PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
esomeprazole

2D structure

Overview

Generic Names: Esomeprazole Sodium; Esomperazole; esomeprazole
Trade Names: Axagon; Esopral; Lucen; Nexiam; Nexium; Nexium IV
PharmGKB Accession Id: PA10075

Description

A highly effective inhibitor of gastric acid secretion used in the therapy of stomach ulcers and zollinger-ellison syndrome. The drug inhibits the H()-K()-ATPase (H()-K()-exchanging ATPase) in the proton pump of gastric parietal cells. PubChem (source: Drug Bank)

Indication

For the treatment of acid-reflux disorders (GERD) and peptic ulcer disease (source: Drug Bank)

ATC Therapeutic Category

  • A02BC:Proton pump inhibitors

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H<sup>+</sup>/K<sup>+</sup>-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. (source: Drug Bank)

Pharmacology

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 <i>H. pylori</i> eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H<sup>+</sup>/K<sup>+</sup> ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, Esomeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. (source: Drug Bank)

Food Interactions

Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

97% (source: Drug Bank)

Absorption

90% (source: Drug Bank)

Toxicity

Blurred vision, confusion, drowsiness, dry mouthflushingheadache, nausea, rapid heartbeat, sweating (source: Drug Bank)

Isomeric SMILES Code:

Cc1cnc(c(c1OC)C)C[S@](=O)c2[nH]c3ccc(cc3n2)OC (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs4986893 at chr10:96530400 in CYP2C19
    In contrast to other PPIs, esomeprazole-induced healing of GERD appears to be unrelated to the CYP2C19*3 variant.
    Variant Name:
    CYP2C19*3
    Related Drugs:
    esomeprazole
    Related Diseases:
    Gastroesophageal Reflux
    Evidence:
    PMID:16338278
  2. rs4244285 at chr10:96531606 in CYP2C19
    In contrast to other PPIs, esomeprazole-induced healing of GERD appears to be unrelated to the CYP2C19*2 variant.
    Variant Name:
    CYP2C19*2
    Related Drugs:
    esomeprazole
    Related Diseases:
    Gastroesophageal Reflux
    Evidence:
    PMID:16338278
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ATP4A
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ATP4B
  •   
  • PD
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
  • CO
  • PD
  • PK
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ATP4A Uncurated Annotation (source: Drug Bank)
ATP12A Uncurated Annotation (source: Drug Bank)
ATP1A1 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
atazanavir Uncurated Annotation This gastric pH modifier decreases the levels/effects of atazanavir (source: Drug Bank)
enoxacin Uncurated Annotation The agent decreases the absorption of enoxacin (source: Drug Bank)
indinavir Uncurated Annotation Omeprazole decreases the absorption of indinavir (source: Drug Bank)
itraconazole Uncurated Annotation The proton pump inhibitor decreases the absorption of imidazole (source: Drug Bank)
ketoconazole Uncurated Annotation The proton pump inhibitor decreases the absorption of imidazole (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Gastroesophageal Reflux
  • CO
  • PD
  • PK
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Peptic Ulcer
  • CO
  • PD
  • PK
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00736
KEGG Drug ID:
D01984
PubChem Compound ID:
4594
PubChem Substance ID:
3865629

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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