Omisak, 20 mg 30 pcs.

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Indications

Peptic ulcer of the stomach and duodenum (including prevention of relapses),

Reflux esophagitis,

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

NSAID gastropathy,

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

Pharmacological effect

Pharmacotherapeutic group: Gastric gland secretion reducing agent – proton pump inhibitor

ATC: 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, maximum after 2 hours. Inhibition of 50% of maximum secretion continues for 24 hours. A single dose per day provides rapid and effective inhibition of daytime and nighttime gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3-4 days after the end of administration. In patients with duodenal ulcer, 20 mg omeprazole maintains intragastric pH above 3 for 17 hours.

Pharmacokinetics:

Absorption is high, time to reach maximum concentration (Tmax) is 0.5-3.5 hours, bioavailability is 30-40% (with liver failure it increases to almost 100%); Possessing high lipophilicity, it easily penetrates the parietal cells of the stomach, the connection with plasma proteins is 90-95% (albumin and acidic alpha1-glycoprotein). The half-life (T1/2) is about 0.5-1 hour (with liver failure – 3 hours), total plasma clearance is 500-600 ml/min. 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 bile (20-30%). In chronic liver failure, excretion decreases in proportion to the decrease in creatinine clearance. In elderly patients, excretion decreases and bioavailability increases.

Special instructions

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

Taking it 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 dissolving the capsule, and you can also mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes.

Impact on the ability to drive vehicles. Wed and fur.:

In normal dosages, the drug does not affect the speed of psychomotor reactions and concentration. 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 that require increased concentration and speed of psychomotor reactions.

Active ingredient

Omeprazole

Composition

Each enteric capsule contains:

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

Excipients included in omeprazole pellets: mannitol, sucrose, sodium hydrogen phosphate, 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, starch corn.

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

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

Pregnancy

The use of omeprazole during pregnancy is possible only in cases where the expected therapeutic benefit outweighs the potential risk to the fetus.

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

Contraindications

Hypersensitivity to the drug, childhood, lactation period.

With caution:

Renal and/or liver failure.

Side Effects

In rare cases, the following, usually reversible, side effects may occur. The frequency of side effects is classified depending on 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, adverse effects are presented in decreasing order of severity.

From 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).

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 – taste disturbance.

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

Disorders of the organ of hearing and balance: infrequently – vertigo.

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

Disorders of the liver and biliary tract: infrequently – increased activity of liver enzymes; rarely – in patients with 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, urticaria; rarely – alopecia, photosensitivity; very rarely – exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the musculoskeletal system: rarely – arthralgia, myalgia; very rarely – muscle weakness.

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

From the genitourinary system: rarely – interstitial nephritis.

From the genital organs and mammary gland: very rarely – gynecomastia.

Other: 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 other drugs (drugs), the mechanism of absorption of which depends on the pH of the gastric juice, may decrease or increase.

Reduces the absorption of ketoconazole and itraconazole.

Increases the 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 approximately 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 gastric pH during omeprazole therapy may affect the absorption of antiretroviral drugs. Interaction at the level of the CYP2C19 isoenzyme is also possible. With the combined use of omeprazole and antiretroviral drugs, such as atazanavir and nelfinavir, a decrease in their serum concentrations is observed. In this regard, the combined use of omeprazole with antiretroviral drugs such as atazanavir and nelfinavir is not recommended.

When omeprazole and saquinavir were administered concomitantly, an increase in saquinavir serum concentrations was observed.
Omeprazole inhibits CYP2C19, the main isoenzyme involved in its metabolism. The combined use of omeprazole with other drugs in the metabolism of which the CYP2C19 isoenzyme is involved, such as diazepam, phenytoin, warfarin, other vitamin K antagonists, cilostazol, can lead to a decrease in the metabolism of these drugs.

It is recommended to monitor plasma phenytoin concentrations during concomitant 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 1 time per day did not cause changes in the concentration of phenytoin in the blood plasma.

When using omeprazole in patients receiving warfarin or other vitamin K antagonists, monitoring of the international normalized ratio (INR) is necessary; 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, 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 at a dose of 40 mg 1 time per day led to an increase in Cmax and area under the concentration-time curve (AUC) of cilostazol by 18% and 26%, respectively; for one of the active metabolites of cilostazol, the increase was 29% and 69%, respectively.

The combined use of omeprazole at a dose of 80 mg led to a decrease in the concentration of the active metabolite of clopidogrel in the blood plasma and a decrease in its antiplatelet effect.

Omeprazole does not affect the metabolism of drugs whose metabolism is carried out using 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. The combined use of omeprazole and inhibitors of the CYP2C19 and CYP3A4 isoenzymes, such as clarithromycin and voripazole, may lead to an increase in the concentration of omeprazole in the blood plasma by slowing down the metabolism of omeprazole. The combined use of voriconazole and omeprazole led to a more than twofold increase in the AUC of omeprazole, which, however, did not require dose adjustment of omeprazole.

Drugs that induce the isoenzymes CYP2C19 and CYP3A4, such as rifampicin and St. John’s wort preparations, when used together with omeprazole, can lead to a decrease in the concentration of omeprazole in the blood plasma by accelerating the metabolism of omeprazole.

Overdose

Symptoms: confusion, blurred vision, drowsiness, dry oral mucosa, headache, nausea, tachycardia, arrhythmia.

Treatment: symptomatic. Hemodialysis is not effective enough.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

2 years. Do not use after the expiration date stated on the package.

Manufacturer

Torrent Pharmaceuticals Ltd, India