Esomeprazole is a specific inhibitor of the gastric enzyme

By | February 27, 2017

Nexium (Esomeprazole) magnesium (a substituted benzimidazole), reduces gastric acid secretion through a highly targeted mechanism of action. It is a specific inhibitor of the gastric enzyme H+, K+-ATPase (the proton pump) which is responsible for acid secretion by the parietal cells of the stomach.

Mechanism of action:

Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of 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. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.

Indications:

Esomeprazole magnesium trihydrate tablets are indicated for treatment of circumstances where a reduction of gastric acid secretion is essential such as: reflux esophagitis, maintenance treatment of patients with reflux esophagitis, symptomatic gastroesophageal reflux disease (i.e. heartburn and regurgitation), and H. pylori eradication.

Side effects:

* dizziness, confusion;
* fast or uneven heart rate;
* jerking muscle movements;
* jittery feeling;
* muscle cramps, muscle weakness or limp feeling;
* cough or choking feeling; or
* Seizure (convulsions).

Contraindications:

* It is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted benzimidazoles
* Symptomatic response to therapy does not rule out the presence of gastric malignancy
* Atrophic gastritis has occasionally been noted with long-term therapy with omeprazole
* PPI therapy may be associated with increased risk of Clostridium difficile-associated diarrhea
* Avoid concomitant use of this product with clopidogrel, due to a reduction in plasma concentrations of the active metabolite of clopidogrel. When using this drug consider alternative anti-platelet therapy
* Long-term and multiple daily dose proton pump inhibitor (PPI) therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine
* Hypomagnesemia has been reported rarely with prolonged treatment with PPI therapy and may require discontinuing PPI therapy
* Concomitant use of this product and St. John’s wort or rifampin can substantially decrease NEXIUM concentrations. Avoid concomitant use

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Precautions:

Esomeprazole may increase the risk for bone fractures, especially with longer use, higher doses, and in older adults. To prevent bone loss/fracture, by taking such as calcium (such as calcium citrate) and vitamin D supplements.
During pregnancy, this medication should be used only when clearly needed.

DOSING:

* For GERD, 20 or 40 mg of esomeprazole is given once daily for 4-8 weeks. In children ages 1-11, the dose is 10 or 20 mg daily.
* For the treatment of H. pylori, 40 mg is administered once daily in combination with amoxicillin and clarithromycin for 10 days.

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