Mesalazine

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.[3]

Mesalazine
Clinical data
Trade namesAsacol, Lialda, Pentasa, others[1]
Other namesmesalamine, 5-aminosalicylic acid, 5-ASA, Mesalazine (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa688021
License data
Pregnancy
category
  • AU: C [2]
  • US: B (No risk in non-human studies) [2]
    Routes of
    administration    		By mouth, rectal
    ATC code
    Legal status
    Legal status
    • AU: S4 (Prescription only)
    • UK: POM (Prescription only)
    • US: ℞-only
    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
    Chemical and physical data
    FormulaC7H7NO3
    Molar mass153.137 g·mol−1
    3D model (JSmol)
    Melting point283 °C (541 °F)
      (verify)

    Common side effects include headache, nausea, abdominal pain, and fever.[1] Serious side effects may include pericarditis, liver problems, and kidney problems.[1][3] Use in pregnancy and breastfeeding appears safe.[3] In people with a sulfa allergy certain formulations may result in problems.[1] Mesalazine is an aminosalicylate and anti-inflammatory.[1][3] It works by direct contact with the intestines.[1]

    Mesalazine was approved for medical use in the United States in 1987.[1][4] It is available as a generic medication and sold under many brand names worldwide.[5][1] In 2017, it was the 246th most commonly prescribed medication in the United States, with more than one million prescriptions.[6][7]

    Medical uses

    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.[3]

    Side effects

    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,[8] people with kidney disease,[8] or people who are allergic to aspirin.[8]

    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.[8]

    Chemistry

    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]

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    References
    1. "Mesalamine Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists.
    2. "Mesalamine Use During Pregnancy". Drugs.com. 18 September 2018. Retrieved 30 December 2019.
    3. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 39–41. ISBN 9780857113382.
    4. "Asacol HD- mesalamine tablet, delayed release". DailyMed. 15 April 2018. Retrieved 30 December 2019.
    5. "ANDA Approval Reports - 2017 First Generic Drug Approvals". Food and Drug Administration (FDA). Retrieved 8 April 2019.
    6. "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
    7. "Mesalamine - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
    8. "Asacol 400mg MR Tablets - Summary of Product Characteristics (SmPC)". (emc). 14 April 2016. Retrieved 30 December 2019.
    9. Lippencott's Illustrated Reviews: Pharmacology, 4th Ed. Finkel, Cubeddu and Clark
    10. Drugs & Therapy Properties 2003 Oct; Vol 19, No. 10
    • "Mesalamine". Drug Information Portal. U.S. National Library of Medicine.
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