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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Cost: Medications

linezolid (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
LINEZOLID 600 MG TABLET Generic $4.61 each
zyvox (on 6/1/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
ZYVOX 100 MG/5 ML SUSPENSION $7.96 per ml
ZYVOX 600 MG TABLET Generic $4.61 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.

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)
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Zyvox (C0876226)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C098010
English Zyvox, zyvox
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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