Omez dsr capsules 30mg + 20mg №30

Domperidone + Omeprazole

Dosage Form: modified release capsules Ingredients:

Each capsule contains:

active ingredients: omeprazole 20 mg (in the composition of the granules with an enteric coating 267 mg) *, Domperidone 30 mg (in the composition of the granules with a prolonged release of 100 mg) **;

Excipients: talc 2 mg.

* The composition of omeprazole granules:

active substance: omeprazole 20 mg;

Excipients: mannitol 137.86 mg, lactose monohydrate 9.66 mg, sodium lauryl sulfate 0.52 mg, sodium hydrogen phosphate 0.89 mg, sucrose (25/30) 24.35 mg, sucrose 8.54 mg, hypromellose 6 cps 0, 14 mg;

coating: hypromellose 6 cps 13 mg;

Enteric coating: methacrylic acid and ethyl acrylate copolymer [1: 1] (methacrylic acid copolymer [type C]) 40.47 mg, sodium hydroxide 0.54 mg, macrogol 6000 4.85 mg, talc 4.05 mg, titanium dioxide 2.13 mg.

** The composition of domperidone granules:

active substance: domperidone 30 mg;

Excipients: nonpairel sugar nugget 58.98 mg, colloidal silicon dioxide 0.48 mg, talc 4.51 mg, hypromellose 5 cps 0.57 mg;

coating: hypromellose 5 cps 2.34 mg, talc 0.71 mg, iron dye yellow oxide 0.12 mg, iron dye red oxide 0.04 mg, titanium dioxide 0.47 mg;

extended release coating: hypromellose 5 cps 0.40 mg, ethyl cellulose 10 cps 1.18 mg, triacetin 0.12 mg, talc 0.086 mg.

The composition of the capsules of gelatinous solid number "1": gelatin 85.42%, water 14.50%, sodium lauryl sulfate 0.08%.

The composition of black ink for inscription on the lid of the capsule: ethanol 29-33%, isopropanol 9-12%, butanol 4-7%, shellac 24-28%, iron dye black oxide (E172) 24-28%, ammonia aqueous 1-3%, propylene glycol 0.5-2%.

The composition of the red ink for inscription on the body of the capsule: ethanol 21-25%, isopropanol 12-16%, butanol 7-10%, shellac 22-27%, crimson dye [Ponso 4R] (E124) 18-24%, titanium dioxide (E171) 5-9%, ammonia water 1-3%, polysorbate 80 0.5-2%, propylene glycol 0.5-2%.

Pharmacotherapeutic group: Reflux esophagitis, combination treatment (proton pump inhibitor + dopamine receptor central blocker) ATX:

A.02.B.X Other anti-ulcer drugs

The combination of two active substances (domperidone and omeprazole) has a complex effect on the main pathogenesis of gastroesophageal reflux disease (GERD), dyspeptic disorders of various genesis. Domperidone enhances and synchronizes physiological peristaltic waves, omeprazole reduces the basal and stimulated secretion of hydrochloric acid.

Omeprazole

Mechanism of action

Omeprazole is concentrated in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, is activated and inhibits the proton pump - the enzyme H⁺/TO⁺-ATPase that provides dose-dependent highly effective inhibition of basal and stimulated secretion of hydrochloric acid, regardless of the stimulating factor.

Effect on stomach acidity

The maximum effect is achieved within 4 days of treatment.In patients with duodenal ulcer, omeprazole in a dose of 20 mg causes a steady decrease in 24-hour gastric acidity of at least 80%. When this is achieved a decrease in the average maximum concentration of hydrochloric acid after stimulation with pentagastrin by 70% within 24 hours. In patients with duodenal ulcer, omeprazole 20 mg with daily oral administration maintains the value of pH> 3 in the intragastric medium for an average of 17 hours per day. Inhibition of the secretion of hydrochloric acid depends on the area under the pharmacokinetic curve "concentration - time" (AUC) of omeprazole, and not on the concentration of the drug in the plasma at a given time.

Action on Helicobacter pylori

Eradication Helicobacter pylori when using omeprazole together with antibacterial agents, it is accompanied by rapid elimination of symptoms, a high degree of healing of the mucosal defects of the gastrointestinal tract and long-term remission of peptic ulcer, which reduces the likelihood of complications such as bleeding, as effectively as constant maintenance therapy.

Other effects

A decrease in the secretion of hydrochloric acid in the stomach leads to a slight increase in the risk of intestinal infections caused by Salmonella spp., Campylobacter spp. and Clostridium difficile. During treatment with drugs that lower the secretion of gastric glands, the concentration of gastrin in the serum increases. Owing to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A increases (see the section "Special Instructions").

Domperidone

A dopamine antagonist, combines peripheral (gastrokinetic) action and antagonism of dopamine receptors in the trigger zone of the brain (central action), due to which it has an antiemetic effect, stimulates the secretion of prolactin from the pituitary and eliminates the inhibitory effect of dopamine on the motor function of the gastrointestinal tract, strengthens and synchronizes the peristaltic waves, thereby accelerating the natural emptying of the stomach and increases the pressure of the sphincter of the lower esophagus.

Pharmacokinetics:

Omeprazole

The absorption of omeprazole is high, the time to reach maximum plasma concentration (Tc_max) is 0.5-1 hours. Bioavailability - 30-40%, after continuous administration 1 time per day increases to 60%.

Distribution. Communication with plasma proteins - 90-95%. Distribution volume 0.3 l / kg.

Metabolism. Part of omeprazole undergoes a presystemic hepatic metabolism involving more CYP2C19 than CYP3A4 with the formation of inactive metabolites. Omeprazole, not included by parietal cells in the process of formation of active metabolites, is completely metabolized in the liver. Total plasma clearance is 0.3-0.6 l / min.

Removal. The half-life (T_1/2) omeprazole is about 40 minutes. Excreted by the kidneys (70-80%) and with bile (20-30%).

In case of abnormal liver function, bioavailability increases and plasma clearance of omeprazole decreases.

In case of impaired renal function or in elderly patients, no changes in the bioavailability of omeprazole were observed.

Domperidone

This dosage form provides a slow release of the active substance.In the acidic dissolution tests, after 8 hours, from 75% to 83% of the nominal content of domperidone in one capsule is determined, and after 12 hours - from 86% to 94%.

Absorption fasting fast. Tc_max - 30-60 minutes. Low bioavailability (15%) is associated with the metabolism of the first passage in the intestinal wall and liver.

Distribution. Communication with plasma proteins - 90%. It penetrates into various tissues, passes badly through the blood-brain barrier.

Metabolized in the liver (including due to the effect of the first passage) and in the intestinal wall (by hydroxylation and N-dealkylation) with the participation of CYP3A4, CYP1A2 and CYP2E1 isoenzymes.

Excretion: 66% through the intestines (in unchanged form - 10%), kidneys - 33% (in unchanged form 1%) in the form of glucuronides. In severe chronic renal failure T_1/2 lengthened.

- dyspepsia, accompanied by slow emptying of the stomach, gastro-esophageal reflux, esophagitis (feeling of fullness in the epigastrium, feeling of bloating, pain in the upper abdomen; belching, flatulence; nausea, vomiting, heartburn with or without a gastrointestinal discharge in the mouth) ;

- Gastroesophageal reflux disease;

- nausea, vomiting, heartburn associated with gastroesophageal reflux disease, gastritis, gastric ulcer and duodenal ulcer, including after conducting eradication therapy.

- Hypersensitivity to the components of the drug and benzimidazoles;

- prolactin-secreting pituitary tumor (prolactinoma);

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

- deficiency of sucrase / isomaltase, fructose intolerance;

- concomitant use of erlotinib, posaconazole, nelfinavir, atazanavir, oral forms of Ketoconazole, Erythromycin, or other CYP3A4 inhibitors that prolong the QT interval, such as Fluconazole, voriconazole, Clarithromycin, amidarone, and telithromycin (see if you use fluconazole, voriconazole, clarithromycin, amidarone, and telithromycin)

- Gastrointestinal bleeding, mechanical obstruction or perforation, i.e. when stimulation of gastrointestinal motility can be dangerous;

- liver failure of moderate and severe severity;

- pregnancy and breastfeeding period;

- children's age up to 18 years.

Carefully:

- In the presence of a stomach ulcer (or suspected stomach ulcer), prior to surgery on the gastrointestinal tract;

- in the presence of "disturbing" symptoms: a significant spontaneous decrease in body weight, repeated vomiting, vomiting with blood, change the color of feces (tarry stools - melena), a violation of swallowing;

- when new symptoms appear or changes in existing symptoms of the gastrointestinal tract;

- in the presence of severe electrolyte disorders or heart disease, such as heart failure).

- with osteoporosis;

- in case of renal failure.

Pregnancy and lactation:

The use of Omez® JEM during pregnancy and during breastfeeding is contraindicated.

Omez® JEM is ingested on an empty stomach, 20-30 minutes before a meal (the contents of the capsule cannot be chewed) with a small amount of water.

Omez® DSR take one capsule once a day in the morning.

The maximum daily dose is 1 capsule of Omez® DSR, which corresponds to 20 mg of omeprazole and 30 mg of domperidone.

Application for violations of the liver. In case of mild abnormal liver function, dosing regimen adjustment is not required

Application for violations of renal function. Correction of a single dose is not required.

Use in the elderly. Correction of the dosing regimen is not required.

Possible side effects are listed below for body systems and the frequency of occurrence for omeprazole and domperidone: very often (> 1/10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000, including isolated cases and the frequency is not known).

Violations of the blood and lymphatic system

Omeprazole - rarely: leukopenia, thrombocytopenia; very rarely: agranulocytosis, pancytopenia, eosinophilia.

Immune system disorders

Omeprazole - rarely: hypersensitivity reactions: fever, angioedema, anaphylactic reaction / anaphylactic shock. Domperidone - very rare: anaphylactic reaction / anaphylactic shock, angioedema.

Metabolic and nutritional disorders

Omeprazole - rarely: hyponatremia; frequency is unknown: hypomagnesemia, which in severe cases can lead to hypocalcemia, hypokalemia.

Mental disorders

Omeprazole - infrequently: insomnia; seldom: hyperexcitability, depression, reversible confusion; very rarely: aggression, hallucinations. Domperidone is very rare: agitation, nervousness, irritability and irritability.

Nervous system disorders

Omeprazole - often: headache; infrequently: dizziness, paresthesias, drowsiness; rarely: taste disturbance. Domperidone - very rare: extrapyramidal effects, convulsions, drowsiness, headache.

Violations by the organ of vision

Omeprazole - infrequently: visual impairment, including a decrease in visual fields, a decrease in sharpness and clarity of visual perception (usually disappear after cessation of therapy).