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mesalamine (Asacol, Rowasa, Pentasa, Pentasacaps, Lialda, Apriso, Canasa, Delzicol)

Tradenames: Asacol, Rowasa, Pentasa, Apriso. Indication: - chronic inflammatory bowel disease - ulcerative colitis - ulcerative proctitis [7] * activity minimal in Crohn's disease [8] Contraindications: pregnancy-category B safety in lactation ? Dosage: 1) Anascol: 800 mg (2 tabs) PO TID 2) Pentasa: 1000 mg (4 tabs) PO QID 3) Lialda 2-4 tablets QD [5] 4) Apriso QD 4 retention enema: 60 mL (4 g) QHS, retained overnight (approximately 8 hours) 5) suppository: insert 1 BID Tabs: 250 mg (Pentasa) & 400 mg (Anascol). Tab (delayed time release): 400 mg. Lialda 1.2 g MMX Multi-Matrix System QD dosing [6] Suppository: 500 mg. Enema: 4 g/60 mL. Pharmacokinetics: 1) mesalamine is poorly absorbed as a rectal enema 2) excreted in the feces 3) mesalamine tablets release drug in the terminal ileum & distally 4) mesalamine capsules release drug throughout the entire GI tract 5) acetylated in the mucosal wall of the gut & by the liver 6) excreted in the urine & feces Adverse effects: 1) common (> 10%) - headache, abdominal pain, cramps, flatulence, gas 2) less common (1-10%) - alopecia 3) uncommon (< 1%) - anal irritation, acute intolerance syndrome (bloody diarrhea, severe abdominal cramps, severe headache) - pericarditis - pancreatitis - hypersensitivity colitis [8] 4) other - nephrotoxicity, interstitial nephritis [8] - nausea (common) [8] Mechanism of action: 1) effect appears to be topical rather than systemic 2) may diminish inflammation by blocking cyclo-oxygenase & inhibiting prostaglandin production in the colon Lialda cost about $275-$550 per month... compared to $236 for Asacol (2007)

Interactions

drug adverse effects of NSAIDs monitor with non steroidal anti-inflammatory agents (NSIADs)

Related

inflammatory bowel disease

General

5-aminosalicylate (5-ASA)

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 356
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Prescriber's Letter 14(3): 2007 Drug Therapy for Ulcerative Colitis Detail-Document#: 230308 (subscription needed) http://www.prescribersletter.com
  6. Kamm MA et al, Once daily, high concentration MMX mesalamine in active ulcerative colitis. Gastroenterology 2007, 132:66 PMID: 17241860
  7. Deprecated Reference
  8. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015