Linezolid--a Review of the First Oxazolidinone

Expert Opin Pharmacother. 2001 Feb;2(2):293-302. doi: 10.1517/14656566.2.2.293.


Linezolid is the first of a truly new class of antibiotics, the oxazolidinones. It acts as an inhibitor of bacterial protein synthesis by blocking the formation of the 70S ribosomal initiation complex. Its activity is bacteriostatic against some species (e.g., enterococci) and bactericidal against others (e.g., pneumococci). The antibacterial spectrum of linezolid includes Gram-positive pathogens and some Gram-negative anaerobic species but not Gram-negative aerobes. Importantly, multi-drug resistant organisms such as methicillin-resistant staphylococci, staphylococci with reduced susceptibility to vancomycin, penicillin- and macrolide-resistant pneumococci and vancomycin-resistant enterococci are fully susceptible to linezolid. Linezolid has almost 100% bioavailability and the area under the plasma concentration curve is identical after oral and iv. administration. This enables initial oral administration of linezolid in those patients who can absorb the drug normally and also an early step-down therapy from iv. to oral. Controlled, randomised clinical studies have documented efficacy and safety of linezolid in hospital- and community-acquired pneumonia, uncomplicated and complicated skin and soft tissue infections and infections caused by vancomycin-resistant enterococci. The safety and tolerability of linezolid are advantageous. Linezolid is a weak and reversible monoamine oxidase (MAO) inhibitor and although no increased frequency of adrenergic or serotonergic adverse events has been reported, it is recommended that linezolid is used with caution in patients treated with other MAO inhibitors.

Publication types

  • Review

MeSH terms

  • Acetamides / adverse effects
  • Acetamides / pharmacokinetics
  • Acetamides / pharmacology*
  • Acetamides / therapeutic use
  • Animals
  • Anti-Bacterial Agents / adverse effects
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use
  • Biological Availability
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Community-Acquired Infections / drug therapy
  • Cross Infection / drug therapy
  • Gram-Negative Anaerobic Bacteria / drug effects*
  • Gram-Negative Bacterial Infections / drug therapy*
  • Gram-Positive Bacterial Infections / drug therapy*
  • Humans
  • Linezolid
  • Microbial Sensitivity Tests
  • Oxazolidinones / adverse effects
  • Oxazolidinones / pharmacokinetics
  • Oxazolidinones / pharmacology*
  • Oxazolidinones / therapeutic use
  • Randomized Controlled Trials as Topic
  • Treatment Outcome


  • Acetamides
  • Anti-Bacterial Agents
  • Oxazolidinones
  • Linezolid