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Isabelfong 23/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, marketed as Carafate in the U.S., is an oral gastrointestinal medication indicated for the short term treatment of active duodenal ulcers.[2] Sucralfate can also be used for the treatment of gastroesophageal reflux disease (GERD) and stress ulcers.[3][4] Unlike other classes of medications used for the treatment of peptic ulcers, sucralfate is a sucrose sulfate-aluminium complex that binds to the ulcer, creating a physical barrier that protects the gastrointestinal tract from stomach acid and prevents the degradation of mucus.[5][6] It also promotes bicarbonate production and acts like an acid buffer with cytoprotective properties.[7] Sucralfate is marketed multiple countries including as Asicot in India, Disuo in China and Citogel in Italy.

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.[5] 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.[5] In addition, it prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids. Recently, it has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus.[6][8][9]

Clinical uses

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Currently, sucralfate is FDA approved for the treatment of active duodenal ulcers not related to NSAID usage, as the mechanism behind these ulcers is due to acid oversecretion.[2] It is not FDA approved for gastric ulcers, as the main mechanism of gastric ulcers is not due to acid oversecretion but rather from diminished protection. The use of sucralfate in peptic ulcer disease has diminished recently, but it remains one of the preferred agents for stress ulcer prophylaxis.[10][11][4][9]

Adverse reactions

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The most common side effect seen while using sucralfate is constipation (2-3%). Less commonly reported (<0.5%) include flatulence, headache, hypophosphatemia, xerostomia (dry mouth), and bezoar formation.[18][19][20]

Use in Renal Impaired and Hepatic Impaired Populations

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Although manufacturer did not provide dose adjustment in the use of Sucralfate in the renal impaired and hepatic impaired populations, it recommends the use of Sucralfate with caution in people with chronic kidney failure, as it might cause aluminium accumulation and toxicity.

Sucralfate is not known to be metabolized by the liver. [21]

Pregnancy and Lactation

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There is a limited number of well-controlled studies investigating the safety and efficacy of sucralfate in children and pregnant women. It is not known whether sucralfate is excreted in breast milk following oral administration due to its poor absorption.[21][22]

Pharmacokinetics

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

Absorption: <5% (PO)

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 [23][24]

References

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  1. ^ a b Merck Index, 12th Edition, 9049.
  2. ^ a b "DailyMed - CARAFATE - sucralfate suspension". dailymed.nlm.nih.gov. Retrieved 2015-11-04.
  3. ^ 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.
  4. ^ a b "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: AJHP: Official Journal of the American Society of Health-System Pharmacists. 56 (4): 347–379. 1999-02-15. doi:10.1093/ajhp/56.4.347. ISSN 1079-2082. PMID 10690219.
  5. ^ a b c Brogden, R. N.; Heel, R. C.; Speight, T. M.; Avery, G. S. (1984-03-01). "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. ISSN 0012-6667. PMID 6368184.
  6. ^ a b Korman, M. G.; Bolin, T. D.; Szabo, S.; Hunt, R. H.; Marks, I. N.; Glise, H. (1994-08-01). "Sucralfate: the Bangkok review". Journal of Gastroenterology and Hepatology. 9 (4): 412–415. doi:10.1111/j.1440-1746.1994.tb01264.x. ISSN 0815-9319. PMID 7948825. S2CID 41841680.
  7. ^ Lam, Shiu Kum; Ching, Chi Kong (1994). "Sucralfate in clinical practice". Journal of Gastroenerology and Hepatology. 9 (4): 401–11. doi:10.1111/j.1440-1746.1994.tb01263.x. PMID 7948824. S2CID 26217267.
  8. ^ "DailyMed - CARAFATE - sucralfate suspension". dailymed.nlm.nih.gov. Retrieved 2015-11-04.
  9. ^ a b Monnig, Andrea A.; Prittie, Jennifer E. (2011-10-01). "A review of stress-related mucosal disease". Journal of Veterinary Emergency and Critical Care (San Antonio, Tex.: 2001). 21 (5): 484–495. doi:10.1111/j.1476-4431.2011.00680.x. ISSN 1476-4431. PMID 22316196.
  10. ^ Hunt, R. H. (1991-08-08). "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. ISSN 0002-9343. PMID 1882894.
  11. ^ Fashner, Julia; Gitu, Alfred C. (2015-02-15). "Diagnosis and Treatment of Peptic Ulcer Disease and H. pylori Infection". American Family Physician. 91 (4): 236–242. ISSN 1532-0650. PMID 25955624.
  12. ^ 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.
  13. ^ 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.
  14. ^ 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.
  15. ^ 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.
  16. ^ 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.
  17. ^ 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.
  18. ^ "Carafate Package Insert" (PDF). September 12, 2013. Retrieved November 2, 2015.
  19. ^ "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: AJHP: Official Journal of the American Society of Health-System Pharmacists. 56 (4): 347–379. 1999-02-15. doi:10.1093/ajhp/56.4.347. ISSN 1079-2082. PMID 10690219.
  20. ^ http://medsfacts.com/study-SUCRALFATE-causing-BEZOAR.php
  21. ^ a b "Sucralfate Monograph" (PDF).
  22. ^ Phupong, Vorapong; Hanprasertpong, Tharangrut (2015-01-01). "Interventions for heartburn in pregnancy". The Cochrane Database of Systematic Reviews. 9 (9): CD011379. doi:10.1002/14651858.CD011379.pub2. ISSN 1469-493X. PMID 26384956.
  23. ^ Steiner, K.; Bühring, K. U.; Faro, H. P.; Garbe, A.; Nowak, H. (1982-01-01). "Sucralfate: pharmacokinetics, metabolism and selective binding to experimental gastric and duodenal ulcers in animals". Arzneimittel-Forschung. 32 (5): 512–518. ISSN 0004-4172. PMID 6896647.
  24. ^ McEvoy, GK (2007). AHFS drug information McEvoy GK, ed. Sucralfate. AHFS. pp. 2983–5.
  • 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


Eric citations: Mechanisms of gastroduodenal protection by sucralfate. Rees WD. Am J Med. 1991 Aug 8;91(2A):58S-63S. Review.

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