Zpallack23/sandbox
Clinical data
Trade namesCarafate
AHFS/Drugs.comMonograph
MedlinePlusa681049
Pregnancy
category
  • B
Routes of
administration
oral, suspension, rectal suspension
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
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[1]
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC12H54Al16O75S8
Molar mass2086.75 g/mol[1] g·mol−1
 ☒NcheckY (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.; Sufrate, Sucralcoat, 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.

Mechanism of action

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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

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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.

Indication

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DUODENAL ULCER: It is used in the short-term (up to 8 weeks) treatment of duodenal ulcer. [9]

Antacids may be used as adjuncts to sucralfate therapy to relieve pain, but should not be taken within 30 minutes before or after administration of sucralfate.

GASTRIC ULCER: Sucralfate has been used in the treatment of patients with gastric ulcer

Prevention and treatment of chemotherapy induced mucositis

Burn

Gastric ulcer

Hyperphosphatemia

Proctitis

Stress ulcer prophylaxis

Ulcer of rectum

Adverse reactions

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The most common side effect seen is constipation 2-3%. Less commonly reported include flatulence, cephalalgia (headache), hypophosphatemia, xerostomia (dry mouth), and bezoar[10] formation. Avoid using this drug in patients with chronic renal failure, it might cause them aluminum-induced nephropathy. Nursing mothers: Uncertain. CAN ADD PACKAGE INSERT AS A REFERENCE

Pharmacokinetics

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Onset: 1-2 hr (initial onset for PUD)

Absorption: <5% (PO)

Duration: Up to 6 hr 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

WHERE ARE THE REFERENCES??

References

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  1. ^ a b 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. S2CID 118845033.
  4. ^ Mendenhall, William M.; McKibben, Brian T.; Hoppe, Bradford S.; Nichols, Romaine C.; Henderson, Randal H.; Mendenhall, Nancy P. (2014-10-01). "Management of radiation proctitis". American Journal of Clinical Oncology. 37 (5): 517–523. doi:10.1097/COC.0b013e318271b1aa. ISSN 1537-453X. PMID 23241500. S2CID 12129192.
  5. ^ Richter, J. E. (2005-11-01). "Review article: the management of heartburn in pregnancy". Alimentary Pharmacology & Therapeutics. 22 (9): 749–757. doi:10.1111/j.1365-2036.2005.02654.x. ISSN 0269-2813. PMID 16225482. S2CID 22545894.
  6. ^ Safdar, Nasia; Crnich, Christopher J.; Maki, Dennis G. (2005-06-01). "The pathogenesis of ventilator-associated pneumonia: its relevance to developing effective strategies for prevention". Respiratory Care. 50 (6): 725–739, discussion 739-741. ISSN 0020-1324. PMID 15913465.
  7. ^ Temir, Z. Günyüz; Karkiner, Aytaç; Karaca, Irfan; Ortaç, Ragip; Ozdamar, Aykut (2005-01-01). "The effectiveness of sucralfate against stricture formation in experimental corrosive esophageal burns". Surgery Today. 35 (8): 617–622. doi:10.1007/s00595-004-3005-0. ISSN 0941-1291. PMID 16034539. S2CID 38080924.
  8. ^ Chun, Mison; Kang, Seunghee; Kil, Hoon-Jong; Oh, Young-Taek; Sohn, Jeong-Hye; Ryu, Hee-Suk (2004-01-01). "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. ISSN 0360-3016. PMID 14697426.
  9. ^ "Carafate Package Insert" (PDF). Retrieved 11/02/2015. {{cite web}}: Check date values in: |accessdate= (help)
  10. ^ http://medsfacts.com/study-SUCRALFATE-causing-BEZOAR.php
  • Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. (2004).
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Category:Drugs acting on the gastrointestinal system and metabolism Category:Equine medications Category:Disaccharides Category:Organosulfates Category:Aluminium compounds