Sucralfate (Oral-Local)


VA CLASSIFICATION
Primary: GA302

Commonly used brand name(s): Apo-sucralfate; Carafate; Sulcrate; Sulcrate Suspension Plus.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antiulcer agent—

gastric mucosa protectant—

Indications

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.

Accepted

Ulcer, duodenal (treatment)—Sucralfate is indicated in the short-term (up to 8 weeks) treatment of duodenal ulcer. {31} {32}

Ulcer, duodenal (prophylaxis)—Sucralfate is used in the prevention of duodenal ulcer recurrence. {02} {31} {32} {48}

[Ulcer, gastric (treatment)]—Sucralfate is used for the short-term treatment of benign gastric ulcer. {03} {31} {48}

[Arthritis, rheumatoid (treatment adjunct)]1—Sucralfate is used for the relief of gastrointestinal symptoms associated with the use of nonsteroidal anti-inflammatory drugs in the treatment of rheumatoid arthritis. {01} {06}

[Stress-related mucosal damage (prophylaxis and treatment) ]—Sucralfate is used to prevent and treat gastrointestinal, stress-induced ulceration and bleeding, especially in intensive care patients. {17} {18} {19} {26}

[Reflux, gastroesophageal (treatment)]—Sucralfate is used in the treatment of gastroesophageal reflux disease . {34} {35} {36} {37} {46}

1 Not included in Canadian product labeling.



Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Sucralfate is an aluminum salt of a sulfated disaccharide.

Mechanism of action/Effect:

Exact mechanism of action is not known; however, sucralfate is thought to form an ulcer-adherent complex with proteinaceous exudate, such as albumin and fibrinogen, at the ulcer site, protecting it against further acid attack {32}. To a lesser extent, sucralfate forms a viscous, adhesive barrier on the surface of intact mucosa of the stomach and duodenum {04}. Sucralfate also inhibits pepsin activity and has been found to bind bile salts in vitro . Recent information suggests that sucralfate may increase the production of prostaglandin E 2 and gastric mucus {08} {09} {31}.

Absorption:

Up to 5% of the disaccharide component and less than 0.02% of aluminum is absorbed from the gastrointestinal tract following an oral sucralfate dose {24} {30}.

Elimination:
    Mostly fecal; small amounts of sulfate disaccharide are eliminated in the urine.


Precautions to Consider

Pregnancy/Reproduction

Pregnancy—
Studies in humans have not been done.

Studies in animals have not shown that sucralfate causes adverse effects on the fetus.

FDA Pregnancy Category B {32}.

Breast-feeding

Problems in humans have not been documented.

Pediatrics

Appropriate studies to date have not demonstrated pediatrics-specific problems that would limit the usefulness of sucralfate in children {34} {35}.


Geriatrics


Although adequate and well-controlled studies on the relationship of age to the effects of sucralfate have not been performed in the geriatric population, no geriatrics-specific problems have been documented to date.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

Aluminum-containing medications, such as:
Antacids
Antidiarrheals
Aspirin, buffered with aluminum
Vaginal douches{11}    (concurrent use with sucralfate in patients with renal failure may cause aluminum toxicity {13} {14} {32})


Antacids    (concurrent use with antacids in the treatment of duodenal ulcer may be indicated for the relief of pain; however, simultaneous administration is not recommended since antacids may interfere with binding of sucralfate to the mucosa; patient should be advised not to take antacids within 1/2 hour before or after sucralfate {31})


Cimetidine{32}{40} or
Ranitidine{32}{39}{40}    (concurrent use with sucralfate may decrease the absorption of cimetidine or ranitidine; patients should be advised to take cimetidine or ranitidine 2 hours before sucralfate {40})


» Ciprofloxacin{45} or
» Norfloxacin{28}{29}{45} or
» Ofloxacin    (concurrent use with sucralfate may decrease the absorption of ciprofloxacin, norfloxacin, or ofloxacin by chelation, resulting in lower serum and urine concentrations of these 3 medicines; patients should be advised to take ciprofloxacin, norfloxacin, or ofloxacin 2 to 3 hours before sucralfate {12} {15} {24})


» Digoxin{05}{32}{45} or
» Theophylline{32}{38}{45}    (concurrent use with sucralfate may decrease the absorption of digoxin or theophylline; patients should be advised not to take sucralfate within 2 hours of digoxin or theophylline {32})


» Phenytoin    (concurrent use with sucralfate may decrease the absorption of phenytoin enough to reduce the steady-state blood concentrations of phenytoin with a resultant loss of seizure control; patients should be advised not to take sucralfate within 2 hours of phenytoin {32} {33})


Tetracyclines, oral    (absorption may be decreased when oral tetracyclines are used concurrently with sucralfate, since sucralfate is an aluminum salt and may form nonabsorbable complexes with tetracycline; patients should be advised not to take sucralfate within 2 hours of tetracyclines {32})


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefits should be considered when the following medical problems exist
Dysphagia or
Gastrointestinal tract obstruction disease    (patients with these conditions may be at risk of bezoar formation because of the protein-binding properties of sucralfate {41} {42})


Renal failure    (absorption of the aluminum in sucralfate in patients with renal failure may cause aluminum toxicity, especially with long-term use {07} {13} {14} {24} {32})


Sensitivity to sucralfate

Patient monitoring
The following may be especially important in patient monitoring (other tests may be warranted in some patients, depending on condition; » = major clinical significance):

Serum aluminum concentrations    (determinations may be increased in patients with renal failure {07} {13} {14} {32})




Side/Adverse Effects

Note: Occurrence of drowsiness progressing to seizures in patients with renal failure may indicate aluminum toxicity.

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent {32}
    
Constipation

Incidence less frequent or rare {32}
    
Backache
    
diarrhea
    
dizziness or lightheadedness
    
drowsiness
    
dryness of mouth
    
indigestion
    
nausea
    
skin rash, hives, or itching
    
stomach cramps or pain





Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Sucralfate (Oral).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to sucralfate
Other medications, especially ciprofloxacin, digoxin, norfloxacin, ofloxacin, phenytoin, and theophylline

Proper use of this medication
Taking on empty stomach 1 hour before meals and at bedtime

Compliance with full course of therapy and keeping appointments for check-ups

» Proper dosing
Missed dose: Taking as soon as possible; not taking if almost time for next dose; not doubling doses

» Proper storage

Precautions while using this medication
» Not taking antacids within 1/2 hour before or after sucralfate


Side/adverse effects
Signs of potential side effects, especially aluminum toxicity


General Dosing Information
Sucralfate should be taken with water on an empty stomach, 1 hour before each meal and at bedtime, for maximum effectiveness. {32}

Short-term treatment with sucralfate may result in complete healing of the ulcer but it may not alter the posthealing frequency or severity of duodenal ulceration.

If required, antacids may be administered 1/2 hour before or after sucralfate for the relief of pain. {31}

Even though the symptoms of duodenal ulcers may subside, unless healing has been documented by x-ray or endoscopic examination, therapy should continue for at least 4 to 8 weeks. {31}

Use of sucralfate in a nasogastric feeding tube has resulted in bezoar formation with other medications or enteral feedings, due to the protein-binding properties of sucralfate. {43} {44}


Oral Dosage Forms

Note: Bracketed uses in the Dosage Forms section refer to categories of use and/or indications that are not included in U.S. product labeling.

SUCRALFATE ORAL SUSPENSION

Usual adult and adolescent dose
Duodenal ulcer (treatment)
Oral, 1 gram four times a day one hour before each meal and at bedtime; or 2 grams two times a day on waking and at bedtime on an empty stomach. {31} {47}

[Gastroesophageal reflux ]
Oral, 1 gram four times a day one hour before each meal and at bedtime. {37} {46}

[Stress-related mucosal damage (prophylaxis)]
Oral, 1 gram four to six times a day {47}.

Note: Duration of treatment for prophylaxis of stress ulceration must be individually determined and should be continued for as long as risk factors are present; usually, treatment does not continue longer than fourteen days {47}.



Usual pediatric dose
Duodenal ulcer (treatment)
Dosage has not been established.

[Gastroesophageal reflux ]
Oral, 500 mg to 1 gram four times a day one hour before each meal and at bedtime. {34} {46}


Strength(s) usually available
U.S.—


500 mg per 5 mL (Rx) [Carafate]

Canada—


500 mg per 5 mL (Rx) [Sulcrate]


1 gram per 5 mL (Rx) [Sulcrate Suspension Plus (caramel-flavored )]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), in a tight container, unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • Shake well.


SUCRALFATE TABLETS USP

Usual adult and adolescent dose
Duodenal ulcer (treatment)
Oral, 1 gram four times a day one hour before each meal and at bedtime {47} {48}.

Duodenal ulcer (prophylaxis)
Oral, 1 gram two times a day on an empty stomach. {31} {32} {47} {48}

[Gastric ulcer (treatment) ] or
Oral, 1 gram four times a day one hour before each meal and at bedtime. {37}

[Gastroesophageal reflux ]
Oral, 1 gram four times a day one hour before each meal and at bedtime. {37}


Usual pediatric dose
Duodenal ulcer (treatment)
Dosage has not been established.

[Gastroesophageal reflux ]
Oral, 500 mg four times a day one hour before each meal and at bedtime. {34}


Strength(s) usually available
U.S.—


1 gram (Rx) [Carafate][Generic]

Canada—


1 gram (Rx) [Apo-sucralfate] [Sulcrate]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), in a tight container, unless otherwise specified by manufacturer.

Auxiliary labeling:
   • Continue medicine for full time of treatment.



Revised: 03/24/1998



References
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  1. Manufacturer comment, 1991 revision cycle.
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