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Sucralfate

Carafate 




Article: Sucralfate

Image:Sucralfate.png
Sucralfate
Systematic (IUPAC) name
alumane; 3,4,5-trisulfooxy-2-(sulfooxymethyl)-6- [3,4,5-trisulfooxy-2- (sulfooxymethyl) oxolan-2-yl] oxy-oxane; icosahydrate
Identifiers
CAS number 54182-58-0
ATC code A02BX02
PubChem 6398525
DrugBank APRD01238
Chemical data
Formula C11H87Al9O55S8
Mol. weight 1599.14 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

Sucralfate is a prescription medication used to treat peptic ulcers. It is marketed under the brand name Carafate. In Pakistan sucralfate is available under the brand name of ulsanic. It can be taken orally, in tablet or suspension form. Sucralfate was approved by the Food and Drug Administration (FDA) in 1981

Chemical makeup

Chemically, it is a complex of the disaccharide sugar, sucrose, combined with sulfate and aluminum. Its chemical formula is C12H14O11(SO3Al(OH)2)8·(Al(OH)3)x·(H2O)y, where x is 8 to 10 and y is 22 to 31. In acidic solutions (e.g. gastric acid) it forms a thick paste that has a strong negative charge.

Usage mechanism

In the presence of acid-induced damage, pepsin mediated hydrolysis of mucosal proteins contributes to mucosal erosion and ulceration. This process can be inhibited by sulfated polysaccharides. Sucralfate consists of octasulfate of sucrose to which aluminum hydroxide has been added. In an acidic environment (pH < 4), it undergoes extensive cross–linking and polymerization to produce a viscous, sticky gel that adheres strongly to epithelial cells and even more strongly to ulcer craters for as long as 6 to 8 hours after a single dose. In addition inhibition of hydrolysis of mucosal proteins by pepsin, sucralfate have additional cytoprotective effects, including stimulation of local production of prostaglandin and epidermal growth factor (EGF & bFGF). Sucralfate also binds bile salts, accounting for its use in some patients with esophagitis or gastritis in whom reflux of bile is thought by some to play a role in pathogenesis. Sucralfate is also useful in the prophylaxis of stress ulcer, where its use may be associated with a lower incidence of nosocomial pneumonia compared to acid suppressing therapy with its tendency to promote gastric bacterial colonization.

Clinical Uses

Duodenal & Gastric Ulcer

It is effective for the healing of duodenal and Gastric ulcers, It is also effective at preventing stress-related gastritis in critically ill patients and is sometimes used to treat patients who are experiencing NSAID-related dyspepsia.

GERD in Pregnancy

Gastro-oesophageal reflux disease during pregnancy should be managed with a step-up algorithm beginning with lifestyle modifications and dietary changes. sucralfate is considered the first-line drug therapy.[Aliment Pharmacol Ther. 2005 Nov 1;22(9):749-57.]

Stress ulcer prophylaxis

The use of SUCRALFATE rather than H(2) antagonists for stress ulcer prophylaxis, and measures to prevent aspiration, such as semirecumbent positioning or continuous subglottic suctioning, have all been shown to reduce the risk of VAP. [Respir Care. 2005 Jun;50(6):725-39; discussion 739-41.]

Inhibitory effect on Stricture formation

SUCRALFATE has an inhibitory effect on stricture formation in experimental corrosive burns and can be used in the treatment of corrosive esophageal burns to enhance mucosal healing and suppress stricture formation [Surg Today. 2005;35(8):617-22.]

Use of sucralfate in combination

Title of the study: Quality of life and cost-effectiveness of combined therapy for reflux esophagitis Objective of the study: To evaluate clinical, Quality of life (Qol) and medical cost outcomes in patients with symptomatic reflux esophagitis (RE) receiving different “Triple Combination Therapy” Conclusion. “Triple Combination Therapy” can significantly improve symptoms and quality of life. Lansoprazole + Cisapride + SUCRALFATE therapy was more cost-effective than Ranitidine combination group. Journal of Zhejiang University 2003 Sep-Oct; 4(5): 602-6

Resources



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December 3, 2009



Page Updated: July 22, 2006
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