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Sucralfate, marketed as Carafate in the U.S., is an oral gastrointestinal medication indicated for the short term treatment of active duodenal ulcers. Sucralfate can also be used for the treatment of gastroesophageal reflux disease (GERD) and stress ulcers. Unlike other classes of medications used for the treatment of peptic ulcers, sucralfate is a sucrose sulfate-aluminium complex that binds to the ulcer, creating a physical barrier that protects the gastrointestinal tract from stomach acid and prevents the degradation of mucus. It also promotes bicarbonate production and acts like an acid buffer with cytoprotective properties. Sucralfate is marketed multiple countries including as Asicot in India, Disuo in China and Citogel in Italy.

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. 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. In addition, it prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. Recently, it has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.

Clinical uses
Currently, sucralfate is FDA approved for the treatment of active duodenal ulcers not related to NSAID usage, as the mechanism behind these ulcers is due to acid oversecretion. It is not FDA approved for gastric ulcers, as the main mechanism of gastric ulcers is not due to acid oversecretion but rather from diminished protection. The use of sucralfate in peptic ulcer disease has diminished recently, but it remains one of the preferred agents for stress ulcer prophylaxis.


 * Active duodenal ulcer not related to NSAID use
 * Maintenance therapy for resolved duodenal ulcers
 * Gastric ulcer not related to NSAID use and gastritis due to GERD. Triple combination therapy with lansoprazole + cisapride + sucralfate can significantly improve symptoms and quality of life and was more cost-effective than ranitidine combination group.
 * Aphthous ulcer and stomatitis due to radiation or chemotherapy.
 * Proctitis from radiation or ulcerative colitis.
 * Gastro-esophageal reflux disease during pregnancy -- first-line drug therapy combined with lifestyle and diet modification.
 * Stress ulcer prophylaxis—The use of sucralfate rather than H2 antagonists for stress ulcer prophylaxis, and measures to prevent aspiration, such as semirecumbent positioning or continuous subglottic suctioning, have all been shown to reduce the risk of ventilator-associated pneumonia (VAP).
 * Prevention of stricture formation—Sucralfate has an inhibitory effect on stricture formation in experimental corrosive burns and can be used in the treatment of corrosive esophageal burns to enhance mucosal healing and suppress stricture formation
 * Rectal bleeding and its management after irradiation for uterine cervical cancer
 * Grade 1 bleeding experienced immediate relief with sucrasulfate enema for 1 month.
 * Grade 2 bleeding, sucrasulfate enema and/or coagulation were effective.
 * Grade 3 bleeding lasted for 1 year despite frequent transfusions and coagulation.
 * Grade 2 and 3 rectal bleeding occurred in 8.5% of patients. The most significant risk factor was the ICRU-CRBED. Prompt treatment with a combination of sucrasulfate enema and coagulation is effective in controlling Grade 1 and 2 rectal bleeding without the development of fistula or stricture.

Adverse reactions
The most common side effect seen while using sucralfate is constipation (2-3%). Less commonly reported (<0.5%) include flatulence, headache, hypophosphatemia, xerostomia (dry mouth), and bezoar formation.

Use in Renal Impaired and Hepatic Impaired Populations
Although manufacturer did not provide dose adjustment in the use of Sucralfate in the renal impaired and hepatic impaired populations, it recommends the use of Sucralfate with caution in people with chronic kidney failure, as it might cause aluminium accumulation and toxicity.

Sucralfate is not known to be metabolized by the liver.

Pregnancy and Lactation
There is a limited number of well-controlled studies investigating the safety and efficacy of sucralfate in children and pregnant women. It is not known whether sucralfate is excreted in breast milk following oral administration due to its poor absorption.

Pharmacokinetics
Onset: 1-2 hr (initial onset for peptic ulcer disease (PUD))

Absorption: <5% (PO)

Duration: Up to 6 hours due to high affinity for defective mucosa (PUD)

Bioavailability: 5% as sucralfate is considered non-systemic, sucrose octasulfate: 5%, aluminum:0.005%

Metabolism: Not metabolized, excreted unchanged in urine

Excretion: Primarily in urine as unchanged drug