Emanera: instructions for use, indications,contraindications, dosage, course

Update: October 2018

Emanera is an effective anti-ulcer drug, characterized by
specific, directed mechanism of action – suppression
secretion of gastric hydrochloric acid. In the acidic secretory environment
tubules of parietal cells lining the gastric mucosa,
goes into the active form and reduces the basal and stimulated
hydrochloric acid secretion.

Emaner’s pills (although it is a philistine name, drug
available in capsules) are included in the treatment regimen of Helicobacter pylori,
demonstrate high efficacy in the complex therapy of infection
and help prevent relapses.

Фармакологическая группа: Средство, снижающее секрецию
gastric glands.

Composition, physico-chemical properties, price

The drug is available in the form of capsules of 20 and 40 mg with
enteric housing and cap.

The main substance (core pellets) 20,645 or 41,29 mg of esomeprazole magnesium
Auxiliary components (core pellets) Sugar lump, povidone, sodium lauryl sulfate
Pellet shell Opadry II white, magnesium hydroxycarbonate, methacrylic acid
and ethyl acrylate copolymer (1: 1); 30% dispersion, talc, macrogol
6000, titanium dioxide, polysorbate 80
Gelatin capsules Dye ferric oxide red, titanium dioxide, gelatin
Physicochemical properties Light pink capsules with white (or almost white) pellets
inside
Packaging On 7, 14, 28 capsules in the blister, in packs cardboard
Price 20 mg № 14: 170-300 rubles., 40 mg № 14: 270-600 rubles.

pharmachologic effect

The active substance Emaners (esomeprazole) is
an inhibitor of proton application of parietal cells of the gastrointestinal tract. Omeprazole
has two isomers: esomeprazole (S-isomer) and R-isomer.
The pharmacodynamics of both isomers is about the same, but for the treatment of
stomach ulcers usually use the first.

The active substance of the drug is a weak base: in acidic
medium concentration of the base increases, it goes into
active form, inhibiting the enzyme H + K + -ATRazu – acid pump.
This causes a suppression of basal and stimulated secretion.
acids.

Already after 1 hour after ingestion, the production of acids in the gastrointestinal tract is suppressed.
The effectiveness of a drug depends on its plasma.
concentration.

  • Reception on 20 mg of an agent once a day 5 days in a row
    leads to a significant decrease in the concentration of hydrochloric acid
    (approximately 91%).
  • Treatment at a dose of 40 mg for 1 month in patients with
    reflux esophagitis in 78% of cases leads to a cure. With
    a two-month course of recovery is 93%.
  • Withем эзомепразола в дозе по 40 мг ежедневно в сочетании с
    antibiotics course 1 week leads to recovery in 90%
    patients with gastric ulcer associated with helicobacter
    pylori
  • The drug is more effective in treating patients with ulcers.
    stomachs that have used nonsteroidal anti-inflammatory
    drugs compared to ranitidine, therefore, is
    the preferred drug of choice.

Emaner is prescribed for the healing of ulcers that have developed on the background
taking nonsteroidal anti-inflammatory drugs, selective
COX-2 inhibitors. Also often prescribed in complex therapy.
for the prevention of gastric ulcers in the treatment of specific
medications that can destroy the gastrointestinal mucosa.

Pharmacokinetics and pharmacodynamics

Esomeprazole is destroyed in an aggressive acid environment, therefore
the active ingredient is placed in an enteric capsule,
inside которых находятся пеллеты лекарства – оболочка пеллет также
resistant to the effects of gastric juice. Small
the proportion of the substance is transformed into the R-isomer in vivo. On reception
food absorption of esomeprazole decreases slightly, but not
substantially.

The drug is well absorbed in the digestive tract, the maximum in blood plasma
determined within 1-2 hours. Bioavailability is 64%, and at
long reception reaches 89%. On suction efficiency in
food that is eaten parallel
with the drug. Associated with plasma proteins by 97%.

Esomeprazole is metabolized in the liver under the influence of cytochrome
P450, as well as with the participation of isoenzymes CYP3A4 and CYP2C19. Plasma
clearance after a single dose of 17 liters per hour, with
long reception – 9 liters per hour. In patients with reduced
CYP2C19 activity metabolism of esomeprazole is CYP3A4, with
this value of concentration increases. Patients with pathologies
kidney and liver metabolism of the active substance may be disturbed.
Pharmacokinetics in patients over the age of 12 years is almost nothing.
does not differ from that in adults.

Does not accumulate and does not accumulate in the tissues. Period
the half-life is about 1.5 hours, with long-term treatment this
the period is lengthened. If the drug was taken once, then it
excreted very quickly. Metabolites are excreted by the kidneys.
or the intestines, about 1% of the substance is present in the urine in
unchanged form.

Pharmacokinetics in some groups of patients

  • About 3% of people have reduced CYP2C19 isoenzyme activity,
    so the metabolism of the drug performed with the participation of CYP3A4. The average
    the plasma concentration of the drug in these patients is 60
    % above.
  • In older people (from 71 years old) no significant changes were noted.
    in the metabolism of the drug.
  • In women, there is an increase in the average AUC value of about
    30% after a single dose. Further sexual differences in
    pharmacokinetics not observed.
  • With тяжелых нарушениях работы печени скорость метаболизма
    reduced, so the maximum dose for these patients is 20 mg per
    day.

Indications for use

Withменение Эманеры показано в следующих случаях:

  • GERD;
  • gastric and duodenal ulcer, including those caused by
    Helicobacter pylori;
  • prevention of diseases of viticulatitis, which may develop on the background
    taking NSAIDs;
  • erosive reflux esophagitis;
  • maintenance therapy after cured erosive
    reflux esophagitis and peptic ulcers (relapse prevention);
  • Helicobacter pylori diseases;
  • prevention of re-development of peptic ulcers and repeated
    bleeding them them during treatment with NSAIDs and after the / m injection
    drugs that can reduce the secretion of hydrochloric acid;
  • conditions associated with increased gastric secretion
    (idiopathic hypersecretion inclusive);
  • Zollinger-Ellison syndrome.

Contraindications

Emanera is contraindicated in the following cases:

  • allergic to the components of the drug;
  • fructose intolerance is hereditary;
  • taking nelfinavir or atazanavir;
  • children’s age up to 12 years and older for other indications for
    исключением GERD;
  • severe kidney disease;
  • glucose-galactose malabsorption;
  • deficiency of sucrase-isomaltase;
  • lactation period.

special instructions

The instructions for use Emaners indicated that in case of violations
liver function dose adjustment is not required. But if there are
serious violations of the liver, then the maximum daily
Reception – only 20 mg.

With развитии симптомов возникновения онкопатологии во время
treatment (vomiting with blood, severe weight loss, reduced
appetite) it is important to eliminate the likelihood of cancer, to perform
additional research and postpone treatment until denial
presumptive diagnosis.

With длительном лечении требуется контроль врача. Besides,
such patients should consult a doctor immediately if
there is any change in symptoms.

The drug contains sucrose.

On concentration and reaction speed
renders.

The appointment during pregnancy is justified only if the expected
positive action for the mother exceeds the likely risks for
fetus. In epidemiological studies and experiments on
animals not identified fetotoksicheskie effects and pathologies of development
of the fetus during treatment with Emaneroy, however this is not a basis
for the free use of Emaners in pregnant women.

With применении Эманеры для лечения Helicobacter pylori важно
consider the interaction of drugs included in the triple therapy.
So, clarithromycin, which is included in the scheme, is strong
CYP3A4 inhibitor – it is important to take into account contraindications and interaction
antibiotic for patients who are simultaneously taking medications,
metabolized by CYP3A4.

Side effects

During the course of treatment, the salt level is significantly reduced.
acid in the stomach. This leads to an increase in gastrin levels.
serum, as well as the growth of enterochromaffin-like
cells.

With лечении повышается риск формирования гландулярных кист в
stomachs that are benign do not require
surgical intervention and are reversible.

Also, treatment to some extent increases the risk of infectious
diseases (salmonellosis, and others). This is due to the fact that
decrease in the acidity of the stomach contents leads to an increase in
the amount of microbial flora that is there in the norm.

The following effects may occur during treatment:

  • CNS: headache, insomnia, drowsiness, dizziness,
    depression, CNS overexcitement, hallucinations, aggression, sweating,
    weakness;
  • Gastrointestinal tract: changes in taste perception, constipation or diarrhea, vomiting,
    flatulence, dry mouth, painful discomfort in the abdomen,
    hepatitis, candidiasis, exacerbation or the development of diseases
    the liver;
  • Urinary system: nephritis, edema;
  • Respiratory system: bronchospasm;
  • The reproductive system: gynecomastia;
  • Musculoskeletal system: myalgia, muscle weakness,
    arthralgia;
  • Bodies of sight: temporary decrease in vision;
  • Hypersensitivity reactions: urticaria, angioedema,
    skin rash, dermatitis, alopecia, anaphylactic shock,
    sensitivity to light, Stephen-Johnson syndrome;
  • Blood side: agranulocytosis, thrombocytopenia, leukopenia,
    pancytopenia, hyponatremia, hypomagnesemia, hypocalcemia,
    hypokalemia.

Dosage

Withнимают внутрь, не измельчая и не разжевывая, запивают большим
amount of water. If the patient cannot
swallow the drug, the contents of the capsules can be dissolved in clean
water (half a glass), stir and take the resulting solution
30 minutes after mixing. After that in the same glass
add more water, rinse it with the walls of the glass and drink. Other
liquids except water, unacceptable – the protective shell of the pellets can
dissolve. Also, do not crush or chew.
pellets.

May be administered by nasogastric tube as follows.
way: the contents of the capsule is poured into a special syringe, add
25-50 ml of water and leave 5-10 ml of air, shake well,
until a suspension is formed. The syringe tip is checked for
passability and connect to the probe (holding tip up),
then the syringe is quickly shaken and turned, part of the suspension
(5-10 ml) immediately injected into the probe. Turn the syringe again
tip up, shake, tilt and reintroduce part
suspensions. The cycle is repeated until the entire drug is injected. If a
part of the drug will remain as a precipitate in the syringe or on its
walls: fill the syringe with 25 ml of water and leave 5 ml of air and
repeat the cycle described above.

Duration of treatment and dosage are always selected by the treating
a doctor with the following recommendations:

  • Symptomatic therapy of GERD: 20 mg 1 time a day for
    4 weeks (the course can be extended further, but only
    after examination, if after 4 weeks of treatment does not occur
    improvements);
  • treatment of erosive reflux esophagitis: 40 mg 1 time per day
    within 30 days (the course can be extended for another month, but after
    break);
  • GERD prophylaxis and support to rule out relapse: 20 mg each
    1 per day;
  • ulcers of the stomach and duodenum (including those caused by
    Helicobacter pylori): in the complex therapy of 20 mg of the drug 2
    once a day for 1-2 weeks;
  • treatment of gastric ulcer with NSAID therapy: 20-40 mg 1 time per
    day, 1-2 months;
  • профилактика язвы желудка: по 20-40 мг 1 per day;
  • prevention of bleeding from peptic ulcers after IV
    drugs that reduce the level of hydrochloric acid: 40 mg 1 time per day
    1 month;
  • idiopathic hypersecretion, Zollinger-Ellison syndrome and
    other conditions characterized by hyperactive gastric
    secretion: 40 mg 2 times a day. Dose and duration of treatment
    selected individually, but most often enough doses of 80-160
    mg / day

Overdose

Officially, there were no cases of overdose. If a
take 280 mg of the drug at once, there will be a weakness and
gastrointestinal dysfunction. There is no specific antidote, hemodialysis
not effective, symptomatic therapy is performed.

Drug interactions

  • With одновременном лечении антацидами, кетоконазолом,
    intraconazole, erlotinib and secretion reducing drugs
    glands of the stomach, the latter can be absorbed worse.
  • Antiretroviral drugs (atazanavir, rhinotavir) with
    combined with Emaner have less efficacy due to
    reduced plasma concentrations insufficient to render
    therapeutic effect.
  • Medicines whose metabolism involves CYP2C19 are better not
    combine with this medicine. For this reason, while
    prescription with diazepam, phenytoin, citalopram, imipramine,
    Clomipramine, voriconozol, need to be careful: probably
    the increase in the concentration of the latter in the plasma, which means that
    require dose adjustment.
  • With сочетании с кумарином, варфарином нужно контролировать
    INR indicators.
  • With комбинации с кларитромицином показатель AUC у эзомепразола
    increases by 2 times.
  • It is well combined with amoxicillin and quinidine.
  • With назначении метотрексата в высоких дозах рекомендуется на
    time to cancel Emaner.

Analogs

Preparations with a similar active ingredient are:

Esomeprazole Canon (20 mg, № 14 – from 200 rub.) Neotext (20 mg, № 14 – from 800 rubles). Nexium (20 mg, number 28 – from 2,200 rubles)

Автор: врач-гигиенист, эпидемиолог

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