Emanera caps 20mg #28

Instruction for Emanera

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Emanera is a drug with antiulcer action.

Release form and composition

Dosage form of release Emanera - enteric capsules: capsule contents - from white to almost white pellets; 20 mg each - light pink, size No. 3; 40 mg each - from pink to pink with a slightly grayish tinge, size No. 1 (7 pcs. in blisters, in a cardboard box 1, 2 or 4 blisters).
Composition of 1 capsule Emanera:
    active ingredient: esomeprazole - 20/40 mg (esomeprazole magnesium - 20.645 or 41.29 mg);
    additional components (pellet core) (20/40 mg): sugar crumbs (sucrose and starch syrup) - 35.58 / 71.16 mg; sodium lauryl sulfate - 0.9 / 1.8 mg; povidone K30 - 7.5 / 15 mg;
    pellet shell (20/40 mg): Opadry II white 85F28751 [polyvinyl alcohol - 9.376 / 18.752 mg; titanium dioxide (E 171) - 5.86 / 11.72 mg; macrogol 3000 - 4.735 / 9.47 mg; talc - 3.469 / 6.938 mg] - 23.44 / 46.88 mg; magnesium hydroxycarbonate (heavy magnesium carbonate) - 3/6 mg; 30% dispersion of a copolymer (1: 1) of ethyl acrylate and methacrylic acid - 127.49 / 254.98 mg; macrogol 6000 - 3.825 / 7.65 mg; talc - 11.925 / 23.85 mg; polysorbate 80 - 1.72 / 3.44 mg; titanium dioxide (E 171) - 3.825 / 7.65 mg;
    capsule body (20/40 mg): titanium dioxide (E 171) - 0.406 / 0.458 mg; dye red iron oxide (E 172) - 0.014 / 0.114 mg; gelatin - 28.38 / 45.028 mg;
    capsule cap (20/40 mg): titanium dioxide (E 171) - 0.271 / 0.305 mg; dye red iron oxide (E 172) - 0.01 / 0.076 mg; gelatin - 18.92 / 30.019 mg.

Pharmacodynamics

Esomeprazole is the S-isomer of omeprazole, which suppresses the secretion of hydrochloric acid in the stomach due to a specific and targeted mechanism of action.
Specifically inhibits the proton pump of parietal cells. The S- and R-isomers of the substance have similar pharmacodynamic activity.
Esomeprazole is a weak base. In a very acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, the substance accumulates, passing into the active form, and inhibits the activity of the H + / K + -ATPase enzyme. Thanks to the action of the substance, both basal and stimulated secretion of hydrochloric acid is suppressed.
The effect of taking esomeprazole develops within 1 hour. When you take a dose of Emanera 20 mg once a day for 5 days, the average peak concentration of hydrochloric acid after stimulation with pentagastrin decreases by 90% (on the 5th day of use - after 6-7 hours after taking the drug).
After daily intake of 20 or 40 mg of esomeprazole for 5 days in patients with GERD (gastroesophageal reflux disease) and in the presence of clinical symptoms, the pH of the stomach contents above 4 remained, as a rule, for 13 and 17 hours, respectively. The proportion of patients taking esomeprazole 20 mg per day, whose gastric pH was above 4 for 8, 12 and 16 hours, was 76, 54 and 24%, respectively, in a daily dose of 40 mg - 97, 92 and 56 %.
The severity of the therapeutic effect is in direct proportion to the AUC (area under the concentration-time curve).
As a result of taking Emanera, the following effect is observed:
    healing of reflux esophagitis (daily dose 40 mg): in 78% of cases after 4 weeks, in 93% - after 8 weeks;
    eradication of Helicobacter pylori (daily dose 40 mg in combination with antibiotic therapy): in 90% of cases after 7 days;
    uncomplicated peptic ulcer disease after eradication therapy (course duration - 7-14 days): continuation of monotherapy with Emanera to eliminate symptoms and ulcer healing is not required.
With the use of the drug, the serum gastrin level in the blood increases.
After prolonged therapy with esomeprazole, some patients have an increase in the number of enterochromaffin-like cells, which may be associated with an increase in the plasma level of gastrin in the blood.
With a long course, there is a slight increase in the frequency of formation of gastric glandular cysts. Such changes are associated with physiological changes due to the suppression of acid secretion over a long period. Cysts are benign and reversible.
A decrease in the acidity of gastric contents is accompanied by an increase in the content of microbial flora in the stomach, which is normally present in the gastrointestinal tract. The use of Emanera may cause a slight increase in the risk of infectious diseases of the gastrointestinal tract, in particular, caused by bacteria of the genus Salmonella and Campylobacter spp.
The substance is more effective in the healing of stomach ulcers in patients who used NSAIDs (non-steroidal anti-inflammatory drugs), including selective inhibitors of COX-2 (cyclooxygenase), compared with ranitidine.
High efficacy of esomeprazole in the prevention of gastric and duodenal ulcers during NSAID therapy [for patients over 60 years of age and (or) with a history of peptic ulcer], including selective COX-2 inhibitors, is noted.

Pharmacokinetics

Esomeprazole is unstable in an acidic environment, therefore it is taken orally in the form of enteric capsules containing pellets, the shell of which is also resistant to gastric juice. An insignificant part of esomeprazole passes into the R-isomer.
Esomeprazole is rapidly absorbed, Cmax (maximum concentration of the substance) is reached in the blood plasma approximately 1-2 hours after oral administration. After a single dose of 40 mg, the absolute bioavailability is 64%, with daily intake of esomeprazole 1 time per day, it increases to 89%. Bioavailability for 20 mg of esomeprazole is 50 and 68%, respectively. In healthy volunteers, Vss is about 0.22 l / kg. The connection with blood plasma proteins is 97%.
Food intake reduces and slows down the absorption of esomeprazole, which has no significant clinical significance.
Esomeprazole is completely metabolized in the liver with the participation of the cytochrome P450 isoenzyme system (most of it is the polymorphic isoenzyme CYP2C19, which is responsible for the formation of demethyl and hydroxyl metabolites; the rest is the isoenzyme CYP3A4, which is responsible for the formation of the main metabolite in the blood plasma - esomeprazole sulfone).
After a single / multiple dose, the total plasma clearance is approximately 17 and 9 l / h, respectively. T1 / 2 (half-life) with long-term administration once a day - 1.3 hours. With repeated administration, AUC increases (dose-dependent increase is non-linear due to a decrease in metabolism during the first passage through the liver). With a single daily dose of esomeprazole in the intervals between doses, it is completely removed from the blood plasma.
The substance does not cumulate. Its main metabolites do not affect the secretion of hydrochloric acid in the stomach. Most (about 80%) of the substance is excreted by the kidneys in the form of metabolites, the way of excretion of the rest is the intestine. Unchanged esomeprazole is found in urine less than 1%.
The metabolism of esomeprazole with a reduced activity of the isoenzyme CYP2C19 is carried out mainly by the isoenzyme CYP3A4. After repeated intake of 40 mg of the substance once a day, the average AUC is approximately 2 times higher than in patients with reduced CYP2C19 activity. In this case, the average value of plasma Cmax increases by approximately 60%.
Esomeprazole metabolism in elderly patients (71–80 years old) does not change significantly.
In mild / moderate impairment of hepatic function, the metabolism of esomeprazole may be impaired; in severe impairment, a decrease in metabolic rate is observed, which is accompanied by a 2-fold increase in AUC. In this regard, the maximum daily dose for this group of patients is 20 mg.

Indications for use

    GERD: therapy for erosive reflux esophagitis; symptomatic treatment of GERD; long-term maintenance therapy after healing of erosive reflux esophagitis to prevent relapse;
    eradication of Helicobacter pylori (simultaneously with antibiotic therapy): duodenal ulcer associated with Helicobacter pylori; prevention of recurrence of peptic ulcer associated with Helicobacter pylori;
    peptic ulcer of the stomach and duodenum;
    long-term use of NSAIDs: healing of stomach ulcers, which is associated with ongoing therapy; prevention of stomach and duodenal ulcers, which is associated with the use of NSAIDs, in patients at risk;
    Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion;
    long-term prevention of recurrence of repeated bleeding from peptic ulcers (after intravenous administration of drugs that reduce the secretion of gastric glands).

Contraindications

Absolute:
    hereditary fructose intolerance, sucrase-isomaltase deficiency or glucose-galactose malabsorption syndrome;
    combined use with nelfinavir and atazanavir;
    age up to 12/18 years (all indications / all indications, except for GERD);
    lactation period;
    the presence of individual intolerance to the components of the drug.
Relative (Emanera is appointed under medical supervision):
    severe renal failure;
    pregnancy.

Instructions for use Emanera: method and dosage

Emanera is taken orally with a small volume of liquid without chewing.
If you have difficulty swallowing, the contents of the capsules can be poured into 1/2 glass of still water. The resulting solution should be stirred and drunk immediately or drunk for 30 minutes. Then you need to refill the glass with the same volume of water, rinse the glass walls and drink.
Emanera should not be mixed with other liquids, as this can lead to a violation of the protective shell of the pellets. Do not chew / crush the pellets.
For patients who cannot swallow on their own, the contents of the capsules are dissolved in still water and administered through a nasogastric tube.
The recommended dosage regimen for the treatment of GERD in adults and children over 12 years old:
    erosive reflux esophagitis (therapy): 1 time per day, 40 mg for 4 weeks. If symptoms persist, an additional course of 4 weeks may be prescribed;
    maintenance therapy after healing of erosive reflux esophagitis (in order to prevent relapse): 1 time per day, 20 mg for a long time;
    symptomatic treatment of GERD: for patients without esophagitis - 1 time per day, 20 mg of Emanera for 4 weeks. If symptoms persist, re-examination is required. After the symptoms disappear, therapy can be continued on demand, that is, if symptoms occur, Emanera is taken 1 time per day, 20 mg. Treatment in this regimen is not recommended for patients taking NSAIDs who are at risk of developing gastric or duodenal ulcers.
Scheme of using Emanera by adult patients for other indications:
    duodenal ulcer associated with Helicobacter pylori, prevention of recurrence of peptic ulcers associated with Helicobacter pylori (as part of the combined eradication treatment of Helicobacter pylori): Emanera - 20 mg; clarithromycin - 500 mg, amoxicillin - 1000 mg. All drugs are taken 2 times a day for a course of 7 to 14 days;
    a stomach ulcer associated with the intake of NSAIDs (for the purpose of healing): 1 time a day, 20 or 40 mg for 4–8 weeks;
    prevention of gastric and duodenal ulcers associated with taking NSAIDs in high-risk patients: 1 time per day, 20 or 40 mg;
    Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion: the initial dose is 40 mg 2 times a day. The dosage regimen is determined by the clinical picture of the disease. In most cases, the therapeutic effect is observed when the drug is taken in a daily dose of 80–160 mg. If a dose of more than 80 mg per day is prescribed, it should be divided into 2 doses;
    long-term prevention of recurrence of recurrent bleeding from peptic ulcers (after intravenous administration of drugs that reduce the secretion of gastric glands): once a day, 40 mg for 4 weeks after the started intravenous prevention of recurrent bleeding.
The maximum daily dose for severe liver failure is 20 mg.
When prescribing Emanera through a nasogastric tube, you need to open the capsule and pour its contents into a special syringe. Add 25 ml of drinking water and approximately 5 ml of air to the syringe. In some cases, to prevent the probe from clogging up with pellets, it may be necessary to dilute the drug in 50 ml of drinking water.
After adding water, the syringe must be shaken immediately to obtain a suspension.
After making sure that the tip is not clogged, it is inserted into the probe, keeping it pointing up. Then the syringe should be shaken and turned over with the tip down. 5-10 ml of the dissolved drug is immediately injected into the probe, after which the syringe must be returned to its original position and shaken.
Then the syringe is again lowered with the tip down and another 5-10 ml of solution is injected into the probe. The procedure is repeated until the entire volume has been injected.
If a sediment remains in the syringe, it is filled with 25 or 50 ml of water and 5 ml of air and the procedure is repeated.

Side effects

Possible adverse reactions (> 10% - very often;> 1% and <10% - often;> 0.1% and <1% - infrequently;> 0.01% and <0.1% - rarely; <0, 01% - very rare):
    respiratory system: rarely - bronchospasm;
    nervous system: often - headache; infrequently - dizziness, insomnia, drowsiness, paresthesia; rarely - agitation, depression, confusion; very rarely - aggressive behavior, hallucinations;
    urinary system: very rarely - interstitial nephritis;
    digestive system: often - vomiting, diarrhea, abdominal pain, flatulence, constipation, nausea; infrequently - increased activity of liver enzymes, dryness of the oral mucosa; rarely - stomatitis, candidiasis of the gastrointestinal tract, hepatitis with and without jaundice; very rarely - hepatic failure, hepatic encephalopathy (with a burdened history of liver disease);
    musculoskeletal system: rarely - myalgia, arthralgia; very rarely - muscle weakness;
    reproductive system: very rarely - gynecomastia;
    sense organs: infrequently - blurred vision; rarely - a change in taste;
    hematopoietic organs: rarely - thrombocytopenia, leukopenia; very rarely - pancytopenia, agranulocytosis;
    skin: infrequently - urticaria, dermatitis, pruritus, skin rash; rarely - photosensitivity, alopecia; very rarely - toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme;
    laboratory data: rarely - hyponatremia; very rarely - hypomagnesemia, hypokalemia / hypocalcemia (due to severe hypomagnesemia);
    allergic reactions: rarely - hypersensitivity reactions (in particular, angioedema, fever, anaphylactic shock / anaphylactic reaction);
    others: infrequently - peripheral edema; rarely - sweating; very rarely - malaise (weakness).

Overdose

Overdose cases have not yet been described. The intake of 280 mg of esomeprazole was accompanied by symptoms from the gastrointestinal tract and general weakness. There are no symptoms after oral administration of Emanera 80 mg.
Hemodialysis is ineffective. There is no specific antidote. In case of an overdose, symptomatic treatment is indicated.

Special instructions

Emanera can reduce the severity of symptoms of malignant neoplasms and delay the diagnosis. In this regard, in the event of the appearance of alarming symptoms (dysphagia, repeated vomiting, significant spontaneous loss of body weight, melena or vomiting with an admixture of blood), as well as if a stomach ulcer is suspected / detected, malignant neoplasms must be excluded.
When carrying out long-term therapy (especially - longer than 12 months), medical supervision should be established for the condition of patients.
In cases of taking the drug on demand, if the nature of the symptoms changes, you should consult your doctor. Also, with this dosing regimen, it is necessary to take into account fluctuations in the plasma concentration of esomeprazole in the blood, especially when using Emanera with other drugs.
In the eradication of Helicobacter pylori, the possible interaction between the components of the triple therapy should be taken into account. Clarithromycin is a potent inhibitor of CYP3A4, therefore, contraindications and drug interactions must be taken into account when prescribing triple therapy to patients who are simultaneously taking drugs metabolized by CYP3A4 (in particular, cisapride).

Application during pregnancy and lactation

    pregnancy: Emanera may be prescribed with caution after evaluating the benefit / risk ratio;
    lactation period: due to limited experience of use, the drug is not prescribed.

Pediatric use

Due to the lack of data confirming the safety / effectiveness of therapy, Emanera is not prescribed to patients under 12 years of age.
In children over 12 years old, the drug can only be used in the treatment of GERD.

With impaired renal function

According to the instructions, Emanera is prescribed with caution in patients with severe renal failure due to limited experience of use.

Drug interactions

Possible interactions:
    drugs, the absorption of which depends on the pH level: a change in their absorption (ketoconazole, itraconazole, erlotinib - decrease; digoxin - increase);
    some antiretroviral drugs (atazanavir, nelfinavir): changes in their absorption (mechanism and clinical significance are not always known); the combination is not recommended;
    saquinavir: an increase in its serum concentration in the blood;
    drugs metabolized by CYP2C19 (citalopram, diazepam, clomipramine, imipramine, phenytoin, etc.): an increase in their plasma concentration in the blood (a decrease in their dose may be required);
    voriconazole, cilostazol: an increase in their Cmax and AUC;
    warfarin (long-term combination therapy): a clinically significant increase in the INR index (it is recommended to control this indicator at the beginning and after the end of combined use, including combinations with other coumarin derivatives);
    cisapride: an increase in AUC and T1 / 2; the Cmax value does not change significantly;
    methotrexate: an increase in its serum concentration (temporary withdrawal of esomeprazole may be required);
    clopidogrel: conflicting data on clinical manifestations of interaction for major cardiovascular events;
    tacrolimus: an increase in its serum concentrations;
    clarithromycin: increase in the AUC value of esomeprazole;
    rifampicin and St. John's wort preparations (drugs that induce CYP2C19 and CYP3A4 isoenzymes): a decrease in the plasma concentration of esomeprazole in the blood;
    voriconazole (a combined inhibitor of isoenzymes CYP2C19 and CYP3A4): a significant increase in the AUC of esomeprazole (in severe hepatic impairment / prolonged therapy, a dose reduction of Emanera may be required).

Terms and conditions of storage

Store out of the reach of children at temperatures up to 30 ° C.
Shelf life is 2 years.

Reviews about Emanera

According to reviews, Emanera is an affordable and effective drug. It is noted that it quickly relieves unpleasant symptoms, including heartburn, causes minimal side effects, and has a long-term effect. Among the shortcomings, they indicate the likelihood of increased abdominal pain and the development of "acid rebound" after the end of therapy.

Terms of sell

You don't need a prescription to buy Emanera.