Ortanol, 40 mg 28 pcs.

Omeprazole is an H⁺,K⁺-ATPase inhibitor.

Pharmacodynamics

Omeprazole inhibits the enzyme H⁺/ K⁺-ATPase (“proton pump”) in the parietal cells of the stomach and thereby blocks the final stage of hydrochloric acid secretion. This leads to a decrease in basal and stimulated secretion, regardless of the nature of the stimulus.

After a single oral dose, the effects of omeprazole occur within the first hour and last for 24 hours. Maximum effect is reached after 2 hours. After discontinuation of the drug secretory activity is fully restored after 3-5 days.

Pharmacokinetics

Omeprazole is rapidly absorbed from the gastrointestinal tract, C_max in plasma is reached after 0.5-3.5 h. Bioavailability is 30-40%. The binding to plasma proteins is about 95%.

Omeprazole is almost completely metabolized in the liver with the isoenzyme CYP2C19 to form 6 pharmacologically inactive enzymes. T_1/2 is 0.5-1 h.

It is excreted as metabolites by the kidneys (70-80%) and in the bile (20-30%).

In patients with hepatic insufficiency bioavailability increases significantly, T_1/2 increases up to 3 h.

In elderly patients, the elimination rate decreases and the bioavailability increases.

Indications

Symptoms of gastroesophageal reflux, such as heartburn, sour belching.

Active ingredient

Composition

1 capsule contains:

The active ingredient:

omeprazole 40 mg;

Associates:

Hyprolose low substituted;

MCC;

anhydrous lactose;

croscarmellose sodium;

povidone;

polysorbate 80;

Hypromellose phthalate; dibutylsebakat; talc;

Capsule shell:

Hypromellose; carrageenan; potassium chloride; titanium dioxide; iron (III) oxide yellow; iron (III) oxide red; water; ink for the inscription (iron (III) oxide black (E172), shellac, anhydrous ethanol, anhydrous isopropanol, propylene glycol, butanol, ammonium hydroxide, potassium hydroxide, purified water).

How to take, the dosage

Ingestion, before meals.

The initial dose is 20 mg (2 capsules) once daily. When symptoms begin to disappear, the dose may be reduced to 10 mg daily and increased again to 20 mg once daily if symptoms reappear. It may be necessary to take the drug for 3 to 4 days to achieve relief of symptoms.

The maximum daily dose of the drug should not exceed 20 mg.

The lowest effective dose should always be used. The maximum course of treatment is 14 days. The interval between 14-day courses of treatment without consulting a physician should be at least 4 months.

If within 2 weeks there is no relief of symptoms or they worsen, you should see your doctor.

The capsule should be swallowed whole with plenty of fluid. If the patient is unable to swallow the Ortanol® capsule whole, the contents may be dissolved in a small amount of water or fruit juice (do not dissolve in carbonated beverages). The resulting solution of the drug should be drunk immediately after preparation, with an additional 1/2 cup of water.

Patients with impaired renal function: No dose adjustment is necessary.

Patients with impaired liver function: Consult a physician before use.

Elderly patients: although the metabolic rate of omeprazole is decreased in elderly patients, no dose adjustment is necessary with a daily dose of 20 mg or less.

Interaction

A physician should be consulted before taking Ortanol® when treating one or more of the drugs listed in this section.

Concomitant use with omeprazole may result in increased or decreased absorption of drugs whose bioavailability is largely determined by gastric acidity (including erlotinib, ketoconazole, itraconazole, iron preparations and cyanocobalamin).

Concomitant use with omeprazole may significantly decrease the plasma concentration of atazanavir. Simultaneous use is possible only if prescribed by a physician (dosage and regimen of atazanavir are corrected if necessary).

The bioavailability of digoxin in concomitant use with omeprazole increases by 10% (dosing regimen of digoxin may need to be adjusted). Caution should be exercised when concomitant use of these drugs in elderly patients.

In concomitant use of omeprazole with clopidogrel a decrease in the antiaggregant effect of the latter is observed.

Concomitant use with omeprazole may increase plasma concentrations and increase T1/2 of warfarin, cilostazol, diazepam, phenytoin and other drugs metabolized in the liver by CYP2C19 isoenzyme (dose reduction of these drugs may be required).

The concomitant use of Omeprazole increases the plasma concentration of tacrolimus, which may require dose adjustment.

Concomitant use of omeprazole increases plasma concentrations of saquinavir/ritonavir up to 70%, and tolerability in patients with HIV infection is not impaired.

Simultaneous use with CYP2C19 and CYP3A4 isoenzyme inhibitors (such as clarithromycin, voriconazole) may lead to increased plasma concentrations of omeprazole, which may require adjustment of the omeprazole dose in patients with severe hepatic impairment if used long-term.

The inducers of CYP2C19 and CYP3A4 isoenzymes (e.g., rifampicin, preparations of Hypericum perforatum) may increase metabolism of omeprazole, thereby reducing its plasma concentration.

No clinically significant interaction of omeprazole with antacids, theophylline, caffeine, quinidine, lidocaine, propranolol, metoprolol, ethanol has been established.

Special Instructions

Omeprazole is not indicated for occasional heartburn (heartburn less than 2 times a week).

Before starting therapy with omeprazole, it is important to rule out the presence of a malignancy, because treatment, by masking symptoms, can delay a correct diagnosis.

Omeprazole will decrease gastric acidity, which may slightly increase the risk of digestive tract infections.

Impact on ability to drive vehicles and perform other activities requiring high concentration and rapid psychomotor reactions

Dizziness, drowsiness, visual disturbances may occur during treatment with omeprazole, so caution should be exercised when driving motor vehicles and performing other potentially hazardous activities requiring high concentration and rapid psychomotor reactions.

Special precautions for disposal of unused drug. Not required.

Contraindications

With caution: Your physician should be consulted before using:

You should also consult your physician before using Ortanol® during pregnancy and lactation.

The drug should not be used for prophylactic purposes.

Side effects

Allergic reactions: infrequent – urticaria, skin rash, itching; rare – fever, angioedema, anaphylactoid reactions; very rare – eosinophilia.

Gastrointestinal disorders: frequently – nausea, vomiting, abdominal pain, diarrhea or constipation, flatulence; infrequently – increased transaminase and ALP activity; rarely – dry mouth, stomatitis, gastrointestinal candidiasis, hepatitis (with or without jaundice); very rarely – liver failure (in patients with previous severe liver disease).

Nervous system: frequently – headache; infrequently – dizziness, paresthesia, somnolence, insomnia; rarely – agitation, reversible confusion, depression, violation of taste; very rarely – aggression, hallucinations; against severe liver disease – encephalopathy.

Skin disorders: infrequent dermatitis, photosensitization, alopecia, very rare erythema multiforme, Stevens-Johnson syndrome (severe erythema multiforme characterized by spots and blisters on the skin and mucous membranes with fever and pain in the joints), toxic epidermal necrolysis.

Sensory organs: rarely – visual impairment.

Musculoskeletal system: rare – myalgia, arthralgia, very rare – muscle weakness.

Respiratory system: rare – bronchospasm.

The urinary system: rarely – interstitial nephritis.

Hematopoietic organs: rare – leukopenia, thrombocytopenia; very rare – agranulocytosis, pancytopenia.

Others: infrequent peripheral edema; rare – increased sweating, hyponatremia; very rare – hypomagnesemia, gynecomastia.

Overdose

Symptoms: dry mouth, nausea, vomiting, increased sweating, headache, drowsiness, confusion, visual disturbances, tachycardia.

Treatment: symptomatic. There is no specific antidote. Hemodialysis is ineffective.

Pregnancy use

The results of three prospective epidemiological studies (more than 1000 observations) have shown that the use of omeprazole in pregnant women has no adverse effect on pregnancy and fetal/newborn health. However, it is recommended that a physician be consulted before using the drug during pregnancy.

Omeprazole penetrates into the breast milk. If it is necessary to use the drug during lactation, discontinuation of breastfeeding should be decided.

Similarities