Esomeprazole, What Is It For?

Esomeprazole belongs to a group of medicines called proton pump inhibitors, known by the acronym PPIs. The mechanism of action of these medications is to reduce the amount of acid that the stomach produces.

Proton pump inhibitors are probably the most prescribed drugs in the world. Esomeprazole is an S-isomer of omeprazole, whose safety profile is very favorable, since it has minimal and not very serious adverse effects.

Here we tell you everything you need to know when taking esomeprazole.

Mechanism of action of esomeprazole

Esomeprazole can be very helpful.

From a chemical point of view, esomeprazole is a weak base, which is concentrated and converted into its active form in the highly acidic environment of the secretory canaliculi of the parietal cell -located in the stomach-.

There it inhibits the enzyme H + K + -ATPase – the so-called proton pump – and therefore inhibits basal acid secretion and stimulated secretion.

When is treatment with esomeprazole indicated?

In adults, esomeprazole treatment is indicated for the treatment of:

  • Gastroesophageal reflux disease (GERD).
  • In combination with an antibacterial therapeutic regimen appropriate for the eradication of Helicobacter pylori.
  • Helicobacter pylori- associated duodenal ulcer healing .
  • Prevention of recurrence of peptic ulcers in patients with ulcers associated with Helicobacter pylori.
  • Healing of gastric ulcers associated with treatment with NSAIDs.

Also in case of:

  • Intravenous-induced peptic ulcer rebleeding prevention continuation therapy.
  • Patients who need continuous treatment with non-steroidal anti-inflammatory drugs  -NSAIDs-, which is a risk factor for the appearance of peptic ulcer.
  • Zollinger Ellison Syndrome Treatment. This is a rare condition in which one or more tumors form in the pancreas or duodenum. These tumors are called gastrinomas and they secrete large amounts of the hormone gastrin which causes our stomach to produce acid in an exaggerated way.

    In adolescents from 12 years of age, treatment with esomeprazole is indicated in case of:

    • Gastroesophageal reflux disease (GERD).
    • In combination with antibiotics in the treatment of duodenal ulcer caused by Helicobacter pylori.

    Dosage and method of administration

    The dosage of esomeprazole depends on the type of condition, although it is usually administered in tablets at a dose of 20 or 40 milligrams, depending on the doctor’s prescription.

    The tablets should be swallowed whole with the help of liquid, without being chewed or crushed. For patients with swallowing difficulties, the tablets can also be dispersed in half a glass of still water. Other liquids should not be used, since the enteric coating that prevents its disintegration in the gastric environment could dissolve.

    For patients who cannot swallow, the tablets can be dispersed in still water and administered through a gastric tube. The intravenous route can also be evaluated if necessary.

    Most common adverse effects

    The most commonly reported adverse reactions are the following:

    • Headache.
    • Dyspepsia.
    • Abdominal pain.
    • Diarrhea and nausea.
    • Rash  or skin rash.

    The safety profile is similar for different formulations, treatment indications, age groups and patient populations. To date, no dose-related adverse reactions have been identified.

    Interactions with other medications

    Esomeprazole cannot be combined with some medications.

    Drug-drug interactions can occur by various mechanisms: either by poor drug absorption due to changes in gastric pH, or by competition for cytochrome P450 enzymes.

    The most significant interactions of esomeprazole with other medications are as follows:

    • Atazinavir.
    • Warfarin
    • Clopidogrel.
    • Cyclosporine.
    • Acenocoumarol.
    • Carbamazepine.
    • Antifungal agents.

    Contraindications

    The main contraindication to the administration of this drug is hypersensitivity to the active principle, to benzimidazoles or to the excipients it contains, for example sucrose.

    The concomitant administration of esomeprazole with atazanavir -antiretroviral used in the prevention and treatment of HIV- is not recommended.

    If deemed necessary, close clinical monitoring along with an increase in the atazanavir dose to 400 milligrams with 100 milligrams ritonavir would be recommended. However, it would not be indicated to exceed the dose of 20 milligrams of esomeprazole.

    Responsible use of proton pump inhibitors

    As we have said, esomeprazole belongs to the group of most widely used drugs in the world. Although we have already seen that it is a very safe drug with very mild adverse effects, they tend to be considered simple “gastric protectors without collateral effects”  and to be administered without a prescription.

    This fact may lead to the erroneous use of esomeprazole for the treatment of symptoms that are not associated with gastric hypersecretion, which is its main indication.

    According to some studies, prolonged and inappropriate use of esomeprazole could lead to :

    • Hypomagnesemia.
    • Increased risk of bone fracture.
    • Increased risk of infection.
    • Poor absorption of vitamins.
    • Complications in risk or polymedicated patients.

    However, esomeprazole is a highly safe and effective drug for the treatment of gastric hypersecretion.

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