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Proton pump inhibitors – new mole-cules, new knowledge


Authors: J. Špičák
Authors‘ workplace: Klinika hepatogastroenterologie ;  Přednosta: prof. MUDr. Julius Špičák, CSc. ;  Institut klinické a experimentální medicíny, Praha
Published in: Prakt. Lék. 2013; 93(5): 207-216
Category: Reviews

Overview

Proton pump inhibitors are the most important drugs in the treatment of acid-related diseases. All proton pump inhibitors are weak bases selectively metabolized in an acid environment and blocking active proton pump function. Proton pump inhibitors provide effective treatment of gastroesophageal reflux disease, Helicobacter pylori eradication, functional dyspepsia, and NSAID-associated gastropathy. First-generation proton pump inhibitors include omeprazole, pantoprazole, and lansoprazole, with second-generation ones represented by esomeprazole and rabeprazole. While proton pump inhibitors differ in their pharmacokinetic properties, these differences do not necessarily have clinically relevant sequels. Generally, second-generation proton pump inhibitors provide a faster onset of effect, longer gastric secretion inhibition and, specifically, the effect of rabeprazole is less dependent on the route of administration and has a smaller effect on cytochrome P450 function. The effect of proton pump inhibitors, especially the first-generation ones, is modified by genetic variability of the CYP2C19 enzyme being significantly lower with rapid metabolizers. Proton pump inhibitors are very safe and immediate complications are exceptional. They can cause progression of gastritis in Helicobacter infection. Despite hypergastrinemia, they do not have a malignant potential. Their long-term use is associated with an increased risk of pelvic and hip fractures, community-acquired pneumonia, and clostridium infection. Proton pump inhibitors may reduce the effect of antiplatelet therapy with clopidogrel thus increasing the risk of recurrent cardiovascular events. Package leaflets for patients are generally not well structured and often lack important information.

Keywords:
proton pump inhibitors (PPI) – H2 receptor antagonists (H2RA) – physiology – equipotent doses – oesophageal reflux disease – Helicobacter pylori eradication – NSAID gastropathy – complications – interactions


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