Sucralfate

SUCRALFATE- sucralfate tablet
Nostrum Laboratories, Inc.

DESCRIPTION

Sucralfate is an α-D-glucopyranoside, β-D-fructofuranosyl-, octakis-(hydrogen sulfate), aluminum complex. It has the following structural formula:

Sucralfate Tablets contain sucralfate and sucralfate is an α-D-glucopyranoside, β-D-fructofuranosyl-, octakis-(hydrogen sulfate), aluminum complex.

Tablets for oral administration contain 1 g of sucralfate, USP.

Also contain: povidone, magnesium stearate, and colloidal silicon dioxide.

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%.
  4. In vitro , sucralfate adsorbs bile salts.

These observations suggest that sucralfate’s antiulcer activity is the result of formation of an ulceradherent 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

Acute Duodenal Ulcer

Over 600 patients have participated in well-controlled clinical trials worldwide. Multicenter trials conducted in the United States, both of them placebo-controlled studies with endoscopic evaluation at 2 and 4 weeks, showed:

STUDY 1

Treatment Groups Ulcer Healing/ No. Patients
2 wk 4 wk (Overall)
Sucralfate 37/105 (35.2%) 82/109 (75.2%)
Placebo 26/106 (24.5%) 68/107 (63.6%)

STUDY 2

Treatment Groups Ulcer Healing/ No. Patients
2 wk 4 wk (Overall)
Sucralfate 8/24 (33%) 22/24 (92%)
Placebo 4/31 (13%) 18/31 (58%)

The sucralfate-placebo differences were statistically significant in both studies at 4 weeks but not at 2 weeks. The poorer result in the first study may have occurred because sucralfate was given 2 hours after meals and at bedtime rather than 1 hour before meals and at bedtime, the regimen used in international studies and in the second United States study. In addition, in the first study liquid antacid was utilized as needed, whereas in the second study antacid tablets were used.

Maintenance Therapy After Healing of Duodenal Ulcer

Two double-blind randomized placebo-controlled U.S. multicenter trials have demonstrated that sucralfate (1 g bid) is effective as maintenance therapy following healing of duodenal ulcers.

In one study, endoscopies were performed monthly for 4 months. Of the 254 patients who enrolled, 239 were analyzed in the intention-to-treat life table analysis presented below.

Duodenal Ulcer Recurrence Rate (%)
Drug Months of Therapy
n 1 2 3 4
Sucralfate 122 20* 30* 38† 42†
Placebo 117 33 46 55 63

*P <0.05, †P <0.01

In this study, prn antacids were not permitted.

In the other study, scheduled endoscopies were performed at 6 and 12 months, but for-cause endoscopies were permitted as symptoms dictated. Median symptom scores between the sucralfate and placebo groups were not significantly different. A life table intention-to-treat analysis for the 94 patients enrolled in the trial had the following results:

Duodenal Ulcer Recurrence Rate (%)
Drug n 6 months 12 months
Sucralfate 48 19* 27*
Placebo 46 54 65

*P <0.002

In this study, prn antacids were permitted.

Data from placebo-controlled studies longer than 1 year are not available.

Sucralfate Indications and Usage

Sucralfate tablets are indicated in:

  • Short-term treatment (up to 8 weeks) of active duodenal ulcer. 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.
  • Maintenance therapy for duodenal ulcer patients at reduced dosage after healing of acute ulcers.

CONTRAINDICATIONS

Sucralfate tablets are contraindicated in patients with known hypersensitivity reactions to the active substance or to any of the excipients.

PRECAUTIONS

The physician should read the “PRECAUTIONS” section when considering the use of this drug 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.

Isolated reports of sucralfate tablet aspiration with accompanying respiratory complications have been received. Therefore, sucralfate tablets should be used with caution by patients who have known conditions that may impair swallowing, such as recent or prolonged intubation, tracheostomy, prior history of aspiration, dysphagia, or any other conditions that may alter gag and cough reflexes, or diminish oropharyngeal coordination or motility.

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.

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