Omeprazol

General characteristics. Structure:

1 capsule contains granules (pellets) of an omeprazol in terms of омепразол – 0,02 g.

Pharmacological properties:

Pharmacodynamics. Omeprazol belongs to antiulcerous anti-secretory drugs. It easily gets into covering cells of a mucous membrane of a stomach, concentrates in them and is activated at acid value рН. The active metabolite – sulphenamide oppresses H+, K +-Atfazu a secretory membrane of covering cells (the proton pump), stopping an exit of ions of hydrogen in a gastric cavity and blocking a final stage of secretion of hydrochloric acid. Dozozavisimo reduces the level of basal and stimulated secretion, total amount of gastric secretion and release of pepsin. Effectively oppresses both night, and day products of hydrochloric acid.
Renders bactericidal effect on Helicobacter pylori. pylori at simultaneous use of an omeprazol and antibiotics allows to stop to Eradikation N. quickly disease symptoms, to reach high extent of healing of the damaged mucous and permanent long remission, reduces probability of development of bleeding from digestive tract. At a reflux ulcer esophagitis normalization of acid exposure in a gullet and maintenance intragastric рН> 4,0 within 24 hours with reduction of the damaging properties of contents of a stomach (braking of transition of a pepsinogen to pepsin) promotes weakening of symptomatology and full healing of injuries of a gullet (level of healing exceeds 90%). It is highly effective at treatment of the heavy and complicated forms of an erosive and ulcer esophagitis, resistant to N2-to blockers of histamine receptors. The long maintenance therapy prevents a recurrence of a reflux esophagitis and reduces risk of development of complications. At a gastroesophageal reflux disease provides remission during 1 year at 85% of patients.

Pharmacokinetics. After intake drug is quickly and rather fully soaked up from digestive tract, however bioavailability makes no more than 50 - 55% (effect of "the first passing" through a liver). Linkng with proteins of a blood plasma (albumine and an acid alfa1-glycoprotein) very high – 95%. After a single dose of 20 mg of an omeprazol oppression of gastric secretion comes within the first hour, reaches a maximum in 2 hours and about 24 hours proceed, expressiveness of effect depends on a dose. Ability of covering cells to produce hydrochloric acid is recovered within 3 – 5 days after the end of therapy. Drug is exposed to biotransformation in a liver with formation, at least, of 6 metabolites which are characterized by practical lack of anti-secretory activity. It is excreted generally by kidneys in the form of metabolites (72 – 80%) and through intestines (18 – 23%). The elimination half-life is equal 0,5 – 1 hour (at normal function of a liver) or 3 hours (at chronic diseases of a liver). At patients of advanced age perhaps some increase in bioavailability and reduction of speed of removal.

Indications to use:

- A peptic ulcer of a stomach, duodenum, an erosive and ulcer esophagitis in an aggravation phase;
- Helicobacter pylori eradikation;
- morbid hyper secretory conditions (Zollingera-Ellison's syndrome, polyendocrine adenomatosis, system mastocytosis, stressful ulcers);
- the erosive cankers of a stomach and duodenum connected with reception of non-steroidal anti-inflammatory drugs (NPVS);
- not ulcer dyspepsia.

Route of administration and doses:

Accept inside to food, without chewing and without damaging the capsule, washing down with a small amount of liquid.
Adults and children are more senior than 14 years Omeprazol accept:
- at a peptic ulcer of a stomach, duodenum and a reflux esophagitis on 20 mg once a day, if necessary the dose is increased to 40 mg (on 1 capsule in the morning and in the evening). Duration of a course of treatment at an ulcer of a 12-perstny gut makes 2 – 4 weeks, and at stomach ulcer and a reflux esophagitis respectively 4 - 8 weeks;
- at Zollingera-Ellison's syndrome the initial dose makes 20 – 60 mg/days, in need of it raise to 120 mg/days. And it is necessary to appoint a daily dose of 80 mg in the dose divided into 2 receptions more within 2 - 8 weeks;
- at the round ulcer caused by Helicobacter pylori for Helicobacter pylori eradikation Omeprazol appoint in a complex with antibiotics, metronidazole, drugs of bismuth and other medicines;
- at resistance to other antiulcerous drugs Omeprazol it is necessary to appoint, since 40 mg a day;
- at the gastroenteropathies connected with reception of non-steroidal anti-inflammatory drugs (NPVS) appoint 20 mg of 1 times a day within 4 – 8 weeks.

Features of use:

It is recommended to accept only to destination and under control of the specialist doctor. Children are not recommended to appoint drug due to the lack of clinical experience of use of Omeprazol for this category of patients. Before an initiation of treatment it is necessary to exclude existence of a malignant new growth in a GIT, especially at stomach ulcer. At patients with a heavy liver failure the dose should not exceed 20 mg/days (in connection with increase in bioavailability and an elimination half-life). At Omeprazol's use distortion of results of laboratory researches of function of a liver and indicators of concentration of gastrin in a blood plasma is possible.

Side effects:

At Omeprazol's reception are possible:
- from bodies of digestive tract: nausea, diarrhea, a lock, an abdominal pain, a meteorism, dryness in a mouth, lack of appetite;
- from a nervous system: headache, dizziness, weakness (including muscular), sleep disorder, drowsiness, depression, alarm;
- from a musculoskeletal system: in certain cases – an arthralgia, muscular weakness, a mialgiya;
- from system of a hemopoiesis: in certain cases – anemia, an eosinophilia, thrombocytopenia;
- allergic reactions: skin rash.

Interaction with other medicines:

Changes bioavailability of any medicine which absorption depends on pH (кетоконазол, iron salts). Omeprazol can increase an elimination half-life and duration of the effect of drugs,
metabolized in a liver by oxidation (diazepam, warfarin); strengthens effect of coumarinic anticoagulants and dipheninum; (Sibazonum) slows down allocation of benzodiazepine tranquilizers. Increases (mutually) concentration in blood of a klaritromitsin. At simultaneous use of Omeprazol with antacids of medicinal interaction it is noted.

Contraindications:

Hypersensitivity to Omeprazol, pregnancy, the lactation period (for the period of treatment it is necessary to stop feeding by a breast), chronic diseases of a liver.

Overdose:

Symptoms: a sight illegibility, confusion of consciousness, a headache, sweating strengthening, drowsiness, dryness in a mouth, nausea, rush of blood to the person, tachycardia.
Treatment: symptomatic.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. A period of validity – 3 years. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules on 0,02 g No. 10 in контурн.