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)

Cefuroxime-axetil, the 1-acetoxyethyl ester of cefuroxime, is a prodrug for oral administration. The indication of this new formulation in the treatment of community acquired RTI required an updating of its activity against respiratory pathogens. A total of 260 isolates were included in a study using MIC determination (agar dilution technique): the mode MICs for Haemophilus spp., Branhamella catarrhalis, streptococci, S. pneumoniae ranged from 0.016 to 0.5 mg/l; no difference was noted between beta-lactamase producers and non producers in Haemophilus and B. catarrhalis; coagulase positive staphylococci, E. coli, K. pneumoniae isolated from RTI exhibited mode MICs not exceeding 4 mg/l (except for methicillin-R staphylococci mode MIC greater than 128 mg/l). Simultaneously the pharmacokinetic parameters were determined in healthy volunteers after a loading dose (500 mg) of the drug: 7 consecutive samples collected after a light meal provided the following data: Cmax = 7.77 +/- 2.2 mg/l; Tmax = 2.33 +/- 0.23 hrs; t1/2 beta = 1.18 +/- 0.19 hrs; AUC = 22.17 +/- 6.4 h.mg/l. Cmax and AUC were half of these values after administration of 250 mg. These results, together with the known intrinsic beta-lactamase stability of cefuroxime, should ensure sufficient in vivo concentrations and effective in vivo antibacterial activity against most respiratory pathogens after oral administration of cefuroxime-axetil.
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PMID:[Role of cefuroxime-axetil in the treatment of respiratory tract infections. Bacteriological and pharmacological data]. 194 11

The pharmacokinetics of single doses of cefaclor at 250 and 375 mg and cefuroxime axetil at 250 mg administered under optimal conditions (i.e., cefuroxime axetil after food and cefaclor in the fasted state) were studied in 24 healthy male volunteers. Drug concentrations in serum were related to MICs for common respiratory tract pathogens by using data generated from a recently completed national survey. The time the concentrations in serum exceeded the MICs for Haemophilus influenzae, Streptococcus pneumoniae, and Moraxella (formerly Branhamella) catarrhalis were significantly greater (P less than 0.05) for cefuroxime axetil at 250 mg than for cefaclor at 250 or 375 mg. With the recommended dosing regimens (cefuroxime axetil at 250 mg and cefaclor at 375 mg twice daily or cefaclor at 250 mg three times daily), cefuroxime concentrations exceed the MIC for 90% of the strains tested for a greater time period than cefaclor concentrations with either regimen. The reasons for this difference are (i) the greater potency and slower clearance of cefuroxime compared with those of cefaclor and (ii) the greater sensitivity of these pathogens to cefuroxime.
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PMID:Pharmacokinetics of cefuroxime axetil and cefaclor: relationship of concentrations in serum to MICs for common respiratory pathogens. 195 58

The E-test (PDM Epsilometer; AB Biodisk, Solna, Sweden) is an antimicrobial agent gradient-coated plastic test strip which allows MIC determinations on agar media. The test is performed in a manner similar to the agar disk diffusion procedure. A collection of Haemophilus influenzae and Streptococcus pneumoniae strains possessing various resistance mechanisms was used to evaluate the E-test method. H. influenzae strains were tested with both Haemophilus test medium (HTM) and PDM ASM II chocolate agar, while the S. pneumoniae strains were tested on Mueller-Hinton sheep blood agar. E-test MICs for a total of 10 antimicrobial agents were compared with broth microdilution MICs determined according to National Committee for Clinical Laboratory Standards methods. In general, E-test MICs for both species were quickly and easily interpreted and agreed within one log2 MIC increment in 89.8% of tests with H. influenzae and in 80.4% of pneumococcal tests. The majority of disagreements between the E-test and conventional MICs occurred with trimethoprim-sulfamethoxazole because of trailing and diffuse E-test MIC endpoints with both species. Ampicillin MICs for beta-lactamase-producing H. influenzae determined by the E-test differed at times from those determined by conventional testing because of the vagaries of interpreting colonies growing within the E-test inhibition ellipses. E-test penicillin MICs for pneumococci tended to be 1 to 2 log2 dilutions lower than those determined by using Mueller-Hinton broth supplemented with lysed horse blood. Nevertheless, strains of both species with documented resistance to the study drugs were detected by E-tests, i.e., 0.7% of the tests had very major errors with H. influenzae and 0.8% had very major errors with S. pneumoniae. Thus, the E-test represents a potential alternative method for antimicrobial susceptibility testing of these two fastidious bacterial species.
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PMID:Quantitative antimicrobial susceptibility testing of Haemophilus influenzae and Streptococcus pneumoniae by using the E-test. 199 44

The in vitro activity of GR69153, a new catechol-substituted cephalosporin, was compared with those of ceftazidime, imipenem, meropenem, and ceftriaxone against 604 recent clinical isolates and other strains with known mechanisms of resistance. The MICs of GR69153 for 90% of the members of the family Enterobacteriaceae tested were less than 0.5 micrograms/ml, with the exceptions of those for Serratia spp. (4 micrograms/ml), Citrobacter spp. (2 micrograms/ml), and Enterobacter spp. (8 micrograms/ml). Ninety percent of Pseudomonas aeruginosa isolates were susceptible to less than or equal to 1 microgram of GR69153 per ml. With the exception of methicillin-resistant strains, 90% of Staphylococcus aureus isolates were susceptible to less than or equal to 2 micrograms/ml, and GR69153 was four- to eightfold more active than ceftazidime and ceftriaxone against these strains. Isolates of Haemophilus influenzae, Branhamella catarrhalis, Neisseria spp., and Streptococcus pneumoniae (penicillin susceptible) were highly susceptible (MIC for 90% of the strains, less than or equal to 0.12 micrograms/ml). GR69153 was stable to hydrolysis by the TEM-1 and TEM-5, SHV-1 and SHV-2, and K1 beta-lactamases, but some susceptibility to hydrolysis by the TEM-3, TEM-9, and P99 enzymes was observed. The protein-binding activity of GR69153 was 74.5 to 66.8%, depending on the concentration, and serum had little effect upon activity.
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PMID:In vitro activity of a catechol-substituted cephalosporin, GR69153. 202 66

Meropenem was 8- to 32-fold more active (MIC for 90% of strains = 0.125 micrograms/ml) than imipenem against a collection of Haemophilus influenzae strains characterized as either susceptible to ampicillin or resistant to that agent by virtue of beta-lactamase or nonenzymatic mechanisms. MBCs and kinetic kill curve tests showed that meropenem (as well as imipenem, several cephalosporins, and amoxicillin-clavulanate) was bactericidal against all strains at or within four times the respective MICs. Thus, meropenem demonstrated greater inhibitory activity than imipenem and activity comparable to that of cefotaxime against these selected strains.
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PMID:Activity of a new carbapenem antibiotic, meropenem, against Haemophilus influenzae strains with beta-lactamase- and non-enzyme-mediated resistance to ampicillin. 203 14

Non-beta-lactamase-mediated insusceptibility to beta-lactams was studied in Haemophilus influenzae. Mutants resistant to ampicillin were selected in a susceptible isolate, while phenotypically similar resistance was transformed from four wild-type isolates into a susceptible recipient. Ampicillin-selected mutants generally had reduced susceptibility to penicillins, cephalosporins and aztreonam. Reduced susceptibility to meropenem was less common, and susceptibility to imipenem was unaffected. MICs of three cephalosporins and aztreonam were much higher for the ampicillin-resistant transformants than for the recipient strain, and were generally equal to, or within one doubling dilution of, the concentrations that inhibited the donor parents. In contrast, reduced susceptibility to imipenem observed with one parent (MIC of 4 mg/l) was not transferred to the recipient (MIC of 0.5 mg/l). Meropenem inhibited 22 of 24 transformants tested at less than or equal to 0.12 mg/l, compared with MICs of greater than or equal to 0.5 mg/l for the donor parents and 0.03 mg/l for the recipient. These results indicated that the mechanisms that confer non-beta-lactamase-mediated insusceptibility to penicillins, cephalosporins and aztreonam in H. influenzae have little or no effect on susceptibility to carbapenems.
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PMID:Selection and transformation of non-beta-lactamase-mediated insusceptibility to beta-lactams in Haemophilus influenzae: lack of cross-resistance between carbapenems and other agents. 208 16

In the second European survey of the prevalence of antimicrobial resistance in Haemophilus influenzae, 2529 clinical isolates collected in 1988/89 from 78 laboratories in nine countries (Austria, Belgium, Federal Republic of Germany, France, Italy, The Netherlands, Spain, Switzerland, United Kingdom) were examined. Of these, 23.8% were type b strains. The overall rate of beta-lactamase production was 9.1%, being slightly higher in type b isolates (10.5%) compared to non-type b isolates (8.6%). The MICs of six antimicrobials (ampicillin, cefaclor, chloramphenicol, erythromycin, tetracycline, and cotrimoxazole) were determined by an agar dilution procedure at a single central laboratory. The proportion of isolates resistant to the antimicrobials varied considerably amongst the individual countries. The highest incidence of resistance to all six drugs was observed in strains collected in Spain, whereas resistance was rarely encountered among strains isolated in Austria and the FRG. Resistance to ampicillin (MIC greater than or equal to 4 mg/l) among strains that lacked beta-lactamase activity was uncommon (0.3%). Based on the NCCLS Haemophilus influenzae breakpoints, the rates of susceptibility and resistance to cefaclor, chloramphenicol, tetracycline, and cotrimoxazole were 96.4/1.5, 96.2/2.8, 92.4/4.7, and 87.9/7.3%, respectively. The rate of susceptibility and resistance to erythromycin was 2.3/19.9. Multiple resistance to ampicillin, chloramphenicol, tetracycline, and cotrimoxazole was observed in 15 isolates (0.6%), and resistance to three drugs simultaneously in 72 (1.5%). The incidence of beta-lactamase producing strains was similar to that seen in the first European study performed in 1986 (9.1% vs. 10.9%), and was half that observed in US isolates collected in 1986.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:The Second European Collaborative Study on the frequency of antimicrobial resistance in Haemophilus influenzae. 208 16

The antibacterial activity of cefapirin was tested against 210 strains isolated from the auricular exudate of childrens' acute otitis media. For 112 strains of Haemophilus studied (20% secreted a beta-lactamase), the MIC 50 and 90 of cefapirin were 2 and 4 mg/l respectively. Ten strains of Branhamella catarrhalis were tested (9 secreted a beta-lactamase) and the MIC ranged from 0.25 to 4 mg/l. Against Streptococcus pneumoniae, cefapirin has an extremely high activity with MIC 50 and 90 less than 0.06 mg/l. Of the strains of Staphylococcus aureus sensitive to meticillin, one had a MIC less than 0.06 mg/l, and 11 had a MIC = 0.25 mg/l. For 14 strains of Enterobacteriaceae studied, we obtained a MIC 50 of 8 mg/l and a MIC 90 of 32 mg/l. The results show that cefapirin is an antibiotic particularly suitable for the treatment of acute otitis media.
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PMID:[Activity of cefapirin against bacterial strains isolated from acute otitis media in children]. 211 4

Concentrations of amoxycillin/clavulanic acid achievable in the respiratory tract following oral dosage were assessed for in-vitro activity against beta-lactamase-producing strains of Branhamella catarrhalis and Haemophilus influenzae. In agar-dilution studies, 8 mg amoxycillin/l was required to inhibit 45 strains of beta-lactamase-producing B. catarrhalis, whereas all the strains were inhibited by 0.5 mg amoxycillin/l in the presence of 0.01 mg clavulanic acid/l. Similarly, 0.1 mg amoxycillin plus 0.05 mg clavulanic acid/l were bactericidal against beta-lactamase-producing strain of B. catarrhalis and prevented regrowth within 24 h. In tests against 43 beta-lactamase-producing strains of H. influenzae, concentrations of up to 128 mg amoxycillin/l were required for inhibition, whereas 32 strains (75%) were fully sensitive to amoxycillin (MIC 0.5 mg/l) in the presence of 0.12 mg clavulanic acid/l. These concentrations of amoxycillin/clavulanic acid were also bactericidal for a beta-lactamase-producing strain of H. influenzae. The study therefore showed that amoxycillin/clavulanic acid, at concentrations similar to those likely to be achieved in the respiratory tract following oral dosage, was bactericidal in vitro for beta-lactamase-producing isolates of B.catarrhalis and H. influenzae.
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PMID:Effect of low concentrations of clavulanic acid on the in-vitro activity of amoxycillin against beta-lactamase-producing Branhamella catarrhalis and Haemophilus influenzae. 212 99

The in vitro activity of faeriefungin, a new pentaene macrolide lactone antibiotic produced by Streptomyces griseus var. autotrophicus, against 263 clinical bacterial isolates was examined. In contrast to the related fungicidal antibiotics nystatin and amphotericin B, which show no activity against bacteria, faeriefungin showed bactericidal activity against all species of gram-positive bacteria examined. MICs for these species ranged from 8 to 64 micrograms/ml, and the MIC for 90% of the isolates tested was 32 micrograms/ml. Isolates of some fastidious gram-negative species, including Neisseria gonorrhoeae, N. meningitidis, and Haemophilus influenzae, were slightly susceptible to faeriefungin, with MICs ranging from 16 to 128 micrograms/ml, but all members of the families Enterobacteriaceae and Pseudomonadaceae, with the exception of Pseudomonas cepacia, were completely resistant to faeriefungin at the concentrations tested. Faeriefungin is also active against fungi, nematodes, and mosquito larvae. The mode of action of faeriefungin against both bacteria and fungi is under investigation.
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PMID:In vitro antibacterial activity of faeriefungin, a new broad-spectrum polyene macrolide antibiotic. 212 89


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