Linezolid

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Information about Linezolid[edit source]

Linezolid is a relatively new and distinctive antibiotic, a single member of an oxazolidinone class, that is used for serious or problematic infections caused by resistant enterococcal or staphylococcal organisms.


Liver safety of Linezolid[edit source]

Prolonged therapy with linezolid has been linked to rare instances of lactic acidosis and liver injury probably as a result of hepatic mitochondrial toxicity.

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Mechanism of action of Linezolid[edit source]

Linezolid (lin ayz' oh lid) is a synthetic antibiotic that belongs to the oxazolidinone class. It has broad bacteriocidal activity against gram positive organisms such as enterococci and staphylococci and most streptococci. It also has moderate activity against Mycobacterium tuberculosis. Linezolid acts by blocking bacterial protein synthesis, probably as a result of blocking the formation of the functional ribosomal 70S subunit.

FDA approval information for Linezolid[edit source]

Linezolid was approved for use in the United States in 2000 and is currently indicated for treatment of vancomycin-resistant enterococcal infections, for nosocomial pneumonia due to staphylococci (either methicillin-sensitive or -resistant) and skin and tissue infections caused by Staphylococcus aureus or pyogenes. Because of its activity against multidrug resistant enterococci and staphylococci, the use of linezolid is usually reserved for severe infections where methicillin or penicillin resistance is found. Linezolid is available in tablets of 400 and 600 mg under the name Zyvox. It is also available as an oral suspension and a solution for intravenous administration. Linezolid is typically given as a 7 to 14 day course of 400 or 600 mg twice daily. Longer courses are sometimes used for persistent infections.

Side effects of Linezolid[edit source]

Common minor side effects include nausea, diarrhea, abdominal upset, headache and skin rash. Rare, but severe side effects include serotonin syndrome, thrombocytopenia, optic and peripheral neuropathy, pancreatitis and lactic acidosis.

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Contributors: Prab R. Tumpati, MD