Preparation: EGILOK ®
Active ingredient: METOPROLOL (METOPROLOL)
ATX code: C07AB02
KFG: Beta 1-blocker
Reg. number: P No. 015639/01
Date of registration: 29.12.06
The owner of the reg. acc.: EGIS PHARMACEUTICALS Plc (Hungary)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Tablets white or almost white, round, biconvex, with a cross-shaped dividing line and a double bevel on one side and an engraving "E435" on the other side, odorless.

Excipients:

Tablets white or almost white, round, biconvex, with a notch on one side and an engraving "E434" on the other side, odorless.

Excipients: microcrystalline cellulose, sodium carboxymethyl starch, anhydrous colloidal silicon dioxide, povidone, magnesium stearate.

30 pcs. - jars of dark glass (1) - packs of cardboard.
60 pcs. - jars of dark glass (1) - packs of cardboard.

Tablets white or almost white, round, biconvex, with a notch on one side and an engraving "E432" on the other side, odorless.

Excipients: microcrystalline cellulose, sodium carboxymethyl starch, anhydrous colloidal silicon dioxide, povidone, magnesium stearate.

30 pcs. - jars of dark glass (1) - packs of cardboard.
60 pcs. - jars of dark glass (1) - packs of cardboard.

The description of the drug is based on officially approved instructions for use and approved by the manufacturer for.

PHARMACHOLOGIC EFFECT

A cardioselective blocker of ?-adrenergic receptors that does not have internal sympathomimetic and membrane stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects.

Blocking in not high doses Oh? 1-adrenergic receptors of the heart, reduces the formation of cAMP from ATP stimulated by catecholamines, reduces intracellular Ca 2+ current, has a negative chrono-, dromo-, batmo- and inotropic effect (slows heart rate, inhibits conductivity and excitability, reduces myocardial contractility).

OPSS at the beginning of the use of the drug (in the first 24 hours after oral administration) increases, after 1-3 days of use it returns to its original level, with further use it decreases.

The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin system and the central nervous system, restoration of the sensitivity of the baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure at rest, during physical exertion and stress.

Blood pressure decreases after 15 minutes, maximum - after 2 hours; the effect persists for 6 hours. A stable decrease is observed after several weeks of regular intake.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening of diastole and improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the frequency and severity of angina attacks and increases exercise tolerance.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, an increase in cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV node) and along additional pathways.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional diseases heart and hyperthyroidism slows heart rate and can even lead to the restoration of sinus rhythm.

Prevents the development of migraine.

With long-term use, it reduces the content of cholesterol in the blood.

When used in average therapeutic doses, it has a less pronounced effect on organs containing? 2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi, uterus) and carbohydrate metabolism.

When used in high doses (more than 100 mg / day), it has a blocking effect on both subtypes of β-adrenergic receptors.

PHARMACOKINETICS

Suction

Rapidly and completely (95%) absorbed from the gastrointestinal tract. C max in plasma is achieved 1.5-2 hours after ingestion. Bioavailability is 50%. During treatment, bioavailability increases to 70%. Eating increases bioavailability by 20-40%.

Distribution

V d is 5.6 l / kg. Binding to plasma proteins - 12%. Penetrates through the BBB and the placental barrier. It is excreted in breast milk in small amounts.

Metabolism

Metoprolol is biotransformed in the liver. Metabolites do not have pharmacological activity.

breeding

T 1 / 2 averages 3.5-7 hours. Metoprolol is almost completely excreted in the urine in 72 hours. About 5% of the dose is excreted unchanged.

Pharmacokinetics in special clinical situations

With severe violations of liver function, the bioavailability and T 1/2 of metoprolol increases, which may require dose adjustment.

In case of impaired renal function, T 1/2 and systemic clearance of metoprolol do not change significantly.

INDICATIONS

Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs), incl. hyperkinetic type;

IHD (secondary prevention of myocardial infarction, prevention of angina attacks);

Cardiac arrhythmias (supraventricular arrhythmias, ventricular extrasystole);

Hyperthyroidism (as part of complex therapy);

Prevention of migraine attacks.

DOSING MODE

At arterial hypertension appoint a daily dose of 50-100 mg / day in 1 or 2 doses (morning and evening). With insufficient therapeutic effect, a gradual increase in the daily dose to 100-200 mg is possible.

At angina pectoris, supraventricular arrhythmias, for prevention of migraine attacks appoint a dose of 100-200 mg / day in 2 divided doses (morning and evening).

For secondary prevention myocardial infarction appoint an average daily dose of 200 mg in 2 divided doses (morning and evening).

At functional disorders cardiac activity accompanied by tachycardia, prescribed in a daily dose of 100 mg in 2 divided doses (morning and evening).

At elderly patients, patients with impaired renal function, and also if hemodialysis is necessary, changes in the dosing regimen are not required.

At patients with severe liver dysfunction the drug should be used in smaller doses, due to a slowdown in the metabolism of metoprolol.

Tablets should be taken orally during or immediately after a meal. Tablets can be divided in half, but not chewed.

SIDE EFFECT

From the side of the central nervous system and peripheral nervous system: fatigue, weakness, headache, slowing down the speed of mental and motor reactions; rarely - paresthesia in the limbs, depression, anxiety, decreased ability to concentrate, drowsiness, insomnia, nightmares, confusion or short-term memory impairment, asthenic syndrome, muscle weakness.

From the sense organs: rarely - decreased vision, decreased secretion of lacrimal fluid, xerophthalmos, conjunctivitis, tinnitus.

From the side of the cardiovascular system: sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension; rarely - a decrease in myocardial contractility, a temporary aggravation of symptoms of chronic heart failure, arrhythmias, increased peripheral circulatory disorders (coldness of the lower extremities, Raynaud's syndrome), myocardial conduction disturbances; in isolated cases - AV blockade, cardialgia.

From the side digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, dry mouth, taste change; increased activity of hepatic transaminases; rarely - hyperbilirubinemia.

Dermatological reactions: urticaria, pruritus, rash, exacerbation of psoriasis, psoriasis-like skin changes, skin flushing, exanthema, photodermatosis, increased sweating, reversible alopecia.

From the side respiratory system: nasal congestion, difficulty exhaling (bronchospasm when administered in high doses or in predisposed patients), shortness of breath.

From the side endocrine system: hypoglycemia (in patients receiving insulin); rarely - hyperglycemia.

From the hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

Others: pain in the back or joints, a slight increase in body weight, a decrease in libido and / or potency.

CONTRAINDICATIONS

Cardiogenic shock;

AV block II and III degree;

Sinoatrial blockade;

Severe bradycardia (heart rate less than 50 bpm);

Heart failure in the stage of decompensation;

Angiospastic angina (Prinzmetal's angina);

Severe arterial hypotension (systolic blood pressure below 100 mm Hg);

lactation period;

Simultaneous reception of MAO inhibitors;

Simultaneous in / in the introduction of verapamil;

Hypersensitivity to metoprolol and other ingredients of the drug.

FROM caution the drug should be prescribed for diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), obliterating diseases peripheral vessels(intermittent claudication, Raynaud's syndrome), chronic liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, AV block I degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, as well as children and adolescents aged up to 18 years, elderly patients.

PREGNANCY AND LACTATION

The use of Egilok during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If it is necessary to prescribe the drug during this period, careful monitoring of the condition of the fetus and newborn within 48-72 hours after birth is necessary, since intrauterine growth retardation, bradycardia, arterial hypotension, respiratory depression, hypoglycemia are possible.

The effect of metoprolol on the newborn during breastfeeding has not been studied, so women taking Egilok should stop breastfeeding.

SPECIAL INSTRUCTIONS

When prescribing the drug Egilok, heart rate and blood pressure should be regularly monitored. The patient should be warned that if the heart rate is less than 50 beats / min, a doctor's consultation is necessary.

In patients with diabetes blood glucose levels should be regularly monitored and, if necessary, the dose of insulin or oral hypoglycemic drugs should be adjusted.

The appointment of Egilok to patients with chronic heart failure is possible only after reaching the stage of compensation.

In patients taking Egilok, it is possible to increase the severity of hypersensitivity reactions (against a aggravated allergic history) and the lack of effect from the administration of conventional doses of epinephrine (adrenaline).

Against the background of the use of Egilok, the symptoms of peripheral circulatory disorders may worsen.

Egilok should be canceled gradually, consistently reducing its dose within 10 days. With a sharp cessation of treatment, a withdrawal syndrome may occur (increased angina attacks, increased blood pressure). During the period of drug withdrawal, patients with angina pectoris should be under close medical supervision.

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

Patients using contact lenses, should take into account that against the background of treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible.

Metoprolol may mask some of the clinical manifestations of hyperthyroidism (tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms.

In diabetes mellitus, taking Egilok may mask the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).

When metoprolol is administered to patients with bronchial asthma simultaneous use of beta 2-agonists is necessary.

In patients with pheochromocytoma, Egilok should be used in combination with alpha-blockers.

Before carrying out any surgical intervention, it is necessary to inform the anesthetist about the ongoing therapy with Egilok (the choice of drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not required.

When prescribing the drug to elderly patients, liver function should be regularly monitored. Correction of the dosing regimen is required only in the case of the appearance in elderly patients of increasing bradycardia, a pronounced decrease in blood pressure, AV blockade, bronchospasm, ventricular arrhythmias, and severe liver dysfunction. Sometimes it is necessary to stop treatment.

Special monitoring of the condition of patients with depressive disorders in history. If depression develops, Egilok should be discontinued.

At simultaneous application Egilok with clonidine in case of cancellation of Egilok, clonidine should be canceled after a few days (due to the risk of withdrawal syndrome).

Drugs that reduce catecholamine stores (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect excessive reduction in blood pressure or bradycardia.

Pediatric use

The efficacy and safety of Egilok in children and adolescents under the age of 18 not defined.

Influence on the ability to drive vehicles and control mechanisms

In patients whose activities require increased attention, the issue of prescribing the drug on an outpatient basis should be decided only after assessing the individual patient response.

OVERDOSE

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, arterial hypotension, arrhythmia, ventricular premature beats, bronchospasm, syncope; in acute overdose - cardiogenic shock, loss of consciousness, coma, AV blockade up to the development of complete transverse blockade and cardiac arrest, cardialgia.

The first signs of an overdose appear 20 minutes to 2 hours after ingestion.

Treatment: gastric lavage, administration of adsorbents, symptomatic therapy: with a pronounced decrease in blood pressure - the Trendelenburg position, in case of acute arterial hypotension, bradycardia and threatening heart failure - in / in (with an interval of 2-5 minutes) the introduction of beta-agonists or / in the introduction of 0.5-2 mg of atropine sulfate, in the absence positive effect- dopamine, dobutamine or norepinephrine. As follow-up measures, it is possible to prescribe 1-10 mg of glucagon, the setting of a transvenous intracardiac pacemaker. With bronchospasm - in / in the introduction of beta 2 -adrenergic stimulants, with convulsions - slow in / in the introduction of diazepam. Metoprolol is poorly excreted by hemodialysis.

DRUG INTERACTIONS

With the simultaneous use of Egilok with MAO inhibitors, a significant increase in the hypotensive effect is possible. The break between taking MAO inhibitors and Egilok should be at least 14 days.

Simultaneous intravenous administration of verapamil can provoke cardiac arrest, while the simultaneous administration of nifedipine leads to a significant decrease in blood pressure.

Means for inhalation anesthesia (derivatives of hydrocarbons), when used simultaneously with Egilok, increase the risk of inhibition of myocardial contractile function and the development of arterial hypotension.

With the simultaneous use of beta-agonists, theophylline, cocaine, estrogens, indomethacin and other NSAIDs reduce the hypotensive effect of Egilok.

With the simultaneous use of Egilok and ethanol, there is an increase in the inhibitory effect on the central nervous system.

With the simultaneous use of Egilok with ergot alkaloids, the risk of peripheral circulatory disorders increases.

With the simultaneous use of Egilok increases the effect of oral hypoglycemic drugs and insulin and increases the risk of hypoglycemia.

With the simultaneous use of Egilok with antihypertensive agents, diuretics, nitrates, calcium channel blockers, the risk of arterial hypotension increases.

With the simultaneous use of Egilok with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, methyldopa, clonidine, guanfacine, general anesthesia agents and cardiac glycosides, there may be an increase in the severity of the decrease in heart rate and inhibition of AV conduction.

Inducers of microsomal liver enzymes (rifampicin, barbiturates) accelerate the metabolism of metoprolol, which leads to a decrease in the concentration of metoprolol in the blood plasma and a decrease in the effect of Egilok.

Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) increase the concentration of metoprolol in blood plasma.

Allergens used for immunotherapy or allergen extracts for skin tests at joint application with Egilok, increase the risk of systemic allergic reactions or anaphylaxis.

Egilok with simultaneous use reduces the clearance of xanthines, especially in patients with initially increased clearance of theophylline under the influence of smoking.

With simultaneous use with Egilok, the clearance of lidocaine decreases and the concentration of lidocaine in plasma increases.

With the simultaneous use of Egilok enhances and prolongs the action of non-depolarizing muscle relaxants; prolongs the action of indirect anticoagulants.

When combined with ethanol, the risk of a pronounced decrease in blood pressure increases.

TERMS AND CONDITIONS OF DISCOUNT FROM PHARMACIES

The drug is dispensed by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of the reach of children at a temperature of 15 ° to 25 ° C. Shelf life - 5 years.

Egilok C is a selective beta-blocker.

Release form and composition

Dosage form - tablets of prolonged action, coated film sheath: biconvex, oval, white, with a risk on both sides (10 pieces in a blister, in a cardboard bundle 3 or 10 blisters and instructions for use Egilok C).

Composition of 1 tablet:

• active substance: metoprolol succinate - 25, 50, 100 or 200 mg;
• auxiliary components: ethylcellulose, methylcellulose, microcrystalline cellulose, glycerol, magnesium stearate, corn starch;
• film shell: Sepifilm LP 770 white (hypromellose, titanium dioxide E171, stearic acid, microcrystalline cellulose).

Pharmacological properties

Pharmacodynamics

The active substance Egilok C, metoprolol succinate, is a beta 1-blocker that is able to block β 1 -adrenergic receptors when using significantly lower doses than required to block β 2 -adrenergic receptors.

Egilok C has little membrane stabilizing activity and is not a partial agonist.

Metoprolol is able to reduce or suppress the agonistic effect exerted on cardiac activity by catecholamines, which are released during physical and nervous stress. It means that medicinal substance may prevent an increase in cardiac output and heart rate (HR), an increase in cardiac contractility and an increase in blood pressure(BP) due to a sharp release of catecholamines.

Unlike conventional tableted selective beta 1 -blockers (including metoprolol tartrate), long-acting metoprolol succinate provides a constant plasma concentration of the drug and a stable clinical effect (beta 1 -blockade) for at least 24 hours. As a result of the absence of significant maximum plasma concentrations of metoprolol succinate has a higher β 1 -selectivity than conventional tablet forms of metoprolol. In addition, Egilok C significantly reduces the potential risk of side effects that often occur at maximum plasma concentrations, such as weakness in the legs when walking or bradycardia.

With concomitant obstructive pulmonary diseases, Egilok C can be prescribed in addition to beta 2-agonists. Metoprolol succinate has less effect on the bronchodilation they cause compared to non-selective beta-blockers.

Metoprolol succinate is less than non-selective beta-blockers, affects carbohydrate metabolism and insulin production, as well as the cardiovascular system in conditions of hypoglycemia.

With arterial hypertension, Egilok C significantly reduces blood pressure, this effect persists for at least 24 hours, both in the supine and standing position, and during physical exertion. At the beginning of the use of the drug, an increase in vascular resistance is observed. However, with prolonged use of metoprolol succinate, a decrease in blood pressure is possible due to a decrease in vascular resistance, while cardiac output does not change.

Pharmacokinetics

Each Egiloc C tablet contains a large number of microgranules (pellets) coated with a polymer shell, due to which a controlled release of the active substance is carried out.

The effect of the drug comes quickly. Getting into gastrointestinal tract(GIT), the tablets are disintegrated into separate pellets, each of which acts separately, and together they provide a uniform release of metoprolol succinate for more than 20 hours. The release rate depends on the acidity of the gastric environment. Thus, the duration of action of Egilok C is more than 24 hours.

Metoprolol succinate is completely absorbed in the gastrointestinal tract. After a single dose, systemic bioavailability is approximately 30-40%.

The substance is characterized by low plasma protein binding - 5-10%.

The drug is metabolized in the liver by oxidation with the formation of three main metabolites that do not have clinically significant activity. It is excreted mainly in the form of metabolites, only about 5% of the dose is eliminated unchanged by the kidneys.

The half-life of free metoprolol is ~ 3.5-7 hours.

Indications for use

• stable chronic heart failure, accompanied by clinical manifestations (II-IV functional class according to the NYHA classification) and impaired systolic function of the left ventricle (as additional drug as part of the main therapy for chronic heart failure);
• arterial hypertension;
• cardiac arrhythmias, including supraventricular tachycardia, a decrease in the frequency of ventricular contraction with ventricular extrasystoles and atrial fibrillation;
• angina;
• functional disorders of cardiac activity, accompanied by tachycardia;
• reduction in the incidence of re-infarction and mortality after acute phase myocardial infarction;
• prevention of migraine attacks.

Contraindications

Absolute:

• arterial hypotension in systolic blood pressure< 90 мм рт. ст.;
• weakness syndrome sinus node(SSSU);
• atrioventricular block II and III degree;
• clinically significant sinus bradycardia with heart rate< 50 уд/мин;
• decompensated heart failure;
• P-Q interval > 0.24 sec;
• suspected acute myocardial infarction with heart rate< 45 уд/мин;
• cardiogenic shock;
• severe disorders of peripheral circulation with the threat of gangrene;
• pheochromocytoma (if alpha-blockers are not used simultaneously);
• age up to 18 years;
• intravenous (in / in) the introduction of blockers of slow calcium channels such as verapamil;
• simultaneous use of monoamine oxidase inhibitors (MAO) (with the exception of type B);
• long-term or course use of inotropic agents and drugs acting on β-adrenergic receptors;
• hypersensitivity to any component of the drug or other beta-blockers.

Egilok C tablets should be used with caution in the following cases (careful assessment of the benefit-risk ratio is required):

• Prinzmetal's angina;
• atrioventricular block I degree;
• obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome);
• metabolic acidosis;
• severe renal/liver failure;
• chronic obstructive pulmonary disease;
• bronchial asthma;
• diabetes;
• thyrotoxicosis;
• psoriasis;
• myasthenia gravis;
• depression;
• pheochromocytoma (with simultaneous reception alpha-blockers);
• simultaneous use of cardiac glycosides;
• elderly age.

Egilok S, instructions for use: method and dosage

Egilok C is taken orally, 1 time per day (regardless of the prescribed dose), preferably in the morning. Tablets must be swallowed whole, without chewing or crushing, and washed down enough liquids. The time of meals does not matter.

The optimal dose is selected by the doctor individually, with caution - in order to avoid the development of bradycardia.

Treatment of stable chronic heart failure (CHF) with clinical manifestations and impaired systolic function of the left ventricle is started only if the patient is in a stable condition without exacerbation episodes for 6 recent weeks. In this case, during the last 2 weeks, you can not change the scheme of the main therapy.

In some cases, beta-blockers (including Egilok C) can cause a temporary worsening of the course of chronic heart failure. Sometimes it is possible to extend therapy or reduce the dose, but some patients require the abolition of metoprolol.

In functional class II CHF, 25 mg is prescribed at the beginning of therapy, after 2 weeks, if necessary, the dose is increased to 50 mg. If in this case the effect is not enough, a further doubling of the dose at intervals of 2 weeks is possible. At long-term treatment the maintenance dose is usually 200 mg.

With CHF III and IV functional classes, Egilok C is prescribed in the first two weeks at a daily dose of 12.5 mg (½ tablet at a dosage of 25 mg). The optimal maintenance dose is selected individually under close medical supervision, since the progression of symptoms of heart failure is possible. After 1-2 weeks, if necessary, increase the daily dose to 25 mg, after another 2 weeks - up to 50 mg. If the therapeutic effect is insufficient, but if the drug is well tolerated, it is possible to double the dose at intervals of 2 weeks until a maximum of 200 mg is reached.

In the event of the development of arterial hypotension and / or bradycardia, it may be necessary to correct the main therapy regimen, or reduce the dose of Egilok C. The development of arterial hypotension during the dose selection period does not always indicate intolerance to the drug at this dose with continued treatment. However, further increase in the dose is possible only after stabilization of the patient's condition. Sometimes you need control functional state kidneys.

• arterial hypertension: 50-100 mg. If the effect is not enough, increase the daily dose to a maximum of 200 mg or add another antihypertensive agent to therapy (preference is given to diuretics and slow calcium channel blockers);
• cardiac arrhythmias: 100-200 mg;
• angina pectoris: 100–200 mg. If the therapeutic effect is insufficient, another antianginal agent is added to the therapy;
• functional disorders of cardiac activity, accompanied by tachycardia: 100 mg, if necessary, the daily dose is increased to 200 mg;
• maintenance therapy after myocardial infarction: 100-200 mg (in this case, the daily dose can be divided into 2 doses);
• prevention of migraine attacks: 100–200 mg.

The elderly, patients with impaired renal function and patients with moderate hepatic impairment do not need to adjust the dose.

In severe functional disorders of the liver (severe cirrhosis, portocaval anastomosis), a dose reduction of Egilok C may be necessary.

Side effects

Egilok C is generally well tolerated. If adverse reactions occur, they are usually mild and reversible.

Possible side effects(classified as follows: very often -> 10% of cases; often - 1-9.9%; infrequently - 0.1-0.9%; rarely - 0.01-0.09%; very rarely -< 0,01%):

• from the side of the cardiovascular system: often - palpitations, orthostatic hypotension (very rarely accompanied by fainting), bradycardia, cold extremities; infrequently - a temporary increase in symptoms of heart failure, pain in the region of the heart, peripheral edema, atrioventricular block I degree, cardiogenic shock in patients with acute infarction myocardium; rarely - other cardiac conduction disorders, arrhythmias; very rarely in patients with previous severe peripheral circulatory disorders - gangrene;
• from the digestive system: often - abdominal pain, constipation, diarrhea, nausea; infrequently - vomiting; rarely - dryness of the oral mucosa, functional impairment of the liver; very rarely - hepatitis;
• from the side of the central nervous system: very often - increased fatigue; often - headache, dizziness; infrequently - insomnia / drowsiness, nightmares, impaired attention, paresthesia, depression, convulsions; rarely - anxiety, increased nervous excitability, sexual dysfunction / impotence; very rarely - depression, memory impairment / amnesia, hallucinations;
• from the sensory organs: rarely - dryness and / or irritation of the eyes, visual impairment, conjunctivitis; very rarely - violations taste sensations, ringing in the ears;
• from the respiratory system: often - shortness of breath with physical effort; infrequently - bronchospasm; rarely - rhinitis;
• from the side musculoskeletal system: very rarely - arthralgia;
• from the side skin: infrequently - urticaria, increased sweating; rarely - hair loss; very rarely - exacerbation of the course of psoriasis, photosensitivity;
• other: infrequently - weight gain; very rarely - thrombocytopenia.

Overdose

The most serious symptoms of an overdose of metoprolol succinate are disorders of the cardiovascular system, but sometimes suppression of pulmonary function and the predominance of signs from the central nervous system are possible.

Possible symptoms: pronounced decrease in blood pressure, AV blockade of I-III degree, bradycardia, poor peripheral perfusion, asystole, cardiogenic shock, heart failure, apnea, depression of lung function, bronchospasm, impaired or loss of consciousness, increased fatigue, increased sweating, tremor, paresthesia, convulsions, spasm of the esophagus, nausea, vomiting, impaired renal function, hyperkalemia, hyperglycemia, hypoglycemia (especially in children), transient myasthenic syndrome. With the concomitant use of alcohol, barbiturates, antihypertensive drugs or quinidine, the patient's condition may worsen. The first symptoms of an overdose may occur 20-120 minutes after taking high doses of Egilok S.

First aid measures: reception activated carbon, if necessary - gastric lavage. Before gastric lavage, due to the risk of stimulating the vagus nerve, atropine is prescribed (adults - 0.25-0.5 mg). If required, provide permeability respiratory tract(by intubation) and adequate ventilation. It is necessary to introduce glucose, replenish the volume of circulating blood, as well as control the electrocardiogram. Atropine is also administered intravenously at a dose of 1–2 mg, if necessary, the administration is repeated (especially in the presence of vagal symptoms). With depression (suppression) of the myocardium, an infusion of dopamine or dobutamine is done. In addition, it is possible to administer intravenous glucagon at a dose of 50–150 mcg/kg with an interval of 1 min. In some cases, it is advisable to add epinephrine (adrenaline) to therapy. With arrhythmia and an expanded ventricular complex, an infusion of a 0.9% sodium chloride solution or sodium bicarbonate is indicated. If necessary, install an artificial pacemaker. Terbutaline is used to relieve bronchospasm (injection or inhalation). In case of cardiac arrest, appropriate resuscitation measures are carried out.

special instructions

Beta-blockers are not recommended for patients with obstructive pulmonary disease. If other antihypertensive drugs are poorly tolerated or do not have the desired therapeutic effect, Egilok C may be used, but the minimum effective dose should be prescribed. If necessary, use beta 2-agonists.

Compared to non-selective beta-blockers, selective beta 1-blockers have less effect on carbohydrate metabolism and mask the symptoms of hypoglycemia, but the risk of such an effect cannot be completely excluded.

In decompensated chronic heart failure, a compensation stage should be achieved before the start of treatment, and it should be maintained during therapy.

Data clinical research the safety and efficacy of Egiloc C in severe stable heart failure (NYHA class IV) are limited.

Metoprolol succinate may worsen symptoms of peripheral circulatory disorders (usually due to a decrease in blood pressure).

For patients with concomitant pheochromocytoma, Egilok C is prescribed simultaneously with an alpha-blocker.

In rare cases, in violation of atrioventricular conduction, worsening (up to AV blockade) is possible. With the development of bradycardia, it is necessary to reduce the dose of metoprolol succinate or gradually cancel it.

Patients who are to surgical intervention, you should warn the anesthesiologist about taking the drug Egilok C. It is not recommended to cancel beta-blockers.

Anaphylactic shock, which develops during therapy with beta-blockers, proceeds in a more severe form. At the same time, the use of adrenaline in standard therapeutic doses does not always cause the desired effect.

The efficacy and safety of Egilok C in patients with symptoms of heart failure in combination with acute myocardial infarction and unstable angina have not been established.

In case of abrupt discontinuation of the drug, it is possible to increase the symptoms of chronic heart failure, increase the risk of myocardial infarction and sudden death especially in high-risk patients. For this reason, it is not recommended to suddenly stop taking Egilok S. This should be done gradually, over a period of at least 2 weeks, reducing the dose by 2 times at each stage, until the final dose of 12.5 mg is reached - it should be taken for at least 4 days until the drug is completely discontinued. If undesirable symptoms appear with this scheme, a slower withdrawal of therapy is recommended.

Influence on the ability to drive vehicles and complex mechanisms

Egilok C can cause dizziness and fatigue, so patients receiving the drug should be careful when driving vehicles and performing potentially hazardous types of work.

Use during pregnancy and lactation

Adequate controlled studies on the use of metoprolol succinate in pregnant women have not been conducted. As a result, Egilok C can only be used in women for whom the expected benefit of therapy outweighs the possible risks.

Beta-blockers can cause some side effects in the fetus, newborns and infants, such as bradycardia.

Metoprolol passes into the mother's milk in small amounts, so the risk of adverse reactions is low. Nevertheless, infants whose mothers receive Egilok C during lactation should be under close medical supervision for possible signs of β-adrenergic blockade.

Application in childhood

Egiloc C is contraindicated under 18 years of age, since its efficacy and safety in pediatric patients have not been established.

For impaired renal function

Patients with chronic kidney failure Egilok C is prescribed with caution.

Correction of the dosing regimen for functional disorders of the kidneys and hemodialysis is not required.

For impaired liver function

Patients with liver failure Egilok C is prescribed with caution. The doctor selects the dose individually, based on the data of the clinical condition.

Use in the elderly

For the treatment of elderly patients, Egilok C tablets are used with caution.

drug interaction

• verapamil: high risk the development of bradycardia and a decrease in blood pressure, there is a complementary inhibitory effect on AV conduction and sinus node function;
• derivatives of barbituric acid: the metabolism of metoprolol is enhanced;
• propafenone: the plasma concentration of metoprolol increases significantly (2-5 times), side effects may develop.

Combinations that require caution and may require dose adjustments:

• class I antiarrhythmics: a negative inotropic effect may accumulate, which is fraught with the development of serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in AV conduction disorders and sick sinus syndrome;
• non-steroidal anti-inflammatory drugs (with the possible exception of sulindac): the antihypertensive effect of metoprolol is weakened;
• cardiac glycosides: AV conduction time increases, bradycardia develops;
• clonidine: after its abrupt cancellation, hypertensive reactions may increase (it is recommended to start the abolition of beta-blockers a few days before stopping the use of clonidine);
• quinidine: in patients with rapid hydroxylation, the metabolism of metoprolol is inhibited, which causes a significant increase in its plasma concentration and an increase in beta-blockade (similar reactions are also possible when using other beta-blockers, in the metabolism of which the CYP2D6 isoenzyme is involved);
• rifampicin: it is possible to increase the metabolism of metoprolol and reduce its plasma concentration;
• oral hypoglycemic agents: there is a possibility of changing their effect, which may require dose adjustment;
• inhalation anesthetics: cardiodepressive effect is enhanced;
• amiodarone: possible development of severe sinus bradycardia. Amiodarone has long period half-life, so the interaction may occur later long time after its cancellation;
• epinephrine: there is a risk of bradycardia and severe arterial hypertension;
• diltiazem: there is a mutual strengthening of the inhibitory effect on the conductivity and function of the sinus node, there are cases of the development of severe bradycardia;
• phenylpropanolamine (norephedrine): it is possible to increase diastolic blood pressure to pathological values ​​and develop a hypertensive crisis (even after a single dose of 50 mg);

Released by prescription.