Small molecule
PubChem CID 9568614
Esomeprazole
Nexium
- Mechanism of action
- Proton pump (H+/K+ ATPase) inhibitor
- In plain language
- Shuts down the stomach's acid-producing pumps at the source, cutting acid output more completely than drugs that just block one trigger for acid release.
- How it works
- Esomeprazole, the S-isomer of omeprazole, is a substituted benzimidazole that irreversibly inhibits the H+/K+-ATPase (proton pump) at the secretory surface of the gastric parietal cell. It is a prodrug that accumulates in the acidic canaliculi of the parietal cell, where it is protonated and converted to its active form, which covalently binds cysteine residues on the proton pump. Because this is the terminal step in acid secretion, esomeprazole suppresses both basal and stimulated gastric acid output regardless of the stimulating agent. Acid suppression requires synthesis of new pump protein to restore secretory activity, giving the drug a longer duration of action than its short plasma half-life would suggest.
- Therapeutic applications
- Indicated for short-term treatment in the healing of erosive esophagitis and maintenance of that healing, short-term treatment of heartburn and other symptoms associated with GERD, risk reduction of NSAID-associated gastric ulcer, Helicobacter pylori eradication in combination with antibiotics, and long-term treatment of pathological hypersecretory conditions including Zollinger-Ellison syndrome.
- Class
- Small molecule
- Therapeutic area
- Gastrointestinal
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