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Mesalazine

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Mesalazine
Clinical data
Trade namesPentasa, Asacol, Canasa, Rowasa, Lialda, Apriso, Salofalk
AHFS/Drugs.comMonograph
MedlinePlusa688021
License data
Routes of
administration		oral, rectal
ATC code
Legal status
Legal status
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
  • 5-amino-2-hydroxybenzoic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.001.745 Edit this at Wikidata
Chemical and physical data
FormulaC7H7NO3
Molar mass153.135 g/mol g·mol−1
3D model (JSmol)
  • O=C(O)c1cc(ccc1O)N
  • InChI=1S/C7H7NO3/c8-4-1-2-6(9)5(3-4)7(10)11/h1-3,9H,8H2,(H,10,11) checkY
  • Key:KBOPZPXVLCULAV-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Mesalazine (INN, BAN), also known as Mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inflammatory drug used to treat inflammatory bowel disease, such as ulcerative colitis[1] and mild-to-moderate Crohn's disease.[2] Mesalazine is a bowel-specific aminosalicylate drug that acts locally in the gut and has its predominant actions there, thereby having few systemic side effects.[3] As a derivative of salicylic acid, 5-ASA is also thought to be an antioxidant that traps free radicals, which are potentially damaging byproducts of metabolism.[3]

5-ASA is considered the active moiety of sulfasalazine, which is metabolized to sulfapyridine and 5_ASA.[4]

Formulations

Mesalazine is formulated for oral ingestion as tablets or granules, and for rectal administration as a rectal suppository, suspension or enemas.[citation needed] It is marketed under a variety of brand names:[citation needed]

  • UK: Asacol, Ipocal, Pentasa, Salofalk, Mezavant XL
  • Ireland: Asacolon, Pentasa, Salofalk, Mezavant XL
  • France: Asacol, Pentasa, Mezavant
  • US: Canasa, Rowasa, Pentasa, Asacol, Lialda, Apriso,Salofalk
  • Canada: Asacol, Pentasa, Salofalk, Mezavant
  • India: Mesacol
  • Mexico: Salofalk
  • Uruguay: Mesacron, Mesalazina

The newest of these is Apriso (Salofalk granules in Europe), approved by the U.S. Food and Drug Administration (FDA) in October 2008, for the induction and maintenance of remission in ulcerative colitis. Its main benefit is that it needs to be taken only once a day, which provides convenient dosing regimen for patients. Several formulations of mesalazine have published data to suggest that once-daily dosing is sufficient in ulcerative colitis.

Pentasa 250 MG Extended Release Capsule

Lialda (Mesavant XL in Europe) contains the highest mesalamine dose per tablet (1.2 g).

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

Preparations that lower stool pH (such as lactulose, a laxative) will possibly affect the binding of mesalazine in the bowel and will therefore reduce its efficacy.[citation needed]

Side effects

Commonly:

  • Diarrhea
  • Nausea
  • Cramping
  • Flatulence[5]

Uncommonly:


Rarely:

Mesalazine avoids the sulfonamide 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

  1. ^ Attention: This template ({{cite pmid}}) is deprecated. To cite the publication identified by PMID 11709512, please use {{cite journal}} with |pmid=11709512 instead.
  2. ^ Sandborn WJ, Feagan BG, Lichtenstein GR (2007). "Medical management of mild to moderate Crohn's disease: evidence-based treatment algorithms for induction and maintenance of remission". Alimentary Pharmacology & Therapeutics. 26 (7): 987–1003. doi:10.1111/j.1365-2036.2007.03455.x. PMID 17877506. Retrieved 2009-12-20. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  3. ^ a b "mesalazine". PharmGKB.
  4. ^ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark.
  5. ^ "Lialda Side Effects & Safety Information". Shire US. 2007. Retrieved 2008-01-07. {{cite web}}: Unknown parameter |month= ignored (help)
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