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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 most common side effects include edema, abdominal pain, diarrhea, dyspepsia, flatulence, peripheral edema, accidental injury, dizziness, pharyngitis, rhinitis, sinusitis, upper respiratory tract infection, and rash. [1] It was approved for medical use in the United States in May 2018. [3]
Celebrex (and other brand names for celecoxib) was introduced in 1999 and rapidly became the most frequently prescribed new drug in the United States. By October 2000, its US sales exceeded 100 million prescriptions per year for $3 billion, and was still rising. Sales of Celebrex alone reached $3.1 billion in 2001.
The therapeutic recommended dosages were 12.5, 25, and 50 mg with an approximate bioavailability of 93%. [12] [13] [14] Rofecoxib crossed the placenta and blood–brain barrier, [12] [13] [15] and took 1–3 hours to reach peak plasma concentration with an effective half-life (based on steady-state levels) around 17 hours.
COX-2 selective inhibitors have fewer gastrointestinal side effects, but promote thrombosis, and some of these agents substantially increase the risk of heart attack. As a result, certain COX-2 selective inhibitors—such as rofecoxib —are no longer used due to the high risk of undiagnosed vascular disease . [ 11 ]
The impetus for development of selective COX-2 inhibitors was the adverse gastrointestinal side-effects of NSAIDs.Soon after the discovery of the mechanism of action of NSAIDs, strong indications emerged for alternative forms of COX, but little supporting evidence was found.