Zheklizol - instructions for use, dose, side effects, contraindications

Specific proton pump inhibitor: inhibits the activity of H + / K + -ATPase in parietal cells of the stomach, blocking the final stage of hydrochloric acid secretion, thereby reducing acid production. Reduces basal and stimulated secretion regardless of the nature of the stimulus.

Omeprazole is a prodrug and is activated in the acidic environment of secretory tubules of parietal cells of the stomach.

The effect is dose-dependent and provides an effective inhibition of both basal and stimulated acid secretion, regardless of the nature of the stimulating factor.

Pharmacokinetics:

The connection with plasma proteins is 90-95% (albumin and acid alpha-1 glycoprotein). Half-life (T_1/2) for the final phase of the plasma-time concentration curve - after intravenous infusion of omeprazole is approximately 40 minutes (for liver failure - 3 hours); the total plasma clearance is from 0.3 to 0.6 l / min. ChangeThere is no evidence of half-life during treatment. Almost completely metabolized in the liver with the participation of the enzymatic system of cytochrome P450 (CYP), with the formation of six pharmacologically inactive metabolites (hydroxyomeprazole, sulfide and sulphonic derivatives and others). A significant portion of the metabolism of omeprazole depends on the polymorphically expressed specific isoform CYP2C19 (S-mephenytoin hydroxylase), responsible for the formation of hydroxyomeprazole, the main plasma metabolite. Is an inhibitor of isoenzyme CYP2C19. Kidney excretion (70-80%) and with bile (20-30%). In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion decreases, bioavailability increases.

Indications:

- Stomach ulcer and duodenal ulcer (including the prevention of relapses).

- Reflux esophagitis.

- Hyper-secretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis).

- NSAID-gastropathy.

- Prevention of aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome).

Contraindications:Hypersensitivity, child age, pregnancy, lactation.

Carefully:Renal and / or hepatic insufficiency.

Pregnancy and lactation:

Dosing and Administration:

For intravenous infusion.

For the treatment of patients who are not suitable for oral administration of the drug, with severe exacerbation of peptic ulcer, reflux esophagitis and NSAID-gastropathy, the recommended daily dose of Zhelkizol® is 40 mg for administration in the form of an intravenous infusion.

In patients with Zollinger-Ellison syndrome, the drug is prescribed in an initial dose of 60 mg / day. The dose should be selected individually, it is possible to administer higher doses (80-120 mg / day). If the daily dose is more than 60 mg, it should be divided into 2-3 infusions within 24 hours.

To prevent aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome), the drug is prescribed for the night at a dose of 40 mg and at least 2 hours before anesthesia / surgery at a dose of 40 mg.

In elderly patients, there is no need to adjust the dose.

Preparation of the infusion solution

A solution for intravenous infusion (infusion) is prepared immediately before use. To prepare a solution for intravenous infusion (infusion), use only 5% glucose solution without preservatives. To dissolve 40 mg of lyophilized omeprazole powder, at least 5 ml of solvent are added to the vial and gently shaken until the lyophilizate is completely dissolved. A prepared solution containing 40 mg of omeprazole, before infusion, is diluted in 100 ml of 5% glucose solution without preservatives for intravenous infusion (for infusion) for at least 30 minutes. Before infusion, it should be ensured that there are no suspended particles in the solution. The chemical and physical stability of the prepared solution of omeprazole is observed for 6 hours from the moment of dissolution of omeprazole in a 5% solution of glucose.

Side effects:

From the hematopoiesis: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

On the part of 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 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 musculoskeletal system: in some cases - arthralgia, myasthenia gravis, myalgia.

From the skin: rarely - skin rash and / or itching, in some cases - photosensitivity, 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 (the consequence of inhibiting the secretion of hydrochloric acid, is benign, reversible).

Overdose:

According to clinical studies with intravenous infusion up to 270 mg of the drug per day and in a dose of up to 650 mg in three days, dose-dependent side effects were not detected.

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 R₄₅₀, can increase the concentration and reduce the excretion of diazepam, anticoagulants of indirect action (warfarin), phenytoin (drugs that are metabolized in the liver via cytochrome CYP2C19), which in some cases may require a reduction in the doses of these drugs.

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

The concentrations of omeprazole and clarithromycin in the blood plasma increase during the simultaneous oral intake of these drugs, while evidence of the interaction of omeprazole with metronidazole and amoxicillin is not revealed.

Special instructions:

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

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increasedconcentration of attention and speed of psychomotor reactions.

Form release / dosage:

Lyophilizate for solution for infusion.

Packaging:

40 mg of the active substance into a vial of colorless glass, sealed with chlorobutyl stopper and an aluminum cap with a plastic lid.

1 The bottle together with the instruction for use is placed in a cardboard box.

10 packets are placed in a cardboard box.

Storage conditions:

In tightly closed containers, in the dark place at a temperature of no higher than 20 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001152

Date of registration:11.11.2011

Expiration Date:11.11.2016

The owner of the registration certificate:Yucea Pharmaceutical Group Co., Ltd.Yucea Pharmaceutical Group Co., Ltd. China

Manufacturer: & nbsp

YUKEA PHARMACEUTICAL GROUP Co., Ltd. China

Representation: & nbspInstitute of Health CJSCInstitute of Health CJSC

Information update date: & nbsp17.05.2017

Illustrated instructions

Instructions

Zhelezol® (Gelcizol®)