Antimicrobials
Linezolid

Linezolid

Restricted

Low
Excellent (90 to 100%)
IV: $19.05/dose; PO: $1.77/dose

Spectrum of Activity

General Information

  • CBC

  • Visual testing for therapy >3 months or if symptoms develop on therapy

  • LFTs

  • Lactic acid in patients with renal dysfunction

  • Serotonin syndrome

  • Thrombocytopenia

  • Rash

  • Elevated liver enzymes

  • Lactic acidosis

  • Myelosuppression (usually with >2weeks therapy; reversible)

  • Peripheral/optic neuropathy with prolonged courses

  • Absorption: Rapid and extensive
  • Distribution: 0.65 L/kg
  • Protein Binding: Adults: 31%
  • Metabolism: 
    • Hepatic via oxidation of the morpholine ring, resulting in two inactive metabolites (aminoethoxyacetic acid, hydroxyethyl glycine)
    • Minimally metabolized, may be mediated by cytochrome P450
  • Bioavailability: Oral: ~100%.
  • Half-Life Elimination: 4.9 hours
  • Time to Peak: Oral: 1-2 hours
  • Excretion: 
    • Urine (30% of total dose as parent drug, ~50% of total dose as metabolites)
    • Two metabolites of linezolid may accumulate in patients with severe renal impairment
    • Feces (9% of total dose as metabolites)