Sucralfate

Overview

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. Its usefulness in people infected by H. pylori is limited. It is used by mouth (for ulcers of the upper gastrointestinal tract) and rectally (for radiation proctitis).[1][2][3] WP

Common side effects include constipation. Serious side effects may include bezoar formation and encephalopathy. Use appears to be safe in pregnancy and breastfeeding. How it works is unclear but is believed to involve binding to the ulcer and protecting it from further damage.[1][4] WP

Sucralfate was approved for medical use in the United States in 1981. It is available as a generic medication. In 2023, it was the 240th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[1][4–7] WP

Uses, dosage and effects

Medical uses

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. In the United States, sucralfate is not approved by the Food and Drug Administration for gastric ulcers, but is widely used because of evidence of efficacy. The use for sucralfate in peptic ulcer disease has diminished recently, but it is still the preferred agent for stress ulcer prevention.[8–13] WP

Sucralfate has also been used for the following conditions: WP

• Active duodenal ulcer not related to NSAID use WP
• Maintenance therapy for resolved duodenal ulcers WP
• Gastric ulcer not related to NSAID use and gastritis due to GERD—Triple combination therapy with lansoprazole + cisapride + sucralfate can significantly improve symptoms and quality of life and was more cost-effective than ranitidine combination group.[14] WP
• Aphthous ulcer and stomatitis due to 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.[15] WP
• Gastro-esophageal reflux disease during pregnancy—First-line drug therapy combined with lifestyle and diet modification.[16] WP
• Stress ulcer prophylaxis—The use of sucralfate rather than H₂ antagonists for stress ulcer prophylaxis, and measures to prevent aspiration, such as continuous subglottic suctioning, have been shown to reduce the risk of ventilator-associated pneumonia (VAP). Sucralfate is less effective for prophylaxis against gastrointestinal bleeding than either a PPI or H2-blocker. For that reason, it is not commonly used for stress ulcer prophylaxis.[17] WP
• 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[18] WP
• Proctitis from ulcerative colitis[19] WP
• Rectal bleeding due to proctitis from radiation to treat cancers of the cervix, prostate, and colon.[3] WP
• Grade 1 bleeding experienced immediate relief with sucrasulfate enema for 1 month. WP
• Grade 2 bleeding, sucrasulfate enema] and/or coagulation were effective. WP
• Grade 3 bleeding lasted for 1 year despite frequent transfusions and coagulation. WP
• 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.[20] WP
• Treatment of anastomotic ulcer after gastric bypass surgery WP
• Sucralfate suspension is recommended by the US-based National Capital Poison Center (Poison Control) as an intervention for known or suspected button battery ingestions to reduce the risk and severity of injury to the esophagus prior to the battery's endoscopic removal.[21][22] WP
• Protection against ventilator-associated pneumonia - Reductions in gastric acidity and volumes increase bacterial overgrowth and the incidence of ventilator-associated pneumonia. 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. A majority of meta-analyses found that sucralfate therapy decreased the incidence of ventilator-associated pneumonia compared to H2-antagonists.[9] WP

Risks and side effects

Side effects

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. 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).[8][12][23–26] WP

Pharmacology

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, sucralfate prevents back diffusion of hydrogen ions, and absorbs both pepsin and bile acids.[27][28] WP

It has been thought that sucralfate also stimulates the production of prostaglandin E₂, epidermal growth factors (EGF), bFGF, and gastric mucus.[8][29] WP

Pharmacokinetics

• Onset: 1–2 hr (initial onset for peptic ulcer disease (PUD)) WP
• Absorption: <5% Orally WP
• Duration: Up to 6 hours due to high affinity for defective mucosa (PUD) WP
• Bioavailability: 5%, sucralfate is considered non-systemic, sucrose octasulfate: 5%, aluminum: 0.005% WP
• Metabolism: Not metabolized, excreted unchanged in urine WP
• Excretion: Primarily in feces as unchanged drug[26][30] WP

Legal status

Brand names

Brand names include: Carafate in the US, Sucramal in Italy, Sucrafil, Sufrate, Sucralpro, Sucral, Sutra, Sulcrate in Canada, Discral (sucralfato) in México, Ulsanic in South Africa and Israel, Andapsin in Sweden, Antepsin in Turkey, and Ulsidex in Indonesia.[31] WP

Chemistry

Formula

C11H60Al9O55S8 PC

Formula (Wikipedia infobox)

C12H54Al16O75S8 WP⚠ Wikipedia and PubChem give different formulas. Both are shown as each source has it.

Molar mass (g/mol)

1571.9 PC

SMILES

C([C@@H]1[C@H]([C@@H]([C@H]([C@@H](O1)O[C@]2([C@H]([C@@H]([C@H](O2)OS(=O)(=O)O)OS(=O)(=O)O)OS(=O)(=O)O)COS(=O)(=O)O)OS(=O)(=O)O)OS(=O)(=O)O)OS(=O)(=O)O)OS(=O)(=O)O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.[Al].[Al].[Al].[Al].[Al].[Al].[Al].[Al].[Al] PC

InChIKey

VGNZFVKOOSPYGY-UDJZYEQASA-N PC

PubChem CID

6398525

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Other Sucralfate Monograph for Professionals. 22 May 2023
2. Journal / agency Maton PN. Profile and assessment of GERD pharmacotherapy. Cleveland Clinic Journal of Medicine. November 2003. doi:10.3949/ccjm.70.Suppl_5.S51 · PMID 14705381
3. Journal / agency Mendenhall WM, McKibben BT, Hoppe BS, Nichols RC, Henderson RH, Mendenhall NP. Management of radiation proctitis. American Journal of Clinical Oncology. October 2014. doi:10.1097/COC.0b013e318271b1aa · PMID 23241500
4. Other British national formulary: BNF 76. 2018
5. Journal / agency Competitive Generic Therapy Approvals. 29 June 2023
6. Other The Top 300 of 2023
7. Other Sucralfate Drug Usage Statistics, United States, 2014 - 2023
8. Journal / agency DailyMed - Carafate - sucralfate suspension
9. Journal / agency Hixson LJ, Kelley CL, Jones WN, Tuohy CD. Current trends in the pharmacotherapy for peptic ulcer disease. Archives of Internal Medicine. April 1992. doi:10.1001/archinte.152.4.726 · PMID 1558429
10. Journal / agency Hunt RH. Treatment of peptic ulcer disease with sucralfate: a review. The American Journal of Medicine. August 1991. doi:10.1016/0002-9343(91)90459-b · PMID 1882894
11. Journal / agency Fashner J, Gitu AC. Diagnosis and Treatment of Peptic Ulcer Disease and H. pylori Infection. American Family Physician. February 2015. PMID 25955624
12. Journal / agency 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. February 1999. doi:10.1093/ajhp/56.4.347 · PMID 10690219
13. Journal / agency Monnig AA, Prittie JE. A review of stress-related mucosal disease. Journal of Veterinary Emergency and Critical Care. October 2011. doi:10.1111/j.1476-4431.2011.00680.x · PMID 22316196
14. Journal / agency Si JM, Wang LJ, Chen SJ, Zhao L, Dai N. Quality of life and cost-effectiveness of combined therapy for reflux esophagitis. Journal of Zhejiang University Science A. 2003. doi:10.1631/jzus.2003.0602 · PMID 12958722
15. Journal / agency 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. Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients. Supportive Care in Cancer. November 2013. doi:10.1007/s00520-013-1871-y · PMID 23832272
16. Journal / agency Richter JE. Review article: the management of heartburn in pregnancy. Alimentary Pharmacology & Therapeutics. November 2005. doi:10.1111/j.1365-2036.2005.02654.x · PMID 16225482
17. Journal / agency Safdar N, Crnich CJ, Maki DG. The pathogenesis of ventilator-associated pneumonia: its relevance to developing effective strategies for prevention. Respiratory Care. June 2005. PMID 15913465
18. Journal / agency Temir ZG, Karkiner A, Karaca I, Ortaç R, Ozdamar A. The effectiveness of sucralfate against stricture formation in experimental corrosive esophageal burns. Surgery Today. 1 January 2005. doi:10.1007/s00595-004-3005-0 · PMID 16034539
19. Other Theodore M. Bayless. Advanced Therapy of Inflammatory Bowel Disease: Ulcerative Colitis (Volume 1), 3e. 14 May 2014
20. Journal / agency Chun M, Kang S, Kil HJ, Oh YT, Sohn JH, Ryu HS. Rectal bleeding and its management after irradiation for uterine cervical cancer. International Journal of Radiation Oncology, Biology, Physics. January 2004. doi:10.1016/s0360-3016(03)01395-6 · PMID 14697426
21. Other Guideline
22. Journal / agency Anfang RR, Jatana KR, Linn RL, Rhoades K, Fry J, Jacobs IN. pH-neutralizing esophageal irrigations as a novel mitigation strategy for button battery injury. The Laryngoscope. January 2019. doi:10.1002/lary.27312 · PMID 29889306
23. Other Study of possible correlation between BEZOAR and SUCRALFATE
24. Journal / agency Carafate Package Insert. 12 September 2013
25. Journal / agency Phupong V, Hanprasertpong T. Interventions for heartburn in pregnancy. The Cochrane Database of Systematic Reviews. September 2015. doi:10.1002/14651858.CD011379.pub2 · PMID 26384956 · PMC9235294
26. Journal / agency Steiner K, Bühring KU, Faro HP, Garbe A, Nowak H. Sucralfate: pharmacokinetics, metabolism and selective binding to experimental gastric and duodenal ulcers in animals. Arzneimittel-Forschung. 1 January 1982. PMID 6896647
27. Journal / agency Brogden RN, Heel RC, Speight TM, Avery GS. Sucralfate. A review of its pharmacodynamic properties and therapeutic use in peptic ulcer disease. Drugs. March 1984. doi:10.2165/00003495-198427030-00002 · PMID 6368184
28. Other Drugs Used to Treat Gastrointestinal Ulcers in Monogastric Animals - Pharmacology
29. Journal / agency Korman MG, Bolin TD, Szabo S, Hunt RH, Marks IN, Glise H. Sucralfate: the Bangkok review. Journal of Gastroenterology and Hepatology. 1 August 1994. doi:10.1111/j.1440-1746.1994.tb01264.x · PMID 7948825
30. Other McEvoy GK. AHFS drug information McEvoy GK, ed. Sucralfate. 2007
31. Other Sucralfate (International database)

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.