Skip to main content
SpringerLink
Log in

Binding of Bile Acids by Sucralfate

  • Chapter
Sucralfate

  • 288 Accesses

Abstract

The gastric mucosal barrier is considered to play an important role in protecting the gastric mucosa from the destructive effects of several luminal agents.1,2 The breakdown of the gastric mucosal barrier has been associated with erosive mucosal injury and ulceration induced by such factors as stress and endogenous compounds including bile salts and urea. 2–5

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 84.99
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 109.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 109.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Davenport HW: Destruction of mucosal barrier by detergents and urea. Gastroenterology 54:175–182, 1968. Classical paper on definition and properties of the gastric mucosal barrier.

    PubMed  CAS  Google Scholar 

  2. Ritchie WP: Bile acids, the “barrier”, and reflux-related clinical disorders of the gastric mucosa. Surgery 82:192–200, 1977. Paper with original data suggesting that bile acid reflux may be responsible for gastritis and barrier-breaking.

    PubMed  CAS  Google Scholar 

  3. Duane WC, Wiegand DM, Siebert CE: Bile acid and bile salt disrupt gastric mucosal barrier by different mechanisms. Am J Physiol 242:G95–G99, 1982.In vitro study demonstrating effects of bile acids on the gastric mucosal barrier.

    PubMed  CAS  Google Scholar 

  4. Black RB, Hole D, Rhodes J: Bile damage to gastric mucosal barrier: The influence of pH and bile acid concentration. Gastroenterology 61:178–184, 1971. Paper showing gastric mucosal injury by bile, as well as concentration-and pH-dependence of the damaging effect.

    Google Scholar 

  5. Geall MG, Phillips SF, Summerskill WHJ: The profile of gastric potential difference in man: Effect of aspirin, alcohol, bile and exogenous acid. Gastroenterology 58:437–442, 1970. Original paper demonstrating effects of aspirin on transmural gastric potential difference in humans.

    PubMed  CAS  Google Scholar 

  6. DuPlessis DJ: Pathogenesis of gastric ulceration. Lancet 1:974–978. 1965. Classical hypothetical paper stressing the importance of bile acids in the pathogenesis of gastric ulcers.

    Article  PubMed  CAS  Google Scholar 

  7. Clain JE, Malagelada JR, Chadwick VS, et al: Binding properties in vitro of antacids for conjugated bile acids. Gastroenlerology 73:556–560, 1977. One of the first papers on in vitro bile acid binding properties of antacids.

    CAS  Google Scholar 

  8. Caspary WF: Einfluβ von Aspirin, Antacida, Alkohol und Gallensauren auf die transmurale elektrische Potentialdifferenz des menschlichen Magens. Dtsch Med Wochenschr 100:1263–1266, 1975. Original paper on the effect of various gastric mucosal barrier breakers on transmural gastric potential difference in humans.

    Article  PubMed  CAS  Google Scholar 

  9. Nagashima R: Development and characteristics of sucralfate. J Clin Gastroenterol 3(suppl 2):105–110, 1981. Excellent review article on the properties of sucralfate.

    Google Scholar 

  10. Nagashima R: Mechanism of action of sucralfate. J Clin Gastroenterol 3(suppl 2):117–127, 1981. Review article with emphasis of the mechanism of action of sucralfate.

    PubMed  CAS  Google Scholar 

  11. McCarthy DM: Sucralfate. New Engl J Med 325:1017–1025. 1991. Most recent comprehensive review article on sucralfate, its mechanism of action, and results of clinical trials.

    Article  PubMed  CAS  Google Scholar 

  12. Bruusgaard A, Elsborg L, Reinecke V: Bile acid binding properties of sucralfate, in Caspary WF (ed): Duodenal Ulcer, Gastric Ulcer: Sucralfate, a New Therapeutic Concept. Munich, Urban &0026; Schwarzenberg, 1981, pp 28–31. Original data of bile acid binding by sucralfate and antacids using natural bile.

    Google Scholar 

  13. Caspary WF: Einfluβ von Glykocholsäure und Sucralfat auf die transmurale elektrische Potentialdifferenz des menschlichen Magens. in Caspary WF (ed): Ulcus duodeni, Ulcus ventriculi Sucralfat, eine neue therapeutische Konzeption. Munich, Urban & Schwarzenberg, 1980. pp 22–27. Clinical study in humans testing the effect of sucralfate on glycocholic acid-induced decrease of gastric transmural potential difference.

    Google Scholar 

  14. Caspary WF, Graf S. Binding of bile acids by sucralfate and cholestyramine, in Caspary WF (ed): Duodenal Ulcer, Gastric Ulcer: Sucralfate, a New Therapeutic Concept. Munich, Urban &0026; Schwarzenberg, 1981, pp 32–38. Comparative in vitro study testing bile acid binding properties of cholestyramine and sucralfate.

    Google Scholar 

  15. Graham DY, Sackman JW, Giesing DH, et at. In vitro adsorption of bile salts and aspirin to sucralfate. Dig Dis Sci 29:402–406, 1984. Original data of a careful in vitro study on bile acid binding properties of sucralfate and aspirin.

    Article  PubMed  CAS  Google Scholar 

  16. Shiau Y-F, Schenkein JP, Liu H-J, et al: Bile salt binding properties of commonly used gastrointestinal drugs: Maalox, Carafate, and questran. J Pharm Sci 77:527–530, 1992 (Abstract). In vitro study comparing bile salt binding properties of Maalox, sucralfate (Carafate) and cholestyramine.

    Article  Google Scholar 

  17. Lipsett P, Gadacz TR: Bile salt binding by Maalox, sucralfate, and Meciadanol: In vitro and clinical comparisons. J Surg Res 47:403–406, 1989. In vitro study comparing bile salt properties at various pH values of Maalox, sucralfate and the flavonoid, Meciadanol, using pure bile acids.

    Article  PubMed  CAS  Google Scholar 

  18. Stanlberg M, Jalovaara P, Laitinen S, et al: Adsorption of bile acids by sucralfate, antacids and cholestyramine. Clin Ther 9:615–621, 1987. Bile acid binding by sucralfate, antacids, or cholestyramine using natural bile acids obtained from gastric or duodenal aspirates.

    Google Scholar 

  19. Kurtz W, Güldütuna S, Leuschner U: Gallensäurebindung durch Antazida in “quasi-natürlichem” Refluxmilieu. Z Gastroenterol 27:370–373, 1989. Binding of bile acids by antacids and sucralfate using reflux mixtures from nonstimulated gastric juice and hepatic bile.

    PubMed  CAS  Google Scholar 

  20. Kurtz W, Güldütuna S, Leuschner U: Einfluβ von pH und Antazidummenge auf die Gallensaurenbindung in quasinatürlichem Refluxmilieu. Z Gastroenterol 29:237–241, 1991. Degree of bile acid adsorption correlated with the lipophilicity of the bile acids used: the most lipophilic and toxic bile acids were bound most effectively.

    PubMed  CAS  Google Scholar 

  21. Tanghoj H, Stenstam H, Tobiasson B: Effects of sucralfate and cholestyramine on bile acid absorption. Gastroenterology 88:1699, 1985 (Abstract). This study demonstrates that administration of sucralfate did not reduce postprandial serum bile acid concentration, but serum bile acid concentration was reduced by sucralfate after a loading dose with chenodeoxycholic acid. Cholestyramine, however, reduced serum bile acids postprandially.

    Google Scholar 

  22. Danesh BJZ, Duncan A, Russel RI: Is an acid pH medium required for the protective effect of sucralfate against mucosal injury? Am J Med83(suppl 38):11–13, 1987. In this paper evidence is presented that sucralfate reduced in rat gastric mucosa the mucosal damage induced by aspirin alone and aspirin combined with bile acids at pH values of both 1.5 and 6.5 and that the protective effect of sucralfate against mucosal injury was not dependent on an acid medium.

    Google Scholar 

  23. Eastwood GL: Effect of pH on bile salt injury to mouse gastric mucosa. Gastroenterology 68:1457–1465, 1975. This publication demonstrates that the erosive activity of aspirin and bile acids is pH-dependent.

    Google Scholar 

  24. Morris GP, Williamson TE, Abonyi S: The effect of sucralfate and luminal stasis on recovery of the chambered rat gastric mucosa from taurocholate-induced damage. Am J Med 91(suppl 2A):2S–14S, 1991. Sucralfate reduced taurocholate-induced damage of chambered rat gastric mucosa. Pretreatment with indomethacin reduced the acceleration of mucosal recovery induced by sucralfate.

    Article  PubMed  CAS  Google Scholar 

  25. Romano M, Razandi M, Ivey KJ: Effect of sucralfate and its components on taurocholate-induced damage to rat gastric mucosal cells in tissue culture. Dig Dis Sci 35:467–476, 1990. It is concluded that sucralfate, but not its components, protected rat gastric mucosal cells against taurocholateinduced damage. Sucralfate stimulated prostaglandin production by cultured cells, but the protective effect of sucralfate did not depend on its stimulatory effect on endogenous prostaglandin synthesis.

    Article  PubMed  CAS  Google Scholar 

  26. Ligumsky M, Karmell F, Rachmilewitz D: Sucralfate protection against gastrointestinal damage: Possible role of prostanoids. Isr J Med Sci 22:801–806, 1986.Sucralfate provided protection against taurocholate-induced gastric mucosal damage. Speculation: stimulation of endogenous gastric mucosal prostanoid formation may, at least in part, explain the protective properties of sucralfate.

    PubMed  CAS  Google Scholar 

  27. Harrington SJ, Schlegel JF, Code CF: The protective effect of sucralfate on the gastric mucosa of rats. J Clin Gastroenterol 3(suppl 2):129–134, 1981. Sucralfate decreased H+ disappearance from rat stomach induced by taurocholate and significantly reduced the index of mucosal damage.

    PubMed  CAS  Google Scholar 

  28. Buch KL, Weinstein WM, Hill TA, et al: Sucralfate therapy in patients with symptoms of alkaline reflux gastritis. A randomized, double-blind study. Am J Med 79(suppl 2C):49–54, 1985. Clinical trial comparing the therapeutic effect of sucralfate versus placebo in patients with alkaline reflux gastritis. Symptom score and endoscopic findings were not improved on sucralfate treatment, but the inflammatory cell score of the sucralfate-treated group was improved.

    Article  PubMed  CAS  Google Scholar 

  29. Meshkinpour H, Elashoff JD, Stewart H, et al: Effect of cholestyramine on the symptoms of reflux gastritis. A randomized double-blind crossover study. Gastroenterology 73:441–443, 1977. Clinical trial showing that treatment of alkaline reflux gastritis with cholestyramine was not beneficial.

    PubMed  CAS  Google Scholar 

  30. Nicolai JJ, Speelman P, Tytgat GNJ, et al: Comparison of the combination of cholestyramine/alginate with placebo in the treatment of postgastrectomy biliary reflux gastritis. Eur J Pharmacol 21:189–194, 1981. This study did not show significant beneficial effects of cholestyramine in biliary reflux gastritis.

    Article  CAS  Google Scholar 

  31. Petit D, Bonncfis M-T, Infante R: Fecal bile acid excretion and liver cholesterol synthesis after sucralfate and cholestyramine administration in the rat. Pharmacol Res Commun 187:317–226, 1986. Cholestyramine induced greater fecal loss of bile acids than sucralfate.

    Google Scholar 

  32. Hunter JR, McCullagh L, Hoeg JM: Sucralfate ameliorates perirectal pain due to bile acid malabsorption. Lancet 1:435, 1986. Anecdotal report on the beneficial effect of sucralfate in treatment of cholerrheic enteropathy.

    Article  PubMed  CAS  Google Scholar 

  33. Maas LC, Kikoler DJ: Sucralfate therapy for choleretic diarrhea. South Med J 76:98, 1983. Anecdotal report on the beneficial effect of sucralfate in treatment of cholerrheic enteropathy.

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Division of Gastroenterology, Department oflnternal Medicine, Frankfurt University Hospital Medical Center, D-60590, Frankfurt am Main, Germany

    W. F. Caspary

Authors
  1. W. F. Caspary
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. Dean’s Office, University of Kansas School of Medicine, Kansas City, 66161-7300

    Daniel Hollander M.D.

  2. Department of Gastroenterology-Hepatology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands

    Guido N. J. Tytgat M.D.

Rights and permissions

Reprints and permissions

Copyright information

© 1995 Plenum Press

About this chapter

Cite this chapter

Caspary, W.F. (1995). Binding of Bile Acids by Sucralfate. In: Hollander, D., Tytgat, G.N.J. (eds) Sucralfate. Springer, Boston, MA. https://doi.org/10.1007/978-0-585-32154-7_6

Download citation

  • DOI: https://doi.org/10.1007/978-0-585-32154-7_6

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-0-306-44740-2

  • Online ISBN: 978-0-585-32154-7

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation