Mesalazine

Mesalazine
Systematic (IUPAC) name
5-Amino-2-hydroxybenzoic acid
Clinical data
Trade names Many names worldwide[1]
AHFS/Drugs.com monograph
MedlinePlus a688021
License data
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration		 oral, rectal
Legal status
Legal status
Pharmacokinetic data
Bioavailability orally: 20-30% absorbed
rectally: 10-35%
Metabolism Rapidly & extensively metabolised intestinal mucosal wall and the liver
Biological half-life 5 hours after initial dose.
At steady state 7 hours
Identifiers
CAS Number 89-57-6 YesY
ATC code A07EC02 (WHO)
PubChem CID 4075
IUPHAR/BPS 2700
DrugBank DB00244 YesY
ChemSpider 3933 YesY
UNII 4Q81I59GXC YesY
KEGG D00377 YesY
ChEBI CHEBI:6775 YesY
ChEMBL CHEMBL704 YesY
Chemical data
Formula C7H7NO3
Molar mass 153.135 g/mol
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Mesalazine (INN, BAN), also known as mesalamine (USAN) or 5-aminosalicylic acid (5-ASA), is an aminosalicylate anti-inflammatory drug[2] used to treat inflammatory bowel disease, including ulcerative colitis,[3][4][5] inflamed anus or rectum,[6] and to maintain remission in Crohn's disease.[3][7]

It is sold in an oral form to maintain remission in Crohn's disease,[3] and as a rectal suppository[4][6] and an enema for the lower bowel conditions.[5] It is generic and sold under many brand names worldwide,[1] and there are many formulations.[8]

There is no data on use in pregnant women, but the drug does cross the placenta and is excreted in breast milk. The drug should not be used in children under two, people with kidney disease, or people who are allergic to aspirin.[4]

Side effects are primary gastrointestinal but may include headache; GI effects include nausea, diarrhoea and abdominal pain. There have been scattered reports of various problems when the oral form is used, including problems caused by myelosuppression (leucopenia, neutropenia, agranulocytosis, aplastic anaemia, and thrombocytopenia, as well as hair loss, peripheral neuropathy, pancreatitis, liver problems, myocarditis and pericarditis, allergic and fibrotic lung reactions, lupus erythematosus-like reactions and rash (including urticaria), drug fever, interstitial nephritis and nephrotic syndrome, usually reversible on withdrawal. Very rarely, use of mesalazine has been associated with an exacerbation of the symptoms of colitis, Stevens Johnson syndrome and erythema multiforme.[3][4]

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.[9] It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.[10]

References

  1. 1 2 Drugs.com International trade names for mesalazine April 20, 2016
  2. ↑ "mesalazine". PharmGKB.
  3. 1 2 3 4 UK Electronic Medicines Compendium UL Oral Label Last revised December 2015
  4. 1 2 3 4 UK Electronic Medicines Compendium Suppository Label Last revised February 2016
  5. 1 2 UK Electronic Medicines Compendium UK Enema Label Last revised January 2016
  6. 1 2 FDA. US Suppository Label Last updated Nov 2015
  7. ↑ 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". Alimentary Pharmacology & Therapeutics 26 (7): 987–1003. doi:10.1111/j.1365-2036.2007.03455.x. PMID 17877506. Retrieved 2009-12-20.
  8. ↑ Ye B, van Langenberg DR. Mesalazine preparations for the treatment of ulcerative colitis: Are all created equal? World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):137-44. PMID 26558148 PMC 4635154
  9. ↑ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark
  10. ↑ Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10

External links

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