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{{Short description|Chemical compound and gastrointestinal medication}}
{{drugbox
{{Use dmy dates|date=August 2021}}
| verifiedrevid = 411558568
{{cs1 config |name-list-style=vanc |display-authors=6}}
| 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>
{{Drugbox
| image = Sucralfate.png
| Verifiedfields = changed
| width = 250px
| Watchedfields = changed
| CAS_number = 54182-58-0
| verifiedrevid = 405746645
| image = Sucralfate.svg
| width = 350

<!-- Clinical data -->
| tradename = Carafate
| Drugs.com = {{drugs.com|monograph|sucralfate}}
| MedlinePlus = a681049
| DailyMedID = Sucralfate
| pregnancy_category =
| routes_of_administration = [[By mouth]], [[Rectal administration|rectal]]
| ATC_prefix = A02
| ATC_prefix = A02
| ATC_suffix = BX02
| ATC_suffix = BX02
| ATC_supplemental =
| ATC_supplemental =

| PubChem = 6398525
| legal_US = Rx-only
| ChEMBL_Ref = {{ebicite|correct|EBI}}= {{ebicite|correct|EBI}}
| legal_US_comment = <ref name="Carafate FDA label" />
| ChEMBL = 611727
| legal_status = Rx-only
| 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"/>
<!-- Pharmacokinetic data -->
| molecular_weight = 2086.75 g/mol<ref name="Merck"/>
| bioavailability = 3-5% (local acting)
| bioavailability = 3-5% (local acting)
| protein_bound =
| protein_bound =
| metabolism = [[gastrointestinal|GI]]; [[liver]]: unknown
| metabolism = [[gastrointestinal|GI]]; [[liver]]: unknown
| elimination_half-life = unknown
| elimination_half-life = unknown
| excretion = [[feces]], [[urine]]
| excretion = [[Feces]], [[urine]]

| pregnancy_category = B
<!--Identifiers-->
| legal_status = ℞-only
| CAS_number_Ref = {{cascite|correct|??}}
| routes_of_administration = [[Wiktionary:oral|oral]], [[suspension (chemistry)|suspension]], [[rectal]] [[suspension (chemistry)|suspension]]}}
| CAS_number = 54182-58-0
| PubChem = 6398525
| DrugBank_Ref = {{drugbankcite|changed|drugbank}}
| DrugBank = DB00364
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 4911161
| UNII_Ref = {{fdacite|changed|FDA}}
| UNII = XX73205DH5
| KEGG = C07314
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 611727

<!--Chemical data-->
| 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-)<nowiki>]]</nowiki>hexadecaaluminum<ref name="Merck">''[[Merck Index]]'', 12th Edition, '''9049'''.</ref>
| C=12 | H=54 | Al=16 | O=75 | S=8
}}

<!-- Definition and medical uses -->
'''Sucralfate''', sold under various brand names, is a [[medication]] used to treat [[Peptic ulcer|stomach ulcers]], [[gastroesophageal reflux disease]] (GERD), [[radiation proctitis]], and [[gastritis|stomach inflammation]] and to prevent [[stress ulcer]]s.<ref name=AHFS2019/><ref name=Mat2003>{{cite journal | vauthors = Maton PN | title = Profile and assessment of GERD pharmacotherapy | journal = Cleveland Clinic Journal of Medicine | volume = 70 | pages = S51-70 | date = November 2003 | issue = Suppl 5 | pmid = 14705381 | doi = 10.3949/ccjm.70.Suppl_5.S51 }}</ref><ref name=Brad2014/> Its usefulness in people infected by ''[[H. pylori]]'' is limited.<ref name=AHFS2019/> It is used by mouth (for upper GIT ulcers) and rectally (for radiation proctitis).<ref name=AHFS2019>{{cite web |title=Sucralfate Monograph for Professionals |url=https://www.drugs.com/monograph/sucralfate.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |date=22 May 2023}}</ref><ref name=Brad2014>{{cite journal | vauthors = Mendenhall WM, McKibben BT, Hoppe BS, Nichols RC, Henderson RH, Mendenhall NP | s2cid = 12129192 | title = Management of radiation proctitis | journal = American Journal of Clinical Oncology | volume = 37 | issue = 5 | pages = 517–23 | date = October 2014 | pmid = 23241500 | doi = 10.1097/COC.0b013e318271b1aa }}</ref>

<!-- Side effects and mechanism -->
Common side effects include [[constipation]].<ref name=AHFS2019/> Serious side effects may include [[bezoar]] formation and [[encephalopathy]].<ref name=BNF76/> Use appears to be safe in [[pregnancy]] and [[breastfeeding]].<ref name=BNF76/> How it works is unclear but is believed to involve binding to the ulcer and protecting it from further damage.<ref name=AHFS2019/><ref name=BNF76/>

<!-- History and culture -->
Sucralfate was approved for medical use in the United States in 1981.<ref name=AHFS2019/> It is available as a [[generic medication]].<ref name=BNF76>{{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=73|edition=76}}</ref><ref>{{cite web | title=Competitive Generic Therapy Approvals | website=U.S. [[Food and Drug Administration]] (FDA) | date=29 June 2023 | url=https://www.fda.gov/drugs/generic-drugs/competitive-generic-therapy-approvals | access-date=29 June 2023 | archive-date=29 June 2023 | archive-url=https://web.archive.org/web/20230629233651/https://www.fda.gov/drugs/generic-drugs/competitive-generic-therapy-approvals | url-status=live }}</ref> In 2022, it was the 214th most commonly prescribed medication in the United States, with more than 1{{nbsp}}million prescriptions.<ref>{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Sucralfate Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Sucralfate | access-date = 30 August 2024 }}</ref>

==Medical uses==
Sucralfate is used for the treatment of active [[Peptic ulcer|duodenal ulcers]] not related to the use of [[nonsteroidal anti-inflammatory drug]]s (NSAIDs), as the [[mechanism of action|mechanism]] behind these ulcers is due to acid oversecretion.<ref name="Carafate FDA label">{{Cite web|title = DailyMed - Carafate - sucralfate suspension|url = http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0fb67b1c-b4c0-46f2-8a81-df1510e006aa|website = dailymed.nlm.nih.gov|access-date = 4 November 2015}}</ref> It is not FDA approved for [[Peptic ulcer|gastric ulcers]], but is widely used because of evidence of efficacy.<ref name=":2">{{cite journal | vauthors = Hixson LJ, Kelley CL, Jones WN, Tuohy CD | title = Current trends in the pharmacotherapy for peptic ulcer disease | journal = Archives of Internal Medicine | volume = 152 | issue = 4 | pages = 726–32 | date = April 1992 | pmid = 1558429 | doi = 10.1001/archinte.152.4.726 }}</ref> The use for sucralfate in [[peptic ulcer disease]] has diminished recently, but it is still the preferred agent for [[stress ulcer]] prevention.<ref>{{cite journal | vauthors = Hunt RH | title = Treatment of peptic ulcer disease with sucralfate: a review | journal = The American Journal of Medicine | volume = 91 | issue = 2A | pages = 102S–106S | date = August 1991 | pmid = 1882894 | doi = 10.1016/0002-9343(91)90459-b }}</ref><ref>{{cite journal | vauthors = Fashner J, Gitu AC | title = Diagnosis and Treatment of Peptic Ulcer Disease and H. pylori Infection | journal = American Family Physician | volume = 91 | issue = 4 | pages = 236–42 | date = February 2015 | pmid = 25955624 }}</ref><ref name=":4">{{cite journal | title = ASHP Therapeutic Guidelines on Stress Ulcer Prophylaxis. ASHP Commission on Therapeutics and approved by the ASHP Board of Directors on November 14, 1998 | journal = American Journal of Health-System Pharmacy | volume = 56 | issue = 4 | pages = 347–79 | date = February 1999 | pmid = 10690219 | doi = 10.1093/ajhp/56.4.347 | doi-access = free }}</ref><ref name=":6">{{cite journal | vauthors = Monnig AA, Prittie JE | title = A review of stress-related mucosal disease | journal = Journal of Veterinary Emergency and Critical Care | volume = 21 | issue = 5 | pages = 484–95 | date = October 2011 | pmid = 22316196 | doi = 10.1111/j.1476-4431.2011.00680.x }}</ref>

Sucralfate has also been used for the following conditions:
* Active [[Peptic ulcer|duodenal ulcer]] not related to NSAID use
* Maintenance therapy for resolved [[Peptic ulcer|duodenal ulcers]]
* [[Peptic ulcer|Gastric ulcer]] not related to NSAID use and [[gastritis]] due to GERD—Triple [[combination therapy]] with [[lansoprazole]] + [[cisapride]] + sucralfate can significantly improve [[symptom]]s and [[quality of life]] and was more cost-effective than [[ranitidine]] combination group.<ref>{{cite journal | vauthors = Si JM, Wang LJ, Chen SJ, Zhao L, Dai N | s2cid = 118845033 | title = Quality of life and cost-effectiveness of combined therapy for reflux esophagitis | journal = Journal of Zhejiang University Science A| volume = 4 | issue = 5 | pages = 602–6 | year = 2003 | pmid = 12958722 | doi = 10.1631/jzus.2003.0602 | bibcode = 2003JZUSA...4..602J }}</ref>
* [[Aphthous ulcer]] and [[stomatitis]] due to [[radiation therapy|radiation]] or [[chemotherapy]]—The 2013 guidelines of the [[International Society of Oral Oncology]] does not recommended sucralfate for the prevention of [[oral mucositis]] in head and neck cancer patients receiving [[radiotherapy]] or [[chemoradiation]] due to a lack of efficacy found in a [[randomized controlled trial]].<ref name="Saunders et al">{{cite journal | vauthors = Saunders DP, Epstein JB, Elad S, Allemano J, Bossi P, van de Wetering MD, Rao NG, Potting C, Cheng KK, Freidank A, Brennan MT, Bowen J, Dennis K, Lalla RV | display-authors = 6 | title = Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients | journal = Supportive Care in Cancer | volume = 21 | issue = 11 | pages = 3191–207 | date = November 2013 | pmid = 23832272 | doi = 10.1007/s00520-013-1871-y | doi-access = free }}</ref>
* [[Gastro-esophageal reflux disease]] during [[pregnancy]]—[[first-line treatment|First-line drug therapy]] combined with [[lifestyle (sociology)|lifestyle]] and [[diet (nutrition)|diet]] modification.<ref>{{cite journal | vauthors = Richter JE | title = Review article: the management of heartburn in pregnancy | journal = Alimentary Pharmacology & Therapeutics | volume = 22 | issue = 9 | pages = 749–57 | date = November 2005 | pmid = 16225482 | doi = 10.1111/j.1365-2036.2005.02654.x | doi-access = free }}</ref>
* [[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 continuous [[glottic|subglottic]] suctioning, have been shown to reduce the risk of [[ventilator-associated pneumonia]] (VAP).<ref>{{cite journal | vauthors = Safdar N, Crnich CJ, Maki DG | title = The pathogenesis of ventilator-associated pneumonia: its relevance to developing effective strategies for prevention | journal = Respiratory Care | volume = 50 | issue = 6 | pages = 725–39; discussion 739–41 | date = June 2005 | pmid = 15913465 }}</ref> Sucralfate is less effective for prophylaxis against gastrointestinal bleeding than either a PPI or H2-blocker. &nbsp;For that reason, it is not commonly used for stress ulcer prophylaxis.
* Prevention of [[Stenosis|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>{{cite journal | vauthors = Temir ZG, Karkiner A, Karaca I, Ortaç R, Ozdamar A | s2cid = 38080924 | title = The effectiveness of sucralfate against stricture formation in experimental corrosive esophageal burns | journal = Surgery Today | volume = 35 | issue = 8 | pages = 617–22 | date = 1 January 2005 | pmid = 16034539 | doi = 10.1007/s00595-004-3005-0 }}</ref>
* [[Proctitis]] from [[ulcerative colitis]]<ref>{{cite book|author1=Theodore M. Bayless|title=Advanced Therapy of Inflammatory Bowel Disease: Ulcerative Colitis (Volume 1), 3e|url=https://books.google.com/books?id=OdUtAwAAQBAJ&pg=PA331|date=14 May 2014|publisher=PMPH-USA|isbn=978-1-60795-216-9|page=331}}</ref>
* [[Lower gastrointestinal bleeding|Rectal bleeding]] due to [[Radiation proctitis|proctitis from radiation]] to treat [[Cervical cancer|cancers of the cervix]], [[Prostate cancer|prostate]], and [[Colorectal cancer|colon]].<ref name=Brad2014/>
** 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 [[Blood transfusion|transfusions]] and coagulation.
** Grade 2 and 3 rectal bleeding occurred in 8.5% of people. 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 name=chun>{{cite journal | vauthors = Chun M, Kang S, Kil HJ, Oh YT, Sohn JH, Ryu HS | title = Rectal bleeding and its management after irradiation for uterine cervical cancer | journal = International Journal of Radiation Oncology, Biology, Physics | volume = 58 | issue = 1 | pages = 98–105 | date = January 2004 | pmid = 14697426 | doi = 10.1016/s0360-3016(03)01395-6 | url = http://repository.ajou.ac.kr/handle/201003/3301 }}</ref>
* Treatment of anastomotic ulcer after [[gastric bypass surgery]]
* Sucralfate suspension is recommended by the US-based National Capital Poison Center (Poison Control) as an intervention for known or suspected [[Button cell#Accidental ingestion|button battery ingestions]] to reduce the risk and severity of injury to the [[esophagus]] prior to the battery's endoscopic removal.<ref name=":1">{{Cite web|url=https://www.poison.org/battery/guideline|title=Guideline|website=www.poison.org|language=en|access-date=5 July 2018}}</ref><ref>{{cite journal | vauthors = Anfang RR, Jatana KR, Linn RL, Rhoades K, Fry J, Jacobs IN | title = pH-neutralizing esophageal irrigations as a novel mitigation strategy for button battery injury | journal = The Laryngoscope | volume = 129 | issue = 1 | pages = 49–57 | date = January 2019 | pmid = 29889306 | doi = 10.1002/lary.27312 | s2cid = 47004940 }}</ref>
*Protection against ventilator-associated pneumonia - Reductions in gastric acidity and volumes increase bacterial overgrowth and the incidence of ventilator-associated pneumonia.&nbsp; Sucralfate may be considered to have the advantage over H2-blockers and PPIs in this regard because sucralfate does not change the pH of gastric fluid. &nbsp;A majority of meta-analyses found that sucralfate therapy decreased the incidence of ventilator-associated pneumonia compared to H2-antagonists.<ref name=":2" />


==Side effects==
'''Sucralfate'''is an cryoprotective agent, an oral [[gastrointestinal]] [[medication]] primarily indicated for the treatment of active [[duodenal|duodenal ulcers]]. Brand names include Sucramal in Italy; Carafate in U.S.A.,Pepsigard,Sucral,sucrafil, hapifate in India, Sutra in parts of South-East Asia, Sulcrate in Canada; and Antepsin in Turkey. Sucralfate 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=10.3949/ccjm.70.Suppl_5.S51}}</ref> and [[Stress (medicine)|stress]] [[Peptic ulcer|ulcers]]. 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 mucosa, thus creating a physical barrier that impairs diffusion of [[hydrochloric acid]] in the [[gastrointestinal tract]] and prevents degeradation of mucus by acid. It also stimulates bicarbonate output and acts like an [[buffering agent|acid buffer]] with [[cytoprotectant|cytoprotective]] properties. Sucralfate was approved by the [[Food and Drug Administration (United States)|U.S. Food and Drug Administration]] (FDA) in [[1981 in science|1981]].
The most common [[adverse effect|side effect]] seen is [[constipation]] (2–3%). Less commonly reported side effects (<0.5%) include [[flatulence]], [[headache]], [[hypophosphatemia]], [[xerostomia]] (dry mouth), and [[bezoar]] formation.<ref>{{cite web | title = Study of possible correlation between BEZOAR and SUCRALFATE | url = http://medsfacts.com/study-SUCRALFATE-causing-BEZOAR.php | archive-url = https://web.archive.org/web/20160918163936/http://factmed.com/study-SUCRALFATE-causing-BEZOAR.php | archive-date = 18 September 2016 | work = MedsFacts.com }}</ref><ref>{{Cite web|url = http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/018333s034,019183s016lbl.pdf|title = Carafate Package Insert|date = 12 September 2013|access-date = 2 November 2015}}</ref><ref>{{cite journal | title = ASHP Therapeutic Guidelines on Stress Ulcer Prophylaxis. ASHP Commission on Therapeutics and approved by the ASHP Board of Directors on November 14, 1998 | journal = American Journal of Health-System Pharmacy | volume = 56 | issue = 4 | pages = 347–79 | date = February 1999 | pmid = 10690219 | doi = 10.1093/ajhp/56.4.347 | doi-access = free }}</ref>
Use of this drug is not recommended for people with [[chronic renal failure|chronic kidney failure]], as it might cause aluminium accumulation and [[Aluminium toxicity in dialysis patients|toxicity]].
A few well-controlled studies have been carried out investigating the safety and efficacy of sucralfate in children and pregnant women ([[Pregnancy Category]] B).<ref name="Carafate FDA label"/><ref>{{cite journal | vauthors = Phupong V, Hanprasertpong T | title = Interventions for heartburn in pregnancy | journal = The Cochrane Database of Systematic Reviews | volume = 2015 | issue = 9 | pages = CD011379 | date = September 2015 | pmid = 26384956 | doi = 10.1002/14651858.CD011379.pub2 | pmc = 9235294 }}</ref><ref name=":0">{{cite journal | vauthors = Steiner K, Bühring KU, Faro HP, Garbe A, Nowak H | title = Sucralfate: pharmacokinetics, metabolism and selective binding to experimental gastric and duodenal ulcers in animals | journal = Arzneimittel-Forschung | volume = 32 | issue = 5 | pages = 512–8 | date = 1 January 1982 | pmid = 6896647 }}</ref>


==Mechanism of action==
==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 (biochemistry)|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]].
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 (biochemistry)|dose]].<ref name=":5">{{cite journal | vauthors = Brogden RN, Heel RC, Speight TM, Avery GS | title = Sucralfate. A review of its pharmacodynamic properties and therapeutic use in peptic ulcer disease | journal = Drugs | volume = 27 | issue = 3 | pages = 194–209 | date = March 1984 | pmid = 6368184 | doi = 10.2165/00003495-198427030-00002 | s2cid = 260482050 }}</ref> It also attaches to [[protein]]s 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]].<ref name=":5"/> In addition, sucralfate prevents back [[diffusion]] of [[hydrogen ion]]s, and absorbs both pepsin and [[bile acid]]s.


It has been thought that sucralfate also stimulates the production of [[prostaglandin]] E<sub>2</sub>, [[epidermal growth factor]]s (EGF), [[bFGF]], and [[gastric juice|gastric mucus]].<ref name="Carafate FDA label"/><ref name=":7">{{cite journal | vauthors = Korman MG, Bolin TD, Szabo S, Hunt RH, Marks IN, Glise H | title = Sucralfate: the Bangkok review | journal = Journal of Gastroenterology and Hepatology | volume = 9 | issue = 4 | pages = 412–5 | date = 1 August 1994 | pmid = 7948825 | doi = 10.1111/j.1440-1746.1994.tb01264.x | s2cid = 41841680 }}</ref>
==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]].


==Pharmacokinetics==
* 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 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 (sociology)|lifestyle]] and [[diet (nutrition)|diet]] modification.<ref>''Aliment Pharmacol Ther.'' 2005 Nov 1;22(9):749-57.</ref>
* [[Stress (medicine)|Stress]] [[Peptic ulcer|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]] (VAP).<ref>''Respir Care''. 2005 Jun;50(6):725-39; discussion 739-41.</ref>
* Prevention of [[Stenosis|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>


* Onset: 1–2 hr (initial onset for [[peptic ulcer disease]] (PUD))
==Adverse reactions==
* Absorption: <5% Orally
The most common [[adverse effect|side effects]] seen are [[constipation]] and [[bezoar]] formation. Less commonly reported include [[flatulence]], [[cephalalgia]] ([[headache]]), [[hypophosphatemia]], and [[xerostomia]] ([[dry mouth]]).
* Duration: Up to 6 hours due to high affinity for defective mucosa ([[Peptic Ulcer|PUD]])
Nursing mothers: Uncertain.
* [[Bioavailability]]: 5%, sucralfate is considered non-systemic, sucrose octasulfate: 5%, aluminum: 0.005%
* Metabolism: Not metabolized, excreted unchanged in urine
* Excretion: Primarily in feces as unchanged drug<ref name=":0" /><ref>{{Cite book|title = AHFS drug information McEvoy GK, ed. Sucralfate| vauthors = McEvoy GK |publisher = AHFS|year = 2007|pages = 2983–5}}</ref>


== Society and culture ==
==Notes==
=== Brand names ===
<references/>
{{unreferenced section|date=February 2024}}
Brand names include Carafate in the US, Sucramal in Italy, Sucrafil, Sufrate, Sucralpro, Sucralcoat, Pepsigard, Sucral, Hapifate, Sucralpro tablets and Sucralpro cream in India, Sutra or Musin in parts of South-East Asia, Sulcrate in Canada, Discral (sucralfato) in México, Ulsanic in South Africa and Israel, Andapsin in Sweden, Antepsin in Turkey, Sucracell in India, and Ulsidex in Indonesia


==References==
== References ==
{{reflist}}
* 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}}
{{Drugs for peptic ulcer and GORD}}
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[[Category:Drugs acting on the gastrointestinal system and metabolism]]
[[Category:Drugs acting on the gastrointestinal system and metabolism]]
[[Category:Equine medications]]
[[Category:Equine medications]]
[[Category:Disaccharides]]
[[Category:Disaccharides]]
[[Category:Organosulfates]]
[[Category:Drugs developed by AbbVie]]
[[Category:aluminium compounds]]
[[Category:Aluminium compounds]]
[[Category:Wikipedia medicine articles ready to translate]]
[[Category:Sulfate esters]]


[[de:Sucralfat]]
[[es:Sucralfato]]
[[hu:Szukralfát]]
[[ja:スクラルファート]]
[[pt:Sucralfato]]
[[ru:Противоязвенные препараты и препараты для лечения гастроэзофагеального рефлюкса#Сукралфат]]
[[ru:Противоязвенные препараты и препараты для лечения гастроэзофагеального рефлюкса#Сукралфат]]

Latest revision as of 03:03, 10 December 2024

Sucralfate
Clinical data
Trade namesCarafate
AHFS/Drugs.comMonograph
MedlinePlusa681049
License data
Routes of
administration		By mouth, rectal
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability3-5% (local acting)
MetabolismGI; liver: unknown
Elimination half-lifeunknown
ExcretionFeces, urine
Identifiers
  • Hexadeca-μ-hydroxytetracosahydroxy[μ8-[1,3,4,6-tetra-O-sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis(hydrogen sulfato)8-)]]hexadecaaluminum[2]
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.053.636 Edit this at Wikidata
Chemical and physical data
FormulaC12H54Al16O75S8
Molar mass2086.67 g·mol−1
 ☒NcheckY (what is this?)  (verify)

Sucralfate, sold under various brand names, is a medication used to treat stomach ulcers, gastroesophageal reflux disease (GERD), radiation proctitis, and stomach inflammation and to prevent stress ulcers.[3][4][5] Its usefulness in people infected by H. pylori is limited.[3] It is used by mouth (for upper GIT ulcers) and rectally (for radiation proctitis).[3][5]

Common side effects include constipation.[3] Serious side effects may include bezoar formation and encephalopathy.[6] Use appears to be safe in pregnancy and breastfeeding.[6] How it works is unclear but is believed to involve binding to the ulcer and protecting it from further damage.[3][6]

Sucralfate was approved for medical use in the United States in 1981.[3] It is available as a generic medication.[6][7] In 2022, it was the 214th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[8][9]

Medical uses

[edit]

Sucralfate is used for the treatment of active duodenal ulcers not related to the use of nonsteroidal anti-inflammatory drugs (NSAIDs), as the mechanism behind these ulcers is due to acid oversecretion.[1] It is not FDA approved for gastric ulcers, but is widely used because of evidence of efficacy.[10] The use for sucralfate in peptic ulcer disease has diminished recently, but it is still the preferred agent for stress ulcer prevention.[11][12][13][14]

Sucralfate has also been used for the following conditions:

Side effects

[edit]

The most common side effect seen is constipation (2–3%). Less commonly reported side effects (<0.5%) include flatulence, headache, hypophosphatemia, xerostomia (dry mouth), and bezoar formation.[24][25][26] Use of this drug is not recommended for people with chronic kidney failure, as it might cause aluminium accumulation and toxicity. A few well-controlled studies have been carried out investigating the safety and efficacy of sucralfate in children and pregnant women (Pregnancy Category B).[1][27][28]

Mechanism of action

[edit]

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.[29] 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.[29] In addition, sucralfate prevents back diffusion of hydrogen ions, and absorbs both pepsin and bile acids.

It has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.[1][30]

Pharmacokinetics

[edit]
  • Onset: 1–2 hr (initial onset for peptic ulcer disease (PUD))
  • Absorption: <5% Orally
  • Duration: Up to 6 hours due to high affinity for defective mucosa (PUD)
  • Bioavailability: 5%, sucralfate is considered non-systemic, sucrose octasulfate: 5%, aluminum: 0.005%
  • Metabolism: Not metabolized, excreted unchanged in urine
  • Excretion: Primarily in feces as unchanged drug[28][31]

Society and culture

[edit]

Brand names

[edit]

Brand names include Carafate in the US, Sucramal in Italy, Sucrafil, Sufrate, Sucralpro, Sucralcoat, Pepsigard, Sucral, Hapifate, Sucralpro tablets and Sucralpro cream in India, Sutra or Musin in parts of South-East Asia, Sulcrate in Canada, Discral (sucralfato) in México, Ulsanic in South Africa and Israel, Andapsin in Sweden, Antepsin in Turkey, Sucracell in India, and Ulsidex in Indonesia

References

[edit]
  1. ^ a b c d "DailyMed - Carafate - sucralfate suspension". dailymed.nlm.nih.gov. Retrieved 4 November 2015.
  2. ^ Merck Index, 12th Edition, 9049.
  3. ^ a b c d e f "Sucralfate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. 22 May 2023.
  4. ^ Maton PN (November 2003). "Profile and assessment of GERD pharmacotherapy". Cleveland Clinic Journal of Medicine. 70 (Suppl 5): S51-70. doi:10.3949/ccjm.70.Suppl_5.S51. PMID 14705381.
  5. ^ a b c Mendenhall WM, McKibben BT, Hoppe BS, Nichols RC, Henderson RH, Mendenhall NP (October 2014). "Management of radiation proctitis". American Journal of Clinical Oncology. 37 (5): 517–23. doi:10.1097/COC.0b013e318271b1aa. PMID 23241500. S2CID 12129192.
  6. ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 73. ISBN 9780857113382.
  7. ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.
  8. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  9. ^ "Sucralfate Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.
  10. ^ a b Hixson LJ, Kelley CL, Jones WN, Tuohy CD (April 1992). "Current trends in the pharmacotherapy for peptic ulcer disease". Archives of Internal Medicine. 152 (4): 726–32. doi:10.1001/archinte.152.4.726. PMID 1558429.
  11. ^ Hunt RH (August 1991). "Treatment of peptic ulcer disease with sucralfate: a review". The American Journal of Medicine. 91 (2A): 102S–106S. doi:10.1016/0002-9343(91)90459-b. PMID 1882894.
  12. ^ Fashner J, Gitu AC (February 2015). "Diagnosis and Treatment of Peptic Ulcer Disease and H. pylori Infection". American Family Physician. 91 (4): 236–42. PMID 25955624.
  13. ^ "ASHP Therapeutic Guidelines on Stress Ulcer Prophylaxis. ASHP Commission on Therapeutics and approved by the ASHP Board of Directors on November 14, 1998". American Journal of Health-System Pharmacy. 56 (4): 347–79. February 1999. doi:10.1093/ajhp/56.4.347. PMID 10690219.
  14. ^ Monnig AA, Prittie JE (October 2011). "A review of stress-related mucosal disease". Journal of Veterinary Emergency and Critical Care. 21 (5): 484–95. doi:10.1111/j.1476-4431.2011.00680.x. PMID 22316196.
  15. ^ Si JM, Wang LJ, Chen SJ, Zhao L, Dai N (2003). "Quality of life and cost-effectiveness of combined therapy for reflux esophagitis". Journal of Zhejiang University Science A. 4 (5): 602–6. Bibcode:2003JZUSA...4..602J. doi:10.1631/jzus.2003.0602. PMID 12958722. S2CID 118845033.
  16. ^ Saunders DP, Epstein JB, Elad S, Allemano J, Bossi P, van de Wetering MD, et al. (November 2013). "Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients". Supportive Care in Cancer. 21 (11): 3191–207. doi:10.1007/s00520-013-1871-y. PMID 23832272.{{cite journal}}: CS1 maint: overridden setting (link)
  17. ^ Richter JE (November 2005). "Review article: the management of heartburn in pregnancy". Alimentary Pharmacology & Therapeutics. 22 (9): 749–57. doi:10.1111/j.1365-2036.2005.02654.x. PMID 16225482.
  18. ^ Safdar N, Crnich CJ, Maki DG (June 2005). "The pathogenesis of ventilator-associated pneumonia: its relevance to developing effective strategies for prevention". Respiratory Care. 50 (6): 725–39, discussion 739–41. PMID 15913465.
  19. ^ Temir ZG, Karkiner A, Karaca I, Ortaç R, Ozdamar A (1 January 2005). "The effectiveness of sucralfate against stricture formation in experimental corrosive esophageal burns". Surgery Today. 35 (8): 617–22. doi:10.1007/s00595-004-3005-0. PMID 16034539. S2CID 38080924.
  20. ^ Theodore M. Bayless (14 May 2014). Advanced Therapy of Inflammatory Bowel Disease: Ulcerative Colitis (Volume 1), 3e. PMPH-USA. p. 331. ISBN 978-1-60795-216-9.
  21. ^ Chun M, Kang S, Kil HJ, Oh YT, Sohn JH, Ryu HS (January 2004). "Rectal bleeding and its management after irradiation for uterine cervical cancer". International Journal of Radiation Oncology, Biology, Physics. 58 (1): 98–105. doi:10.1016/s0360-3016(03)01395-6. PMID 14697426.
  22. ^ "Guideline". www.poison.org. Retrieved 5 July 2018.
  23. ^ Anfang RR, Jatana KR, Linn RL, Rhoades K, Fry J, Jacobs IN (January 2019). "pH-neutralizing esophageal irrigations as a novel mitigation strategy for button battery injury". The Laryngoscope. 129 (1): 49–57. doi:10.1002/lary.27312. PMID 29889306. S2CID 47004940.
  24. ^ "Study of possible correlation between BEZOAR and SUCRALFATE". MedsFacts.com. Archived from the original on 18 September 2016.
  25. ^ "Carafate Package Insert" (PDF). 12 September 2013. Retrieved 2 November 2015.
  26. ^ "ASHP Therapeutic Guidelines on Stress Ulcer Prophylaxis. ASHP Commission on Therapeutics and approved by the ASHP Board of Directors on November 14, 1998". American Journal of Health-System Pharmacy. 56 (4): 347–79. February 1999. doi:10.1093/ajhp/56.4.347. PMID 10690219.
  27. ^ Phupong V, Hanprasertpong T (September 2015). "Interventions for heartburn in pregnancy". The Cochrane Database of Systematic Reviews. 2015 (9): CD011379. doi:10.1002/14651858.CD011379.pub2. PMC 9235294. PMID 26384956.
  28. ^ a b Steiner K, Bühring KU, Faro HP, Garbe A, Nowak H (1 January 1982). "Sucralfate: pharmacokinetics, metabolism and selective binding to experimental gastric and duodenal ulcers in animals". Arzneimittel-Forschung. 32 (5): 512–8. PMID 6896647.
  29. ^ a b Brogden RN, Heel RC, Speight TM, Avery GS (March 1984). "Sucralfate. A review of its pharmacodynamic properties and therapeutic use in peptic ulcer disease". Drugs. 27 (3): 194–209. doi:10.2165/00003495-198427030-00002. PMID 6368184. S2CID 260482050.
  30. ^ Korman MG, Bolin TD, Szabo S, Hunt RH, Marks IN, Glise H (1 August 1994). "Sucralfate: the Bangkok review". Journal of Gastroenterology and Hepatology. 9 (4): 412–5. doi:10.1111/j.1440-1746.1994.tb01264.x. PMID 7948825. S2CID 41841680.
  31. ^ McEvoy GK (2007). AHFS drug information McEvoy GK, ed. Sucralfate. AHFS. pp. 2983–5.
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