Emanera capsules 20 mg 14 pcs
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Active ingredients
Esomeprazole
Release form
Capsules
Composition
1 capsule contains: esomeprazole magnesium 20.645 mg, which corresponds to the content of esomeprazole 20 mg. Substances: sugar pellets - 35.58 mg, povidone K30 - 7.5 mg, sodium lauryl sulfate - 0.9 mg. Composition of pellets: opadry II white 85F28751 (polyvinyl alcohol - 3.3 mg, titanium dioxide (E171) - 5.86 mg, macrogol 3000 - 4.735 mg, talc - 3.469 mg) - 23.44 mg, magnesium hydroxycarbonate (heavy magnesium carbonate) - 3 mg, methacrylic acid-ethyl acrylate copolymer (1: 1) dispersion 30% - 127.49 mg, talc - 11.925 mg, macrogol 6000 - 3.825 mg, titanium dioxide (E171) - 3.825 mg, polysorbate 80 - 1.72 mg. Gel oic capsule - 48 mg.Sostav empty capsules: body - iron oxide red dye (E172) - 0.014 mg of titanium dioxide (E171) - 0.406 mg, gelatin - 28.38 mg; the cap - iron dye red oxide (E172) - 0.01 mg, titanium dioxide (E171) - 0.271 mg, gelatin - 18.92 mg.
Pharmacological effect
Pharmacological action - anti-ulcer.
Pharmacokinetics
Absorption and distributionEzomeprazole is unstable in an acidic environment, therefore, is taken orally in the form of enteric capsules containing the pellets of the drug, the shell of which is also resistant to the action of gastric juice. In vivo, a small portion of the esomeprazole is converted to the R isomer. Esomeprazole is rapidly absorbed, reaching Cmax in the blood plasma approximately 1–2 hours after ingestion. Absolute bioavailability is 64% after a single dose of 40 mg and increases to 89% on the background of daily intake of esomeprazole 1 time per day. Bioavailability for esomeprazole at a dose of 20 mg is 50 and 68%, respectively. Vss in healthy volunteers is approximately 0.22 l / kg. Communication with plasma proteins - 97%. Food intake slows down and reduces the absorption of esomeprazole, which has no significant clinical significance. Metabolism and elimination Esomeprazole is completely metabolized with the participation of cytochrome P450 isoenzymes in the liver. Most of the metabolized with the participation of the polymorphic isoenzyme CYP2C19, which is responsible for the formation of hydroxy - and demethylated metabolites. The rest of esomeprazole is metabolized by CYP3A4 isoenzyme, which is responsible for the formation of esomeprazole sulfone, the main metabolite in the blood plasma. The total plasma clearance after a single dose is approximately 17 and 9 l / h after multiple administration. T1 / 2 is 1.3 hours with long-term use of the drug 1 time per day. AUC increases with repeated use.The dose-dependent increase in AUC with repeated use is non-linear due to a decrease in metabolism during the first passage through the liver, a decrease in clearance, probably caused by inhibition of the CYP2C19 isoenzyme by esomeprazole and / or its sulfa-containing metabolite. With a single daily intake, esomeprazole is completely removed from the blood plasma during the interval between doses. Esomeprazole does not accumulate. The major metabolites of esomeprazole do not affect the secretion of hydrochloric acid in the stomach. Almost 80% of the orally administered esomeprazole dose is excreted by the kidneys as metabolites, and the rest through the intestines. Less than 1% of unchanged esomeprazole is detected in the urine. Pharmacokinetics in certain groups of patients. In approximately 2.9 ± 1.5% of the population, the activity of CYP2C19 isoenzyme has been reduced. In these patients, the metabolism of esomeprazole is carried out mainly by CYP3A4 isoenzyme. After repeated administration of esomeprazole at a dose of 40 mg 1 time per day, the average AUC value is about 2 times higher than in patients with reduced CYP2C19 activity. The mean plasma Cmax value increases by approximately 60%. In elderly patients (71–80 years old), the metabolism of esomeprazole does not change significantly. After a single dose of 40 mg of esomeprazole, the average AUC value is approximately 30% higher in women than in men. Subsequently, with systematic daily intake of esomeprazole 1 time per day, no differences in pharmacokinetics were observed in patients of both sexes. These features do not affect the dose and method of use of the drug. Esomeprazole metabolism may be impaired in people with mild or moderate liver dysfunction. The metabolic rate is reduced in severe impaired liver function, which is accompanied by a twofold increase in AUC. Therefore, the maximum daily dose of esomeprazole in these patients is 20 mg. The study in patients with reduced kidney function was not conducted. Since not the esomeprazole itself but its metabolites are eliminated through the kidneys, the metabolism of esomeprazole does not change in these patients. After repeated administration of 20 and 40 mg of esomeprazole, the levels of AUC and the time to reach Cmax in children aged 12-18 and adults were the same.
Indications
Gastroesophageal Reflux Disease (GERD): treatment of erosive reflux esophagitis; long-term supportive treatment afterhealing of erosive reflux esophagitis with the aim of preventing recurrence; symptomatic treatment of GERD.yc. cyns; pylori.Patients who have been taking non-steroidal anti-inflammatory drugs (NSAIDs) for a long time: healing of a stomach ulcer associated with taking NSAIDs; prevention of ulcers and duodenal ulcer associated with taking NSAIDs in patients at risk. Durable prevention of recurrence of recurrent bleeding from peptic ulcers (after intravenous administration of drugs that lower the secretion of gastric glands); Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion , including idiopathic hypersecretion.
Contraindications
Hypersensitivity to esomeprazole, substituted benzimidazoles or other components of the drug, children under 12 years old (no data on efficacy and safety) and children over 12 years of age for other indications except gastroesophageal reflux disease (GERD), simultaneous intake with atazanavir and nelfinavir
Use during pregnancy and lactation
Use of the drug Emaner during pregnancy is possible only if the expected benefit to the mother exceeds the possible risk to the fetus, insufficient data on the use of esomeprazole in pregnant women. In epidemiological studies during the use of the racemic mixture of omeprazole, no fetotoxic effects or fetal developmental disorders were detected. In studies with esomeprazole in animals, no direct or indirect negative effect on the development of the embryo or fetus was detected; there was also no direct or indirect negative effect on the course of pregnancy, childbirth and the postnatal period of the newborn. It is currently unknown whether esomeprazole is excreted in breast milk, therefore Emanera should not be used during breastfeeding.
Dosage and administration
Inside, without chewing, washing down with a small amount of liquid.For patients with difficulty swallowing, pour the contents of the capsules into half a glass of non-carbonated water, stir and drink immediately or within 30 minutes. Then re-fill the glass with water by half, rinse the walls of the glass and drink. Do not mix the drug with other liquids, because This may lead to the dissolution of the pellet containment shell. Pellets should not be chewed or crushed. For patients who cannot swallow, the contents of the capsules should be dissolved in non-carbonated water and injected esomeprazole through a nasogastric tube. It is necessary to check the compliance of the syringe for the injection and the probe. Instructions on the preparation and administration of the drug through a nasogastric tube are given in the subsection “Nasogastric tube administration”. Adults and teenagers over 12 years old Gastroesophageal reflux disease (GERD): Erosive reflux esophagitis (treatment): 40 mg 1 time per day for 4 hours weeks. If, after the first course of therapy, the healing of esophagitis does not occur or symptoms persist, an additional 4-week course of treatment with esomeprazole is recommended. Long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse: 20 mg 1 time per day. Symptomatic treatment of GERD: 20 mg 1 once a day - to patients without esophagitis. If, after 4 weeks of treatment, it was not possible to control the symptoms, it is necessary to re-examine the patient. After the symptoms are eliminated, you can continue taking Emaner “on demand”, i.e. take 20 mg of the drug 1 time per day if symptoms occur. Patients taking NSAIDs that are at risk of developing stomach ulcers or duodenal ulcers are not recommended for on-demand treatment. Adults Helicobacter pylori associated with and prevention of recurrence of peptic ulcers associated with Helicobacter pylori: the combined eradication therapy of Helicobacter pylori includes: Emanera 20 mg, and Moxicillin 1 g and clarithromycin 500 mg. All drugs are taken 2 times a day for 7-14 days. Patientslong-term nonsteroidal anti-inflammatory drugs (NSAIDs): Healing of gastric ulcers associated with taking NSAIDs: 20 mg or 40 mg 1 time per day for 4-8 weeks. Prevention of gastric and duodenal ulcers associated with taking NSAIDs in patients related to risk group: drug Emanera 20 mg or 40 mg 1 per day. Long-term prophylaxis of recurrence of repeated bleeding from peptic ulcers (after intravenous administration of drugs that lower the secretion of gastric glands): Emanera 40 mg 1 time per day 4 weeks after the start of intravenous prevention of recurrent bleeding. Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion: the initial dose of Emaner 40 mg 2 times a day. The dose of the drug and the duration of treatment are selected individually depending on the clinical picture of the disease. The disease in most patients is controlled by taking the drug in a dose of 80 mg to 160 mg per day. If necessary, the use of the drug Emanera over 80 mg per day, the daily dose is divided into two doses. Violation of the kidney function Patients with impaired renal function do not need to change the dose. Experience with the use of esomeprazole in patients with severe renal insufficiency is limited; therefore, caution should be exercised in prescribing such patients. Liver dysfunction Patients with mild or moderate hepatic impairment do not need to change the dose. In severe hepatic insufficiency, the maximum daily dose should not exceed 20 mg. Elderly Patients Elderly patients do not need dose adjustment. Administration of the drug through a nasogastric tube When prescribing the drug through a nasogastric tube: Open the capsule and empty the contents of the capsule into a special syringe. Add 25 ml of drinking water and about 5 ml of air to the syringe. For some probes, it may be necessary to dilute the drug in 50 ml of drinking water in order to prevent pellets contained in the capsule from clogging the probe. After adding water, immediately shake the syringe to obtain a suspension. Make sure that the tip is not clogged (pressing the plunger a little while holding the syringe in the position of the tip up). Insert the tip of the syringe into the probe, continuing to keep it pointing up. Shake the syringe and turn it upside down. Immediately enter 5-10 ml of the dissolved drug into the probe.After inserting the solution, return the syringe to its previous position and shake (the syringe should be kept tip up to avoid clogging the tip). Again, lower the syringe tip down and add another 5-10 ml of solution to the probe. Repeat the procedure until the syringe is empty. If any 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 procedures described in paragraphs 5 and 6. For some probes, 50 ml may be necessary for this purpose. drinking water.
Side effects
Classification of the incidence of side effects of the World Health Organization (WHO): very often ≥1 / 10, often from ≥ 1/100 to <1/10, rarely from ≥1 / 1000 to <1/100 rarely from ≥1 / 10000 to <1/1000 very rarely, from <1/10000, the frequency unknown cannot be estimated based on the available data. In each group, unwanted effects are presented in order of decreasing severity. For the nervous system: often: headache; infrequently: insomnia, dizziness, paresthesias, drowsiness; rarely: depression, agitation, confusion; very rarely: hallucinations, aggressive behavior. On the part of the respiratory system: rarely: bronchospasm; On the part of the digestive system: often: abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting; infrequently: dryness of the oral mucosa, increased activity of “liver” enzymes; rarely: stomatitis, gastrointestinal candidiasis, hepatitis (with or without jaundice); very rare: liver failure, hepatic encephalopathy in patients with a history of liver disease; From the urinary system: very rare: interstitial nephritis; From the reproductive system: very rare: gynecomastia; From the musculoskeletal system: rarely: arthralgia, myalgia; very seldom: muscular weakness; From the skin: infrequently: dermatitis, skin rash, pruritus, urticaria; rarely: alopecia, photosensitivity; very rare: erythema multiforme, Stephen-Johnson syndrome, toxic epidermal necrolysis; On the part of the blood-forming organs: rarely: leukopenia, thrombocytopenia; very rarely: agranulocytosis, pancytopenia; From the sense organs: infrequently: blurred vision; rarely: change in taste; Allergic reactions: rarely: hypersensitivity reactions (for example, fever, angioedema, anaphylactic reaction / anaphylactic shock); Laboratory data: rarely: hyponatremia. Others: infrequently: peripheral edema; rarely: sweating; very rarely: weakness (malaise).
Interaction with other drugs
Effect of esomeprazole on the pharmacokinetics of other drugs Drugs, the absorption of which depends on the pH level. Reduced secretion of hydrochloric acid in the stomach during treatment with esomeprazole and other proton pump inhibitors may lead to changes in the absorption of drugs, the absorption of which depends on the acidity of the medium. Like antacids and other drugs that reduce the acidity of gastric juice, the use of esomeprazole may reduce the absorption of ketoconazole, itraconazole and erlotinib, and increase the absorption of drugs such as digoxin. Simultaneous administration of omeprazole at a dose of 20 mg once a day and digoxin increases bioavailability digoxin. 10% (digoxin bioavailability increased by up to 30% in 2 out of 10 patients). It is known that omeprazole interacts with some antiretroviral drugs. The mechanism and clinical significance of these interactions are not always known. Reducing the acidity of gastric juice during therapy with omeprazole may affect the absorption of antiretroviral drugs. Interaction at the level of an isoenzyme CYP2C19 is also possible. During therapy with omeprazole, a decrease in the serum concentration of certain antiretroviral drugs (atazanavir and nelfinavir) has been observed. Therefore, simultaneous use is not recommended. The simultaneous use of omeprazole (40 mg once daily) with atazanavir 300 mg / ritonavir 100 mg in healthy volunteers is accompanied by a marked decrease in the exposure to atazanavir (AUC, Cmax and Cmin in plasma decreased by about 75%). An increase in the dose of atazanavir to 400 mg did not compensate for the effects of omeprazole on the bioavailability of atazanavir. not recommended. CYP2C19 metabolized drugs. Esomeprazole inhibits CYP2C19, the main isoenzyme of the metabolism of esomeprazole. Thus, with simultaneous use of esomeprazole with drugs whose metabolism involves the CYP2C19 isoenzyme, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., the plasma concentration of these drugs may increase and, accordingly, their dose reduction may be required .It is especially necessary to take into account when prescribing the drug Emaner in the mode of necessity.So, with simultaneous use with 30 mg of esomeprazole, diazepam clearance (CYP2C19 isoenzyme substrate) is reduced by 45%. Simultaneous use of esomeprazole at a dose of 40 mg leads to an increase in plasma phenytoin concentration in epilepsy by 13%. It is recommended to monitor plasma phenytoin concentrations in plasma. of blood at the beginning of therapy with esomeprazole and when it is canceled. When using omeprazole at a dose of 40 mg, the Cmax and AUC of voriconazole (CYP2C19 isoenzyme substrate) increases by 15 and 41%, respectively. The coagulation time is simultaneous Receiving warfarin and esomeprazole 40mg remains within acceptable limits. However, several cases of a clinically significant increase in the INR index have been reported. It is recommended to control INR at the beginning and at the end of simultaneous use of esomeprazole and warfarin or other coumarin derivatives. The use of omeprazole at a dose of 40 mg resulted in 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. Simultaneous use of esomeprazole in a dose of 40 mg with cisapride leads to an increase in the values of pharmacokinetic parameters of cisapride in healthy volunteers: AUC - by 32% and T1 / 2 - by 31%, but Cmax it does not change significantly. A slight lengthening of the QT interval on the ECG, which is observed with cisapride monotherapy, did not increase with the addition of esomeprazole. Some patients noted an increase in serum methotrexate concentration against the background of simultaneous use with proton pump inhibitors. When using high doses of methotrexate, the possibility of temporary withdrawal of esomeprazole should be considered. Esomeprazole does not cause clinically significant changes in the pharmacokinetics of amoxicillin and quinidine. Simultaneous short-term use of esomeprazole and naproxen or rofecoxib did not reveal any clinically significant pharmacokinetic interaction. loading dose, then - 75 mg / day) with omeprazole (80 mg) at one time, at the same time during 5 days. The activity of the thiol metabolite (active metabolite) of clopidogrel was reduced by 46% (1st day of therapy) and 42% (5th day of therapy), while taking clopidogrel and omeprazole at the same time.When taking clopidogrel and omeprazole at one time, the average suppression of platelet aggregation (IPA) was reduced by 47% (during 24 hours of therapy) and 30% (5th day of therapy). According to another study: omeprazole when used with clopidogrel at the same time , at different times, has no inhibitory effect on the CYP2C19 isoenzyme. In the studies, conflicting data on clinical manifestations of interaction with clopidogrel on major cardiovascular events were recorded. With simultaneous use with tacrolimus, serum concentrations of tacrolimus may increase. The effect of drugs on the pharmacokinetics of esomeprazole CYP2C19 and CYP3 isoenzymes take part in the metabolism of esomeprazole. With simultaneous use of esomeprazole with clarithromycin (500 mg 2 times a day) (CYP3A4 isoenzyme inhibitor), the AUC value of esomeprazole increases by a factor of 2. Simultaneous use of esomeprazole and the combined inhibitor of isoenzymes CYP2C19 and CYP3A4, such as voriconazole, can be applied with an Io-enzyme and a combined inhibitor of isoenzymes CYP2C19 and CYP3A4; times. Usually in such situations, no change in the dose of esomeprazole is required. In patients with severe impairment of liver function or if necessary long-term therapy should be considered for dose reduction ezomeprazola.Lekarstvennye drugs inducing isozymes CYP2C19 and CYP3A4, such as rifampicin and preparations Hypericum perforatum, while the use of esomeprazole can lead to a reduction in the plasma concentration of esomeprazole blood by accelerating the metabolism of esomeprazole.
special instructions
If anxious symptoms appear (such as significant spontaneous weight loss, repeated vomiting, dysphagia, vomiting with blood or melena), as well as suspected or detected gastric ulcers, it is necessary to exclude a malignant neoplasm, because the use of Emanera can reduce the severity of symptoms and delay diagnosis. Patients who have been taking Emanera for a long time (especially for more than a year) must be under regular medical supervision. Patients who take the drug according to Rebirth should be informed of the need to go to the doctor when the nature of the symptoms changes. Considering fluctuations in the concentration of esomeprazole in the blood plasma when using the drug on an as-needed basis, interactions with other drugs should be considered (see"Interaction"). When using esomeprazole to eradicate Helicobacter pylori, consideration should be given to the possible interaction between the components of triple therapy. Clarithromycin is a potent inhibitor of CYP3A4, therefore, contraindications and drug interaction of clarithromycin should be considered when prescribing triple therapy to patients who are simultaneously taking drugs metabolized by CYP3A4, such as cisapride. malabsorption or deficiency of sucrase-isomaltase. The effect on the ability to drive and others is difficult mi mechanisms. The drug Emanera does not affect the control of vehicles and work with other technical devices, requiring increased concentration of attention and speed of psychomotor reactions.