COX-2 inhibitor

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COX-2 inhibitor

A drug class that relieves inflammation and pain by inhibiting the action of cyclooxygenase-2.

Prostanoids that mediate inflammation, pain, and fever are synthesized through the action of cyclooxygenase-2 (COX-2), an enzyme that is constitutively expressed in the brain but can be induced in other tissues by cytokines. In both osteoarthritis and rheumatoid arthritis, COX-2 inhibitors have been shown to be superior in pain relief to acetaminophen and placebo, and equivalent to nonselective nonsteroidal antiinflammatory drugs (NSAIDs) such as ibuprofen and naproxen. In rheumatoid arthritis, COX-2 inhibitors are not disease-modifying drugs. Because nonselective NSAIDs inhibit not only COX-2 but also inhibit COX-1, which plays a role in platelet aggregation and gastric mucosal protection, their use is associated with a higher risk of gastrointestinal bleeding than that of selective COX-2 inhibitors. Like NSAIDs, however, the selective agents can cause liver and kidney toxicity, fluid retention, and hypertension. One of them (rofecoxib) was withdrawn by the manufacturer after 5 years on the market because of an unacceptably high incidence of heart attack and thrombotic stroke in patients receiving it for 18 months or more. For these reasons and because they are more expensive than NSAIDs, COX-2 inhibitors are indicated chiefly in patients who are at increased risk of gastrointestinal bleeding.

COX-2 inhibitor

n.
Any of a class of nonsteroidal anti-inflammatory drugs that selectively block prostaglandin formation so as to cause minimal gastrointestinal side effects.

COX-2 inhibitor

Cyclooxygenase-2 inhibitor Pain management A class of analgesics with fewer side effects than those of conventional NSAIDs–which inhibit both cyclooxygenases–COX-1 and COX-2; COX-1 protects the gastric mucosa, preventing ulcers, bleeding, and other digestive tract problems. See COX-2, Prostaglandin.

COX-2 in·hib·i·tor

(in-hibi-tŏr)
A drug class that relieves inflammation and pain by inhibiting the action of cyclooxygenase-2.
References in periodicals archive ?
26) The Coxib and Traditional NSAID Trialists' (CNT) Collaboration identified 639 randomized trials of an NSAID vs placebo or 1 NSAID regimen vs another for analysis.
The real advance, therefore, is natural or herbal coxibs --wonder medicines, derived from nature--which have proved their worth for thousands of years, not to speak of availability and ease of use.
Other drugs in the coxib class include cerecoxib, sold by Pfizer under the brand name Celebrex, and etoricoxib, sold by Merck under the brand name Arcoxia.
This study compared nsNSAIDs as the reference treatment with coxibs and opioids in 12,840 Medicare patients with osteoarthritis or rheumatoid arthritis (4,280 for each drug category).
Based on increasing reports of thrombotic events associated with rofecoxib, celecoxib, and valdecoxib, the Food and Drug Administration (FDA) issued a health advisory on December 23, 2004, concerning the use of all COXIBs.
Am J Gastroenterol 2008;103:221-227) Low GI risk High GI risk * Low CV Non-selective Non-selective risk NSAID NSAID + PPI or coxib as monotherapy High Aspirin + Avoid all CV naproxen + PPI NSAIDs risk# GI=gastrointestinal, CV=cardiovascular, NSAID=non-steroidal anti-inflammatory drug, coxib=selective cyclo-oxygenase-2 inhibitor, PPI=proton pump inhibitor.
Data Source: A propensity score-matched cohort analysis involving 12,840 elderly patients taking opioids, NSAIDs, or coxibs for rheumatoid arthritis or osteoarthritis pain.
This explains, in part, the increased cardiovascular mortality due to ovcrutilization of coxibs such as rofecoxib/Vioxx, withdrawn from the US market in 2005 by the US FDA due to its causal role in increasing cardiovascular deaths.
The two coxibs each linked with about an 80% increased risk.
Bandolier Extra 2004 Evidence-based Healthcare NSAIDs, coxibs, smoking and bone Available from: www.