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

Excipients: mannitol-39.6 mg, sucrose-63.7 mg, sodium hydrogen phosphate-3.0 mg, sodium lauryl sulfate-0.8 mg, lactose-7.9 mg, calcium carbonate-7.9 mg, hypromellose-20.4 mg, methacrylic acid and ethyl acrylate copolymer [1: 1] 30% dispersion [contains: sodium lauryl sulfate, polysorbate-80] - 58.2 mg, propylene glycol 1.9 mg, diethyl phthalate 5.8 mg, cetyl alcohol 1, 7 mg, sodium hydroxide 0.3 mg, polysorbate 80 mg 0.7 mg, povidone 0.6 mg, titanium dioxide E 171 0.4 mg, talc 0.1 mg;

capsules, hard gelatin - 63.0 mg:

body: titanium dioxide E 171 - 2.0 %, gelatin - up to 100%;

cap: titanium dioxide E 171 - 2.0%, dye quinoline yellow E 104 0.0249%, blue patented E 131 - 0.0285%, diamond black black E 151 0.0044%, gelatin up to 100 %.

Description:

Capsules № 2 of white color with a lid of green color. The contents of the capsules are ball-shaped micro pellets, coated with a white or almost white coating.

Pharmacotherapeutic group:Iron of the stomach secretion is a reducing agent - a proton pump inhibitor

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

Proton pump inhibitor, reduces acid production - inhibits the H + / K + -ATPase of parietal cells of the stomach and blocks the final stage of hydrochloric acid secretion.The drug is a prodrug and is activated in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa.

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

Pharmacokinetics:

Omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum concentration in the blood plasma is reached after 0.5-1 hour. Bioavailability is 30-40% (with liver failure increases almost to 100%), having a high lipophilicity, easily penetrates into the parietal cells of the stomach. At repeated reception bioavailability reaches 60-70% and depends on the accepted dose. The connection with plasma proteins is 90%. Omeprazole 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.

The half-life is 0.5-1 hour (with liver failure - 3 hours), the clearance is 500-600 ml / min. It is excreted mainly by the kidneys (70-80%), in the form of metabolites and with bile (20-30%). In chronic renal 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;

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

- prevention of aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome);

- ulcers and erosion of the stomach and duodenum caused by the use of non-steroidal anti-inflammatory drugs;

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

Contraindications:

- Pincreased sensitivity to the components that make up the drug;

- sugarase / isomaltase deficiency, fructose intolerance, lactose intolerance, lactase deficiency, glucose-galactose malabsorption (due to the presence of sucrose and lactose);

- children's age till 18 years;

- lactation period.

Carefully:

Renal and / or liver failure, diabetes (due to the presence of sugar in the drug).

Pregnancy and lactation:

The use of omeprazole in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

Omeprazole penetrates into breast milk. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside, squeezed a small amount of water (immediately before meals or during meals). Capsules are usually taken in the morning. Capsules can not be chewed.

With exacerbation of peptic ulcer, reflux-esophagitis, ulcers and erosions of the stomach and duodenum caused by the use of non-steroidal anti-inflammatory preparations, - 20 mg once a day. For patients with severe reflux esophagitis, the dose is increased to 40 mg once a day. The course of treatment for duodenal ulcer is 2-3 weeks, if necessary - 4-5 weeks; with peptic ulcer and esophagitis - 4-8 weeks. Patients who are resistant to treatment with other antiulcer drugs are prescribed 40 mg once a day. The course of treatment for peptic ulcer 12 weeks - 4 weeks, with peptic ulcer and reflux-esophagitis - 8 weeks. For the prevention of recurrences of peptic ulcer - 10 mg once a day.

With Zollinger-Ellison syndrome - 60 mg once a day; if necessary, increase the dose to 80-120 mg per day (in this case, it is prescribed in 2-3 sessions). Prophylaxis of Mendelssohn syndrome - 40 mg per hour before surgery (in case of an operation longer than 2 hours the necessary dose of the drug should be re-entered).

For eradication Helicobacter pylori use a three-component treatment regimen (within 1 week: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg - twice a day; or omeprazole 20 mg, clarithromycin 250 mg, metronidazole 400 mg - twice a day; or omeprazole 40 mg once a day, amoxicillin 500 mg and metronidazole 400 mg - 3 times a day) or a two-component treatment regimen (within 2 weeks: omeprazole 20-40 mg and amoxicillin 750 mg - twice a day; or omeprazole 40 mg - once a day and clarithromycin 500 mg - 3 times a day or amoxicillin 0,75-1,5 g - 2 times a day).

Side effects:

From the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence, increased activity of "liver" enzymes, taste disorders, dryness of the oral mucosa, stomatitis, in patients with a previous severe liver disease - hepatitis (including jaundice), violation function of the liver.

On the part of the organs of hematopoiesis: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

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

From the side of the musculoskeletal system: arthralgia, myasthenia gravis, myalgia.

From the skin: skin rash and / or itching, photosensitization, multiform exudative erythema, alopecia.

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

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

Overdose:

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

Treatment: conducting symptomatic therapy. There is no specific antidote.

Hemodialysis is not effective enough to remove omeprazole from the body due to the high degree of its binding to plasma proteins.

Interaction:

Can reduce the absorption of esters of ampicillin, iron salts, itraconazole and ketoconazole and other drugs (LC), the absorption of which depends on the pH value.

Being an inhibitor of cytochrome P450, omeprazole can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin (LC, which are metabolized in the liver by isoenzyme CYP2C19), that in some cases may require a reduction in the doses of these AC. At the same time, long-term use of omeprazole 20 mg once a day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol does not change their plasma concentration.

There was no clinically significant interaction of omeprazole with concomitant antacid preparations.

Increases the inhibitory effect on the hemopoietic system of other LC.

No interaction of omeprazole with concomitant antacids was noted. Concentrations of omeprazole and clarithromycin in plasma increase with the combined use of these drugs.

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 the effectiveness of the drug.

Patients with diabetes should pay attention to the sugar content of the drug.In one capsule of omeprazole contains 63.7 mg of sucrose (corresponding to 0.005 bread units (XE)).

Effect on the ability to drive transp. cf. and fur:

Considering possible side effects of the drug, care should be taken when driving vehicles or other potentially dangerous mechanisms.

Form release / dosage:

Capsules 20 mg.

Packaging:

For 7 or 10 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

2 contour packs of 7 capsules or 3 contour packs of 10 capsules together with instructions for use are placed in a pack of cardboard.

Storage conditions:

AT protected from light 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:P N002300 / 01

Date of registration:29.01.2009 / 18.03.2013

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Representation: & nbspVALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Information update date: & nbsp07.06.2017

Illustrated instructions

Instructions

Omeprazole (Omeprazole)