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)

The in-vitro activity of two new quinolone antimicrobials, rufloxacin and MF 961, together with the desmethylated metabolite of rufloxacin (MF 922) were compared with other orally administered agents against 622 bacterial strains. Against Enterobacteriaceae and Pseudomonas aeruginosa rufloxacin was generally active (MIC90 1-8 mg/L) with the exception of Klebsiella and Serratia spp. (MIC90 32 mg/L and Enterobacter spp. (MIC90) 64 mg/L. The respiratory pathogens Haemophilus influenzae and Moraxella catarrhalis were susceptible to rufloxacin (MIC90 0.5 and 1 mg/L respectively) but Streptococcus pneumoniae was less susceptible (MIC90 32 mg/L). Staphylococcus aureus were susceptible to rufloxacin (MIC90 2 mg/L). The rufloxacin metabolite MF 922 was generally as active as its parent. MF 961 was usually two-fold more active than rufloxacin. All three compounds were four to 16 times less active than norfloxacin, but rufloxacin was as active or somewhat more active than norfloxacin against Staphylococcus spp. Any strains showing decreased susceptibility to other quinolones exhibited cross resistance to these new agents. The MBC of rufloxacin and MF 922 was within one dilution of the MIC and human serum had little effect upon the activity of both agents. The protein binding of rufloxacin and MF 922 at 1 and 10 mg/L were 55% and 63.8% and 30.3% and 32.6% respectively. The activity of rufloxacin against four strains of Chlamydia trachomatis and one strain of Chlamydia pneumoniae was determined. The MICs for C. trachomatis were 4-8 mg/L and 4 mg/L for C. pneumoniae.
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PMID:The in-vitro activity of two new quinolones: rufloxacin and MF 961. 132 39

The plasma bactericidal activity of a new C-5 methyl fluoroquinolone, OPC-17116, was determined after once-daily oral ingestion of 400 mg and 800 mg in normal, healthy volunteers. OPC-17116 at a 400-mg dose produced plasma bactericidal titers greater than or equal to 1:16 at 12 hours against Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Haemophilus influenzae, and Moraxella catarrhalis. OPC-17116 bactericidal titers against Pseudomonas aeruginosa were 1:2 or 1:4 at 6 and 12 hours. The plasma bactericidal titers against Streptococcus pyogenes and Streptococcus pneumoniae were 1:4 or greater, but bactericidal titers against Staphylococcus aureus were 1:2 at 12 hours and less than 1:2 at 24 hours. The 800-mg dose of OPC-17116 produced bactericidal titers of at least 1:32 at 12 hours for the Enterobacteriaceae, Haemophilus, and Moraxella, and 1:4 for S. pyogenes and S. pneumoniae, but bactericidal titers against S. aureus were 1:2. These data would suggest that an 800-mg dose of OPC-17116 taken orally once daily would provide adequate concentrations to treat infections due to the pathogens examined in this study.
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PMID:Plasma bactericidal activity of a new C-5 methyl fluoroquinolone after oral doses of 400 and 800 mg. 133 Dec 5

AM-1155 is a new quinolone with a wide spectrum of antibacterial activity against various bacteria including anaerobes and Mycoplasma pneumoniae. AM-1155 was 2- to 16-fold more active than ciprofloxacin and ofloxacin against Staphylococcus aureus including methicillin-resistant strains, Staphylococcus epidermidis, Streptococcus pneumoniae, and Enterococcus faecalis; its MICs for 90% of strains tested were 0.10 to 0.78 micrograms/ml. The activity of AM-1155 was comparable to that of ciprofloxacin against members of the family Enterobacteriaceae, Branhamella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae, but was fourfold less than that of ciprofloxacin against Pseudomonas aeruginosa. Against Xanthomonas maltophilia, Acinetobacter calcoaceticus, and Campylobacter jejuni, AM-1155 was two- to fourfold more active than ciprofloxacin. At a concentration of 1.56 micrograms/ml, AM-1155 inhibited 90% of Bacteroides fragilis strains tested; its activity was 8- to 10-fold higher than those of ofloxacin and ciprofloxacin. Development of resistance to AM-1155 in S. aureus and S. epidermidis occurred at a lower frequency than did that to ciprofloxacin after eight transfers in the presence of drug. In the oral treatment of mouse systemic infections, AM-1155 was four- to eightfold more effective than ciprofloxacin against gram-positive cocci and was as active as ciprofloxacin against gram-negative rods. The efficacy of an oral or a subcutaneous dose of AM-1155 was two- to fivefold greater than that of ofloxacin. Against experimental pneumonia with Klebsiella pneumoniae and P. aeruginosa, AM-1155 was two- to fourfold more active than ciprofloxacin and ofloxacin. AM-1155 also had good efficacy against mouse ascending urinary tract infections with Escherichia coli and P. aeruginosa. These results suggest that AM-1155 may be a potent antibacterial agent applicable to various infections.
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PMID:In vitro and in vivo antibacterial activities of AM-1155, a new 6-fluoro-8-methoxy quinolone. 133 87

The in vitro antibacterial activity of OPC-17116, a new fluoroquinolone, against a wide variety of clinical isolates was evaluated and compared with those of ciprofloxacin, ofloxacin, and norfloxacin. OPC-17116 showed potent broad-spectrum activity against gram-positive and -negative bacteria. The activity of this compound against gram-positive bacteria was higher than those of other quinolones, and its activity against gram-negative and anaerobic bacteria was roughly comparable to those of other quinolones. OPC-17116 had potent activity against important pathogens of respiratory tract infections such as Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Pseudomonas aeruginosa, Haemophilus influenzae, and Branhamella catarrhalis. The MICs of this compound against 90% of these organisms, except for methicillin-resistant S. aureus, ranged from less than or equal to 0.006 to 3.13 micrograms/ml. OPC-17116 at more than one-half the MICs was bactericidal against clinical isolates of S. aureus, Escherichia coli, K. pneumoniae, and P. aeruginosa. The activity of OPC-17116 was decreased by several culture conditions such as acidic pH, high concentration of Mg2+ ions, and inoculum size of 10(7) CFU/ml. OPC-17116 inhibited the supercoiling activity of DNA gyrases from E. coli KL-16 and S. aureus SA113 (50% inhibitory concentrations, 0.19 and 23.0 micrograms/ml, respectively). The amount of OPC-17116 accumulation was higher than that of other quinolones in S. aureus.
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PMID:Comparative in vitro activities of a new quinolone, OPC-17116, possessing potent activity against gram-positive bacteria. 133 89

A total of 818 clinical bacterial isolates were tested for the production of beta-lactamase by rapid chromogenic cephalosporin method and for the susceptibility to ticarcillin alone and in combination with clavulanic acid (2 micrograms/mL) by agar dilution method. These included 83 strains of methicillin-sensitive Staphylococcus aureus (MSSA), 31 of methicillin-resistant S. aureus (MRSA), 49 of Neisseria gonorrhoeae, 58 of Haemophilus influenzae, 112 of Escherichia coli, 118 of Klebsiella pneumoniae, 58 of Proteus mirabilis, 30 of Proteus vulgaris, 60 of Serratia marcescens, 113 of Enterobacter cloacae, 60 of Pseudomonas aeruginosa and 46 of Bacteroides fragilis. The results revealed that 46.6% of P. mirabilis, 53.4% of H. influenzae, 57.1% of N. gonorrhoeae, 80% of P. vulgaris, 83.9% of MRSA, 85.6% of MSSA, 87.5% of E. coli, 91.7% of S. marcescens, 95.7% of B. fragilis, 98.2% of E. cloacae, and 100% of K. pneumoniae and P. aeruginosa strains produced beta-lactamase. In general, beta-lactamase nonproducers were more susceptible to ticarcillin than beta-lactamase producers. The ranges of minimum inhibitory concentrations (MICs) of ticarcillin for beta-lactamase nonproducers of MSSA, MRSA, H. influenzae, E. coli, P. vulgaris, S. marcescens, E. cloacae, B. fragilis and beta-lactamase producers of MSSA, H. influenzae strains were all within the in vitro susceptible range. The presence of clavulanic acid resulted in a significant enhancement of the antibacterial activity of ticarcillin against beta-lactamase producers of MRSA, N. gonorrhoeae, E. coli, K. pneumoniae, P. mirabilis, P. vulgaris and B. fragilis strains. Clavulanic acid had no synergistic activity for ticarcillin against S. marcescens, P. aeruginosa and E. cloacae.
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PMID:In vitro antibacterial activities of ticarcillin alone and ticarcillin plus clavulanic acid against beta-lactamase producing and non-producing microorganisms. 134

Detailed structural analyses revealed a family of periplasmic chaperones in Gram-negative prokaryotes which are structurally and possibly evolutionarily related to the immunoglobulin superfamily and assist in the assembly of adhesive pili. The members of this family have similar structures consistent with the overall topology of an immunoglobulin fold. Seven pilus chaperone sequences from Escherichia coli, Haemophilus influenzae and Klebsiella pneumoniae were aligned and their consensus sequence was superimposed onto the known three-dimensional structure of PapD, a representative member of the family. The molecular details of the conserved and variable structural motifs in this family of periplasmic chaperones give important insight into their structure, function, mechanism of action and evolutionary relationship with the immunoglobulin superfamily.
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PMID:Conserved immunoglobulin-like features in a family of periplasmic pilus chaperones in bacteria. 134 92

We have analyzed the clinical significance of secondary infections associated with lung cancer patients. The incidence of secondary infections was 51.4% in 214 in-patients with lung cancer admitted to our institution in 1988 and 1989, and almost all of them had respiratory tract infections. The incidence was high in patients with cell types other than adenocarcinoma, and in those with hypoproteinemia, impaired cellular immunity and obstruction of the airway. The prognosis in patients with infection was much poorer than that in patients without infection. Major causative pathogens were Staphylococcus aureus including methicillin-resistant S. aureus (MRSA), Haemophilus influenzae, Klebsiella spp. and Pseudomonas aeruginosa. These pathogens except for H. influenzae were isolated at the terminal stage, in cases with airway obstruction and in post cancer-chemotherapeutic phase. The efficacy rate of 194 chemotherapeutic regimens against infection was 57.7%. Although the efficacy rate in 1988 and 1989 exceeded that in the 1970s, there was no significant difference in the efficacy rate between monotherapy (57.1%) and combined therapy (59.3%). The effectiveness was very poor for infections caused by P. aeruginosa and MRSA, or for cases with airway obstruction and marked impairment of pulmonary blood flow. The above results showed that a new combined therapy as well as the measures to improve the general condition of compromised hosts are required in the treatment of secondary infections in these patients.
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PMID:[Respiratory infections associated with lung cancer]. 137 Oct 46

BK-218 is a novel cephalosporin with a dual route of administration and spectrum of activity most similar to that of second-generation cephalosporins. BK-218 was active against Streptococcus pneumoniae, Haemophilus influenzae and Moraxella catarrhalis but strains resistant to penicillins had higher MICs. BK-218 had greater activity (8-fold) than cefuroxime or cefaclor against oxacillin-susceptible Staphylococcus spp. Moderate BK-218 activity was observed against Neisseria gonorrhoeae and commonly isolated Enterobacteriaceae such as Escherichia coli (MIC90, 1 mg/l), Klebsiella spp. (MIC90, 2 mg/l), and Proteus mirabilis (MIC90, 2 mg/l). The following organisms were generally BK-218-resistant (MIC90, greater than 16 mg/l): Bacteroides fragilis, Pseudomonas spp., Acinetobacter spp., Xanthomonas maltophilia, Citrobacter spp., Enterobacter spp., indole-positive Proteus, Serratia spp., enterococci and oxacillin-resistant staphylococci.
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PMID:Antibacterial activity of the investigational oral and parenteral cephalosporin BK-218. 139 35

An attempt was made to interpret the clinical significance of secondary infections associated with lung cancer. The incidence of secondary infections was 51.4% in 214 in-patients with lung cancer in our institution in 1988 and 1989, and almost all of them had respiratory infections caused by commonly encountered bacteria. The incidence of infection was high in lung cancer of cell types other than adenocarcinoma, and in those with hypoalbuminemia, impaired cellular immunity and obstruction of the airway. The prognosis in patients with infection was much poorer than that in patients without infection. Major pathogens responsible for infection were Staphylococcus aureus including methicillin-resistant S. aureus (MRSA), Haemophilus influenzae, Klebsiella spp. and Pseudomonas aeruginosa. These pathogens, except for H. influenzae, were isolated in the terminal stage in cases with airway obstruction and post cancer chemotherapy. The efficacy rate of 194 therapeutic regimens against infection was 57.7%. It was thus found that the efficacy rate in 1988 and 1989 exceeded that in the 1970s. The effectiveness was very poor for infections caused by S. aureus and P. aeruginosa, and for cases with airway obstruction and marked impairment of pulmonary blood flow. The efficacy rate of single-drug regimens was 57.1% (80/140) and that of combined regimens was 59.3% (32/54). The above results indicate that a new combined therapy which includes a beta-lactam antibiotic as well as measures to improve the general health of compromised hosts are required in the treatment of secondary infections in these patients.
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PMID:[Clinical significance of respiratory infections associated with lung cancer patients]. 140

We present the bacteriological findings in 329 aspirates from fiberoptic bronchoscopy. Quantitative cultures were not performed. 92 of the patients had radiologically confirmed pneumonia, 58 possibly had infectious bronchitis or pneumonia which was not verified radiologically, 154 had other pulmonary diseases and 25 had no verified pulmonary disease. 13% of aspirates contained no bacterial isolates and 33% revealed growth of multiple bacteria, classified as "normal pharyngeal flora". Among the 54% with specified bacterial findings the most frequent bacteria were viridans streptococci, staphylococci, Haemophilus influenzae, and Streptococcus pneumoniae. The differences in bacterial flora between the patient groups were only minimal. Klebsiella and Escherichia coli were the only bacteria indicating presence of pneumonia. S pneumoniae were found more frequently among patients with no signs of infection. Bronchial aspirates obtained with a fiberbronchoscope may give false positive results and are of limited value in diagnosing pneumonia. However, the presence of gram negative intestinal rods may indicate bacterial respiratory infection in hospitalized patients. Improving sampling and culture techniques can possibly improve the value of bacteriological findings.
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PMID:[Bacteriological examination of bronchial aspirates obtained via fiberoptic bronchoscopy]. 141 5


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