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Linezolid
Aka: Linezolid, Zyvox, Tedizolid, Sivextro
- See Also
- Antibiotic Resistance
- Indications
- Vancomycin Resistant Enterococcus
- Nosocomial Pneumonia
- Methicillin Resistant Staphylococcus Aureus
- Penicillin Sensitive Streptococcus Pneumoniae
- Complicated Skin Infections
- Methicillin Resistant Staphylococcus Aureus
- Streptococcus Pyogenes
- Streptococcus agalactiae
- Community Acquired Pneumonia (Not first line agent)
- Does not cover HaemophilusInfluenzae
- Methicillin Sensitive Staphylococcus aureus
- Penicillin Sensitive Streptococcus Pneumoniae
- Mechanism
- Linezolid is a prototype for new Oxazolidinone Class
- Inhibits protein synthesis at unique site
- Spectrum
- Minimal activity against Gram Negative Bacteria
- Bacteriostatic activity
- Vancomycin Resistant Enterococcus faecium
- Methicillin Resistant Staphylococcus Aureus
- Bactericidal activity
- Streptococcus Pneumoniae
- Streptococcus Pyogenes
- Streptococcus agalactiae
- Pharmacokinetics
- Linezolid (Zyvox)
- Half Life: 5 hours
- Near 100% bioavailability after oral intake
- 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
- Adverse Effects
- Rash
- Headache
- Diarrhea
- Nausea or Vomiting
- Insomnia
- Constipation
- Fever
- Myelosuppression (requires discontinuation)
- Thrombocytopenia (2.4%)
-
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
- 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
- Tedizolid (Sivextro)
- No Complete Blood Count monitoring required
- Cost
- Linezolid (Zyvox) costs $1350 to $2700
- Tedizolid (Sivextro) costs $1700 for a 6 day course
- References
- (2000) Med Lett Drugs Ther 42:45-6 [PubMed]
- Ament (2002) Am Fam Physician 65(4):663-70 [PubMed]
- Moellering (2003) Ann Intern Med 138:135-42 [PubMed]