Lyophilisate for preparation of solution for infusion
Specific proton pump inhibitor: inhibits the activity of H + / K + -ATPase in the parietal cells of the stomach, blocking the final stage of the secretion of hydrochloric acid, thereby reducing acid production.
Reduces basal and stimulated secretion regardless of the nature of the stimulus.
Omeprazole is a prodrug and is activated in the acidic environment of the secretory tubules of the parietal cells of the stomach.
Exposure is dose-dependent and provides effective inhibition of both basal and stimulated acid secretion, regardless of the nature of the stimulating factor.
The antisecretory effect after taking 20 mg occurs within the first hour, a maximum of 2 hours. Inhibition of 50% of maximum secretion lasts 24 hours.
A single dose per day provides quick and effective inhibition of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end 3â4 days after the end of administration. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH of 3 for 17 hours.
During the use of drugs that reduce the secretion of the gastric glands, the concentration of gastrin in the blood plasma increases.
Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A
increases (see the section “Special Instructions”).
Communication with plasma proteins – 90-95% (albumin and acid alpha1-glycoprotein).
The elimination half-life (T1 / 2) for the final phase of the concentration-time pharmacokinetic curve in blood plasma after intravenous administration of omeprazole is about 40 minutes (with liver failure 3 hours), the total plasma clearance is from 0.3 to 0.6 l / min There is no change in the half-life during treatment.
Almost completely metabolized in the liver with the participation of the enzyme system of cytochrome P450 (CYP) with the formation of six pharmacologically inactive metabolites: hydroxyomeprazole, sulfide and sulfone derivatives, and others.
A significant part of omeprazole metabolism depends on the polymorphically expressed specific isoform of CYP2C19 (S-mephenytoin hydroxylase), which is responsible for the formation of hydroxyomeprazole, the main plasma metabolite. It is an inhibitor of the isoenzyme CYP2C19.
Excretion by the kidneys (70â80%) and with bile (20â30%). In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients, excretion decreases, bioavailability increases.
As an alternative to oral therapy if it is not possible:
for gastric and duodenal ulcer (including prevention of relapse)
for gastroesophageal reflux disease (GERD)
for hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, and for 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, p pticheskaya ulcer
to prevent aspiration of acidic stomach contents into the airway during general anesthesia (Mendelson’s syndrome).
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 formulation).
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, consult a doctor in the following cases:
in the presence of a previously diagnosed gastric ulcer of a serious liver disease, accompanied by hepatic 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 a dash of blood, discoloration of feces (tarry stool – melena), impaired swallowing
when the appearance of new symptoms or a change in existing symptoms from the gastrointestinal tract
while using one or more of these same drugs: clopidogrel, digoxin, ketoconazole, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampicin, Hypericum perforatum preparations (see “Interaction with other drugs.”).
Osteoporosis. Although a causal relationship with the use of omeprazole with fractures associated with osteoporosis has not been established, patients with a risk of developing osteoporosis or fractures against its background should be under appropriate clinical supervision.
Use during pregnancy and lactation
Use of the drug during pregnancy is only possible if the intended benefit to the mother outweighs the potential risk to the fetus.
During lactation, breast-feeding should be discontinued.
Each vial contains: Active ingredient:
omeprazole 40 mg.
Excipients: sodium hydroxide 5.28 mg,
disodium edetate 1.00 mg.
The frequency of adverse drug reactions is described in accordance with the following gradation: 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). Disorders of the skin and subcutaneous tissues: infrequently – dermatitis, skin itching, skin rash, urticaria rarely – alopecia, photosensitivity reactions, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Violations of the musculoskeletal and connective tissue: infrequently – fractures of the hip, bones of the wrist, vertebrae rarely – arthralgia, myalgia, muscle weakness. Disorders of the nervous system: often – headache infrequently – dizziness, paresthesia, drowsiness rarely – taste disturbance. Mental disorders: infrequently – insomnia rarely – increased irritability, aggressiveness, impaired consciousness, depression, hallucinations. Disorders of the gastrointestinal tract: often – abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting rarely – dry mouth, stomatitis, gastrointestinal candidiasis, microscopic colitis. Disorders from the liver and biliary tract: infrequently – increased activity of “liver” enzymes rarely – hepatitis with / without jaundice, liver failure, encephalopathy in patients with previous severe liver diseases. Disorders from the genitals and mammary gland: rarely – gynecomastia. Disorders from the blood and lymphatic system: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia. Immune system disorders: rarely – hypersensitivity reactions: fever, angioedema, anaphylactic reaction / anaphylactic shock. Disorders of the respiratory system, chest and mediastinal organs: rarely – bronchospasm. Disorders of the kidneys and urinary tract: rarely – interstitial nephritis. Hearing disorders and labyrinth disorders: infrequently – vertigo. Violations of the organ of vision: rarely – blurred vision. Metabolic and nutritional disorders: rarely – hyponatremia very rarely – hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia. General disorders: infrequently – malaise rarely – increased sweating, peripheral edema. Drug Interaction Long-term administration of omeprazole at a dose of 20 mg 1 time per day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, cyclosporidio blood. No interaction with concurrent antacids was noted. Changes the bioavailability of any drug, the absorption of which depends on the pH (eg, iron salts). Overdose Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia. Treatment: symptomatic. Hemodialysis is not effective enough. Storage conditions In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children! Expiration 2 years. Deystvuyuschee substance omeprazole Terms of delivery from pharmacies Prescription dosage form dosage form infusion solution