ASSESSMENT OF TEMAFLOXACIN NEUROTOXICITY IN RODENTS

Temafloxacin hydrochloride (HCl) was studied in fenbufen-treated mice and for its effects on the locomotor activity of rats. Mice were observed for convulsions for 90 minutes after the administration of temafloxacin HCl (100 mg/kg orally [p.o.]), ciprofloxacin HCl (100 mg/kg p.o.), enoxacin (100 mg/kg p.o.), or oxolinic acid (100 mg/kg p.o.). The quinolones were coadministered with either saline (0.2 mL p.o.) or fenbufen (100 mg/kg p.o.), a nonsteroidal antiinflammatory compound. No convulsions occurred following the administration of the quinolones with saline. Clonic convulsions occurred in 90% of mice receiving enoxacin and fenbufen and in 20% of mice receiving ciprofloxacin HCl and fenbufen. No convulsions occurred in mice receiving temafloxacin HCl or oxolinic acid with fenbufen. At doses of 30, 100, and 300 mg/kg p.o., temafloxacin HCl and enoxacin had no effect on locomotor activity of rats, but oxolinic acid markedly stimulated locomotor activity. The lack of central nervous system (CNS) stimulation and the absence of interaction with fenbufen suggest that temafloxacin may have less potential for adverse CNS effects than other quinolone compounds.