Nonsteroidal anti-inflammatory drugs (NSAIDs) constitute a well-known group of drugs that are most widely used for a variety of inflammatory conditions and pain. However, their gastrointestinal side-effects, i.e. ulcers and gastrointestinal bleeding, hamper their usefulness in many clinical settings. The selective cyclo-oxygenase 2 (COX-2) inhibitors (the coxibs) promised to be a group of antiinflammatory drugs with significantly fewer, or no gastrointestinal side-effects. Nevertheless, more recent research into their effectiveness and safety profiles revealed that they are also associated with an increased risk of upper- and lower-gastrointestinal toxicity. Guidelines suggest that patients at risk of NSAID-induced gastrointestinal ulcers and toxicity should be given preventative treatment. However, only a small percentage of these patients receive any therapeutic intervention. Multiple strategies exist for reducing the risk of NSAID-induced gastrointestinal complications. An overview of these strategies and treatment options is provided in the article, as well as novel approaches to developing gastrointestinal- sparing NSAIDs (using selective inhibition of terminal prostaglandin synthases, and modified NSAIDs to slowly release gastroprotective gaseous mediators, e.g. nitric oxide and hydrogen sulphide). © Medpharm.
|Number of pages||7|
|Journal||SA Pharmaceutical Journal|
|Publication status||Published - 11 Jun 2012|