Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: 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)

In the present study, five non-beta-lactamase- and five beta-lactamase-producing strains of Haemophilus influenzae were used to determine whether three different growth media, Mueller-Hinton broth and agar, brain heart infusion broth and agar, and tryptic soy broth and agar, and their added supplements (0.2% hemin-0.1% IsoVitaleX, 1% hemin-1% IsoVitaleX, 2% sheep blood, 10% Fildes enrichment, 5% Fildes enrichment, 1% supplement B, 5% horse erythrocytes, and 2% hemoglobin-1% IsoVitaleX) would influence the growth rate of this microorganism and the antibacterial activity of eight antibiotics, including ampicillin, tetracycline, chloramphenicol, gentamicin, cefamandole, erythromycin, trimethoprim-sulfamethoxazole (TMP-SMX), and cefoperazone. The growth curve studies were carried out with an initial inoculum of 10(4) bacteria per ml, and MICs were determined with an inoculum of 5 X 10(5) microorganisms. Mueller-Hinton broth, brain heart infusion broth, and tryptic soy broth enriched with 5% Fildes resulted in a maximal growth of more than 10(8) CFU/ml at 24 h. When 10% Fildes or 2% sheep blood was added as enrichment to Mueller-Hinton broth, a considerable reduction in the growth rate of H. influenzae strains resulted (P less than 0.01). Significant variations in MICs (P less than 0.01) were observed with chloramphenicol, TMP-SMX, erythromycin, and cefoperazone when brain heart infusion agar, Mueller-Hinton agar, or tryptic soy agar was used. Chloramphenicol, gentamicin, erythromycin, and TMP-SMX were all affected by the different enrichments added to Mueller-Hinton agar. MICs were in general higher with 5% Fildes enrichment and lower with 1% supplement B. Cefoperazone was the only drug which exhibited a lower MIC in 5% Fildes enrichment for ampicillin-resistant H. influenzae strains.
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PMID:Influence of growth medium and supplement on growth of Haemophilus influenzae and on antibacterial activity of several antibiotics. 349 45

Cefoperazone was compared with penicillin against Streptococcus pneumoniae, gentamicin against Escherichia coli, and ampicillin and chloramphenicol against Haemophilus influenzae in the therapy of experimental meningitis in rabbits. Meningitis was produced by intracisternal inoculation into cerebrospinal fluid, and all antibiotics were administered intravenously over 8 h in dosages that would achieve serum levels comparable to those found in humans. The mean percent penetration into purulent cerebrospinal fluid, expressed as (cerebrospinal fluid concentration/serum concentration) x 100%, was 2.6% for penicillin, 22.0% for gentamicin, 12.1% for ampicillin, 23.8% for chloramphenicol, and 6.4% for cefoperazone. The mean cerebrospinal fluid antibiotic concentrations exceeded the minimum bactericidal concentration for the test strain in each experimental model, except for ampicillin in experimental meningitis due to the beta-lactamase-producing H. influenzae. Cefoperazone produced a significantly faster bactericidal effect after 4 h of treatment when compared with penicillin (P = 0.037) and ampicillin (P = 0.01) in meningitis caused by S. pneumoniae and H. influenzae (ampicillin susceptible), respectively. In meningitis caused by E. coli, cefoperazone was significantly (P = 0.006) more rapidly bactericidal after 8 h of treatment when compared to gentamicin. In addition, cefoperazone was significantly more rapidly bactericidal than either ampicillin or chloramphenicol in experimental meningitis due to beta-lactamase-producing H. influenzae. Cefoperazone deserves further evaluation in the therapy of bacterial meningitis in humans.
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PMID:Comparison of cefoperazone with penicillin, ampicillin, gentamicin, and chloramphenicol in the therapy of experimental meningitis. 621 85

The in vitro qualities of cefoperazone were reviewed on the basis of international medical literature and some new observations. Cefoperazone is highly active against the Enterobacteriaceae. Its activity against Staphylococcus aureus is comparable to that of the other newer cephem antibiotics. Cefoperazone is also active against all beta-hemolytic streptococci and Streptococcus pneumoniae and is relatively inactive against methicillin-resistant S. aureus and enterococci. Against Pseudomonas aeruginosa cefoperazone is at least fourfold more active than cefotaxime or moxalactam and is approximately as active as azlocillin or piperacillin. Haemophilus and Neisseria species, regardless of beta-lactamase production, are highly susceptible to cefoperazone. Against the Bacteroides fragilis group, cefoperazone is either very active or quite inactive because of endemic variations. The drug is slightly less stable to some beta-lactamases than are cefotaxime-like or 7-methoxy cephem drugs. Cefoperazone is a bactericidal beta-lactam, and its minimal inhibitory concentrations are influenced only by high inoculum concentrations of beta-lactamase-producing strains. Its ability to permeate bacterial cell membranes appears similar to that of cefotaxime. Synergy studies with cefoperazone plus beta-lactamase inhibitors or aminoglycosides against Enterobacteriaceae and P. aeruginosa show enhanced killing. Cefoperazone is 70%-94% protein bound and has high affinities for bacterial penicillin-binding proteins 3, 1a, 2, and 1 bs.
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PMID:Cefoperazone: a review of its antimicrobial spectrum, beta-lactamase stability, enzyme inhibition, and other in vitro characteristics. 622 81

The antimicrobial activity of three 7-alpha-methoxy beta-lactams were compared to cefoperazone and ceftriaxone. All had a similar spectrum of activity against the Enterobacteriaceae, except cefoxitin. Cefotetan was only slightly less active than moxalactam against the Enterobacter spp. Ceftriaxone was most effective on Neisserias, Haemophilus spp, nonenterococcal Streptococcus spp, and Acinetobacter spp. Cefoperazone generally inhibited more pseudomonads while all of the "cephamycins" showed activity against Bacteroides fragilis and B. thetaiotaomicron. Beta-lactamase hydrolysis studies of six substrates having pharmacologic serum half lives of greater than or equal to 2 hrs were performed by bioassay and automated procedures. Excellent correlations were found between methods up to 24 hrs. A "lag-phase" was observed for several drug/enzyme combinations before initiation of significant substrate hydrolysis. The 7-alpha-methoxy beta-lactams were routinely more stable to the six representative enzymes (Richmond-Sykes types I-V) than other "stable" cephalosporins. Substrate hydrolysis rates resulting in greater than 50% drug loss in less than or equal to 1 hr generally produced resistant in vitro test results. Cefotetan, cefoxitin, moxalactam, ceftriaxone, and dicloxacillin were potent inhibitors of Type I (P99) beta-lactamases. Moxalactam demonstrated significant inhibition and affinity for the Type V enzyme while cefoperazone uniquely possesses affinity (so-called inhibition) for all tested beta-lactamases. Cefotetan appears to be a promising, beta-lactam compound with some in vitro characteristics comparable to the 1-oxa-beta-lactams and alpha-methoxyimino cephalosporins.
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PMID:Antimicrobial activity, beta-lactamase stability and beta-lactamase inhibition of cefotetan and other 7-alpha-methoxy beta-lactam antimicrobials. 632 95

The safety and clinical efficacy of cefoperazone were evaluated in a multicenter trial conducted at institutions in Japan, Korea, and Taiwan. Cefoperazone was given as the sole antibiotic for 481 respiratory tract infections in 476 patients. An overall satisfactory clinical response was achieved in 73.7% of patients. Cefoperazone was effective in 78.9% of cases of pneumonia, 81.1% of acute exacerbations of chronic bronchitis, and 69.4% of bronchiectasis with infection. A satisfactory bacteriological effect was obtained in 93.2% of cases in which Haemophilus influenzae was isolated, 70.2% of Klebsiella infections, and 84.6% of infections with Streptococcus pneumoniae. Although the eradication rate was only 38.6% in patients with Pseudomonas aeruginosa, the success rate increases to 59.1% if patients showing a decrease in the number of organisms are included. Cefoperazone was effective in 63.5% of the 148 cases that had failed to respond to treatment with other antibiotics. Adverse reactions occurred in 8.0% of patients and consisted primarily of rash, diarrhea, and fever. Cefoperazone appears to be an extremely useful injectable antibiotic for the treatment of respiratory tract infections in hospitalized patients.
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PMID:Asian multicenter trial of cefoperazone in respiratory tract infection. 639 68

The safety and clinical efficacy of cefoperazone were evaluated at 149 institutions in Japan. A total of 979 hospitalized patients were treated with cefoperazone alone for 1,059 infections. In the 984 infections evaluated, there was an overall satisfactory clinical response in 824 (83.7%). Cefoperazone was effective in 83.0% of the respiratory tract infections, 84.9% of urinary tract infections, and 89.6% of hepatobiliary tract infections. Clinical response was satisfactory in 90% or more of the cases in which Escherichia coli, Serratia sp, Haemophilus influenzae or Staphylococcus sp were isolated. Sixty percent to 90% of the infections with Klebsiella sp, Enterobacter sp, Proteus sp, and Pseudomonas aeruginosa responded satisfactorily to cefoperazone. Cefoperazone was effective in 76.2% of 260 evaluated cases that had failed to respond to prior treatment with other cephalosporins. The adverse reactions that occurred in 19 (1.9%) of the 979 patients included rash (1%), diarrhea (0.6%), and fever (0.4%). Cefoperazone appears to be extremely useful in the treatment of various infections in hospitalized patients.
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PMID:Multicenter clinical trials of cefoperazone in Japan. 639 29

Six third-generation cephalosporins--cefotaxime, moxalactam, cefoperazone, ceftizoxime, ceftriaxone, and cefmenoxime--are reviewed; covered are chemistry and structure-activity relationships, mechanism of action, spectra of activity, pharmacokinetics, clinical utility, adverse effects, and cost effectiveness. The third-generation cephalosporins have a similar mechanism of action to that of other beta-lactam antibiotics. None of the agents is particularly active against certain gram-positive bacteria, including methicillin-resistant Staphylococcus aureus; the drugs are effective against gonococci, Haemophilus influenzae, and Neisseria meningitidis. Several common gram-negative pathogens are susceptible to the third-generation cephalosporins, including Escherichia coli, Klebsiella, Citrobacter diversus, Proteus, and Morganella. About 50% of Pseudomonas aeruginosa isolates are susceptible. Only moxalactam has good activity against Bacteriodes fragilis. The pharmacokinetic profiles of the six agents reveal some important differences. The half-life of ceftriaxone allows once-daily dosing in many patients; the half-lives of ceftizoxime and cefoperazone permit dosing every 8-12 hours. Cefoperazone and ceftriaxone are highly protein bound, but the clinical relevance of this is unknown. Generally, the agents penetrate most body tissues and fluids well. Moxalactam and cefotaxime and possibly ceftriaxone effectively penetrate into the cerebrospinal fluid well. The third-generation cephalosporins have become the accepted drugs of choice for the treatment of adult gram-negative bacillary meningitis; as more experience is gained, they are likely to become the drugs of first choice for neonatal (with ampicillin) and childhood (except for moxalactam) meningitis. Serious infections of Enterobacteriaceae can be treated with these agents, thereby avoiding use of the aminoglycosides. Moxalactam is comparable with combination therapy in treating intra-abdominal infections. Adverse effects associated with use of the third-generation cephalosporins are generally similar to those that occur with other beta-lactam antibiotics with the exception of coagulopathies and the disulfiram reaction seen with moxalactam and cefoperazone. Despite the relatively high cost of the third-generation cephalosporins, they are often cost effective because of their reduced dosing frequencies, broad spectra of activity, and effectiveness in serious infections for which more toxic antibiotics have been required in the past.
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PMID:Third-generation cephalosporins: a critical evaluation. 643 20

Cefoperazone is a new semisynthetic cephalosporin with excellent antibacterial activity. This study included more than 1,500 clinical isolates whose susceptibility to cefoperazone was determined by minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). Cefoperazone was highly active against Enterobacteriaceae including indolepositive Proteus, Serratia and Enterobacter sp. Particularly noteworthy was the high activity of cefoperazone against Pseudomonas and Acinetobacter strains, which are usually resistant to first- and second-generation cephalosporins. The activity of cefoperazone against Staphylococcus aureus, Staphylococcus epidermidis, group D streptococci and Haemophilus was also determined. In general, the differences between MIC and MBC were minimal. Additional studies were carried out to determine the effect of inoculum size on cefoperazone activity.
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PMID:In vitro activity of a new semisynthetic cephalosporin: cefoperazone. 644 1

Cefoperazone is a new cephalosporin with a very wide spectrum of antibacterial activity, including Enterobacteriaceae, Pseudomonas aeruginosa, staphylococci, streptococci (other than serological group D strains), Neisseria and Haemophilus species (including beta-lactamase positive strains) and some anaerobes. On testing more than 8700 clinical isolates, approximately 93% were inhibited by 16 micrograms/ml of cefoperazone, 95% by 32 micrograms/ml and 98% by 64 micrograms/ml. The drug is less active on Acinetobacter and group D streptococci. We recommend that a disc containing 75 micrograms of cefoperazone be used in the diffusion test with 'breakpoints' of less than or equal to 14 mm for resistant, 15-17 mm for intermediate, and greater than or equal to 18 mm for susceptible bacteria.
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PMID:Cefoperazone: spectrum of antibacterial activity and disc diffusion testing. 645 89

The sensitivity of a number of beta-lactamase producing strains of Enterobacter aerogenes, Enterobacter cloacae, Enterobacter species, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa and Serratia marcescens to cefamandole, cefoxitin, cefuroxime, cefotaxime and cefoperazone was determined in vitro. All bacterial cultures were examined for beta-lactamase production using the chromogenic cephalosporin compound 87/312. All strains were typed by means of antibiotic and chemotherapeutic sensitivities. Only non-identical strains were used. A tray method was used to determine the quantity of antimicrobial product necessary for a complete growth inhibition at various culture dilutions. The results showed that all strains of H. influenzae, especially in the dilution 2.10(6), were sensitive to the five cephalosporins. The other species and genus of bacteria had a varying sensitivity to the five cephalosporins. Cefoperazone had potent activity against Ps. aeruginosa. Differences between the five cephalosporins with regard to the effect of culture dilution were only small.
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PMID:A comparison of cefamandole, cefoxitin, cefuroxime, cefotaxime and cefoperazone: an in vitro test on a number of beta-lactamase producing strains of 9 species and 1 genus of bacteria. 697 Dec 10


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