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

Excipients: sugar granules (sucrose 80.0 - 91.5%, corn starch 8.5 - 20.0%, water purified 1.5%) - 83.960 mg, anhydrous - 4.090 mg, hypromellose 2910/6 - 8,500 mg, giprolose - 3,065 mg, sodium lauryl sulfate 0.255 mg, sodium hydrogen phosphate dodecahydrate 0.410 mg, triethyl citrate 2.865 mg, talc 12,000 mg, methacrylic acid and ethyl acrylate copolymer [1: 1] 24.855 mg;

Capsule shell: body: (E 172) 0.02%, iron dye oxide red (E 172) 0.04%, titanium dioxide (E 171) 4.00%, iron dye oxide yellow (E 172) 0 , 22%, gelatin - up to 100.00 %; lid: iron dye oxide red (E 172) 0.06%, titanium dioxide (E 171) 1.33%, iron dye oxide yellow (E 172) 0.65%, gelatin to 100.00%.

Description:

Hard gelatin capsules # 3, body: light brownish yellow color,

lid: light orange color.

Contents of capsules: from white to white with a light yellowish-brownish hue of color spherical pellets.

Pharmacotherapeutic group:glands of the stomach secretion-lowering agent - proton pump inhibitor

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

Mechanism of action

Omeprazole has a highly selective mechanism of action, which reduces the secretion of gastric juice. It is a specific inhibitor of the proton pump of parietal cells of the stomach. The action of the drug occurs quickly and is mediated by reversible inhibition of the secretion of gastric juice.

Omeprazole is a weak base. Concentrates in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, is activated and inhibits the proton pump - the enzyme H⁺, K⁺ATPase. Effect of omeprazole on the last stage of the process of formation of hydrochloric acid in the stomach is dose-dependent and provides a highly effective inhibition of basal and stimulated secretion of hydrochloric acid regardless of the stimulating factor.

Effect on secretion of gastric juice

Omeprazole with a daily oral administration provides a fast and effective inhibition of day and night secretion of hydrochloric acid. The maximum effect is achieved within 4 days of treatment.In patients with duodenal ulcer omeprazole 20 mg causes a steady decrease in 24-hour gastric acidity by at least 80%. At the same time, the average maximum concentration of hydrochloric acid is reduced after pentagastrin stimulation by 70% within 24 hours.

In patients with duodenal ulcer omeprazole 20 mg with daily use maintains in the intragastric environment the pH value of pH> 3 on average for 17 hours per day.

Inhibition of the secretion of hydrochloric acid depends on the area under the concentration-time curve (AUC) of omeprazole, and not on the concentration of the drug in the blood plasma at a given time.

Action on Helicobacter pylori

Omeprazole has a bactericidal effect on Helicobacter pylori in vitro. Eradication Helicobacter pylori when omeprazole is used together with antibacterial agents it is accompanied by a rapid elimination of symptoms, a high degree of healing of defects in the gastrointestinal mucosa and a prolonged remission of peptic ulcer, which reduces the likelihood of complications such as bleeding, as effectively as constant maintenance therapy.

Pharmacokinetics:

Suction

Omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum concentration in the plasma is reached after 0.5-1 h. Omeprazole It is absorbed in the small intestine, usually within 3-6 hours. Bioavailability after a single oral intake is approximately 30-40%, after a constant intake of 1 time per day, bioavailability increases to 60%. Eating does not affect the bioavailability of omeprazole.

Distribution

The binding of omeprazole to plasma proteins is about 95%, the volume of distribution is 0.3 l / kg.

Metabolism

Omeprazole is completely metabolized in the liver. The main isoenzymes involved in the metabolic process, CYP2C19 and CYP3A4. Given the high affinity of omeprazole for isoenzyme CYP2C19 it is possible to compete with other drugs in the metabolism of which this isoenzyme is involved. Hydroxy- omeprazole is the main metabolite produced by isoenzyme CYP2C19. The resulting metabolites - sulfone and sulfide - do not have a significant effect on the secretion of hydrochloric acid.

Excretion

The half-life is about 40 minutes (30-90 minutes).About 80% is excreted as metabolites by the kidneys, and the rest is through the intestine.

Special patient groups Elderly patients

In elderly patients there was a slight decrease in the metabolism of omeprazole. Patients with impaired renal function

In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance.

Patients with impaired liver function

In patients with impaired liver function, there is an increase in the area under the concentration-time curve (AUC). Omeprazole does not have a cumulative effect.

Indications:

Symptomatic treatment of reflux symptoms (heartburn, nausea, acidic eructation) in adults associated with gastroesophageal reflux disease (GERD).

Contraindications:

- Hypersensitivity to omeprazole, substituted benzimidazoles or other ingredients in the formulation.

- Deficiency of lactase, sucrose / isomaltase, lactose intolerance, fructose, glucose-galactose malabsorption.

- Joint use with nelfinavir.

- Children's age (under 18 years).

Carefully:

In patients with osteoporosis (risk of hip fractures, wrist and spine bones), with simultaneous use with atazanavir (dose of omeprazole should not exceed 20 mg per day).

In the presence of symptoms such as significant weight loss, frequent vomiting, dysphagia, vomiting with blood or melena, and with a stomach ulcer (or suspected gastric ulcer), the presence of a malignant tumor should be excluded, since treatment can lead to masking of symptoms and, thus delaying the setting of the correct diagnosis.

Pregnancy and lactation:

The results of the studies showed no side effects of omeprazole on the health of pregnant women, on the fetus or on the newborn. Omeprazole Zentiva can be used during pregnancy.

Omeprazole penetrates into breast milk, but when applied in therapeutic doses, exposure to the baby is unlikely. Omeprazole Zentiva can be used during breastfeeding.

Dosing and Administration:

Inside, squeezed with a small amount of water (the contents of the capsule can not be chewed).

If you have difficulty swallowing the whole capsule, you can swallow its contents after opening or dissolving the capsule, and you can mix the contents of the capsule with a slightly acidified liquid (juice, yogurt) and use the resulting suspension for 30 minutes. DO NOT USE with milk or soda water.

The usual dose is 2 capsules of the drug Omeprazole Zentiva (or 20 mg) once a day (preferably in the morning, on an empty stomach).

Reduction in the severity of symptoms is usually observed after 2-3 days of regular intake of capsules.

In most patients, heartburn completely disappears within 7 days. After complete disappearance of the symptoms, treatment should be discontinued.

Treatment without medical supervision is carried out for 14 consecutive days.

Special patient groups Impaired renal function

In patients with impaired renal function, dose adjustment is not required.

Impaired liver function

Patients with impaired liver function before starting the drug Omeprazole Zentiva is advised to consult a doctor.

Older persons (aged> 65 years)

In elderly people, dose adjustment is not required.

Side effects:

The side effects of omeprazole are usually minor and reversible. Possible occurrence of the following side effects, which are divided into system-organ classes according to the classification of the Medical Dictionary of Regulatory Activities (MedDRA).The WHO classification was used to indicate the frequency of side effects: very often (> 10%); often (> 1% and <10%); infrequently (> 0.1% and <1%, rarely (> 0.01% and <0.1%), very rarely (<0.01%), the frequency is unknown (according to available data, it is not possible to determine the occurrence frequency of the side effect possible).

Violations of the blood and lymphatic system

Rarely - Lakopenia, thrombocytopenia; rarely agranulocytosis, pancytopenia.

Immune system disorders

Rarely - Hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction / anaphylactic shock).

Disorders from the metabolism and nutrition

Rarely - hyponatremia; unknown frequency: hypomagnesemia.

Disorders of the psyche

Infrequently - insomnia; rarely - agitation, confusion, depression; rarely - aggression, hallucinations.

Disturbances from the nervous system

Often - headache; infrequently - dizziness, paresthesia, drowsiness; rarely - a taste disorder.

Disorders from the organ of vision Rarely blurred vision.

Hearing impairments and labyrinthine infringements infrequently - dizziness.

Disturbances from the respiratory system, chest and mediastinal organs Rarely - bronchospasm.

Disorders from the gastrointestinal tract

Often - diarrhea, constipation, nausea, vomiting, flatulence, abdominal pain; rarely - dry mouth, stomatitis, candidiasis of the gastrointestinal tract, microscopic colitis.

Disturbances from the liver and bile ducts

Infrequently - increased activity of "hepatic" enzymes; rarely - hepatitis (with jaundice or without); rarely - hepatic insufficiency, encephalopathy in patients with liver disease.

Disturbances from the skin and subcutaneous tissues

Infrequently - dermatitis, itching, rash, hives; rarely - alopecia, photosensitivity; rarely - multiform erythema, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Disorders from the musculoskeletal and connective tissue

Infrequently - fracture of the hip, bones of the wrist and vertebrae; rarely - arthralgia, myalgia; highly

rarely - muscle weakness.

Disorders from the kidneys and urinary tracts Rarely - interstitial nephritis.

Violations from the genitals and mammary gland Very rarely - gynecomastia.

General violations and violations at the site of introduction

Infrequently - malaise, peripheral edema; rarely - increased sweating. It has been reported cases of the formation of gastric glandular cysts during long-term treatment with proton pump inhibitors (a consequence of inhibiting the secretion of hydrochloric acid, is benign reversible in nature).

Overdose:

Single doses of omeprazole 560 mg when taken by adults caused symptoms of moderate intoxication. A case of taking a single dose of 2,400 mg of omeprazole is described, which does not cause any severe toxic symptoms. With increasing dose, the elimination rate of the drug did not change (first-order kinetics), but no specific treatment was required.

Symptoms: dizziness, confusion, apathy, depression, headache, tachycardia, nausea, vomiting, flatulence, diarrhea.

Treatment: symptomatic treatment, if necessary, gastric lavage,

purpose activated carbon.

Interaction:

Active substances with pH-dependent absorption

Absorption of some drugs may vary due to a decreased acidity of the gastric environment.

As well as with the use of other drugs that suppress the secretion of hydrochloric acid, or antacid agents,treatment with omeprazole may lead to a decrease in absorption of posaconazole, erlotinib, ketoconazole or itraconazole.

Digoxin

With the simultaneous use of omeprazole (at a dose of 20 mg per day) and digoxin in healthy volunteers, the bioavailability of digoxin increased by 10%. In rare cases, toxic effects of digoxin have been reported. Nevertheless, when using omeprazole in high doses in elderly people should be careful. In this regard, it is necessary to carry out careful therapeutic control of the patient.

Clopidogrel

With the simultaneous use of omeprazole with clopidogrel, there was a decrease in the plasma content of the active metabolite clopidogrel by 46% on the first day and by 42% on the fifth day of treatment, while the administration of omeprazole and clopidogrel at different times does not exclude the interaction of these drugs. Probably, the observed effect is due to the inhibitory effect of omeprazole on isoenzyme CYP2C19. Nelfinavir, atazanavir

With simultaneous application with omeprazole, the concentrations of nelfinavir and atazanavir in blood plasma decrease.

Joint use with nelfinavir is contraindicated (see.section "Contraindications"),

The simultaneous use of atazanavir and omeprazole is not recommended. If joint use of atazanavir and omeprazole is not possible, careful clinical observation of the patient is recommended, and an increase in the dose

atazanavir to 400 mg with the use of ritonavir in a dose of 100 mg, while the dose of omeprazole should not exceed 20 mg per day.

Tacrolimus

With the simultaneous use of omeprazole, an increase in the concentration of tacrolimus in the blood plasma was reported. It is necessary to carefully monitor the concentration of tacrolimus in the blood plasma, as well as monitor kidney function (creatinine clearance), and, if necessary, adjust the dose of tacrolimus. Methotrexate

Some patients reported an increase in the content of methotrexate in blood plasma when used simultaneously with proton pump inhibitors. When applying high doses of methotrexate, consideration may be given to the temporary removal of omeprazole.

Saquinavir

With the simultaneous use of omeprazole and saquinavir / ritonavir, saquinavir concentrations in the plasma increased to 70%.This increase in concentration in HIV-infected patients was well tolerated.

Preparations, metabolism of which is carried out with the participation of iso-ferment CYP2C19 Because the omeprazole is metabolized in the liver with the participation of isoenzyme CYP2C19, elimination of diazepam, warfarin (R-varfarin), cilostazol and phenytoin can be slowed down. It is recommended that patients who receive phenytoin and warfarin, you may need to reduce the dose of the above drugs. However, concomitant drug treatment in a daily dose of 20 mg does not affect the concentration of phenytoin in the blood plasma in patients taking a drug for a long time; concomitant treatment with omeprazole Zentiva in a daily dose of 20 mg does not lead to a change in coagulation time in patients taking long-term warfarin.

Inhibitor inhibitors CYP2C19 and / or CYP3A4

Isozyme inhibitory drugs CYP2C19 and CYP3A4, such as, voriconazole and clarithromycin, with simultaneous application with omeprazole may lead to an increase in omeprazole in the blood plasma due to a decrease in the metabolic rate of the drug.Patients with a dysfunction of the liver with prolonged use of omeprazole Zentiva may need a dose reduction. Inductors of isoenzymes CYP2C19 and / or CYP3A4

Medicines that induce isoenzymes CYP2C19 and CYP3A4, such as,

rifampicin and preparations of St. John's wort perfumed, when used together with the drug Omeprazole Zentiva may lead to a decrease in its concentration in the blood plasma by accelerating the metabolism of the drug.

Interaction with food or antacids was not revealed.

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. If after the start of taking the drug Omeprazole Zentiva within 5 days there is no improvement, or heartburn becomes even stronger, it is necessary to interrupt treatment and consult a doctor.

Patients over the age of 45 with symptoms of heartburn, suffering from heartburn for the first time, can take the drug Omeprazole Zentiva only after consulting a doctor.The drug Omeprazole Zentiva should not be taken without supervision by the doctor if there is one of the following symptoms or one of the conditions:

- reduced body weight for no apparent reason and / or lack of appetite, fatigue;

- prolonged pain in the abdominal cavity;

- gastric ulcer and / or duodenal ulcer in anamnesis;

- frequent vomiting;

- Swallowing / swallowing pain;

- bloody vomiting / melena / rectal bleeding;

- stable heartburn (more than three months);

- chronic cough, labored breathing;

- jaundice;

- pain in the chest (especially chest compressions or pain giving to the neck or upper limbs), if associated with sweating, shortness of breath or dizziness;

- cancer of the stomach or esophagus in the anamnesis of the next of kin;

- liver failure;

- rare hereditary disorders, for example, galactose intolerance, Lappease lactase deficiency, fructose deficiency, impaired glucose-galactose absorption, or isohalase isomaltase insufficiency.

If any of these symptoms / conditions occur, treatment should be controlled by a doctor.

Risk of hip fractures, wrist and vertebra bones

Proton pump inhibitors, especially when used in high doses and for long-term use (> 1 year), can moderately increase the risk of fractures of the hip, wrist and vertebrae, especially in elderly patients or other risk factors. The results of observational studies suggest that proton pump inhibitors can increase the overall fracture risk by 10-40%. Patients at risk for developing osteoporosis should receive treatment in accordance with the latest clinical recommendations.

Hypomagnesemia

In patients who received omeprazole for at least three months, severe hypomagnesemia was recorded. There may be fatigue, delirium, convulsions, dizziness and ventricular arrhythmia. In most patients hypomagnesemia was stopped after the withdrawal of proton pump inhibitors and the administration of magnesium preparations. Patients in whom long-term therapy is planned or assigned omeprazole with digoxin or other drugs that can cause hypomagnesemia (eg, diuretics), you should evaluate the magnesium content before starting therapy and periodically monitor it during treatment.

Effect on absorption of vitamin B12 (cyanocobalamin)

Omeprazole, like all drugs that reduce acidity, can lead to a decrease in vitamin absorption B₁₂ (cyanocobalamin), since it causes hypo- or achlorhydria. This should be remembered for patients with a reduced supply of vitamin B12 in the body or with risk factors for vitamin absorption abnormalities B₁₂ with prolonged therapy.

Other effects associated with inhibition of hydrochloric acid secretion.

Patients taking drugs that reduce the secretion of the glands of the stomach for a long period of time, more often noted the formation of glandular cysts in the stomach, which pass independently on the background of continued therapy. These phenomena are caused by physiological changes due to inhibition of hydrochloric acid secretion.

The decrease in the secretion of hydrochloric acid in the stomach by proton pump inhibitors or other acid-inhibiting agents leads to an increase in the growth of normal intestinal microflora, which in turn can lead to a slight increase in the risk of intestinal infections caused by bacteria of the genus Salmonella spp. and Campylobacter spp. and probably also a bacterium Clostridium difficile in hospitalized patients.

Impact on survey results

Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA). Increase in concentration CgA can influence the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, it is necessary to temporarily stop taking omeprazole 5 days before the concentration test CgA.

Taking omeprazole Zentiva simultaneously with food does not affect its effectiveness.

Effect on the ability to drive transp. cf. and fur:

There are no data on the effect of the drug on the ability to drive a car or other mechanisms. However, due to the fact that during the therapy there may be dizziness, blurred vision and drowsiness, care should be taken when driving vehicles or while working with mechanisms that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Capsules intestine soluble 10 mg.

Packaging:For 14 or 28 capsules in dark glass bottles, equipped with a plastic screw cap with autopsy control,containing a moisture drier. Each vial with instructions for use is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

The shelf life of the capsules in the vial after the first autopsy is 3 months.

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

Terms of leave from pharmacies:Without recipe

Registration number:П N011336 / 01

Date of registration:18.05.2010

Date of cancellation:2018-06-14

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA ZENTIVA Czech Republic

Information update date: & nbsp14.06.2018

Illustrated instructions

Instructions

Omeprazole Zentiva (Omeprazole Zentiva)