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Mesalamine

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Mesalamine, Sulfa-free 5-Aminosalacylic acid, Sulfa-free 5-ASA, Asacol, Pentasa, Rowasa, Mesalamine MMX, Lialda, Delzicol

  • See Also
  1. 5-Aminosalicylic Acid Derivative
  2. Sulfasalazine
  1. Ulcerative Colitis
  2. Crohns Disease (off-label use)
  • Mechanism
  1. 5-Aminosalicylic Acid Derivative
  2. Mesalamine is the active agent of the antiinflammatory Sulfasalazine
  3. Mesalamine decreases gastrointestinal inflammation via inhibition of cyclooxygenase and Prostaglandin
  4. Minimal absorption and acts locally within the bowel
  1. Background
    1. Rectal forms are preferred for Proctitis
    2. Use oral and rectal forms combined for better results where pancolitis is present
  2. Oral
    1. Active disease: 2.4 to 4.8 grams/day divided 1 to 3 times daily for 6 to 8 weeks (depending on agent)
      1. Delzicol 800 mg orally three times daily
      2. Pentasa 1 g orally four times daily (may be opened and mixed with water or applesauce)
      3. Mesalamine MMX (e.g. Lialda) 2.4 to 4.8 g orally daily with meals
      4. Asacol HD 1.6 g orally three times daily
    2. Maintenance: 1.2 to 2.4 grams/day divided 1 to 3 times daily (depending on agent)
      1. Delzicol 800 mg orally twice daily
      2. Apriso 1.5 g orally daily
      3. Mesalamine MMX (e.g. Lialda) 2.4 g orally daily
      4. Asacol HD 2.4 to 4.8 g/day orally divided three times daily
  3. Diazo-Bonded 5-ASA product Formulations (oral agents activated in colon)
    1. See Balsalazide
    2. See Olsalazine
  4. Suppository (e.g. Cantasa, for Ulcerative Proctitis)
    1. Active disease: 1000 mg once daily at bedtime
    2. Maintenance: 500 mg once to twice daily
  5. Enema (e.g. Rowasa 4 g in 60 ml, provides high descending colon concentrations)
    1. Active disease: 1 to 4 grams daily
    2. Maintenance: 2-4 grams daily to every third day
  • Dosing
  • Child
  1. Indicated in age 5 years and older
  2. Weight 17 to 32 kg
    1. Mesalamine 36 to 71 mg/kg/day (maximum 1.2 g/day)
  3. Weight 33 to 53 kg
    1. Mesalamine 37 to 61 mg/kg/day (maximum 2.0 g/day)
  4. Weight 54 to 90 kg
    1. Mesalamine 27 to 4 mg/kg/day (maximum 2.4 g/day)
  • Adverse Effects
  1. Most common
    1. Headache
    2. Abdominal Pain
    3. Fever
    4. Rash
  2. Other
    1. Interstitial Nephritis
    2. Hepatic failure (risk in preexisting liver disease)
    3. Suppositories and enemas may cause rectal irritation
    4. Phenylketonuria Risk (Apriso)
      1. Apriso contains Phenylalanine
    5. Digoxin
      1. Mesalamine may decrease levels
    6. Urine Color change
      1. Yellow-brown discolored urine
  • Drug Interactions
  1. False positive Urine Metanephrines
  • Safety
  1. Pregnancy Category C
  2. Unknown safet in Lactation
  • Resources
  1. Mesalamine Delayed Release Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ba1e3bd4-fbe0-46a5-961e-167ccb09672c
  2. Mesalamine Delayed Release Capsule (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6fd0a906-e1b5-4238-a79b-a195510ddc84
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. (2022) Treatment of Mild to Moderate Ulcerative Colitis, Presc Lett, #350406
  3. (2023) Drugs for Inflammatory Bowel Disease, Med Lett Drug Ther 65: 105-12
  4. Adams (2013) Am Fam Physician 87(10): 699-705 [PubMed]
  5. Adams (2022) Am Fam Physician 105(4): 406-11 [PubMed]
  6. Kornbluth (2010) Am J Gastroenterol 105(3): 501-23 [PubMed]