Ex vivo antibacterial properties of rufloxacin compared with those of norfloxacin in a study with healthy volunteers.
Twelve adult males participated in a randomized crossover phase I clinical trial comparing serum bactericidal titers (SBTs), urine bactericidal titers (UBTs), and urine killing rates (UKRs) against Escherichia coli ATCC 25922 and Staphylococcus aureus ATCC 29213, after the administration of single 400-mg doses of rufloxacin and norfloxacin at different times up to 72 h postdose. SBTs were significantly higher (P < 0.05) against E. coli from 8 to 48 h and against S. aureus from 4 to 24 h with rufloxacin. UBTs for E. coli were higher (P < 0.05) for norfloxacin at early sample times (0 to 8 h) but higher for rufloxacin (P < 0.05) at sample times from 16 h on for both E. coli and S. aureus. Similar UKRs were obtained for both quinolones for 0 to 2 h and 8 to 12 h, but the UKR was maintained for 72 h with rufloxacin. The high and sustained mean levels of rufloxacin in urine (> 35 micrograms/ml), median UBTs (> 32 for E. coli and 16 for S. aureus) and UKRs for E. coli suggest prolonged urine antibacterial activity (for at least 72 h) and its use as a single 400-mg dose in the treatment of uncomplicated cystitis.
Aguilar
L
L
Medical Department, SmithKline Beecham Pharmaceuticals, Universidad Complutense, Madrid, Spain.
Balcabao
I P
IP
Salvá
P
P
Martín
M
M
Costa
J
J
Prieto
J
J
Dal-ré
R
R
D000328:Adult; D000890:Anti-Infective Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000652:urine; D001437:Bacteriuria / Q000188:drug therapy / Q000382:microbiology*; D018592:Cross-Over Studies; D004927:Escherichia coli Infections / Q000188:drug therapy / Q000652:urine; D024841:Fluoroquinolones; D006801:Humans; D008297:Male; D008826:Microbial Sensitivity Tests; D009643:Norfloxacin / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000652:urine; D015363:Quinolones / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000652:urine; D015610:Serum Bactericidal Test; D013203:Staphylococcal Infections / Q000188:drug therapy / Q000652:urine
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D015363:Quinolones; D009643:Norfloxacin; C060328:rufloxacin