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(Introduction)
(Introduction)
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== Introduction ==
== Introduction ==
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'''Esomeprazole''' is a Proton Pump Inhibitor (PPI) that binds to H+/K+-ATPase and inhibits the secretion of gastric acid from the parietal cells into the lumen of the stomach. The H+/K+-ATPase pump, located within the cytoplasmic membrane of resting parietal cells, gets translocated upon activation to the canalicular membrane and pumps cytoplasmic H+ into the canalicular space, in exchange for extracellular K+ ions. It is a pro-drug that is protonated twice in the acidic environment of the parietal cell to form the active inhibitor, sulfenamide which forms disulfide bonds with Cys 813 and Cys 892 on the α subunit of the H+/K+-ATPase. Esomeprazole inhibits the final step in the secretion of gastric acid.
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'''Esomeprazole''' is a Proton Pump Inhibitor (PPI) that binds to H+/K+-ATPase and inhibits the secretion of gastric acid from the parietal cells into the lumen of the stomach. Esomeprazole’s commercial brand name, Nexium, is used to treat Gastro-esophageal Reflux Disease (GERD), peptic and gastric ulcers, and Zollinger-Ellison syndrome. Ulcers caused by the bacterium ''Helicobacter pylori'' can be treated using Esomeprazole in conjunction with proper antibiotics.1 These result in gastric acid accumulation into the lumen of the stomach from the parietal cells.2 Gastric acid is released through the H+/K+-ATPase pump, which is the final step in acid release.2 Esomeprazole is an irreversible inhibitor of the pump.2
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The H+/K+-ATPase pump, located within the cytoplasmic membrane of resting parietal cells, gets translocated upon activation to the canalicular membrane and pumps cytoplasmic H+ into the canalicular space, in exchange for extracellular K+ ions. It is a pro-drug that is protonated twice in the acidic environment of the parietal cell to form the active inhibitor, sulfenamide which forms disulfide bonds with Cys 813 and Cys 892 on the α subunit of the H+/K+-ATPase. Esomeprazole inhibits the final step in the secretion of gastric acid.
[[Image:2xzb bio r 250.jpg|300px|left|thumb| Pig Gastric H,K-ATPase with bound BeF and SCH28080]]
[[Image:2xzb bio r 250.jpg|300px|left|thumb| Pig Gastric H,K-ATPase with bound BeF and SCH28080]]
[[Image:Esomeprazole2d.png|300px|left|thumb| Esomeprazole 2D Structure]]
[[Image:Esomeprazole2d.png|300px|left|thumb| Esomeprazole 2D Structure]]

Revision as of 16:35, 4 December 2013

Introduction

Esomeprazole is a Proton Pump Inhibitor (PPI) that binds to H+/K+-ATPase and inhibits the secretion of gastric acid from the parietal cells into the lumen of the stomach. Esomeprazole’s commercial brand name, Nexium, is used to treat Gastro-esophageal Reflux Disease (GERD), peptic and gastric ulcers, and Zollinger-Ellison syndrome. Ulcers caused by the bacterium Helicobacter pylori can be treated using Esomeprazole in conjunction with proper antibiotics.1 These result in gastric acid accumulation into the lumen of the stomach from the parietal cells.2 Gastric acid is released through the H+/K+-ATPase pump, which is the final step in acid release.2 Esomeprazole is an irreversible inhibitor of the pump.2 The H+/K+-ATPase pump, located within the cytoplasmic membrane of resting parietal cells, gets translocated upon activation to the canalicular membrane and pumps cytoplasmic H+ into the canalicular space, in exchange for extracellular K+ ions. It is a pro-drug that is protonated twice in the acidic environment of the parietal cell to form the active inhibitor, sulfenamide which forms disulfide bonds with Cys 813 and Cys 892 on the α subunit of the H+/K+-ATPase. Esomeprazole inhibits the final step in the secretion of gastric acid.

Image:2xzb bio r 250.jpg
Pig Gastric H,K-ATPase with bound BeF and SCH28080
Image:Esomeprazole2d.png
Esomeprazole 2D Structure

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Deepa Patel

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