From the Guidelines
Linezolid is an oxazolidinone antibiotic that inhibits bacterial protein synthesis by preventing the fusion of 30S and 50S ribosomal subunits 1.
Key Characteristics of Linezolid
- It is used to treat various infections, including skin and soft tissue infections, methicillin-resistant Staphylococcus aureus (MRSA) infections, and drug-resistant tuberculosis 1.
- Linezolid has been shown to be effective against MRSA, with a significantly better clinical and microbiological cure rate compared to vancomycin in some studies 1.
- The recommended dose of linezolid varies depending on the infection being treated, with a common dose being 600 mg daily 1.
- Linezolid can cause adverse events, including peripheral neuropathy, optic neuritis, anemia, and leukopenia, particularly with long-term use 1.
- It is generally not recommended to administer linezolid to patients taking serotonergic agents, such as monoamine oxidase inhibitors, due to the potential for serious CNS reactions 1.
Clinical Use of Linezolid
- Linezolid is used as an alternative to vancomycin for the treatment of complicated skin and soft tissue infections (cSSTIs) caused by MRSA 1.
- It has been shown to be effective in the treatment of cSSTIs, with a shorter length of stay and duration of intravenous therapy compared to vancomycin 1.
- Linezolid is also used in the treatment of drug-resistant tuberculosis, often in combination with other antibiotics 1.
From the FDA Drug Label
Linezolid is a synthetic antibacterial agent of a new class of antibiotics, the oxazolidinones, which has clinical utility in the treatment of infections caused by aerobic Gram-positive bacteria. Linezolid inhibits bacterial protein synthesis through a mechanism of action different from that of other antibacterial agents; therefore, cross-resistance between linezolid and other classes of antibiotics is unlikely Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process.
Linezolid is a synthetic antibacterial agent that belongs to the class of oxazolidinones. It is used to treat infections caused by aerobic Gram-positive bacteria. Its mechanism of action involves inhibiting bacterial protein synthesis, which is different from other antibacterial agents, making cross-resistance unlikely. 2
From the Research
Definition and Classification of Linezolid
- Linezolid is the first of an entirely new class of antibiotics, the oxazolidinones, in decades 3.
- It is a synthetic antibiotic that inhibits bacterial protein synthesis through binding to rRNA 4.
- Linezolid has a unique mechanism of action, making cross-resistance with other antimicrobial agents unlikely 3, 5.
Spectrum of Activity
- Linezolid has a spectrum of activity against virtually all important Gram-positive pathogens 3.
- It is active against many gram-positive organisms, including vancomycin-resistant Enterococcus faecium, methicillin-resistant Staphylococcus aureus, and penicillin-resistant Streptococcus pneumoniae 6, 7.
- Linezolid also has activity against some anaerobes, such as Clostridium spp., Peptostreptococcus spp., and Prevotella spp. 5.
Pharmacokinetics and Formulations
- Linezolid has both intravenous and oral formulations, with the latter being 100% bioavailable 3.
- It has good pharmacokinetics, with equal bioavailability by both oral and intravenous routes and no need for dose adjustment in patients with renal impairment 7.
Clinical Uses
- Linezolid has been approved for the treatment of infections caused by vancomycin-resistant Enterococcus faecium, hospital-acquired pneumonia caused by Staphylococcus aureus, complicated skin and skin structure infections, and community-acquired pneumonia caused by Streptococcus pneumoniae 4.
- It is also used to treat uncomplicated skin and skin structure infections caused by methicillin-susceptible S. aureus or Streptococcus pyogenes 4.