新経口合成抗菌薬grepafloxacinのテオフィリン血中濃度に及ぼす影響

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  • Effect of grepafloxacin on serum concentration of theophylline

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The effect of a new oral synthetic quinolone antibacterial agent, grepafloxacin (GPFX), on the serum level of theophylline was studied in 5 healthy male adult volunteers. A slow-release preparation of theophylline at a daily dose of 400 mg was given orally for 4 days prior to GPFX administration. The serum level of theophylline was determined on the 4th day and used as the control level. GPFX was then given orally at 200 mg once daily in the morning for 5 days with concomitant administration of theophylline at the same dose as above. The mean Cmax and AUC values of theophylline on the 3rd day with GPFX were, respectively, 1.29 and 1.31 times the control values, and total body clearance was decreased to 0.76 times the control value. On the 5th day with GPFX, the above parameters were 1.28, 1.33 and 0.74 times the control values, respectively, indicating no marked difference from the 3rd day. One volunteer complained of hand and finger tremor and slight aggravation of hot flushes after administration of theophylline alone from the 1st day of concomitant administration, but this did not necessitate discontinuation of the concomitant administration. From the above results, GPFX was considered to increase the serum level of concomitantly administered theophylline, indicating an increase similar to that for ciprofloxacin and tosufloxacin.

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