Omeprazol

General characteristics. Structure:

Active ingredient: 20 mg of an omeprazol in 1 capsule.

Excipients of pellets: calcium carbonate, potassium phosphate disubstituted; gidroksipropilmetiltsellyuloz (gipromelloz); Mannitolum; sugar pellets (sucrose); sugar syrup (sucrose); polyethyleneglycol 6000; поливинилпироллидон K-30; sodium hydroxide; sodium lauryl sulfate; talc; titanium dioxide; twin 80.

Structure of an obolchka of pellets: acrylic covering of L30D.

Structure of the capsule gelatinous: azoruby, gelatin, метилпарагидроксибензонат, пропилпарагидроксибензоат, acetic acid.

Powerful anti-secretory antiulcerous tool.

Pharmacological properties:

Pharmacodynamics. Inhibitor of the protonew pump, reduces a kislotoproduktion - brakes activity of N+/K+-ATF-azy in covering cells of a stomach and blocks thereby a final stage of secretion of HCl. 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 h.

The inhibition of 50% of the maximum secretion 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 at the level of 3 during 17 h.

Pharmacokinetics. Absorption - high, TCmax - 0.5-3.5 h, 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). There is 0.5-1 h T1/2 (at a liver failure - 3 h), 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 derivatives, etc.), pharmacological inactive. Is CYP2C19 isoenzyme inhibitor. Removal by kidneys (70-80%) and with bile (20-30%). At HPN removal decreases in proportion to decrease in KK. 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 a GIT, polyendocrine adenomatosis, system mastocytosis); NPVP-gastropathy.

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 in other antiulcerous HP, 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 the dose is increased up to 80-120 mg/days (in this case it is appointed in 2-3 receptions). 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 (during 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 (during 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).

Specific mode of dosing. At a liver failure appoint 10-20 mg; at a renal failure and it is not required from elderly patients of correction of the mode of dosing.

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.

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 HCl, has high-quality, reversible character).

Interaction with other medicines:

Can reduce absorption of ethers of ampicillin, Fe salts, an itrakonazol and a ketokonazol (омепразол raises stomach pH).

Being P450 cytochrome inhibitors, 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 other ЛС.Не it is noted interactions with at the same time accepted antacids.

Contraindications:

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

With care. Renal and/or liver failure.

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 dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 10 or 20 capsules in a blister strip packaging. On 1, 2, or 3 blister strip packagings together with the application instruction in a pack from a cardboard.