Omeprazole-OBL - instructions for use, dose, side effects, contraindications

Auxiliary substances of pellets: calcium carbonate; Potassium phosphate is disubstituted; hydroxypropylmethylcellulose (hypromellose); mannitol; sugar pellets (sucrose); sugar syrup (sucrose); polyethylene glycol 6000; polyvinylpyrrolidone K-30; sodium hydroxide; sodium lauryl sulfate; talc; titanium dioxide; tween 80

Pellet shell composition: acrylic coating L30D

The composition of the gelatin capsule: azorubine, gelatin, methyl parahydroxybenzoate, propyl parahydroxybenzoate, acetic acid.

Description:

Capsules № 2 are transparent, colorless with a lid of transparent pink color. The contents of the capsules are pellets of white or almost white color.

Pharmacotherapeutic group:The iron of the stomach secretion is a reducing agent - a proton pump inhibitor

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

Omeprazole - antiulcer drug, inhibitor of the enzyme H⁺/TO⁺ adenosine triphosphate (ATP) phase. It inhibits the activity of H⁺/TO⁺ - adenosine triphosphate (ATP) - phase (H⁺/TO⁺ - adenosine triphosphate (ATP) phase, it is also a "proton pump"), in parietal cells of the stomach, thereby blocking the transfer of hydrogen ions and the final stage of synthesis of hydrochloric acid in the stomach. Omeprazole is a prodrug.In the acidic environment of the tubules of parietal cells Omeprazole is converted into an active metabolite, sulfenamide, which inhibits membrane H⁺/TO⁺ - adenosine triphosphate (ATP) - phase, connecting with it due to the disulfite bridge. This explains the high selectivity of the action of omeprazole on parietal cells, where there is a medium for the formation of sulfenamide. Biotransformation of omeprazole to sulfenamide occurs rapidly (after 2-4 min). Sulfenamide is a cation and is not absorbed.

Omeprazole suppresses the basal and hydrochloric acid secretion stimulated by any stimulus at the final stage. Reduces the total volume of gastric secretion and inhibits the release of pepsin. Gastroprotective activity was detected in omeprazole, the mechanism of which is not clear. Does not affect the production of the internal factor of the Castle and the speed the transition of the food mass from the stomach to the duodenum. Omeprazole does not affect acetylcholine and histamine receptors.

Omeprazole capsules contain coated microgranules, gradual release and the onset of omeprazole starts 1 hour after admission, reaches a maximum after 2 hours.Stays for 24 hours or more.

Inhibition of 50% of the maximum secretion after a single dose of 20 mg of the drug lasts 24 hours.

A single dose per day provides rapid and effective suppression of day and night gastric secretion, reaching its maximum after 4 days of treatment.

In patients with duodenal ulcer, taking 20 mg of omeprazole maintains the pH at level 3 inside the stomach for 17 hours.

Pharmacokinetics:

Absorption is high. Bioavailability - 30-40% (with liver failure increases almost to 100%); increases in elderly people and in patients with impaired liver function, the failure of renal function has no effect. The time required to reach the maximum TC concentration_mOh- 0.5-3.5 h. Possessing high lipophilicity, it easily penetrates into the parietal cells of the stomach, communication with plasma proteins - 90-95% (albumin and acid alpha-1-glycoprotein). Half-life T_1/2- 0.5-1 h (with liver failure - 3 h), clearance - 500-600 ml / min. Almost completely metabolized in the liver with the participation of the enzyme system CYP₂_C₁₉, with the formation of 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulphonic derivatives, etc.). Is an inhibitor of isoenzyme CYP₂_C₁₉. Kidney excretion (70-80%) and bile (20-30%) in the form of metabolites In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion decreases, bioavailability increases.

Indications:

Peptic ulcer of stomach and duodenum (in the phase of exacerbation and anti-relapse treatment), incl. associated Helicobacter pylori (as part of combination therapy), reflux esophagitis (including erosive), hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis); gastropathy caused by the use of non-steroidal anti-inflammatory drugs.

Contraindications:

Hypersensitivity, child age, pregnancy, lactation.

Carefully:

Renal and / or hepatic insufficiency.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Inside, capsules are usually taken in the morning, without chewing, with a small amount of water (just before eating).

With exacerbation of peptic ulcer, reflux-esophagitis and gastropathy,caused by the use of non-steroidal anti-inflammatory drugs - 20 mg once a day. For patients with severe reflux esophagitis, the dose is increased to 40 mg once a day.

The course of treatment for duodenal ulcer is 2-4 weeks, if necessary - 4-5 weeks; with gastric ulcer, with reflux-esophagitis, with erosive-ulcerative lesions of the gastrointestinal tract caused by the use of non-steroidal anti-inflammatory drugs for 4-8 weeks.

Reduction of symptoms of the disease and scarring of the ulcer in most cases occurs within 2 weeks. Patients who have not had complete cicatrization of the ulcer after a two-week course should continue treatment for 2 more weeks.

Patients who are resistant to treatment with other antiulcer drugs are prescribed 40 mg / day. The course of treatment for peptic ulcer of 12 duodenal ulcer - 4 weeks, with peptic ulcer and reflux-esophagitis - 8 weeks. With Zollinger-Ellison syndrome - 60 mg once a day; if necessary, increase the dose to 80-120 mg / day (in this case, the dose is divided into 2-3 doses). For the prevention of recurrences of peptic ulcer - 10 mg once a day.

For eradication Helicobacter pylori use "triple" therapy (within 1 week: omeprazole 20 mg, amoxicillin 1 g, clarithromycin 500 mg - twice a day; or omeprazole 20 mg, clarithromycin 250 mg, metronidazole 400 mg - twice a day; or omeprazole 40 mg once a day, amoxicillin 500 mg and metronidazole 400 mg - 3 times a day) or "double" therapy (within 2 weeks: omeprazole 20-40 mg and amoxicillin 750 mg - twice a day or omeprazole 40 mg -1 once a day and clarithromycin 500 mg - 3 once a day or amoxicillin 0,75-1,5 g - 2 times a day).

In special situations:

For hepatic insufficiency appoint 10-20 mg once a day (with severe liver failure, the daily dose should not exceed 20 mg); if there is a violation of kidney function and in elderly patients, correction of the dosing regimen is not required.

Side effects:

From the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; in rare cases - increased activity of "liver" enzymes, taste disorders; in some cases - dry mouth, stomatitis, in patients with a previous severe liver disease - hepatitis (including jaundice), a violation of liver function.

From the nervous system: in patients with severe concomitant somatic diseases - dizziness, headache, agitation, depression, in patients with a previous severe liver disease - encephalopathy.

From the side of the musculoskeletal system: in some cases - arthralgia, myasthenia gravis, myalgia.

On the part of the hematopoiesis system: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

From the skin: rarely - skin rash and / or itching, in some cases - photosensitization, multiform exudative erythema, alopecia.

Allergic reactions: urticaria, angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock.

Other: rarely - gynecomastia, malaise, visual impairment, peripheral edema, increased sweating, the formation of gastric glandular cysts during long-term treatment (consequence of inhibition of HC1 secretion, is benign, reversible).

Overdose:

Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.

Treatment: symptomatic. Hemodialysis is not effective enough.

Interaction:

Can reduce the absorption of esters of ampicillin, iron salts, itraconazole and ketoconazole (omeprazole increases the pH of the stomach).

Being an inhibitor of cytochrome P450, can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action, phenytoin (drugs that are metabolized in the liver via cytochrome CYP₂_C₁₉), which in some cases may require a reduction in the doses of these drugs.

At the same time, the long-term use of omeprazole 20 mg once daily in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not change their plasma concentration.

Increases the inhibitory effect on the hematopoiesis system of other drugs. No interaction with concomitant antacids was noted.

Special instructions:

Before the start of therapy, it is necessary to exclude the presence of a malignant process (especially with gastric ulcer), since treatment, masking the symptoms, can delay the setting of the correct diagnosis.

Admission simultaneously with food does not affect its effectiveness.

Form release / dosage:

Capsules 20 mg

Packaging:

For 10 or 20 capsules in a contour mesh package.

By 1,2, or 3 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

List B. Store in a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 of the year. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001558 / 01

Date of registration:25.03.2009 / 14.05.2015

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp07.06.2017

Illustrated instructions

Instructions

Omeprazole-OBL (Omeprazole-OBL)