OPIZOL 20 [Omeprazole] 20 mg Capsules

instructions for the medical use of the medicinal product

OPIZOL-20

Tradename

Opizol-20, Опизол-20

International non-proprietary name or generic name

Omeprazole, Омепразол

Composition

Each capsule contains: Omeprazole 20 mg

Dosage form

Capsules.

Pharmacotherapeutic group

An agent that reduces the secretion of the glands of the stomach - a proton pump inhibitor.

Pharmacological properties

Pharmacodynamics

Omeprazole is an antiulcer drug, an inhibitor of the enzyme H + / K + -adenosine triphosphate (ATP) -phase. Inhibits the activity of H + / K + - adenosine triphosphate (ATPase (H + / K + -adenosine triphosphate (ATP) -phase, it is also a "proton pump" or "proton pump") in the parietal cells of the stomach, thereby blocking the transfer of ions hydrogen and the final stage of the synthesis of hydrochloric acid in the stomach.Omeprazole is a prodrug.In the acidic environment of the tubules of parietal cells, omeprazole is converted to the active metabolite sulfenamide, which inhibits the membrane H + / K + - adenosine triphosphate (ATP) -phase, connecting to it due to the disulfide bridge This explains the high selectivity of the action of omeprazole specifically on parietal cells, where there is a medium for the formation of sulfenamide.Biotransformation of omeprazole into sulfenamide occurs quickly (after 2-4 minutes).Sulfenamide is a cation and is not absorbed.

Omeprazole suppresses basal and stimulated by any stimulus secretion of hydrochloric acid at the final stage. Reduces the total volume of gastric secretion and inhibits the release of pepsin. It does not affect the production of the internal factor of Castle and the rate of transition of the food mass from the stomach to the duodenum. Omeprazole does not act on acetylcholine and histamine receptors.

After a single dose of the drug inside, the effect of omeprazole occurs within the first hour and lasts for 24 hours, the maximum effect is achieved after 2 hours. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH of 3.0 for 17 hours. After stopping the drug, secretory activity is fully restored after 3-5 days.

Pharmacokinetics

Absorption is high. Bioavailability of 30-40% (with liver failure increases to almost 100%), increases in the elderly and in patients with impaired liver function, renal failure has no effect. The time required to reach the maximum concentration (TCmax) is 0.5-3.5 hours. Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach. Communication with plasma proteins - 90-95% (albumin and acidic alpha1-glycoprotein).

The half-life (T1 / 2) is 0.5-1 hour (with liver failure - 3 hours), clearance - 500-600 ml / min. Almost completely metabolized in the liver with the participation of the CYP2C19 enzyme system, with the formation of 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulfonic derivatives, etc.). It is an inhibitor of the CYP2C19 isoenzyme. Excretion by the kidneys (70-80%) and bile (20-30%) in the form of metabolites.

Indications for use

• peptic ulcer of the stomach and duodenum;

• reflux esophagitis;

• erosive and ulcerative lesions of the stomach and duodenum associated with the use of NSAIDs, stress ulcers;

• erosive and ulcerative lesions of the stomach and duodenum associated with Helicobacter pylori (as part of complex therapy);

• Zollinger Ellison's syndrome.

Contraindications

• hypersensitivity;

• pregnancy;

• breast-feeding;

• children and adolescents up to 18 years of age.

Method of administration and dosage

Inside, capsules are usually taken in the morning, without chewing, with a small amount of water (just before meals).

Peptic ulcer of the duodenum in the acute phase - 1 capsule (20 mg) per day for 2-4 weeks (in resistant cases up to 2 capsules per day).

Gastric ulcer in the acute phase and erosive and ulcerative esophagitis - 1-2 capsules per day for 4-8 weeks.

Erosive and ulcerative lesions of the gastrointestinal tract caused by taking NSAIDs - 1 capsule per day for 4-8 weeks.

Eradication of Helicobacter pylori - 1 capsule 2 times a day for 7 days in combination with antibacterial agents.

Anti-relapse treatment of gastric ulcer and duodenal ulcer - 1 capsule per day.

Anti-relapse treatment of reflux esophagitis - 1 capsule per day for long-term treatment (up to 6 months).

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

Special instructions and precautions

Before using the drug, consult a doctor.

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

Taking it with food does not affect its effectiveness.

Be wary appoint in renal and / or hepatic insufficiency.

Interaction with other medicinal products

May reduce the absorption of ampicillin esters, 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, indirect anticoagulants, phenytoin (drugs that are metabolized in the liver by cytochrome CYP2C19), which in some cases may require a reduction in doses of these drugs. May increase plasma concentrations of clarithromycin.

Enhances the inhibitory effect on the hematopoietic system and other drugs.

Side effect

From the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; in rare cases - increased activity of liver enzymes, taste disturbances, in some cases - dry mouth, stomatitis, in patients with previous severe liver disease - hepatitis (including jaundice), impaired liver function.

From the nervous system: in patients with severe concomitant somatic diseases - headache, dizziness, agitation, depression, in patients with previous severe liver disease - encephalopathy.

From the musculoskeletal system: in some cases - arthralgia, myasthenia gravis, myalgia.

From the hematopoietic system: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

On the part of the skin: rarely - skin rash and / or itching, in some cases photosensitivity, erythema multiforme exudative, alopecia.

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

Other: rarely - visual disturbances, malaise, peripheral edema, increased sweating, gynecomastia, the formation of gastric glandular cysts during long-term treatment (a consequence of inhibition of hydrochloric acid secretion, is benign, reversible).

If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: confusion, blurred vision, drowsiness, dry mouth, nausea, vomiting, tachycardia, arrhythmia, headache.

Treatment: symptomatic. There is no specific antidote.

Storage conditions

Store in a cool and dry place, at a temperature not exceeding 25°C.

Keep out of the reach of children!

Shelf life

3 years. Do not use after the expiry date stated on the packaging.

Vacation conditions

Dispensed by prescription.

Release form

10 capsules in an aluminum foil blister. 3 blisters with instructions for use in a cardboard box.