Antiinflamatory Agents Less Dangerous for Gastrointestinal Tract

Authors: Rodriguez-Tellez, M.; Arguelles, F.; Herrerias Jr., J.M.; Ledro, D.; Esteban, J.; Herrerias, J.M.

Source: Current Pharmaceutical Design, Volume 7, Number 10, 1 July 2001 , pp. 951-976(26)

Publisher: Bentham Science Publishers

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Abstract:

NSAIDs represent one of the most commonly used therapeutic drug groups worldwide. 1.5percent of the world population is estimated as taking NSAIDs. However, their use is not risk free and gastrointestinal (GI) lesions do appear, which is indeed the main reason for their toxicity. Frequently (50percent) NSAID-induced GI-Lesions are asymptomatic, 71percent of GI perforations and 50percent of upper gastric hemorrhages (UGH) are associated with taking NSAIDs

How frequent GI lesions appear is directly related to whether the patient is in a risk group or not. Factors increasing the risk of GI lesions occurring are the following: being older than 60, using corticoids or other NSAIDs concomitantly, having a history of duodenal ulcer, alcohol consumption, smoking or taking oral anticoagulants. As the toxicity and how frequent the lesions appear depend on which drug is used, there is a need for research into new drugs which are both clinically effective and safer to use.

GI toxicity of NSAIDs is mediated by two mechanisms, direct toxicity and prostaglandin synthesis inhibition or sistemic mechanism. Due to the relatively recent discoveries concerning the physiopathology of inflammation and gastric physiology, research into new NSAID derivatives is taking place. Such derivatives are prodrugs, galenic buffer forms, selective COX-2 inhibitors, isomeric compounds, NO-donors, and as a future possibility, phosphodiesterase inhibitors.
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  • Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

    Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
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