It was the first commercially available oxazolidinone antibiotic and is usually reserved for the treatment of serious bacterial infections where older antibiotics have failed due to antibiotic resistance. Conditions such as skin infections or nosocomial pneumonia where methicillin or penicillin resistance is found are indicators for linezolid use. Compared to the older antibiotics it is quite expensive.

The drug works by inhibiting the initiation of bacterial protein synthesis; it is the only antibiotic to work in this manner. That and its synthetic nature raised hopes that bacteria would be unable to develop resistance to it and also remove the chance of cross-resistance. (However, in 1997 Staphylococcus aureus was first identified in Japan as being resistant to linezolid.) Linezolid is effective against gram-positive pathogens, notably Enterococcus faecium, Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pneumoniae, and Streptococcus pyogenes. It has almost no effect on gram-negative bacteria and is only bacteriostatic against most Enterococcus species.

The oxazolidinone class was discovered by researchers at E.I. duPont de Nemours and reported in 1987. Pharmacia Corporation developed linezolid and FDA approval was granted in April 2000. It is sold in the US under the tradename Zyvox in either tablet form, oral suspension powder, or in an inactive medium for intravenous injection.

Adverse effects

Side effects include rashes, loss of appetite, diarrhea, nausea, constipation and fever. A small number of patients will incur a severe allergic reaction, or tinnitis, or pseudomembranous colitis, or thrombocytopenia. Linezolid is a weak monoamine oxidase inhibitor (MAOI) and cannot be used with tyramine containing foods or pseudoephedrine.

Linezolid is toxic to mitochondria (probably because of the similarity of mitochondrial ribosomes to bacteria mitochondria). Signs of mitochondrial toxicity include lactic acidosis and peripheral neuropathy (Soriano et al., 2005).

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Will linezolid eradicate MRSA from surgical sites? Site infections are a major cause of surgical morbidity. The proportion of infections caused by methicillin-resistant Staphylococcus aureus (MRSA) has ... From American Family Physician, 10/1/05 by Anne D. Walling

Clinical efficacy of linezolid, clarithromycin and capreomycin in the treatment of multi-drug resistant pulmonary tuberculosis PURPOSE: Objective of the study was to see the clinical efficacy of a combination therapy with linezolid (L), azithromycin (AZ), capreomycin (CPM) and ... From CHEST, 10/1/05 by Sudhir K. Agarwal

Linezolid and vancomycin for methicillin-resistant Staphylococcus aureus nosocomial pneumonia: the subtleties of subgroup analyses To the Editor: Wunderink et al (November 2003) (1) claim that initial therapy with linezolid was associated with significantly better survival and ... From CHEST, 7/1/04 by John H. Powers

Unresolved questions with the use of linezolid vs vancomycin for nosocomial pneumonia To the Editor: We believe several issues must still be addressed in the study by Wunderink et al (November 2003) (1) published in CHEST. First, it ... From CHEST, 6/1/04 by Andre C. Kalil

Linezolid and quinupristin/dalfopristin: novel antibiotics for gram-positive infections of the skin Abstract With the continuing development of clinical drug resistance among bacteria, the need for new, effective agents to treat multi-drug-resistant ... From Journal of Drugs in Dermatology, 8/1/03 by Jeffrey M Weinberg

Linezolid is the first of a new class of antibiotics - Tips - oxazolidinone antibiotics In response to the emergence of resistant bacteria, efforts are being made to develop antimicrobial agents that are active against these resistant organisms. From American Family Physician, 7/1/03 by Richard Sadovsky

Linezolid in the treatment of complicated skin and soft tissue due to methicillin-resistant staphylococcus aureus This study is currently recruiting patients. Sponsored by Pfizer. This is a Phase IV randomized, multi-center, open-label trial to compare the clinical ... From Journal of Drugs in Dermatology, 9/1/05

Linezolid in the treatment of complicated skin and soft tissue due to methicillin-resistant staphylococcus aureus This study is currently recruiting patients. Sponsored by Pfizer. This is a Phase IV randomized, multi-center, open label trial to compare the clinical ... From Journal of Drugs in Dermatology, 5/1/05

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