Drug gastric protection
Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used for acute and long-term treatment of painful and inflammatory conditions. Active ingredients used include, for example, diclofenac, acetylsalicylic acid, ibuprofen, naproxen, and mefenamic acid. However, their use is limited by adverse effects that affect the upper digestive tract and are due to inhibition of prostaglandin synthesis. A relevant proportion of patients develop gastric or intestinal ulceration during chronic use, which can lead to bleeding and perforation. This results in hospitalizations and deaths. Known risk factors for complications include:
- History of gastric or intestinal ulceration in the patient.
- Age > 65 years
- High dose of NSAIDs
- Concomitant administration of glucocorticoids, anticoagulants, or other NSAIDs including acetylsalicylic acid 100 mg (aspirin cardio)
- Infection with Helicobacter pylori
For prevention, painkillers are combined with a so-called drug “stomach protection” in patients at risk. These are drugs that primarily reduce the formation of aggressive gastric acid. These include proton pump inhibitors, H2 antihistamines and misoprostol. Today, proton pump inhibitors (PPIs) such as pantoprazole and omeprazole are mainly used because misoprostol often causes diarrhea and cramps, and the H2 antihistamines are considered less effective. Clinical trials have documented that PPIs are able to reduce the risk of developing a gastric or intestinal ulcer to a significant degree. A new trend is the fixed combination of NSAIDs and gastric protection in a single tablet. In May 2011, a combination of naproxen and esomeprazole (Vimovo, AstraZeneca AG) was approved in many countries. One potential advantage is the improved adherence to therapy. A disadvantage, on the other hand, is the low flexibility in dosing and choice of active ingredients. Naproxen is included in the combination because it is thought to have a better cardiovascular side effect profile than other NSAIDs. The combination acetylsalicylic acid and esomeprazole (Axanum) was registered in 2012. According to their individual risk, patients can be divided into groups for which defined recommendations apply (e.g., Lanza et al., 2009). COX-2 inhibitors such as celecoxib and etoricoxib represent an alternative for gastric protection. However, the increased cardiovascular risk must be considered with this group of drugs. COX-2 inhibitors are also combined with PPIs to further reduce the adverse event rate. In summary, before treatment with a nonsteroidal anti-inflammatory drug, an individual risk assessment must take place and therapy must be tailored accordingly.
