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The effects of KR-10876, a new quinolone antimicrobial agent, on the central nervous system

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Abstract

To evaluate KR-10876, a new fluoroquinolone antibacterial agent, its effects on the central nervous system (CNS) were investigated in mice as part of pharmacological study, and the results were compared with those for ciprofloxacin and ofloxacin, two prototypes of quinolone antibacterial agents. All the parameters indicative of CNS function and acute toxicity were measured by close observation of the animals at regular time intervals after oral treatment of test compounds. KR-10876, ciprofloxacin and ofloxacin exerted a dose-dependent effect on the CNS functions studied. KR-10876 did not have any effects on the parameters measured at lower dose (100, 300 mg/kg, p.o.), but at high dose (1,000 mg/kg, p.o.), it caused ptosis, suppressed spontaneous locomotor activity, hypothermia, and prolonged hexobarbital-induced sleeping time. KR-10876 also had a slight effect on motor coordination only at high dose. Simialr to ciprofloxacin and ofloxacin, KR-10876 did not protect mice from pentylenetetrazol-, strychnine-, and electroshock-inducedl convulsions at doses tested. These findings demonstrate that KR-10876 affects CNS functions only at high doses. The rank order for effects is ofloxacin≥KR-10876>ciprofloxacin.

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Kim, E.J., Cha, S.W., Shin, H.S. et al. The effects of KR-10876, a new quinolone antimicrobial agent, on the central nervous system. Arch. Pharm. Res. 16, 6–12 (1993). https://doi.org/10.1007/BF02974120

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