KEY POINTS
- Linezolid (Zyvox) is an oxazolidinone antibiotic that works on susceptible bacteria through interfering with bacterial protein synthesis. It binds to the bacterial 23S ribosomal RNA of the 50S subunit, which prevents formation of a functional 70S initiation complex essential to bacterial translation.
- Active against many Gram positive bacteria
- Bacteriostatic versus Staphylococci and Enterococci
- A common drug to consider for treating vancomycin-resistant Enterococci (VRE)
- Considered non-inferior to vancomycin for treatment of MRSA pneumonia. NOTE: vancomycin is bactericidal versus MRSA, but does not penetrate the lungs as well as linezolid
- Generally, linezolid is avoided for MRSA bloodstream infection due to being bacteriostatic
- Bacetricidal versus most Streptococci
- Bacteriostatic versus Staphylococci and Enterococci
- Active against a variety of mycobacteria and sometimes used in salvage regimens for treating Mycobacterium tuberculosis or Mycobacterium abscessus
- Active against many Gram positive bacteria
- Typical dose is 600mg oral or intravenous given twice daily
- 100% bioavailable, can even be used as oral for bloodstream infection
- No need to adjust doses for renal or hepatic function per package insert
- A dose of 600mg per day or 300mg per day is sometimes used in patients on long-term treatment, to try to reduce the chances for toxicity
- Higher than standard dosing may be considered in patients who are obese and/or critically ill
- Oral solution is rarely used in adults, the tablets are commonly crushed and administered orally when the patient cannot swallow
- Beware drug-drug interactions with tyramine containing foods (e.g., cured meats), selective seritonin repute inhibitors (SSRIs) and monamine oxidase inhibitors (MAOIs)
- Risk serotonin syndrome
- Beware thrombocytopenia (low platelets), especially with durations of therapy greater than 10 days
- Beware irreversible peripheral neuropathy and optic neuritis, both of which are associated with durations of therapy greater than 28 days
- Since going generic has dropped substantially in price, with the oral formulation now being more widely accepted as an anti-MRSA or anti-VRE agent
RESOURCES
- Linezolid Package Insert (oral tablet, oral solution, injectable)
- Linezolid review in JAC (2016)
- Treatment considerations in vancomycin-resistant Enterococcal bacteremia: daptomycin or linezolid? A review (IJCP, 2013)
- Systematic review and meta-analysis of linezolid versus daptomycin for treatment of vancomycin-resistant Enterococcal bacteremia (AAC, 2014)
- Linezolid pharmacokinetics and pharmacodynamics in clinical treatment (JAC, 2011)
- IDSA Practice Guidelines