| Systematic (IUPAC) name | |
|---|---|
| 5-amino-2-hydroxybenzoic acid | |
| Clinical data | |
| Trade names | Pentasa, Asacol, Canasa, Rowasa, Lialda, Apriso, Salofalk |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a688021 |
| Licence data | US Daily Med:link |
| Pregnancy cat. | B(US) |
| Legal status | ℞-only (US) |
| Routes | oral, rectal |
| Pharmacokinetic data | |
| Bioavailability | orally: 20-30% absorbed rectally: 10-35% |
| Metabolism | Rapidly & extensively metabolised intestinal mucosal wall and the liver |
| Half-life | 5 hours after initial dose. At steady state 7 hours |
| Identifiers | |
| CAS number | 89-57-6 |
| ATC code | A07EC02 |
| PubChem | CID 4075 |
| DrugBank | APRD01098 |
| ChemSpider | 3933 |
| UNII | 4Q81I59GXC |
| KEGG | D00377 |
| ChEBI | CHEBI:6775 |
| ChEMBL | CHEMBL704 |
| Chemical data | |
| Formula | C7H7NO3 |
| Mol. mass | 153.135 g/mol |
| SMILES | eMolecules & PubChem |
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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 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]
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Mesalazine is formulated for oral ingestion as tablets or granules, and for rectal administration as a rectal suppository, suspension or enemas. It is marketed under a variety of brand names:
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.
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.
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.
Commonly:
Uncommonly:
Rarely:
Mesalazine avoids the sulphonamide side effects of sulfasalazine (which contains additional sulfapyridine), but carries additional rare risks of:
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.
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