What are the relative potencies of available mucosal corticosteroids (corticosteroids), such as budesonide, prednisolone, and fluticasone, for treating gastrointestinal ulcers?

Relative Potencies of Mucosal Corticosteroids for Gastrointestinal Ulcers

Beclomethasone dipropionate (BDP) has the highest topical anti-inflammatory potency among mucosal corticosteroids for gastrointestinal ulcers, followed by budesonide, with prednisolone having the lowest mucosal potency but highest systemic effects. 1

Comparison of Available Mucosal Corticosteroids

Beclomethasone Dipropionate (BDP)

• Highest topical anti-inflammatory effect
• High first-pass metabolism (low systemic bioavailability)
• Dosing: 5 mg/day as prolonged release tablet for 4 weeks
• Efficacy: Similar to 5-ASA for inducing remission in mild to moderate ulcerative colitis
• Clinical evidence shows BDP 5 mg is as effective as prednisolone for clinical response (64.6% vs 66.2%) with fewer systemic effects 1

Budesonide

• High topical anti-inflammatory activity with minimal systemic absorption
• Available in multiple formulations:
  • Budesonide MMX: Designed for release throughout the colon
  • Controlled ileal release (CIR): Primarily released in distal ileum and right colon 2
• Dosing: 9 mg/day for 8 weeks for induction of remission
• Efficacy: Moderate quality evidence supports its use, particularly effective for left-sided colitis 3
• Significantly more effective than placebo (15% vs 7% remission rates) 3

Prednisolone

• Highest systemic effects with significant side effect profile
• Lowest mucosal-specific potency
• Dosing: 40 mg daily tapering over 6-8 weeks
• Efficacy: Superior to placebo for inducing remission in UC (RR of no remission 0.65; 95% CI 0.45 to 0.93) 1
• Causes significant adrenal suppression compared to topical steroids 1, 4

Potency Comparison Based on Clinical Outcomes

1. Topical Anti-inflammatory Potency: BDP > Budesonide > Prednisolone
2. Systemic Effects: Prednisolone > BDP > Budesonide
3. Morning Cortisol Suppression: Prednisolone (significant) > BDP (minimal) > Budesonide (negligible) 4, 3

Clinical Application Algorithm

For Mild to Moderate Ulcerative Colitis:

1. First-line: 5-ASA (oral and/or topical)
2. If 5-ASA fails or is not tolerated:
   • Preferred: Budesonide MMX 9 mg daily for 8 weeks or BDP 5 mg daily for 4 weeks 1
   • Consider disease location: Budesonide MMX is most effective for left-sided disease 3

For Moderate to Severe Ulcerative Colitis:

1. First-line: Prednisolone 40 mg daily with tapering over 6-8 weeks 1
2. If systemic effects are concerning: Consider BDP as it has similar efficacy to prednisolone with fewer systemic effects 1

For Ulcerative Proctitis:

• Topical corticosteroids (suppositories/foam/enema) are effective
• Budesonide 4 mg suppository is more effective than 2 mg for inducing clinical remission 1

Important Clinical Considerations

• Adrenal Suppression: While budesonide and BDP can suppress morning cortisol to some extent, mean values typically remain within normal range, unlike with prednisolone 3

• Duration of Therapy: Mucosal corticosteroids are not recommended for long-term maintenance therapy due to potential corticosteroid-related adverse effects 2

• Formulation Selection:

  • For distal disease: Consider topical preparations
  • For left-sided colitis: Budesonide MMX shows highest efficacy 3
  • For extensive colitis: Systemic prednisolone may be necessary

• Common Adverse Events: Worsening ulcerative colitis, headache, pyrexia, insomnia, back pain, nausea, abdominal pain, diarrhea, flatulence and nasopharyngitis 3

• Monitoring: For patients on long-term therapy, monitor for systemic effects and adrenal suppression

By understanding the relative potencies and specific formulations of mucosal corticosteroids, clinicians can optimize treatment selection to maximize therapeutic benefit while minimizing systemic side effects for patients with gastrointestinal ulcers.