Omeprazol

General characteristics. Structure:

Active agent of an omeprazol of 20 mg;
excipients: Mannitolum, sucrose, sodium hydrophosphate (sodium phosphate disubstituted), sodium lauryl sulfate, lactose, calcium carbonate, methacrylic acid and ethyl acrylate copolymer [1:1] (copolymer of acid of methacrylic L30D), gipromelloz (gidroksipropilmetiltsellyuloz), propylene glycol, diethyl phthalate, cetyl alcohol, sodium hydroxide (sodium hydroxide), polysorbate-80 (twin-80), povidone (polyvinylpirrolidone), titanium dioxide, talc.
Structure of a gelatinous solid capsule: the case - titanium dioxide, gelatin; a cover - titanium dioxide, gelatin, dye quinolinic yellow, dye patentovy blue, dye diamond black.

Description: the capsules No. 2 consisting of the case of white color and a cover of green color. Contents of capsules - white or almost white spherical pellets.

Pharmacological properties:

Inhibitor of the proton pump, reduces a kislotoproduktion - brakes activity of H+/K +-adenozintrifosfatazy ("the proton pump") 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 within 17 hours.

Pharmacokinetics. Absorption - high, time of achievement of the maximum concentration (TCmax) - 0.5-3.5 hours, bioavailability - 30-40% (at a liver failure increases practically up to 100%); having high lipophilicity, easily gets into covering cells of a stomach, communication with proteins of plasma - 90-95% (albumine and an acid alfa1-glycoprotein). An elimination half-life (T1/2) - 0.5-1 hour (at a liver failure - 3 hours), clearance - 500-600 ml/min. It is almost completely metabolized in a liver with participation of the fermental CYP2C19 system, with formation of 6 metabolites (гидроксиомепразол, sulphidic and sulfonic derivative and others), 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, hyper secretory states (Zollingera-Ellison's syndrome, stressful ulcers of digestive tract, polyendocrine adenomatosis, system mastocytosis). Prevention of aspiration of acid contents of a stomach in respiratory tracts during the general anesthesia (Mendelssohn's syndrome). The gastropathy caused by reception of non-steroidal anti-inflammatory drugs (NPVP).
Eradikation Helicobacter pylori 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, capsules usually accept in the morning, capsules cannot be chewed, 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 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 medicines (M), 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; if necessary a dose increase do80-120 mg/days (in this case it is appointed in 2-3 receptions).
- Prevention of a syndrome of Mendelssohn - 40 mg in 1 hour prior to operation (in case of carrying out operation longer than 2 hours, it is necessary to enter a necessary dose of drug repeatedly).
- 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 20 mg, amoxicillin of 1 g, кларитромицин 500 mg - on 2 times a day; or омепразол 20 mg, кларитромицин 250 mg, metronidazole of 400 mg - on 2 times a day; or омепразол 40 mg of 1 times a day, amoxicillin of 500 mg and metronidazole of 400 mg - on 3 times a day) or "double" therapy (within 2 weeks: омепразол 20 - 40 mg and amoxicillin of 750 mg - on 2 times a day, or омепразол 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) as treatment, masking symptomatology, can delay statement of the correct diagnosis.
Reception along with food does not influence its efficiency.

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 serious accompanying somatopathies 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 hydrochloric acid, 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 P450 cytochrome inhibitor, can increase concentration and reduce removal of diazepam, anticoagulants of indirect action, Phenytoinum (HP which are metabolized in a liver by means of CYP2C19 cytochrome) that in certain cases can demand reduction of doses of these HP.
At the same time prolonged use of an omeprazol 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.
Strengthens an inhibiting effect on system of a hemopoiesis of other HP.
Interaction with at the same time accepted antacids is noted.

Contraindications:

Hypersensitivity, children's age, pregnancy, lactation period.

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. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Capsules on 20 mg.
On 10 or 15 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3 blister strip packagings on 10 capsules or on 1, 2, 3, 4 blister strip packagings on 15 capsules together with the application instruction place in a pack from a cardboard.