SUCRALFATE

Chemistry - A basic, aluminum complex of sucrose sulfate, sucralfate occurs as a white, amorphous powder. It is practically insoluble in alcohol or water.
Sucralfate is structurally related to heparin, but does not posses any appreciable anticoagulantactivity. It is also structurally related to sucrose, but is not utilized as a sugar by the body. Sucralfateis also known as aluminum sucrose sulfate, basic.

Storage, Stability, Compatibility

Store sucralfate tablets in tight containers at room temperature.

Pharmacology - SUCRALFATE

While the exact mechanism of action of sucralfate as an antiulcer agent is notknown, the drug has a local effect rather than a systemic one. After oral administration, sucralfatereacts with hydrochloric acid in the stomach to form a paste-like complex that will bind to theproteinaceous exudates that generally are found at ulcer sites. This insoluble complex forms abarrier at the site and protects the ulcer from further damage caused by pepsin, acid or bile.
Sucralfate may have some cytoprotective effects, possibly by stimulation of prostaglandin E2 and I2. Sucralfate also has some antacid activity, but it is believed that this is not of clinical importance.
Sucralfate does not significantly affect gastric acid output, or trypsin or pancreatic amylase activity. It may decrease the rate of gastric emptying.
Uses, Indications - Sucralfate has been used in the treatment of oral, esophageal, gastric andduodenal ulcers. It has also been employed to prevent drug-induced (e.g., aspirin) gastric erosions.

Pharmacokinetics - SUCRALFATE

Animal studies have indicated that only 3-5% of an oral dose is absorbedwhich is excreted in the urine unchanged within 48 hours. The remainder of the drug is converted tosucrose sulfate in the gut by reacting with hydrochloric acid and is excreted in the feces within 48hours. The duration of action (binding to ulcer site) may persist up to 6 hours after oral dosing.
Contraindications/Precautions - There are no known contraindications to the use of sucralfate.
Because it may cause constipation, it should be used with caution in animals where decreased intestinal transit times may be deleterious.
It is unknown if sucralfate crosses the placenta and whether it may be used safely during pregnancy. In rats, dosages up to 38 times those used in humans caused no impaired fertility and dosesup to 5O times normal caused no symptoms of teratogenicity.

Adverse Effects, Warnings

Adverse effects are uncommon with sucralfate therapy. Constipationis the most prominent adverse effect reported in humans (2%) and dogs taking the drug.
Overdosage - Overdosage is unlikely to cause any significant problems. Laboratory animals receiving up to 12 grams/kg orally demonstrated no incidence of mortality.

Drug Interactions

Cimetidine, tetracycline, phenytoin and digoxin bioavailability may bereduced if administered with sucralfate. To avoid this problem, give sucralfate at least 2 hours apartfrom these other drugs. Because sucralfate requires an acidic environment to be effective, givesucralfate doses before (at least 1/2 hour) cimetidine (or other H2 antagonist) or antacids.