Composition, form of production and packaging
Intestine-soluble hard gelatine capsules, opaque, size 3, with a yellow body, a light purple lid and a black marking "OMEZ 10" on the cap and capsule body; the contents of the capsules are granules from almost white to light yellow in color.
1 caps.
omeprazole 10 mg
Excipients: mannitol - 59 mg, crospovidone - 4.5 mg, poloxamer (407) - 1.25 mg, hypromellose (1828) - 2 mg, meglumine - 0.75 mg.
The composition of the coating: povidone K30 - 6.7 mg.
The composition of the enteric coating: a copolymer of methacrylic acid and ethyl acrylate [1: 1] (methacrylic acid copolymer [type C]) - 18 mg, triethyl acetate - 1.8 mg, magnesium stearate - 1 mg.
The composition of the body of the capsule: iron dye oxide yellow (E172), titanium dioxide (E171), sodium lauryl sulfate, water, gelatin.
The composition of the capsule capsule: dye of the capsule: blue color dye (E133), dye sunset yellow (E110), dye red enchanting (E129), dye floxin B (red D & C RED # 28 dye), titanium dioxide (E171), sodium lauryl sulfate, water, gelatin .
Composition of the black inscription on the capsules: ink S-1-8114: shellac (20% esterified) in ethanol, iron dye oxide black (E172), n-butanol, propylene glycol (E1520), indigo carmine dye (E132), dye red charming E129), dye quinoline yellow (E104), a brilliant blue dye (E133); Inks S-1-8115: shellac (20% esterified) in ethanol, iron dye oxide black (E172), ethanol, methanol, indigo carmine dye (E132), red enchanting dye (E129), quinoline yellow (E104) dye, blue (E133).
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
Intestine-soluble hard gelatine capsules, opaque, size No. 0, with a light purple body, yellow lid and black marking "OMEZ 40" on the cap and capsule body; the contents of the capsules are granules from almost white to light yellow in color.
1 caps.
omeprazole 40 mg
Excipients: mannitol - 236 mg, crospovidone - 18 mg, poloxamer (407) - 5 mg, hypromellose (1828) - 8 mg, meglumine - 3 mg.
The composition of the coating: povidone K30 - 26.8 mg.
The composition of the enteric coating: methacrylic acid-ethyl acrylate copolymer (1: 1) (methacrylic acid copolymer [type C]) 72 mg, triethyl acetate 7.2 mg, magnesium stearate 4 mg.
The composition of the capsule body: dye blue diamond (E133), dye sunset yellow (E110), dye red charming (E129), dye floxin B (dye red D & C RED # 28), titanium dioxide (E171), sodium lauryl sulfate, water, gelatin .
Composition of capsule capsule: iron oxide oxide yellow (E172), titanium dioxide (E171), sodium lauryl sulfate, water, gelatin.
Composition of the black inscription on the capsules: ink S-1-8114: shellac (20% esterified) in ethanol, iron dye oxide black (E172), n-butanol, propylene glycol (E1520), indigo carmine dye (E132), dye red charming E129), dye quinoline yellow (E104), a brilliant blue dye (E133); Inks S-1-8115: shellac (20% esterified) in ethanol, iron dye oxide black (E172), ethanol, methanol, indigo carmine dye (E132), red enchanting dye (E129), quinoline yellow (E104) dye, blue (E133).
7 pcs. - blisters (4) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Specific proton pump inhibitor: inhibits the activity of H + -K + -ATPase in parietal cells of the stomach, blocking the final stage of hydrochloric acid secretion, thereby reducing the production of hydrochloric acid.
Omeprazole is a prodrug and is activated in the acidic environment of secretory tubules of parietal cells of the stomach.
The effect is dose-dependent and provides an 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 after 2 hours. Inhibition of 50% of maximum secretion lasts 24 hours.
A single dose per 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 admission. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH above 3 for 17 hours.
PHARMACOKINETICS
Suction
Absorption is high, the time to reach Cmax is 0.5-3.5 hours. Bioavailability is 30-40%.
Distribution
Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach. Binding to plasma proteins (albumin and acid alpha-1-glycoprotein) is 90-95%.
Metabolism
It is practically completely metabolized in the liver with the participation of the cytochrome P450 (CYP) enzyme system, with the formation of 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc.). It is an inhibitor of the isoenzyme CYP2C19.
Excretion
T 1/2 is 0.5-1 h; 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
With hepatic insufficiency, bioavailability increases practically up to 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.
INDICATIONS
- 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);
- NSAIDs-gastropathy;
- eradication of Helicobacter pylori in infected patients with peptic ulcer of stomach and duodenum (as part of combination therapy);
- prevention of aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome).
DOSING MODE
Take inside, washed down with a small amount of water (the contents of the capsule can not be chewed), 30 minutes before meals or just before meals.
With exacerbation of gastric ulcer and duodenal ulcer, reflux-esophagitis and NSAID-gastropathy - 20 mg 2 times / day. The course of treatment for duodenal ulcer - 2-3 weeks, if necessary - 4-5 weeks; with gastric ulcer and reflux-esophagitis - 4-8 weeks.
In Zollinger-Ellison syndrome, the dose is selected individually depending on the initial level of gastric secretion, usually starting at 60 mg / day; if necessary, increase the dose to 80-120 mg / day (in this case, it is prescribed in 2-3 sessions).
For the prevention of Mendelssohn syndrome - 40 mg per hour before surgery.
For the prevention of recurrences of peptic ulcer of the stomach and duodenum - 10-20 mg 1 time / day.
Antrepid treatment of reflux esophagitis - 20 mg / day for a long period.
To eradicate Helicobacter pylori - 20 mg 2 times / day for 7-14 days (depending on the treatment regimen used) in combination with antibacterial agents.
In elderly patients, there is no need to adjust the dose.
SIDE EFFECT
The frequency of side effects is classified according to the incidence of the event: often (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01%, including individual reports).
On the part of the hematopoiesis system: very rarely - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.
From the digestive system: sometimes - diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; rarely - increased activity of liver enzymes, taste disorders; very rarely - dry mouth, stomatitis, in patients with a previous severe liver disease - hepatitis (including jaundice), a violation of liver function.
From the side of the 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: very rarely - arthralgia, myasthenia gravis, myalgia.
From the skin: rarely - skin rash and / or itching; in some cases - photosensitivity, multiform exudative erythema, alopecia.
Allergic reactions: often - hives; very rarely - 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).
CONTRAINDICATIONS
- childhood;
- Pregnancy;
- lactation period;
- Hypersensitivity to the drug.
With caution should prescribe the drug for kidney and / or liver failure.
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
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
Contraindications for children.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, there is no need to adjust the dose.
SPECIAL INSTRUCTIONS
Before the start of therapy, it is necessary to exclude the presence of a malignant process (especially with peptic ulcer disease), because treatment, masking symptoms, can delay the setting of the correct diagnosis.
Taking the drug simultaneously with food does not affect its effectiveness.
Impact on the ability to drive vehicles and manage mechanisms
The effects of omeprazole on driving and the use of other equipment are unlikely.
OVERDOSE
Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.
Treatment: symptomatic therapy, hemodialysis is not effective enough.
DRUG INTERACTION
Can reduce the absorption of esters of ampicillin, iron salts, itraconazole and ketoconazole (omeprazole increases the pH of the stomach).
Being inhibitors of cytochrome P450, it can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action (warfarin), phenytoin (drugs that are metabolized in the liver via the CYP 2C19 isoenzyme), 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 lead to a change in 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.
No interaction with concomitant antacids was noted.
TERMS OF RELEASE FROM PHARMACY
The drug is prescription
TERMS AND CONDITIONS OF STORAGE
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.
