Omeprazole-OBL, 20mg capsules 28pcs

Composition

Active ingredient

Omeprazole – 20 mg.

Auxiliary substances of pellets:

calcium carbonate,

potassium phosphate di-substituted;

hydroxypropylmethylcellulose (hypromellose);

mannitol;

sugar pellets (sucrose);

sugar syrup (sucrose);

polyethylene glycol 6000;

polyvinylpyrolidone K-30;

sodium hydroxide;

sodium lauryl sulfate;

talc;

titanium dioxide;

tween 80.

Composition of the pellet wrapper:  

L30D acrylic coating

Composition of gelatin capsule:

azorubin,

gelatin,

methylparahydroxybenzonate,

propylparahydroxybenzoate,

acetic acid.

Pharmacological action

Pharmacotherapy group:

 Anti-ulcer agent, proton pump inhibitor.

Pharmaceutical action:

Proton pump inhibitor, reduces acid production-inhibits the activity of H+ / K+ – ATPASE in the parietal cells of the stomach and thereby blocks the final stage of HCl secretion. The drug is a prodrug and is activated in the acidic environment of the secretory tubules of parietal cells.

Reduces basal and stimulated secretion regardless of the nature of the stimulus. The antisecretory effect after taking 20 mg occurs within the first hour, maximum – after 2 hours.

Inhibition of 50% of the maximum secretion 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 and disappearing by the end of 3-4 days after the end of the intake.

In patients with duodenal ulcer disease, taking 20 mg of omeprazole keeps the intragastric pH at 3 for 17 hours.

Pharmacokinetics:

Absorption – high, TCmax-0.5-3.5 h, bioavailability-30-40% (with hepatic insufficiency increases to almost 100%); with high lipophilicity, it easily penetrates the parietal cells of the stomach, binding to plasma proteins-90-95% (albumin and acid alpha-1-glycoprotein). T1/2 – 0.5-1 h (in case of hepatic insufficiency-3 h), clearance – 500-600 ml/min.

It is almost completely metabolized in the liver with the participation of the CYP2C19 enzyme system, with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc. ), pharmacologically inactive.

It is an inhibitor of the CYP2C19 isoenzyme.

Excretion by the kidneys (70-80%) and with bile (20-30%). In CRF, excretion decreases in proportion to the decrease in creatinine clearance.

In elderly patients, excretion decreases, and bioavailability increases.

Indications

Peptic ulcer of the stomach and duodenum (including prevention of relapses), reflux esophagitis, hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis);

NSAIDs-gastropathy. Eradication of Helicobacter pylori in infected patients with peptic ulcer of the stomach and duodenum 12 (as part of combination therapy).

Contraindications

Hypersensitivity, childhood, pregnancy, lactation.

With caution.

Renal and / or hepatic insufficiency.

Side effects

From 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 previous severe liver disease-hepatitis (including jaundice), impaired liver function.

From the hematopoietic organs: in some cases – leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

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

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

From the skin: rarely-skin rash and / or pruritus, in some cases – photosensitization, erythema multiforme, alopecia.

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

Other: rarely-gynecomastia, malaise, visual disturbances, peripheral edema, increased sweating, formation of gastric glandular cysts during long-term treatment (due to inhibition of HCl secretion, is benign, reversible).

Overdose.

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

Treatment: symptomatic. Hemodialysis is not effective enough.

Interaction

It can reduce the absorption of ampicillin esters, Fe salts, itraconazole and ketoconazole (omeprazole increases the pH of the stomach).

Taking cytochrome P450 inhibitors may increase the concentration and decrease the excretion of diazepam, indirect anticoagulants, and phenytoin (drugs that are metabolized in the liver by cytochrome CYP2C19), which in some cases may require a reduction in the doses of these drugs.

At the same time, long-term use of omeprazole at a dose of 20 mg once a day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not lead to a change in their plasma concentrations. Enhances the inhibitory effect on the hematopoietic system of other drugs.

There was no interaction with concomitant antacids.

How to take, course of use and dosage

Inside, capsules are usually taken in the morning, capsules should not

be chewed with a small amount of water (just before meals or during meals). In case of exacerbation of peptic ulcer disease, reflux esophagitis and NSAID gastropathy-20 mg once a day. In 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; for gastric ulcer and esophagitis-4-8 weeks. Patients who are resistant to treatment, etc. anti-ulcer drugs are prescribed at 40 mg/day. The course of treatment for duodenal ulcer is 4 weeks, for gastric ulcer and reflux esophagitis-8 weeks.

With Zollinger-Ellison syndrome – 60 mg; if necessary, the dose is increased to 80-120 mg/day (in this case, it is prescribed in 2-3 doses). For the prevention of peptic ulcer relapses – 10 mg 1 time a day.

For eradication of Helicobacter pylori, “triple” therapy is used (for 1 week: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg – 2 times a day; or omeprazole 20 mg, clarithromycin 250 mg, metronidazole 400 mg – 2 times a day; or omeprazole 40 mg 1 time 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 – 1 time a day and clarithromycin 500 mg – 3 times a day or amoxicillin 0.75-1.5 g – 2 times a day).

Special dosage regimen.

In case of hepatic insufficiency,10-20 mg is prescribed; in case of impaired renal function and in elderly patients, no dosage adjustment is required.

Special instructions

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

Taking it simultaneously with food does not affect its effectiveness.

Form of production

Capsules No. 2 are transparent, colorless with a transparent pink lid.

The contents of the capsules are white or almost white pellets.

Active ingredient

Omeprazole

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Description

For adults as directed by your doctor

Indications

Gastrointestinal infections caused by Helicobacter Pylori, Reflux Esophagitis, Gastric and Duodenal ulcers