Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: KEGG:D00446 (Sucralfate)
 278 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A method producing persistent gastric ulcers in the rhesus monkey by combined mucosal injury and gamma-irradiation was modified and evaluated in the rabbit. gamma-Irradiation (800-1000 cGy) immediately after removal of 2-mm-diameter sections of antral mucosa resulted in ulcer craters 5-7 days later. Ulcer sites were characterized by loss of the mucosa, muscularis mucosa, and much of the submucosa. The exposed submucosa was coated with fibrin and necrotic debris infiltrated with heterophils, the rabbit equivalent of neutrophils. These ulcers strongly resemble human chronic gastric ulcers. Binding of Carafate (sucralfate; Marion Laboratories, Inc., Kansas City, MO) and Maalox (magnesia-alumina oral suspension; Wm. H. Rorer, Inc., Ft. Washington, PA) to ulcer and nearby nonulcer sites in the antrum was assessed 1 hour after drug dosing. Drug binding was determined by aluminum quantitation of stomach wall punch biopsies at necropsy. Both drugs significantly increased aluminum bound to the stomach wall compared with vehicle treatment. Significantly more antiulcer drug was bound to ulcer sites than to nearby nonulcer sites only after sucralfate administration. This model of persistent gastric ulcer should be useful to further study gastric ulcer pathogenesis and treatment.
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PMID:Mucosal injury and gamma-irradiation produce persistent gastric ulcers in the rabbit. Evaluation of antiulcer drug binding to experimental ulcer sites. 201 69

The pharmacology, pharmacokinetics, clinical studies, adverse reactions, and dosage of sucralfate (Carafate, Marion Laboratories), a unique drug for peptic-ulcer disease, are reviewed. Sucralfate exerts its antiulcer effect by binding with proteinacious material, neutralizing local acidity without affecting gastric pH, and forming a protective barrier at the ulcer site. It also inhibits the diffusion of hydrogen ion, inhibits the action of pepsin, and adsorbs bile salts. Approximately 3-5% of an orally administered dose of sucralfate is absorbed; more than 90% of the dose is excreted unchanged in the feces. Sucralfate remains at the site of gastric ulcers for up to six hours. In the treatment of duodenal ulcers, sucralfate is more effective than placebo and comparable with cimetidine and intensive antacid therapy. Healing rates for gastric ulcers are less impressive but are comparable with those produced by cimetidine and antacids. Additive or synergistic effects of sucralfate with cimetidine or intensive antacid therapy have not been studied. Sucralfate has few side effects because it is not absorbed; most frequently reported are constipation (3-4%), xerostomia (1%), and skin eruptions (0.6%). No drug-drug interactions have been reported. The recommended dose of sucralfate is 1 g four times a day one hour before meals and at bedtime. Sucralfate is a unique antiulcer drug that compares favorably with cimetidine and antacid therapy in terms of safety and efficacy. Sucralfate is FDA-approved for short-term (up to eight weeks) treatment of duodenal ulcers.
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PMID:Sucralfate--alternative therapy for peptic-ulcer disease. 676 89