Meloxicam metabolism

Meloxicam reaches peak plasma concentrations about 8 h after oral dosing. More than 99.5% binds to plasma proteins and it has an elimination half-life of 20 h. Meloxicam is metabolized to four inactive metabolites and excreted in the urine and faeces. 

Blot L, Marcelis A, Devogelaer JP, Manicourt DH. Effects of diclofenac, aceclofenac and meloxicam on the metabolism of proteoglycans and hyaluronan in osteoarthritic human cartilage. Br J Pharmacol. 2000 131 1413-1421. 

Meloxicam, a COX-2 inhibitor, has been marketed in some countries and promoted as having an improved safety profile over current NSAIDs. It has a long half-life, is highly protein-bound, is metabolized to inactive compounds, and is excreted in the urine and feces. 

Obach RS, Kalgutkar AS, Ryder TF, Walker GS. In vitro metabolism and covalent binding of enol-carboxamide derivatives and anti-inflammatory agents sudoxicam and meloxicam Insights into the hepatotoxicity of sudoxicam. Chem Res Toxicol. 2008 21(9) 1890-1899. 

Meloxicam is metabolized in the liver via P450 enzymes and converted into four inactive metabolites [1,3] The mean of meloxicam is 15 to 20 hours. Most of meloxicam is excreted in the form of metabolites very little of the drug is excreted in its unchanged form. Near equal parts of meloxicam s metabolites are excreted in both the urine and feces. Significant biliary and enteral secretion has been demonstrated [1]. 

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