Celecoxib: A COX-2 inhibitor for the treatment of osteoarthritis and rheumatoid arthritis
Celecoxib (Celebrex), a nonsteroidal anti-inflammatory drug (NSAID) indicated for use in osteoarthritis and rheumatoid arthritis, is the first specific cyclooxygenase-2 (COX-2) inhibitor approved by the FDA. By not inhibiting COX-l, celecoxib is expected to have fewer gastrointestinal (GI) and platelet effects. Celecoxib, which has a sulfonamide component to its chemical structure, is 99% absorbed over 1 to 3 hours, 97% protein bound, and extensively metabolized. It has a half-life of 11 hours under fasting conditions, which allows once- and twice-daily dosing (200 to 400 mg/day). Celecoxib is a substrate for CYP2C9 and inhibits CYP2D6; both of these features may lead to drug interactions. Celecoxib is as effective as other NSAIDs in the treatment of osteoarthritis and rheumatoid arthritis and superior to placebo. It is associated with fewer adverse effects than other NSAIDs, although GI symptoms and headaches are still the most common. Celecoxib may be beneficial for patients at risk for GI ulcers.
Boyce, E. G.,
Breen, G. A.
Celecoxib: A COX-2 inhibitor for the treatment of osteoarthritis and rheumatoid arthritis.
Formulary, 34(5), 405–412.