Omeprazole - instructions for use, dose, side effects, contraindications

Auxiliary components, magnesium carbonate, giprolase (hydroxypropylcellulose), sodium hydrogen phosphate (disodium hydrogen phosphate), starch, talc, sucrose (sugar), inert spherical cores from starch and sugar, methacrylic acid and ethyl acrylate copolymer (1: 1) * (eudragit L 30 D), titanium dioxide, polysorbate - 80, macrogol (polyethylene glycol), silicon dioxide colloid, hypromellose (hydroxypropylmethylcellulose).

* - additionally contains sodium lauryl sulfate 0,7% and polysorbate - 80 2,3%.

Capsule composition: gelatin pharmaceutical, glycerol, methyl parahydroxybenzoate, propylparahydroxybenzoate, sodium lauryl sulfate, purified water.

Description:

Hard gelatin capsules number 1, body - white, cap - white. The contents of capsules are spherical granules of the correct form of white or almost white color.

Pharmacotherapeutic group:a means of reducing the secretion of the glands of the stomach - the proton pump inhibitor.

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

Omeprazole penetrates the parietal cells of the gastric mucosa, accumulates in them and is activated at an acidic pH.The active metabolite - sulfenamide inhibits the H +, K + - ATPase of the secretory membrane of parietal cells (proton pump), stops the release of hydrogen ions into the stomach cavity, and blocks the final stage of hydrochloric acid secretion. Dose-dependent decreases the level of basal and stimulated secretion, the total volume of gastric secretion and the release of pepsin. Effectively depresses both night and daytime acid production.

After a single dose of the drug occurs within 1 hour and persists for 24 hours or more, the maximum effect is achieved after 3 hours.

After discontinuation of the drug secretory activity is completely restored after 3-5 days.

Pharmacokinetics:

Absorption is high, the time to reach the maximum concentration (TCmah) - 0.5-3.5 h, bioavailability - 30-40% (with liver failure increases almost to 100%); possessing high lipophilicity, easily penetrates into the parietal cells of the stomach, the connection with plasma proteins - 90-95% (albumin and acid alpha-1-glycoprotein). The half-life (T1 / 2) is 0.5-1 h (with hepatic insufficiency - 3 h), the clearance is 500-600 ml / min. Almost completely metabolized in the liver with the participation of the enzyme system CYP2C19, with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulphonic derivatives and others), pharmacologically inactive. Is an inhibitor of isoenzyme CYP2C19. Kidney excretion (70-80%) and with bile (20-30%).

In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion slows down, bioavailability increases.

Indications:

Stomach ulcer and duodenal ulcer (treatment and prevention); NSAIDs - associated stomach and duodenal ulcer; peptic ulcer of the stomach and duodenum, associated with Helicobacter pylori; gastroesophageal reflux disease, reflux esophagitis, acid-dependent dyspepsia, hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis).

Contraindications:

Hypersensitivity to omeprazole, pregnancy, breast-feeding, children's age.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Inside, in the morning before a meal or during a meal, without chewing and washing down with a small amount of liquid.

With duodenal ulcer in the phase of exacerbation appoint 20 mg

1 once / day for 2-4 weeks. In resistant cases it is possible to increase the dose to 40 mg / day. With gastric ulcer in the acute phase and erosive-ulcerative esophagitis - 20-40 mg / day for 4-8 weeks.

For eradication Helicobacter pylori - 20 mg 2 times / day for 7 days in combination with antibacterial drugs.

For prevention of peptic ulcer disease peptic ulcer and duodenal ulcer is prescribed in a dose of 20 mg / day.

For prevention of exacerbation of reflux esophagitis - 20 mg / day for a long time (up to 6 months).

With erosive and ulcerative lesions of the gastrointestinal tract caused by the intake of NSAIDs - 20 mg / day. for 4-8 weeks.

In Zollinger-Ellison syndrome, the dose is selected individually depending on the initial level of gastric secretion, usually starting at 60 mg / day. If necessary, increase the dose to 80-120 mg / day in 2 divided doses.

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

Side effects:

On the part of the digestive system: nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, dry mouth, taste disorders, stomatitis, transient enhancement

activity of hepatic transaminases; patients with previous severe liver disease - hepatitis (including jaundice), a violation of liver function.

From the side of the central nervous system and the peripheral nervous system: headache, dizziness, agitation, drowsiness, insomnia, paresthesia, depression, hallucinations; in patients with severe concomitant somatic diseases, patients with previous severe liver disease - encephalopathy.

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

On the part of the hematopoiesis system: in some cases - leukopenia,

thrombocytopenia, agranulocytosis, pancytopenia.

Dermatological reactions: itching, in some cases - photosensitivity, erythema multiforme, alopecia.

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

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

Overdose:

Interaction:

Omeprazole can prolong the half-life and the duration of action of drugs metabolized in the liver by oxidation (warfarin, diazepam and etc.).

No interaction with propranolol or theophylline has been established, but interactions with other drugs, also metabolized by the enzyme system of cytochrome P450.

With simultaneous application with omeprazole, absorption of ketoconazole, ampicillin, and iron preparations may decrease.

When combined, the absorption of omeprazole and clarithromycin increases.

Special instructions:

For eradication Helicobacter pylori prescribe in combination with antibiotics, metronidazole, bismuth preparations and other medicines.

The diagnosis of reflux esophagitis should be confirmed endoscopically. Omeprazole for long-term treatment of reflux esophagitis should be used only in patients with a tendency to frequent relapses of the disease, as well as in those who have ineffective prevention of individual courses.

Before starting treatment, the drug should exclude the presence of a malignant tumor of the stomach, because the treatment can mask its symptoms and delay the establishment of the correct diagnosis.

Patients with severe impairment of liver function during treatment with omeprazole should regularly monitor the level of liver enzymes.

Form release / dosage:

Capsules 20 mg.

Packaging:10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil. 3 contour mesh packages with instructions for use are placed in a cardboard pack.

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:

2 of the year.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006469/09

Date of registration:13.08.2009

The owner of the registration certificate:LEKFARM, SOOO LEKFARM, SOOO Republic of Belarus

Manufacturer: & nbsp

LEKFARM, SOOO Republic of Belarus

Information update date: & nbsp15.02.2011

Illustrated instructions

Instructions

Omeprazole (Omeprazol)