Composition, form of production and packaging
Liofilizate for the preparation of a solution for infusions in the form of a homogeneous porous cake or parts thereof or in the form of a white or almost white powder.
omeprazole 40 mg
Excipients: sodium hydroxide - 5.28 mg, disodium edetate - 1 mg.
Vials of colorless glass (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
Antiulcer drug, a specific proton pump inhibitor. It inhibits the activity of H + -K + -ATPase in parietal cells of the stomach, blocking the final stage of hydrochloric acid secretion, thereby reducing acid production. Reduces basal and stimulated secretion irrespective of the nature of the stimulus.
Omeprazole is a prodrug and is activated in the acidic environment of secretory tubules of parietal cells of the stomach.
The antisecretory effect after taking in a dose of 20 mg occurs within the first hour, the maximum of action is after 2 hours. Inhibition of 50% of maximum secretion lasts 24 hours.
A single dose per day provides a rapid and effective suppression of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3 to 4 days after the end of admission.
In patients with duodenal ulcer, taking 20 mg of omeprazole maintains a pH in the stomach at level 3 for 17 hours.
Distribution and Metabolism
It binds to plasma proteins by 90-95% (albumin and acid alpha-glycoprotein).
It is practically completely metabolized in the liver with the participation of the cytochrome P450 enzyme system with the formation of 6 pharmacologically inactive metabolites (including hydroxyomeprazole, sulfide and sulfone derivatives). A significant part of the metabolism of omeprazole depends on the polymorphically expressed specific isoform CYP2C19 (S-mefenitoin hydroxylase), responsible for the formation of hydroxyomeprazole, the main plasma metabolite. It is an inhibitor of the isoenzyme CYP2C19.
T 1/2 for the final phase of AUC after intravenous administration of omeprazole is approximately 40 minutes (with hepatic insufficiency - 3 hours); the total plasma clearance is from 0.3 to 0.6 l / min. Changes in T 1/2 during treatment do not occur.
It is excreted in urine (70-80%) and with bile (20-30%).
Pharmacokinetics in special clinical cases
In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance.
In elderly patients excretion decreases, bioavailability increases.
- Stomach ulcer and duodenal ulcer (including the prevention of relapses);
- reflux esophagitis;
- hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis);
- prevention of aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome).
With severe exacerbation of peptic ulcer, reflux esophagitis and NSAIDs , patients who are not shown oral administration of the drug, the recommended daily dose of Omez В® is 40 mg for administration in the form of an IV infusion.
With Zollinger-Ellison syndrome, the drug is prescribed in an initial dose of 60 mg / day. The dose should be selected individually, it is possible to administer at higher doses (80-120 mg / day). If the daily dose is more than 60 mg, it should be divided into 2-3 infusions within 24 hours.
With Mendelssohn syndrome, the drug is prescribed for the night at a dose of 40 mg and at least 2 hours before anesthesia / surgery at a dose of 40 mg.
In elderly patients, there is no need to adjust the dose.
Rules for the preparation of an infusion solution
The solution for IV infusion is prepared immediately before use. To prepare a solution for IV infusion, use only 5% solution of dextrose (glucose) without preservatives. To dissolve 40 mg of lyophilized omeprazole powder, at least 5 ml of solvent is added to the vial and gently shaken until the lyophilizate is completely dissolved. A prepared solution containing 40 mg of omeprazole, before administration, is diluted in 100 ml of a 5% solution of dextrose (glucose) without preservatives for IV infusion for at least 30 minutes. Before the introduction, it should be ensured that there are no suspended particles in the solution. The chemical and physical stability of the prepared solution of omeprazole is observed for 6 hours after the dissolution of omeprazole in a 5% solution of dextrose (glucose).
On the part of the hematopoiesis system: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.
On the part of the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; rarely - increased activity of liver enzymes, taste disorders;in some cases - dry mouth, stomatitis, in patients with a previous severe liver disease - hepatitis (including jaundice), a violation of liver function.
From the side of the central nervous system: in patients with severe concomitant somatic diseases - dizziness, headache, agitation, depression; in patients with a previous severe liver disease - encephalopathy.
From the musculoskeletal system: in some cases - arthralgia, myasthenia gravis, myalgia.
Dermatological reactions: rarely - skin rash and / or itching; in some cases - photosensitivity, multiform exudative erythema, alopecia.
Allergic reactions: urticaria, angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock.
Other: rarely - gynecomastia, malaise, visual impairment, peripheral edema, increased sweating, the formation of gastric glandular cysts during long-term treatment (consequence of inhibition of hydrochloric acid secretion, is benign reversible).
- lactation period;
- Hypersensitivity to the drug.
With caution should prescribe the drug for kidney and / or liver failure.
PREGNANCY AND LACTATION
The use of Omez В® during pregnancy and lactation (breastfeeding) is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure.
APPLICATION FOR CHILDREN
Contraindicated in the appointment of children.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, there is no need to adjust the dose.
Before the start of therapy, it is necessary to exclude the presence of malignant process (especially with stomach ulcer), since treatment, masking the symptoms, can delay the setting of the correct diagnosis.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.
According to clinical studies with iv administration of omeprazole in a dose of up to 270 mg / day and in a dose of up to 650 mg for 3 days of dose-dependent side effects was not detected.
Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.
Treatment: symptomatic. Hemodialysis is not effective enough.
With simultaneous application of Omega В® can reduce the absorption of esters of ampicillin, iron salts, itraconazole and ketoconazole, t. omeprazole increases the pH of the stomach.
Being an inhibitor of cytochrome P450, omeprazole can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action (warfarin), phenytoin (drugs metabolized in the liver with CYP2C19), which in some cases may require a reduction in the doses of these drugs.
At the same time, long-term use of omeprazole at a dose of 20 mg 1 time / day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not change their plasma concentration.
Concentrations of omeprazole and clarithromycin in the blood plasma increase during the simultaneous oral administration of these drugs, while evidence of the interaction of omeprazole with metronidazole and amoxicillin is not revealed.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years.