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.