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 One of them (rofecoxib) was withdrawn by the manufacturer after 5 years on the market because of an unacceptably high incidence of heart attack and thrombotic stroke in patients receiving it for 18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 ?
You may now want to quiz why inhibition of COX-2 enzyme is so important, and why it needs to be carefully cowed down and "put on hold.
The beneficial anti-inflammatory effect of the NSAIDs had been attributed to inhibition of COX-2, while the gastrointestinal (GI), renal and anti-platelet adverse effects were attributed to COX-1 inhibition (4).
The inhibitory effects of gammaT and gamma-CEHC stemmed from their inhibition of COX-2 activity, rather than affecting protein expression or substrate availability, and appeared to be independent of antioxidant activity.
49-55) However, although COX-2 is upregulated in inflammation, its activity is also upregulated in healing damaged tissue; thus, inhibition of COX-2 activity may delay healing in certain circumstances.
The similar risk of thrombotic events between etoricoxib and diclofenac can be explained by the profound inhibition of COX-2 shared by the two agents.
It is now recognized that the antiinflammatory and analgesic actions of nonsteroidal antiinflammatory drugs are largely attributable to inhibition of COX-2 isoenzyme.
Some researchers suggest that aspirin's inhibition of Cox-2 may explain why it seems to defend against colon cancer.
Methyl syringate inhibition of COX-2 protein expression under hypoxic conditions was significantly blocked by HC-030031 (Fig.
Growing evidence suggests that inhibition of COX-2 might have an important role in the delay of progression in established cancer, and COX-2 inhibitors may be considered as novel agents in addition to standard treatment, while the enzyme superoxide dismutase may inhibit metastasis promotion and suppress tumor growth.
The results of this observational study "suggest that the anticancer benefit of aspirin is mediated, at least in part, by inhibition of COX-2," Dr.

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