Linezolid is an oxazolidinone antibacterial agent that acts by inhibiting t
he initiation of bacterial protein synthesis, Cross-resistance between line
zolid and other inhibitors of protein synthesis has not been demonstrated.
Linezolid has a wide spectrum of activity against Gram-positive organisms i
ncluding methicillin-resistant staphylococci, penicillin-resistant pneumoco
cci ana vancomycin-resistant Enterococcus faecalis and E. faccium. Anerobes
such as Clostridium spp., Peptostreptococcus spp. and Prevotella spp. are
also susceptible to linezolid.
Linezolid is bacteriostatic against most susceptible organisms but displays
bactericidal activity against some strains of pneumococci, Bacteroides fra
gilis and C. perfringens.
In clinical trials involving hospitalised patients with skin/soft tissue in
fections (predominantly S. aureus), intravenous/oral linezolid (up to 1250m
g mddav) produced clinical success in >83% of individuals, In patients with
community-acquired pneumonia, success rates were >94%.
Preliminary clinical data also indicate that twice daily intravenous/oral l
inezolid 600mg is as effective as intravenous vancomycin ig in the treatmen
t of patients: with hospital-acquired pneumonia and in those with infection
s caused by methicillin-resistant staphylococci. Moreover, linezolid 600mg
twice daily produced >85% clinical/microbiological cure in vancomycin-resis
tant enterococcal infections.
Linezolid is generally well tolerated and gastrointestinal disturbances are
the most commonly occurring adverse events, No clinical evidence of advers
e reactions as a result of monoamine oxidase inhibition has been reported.