Pharmacotherapeutic Group: Gastro-Duodenal Cytoprotective Agent.
Pharmacology: Pharmacodynamics: Sucralfate exerts a generalized gastric cytoprotective effect by enhancing natural mucosal defense mechanisms. Studies conducted in animals and clinical trials in humans have demonstrated that sucralfate can protect the gastric mucosa against various irritants such as alcohol, aspirin, hydrochloric acid, sodium hydroxide or sodium taurocholate.
In addition, sucralfate has been demonstrated to have a greater affinity for ulcerated gastric or duodenal mucosa than for non-ulcerated mucosa.
Sucralfate produces an adherent and cytoprotective barrier at the ulcer site. This barrier protects the ulcer site from the potential ulcerogenic properties of acid, pepsin and bile. Furthermore, sucralfate blocks acid diffusion across the sucralfate protein barrier and also complexes directly with pepsin and bile.
The action of sucralfate is non-systemic as the drug is only minimally absorbed from the gastrointestinal tract. The minute amounts of the sulfated disaccharide which are absorbed are primarily excreted in the urine.
Each gram of sucralfate contains approximately 200 mg of aluminium. The aluminium moiety can dissociate at low pH and aluminium release in the stomach can be expected; however, aluminium is poorly absorbed from the intact gastrointestinal tract. Following administration of 1 g of sucralfate tablets four times a day to individuals with normal renal function, approximately 0.001% to 0.017% of sucralfate's aluminium content is absorbed and excreted in the urine. This results in an aluminium load of between 0.008 mg and 0.136 mg following a 4 g daily dose. Individuals with normal renal function excrete absorbed aluminium can respond to an increased aluminium load by increasing urinary excretion. These values were determined in individuals with intact gastrointestinal mucosa. Available evidence does not indicate that absorption of aluminium would be different in individuals with ulcerated gastrointestinal mucosa.
Experiments have shown that sucralfate is not an antacid.
A comparative clinical trial of the efficacy of sucralfate following administration of Apo-Sucralfate and in 63% of patients given Sucralfate. There was no statistical difference between treatments in terms of ulcer healing.