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Linezolid

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Linezolid, Zyvox, Oxazolidinone Antibiotic

  • See Also
  1. Tedizolid
  • 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
  • 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
  • Medications
  1. Tablets 600 mg
  2. Suspension 100 mg/5 ml
    1. Gently turn bottle 5 times to mix (do not shake)
    2. May store at room Temperature
  • Dosing
  1. Adult (or child age >12 years)
    1. Take 600 mg orally or IV infused over 30 to 120 min every 12 hours
  2. Child (age <12 years)
    1. Take 10 mg/kg (up to 600 mg) orally or IV infused over 30 to 120 min every 8 hours
  • Adverse Effects
  1. Rash
  2. Headache
  3. Diarrhea
  4. Nausea or Vomiting
  5. Insomnia
  6. Constipation
  7. Fever
  8. Lactic Acidosis
  9. Myelosuppression (requires discontinuation)
    1. Thrombocytopenia (2.4%)
  10. Neuropathy (with use >1 month)
    1. Optic Neuropathy (dilated Eye Exam if symptoms occur)
    2. Peripheral Neuropathy
  • Safety
  1. Pregnancy category C
  2. Unknown safety in Lactation
  • Pharmacokinetics
  1. Half Life: 5 hours
  2. Near 100% Bioavailability after oral intake
  • Drug Interactions
  1. No Cytochrome P450 activity or related Drug Interaction
  2. Reversible MAO Inhibitor (Hypertensive response)
    1. Limit Tyramine Containing Foods (<100 mg/meal)
    2. Avoid with adrenergic drugs
      1. Avoid concurrent Pseudoephedrine use
      2. Use caution with concurrent Dopamine or Epinephrine (decrease initial dosing)
  3. Serotonin Syndrome (theoretical, rare)
    1. Not observed in Clinical Trials
    2. Use caution with SSRI and SNRI Antidepressants
  4. Rifampin
    1. May decrease Linezolid levels and effect
  5. Hypoglycemic agents or Insulin
    1. Increased Hypoglycemia risk
  • Monitoring
  1. See Tedizolid (Sivextro) which does not require cbc monitoring
  2. 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
  • Resources
  1. Linezolid (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=6e70e63b-bfd5-478d-a8ee-8ba22c9efabd
  • 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]