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KMID : 1037820140030020052
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Journal of Pain and Autonomic Disorders
2014 Volume.3 No. 2 p.52 ~ p.59
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Clinical Understanding of Coxibs
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Lee Dong-Kuck
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Abstract
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The cyclooxygenase (COX) inhibitors are the most common drugs used worldwide. COX, also known as prostaglandin endoperoxide synthase, is the key enzyme required for the conversion of arachidonic acid to prostaglandins. Two COX isoforms have been identified, COX-1 and COX-2. In many situations, the COX-1 enzyme is produced constitutively (e.g., in grastric mucosa), whereas COX-2 is highly inducidle(e.g., at sites of inflammation and cancer). And COX-1, which is largely associated with physiological functions, and COX-2, which is largely associated with pathological functions. Traditional non-steroidal anti-inflammatory drugs (NSAIDs) inhibit both enzymes, and a new class of COX-2 selective inhibitors(Coxibs) preferentially inhibit the COX-2 enzyme. Because of the pivotal role of COX in the inflammatory processes, NSAIDs that suppress COX activities have been used clinically for the treatment of inflammatory diseases/syndromes; however, traditional NSAIDs exhibit serious side effects such as gastrointestinal damage and hypersensitivity owing to their COX-1 inhibition. The COX-2 selective inhibition was designed to minimize gastrointestinal complications of non-selective inhibition However, this exclusive COX-2 inhibition associated with serious cardiovascular
events, for causing an imbalance between prostacyclin and thromboxane production.
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KEYWORD
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Cyclooxygenase, Cyclooxygenase-2, Coxibs
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