Mesalazine
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Mesalazine
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| Systematic (IUPAC) name | |
| 5-amino-2-hydroxybenzoic acid | |
| Identifiers | |
| CAS number | |
| ATC code | A07 |
| PubChem | |
| DrugBank | |
| ChemSpider | |
| Chemical data | |
| Formula | C7H7NO3 |
| Mol. mass | 153.135 g/mol |
| SMILES | & |
| 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 |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | oral rectal |
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 and mild to moderate Crohn's disease. 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. 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.
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[edit] 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 and Salofalk. US: Canasa, Rowasa, Pentasa, Asacol, Lialda, and Apriso. India: Masacol). The newest of these is Apriso, approved by the FDA in October 2008 for induction 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.
Lialda contains the highest mesalamine dose per tablet (1.2 g). Other currently available mesalamines require three to four times daily dosing and 6 to 16 pills a day. Whether convenience leads to improved compliance and adherence to therapy long term remains to be proven. Adherence to IBD therapy is multifactorial.
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.
[edit] Side effects
Commonly:
- Diarrhea
- Nausea
- Cramping
- Flatulence [1]
Uncommonly:
- Headache
- Exacerbation of the colitis
- Hypersensitivity reactions (including rash, urticaria aka hives, interstitial nephritis and lupus erythematosus-like syndrome)
- Hair Loss
- Interstitial nephritis
Rarely:
- Acute pancreatitis,
- Hepatitis
- Nephrotic syndrome
- Blood disorders (including agranulocytosis, aplastic anaemia, leukopenia, neutropenia, thrombocytopenia)
Mesalazine avoids the sulphonamide side effects of Sulfasalazine (which contains additional sulfapyridine), but carries additional rare risks of:
- Allergic lung reactions
- Allergic myocarditis
- Methaemoglobinaemia
[edit] 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.
[edit] References
- ^ "Safety Information about Lialda". Lialda Side Effects. October 2007. http://www.lialda.com/aboutLialda/sideEffect.asp. Retrieved on 2008-01-07.
- 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.
[edit] External links
- Optimal Dosing of 5-Aminosalicylic Acid: 5 Decades of Choosing Between Politicians
- "Novel formulation increases efficacy of mesalamine for treating ulcerative colitis" Reuters article on Lialda/Mezavant trial success.
- [www.ccfa.org/reuters/mesalazine Once daily mesalazine effective in active ulcerative colitis: study]
- Pentasa Official Site
- Asacol Official Site
- [www.lialda.com/ Lialda Official Site]
- [www.apriso-uc.com/ Apriso Official Site]
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