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 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 new carbapenem antibiotic that is stable to human renal dehydropeptidase-I (DHP-I) and exhibits potent bactericidal activity against almost all clinically significant aerobic and anaerobic bacteria. Activity is achieved through rapid entry into bacteria, resisting hydrolysis by all serine-based beta-lactamases, both of chromosomal or plasmid origin, and high affinity for vital penicillin binding proteins. The antibacterial spectrum of meropenem has been investigated extensively in a world-wide programme of studies. The results from all of these studies are consistent and identify in vitro differences between meropenem and imipenem. Both agents demonstrate high activity against Gram-positive aerobes with meropenem slightly less active than imipenem but significantly more potent than imipenem against Haemophilus influenza, all Enterobacteriaceae and 2-4 fold more active against Pseudomonas aeruginosa and most other pseudomonas. The spectrum of carbapenems is superior to that of all other beta-lactams. This is achieved, in part, by stability to the chromosomal beta-lactamases which hydrolyse ceftazidime, cefotaxime and ceftriaxone and against which newer agents like cefpirome and cefepime are not fully stable. Meropenem is also stable to the new plasmid-mediated enzymes which are responsible for significant elevation of MIC's of all cephalosporins and penicillins. When tested against P. Aeruginosa which have become resistant to imipenem therapy, these strains remained susceptible to meropenem. The activity of meropenem against anaerobes is at least as potent as metronidazole and clindamycin. These impressive in vitro data have been the basis for an extensive clinical evaluation programme in many indications including infections caused by single or multiple pathogens.
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PMID:[Preclinical evaluation of meropenem, a new parenteral carbapenem]. 857 29

Infection remains the major cause of morbidity and mortality for cancer patients who become granulocytopenic. Combinations of beta-lactams plus aminoglycosides have been the standard empiric therapy for febrile granulocytopenic patients, especially those with profound long-lasting granulocytopenia. The advent of new broad-spectrum cephalosporins and carbapenems has favoured the possibility of empiric monotherapy. Meropenem is a parenteral carbapenem antibiotic stable to renal dehydropeptidase-I which has excellent bactericidal activity against almost all clinically significant aerobic and anaerobic organisms. Meropenem hasta an antibacterial spectrum similar to that of imipenem but it is more active against Pseudomonas aeruginosa, all Enterobacteriaceae, Haemophilus influenzae, Proteus spp, Morganella spp and Providencia spp. Recently, the efficacy, safety, and tolerance of meropenem monotherapy for the empirical treatment of fever in granulocytopenic cancer patients have been compared in two large prospective randomized multicenter trials. The Meropenem Study Group compared monotherapy with meropenem versus ceftazidime and the EORTC conducted a comparative study of meropenem monotherapy versus the combination of ceftazidime plus amikacin. In both groups, success rates were similar by type of infection and infection-related mortality was low. Related adverse events were also similar in both groups. These studies confirm that monotherapy with meropenem is as effective as ceftazidime-containing regimens for the empiric treatment of fever in granulocytopenic patients.
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PMID:[Monotherapy with meropenem in febrile granulocytopenic patients]. 941 73

LJC 11,036 is the active metabolite of L-084, a novel oral carbapenem that exhibits potent broad-spectrum activity. Antibacterial activities of LJC 11,036 against clinical isolates from respiratory infections, such as Streptococcus pneumoniae (n = 52), Streptococcus pyogenes (n = 19), Haemophilus influenzae (n = 50), Klebsiella pneumoniae (n = 53), and Moraxella catarrhalis (n = 53), and from urinary-tract infections, such as Escherichia coli (n = 53) (MICs at which 90% of the isolates were inhibited [MIC(90)s], 0.1, </=0.006, 0.39, 0.05, 0.05, and 0.05 microg/ml, respectively), were 2- to 64-fold higher than those of imipenem, cefdinir, and faropenem. Moreover, against these bacterial species, except for H. influenzae, the MIC(90)s of LJC 11,036 were 4- to 512-fold lower than those of levofloxacin. LJC 11,036 showed bactericidal activity equal or superior to that of imipenem. Bactericidal activity against penicillin-resistant S. pneumoniae (PRSP) did not vary with the phase of growth. LJC 11,036 had potent activity against various beta-lactamase-producing strains, excluding carbapenemase producers. Against renal dehydropeptidase-I, LJC 11,036 was more stable than imipenem. Furthermore, LJC 11,036 produced in vitro postantibiotic sub-MIC effects against PRSP HSC-3 (6.0 h at one-fourth the MIC) and H. influenzae LJ5 (9.2 h at one-half the MIC). LJC 11,036 showed high binding affinities for PBP1A, -1B, -2A/2X, -2B, and -3 of PRSP and for PBP1B, -2, -3A, and -3B of H. influenzae.
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PMID:In vitro antibacterial activity of LJC 11,036, an active metabolite of L-084, a new oral carbapenem antibiotic with potent antipneumococcal activity. 1042 28