Sulcrate - Product Information
|Condition:||Duodenal Ulcer Prophylaxis, Duodenal Ulcer, GERD, Hyperphosphatemia of Renal Failure, Stress Ulcer Prophylaxis, Stomatitis, Stomach Ulcer (Gastric Ulcer)|
|Class:||Miscellaneous GI agents|
|Ingredients:||sucralfate, hydrogenated vegetable oil, calcium carboxy-methylcellulose, magnesium stearate, microcrystalline cellulose, glycerine, sodium methylparaben, sodium propylparaben, sodium phosphate monobasic, xanthan gum, caramel artificial flavour|
1 g Tablets
SULCRATE SUSPENSION PLUS
1 g/5 mL Oral Suspension
Action and Clinical Pharmacology
SULCRATE (sucralfate) exerts a generalized gastric cytoprotective effect by enhancing natural mucosal defence mechanisms. Studies conducted in animals and clinical trials in humans have demonstrated that sucralfate can protect the gastric mucosa against various irritants such as alcohol, acetylsalicylic acid (ASA), hydrochloric acid, sodium hydroxide or sodium taurocholate.
In addition, sucralfate has been demonstrated to have a greater affinity for ulcerated gastric or duodenal mucosa than for non-ulcerated mucosa.
Sucralfate produces an adherent and cytoprotective barrier at the ulcer site. This barrier protects the ulcer site from the potential ulcerogenic properties of acid, pepsin and bile.
Furthermore, sucralfate blocks acid diffusion across the sucralfate protein barrier and also complexes directly with pepsin and bile.
The action of sucralfate is non-systemic as the drug is only minimally absorbed from the gastrointestinal tract. The minute amounts of the sulfated disaccharide which are absorbed are primarily excreted in the urine.
Each gram of sucralfate contains approximately 200 mg of aluminum. The aluminum moiety can dissociate at low pH and aluminum release in the stomach can be expected; however, aluminum is poorly absorbed from the intact gastrointestinal tract. Following administration of 1 g of sucralfate (tablets or suspension) four times a day to individuals with normal renal function, approximately 0.001% to 0.017% of sucralfate's aluminum content is absorbed and excreted in the urine. This results in an aluminum load of between 0.008 mg and 0.136 mg following a 4 g daily dose. Individuals with normal renal function excrete absorbed aluminum and can respond to an increased aluminum load by increasing urinary excretion.
These values were determined in individuals with intact gastrointestinal mucosa. Available evidence does not indicate that absorption of aluminum would be different in individuals with ulcerated gastrointestinal mucosa.
Experiments have shown that sucralfate is not an antacid.
Indications and Clinical Use
SULCRATE (sucralfate) tablets are indicated for the treatment of duodenal and onmalignant gastric ulcer.
SULCRATE tablets are also indicated for the prophylaxis of duodenal ulcer recurrence.
SULCRATE SUSPENSION PLUS is indicated for the treatment of duodenal ulcer and for the prophylaxis of gastrointestinal hemorrhage due to stress ulceration in critically ill patients.
Patients with known hypersensitivity to the active substance or to any of the excipients.
The physician should read the "WARNINGS" section when considering the use of this drug in pregnant or pediatric patients, or patients of childbearing potential.
Use in Pregnancy
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.
Clinical experience in children is limited. Therefore, sucralfate therapy cannot be recommended for children under 18 unless, in the judgment of the physician, anticipated benefits outweigh the potential risk.
SULCRATE must not be administered intravenously. Inadvertent intravenous administration of insoluble sucralfate and its insoluble excipients may induce fatal complications including pulmonary and cerebral emboli. Other severe complications including aluminium intoxication are reported after intravenous administration.
The following should be taken into account before treating patients with SULCRATE (sucralfate):
- Recurrence may be observed in patients after a successful course of treatment for gastric or duodenal ulcers. While the 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 underlying cause of ulcer disease.
- Proper diagnosis is important since symptomatic response to sucralfate therapy does not rule out the presence of a gastric malignancy.
- 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.
- Due to the carbohydrate content of sucralfate suspension excipients, 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.
Antacids should not be taken within half an hour before or after sucralfate intake because of the possibility of decreased binding of sucralfate with the gastro-duodenal mucosa as a consequence of a change of intra-gastric pH.
Animal studies have shown that simultaneous administration of sucralfate with tetracycline, phenytoin or cimetidine results in a statistically significant reduction in the bioavailability of these agents. Cimetidine absorption was not reduced in humans.
In clinical trials, the concomitant administration of sucralfate reduced the bioavailability of digoxin. In case of simultaneous administration, the extent of absorption of phenytoin, warfarin, and fluoroquinolone antibiotics (e.g. ciprofloxacin and norfloxacin) is also reduced. These interactions appear to be non-systemic and to result from the binding of sucralfate the concomitantly administered drug in the gastrointestinal tract. In all cases, complete bioavailability was restored by separating the administration of sucralfate from that of the other agent by 2 hours.
Sucralfate, administered respectively 30 and 60 minutes before ASA or ibuprofen did not alter the bioavailability of these agents. In a study comparing the prior administration of a single dose of sucralfate tablets on the bioavailability of naproxen, indomethacin or ketoprofen versus administration in the absence of sucralfate, it was shown that the total amount of these drugs absorbed was not altered; however, the peak concentration of each was reduced, and the time to reach peak concentration was delayed. A single dose of SULCRATE SUSPENSION PLUS administered one-half hour before naproxen had a similar effect on the bioavailability of naproxen.
The physician should consider the possible clinical implications of these interactions. It is recommended to separate the administration of any drug from that of sucralfate when the potential for altered bioavailability is felt to be critical to the effectiveness of that drug.
Unless specified, the above data are based on studies carried out with SULCRATE tablets.
Chronic Renal Failure
Sucralfate should be used with caution in patients with chronic renal failure. When sucralfate is administered orally, small amounts of aluminum are absorbed from the gastrointestinal tract (see ACTIONS AND CLINICAL PHARMACOLOGY). Existing evidence indicates that patients with normal renal function receiving the recommended doses of sucralfate adequately excrete aluminum in the urine; however, patients with chronic renal failure or those receiving dialysis have impaired excretion of absorbed aluminum, and in these individuals, aluminum is known to accumulate in serum and in tissues. In particular, dialysis patients are at greater risk as aluminum does not cross dialysis membranes of the dialysis machine since it is bound to plasma proteins, most notably albumin and transferrin.
In patients with chronic renal failure undergoing dialysis, aluminum-related toxicity (encephalopathy and aluminum-related bone disease), associated with the administration of sucralfate and/or other sources of aluminum has been reported. Consideration should therefore be given to the total daily load of aluminum before administering sucralfate in combination with other aluminum-containing medications, such as aluminum-containing antacids.
In a study of six nondialyzed chronic renal failure patients with glomerular filtration rates ranging from approximately 10 to 40% of normal, sucralfate administered at a dose of 1 g QID for three weeks resulted in elevated serum aluminum concentrations which plateaued at approximately 23 μg/L after one week of treatment from a pretreatment level of 3 μg/L. Renal aluminum clearance increased in relation to the increase in serum levels and returned to baseline within two weeks following discontinuation of sucralfate as did serum aluminum concentrations. No adverse events were reported in these patients.
These data indicate that the use of sucralfate in nondialyzed chronic renal failure patients requires physician discretion since the excretion of absorbed aluminum may be impaired in these individuals.
Cases of hypersensitivity have been reported with the use of sucralfate, including anaphylactic reactions, bronchospasm, dyspnoea, laryngeal oedema, lip swelling, oedema mouth, pharyngeal oedema, pruritus, rash, respiratory tract oedema, swelling face and urticaria.
- SULCRATE Tablets
Very few side effects have been reported with SULCRATE (sucralfate) tablets. They are mild in nature and have only exceptionally led to discontinuation of therapy.
The main complaint has been constipation ranging from 1.7% to 3.3% of patients.
Other side effects reported included diarrhea, nausea, gastric discomfort, indigestion, dry mouth, back pain, dizziness, sleepiness and vertigo.
Bezoars have been reported in patients treated with sucralfate (SULCRATE tablets). 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.
- SULCRATE SUSPENSION PLUS
In a placebo-controlled clinical trial involving 184 patients, the adverse event rates for SULCRATE SUSPENSION PLUS were similar to that seen in the placebo group (SULCRATE SUSPENSION PLUS 10.2% vs placebo 7.4%). The most common adverse event was headache (3.4%) followed by nausea (2.3%), abdominal pain (2.3%), constipation (1.1%), diarrhea (1.1%), and urticaria (1.1%). Only headache, abdominal pain and nausea had a higher incidence in the SULCRATE SUSPENSION PLUS group relative to placebo.
Bezoars have also been reported in patients treated with sucralfate (SULCRATE SUSPENSION PLUS). 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.
See the PRECAUTIONS section for information on the potential for aluminum toxicity in dialyzed chronic renal failure patients.
Due to the carbohydrate content of sucralfate suspension excipients, episodes of hyperglycemia have been reported in diabetic patients.
Symptoms and Treatment of Overdosage
Overdosage has never been observed with SULCRATE (sucralfate) and appears to be unlikely since, using maximal doses of up to 12 g/kg/body weight in a variety of animal species, a lethal dose could not be established.
Overdosage is likely to be associated with symptoms similar to those described in the ADVERSE REACTION section, such as constipation. These should be treated symptomatically.
|For management of suspected drug overdose, contact your regional Poison Control Center.|
Dosage and Administration
The recommended adult oral dosage of SULCRATE (sucralfate) for duodenal and gastric ulcer is one tablet of 1 g four times a day, one hour before meals and at bedtime, on an empty stomach. For duodenal ulcer, SULCRATE may also be administered as two 1 g tablets twice daily, on waking and at bedtime on an empty stomach.
In duodenal ulcers, while healing with SULCRATE often occurs within two to four weeks, treatment should be continued for a maximum of 8 to 12 weeks unless healing has been demonstrated by X-Ray and/or endoscopic examination.
In the case of gastric ulcers, an alternative treatment should be considered if no objective improvement is observed following 6 weeks of SULCRATE therapy. However, patients with a large gastric ulcer that has demonstrated a progressive healing tendency may require an additional 6 weeks of treatment.
For the prophylaxis of duodenal ulcer recurrence, the recommended dosage is one tablet of 1 g twice daily, on an empty stomach. Treatment may be continued for up to one year. For relief of pain, antacids may be added to the treatment. However, antacids should not be taken within ½ hour before or after SULCRATE intake.
SULCRATE SUSPENSION PLUS (1 g/5 mL)
SULCRATE must not be administered intravenously.
The recommended adult dose of SULCRATE SUSPENSION PLUS for the treatment of (acute) duodenal ulcer is 2 g (10 mL) twice a day on waking and at bedtime on an empty stomach.
For the prophylaxis of gastrointestinal hemorrhage due to stress ulceration, administer 1 g (5 mL) orally or via nasogastric tube four to six times a day. To prevent clogging of the nasogastric tube flush with 10 mL of water following each administration.
The duration of treatment for prophylaxis of stress ulceration must be individually determined. Treatment should be continued for as long as one or more of the risk factors for stress ulceration is present but normally not for more than 14 days.
Duration of continuous treatment in patients with chronic renal failure receiving dialysis should be evaluated by periodic monitoring of serum aluminum levels, due to the possibility of aluminum accumulation in these patients (see PRECAUTIONS). According to information widely available in the literature, patients with serum aluminum concentrations that approach 100 μg/L should be carefully monitored for symptoms of aluminum toxicity and treatment should be discontinued if such symptoms appear.
There is no evidence to indicate that patients with chronic renal failure, who do not require dialysis, are at risk of developing aluminum toxicity while receiving the recommended doses of sucralfate. Physician discretion should be exercised when considering the duration of treatment (see PRECAUTIONS).