Sucralfate is a unique anti-ulcer drug. It is a basic aluminum salt of sucrose octasulfate. The labeled use of sucralfate is as below:
1. Treatment of duodenal ulcer: Sucralfate is FDA approved for the treatment of duodenal ulcers up to 8 weeks (short term). Duodenal ulcers are treated with 1g four times daily for eight weeks, followed by 1 g twice daily for maintenance therapy. The efficacy of sucralfate in the treatment of duodenal ulcers is shown to be comparable to that of cimetidine and intensive antacid therapy.[1] Sucralfate forms a protective coat and protects the gastric mucosa from pepsin, pectic acid, and bile salts. It binds to positively charged proteins in exudates, forming a thick viscous substance locally.
Sucralfate has also been used to treat various other conditions that are non-FDA approved as outlined below
The principal action of sucralfate is unknown. The following actions of sucralfate have been the object of study in vitro, but the in vivo actions remain unknown[2]:
1. Antipeptic effects - It prevents hydrolysis by preventing the formation of the enzyme-substrate complex. It adsorbs to pepsin and decreases its concentration
2. Site-protective effects - By forming a polyanion gel, it acts as a physical barrier between luminal contents and mucosa
3. Effects on mucus- Increases mucous hydrophobicity, viscosity, sulfation, and the aluminum and carbohydrate content, which leads to improved mucosal protection from acid. It also increases the production of mucus by increasing prostaglandin production. Sucralfate prevents the breakdown of mucus by pepsin A, reducing ulcerogenesis.
4. Effect on bicarbonate output - It increases prostaglandin dependent and independent production of bicarbonate by stomach and duodenum.
5. Effects on tissue growth, regeneration, and repair- It binds epidermal growth factor and tissue growth factor to tissues and facilitates repair.
Sucralfate administration can be via oral, rectal, and topical routes:
1. Oral forms:
a. Tablet - Sucralfate is a basic aluminum salt of sucrose octasulfate. When given orally, it disintegrates in the stomach in the presence of acid and binds to normal and damaged mucosa forming a protective layer. It releases aluminum and binds to positively charged compounds like proteins, peptides, glycoproteins, and glycolipoproteins, forming an adhesive layer and thereby protecting the mucosa. The onset of action is within 1 to 2 hours, and 1 g of sucralfate can neutralize 14 to 16 mEq of acid. The tablets are available as 1 g tablets
b. Suspension: Suspension is available as 1 g/10 mL or 500 mg/5mL.
2. Rectal: Sucralfate tablets have been mixed with water to form a sucralfate paste enema: 2 tablets (that is 2g of sucralfate) mixed with 4.5 ml of water and is an option in the treatment of hemorrhagic radiation proctitis. Sucralfate enema is also useful in solitary rectal ulcer syndrome and diversion colitis
3. Topical: Sucralfate is used topically in the treatment of skin conditions and also for mucosal ulcers.
Sucralfate acts locally with negligible absorption making it relatively safe. The most common side effect is constipation seen in 1-10% of patients. Hyperglycemia is also reported in diabetic patients using sucralfate. Some of the other negligible side effects are nausea, vomiting, flatulence, headache, dry mouth, pruritis, skin rash, gastric bezoar formation, aluminum intoxication, hypophosphatemia. Inadvertent IV use of sucralfate has caused fatal complications such as pulmonary emboli and cerebral edema.
Long term users of sucralfate are shown to retain aluminum that is negligible, except when a patient has renal insufficiency. Uremia causes increased absorption of aluminum from the gut, and the quantity of aluminum absorbed is similar to that of aluminum hydroxide. Sucralfate should be used with caution in patients with end-stage renal disease or avoided altogether to prevent aluminum intoxication.[2][8]
Sucralfate has several drug interactions and can decrease the serum concentrations of digoxin, levothyroxine, furosemide, quinolones, oral phosphate supplements, warfarin, antiretrovirals like raltegravir, bisphosphonates amongst others. Sucralfate administration should have at least a 2-hour gap from the administration of these medications. Multivitamins can increase the serum concentration of sucralfate and aluminum. A few medications like antacids administered within 15 minutes of sucralfate can reduce its efficacy by decreasing the binding ability of sucralfate to gastric ulcers.
Documented hypersensitivity to sucralfate is an absolute contraindication as it can cause an anaphylactic reaction. Some of the relative contraindications include end-stage renal disease, uncontrolled diabetes mellitus with hyperglycemia, impaired swallowing/gag reflex. Sucralfate was an FDA category B medication under the prior pregnancy classification system, and its safety in pregnancy, breastfeeding, infants, is not established.
No therapeutic monitoring has been recommended for this medication as it undergoes minimal absorption from the enteral system.
Risks associated with sucralfate overdosing is minimal as sucralfate has minimal absorption from the gastrointestinal system; many patients that overdosed on sucralfate remained asymptomatic. Due to the small amount of aluminum that is absorbed with oral intake of sucralfate, it can cause aluminum accumulation and toxicity in patients with chronic kidney disease or those receiving dialysis.
Patient satisfaction and relief of symptoms are very valuable to caregivers in the age of medicine. Managing the side effects of chemotherapy and radiation has become a challenge and encountered more often by physicians with new treatment regimens and prolonged survival of oncology patients. The incidence of peptic ulcer disease is also on the rise, with population migration from regions endemic to Helicobacter pylori, lifestyle changes, and overuse of pain medications like NSAIDs. Understanding medications like sucralfate seen in everyday practice by the providers, nurses, and pharmacists can provide the best patient outcomes.
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[2] | McCarthy DM, Sucralfate. The New England journal of medicine. 1991 Oct 3; [PubMed PMID: 1886624] |
[3] | Masuelli L,Tumino G,Turriziani M,Modesti A,Bei R, Topical use of sucralfate in epithelial wound healing: clinical evidences and molecular mechanisms of action. Recent patents on inflammation [PubMed PMID: 19832693] |
[4] | McElvanna K,Wilson A,Irwin T, Sucralfate paste enema: a new method of topical treatment for haemorrhagic radiation proctitis. Colorectal disease : the official journal of the Association of Coloproctology of Great Britain and Ireland. 2014 Apr; [PubMed PMID: 24299100] |
[5] | Kochhar R,Patel F,Dhar A,Sharma SC,Ayyagari S,Aggarwal R,Goenka MK,Gupta BD,Mehta SK, Radiation-induced proctosigmoiditis. Prospective, randomized, double-blind controlled trial of oral sulfasalazine plus rectal steroids versus rectal sucralfate. Digestive diseases and sciences. 1991 Jan; [PubMed PMID: 1670631] |
[6] | Fernandez OOA,Pereira JA,Campos FG,Araya CM,Marinho GE,Novo RS,Oliveira TS,Franceschi YT,Martinez CAR, EVALUATION OF ENEMAS CONTAINING SUCRALFATE IN TISSUE CONTENT OF MUC-2 PROTEIN IN EXPERIMENTAL MODEL OF DIVERSION COLITIS. Arquivos brasileiros de cirurgia digestiva : ABCD = Brazilian archives of digestive surgery. 2017 Apr-Jun; [PubMed PMID: 29257850] |
[7] | Driks MR,Craven DE,Celli BR,Manning M,Burke RA,Garvin GM,Kunches LM,Farber HW,Wedel SA,McCabe WR, Nosocomial pneumonia in intubated patients given sucralfate as compared with antacids or histamine type 2 blockers. The role of gastric colonization. The New England journal of medicine. 1987 Nov 26; [PubMed PMID: 2891032] |
[8] | Burgess E, Aluminum toxicity from oral sucralfate therapy. Nephron. 1991; [PubMed PMID: 1758558] |