Egilok (Metoprolol)

1 tablet contains metoprolol tartrate 100 mg;

Excipients:

MCC;

sodium carboxymethyl starch;

colloidal anhydrous silicon dioxide;

povidone;

magnesium stearate.

Egilok is a cardioselective b-adrenergic receptor blocker that does not possess internal sympathomimetic and membrane-stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects.
Blocking in low doses b ₁ -adrenergic receptors of the heart, reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular current of Ca ²⁺ , has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility ).

OPSS at the beginning 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 the 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 influences. Reduces high blood pressure at rest, during physical exertion and stress.

Blood pressure decreases after 15 minutes, maximum - after 2 hours; the effect lasts 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 (lengthening of diastole and an 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 manifested by a decrease in the automatism of the sinus node, a decrease in heart rate, a slowdown in AV conduction, a decrease in myocardial contractility and excitability, and cardiac output.

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

Prevents the development of migraines.

When taken for many years, it reduces blood cholesterol levels.

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

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

- 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);
- IHD (secondary prevention of myocardial infarction, prevention of angina attacks);
- heart rhythm disturbances (supraventricular arrhythmias, ventricular premature beats);
- hyperkinetic cardiac syndrome;
- hyperthyroidism (as part of complex therapy);
- prevention of migraine attacks.

- 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's angina);
- severe arterial hypotension (systolic blood pressure below 100 mm Hg);
- lactation period;
- simultaneous intake of MAO inhibitors;
- simultaneous intravenous administration of verapamil;
- hypersensitivity to metoprolol and other ingredients of the drug.

The drug should be prescribed with caution in diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), obliterating peripheral vascular diseases (intermittent claudication, Raynaud's syndrome), liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma , AV blockade of the 1st degree, thyrotoxicosis, depression (including history), psoriasis, as well as in children and adolescents under the age of 18 and in elderly patients.

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

From the senses: rarely - decreased vision, decreased secretion of tear 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 worsening of symptoms of chronic heart failure, arrhythmias, an increase in peripheral circulatory disorders (cooling of the lower extremities, Raynaud's syndrome), myocardial conduction disorders; in isolated cases - AV blockade, cardialgia.

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

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

From the respiratory system: nasal congestion, difficulty in exhaling (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 hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

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

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 Egilok should be at least 14 days.

Simultaneous intravenous administration of verapamil can provoke cardiac arrest, 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-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 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 drugs, 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 anesthetics and cardiac glycosides, an increase in the severity of a decrease in heart rate and inhibition of AV conduction can be observed.

Inductors of microsomal liver enzymes (rifampicin, barbiturates) accelerate the metabolism of metoprolol, which leads to a decrease in the concentration of metoprolol in 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 Egilok, increase the risk of systemic allergic reactions or anaphylaxis.

Iodine-containing radio-opaque substances for intravenous administration when used simultaneously with Egilok increase the risk of developing anaphylactic reactions.

Egilok, with simultaneous use, reduces the clearance of xanthines, especially in patients with an 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 effect of non-depolarizing muscle relaxants; lengthens the action of indirect anticoagulants.

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

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, an average daily dose of 200 mg is prescribed in 2 divided doses (morning and evening).

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

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

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

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

Treatment: gastric lavage, the appointment of adsorbents, symptomatic therapy: with a pronounced decrease in blood pressure - the Trendelenburg position, in the case of acute arterial hypotension, bradycardia and threatening heart failure - intravenous (with an interval of 2-5 minutes) introduction of beta-adrenostimulants or intravenous administration 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, the setting of a transvenous intracardiac pacemaker. With bronchospasm - intravenous administration of beta2-adrenostimulants, with convulsions - slow intravenous administration of diazepam. Metoprolol is poorly excreted by hemodialysis.

When prescribing Egilok, you should regularly monitor heart rate and blood pressure. 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 mellitus, blood glucose levels should be regularly monitored and, if necessary, the dose of insulin or oral hypoglycemic drugs should be adjusted.

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

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

Against the background of the use of Egilok, it is possible to aggravate the symptoms of impaired peripheral circulation.

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

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

Patients using contact lenses should take into account that during treatment with beta-blockers, it is possible to reduce the production of tear fluid.

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

With diabetes, taking Egilok can mask the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
When metoprolol is prescribed to patients with bronchial asthma, the simultaneous use of beta ₂ -adrenomimetics 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 anesthesiologist about the ongoing therapy with Egilok (the choice of a drug for general anesthesia with a minimal negative inotropic effect); drug withdrawal is not required.

When prescribing the drug, elderly patients should regularly monitor liver function. Correction of the dosage regimen is required only if elderly patients develop an 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 should be carried out for patients with a history of depressive disorders. If depression develops, Egilok should be canceled.

Use in pediatrics

The effectiveness and safety of Egilok's use in children and adolescents under the age of 18 have not been determined.

Influence on the ability to drive vehicles and use mechanisms

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

Pills.