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Indication for proton pump inhibitors
used to treat GERD, esophagitis, gastritis, active PUD, and Zollinger Ellison syndrome.
If a person has esophagitis and does not respond to H2RAs. What drugs have been also been effective in healing esophagitis.
PPIs. PPIs have show to be better than H2RAs for system relief and mucosal healing
PUD treated with PPI heals rapidly. But what frequently happens following this course?
Recurrence is frequent unless H. Pylori are unliminated.
Should PPIs be used in Treatment of NSAID related GI complications
PPIs reduce dyspepsia and have been shown to prevent endoscopically detected ulcers, but there is no compelling evidence to date that they prevent serious NSAID related GI complications.
Explain pharmacodynamics of Proton Pump Inhibitors?
PPIs produce a profound, long lasting suppression of gastric acid secretion (in greater than 90% pts) and thus are able to maintain the gastric PH above 4 , even during the acid surges that occur after eating.
Parent drug is inactive, but under the highly acidic conditions inside the parietal cell, it is converted to sulfonamide. The sulfonamide combines irreversible with the H+K+ATPase proton pump system that prevents hydrogen secretion into the gastric lumen. blocking final step in basal, nocturnal, and stimulated acid production. What is the name of this type of drugs?
Proton Pump Inhibitors
Why do PPIs have little action on other ion pumps in the body?
Sulfonamide does not readily cross biologic membranes, and because of the unique nature of the proton pump, PPIs have little action on other ion pumps in the body
The suppression of this substance results in decreased blood flow to the antrum, pyloris, and duodenal bulb? What other effects are noted with suppression of secretion of this?
Supression of gastric acid secretion.
Also Pepsin activity decreases, and serum pepsinogen levels increase.
regarding PPIs use
What happens in initial therapy using PPI to treat a gastric ulcer?
increase in nitrate producing bacteria and an elevation of nitrate concentrations in gastric juices. initial compensatory increases in serum gastrin levels, but no additional increase occurs with continued treatment, and there do not appear to be ill effects from this increase. Tolerance to the antisecretory effect has not been reported.
Pharmacokinetics of PPIs. How well are they absorbed? Routes of administration? 1/2 life? Biotransformed? Elimination?
well abobsorbed PO. Half life generally 1-2H. Duration of action longer and more varied. Biotransformed in liver to inactive metabolites that are eliminated primarily in the urine.