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

Auxiliary substances of pellets: calcium carbonate, potassium hydrogen phosphate (potassium phosphate disubstituted), hypromellose (hydroxypropylmethylcellulose), mannitol, sugar grits [sucrose, molasses starch] (sugar pellets), sugar syrup [sucrose, water], macrogol-6000 (polyethylene glycol-6000), povidone- K30 (polyvinylpyrrolidone-K30), sodium hydroxide, sodium lauryl sulfate, talc, titanium dioxide, polysorbate-80 (tween-80).

Pellet shell composition: methacrylic acid and ethyl acrylate copolymer (acrylic coating L30D).

The composition of the gelatin capsule: titanium dioxide, gelatin, dye quinoline yellow (yellow quinoline), dye sunset yellow (sunset yellow), methyl para- hydroxybenzoate (methylhydroxybenzoate), propyl parahydroxybenzoate (propylhydroxybenzoate), acetic acid.

Description:

Gelatin capsules No. 2 with a white casing, yellow lid. The contents of capsules are white or almost white pellets of spherical shape.

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

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

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

Omeprazole suppresses the basal and hydrochloric acid secretion stimulated by any stimulus at the final stage. Reduces the total volume of gastric secretion and inhibits the release of pepsin.Gastroprotective activity was detected in omeprazole, the mechanism of which is not clear. Does not affect the production of the internal factor of Castle and the rate of the transition of the food mass from the stomach to the duodenum. Omeprazole does not affect acetylcholine and histamine receptors.

Omeprazole capsules contain coated microgranules, gradual release and the onset of omeprazole starts through 1 hour after admission, reaches a maximum after 2 hours, persists for 24 hours or more. Inhibition of 50% of the maximum secretion after a single dose of 20 mg of the drug 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. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains a pH of 3 inside the stomach for 17 hours. After discontinuation of the drug secretory activity is completely restored after 3-5 days.

Pharmacokinetics:

Absorption is high. Bioavailability of 30-40 % (with hepatic insufficiency increases to almost 100 %), is increased in elderly people and in patients with impaired liver function, the failure of renal function has no effect. The time required to reach the maximum concentration (TC_mOh) - 0.5-3.5 hours. Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach. Connection with plasma proteins - 90-95 % (albumin and acid alpha-1 glycoprotein).

Half-life (T_1/2) - 0.5-1 hour (with hepatic insufficiency - 3 hours), clearance - 500-600 ml / min. Almost completely metabolized in the liver with the participation of the enzyme system CYP_2C19, with the formation of 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulphonic derivatives, etc.). Is an inhibitor of isoenzyme CYP_2C19. Kidney excretion (70-80 %) and with bile (20-30 %) in the form of metabolites.

In chronic renal failure, excretion decreases in proportion to a decrease in creatine clearance. In elderly patients excretion decreases.

Indications:

- Peptic ulcer of the stomach and duodenum (in the phase of exacerbation and anti-relapse treatment), incl. associated with Helicobacter pylori (as part of combination therapy);

- Reflux-esophagitis (including erosive).

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

- Gastropathy caused by the use of non-steroidal anti-inflammatory drugs.

Contraindications:

Hypersensitivity, child age, pregnancy, lactation.

Carefully:

Renal and / or hepatic insufficiency.

Dosing and Administration:

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

With exacerbation of peptic ulcer, reflux esophagitis and gastropathy caused by the use of non-steroidal anti-inflammatory drugs - 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 2-4 weeks, if necessary - 4-5 weeks; with gastric ulcer, with reflux-esophagitis, with erosive-ulcerative lesions of the gastrointestinal tract (GIT), caused by the use of non-steroidal anti-inflammatory drugs - for 4-8 weeks.

Reduction of symptoms of the disease and cicatrization of the ulcer in most cases occurs within 2 weeks. Patients who have not had complete cicatrization of the ulcer after a two-week course should continue treatment 2 of the week.

Patients who are resistant to treatment with other antiulcer drugs are prescribed 40 mg per day. The course of treatment for duodenal ulcer is 4 weeks, with peptic ulcer and reflux esophagitis - 8 weeks.

With Zollinger-Elisson syndrome - usually 60 mg once a day; if necessary, increase the dose to 80-120 mg / day (the dose is divided into 2 reception).

For the prevention of recurrences of peptic ulcer - 10 mg once a day.

For eradication Helicobacter pylori use "triple" therapy (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 "double" therapy (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).

In special situations. When liver failure is prescribed for 10-20 mg once a day (with severe liver failure, the daily dose should not exceed 20 mg); if there is a violation of kidney function and in elderly patients, correction of the dosing regimen is not required.

Side effects:

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

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

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

On the part of the hematopoiesis system: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

From the skin: rarely - skin rash and / or itching, in some cases photosensitization, multiform exudative erythema, alopecia.

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

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

Overdose:

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

Treatment: symptomatic. Hemodialysis is not effective enough.

There is no specific antidote. Treatment is symptomatic.

Interaction:

Can reduce the absorption of esters of ampicillin, iron salts, itraconazole and ketoconazole (omeprazole increases the pH of the stomach).

Being inhibitors of cytochrome P450, can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin (drugs that are metabolized in the liver via cytochrome CYP_2C19), which in some cases may require a reduction in the doses of these drugs.Can increase the concentration of clarithromycin in the blood plasma.

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 did not change their plasma concentration.

Increases the inhibitory effect on the hemopoietic system and other medicines.

No interaction with concomitant antacids was noted.

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 its effectiveness.

Form release / dosage:

Capsules 20 mg.

Packaging:

10 capsules per contour cell package.

3 contour squares, together with instructions for use, are placed in a pack of cardboard.

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:

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

Terms of leave from pharmacies:On prescription

Registration number:P N001520 / 01

Date of registration:14.08.2008

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp07.06.2017

Illustrated instructions

Instructions

Omeprazole (Omeprazol)