Proton pump inhibitors are common clinical drugs that are effective in treating acid-related diseases. They work by reducing the amount of acid produced by gastric glands in the mucous membrane in the stomach. The gastric proton pump resides in this gastric mucosa at the apical pole of the parietal cells. Under normal circumstances, approximately three liters of stomach acid is produced in a day under the regulation of the parasympathetic nervous system. The principle stimulant of acid secretion by the gastric proton pump is food intake, which acts by releasing gastrin. Once the gastrin has been released, the protein kinases activate, via the cAMP, and ultimately the H+/K+-ATPase, or gastric proton pump, is activated and acid is secreted.
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Once the protons have crossed the membrane, they are secreted into the gastric fluid, which eventually becomes stomach acid. In moderation, stomach acid is a valuable contributor to aid in the process in digestion. However, when stomach acid is overproduced, it can irritate the esophagus and cause Gastroesophageal Reflux Disease or initiate the development of ulcers in the stomach and duodenum. Through regular use of proton pump inhibitors, acid reflux into the esophagus is reduced and associated symptoms are alleviated over time. While effective, a number of side effects have been associated with proton pump inhibitor use.
Proton pump inhibitors are initially absorbed via the small intestine and then distributed to gastric parietal cells. They are activated in the acidic environment of the parietal cell’s vesicles and secretory canaliculi (Suzuki). Proton pump inhibitors require profound acidity (a pH level less than 1 is ideal) in order to be effective. Parietal cells are one of the only sites in the human body that can uphold this pH, therefore proton pump inhibitors are only actively beneficial in the …show more content…
Proton pump inhibitors are considered acid-activated prodrugs because they discontinue acid production and ATPase activity. They require gastric acid secretion to be converted to sulfenic acid, which covalently bonds with the cysteines on the surface of ATPase (Shin). The sulfenic bond is responsible for stopping the acid secretion once it has successfully bonded with the ATPase of parietal cells, which raises the pH of the stomach acid. Acid-related diseases, such as peptic ulcers and gastroesophageal reflux disease, are then able to heal once the intragastric pH is greater than 4. About 93.7%-94.1% of patients find that their acid-related diseases heal within eight weeks
Once the protons have crossed the membrane, they are secreted into the gastric fluid, which eventually becomes stomach acid. In moderation, stomach acid is a valuable contributor to aid in the process in digestion. However, when stomach acid is overproduced, it can irritate the esophagus and cause Gastroesophageal Reflux Disease or initiate the development of ulcers in the stomach and duodenum. Through regular use of proton pump inhibitors, acid reflux into the esophagus is reduced and associated symptoms are alleviated over time. While effective, a number of side effects have been associated with proton pump inhibitor use.
Proton pump inhibitors are initially absorbed via the small intestine and then distributed to gastric parietal cells. They are activated in the acidic environment of the parietal cell’s vesicles and secretory canaliculi (Suzuki). Proton pump inhibitors require profound acidity (a pH level less than 1 is ideal) in order to be effective. Parietal cells are one of the only sites in the human body that can uphold this pH, therefore proton pump inhibitors are only actively beneficial in the …show more content…
Proton pump inhibitors are considered acid-activated prodrugs because they discontinue acid production and ATPase activity. They require gastric acid secretion to be converted to sulfenic acid, which covalently bonds with the cysteines on the surface of ATPase (Shin). The sulfenic bond is responsible for stopping the acid secretion once it has successfully bonded with the ATPase of parietal cells, which raises the pH of the stomach acid. Acid-related diseases, such as peptic ulcers and gastroesophageal reflux disease, are then able to heal once the intragastric pH is greater than 4. About 93.7%-94.1% of patients find that their acid-related diseases heal within eight weeks