What is the mode of action of oxazolidinones?

The main action of oxazolidinones is by binding P site, inhibition of initiation complex and also translocation of peptidyl-tRNA from A site to P site (Fig. 1).

What is the mechanism of action of linezolid?

Linezolid disrupts bacterial growth by inhibiting the initiation process of protein synthesis—a mechanism of action that is unique to this class of drugs. It is well absorbed with high bioavailability that allows conversion to oral therapy as soon as the patient is clinically stable.

What do oxazolidinones do?

Oxazolidinones are primarily used for the treatment of antimicrobial-resistant gram-positive bacterial infections caused by methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant pneumococci. Linezolid is also used to treat multidrug-resistant Mycobacterium tuberculosis.

What is the target of oxazolidinones?

A novel class of antimicrobial agents, the oxazolidinones, target a wide spectrum of gram-positive and anaerobic bacteria (4, 6, 9, 28). These compounds act by inhibiting protein synthesis and have no effect on replication or transcription (8).

What is the mechanism of action of oxazolidinones?

Even though the binding sites overlap, the mechanism of action of oxazolidinones is different from all existing protein synthesis inhibitors. The main action of oxazolidinones is by binding P site, inhibition of initiation complex and also translocation of peptidyl-tRNA from A site to P site ( Fig. 1 ).

What kind of bacteria does oxazolidinone kill?

The rather unique mode of action of oxazolidones gives them excellent activity against Gram-positive pathogens including Staphylococcus aureus, Enterococcus spp, and Streptococcus pneumoniae – all of which have shown alarming rates of antibacterial resistance in clinical settings.

How are oxazolidinones different from tetracyclines and macrolides?

The oxazolidinones are a class of bacterial protein synthesis inhibitors, but their uniqueness lies in how early in the process they start inhibiting synthesis. While tetracyclines block aminoacyl tRNA entry and macrolides cause premature termination, oxazolidinones prevent the assembly of the ribosome.

When did the first oxazolidinones come out?

Oxazolidinones The first oxazolidinones developed by EI DuPont de Nemours & Co. Inc. in 1978, were synthesized because of their activity against certain plant pathogens. Nine years later, in 1987, two antibacterial oxazolidinones, DuP 721 and DuP 105, were synthesized as antibacterials against human pathogens [8].