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Oxazolidinones<br />

12<br />

Agent: linezolid<br />

Currently, linezolid is the only available member of<br />

the oxazolidinone class. Thanks to its broad Grampositive<br />

activity and excellent oral bioavailability,<br />

linezolid has become a useful (albeit expensive)<br />

antibiotic for the treatment of various resistant<br />

Gram-positive infections. Its advantage over other<br />

agents active against MRSA is its modern data<br />

supporting its use for MRSA pneumonia.<br />

Mechanism of Action<br />

Linezolid is a protein synthesis inhibitor that binds<br />

to the 50S ribosomal subunit, blocking the formation<br />

of a stable 70S initiation complex and preventing<br />

translation. This binding site is distinct from<br />

other protein synthesis inhibitors.<br />

Spectrum<br />

Good: MSSA, MRSA, streptococci (including<br />

multidrug-resistant S. pneumoniae), enterococci<br />

(including VRE), Nocardia<br />

Moderate: some atypicals, Mycobacterium<br />

tuberculosis<br />

Poor: all Gram-negatives, anaerobes

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