Celecoxib, a COX-2--specific inhibitor: the clinical data.
Celecoxib offers the unique therapeutic prospect of alleviating pain and inflammation without the untoward gastrointestinal, renal, and platelet effects associated with conventional nonsteroidal anti-inflammatory drugs. This is possible because celecoxib is a cyclooxygenase-2 (COX-2)-specific inhibiting agent that inhibits the conversion of arachidonic acid to the prostaglandins that mediate pain and inflammation while having no effect on the formation of the prostaglandins that mediate normal homeostasis in the gastrointestinal tract, kidneys, and platelets and that are formed under the control of cyclooxygenase-1 (COX-1). Double-blind clinical trials have demonstrated that celecoxib is as effective in ameliorating the signs and symptoms of osteoarthritis and rheumatoid arthritis as naproxen and as effective as aspirin in reducing pain following dental extraction. Controlled trials have also shown that the incidence of gastroduodenal ulcers and the combined incidence of gastroduodenal ulcers and erosions are significantly lower with celecoxib therapy than with naproxen therapy and are similar to those associated with placebo administration. In a study of platelet function, it was found that a single 650-mg dose of aspirin profoundly diminished platelet function, while therapeutic doses of celecoxib exhibited no such effect. Celecoxib has been shown to be well tolerated, with incidences of adverse events similar to placebo in most instances. In summary, evidence to date indicates that celecoxib is a safe and effective therapeutic modality for the management of arthritis and pain.
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Medical Affairs, G.D. Searle & Co, Skokie, Illinois, USA.
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects; D001792:Blood Platelets / Q000187:drug effects; D000068579:Celecoxib; D002986:Clinical Trials as Topic; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use*; D004064:Digestive System / Q000187:drug effects; D006801:Humans; D007527:Isoenzymes; D008565:Membrane Proteins; D011451:Prostaglandin-Endoperoxide Synthases; D011720:Pyrazoles; D013449:Sulfonamides / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use*
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D011720:Pyrazoles; D013449:Sulfonamides; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; D000068579:Celecoxib