Background: Finafloxacin is a novel 8-cyano-fluoroquinolone under investigation for treatment of urinary tract infection. Methods: Urinary concentrations and urinary bactericidal titers (UBT) of finafloxacin 200- and 800-mg single doses in 6 healthy volunteers were measured up to 48 h. UBT were determined for a reference strain and 9 selected clinical uropathogens at the pH of native, acidified (pH 5.5) and alkalinized (pH 8.0) urine. Results: The mean maximum urine concentrations for 200 and 800 mg finafloxacin were 69.3 mg/l (0–2 h) and 150 mg/l (4–8 h). Median UBT were between 0 and 1:>2,048 and were in general agreement with minimal inhibitory concentrations of strains and urinary pH values. UBT in alkaline urine were significantly lower than those in native or acidic urine, except for Enterococcus faecalis.Conclusions: Finafloxacin exhibited significant bactericidal activity against susceptible uropathogens. The urinary bactericidal activity of finafloxacin was enhanced in acidic urine and significantly lower in alkaline urine.
Thirty male patients with chronic tonsillitis and 30 male patients with chronic Sinusitis maxillaris were pre-treated for four days with either 2 X 1 g erythromycin daily per os or 3 X 0.75 g amoxicillin daily per os in an open and randomised comparative study. MIC values for the relevant bacteria were determined beforehand. The intended tonsillectomy or radical operation was performed on the third day of pre-treatment, circa 1.5 h after the final administration of antibiotics. The tonsils or the sinus membrane were examined bacteriologically; the concentrations of erythromycin or amoxicillin were determined. At the same time, the concentration of the antibiotic administered was determined in the serum. The average concentration of erythromycin in the tonsil tissue was 1.24 micrograms/g; it was 1.21 micrograms/g in the sinus membrane. Amoxicillin was found at a concentration of 0.17 microgram/g in the tonsil tissue, and 0.1 microgram/g in the sinus membrane. While the levels of erythromycin in the tissue generally equalled or exceeded the MIC value for the pathogen in question, the levels of amoxicillin only reached the relevant MIC value for the given pathogen in a few cases since the concentration in the tissue was insufficient. The clinical tolerance of both antibiotics was good.
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