The "aspirin" of the new millennium: cyclooxygenase-2 inhibitors.
Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit prostaglandin synthesis via the cyclooxygenase (COX) enzyme, the key to both therapeutic benefits and toxicity. COX enzyme exists in 2 isoforms, COX-1 and COX-2. COX-1 enzyme is thought to mediate "housekeeping" or homeostatic functions, and COX-2 is considered an inducible enzyme in response to injury or inflammation. COX-2 inhibitors are the "next-generation" NSAIDs that may selectively block the COX-2 isoenzyme without affecting COX-1 function. This may result in control of pain and inflammation with a lower rate of adverse effects compared with older nonselective NSAIDs. Rapidly evolving evidence suggests that COX-2 enzyme has a diverse physiologic and pathologic role. This article addresses the role of COX-2 enzyme in health and disease as well as the potential therapeutic value and safety issues related to COX-2 inhibition.
Buttar
N S
NS
Division of Gastroenterology and Hepatology and Internal Medicine, Mayo Clinic, Rochester, Minn. 55905, USA.
Wang
K K
KK
D000700:Analgesics / Q000627:therapeutic use; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000627:therapeutic use*; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000627:therapeutic use*; D006706:Homeostasis / Q000502:physiology; D006801:Humans; D007249:Inflammation / Q000517:prevention & control; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000502:physiology; D008565:Membrane Proteins; D010146:Pain / Q000517:prevention & control; D010544:Peroxidases / Q000037:antagonists & inhibitors*; D011451:Prostaglandin-Endoperoxide Synthases / Q000502:physiology
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D008565:Membrane Proteins; D010544:Peroxidases; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; C496511:PTGS1 protein, human; C496540:PTGS2 protein, human; D011451:Prostaglandin-Endoperoxide Synthases