Esomeprazole

The drug Esomeprazole belongs to the category of proton pump inhibitor drugs - this is a wide range of medications that are used in the treatment of duodenal ulcers and gastroesophageal reflux pathology.

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Indications Esomeprazole

Esomeprazole is indicated:

• as an antisecretory drug;
• for gastroesophageal reflux pathology in individuals with complicated reflux or esophagitis;
• for gastric ulcer caused by taking non-steroidal anti-inflammatory drugs;
• to prevent the development of peptic ulcer and duodenal ulcer during treatment with non-steroidal anti-inflammatory drugs;
• for short-term maintenance of hemostasis and prevention of recurrent bleeding in patients after endoscopic therapy of acute bleeding ulcer.

Release form

Esomeprazole is produced as a lyophilisate for the preparation of an injection solution.

One vial with lyophilisate contains the active ingredient of the drug - sodium esomeprazole, in an alternative to esomeprazole amount of 40 mg.

The cardboard packaging contains one glass bottle with a rubber stopper and a rolled-up aluminum lid with a flip-opening device.

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Pharmacodynamics

Esomeprazole is the s-isomer of omeprazole, which reduces gastric acid production. It is a specific proton pump inhibitor with targeted pharmacodynamic activity.

The active ingredient of the drug Esomeprazole belongs to weak bases - the substance accumulates and is activated in the acidic environment of the excretory ducts of the parietal cellular structures, where inhibition of the enzyme H+K+ATPase - the acid pump, as well as inhibition of acid production occurs.

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Pharmacokinetics

The drug is absorbed quickly, reaching high concentrations within half an hour after taking the dose. Complete bioavailability can be 90%. Plasma protein binding is 95%.

Concomitant use of food reduces absorption and slows down the assimilation of Esomeprazole.

The drug is metabolized by the cytochrome P450 system. A large percentage of metabolism is dependent on CYP3A4, which is responsible for the formation of esomeprazole sulfone, the main plasma metabolite.

The half-life is 60-90 minutes. The plasma concentration-time relationship increases with repeated administration of the drug. This increase is dose-dependent and results in a non-linear relationship with repeated administration.

This time dependence is due to a decrease in first-pass metabolic processes, as well as systemic clearance rates due to inhibition of the CYP2C19 enzyme.

The active substance is completely eliminated from the bloodstream in the period between doses, without accumulation, with daily administration of Esomeprazole once a day.

The presence of the main metabolic products does not show any effect on the production of gastric juice. Approximately 80% of the taken amount of the drug leaves the body with urine, and the rest - with feces.

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Dosing and administration

Persons who are contraindicated for internal use of the drug may be prescribed parenteral administration in an amount of 20 to 40 mg daily. For reflux esophagitis, 40 mg of Esomeprazole is taken per day. For symptomatic therapy of gastroesophageal reflux disease, 20 mg of the drug is prescribed daily.

For gastric and duodenal ulcers caused by taking nonsteroidal anti-inflammatory drugs, a standard dosage of 20 mg daily is prescribed. For preventive purposes, the amount of the drug is not changed.

The duration of the therapy period with Esomeprazole is determined by the doctor and is not long-term.

After endoscopic stopping of gastric bleeding, 80 mg of Esomeprazole is used as a half-hour infusion, after which a prolonged (72 hours) intravenous infusion of 8 mg per hour is expected.

After parenteral administration of the drug, agents are prescribed that inhibit the secretion of acid by the stomach - in particular, tablets based on esomeprazole.

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Use Esomeprazole during pregnancy

The drug Esomeprazole is not prescribed to pregnant and lactating patients, since there is no reliable clinical information regarding the safety of the proposed drug for the fetus and newborn baby.

Contraindications

Esomeprazole is contraindicated:

• in case of hypersensitivity reactions to the ingredients of the drug;
• in combination with Nelphigavir or Atazanavir;
• pediatric patients (under 18 years of age);
• during pregnancy;
• during breastfeeding.

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Side effects Esomeprazole

Esomeprazole therapy may be accompanied by:

• decreased levels of leukocytes and platelets in the blood;
• allergies, including anaphylaxis;
• swelling of the extremities;
• sleep disturbance;
• depression, disorders of consciousness;
• headaches, fatigue;
• visual and hearing impairment;
• dizziness;
• signs of bronchospasm;
• dyspepsia, abdominal pain;
• thirst;
• jaundice, hepatitis;
• dermatitis, skin rashes, zonular alopecia;
• pain in joints and muscles;
• increased sweating.

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Overdose

Little information is available on Esomeprazole overdose. Signs of overdose may correspond to side effects and occur after oral administration of more than 280 mg of the drug.

No specific antidote has been established.

Hemodialysis is considered to be ineffective, and for this reason, in case of excessive dosing, doctors limit themselves to symptomatic and supportive therapeutic measures.

Interactions with other drugs

Reduced gastric acidity when taking Esomeprazole may affect the absorption of drugs if their absorption processes depend on the degree of acidity. It has been noted that taking other drugs that inhibit acid production, as well as antacids, provokes a decrease in the absorption of Ketoconazole or Itraconazole during therapy with Esomeprazole.

Esomeprazole in combination with drugs that metabolize CYP2C19 (Diazepam, Phenytoin, Imipramine) can provoke an increase in the concentration of the listed drugs. Taking this into account, it is necessary to reduce their dosage.

Co-administration of 30 mg Esomeprazole will result in a 45% decrease in clearance of the substrate Diazepam.

Concomitant use of Esomeprazole will result in increased serum Phenytoin concentrations in individuals with epilepsy. The amount of drug in the bloodstream should be monitored when Esomeprazole is prescribed or discontinued.

Taking Esomeprazole in combination with the drug Warfarin requires monitoring the quality of blood clotting.

Combination with Voriconazole and other CYP2C19 and CYP3A4 inhibitors may result in a more than two-fold increase in exposure to the active component Esomeprazole, which, however, does not require dosage adjustment of the drug.

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Storage conditions

Esomeprazole should be stored at room temperature, out of the reach of children.

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Shelf life

Esomeprazole in the form of a lyophilisate is stored in the original unopened packaging for up to 2 years. Unused Esomeprazole solution is not subject to storage - it is disposed of.

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