Omizak - instructions for use, doses, side effects, contraindications

Each capsule contains: Active substance: omeprazole (in the form of pellets, coated with enteric coating) 20 mg; Excipients, included in the pellet omeprazole: Mannitol 50.41 mg, sucrose 67.87 mg, sodium dihydrogen phosphate 3.21 mg, sodium lauryl sulfate 0.67 mg, lactose 9.88 mg, calcium carbonate 9.88 mg, hypromellose (E-15) 21.00 mg, propylene glycol 0.99 mg, methacrylic acid (1-30 D) 49.41 mg, polysorbate (Tween 80) 0.44 mg, diethyl phthalate 1.98 mg, sodium hydroxide 0.44 mg, cetyl alcohol 0.99 mg, starch 9.88 mg.

Composition of empty hard gelatin capsule: body: methyl parahydroxybenzoate 0.64%, propyl parahydroxybenzoate 0.16%, titanium dioxide 1.98%, gelatin - up to 100 %. cap: methylparahydroxybenzoate 0.64 %, propyl parahydroxybenzoate 0.16%, iron oxide yellow 0.108%, carmosine (azorubin) 0.042%, brilliant blue 0.022%, titanium dioxide 2.1%; gelatin - up to 100%.

Description:

Hard gelatin capsule №2 with a gray lid and a white body with an inscription "OMIZAC" and a logo (square emblem) on the shell of a capsule containing pellets coated with an enteric coating, white or almost white.

Pharmacotherapeutic group:glands of the stomach secretion-lowering agent - proton pump inhibitor

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

Specific inhibitor of the proton pump: inhibits the activity of H + K + ATPase in parietal cells of the stomach, blocking the final stage of secretion of hydrochloric acid, thereby reducing acid production.

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 basal and stimulated acid secretion, regardless of the nature of the stimulus. The antisecretory effect after taking 20 mg occurs within the first hour, a maximum after 2 hours. Inhibition 50 % 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 admission. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH above 3 for 17 hours.

Pharmacokinetics:

Absorption is high, the time to reach the maximum concentration (Tmah) - 0.5-3.5 h, bioavailability - 30-40% (with hepatic insufficiency increases to almost 100%); possessing high lipophilicity, easily penetrates into the parietal cells of the stomach,association with plasma proteins - 90-95% (albumin and acid alpha-1 glycoprotein). The half-life period (T1 / 2) is about 0.5-1 hour (with liver failure - 3 hours), the total plasma clearance is 500-600 ml / min. Almost completely metabolized in the liver with the participation of the enzymatic system of cytochrome P450 (CYP) with the formation of six pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulphonic derivatives, etc.). Is an inhibitor of the isoenzyme CYP2C19. Kidney excretion (70-80%) and with bile (20-30%). In chronic liver failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion decreases, bioavailability increases.

Indications:

Peptic ulcer of stomach and duodenum (including prevention of relapses), Reflux-esophagitis

Hyper-secretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis),

NSAIDs-gastropathy,

Eradication Helicobacter pylori in infected patients with peptic ulcer and duodenal ulcer (as part of combination therapy).

Contraindications:

Hypersensitivity to the drug, children's age, lactation.

Carefully:

Renal and / or hepatic insufficiency.

Pregnancy and lactation:

The use of omeprazole during pregnancy is only possible if the expected therapeutic benefit 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 a little water (the contents of the capsule can not be chewed) before eating.

Peptic ulcer of duodenum in the phase of exacerbation - 20 mg per day for 2-4 weeks (in resistant cases, up to 40 mg per day).

Stomach ulcer in the phase of exacerbation and erosive-ulcerative esophagitis - 20-40 mg per day for 4-8 weeks.

Erosive-ulcerative lesions of the gastrointestinal tract caused with the intake of NSAIDs by 20 mg per day for 4-8 weeks.

Eradication Helicobacter pylori - 20 mg twice a day for 7 or 14 days (depending on the treatment regimen used) in combination with antibacterial agents.

For the prevention of recurrences of peptic ulcer of stomach and duodenum - 20mg day.

For the prevention of relapses of reflux esophagitis - 20 mg per day for a long time (up to 6 months). Reception on demand (symptomatic treatment).

Zollinger-Ellison Syndrome - the dose is selected individually depending on the initial level of gastric secretion, usually starting at 60 mg per day. If necessary, increase the dose to 80-120 mg per day, in this case it is divided into 2 divided doses.

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

Side effects:

In rare cases, the following, usually reversible, side reactions may occur. The frequency of side effects is classified according to the incidence of the case: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1 / 10,000 and less than 1/1000, very rarely - less than 1/10000, including isolated cases. Within each class of frequencies, undesirable effects are presented in order of decreasing severity.

From the side of the blood and lymphatic system: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis, pancytopenia.

Allergic reactions: rarely - hypersensitivity reactions, including fever, angioedema and anaphylactic reactions (including anaphylactic shock).

From the side of metabolism and nutrition: rarely - hyponatremia, very rarely - hypomagnesemia.

Mental disorders: infrequently - insomnia, rarely - agitation; confusion, depression; very rarely - aggression, hallucinations.

From the nervous system: often - headache; infrequently - dizziness, paresthesia, drowsiness; rarely - a taste disorder.

From the side of the organ of vision: rarely - blurred vision.

Hearing and balance disorders: infrequently - vertigo.

From the gastrointestinal tract: often - diarrhea or constipation, nausea, vomiting, flatulence, abdominal pain; rarely - dry mouth, stomatitis, candidiasis of the mucous membrane of the gastrointestinal tract,

Disorders from the liver and bile ducts: infrequently - increased activity of "hepatic" enzymes; rarely - in patients with a previous severe liver disease - hepatitis (including jaundice), very rarely - liver failure, incl. with the development of encephalopathy (in patients with a history of liver disease).

From the skin: infrequently - dermatitis, itching, rash, hives; rarely - alopecia, photosensitization; very rarely - multiforme exudative erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the side of the musculoskeletal system: rarely - arthralgia, myalgia; very rarely - muscle weakness.

Allergic reactions: urticaria, angioedema, bronchospasm,

interstitial nephritis, anaphylactic shock, fever.

From the genitourinary and system: rarely - interstitial nephritis From the genitals and breast: very rarely - gynecomastia.

Other: infrequently - malaise, peripheral edema; rarely - bronchospasm, increased sweating.

Overdose:

Symptoms: confusion, unclear vision, drowsiness, dryness of the oral mucosa, headache, nausea, tachycardia, arrhythmia. Treatment: symptomatic. Hemodialysis is not effective enough.

Interaction:

Due to a decrease in the acidity of gastric juice in the treatment with omeprazole, absorption of other drugs (LS) may decrease or increase, the absorption mechanism of which depends on the pH of the gastric juice.

Reduces the absorption of ketoconazole and itraconazole.

Increases absorption of digoxin. The combined use of omeprazole at a dose of 20 mg 1 time per day and digoxin increases the bioavailability of digoxin by about 10%.

It was shown that omeprazole interacts with some antiretroviral AC. The mechanisms and the clinical significance of these interactions are not always known. An increase in pH in the stomach with omeprazole therapy may affect the absorption of antiretroviral drugs. It is also possible to interact at the isoenzyme level CYP2C19. When combined with omeprazole and antiretroviral drugs, such as atazanavir and nelfinavir, there is a decrease in their concentration in the serum. In this regard, the joint use of omeprazole with antiretroviral drugs, such as atazanavir and nelfinavir, Not recommended.

With the simultaneous use of omeprazole and saquinavir, an increase in the concentration of saquinavir in serum was noted.

Omeprazole inhibits CYP2C19 is the basic isoenzyme involved in its metabolism. Joint use of omeprazole with other drugs, in the metabolism of which the isoenzyme СУР2С19, such as diazepam, phenytoin, warfarin, other antagonists of vitamin K, cilostazol, can lead to a decrease in the metabolism of these drugs.

It is recommended to control the concentration of phenytoin in the plasma with simultaneous application of phenytoin and omeprazole; in some casesit may be necessary to reduce the dose of phenytoin. At the same time, in patients with long-term phenytoin, the combined use of omeprazole at a dose of 20 mg 1 time per day did not cause a change in the concentration of phenytoin in the blood plasma.

When using omeprazole in patients receiving warfarin or other antagonists of vitamin K, control of the international normalized relationship (INR) is necessary; in some cases, it may be necessary to reduce the dose of warfarin or another, a vitamin K antagonist. At the same time, in patients taking long-term warfarin, the combined use of omeprazole at a dose of 20 mg 1 time per day did not cause a change in clotting time.

The use of omeprazole in a dose of 40 mg once a day led to an increase in stachia and area under the curve "concentration-time" (AUC) of cystostaxol by 18% and 26%, respectively; for one of the active metabolites of cilostazol, the increase was 29% and 69%, respectively.

Joint use of omeprazole at a dose of 80 mg led to a decrease in the concentration of the active metabolite clopidogrel in blood plasma and reduce its antiaggregant effect.

Omeprazole does not affect the metabolism of AC, metabolism of which is carried out with the help of isoenzyme CYP3A4, such as, ciclosporin, lidocaine, quinidine, estradiol, erythromycin and budesonide.

With the simultaneous use of omeprazole and tacrolimus, an increase in the concentration of tacrolimus in serum was noted.

In the metabolism of omeprazole, isozymes participate CYP2C19 and CYP3A4. The combined use of omeprazole and isozyme inhibitors CYP2C19 and CYP3A4, such as, clarithromycin and vorikopolazl, can lead to an increase in the concentration of omeprazole in the blood plasma due to a slowing of the metabolism of omeprazole. The combined use of voriconazole and omeprazole led to more than a twofold increase AUC omeprazole, which, however, did not require correction of the dose of omeprazole.

LC, inducing isoenzymes CYP2C19 and CYP3A4, such as, rifampicin and preparations of St. John's wort perfumed, when combined with omeprazole may lead to a decrease in the concentration of omeprazole in the blood plasma due to the acceleration of the metabolism of omeprazole.

Special instructions:

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

Admission simultaneously with food does not affect its effectiveness.

In special cases, if there are difficulties with swallowing a whole capsule, you can swallow its contents after opening or dissolving the capsule, and you can mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.

Effect on the ability to drive transp. cf. and fur:In normal dosages, the drug does not affect the speed of psychomotor reactions and concentration of attention. Due to the fact that dizziness and drowsiness may occur during treatment with Omizak®, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Capsules 20 mg.

Packaging:10 capsules in an aluminum foil blister. 3 or 5 blisters in a cardboard box together with instructions for use. Sample not for sale: 10 capsules in an aluminum foil blister. 1 blister with instructions for use in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012403 / 01

Date of registration:03.02.2012

The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

TORRENT PHARMACEUTICALS, Ltd. India

Representation: & nbspTORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India

Information update date: & nbsp03.02.2012

Illustrated instructions

Instructions

Omizak ® (Omizac)