Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0348321 (Haemophilus)
 15,372 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Sparfloxacin (CI-978, AT-4140 and PD 131501) is a new antimicrobial agent of the piperazinyl quinolone class. Relative to other quinolones, it is a potent antistaphylococcal and antistreptococcal drug in vitro: The microbroth 90% minimum inhibitory concentration (MIC90) (in microgram/ml) was 0.25 vs 26 methicillin-resistant and -sensitive coagulase-positive and -negative staphylococci and 20 Streptococcus pneumoniae; 0.5 vs 20 strains each of S. pyogenes, S. agalactiae, and Enterococcus faecalis. The data indicate sparfloxacin to be generally superior to ciprofloxacin, ofloxacin, oxacillin, cefazolin, doxycycline, amikacin, and vancomycin against these Gram-positive bacterial groups. Additional MIC90s were determined for Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, and Neisseria gonorrhoeae (less than or equal to 0.03); Enterobacteriaceae (0.5); and Listeria monocytogenes (1). Activity was generally unchanged with light, 50% human serum, aerobic-anaerobic atmosphere, 5% sodium cholate, cation supplementation, and 100-fold increased or decreased inoculum; as with other quinolones, potency was measurably diminished with decreasing pH (pH less than or equal to 6.0) and in 100% urine. Naturally occurring resistant mutants occurred at frequencies of 10(-8) or lower.
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PMID:In vitro activity of sparfloxacin (CI-978, AT-4140, and PD 131501). A quinolone with high activity against gram-positive bacteria. 166 75

Sparfloxacin (AT-4140 and CI-978) was evaluated for activity against 194 clinical isolates of staphylococci, streptococci, Enterococcus faecalis, anaerobic Gram-positive cocci, and Haemophilus sp. The MIC of sparfloxacin for greater than 93% of the strains tested was less than or equal to 0.5 microgram/ml. Sparfloxacin demonstrated increased activity against enterococci, staphylococci, pneumococci, and anaerobic cocci when compared with ciprofloxacin.
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PMID:In vitro activity of sparfloxacin (AT-4140 and CI-978), a new quinolone antimicrobial agent, against Haemophilus and gram-positive cocci. 188 86

Sparfloxacin (AT-4140, CI-978, PD 131501) was tested against over 800 recent bacteremic strains and compared with ciprofloxacin and six other fluoroquinolones. The 90% minimum inhibitory concentration (MIC90) ranges for the Enterobacteriaceae species were (a) sparfloxacin, 0.03-1 microgram/ml and (b) ciprofloxacin, 0.015-0.25 microgram/ml. Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae were very susceptible to sparfloxacin (MIC90s, 0.004- less than or equal to 0.03 microgram/ml) and the other comparison drugs. Staphylococcus aureas and other staphylococci were generally susceptible to the tested fluoroquinolones but very susceptible to sparfloxacin and WIN 57273. All beta-hemolytic streptococci, enterococci, and pneumococci had sparfloxacin MICs of less than or equal to 1 microgram/ml. Sparfloxacin was quite active against anaerobic bacteria including Bacteroides fragilis gr. and Gram-positive strains (MIC90s, less than or equal to 2 micrograms/ml). The most resistant enteric bacilli were among Serratia marcescens and the Proteae, especially the Providencia spp. (two- to eightfold higher MICs). Pseudomonas aeruginosa strains were also susceptible to sparfloxacin (MIC90, 2 micrograms/ml). Magnesium ions, CO2 incubation, and low pH had some adverse effect on sparfloxacin MICs, and resistance development was documented among current clinical isolates of staphylococci, pseudomonas, and some enteric species.
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PMID:In vitro antimicrobial activity of sparfloxacin (AT-4140, CI-978, PD 131501) compared with numerous other quinolone compounds. 190 15

The in-vitro activity of sparfloxacin (AT-4140), a new difluorinated quinolone, was compared with those of ciprofloxacin, temafloxacin and selected members of other groups of antimicrobial agents, against 651 recent distinct clinical isolates and strains with known mechanisms of resistance. Three strains of Chlamydia trachomatis were also studied. The MICs for 90% of the Enterobacteriaceae were between 0.06 and 1 mg/l; for Pseudomonas aeruginosa the MIC90 was 2 mg/l. Sparfloxacin was 16-fold more active against Acinetobacter spp. than ciprofloxacin. For Staphylococcus spp., Streptococcus, spp. and Enterococcus faecalis the MIC90 was between 0.25 and 1 mg/l; sparfloxacin was four-fold more active against Str. pneumoniae than ciprofloxacin. Ninety percent of strains of Haemophilus influenzae, Branhamella catarrhalis and Neisseria spp. were inhibited by less than 0.03 mg/l; for Bacteroides fragilis the MIC90 was 1 mg/l. The three strains of Chl. trachomatis were susceptible to 0.06-0.12 mg/l sparfloxacin, which was 16-fold more active than ciprofloxacin. There was cross resistance among the quinolones, but not between the quinolones and other groups of antimicrobials. The protein binding of sparfloxacin was 40% and serum had little effect on its activity.
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PMID:In-vitro activity of sparfloxacin, a new quinolone antimicrobial agent. 207 49

The in vitro activity of sparfloxacin (CI-978; AT-4140) was compared with those of other antimicrobial agents against isolates of staphylococci, enterococci, and various respiratory tract pathogens. Sparfloxacin was the most active drug tested against staphylococci (MIC for 90% of the strains tested [MIC90], 0.125 micrograms/ml) and enterococci (MIC90, 1.0 microgram/ml). It was also active against Haemophilus influenzae (MIC90, less than or equal to 0.06 microgram/ml), Moraxella (Branhamella) catarrhalis (MIC90, 0.125 microgram/ml), Streptococcus pneumoniae (MIC90, 0.5 microgram/ml), and Streptococcus pyogenes (MIC90, 1.0 microgram/ml).
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PMID:Comparative in vitro activities of sparfloxacin (CI-978; AT-4140) and other antimicrobial agents against staphylococci, enterococci, and respiratory tract pathogens. 212 51

Sparfloxacin and levofloxacin were evaluated against 150 Haemophilus influenzae isolates and 149 Neisseria gonorrhoeae isolates in order to define susceptibility testing parameters. Sparfloxacin-susceptible H. influenzae strains were defined as those for which the MICs were < or = 0.25 microgram/ml and the zones were > or = 30 mm, and N. gonorrhoeae susceptible strains were those for which the MICs were < or = 0.03 microgram/ml and the zones were > or = 39 mm (5-micrograms disks). Levofloxacin-susceptible strains of H. influenzae included those for which the MICs were < or = 0.12 microgram/ml and the zones were > or = 32 mm and N. gonorrhoeae susceptible strains were those for which the MICs were < or = 0.12 microgram/ml and the zones were > or = 37 mm (5-micrograms disks). Criteria for a resistant category cannot yet be defined for either quinolone. In multilaboratory studies with different lots of Haemophilus Test Medium, replicate tests with the standard control strain of H. influenzae (ATCC 49247) were evaluated. For sparfloxacin disk tests, the proposed zone size limits were 33 to 42 mm and broth microdilution MIC limits were 0.004 to 0.016 microgram/ml, whereas for levofloxacin tests, zone size limits were 32 to 41 mm and broth microdilution MIC limits were 0.008 to 0.03 microgram/ml. Other multilaboratory studies evaluated tests with supplemented GC agar and N. gonorrhoeae ATCC 49226; for both drugs, zone size limits were 44 to 52 mm and agar dilution MIC limits were 0.004 to 0.016 microgram/ml.
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PMID:Tentative criteria for confirming the in vitro susceptibilities of Haemophilus influenzae and Neisseria gonorrhoeae to two fluoroquinolones (sparfloxacin and levofloxacin), including quality control parameters. 840 59

We determined the bactericidal kinetics and postantibiotic effect (PAE) of sparfloxacin against Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, Klebsiella pneumonia, Streptococcus pneumoniae, and Staphylococcus aureus. Time-kill studies were performed by using 1 x and 4 x the minimum inhibitory concentrations (MICs) of sparfloxacin, ciprofloxacin, co-trimoxazole, amoxicillin/clavulanic acid and erythromycin (inoculum 10(5) and 10(7) CFU/ml). The PAE was induced by exposing the strains to 1xMIC and 4xMIC of sparfloxacin and ciprofloxacin for 1 h. Sparfloxacin was the most bactericidal of all the antibiotics tested, being active against Gram-positive and Gram-negative isolates with a 99.9% reduction within 3 to 6 h of exposure, depending upon strain, inoculum and concentration. The PAE of sparfloxacin against all species tested ranged from 1.1 to 2.6 hours; the most notable PAE occurring with M. catarrhalis.
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PMID:Bactericidal kinetics and postantibiotic effect of sparfloxacin against selected species of respiratory pathogens. 866 38

In a double-blind, placebo-controlled trial, patients with acute exacerbations of chronic obstructive pulmonary disease (COPD) were randomly allocated to oral treatment with sparfloxacin (200 mg loading dose followed by 100 mg once daily) or amoxycillin/clavulanic acid (500 mg/125 mg tds) for a total treatment duration of 7 to 14 days. Patients were evaluable if they had a FEV1/FVC ratio of less than 70% at stable state and presented with a suspected infectious exacerbation defined as increases in dyspnoea, sputum volume and sputum purulence. The primary efficacy variable was the overall success (defined as disappearance or improvement of dyspnoea and reductions in sputum volume and purulence) at end of treatment and follow-up. Overall efficacy was assessed in both the intent-to-treat (728 patients) and the evaluable (351 patients) populations. At the end of treatment and follow-up, success rates were identical for the sparfloxacin (87.3% and 78.7%) and amoxycillin-clavulanic acid (88.8% and 79.8%) treatment groups. Similar figures were found for the intent-to-treat population. The analysis of drug safety was similar for both treatment groups. The most frequently encountered pathogens were Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Sparfloxacin appeared superior for bacteriological eradication of Haemophilus influenzae, and Moraxella catarrhalis. Sparfloxacin in a single daily dose appears at least as effective as amoxycillin/clavulanic acid in the treatment of patients with acute exacerbations of COPD.
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PMID:Comparative safety and efficacy of sparfloxacin in the treatment of acute exacerbations of chronic obstructive pulmonary disease: a double-blind, randomised, parallel, multicentre study. 873 29

Sparfloxacin is a piperazinyl, cyclopropyl-fluoroquinolone with broad-spectrum antibacterial activity. Compared to other quinolones, sparfloxacin displays improved activity against a variety of pathogens including Staphylococcus, Streptococcus, Enterococcus, Chlamydia, Mycoplasma, Ureaplasma, and Mycobacteria species. Other susceptible organism group include Haemophilus, Legionella, Moraxella, Neisseria, Aeromonas, Acinetobacter, Bordetella, Brucella, Campylobacter, Gardnerella, and Helicobacter species. Most Enterobacteriaceae are also susceptible, whereas most isolates of Pseudomonas aeruginosa are not. Sparfloxacin is bactericidal. Activity is generally stable to variations of inoculum, pH, and cation concentration, and it is unchanged in the presence of 5% sodium cholate or 70% human serum. Susceptibility to the drug is diminished in urine. Cross-resistance, although incomplete, has been documented with other quinolones, but not with other antimicrobic classes.
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PMID:Sparfloxacin worldwide in vitro literature: isolate data available through 1994. 888 90

Sparfloxacin, a new orally administered fluoroquinolone, was tested against 14,182 clinical strains isolated (generally blood stream and respiratory tract cultures) at nearly 200 hospitals in the United States (USA) and Canada. Sparfloxacin activity was compared with 13 other compounds by Etest (AB BIODISK, Solna, Sweden), broth microdilution, or a standardized disk diffusion method. Using the Food and Drug Administration/product package insert MIC breakpoint for sparfloxacin susceptibility (< or = 0.5 microgram/ml), 94% of Streptococcus pneumoniae (2666 isolates) and 89% of the other streptococci (554 isolates) were susceptible. However, at < or = 1 microgram/ml (the breakpoint for all nonstreptococcal species) sparfloxacin susceptibility rates increased to 100% and 98%, respectively, for the two groups of streptococci. Only 50% and 65% of pneumococci were susceptible to ciprofloxacin (MIC90, 3 micrograms/ml) and penicillin (MIC90, 1.5 micrograms/ml), respectively. Although there were significant differences between regions in the USA in the frequency of penicillin-resistant pneumococcal strains, results indicate that the overall sparfloxacin MIC90 was uniformly at 0.5 microgram/ml. Nearly all (> or = 99%) Haemophilus species and Moraxella catarrhalis, including those harboring beta-lactamases, were susceptible to sparfloxacin, ciprofloxacin, and amoxicillin/clavulanic acid. Only cefprozil and macrolides demonstrated lower potency and spectrum against these two species. Sparfloxacin was active against oxacillin-susceptible Staphylococcus aureus (96 to 97%), Klebsiella spp. (95%), and other tested enteric bacilli (93%). Comparison between broth microdilution MIC and disk diffusion interpretive results for M. catarrhalis, Staphylococcus aureus, and the Enterobacteriaceae showed an absolute intermethod categorical agreement of > 95% using current sparfloxacin breakpoints, in contrast to those of cefpodoxime for S. aureus where a conspicuous discord (98% versus 59%) between methods was discovered. These results demonstrate that sparfloxacin possesses sufficient in vitro activity and spectrum versus pathogens that cause respiratory tract infections (indications), especially strains resistant to other drug classes such as the earlier fluoroquinolones, oral cephalosporins, macrolides, and amoxicillin/clavulanic acid. The sparfloxacin susceptibility breakpoint for streptococci may require modification (< or = 1 microgram/ml) based on the MIC population analysis presented here. A modal MIC (0.38 to 0.5 microgram/ml) was observed at the current breakpoint. Regardless, sparfloxacin inhibited 89% (nonpneumococcal Streptococcus spp.) to 100% (Haemophilus spp., M. catarrhalis) of the isolates tested with a median activity of 97% against indicated species.
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PMID:Comparative in vitro assessment of sparfloxacin activity and spectrum using results from over 14,000 pathogens isolated at 190 medical centers in the USA. SPAR Study Group. 940 10


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