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Linezolid

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Pharmacology

Summary

Linezolid is an antibiotic known for its activity against serious infections caused by gram-positive organisms, specifically by Staphylococci, Streptococci, and Enterococci. It hinders bacterial protein synthesis by binding to the 50S ribosomal subunit, which effectively prevents protein synthesis and therefore, bacterial growth.

Linezolid is effective against a number of serious infections, notably nosocomial pneumonia and complicated skin and soft tissue infections due to Methicillin-resistant Staphylococcus aureus (MRSA) and Vancomycin-resistant Enterococcus (VRE).

The primary toxicity associated with linezolid, however, is hematologic, with thrombocytopenia as the most common manifestation, followed by anemia and neutropenia. Other adverse effects include optic neuropathy and peripheral neuropathy. Additionally, linezolid is a weak inhibitor of monoamine oxidase and can precipitate serotonin syndrome; it should be used with caution in patients taking serotonergic agents (e.g. SSRIs, SNRIs, MAO inhibitors, or bupropion.)

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FAQs

What is linezolid and what is its mode of action?

Linezolid is an antibiotic that is active against gram-positive bacteria, including MRSA and VRE. It works by binding to the bacterial 50S ribosomal subunit and prevents the formation of the initiation complex, which then disrupts protein synthesis and hinders bacterial growth. Linezolid is bacteriostatic, meaning that it inhibits the growth of bacteria rather than killing them directly.

What types of infections can linezolid be used to treat?

Linezolid has broad activity against a variety of gram-positive bacteria that cause a range of infections. It is frequently used to treat infections caused by methicillin-resistant Staphylococcus aureus (MRSA), including hospital-acquired pneumonia. Furthermore, it's effective against vancomycin-resistant Enterococcus (VRE), and can be used in the treatment of other nosocomial infections.

How effective is linezolid in combating strains of bacteria resistant to other antibiotics?

Linezolid shows good activity against certain bacterial strains that are resistant to other antibiotics. Notably, it has effectiveness against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). This makes it an important option in the treatment of serious infections where other antibiotics may be ineffective.

What are some potential side effects associated with the use of linezolid?

While Linezolid is often well-tolerated, side effects can occur. Most notably, it has been associated with thrombocytopenia, or a decrease in platelets, which can increase the risk of bleeding. Other side effects include optic neuropathy, which can affect vision, and stocking-glove peripheral neuropathy, which can cause weakness, numbness, or pain in the hands and/or feet. It can also cause serotonin syndrome, a potentially serious condition resulting from excessive levels of serotonin in the brain.