Esomeprazole

Medication Esomeprazole belongs to the category of proton pump inhibitor drugs - it is a wide range of medicines that are used in the therapy of ulcer of duodenal ulcer and gastroesophageal reflux pathology.

[1], [2], [3],

Indications Esomeprazole

Esomeprazole is indicated:

• as an antisecretory drug;
• at a gastroesophageal reflux pathology at persons with the complicated reflux or esophagitis;
• with gastric ulcer caused by the use of non-steroidal anti-inflammatory drugs;
• to prevent the development of peptic ulcer and ulcer of duodenum during treatment with nonsteroidal anti-inflammatory agents;
• for short-term support of hemostasis and prevention of recurrent bleeding in patients after endoscopic therapy of an acute bleeding ulcer.

Release form

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

In one flacon with lyophilizate contains the active ingredient of the drug - sodium esomeprazole, in an alternative esomeprazole amount of 40 mg.

In the packaging of cardboard is one glass bottle with a cork of rubber and a rolled aluminum cover with a "flip" opening device. 

[4], [5], [6]

Pharmacodynamics

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

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

[7], [8], [9], [10], [11],

Pharmacokinetics

The drug is absorbed rapidly, reaching high concentrations for half an hour after the use of the dosage. Full bioavailability can be 90%. The connection with plasma proteins is 95%.

Simultaneous eating reduces absorption and slows down the absorption of esomeprazole.

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

The half-life is 60-90 minutes. The ratio of plasma concentration and time increases with repeated use of the drug. This increase depends on the dosage of esomeprazole and provokes a non-linear relationship with repeated admission.

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

The active substance is fully excreted from the bloodstream during the period between doses of regular doses, without accumulation, with daily intake of esomeprazole 1 time per day.

The presence of basic 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 the urinary fluid, and the remaining amount - with the calves.

[12], [13], [14], [15], [16], [17], [18]

Dosing and administration

Individuals who are contraindicated with the internal use of the drug may be prescribed parenteral administration in the amount of 20 to 40 mg daily. With reflux esophagitis take 40 mg of esomeprazole per day. With symptomatic therapy of gastroesophageal reflux disease, 20 mg of medication are prescribed daily.

With gastric and duodenal ulcers caused by the use of non-steroidal anti-inflammatory drugs, a standard dosage of 20 mg is prescribed daily. For preventive purposes, the amount of the drug does not change.

The duration of the period of therapy with esomeprazole is determined by the doctor and does not happen long.

After endoscopic stoppage of gastric bleeding, 80 mg of esomeprazole is used in the form of a half-hour infusion, after which a prolonged (72 h) intravenous infusion of 8 mg per hour is expected.

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

[23]

Use Esomeprazole during pregnancy

Drug esomeprazole is not prescribed for pregnant and lactating patients, as there is no reliable clinical information regarding the safety of the proposed drug for the fetus and the newborn baby.

Contraindications

Esomeprazole is contraindicated:

• when hypersensitivity reactions to the ingredients of the drug;
• in combination with Nelfigavir or Atazanavir;
• patients of children's age (under 18 years);
• during pregnancy;
• in the period of breastfeeding.

[19], [20]

Side effects Esomeprazole

Esomeprazole therapy may be accompanied by:

• a decrease in the level of leukocytes and platelets in the blood;
• allergy, up to anaphylaxis;
• swelling of the extremities;
• sleep disturbance;
• depression, disorders of consciousness;
• pain in the head, fatigue;
• disorder of visual function, hearing;
• dizziness;
• signs of bronchospasm;
• dyspepsia, abdominal pain;
• thirst;
• jaundice, hepatitis;
• dermatitis, skin rashes, zonal baldness;
• pain in the joints and muscles;
• increased sweating.

[21], [22]

Overdose

Information on the overdose of esomeprazole is not enough. Signs of an overdose may correspond to adverse events and occur after oral intake of more than 280 mg of the drug.

Specific antidote is not installed.

Hemodialysis is considered ineffective, and for this reason, with excessive dosing, doctors are limited to symptomatic and supportive therapeutic interventions.

Interactions with other drugs

Reduced gastric acidity when taking esomeprazole may affect the absorption of drugs, if the processes of their assimilation depend on the degree of acidity. It is noted that the use of other drugs that inhibit the production of acid, as well as antacids, provokes a decrease in absorption of ketoconazole or Intraconazole during the period of therapy with esomeprazole.

Esomeprazole in combination with medications that metabolize CYP2C19 (diazepam, phenytoin, imipramine) can cause an increase in the concentration of these drugs. Given this, it is necessary to lower their dosage.

Co-administration of 30 mg of esomeprazole will result in a reduced clearance of the substrate Diazepam by 45%.

Joint use of esomeprazole will lead to an increase in the concentration of phenytoin in the blood serum in people with epilepsy. It should be monitored for the amount of the drug in the bloodstream at the time of appointment or withdrawal of esomeprazole.

Admission Esomeprazole in combination with the medication Warfarin requires the quality control of blood clotting.

The combination with Voriconazole and other inhibitors of CYP2C19 and CYP3A4 can lead to an increase in exposure of the active component of esomeprazole by more than two times, which, however, does not require correction of the dosage of the drug.

[24], [25], [26], [27], [28]

Storage conditions

Esomeprazole is stored at normal room temperature, away from children's access.

[29], [30],

Shelf life

Esomeprazole in the form of lyophilizate is stored in factory unopened packaging for up to 2 years. Unused solution Esomeprazole is not stored - it is disposed of.

[31], [32], [33], [34]