What is the recommended use and dosage of mesalamine (mesalamine) for treating ulcerative colitis and Crohn's disease?

Mesalamine for Ulcerative Colitis Management

For ulcerative colitis, standard-dose mesalamine (2-3 g/day) is strongly recommended as first-line therapy for both induction and maintenance of remission, with higher doses (>3 g/day) recommended for patients with moderate disease activity or suboptimal response. 1

Dosing Recommendations

Induction of Remission

• Adults:
  • Mild-moderate UC: 2.4-4.8 g once daily 2
  • For moderate disease: 4.8 g/day (high-dose) is more effective than 2.4 g/day 3
  • Left-sided or distal disease may require higher doses 4

Maintenance of Remission

• Adults: 2.4 g once daily 2
• Once-daily dosing is as effective as twice-daily dosing and improves adherence 5

Pediatric Dosing (for patients ≥24 kg who can swallow tablets whole) 2

• Initial treatment (Weeks 0-8):
  • 24-35 kg: 2.4 g daily

  • 35-50 kg: 3.6 g daily

  • 50 kg: 4.8 g daily

• Maintenance (After Week 8):
  • 24-35 kg: 1.2 g daily

  • 35-50 kg: 2.4 g daily

  • 50 kg: 2.4 g daily

Administration Instructions

• Swallow tablets whole; do not split or crush 2
• Take with food 2
• Drink adequate fluids to prevent nephrolithiasis 2

Disease-Specific Recommendations

Extensive Ulcerative Colitis

• Oral mesalamine (standard-dose 2-3 g/day) 6
• Consider adding rectal mesalamine for enhanced efficacy 1

Left-sided UC/Proctosigmoiditis

• Combination of oral and rectal mesalamine is more effective than oral therapy alone 1
• Balsalazide 6.75 g/day may be more effective than standard-dose mesalamine 2.4 g/day, but high-dose mesalamine (4.8 g/day) may provide similar benefit 4

Ulcerative Proctitis

• Mesalamine suppositories are first-line therapy 1
• If intolerant to suppositories, rectal corticosteroid therapy is recommended 1

Management of Suboptimal Response

• For patients with inadequate response to standard-dose:
  • Increase to high-dose mesalamine (>3 g/day) 6, 7
  • Add rectal mesalamine to oral therapy 1
  • For patients who relapse on low-dose maintenance (1.5-2.25 g/day), increasing to 4.0 g/day can achieve clinical improvement in 66% of patients 7
• If refractory to optimized 5-ASA therapy:
  • Add oral prednisone or budesonide MMX 6

Monitoring

• Evaluate renal function prior to initiation and periodically during therapy 2
• Monitor for signs of mesalamine-induced acute intolerance syndrome (symptoms may mimic UC flare) 2
• Watch for hypersensitivity reactions including myocarditis and pericarditis 2
• Consider periodic liver function tests 2

Adverse Effects

• Most common adverse reactions in adults (≥2%): headache, flatulence, abnormal liver function tests, abdominal pain, and diarrhea 2
• Most common adverse reactions in pediatric patients (≥5%): abdominal pain, upper respiratory tract infection, vomiting, anemia, headache, and viral infection 2
• Rare but serious: interstitial nephritis, severe cutaneous adverse reactions 2

Clinical Efficacy

• High-dose mesalamine (>3 g/day) is superior to low-dose (<2 g/day) for induction of remission (RR 0.81,95% CI 0.71-0.92) 6
• Standard-dose (2-3 g/day) is superior to low-dose for induction (RR 0.88,95% CI 0.79-0.99) and maintenance of remission (RR 0.63,95% CI 0.55-0.78) 6
• No significant benefit of high-dose over standard-dose for maintenance of remission (RR 0.93,95% CI 0.71-1.17) 6

Important Considerations

• Mesalamine is not FDA-approved for Crohn's disease, though limited data suggest potential benefit in active and quiescent Crohn's disease 4
• Patients with left-sided or distal disease may require higher doses or combination with rectal therapy 4
• Mesalamine is effective in sulfasalazine-intolerant patients 4