Sucralfate (Carafate Tablets 1 G, Suspension 1 G / 10 Ml)
Sucralfate is a gastrointestinal agent that adheres to ulcer in acidic gastric juice, forming a protective layer that serves as a barrier against acid, bile salts, and enzymes present in the stomach and duodenum. It is indicated in short-term treatment of duodenal ulcer; and maintenance therapy of duodenal ulcer (tablets only).
In the presence of acid-induced damage, pepsin-mediated hydrolysis of mucosal proteins contributes to mucosal erosion and ulcerations. This process can be inhibited by sulfated polysaccharides. Sucralfate (Carafate) consists of the octasulfate of sucrose to which Al(OH)3 has been added. In an acid environment (pH < 4), sucralfate undergoes extensive cross-linking to produce a viscous, sticky polymer that adheres to epithelial cells and ulcer craters for up to 6 hours after a single dose. In addition to inhibiting hydrolysis of mucosal proteins by pepsin, sucralfate may have additional cytoprotective effects, including stimulation of local production of prostaglandins and epidermal growth factor. Sucralfate also binds bile salts; thus, some clinicians use sucralfate to treat individuals with the syndromes of biliary esophagitis or gastritis.
The use of sucralfate to treat peptic acid disease has diminished in recent years. Nevertheless because increased gastric pH may be a factor in the development of nosocomial pneumonia in critically ill patients, sucralfate may offer an advantage over proton-pump inhibitors and H2-receptor antagonists for the prophylaxis of stress ulcers. Due to its unique mechanism of action, sucralfate also has been used in several other conditions associated with mucosal inflammation / ulceration that may not respond to acid suppression, including oral mucositis (radiation and aphthous ulcers) and bile reflux gastropathy. Administered by rectal enema, sucralfate also has been used for radiation proctitis and solitary rectal ulcers.
Since it is activated by acid, sucralfate should be taken on an empty stomach 1 hour before meals. The use of antacids within 30 minutes of a dose of sucralfate should be avoided. The usual dose of sucralfate is 1 g four times daily (for active duodenal ulcer) or 1 g twice daily (for maintenance therapy).
The most common side effect of sucralfate is constipation (about 2%). As some aluminum can be absorbed, sucralfate should be avoided in patients with renal failure who are at risk for aluminum overload. Likewise, aluminum-containing antacids should not be combined with sucralfate in these patients. Sucralfate forms a viscous layer in the stomach that may inhibit absorption of other drugs, including phenytoin, digoxin, cimetidine, ketoconazole, and fluoroquinolone antibiotics. Sucralfate therefore should be taken at least 2 hours after the administration of other drugs. The “sticky” nature of the viscous gel produced by sucralfate in the stomach also may be responsible for the development of bezoars in some patients, particularly in those with underlying gastroparesis.