Sucralfate

drugbox
IUPAC_name = Hexadeca-μ-hydroxytetracosahydroxy [μ₈- [1,3,4,6-tetra-"O"-sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis(hydrogen sulfato)8-)] hexadecaaluminum"Merck Index", 12th Edition, 9049.]

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width = 250px
CAS_number = 54182-58-0
ATC_prefix = A02
ATC_suffix = BX02
ATC_supplemental =
PubChem = 6398525
DrugBank = APRD01238
chemical_formula = C₁₂H₅₄Al₁₆O₇₅S₈
molecular_weight = 2086.75 g/mol
bioavailability = 3-5% (local acting)
protein_bound =
metabolism = GI; liver: unknown
elimination_half-life = unknown
excretion = feces, urine
pregnancy_category = B
legal_status = ℞-only
routes_of_administration = , suspension, rectal suspension

Sucralfate (brand names Sucramal in Italy; Carafate in U.S.A.; Sucrafil, in India; Sutra in parts of South-East Asia, Sulcrate in Canada; Antepsin in Turkey) is an oral gastrointestinal medication primarily indicated for the treatment of active duodenal ulcers. It is also used for the treatment of gastroesophageal reflux disease (GERD)cite journal |author=Maton PN |title=Profile and assessment of GERD pharmacotherapy |journal=Cleve Clin J Med |volume=70 Suppl 5 |issue= |pages=S51–70 |year=2003 |pmid=14705381 |doi=] and stress ulcers. Unlike the other classes of medications used for treatment of peptic ulcers, sucralfate is a sucrose sulfate-aluminium complex that binds to the hydrochloric acid in the stomach and acts like an acid buffer with cytoprotective properties. Sucralfate was approved by the Food and Drug Administration (FDA) in 1981.

Mechanism of action

Sucralfate is a locally acting substance that in an acidic environment (pH < 4), reacts with hydrochloric acid in the stomach to form a cross-linking, viscous, paste-like material capable of acting as an acid buffer for as long as 6 to 8 hours after a single dose. It also attaches to proteins on the surface of ulcers, such as albumin and fibrinogen, to form stable insoluble complexes. These complexes serve as protective barriers at the ulcer surface, preventing further damage from acid, pepsin, and bile. In addition, it prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. Recently, it has been indicated that sucralfate also stimulates the increase of prostaglandin E₂, epidermal growth factors (EGF), bFGF), and gastric mucus.

Clinical uses

The only FDA-approved indication for sucralfate is for the treatment of active duodenal ulcers not related to NSAID usage because the mechanism behind these ulcers is secondary to acid oversecretion. It is not technically approved for gastric ulcers because the main mechanism is not due to acid oversecretion but rather from diminished protection. The use for sucralfate in peptic ulcer disease has diminished recently, but it is still the preferred agent for stress ulcer prophylaxis.

* Active duodenal ulcer not related to NSAID use -- 1 g PO four times a day given 1 hr before meals and at bedtime for 4-8 weeks
* Maintenance therapy for resolved duodenal ulcers -- 1 g PO bid on empty stomach
* Gastric ulcer not related to NSAID use and gastritis due to GERD -- 1 g PO four times a day 1 hr before meals and at bedtime. Triple combination therapy with lansoprazole + cisapride + sucralfate can significantly improve symptoms and quality of life and was more cost-effective than ranitidine combination group. [Journal of Zhejiang University 2003 Sep-Oct; 4(5): 602-6]
* Aphthous ulcer and stomatitis due to radiation or chemotherapy -- 5-10 mL PO suspension swish and spit/swallow four times a day.
* Proctitis from radiation or ulcerative colitis -- 3 g/15 mL rectal suspension once or twice daily.
* Gastro-esophageal reflux disease during pregnancy -- first-line drug therapy combined with lifestyle and diet modification. ["Aliment Pharmacol Ther." 2005 Nov 1;22(9):749-57.]
* Stress ulcer prophylaxis -- The use of sucralfate rather than H₂ 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 ventilator-associated pneumonia (VAP). ["Respir Care". 2005 Jun;50(6):725-39; discussion 739-41.]
* Prevention of 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.]
* Rectal bleeding and its management after irradiation for uterine cervical cancerGrade 1 bleeding experienced immediate relief with sucrasulfate enema for 1 month.Grade 2 bleeding, sucrasulfate enema and/or coagulation were effective.Grade 3 bleeding lasted for 1 year despite frequent transfusions and coagulation.Grade 2 and 3 rectal bleeding occurred in 8.5% of patients. The most significant risk factor was the ICRU-CRBED. Prompt treatment with a combination of sucrasulfate enema and coagulation is effective in controlling Grade 1 and 2 rectal bleeding without the development of fistula or stricture. ["International Journal Radiation Oncology Biological Physics", 2004 Jan 1;58(1):98-105]

Adverse reactions

The most common side effects seen are constipation and bezoar formation. Less commonly reported include flatulence, cephalalgia (headache), hypophosphatemia, and xerostomia (dry mouth).Nursing mothers: Uncertain.

Notes

References

* Journal of Zhejiang University 2003 Sep-Oct; 4(5): 602-6
* Katzung, Bertram G. "Basic and Clinical Pharmacology", 9th ed. (2004).

External links

* [http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a681049.html Medline Plus]
* [http://www.marvistavet.com/html/sucralfate.html Mar Vista Animal Medical Center]
* [http://www.medicinenet.com/sucralfate/article.htm Medicine Net]
* [http://www.rxlist.com/cgi/generic/sucral.htm Rx List]
* [http://www.drugs.com/MTM/sucralfate.html Drugs.com]
* [http://www.wholehealthmd.com/refshelf/drugs_view/1,1524,573,00.html Whole Health MD]
* [http://www.genome.jp/dbget-bin/www_bget?dr+D00446 Kyoto Encyclopedia of Genes and Genomes]
* [http://www.axcanscandipharm.com/prescribinginfo_carafate.php Carafate prescribing information]