Linezolid: First of a New Drug Class for Gram-Positive Infections

In This Article

Abstract and Introduction

Linezolid is an oxazolidinone-type antibacterial agent which inhibits bacterial protein synthesis by specifically binding to the 50S ribosomal subunit. Linezolid is active against Gram-positive organisms and certain anaerobes, and has shown some bactericidal activity. Methicillin-resistant staphylococci, penicillin-resistant Streptococcus pneumoniae and vancomycin-resistant Enterococcus faecalis and E. faecium are susceptible to linezolid.

This agent is effective in patients with skin and soft tissue infections, community-acquired and nosocomial pneumonia, and bacteraemia, and has similar efficacy to that of other standard treatments. Resistance to linezolid has been reported in a small number of patients infected with E. faecium.

Linezolid is generally well tolerated and most events (mainly GI-related) are of mild to moderate intensity, resolve during continuous linezolid treatment and are not dose-related. Linezolid is an important new drug which is likely to be of use in the treatment of serious or complicated infections due to potentially resistant Gram-positive organisms.

The widespread emergence of multiply resistant Gram-positive organisms has prompted the development of new antimicrobial agents. The oxazolidinones are a new class of drug, first developed in the 1980s, with good activity against Gram-positive pathogens.[1]

Linezolid is the first member of this class to undergo intensive clinical investigation. Like other oxazolidinones, it inhibits bacterial protein synthesis in a unique manner, by specifically binding to the 50S ribosomal subunit. Because its mechanism of action differs from that of other antibacterials which also act by inhibiting protein synthesis, linezolid is not expected to show cross-resistance with existing antibacterial agents.[1,2,3]


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