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Proton Pump Inhibitors Research Paper

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Proton Pump Inhibitors are all benzimidazole derivatives that control gastric acid secretion by inhibition of gastric H+,K+ -ATPase, the enzyme responsible for the final step in gastric acid secretion from the parietal cells. The PPIs are inactive pro drugs that are carried in the bloodstream to the parietal cells in the gastric mucosa. The pro drugs readily cross the parietal cell membrane in the cytosol. These drugs are weak bases and therefore have a high affinity for acidic environments. They diffuse across the secretory membrane on the parietal cell into the extracellular secretory canaliculus, the site of active proton pump. Under this acidic conditions the prodrugs are converted to their active form, which irreversibily binds the proton pump, inhibiting acid secretions. Since the’ active principles ‘ forms at a low pH it concentrates selectively in the acidic enviorment of the proton pump and results in extremely effective inhibition of acid secretion.The different PPIs(Omeprazole,Esomeprazole,Lanzoprazole, Pantoprazole and Rabeprazole ) bind to different sites on the proton pump, which may explain their differences in potency on a milligram per milligram basis. PPIs require an enteric coating to …show more content…

The apparent half-life is approximately 48h.This prolong duration of action allows once -daily dosing of PPIs, although twice- daily dosing is recommended in some cases of erosive oesophagitis or Barrett’s oesophagus when a sustained gastric pH of greater than 4.0 is required. All PPIs are most effective if taken about 30min before a meal as they inhibit only actively secreting proton pumps. Meals are the main stimulus to proton pump activity. The optimal dosing time is 30-60min before the first meal of the

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