Disease relevance of fleroxacin

• A rabbit model of CAUTI using a closed urinary catheter drainage system and the mutant strain of Escherichia coli (WE 6933) were used to examine three dosage regimens (30 mg/kg q8h i.v.; 20 mg/kg q8h i.v.; and 10 mg/kg q8h++i.v.) of fleroxacin administered intravenously for 4 days [1].
• Fleroxacin and the three other quinolones were all active against Enterobacteriaceae, with 95-97% of the strains susceptible [2].
• The trifluoroquinolone fleroxacin inhibits the majority of Enterobacteriaceae at concentrations < or = 1 micrograms/mL and most Pseudomonas aeruginosa and staphylococci at < or = 2 micrograms/mL [3].
• The eradication rate for Staphylococcus aureus was 100% (11 of 11) in the fleroxacin group and 89% (17 of 19) in the AMX/CP group; 18 (82%) of the fleroxacin group and 25 (76%) of the AMX/CP group were clinically cured [4].
• One Haemophilus parainfluenzae strain persisted with fleroxacin [5].

Psychiatry related information on fleroxacin

• Clinical cure was achieved in 12 (60%) and 18 (81.8%) patients, and improvement in 2 (10%) and 1 (4.5%) patients in the fleroxacin and conventional therapy group, respectively [6].

High impact information on fleroxacin

• We analyzed the effect of ciprofloxacin, fleroxacin, and ceftazidime on production of colony-stimulating factors (CSF) by cultured murine spleen cells in the presence of pokeweed mitogen (PWM) [7].
• Multicenter study of single-dose and multiple-dose fleroxacin versus ciprofloxacin in the treatment of uncomplicated urinary tract infections [8].
• Overview of the pharmacokinetics of fleroxacin [9].
• Therapeutic efficacy of fleroxacin for eliminating catheter-associated urinary tract infection in a rabbit model [1].
• Patients were entered in a double-blind, placebo-controlled, multicenter study to compare low- and high-dose fleroxacin with norfloxacin for the treatment of complicated urinary tract infection (UTI) [10].

Chemical compound and disease context of fleroxacin

• In the low-dose fleroxacin group, 68 (96%) of 71 patients had bacteriologic cures (eight with superinfection), compared with 56 (92%) of 61 in the high-dose fleroxacin group (two with superinfection) and 52 (90%) of 58 in the norfloxacin group (four with superinfection) [10].
• Multicenter trial of fleroxacin versus ceftriaxone in the treatment of uncomplicated gonorrhea [11].
• Comparison of oral fleroxacin with oral amoxicillin/clavulanate for treatment of skin and soft tissue infections [4].
• The combination of fleroxacin with such aminoglycosides as gentamicin, amikacin, and tobramycin is indifferent against most Enterobacteriaceae, as is the combination of fleroxacin with penicillins, cephalosporins, rifampin, clindamycin, and metronidazole [3].
• Comparative efficacy and safety of oral fleroxacin and amoxicillin/clavulanate potassium in skin and soft tissue infections [12].

Biological context of fleroxacin

• Patients with renal disease (mean glomerular filtration rate [GFR], 22 mL/min) and healthy subjects (mean GFR, 100 mL/min) received 400 mg of fleroxacin orally and 100 mg of fleroxacin intravenously in a crossover design [13].
• Aside from the modest effect of metals on its absorption, fleroxacin does not interact/compete with substances oxidized in the liver, such as theophylline, and drug interactions are minimal [9].
• The elimination half-life of fleroxacin in milk was identical to that in plasma, and the AUC reached 43.3 mg.h/liter [14].
• The protein binding of Ro 23-6240 (5 micrograms/ml) was 27% [15].
• Oral clearance of fleroxacin (CL = CL/F, where F is bioavailability was slightly, but not significantly, reduced during the bacteremic phase (oral clearance, 43.8+/- 23.5 versus 48.5 +/- 17.5 ml/min [16].

Anatomical context of fleroxacin

• In most biologic specimens, such as myometrium, fallopian tube, bile bladder wall, bone, tonsils, maxillary sinus mucosa, prostatic adenoma, sputum, inflammatory fluid, synovia, lymph, saliva, and tears, the levels of fleroxacin were similar to those in plasma [17].
• In the fleroxacin group, adverse events affecting the central nervous system (mainly dizziness, insomnia, somnolence) also were reported [12].
• Samples of body fluids and tissues were obtained at various intervals after oral administration, and fleroxacin concentrations were determined by high-performance liquid chromatography [17].
• Renal impairment had no influence on the complete absorption of fleroxacin from the gastrointestinal tract, the maximal plasma concentration, and the steady-state volume of distribution (Vd-ss > 1 L/kg) [13].
• Penetration of fleroxacin into fat, lens, bronchial secretions, sweat, and aqueous humor was limited, with drug levels reaching only 10-40% of the concomitant levels in plasma [17].

Associations of fleroxacin with other chemical compounds

• Comparison of intravenous fleroxacin with ceftazidime for treatment of complicated urinary tract infections [18].
• Among evaluable men, fleroxacin eradicated 154 of 155 (99%; 95% confidence interval [CI]: 98.1-100%) urethral and 2 of 2 pharyngeal infections, while ceftriaxone eradicated 156 of 156 (95% CI: 99.4-100%) urethral and 5 of 5 pharyngeal infections [11].
• Cure at 5-9 days after treatment was achieved in 32 (97%) of the fleroxacin-treated patients and in 22 (56%) of the amoxicillin-treated patients (p < 0.001) [19].
• Magnetic resonance spectroscopy of fluorine (19F) has been used to noninvasively study the in vivo pharmacokinetics of a model drug, fleroxacin (a fluoroquinolone antibiotic agent), in healthy human subjects [20].
• Twelve healthy volunteers participated in this randomized crossover study to compare the concentrations and recovery levels of fleroxacin and pefloxacin in urine and to assess their bactericidal activities against 12 strains of urinary pathogens with different susceptibilities over a wide range of MICs [21].

Gene context of fleroxacin

• The maximum recA inducing concentrations after 60 min exposure to the quinolones in E. coli were 0.5 mg/L of rufloxacin, MF961, ofloxacin and 0.05 mg/L of fleroxacin [22].
• Fleroxacin (100 mg/L) enhanced basal levels of IL-8 [23].
• Fleroxacin neither enhances nor antagonizes the in vitro activity of Amph B at high concentration (50-100 micrograms/ml) [24].
• Accordingly, they had altered porins and replicative DNA biosynthesis resistant to fleroxacin [25].
• Ro 23-6240 inhibited beta-lactamase-producing bacteria resistant to broad-spectrum cephalosporins [26].

Analytical, diagnostic and therapeutic context of fleroxacin

• Safety of fleroxacin in clinical trials [27].
• A multicenter study on the comparative in vitro activity of fleroxacin and three other quinolones: an interim report from 27 centers [2].
• Pharmacokinetics of fleroxacin as studied by positron emission tomography and [18F]fleroxacin [28].
• Quantitative bacterial counts, urinary concentrations of fleroxacin and desmethylferoxacin, histopathologic changes, and electron microscopic evaluation of catheter-associated biofilm and mucosal biofilm were performed [1].
• Histopathologic changes were significantly reduced in all fleroxacin-treated rabbits, and scanning electron microscopy showed deterioration of the bacterial biofilm on the surface of the Foley catheter in treated animals [1].

References