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Analgesics for Osteoarthritis—An Update

Slide: 5 of 32

Background: Nonsteroidal Anti-inflammatory Drugs

NSAIDs work by blocking cyclooxygenase (COX) enzymes, particularly COX-1 and COX-2. COX-1 mediates the mucosal protection of the gastrointestinal (GI) mucosa. COX-2 mediates effects on pain and inflammation.

By blocking COX-2 enzymes, NSAIDs decrease pain and inflammation. Nonselective NSAIDs block both COX-1 and COX-2 enzymes. NSAIDs that block COX-1 can cause GI adverse effects, including bleeding.

Selective or partially selective (in vitro) NSAIDs block mostly COX-2, and thus should be safer with regard to GI adverse effects. However, it is unclear if partially selective NSAIDs are truly different from nonselective NSAIDs because COX-2 selectivity may be lost at higher doses. The effects of in vitro COX-2 selectivity on clinical outcomes is uncertain.

All NSAIDs can also cause cardiovascular adverse effects.