III. 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

IV. Pharmacokinetics

  1. Linezolid (Zyvox)
    1. Half Life: 5 hours
    2. Near 100% bioavailability after oral intake

V. 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

VI. 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%)

VII. 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

VIII. 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

IX. Cost

  1. Linezolid (Zyvox) costs $1350 to $2700
  2. Tedizolid (Sivextro) costs $1700 for a 6 day course

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Cost: Medications

linezolid (on 8/17/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
LINEZOLID 600 MG TABLET Generic $8.46 each
zyvox (on 6/1/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
ZYVOX 100 MG/5 ML SUSPENSION $6.64 per ml
ZYVOX 600 MG TABLET Generic $8.46 each

Ontology: linezolid (C0663241)

Definition (NCI) A synthetic oxazolidinone derivative, Linezolid selectively inhibits an early step in bacterial protein synthesis and affects blood pressure through monoamine oxidase inhibition. It is effective against Gram-positive organisms, including methicillin-resistant Staphylococcus aureus strains, coagulase-negative Staphylococci, vancomycin-resistant Enterococci, and penicillin-resistant Streptococcus pneumoniae strains. (NCI04)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C098010
SnomedCT 125695009, 387056004
LNC LP21256-0, MTHU013614
English N-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide, linezolid (medication), linezolid, linezolid [Chemical/Ingredient], LINEZOLID, linezolide, Linezolid (product), Linezolid (substance), Linezolid
Spanish linezolid, linezolid (producto), linezolida (producto), linezolid (sustancia), linezolida, linezolida (sustancia)

Ontology: Zyvox (C0876226)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C098010
English Zyvox, zyvox