Sucralfate

Sucralfate
Names
Trade namesCarafate
IUPAC name
  • Hexadeca-μ-hydroxytetracosahydroxy[μ8-[1,3,4,6-tetra-O-sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis(hydrogen sulfato)8-)]]hexadecaaluminum[1]
Clinical data
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • B
Routes of
use
By mouth, rectal
Defined daily dose4 gram[2]
External links
AHFS/Drugs.comMonograph
MedlinePlusa681049
Legal
License data
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetics
Bioavailability3-5% (local acting)
MetabolismGI; liver: unknown
Elimination half-lifeunknown
ExcretionFeces, urine
Chemical and physical data
FormulaC12H54Al16O75S8
Molar mass2086.67 g·mol−1

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 and rectally.[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] In the United States the wholesale cost is about US$0.22 per dose.[7] In 2017, it was the 218th most commonly prescribed medication in the United States, with more than two million prescriptions.[8][9]

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.[10] It is not FDA approved for gastric ulcers, but is widely used because of evidence of efficacy.[11] The use for sucralfate in peptic ulcer disease has diminished recently, but it is still the preferred agent for stress ulcer prevention.[12][13][14][15]

Sucralfate has also been used for the following conditions:

Dosage

The defined daily dose is 4 grams by mouth.[2]

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.[25][26][27] 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).[10][28][29]

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.[30] 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.[30] In addition, sucralfate prevents back diffusion of hydrogen ions, and adsorbs 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.[10][31]

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 (PUD)

Bioavailability: 5% as sucralfate is considered non-systemic, sucrose octasulfate: 5%, aluminum:0.005%

Metabolism: Not metabolized, excreted unchanged in urine

Excretion: Primarily in urine as unchanged drug[29][32]

Names

Brand names include Carafate in U.S.A., Sucramal in Italy, Sucrafil, Sufrate, Sucralpro, Sucralcoat, Pepsigard, Sucral, Hapifate, Sucralpro 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 and Antepsin in Turkey.

Society and culture

Cost

In the United States the wholesale cost is about US$0.22 per dose.[7] In 2017, it was the 218th most commonly prescribed medication in the United States, with more than two million prescriptions.[8][9]

References

  1. Merck Index, 12th Edition, 9049.
  2. 1 2 "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 22 January 2021. Retrieved 8 September 2020.
  3. 1 2 3 4 5 6 "Sucralfate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 2020-08-15. Retrieved 2019-04-08.
  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. 1 2 3 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. 1 2 3 4 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 73. ISBN 9780857113382.
  7. 1 2 "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Archived from the original on 2019-03-06. Retrieved 3 March 2019.
  8. 1 2 "The Top 300 of 2020". ClinCalc. Archived from the original on 18 March 2020. Retrieved 11 April 2020.
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  10. 1 2 3 "DailyMed - CARAFATE - sucralfate suspension". dailymed.nlm.nih.gov. Archived from the original on 2015-09-10. Retrieved 2015-11-04.
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  20. Temir ZG, Karkiner A, Karaca I, Ortaç R, Ozdamar A (2005-01-01). "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.
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  30. 1 2 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.
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