Sucralfate

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Sucralfate
Systematic (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
Trade namesCarafate
AHFS/Drugs.commonograph
MedlinePlusa681049
Pregnancy cat.B
Legal status℞-only
Routesoral, suspension, rectal suspension
Pharmacokinetic data
Bioavailability3-5% (local acting)
MetabolismGI; liver: unknown
Half-lifeunknown
Excretionfeces, urine
Identifiers
CAS number54182-58-0 YesY
ATC codeA02BX02
PubChemCID 6398525
DrugBankDB00364
ChemSpider4911161 N
UNIIXX73205DH5 N
ChEMBLCHEMBL611727 N
Chemical data
FormulaC12H54Al16O75S8[1]
Mol. mass2086.75 g/mol[1]
 N (what is this?)  (verify)
 
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Sucralfate
Systematic (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
Trade namesCarafate
AHFS/Drugs.commonograph
MedlinePlusa681049
Pregnancy cat.B
Legal status℞-only
Routesoral, suspension, rectal suspension
Pharmacokinetic data
Bioavailability3-5% (local acting)
MetabolismGI; liver: unknown
Half-lifeunknown
Excretionfeces, urine
Identifiers
CAS number54182-58-0 YesY
ATC codeA02BX02
PubChemCID 6398525
DrugBankDB00364
ChemSpider4911161 N
UNIIXX73205DH5 N
ChEMBLCHEMBL611727 N
Chemical data
FormulaC12H54Al16O75S8[1]
Mol. mass2086.75 g/mol[1]
 N (what is this?)  (verify)

Sucralfate is a cytoprotective agent, an oral gastrointestinal medication primarily indicated for the treatment of active duodenal ulcers. Brand names include Sucramal in Italy; Carafate in U.S.A.; Pepsigard, Sucral, Sucrafil, Hapifate in India; Sutra or Musin in parts of South-East Asia; Sulcrate in Canada; Ulsanic in South Africa and Israel; and Antepsin in Turkey. Sucralfate is also used for the treatment of gastroesophageal reflux disease (GERD)[2] and stress ulcers. Unlike the other classes of medications used for treatment of peptic ulcers, sucralfate is a sucrose sulfate-aluminium complex that binds to the mucosa, thus creating a physical barrier that impairs diffusion of hydrochloric acid in the gastrointestinal tract and prevents degradation of mucus by acid. It also stimulates bicarbonate output and acts like an acid buffer with cytoprotective properties. Sucralfate was approved by the U.S. Food and Drug Administration (FDA) in 1981.

Contents

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, it prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. Recently, it has been indicated that sucralfate also stimulates the increase of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.

Clinical uses

The only FDA-approved indication for sucralfate is for the treatment of active duodenal ulcers not related to NSAID usage because the mechanism behind these ulcers is secondary to acid oversecretion. It is not technically approved for gastric ulcers 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 ulcer prophylaxis.

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.[7]

Adverse reactions

The most common side effects seen are constipation 2-3% and bezoar formation. Less commonly reported include flatulence, cephalalgia (headache), hypophosphatemia, and xerostomia (dry mouth). Avoid using this drug in patients with chronic renal failure, it might cause them aluminum-induced nephropathy. Nursing mothers: Uncertain.

References

  1. ^ a b c Merck Index, 12th Edition, 9049.
  2. ^ Maton PN (2003). "Profile and assessment of GERD pharmacotherapy". Cleve Clin J Med 70 Suppl 5: S51–70. doi:10.3949/ccjm.70.Suppl_5.S51. PMID 14705381.
  3. ^ Jian-Min, Si; Liang-Jing, Wang; Shu-Jie, Chen; Lan, Zhao; Ning, Dai (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.
  4. ^ Aliment Pharmacol Ther. 2005 Nov 1;22(9):749-57.
  5. ^ Respir Care. 2005 Jun;50(6):725-39; discussion 739-41.
  6. ^ Surg Today. 2005;35(8):617-22.
  7. ^ International Journal Radiation Oncology Biological Physics, 2004 Jan 1;58(1):98-105

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