Emanera - instructions for use, analogs, reviews and release forms (capsules or tablets of 20 mg and 40 mg) of an esomeprazole-based medication for the treatment of ulcers, gastritis and reflux in adults, children, and pregnancy. Composition

In this article, you can read the instructions for using the drug Emanera. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Emanera in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogs of the Emanera in the presence of existing structural analogs. Use to treat ulcers, gastritis and reflux in adults, children, as well as during pregnancy and lactation. Composition of the drug based on esomeprazole.

Emanera - a drug that reduces gastric secretion, a proton pump inhibitor. Esomeprazole (the active substance of the drug Emanera) is an S-isomer of Omeprazole and suppresses the secretion of hydrochloric acid in the stomach due to a specific and directional mechanism of action. Specifically inhibits the proton pump of parietal cells. Both isomers of omeprazole, R- and S-, have similar pharmacodynamic activity.

Mechanism of action

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

Effect on secretion of acid in the stomach

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

The therapeutic effect achieved by suppressing acid secretion

The healing of reflux esophagitis, when taking esomeprazole at a dose of 40 mg, occurs in about 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 the corresponding antibiotics leads to successful eradication of Helicobacter pylori (helicobacter) in 90% of patients.

Uncomplicated peptic ulcer after eradication therapy (duration from 7 to 10-14 days) does not require continuation of monotherapy with antisecretory drugs for ulcer healing and elimination of symptoms.

Other effects associated with the suppression of acid secretion

Against the background of therapy with antisecretory drugs, the level of gastrin in blood serum increases in response to a decrease in acid secretion.

In some patients, after prolonged therapy with esomeprazole, there has been an increase in the number of enterochromaffin-like (ELC) cells, probably due to an increase in the level of gastrin in the blood plasma.

With prolonged administration of antisecretory drugs, there was a slight increase in the frequency of formation of the glandular cysts of the stomach. These changes are due to physiological changes resulting from prolonged inhibition of acid secretion. Cysts are benign and have a reversible character.

Reduction of acidity of gastric contents against the background of antisecretory medication is accompanied by an increase in the content of microbial flora in the stomach present in the gastrointestinal tract in norm. Therapy with proton pump inhibitors can lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract, for example caused by bacteria of the genus Salmonella spp. (Salmonella) and Campylobacter spp.

Esomeprazole is more effective in healing gastric ulcers in patients who have used non-steroidal anti-inflammatory drugs (NSAIDs), incl. selective inhibitors of COX-2 in comparison with ranitidine.

High efficacy of esomeprazole in the prevention of gastric and duodenal ulcers in patients taking NSAIDs (for patients older than 60 and / or with a peptic ulcer in a history) is noted, among others. selective inhibitors of COX-2.

Composition

Esomeprazole magnesium + auxiliary substances.

Pharmacokinetics

Esomeprazole is unstable in an acidic medium, therefore it is intended for oral administration in the form of enteric-soluble capsules containing pellets of the Emaner preparation, the shell of which is also resistant to the action of gastric juice.In vivo, an insignificant portion of esomeprazole is converted to the R-isomer. Esomeprazole is quickly absorbed, reaching Cmax in the blood plasma approximately 1-2 hours after ingestion. Absolute bioavailability is 64% after taking a single dose of 40 mg, which rises to 89% against the daily intake of esomeprazole once a day. Bioavailability of esomeprazole at a dose of 20 mg is 50% and 68%, respectively. Eating slows and reduces absorption of esomeprazole, while it has no significant clinical significance. With a single daily intake of esomeprazole completely removed from the blood plasma during a break between doses. Do not cumulate. The main metabolites of esomeprazole do not affect the secretion of hydrochloric acid in the stomach. Almost 80% of the ingested dose of esomeprazole is excreted by the kidneys in the form of metabolites, and the rest - through the intestine. In urine, less than 1% of unchanged esomeprazole is found.

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

After repeated use of esomeprazole in doses of 20 mg and 40 mg, the AUC and the time to reach Cmax 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 in order to prevent relapses;
symptomatic treatment of GERD.

Peptic ulcer of the stomach and duodenum - as part of combined antibiotic therapy for the eradication of Helicobacter pylori:

duodenal ulcer associated with Helicobacter pylori;
prevention of recurrence of peptic ulcer associated with Helicobacter pylori.

Patients taking long-term non-steroidal anti-inflammatory drugs (NSAIDs):

with the purpose of healing of gastric ulcer associated with the intake of NSAIDs;
prevention of gastric ulcer and duodenal ulcer associated with the administration of NSAIDs in patients at risk.

Long-term prophylaxis of relapse of repeated bleeding from peptic ulcers (after intravenous administration of drugs that reduce the secretion of the stomach glands).

Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, incl. idiopathic hypersecretion.

Forms of release

Capsules enteric soluble 20 mg and 40 mg (sometimes mistakenly called tablets).

Instructions for use and dosing regimen

The drug is taken orally. Capsules are taken without chewing, before eating, squeezed with a small amount of liquid.

For patients with difficulty swallowing, pour the contents of the capsules into half a glass of still water, stir and drink immediately or within 30 minutes. Then again fill the glass with water halfway, rinse the walls of the glass and drink.

Do not mix the drug with other liquids, t. this can lead to the dissolution of the protective coating of pellets. Pellets should not be chewed or crushed.

Patients who can not swallow independently, the contents of the capsules should be dissolved in still water and injected esomeprazole through the nasogastric tube. It is necessary to check the conformity of the syringe for the administration of the preparation and the probe. Guidance on the preparation and administration of the drug through the nasogastric tube is given below.

Adults and teenagers over 12 years of age

Gastroesophageal reflux disease

Erosive reflux esophagitis (treatment): 40 mg once a day for 4 weeks.If, after the first course of therapy, esophagitis does not heal or symptoms persist, an additional 4-week course of treatment with esomeprazole is recommended.

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

Symptomatic treatment of GERD: 20 mg once a day - patients without esophagitis. If after 4 weeks of therapy the symptoms can not be controlled, a second examination of the patient is necessary. After eliminating the symptoms, you can continue taking Emaner's drug, i.e. Take 20 mg of the drug once a day if symptoms occur. Patients taking NSAIDs that are at risk for developing gastric or duodenal ulcers are not recommended on-demand treatment.

Adults

Stomach ulcer and duodenal ulcer

In the combination of antibacterial therapy for the eradication of Helicobacter pylori

Duodenal ulcer associated with Helicobacter pylori and prevention of recurrence of peptic ulcer associated with Helicobacter pylori: Helicobacter pylori combined eradication therapy includes Emanera 20 mg, Amoxicillin 1 g and Clarithromycin 500 mg.All medications should be taken 2 times a day for 7-14 days.

Patients taking long-term NSAIDs

Healing of gastric ulcer associated with taking NSAIDs: 20 mg or 40 mg once a day for 4-8 weeks.

Prevention of gastric ulcer and duodenal ulcer associated with the use of NSAIDs in patients at risk: the drug Emanera 20 mg or 40 mg once a day.

Prolonged prophylaxis of recurrent bleeding recurrences from peptic ulcers (after intravenous use of drugs that reduce the secretion of the gastric glands)

The drug Emanera appointed at a dose of 40 mg 1 time per day for 4 weeks after the beginning of / in the prevention of repeated bleeding.

Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, incl. idiopathic hypersecretion

The initial dose of the drug Emanera - 40 mg 2 times a day. The dose of the drug and the duration of treatment are selected individually depending on the clinical picture of the disease. The disease in most patients is controlled by taking the drug at a dose of 80 mg to 160 mg per day. If you need to use the drug Emanera more than 80 mg per day, the daily dose is divided into 2 divided doses.

Patients with impaired renal function do not need to change the dose.The experience with esomeprazole in patients with severe renal insufficiency is limited. Therefore, when prescribing the drug, such patients should be careful.

Patients with mild or moderate impairment of liver function are not required to change the dose. In severe hepatic insufficiency, the maximum daily dose should not exceed 20 mg.

Older patients do not need a dose adjustment.

Rules for the administration of the drug through the nasogastric tube:

Open the capsule and pour its contents into a special syringe. Add 25 ml of drinking water and about 5 ml of air to the syringe. For some probes, it may be necessary to dilute the preparation in 50 ml of drinking water in order to prevent the probe from clogging the 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 (pressing slightly on the piston, holding the syringe in the position with the tip up).
Insert the tip of the syringe into the probe, continuing to hold it pointed upwards.
Shake the syringe and turn it with the tip down. Immediately introduce 5-10 ml of dissolved drug into the probe.After the administration of the solution, return the syringe to its previous position and shake (the syringe must be held by the tip
up; to avoid clogging the tip).
Again, lower the syringe with the tip down and insert another 5-10 ml of solution into the probe. Repeat the procedure until the syringe is empty.
If the remainder of the preparation is in the form of a sludge in the syringe: fill the syringe with 25 ml of water and 5 ml of air and repeat the procedures described in paragraphs 5 and 6. For some probes, 50 ml of drinking water may be needed for this purpose.

Side effect

headache;
insomnia;
dizziness;
paresthesia;
drowsiness;
depression;
excitation;
hallucinations;
aggressive behavior;
bronchospasm;
abdominal pain;
constipation, diarrhea;
flatulence;
nausea, vomiting;
dryness of the oral mucosa;
stomatitis;
Candidiasis of the gastrointestinal tract;
hepatitis (with jaundice or without);
interstitial nephritis;
gynecomastia;
arthralgia;
myalgia;
muscle weakness;
dermatitis;
skin rash;
itching;
hives;
alopecia;
photosensitization;
erythema multiforme;
Stephen-Johnson syndrome;
toxic epidermal necrolysis;
leukopenia, thrombocytopenia, agranulocytosis, pancytopenia;
blurred vision;
change in taste;
hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction / anaphylactic shock);
peripheral edema;
sweating;
weakness (malaise).

Contraindications

simultaneous reception with atazanavir and nelfinavir;
children under 12 years of age (no data on effectiveness and safety);
children age over 12 years for other indications, except for GERD;
hereditary fructose intolerance, glucose-galactose malabsorption syndrome, or isomaltase sugarase deficiency;
hypersensitivity to the components of the drug;
hypersensitivity to substituted benzimidazoles.

Application in pregnancy and lactation

The use of the drug Emanera is possible only if the expected benefit for the mother exceeds the potential risk to the fetus, because There is insufficient data on the use of esomeprazole in pregnant women.

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

In studies with esomeprazole, no direct or indirect adverse effects on the development of the embryo or fetus have been found in animals.There was no direct or indirect adverse effect on the course of pregnancy, childbirth and the postnatal period of the newborn.

At present, it is not known whether esomeprazole is excreted in breast milk, therefore, do not use Emanera during lactation (breast-feeding).

Use in children

Contraindicated in children under 12 years of age (no data on efficacy and safety). Contraindicated in childhood over 12 years of age on other indications, except for GERD.

Application in elderly patients

Older patients do not need a dose adjustment.

special instructions

If you have anxious symptoms (such as a significant, spontaneous loss of body weight, repeated vomiting, dysphagia, vomiting with a trace of blood or melena), and if you suspect or identify a stomach ulcer, you must exclude a malignant tumor, because the use of the drug Emanera can reduce the severity of symptoms and delay the diagnosis.

Patients who have been taking the drug 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 of the need to see a doctor when changing the nature of the symptoms. Taking into account fluctuations in the plasma esomeprazole concentration when the drug is used in the "on demand" mode, interaction with other medicinal products should be taken into account.

When esomeprazole is used to eradicate Helicobacter pylori, the possible interaction between the components of triple therapy should be considered. Clarithromycin is a potent inhibitor of CYP3A4; therefore, contraindications and drug interactions of clarithromycin should be considered when administering triple therapy to patients taking CYP3A4-metabolized drugs such as cisapride.

The preparation of Emanera contains sucrose, therefore its use is contraindicated in patients with hereditary intolerance to fructose, glucose-galactose malabsorption syndrome or isomaltase deficiency.

Impact on the ability to drive vehicles and manage mechanisms

Emanera does not affect the management of vehicles and work with other technical devices,requiring increased concentration of attention and speed of psychomotor reactions.

Drug Interactions

The effect of esomeprazole on the pharmacokinetics of other drugs

Drugs, the absorption of which depends on the pH level

Reduction of the acidity level of gastric juice on the background of treatment with esomeprazole may lead to a change in the absorption of drugs, the absorption of which depends on the acidity of the medium. Like antacids and other drugs that reduce the secretion of the gastric glands, esomeprazole reduces the absorption of Ketoconazole and itraconazole.

The simultaneous use of omeprazole (40 mg once a day) and some antiretroviral drugs (atazanavir 300 mg / ritonavir 100 mg) in healthy volunteers is accompanied by a marked decrease in exposure to atazanavir (AUC, Cmax and Cmin in blood plasma decreased by approximately 75%.

An increase in the dose of atazanavir to 400 mg did not compensate for this decrease in exposure.

Inhibitors of the proton pump, incl. esomeprazole, should not be taken concomitantly with atazanavir.

Drugs metabolized by the isoenzyme CYP2C19

Esomeprazole inhibits CYP2C19, the main isoenzyme of esomeprazole metabolism.Thus, with the simultaneous use of esomeprazole with preparations in the metabolism of which the isoenzyme CYP2C19 participates, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, the concentration of these drugs in the blood plasma may increase and, accordingly, a reduction in their dose is required.

This is especially necessary to take into account when appointing the drug Emanera in the "on-demand" mode. Thus, with simultaneous use with esomeprazole at a dose of 30 mg, the clearance of Diazepam (substrate CYP2C19) decreases by 45%.

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

Emanera does not cause a clinically significant change in the pharmacokinetics of amoxicillin and quinidine.

The time of bleeding with simultaneous administration of Warfarin and esomeprazole at a dose of 40 mg remains within acceptable limits. However, several cases of clinically significant enhancement of MHO have been reported. It is recommended to monitor MHO in cases when the use of esomeprazole begins or stops with warfarin or other coumarin derivatives.

Simultaneous short-term use of esomeprazole and Naproxen or rofecoxib did not reveal clinically significant pharmacokinetic interaction.

The effect of drugs on the pharmacokinetics of esomeprazole

Esomeprazole is metabolized by the isoenzymes CYP2C19 and CYP3A4.

With the simultaneous use of esomeprazole with clarithromycin (500 mg twice daily) (inhibitor CYP3A4), the value of esomeprazole AUC doubles.

Simultaneous use of esomeprazole and a combined inhibitor of CYP2C19 and CYP3A4 may be accompanied by an increase in the AUC of esomeprazole by more than 2 times. Inhibitors of CYP2C19 and CYP3A4, for example, voriconazole, increased the esomeprazole AUC by 280%. Usually, in such situations, there is no need for a change in the dose of esomeprazole, but in patients with significant impairment of liver function or if prolonged therapy is necessary, the dose of esomeprazole should be reduced.

Analogues of the drug Emanera

Structural analogs for the active substance:

Nexium;
Neo text.

Analogues on the pharmacological group (agents for the treatment of gastroesophageal reflux):

Acrylase;
Aksid;
Almagel Neo;
Gastal;
Gaviscon;
Dexylant;
Digestal;
Zantak;
Zolser;
Zulbeks;
Kwamatel;
Controllers;
Lanzap;
Losek;
Metoclopramide;
Milk of magnesia;
Nolpaz;
Omez;
Omeprazole;
Omitox;
Ortanol;
Parries;
Passion;
Penzital;
Pepticum;
Ranigast;
Ranitidine;
Simesan;
Talcid;
Ulcozol;
Ulkosan;
Ultop;
Famotidine;
Phosphalugel;
Hirabesol;
Cerucal;
Cimetidine;
Cisagast;
Andrews liver salt.

If there are no analogues of the medication for the active substance, you can go to the links below for diseases, from which the corresponding drug helps, and to look at the available analogs for therapeutic effects.

Used for the treatment of diseases: gastritis, ulcer, reflux, gerb, Zollinger-Ellison syndrome, Helicobacter, duodenal ulcer, reflux esophagitis, gastric ulcer, gastroesophageal reflux disease, gastroesophageal reflux, peptic ulcer