Gastroprotective agents
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Gastroprotective Agents: Types and Mechanisms
Gastroprotective agents are medications used to prevent or treat damage to the stomach lining, especially in patients at risk of ulcers or gastrointestinal (GI) bleeding. The main types include proton pump inhibitors (PPIs), histamine-2 receptor antagonists (H2RAs), prostaglandin analogues, and mucoprotective agents such as misoprostol, rebamipide, and sucralfate. These agents work by reducing gastric acid secretion, enhancing mucosal defense, or forming protective barriers over the stomach lining 12479.
Effectiveness in Preventing NSAID-Related GI Injury
Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used for pain and inflammation but are known to cause GI side effects, including ulcers and bleeding. Co-prescription of gastroprotective agents with NSAIDs is common practice to reduce these risks. Studies consistently show that PPIs and H2RAs significantly lower the risk of GI injury and bleeding in NSAID users, with PPIs generally providing the greatest protection. Mucoprotective agents like misoprostol and rebamipide also offer some benefit, though to a lesser extent than PPIs 1246810.
Use in Elderly and High-Risk Populations
Elderly patients are at higher risk for NSAID-induced GI complications. Guidelines recommend routine use of gastroprotective agents in this group. However, real-world data show that only a minority of elderly patients receive appropriate gastroprotection. When used, these agents are effective in reducing GI events, but more consistent prescribing is needed to maximize benefits in this vulnerable population 618.
Gastroprotection Beyond NSAIDs: Anticoagulants and Other Drugs
Gastroprotective agents are also important for patients taking other medications that increase GI bleeding risk, such as dabigatran (a blood thinner) and antiplatelet drugs. Studies show that PPIs and H2RAs reduce the risk of upper GI bleeding in patients on dabigatran, especially those with a history of ulcers or GI bleeding 310. Full adherence to PPI therapy is crucial for effective protection in these settings .
Mechanisms of Action: Prostaglandins, Mucosal Defense, and Novel Agents
Prostaglandins play a key role in mucosal defense by increasing mucus and bicarbonate secretion and maintaining blood flow. Some gastroprotective agents, such as misoprostol, act as prostaglandin analogues. Other agents, like sucralfate and sofalcone, protect the stomach lining through different mechanisms, including binding growth factors and scavenging free radicals. Recent research highlights the potential of natural compounds, such as xanthones, which may protect the stomach by modulating antioxidant pathways 579.
Prescribing Patterns and Rational Use
Studies of prescribing patterns show that PPIs are the most commonly used gastroprotective agents, often at appropriate doses. However, some H2RAs are prescribed at suboptimal doses or for indications other than GI protection. There is also evidence of overuse in low-risk patients and underuse in high-risk groups, highlighting the need for rational prescribing to optimize patient outcomes and reduce unnecessary healthcare costs 18.
Conclusion
Gastroprotective agents, especially PPIs, are effective in preventing and treating GI injury caused by NSAIDs, anticoagulants, and other risk factors. Their use is particularly important in elderly and high-risk patients. While current agents are effective, ongoing research into new compounds and a better understanding of underlying mechanisms may further improve gastroprotection in the future. Rational and consistent use of these agents is essential to maximize benefits and minimize risks.
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