last updated 21-12-2024

Salicylates in IBD

Salicylates in IBD

Ulcerative colitis is often treated with aminosalicylates. These agents reduce the symptoms in mild disease and maintenance treatment reduces the relapse rates of patients in remission. Sulfasalazine was a commonly used combination of 5-aminosalicyclic acid with sulphapyridine which carried the former moiety to the lower part of the GI prior to cleavage and absorption. However, the carrier moiety was found to produce the typical toxic effects of sulphonamides (nausea, rash, blood dyscrasias) and the less toxic agents of mesalazine, olsalazine were produced.

The exact mechanism of action of the salicylates in inflammatory bowel disease is unknown, although COX inhibition is presumed to play a role. However the benefits of the various products can vary depending on their site of action. Mesalazine is most often used as either an enema or suppository preparation, or coated in pH-sensitive polymer to prevent absorption until the lower part of the GI when taken orally. The product Pentasa encapsulates ethylcellulose-coated, acid-resistant microgranules and releases its active ingredient in the duodenum, jejunum, ileum, and colon. Finally, olsalazine (5-ASA dimerised with an azo bond) is not absorbed until the lower GI tract when taken orally.

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In order to achieve the most therapeutic benefit in Crohn’s disease, the salicylate product would have to be capable of providing liberated 5-aminosalicylic acid throughout the gastrointestinal tract. Which product would you recommend?

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