oxazolidinones

Oxazolidinones are a class of synthetic antibiotics defined by a 2-oxazolidinone ring in their core structure. They inhibit bacterial protein synthesis by binding to the 50S ribosomal subunit and interfering with the formation of the initiation complex, thereby blocking translation. The activity is mainly against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE); Gram-negative activity is limited.

Clinically used members include linezolid and tedizolid. Linezolid is approved for complicated skin and soft tissue infections, and community- and hospital-acquired pneumonia. Tedizolid is approved for acute bacterial skin and skin structure infections and has once-daily dosing due to longer half-life. Both are available as IV or oral formulations with high oral bioavailability (linezolid ~100%).

Adverse effects include myelosuppression (especially with prolonged therapy, thrombocytopenia), peripheral and optic neuropathy, and serotonin syndrome risk when combined with serotonergic drugs due to MAOI-like effects of linezolid; there is potential for drug interactions. They can be bacteriostatic against many Gram-positive bacteria, and resistance can arise from mutations in the 23S rRNA or acquisition of the cfr methyltransferase gene.

History: Linezolid was the first oxazolidinone to reach clinical use, approved by the U.S. Food and Drug Administration in 2000. Tedizolid followed with approval in 2014 for ABSSSI. Ongoing research aims to expand indications, improve pharmacokinetic profiles, and address emerging resistance while monitoring safety in long courses.