Esmoprazole acts by inhibiting
Correct Answer: H+K+ ATPase pump
Description: Ans. a (H+K+ ATPase pump). (Ref. Harrison's internal medicine, 16th ed., 1753)Esmoprazole# s-enantiomer of omeprazole.# It is claimed to produce better control of pH in stomach than omeprazole in GERD.# It is effective as Omez in healing gastric/duodenal ulcer and in inhibiting H. pylori.# Side effects and drug reactions are same as Omez.Rabeprazole,A newer PPI causing fastest acid suppression and aids ingastric mucin synthesis.PantoprazoleMore acid stable and active at high pH and drug interactions are minimal.LansoprazoleReversible inhibitor. Proton Pump (H+,K+-ATPase) Inhibitors# Omeprazole, esmoprazole, lansoprazole, rabeprazole, and pantoprazole are substituted benzimidazole derivatives that covalently bind and irreversibly inhibit H+,K+-ATPase.# Esmoprazole, the newest member of this drug class, is the S-enantiomer of omeprazole.# These are the most potent acid inhibitory agents available.# Omeprazole and lansoprazole are the PPIs that have been used for the longest time. Both are acid-labile and are administered as enteric-coated granules in a sustained-release capsule that dissolves within the small intestine at a pH of 6. These agents are lipophilic compounds; upon entering the parietal cell, they are protonated and trapped within the acid environment of the tubulovesicular and canalicular system. These agents potently inhibit all phases of gastric acid secretion. Onset of action is rapid, with a maximum acid inhibitory effect between 2 and 6 h after administration and duration of inhibition lasting up to 72-96 h. With repeated daily dosing, progressive acid inhibitory effects are observed, with basal and secretagogue-stimulated acid production being inhibited by >95% after 1 week of therapy# The half-life of PPIs is --18 h; thus, it can take between 2 and 5 days for gastric acid secretion to return to normal levels once these drugs have been discontinued.# PPIs may interfere with absorption of drugs such as ketoconazole, ampicillin, iron, and digoxin. Hepatic cytochrome P450 can be inhibited by the earlier PPIs (omeprazole, lansoprazole). Rabeprazole, pantoprazole, and esmoprazole do not appear to interact significantly with drugs metabolized by the cytochrome P450 system. Caution should be taken when using warfarin, diazepam, atazanavir, and phenytoin concomitantly with PPIs. Long-term acid suppression, especially with PPIs, has been associated with a higher incidence of community-acquired pneumonia.# Tenatoprazole is a PPI containing an imidazopyridine ring instead of a benzimidazole ring, which promotes irreversible proton pump inhibition. This agent has a longer half-life than the other PPIs and may be beneficial for inhibiting nocturnal acid secretion, which has significant relevance in GERD. A second new class of agents is the potassium- competitive acid pump antagonists (P-CABs). These compounds inhibit gastric acid secretion via potassium competitive binding of the H+,K+-ATPase.
Category:
Pharmacology
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