Cyclooxygenase-2 inhibitors gastrointestinal effects

The major problem of NSAIDs is gastrointestinal (GI) irritation, leading to ulceration. Recent drugs such as celecoxib (a cyclooxygenase-II inhibitor) have a mild effect on the GI tract and have proven to be the drugs of choice for the treatment of rheumatoid arthritis. 

Pfizer) are selective cyclooxygenase type 2 (COX-2) inhibitors and are useful in the treatment of arthritis. The compounds exert their pharmacological effect by selectively blocking the COX-2 enzyme to produce an antiinflammatory effect without adverse gastrointestinal side effects. In addition, they also display analgesic and antipyretic activities in animal models. 

Simon LS, Lanza FL, Lipsky PE, Hubbard RC, Talwalker S, Schwartz BD, Isakson PC, Geis GS. Preliminary study of the safety and efficacy of SC-58635, a novel cyclooxygenase 2 inhibitor efficacy and safety in two placebo-controlled trials in osteoarthritis and rheumatoid arthritis, and studies of gastrointestinal and platelet effects. Arthritis Rheum 1998 41(9) 1591-602. 

Aspirin and the older nonselective NSAlDs inhibit both cyclooxygenase isoforms and thereby decrease prostaglandin and thromboxane synthesis throughout the body. Prostaglandins necessary for normal cell function are depleted, as well as prostaglandins involved in inflammation. Theoretically, the COX-2-selective inhibitors should have less effect upon the prostaglandins involved in normal cell function, particularly those in the gastrointestinal tract. 

Jarupongprapa S, Ussavasodhi P, Katchamart W. Comparison of gastrointestinal adverse effects between cyclooxygenase-2 inhibitors and non-selective, non-steroidal anti-inflammatory drugs plus proton pump inhibitors a systematic review and meta-analysis. J Gastroenterol July 2013 48(7) 830-8. 

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