Mesalamine

5-aminosalicylate (5-ASA), IBD medication, Anti-inflammatory

Mesalamine (5-aminosalicylic acid, 5-ASA)

Asacol HD, Pentasa, Lialda, Apriso, Delzicol, Rowasa (rectal), Canasa (suppository)

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Summary

Classes

5-aminosalicylate (5-ASA), IBD medication, Anti-inflammatory

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)

Bioavailability

Highly formulation-dependent; the goal is colonic delivery with minimal systemic exposure

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.