Oxazolidinone antibiotics.
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.
Diekema
D J
DJ
Division of Infectious Diseases, Department of Internal Medicine, University of Iowa College of Medicine, Iowa City, Iowa 52242, USA. daniel-diekema@uiowa.edu
Jones
R N
RN
D000081:Acetamides / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D004352:Drug Resistance, Microbial; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy*; D006801:Humans; D000069349:Linezolid; D023303:Oxazolidinones / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D011500:Protein Synthesis Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use
D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D011500:Protein Synthesis Inhibitors; D000069349:Linezolid