Omeprazole-OBL, 20 mg capsules 28 pcs

Pharmacotherapeutic group:

An anti-ulcer agent, proton pump inhibitor.

Pharmic action:

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

It 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 in 2 hours.

The inhibition of 50% of maximum secretion lasts for 24 h. A single daily administration provides fast and effective suppression of gastric secretion during the day and night, which reaches its maximum after 4 days of treatment and disappears by the end of 3-4 days after the end of administration.

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

Pharmacokinetics:

Absorption is high, TCmax is 0.5-3.5 h, bioavailability – 30-40% (in case of hepatic insufficiency it increases almost to 100%); having high lipophilicity easily penetrates into parietal cells of the stomach, binding to plasma proteins – 90-95% (albumin and acidic alpha1-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 participation of CYP2C19 enzymatic system, with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulfone derivatives and others), pharmacologically inactive.

It is an inhibitor of CYP2C19 isoenzyme.

Elevation by kidneys (70-80%) and with bile (20-30%).In CKD the excretion decreases in proportion to the decrease in CK.

In elderly patients, excretion decreases and bioavailability increases.

Indications

Gastric and 12 duodenal ulcers (including Prevention of relapse), reflux esophagitis, hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the stomach, polyendocrine adenomatosis, systemic mastocytosis);

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

Active ingredient

Composition

Active substance

Omeprazole – 20 mg.

Pellet excipients:

Calcium carbonate,

Potassium phosphate displaced;

Hydroxypropyl methylcellulose (hypromellose);

mannitol;

sugar pellets (sucrose);

sugar syrup (sucrose);

Polyethylene glycol 6000;

Polyvinylpyrrolidone K-30;

sodium hydroxide;

sodium lauryl sulfate;

talc;

titanium dioxide;

tween 80.

Pellet shell composition:

L30D acrylic coating

Composition of jellatin capsule:

azorubin,

gelatin,

methylparahydroxybenzonate,

How to take, the dosage

Overly, capsules are usually taken in the morning, capsules should not be chewed with a small amount of water (immediately before or during a meal).In acute peptic ulcer disease, reflux esophagitis and NSAID gastropathy – 20 mg once a day. In patients with severe reflux esophagitis the dose is increased up to 40 mg once daily.

The course of treatment for duodenal ulcer is 2-3 weeks, if necessary – 4-5 weeks; for peptic ulcer and esophagitis – 4-8 weeks. 40 mg per day is prescribed to patients who are resistant to treatment with other antiulcer drugs. The course of treatment in case of duodenal ulcer is 4 weeks, in case of gastric ulcer and reflux esophagitis – 8 weeks.

In 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 prevention of recurrence of peptic ulcer disease – 10 mg once daily.

For eradication of Helicobacter pylori a “triple” therapy is used (for 1 week: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg, 2 times daily; or omeprazole 20 mg, clarithromycin 250 mg, metronidazole 400 mg, 2 times daily; or omeprazole 40 mg once daily, amoxicillin 500 mg and metronidazole 400 mg, 3 times daily) or “dual” therapy (for 2 weeks: omeprazole 20-40 mg and amoxicillin 750 mg 2 times daily or omeprazole 40 mg once daily and clarithromycin 500 mg 3 times daily or amoxicillin 0.75-1.5 g – 2 times a day).

Particular dosing regimen.

In case of hepatic insufficiency, 10-20 mg is prescribed; in renal dysfunction and elderly patients dosage regimen does not need to be adjusted.

Interaction

May decrease absorption of ampicillin esters, Fe salts, itraconazole and ketoconazole (omeprazole increases gastric pH).

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

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

The interaction with concomitantly taken antacids has not been noted.

Special Instructions

Before therapy, it is necessary to rule out the presence of a malignant process (especially for gastric ulcers), because treatment, by masking symptoms, can delay the correct diagnosis.

Taking with food at the same time does not affect its effectiveness.

Contraindications

Hypersensitivity, childhood, pregnancy, lactation.

With caution.

Renal and/or hepatic insufficiency.

Side effects

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), liver function failure.

Hematopoietic organs: in single cases – leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

Nervous system disorders: in patients with severe concomitant somatic diseases – dizziness, headache, agitation, depression, in patients with previous severe liver disease – encephalopathy.

Musculoskeletal system: in some cases – arthralgia, myasthenia, myalgia.

The skin: rare – skin rash and/or itching, in some cases – photosensitization, erythema multiforme exudative, alopecia.

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

Others: rare – gynecomastia, malaise, visual disturbances, peripheral edema, increased sweating, formation of gastric glandular cysts during long-term treatment (consequence of inhibition of HCl secretion, is benign, reversible).

Overdose.

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

Treatment: symptomatic. Hemodialysis is not sufficiently effective.

Similarities