Эзолонг

General characteristics. Structure:

Active ingredient: magnesium esomeprazole trihydrate of equivalent 20 or 40 mg of esomeprazole.

Excipients: the tselyulloza is microcrystallic, Natrii hydrocarbonas, silicon dioxide of kolloidniya anhydrous, коповидон, povidone (K-30), magnesium stearate, talc, fragrance of myatniya.

It is applied to treatment of diseases of digestive tract, reduces secretion of a gastric juice.

Pharmacological properties:

Pharmacodynamics. Antiulcerous means — inhibitor of the protonew pump, dextrorotatory isomer of an omeprazol; reduces secretion of HCl in a stomach by specific inhibition of the protonew pump in covering cells. Being the weak basis and passing into an active form in acid medium of secretory tubules of covering cells of a mucous membrane of a stomach, it is activated and suppresses the proton pump — H+/K+ to ATFAZ. Suppresses basal and stimulated secretion of HCl. Action comes in 1 h after oral administration of 20 mg or 40 mg.

At daily administration of drug within five days in a dose of 20 mg of 1 times a day average maximum concentration of HCl after stimulation by Pentagastrinum decreases by 90%. At reception of esomeprazole in a dose of 40 mg treatment the reflux esophagitis comes approximately at 78% of patients in 4 weeks of therapy and at 93% — in 8 weeks. Treatment by esomeprazole in a dose of 20 mg 2 times a day in a combination with standard antibacterial HP during 1 week leads to a successful eradikation of Helicobacter pylori approximately at 90% of patients.

Patients with an uncomplicated ulcer of a 12-perstny gut after 1 week of an eradikatsionny course do not need the subsequent monotherapy by anti-secretory drugs for healing of an ulcer and elimination of symptoms.

Pharmacokinetics. It is unstable in acid medium.

In vivo only an insignificant part of esomeprazole turns into R-isomer. It is quickly absorbed. TCmax is 1–2 h. Absolute bioavailability at repeated reception of 20 mg once in days — 89%. Distribution volume — 0,22 l/kg. Communication with proteins of plasma — 97%. It is completely metabolized with participation of system of P450 cytochrome. The main part is metabolized with the participation of a specific polymorphic isoenzyme of CYP2C19, at the same time hydroxies - and demetilirovanny metabolites of esomeprazole are formed. Metabolism of the rest is carried out by other specific isoenzyme of CYP3A4; at the same time it is formed sulfoderivative esomeprazole, being the main metabolite defined in plasma. All metabolites pharmacological are inactive.

Patients with an active isoenzyme have CYP2C19 ("bystry" metabolizator) system clearance — 17 l/h after a single dose and 9 l/h — after multiple dose. T1/2 is 1,3 h at systematic reception in the mode of dosing of 1 times a day. AUC increases against the background of multiple dose (nonlinear dependence of a dose and AUC at systematic reception that is a consequence of decrease in metabolism at "the first passing" through a liver, and also decrease in the system clearance caused by CYP2C19 isoenzyme inhibition esomeprazole and/or its sulfocontaining metabolite).

Does not kumulirut. To 80% of the accepted dose it is removed in the form of metabolites by kidneys (less than 1% — in not changed look), other quantity — with bile. At "slow" metabolizator (1–2%) metabolism of esomeprazole is carried out generally with participation of CYP3A4. At systematic reception of 40 mg of esomeprazole of 1 times a day average AUC for 100% exceeds value of this parameter at patients with active metabolism. Average Cmax values in plasma at patients with inactive metabolism are increased approximately for 60%.

At patients of advanced age (71–80 years) metabolism of esomeprazole does not undergo considerable changes. Metabolism of esomeprazole at patients with a slight or average liver failure is similar to that at patients with normal function of a liver. At a heavy liver failure the speed of metabolism is reduced that is followed by increase in AUC twice. Metabolism of esomeprazole at patients with a renal failure does not change.

Indications to use:

Gastroesophageal reflux disease (GERB): an erosive reflux esophagitis (treatment), prevention of a recurrence at patients with the cured esophagitis, a symptomatic treatment of GERB. As a part of a combination therapy: the peptic ulcer of a stomach and a 12-perstny gut associated with Helicobacter pylori (treatment and prevention).

Route of administration and doses:

Inside. The tablet should be swallowed entirely, washing down with liquid. Tablets cannot be chewed or broken.

Treatment erosive reflux esophagitis: on 40 mg of 1 times a day during 4 weeks.

The additional 4 weeks course of treatment is recommended when after the first course treatment of an esophagitis does not come or symptoms remain.

Prevention of a recurrence at patients with the cured esophagitis: on 20 mg of 1 times a day.

Symptomatic treatment of GERB: 20 mg of 1 times a day — to patients without esophagitis. If after 4 weeks of treatment symptoms do not disappear, it is necessary to conduct additional examination of the patient.

In a combination with the corresponding antibacterial therapy for Helicobacter pylori eradikation, treatment of an ulcer of the 12-perstny gut associated with Helicobacter pylori, prevention of a recurrence of round ulcers at patients with the peptic ulcer associated with Helicobacter pylori: esomeprazole — 20 mg, amoxicillin — 1 g and кларитромицин — 500 mg 2 times a day within 7 days.

With a renal failure and for patients of advanced age of dose adjustment it is not required to patients.

At a heavy liver failure the dose should not exceed 20 mg/days

Features of use:

In the presence of any alarming symptoms (for example such as considerable spontaneous loss of body weight, frequent vomiting, a dysphagy, vomiting with blood or a melena), and also in the presence of stomach ulcer (or at suspicion of stomach ulcer) it is necessary to exclude a possibility of a malignant new growth as treatment by esomeprazole can lead to smoothing of symptomatology and thus detain statement of the correct diagnosis.

The patients accepting drug during the long period (especially more than 1 year), have to be under regular observation of the doctor.

During treatment by inhibitors of the protonew pump concentration of gastrin in plasma increases as a result of reduced intragastric secretion of HCl.

At the patients accepting inhibitors of the protonew pump for a long time formation of ferruterous cysts in a stomach is more often noted. These phenomena are caused by physiological changes in result of inhibition of secretion of HCl. Cysts high-quality also show a tendency to disappearance.

There are no data on use of esomeprazole during pregnancy now. At administration of esomeprazole the animal did not reveal any direct or indirect negative impact on development of an embryo or a fruit. Administration of racemic drug also did not make any negative impact on animals during pregnancy, childbirth, and also during post-natal development. Nevertheless it is necessary to appoint drug pregnant only in that case when the expected advantage for mother exceeds possible risk for a fruit. It is unknown whether esomeprazole with breast milk is emitted.

Do not apply in pediatrics.

Side effects:

During clinical trials and after implementation of Ezolonga in broad medical practice the listed below side effects were established. Dozozavisimy effects were not revealed.

Disturbances of system of blood and lymph: leukopenia, thrombocytopenia, агрунолоцитоз, pancytopenia.

Disturbances of immune system: hypersensitivity reactions, such as fever, Quincke's disease and acute anaphylaxis.

Metabolism disturbances: peripheral hypostases, hyponatremia.

Mental disorders: sleeplessness, excitement, depression, confusion of consciousness, aggression, hallucinations.

Disturbances of a nervous system: headache, weakness, paresthesia, drowsiness, taste disturbance.

Vision disorders: sight illegibility, conjunctivitis.

Disturbances from an acoustic organ: dizziness.

Disturbances of respiratory system: bronchospasm.

Digestion disturbances: an abdominal pain, a lock, diarrhea, abdominal distention, nausea, vomiting, dryness in a mouth, stomatitis, GIT candidiasis.

Disturbances of gepatobiliarny system: increase in levels of liver enzymes, hepatitis with/without jaundice, a liver failure, encephalopathy at patients with liver diseases.

Disturbance of skin and soft tissues: dermatitis, an itch, rash, an alopecia, photosensitivity, a multiformny erythema, Stephens's syndrome — Johnson, a toksichchesky epidermal necrolysis.

Musculoskeletal disturbances: arthralgia, mialgiya, muscular weakness.
Disturbances from kidneys and an urinary system: intersticial nephrite.

Disturbances of reproductive system: gynecomastia.

General disturbances: the increased sweating.

Interaction with other medicines:

Reduces absorption of a ketokonazol and itrakonazol.

Esomeprazole inhibits CYP2C19 and CYP3A4 therefore combined use of esomeprazole with other. Can lead hp in which metabolism CYP2C19 takes part (diazepam, to tsitalopra, Imipraminum, кломипрамин, Phenytoinum, etc.) to increase in their concentration in plasma and demand a dose decline.

Esomeprazole does not cause clinically significant changes of pharmacokinetics of amoxicillin, quinidine and warfarin.

At joint reception of 30 mg of esomeprazole and diazepam the clearance enzyme - a substrate complex (CYP2C19 diazepam) decreases by 45%.

In plasma of patients with epilepsy the minimum concentration of Phenytoinum increase by 13% at its combination from 40 mg of esomeprazole. In this regard it is recommended to control concentration of Phenytoinum in plasma in an initiation of treatment esomeprazole and at its cancellation.

The concomitant use of 40 mg of esomeprazole with tsizapridy leads to increase in values of pharmacokinetic parameters of a tsizaprid: AUC — for 32% and T1/2 — for 31%, however concentration of a tsizaprid in plasma at the same time considerably do not change; цизаприд does not exert impact on electrophysiologic parameters of heart at this combination.

Combined use of esomeprazole with klaritromitsiny (500 mg 2 times a day) which inhibits CYP3A4, leads to increase in AUC esomeprazole twice. Correction of the mode of dosing of esomeprazole in this case is not required.

Reduces concentration of an atazanavir in a blood plasma.

Contraindications:

Hypersensitivity (including to the replaced benzimidazoles), a concomitant use with atazanaviry (concentration in plasma of an atazanavir decreases), the lactation period.

With care. Pregnancy.

Do not apply to children.

Overdose:

The overdoses of Ezolonga given relatively are limited. Gastrointestinal symptoms and weakness are described after reception of esomeprazole in a dose of 280 mg. The single dose of esomeprazole of 80 mg will not cause heavy side effects. The special antidote is unknown. Esomeprazole substantially contacts proteins of a blood plasma and therefore it is not dialyzed. At overdose treatment has to be symptomatic, it is also possible to hold the supporting events.

Storage conditions:

To store in original packaging in places, unavailable to children, at a temperature of 25 degrees Celsius.

Issue conditions:

According to the recipe

Packaging:

On 7 tablets in the blister. On 1 or 2 blisters in a cardboard box.