Emanera, 40mg capsules, 14pcs

Composition

1 capsule enteric 20 mg/ 40 mg contains:

Pellet core:

Active substance:

Esomeprazole magnesium dihydrate 21.688 mg/43.376 mg (equivalent to Esomeprazole magnesium 20.645 mg/41.290 mg, equivalent to Esomeprazole 20,000 mg/40,000 mg)

Auxiliary substances: granulated sugar [sucrose, starch molasses], povidone K 30, Sodium lauryl sulfate

Pellet shell:

Opadray II White 85F28751*, magnesium hydroxycarbonate (magnesium carbonate heavy), methacrylic acid and ethyl acrylate copolymer [1: 1], dispersion 30%**, talc, macrogol-6000, titanium dioxide (E 171), polysorbate-80

Gelatin capsule

Composition of empty gelatin capsules:

Capsule body:

Dye iron oxide red (E172), titanium dioxide (E171), gelatin

Capsule cap:

Dye iron oxide red (E172), titanium dioxide (E171), gelatin

* Opadray II White 85F28751 is a mixture of:

Polyvinyl alcohol, titanium dioxide (E 171), macrogol-3000, talc

**Dispersion of Eudragit L30D contains besides methacrylic acid, copolymer and ethylacrylate water, sodium lauryl sulfate (0,7% based on the solids of the dispersion) and Polysorbate-80 (2.3% based on the solids of the dispersion) as emulsifiers.

Pharmacological action

of gastric glands Secretion Lowering agent-Proton Pump Inhibitor

Clinical Pharmacology

Pharmacodynamics

Esomeprazole is an S-isomer of omeprazole and inhibits the secretion of hydrochloric acid in the stomach due to a specific and directed mechanism of action. Specifically inhibits the proton pump of parietal cells. Both omeprazole isomers, R – and S -, have similar pharmacodynamic activity.

Mechanism of action

Esomeprazole is a weak base, so it accumulates and passes into the active form in a highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, where it suppresses the activity of the H+/K+-ATPase enzyme. It suppresses both basal and stimulated hydrochloric acid secretion.

Effect on gastric acid secretion

The effect develops within 1 hour after ingestion of 20 mg or 40 mg of esomeprazole. With repeated use of 20 mg of esomeprazole once a day for 5 days, the average peak concentration of hydrochloric acid after stimulation with pentagastrin decreases by 90% (on the 5th day of therapy 6-7 hours after taking the drug).

In patients with gastroesophageal reflux disease (GERD) and the presence of clinical symptoms after daily use of esomeprazole at a dose of 20 mg or 40 mg for 5 days, the pH of the stomach contents above 4.0 remained on average for 13 and 17 hours, respectively. The proportion of patients treated with esomeprazole 20 mg/day, in which the pH of gastric contents exceeded 4.0 for 8,12 and 16 hours, was 76%,54% and 24%, respectively, and for esomeprazole 40 mg/day – 97%,92% and 56%.

The degree of suppression of acid secretion by esomeprazole is directly related to the area under the concentration-time curve.

Therapeutic effect achieved by suppressing acid secretion

Healing of reflux esophagitis with esomeprazole 40 mg occurs in approximately 78% of patients after 4 weeks and in 93% of patients after 8 weeks of therapy.

Treatment with esomeprazole 20 mg twice daily for 1 week in combination with appropriate antibiotics leads to successful eradication of Helicobacter Pylori in 90% of patients.

In uncomplicated peptic ulcer disease, after eradication therapy (lasting from 7 to 10-14 days), no continuation of monotherapy with antisecretory drugs is required to heal the ulcer and eliminate symptoms.

Other effects associated with suppressing acid secretion

During treatment with antisecretory drugs, an increase in the serum concentration of gastrin occurs. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) in the blood plasma increases. An increase in the concentration of CgA in blood plasma may affect the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, therapy with proton pump inhibitors (PPIs) should be suspended 5 days before the study of the concentration of CgA in blood plasma. If gastrin and CgA plasma concentrations do not return to normal values after 5 days, the study should be repeated 14 days after esomeprazole discontinuation.

In some patients, an increase in the number of enterochromaffin-like (ELC) cells was observed after long-term esomeprazole therapy, probably due to an increase in the concentration of gastrin in blood plasma.

With prolonged use of antisecretory drugs, a slight increase in the frequency of formation of glandular cysts of the stomach was noted. These changes are due to physiological changes resulting from prolonged suppression of acid secretion. The cysts are benign and reversible.

A decrease in the acidity of gastric contents against the background of taking antisecretory agents is accompanied by an increase in the content of microbial flora in the stomach, which is present in the gastrointestinal tract (GIT) normally. PPI therapy can lead to a slight increase in the risk of developing infectious diseases of the gastrointestinal tract, for example, caused by Salmonella and Campylobacterspp bacteria.

Esomeprazole is more effective in healing gastric ulcers in patients treated with nonsteroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors, compared to ranitidine.

Esomeprazole is highly effective in preventing gastric and duodenal ulcers in patients taking NSAIDs (for patients over 60 years of age and/or with a history of peptic ulcer), including selective cyclooxygenase-2 (COX-2) inhibitors.

Pharmacokinetics

Suction and distribution

Esomeprazole is unstable in an acidic environment, so it is taken orally in the form of enteric capsules containing pellets of the drug, the shell of which is also resistant to the action of gastric juice. Under invivo conditions, a small portion of esomeprazole is converted to the R-isomer. Esomeprazole is rapidly absorbed, reaching maximum plasma concentrations (cmax) approximately 1-2 hours after oral use. Absolute bioavailability is 64% after taking a single dose of 40 mg, which increases to 89% against the background of daily use of esomeprazole once a day. Bioavailability for esomeprazole at a dose of 20 mg is 50% and 68%, respectively. The volume of distribution at steady state in healthy volunteers is approximately 0.22 l / kg of body weight. Binding to plasma proteins is 97%.

Food intake slows down and reduces the absorption of esomeprazole, but has no significant clinical significance.

Metabolism and elimination

Esomeprazole is completely metabolized by the cytochrome P450 system in the liver. Most of them are metabolized with the participation of the polymorphic isoenzyme CYP2C19, which is responsible for the formation of hydroxy – and demethylated metabolites. The remainder of esomeprazole is metabolized by the isoenzyme CYP3A4, which is responsible for the formation of esomeprazole sulfone, the main metabolite in blood plasma.

Total plasma clearance after a single dose is approximately 17 l / h and 9 l / h after a multiple dose. The half-life (T_1/2) is 1.3 hours with prolonged use of the drug once a day. The area under the concentration-time curve (AUC) increases with repeated use. The dose-dependent increase in AUC with repeated use is non-linear due to a decrease in metabolism during the “primary passage” through the liver, a decrease in clearance, probably caused by inhibition of the CYP2C19 isoenzyme by esomeprazole and/or its sulfide-containing metabolite. With a single daily dose, esomeprazole is completely eliminated from the blood plasma between doses. Esomeprazole does not accumulate.

The main metabolites of esomeprazole do not affect the secretion of hydrochloric acid in the stomach. Almost 80% of the oral dose of esomeprazole is excreted by the kidneys in the form of metabolites, and the rest is excreted through the intestines. Less than 1% of unchanged esomeprazole is detected in the urine.

Pharmacokinetics in selected groups of patients

Approximately 2.9±1.5% of the population has reduced activity of the CYP 2C19 isoenzyme. In such patients, esomeprazole is primarily metabolized by the CYP3A4 isoenzyme. After repeated use of esomeprazole at a dose of 40 mg once a day, the average AUC value is approximately 2 times higher than in patients with reduced CYP2C19 activity. The average values of_cmaxin blood plasma increase by about 60%.

In elderly patients (71-80 years), the metabolism of esomeprazole does not change significantly.

After a single 40 mg dose of esomeprazole, the mean AUC value in women is approximately 30% higher than in men. In the future, no differences in pharmacokinetics were observed in patients of both sexes when esomeprazole was systematically taken once a day. These features do not affect the dose and method of use of the drug.

Esomeprazole metabolism may be impaired in patients with mild to moderate hepatic impairment. The metabolic rate is reduced in severe hepatic impairment, which is accompanied by a twofold increase in AUC. Therefore, the maximum daily dose of esomeprazole in these patients is 20 mg.

Pharmacokinetics have not been studied in patients with reduced renal function. Since esomeprazole metabolites, rather than esomeprazole itself, are eliminated through the kidneys, the metabolism of esomeprazole in these patients does not change.

After repeated use of 20 mg and 40 mg of esomeprazole, the AUC and time to reach maximum concentration (TC_max) values in children aged 12-18 years and adults were the same.

Indications

* Gastroesophageal reflux disease (GERD):

– treatment of erosive reflux esophagitis;

–long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse;

–symptomatic treatment of GERD.

·  Peptic ulcer of the stomach and duodenum.

As part of combination therapy:

– treatment of duodenal ulcers associated with Helicobacter pylori;

– prevention of relapses of peptic ulcers associated with Helicobacter pylori

· * Long-term acid-suppressing therapy in patients who have suffered bleeding from peptic ulcers (after intravenous use of drugs that reduce the secretion of gastric glands, to prevent relapse).

* Patients taking long-term nonsteroidal anti-inflammatory drugs (NSAIDs):

– healing of stomach ulcers associated with NSAID use;

– prevention of gastric and duodenal ulcers associated with NSAID use in patients at risk.

* Zollinger-Ellison syndrome and other conditions characterized by abnormal hypersecretion of the gastric glands, including idiopathic hypersecretion.

Use during pregnancy and lactation

There are insufficient data on the use of esomeprazole in pregnant women.

In epidemiological studies, no fetotoxic effects or fetal developmental disorders were detected during the use of the racemic mixture of omeprazole.

Studies with esomeprazole in animals did not reveal a direct or indirect negative effect on the development of the embryo or fetus, nor did they reveal a direct or indirect negative effect on the course of pregnancy, childbirth and in the postnatal period of development of the newborn. Pregnant women should be prescribed the drug only if the expected benefit to the mother exceeds the possible risk to the fetus.

Currently, it is not known whether esomeprazole is excreted in breast milk, so the drug Emanera® should not be used during breastfeeding.

Contraindications

·  Hypersensitivity to esomeprazole, substituted benzimidazoles or other components of the drug.

* Children under 12 years of age (no efficacy or safety data available) and children over 12 years of age for indications other than gastroesophageal reflux disease (GERD).

* Concomitant use with atazanavir and nelfinavir (see section “Interactions with other medicinal products”).

* Hereditary fructose intolerance, glucose-galactose malabsorption syndrome, or sucrose-isomaltase deficiency (Emanera ® contains sucrose).

Side effects

The following are side effects, independent of the dosage regimen of Emanera®, observed with the use of esomeprazole, both in clinical studies and in post-marketing studies.

Classification of the incidence of side effects recommended by the World Health Organization (WHO):

very common ≥ 1/10

common ≥ 1/100 to < 1/10

uncommon ≥ 1/1000 to < 1/100

rare ≥ 1/10000 to < 1/1000

very rare < 1/10000

frequency unknown cannot be estimated based on available data.

In each group, undesirable effects are presented in decreasing order of severity.

Disorders of the blood and lymphatic system:

rare: leukopenia, thrombocytopenia;

very rare: agranulocytosis, pancytopenia.

Immune system disorders:

rarely: hypersensitivity reactions(e. g. fever, angioedema, anaphylactic reaction/anaphylactic shock).

Metabolic and nutritional disorders:

infrequently: peripheral edema;

rarely: hyponatremia;

very rarely: hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia.

Mental disorders:

infrequently:insomnia;

rarely: depression, agitation, confusion;

very rarely: hallucinations, aggressive behavior.

Nervous system disorders:

common: headache;

infrequent:dizziness, paresthesia, drowsiness;

rarely: taste changes.

Visual disturbances:

rare: blurred vision.

Respiratory, thoracic and mediastinal disorders:

rare: bronchospasm.

Disorders of the digestive system:

common: abdominal pain, constipation, diarrhea, flatulence, nausea/vomiting, glandular polyps of the stomach floor (benign);

infrequent: dry oral mucosa;

rare: stomatitis, candidiasis of the gastrointestinal tract;

very rare: microscopic colitis (confirmed histologically).

Liver and biliary tract disorders:

infrequently: increased activity of “liver” enzymes in blood plasma;

rarely: hepatitis (with or without jaundice);

very rarely: liver failure, hepatic encephalopathy in patients with liver diseases.

Skin and subcutaneous tissue disorders:

infrequently:dermatitis, skin rash, pruritus, urticaria;

rare: alopecia, photosensitization;

very rare: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis;

frequency unknown: subacute cutaneous lupus erythematosus (PKKV).

Musculoskeletal and connective tissue disorders:

infrequently: fracture of the femoral neck, wrist or spine;

rarely: arthralgia, myalgia;

very rarely: muscle weakness.

Kidney and urinary tract disorders:

very rare:interstitial nephritis, some patients have been reported to have renal failure.

Genital and breast disorders:

very rare:gynecomastia.

General disorders and disorders at the injection site:

rarely: malaise, increased sweating.

Interaction

Effect of esomeprazole on the pharmacokinetics of other drugs

Medicinal products whose absorption depends on the pH level

A decrease in the secretion of hydrochloric acid in the stomach during treatment with esomeprazole and other PPIs may lead to a change in the absorption of drugs, the absorption of which depends on the level of acidity of the medium. Similar to antacids and other drugs that reduce the acidity of gastric juice, the use of esomeprazole can lead to a decrease in the absorption of ketoconazole, itraconazole and erlotiniband increase the absorption of drugs such as digoxin.

Concomitant use of omeprazole at a dose of 20 mg once a day and digoxin increases the bioavailability of digoxin by 10% (digoxin bioavailability increased by up to 30% in two out of ten patients).

Omeprazole is known to interact with some antiviral drugs. The mechanism and clinical significance of these interactions are not always known. A decrease in the acidity of gastric juice during omeprazole therapy may affect the absorption of antiviral drugs. Interaction at the level of the CYP2C19 isoenzyme is also possible. During omeprazole therapy, there is a decrease in serum concentrations of some antiviral drugs (atazanavir and nelfinavir). Therefore, simultaneous use is contraindicated. Concomitant use of omeprazole (40 mg once daily) with atazanavir 300 mg/ritonavir 100 mg in healthy volunteers is accompanied by a marked decrease in the bioavailability of atazanavir (AUC, _{cmax, and minimum plasma concentration [cmin}]decreased by approximately 75%). Increasing the dose of atazanavir to 400 mg did not compensate for the effect of omeprazole on the bioavailability of atazanavir.

Concomitant use of omeprazole with saquinavir increases the concentration of saquinavir in the blood serum.

Given the similar pharmacokinetic and pharmacodynamic properties of omeprazole and esomeprazole, concomitant use of esomeprazole with antiviral drugs such as atazanavir and nelfinaviris contraindicated.

Medicinal products that are metabolized by the CYP2 C19 isoenzyme

Esomeprazole inhibits the CYP2C19 isoenzyme, the main isoenzyme of esomeprazole metabolism. Thus, when esomeprazole is co-administered with drugs whose metabolism involves the CYP2C19 isoenzyme, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., the concentration of these drugs in the blood plasma may increase and, accordingly, their dose may need to be reduced.

This is especially important to consider when prescribing Emanera® in the “on-demand” mode. Thus, when co-administered with 30 mg of esomeprazole, the clearance of diazepam (a substrate of the CYP2C19 isoenzyme) decreases by 45%.

Concomitant use of esomeprazole at a dose of 40 mg leads to an increase in the concentration of phenytoin in blood plasma in patients with epilepsy by 13%. It is recommended to monitor the concentration of phenytoin in blood plasma at the beginning of esomeprazole therapy and when it is discontinued.

Omeprazole 40 mg increases the_cmaxand AUCof voriconazole (a substrate of the CYP2C19 isoenzyme) by 15% and 41%, respectively.

The coagulation time with simultaneous long-term use of warfarin and esomeprazole at a dose of 40 mg remains within acceptable limits. However, several cases of clinically significant increases in the international normalized ratio (INR) index have been reported. It is recommended to monitor INR at the beginning and end of concomitant use of esomeprazole and warfarin or other coumarin derivatives.

The use of omeprazole at a dose of 40 mg resulted in an increase in the_cmaxand AUC of cilostazol by 18% and 26%, respectively, for one of the active metabolites of cilostazol, the increase was 29% and 69%, respectively.

Concomitant use of esomeprazole at a dose of 40 mg with cisapride leads to an increase in the pharmacokinetic parameters of cisapride in healthy volunteers: AUC-by 32% and T_1/2– by 31%, but_Cmax does not change significantly. The slight prolongation of the QT interval on the ECG, which is observed with cisapride monotherapy, did not increase with the addition of esomeprazole.

In some patients, an increase in the concentration of methotrexate in the blood serum was noted against the background of simultaneous use with PPIs. When using high doses of methotrexate, temporary discontinuation of esomeprazole should be considered.

Esomeprazole does not cause clinically significant changes in the pharmacokinetics of amoxicillin and quinidine.

Concomitant short-term use of esomeprazole and naproxen or rofecoxib did not reveal a clinically significant pharmacokinetic interaction.

The results obtained in studies involving healthy volunteers proved a pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg/maintenance dose 75 mg per day) and esomeprazole (40 mg per day when taken orally), which leads to a decrease in systemic exposure to the active metabolite of clopidogrel by an average of 40% and to a decrease in the maximum suppression (ADP-induced) of platelet aggregation by an average of 14%.

When clopidogrel was administered simultaneously with a fixed combination of 20 mg esomeprazole/81 mg acetylsalicylic acid (ASA) compared to clopidogrel alone, a study in healthy volunteers showed a decrease in systemic exposure to the active metabolite of clopidogrel by almost 40%. However, the maximum levels of suppression (ADP-induced) of platelet aggregation in these healthy volunteers were the same in the clopidogrel and clopidogrel-fixed combination groups (esomeprazole/ASA).

In both observational and clinical studies, conflicting data have been obtained regarding the clinical effects of the pharmacokinetic/pharmacodynamic interaction of esomeprazole on major cardiovascular events. As a precautionary measure, concomitant use of clopidogrel should be avoided.

When used concomitantly with tacrolimus, it is possible to increase the serum concentrations of tacrolimus.

Effect of medicinal products on the pharmacokinetics of esomeprazole

The isoenzymes CYP2C19 and CYP3A4 are involved in the metabolism of esomeprazole.

When esomeprazole is co-administered with clarithromycin (500 mg twice daily) (an inhibitor of the CYP3A4 isoenzyme), the AUC of esomeprazole increases by 2 times.

Concomitant use of esomeprazole and a combined inhibitor of the CYP2C19 and CYP3A4 isoenzymes (for example, voriconazole) may be accompanied by an increase in the AUC of esomeprazole by more than 2 times. Esomeprazole dosage changes are usually not required in these situations. In patients with severe hepatic impairment or if long-term therapy is necessary, esomeprazole dose reduction should be considered.

Drugs that induce the isoenzymes CYP2C19 and CYP3A4, such as rifampicin and St. John’s wort, when used concomitantly with esomeprazole, can lead to a decrease in the concentration of esomeprazole in blood plasma due to the acceleration of esomeprazole metabolism.

How to take, course of use and dosage

Inside. The capsule should be swallowed whole, without chewing, with a small amount of liquid.

For patients with difficulty swallowing, the contents of the capsule can be poured into half a glass of still water (do not use other liquids, as the protective shell of pellets may dissolve), stir, and then the pellet suspension should be drunk immediately or within 30 minutes. Then fill the glass half full again, rinse the sides of the glass, stir the rest and drink. Pellets should not be chewed or crushed.

Patients who cannot swallow on their own should dissolve the contents of the capsules in still water and inject esomeprazole through a nasogastric tube. It is important that the selected syringe and probe are suitable for performing this procedure. Instructions for preparation and use of the drug through a nasogastric tube are given in the subsection “use of the drug through a nasogastric tube”.

Adults and children over 12 years of age

Gastroesophageal reflux disease (GERD)

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

An additional 4-week course of treatment is recommended in cases where healing of esophagitis does not occur after the first course of treatment or symptoms persist.

Long-term maintenance treatment after erosive reflux esophagitis has healed to prevent relapse: 20 mg once a day.

Symptomatic treatment of GERD: 20 mg once a day for patients without esophagitis. If after 4 weeks of treatment the symptoms do not disappear, an additional examination of the patient should be performed. After the symptoms are resolved, you can switch to an “on-demand” regimen, i. e. take Emanera® 20 mg once a day if symptoms resume. For patients taking NSAIDs who are at risk of developing gastric or duodenal ulcers, on-demand treatment is not recommended.

Adult patients

Peptic ulcer of the stomach and duodenum

As part of a combination therapy for the eradication of Helicobacter pylori

• , treatment of duodenal ulcers associated with Helicobacter pylori: Emanera® 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All medications are taken twice a day for 7-14 days.
• prevention of recurrent peptic ulcers associated with Helicobacter pylori: Emanera ® 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All medications are taken twice a day for 7-14 days.

Long-term acid-suppressing therapy in patients who have suffered bleeding from a peptic ulcer (after intravenous use of drugs that reduce the secretion of gastric glands, to prevent relapse)

Emanera 40 mg once daily for 4 weeks after the end of intravenous therapy with drugs that reduce the secretion of gastric glands.

Patients taking NSAIDs for a long

• time healing of stomach ulcers associated with NSAID use: Emanera® 20 mg or 40 mg once a day. The duration of treatment is 4-8 weeks.
• prevention of stomach and duodenal ulcers associated with NSAIDs: Emanera 20 mg or 40 mg once daily.

Conditions associated with abnormal gastric gland hypersecretion, including Zollinger-Ellison syndrome and idiopathic hypersecretion

The recommended starting dose of Emanera is 40 mg twice daily. In the future, the dose is selected individually, the duration of treatment is determined by the clinical picture of the disease. There is experience of using the drug in doses up to 120 mg 2 times a day.

Kidney failure: dose adjustment of Emanera® is not required. However, experience with esomeprazole in patients with severe renal insufficiency is limited, and therefore caution should be exercised when prescribing Emanera® to such patients (see section “Pharmacokinetics”).

Liver failure: in patients with mild to moderate hepatic insufficiency, dose adjustment of Emanera® is not required. For patients with severe hepatic insufficiency, the maximum daily dose should not exceed 20 mg.

Elderly patients: dose adjustment of Emanera® is not required.

use of the drug through a nasogastric tube

When prescribing the drug through a nasogastric tube

Open the capsule and pour the contents of the capsule into a special syringe. Add 25 ml of drinking water and approximately 5 ml of air to the syringe. For some probes, it may be necessary to dilute the drug in 50 ml of drinking water in order to prevent clogging of the probe with pellets contained in the capsule.

After adding water, immediately shake the syringe until a suspension is obtained.

Make sure that the tip is not clogged (by applying a little pressure on the plunger, holding the syringe in the tip-up position).

Insert the tip of the syringe into the probe, keeping it pointing upwards.

Shake the syringe and turn it upside down. Immediately inject 5-10 ml of the dissolved drug into the probe. After the solution is inserted, return the syringe to its original position and shake (the syringe should be held tip up to avoid clogging the tip).

Lower the syringe tip down again and inject another 5-10 ml of the solution into the probe. Repeat the procedure until the syringe is empty.

If some of the drug remains as a sediment in the syringe: fill the syringe with 25 ml of water and 5 ml of air and repeat the procedures described in points 5 and 6. For some probes,50 ml of drinking water may be required for this purpose.

Overdose

Currently, extremely rare cases of deliberate overdose of esomeprazole have been described. Oral use of esomeprazole at a dose of 280 mg was accompanied by general weakness and symptoms from the gastrointestinal tract. A single dose of 80 mg of esomeprazole did not cause any negative consequences. The antidote of esomeprazole is unknown. Esomeprazole binds well to plasma proteins, so dialysis is ineffective. In case of overdose, it is necessary to conduct symptomatic and general supportive treatment.

Description

20 mg Capsules:

Capsules No. 3. The body and cap of the capsule are light pink in color. Capsule contents: pellets are white to almost white in color.

40 mg Capsules:

Capsules No. 1. The body and cap of the capsule are pink to pink with a faint grayish tinge of color. Capsule contents: pellets are white to almost white in color.

Special instructions

Severe renal failure (limited experience).

It is contraindicated in children under 12 years of age (there are no data on efficacy and safety) and is contraindicated in children over 12 years of age for other indications other than gastroesophageal reflux disease (GERD).

Children over 12 years of age

Gastroesophageal reflux disease (GERD)

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

Long-term maintenance treatment after erosive reflux esophagitis has healed to prevent relapse: 20 mg once a day.

Symptomatic treatment of GERD: 20 mg once a day for patients without esophagitis. After the symptoms are resolved, you can switch to an “on-demand” regimen, i. e. take Emanera® 20 mg once a day if symptoms resume.

Kidney failure: dose adjustment of Emanera® is not required. However, experience with esomeprazole in patients with severe renal insufficiency is limited, and therefore caution should be exercised when prescribing Emanera® to such patients (see section “Pharmacokinetics”).

Liver failure: in patients with mild to moderate hepatic insufficiency, dose adjustment of Emanera® is not required. For patients with severe hepatic insufficiency, the maximum daily dose should not exceed 20 mg.

Elderly patients: dose adjustment of Emanera® is not required.

If there are disturbing symptoms (for example, such as significant, spontaneous weight loss, repeated vomiting, dysphagia, vomiting with blood or melena), as well as if a stomach ulcer is suspected or detected, it is necessary to exclude a malignant neoplasm, since the use of Emanera® can reduce the severity of symptoms and delay diagnosis.

Patients taking Emanera® for a long time (especially for more than a year) should be under regular medical supervision.

Patients taking the drug “on demand” should be informed about the need to consult a doctor if the nature of symptoms changes. Taking into account fluctuations in the concentration of esomeprazole in blood plasma when using the drug in the “on-demand” mode, interactions with other drugs should be taken into account (see the section “Interaction with drugs”).

When using esomeprazole for the eradication of Helicobacter Pylori, possible interactions between the components of triple therapy should be considered. Clarithromycin is a potent inhibitor of CYP3A4, so contraindications and drug interactions of clarithromycin should be considered when prescribing triple therapy to patients simultaneously taking drugs that are metabolized by the CYP3A4 isoenzyme, such as cisapride.

Influence on the results of laboratory tests

An increase in the concentration of CgA in blood plasma may affect the results of studies conducted to diagnose neuroendocrine tumors. To avoid this effect, treatment with Emanera® should be discontinued at least 5 days before determining the concentration of CgA (see section ” Pharmacodynamics “of the section “Pharmacological properties”) in blood plasma. If CgA and gastrin concentrations do not return to the normal range after the initial measurement, a follow-up study should be performed 14 days after stopping PPI treatment.

Hypomagnesemia

Cases of severe hypomagnesaemia have been reported in patients treated with PPIs such as esomeprazole for at least three months and, in most cases, within a year. Severe manifestations of hypomagnesemia may occur, such as fatigue, tetany, delirium, seizures, dizziness, and ventricular arrhythmia, but they may develop gradually and may be overlooked. In patients with the most severe disorders, hypomagnesemia decreased after magnesium replacement therapy and PPI discontinuation.

In patients who are scheduled for long-term therapy or who are taking PPIs simultaneously with digoxin or drugs that cause hypomagnesemia (for example, diuretics), health professionals should consider monitoring the magnesium content in the blood plasma before starting treatment with PPIs and periodically during treatment.

Fractures of the femoral neck, wrist bones and spine

PPI, especially when used in high doses and for a long time (more than 1 year), may moderately increase the risk of fractures of the femoral neck, wrist bones and spine, mainly in the elderly or in the presence of other identified risk factors. According to the results of observational studies, PPIs can increase the overall risk of fracture by 10-40%. A certain degree of this increase may be due to other risk factors. Patients at risk of developing osteoporosis should be treated in accordance with current clinical guidelines and should consume adequate amounts of vitamin D and calcium.

Subacute cutaneous lupus erythematosus (PKKV)

The use of PPIs is associated with extremely rare cases of PCV. In case of pathological changes in the skin, especially in open areas, accompanied by arthralgia, the patient should immediately seek medical help. Your doctor should consider discontinuing the drug Emanerase. PKKV due to previous PPI therapy may increase the risk of developing PKKV with subsequent therapy with other PPIs.

Special information on excipients

Emanera ® contains sucrose, so its use is contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption syndrome or sucrose-isomaltase deficiency.

During treatment with the drug, care should be taken when performing potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Enteric capsules,20 mg,40 mg.

7 capsules in a blister of combined OPA/Al/PVC and aluminum foil(OPA/Al/PVCfoilandaluminiumfoil).

1,2,4 blisters are placed in a cardboard pack together with the instructions for use.

Storage conditions

At a temperature not exceeding 25 ° C, in the original packaging.

Keep out of reach of children.

Shelf

life is 2 years.

Do not use the drug after the expiration date.

Active ingredient

Esomeprazole

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

Pregnant women as prescribed by a doctor, Adults as prescribed by a doctor, Children over 12 years of age, Children as prescribed by a doctor

Indications

for Reflux Esophagitis, Gastrointestinal infections caused by Helicobacter Pylori