Linezolid Antimicrobial Coverage
Linezolid is effective against a broad spectrum of gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), and penicillin-resistant Streptococcus pneumoniae, making it a valuable option for treating serious gram-positive infections. 1
Gram-Positive Coverage
Staphylococci
- Staphylococcus aureus (including methicillin-resistant strains)
- Staphylococcus epidermidis (including methicillin-resistant strains)
- Staphylococcus haemolyticus
Enterococci
- Enterococcus faecium (including vancomycin-resistant strains)
- Enterococcus faecalis (including vancomycin-resistant strains)
Streptococci
- Streptococcus pneumoniae (including multi-drug resistant isolates)
- Streptococcus pyogenes (Group A streptococci)
- Streptococcus agalactiae (Group B streptococci)
- Viridans group streptococci
Limited Gram-Negative Coverage
- Pasteurella multocida
Anaerobic Coverage
- Clostridium perfringens
- Clostridium difficile
- Peptostreptococcus species
- Bacteroides fragilis
Clinical Applications
Linezolid is particularly valuable for treating infections caused by resistant gram-positive pathogens:
MRSA infections: Linezolid is recommended as an oral option for MRSA skin and soft-tissue infections with a strong recommendation (1A) 2
Vancomycin-resistant enterococci: Linezolid is considered the drug of choice for infections caused by vancomycin-resistant enterococci 2
Multi-drug resistant Streptococcus pneumoniae: Effective against pneumococcal strains resistant to multiple antibiotics 1
Mechanism of Action
Linezolid works through a unique mechanism that differs from other antibiotics:
- Binds to the bacterial 23S ribosomal RNA of the 50S subunit
- Prevents formation of functional 70S initiation complex
- Inhibits bacterial protein synthesis
- Generally bacteriostatic against staphylococci and enterococci
- Bactericidal against streptococci 1
Important Clinical Considerations
Resistance concerns: Resistance to linezolid can develop, particularly in Enterococcus faecium with prolonged use or in patients with unremoved prosthetic devices or undrained abscesses 1
Adverse effects: Long-term use is limited by:
- Myelosuppression (thrombocytopenia most common)
- Peripheral and optic neuropathy (potentially irreversible)
- Lactic acidosis
- Serotonin syndrome (when used with serotonergic medications) 2
Monoamine oxidase inhibition: Linezolid is a reversible, nonselective inhibitor of monoamine oxidase, which can lead to interactions with adrenergic and serotonergic agents 1
Dosing Considerations
- Standard dose: 600 mg twice daily for most infections
- For uncomplicated skin infections: 400 mg twice daily
- No dosage adjustment needed for mild to moderate renal or hepatic impairment 2
Linezolid's excellent oral bioavailability allows for easy transition from intravenous to oral therapy, making it valuable for outpatient management of serious gram-positive infections that would otherwise require prolonged intravenous therapy.