Description
Description
Hard gelatin transparent capsules of size “2” with a colorless body, pink cap and black marking “OMEZ” on both sides of the capsule.
The contents of the capsule are granules of white or almost white color.
Latin name
Omez
Packing
30 pcs
Pharmacological action
Pharmacodynamics
Mechanism of action
Omeprazole is a weak base. It is concentrated in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, it activates and inhibits the proton pump, the enzyme H + / K + -ATPase.
The effect of omeprazole on the last stage of the formation of hydrochloric acid in the stomach is dose-dependent and provides highly effective inhibition of basal and stimulated secretion of hydrochloric acid, regardless of the stimulating factor.
Effect on gastric acid secretion
Omeprazole with daily oral administration provides fast and effective inhibition of daytime and nighttime hydrochloric acid secretion.
Maximum effect is achieved within 4 days of treatment. In patients with duodenal ulcer, omeprazole at a dose of 20 mg causes a steady decrease in 24-hour gastric acidity by at least 80%. This achieves a decrease in the average maximum concentration of hydrochloric acid after stimulation with pentagastrin by 70% within 24 hours.
In patients with a duodenal ulcer, does omeprazole 20 mg, with daily oral administration, maintain a pH value in the intragastric medium 3 on average for 17 hours a day.
Inhibition of hydrochloric acid secretion depends on the area under the pharmacokinetic curve ² Ñconcentration-time ² Ñ (AUC) of omeprazole, and not on the concentration of the drug in plasma at a given time.
Effect on Helicobacter pylori
Omeprazole has a bactericidal effect on Helicobacter pylori in vitro.
Eradication of Helicobacter pylori with omeprazole in combination with antibacterial agents is accompanied by a rapid elimination of symptoms, a high degree of healing of defects in the mucous membrane of the gastrointestinal tract and prolonged remission of peptic ulcer, which reduces the likelihood of complications such as bleeding, as effectively as continuous maintenance therapy.
Other effects associated with inhibition of hydrochloric acid secretion
In patients taking drugs that lower the secretion of the gastric glands for a long period of time, the formation of glandular cysts in the stomach of the cyst is benign and disappears on its own against the background of continued therapy.
A decrease in the secretion of hydrochloric acid in the stomach leads to a slight increase in the risk of developing intestinal infections caused by Salmonella spp., Campylobacter spp. and Clostridium difficile.
During treatment with drugs that lower the secretion of the glands of the stomach, the concentration of gastrin in the blood serum increases. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A increases (see the section “Special Instructions”).
Pharmacokinetics
Absorption
Omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum concentration (Cmax) of omeprazole in the blood plasma is reached after 0.5 ² 1 hours. Bioavailability after a single oral administration is 30 ² 40%, after constant administration once a day, bioavailability increases to 60%. Eating does not affect the bioavailability of omeprazole.
Distribution of
The binding index of omeprazole to plasma proteins is about 95%, the distribution volume is 0.3 l / kg.
Metabolism
A portion of omeprazole undergoes a presystemic hepatic metabolism involving the isoenzymes CYP2C19 and CYP3A4 to form inactive metabolites of sulfone, sulfide and hydroxy-omeprazole. Omeprazole, not included by parietal cells in the formation of active metabolites, is completely metabolized in the liver also with the participation of CYP2C19 and CYP3A4 isoenzymes.
The total plasma clearance is 0.3-0.6 l / min.
Excretion
The elimination half-life is about 40 minutes (30-90 minutes). About 80% is excreted as metabolites by the kidneys, and the rest by the intestines.
Special patient groups
No significant changes in the bioavailability of omeprazole in elderly patients or in patients with impaired renal function. In patients with impaired liver function, an increase in the bioavailability of omeprazole and a significant decrease in plasma clearance are noted.
Indications
Adults
Peptic ulcer of the stomach and duodenum (including prevention of relapse).
Gastroesophageal reflux disease (GERD).
Hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis).
Helicobacter pylori eradication in infected patients with peptic ulcer and duodenal ulcer (as part of combination therapy).
Prevention and treatment of damage to the mucous membrane of the stomach and duodenum due to the use of non-steroidal anti-inflammatory drugs (NSAIDs-gastropathy): dyspepsia, erosion of the mucous membrane, peptic ulcer.
Prevention of Mendelssohn syndrome (aspiration pneumonitis).
Children
Over the age of 2 years, weighing more than 20 kg: for the treatment of gastroesophageal reflux disease
over the age of 4 years, weighing more than 20 kg: for treating the duodenal ulcer caused by Helicobacter pylori.
Safety and effectiveness for other indications in pediatric patients not established.
Contraindications
Hypersensitivity to omeprazole, substituted benzimidazoles or other components of the drug.
sucrose / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption (due to the presence of sucrose in the preparation).
Concomitant use with erlotinib, posaconazole, nelfinavir and atazanavir.
The use of omeprazole in children is contraindicated, except as indicated: gastroesophageal reflux disease for children over 2 years of age and duodenal ulcer caused by Helicobacter pylori for children over 4 years of age (see section “Method of administration and dosage”).
Before using the drug, it is necessary to consult a doctor in the following cases: in the presence of a previously diagnosed stomach ulcer of a serious liver disease, accompanied by liver failure of renal failure of jaundice previous surgical intervention on the gastrointestinal tract
in the presence of “disturbing” symptoms: significant spontaneous weight loss, repeated vomiting, vomiting with blood, change in stool color (tarry stool – melena),
swallowing disorder when new symptoms appear or existing symptoms of the gastrointestinal tract
change with simultaneous use with one or more of the following drugs: clopidogrel, digoxin, ketoconazole, itraconazole, warfarin, cilostazole, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampicin, hypericum preparations ennogo (see. See “The interaction with other drugs”).
Osteoporosis. Although a causal relationship with the use of omeprazole with fractures in the setting of osteoporosis has not been established, Patients at risk of developing osteoporosis or fractures against its background should be under appropriate clinical supervision.
Use during pregnancy and lactation
Research results have shown that there is no adverse effect of omeprazole on the health of pregnant women, the fetus or the newborn.
Omeprazole is excreted in breast milk, but when used in therapeutic doses, exposure to the baby is unlikely.
Omeprazole is approved for use during pregnancy and during breastfeeding.
Special instructions
In the presence of any alarming symptoms, such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting with blood or melena, and also if there is a stomach ulcer (or if a stomach ulcer is suspected), the possibility of a malignant neoplasm should be excluded, since treatment with Omez ® can smooth out the symptoms and delay the diagnosis.
Decreased hydrochloric acid secretion in the stomach by proton pump inhibitors leads to an increase in the growth of normal intestinal microflora and can lead to a slight increase in the risk of intestinal infections caused by bacteria of the genus Salmonella spp., Campylobacter spp., as well as bacteria Clostridium difficile.
A decrease in acidity while taking omeprazole can also lead to a decrease in the absorption of vitamin B12 (cyanocobalamin).
With the simultaneous use of omeprazole with clopidogrel, a decrease in the antiplatelet effect of the latter is observed.
Patients at risk of developing osteoporosis or fractures on its background should be under appropriate clinical supervision, although a causal relationship between the use of omeprazole / esomeprazole and fractures on the background of osteoporosis has not been established.
There are reports of severe hypomagnesemia in patients receiving proton pump inhibitor therapy, including omeprazole, over one year old. Patients receiving omeprazole therapy for a long time, especially in combination with digoxin or other drugs that reduce plasma magnesium (diuretics), require regular monitoring of magnesium content.
Effect on laboratory tests
Decreasing the level of hydrochloric acid secretion can lead to an increase in the concentration of chromogranin A (CgA), which affects the results of examinations to detect neuroendocrine tumors. To prevent this effect, therapy with proton pump inhibitors must be stopped 5 days before the study of CgA concentration.
During treatment with omeprazole, dizziness, drowsiness, and visual impairment may occur, therefore care should be taken when driving vehicles and performing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Composition
Each capsule contains:
Active ingredient:
omeprazole 20 mg.
Excipients:
Granules:
mannitol 143.567 mg,
lactose 10.14 mg,
sodium lauryl sulfate 0.545 mg,
sodium hydrogen phosphate 0.923 mg,
sucrose 8.951 mg,
sucrose 25.25 (25rd) 0.139 mg.
Coverage:
hypromellose 6 cps 10.49 mg.
Enteric coating:
methacrylic acid and methyl methacrylate copolymer [1: 1] (methacrylic acid copolymer [type C]) 37.8 mg,
sodium hydroxide 0.504 mg,
macrogol-6000 4.536 mg,
talc 4.41 mg,
talc 4.41 mg,
titanium dioxide 3.15 mg.
Composition of gelatin hard capsules No. 2:
propyl parahydroxybenzoate,
methyl parahydroxybenzoate,
sodium lauryl sulfate,
water,
dye azorubine (E122) (capsule cap),
gelatin.
Dosage and administration
Inside, washed down with a sufficient amount of water (the contents of the capsule should not be chewed), 30 minutes before a meal.
If the patient cannot swallow the whole capsule, you can mix its contents with a slightly acidified liquid, juice, or fruit puree. DO NOT DISSOLVE in carbonated drinks or milk. The resulting mixture should be taken orally immediately after preparation.
Adults
In case of gastric and duodenal ulcer (including for the prevention of relapse) – 20 mg once a day for patients resistant to treatment with other anti-ulcer drugs, a dose of 40 mg / day is prescribed, the course of treatment for duodenal ulcer is 2 weeks, if necessary – up to 4 weeks with gastric ulcer – 4-8 weeks.
In gastroesophageal reflux disease (GERD), depending on the severity of esophagitis, from 20 mg to 80 mg per day. The duration of the main course also depends on the severity of esophagitis and is 4-8 weeks. Maintenance therapy should be carried out at the lowest effective dose, including on demand and intermittent courses. The duration of maintenance therapy is determined by the doctor.
In hypersecretory conditions (Zollinger-Ellison syndrome, stressful ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis) – 60 mg if necessary, increase the dose to 80-120 mg / day (in this case, it is prescribed in 2-3 doses).
To eradicate Helicobacter pylori in infected patients with gastric and duodenal ulcer according to the recommendations of the Maastricht-4 Omez ® working group, it can be included in the following treatment regimens:
First line (standard triple regimen)
Omez ® 20 mg 2 times per day + clarithromycin 500 mg 2 times a day + amoxicillin 1000 mg 2 times a day. To increase the effectiveness of therapy, it is possible to prescribe Omez ® at a dose of 40 mg (2 capsules of 20 mg) 2 times a day (doubling the standard dose) and increasing the duration of the course from 7 to 10-14 days.
Second line (four-component)
It is used if the standard triple therapy is ineffective, or if the penicillin group is intolerant. Bismuth tripotassium dicitrate (120 mg 4 times a day) in combination with Omez ® 20 mg 2 times a day, tetracycline (500 mg 4 times a day), metronidazole (500 mg 4 times a day) for 10 days.
The third line and other alternative treatment options are prescribed based on a study of the individual susceptibility of H. pylori to antibacterial drugs.
– For the prevention and treatment of injuries of the mucous membrane of the stomach and duodenum caused by the use of non-steroidal anti-inflammatory drugs (NSAIDs gastropathy), such as dyspepsia, mucosal erosion, peptic ulcer, Omez ® is prescribed at a dose of 20 mg daily for 30 minutes to prevent it before breakfast during the entire course of treatment of NSAIDs for the purpose of treatment – at a dose of 20 mg 2 times or once 40 mg per day for 4-8 weeks.
– For the prevention of Mendelssohn syndrome (aspiration pneumonitis) – 40 mg once.
Children
over the age of 2 years,ki)
over the age of 4 years, with a body weight of more than 20 kg: with a duodenal ulcer caused by Helicobacter pylori, at a dose of 20 mg once a day in combination with antibacterial drugs (recommended dose of omeprazole in Helicobacter pylori eradication schemes in pediatric practice is 1-2 mg per kilogram of body weight per day).
Use of the drug in special cases
Impaired renal function. Dose adjustment is not required.
Impaired liver function. In patients with impaired liver function, the bioavailability and clearance of omeprazole increase. In this regard, the therapeutic dose should not exceed 20 mg per day.
Old age. The metabolic rate of omeprazole in the elderly is reduced, but dose adjustment is not required.
Side effects
The incidence of adverse drug reactions is presented according to the following gradation: very common (> 1/10) often ( 1/100, < 1/10) infrequently ( 1/1000, <1/100) rarely ( 1/10000, <1/1000) very rarely (<1/10000, including isolated cases). Blood and lymphatic system disorders: rarely – leukopenia, thrombocytopenia, hypochromic microcytic anemia in children very rarely – agranulocytosis, pancytopenia, eosinophilia. Immune system disorders: rarely hypersensitivity reactions: fever, angioedema, anaphylactic reaction / anaphylactic shock. Metabolism and nutrition disorders: rarely – hyponatremia frequency is unknown – hypomagnesemia, which in severe cases can lead to hypocalcemia, hypokalemia. Disorders of the psyche: infrequently – insomnia is rare – increased arousal, depression, reversible confusion very rarely – aggression, hallucinations. Nervous system disorders: often – headache is infrequent – dizziness, paresthesia, drowsiness rarely – impaired taste. Visual impairment: rarely – blurred vision. Hearing disorders and labyrinthine disorders: infrequently – impaired auditory perception, vertigo. Respiratory, chest and mediastinal disorders: rare – bronchospasm. Gastrointestinal disorders: often – abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting rarely – dry mouth, stomatitis, gastrointestinal candidiasis, microscopic colitis single cases – formation of gastric glandular cysts during prolonged cystic lengthening with clarithromycin (a consequence of inhibiting hydrochloric acid secretion, is benign, reversible). Disorders from the liver and biliary tract: infrequently – increased activity of “hepatic” enzymes and alkaline phosphatase (reversible) rarely – hepatitis (with jaundice or without), liver failure, encephalopathy in patients with pre-existing disease. Violations withsides of the skin and subcutaneous tissues: infrequently – dermatitis, skin itching, skin rash, urticaria rarely – alopecia, photosensitivity reactions in the form of skin redness after UFO, multiform exudative erythema, toxic epidermal necrolysis, Stevens-Johnson syndrome. Musculoskeletal and connective tissue disorders: infrequently – fractures of the vertebrae, wrist bones, femoral heads associated with osteoporosis (see section “Special instructions”) are rare – arthralgia, myalgia, muscle weakness. Renal and urinary tract disorders: rarely – interstitial nephritis. Genital and breast disorders: rarely – gynecomastia. General disorders: infrequently – malaise rarely – excessive sweating, peripheral edema. In case of side effects, Not indicated in this manual, you should consult your doctor immediately. Drug Interaction Slows elimination of warfarin, diazepam, phenytoin. Overdose Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia. Treatment: symptomatic. Hemodialysis is not effective enough. Storage Conditions At a temperature not exceeding 25 ° C. Keep out of the reach and sight of children! Term hodnosty 3 years active substance Omeprazole
