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Sucralfate

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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 2021, it was the 186th most commonly prescribed medication in the United States, with more than 2 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

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  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 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  9. ^ "Sucralfate - Drug Usage Statistics". ClinCalc. Retrieved 14 January 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. 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.
  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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