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)

Meropenem (MEPM), a novel parenteral carbapenem antibiotic, was examined in a cooperative study involving 12 pediatric and 1 neonatologic facilities. The results are summarized as follows. 1. Antibacterial activity Antibacterial activity of MEPM against stock organisms including 31 strains of Streptococcus agalactiae, 14 of Listeria monocytogenes, 4 of Bordetella pertussis and 3 of Neisseria meningitidis ranged from 0.025 to 0.10 micrograms/ml in MIC90's, which were equal or lower than those of control drugs such as imipenem cefazolin, cefotiam, cefotaxime, ceftazidime and latamoxef. MICs against clinical isolates were as follows: In Gram-positive bacteria, MICs were 0.20 micrograms/ml to 6.25 micrograms/ml against 3 strains of Staphylococcus aureus, and 0.025 micrograms/ml or less against 4 of Streptococcus pneumoniae. In Gram-negative bacilli, MICs were 0.10 micrograms/ml to 0.20 micrograms/ml against 3 strains of Haemophilus influenzae and 0.78, 0.10 and 0.78 micrograms/ml, respectively, against one strain each of Enterobacter cloacae, Morganella morganii and Pseudomonas aeruginosa. MIC against 1 strain of Peptococcus saccharolyticus was < or = 0.025 micrograms/ml. 2. Pharmacokinetics Maximum plasma concentrations after intravenous infusion of MEPM over 30 minutes at doses of 10, 20 and 40 mg/kg, respectively, to 3 different groups of 3 children (total 9 cases) were observed at the completion of the treatment. Mean maximum concentrations in the 3 groups were 36.3, 69.5 and 129.8 micrograms/ml, respectively, exhibiting clear dose response. Mean plasma half lives in beta phase were 0.94, 0.86 and 0.94 hours, respectively, exhibiting no difference by doses, and this trend was observed also by HPLC. Urinary excretion rates in the first 6 hours after dose in the 10, 20 and 40 mg/kg groups were 67.3, 65.6 and 68.4%, respectively. Concentrations of MEPM in cerebrospinal fluid were determined in 2 cases of pyogenic meningitis. In 1 case, 500 mg (5.9 mg/kg) of MEPM was infused intravenously over 30 minutes and concentrations on Days 6, 8 and 15 observed at 190, 60 and 100 minutes after respective doses were 0.13, 0.10 micrograms/ml and less than the detection limit. Cerebrospinal fluid-plasma concentration ratio was determinable only on Day 8 and was 2.8%. In another case to which 250 mg (38.5 mg/kg) of MEPM was infused intravenously over 30 minutes, the concentration at Days 6, 7 and 10, 1 hour after the dose were less than the detection limit on day 6, and 2.04 and 2.62 micrograms/ml, respectively on days 7 and 10. 3. Clinical efficacy Clinical efficacies were evaluated in 49 cases and the efficacy rate was 93.9%.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Basic and clinical study of meropenem in pediatric field]. 147 87

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

A multicentre in-vitro study was undertaken to evaluate the susceptibility of bacterial pathogens isolated in different Italian hospitals to meropenem. A total of 1399 aerobic and 452 anaerobic strains was analysed. Comparative agents were imipenem, cefotaxime, ceftazidime, ceftriaxone, piperacillin, ciprofloxacin, gentamicin, amikacin, plus vancomycin when appropriate. The MIC ranges (mg/l) of meropenem were: 0.015-2 for Klebsiella spp., Proteus spp., Morganella morganii and Providencia spp.; less than 0.008-1 for Escherichia coli; 0.016-32 for Serratia spp.; 0.03-2 for Enterobacter spp. and Citrobacter spp.; 0.03- greater than 128 for Acinetobacter anitratus; 0.03-32 for Pseudomonas spp.; less than 0.008-0.5 for Haemophilus spp. and Neisseria spp.; 0.015-64 for Staphylococcus spp.; 0.06- greater than 128 for Enterococcus spp.; less than 0.008-0.25 for Streptococcus spp.; 0.016-8 for Fusobacterium spp.; 0.03-8 for Bacteroides spp.; less than 0.06-0.5 for anaerobic Gram-positive cocci; 0.08-2 for Clostridium spp. Meropenem exhibited superior antibacterial activity against the aerobic and anaerobic strains tested when compared to the other beta-lactam drugs. The new carbapenem was as active as ciprofloxacin and more active than imipenem and the aminoglycosides against Enterobacteriaceae and Ps. aeruginosa. It was also more active than ciprofloxacin against most strains of Gram-positive cocci. Meropenem was slightly less potent than imipenem against staphylococci and enterococci, with the exception of oxacillin-susceptible Staph. aureus against which meropenem and imipenem exhibited similar antibacterial activity.
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PMID:In-vitro activity of meropenem against clinical isolates in a multicentre study in Italy. 268 Nov 28

The in vitro antimicrobial activity of the new carbapenem meropenem (SM-7338) was determined by an agar dilution method in comparison with imipenem, ticarcillin/calvulanic acid, ceftazidime and the fourth-generation cephalosporin cefepime (BMY 28142). Meropenem showed superior activity against Enterobacteriaceae (MIC90 less than or equal to 0.06 mg/l) and against non-fermentative gram-negative rods, with the exception of Xanthomonas maltophilia. Meropenem had excellent activity against beta-lactamase-producing Haemophilus influenzae and Neisseria gonorrhoeae, and against the Bacteroides fragilis group. Imipenem was slightly more active then meropenem against gram-positive cocci especially Enterococcus faecalis.
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PMID:Comparative in vitro antibacterial activity of the new carbapenem meropenem (SM-7338). 269 28

MICs of meropenem were determined for a wide range of common bacteria of clinical importance. For Enterobacteriaceae, Aeromonas spp., Haemophilus influenzae, Branhamella catarrhalis, Neisseria gonorrhoeae, Gardnerella vaginalis, Campylobacter coli/jejuni, beta-haemolytic streptococci and anaerobes other than Clostridium difficile, MICs were almost always within the range 0.002-0.5 mg/l. The activity of meropenem for these organisms was always greater than that of imipenem and piperacillin, and was similar to that of ceftazidime and cefotaxime except that strains resistant to these latter, and to piperacillin, were usually sensitive to imipenem and meropenem. Meropenem was also active against most non-fermentative Gram-negative bacilli, with MICs in the range 0.12-4 mg/l but Pseudomonas (Xanthomonas) maltophilia was often resistant, as it was to all the other drugs tested. Staphylococci, Strreptococcus pneumoniae and other alpha-haemolytic streptococci were usually more sensitive to imipenem than to meropenem, but even methicillin-resistant staphylococci were sensitive to both drugs (MICs less than 4 mg/l). Enterococci were also less sensitive to meropenem than to imipenem, and Enterococcus faecium was invariably highly resistant to all the drugs tested except ciprofloxacin, which had marginal activity. Results for Ps. maltophilia and Haem. influenzae were affected by media used for sensitivity testing.
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PMID:Comparative in-vitro activity of meropenem on clinical isolates from the United Kingdom. 280 14

The in-vitro activity of meropenem, a new parenteral carbapenem, was compared with that of imipenem, ceftazidime, cefotaxime, piperacillin, gentamicin and, where appropriate, other antibiotics against recent clinical isolates and characterized beta-lactamase producers. MICs were determined by a standard agar dilution procedure and two inocula (10(4) and 10(6) cfu) were used throughout. Meropenem inhibited 90% of isolates of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, indole-positive Proteus spp., Enterobacter spp., Serratia marcescens and Providencia stuartii at less than or equal to 0.25 mg/l and was four- to 16-fold more active than imipenem against these species. Against the enteric pathogens Salmonella typhi, Shigella sonnei, Yersinia enterocolitica and Campylobacter jejuni, meropenem was four- to eight-fold more active than imipenem, inhibiting all isolates at less than or equal to 0.03 mg/l. Meropenem was also more active than imipenem against Haemophilus influenzae (MIC90 0.06 mg/l) but had similar activity against the Bacteroides fragilis group (MIC90 0.25 mg/l), against Pseudomonas aeruginosa (MIC90 2 mg/l) and against streptococci. Imipenem was four-fold more active than meropenem against Acinetobacter spp. and two- to eight-fold more active against all species of staphylococci tested. Both meropenem and imipenem were inactive against Ps. (Xanthomonas) maltophilia.
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PMID:In-vitro activity of meropenem against clinical isolates obtained in Canada. 280 16

Meropenem and imipenem are carbapenems which are distinguishable from all other currently available beta-lactam antibiotics by breadth of antibacterial spectrum and stability to beta-lactamases, but can be differentiated one from another. Meropenem is relatively stable to human renal dehydropeptidase-I (DHP-I); it does not require to be co-administered with cilastatin and consequently, unlike imipenem, will be administered as a single agent. In vitro both meropenem and imipenem are active against almost all clinically important aerobic and anaerobic bacteria. Differences in potency are seen but few may be of clinical significance: imipenem is more active against enterococci and meropenem is more active against Pseudomonas aeruginosa, Pseudomonas cepacia, Haemophilus influenzae and Proteus, Morganella and Providencia species. The primary target of imipenem is PBP2 in P. aeruginosa whilst meropenem has high affinity for both PBP2 and 3; this may contribute to greater potency against this organism. Laboratory evaluations predict that meropenem will not be seizurogenic, which combined with activity against likely pathogens, identified its potential for the treatment of bacterial meningitis. This has been investigated in a guinea-pig model in which meropenem exhibited potent activity against the common meningeal pathogens and also infections caused by penicillin-resistant Streptococcus pneumoniae or Listeria monocytogenes. Clinical experience will determine the significance of these differences.
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PMID:Laboratory data which differentiate meropenem and imipenem. 765 4

Meropenem is a parenteral carbapenem antibiotic which has excellent bactericidal activity in vitro against almost all clinically significant aerobes and anaerobes. Its high activity is explained by ease of entry into bacteria combined with good affinity for essential penicillin binding proteins, including those associated with cell lysis. Breadth of spectrum is due, in part, to stability to all serine-based beta-lactamases, including those which hydrolyse third-generation cephalosporins. Meropenem has an antibacterial spectrum which is broadly similar to that of imipenem but, whilst slightly less active against staphylococci and enterococci, it is more active against Pseudomonas aeruginosa, all Enterobacteriaceae and Haemophilus influenzae. Amongst common human pathogens, only methicillin-resistant staphylococci and Enterococcus faecium are uniformly resistant to meropenem. The meropenem MICs for penicillin-resistant Streptococcus pneumoniae are higher than for penicillin-susceptible strains but the organisms remain susceptible. Clinical susceptibility in vitro to meropenem is defined by MICs of < or = 4 mg/L, intermediate susceptibility by MICs of 8 mg/L and MICs of > or = 16 mg/L define resistance; equivalent figures for zones of growth inhibition are > or = 14 (susceptible), 12-13 (intermediate) and < or = 11 (resistant) mm. Studies in guinea pig models of systemic infection and infections localised to the lungs, urinary tract and the central nervous system, some of which used immunocompromised animals, confirm the potential of meropenem demonstrated in vitro. These factors, combined with the human plasma, tissue or urinary concentrations of meropenem which exceed modal MICs for the pathogens isolated in clinical trials for most or all of the recommended 8 h dosing interval, predict that meropenem should be efficacious in the treatment of infections at many body sites.
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PMID:Meropenem: a microbiological overview. 854 86

Meropenem and imipenem/cilastatin were compared in an open, randomised prospective multicentre study in the treatment of acute exacerbations of severe chronic obstructive pulmonary disease in hospitalised patients. One-hundred-and-seventy-three patients were enrolled; 164 were evaluable for clinical efficacy and 98 for bacteriological efficacy, with 144 pathogens isolated. The predominant pathogens were Haemophilus influenzae (n = 30), Streptococcus pneumoniae (18), Staphylococcus aureus (12), Pseudomonas aeruginosa (11), Moraxella catarrhalis (8), other Gram-negative bacteria (Neisseria, Klebsiella, Proteus, and Enterobacter spp.) (53) and other Gram-positive bacteria (12). A single bacterial pathogen was identified in 61 patients, whereas two bacterial pathogens were isolated in 31 patients and three in six patients. The clinical response at the end of treatment was very high in both groups with a satisfactory outcome (cured or improved) in 97.6% of the meropenem patients and in 96.3% of the imipenem/cilastatin patients; at follow-up the rates were 89.1% and 89.8%, respectively. The bacterial success (eradication or presumed eradication) was 88.2% in the meropenem group and 89.4% in the comparator group. Nausea or vomiting were reported more frequently in patients treated with imipenem/cilastatin, whereas in the meropenem group an increase in aminotransferases was reported. One patient treated with imipenem/cilastatin was withdrawn from the study due to seizures. Meropenem and imipenem/cilastatin were highly effective for the treatment of severe bacterial exacerbations of chronic bronchitis but meropenem was better tolerated.
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PMID:Treatment of acute bacterial exacerbations of chronic obstructive pulmonary disease in hospitalised patients--a comparison of meropenem and imipenem/cilastatin. COPD Study Group. 854 88


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