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Sucralfate

Drug Approvals

(British Approved Name, US Adopted Name, rINN)

SucralfateSynonyms: Sucralfato; Sucralfatum; Sukralfaatti; Sukralfat
BAN: Sucralfate
USAN: Sucralfate
INN: Sucralfate [rINN (en)]
INN: Sucralfato [rINN (es)]
INN: Sucralfate [rINN (fr)]
INN: Sucralfatum [rINN (la)]
INN: Сукральфат [rINN (ru)]
Chemical name: Sucrose hydrogen sulphate basic aluminium salt; Sucrose octakis(hydrogen sulphate) aluminium complex; β-d-Fructofuranosyl-αd-glucopyranoside octakis (hydrogen sulphate) aluminium complex
Molecular formula: C12HmAl16OnS8
CAS: 54182-58-0
ATC code: A02BX02
Read code: y01Q0

Pharmacopoeias. In China, Japan, and US.

The United States Pharmacopeia 31, 2008 (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. It advised caution in the use of sucralfate in seriously ill patients because of the risks of bezoar formation and intestinal obstruction. 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.

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 4g daily reflecting gastrointestinal absorption of aluminium aluminium concentrations in serum and urine were significantly higher in patients with chronic renal impairment than in subj ects with normal renal function, and similar serum increases have been seen in children with acute renal failure. Aluminium toxicity in patients with normal renal function receiving sucralfate would not be expected, but seizures, muscle weakness, bone pain, and severe aluminium encephalopathy 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.

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 ulcer disease, or the prophylaxis of stress ulceration in children in intensive care (but see also under Bezoar Formation, above):

• 1 month to 2 years: 250 mg four to six times daily

• 2 to 12 years: 500 mg four to six times daily

• 12 to 18 years: 1 g four to six times daily

The oral suspension blocks fine-bore feeding tubes and tablets should be crushed and dispersed in water instead.

Gastrointestinal bleeding. Sucralfate is an effective drug for the prophylaxis and management of stress-induced gastrointestinal bleeding in severely ill patients but whether it should be chosen over an H2-antagonist has been subject to debate. One study suggested it might reduce the risk of late-onset pneumonia compared with ranitidine. Another study found ranitidine to be more effective than sucralfate in reducing the risk of gastrointestinal bleeding while there was a trend towards a lower rate of pneumonia among patients receiving sucralfate, the difference was not significant. However, meta-analyses found an increased risk of pneumonia with ranitidine compared with sucralfate, but no difference in the rate of pneumonia with sucralfate and placebo insufficient data were available to conduct a meta-analysis of sucralfate’s efficacy in terms of rates of bleeding, and a re-assessment of recommendations for the prophylaxis of stress ulcers was called for. Later guidelines concluded that the use of sucralfate did not influence the incidence of ventilator-associated pneumonia compared with placebo. For further discussion of stress ulceration and bleeding, including the use of sucralfate, see under Peptic Ulcer Disease. There is also some evidence from a study that sucralfate reduces gastrointestinal bleeding associated with NSAID use, although it does not prevent drug-induced gastric erosion.

In a study to assess whether oral prophylactic sucralfate could ameliorate the symptoms of acute radiation proctitis, sucralfate was found to increase the incidence of rectal bleeding compared with placebo the cause of this increased bleeding was unclear.

Gastro-oesophageal reflux disease. Although sucralfate has been tried for gastro-oesophageal reflux disease the results of studies have been inconsistent. However, if lifestyle or dietary measures prove insufficient for the management of heartburn in pregnancy, sucralfate may be considered for first-line therapy.

Mouth ulceration. Sucralfate has been investigated as a mouth rinse in the treatment and prophylaxis of stomatitis induced by cancer chemotherapy although evidence of benefit for any drug is ambiguous (see Mucositis). One study in 40 patients found a significant reduction in symptoms among 23 eval-uable patients given sucralfate prophylactically. Seven patients withdrew due to aggravation of chemotherapy-induced nausea. It was suggested that to overcome this problem, the suspension should have a neutral taste, should not be swallowed after rinsing, and that rinsing should not be started until nausea had stopped. However, another study involving 80 patients treated with fluorouracil for colorectal cancer found no significant difference in self-reported mucositis symptoms between patients given sucralfate suspension and those given placebo. Sucralfate has also been reported to be of benefit in patients with recurrent aphthous stomatitis (mouth ulceration). A study involving 21 such patients over 2 years found that topical application of sucralfate suspension 4 times daily was superior to treatment with an antacid (aluminium hydroxide with magnesium hydroxide) or placebo.

In patients with Behcefs syndrome, topical sucralfate suspension significantly decreased the frequency, healing time, and pain of oral ulceration, as well as the healing time and pain of genital ulceration, when compared with placebo.

Skin ulceration. Sucralfate has reportedly been applied topically with some success to treat bleeding skin ulcers associated with malignancy, and to promote the healing of venous stasis ulcers. It has been suggested that sucralfate promotes angiogenesis by binding to, and preventing degradation of, basic fibroblast growth factor (bFGF). Topical sucralfate 7% cream was also reported to decrease pain and speed healing of the wound after open surgical removal of haemorrhoids.

Preparations

The United States Pharmacopeia 31, 2008: Sucralfate Tablet.

Proprietary Preparations

 

Argentina: Antepsin Netunal Sucralmax

Australia:: Carafate Ulcyte

Austria: Citogel Sucralan Sucralbene Sucralstad Sucramed Ulceral Ulcogant

Belgium: Ulcogant

Brazil: Sucrafilm

Canada: Novo-Sucralate Sulcrate

Chile: Gastrocol Mulcatel Sulcran

Czech Republic: Sucralan Ulcogant Venter

Denmark: Antepsin Hexagastron

Finland: Alsucral Antepsin Fn Keal Ulcar

Germany: Sucrabest Sucraphil Ulcogant

Greece: Peptonorm Sucrate

Hong Kong: Sucari Ulsanic

Hungary: Alusulin Ulcogant Venter

India: Alfate Sucrase Ulcekon

Indonesia: Inpepsa Musin Neciblok Ulcumaag Ulsafate Ulsicral Ulsidex

Ireland: Antepsin

Israel: Ulsanic

Italy: Antepsin Citogel Crafilm Escudo Gastrogel Ipagastril-b Sucrager Sucral Sucralfin Sucramal Sucrate Sucroril Sugar Sugast Suril Ulcrast Zenodian

Japan: Ulcerlmin

Malaysia: Alsucral Ulcertec

Mexico: Apo-Lato Unival

The Netherlands: Ulcogant

Norway: Antepsin

New Zealand: Carafate

Philippines: Iselpin

Poland: Ulgastran Venter

Portugal: Calfate Cinebil Sucralum Ulcermate Ulcermin Ulcimer

Russia: Venter

South Africa: Ulcetab Ulsanic

Singapore: Alsucral Ulcertec

Spain: Gastral Urbal

Sweden: Andapsin

Switzerland: Ulcogant

Thailand: Sucrafen Sucral Sucrate Ulcefate Ulcrafate Ulsanic

Turkey: Antepsin

United Arab Emirates: Sucralose

UK: Antepsin

USA: Carafate

Venezuela: Dip Exinol Ulciram Ulcon

 

Multi-ingredient

 

Chile: Cicalfate

France: Cicalfate

Greece: Profenil

Used as an adjunct in: Italy: Ketodol

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