Mesalazine
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Overview
| Image:Mesalazine structure.svg | |
| Mesalazine
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| Systematic (IUPAC) name | |
| 5-amino-2-hydroxybenzoic acid | |
| Identifiers | |
| CAS number | |
| ATC code | A07 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C7H7NO3 |
| Mol. mass | 153.135 g/mol |
| 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 |
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Ongoing Trials on Mesalazine at Clinical Trials.gov Clinical Trials on Mesalazine at Google
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US National Guidelines Clearinghouse on Mesalazine
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Patient resources on Mesalazine Discussion groups on Mesalazine Patient Handouts on Mesalazine Directions to Hospitals Treating Mesalazine Risk calculators and risk factors for Mesalazine
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Causes & Risk Factors for Mesalazine | |
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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 (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:
- Headache
- Exacerbation of the colitis
- Hypersensitivity reactions (including rash, urticaria, 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
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
- (November 30, 2004) in Edited by Sean C. Sweetman: Martindale: The complete drug reference, 34th edition, London: Pharmaceutical Press. ISBN 0-85369-550-4.
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.
Antidiarrheals, intestinal anti-inflammatory/anti-infective agents (A07) | |
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| Intestinal anti-infectives | Antibiotics (Neomycin, Nystatin, Natamycin, Streptomycin, Polymyxin B, Paromomycin, Amphotericin B, Kanamycin, Vancomycin, Colistin, Rifaximin)
Sulfonamides (Phthalylsulfathiazole, Sulfaguanidine, Succinylsulfathiazole) other (Miconazole, Broxyquinoline, Acetarsol, Nifuroxazide, Nifurzide) |
| Intestinal adsorbents | Charcoal - Bismuth - Pectin - Kaolin - Crospovidone - Attapulgite - Diosmectite |
| Antipropulsives | Diphenoxylate - Opium - Loperamide - Difenoxin |
| Intestinal anti-inflammatory agents | corticosteroids acting locally (Prednisolone, Hydrocortisone, Prednisone, Betamethasone, Tixocortol, Budesonide, Beclometasone)
antiallergic agents, excluding corticosteroids (Cromoglicic acid) aminosalicylic acid and similar agents (Sulfasalazine, Mesalazine, Olsalazine, Balsalazide) |
| Antidiarrheal micro-organisms | Saccharomyces boulardii |
| Other antidiarrheals | Albumin tannate - Ceratonia - Racecadotril |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
