Omeprazol-Teva, 20 mg 28 pcs

Indications

For adults:

peptic ulcer of the stomach and duodenum (treatment and prevention);
eradication of Helicobacter pylori for gastric and duodenal ulcers (as part of combination therapy);
NSAID-associated ulcers and erosions of the stomach and duodenum (treatment and prevention);
reflux esophagitis; symptomatic gastroesophageal reflux disease (GERD);
dyspepsia associated with high acidity;
Zollinger-Ellison syndrome.

Children over 2 years old:

reflux esophagitis, symptomatic treatment of heartburn and sour belching with GERD in children over 2 years of age and weighing ≥ 20 kg;

Children over 4 years old:

eradication of Helicobacter pylori in duodenal ulcer (as part of combination therapy).

Pharmacological effect

Pharmacotherapeutic group: gastric gland secretion reducing agent – proton pump inhibitor

ATX code: A02BC01

Pharmacological properties

Pharmacodynamics

Omeprazole is a racemic mixture of two enantiomers that reduces the secretion of hydrochloric acid due to specific inhibition of the proton pump of gastric parietal cells. With a single use, it acts quickly and has a reversible inhibition of hydrochloric acid secretion.

Mechanism of action

Omeprazole is a weak base, it becomes active in the acidic environment of the tubules of the cells of the parietal layer of the gastric mucosa, where it is activated and inhibits the H+/K+-ATPase of the proton pump. It has a dose-dependent effect on the last stage of hydrochloric acid synthesis, inhibits both basal and stimulated secretion, regardless of the stimulating factor.

Effect on the secretion of hydrochloric acid in the stomach

After oral administration of omeprazole once a day, there is a rapid and effective decrease in daytime and nighttime secretion of hydrochloric acid, which reaches a maximum within 4 days of treatment.

In patients with duodenal ulcer, 20 mg omeprazole causes a sustained reduction in 24-hour gastric acidity by at least 80%. In this case, a 70% decrease in the average maximum concentration of hydrochloric acid after stimulation with pentagastrin is achieved within 24 hours. Daily oral administration of 20 mg omeprazole in patients with duodenal ulcer maintains acidity at pH ≥3 for an average of 17 hours.

The degree of inhibition of hydrochloric acid secretion is proportional to the area under the concentration-time curve (AUC) of omeprazole and is not proportional to the actual concentration of the drug in the blood at a given time. No tachyphylaxis was observed during treatment with omeprazole.

Omeprazole in vitro has a bactericidal effect on Helicobacter pylori. Eradication of Helicobacter pylori when using omeprazole in conjunction with antibacterial agents is accompanied by rapid elimination of symptoms, a high degree of healing of defects in the mucous membrane of the gastrointestinal tract and long-term remission of peptic ulcer disease, which reduces the likelihood of complications such as bleeding, and is as effective as continuous maintenance therapy.

Pharmacokinetics

Suction. Omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum concentration in plasma is reached after 1-2 hours. Absorbed in the small intestine, usually within 3-6 hours. Bioavailability after a single oral dose is approximately 40%; after continuous once-daily dosing, bioavailability increases to 60%. Concomitant food intake 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 are CYP2C19 and CYP3A4. Hydroxyomeprazole is the main metabolite formed under the action of the CYP2C19 isoenzyme. Metabolites sulfone and sulfide do not affect the secretion of hydrochloric acid.

Excretion. The half-life is approximately 40 minutes (30-90 minutes). About 80% is excreted in the form of metabolites by the kidneys, the rest through the intestines.

Special groups of patients. In elderly patients (75-79 years old), a slight decrease in the metabolism of omeprazole was noted.

In patients with impaired renal function, no dose adjustment is required. The metabolism of omeprazole in patients with impaired liver function slows down, which leads to an increase in its bioavailability.

When treating children aged 1 year, plasma concentrations of omeprazole were similar to those in adults.

Special instructions

Before starting therapy, it is necessary to exclude the presence of a malignant process in the upper gastrointestinal tract, because Taking Omeprazole-Teva may mask symptoms and delay the correct diagnosis. Reducing gastric acidity, including when using proton pump blockers, increases the number of bacteria in the gastrointestinal tract, which increases the risk of gastrointestinal infections.

Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. Increased concentrations of CgA may affect 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 CgA concentration test.

In patients with severe liver dysfunction, it is necessary to regularly monitor liver enzymes during therapy with Omeprazole-Teva.

The drug Omeprazole-Teva contains sucrose and is therefore contraindicated in patients with congenital disorders of carbohydrate metabolism (fructose intolerance, sucrase/isomaltase deficiency, glucose-galactose malabsorption).

When treating erosive and ulcerative lesions associated with NSAID use, the possibility of limiting or discontinuing NSAID use should be carefully considered to increase the effectiveness of antiulcer therapy.

The drug contains sodium, which should be taken into account in patients on a controlled sodium diet.

The risk-benefit ratio of long-term (more than 1 year) maintenance therapy with Omeprazole-Teva should be regularly assessed. There is evidence of an increased risk of fractures of the vertebrae, wrist bones, and head of the femur, mainly in elderly patients, as well as in the presence of predisposing factors. Patients at risk of developing osteoporosis should ensure adequate intake of vitamin D and calcium.

There are reports of the occurrence of severe hypomagnesemia in patients receiving therapy with proton pump inhibitors, including omeprazole, for more than 1 year.

Patients receiving omeprazole therapy for a long time, especially in combination with digoxin or other drugs that reduce the level of magnesium in the blood plasma (diuretics), require regular monitoring of magnesium levels.

Omeprazole, like all drugs that reduce acidity, can lead to decreased absorption of vitamin B12 (cyanocobalamin). This must be remembered in patients with a reduced supply of vitamin B12 in the body or with risk factors for impaired absorption of vitamin B12 during long-term therapy.

In patients who took drugs orally for a long time that reduce the secretion of gastric glands, the formation of glandular cysts in the stomach was more often observed. These phenomena are caused by physiological changes as a result of inhibition of hydrochloric acid secretion, and undergo reverse development as therapy continues.

A decrease in the secretion of hydrochloric acid in the stomach leads to an increase in the growth of normal intestinal microflora, which, in turn, can lead to a slight increase in the risk of developing intestinal infections caused by bacteria of the genus Salmonella spp. and Campylobacter spp., as well as probably Clostridium difficile.

Impact on the ability to drive vehicles and machinery

Considering the possibility of undesirable effects on the central nervous system and the organ of vision, during treatment with omeprazole, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Omeprazole

Composition

1 capsule contains: active ingredient omeprazole 20.00 mg;

excipients: granulated sugar [sucrose, starch syrup] 86.98 mg, sodium carboxymethyl starch type A 5.10 mg, sodium lauryl sulfate 6.07 mg, povidone-K30 9.66 mg, sodium phosphate dodecahydrate 0.67 mg, sodium hydroxide 0.14 mg, hypromellose 14.42 mg, methacrylic acid and ethyl acrylate copolymer [1:1] 42.53 mg, triethyl citrate 6.17 mg, titanium dioxide (E 171) 3.31 mg, talc 0.19 mg.

Gelatin capsule: cap: titanium dioxide (E 171) 0.48-0.504 mg, water 3.48-3.654 mg, gelatin 20.04-23.912 mg; body: titanium dioxide (E 171) 0.732-0.78 mg, water 5.481-5.655 mg, gelatin 31.563-35.868 mg.

Pregnancy

Research results indicate no adverse effects on the course of pregnancy, the health of the fetus and newborn child. Omeprazole can be used with caution during pregnancy.
Omeprazole is excreted in breast milk. However, when used in therapeutic doses, the effect on a child is unlikely.

Contraindications

Hypersensitivity to omeprazole or any of the components of the drug; fructose intolerance; sucrase/isomaltase deficiency; glucose-galactose malabsorption; simultaneous use with clarithromycin (in patients with liver failure), atazanavir, St. John’s wort, erlotinib, posaconazole.

Children over 2 years of age for indications other than reflux esophagitis and symptomatic gastroesophageal reflux disease; children over 4 years of age for indications other than reflux esophagitis, symptomatic gastroesophageal reflux disease and duodenal ulcer caused by Helicobacter pylori. Children under 18 years of age (for all indications, except for reflux esophagitis and eradication of Helicobacter pylori in duodenal ulcer).

With caution

Liver failure; renal failure; osteoporosis; simultaneous use with clarithromycin, simultaneous use with clopidogrel, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, voriconazole, rifampicin, use with digoxin, St. John’s wort preparations; significant spontaneous loss of body weight; repeated vomiting, vomiting blood; swallowing disorder; change in stool color (tarry stool); and also in the presence of a stomach ulcer (or if its presence is suspected), a malignant neoplasm should be excluded before starting treatment, since treatment can lead to masking of symptoms and delay the correct diagnosis.

Side Effects

The frequency of side effects is classified in accordance with the recommendations of the World Health Organization: very often – at least 10%; often – at least 1%, but less than 10%; infrequently – not less than 0.1%, but less than 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely (including isolated cases) – less than 0.01%.

From the blood and lymphatic system: rarely – hypochromic microcytic anemia in children; very rarely – reversible thrombocytopenia, leukopenia, pancytopenia, agranulocytosis.

From the immune system: very rarely – rash, fever, angioedema, bronchospasm, allergic vasculitis, fever, anaphylactic reactions/shock.

From the nervous system: often – headache, drowsiness, lethargy (the listed side effects tend to worsen with long-term therapy); infrequently – insomnia, dizziness; rarely – paresthesia, confusion, hallucinations, especially in elderly patients or in severe cases of the disease; very rarely – anxiety, depression, especially in elderly patients or in severe cases of the disease.

From the side of the organ of vision: infrequently – visual disturbances, incl. decrease in visual fields, decrease in the acuity and clarity of visual perception (usually disappear after cessation of therapy).

From the organ of hearing and labyrinthine disorders: infrequently – vertigo, disorders of auditory perception, incl. “ringing in the ears” (usually disappears after cessation of therapy).

From the gastrointestinal tract: often – nausea, vomiting, flatulence, constipation, diarrhea, abdominal pain (in most cases, the severity of these phenomena increases with continued therapy), glandular polyps of the fundus of the stomach (benign); rarely – taste disturbance, change in color of the tongue to brown-black and the appearance of benign cysts of the salivary glands when used simultaneously with clarithromycin (the phenomena are reversible after cessation of therapy), microscopic colitis; very rarely – dry mouth, stomatitis, candidiasis, pancreatitis.

From the liver and biliary tract: infrequently – changes in the activity of “liver” enzymes (reversible); very rarely – hepatitis, jaundice, liver failure, encephalopathy in patients with underlying liver diseases.

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

From the musculoskeletal and connective tissue side: infrequently – fractures of the vertebrae, wrist bones, femoral head (see section “Special instructions”); rarely – myalgia, arthralgia; very rarely – muscle weakness.

From the kidneys and urinary tract: rarely – interstitial nephritis.

General disorders and disorders at the injection site: infrequently – peripheral edema (usually disappears after cessation of therapy); rarely – hyponatremia; very rarely – gynecomastia; frequency unknown – hypomagnesemia (see section “Special instructions”).

Interaction

Active substances with pH-dependent absorption

Reducing the acidity of gastric juice when using omeprazole can increase or decrease the absorption of pharmacologically active substances.

Nelfinavir, atazanavir

When used concomitantly with omeprazole, a significant decrease in plasma concentrations of atazanavir and nelfinavir may be observed.

The simultaneous use of omeprazole and nelfinavir is contraindicated. Concomitant use of omeprazole (40 mg daily) reduces nelfinavir exposure by approximately 40%, and mean exposure to the pharmacologically active metabolite M8 is reduced by 75-90%. The interaction may involve a mechanism of CYP1C19 inhibition. Concomitant use of omeprazole with atazanavir is not recommended. Coadministration of omeprazole (40 mg daily) and atazanavir 300 mg/ritonavir 100 mg in healthy volunteers resulted in a 75% reduction in atazanavir exposure. Increasing the atazanavir dose to 400 mg does not compensate for the effect of omeprazole on atazanavir exposure. Administration of 20 mg omeprazole per day with 400 mg atazanavir and 100 mg ritonavir to healthy volunteers resulted in an approximately 30% reduction in atazanavir exposure and was comparable to exposure with a single dose of 300 mg atazanavir and 100 mg ritonavir.

Digoxin

Concomitant treatment with omeprazole (20 mg daily) and digoxin in healthy volunteers increased the bioavailability of digoxin by 10%. Although glycoside toxicity with omeprazole is not a common event, increased monitoring is necessary, especially when treating elderly patients.

Clopidogrel

In a crossover clinical study, the duration of taking clopidogrel at a loading dose of 300 mg (75 mg per day) and the combination of clopidogrel with omeprazole at a dose of 80 mg was 5 days. Exposure to the active metabolite of clopidogrel was reduced by 46% (on day 1) and 42% (on day 5) when clopidogrel was coadministered with omeprazole. The mean time to platelet aggregation inhibition was reduced by 47% (24 hours) and 30% (day 5) when clopidogrel and omeprazole were co-administered. Another study showed that taking clopidogrel and omeprazole at different times did not prevent their interaction, which is likely due to the inhibitory effect of omeprazole on CYP2C19. Observational and clinical studies have provided conflicting data on the clinical impact of these PK/PD interactions on the development of severe cardiovascular events.

Other medicines

The absorption of posaconazole, erlotinib, ketaconazole and itraconazole is significantly reduced, and their clinical effectiveness is accordingly impaired. Avoid co-administration of omeprazole with posaconazole or erlotinib.

Medicines metabolized by the CYP2C19 isoenzyme

Omeprazole moderately inhibits CYP2C19, the main enzyme in the metabolism of omeprazole. Thus, the metabolism of other drugs also metabolized by CYP2C19 may be reduced and their systemic exposure increased. Examples of such drugs are R-warfarin and other vitamin K antagonists, cilostazol, diazepam and phenytoin.

Cilostazol

In a crossover clinical study, administration of omeprazole 40 mg to healthy volunteers increased the Cmax and AUC of cilostazol by 18% and 26%, respectively, and one of the active metabolites of cilostazol by 29% and 69%, respectively.

Phenytoin

Monitoring plasma concentrations of phenytoin is recommended during the first two weeks after initiation of omeprazole therapy and in case of dose adjustment of phenytoin; Monitoring and subsequent dose adjustment of phenytoin should be carried out until the end of treatment with omeprazole.

Unknown interaction mechanism

Saquinavir

Coadministration of omeprazole and saquinavir/ritonavir is well tolerated in HIV-infected patients and also results in a reduction in saquinavir plasma concentrations of approximately 70%.

Tacrolimus

Coadministration with omeprazole reduces the serum concentration of tacrolimus. Increased monitoring of tacrolimus concentrations and renal function (creatinine clearance) should be carried out, with tacrolimus dose adjustments if necessary.

The influence of other drugs on the pharmacokinetics of omeprazole

Inhibitors of the isoenzyme CYP2C19 and/or CYP3A4

Given the metabolism of omeprazole through the isoenzymes CYP2C19 and CYP3A4, drugs that can inhibit these enzymes (such as clarithromycin and voriconazole) may reduce the serum concentration of omeprazole, increasing the rate of its metabolism.

No effect on metabolism

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

No interaction of omeprazole with the following drugs has been identified: antacids, caffeine, theophylline, S-warfarin, piroxicam, diclofenac, naproxen, metoprolol, propranolol and ethanol.

Overdose

Symptoms: vomiting, abdominal pain, diarrhea, dizziness, depression, blurred vision, drowsiness, agitation, confusion, headache, increased sweating, dry mouth, nausea, arrhythmia.

Treatment: symptomatic therapy, hemodialysis is not effective enough. A specific antidote is not known.

Storage conditions

Store at a temperature not exceeding 25 ºС.
Keep out of the reach of children!

Shelf life

2 years.
Do not use after expiration date.

Manufacturer

Teva Pharma, S.L.U., Spain