Sucralfate
2558409
223429756
2008-07-04T01:14:14Z
70.79.106.150
{{drugbox
| IUPAC_name = Hexadeca-μ-hydroxytetracosahydroxy[μ<sub>8</sub>-[1,3,4,6-tetra-''O''-sulfo-β-<small>D</small>fructofuranosyl-α-<small>D</small>-glucopyranoside tetrakis(hydrogen sulfato)8-)]]hexadecaaluminum<ref name="Merck">''[[Merck Index]]'', 12th Edition, '''9049'''.</ref>
| image = Sucralfate.png
| width = 250px
| CAS_number = 54182-58-0
| ATC_prefix = A02
| ATC_suffix = BX02
| ATC_supplemental =
| PubChem = 6398525
| DrugBank = APRD01238
| chemical_formula = C<sub>12</sub>H<sub>54</sub>Al<sub>16</sub>O<sub>75</sub>S<sub>8</sub><ref name="Merck"/>
| molecular_weight = 2086.75 g/mol<ref name="Merck"/>
| bioavailability = 3-5% (local acting)
| protein_bound =
| metabolism = [[gastrointestinal|GI]]; [[liver]]: unknown
| elimination_half-life = unknown
| excretion = [[feces]], [[urine]]
| pregnancy_category = B
| legal_status = ℞-only
| routes_of_administration = [[Wiktionary:oral|oral]], [[suspension (chemistry)|suspension]], [[rectal]] [[suspension (chemistry)|suspension]]}}
'''Sucralfate''' (brand names '''Sucramal''' in Italy; '''Carafate''' in U.S.A.; '''Pepsigard''', '''Sucral''' in India; '''Sutra''' in parts of South-East Asia, '''Sulcrate''' in Canada) is an oral [[gastrointestinal]] [[medication]] primarily indicated for the treatment of active [[duodenal|duodenal ulcers]]. It is also used for the treatment of [[gastroesophageal reflux disease]] ([[GERD]])<ref name="pmid14705381">{{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=}}</ref> and [[Stress (medicine)|stress]] [[ulcer]]s. Unlike the other classes of [[medications]] used for treatment of [[peptic ulcers]], sucralfate is a [[sucrose]] [[sulfate]]-[[aluminium]] [[complex (chemistry)|complex]] that binds to the [[hydrochloric acid]] in the [[stomach]] and acts like an [[buffering agent|acid buffer]] with [[cytoprotectant|cytoprotective]] properties. Sucralfate was approved by the [[Food and Drug Administration]] (FDA) in [[1981 in science|1981]].
==Mechanism of action==
Sucralfate is a locally acting [[chemical substance|substance]] that in an [[acidic]] environment (pH < 4), reacts with [[hydrochloric acid]] in the [[stomach]] to form a cross-linking, [[viscosity|viscous]], paste-like material capable of acting as an [[buffering agent|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 [[albumins|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 acid]]s. Recently, it has been indicated that sucralfate also stimulates the increase of [[prostaglandin]] E<sub>2</sub>, [[epidermal growth factor]]s (EGF), [[bFGF]]), and [[gastric juice|gastric mucus]].
==Clinical uses==
The only [[FDA]]-approved indication for sucralfate is for the treatment of active [[duodenal|duodenal ulcers]] not related to [[NSAID]] usage because the [[mechanism of action|mechanism]] behind these ulcers is secondary to acid oversecretion. It is not technically approved for [[gastric ulcer]]s 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 (medicine)|stress]] ulcer [[prophylaxis]].
* Active [[duodenal|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|duodenal ulcers]] -- 1 g PO bid on empty [[stomach]]
* [[Gastric ulcer]] not related to [[NSAID]] use and [[gastritis]] due to [[gastroesophageal reflux disease|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 therapy|radiation]] or [[chemotherapy]] -- 5-10 mL PO [[suspension (chemistry)|suspension]] swish and spit/swallow four times a day.
* [[Proctitis]] from radiation or [[ulcerative colitis]] -- 3 g/15 mL [[rectal]] [[suspension (chemistry)|suspension]] once or twice daily.
* [[Gastro-esophageal reflux disease]] during [[pregnancy]] -- [[first line treatment|first-line drug therapy]] combined with [[lifestyle]] and [[diet (nutrition)|diet]] modification.<ref>''Aliment Pharmacol Ther.'' 2005 Nov 1;22(9):749-57.</ref>
* [[Stress (medicine)|Stress]] [[ulcer]] [[prophylaxis]] -- The use of sucralfate rather than H<sub>2</sub> [[receptor antagonist|antagonists]] for stress ulcer prophylaxis, and measures to prevent [[pulmonary aspiration|aspiration]], such as semirecumbent positioning or continuous [[glottic|subglottic]] suctioning, have all been shown to reduce the [[risk]] of [[ventilator-associated pneumonia]] ([[ventilator-associated pneumonia|VAP]]).<ref>''Respir Care''. 2005 Jun;50(6):725-39; discussion 739-41.</ref>
* 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 [[esophagus|esophageal]] burns to enhance [[mucosal]] healing and suppress stricture formation<ref>''Surg Today''. 2005;35(8):617-22.</ref>
* [[Rectal bleeding]] and its management after [[irradiation]] for [[uterus|uterine]] [[cervical cancer]]
Grade 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]].<ref>''International Journal Radiation Oncology Biological Physics'', 2004 Jan 1;58(1):98-105</ref>
== 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/>
==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]
{{Drugs for peptic ulcer and GORD}}
[[Category:Gastrointestinal system drugs]]
[[Category:Equine medications]]
[[Category:Disaccharides]]
[[Category:Organosulfates]]
[[Category:Aluminium compounds]]
[[de:Sucralfat]]
[[es:Sucralfato]]
[[ja:スクラルファート]]