Mesalamine
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Mesalamine (5-aminosalicylic acid, 5-ASA)
Asacol HD, Pentasa, Lialda, Apriso, Delzicol, Rowasa (rectal), Canasa (suppository)
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Summary
Common uses
Ulcerative colitis (induction and maintenance)0, Mild Crohn's colitis (limited evidence; less effective than in UC)0
Pharmacy
Starting dose
Active UC: Lialda 2.4-4.8 g PO once daily, Apriso 1.5 g PO once daily; maintenance 1.2-2.4 g/d; rectal Rowasa enema 4 g HS for distal disease; Canasa 1 g suppository HS for proctitis
Preparations
Multiple non-bioequivalent oral formulations (pH-, time-, and moisture-dependent release); rectal enema 4 g/60 mL; 1 g rectal suppository
US FDA Max
Formulation-specific; ~4.8 g/d typical maximum oral
Pharmacology
Routes
Oral, rectal
Onset
Symptomatic improvement 2-4 weeks
Duration
24 hours (most ER formulations)
Half-life
~5-10 hours (5-ASA)[1]
Bioavailability
Highly formulation-dependent; the goal is colonic delivery with minimal systemic exposure[1]
Pregnancy
Generally considered safe at standard doses; benefits typically outweigh in active IBD.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Mesalamine's mechanism in IBD is incompletely characterized; proposed actions include inhibition of NF-κB-driven cytokine production, scavenging of reactive oxygen species, modulation of arachidonic acid metabolism (inhibition of both lipoxygenase and cyclooxygenase pathways), and PPARγ activation in colonic epithelium.0 The various oral formulations (Asacol HD pH-dependent, Pentasa ethylcellulose time/moisture, Lialda MMX multi-matrix) achieve different colonic delivery patterns; rectal formulations are highly effective for distal disease. Renal monitoring (interstitial nephritis is rare but well-documented) is standard practice during chronic use[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Lialda (mesalamine), Shire/Takeda, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022000s022lbl.pdf