Overdose
To date, extremely rare cases of intentional overdose have been described. Oral administration of esomeprazole at a dose of 280 mg was accompanied by general weakness and gastrointestinal symptoms. A single dose of 80 mg of Nexium® 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 provided.
Drug interactions
The effect of esomeprazole on the pharmacokinetics of other drugs.
A decrease in the secretion of hydrochloric acid in the stomach during treatment with esomeprazole and other proton pump inhibitors can lead to a decrease or increase in the absorption of drugs, the absorption of which depends on the acidity of the environment. Like other drugs that reduce gastric acidity, treatment with esomeprazole may result in decreased absorption of ketoconazole, itraconazole and erlotinib, as well as increased absorption of drugs such as digoxin. Co-administration of omeprazole 20 mg once daily and digoxin increases the bioavailability of digoxin by 10% (the bioavailability of digoxin 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 omeprazole therapy may affect the absorption of antiretroviral drugs. Interaction at the level of the CYP2C19 isoenzyme is also possible. When omeprazole is co-administered with certain antiretroviral drugs, such as atazanavir and nelfinavir, during omeprazole therapy, a decrease in their serum concentrations is observed. Therefore, their simultaneous use is not recommended. Co-administration of omeprazole (40 mg once daily) with atazanavir 300 mg/ritonavir 100 mg in healthy volunteers resulted in a significant decrease in the bioavailability of atazanavir (AUC, Cmax and Cmin decreased by approximately 75%). Increasing the atazanavir dose to 400 mg did not compensate for the effect of omeprazole on the bioavailability of atazanavir.
With the simultaneous use of omeprazole and saquinavir, an increase in the concentration of saquinavir in the serum was noted; when used 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 antiretroviral drugs 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., may lead to increased plasma concentrations of these drugs, which, in turn, may require dose reduction. This interaction is especially important to remember when using Nexium® in an as-needed regimen. When 30 mg of esomeprazole and diazepam, which is a substrate of the CYP2C19 isoenzyme, are taken together, a decrease in the clearance of diazepam by 45% is observed.
The use of esomeprazole at a dose of 40 mg led to an increase in residual phenytoin concentrations in patients with epilepsy by 13%. In this regard, it is recommended to monitor plasma concentrations of phenytoin when starting treatment with esomeprazole and when discontinuing it.
The use of omeprazole at a dose of 40 mg once daily led to an increase in the area under the concentration-time curve and Cmax of voriconazole (CYP2C19 isoenzyme substrate) by 15% and 41%, respectively.
Co-administration of warfarin with 40 mg esomeprazole does not lead to a change in coagulation time in patients taking warfarin for a long time. However, several cases of clinically significant increases in INR (international normalized ratio) have been reported with the combined use of warfarin and esomeprazole. It is recommended to monitor the INR at the beginning and at the end of the combined use of esomeprazole and warfarin or other coumarin derivatives.
According to the results of the studies, a pharmacokinetic/pharmacodynamic interaction was noted between clopidogrel (loading dose of 300 mg and maintenance dose of 75 mg/day) and esomeprazole (40 mg/day orally), which leads to a decrease in the exposure of the active metabolite of clopidogrel by an average of 40% and a decrease in maximum inhibition of ADP-induced platelet aggregation by an average of 14%.
The clinical significance of this interaction is unclear. In a prospective study in patients receiving placebo or omeprazole 20 mg/day. simultaneously with therapy with clopidogrel and acetylsalicylic acid (ASA), and when analyzing the clinical outcomes of large-scale randomized trials, there was no increase in the risk of cardiovascular complications with the combined use of clopidogrel and proton pump inhibitors, including esomeprazole.
The results of a number of observational studies are contradictory and do not provide a clear answer about the presence or absence of an increased risk of thromboembolic cardiovascular complications during the combined use of clopidogrel and proton pump inhibitors.
When clopidogrel was used together with a fixed combination of 20 mg esomeprazole and 81 mg ASA, exposure to the active metabolite of clopidogrel decreased by almost 40% compared with clopidogrel monotherapy, while the maximum levels of inhibition of ADP-induced platelet aggregation were the same, which is likely due to simultaneous administration ASA in low dose.
Esomeprazole, like omeprazole, inhibits the CYP2C19 isoenzyme. Co-administration of cilostazol and 40 mg omeprazole leads to an increase in the pharmacokinetic parameters of cilostazol in healthy volunteers: Cmax and AUC by 18% and 26%, respectively. Similar parameters of one of the active metabolites of cilostazol increase by 29% and 69%, respectively.
Co-administration of cisapride with 40 mg of esomeprazole leads to an increase in the pharmacokinetic parameters of cisapride in healthy volunteers: AUC by 32% and half-life by 31%, but the maximum concentration of cisapride in plasma does not change significantly. The slight prolongation of the QT interval, which was observed with cisapride monotherapy, did not increase with the addition of Nexium® (see section "Special Instructions").
With the simultaneous use of esomeprazole and tacrolimus, an increase in the concentration of tacrolimus in the blood serum was noted.
In some patients, an increase in the concentration of methotrexate was observed during combined use with proton pump inhibitors. When using high doses of methotrexate, the possibility of temporary withdrawal of esomeprazole should be considered.
Nexium® does not cause clinically significant changes in the pharmacokinetics of amoxicillin and quinidine.
Studies evaluating short-term co-administration of esomeprazole and naproxen or rofecoxib did not reveal a clinically significant pharmacokinetic interaction.
Effect of drugs on the pharmacokinetics of esomeprazole.
The isoenzymes CYP2C19 and CYP3A4 are involved in the metabolism of esomeprazole. The combined use of esomeprazole with clarithromycin (500 mg 2 times a day), which inhibits the CYP3A4 isoenzyme, leads to an increase in the AUC value of esomeprazole by 2 times. Co-administration of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19 isoenzymes, for example, voriconazole, may lead to a more than 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 liver dysfunction and with long-term use. Long-term use of the drug is not indicated for children and adolescents under 12 years of age.
Drugs that induce the isoenzymes CYP2C19 and CYP3A4, such as rifampicin and St. John's wort preparations, when used together with esomeprazole, may lead to a decrease in the concentration of esomeprazole in the blood plasma by accelerating the metabolism of esomeprazole.
Compound
Esomeprazole magnesium trihydrate 11.1 mg,
which corresponds to the content of esomeprazole 10 mg
Excipients: copolymer of methacrylic acid and ethyl acrylate (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, yellow iron oxide dye - 1.8 mg.
pharmachologic effect
Esomeprazole is the S-isomer of omeprazole and reduces gastric acid secretion by specifically inhibiting the proton pump in gastric parietal cells. The S- and R-isomers of omeprazole have similar pharmacodynamic activities.
Mechanism of action
Esomeprazole is a weak base that transforms into an active form 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, thereby inhibiting both basal and stimulated secretion of hydrochloric acid.
Effect on the secretion of hydrochloric acid in the stomach
The effect of esomeprazole develops within 1 hour after oral administration of 20 mg or 40 mg. When taking the drug daily for 5 days at a dose of 20 mg once a day, the average maximum concentration 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 patients with gastroesophageal reflux disease (GERD) and the presence of clinical symptoms, after 5 days of daily oral esomeprazole 20 mg or 40 mg, intragastric pH values above 4 were maintained for an average of 13 and 17 hours out of 24 hours. When taking esomeprazole at a dose of 20 mg per day, an intragastric pH value 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 is 97%, 92% and 56%, respectively.
A correlation was found between the concentration of the drug in plasma and the inhibition of hydrochloric acid secretion (the AUC parameter (area under the concentration-time curve) was used to assess the concentration).
The therapeutic effect achieved by inhibiting 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 disease after a week-long eradication course do not require subsequent monotherapy with drugs that reduce the secretion of gastric glands to heal the ulcer and eliminate symptoms.
The effectiveness of the drug Nexium® has been shown for bleeding from peptic ulcers, confirmed by endoscopic examination.
Use for GERD in children (aged 1-11 years)
Healing of erosive esophagitis, confirmed by endoscopic examination, was observed in 93.3% of patients aged 1-11 years after 8 weeks of therapy with Nexium®. Patients weighing less than 20 kg took Nexium® at a daily dose of 5 mg or 10 mg, and patients weighing more than 20 kg took a daily dose of 10 mg or 20 mg.
Other effects associated with inhibition of hydrochloric acid secretion
During treatment with drugs that reduce the secretion of gastric glands, the concentration of gastrin in the plasma increases as a result of a decrease in the secretion of hydrochloric acid. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. Increased concentrations of CgA 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 testing CgA concentrations. If during this time the CgA concentration has not returned to normal, the study should be repeated. In children and adult patients receiving esomeprazole for a long time, there is an increase in the number of enterochromaffin-like cells, probably associated with an increase in plasma gastrin concentrations. This phenomenon has no clinical significance.
Patients taking drugs that reduce the secretion of gastric glands for a long period of time are more likely to develop glandular cysts in the stomach. These phenomena are caused by physiological changes as a result of pronounced inhibition of hydrochloric acid secretion. Cysts are benign and undergo reverse development.
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 that 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 Salmonella spp., Campylobacter spp. and, in hospitalized patients, probably Clostridium difficile.
Nexium® showed superior efficacy compared to ranitidine in healing gastric ulcers in patients treated with nonsteroidal anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase-2 (COX-2) inhibitors.
Nexium® showed high effectiveness in preventing gastric and duodenal ulcers in patients receiving NSAIDs (age group over 60 years and/or with a history of peptic ulcers), including selective COX-2 inhibitors.
Pharmacokinetics.
Absorption and distribution
Esomeprazole is unstable in an acidic environment, so enteric-coated pellets are used for oral administration. Under in vivo conditions, only a small portion of esomeprazole is converted to the R-isomer. The drug is rapidly absorbed: maximum plasma concentration is achieved 1-2 hours after administration. The absolute bioavailability of esomeprazole after a single dose of 40 mg is 64% and increases to 89% with daily dosing once daily. For a dose of 20 mg esomeprazole, these figures are 50% and 68%, respectively. The volume of distribution at steady state concentration in healthy people is approximately 0.22 l/kg body weight. Esomeprazole is 97% bound to plasma proteins.
Eating slows down and reduces the absorption of esomeprazole in the stomach, but this does not have a significant effect on the effectiveness of inhibition of hydrochloric acid secretion.
Metabolism and excretion
Esomeprazole is metabolized via the cytochrome P450 system. The main part is metabolized with the participation of a specific polymorphic isoenzyme CYP2C19, resulting in the formation of hydroxylated and demethylated metabolites of esomeprazole. The remainder is metabolized by the CYP3A4 isoenzyme; this produces a sulfo derivative of esomeprazole, which is the main metabolite detected in plasma.
The parameters given below mainly reflect the nature of pharmacokinetics in patients with increased activity of the CYP2C19 isoenzyme. The total clearance is approximately 17 l/h after a single dose of the drug and 9 l/h after repeated doses. The half-life is 1.3 hours when taken systematically once a day. The area under the concentration-time curve (AUC) increases with repeated dosing of esomeprazole. The dose-dependent increase in AUC with repeated administration of esomeprazole is non-linear, 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 inhibition of the CYP2C19 isoenzyme by esomeprazole and/or its sulfo derivatives. When taken daily once a day, esomeprazole is completely eliminated from the blood plasma in the interval 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 in the form of metabolites in the urine, the rest is excreted in feces. Less than 1% unchanged esomeprazole is found in 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 these patients, esomeprazole is metabolized primarily through the action of CYP3A4. When systematically taking 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 maximum plasma concentrations in patients with reduced isoenzyme activity are increased by approximately 60%. These features do not affect the dose and method of administration of esomeprazole. In elderly patients (71-80 years), the metabolism of esomeprazole does not undergo significant changes.
After a single dose of 40 mg esomeprazole, the average AUC value in women is 30% higher than that in men. When taking the drug daily once a day, there are no differences in pharmacokinetics between men and women. These features do not affect the dose and method of administration of esomeprazole. In patients with mild to moderate hepatic impairment, the metabolism of esomeprazole may be impaired. In patients with severe liver failure, the metabolic rate is reduced, which leads to a 2-fold increase in the AUC value for esomeprazole. For patients with severe liver failure, the maximum daily dose should not exceed 20 mg. When taken once a day, no accumulation of esomeprazole and its main metabolites was observed.
Pharmacokinetic studies have not been conducted in patients with renal failure. Since it is not esomeprazole itself that is excreted through the kidneys, but its metabolites, it can be assumed that the metabolism of esomeprazole in patients with renal failure does not change.
In children aged 12-18 years, after repeated administration of 20 mg and 40 mg of esomeprazole, the AUC and TCmax values in the blood plasma were similar to the AUC and TCmax values in adults.
In children aged 1-11 years, after repeated dosing of 10 mg esomeprazole, the AUC value was similar to the AUC value in adolescents and adults when taking 20 mg esomeprazole.
In children aged 1-11 years, after repeated dosing of 20 mg esomeprazole, the AUC value was 6-11 times higher than the AUC value in adolescents and adults when taking 20 mg esomeprazole.
special instructions
If any alarming symptoms are present (eg, significant spontaneous weight loss, repeated vomiting, dysphagia, hematemesis, or melena), or if a gastric ulcer is present (or if a gastric ulcer is suspected), malignancy should be excluded because Treatment with Nexium® may lead to a smoothing of symptoms and delay diagnosis.
In rare cases, in patients who took omeprazole for a long time, histological examination of biopsies of the mucous membrane of the gastric body revealed atrophic gastritis.
Patients taking the drug for a long period (especially more than a year) should be under regular medical supervision.
Long-term use of the drug is not indicated for children and adolescents under 12 years of age.
Patients taking Nexium® on an as-needed basis should be instructed to contact their physician if their 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 section “Interaction with other drugs and other types of drug interactions”). 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 the CYP3A4 isoenzyme, therefore, when prescribing eradication therapy to patients receiving other drugs metabolized by the CYP3A4 isoenzyme (for example, cisapride), it is necessary to take into account possible contraindications and interactions of clarithromycin with these drugs.
The drug Nexium® contains sucrose and dextrose, therefore it is contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency.
According to the study results, a pharmacokinetic/pharmacodynamic interaction was noted between clopidogrel (loading dose of 300 mg and maintenance dose of 75 mg/day) and esomeprazole (40 mg/day orally), which leads to a decrease in exposure to the active metabolite of clopidogrel by an average of 40% and a decrease in maximum inhibition of ADP-induced platelet aggregation by an average of 14%. Therefore, the simultaneous use of esomeprazole and clopidogrel should be avoided (see section “Interaction with other drugs and other types of drug interactions”).
Individual observational studies indicate that proton pump inhibitor therapy may modestly increase the risk of osteoporosis-related fractures, but other similar studies have not reported an increased risk.
Randomized, double-blind, controlled clinical trials of omeprazole and esomeprazole, including two open-label studies of long-term therapy (more than 12 years), did not confirm the association of osteoporotic fractures with the use of proton pump inhibitors. Although a causal relationship between the use of omeprazole/esomeprazole and osteoporotic fractures has not been established, patients at risk of developing osteoporosis or osteoporotic fractures should be under appropriate clinical supervision.
Impact on the ability to drive vehicles and operate machinery
Due to the fact that dizziness, blurred vision and drowsiness may occur during therapy with Nexium®, caution should be exercised when driving vehicles and other mechanisms.
Indications for use
GERD:
treatment of erosive reflux esophagitis;
long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse;
symptomatic treatment of GERD.
Peptic ulcer of the stomach and duodenum
As part of combination therapy:
treatment of duodenal ulcer associated with Helicobacter pylori;
prevention of relapses of peptic ulcers associated with Helicobacter pylori.
Long-term acid suppression therapy in patients who have suffered bleeding from a peptic ulcer (after intravenous use of drugs that reduce the secretion of gastric glands to prevent relapse).
Patients taking NSAIDs for a long time:
healing of stomach ulcers associated with taking NSAIDs;
prevention of gastric and duodenal ulcers associated with taking NSAIDs in patients at risk;
Zollinger-Ellison syndrome or other conditions characterized by pathological hypersecretion of the gastric glands, incl. idiopathic hypersecretion.
Directions for use and doses
Nexium® in the dosage form of enteric-coated pellets and granules for oral suspension is intended primarily for pediatric patients and persons with difficulty swallowing.
Inside. To take 10 mg of Nexium®, pour the contents of one packet into a glass containing 15 ml of water. To take 20 mg of Nexium®, pour the contents of 2 packets into a glass containing 30 ml of water. To take 40 mg of Nexium®, pour the contents of 4 packets into a glass containing 60 ml of water. The contents of the glass should be stirred and waited a few minutes for a suspension to form. The suspension can be taken orally immediately or within 30 minutes after preparation, stirring again before use. Then you should again add 15 ml of water to the glass, stir the remainder and take it orally. Carbonated water should not be used. Pellets and granules must not be chewed or crushed.
The suspension can be administered through a nasogastric tube. Instructions for preparing and administering the drug through a nasogastric tube are given in the section “Administering the drug through a nasogastric tube.”
Children 1-11 years old with body weight > 10 kg
GERD
Treatment of erosive reflux esophagitis: for patients weighing more than 10 kg but less than 20 kg - 10 mg once a day for 8 weeks. For patients weighing 20 kg or more - 10 mg or 20 mg once a day for 8 weeks.
Symptomatic treatment of GERD: 10 mg once a day for up to 8 weeks. The use of esomeprazole in doses greater than 1 mg/kg/day has not been studied.
Adults and children from 12 years old
GERD
Treatment of erosive reflux esophagitis: 40 mg once a day for 4 weeks.
An additional 4-week course of treatment is recommended in cases where, after the first course, healing of esophagitis does not occur or symptoms persist.
Long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse: 20 mg once a day.
Symptomatic treatment of GERD: 20 mg once daily for patients without esophagitis. If symptoms do not disappear after 4 weeks of treatment, the patient should be further examined. After eliminating the symptoms, you can switch to the “as needed” regimen of taking the drug, i.e. take Nexium® 20 mg once daily if symptoms return. For patients taking NSAIDs who are at risk of developing gastric or duodenal ulcers, treatment on an as-needed basis is not recommended.
Adults
Peptic ulcer of the stomach and duodenum
As part of combination therapy for eradication with Helicobacter pylori:
treatment of duodenal ulcer associated with Helicobacter pylori: Nexium® 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All drugs are taken twice a day for 1 week.
prevention of relapse of peptic ulcers associated with Helicobacter pylori: Nexium® 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All drugs are taken twice a day for 1 week.
Long-term acid suppression therapy in patients who have suffered bleeding from a peptic ulcer (after intravenous use of drugs that reduce the secretion of gastric glands to prevent relapse)
Nexium® 40 mg 1 time per day for 4 weeks after the end of intravenous therapy with drugs that reduce the secretion of gastric glands.
Patients taking NSAIDs for a long time:
healing of stomach ulcers associated with taking NSAIDs: Nexium® 20 mg or 40 mg once a day. The duration of treatment is 4-8 weeks.
prevention of gastric and duodenal ulcers associated with taking NSAIDs: Nexium® 20 mg or 40 mg once daily.
Conditions associated with pathological hypersecretion of the gastric glands, including Zollinger-Ellison syndrome and idiopathic hypersecretion:
The recommended starting dose is Nexium® 40 mg twice daily. In the future, the dose is selected individually, the duration of treatment is determined by the clinical picture of the disease. There is experience using the drug in doses of up to 120 mg 2 times a day.
Children under 1 year of age or weighing less than 10 kg: Due to the lack of data on efficacy and safety, Nexium® should not be used in children under 1 year of age or weighing less than 10 kg.
Renal failure: no dose adjustment is required. However, experience with the use of Nexium® in patients with severe renal failure is limited; in this regard, caution should be exercised when prescribing the drug to such patients (see section “Pharmacokinetics”).
Liver failure: in case of mild to moderate liver failure, no dose adjustment is required. For patients with severe hepatic impairment, the maximum daily dose should not be exceeded - 10 mg for patients aged 1-11 years and 20 mg for patients over 12 years of age.
Elderly patients: no dose adjustment is required.
Administration of the drug through a nasogastric tube:
1. To administer 10 mg of Nexium®, pour the contents of one packet into a glass containing 15 ml of water.
2. To administer 20 mg of Nexium®, pour the contents of 2 packets into a glass containing 30 ml of water.
3. To administer 40 mg of Nexium®, pour the contents of 4 packets into a glass containing 60 ml of water.
4. Stir the contents of the glass and wait a few minutes for a suspension to form.
5. Mix the suspension again and draw it into the syringe.
6. Administer the suspension immediately or within 30 minutes after preparation.
7. Draw another 15 ml (for a dose of 10 mg), or 30 ml (for a dose of 20 mg), or 60 ml (for a dose of 40 mg) of water into the syringe, shake the syringe and inject the remaining suspension into the nasogastric tube.
Unused suspension should be destroyed.
Contraindications
Hypersensitivity to esomeprazole, substituted benzimidazoles or other ingredients included in the drug;
hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency;
children under 1 year of age or body weight less than 10 kg (due to the lack of data on the effectiveness and safety of the drug in this group of patients), children aged 1-11 years (for other indications, except for the treatment of erosive esophagitis and symptomatic treatment of GERD) and children over 12 years of age for indications other than GERD;
esomeprazole should not be taken together with atazanavir and nelfinavir (see section “Interaction with other drugs and other types of drug interactions”).
With caution: severe renal failure (experience is limited).
Use during pregnancy and breastfeeding
Currently, there is not enough data on the use of Nexium® during pregnancy. The results of epidemiological studies of omeprazole, which is a racemic mixture, showed the absence of fetotoxic effects or impaired fetal development.
When esomeprazole was administered to animals, no direct or indirect negative effects on the development of the embryo or fetus were detected. The introduction of a racemic mixture of the drug also did not have any negative effects on animals during pregnancy, childbirth, or during postnatal development.
The drug should be prescribed to pregnant women only if the expected benefit to the mother outweighs the possible risk to the fetus.
It is not known whether esomeprazole is excreted in breast milk, therefore Nexium® should not be administered during breastfeeding.
