Nexium - instructions for use, reviews, analogs and formulations (tablets 10 mg, 20 mg and 40 mg, injections in ampoules) for treatment of ulcers and gastritis in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Nexium. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Nexium 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. Analogues of Nexium in the presence of existing structural analogues. Use to treat ulcers and gastritis in adults, children, as well as during pregnancy and lactation.Composition of the preparation.

Nexium - inhibitor of H-K-ATPase. Esomeprazole (the active substance of the preparation Nexium) is the S-isomer of omeprazole, reduces the secretion of hydrochloric acid in the stomach by specifically inhibiting the proton pump in parietal cells. The S- and R-isomer of Omeprazole have similar pharmacodynamic activity.

Mechanism of action

Esomeprazole is a weak base, accumulates and transforms into an active form in the acidic environment of the secretory tubules of parietal cells of the gastric mucosa, where the proton pump, the enzyme H-K-ATPase, is inhibited. Esomeprazole inhibits both basal and stimulated gastric secretion.

Effect on secretion of acid in the stomach

The effect of the drug develops within 1 hour after its intake in a dose of 20 mg or 40 mg. With daily intake of the drug for 5 days to 20 mg once a day. the average maximum concentration of acid in the gastric contents after stimulation with pentagastrin is reduced by 90% (when measuring the acid concentration 6-7 hours after taking the dose on the 5th day of therapy).

In patients with gastroesophageal reflux disease (GERD) and the presence of clinical symptoms after 5 days of daily intake of Nexium inside at a dose of 20 mg or 40 mg, the pH in the stomach was higher than 4 for an average of 13 and 17 hours of 24 hours.Against the background of taking the drug at a dose of 20 mg per day, the intragastric pH above 4 was maintained for 8, 12 and 16 hours in 76%, 54% and 24% of patients, respectively. For 40 mg of esomeprazole, this ratio is 97%, 92% and 56%, respectively.

A correlation was found between acid secretion and drug concentration in plasma (AUC parameter was used to estimate the concentration).

The therapeutic effect achieved by inhibiting acid secretion

When taking Nexium at a dose of 40 mg per day, reflux esophagitis is cured in approximately 78% of patients after 4 weeks of therapy and 93% after 8 weeks of therapy.

Treatment with Nexium 20 mg twice daily in combination with appropriate antibiotics for one week leads to successful eradication of Helicobacter pylori in approximately 90% of patients.

Patients with uncomplicated peptic ulcer after a weekly eradication course do not need follow-up monotherapy with antisecretory drugs for ulcer healing and symptom management.

The efficacy of Nexium in bleeding from peptic ulcers was shown in a study of patients with peptic ulcer bleeding confirmed endoscopically.

Other effects associated with inhibition of acid secretion

During treatment with antisecretory drugs, the level of gastrin in the plasma increases as a result of decreased acid secretion. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. An increase in CgA concentration may influence the results of the examinations to identify neuroendocrine tumors. To prevent this effect, it is necessary to temporarily stop taking esomeprazole 5 days before the study of the concentration of CgA.

In patients who have been receiving esomeprazole for a long time, there is an increase in the number of enterochromaffin-like cells, probably due to an increase in the level of gastrin in the plasma.

In patients receiving antisecretory drugs for a long time, the formation of glandular cysts in the stomach is more often noted. This phenomenon is due to physiological changes as a result of pronounced inhibition of acid secretion. Cysts are benign and undergo reverse development.

The use of antisecretory drugs, incl. inhibitors of the proton pump, is accompanied by an increase in the content of the microbial flora in the stomach, normally present in the gastrointestinal tract.The use of proton pump inhibitors can lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract caused by bacteria of the genus Salmonella spp. and Campylobacter spp. and in hospitalized patients, probably Clostridium difficile.

In two comparative studies with ranitidine, Nexium was more effective in healing peptic ulcers in patients receiving non-steroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors.

In two efficacy studies, Nexium showed high efficacy in preventing gastric and duodenal ulcers in patients (age group over 60 and / or peptic ulcer in the anamnesis) who received NSAIDs, including selective COX-2 inhibitors.

Composition

Esomeprazole magnesium trihydrate (esomeprazole) + auxiliary substances.

Pharmacokinetics

Esomeprazole is unstable in an acidic medium, therefore for oral administration, tablets are used containing granules of the preparation coated with a coating that is resistant to the action of gastric juice. After taking Nexium, esomeprazole is rapidly absorbed from the digestive tract.Simultaneous food intake slows down and reduces absorption of esomeprazole in the stomach, but this does not have a significant effect on the inhibition of hydrochloric acid secretion. The main metabolites of esomeprazole do not affect the secretion of gastric acid. When taking the drug inside up to 80% of the dose is excreted in the form of metabolites with urine, the rest of the amount is excreted with feces. In urine, less than 1% of unchanged esomeprazole is found.

Indications

Gastroesophageal reflux disease:

• treatment of erosive reflux esophagitis;
• long-term maintenance therapy in patients after healing of erosive reflux esophagitis to prevent relapse;
• symptomatic therapy of gastroesophageal reflux disease.

Stomach ulcer and duodenal ulcer (as part of combination therapy):

• treatment of duodenal ulcer associated with Helicobacter pylori (Helicobacter pylori);
• prevention of recurrence of peptic ulcer associated with Helicobacter pylori.

Prolonged kislotopodavlyayuschaya therapy in patients after bleeding from peptic ulcers (after / in the use of drugs which reduce the secretion of gastric glands to relapse prophylaxis).

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

• 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.

Zollinger-Ellison syndrome or other conditions characterized by pathological hypersecretion (including idiopathic hypersecretion).

Forms of release

Tablets coated with 10 mg, 20 mg and 40 mg.

Lyophilizate for the preparation of a solution for intravenous administration (injections in ampoules for injections).

Instructions for use and reception scheme

Adults and children 12 years and older

With gastroesophageal reflux disease, Nexium is prescribed for the treatment of erosive reflux esophagitis in a single dose of 40 mg once a day for 4 weeks. An additional 4-week course of therapy is recommended in those cases when after the first course there is no cure for esophagitis or the symptoms of the disease persist.

For prolonged maintenance therapy of patients with cured erosive esophagitis to prevent recurrence, the drug is prescribed 20 mg once a day.

For symptomatic therapy of gastroesophageal reflux disease without esophagitis, the drug is prescribed in a dose of 20 mg once a day.If after 4 weeks of treatment the symptoms do not disappear, you should conduct an additional examination of the patient. After eliminating the symptoms, you can go to the mode of taking the drug "as needed", i.e. Take Nexium 20 mg once a day if symptoms occur before they are withdrawn. For patients taking NSAIDs and those at risk of developing gastric or duodenal ulcers, treatment is not recommended in the "as needed" regime.

Adults

With peptic ulcer of the stomach and duodenum as part of the combination therapy for eradication of Helicobacter pylori, as well as for treatment of duodenal ulcer associated with Helicobacter pylori, and for the prevention of recurrences of peptic ulcers associated with Helicobacter pylori in patients with peptic ulcer, Nexium is prescribed in a single dose 20 mg, Amoxicillin - 1 g, Clarithromycin - 500 mg. All drugs are taken 2 times a day for 1 week.

With the aim of prolonged acid-suppressing therapy in patients who have undergone bleeding from the peptic ulcer (after IV application of antisecretory drugs, for the prevention of relapse), Nexium is prescribed at a dose of 40 mg once a day for 4 weeks after the end of intravenous therapy with antisecretory drugs.

Patients taking long-term non-steroidal anti-inflammatory drugs (NSAIDs) to heal stomach ulcers associated with NSAID intake, Nexium is prescribed at a dose of 20 mg or 40 mg once a day. The duration of treatment is 4-8 weeks.

For the prevention of gastric ulcer and duodenal ulcer associated with the administration of NSAIDs, Nexium is prescribed in a dose of 20 mg or 40 mg once a day.

In conditions characterized by pathological hypersecretion, incl. Zollinger-Ellison syndrome and idiopathic hypersecretion, the recommended initial dose of Nexium is 40 mg 2 times a day. In the future, the dose is selected individually, the duration of treatment is determined by the clinical picture of the disease. There is an experience of using the drug in doses up to 120 mg twice a day.

When the drug is prescribed for patients with impaired renal function, dose adjustment is not required. With caution apply the drug in patients with severe renal failure due to limited clinical experience in its use in this category of patients.

When Nexium is prescribed for patients with mild or moderate hepatic insufficiency, dose adjustment is notit takes. Patients with severe hepatic insufficiency used dose should not exceed 20 mg per day.

Older patients are not required to adjust the dosage regimen.

Tablets should be swallowed whole, washed down with liquid. Tablets can not be chewed or crushed. For patients with difficulty swallowing, you can dissolve the tablet in half a glass of still water (do not use other liquids, because the protective shell of microgranules can dissolve), stir until the tablet dissolves and drink the slurry of microgranules immediately or within 30 minutes. Then, again, fill the glass with water halfway, stir leftovers and drink. Do not chew or grind microgranules.

For patients who can not swallow, the tablets should be dissolved in still water and injected through a nasogastric tube. It is important that the selected syringe and probe are suitable for performing this procedure.

Administration of the drug through a nasogastric tube

1. Place the tablet in a syringe and fill the syringe with 25 ml of water and about 5 ml of air. For some probes, it may be necessary to dilute the preparation in 50 ml of drinking water,To prevent the probe from clogging the pellets with a tablet.
2. Immediately shake the syringe for about 2 minutes to dissolve the tablet.
3. Keep the syringe tipped up and make sure that the tip is not clogged.
4. Insert the tip of the syringe into the probe, continuing to hold it pointed upwards.
5. Shake the syringe and turn it with the tip down. Immediately introduce 5-10 ml of dissolved drug into the probe. After the injection, return the syringe to its previous position and shake it up (the syringe should be held up with a tip to avoid clogging the tip).
6. Turn the syringe with the tip down and insert another 5-10 ml of the drug into the probe. Repeat this operation until the syringe is empty.
7. In the case of the remainder of the preparation as a deposit in the syringe, fill the syringe with 25 ml of water and 5 ml of air and repeat the operations described in paragraph 5. For some probes, 50 ml of drinking water may be needed for this purpose.

Side effect

• headache;
• abdominal pain;
• diarrhea;
• flatulence;
• nausea, vomiting;
• constipation;
• dermatitis;
• itching;
• rash;
• hives;
• drowsiness;
• insomnia;
• dizziness;
• dry mouth;
• peripheral edema;
• hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction / anaphylactic shock);
• bronchospasm;
• leukopenia, thrombocytopenia, agranulocytosis, pancytopenia;
• depression;
• excitation;
• a taste disorder;
• stomatitis;
• Candidiasis of the gastrointestinal tract;
• alopecia;
• photosensitization;
• malaise;
• sweating;
• blurred vision;
• hallucinations;
• aggressive behavior;
• encephalopathy in patients with liver disease;
• interstitial nephritis;
• gynecomastia;
• toxic epidermal necrolysis;
• erythema multiforme.

Contraindications

• hereditary intolerance to fructose;
• glucose-galactose malabsorption;
• sugarazo-isomaltaznaya insufficiency;
• Children under 12 years of age (due to the lack of data on the effectiveness and safety of the drug in this group of patients);
• children age over 12 years according to other indications, except for gastroesophageal reflux disease;
• joint use with atazanavir and nelfinavir;
• increased sensitivity to esomeprazole, substituted benzimidazoles or other components of the drug.

Application in pregnancy and lactation

Currently, there is insufficient data on the use of Nexium in pregnancy. The administration of the drug to such patients is possible only if the expected benefit to the mother exceeds the potential risk to the fetus.

The results of epidemiological studies of omeprazole, which is a racemic mixture, showed no fetotoxic effect or impaired fetal development.

In experimental animal studies, no adverse effects of esomeprazole on embryo or fetal development have been identified. The introduction of the racemic preparation also did not have any negative effect on the course of pregnancy, childbirth and on the period of postnatal development in animals.

It is currently unknown whether esomeprazole is released in breast milk, therefore, should not be given Nexium during breastfeeding.

special instructions

If any alarming symptoms (including significant spontaneous loss of body weight, repeated vomiting, dysphagia, vomiting with blood or melena), and in the presence of gastric ulcers (or suspected stomach ulcer) should exclude the presence of cancer,Since treatment with Nexium can lead to a smoothing of the symptoms and delay the diagnosis.

In rare cases, patients who had been taking omeprazole for a long time, at histological examination of biopsy specimens of the mucous membrane of the body of the stomach, showed atrophic gastritis.

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

Patients on the "as needed" therapy regimen should be instructed to contact their physician if the symptoms change. Taking into account the fluctuations in the plasma esomeprazole concentration when the drug is administered in the "if necessary" therapy regimen, the interaction of the drug with other drugs should be taken into account.

When Nexium is prescribed for the eradication of Helicobacter pylori, the possibility of drug interaction for all components of triple therapy should be considered. Clarithromycin is a potent inhibitor of CYP3A4, therefore, in the appointment of eradication therapy to patients receiving other drugs metabolized with CYP3A4 (eg, cisapride),it is necessary to take into account possible contraindications and interaction of clarithromycin with these drugs.

Tablets contain sucrose, therefore, Nexium should not be administered to patients with hereditary intolerance to fructose, glucose-galactose malabsorption or sugar-isomaltase deficiency.

Impact on the ability to drive vehicles and manage mechanisms

Due to the fact that during the therapy with Nexium, dizziness, blurred vision and drowsiness may occur, caution should be exercised when driving vehicles and other mechanisms.

Drug Interactions

Effect of esomeprazole on the pharmacokinetics of other drugs

Decreased secretion of hydrochloric acid in the stomach against 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 other drugs that reduce the acidity of gastric juice, treatment with esomeprazole may lead to a decrease in the absorption of ketoconazole, Itraconazole and erlotinib and increase the absorption of drugs such as digoxin.Joint omeprazole 20 mg once a day and Digoxin increases the bioavailability of digoxin by 10% (the bioavailability of digoxin was increased by up to 30% in 2 of 10 patients).

It has been shown that omeprazole interacts with some antiretroviral drugs. The mechanisms and clinical significance of this interaction are not always known. An increase in pH on the background of omeprazole therapy may affect the absorption of antiretroviral drugs. It is also possible to interact at the level of the isoenzyme CYP2C19. In the combined use of omeprazole and some antiretroviral drugs, such as atazanavir and nelfinavir, against the background of omeprazole therapy, there is a decrease in their concentration in the serum. Therefore, their simultaneous application is not recommended. The combined use of omeprazole (40 mg once daily) with atazanavir 300 mg / ritonavir 100 mg in healthy volunteers resulted in a significant decrease in the bioavailability of 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 the effects of omeprazole on the bioavailability of atazanavir.

With the simultaneous use of omeprazole and saquinavir, there was an increase in the concentration of saquinavir in the serum, with the appointment with some other antiretroviral drugs, their concentration did not change. Given the similar pharmacokinetic and pharmacodynamic properties of omeprazole and esomeprazole, the combined use of esomeprazole with antiretroviral drugs such as atazanavir and nelfinavir is not recommended.

Esomeprazole inhibits CYP2C19, the main enzyme involved in its metabolism. Accordingly, the joint use of esomeprazole with other drugs in the metabolism of which CYP2C19 (such as diazepam, citalopram, imipramine, clomipramine, phenytoin) takes part, can lead to an increase in plasma concentrations of these drugs, which in turn will lead to the need for dose reduction . It is especially important to remember this interaction when applying Nexium in the "if necessary" therapy regimen. With the joint ingestion of esomeprazole in a dose of 30 mg and diazepam, which is a substrate of CYP2C19, a decrease in clearance of Diazepam by 45% is noted.

The use of esomeprazole at a dose of 40 mg caused an increase in the residual concentration of phenytoin in patients with epilepsy by 13%.In this regard, it is recommended to monitor the concentration of phenytoin in the plasma at the beginning of treatment with esomeprazole and when it is withdrawn.

The use of omeprazole 40 mg once a day led to an increase in AUC and Cmax voriconazole (substrate CYP2C19) by 15% and 41%, respectively.

The simultaneous administration of Warfarin with esomeprazole at a dose of 40 mg does not lead to a change in coagulation time in patients taking warfarin for a long time. However, several cases of clinically significant increases in INR have been reported with the combined use of warfarin and esomeprazole. It is recommended to monitor MHO at the beginning and after the end of the joint use of esomeprazole and warfarin or other coumarin derivatives.

Joint use of cisapride with esomeprazole at a dose of 40 mg leads to an increase in the pharmacokinetic parameters of cisapride in healthy volunteers: AUC by 32% and T1 / 2 by 31%, but Cmax of cisapride in plasma does not change significantly. The slight prolongation of the QT interval, which was observed with monotherapy with cisapride, did not increase with the addition of Nexium.

Some patients reported increased concentrations of Methotrexate against a background of combined use with proton pump inhibitors.When appointing methotrexate in high doses, the possibility of temporary withdrawal of esomeprazole should be considered.

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

Studies evaluating the joint use of esomeprazole and Naproxen or rofecoxib have not revealed a clinically significant pharmacokinetic interaction.

The effect of drugs on the pharmacokinetics of esomeprazole

The isozymes CYP2C19 and CYP3A4 are involved in the metabolism of esomeprazole. The combined use of esomeprazole with clarithromycin (500 mg twice daily), which inhibits CYP3A4, leads to an increase in the AUC of esomeprazole by a factor of 2. The combined use of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19, for example, voriconazole, can lead to a more than 2-fold increase in the value of esomeprazole AUC. In such cases, dosage adjustment of esomeprazole is not required. Correction of the dose of esomeprazole may be required in patients with severe impairment of liver function and with prolonged use.

Drugs that induce isoenzymes CYP2C19 and CYP3A4, such as rifampicin and St. John's wort preparations,when combined with esomepromazole may lead to a decrease in the concentration of esomeprazole in the blood plasma by accelerating the metabolism of esomeprazole.

Analogues of the medicinal product Nexium

Structural analogs for the active substance:

• Esomeprazole.

Analogues for the pharmacological group (proton pump inhibitors):

• Acrylase;
• Vero Omeprazole;
• Gastrozole;
• Demeprazole;
• Zhelezolic;
• A zerocide;
• Zipantola;
• Zolispan;
• Zolser;
• Zulbeks;
• Controllers;
• Chrismel;
• Crosatide;
• Lanzabel;
• Lanzap;
• Lansoptol;
• Lansoprazole;
• Lansofed;
• Lancid;
• Losek;
• Loenzar sanovel;
• Nolpaz;
• Omez;
• Omez Insta;
• Omesol;
• Omekaps;
• Omeprazole;
• Omepros;
• Omeface;
• OmiPix;
• Ontime;
• Ortanol;
• Ozid;
• Pantaz;
• Panum;
• Parries;
• Pepazol;
• Pepticum;
• Pomez;
• Puloreph;
• Rabelock;
• Rabeprazole;
• Romesque;
• Sunpras;
• Ulzol;
• Ulcozol;
• Ulter;
• Ultop;
• Hirabesol;
• Helicid;
• Helol;
• Cisagast;
• Epicurus.

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