Linezolid

Aka: Linezolid, Zyvox, Tedizolid, Sivextro

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II. Indications

  1. Vancomycin Resistant Enterococcus
  2. Nosocomial Pneumonia
    1. Methicillin Resistant Staphylococcus Aureus
    2. Penicillin Sensitive Streptococcus Pneumoniae
  3. Complicated Skin Infections
    1. Methicillin Resistant Staphylococcus Aureus
    2. Streptococcus Pyogenes
    3. Streptococcus agalactiae
  4. Community Acquired Pneumonia (Not first line agent)
    1. Does not cover HaemophilusInfluenzae
    2. Methicillin Sensitive Staphylococcus aureus
    3. Penicillin Sensitive Streptococcus Pneumoniae

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

X. References

  1. (2000) Med Lett Drugs Ther 42:45-6 [PubMed]
  2. Ament (2002) Am Fam Physician 65(4):663-70 [PubMed]
  3. Moellering (2003) Ann Intern Med 138:135-42 [PubMed]

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Related Studies

Cost: Medications

linezolid (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
LINEZOLID 600 MG TABLET Generic $1.66 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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