Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0032285 (pneumonia)
 54,520 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We tested ertapenem (MK-0826), a new carbapenem, and 13 other antimicrobials by microbroth dilution against 102 isolates of Streptococcus pneumoniae, selected to include organisms resistant to a variety of drug classes. Ertapenem MICs ranged from < or =0.008 to 4 mg/l, MIC(50)=0.5 mg/l, and MIC(90)=2 mg/l. Based on MIC(90), ertapenem potency was 4-fold greater than cefuroxime, 2-fold greater than amoxycillin/clavulanate, =penicillin, 2-fold less than meropenem and ceftriaxone, and 4-fold less than imipenem. Other drug classes including macrolides, tetracycline and fluoroquinolones were less potent overall than the carbapenems. Linezolid (MIC(90)=1 mg/l) was the only agent tested for which all isolates were fully susceptible. Activity of ertapenem decreased as MICs to penicillins, cephalosporins, other carbapenems and macrolides increased. Isolates resistant to clindamycin, tetracycline or fluoroquinolones showed no obvious decrease in ertapenem activity when compared with susceptible isolates with the majority of isolates resistant to these drug classes inhibited by ertapenem at concentrations less than 1 mg/l. Ertapenem may prove useful as an alternative to ceftriaxone and other agents in the treatment of community-acquired pneumonia (CAP) due to S. pneumoniae, including infections caused by organisms with reduced susceptibilities to other antimicrobial agents.
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PMID:In vitro activity of ertapenem (MK-0826) against multi-drug resistant Streptococcus pneumoniae compared with 13 other antimicrobials. 1229 63

This study compared the in vitro activity of ertapenem, ceftriaxone, cefepime, ciprofloxacin and amoxicillin-clavulanate against 381 aerobic and facultative bacterial pathogens isolated from 320 patients with acute bacterial exacerbation of chronic bronchitis or community-acquired pneumonia. Streptococcus pneumoniae and Haemophilus influenzae accounted for 54.6% of the isolates. The ertapenem MIC was < or =2 mg/L for 98.4% of isolates and > or =8 mg/L for 1.0% (all methicillin-resistant Staphylococcus aureus). Ertapenem had the most potent activity against Enterobacteriaceae, Moraxella catarrhalis, and methicillin-susceptible S. aureus, and its activity against H. influenzae and H. parainfluenzae, all strains of which were susceptible, was not altered by beta-lactamase production. Only one S. pneumoniae strain, a penicillin-resistant isolate, was resistant to ertapenem. Ertapenem was highly active in vitro against pyogenic bacteria recovered from patients with community-acquired lower respiratory tract infections.
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PMID:Comparative in vitro activity of ertapenem against bacterial pathogens isolated from patients with lower respiratory tract infections. 1244 16

Ertapenem sodium (trade name Invanz, also designated as MK-0826, MK-826 and L-749345), manufactured by Merck & Co., Inc. is a structurally unique parenteral 1 beta-methyl carbapenem. It has a broad spectrum of antimicrobial activity, including common community-acquired Gram-positive and Gram-negative aerobic and anaerobic pathogens, and restricted activity against nosocomial pathogens such as Pseudomonas aeruginosa, Acinetobacter species, methicillin-resistant staphylococci and enterococci. Ertapenem demonstrates excellent activity against cephalosporin-resistant enteric organisms producing extended spectrum beta-lactamases (ESBLs) or AmpC beta-lactamases and excellent activity against penicillin-resistant Streptococcus pneumoniae. Its high level of protein binding and serum half-life of 4 h allows it to be dosed once daily. Ertapenem may be administered intravenously or intramuscularly and has an excellent adverse reaction and tolerability profile. Invanz was approved by the United States Food and Drug Administration in November 2001 for the treatment of adult patients with moderate to severe infections caused by designated strains of susceptible microorganisms. The infections include complicated intraabdominal infections, complicated skin and skin structure infections, community-acquired pneumonia, complicated urinary tract infections including pyelonephritis and acute pelvic infections including postpartum endomyometritis, septic abortion and post surgical gynecologic infections. Invanz has also been approved in Mexico, Brazil and New Zealand.
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PMID:Ertapenem. A review of its microbiologic, pharmacokinetic and clinical aspects. 1253 75

Ertapenem is a carbapenem that shares the activity of imipenem and meropenem against most species, but is less active against non-fermenters. Activity is retained against most strains with AmpC and extended-spectrum beta-lactamases, although resistance can arise if these enzymes are combined with extreme impermeability. Resistance can also be caused by IMP, VIM, KPC and NMC carbapenemases, but again, co-requires impermeability. Although the spread of carbapenemases in the future is a concern, they are currently very rare. Given as a 1 g intravenous (iv) infusion once daily, ertapenem has a plasma half-life of approximately 4 h in healthy volunteers, and a Cmax of 155 mg/L and 13 mg/L for total and free drug, respectively. Excretion is largely renal, divided equally between native drug and an open-ring derivative. Trials show equivalence to piperacillin/tazobactam or ceftriaxone in (a) intra-abdominal infections, (b) community-acquired pneumonia, (c) acute pelvic infections, (d) skin and skin structure infections and (e) complicated urinary tract infections. The USA licence grants all these five indications; the EU licence grants the first three. Further potential uses include home iv therapy, directed therapy against Enterobacteriaceae with AmpC or extended-spectrum cephalosporinases, and tentatively, surgical prophylaxis. Widening the usage of carbapenems raises public health concerns, somewhat allayed by the continued rarity of carbapenemases after 17 years of imipenem use, and by the fact that carbapenemases occur mostly in non-fermenters outside the spectrum of ertapenem, and co-require impermeability to confer resistance in Enterobacteriaceae. Nevertheless, if ertapenem is to be used widely, its effects on the resistance ecology need to be monitored carefully.
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PMID:Properties and potential of ertapenem. 1291 43

Infectious diseases play an important role in the elderly. Disease progression is often more severe, displaying a higher complication rate and causing increased mortality. Elderly patients suffer more frequently than younger under pneumonia, exacerbations of chronic bronchitis, urinary tract infections as well as skin and soft tissue infections. When starting empiric antibiotic therapy one should consider that the bacterial spectrum afflicting elderly patients may differ from that afflicting younger patients. In addition an increasing number of nosocomial and multiresistant pathogens is seen in elderly patients due to more frequent hospitalisation and living in nursing homes. Patient multimorbidity and multiple co-medications make awareness of important drug-interactions essential. The purpose of this article is to review the indications and side-effects of well-tried and newer antibiotics with respect to patients age. Especially the newer antibiotics Ertapenem, Linezolid, Quinupristin/Dalfopristin and Telithromycin are discussed in detail.
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PMID:[Problems of pharmacotherapy of infections in the aged]. 1467 13

Ertapenem is a long-acting, 1beta-methyl parenteral Group 1 carbapenem antibiotic that has a broad antibacterial spectrum and once-a-day dosing supported by clinical studies. Ertapenem is active against both Gram-positive and Gram-negative bacteria, including Enterobacteriaceae, Streptococcus pneumoniae and most species of anaerobic bacteria. Isolates from a variety of infections (intra-abdominal infections, skin/soft-tissue infections, community-acquired pneumonia, pelvic infections and urinary tract infections) are inhibited by ertapenem. It has restricted activity against nosocomial pathogens such as Pseudomonas aeruginosa, Acinetobacter species, methicillin-resistant staphylococci and enterococci. Ertapenem has potent activity against the majority of anaerobic isolates from intra-abdominal infections, and against most of the aerobes isolated from these infections, with the exceptions of the nosocomial pathogens mentioned above. MIC(90)s for most species of Enterobacteriaceae were <1 mg/L, significantly lower than those of imipenem. MIC(90)s for most Bacteroides fragilis group isolates ranged from 1 to 4 mg/L, and MIC(90)s were species specific for Clostridium, ranging from 0.06 mg/L for Clostridium perfringens to 4 mg/L for Clostridium clostridioforme. Ertapenem was equivalent to or better than piperacillin-tazobactam in activity against most anaerobic species isolated from these infections, and was more potent than piperacillin-tazobactam and ceftriaxone against the most common skin pathogens (e.g. methicillin-susceptible Staphylococcus aureus). Ertapenem was highly active against most of the pathogens isolated from patients with community-acquired pneumonia, except for isolates of methicillin-resistant S. aureus (which are infrequent causes of community-acquired infection); these isolates were also resistant to ceftriaxone. Resistance to ertapenem is most commonly attributable to a variety of mechanisms including alterations in penicillin-binding proteins in Gram-positive organisms, and combinations of potent metallo-beta-lactamase enzymes, porin protein defects and efflux pumps in Gram-negative organisms.
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PMID:In vitro activity of ertapenem: review of recent studies. 1515 Jan 79

Ertapenem, a Group 1 carbapenem, is a once-a-day parenteral beta-lactam antibiotic recently licensed in the USA and Europe. Monotherapy with ertapenem dosed as 1 g once a day has been shown to be highly effective in clinical trials for the treatment of complicated infections of skin and skin structures, complicated intra-abdominal infections, community-acquired pneumonia, acute pelvic infections and complicated urinary tract infections. Dosing modifications have not been recommended for adults on the basis of gender, age, weight or liver disease. Presently there are no data regarding the use of ertapenem in children. Dose reductions are indicated for patients with advanced renal insufficiency. Ertapenem is neither a substrate nor an inhibitor of P-glycoprotein or cytochrome P450 enzymes; significant drug interactions between ertapenem and drugs handled by these systems are not expected.
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PMID:Pharmacokinetics and pharmacodynamics of ertapenem: an overview for clinicians. 1515 Jan 80

The carbapenems are beta-lactam-type antibiotics with an exceptionally broad spectrum of activity. Ertapenem is a new carbapenem developed to address the pharmacokinetic shortcomings (short half-life) of imipenem and meropenem. Ertapenem shares similar structural features with meropenem, including its stability to dehydropeptidase-1, allowing it to be administered without a dehydropeptidase-1 inhibitor. Ertapenem, like imipenem and meropenem, demonstrates broad-spectrum antimicrobial activity against many Gram-positive and -negative aerobes and anaerobes and is resistant to nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpCs. However, it differs from both imipenem and meropenem in demonstrating limited activity against Enterococcusspp., Pseudomonasaeruginosa and other nonfermentative Gram-negative bacteria commonly associated with nosocomial infections. The extensive protein binding of ertapenem extends the half-life and allows for once-daily dosing. Prospective, multicenter, randomized, double-blind, comparative clinical studies demonstrate similar clinical efficacy of ertapenem compared with other agents. Clinical trials of complicated intra-abdominal infection, acute pelvic infection, complicated skin and soft-structure infection, community-acquired pneumonia and complicated urinary tract infections demonstrated that ertapenem has equivalent efficacy and safety compared with ceftriaxone and piperacillin/tazobactam. Ertapenem is a promising new carbapenem with excellent efficacy and safety for the treatment of a variety of community-acquired infections. It also appears to be of great value as an outpatient parenteral antimicrobial therapy.
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PMID:Ertapenem: review of a new carbapenem. 1575 55

Ertapenem is approved for the treatment of community-acquired pneumonia (CAP), but its in vivo penetration into lung tissue (LT), epithelial lining fluid (ELF), and alveolar cells (AC) is unknown. Fifteen patients undergoing thoracotomy were treated with 1 g intravenously for perioperative prophylaxis. Bronchoalveolar lavage was performed 1, 3, and 5 hours after ertapenem infusion. Normal LT was sampled at the time of lung extraction. Blood was collected before and at different time points up to 24 hours after infusion. Mean concentrations of ertapenem in plasma, ELF, and AC were at 1.0 hour, 63.1, 4.06, 0.004 mg/L; at 3.0 hours, 39.7, 2.59, 0.003 mg/L; and at 5.0 hours, 27.2, 2.83, 0.007 mg/L. Mean (range) concentration in LT was 7.60 (2.5-19.4) mg/kg tissue 1.5 to 4.5 hours after infusion. In plasma, ertapenem exhibited a Cmax of 94.7 +/- 23.3 mg/L and an AUC(0-last) of 501.1 +/- 266.3 mg x h/L. These results, combined with the reported (MIC)90 of most CAP bacteria, support the previously observed clinical efficacy of ertapenem in the treatment of CAP.
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PMID:Penetration of ertapenem into different pulmonary compartments of patients undergoing lung surgery. 1590 47

The Group 1, 1 beta-methyl carbapenem ertapenem (Invanz) is approved for parenteral use in patients with complicated intra-abdominal infection (cIAI), community-acquired pneumonia (CAP) and acute pelvic infection caused by susceptible strains of certain designated organisms in both the US and the EU. Additional approved indications in the US include complicated skin and skin structure infection (cSSSI) and complicated urinary tract infection (cUTI). Ertapenem is approved for use in adults in both the US and the EU and in paediatric patients aged >or=3 months in the US. Ertapenem has a broad spectrum of in vitro activity against Gram-negative pathogens, including extended-spectrum beta-lactamase (ESBL)- and AmpC-producing Enterobacteriaceae, Gram-positive pathogens and anaerobic pathogens. It has similar efficacy to comparator antibacterials such as piperacillin/tazobactam in cSSSI (including diabetic foot infection), cIAI and acute pelvic infection and ceftriaxone with or without metronidazole in cIAI, cUTI and CAP. The drug has also shown efficacy in the treatment of paediatric patients with complicated community-acquired bacterial infections. Ertapenem has a convenient once-daily administration schedule and is generally well tolerated. Thus, ertapenem is an important option for the empirical treatment of complicated community-acquired bacterial infections in hospitalised patients.
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PMID:Ertapenem: a review of its use in the treatment of bacterial infections. 1622 76


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