title: Bactericidal activity of ciprofloxacin, norfloxacin and ofloxacin in serum and urine after oral administration to healthy volunteers.
abstract: A 200 mg oral dose of ciprofloxacin, norfloxacin or ofloxacin was administered to six healthy male volunteers in a three way cross-over study in order to examine the kinetics in humans in relation to the bactericidal activity in serum and urine. Serum concentrations for ciprofloxacin were similar to norfloxacin and lower than ofloxacin. Despite this fact, ciprofloxacin showed the highest serum bactericidal titers compared to norfloxacin and ofloxacin when serum-resistant Escherichia coli C14 was used as a test organism. These results correlate with observations from timekill curve studies in human whole blood, where ciprofloxacin showed superior bactericidal activity compared to norfloxacin or ofloxacin. The amounts of unchanged drug excreted in urine (48 h period) were found to be 35%, 24% and 77% for ciprofloxacin, norfloxacin and ofloxacin respectively, indicating different excretion kinetics. The volumes of urine excreted in the different collection periods were comparable for the three drugs tested. Mean urine concentrations for ciprofloxacin were higher during the 0 to 4 h collection periods, whereas ofloxacin was excreted into the urine over a longer time period. Measurements of urine bactericidal activity showed that ciprofloxacin had the highest titers during the early collection periods, whereas the prolonged excretion of ofloxacin did not result in higher urine bactericidal titers, compared to ciprofloxacin.
authors.affiliation: Department of Chemotherapy, Bayer AG, Research and Development, Wuppertal.
authors.forename: H J
authors.initials: HJ
authors.lastname: Zeiler
authors.forename: D
authors.initials: D
authors.lastname: Beermann
authors.forename: W
authors.initials: W
authors.lastname: Wingender
authors.forename: D
authors.initials: D
authors.lastname: Förster
authors.forename: P
authors.initials: P
authors.lastname: Schacht
mesh_terms: D000284:Administration, Oral; D002939:Ciprofloxacin / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects; D006801:Humans; D007711:Klebsiella pneumoniae / Q000187:drug effects; D008297:Male; D008826:Microbial Sensitivity Tests; D009643:Norfloxacin / Q000493:pharmacokinetics* / Q000494:pharmacology*; D015242:Ofloxacin; D010078:Oxazines / Q000493:pharmacokinetics* / Q000494:pharmacology*
chemical_list: D010078:Oxazines; D002939:Ciprofloxacin; D015242:Ofloxacin; D009643:Norfloxacin