Egilok tablets 25 mg 60 pcs. (Metoprolol)

Release form

Tablets.

Packing

60 pcs.

Pharmacological action

Egilok is a cardioselective b-adrenergic blocker that does not have internal sympathomimetic and membrane-stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects.

Blocking heart b1-adrenergic receptors in low doses, reduces catecholamine-stimulated cAMP production from ATP, reduces intracellular Ca2 + current, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conduction 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 the initial 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 central nervous system, restoration of the sensitivity of the aortic arch baroreceptors (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic effects. Reduces elevated blood pressure at rest, with 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 use.

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

Antiarrhythmic effect is manifested due to a decrease in the automatism of the sinus node, a decrease in heart rate, a slowdown in AV conduction, a decrease in contractility and excitability of the myocardium, and cardiac output.

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

Prevents the development of migraines.

When taken for many years, lowers blood cholesterol.

When used in medium therapeutic doses, it has a less pronounced effect on organs containing b2-adrenergic receptors (pancreas, skeletal muscle, smooth muscles of peripheral arteries, bronchi, uterus) and carbohydrate metabolism.

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

Indications

- arterial hypertension (in monotherapy or in combination with other antihypertensive drugs)

- chronic heart failure in the stage of compensation (in addition to standard therapy with diuretics, ACE inhibitors, cardiac glycosides)

- prevention of heart disease (IHD) (secondary) angina attacks)

- cardiac arrhythmias (supraventricular arrhythmias, ventricular extrasystole)

- hyperkinetic cardiac syndrome

- hyperthyroidism (as part of comp eksnoy therapy)

- prevention of migraine attacks.

Contraindications

- cardiogenic shock

- AV block II and III degree

- sinoatrial blockade

- SSSU

- severe bradycardia (heart rate less than 50 beats. / min)

- heart failure in the stage of decompensation

- angiospastic angina (Prinzmetal angina)

- severe arterial hypotension (systolic blood pressure below 100 mmHg)

- lactation period

- concomitant use of MAO inhibitors in conjunction with - MAO inhibitors - the introduction of verapamil

- hypersensitivity to metoprolol and other ingredients of the drug.

Precautions should be prescribed for diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), peripheral vascular disease obliterans (intermittent claudication, Raynaud's syndrome), liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, grade I AV blockade, thyrotoxicosis, depression (including history), psoriasis, as well as in children and adolescents under the age of 18 years and in elderly patients.

Special instructions

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

In patients with diabetes mellitus, blood glucose levels should be regularly monitored and, if necessary, dose adjustment of insulin or oral hypoglycemic drugs should be carried out.

Prescribing Egiloc 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 the background of a burdened allergic history) and the lack of effect from the introduction of the usual doses of epinephrine (adrenaline).

Against the background of the use of Egilok, exacerbation of symptoms of peripheral circulation disorders is possible.

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

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

Patients using contact lenses should consider that tear fluid production may be reduced with beta-blockers.

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

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

When prescribing metoprolol to patients with asthma, simultaneous use of beta2-adrenergic agonists is necessary.

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

Before any surgery, it is necessary to inform the anesthesiologist about the ongoing Egiloc therapy (choosing a drug for general anesthesia with minimal negative inotropic effect) drug withdrawal 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 elderly patients with increasing bradycardia, a marked decrease in blood pressure, AV blockade, bronchospasm, ventricular arrhythmias, and severe liver dysfunction. Sometimes it is necessary to stop treatment.

A special history of patients with a history of depressive disorders should be monitored. If depression develops, Egiloc should be discontinued.

Pediatric use

Efficacy and safety of the use of Egiloc in children and adolescents under the age of 18 have not been determined.

Influence on the ability to drive vehicles and control mechanisms

In patients whose activities require increased attention, the issue of prescribing the drug as an outpatient should be decided only after evaluating the individual patient's response.

Composition

1 tablet contains metoprolol tartrate 25 mg

excipients: MCC sodium carboxymethyl starch silicon dioxide colloidal anhydrous povidone magnesium stearate.

Dosage and administration of

Egilok is prescribed for arterial hypertension in a daily dose of 50-100 mg / day in 1 or 2 doses. With insufficient therapeutic effect, a gradual increase in the daily dose to 100-200 mg is possible.

With angina pectoris, supraventricular arrhythmias, for the prevention of migraine attacks, a dose of 100-200 mg / day is prescribed in 2 doses (morning and evening).

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

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

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

Side effects

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 sensory organs: rarely - decreased vision, decreased secretion of lacrimal fluid, xerophthalmus, conjunctivitis, tinnitus.

On the part of the cardiovascular system: sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension, rarely - decreased myocardial contractility, temporary worsening of symptoms of chronic heart failure, arrhythmias, increased peripheral circulation disorders (coldness of the lower extremities, Raynaud's syndrome), myocardial conduction disturbances isolated cases - AV blockade, cardialgia.

From the 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 hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

From the respiratory system: nasal congestion, difficulty breathing out (bronchospasm when prescribed in high doses or in predisposed patients), shortness of breath.

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

From the hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

Other: back or joint pain, slight increase in body weight, decreased libido and / or potency.

Drug interaction

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

The simultaneous iv administration of verapamil can cause cardiac arrest, the simultaneous administration of nifedipine leads to a significant decrease in blood pressure.

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

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

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

With the simultaneous use of Egiloc with ergot alkaloids, the risk of peripheral circulation disorders increases.

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

With the simultaneous use of Egiloc with antihypertensive agents, diuretics, nitrates, calcium channel blockers increase the risk of hypotension.

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

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 when used together with Egiloc, increase the risk of systemic allergic reactions or anaphylaxis.

Iodine-containing radiopaque substances for iv administration with simultaneous use with Egilok increase the risk of anaphylactic reactions.

Egiloc 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 the plasma increases.

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

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

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, hypotension, arrhythmia, ventricular extrasystole, bronchospasm, fainting in acute overdose - cardiogenic shock, loss of consciousness, coma, AV blockade up to the development of a 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 - Trendelenburg position, in case of acute arterial hypotension, bradycardia and imminent heart failure - iv (with an interval of 2-5 min) administration of beta-adrenostimulants or iv in the introduction of 0.5-2 mg of atropine sulfate, in the absence of a positive effect - dopamine, dobutamine or norepinephrine. As a follow-up, it is possible to prescribe 1-10 mg of glucagon, staging a transvenous intracardial electrostimulator. With bronchospasm - in / in the introduction of beta2-adrenostimulants, with convulsions - slow intravenous administration of diazepam. Metoprolol is poorly excreted by hemodialysis.

Storage conditions

Keep out of the reach and sight of children at temperatures between 15 ° and 25 ° C.

PMA

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