Drugs online research references
Antimicrob Agents Chemother. 1990 Jun;34(6):1088-93.
Mechanism of action of lomefloxacin.
Piddock LJ, Hall MC, Wise R.
Department of Medical Microbiology, University of Birmingham Medical School, United Kingdom.
The inhibition of supercoiling activity of reconstituted Escherichia coli DNA gyrase by lomefloxacin, ciprofloxacin, and norfloxacin was determined. The concentrations of quinolones needed to inhibit DNA synthesis in Escherichia coli, Enterobacter cloacae, Serratia marcescens, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus were also measured. The kinetics of uptake of [14C]lomefloxacin and unlabeled lomefloxacin into whole cells of E. coli KL-16 and S. aureus NCTC 8532 and the induction of RecA in E. coli GC2241 were assayed. All strains had wild-type susceptibilities to quinolones. The concentration of quinolones needed to inhibit DNA synthesis by 50% correlated with the MIC for members of the family Enterobacteriaceae and P. aeruginosa. The concentration of quinolones needed to inhibit DNA synthesis by 50% for late-logarithmic-phase S. aureus also correlated with the MIC, unlike the data from early-logarithmic-phase cultures. E. coli and S. aureus showed a similar pattern of uptake kinetics of [14C]lomefloxacin and unlabeled lomefloxacin, indicating that the difference in the susceptibilities of the two species is probably due to different target site affinities. Essentially, lomefloxacin was less active than ciprofloxacin and ofloxacin and had activity similar to those of norfloxacin and enoxacin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2168142&dopt=Abstract
J Antimicrob Chemother. 1988 Dec;22(6):881-4.
In-vitro assessment of lomefloxacin (SC-47111)--a new quinolone derivative.
Finch R, Martin J, Pilkington R.
Department of Microbial Diseases, City Hospital, Nottingham, UK.
The activity of lomefloxacin (SC-47111) was studied in vitro against 500 clinical isolates. Comparison was made with enoxacin and ciprofloxacin. Lomefloxacin was comparable in activity to enoxacin, but less active than ciprofloxacin. Most Gram-negative bacilli were susceptible, including several multi-resistant strains. Pseudomonas aeruginosa showed variable susceptibility. Streptococci, including Streptococcus pneumoniae, were generally the least susceptible organisms.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3243735&dopt=Abstract
Diagn Microbiol Infect Dis. 1989 May-Jun;12(3 Suppl):29S-34S.
Bactericidal activity of lomefloxacin SC 47111 (NY-198) and ciprofloxacin against selected pathogens.
Stratton CW, Weeks LS.
Department of Pathology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232.
The bacterial activity of lomefloxacin and ciprofloxacin against selected pathogens was compared using kill-kinetic methods to assess inhibitory (1 x MIC) and suprainhibitory (4 x MIC) concentrations. Five strains each of the following microorganisms were studied: Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. We found that lomefloxacin was 8- to 16-fold less active than ciprofloxacin as measured by MICs. However, the bactericidal activities of both lomefloxacin and ciprofloxacin were comparable when concentrations 1 x MIC and 4 x MIC were tested. For many of the isolates tested, such concentrations would be achieved clinically. The low MICs seen for the Gram-negative bacilli did not correlate with killing ability for either drug: concentrations 8-16 x MIC were needed for 99.9% killing of the final inoculum. Although higher concentrations of lomefloxacin are needed for inhibitory and bactericidal activity, the improved pharmacokinetics of lomefloxacin may result in this agent being comparable to ciprofloxacin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2791495&dopt=Abstract
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