Sucralfate CAS 54182-58-0

Sucralfate is indicated for the symptomatic treatment of gastric ulceration from various causes. In humans, sucralfate is as effective as antacids or H2-receptor antagonists in healing ulcers. It does not appear to be successful, however, in preventing corticosteroid-induced ulceration in dogs subjected to spinal surgery. Its efficacy in preventing NSAID-induced ulcers is unproven in the dog. Sucralfate has also been used to treat oral and esophageal ulcers and esophagitis.

FDA-Approved Indications
● Sucralfate is a unique anti-ulcer drug and is a basic aluminum salt of sucrose octa-sulfate. The labeled use of sucralfate is as follows:
● Duodenal Ulcer: Sucralfate is FDA-approved for treating duodenal ulcers for up to 8 weeks (short-term). Duodenal ulcers are treated with 1 g 4 times daily for 8 weeks, followed by 1 g twice-daily for maintenance therapy. The efficacy of sucralfate in the treatment of duodenal ulcers is shown to be comparable to that of cimetidine and intensive antacid therapy.
Sucralfate forms a protective coat and protects the gastric mucosa from pepsin, pectic acid, and bile salts. This drug binds to positively charged proteins in exudates, locally forming a thick viscous substance.

Off-Label Uses
● Dyspepsia: Sucralfate has been shown to reduce the frequency and intensity of dyspeptic symptoms and gastric erosion during NSAID therapy, and the efficacy is similar to that of an H2 receptor blocker.
● Epithelial wounds: Sucralfate has also been used as a topical drug in treating various epithelial wounds such as ulcers, inflammatory dermatitis, mucositis, and burns wounds. Several studies have been conducted to study sucralfate's efficacy in treating epithelial wounds.
Sucralfate increases the bioavailability of growth factors, especially fibroblast growth factor (FGF), which is pivotal in angiogenesis and promotes epithelial wound healing.
● Chemotherapy-induced mucositis: The results of a study by showed that high-potency sucralfate accelerates the activation of growth factors and helps treat chemotherapy-induced mucositis of the oropharynx and alimentary tract. This resulted from administering 1.5 g of sucralfate 3 times daily at the onset of mucositis for 2 days, followed by 1.5 g twice-daily throughout cancer therapy and 2 weeks after the completion of treatment.
● Radiation proctitis: Sucralfate paste enema has shown clinical improvement in hemorrhagic radiation proctitis treatment. This therapy uses a low-volume paste in an enema applicator, and pre-treatment and post-treatment improvements were assessed using clinical proctitis scores with a positive outcome. A study al has shown that a sucralfate enema is better than oral sulfasalazine in the short-term treatment of radiation proctitis.
● Prevention of ulceration of diversion colitis: Enemas containing sucralfate are shown to preserve the mucus layer covering the epithelium, thereby reducing inflammation in diversion colitis. The concentration of sucralfate used in the enema is 2 g/kg/d.
● Stress ulcer prophylaxis in ventilated patients: Research has shown that sucralfate is better for stress ulcer prophylaxis when compared to H2 blockers or antacids in patients receiving ventilation therapy as the latter increases the pH of gastric contents causing stagnation of gram-negative bacilli and subsequently increasing the risk of nosocomial pneumonia.
● Behcet disease: Topical sucralfate 1 g/5 mL 4 times daily alone or in combination with topical corticosteroids reduces pain and promotes the healing of oral ulcers in Behçet disease. Sucralfate suspension is the dosage form for treating oral ulcers in Behçet disease.
Gastroesophageal reflux disease: According to American College of Gastroenterology guidelines, sucralfate can be used during pregnancy for GERD.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric
Appropriate studies have not been performed on the relationship of age to the effects of sucralfate in the pediatric population. Safety and effectiveness have not been established.

Geriatric
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of sucralfate in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require caution and an adjustment in the dose for patients receiving this medicine.

Breastfeeding
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Drug Interactions
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
● Bictegravir
● Digoxin
● Dolutegravir
● Elvitegravir
● Ketoconazole
● Levoketoconazole
● Raltegravir
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
● Ciprofloxacin
● Delafloxacin
● Fleroxacin
● Gemifloxacin
● Grepafloxacin
● Moxifloxacin
● Norfloxacin
● Ofloxacin
● Sparfloxacin
● Trovafloxacin Mesylate
● Warfarin

Other Interactions
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
● Diabetes-Use with caution. May make this condition worse.
● Kidney disease (including patients with chronic kidney failure or those receiving dialysis)-Use with caution. The effects may be increased because of slower removal of the medicine from the body.
● Stomach and bowel disease-Sucralfate may bind with other foods and drugs which may cause blockage of the stomach and bowels.

Sucralfate CAS 54182-58-0 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 sucralfate forms an ulcer-adherent complex with proteinaceous exudate at the ulcer site.
● In vitro, a sucralfate-albumin film provides a barrier to diffusion of hydrogen ions.
● 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.

● Sucralfate may be used to treat stomach conditions, such as duodenal ulcers.

● The exact way sucralfate works is not known; however, research shows it forms a film with albumin (a protein) exuded from the ulcer site. This film acts as a barrier to gastric acid, pepsin (one of the main digestive enzymes), and bile salts.

● Sucralfate belongs to the class of medicines known as disaccharide sulfates. It is also known as a protectant anti-ulcer medicine.