The efficacy and safety of
rufloxacin (400 mg, single dose) were compared to those of
norfloxacin (400 mg twice a day for 3 days) for the treatment of women with uncomplicated
cystitis. In addition, urine levels,
drug level/MIC ratio, and urine antibacterial activity 72 to 84 h
after treatment initiation were determined in a subgroup of patients for pharmacodynamic assessment. A total of 203 women were included and treated in this open, randomized clinical trial; 100 patients received
norfloxacin, whereas 103 received
rufloxacin. Of these, 156 (74 and 82 patients in the
norfloxacin and
rufloxacin groups, respectively) were considered bacteriologically evaluable. At the first follow-up visits (3 to 12 days after starting the treatment), bacteriological cure rates were 99 and 94% for
norfloxacin and
rufloxacin, respectively. Seventy-nine percent (119 of 150) of bacteriologically cured patients attended a long-term follow-up visit (4 to 6 weeks after starting the treatment), where a relapse rate of 4% (2 of 54) and 5% (3 of 64) were found in the
norfloxacin and
rufloxacin groups, respectively. The pharmacodynamic evaluation performed in 35 patients showed similar median urine levels (approximately equal to 25 micrograms/ml) and urine antibacterial activity for both treatment groups against initial isolates, despite a higher
norfloxacin level/MIC ratio due to the lower MIC of
norfloxacin. Twenty-one patients (20%) in the
rufloxacin group and 12 patients (12%) in the
norfloxacin group reported 39 and 16 adverse events, respectively, almost all of them being mild and lasting < 24 h. Overall, gastrointestinal reactions were the most frequent adverse events reported. However, 12 patients treated with
rufloxacin reported 15 central nervous system adverse events. This study shows that single doses of
rufloxacin are as effective as a
norfloxacin 3-day standard treatment in uncomplicated
cystitis. The results obtained with
rufloxacin are consistent with its pharmacodynamic properties.