Kulent-O

Sucralfate:

• Description
• Clinical pharmacology
• Clinical trials
• Indications and usage
• Contraindications
• Precautions
• Adverse reactions
• Overdosage
• Dosage and administration
• Sucralfate 1gm tablet
• Kulent-O (Sucralfate) reviews

DESCRIPTION

Kulent-O (Sucralfate) is an α-D-glucopyranoside, β-D-fructofuranosyl-, octakis(hydrogen sulfate), aluminum complex.

R = SO Al(OH) _{3 2}

Tablets for oral administration contain 1 g of Kulent-O (Sucralfate).

Structural formula for Kulent-O (Sucralfate)

CLINICAL PHARMACOLOGY

Kulent-O (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 Kulent-O (Sucralfate) forms an ulcer-adherent complex with proteinaceous exudate at the ulcer site.
• , a sucralfate-albumin film provides a barrier to diffusion of hydrogen ions. In vitro
• In human subjects, Kulent-O (Sucralfate) given in doses recommended for ulcer therapy inhibits pepsin activity in gastric juice by 32%.
• , Kulent-O (Sucralfate) absorbs bile salts. In vitro

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 Kulent-O (Sucralfate).

CLINICAL TRIALS

INDICATIONS AND USAGE

Kulent-O (Sucralfate) is indicated in:

• Short-term treatment (up to 8 weeks) of active duodenal ulcer. While healing with Kulent-O (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

There are no known contraindications to the use of Kulent-O (Sucralfate).

PRECAUTIONS

Duodenal ulcer is a chronic, recurrent disease. While short-term treatment with Kulent-O can result in complete healing of the ulcer, a successful course of treatment with Kulent-O (Sucralfate) should not be expected to alter the posthealing frequency or severity of duodenal ulceration.

Special Populations

Drug Interactions

Some studies have shown that simultaneous Kulent-O 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 Kulent-O (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 Kulent-O (Sucralfate) to chronic warfarin therapy.

The mechanism of these interactions appears to be nonsystemic in nature, presumably resulting from Kulent-O (Sucralfate) binding to the concomitant agent in the gastrointestinal tract. In all case studies to date (cimetidine, ciprofloxacin, digoxin, norfloxacin, ofloxacin, and ranitidine), dosing the concomitant medication 2 hours before Kulent-O (Sucralfate) eliminated the interaction. Because of the potential of Kulent-O (Sucralfate) to alter the absorption of some drugs, Kulent-O (Sucralfate) 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

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 Kulent-O is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Clinical studies of Kulent-O (Sucralfate) tablets 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. DOSAGE AND ADMINISTRATION

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. PRECAUTIONS Special Populations Chronic Renal Failure and Dialysis Patients

ADVERSE REACTIONS

Adverse reactions to Kulent-O (Sucralfate) in clinical trials were minor and only rarely led to discontinuation of the drug. In studies involving over 2700 patients treated with Kulent-O (Sucralfate) tablets, 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:

OVERDOSAGE

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

DOSAGE AND ADMINISTRATION

Kulent-O 1gm Tablet