Linezolid

Brand Names: ZYVOX

Drug Class: Oxazolidinone antibacterial

Overview

Linezolid is an oxazolidinone-class antibacterial agent used to treat serious Gram-positive bacterial infections. It works by inhibiting bacterial protein synthesis through binding to the 50S ribosomal subunit. It is effective against vancomycin-resistant Enterococcus faecium, hospital-acquired and community-acquired pneumonia, and complicated skin infections.

Mechanism of Action

Linezolid is a synthetic antibacterial agent of the oxazolidinone class that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit, preventing formation of the initiation complex in bacterial translation.

Indications

  • Vancomycin-resistant Enterococcus faecium infections
  • Nosocomial pneumonia caused by Staphylococcus aureus or Streptococcus pneumoniae
  • Complicated skin and skin structure infections caused by susceptible Gram-positive bacteria
  • Community-acquired pneumonia caused by susceptible Gram-positive bacteria

Common Doses

  • 600 mg tablet
  • 600 mg/300 mL injection
  • 100 mg/5 mL oral suspension

Dosage

Adults: 600 mg every 12 hours IV or orally. Duration varies by infection type: 10-14 days for pneumonia, 10-28 days for skin infections, 14-28 days for vancomycin-resistant Enterococcus infections. Pediatric dosing based on weight.

Contraindications

  • Known hypersensitivity to linezolid or any component of the formulation
  • Concurrent use or within 2 weeks of MAO inhibitors due to risk of serotonin syndrome
  • Uncontrolled hypertension, pheochromocytoma, thyrotoxicosis, carcinoid syndrome

Side Effects

  • Myelosuppression
  • Peripheral and optic neuropathy
  • Serotonin syndrome
  • Clostridioides difficile-associated diarrhea
  • Lactic acidosis
  • Convulsions
  • Rhabdomyolysis
  • Hypoglycemia
  • Hyponatremia and SIADH
  • Headache
  • Diarrhea
  • Nausea
  • Vomiting
  • Insomnia
  • Dizziness
  • Rash

Interactions

  • MAO inhibitors (contraindicated)
  • Serotonergic drugs (SSRIs, SNRIs, TCAs, triptans, opioids) - increased serotonin syndrome risk
  • Adrenergic agents (pressors, decongestants) - potential hypertensive crisis
  • Tyramine-rich foods - limited risk but caution advised

Counseling Points

  • Complete full course even if feeling better
  • Report vision changes, numbness, or tingling immediately
  • Avoid foods high in tyramine (aged cheeses, cured meats)
  • Inform all providers about linezolid use due to interaction risks
  • Monitor for diarrhea and report severe cases
  • Avoid MAO inhibitors and certain antidepressants
  • Regular blood tests required to monitor blood counts