Омез® Insta

General characteristics. Structure:

Each bag contains: active agent: омепразол 20 mg; excipients: Natrii hydrocarbonas of 1680 mg, ксилитол 2000 mg, sucrose of 2070 mg, sukraloza of 30 mg, gum of xanthane 55 mg, fragrance of mint 30 mg.

Description

Powder from white till almost white color with a mint smell.

Pharmacological properties:

Pharmacodynamics. Specific inhibitor of the proton pump: brakes aktivnostn+/K+-ATF-azy in covering cells of a stomach, blocking a final stage of secretion of hydrochloric acid, thereby, reduces a kislotoproduktion.
Omeprazol is pro-medicine and is activated in acid medium of secretory tubules of covering cells of a stomach.
Influence is dozozavisimy and provides effective inhibition to both basal, and stimulated secretion of acid, irrespective of the nature of the stimulating factor.
Elimination of heartburn after administration of drug happens within 30 minutes. The inhibition of 50% of the maximum secretion of hydrochloric acid proceeds 24 h.
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 pH higher than 3 during 17 h.

Pharmacokinetics. Absorption - high; time of achievement of the maximum concentration (TCmax), on average, 30 min. (10-90 min.), 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 - 95% (albumine and an acid alfa1-glycoprotein).
The elimination half-life (T1/2) makes about 0,5-1 h (at a liver failure - 3 h); the general clearance of plasma - from 0,3 to 0,6 l/min. Change of the size T1/2 during treatment does not happen.
It is almost completely metabolized in a liver with participation of fermental system of P450 (CYP) cytochrome, with formation of six pharmacological inactive metabolites (гидроксиомепразол, sulphidic and sulfonic derivatives, etc.). A considerable part of metabolism of an omeprazol depends from polimorfno the expressed specific CYP2C19 isoform (S-Mephenytoinum a hydroxylase) which is responsible for formation of a gidroksiomeprazol, main plasma metabolite. 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:

The heartburn and other symptoms associated with a gastroesophageal reflux disease (GERB);
not erosive and erosive (reflux esophagitis) of the GERB form;
peptic ulcer of a stomach and duodenum (including, prevention of a recurrence);
Helicobacter pylori eradikation at the infected patients with a peptic ulcer of a stomach and duodenum (as a part of a combination therapy);
NPVP-gastropathy;
hyper secretory states (Zollingera-Ellison's syndrome, stressful ulcers of digestive tract, polyendocrine adenomatosis, system mastocytosis).

Route of administration and doses:

Inside, in 30 minutes prior to food. To pour out contents of a bag in a cup, to add 1-2 tablespoons of water (do not use other liquids or foodstuff!), carefully to stir before receiving homogeneous suspension and at once to drink. As necessary it is possible to wash down with a small amount of water.
The single dose of 20 mg of drug is sufficient for bystry stopping of symptoms of heartburn.
To patients from not erosive GERB - on 20 mg of 1 time/days within 4 weeks.
To patients with the GERB erosive form (reflux esophagitis) - on 20 mg of 2 times/days within 4-8 weeks, depending on severity of an esophagitis.
For prevention of an aggravation a reflux esophagitis - 20 mg/days, duration of a maintenance therapy is defined individually.
At an aggravation of a peptic ulcer of a stomach or a 12-perstny gut which is not associated with Helicobacter pylori - on 20 mg in the morning of 1 time/days during 4-8 weeks.
For an eradikation of Helicobacter pylori use therapy in various combinations: within 7-14 days омепразол 20 mg, amoxicillin of 1 g, кларитромицин 500 mg - on 2 times/days; or омепразол 20 mg, кларитромицин 500 mg, metronidazole of 500 mg - on 2 times/days; or омепразол 20 mg - 2 times/days, bismuth drugs in a dose of 120 mg - 4 times/days, metronidazole of 500 mg - 3 times/days and tetracycline of 500 mg - 4 times/days.
For prevention of a peptic ulcer of a stomach or a 12-perstny gut - on 20 mg in the morning of 1 time/days during 4-8 weeks.
For treatment of NPVP-gastropathies - on 20 mg of 2 times/days within 4-6 weeks, for prevention - 20 mg/days for use of NPVP are at the patients having risk factors of development of the NPVP-gastropathy.
At hyper secretory states - on 20 mg in the morning of 1 time/days during 4-8 weeks.
At treatment of a syndrome of Zollingera-Ellison of a dose are selected individually, depending on a clinical state. The recommended initial dose - 60 mg a day. At most of patients the state is adequately controlled in the range of doses of 20-120 mg. In need of use of a dose over 80 mg, it is necessary to divide it into 2 introductions.
Elderly patients and at a renal failure have no need to adjust a dose. At a liver failure there can be sufficient a daily dose of 20 mg.

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.
Impact on driving and use of other equipment.
Омез® Insta does not influence ability to manage transport and work with mechanisms.
Because during therapy dizziness and drowsiness can be observed by the drug Omez® of Inst, it is necessary to be careful at control of motor transport, etc. mechanisms.

Side effects:

In rare instances there can be following, usually reversible side reactions.
Frequency of side effects is classified depending on the frequency of occurrence of a case: very often (≥1/10), it is frequent (from ≥1/100 to <1/10), infrequently (from ≥1/1000 to <1/100), is rare (from ≥1/10000 to <1/1000), is very rare (<1/10000), including separate messages.
From bodies of a hemopoiesis: seldom - a leukopenia, thrombocytopenia; very seldom - an agranulocytosis, a pancytopenia.
From system of digestion: often - diarrhea or a lock, an abdominal pain, nausea, vomiting, a meteorism; seldom - increase in activity of "hepatic" enzymes, taste disturbances; very seldom - dryness in a mouth, stomatitis, candidiasis of a mucous membrane of a GIT; patients with the previous serious illness of a liver have a hepatitis (including, with jaundice); very seldom - a liver failure, including with development of encephalopathy (at patients with liver diseases in the anamnesis).
From a nervous system: often - a headache, infrequently - dizziness, paresthesias, drowsiness, is rare - taste disturbance.
Mental disturbances: infrequently - insomnia; seldom - agitation, confusion of consciousness, a depression, it is very rare - aggression, hallucinations.
From sense bodys: infrequently - вертиго; seldom - a sight illegibility.
From a musculoskeletal system: seldom - an arthralgia, a mialgiya; very seldom - muscular weakness.
From integuments: infrequently - dermatitis, an itch, rash, urticaria; seldom - an alopecia, a photosensitization, it is very rare - a multiformny exudative erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis.
Allergic reactions: seldom - hypersensitivity reactions, including fever, a Quincke's disease and anaphylactic reactions (including an acute anaphylaxis).
From urinogenital and reproductive system: seldom - intersticial nephrite, it is very rare - a gynecomastia.
Metabolic disturbances: seldom - a hyponatremia, it is very rare - a hypomagnesiemia.
Others: infrequently - the indisposition, peripheral hypostases, is rare - a bronchospasm, sweating strengthening.

Interaction with other medicines:

Owing to decrease in acidity of a gastric juice at treatment omeprazoly absorption of other medicines (M) which mechanism of absorption depends from рН a gastric juice can decrease or increase.
Reduces absorption of a ketokonazol and itrakonazol.
Increases digoxin absorption. Combined use of an omeprazol in a dose of 20 mg of 1 times a day and digoxin increases bioavailability of digoxin approximately for 10%.
It was shown what омепразол interacts with some anti-retrovirus HP.
Mechanisms and clinical value of these interactions are not always known. Increase рН in a stomach against the background of therapy omeprazoly can influence absorption of anti-retrovirus HP.
Interaction at the level of CYP2C19 isoenzyme is also possible. At combined use of an omeprazol and anti-retrovirus HP, such as атазанавир and нелфинавир, against the background of therapy omeprazoly, decrease in their concentration in serum is noted. In this regard combined use of an omeprazol with anti-retrovirus drugs, such as атазанавир and нелфинавир, it is not recommended.
At simultaneous use of an omeprazol and sakvinavir increase in concentration of a sakvinavir in blood serum was noted.
Omeprazol inhibits CYP2C19 - the main isoenzyme participating in his metabolism.
Combined use of an omeprazol with other. Hp in which metabolism CYP2C19 isoenzyme takes part such as diazepam, Phenytoinum, warfarin, other antagonists of vitamin K and цилостазол, can lead to decrease in metabolism of these drugs.
Control of concentration of Phenytoinum in plasma at simultaneous use of Phenytoinum and omeprazol is recommended; in some cases Phenytoinum dose decline can be required. At the same time, at patients, it is long accepting Phenytoinum, combined use of an omeprazol in a dose of 20 mg of 1 times a day did not cause change of concentration of Phenytoinum in a blood plasma.
At use of an omeprazol for the patients receiving warfarin or other antagonists of vitamin K control of the international normalized relation (INR) is necessary; in some cases the dose decline of warfarin or other antagonist of vitamin K can be required. At the same time, at patients, it is long accepting warfarin, combined use of an omeprazol in a dose of 20 mg of 1 times a day did not cause change of time of coagulation.
Use of an omeprazol in a dose of 40 mg of 1 times a day led to increase in Cmax and the area under a curve "concentration time" (AUC) of a tsilostazol for 18% and 26%, respectively; for one of active metabolites of a tsilostazol increase made 29% and 69%, respectively.
Omeprazol does not influence metabolism of HP which metabolism is carried out by means of an isoenzyme of CYP3A4, such as cyclosporine, lidocaine, quinidine, oestradiol, erythromycin and будесонид.
At simultaneous use of an omeprazol and takrolimus increase in concentration of a takrolimus in blood serum was noted.
Isoenzymes of CYP2C19 and CYP3A4 participate in metabolism of an omeprazol. Combined use of an omeprazol and inhibitors of isoenzymes of CYP2C19 and CYP3A4, such as кларитромицин and вориконазол, can lead to increase in concentration of an omeprazol in a blood plasma due to delay of metabolism of an omeprazol. Combined use of a vorikonazol and omeprazol led more than to double increase in AUC of an omeprazol that however did not demand dose adjustment of an omeprazol.
The HP inducing isoenzymes of CYP2C19 and CYP3A4 which such as rifampicin and drugs of a St. John's Wort is made a hole at combined use with omeprazoly can lead to decrease in concentration of an omeprazol in a blood plasma due to acceleration of metabolism of an omeprazol.

Contraindications:

Hypersensitivity, intolerance of fructose, deficit of invertase/isomaltase, glyukozo-galaktozny malabsorption (owing to existence in composition of drug of sucrose), children's age, pregnancy, the lactation period.
Drug should not be used together with atazanaviry and nelfinaviry.

With care

Renal and/or liver failure.

Overdose:

Symptoms: a headache, dizziness, block, confusion of consciousness, tachycardia, arrhythmia, a sight illegibility, drowsiness, dryness in a mouth, nausea, vomiting, a meteorism.
Treatment: symptomatic. If necessary - a gastric lavage, absorbent carbon. The hemodialysis is insufficiently effective.

Storage conditions:

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 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

The powder for preparation of suspension for intake containing 20 mg of an omeprazol.
On 5,885 g of powder in a bag from the combined material (polyethylene of low density / aluminum foil / polyethylene of low density / glassine).
On 5, 10, 20, 30 bags together with the application instruction in a pack cardboard.