Zyvox
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Zyvox
LinezolidSystematic (IUPAC) nameN-{-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamideIdentifiersCAS number165800-03-3ATC codeJ01XX08PubChem441401DrugBankAPRD01073ChemSpider390139Chemical dataFormulaC16H20FN3O4 Mol. mass337.346 g/molPharmacokinetic dataBioavailability~100% (oral)Protein bindingLow (31%)MetabolismHepatic (50–70%, CYP not involved)Half life4.2–5.4 hoursExcretionRenal (80–85%)Therapeutic considerationsLicence dataUS FDA:linkPregnancy cat.C (Au), C (U.S.)Legal statusS4 (Au), POM (UK), ℞-only (U.S.)RoutesIntravenous, oralLinezolid (INN) (pronounced /lɪˈnɛzəlɪd/) is a synthetic antibiotic of the oxazolidinone class used for the treatment of infections caused by multi-resistant bacteria including streptococci and methicillin-resistant Staphylococcus aureus (MRSA). It is marketed by Pfizer under the trade name Zyvox (in the United States and several other countries), Zyvoxam (in Canada and Mexico), or Zyvoxid (in Europe).Linezolid was the first commercially available oxazolidinone antibiotic. Therapy using linezolid can be quite expensive, with prices for a course of treatment ranging up to several thousands of dollars; nonetheless, it appears to be more cost-effective than vancomycin or teicoplanin.// HistoryThe oxazolidinone class was discovered by researchers at E.I. duPont de Nemours and reported in 1987. Early compounds were found to produce liver toxicity, however, and development was discontinued. Pharmacia & Upjohn (now part of Pfizer) started their own oxazolidinone research program in the 1990s, and two compounds were taken to Phase I clinical trials: linezolid and eperezolid. Linezolid was found to have better pharmacokinetic properties, and it proceeded to further trials; Food and Drug Administration (FDA) approval was granted on April 18, 2000. It is sold in the U.S. under the tradename Zyvox in either tablet form, oral suspension powder, or in an inactive medium for intravenous injection.Initially there was hope that bacteria would be unable to develop resistance to it. However, resistance was reported as early as 1999, in two patients with severe, multidrug-resistant Enterococcus faecium infection who received the drug through a compassionate use program. Linezolid-resistant Staphylococcus aureus was first isolated in 2001. Clinical useIt 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.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. Linezolid also provides some anaerobic coverage.In combination with other drugs, linezolid has been used to treat tuberculosis. The optimal dose for use in tuberculosis is not known. In adults, 600 mg daily or 600 mg twice daily have both been used to good effect. The treatment often needs to be continued for many months and the rate of adverse effects is high. The lower dose is not associated with a lower rate of adverse effects. Adverse effectsSide effects include diarrhea, headache, nausea, rashes, loss of appetite, constipation and fever. A small number of patients will incur a severe allergic reaction, or tinnitus, or pseudomembranous colitis. Thrombocytopenia is uncommon in patients who receive linezolid for 14 days or fewer (as recommended by the manufacturer), but in patients who receive longer courses, or who have renal failure, the rate is much higher. The anemia and thrombocytopenia caused by linezolid are not prevented by concurrent administration of pyridoxine 125 mg daily.Linezolid is toxic to mitochondria (probably because of the similarity between mitochondrial and bacterial ribosomes). Signs of mitochondrial toxicity include lactic acidosis and peripheral neuropathy. Painful sensory neuropathy. Mechanism of actionLinezolid works on the initiation of protein synthesis. (This is in contrast to most other protein synthesis inhibitors, which inhibit elongation.)It does this by stopping the 30S and 50S subunits of the ribosome from binding together. Linezolid binds on the 23S portion of the 50S subunit close to the peptidyl transferase and chloramphenicol binding sites. This then stops the interaction with the 30S subunit. ResistanceResistance to linezolid usually develops as the result of a point mutation known as G2576T, in which a guanine base is replaced with thymine in base pair 2576 of the genes coding for 23S ribosomal RNA. This is the most common mechanism of resistance in staphylococci, and the only one known to date in isolates of Enterococcus faecium.In the United States, resistance to linezolid has been monitored and tracked since 2004 through a program named LEADER, which (as of 2007) was conducted in 60 medical institutions throughout the country. Resistance has remained stable and extremely low (less than one-half of one percent of isolates). Some authors have predicted that resistance in E. faecium will increase if linezolid use continues at current levels or increases. InteractionsLinezolid is a weak monoamine oxidase inhibitor (MAOI), and should not be used concomitantly with other MAOIs, tyramine-containing foods, or pseudoephedrine; there have been postmarketing reports of serotonin syndrome when linezolid was given with serotonergic drugs.Linezolid may enhance the blood pressure-increasing effects of sympathomimetic drugs such as pseudoephedrine or phenylpropanolamine.
It works by interfering with the production of proteins needed by bacteria to grow..ZYVOX is used to treat different types of serious bacterial infections, such as pneumonia, skin infections, and infections that are resistant to other antibiotics.ZYVOX is an oxazolidinone
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Zyvox
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