Universal reference book for medicines
Name of the drug: OMEPRAZOL (OMEPRAZOL)

Active substance: omeprazole

Type: H + -K + -ATPase inhibitor.
Antiulcer drug
Manufacturer: SYNTHESIS (Russia)
Composition, form of production and packaging
Capsules
gelatinous, with a white casing and a yellow lid;
the contents of the capsules are ball-shaped micro-granules coated with a coating, white or white with a cream-colored hue.
1 caps.

omeprazole 20 mg

10 pieces.
- packings cellular planimetric (3) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

Omeprazole - antiulcer drug, inhibitor of the enzyme H + / K + -adenosine triphosphate (ATP) -phase.
It inhibits the activity of H + / K + -adenosine triphosphate (ATP phase (H + / K + -adenosine triphosphate (ATP) phase, it is also a "proton pump" or "proton pump") in 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 an active metabolite, sulfenamide, which inhibits the membrane H + / K + - adenosine triphosphate (ATP) phase, connecting with it through a 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.The 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 action of omeprazole begins 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 fast 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 liver failure increases almost to 100%), increases in elderly people and in patients with impaired liver function, failure of renal function has no effect. TC max is 0.5-3.5 hours.
Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach.
The connection with plasma proteins is 90-95% (albumin and acid alpha 1-glycoprotein).
T 1/2 - 0.5-1 h (with hepatic insufficiency - 3 h), clearance - 500-600 ml / min.
Almost completely metabolized in the liver with the participation of the enzyme system CYP2C19, with the formation of 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc.). It is an inhibitor of the isoenzyme CYP2C19. Kidney excretion (70-80%) and 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

- Stomach ulcer and duodenal ulcer (in the phase of exacerbation and anti-relapse treatment), incl.
Associated with Helicobacter pylori (as part of combination therapy);
- reflux esophagitis (including erosive).

- hypersecretory 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.

DOSING MODE

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 intake of NSAIDs - 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 caused by the intake of NSAIDs - within 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 for 2 more weeks.
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 divided doses).
For the prevention of recurrences of peptic ulcer - 10 mg once a day.

For the eradication of Helicobacter pylori , triple therapy is used (for 1 week: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg twice daily, omeprazole 20 mg, clarithromycin 250 mg, metronidazole 400 mg twice daily day, or omeprazole 40 mg once a day, amoxicillin 500 mg and metronidazole 400 mg - 3 times a day)

or "double" therapy (for 2 weeks: omeprazole 20-40 mg and amoxicillin 750 mg - 2 times 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).

For hepatic insufficiency appoint 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 functionand in elderly patients, correction of the dosing regimen is not required.
SIDE EFFECT

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

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

From the skin: rarely - skin rash and / or itching, in some cases photosensitization, multiforme 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).

CONTRAINDICATIONS

- childhood;

- Pregnancy;

- lactation period;

hypersensitivity.

With caution : renal and / or hepatic insufficiency.

PREGNANCY AND LACTATION

Contraindicated during pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution: kidney failure.
If the renal function is not corrected, the dosage regimen is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution: liver failure.
For hepatic insufficiency appoint 10-20 mg once a day (with severe liver failure, the daily dose should not exceed 20 mg);
APPLICATION FOR CHILDREN

Contraindicated in children.

APPLICATION IN ELDERLY PATIENTS

in elderly patients, correction of the dosing regimen is not required.

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.

OVERDOSE

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

Treatment: symptomatic.
Hemodialysis is not effective enough. There is no specific antidote.
DRUG 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, it can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin (drugs that are metabolized in the liver via cytochrome CYP2C19), 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.

TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

List B. 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.
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