Drugs online research references
J Antimicrob Chemother. 1988 Oct;22 Suppl D:3-17.
Fleroxacin: in-vitro activity worldwide against 20,807 clinical isolates and comparison to ciprofloxacin and norfloxacin.
Paganoni R, Herzog C, Braunsteiner A, Hohl P.
Department of Clinical Research, F. Hoffmann-La Roche, Basel, Switzerland.
By June 1987 worldwide investigators from 37 centres in 12 countries had completed epidemiological susceptibility testing studies comparing the in-vitro activity of fleroxacin with that of ciprofloxacin, norfloxacin and other antibacterials. In this paper the results of these studies, expressed primarily as MIC90S, are reviewed and analysed for centre to centre variability. Twenty thousand eight hundred and seven strains were evaluable for comparative analysis. All three quinolones exhibited high in-vitro activity against Enterobacteriaceae (MIC90 less than or equal to 0.125-2 mg/l), other common aerobic Gram-negative bacilli or coccobacilli (MIC90 less than or equal to 0.125-1 mg/l) and staphylococci, including selected resistant isolates (MIC90 less than or equal to 0.5-4 mg/l), and moderate to weak activity against streptococci and anaerobes (MIC90 = 1- greater than or equal to 8 mg/l). The activity of fleroxacin and norfloxacin was quite similar, but was usually inferior to that of ciprofloxacin. Comparison of data from the various investigating centres showed divergent results for many bacterial species, the MIC90S for the same quinolone varying by two to four dilution steps or more from centre to centre.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3144545&dopt=Abstract
J Clin Pharm Ther. 1992 Apr;17(2):111-5.
A simple high-performance liquid chromatographic assay for ciprofloxacin in human serum.
Jim LK, el-Sayed N, al-Khamis KI.
Department of Clinical Pharmacy, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
A simple and selective high-performance liquid chromatographic (HPLC) method for the determination of ciprofloxacin in serum has been developed and evaluated. Serum protein was precipitated with acetonitrile. The drug and the internal standard (quinine) were evaluated from a 10 microns U-Bondapack C-18 cartridge at ambient temperature with a mobile phase consisting of acetonitrile: 0.1 M sodium dihydrogen phosphate (20:80%, v/v) adjusted to pH 3.9 with phosphoric acid, and at a flow rate of 2.5 ml/min. The effluent was monitored on a fluorescence detector using an excitation and emission wavelength of 280 and 455 nm, respectively. Each analysis required no longer than 6 min. Quantification was achieved by the measurement of the peak-height ratio and the limit of quantification for ciprofloxacin in serum is 25 ng/ml. The intraday coefficient of variation (CV) ranged from 0.4 to 5.8%, and interday CV from 4.6 to 8.8% at three different concentrations. Relative recovery ranged from 98 to 100.2% at three different concentrations. Preliminary stability tests show that ciprofloxacin is stable for at least 3 weeks in serum after freezing.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1583077&dopt=Abstract
J Exp Med. 1992 Nov 1;176(5):1439-47.
Gemfibrozil enhances the listeriacidal effects of fluoroquinolone antibiotics in J774 macrophages.
Rudin DE, Gao PX, Cao CX, Neu HC, Silverstein SC.
Department of Physiology and Cellular Biophysics, Columbia University, New York, New York 10032.
J774 macrophage-like cells express organic anion transporters that promote the efflux of fluoroquinolone antibiotics such as norfloxacin (NFX) from these cells. Gemfibrozil (GFZ) blocks organic anion transport in J774 cells, thereby facilitating the intracellular accumulation of NFX (Cao, C., H.C. Neu, and S.C. Silverstein. 1991. J. Cell Biol. 115:467a [Abstr.]). To determine whether GFZ enhances the efficacy of fluoroquinolone antibiotics against intracellular bacterial pathogens, J774 cells were infected with Listeria monocytogenes and incubated in medium containing a fluoroquinolone antibiotic in the presence or absence of GFZ. Intracellular growth of L. monocytogenes was evaluated by lysing J774 cells and assaying for colony-forming units of Listeria. GFZ intensified the bacteriostatic effect of 4 micrograms/ml NFX and rendered 8 micrograms/ml bactericidal for L. monocytogenes. GFZ had a similar potentiating effect when used in combination with 2 micrograms/ml ciprofloxacin (CFX). CFX plus GFZ was bactericidal for intracellular L. monocytogenes. Treatment of J774 cells with NFX plus GFZ markedly reduced the cytotoxic effect of the bacteria on these cells. Over 55% of cells treated with 8 micrograms/ml NFX alone were dead 16 h after infection, whereas only 5% of cells treated with 8 micrograms/ml NFX plus GFZ were dead at 16 h. Similarly, GFZ potentiated the ability of 2 micrograms/ml to protect J774 cells against the cytocidal effect of Listeria. NFX in combination with GFZ limited cell-to-cell spread of L. monocytogenes. In antibiotic-free medium, > 99% of J774 cells contained intracellular L. monocytogenes at 14 h after infection. NFX alone in the medium did not change this outcome. However, 4 micrograms/ml NFX plus GFZ decreased bacterial spread by approximately 40% at 24 h postinfection, and 8 micrograms/ml NFX plus GFZ prevented all spread beyond the initially infected cell population. These results suggest that GFZ could be used clinically to enhance the efficacy of fluoroquinolone and of other anionic antibiotics against bacteria that grow and/or reside within macrophages and/or other cells.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1402686&dopt=Abstract
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