Omizac capsules enteric soluble 20mg, 30pcs

Composition

Each enteric capsule contains:

Active ingredient:  omeprazole (in the form of pellets coated with enteric coating) 20 mg.

Excipients included in omeprazole pellets:  mannitol, sucrose, sodium hydrophosphate, sodium lauryl sulfate, lactose monohydrate, calcium carbonate, hypromellose (E-15), propylene glycol, methacrylic acid and ethyl acrylate copolymer [1: 1], polysorbate-80, diethyl phthalate, sodium hydroxide, cetyl alcohol, corn starch.

Composition of an empty solid gelatin capsule: cap:  gelatin, purified water, methyl parahydroxybenzoate, propyl parahydroxybenzoate, diamond blue dye, iron oxide yellow dye, titanium dioxide, azorubin dye; body:  gelatin, purified water, methyl parahydroxybenzoate, propyl parahydroxybenzoate, titanium dioxide.

Composition of ink for marking the capsule shell: black ink: shellac, dehydrated alcohol, isopropanol, butanol, propylene glycol, iron oxide black dye (E 172), purified water; white ink: shellac, dehydrated alcohol, isopropanol, butanol, propylene glycol, titanium dioxide (E 171), polysorbate 80.

Pharmacological action

Pharmacotherapy group: Gastric glands secretion reducing agent-proton pump inhibitor ATH: A. 02. B. C. 01 Omeprazole Pharmacodynamics :

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

Omeprazole is a prodrug and is activated in the acidic environment of the secretory tubules of the parietal cells of the stomach.

The effect is dose-dependent and provides 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 of 2 hours. Inhibition of 50% of the maximum secretion lasts 24 hours. A single dose per day provides rapid and effective suppression of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3-4 days after the end of the intake. In patients with duodenal ulcer disease, taking 20 mg of omeprazole maintains an intragastric pH above 3 for 17 hours.

Pharmacokinetics:

Absorption – high, time to reach the maximum concentration (Tmax) – 0.5-3.5 hours, bioavailability – 30-40% (with hepatic insufficiency increases to almost 100%); having high lipophilicity, it easily penetrates the parietal cells of the stomach, binding to plasma proteins – 90-95% (albumin and acid alpha-1-glycoprotein). The half-life (T 1/2) is about 0.5-1 h (with hepatic insufficiency-3 h), the total plasma clearance is 500-600 ml / min. It is almost completely metabolized in the liver with the participation of the cytochrome P450 (CYP)enzyme system with the formation of six pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc. ). It is an inhibitor of the CYP2C19 isoenzyme. Excretion by the kidneys (70-80%) and with bile (20-30%). In chronic hepatic insufficiency, excretion decreases in proportion to the decrease in creatinine clearance. In elderly patients, excretion decreases, and bioavailability increases.

Indications

Peptic ulcer of the stomach and duodenum 12 (including 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 the stomach and duodenum 12 (as part of combination therapy).

Use during pregnancy and lactation

The use of omeprazole during pregnancy is possible only 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 drug.

Recommendations for use

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

Contraindications

Hypersensitivity to the drug, children’s age, lactation period.

With caution:

Renal and / or hepatic insufficiency.

Side effects

In rare cases, the following usually reversible adverse reactions may occur. The frequency of side effects is classified according to the frequency of occurrence 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 1/10000 and less than 1/1000, very rarely-less than 1/10000, including isolated cases. Within each frequency class, undesirable effects are presented in decreasing order of severity.

Blood and lymphatic system disorders:  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.

Nervous system disorders:  often – headache; infrequently-dizziness, paresthesia, drowsiness; rarely-taste disorders.

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 gastrointestinal mucosa,

Liver and biliary tract disorders:  infrequently-increased activity of “liver” enzymes; rarely-in patients with previous severe liver disease-hepatitis (including jaundice), very rarely – liver failure, including with the development of encephalopathy (in patients with a history of liver disease).

From the side of the skin:  infrequently-dermatitis, pruritus, rash, urticaria; rarely-alopecia, photosensitization; very rarely-erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Musculoskeletal disorders: rarely-arthralgia, myalgia; very rarely-muscle weakness.

Allergic reactions:  urticaria, angioedema, bronchospasm, interstitial nephritis, anaphylactic shock, fever.

Urogenital and systemic disorders:  rarely-interstitial nephritis.

From the genitals and breast: very rarely – gynecomastia.

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

Interaction

Due to a decrease in the acidity of gastric juice during treatment with omeprazole, the absorption of others may decrease or increase. medicinal products (LS), the mechanism of absorption of which depends on the pH of gastric juice. Reduces the absorption of ketoconazole and itraconazole. Increases digoxin absorption. The combined use of omeprazole at a dose of 20 mg once a day and digoxin increases the bioavailability of digoxin by about 10%. Omeprazole has been shown to interact with some antiretroviral drugs. The mechanisms and clinical significance of these interactions are not always known. An increase in pH in the stomach during omeprazole therapy may affect the absorption of antiretroviral drugs. Interaction at the level of the CYP2C19 isoenzyme is also possible. When omeprazole is co-administered with anti-retroviral drugs such as atazanavir and nelfinavir, there is a decrease in their serum concentrations. Therefore, co-use of omeprazole with antiretroviral drugs such as atazanavir and nelfinavir is not recommended. When omeprazole and saquinavir were co-administered, an increase in the concentration of saquinavir in the blood serum was noted. Omeprazole inhibits CYP2C19, the main isoenzyme involved in its metabolism. The combined use of omeprazole with other drugs that are metabolized by the SUR 2 C19 isoenzyme, such as diazepam, phenytoin, warfarin, other vitamin K antagonists, and cilostazol, may lead to a decrease in the metabolism of these drugs. It is recommended to monitor the concentration of phenytoin in plasma with simultaneous use of phenytoin and omeprazole; in some cases, it may be necessary to reduce the dose of phenytoin. At the same time, in patients taking phenytoin for a long time, the combined use of omeprazole at a dose of 20 mg once a day did not cause changes in the concentration of phenytoin in blood plasma. When using omeprazole in patients receiving warfarin or other vitamin K antagonists, it is necessary to monitor the international normalized ratio (INR); in some cases, it may be necessary to reduce the dose of warfarin or another vitamin K antagonist. At the same time, in patients taking warfarin for a long time, co-use of omeprazole at a dose of 20 mg once a day did not cause changes in clotting time. The use of omeprazole at a dose of 40 mg once a day led to an increase in Cmax and the area under the concentration-time curve (AUC) cilostazol increased by 18% and 26%, respectively; for one of the active metabolites of cilostazol, the increase was 29% and 69%, respectively.Co-use of omeprazole at a dose of 80 mg resulted in a decrease in the concentration of the active metabolite of clopidogrel in blood plasma and a decrease in its antiplatelet effect. Omeprazole does not affect the metabolism of drugs that are metabolized by the CYP3A4 isoenzyme, such as cyclosporine, lidocaine, quinidine, estradiol, erythromycin and budesonide. With the simultaneous use of omeprazole and tacroliamus, an increase in the concentration of tacrolimus in the blood serum was noted. The isoenzymes CYP2C19 and CYP3A4 are involved in the metabolism of omeprazole. Concomitant use of omeprazole and inhibitors of the CYP2C19 and CYP3A4 isoenzymes, such as clarithromycin and voricopazole, can lead to an increase in the concentration of omeprazole in blood plasma due to slowing down the metabolism of omeprazole. Concomitant use of voriconazole and omeprazole resulted in a more than twofold increase in the AUC of omeprazole, which, however, did not require a dose adjustment of omeprazole. Drugs that induce CYP2C19 and CYP3A4 isoenzymes, such as rifampicin and St. John’s wort preparations, when combined with omeprazole, can lead to a decrease in the concentration of omeprazole in blood plasma due to the acceleration of omeprazole metabolism.

How to take, course of use and dosage

Inside, drink a small amount of water (the contents of the capsule can not be chewed) before eating.

Duodenal ulcer in the acute phase – 20 mg per day for 2-4 weeks (in resistant cases up to 40 mg per day).

Gastric ulcer in the acute phase and erosive-ulcerative esophagitis – 20-40 mg per day for 4-8 weeks.

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

Eradication of Helicobacter pylori – 20 mg 2 times a day for 7 or 14 days (depending on the treatment regimen used) in combination with antibacterial agents.

To prevent relapses of peptic ulcer of the stomach and duodenum 12-20 mg per day.

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

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

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

Overdose

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

Special instructions

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

Taking it simultaneously with food does not affect its effectiveness.

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

Influence on the ability to drive vehicles and mechanisms: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 Omizac®, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of reach of children!

Shelf

life is 2 years. Do not use after the expiration date indicated on the package.

Active ingredient

Omeprazole

Conditions of release from pharmacies

By prescription

Dosage form

Capsules