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)

Pharmacologic management of peptic ulcer disease continues to evolve with the introduction of diverse types of new therapeutic agents. The ideal aims of treatment of peptic ulcer disease are to relieve pain, heal the ulcer, and delay ulcer recurrence. This article provides a broad perspective on the pharmacology and therapeutic actions of antiulcer drugs. To date, no drug meets all goals of therapy. Drug treatment of peptic ulcers is targeted at either counteracting aggressive factors or stimulating the mucosal defense. Drugs that inhibit or neutralize gastric acid secretion include histamine H2-receptor antagonists, proton pump inhibitors, anticholinergics, prostaglandins, and antacids. H2-receptor antagonists have become first-line drugs for treatment of uncomplicated duodenal ulcers, gastric ulcers, prevention of ulcer relapse, and mild esophagitis. However, H2-receptor antagonists, like other gastric antisecretory/antiulcer drugs, have high rates of ulcer recurrence following discontinuation of therapy. They therefore need to be administered continuously in patients prone to such recurrences. Omeprazole has emerged as a major drug for the treatment of severe erosive esophagitis, refractory ulcers, and Zollinger-Ellison syndrome. The major disadvantage of proton pump inhibitors is the concern for their long-term safety. The roles of M1-antimuscarinic agents and antacids have not been fully defined. Misoprostol, effective for the treatment of gastric and duodenal ulcers, is now the only drug that prevents ulcers induced by nonsteroidal anti-inflammatory drugs. Mucosal protective drugs that do not inhibit gastric acid secretion include sucralfate and organic bismuth salts. Sucralfate is a nonsystemic, well-tolerated, effective drug for treatment of duodenal ulcers and prevention of duodenal ulcer relapse. The organic bismuth salt bismuth subcitrate is efficacious in the treatment of duodenal and gastric ulcers. Furthermore, it has also been established that it alters the course of ulcer recurrence. However, bismuth encephalopathy is a major toxicity concern that needs to be addressed.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Drugs for treatment of peptic ulcers. 135 99

We have studied the effect of the aluminum complex of sucrose sulphate (Sucralfate suspension) and the sodium salt of sucrose sulphate (sodium sucrose sulphate solution) on patients with keratoconjunctivitis sicca. Eyes treated with either of these two drugs showed a decrease in painfulness and blurring of vision. On examination the surface area of the corneal lesions, stained with fluorescein, diminished during treatment. As for the difference in effect between the two eyedrops, the solution was better tolerated.
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PMID:Sucralfate and sodium sucrose sulphate in the treatment of superficial corneal disease in keratoconjunctivitis sicca. 141 98

Drugs used in the treatment of peptic ulcer disease may interact with the renal system in a variety of ways. Since many agents are eliminated by renal excretion, clearance of these agents may be reduced and half-life extended in the presence of renal insufficiency. The histamine H2-receptor antagonists may interfere with renal tubular excretion of creatinine and cationic drugs, resulting in elevated serum concentrations and reduced renal clearance. The prostaglandin E1 analogue misoprostol is used as a cytoprotective agent but has renal effects. The renal effects differ between systems studied. In the rat, misoprostol reduces cyclosporin-induced renal tubular toxicity, whereas in humans it has been shown to attenuate renal allograft rejection. Sucralfate is the aluminium salt of sucrose octasulfate. It permits the absorption of aluminium in amounts similar to aluminium-containing antacids, and toxicity has been demonstrated in the presence of renal insufficiency. Bismuth compounds are used increasingly to treat peptic ulcer disease, and bismuth toxicity has been described in association with renal insufficiency. Aluminium-, calcium- and magnesium-containing antacids are used as oral phosphate binders in patients with renal insufficiency in addition to their usual indications. Cation absorption and accumulation with all of these antacid preparations has been described and may lead to toxicity.
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PMID:Renal effects of peptic ulcer therapy. 152

Sucralfate, a basic aluminum salt of sucrose, was the first successful drug with a major cytoprotective mechanism of action. It binds bile acids and pepsin and adheres to both ulcerated and nonulcerated mucosa. Sucralfate stimulates the synthesis and release of gastric mucosal prostaglandins as well as bicarbonate and the epidermal growth factor which stimulates healing. Sucralfate is the safest drug available today in the treatment of dyspeptic symptoms and compared to ranitidine and cimetidine it has the following characteristics. (2) The short-term healing of duodenal ulcers is the same for sucralfate, cimetidine and ranitidine. (3) Sucralfate-treated patients have a lower recurrence rate of duodenal ulceration after healing when compared with cimetidine and the recurrence rate is not connected with the presence or absence of Campylobacter pylori.
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PMID:Role of sucralfate in peptic disease. 161 11

Sucralfate, an aluminum salt of sucrose octasulfate, has been shown to be effective in reducing the discomfort of radiation therapy-induced oral mucositis. This study was done to determine whether sucralfate could be used as a nutritional source for dental caries-producing organisms. Three Streptococcus strains were cultured in a defined medium. Sucralfate powder was evaluated for its ability to be used as a carbohydrate food source by these organisms. The addition of sucralfate alone did not stimulate the organism's growth. The addition of sucralfate and glucose resulted in less growth than the addition of glucose alone. Increasing the sucralfate concentration from 1% to 10% in the glucose-containing cultures resulted in statistically significant growth inhibition (p less than 0.02). Sucralfate appears to have no cariogenic potential and may have some cariostatic potential.
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PMID:The effect of sucralfate on the growth of cariogenic streptococci. 177 88

Inhibition of gastric acid secretion is a major factor in protecting the gastric mucosa, although other mechanisms such as bile salt binding may contribute to the protective properties of individual agents. Sucralfate, antacid (Maalox), and Meciadanol, a new flavonoid, were compared with cholestyramine resin for binding bile salts. The free, glycine, and taurine conjugates of the human bile salts, cholate, chenodeoxycholate, and deoxycholate, were incubated with each of the above. Cholestyramine resin adsorbed 91-97% of all bile salts tested. Meciadanol adsorbed all of the bile salts fairly well except for the free forms of chenodeoxycholate and deoxycholate. Meciadanol (53 to 84%) adsorbed bile salts better than sucralfate (4.2 to 61%), and significantly (P less than 0.05) better than Maalox (10 to 47%). In our in vitro studies, sucralfate was not as effective in binding bile salts as previously reported. Patients in the surgical intensive care unit were randomized prospectively to receive nasogastric instillation of Maalox, sucralfate, or Meciadanol to prevent gastrointestinal bleeding. The gastric aspirates were analyzed for bile salt concentration. The mean bile salt concentration of those treated with Maalox (0.24 mM), Meciadanol (0.24 mM), or sucralfate (0.35 mM) was significantly lower than those treated with nasogastric aspiration (0.87 mM) alone (P less than 0.01). This suggests that these substances bind bile salts and may provide additional protection to the gastric mucosa along with their ability to neutralize gastric acid.
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PMID:Bile salt binding by maalox, sucralfate, and meciadanol: in vitro and clinical comparisons. 268 4

Stress-related mucosal damage (SRMD) of the upper gastrointestinal tract is being increasingly recognized in critically ill patients. Its precise pathogenesis is unknown. Acid is a prerequisite for the development of mucosal injury. However, mucosal defense factors that maintain the integrity of the gastric mucosal barrier are equally important. Therapy is directed toward reducing the intraluminal acid concentration. Since histamine H2-receptor antagonists became available in 1977, they have been used for the prevention and treatment of SRMD. They offer the potential for use as an effective parenteral as well as oral agent that could obviate the need for frequent antacid administration and eliminate some of the troublesome side effects that accompany an intensive antacid regimen. Although the beneficial effects of H2 blockers are probably related to their ability to inhibit acid secretion, recent evidence suggests that they may also act by mechanisms independent of their antisecretory effect. Numerous controlled studies have confirmed that cimetidine, being superior to placebo and equivalent to antacids, is effective therapy for SRMD. Sucralfate, a basic aluminum salt of sucrose octasulfate, has been shown to protect animal and human gastric mucosa from a variety of injurious agents. However, few clinical trials have evaluated the efficacy of sucralfate in SRMD. Exogenous prostaglandins also have been shown to protect gastric mucosa from a variety of insults. Although exogenous prostaglandins may work by augmenting mucosal defense mechanisms, most clinical studies have used antisecretory doses of prostaglandin drugs, making it difficult to discount the antisecretory component as being responsible for efficacy.
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PMID:Stress-related mucosal damage. 287 27

We have validated a method to measure bile salt binding by Maalox (aluminum hydroxide and magnesium hydroxide), Carafate (sucralfate), and Questran (cholestyramine) in vitro. The method used in this study involves a correction for adherent water volume and thus provides a correct measure of bile salt binding. With this approach, we described the binding properties of Maalox, Carafate, and Questran. The bile salt binding capacities of Carafate and Maalox are limited and do not have physiological or pharmacological significance. On the other hand, we found that Questran has substantial bile salt binding capacity. At the recommended dosage, Questran could deplete the total bile salt pool. We also found that Carafate, although not used as an antacid, has buffering capacity (maintaining a pH of solution in the range 4.2-4.8) which might contribute to its effectiveness as an ulcer treatment drug.
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PMID:Bile salt binding properties of commonly used gastrointestinal drugs: maalox, carafate, and questran. 317 34

Sucralfate has been evaluated in reflux esophagitis. The rationale for its effectiveness is based on its protective adherence to denuded mucosal surfaces and its bile salt binding properties. According to Weiss et al (5), healing occurred in 72% and improvement in 14% of sucralfate treated patients, compared respectively to 40% and 20% receiving placebo (p less than 0.05). According to Laitinen et al (6) esophagitis healed in 53% of patients receiving sucralfate, against 34% of an alginate/antacid-treated group. Symptoms disappeared, or improved in almost 70% of both groups. Hameeteman et al (7) found improvement of esophagitis in 53% and healing in 31% after sucralfate, compared with 67% and 14% respectively after cimetidine. Symptomatic improvement was good and comparable in both groups. Simon et al (8) found endoscopic healing in 64% and improvement in 27% of sucralfate-healed patients, compared with 68% and 21% respectively after ranitidine. Symptom relief and antacid consumption was comparable in both groups. Sucralfate appears to be a safe and efficacious locally active mucosal protecting agent for the treatment of reflux esophagitis. Its efficacy is comparable to that of H2-receptor blockers.
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PMID:Clinical efficacy of sucralfate in reflux oesophagitis. 332 82

Sucralfate has been evaluated in reflux esophagitis, based on its protective adherence to denuded surfaces, its bile salt-binding properties, and its cytoprotective properties. Histamine (H2)-receptor blockers are currently considered the standard therapy. The goal of this study was to compare the potential efficacy of sucralfate with that of cimetidine. A single-blind, randomized, multicenter study was performed in 42 patients with endoscopically documented reflux esophagitis. Patients were randomly given 1 g of sucralfate suspension four times daily or 400 mg of cimetidine four times daily for eight weeks. Forty patients were evaluated after eight weeks. Symptomatic improvement was good and comparable in both groups. In two patients given sucralfate and one given cimetidine, side effects were noted but did not necessitate withdrawal from the study. Endoscopy showed improvement in 53 percent of patients and healing of esophagitis in 31 percent after sucralfate treatment. With cimetidine, improvement was seen in 67 percent and healing occurred in 14 percent. In one patient receiving cimetidine, distal esophageal stenosis developed, requiring dilatation therapy. It is concluded that treatment with sucralfate improves the symptomatology and severity of reflux esophagitis. The results obtained with sucralfate appear comparable to those with cimetidine. Sucralfate may therefore be considered as a valid alternative to H2-receptor antagonist therapy in treating reflux esophagitis.
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PMID:Clinical efficacy of sucralfate in reflux esophagitis. Comparison with cimetidine. 366 10


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