GENERAL PHARMACOLOGICAL PROPERTIES OF FLEROXACIN

• Published in: CHEMOTHERAPY Vol. 38; no. Supplement2; pp. 203 - 240
• Main Authors: MOMO, KENJIRO, NAKAMURA, KOHJI, TACHIIRI, TOKUEI, MIYAZAKI, KENJI, KINOSHITA, OSAMU, NISHIKAWA, TAKASHI, HIRAYAMA, TAKASHI, YAMANISHI, ATSUHIRO, TAGA, FUKUTARO
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1990
• Subjects: Floxacin
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.38.Supplement2_203

We investigated the general pharmacological properties of fleroxacin with the following results. 1. Central nervous system: fleroxacin, at an oral dose of 100mg/kg, showed an anti-nociceptive effect and decrease in body temperature in mice; at 300 mg/kg or more it showed antipyretic action, suppressed spontaneous motor activity, prolonged thiopental-induced sleeping time and promoted reserpin-induced hypothermia in mice; and at 1000 mg/kg it showed muscle relaxation. A transient EEG arousal pattern was evoked in conscious, unrestrained cats at over 5mg/kg, intravenously. 2. Respiratory and cardiovascular system: fleroxacin decreased blood pressure in anesthetized dogs at an intravenous dose of 10mg/kg. But it showed little effect on any parameters at an intravenous dose of 10mg/kg in anesthetized rabbits, and on blood pressure at an infusion of 10mg/kg/10 min in unanesthetized, unrestrained cats. 3. Smooth muscles and autonomic nervous system: fleroxacin slightly suppressed the contractile response of isolated rat was deferens to noradrenaline and slightly enhanced the contractile response of isolated guinea pig trachea to histamine. It also slightly inhibited the spontaneous motility of isolated rabbit ileum and uterus at concentrations of 10-4g/ml and more. It inhibited the motility of urinary bladder at over 10mg/kg i. v., and of rabbit stomach at an i. v. dose of 30 mg/kg, but hadlittle effect on the motility of uterus. 4. Miscellaneous: fleroxacin, at oral doses above 100 mg/kg, increased bile secretion, free fatty acid levels in serum, and ketone bodies in rat urine. It produced a transient decrease in urine volume and blood glucose, showed anti-inflammatory and anti-ulcer effect, and suppressed reticuloendothelial function at oral doses of 300 mg/kg or more. It had no effect on ERG pattern and blood coagulation ability, and no hemolytic action.