Ricochet Nexium. Nexium - indications for use

Compound

One vial contains:

Active Ingredients:

Esomeprazole sodium 42.5 mg, equivalent to 40 mg esomeprazole.

Auxiliary ingredients:

Ethylenediaminetetraacetic acid disodium salt 1.5 mg, sodium hydroxide 0.2-1 mg, nitrogen for injection, water for injection.

Description

Lyophilisate of white or almost white color in the form of a compressed mass.

pharmachologic effect

Esomeprazole is the S-isomer of omeprazole and reduces gastric acid secretion by specific inhibition of the proton pump in gastric parietal cells. The S- and /^-isomer of omeprazole have similar pharmacodynamic activity.

Mechanism of action

Esomeprazole is a weak base that becomes active in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa and inhibits the proton pump - the enzyme H + / K + - ATPase, while inhibiting both basal and stimulated secretion of hydrochloric acid.

Influence on the secretion of hydrochloric acid in the stomach

After oral administration of esomeprazole at a dose of 20 mg or 40 mg for 5 days, patients with gastroesophageal reflux disease (GERD) with symptoms showed a decrease in the secretion of hydrochloric acid in the stomach for most of the day. The effect was the same when administered intravenously and when taken orally. Analysis of pharmacokinetic data revealed the relationship. between inhibition of hydrochloric acid secretion and plasma concentration of the drug: after oral administration (the concentration-time curve parameter was used to estimate the concentration).

Against the background of intravenous administration of 80 mg of esomeprazole over 30 minutes to healthy volunteers, followed by prolonged intravenous infusion of esomeprazole at a dose of 8 mg / h for 23.5 hours, the gastric pH value was above 4 for an average of 21 hours, and above 6 - within 11-13 hours.

Therapeutic effect achieved as a result of inhibition of hydrochloric acid secretion

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

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

Other effects associated with inhibition of hydrochloric acid secretion During treatment with drugs that reduce the secretion of gastric glands, plasma gastrin concentration increases as a result of a decrease in hydrochloric acid secretion.

In patients taking esomeprazole orally for a long period of time, there was an increase in the number of enterochromaffin-like cells, which is probably associated with an increase in plasma gastrin concentration.

In patients taking orally for a long time drugs that reduce the secretion of the glands of the stomach, the formation of glandular cysts in the stomach was more often noted. These phenomena are due to physiological changes as a result of inhibition of the secretion of hydrochloric acid. The cysts are benign and regress.

The use of drugs that suppress the secretion of hydrochloric acid in the stomach, including proton pump inhibitors, is accompanied by an increase in the content of microbial flora in the stomach, which is normally present in the gastrointestinal tract. The use of proton pump inhibitors may 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.

Pharmacokinetics

Absorption and distribution

The apparent volume of distribution at steady state in healthy people is approximately 0.22 l/kg of body weight. Esomeprazole binds to plasma proteins by 97%.

Metabolism and excretion

Esomeprazole undergoes complete metabolism with the participation of the cytochrome P450 system. The main part is metabolized with the participation of a specific polymorphic CYP2C19 isoenzyme, with the formation of hydroxylated and desmethylated metabolites of esomeprazole. The metabolism of the remaining part is carried out by the CYP3A4 isoenzyme; in this case, a sulfo derivative of esomeprazole is formed - the main metabolite determined in plasma.

The parameters below reflect mainly the nature of the pharmacokinetics in patients with increased activity of the CYP2C19 isoenzyme.

The total plasma clearance is approximately 17 l / h after a single dose - x of the drug and 9 l / h - with repeated doses. The elimination half-life is 1.3 hours with repeated doses of the drug once a day. Area under the concentration curve.

Time "(AUC) increases with repeated administration. This increase is time- and dose-dependent, which is a consequence of a decrease in first-pass metabolism through the liver, as well as a decrease in systemic clearance, probably caused by the fact that esomeprazole and / or its sulfo derivative inhibit the CYP2C19 isoenzyme.

With daily intake once a day, esomeprazole is completely eliminated from the plasma in the interval between doses, there is no tendency for the drug to accumulate.

With repeated intravenous administration of esomeprazole at a dose of 40 mg, the average peak plasma concentration is approximately 13.6 µmol / l. When ingested at similar doses, the mean plasma peak concentration is 4.6 µmol/L. Slightly less increase in total exposure (approximately 30%) with intravenous administration of esomeprazole compared with oral administration.

With intravenous administration of esomeprazole at doses of 40 mg, 80 mg and 120 mg for 30 minutes. followed by intravenous administration at a dose of 4 mg / h or 8 mg / h for 23.5 h, a linear dependence of AUC on the administered dose was shown.

The main metabolites of esomeprazole do not affect the secretion of hydrochloric acid in the stomach. When administered orally, up to 80% of the dose of the drug is excreted as metabolites by the kidneys, the other part - by the intestines. Less than 1% of unchanged esomeprazole is found in the urine.

Features of pharmacokinetics in some groups of patients Approximately 2.9 ± 1.5% of the population has reduced activity of the CYP2C19 isoenzyme. In such patients, the metabolism of esomeprazole is mainly carried out by CYP3A4, and with repeated oral administration of 40 mg of esomeprazole once a day, the average area under the concentration-time curve is 100% higher than in patients with increased activity of the CYP2C19 isoenzyme. Mean values ​​of peak plasma concentrations in patients with reduced activity of the isoenzyme are increased by approximately 60%. Similar differences were found with intravenous administration of esomeprazole. The noted features do not affect the dose and route of administration of esomeprazole.

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

In patients with mild to moderate hepatic impairment, the metabolism of esomeprazole may be impaired. In patients with severe hepatic impairment, the metabolic rate is reduced, resulting in a doubling of the area under the concentration-time curve for esomeprazole. There is no trend towards cumulation of esomeprazole and its main metabolites when taking the drug once a day.

The study of pharmacokinetics in patients with reduced renal function has not been conducted. Since not esomeprazole itself is excreted through the kidneys, but its metabolites, it can be assumed that the metabolism of esomeprazole in patients with impaired renal function does not change.

Indications for use

As an alternative to oral therapy when it is not possible

For gastroesophageal reflux disease in patients with esophagitis and/or severe symptoms of reflux disease

For the healing of peptic ulcers associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs)

For the prevention of peptic ulcers associated with the use of VPDP in patients at risk

To prevent recurrence of bleeding from a peptic ulcer, endoscopic hemostasis has ripened

Contraindications

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

Children's age (due to the lack of data on the use of the drug in this group of patients).

Esomeprazole should not be co-administered with atazanavir and nelfinavir (see section "Interaction with other medicinal products and other forms of interaction").

With caution: patients with severe renal insufficiency.

Pregnancy and lactation

There are currently limited data on the use of esomeprazole during pregnancy. Animal studies have not revealed any direct or indirect negative effects of Nexium® on the development of the embryo or fetus. The introduction of the racemic mixture of the drug also did not have any negative effect on animals during pregnancy, childbirth, and also during postnatal development.

The drug should be prescribed during pregnancy only if the expected benefit to the mother outweighs the possible risk to the fetus.

There are no data on the use of the drug by women during lactation. It is not known whether esomeprazole is excreted in breast milk, so Nexium® should not be prescribed during breastfeeding.

Dosage and administration

adults

As an alternative to oral therapy when it is not possible. If oral therapy is not possible, patients may be recommended parenterally esomeprazole at a dose of 20-40 mg 1 time per day.

For the healing of peptic ulcers associated with the use of NSAIDs, esomeprazole at a dose of 20 mg 1 time per day is recommended.

For the prevention of peptic ulcers associated with the use of NSAIDs, esomeprazole is recommended at a dose of 20 mg 1 time per day.

As a rule, the period of treatment with the intravenous form is short, the patient should be transferred to oral administration of the drug as soon as possible.

To prevent recurrence of bleeding from a peptic ulcer After endoscopic hemostasis, esomeprazole at a dose of 80 mg as an intravenous infusion over 30 minutes is recommended, followed by an extended intravenous infusion of esomeprazole at a dose of 8 mg / h for 3 days (72 hours). After the end of parenteral therapy, antisecretory therapy (eg, esomeprazole 40 mg 1 time per day for 4 weeks) is recommended to suppress acid secretion.

Injection Dose 40 mg

The prepared solution of esomeprazole is administered intravenously for at least 3 minutes.

Dose 20 mg

Half of the prepared solution of esomeprazole is administered intravenously for at least 3 minutes. Unused solution residue must be disposed of.

Infusion Dose 40 mg

The prepared solution of esomeprazole is administered as an intravenous infusion over 10-30 minutes.

Dose 20 mg

Half of the prepared solution of esomeprazole is administered as an intravenous infusion over 10-30 minutes. Unused solution residue must be disposed of.

Dose 80 mg

The prepared solution of esomeprazole is administered as an intravenous infusion over 30 minutes.

Dose 8 mg/kg

The prepared solution of esomeprazole is administered as an extended intravenous infusion over 71.5 hours (8 mg/hour). (Conditions and shelf life of the prepared solution - see the section ''Preparation of the solution'.)

Impaired kidney function

Dose adjustment of Nexium® in patients with impaired renal function is not required. Due to the limited experience of using Nexium® in patients with severe renal insufficiency, caution should be exercised when treating such patients (see the Pharmacokinetics section).

Impaired liver function

GERD: dose adjustment of Nexium® in patients with mild to moderate hepatic impairment is not required. In patients with severe hepatic impairment, the maximum daily dose is 20 mg (see the Pharmacokinetics section),

Bleeding from a peptic ulcer, dose adjustment of Nexium® in patients with mild to moderate hepatic impairment is not required. In patients with severely impaired liver function, the following Nexium® administration regimen is recommended: 80 mg as an intravenous infusion over 30 minutes, followed by an extended intravenous infusion at a maximum dose of 4 mg / h for 71.5 hours (see section "Pharmacokinetics" ).

Elderly patients.

Dose adjustment of Nexium® in elderly patients is not required.

Solution preparation

The degradation of the prepared solution mainly depends on the pH value, and therefore only 0.9% sodium chloride solution for intravenous administration should be used to dissolve the drug.

The prepared solution should not be mixed or administered together with other drugs.

Before use, the solution should be evaluated visually for the absence of visible mechanical impurities and discoloration. Only a clear solution may be used. The prepared solution is recommended to be administered immediately after preparation (from a microbiological point of view).

The prepared solution should be used within 12 hours. Store at a temperature not exceeding 30°C.

When prescribing 20 mg of esomeprazole, half of the prepared solution is injected. Unused solution residue must be disposed of.

Injections

Solution for injection is prepared by adding 5 ml of 0.9% sodium chloride solution for intravenous administration to a vial of esomeprazole. The diluted solution of esomeprazole is a clear, colorless to pale yellow liquid.

The infusion solution is prepared by dissolving the contents of one vial of esomeprazole in 100 ml of 0.9% sodium chloride solution for intravenous administration. The diluted solution of esomeprazole is a clear, colorless to pale yellow liquid.

Infusion 80 mg

The infusion solution is prepared by dissolving the contents of two vials of esomeprazole 40 mg in 100 ml of 0.9% sodium chloride solution for intravenous administration.

Side effect

The following are the side effects observed with intravenous and oral use of Nexium® during clinical trials and in post-marketing studies of Nexium® for oral administration.

Individual cases of irreversible visual impairment have been reported with intravenous administration of omeprazole to critically ill patients, especially with the introduction of high doses, a causal relationship with the drug has not been established.

Overdose

To date, extremely rare cases of intentional overdose have been described. Gastrointestinal weakness and symptoms have been described with oral administration of 280 mg esomeprazole. A single dose of 80 mg of esomeprazole orally and intravenous administration of 308 mg for 24 hours did not cause any negative effects.

There is no known antidote for esomeprazole. Esomeprazole binds well to plasma proteins, so dialysis is ineffective. In case of overdose, symptomatic and general supportive treatment should be carried out.

Interaction with other drugs

Effect of esomeprazole on the pharmacokinetics of other medicinal products Decreased gastric acidity during treatment with esomeprazole may lead to a decrease or increase in the absorption of other drugs, the mechanism of absorption of which depends on the acidity of the environment. As with other drugs that suppress the secretion of hydrochloric acid or antacids, treatment with esomeprazole may lead to a decrease in the absorption of ketoconazole or itraconazole.

Omeprazole has been shown to interact with some antiretroviral drugs. The mechanisms and clinical significance of these interactions are not always known. An increase in pH during therapy with omeprazole may affect the absorption of antiretroviral drugs. Interaction at the level of CYP2C19 is also possible. With the joint appointment of omeprazole and certain antiretroviral drugs, such as atazanavir and nelfinavir, during therapy with omeprazole, there is a decrease in their serum concentration. Therefore, their simultaneous use is not recommended. Co-administration of omeprazole (40 mg once daily) with atazanavir 300 mg/ritonavir 100 mg to healthy volunteers resulted in a significant decrease in the bioavailability of atazanavir (area under the concentration-time curve, maximum (Cmax) and minimum (Cmin) concentrations 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.

With the simultaneous appointment of omeprazole and saquinavir, an increase in the concentration of saquinavir in serum was noted, when administered with some other antiretroviral drugs, their concentration did not change. Given the similar pharmacokinetic and pharmacodynamic properties of omeprazole and esomeprazole, co-administration of esomeprazole with antiretrovirals such as atazanavir and nelfinavir is not recommended.

Esomeprazole inhibits CYP2C19, the main isoenzyme involved in its metabolism. Co-administration of esomeprazole with other drugs metabolized by CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., may lead to an increase in plasma concentrations of these drugs and require a dose reduction. With oral co-administration of 30 mg of esomeprazole and diazepam, the clearance of diazepam, which is a substrate of CYP2C19, is reduced by 45%.

When esomeprazole was taken orally at a dose of 40 mg and phenytoin in patients with epilepsy, the residual plasma concentration of phenytoin increased by 13%. In this regard, it is recommended to control the concentration of phenytoin in plasma at the beginning of treatment with esomeprazole and when it is canceled. The administration of omeprazole at a dose of 40 mg once a day led to an increase in the area under the concentration-time curve and Cmax of voriconazole (CYP2C19 substrate) by 15% and 41%, respectively.

When prescribing oral esomeprazole at a dose of 40 mg to patients receiving warfarin, coagulation time remained within acceptable values. However, several cases of a clinically significant increase in the INR index (international normalized ratio) have been reported with the combined use of warfarin and esomeprazole. In this regard, monitoring is recommended at the beginning and at the end of the combined use of these drugs.

In healthy volunteers, co-administration of esomeprazole 40 mg and cisapride increased the area under the concentration-time curve (AUC) by 32% and increased the half-life (t 1/2) for cisapride by 31%; peak plasma concentrations of cisapride did not change significantly. A slight prolongation of the QT interval, which was observed with cisapride monotherapy, did not increase with the addition of esomeprazole (see section "Special Instructions").

It has been shown that esomeprazole does not cause clinically significant changes in the pharmacokinetics of amoxicillin and quinidine.

Studies on the interaction of esomeprazole with other drugs when administered intravenously at high doses (80 mg followed by a dose of 8 mg / h) have not been conducted. It is possible that with this dosing regimen, esomeprazole has a more pronounced effect on the pharmacokinetics of CYP2C19 substrates. Therefore, patients should be under close medical supervision during intravenous administration of esomeprazole.

The effect of drugs on the pharmacokinetics of Nexium®

Esomeprazole is metabolized by CYP2C19 and CYP3A4. Co-administration of esomeprazole and the CYP3A4 inhibitor kparithromycin (500 mg twice daily) resulted in a two-fold increase in the AUC for esomeprazole. Co-administration of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19, such as voriconazole, may result in more than a 2-fold increase in the AUC value for esomeprazole. As a rule, in such cases, no dose adjustment of esomeprazole is required. Dose adjustment of esomeprazole may be required in patients with severe hepatic impairment and long-term use.

To dissolve the drug, only the drugs mentioned in the "Preparation of the solution" section should be used.

Application features

If any worrisome symptoms are present (eg, such as significant spontaneous weight loss, recurrent vomiting, dysphagia, hematemesis, or melena), or if a stomach ulcer is present (or if a stomach ulcer is suspected), malignancy should be ruled out because treatment with Nexium® may lead to symptomatic relief and delay diagnosis.

In rare cases, in patients who have taken omeprazole for a long time, a histological examination of biopsy specimens of the mucous membrane of the body of the stomach revealed atrophic gastritis.

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

A bottle without a carton can be stored under room lighting for no more than 24 hours.

Best before date

Do not use after the expiry date stated on the packaging.

• 28 bags in a pack 7 - blisters (1) - packs of cardboard. 7 - blisters (2) - packs of cardboard. 7 - blisters (4) - cardboard packs 7 - blisters (2) - cardboard packs. Lyophilizate for the preparation of a solution for intravenous administration, 40 mg in a glass bottle of 5 ml - 10 pcs in a pack. Film-coated tablets - 14 pcs per pack. Film-coated tablets - 28 pcs per pack. Coated tablets 20mg - 14 pcs per pack.

Description of the dosage form

• Dosage form: enteric-coated pellets and granules for suspension for oral administration. Pale yellow granules of various sizes (the bulk are finely divided granules and larger ones are pellets). Brownish granules may occur. Lyophilizate in the form of a compressed mass of white or almost white color. Pink film-coated tablets, oblong, biconvex, debossed with "40 mg" on one side and "A/EI" in the form of a fraction on the other; on a break - white color with yellow impregnations (croup type). Pink film-coated tablets, oblong, biconvex, debossed with "40 mg" on one side and "A/EI" in the form of a fraction on the other; on a break - white color with yellow impregnations (croup type). Light pink film-coated tablets, oblong, biconvex, debossed with "20 mG" on one side and "A / EH" in the form of a fraction on the other; on a break - white color with yellow impregnations (croup type). Light pink film-coated tablets, oblong, biconvex, debossed with "20 mG" on one side and "A / EH" in the form of a fraction on the other; on a break - white color with yellow impregnations (croup type). Light pink film-coated tablets, oblong, biconvex, debossed with "20 mG" on one side and "A / EH" in the form of a fraction on the other; on a break - white color with yellow impregnations (croup type).

pharmachologic effect

Esomeprazole is the S-isomer of omeprazole and reduces gastric acid secretion by specific inhibition of the proton pump in gastric parietal cells. The S- and R-isomers of omeprazole have similar pharmacodynamic activity. Mechanism of action Esomeprazole is a weak base that passes into the active form in the strongly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa and inhibits the proton pump - the enzyme H + / K + ATPase, while inhibiting both basal and stimulated secretion of hydrochloric acid. Influence on gastric acid secretion The action of esomeprazole develops within 1 hour after oral administration of 20 or 40 mg. With daily administration of the drug for 5 days at a dose of 20 mg 1 time per day, the average Cmax of hydrochloric acid after stimulation with pentagastrin is reduced by 90% (when measuring the acid concentration 6-7 hours after taking the drug on the 5th day of therapy). In symptomatic GERD patients, after 5 days of daily oral administration of esomeprazole at a dose of 20 or 40 mg, intragastric pH above 4 was maintained for an average of 13 and 17 hours out of 24 hours. While taking esomeprazole at a dose of 20 mg / day the value of intragastric pH above 4 was maintained for at least 8, 12 and 16 hours in 76, 54 and 24% of patients, respectively. For 40 mg esomeprazole, this ratio was 97%, 92% and 56%, respectively. A correlation was found between the plasma concentration of the drug and the inhibition of hydrochloric acid secretion (the AUC parameter was used to estimate the concentration). The therapeutic effect achieved as a result of inhibition of the secretion of hydrochloric acid. When taking Nexium® at a dose of 40 mg, healing of reflux esophagitis occurs in approximately 78% of patients after 4 weeks of therapy and in 93% after 8 weeks of therapy. Treatment with Nexium® at a dose of 20 mg 2 times a day 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 require subsequent monotherapy with drugs that reduce the secretion of the gastric glands to heal the ulcer and eliminate symptoms. The efficacy of Nexium® in peptic ulcer bleeding was shown in a study in patients with endoscopically confirmed peptic ulcer bleeding. Other effects associated with inhibition of hydrochloric acid secretion. During treatment with drugs that reduce the secretion of the gastric glands, the concentration of gastrin in plasma increases as a result of a decrease in 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 affect the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, therapy with proton pump inhibitors should be suspended 5-14 days before the study of CgA concentration. If during this time the concentration of CgA has not returned to normal, the study should be repeated. In children and adult patients who have received esomeprazole for a long time, there is an increase in the number of enterochromaffin-like cells, probably associated with an increase in plasma gastrin concentration. This phenomenon has no clinical significance. In patients who have been taking drugs that reduce the secretion of the gastric glands for a long time, the formation of glandular cysts in the stomach is more often noted. These phenomena are due to physiological changes as a result of a pronounced inhibition of the secretion of hydrochloric acid. The cysts are benign and regress. The use of drugs that suppress the secretion of hydrochloric acid in the stomach, incl. proton pump inhibitors, accompanied by an increase in the content of microbial flora in the stomach, which is normally present in the gastrointestinal tract. The use of proton pump inhibitors may 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 probably Clostridium difficile (in hospitalized patients). In the course of two comparative studies conducted with ranitidine, Nexium® showed better efficacy in the healing of gastric ulcers in patients treated with NSAIDs, including selective COX-2 inhibitors. In two studies, Nexium® showed high efficacy in preventing gastric and duodenal ulcers in patients treated with NSAIDs (age group - over 60 years and / or with a history of peptic ulcer), including selective COX inhibitors

Pharmacokinetics

absorption and distribution. Esomeprazole is unstable in an acidic environment, therefore, tablets containing granules of the drug, the shell of which is resistant to the action of gastric juice, are used for oral administration. Under in vivo conditions, only a small part of esomeprazole is converted to the R-isomer. The drug is rapidly absorbed: Cmax in plasma is reached 1-2 hours after administration. The absolute bioavailability of esomeprazole after a single dose of 40 mg is 64% and increases to 89% against the background of daily administration 1 time per day. For a dose of 20 mg of esomeprazole, these figures are 50 and 68%, respectively. Vss in healthy people is approximately 0.22 l/kg. Esomeprazole binds to plasma proteins by 97%. Eating slows down and reduces the absorption of esomeprazole in the stomach, but this does not significantly affect the effectiveness of inhibition of hydrochloric acid secretion. Metabolism and excretion. Esomeprazole is metabolized with the participation of the cytochrome P450 system. The main part is metabolized with the participation of a specific polymorphic isoenzyme CYP2C19, with the formation of hydroxylated and desmethylated metabolites of esomeprazole. The metabolism of the remaining part is carried out by the CYP3A4 isoenzyme; in this case, a sulfo derivative of esomeprazole is formed, which is the main metabolite determined in plasma. The parameters below reflect mainly the nature of the pharmacokinetics in patients with increased activity of the CYP2C19 isoenzyme. The total Cl after a single dose of the drug is approximately 17 l / h, after multiple doses - 9 l / h. T1 / 2 - 1.3 hours with a systematic intake 1 time per day. AUC increases with repeated administration of esomeprazole. The dose-dependent increase in AUC with repeated administration of esomeprazole is non-linear, which is a consequence of a decrease in metabolism during the first passage through the liver, as well as a decrease in systemic clearance, probably caused by inhibition of the CYP2C19 isoenzyme by esomeprazole and / or its sulfo derivative. When taken once a day, esomeprazole is completely eliminated from the blood plasma between doses and does not accumulate. The main metabolites of esomeprazole do not affect the secretion of gastric acid. When administered orally, up to 80% of the dose is excreted as metabolites in the urine, the rest is excreted in the faeces. Less than 1% of unchanged esomeprazole is found in the urine. Features of pharmacokinetics in some groups of patients Patients with reduced activity of the CYP2C19 isoenzyme. Approximately (2.9±1.5)% of the population has reduced activity of the CYP2C19 isoenzyme. In such patients, the metabolism of esomeprazole is mainly carried out as a result of the action of CYP3A4. With the systematic administration of 40 mg of esomeprazole once a day, the average AUC value is 100% higher than the value of this parameter in patients with increased activity of the CYP2C19 isoenzyme. The average values ​​of Cmax in plasma in patients with reduced activity of the isoenzyme are increased by approximately 60%. These features do not affect the dose and route of administration of esomeprazole. Elderly age. In elderly patients (71–80 years), the metabolism of esomeprazole does not undergo significant changes. Floor. After a single dose of 40 mg of esomeprazole, the average AUC value in women is 30% higher than that in men. With daily administration of the drug 1 time per day, there are no differences in pharmacokinetics in men and women. These features do not affect the dose and route of administration of esomeprazole. Liver failure. In patients with mild to moderate hepatic insufficiency, the metabolism of esomeprazole may be impaired. In patients with severe hepatic insufficiency, the metabolic rate is reduced, which leads to an increase in the AUC value for esomeprazole by 2 times. Renal failure. The study of pharmacokinetics in patients with renal insufficiency has not been conducted. Since not esomeprazole itself is excreted through the kidneys, but its metabolites, it can be assumed that the metabolism of esomeprazole in patients with renal insufficiency does not change. Childhood. In children aged 12–18 years, after repeated administration of 20 and 40 mg of esomeprazole, the values ​​of AUC and Tmax in blood plasma were similar to those of AUC and Tmax in adults.

Special conditions

If there are any warning signs (such as significant spontaneous weight loss, recurrent vomiting, dysphagia, vomiting of blood or melena), or if a stomach ulcer is present (or if a stomach ulcer is suspected), malignancy should be ruled out because treatment drug Nexium® can lead to a smoothing of symptoms and delay the diagnosis. In rare cases, in patients who have been taking omeprazole for a long time, a histological examination of biopsy specimens of the gastric mucosa of the body of the stomach revealed atrophic gastritis. Patients taking the drug for a long period (especially more than 1 year) should be under regular medical supervision. Patients taking Nexium as needed should be instructed to contact their doctor if symptoms change. Taking into account fluctuations in the concentration of esomeprazole in plasma when prescribing therapy as needed, the interaction of the drug with other drugs should be taken into account (see "Interaction"). When prescribing Nexium® for the eradication of Helicobacter pylori, the possibility of drug interactions for all components of triple therapy should be taken into account. Clarithromycin is a potent inhibitor of CYP3A4, therefore, when prescribing eradication therapy to patients receiving other drugs that are metabolized with the participation of CYP3A4 (for example, cisapride), it is necessary to take into account possible contraindications and interactions of clarithromycin with these drugs. Nexium® tablets contain sucrose, therefore they are contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency. Studies have shown a pharmacokinetic/pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg/day) and esomeprazole (40 mg/day, orally), leading to a reduction in exposure to the active metabolite of clopidogrel by an average of 40% and a decrease in the maximum inhibition of ADP-induced platelet aggregation by an average of 14%. Therefore, the simultaneous use of esomeprazole and clopidogrel should be avoided (see "Interaction"). Separate observational studies indicate that proton pump inhibitor therapy may slightly increase the risk of osteoporosis-related fractures, but other similar studies have not noted an increase in risk. In randomized, double-blind, controlled clinical trials of omeprazole and esomeprazole, including two open-label studies of long-term therapy (more than 12 years), the association of fractures due to osteoporosis with the use of proton pump inhibitors has not been confirmed. Although a causal relationship between the use of omeprazole/esomeprazole and fractures due to osteoporosis has not been established, patients at risk of developing osteoporosis or fractures due to it should be under appropriate clinical supervision. Influence on the ability to drive a car and other mechanisms. Due to the fact that during therapy with Nexium® dizziness, blurred vision and drowsiness may occur, care should be taken when driving vehicles and operating other mechanisms.

Compound

• 1 tab. esomeprazole magnesium trihydrate 22.3 mg, which corresponds to the content of esomeprazole 20 mg (E172) - 20 mcg, magnesium stearate - 1.2 mg, copolymer of methacrylic and ethacrylic acid (1: 1) - 35 mg, microcrystalline cellulose - 273 mg, paraffin - 200 mcg, macrogol - 3 mg, polysorbate 80 - 620 mcg, crospovidone - 5.7 mg, sodium stearyl fumarate - 570 mcg, sucrose spherical granules (sugar, spherical granules) (size 0.250-0.355 mm) - 28 mg, titanium dioxide (E171) - 2.9 mg, talc - 14 mg, triethyl citrate - 10 mg. 1 tab. esomeprazole magnesium trihydrate 44.5 mg, which corresponds to the content of esomeprazole 40 mg mg, copolymer of methacrylic and ethacrylic acids (1:1) - 46 mg, microcrystalline cellulose - 389 mg, paraffin - 300 mcg, macrogol - 4.3 mg, polysorbate 80 - 1.1 mg, crospovidone - 8.1 mg, sodium stearyl fumarate - 810 mcg, sucrose spherical granules (sugar, spherical granules) (size 0.250-0.355 mm) - 30 mg, titanium dioxide (E171) - 3.8 mg, talc - 20 mg, triethyl citrate - 14 mg. One package contains: active substance: esomeprazole magnesium trihydrate 11.1 mg, equivalent to 10 mg of esomeprazole; excipients: methacrylic acid and ethyl acrylate copolymer (1:1) 9.5 mg, talc 8.4 mg; sucrose, spherical granules (sugar, spherical granules) (size 0.250 - 0.355 mm) 7.4 mg, hyprolose 32.2 mg, hypromellose 1.7 mg, triethyl citrate 0.95 mg, magnesium stearate 0.65 mg, glycerol monostearate 40 -55 0.48 mg, Polysorbate 80 0.27 mg, dextrose 2813 mg, crospovidone 75 mg, xanthan gum 75 mg, anhydrous citric acid 4.9 mg, iron oxide yellow dye 1.8 mg esomeprazole sodium 42.5 mg, which corresponds to content of esomeprazole 40 mg Excipients: ethylenediaminetetraacetic acid disodium salt, sodium hydroxide, nitrogen for injection, water for injection. Esomeprazole magnesium trihydrate 22.3 mg, which corresponds to the content of esomeprazole 20 mg 1:1), microcrystalline cellulose, paraffin, macrogol, polysorbate 80, crospovidone, sodium stearyl fumarate, sucrose spherical granules, titanium dioxide (E171), talc, triethyl citrate. Esomeprazole magnesium trihydrate 44.5 mg, which corresponds to the content of esomeprazole 40 mg paraffin, macrogol, polysorbate 80, crospovidone, sodium stearyl fumarate, sucrose spherical granules, titanium dioxide (E171), talc, triethyl citrate.

Nexium indications for use

• gastroesophageal reflux disease: - treatment of erosive reflux esophagitis; - long-term maintenance treatment after healing of erosive reflux esophagitis to prevent recurrence; - symptomatic treatment of gastroesophageal reflux disease; peptic ulcer of the stomach and duodenum (as part of combination therapy): - treatment of duodenal ulcer associated with Helicobacter pylori; - prevention of recurrence of peptic ulcer associated with Helicobacter pylori; long-term acid-suppressing therapy in patients who have had bleeding from a peptic ulcer (after intravenous use of drugs that reduce the secretion of the gastric glands), to prevent relapse; patients taking NSAIDs for a long time: - healing of gastric ulcer associated with taking NSAIDs; - prevention of gastric and duodenal ulcers associated with the use of NSAIDs in patients at risk; Zollinger-Ellison syndrome or other conditions characterized by abnormal hypersecretion

Nexium contraindications

• - hereditary fructose intolerance; - glucose-galactose malabsorption; - sucrase-isomaltase deficiency; - children's age up to 12 years (due to the lack of data on the efficacy and safety of the drug in this group of patients); - children over 12 years of age for indications other than gastroesophageal reflux disease; - combined use with atazanavir and nelfinavir; - hypersensitivity to esomeprazole, substituted benzimidazoles or other components of the drug. With caution, the drug should be prescribed for severe renal failure (experience is limited). Use during pregnancy and lactation Currently, there is insufficient data on the use of Nexium during pregnancy. Prescribing the drug to such patients is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. The results of epidemiological studies of omeprazole, which is a racemic mixture, showed no

Nexium dosage

• 10 mg 20 mg 40 mg

Nexium side effects

• The following are the side effects that do not depend on the dosage regimen of the drug, noted with the use of the drug Nexium®, both during clinical trials and in post-marketing studies. The frequency of side effects is given as the following gradation: very often (? 1/10); often (?1/100,

drug interaction

Effect of esomeprazole on the pharmacokinetics of other drugs. A decrease in the acidity of gastric juice during treatment with esomeprazole can lead to a change in the absorption of drugs, the absorption of which depends on the acidity of the environment. As with other drugs that suppress the secretion of hydrochloric acid or antacids, treatment with esomeprazole can lead to a decrease in the absorption of ketoconazole or itraconazole, as well as an increase in the absorption of digoxin. Co-administration of omeprazole 20 mg once daily with digoxin increases the bioavailability of digoxin by 10% (digoxin bioavailability increased by up to 30% in 20% of patients). Omeprazole has been shown to interact with some antiretroviral drugs. The mechanisms and clinical significance of these interactions are not always known. An increase in pH during therapy with omeprazole may affect the absorption of antiretroviral drugs. Interaction at the level of the CYP2C19 isoenzyme is also possible. With the joint appointment of omeprazole and some antiretroviral drugs, such as atazanavir and nelfinavir, during therapy with omeprazole, there is a decrease in their serum concentration. Therefore, their simultaneous use is not recommended. Co-administration of omeprazole (40 mg once a day) with atazanavir 300 mg / ritonavir 100 mg in healthy volunteers resulted in a significant decrease in the bioavailability of atazanavir (area under the concentration-time curve, maximum (Cmax) and minimum (Cmin) concentrations decreased by approximately 75%). Increasing the dose of atazanavir to 400 mg did not compensate for the effects of omeprazole. on the bioavailability of atazanavir.With the simultaneous appointment of omeprazole and saquinavir, an increase in serum concentrations of saquinavir was noted, when administered with some other antiretroviral drugs, their concentration did not change.Given the similar pharmacokinetic and pharmacodynamic properties of omeprazole and esomeprazole, co-administration of Changing esomeprazole with antiretrovirals such as atazanavir and nelfinavir is not recommended. Esomeprazole inhibits CYP2C19, the main isoenzyme involved in its metabolism. Accordingly, the combined use of esomeprazole with other drugs, in the metabolism of which the CYP2C19 isoenzyme is involved, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., can lead to an increase in plasma concentrations of these drugs, which, "in" [its own , turn, may require a dose reduction. It is especially important to remember this interaction when prescribing Nexium® in the “as needed” mode. When co-administered "30 mg of esomeprazole and diazepam, which is a substrate of the isoenzyme - CYP2C19, there is a decrease in the clearance of diazepam by 45%. The administration of esomeprazole at a dose of 40 mg led to an increase in the residual concentration of phenytoin in patients with epilepsy by 13%. In this regard, it is recommended control plasma concentrations of phenytoin at the beginning of treatment with esomeprazole and when it is canceled.Administration of omeprazole at a dose of 40 mg once a day led to an increase in the area under the concentration-time curve and Cmax of voriconazole (CYP2C19 isoenzyme substrate) by 15% and 41%, co-administration of warfarin with 40 mg of esomeprazole does not lead to a change in coagulation time in patients taking warfarin long-term.However, several cases of clinically significant increase in INR (international normalized ratio) have been reported with the combined use of warfarin and esomeprazole.It is recommended to control INR at the beginning and after termination of co-administration of esomeprazole and warfarin or other coumarin derivatives. See instructions for more details.

Overdose

described with oral administration of esomeprazole at a dose of 280 mg, were accompanied by general weakness and gastrointestinal manifestations. A single dose of 80 mg of esomeprazole orally and iv administration of 308 mg for 24 hours did not cause any negative effects.

Storage conditions

• store at room temperature 15-25 degrees
• keep away from children

Information provided

H+-K+-ATPase inhibitor.
Preparation: NEXIUM
The active substance of the drug: esomeprazole
ATX encoding: A02BC05
CFG: H+-K+-ATPase inhibitor
Registration number: P No. 013775/01
Date of registration: 31.05.07
The owner of the reg. Award: ASTRAZENECA AB (Sweden)

Nexium release form, drug packaging and composition.

Light pink film-coated tablets, oblong, biconvex, debossed with "20 mg" on one side and "A/EN" in the form of a fraction on the other.
1 tab.

22.3 mg

20 mg

Excipients: glycerol monostearate 40-55, hyprolose, hypromellose, iron oxide red, iron oxide yellow, magnesium stearate, copolymer of methacrylic and ethacrylic acid (1: 1), microcrystalline cellulose, synthetic paraffin, macrogol, polysorbate 80, crospovidone, sodium stearyl fumarate , sucrose spherical granules, titanium dioxide, talc, triethyl citrate.

Pink, oblong, biconvex film-coated tablets, debossed with "40 mg" on one side and "A/EI" in the form of a fraction on the other.
1 tab.
esomeprazole magnesium trihydrate
44.5 mg
which corresponds to the content of esomeprazole
40 mg

Excipients: glycerol monostearate 40-55, hyprolose, hypromellose, iron oxide red, magnesium stearate, copolymer of methacrylic and ethacrylic acid (1:1), microcrystalline cellulose, synthetic paraffin, macrogol, polysorbate 80, crospovidone, sodium stearyl fumarate, sucrose spherical granules , titanium dioxide, talc, triethyl citrate.

7 pcs. - blisters (1) - packs of cardboard.
7 pcs. - blisters (2) - packs of cardboard.
7 pcs. - blisters (4) - packs of cardboard.

The description of the drug is based on the officially approved instructions for use.

Pharmacological action of Nexium

H+-K+-ATPase inhibitor. The active substance of the drug Nexium - esomeprazole - is the S-isomer of omeprazole, reduces the secretion of hydrochloric acid in the stomach by specific inhibition of the proton pump in parietal cells. The S- and R-isomers of omeprazole have similar pharmacodynamic activity.

Mechanism of action

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

Effect on gastric acid secretion

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

In patients with gastroesophageal reflux disease and the presence of clinical symptoms, after 5 days of daily intake of Nexium orally at a dose of 20 mg or 40 mg, the pH in the stomach was above 4 for an average of 13 and 17 hours out of 24 hours. While taking the drug at a dose of 20 mg /day the value of intragastric pH above 4 was maintained for 8, 12 and 16 hours is achieved 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 plasma concentration of the drug (the AUC parameter was used to estimate the concentration).

Therapeutic effect achieved as a result of inhibition of acid secretion

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

Treatment with Nexium at a dose of 20 mg 2 times / day in combination with appropriate antibiotics for one week leads to successful eradication of Helicobacter pylori in approximately 90% of patients.

Patients with an uncomplicated ulcer after a week of eradication do not require subsequent monotherapy with antisecretory drugs to heal the ulcer and eliminate symptoms.

Other effects associated with inhibition of acid secretion

During treatment with antisecretory drugs, plasma gastrin levels rise as a result of decreased acid secretion.

In patients who have received esomeprazole for a long time, there is an increase in the number of enterochromaffin-like cells, probably associated with an increase in plasma gastrin levels.

In patients who have used antisecretory drugs for a long time, the formation of glandular cysts in the stomach is more common. This phenomenon is due to physiological changes resulting from the inhibition of acid secretion. The cysts are benign and reversible.

In the course of two comparative studies conducted with ranitidine, Nexium showed better efficacy in healing peptic ulcers in patients receiving non-steroidal anti-inflammatory therapy, including selective COX-2 inhibitors.

In two efficacy studies, Nexium showed better efficacy in preventing peptic ulcers in patients (age group older than 60 years and / or with a history of peptic ulcer) who received non-steroidal anti-inflammatory therapy, including the use of selective COX-2 inhibitors.

Pharmacokinetics of the drug.

Suction and distribution

Esomeprazole is unstable in an acidic environment, therefore, tablets containing drug granules coated with a shell that is resistant to the action of gastric juice are used for oral administration.

After oral administration, esomeprazole is rapidly absorbed from the gastrointestinal tract; Cmax is achieved after 1-2 hours. Absolute bioavailability after a single dose of 40 mg is 64% and increases to 89% against the background of daily intake 1 time / day. For a dose of 20 mg of esomeprazole, these figures are 50% and 68%, respectively. In an equilibrium state, Vd in healthy people is approximately 0.22 l / kg of body weight. Plasma protein binding - 97%. Simultaneous food intake slows down and reduces the absorption of esomeprazole in the stomach.

Metabolism and excretion

Under in vivo conditions, only a small part of esomeprazole is converted to the R-isomer. Esomeprazole is completely biotransformed with the participation of enzymes of the cytochrome P450 (CYP) system. The main part is metabolized with the participation of a specific polymorphic isoform of CYP2C19, with the formation of hydroxy- and demethylated metabolites of esomeprazole. The remainder is metabolized by another specific CYP3A4 isoform, producing the sulfo derivative of esomeprazole, which is the major plasma metabolite.

The parameters below reflect, in general, the nature of the pharmacokinetics in patients with an active CYP2C19 enzyme (patients with a rapid metabolism).

The total clearance is approximately 17 l / h after a single dose of the drug and 9 l / h after multiple doses. T1 / 2 is 1.3 hours with a systematic intake of 1 time / day. AUC dose-dependently increases with regular intake and is expressed in a non-linear dose and AUC relationship. This time and dose dependence is a consequence of a decrease in the metabolism of esomeprazole during the "first pass" through the liver, as well as a decrease in systemic clearance, probably caused by the fact that esomeprazole and / or its sulfo-containing metabolite inhibit the CYP2C19 enzyme. With daily intake 1 time / day, esomeprazole is completely eliminated from the blood plasma between doses and does not accumulate.

None of the major metabolites of esomeprazole affects gastric acid secretion. When taking the drug orally, up to 80% of the dose is excreted as metabolites in the urine, the rest is excreted in the feces. Less than 1% of unchanged esomeprazole is found in the urine.

Pharmacokinetics of the drug.

in special clinical situations

Approximately 1-2% of the population has reduced activity of the CYP2C19 isoenzyme (patients with a slow metabolism). In such patients, the metabolism of esomeprazole is mainly carried out as a result of the action of CYP3A4. With the systematic administration of 40 mg of esomeprazole 1 time / day, AUC is 100% higher than the value of this parameter in patients with an active CYP2C19 enzyme (patients with a rapid metabolism). The average value of Cmax in patients with a slow metabolism is increased by approximately 60%.

In elderly patients (71-80 years), the metabolism of esomeprazole does not undergo significant changes.

After a single dose of 40 mg of esomeprazole, the mean AUC in women is 30% higher than that in men. With systematic daily administration of the drug 1 time / day, differences in pharmacokinetics in patients of both sexes are not observed (these differences do not affect

drug).

In patients with mild to moderate hepatic insufficiency, the metabolism of esomeprazole may be impaired. In patients with severe hepatic insufficiency, the metabolic rate is reduced, resulting in a 2-fold increase in AUC for esomeprazole.

The study of pharmacokinetics in patients with renal insufficiency has not been conducted. Since not esomeprazole itself is excreted through the kidneys, but its metabolites, it can be assumed that the metabolism of esomeprazole in patients with renal insufficiency does not change.

In children aged 12-18 years, after repeated administration of esomeprazole at a dose of 20 mg and 40 mg, the AUC value and the time to reach maximum plasma concentration were similar to those in adults.

Indications for use:

Gastroesophageal reflux disease:

Treatment of erosive reflux esophagitis;

Long-term maintenance therapy in patients after healing of erosive reflux esophagitis to prevent recurrence;

Symptomatic therapy of gastroesophageal reflux disease.

Peptic ulcer of the stomach and duodenum (as part of combination therapy):

Treatment of duodenal ulcer associated with Helicobacter pylori;

Prevention of recurrence of peptic ulcer associated with Helicobacter pylori.

Patients taking NSAIDs for a long time:

Healing of gastric ulcers associated with taking NSAIDs;

Prevention of gastric and duodenal ulcers associated with the use of NSAIDs in patients at risk.

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

Dosage and method of application of the drug.

In gastroesophageal reflux disease, adults and children over 12 years of age are prescribed Nexium for the treatment of erosive reflux esophagitis in a single dose of 40 mg 1 time / day for 4 weeks. An additional 4-week course of therapy is recommended in cases where, after the first course, there is no cure for esophagitis or symptoms of the disease persist. For long-term maintenance therapy of patients with cured erosive esophagitis to prevent relapse, the drug is prescribed 20 mg 1 time / day. For symptomatic therapy of gastroesophageal reflux disease without esophagitis, the drug is prescribed at a dose of 20 mg 1 time / day. If after 4 weeks of treatment the symptoms do not disappear, an additional examination of the patient should be carried out. After the symptoms are eliminated, you can switch to the regimen of taking the drug "as needed", i.e. take Nexium 20 mg 1 time / day if symptoms occur until they are relieved. For patients taking NSAIDs and at risk of developing gastric or duodenal ulcers, treatment on an as-needed basis is not recommended.

For adults with peptic ulcer of the stomach and duodenum as part of combination therapy for the eradication of Helicobacter pylori, as well as for the treatment of duodenal ulcer associated with Helicobacter pylori and for the prevention of recurrence 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 / day for 7 days.

For patients taking NSAIDs for a long time, for the healing of gastric ulcers associated with taking NSAIDs, Nexium is prescribed at a dose of 20 mg or 40 mg 1 time / day. The duration of treatment is 4-8 weeks.

For the prevention of gastric and duodenal ulcers associated with the use of NSAIDs, Nexium is prescribed at a dose of 20 mg or 40 mg 1 time / day.

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

When prescribing the drug to patients with impaired renal function, dose adjustment is not required. The drug is used with caution in patients with severe renal insufficiency due to the limited clinical experience of its use in this category of patients.

When prescribing Nexium to patients with mild or moderate hepatic insufficiency, dose adjustment is not required. In patients with severe hepatic insufficiency, the dose used should not exceed 20 mg / day.

Elderly patients do not need to adjust the dosage regimen.

Tablets should be swallowed whole with liquid. Tablets should not be chewed or crushed. Patients with difficulty in swallowing can dissolve the tablet in half a glass of non-carbonated water (other liquids should not be used, as the protective shell of the microgranules may dissolve), stir until the tablet disintegrates and drink the suspension of microgranules immediately or within 30 minutes. Then you should again fill the glass with water halfway, stir the rest and drink. Microgranules should not be chewed or crushed.

For patients who cannot swallow, tablets should be dissolved in still water and administered via a nasogastric tube. It is important that the selected syringe and probe are thoroughly tested.

The introduction of the drug through a nasogastric tube

1. Place a tablet in a syringe and fill the syringe with 25 ml of water and approximately 5 ml of air. 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 tablet granules.

2. Shake the syringe immediately for about 2 minutes to dissolve the tablet.

3. Hold the syringe with the tip up and check that the tip is not clogged.

4. Insert the tip of the syringe into the probe while continuing to hold it pointing up.

5. Shake the syringe and turn it upside down. Inject 5-10 ml of the dissolved drug into the tube immediately. After injection, return the syringe to its original position and shake (the syringe must be held with the tip up to avoid clogging the tip).

6. Turn the syringe upside down and inject another 5-10 ml of the drug into the probe. Repeat this operation until the syringe is empty.

7. If part of the drug remains in the form of sediment 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 effects of Nexium:

The following side effects do not depend on the dose of the drug.

Often (>1/100,<1/10): головная боль, боль в животе, диарея, метеоризм, тошнота, рвота, запор.

Less often (>1/1000,<1/100): дерматит, зуд, крапивница, сыпь, головокружение, сухость во рту, бессонница, парестезия, сонливость, повышение активности печеночных ферментов, периферические отеки.

Rare (>1/10000,<1/1000): лейкопения, тромбоцитопения, аллергические реакции: лихорадка, ангионевротический отек, анафилактоидная реакция; возбуждение, депрессия, замешательство, изменения вкуса, гипонатриемия, нечеткость зрения, бронхоспазм, стоматит, желудочно-кишечный кандидоз, гепатит с (или без) желтухой, фотосенсибилизация, алопеция, артралгия, миалгия, недомогание.

Very rarely (<1/10000): агранулоцитоз, панцитопения, галлюцинации (преимущественно у ослабленных пациентов), агрессивное поведение, печеночная недостаточность, печеночная энцефалопатия, многоформная экссудативная эритема, синдром Стивенса-Джонсона, токсический эпидермальный некролиз, мышечная слабость, интерстициальный нефрит, гинекомастия.

Contraindications to the drug:

hereditary fructose intolerance;

Glucose-galactose malabsorption;

Sugarase-isomaltase deficiency;

Children under 12 years of age (due to the lack of data on the efficacy and safety of the drug in this group of patients);

Children over 12 years of age for indications other than gastroesophageal reflux disease;

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

With caution, the drug should be prescribed for severe renal failure (experience is limited). Esomeprazole (like other proton pump inhibitors) should not be co-administered with atazanavir.

Use during pregnancy and lactation.

Currently, there is not enough data on the use of Nexium during pregnancy. The appointment of the drug during this period is possible only if the intended benefit to the mother outweighs 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 negative effects of esomeprazole on the development of the embryo or fetus have been identified. The introduction of the racemic preparation also did not have any negative effect on the course of pregnancy, childbirth and the period of postnatal development in animals.

It is currently unknown whether esomeprazole is excreted in breast milk, so Nexium should not be prescribed during breastfeeding.

Special instructions for the use of Nexium.

In the presence of any alarming symptoms (including significant spontaneous weight loss, repeated vomiting, dysphagia, vomiting with blood or melena), as well as in the presence of a stomach ulcer (or if a stomach ulcer is suspected), the presence of a malignant neoplasm should be excluded, since treatment with Nexium can lead to a smoothing of symptoms and delay the diagnosis.

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

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

When appointing Nexium for the eradication of Helicobacter pylori, the possibility of drug interactions for all components of triple therapy should be taken into account. Clarithromycin is a potent inhibitor of CYP3A4, therefore, when prescribing eradication therapy to patients receiving other drugs that are metabolized with the participation of CYP3A4 (for example, cisapride), possible contraindications and interactions of clarithromycin with these drugs should be taken into account.

Influence on the ability to drive vehicles and control mechanisms

There was no effect of the drug on the ability to drive vehicles and control mechanisms.

Drug overdose:

Currently, extremely rare cases of intentional overdose have been described.

Symptoms: when taking esomeprazole at a dose of 280 mg orally, general weakness and manifestations of the gastrointestinal tract were noted. A single dose of Nexium at a dose of 80 mg orally did not cause any negative consequences.

Treatment: if necessary, carry out symptomatic and supportive therapy. The specific antidote is unknown. Dialysis is ineffective, because. Esomeprazole binds to plasma proteins.

Interaction of Nexium with other drugs.

Effect of esomeprazole on the pharmacokinetics of other drugs

A decrease in the acidity of gastric juice during treatment with esomeprazole can lead to a change in the absorption of drugs, the absorption of which depends on the acidity of the environment.

Esomeprazole, like antacids and other drugs that reduce gastric acid secretion, can lead to a decrease in the absorption of ketoconazole and itraconazole.

Co-administration of omeprazole at a dose of 40 mg 1 time / day and atazanavir 300 mg / ritonavir 100 mg led to a significant decrease in AUC values, as well as maximum and minimum concentrations of atazanavir in healthy volunteers. Increasing the dose of atazanavir to 400 mg did not compensate for the effect of omeprazole on atazanavir concentrations. Therefore, esomeprazole should not be co-administered with atazanavir.

Esomeprazole inhibits CYP2C19, the main enzyme involved in its metabolism. Accordingly, the co-administration of esomeprazole with other drugs metabolized by CYP2C19 (eg, diazepam, citalopram, imipramine, clomipramine, phenytoin) may lead to increased plasma concentrations of these drugs, which in turn will lead to the need to reduce the dose . This phenomenon is especially pronounced when Nexium is used in the “as needed” therapy mode. When co-administered 30 mg of esomeprazole and diazepam, the clearance of the enzyme-substrate complex (CYP2C19-diazepam) is reduced by 45%.

The minimum plasma concentrations of phenytoin in patients with epilepsy increased by 13% when combined with esomeprazole at a dose of 40 mg. In this regard, it is recommended to control plasma concentrations of phenytoin at the beginning of treatment with esomeprazole and when it is canceled.

Co-administration of warfarin with esomeprazole 40 mg does not lead to a change in coagulation time in patients taking warfarin for a long time. However, several cases of a clinically significant increase in the INR index have been reported with the combined use of warfarin and esomeprazole. In this connection, monitoring of patients at the beginning and at the end of the joint use of these drugs is recommended.

Co-administration of cisapride with esomeprazole at a dose of 40 mg leads to an increase in the values ​​of the pharmacokinetic parameters of cisapride: AUC - by 32% and T1 / 2 - by 31%, however, plasma concentrations of cisapride did not change significantly. A slight prolongation of the QT interval, which was observed with cisapride monotherapy, did not increase with the addition of Nexium.

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

Studies evaluating the co-administration of esomeprazole and naproxen or rofecoxib did not reveal a clinically significant pharmacokinetic interaction.

The effect of drugs on the pharmacokinetics of esomeprazole

Esomeprazole is metabolized by CYP2C19 and CYP3A4. The combined use of esomeprazole with clarithromycin (500 mg 2 times / day), which inhibits CYP3A4, leads to a 2-fold increase in esomeprazole AUC exposure. Co-administration of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19, such as voriconazole, may result in a more than 2-fold increase in the AUC value for esomeprazole. In such cases, no dose adjustment of esomeprazole is required.

Conditions of sale in pharmacies.

The drug is dispensed by prescription.

Terms of the storage conditions of the drug Nexium.

Tablets should be stored out of the reach of children at a temperature not exceeding 30 ° C in the original packaging. Shelf life - 3 years. Do not use after the expiration date.

Nexium (generic international name - esomeprazole) is a medication, the action of which is aimed at reducing the production of hydrochloric acid by the gastric glands.

Due to the suppression of secretory activity, the agent helps to reduce the level of acidity and is used in the complex therapy of various conditions associated with excessive acid secretion. About how to take the drug and how to choose the right dose, the instructions for the use of Nexium or the attending physician will tell.

Application

A drug such as Nexium INN is available in the following forms:

• 20 mg and 40 mg pills.
• Granules, pellets of 10 mg.
• Lyophilizate 40 mg. This form is used exclusively for injection.

Therefore, the drug - "Nexium" has 2 main variations of application:

Nexium tablets are most often used, as this is the most familiar and convenient option. The rare use of pellets is explained by the fact that a smaller amount of the active substance is contained in the composition. As a rule, the drug in Nexium pills is used for children or patients who are not able to swallow the pill. The drug "lyophilisate" Nexium is used when it is impossible to use the drug orally.

The composition of the drug includes the active substance esomeprazole in different dosages. For example, Nexium tablets contain 20 mg-40 mg of the active ingredient, granules - 10 mg each, and for injections - 40 mg in a vial. Therefore, it is possible to come across such a name as "Nexium 40, 20 or 10 mg" and "Nexium powder". This kind of terminology is unofficial, but widely used.

The composition of 1 pill fits:

1. Esomeprazole.
2. Glycerol monostearate, hyprolose, hypromellose, dye (E172), cellulose, magnesium stearate, copolymer of methacrylic and ethacrylic acids, paraffin, polysorbate, macrogol, crospovidone, titanium dioxide, talc, triethyl citrate.

The composition of 1 package of granules includes almost the same number of auxiliary components. Dextrose is added to this form.

The composition of 1 bottle of lyophilizate includes: esomeprazole, disodium edetate dihydrate, sodium hydroxide.

In pharmacies, Nexium pills come in packages that are equipped with a first opening test. You can buy a package with 1, 2 or 4 blisters of 7 pills each. Pellets - granules in sachets (10 mg) are assembled in 10 or 28 pieces. For injection, a medicine such as Nexium is sold in 10 vials per pack.

Pellets or granules have a yellowish or brown color. Pills - oval-shaped with a pinkish color, on the front side the inscription "40 mg" or "20 mg", depending on the amount of active substance, on the reverse side of the letter "A / EI". Lympholisate is represented by a mass of white color.

Important! The drug is released strictly according to the prescription.

Therapeutic influence

This drug is designed to reduce the release of hydrochloric acid. This kind of influence is of considerable importance, since the need to reduce acidity is a key moment in the course of the treatment of many diseases. According to the mechanism of action, the drug is classified as a proton pump inhibitor.

A characteristic feature of the drug is the ability to eliminate excessive production of acid. The remedy begins to act after 1 hour after ingestion.

It should be noted that esomeprazole does not have acid resistance. For this reason, in the manufacture of products of this group, the active ingredients are wrapped in a shell that is not affected by an acidic environment.

Many patients have a question how to take Nexium: before meals or after? It should be noted that after taking the pill, its rapid absorption from the gastrointestinal tract is noted.

Experts note that if the drug is taken with food, then the absorption of the active substance will be significantly inhibited, but this practically does not affect the effectiveness of the drug. The summary states that the intake of the drug and food should be separated by about 30-60 minutes. Therefore, you need to take Nexium before meals or after a meal with an interval of 30-60 minutes.

The use of a medication at 40 mg per day for 4 weeks allows 78% to cure gastroesophageal reflux disease. If the treatment is extended to 8 weeks, then the percentage of cured patients rises to 90.

The use of a drug of 20 mg in combination with antibiotics contributes to the elimination of Helicobacter in 90% of patients after 2 weeks. In addition, patients who used Nexium in the treatment of gastric or duodenal ulcers should not, upon completion of therapeutic measures, drink other aids for scarring ulceration.

When appointed

Medication Nexium and its indications for use will help get rid of the symptoms and foci of inflammation. Nexium is prescribed for the treatment and prevention of a number of pathologies.

These include:

1. Gastroesophageal reflux disease.
2. Ulcer of the stomach and duodenum.
3. Diseases of the stomach that arose against the background of prolonged use of NVPS.
4. Other diseases associated with increased secretion of hydrochloric acid.

1. Auxiliary measures for incurable esophagitis, aimed at preventing exacerbation.
2. Elimination of symptoms.
3. Treatment of erosive GERD.

Peptic ulcer of the stomach and duodenum:

1. Treatment of the disease provoked by Helicobacter pylori.
2. Relapse prevention.

Pathologies of the stomach that have arisen in patients who have been taking NSAIDs for a long time:

1. Therapy of ulcers caused by taking medications from the NVS group.
2. Relapse prevention.

Indications for the use of lyophilisate:

1. GERD in combination with esophagitis.
2. Scarring and prevention of peptic ulcers.
3. Prevention of blood loss from a peptic ulcer.

Important! Lyophilizate Nexium for children is prescribed from 1 year.

Contraindications

Nexium has contraindications that must be taken into account. The tool does not need to be used:

1. With congenital fructose intolerance.
2. Up to 12 years old.
3. After 12 years can be used only in the presence of GERD.
4. With increased susceptibility to the components.

Nexium should be replaced with its analogue in such situations:

1. Hypersensitivity to the active substance.
2. Diseases of the kidneys.
3. GW period and pregnancy.

Rules for use and dosage

Before you start taking it, you need to familiarize yourself with the drug Nexium and its instructions for use. The use of the drug is intended for oral administration before or after meals. The medicine should be swallowed whole with plenty of water.

Important! It is forbidden to crush or chew the medicine.

For patients who have difficulty swallowing, the medication can be diluted in 0.5 tbsp. liquids. For patients who do not have the opportunity to swallow pills at all, the introduction is made by a nasogastric tube.

Pellets and granules are applied orally. To receive 10 mg of the drug, you need to dilute 1 sachet in 15 ml of liquid. Patients taking 20 mg of the drug will need to dissolve 2 packets in 30 ml of liquid.

The lyophilisate is intended for injection and infusion. The dosage and frequency of use is determined by the doctor.

Negative influence

Nexium has side effects that should be considered during therapy.

Side effects of Nexium are expressed as follows:

1. CNS. Often the drug causes a migraine. There may also be a taste disorder. Sometimes there is lethargy, dizziness.
2. At times, bronchospasm may occur.
3. On the part of the gastrointestinal tract, nausea, vomiting, pain in the abdominal cavity, bloating, upset stool can be observed.
4. The reaction to the drug may be irritation, dermatitis, rash.
5. Vision may be impaired.
6. General disorder: profuse sweating, malaise.

Signs of an overdose: weakness and upset of the digestive system.

During pregnancy

Particular attention should be paid to the fact that it is undesirable to prescribe Nexium during pregnancy, since there is no verified information about its effect on a woman's body during this period. There is also no information about whether the drug passes into the mother's milk. Therefore, during the GV period, the medicine should not be used either.

Analogues

Help for people with acid-dependent pathologies was the release of the medication Emaner. Despite the fact that Nexium analogs may contain different active ingredients, this analog contains esomeprazole. Therefore, this analogue is considered an excellent replacement for Nexium. Emenera is produced in coated capsules. The tool has the same indications for use as Nexium.

Photos, videos and reviews on the effect of this analogue on the body can be viewed on the Runet. It should be noted that the reviews about this medication are different, for example, “I didn’t like Emanera. It does not relieve the burning sensation, I additionally drink Gaviscon.

Important! Patients who take the drug for a long time must necessarily undergo consultations on time, since a large dosage of the drug can significantly increase the risk of fractures.

The composition of Emaner includes sucrose, as a result of which the drug is contraindicated in patients with fructose intolerance.

The effectiveness of the impact of any acid-blocking drug is determined primarily by the genetic characteristics of the patient, the list of medications used. Do not choose your own medicines for treatment. An incorrectly chosen drug or an incorrect dosage can adversely affect health. The purpose of the drug and its dosage should be selected individually on the basis of examination and examination.

www.kogdaizzhoga.com

Nexium

Compound

As part of tablets, esomeprazole magnesium trihydrate 22.3 mg or 44.5 mg + excipients (hyprolose, E172, magnesium stearate, glycerol monostearate, hypromellose, triethyl citrate, copolymer of ethacrylic and methacrylic acids, macrogol, crospovidone, paraffin, polysorbate 80, stearyl fumarate sodium, macrogol, E171, sucrose, talc).

Mass for solution preparation: esomeprazole 40 mg + sodium hydroxide and disodium dihydrate edetate.

Release form

Nexium 20 mg and Nexium 40 mg are coated tablets, oblong, convex. Color - pink, 20 mg - lighter, 40 mg - darker. The dosage is engraved on one side of the tablet, and the inscription A / EH or A / EI on the other. Cardboard packages of 7, 14, 28 pieces.

Powder - pressed white mass for the preparation of a solution. In glass vials of 5 ml.

pharmachologic effect

proton pump inhibitor.

Pharmacodynamics and pharmacokinetics

The active substance is a derivative of omeprazole (its S-isomer). Esomeprazole reduces the activity of hydrochloric acid secretion on the gastric mucosa by suppressing the proton pump (enzyme H + K + -ATPase) of parental cells on the walls of the stomach.

When combined with antibiotics, it is effective against Helicobacter pylori, which is usually the cause of stomach ulcers.

As a specific response to decreased acid secretion, benign cysts may form and plasma gastrin levels may increase.

1-2 hours after taking the drug is already beginning to have an active effect on the level of hydrochloric acid. About 90% of the active substance binds to plasma proteins. Metabolized, excreted in urine and feces.

Pharmacokinetics in people with reduced CYP2C19 enzyme activity and severe liver disease differs from the main group of people. It is necessary to make a dose adjustment of the drug.

Indications for use

Tablets:

• erosive reflux esophagitis, treatment and supportive care;
• gastric and duodenal ulcer (treatment and prevention, in combination with other means);
• pathological hypersecretion of the glands of the stomach;
• people who take NSAIDs for a long time and treatment of diseases caused by their intake;
• prevention and treatment of bleeding from peptic ulcers;
• idiopathic hypersecretion.

A solution for intramuscular administration is prescribed if it is impossible to take the tablet form of the drug.

The indication is:

• gastroesophageal reflux disease;
• peptic ulcers, including prevention of bleeding after endoscopic hemostasis.

Contraindications

The drug is contraindicated:

• patients with allergies to any of the components, including fructose (for tablet form);
• when taking atazanavir or nelfinavir;
• children under 12 years old.

In the case of gastroesophageal reflux disease, the drug may be prescribed to children over 12 years of age.

Severe renal failure is not a direct contraindication to the use of the drug, but in this case, caution should be exercised.

Side effects

• nausea, headache, constipation, pain in the epigastric region;
• allergic reactions on the skin, sleep disturbance, paresthesia;
• bronchospasm, stomatitis, anaphylactic shock, myalgia, agitation, arthralgia;
• possible inflammation and redness at the injection site with intravenous and intramuscular use.

Application instruction of Nexium (Way and dosage)

Tablets are drunk whole or dissolved in water without gas. If necessary, the dissolved tablet can be administered through a nasogastric tube.

How to take, before meals or after?

According to the instructions for use of Nexium, food intake practically does not affect the effectiveness of the product. In the treatment and prevention of ulcers, as a rule, the daily dose of the drug is 20 mg, divided into two doses in combination with other drugs. The course is 7 days.

When carrying out acid-suppressing therapy, Nexium 40 mg is prescribed, every day for a month.

In conditions caused by taking NSAIDs, the daily dosage is 20-40 mg. The course is up to two months.

In severe liver disease, the daily dose should not exceed 20 mg.

Dosage for children (12+)

With erosive reflux esophagitis, the daily dose is 40 mg, at one time, for one month. In other cases, it is enough to take 20 mg of the drug per day.

Intramuscular injections

If necessary, injections of the drug or intravenous infusions may be prescribed instead of the tablet form. Dosage matches. The time of intramuscular injection should be at least three minutes.

Intravenously - from 10 minutes to half an hour. The drug is diluted with 0.9% solution of sodium chloride, without mixing with other drugs.

You can store the prepared preparation for no more than 12 hours, it is best to use it immediately after preparation.

Overdose

In people who used 0.28 grams of the drug, weakness and discomfort in the gastrointestinal tract were noted.

The medicine has no specific antidote. Treatment is symptomatic.

Interaction

When esomeprazole is combined with drugs such as ketoconazole and itraconazole, the absorption of drugs from the gastrointestinal tract may be impaired.

Atazanavir, nelfinavir, omeprazole, when combined with Nexium, become less effective. However, when combined with saquinavir, its serum concentration increases.

Simultaneous reception with drugs in the assimilation of which CYP2C19 is involved will lead to an increase in their effect. These drugs include imipramine, diazepam, clomipramine, citalopram, phenytoin.

For persons suffering from epilepsy, the remedy should be taken with caution. Epilepsy drugs (phenytoin) do not mix well with Nexium.

With caution, combine the drug with warfarin and cisapride.

Terms of sale

Need a prescription.

Storage conditions

Dark, cool place, away from children.

Store the bottle with the powder in its original packaging, in the light - no more than a day.

Best before date

3 years - pills.

2 years - powder for solution preparation.

Analogues of Nexium

What can replace the drug? In fact, the synonyms of the drug are: Nexpro, Ezoxium, Esonexa, Ezoks, Ezolong.

The most common analogues: Esomealox, Emanera, Barol, Esomeprazole, Veloz, Geerdin, Controloc, Ozol, Omez, Normicid, Rabimak, Panum, Pariet, Razol, Ultop.

The price of analogues can differ significantly from the original.

Which is better: Pariet or Nexium?

In general, the question of the use of a particular agent should be determined individually, depending on the results of the tests, the sensitivity of the body to a particular agent. However, among experts there is an opinion that Pariet is somewhat more effective than Nexium. Its action comes faster, the daily dosage is less, and side effects are less common. Both tools are not cheap, which is fully justified by their effectiveness.

Reviews about Nexium

Doctors' comments about Nexium: In general, proton pump inhibitors are currently the most effective drugs that regulate acidity in the gastrointestinal tract. Nexium is a very good drug of this series, with a pronounced strong therapeutic effect.

Reviews on the forums are good. The medicine is quite effective, relief comes quickly. Side effects appear infrequently. The disadvantage is the high cost.

Nexium price (where to buy)

The price of Nexium 40 mg tablets is about 1750 rubles for 14 pieces.

The price of Nexium 20 mg in Moscow is 1310 rubles for 14 pieces.

You can buy pellets and granules of the drug for 2061 rubles per 10 mg, 28 pieces each.

• Internet pharmacies in RussiaRussia
• Internet pharmacies of UkraineUkraine
• Internet pharmacies of KazakhstanKazakhstan

WER.RU

• Nexium tablets 40 mg 14 pcs.
• Nexium tablets 20 mg 14 pcs.
• Nexium pellets 10 mg 3042.7 mg 28 pcs. AstraZeneca AB [AstraZeneca]
• Nexium tablets 20 mg 28 pcs.
• Nexium tablets 40 mg 28 pcs.

ZdravZone

• Nexium 40mg №14 tablets AstraZeneca
• Nexium 20mg №14 tablets AstraZeneca
• Nexium 20mg №7 tablets AstraZeneca
• Nexium liof. for the preparation of a solution for intravenous injection. 40mg #10AstraZeneca
• Nexium 40mg №28 tabletsAstraZeneca

Pharmacy IFK

• NexiumAstra Zeneca, Sweden
• Nexium pellets p/kish/o gran.d/prig. suspensions 10mg pack. №28Astra Zeneca, Switzerland
• NexiumAstraZeneca/ ZiO-Zdorovye CJSC, Russia
• NexiumAstraZeneca/ ZiO-Zdorovye CJSC, Russia

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Pharmacy24

• Nexium tablets 20mg №14Zeneca (UK)
• Nexium tablets 40mg №14Zeneca (UK)
• Nexium powder for solution for injection 40mg №10Zeneca (UK)
• NexiumAstraZeneca (Sweden)

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BIOSPHERE

• Nexium 20 mg No. 14 tablets p.o. Astra Zeneka AB (Sweden)
• Nexium 40 mg No. 14 tablets p.o. Astra Zeneka AB (Sweden)

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NOTE! Information about medicines on the site is a general reference, collected from publicly available sources and cannot serve as a basis for making a decision on the use of medicines in the course of treatment. Before medicine use Nexium surely consult with the attending physician.

medicalmed.ru

Nexium

Nexium is a drug that helps to reduce the secretion of hydrochloric acid in the stomach.

Release form and composition

Nexium is available in the following dosage forms:

• Enteric-coated pellets and granules for suspension for oral administration: pale yellow, brown granules can be found, of various sizes (3042.7 mg each in triple laminated bags, 28 bags in a cardboard box);
• Film-coated tablets: oblong, biconvex, on a break - white with yellow patches; 20 mg each - light pink, on one side engraved in the form of a fraction "A / EH", on the other - "20 mg"; 40 mg each - pink, on one side engraved in the form of a fraction "A / EI", on the other - "40 mg" (7 pcs in blisters, 1, 2 or 4 blisters in a cardboard box);
• Lyophilizate for the preparation of a solution for intravenous administration: almost white or white compressed mass (in glass bottles of 5 ml, 10 bottles in paper racks, 1 rack in a cardboard box with first opening control).

The composition of 1 package of pellets and granules includes:

• Active ingredient: esomeprazole - 10 mg (in the form of magnesium esomeprazole trihydrate - 11.1 mg);
• Auxiliary components: anhydrous citric acid - 4.9 mg; giprolose - 32.2 mg; talc - 8.4 mg; copolymer (1:1) of ethyl acrylate and methacrylic acid - 9.5 mg; sugar, spherical granules (sucrose, spherical granules ranging in size from 0.25 to 0.355 mm) - 7.4 mg; hypromellose - 1.7 mg; dextrose - 2813 mg; magnesium stearate - 0.65 mg; triethyl citrate - 0.95 mg; glycerol monostearate 40-55 - 0.48 mg; polysorbate 80 - 0.27 mg; xanthan gum - 75 mg; dye crospovidone - 75 mg; iron oxide yellow - 1.8 mg.

The composition of 1 tablet includes:

• Active ingredient: esomeprazole - 20 or 40 mg (in the form of magnesium esomeprazole trihydrate - 22.3 or 44.5 mg);
• Auxiliary components (tablets of 20/40 mg, respectively): sodium stearyl fumarate - 0.57 / 0.81 mg; macrogol - 3 / 4.3 mg; magnesium stearate - 1.2 / 1.7 mg; giprolose - 8.1 / 11 mg; glyceryl monostearate 40-55 - 1.7 / 2.3 mg; microcrystalline cellulose - 273/389 mg; hypromellose - 17/26 mg; red dye iron oxide (E172) - 0.06 / 0.45 mg; yellow dye iron oxide (E172) - 0.02 / 0 mg; copolymer (1:1) of methacrylic and ethacrylic acid - 35/46 mg; paraffin - 0.2 / 0.3 mg; polysorbate 80 - 0.62 / 1.1 mg; triethylcitrate - 10/14 mg; crospovidone - 5.7 / 8.1 mg; sugar, spherical granules (sucrose, spherical granules ranging in size from 0.25 to 0.355 mm) - 28/30 mg; talc - 14/20 mg; titanium dioxide (E171) - 2.9 / 3.8 mg.

The composition of 1 bottle of lyophilisate for the preparation of an injection solution includes:

• Active ingredient: esomeprazole - 40 mg (in the form of esomeprazole sodium - 42.5 mg);
• Auxiliary components: disodium edetate dihydrate - 1.5 mg; sodium hydroxide - 0.2-1 mg.

Indications for use

• Erosive reflux esophagitis (treatment);
• Peptic ulcer associated with Helicobacter pylori (relapse prevention);
• Condition after healing of erosive reflux esophagitis (long-term maintenance treatment with a preventive purpose);
• Duodenal ulcer associated with Helicobacter pylori (treatment);
• Condition after bleeding from a peptic ulcer: after intravenous use of drugs that reduce the secretion of the gastric glands (long-term acid-suppressing therapy to prevent relapse);
• Gastroesophageal reflux disease (symptomatic treatment);
• Gastric ulcer associated with the use of non-steroidal anti-inflammatory drugs (treatment for the purpose of healing);
• Gastric and duodenal ulcer associated with the use of non-steroidal anti-inflammatory drugs (prophylaxis in patients at risk);
• Zollinger-Ellison syndrome or other conditions accompanied by pathological hypersecretion, including idiopathic hypersecretion (treatment).

injection solution

Nexium in the form of an injection solution is used as an alternative when it is impossible to take the drug inside.

The solution is prescribed for adults in the presence of the following indications:

• Gastroesophageal reflux disease with esophagitis and / or pronounced signs of reflux disease (treatment);
• Peptic ulcers associated with the use of non-steroidal anti-inflammatory drugs (prophylaxis in patients at risk);
• Peptic ulcers associated with the use of non-steroidal anti-inflammatory drugs (treatment for the purpose of healing);
• Bleeding from a peptic ulcer after endoscopic hemostasis (prevention of recurrence).

For children aged 1-18 years, Nexium is prescribed for gastroesophageal reflux disease against the background of erosive reflux esophagitis and / or severe symptoms of reflux disease.

Contraindications

• Glucose-galactose malabsorption, sucrase-isomaltase deficiency, hereditary fructose intolerance (tablets, oral suspension);
• Co-administration with nelfinavir and atazanavir;
• Hypersensitivity to the components of the drug, as well as to substituted benzimidazoles.

Nexium should be used with caution in severe renal failure.

For children, depending on the dosage form, the drug is prescribed:

• Suspension for oral administration: from 1 year (weighing at least 10 kg) in the treatment of erosive esophagitis and symptomatic therapy of gastroesophageal reflux disease; from the age of 12 in the treatment of gastroesophageal reflux disease;
• Tablets: from the age of 12 in the treatment of gastroesophageal reflux disease;
• Injectable solution: from 1 year in the treatment of gastroesophageal reflux disease.

During pregnancy, Nexium can be prescribed only after the doctor has assessed the ratio of benefits to the health of the mother with the risk to the fetus. If necessary, the use of the drug during lactation, breastfeeding should be interrupted.

Method of application and dosage

Tablets, oral suspension

Nexium tablets are swallowed whole (without crushing or chewing), washing down with liquid. If swallowing is difficult, a single dose of the drug can be dissolved in 1/2 cup of non-carbonated water. The resulting suspension of microgranules should be drunk for 30 minutes, then the glass should be filled again with 100 ml of water and the suspension should be drunk with the remnants of the dissolved tablet.

Granules and pellets for the preparation of a suspension for oral administration Nexium are prescribed, as a rule, for children and patients with problems with swallowing. To obtain 10 mg, the contents of 1 sachet must be dissolved in 15 ml of water. Before taking, you need to wait a few minutes until a suspension forms. The resulting suspension should be taken within 30 minutes, then the glass should be filled again with the same volume of water and the suspension should be drunk with the remnants of the dissolved granules. Use carbonated water to obtain a suspension, as well as chewing or crushing microgranules should not be.

If it is difficult to swallow diluted tablets or suspensions, they are administered through a nasogastric tube.

• Erosive reflux esophagitis (treatment; prescribed for children aged 1-11 years weighing over 10 kg in the dosage form of a suspension for oral administration): a single dose for children weighing 10-20 kg - 10 mg, more than 20 kg - 10-20 mg, frequency of use - 1 time per day, course duration - 8 weeks;
• Erosive reflux esophagitis (treatment; prescribed for adults and children from 12 years of age): single dose - 40 mg, frequency of use - 1 time per day, course duration - 4 weeks. It is possible to conduct an additional course of the same duration if the symptoms of the disease persist or if the cure for esophagitis does not occur after one course;
• Erosive reflux esophagitis (long-term maintenance therapy after healing to prevent relapse; prescribed for adults and children from 12 years of age): single dose - 20 mg, frequency of use - 1 time per day;
• Gastroesophageal reflux disease (symptomatic treatment; prescribed for children aged 1-11 years with a body weight of 10 kg in the dosage form of a suspension for oral administration): single dose - 10 mg, frequency of use - 1 time per day, course duration - up to 8 weeks;
• Gastroesophageal reflux disease without esophagitis (symptomatic therapy; prescribed for adults and children from 12 years of age): single dose - 20 mg, frequency of use - 1 time per day. If after a month from the start of treatment the symptoms do not disappear, an additional examination is recommended. After the condition improves, it is possible to switch to the “as needed” regimen of using Nexium, which involves taking the drug when symptoms of the disease occur until they are removed in a single dose of 20 mg with a frequency of administration 1 time per day. For patients taking non-steroidal anti-inflammatory drugs and patients who are at risk of developing gastric or duodenal ulcers, on-demand therapy is not recommended;
• Peptic ulcer of the stomach and duodenum for the eradication of Helicobacter pylori, as well as duodenal ulcer associated with Helicobacter pylori (combination therapy, as well as prevention of recurrence of peptic ulcers associated with this bacterium in patients with peptic ulcer; prescribed for adults): Nexium - 20 mg, clarithromycin - 500 mg, amoxicillin - 100 mg, the frequency of taking each of the drugs - 2 times a day, the duration of the course - 7 days;
• Conditions after bleeding from a peptic ulcer after intravenous use of antisecretory drugs (long-term acid-suppressing therapy and prevention of relapse; prescribed for adults): single dose - 40 mg, frequency of use - 1 time per day, course duration - 30 days;
• Gastric ulcer associated with prolonged use of non-steroidal anti-inflammatory drugs (treatment for the purpose of healing; prescribed for adults): single dose - 20 or 40 mg, frequency of use - 1 time per day, course duration - 1-2 months;
• Ulcer of the stomach and duodenum associated with the use of non-steroidal anti-inflammatory drugs (prevention; prescribed for adults): single dose - 20 or 40 mg, frequency of use - 1 time per day;
• Conditions characterized by pathological hypersecretion, including idiopathic hypersecretion and Zollinger-Ellison syndrome: the initial single dose is 40 mg (then the dose is selected individually), the frequency of use is 2 times a day, the duration of the course is determined by the doctor based on the clinical picture of the disease.

injection solution

Intravenous administration of the drug is indicated when oral administration is not possible. Parenteral use of Nexium, as a rule, is short-lived, and it is recommended that the patient be switched to taking the drug in the form of a suspension or tablets as soon as possible.

Only 0.9% sodium chloride solution can be used to dissolve the lyophilisate. It is recommended to administer the drug immediately after its preparation. If necessary, it can be stored at temperatures up to 30 ° C for 12 hours.

Do not mix or inject the Nexium injection solution simultaneously with other drugs.

The dosage regimen is determined by the indications (daily dose with a frequency of use 1 time per day):

• Esophagitis in gastroesophageal reflux disease (treatment): children 1-11 years old weighing up to 20 kg - 10 mg, children 1-11 years old weighing from 20 kg - 10 or 20 mg, children from 12 years old and adults - 40 mg;
• Gastroesophageal reflux disease (symptomatic treatment): children 1-11 years old - 10 mg, children from 12 years old and adults - 20 mg;
• Peptic ulcers associated with taking non-steroidal anti-inflammatory drugs (treatment for the purpose of healing): adults - 20 mg;
• Peptic ulcers associated with the use of non-steroidal anti-inflammatory drugs (prophylaxis): adults - 20 mg.

In order to prevent recurrence of bleeding from a peptic ulcer after endoscopic hemostasis, as a rule, 80 mg of Nexium is used as an intravenous infusion over 30 minutes, followed by an extended intravenous infusion at a dose of 8 mg per hour for 72 hours. To suppress the secretion of acid after the end of parenteral use of the drug, it is recommended to carry out antisecretory therapy (for example, for 1 month, esomeprazole 1 time per day, 40 mg).

The duration of the introduction of Nexium is:

• Intravenous injections: at a dose of 10, 20 and 40 mg - from 3 minutes;
• Intravenous infusions: at a dose of 10, 20 and 40 mg - 10-30 minutes; 80 mg - 30 minutes; 8 mg / h - 71.5 hours (extended infusion).

When bleeding from a peptic ulcer in patients with severe hepatic impairment, Nexium is prescribed 80 mg as an intravenous infusion over 30 minutes, followed by an extended intravenous infusion at a maximum dose of 4 mg per hour for 71.5 hours.

Dosage adjustments in elderly patients should not be made.

In case of impaired renal function during the use of Nexium in any dosage form, the dose should not be adjusted. In patients with renal insufficiency, the drug is prescribed with caution.

Due to limited clinical experience, Nexium should be used with caution in patients with severe hepatic impairment. The maximum daily dose in adults and children from 12 years old should not exceed 20 mg, in children 1-11 years old - 10 mg.

Side effects

• Musculoskeletal system: rarely - myalgia, arthralgia; very rarely - muscle weakness;
• Nervous system: often - headache; infrequently - drowsiness, paresthesia, dizziness; rarely - a violation of taste;
• Urinary system: very rarely - interstitial nephritis;
• Hematopoietic system: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis, pancytopenia;
• Gastrointestinal tract: often - vomiting and / or nausea, constipation, abdominal pain, flatulence, diarrhea; infrequently - dry mouth; rarely - stomatitis, candidiasis of the gastrointestinal tract; very rarely - microscopic colitis confirmed by histological studies;
• Respiratory system: rarely - bronchospasm;
• Reproductive system and mammary glands: very rarely - gynecomastia;
• Skin and subcutaneous tissues: often - reactions at the injection site of the solution (with intravenous administration); infrequently - itching, dermatitis, rash, urticaria; rarely - photosensitivity, alopecia; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme;
• Organ of vision: rarely - blurred vision;
• Liver and biliary tract: infrequently - increased activity of liver enzymes; rarely - hepatitis (with or without jaundice); very rarely - liver failure, encephalopathy in patients with liver disease;
• Mental disorders: infrequently - insomnia; rarely - depression, agitation, confusion; very rarely - hallucinations, aggressive behavior;
• Allergic reactions: rarely - hypersensitivity reactions (in the form of fever, angioedema, anaphylactic shock and / or anaphylactic reactions);
• Metabolism: rarely - hyponatremia; very rarely - hypomagnesemia, hypocalcemia associated with severe hypomagnesemia, hypokalemia associated with hypomagnesemia;
• Others: infrequently - peripheral edema; rarely - malaise, sweating.

In critically ill patients with intravenous administration of Nexium, especially when using high doses, irreversible visual impairment may develop (a causal relationship with therapy has not been established).

special instructions

When conducting long-term therapy (especially longer than 12 months), patients should undergo regular medical examinations.

With the development of any alarming signs (vomiting with blood, repeated vomiting, dysphagia, significant sudden weight loss), as well as with a stomach ulcer (or if it is suspected), the presence of malignant neoplasms should be excluded, since Nexium therapy is due to the smoothing of symptoms may delay diagnosis.

When conducting combined treatment for Helicobacter pylori, it is necessary to take into account the possibility of drug interactions of all drugs used.

If there is a high risk of developing osteoporosis or fractures, careful monitoring is necessary for the condition of patients.

During the use of Nexium, care must be taken when driving vehicles, since dizziness, blurred vision and drowsiness may develop during therapy.

drug interaction

With the joint appointment of Nexium with some drugs, the following effects may develop:

• Digoxin: strengthening its absorption;
• Rifampicin, preparations of St. John's wort: a decrease in the concentration of esomeprazole in the blood plasma;
• Itraconazole, ketoconazole, erlotinib: decrease in their absorption;
• Saquinavir, methotrexate, tacrolimus: an increase in their serum concentration;
• Antiretroviral drugs (nelfinavir, atazanavir): a decrease in their serum concentration (simultaneous use is not recommended);
• Clomipramine, citalopram, diazepam, phenytoin, imipramine and other drugs in the metabolism of which the CYP2C19 isoenzyme is involved: an increase in their plasma concentration;
• Phenytoin: increase in its residual concentration in patients with epilepsy.

Terms and conditions of storage

Keep out of the reach of children.

Best before date:

• Granules and pellets for the preparation of a suspension for oral administration: 3 years at a storage temperature of up to 25 ° C;
• Tablets: 3 years when stored at 30°C;
• Lyophilizate for the preparation of an injection solution: 2 years at a storage temperature of up to 30 ° C in a place protected from light. A vial with the drug under room lighting without carton packaging can be stored up to 24 hours.

spravka03.net

Nexium application (instruction)

Tablets Nexium instruction

Instructions for the drug Nexium are enclosed in each package with tablets and contain all the necessary information about it. Here is information about the composition of the tablets, terms and conditions of storage. Pharmacological and pharmacokinetic data are intended to increase the patient's knowledge of the effect of this drug. Indications for use are described in detail in the accompanying sheet and recommendations are given for its use with a dosing regimen.

It also contains instructions and warning instructions about the contraindications of Nexium tablets, side effects from their treatment and cases of overdose. Descriptions of drug interactions of the drug with other drugs and recommendations for use by various categories of patients are given.

Form, composition, packaging

Nexium 20 mg is produced in the form of tablets, which are coated with an oblong biconvex shell. The color is light pink. Both sides of the tablet are engraved with "20mG" on one side and "A/EN" on the other. The kink of the tablet is white interspersed with yellow.

The active substance of the drug is esomeprazole magnesium trihydrate in an amount that corresponds to a concentration of esomeprazole 20 milligrams. As auxiliary substances, glyceryl monostearate, hyprolose, hypromellose, iron oxide red dye (E172), iron oxide yellow dye (E172), magnesium stearate, copolymer of methacrylic and ethacrylic acid taken one to one, microcrystalline cellulose, paraffin, macrogol, polysorbate 80 , crospovidone, sodium stearyl fumarate, sucrose spherical granules, titanium dioxide (E171), talc, triethyl citrate in the required proportions.

In pharmacies, the drug comes in packs of cardboard, which are equipped with the control of the first opening. It is possible to purchase a package with the drug, where four, two or one aluminum blister is placed with the number of tablets of 7 pieces.

The drug is released only on prescription.

Nexium 40 mg is produced in the form of tablets, which are coated with an oblong biconvex shell. Pink colour. Both sides of the tablet are engraved with "40mG" on one side and "A/EI" on the other. The kink of the tablet is white interspersed with yellow.

The active substance of the drug is esomeprazole magnesium trihydrate in an amount that corresponds to a concentration of esomeprazole 40 milligrams. Hyprolose, iron oxide red dye (E172), iron oxide yellow dye (E172), glyceryl monostearate, magnesium stearate, copolymer of methacrylic and ethacrylic acid taken one to one, triethyl citrate, microcrystalline cellulose, talc, hypromellose, paraffin, macrogol, crospovidone, sodium stearyl fumarate, polysorbate 80, sucrose spherical granules, titanium dioxide (E171) in the required proportions.

On pharmacy shelves, the drug can be seen in cardboard packs that have protection in the form of a first opening control. It is possible to choose a drug package containing one, two or four aluminum blisters with seven tablets each.

The drug is released only on prescription.

Terms and conditions of storage

The drug should be stored in its original packaging for no more than three years. The temperature in the place of storage should not exceed 30 degrees. Children should not have access to it.

Pharmacology

Being an inhibitor of H + - K + - ATPase, the drug is capable of reducing the secretion of hydrochloric acid in the stomach. This is possible due to specific inhibition of the proton pump in parietal cells.

Mechanisms of influence

Being a weak base, esomeprazole accumulates, turning into an active form in the acidic environment of the mucosa and its cells, parietal with secretory tubules. There, the proton pump and the enzyme H + - K + - ATP-ase are inhibited, as a result of which the gastric secretion, both basal and stimulated, is suppressed.

The effect of the drug on the formation of acid in the stomach

The pharmacological effect of taking the drug develops within an hour, regardless of the dose taken. Taking Nexium daily once a day for five days, you can achieve a decrease in the concentration of hydrochloric acid in the contents of the stomach by 90 percent.

Inhibition of hydrochloric acid formation and related therapeutic effects

After a month of treatment with Nexium (40 milligrams), about 78 percent of patients diagnosed with reflux esophagitis recover. As a result of the use of the drug for two months, up to 93 percent of patients are cured.

A two-time use of the drug at a dose of 20 milligrams per day with the addition of a course of treatment with appropriate antibiotics leads to the successful elimination of foci of Helicobacter pylori infection in a week of treatment. If the patient had no complications during the course of peptic ulcer, then after this course of treatment he will not need to prescribe antisecretory drugs in order to eliminate the symptoms and heal the ulcer.

Also, Nexium, according to confirmed endoscopic studies, is quite effective in bleeding from peptic ulcers.

Additional effect of acid suppression

When treated with Nexium, as well as with other antisecretory drugs, patients experience an increase in plasma gastrin concentration, which is associated with a decrease in acid formation. This process also affects the increase in the concentration of chromogranin, which in turn can affect the results of those studies that are conducted to detect a neuroendocrine tumor. To avoid errors in diagnosis, you should stop taking these medicines about two weeks before the examination.

In those patients who received esomeprazole preparations for a long time, both in adults and in children, the number of enterochromaffin-like cells may be increased. This phenomenon is associated with the fact that the content of gastrin increases in the plasma. However, it is not clinically significant.

Also, in patients after long-term treatment with antisecretory-type drugs, the formation of a glandular cyst in the stomach is often observed, which is due to a number of physiological changes in a pronounced suppression of acid formation. However, neoplasms are usually benign and reversible after appropriate treatment.

With treatment with drugs to suppress the formation of acid, there is a risk of infections in the gastrointestinal tract. This is due to the fact that the microflora of the stomach that exists in the normal state with the use of these drugs increases, not excluding the content of pathogens that lead to diseases.

The following should be noted: according to the results of comparative studies, it was found that the therapeutic efficacy of Nexium for the treatment of patients with peptic ulcer of the stomach is more pronounced. The same can be said about the implementation of preventive measures using the drug in relation to gastric and duodenal ulcers.

Pharmacokinetics

absorption and distribution

Since the active substance of the drug Nexium esomeprazole is unstable to acidic environments, in the manufacture of tablets it is wrapped in a shell that is not affected by gastric juice.

After taking the tablet, it is rapidly absorbed from the gastrointestinal tract. The maximum effect can be achieved in no more than two hours. The percentage of absolute bioavailability after taking the drug at a concentration of 40 milligrams once can be more than sixty and increase to almost ninety when taken daily. For a dosage of 20 milligrams of the drug, these figures will correspond to 50 and 68 percent. Almost complete (97%) binding to plasma protein occurs. If Nexium is taken simultaneously with food, the absorption of the active substance will be slowed down and reduced, but this has almost no effect on the effectiveness of the drug.

Metabolic processes and drug excretion

The main metabolites of esomeprazole that can be detected in plasma are its sulfo derivatives. Basically, the metabolism of the active substance occurs with the participation of several isoenzymes.

When taking the drug once a day, daily, its active substance is able to be completely excreted from the plasma. In the period between taking the drug, its accumulation does not occur.

Esomeprazole, in the form of its main metabolites, does not affect the secretion of gastric acid. They are excreted when taking the tablets orally with urine up to 80 percent, and the remaining amount is excreted along with the feces. Invariably, esomeprazole can only be detected in the urine, and then no more than 1 percent.

Pharmacokinetics Nexium. Special clinical cases

It is known that metabolism in the human body occurs at different rates. Therefore, patients are distinguished with slow and fast metabolic processes. Of course, the indicator of achieving the maximum concentration of the drug in plasma will be different for these categories of patients, which, in general, does not affect the dosage of the drug and the methods of its administration.

The metabolism of the active substance Nexium in elderly patients has practically no differences.

Hepatic insufficiency in a patient, which is expressed as mild or moderate severity, can lead to impaired metabolism of esomeprazole. When liver failure is severe, this may cause a decrease in the metabolism of the active substance of the drug.

Pharmacokinetics in patients with known renal insufficiency has not been studied. However, it can be assumed that in patients of this category, the metabolism of esomeprazole will remain unchanged. Since the kidneys do not excrete the substance itself, but only its metabolites.

All indicators regarding the intake of the drug at any of its concentrations in adolescents and patients in childhood are no different from those in adults.

Nexium indications for use

Nexium is indicated for use in those patients who suffer from the following diseases:

For gastroesophageal reflux disease:

• For the treatment of reflux esophagitis of an erosive nature;
• For the implementation of long-term maintenance therapy in those patients who have healed reflux esophagitis of the erosive type. Therapy is necessary in order to prevent the occurrence of relapse;
• For symptomatic therapy of gastroesophageal reflux disease.

With peptic ulcer of the duodenum and stomach (as a component of the combined therapy):

• For the treatment of duodenal ulcer associated with Helicobacter pylori;
• To carry out preventive measures to avoid the recurrence of peptic ulcer, which is associated with Helicobacter pylori;
• With long-term therapy that suppresses the formation of acid in those patients who have suffered bleeding from peptic ulcers.

With long-term use of non-steroidal anti-inflammatory drugs:

• In order to heal a stomach ulcer, which was formed with the use of NSAIDs;
• For preventive measures to prevent duodenal and gastric ulcers associated with the use of NSAIDs in those patients who are at risk.

In the presence of Zollinger-Ellison syndrome or other conditions that are characterized by hypersecretion of a pathological nature, for example, idiopathic.

Contraindications

It has a drug and a number of contraindications that should be taken into account when prescribing. So Nexium should not be used for treatment:

• With hereditary fructose intolerance;
• With glucose-galactose malabsorption;
• With insufficiency of sucrase-isomaltase;
• In children under 12 years of age, since there are no accurate data on the safety and efficacy of Nexium for this category of patients;
• In children after 12 years of age, do not use for any other indications, except for gastroesophageal reflux disease;
• When treating drugs with nelfinavir and atazanavir in order to exclude their combined use;
• With increased sensitivity to esomeprazole and other components of the drug.

Nexium requires careful appointment when a patient has severe renal failure.

Nexium instructions for use

The drug is taken orally. Each of the tablets must be swallowed as a whole without destroying the shell. Drink water.

For those patients who find it difficult to swallow a tablet, it can be dissolved in clean non-carbonated drinking water. Do not use other liquids. After the disintegration of the tablet, the contents of the glass should be drunk immediately. Then again fill the glass halfway with water and drink the remaining suspension of the drug.

For those patients who cannot swallow, the drug should be administered by administration through a nasogastric tube.

For adults and children over the age of twelve

Gastroesophageal reflux disease

The appointment of the drug Nexium is carried out in single doses of 40 milligrams per single dose during the day, lasting 1 month. If the symptoms of the disease persist after treatment, an additional monthly course of therapy can be prescribed.

Long-term maintenance therapy for those who have recovered from erosive esophagitis

To avoid possible relapses of the disease, the patient is prescribed a single dose of 20 milligrams of the drug per day.

Symptomatic therapy of gastroesophageal reflux disease without esophagitis

Nexium is prescribed at 20 milligrams for a single dose per day for four weeks. Non-cessation of symptoms requires additional examination of the patient. When the symptoms are eliminated, they switch to taking the drug as needed, when symptoms occur and until they are removed, 1 tablet of 20 milligrams is allowed. However, in this regimen, Nexium should not be taken by those patients who take NVPS and are at risk of developing ulcers in the gastrointestinal tract.

Adults Only

Peptic ulcer of the duodenum and stomach

For treatment, the drug is used as part of combination therapy, where Nexium is prescribed in single doses of 20 milligrams together with amoxicillin at a concentration of 1 gram and clarithromycin 500 milligrams each. Each of the medicines should be taken twice a day for one week.

For long-term acid suppression therapy in patients who have experienced bleeding from a peptic ulcer

Tablets are prescribed 40 milligrams once a day within a month after the treatment with antisecretory drugs is completed by intravenous administration.

For the treatment of ulcers due to long-term use of NSAIDs

20 or 40 milligrams once a day. The course of treatment is a month or a half.

For preventive measures of gastric or duodenal ulcers from taking NVPS

Take Nexium once a day at 20 or 40 milligrams.

In those conditions of the patient that are characterized by hypersecretion of a pathological nature (Zollinger-Ellison syndrome, idiopathic hypersecretion)

It is recommended in the initial dose of 40 milligrams twice a day. Further, the doctor doses the drug, using an individual approach to the patient. The duration of therapy directly depends on the clinical manifestations of the disease.

Kidney dysfunction

There is no need to adjust the dosage, however, if the violations are severe, then the drug should be used carefully.

Violation of the functionality of the liver

When violations are of mild or moderate severity, there is no need to adjust the dose, but in severe violations, the maximum daily dose is 20 milligrams of the drug and no more.

In old age

The dosing regimen is unchanged.

The use of Nexium for children

The use of Nexium for children is contraindicated before they reach the age of 12 years, since there is no data on how safe and effective the drug is for the child's body.

Nexium during pregnancy

It is not advisable to prescribe Nexium during pregnancy, since there is no reliable data on its use for a woman who is expecting a baby. Also, it is not known whether the drug is excreted in breast milk. Therefore, lactating women should not use the drug.

Instructions for use of the drug by nasogastric tube

• Pour a tablet placed in a syringe with drinking water in an approximate amount of 25 to 50 milliliters and add air in a 5 milliliter volume.
• Shake the syringe well, dissolving the tablet for about two minutes.
• Hold the syringe in your hands with the tip up to prevent clogging.
• While continuing to hold the syringe in this direction, insert its tip into the probe.
• Shake the syringe to turn it over. Tip at the bottom. Quickly inject 5 to 10 milliliters of the drug solution into the tube. Then return the syringe to its original position.
• Repeat the procedure until the syringe is completely released.
• If a precipitate from the drug remains in the syringe, water (25 milliliters) and air (5 milliliters) should be added again and the injection procedure repeated.

Side effects

The drug Nexium has an extensive list of side effects, which must be taken into account when treating with its use.

Skin and subcutaneous tissue

• in the form of dermatitis
• in the form of itching
• in the form of a rash,
• In the form of urticaria;
• in the form of alopecia
• In the form of photosensitivity;
• in the form of erythema multiforme,
• In the form of Stevens-Johnson syndrome,
• In the form of toxic epidermal necrolysis.

Musculoskeletal system

• in the form of arthralgia
• in the form of myalgia;
• in the form of muscle weakness.

nervous system

• in the form of a headache;
• In the form of dizziness
• in the form of paresthesia
• in the form of drowsiness;
• In the form of a violation of taste.

Mental disorders

• in the form of insomnia;
• In the form of depression
• In the form of excitement
• in the form of confusion;
• as hallucinations,
• in the form of aggressive behavior.

Digestive system

• In the form of pain in the abdomen,
• In the form of constipation
• in the form of diarrhea
• in the form of flatulence
• In the form of attacks of nausea and vomiting;
• In the form of dry mouth;
• in the form of stomatitis
• In the form of candidiasis of the gastrointestinal tract;
• In the form of microscopic colitis;

Liver and bile ducts

• In the form of increased activity of liver enzymes;
• In the form of hepatitis;
• as liver failure,
• In the form of encephalopathy in patients with hepatic diseases.

reproductive system

Hematopoietic system

• in the form of leukopenia
• In the form of thrombocytopenia;
• In the form of agranulocytosis,
• In the form of pancytopenia;

Allergy

• Like hay fever
• in the form of angioedema,
• In the form of anaphylactic shock;

Respiratory system

Urinary system

• In the form of interstitial nephritis;

Organs of vision

• In the form of blurred vision;

Metabolism

• In the form of hyponatremia;
• In the form of hypomagnesemia,
• In the form of hypocalcemia due to severe hypomagnesemia,
• In the form of hypokalemia due to hypomagnesemia.

Others:

• In the form of peripheral edema;
• In the form of malaise and sweating.

Overdose

Cases of overdose with Nexium were quite rare.

Symptoms of excessive use of the drug in a dose of up to 280 milligrams, there were manifestations of general weakness of the body and side effects from digestion. Taking the drug at a time at once 80 milligrams does not cause any signs of overdose.

To eliminate the consequences of an overdose, symptomatic and supportive treatment should be carried out. There is no specific antidote. Carrying out dialysis will not give the expected effect, since the active substance of the drug has good binding to plasma protein.

Drug Interactions

Since the action of the drug Nexium is based on the suppression of the formation of acid in the stomach, this can significantly affect the pharmacological and pharmacokinetic effects of other drugs when they are used together.

• Decreased absorption of ketoconazole, itraconazole, erlotinib.
• Increased absorption of digoxin.
• It is not recommended to take Nexium together with antiretroviral drugs: atazanovir and nelfinovir due to the effect of its active substance on the absorption of these drugs.
• Increased plasma concentrations of diazepam, citalopram, imipramine, clomipramine, phenytoin. This is especially important to consider if you take Nexium in the "as needed" mode.
• If Nexium is used at a concentration of 40 mg together with phenytoin in patients with epilepsy, then it is necessary to control the residual concentration of the latter in the patient's plasma both at the beginning of Nexium therapy and canceling it.
• The use of the drug in conjunction with tacrolimus leads to an increase in its concentration in the patient's blood serum.
• The use of methotrexate requires a temporary withdrawal of drugs with esomeprazole, since it significantly increases its concentration.
• The drug Nexium does not contribute to a change in the pharmacokinetic parameters of quinidine and amoxicillin.
• Nexium does not interact with naproxen and rofecoxib.
• The combined use of esomeprazole preparations with clarithromycin and variconazole requires dose adjustment of esomeprazole for those patients who suffer from liver disorders, as well as if the use of drugs is prolonged.
• Rifampicin and St. John's wort reduce the plasma concentration of esomeprazole preparations.

Preparations with the active substance esomeprazole also interact with other medicines. However, their pharmacological and pharmacokinetic actions are not yet fully understood.

Additional instructions

When a patient has alarming symptoms in the form of significant spontaneous weight loss, repeated vomiting attacks, especially with an admixture of blood, dysphagia or black semi-liquid stools with an unpleasant odor, and a stomach ulcer is diagnosed, before starting treatment with Nexium, an examination should be carried out to exclude the presence of a malignant tumor. Otherwise, the drug can smooth out its symptoms and lead to a delay in the correct diagnosis.

With prolonged use of drugs with a similar active substance, atrophic gastritis has occasionally been noted in patients.

Long-term use of Nexium, especially if it lasts more than a year, requires regular medical supervision.

Taking the drug in the "as needed" mode, patients should be attentive to their condition. Don't forget about drug interactions. The slightest change in symptoms should be reported to the doctor.

When prescribing complex therapy with the participation of esomeprazole preparations, it is necessary to take into account their interaction with other medicinal components, as well as possible contraindications and side effects of each of them.

Nexium tablets contain a certain amount of sucrose, so it is not recommended to prescribe the drug to those patients who have an appropriate intolerance.

According to unconfirmed research data, some association has been established between taking the drug and an increased risk of fractures in patients with osteoporosis. Although the data are not reliable, patients with osteoporosis during treatment should be kept under observation in a hospital setting.

Due to the occurrence of states of drowsiness, loss of clarity of vision and dizziness during treatment, you should refrain from driving vehicles and working with mechanisms.

Nexium analogues

Analogues of the drug Nexium are preparations with the same active substance esomeprazole, which are also produced in the form of enteric-coated tablets. They are called Esomeprazole and Neo-Zext. These medications can successfully replace Nexium during treatment.

Nexium price

The cost of the drug is quite high and depends on the number of tablets in the package and the concentration of its active substance.

Nexium 20 mg price

The price of Nexium 20 mg is 2692 rubles per pack of tablets, where there are 28 pieces. A package with fourteen tablets will cost the patient 1413 rubles.

Nexium 40 mg price

The price of the drug Nexium 40 mg per package, where 14 tablets are invested, is 1400 rubles, and the corresponding pack inside which 28 pieces of the drug will cost 3395 rubles.

Nexium reviews

There are not so many reviews about Nexium, however, almost all of them are in a positive way. People like the effectiveness of the drug, but its high cost and a large list of side effects prevent many from using pills for treatment. There are also such patients who purchased the medication, despite its cost and note its uselessness for themselves, but there are not many of them, mainly those who underwent course treatment with the drug were satisfied with its therapeutic effect.

Galina: I can evaluate Nexium from the category of expensive medicines as a highly effective medicine, however, based on my own experience, I do not recommend its long-term use. Course application, I think is more than enough, and you should not delay the treatment further. Further, oddly enough, it can get worse. Personally, having problems with my stomach, like many, for reliability, I decided to take a medicine that helps so well for a longer time, and the pills still remained after the end of the course. However, everything is fine while you drink them, as soon as you stop, everything starts to hurt again and a whole bunch of side effects appear. In general, the withdrawal of such treatment is effective, but should be carried out in moderation.

Khanuma: My husband had stomach problems for a long time, and you can't lure him to the hospital. Well, I also decided to check my stomach and at the same time persuade him to go, how much you can suffer. It turned out he had reflux, and the doctor prescribed him several drugs, including Nexium. It must be said that the drug is not cheap, but health is more expensive, therefore, having bought everything strictly according to the prescription, they began treatment. There were fourteen large tablets in the pack, which are not so easy to swallow. After my husband drank one blister, his pains noticeably eased, and he even began to eat with pleasure. And recently, because of the pain, he became very irritable at the table. However, at the next examination, the doctor said that the medicine would have to be bought in addition. Expensive, what can I say. But seeing its effectiveness, let's go to the pharmacy unconditionally. Of course, I can recommend the drug to everyone in need, it helps perfectly, but without a doctor's prescription, you probably shouldn't carry out treatment. Take better care of your stomach.

Julia: No one will argue that today it is very difficult to stay within the framework of proper nutrition, when there are so many temptations around. However, everyone knowing the price of preservatives, food additives and other components of beautiful food packaging that are not useful for the stomach, not to mention fast food, still consumes all this every day, hoping that digestive problems and even worse gastrointestinal diseases will bypass him. And I was no exception. Having a higher medical education, and perfectly understanding all this, I still like to eat unhealthy food. As a result, gastritis and all its charms. However, I suffered so much until I discovered Nexium for myself - a miracle drug that is literally effective. Its only drawback is the cost, which is quite impressive, but the result is worth it. One pill saves me from pain and brings me back to life within half an hour. Another advantage for me in this preparation is the form of its release. Because I can't drink drugs that taste on my tongue, I immediately begin to vomit. I also endure the injections with difficulty, because for a long time I suffer from the pain of a certain place after them. And Nexium tablets are a godsend for me in this regard. You can’t chew them, too, until you swallow, there is no taste either, because they are in the shell. In a word, this medicine suits me in all respects, I have already come to terms with the cost. Thus, I want to summarize and say that the drug is very effective in the presence of problems with the digestive tract. I have been using it for more than five years when necessary, and it has never let me down. However, in recommending a remedy, I do not encourage anyone to self-medicate. Before using it, I advise you to consult a doctor. I did the same when I decided to try it for the first time.

Victor: Having a whole range of problems with the digestive tract, he sought medical help and, having passed the necessary examination, received a doctor's prescription for treatment. Having suffered enough with my sores, I decided to strictly follow the doctor's instructions and bought everything at the pharmacy according to the prescription, although it did not cost me cheap. Among the prescriptions was the drug Nexium, for which I needed as many as three packs for treatment, when even one is very expensive. But as I already said, I decided to buy everything for a full course of treatment and approach it with all responsibility. To my great regret and surprise, Nexium did not help me at all. Although I took his full course and fulfilled all the prescriptions of the attending physician. Complete disappointment. It's a shame not even for the high costs of such an imaginary treatment, but simply for the lost time and the problem that has not gone away. Therefore, I want to sincerely wish all my fellow sufferers, when you are prescribed an expensive drug, do not take it in full, but take one package for a test and see what effect it will have on you. Perhaps the drug Nexium is really very effective, as many write about it, but for some reason its effect did not manifest itself in me. Maybe he just doesn't suit me. After all, each person's body is different. Be healthy.

Yana: My acquaintance with the drug Nexium began after a visit to a doctor who, after I applied with terrible pain in the abdomen, first prescribed me an examination and, based on its results, treatment with these pills. He somehow kept silent about the cost of the drug. Arriving at the pharmacy, I went home with nothing, because I didn’t even have money for one package of the drug with me. At home, I looked online for reviews about Nexium and decided, regardless of the cost, to try to get treated, because the reviews inspired confidence. I bought the pills the next day and started treatment. From the very first day of taking it, I began to suffer from headaches and dizziness, which are absolutely not characteristic of me. It turned out that these were the side effects of the pills. Since the treatment had just begun, I decided to be patient and continue it. Nevertheless, after drinking the whole package, I did not notice much improvement in the condition in the gastrointestinal tract, and I began to get used to the headache in two weeks of taking the drug. Another doctor's office. New Nexium appointment for another two weeks. She did not continue such treatment, deciding to look for an alternative. When I find something worthwhile, I will write a review again. In the meantime, I would like to advise everyone who needs help in treating diseases, use only effective therapy, and if it is clear that it does not suit you, it is better to replace it, doctors can also be wrong.

Lyubov: Having problems with the stomach, she practiced the experience of treatment on the recommendation of a doctor with Nexium. After drinking a dozen tablets for his intended purpose, I then confess I did not understand why I needed it. There were four tablets left, and I put them in the first-aid kit, they will suddenly come in handy. For a while, I didn’t even remember the stomach, but the drug helped, until one day I started having terrible heartburn. Having tried all the known remedies for her, in the form of soda and milk, she suddenly remembered Nexium tablets. Imagine my surprise when, in a matter of minutes, the unpleasant burning sensation disappeared, and the heartburn did not recur. Now I use the drug as needed, when heartburn sticks. It helps 100% and the pills have never failed. By the way, when she began to save herself from heartburn with the help of Nexium, she visits me much less often. I recommend to everyone who also suffers from this trouble, buy the drug - you will not regret it. The pills are expensive, but last a long time. I even sometimes take half a tablet, and it is enough. All health and excellent well-being.

Barbara: Periodically suffering from pain in the stomach, I was not particularly worried about this. I take a pill and after sitting on a sparing diet for several days, I felt that everything had returned to normal. However, as they say, for the time being. And so it turned out for me. Once my stomach was so seized that it was already before the diet, I went straight to the doctor. After a series of examinations, it seems that nothing particularly terrible was revealed, but a course of treatment was nevertheless prescribed. When I bought the medicine for treatment by prescription, I was unpleasantly shocked. One of the prescription drugs was very expensive. But I decided to heal. And although the family budget suffered a little during my treatment, the whole family unanimously approved the purchase of the medicine, which, by the way, turned out to be very effective and eliminated my pain literally at the beginning of the intake. However, following the doctor's instructions, I recovered and am very pleased with the effect. More than a year has passed, and the pain has never shown itself again. I recommend everyone to follow the doctor's prescriptions and not abandon the treatment halfway at the first relief. And it is better to take care of your health and not get sick at all.

Aleksey: I have been suffering from a stomach ulcer for more than a year, and periodically undergo treatment. Until recently, I did not know about Nexium, but then I received his appointment from my doctor. My doctor has been guiding me for a long time and knows my problems. They tried to treat my sore with various drugs and even folk remedies from which, of course, the effect was, but short-lived. But Nexium gave me more long-term relief. When the problem resumes, I immediately begin to take it and you can live on even without depriving yourself of your favorite food. As opposed to what it was before. I can’t even say what I suffered more from pain or from the prohibition of certain foods. Although, of course, at first there were doubts whether to buy it or not - it was too expensive. However, now I firmly believe and recommend it to everyone - an excellent drug for stomach problems. By the way, the instructions for the pills list a lot of side effects, the doctor warned me about them, as well as about the cost of the drug, but none of them touched me. Although, of course, you should pay attention to them, and discuss with your doctor. Treat yourself to health.

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