FDA-Approved for Treatment of Resistant Gram-Positive Bacterial Infections
Vancomycin-Resistant Enterococcus Faecium (VRE) (see Enterococcus Faecium, [[Enterococcus Faecium]])
Pharmacology
Oxazolidinone Antibiotic: first commercially available from this class
Mechanism: binds to bacterial 50S ribosomal subunit -> inhibition of bacterial protein synthesis
Bacteriostatic: against most organisms
Inhibits synthesis of Panton-Valentine Leukocidin (PVL), alpha-hemolysin, and toxic shock syndrome toxin-1
Impairment of Human Mitochondrial Function: linezolid is believed to interact with human mitochondrial 16S RNA, due to its resemblance to bacterial 23S rRNA
MAO Inhibitor Activity In Humans: MAO normally functions to degrades serotonin in the brain
FDA Alert (7/26/11): avoid use in conjunction with SSRI’s
Metabolism
xx
Administration
PO (Community-Acquired Pneumonia, Healthcare-Associated Pneumonia, Uncomplicated or Complicated Skin/Skin Structure Infections, VRE with or without Bacteremia): 600 mg q12 hrs
IV (Healthcare-Associated Pneumonia, Complicated Skin/Skin Structure Infections, VRE with or without Bacteremia): 600 mg q12 hrs
Dose Adjustment
Hepatic
Child-Pugh Class A or B: none
Child-Pugh Class C: use has not been evaluated
Renal: none
Adverse Effects
Gastrointestinal Adverse Effects
Altered Taste: occurs in 1.2% of cases
Diarrhea (see xxxx, [[xxxx]]): occurs in 4.3% of cases
Nausea (see xxxx, [[xxxx]]): occurs in 3.4% of cases
Hematologic Adverse Effects
Myelosuppression: risk is increased with renal failure, baseline cytopenias, and duration of therapy >14 days
Thrombocytopenia (see Thrombocytopenia, [[Thrombocytopenia]]): most frequently observed cytopenia with linezolid
Case reports describe reversal of thrombocytopenia with administration of pyridoxine
Neurologic Adverse Effects
Headache (see xxxx, [[xxxx]]): occurs in 2.2% of cases
Peripheral Neuropathy (see Peripheral Neuropathy, [[Peripheral Neuropathy]]): due to impairment of mitochondrial functio
Opthalmologic Adverse Effetcs
Optic Neuritis (see Optic Neuritis, [[Optic Neuritis]]): may be due to impairment of mitochondrial function or nutritional deficiency
Renal Adverse Effects
Lactic Acidosis (see Lactic Acidosis, [[Lactic Acidosis]]): due to impairment of mitochondrial function
