What is sucralfate?

Sucralfate (Carafate): A Comprehensive Overview

Sucralfate is a non-systemically absorbed aluminum hydroxide complex that forms a protective barrier at ulcer sites, primarily used for the treatment of duodenal ulcers with healing rates of over 90% compared to 58% with placebo. 1, 2

Mechanism of Action

Sucralfate works through local rather than systemic action:

• Forms an ulcer-adherent complex with proteinaceous exudate at ulcer sites 1
• Creates a physical barrier that protects against acid, pepsin, and bile salts 1, 3
• Inhibits pepsin activity in gastric juice by approximately 32% 1
• Provides acid-neutralizing capacity (14-16 mEq per 1g dose) 1
• Binds to both damaged and intact mucosa 3

Pharmacokinetics

• Minimal systemic absorption (only 3-5% absorbed from GI tract) 1, 4
• Excreted primarily unchanged in feces (>90%) 4
• Remains at gastric ulcer sites for up to six hours 4

Clinical Applications

FDA-Approved Uses

• Short-term treatment of duodenal ulcers (up to 8 weeks) 4

Other Clinical Uses

• Treatment of NSAID-associated duodenal ulcers (particularly when NSAID is discontinued) 5
• Investigated for radiation proctitis management 5
• Used for stress ulcer prophylaxis in critically ill patients 6

Efficacy

• Duodenal Ulcers: 91.7% healing rate after 4 weeks (vs. 58.1% with placebo) 2
• Gastric Ulcers: Effective but with less impressive healing rates compared to duodenal ulcers 4
• Stress Ulcer Prophylaxis: Associated with lower incidence of nosocomial pneumonia compared to H2-receptor antagonists 6
• Radiation-Induced Diarrhea: Mixed results, with some European trials showing benefit but others showing no improvement or worsening of GI symptoms 6, 5

Dosing

• Standard dose: 1g four times daily, one hour before meals and at bedtime 4
• Prophylactic dose for duodenal ulcer recurrence: 2g daily 7

Safety Profile

• Well-tolerated due to minimal systemic absorption 7
• Most common side effects:
  • Constipation (2-4% of patients) 7, 4
  • Dry mouth (xerostomia) (1%) 4
  • Skin eruptions (0.6%) 4
• No significant drug-drug interactions reported 4

Comparative Efficacy

• Similar efficacy to cimetidine and intensive antacid therapy for duodenal and gastric ulcers 7, 4
• For stress ulcer prophylaxis, associated with lower mortality rate (OR = 0.73; 95% CI 0.54–0.97) relative to antacids and H2-receptor antagonists 6
• Lower risk of ventilator-associated pneumonia compared to H2-receptor antagonists (16.2% vs 19.1%) 6

Clinical Considerations and Pitfalls

• Not effective for treatment or prevention of NSAID-related gastric ulcers 5
• PPIs are generally preferred over sucralfate for therapy and prophylaxis of NSAID and ASA-associated GI injury 5
• When used for stress ulcer prophylaxis, sucralfate may be preferable to H2-receptor antagonists due to lower risk of ventilator-associated pneumonia 6
• Additive or synergistic effects with cimetidine or intensive antacid therapy have not been well-studied 4

Sucralfate represents a unique approach to ulcer treatment through its local protective effects rather than acid suppression, making it particularly valuable in settings where systemic effects need to be minimized.