Cox-2 inhibition non steroidal anti-inflammatory drugs

NSAIDs have anti-inflammatory (reduce inflammation), analgesic (relieve pain) and antipyretic (lower temperature) effects. Although different NSAIDs have different structures, they all work by blocking cyclooxygenase (COX) enzymes. There are two main types of COX enzymes: COX-1 and COX-2. Both types produce prostaglandins; however, the main function of COX-1 enzymes is to produce baseline levels of prostaglandins that activate platelets and protect the lining of the gastrointestinal tract, whereas COX-2 enzymes are responsible for releasing prostaglandins after infection or injury. Prostaglandins have a number of different effects, one of which is to regulate inflammation. Most NSAIDs inhibit both enzymes, although a few are available that mainly inhibit COX-2. The pain-relieving and anti-inflammatory effects of NSAIDs are mainly due to inhibition of COX-2, and their unwanted side effects are largely due to inhibition of COX-1.

The primary difference between competitive and non-competitive is that competitive inhibition effects the substrates ability to bind by binding an inhibitor in place of a substrate, this lowers the affinity of the enzyme for the substrate. In non-competitive inhibition the inhibitor binds to an allosteric site and prevents the enzyme-substrate complex from performing a chemical reaction. This does not affect the Km (affinity) of the enzyme (for the substrate). Non-competitive inhibition differs from uncompetitive inhibition in that it still allows for the substrate to bind to the enzyme-inhibitor complex and form an enzyme-substrate-inhibitor complex, this is not true in uncompetitive inhibition, it prevents the substrate from binding to the enzyme inhibitor through conformational change upon allosteric binding.

SUMMARY AND SUGGESTIONS There is no doubt that inhibiting eicosanoid synthesis by modern drugs therapies is effective for many people in reducing the inflammation and the accompanying pain of many diseases, particularly arthritis. It has been shown that regular consumption of aspirin, even in small doses of about 80 mg/day, reduces risk of heart attack and colon cancer, and this effect appears to be mediated, at least in part, by inhibiting eicosanoids. For those suffering from serious diseases, many wish to avoid using the standard drugs, or avoid using them frequently, due to experience of side effects or concerns about side effects. Prolonged use of corticosteroid drugs and NSAIDS has been linked to serious reactions in some individuals. In order to take reasonable steps to minimize the symptoms of these diseases through means other than relying on the drugs, it is important to understand the process by which the inflammation and other disease manifestations (., platelet sticking, bronchiospasms) occur.

Cox-2 inhibition non steroidal anti-inflammatory drugs

cox-2 inhibition non steroidal anti-inflammatory drugs


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