Pharm

Linezolid

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Linezolid, Zyvox, Tedizolid, Sivextro

  • Mechanism
  1. Linezolid is a prototype for new Oxazolidinone Class
  2. Inhibits protein synthesis at unique site
  3. Spectrum
    1. Minimal activity against Gram Negative Bacteria
    2. Bacteriostatic activity
      1. Vancomycin Resistant Enterococcus faecium
      2. Methicillin Resistant Staphylococcus Aureus
    3. Bactericidal activity
      1. Streptococcus Pneumoniae
      2. Streptococcus Pyogenes
      3. Streptococcus agalactiae
  • Pharmacokinetics
  1. Linezolid (Zyvox)
    1. Half Life: 5 hours
    2. Near 100% bioavailability after oral intake
  • Dosing
  1. Linezolid (Zyvox)
    1. Dose: 400 to 600 mg PO or IV q12 hours
    2. Administer intravenously over 30 to 120 minutes
  2. Tedizolid (Sivextro)
    1. Dosed once daily
  • Adverse Effects
  1. Rash
  2. Headache
  3. Diarrhea
  4. Nausea or Vomiting
  5. Insomnia
  6. Constipation
  7. Fever
  8. Myelosuppression (requires discontinuation)
    1. Thrombocytopenia (2.4%)
  • Drug Interactions
  1. No Cytochrome P450 activity or related Drug Interaction
  2. Reversible MAO inhibitor (Hypertensive response)
    1. Do not use with Tyramine Containing Foods
    2. Avoid with adrenergic drugs
      1. Avoid concurrent Pseudoephedrine use
      2. Use caution with concurrent Dopamine or Epinephrine
  3. Serotonin Syndrome (theoretical)
    1. Not observed in clinical trials
    2. Use caution with SSRI Antidepressants
  • Monitoring
  1. Linezolid (Zyvox)
    1. Weekly Complete Blood Count Indications
      1. Linezolid use longer than 2 weeks
      2. Preexisting Myelosuppression or risk factors
      3. Chronic infection on concurrent other antibiotics
  2. Tedizolid (Sivextro)
    1. No Complete Blood Count monitoring required
  • Cost
  1. Linezolid (Zyvox) costs $1350 to $2700
  2. Tedizolid (Sivextro) costs $1700 for a 6 day course