Oxazolidinones: Activity, Mode of Action, and Mechanism of Resistance

Int J Antimicrob Agents. 2004 Feb;23(2):113-9. doi: 10.1016/j.ijantimicag.2003.11.003.


Oxazolidinones are a new group of antibiotics. These synthetic drugs are active against a large spectrum of Gram-positive bacteria, including methicillin- and vancomycin-resistant staphylococci, vancomycin-resistant enterococci, penicillin-resistant pneumococci and anaerobes. Oxazolidinones inhibit protein synthesis by binding at the P site at the ribosomal 50S subunit. Resistance to other protein synthesis inhibitors does not affect oxazolidinone activity, however rare development of oxazolidinone resistance cases, associated with 23S rRNA alterations during treatment have been reported. Linezolid, the first oxazolidinone available, has already taken its place in the clinic for treatment of Gram-positive infections. Pharmacokinetic properties as well as its good penetration and accumulation in the tissue including bone, lung, vegetations, haematoma and cerebrospinal fluid, allow its use for surgical infections.

Publication types

  • Review

MeSH terms

  • Acetamides / pharmacology
  • Anti-Infective Agents / pharmacology*
  • Base Sequence
  • Drug Resistance, Bacterial / genetics*
  • Gram-Positive Bacteria / drug effects*
  • Gram-Positive Bacteria / genetics
  • Gram-Positive Bacterial Infections / microbiology
  • Humans
  • Linezolid
  • Molecular Sequence Data
  • Mutation
  • Oxazolidinones / pharmacology*
  • Peptidyl Transferases / genetics
  • RNA, Ribosomal, 23S / genetics


  • Acetamides
  • Anti-Infective Agents
  • Oxazolidinones
  • RNA, Ribosomal, 23S
  • Peptidyl Transferases
  • Linezolid