Composition, form of production and packaging
Capsules are opaque, hard gelatinous, size 2, with a body of light pink color and a cap of a pinkish-brown color; the contents of capsules - pellets from white to almost white.
omeprazole 20 mg
Auxiliary substances: mannitol, sucrose, sodium lauryl sulfate, sodium hydrophosphate (disodium phosphate disubstituted), calcium carbonate, lactose, hypromellose (hydroxypropylmethylcellulose), methacrylic acid and ethyl acrylate copolymer (methacrylic acid copolymer L30D), propylene glycol, diethyl phthalate, cetyl alcohol, sodium hydroxide, polysorbate-80 (tween-80), povidone (polyvinylpyrrolidone), titanium dioxide, talc.
The composition of the body and capsule capsules: iron oxide red (E172), titanium dioxide (E171), methyl parahydroxybenzoate (methylhydroxybenzoate), propylparahydroxybenzoate (propylhydroxybenzoate), gelatin; or iron oxide red (E172), titanium dioxide (E171), gelatin.
7 pcs. - packings without cell contour (1) - packs cardboard.
7 pcs. - Packings without glue contour (2) - packs cardboard.
10 pieces. - packings without cell contour (1) - packs cardboard.
10 pieces. - Packings without glue contour (2) - packs cardboard.
10 pieces. - polymer cans (1) - packs of cardboard.
14 pcs. - polymer cans (1) - packs of cardboard.
28 pcs. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
Antiulcer drug, inhibitor of H + -K + -ATPase (proton pump). Omeprazole reduces acid production - inhibits the activity of H + -K + -ATPase in parietal cells of the stomach and blocks the final stage of synthesis of hydrochloric acid. The drug is a prodrug and is activated in the acidic environment of the secretory tubules of parietal cells.
Reduces the level of basal and stimulated secretion, regardless of the nature of the stimulus.
After taking the drug inside at a dose of 20 mg, the antisecretory effect develops within the first hour, a maximum after 2 hours. Inhibition of 50% of maximum secretion continues for 24 hours.
Taking the drug 1 time / day provides fast and effective suppression of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3-4 days after the end of the drug. In patients with duodenal ulcer, taking a drug at a dose of 20 mg maintains an intragastric pH at level 3 for 17 hours.
After taking the drug, omeprazole is rapidly absorbed from the digestive tract. Cmax in blood plasma is achieved after 0.5-3.5 hours. Bioavailability is 30-40%. At repeated reception bioavailability reaches 60-70% and depends on the accepted dose.
Binding to plasma proteins is 90-95% (albumin and acidic? 1- glycoprotein).
Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach.
Omeprazole is almost completely metabolized in the liver with the participation of the CYP2C19 isoenzyme with the formation of 6 pharmacologically inactive metabolites: hydroxyomeprazole, sulfide and sulfone derivatives. It is an inhibitor of the isoenzyme CYP2C19.
T 1/2 is 0.5-1 h. The clearance is 500-600 ml / min. It is excreted by the kidneys (70-80%) and with bile (20-30%).
Pharmacokinetics in special clinical cases
With hepatic failure, bioavailability increases to almost 100%, T 1/2 is 3 hours.
In chronic renal failure, excretion decreases in proportion to the decrease in QC.
In elderly patients excretion decreases, bioavailability increases.
- treatment of peptic ulcer of the stomach and duodenum;
- prevention of recurrences of peptic ulcer of the stomach and duodenum;
- reflux esophagitis;
- hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis);
- for the purpose of eradication of Helicobacter pylori in infected patients with peptic ulcer of the stomach and duodenum (as part of combination therapy).
The drug is taken orally, usually in the morning, the capsules are not chewed and washed down with a small amount of water (immediately before meals or during meals).
With duodenal ulcer in the phase of exacerbation, the drug is prescribed at a dose of 20 mg / day for 2-4 weeks, with insufficient effectiveness, the dose can be increased to 40 mg / day.
With gastric ulcer in the acute phase and erosive-ulcerative esophagitis - 20-40 mg / day for 4-8 weeks.
With erosive and ulcerative lesions of the gastrointestinal tract caused by the intake of NSAIDs - 20 mg / day for 4-8 weeks.
For the purpose of eradication, Helicobacter pylori is prescribed 20 mg twice a day for 7 days in combination with antibacterial agents.
For the prevention of recurrences of peptic ulcer of the stomach and duodenum - 20 mg / day.
For the prevention of relapses of reflux esophagitis - 20 mg / day for a long time (up to 6 months).
In Zollinger-Ellison syndrome, the dose is set individually depending on the initial level of gastric secretion, usually starting at 60 mg / day. If necessary, the dose is increased to 80-120 mg / day, in this case it is divided into 2 divided doses.
On the part of the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; rarely - increased activity of hepatic transaminases, taste disorders, the formation of gastric glandular cysts during long-term treatment (consequence of inhibition of the secretion of hydrochloric acid in the stomach, is benign, reversible); in some cases - dry mouth, stomatitis; in patients with a previous severe liver disease - hepatitis (including jaundice), a violation of liver function.
On the part of the hematopoiesis system: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.
From the central nervous system and peripheral 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, anaphylactic shock.
Other: rarely - gynecomastia, malaise, visual impairment, peripheral edema, increased sweating.
- lactation period (breastfeeding);
- Hypersensitivity to the drug.
Precautions should be taken with renal and / or liver failure.
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Caution should be used in patients with renal insufficiency.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should be used in patients with liver failure.
APPLICATION FOR CHILDREN
Contraindicated: children's age.
Before the beginning of treatment, it is necessary to exclude the presence of malignant process (especially with peptic ulcer), t. Gastrozole may mask symptoms and delay the diagnosis.
Taking the drug simultaneously with food does not affect its effectiveness.
Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.
Treatment: symptomatic therapy. Hemodialysis is not effective enough.
Gastrozole can reduce the absorption of esters of ampicillin, iron salts, itraconazole and ketoconazole, because omeprazole increases the pH of the stomach.
Being an inhibitor of cytochrome P 450 isoenzymes, omeprazole can increase the concentration in the blood plasma and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin (drugs metabolized in the liver with the participation of CYP2C19), which in some cases may require a reduction in the doses of these drugs.
With long-term use of omeprazole 20 mg once a day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranol, ethanolol, cyclosporine, quinidine and estradiol did not change their plasma concentration.
Gastrozol enhances the inhibitory effect on the hemopoietic system of other drugs.
No interaction of omeprazole with concomitant antacids was noted.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C. Shelf life - 3 years.