Omeprazol

General characteristics. Structure:

Each capsule contains pellet of an omeprazol — 0,235 g in terms of 20 mg of an omeprazol. Structure of pellets: омепразол, Mannitolum, sucrose, sodium hydrophosphate (sodium phosphate disubstituted), sodium lauryl sulfate, lactose, calcium carbonate, gipromelloz (gidroksipropilmetiltsellyuloz), methacrylic acid and ethyl acrylate copolymer (copolymer of acid of methacrylic L30D), propylene glycol, diethyl phthalate, cetyl alcohol, sodium hydroxide (sodium hydroxide), polysorbate-80 (twin-80), povidone (polyvinylpirrolidone), titanium dioxide, talc.

Structure of the capsule: titanium dioxide (Е 171), dye quinolinic yellow (Е 104), dye yellow sunset (Е 110), gelatin.

Pharmacological properties:

Omeprazol inhibits H+ K enzyme + ATP-ase ("the proton pump") in covering cells of a stomach and blocks thereby a final stage of synthesis of hydrochloric acid. It leads to decrease in level of basal and stimulated secretion, irrespective of the irritant nature. After a single dose of drug inside action of an omeprazol comes within the first hour and continues within 24 hours, the maximum of effect is reached in 2 hours. At patients with a peptic ulcer of a duodenum reception of 20 mg of an omeprazol supports intragastric рН — 3,0 pieces within 17 hours. After the termination of administration of drug secretory activity is completely recovered in 3-5 days.

Pharmacokinetics. Omeprazol is quickly absorbed from digestive tract, the maximum concentration in plasma is reached in 0,5-1 hour. Bioavailability makes 30-40%. Communication with proteins of plasma — about 90%. Omeprazol is almost completely metabolized in a liver. An elimination half-life — 0,5-1 hour. It is removed generally by kidneys in the form of metabolites. At a chronic renal failure removal decreases in proportion to decrease in clearance of creatinine. At elderly patients removal decreases, bioavailability increases. At a liver failure a bisdostupnost — 100%, an elimination half-life — 3 hours.

Indications to use:

— Peptic ulcer of a stomach and duodenum;
— Reflux esophagitis;
— The erosive cankers of a stomach and duodenum connected with reception of non-steroidal anti-inflammatory drugs (NPVP), stressful ulcers;
— The erosive cankers of a stomach and duodenum associated with Helicobacter pylori (as a part of complex therapy);
— Zollingera-Ellison's syndrome.

Route of administration and doses:

Inside, washing down with a small amount of water (contents of the capsule cannot be chewed). A peptic ulcer of a duodenum in an aggravation phase — on 1 capsule (20 mg) a day within 2-4 weeks (in resistant cases to 2 capsules a day). A peptic ulcer of a stomach in a phase of an aggravation and  an erosive and ulcer esophagitis  — on 1-2 capsule a day within 4-8 weeks.  The digestive tract erosive cankers  caused  by reception of NPVP — on 1 capsule a day within 4-8 weeks.
Eradikation Helicobacter pylori — on 1 capsule 2 times a day within 7 days in combination with antibacterial agents.
Antirecurrent treatment of a peptic ulcer of a stomach and 12-perstny gut — on 1 capsule a day.
Antirecurrent treatment a reflux esophagitis — 1 capsule a day for a long time (up to 6 months). Zollingera-Ellison's syndrome — a dose is selected individually depending on the initial level of gastric secretion, usually since 60 mg a day. If necessary the dose is increased to 80-120 mg a day, in this case it is divided into 2 receptions.

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.
Reception along with food does not influence its efficiency.
At emergence of difficulties with a proglatyvaniye of the whole capsule, it is possible to swallow its contents after opening or a rassasyvaniye of the capsule, and also it is possible to mix capsule contents with slightly acidified liquid (juice, yogurt) and to use the received suspension within 30 min. At patients with a heavy liver failure the daily dose should not exceed 20 mg.

Side effects:

In rare instances there can be following, usually reversible, by-effects:
- From digestive organs: diarrhea or a lock, nausea, vomiting, a meteorism, an abdominal pain, dryness in a mouth, taste disturbances, stomatitis, tranzitorny increase in level of "hepatic" enzymes in plasma; patients with the previous serious illness of a liver have a hepatitis (including with jaundice), an abnormal liver function.
- From a nervous system: headache, dizziness, excitement, drowsiness, sleeplessness, paresthesias, depression, hallucinations; at patients with the serious accompanying somatopathies, patients with the previous serious illness of a liver — encephalopathy. From a musculoskeletal system: muscular weakness, mialgiya, arthralgia.
- From system of a hemopoiesis: leukopenia, thrombocytopenia; in some cases — an agranulocytosis, a pancytopenia.
- From integuments: itch; seldom, in some cases — a photosensitization, a multiformny erythema, an alopecia.
- Allergic reactions: small tortoiseshell, Quincke's disease, bronchospasm, intersticial nephrite and acute anaphylaxis.
- Other: vision disorder, peripheral hypostases, sweating strengthening, fever, gynecomastia; seldom — 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:

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. Interaction with at the same time accepted antacids is noted. Changes bioavailability of any drug which absorption depends on value рН (for example, iron salts).

Contraindications:

Hypersensitivity to drug, children's age, pregnancy, the lactation period.

Overdose:

Symptoms of overdose are the vision disorder, drowsiness, excitement, confusion of consciousness, a headache, increase in sweating, dryness in a mouth, nausea, arrhythmia.
The specific antidote does not exist.
Symptomatic treatment. The hemodialysis — is insufficiently effective.

Storage conditions:

List B. In dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Capsules on 20 mg.
On 10 capsules in blister strip packagings.
On 10,20, 30,40, 50 or 100 capsules in containers polymeric.
One container or 1, 2, 3, 4, 5, 6, 8 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.
On 10 or 20 containers or on 10, 20, 40, 60, 80 and 100 blister strip packagings together with the corresponding number of instructions put in a box from a cardboard.