Active substanceOmeprazoleOmeprazole
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  • Dosage form: & nbspenteric-coated capsules
    Composition:

    : 1 capsule contains

    active substance: pellets of omeprazole - 233 mg, in terms of omeprazole - 20 mg; Excipients: mannitol - 39.61 mg, sucrose - 63.5 mg, sodium hydrogen phosphate

    - 2.96 mg, sodium lauryl sulfate 0.79 mg, lactose 7.9 mg, calcium carbonate 7.9 mg, hypromellose hydroxypropyl methyl cellulose 20.39 mg, methacrylic acid and ethyl acrylate copolymer [1: 1] 58 , 25 mg, propylene glycol 1.9 mg, diethyl phthalate 5.83 mg, cetyl alcohol 1.75 mg, sodium hydroxide 0.35 mg, polysorbate 80 (twin 80) 0.7 mg, povidone (polyvinylpyrrolidone) 0 , 61 mg, titanium dioxide 0.42 mg, talc 0.14 mg; hard gelatin capsules No. 1: gelatin, titanium dioxide, dye sunset yellow [E 110].

    Description:

    hard gelatin capsules number 1 orange. Contents of capsules - white or white with a creamy shade of color spherical pellets.

    Pharmacotherapeutic group:a drug that reduces the secretion of the glands of the stomach - the proton pump inhibitor
    ATX: & nbsp

    A.02.B.C.01   Omeprazole

    Pharmacodynamics:

    Omeprazole inhibits the enzyme H * / K+-AT Phase ("proton pump") in parietal cells of the stomach and thereby blocks the final stage of synthesis of hydrochloric acid.This leads to a decrease in basal and stimulated secretion, independently


    from nature stimulus. After a single dose of the drug inside the action

    omeprazole occurs within the first hour and lasts for 24 hours, the maximum effect is achieved through 2 h. One-time reception per day provides a fast and

    effective suppression of day and night gastric secretion, reaching its maximum against the background of course treatment after 4 days. After discontinuation of the drug, the secretory activity is completely restored after 3-5 days. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH at 3.0 for 17 hours. With the withdrawal of the drug, there is no "ricochet" syndrome.
    Pharmacokinetics:

    Omeprazole is rapidly absorbed from the gastrointestinal tract (GIT), the maximum concentration in the plasma is achieved after 0.5-3.5 hours. The rate of absorption is not dependent on food intake. Bioavailability is 30-40% (in patients with chronic liver diseases, the bioavailability of the drug is increased to 100%). Binding with

    plasma proteins - 90-95 %. The half-life of plasma is 0.5-1 h and does not change with prolonged admission (for liver failure - 3 h).

    Omeprazole is almost completely metabolized in the liver with the participation of the enzyme system of cytochromes CYP2C19 and CYP3A4 with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulphonic derivatives, etc.), pharmacologically inactive. It is excreted mainly by the kidneys (70-80%) and bile (20-30%) in the form of metabolites. In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion decreases, bioavailability increases.

    Indications:

    Peptic ulcer of the stomach and duodenum (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).

    Gastropathy associated with the use of non-steroidal anti-inflammatory drugs (NSAIDs).

    Eradication Helicobacter pylori in infected patients with peptic ulcer of the stomach and duodenum (as part of a combination therapy).

    Contraindications:Hypersensitivity to the drug, children's age; lactase deficiency, sugarase / isomaltase deficiency, lactose intolerance, fructose intolerance, glucose galactose malabsorption (the preparation contains lactose and sucrose); simultaneous use with atazanavir and nelfinavir.
    Pregnancy and lactation:

    The drug is contraindicated in pregnancy, except when the intended benefit to the mother exceeds the potential risk to the fetus.

    During lactation it is necessary to decide whether to stop breastfeeding or stop taking the medication.

    Dosing and Administration:

    Inside, squeezed with a small amount of water, (the contents of the capsule can not be chewed), it is recommended to take it in the morning on an empty stomach or immediately before eating (reception with food is possible).

    Peptic ulcer of duodenum in the phase of exacerbation - 1 capsule (20 mg) once a day for 2-4 weeks.

    Stomach ulcer in the phase of exacerbation and erosive-ulcerative esophagitis - 1 capsule per day for 4-8 weeks. For patients with severe reflux esophagitis, the dose is increased to 2 capsules 1 time per day.

    Erosive-ulcerative lesions of the gastrointestinal tract caused by the intake of NSAIDs

    - 1 capsule per day for 4 weeks.

    Duodenal ulcer, peptic ulcer disease - 1 capsule per day for 4 weeks.

    Eradication Helicobacter pylori - a three-component treatment regimen for 1 week (omeprazole 20 mg, amoxicillin 1 g and clarithromycin 500 mg twice a day; or omeprazole 20 mg, metronidazole 400 mg and clarithromycin 250 mg twice a day; or omeprazole 40 mg once a day, amoxicillin 500 mg and metronidazole 400 mg three times a day); a two-component treatment regimen for 2 weeks (omeprazole 20-40 mg and amoxicillin 750 mg - 1 g twice daily; or, omeprazole 40 mg once a day and clarithromycin 500 mg three times a day).

    Anti-relapse treatment of peptic ulcer of the stomach and duodenum - 1 capsule per day.

    Contraceptive treatment reflux esophagitis 1 capsule per day for

    long time (safety and efficacy of maintenance therapy for 12 months have been proven).

    Syndrome Zolliiger-Ellison - the dose is selected individually depending on the initial level of gastric secretion, usually starting from 60 mg once a day. If necessary, the dose is increased to 80-120 mg / day, in this case it is divided into 2 divided doses.Treatment is continued according to clinical indications (long-term administration is possible - up to 5 years).

    Acid-dependent dyspepsia - 1 capsule 1 time per day for 2-4 weeks.

    Prevention of Mendelssohn syndrome - 2 capsules 1 hour before the operation (in case of an operation longer than 2 hours the necessary dose of the drug should be re-entered).

    In patients with severe hepatic insufficiency, the daily dose should not exceed 20 mg.

    Patients with impaired renal function are not required to adjust the dose.

    Older patients are not required to adjust the dose.

    Side effects:

    Classification of unwanted adverse reactions according to the frequency of development: often - 1-10%, not often-0.1-1%, rarely-0.01 -0.1%.

    From the digestive system: often - diarrhea, constipation, abdominal pain, nausea, vomiting, flatulence; not often - a transient increase in the activity of "liver" enzymes; rarely - taste disorders, dryness of the oral mucosa, stomatitis, lack of appetite, in patients with a previous severe liver disease - hepatitis (including jaundice), liver dysfunction, candidiasis of the gastrointestinal tract, the formation of gastric glandular cysts during long-term treatment (the consequence of inhibiting the secretion of hydrochloric acid, is benign, reversible).

    From the central and peripheral nervous system: often - headache; not often - dizziness, paresthesia, drowsiness, insomnia; rarely - reversible confusion, agitation, aggressiveness, depression and hallucinations (mainly in patients with severe concomitant somatic diseases), in patients with a previous severe liver disease - encephalopathy.

    From the musculoskeletal system: rarely - muscle weakness, myalgia, arthralgia.

    From the side - bodies hematopoiesis: rarely - leukopenia, thrombocytopenia;

    agranulocytosis, pancytopenia.

    From the skin: not often - skin rash and / or itching, rarely - photosensitization, multiforme exudative erythema, Stevens-Johnson syndrome, alopecia, toxic epidermal necrolysis.

    Allergic reactions: not often - hives, rarely - angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock.

    From the genitourinary system: rarely - hematuria, proteinuria, urinary tract infection.

    From the endocrine system: rarely - gynecomastia.

    Other: not often - malaise, rarely - visual impairment, peripheral edema, increased sweating, hyponatremia.

    Overdose:

    Symptoms: confusion, unclear vision, drowsiness, dryness of the oral mucosa, headache, agitation, increased sweating, nausea, tachycardia, arrhythmia.

    There is no specific antidote. Treatment is symptomatic (gastric lavage, taking activated charcoal). Hemodialysis is not effective enough.

    Interaction:

    Omeprazole slows the metabolism of drugs metabolized by enzymes of the cytochrome P450 system. It can increase the concentration in the blood plasma of diazepam, carbamazepine, nifedipine, aminophenazone, phenytoin, warfarin, which in some cases may require a reduction in the doses of these drugs. Increases the level of tacrolimus in the blood.

    Omeprazole in a dose of 80 mg reduces the effectiveness of clopidogrel (reduces the concentration of the active metabolite of clopidogrel in the blood plasma).

    Strengthens the action of coumarins and diphenine.

    With simultaneous use, the concentration of both clarithromycin and omeprazole in the blood plasma can increase.

    Long-term use of omeprazole 20 mg once daily in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, amoxicillin, metoprolol, propranolol, ethanol cyclosporine, lidocaine, quinidine and estradiol did not change their plasma concentration.

    No interaction with concomitant antacids was noted.


    Changes the bioavailability of any drug, the absorption of which depends on the pH value (slows the absorption of ampicillin, itraconazole, ketoconazole, iron salts). Simultaneous reception with atazanavir leads to a decrease in the area under the pharmacokinetic curve "concentration-time" atazanavir by 76%, the maximum concentration of the drug in the blood - by 72%, the minimum concentration - by 79%.

    Special instructions:

    Before the start of therapy, it is necessary to exclude the presence of a malignant process (especially with gastric ulcer), since treatment, masking the symptoms, can delay the setting of the correct diagnosis.

    Admission simultaneously with food is not affected by its effectiveness.

    If there are difficulties with swallowing the whole capsule, you can swallow its contents after opening or dissolving the capsule,and it is also possible to mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.

    When prescribing a drug for patients with diabetes mellitus, it should be borne in mind that in

    Each capsule contains 63.5 mg sucrose.
    Effect on the ability to drive transp. cf. and fur:

    The drug should be used with caution by persons who operate vehicles or other mechanisms, which is associated with a risk of side effects from the nervous system.

    Form release / dosage:

    Capsules enteric in solution 20 mg.


    Packaging:

    10 capsules in a contour cell box made of polyvinylchloride film and aluminum foil.

    1,2, 3, 5, 8 or 10 contour mesh packages together with instructions for use in a pack of cardboard.

    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:3 years.
    Do not use after expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N002483 / 01
    Date of registration:25.04.2008
    The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia
    Manufacturer: & nbsp
    Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia
    Information update date: & nbsp25.03.2013
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