Omeprazol

General characteristics. Structure:

Active ingredient: omeprazole;

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

excipients: granules (pellet) contain: mannitol (Е 421); sucrose; sodium додецилсульфат; sodium hydrophosphate, dodecahydrate; calcium carbonate (Е 170); to a gipromeloz; cetyl alcohol; titanium dioxide (Е 171); sodium methylparaben (Е 219); sodium propylparaben (Е 217).

Pharmacological properties:

Pharmacodynamics. Omeprazol – antiulcerous anti-secretory drug. 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 +-ATF-azu 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 H2 blockers of histamine receptors. The long maintenance therapy prevents a recurrence of a reflux esophagitis and reduces risk of development of complications.

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 completion of therapy. Drug is transformed 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.

Pharmaceutical characteristics.

Main physical and chemical properties: solid gelatin capsules. The case and a lid of the capsule - blue color. Capsule contents – granules (pellet) from white till almost white color, spherical shape.

Indications to use:

Benign stomach ulcer and ulcer of a duodenum, including connected with reception of non-steroidal anti-inflammatory drugs; Helicobacter pylori eradikation (as a part of a combination therapy with antibacterial agents); gastroesophageal reflux disease; prevention of aspiration of acid contents of a stomach; Zollingera-Ellison's syndrome; reduction of symptoms of kislotozavisimy dyspepsia.

Route of administration and doses:

Accept inside before food or during meal, without chewing and without damaging the capsule, washing down with a small amount of liquid. The mode of dosing depends on a look and disease severity and is established by the doctor individually for each patient.

Adults and children are more senior than 12 years.

Ulcer of a duodenum and stomach: a daily dose – 1 capsule. Usually the course of treatment of an ulcer of a duodenum makes 4 weeks, stomach ulcers – 8 weeks. If necessary it is possible to increase a daily dose to 2 capsules.

Treatment and prevention of an ulcer of a duodenum and stomach, and also the gastroduodenal erosion and dispeptic symptoms connected with reception of non-steroidal anti-inflammatory drugs: the recommended daily dose makes 20 mg. A course of treatment – 4-8 weeks.

For Helicobacter pylori eradikation: Omeprazol appoint in a daily dose 40 mg (on 20 mg 2 times a day) as a part of complex therapy according to the approved international schemes:

"Triple" therapy at a duodenum ulcer: within 1 week on 2 times a day: amoxicillin of 1 g and кларитромицин 500 mg; within 1 week on 2 times a day: кларитромицин 250 mg and metronidazole of 400 mg (or Tinidazolum of 500 mg); within 1 week on 3 times a day: amoxicillin of 500 mg and metronidazole of 400 mg.

"Double" therapy at a duodenum ulcer: within 2 weeks on 2 times a day: amoxicillin of 750 mg – 1 g; within 2 weeks on 3 times a day: кларитромицин 500 mg.

"Double" therapy at stomach ulcer: within 2 weeks on 2 times a day: amoxicillin –

750 mg – 1 g.

Gastroesophageal reflux disease: a daily dose – 1 capsule, a course of treatment – 4-8 weeks. The patient a reflux esophagitis, resistant to treatment, use 2 capsules daily within 8 weeks.

Prevention of aspiration of acid contents of a stomach: the recommended dose of an omeprazol – 40 mg overnight and 40 mg in 2-6 hours before an anesthesia.

Zollingera-Ellison's syndrome: the initial dose of Omeprazol which is accepted once in the morning makes 60 mg a day; if necessary the daily dose is increased to 80-120 mg. The dose should be selected individually taking into account reaction of an organism. If the daily dose exceeds 80 mg, it needs to be divided into 2-3 receptions.

Kislotozavisimy dyspepsia: the daily dose makes 10-20 mg disposable for 2-4 weeks. If in 4 weeks symptoms do not disappear or shortly again appear, it is necessary to revise the diagnosis of the patient. In need of Omeprazol's use in a single dose less than 20 mg use drug with the smaller content of active ingredient.

Dose adjustment of Omeprazol and at patients with a renal failure is not required from elderly people.

At patients with an abnormal liver function the maximum daily dose of Omeprazol makes 20 mg.

Children. This dosage form of Omeprazol is applied to children 5 years with body weight not less than 20 kg are more senior.

At a reflux esophagitis a course of treatment – 4-8 weeks; at a symptomatic treatment of heartburn and regurgitation of hydrochloric acid at a gastroesophageal reflux disease – 2-4 weeks. The daily dose makes 20 mg, if necessary it is possible to increase a daily dose to 40 mg.

If the child cannot swallow the capsule, it should be opened, and to mix contents with a small amount of apple juice or yogurt (approximately in 10 ml). It is necessary to track that the child swallowed this mix immediately after preparation.

Perhaps Omeprazol's use as a part of complex therapy for Helicobacter pylori eradikation to children is more senior than 5 years, however this therapy should be carried out with extra care under careful observation of the doctor. A course of treatment – 7 days, if necessary prolong a course of treatment up to 14 days.

Scheme of treatment: children with the body weight of 30-40 kg: Omeprazol of 20 mg, amoxicillin of 750 mg, кларитромицин 7,5 mg/kg of body weight 2 times a day within 7 days;

children with body weight more than 40 kg: Omeprazol of 20 mg, amoxicillin of 1 g, кларитромицин 500 mg 2 times a day within 7 days.

Features of use:

Before an initiation of treatment it is necessary to exclude existence of a malignant new growth in digestive tract, especially at stomach ulcer as treatment masks symptomatology and can delay statement of the correct diagnosis.

Dose adjustment of Omeprazol with a renal failure is not required from elderly people and patients. Dialysis which is carried out at patients with chronic diseases of kidneys does not influence Omeprazol's pharmacokinetics. At an abnormal liver function the maximum daily dose of Omeprazol makes 20 mg.

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.

Decrease in secretion of acid in a stomach under the influence of inhibitors of the proton pump or other kislotoingibiruyushchy agents leads to increase in growth of microflora of digestive tract. Therefore it is necessary to consider that decrease in acidity of gastric contents can increase risk of development of the intestinal infections caused by such bacteria as Salmonella and Campylobacter.

There are messages on cases of moderate deficit of B12 vitamin at long and continuous reception of inhibitors of the proton pump therefore there can be reasonable a monitoring procedure of level of B12 vitamin in blood serum.

Ability to influence speed of response at control of motor transport or work with other mechanisms. Drug should be used with care to the persons managing motor transport or other mechanisms that is connected with risk of emergence of side effects from a nervous system.

Side effects:

Criteria for evaluation of frequency of development of side reactions of medicine: often (≥ 1/100); infrequently (≥ 1/1000 and <1/100); seldom (<1/1000).

At Omeprazol's use disturbances are possible:
from the central and peripheral nervous system: often – a headache; infrequently – dizziness, a loss of consciousness, the general weakness, sleeplessness, drowsiness, alarm, paresthesias; seldom – excitement, reversible confusion of consciousness, aggression, depressions and hallucinations;
from digestive tract: often – diarrhea, a lock, an abdominal pain, nausea, vomiting, a meteorism; seldom – dryness in a mouth, stomatitis, digestive tract candidiasis, lack of appetite;
from a liver and biliary system: infrequently – taste disturbance, increase in activity of "hepatic" enzymes; seldom – patients with the previous serious illness of a liver have a hepatitis (including with jaundice), encephalopathy, a heavy abnormal liver function (including a liver failure);
from a musculoskeletal system: seldom – an arthralgia, muscular weakness, a mialgiya;
from system of a hemopoiesis: seldom – anemia, a leukopenia, a pancytopenia, thrombocytopenia, an agranulocytosis, an eosinophilia;
from skin and its derivatives: infrequently – rash (including violent) and/or an itch, dermatitis, urticaria; seldom – a photosensitization, a multiformny exudative erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, an alopecia;
allergic reactions: seldom – a Quincke's disease, fever, a bronchospasm, an acute anaphylaxis;
others: infrequently – an indisposition; seldom - intersticial nephrite, a gynecomastia, a vision disorder, peripheral hypostases, sweating strengthening, impotence, a hyponatremia.

Interaction with other medicines:

Omeprazol can increase an elimination half-life and duration of effect of diazepam, coumarinic anticoagulants of indirect action (warfarin), Phenytoinum, Sibazonum that in certain cases can demand reduction of doses of these medicines. However at simultaneous use of Phenytoinum and omeprazol in a daily dose of 20 mg at the patients who are on continuous treatment by Phenytoinum change of its concentration in blood was not observed.

At a concomitant use of an omeprazol with warfarin or other antagonists of vitamin K continuous monitoring of limits INR (the international normalized relation) is necessary.

Changes bioavailability of medicines which absorption depends on pH (кетоконазол or итраконазол, iron salts, ampicillin ethers).

Does not interact with acetphenetidiene, theophylline, caffeine, propranolol, piroxicam, diclofenac, Naproxenum, metoprololy, cyclosporine, lidocaine, quinidine, ethanol, oestradiol or antiacid means.

Strengthens an inhibiting effect of other medicines on system of a hemopoiesis. Increases (mutually) concentration in blood of a klaritromitsin, there is no interaction with metronidazole or amoxicillin.

Simultaneous administration of drug Omeprazol and digoxin to healthy volunteers increases bioavailability (by 10%) digoxin owing to increase рН gastric contents.

Omeprazol increases the level of a takrolimus in blood. The concomitant use with a complex - атазанавир 300 mg and ритонавир 100 mg as joint reception leads to reduction of AUCT (the area under a curve "concentration time") an atazanavira for 76% is not recommended, to Cmax – for 72%, Cmin – for 79%. At a concomitant use of an omeprazol and a vorikonazol there is a competitive inhibition of metabolism by means of P450 cytochrome isoenzymes - CYP2C19 and CYP3A4. Omeprazol (40 mg of 1 times a day) raises Cmax and AUST of a vorikonazol for 15 and  41% respectively. Dose adjustment of a vorikonazol is not recommended. Vorikonazol raises Cmax and AUST of an omeprazol for 116 and 280% respectively. Therefore at purpose of a vorikonazol the patients receiving омепразол are recommended to reduce a dose of the last twice.

Contraindications:

Hypersensitivity to active ingredient and/or to other components of drug; simultaneous use with atazanaviry; children's age up to 5 years; feeding period breast.

Overdose:

At Omeprazol's overdose there are symptoms characteristic of side effect.

Treatment. There is no specific antidote. It is badly removed by means of dialysis. The gastric lavage, the symptomatic and supporting treatment is shown.

Use during pregnancy or feeding by a breast.

Use of drug at pregnancy is possible if the expected positive effect for mother exceeds potential risk for a fruit.

In case of need uses of drug for treatment it is necessary to stop feeding by a breast.

Children.

Drug is used to children of 5 years on doctor's orders at a reflux esophagitis and a symptomatic treatment of heartburn and regurgitation of hydrochloric acid at a gastroesophageal reflux disease.

Storage conditions:

Period of validity. 3 years. Not to use drug after the termination of the period of validity specified on packaging. To store in protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in the blister. On 1 or 3 blisters enclosed in a pack.