Sucralfate
Sucralfate
Generic Name
Sucralfate
Mechanism
- Protective film formation: Sucralfate (a complex of aluminum sucrose sulfate) precipitates at low GI pH, amassing on ulcer surfaces to create a viscous, occlusive barrier.
- Aluminum‑centric oxidation: The aluminum component catalyzes the formation of a resistant polysaccharide shield.
- Local acid/base effects: Sucralfate neutralizes pepsin activity and provides a micro‑environment favorable for epithelial regeneration.
- Immunomodulation: Reduces mucosal inflammation by local inhibition of leucocyte adhesion.
Pharmacokinetics
- Absorption: Minimal systemic absorption (least 0.001% of dose). Concentrated locally in the GI tract.
- Distribution: Primarily limited to the gastric lumen; no significant plasma distribution.
- Metabolism: Not metabolized; remains unchanged throughout the upper GI tract.
- Elimination: Excreted unchanged via feces; only a very small fraction found in urine.
- Half‑life: No meaningful systemic clearance; the drug persists in the GI lumen until passage.
> Key takeaway: With almost complete lack of systemic absorption, sucralfate’s actions are restricted to the mucosal surface, making it a safe, gastrointestinal‑specific agent.
Indications
- Peptic ulcer disease (gastric and duodenal ulcers) for prevention and treatment.
- Acid‑reflux prophylaxis in high‑risk surgical patients.
- Erosion‑preventive therapy in patients on NSAID or corticosteroid regimens.
- Treatment of radiation‑induced esophageal or gastric mucositis.
> Note: Not indicated for ulcer perforation, cancer, or for any scenario that requires direct mucosal eradication (e.g., Helicobacter pylori infection alone).
Contraindications
Contraindications
• *Hypersensitivity* to sucralfate or any component.
• *Active ulcer perforation* or severe GI bleeding: drug may worsen perforation.
• Severe *renal failure* (unless doses are reduced, as retained aluminum is a concern).
Warnings
• Aluminum accumulation: Long‑term use >5 weeks may increase serum aluminum; monitor if chronic usage.
• Interactions: Reduces bioavailability of orally administered drugs (e.g., *tetracyclines, sulfamethoxazole, ranitidine*) due to precipitation in GI tract. Separate dosing times by at least 2 hours.
• Use in pregnancy: Generally considered category B; caution recommended.
Dosing
- Adult dosing: 1 g orally, 4 times daily (every 6 hours), preferably with meals or immediately after meals to enhance film formation.
- Pediatric dosing: 20–60 mg/kg/meal, divided 4 times daily, with careful attention to dosing frequency.
- Enteral feeding/IV: Sucralfate can be given enterally through a feeding tube; do not give via IV except in very rare, case‑by‑case situations where short‑term therapy is required (IV route is not FDA‑approved).
- Pulse dosing: For ulcer prevention in high‑risk surgical settings, 1 g nightly pre‑operatively and 1 g every 12 hours for the first 3 days post‑op.
Administration Tips
• Avoid concurrent citrate or other substances that could chelate aluminum.
• Separate dosing from other oral medications (e.g., *NSAIDs, PPIs*, and antibiotics) by at least 2 hours to prevent precipitation.
Adverse Effects
| Category | Typical Adverse Effects |
| GI | Constipation, nausea, flatulence, dry mouth, abdominal pain. |
| Systemic | Rarely, aluminum overload (neurologic deficits, osteomalacia). |
| Allergic | Rash, itching, angioedema; treat as with any drug allergy. |
| Drug‑Drug Interactions | Decreased absorption of other oral drugs (tetracyclines, sulphadiazine). |
> Serious: Aluminum-induced encephalopathy, seizures, and fatigue in chronic users.
Monitoring
- Baseline renal function (serum creatinine, eGFR) before initiating therapy and periodically every 3–6 months if >5 weeks of use.
- Aluminum levels in serum if patient is on long‑term sucralfate or has pre‑existing renal dysfunction.
- Stool occult blood after 4–6 weeks if ulcer healing not evident.
- Assess GI symptoms (constipation, pain) at each follow‑up visit for dose adjustment.
Clinical Pearls
1. Supersize the “film” – Sucralfate’s protective film works best during the first 2–3 hours after dose; avoid meals that are too heavy; small, frequent meals enhance contact and adhesion.
2. Separate from PPIs – Although PPIs reduce acid, they can interfere with sucralfate’s acid‑dependent film formation; dose therapy 2 hours apart to maximize benefit.
3. Wordscapes – Sucralfate is sometimes mistakenly thought to “stick to ulcers” but actually adhesive to the ulcer base; do not expect to “inject” it to ulcer site.
4. Kidney‑friendly – In patients with moderate CKD, the sucralfate dose is reduced to ½‑dose to minimize systemic aluminum exposure.
5. Number‑of‑doses “rule” – 4 doses/day ensures enough “coverage” across gastric secretion cycles and protects against nighttime reflux.
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