Esomeprazole - instructions for use, dose, side effects, contraindications

Antiulcer means proton pump inhibitor, dextrorotatory isomer of omeprazole. Reduces the secretion of hydrochloric acid in the stomach by specifically inhibiting the proton pump in parietal cells. Being a weak base and passing into the active form in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, it activates and inhibits the proton pump - enzyme H⁺-K⁺-ATP-ase. Inhibits both basal and stimulated secretion of hydrochloric (hydrochloric) acid. The action occurs 1 hour after oral administration of 20 mg or 40 mg. With daily use for 5 days at a dose of 20 mg once a day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin is reduced by 90%.

Pharmacokinetics:

Prodrug. Absorption - 50-64%, increases with repeated administration to approximately 68 and 89% for doses of 20 and 40 mg, respectively. Half-life0.5-1 hour. The connection with plasma proteins is 97%. Biotransformation in the liver predominantly CYP2S19, to a lesser extent CYP34 with the formation of inactive metabolites. With repeated administration, the effect of primary passage through the liver, probably related to inhibition of CYP2C19 activity, decreases. The administration of equimolar doses of the S and R isomers results in a higher plasma concentration of the S-, rather than the R-isomer. Creatinine clearance is 500-600 ml / min. Elimination of the kidneys 70-80% (inactive metabolite), with faeces 20-30% (inactive metabolite).

Indications:

Gastroesophageal reflux disease: erosive reflux-esophagitis (treatment), prevention of relapses in patients with cured esophagitis, symptomatic treatment of gastroesophageal reflux disease.

As part of combination therapy: eradication Helicobacter pylori, duodenal ulcer associated with Helicobacter pylori, prevention of recurrence of peptic ulcers in patients with peptic ulcer associated with Helicobacter pylori.

ICD-10

XI.K20-K31.K27 Peptic ulcer of unspecified site

XI.K20-K31.K26 Duodenal ulcer

XI.K20-K31.K25 Stomach ulcer

XI.K20-K31.K21.0 Gastroesophageal reflux with esophagitis

XI.K20-K31.K21 Gastroesophageal reflux

XI.K90-K93.K92.2 Gastrointestinal bleeding, unspecified

Contraindications:

Hypersensitivity (including substituted benzimidazoles); simultaneous reception with atazanavir (reduced concentration in plasma atazanavir); lactation period, children under 12 years of age (due to the lack of data on the efficacy and safety of the drug in this group of patients) and children over 12 years of age on other indications, except for gastroesophageal reflux disease; severe renal failure (experience with use is limited); hereditary intolerance to fructose, glucose-galactose malabsorption or sugar-isomaltase deficiency.

Carefully:

Pregnancy.

Before the beginning of therapy to exclude the presence of malignant process (especially with ulcer of the stomach), as treatment, masking the symptoms, can delay the establishment of the correct diagnosis.

Pregnancy and lactation:

Recommendations for FDA - Category B. Currently, there is no data on the use of esomeprazole during pregnancy. With the introduction of esomeprazole, no direct or indirect adverse effects on the development of the embryo or fetus have been identified in animals. The introduction of the racemic preparation also did not have any negative impact on animals during pregnancy, childbirth, and also during postnatal development. Nevertheless, prescribe the drug to pregnant women only if the expected benefit to the mother exceeds the possible risk to the fetus.

It is not known whether esomeprazole with breast milk. Do not apply.

Dosing and Administration:

Inside. The tablet should be swallowed whole, washed down with liquid. Tablets can not be chewed or broken.

Treatment of erosive reflux esophagitis: 40 mg once a day for 4 weeks.

An additional 4-week course of treatment is recommended in those cases when, after the first course, there is no cure for esophagitis or the symptoms remain.

Prevention of relapse in patients with cured esophagitis: 20 mg once a day.

Symptomatic treatment of gastroesophageal reflux disease: 20 mg once a day - for patients without esophagitis. If after 4 weeks of treatment the symptoms do not disappear, you should conduct an additional examination of the patient.

In combination with appropriate antibiotic therapy for eradication Helicobacter pylori, treatment of duodenal ulcer associated with Helicobacter pylori, prevention of recurrence of peptic ulcers in patients with peptic ulcer associated with Helicobacter pylori: esomeprazole - 20 mg, amoxicillin - 1 g and clarithromycin - 500 mg 2 times a day for 7 days.

Patients with renal insufficiency and for elderly patients do not need dose adjustment.

In severe hepatic insufficiency, the dose should not exceed 20 mg per day.

Side effects:

Frequent (0.1-1%): headache, abdominal pain, diarrhea, flatulence, nausea, vomiting, constipation.

Rare (0.01-0.1%): dermatitis, itching, hives, dizziness, dry mouth.

Overdose:

Treatment: a specific antidote is unknown, dialysis is ineffective, if necessary, symptomatic therapy is performed.

Interaction:

It is believed that with simultaneous use, it is possible to increase concentrations in the blood plasma and enhance the effects of imipramine, clomipramine, citalopram.

It is believed that with simultaneous use, it is possible to reduce the concentrations in the blood plasma and the clinical efficacy of itraconazole and ketoconazole.

With simultaneous use with clarithromycin, the case of a significant increase in systemic exposure of esomeprazole has been described due to the inhibition of its metabolism under the influence of clarithromycin.

With simultaneous use, it is possible to increase the concentrations in the blood plasma of diazepam and phenytoin, which, apparently, has no clinical significance.

Digoxin - increased absorption.

Special instructions:

In the presence of any anxiety symptoms (for example, such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting with blood or melena), and in the presence of a stomach ulcer (or suspected gastric ulcer), the possibility of malignant neoplasm should be excluded, esomeprazole can lead to a smoothing of the symptoms and thus delay the setting of the correct diagnosis.

Patients taking the drug for a long period (especially more than 1 year) should be under regular medical supervision.

During treatment with proton pump inhibitors, the concentration of gastrin in the plasma is increased as a result of reduced intragastric secretion of hydrochloric acid.

In patients taking proton pump inhibitors for a long time, the formation of glandular cysts in the stomach is more common. These phenomena are caused by physiological changes due to inhibition of hydrochloric acid secretion. Cysts are benign and tend to disappear.

Instructions

Esomeprazole (Esomeprazolum)