Sucralfate

SUCRALFATE- sucralfate suspension
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DESCRIPTION

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

Chemical Structure
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Sucralfate Oral Suspension for oral administration contains 1 g of sucralfate, USP per 10 mL.

Sucralfate Oral Suspension also contains: cherry flavor, colloidal silicon dioxide, FD&C Red #40, glycerin, methylcellulose, methylparaben, microcrystalline cellulose, purified water, simethicone emulsion, and sorbitol solution. Therapeutic category: antiulcer.

CLINICAL PHARMACOLOGY

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:

  1. 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.
  2. In vitro , a sucralfate-albumin film provides a barrier to diffusion of hydrogen ions.
  3. 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.

CLINICAL TRIALS

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

Results from Clinical Trials Healing Rates for Acute Duodenal Ulcer

Treatment

n

Week 2 Healing Rates

Week 4 Healing Rates

Week 8 Healing Rates

Sucralfate Oral Suspension

145

23 (16%) *

66 (46%)

95 (66%)

Placebo

147

10 (7%)

39 (27%)

58 (39%)

* P =0.016 P =0.001 P =0.0001

Equivalence of Sucralfate Oral Suspension to sucralfate tablets has not been demonstrated.

INDICATIONS AND USAGE

Sucralfate Oral Suspension is indicated in the short-term (up to 8 weeks) treatment of active duodenal ulcer.

CONTRAINDICATIONS

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

WARNINGS

Fatal complications, including pulmonary and cerebral emboli have occurred with inappropriate intravenous administration of Sucralfate Oral Suspension. Administer Sucralfate Oral Suspension only by the oral route. Do not administer intravenously.

PRECAUTIONS

The physician should read the ” PRECAUTIONS ” section when considering the use of sucralfate oral suspension 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 Oral Suspension is recommended. Adjustment of the anti-diabetic treatment dose during the use of Sucralfate Oral 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 Sucralfate Oral Suspension’s potential to alter the absorption of some drugs, Sucralfate Oral Suspension should be administered separately from other drugs when alterations in bioavailability are felt to be critical. In these cases, patients should be monitored appropriately.

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.

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.

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