Novel Insights and Therapeutical Applications in the Field of Inhibitors of COX-2

Author(s): W. Kiefer, G. Dannhardt

Journal Name: Current Medicinal Chemistry

Volume 11 , Issue 24 , 2004

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The discovery of the two isoenzymes COX-1 and COX-2 and the knowledge of their function, localisation and regulation has initiated the development of COX-2 selective inhibitors (coxibs). Inducible COX-2 at the peripheral site of inflammation has been detected in the early 1990s, the involvement of recently detected spinal COX-2 has led to new insights into mechanisms of pain and may explain analgesic and antipyretic properties of COX-2 selective inhibitors. The coxibs rofecoxib and celecoxib have been introduced into therapy and seem to offer some advantages over the classical non-selective NSAIDs. The search for new COX-2 inhibitors is going on, the development of etoricoxib and lumiracoxib is a step ahead concerning efficacy, tolerability and safety. Until today COX-2 selective inhibitors have found their place in therapy of arthritis, osteoarthritis, dysmenorrhea and acute pain. A new paradigm in pain therapy seems to justify their use in perioperative settings in a preemptive or multimodal therapeutical strategy. In the future COX-2 selective inhibitors as opioid sparing agents could become an important tool in pain therapy. Even a therapeutical benefit of COX-2 selective inhibitors in the treatment of Alzheimers Disease or in the prevention or treatment of colorectal or prostate cancer is presently intensely investigated. Recently some authors reported on COX-3, a splicing variant of COX-1. If COX-3 really represents the target for acetaminophen must be called into question.

Keywords: cox-1, cox-2, mechanism of pain, spinal cord cox-2, preemptive and multimodal analgesia, lox, coxinhibitors, cox-2 inhibitors in alzheimers disease and cancer

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Article Details

Year: 2004
Page: [3147 - 3161]
Pages: 15
DOI: 10.2174/0929867043363668
Price: $65

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