Penetration of grepafloxacin in prostatic fluid and a clinical study in urinary tract infection

A new oral quinolone antibacterial drug, grepafloxacin (GPFX), was administered to a total of 52 patients, including 51 cases of urinary tract infections (UTI) and 1 case of chronic prostatitis, to examine its therapeutic efficacy and safety. In addition, its concentration in prostatic fluid was measured. GPFX was administered to patients with uncomplicated cystitis at a dose of 100 mg once a day for 3∼5 days, and for patients with complicated UTI, the drug was given at a doses of 200∼300 mg once a day or divided into 2 doses a day for 5 days. According to the criteria proposed by the Japanese UTI Committee, the efficacy rate was 100%(11/11) in uncomplicated cystitis, while it was 44.4%(12/27) in complicated UTI. In complicated UTI, the bacterial eradication rate was 10/15 (66.7%) for gram-positive cocci and 15/24 (62.5%) for gramnegative bacteria. The prostatic fluid concentration of GPFX at 1∼4 hours after oral administration at doses of 200∼300 mg was 0.03∼0.53μg/ml, with a serum ratio of 0.12∼1.71. In regard to safety, subjective adverse reactions included 2 cases of GI disorder, 3 cases of CNS disorder and 1 case of allergic skin eruption. Abnormal laboratory findings included 1 case of slight elevation of sGOT, increase of neutrophils and lymphocytopenia.