Sucralfate

Sucralfate, sold under various brand names, is a medication used to treat stomach ulcers, gastroesophageal reflux disease (GERD), radiation proctitis, and stomach inflammation and to prevent stress ulcers.[2] Its usefulness in people infected by H. pylori is limited. It is used by mouth (for ulcers of the upper gastrointestinal tract) and rectally (for radiation proctitis).[3][4]

Common side effects include constipation.[3] Serious side effects may include bezoar formation and encephalopathy. Use appears to be safe in pregnancy and breastfeeding. How it works is unclear but is believed to involve binding to the ulcer and protecting it from further damage.[3]

Sucralfate was approved for medical use in the United States in 1981.[3] It is available as a generic medication.[5][6] In 2023, it was the 240th most commonly prescribed medication in the United States, with more than 1million prescriptions.[7][8]

Medical uses

Sucralfate is used for the treatment of active duodenal ulcers not related to the use of nonsteroidal anti-inflammatory drugs (NSAIDs), as the mechanism behind these ulcers is due to acid oversecretion.[9] In the United States, sucralfate is not approved by the Food and Drug Administration for gastric ulcers, but is widely used because of evidence of efficacy.[10] The use for sucralfate in peptic ulcer disease has diminished recently, but it is still the preferred agent for stress ulcer prevention.[11][12][13][14]

Side effects

The most common side effect seen is constipation (2–3%). Less commonly reported side effects (<0.5%) include flatulence, headache, hypophosphatemia, xerostomia (dry mouth), and bezoar formation.[24][25][26] Use of this drug is not recommended for people with chronic kidney failure, as it might cause aluminium accumulation and toxicity. A few well-controlled studies have been carried out investigating the safety and efficacy of sucralfate in children and pregnant women (Pregnancy Category B).[9][27][28]

Mechanism of action

Sucralfate is a locally acting substance that in an acidic environment (pH < 4) reacts with hydrochloric acid in the stomach to form a cross-linking, viscous, paste-like material capable of acting as an acid buffer for as long as 6 to 8 hours after a single dose.[29] It also attaches to proteins on the surface of ulcers, such as albumin and fibrinogen, to form stable insoluble complexes. These complexes serve as protective barriers at the ulcer surface, preventing further damage from acid, pepsin, and bile.[29] In addition, sucralfate prevents back diffusion of hydrogen ions, and absorbs both pepsin and bile acids.[30]

It has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.[9]

Pharmacokinetics

• Onset: 1–2 hr (initial onset for peptic ulcer disease (PUD))
• Absorption: <5% Orally
• Duration: Up to 6 hours due to high affinity for defective mucosa (PUD)
• Bioavailability: 5%, sucralfate is considered non-systemic, sucrose octasulfate: 5%, aluminum: 0.005%
• Metabolism: Not metabolized, excreted unchanged in urine
• Excretion: Primarily in feces as unchanged drug[28][32]

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