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Celecoxib, sold under the brand name Celebrex among others, is a COX-2 inhibitor and nonsteroidal anti-inflammatory drug (NSAID). [7] It is used to treat the pain and inflammation in osteoarthritis, acute pain in adults, rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, painful menstruation, and juvenile rheumatoid arthritis. [7]
The COX-2 enzyme was discovered in 1988 by Daniel Simmons, a Brigham Young University researcher. [30] The mouse COX-2 gene was cloned by UCLA scientist Harvey Herschman, a finding published in 1991. [31] The basic research leading to the discovery of COX-2 inhibitors has been the subject of at least two lawsuits.
Common side effects include abdominal pain, dizziness, swelling, headache, and a rash. [11] Serious side effects may include heart disease, stroke, kidney problems, and stomach ulcers. [11] Use is not recommended in the third trimester of pregnancy. [11] It blocks cyclooxygenase-2 (COX-2) more than it blocks cyclooxygenase-1 (COX-1). [11]
The selectivity of COX-2 does not seem to negate other side-effects of NSAIDs, most notably an increased risk of kidney failure, and there is evidence that indicates an increase in the risk of heart attack, thrombosis, and stroke through an increase of thromboxane unbalanced by prostacyclin (which is reduced by COX-2 inhibition). [8]
Since PTGS2 (COX-2) is generally expressed only in cells where prostaglandins are upregulated (e.g., during inflammation), drug-candidates that selectively inhibit PTGS2 (COX-2) were suspected to show fewer side-effects [24] but proved to substantially increase risk for cardiovascular events such as heart attack and stroke. Two different ...
Rofecoxib is a selective COX-2 inhibitor, or "coxib". Though the class of coxibs includes several agents, degrees of COX-2 selectivity vary among them, with celecoxib (Celebrex) being the least COX-2 selective, and rofecoxib (Vioxx), valdecoxib (Bextra), and etoricoxib (Arcoxia), being highly COX-2 selective. [10]
COX-2 is an enzyme facultatively expressed in inflammation, and it is inhibition of COX-2 that produces the desirable effects of NSAIDs. [125] When nonselective COX-1/COX-2 inhibitors (such as aspirin, ibuprofen, and naproxen) lower stomach prostaglandin levels, ulcers of the stomach or duodenum and internal bleeding can result. [126]
Ketorolac is a non-selective COX inhibitor. [26] It is considered a first-generation NSAID, [15]: 279 a group of drugs that non-selectively inhibit both COX-1 and COX-2 enzymes, which can lead to gastrointestinal side effects. [27]