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Query: UNIPROT:Q29983 (MIC)
 21,138 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Disk diffusion zone diameter breakpoint criteria for Tosufloxacin and Lomefloxacin were tentatively established by correlating MICs with 1-, 5- and 10 micrograms of Tosufloxacin disk inhibitory zone diameters and with 10 micrograms of Lomefloxacin disk of those to 418 clinical isolates representing 32 species. We recommend 5 micrograms disks for Tosufloxacin with the following breakpoints: Susceptible (MIC, less than or equal to 0.5 microgram/ml), greater than or equal to 22 mm; intermediate, 17 to 21 mm; and resistant (MIC, greater than or equal to 2.0 micrograms/ml), less than or equal to 16 mm. We recommend 10 micrograms disks for Lomefloxacin with the following breakpoints: Susceptible (MIC, less than or equal to 2.0 micrograms/ml), greater than or equal to 21 mm; intermediate, 16 to 20 mm; and resistant (MIC, greater than or equal to 8.0 micrograms/ml), less than or equal to 15 mm. Using these criteria for Tosufloxacin and Lomefloxacin, the occurrence rate of major errors in judging susceptibility and resistance was 0.48%.
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PMID:[Evaluation of proposed criteria of disk susceptibility testing for tosufloxacin and lomefloxacin in NCCLS guidelines and WHO standards]. 131 83

Lomefloxacin has marked activity against Gram-negative bacilli including Enterobacteriaceae, non-fermenting strains and Haemophilus influenzae with 98% of all isolates tested having MICs of 0.25 mg/l or less. Sixty-eight per cent of Pseudomonas aeruginosa strains were sensitive to 1 mg/l with a few strains resistant to 8 or 16 mg/l. Gram-positive cocci were more resistant, particularly streptococci, where the MICs vary between 1 and 8 mg/l. Bactericidal activity was similar to inhibitory activity and the effect of increasing serum concentrations and bacterial inocula was minimal. The MIC and MBC were increased in the presence of urine, particularly at an acid pH 5. Comparative MICs showed that lomefloxacin was more active than ofloxacin and pefloxacin, similar to norfloxacin but less active than ciprofloxacin for Gram-negative bacteria but not for Gram-positive cocci. Comparative studies with sensitivity disc concentrations showed that a 5 micrograms disc was more satisfactory than the 10 micrograms disc as the zone sizes were more suitable for routine testing. Solutions of lomefloxacin showed instability in bright sunlight when 52% of activity was lost in 1 h. Similar instability was shown in impregnated discs which lost up to 40% activity in 6 h exposure. Lomefloxacin showed a wide range of activity against Gram-negative bacteria including multiresistant strains and Pseudomonas spp. Gram-positive bacteria were less susceptible, with streptococci more resistant than staphylococci. Lomefloxacin is well absorbed after oral administration giving high blood and urine concentrations and its prolonged half-life means once daily dosing in the treatment of many types of bacterial infection may be possible.
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PMID:Antibacterial activity of lomefloxacin. 188 17

A total of 3,144 clinical isolates from 3,011 consecutive patients were tested against lomefloxacin by the agar dilution method. They consisted of 1,380 isolates of Enterobacteriaceae, 527 pseudomonads, 47 Haemophilus influenzae, 53 Acinetobacter, 42 Brucella melitensis, 903 staphylococci and 192 strains of enterococci. In vitro activity of lomefloxacin was compared with ciprofloxacin, norfloxacin, beta-lactams and aminoglycosides. Over 98% of Enterobacteriaceae were susceptible to lomefloxacin with an MIC of 0.06-4.0 micrograms/ml. It also inhibited 93 and 85% clinical isolates of Pseudomonas aeruginosa and Xanthomonas maltophilia, respectively. All isolates of Haemophilus, Brucella and Staphylococcus aureus were susceptible to this fluoroquinolone. However, only 43% of the 192 strains of enterococci exhibited in vitro susceptibility. Lomefloxacin was found to be comparable to ciprofloxacin and norfloxacin in its in vitro activity, and superior to most penicillins, cephalosporins and aminoglycosides against both gram-negative and gram-positive bacteria except enterococci.
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PMID:In vitro activity of lomefloxacin, a difluorinated quinolone, compared with other antimicrobials. 188 4

Lomefloxacin (NY-198) is a chemotherapic agent from the new 4-quinolone group, acting on DNA gyrase system. Lomefloxacin (LFLX), as some other new 4-quinolone compounds are antimicrobials of potential use for ophthalmic application. A first approach on the oculotoxicity of LFLX is the main purpose of this study. Four concentrations of LFLX (10, 30, 100 and 300 micrograms/ml) were tested on the first subculture of pigmented rabbit corneal epithelial cells. Cell number, protein contents, neutral red stain and wound healing were evaluated. The results showed that the lower concentrations (10 & 30 micrograms/ml) had no effect while the highest one had a remarkable cytotoxic effect. Pharmacokinetic data show that peak values achieved in the cornea and other ocular structures are lower than 40 micrograms/g (0.3% topical application) and, on another hand, MIC values range from less than or equal to 0.05 to 16 micrograms/ml. So, these "critical" concentrations have no cytotoxic effects according to our results. Then, it is concluded that Lomefloxacin could be a useful drug for topical ophthalmic development.
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PMID:In vitro toxicity of lomefloxacin in rabbit corneal epithelial cell cultures. 210 Jan 73

The post-antibiotic effect (PAE) of lomefloxacin against Escherichia coli and Pseudomonas aeruginosa was determined and compared with various other antibiotics. All the quinolones tested, and chloramphenicol and gentamicin, possessed PAE activity. At 10 x MIC and 30 min exposure, the PAEs against E. coli were 1.6, 1.3, and 1.8 h for lomefloxacin, ciprofloxacin and norfloxacin respectively, and for P. aeruginosa the equivalent PAEs were 1.1, 1 and 0.5 h. The lomefloxacin PAE was dose-dependent and exposure for 5 min was sufficient to give optimal PAE at high concentrations of lomefloxacin. Such brief exposure rapidly blocked bacterial nucleic acid biosynthesis. Lomefloxacin pretreated bacteria were more susceptible to killing by PMN than untreated bacteria. Optimum enhancement of phagocytic killing of E. coli occurred when exposure to lomefloxacin was associated with an 80% decrease in cfu during pretreatment. Maximum PMN activity against P. aeruginosa occurred when bacteria were exposed to lomefloxacin producing change in cfu of +0.2 log10 to -0.7 log10. These results indicate that phenotypic changes of P. aeruginosa and E. coli exposed to lomefloxacin render the bacteria more susceptible to phagocytic killing.
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PMID:Lomefloxacin-induced modification of the kinetics of growth of gram-negative bacteria and susceptibility to phagocytic killing by human neutrophils. 210 16

The in vitro activity of lomefloxacin, a new difluoroquinolone, was compared with that of norfloxacin, ciprofloxacin, gentamicin and ceftazidime against a total of 577 recent clinical isolates. MICs were determined by a standard agar dilution procedure, and two inocula (10(4) and 10(6) CFU) were used throughout. Lomefloxacin inhibited most species of the Enterobacteriaceae, Staphylococcus aureus (including methicillin-resistant strains) and Haemophilus influenzae at less than or equal to 1 mg/l. Pseudomonas aeruginosa (MIC 90, 4 mg/l) was somewhat more resistant, and Pseudomonas maltophilia (MIC 90, 16 mg/l) and the Bacteroides fragilis group (MIC 90, 32 mg/l) were considerably more resistant. Overall, lomefloxacin was as active as norfloxacin, but was two- to eightfold less active than ciprofloxacin against most species tested.
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PMID:Comparative in vitro activity of lomefloxacin, a new difluoroquinolone. 249 1

Antibacterial activity of lomefloxacin was studied in the urine after single dose of 400 mg in ten healthy female volunteers. Urine was collected in 7 periods: 0-3 h, 3-6 h, 6-12 h, 12-24 h, 24-48 h, 48-72 h, 72-96 h. Lomefloxacin concentration were assayed in all samples by microbiological method. Urine antibacterial activity was determined towards five strains isolated in urine: 2 E. Coli strains one sensitive and the other resistant to nalidixic acid (Nal-A), 1 Klebsiella pneumoniae resistant to nalidixic acid (Nal-B), 1 Staphylococcus saprophyticus and 1 Streptococcus faecalis. MIC's of lomefloxacin against these strains were respectively 0.06, 0.50, 0.50, 0.25 and 4 micrograms/ml. Lomefloxacin mean concentrations were 208.5 +/- 44.2, 104.3 +/- 15.2, 100.5 +/- 17.9, 36.8 +/- 8.2, 9.6 +/- 2.2 micrograms/ml in the five first urine samples. Low levels were present in urine the 4th day. Mean urine elimination percentage was 62.2 +/- 4.2% for the four days, with extreme values from 91.2 to 41.8%. Urine bacteriostatic activity against enterobacteriacae was greater than or equal to 32 the first day reaching 8,192 for the Nal-S E. Coli, it was greater than or equal to 4 the second day. Against staphylococcus it was greater than or equal to 64 the first day, greater than or equal to 16 the second day. Against enterococcus it was greater than or equal to 4 the first day. Against the strains implicated in UTI a bacteriostatic activity was present during 2 days in all subjects.
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PMID:[Antibacterial activity of lomefloxacin in the urine during the 4 days following a single 400 mg oral dose]. 250 15

Lomefloxacin was found to be comparable to ciprofloxacin in its ability to inhibit the in vitro growth of Mycoplasma pneumoniae (MIC range 2-8 mcg/ml), but it was significantly less active than erythromycin. Although 30 different strains from widely differing geographic areas and isolation time periods were examined, no macrolide-resistant strains were observed.
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PMID:Comparative susceptibility of Mycoplasma pneumoniae to erythromycin, ciprofloxacin, and lomefloxacin. 251 25

The antimicrobial activity of a new fluoro-quinolone, lomefloxacin (NY-198, SC47111), was evaluated by standardized susceptibility testing methods at ten laboratories in Argentina. Lomefloxacin was found to be the most active drug against 1,316 recent clinical isolates compared directly to norfloxacin, co-trimoxazole, and gentamicin. Only 1.4% of Enterobacteriaceae were lomefloxacin-resistant (MIC greater than 4 micrograms/ml), and the lomefloxacin MIC90 for all staphylococci was 2 micrograms/ml, including methicillin-resistant isolates. Streptococci, enterococci, and some Pseudomonads (9% resistance) were less susceptible to lomefloxacin. Lomefloxacin was the most active against Neisseria gonorrhoeae strains compared to penicillin, cefuroxime, and spectinomycin. Among the tested Mycobacteria, only the nontuberculosis, slow growers had lomefloxacin MICs of greater than 4 micrograms/ml.
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PMID:A ten-laboratory study of lomefloxacin (NY-198 or SC 47111) antimicrobial activity in Argentina. 267 28

This was a randomized, double-blind, placebo-controlled study comparing the safety and tolerance of 400 mg lomefloxacin, given orally twice daily, to that of placebo administered to eight and four subjects, respectively, for 2 wk. This dose, interval, and duration of dosing were chosen to be identical to the highest anticipated clinical dose for the longest anticipated clinical duration. Subject assessments included ophthalmological examinations performed prior to the study, at midstudy, and after the dosing. No clinically significant differences from baseline were observed for any test result. Analysis of trough plasma concentrations, CMIN, showed that steady state was achieved on Day 4 (Fig. 2). At steady-state, mean plasma concentrations of lomefloxacin ranged from a maximum of 4.86 micrograms/ml to a minimum of 1.47 micrograms/ml. Mean time to maximum plasma concentration on Day 14 was 1.23 hr in the morning and 3.81 hr in the evening. Plasma half-life was approximately 8 hr. Lomefloxacin was well tolerated at 400 mg administered twice daily for 2 wk; plasma concentrations were maintained at a level that is above the MIC of most clinically significant isolates.
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PMID:Pharmacokinetics and safety of lomefloxacin following multiple doses. 275 16


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