Active substanceMetoprololMetoprolol
Similar drugsTo uncover
  • Betaloc®
    pills inwards 
    AstraZeneca AB     Sweden
  • Betaloc®
    solution in / in 
    AstraZeneca AB     Sweden
  • Betalok® ZOK
    pills inwards 
    AstraZeneca AB     Sweden
  • Corvitol® 100
    pills inwards 
    Berlin-Chemie, AG     Germany
  • Corvitol® 50
    pills inwards 
    Berlin-Chemie, AG     Germany
  • Metocard®
    pills inwards 
  • Metocor Adipharm
    solution in / in 
    Adifarm, EAD     Bulgaria
  • Metocor Adipharm
    pills inwards 
    Adifarm, EAD     Bulgaria
  • Metoprolol
    pills inwards 
    AVEKSIMA, JSC     Russia
  • Metoprolol
    pills inwards 
  • Metoprolol
    pills inwards 
    MARBIOFARM, OJSC     Russia
  • Metoprolol
    pills inwards 
    OZONE, LLC     Russia
  • Metoprolol
    pills inwards 
    OZONE, LLC     Russia
  • Metoprolol
    pills inwards 
  • Metoprolol
    pills inwards 
  • Metoprolol
    pills inwards 
    Hemofarm AD     Serbia
  • Metoprolol
    solution in / in 
  • Metoprolol Zentiva
    pills inwards 
    Zentiva as.     Czech Republic
  • Metoprolol Organica
    pills inwards 
    ORGANICS, JSC     Russia
  • Metoprolol-OBL
    pills inwards 
  • Metoprolol-Acrychin
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
  • Metoprolol-CRC
    pills inwards 
  • Metoprolol-Teva
    pills inwards 
  • Serdol
    pills inwards 
  • Egilok®
    pills inwards 
  • Egilok® Retard
    pills inwards 
  • Egilok® С
    pills inwards 
  • Dosage form: & nbspTlong-acting aberrations covered with a film sheath.
    Composition:

    Each tablet contains:

    active substance: metoprolol tartrate 50 or 100 mg;

    Excipients: sugar grits [sucrose, molasses starch], macrogol 6000, talc, ethyl cellulose, triethyl citrate, giprolose, magnesium stearate, microcrystalline cellulose, silicon dioxide colloidal anhydrous, hypromellose, titanium dioxide (E 171).

    Description:

    White or almost white, biconvex, oblong tablet shape with a risk on both sides of the tablet.

    Pharmacotherapeutic group:beta1-blocker selective
    ATX: & nbsp

    C.07.A.B   Selective beta-blockers

    C.07.A.B.02   Metoprolol

    Pharmacodynamics:

    Metoprolol - cardioselective β1-adrenoblocker, does not have its own sympathomimetic activity and membrane-stabilizing properties.

    Mechanism of action

    Metoprolol suppresses the effect of increased activity of the sympathetic system on the heart, and also causes a rapid decrease in heart rate and cardiac output.

    With arterial hypertension metoprolol lowers arterial pressure (BP) in patients in a standing and lying position. The prolonged antihypertensive effect of the drug is associated with a gradual decrease in the total peripheral vascular resistance.

    With a single and short-term multiple intake metoprolol reduces the activity of renin plasma, which is due to the suppression of renal β1adrenoreceptors, which leads to a decrease in the production of renin and, accordingly, the reduction of angiotensin mediated vasoconstriction.

    With arterial hypertension, prolonged use of metoprolol leads to a statistically significant decrease in the mass of the left ventricle.

    Like other beta-blockers, metoprolol reduces the need for myocardium in oxygen by reducing systemic blood pressure, heart rate and heart contractility. By decreasing the heart rate (heart rate) and the corresponding diastole lengthening, metoprolol improves blood supply and oxygenation of areas of the myocardium with disturbed blood flow. Therefore, the drug reduces the frequency of attacks of angina and increases the physical performance of patients.

    After admission after myocardial infarction metoprolol reduces the risk of repeated myocardial infarction.

    In therapeutic doses, peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than those of nonselective beta-blockers.

    Compared with non-selective beta-blockers metoprolol less impact on insulin production and carbohydrate metabolism. It does not significantly change cardiovascular reactions to hypoglycemia and does not increase the duration of hypoglycemic episodes.

    Pharmacokinetics:

    Metoprolol is absorbed almost completely (approximately 95%) in the gastrointestinal tract. However, after absorption metoprolol is largely exposed to the metabolism of the "first pass" through the liver. Bioavailability is approximately 35%.

    The curve of the dependence of the concentration in the blood plasma on time has the features typical for sustained-release preparations. During 4-6 hours after taking the slow-absorption phase passes into a roughly 6-hour plateau (Cmah - 37.4 ng / ml after the administration of a single dose and 54.7 ng / ml in the equilibrium state), followed by the slow elimination phase.

    Half-life (t1/2) is 6-12 hours, which is much more than the half-life of metoprolol (approximately 3 hours). A longer half-life can be explained by delayed absorption.

    Since the metabolism of the drug is carried out by polymorphic enzymes, its level in the blood plasma has significant (up to 17-fold) differences in different patients.

    The connection with plasma proteins is 10%.

    Metoprolol is well distributed in tissues and has a high volume of distribution (5.5 l / kg). Pharmacokinetics of metoprolol is linear up to a dose of 800 mg. With multiple admission, the area under the pharmacokinetic curve (AUC) increases by about 20%.

    Metoprolol is metabolized in the liver by cytochrome P-450 enzymes.

    The drug is excreted mainly through the kidneys (approximately 95%). About 10% of the administered dose of metoprolol is excreted unchanged.

    Metabolites (O-desmethylmethoprolol and α-hydroxymethoprolol) do not possess beta-adrenoblocking activity. They are excreted with bile.

    It is not removed during hemodialysis.

    Patient treatment with decreased renal function does not require correction of the dose of the drug.

    Impaired liver function slows the metabolism of metoprolol, and in cases of insufficient liver function the dose of the drug should be reduced.

    Indications:

    - Arterial hypertension (as a monotherapy or (if necessary) in combination with other antihypertensive drugs);

    - Chronic heart failure in the stage of compensation (in combination with standard therapy with diuretics, ACE inhibitors and cardiac glycosides);

    - Ischemic heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks;

    - hyperkinetic cardiac syndrome, tachycardia;

    - Prevention of cardiac arrhythmias, especially supraventricular tachycardia and ventricular tachycardia caused by adrenergic-dependent lengthening of the interval QT;

    - hyperthyroidism (complex therapy);

    - prevention of migraine attacks.

    Contraindications:

    - Hypersensitivity to metoprolol and / or any other component of the drug. atrioventricular blockade (AV) II and III degrees;

    - sinoatrial (SA) blockade;

    - heart failure in the stage of decompensation;

    - Prinzmetal angina;

    - pronounced bradycardia (heart rate less than 50 beats per minute);

    - arterial hypotension;

    - syndrome of weakness of the sinus node;

    - cardiogenic shock;

    - severe disturbances of peripheral arterial blood flow;

    - simultaneous administration of monoamine oxidase inhibitors (MAO) or simultaneous intravenous administration of verapamil (see section "Interaction with other drugs");

    - Lactation period (see the section "Pregnancy and lactation period");

    - Due to the limited clinical data, the use of the drug is contraindicated in myocardial infarction under the following conditions: heart rate less than 45 beats / min, interval PQ exceeds 0.24 s, systolic blood pressure less than 100 mm Hg, severe heart failure and an atrioventricular block of II or III degree;

    - age under 18 years (efficiency and safety not established).

    Carefully:

    Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), obliterating peripheral vascular diseases (intermittent claudication, Raynaud's syndrome), chronic renal and / or hepatic insufficiency, myasthenia gravis, pheochromocytoma, AV blockade of the 1st degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, advanced age, fructose intolerance, glucose-galactose absorption disorders, sugarase / isomaltase insufficiency (see section "Special instructions").

    Pregnancy and lactation:

    In the absence of controlled clinical trials in pregnant and lactating women, Egiloc® Retard can be prescribed during pregnancy only on strict indications taking into account the benefit / risk ratio (in connection with the possibility of developing fetal bradycardia, arterial hypotension, hypoglycemia).At the same time, careful monitoring is carried out, especially for fetal development. Treatment should be interrupted for 48-72 hours before childbirth. In cases where this is not possible, it is necessary to provide observation of newborns within 48-72 hours after delivery.

    Effect of Egiloc® Retard on Newborn when breastfeeding not studied, so women taking the drug, it is recommended to stop breastfeeding.

    Dosing and Administration:

    Tablets are taken once a day, in the morning, without liquid, squeezed with liquid. Tablets can be taken regardless of food intake. If necessary, the tablet can be broken in half. In order to prevent bradycardia, the dose is selected individually and increased gradually.

    Arterial hypertension: the recommended initial dose is 50 mg once a day. If the therapeutic effect is insufficient, the daily dose can be increased to 100 mg or 200 mg, or add another antihypertensive agent.

    The maximum daily dose is 200 mg.

    Angina pectoris: the recommended initial dose for angina is 50 mg once a day.

    If the therapeutic effect is insufficient, the daily dose can be increased to 100 mg or 200 mg, or another antianginal agent can be added.

    Secondary prevention of myocardial infarction: the usual maintenance dose is 200 mg once a day.

    Heart failure in the compensation stage: the recommended initial dose is 25 mg once a day. After two weeks, the daily dose can be increased to 50 mg, then two weeks to 100 mg and finally, two weeks to 200 mg.

    Arrhythmias: the usual dose is 50-200 mg once a day.

    Hyperthyroidism: the usual dose is 50-200 mg once a day.

    Functional disorders of cardiac activity, accompanied by tachycardia: the usual dose is 50-200 mg once a day.

    Preventing migraine attacks: 100-200 mg once a day.

    Elderly patients with renal insufficiency or patients on hemodialysis, dose adjustment is not required.

    Dysfunction of the liver affect the removal of metoprolol, and in connection with severe hepatic insufficiency should reduce the dose of the drug in accordance with the clinical condition of the patient.

    Side effects:

    The incidence of adverse reactions described below was determined as follows: very often (≥1 / 10), often (≥1 / 100, <1/10); sometimes (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000), including individual messages.

    From the central nervous system: very often (especially at the beginning of the course of treatment) there are: increased fatigue, weakness, dizziness and headache; sometimes: decreased concentration of attention, slowed down the speed of mental and motor reactions, sleep disturbances, drowsiness, insomnia, nightmarish dreams, depression, tremors, convulsions, anxiety. Rarely: excitability, anxiety, paresthesia in the extremities (in patients with "intermittent" lameness and Raynaud's syndrome). Very rarely: short-term memory loss confusion and hallucinations, muscle weakness, asthenia, myasthenia gravis.

    From the sense organs: rarely - reduced vision, reduced secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus, hearing loss.

    From the side of the cardiovascular system: often: excessive decrease in blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness), increased heart rate, sinus bradycardia; rarely: a decrease in myocardial contractility, the development of heart failure (edema, edema of the feet and / or lower legs, shortness of breath), heart rhythm disturbances, manifestation of angiospasm (increased peripheral circulatory disturbance, coldness of the lower extremities, Raynaud's syndrome), impaired myocardial conductivity ,cardialgia; very rarely - aggravation of pre-existing AV conduction disorders.

    From the digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea, in some cases - impaired liver function (dark urine, icteric sclera or skin, cholestasis), changes in taste.

    From the skin: increased sweating; rarely: rashes on the skin (exacerbation of psoriasis), skin hyperemia, exanthema, reversible alopecia; very rarely: photodermatosis, psoriasis-like skin reactions.

    Allergic reactions: urticaria, skin itching, rash.

    From the respiratory system: congestion of the nose, bronchospasm at the appointment in high doses (loss of selectivity and / or in predisposed patients), dyspnea.

    Laboratory indicators: very rarely: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of "liver" enzymes, hyperbilirubinemia.

    From the endocrine system: a decrease in the level of high-density lipoprotein cholesterol and an increase in the triglycerides level (along with the normal level of total cholesterol), hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), and hypothyroid status.

    Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

    Other: pain in the back or joints, weight gain, decreased libido and / or potency, with a sharp cessation of treatment - withdrawal syndrome (increased angina attacks, increased blood pressure).

    Overdose:

    Symptoms: severe depression of blood pressure, severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, arrhythmia, ventricular extrasystole, bronchospasm, syncope, cardiogenic shock in acute overdose, unconsciousness, coma, atrioventricular block (up to the development of complete transverse blockade and cardiac arrest ), cardialgia.

    The first symptoms of an overdose appear after 20 minutes - 2 hours after taking the drug. The above symptoms can worsen with simultaneous use of alcohol, antihypertensive drugs, quinidine and barbiturates.

    Treatment: intensive therapy and careful monitoring of the patient (parameters of blood circulation and respiration, kidney function, blood glucose level, serum electrolytes).

    If the drug is taken recently, its further absorption can be reduced by washing the stomach, stimulating vomiting and introducing activated charcoal.

    If there is a marked decrease in blood pressure, the patient should be in the Trendelenburg position; in case of excessive reduction in blood pressure, bradycardia and the threat of heart failure, intravenous beta-adrenostimulants should be injected with an interval of 2-5 minutes, until the desired effect is achieved or 0.5-2 mg of atropine sulfate is injected intravenously.

    In the absence of a sufficient effect, dopamine, dobutamine or norepinephrine (norepinephrine).

    As a follow-up, it is possible to prescribe 1-10 mg of glucagon, the formulation of an artificial pacemaker.

    Bronchospasm can be removed by intravenous injection of stimulants β2β-adrenoreceptors (e.g., terbutaline).

    Metoprolol is poorly excreted by hemodialysis.

    Interaction:

    It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive effect. A break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days.

    Simultaneous iv injection of verapamil may provoke cardiac arrest.

    When combined with antihypertensive drugs, diuretics, nitroglycerin, or blockers of "slow" calcium channels candevelop a sharp decrease in blood pressure (special caution is necessary when combined with prazosin); increased severity of heart rate reduction and inhibition of atrioventricular conduction, with metoprolol with verapamil, diltiazem, antiarrhythmics (amiodarone), reserpine, methyldopa, clonidine, guanfacin, general anesthetic agents and cardiac glycosides.

    Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of oppression of myocardial function and development of arterial hypotension.

    Simultaneous administration of nifedipine leads to a significant reduction in blood pressure.

    Beta-adrenostimulants, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blockage of prostaglandin synthesis by the kidneys) weaken the hypotensive effect.

    Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), sedative and hypnotic drugs increase the CNS depression.

    When combined with hypoglycemic agents for oral administration, a decrease in their effect is possible;with insulin - increased risk of hypoglycemia, increased its severity and lengthening, masking of some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

    If metoprolol and clonidine take simultaneously, then with the cancellation of metoprolol clonidine cancellation after a few days (due to the risk of the syndrome of "withdrawal").

    Inductors of microsomal liver enzymes (rifampicin, barbiturates) lead to increased metabolism of metoprolol, a decrease in the concentration of metoprolol in the blood plasma and a decrease in the effect. Inhibitors (cimetidine, oral contraceptives, phenothiazines) - increase the concentration in the blood plasma.

    Allergens used for immunotherapy or allergen extracts for skin tests when combined with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiopaque substances for intravenous administration increase the risk of developing anaphylactic reactions.

    Reduces the clearance of xanthine derivatives, especially with the initially elevated clearance of theophylline under the influence of smoking.

    Reduces the clearance of lidocaine, increases the concentration of lidocaine in the blood plasma.

    Strengthens and prolongs the effect of antidepolarizing muscle relaxants; prolongs the anticoagulant effect of coumarins.

    When combined with ethanol, the risk of a marked decrease in blood pressure increases and the inhibitory effect on the central nervous system is noted.

    When combined with ergot alkaloids, the risk of peripheral circulatory disorders increases.

    Special instructions:

    Control of patients taking beta-blockers includes regular monitoring of heart rate (heart rate) and blood pressure, glucose content in patients with diabetes mellitus. You should teach the patient how to calculate heart rate and instruct you about the need for medical consultation at a heart rate of less than 50 beats per minute. When taking the drug at a dose above 200 mg per day, cardioselectivity decreases.

    Chronic heart failure should be compensated before treatment begins and the condition of compensation should be maintained throughout the treatment.

    It is possible to increase the severity of reactions of hypersensitivity (against a background of a burdened allergic anamnesis) and the absence of the effect of the administration of usual doses of epinephrine (epinephrine).In patients taking the drug, anaphylactic shock can occur particularly hard.

    The drug can strengthen the existing bradycardia. In patients receiving beta-blockers, epinephrine (adrenaline) can raise blood pressure and cause (reflex) bradycardia; this reaction is less likely in the case of selective beta-blockers.

    The drug may increase the symptoms of peripheral circulatory disorders.

    If it is necessary to prescribe a preparation for a patient with bronchial asthma, simultaneous application of β2-adrenostimulants (dose change of previously used β2- adrenostimulants).

    If necessary, the appointment of a patient with pheochromocytoma should be prescribed by alpha-blockers.

    Reception of the drug may mask some clinical manifestations of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.

    With angina pectoris, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats / min.

    In smokers, the effectiveness of the drug may be lower.

    When prescribing a patient with diabetes mellitus, it is necessary to more often monitor the parameters of carbohydrate metabolism and, if necessary, adjust the dose of insulin and hypoglycemic agents for oral administration. In diabetes mellitus can mask tachycardia caused by hypoglycemia. Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.

    Drugs that reduce catecholamine stocks (for example, reserpine), may increase the effect of the drug Egilok® Retard, so patients taking such combinations of drugs should be under constant monitoring of the doctor for the detection of excessive reduction in blood pressure and bradycardia.

    Patients with severe renal failure are advised to monitor kidney function (1 every 4-5 months).

    Bioavailability of metoprolol may increase with cirrhosis of the liver.

    In elderly patients, it is recommended to regularly monitor liver function. Correction of the dosing regimen is required only if elderly patients experience an increasing bradycardia (less than 50 beats per minute)a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction, and sometimes treatment should be discontinued.

    Special monitoring should be carried out on the condition of patients with depressive disorders taking the drug; in the case of development of depression, it is recommended to stop therapy.

    Patients using contact lenses should take into account that, against the background of drug treatment, tear production can be reduced.

    Before any surgical operation, the anesthetist should be warned that the patient is taking Egiloc® Retard. Cancellation of the drug should be performed at least 48 hours before surgery, except in special cases, such as thyrotoxicosis or pheochromocytoma. In cases where withdrawal of the drug before surgery is not possible, you should choose a means for general anesthesia with minimal negative inotropic action.

    With combined therapy with clonidine, administration of the latter should be discontinued several days after the withdrawal of the drug Egilok® Retard, in order to avoid a hypertensive crisis.

    With a sharp cessation of treatment, there may be a "cancellation" syndrome (increased angina attacks, increased blood pressure), so the drug is canceled gradually, reducing the dose within 10 days. Particular attention should be paid to patients with angina when removing the drug.

    Taking into account that the preparation contains sucrose, it is not recommended to appoint it to patients with intolerance to fructose, impaired absorption of glucose-galactose, and also with insufficiency of sucrose / isomaltase.

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

    During the treatment period, care must be taken when driving motor vehicles and taking other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets of prolonged action, film-coated, 50 mg and 100 mg.

    Packaging:

    For 10 tablets in a blister of PP film and aluminum foil.

    1, 2 or 3 blisters together with instructions for use in a cardboard box.

    Storage conditions:At a temperature of no higher than 30 ° C.
    Keep out of the reach of children.
    Shelf life:

    5 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N015121 / 01
    Date of registration:17.06.2008 / 28.01.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Manufacturer: & nbsp
    Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Information update date: & nbsp25.07.2016
    Illustrated instructions
      Instructions
      Up