Sucralfate

Chemical formula: C₁₁H₂₈Al₈O₅₁S₈  Molecular mass: 1,558.67 g/mol  PubChem compound: 70789197

Pharmacodynamic properties

The action of sucralfate is non-systemic as the drug is only minimally absorbed from the gastro-intestinal tract. The small amounts that are absorbed are excreted primarily in the urine. Sucralfate exerts a generalised cytoprotective effect by preventing gastro-intestinal mucosal injury.

Studies in humans and animal models show that sucralfate forms an ulcer adherent complex with the proteinaceous exudate of the ulcer site. This property enables sucralfate to form a protective barrier over the ulcer lesion giving sustained protection against the penetration and action of gastric acid, pepsin and bile.

Studies both in humans and animals demonstrate that sucralfate protects the gastric mucosa against various irritants such as alcohol, acetylsalicyclic acid and sodium taurocholate.

Sucralfate also directly inhibits pepsin activity and absorbs bile salts. It has only weak antacid activity. It does not alter gastric emptying time, nor normal digestive function. Sucralfate has no demonstrated pharmacological effect on the cardiovascular or central nervous systems.

Pharmacokinetic properties

Absorption

Sucralfate is only minimally absorbed from the gastro-intestinal tract. The small amounts that are absorbed are excreted primarily in the urine. Absorption of aluminium from sucralfate may be increased in patients on dialysis or with renal dysfunction.

Preclinical safety data

There was no evidence of carcinogenesis in mice and rats receiving oral sucralfate in dosages of up to 1 g/kg daily (12 times the usual human dosage) for 2 years. In animal studies there was no effect evidence of impaired fertility. The effect of sucralfate on human fertility is not known.

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