Oxazolidinones are a relatively new class of synthetic antibiotics. The best-known drug currently in clinical use is linezolid. Promising drug candidates are in development. All oxazolidinones share a core structure consisting of five-membered heterocyclic rings.
Oxazolidinones interfere with bacterial protein synthesis. They bind to the 23S ribosomal RNA of the 50S bacterial ribosome subunit. This prevents the formation of the initiation complex, a structure essential for bacterial protein biosynthesis. Linezolid is considered a bacteriostatic antibiotic but may have a limited bactericidal effect against certain bacteria. Resistance mechanism include efflux pumps reducing the intracellular drug level and mutations at the binding site. Currently, resistances against linezolid are still rare.
Oxazolidinones are very active against gram-positive organisms, including many multi-drug resistant strains. They show excellent activity against mycobacteria, and linezolid may be used for treatment of multi-drug resistant tuberculosis. It should be noted that clinical data are still scarce. Tedizolid is primarily used to treat acute skin infections.
Bioavailability, tissue and CSF penetration are excellent after oral administration. Linezolid and tedizolid are metabolised by the liver and excreted primarily by the kidneys (linezolid) or via faeces (tedizolid).
Known adverse effects include vomiting, nausea, diarrhoea and reversible thrombocytopenia.