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Concept
COX-2 inhibitor
Summary
COX-2 inhibitors (coxibs) are a type of nonsteroidal anti-inflammatory drug (NSAID) that directly target cyclooxygenase-2, COX-2, an enzyme responsible for inflammation and pain. Targeting selectivity for COX-2 reduces the risk of peptic ulceration and is the main feature of celecoxib, rofecoxib, and other members of this drug class.
After several COX-2-inhibiting drugs were approved for marketing, data from clinical trials revealed that COX-2 inhibitors caused a significant increase in heart attacks and strokes, with some drugs in the class having worse risks than others. Rofecoxib (sold under the brand name Vioxx) was taken off the market in 2004 because of these concerns, while celecoxib (sold under the brand name Celebrex) and traditional NSAIDs received boxed warnings on their labels. Many COX-2-specific inhibitors have been removed from the US market. As of December 2011, only Celebrex (generic name of celecoxib) is still available for purchase in the United States. In the European Union, celecoxib, parecoxib and etoricoxib have been approved for use by the European Medicines Agency.
Paracetamol (acetaminophen) is also a COX-2 inhibitor almost exclusively within the brain, and only minimally in the rest of the body although its not considered an NSAID since it has only minor anti-inflammatory activity.
Some COX-2 inhibitors are used in a single dose to treat pain after surgery. In this role Etoricoxib appears as good as, if not better than, other pain medications and Celecoxib appears to be about as useful as ibuprofen.
NSAIDs are often used in treatment of acute gout attacks. COX-2 inhibitors appear to work as well as nonselective NSAIDS, such as Aspirin. They have not been compared to other treatment options such as colchicine or glucocorticoids.
COX-2 appears to be related to cancers and abnormal growths in the intestinal tract. Overexpression of COX-2 produces excess prostaglandins which have been shown to increase the possibility of colorectal cancer. COX inhibitors have been shown to reduce the occurrence of cancers and pre-cancerous growths.
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