Омепразол-Акри®

General characteristics. Structure:

Active ingredient: 20 mg of an omeprazol.

Excipients: Mannitolum, sucrose, sodium hydrophosphate (sodium phosphate disubstituted), sodium lauryl sulfate, lactose, calcium carbonate, gipromelloz (gidroksipropilmetiltsellyuloz), methacrylic acid copolymer, propylene glycol, diethyl phthalate, cetyl alcohol, sodium hydroxide (sodium hydroxide), polysorbate (twin-80), povidone (polyvinylpirrolidone), titanium dioxide, talc.

Structure of the capsule: titanium dioxide (capsule case, capsule cover), ferrous oxide yellow (capsule case, capsule cover), ferrous oxide black (capsule cover), indigotin (capsule cover), gelatin (capsule case, capsule cover).

Pharmacological properties:

Pharmacodynamics. Inhibitor of the protonew pump, reduces a kislotoproduktion — brakes activity of H+/K +-ATF-azy in covering cells of a stomach and blocks thereby a final stage of secretion of hydrochloric acid. Drug is pro-medicine and is activated in acid medium of secretory tubules of covering cells. Reduces basal and stimulated secretion irrespective of the irritant nature.

The anti-secretory effect after reception of 20 mg occurs within the first hour, at most — in 2 hours. The inhibition of 50% of the maximum secretion proceeds 24 hours.

The single dose in days provides the bystry and effective oppression of day and night gastric secretion reaching the maximum in 4 days of treatment and disappearing by the outcome 3-4 days after the end of reception. At patients with a peptic ulcer of a 12-perstny gut reception of 20 mg of an omeprazol supports intragastric рН at the level of 3,0 within 17 hours.

Pharmacokinetics. Absorption — high, maximum concentration in a blood plasma is reached during 0,5-3,5 h, bioavailability — 30-40% (at a liver failure increases practically up to 100%); having high lipophilicity, drug easily gets into covering cells of a stomach, communication with proteins of plasma — 90-95% (albumine and an acid alfa1-glyco-protein).

Elimination half-life — 0,5-1 h (at a liver failure — 3 h), clearance — 500-600 ml/min. It is almost completely metabolized in a liver with participation of the fermental CYP2C19 system, with formation of several metabolites (гидроксиомепразол, sulphidic and sulfonic derivatives, etc.), pharmacological inactive. Is CYP2C19 isoenzyme inhibitor. Removal by kidneys (70-80%) and with bile (20-30%).

At a chronic renal failure removal decreases in proportion to decrease in clearance of creatinine. At elderly patients removal decreases, bioavailability increases.

Indications to use:

• peptic ulcer of a stomach and 12-perstny gut (including prevention of a recurrence);
• reflux esophagitis;
• Zollingera-Ellison's syndrome;
• stressful ulcers of the digestive tract (DT);
• polyendocrine adenomatosis;
• system mastocytosis;
• the gastropathy caused by reception of non-steroidal anti-inflammatory drugs (NPVP-gastropathy);
• Helicobacter pylori eradikation at the infected patients with a peptic ulcer of a stomach and a 12-perstny gut (as a part of a combination therapy).

Route of administration and doses:

Inside, not to chew. Capsules usually accept in the morning, washing down with a small amount of water (just before food or during meal).

At an aggravation of a peptic ulcer, a reflux esophagitis and NPVP-gastropathies — 20 mg of 1 times a day. To patients with a heavy current the reflux esophagitis a dose ^{of Omeprazola-Akri®} is increased to 40 mg of 1 times a day. A course of treatment at a peptic ulcer of a 12-perstny gut — 2-3 weeks, if necessary — 4-5 weeks; at a peptic ulcer of a stomach and an esophagitis — 4-8 weeks.

Sick, resistant to treatment by other antiulcerous drugs, ^{Omeprazol-Akri®} appoint 40 mg/days. A course of treatment at a peptic ulcer of a 12-perstny gut — 4 weeks, at a peptic ulcer of a stomach and a reflux esophagitis — 8 weeks.

At Zollingera-Ellison's syndrome - 60 mg/days; if necessary the dose is increased up to 80-120 mg/days (in this case it is appointed in 2-3 receptions).

For prevention of a recurrence of a peptic ulcer — 10 mg of 1 times a day.

For an eradikation of Helicobacter pylori use "triple" therapy (within 1 week: ^{Омепразол-Акри® 20} mg, amoxicillin of 1 g, кларитромицин 500 mg — on 2 times a day; or ^{Омепразол-Акри® 20} mg, кларитромицин 250 mg, metronidazole of 400 mg — on 2 times a day; or ^{Омепразол-Акри® 40} mg of 1 times a day, amoxicillin of 500 mg and metronidazole of 400 g — on 3 times a day) or "double" therapy (during 2 weeks: ^{Омепразол-Акри® 20-40} mg and amoxicillin of 750 mg — on 2 times a day or ^{Омепразол-Акри® 40} mg — 1 time a day and кларитромицин 500 mg — 3 times a day or amoxicillin of 0,75-1,5 g — 2 times a day).

Features of use:

Before therapy it is necessary to exclude existence of malignant process (especially at stomach ulcer) since treatment, masking symptomatology, can delay statement of the correct diagnosis.

Side effects:

From the alimentary system: diarrhea or locks, abdominal pain, nausea, vomiting, meteorism; in rare instances — increase in activity of "hepatic" enzymes, taste disturbances; in some cases — dryness in a mouth, stomatitis, at patients with the previous serious illness of a liver is hepatitis (including with jaundice), an abnormal liver function.

From bodies of a hemopoiesis: in some cases — a leukopenia, thrombocytopenia, an agranulocytosis, a pancytopenia.

From a nervous system: patients with the heavy accompanying somatic diseases have a dizziness, a headache, excitement, a depression, patients with the previous serious illness of a liver have an encephalopathy.

From a musculoskeletal system: in some cases — an arthralgia, a myasthenia, a mialgiya.

From integuments: seldom — skin rash and/or an itch, in some cases — a photosensitization, a multiformny exudative erythema, an alopecia.

Allergic reactions: small tortoiseshell, Quincke's disease, fever, bronchospasm, intersticial nephrite and acute anaphylaxis.

Others: seldom — a gynecomastia, an indisposition, vision disorders, peripheral hypostases, sweating strengthening, formation of gastric glandulyarny cysts during prolonged treatment (a consequence of inhibition of secretion of HSL, has high-quality, reversible character).

Interaction with other medicines:

Can reduce absorption of ethers of ampicillin, salts of iron, an itrakonazol and ketokonazol (омепразол raises рН a stomach).

Being inhibitor of P450 cytochrome, ^{Omeprazol-Akri®} can increase concentration and reduce removal of diazepam, anticoagulants of indirect action, Phenytoinum (drugs which are metabolized in a liver by means of CYP2C19 cytochrome) that in certain cases can demand reduction of doses of these medicines.

At the same time prolonged use ^{of Omeprazola-Akri®} in a dose of 20 mg of 1 times a day in a combination with caffeine, theophylline, piroxicam, diclofenac, Naproxenum, metoprololy, propranolol, ethanol, cyclosporine, lidocaine, quinidine and oestradiol did not lead to change of their concentration in plasma.

Interaction with at the same time accepted antacids is noted.

Contraindications:

• hypersensitivity;
• children's age;
• pregnancy;
• lactation period.

With care. Renal and/or liver failure.

Overdose:

Symptoms: confusion of consciousness, a sight illegibility, drowsiness, dryness in a mouth, a headache, nausea, tachycardia, arrhythmia.

Treatment: symptomatic. The hemodialysis is insufficiently effective.

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Not to use drug after a period of validity. A period of storage - 2 years.

Issue conditions:

According to the recipe

Packaging:

Capsules of 20 mg. On 10 capsules in a blister strip packaging. 1, 2 or 3 blister strip packagings together with the application instruction place in a pack from a cardboard.