Sucralfate

Sucralfate
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1];

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Overview

Sucralfate is an antiulcer agent that is FDA approved for the {{{indicationType}}} of active duodenal ulcer. Common adverse reactions include constipation, hyperglycemia.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Active Duodenal ulcer

• Dosing Information

• The recommended adult oral dosage for duodenal ulcer is 1 g (10 mL/2 teaspoons) four times per day. CARAFATE should be administered on an empty stomach.
• Antacids may be prescribed as needed for relief of pain but should not be taken within one-half hour before or after sucralfate.
• While healing with sucralfate may occur during the first week or two, treatment should be continued for 4 to 8 weeks unless healing has been demonstrated by x-ray or endoscopic examination.
• Elderly: 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.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Sucralfate in adult patients.

Non–Guideline-Supported Use

Burn

• Dosing Information

• Topical sucralfate lowered healing times in burn patients.

Gastric ulcer

• Dosing Information

• Combination therapy with sucralfate 1 gram 3 times daily plus ranitidine 300 milligrams (mg) at bedtime.

Gastritis

• Dosing Information

• Sucralfate was given as 12 grams (60 milliliters) through the nasogastric tube.

Hyperphosphatemia

• Dosing Information

• 1 gram sucralfate for 475 milligrams aluminum hydroxide.

Proctitis

• Dosing Information

• Sucralfate enemas twice daily for 14 to 23 days .

Stress ulcer; Prophylaxis

• Dosing Information

• Nasogastric sucralfate (1 grams every 6 hours).

Ulcer of rectum, Solitary

• Dosing Information

• Sucralfate rectal retention enema therapy for 6 to 8 weeks.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Sucralfate in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Sucralfate in pediatric patients.

Non–Guideline-Supported Use

Epidermolysis bullosa

• Dosing Information

• Suspension prepared with sucralfate powder to oral mucosa (especially blisters) 4 times a day.

Contraindications

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

Warnings

Precautions

• The physician should read the "PRECAUTIONS" section when considering the use of CARAFATE in pregnant or pediatric patients, or patients of childbearing potential.

• Duodenal ulcer is a chronic, recurrent disease. While short-term treatment with sucralfate can result in complete healing of the ulcer, a successful course of treatment with sucralfate should not be expected to alter the post healing frequency or severity of duodenal ulceration.

• Episodes of hyperglycemia have been reported in diabetic patients. Close monitoring of glycemia in diabetic patients treated with sucralfate suspension is recommended. Adjustment of the anti-diabetic treatment dose during the use of sucralfate suspension might be necessary.

• Special Populations: Chronic Renal Failure and Dialysis Patients

• When sucralfate is administered orally, small amounts of aluminum are absorbed from the gastrointestinal tract. Concomitant use of sucralfate with other products that contain aluminum, such as aluminum-containing antacids, may increase the total body burden of aluminum. Patients with normal renal function receiving the recommended doses of sucralfate and aluminum-containing products adequately excrete aluminum in the urine. Patients with chronic renal failure or those receiving dialysis have impaired excretion of absorbed aluminum. In addition, aluminum does not cross dialysis membranes because it is bound to albumin and transferrin plasma proteins. Aluminum accumulation and toxicity (aluminum osteodystrophy, osteomalacia, encephalopathy) have been described in patients with renal impairment. Sucralfate should be used with caution in patients with chronic renal failure.

• Drug Interactions

• Some studies have shown that simultaneous sucralfate administration in healthy volunteers reduced the extent of absorption (bioavailability) of single doses of the following: cimetidine, digoxin, fluoroquinolone antibiotics, ketoconazole, l-thyroxine, phenytoin, quinidine, ranitidine, tetracycline, and theophylline. Subtherapeutic prothrombin times with concomitant warfarin and sucralfate therapy have been reported in spontaneous and published case reports. However, two clinical studies have demonstrated no change in either serum warfarin concentration or prothrombin time with the addition of sucralfate to chronic warfarin therapy.
• The mechanism of these interactions appears to be nonsystemic in nature, presumably resulting from sucralfate binding to the concomitant agent in the gastrointestinal tract. In all cases studied to date (cimetidine, ciprofloxacin, digoxin, norfloxacin, ofloxacin, and ranitidine), dosing the concomitant medication 2 hours before sucralfate eliminated the interaction. Due to CARAFATE's potential to alter the absorption of some drugs, CARAFATE should be administered separately from other drugs when alterations in bioavailability are felt to be critical. In these cases, patients should be monitored appropriately.

Adverse Reactions

Clinical Trials Experience

• Adverse reactions to sucralfate tablets in clinical trials were minor and only rarely led to discontinuation of the drug. In studies involving over 2700 patients treated with sucralfate, adverse effects were reported in 129 (4.7%).

• Constipation was the most frequent complaint (2%). Other adverse effects reported in less than 0.5% of the patients are listed below by body system:

• Gastrointestinal: diarrhea, dry mouth, flatulence, gastric discomfort, indigestion, nausea, vomiting

• Dermatological: pruritus, rash

• Nervous System: dizziness, insomnia, sleepiness, vertigo

• Other: back pain, headache

Postmarketing Experience

• Post-marketing cases of hypersensitivity have been reported with the use of sucralfate suspension, including anaphylactic reactions, dyspnea, lip swelling, edema of the mouth, pharyngeal edema, pruritus, rash, swelling of the face and urticaria.

• Cases of bronchospasm, laryngeal edema and respiratory tract edema have been reported with an unknown oral formulation of sucralfate.

• Cases of hyperglycemia have been reported with sucralfate

• Bezoars have been reported in patients treated with sucralfate. The majority of patients had underlying medical conditions that may predispose to bezoar formation (such as delayed gastric emptying) or were receiving concomitant enteral tube feedings.

• Inadvertent injection of insoluble sucralfate and its insoluble excipients has led to fatal complications, including pulmonary and cerebral emboli. Sucralfate is not intended for intravenous administration.

Drug Interactions

• Some studies have shown that simultaneous sucralfate administration in healthy volunteers reduced the extent of absorption (bioavailability) of single doses of the following: cimetidine, digoxin, fluoroquinolone antibiotics, ketoconazole, l-thyroxine, phenytoin, quinidine, ranitidine, tetracycline, and theophylline. Subtherapeutic prothrombin times with concomitant warfarin and sucralfate therapy have been reported in spontaneous and published case reports. However, two clinical studies have demonstrated no change in either serum warfarin concentration or prothrombin time with the addition of sucralfate to chronic warfarin therapy.

• The mechanism of these interactions appears to be nonsystemic in nature, presumably resulting from sucralfate binding to the concomitant agent in the gastrointestinal tract. In all cases studied to date (cimetidine, ciprofloxacin, digoxin, norfloxacin, ofloxacin, and ranitidine), dosing the concomitant medication 2 hours before sucralfate eliminated the interaction. Due to CARAFATE's potential to alter the absorption of some drugs, CARAFATE should be administered separately from other drugs when alterations in bioavailability are felt to be critical. In these cases, patients should be monitored appropriately.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

• 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.

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Sucralfate in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Sucralfate during labor and delivery.

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

• Safety and effectiveness in pediatric patients have not been established.

Geriatic Use

• Clinical studies of CARAFATE 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. Because 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.

Gender

There is no FDA guidance on the use of Sucralfate with respect to specific gender populations.

Race

There is no FDA guidance on the use of Sucralfate with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Sucralfate in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Sucralfate in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Sucralfate in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Sucralfate in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

Monitoring

• Close monitoring of glycemia in diabetic patients treated with sucralfate suspension is recommended.

IV Compatibility

There is limited information regarding IV Compatibility of Sucralfate in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

• 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.

Management

• Due to limited experience in humans with overdosage of sucralfate, no specific treatment recommendations can be given.

Chronic Overdose

There is limited information regarding Chronic Overdose of Sucralfate in the drug label.

Pharmacology

Sucralfate
Systematic (IUPAC) name
Hexadeca-μ-hydroxytetracosahydroxy[μ8-[1,3,4,6-tetra-O-sulfo-β-Dfructofuranosyl-α-D-glucopyranoside tetrakis(hydrogen sulfato)8-)]]hexadecaaluminum
Identifiers
CAS number	54182-58-0
ATC code	A02BX02
PubChem	6398525
DrugBank	DB00364
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	2086.75 g/mol
Pharmacokinetic data
Bioavailability	3-5% (local acting)
Metabolism	GI; liver: unknown
Half life	unknown
Excretion	feces, urine
Therapeutic considerations
Pregnancy cat.	B
Legal status	℞-only
Routes	oral, suspension, rectal suspension

Mechanism of Action

• Sucralfate is only minimally absorbed from the gastrointestinal tract. The small amounts of the sulfated disaccharide that are absorbed are excreted primarily in the urine.

• Although the mechanism of sucralfate’s ability to accelerate healing of duodenal ulcers remains to be fully defined, it is known that it exerts its effect through a local, rather than systemic, action. The following observations also appear pertinent:

• Studies in human subjects and with animal models of ulcer disease have shown that sucralfate forms an ulcer-adherent complex with proteinaceous exudate at the ulcer site.
• In vitro, a sucralfate-albumin film provides a barrier to diffusion of hydrogen ions.
• In human subjects, sucralfate given in doses recommended for ulcer therapy inhibits pepsin activity in gastric juice by 32%.
• In vitro, sucralfate adsorbs bile salts.

• These observations suggest that sucralfate’s antiulcer activity is the result of formation of an ulcer-adherent complex that covers the ulcer site and protects it against further attack by acid, pepsin, and bile salts. There are approximately 14 to 16 mEq of acid-neutralizing capacity per 1 g dose of sucralfate.

Structure

• CARAFATE Suspension contains sucralfate and sucralfate is an α-D-glucopyranoside, β-D-fructofuranosyl-, octakis-(hydrogen sulfate), aluminum complex.

This image is provided by the National Library of Medicine.

• CARAFATE Suspension for oral administration contains 1 g of sucralfate per 10 mL.

• CARAFATE Suspension also contains: colloidal silicon dioxide NF, FD&C Red #40, flavor, glycerin USP, methylcellulose USP, methylparaben NF, microcrystalline cellulose NF, purified water USP, simethicone USP, and sorbitol solution USP. Therapeutic category: antiulcer.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Sucralfate in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Sucralfate in the drug label.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

• Chronic oral toxicity studies of 24 months’ duration were conducted in mice and rats at doses up to 1 g/kg (12 times the human dose).

• There was no evidence of drug-related tumorigenicity. A reproduction study in rats at doses up to 38 times the human dose did not reveal any indication of fertility impairment. Mutagenicity studies were not conducted.

Clinical Studies

• In a multicenter, double-blind, placebo-controlled study of CARAFATE Suspension, a dosage regimen of 1 g (10 mL) four times daily was demonstrated to be superior to placebo in ulcer healing.

This image is provided by the National Library of Medicine.

• Equivalence of sucralfate suspension to sucralfate tablets has not been demonstrated.

How Supplied

• CARAFATE (sucralfate) Suspension 1 g/10 mL is a pink suspension supplied in bottles of 14 fl oz (NDC 58914-170-14).

• SHAKE WELL BEFORE USING. AVOID FREEZING.

• Store at controlled room temperature 20-25°C (68-77°F).

Storage

There is limited information regarding Sucralfate Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Sucralfate in the drug label.

Precautions with Alcohol

• Alcohol-Sucralfate interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• Carafate®

Look-Alike Drug Names

There is limited information regarding Sucralfate Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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