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Sucralfate

Increases barrier to acid penetration in the esophagus but has limited clinical efficacy in GERD.

A medication used to treat stomach ulcers, gastroesophageal reflux disease (GERD), radiation proctitis, and stomach inflammation and to prevent stress ulcers.

Sucralfate is a topical mucosal protective agent to control symptoms, and promotes healing of erosive, esophagitis, and prevention of symptom recurrence

A locally acting substance that in an acidic environment 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 attaches to proteins on the surface of ulcers, such as albumin and fibrinogen, to form stable insoluble complexes preventing further damage from acid, pepsin, and bile.

It is used by mouth and rectally.

Trade names Carafate

Pregnancy category B.

It is safe in pregnancy and breastfeeding.

Bioavailability 3-5%

Metabolism GI

Elimination half-life unknown

Excretion Feces, urine

Side effects include constipation, bezoar formation and encephalopathy.

It is believed to involve binding to gastrointestinal mucosa protecting it from further damage.

It prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids.

Sucralfate is used for the treatment of active duodenal ulcers that are not related to the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

The mechanism behind these other ulcers is due to acid oversecretion.

It is not FDA approved for gastric ulcers.

Other uses include:

Gastro-esophageal reflux disease during pregnancy

stress ulcer prophylaxis

measures to prevent aspiration

decreases the incidence of ventilator-associated pneumonia compared to H2-antagonists.

It is less effective for prophylaxis against gastrointestinal bleeding than either a PPI or H2-blocker.

Can be used in the treatment of corrosive esophageal burns to enhance mucosal healing and suppress stricture formation.

Utilized in proctitis from ulcerative colitis, and from radiation via sucrasulfate enema.

Treatment of anastomotic ulcer after gastric bypass surgery.

Side effects: most common side effect seen is constipation (2-3%).

Less common side effects include: flatulence, headache, hypophosphatemia, xerostomia, and bezoar formation.

With renal Insufficiency it may cause aluminum accumulation and toxicity.

It may increase the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.

Orally less than 5% is absorbed,and is considered non-systemic.

The onset of activity is 1/2-1 hr, with a duration of up to 6 hours due to high affinity for defective gastrointestinal mucosa

It is excreted unchanged in urine.

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