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 One of them (rofecoxib) was withdrawn by the manufacturer after 5 years on the market because of an unacceptably high incidence of heart attack and thrombotic stroke in patients receiving it for 18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.

Farlex Partner Medical Dictionary © Farlex 2012

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.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.

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.
McGraw-Hill Concise Dictionary of Modern Medicine. © 2002 by The McGraw-Hill Companies, Inc.

COX-2 in·hib·i·tor

(in-hibi-tŏr)
A drug class that relieves inflammation and pain by inhibiting the action of cyclooxygenase-2.
Medical Dictionary for the Dental Professions © Farlex 2012
References in periodicals archive ?
While specific inhibition of COX-2 with celecoxib alone was sufficient to cause increased utilization of arachidonate by the lipoxygenase pathway, increases of LTB4 production were even greater in the presence of indomethacin, suggesting that the inhibition of both COX-1 and COX-2 provided more arachidonate substrate for metabolism by the lipoxygenase pathway.
pilosa, was studied using mouse skin and in vitro cell lines, and found to markedly suppress several of these cytokines, with significant inhibition of COX-2 expression.
The pharmacology of selective inhibition of COX-2. Thromb Haemost 2006; 96:391-392.
International contributors to eight chapters present findings from preclinical and clinical studies: e.g., evidence that inhibition of COX-2 can reduce damage to normal tissues in conventional lung cancer therapy; treatment of mantle cell lymphoma ands central nervous system lymphoma; nerve-sparing radical hysterectomy to preserve bladder function in invasive cervical cancer; and the use of nanoparticles in treating tumors.
Conversely, the COX-2 inhibitors display irreversible covalent binding to COX, which may partly explain the greater inhibition of COX-2 during intermittent use and at lower doses.
[Mechanism of inhibition OF COX-2 and COX-3 in gastrointestinal damage induced by NSAID in rats].
These newly recognized effects seem to result from activities beyond the drugs' inhibition of COX-2.
More importantly, inhibition of COX-2 activity using the COX-2 selective inhibitor, NS398 results in a dose-dependent attenuation of A[beta]-induced cell death (Fig.
One study favoring this interpretation showed that selective iv inhibition of COX-2 by valdecoxib increased gastric tonus in rats (52), suggesting that the abnormal gastric motility detected when indomethacin was administered by the parenteral route (50) may have been due to a predominant inhibition of COX-2.
Inhibition of COX-2 activity by celecoxib reverses the attenuation of vascular function [15, 16].
Previously we have also documented that UP446 consists primarily of baicalin from Scutellaria baicalensis and catechin from Acacia catechu to possess activities suggestive of benefit in OA including (i) dual inhibition of COX and LOX (Burnett et al., 2007), (ii) normalization of COX-2, tumor necrosis factor-a (TNF-a), IL-1[beta], IL-6, and nuclear factor-[beta]B (NFkB) gene expression in lipopolysaccharide- (LPS-) induced human and animal cell lines (Tseng-Crank et al., 2010), and (iii) inhibition of COX-2, 5-LOX, and inducible-nitric oxide synthase (iNOS) gene expression and moderation of NFkB binding activity in endotoxin-stimulated rat peritoneal macrophages (Altavilla et al., 2009).
Inhibition of COX-2 and PGE2 in LPS-stimulated RAW264.7 cells by lonimacranthoide VI, a chlorogenic acid ester saponin.

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