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)

The in vitro activity of LJC 10,627, a new carbapenem, was compared with those of imipenem, cefotaxime, ceftazidime, and gentamicin. LJC 10,627 inhibited 90% of Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Hafnia alvei, Citrobacter freundii, Citrobacter diversus, Proteus mirabilis, Morganella morganii, Proteus rettgeri, Serratia marcescens, Pseudomonas cepacia, salmonellae, shigellae, aeromonas, and yersiniae at less than or equal to 2 micrograms/ml. Haemophilus influenzae was inhibited by 0.5 microgram/ml, and moraxellae were inhibited by 0.12 microgram/ml. LJC 10,627 was twofold more active than imipenem against aerobic gram-negative organisms and inhibited ceftazidime-, cefotaxime-, and gentamicin-resistant members of the genera Klebsiella, Enterobacter, Citrobacter, and Serratia at less than or equal to 2 micrograms/ml. Xanthomonas maltophilia strains were resistant to the drug. Imipenem was two- to fourfold more active than LJC 10,627 against Staphylococcus aureus and Staphylococcus epidermidis. LJC 10,627 did not inhibit most methicillin-resistant Staphylococcus aureus or methicillin-resistant Staphylococcus epidermidis strains. LJC 10,627 inhibited Streptococcus pyogenes and Streptococcus pneumoniae at 0.06 and 0.12 microgram/ml, respectively. Bacteroides fragilis and other Bacteroides spp. were inhibited by 0.5 microgram of LJC 10,627 per ml. Serum (50%) did not affect the MICs. LJC 10,627 was not hydrolyzed by plasmid-mediated beta-lactamases of Bush types 2b, 2b', TEM-1, TEM-2, TEM-3, TEM-5, TEM-7, TEM-9, and SHV-1; the chromosomal beta-lactamases of Bush type 1; P-99; a Morganella enzyme; or a Citrobacter freundii enzyme. The Bush type 2c and 2d enzymes OXA-1, OXA-2, PSE-1, PSE-2, and PSE-4 did not hydrolyze LJC 10,627, nor did the beta-lactamases of Staphylococcus aureus, Moraxella spp., Bacteroides fragilis, and Proteus vulgaris. The beta-lactamase of Xanthomonas hydrolyzed LJC 10,627, albeit at approximately one-third the rate that imipenem was hydrolyzed.
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PMID:In vitro activity and beta-lactamase stability of LJC 10,627. 151 Apr 36

Fifty-two patients with moderate or severe infections associated with internal medicine were treated with imipenem/cilastatin sodium (IPM/CS) and the efficacy and the safety of this drug were evaluated. There were 20 patients with pneumonia, 10 with acute exacerbation of chronic respiratory tract infections, 9 with sepsis, 2 with pyothorax, 3 with intraabdominal infection, 2 with urinary tract infection, 1 with pulmonary abscess, 1 with infective endocarditis, 4 with fever of unknown origin. Forty-four patients were evaluable for the efficacy. Clinical efficacies were excellent in 12 patients, good in 26, fair in 3 and poor in 3. The overall clinical efficacy was 86.4%. The efficacy rate was 63.6% in patients previously treated and 93.9% in patients previously untreated with other antibiotics. Bacteriologically, Staphylococcus aureus (8 strains), Streptococcus pneumoniae (5), Streptococcus pyogenes (1), other Gram-positive coccus (1), Klebsiella pneumoniae (8), Haemophilus influenzae (4), Pseudomonas aeruginosa (3), Serratia marcescens (3), Escherichia coli (3), Branhamella catarrhalis (1), Citrobacter freundii (1), Klebsiella oxytoca (1), Enterobacter sp. (1), and Peptostreptococcus sp. (1) were eradicated. P. aeruginosa (3) and Acinetobacter sp. (1) decreased. S. aureus (1), S. epidermidis (1), P. aeruginosa (5), and S. marcescens (1) persisted or appeared. The eradication rate was 83.7%. Six patients showed adverse reactions including general fatigue 1, epigastralgia 1, eruption 1, eosinophilia 1 and elevation of S-GOT 2. But all of the adverse reactions were mild or slight, and transient. These findings indicate that IPM/CS is a useful and safe drug against bacterial infections in internal medicine.
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PMID:[Clinical evaluation of imipenem/cilastatin sodium in the internal medicine]. 192 Aug 13

Imipenem is the first of a new class of beta-lactam antibiotics, the carbapenems, to be released for clinical use. It has the broadest antibacterial activity of all antibiotics available for systemic use in humans. It is active against streptococci, methicillin-sensitive staphylococci, Neisseria, Haemophilus, anaerobes, and the common aerobic gram-negative nosocomial pathogens including Pseudomonas. Resistance to imipenem may emerge during treatment of P. aeruginosa infections, as has occurred with other beta-lactam agents; P. maltophilia and P. cepacia are typically resistant to it. Like the penicillins, imipenem has inhibitory activity against enterococci. Daily doses may range from 500 mg to 1 g, every 6 to 8 hours, in patients with normal renal function. The principal toxic effects have been nausea and vomiting, which occur during intravenous infusion, and seizures, which develop in 1 to 3% of treated patients and are likely to occur in the setting of renal insufficiency and underlying disease of the central nervous system. Imipenem should be considered for treatment of mixed bacterial infections and treatment of resistant aerobic gram-negative bacteria that are not susceptible to other beta-lactam agents. In addition to provoking unnecessary toxicity, indiscriminate use of this agent will promote dissemination of resistance against it.
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PMID:Imipenem. 192 91

Phase contrast microscopy, killing curves and turbidimetric growth curves were used in a comparative study of the antibacterial effects of imipenem and meropenem on Haemophilus influenzae. The minimal inhibitory concentrations (MICs) and their ranges of meropenem and imipenem using five beta-lactamase-producing strains of H. influenzae were 0.03 (0.015-0.06) and 0.6 (0.5-1) micrograms/ml, respectively. Imipenem and meropenem induced spheroplast formation in cultures. Killing curves showed a bacteriostatic activity for meropenem and imipenem for MIC values, and a lag of 2 h in killing for MIC x 2 to MIC x 64. For these concentrations the killing rates of the two antibiotics were similar. Turbidimetric growth curves showed a higher early increase in optical density for meropenem. As far as the MIC value of meropenem was 10 times lower than the MIC value of imipenem, we may conclude that meropenem was more active than imipenem on beta-lactamase-producing strains of H. influenzae.
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PMID:Antibacterial effects of meropenem and imipenem against Haemophilus influenzae. 201 40

Imipenem proved highly active against Enterobacteriaceae: the different bacterial groups exhibited similar mode MICs (0.12 to 0.25 micrograms/ml), except for Serratia (0.25-0.5 micrograms/ml), Proteus mirabilis (0.5 micrograms/ml), indole-positive Proteus (2 micrograms/ml) and Providencia (1 mu/ml). The MICs of cefotaxime-resistant strains (cephalosporinase hyperproducing or very broad spectrum betalactamase producing) were within the susceptibility range. Imipenem also exhibited satisfactory activity against Pseudomonas aeruginosa (mode MIC 1-2 micrograms/ml), although resistant strains by decrease of permeability were observed, and against Acinetobacter (mode MIC 0.25-0.5 micrograms/ml). The MICs ranged from 0.03 to 4 micrograms/ml (mode MIC 0.5) for Haemophilus and from 0.25 to 1 micrograms/ml for Neisseria gonorrhoeae, regardless of the betalactamase producing status. The MICs for N. meningitidis were less than 0.06 micrograms/ml. Methicillin-susceptible staphylococci had low MICs ranging from 0.008 to 0.5 micrograms/ml (mode MIC 0.016). The MICs for methicillin-resistant strains varied widely from 0.016 to 64 micrograms/ml and were higher after incubation at 30 degrees C. Streptococci and pneumococci were highly susceptible (usually 0.008 to 0.03 micrograms/ml). The MICs for enterococci varied from 0.12 to 32 micrograms/ml (mode MIC 1-2). With the exception of Clostridium difficile, anaerobic bacteria were inhibited by concentrations lower than 1 (mode MIC 0.06 for C. Perfringens and 0.03 for Bacteroides fragilis).
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PMID:[In vitro activity of imipenem against hospital bacteria]. 213 36

Imipenem/cilastatin sodium (IPM/CS) was administered to 55 patients with respiratory tract infections (RTI). A clinical evaluation of IPM/CS was carried out in 51 patients, 28 with pneumonia, 4 with pulmonary abscess, 1 with pyothorax, 6 with bronchitis, 9 with bronchiectasis, 1 with diffuse panbronchiolitis and 2 with RTI with chronic obstructive pulmonary disease, and the clinical efficacy rate was 78.4%. Causative organisms were isolated in 23 strains out of 20 patients, such as Staphylococcus aureus 4 strains, Staphylococcus epidermidis 1 strain, Streptococcus pneumoniae 1 strain, Branhamella catarrhalis 1 strain, Haemophilus influenzae 2 strains, Klebsiella pneumoniae 4 strains, Pseudomonas aeruginosa 6 strains, Pseudomonas sp. 1 strain, Acinetobacter calcoaceticus 1 strain, Acinetobacter sp. 1 strain and glucose non-fermentative Gram-negative rod 1 strain. An eradication rate of 70.6% was obtained. An overall eradication rate of main causative organisms in RTI including S. aureus, S. pneumoniae, H. influenzae and K. pneumoniae was 75.0%. Clinical adverse effects were observed in 5 patients, and these were eruption in 2, itching in 1, vomiting in 1 and drug fever in 1. Abnormalities in laboratory test results were observed in 8 patients. These disappeared or returned to normal values after completion or discontinuation of IPM/CS administration. IPM/CS appears to be a useful antibiotic for the treatment of RTI, especially severe infections.
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PMID:[Evaluation of imipenem/cilastatin sodium in the treatment of respiratory tract infections]. 234 50

Imipenem-cilastatin was evaluated for tolerability and efficacy in a multicenter open, noncomparative trial involving 178 infants and children with bacterial infections. Imipenemcilastatin was administered in total daily dosages of 100 mg/kg for patients up to 3 years of age and 60 mg/kg for those more than 3 years of age. Favorable clinical response was achieved in 98 of 100 patients judged evaluable for efficacy. Adverse effects were generally mild and reversible and included diarrhea alone or with vomiting (5.1%), irritation of intravenous infusion site (3.3%) and rash (2.2%). Changes in laboratory test values reported most frequently were thrombocytosis (8.9%), elevations in aspartate aminotransferase (7.9%) and alanine aminotransferase (5.6%) and eosinophilia (8.4%). This safety profile appears to be comparable to that of other beta-lactam antibiotics. Moreover imipenem-cilastatin was effective in infections caused by a broad spectrum of pathogens that include Haemophilus influenzae, Staphylococcus aureus, P. aeruginosa and anaerobes. These attributes suggest that imipenem-cilastatin should be safe and effective in selected pediatric patients.
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PMID:Imipenem-cilastatin in pediatric patients: an overview of safety and efficacy in studies conducted in the United States. 268 88

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

Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium (IPM/CS) were performed in neonates. The results obtained are summarized as follows. 1. Plasma levels and urinary excretion of IPM and CS sodium were determined in 7 neonates with ages between 7 and 26 days (gestation periods were 37 to 41 weeks and birth weights were 2,410 to 3,890 g) upon 1 hour drip intravenous infusion of IPM/CS at 10 mg/10 mg/kg, or 20 mg/20 mg/kg. Mean plasma concentrations of IPM reached their peaks at the end of infusion with levels of 12.7 +/- 3.0 micrograms/ml for the group given 10 mg/10 mg/kg, and 19.1 +/- 4.1 micrograms/ml for 20 mg/20 mg/kg. The concentration of IPM in plasma showed a dose-response to the 10 mg/10 mg/kg and 20 mg/20 mg/kg dosages. Concentrations decreased with half-lives of 1.87 +/- 0.71 hours and 1.97 +/- 0.21 hours for the low and the high dosages, and plasma levels at 8 hours after administration were 0.3 +/- 0.1 microgram/ml and 0.8 +/- 0.3 microgram/ml, respectively. Mean urinary recovery rates in 8 hours after administration were 37.6 +/- 11.8% and 26.8 +/- 17.2% for the low and the high dosages. While, mean plasma concentrations and mean urinary recovery rates of CS were higher than those of IPM, mean plasma half-lives of CS were similar to IPM. 2. IPM/CS was administered to 11 neonatal patients (with ages between 1 and 26 days) of various bacterial infections, and clinical effectiveness, bacteriological efficacy and adverse reactions were evaluated. Clinical efficacies in cases including 7 with acute pneumonia and 1 each with suspected septicemia, intrauterine infection, acute urinary tract infection and periproctal abscess were judged excellent in 10 and good in 1 case, and the efficacy rate was 100%. Causative organisms isolated from these patients included 3 strains of Escherichia coli and 1 strain each of Streptococcus pyogenes, Streptococcus agalactiae Enterococcus faecalis and Haemophilus influenzae. All the organisms were eradicated by IPM/CS, thus the bacteriological eradication rate was 100%. No adverse reactions were observed, but decreased platelet in 1 patient and increased GOT in 2 patients were found as abnormal laboratory test values. These changes, however were transient, and returned to normal after discontinuation of IPM/CS. It was concluded that the clinical results of IPM/CS are indicative of excellent efficacy, safety and usefulness of the drug in the treatment of infections in neonates.
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PMID:[Pharmacokinetic, bacteriological and clinical studies on imipenem/cilastatin sodium in neonates]. 274 58

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


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