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linezolid : ウィキペディア英語版
linezolid


Linezolid is a antibiotic used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to other antibiotics. Linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant ''Staphylococcus aureus'' (MRSA). The main uses are infections of the skin and pneumonia although it may be use for a variety of other infections.

When administered for short periods, linezolid is a relatively safe. It can be used in people of all ages and in people with liver disease or poor kidney function. Common adverse effects of short-term use include headache, diarrhea, and nausea. Long-term use, however, has been associated with serious adverse effects such as bone marrow suppression and low platelet counts, particularly when used for more than two weeks. If used for longer periods still, it may cause sometimes irreversible chemotherapy-induced peripheral neuropathy and optic nerve damage, and lactic acidosis (a buildup of lactic acid in the body), all most likely due to mitochondrial toxicity.〔

As a protein synthesis inhibitor, it stops the growth of bacteria by disrupting their production of proteins, that is, it is a bacteriostatic agent, not bacteriocidal. Although many antibiotics work this way, the exact mechanism of action of linezolid appears to be unique in that it blocks the initiation of protein production, and not one of the later steps.〔 Bacterial resistance to linezolid has remained very low since it was first detected in 1999, although it may be increasing. It is a member of the oxazolidinone class of drugs.〔

Linezolid was discovered in the 1990s by a team at Pharmacia and Upjohn Company and first approved for use in 2000. It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system. Linezolid costs approximately US$100 per tablet in the United States.〔 Nonetheless, it appears to be more cost-effective than generic alternatives such as vancomycin, mostly because of the possibility of switching from intravenous to oral administration as soon as patients are stable enough, without the need for dose adjustments.
==Medical uses==
The main indication of linezolid is the treatment of severe infections caused by Gram-positive bacteria that are resistant to other antibiotics; it should not be used against bacteria that are sensitive to drugs with a narrower spectrum of activity, such as penicillins and cephalosporins. In both the popular press and the scientific literature, linezolid has been called a "reserve antibiotic"—one that should be used sparingly so that it will remain effective as a drug of last resort against potentially intractable infections.
In the United States, the indications for linezolid use approved by the U.S. Food and Drug Administration (FDA) are the treatment of vancomycin-resistant ''Enterococcus'' ''faecium'' infections, with or without bacterial invasion of the bloodstream; nosocomial pneumonia (hospital-acquired) and community-acquired pneumonia caused by ''S. aureus'' or ''S. pneumoniae''; complicated skin and skin structure infections (cSSSI) caused by susceptible bacteria, including diabetic foot infection, unless complicated by osteomyelitis (infection of the bone and bone marrow); and ''uncomplicated'' skin and soft tissue infections caused by ''S. pyogenes'' or ''S. aureus''.〔 The manufacturer advises against the use of linezolid for community-acquired pneumonia or ''uncomplicated'' skin and soft tissue infections caused by MRSA.〔 In the United Kingdom, pneumonia and cSSSIs are the only indications noted in the product labeling.
Linezolid appears to be as safe and effective for use in children and newborns as it is in adults.〔

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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