Which medications in the drug class 5-Aminosalicylic Acid Derivatives are used in the treatment of Pediatric Crohn Disease?

Updated: Oct 23, 2018
  • Author: Andrew B Grossman, MD; Chief Editor: Carmen Cuffari, MD  more...
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Answer

5-Aminosalicylic Acid Derivatives

5-ASA derivatives are used to treat mild-to-moderate Crohn disease and to maintain remission.

Mesalamine (Asacol, Pentasa, Rowasa, Canasa)

Mesalamine inhibits leukotriene biosynthesis via the lipoxygenase pathway of arachidonic acid metabolism and interferes with myeloperoxidase activity and reactive oxygen species. The oral mesalamine products currently approved in the United States differ only with respect to the mechanism of drug delivery. Mesalamine is approved by the US Food and Drug Administration (FDA) for treatment of UC but is widely used off label for treatment of Crohn disease.

Mesalamine products have not been approved for use in children but are considered standard of care for inflammatory bowel disease (IBD) and are supported by numerous reports in the literature.

Asacol contains mesalamine within a Eudragit-S coating that dissolves and releases the mesalamine at pH 7, which typically occurs in the terminal ileum. Pentasa contains 5-ASA in ethylcellulose and has a time-release coating. Release of mesalamine from Pentasa begins at the pylorus; consequently, this drug is often used when proximal intestinal Crohn disease is suggested. Despite the drug's proximal release site, there are no convincing data to indicate that the site of release translates into clinical superiority.

Rectal dosage forms deliver high concentrations of mesalamine to the left colon as high as the splenic flexure (enema with 30 minutes retention) or to the rectum for use in proctitis (suppository). Although mesalamine is effective, it is associated with a relatively high relapse rate upon discontinuance. In many cases, widespread use of topical agents is limited by patient acceptance; often, patients with active rectal disease have difficulty holding in the enema.


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