II. Indications: Inflammatory Bowel Disease

III. 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

IV. Dosing: Ulcerative Colitis (Adults)

  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

V. 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)

VI. 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

VII. Drug Interactions

  1. False positive Urine Metanephrines

VIII. Safety

  1. Pregnancy Category C
  2. Unknown safet in Lactation

X. 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]

Images: Related links to external sites (from Bing)

Related Studies

Cost: Medications

mesalamine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
MESALAMINE 1,000 MG SUPP Generic $2.21 each
MESALAMINE 4 GM/60 ML ENEMA Generic $0.13 per ml
MESALAMINE 4 GM/60 ML KIT Generic $116.13 each
MESALAMINE 800 MG DR TABLET Generic $5.99 each
MESALAMINE DR 1.2 GM TABLET Generic $2.22 each
MESALAMINE DR 400 MG CAPSULE Generic $2.53 each
MESALAMINE ER 0.375 GRAM CAP Generic $0.89 each
MESALAMINE ER 500 MG CAPSULE Generic $4.64 each
pentasa (on 2/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
PENTASA 250 MG CAPSULE $2.91 each
PENTASA 500 MG CAPSULE Generic $4.64 each
lialda (on 6/14/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
LIALDA DR 1.2 GM TABLET Generic $2.05 each
delzicol (on 7/19/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
DELZICOL DR 400 MG CAPSULE Generic $2.11 each

Ontology: mesalamine (C0127615)

Definition (NCI) An agent derived from sulfasalazine, an antiinflammatory agent. Mesalamine may reduce inflammation through inhibition of cyclooxygenase and prostaglandin production. Following rectal or oral administration, only a small amount of mesalamine is absorbed; the remainder, acting topically, reduces bowel inflammation, diarrhea, rectal bleeding and stomach pain. (NCI04)
Definition (MSH) An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D019804
SnomedCT 387501005, 346319009, 317439005, 363629007, 86977007
English Mesalamine, Mesalazine duplicate deleted, 5 Aminosalicylic Acid, 5-Aminosalicylic Acid, 5-Amino-2-hydroxybenzoic Acid, m Aminosalicylic Acid, m-Aminosalicylic Acid, meta Aminosalicylic Acid, meta-Aminosalicylic Acid, mesalamine (medication), mesalamine (Rowasa), MESALAMINE, Mesalamine [Chemical/Ingredient], 5 asa, m-aminosalicylic acid, 5-asa, asa 5, mesalazine, Mesalazine duplicate deleted (product), Mesalamine product (product), 5-aminosalicylic acid (substance), 5-ASA, 5-Aminosalicylic acid, Fisalamine, m-Aminosalicylic acid, Mesalamine (substance), 5-aminosalicylic acid, 5ASA - Mesalazine, Mesalamine (product), Mesalamine product, Mesalamine product (substance), Mesalazine duplicate deleted (substance), Mesalazine, mesalamine
Swedish Mesalamin
Czech mesalazin, mesalamin
Finnish Mesalatsiini
Russian MEZALAMIN, MEZALAZIN, 5-AMINOSALITSILAT, 5-АМИНОСАЛИЦИЛАТ, МЕЗАЛАЗИН, МЕЗАЛАМИН
Spanish mesalazina, mesalamina, mesalazina (sustancia), 5-ASA, mesalazina (producto), mesalazina (duplicado borrado) (producto), mesalamina, producto (producto), mesalamina, producto, mesalazina (duplicado borrado), mesalamina (producto), mesalamina (sustancia), fisalamina, ácido 5-aminosalicílico, ácido m-aminosalicílico, Mesalacina, Mesalamina
Japanese メサラミン, ペンタサ, 5-アミノサリチル酸, フィサラミン(メサラジン), メサラジン
French Acide 5-amino-salicylique, Acide 5-aminosalicylique, Mésalazine, Fisalamine, Mésalamine
Polish Mesalamina, Mesalazyna, 5-aminosalicylan, Kwas 5-aminosalicylowy, 5-ASA
German Mesalamine
Italian Mesalamina
Portuguese Mesalamina, Mesalazina

Ontology: Pentasa (C0678171)

Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D019804
English pentasa, Pentasa, Allphar Brand of Mesalamine, Ferring Brand of Mesalamine, Yamanouchi Brand of Mesalamine

Ontology: Asacol (C0678172)

Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D019804
English asacol, Asacol, Byk Brand of Mesalamine, Procter & Gamble Brand of Mesalamine

Ontology: Rowasa (C0699623)

Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D019804
English rowasa, Rowasa, Solvay Brand of Mesalamine

Ontology: Lialda (C1873792)

Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
English Lialda