This paper is only available as a PDF. To read, Please Download here.
Abstract
Over the past 5–10 years, a number of studies have shown that topical sucralfate enhances
a number of gastric and duodenal mechanisms, e.g., the “mucus-bicarbonate barrier,”
mucosal hydrophobicity, mucosal blood flow, cell viability, and local production of
prostaglandins, as well as endogenous mediators of tissue injury and repair.
It seems likely that the complex actions of sucralfate are in part related to direct
interaction between the drug or its components (aluminum, sucrose, and sulfate) and
gastric mucosal tissues, and in part related to effects of the drug on the various
mucosal mediators of tissue injury and repair.
Local actions may play a role in accelerating healing of ulcer-damaged mucosa, but
this does not explain the protective actions of sucralfate on normal mucosa. Thus
sucralfate appears to enhance the protective function of the “mucus-bicarbonate” barrier
by actions on both components. This may depend in part on an interaction with the
unstirred layer overlying gastric epithelium. Sucralfate has also been shown to increase
the hydrophobicity of mucus gel.
There is little doubt that sucralfate increases local production and release of protective
prostaglandins (PGs), but the precise role played by these agents in mediating mucosal
protection and in chronic ulcer healing remains uncertain. Currently, the mechanism
of action of sucralfate on vascular integrity remains unknown and the role of PGs
in this protective function is unclear. There is little evidence that epidermal growth
factor plays any role in mediating mucosal protection by sucralfate, but it may be
important in its ulcer-healing action.
Sucralfate has been shown to be truly “cytoprotective” in that it protects isolated
epithelial cells from damage by noxious agents. In animals treated with sucralfate,
the surface epithelial cells were disrupted, but necrotic lesions in the deep proliferative
zone were virtually absent.
It seems likely that investigations of the actions of sucralfate and its components
will move ever closer to defining the target cells, the intracellular events, and
the mediators that bring about its protective and ulcer-healing activity.
To read this article in full you will need to make a payment
Purchase one-time access:
Academic & Personal: 24 hour online accessCorporate R&D Professionals: 24 hour online accessOne-time access price info
- For academic or personal research use, select 'Academic and Personal'
- For corporate R&D use, select 'Corporate R&D Professionals'
Subscribe:
Subscribe to The American Journal of MedicineAlready a print subscriber? Claim online access
Already an online subscriber? Sign in
Register: Create an account
Institutional Access: Sign in to ScienceDirect
References
- Specific binding of 14C Sucralfate to acetic acid-induced gastric and duodenal ulcers in the rat.in: Caspary WF Duodenal ulcer, gastric ulcer: sucralfate, a new therapeutic concept. Urban and Schwarzenberg, Urban1981: 19-21
- Selective binding of sucralfate to gastric ulcer in man.Dig Dis Sci. 1981; 26: 297-300
- Mechanism of action studies of sucralfate.in: Caspary WF Duodenal ulcer, Gastric ulcer: sucralfate, a new therapeutic concept. Urban and Schwarzenberg, Baltimore1981: 3-12
- Inhibition of peptic aggression by sucralfate.in: The view from the ulcer crater. Scand J Gastroenterol. 18. 1983: 7-11 (Suppl 83)
- Am J Med. 1985; 79 (Suppl. 2C): 15-18
- In vitro adsorbtion of bile salts and aspirin to sucralfate.Dig Dis Sci. 1984; 29: 402-406
- The protective effect of sucralfate against alcohol-induced gastric mucosal injury in the rat.in: Macroscopic, histologic, ultrastructural and functional time sequence analysis. Gastroenterology. 88. 1985: 366-374
- Pathways of Gastrointestinal protection and repair: mechanisms of action of sucralfate.Am J Med. 1989; 86: 23-31
- Effect of sucralfate and its components on taurocholate-induced damage to rat gastric mucosal cells in tissue culture.Dig Dis Sci. 1990; 35: 467-476
- Sucralfate protection of gastric mucosa against alcohol induced necrosis: a prostaglandin mediated process?.Gastroenterology. 1983; 84 (Abstr): 1331
- Prostaglandin protection of the gastric mucosa against alcohol injury, a dynamic time related process.in: The role of the mucosal proliferative zone. Gastroenterology. 88. 1985: 334-352
- Prostaglandin protection of the human gastric mucosa against alcohol-induced injury.Scand J Gastroenterol. 1986; 21: 165-169
- Gastroprotection by sucraltate against acetylsalicyclic acid in humans: role of endogenous prostaglandins.Scand J Gastroenterol. 1987; 22: 19-22
- Protective effect of sucralfate against aspirin-induced damage to the human gastric mucosa.Am J Med. 1987; 83: 83-85
- Sucralfate protection of human gastric mucosa against acute ethanol injury.Gastroenterology. 1989; 96: 292-298
- The mechanism of protective, therapeutic and prophylactic actions of sucralfate.Scand J Gastroenterol. 1987; 22: 7-13
- Protection of rat gastric mucosa by sucralfate.in: Effects of luminal stasis and inhibition of prostaglandin synthesis. Am J Med. 86. 1986: 11-16 (Suppl 6A)
- Sucralfate prevents the development of haemorrhagic erosions when applied after exposure of the rat gastric mucosa to damaging concentrations of bile salt.Am J Med. 1991; 91: 2S-14S
- Effect of intragastric pH on mucosal protective action of sucralfate.Gut. 1988; 29: 1379-1385
- Role of acid milieu in the gastroprotective and ulcer-healing activity of sucralfate.Am J Med. 1991; 91: 20S-29S
- Stimulation of amphibian gastroduodenal bicarbonate secretion by sucralfate and aluminum: role of local prostaglandin metabolism.Gut. 1988; 29: 903-908
- Effect of sucralfate on gastroduodenal bicarbonate secretion and prostaglandin E2 metabolism.Am J Med. 1987; 83: 14-18
- Effects of protective drugs on gastric alkaline secretion in man.Scand J Gastroenterol. 1987; 22: 1059-1063
- Effect of bismith subcitrate and sucralfate on rat duodenal and human gastric bicarbonate secretion in vivo.Gut. 1990; 31: 26-31
- In vivo inhibition of petic degradation of porcine gastric mucus glycoprotein by sucralfate.Scand J Gastroenterol. 1985; 20: 858-860
- Effect of sucralfate on the viscosity of gastric mucus and the permeability to hydrogen ion.Digestion. 1986; 33: 146-151
- Sucralfate interactions with gastric mucus.Am J Med. 1989; 86: 5-9
- (in: The effects of Campylobacter pylori infection and sucralfate. Scand J Gastroenterol. 24. 1989: 781-786
) ions exchange property of postmortem human gastric mucus.
- Enhancement of the protective qualities of gastric mucus by sucralfate: role of phosphoinositides.Am J Med. 1991; 91: 30S-36S
- Gastric mucosal barrier: hydrophobic lining to the lumen of the stomach.Am J Physiol. 1983; 7: G561-G568
- Luminal surface hydrophobicity of canine gastric mucosa is dependent on a surface mucus gel.Gastroenterology. 1990; 98: 361-370
- Nature of the enhancement of the protective qualities of gastric mucus by sucralfate.Digestion. 1989; 44: 222-231
- A physical basis for the gastric mucosal barrier.Am J Med. 1991; 91: 43S-51S
- Prostaglandin protection of the gastric mucosa against alcohol injury-a dynamic time-related process.in: Role of mucosal proliferative zone. Gastroenterology. 88. 1985: 334-352
- Effect of sucralfate on the normal human gastric mucosa.in: Endoscopic, histologic and ultra structural as sessment. Scand J Gastroenterol. 22. 1987: 111-123 (Suppl 127)
- Trophic effect of long term sucralfate treatment on the gastric mucosa.in: A key to prophylactic efficiency. Gastroenterology. 88. 1985: 1610A
- The protective effect of sucralfate on the gastric mucosa of rats.J Clin Gastroenterol. 1981; 3: 129-134
- Prevention of ethanol-induced vascular injury and gastric mucosal lesions by sucralfate and its compounds: possible role of endogenous sulfhydryls.in: Proc Soc Exp Biol Med. 185. 1987: 493-497
- Effect of sucralfate on gastric mucosal blood flow in rats.Gut. 1989; 30: 1544-1551
- Gastroenterology by colloidal bismith subcitrate (De-Nol) and sucralfate.in: Role of endogenous prostaglandins. Gut. 28. 1987: 201-205
- Effect of 16,16 dimethyl prostaglandin E2 on the surface hydrophobicity of aspirin treated canine gastric mucosa.Gastroenterology. 1985; 88: 308-314
- Effects of sucralfate on gastric prostaglandin and leukotriene synthesis: relationship to protective actions.Can J Physiol-Pharmacol. 1988; 66: 666-670
- Effect of sucralfate or mild irritants on experimental gastritis and prostaglandin production.Am J Med. 1987; 83: 24-30
- Sucrose octasulfate stimulates gastric somatostatin release.Am J Med. 1991; 91: 52S-57S
- Does epidermal growth factory play a role in the action of sucralfate?.Scand J Gastroenterol. 1987; : 45-49
- Epidermal growth factor in the gastroprotective and ulcer-healing actions of sucralfate in rats.Am J Med. 1989; 86: 32-37
- “mucus-bicarbonate” barrier—shield or sieve.Gut. 1987; 28: 1553-1556
- Effects of sucralfate cimetidine, and AG1749, a new proton pump inhibitor, on the delayed healing by hydrocortisone sodium phosphate of chronic gastric ulcers in the rat.Am J Med. 1990; (in press)
- Sucralfate in the prevention of porcine experimental peptic ulceration.Am J Med. 1989; 86: 21-22
- Administration of sucralfate prolongs survival of animals with experimental peptic ulceration.Am J Med. 1991; 91: 37S-42S
- Effect of sucralfate and sucrose octasulfate (SOS) on angiogenesis and granulation tissue implications for ulcer-healing.Am J Med. 1991; 91: 158S-160S
- Mucosal protection by sucralfate and its components in acid-exposed rabbit oesophagus.Gastroenterology. 1987; 93: 352-361
- Release of cytoprotective PGE2 from cultured macrophages induced by antacids and sucralfate.Agents Actions. 1986; 18: 375-380
Article Info
Identification
Copyright
© 1991 Published by Elsevier Inc.