Mesalazine

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Overview

Mesalazine
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Clinical data
Routes of
administration
oral rectal
ATC code
Pharmacokinetic data
Bioavailabilityorally: 20-30% absorbed
rectally: 10-35%
MetabolismRapidly & extensively metabolised intestinal mucosal wall and the liver.
Elimination half-life5 hours after initial dose.
At steady state 7 hours
Identifiers
CAS Number
PubChem CID
DrugBank
E number{{#property:P628}}
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Chemical and physical data
FormulaC7H7NO3
Molar mass153.135 g/mol

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List of terms related to Mesalazine

Mesalazine (INN, BAN), also known as Mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammation of the digestive tract (Crohn's disease) and mild to moderate ulcerative colitis. Mesalazine is a bowel-specific aminosalicylate drug that is metabolized in the gut and has its predominant actions there, thereby having fewer systemic side effects.

As a derivative of salicylic acid, 5-ASA is also an antioxidant that traps free radicals, which are potentially damaging by-products of metabolism.

5-ASA is considered the active moiety of sulfasalazine, which is metabolized to it.

Formulations

It is formulated for oral ingestion as tablets or granules, and for rectal administration as rectal suppository, suspension or enemas. It is sold under a variety of brand names (UK: Asacol, Ipocal, Pentasa & Salofalk. US: Canasa, Rowasa, Pentasa, Asacol and Lialda). The newest of these is Lialda, approved by the FDA in January 2007 for induction of remission in ulcerative colitis. Its main benefit is that it needs to be taken only once a day, which improves convenience and treatment compliance.

Dosing depends on the preparation used, in particular, slow-release tablets may have quite different drug delivery characteristics and are not interchangeable.

Preparations that lower stool pH (such as lactulose, a laxative) will affect the binding of Mesalazine in the bowel and will therefore reduce its efficacy.

Side effects

Commonly:

  • Diarrhea
  • Nausea
  • Cramping

Uncommonly:

Rarely:

Mesalazine avoids the sulphonamide side effects of Sulfasalazine (which contains additional (sulfapyridine), but carries additional rare risks of:

Monitoring

As a result of the small risks of kidney, liver and blood disorders, blood tests should be taken before and after starting treatment. Patients are advised to report any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that occurs during treatment so that a full blood count can be urgently taken.

References

  • British National Formulary 45 March 2003
  • Edited by Sean C. Sweetman, ed. (November 30, 2004). Martindale: The complete drug reference (34th edition ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4.

External links


de:5-Aminosalicylsäure hr:Mesalazin



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