Esomeprazole original drug name. Esomeprazole and other drugs

Esomeprazole belongs to the class proton load inhibitors , secretion blockers of hydrochloric acid . This substance is widely used as an antiulcer agent. Molar mass = 345.4 grams per mole. The chemical compound is S-isomer of omeprazole . Similar to his R-isomer , the substance specifically inhibits proton loading in parietal cells. The medicine is available in the form of tablets or capsules for oral administration, liquid for administration through nasogastric tube.

pharmachologic effect

Antiulcer .

Pharmacodynamics and pharmacokinetics

The substance reduces the activity of hydrochloric acid production in the stomach by specifically inhibiting the process of proton transport in the parietal cells of the gastrointestinal tract. The remedy itself is a weak basis and only in acidic environment goes into active form, is activated and begins to suppress H+/K+ ATPase . The drug inhibits stimulated and basal secretion HCl .

Esomeprazole begins to act 60 minutes after taking the standard dosage. With daily use of the medicine for 5 days, once a day at a dosage of 20 mg, the level of secretion of gastric acids is reduced by 90%. Clinical studies have shown that during treatment reflux esophagitis With the help of this substance, cure occurs in approximately 79% of experimental subjects within a month. In 93% of patients, cure occurred within 2 months.

When carrying out therapy with the drug according to the regimen of 20 mg 2 times a day, in combination with standard antibacterial drugs, eradication is successfully performed Helicobacter bacteria . For the treatment of uncomplicated duodenal ulcers It is enough to use this substance for 7 days.

The drug is extremely unstable in acidic environments. In a living organism, a small part of the substance passes into R-isomer . After penetration into the gastrointestinal tract or directly into the blood, the product is quickly absorbed. The maximum concentration when taking the tablet form is achieved within 60-120 minutes. Repeated dose bioavailability is 89%.

The degree of binding to blood plasma proteins is about 97%. Metabolism of the drug occurs with the participation of the system cytochrome P450 (CYP2C19) , with education demethylated And hydroxymethylated metabolites . The remaining substance is metabolized by other specific CYP3A4 isoenzymes , as a result of which sulfide derivatives are formed, which act as the main metabolites.

When taking the tablets once a day, the half-life is about 1-3 hours. The drug does not accumulate in the body; about 80% of the drug is excreted through the kidneys in the form of inactive metabolites.

In patients with a slow metabolism of this drug. means (1-2% of the population) the process is carried out by the CYP3A4 system . The average AUC in such patients is 2 times higher than in individuals with normal metabolism of Esomeprazole. The maximum concentration in blood plasma is 60% higher.

In older people, metabolism proceeds normally. For liver disease or kidney lung And medium degree severity, no dosage adjustment is required. For severe liver failure metabolic rate is reduced, and AUC is increased by 2 times.

Indications for use

The medicine is prescribed:

  • as part of complex treatment at duodenal ulcer ;
  • at erosive reflux esophagitis ;
  • as prophylactic in people who have recovered from esophagitis ;
  • in the chambers of complex, symptomatic treatment GERD ;
  • for bacteria eradication Helicobacter (in combination with antibacterial agents);
  • for prevention peptic ulcers .

Contraindications

Esomeprazole preparations are not used:

  • if available for this substance, including substituted benzimidazolam generally;
  • in combination with atazanavir ;
  • during breastfeeding;
  • in pediatric practice.

The drug is prescribed with extreme caution to pregnant women or in cases of severe renal failure.

Side effects

When using minimum therapeutic doses probability of occurrence side effects much lower.

The most frequently observed were: abdominal pain, headaches, nausea, constipation, vomiting. Less common: allergic skin reactions, dry mucous membranes, impaired visual acuity, itching of the skin, dizziness.

Rarely and very rarely, patients experienced:

  • pancytopenia , increased activity of liver enzymes;
  • anaphylactoid reactions , Stevens-Johnson syndrome ;
  • myalgia , thrombocytopenia , ;
  • leukopenia , exudative erythema multiforme .

It is also assumed that as a result of treatment with the drug, reactions that are observed during administration may develop.

Esomeprazole, instructions for use (Method and dosage)

The medicine is prescribed orally or, if taking tablets is not possible, through a nasogastric tube. Depending on the disease used various schemes dosing.

Instructions for Esomeprazole

The tablets are taken orally, whole, with a sufficient amount of neutral liquid.

For treatment erosive reflux esophagitis use 40 mg of the drug, 1 time per day. The duration of therapy is one month. If after the first course of the drug some symptoms of the disease persist or a relapse occurs, the course can be repeated. As a prophylactic agent after treatment of esophagitis, 20 mg of the drug is used, 1 time per day.

For symptomatic treatment GERD Prescribe 20 mg of the drug once a day. However, if there is no improvement in the patient’s condition within a month, it is recommended to additional examination patient and find out the causes of the ailment.

For elimination Helicobacter pylori , treatment duodenal ulcers caused by this bacterium, or to prevent relapse, the substance is prescribed in a daily dosage of 20 mg. It is also additionally recommended to use 1 gram, 0.5 g twice a day. The duration of treatment is 7 days.

As a prophylactic for long-term use NSAIDs or for treatment peptic ulcers caused by NSAIDs , the medicine is prescribed in a dosage of 20 mg, 1 time per day. The course of treatment is from 1 to 2 months.

For patients with severe liver disease daily dosage Esomeprazole should not exceed 20 mg.

If the patient has difficulty swallowing, the tablet can be dissolved in water and a suspension of microgranules can be drunk within half an hour. The granules should not be chewed, crushed or left on the walls of the glass; the entire contents of the capsule must be taken.

The medication is administered through a nasogastric tube in accordance with the instructions.

Overdose

The likelihood of developing an accidental overdose of the drug is extremely low. When deliberately taking 280 mg of the substance, an increase in the frequency and strength of manifestation is observed adverse reactions. May occur: general weakness, dizziness, heaviness and pain in the area gastrointestinal tract. A single dose of 80 mg of the substance did not lead to any negative consequences.

As treatment, maintenance therapy is carried out, eliminating unpleasant symptoms. The medicine does not have a specific antidote and is ineffective.

Interaction

As a result of treatment with the drug, a decrease in acidity is observed gastric juice, which can lead to changes in the absorption capacity of drugs depending on the pH of the stomach.

This substance inhibits the enzyme CYP2C19 , therefore the combination of the drug with , , , may lead to an increase in plasma concentrations of these drugs. It is recommended to adjust the dosage of drugs metabolized by CYP2C19 .

It is known that taking Esomeprazole does not lead to a change in PTI in patients taking the anticoagulant for a long time. However, several have been described isolated cases increase in INR with this combination.

The drug lowers plasma levels atazanavir in blood plasma.

Terms of sale

Need a recipe.

special instructions

According to clinical research, with long-term use proton load inhibitors patients are more likely to develop benign glandular cysts in the stomach. Most often, cysts disappear after stopping treatment with the drug.

Treatment with this drug may delay the diagnosis of gastrointestinal malignancies. Therefore, if there are any anxiety symptoms(weight loss, bloody vomiting, melena , stomach ulcer ) the patient should be further examined.

When carrying out therapy for more than 1 year, patients should be under the supervision of the attending physician.

It should be taken into account that under the influence of the drug the plasma concentration increases, as a result of a decrease in intragastric secretion of hydrochloric acid.

During treatment, you may drive a car or perform work that requires increased concentration attention and speed of psychomotor reactions.

During pregnancy and lactation

There is not enough data to confirm the safety of using the drug during pregnancy. However, animal studies did not reveal any embryogenic or teratogenic effects of the substance on the body. The medicine can be prescribed in a minimum dosage by the attending physician according to indications. The product is contraindicated for use during breastfeeding.

Medicines containing (Esomeprazole analogues)

Level 4 ATX code matches:

The most common structural analogues of Esomeprazole (synonyms): Neo-Zext , Esomeprazole magnesium dihydrate , , Esomeprazole Canon , .

Esomeprazole is a drug for the complex treatment of gastric diseases. Available in the form of a solution for injection and infusion, as well as in the form of tablets. We'll tell you how it works this medicine, and we will describe all its contraindications.

Doctors prescribe Esomeprazole for therapy with the following diagnoses:

  1. Reflux disease;
  2. Symptoms of esophagitis;
  3. Attacks of stomach ulcers;
  4. Disease Prevention duodenum;
  5. Temporary support for hemostasis;
  6. Prophylaxis for recurrent bleeding due to stomach ulcers;
  7. Can be used for children from 1 year of age with reflux diseases, if the oral route of administration is prohibited.

Before using the drug, you need to determine the exact dosage for a specific diagnosis. Therefore, be sure to visit a doctor and undergo all examinations.

Contraindications for use

Doctors prohibit the use of Esomeprazole only if the patient increased sensitivity and its composition. In any other cases, the drug is approved for use and is safe even for children over 1 year old.

Use of the drug during pregnancy

Research by scientists had not been conducted on this group of patients at the time of testing Esomeprazole. Therefore, there is no exact data on the reaction of the drug to the woman’s body. It is recommended to use the medicine with caution only after your doctor's permission. During breastfeeding, you should not use Esomeprazole so that its composition does not pass through the milk into the baby’s body. Otherwise, it can lead to allergies or severe poisoning.

Impact on transport management

Doctors noted that with prolonged use of Esomeprazole, problems with nervous system and blurred vision. Therefore, if you have such symptoms, you should not drive or operate mechanical devices. Patients should temporarily abandon work that requires quick reactions and increased concentration.

Drug overdose

Doctors have little experience with Esomeprazole overdose. There were cases when the patient took more than 300 mg of the drug. After this, the person had stomach problems, abdominal pain and weakness throughout the body. An antidote to the drug has not yet been discovered. Therefore, in case of an overdose, you should immediately go to the hospital and be under the supervision of doctors. The main thing is to immediately undergo symptomatic therapy and perform gastric lavage.

Side effects on the medicine

The instructions for use of Esomeprazole describe some side effects. They occur when the dosage is too high or when the patient reacts individually to the drug.

Where do they arise?Adverse reactions
Such reactions occur in the bloodThe occurrence of leukopenia;
Severe thrombocytopenia;
Agranulocytosis rarely occurs;
Manifestation of pancytopenia.
IN immune system such complications are observedHigh fever;
Allergic reaction;
The occurrence of angioedema;
The patient is in severe shock.
Such adverse reactions may begin in the psycheFrequent insomnia;
Severe agitation;
Confusion occurs;
Low mood and depression;
Headache;
Attacks of dizziness;
Feeling sleepy during the day;
Aggressive state;
Frequent hallucinations;
Change in taste sensations patient.
The following complications can be observed in the digestive area:Gastrointestinal candidiasis occurs;
Severe colitis;
Feeling of dry mouth;
Abdominal pain;
Frequent constipation;
Diarrhea occurs;
Flatulence occurs;
Attacks of nausea and vomiting;
Increased liver enzymes;
The occurrence of liver failure.
The following side effects may occur on the skin:The appearance of a rash;
Severe itching;
Hives;
Manifestation of alopecia;
The occurrence of photosensitivity;
Stevens-Johnson syndrome;
Manifestation of skin necrolysis.
Other adverse reactionsThe patient begins to sweat heavily;
Feeling unwell;
Gynecomastia occurs;
Severe myalgia;
Vertigo rarely occurs;
Vision deteriorates.

If the patient experiences any side effects, he should immediately report these symptoms to his doctor. The doctor may prescribe another drug or reduce the dose of Esomeprazole.

Method of using tablets

Esomeprazole tablets should be taken orally and washed down big amount water. The medicine should be swallowed whole and should not be chewed under any circumstances. To treat reflux disease, doctors prescribe a dosage of 40 mg per day. The standard course of treatment lasts 1 month. However, this will depend on the patient's condition and the stage of the disease. If after the first course of therapy the symptoms do not go away and the disease still persists, then the doctor prescribes Esomeprazole for another 4 weeks.

After the main therapy, it is necessary to observe prophylaxis and take 20 mg tablets once a day. The doctor will constantly monitor the patient’s condition and adjust the dosage. Even after stopping the drug, sometimes you will need to take one tablet at a time. Typically, patients take a one-time dose of Esomeprazole if there is a weak response to the symptoms of the disease.

To treat stomach ulcers and disease in the duodenum, doctors prescribe 20 mg of Esomeprazole twice a day. The course of therapy lasts about a week. After this, you need to use the drug prophylactically for another 1 week at the same dosage.

If the patient has had bleeding due to a peptic ulcer, then the doctor prescribes acid suppression treatment with Esomeprazole. It is necessary to take 40 mg of the drug per day. The course of therapy will last one month. Before this, the doctor may prescribe several injections of the drug of the same name.

For patients with gastric ulcers due to NSAID use, 20 mg of esomeprazole should be prescribed once a day. The duration of therapy ranges from 4 to 8 weeks depending on the severity of the diagnosis.

To treat Zollinger-Ellison disease, doctors prescribe 40 mg of the drug twice a day. After a couple of weeks of treatment, it is necessary to adjust the therapy individually for the patient. At emergency You can use from 80 to 150 mg of the drug per day. This dose is best divided into 2-3 approaches.

If the patient has kidney failure or problems with the liver, then the doctor should not prescribe the medicine in a dose of more than 20 mg. Otherwise, such patients will often experience adverse reactions.

Rules for using the medicinal solution

Doctors prescribe solution therapy to the patient if he is unable to take the medicine orally. To treat relux disease, the doctor prescribes a dose of 40 mg solution per day. For symptomatic therapy A dosage of 20 mg is used.

Stomach ulcer treatment is required minimum dosage at 20 mg per day. Esomeprazole can be administered intravenously, but not for too long. After a couple of days of injections, you need to switch to tablets of the same name.

To treat sudden bleeding in the stomach due to an ulcer, you need to administer 80 mg of solution as an infusion. The administration time ranges from 20 to 30 minutes. After this, administration should not be stopped for 3 days. The rate is reduced to 8 mg of the drug per 1 hour. After this effective therapy you need to switch to the tablet form of Esomeprazole.

Typically, the injection of the drug must be done at a speed of at least 3 minutes. For this, 8 mg of solution is used. Any unused amount of the drug must be disposed of immediately.

Infusions of Esomeprazole solution should be done over 20-30 minutes with a dosage of 40 mg. Be sure to read the instructions for use, which describe the rules for preparing the solution and precautions.

Features of the drug use

  1. If the patient experiences unpleasant symptoms when taking it and sharp deterioration, he should go to the hospital immediately. The doctor will prescribe a re-diagnosis, since the drug Esomeprazole may, through its action, reveal some diseases in the body;
  2. The drug reduces the absorption of vitamin B 12. Therefore, it should be prescribed with caution to patients whose body levels of this vitamin are low;
  3. In the moment long-term treatment The doctor should reduce the patient's magnesium level with other drugs. It is necessary to monitor this indicator during therapy;
  4. If you take Esomeprazole for a long time, it can increase the risk of hip and spine fractures. This is especially true for elderly patients. The risk increases by an average of 30-40 percent. To avoid this, the doctor must include vitamin D and calcium in large quantities in the therapy;
  5. The drug Esomeprazole may lead to errors in diagnosing tumors in a patient. Therefore, doctors recommend stopping taking the drug at least 5 days before the examination.

Interaction with other drugs

Before taking it, you need to know how Esomeprazole will behave together with other drugs. To do this, you need to study a number of interactions in the instructions for use:

  • Taking a PPI may increase the absorption of Esomeprazole. This may most often occur in older patients;
  • You should not take Omeprazole and Esomeprazole at the same time. This may lead to a decrease serum levels and to complications in the body;
  • Imipramine, Phenytoin and Diazepam should only be taken under the supervision of a physician. The fact is that Esomeprazole increases the concentration of these drugs in the blood. Therefore, it is necessary to adjust the dosage before treatment;
  • If the patient is taking Warfarin, then the doctor must constantly measure blood clotting and monitor the norm of this indicator. At the end of therapy, the patient should also be examined;
  • Doctors allow the parallel use of Esomeprazole and Amoxicillin. These drugs do not affect each other;
  • Esomeprazole should be used with caution with drugs that are metabolized. Negative Impact the drugs Clopidogrel and Omeprazole may help;
  • If long time take inhibitors proton pump, the patient may experience dizziness, severe arrhythmia, constant fatigue and convulsions. If you stop such drugs and leave only Esomeprazole, then all the unpleasant symptoms will go away immediately.

Be sure to tell your doctor which tablets you have taken previously and which ones you are using for this moment. This will help the specialist accurately set the dosage and stop dangerous medications.

Rules for storing medicine

Keep the solution out of the sun in a cool place. Optimal temperature for proper storage– no higher than + 25 degrees. Do not keep Esomeprazole in the refrigerator or freezer. It is important that young children are not able to obtain the medicine and take it in large doses. Shelf life – 2 years from the date of production. Under no circumstances should Esomeprazole be used if it is expired.


Before taking any medicine, carefully read the instructions for use and study a number of contraindications. To avoid mistakes when taking it, consult your doctor. Let him determine the exact dosage.

Price for the drug

You can purchase the drug Esomeprazole at any pharmacy with a prescription from a doctor. Now average price for solution - from 320 to 370 rubles per 40 mg. And Esomeprazole canon tablets can be purchased for 200-330 rubles per pack.

Proton pump inhibitors have changed ideas about the possibilities of treating gastritis, peptic ulcers and reflux esophagitis, making it possible to reduce the percentage of relapses and complications.

The article talks about Esomeprazole - the most effective means this group are given practical advice on the choice of analogues, based on the properties of the drugs and their comparison, instructions for use, prices and reviews.

Properties of the drug

Esomeprazole is a levorotatory isomer of omeprazole, an improved version of a reliable inhibitor proton pump stomach. The product reduces acidity.

The original drug of esomeprazole is Nexium, which is assigned in the form oral forms and intravenous infusions. It is used in the form of tablets of 20 and 40 milligrams and bottles with 20 mg of esomeprazole in powder form for the preparation of an infusion solution.

Oral Nexium is used to treat:

  • gastroesophageal reflux disease, esophagitis;
  • ulcers of the stomach and duodenum;
  • other erosive lesions and ulcerative processes associated with the use of anti-inflammatory drugs;
  • in Helicobacter pylori eradication schemes in combination with antibiotics;
  • gastrointestinal bleeding, Zollinger-Ellison syndrome.

Esomeprazole is used to prevent damage to the stomach and duodenum in people taking non-steroidal anti-inflammatory drugs.

The infusion form is used in cases where oral use of the drug is impossible.

Tablets are prescribed in a dose of 20-40 mg 1 time per day. In the treatment of Helicobacter pylori infection, Nexium is used twice 20 mg with antibacterial agents for a course of 1-2 weeks. Administered intravenously in the same doses for severe bleeding daily dose reaches 160 mg. For reflux disease, the course of maintenance therapy lasts up to six months.

Esomeprazole cannot be combined with clopidogrel– the main antiplatelet agent for the prevention of myocardial infarction and strokes, used by most patients with cardiac and vascular pathology.

It is not combined with diazepam, antiretroviral drugs, methotrexate.

The drug is well tolerated, occasionally unwanted effects in the form of dyspeptic disorders, swelling and drowsiness, allergic reactions are rarely noted. P contraindications are associated with age restrictions and allergies– the parenteral form of Nexium is used from the age of 18, tablets are not prescribed to children under 12 years of age, the drug is not used if its components are intolerant.

The cost of 14 tablets of 20 and 40 mg is 1500 and 2000 rubles, a bottle with 40 mg of the drug for infusion costs 600 rubles.

Inexpensive analogues of Nexium

In addition to the expensive original medicine, pharmacies sell cheap synonyms of esomeprazole and other PPIs.

Based on Esomeprazole

Generic tablet preparations of esomeprazole, identical to Nexium:

  • Neo-Zext and Emanera (Slovenia) 28 tablets of the first, 20 and 40 mg each, cost 2100 and 2600 rubles, the second drug is cheaper, 14 capsules of 20 mg each cost 220 rubles;
  • domestic generic – Esomeprazole Canon, price of 14 tablets of 20 and 40 mg – 190 and 300 rubles.

These medications completely replicate the composition and action of Nexium, have the same indications and features of use.

The drug for parenteral use is Esomeprazole-native (Nativa LLC, Russia), it is registered, but is not yet commercially available. Injection form Nexium will have to be replaced with drugs of a different composition– products based on omeprazole and pantoprazole.


Other APIs

Other proton pump inhibitors can be successfully used as a replacement for Esomeprazole: panthorazole (Controloc, Nolpaza), omeprazole (Omez), rabeprazole, lansoprazole.

Omez

A PPI drug that was the first to appear in pharmacies. Available in capsules of 10 and 20 mg, and bottles of 40 mg. Used to treat adults and children from 1 year of age. The oral form is taken 1 capsule 2 times a day.

Popular due to the optimal ratio between price and quality. 30 capsules of 20 mg and 1 bottle cost 170 rubles. Domestic Omeprazole from different manufacturers costs 3-5 times less.

Control

The original drug of pantoprazole in tablets of 20 and 40 mg and bottles of 40 mg. Prescribed 1 tablet per day. Provides strong and long-lasting acidity reduction. Has the fewest drug-drug interactions among PPIs.

Can be prescribed with clopidogrel. Parenteral form - the main proton pump inhibitor for prophylactic use in departments surgical profile. The price of 14 tablets is 350 rubles, a bottle of medicine costs 400 rubles. The generic drug Nolpaza costs 140 and 200 rubles for 14 tablets of 20 and 40 mg.

Rabeprazole

Capsules of 10 and 20 mg, taken 1 time per day. Only used in medicinal purposes, contraindicated during pregnancy and lactation. 14 capsules are sold for 100 and 150 rubles.

Lansoprazole

It has fewer indications and more restrictions - not recommended for prevention, not used at the beginning of pregnancy, during breastfeeding and for the treatment of children. Russian drug Available in capsules of 0.03 grams under the name "Epicure". Package No. 14 costs 400 rubles.

When choosing a proton pump inhibitor, you need to consider that the main drugs with the greatest effectiveness are esomeprazole and pantoprazole. In addition to effectiveness, the difference lies in drug-drug interactions and the speed of development of the effect.

In a simplified approach to drug selection, esomeprazole is recommended for young patients and pantoprozole for older people taking other medications long-term or life-long, such as clopidogrel or benzodiazepines.

In Helicobacter eradication schemes, there are no differences in the choice of PPIs; the decisive role in success combination therapy determined by a combination of antibiotics. In such cases, they are all taken 2 times a day along with antibacterial agents.

Esomeprazole(English) esomeprazole) is an antiulcer drug, a proton pump inhibitor (PPI).

Chemical compound:(S)-5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-3H-benzimidazole. Empirical formula C 17 H 19 N 3 O 3 S.

Esomeprazole - international generic name(INN) medicine. According to the pharmacological index, it belongs to the group “Proton pump inhibitors”. According to ATC, it belongs to the group “Proton pump inhibitors” and has the code A02BC05.

Indications for use of esomeprazole
Gastroesophageal reflux disease (GERD): erosive reflux esophagitis (treatment), prevention of relapse in patients with treated esophagitis, symptomatic GERD treatment. As part of combination therapy: eradication of Helicobacter pylori, duodenal ulcer associated with Helicobacter pylori, prevention of relapse of ulcers in patients with peptic ulcer stomach and duodenum associated with Helicobacter pylori.
Doses and order of taking esomeprazole
The esomeprazole tablet should be swallowed whole with liquid. Tablets must not be chewed or broken. For patients who have problems swallowing, esomeprazole tablets are dissolved in still water and the solution is administered through a nasogastric tube.

The pharmacokinetics of esomeprazole are less subject to individual fluctuations compared to the pharmacokinetics of omeprazole. This indicates a reduction in interindividual variability in acid control and, therefore, an increase in clinical predictability and reliability of pharmacotherapy using esomeprazole. Due to improved pharmacokinetics, the antisecretory effect of esomeprazole is more pronounced, faster to manifest and more stable compared to that of omeprazole. By doing daily pH-metry against the background of oral administration of 40 mg of esomeprazole or omeprazole after 12 hours, the proportion of patients with intragastric pH > 4 was 88 and 75%, respectively, and after 24 hours the proportion of patients with intragastric pH > 4 was 68.4% of all those receiving esomeprazole and 62.0 % of all those receiving omeprazole. A comparative analysis of the pharmacodynamic parameters of oral forms of esomeprazole 40 mg, pantoprazole 40 mg, rabeprazole 20 mg allowed us to conclude that esomeprazole has a fundamentally better efficacy profile. Daily pH-metry against the background of oral administration of drugs established that on the 5th day the proportion of patients with intragastric pH > 4 was 69.8% in the esomeprazole group, 44.8% in the pantoprazole group and 44.5 in the rabeprazole group % (Golovin R.A. et al.).

However, the cost of a comparable dose of esomeprazole is significantly higher than that of omeprazole. At the same time, there are studies showing that treatment of GERD with esomeprazole is more cost-effective than rabeprazole (Rudakova A.V.).


Esomeprazole has contraindications, side effects and application features; consultation with a specialist is necessary.

Included in the preparations

Included in the list (Order of the Government of the Russian Federation No. 2782-r dated December 30, 2014):

VED

ONLS

ATX:

A.02.B.C.05 Esomeprazole

Pharmacodynamics:

Antiulcer agent - 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 transforming into an 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 - the enzyme H + -K + -ATPase. Inhibits both basal and stimulated secretion of hydrochloric (hydrochloric) acid. The effect occurs 1 hour after oral administration of 20 mg or 40 mg. When used daily for 5 days at a dose of 20 mg 1 time per day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin is reduced by 90%.

 Pharmacokinetics:

Prodrug. Absorption - 50-64%, increases with reintroduction to approximately 68 and 89% for the 20 and 40 mg doses, respectively. The half-life is 0.5-1 hour. Bonding with plasma proteins is 97%. Biotransformation in the liver is predominantly CYP2C19, to a lesser extent CYP34 with the formation of inactive metabolites. With repeated administration, there is a decrease in the effect of first pass through the liver, probably associated with suppression of CYP2C19 activity. Taking equimolar doses of the S and R isomers results in higher plasma concentrations of the S rather than the R isomer. Creatinine clearance - 500-600 ml/min. Elimination by the kidneys is 70-80% (inactive metabolite), with feces 20-30% (inactive metabolite).

 Indications:

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

As part of combination therapy: eradication Helicobacter pylori, duodenal ulcer associated with Helicobacter pylori Helicobacter pylori.

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

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 to substituted benzimidazoles); simultaneous administration with atazanavir (plasma concentration of atazanavir decreases); lactation period, childhood up to 12 years of age (due to the lack of data on the effectiveness and safety of the drug in this group of patients) and children over 12 years of age for indications other than gastroesophageal reflux disease; severe renal failure (experience is limited); hereditary intolerance fructose, glucose-galactose malabsorption or sucrase-isomaltase deficiency.

 Carefully:

Pregnancy.

Before starting therapy, rule out the presence of malignant process(especially with a stomach ulcer), since treatment, masking symptoms, can delay the establishment correct diagnosis.

 Pregnancy and lactation:

Recommendations for FDA - category B. There are currently no data on the use of esomeprazole during pregnancy. When esomeprazole was administered to animals, no direct or indirect negative effects on the development of the embryo or fetus were detected. The administration of the racemic drug also did not have any negative effects on animals during pregnancy, childbirth, or during postnatal development. However, the drug should be prescribed to pregnant women only if the expected benefit to the mother exceeds possible risk for the fetus.

It is unknown whether it is released from breast milk. Do not apply.

 Directions for use and dosage:

Inside. The tablet should be swallowed whole with liquid. Tablets should not be chewed or broken.

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

Prevention of relapses in patients with cured esophagitis: 20 mg 1 time per day.

Symptomatic treatment gastroesophageal reflux disease: 20 mg 1 time per day - patients without esophagitis. If symptoms do not disappear after 4 weeks of treatment, the patient should be further examined.

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

Patients with renal failure and for elderly patients no dose adjustment is required.

In severe liver failure, 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, urticaria, dizziness, dry mouth.

 Overdose:

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

 Interaction:

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

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

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

With simultaneous use, it is possible to increase the plasma concentrations of diazepam and phenytoin, which apparently does not have clinical significance.

Digoxin - increased absorption.

 Special instructions:

If you have any alarming symptoms (for example, significant spontaneous weight loss, frequent vomiting, dysphagia, hematemesis or melena), as well as in the presence of a gastric ulcer (or if a gastric ulcer is suspected), the possibility of malignant neoplasm, since treatment with esomeprazole may lead to a smoothing of symptoms and thus delay the correct diagnosis.

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

During treatment with proton pump inhibitors, plasma gastrin concentrations increase as a result of decreased intragastric secretion of hydrochloric acid.

Patients taking proton pump inhibitors for a long time are more likely to develop glandular cysts in the stomach. These phenomena are due physiological changes as a result of inhibition of hydrochloric acid secretion. Cysts are benign and tend to disappear.

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