Cyclooxygenase-2 inhibitor

Cyclooxygenase-2 inhibitors (COX-2 inhibitors), also known as 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.[1]

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 (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.[2]

Paracetamol (acetaminophen) inhibits COX-2 almost exclusively within the brain and only minimally in the rest of the body, although it is not considered an NSAID, since it has only minor anti-inflammatory activity.[3][4]

  1. ^ Lipfert P, Seitz R, Arndt JO (February 1987). "Studies of local anesthetic action on natural spike activity in the aortic nerve of cats". Anesthesiology. 66 (2). Ovid Technologies (Wolters Kluwer Health): 210–213. doi:10.1097/00000542-198702000-00016. PMID 3813081. Non-steroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs).
  2. ^ "Public data from Article 57 database". European Medicines Agency. 17 September 2018. Archived from the original on 2018-10-02. Retrieved 25 June 2021.
  3. ^ Hinz B, Cheremina O, Brune K (February 2008). "Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man". FASEB Journal. 22 (2): 383–90. doi:10.1096/fj.07-8506com. PMID 17884974. S2CID 9633350.
  4. ^ Page CP, Curtis MJ, Sutter M, Walker M, Hoffman B (1998). Farmacología integrada (in Spanish). Elsevier España. ISBN 84-8174-340-2 – via Google Books.