Correct dosage of the antihypertensive drug Egilok. Recommendations for the use of Egilok Egilok 25 instructions for use

APPROVED

By order of the chairman
Pharmaceutical Control Committee

Ministry of Health

Republic of Kazakhstan

From "____"______________200

№ ______________

Instructions for medical use

Medicine

EGILOK®

Tradename

International nonproprietary name

Metoprolol

Dosage form

Tablets 25mg, 50mg, 100mg

Compound

One tablet contains

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

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

Description

25 mg tablets: white or off-white, round, biconvex tablets, with a cross-shaped dividing line and a double bevel (double snap shape) on one side and engraved with a stylized letter "E" and the number 435 on the other side, with little or no odor.

50 mg tablets: white or off-white, round, biconvex tablets, scored on one side and engraved with a stylized letter "E" and the number 434 on the other side, with little or no odor.

100 mg tablets: white or off-white, round, biconvex tablets, beveled, scored on one side and engraved with a stylized letter “E” and the number 432 on the other side, with little or no odor.

Pharmacotherapeutic group

Antihypertensive drugs. Beta-blockers are selective.

ATC code C07A B02

Pharmacological properties

Pharmacokinetics

Metoprolol is quickly and completely absorbed from the gastrointestinal tract.

In the therapeutic dose range, the drug is characterized by linear pharmacokinetics. The maximum concentration in blood plasma is achieved 1.5-2 hours after administration. Despite significant individual variations in plasma drug levels, these differences are minor in each individual patient. After absorption, metoprolol undergoes significant first-pass metabolism through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with multiple doses. At the same time, eating can increase the bioavailability of metoprolol by 30 - 40%. Binds to plasma proteins by approximately 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 enzymes. Metabolites have no clinical significance. The 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 dose taken orally is excreted in the urine, of which 5% is unchanged (in some cases it can reach 30%). There were no significant changes in the pharmacokinetics of metoprolol in elderly patients. 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), significant accumulation of metabolites is observed. However, this accumulation of metabolites does not enhance 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 portacaval shunt, bioavailability may increase and total clearance may decrease. After portacaval shunting, the total clearance of the drug is approximately 0.3 L/min, and the area under the concentration-time curve increases approximately 6-fold compared with healthy individuals.

Pharmacodynamics

Metoprolol is a cardioselective beta1-blocker that does not have intrinsic sympathomimetic or membrane-stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic effects.

By blocking β1-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 the heart rate, inhibits conductivity and excitability, reduces myocardial contractility) .

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

The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance. At 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. Blood pressure decreases after 15 minutes, maximum - after 2 hours; the effect lasts for 6 hours. A stable decrease is observed after several weeks of regular use.

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

In case of myocardial infarction, the drug helps limit the ischemic zone of the heart muscle and reduces the risk of developing arrhythmias, and reduces the possibility of recurrent myocardial infarction. With long-term use, the drug reduces the incidence and risk deaths at cardiovascular diseases(including risk sudden death) and the risk of recurrent infarction (including patients with diabetes mellitus.)

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity 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 atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node) and along additional pathways.

With supraventricular tachycardia, atrial fibrillation, ventricular extrasystole, sinus tachycardia in functional heart diseases and hyperthyroidism, metoprolol reduces the heart rate and the number of ventricular extrasystoles.

In therapeutic doses, Egilok has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers. Egilok has a lesser effect on insulin secretion and carbohydrate metabolism and on the activity of the heart vascular system in conditions of hypoglycemia and does not increase the duration of hypoglycemia attacks.

Metoprolol causes a slight increase in triglyceride levels and a decrease in free fatty acids in blood serum. In some cases, a slight decrease in the high-density lipoprotein (HDL) fraction was noted, which is less pronounced than in the case of the use of non-selective beta-blockers. When taken for many years, metoprolol reduces the level of total serum cholesterol.

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 drugs, as well as for the prevention of angina attacks)

Secondary prevention after myocardial infarction (maintenance therapy)

Violations heart rate(sinus tachycardia, supraventricular tachycardia, ventricular extrasystoles)

Hyperthyroidism (to lower heart rate)

Preventing migraine attacks

Functional cardiac disorders accompanied by tachycardia.

Directions for use and doses

The tablets can be taken regardless of meals. If necessary, the tablet can be divided in half. The dose is selected individually to avoid excessive bradycardia.

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

Special patient groups:

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

When prescribing the drug to patients with severe liver dysfunction (for example, patients with cirrhosis who have undergone bypass surgery), it may be necessary to reduce its dose. In patients with liver cirrhosis, there is no need to adjust the dosage regimen due to the low binding of metoprolol to plasma proteins (5-10%).

Side effects

Metoprolol is usually well tolerated by patients side effects usually mild and reversible. The following side effects have been reported in clinical trials and at therapeutic use metoprolol. In some cases, the connection between an adverse event and the use of the drug has not been reliably established.

Very often (? 10%):

Increased fatigue

Often (1-9.9%):

Dizziness, headache

Bradycardia, cold extremities, increased heart rate, orthostatic hypotension, which is very rarely associated with syncope

Nausea, abdominal pain, diarrhea, constipation

Tension dyspnea

Uncommon (0.1-0.9%):

Increased symptoms of heart failure, first degree atrioventricular block, peripheral edema, pain in the heart area

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

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

Weight gain

Rarely (0.01-0.09%):

Dry mouth

Complaints of paresthesia, muscle spasms, depression, attention disturbance, sleep disturbance, drowsiness, insomnia, nightmares, nervous excitability, anxiety

Violation of potency

Arrhythmias, myocardial conduction disorders

Changes in liver function tests

Reversible alopecia

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

Very rare (? 0.01%):

Amnesia, impaired or diminished memory, confusion, hallucinations, tinnitus

Worsening of pre-existing peripheral circulatory disorders, worsening symptoms of intermittent claudication or Raynaud's disease

Photosensitivity

Exacerbation of psoriasis

Change in taste sensations

Thrombocytopenia

Joint pain (arthralgia)

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

Contraindications

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

Atrioventricular block II or III degree

Heart failure in the stage of decompensation

Severe bradycardia

Sick sinus syndrome

Cardiogenic shock

Severe peripheral arterial circulation disorders

Acute myocardial infarction if:

Heart rate below 45 beats per minute,

P-Q interval exceeds 240 m/s,

Systolic blood pressure is below 100 mmHg.

Patients requiring chronic or intermittent treatment with inotropes (beta-agonists)

Simultaneous intravenous administration verapamil or other similar calcium channel blockers

First trimester of pregnancy and lactation period

Children's and adolescence up to 18 years of age (due to lack of sufficient clinical data).

Drug interactions

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

Intravenous administration of calcium channel blockers such as verapamil is not recommended for patients taking beta-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 drugs

When used simultaneously with oral antiarrhythmic drugs (such as quinidine and amiodarone), as well as parasympathomimetics, there may be a risk of developing arterial hypotension, bradycardia, and atrioventricular block.

When used simultaneously with digitalis glycosides, there may be a risk of developing bradycardia and conduction disorders; metoprolol does not affect the positive inotropic effect of digitalis preparations.

When used simultaneously with other antihypertensive drugs (reserpine, guanfacine, methyldopa, clonidine), severe bradycardia may develop.

At combination therapy with clonidine, the latter should be discontinued several days after metoprolol is discontinued, in order to avoid a hypertensive crisis.

When used simultaneously with barbiturates, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol, there may be a risk of developing arterial hypotension.

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

When used simultaneously with β- and β-sympathomimetics, there is a possible risk of developing arterial hypertension, severe bradycardia, and a possible risk of cardiac arrest.

When used simultaneously with ergotamine, peripheral circulatory disorders may increase.

When used simultaneously with β2-sympathomimetics, functional antagonism is possible.

When used simultaneously with non-steroidal anti-inflammatory drugs (indomethacin), the hypotensive effect of metoprolol may be reduced.

When used simultaneously with estrogens, the antihypertensive effect of metoprolol is reduced.

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

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

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

With simultaneous use of Egilok with inducers of microsomal liver enzymes (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 therapy with Egilok, patients simultaneously taking ganglion blockers, other beta-blockers (including in the form 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 proceeds more severely.

Very rarely, during therapy with Egilok, patients with conduction disorders may experience a deterioration in their condition, sometimes with the development of atrioventricular block. If bradycardia develops during treatment, the dose of the drug should be reduced or the drug should be gradually discontinued.

The use of Egilok may worsen the symptoms of peripheral circulatory disorders.

The drug is withdrawn gradually, reducing the dose over approximately 14 days. Abrupt cessation of treatment may increase the symptoms of angina and increase the risk of coronary events. Special attention when discontinuing the drug, it should be given to patients with disease coronary arteries.

Despite the fact that cardioselective beta-blockers have less effect on respiratory function compared to non-selective beta-blockers, Egilok is prescribed with caution to patients with chronic obstructive diseases respiratory tract. When prescribing metoprolol to patients with bronchial asthma simultaneous use of beta2-adrenergic agonists (in the form of tablets or aerosol) is necessary.

Selective beta-blockers, unlike non-selective ones, relatively 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 alpha-blockers.

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

Pregnancy and lactation

The use of the drug in the second and third trimesters 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 is necessary for 48-72 hours after birth, since intrauterine growth retardation, bradycardia, arterial hypotension, respiratory depression, and hypoglycemia are possible. Metoprolol penetrates only in small quantities into breast milk However, it is recommended to stop breastfeeding.

Impact on management ability vehicles and working with mechanisms

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 case of acute overdose - loss of consciousness, cardiogenic shock, atrioventricular block, coma. The first symptoms of an overdose appear 20 minutes - 2 hours after taking the drug.

Treatment: Gastric lavage (if lavage is impossible and if the patient is conscious, vomiting can be induced), administration of adsorbents, symptomatic therapy. Intensive therapy and careful monitoring of circulatory and respiratory parameters, renal function, blood glucose levels, and serum electrolytes are required. For severe arterial hypotension, bradycardia and threatening heart failure - intravenous administration of beta-agonists at intervals of 2-5 minutes or by infusion until the desired effect is achieved or intravenous administration of atropine. If there is no positive effect, dopamine, dobutamine or norepinephrine are used. Administration of glucagon in doses of 1-10 mg may also be useful in achieving reversal of the effects of strong beta-receptor blockade. In cases of severe bradycardia that are resistant to pharmacotherapy, implantation of a cardiac pacemaker may be required. For bronchospasm - intravenous administration of a β2-agonist (for example, terbutaline). These antidotes can be used in doses exceeding therapeutic ones. Metoprolol cannot be effectively removed by hemodialysis.

Release form and packaging

Tablets 25mg, 50mg (30 tablets each) and 100mg tablets (30 or 60 tablets each) in brown glass bottles. One bottle along with instructions for medical use in a cardboard box.

Storage conditions

Store at temperatures between +15 and + 25°C

Keep out of the reach of children!

Shelf life

Do not use after expiration date.

Conditions for dispensing from pharmacies

On prescription

Manufacturer

JSC PHARMACEUTICAL PLANT EGIS

1106 Budapest, st. Keresturi, 30-38 HUNGARY

Phone: (36-1) 265-5555, Fax: (36-1) 265-5529

Active ingredient: one film-coated tablet with a delayed release of 50 mg contains metoprolol (in the form of 47.5 mg of metoprolol succinate, which corresponds to 50 mg of metoprolol tartrate), 100 mg contains metoprolol (in the form of 95 mg of metoprolol succinate, which corresponds to 100 mg of metoprolol tartrate ), 200 mg contains metoprolol (in the form of 190 mg metoprolol succinate, corresponding to 200 mg metoprolol tartrate), respectively.

Excipients: microcrystalline cellulose PH 101, methylcellulose,
glycerol, corn starch, ethylcellulose, magnesium stearate.
Tablet shell: microcrystalline cellulose, hypromellose, stearic acid, titanium dioxide (E171).

Description

Appearance:
CP film-coated tablets, sustained release 50 mg: white, oval, biconvex film-coated tablets, measuring 11 x 6 mm, with a dividing line
risk on both sides.
Egnpok' CP film-coated tablets with sustained release 100 mg: white, oval, biconvex film-coated tablets, measuring 16 x 8 mm, with scoring lines on both sides.
Egilok' CP film-coated tablets with delayed release 200 mg: white, oval, biconvex film-coated tablets, measuring 19 x 10 mm, with scoring lines on both sides.

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pharmachologic effect

Ardioselective beta blocker without sympathomimetic and membrane stabilizing activity. The main effect is hypotensive. Able to reduce heart rate. Reduces the severity and frequency of angina attacks, improves the patient’s physical well-being, and reduces the risk of recurrent myocardial infarction. Has certain antiarrhythmic activity. Most effective for rhythm disturbances with increased heart rate. Egilok reduces the heart rate (HR) by reducing the automaticity of the sinus node, slowing down the conduction of the exciting impulse, reducing the excitability and contractility of the myocardium. Prevents migraine attacks. When taken in therapeutic doses, the drug has virtually no effect on the smooth muscles of the bronchi and peripheral arteries. When taken orally, the drug has maximum effect after 1.5 hours of administration. About 5% of the drug is excreted unchanged in the urine, the rest undergoes biotransformation in the liver. Therefore, if liver function is impaired, an accumulation effect of the drug may be observed and dose adjustment may be necessary.

Indications for use

Arterial hypertension (increased blood pressure), including in patients over 60 years of age; - rhythm disturbances associated with an increase in heart rate (supraventricular arrhythmias, extrasystoles); - prevention of migraine attacks; - ischemic disease hearts; - heart failure; - myocardial infarction. -

Contraindications

Sinus bradycardia with a heart rate less than 50-60 beats per minute; - AV - blockade 2 or 3 degrees; - sinoatrial block; - sick sinus syndrome; - severe peripheral circulatory disorders; - arterial hypotension (decrease in blood pressure below 90-100 mm Hg; - increased sensitivity to the components of the drug.

Pregnancy and lactation

The use of the drug during pregnancy is possible only if the expected benefit to the mother exceeds the potential possible risk for the fetus. When using the drug during pregnancy, careful monitoring (observation) of the condition of the fetus in utero is necessary, as well as observation of the newborn for several days after birth to exclude arterial hypotension, bradycardia (slow heart rate), respiratory depression, hypoglycemia (decrease in blood sugar levels). blood). Egilok is practically not excreted in breast milk; when treating the mother, constant monitoring of the state of the child’s cardiovascular and respiratory systems is necessary.

Directions for use and doses

The dosage is selected by the attending physician individually in each case.
For arterial hypertension, the initial average therapeutic dose is 50 mg/day in 1 or 2 doses. If there is no effect or hypotensive effect insignificant, it is possible to increase the dosage of the drug to 100-200 mg/day.
For angina pectoris, the drug is prescribed at a dosage of 100-200 mg/day in 1 or 2 doses.

For extrasystole and supraventricular arrhythmias, the average therapeutic dose ranges from 100-200 mg/day in 2 doses (morning and evening), distributing the drug as evenly as possible throughout the day.

For secondary prevention of myocardial infarction, patients are prescribed 200 mg/day in 2 divided doses.
To prevent migraine attacks, 100-200 mg/day of the drug is prescribed in 2 doses (morning and evening).
It should be noted that in patients with severe renal and liver dysfunction, the drug should be dosed with caution, because cumulation (i.e. accumulation) of the drug in the blood is possible.

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Side effect

From the central nervous system: increased fatigue, dizziness, headaches, depression, drowsiness, insomnia, nightmares, decreased ability to concentrate, less often - parasthesia, muscle spasms.

From the senses: rare disorders such as visual impairment, conjunctivitis, ringing in the ears.

From the cardiovascular system: bradycardia (decreased heart rate), heart failure, less often - conduction disturbances, Raynaud's syndrome.

From the outside respiratory system: shortness of breath, bronchospasm, and rhinitis may rarely occur.

From the digestive system: nausea, vomiting, diarrhea, constipation, abdominal pain, dry mouth, impaired liver function.

From the outside skin: photodermatosis, urticaria, erythema, psoriasis-like and dystrophic skin changes, alopecia (baldness), increased sweating.

Others: thrombocytopenia, weight gain.

Overdose

From the cardiovascular system: arterial hypotension, bradycardia, AV block, heart failure. From the digestive system: nausea, vomiting.

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Interaction with other drugs

The simultaneous use of Egilok with digitalis preparations, nitrates, calcium channel blockers, parasympathomimetics and other antihypertensive, antianginal (angina), antiarrhythmic drugs increases the risk of developing arterial hypotension (collapse), bradycardia, and AV block.

When used with opioid analgesics, the effects of the drugs are mutually enhanced.
Egilok enhances the effect of hypoglycemic (blood sugar-lowering) drugs. When Egilok is used together with alpha and beta adrenergic agonists, the risk of developing arterial hypotension, bradycardia, and sudden cardiac arrest increases.

Estrogens, NSAIDs (non-steroidal anti-inflammatory drugs), rifampicin, barbiturates can reduce the hypotensive effect of Egilok.
The drug enhances the effect of curare-like muscle relaxants.

Store out of the reach of children at a temperature of 15° to 25°C.

Expiration date from date of manufacture

Product description

pharmachologic effect

Cardioselective β-adrenergic receptor blocker.
Metoprolol suppresses the effects of increased activity sympathetic system on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.
For 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 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 diastolic function. In men with mild or 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. A decrease in heart rate and a corresponding prolongation of diastole when taking metoprolol ensures improved blood supply and oxygen uptake by the myocardium with impaired blood flow. Therefore, for 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 by reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes ventricular fibrillation. A reduction in mortality rates can also be observed with the use of metoprolol, both early and late. late phase myocardial infarction, as well as in patients of the group high risk and patients with diabetes. Use of the drug after myocardial infarction reduces the likelihood of non-fatal recurrent infarction. In chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken in low doses (2x5 mg/day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.
In case of supraventricular tachycardia, atrial fibrillation and ventricular extrasystoles, 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 with non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism and does not increase the duration of hypoglycemia attacks.
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 total serum cholesterol concentrations after using metoprolol for several years.

Pharmacokinetics

Suction
Metoprolol is quickly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range. Cmax in blood plasma is achieved 1.5-2 hours after oral administration. Bioavailability is approximately 50% with a single dose and approximately 70% with regular use. Taking the drug simultaneously with food can increase bioavailability by 30-40%.
Distribution
Metoprolol is slightly (approximately 5-10%) bound to plasma proteins. Vd is 5.6 l/kg.
Metabolism
After absorption, metoprolol is largely subject to a first-pass effect through the liver. Metabolized in the liver by cytochrome P450 isoenzymes. Metabolites do not have pharmacological activity.
Removal
T1/2 averages 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% as unchanged metoprolol. In some cases this value can reach 30%.
Pharmacokinetics in special clinical situations
There were no significant changes in the pharmacokinetics of metoprolol in elderly patients.
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) Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after portacaval anastomosis, bioavailability may increase, and the total clearance from the body may decrease. After portacaval shunt, the total clearance of the drug from the body is approximately 0.3 l /min, and AUC increases approximately 6 times compared to that in healthy volunteers.

Indications for use

Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);
- functional disorders of cardiac activity, accompanied by tachycardia;
- IHD (secondary prevention of myocardial infarction, prevention of angina attacks);
- heart rhythm disturbances (supraventricular arrhythmias, ventricular extrasystole);
- hyperthyroidism (as part of complex therapy);
- prevention of migraine attacks.

Use during pregnancy and lactation

The use of the drug is not recommended during pregnancy. The use of the drug is possible only when the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to prescribe the drug during pregnancy, careful monitoring of the condition of the fetus and newborn is necessary for 48-72 hours after birth, since bradycardia, arterial hypotension, hypoglycemia and respiratory depression may develop.
Despite the fact that when using the drug in therapeutic doses, only a small amount of metoprolol is excreted in breast milk, the condition of the newborn should be monitored (bradycardia is possible). The use of the drug during lactation is not recommended. If it is necessary to use Egilok® during lactation, breastfeeding should be stopped.

special instructions

When prescribing Egilok®, heart rate and blood pressure should be regularly monitored. The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation with heart rate. Patients with diabetes mellitus should regularly monitor blood glucose levels and, if necessary, adjust the dose of insulin or oral hypoglycemic drugs.
When using the drug at a dose exceeding 200 mg/day, cardioselectivity decreases.
Prescribing Egilok to patients with chronic heart failure is possible 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 there may be no effect from the administration of usual doses of epinephrine (adrenaline).
Anaphylactic shock may be more severe in patients taking Egilok®.
The use of Egilok may worsen the symptoms of peripheral circulatory disorders.
Egilok® should be discontinued gradually, gradually reducing its dose over 14 days. Abrupt cessation of treatment may increase angina attacks and the risk of developing coronary disorders. During drug withdrawal, patients with coronary artery disease should be under close medical supervision.
For exertional angina, the selected dose of Egilok® should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min.
Patients using contact lenses, should take into account that during treatment with beta-blockers, a decrease in the production of tear fluid is possible.
Egilok® may mask some clinical manifestations hyperthyroidism (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.
In diabetes mellitus, taking Egilok can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the recovery of blood glucose concentrations to normal level.
When prescribing metoprolol to patients with bronchial asthma, simultaneous use of beta2-adrenergic agonists 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 surgeon/anesthesiologist about the therapy being carried out with Egilok (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not required.
Drugs that reduce catecholamine levels (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.
When prescribing the drug to elderly patients, liver function should be regularly monitored. Correction of the dosage regimen is required only if increasing bradycardia appears in elderly patients (Patients with renal failure In severe cases, monitoring of renal function is recommended.
Special monitoring of the condition of patients with depressive disorders. If depression occurs due to the use of beta-blockers, therapy should be discontinued.
If progressive bradycardia occurs, the dose should be reduced or the drug discontinued.
Use in pediatrics
Due to the lack of sufficient clinical data, the drug is not recommended for use in children and adolescents under 18 years of age.
Impact on the ability to drive vehicles and operate machinery
Caution must be exercised when driving and engaging in potentially dangerous activities. dangerous species activities that require increased concentration (risk of dizziness and increased fatigue).

With caution (Precautions)

The drug should be prescribed with caution for diabetes mellitus; metabolic acidosis; bronchial asthma; COPD; renal/liver failure; myasthenia gravis; pheochromocytoma (when used simultaneously with alpha-blockers); thyrotoxicosis; AV blockade of the first degree, depression (including a history); psoriasis; obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pregnancy; during lactation; elderly patients; patients with a history of allergic reactions (possible decreased response when using adrenaline).

Contraindications

Cardiogenic shock;
- AV blockade II and III degrees;
- sinoatrial blockade;
- SSSU;
- sinus bradycardia (HR - heart failure in the stage of decompensation;
- severe peripheral circulatory disorders;
- age under 18 years (due to lack of sufficient clinical data);
- simultaneous intravenous administration of verapamil;
- severe form of bronchial asthma;
- pheochromocytoma without simultaneous use of alpha-blockers;
- hypersensitivity to metoprolol or any other component of the drug;
- increased sensitivity to other beta-blockers.
Due to insufficient clinical data, Egiolok® is contraindicated in acute heart attack myocardium, accompanied by a heart rate of 240 ms, and systolic blood pressure

Directions for use and doses

The drug should be taken orally during or regardless of meals. If necessary, the tablet can be broken in half.
The dose should be adjusted gradually and individually to avoid the development of excessive bradycardia. The maximum daily dose is 200 mg.
When soft or moderate degree arterial hypertension, the initial dose is 25-50 mg 2 times a day (morning and evening). If necessary, the dose can be gradually increased to 100-200 mg/day or another antihypertensive agent can be added.
For angina pectoris, the initial dose is 25-50 mg 2-3 times a day. Depending on the effect, the dose can be gradually increased to 200 mg/day or another antianginal drug can be added.
The recommended dose of the drug for maintenance therapy after myocardial infarction is 100-200 mg/day, divided into 2 doses (morning and evening).
For cardiac arrhythmias, the initial dose is 25-50 mg 2-3 times a day. If necessary, the daily dose can be gradually increased to 200 mg/day or another antiarrhythmic agent can be added.
For hyperthyroidism, the usual daily dose is 150-200 mg in 3-4 doses.
At functional disorders heart disease, accompanied by a feeling of palpitations, the usual dose is 50 mg 2 times a day (morning and evening); if necessary, the dose can be increased to 200 mg in 2 doses.
For the prevention of migraine attacks, the recommended dose is 100 mg/day in 2 divided doses (morning and evening); if necessary, the dose can be increased to 200 mg/day in 2 divided doses.
In patients with impaired renal function, no change in dosage regimen is required.
In liver cirrhosis, dose changes are usually not required due to the low binding of metoprolol to plasma proteins. In case of severe liver failure (for example, after portacaval shunting), it may be necessary to reduce the dose of Egilok®.
In elderly patients, no dose adjustment is required.

Overdose

Symptoms: marked decrease in blood pressure, sinus bradycardia, AV block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase when used simultaneously with ethanol, antihypertensive drugs, quinidine and barbiturates.
The first symptoms of overdose appear 20 minutes to 2 hours after taking the drug.
Treatment: careful monitoring of the patient is necessary (monitoring blood pressure, heart rate, respiratory rate, renal function, blood glucose concentration, serum electrolytes) in the department intensive care. If the drug has been taken recently, gastric lavage using activated carbon may reduce further absorption of the drug (if lavage is not possible, vomiting may be induced if the patient is conscious). In case of excessive decrease in blood pressure, bradycardia and threat of heart failure - intravenous administration of beta-adrenergic agonists (until the desired effect is achieved) or intravenous administration of 0.5-2 mg of atropine at intervals of 2-5 minutes. If there is no positive effect, dopamine, dobutamine or norepinephrine (norepinephrine). For hypoglycemia - administration of 1-10 mg of glucagon, installation of a temporary pacemaker. For bronchospasm - administration of beta2-adrenergic agonists. For convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

Side effect

Egilok® is usually well tolerated by patients. Side effects are usually mild and reversible. The following side effects have been reported in clinical trials and during therapeutic use of metoprolol. In some cases, the connection between an adverse event and the use of the drug has not been reliably established. The following parameters for the frequency of side effects are defined as follows: very often (>10%), often (1-9.9%), infrequently (0.1-0.9%), rarely (0.01-0.09%), very rarely, including isolated messages (Co side of the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - increased excitability, anxiety; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; , depression, hallucinations.
From the outside of cardio-vascular system: often - bradycardia, orthostatic hypotension (in some cases syncope is possible), coldness lower limbs, feeling of heartbeat; uncommon - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV block of the first degree; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders).
From the respiratory system: often - shortness of breath with physical effort; uncommon - bronchospasm in patients with bronchial asthma; rarely - rhinitis.
From the outside digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function.
From the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis.
From the senses: rarely - blurred vision, dryness and/or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, disturbance of taste.
From the reproductive system: rarely - impotence/sexual dysfunction.
Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia.
The use of Egilok® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably determined.

Compound

In 1 tab.
metoprolol tartrate 25 mg
Excipients: microcrystalline cellulose - 41.5 mg, sodium carboxymethyl starch (type A) - 7.5 mg, colloidal anhydrous silicon dioxide - 2 mg, povidone K90 - 2 mg, magnesium stearate - 2 mg.

Interaction with other drugs

The antihypertensive effects of Egilok® when used simultaneously with other antihypertensive drugs are usually enhanced. To avoid hypotension, careful monitoring of patients receiving combinations of these drugs is necessary. However, the summation of the effects of antihypertensive drugs can be used, if necessary, to achieve effective blood pressure control.
The simultaneous use of metoprolol and slow calcium channel blockers such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. IV administration of calcium channel blockers such as verapamil should be avoided in patients receiving beta-blockers.
Combinations requiring caution
Oral antiarrhythmic drugs(such as quinidine and amiodarone): risk of developing bradycardia, AV block.
Cardiac glycosides: risk of developing bradycardia, conduction disorders; metoprolol does not affect the positive inotropic effect of cardiac glycosides.
Other antihypertensive drugs (especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine groups): risk of developing arterial hypotension and/or bradycardia.
Discontinuation of the simultaneous use of metoprolol and clonidine should be started by discontinuing metoprolol, and then (after a few days) clonidine; If clonidine is first discontinued, a hypertensive crisis may develop.
Some drugs acting on the central nervous system (for example, hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol): risk of developing arterial hypotension.
Anesthesia: risk of cardiac depression.
Alpha and beta sympathomimetics: risk of developing arterial hypertension, significant bradycardia, possible cardiac arrest.
Ergotamine: increased vasoconstrictor effect.
Beta2-sympathomimetics: functional antagonism.
NSAIDs (for example, indomethacin): the antihypertensive effect may be weakened.
Estrogens: the antihypertensive effect of metoprolol may be reduced.
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 (eg, cimetidine, ethanol, hydralazine; selective inhibitors serotonin reuptake agents, for example, paroxetine, fluoxetine and sertraline): the effects of metoprolol may be enhanced due to an increase in its concentration in the blood plasma.
Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to increased hepatic metabolism.
Concomitant use of sympathetic ganglion blockers or other beta blockers (eg, eye drops) or MAO inhibitors requires close medical monitoring.

Release form

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

A drug Egilok- it is beta1-adrenergic blocking, antiarrhythmic, hypotensive, antianginal.
Metoprolol suppresses the effect of increased sympathetic system activity on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.
For 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 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 diastolic function. In men with mild or 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. A decrease in heart rate and a corresponding prolongation of diastole when taking metoprolol ensures improved blood supply and oxygen uptake into the myocardium with impaired blood flow. Therefore, for 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 by reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A reduction 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. Use of the drug after myocardial infarction reduces the likelihood of non-fatal recurrent infarction.
In case of CHF against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, starting with 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.
In case of supraventricular tachycardia, atrial fibrillation and ventricular extrasystoles, 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 attacks.
Metoprolol causes slight increase triglyceride concentrations and a slight decrease in serum free fatty acid concentrations. There is a significant decrease in total serum cholesterol concentrations after several years of taking metoprolol.

Pharmacokinetics

Metoprolol is quickly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range.
Cmax in blood plasma is achieved 1.5-2 hours after oral administration. After absorption, metoprolol undergoes significant first-pass metabolism through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with regular use.
Taking with food can increase the bioavailability of metoprolol by 30-40%. Metoprolol is slightly (~5-10%) bound 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% as unchanged metoprolol. In some cases this value can reach 30%.
No significant changes in pharmacokinetics were detected in elderly patients.
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 (rate glomerular filtration 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 portacaval shunt, bioavailability may increase and overall body clearance may decrease. After portacaval shunt, the total clearance of the drug from the body is approximately 0.3 L/min, and the AUC increases approximately 6 times compared with that in healthy volunteers.

Indications for use

Indications for 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 food or without regard to meals. 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. For 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 pectoris. 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 is 100-200 mg/day, divided into two doses (morning and evening).
Heart rhythm disturbances. 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 in 3-4 doses.
Functional heart disorders, accompanied by a feeling 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 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
If renal function is impaired, no change in dosage regimen is required.
In liver cirrhosis, a dose change is usually not required due to the low binding of metoprolol to plasma proteins (5-10%). In case of severe liver failure (for example, after portacaval shunt surgery), it may be necessary to reduce the dose of Egilok.
In elderly patients, no dose adjustment is 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 - increased excitability, anxiety, impotence/sexual dysfunction; uncommon - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; very rarely - amnesia/memory impairment, depression, hallucinations.
From the cardiovascular system: often - bradycardia, orthostatic hypotension (in some cases, syncope is possible), coldness of the lower extremities, palpitations; uncommon - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV block 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.
From the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis.
From the respiratory system: often - shortness of breath with physical effort; uncommon - bronchospasm in patients with bronchial asthma; rarely - rhinitis.
From the senses: rarely - blurred vision, dryness and/or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, disturbance of taste.
Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia.
Taking Egilok should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably determined.

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 block; sinus bradycardia (heart rate less than 50 beats/min); sick sinus syndrome; cardiogenic shock; severe peripheral circulatory disorders; heart failure in the stage of decompensation; age under 18 years (due to lack of sufficient clinical data); simultaneous intravenous administration of verapamil; severe form of bronchial asthma; pheochromocytoma without simultaneous use of alpha-blockers.
Due to insufficient 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 SBP below 100 mmHg.

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 of the first degree; depression (including history); psoriasis; obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pregnancy; lactation period; elderly age; patients with a history of allergic reactions (possible decreased response when using adrenaline).

Pregnancy

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

Interaction with other drugs

Antihypertensive effects of the drug Egilok and other antihypertensive drugs for joint use usually intensify. To avoid hypotension, careful monitoring of patients receiving combinations of these drugs is necessary. However, the summation of the effects of antihypertensive drugs can be used, if necessary, to achieve effective blood pressure control.
Concomitant use of metoprolol and CCBs such as diltiazem and verapamil may lead to increased negative inotropic and chronotropic effects. IV administration of CCBs such as verapamil should be avoided in patients receiving beta-blockers.
Caution should be exercised when taken concomitantly with the following drugs
Oral antiarrhythmic drugs (such as quinidine and amiodarone) - risk of bradycardia, AV block.
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.
Stopping the simultaneous use of metoprolol and clonidine should definitely begin by stopping metoprolol, and then (after a few days) clonidine; If clonidine is first discontinued, 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.
Anesthesia (risk of cardiac depression).
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 (possibly reducing 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 the blood plasma.
Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to increased hepatic metabolism.
Concomitant use of sympathetic ganglion blockers or other beta blockers (eg eye drops), or MAO inhibitors, requires careful medical supervision.

Overdose

:
Symptoms of drug overdose Egilok: marked 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 be exacerbated by concomitant use of ethanol, antihypertensive drugs, quinidine and barbiturates.
The first signs of overdose appear 20 minutes - 2 hours after taking the drug.
Treatment: careful monitoring of the patient is necessary (monitoring blood pressure, heart rate, respiratory rate, renal function, blood glucose concentration, serum electrolytes) in the 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 excessive decrease in blood pressure, bradycardia and threat of heart failure, beta-agonists are prescribed intravenously at intervals of 2-5 minutes until the desired effect is achieved, or 0.5-2 mg of atropine is administered intravenously. If there is no positive effect, dopamine, dobutamine or norepinephrine (norepinephrine). For hypoglycemia - administration of 1-10 mg of glucagon; installation of a temporary pacemaker. For bronchospasm, beta2-agonists should be administered. For convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

Storage conditions

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

Release form

Egilok - tablets, 25 mg. 60 tablets each. in a brown glass bottle with a PE cap with an accordion shock absorber, with first opening control. 1 fl. in a cardboard box. Or 20 tablets. in a blister made of PVC/PVDC//aluminum foil. 3 blisters in a cardboard box.
Egilok - tablets, 50 mg. 60 tablets each. in a brown glass bottle with a PE cap with an accordion shock absorber, with first opening control. 1 fl. in a cardboard box. Or 15 tablets. in a blister made of PVC/PVDC//aluminum foil. 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 first opening control. 1 fl. 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; colloidal silicon dioxide 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. 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 instructed about the need for medical consultation if the heart rate is less than 50 beats/min. When taking a dose above 200 mg per day, cardioselectivity decreases.
In case of heart failure, treatment with Egilok® begins only after reaching the stage of compensation of cardiac function.
Possible increased severity of reactions hypersensitivity and the lack of effect from the administration of usual doses of epinephrine (adrenaline) in patients with a history of allergic reactions.
Anaphylactic shock may be more severe in patients taking Egilok®.
May increase symptoms of peripheral arterial circulation disorders.
Abrupt discontinuation of Egilok® should be avoided. The drug should be discontinued gradually by reducing doses over approximately 14 days. Abrupt withdrawal may worsen angina symptoms and increase the risk of coronary events. When discontinuing the drug, special attention should be paid to patients with coronary artery disease.
For exertional angina, the selected dose of Egilok® should ensure the heart rate at rest is within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min.
Patients who use contact lenses should take into account that during treatment with beta-blockers, there may be a decrease in the production of tear fluid.
Egilok may mask some clinical manifestations of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated as it can increase symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels. When prescribing Egilok® to patients with diabetes mellitus, blood glucose concentrations should be monitored and, if necessary, the dose of insulin or oral hypoglycemic agents should be adjusted.
If it is necessary to prescribe to patients with bronchial asthma, beta2-adrenergic stimulants are used as concomitant therapy; for pheochromocytoma - alpha-blockers.
If surgical intervention is necessary, it is necessary to warn the surgeon/anesthesiologist about the therapy being performed (choosing a general anesthesia agent with minimal negative inotropic effect); discontinuation of the drug is not recommended.
Drugs that reduce catecholamine reserves (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.
In elderly patients, regular monitoring of liver function is recommended. Correction of the dosage regimen is required only if increasing bradycardia (less than 50 beats/min), a pronounced decrease in blood pressure (sBP is 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, appears in elderly patients. severe violations liver functions; sometimes it is necessary to stop treatment. In patients with severe renal failure, monitoring of renal function is recommended.
Special monitoring of the condition of patients with depressive disorders taking metoprolol should be carried out; in case of depression caused by taking beta-blockers, it is recommended to discontinue therapy.
If progressive bradycardia occurs, the dose should be reduced or the drug discontinued.
Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Impact on the ability to drive vehicles and operate machinery. Care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration (risk of dizziness and fatigue).

Main settings

Name:	EGILOK
ATX code:	C07AB02 -

In this article you can find instructions for use medicinal product Egilok. Feedback from site visitors - consumers - is presented of this medicine, as well as the opinions of specialist doctors on the use of Egilok in their practice. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Egilok in the presence of existing structural analogues. Use for treatment of ischemic heart disease and arterial hypertension in adults, children, as well as during pregnancy and lactation. Combination of the drug with alcohol.

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

By blocking beta1-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-, bathmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility).

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

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

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

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

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 via the AV node) and along additional paths.

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 migraine.

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

When used in average therapeutic doses, it has a less pronounced effect on organs containing beta2-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 per day), it has a blocking effect on both subtypes of beta-adrenergic receptors.

Compound

Metoprolol tartrate + excipients.

Pharmacokinetics

Quickly and completely (95%) absorbed from the gastrointestinal tract. Bioavailability is 50%. During treatment, bioavailability increases to 70%. Eating increases bioavailability by 20-40%. Metoprolol is biotransformed in the liver. Metabolites do not have pharmacological activity. Metoprolol is almost completely excreted in the urine within 72 hours. About 5% of the dose is excreted unchanged.

Indications

• arterial hypertension (in monotherapy or in combination with other antihypertensive drugs), incl. hyperkinetic type;
• IHD (secondary prevention of myocardial infarction, prevention of angina attacks);
• heart rhythm disturbances (supraventricular arrhythmias, ventricular extrasystole);
• hyperthyroidism (as part of complex therapy);
• prevention of migraine attacks.

Release forms

Tablets 25 mg, 50 mg and 100 mg.

Extended-release film-coated tablets 50 mg and 100 mg (Egilok Retard).

Extended-release film-coated tablets 25 mg, 50 mg, 100 mg and 200 mg (Egilok S).

Instructions for use and dosage

For arterial hypertension, it is prescribed in daily dose 50-100 mg per day in 1 or 2 doses (morning and evening). In case of insufficient therapeutic effect it is possible to gradually increase the daily dose to 100-200 mg.

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

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

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

In elderly patients, patients with impaired renal function, and if hemodialysis is necessary, no change in dosage regimen is required.

In patients with severe liver dysfunction, the drug should be used in lower doses due to the slower metabolism of metoprolol.

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

Side effect

• increased fatigue;
• weakness;
• headache;
• slowing down the speed of mental and motor reactions;
• depression;
• anxiety;
• decreased ability to concentrate;
• drowsiness;
• insomnia;
• "nightmare" dreams;
• confusion or short-term disturbance memory;
• asthenic syndrome;
• muscle weakness;
• decreased vision;
• decreased secretion of tear fluid;
• conjunctivitis;
• noise in ears;
• sinus bradycardia;
• heartbeat;
• decrease in blood pressure;
• orthostatic hypotension;
• arrhythmias;
• increased peripheral circulatory disorders (coldness of the lower extremities, Raynaud's syndrome);
• myocardial conduction disorders;
• nausea, vomiting;
• stomach ache;
• diarrhea;
• constipation;
• dry mouth;
• change in taste;
• hives;
• skin itching;
• rash;
• exacerbation of psoriasis;
• skin hyperemia;
• increased sweating;
• reversible alopecia;
• nasal congestion;
• difficulty exhaling (bronchospasm when prescribed in high doses or in predisposed patients);
• dyspnea;
• hypoglycemia (in patients receiving insulin);
• thrombocytopenia, agranulocytosis, leukopenia;
• back or joint pain;
• slight increase in body weight;
• decreased libido and/or potency.

Contraindications

• cardiogenic shock;
• 2nd and 3rd degree AV block;
• sinoatrial block;
• SSSU;
• severe bradycardia (HR<50 уд./мин);
• heart failure in the stage of decompensation;
• angiospastic angina (Prinzmetal's angina);
• severe arterial hypotension (systolic blood pressure<100 мм рт.ст.);
• lactation period;
• simultaneous use of MAO inhibitors;
• simultaneous intravenous administration of verapamil;
• hypersensitivity to metoprolol and other ingredients of the drug.

Use during pregnancy and breastfeeding

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

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

Use in children

The drug should be prescribed with caution to children and adolescents under the age of 18 years.

special instructions

When prescribing Egilok, heart rate and blood pressure should be regularly monitored. The patient should be warned that if the heart rate<50 уд./мин необходима консультация врача.

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

Prescribing Egilok to patients with chronic heart failure is possible 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 there may be no effect from the administration of usual doses of epinephrine (adrenaline).

The use of Egilok may worsen the symptoms of peripheral circulatory disorders.

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

For exertional angina, the selected dose of the drug should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min.

Patients who use contact lenses should take into account that during treatment with beta-blockers, there may be a decrease in the production of tear fluid.

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

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

When prescribing metoprolol to patients with bronchial asthma, simultaneous use of beta2-adrenergic agonists 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 therapy being carried out with Egilok (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not required.

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

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

When using Egilok simultaneously with clonidine (Clonidine), in case of Egilok withdrawal, clonidine should be discontinued after a few days (due to the risk of withdrawal syndrome).

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

Impact on the ability to drive vehicles and operate machinery

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

Drug interactions

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

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

Inhalation anesthetics (hydrocarbon derivatives) when used simultaneously with Egilok increase the risk of inhibition of myocardial contractile function and the development of arterial hypotension.

When used simultaneously, beta-agonists, theophylline, cocaine, estrogens, indomethacin and other NSAIDs reduce the hypotensive effect of Egilok.

With the simultaneous use of Egilok and ethanol (alcohol), an increased inhibitory effect on the central nervous system is observed.

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

When used simultaneously, Egilok increases the effect of oral hypoglycemic drugs and insulin and increases the risk of developing hypoglycemia.

When Egilok is used simultaneously with antihypertensive drugs, diuretics, nitrates, and calcium channel blockers, the risk of developing arterial hypotension increases.

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

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

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

Allergens used for immunotherapy or allergen extracts for skin testing when used together with Egilok increase the risk of systemic allergic reactions or anaphylaxis.

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

When used simultaneously with Egilok, the clearance of lidocaine decreases and the concentration of lidocaine in plasma increases.

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

When used together with ethanol (alcohol), the risk of a pronounced decrease in blood pressure increases.

Analogs of the drug Egilok

Structural analogues of the active substance:

• Betalok;
• Betaloc ZOK;
• Vasocardin;
• Corvitol 100;
• Corvitol 50;
• Metozok;
• Metocard;
• Metokor Adifarm;
• Metolol;
• Metoprolol;
• Metoprolol succinate;
• Metoprolol tartrate;
• Egilok Retard;
• Egilok S;
• Emzok.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.