Esomeprazole

Drug Class: Proton-pump inhibitors

Mode of Action

• Esomeprazole magnesium reduces gastric acid secretion by inhibiting gastric enzyme H+, K+-ATPase (the proton pump) which is responsible for acid secretion by the parietal cells of the stomach.

Pharmacokinetics

• Absorption of esomeprazole in healthy subjects results in peak plasma levels occurring 1 to 2 hours after dosing. 

• The systemic bioavailability is 64% after a single 40 mg dose and 89% after repeated once daily oral administration. 

• Esomeprazole is 97% protein bound and optically stable in vivo, with negligible inversion to the other isomer.

Pharmacodynamics

• Absorption of esomeprazole in healthy subjects results in peak plasma levels occurring 1 to 2 hours after dosing. 

• The systemic bioavailability is 64% after a single 40 mg dose and 89% after repeated once daily oral administration. 

• The apparent volume of distribution at a steady state in healthy subjects is around 0.22 L/kg body weight.

Contraindication

• Esomeprazole magnesium is contraindicated in patients with known hypersensitivity to substituted benzimidazoles or any component of the formulation. 

• Hypersensitivity reactions may include anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute interstitial nephritis, and urticaria.

Better compared to other PPI

• Esomeprazole 40 mg provides more effective acid control than omeprazole in patients with symptoms of gastroesophageal reflux disease.