Linezolid: a review of its properties, function, and use in critical care

doi:10.2147/DDDT.S164515

Paper

Linezolid: a review of its properties, function, and use in critical care

Published Jun 1, 2018 · S. Hashemian, T. Farhadi, Mojdeh Ganjparvar

Drug Design, Development and Therapy

Q1 SJR score

251

Citations

9

Influential Citations

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Abstract

Linezolid can be considered as the first member of the class of oxazolidinone antibiotics. The compound is a synthetic antibiotic that inhibits bacterial protein synthesis through binding to rRNA. It also inhibits the creation of the initiation complex during protein synthesis which can reduce the length of the developed peptide chains, and decrease the rate of reaction of translation elongation. Linezolid has been approved for the treatment of infections caused by vancomycin-resistant Enterococcus faecium, hospital-acquired pneumonia caused by Staphylococcus aureus, complicated skin and skin structure infections (SSSIs), uncomplicated SSSIs caused by methicillin-susceptible S. aureus or Streptococcus pyogenes, and community-acquired pneumonia caused by Streptococcus pneumoniae. Analysis of high-resolution structures of linezolid has demonstrated that it binds a deep cleft of the 50S ribosomal subunit that is surrounded by 23S rRNA nucleotides. Mutation of 23S rRNA was shown to be a linezolid resistance mechanism. Besides, mutations in specific regions of ribosomal proteins uL3 and uL4 are increasingly associated with linezolid resistance. However, these proteins are located further away from the bound drug. The methicillin-resistant S. aureus and vancomycin-resistant enterococci are considered the most common Gram-positive bacteria found in intensive care units (ICUs), and linezolid, as an antimicrobial drug, is commonly utilized to treat infected ICU patients. The drug has favorable in vitro and in vivo activity against the mentioned organisms and is considered as a useful antibiotic to treat infections in the ICU.

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Study Snapshot

Linezolid is a useful antibiotic for treating infections caused by vancomycin-resistant bacteria and is commonly used in ICUs to treat infections caused by methicillin-resistant S. aureus and vancomycin-resistant enterococci.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Linezolid: a review of its properties, function, and use in critical care

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References

Comparing the cost-effectiveness of linezolid to trimethoprim/sulfamethoxazole plus rifampicin for the treatment of methicillin-resistant Staphylococcus aureus infection: a healthcare system perspective.

Trimethoprim-sulfamethoxazole plus rifampicin is more cost-effective than linezolid for treating MRSA infection, with a 95% discount needed for better value for money.

Structural Basis for Linezolid Binding Site Rearrangement in the Staphylococcus aureus Ribosome

A single amino acid deletion in ribosomal protein uL3 leads to linezolid resistance in Staphylococcus aureus, providing a potential strategy for designing oxazolidinone antibiotics to combat known resistance mechanisms.

Virtual Screening for Potential Inhibitors of CTX-M-15 Protein of Klebsiella pneumoniae

Three novel drug-like compounds identified through virtual screening show potential as competitive inhibitors against Klebsiella pneumoniae's CTX-M-15 protein, potentially aiding in the development of anti-bacterial novel drug candidates.

Comparing the cost-effectiveness of linezolid to trimethoprim/sulfamethoxazole plus rifampicin for the treatment of MRSA infection: a health-care system perspective

Linezolid is more cost-effective than trimethoprim-sulfamethoxazole plus rifampicin for treating MRSA infection, as demonstrated by a stochastic cost-effectiveness analysis.

Successful Treatment of Necrotizing Fasciitis and Streptococcal Toxic Shock Syndrome with the Addition of Linezolid

Linezolid can effectively improve clinical outcomes in patients with streptococcal necrotizing fasciitis and toxic shock syndrome not improving with standard therapy.

Daptomycin versus linezolid for the treatment of vancomycin-resistant enterococcal bacteraemia: implications of daptomycin dose.

Higher-dose daptomycin (9 mg/kg) is associated with better survival than lower-dose daptomycin for treating vancomycin-resistant enterococcal bacteraemia.

Linezolid-associated reticulocytopenia

Linezolid-associated reticulocytopenia is a rare and uncommon side effect of antibiotic therapy, with reticulocyte counts returning to normal after discontinuing the drug.

Linezolid-Associated Optic Neuropathy in Drug-Resistant Tuberculosis Patients in Mumbai, India

One out of four drug-resistant TB patients in Mumbai, India, experienced optic neuropathy, highlighting the need for systematic monitoring and specialized diagnostic services.

Similar efficacy and safety of daptomycin versus linezolid for treatment of vancomycin-resistant enterococcal bloodstream infections: a meta-analysis.

Daptomycin and linezolid show similar efficacy and safety for treating vancomycin-resistant enterococcal bloodstream infections, but the meta-analysis is limited by heterogeneity between small-scale retrospective studies.

Citations

Historical examination of tuberculosis; from ancient affliction to modern challenges.

Tuberculosis has evolved from an ancient affliction to a modern challenge, with advancements in diagnosis and treatment, but drug resistance remains a significant concern for the future.

Prevalence and genetic insights of linezolid resistance in tuberculosis: A study of sensitive and resistant clinical isolates.

Linezolid resistance is detected in 6.6% of tuberculosis cases, highlighting the need for drug susceptibility testing in managing complex drug-resistant infections.

High prevalence and plasmidome diversity of optrA-positive enterococci in a Shenzhen community, China

OptrA-positive enterococci and pAD1 + DOp1-type plasmids pose a greater public health threat than their non-optrA-positive counterparts, with many antimicrobial resistance genes co-existing on these plasmids.

Response of Staphylococcus aureus to combination of virulent bacteriophage vB_SauM-515A1 and linezolid

Combining bacteriophage vB_SauM-515A1 and linezolid effectively inhibits Staphylococcus aureus growth, with potential for combination therapy approaches in infectious disease treatments.

CSF pharmacokinetics-pharmacodynamics of linezolid in critically brain injured patients, with or without central nervous system healthcare-associated infection. The PK-Pop-LCR Study: A Multicenter Pharmacokinetics and Pharmacodynamics Population Study.

Higher doses of linezolid than recommended should be considered for treating central nervous system infections in critically brain injured patients.

Vancomycin and linezolid: severe cutaneous adverse reactions to drugs.

Vancomycin presents a higher risk of severe cutaneous adverse reactions compared to linezolid, particularly for Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS).

Linezolid-Induced Lactic Acidosis: A Case Report

Prolonged use of linezolid for treating resistant gram-positive bacteria can lead to lactic acidosis, even with normal liver and kidney function.