Linezolid is a last-resort antibiotic used to treat bacterial infections resistant to other antibiotics. Linezolid works by binding to the 50S ribosomal subunit of bacteria to prevent bacterial protein synthesis. Adverse effects include bone marrow suppression, neuropathy, and serotonin syndrome.

Key Points

  • Linezolid
    • Mechanism
      • Binds to 50S subunit of bacterial ribosomes
        • Prevents formation of initiation complex and inhibits bacterial protein synthesis
    • Clinical Use
      • Gram-positive species including MRSA and VRE
      • Usually used as a last-resort for multi-drug resistant infections
    • Adverse Effects
      • Bone marrow suppression
        • Anemia, leukopenia, and thrombocytopenia are common
      • Neuropathy
        • Includes optic neuritis and peripheral neuropathy
      • Serotonin syndrome
        • Due to partial monoamine oxidase (MAO) inhibition
        • Risk is compounded with use of other serotonergic drugs (e.g. MAOIs, SSRIs)
    • Resistance
      • Point mutation of ribosomal RNA changes 50S binding site