Sucralfate: Difference between revisions

{{Short description|Chemical compound and gastrointestinal medication}}

{{Use dmy dates|date=August 2021}}

{{Drugbox

| Verifiedfields = changed

| Watchedfields = changed

| 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_supplemental =

| legal_US = Rx-only

| legal_US_comment = <ref name="Carafate FDA label" />

| legal_status = Rx-only

<!-- Pharmacokinetic data -->

| protein_bound =

| elimination_half-life = unknown

| excretion = [[Feces]], [[urine]]

<!--Identifiers-->

| CAS_number_Ref = {{cascite|correct|??}}

| 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[μ₈-[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 2021, it was the 186th most commonly prescribed medication in the United States, with more than 2{{nbsp}}million prescriptions.<ref>{{cite web | title=The Top 300 of 2021 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=14 January 2024 | archive-date=15 January 2024 | archive-url=https://web.archive.org/web/20240115223848/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Sucralfate - Drug Usage Statistics | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Sucralfate | access-date = 14 January 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 }}</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 H₂ [[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==

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>

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]] E₂, [[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>

==Pharmacokinetics==

* 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 ([[Peptic Ulcer|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<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 ==

=== Brand names ===

{{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 ==

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