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QuickView for esomeprazole (compound)

Name: Esomeprazole
Name (isomeric): DB00736
Drug Type: small molecule
Description: The S-isomer of omeprazole
Esomperazole; Esomeprazole Sodium
Brand: Nexium IV, Nexium, Lucen, Esopral, Nexiam, Axagon
Category: Antihistamines, Anti-Ulcer Agents, Enzyme Inhibitors, Proton-pump Inhibitors
CAS number: 161796-78-7
Indication: For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use.
Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazo...
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Mechanism of Action: Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
Absorption: 90%
Protein binding: 97%
Biotransformation: Mainly hepatic. Esomeprazole is completely metabolized by the cytochrome P450 system via CYP2C19 and CYP3A4. Metabolism produces inactive hydroxy and desmethyl metabolites, which have no effect on gastric acid secretion. Less than 1% of the parent drug is excreted in urine.
Route of elimination: Approximately 80% of the administered dose of esomeprazole is excreted as metabolites in urine and the remaining 20% is excreted in feces.
Half Life: 1-1.5 hours
Toxicity: Blurred vision, confusion, drowsiness, dry mouth, flushing headache, nausea, rapid heartbeat, sweating
Affected organisms: Humans and other mammals
Food interaction:
Take without regard to meals.
Drug interaction:
TipranavirTipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Esomeprazole. Consider alternate therapy or increase the dose of Esomeprazole based on the therapeutic response.
IndinavirOmeprazole decreases the absorption of indinavir
AtazanavirThis gastric pH modifier decreases the levels/effects of atazanavir
EnoxacinEsomeprazole may decrease the absorption of enoxacin.
CefditorenProton pump inhibitors such as esomeprazole may decrease the serum concentration of cefditoren. If possible, avoid use of cefditoren with proton pump inhibitors (PPIs). Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of PPIs can not be avoided.
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