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

Active substance: omeprazole-20 mg (In the form of pellets - 0.235 g containing mannitol, sucrose, sodium lauryl sulfate, sodium hydrogen phosphate (disodium phosphate dibasic), calcium carbonate, lactose, hypromellose (hydroxypropylmethyl cellulose), methacrylic acid-ethyl acrylate copolymer (copolymer of methacrylic acid L30D), propylene glycol, dietilfta- lat, cetyl alcohol, sodium hydroxide (sodium hydroxide), Polysorbate-80 (Tween-80), povidone (polyvinylpyrrolidone), titanium dioxide, talc.

Capsule composition:

The body and lid: iron oxide red (E172), titanium dioxide (E171), metilparagidroksiben- benzoate (methyl hydroxybenzoate), propyl parahydroxybenzoate (propyl) gelatin.

Or hard gelatin capsules number 2.

Body and lid: iron oxide red (E172), titanium dioxide (E171), gelatin.

Description:Opaque capsules No. 2. The body is white, the cap is pinkish brown. The contents of capsules are pellets from white to almost white.

Pharmacotherapeutic group:a means of reducing the secretion of glands ¬ ¬ дка - - proton pump inhibitor

ATX: & nbsp

A.02.B.C.01 Omeprazole

Pharmacodynamics:

The proton pump inhibitor reduces acid production - inhibits the activity of H + / K + -ATPase in the parietal cells of the stomach and blocks the final stage of hydrochloric acid secretion. The drug is a prodrug and is activated in the acidic environment of the secretory tubules of parietal cells.

Reduces basal and stimulated secretion irrespective of the nature of the stimulus. Antisecretory effect after taking 20 mg occurs within the first hour, a maximum - through

1 hours. Inhibition of 50% of maximum secretion lasts 24 hours.

A single dose per day provides fast and effective suppression of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing to the end

3- 4 days after the end of admission. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH at level 3 for 17 hours.

Pharmacokinetics:

Absorption of the preparation is high, the time to reach the maximum concentration (TCmah) - 0.5-3.5 hours, bioavailability - 30-40% (with liver failure increases almost to 100%); possessing high lipophilicity, easily penetrates into the parietal cells of the stomach, communication with plasma proteins - 90-95% (albumin and acidic α₁glycoprotein).

The half-life (T1/2) - 0.5-1 hour (with hepatic insufficiency - 3 hours), clearance - 500-600 ml / min. Almost completely metabolized in the liver with the participation of the enzyme system CYP2C19, with the formation of 6 metabolites (hydroxyomeprazole, sulfide and sulfone derivatives, etc.), pharmacologically inactive. 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, hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis); NSAIDs are gastropathy. Eradication Helicobacter pylori in infected patients with peptic ulcer and duodenal ulcer (as part of combination therapy).

Contraindications:

hypersensitivity to omeprazole, substituted benzimidazoles or other ingredients in the formulation;
deficiency of lactase, sucrose / isomaltase, lactose intolerance, fructose, glucose-galactose malabsorption;

- combined use with erlotinibom, posaconazole, clarithromycin (in patients with hepatic insufficiency), St. John's wort;

children under 18, except;

- gastroesophageal reflux disease - children under 2 years old and body weight up to 20 kg;

- ulcer disease of the duodenum, associated with Helicobacter pylori

- Children under 4 years of age and body weight less than 31 kg.

Carefully:

Patients with osteoporosis, renal and / or liver failure, during pregnancy.

With simultaneous use with clarithromycin, clopidogrel, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, voriconazole, rifampicum.

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. Gastrozol® can be used during pregnancy. Omeprazole penetrates into breast milk, but when applied in therapeutic doses, the effect on the baby is unlikely.

Dosing and Administration:

The drug is taken orally, the capsules are not chewed, usually in the morning,with a small amount of water (immediately before meals or during meals).

Peptic ulcer of duodenum in the phase of exacerbation - 1 capsule (20 mg) per day for 2-4 weeks (in resistant cases up to 2 capsules per day).

Stomach ulcer in the phase of exacerbation and erosive-ulcerative esophagitis - 1-2 capsules per day for 4-8 weeks.

Erosive-ulcerative lesions of the gastrointestinal tract caused by the intake of NSAIDs - 1 capsule per day for 4- 8 weeks.

Eradication Helicobakter pylori - 1 capsule 2 times a day for 7 days in combination with antibacterial agents.

Anti-relapse treatment of peptic ulcer and 12 duodenum - 1 capsule per day.

Anti-relapse treatment of reflux esophagitis - 1 capsule per day for a long time (up to 6 months).

The syndrome of Zolinger-Ellison - the dose is selected individually depending on the initial level of gastric secretion, usually starting at 60 mg per day. If necessary, increase the dose to 80 - 120 mg per day, in this case, it is divided into 2 divided doses.

Side effects:

The following side effects are independent of the dosing regimen of omeprazole, which were noted during clinical trials, as well as in post-marketing applications.The following undesirable phenomena noted with the use of omeprazole. are distributed according to the frequency of occurrence in accordance with the following gradation: very often (> 1/10). often (> 1/100 to <1/10), infrequently (> 1/1000 to <1/100), rarely (> 1/10000 to <1/1000), very rarely (<1/10000), frequency, unspecified (can not be calculated from available data).

From the digestive system: often - diarrhea, constipation, abdominal pain, nausea, vomiting, flatulence; rarely - dry mouth, stomatitis, candidiasis of the gastrointestinal tract, microscopic colitis.

From the liver and bile ducts: infrequently - increased activityenrichment "enzymes;

rarely - hepatitis (with jaundice or without), hepatic insufficiency. Encephalopathy in patients with liver disease.

From the hematopoiesis: rarely - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, hypochromic microcytaric anemia in children.

From the nervous system: often - headache; infrequently - vertigo, paresthesia, drowsiness; rarely - a taste disorder.

From the musculoskeletal system: infrequently - fractures of the hip, bones of the wrist and vertebrae; rarely - arthralgia, myalgia, muscle weakness.

From the skin and subcutaneous tissues: infrequently - dermatitis, rash, itching, urticaria; rarely - alopecia, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the immune system: rarely - hypersensitivity reactions (eg, angioedema, fever, anaphylactic reaction / anaphylactic shock).

From the side of metabolism and nutrition: rarely - hyponatremia; very rarely - hypocalcemia due to severe hypo- magnemia, hypokalemia due to hypomagnesemia; unspecified frequency - hypomagnesemia.

From the side of the psyche: infrequently - insomnia; rarely - agitation, aggression, confusionhallucinations, depression.

From the side of the organ of vision: rarely - blurred vision.

From the respiratory system, chest and mediastinum: rarely - bronchospasm.

From the side of the kidneys and urinary tract: rarely interstitial nephritis.

From the genitals and the breast: rarely - gynecomastia.

General violations and violations at the place of introduction: infrequently - malaise; rarely - sweating. peripheral edema.

There have been reports of cases of the formation of glandular cysts in the stomach in patients,taking drugs that reduce the secretion of the glands of the stomach, for a long period of time; on their own against the backdrop of continued therapy.

Overdose:

Single oral doses of omeprazole up to 400 mg (2 capsules) did not cause any severe symptoms. Single doses of omeprazole 560 mg when taken by adults caused symptoms of moderate intoxication. With increasing dose, the elimination rate of the drug did not change, no specific treatment was required.

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

Treatment: symptomatic, if necessary, gastric lavage, the purpose of activated charcoal.

Interaction:

Effect of omeprazole on the pharmacokinetics of other drugs The decrease in the secretion of hydrochloric acid in the stomach in the treatment with omeprazole and other inhibitors of the proton pump can lead to a decrease or increase in the absorption of other drugs, the absorption of which depends on the acidity of the medium.

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 the absorption of erlotinib, ketoconazole or itraconazole, as well as increased absorption of digoxin. With the simultaneous use of omeprazole (at a dose of 20 mg per day) and digoxin, the bioavailability of digoxin increases by 10%.

It was shown that omeprazole interacts with some antiretroviral drugs. The mechanisms and the clinical significance of these interactions are not always known. An increase in pH on the background of omeprazole therapy may affect the absorption of antiretroviral drugs. It is also possible to interact at the isoenzyme level CYP2C19. When combined with omeprazole and some antiretroviral drugs, such as atanavir and nelfinavir, against the background of therapy with omeprazole there is a decrease in their concentration in serum. In this regard, the joint use of omeprazole with antiretroviral drugs, such as atazanavir and nelfinavir, Not recommended. With the simultaneous use of omeprazole and saquinavir, an increase in the concentration of saquinavir in the serum was noted, when used with some other antiretroviral drugs, their concentration did not change.

Omeprazole inhibits CYP2C19 - the main isoenzyme involved in its metabolism.Joint use of omeprazole with other drugs, in the metabolism of which isoenzyme participates CYP2C19, such as diazepam, warfarin (R-varfarin) or other antagonists of vitamin K, phenytoin and cilostosol, can lead to a slowing of the metabolism of these drugs. It is recommended that patients who receive phenytoin and omeprazole, it may be necessary to reduce the dose of phenytoin. However, concomitant treatment with omeprazole at a daily dose of 20 mg does not affect the concentration of phenytoin in the blood plasma in patients taking the drug for a long time. When using omeprazole by patients receiving warfarin or other antagonists of vitamin K, monitoring of the international normalized relationship is necessary; in some cases, a reduction in the dose of warfarin or another vitamin K antagonist may be necessary. At the same time, concomitant treatment with omeprazole at a daily dose of 20 mg does not leads to a change in coagulation time in patients taking long-term warfarin.

The use of omeprazole at a dose of 40 mg once a day led to an increase in C_mOh and AUC of cystostaxol by 18% and 26%, respectively; for one of the active metabolites of cilostazol, the increase was 29% and 69%, respectively.

Pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg / day) and omeprazole (80 mg / day inwards), which leads to an average decrease in exposure to the active metabolite of clopidogrel, is 46% and decrease in the maximum inhibition of ADP-

induced platelet aggregation by an average of 16%.

The clinical significance of this interaction is not clear. An increased risk of cardiovascular complications with the combined use of clopidogrel and proton pump inhibitors, including omeprazole, has not been shown in randomized clinical trials. The results of a number of observational studies are contradictory and do not give an unambiguous answer about the presence or absence of an increased risk of thromboembolic cardiovascular complications on the background of joint application

clopidogrel and proton pump inhibitors.

Omeprazole does not affect the metabolism of drugs metabolized by the isoenzyme CYP3A4, such as ciclosporin, estradiol, budesonide, quinidine, lidocaine.

There was no interaction of omeprazole with the following drugs: antacids, theophylline, caffeine, propra- ethanol, S-warfarin, piroxicam, diclofan, naproxen, metoprolol.

With the simultaneous use of omeprazole and tacrolimus, there was an increase in the concentration of tacrolimus in the blood serum.

Some patients reported a slight increase in plasma methotrexate concentration when used simultaneously with proton pump inhibitors. When using high doses of methotrexate, stop taking omeprazole temporarily.

The effect of drugs on the pharmacokinetics of omeprazole In the metabolism of omeprazole, isozymes participate CYP2C19 and CYP3A4. The combined use of omeprazole and isozyme inhibitors CYP2C19 and CYP3A4, such as clarithromycin, erythromycin and voriconazole, can lead to an increase in the concentration of omeprazole in the blood plasma by slowing the metabolism of omeprazole. The combined use of omeprazole and voriconazole results in a more than two-literacy AUC omeprazole. In connection with the good tolerability of high doses of omeprazole, with a short joint use of these drugs does not require a correction of the dose of omeprazole.Medicines that induce isoenzymes CYP2C19 and CYP3A4, such as, rifampicin and preparations of St. John's wort perfumed, when combined with omeprazole may lead to a decrease in its concentration in the blood plasma due to the acceleration of the metabolism of the drug. The simultaneous administration of omeprazole with amoxicillin or metronidazole does not affect the concentration of omeprazole in the blood plasma.

Special instructions:

In the presence of any anxiety symptoms (for example, such as significant spontaneous weight loss, repeated vomiting, dysphagia, vomiting with a trace of blood or melena), and if there is a stomach ulcer (or suspected gastric ulcer), the presence of malignant neoplasm, t .to. treatment with omeprazole, masking the symptoms, can delay the formulation of the correct diagnosis.

It is not recommended to use omeprazole together with such drugs as atazanavnar and nelfinavir.

Based on the results of the studies, the pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance

a dose of 75 mg / day) and omeprazole (80 mg / day inside),which leads to a decrease in exposure to the active metabolite of clopidogrel on average by 46% and a decrease in the maximum inhibition of ADP-induced platelet aggregation by an average of 16%. Therefore, simultaneous use of omeprazole and clopidogrel should be avoided (see section "Interaction with other drugs"). Separate observational studies indicate that proton pump inhibitor therapy may slightly increase the risk of osteoporotic fractures. However, in other similar studies, there was no increase in risk. In randomized, double-blind, controlled clinical trials of omeprazole and esomeprazole, including two open trials with a duration of therapy of more than 12 years, the connection of fractures against osteoporosis with proton pump inhibitors was not confirmed. Although the causal relationship between the use of omeprazole / esomeprazole with fractures against osteoporosis is not established, patients with a risk of developing osteoporosis or a fracture against it should be under appropriate clinical supervision.

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

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 20 mg.

Packaging:

7 capsules per contour cell package.

For 7 or 10 capsules in a contour non-cellular package made of aluminum foil.

10, 14 or 28 capsules in cans of polymer with drying agent.

1, 2,3 or 4 contour packs or one jar along with the instructions for use are placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

2 of the year. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000770 / 01

Date of registration:20.09.2007

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Representation: & nbspPHARMSTANDART JSC PHARMSTANDART JSC Russia

Information update date: & nbsp06.08.2015

Illustrated instructions

Instructions

Gastrozole® (Gastrozol®)