GENERAL PHARMACOLOGY OF T-3262, A NEW PYRIDONECARBOXYLIC ACID

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  • 新しいピリドンカルボン酸系経口抗菌剤T-3262の一般薬理作用

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Abstract

General pharmacological activities of (±)-7-(3-amino-1-pyrrolidinyL)-6-fluoro-1-(2, 4-difluorophenyL)-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxylic acid p-toluenesulfonate hydrate (T-3262), which is a new pyridonecarboxylic acid, were examined with the following results.<BR>1. Central nervous system: T-3262 did not show any significant pharmacological effects at oral doses of 100-1,000mg/kg but caused slow waves in spontaneous EEG in cats at intravenous doses of 10-30mg/kg.<BR>2. Respiratory and cardiovascular system:<BR>T-3262 produced little effect in normotensive rats and anesthetized rabbits at oral doses of 100-1,000mg/kg and intravenous doses of 3-30mg/kg, respectively. But T-3262 caused, dosedependently, an increase of respiratory rate, hypotension, decrease of heart rate and changes in ECG patterns (elevation of T waves, slow amplitudes of QRS complexes and prolongation of RR interval, etc.) in anesthetized dogs at intravenous doses of 3-10mg/kg.<BR>3. Renal functions: T-3262 increased electrolyte excretions at oral doses of 300-1,000mg/kg but did not affect PSP excretion in rats.<BR>4. Autonomic nervous system and smooth muscle organs:<BR>T-3262 exerted slight inhibition of gastric output in rats and slight miosis in mice at an oral dose of 1,000mg/kg. But T-3262 did not affect the contraction of nictitating membrane in anesthetized cats at intravenous doses of 1-30mg/kg. T-3262 increased spontaneous motilities of isolated stomach, ileum and uterus, but decreased that of isolated colon at concentrations of 10-5-10-4g/ml.<BR>5. Hematological examinations: T-3262 did not show any significant effects on bleeding time, blood coagulation, platelet aggregation and blood glucose level in rats at oral doses of 100-1,000mg/kg.<BR>6. Miscellaneous effects: T-3262 exerted slight inhibitions of gastric secretion and of carrageenin-induced hind paw edema in rats at a dose of 1,000mg/kg administered intraduodenally and orally, respectively. T-3262 did not affect neuromuscular junction and bile secretion in rats at intravenous doses of 3-30mg/kg and oral doses of 100-1,000mg/kg, respectively.<BR>From these results, it can be assumed that T-3262 has a wide safety margin as an oral antibacterial agent.

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