Mesalazine Explained

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. It is generally used for mildly to moderately severe disease. It is taken by mouth or rectally. The formulations which are taken by mouth appear to be similarly-effective.

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

Mesalazine was approved for medical use in the United States in 1987.[2] [3] It is on the World Health Organization's List of Essential Medicines.[4] It is available as a generic medication.[2] [5] [6] [7] In 2021, it was the 239th most commonly prescribed medication in the United States, with more than 1million prescriptions.[8] [9]

Medical uses

See also: 4-Aminosalicylic acid. It is used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease (effective only in colonic diseases).[2]

In 2022 Germany introduced guidance to use mesalamine to treat acute uncomplicated diverticulitis.[10]

Side-effects

Most often reported side-effects are gastrointestinal (GI) (but may also include headache), including: nausea, diarrhea, and abdominal pain.

Very rarely, use of mesalazine has been associated with an exacerbation of the symptoms of colitis, Stevens Johnson syndrome, and erythema multiforme.[11]

Pregnancy

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 years of age, people with kidney disease, or people who are allergic to aspirin.

Chemistry

Mesalazine is the active moiety of sulfasalazine, which is metabolized to sulfapyridine and mesalazine.[12] It is also the active component of the prodrug balsalazide along with the inert carrier molecule 4-aminobenzoyl-beta-alanine.[13] It is in the category of disease-modifying antirheumatic drugs (DMARDs) family of medications.[14] It is unclear exactly how it works.[14] Mesalazine is claimed to be a PPAR-γ agonist.[15]

Mechanism of action

Exact mechanism of mesalazine is unknown, but is speculated that mesalazine decreases synthesis of prostaglandin and leukotriene, modulating the inflammatory response derived from the cyclooxygenase and lipooxygenase pathways.[16] It appears to act locally on colonic mucosa.[17]

Society and culture

Brand names

Mesalazine is sold under various names including Apriso, Asacol, Asacol HD, Canasa, Delzicol, Fivasa, Lialda, Salofalk, Pentasa, Rowasa, Octasa, and Sfrowasa. In Europe, it is sold under the name Salofalk (rectal suppository). [18] [19]

Notes and References

  1. Book: British national formulary: BNF 76. 2018. Pharmaceutical Press. 9780857113382. 39–41. 76.
  2. Web site: Mesalamine Monograph for Professionals . Drugs.com . American Society of Health-System Pharmacists .
  3. Web site: Asacol HD- mesalamine tablet, delayed release . DailyMed . 15 April 2018 . 30 December 2019.
  4. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 22nd list (2021) . 2021 . 10665/345533 . World Health Organization . World Health Organization . Geneva . WHO/MHP/HPS/EML/2021.02 . free .
  5. Web site: ANDA Approval Reports - 2017 First Generic Drug Approvals . Food and Drug Administration (FDA) . 3 November 2018 . 8 April 2019 .
  6. Web site: 2022 First Generic Drug Approvals . U.S. Food and Drug Administration (FDA) . 3 March 2023 . https://web.archive.org/web/20230630003602/https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/2022-first-generic-drug-approvals . 30 June 2023 . live . 30 June 2023.
  7. Web site: Competitive Generic Therapy Approvals . U.S. Food and Drug Administration (FDA) . 29 June 2023 . 29 June 2023 . 29 June 2023 . https://web.archive.org/web/20230629233651/https://www.fda.gov/drugs/generic-drugs/competitive-generic-therapy-approvals . live .
  8. Web site: The Top 300 of 2021 . ClinCalc . 14 January 2024 . 15 January 2024 . https://web.archive.org/web/20240115223848/https://clincalc.com/DrugStats/Top300Drugs.aspx . live .
  9. Web site: Mesalamine - Drug Usage Statistics . ClinCalc . 14 January 2024.
  10. New German guidelines for the management of diverticulitis. Anne F.. Peery. November 12, 2022. United European Gastroenterology Journal. 10. 9. 913–914. 10.1002/ueg2.12331. 36302089. 9731652.
  11. Web site: Asacol 400mg MR Tablets - Summary of Product Characteristics (SmPC) . (emc) . 14 April 2016 . 30 December 2019.
  12. Book: Finkel R, Clark MA, Cubeddu LX . Lippincott's Illustrated Reviews: Pharmacology . 2009 . Lippincott Williams & Wilkins . Fourth . 978-0-7817-7155-9 .
  13. Balsalazide: increasing the choice for patients with ulcerative colitis. . Drugs & Therapy Perspectives . 19 . 1–4 . 2003 . 1–4 . 10.2165/00042310-200319100-00001 . 195230977 .
  14. Web site: Sulfasalazine. The American Society of Health-System Pharmacists. 8 December 2016. live. https://web.archive.org/web/20161221012800/https://www.drugs.com/monograph/sulfasalazine.html. 21 December 2016.
  15. Cevallos SA, Lee JY, Velazquez EM, Foegeding NJ, Shelton CD, Tiffany CR, Parry BH, Stull-Lane AR, Olsan EE, Savage HP, Nguyen H, Ghanaat SS, Byndloss AJ, Agu IO, Tsolis RM, Byndloss MX, Bäumler AJ . 5-Aminosalicylic Acid Ameliorates Colitis and Checks Dysbiotic Escherichia coli Expansion by Activating PPAR-γ Signaling in the Intestinal Epithelium . mBio . 12 . 1 . e03227–20 . January 2021 . 33468700 . 7845635 . 10.1128/mBio.03227-20 . Ehrt S .
  16. Book: Nakashima J, Preuss CV . Mesalamine (USAN) . 2022 . http://www.ncbi.nlm.nih.gov/books/NBK551714/ . StatPearls . Treasure Island (FL) . StatPearls Publishing . 31869178 . 1 September 2022 .
  17. Iacucci M, de Silva S, Ghosh S . Mesalazine in inflammatory bowel disease: a trendy topic once again? . Canadian Journal of Gastroenterology . 24 . 2 . 127–133 . February 2010 . 20151072 . 2852235 . 10.1155/2010/586092 . free .
  18. Web site: Substance Name: Mesalamine [USAN:USP] ]. ChemIDplus . 2 October 2020.
  19. Web site: Mesalamine Uses, Side Effects & Warnings . Drugs.com . 30 August 2019 . 2 October 2020.

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