title: Urine bactericidal activity of pefloxacin versus norfloxacin in healthy female volunteers after a single 800-mg oral dose.
abstract: In an open randomised crossover study the antibacterial activity of pefloxacin and norfloxacin was assessed in the urine after a single 800-mg oral dose in 14 healthy female volunteers. Pefloxacin demonstrated lower peak concentrations in the urine than norfloxacin (mean, 217.2 mg/l versus 492.9 mg/l as determined by the microbiological assay) but pefloxacin was present over a longer period of time in sufficient concentrations than norfloxacin. Mean urine levels of at least 2 mg/l were present for 7 days after pefloxacin administration and 2 days after norfloxacin administration as determined by the microbiological assay. Overall, the urinary recovery of pefloxacin and norfloxacin amounted to 49.3% and 25.1%, respectively, of the total administered dose. The average urine bactericidal activity against the five test organisms was as follows: against reference strain Escherichia coli ATCC 25922 susceptible to nalidixic acid (Nal-S) for 5 days with pefloxacin and 2 days with norfloxacin; against three clinical isolates, one strain each of E. coli resistant to nalidixic acid (Nal-R), Klebsiella pneumoniae Nal-R, and Staphylococcus saprophyticus, for 3 days with pefloxacin and 24 h with norfloxacin; and against a clinical isolate of Enterococcus faecalis for 2 days with pefloxacin and 12 h with norfloxacin. In conclusion, pefloxacin as a single dose proved to have sufficiently high and long-lasting urine bactericidal activity against urinary pathogens. These findings support the results of a meta-analysis of seven clinical trials in patients with uncomplicated lower UTI, demonstrating a single oral dose of 800 mg pefloxacin to be as effective as a conventional treatment with comparative drugs.
authors.affiliation: Urologische Klinik, Klinikum St. Elisabeth, Straubing, Germany.
authors.forename: H
authors.initials: H
authors.lastname: Hofbauer
authors.forename: K G
authors.initials: KG
authors.lastname: Naber
authors.forename: M
authors.initials: M
authors.lastname: Kinzig-Schippers
authors.forename: F
authors.initials: F
authors.lastname: Sörgel
authors.forename: C
authors.initials: C
authors.lastname: Rustige-Wiedemann
authors.forename: B
authors.initials: B
authors.lastname: Wiedemann
authors.forename: A
authors.initials: A
authors.lastname: Reiz
authors.forename: M
authors.initials: M
authors.lastname: Kresken
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology / Q000652:urine*; D000892:Anti-Infective Agents, Urinary / Q000008:administration & dosage / Q000009:adverse effects / Q000652:urine*; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004352:Drug Resistance, Microbial; D013293:Enterococcus faecalis / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D005260:Female; D006801:Humans; D007711:Klebsiella pneumoniae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009268:Nalidixic Acid / Q000494:pharmacology; D009643:Norfloxacin / Q000008:administration & dosage / Q000009:adverse effects / Q000652:urine*; D015366:Pefloxacin / Q000008:administration & dosage / Q000009:adverse effects / Q000652:urine*; D013210:Staphylococcus / Q000187:drug effects; D014552:Urinary Tract Infections / Q000188:drug therapy* / Q000382:microbiology*; D014556:Urine / Q000737:chemistry*
chemical_list: D000890:Anti-Infective Agents; D000892:Anti-Infective Agents, Urinary; D015366:Pefloxacin; D009268:Nalidixic Acid; D009643:Norfloxacin