Sucralfate

Sucralfate is a Gastro-duodenal protective belonging to Antiulcer agent.

Sucralfate is a gastro-duodenal protective agent used in the treatment of gastric and duodenal ulcers and to prevent duodenal ulcer recurrence.

Sucralfate minimally absorbed from the gastrointestinal tract (as sucrose sulfate). Small amounts of may be absorbed after sucralfate administration. Sucralfate locally acts to ulcer sites; unbound in the gastrointestinal tract to Al and sucrose octasulfate. Sucralfate mainly excreted via urine (small amounts of sulfated disaccharide).

Sucralfate shows side effects like Constipation.

Sucralfate is available in the form of oral suspension and oral tablet.

Sucralfate is available in India, US, Canada, Malaysia, Philippines, Singapore, Italy, spain, France, and Australia.

Sucralfate belongs to the Antiulcer agent acts as a Gastro-duodenal protective.

Sucralfate is a basic, Al complex of sucrose Octasulfate. It binds with positively charged protein exudates at the ulcer site, forming a viscous paste-like ulcer-adherent complex. This complex acts as a protective barrier on the gastric lining against pepsin, peptic acid and bile salts. It also inhibits pepsin activity.

The onset of action of Sucralfate can be observed in 1 to 2 hours.

The duration of action of Sucralfate lasts for an average duration of 6 hours.

Sucralfate is available in the form of oral suspension and oral tablet.

Sucralfate suspension and tablet is taken orally, usually three to four times daily.

Sucralfate is an antiulcer agent which is used for the treatment of gastric (painful sores in the stomach lining) and duodenal ulcers (a peptic ulcer that develops in the first part of the small intestine) caused by excessive acid production in your stomach. Sucralfate works by forming a protective layer over the ulcer and prevents the exposure of the ulcer to gastric acid, allowing it to heal.

Sucralfate is a Gastro-duodenal protective belonging to Antiulcer agent.

Sucralfate forms a complex by binding with positively charged proteins in exudates, forming a viscous paste-like, adhesive substance. This selectively forms a protective coating that acts locally to protect the gastric lining against peptic acid, pepsin, and bile salts.

Sucralfate is approved for use in the following clinical indications

Adult indication

• Duodenal ulcer
• Gastroesophageal reflux disease in pregnancy
• Marginal (anastomotic) ulceration after bariatric surgery
• Oral ulcers, simple recurrent stomatitis and ulcers associated with Behçet disease
• Proctitis due to radiation
• Upper GI toxicity following radiation therapy

Paediatric indication

• Peptic ulcer disease, adjunct therapy
• Esophagitis

Adult Dose

• Duodenal ulcer

Suspension, tablet: Initial: 1 g four times daily for 4 to 8 weeks.

Maintenance therapy: Tablet: 1 g twice daily.

• Gastroesophageal reflux disease in pregnancy

Oral: 1 g three times daily; if symptoms do not improve, additional or alternative therapy should be considered.

• Marginal (anastomotic) ulceration after bariatric surgery

Oral: Suspension: 1 g four times daily in combination with twice-daily proton pump inhibitor; institutional guidelines vary; refer to center-specific protocol.

• Oral ulcers, simple recurrent stomatitis and ulcers associated with Behçet disease

Oral: Suspension: 1 g for 1 to 2 minutes after routine mouth care 4 times daily; alternatively, suspension may be applied directly to the oral ulcer 4 times daily using a cotton-tip applicator.

• Proctitis due to radiation

Rectal: Retention enema: 2 g (tablets or suspension) dissolved in 20 mL water twice daily for at least 4 weeks or until resolution of symptoms; retain each enema for as long as possible or at least 5 minutes.

• Upper GI toxicity following radiation therapy

Oral: Suspension: 1 g four times daily generally for 2 weeks post-procedure as a component of a combination regimen (eg, with antisecretory agent[s], analgesic[s], and/or local anesthetic as needed). Optimal regimen has not been established; refer to published and institutional protocols.

Pediatric Dose

• Peptic ulcer disease, adjunct therapy

Infants, Children, and Adolescents: Oral: 40 to 80 mg/kg/day divided every 6 hours. Maximum dose: 1,000 mg/dose.

• Esophagitis

Infants ≥3 months and Children <6 years: Oral: 500 mg/dose four times daily.

Children ≥6 years: Oral: 1,000 mg/dose four times daily.

Sucralfate is available in various strengths as 1 g/10 mL and 1 g.

Sucralfate is available in the form of oral suspension and oral tablet.

• Dosage Adjustment in Kidney Patient

CrCl ≥30 mL/minute: No dosage adjustment necessary (minimal systemic absorption).

CrCl <30 mL/minute: No dosage adjustment necessary.

Sucralfate is contraindicated in patients with

• Sucralfate is contraindicated for patients with known hypersensitivity reactions to the active substance or to any of the excipients.

• Diabetes: Hyperglycemia has been reported with sucralfate suspension in patients with diabetes; monitor glycemia closely; adjustment of antidiabetic treatment may be necessary.
• Duodenal ulceration: Because sucralfate acts locally at the ulcer, successful therapy with sucralfate should not be expected to alter the posthealing frequency of recurrence or the severity of duodenal ulceration.
• Renal impairment: Use with caution in patients with advanced kidney impairment. Sucralfate is an aluminum complex; small amounts of aluminum are absorbed following oral administration. Excretion of aluminum may be decreased in patients with advanced kidney impairment or on dialysis, increasing the risk of aluminum accumulation and toxicity (eg, aluminum osteodystrophy, osteomalacia, and encephalopathy).

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when sucralfate is administered to a nursing woman.

Pregnancy category B: Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.

Common

• Constipation, diarrhea, flatulence, gastric discomfort, dry mouth, dyspepsia, nausea, vomiting, Hypersensitivity reactions (e.g. dyspnoea, urticaria, anaphylaxis), Back pain, Dizziness, drowsiness, headache, Insomnia, Pruritus, rash.

• Deferiprone: Polyvalent Cation Containing Products may decrease the serum concentration of Deferiprone. Management: Separate administration of deferiprone and oral medications or supplements that contain polyvalent cations by at least 4 hours.
• Digoxin: Sucralfate may decrease the serum concentration of Digoxin. Specifically, sucralfate may decrease the absorption of digoxin. Management: Administer digoxin at least 2 hours before sucralfate. Concomitant administration should be avoided. Monitor for decreased digoxin levels/effects with initiation of sucralfate therapy.
• Dolutegravir: Sucralfate may decrease the serum concentration of Dolutegravir. Management: Administer dolutegravir at least 2 hours before or 6 hours after sucralfate. Administer the dolutegravir/rilpivirine combination product at least 4 hours before or 6 hours after sucralfate.
• Eltrombopag: Polyvalent Cation Containing Products may decrease the serum concentration of Eltrombopag. Management: Administer eltrombopag at least 2 hours before or 4 hours after oral administration of any polyvalent cation containing product.
• Raltegravir: Polyvalent Cation Containing Products may decrease the serum concentration of Raltegravir. Management: Administer raltegravir 2 hours before or 6 hours after administration of the polyvalent cations. Dose separation may not adequately minimize the significance of this interaction.
• Roxadustat: Polyvalent Cation Containing Products may decrease the serum concentration of Roxadustat. Management: Administer roxadustat at least 1 hour after the administration of oral polyvalent cation containing products.
• Sulpiride: Sucralfate may decrease the serum concentration of Sulpiride. Management: Separate administration of sucralfate and sulpiride by at least 2 hours in order to minimize the impact of sucralfate on sulpiride absorption.
• Tetracyclines: Sucralfate may decrease the absorption of Tetracyclines. Management: Administer most tetracycline derivatives at least 2 hours prior to sucralfate in order to minimize the impact of this interaction. Administer oral omadacycline 4 hours prior to sucralfate.
• Trientine: Polyvalent Cation Containing Products may decrease the serum concentration of Trientine. Management: Avoid concomitant use of trientine and polyvalent cations. If oral iron supplements are required, separate the administration by 2 hours. For other oral polyvalent cations, give trientine 1 hour before, or 1 to 2 hours after the polyvalent cation.
• Bictegravir: Polyvalent Cation Containing Products may decrease the serum concentration of Bictegravir. Management: Administer bictegravir under fasting conditions at least 2 hours before or 6 hours after polyvalent cation containing products. Co-administration of bictegravir with or 2 hours after most polyvalent cation products is not recommended.
• Bisphosphonate Derivatives: Polyvalent Cation Containing Products may decrease the serum concentration of Bisphosphonate Derivatives. Management: Avoid administration of oral medications containing polyvalent cations within: 2 hours before or after tiludronate/clodronate/etidronate; 60 minutes after oral ibandronate; or 30 minutes after alendronate/risedronate.

The common side effects of Sucralfate include the following

Common side effects

• Constipation.

Rare side effects

• Hives, rash, itching, difficulty breathing or swallowing, swelling of the face, throat, tongue, or lips.

• Pregnancy

Teratogenic effects. Pregnancy Category B.

Teratogenicity studies have been performed in mice, rats, and rabbits at doses up to 50 times the human dose and have revealed no evidence of harm to the fetus due to sucralfate. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

• Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when sucralfate is administered to a nursing woman.

• Pediatric Use

As per FDA, the Safety and effectiveness in pediatric patients have not been established.

• Geriatric Use

Clinical studies of sucralfate Suspension did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Specially elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

Due to limited experience in humans with over dosage of sucralfate, no specific treatment recommendations can be given. Acute oral studies in animals, however, using doses up to 12 g/kg body weight, could not find a lethal dose. Sucralfate is only minimally absorbed from the gastrointestinal tract. Risks associated with acute overdosage should, therefore, be minimal. In rare reports describing sucralfate overdose, most patients remained asymptomatic. Those few reports where adverse events were described included symptoms of dyspepsia, abdominal pain, nausea, and vomiting.

Pharmacodynamic

Pharmacokinetics

• Absorption

Sucralfate minimally absorbed from the gastrointestinal tract (as sucrose sulfate). Small amounts of may be absorbed after sucralfate administration.

• Distribution

Sucralfate locally acts to ulcer sites; unbound in the gastrointestinal tract to Al and sucrose octa sulfate.

• Metabolism and Excretion

Sucralfate mainly excreted via urine (small amounts of sulfated disaccharide).

• https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019183s019lbl.pdf
• https://www.drugs.com/mtm/sucralfate.html
• https://go.drugbank.com/drugs/DB00364
• https://medlineplus.gov/druginfo/meds/a681049.html
• https://www.practo.com/medicine-info/sucralfate-260-api