From the Guidelines
Carafate (sucralfate) works by forming a protective barrier over ulcers and damaged tissue in the gastrointestinal tract, allowing natural healing processes to occur. When taken orally, sucralfate reacts with stomach acid to form a sticky, paste-like substance that adheres specifically to ulcer sites and areas of inflammation. This protective coating physically shields the damaged tissue from further injury by stomach acid, pepsin, and bile salts. Additionally, sucralfate binds to growth factors and keeps them at the ulcer site, which promotes tissue repair. It also adsorbs pepsin and bile acids, reducing their damaging effects. Some key points to consider when using sucralfate include:
- Minimal systemic absorption (less than 5%), making it a local-acting medication with few systemic side effects 1
- The standard dosage is typically 1 gram taken four times daily on an empty stomach, at least 1 hour before meals and at bedtime
- For maximum effectiveness, patients should take it consistently as prescribed, usually for 4-8 weeks for ulcer treatment
- Patients should be aware that sucralfate may decrease the absorption of certain medications, so it should be taken at least 2 hours apart from other drugs. It's also worth noting that while sucralfate has been used for stress bleeding prophylaxis, its effectiveness compared to other agents such as H2 blockers is still a topic of debate, with some studies suggesting that sucralfate may be associated with a lower risk of certain complications, such as ventilator-associated pneumonia 1.
From the FDA Drug Label
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.
The mechanism of action of Carafate (sucralfate) is through local action, where it forms an ulcer-adherent complex that protects the ulcer site from further attack by acid, pepsin, and bile salts. Key points include:
- Inhibition of pepsin activity in gastric juice
- Barrier to diffusion of hydrogen ions
- Adsorption of bile salts 2
From the Research
Mechanism of Action of Carafate (Sucralfate)
The mechanism of action of Carafate (sucralfate) involves several key processes:
- Binding to defective mucosa, forming a protective barrier at the ulcer site 3
- Neutralizing local acidity without affecting gastric pH 4
- Inhibiting the diffusion of hydrogen ions and the action of pepsin 4, 3
- Adsorbing bile salts 4, 3
- Enhancing the natural defensive mechanisms of the gastric mucosa, stimulating mucus, bicarbonate, and prostaglandin release, and mucosal cell renewal 5
- Having a trophic effect on the entire mucosa, facilitating healing and re-epithelialization 5
Key Properties of Sucralfate
Some key properties of sucralfate include:
- Minimal absorption after oral administration, with approximately 3-5% of the dose being absorbed 4
- Formation of a protective barrier at the ulcer site, reducing pepsin and H+ injury 5
- Binding of pepsin and bile acids, preventing their damaging effects on the mucosa 4, 3
- Stimulation of mucosal cell renewal and enhancement of defensive capabilities of the mucosa 5
Therapeutic Effects of Sucralfate
The therapeutic effects of sucralfate include: