Emanera enteric capsules 40mg №7×4

Name:
Emanera caps. intestinal sol. 40mg per blister. No. 7×4
Description:
Enteric capsules 20 mg: body and cap of the capsule are light pink in color. Enteric capsules 40 mg: the body and cap of the capsule are brownish-pink. The main active ingredient Esomeprazole Form of release Capsules Dosage 20 mg Special instructions Before taking the drug, tell your doctor if you have: severe liver disease, severe kidney disease, vitamin B12 deficiency, previously, after using a similar drug (which reduces the production of gastric acid), skin irritation was noted, you should perform a specific blood test (Chromogranin A). Pharmacological action Pharmacological action – antiulcer. Pharmacodynamics Esomeprazole is the S-isomer of omeprazole and inhibits the secretion of hydrochloric acid in the stomach through a specific and targeted mechanism of action. Specifically inhibits the proton pump of parietal cells. Both isomers of omeprazole, R- and S-, have similar pharmacodynamic activity. Mechanism of action Esomeprazole is a weak base, therefore it accumulates and becomes active in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, where it inhibits the activity of the H + / K + -ATPase enzyme. Suppresses both basal and stimulated secretion of hydrochloric acid. Influence on the secretion of acid in the stomach The effect develops already within 1 hour after ingestion of 20 mg or 40 mg of esomeprazole. With repeated administration of 20 mg of esomeprazole 1 time per day for 5 days, the average peak concentration of hydrochloric acid after stimulation with pentagastrin is reduced by 90% (on the 5th day of therapy, 6-7 hours after taking the drug). In symptomatic GERD patients, after daily administration of esomeprazole 20 or 40 mg for 5 days, gastric pH above 4 was maintained for an average of 13 and 17 hours, respectively. The proportion of patients taking esomeprazole at a dose of 20 mg / day, in which the pH level of gastric contents exceeded 4 for 8, 12 and 16 hours, respectively, was 76%, 54% and 24%, and for esomeprazole 40 mg / day – 97 %, 92% and 56%. The degree of suppression of acid secretion by esomeprazole is directly dependent on AUC. Therapeutic effect achieved as a result of suppression of acid secretion Healing of reflux esophagitis, when taking esomeprazole at a dose of 40 mg, occurs in approximately 78% of patients after 4 weeks and in 93% of patients after 8 weeks of therapy. Treatment with esomeprazole at a dose of 20 mg 2 times a day for 1 week in combination with appropriate antibiotics leads to successful eradication of Helicobacter pylori in 90% of patients. In uncomplicated peptic ulcer after eradication therapy (lasting from 7 to 10-14 days), continuation of monotherapy with antisecretory drugs is not required to heal the ulcer and eliminate symptoms. Other effects associated with the suppression of acid secretion During therapy with antisecretory drugs, the level of gastrin in the blood serum increases in response to a decrease in acid secretion. In some patients, after long-term therapy with esomeprazole, an increase in the number of enterochromaffin-like (ELC) cells has been noted, probably associated with an increase in the level of gastrin in the blood plasma. With prolonged use of antisecretory drugs, there was a slight increase in the frequency of formation of gastric glandular cysts. These changes are due to physiological changes as a result of long-term suppression of acid secretion. The cysts are benign and reversible. A decrease in the acidity of gastric contents while taking antisecretory agents is accompanied by an increase in the content of microbial flora in the stomach, which is normally present in the gastrointestinal tract. Therapy with proton pump inhibitors may lead to a slight increase in the risk of infectious diseases of the gastrointestinal tract, such as those caused by bacteria of the genus Salmonella and Campylobacter spp. Esomeprazole is more effective in healing gastric ulcers in patients who used non-steroidal anti-inflammatory drugs (NSAIDs), incl. selective COX-2 inhibitors compared with ranitidine. Esomeprazole was highly effective in preventing gastric and duodenal ulcers in patients taking NSAIDs (for patients over 60 years of age and / or with a history of peptic ulcer), incl. selective COX-2 inhibitors. Pharmacokinetics Absorption and distribution Esomeprazole is unstable in an acidic environment, therefore it is taken orally in the form of enteric capsules containing drug pellets, the shell of which is also resistant to the action of gastric juice. Under in vivo conditions, a small part of esomeprazole passes into the R-isomer. Esomeprazole is rapidly absorbed, reaching Cmax in plasma approximately 1-2 hours after ingestion. Absolute bioavailability is 64% after taking a single dose of 40 mg and increases to 89% against the background of daily administration 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 blood plasma proteins – 97%. Eating slows down and reduces the absorption of esomeprazole, which has no significant clinical significance. Metabolism and excretion Esomeprazole is completely metabolized with the participation of the cytochrome P450 isoenzyme system in the liver. Most of it is metabolized with the participation of the polymorphic CYP2C19 isoenzyme, which is responsible for the formation of hydroxy- and demethylated metabolites. The rest of esomeprazole is metabolized by the CYP3A4 isoenzyme responsible for the formation of esomeprazole sulfone, the main metabolite in plasma. The total plasma clearance after taking a single dose is approximately 17 and 9 l / h – after multiple doses. T1 / 2 is 1.3 hours with long-term administration of the drug 1 time per day. AUC increases with repeated administration. 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 sulfo-containing metabolite. With a single daily dose, esomeprazole is completely eliminated from the blood plasma between doses. Esomeprazole does not accumulate. The main metabolites of esomeprazole do not affect the secretion of hydrochloric acid in the stomach. Almost 80% of the oral dose of esomeprazole is excreted by the kidneys in the form of metabolites, and the rest through the intestines. Less than 1% of unchanged esomeprazole is found in the urine. Pharmacokinetics in certain 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 carried out mainly by the CYP3A4 isoenzyme. After repeated administration of esomeprazole at a dose of 40 mg 1 time per day, the average AUC value is approximately 2 times higher than in patients with reduced CYP2C19 activity. The average value of plasma Cmax increases by about 60%. In elderly patients (71–80 years), the metabolism of esomeprazole does not change significantly. After a single dose of 40 mg of esomeprazole, the mean AUC in women is approximately 30% higher than in men. Subsequently, with the 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 route of administration of the drug. The metabolism of esomeprazole may be impaired in people with mild or moderate hepatic impairment. The metabolic rate is reduced in severe liver dysfunction, which is accompanied by a two-fold increase in AUC. Therefore, the maximum daily dose of esomeprazole in these patients is 20 mg. The study in patients with reduced renal function has not been conducted. Since not esomeprazole itself is excreted through the kidneys, but its metabolites, the metabolism of esomeprazole in these patients does not change. 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 years and adults were the same. Emanera® Enteric Capsules are indicated for use in adults for the following indications: Gastroesophageal reflux disease (GERD) This is a condition in which acid backs up from the stomach into the esophagus (the tube that connects the throat to the stomach), causing inflammation, pain and heartburn . gastric or duodenal ulcer associated with Helicobacter pylori. If you have this disease, your doctor may prescribe this drug in combination with antibiotics and drugs to heal ulcers. gastric ulcers associated with the use of NSAIDs (non-steroidal anti-inflammatory drugs). if you are taking an NSAID, Emanera may be prescribed to prevent stomach ulcers. increased gastric acid levels due to enlargement of the pancreas (Zollinger-Ellison syndrome), prevention of recurrence as long-term therapy after intravenous treatment of peptic ulcer bleeding. Adolescents 12 years and older: Gastroesophageal reflux disease (GERD) This is a condition in which acid from the stomach backs up into the esophagus (the tube that connects the throat to the stomach), causing inflammation, pain, and heartburn. Gastric or duodenal ulcers associated with Helicobacter pylori. If you have this disease, your doctor may prescribe this drug in combination with antibiotics and drugs to heal ulcers. Dosage and administration Always take the drug in full accordance with the recommendations of your doctor. If in doubt, consult your doctor. If you are taking this drug for a long period of time, your doctor should monitor your condition (especially if taken for more than a year). It is necessary to tell the doctor about the change in any symptoms in the case of taking the drug “on demand”. How much to take the drug The doctor will prescribe the dose and method of application of the drug. It depends on the condition of the patient, his age and liver function. Recommended doses are listed below. Adults To treat heartburn caused by gastroesophageal reflux disease If your doctor finds that your food tube (esophagus) is slightly damaged, the recommended dose is 40 mg once a day for 4 weeks. Your doctor may advise you to take the same dose for another 4 weeks if your esophagus has not yet healed or symptoms persist. The recommended dose after healing of the esophagus is one Emaner® 20 mg enteric capsule per day. If your esophagus has not been damaged, the recommended dose is one Emaner® 20 mg enteric capsule daily. Once your symptoms are under control, your doctor may advise you to take your medicine as needed, up to a maximum of one Emaner® 20 mg enteric capsule per day. If you have severe liver problems, your doctor may prescribe lower doses for you. For the treatment and prevention of recurrence of ulcers caused by Helicobacter pylori The recommended dose is one Emaner® 20 mg enteric capsule twice daily for one week. Your doctor will also advise you to take antibiotics such as amoxicillin and clarithromycin. For the treatment of gastric ulcers associated with the use of NSAIDs (non-steroidal anti-inflammatory drugs) The recommended dose is one Emaner® 20 mg enteric capsule once a day for 4-8 weeks. To prevent the formation of gastric ulcers while taking NSAIDs (non-steroidal anti-inflammatory drugs) The recommended dose is one Emaner enteric capsule 20 mg once a day. For the treatment of increased stomach acid due to enlargement of the pancreas (Zollinger-Ellison syndrome) The recommended dose is one Emaner® 40 mg enteric capsule twice daily. Your doctor will adjust the dose and duration of the drug depending on your condition. The maximum dose is 80 mg twice a day For the prevention of recurrence as long-term therapy after intravenous treatment of peptic ulcer bleeding. The recommended dose is one Emaner® 40 mg enteric capsule for 4 weeks. Adolescents 12 years of age and older To treat heartburn caused by gastroesophageal reflux disease: If your doctor finds that your food tube (esophagus) is slightly damaged, the recommended dose is 40 mg once a day for 4 weeks. Your doctor may advise you to take the same dose for another 4 weeks if your esophagus has not yet healed or symptoms persist. The recommended dose once the esophagus has healed is one Emaner® 20 mg enteric capsule daily If your esophagus has not been damaged, the recommended dose is one Emaner® 20 mg enteric capsule daily. If you have severe liver problems, your doctor may prescribe lower doses for you. For the treatment and prevention of recurrence of ulcers caused by Helicobacter pylori The recommended dose is one Emaner® 20 mg enteric capsule twice daily for one week. Your doctor will also advise you to take antibiotics such as amoxicillin and clarithromycin. You can take the capsules at any time of the day. You may take the capsules with food or on an empty stomach. Capsules must be swallowed whole with water. Do not chew or crush them. This is due to the fact that the inside contains film-coated pellets that protect the drug from the effects of acid in the stomach. It is important not to damage the pellets. Use during pregnancy and lactation If you are pregnant, think you are pregnant, or plan to become pregnant, consult your doctor before using the drug. The doctor will decide whether it is possible to use Emanera® during this period. It is not known whether esomeprazole is excreted in breast milk. Consequently; use during breastfeeding is not recommended. Precautions If you develop a skin rash, especially in areas exposed to the sun, tell your doctor as soon as possible, as you may need to stop taking the medicine. Be sure to also report any other painful conditions, such as joint pain. Emanera® may mask the symptoms of other diseases. Therefore, if you experience any of these symptoms before or while taking the drug, tell your doctor immediately: you lose a lot of weight for no apparent reason, and you have trouble swallowing, you have stomach pain or indigestion , in the presence of vomiting, including with blood, when staining the stool black (feces stained with blood). If you are taking Emanera® “on demand”, but the symptoms of the disease persist or change, you should consult a doctor. When using a proton pump inhibitor, especially for more than one year, the risk of a fracture in the hip joint, wrist may be slightly increased tell your doctor if you have osteoporosis or if you are taking corticosteroids (which may increase your risk of osteoporosis). , including sold from pharmacies without a doctor’s prescription.This is due to the fact that Emanera® may affect the action of these drugs, or they may affect the effectiveness of Emanera®.Do not take Emanera® capsules together with medicines containing nelfinavir (to treat HIV) Tell your doctor if you are taking any of these medicines stv: atazanavir, digoxin, ketoconazole, itraconazole or voriconazole, erlotinib, citalopram, imipramine or clomipramine, diazepam, phenytoin. In this case, at the beginning and at the end of the use of the drug Emanera, you should be under the supervision of a physician. drugs to reduce blood viscosity, such as warfarin. In this case, at the beginning and at the end of the use of the drug Emanera, you should be under the supervision of a physician. cilostazol, cisapride methotrexate. If you are taking high doses of methotrexate, your doctor may recommend that you temporarily stop taking Emanera®. clopidogrel, tacrolimus, rifampicin, St. John’s wort (Hypericum perforatum). If your doctor has given you antibiotics, such as amoxicillin or clarithromycin, to treat an ulcer caused by Helicobacter pylori at the same time as Emanera®, it is especially important to let him know that you are taking any other medicines. Contraindications if you are allergic to esomeprazole or any of the other ingredients of this medicine (listed in section 6 of the package insert), if you have ever had an allergic reaction to other proton pump inhibitors (eg pantoprazole, lansoprazole, rabeprazole, omeprazole), if you are taking medicines containing nelfinavir (used to treat HIV). Do not take Emanera® if any of the above apply to you. If you are not sure, talk to your doctor before taking this medicine. Composition Active substance: esomeprazole. Each enteric capsule contains 20 mg esomeprazole or 40 mg esomeprazole (as esomeprazole magnesium dihydrate). List of excipients: sugar spheres (sucrose and corn starch), povidone KZO, sodium lauryl sulfate, polyvinyl alcohol, titanium dioxide (E171), macrogol 6000, macrogol 3000, talc (E553b), magnesium carbonate, polysorbate 80 (E433), methacrylic acid and ethyl acrylate copolymer (1: 1) dispersion 30% – in the composition of pellets and gelatin (E441), titanium dioxide (E171) and iron oxide red (E172) as part of the capsule shell. Emanera® contains sucrose. Overdose To date, cases of overdose of Emaner have not been described. Ingestion of esomeprazole at a dose of 280 mg was accompanied by general weakness and gastrointestinal symptoms. A single oral dose of 80 mg of esomeprazole was not accompanied by any symptoms. There is no specific antidote. Esomeprazole actively binds to plasma proteins, so hemodialysis is ineffective. Treatment: in case of overdose, symptomatic therapy should be carried out. Side effects Like all medicines, this medicine can cause side effects, although not everybody gets them. If you experience any of the following adverse reactions, you should stop taking the drug and contact your doctor immediately. Sudden wheezing (wheezing), swelling of the lips, tongue and throat or body, rash, fainting or difficulty swallowing (severe allergic reaction). Skin redness, blistering or peeling. There may be large blisters and bleeding from the lips, eyes, mouth, nose, and genitals (Stevens-Johnson syndrome or toxic epidermal necrolysis). Yellow skin, dark urine, and increased fatigue can be symptoms of liver disease. These reactions are rare and may affect up to 1 in 1,000 people. Other unwanted reactions are listed below. Common (? 1/100 to < 1/10) Headache Abdominal pain, constipation, diarrhea, flatulence Nausea or vomiting , tingling sensation, drowsiness Vertigo Dry mouth Changes in laboratory values reflecting liver function Skin rash, skin peeling and itching Fracture of the hip, wrist or spine (if the drug is used in high doses and for a long period of time) Rare (? 1/10,000 up to < 1/1,000) Leukopenia, thrombocytopenia Hyponatremia Agitation, confusion, depression Taste disorder Blurred vision Sudden decrease in breathing (bronchospasm) Inflammation of the oral mucosa Gastrointestinal candidiasis Liver disease, including jaundice, which may manifest as yellowing of the skin, dark urine , fatigue Hair loss (alopecia) Skin reactions in response to sun exposure Joint pain (arthralgia) and muscle pain (myalgia) General deterioration of well-being and decreased performance Increased sweating Very rare (< 1/10,000) Agranulocytosis, pancytopenia Aggression Hallucinations Severe liver disease leading to liver failure and encephalopathy Sudden onset of severe rash or peeling of the skin. Symptoms may be accompanied by fever and joint pain (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis). Muscle weakness Severe kidney disease Male breast enlargement Frequency unknown (cannot be estimated from the available data) If you take the drug for more than three months, the level of magnesium in the blood may decrease, which may manifest as fatigue, involuntary muscle contractions, confusion , convulsions, dizziness, increased heart rate. If you experience any of these symptoms, tell your doctor immediately. Low magnesium levels can also lead to low levels of potassium or calcium in the blood. Your doctor may decide to have regular blood tests to check your magnesium levels. Inflammation of the intestines (leading to diarrhea). Rash, possibly accompanied by joint pain. Emanera can, in very rare cases, affect white blood cells, leading to immune deficiency. If you have an infection that is accompanied by a fever with a sharp deterioration in the general condition or a fever with symptoms of local infection, such as pain in the neck, throat, mouth, difficulty urinating, you should consult a doctor as soon as possible and get tested to rule out agranulocytosis. It is important to report all medications you take. Reporting adverse reactions If you experience any adverse reactions, please tell your doctor or pharmacist. This recommendation applies to any possible adverse reactions, including those not listed in this package insert. By reporting adverse reactions, you help to get more information about the safety of the drug. Storage conditionsKeep out of the reach of children. Do not use the drug after the expiry date which is stated on the package. The expiry date is the last day of the month. Store at a temperature not exceeding 30 °C. Store in original packaging to protect from moisture. Do not dispose of the drug in the water supply or sewerage. Ask your pharmacist how to dispose of drugs you no longer need. These measures will help protect the environment. Buy Emaner enteric capsules 40mg №7x4