Mesalazine

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Mesalazine
Mesalazine structure.svg
Clinical data
Trade namesAsacol, Lialda, Pentasa, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa688021
License data
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration
By mouth, rectal
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailabilityorally: 20–30% absorbed
rectally: 10–35%
MetabolismRapidly & extensively metabolised intestinal mucosal wall and the liver
Elimination half-life5 hours after initial dose.
At steady state 7 hours
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.001.745 Edit this at Wikidata
Chemical and physical data
FormulaC7H7NO3
Molar mass153.135 g/mol g·mol−1
3D model (JSmol)
  (verify)

Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease.[1] It is generally used for mildly to moderately severe disease.[1] It is taken by mouth or rectally.[1] The formulations which are taken by mouth appear to be similarly effective.[2]

Common side effects include headache, nausea, abdominal pain, and fever.[1] Serious side effects may include pericarditis, liver problems, and kidney problems.[1][2] Use in pregnancy and breastfeeding appears safe.[2] In people with a sulfa allergy certain formulations may result in problems.[1] Mesalazine is an aminosalicylate and anti-inflammatory.[1][2] It works by direct contact with the intestines.[1]

Mesalazine was approved for medical use in the United States in 1987.[1] It is avaliable as a generic medication and sold under many brand names worldwide.[3][1] A month supply in the United Kingdom costs the NHS about 43 £ as of 2019.[2] In the United States the wholesale cost of this amount is about 288 USD.[4] In 2016 it was the 240th most prescribed medication in the United States with more than 2 million prescriptions.[5]

Medical uses[edit]

It is used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease.[1] It is generally used for mildly to moderately severe disease.[1] It is taken by mouth or rectally.[1] The formulations which are taken by mouth appear to be similarly effective.[2]

Side effects[edit]

There are 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.[6]

Side effects are primarily gastrointestinal but may also include headache; GI effects include nausea, diarrhea and abdominal pain. There have been scattered reports of various problems when the oral form is used, including: problems caused by myelosuppression (leukopenia, 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.[7][6]

Chemistry[edit]

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.[8] It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.[9]

References[edit]

  1. ^ a b c d e f g h i j k l m n "Mesalamine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.
  2. ^ a b c d e f British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 39–41. ISBN 9780857113382.
  3. ^ "ANDA Approval Reports - 2017 First Generic Drug Approvals". www.fda.gov. Retrieved 8 April 2019.
  4. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
  5. ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
  6. ^ a b UK Electronic Medicines Compendium Suppository Label Last revised February 2016
  7. ^ UK Electronic Medicines Compendium UL Oral Label Last revised December 2015
  8. ^ Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark
  9. ^ Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10

External links[edit]