Information about Mesalamine
Mesalamine, also known as mesalazine and 5-aminosalicylate, is an orally available, antiinflammatory agent used for the treatment of ulcerative colitis to both induce and maintain remissions in disease.
Liver safety of Mesalamine
Mesalamine therapy has been associated with a low rate of serum enzyme elevations during therapy and with rare instances of clinically apparent acute liver injury.
Mechanism of action of Mesalamine
Mesalamine (me sal’ a meen) is used to treat disease flares in ulcerative colitis and to maintain disease remission. Mesalamine has antiinflammatory, antioxidant and antimicrobial activity and is locally active in the large intestine in reducing inflammation and injury. Mesalamine appears to act by inhibition of lipooxygenase activity, thereby inhibiting production of leukotrienes and leading to reduction in interleukin 1 (IL-1) and tumor necrosis factor (TNF) alpha.
FDA approval information for Mesalamine
Mesalamine was approved for use in the United States in 1985 and remains a first line agent in the therapy of ulcerative colitis, both for induction and maintenance of clinical remission. It is poorly effective in Crohn disease, its major activity being in the large, rather than the small intestine. Mesalamine by itself is largely absorbed in the small intestine and little reaches the colon. For this reason, it is formulated to avoid absorption in the upper intestine and to be released in active form in the colon. The delayed absorption is accomplished either by enteric coating or by formulation as a pro-drug that is activated in the large intestine by local conditions or bacterial enzymes. Formulations of mesalamine include extended or delayed release formulations (Pentasa, Asacol, Lialda, Apriso) and mesalamine pro-drugs including sulfasalazine, olsalazine and balsalazide.
Dosage and administration for Mesalamine
Typical doses range considerable and vary by preparation, but are generally in the range of 1.5 to 4.8 g of mesalamine daily. Mesalamine is also available as an enema (Rowasa and others) and rectal suppositories (Canasa), which are useful for ulcerative proctitis and in ameliorating symptoms in mildly active, distal ulcerative colitis.
Balsalazide (bal sal’ a zide) is a pro-drug of mesalamine that consists of 5-aminosalicylate with an azo bond to a phenyl-hydroxybenzoid acid moiety which is cleaved off in the large intestine by bacterial enzymes, releasing free mesalamine. Balsalazide was approved as treatment of mildly to moderately active ulcerative colitis in adults in the United States in 2000 and is available generically and under the brand name Colazal in capsules of 750 mg; the usual dosage being 2.25 to 6.75 g daily in three divided doses.
Olsalazine (ol sal’ a zeen) is a prodrug of mesalamine that consists of two molecules of 5-aminocsalicylate (5’5’-azodisalicylate) joined at the amino-terminus with an azo bond that is cleaved by bacterial action in the colon, releasing two molecules of mesalamine. Olsalazine was approved in the United States for maintenace of remission of ulcerative colitis in patients intolerant of sulfasalazine in 2007 and is available under the brand name Dipentum in capsules of 250 mg, the usual dose being 500 mg twice daily.
Sulfasalazine (sul" fa sal' a zeen) is a prodrug of mesalamine that consists of 5-aminosalicylate joined with an azo bond to sulfapyridine. Sulfasalazine has been used extensively in the treatment of ulcerative colitis, but adverse reactions to the sulfonamide component of the agent can be problematic and has led to a decline in its use in favor of mesalamine by itself.
Mesalamine is generally well tolerated and adverse event rates are similar to what is reported with placebo therapy of ulcerative colitis. Side effects may include diarrhea, headache, dizziness and nausea. Hypersensitivity reactions and pancreatitis can occur, but are rare.
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