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Query: UMLS:C0519030 (Klebsiella)
 21,988 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Moxalactam exhibited excellent in vitro activity against all pathogens commonly associated with biliary tract infections. The drug retained bactericidal activity against all of these organisms, with the possible exception of Klebsiella pneumoniae, even in the presence of bile. Pharmacokinetic studies revealed high concentrations of moxalactam in the bile after intravenous administration. Twenty-seven of 28 patients with severe, complicated biliary tract infections responded favorably to the administration of moxalactam.
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PMID:Pharmacokinetics and clinical efficacy of moxalactam in biliary tract infections. 621 84

843 isolates from clinical specimens were tested against moxalactam by disc agar diffusion. The bacteria used in this study consisted of Escherichia coli, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Klebsiella pneumoniae, Proteus mirabilis, Providencia rettgeri, Pseudomonas aeruginosa, Serratia marcescens, Staphylococcus aureus, Staphylococcus epidermidis and group B and group D Streptococci. In vitro activity of moxalactam was compared with the following antibiotics: ampicillin, amikacin, carbenicillin, cefamandole, cefoxitin, cephalothin, chloramphenicol, clindamycin, colistin, erythromycin, gentamicin, oxacillin, penicillin, tetracycline, tobramycin, trimethoprim-sulfamethoxazole and vancomycin. Of the 471 strains of Enterobacteriaceae tested, 466 (98.9%) were susceptible to moxalactam. Except for penicillin G, the gram-positive cocci were generally more resistant to moxalactam than the other beta-lactam antibiotics. Moxalactam was comparable to gentamicin, as far as its activity against P. aeruginosa was concerned, but was less effective than amikacin, tobramycin, carbenicillin or colistin.
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PMID:In vitro activity of moxalactam against pathogenic bacteria and its comparison with other antibiotics. 621 65

Moxalactam disodium in combination with ticarcillin disodium or tobramycin sulfate was used to treat 445 episodes of suspected or confirmed infection in patients with cancer. The majority had leukemia and neutropenia. The rate of cures during the 231 confirmed infections was 65% for moxalactam and ticarcillin and 64% for moxalactam and tobramycin. Both regimens were comparable against aerobic gram-negative and polymicrobial infections. In gram-positive infections, the response rate for moxalactam and ticarcillin was 73% and for moxalactam and tobramycin, 53%. Only three of nine enterococcal infections responded to treatment. Thirteen percent of all organisms recovered were resistant to moxalactam. Side effects occurred infrequently; the most important was coagulopathy due to moxalactam. Nephrotoxic effects occurred in six patients receiving moxalactam and tobramycin and in none of those receiving moxalactam and ticarcillin. In 39 patients, a superinfection was confirmed. Fourteen were fungal, three were due to enterococcus, and one due to Klebsiella species. Eleven of the 14 fungal episodes occurred in the moxalactam-ticarcillin group. Moxalactam with ticarcillin and moxalactam with tobramycin are equally active for the initial treatment of presumed infection in patients with neutropenia.
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PMID:Moxalactam plus ticarcillin or tobramycin for treatment of febrile episodes in neutropenic cancer patients. 638 46

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

The antibacterial activity of moxalactam was studied in vitro against 229 clinical isolates of gram-positive and gram-negative aerobic microorganisms using the agar dilution technique. Mueller-Hinton agar was used as growth medium. The results were compared to those obtained with cefamandole. All isolates of Staphylococcus aureus and Streptococcus pneumoniae were inhibited by moxalactam at a concentration of 8 microgram/ml or less. The concentrations of cefamandole with which the same effect was obtained were 0.5 microgram/ml and 2 microgram/ml respectively. Moxalactam was highly inhibitory against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and Proteus morganii - 90% of the strains were inhibited by 0.125 microgram/ml. Moxalactam was highly superior against Proteus rettgeri and Pseudomonas aeruginosa, which are usually resistant to cefamandole: the MIC100 and MIC90 were 0.25 microgram/ml and 8 microgram/ml respectively. High sensitivity was found in strains of Salmonella species, nine of which were Salmonella typhi: the MIC90 was < 0.063 microgram/ml versus the eightfold higher concentration of cefamandole. The broad-spectrum activity and unusual MIC patterns of moxalactam - eight or manyfold higher concentrations of cefamandole were needed to inhibit 90% of most gram-negative strains studied - make moxalactam an unusual and promising antibiotic.
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PMID:In vitro antibacterial activity of moxalactam, a new broad-spectrum semisynthetic antibiotic. 644 72

Moxalactam (LY127935) is a 1-oxa-beta-lactam which was active in vitro against the majority of 128 strains of gram-negative enteric bacilli isolated from meningitis in neonates. Pharmacokinetics and bacteriological efficacy of LY127935 were studied in a lapin meningitis model. The average penetration of this investigational oxa-cephalosporin into cerebrospinal fluid of infected rabbits was 23% compared with 25% for netilmicin and 11% for ampicillin. The cerebrospinal fluid concentrations of LY127935 produced median bactericidal titers of 1:64 to 1:128 against five coliform organisms (two Escherichia coli K1 strains, Klebsiella pneumoniae, Salmonella saint-paul, and Citrobacter diversus) used in these experiments compared with median titers of 1:2 to 1:8 for netilmicin and 1:2 to 1:4 for ampicillin. LY127935 was statistically significantly more effective than netilmicin or ampicillin in reducing cerebrospinal fluid bacterial colony counts and in sterilizing cerebrospinal fluid of experimentally infected rabbits. These results suggest that LY127935 has theoretical advantages over netilmicin and ampicillin for therapy of gram-negative bacillary meningitis.
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PMID:Pharmacokinetics and bacteriological efficacy of moxalactam (LY127935), netilmicin, and ampicillin in experimental gram-negative enteric bacillary meningitis. 644 76

Comparison of the activity of cefoperazone, cefamandole, cefotaxime, cephalothin and moxalactam against Enterobacteriaceae showed cefoperazone to be twofold (Escherichia coli, Klebsiella) to eigthfold (Enterobacter) more active than cefamandole. The lowes MIC values were found for cefotaxime (0.03 - 0.25 microgram/ml) followed by moxalactam (0.06 - 0.25 microgram/ml). Cefoperazone stood out in activity against Pseudomonas aeruginosa (MIC50 4 microgram/ml). Cephalothin resistance affected the MIC values of cefoperazone and moxalactam only to a small degree. From beta-lactamase susceptibility studies it was concluded that cefoperazone may be hydrolyzed by TEM type beta-lactamases, but that the cephalosporinases (class I) and the chromosomal broad-spectrum beta-lactamases (class IV) only have little effect on this antibiotic. Moxalactam was not degraded by any of the beta-lactamase preparations tested.
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PMID:Activity and specific beta-lactamase susceptibility of cefoperazone and moxalactam. Comparison with other cephalosporins. 645 58

Meningitis caused by enteric gram-negative bacilli is relatively uncommon but is very difficult to treat despite susceptibility in vitro to many antimicrobics. A major problem appears to be poor entry of many drugs into the central nervous system. Moxalactam is an investigational cephalosporin that attains concentrations in the cerebrospinal fluid that are 15% to 30% of contemporaneous serum concentrations; moreover, it is quite active against many of the enteric gram-negative bacilli. We used moxalactam to treat meningitis caused by Enterobacter cloacae, Klebsiella pneumoniae, and Escherichia coli in four adults and one child, giving up to 100 mg/kg body weight per day by intravenous injection. The concentrations of moxalactam in serum, lumbar, and ventricular cerebrospinal fluid exceeded the minimal lethal concentrations of all causative bacteria. The patients were cured. In this small series, moxalactam, when administered intravenously as the sole agent of therapy, was effective in the treatment of meningitis caused by susceptible gram-negative bacilli.
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PMID:Successful treatment of gram-negative bacillary meningitis with moxalactam. 645 50

Moxalactam, a novel beta-lactam antimicrobial agent in which oxygen has replaced sulfur in the six-membered ring of the conventional cephem nucleus, has in vitro activity against almost all commonly isolated bacterial pathogens including Staphylococcus aureus, the Enterobacteriaceae, Pseudomonas aeruginosa, Bacteroides fragilis, and Haemophilus influenzae. The clinical efficacy an toxicity of moxalactam alone was evaluated in the treatment of 100 infections, including 22 septicemias. Thirty-two infections involved P aeruginosa, while organisms resistant to one or more of the currently available cephalosporins or cefoxitin were isolated from cultures in 63 of the cases. The overall clinical response was favorable (infection cured or improved) in 86% of the infections. A child with Klebsiella pneumoniae ventriculitis and meningitis was cured with intravenous moxalactam alone. Six of 14 treatment failures involved P. aeruginosa, and P aeruginosa isolates resistant to moxalactam emerged during therapy of 12 infections. Side effects, usually mild diarrhea, occurred in only 8.8% of the patients. Except for some severe P aeruginosa infections outside the urinary tract, moxalactam is effective and safe single-agent therapy for infections caused by susceptible organisms and represents a major advancement in beta-lactam antimicrobial therapy.
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PMID:Moxalactam therapy for bacterial infections. 645 53

The agar dilution in-vitro susceptibility of 370 isolates of aerobic Gram-negative bacteria isolated at Ben Taub General Hospital in Houston, Texas were determined for five new and five currently available agents. Ceftazidime, moxalactam, cefotaxime, ceftizoxime and cefoperazone, all of which are new beta-lactam compounds, were compared with two penicillins, piperacillin, ticarcillin, and three aminoglycosides, gentamicin, tobramycin and amikacin. Ceftazidime inhibited 100% of pseudomonas strains at a concentration of 12.5 mg/l, whereas the aminoglycosides inhibited 88-93% and ticarcillin and piperacillin inhibited 47 and 85% of these strains at this concentration. Ceftazidime at a level of 125 mg/l was the most effective agent against all strains of indole positive Proteus spp., Serratia spp., Klebsiella spp., Citrobacter spp., and Echerichia coli. Moxalactam was the most effective agent against Enterobacter spp., and ceftazidime was the next most effective agent. Ceftazidime is a potent new beta-lactam which should be useful against hospital strains of Gram-negative bacteria.
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PMID:In-vitro comparison of ceftazidime and nine other antimicrobial agents against hospital strains of Gram-negative bacteria. 1980 69


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