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Query: UMLS:C0032285 (pneumonia)
 54,520 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The activities of fleroxacin against 22 clinical Legionella isolates were determined by agar and broth microdilution susceptibility testing. The fleroxacin MIC required to inhibit 90% of strains tested on buffered charcoal yeast extract agar medium supplemented with 0.1% alpha-ketoglutarate was 0.64 micrograms/ml and was 0.04 microgram/ml when testing was done with buffered yeast extract broth supplemented with 0.1% alpha-ketoglutarate. Fleroxacin (0.25 microgram/ml) reduced the bacterial counts of two L. pneumophila strains grown in guinea pig alveolar macrophages by 1 log10 CFU/ml, but regrowth occurred over a 3-day period; fleroxacin was significantly more active than erythromycin in this assay. Single-dose (10 mg/kg of body weight given intraperitoneally) pharmacokinetic studies performed in guinea pigs with L. pneumophila pneumonia revealed peak levels in plasma and lungs to be 3.3 micrograms/ml and 3.5 micrograms/g, respectively, at 0.5 h and 0.8 microgram/ml and 0.8 microgram/g, respectively, at 1 h. The half-life of the terminal phase of elimination from plasma and lung was approximately 2 h. All 17 infected guinea pigs treated with fleroxacin (10 mg/kg/day) for 2 days survived for 14 days post-antimicrobial therapy, as did all 16 guinea pigs treated with the same dose of fleroxacin for 5 days. Only 1 of 16 animals treated with saline survived. The animals treated with fleroxacin for 2 days lost more weight and had higher temperatures than those treated with the antibiotic for 5 days. Fleroxacin is effective against L. pneumophila in vitro and in a guinea pig model of Legionnaires' disease. Fleroxacin should be evaluated as a treatment for human Legionnaires' disease.
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PMID:In vitro activities of fleroxacin against clinical isolates of Legionella spp., its pharmacokinetics in guinea pigs, and use to treat guinea pigs with L. pneumophila pneumonia. 148 82

Fleroxacin, a new quinolone antimicrobial agent, was evaluated as part of a multicenter, comparative, open-label, randomized trial with ceftazidime in the treatment of lower respiratory tract infections and skin and soft-tissue infections. After written informed consent was obtained, 20 patients were entered at our center. Twelve patients were assigned to the fleroxacin group; 6 in each infection category. Of these 12 patients, 2 with pneumonia and 3 with skin and soft-tissue infection were not clinically evaluable. The mean duration of therapy was 5.7 +/- 3.0 days in the fleroxacin group versus 7.9 +/- 2.0 days in the ceftazidime group. The gram-positive organisms responsible for those infections not evaluable were methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, and group F streptococcus, all of which were resistant to fleroxacin. In total, 6 gram-positive isolates were resistant to fleroxacin. All but 2 S aureus isolates were susceptible to ceftazidime. Adverse reactions in both groups were negligible. Fleroxacin was found to be as effective as ceftazidime against a variety of gram-negative pathogens, but local susceptibility patterns for quinolones should be checked before empiric use of fleroxacin against gram-positive pathogens such as streptococci.
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PMID:Intravenous fleroxacin versus ceftazidime for lower respiratory tract and skin and soft-tissue infections. 152 93

The dual-action antibacterial R 23-9424 (desacetylcefotaxime linked to the quinolone fleroxacin) is a new antibacterial agent with excellent in vitro activity. It was evaluated for in vivo efficacy in comparison with the cephalosporin cefotaxime and the quinolone component, fleroxacin. Ro 23-9424 demonstrated significant activity against all strains tested in systemic infections, including those strains resistant in vivo to cefotaxime (Staphylococcus aureus 753, Serratia marcescens SM and Pseudomonas aeruginosa 8780) and fleroxacin (Streptococcus pneumoniae 6301 and Streptococcus pyogenes. In prophylactic studies, Ro 23-9424 compared favorably with fleroxacin against Escherichia coli and with cefotaxime against S. pyogenes, but Ro 23-9424 was considerably more active than cefotaxime against E. coli and more active than fleroxacin against S. pyogenes. In a murine pneumonia model, Ro 23-9424 was equivalent in activity to cefotaxime against S. pneumoniae and more active than cefotaxime against Klebsiella pneumoniae. Fleroxacin was inactive against S. pneumoniae and about 20-fold more active than Ro 23-9424 against K. pneumoniae. In a murine meningitis infection caused by S. pneumoniae, Ro 23-9424 was 3 times as active as cefotaxime, while fleroxacin was inactive. When meningitis was induced by K. pneumoniae, Ro 23-9424 was as active as the quinolone, while cefotaxime was inactive. In a neutropenic (immunocompromised) model, Ro 23-9424 was more active than cefotaxime against P. aeruginosa and 5-fold less active than fleroxacin. In the control normal (immunocompetent) mouse infection, Ro 23-9424 was 3-fold more active than cefotaxime, but 10-fold less active than fleroxacin.
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PMID:In vivo evaluation of a dual-action antibacterial, Ro 23-9424, compared to cefotaxime and fleroxacin. 210 64

Fleroxacin is a newly developed quinolone derivative with marked antimicrobial activity. In this study, we have compared the therapeutic effects of fleroxacin with those of ofloxacin, norfloxacin, ciprofloxacin, pipemidic acid and cefaclor against pneumonia in mice caused by Klebsiella pneumoniae. Fleroxacin showed a high therapeutic effect against the experimental pneumonia with an ED50 of 3.4 mg/kg/day, after three times a day oral administration. It was about twice as effective as ofloxacin and ciprofloxacin and more than 15 times more active than norfloxacin. Once or twice a day administration of fleroxacin also showed outstanding therapeutic effects.
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PMID:Therapeutic effect of fleroxacin against experimental pneumonia in mice. 314 31

Fleroxacin, administered intravenously at a dosage of 400 mg once a day, was compared with ceftazidime, 0.5-2 g three times daily or 1-2 g twice daily, administered for 4-21 days, for treatment of nonpneumococcal lower respiratory tract infections. A total of 319 patients were enrolled and randomized to receive treatment with fleroxacin or ceftazidime in a 2:1 ratio. Of those enrolled, 68 fleroxacin- and 49 ceftazidime-treated patients were included in the efficacy analysis. The most common diagnoses were pneumonia or pneumonitis (47% of the fleroxacin group and 57% of the ceftazidime group) and exacerbation of chronic bronchitis (38% and 33%, respectively). In the fleroxacin group, 59 (88%) of 67 patients were bacteriologic cures, and in the ceftazidime group, 40 (90%) of 49 were bacteriologic cures. It could be concluded with 95% confidence that the bacteriologic outcomes, by infection, for the two groups were equivalent (fleroxacin, 88%; ceftazidime, 90%). The rates of clinical cure were 59 (88%) of 67 for the fleroxacin group and 40 (82%) of 49 in the ceftazidime group, but since the 95% confidence limit around the between-group difference was greater than the stipulated +/- 15%, it could not be concluded that the outcomes were equivalent. The percentage of patients who experienced adverse clinical or laboratory events was similar in the two treatment groups (12% and 13%). The bacteriologic outcomes, by infection, were equivalent for the two treatment groups. Protocol requirements permitting a determination of equivalence of the outcomes for clinical cure were not met, although the rates were similar.
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PMID:Intravenous fleroxacin versus ceftazidime in the treatment of acute nonpneumococcal lower respiratory tract infections. 845 71

Fleroxacin is a new oral and intravenous trifluorinated 4-quinolone, which acts by inhibiting the essential bacterial enzyme DNA gyrase. Fleroxacin exhibits a broad spectrum of action, characterized by pronounced activity against aerobic gram-negative bacteria, but also against gram-positive pathogens such as staphylococci. Fleroxacin is distinguished by its excellent bioavailability, high concentrations in the plasma and other body fluids, good tissue penetration, and a long half-life of 10-12 h, thus allowing once-a-day administration. A single oral dose of 400 mg fleroxacin is effective in uncomplicated cystitis in women, uncomplicated gonococcal infections, bacterial enteritis, and traveler's diarrhea. A single daily dose of 200 mg administered for 3 days is effective in uncomplicated urinary tract infection (UTI), while longer treatment and higher doses may be required in acute uncomplicated pyelonephritis and complicated UTI. Skin, soft tissue, bone and joint infections, and lower respiratory tract infections including exacerbation of chronic bronchitis and non-pneumococcal pneumonia are further indications for fleroxacin.
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PMID:Fleroxacin overview. 886 29