We studied the optimal clinical dose of pazufloxacin mesilate, a new quinolone antibiotic for injection, in respiratory tract infection and complicated urinary tract infection based on clinical results in open and dose-finding studies.
1) Respiratory tract infection
In an open study, clinical efficacy was 75.4%(172/228). Efficacy in the 600mg a day group was 75.4 %(49/65) and 74.4%(116/156) in the 1, 000mg a day group. In a dose-finding study on bacterial pneumonia, clinical efficacy was 100%(32/32) in the 600mg a day group and 92.6%(25/27) in the 1, 000 mg a day group, with no significant difference between groups. The incidence of adverse effects was 2.6%(2/77) in the 600mg group and 5.1%(9/175) in the 1, 000mg group in an open study and 0%(0/35) in the 600mg group and 3.0%(1/33) in the 1, 000mg group in a dose-finding study. The incidence of abnormal change in laboratory findings was 17.4%(12/69) in the 600mg group and 12.4%(20/161) in the 1, 000mg group in an open study and 14.7%(5/34) in the 600mg group and 24.1%(7/29) in the 1, 000 mg group in a dose-finding study. The major abnormalities were transaminase elevation and eosinophilia. In the 1, 000mg a day group, moderate to severe cases with underlying disease or complications were treated effectively, with no severe adverse effects observed. From these results, we concluded that a daily dose of 1, 000mg was the optimal clinical dose for pazufloxacin mesilate in respiratory tract infection.
2) Complicated urinary tract infection
In an open study, overall clinical efficacy was 78.7%(118/150). Efficacy in the 600mg a day group was 81.6%(40/49) and 77.0%(77/100) in the 1, 000mg a day group. In a dose-finding study on complicated urinary tract infection, overall clinical efficacy was 86.7%(26/30) in the 600mg group and 78.8%(26/33) in the 1, 000mg group, with no significant difference between groups. The incidence of adverse effects was 1/1 in the 300mg a day group and 0.8%(1/123) in the 1, 000mg group in an open study and 2.8%(1/36) in the 600mg group and 0%(0/38) in the 1, 000mg group in a dose-finding study. The incidence of abnormal change in laboratory findings was 6.3%(3/48) in the 600mg group and 8.8%(10/113) in the 1, 000mg group in an open study and 14.3%(5/35) in the 600mg group and 16.2%(6/37) in the 1, 000 mg group in a dose-finding study. The major abnormalities were transaminase elevation and eosinophilia. The bacteriological response, especially eradication against resistant strains, was better in the 1, 000mg group than in the 600mg group in a dose-finding study, and no severe adverse effects were observed in the 1, 000mg group. From these results, we concluded that a daily dose of 1, 000mg was the optimal clinical dose for pazufloxacin mesilate in complicated urinary tract infection.
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