Pharmacodynamics alt=Diagram: A colored ribbon, representing messenger RNA (mRNA), passes through a cartoon diagram of an assembled ribosome. Cartoon representations of transfer RNA (tRNA) enter and exit the ribosome and occupy its A and P sites. A string of colored spheres, representing a newly formed protein, comes out of the top of the ribosome.<unk> , like other oxazolidinones, is a bacterial protein synthesis inhibitor and a weak, non-selective, reversible monoamine oxidase inhibitor. As a protein synthesis inhibitor,<unk>  stops the growth and reproduction of bacteria by disrupting translation of messenger RNA (mRNA) into proteins in bacterial ribosomes.<unk>  inhibits translation at the first step of protein synthesis, initiation, unlike most other protein synthesis inhibitors, which inhibit elongation. It does so by preventing the formation of the initiation complex, composed of the 30S and 50S subunits of the ribosome, tRNA, and mRNA.<unk>  binds to the 23S portion of the 50S subunit (the center of peptidyl transferase activity), close to the binding sites of chloramphenicol, lincomycin, and other antibiotics. Due to this unique mechanism of action, cross-resistance between<unk>  and other protein synthesis inhibitors is highly infrequent or nonexistent. In 2008, the crystal structure of<unk>  bound to the 50S subunit of a ribosome from the archaean Haloarcula marismortui was elucidated by a team of scientists from Yale University and deposited in the Protein Data Bank. Another team in 2008 determined the structure of<unk>  bound to a 50S subunit of Deinococcus radiodurans. The authors proposed a refined model for the mechanism of action of oxazolidinones, finding that<unk>  occupies the A site of the 50S ribosomal subunit, inducing a conformational change that prevents tRNA from entering the site and ultimately forcing tRNA to separate from the ribosome. Pharmacokinetics alt=Upper left: structural formula of the unaltered<unk>  molecule, with the morpholino group highlighted in red. Lower left: main carboxylic acid metabolite, accounting for 10% of an excreted dose; the morpholine ring has been cleaved at the nitrogen atom. Lower right: structural formulae of two distinct molecules, a carboxylic acid and a lactone, with an equilibrium arrow between them; this metabolite accounts for 45% of a dose. Upper right: structure of a minor carboxylic acid metabolite, which accounts for aroune 3.3% of a dose. One of the advantages of<unk>  is that it has an absolute oral bioavailability of 100% due to its rapid and complete absorption after oral administration; in other words, the entire dose reaches the bloodstream, as if it had been given intravenously. This means that people receiving intravenous<unk>  may be switched to oral<unk>  as soon as their condition allows it, whereas comparable antibiotics (such as vancomycin and quinupristin/dalfopristin) can only be given intravenously. Taking<unk>  with food somewhat slows its absorption, but the area under the curve is not affected.<unk> 's plasma protein binding is approximately 31% (range ) and its volume of distribution at steady state averages liters in healthy adult volunteers. Peak plasma concentrations (Cmax) are reached one to two hours after administration of the drug.<unk>  is readily distributed to all tissues in the body apart from bone matrix and white adipose tissue. Notably, the concentration of<unk>  in the epithelial lining fluid (ELF) of the lower respiratory tract is at least equal to, and often higher than, that achieved in serum (some authors have reported bronchial fluid concentrations up to four times higher than serum concentrations), which may account for its efficacy in treating pneumonia. However, a meta-analysis of clinical trials found that<unk>  was not superior to vancomycin, which achieves lower concentrations in the ELF. Cerebrospinal fluid (CSF) concentrations vary; peak CSF concentrations are lower than serum ones, due to slow diffusion across the blood–brain barrier, and trough concentrations in the CSF are higher for the same reason. The average half-life is three hours in children, four hours in teenagers, and five hours in adults.<unk>  is metabolized in the liver, by oxidation of the morpholine ring, without involvement of the cytochrome P450 system. This metabolic pathway leads to two major inactive metabolites (which each account for around 45% and 10% of an excreted dose at steady state), one minor metabolite, and several trace metabolites, none of which accounts for more than 1% of an excreted dose. Clearance of<unk>  varies with age and gender; it is fastest in children (which accounts for the shorter half-life), and appears to be 20% lower in women than in men. There is a strong correlation between<unk>  clearance and creatinine clearance.
Linezolid
Meropenem
Teicoplanin
Vancomycin
Resistin
Daptomycin
Ertapenem
Colistin