II. Indications
- Vancomycin Resistant Enterococcus
- Nosocomial Pneumonia
- Complicated Skin Infections
-
Community Acquired Pneumonia (Not first line agent)
- Does not cover Haemophilus Influenzae
- Methicillin Sensitive Staphylococcus Aureus
- Penicillin Sensitive Streptococcus Pneumoniae
III. Mechanism
- Linezolid is a prototype for a new Oxazolidinone Class
-
Anti-Ribosomal Antibiotic
- Linezolid binds the 50S ribosome subunit at a unique site (23S ribosomal RNA site)
- Prevents formation of a functional 70S ribosome initiation complex
- Spectrum
- Minimal activity against Gram Negative Bacteria
- Bacteriostatic activity
- Bactericidal activity
IV. Medications
- Tablets 600 mg
- Suspension 100 mg/5 ml
- Gently turn bottle 5 times to mix (do not shake)
- May store at room Temperature
V. Dosing
- Adult (or child age >12 years)
- Take 600 mg orally or IV infused over 30 to 120 min every 12 hours
- Child (age <12 years)
- Take 10 mg/kg (up to 600 mg) orally or IV infused over 30 to 120 min every 8 hours
VI. Adverse Effects
- Rash
- Headache
- Insomnia
- Fever
- Lactic Acidosis
- Gastrointestinal symptoms
- Myelosuppression (requires discontinuation)
- Thrombocytopenia (2.4%)
- May also cause Anemia and Neutropenia
-
Neuropathy (with use >1 month)
- Optic Neuropathy (dilated Eye Exam if symptoms occur)
- Peripheral Neuropathy
VII. Safety
- Pregnancy category C
- Unknown safety in Lactation
VIII. Pharmacokinetics
- Half Life: 5 hours
- Near 100% Bioavailability after oral intake
IX. Drug Interactions
- No Cytochrome P450 activity or related Drug Interaction
- Reversible MAO Inhibitor (Hypertensive response)
- Limit Tyramine Containing Foods (<100 mg/meal)
- Avoid with adrenergic drugs
- Avoid concurrent Pseudoephedrine use
- Use caution with concurrent Dopamine or Epinephrine (decrease initial dosing)
-
Serotonin Syndrome (theoretical, rare)
- Not observed in Clinical Trials
- Use caution with SSRI and SNRI Antidepressants
-
Rifampin
- May decrease Linezolid levels and effect
- Hypoglycemic agents or Insulin
- Increased Hypoglycemia risk
X. Monitoring
- See Tedizolid (Sivextro) which does not require cbc monitoring
- Linezolid (Zyvox)
- Weekly Complete Blood Count Indications
- Linezolid use longer than 2 weeks
- Preexisting Myelosuppression or risk factors
- Chronic infection on concurrent other Antibiotics
- Weekly Complete Blood Count Indications
XI. Resources
Images: Related links to external sites (from Bing)
Related Studies
| linezolid (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| LINEZOLID 600 MG TABLET | Generic | $1.66 each |