very slight and autopsy did not reveal lesions which could be attributed to the test substance.