Apo-Sucralfate

Apo-Sucralfate

sucralfate

Manufacturer:

Apotex

Distributor:

Pharmaforte
Full Prescribing Info
Contents
Sucralfate.
Description
Each tablet contains 1 g of sucralfate.
Action
Pharmacotherapeutic Group: Gastro-Duodenal Cytoprotective Agent.
Pharmacology: Pharmacodynamics: Sucralfate exerts a generalized gastric cytoprotective effect by enhancing natural mucosal defense 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, aspirin, 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 aluminium. The aluminium moiety can dissociate at low pH and aluminium release in the stomach can be expected; however, aluminium is poorly absorbed from the intact gastrointestinal tract. Following administration of 1 g of sucralfate tablets four times a day to individuals with normal renal function, approximately 0.001% to 0.017% of sucralfate's aluminium content is absorbed and excreted in the urine. This results in an aluminium load of between 0.008 mg and 0.136 mg following a 4 g daily dose. Individuals with normal renal function excrete absorbed aluminium can respond to an increased aluminium load by increasing urinary excretion. These values were determined in individuals with intact gastrointestinal mucosa. Available evidence does not indicate that absorption of aluminium would be different in individuals with ulcerated gastrointestinal mucosa.
Experiments have shown that sucralfate is not an antacid.
A comparative clinical trial of the efficacy of sucralfate following administration of Apo-Sucralfate and in 63% of patients given Sucralfate. There was no statistical difference between treatments in terms of ulcer healing.
Indications/Uses
APO-SUCRALFATE (sucralfate) is indicated for the treatment of duodenal and non-malignant gastric ulcer.
APO-SUCRALFATE is also not indicated for the prophylaxis of duodenal ulcer recurrence.
Dosage/Direction for Use
The recommended adult oral dosage of APO-SUCRALFATE (sucralfate) for duodenal and gastric ulcer is one tablet of 1 gram four times a day, one hour before meals and at bedtime, on an empty stomach. For duodenal ulcer, APO-SUCRALFATE 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 sucralfate 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 APO-SUCRALFATE 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 1/2 hour before or after APO-SUCRALFATE intake.
Duration of continuous treatment in patients with chronic renal failure receiving dialysis should be elevated by periodic monitoring of serum aluminium levels, due to the possiblity of aluminium accumulation in these patients (see PRECAUTIONS). According to information widely available in the literature, patients with serum aluminium concentrations that approach to 100 ug/L should be carefully monitored for symptoms of aluminium 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 aluminium toxicity while receiving the recommended doses of sucralfate. Physician discretion should be exercised when considering the duration of treatment (see PRECAUTIONS).
Overdosage
Overdosage has never been observed with 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 under ADVERSE REACTIONS, such as constipation. These should be treated symptomatically.
Contraindications
There are no known contraindications to the use of APO-SUCRALFATE (sucralfate). However, the physician should read text under "WARNINGS" when considering the use of this drug in pregnant women or women of child-bearing potential.
Warnings
Use in pregnancy: There has been no experience to date with the use of APO-SUCRALFATE (sucralfate). Therefore, sucralfate should not be used in pregnant women or women of child-bearing potential unless, in the judgement of the physician, the anticipated benefits outweigh the potential risk.
Use in children: Clinical experience in children is limited. Therefore, sucralfate therapy cannot be recommended for children under 18 unless, in the judgement of the physician, anticipated benefits outweigh the potential risk.
Special Precautions
General: The following should be taken into account before treating patients with APO-SUCRALFATE (sucralfate): Recurrence may be observed in patients after a successful course of treatment for gastric or duodenal ulcers. While 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.
Use In Pregnancy & Lactation
Use in pregnancy: There has been no experience to date with the use of APO-SUCRALFATE (sucralfate). Therefore, sucralfate should not be used in pregnant women or women of child-bearing potential unless, in the judgement of the physician, the anticipated benefits outweigh the potential risk.
Adverse Reactions
Very few side effects have been reported with sucralfate. They are mild in nature and have only exceptionally led to discontinuation of therapy.
The main complaint has been constipation ranging from .7% to 3.3% of patients.
Other side effects reported included diarrhea, nausea, gastric discomfort, indigestion, dry mouth, skin rash, pruritus, back pain, dizziness, sleepiness and vertigo.
Drug Interactions
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.
Animals studies have shown that simultaneous administration of sucralfate with tetracycline, phenytoin or cimetidine results in 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.
These interactions appear to be non-systemic and to result from the binding of sucralfate to 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.
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.
Chronic Renal Failure: Dialyzed Patients: Sucralfate should be used with caution in patients with chronic renal failure. When sucralfate is administered orally, small amounts of aluminium are absorbed from the gastrointestinal tract (see PHARMACOLOGY under ACTIONS). Existing evidence indicates that patients with normal renal function receiving the recommended doses of sucralfate adequately excrete aluminium in the urine; however, patients with chronic renal failure or those receiving dialysis have impaired excretion of absorbed aluminium, and in these individuals, aluminium is known to accumulate in serum and in tissues. In particular, dialysis patients are at greater risk as aluminium does not cross dialysis membranes of the dialysis machine since it is bound to plasma proteins, most notably albumin and trasferrin.
In patients with chronic renal failure undergoing dialysis, aluminium-related toxicity (encephalopathy and aluminium-related bone disease), associated with the administration of sucralfate and/or other sources of aluminium before administering sucralfate in combination with other aluminium-containing medications, such as aluminium-containing antacids.
Nondialyzed Patients: 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 aluminium concentrations which plateaued at approximately 23 ug/L after one week of treatment from a pretreatment level of 3 ug/L. Renal aluminium clearance increased in relation to the increase in serum levels and returned to baseline within two weeks following discontinuation of sucralfate as did serum aluminium 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 aluminium may be impaired in these individuals.
Storage
Keep container tightly closed. Store at room temperature. Protect from humidity.
ATC Classification
A02BX02 - sucralfate ; Belongs to the class of other drugs used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Presentation/Packing
Tab 1 g (white capsule-shaped, engraved "APO-1g on one side) x 100's.
Exclusive offer for doctors
Register for a MIMS account and receive free medical publications worth $139 a year.
Sign up for free
Already a member? Sign in