Instruction for use: Nexium

Active substance Esomeprazol

ATX code A02BC05 Esomeprazol

Pharmacological group

Proton pump inhibitors

Nosological classification (ICD-10)

K21.0 Gastro-oesophageal reflux with oesophagitis

Reflux gastritis, Reflux esophagitis, Erosive and ulcerative esophagitis

K25 Gastric ulcer

Helicobacter pylori, Pain syndrome in gastric ulcer, Pain syndrome in gastric ulcer and duodenal ulcer, Inflammation of the gastric mucosa, Inflammation of the gastrointestinal mucosa, Benign gastric ulcer, The disease of the stomach and duodenum, asotsiirovannoe with Helicobacter pylori, Aggravation gastroduodenita on the background of peptic ulcer, Exacerbation of peptic ulcer, The aggravation of gastric ulcer, The organic gastrointestinal disease, Peptic ulcer of the stomach and duodenum, Postoperative gastric ulcer, Recurrent ulcers, Symptomatic gastric ulcers, Chronic inflammatory disease of the upper gastrointestinal tract, associated with Helicobacter pylori, Helicobacter pylori eradication, Erosive and ulcerative lesions of the stomach, Erosive lesions of the stomach, The erosion of the gastric mucosa, Peptic ulcer disease, Stomach ulcer, Gastric lesion, Ulcerative lesions of the stomach, Symptomatic ulcers of the stomach and duodenum

K26 Duodenal Ulcer

Pain with duodenal ulcer, Pain syndrome in gastric ulcer and duodenal ulcer, The disease of the stomach and duodenum, asotsiirovannoe with Helicobacter pylori, Exacerbation of peptic ulcer, The worsening of duodenal ulcer, Peptic ulcer of the stomach and duodenum, Relapse of duodenal ulcers, Symptomatic ulcers of the stomach and duodenum, Helicobacter pylori eradication, Erosive and ulcerative lesions of the duodenum, Erosive-ulcerative lesions of duodenal ulcers associated with Helicobacter pylori, Erosive lesions of the duodenum, Duodenal ulcer, Ulcerative lesions of the duodenum]

K31.8.2 * Hyperacidity of gastric juice

Pathological hypersecretion, Hyperacid indigestion, Hyperadic states, Increased secretion of gastric juice, Increased acid formation, Hyperacidosis,Hyper secretion of gastric juice, Increased acidity of gastric juice, High acidity

K86.8.3 * Zollinger-Ellison Syndrome

Adenoma of the pancreas ulzerogennosti, gastrinoma, Zollinger-Ellison Syndrome, gastrinoma

Y45 adverse reactions in therapeutic use of analgesic, antipyretic and anti-inflammatory agents

Composition

Tablets, coated 1 tab.

active substance:

Esomeprazole Magnesium Trihydrate 22.3 / 44.5 mg

(equivalent to 20/40 mg of esomeprazole, respectively)

excipients: glyceryl monostearate 40–55 - 1.7 / 2.3 mg; hyprolosis - 8.1 / 11 mg; hypromellose - 17/26 mg; iron dye red oxide (E172) - 0.06 / 0.45 mg; iron dye yellow oxide (E172) - 0.02 / - mg; magnesium stearate - 1.2 / 1.7 mg; methacrylic and ethacrylic acid copolymer (1: 1) - 35/46 mg; MCC - 273/389 mg; paraffin - 0.2 / 0.3 mg; macrogol - 3 / 4.3 mg; polysorbate 80 - 0.62 / 1.1 mg; Crospovidone - 5.7 / 8.1 mg; sodium fumarate - 0.57 / 0.81 mg; sucrose spherical granules (sugar, spherical granules, size 0.25–0.355 mm) - 28/30 mg; titanium dioxide (E171) - 2.9 / 3.8 mg; talc - 14/20 mg; triethyl citrate - 10/14 mg

Description of the dosage form

Tablets, 20 mg: oblong biconvex, light pink color, coated, with engraving "20 mg" on one side and "A / EH" - on the other.

Tablets, 40 mg: oblong biconvex, pink coated, with an engraving of "40 mg" on one side and "A / EI" - on the other.

The color on the break is white with yellow blotches (such as croup).

pharmachologic effect

Pharmacological action - inhibiting proton pump.

Pharmacodynamics

Esomeprazole is the S-isomer of omeprazole and reduces the secretion of hydrochloric acid in the stomach by specifically inhibiting the proton pump in the parietal cells of the stomach. S- and R-isomer of omeprazole have similar pharmacodynamic activity.

Mechanism of action

Esomeprazole is a weak base that becomes active 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, and inhibition of both basal and stimulated secretion of hydrochloric acid occurs.

Effect on gastric acid secretion

The effect of esomeprazole develops within 1 hour after oral administration of 20 or 40 mg. When taking the drug daily 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 patients with GERD and the presence of clinical symptoms, after 5 days of daily oral administration of esomeprazole at a dose of 20 or 40 mg, the intragastric pH above 4 was maintained for an average of 13 and 17 hours out of 24 hours. In patients receiving 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 of esomeprazole, this ratio was 97, 92 and 56%, respectively.

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

The therapeutic effect achieved by inhibiting the secretion of hydrochloric acid. When Nexium® is taken in a dose of 40 mg, reflux esophagitis heals in approximately 78% of patients after 4 weeks of therapy and in 93% of patients 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 lower the secretion of the gastric glands to heal the ulcer and eliminate the symptoms.

The effectiveness of Nexium® in bleeding from peptic ulcers has been shown in a study in patients with bleeding from peptic ulcers, confirmed endoscopically.

Other effects associated with inhibition of the secretion of hydrochloric acid. During treatment with drugs that lower the secretion of 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. Increasing the CgA concentration can influence the results of examinations to identify neuroendocrine tumors. To prevent this effect, therapy with proton pump inhibitors should be stopped 5–14 days prior to the study of CgA concentration. If during this time the concentration of CgA did not return to normal, the study should be repeated.

In children and adult patients who received esomeprazole for a long time, an increase in the number of enterochromaffin-like cells is observed, probably due to an increase in plasma gastrin concentration. This phenomenon has no clinical significance.

For patients for a long time taking drugs that lower the secretion of the glands of the stomach, more often marked the formation of glandular cysts in the stomach. These phenomena are due to physiological changes as a result of marked inhibition of the secretion of hydrochloric acid. The cysts are benign and reverse developed.

The use of drugs that suppress the secretion of hydrochloric acid in the stomach, including proton pump inhibitors, accompanied by an increase in the content of gastric microbial flora, normally present in the gastrointestinal tract. The use of proton pump inhibitors can lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract caused by bacteria of the genus Salmonella spp. and Campylobacter spp., and probably Clostridium difficile (in hospitalized patients).

In the course of two comparative studies conducted with ranitidine Nexium® showed the best efficacy in the healing of gastric ulcers in patients who received NSAIDs, including selective COX-2 inhibitors. In two studies, Nexium® showed high efficacy in the prevention of gastric and duodenal ulcers in patients who received NSAIDs (age group over 60 years old and / or with a peptic ulcer in history), including selective COX-2 inhibitors.

Pharmacokinetics

Absorption and distribution. Esomeprazole is unstable in an acidic environment, therefore, for oral use, tablets containing the drug granules are used, the shell of which is resistant to the action of gastric juice. In vivo, only a small fraction of esomeprazole is converted to the R-isomer. The drug is rapidly absorbed: Cmax in plasma is achieved within 1–2 hours after administration. The absolute bioavailability of esomeprazole after a single dose of 40 mg is 64% and increases to 89% on the background of daily intake 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 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 the secretion of hydrochloric acid.

Metabolism and excretion. Esomeprazole is metabolized by the cytochrome P450 system. The main part is metabolized with the participation of a specific polymorphic isoenzyme CYP2C19, thus forming hydroxylated and desmethylated metabolites of esomeprazole. Metabolism of the rest is carried out by CYP3A4 isoenzyme; this produces a sulfose derivative of esomeprazole, which is the main metabolite, which is determined in plasma.

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

Total Cl after a single dose of the drug is about 17 l / h, after repeated intake - 9 l / h. T1 / 2 - 1.3 hours with regular admission 1 time per day. AUC increases with repeated administration of esomeprazole. The dose-dependent increase in AUC upon repeated administration of esomeprazole is non-linear in nature, 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 sulfonic. With daily intake 1 time per day, esomeprazole is completely removed from the blood plasma during the interval between doses and does not accumulate.

The major 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 the feces. 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 isoenzyme CYP2C19. Approximately (2.9 ± 1.5)% of the population has decreased CYP2C19 isoenzyme activity. In these patients, the metabolism of esomeprazole is mainly carried out as a result of the action of CYP3A4. When systematically receiving 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. Mean plasma Cmax values in patients with reduced isoenzyme activity are increased by approximately 60%. These features do not affect the dose and method of application 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 in men. With daily intake of the drug 1 time per day, differences in pharmacokinetics in men and women are not observed. These features do not affect the dose and method of application of esomeprazole.

Liver failure. In patients with mild and moderate liver failure, the metabolism of esomeprazole may be disturbed. In patients with severe hepatic insufficiency, the metabolic rate is reduced, which leads to an increase in the value of AUC for esomeprazole by 2 times.

Renal failure. The study of pharmacokinetics in patients with renal insufficiency was not conducted. Since not the esomeprazole itself but its metabolites are eliminated through the kidneys, it can be assumed that the metabolism of esomeprazole does not change in patients with renal insufficiency.

Childhood. In children aged 12–18 years after repeated administration of 20 and 40 mg of esomeprazole, the value of AUC and Tmax in plasma was similar to the values of AUC and Tmax in adults.

Indications

gastroesophageal reflux disease:

- treatment of erosive reflux esophagitis;

- long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse;

- symptomatic treatment of gastroesophageal reflux disease;

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

- treatment of duodenal ulcer associated with Helicobacter pylori;

- prevention of recurrence of peptic ulcers associated with Helicobacter pylori;

long-term acid suppression therapy in patients who have undergone bleeding from peptic ulcers (after intravenous use of drugs that lower the secretion of the gastric glands) to prevent relapse;

long-term patients taking NSAIDs:

- the healing of gastric 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, including idiopathic hypersecretion.

Contraindications

hypersensitivity to esomeprazole, substituted benzimidazoles or other ingredients that make up the drug;

hereditary fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency;

combined use with atazanavir and nelfinavir (see. "Interaction");

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's age over 12 years old (according to other indications, except for gastroesophageal reflux disease).

With care: a heavy renal failure (experience of use is limited).

pregnancy and lactation

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 no fetotoxic effect or impaired fetal development.

With the introduction of esomeprazole animals did not reveal any direct or indirect negative impact on the development of the embryo or fetus. The introduction of the racemic mixture of the drug also did not have any negative impact on animals during pregnancy, childbirth, and postnatal development.

It is necessary to appoint drug to pregnant women only in that case when the expected advantage for mother exceeds possible risk for a fruit.

It is not known whether esomeprazole is excreted in breast milk; therefore, Nexium® should not be administered during breastfeeding.

Side effects

The following are side effects that are not dependent on the dosage regimen of the drug, noted during the use of Nexium®, both in clinical studies and in post-marketing research.

The frequency of side effects is given in the form of the following gradation: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000).

On the part of the skin and subcutaneous tissues: rarely - dermatitis, itching, rash, urticaria; rarely - alopecia, photosensitivity; very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the musculoskeletal and connective tissues: rarely - arthralgia, myalgia; very rarely - muscle weakness.

On the part of the nervous system: often - headache; infrequently - dizziness, paresthesias, drowsiness; rarely - a violation of taste.

Mental Disorders: Infrequently - insomnia; rarely - depression, agitation, confusion; very rarely - hallucinations, aggressive behavior.

On the part of the digestive tract: often - abdominal pain, constipation, diarrhea, flatulence, nausea / vomiting; infrequently - dry mouth; rarely - stomatitis, gastrointestinal candidiasis; very rarely - microscopic colitis.

On the part of the 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 diseases.

On the part of the genitals and mammary gland: very rarely - gynecomastia.

From the side of blood and lymphatic system: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis, pancytopenia.

Immune system disorders: rarely, hypersensitivity reactions (for example, fever, angioedema, anaphylactic reaction / anaphylactic shock).

On the part of the respiratory system, organs of the chest and mediastinum: rarely - bronchospasm.

On the part of the kidneys and urinary tract: very rarely - interstitial nephritis.

On the part of the organ of vision: rarely - blurred vision.

On the part of metabolism and nutrition: infrequently - peripheral edema; rarely, hyponatremia; very rarely - hypomagnesemia; hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia.

General disorders: rarely - indisposition, sweating.

Interaction

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 medium. Like other drugs that reduce the acidity of gastric juice, treatment with esomeprazole can lead to a decrease in the absorption of ketoconazole, itraconazole and erlotinib and increase the absorption of drugs such as digoxin. Joint administration of omeprazole in a dose of 20 mg 1 time per day and digoxin increases the bioavailability of digoxin by 10% (the bioavailability of digoxin increased by up to 30% in 2 out of 10 patients).

Omeprazole has been shown to interact with certain antiretroviral drugs. The mechanisms and clinical significance of these interactions are not always known. Increasing the pH value during omeprazole therapy may affect the absorption of antiretroviral drugs. Interaction at the level of an isoenzyme CYP2C19 is also possible. With the joint use of omeprazole and some antiretroviral drugs such as atazanavir and nelfinavir, a decrease in their concentration in serum is observed during therapy with omeprazole. Therefore, their simultaneous use is not recommended. The combined use of omeprazole (40 mg 1 time per day) 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 dose of atazanavir to 400 mg did not compensate for the effect of omeprazole on the bioavailability of atazanavir.

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

Esomeprazole inhibits CYP2C19 - the main isoenzyme involved in its metabolism. Accordingly, the combined use of esomeprazole with other drugs whose metabolism involves the CYP2C19 isoenzyme, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., can lead to an increase in plasma concentrations of these drugs, which in turn may require a dose reduction. . This interaction is especially important to remember when using the Nexium® preparation in the “as needed” mode.

With the joint intake of 30 mg of esomeprazole and diazepam, which is a substrate of the isoenzyme CYP2C19, a decrease in the clearance of diazepam is noted by 45%. The use 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 to monitor the concentration of phenytoin in plasma at the beginning of treatment with esomeprazole and with its cancellation.

The use of omeprazole in a dose of 40 mg 1 time per day led to an increase in the AUC and Cmax of voriconazole (substrate of the isoenzyme CYP2C19) by 15 and 41%, respectively.

Combined use of warfarin with 40 mg of esomeprazole does not cause a change in the coagulation time in patients who take 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. It is recommended to control INR at the beginning and at the end of the combined use of esomeprazole and warfarin or other coumarin derivatives.

According to the research results, pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose - 300 mg and maintenance dose - 75 mg / day) and esomeprazole (40 mg / day, orally) is noted, which reduces the exposure of the active metabolite of clopidogrel to an average of 40% and maximum inhibition of ADP-induced platelet aggregation by an average of 14%.

The clinical significance of this interaction is unclear. In a prospective study, patients receiving placebo or omeprazole at a dose of 20 mg / day concurrently with clopidogrel and acetylsalicylic acid (ASA) therapy, and when analyzing the clinical outcome of large-scale randomized trials, there was no increase in the risk of cardiovascular complications with co-use of clopidogrel and inhibitors proton pump, including esomeprazole.

The results of a number of observational studies are contradictory and do not give an unambiguous answer about the presence or absence of an increased risk of thromboembolic cardiovascular complications against the background of the combined use of clopidogrel and proton pump inhibitors.

When clopidogrel was used together with a fixed combination of 20 mg of esomeprazole and 81 mg of ASK, the active metabolite of clopidogrel decreased by almost 40% compared to clopidogrel monotherapy, and the maximum levels of inhibition of ADP-induced platelet aggregation were the same, which was probably due to simultaneous administration ASC in a low dose.

The use of omeprazole at a dose of 40 mg led to an increase in Cmax and AUC of Cilostazol by 18 and 26%, respectively; for one of the active metabolites of Cilostazol, the increase was 29 and 69%, respectively.

Joint administration of cisapride with 40 mg of esomeprazole leads to an increase in the values of pharmacokinetic parameters of cisapride in healthy volunteers: AUC - by 32% and T1 / 2 - by 31%, however, Cmax of cisapride in plasma does not significantly change. The slight lengthening of the QT interval, which was observed with cisapride monotherapy, did not increase with the addition of the drug Nexium® (see "Special Instructions").

With simultaneous use of esomeprazole and tacrolimus, an increase in serum tacrolimus concentration was noted.

Some patients noted an increase in the concentration of methotrexate on the background of joint 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.

The effect of drugs on the pharmacokinetics of esomeprazole. CYP2C19 and CYP3A4 isoenzymes are involved in the metabolism of esomeprazole. The combined use of esomeprazole with clarithromycin (500 mg 2 times a day), which inhibits the isoenzyme CYP3A4, leads to an increase in the AUC value of esomeprazole by 2 times.

The combined use of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19 isoenzymes, such as voriconazole, can lead to a more than 2-fold increase in the AUC value for esomeprazole. As a rule, in such cases, dose adjustment of esomeprazole is not required. Dose adjustment of esomeprazole may be required in patients with severely impaired liver function and with prolonged use.

Drugs that induce CYP2C19 and CYP3A4 isoenzymes, such as rifampicin and Hypericum perforatum drugs, when used together with esomeprazole can lead to a decrease in the concentration of esomeprazole in the blood plasma due to the acceleration of the metabolism of esomeprazole.

Dosage and administration

Inside The tablet should be swallowed whole with a liquid; tablets can not be chewed or crushed.

For patients with difficulty swallowing, tablets can be dissolved in half a glass of non-carbonated water. Do not use other liquids, because the protective shell of the microgranules may dissolve. When the tablet is dissolved, stir the water until the tablet disintegrates and drink the suspension of microgranules immediately or no later than within 30 minutes. Then fill the glass in half with water, stir the residue and drink. Do not chew or crush microgranules.

For patients who cannot swallow, tablets should be dissolved in non-carbonated water and administered through a nasogastric tube. It is important that the selected syringe and probe are suitable for this procedure. Instructions on the preparation and administration of the drug through a nasogastric tube are given in the subsection "Dosing the drug through a nasogastric tube".

Adults and children from 12 years

GERD

Treatment of erosive reflux esophagitis: 40 mg 1 time per day for 4 weeks. An additional 4-week course of treatment is recommended in cases where after the first course of healing of the esophagitis does not occur or symptoms persist.

Prolonged supportive treatment of patients after healing of erosive reflux esophagitis to prevent relapse: 20 mg 1 time per day.

Symptomatic treatment of GERD in patients without esophagitis: 20 mg 1 time per 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 mode of taking the drug "as needed", i.e. in the event of symptoms, take Nexium® 20 mg 1 time per day when symptoms resume. For patients taking NSAIDs and those at risk of developing stomach ulcers or duodenal ulcers, treatment is not recommended in the "as needed" mode.

Adults

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

Treatment of duodenal ulcers associated with Helicobacter pylori: Nexium® 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All drugs are taken 2 times a day for 1 week.

Prevention of recurrence of peptic ulcers associated with Helicobacter pylori: Nexium® 20 mg, amoxicillin 1 g and clarithromycin 500 mg. All drugs are taken 2 times a day for 1 week.

Prolonged acid suppression therapy in patients undergoing bleeding from peptic ulcers (after intravenous use of drugs that lower the secretion of the gastric glands) to prevent relapse

Nexium® 40 mg 1 time per day for 4 weeks after the end of IV therapy with drugs that lower the secretion of the gastric glands.

Patients for a long time taking NSAIDs

Healing of gastric ulcers associated with taking NSAIDs: Nexium® 20 or 40 mg 1 time per day. The duration of treatment is 4-8 weeks.

Prevention of gastric and duodenal ulcers associated with taking NSAIDs: Nexium® 20 or 40 mg 1 time per day.

Conditions associated with pathological hypersecretion of the gastric glands, incl. Zollinger-Ellison syndrome and idiopathic hypersecretion

The recommended initial dose is Nexium® 40 mg 2 times a day. In the future, the dose is selected individually, the duration of treatment is determined by the clinical picture of the disease. There is experience of using the drug in doses up to 120 mg 2 times a day.

Special patient groups

Renal failure: dose adjustment is not required. However, experience with Nexium® in patients with severe renal insufficiency is limited; In this regard, in the appointment of the drug in such patients should be careful (see "Pharmacokinetics").

Hepatic insufficiency: with mild and moderate hepatic insufficiency, dose adjustment is not required. For patients with severe hepatic impairment, the maximum daily dose should not exceed 20 mg.

Elderly patients: dose adjustment is not required.

Nasogastric tube administration

1. Place a pill in a syringe and fill it with 25 ml of water and approximately 5 ml of air. Some probes may require dilution of the drug in 50 ml of drinking water in order to prevent the pellets from clogging the probe with tablet pellets.

2. Immediately shake the syringe for about 2 minutes to dissolve the tablet.

3. Hold the syringe tip up and make sure that the tip is not clogged.

4. Insert the syringe tip into the probe, continuing to hold it upwards.

5. Shake the syringe and tip it upside down. Immediately inject 5–10 ml of the dissolved drug into the probe. After insertion, return the syringe to its previous position and shake (the syringe should be kept tip up to avoid clogging of the tip).

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

7. If a part of the drug in the form of sediment remains in the syringe, fill the syringe with 25 ml of water and 5 ml of air and repeat the operations described in paragraphs 5 and 6. For some probes, 50 ml of drinking water may be needed for this purpose.

Overdose

Symptoms: at the moment, extremely rare cases of deliberate overdose are described. Oral administration of esomeprazole at a dose of 280 mg was accompanied by general weakness and symptoms of the gastrointestinal tract. Single dose of 80 mg Nexium® did not cause any negative effects.

Treatment: symptomatic and general supportive therapy. Esomeprazole binds well to plasma proteins, so dialysis is ineffective. The antidote esomeprazole is unknown.

special instructions

If there are any alarming symptoms (such as significant spontaneous weight loss, recurrent 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, as treatment the drug Nexium® can lead to a smoothing of symptoms and delay the diagnosis.

In rare cases, atrophic gastritis was detected by histological examination of biopsy specimens of the gastric mucosa in patients who took omeprazole for a long time.

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

Patients taking Nexium® as needed should be instructed to contact their physician when symptoms change. Taking into account fluctuations in the concentration of esomeprazole in plasma in the appointment of therapy as necessary, you should consider the interaction of the drug with other drugs (see. "Interaction"). When prescribing Nexium® for 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 metabolized with CYP3A4 (for example, cisapride), it is necessary to take into account possible contraindications and interactions of clarithromycin with these drugs.

Nexium® tablets contain sucrose, so they are contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltase deficiency.

According to research results, pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg / day) and esomeprazole (40 mg / day, orally) is noted, which leads to a decrease in the active metabolite of clopidogrel by 40% and reduce 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 in other similar studies there has been no increase in risk.

In randomized double-blind controlled clinical trials of omeprazole and esomeprazole, including two open-label long-term therapy studies (over 12 years), the association of fractures with osteoporosis with the use of proton pump inhibitors has not been confirmed. Although the causal relationship between the use of omeprazole / esomeprazole and fractures against osteoporosis has not been established, patients at risk of developing osteoporosis or fractures against its background should be under appropriate clinical supervision.

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

Release form

Coated tablets, 20 mg and 40 mg. At 7 tab. in aluminum blisters. 1, 2 or 4 blisters are placed in a cardboard box with the control of the first opening.

Pharmacy sales terms

On prescription.

Storage conditions

At temperatures not higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiration date printed on the package.