II. Indications
- Vancomycin Resistant Enterococcus
- Nosocomial Pneumonia
- Complicated Skin Infections
- Community Acquired Pneumonia (Not first line agent)
- Does not cover HaemophilusInfluenzae
- Methicillin Sensitive Staphylococcus aureus
- Penicillin Sensitive Streptococcus Pneumoniae
III. Mechanism
- Linezolid is a prototype for new Oxazolidinone Class
- Inhibits protein synthesis at unique site
- Spectrum
- Minimal activity against Gram Negative Bacteria
- Bacteriostatic activity
- Bactericidal activity
IV. Pharmacokinetics
- Linezolid (Zyvox)
- Half Life: 5 hours
- Near 100% bioavailability after oral intake
V. Dosing
- Linezolid (Zyvox)
- Dose: 400 to 600 mg PO or IV q12 hours
- Administer intravenously over 30 to 120 minutes
- Tedizolid (Sivextro)
- Dosed once daily
VI. Adverse Effects
- Rash
- Headache
- Diarrhea
- Nausea or Vomiting
- Insomnia
- Constipation
- Fever
- Myelosuppression (requires discontinuation)
- Thrombocytopenia (2.4%)
VII. Drug Interactions
- No Cytochrome P450 activity or related Drug Interaction
- Reversible MAO inhibitor (Hypertensive response)
- Do not use with Tyramine Containing Foods
- Avoid with adrenergic drugs
- Avoid concurrent Pseudoephedrine use
- Use caution with concurrent Dopamine or Epinephrine
-
Serotonin Syndrome (theoretical)
- Not observed in clinical trials
- Use caution with SSRI Antidepressants
VIII. 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
- Tedizolid (Sivextro)
- No Complete Blood Count monitoring required
IX. Cost
- Linezolid (Zyvox) costs $1350 to $2700
- Tedizolid (Sivextro) costs $1700 for a 6 day course
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Related Studies (from Trip Database) Open in New Window
| 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 |
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 |
