Linezolid
Linezolid is a synthetic antibiotic, the first of the
oxazolidinone class, used for the treatment of infections
caused by multi-resistant bacteria including streptococcus
and methicillin-resistant Staphylococcus aureus (MRSA).
The drug works by inhibiting the initiation of bacterial
protein synthesis.
PHARMACOLOGY
Indication
For the treatment of bacterial infections caused by
susceptible strains of vancomycin resistant Enterococcus
faecium, Staphylococcal aureus (methicillin resistant and
susceptible strains), Streptococcus
pneumoniae, Streptococcus pyogenes, Streptococcus
agalactiae.
Associated Conditions
Bacterial Infections
Community Acquired Pneumonia (CAP)
Complicated Skin and Skin Structure Infection
Nosocomial Pneumonia
Uncomplicated Skin and Skin Structure Infections
Pharmacodynamics
Linezolid is a synthetic antibacterial agent of a new class of
antibiotics, the oxazolidinones, which has clinical utility in
the treatment of infections caused by aerobic Gram-positive
, bacteria. The in vitro spectrum of activity of linezolid also
includes certain Gram-negative bacteria and anaerobic
bacteria. Susceptible organisms include methicillin- and
vancomycin-resistant staphylococci, vancomycin-resistant
enterococci, penicillin-resistant pneumococci and anaerobes.
Oxazolidinones inhibit protein synthesis by binding at the P
site at the ribosomal 50S subunit. Resistance to other protein
synthesis inhibitors does not affect oxazolidinone activity,
however rare development of oxazolidinone resistance
cases, associated with 23S rRNA alterations during
treatment have been reported. Linezolid inhibits bacterial
protein synthesis through a mechanism of action different
from that of other antibacterial agents; therefore, cross-
resistance between linezolid and other classes of antibiotics
is unlikely.
Mechanism of action
Linezolid is a synthetic antibacterial agent of the
oxazolidinone class of antibiotics. It has in vitro activity
against aerobic Gram-positive bacteria, certain Gram-
negative bacteria and anaerobic microorganisms. It
selectively inhibits bacterial protein synthesis through
binding to sites on the bacterial ribosome and prevents the
formation of a functional 70S-initiation complex.
Specifically, linezolid binds to a site on the bacterial 23S
ribosomal RNA of the 50S subunit and prevents the
formation of a functional 70S initiation complex, which is
an essential component of the bacterial translation process.
The results of time-kill studies have shown linezolid to be
bacteriostatic against enterococci and staphylococci. For
streptococci, linezolid was found to be bactericidal for the
majority of strains. Linezolid is also a reversible,
nonselective inhibitor of monoamine oxidase. Therefore,
Linezolid is a synthetic antibiotic, the first of the
oxazolidinone class, used for the treatment of infections
caused by multi-resistant bacteria including streptococcus
and methicillin-resistant Staphylococcus aureus (MRSA).
The drug works by inhibiting the initiation of bacterial
protein synthesis.
PHARMACOLOGY
Indication
For the treatment of bacterial infections caused by
susceptible strains of vancomycin resistant Enterococcus
faecium, Staphylococcal aureus (methicillin resistant and
susceptible strains), Streptococcus
pneumoniae, Streptococcus pyogenes, Streptococcus
agalactiae.
Associated Conditions
Bacterial Infections
Community Acquired Pneumonia (CAP)
Complicated Skin and Skin Structure Infection
Nosocomial Pneumonia
Uncomplicated Skin and Skin Structure Infections
Pharmacodynamics
Linezolid is a synthetic antibacterial agent of a new class of
antibiotics, the oxazolidinones, which has clinical utility in
the treatment of infections caused by aerobic Gram-positive
, bacteria. The in vitro spectrum of activity of linezolid also
includes certain Gram-negative bacteria and anaerobic
bacteria. Susceptible organisms include methicillin- and
vancomycin-resistant staphylococci, vancomycin-resistant
enterococci, penicillin-resistant pneumococci and anaerobes.
Oxazolidinones inhibit protein synthesis by binding at the P
site at the ribosomal 50S subunit. Resistance to other protein
synthesis inhibitors does not affect oxazolidinone activity,
however rare development of oxazolidinone resistance
cases, associated with 23S rRNA alterations during
treatment have been reported. Linezolid inhibits bacterial
protein synthesis through a mechanism of action different
from that of other antibacterial agents; therefore, cross-
resistance between linezolid and other classes of antibiotics
is unlikely.
Mechanism of action
Linezolid is a synthetic antibacterial agent of the
oxazolidinone class of antibiotics. It has in vitro activity
against aerobic Gram-positive bacteria, certain Gram-
negative bacteria and anaerobic microorganisms. It
selectively inhibits bacterial protein synthesis through
binding to sites on the bacterial ribosome and prevents the
formation of a functional 70S-initiation complex.
Specifically, linezolid binds to a site on the bacterial 23S
ribosomal RNA of the 50S subunit and prevents the
formation of a functional 70S initiation complex, which is
an essential component of the bacterial translation process.
The results of time-kill studies have shown linezolid to be
bacteriostatic against enterococci and staphylococci. For
streptococci, linezolid was found to be bactericidal for the
majority of strains. Linezolid is also a reversible,
nonselective inhibitor of monoamine oxidase. Therefore,
