What is prescription mesalamine (mesalamine) used for?

Prescription Mesalamine: A First-Line Treatment for Inflammatory Bowel Disease

Mesalamine is an aminosalicylate medication primarily used for the induction and maintenance of remission in patients with mild to moderate ulcerative colitis, available in various oral and topical formulations. 1

Indications

• FDA-approved for both induction and maintenance of remission in adult patients with mild to moderately active ulcerative colitis 1
• Also indicated for treatment of mild to moderately active ulcerative colitis in pediatric patients weighing at least 24 kg 1
• First-line therapy for mild to moderate ulcerative colitis, particularly effective for distal disease (proctitis, proctosigmoiditis) 2, 3
• Can be used in Crohn's disease, though evidence is stronger for ulcerative colitis 2, 4

Formulations and Administration

Oral Formulations

• Available as delayed-release tablets, controlled-release capsules, and MMX extended-release tablets 2
• Standard dosing for adults: 2.4-4.8g daily for induction of remission 2, 1
• Maintenance dosing typically 2.4g daily 2, 1
• Once-daily dosing is as effective as multiple daily doses, improving compliance 2
• Should be taken with food to optimize absorption 1
• Tablets should be swallowed whole, not split or crushed 1

Topical Formulations

• Suppositories (1g) for proctitis (disease limited to rectum) 2, 5
• Enemas (1-4g) for left-sided colitis or proctosigmoiditis 2
• Topical therapy often combined with oral therapy for enhanced efficacy 2

Treatment Algorithms

For Distal Disease (Proctitis/Proctosigmoiditis):

1. First-line: Topical mesalamine (suppositories for proctitis, enemas for proctosigmoiditis) combined with oral mesalamine 2-4g daily 2, 5
2. If inadequate response: Increase oral mesalamine to >3g daily while continuing topical therapy 2
3. For refractory cases: Add oral prednisolone 40mg daily with gradual taper over 8 weeks 2

For Extensive Disease:

1. First-line: Oral mesalamine 2.4-4.8g daily 2, 1
2. Consider adding rectal mesalamine for enhanced efficacy 2
3. For suboptimal response: Increase to high-dose mesalamine (>3g daily) 2
4. For refractory cases: Add oral prednisone or budesonide MMX 2

Efficacy and Mechanism

• Acts locally in the intestinal mucosa to reduce inflammation 6, 4
• Systemic absorption limited to approximately 21-22% of administered dose 6
• More effective than placebo for both induction and maintenance of remission 2, 4
• Combination of oral and topical therapy more effective than either alone 2, 5
• Higher doses (>3g daily) achieve significantly higher rates of clinical and endoscopic remission 2, 3

Monitoring and Safety

• Evaluate renal function prior to initiation and periodically during therapy 6, 1
• Generally well-tolerated with fewer side effects than sulfasalazine 7, 4
• Common side effects include headache, nausea, and diarrhea 6, 7
• Rare but serious adverse effects may include renal impairment, acute and chronic interstitial nephritis 1
• Safe for long-term use in both adults and children 8, 3
• Considered safe during pregnancy, except for formulations containing dibutyl phthalate 3

Common Pitfalls to Avoid

• Underdosing: Using inadequate doses (<2.4g daily) for active disease 2, 3
• Not combining oral and topical therapy when appropriate 2, 5
• Failure to treat proximal constipation in patients with distal disease 2, 5
• Not recognizing diarrhea as a potential side effect of mesalamine 7
• Inadequate monitoring of renal function during long-term therapy 6, 1
• Poor adherence to therapy, particularly with multiple daily dosing regimens 2, 3