Usage
Sucralfate is prescribed for the short-term (up to 8 weeks) treatment of active duodenal ulcers. It is also used for maintenance therapy following healing of acute duodenal ulcers to reduce ulcer recurrence. Off-label uses include treatment of gastric ulcers, stress ulcer prophylaxis, treatment of oral ulcerations and dysphagia in patients with epidermolysis bullosa, and treatment of oral complications of chemotherapy in bone marrow transplant recipients. Sucralfate falls under the pharmacological classification of a mucosal protectant. It creates a protective barrier over ulcers, shielding them from stomach acid and other irritants to facilitate healing.
Alternate Names
Sucralfate is also known by its brand name, Carafate. There are no widely recognized international or regional variations of the name.
How It Works
Pharmacodynamics: Sucralfate acts locally in the stomach and duodenum. It selectively binds to the base of ulcers, forming a protective barrier against pepsin, acid, and bile salts, thus promoting ulcer healing.
Pharmacokinetics: Sucralfate is minimally absorbed systemically, with only small amounts of aluminum hydroxide being absorbed. It is primarily eliminated through the gastrointestinal tract.
Mode of Action: In the acidic environment of the stomach, sucralfate undergoes cross-linking and polymerization, forming a viscous, sticky paste that adheres to the ulcer surface. This physical barrier shields the ulcer from the damaging effects of acid, pepsin, and bile. The binding to ulcer proteins is thought to be electrostatic in nature.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Sucralfate does not bind to specific receptors, inhibit enzymes, or modulate neurotransmitters. Its action is primarily physical.
Elimination Pathways: Sucralfate is mostly eliminated unchanged in the feces. The small amount of aluminum hydroxide absorbed is primarily excreted by the kidneys.
Dosage
Standard Dosage
Adults:
- Active Duodenal Ulcer: 1 g orally four times a day on an empty stomach (1 hour before meals and at bedtime) for 4-8 weeks.
- Duodenal Ulcer Maintenance: 1 g orally twice a day.
- Gastric Ulcer (Off-label): 1 g orally four times a day.
Children:
The safety and efficacy in children have not been fully established. Pediatric dosing is determined by the doctor on a case-by-case basis and is considered off-label. Doses ranging from 40-80 mg/kg/day divided every 6 hours have been used.
Special Cases:
- Elderly Patients: Start at the lower end of the dosing range and titrate as needed, monitoring for adverse effects and renal function.
- Patients with Renal Impairment: Use with caution. Aluminum accumulation may occur. Close monitoring of serum aluminum levels is recommended, particularly for patients receiving dialysis.
- Patients with Hepatic Dysfunction: No dosage adjustment is typically necessary.
- Patients with Comorbid Conditions: Monitor blood glucose in patients with diabetes, especially those receiving the oral suspension.
Clinical Use Cases
Sucralfate does not have labeled indications for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its use in these settings is limited.
Dosage Adjustments
Dose adjustments may be necessary in patients with renal impairment. If creatinine clearance is less than 30 mL/min, consider reducing the dose and monitoring aluminum levels.
Side Effects
Common Side Effects
Constipation is the most common side effect. Diarrhea, dry mouth, nausea, vomiting, gastric discomfort, indigestion, and flatulence may also occur.
Rare but Serious Side Effects
Bezoar formation (especially in patients with underlying conditions or receiving enteral feedings), hypersensitivity reactions (including anaphylaxis, rash, itching, swelling), and severe allergic reactions (rare).
Long-Term Effects
Aluminum toxicity (including osteomalacia, encephalopathy) is a potential concern with long-term use, especially in patients with renal impairment.
Adverse Drug Reactions (ADR)
Serious ADRs include bezoar formation, allergic reactions, and aluminum toxicity.
Contraindications
Hypersensitivity to sucralfate or its components.
Drug Interactions
Sucralfate can reduce the absorption of several medications, including:
- Antacids: Administer at least 30 minutes apart.
- Ciprofloxacin, norfloxacin, ofloxacin: Administer 2 hours apart.
- Digoxin: Administer 2 hours apart.
- Ketoconazole: Administer 2 hours apart.
- Levothyroxine: Administer 2 hours apart.
- Phenytoin: Administer 2 hours apart.
- Tetracycline: Administer 2 hours apart.
- Ranitidine: Administer 2 hours before or 30 minutes after.
- Furosemide: May reduce diuretic and antihypertensive effects. Monitor closely.
- Gemifloxacin: May decrease gemifloxacin levels.
It is important to note that many medications, particularly those involving metal ions, can have reduced absorption if co-administered with sucralfate.
Pregnancy and Breastfeeding
Sucralfate is classified as Pregnancy Category B (old classification system). It is considered relatively safe to use during pregnancy due to minimal systemic absorption. Limited data exists on breastfeeding, but it is generally considered safe due to minimal absorption.
Drug Profile Summary
- Mechanism of Action: Forms a protective barrier over ulcers, shielding them from acid and promoting healing.
- Side Effects: Constipation, diarrhea, dry mouth, nausea.
- Contraindications: Hypersensitivity to sucralfate.
- Drug Interactions: Numerous drug interactions due to chelation and reduced absorption. See above for specifics.
- Pregnancy & Breastfeeding: Generally considered safe.
- Dosage: 1 g four times a day for active duodenal ulcer, 1 g twice daily for maintenance.
- Monitoring Parameters: Renal function (especially in patients with pre-existing renal disease), serum aluminum levels (long-term use or renal impairment), blood glucose (diabetes).
Popular Combinations
Sucralfate is often used alone. While antacids can be used for symptom relief, they should be administered at least 30 minutes before or after sucralfate.
Precautions
- General Precautions: Monitor renal function and serum aluminum levels, especially in patients with renal impairment. Monitor blood glucose in diabetic patients.
- Specific Populations: Monitor for bezoar formation in patients with delayed gastric emptying or receiving enteral feedings.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Sucralfate?
A: For adults with active duodenal ulcers, the recommended dose is 1 gram four times daily on an empty stomach. For maintenance therapy, the dose is 1 gram twice daily.
Q2: How does Sucralfate work?
A: Sucralfate forms a protective barrier over ulcers, protecting them from acid, pepsin, and bile salts.
Q3: What are the common side effects of Sucralfate?
A: Constipation is the most common side effect. Diarrhea, nausea, and dry mouth may also occur.
Q4: Can Sucralfate be used during pregnancy?
A: Sucralfate is generally considered safe to use during pregnancy due to minimal systemic absorption.
Q5: What are the major drug interactions with Sucralfate?
A: Sucralfate can decrease the absorption of many medications, including antacids, some antibiotics (ciprofloxacin, norfloxacin, ofloxacin, tetracycline), digoxin, ketoconazole, levothyroxine, and phenytoin.
Q6: What precautions should be taken in patients with renal impairment?
A: Use with caution in patients with renal impairment as aluminum accumulation may occur. Monitor serum aluminum levels, especially in patients on dialysis.
Q7: How should Sucralfate be administered?
A: Administer orally on an empty stomach, at least 1 hour before meals and at bedtime. Antacids can be used for symptom relief, but should not be taken within 30 minutes before or after sucralfate.
Q8: What is the duration of treatment for duodenal ulcers with Sucralfate?
A: Treatment typically lasts 4-8 weeks, but may be extended up to 12 weeks in resistant cases.
Q9: Can Sucralfate be crushed or chewed?
A: No. Tablets should be swallowed whole. The suspension should be shaken well before each use.
Q10: What should patients do if they miss a dose of Sucralfate?
A: They should take the missed dose as soon as they remember, unless it is close to the time for the next dose. They should not double the dose.
