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 aminothiazolyl-cephalosporin RU 29 246 is the active metabolite of the prodrug-pivaloyl-oxyethyl-ester HR 916. RU 29 246 in vitro activity includes a wide range of clinically relevant bacterial pathogens. Against methicillin-sensitive Staphylococci RU 29 246 (MIC90 of 0.25 approximately 2 micrograms/ml) was clearly more active than cefaclor, cefuroxime, cefpodoxime, cefixime and ceftibuten, but slightly less active than cefdinir. RU 29 246 inhibited hemolytic Streptococci of the serogroups A, B, C and G as well as penicillin-sensitive Streptococcus pneumoniae at concentrations similar to cefdinir, cefpodoxime and cefuroxime (MIC90 less than or equal to 0.13 micrograms/ml), but less than the other oral cephalosporins investigated (cefixime, cefaclor and ceftibuten). MIC90s of RU 29 246 against Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Salmonella spp., Shigella spp., Proteus mirabilis and Haemophilus influenzae were less than or equal to 0.5 micrograms/ml. Only RU 29 246 and cefdinir demonstrated moderate activity against Acinetobacter baumannii (MIC90 greater than or equal to 4 micrograms/ml). Most strains of Pseudomonas spp., Serratia marcescens, Enterobacter spp., Hafnia alvei and Bacteroides spp. were resistant to RU 29 246. RU 29 246 killed Escherichia coli and Staphylococcus aureus at a rate of 99% to 99.9% at concentrations of two times MIC. The pH value of the medium (range 5.5 to 8.5) and the inoculum size (range 10(5) to 10(7) cfu/ml) had no or only low influence on the antibacterial activity of RU 29 246. RU 29 246 is a broad spectrum cephalosporin including in its activity both Gram-positive and Gram-negative pathogens and therefore--depending on the bioavailability of its prodrug--looks promising as to its therapeutic perspective.
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PMID:RU 29 246, the active compound of the cephalosporin-prodrug-ester HR 916. I. Antibacterial activity in vitro. 159 83

In a randomized crossover trial, six volunteers received 200- and 400-mg doses of loracarbef (LY 163892), a new oral cephalosporin. Mean +/- standard error of the mean concentrations in serum obtained after 1.5 and 3 h were 13.2 +/- 2.8 and 4.3 +/- 0.7 mg/liter, respectively, after the 400-mg dose and 6.9 +/- 1.0 and 1.7 +/- 0.2 mg/liter, respectively, after the 200-mg dose. Bactericidal reciprocal titers measured against respiratory pathogens in serum suggested that loracarbef would be highly effective against Streptococcus pneumoniae and Streptococcus pyogenes (median titers, 8 to 128 at 1.5 h and less than 2 to 32 at 3 h) and beta-lactamase-negative Haemophilus influenzae (median titers, 4 at 1.5 h and 2 to 4 at 3 h). Other species (Branhamella catarrhalis, Streptococcus anginosus, Staphylococcus aureus) were associated with lower bactericidal titers. Killing curves performed against 12 strains demonstrated that the bioactivity of loracarbef (measured by the reduction in the area under the control growth curve) was significantly correlated with the concentration/MIC ratio, whereas the initial rate of killing was not, once the concentration was greater than the MIC. Our results suggest that administration of 400 mg of loracarbef every 8 h might be associated with more favorable pharmacodynamic parameters against target bacteria.
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PMID:Bactericidal titers of loracarbef (LY 163892) in serum and killing rates in volunteers receiving 400 versus 200 milligrams. 162 60

It was noted in our laboratory that certain strains of Haemophilus influenzae yielded zone sizes interpreted as resistant to the ampicillin (AMP) disk on chocolate-Mueller-Hinton agar (CMH) but showed no evidence of beta-lactamase (beta-Lac) activity. Although it is known that a second mechanism of AMP resistance exists, strains with this mechanism are uncommon. To investigate this apparent discrepancy, a study of 100 consecutive clinical isolates of H. influenzae collected over a 6-month period was performed. Isolates were simultaneously tested against five antibiotics (AMP, chloramphenicol, cefotaxime, ciprofloxacin, and AMP-sulbactam) on CMH and on two brands of Haemophilus test medium (HTM) by using the disk diffusion procedure and National Committee for Clinical Laboratory Standards (NCCLS) standards. By using CMH and NCCLS standard M2-A3-S2, strains of H. influenzae showing zone sizes of greater than or equal to 20 mm with AMP were considered sensitive. By using HTM and NCCLS standard M2-A4, strains showing zone sizes of greater than or equal to 25 mm to AMP on HTM were considered sensitive. Intermediate strains had zone sizes of 22 to 24 mm. The majority of isolates (68%) were sensitive to all antibiotics. Two percent of the isolates were resistant to chloramphenicol. Seventeen percent of the isolates were AMP-resistant, beta-Lac-producing strains of H. influenzae. Thirteen percent of the isolates gave at least one intermediate or resistant zone for AMP but were beta-Lac negative. MIC determinations with NCCLS standard M7-A2 were performed with resistant and intermediate strains. MICs for beta-Lac-producing strains of H. influenzae were >/= 8.0 microgram/ml. MICs for beta-Lac-negative strains were </= 1.0 microgram/ml and were highly reproducible. If one uses the current NCCLS zone diameter interpretive criteria, results should be viewed with caution. Further investigation of zone size interpretive criteria is warranted. It is suggested that in the case of serious infections with H. influenzae, beta-Lac-negative, AMP-resistant or -intermediate strains be confirmed by the MIC procedure.
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PMID:Investigation of ampicillin-intermediate strains of Haemophilus influenzae by using the disk diffusion procedure and current National Committee for Clinical Laboratory Standards guidelines. 162 20

Mersacidin, a new peptide antibiotic, was four- to eightfold less active (MIC for 90% of isolates, 8 micrograms/ml) than vancomycin, teicoplanin, or daptomycin against Staphylococcus aureus. Coagulase-negative staphylococci were inhibited by 8 micrograms/ml, and the MICs of mersacidin for hemolytic streptococci and Streptococcus pneumoniae were 4 to 8 micrograms/ml. The mersacidin MICs for anaerobic organisms were as follows: Clostridium perfringens, 4 micrograms/ml; Propionibacterium acnes, 8 micrograms/ml; peptococci, 1 microgram/ml; and peptostreptococci, 8 micrograms/ml. Mersacidin had no activity against members of the family Enterobacteriaceae, Neisseria and Haemophilus species, or Pseudomonas aeruginosa. The size of the inoculum, the pH of the assay (5.5 to 7.5), the type of medium, and the anaerobic conditions had minimal effects on the MICs and MBCs of mersacidin. Overall, mersacidin proved less active than available glycopeptides and peptolides.
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PMID:Activity of mersacidin, a novel peptide, compared with that of vancomycin, teicoplanin, and daptomycin. 164 77

Temafloxacin, like other 4-quinolones, was highly active against most isolates of Enterobacteriaceae. It was slightly less active than ciprofloxacin but approximately as active as ofloxacin and enoxacin. It was the most active of the quinolones against Acinetobacter spp. and Xanthomonas maltophilia but was slightly less active than ciprofloxacin against Pseudomonas spp. Temafloxacin was highly active against Haemophilus influenzae, Moraxella catarrhalis and Neisseria gonorrhoeae and was the most active of the quinolones against Gardnerella vaginalis and Campylobacter coli/jejuni. It was more active than ciprofloxacin against most staphylococci and equally active against streptococci and enterococci. Temafloxacin was the most active quinolone against anaerobic bacteria and, with the exception of a few isolates of Bacteroides spp. and some clostridia, all anaerobes were within the sensitive range (MIC less than or equal to 2 mg/l).
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PMID:The in-vitro activity of temafloxacin compared with other antimicrobial agents. 165 55

In vitro experiments were performed in which 6 to 12 strains of Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae and Enterobacteriaceae were passaged nine times in sub-lethal concentrations of azithromycin or control antibiotics. Streptococcus pyogenes and Staphylococcus aureus quickly became resistant to rifampin as the MIC90 increased from 0.1 to greater than 50 micrograms/ml for both species. The MIC90 of azithromycin, erythromycin, amoxicillin and cefaclor increased by three dilutions for Staphylococcus aureus. The MIC values of azithromycin for Streptococcus pyogenes, Haemophilus influenzae and Enterobacteriaceae strains did not change significantly. However, for Haemophilus influenzae and the Enterobacteriaceae strains, the MIC values of erythromycin and oral cephalosporins increased four-fold. In the in vivo experiments, mice infected with Staphylococcus aureus or Escherichia coli contaminated sutures were administered azithromycin for three days, and on day 6 viable bacterial cells were recovered from the infection site. The sustained tissue concentrations of azithromycin indicated that the organisms would have been continuously exposed to azithromycin at the site of infection. Colonies isolated from azithromycin-treated and non-treated mice were cultured and their susceptibility to azithromycin compared. The azithromycin MIC values for Staphylococcus aureus cultures from treated and non-treated animals were identical. The azithromycin MICs for Escherichia coli recovered from treated animals were on average, less than one dilution higher than for control cultures. Emergence of significant resistance to azithromycin in the laboratory was not observed with the pathogens tested.
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PMID:Lack of emergence of significant resistance in vitro and in vivo to the new azalide antibiotic azithromycin. 166 28

Azithromycin and erythromycin disk test results were compared to MIC values obtained in six different media. One hundred isolates were tested in triplicate, and geometric mean MICs were plotted against arithmetic mean zone diameters and regression statistics calculated. The test media evaluated did not markedly influence MIC values, but incubation in 5-7% CO2 resulted in a two- to four-fold decrease in the activity of both drugs. For testing Haemophilus influenzae and other species that need to be tested in 5-7% CO2, interpretive breakpoints for the macrolides and azalides should be modified to compensate for the anticipated decrease in activity.
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PMID:Influence of the test medium on azithromycin and erythromycin regression statistics. 166 29

The strategy of antimicrobial therapy in acute otitis media rests on bacteriologic and pharmacokinetic data. Pneumococci and Haemophilus are still the two most prevalent pathogens in acute otitis media and raise problems regarding susceptibility: 25% of Haemophilus beta-strains produce beta-lactamases and 6 to 12% of pneumococci are intermediate or resistant to penicillin. Pharmacologic features required of antimicrobials used in acute otitis media include good penetration in the ear and sustained supra-MIC levels in middle ear fluid. Kinetics of drugs in the ear are still often incompletely understood. The last selection criterion is analysis of comparative trials. Available data do not point to superiority of any drug over the others. Amoxicillin should no longer be given as first-line therapy. Amoxicillin combined with clavulanic acid (Augmentin) is effective on the entire spectrum of causative organisms. Higher levels of amoxicillin may be needed (concomitant use of amoxicillin and (Augmentin). First-generation cephalosporins are effective but may prove unsuccessful in patients with large inocula. Pediazole is clinically effective although penetration of erythromycin in the ear is delayed. The new oral third generation cephalosporins are effective in infections due to beta-lactamase-producing Haemophilus strains. A bacteriologic study should be performed routinely whenever otitis media occurs in an infant under three months of age.
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PMID:[Antibiotic treatment of acute otitis media]. 174 53

Cefcanel is a new orally absorbed cephalosporin. Its activity was compared with that of cefuroxime, cefaclor, cephalexin, and cefixime against gram-positive and negative aerobic and anaerobic bacteria. Cefcanel had excellent activity against methicillin-susceptible Staphylococcus aureus and Staphylococcus epidermidis, MIC90 1 micrograms/ml, superior to the other oral cephalosporins. However, methicillin-resistant staphylococci were resistant, MIC greater than or equal to 16 micrograms/ml. Streptococcus pyogenes and Streptococcus pneumoniae were inhibited by 0.015-1 micrograms/ml, concentrations comparable to other cephalosporins. Clostridium spp. were inhibited by 0.25 micrograms/ml, 8- to 128-fold lower concentrations than were found for other agents, but the MICs were greater than 64 micrograms/ml for Bacteroides spp. The MIC90 for Moraxella catarrhalis was 1 micrograms/ml, similar to cefuroxime but 16-fold greater than the MICs of cefixime. Escherichia coli and Klebsiella pneumonia which were high beta-lactamase producers were resistant, MICs greater than 64 micrograms/ml, and 50% of Enterobacter cloacae and Citrobacter freundii were resistant. Cefcanel was hydrolyzed by TEM-1, TEM-3 and Moraxella Bro-1 beta-lactamases. Escherichia coli containing TEM-1, 2, 3, 5, 7, and 9 had cefcanel MICs of greater than or equal to 16 micrograms/ml. Although cefcanel inhibited gram-positive species as well as or at lower concentrations than other cephalosporins, it lacked activity against gram-negative species that produced common plasmid beta-lactamase although it inhibited Haemophilus influenzae carrying TEM-1.
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PMID:In vitro activity of cefcanel versus other oral cephalosporins. 174 25

Haemophilus influenzae, a normal host of the nasopharynx of humans, may become a pathogen. The first step of infection is adherence to epithelial cells of the nasopharynx through glycopeptidic adhesins, or pili. Adherence to human epithelial cells in continuous lines, HeLa and Hep2, of 8 piliated strains of Haemophilus influenzae isolated from human infections of the respiratory tract was studied in vitro in the presence of fusafungine, a local bacteriostatic antibiotic. When the bacteria were grown in the presence of 0.5 x the MIC, fusafungine afforded 45-75% of adherence inhibition, but this inhibitory effect did not parallel the MICs. In contrast, no significant effect could be observed either when epithelial cells were exposed to 0.5 x the MIC before use in the adherence assay, or when this assay was performed in the presence of 0.5 x the MIC of fusafungine. The partial adherence inhibition observed suggests that fusafungine interacts with the bacterial binding sites but that other mechanisms may contribute to the inhibitory process. This effect of fusafungine should prevent but not eradicate colonization of the nasopharyngeal mucosa by Haemophilus influenzae and may account for the therapeutic efficacy reported in infections of the respiratory tract due to Haemophilus influenzae.
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PMID:Effect of fusafungine on adherence of Haemophilus influenzae type b to human epithelial cells in vitro. 176 May 21


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