Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0034186 (pyelonephritis)
 6,144 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The fluoroquinolone antibacterial agent fleroxacin has a broad spectrum of in vitro activity which encompasses most Gram-negative species (particularly Enterobacteriaceae) and a number of Gram-positive organisms, including methicillin-sensitive staphylococci. It is available as oral and intravenous formulations. In clinical trials, fleroxacin has been evaluated in the treatment of uncomplicated urinary tract infections (single or multiple once-daily oral doses of 200 or 400mg), gonorrhoea and chancroid (single oral doses of 200 or 400mg), complicated urinary tract, nonpneumococcal lower respiratory tract and skin and soft tissue infections and typhoid fever (multiple once-daily oral or intravenous regimens, usually 400 mg/day), bacterial enteritis, and traveller's diarrhoea (single or multiple once-daily oral doses of 400mg). Bacteriological cure rates were generally around 90% or higher in complicated and uncomplicated urinary tract infections, uncomplicated gonorrhoea (approximately 100%), pyelonephritis, bacterial enteritis and typhoid fever, and exceeded 80% in lower respiratory tract, and skin and soft tissue infections and chancroid. These cure rates were similar to, or better than, those achieved with standard comparator antibacterial agents such as penicillins, cephalosporins, cotrimoxazole, or other quinolones. Fleroxacin 400mg once daily also achieved bacteriological cure in approximately 80% of patients with bone and joint infections in preliminary studies. In Japanese studies using a lower dosage of 200 or 300 mg/day, fleroxacin was reported to be bacteriologically effective in a range of infections, including urinary tract and upper and lower respiratory tract infections. Fleroxacin has a relatively long elimination half-life, which allows once-daily administration, and it appears to have less propensity for interactions with other medications in comparison to many other fluoroquinolones. Its tolerability profile is typical of this class of compound, with adverse events mostly relating to the gastrointestinal tract, CNS, and skin and appendages (including phototoxicity). Recent pooled tolerability data from worldwide clinical trials indicate that adverse events are reported by approximately 27% of patients receiving 200 mg/day orally or 400 mg/day orally or intravenously, and 17% of those receiving a single oral dose of 400mg. These exceed incidences reported for established fluoroquinolones, possibly indicating recent trends towards increased rates of reported adverse effects with these agents. However, in direct comparative studies with twice-daily fluoroquinolones, fleroxacin 400mg once daily produced a similar incidence of adverse effects to ofloxacin 800 mg/day and a slightly higher incidence than ciprofloxacin 1000 mg/day, while fleroxacin 200mg once daily produced a similar incidence to norfloxacin 800 mg/day.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Fleroxacin. A review of its pharmacology and therapeutic efficacy in various infections. 760 Oct 15

Intravenous fleroxacin, 400 mg once daily, was compared with intravenous ceftazidime, 0.5-2 g three times a day or 1-2 g twice a day, administered for 4-21 days for treatment of complicated urinary tract infections (UTIs) due to susceptible organisms. Fleroxacin also was tested in an uncontrolled trial. The trial was a multicenter, randomized, open-label study of adults with pyelonephritis or signs and symptoms of UTI and complicating factors. In the controlled trial, 474 patients were randomly assigned in a 2:1 ratio to receive fleroxacin (n = 320) or ceftazidime (n = 154). The microbiologic criterion for diagnosis of UTI was the isolation of > or = 10(5) colony-forming units (CFU) of pathogenic bacteria/mL of urine. The efficacy analyses included 165 fleroxacin-treated and 82 ceftazidime-treated patients in the controlled trial and 97 patients in the uncontrolled trial. In the controlled trial, 317 fleroxacin-treated and 150 ceftazidime-treated patients were included in the safety analysis. In the controlled trial, the respective rates of bacteriologic cure (< or = 10(4) CFU/mL of urine 48-96 hours after first dose and 2-5 days posttherapy) were 94% (confidence interval [CI], 89-97%) and 95% (CI, 88-99%) in the fleroxacin and ceftazidime groups, and those of clinical cure were 86% (CI, 80-91%) and 89% (CI, 80-95%). Rates of clinical and bacteriologic cure in the uncontrolled study were 95%. In the controlled trial, 9% of the patients in each treatment group experienced one or more adverse events possibly or probably related to the study drug. The percentage of patients terminating therapy prematurely was higher in the fleroxacin than in the ceftazidime group. Once-daily dosing with 400 mg of intravenous fleroxacin was equivalent to a standard multidose regimen with respect to rates of bacteriologic and clinical cure in the treatment of complicated UTI.
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PMID:Comparison of intravenous fleroxacin with ceftazidime for treatment of complicated urinary tract infections. 845 67

This study enrolled patients with complicated urinary tract infections (UTIs) in a trial to determine the efficacy and safety of sequential therapy with intravenous fleroxacin (first 3 days) followed by oral fleroxacin, for a total course of 7-14 days, both administered at a dosage of 400 mg once a day. We enrolled 68 patients with complicated UTIs or acute pyelonephritis, 32 of whom were evaluable for bacteriologic and clinical efficacy. The pathogens isolated included Escherichia coli, 15; enterococci, 9; miscellaneous, 15. Intravenous fleroxacin was given for a mean of 3.2 days, followed by oral fleroxacin for a mean of 5.3 days. A total of 27 patients were clinically cured (84%), two improved, and three failed. A total of 26 patients were bacteriologically cured (81%), and six failed (19%). The bacteria that were not eradicated included enterococci, 4; Staphylococcus epidermidis, 1; and Pseudomonas species, 1. One enterococcal isolate became resistant to fleroxacin. Four patients were bacteremic (E. coli, 3; Proteus mirabilis, 1); the pathogen was eradicated in all cases. Two patients developed urinary enterococcal superinfections. A total of 12 patients experienced 16 adverse reactions remotely, possibly, or probably related to fleroxacin (insomnia, 3; dizziness, 2; miscellaneous, 11). One patient had a grand mal seizure after aspirating gastric contents; the seizure was thought to be only remotely related to the study drug. Fleroxacin was discontinued in two patients because of adverse effects (phlebitis at intravenous access site, 1; anxiety and insomnia, 1). Only minor and asymptomatic laboratory abnormalities were observed. All clinical and laboratory abnormalities resolved with discontinuation of the study drug. Fleroxacin is a safe and effective antibiotic for sequential intravenous and oral treatment of acute pyelonephritis and complicated UTIs. Enterococci may be problematic pathogens, as reported with other fluoroquinolones.
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PMID:A sequential study of intravenous and oral fleroxacin in the treatment of complicated urinary tract infection. 845 68

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