Vol.55 No.S-1 October 2007
Single-dose toxicity studies of garenoxacin in mice, rats, and dogs
Research Laboratories, Toyama Chemical Co., Ltd., 2-4-1 Shimookui, Toyama, Japan
Abstract
Single oral and intravenous toxicity studies of garenoxacin mesilate hydrate(GRNX) were conducted in mice, rats, and dogs.
No mice, rats, or dogs died at the maximum dose of 2,000 mg/kg in oral administration. The lethal dose was exceeded 2,000 mg/kg in all species. Soft feces was observed at 2,000 mg/kg in rats. In dogs, decreased locomotor activity, vomiting, salivation, hypothermia and increased pulse rate were seen at 1,000 mg/kg or higher, and body weight and food consumption decreased transiently at 2,000 mg/kg.
Lethal doses in single intravenous dose studies were 200-250 mg/kg in male and 250 mg/kg in female mice; 250-300 mg/kg in both male and female rats; and 200-300 mg/kg in male dogs. In mice and rats, decreased locomotor activity, lateral/prone position, staggering gait, crawling, decreased respiration, clonic convulsion, mydriasis, straub tail, and/or salivation were observed at 150 mg/kg or higher. Decreased body weight and suppression of body weight gain were transiently observed at 150 mg/kg or higher in mice and 200 mg/kg or higher in rats. In dogs, at 200 mg/kg or higher, decreased locomotor activity, salivation, flushing, vomiting, hypothermia, increased pulse rate, and decreased body weight and food consumption were observed, with edema of the head and tonic convulsions noted at 300 mg/kg. In dead rats and dogs, congestion was observed in the lung, liver, stomach, and small intestine.
Results in single-dose toxicity studies of GRNX in mice, rats, and dogs indicate that toxic changes were similar to those of fluoroquinolone antibacterial agents, there was no specific toxicity to GRNX.
Key word
garenoxacin, des-fluoro(6)-quinolone, single dose toxicity
Received
May 9, 2007
Accepted
July 6, 2007
Jpn. J. Chemother. 55 (S-1): 28-33, 2007
