Linezolid
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| Pronunciation | /lɪˈnɛzəlɪd/ or /lɪˈneɪzəlɪd/, li-NEZ-ə-lid |
| Trade names | Zyvox, Zyvoxid, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a602004 |
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intravenous infusion, by mouth |
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| Pharmacokinetic data | |
| Bioavailability | ~100% (oral) |
| Protein binding | Low (31%) |
| Metabolism | liver (50–70%, not involved) |
| Biological half-life | 4.2–5.4 hours (shorter in children) |
| Excretion | non-kidney, kidney, and fecal |
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| ECHA InfoCard | 100.121.520 |
| Chemical and physical data | |
| Formula | C16H20FN3O4 |
| Molar mass | 337.346 g/mol |
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Linezolid is an antibiotic used for the treatment of infections caused by Gram-positive bacteria that are resistant to other antibiotics. Linezolid is active against most Gram-positive bacteria that cause disease, including , vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA). The main uses are infections of the skin and pneumonia although it may be used for a variety of other infections including drug resistant tuberculosis. It is used either by injection into a vein or by mouth. Linezolid is a member of the oxazolidinone class of medications.
When given for short periods, linezolid is a relatively safe antibiotic. It can be used in people of all ages and in people with liver disease or poor kidney function. Common side effects with short-term use include headache, diarrhea, rash, and nausea. Serious side effects may include serotonin syndrome, bone marrow suppression, and high blood lactate levels, particularly when used for more than two weeks. If used for longer periods still, it may cause sometimes irreversible nerve damage including optic nerve damage.
As a protein synthesis inhibitor, it affects the ability of bacteria to produce protein. This either stops growth or results in bacterial death. Although many antibiotics work this way, the exact mechanism of action of linezolid appears to be unique in that it blocks the start of protein production, rather than one of the later steps. As of 2014 bacterial resistance to linezolid has remained low.
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