Therapy of Inflammatory Bowel Disease using New 5-ASA Compounds: An Introduction
Strong evidence has been accumulating that mesalazine (5- aminosalicylic acid, 5-ASA) represents the therapeutic moiety of the standard drug sulphasalazine. Since the active metabolite avoids the toxic potential of sulphapyridine, this perception has initiated new therapeutic approaches, for example...
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Main Author: | |
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Format: | Article |
Language: | English |
Published: |
Wiley
1989-01-01
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Series: | Canadian Journal of Gastroenterology |
Online Access: | http://dx.doi.org/10.1155/1989/434838 |
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Summary: | Strong evidence has been accumulating that mesalazine (5-
aminosalicylic acid, 5-ASA) represents the therapeutic moiety of the standard
drug sulphasalazine. Since the active metabolite avoids the toxic potential of
sulphapyridine, this perception has initiated new therapeutic approaches, for
example, two 5-ASA molecules have been coupled to form another prodrug
(olsalazine) which again depends on a proper cleavage of the azobond by bacteria
in the colon A more direct way has been applied successfully by administering
5-ASA itself in special galenic formulation (suppositories, enemas, controlled release
preparations) to provide enough active material at the proposed sites of action in
the terminal ileum and/or colon. One major advantage of all 5-ASA compounds,
compared to sulphasalazine, is their 10-fold lower potential (incidence) for inducing
allergic reactions or causing intolerance. Aside from rare hypersensitivity reactions,
5-ASA can cause nausea. vomiting, headache and gastrointestinal disturbances
in 1 to 5% of patients. However, the new azocompound olsalazine induced
diarrhea or loose stool in at least 10 to 15% of the treated patients which might
limit its use in inflammatory bowel disease (IBD). In conclusion, the ‘old’ metabolite
5-ASA, in a ‘new’ design, offers an effective and very safe choice for the treatment of IBD. |
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ISSN: | 0835-7900 |