Oxazolidinone antibiotics

Abstract

Many common gram-positive pathogens (eg, Staphylococcus aureus, Enterococcus spp, and Streptococcus pneumoniae) have become increasingly resistant to antimicrobial agents, and new drugs with activity against gram-positive bacteria are urgently needed. The oxazolidinones, a new chemical class of synthetic antimicrobial agent, have a unique mechanism of inhibiting bacterial protein synthesis. Linezolid, the first oxazolidinone to be approved for clinical use, displays in-vitro activity (generally bacteriostatic) against many important resistant pathogens, including meticillin-resistant Staph aureus, vancomycin-resistant enterococci, and penicillin-resistant Strep pneumoniae. Linezolid is a parenteral agent that also possesses near-complete oral bioavailability plus favourable pharmacokinetic and toxic effect profiles. Clinical trials confirm the activity of linezolid in the setting of pneumonia, skin and soft-tissue infections, and infections due to vancomycin-resistant enterococci. Linezolid shows promise as an alternative to glycopeptides and streptogramins to treat serious infections due to resistant gram-positive organisms. New agents with greater potency and new spectra of activity could arise from further modification of the oxazolidinone nucleus.