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J Antimicrob Chemother. 1994 Sep;34(3):383-90.
Effect of newer quinolones on the extra- and intra-cellular chemiluminescence response of human polymorphonuclear leucocytes.

Aoki M, Ono Y, Kunii O, Goldstein E.

Second Department of Internal Medicine, Teikyo University School of Medicine, Tokyo, Japan.

The direct effect of four quinolones on the intracellular production and extracellular release of reactive oxygen species was investigated in vitro using a chemiluminescence (CL) assay. Polymorphonuclear leucocytes (PMNs) were obtained from healthy volunteers and exposed for 10 min at 37 degrees C to 1.6, 6.25 and 25 mg/L ofloxacin, ciprofloxacin, sparfloxacin and temafloxacin. The luminol-dependent CL response of the PMNs was then measured for 30 min following stimulation with nonopsonized zymosan or phorbol myristate acetate (PMA). The intracellular CL response was also measured for 30 min during phagocytosis of lumispheres. The integrated CL was calculated and compared for cells which were incubated with the antibiotic and unincubated controls. Preincubation with ofloxacin resulted in increased zymosan and PMA-induced, luminol-dependent CL. Similar increases were observed for ciprofloxacin except that 25 mg/L decreased the PMA-induced, luminol dependent CL. Preexposure to ofloxacin and ciprofloxacin did not affect lumisphere-induced CL significantly, although there was a tendency for this to decrease after exposure to ciprofloxacin. In contrast sparfloxacin and temafloxacin caused progressive decreases in zymosan and PMA-induced, luminol-dependent PMN CL which reached statistical significance at the higher concentrations. The same pattern was observed in the experiments using lumispheres. These findings indicate that these quinolones modulate the oxygen metabolism of PMNs and that this effect varies with the individual drug.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7829412&dopt=Abstract




Antimicrob Agents Chemother. 1998 Feb;42(2):289-92.
Influence of renal failure on ciprofloxacin pharmacokinetics in rats.

Nouaille-Degorce B, Veau C, Dautrey S, Tod M, Laouari D, Carbon C, Farinotti R.

Service de Pharmacie Clinique et des Biomateriaux, G. H. Bichat-C. Bernard, Paris, France.

Ciprofloxacin pharmacokinetics have been shown to be modified in patients with renal failure (e.g., the intestinal secretion of ciprofloxacin is increased). This study investigated the influence of renal failure on the pharmacokinetics of ciprofloxacin following oral and parenteral administration to rats of a dose of 50 mg/kg of body weight. After parenteral administration, only renal clearance (CLR) was reduced in nephrectomized rats (5.3+/-1.4 versus 17.8+/-4.7 ml/min/kg, P < 0.01, nephrectomized versus control rats). However, nonrenal clearance was increased in nephrectomized rats (32+/-4 versus 15+/-5 ml/min/kg, P < 0.01, nephrectomized versus control rats), suggesting compensatory mechanisms for reduced renal function. After oral administration, apparent total clearance and CLR were reduced (P < 0.01) in nephrectomized rats (117+/-25 and 6.8+/-4.4 ml/min/kg, respectively) compared with the values for control rats (185+/-9 and 22.6+/-5.3 ml/min/kg, respectively) and the area under the concentration-time curve was higher (P < 0.01) for nephrectomized rats (436.3+/-90.5 mg. min/liter) than for control rats (271.3+/-14.3 mg.min/liter). Terminal elimination half lives in the two groups remained constant after oral and parenteral administration. These results suggest an increased bioavailability of ciprofloxacin in nephrectomized rats, which was confirmed by a nonlinear mixed-effect model.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9527774&dopt=Abstract




J Antimicrob Chemother. 1993 Apr;31(4):497-504.
The in-vitro activity of OPC-17116, a new 5-methyl substituted quinolone.

Wise R, Andrews JM, Brenwald N.

Department of Microbiology, Dudley Road Hospital, Birmingham, UK.

The in-vitro activity of the new 5-methylated fluoroquinolone OPC-17116 was compared with that of other fluoroquinolines and beta-lactams against a total of 690 bacterial strains. With the exception of Klebsiella and Serratia spp., 90% of the Enterobacteriaceae were inhibited by 0.25 mg/L. OPC-17116 inhibited 90% of Serratia spp. at 8 mg/L and Klebsiella spp. at 4 mg/L. Moraxella catarrhalis and Haemophilus influenzae were highly susceptible (MIC90 < or = 0.03 mg/L). Pseudomonas aeruginosa were more susceptible to ciprofloxacin (MIC90 0.25 mg/L) than OPC-17116 (MIC90 1 mg/L). Generally, OPC-17116 was more active than ciprofloxacin against Gram-positive cocci, 90% of Staphylococcus spp. being inhibited by < or = 0.25 mg/L. OPC-17116 displayed greater activity than ciprofloxacin against Chlamydia spp. (MICs < or = 0.12 and < or = 2 mg/L, respectively).

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8390433&dopt=Abstract













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