Index of drugs

Hypertension. Ischemic heart disease. Treatment of symptomatic, chronic heart failure with impaired left ventricular function. Prevention of sudden cardiac death or reinfarction in patients after an acute phase of infarction. Cardiac arrhythmias, especially in the case of supraventricular tachycardia, ventricular extrasystole and atrial fibrillation (to slow down ventricular function). Functional heart disorder with paroxysmatic arrhythmias. Prophylaxis of migraine.

1 tabl sustained release contains 23.75 mg, 47.5 mg or 95 mg Metoprolol succinate (equivalent to 25 mg, 50 mg or 100 mg metoprolol tartrate).

A selective antagonist of ß receptors₁. The selectivity of the preparation depends on the dose. Thanks to the use of the ZOK form, we managed to reduce the maximum concentration of the drug in the blood, compared to traditional tablets. The use of this drug form increased the selectivity of the preparation relative to the ß receptors₁. Metoprolol has a slight stabilizing effect on the cell membrane. It has a negative inotropic and chronotropic effect. Metoprolol limits or inhibits the action of catecholamines released during exercise or stress on the heart muscle. In therapeutic doses, metoprolol has a much smaller effect on bronchial muscle contraction than non-selective beta-blockers. Can be used simultaneously with ß₂-mimetic agents in patients with asthma or symptoms of chronic obstructive pulmonary disease. To a lesser extent than non-selective beta-blockers affect the release of insulin and carbohydrate metabolism. In patients with hypertension, the product lowers blood pressure throughout the day, both in a standing position, lying down, as well as during exercise. In men with moderate or severe hypertension treated with Metoprolol, a reduction in the risk of sudden cardiac death was observed. No electrolyte disturbances were observed during treatment with metoprolol. In a clinical study in patients with heart failure (from NYHA groups II-IV) and decreased ejection fraction (≤40), an increase in patient survival and a reduction in the frequency of hospitalization were observed after administration of the formulation. During the long-term treatment with the preparation, an improvement in symptoms of heart failure was observed. In patients with arrhythmias with fast heart rate, metoprolol inhibits the stimulation of the sympathetic nervous system, thereby reducing the automatism of cells in the cardiac conduction system and the conduction time in the conductive system. It reduces the risk of re-infarction or sudden cardiac death in patients after myocardial infarction. After oral administration, the drug is completely absorbed throughout the gastrointestinal tract, including the colon. Bioavailability is 30-40%. The active substance is released in a controlled manner. The release does not depend on the pH of the intestinal juice and occurs at a constant rate for about 20 hours. The ZOK pharmaceutical form provides a constant concentration of metoprolol in plasma and efficacy for 24 hours after taking the drug. Metoprolol is metabolised in the liver, mainly by the CYP2D6 isoenzyme. Three main metabolites have been identified, none of which show clinically significant ß-blocking effects. About 5% of the administered dose is excreted in the urine in unchanged form, the remainder of the dose is excreted as metabolites.

Hypersensitivity to metoprolol or another β-blocker or other components of the preparation. Cardiogenic shock. Sick node syndrome. Atrio-ventricular block IIst. or III. Unstable, decompensated heart failure (pulmonary edema, organ ischaemia or low blood pressure). Short-term or long-term treatment with inotropic drugs, acting agonistically on ß-adrenergic receptors. Clinically important sinus bradycardia or hypotension.Suspicion of a recent myocardial infarction if the heart rate is less than 45 beats per minute, the PQ interval is longer than 0.24 s or the systolic pressure is less than 100 mmHg. Patients with heart failure whose systolic pressure remains below 100 mmHg should be re-examined before metoprolol treatment. Significant peripheral circulation disorders with the threat of gangrene.

Do not administer Verapamil intravenously to patients treated with beta-blockers. Metoprolol should be used with caution in patients with intermittent claudication, severe renal failure, and in severe general condition, if one of the symptoms is metabolic acidosis. Caution should be exercised when using metoprolol and digitalis preparations. Patients with Prinzmetal angina should not be treated with non-selective beta-blockers, and selective ß₁-adrenolytics should be used with extreme caution. In patients with bronchial asthma or other chronic obstructive pulmonary diseases, bronchodilators should be used together with the product (in some cases, it may be necessary to increase the dose of ß₂agonists). When administering to patients with pheochromocytoma, a concomitant use of an alpha-blocker should be considered. Clinical data on the safety and efficacy of treatment with patients with severe stable heart failure (NYHA Group IV) are limited. Treatment with the preparation in this group of patients should be started by doctors with extensive experience in the treatment of severe heart failure. In clinical trials for the treatment of heart failure, patients with symptoms of heart failure in the course of myocardial infarction and unstable ischemic heart disease were not eligible, there is no clinical data on the safety and efficacy of metoprolol treatment in this group of patients - the use of the preparation in unstable decompensated heart failure is contraindicated.

It must not be used during pregnancy unless clearly necessary. β-blockers can cause bradycardia in the fetus and newborn, which should be remembered when using these drugs in the third trimester of pregnancy and in the perinatal period. ß-blockers can cause bradycardia in a breast-fed child. Metoprolol passes into breast milk, however, the effect on a breast-fed child is insignificant clinically if the mother takes the preparation in therapeutic doses.

They occur in about 10% of patients treated with metoprolol; their onset and severity usually depends on the size of the dose. Side effects commonly occurring (> 1/100): tiredness, pain and dizziness, bradycardia, feeling cold in the peripheral limbs, palpitations, abdominal pain, nausea, vomiting, diarrhea or constipation. Uncommon (<1/100 and> 1/1000): chest pain, weight gain, transient worsening of heart failure, cardiogenic shock in patients with acute myocardial infarction, sleep disturbances, paresthesia, shortness of breath, bronchospasm in patients with bronchial asthma. Rarely (<1/1000 and> 1 / 10,000): excessive perspiration, hair loss, taste disturbances, transient libido disorders, thrombocytopenia, prolonged atrioventricular conduction time, arrhythmia, edema, fainting, nightmares, memory deficits , confusion, nervousness, anxiety, hallucinations, depression, skin hypersensitivity reactions, exacerbation of psoriasis symptoms, hypersensitivity to light, transaminase elevation, visual impairment, dryness or eye irritation, tinnitus. A single report concerned the occurrence of joint pain, hepatitis, muscle cramps, dry mouth, symptoms of conjunctivitis, rhinitis, concentration disorders and gangrene in patients with peripheral circulation disorders.

Orally. The product should be taken once a day, preferably in the morning. The dose of the preparation should be determined individually, the doses given below should be considered as recommended.Hypertensionthe recommended dose is 50-100 mg once a day; in patients who do not have sufficient 100 mg, another blood pressure-lowering medicine (preferably a diuretic or dihydropyridine-derived diuretic) may be added to the treatment or the dose may be increased.Ischemic heart diseaseThe recommended dose is 100-200 mg once a day, if necessary, the dose can be increased or added to the treatment with nitrate group drugs.Treatment of symptomatic, chronic heart failure: treatment can be started in patients with stable heart failure, the patient should not have exacerbations of heart failure in the last 6 weeks, and the basic treatment should not be changed in the last 2 weeks; after starting treatment of ß-blockers, transient exacerbation of symptoms may occur, in the case of exacerbation of symptoms in some patients it is possible to continue treatment with the same or reduced dose, in some patients discontinuation of the drug is necessary; treatment of severe heart failure (NYHA group IV) should be started by doctors with extensive experience in the treatment of severe heart failure. In patients with stable heart failure (NYHA class II), the recommended starting dose is 25 mg once a day, the starting dose should be used for the first 2 weeks of treatment, after which the dose can be increased to 50 mg once a day, the dose can be double every 2 weeks for a dose of 200 mg, for long-term treatment, the recommended dose is 200 mg once a day. In patients with stable heart failure (NYHA class III and IV), the recommended starting dose is 12.5 mg (1/2 tables 25 mg) once a day, the dose should be determined individually for each patient under close medical supervision; after 1-2 weeks, the dose may be increased to 25 mg once a day, after another 2 weeks, the dose may be increased to 50 mg once a day, in patients who tolerate well the dose may be doubled every subsequent 2 weeks maximum 200 mg once a day. In patients who develop bradycardia and / or hypotension, it may be necessary to reduce the dose of other medicines used to treat heart failure or reduce the dose.Prevention of sudden cardiac death and re-infarction in patients after an acute phase of infarctionThe recommended maintenance dose is 200 mg once a day.Heart arythmiaThe recommended dose is 100-200 mg once a day, if necessary, the dose can be increased.Functional heart disorder with paroxysmatic arrhythmiasThe recommended dose is 100 mg once a day, if necessary the dose can be increased.Prophylaxis of migraineThe recommended dose is 100-200 mg once a day.Children over 6 years of age.: initially 1 mg / kg, not more than 50 mg, once a day in the form of a tablet with a power similar to the estimated dose. If there is no clinical response, the dose may be increased to a maximum daily dose of 2 mg / kg. No studies on doses above 200 mg once a day have been performed in children and adolescents, and the efficacy and safety of metoprolol in children under the age of 6 years. The tablets can be divided in half. They should not be chewed or crushed. The tablets should be swallowed with at least half a glass of water.