Sucralfate

(BAN, USAN, rINN)
Sucralfate Chemical formula
Synonyms: Sucralfato; Sucralfatum; Sukralfaatti; Sükralfat; Sukralfat. Sucrose hydrogen sulphate basic aluminium salt; Sucrose octakis(hydrogen sulphate) aluminium complex; copyranoside octakis (hydrogen sulphate) aluminium complex.
Cyrillic synonym: Сукральфат.

💊 Chemical information

Chemical formula: C12H m Al16O n S8.
CAS — 54182-58-0.
ATC — A02BX02.
ATC Vet — QA02BX02.

Pharmacopoeias.

In Chin., Jpn, and US.

USP 31

(Sucralfate). The hydrous basic aluminium salt of sucrose octasulfate. Store in airtight containers.

💊 Adverse Effects and Precautions

Constipation is the most frequently reported adverse effect of sucralfate although diarrhoea, nausea, vomiting, flatulence, or gastric discomfort may also occur. Other adverse effects include dry mouth, dizziness, drowsiness, headache, vertigo, back pain, and skin rashes. Hypersensitivity reactions such as pruritus, oedema, urticaria, respiratory difficulty, rhinitis, laryngospasm, and facial swelling have been reported. Great caution is needed in patients with renal impairment (below) as absorption and accumulation of aluminium may cause adverse effects.

Bezoar formation.

As of March 1999, the UK CSM was aware of 7 reports worldwide of bezoar formation associated with sucralfate use in intensive care patients.1 It advised caution in the use of sucralfate in seriously ill patients because of the risks of bezoar formation and intestinal obstruction.1 Patients with delayed gastric emptying or receiving concomitant enteral feeds may be at increased risk. A report by the French Pharmacovigilance System at about the same time made similar recommendations but also contra-indicated the use of sucralfate in premature and immature neonates.2
1. Committee on Safety of Medicines/Medicines Control Agency. Bezoar formation with sulcralfate [sic] (Antepsin). Current Problems 1999; 25: 6. Also available at: http://www.mhra.gov.uk/home/ idcplg?IdcService=GET_FILE&dDocName=CON2023235& RevisionSelectionMethod=LatestReleased (accessed 07/11/06
2. Guy C, Ollagnier M. Sucralfate et bézoard: bilan de l’enquête officielle de pharmacovigilance et revue de la littérature. Therapie 1999; 54: 55–8.

Renal impairment.

Sucralfate under acid conditions can release aluminium ions that may be absorbed systemically. Significant increases in the urinary excretion of aluminium have been seen in healthy subjects given sucralfate 4 g daily,1,2 reflecting gastrointestinal absorption of aluminium; aluminium concentrations in serum and urine were significantly higher in patients with chronic renal impairment than in subjects with normal renal function,3 and similar serum increases have been seen in children with acute renal failure.4 Aluminium toxicity in patients with normal renal function receiving sucralfate would not be expected, but seizures, muscle weakness, bone pain,1 and severe aluminium encephalopathy5 have been reported in patients with end-stage renal disease requiring dialysis. Sucralfate should be used with caution in patients with renal impairment, especially if other aluminium-containing agents are also taken, and such patients should be monitored for signs of aluminium toxicity.4,6
1. Robertson JA, et al. Sucralfate, intestinal aluminium absorption, and aluminium toxicity in a patient on dialysis. Ann Intern Med 1989; 111: 179–81
2. Allain P, et al. Plasma and urine aluminium concentrations in healthy subjects after administration of sucralfate. Br J Clin Pharmacol 1990; 29: 391–5
3. Burgess E, et al. Aluminum absorption and excretion following sucralfate therapy in chronic renal insufficiency. Am J Med 1992; 92: 471–5
4. Thorburn K, et al. Aluminum accumulation in critically ill children on sucralfate therapy. Pediatr Crit Care Med 2001; 2: 247–9
5. Withers DJ, et al. Encephalopathy in patient taking aluminiumcontaining agents, including sucralfate. Lancet 1989; ii: 674
6. Hemstreet BA. Use of sucralfate in renal failure. Ann Pharmacother 2001; 35: 360–4.

💊 Interactions

Sucralfate may interfere with the absorption of other drugs and it has been suggested that there should be an interval of 2 hours between giving sucralfate and other non-antacid medication. Some of the drugs reported to be affected by sucralfate include cimetidine, ranitidine, digoxin, fluoroquinolone antibacterials, ketoconazole, levothyroxine, phenytoin, tetracycline, quinidine, theophylline, and possibly warfarin. The recommended interval between sucralfate and antacids is 30 minutes. An interval of 1 hour should elapse between giving sucralfate and enteral feeding.

💊 Pharmacokinetics

Sucralfate is only slightly absorbed from the gastrointestinal tract after oral doses. However, there can be some release of aluminium ions and of sucrose sulfate; small quantities of sucrose sulfate may then be absorbed and excreted, primarily in the urine; some absorption of aluminium may also occur (see Renal Impairment, above).

💊 Uses and Administration

Sucralfate is a cytoprotective drug that, under acid gastrointestinal conditions, forms an adherent complex with proteins which coats the gastric mucosa and is reported to have a special affinity for ulcer sites. It also inhibits the action of pepsin and adsorbs bile salts. Sucralfate has been used in the treatment of peptic ulcer disease and chronic gastritis. It is given orally and should be taken on an empty stomach before meals and at bedtime. The usual dose is 1 g four times daily or 2 g twice daily for 4 to 8 weeks; if necessary the dose may be increased to a maximum of 8 g daily. If longer-term therapy is required sucralfate may be given for up to 12 weeks. Where appropriate a maintenance dose of 1 g twice daily may be given to prevent the recurrence of duodenal ulcers. For prophylaxis of gastrointestinal haemorrhage from stress ulceration the usual dose of sucralfate is 1 g six times daily; a dose of 8 g daily should not be exceeded. For children’s doses see below.

Administration in children.

Although sucralfate is not licensed in the UK for use in children under 15 years, the BNFC recommends the following oral doses for the treatment of peptic
Published April 08, 2019.