Hypotensive, antiarrhythmic drug Egilok: instructions for use, side effects and analogues. How long can I take Egiloc Egiloc for heart failure

INN: metoprolol

Manufacturer: CJSC "Pharmaceutical plant EGIS"

Anatomical-therapeutic-chemical classification: Metoprolol

Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 012140

Registration period: 15.02.2018 - 15.02.2023

ALO (Included in the Free Outpatient Drug Supply List)

Instruction

Tradename

Minternational nonproprietary name

metoprolol

Dosage form

Tablets 25mg, 50mg, 100mg

Compound

One tablet contains

active substance- metoprolol tartrate 25mg, 50mg, 100mg,

Excipients: microcrystalline cellulose, sodium starch glycolate (type A), anhydrous colloidal silicon dioxide, povidone (K-90), magnesium stearate.

Description

Tablets white or almost white, round, biconvex, with a cross-shaped dividing line and a double bevel ("double snap") on one side and engraved with a stylized letter "E" and the number 435 on the other side, odorless or almost odorless (for dosage25mg)

Tablets white or almost white, round, biconvex surface, scored on one side and engraved with a stylized letter "E" and the number 434 on the other side, odorless or almost odorless (for dosage50mg)

Tablets white or almost white, round, biconvex, beveled, scored on one side and engraved with a stylized letter "E" and the number 432 on the other side, odorless or almost odorless (for dosage100mg)

Pharmacotherapeutic group

Preparations for the treatment of diseases of the cardiovascular system. Beta-blockers are selective. Metoprolol.

ATX code C07A B02

Pharmacological properties

Pharmacokinetics

Metoprolol is rapidly and completely absorbed from the gastrointestinal tract. In the therapeutic dose range, the drug is characterized by linear pharmacokinetics. The maximum plasma concentration is reached 1.5-2 hours after ingestion. Despite significant individual fluctuations in plasma levels of the drug, in each individual patient, these differences are insignificant. After absorption, metoprolol is largely metabolized by the first pass through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with multiple doses. At the same time, food intake can increase the bioavailability of metoprolol by 30-40%. It binds to plasma proteins by about 5-10%. Metoprolol is widely distributed in tissues and has a high volume of distribution (5.6 l/kg). Metoprolol is metabolized in the liver by cytochrome P-450 CYP2D6 enzymes. Metabolites have no clinical significance. The elimination half-life averages 3.5 hours (range 1 to 9 hours). The total clearance of the drug is approximately 1 l / min. About 95% of the oral dose is excreted in the urine, of which 5% is unchanged (in some cases it can reach 30%).

Special patient groups

Significant changes in the pharmacokinetics of metoprolol in elderly patients have not been identified.

Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases, there is a decrease in the excretion of metabolites.

In severe renal failure (GFR 5 ml / min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the degree of β-adrenergic blockade. Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe cirrhosis of the liver and after the imposition of a porto-caval shunt, bioavailability may increase, and overall clearance may decrease. After porto-caval shunting, the total clearance of the drug is approximately 0.3 l / min, and the area under the concentration-time curve increases by about 6 times compared with healthy individuals.

Pharmacodynamics

Metoprolol is a cardioselective β1-blocker that does not have intrinsic sympathomimetic or membrane stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects.

Metoprolol prevents the stimulating effect of the sympathetic nervous system on the heart and causes a rapid decrease in heart rate, contractility, minute volume and blood pressure during physical and mental stress and stress.

With an increased level of endogenous adrenaline, metoprolol has a lesser effect on blood pressure than non-selective β-blockers. If necessary, metoprolol in combination with a β2-agonist can be prescribed to patients with obstructive pulmonary diseases. At therapeutic doses, metoprolol has a lesser effect on the bronchodilatory effect of β2-agonists than non-selective β-blockers.

Compared with non-selective β-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism. The drug does not significantly change the cardiovascular response to hypoglycemia and does not increase the duration of hypoglycemic attacks.

In clinical studies, it was found that metoprolol slightly increases the level of triglycerides and slightly lowers the level of free fatty acids in the blood plasma. In some cases, a slight decrease in HDL levels was observed. This decrease was less pronounced than with the use of non-selective β-blockers. However, in a long-term study, a statistically significant reduction in cholesterol levels was observed after several years of treatment with metoprolol. During treatment with metoprolol, the quality of life did not change or improved. Treatment with metoprolol after myocardial infarction improved quality of life.

With arterial hypertension it lowers blood pressure in patients standing and lying down. At the beginning of treatment with metoprolol, a short-term (lasting for several hours), clinically insignificant increase in peripheral vascular resistance was observed. The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance.

In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its filling and diastolic function.

In men with moderate or moderate arterial hypertension, metoprolol reduces mortality from cardiovascular disorders (primarily sudden death, fatal and non-fatal myocardial infarctions and strokes).

Like other β-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic arterial pressure, heart rate and myocardial contractility. By reducing the heart rate and the corresponding lengthening of the diastole, metoprolol improves the blood supply and oxygenation of areas of the myocardium with impaired blood flow.

For cardiac arrhythmias(supraventricular tachycardia, atrial fibrillation and ventricular extrasystole) metoprolol lowers the heart rate and the number of ventricular extrasystoles).

With myocardial infarction metoprolol reduces mortality by reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. The mechanism of this effect is twofold:

(1) central excitation of the vagus nerve has a beneficial effect on the electrical stability of the myocardium,

(2) blocking the effects of the sympathetic nervous system reduces myocardial contractility, heart rate, and blood pressure. A decrease in mortality can also be observed with metoprolol in both the early and late phases, as well as in high-risk patients (suffering from cardiovascular diseases) and patients with diabetes mellitus. The use of the drug after myocardial infarction reduces the likelihood of non-fatal re-infarction.

treatment of functional heart disorders with palpitations.

Metoprolol can be used for prevention of migraine attacks.

At hyperthyroidism metoprolol reduces the clinical manifestations of the disease, so it can be used as an additional therapy.

Indications for use

Arterial hypertension (as monotherapy or in combination with other antihypertensive drugs;

Stable and unstable angina (as monotherapy or in combination with other antianginal agents, as well as for the prevention of angina attacks)

Secondary prevention after myocardial infarction (maintenance therapy)

Cardiac arrhythmias (sinus tachycardia, supraventricular tachycardia, ventricular extrasystoles)

Prevention of migraine attacks

Functional disorders of cardiac activity, accompanied by tachycardia (including hyperthyroidism)

Dosage and administration

The tablets can be taken with or without food. If necessary, the tablet can be divided into equal doses. The dose is selected individually to avoid excessive bradycardia.

With arterial hypertension: the recommended initial dose is 25-50 mg twice a day (morning and evening). With insufficient clinical effect, the daily dose can be increased to 100 mg twice a day, or Egilok can be used in combination with other antihypertensive drugs. The maximum dose is 200 mg per day, divided into several doses.

For angina pectoris: the recommended initial dose is 25-50 mg 2-3 times a day. With insufficient clinical effect, this dose can be gradually increased to 200 mg per day or Egilok can be used in combination with other antianginal drugs.

Maintenance therapy after myocardial infarction: recommended dose

50-100 mg twice a day (morning and evening).

For arrhythmias: the recommended initial dose is 25-50 mg 2-3 times a day. With insufficient clinical effect, this dose can be gradually increased to 200 mg or Egilok can be used in combination with other antiarrhythmic drugs.

To prevent migraine attacks: the recommended dose is 50 mg twice a day (morning and evening); if necessary, it can be increased to 100 mg twice a day.

With functional disorders of cardiac activity, accompanied by tachycardia (including hyperthyroidism): the recommended daily dose is 50 mg twice a day (morning and evening); if necessary, it can be increased to 100 mg twice a day.

Special patient groups:

When prescribing the drug patients with impaired renal function or the elderly there is no need to adjust the dosing regimen.

When prescribing the drug patients with severe hepatic impairment(for example, in patients with cirrhosis who underwent bypass surgery) its dose may need to be reduced. In patients with cirrhosis of the liver, there is no need to adjust the dosing regimen due to the low binding of metoprolol to plasma proteins (5-10%).

Children and adolescents under the age of 18

There is limited experience with the drug in children and adolescents. There are no data on the efficacy and safety of the use of Egilok tablets.

Side effects

The side effects listed below have been reported in clinical trials and in the therapeutic use of metoprolol. In some cases, the relationship of an adverse event with the use of the drug has not been reliably established.

Very often (≥1/10)

Fatigue

Often (≥1/100 -<1/10)

Dizziness, headache

Bradycardia, cold extremities, palpitations, orthostatic hypotension, which is very rarely associated with syncope

Nausea, abdominal pain, diarrhea, constipation

Tension dyspnea

Uncommon (≥1/1000 -<1/100)

- increased symptoms of heart failure, atrioventricular block I degree, peripheral edema, pain in the heart, cardiogenic shock in patients with acute myocardial infarction

Depression, impaired concentration, sleep disturbance, drowsiness, insomnia, nightmares

Paresthesia, muscle spasms

Skin itching, rash, urticaria, psoriasis-like skin lesions, degenerative skin lesions, increased sweating

Bronchospasm (even in the absence of diagnosed obstructive pulmonary disease)

Weight gain

Rarely (≥1/10 000 -<1/1000)

Dry mouth

Complaints about paresthesia, muscle spasms, nervous irritability, anxiety

Violation of potency, violation of sexual function

Arrhythmias, myocardial conduction disorders

Altered liver function tests, hepatitis

Hair loss

Conjunctivitis, dry and irritated eyes (which may cause difficulty for contact lens wearers), blurred vision

Very rare (≥1/10,000)

Amnesia, impaired or impaired memory, confusion, hallucinations, tinnitus, hearing impairment

Exacerbation of a pre-existing peripheral circulatory disorder , increased symptoms of intermittent claudication or Raynaud's disease, gangrene in patients with previous severe peripheral circulatory disorders

photosensitivity

Exacerbation of psoriasis

Change in taste sensations

Thrombocytopenia

Joint pain (arthralgia)

Egilok should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably established.

Contraindications

Hypersensitivity to metoprolol or other components of the drug, as well as to other β-blockers

Arterial hypotension

Atrioventricular block II or III degree

Decompensated heart failure

Clinically significant sinus bradycardia

Sick sinus syndrome

Cardiogenic shock

Severe peripheral circulatory disorders

Acute myocardial infarction if:

heart rate below 45 beats per minute,

P-Q interval exceeds 240 m/s,

systolic blood pressure below 100 mm Hg.

Patients requiring continuous or intermittent treatment with inotropic agents (β-agonists)

Simultaneous intravenous administration of verapamil or other similar calcium channel blockers

Severe peripheral vascular disease with the threat of gangrene

I trimester of pregnancy and lactation

Children under 18 years of age (due to lack of sufficient clinical data).

Drug Interactions

The antihypertensive effects of the drug Egilok and other antihypertensive agents are usually summed up, therefore, in order to avoid the development of arterial hypotension, careful monitoring of the condition of patients receiving combinations of such agents is necessary. However, the summation of the effects of antihypertensive drugs can, if necessary, be used to achieve more effective control of blood pressure.

Intravenous administration of calcium channel blockers such as verapamil is not recommended for patients taking β-blockers. The simultaneous use of metoprolol with calcium channel blockers such as verapamil or diltiazem leads to an increase in negative inotropic and chronotropic effects.

Caution should be exercised when combined with the following agents

With simultaneous use with oral antiarrhythmic drugs (such as quinidine and amiodarone), as well as parasympathomimetics, there is a risk of developing arterial hypotension, bradycardia, atrioventricular blockade.

With simultaneous use with digitalis glycosides, there is a risk of developing bradycardia, conduction disturbances; metoprolol does not affect the positive inotropic effect of digitalis preparations.

With simultaneous use with other antihypertensive drugs (guanethidine, reserpine, methyldopa, clonidine, guanfacine), severe bradycardia may develop.

In combination therapy with clonidine, the latter should be discontinued a few days after the abolition of metoprolol, in order to avoid a hypertensive crisis.

With simultaneous use with barbiturates, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol, there may be a risk of arterial hypotension.

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 simultaneous use with - and -sympathomimetics, there is a risk of developing arterial hypertension, severe bradycardia, and a risk of cardiac arrest.

With simultaneous use with ergotamine, it is possible to increase peripheral circulation.

With simultaneous use with 2-sympathomimetics, functional antagonism is possible.

With simultaneous use with non-steroidal anti-inflammatory drugs (indomethacin), it is possible to reduce the hypotensive effect of metoprolol.

With simultaneous use with estrogens, the antihypertensive effect of metoprolol decreases.

When taken simultaneously with oral hypoglycemic drugs, their effect may be reduced; with insulin - an increase in the risk of developing hypoglycemia, increasing its severity and lengthening, masking the symptoms of hypoglycemia.

With the simultaneous use of Egilok enhances the effect of curare-like muscle relaxants.

With the simultaneous use of Egilok with inhibitors of microsomal liver enzymes (cimetidine, ethanol, hydralazine; serotonin reuptake inhibitors - paroxetine, fluoxetine and sertraline), it is possible to increase the effects of metoprolol due to an increase in its plasma concentration.

With the simultaneous use of Egilok with inducers of microsomal liver enzymes CYP2D6 (rifampicin and barbiturates), it is possible to 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.

During the period of therapy with Egilok, patients simultaneously taking ganglioblockers, other β-blockers (including in the form of eye drops) or MAO inhibitors should be under close medical supervision.

special instructions

Clinical experience with metoprolol in children is limited.

In patients taking metoprolol, anaphylactic shock is more severe.

Very rarely, during therapy with Egilok in patients with impaired conduction, the condition may worsen, sometimes with the development of atrioventricular blockade. If bradycardia develops during treatment, the dose of the drug should be reduced or the drug should be gradually discontinued.

Against the background of the use of Egilok, the symptoms of impaired peripheral arterial circulation may worsen.

Cancellation of the drug is carried out gradually, reducing the dose for about 14 days. With a sharp cessation of treatment, it is possible to increase the symptoms of angina pectoris and increase the risk of coronary disorders. Particular attention should be paid to patients with coronary artery disease when discontinuing the drug.

Despite the fact that cardioselective β-blockers have a lesser effect on respiratory function, compared with non-selective β-blockers, Egilok is prescribed with caution to patients with chronic obstructive airway diseases. When prescribing metoprolol to patients with bronchial asthma, the simultaneous use of β2-agonists (in the form of tablets or aerosol) is necessary.

Selective β-blockers, unlike non-selective ones, rarely affect carbohydrate metabolism or mask the symptoms of hyperglycemia. In patients with diabetes mellitus taking Egilok, blood glucose levels should be regularly monitored and, if necessary, the dose of insulin or oral hypoglycemic drugs should be adjusted.

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

If it is necessary to perform surgical intervention, it is necessary to warn the anesthesiologist about the ongoing therapy with Egilok (the choice of a drug for general anesthesia with a minimal negative inotropic effect); discontinuation of the drug is not required.

Pregnancy and lactation

The use of the drug during pregnancy requires a careful assessment of the risks and benefits. 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. Metoprolol passes into breast milk only in small amounts, however, it is recommended to stop breastfeeding.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms.

Metoprolol adversely affects the patient's ability to drive vehicles and perform work with an increased risk of accidents, especially at the beginning of treatment and while taking alcohol (dizziness and fatigue may develop). In patients whose activities require increased attention and speed of psychomotor reactions, dose selection should be decided only after assessing the patient's individual response to the drug.

Overdose

Symptoms: arterial hypotension, severe sinus bradycardia, heart failure, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia; in acute overdose - loss of consciousness, cardiogenic shock, atrioventricular blockade, coma. The first symptoms of an overdose appear 20 minutes - 2 hours after taking the drug.

The above symptoms may be aggravated while taking the drug with alcohol, other antihypertensive drugs, quinidine and barbiturates.

Treatment: Gastric lavage (if lavage is not possible and if the patient is conscious, you can induce vomiting), the appointment of adsorbents, symptomatic therapy. Intensive therapy and careful monitoring of circulatory and respiratory parameters, kidney function, blood glucose levels, blood serum electrolytes are necessary. Atropine sulfate (0.25-0.5mg IV for adults, 10-20mcg/kg for children) should be given prior to gastric lavage (due to the risk of vagus nerve stimulation). In severe arterial hypotension, bradycardia and threatening heart failure - intravenous administration of β-agonists at intervals of 2-5 minutes or by infusion until the desired effect is achieved, or intravenous administration of atropine. In the absence of a positive effect, dopamine, dobutamine or norepinephrine are used. The administration of glucagon at doses of 1-10 mg may also be useful in reversing the effects of strong β-receptor blockade. With severe bradycardia that is resistant to pharmacotherapy, implantation of a pacemaker may be required. With bronchospasm - intravenous administration of a 2-agonist (for example, terbutaline). These antidotes can be used in doses higher than therapeutic. Metoprolol cannot be effectively removed by hemodialysis.

Release form and packaging

A drug Egilok- it is a beta1-blocker, antiarrhythmic, hypotensive, antianginal.
Metoprolol suppresses the effect of increased activity of the sympathetic system on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.
With arterial hypertension, metoprolol reduces blood pressure in patients in a standing and lying position. The long-term antihypertensive effect of the drug is associated with a gradual decrease in OPSS.
In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its diastolic function. In men with mild to moderate hypertension, metoprolol reduces mortality from cardiovascular causes (primarily sudden death, fatal and non-fatal heart attack and stroke).
Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic blood pressure, heart rate and myocardial contractility. The decrease in heart rate and the corresponding lengthening of diastole when taking metoprolol provide an improvement in blood supply and oxygen uptake by the myocardium with impaired blood flow. Therefore, in angina pectoris, the drug reduces the number, duration and severity of attacks, as well as asymptomatic manifestations of ischemia and improves the patient's physical performance.
In myocardial infarction, metoprolol reduces the mortality rate, reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A decrease in mortality can also be observed with the use of metoprolol in both the early and late phases of myocardial infarction, as well as in high-risk patients and patients with diabetes mellitus. The use of the drug after myocardial infarction reduces the likelihood of non-fatal re-infarction.
In CHF against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, starting from low doses (2 × 5 mg / day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.
With supraventricular tachycardia, atrial fibrillation and ventricular premature beats, metoprolol reduces the frequency of ventricular contractions and the number of ventricular extrasystoles.
At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than the same effects of non-selective beta-blockers.
Compared to non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism. It does not increase the duration of hypoglycemic episodes.
Metoprolol causes a slight increase in the concentration of triglycerides and a slight decrease in the concentration of free fatty acids in the blood serum. There is a significant decrease in the total concentration of serum cholesterol after several years of taking metoprolol.

Pharmacokinetics

Metoprolol is rapidly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range.
Cmax in plasma is achieved 1.5-2 hours after ingestion. After absorption, metoprolol is largely metabolized by the primary passage through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with regular administration.
Reception simultaneously with food can increase the bioavailability of metoprolol by 30-40%. Metoprolol slightly (~5-10%) binds to plasma proteins. Vd is 5.6 l/kg. Metoprolol is metabolized in the liver by cytochrome P450 isoenzymes. Metabolites do not have pharmacological activity. T1 / 2 on average - 3.5 hours (from 1 to 9 hours). The total clearance is approximately 1 l / min. Approximately 95% of the administered dose is excreted by the kidneys, 5% - in the form of unchanged metoprolol. In some cases, this value can reach 30%.
Significant changes in pharmacokinetics in elderly patients have not been identified.
Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases, there is a decrease in the excretion of metabolites. In severe renal failure (glomerular filtration rate less than 5 ml / min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade.
Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after a porto-caval shunt, bioavailability may increase and total clearance from the body may decrease. After porto-caval shunting, the total clearance of the drug from the body is approximately 0.3 l / min, and the AUC increases by approximately 6 times compared with that in healthy volunteers.

Indications for use

Indications for the use of the drug Egilok are: arterial hypertension (in monotherapy or (if necessary) in combination with other antihypertensive drugs); coronary heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks; heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole); functional disorders of cardiac activity, accompanied by tachycardia; hyperthyroidism (complex therapy); prevention of migraine attacks.

Mode of application

inside, Egilok The tablets can be taken with or without food. If necessary, the tablet can be broken in half.
The dose should be adjusted gradually and individually to avoid excessive bradycardia. The maximum daily dose is 200 mg.
Recommended doses
Arterial hypertension. With mild or moderate arterial hypertension, the initial dose is 25-50 mg twice a day (morning and evening). If necessary, the daily dose can be gradually increased to 100-200 mg / day or another antihypertensive agent can be added.
Angina. The initial dose is 25-50 mg two to three times a day. Depending on the effect, this dose can be gradually increased to 200 mg per day or another antianginal drug can be added.
Maintenance therapy after myocardial infarction. The usual daily dose - 100-200 mg / day, divided into two doses (morning and evening).
Heart rhythm disorders. The starting dose is 25 to 50 mg two or three times a day. If necessary, the daily dose can be gradually increased to 200 mg / day or another antiarrhythmic agent can be added.
Hyperthyroidism. The usual daily dose is 150-200 mg per day for 3-4 doses.
Functional disorders of the heart, accompanied by a sensation of palpitations. The usual daily dose is 50 mg 2 times a day (morning and evening); if necessary, it can be increased to 200 mg in two divided doses.
Prevention of migraine attacks. The usual daily dose is 100 mg/day in two divided doses (morning and evening); if necessary, it can be increased to 200 mg / day in 2 divided doses.
Special patient groups
In case of impaired renal function, a change in the dosing regimen is not required.
With cirrhosis of the liver, a dose change is usually not required due to the low binding of metoprolol to plasma proteins (5-10%). In severe hepatic insufficiency (for example, after portocaval bypass surgery), it may be necessary to reduce the dose of Egilok.
In elderly patients, dose adjustment is not required.

Side effects

Egilok usually well tolerated by patients. Side effects are usually mild and reversible.
From the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - irritability, anxiety, impotence / sexual dysfunction; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; very rarely - amnesia / memory impairment, depression, hallucinations.
From the side of the CCC: often - bradycardia, orthostatic hypotension (in some cases, syncopal conditions are possible), coldness of the lower extremities, palpitations; infrequently - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV blockade of the first degree; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders).
From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function.
On the part of the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of the course of psoriasis.
From the respiratory system: often - shortness of breath with physical effort; infrequently - bronchospasm in patients with bronchial asthma; rarely - rhinitis.
From the sensory organs: rarely - blurred vision, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, a violation of taste sensations.
Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia.
Egilok should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably established.

Contraindications

:
Contraindications to the use of the drug Egilok are: hypersensitivity to metoprolol or any other component of the drug, as well as other beta-blockers; atrioventricular (AV) block II or III degree; sinoatrial blockade; sinus bradycardia (heart rate less than 50 bpm); sick sinus syndrome; cardiogenic shock; severe disorders of peripheral circulation; heart failure in the stage of decompensation; age up to 18 years (due to lack of sufficient clinical data); simultaneous intravenous administration of verapamil; severe form of bronchial asthma; pheochromocytoma without the simultaneous use of alpha-blockers.
Due to the lack of clinical data, Egilok is contraindicated in acute myocardial infarction, accompanied by a heart rate below 45 beats / min, with a PQ interval of more than 240 ms and a SBP below 100 mm Hg.

Art.
With caution: diabetes mellitus; metabolic acidosis; bronchial asthma; COPD; renal/liver failure; myasthenia gravis; pheochromocytoma (when used simultaneously with alpha-blockers); thyrotoxicosis; AV block I degree; depression (including history); psoriasis; obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pregnancy; lactation period; elderly age; patients with a burdened allergic history (possible decrease in response to the use of adrenaline).

Pregnancy

:
Application of the drug Egilok not recommended during pregnancy. The use of the drug is possible only if the benefit to the mother outweighs the potential risk to the fetus. If the drug is necessary, you should carefully monitor the fetus, and then the newborn for several days (48-72 hours) after delivery, because. possible development of bradycardia, respiratory depression, lowering blood pressure and hypoglycemia.
Despite the fact that when taking therapeutic doses of metoprolol, only small amounts of the drug are excreted into breast milk, the newborn should be kept under observation (possible bradycardia). The use of the drug during lactation is not recommended. If necessary, the use of the drug during lactation is recommended to stop breastfeeding.

Interaction with other drugs

Antihypertensive effects of the drug Egilok and other antihypertensive drugs when used together are usually enhanced. In order to avoid arterial hypotension, careful monitoring of patients receiving combinations of such agents is necessary. However, the summation of the effects of antihypertensive drugs can be used if necessary to achieve effective control of blood pressure.
The simultaneous use of metoprolol and CCBs such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. The intravenous administration of CCBs such as verapamil should be avoided in patients receiving beta-blockers.
Caution should be exercised when taken concomitantly with the following agents
Oral antiarrhythmic drugs (such as quinidine and amiodarone) - risk of bradycardia, AV blockade.
Cardiac glycosides (risk of bradycardia, conduction disturbances; metoprolol does not affect the positive inotropic effect of cardiac glycosides).
Other antihypertensive drugs (especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine groups) - due to the risk of hypotension and / or bradycardia.
Cessation of the simultaneous use of metoprolol and clonidine should be started by canceling metoprolol, and then (after a few days) clonidine; if clonidine is discontinued first, a hypertensive crisis may develop.
Some drugs that act on the central nervous system, such as hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol, increase the risk of arterial hypotension.
Means for anesthesia (risk of oppression of cardiac activity).
Alpha- and beta-sympathomimetics (risk of arterial hypertension, significant bradycardia; possibility of cardiac arrest).
Ergotamine (increased vasoconstrictor effect).
Beta1-sympathomimetics (functional antagonism).
NSAIDs (eg indomethacin) - may weaken the antihypertensive effect.
Estrogens (may reduce the antihypertensive effect of metoprolol).
Oral hypoglycemic agents and insulin (metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia).
Curare-like muscle relaxants (increased neuromuscular blockade).
Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline) - increased effects of metoprolol due to an increase in its concentration in blood plasma.
Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to increased hepatic metabolism.
The simultaneous use of drugs that block the sympathetic ganglia, or other beta-blockers (eg eye drops), or MAO inhibitors, requires careful medical supervision.

Overdose

:
Symptoms of drug overdose Egilok: pronounced decrease in blood pressure, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma.
The symptoms listed above may increase with the simultaneous use of ethanol, antihypertensive drugs, quinidine and barbiturates.
The first signs of an overdose appear 20 minutes - 2 hours after taking the drug.
Treatment: it is necessary to carefully monitor the patient (control of blood pressure, heart rate, respiratory rate, kidney function, blood glucose concentration, blood serum electrolytes) in an intensive care unit.
If the drug has been taken recently, gastric lavage with activated charcoal may reduce further absorption of the drug (if lavage is not possible, vomiting can be induced if the patient is conscious).
In case of an excessive decrease in blood pressure, bradycardia and the threat of heart failure - in / in, with an interval of 2-5 minutes, beta-adrenergic agonists are prescribed - until the desired effect is achieved, or 0.5-2 mg of atropine is administered intravenously. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine). With hypoglycemia - the introduction of 1-10 mg of glucagon; setting a temporary pacemaker. With bronchospasm, beta2-agonists should be administered. With convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

Storage conditions

Pills Egilok should be stored at 15-25°C. Keep out of the reach of children.

Release form

Egilok - tablets, 25 mg. 60 tab. in a brown glass bottle with a PE cap with an accordion shock absorber, with the control of the first opening. 1 vial in a cardboard box. Or 20 tab. in PVC/PVDC//aluminum foil blister. 3 blisters in a cardboard box.
Egilok - tablets, 50 mg. 60 tab. in a brown glass bottle with a PE cap with an accordion shock absorber, with the control of the first opening. 1 vial in a cardboard box. Or 15 tab. in PVC/PVDC//aluminum foil blister. 4 blisters in a cardboard box.
Egilok - tablets, 100 m g. 30 or 60 tablets. in a brown glass bottle with a PE cap with an accordion shock absorber, with the control of the first opening. 1 vial in a cardboard box.

Compound

:
1 tablet Egilok contains: active substance: metoprolol tartrate 25 mg; 50 mg and 100 mg.
Excipients: MCC - 41.5 / 83 / 166 mg; sodium carboxymethyl starch (type A) - 7.5 / 15 / 30 mg; silicon dioxide colloidal anhydrous - 2/4/8 mg; povidone (K90) - 2/4/8 mg; magnesium stearate - 2/4/8 mg.

Additionally

:
Monitoring of patients taking beta-blockers includes regular measurement of heart rate and blood pressure, blood glucose concentration in patients with diabetes mellitus. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents for oral administration should be selected individually. The patient should be taught how to calculate heart rate and should be instructed to consult a doctor if the heart rate is less than 50 bpm. When taking a dose above 200 mg per day, cardioselectivity decreases.
In heart failure, treatment with Egilok® is started only after reaching the stage of compensation of cardiac function.
It is possible to increase the severity of hypersensitivity reactions and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline) in patients with a burdened allergic history.
Anaphylactic shock may be more severe in patients taking Egilok®.
May exacerbate symptoms of peripheral arterial circulatory disorders.
Abrupt discontinuation of Egilok should be avoided. The drug should be discontinued gradually, by reducing doses over a period of approximately 14 days. Abrupt withdrawal may exacerbate angina symptoms and increase the risk of coronary disorders. Particular attention should be paid to patients with coronary artery disease when discontinuing the drug.
With exertional angina, the selected dose of Egilok® should provide heart rate at rest in 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.
Egilok may mask some of the clinical manifestations of hyperthyroidism (eg tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels. In the case of the appointment of the drug Egilok®, patients with diabetes mellitus should monitor the concentration of blood glucose and, if necessary, adjust the dose of insulin or hypoglycemic agents for oral administration.
If it is necessary to prescribe to patients with bronchial asthma, beta2-agonists are used as concomitant therapy; with pheochromocytoma - alpha-blockers.
If it is necessary to perform a surgical intervention, it is necessary to warn the surgeon / anesthesiologist about the therapy being carried out (the choice of a general anesthesia agent with a minimal negative inotropic effect), drug withdrawal is not recommended.
Drugs that reduce catecholamine stores (for example, reserpine) can enhance 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.
In elderly patients, regular monitoring of liver function is recommended. Correction of the dosing regimen is required only in the case of the appearance in elderly patients of increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (SAD is 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction; sometimes it is necessary to stop treatment. Patients with severe renal insufficiency are advised to monitor renal function.
Special monitoring of the condition of patients with depressive disorders taking metoprolol should be carried out; in case of development of depression caused by taking beta-blockers, it is recommended to stop therapy.
If progressive bradycardia occurs, the dose should be reduced or the drug should be discontinued.
Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Influence on the ability to drive vehicles and work with mechanisms. Care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration (risk of dizziness and increased fatigue).

Main settings

Name:	EGILOK
ATX code:	C07AB02 -

More and more popular among hypertensive patients is egilok, a drug produced in Hungary. Having a pressure-lowering effect, at the same time, Egilok alleviates the condition of the heart affected by complications of hypertension and atherosclerosis. The drug also helps with diseases that are not directly related to high blood pressure. Many patients prefer exactly egilok, ignoring analogues, of which there are many. What motivates them to make a particular choice?

Instructions for use

The name "egilok" is a trademark given to the drug by the manufacturer (Hungary). There is also Indian Egilok.

The INN of egilok is metoprolol. This is the main active ingredient, supplemented by auxiliary: anhydrous colloidal silicon dioxide, microcrystalline cellulose, magnesium stearate, sodium carboxymethyl starch and povidone. Dosage form of release: tablets.

Auxiliary components serve to preserve the base (active substance - metoprolol tartrate) before use. They serve as enterosorbents, emulsifiers, fillers, stabilizers. The components are arranged in such a way that they ensure the stability of the composition and the safety of the drug. Once in the body, they help the main component to fully manifest the desired action.

In Latin, egilok is Egilok, and according to the current beginning it is designated: Metoprolol tartat, if it is a fast-acting form. Prolonged egilok retard contains another metoprolol compound - succinate. Accordingly: Metoprolol succinate.

Tablets are dosed in milligrams of the active substance, three types of dosage: 25, 50, 100 mg. All of them are white or close to white, biconvex. On tablets of a smaller (25 mg) dosage, the surface is marked with a cross-shaped notch. This makes it easier to split (break) the tablet when even smaller doses are needed. Usually - at the beginning of taking the drug, when the optimal dosage is being selected, this is necessary.

Tablets of large dosages have risks that help neat breaking. The tablet preparation has no smell.

Pharmacological group, mechanism of action

Pharmacotherapeutic group of Egilok: beta1-blockers. Egilok refers to cardioselective - drugs of selective action, focused on the myocardium and the coronary vessels that feed it.

Selective beta1-blockers at a reasonable dosage work only with β1-adrenergic receptors, block only them. Another type responsible for respiration, gestation, peripheral vessels - β2-adrenergic receptors - quietly continues to work, egilok is not directed at them. The drug purposefully moves towards the intended target, finds the receptors for which it was created. Contacting them, egilok does not allow catecholamines to produce a strong shake-up of the body with provoking factors:

1. emotional stress;
2. Increased physical activity;
3. A sharp change in the weather (almost 100% of "vascular" patients react to this with a deterioration in their condition).

The sympathetic system under the action of Egilok reduces activity in relation to the myocardium. Egilok, blocking β1-adrenergic receptors, slows down the pulse, reduces four important values ​​​​at once: heart rate, cardiac output, contractility and blood pressure numbers.

Such support to the heart and its vessels improves the quality of life, significantly prolongs it.

When blocking beta1-adrenergic receptors, the heart works calmly. Its blood supply is carried out more fully and without overload, at the moment of relaxation (diastolic phase) of the ventricles. The group's medicines are a lucky find for pharmacists. Egilok () is a typical representative of a number of beta-blockers.

The problem of patients with high blood pressure is left ventricular dysfunction, an increase in the ventricle from excessive load (blood pressure) on it. Regular long-term use of Egilok allows you to reverse this pathology. The ventricle, without experiencing overload, changes its size: it returns closer to normal.

Normalization of the size and functions of the left ventricle, restoration of the time needed for rest (diastole) has a direct impact on the survival of patients. Mortality from vascular accidents, especially in men, is significantly reduced. From what they take Egilok tablets: to prevent such misfortunes as heart attacks, strokes, cases of sudden death. If hypertension is moderate, “mild”, then the therapeutic effect is more pronounced.

The need of the heart muscle for oxygen supply with blood decreases, blood filling increases. The preload on the heart is reduced, it does not need to make as much effort to pump blood as before taking the medicine. Oxygen is absorbed better than it happened at high heart rate and pressure.

The selectivity of Egilok is an advantage over non-selective drugs of the same group. It almost does not show (at adequate doses) a spasmodic effect on the respiratory muscles (bronchi), as well as the smooth muscles of the walls of peripheral vessels. It does not affect the tissues of the muscles that are not included in the myocardial zone. Works only cardiologically, with a positive effect.

Egilok is good for diabetics: without affecting metabolic processes, it does not provoke hypoglycemia. The secretion of insulin does not depend on the presence of metoprolol (egilok) in the blood. Cholesterol levels during long-term therapy with Egilok are significantly reduced.

Pharmacokinetics

The absorption of the active substance after passing through the metabolic barrier of the liver occurs quickly. The process improves with an increase in the percentage of bioavailability, if Egilok tablets, according to the instructions for its use, are consumed with food. The liver controls everything that enters the gastrointestinal tract, so with food it is easier to “slip through” it unchanged to egilok. It becomes more accessible to the body by 40% than taken on an empty stomach. Metabolites lose the therapeutic activity of Egilok.

The percentage of metoprolol binding to blood proteins fluctuates. It is small with a healthy liver, but reaches 10% with its pathology.

The drug is excreted by the kidneys. It can be slowed down in kidney failure, but this does not cause measurable harm.

Indications for use

For egilok, the indications for its use are similar to the use of other beta-blockers. From what these tablets are prescribed, you can understand by examining the mechanism of action of egilok. The drug is used for:

• Hypertensive disease of all stages (arterial hypertension) - monotherapy or as a component in a complex of drugs;
• Tachyarrhythmias (tachycardias) of inorganic origin - functional reversible failures of the myocardium;
• Arrhythmias with organic causes: supraventricular tachycardia, paroxysmal, atrial extrasystole, ventricular, supraventricular;
• Angina pectoris, stable course;
• Prevention of exacerbation of migraine, prevention of pain attacks;
• Hyperthyroidism (removal of symptoms, addition of specific therapeutic methods);
• Angina pectoris complicated by a heart attack - egilok in the complex of basic therapeutic measures. Treatment of a post-infarction condition, simultaneous prevention of recurrence, prevention of a new heart attack.

Instructions for use indicate at what pressure Egilok is effective. It is prescribed for any of the stages of this disease. With a slight excess of the norm of blood pressure, the drug can help alone (monotherapy). Then the instructions for use provide for a minimum - 25 mg of Egilok per reception may already be enough.

Ischemia - narrowing, infringement. In fact, there is no infringement, there is a strong narrowing of the supply arteries. In acute cases, and - blockage of them, closure of the lumen in atherosclerosis (plaques come off), thrombosis (blockage of the vessel by a thrombus). When the lumen of the vessels is narrowed, the nutrition of the myocardium is inevitably disturbed. Egilok relaxes the vessels, facilitates the passage of blood through them to the myocardium. IHD is a form of angina "with experience", its dangerous phase. By improving blood supply, nourishing the heart, egilok helps it survive.

Applied after heart attacks, protects against repeated ones, increases survival

These occur with neurosis, in those suffering from dystonia, other disorders of the nervous system or cardiovascular. Among the whole complex of symptoms, tachycardia often comes out ahead of the rest. It worries more, generates fear, intensifies itself and intensifies the rest of the symptoms. There is no better beta-blocker remedy here. Egilok will take away a frequent pulse and, having some anxiolytic, anti-anxiety effect, will calm a person. At the same time, other unpleasant symptoms will also go away: fear, sweating, tremor. Even a heart that does not have organic changes does not benefit from such an alarming state. The drug will help return everything to normal.

Arrhythmia of organic origin

Complex, severe rhythm disturbances. They are caused by various reasons: atherosclerosis, impaired conduction of myocardial impulses, pathology of the sinus node. Beta-blockers regulate the rhythm during tachycardia (reduce heart rate). Some types of extrasystoles lend themselves to egilok, the rhythm evens out. Or extrasystoles at least become less frequent, acquire a sinus rhythm instead of a chaotic one. The drug egilok is sometimes used even with implicitly expressed bradycardia - for health reasons. Special care is needed here, but it is necessary to save the patient's life. Even Egilok 25 may turn out to be an excess, it is divided, dosed at first with a quarter of such a tablet. And this small dose will still have the desired effect. Almost without slowing down the pulse contractions.

Instructions for use refer bradycardia to the contraindications of egilok, but the reviews of practicing cardiologists indicate: sometimes, in the smallest doses, it is necessary. Grinding (again contrary to the instructions), right under the tongue - for speed of action. This will save a life in an acute situation, and the selection of other drugs - only later.

If the heart rate allows (not too low), beta-blockers help out with this diagnosis. Attacks of angina pectoris, it is not without reason that it is named with the addition of the word "stress", occur during physical or mental overstrain. Egilok, taken constantly, relieves stress. Attacks become rare and manifest weakly.

Migraine, prevention of attacks

The disease is common, but little studied. The culprit of the pain today is considered dilatation (expansion) of the cerebral vessels from overfilling them with blood and high blood pressure.

By lowering blood pressure, egilok warns, blocks dilatation.

Additionally, an anti-anxiety effect works: it has been noticed that migraine attacks are a frequent occurrence in anxious individuals. No anxiety, no migraine.

The disease is not treated with beta-blockers. But with an auxiliary purpose they are used. Egilok will help to calm the frequent pulse characteristic of the disease. Along the way, the intensity of sweating, tremor, and blood pressure decrease. The symptoms of hyperthyroidism are smoothed out, this is important for the patient's well-being.

Prevention of recurrent heart attacks

The drug in combination with others helps protect a person from the risk of a recurrence of a heart attack. The weakened heart may not withstand the second heart attack. Here the role of drugs and the doctor's ability to navigate in their selection, building treatment tactics are vital.

Now you know what egilok helps with. It's time to find out when it's not shown. Contraindications to taking Egilok are:

Use with caution

• Pheochromocytoma - a combination with alpha-blockers is necessary; without them, egilok is not used.
• Diabetes mellitus is a dose-dependent effect; at high doses, stimulation of hypoglycemia is not excluded.
• Metabolic acidosis - there may be an intervention in the failure of the metabolic processes of a beta-blocker with an unpredictable result.
• Bronchial asthma - a small effect on the type 2 receptors that control the respiratory system - β2-adrenergic receptors occasionally in sensitive, asthmatic patients - occurs.
• Obliterating endarteritis, peripheral vascular pathology.
• Insufficiency - renal, hepatic: clearance problems, delayed withdrawal, an increase in the concentration of the drug above the recommended one in the body are possible.
• Depression is a stage of exacerbation or remission.
• Tendency to allergies - if it is necessary to administer anti-shock drugs (adrenaline), the body may not respond to them under the influence of egilok.
• Hyperthyroidism (thyrotoxicosis) - increased hormonal activity of the affected thyroid gland requires careful selection of drugs and doses, even for symptomatic treatment.
• COPD - severe lung disease makes the respiratory system sensitive even to almost neutral selective beta-blockers. The cardioselectivity of Egilok does not exclude micro-influences on other systems. If they are disturbed by the disease, special control is required.

Pregnancy, lactation

If both are at risk: the mother - from the abolition of Egilok, the fetus - from its use, doctors correlate the risks. If possible, a drug that is gentle on the child is selected for the pregnant woman. If such a possibility is excluded, and it is the egilok (according to vital indications) that is needed, they try to save both. The effect of the drug on the developing organism is carefully monitored.

The newborn is immediately examined, checked for possible pathological deviations of systems and organs.

In the presence of such, intensive therapy is carried out, they try to correct the negative effect of the drug obtained in utero.

The child may be under observation for a long time.

Method of application, dosage

Take the drug, not strictly linking the time of admission - with food. Do not wait minutes before or after eating. You can - right along with food, it will even be better absorbed. According to the recommendations of the instructions, the daily dose of Egilok is divided into two doses - morning and evening. The minimum is set based on the condition, concomitant diseases. Start with small doses. By gradual selection reach the optimal. At each such increasing "step" they are delayed up to two weeks - they check the effectiveness.

Daily maximum: 200 mg, no more, the risk of side effects will increase. If the recommended daily dose is exceeded, the selectivity of Egilok is partially lost. The active substance may begin to block both types of adrenergic receptors, which should not be allowed. Doctor's prescriptions should be carried out scrupulously: he knows how much to prescribe, and takes into account all the features of the drug.

The dosage of Egilok according to the type of disease can and should vary. There may be identical doses for some diagnoses.

The dosage of Egilok varies from the initial - 25 mg to the maximum - 200 mg. The selection is individual, stepwise. Reception according to the scheme: morning + evening, the dose is divided in half. Stop at the most comfortable dose that provides the expected effect. Arterial hypertension, detected in time, at the onset stage, can be corrected by Egilok monotherapy. With a persistent course of the disease, high blood pressure, well-combined drugs of other groups that lower blood pressure are added.

Start with 25 or 50 mg, according to the patient's condition and overall drug tolerance. This dosage for IHD is taken twice or thrice a day. The daily dose can be brought up to 200 mg. If such an amount is poorly tolerated, and a smaller amount did not give the desired effect, they are left in a normally tolerated amount. The treatment is corrected by the addition of another drug that complements egilok, which alleviates the patient's condition.

Functional tachyarrhythmia

Appointment: morning and evening - 50 mg. If the effect is insufficient - 100 mg. Usually monotherapy works well.

Extrasystole, tachycardia

Start with 25 or 50 mg. Multiplicity of reception: three times a day. With good tolerance, but low efficiency, the dose is increased. Do not exceed the maximum bar - 200 mg. You can practice the combined treatment of arrhythmias. It is better to start - permanently.

Stable exertional angina

The treatment regimen is similar to the treatment of coronary heart disease, since coronary artery disease is formed during the progression of angina pectoris and is one of its stages.

Prevention of migraine attacks

Dose selection is individual. Usually it is 100 mg divided into two doses. Or - the maximum daily dose of two hundred milligrams. It is also divided in half, taken twice (morning + evening).

If migraine attacks are rare, do not practice continuous use. The approach of an attack is characterized by harbingers (decreased vision, flashing bright spots before the eyes). When such precursors are present, Egilok is immediately taken in a pre-selected dose. Continue for several days.

With often annoying migraine, Egilok is indicated for use - constantly

Up to four doses per day. The maximum daily dose or - close to it (150 - 100 mg).
Prevention of recurrent heart attacks. The maximum or half daily dose of the drug (200 or 100 mg). Divided in two, reception: morning and evening.

Side effects

Egilok has side effects, which is understandable: the drug, even with its selectivity, is in the systemic circulation. Organisms are different, reactivity too. What is useful for most is not suitable for everyone. Undesirable effects from taking Egilok:

• headache, dizziness;
• Inhibition or activation of nervous processes: from excessive excitability to severe fatigue;
• Sexual dysfunction - decreased libido / potency;
• Amnestic-confabulatory syndrome (memory problems);
• Increased unmotivated anxiety;
• Feeling of cold feet;

• Drying of the mucous membranes of the mouth;
• insomnia or drowsiness;
• Symptomatic exacerbation of heart failure;
• orthostatic hypotension;
• hallucinations;
• Painful heartbeat;
• Cardiogenic shock;
• Liver failure;
• Abdominal pain,
• Violation of cardiac conduction;
• Constipation;

• Gangrene (due to aggravation of peripheral circulatory disorders);
• Vomit;
• Tinnitus;
• Conjunctivitis;
• Distortion of taste perception;
• Decreased vision;
• Rhinitis;
• Alopecia;
• Bronchospasm;
• Irritation of the mucous membrane of the eyes;
• photosensitization;
• Shortness of breath on exertion;
• Hives;
• Arthralgia;
• Strong sweating;
• Increased weight gain.

Blockade of myocardial departments (atrioventricular);

Bronchospasm;

hypoglycemia;

Cyanosis (cyanosis) of the skin;

Unconscious state;

Falling into a coma.

An overdose of the drug Egilok against the background of therapy with blood pressure-lowering drugs, taking barbiurates, in the presence of ethanol taken in the body is more dangerous. Symptoms worsen, prognosis worsens.

Help is needed urgently, hospitalization, a complex of rehabilitation measures are required.

Before the ambulance arrives, if consciousness is preserved, you can give an enterosorbent, try to induce vomiting.

drug interaction

Co-administration with antihypertensive drugs causes an additive effect. Combination therapy is prescribed, started and controlled by a doctor. The total effect is the goal of such treatment, but it should not be excessive. Busting with doses is dangerous with hypotension, which can cause a number of complications. Some of them are more dangerous than pressure rise.

It is risky to combine egilok and other beta-blockers with calcium channel blockers (slow). Especially dangerous is the intravenous use of verapamil, there is a threat of asystole (cardiac arrest).

Antiarrhythmics taken orally (cordarone, quinine) can provoke atrioventricular blockade. Severe bradycardia has not been excluded.

Do not combine egilok with cardiac glycosides: the conductive function of the heart may suffer, severe bradycardia may develop.

Reserpine, some other antihypertensive drugs are not combined with egilok, a representative of beta-blockers. The situation is fraught with hypotension, bradycardia.

If clonidine is still taken with aegiloc, long-term use of clonidine is not currently practiced. It is impossible to cancel drugs at the same time. The sequence is as follows: first stop taking metoprolol (egilok). Clonidine remains "on the drug menu" for several more days. Then it is cancelled. If you do otherwise, remove clonidine first - there is a high probability of two consequences. There is a development of a hypertensive crisis and the formation of drug dependence.

CNS depressants (neuroleptics, tranquilizers, ethanol and other substances of similar action) together with egilok can cause critical hypotension. Urgent recovery measures will be required. And if the user of a beta-blocker is given anesthesia, there is a risk of asystole.

Do not combine alpha- and beta-sympathomimetics with Egilok (sharp hypotension, clinically significant bradycardia, high risk of cardiac arrest).

Ergotamine gives a vasoconstrictor effect, a beta-blocker cannot resist it in this combination.

Egilok has many incompatibilities with drugs. NSAIDs - anti-inflammatory drugs of this type reduce its effectiveness.

Hypoglycemic and insulin activity paired with Egilok - increase (risk of hypoglycemia).

Estrogens "prevent" beta-blockers from lowering blood pressure

Inhibitors of various enzymes, neurotransmitters - the effect of the drug is enhanced by increasing its concentration in the body.

Barbiurates and other enzyme inducers inhibit metoprolol, the effect of egilok weakens.

If substances are used that block the nodes (ganglia) of the sympathetic NS (nervous system), and drugs of the same group with egilok (beta-blockers), even when it is eye drops, special control is needed. The reactions of the body to these combinations are unpredictable.

special instructions

Analogues

Egilok, as the instructions for use reveal, is the same metoprolol (price and place of production differ).

The medicine is effective, common, and necessary for many people. Egilok has many analogues in the country and around the world. Most are given a name that matches the active substance, some - according to the companies that produce them. The price of egilok is not the lowest, nor is it low: for thirty tablets of 100 mg, the patient will pay 130 - 150 rubles. You can buy a cheap analogue of egilok, instructions, composition, properties are the same: metoprolol (after agreeing a replacement with the doctor) is German, the same package is 55 rubles.

The most famous analogues:

• Metoprolol: Russia, Poland;
• Lidaloc: Russia;
• Metoprolol teva: Israel;
• Metolol: Russia;
• Metoprolol ratiopharm: Germany;
• Emsok: Germany;
• Metoprolol organic: Russia;
• Metoprolol zentiva: Slovenia;
• Egilok Retard (prolonged): Switzerland, Hungary;
• Metoprolol-Obl: Russia;
• Metoprolol succinate: India;
• Metozok: Russia;
• Metokor adifarm: Bulgaria;
• Metoprolol tartrate: Ukraine;
• Corvitol 50: Germany;
• Betalok, Betalok ZOK (prolonged): Sweden, France;
• Metocard: Russia, Poland;
• Metoprolol-acry: Russia;
• Vasocardin: Slovenia;
• Betaloc: Sweden;
• Egilok C (prolonged): Hungary;
• Serdol: Romania;
• Egilok: Hungary.

Vacation - prescription.

Result: neutral feedback

Not a bad remedy

Benefits: helps well

Cons: side effects

Egilok tablets were prescribed to me for migraine, more precisely after migraine, namely after a course of treatment, so as not to cause repeated attacks. I am 35, but migraine has been tormenting me for more than six months. I want to say that several months have already passed, and everything is fine with me, as if such an illness had never happened before. I forgot how I felt this pain. But there is one thing! Psoriasis worsened after taking the pills. The doctor did not ask me about this, and I myself did not think that Egilok should be used with caution in such cases. Now I reduce the dose of the pill, the skin has recovered.

Result: positive feedback

Helps

Benefits: effective

Disadvantages: there are contraindications

I have been taking this drug for more than fifteen years, and it was prescribed for the treatment of high blood pressure. Egilok is a Hungarian medicine, and therefore, probably, the price for it is rather big, which is not at all pleasing. Initially, she took two tablets a day, but over time, the doctor increased the dose. A big plus of the medicine is that you can take Egilok regardless of when you ate. The drug begins to act in about seven minutes, and after an hour and a half, the pressure is completely equalized and I can already calmly go about my business, even take care of the garden. I note that for 15 years of taking the drug there have never been any side effects, which is also a huge plus.

Result: negative feedback

Didn't help migraine

Benefits: Inexpensive

Cons: Doesn't help migraines

Egilok was prescribed to me by a neuropathologist in our district clinic, and I was at his appointment with complaints of migraine. Having already bought the medicine, I read the instructions for it at home and I was alerted by the fact that the drug is indicated for hypertension, on the contrary, I often suffered from low blood pressure, and I informed the doctor about this at the appointment. I decided to contact him through my therapist and tell him about my doubts, to which I was told that it's okay, take half a tablet 2 times a day, 30 days, and monitor your condition. I began to follow the prescription and after three days I noticed that my condition had changed to sluggish, some kind of "cotton". Well, I think the already low pressure has fallen! I began to expect some positive action in relation to my migraine and was disappointed, the migraine, as it was, was in no hurry to go anywhere. To recommend Egilok or not - I don’t know, unfortunately he didn’t help me with my problem.

Result: positive feedback

Lowers blood pressure

Benefits: Efficient

Cons: addictive

I often suffer from high blood pressure and the doctor prescribed to take Egilok tablets. The first year I was delighted with them, the pressure really returned to normal, my head didn’t hurt and it became much easier for me, it happened that I rarely drank a pill. But then I began to notice that I became addicted to this drug, one tablet was enough for me for just a few hours, or the pressure generally remained the same, as if I didn’t drink it at all. I had to completely abandon Egilok and take other medicines. In general, if the pressure does not rise often, then the tablets are excellent.

Result: negative feedback

It did not help, but aggravated the situation, although it may not be the case ....

Advantages: for myself - did not find

Cons: Made it worse

Doctors often advise Egilok, especially for hypertensive patients, from frequent heartbeats and dizziness. So my therapist prescribed me to take 2 times a day, 1 tablet. I responsibly approached this matter and began to eat 1 tablet after meals. On the second day, I felt so bad that I had to call an ambulance. When the doctor stopped the hypertensive crisis, he began to ask me what pills I was taking. In addition to Egilok, I also take other medications, for example, sometimes I drink sleeping pills or tablets for the gastrointestinal tract. The doctor was very surprised to learn that Egilok prescribed me, without finding out what other pills I use, since Egilok is not compatible with all pharmaceuticals. In general, I no longer take this remedy, but for the future I realized for myself that it is necessary to warn the attending physician about all the medicines that you are currently taking.

Photo of the preparation

Latin name: Egilok

ATX Code: C07AB02

Active substance: Metoprolol (Metoprolol)

Manufacturer: EGIS Pharmaceuticals PLC (Hungary)

The description applies to: 10.11.17

Egilok is a drug that is designed to treat diseases of the cardiovascular system. The use of Egilok helps to reduce the frequency of ventricular heart contractions with supraventricular tachycardia, ventricular extrasystole and atrial fibrillation.

Active substance

Metoprolol (Metoprolol).

Release form and composition

Available in the form of round, biconvex white tablets. They are sold in dark glass jars of 30 and 60 tablets, in cardboard packages.

Indications for use

• myocardial infarction;
• angina;
• arterial hypertension;
• heart rhythm disturbances;
• migraine (in complex therapy);
• hyperthyroidism (as part of complex treatment).

Contraindications

• heart failure in the phase of decompensation;
• SSSU;
• sinoatrial blockade;
• cardiogenic shock;
• severe arterial hypotension;
• angiospastic angina;
• AV blockade of the second and third degree;
• severe bradycardia;
• persons under 18 years of age;
• hypersensitivity to metoprolol and other components of the drug;
• breastfeeding.

With extreme caution, it is prescribed for the following pathologies: metabolic acidosis, diabetes mellitus, bronchial asthma, obliterating peripheral vascular disease, chronic obstructive pulmonary disease, chronic renal failure, myasthenia gravis, psoriasis, depression, chronic liver failure and thyrotoxicosis.

Instructions for use Egilok (method and dosage)

Tablets are taken orally, regardless of the meal. For ease of swallowing, the tablet can be broken in half.

The dosage is selected individually in each case. The maximum daily dosage should not exceed 200 mg.

For the treatment of moderate or mild hypertension, therapy should be started with 25-50 mg twice a day (in the morning and afternoon). The dosage can be gradually increased to 100-200 mg per day or combined with other antihypertensive agents.

• With angina pectoris, treatment begins with 25-50 mg 2-3 times a day. Gradually, the dosage can be increased to 200 mg per day.
• After myocardial infarction for maintenance therapy, 100-200 mg is prescribed. Which are divided into two equivalent methods.
• In violation of the heart rhythm, treatment should begin with 25-50 mg 2-3 times a day. Gradually, the dosage can be increased to 200 mg.
• For the treatment of hyperthyroidism, 150-200 mg is prescribed in 3-4 doses.
• With functional disorders of the heart, 50 mg is prescribed twice a day, if necessary, the dose can be increased to 200 mg.
• For the prevention of migraine, it is necessary to take 100 mg in two doses, with the possibility of increasing to 200 mg.

Side effects

The use of tablets can cause the following side effects:

• on the part of the cardiovascular system: palpitations, sinus bradycardia, orthostatic hypotension, decreased myocardial contractility, impaired myocardial conduction, cardialgia, arrhythmia, temporary aggravation of symptoms of chronic heart failure;
• from the nervous system: weakness, fatigue, headache, inhibition of motor and mental reactions, depression, paresthesia in the limbs, insomnia or drowsiness, confusion, asthenic syndrome, nightmares, short-term memory impairment;
• from the gastrointestinal tract: abdominal pain, dry mouth, constipation, nausea, vomiting, taste changes, hyperbilirubinemia;
• from the hematopoietic system: leukopenia, agranulocytosis, thrombocytopenia;
• from the respiratory system: difficulty exhaling, nasal congestion, shortness of breath;
• dermatological reactions: skin itching, urticaria, rash, exacerbation of psoriasis, increased sweating, photodermatosis, exanthema, skin flushing, reversible alopecia;
• others: decreased libido and potency, weight gain, back pain, hypoglycemia, decreased vision, tinnitus, conjunctiva.

Overdose

An overdose of the drug is manifested by the following symptoms: sinus bradycardia, heart failure, lowering blood pressure, vomiting, nausea, cyanosis, coma, loss of consciousness. The first signs appear half an hour or 2 hours after an overdose.

Treatment is carried out in intensive care. Gastric lavage, activated charcoal are recommended, and symptomatic therapy is also used. Additionally, the introduction of norepinephrine or dobutamine is recommended; with convulsions - diazepam; with bronchospasm, beta2-agonists are prescribed.

Analogues

Analogues for the ATX code: Betaloc, Vasocardin, Metroprolol, Serdok, Emzok.

Drugs with a similar mechanism of action (coincidence of the ATC code of the 4th level): Atenolol Belupo.

Do not make the decision to change the drug yourself, consult your doctor.

pharmachologic effect

Egilok is an effective drug that belongs to beta1-blockers. The main active ingredient of the drug is metoprolol. This substance has hypotensive, antiarrhythmic and antianginal effects. By blocking beta1-adrenergic receptors, metoprolol reduces the excitatory effect of the sympathetic nervous system on the heart, and also instantly reduces blood pressure and heart rate. As for the hypotensive effect of the drug, it is quite long, since the resistance of peripheral vessels decreases gradually.

• Prolonged use at high blood pressure may lead to a decrease in the mass of the left ventricle. The drug reduces cardiovascular mortality in males with moderately elevated blood pressure.
• Due to a decrease in heart rate and blood pressure, it reduces the need for oxygen in the heart muscle, due to which the diastole is lengthened. This effect reduces the frequency of angina attacks and significantly improves the quality of life and physical condition of the patient.
• Indications for Egilok are atrial fibrillation, supraventricular tachycardia and ventricular extrasystole. With these pathologies, the medicine helps to reduce the ventricular heart rate. Regular intake of the drug for several years leads to a decrease in blood cholesterol.

special instructions

• Before starting therapy and during treatment, blood pressure and heart rate should be monitored. If the heart rate falls below 50 beats per minute, medical attention is required.
• Patients with diabetes should regularly monitor their glucose levels and, if necessary, adjust the dosage of insulin.
• It should be discontinued gradually, reducing the dosage over two weeks to avoid withdrawal syndrome, coronary disorders and angina pectoris.
• Patients wearing contact lenses may experience decreased tear secretion.
• It is recommended to exercise caution when driving vehicles and when engaging in potentially hazardous activities that require increased concentration.

During pregnancy and breastfeeding

Contraindicated during pregnancy and breastfeeding.

In childhood

Contraindicated in children and adolescents under 18 years of age.

In old age

Elderly people do not require dose adjustment.

For impaired renal function

Patients with impaired renal function do not require dosage adjustment.

For impaired liver function

With special care is prescribed for liver failure.