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 One of them (rofecoxib) was withdrawn by the manufacturer after 5 years on the market because of an unacceptably high incidence of heart attack and thrombotic stroke in patients receiving it for 18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 ?
No inhibition of COX-2 mRNA, COX-2 promoter activity, and NF-[kappa]B reporter activity by KRG-WE was observed when the sirtinol and EX527 were administrated (Fig.
Additionally, COX-2 is a strong pro-angiogenic factor in potentiating cancer metastasis (Gately and Li 2004), so we thought that inhibition of COX-2 and downstream signaling pathways were involved in the anti-angiogenesis effects mediated by DSS.
The beneficial actions of NSAIDs, to go back a bit in our narrative, are associated with the inhibition of COX-2, just as much as their adverse effects are related to the inhibition of COX-1.
These results revealed synergistic effect of guggulsterone and imatinib in inducing apoptosis in K562/IMA cells, by a mechanism involving the inhibition of COX-2 and down-regulation of P-glycoprotein expression.
Inhibition of COX-2 and activation of peroxisome proliferator-activated receptor gamma synergistically inhibits proliferation and induces apoptosis of human pancreatic carcinoma cells.
Moreover WVSM and PPG produced a dose dependent manner inhibition of COX-2 resulting in reduction in PGE2 production (Fig.
The anti-tumor and anti-metastatic actions of wogonin may be associated with the inhibition of VEGF-C-induced lymphangiogenesis through a reduction in VEGF-C-induced VEGFR-3 phosphorylation by the inhibition of COX-2 expression and IL-11.
COX-2 synthesis has also been shown to be dependent upon ERK 1/2 and p38 thus it is conceivable that the inhibition of these signaling molecules results in the inhibition of COX-2 expression and PGE2 synthesis.
2002; Wolfe and Liu 2008), with inhibition of COX-2 (Hou et al.
This iridoid has been found to exert a series of effects possibly connected with DC anti-inflammatory properties, including inhibition of COX-2, inhibition of NF-[kappa]B activation and down-regulation of iNOS (Kaszkin et al.
The results of the present study, therefore, would suggest that the inhibition of COX-2 maybe play a key role in the inhibition of [PGF.

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