Egilok, pills 100mg 60pcs

Composition

1 tablet contains metoprolol tartrate 100 mg;

excipients:

MCC;

sodium carboxymethyl starch;

colloidal anhydrous silicon dioxide;

povidone;

magnesium stearate.

Pharmacological action

Pharmacogroup:

beta-1-adrenoblocker selective.

Pharmaceutical action:  

Egilok is a cardioselective blocker of beta-adrenergic receptors, which does not have internal sympathomimetic and membrane-stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects. Blocking the beta-1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular Ca2+ current, has a negative chrono -, dromo -, batmo-and inotropic effect (reduces heart rate, inhibits conduction and excitability, reduces myocardial contractility).

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

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 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 elevated 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 use.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (prolongation of diastole and improvement of 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, increased cAMP content, 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 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 the cholesterol content in the blood.

When used in medium therapeutic doses, it has a less pronounced effect on organs containing beta-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 beta-adrenergic receptors.

Pharmacokinetics:  

Suction

Rapidly and completely (95%) absorbed from the gastrointestinal tract. Cmax in plasma is reached in 1.5-2 hours after oral use. Bioavailability is 50%. During treatment, bioavailability increases to 70%. Food intake increases bioavailability by 20-40%.

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

Metabolism Metoprolol is biotransformed in the liver. The metabolites have no pharmacological activity.

Excretion1 / 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 cases

With severe hepatic impairment, the bioavailability and T1/2 of metoprolol increases, which may require dose adjustment.

With impaired renal function, T1 / 2 and systemic clearance of metoprolol do not significantly change.

Indications

– arterial hypertension (monotherapy or in combination with other antihypertensive drugs);– chronic heart failure in the stage of compensation (in addition to standard treatment with diuretics, ACE inhibitors, cardiac glycosides);– ischemic heart disease (secondary prevention of myocardial infarction, prevention of angina attacks); the heart rhythm disturbances (supraventricular arrhythmia, ventricular extrasystoles);– cardiac hyperkinetic syndrome;– hyperthyroidism (in the complex therapy); prevention of migraine attacks.

Contraindications

– cardiogenic shock;– AV-block II and III degree;– sinoatrial block;– SSSU;– severe bradycardia (heart rate less than 50 beats/min); heart failure in the stage of decompensation;– angioplastika angina (Prinzmetal’s angina);– severe hypotension (systolic blood pressure below 100 mm Hg. St. )– lactation period;– simultaneous reception of MAO inhibitors;– simultaneous in/in the introduction of verapamil;– hypersensitivity to metoprolol and other ingredients of the preparation.

With caution, the drug should be prescribed for diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (emphysema of the lungs, chronic obstructive bronchitis), obliterating peripheral vascular diseases (intermittent claudication, Raynaud’s syndrome), liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, AV block I degree, thyrotoxicosis, depression (including in psoriasis, as well as in children and adolescents under 18 years of age and in elderly patients.

Side effects

From the central nervous system and peripheral nervous system: increased fatigue, weakness, headache, slowing down 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 sensory organs: rarely-decreased vision, decreased secretion of tear fluid, xerophthalmus, conjunctivitis, tinnitus.

From the cardiovascular system: sinus bradycardia, palpitation, decreased blood pressure, orthostatic hypotension; rarely-decreased myocardial contractility, temporary aggravation of symptoms of chronic heart failure, arrhythmias, increased peripheral circulatory disorders (cold of the lower extremities, Raynaud’s syndrome), myocardial conduction disorders; in isolated cases – AV block, cardialgia.

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

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

From the respiratory system: nasal congestion, difficulty 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 or joint pain, slight weight gain, decreased libido and / or potency.

Interaction

With the simultaneous use of 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 use of verapamil may cause cardiac arrest, while simultaneous use of nifedipine leads to a significant decrease in blood pressure. Means for inhalation anesthesia (hydrocarbon derivatives) when used simultaneously with Egilok increase the risk of inhibition of myocardial contractility and the development of arterial hypotension.

Concomitant use of beta-adrenostimulants, theophylline, cocaine, estrogens, indomethacin and other NSAIDs reduces the hypotensive effect of Egilok.

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

When Egiloc is co-administered with ergot alkaloids, the risk of peripheral circulatory disorders increases. Concomitant use of Egilok increases the effect of oral hypoglycemic drugs and insulin and increases the risk of hypoglycemia.

Concomitant use of Egiloc with antihypertensive agents, diuretics, nitrates, and calcium channel blockers increases the risk of hypotension.

When Egiloc is co-administered with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, methyldopa, clonidine, guanfacine, general anesthesia and cardiac glycosides, an increase in the severity of heart rate reduction and suppression of AV conduction may occur.

Inducers 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 Egilok effect.

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 combined with Egilok increase the risk of systemic allergic reactions or anaphylaxis.

Iodine-containing radiopaque agents for intravenous use when used simultaneously with Egilok increase the risk of anaphylactic reactions.

Egilok, when used concomitantly, reduces the clearance of xanthines, especially in patients with an initially increased clearance of theophylline under the influence of smoking.

When used concomitantly with Egiloc, the clearance of lidocaine decreases and the concentration of lidocaine in plasma increases.

When used simultaneously, Egilok enhances and prolongs the effect of non-depolarizing muscle relaxants; prolongs the effect of indirect anticoagulants.

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

How to take, course of use and dosage

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

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

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

Overdose

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

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

Treatment: gastric lavage, use 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) use of beta-adrenostimulants or intravenous use 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, and install a transvenous intracardial electrostimulator. With bronchospasm-intravenous use of beta-2-adrenostimulants, with convulsions-slow intravenous use of diazepam. Metoprolol is poorly excreted by hemodialysis.

Special instructions

When prescribing Egilok, you should regularly monitor your 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 monitored regularly and, if necessary, the dose of insulin or oral hypoglycemic drugs should be adjusted.

Egilok can be prescribed to patients with chronic heart failure only after reaching the compensation stage. In patients taking Egilok, the severity of hypersensitivity reactions may increase (against the background of a burdened allergic history) and the lack of effect from the introduction of conventional doses of epinephrine (epinephrine).

Against the background of the use of Egilok, it is possible to aggravate the symptoms of peripheral circulatory disorders.

Egilok should be discontinued gradually, gradually reducing its dose over 10 days. If treatment is abruptly discontinued, withdrawal symptoms may occur (increased angina attacks, increased blood pressure). Patients with angina pectoris should be under close medical supervision during drug withdrawal.

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

Patients who use contact lenses should take into account that against the background of treatment with beta-blockers, tear fluid production may decrease.

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

In diabetes mellitus, Egilok may mask the symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure). When prescribing metoprolol to patients with bronchial asthma, simultaneous use of beta-2-adrenomimetics is necessary. In patients with pheochromocytoma, Egilok should be used in combination with alpha-blockers.

Before performing any surgical intervention, it is necessary to inform the anesthesiologist about the ongoing therapy with Egiloc (the choice of 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 dosage regimen is required only if elderly patients develop increasing bradycardia, a pronounced decrease in blood pressure, AV block, bronchospasm, ventricular arrhythmias, and severe liver function disorders. Sometimes it is necessary to stop treatment.

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

Use in pediatrics

The efficacy and safety of Egiloc in children and adolescents under 18 years of age have not been determined.

Influence on the ability to drive motor vehicles and manage mechanisms

In patients whose activity requires increased attention, the question of prescribing the drug on an outpatient basis should be decided only after evaluating the individual patient response.

Form of production

Pills.

Storage conditions

At a temperature of 15-25 °C

Shelf life

5 years

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Angina, Arrhythmia, Myocardial Infarction, Migraine, Hypertension