Overview of 5-ASA in Therapy of Inflammatory Bowel Disease

There are two forms of 5-aminosalicylic acid (5-ASA) drug delivery. First, a pro-drug form in which 5-ASA, the active principal, is attached to a c.arrier molecule and released in the intestine by bacterial cleavage. An example of this is sulfasalazine, originally developed in the 1940s and found to...

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Main Author: CN Williams
Format: Article
Language:English
Published: Wiley 1994-01-01
Series:Canadian Journal of Gastroenterology
Online Access:http://dx.doi.org/10.1155/1994/756973
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author CN Williams
author_facet CN Williams
author_sort CN Williams
collection DOAJ
description There are two forms of 5-aminosalicylic acid (5-ASA) drug delivery. First, a pro-drug form in which 5-ASA, the active principal, is attached to a c.arrier molecule and released in the intestine by bacterial cleavage. An example of this is sulfasalazine, originally developed in the 1940s and found to be effective, cheap, but limited by side effects due to the sulfapyridine component. The second drug delivery system depends on an enteric coating for delayed pH-dependent release or for a timed-released mechanism. 5-ASA inhibits 5-lipoxygenase, modulates leukocyte function and inhibits soluble mediator release, and is an effective scavenger action of free oxygen radicals, the relative importance of which is unknown. The multiplicity of action is probably its strength because drugs that have only one of these actions are relatively ineffective in inflammatory bowel disease. 5-ASA compounds are effective in treating mild to moderate acute ulcerative colitis and in maintaining remission, and are equivalent to sulfasalazine in this regard. 5-ASA used topically in enema or suppository form is highly efficient in both acute disease and in maintaining remission. 5-ASA is also effective in active Crohn’s disease, but not as effective as in maintenance therapy compared with ulcerative colitis. The pro-drugs tend to have more side effects. Slow release compounds are well tolerated with few side effects, allowing increases to effective dosage. In patients intolerant of sulfasalazine, switching to a 5-ASA preparation usually results in tolerance and therapeutic benefit, with an occasional allergic reaction to the 5-ASA molecule limiting its use.
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spelling doaj-art-7cfd52c8803543d3a8f755d707db5a972025-02-03T01:30:45ZengWileyCanadian Journal of Gastroenterology0835-79001994-01-018637938210.1155/1994/756973Overview of 5-ASA in Therapy of Inflammatory Bowel DiseaseCN Williams0Division of Gastroenterology, Department of Medicine, Dalhousie University, Halifax, Nova Scotia, CanadaThere are two forms of 5-aminosalicylic acid (5-ASA) drug delivery. First, a pro-drug form in which 5-ASA, the active principal, is attached to a c.arrier molecule and released in the intestine by bacterial cleavage. An example of this is sulfasalazine, originally developed in the 1940s and found to be effective, cheap, but limited by side effects due to the sulfapyridine component. The second drug delivery system depends on an enteric coating for delayed pH-dependent release or for a timed-released mechanism. 5-ASA inhibits 5-lipoxygenase, modulates leukocyte function and inhibits soluble mediator release, and is an effective scavenger action of free oxygen radicals, the relative importance of which is unknown. The multiplicity of action is probably its strength because drugs that have only one of these actions are relatively ineffective in inflammatory bowel disease. 5-ASA compounds are effective in treating mild to moderate acute ulcerative colitis and in maintaining remission, and are equivalent to sulfasalazine in this regard. 5-ASA used topically in enema or suppository form is highly efficient in both acute disease and in maintaining remission. 5-ASA is also effective in active Crohn’s disease, but not as effective as in maintenance therapy compared with ulcerative colitis. The pro-drugs tend to have more side effects. Slow release compounds are well tolerated with few side effects, allowing increases to effective dosage. In patients intolerant of sulfasalazine, switching to a 5-ASA preparation usually results in tolerance and therapeutic benefit, with an occasional allergic reaction to the 5-ASA molecule limiting its use.http://dx.doi.org/10.1155/1994/756973
spellingShingle CN Williams
Overview of 5-ASA in Therapy of Inflammatory Bowel Disease
Canadian Journal of Gastroenterology
title Overview of 5-ASA in Therapy of Inflammatory Bowel Disease
title_full Overview of 5-ASA in Therapy of Inflammatory Bowel Disease
title_fullStr Overview of 5-ASA in Therapy of Inflammatory Bowel Disease
title_full_unstemmed Overview of 5-ASA in Therapy of Inflammatory Bowel Disease
title_short Overview of 5-ASA in Therapy of Inflammatory Bowel Disease
title_sort overview of 5 asa in therapy of inflammatory bowel disease
url http://dx.doi.org/10.1155/1994/756973
work_keys_str_mv AT cnwilliams overviewof5asaintherapyofinflammatoryboweldisease