Mesalazine: Mesalazine (INN, BAN), Also Known As Mesalamine (USAN) or 5-Aminosalicylic Acid

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Mesalazine - Wikipedia, the free encyclopedia

http://en.wikipedia.org/wiki/Mesalazine

Mesalazine
From Wikipedia, the free encyclopedia

Mesalazine (INN, BAN), also known as mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an anti-inammatory drug used to treat inammatory bowel disease, such as [1] ulcerative colitis and mild-to-moderate [2] Crohn's disease. Mesalazine is a bowelspecic aminosalicylate drug that acts locally in the gut and has its predominant actions there, [3] thereby having few systemic side eects. As a derivative of salicylic acid, mesalazine is also thought to be an antioxidant that traps free radicals, which are potentially damaging [3] byproducts of metabolism. Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and [4] mesalazine. Mesalazine is formed from the prodrug balsalazide along with the inert carrier molecule [5] 4-aminobenzoyl-beta-alanine.

Mesalazine

Systematic (IUPAC) name


5-amino-2-hydroxybenzoic acid

Clinical data Trade names Pentasa, Delzicol, Canasa, Rowasa, Lialda, Apriso, Salofalk AHFS/Drugs.com monograph MedlinePlus Licence data Pregnancy cat. Legal status Routes Bioavailability a688021 US Daily Med:link B
(US) (US)

Contents
1 2 3 4 5 Side eects Monitoring Formulations References External links

-only

oral, rectal Pharmacokinetic data orally: 20-30% absorbed rectally: 10-35%

Metabolism

Rapidly & extensively metabolised intestinal mucosal wall and the liver

Side eects
Commonly: Diarrhea Nausea Cramping Flatulence[6] Uncommonly:
Half-life

5 hours after initial dose. At steady state 7 hours Identiers

CAS number

89-57-6

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Mesalazine - Wikipedia, the free encyclopedia

http://en.wikipedia.org/wiki/Mesalazine

Headache Exacerbation of the colitis Hypersensitivity reactions (including rash, urticaria aka hives, interstitial nephritis and lupus erythematosus-like syndrome) Hair loss Rarely: Acute pancreatitis Hepatitis Nephrotic syndrome Blood disorders (including agranulocytosis, aplastic anaemia, leukopenia, neutropenia, thrombocytopenia) Fever [7] Mesalazine avoids the sulfonamide side eects of sulfasalazine (which contains additional sulfapyridine), but carries additional rare risks of: Allergic lung reactions Allergic myocarditis Methaemoglobinaemia

ATC code PubChem IUPHAR ligand DrugBank ChemSpider UNII KEGG ChEBI ChEMBL Formula Mol. mass
SMILES InChI

A07EC02 CID 4075 2700 DB00244 3933 4Q81I59GXC D00377 CHEBI:6775 CHEMBL704 Chemical data C7H7NO3 153.135 g/mol

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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.

Formulations
Mesalazine is formulated for oral ingestion as tablets or granules, and for rectal administration as a rectal suppository, [citation needed] It is marketed under a suspension or enemas. [citation needed] variety of brand names: UK: Asacol, Ipocal, Pentasa, Salofalk, Mezavant XL Ireland: Asacolon, Pentasa, Salofalk, Mezavant XL France: Asacol, Pentasa, Mezavant US: Canasa, Rowasa, Pentasa, Delzicol, Lialda, Apriso, Salofalk Spain / Espaa: Pentasa, Claversal, Lixacol, Mezavant, Salofalk Canada: Asacol, Pentasa, Salofalk, Mezavant
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Pentasa 250 MG Extended Release Capsule

Thursday 26 September 2013 08:01 AM

Mesalazine - Wikipedia, the free encyclopedia

http://en.wikipedia.org/wiki/Mesalazine

India: Mesacol (available as tablets, suppositories, enema), VEGAZ-OD. Mexico: Salofalk Serbia: Salofalk Uruguay: Mesacron, Mesalazina Brazil: Mesalazina, Mesalazina Enema, Mesacol, Mesacol MNX, Asalit, Australia: Mesasal Egypt: Pentasa, Salofalk Chron-asa 5, Pentasa, Pentasa Enema, Mesaneo Dosing depends on the preparation used; in particular, slow-release tablets may have [citation needed] quite dierent drug delivery characteristics and are not interchangeable. Preparations that lower stool pH (such as lactulose, a laxative) will possibly aect the [citation needed] binding of mesalazine in the bowel and will therefore reduce its ecacy.

References
1. ^ Kruis, W.; Schreiber, I.; Theuer, D.; Brandes, J. W.; Schtz, E.; Howaldt, S.; Krakamp, B.; Hmling, J.; Mnnikes, H.; Koop, I.; Stolte, M.; Pallant, D.; Ewald, U. (2001). "Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses" (http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1728533). Gut 49 (6): 783789. doi:10.1136/gut.49.6.783 (http://dx.doi.org/10.1136%2Fgut.49.6.783). PMC 1728533 (//www.ncbi.nlm.nih.gov/pmc/articles/PMC1728533). PMID 11709512 (//www.ncbi.nlm.nih.gov/pubmed/11709512). 2. ^ Sandborn WJ, Feagan BG, Lichtenstein GR (October 2007). "Medical management of mild to moderate Crohn's disease: evidence-based treatment algorithms for induction and maintenance of remission" (http://www3.interscience.wiley.com/cgi-bin/fulltext/117987903 /HTMLSTART). Alimentary Pharmacology & Therapeutics 26 (7): 9871003. doi:10.1111/j.1365-2036.2007.03455.x (http://dx.doi.org /10.1111%2Fj.1365-2036.2007.03455.x). PMID 17877506 (//www.ncbi.nlm.nih.gov/pubmed /17877506). Retrieved 2009-12-20. 3. ^ a b "mesalazine" (http://www.pharmgkb.org/drug/PA450384#tabview=tab2&subtab=31). PharmGKB. 4. ^ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark 5. ^ Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10 6. ^ "Lialda Side Eects & Safety Information" (http://www.lialda.com/aboutLialda /sideEect.asp). Shire US. October 2007. Retrieved 2008-01-07. 7. ^ "Desensitization after fever induced by mesalazine" (http://onlinelibrary.wiley.com /doi/10.1034/j.1398-9995.1999.00298.x/full). December 2001. Retrieved 2001-12-24.

Mehta, Dinesh K, ed. (March 2003). British National Formulary 45. London: Pharmaceutical Press. ISBN 0-85369-555-5. Sweetman, Sean C, ed. (November 2004). Martindale: The complete drug reference (34th ed.). London: Pharmaceutical Press. ISBN 0-85369-550-4.

External links
3 of 4 Thursday 26 September 2013 08:01 AM

Mesalazine - Wikipedia, the free encyclopedia

http://en.wikipedia.org/wiki/Mesalazine

Bickston, S. J.; Cominelli, F. (January 2003). "Optimal dosing of 5-aminosalicylic acid: 5 Decades of choosing between politicians". Clinical Gastroenterology and Hepatology 1 (1): 34. doi:10.1053/jcgh.2003.50001 (http://dx.doi.org /10.1053%2Fjcgh.2003.50001). PMID 15017510 (//www.ncbi.nlm.nih.gov/pubmed /15017510). "Novel formulation increases ecacy of mesalamine for treating ulcerative colitis" (http://www.ccfa.org/reuters/mesalamine). Reuters. February 16, 2007. "Once daily mesalazine eective in active ulcerative colitis: study" (http://www.ccfa.org/reuters/mesalazine). Reuters. January 30, 2009. Pentasa Ocial Site (http://www.pentasaus.com/) Asacol Ocial Site (http://www.asacol.com/) Lialda Ocial Site (http://www.lialda.com/) Apriso Ocial Site (http://www.apriso-uc.com/) Pentasa Full Prescribing Information (http://pi.shirecontent.com/PI/PDFs /Pentasa_USA_ENG.pdf) Shire Asacol Full Prescribing Information (http://www.asacol.com/pdf/asacol-info.pdf) Warner Chilcott Lialda Full Prescribing Information (http://pi.shirecontent.com/PI/PDFs /Lialda_USA_ENG.pdf) Shire Apriso Full Prescribing Information (http://www.aprisorx.com/assets/pdf/aprisopi.pdf) Salix Pharmaceuticals Retrieved from "http://en.wikipedia.org/w/index.php?title=Mesalazine& oldid=573334294" Categories: Anilines Anti-inammatory agents Gastroenterology Salicylic acids Antioxidants This page was last modied on 17 September 2013 at 14:59. Text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia is a registered trademark of the Wikimedia Foundation, Inc., a non-prot organization.

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