2717 Linezolid Linezolid is only found in individuals that have used or taken this drug. It is a synthetic antibiotic, the first of the oxazolidinone class, used for the treatment of infections caused by multi-resistant bacteria including streptococcus and methicillin-resistant Staphylococcus aureus (MRSA). Linezolid is a synthetic antibacterial agent of the oxazolidinone class of antibiotics. It has in vitro activity against aerobic Gram positive bacteria, certain Gram negative bacteria and anaerobic microorganisms. It selectively inhibits bacterial protein synthesis through binding to sites on the bacterial ribosome and prevents the formation of a functional 70S-initiation complex. Specifically, linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is an essential component of the bacterial translation process. The results of time-kill studies have shown linezolid to be bacteriostatic against enterococci and staphylococci. For streptococci, linezolid was found to be bactericidal for the majority of strains. Linezolid is also a reversible, nonselective inhibitor of monoamine oxidase. Therefore, linezolid has the potential for interaction with adrenergic and serotonergic agents. 165800-03-3 441401 C16H20FN3O4 337.143780 Whitish crystalline powder (MSDS, A308). 182°C 3 mg/mL Inhalation (MSDS). Linezolid is rapidly and extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%. Linezolid targets the large 39S subunit of the mitochondrial ribosome thereby deactivation mitochondrial protein synthesis. As a result Linezolid is cytotoxic to the most metabolically active cells or tissues including the heart, liver, thymus and bone-marrow. (A7823). The likely target of Linezolid is the 16S rRNA molecule in the mitochondrial ribosome, which is analogous to the 23S rRNA in bacterial ribosomes. Linezolid is rapidly and extensively absorbed after oral dosing. Maximum plasma concentrations are reached approximately 1 to 2 hours after dosing, and the absolute bioavailability is approximately 100%. Linezolid is primarily metabolized by oxidation of the morpholine ring, which results in two inactive ring-opened carboxylic acid metabolites: the aminoethoxyacetic acid metabolite (A), and the hydroxyethyl glycine metabolite (A308). Half Life: 4.5-5.5 hours. No indication of carcinogenicity to humans (not listed by IARC). For the treatment of bacterial infections caused by susceptible strains of vancomycin resistant <i>Enterococcus faecium</i>, <i>Staphylococcal aureus</i> (methicillin resistant and susceptible strains), <i>Streptococcus pneumoniae</i>, <i>Streptococcus pyogenes</i>, <i>Streptococcus agalactiae</i> (A308). Common adverse effects of short-term use include headache, diarrhea, and nausea. Long-term use, however, has been associated with serious adverse effects; linezolid can cause 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. Clinical signs of acute toxicity lead to decreased activity, ataxia, vomiting and tremors. Drug therapy is discontinued immediately; exchange transfusion may be required to remove the drug. Sometimes, phenobarbital (UGT induction) is used. 2009-07-15T20:47:03Z 2014-12-24T20:25:49Z Monoamine oxidase type A (MAO-A) (P21397). http://en.wikipedia.org/wiki/Linezolid C08146 63607 Linezolid DB00601 ZLD true Monoamine oxidase type A (P21397) (A308) CC(=O)NC[C@H]1CN(C(=O)O1)C1=CC(F)=C(C=C1)N1CCOCC1 C16H20FN3O4 InChI=1S/C16H20FN3O4/c1-11(21)18-9-13-10-20(16(22)24-13)12-2-3-15(14(17)8-12)19-4-6-23-7-5-19/h2-3,8,13H,4-7,9-10H2,1H3,(H,18,21)/t13-/m0/s1 InChIKey=TYZROVQLWOKYKF-ZDUSSCGKSA-N 337.3461 337.143784348 Exogenous Solid 0.9 HMDB14739 CHEMBL126 390139 <p><a href="http://www.drugsyn.org/Linezolid.htm">DrugSyn.org</a></p>