What is Egilok taken from? Correct dosages of the antihypertensive drug Egilok

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Egilok represents medicinal product from the group of beta1-blockers, which has antianginal, hypotensive and antiarrhythmic effects. The antianginal effect is to reduce the heart's need for oxygen and increase its endurance in conditions of coronary artery disease, which prevents angina attacks and myocardial infarction. The hypotensive effect is the ability to lower blood pressure. And the antiarrhythmic effect is to normalize the heart rhythm by stopping tachycardia and extrasystole. Thus, Egilok has a complex positive effect on the functioning of the heart, which is used in treatment of ischemic heart disease, heart failure, arrhythmias, heart attacks, hyperthyroidism, migraines and other conditions associated with high blood pressure and oxygen starvation of heart tissue.

Composition, names, varieties and release forms of Egilok

Currently, the drug Egilok is available in the following three varieties:
1. Egilok tablets with regular duration of action: 25 mg, 50 mg and 100 mg;
2. Egilok Retard tablets with prolonged action, 50 mg and 100 mg;
3. Egilok S tablets with prolonged action of 25 mg, 50 mg, 100 mg and 200 mg.

Accordingly, tablets with a normal duration of action are simply called “Egilok” in everyday speech and a number corresponding to the dosage of the active component is added, for example, “Egilok 50” or “Egilok 25”, etc. Extended-release tablets are called "Egilok Retard" and, as a rule, do not add a number indicating the dosage. Egilok S tablets in everyday speech are often called “Egilok with succinate”, since in this type of drug the active substance is contained precisely in the form of succinate, and in Egilok Retard and in Egilok with the usual duration of action in the form of tartrate. Egilok S and Egilok Retard have a prolonged effect, but simply Egilok has a regular effect.

The three listed varieties of the drug Egilok are produced by the Hungarian pharmaceutical concern EGIS Pharmaceuticals PLC. In addition to these drugs, pharmaceutical market There is another cheaper option called Egilok SR and is produced by the Indian pharmaceutical plant Intas Pharmaceuticals Ltd under license. Egilok SR is a cheaper version of Egilok S.

All three varieties of Egilok are available in the form of tablets for oral administration. Egilok tablets with a normal duration of action have a round, biconvex shape and are white or almost white in color. The 25 mg tablets have a cross-shaped line on one side and “E 435” on the other. Tablets of 50 mg and 100 mg are scored on one side and engraved “E 434” and “E 432” on the other, respectively.

Egilok Retard tablets of all dosages are coated white, have an oblong biconvex shape and a mark on both sides. Egilok C tablets of all dosages are white in color, have an oval, biconvex shape and are scored on both sides.

Egilok and Egilok Retard contain as active substance metoprolol tartrate, and Egilok S – metoprolol succinate. Both substances are different salts of metoprolol, which is actually the active component of the drug. In the body, salt breaks down and metoprolol is released from it, which has a direct effect therapeutic effect. Therefore, all varieties of Egilok can be considered exactly the same, because metoprolol tartrate and succinate differ slightly only in the rate of absorption into the blood and the development of the therapeutic effect.
Auxiliary components of three varieties of Egilok are shown in the table.

Egilok	Egilok Retard	Egilok S
	Colloidal silicon dioxide	Microcrystalline cellulose
Sodium carboxymethyl starch (type A)	Magnesium stearate	Methylcellulose
Colloidal silicon dioxide	Macrogol 6000	Glycerol
Povidone	Sucrose	Corn starch
Magnesium stearate	Starch syrup	Ethylcellulose
	Triethyl citrate	Magnesium stearate
	Hyprolose	Hypromellose
	Ethylcellulose	Stearic acid
	Talc	Titanium dioxide
	Titanium dioxide

Egilok - recipe

The prescription for Egilok is written as follows:
Rp.: Egilok 25 mg N 40
D.S. 1 tablet 3 times a day.

After the letters "Rp." The full name of the drug and the dosage of the active substance are indicated (in in this example Egilok 25 mg). Then they write the letter “N” and indicate after it a number indicating the number of tablets that need to be sold to a person at the pharmacy. On the second line of the recipe after the letters "D. S." The tablet dosage regimen is indicated.

Therapeutic effect of the drug

All varieties of the drug Egilok have antiarrhythmic, hypotensive and antianginal effects due to the ability of the active substance to block beta1-adrenergic receptors of the heart.

By blocking adrenergic receptors, Egilok reduces the heart rate, the force of contractile movement of the myocardium and the volume of blood ejected into the aorta, and also moderately reduces blood pressure. Egilok reduces blood pressure in people standing and lying down. Long-term use of Egilok for hypertension has a beneficial effect on the heart, reducing its load and thereby reducing the risk of sudden cardiac death, heart attack and stroke.

In addition, Egilok reduces the heart's need for oxygen by reducing blood pressure, heart rate and strength of myocardial contractile movements. Reducing the heart rate and lengthening the period of cardiac relaxation (diastole) improves blood supply to the myocardium itself and the absorption of oxygen by its cells. That is why Egilok ensures improved nutrition and oxygen supply to the heart, which prevents angina attacks and increases human performance.

Regular use of Egilok can reduce the risk of sudden cardiac death during the development of myocardial infarction. Using the drug after a heart attack prevents recurrent attacks.

When Egilok is used in complex therapy of coronary artery disease, the drug normalizes heart rhythm, preventing the appearance of extrasystoles and tachycardia. This effect creates a stable heart rhythm, which, even during attacks, is not disturbed with the development of deadly ventricular fibrillation. That is why regular use of Egilok reduces the risk fatal outcome for heart failure and ischemic heart disease.

Thus, we can say that Egilok is a drug for attacks of angina and heart failure, since it improves the functioning of the heart and increases its stability and endurance, which allows a person to calmly endure physical and emotional stress. Egilok does not treat angina pectoris, ischemic heart disease and heart failure, it only ensures the normal functioning of the heart in adverse conditions, relieving and stopping the painful symptoms of diseases and allowing a person to lead familiar image life. That is, Egilok is a drug to eliminate symptoms cardiovascular diseases and prevention of angina attacks, hypertensive crises, heart attacks and strokes.

Egilok - indications for use

In principle, all varieties of Egilok are indicated for use for the same diseases. However, due to the characteristics and duration of the therapeutic effects, varieties of the drug Egilok are indicated for use in various variants of the same diseases. For ease of perception and to avoid confusion, indications for the use of three varieties of Egilok are given in the table.

Indications for use of Egilok	Indications for use of Egilok Retard	Indications for use of Egilok S
Preventing migraine attacks
Arterial hypertension (Egilok can be used as a single drug or as part of complex therapy)
Prevention of angina attacks
Prevention of recurrent myocardial infarction (Egilok is used as part of complex therapy)
	Hyperthyroidism (Egilok is used as part of complex therapy)	Elimination of ventricular extrasystoles
	Hyperkinetic cardiac syndrome
Prevention of ventricular extrasystoles	Prevention of supraventricular and ventricular tachycardias	Reducing the frequency of ventricular contractions in atrial fibrillation
Prevention of supraventricular arrhythmias	Chronic heart failure (Egilok is used in combination with diuretics, cardiac glycosides and ACE inhibitors)	Stable chronic heart failure of any functional class, combined with impaired left ventricular systole (Egilok is used as part of complex therapy)
		Reducing the risk of death in late phases of myocardial infarction
		Functional cardiac disorders associated with tachycardia

Egilok - instructions for use

General admission rules

Tablets of any type of Egilok should be swallowed whole, without chewing or crushing in any other way, but with a small amount of still water. If necessary, tablets can only be broken in half according to the existing risks. The tablets can be taken regardless of food, since food does not affect the absorption of the drug into the bloodstream. However, it is recommended to take the drug during or immediately after a meal, as this reduces the risk and severity of side effects from the gastrointestinal tract.

The dosage of Egilok, Egilok Retard and Egilok S is selected individually, gradually increasing it to required value. This gradual increase in dosage to the therapeutic dose is necessary in order to avoid bradycardia at the beginning of treatment. The maximum permissible daily dosage is 200 mg. When selecting a dosage for angina pectoris, it is necessary to focus on the pulse, which should be 55–60 beats per minute at rest, and no more than 110 during exercise.

There is no need to change the dosage in older people or those suffering from renal or liver failure. A reduction in the recommended dosage is required only in cases of severe liver failure. In addition, it is necessary to reduce the dosage of Egilok if bradycardia develops with a pulse less than 50 beats per minute, a severe decrease in pressure, AV blockade, bronchospasm, ventricular arrhythmia or severe liver dysfunction.

Egilok is discontinued slowly, reducing the dosage over 10 to 14 days to the minimum (25 mg for Egilok and Egilok Retard and 12.5 mg for Egilok S). The minimum dosage must be taken for 4 to 5 days, after which the drug should be completely discontinued. If you abruptly stop taking the drug, withdrawal syndrome develops, which is manifested by increased angina and increased blood pressure.

Treatment with Egilok of various diseases

For hypertension, start taking Egilok 20–50 mg 2 times a day (morning and evening). If given dosage is not effective enough, then it is increased to 50–100 mg 2 times a day.

For angina pectoris and arrhythmias, start taking Egilok 25–50 mg 2–3 times a day, if necessary increasing the dosage to 100 mg 2 times a day.

Prevention of a recurrent heart attack is to take Egilok 50–100 mg twice a day.

To relieve tachycardia in hyperthyroidism, it is recommended to take Egilok 50 mg 3 to 4 times a day.

For functional disorders accompanied by tachycardia (for example, vegetative-vascular dystonia, panic attack, etc.), Egilok is taken 50 mg 2 times a day. If ineffective, the dosage is increased to 100 mg 2 times a day.

Egilok can provoke increased allergic reactions, so people prone to allergies should take this aspect into account. Egilok also reduces the production of tears, which is important for people who use contact lenses. To prevent dry eyes, they will have to use artificial tears or give up contact lenses in favor of glasses.

In the presence of heart failure, Egilok can be taken only after the compensation stage has been reached. With a gradual increase in the dosage of Egilok for heart failure, an increase in symptoms may initially be observed, which gradually decreases over two weeks. Because of this feature, you cannot increase the dosage of Egilok sharply.

Peripheral circulation may deteriorate while using Egilok.

Egilok should be used simultaneously with beta-2 adrenergic agonists in people suffering from bronchial asthma, or with alpha-blockers for pheochromocytoma. In addition, while taking Egilok, drugs from the group of blockers cannot be administered intravenously calcium channels, for example, Verapamil et al.

There is no need to stop Egilok for any surgical operations, but you should tell the anesthesiologist that the person is taking this drug. In some cases, in the absence of the necessary range of drugs for anesthesia, it may be necessary to discontinue Egilok 48 hours before surgery.

Egilok should be discontinued if a person develops depression.

Egilok Retard should not be used by people suffering from fructose or galactose intolerance, as well as sucrose or isomaltase deficiency, since the tablets contain sucrose.

Egilok during pregnancy and breastfeeding

Any type of Egilok during pregnancy and breastfeeding can only be used if the potential benefit to the mother outweighs all possible risks to the fetus.

When using the drug during pregnancy, it should be discontinued 2-3 days before birth, since otherwise the newborn may experience growth retardation, bradycardia, low blood pressure, respiratory depression and hypoglycemia after birth. If Egilok was not canceled on time, then after birth the child’s condition should be monitored for 48 to 72 hours.

Despite the fact that Egilok passes into breast milk in small quantities, it has adrenergic blocking effects on the baby's heart function. Therefore, if it is necessary to take Egilok, you should stop breastfeeding and transfer the child to artificial formula.

Compatibility with other drugs

When using Egilok together with drugs that are inhibitors of the CYP2D6 enzyme (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine), fluctuations in its concentration in the blood serum may occur.

Egilok should not be used in combination with the following medications:

Barbiturates (Phenobarbital, Phenazepam, etc.);
Propafenone;
Verapamil.

The dosage of Egilok should be adjusted when joint use with the following drugs:

Adrenaline (epinephrine);
Amiodarone;
Class I antiarrhythmic drugs;
Beta blockers (such as atenolol, propranolol and pindolol);
Hydrazaline;
Guanfacine;
Diphenhydramine;
Diltiazem;
Clonidine;
Methyldopa;
Nonsteroidal anti-inflammatory drugs (for example, Aspirin, Paracetamol, Ibuprofen, Nimesulide, Indomethacin, Diclofenac, etc.);
Norephedrine (phenylpropanolamine);
Reserpine;
Theophylline;
Quinidine;
Cimetidine;
Estrogen hormones (including combined oral contraceptives);
Ergotamine.

Cardiac glycosides (Strofanthin, etc.) when used simultaneously with Egilok can provoke bradycardia. Drugs acting on the central nervous system (hypnotics, tranquilizers, antidepressants, antipsychotics and ethanol), when used simultaneously with Egilok, increase the risk sharp decline blood pressure.

Egilok prolongs effects indirect anticoagulants(for example, Warfarin, Dicumarin, etc.).

The risk of allergic reactions increases significantly when special solutions for skin allergy tests and iodine-containing radiocontrast substances are used simultaneously with Egilok.

In smokers, the effects of Egilok may be much less pronounced.

Impact on the ability to operate machinery

While taking Egilok, you can exercise various types activities requiring excellent concentration and high speed of reactions only with caution, since the drug reduces the ability to control mechanisms due to the possible development of dizziness and increased fatigue.

Overdose

An overdose of any type of Egilok is possible and manifests itself the following symptoms:

Severe decrease in blood pressure;
Severe bradycardia with a heart rate less than 50 beats per minute;
Dizziness;
Cyanosis (blue discoloration of lips, nails, fingertips);
Arrhythmia;
Extrasystole;
Bronchial spasm;
Cardiogenic shock;
AV block (up to complete cardiac arrest);
Pain in the heart (cardialgia);
Respiratory depression;
Fatigue;
Increased sweating;
Impaired sensitivity (feeling of goosebumps, etc.);
Mi asthenic syndrome.

The first symptoms of an Egilok overdose develop 20 to 120 minutes after taking the drug. Overdose symptoms often develop when taking alcohol, quinidine, barbiturates, or blood pressure lowering drugs.

Treatment of overdose with Egilok is carried out in intensive care, since it is necessary to carry out measures intensive care and constant monitoring of the person’s condition. If the tablets were taken within the next 40 minutes, then the stomach is washed and the person is given a sorbent (for example, activated carbon, Polysorb, Polyphepan, etc.). Subsequently, symptomatic therapy is carried out aimed at normalizing the main indicators of the cardiovascular system and maintaining the functioning of vital organs.

Egilok - side effects

All three varieties of Egilok can provoke the development of almost identical side effects from any organs and systems. The list below shows the side effects of all three types of Egilok. Moreover, if any side effect is characteristic only of one type of Egilok, then this is indicated in parentheses.
So, the side effects of Egilok are as follows:

1. From the nervous system:

Fatigue;
Dizziness;
Headache;
Excitability;
Convulsions;
Paresthesia (pins and needles sensation and other sensory disturbances);
Depression;
Deterioration in concentration;
Nightmares;
Depression;

2. From the cardiovascular system:

Bradycardia;
Orthostatic hypotension ( sharp drop pressure when moving to a standing position);
Fainting;
Cold feet;
Heartbeat;
Temporary increase in symptoms of heart failure;
Cardiogenic shock in people who have had myocardial infarction;
AV block of the first degree;
Arrhythmia;
Pain in the heart area;
Swelling in the extremities (for Egilok Retard and Egilok S).

3. From the gastrointestinal tract:

Nausea;
Vomit;
Dry mouth;
Impaired liver function (darkness of urine, yellowness of the sclera or skin, stagnation of bile);
Hepatitis (for Egilok S);
Increased activity of AST and ALT;
Increased concentration of bilirubin in the blood.

4. From the skin:

Increased sweating;
Alopecia (baldness);
Photosensitivity (sensitivity to sunlight);
Exacerbation of psoriasis;
Skin itching;
Redness of the skin;
Exanthema.

5. From the respiratory system:

Shortness of breath when physical stress;
Bronchospasm;

6. From the senses:

Visual impairment;
Dryness and irritation of the surface of the eye;
Taste disturbance.

7. Others:

Weight gain;
Joint pain (arthralgia);
Thrombocytopenia of platelets in the blood);
Leukopenia (decrease in the total number of white blood cells);
Agranulocytosis (decrease in the content of neutrophils, eosinophils and basophils in the blood);
Reducing the level of high-density lipoprotein (HDL) in the blood;
Increased levels of triglycerides (TG) in the blood.

Side effects of Egilok are usually mild and temporary. If any side effect begins to occur intensely, requiring special treatment, then you should stop taking Egilok.

Contraindications for use

Varieties of Egilok have relative and absolute contraindications. If present, the drug must not be used under any circumstances. And in case of relative contraindications, careful use of Egilok under the supervision of a physician is allowed.

TO absolute contraindications The following conditions apply to the use of Egilok:

Hypersensitivity, intolerance or allergic reactions to drug components;
Atrioventricular (AV) block II or III degree;
Sinoatrial block;
Bradycardia with a heart rate less than 50 beats per minute;
Sick sinus syndrome;
Cardiogenic shock;
Severe peripheral circulatory disorders (for example, trophic ulcers, marbling of the skin of the extremities, etc.);
Heart failure in the stage of decompensation;
Age under 18 years;
Severe bronchial asthma;
Simultaneous intravenous administration Verapamil;
Acute myocardial infarction with pulse less than 45 beats per minute, PQ interval more than 240 ms and top pressure below 100 mm Hg. Art.;
Concomitant use of drugs that inhibit the enzyme CYP2D6;
Pregnancy and breastfeeding period;
Long-term use inotropic drugs and beta-blockers or mimetics (for Egilok S);
Prinzmetal's angina (for Egilok);
Intolerance to fructose, galactose or deficiency of sucrose or isomaltase (for Egilok Retard).

Relative contraindications to the use of Egilok are the following conditions:

Diabetes;

The following drugs are synonyms for Egilok:

Betaloc solution and tablets;
Betaloc Zok extended-release tablets;
Vasocardin and Vasocardin Retard tablets;
Corvitol 50 and 100;
Lidalok tablets;
Metozok tablets;
Metocard tablets;
Metokor Adifarm tablets and solution;
Metoprolol tablets;
Serdol tablets.

The following drugs are analogues of Egilok:

Aritel and Aritel Cor tablets;
Atenolol tablets;
Betak tablets;
Betacard tablets;
Betaxolol tablets;
Bidop tablets;
Binelol tablets;
Biol tablets;
Biprol tablets;
Bisogamma tablets;
Bisocard tablets;
Bisomore tablets and lyophilisate;
Bisoprolol tablets;
Breviblok solution;
Vero-Atenolol tablets;
Concor and Concor Cor tablets;
Corbis tablets;
Cordanum tablets;
Cordinorm tablets;
Coronal tablets;
Lokren tablets;
Nebivator tablets;
Nebivolol tablets;
Nebicor tablets;
Nebilan Lannacher tablets;
Nebilet tablets;
Nebilong tablets;
Nevotenz tablets;
Niperten tablets;
OD-Nab tablets;
Tirez tablets;
Estekor tablets.

Egilok - reviews

heart rate

high efficiency

general state

Also in the reviews people note good efficiency Egilok at course application to lower blood pressure. The advantages of the drug according to people are fast development effect, good tolerability and the possibility of long-term use for several years in a row.

In reviews of the use of Egilok for arrhythmia, people note that the drug very quickly and literally perfectly equalizes the rhythm, relieving painful symptoms and returning normal well-being.

Negative reviews about Egilok are associated with the development of side effects and the need to stop taking the drug. That is, negative reviews usually left by people for whom Egilok was not suitable for some reason.

Concor or Egilok?

In principle, the therapeutic effect of Concor and Egilok is practically no different, but one drug is better for some people, and the second for another person. There is only one way to find out which drug is best for you - try taking both. If desired, you can easily replace one drug with another, knowing that 5 mg of Concor corresponds to 50 mg of Egilok. However, Egilok has a little more strong action compared to Concor, therefore it is recommended to choose the first drug if the second is ineffective.

In general, the only significant difference between Concor and Egilok is the possibility of its use in cases of severe bradycardia (pulse less than 55 beats per minute). Therefore, if you have a tendency to bradycardia, Egilok is preferable.

Egilok, Egilok Retard and Egilok S – price

former USSR

Prices for all varieties of Egilok are shown in the table.

Before use, you should consult a specialist.

Photo of the drug

Latin name: Egilok

ATX code: C07AB02

Active substance: Metoprolol

Manufacturer: EGIS Pharmaceuticals PLC (Hungary)

Description is valid on: 10.11.17

Egilok – medicine, which is developed for the treatment of diseases of the cardiovascular system. The use of Egilok helps reduce the ventricular heart rate in cases of supraventricular tachycardia, ventricular extrasystole and atrial fibrillation.

Active substance

Metoprolol.

Release form and composition

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

Indications for use

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

Contraindications

heart failure in the decompensation phase;
SSSU;
sinoatrial block;
cardiogenic shock;
expressed 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.

Prescribed with extreme caution 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 of Egilok (method and dosage)

The tablets are taken orally, regardless of food intake. For ease of swallowing, the tablet can be broken in half.

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

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

For 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, 100-200 mg is prescribed for maintenance therapy. Which are divided into two equal steps.
In case of heart rhythm disturbances, 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.
For functional heart disorders, 50 mg is prescribed twice a day; if necessary, the dose can be increased to 200 mg.
To prevent migraines, you need to take 100 mg in two doses, with the possibility of increasing to 200 mg.

Side effects

The use of tablets may cause the following side effects:

from the cardiovascular system: palpitations, sinus bradycardia, orthostatic hypotension, decreased myocardial contractility, impaired myocardial conduction, cardialgia, arrhythmia, temporary worsening of the symptoms of chronic heart failure;
from the nervous system: weakness, increased 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, change in taste, hyperbilirubinemia;
from the hematopoietic system: leukopenia, agranulocytosis, thrombocytopenia;
from the outside respiratory system: difficulty exhaling, nasal congestion, shortness of breath;
dermatological reactions: skin itching, urticaria, rash, exacerbation of psoriasis, increased sweating, photodermatosis, exanthema, skin hyperemia, reversible alopecia;
other: decreased libido and potency, weight gain, back pain, hypoglycemia, decreased vision, tinnitus, conjunctivitis.

Overdose

An overdose of the drug is manifested by the following symptoms: sinus bradycardia, heart failure, decreased 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 conditions. Gastric lavage, Activated Carbon intake are recommended, and symptomatic therapy is also used. Additionally, the administration of norepinephrine or dobutamine is recommended; for convulsions - diazepam; for bronchospasm, beta2-adrenergic agonists are prescribed.

Analogs

Analogs by ATC code: Betalok, Vasocardin, Metroprolol, Serdok, Emzok.

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

Do not decide to change the drug on your own; consult your doctor.

pharmachologic effect

Egilok is an effective drug that belongs to beta1-blockers. Main active component The medication is metoprolol. This substance has hypotensive, antiarrhythmic and antianginal effects. By blocking beta1-adrenoceptors, metoprolol reduces the excitatory effect of the sympathetic nervous system on the heart, and also immediately reduces blood pressure and heart rate. As for the hypotensive effect of the drug, it is quite long-lasting, since peripheral vascular resistance decreases gradually.

Long-term use in high blood pressure may lead to a decrease in left ventricular mass. The drug reduces mortality from cardiovascular diseases in males with a moderate increase in blood pressure.
Due to a decrease in heart rate and blood pressure, it reduces the need of the heart muscle for oxygen, due to which diastole lengthens. This effect reduces the frequency of angina attacks and significantly improves the patient’s quality of life and physical condition.
Indications for Egilok are atrial fibrillation, supraventricular tachycardia and ventricular extrasystole. In these pathologies, the medicine helps reduce the ventricular heart rate. Regular use of the medicine 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 your heart rate drops below 50 beats per minute, medical attention is required.
Patients with diabetes should regularly monitor their glucose levels and adjust their insulin dosage if necessary.
Should be discontinued gradually, reducing the dosage over two weeks to avoid withdrawal symptoms, coronary disorders and angina.
Patients who wear contact lenses may experience decreased tear secretion.
Caution is recommended when operating vehicles and during classes potentially dangerous species 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 liver dysfunction

It is prescribed with extreme caution for liver failure.

Drug interactions

The drug cannot be combined with MAO inhibitors and Verapamil, since the toxicity of Egilok may increase.
The effect of the drug is enhanced when taken in combination with other antihypertensive drugs. In order to prevent arterial hypotension, blood pressure and the general condition of the patient should be constantly monitored.
When used in combination with antiarrhythmic drugs and cardiac glycosides, the risk of developing AV block and bradycardia increases.

There are contraindications. Before starting use, consult your doctor.

Commercial names abroad (abroad) - Apo-Metoprolol, Azumetop, Beloc-Zok, Beloken, Betazok, Bloxan, Denex, Doplin, Emzok, Jeprolol, Lanoc, Lopressor, Mepronet, Metapro, Metblock, Metodura, Metohexal, Metolar, Metolol , Metomerck, Metopress, Metoros, Metostad, Metrol, Met-XL, Meto Zerok, Minax, Neobloc, Presolol, Prolaken, Prolomet-XL, Restopress, Ritmetol, Seloken, Selopral, Selozok, Sitelol, Spesicor, Starpress, Supermet, Toprol- XL, Vivalol, Zoticus.

All drugs used in cardiology.

You can ask a question or leave a review about the medicine (please, do not forget to indicate the name of the drug in the text of the message).

Preparations containing Metoprolol (Metoprolol, ATC code C07AB02):

Common forms of release (more than 100 offers in Moscow pharmacies)
Name	Release form	Packaging, pcs.	Manufacturer country	Price in Moscow, r	Offers in Moscow
Betaloc - original	tablets 100mg	100	Sweden, Astra Zeneca	380- (average 494↗) -565	285↗
	tablets 25mg	14	Sweden, Astra Zeneca	105- (average 142) -312	902↗
Betaloc ZOK - original (slow release)	tablets 50mg	30	Sweden, Astra Zeneca	235- (average 286↗) -343	899↗
Betaloc ZOK - original (slow release)	tablets 100mg	30	Sweden, Astra Zeneca	329- (average 416↗) -491	855↗
Vasocardin	tablets 50mg	50	Slovakia, Zentiva	53- (average 69) -124	433↘
Vasocardin	tablets 100mg	50	Slovakia, Zentiva	93- (average 123↗) -152	678↗
Corvitol 50 (Corvitol 50)	tablets 50mg	50	Germany, Berlin-Chemie	82- (average 205↘) -273	450↘
Corvitol 100 (Corvitol 100)	tablets 100mg	50	Germany, Berlin-Chemie	112- (average 254↘) -343	414↘
Metozoc	tablets 25mg	30	Russia, Akrikhin	94- (average 175↗) -203	112↘
Metozoc	tablets 50mg	30	Russia, Akrikhin	173- (average 229↗) -261	139↘
Metocard	tablets 50mg	30	Poland, Polpharma	42- (average 57) -75	400↗
Metocard	tablets 100mg	30	Poland, Polpharma	24- (average 73) -96	365↘
Metoprolol Acri	tablets 50mg	30	Russia, Akrikhin	15- (average 45) -52	110↗
Metoprolol Ratiopharm	tablets 50mg	30, 50, 100	Germany, Ratiopharm	23- (average 28) -32	241↗
Metoprolol Ratiopharm	tablets 100mg	30	Germany, Merkle	26- (average 50) -76	404↗
Egilok	tablets 25mg	60	Hungary, Egis	100- (average 122) -142	950↗
Egilok	tablets 50mg	60	Hungary, Egis	98- (average 146↗) -170	959↗
Egilok	tablets 100mg	30 and 60	Hungary, Egis	for 30pcs: 96- (average 134↗) -365 for 60pcs: 131- (average 200↗) - 227	944↘
	tablets 50mg	30	Switzerland, Atsino Pharma	119- (average 211↗) -327	700↘
Egilok Retard (slow release)	tablets 100mg	30	Switzerland, Atsino Pharma	110- (average 285) -330	600↘
Egilok C	tablets 100mg	30	India, Intas	148- (average 288) -361	155↘
Rarely encountered and discontinued release forms (less than 100 offerings in Moscow pharmacies)
Name	Release form	Packaging, pcs.	Country, company	Price in Moscow, r	Offers in Moscow
Betaloc - original	solution for intravenous injections 5 mg in 5 ml, ampoules	5	Sweden, Astra Zeneca	715- (average 854↗) -976	74↗
Metoprolol	tablets 50mg	28, 30 and 40	Different	12- (average 67) -86	71↘
Egilok C	tablets 50mg	30	India, Intas	105- (average 198↘) -262	71↘
Vasocardin Retard (slow release)	tablets 200mg	30	Slovakia, Zentiva	No	No
Methohexal	tablets 100mg	20	Germany, Hexal	No	No
Metozoc	tablets 100mg	30	Russia, Akrikhin	255- (average 326) -419	48↘
Metocard Retard	tablets 200mg	30	Poland, Polpharma	No	No
Metokor Adifarm	solution for intravenous injection 1 mg/ml 5 ml	10	Bulgaria, Adifarm	729-730	4↗
Metolol	tablets 50mg	30	Austria, Merkle	No	No
Metolol	tablets 100mg	10	Austria, Merkle	No	No
Metoprolol	tablets 25mg	60	Russia, Ozone	43- (average 59) -86	15↗
Metoprolol	tablets 100mg	30 and 50	Serbia, Hemofarm	26- (average 74) -111	83↗
Metoprolol Organics	tablets 25mg	60	Russia, Organika JSC	43- (average 56) -68	18↗
Metoprolol Organics	tablets 50mg	30 and 60	Russia, Organika JSC	18-86	9↗
Egilok C	tablets 25mg	30	India, Intas	112- (average 167) -299	73↗
Egilok C	tablets 200mg	30	India, Intas	238- (average 281) -317	32↗
Serdol	tablets 50mg	30	Romania, Labormed	No	No

Betaloc ZOK (original Metoprolol sustained release) - official instructions for use. The drug is a prescription, the information is intended only for healthcare professionals!

Clinical and pharmacological group:

Beta1 blocker

pharmachologic effect

Cardioselective beta1-blocker without intrinsic sympathomimetic activity. Has a slight membrane stabilizing effect. It has antihypertensive, antianginal and antiarrhythmic effects. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress: it prevents an increase in heart rate, an increase in blood pressure, reduces cardiac output and reduces myocardial contractility.

Due to the peculiarities of the dosage form, a constant concentration of metoprolol in plasma is maintained and a stable clinical effect of the drug is ensured for 24 hours. Due to the absence of concentration peaks in plasma, Betaloc® ZOK is clinically characterized by better beta1-selectivity compared to traditionally used tablet forms of metoprolol. Besides, in to a large extent the potential risk of side effects observed at peak plasma concentrations of the drug (for example, bradycardia or weakness in the legs when walking) is reduced.

When used in average therapeutic doses, Betaloc® ZOK has a less pronounced effect on bronchial smooth muscle than non-selective beta-blockers. If necessary, Betaloc® ZOK in combination with beta2-agonists can be prescribed to patients with obstructive pulmonary disease.

Betaloc® ZOK has a lesser effect on insulin secretion and carbohydrate metabolism and on the activity of the cardiovascular system in conditions of hypoglycemia compared with non-selective beta-blockers.

The use of the drug Betalok® ZOK for arterial hypertension leads to a significant decrease in blood pressure for more than 24 hours (in the supine position, standing, during exercise). At the beginning of metoprolol therapy, an increase in peripheral vascular resistance is observed. At long-term use a decrease in blood pressure is possible due to a decrease in peripheral vascular resistance with unchanged cardiac output.

In MERIT-HF, a survival study in chronic heart failure (II-IV functional class according to the NYHA classification) with reduced ejection fraction (? 40%), which included 3991 patients, Betaloc® ZOK showed an increase in survival and a decrease in the frequency of hospitalization. At long-term treatment Patients achieved a general improvement in well-being and a decrease in the severity of symptoms (according to NYHA functional classes). Also, therapy with the drug Betaloc® ZOK showed an increase in left ventricular ejection fraction, a decrease in end-systolic and end-diastolic volumes of the left ventricle.

The quality of life does not deteriorate or improves during treatment with Betaloc® ZOK. An improvement in the quality of life during treatment with Betaloc® ZOK was observed in patients after myocardial infarction.

Pharmacokinetics

Suction and distribution

After oral administration, metoprolol is completely absorbed from the gastrointestinal tract.

The rate of release of the active substance depends on the acidity of the medium. After taking the Betaloc® ZOK tablet (a dosage form with sustained release of metoprolol), the duration of the therapeutic effect is more than 24 hours, and a constant rate of release of the active substance is achieved within 20 hours.

Bioavailability after a single dose is approximately 30-40%. The binding of metoprolol to plasma proteins is low - approximately 5-10%.

Metabolism

Metoprolol is biotransformed in the liver by oxidation. The three main metabolites of metoprolol did not exhibit a clinically significant beta-blocking effect.

Removal

T1/2 averages 3.5 hours. About 5% of the oral dose of the drug is excreted unchanged in the urine, the rest of the drug is excreted in the form of metabolites.

Indications for use of the drug BETALOK® ZOK

arterial hypertension;
angina pectoris;
stable symptomatic chronic heart failure with impaired systolic function left ventricle (as an adjuvant therapy to the main treatment of heart failure);
maintenance treatment after the acute phase of myocardial infarction (to reduce mortality and recurrent infarction);
heart rhythm disturbances (including supraventricular tachycardia), as well as to reduce the frequency of ventricular contractions during atrial fibrillation and ventricular extrasystoles;
functional disorders of cardiac activity accompanied by tachycardia;
prevention of migraine attacks.

Dosage regimen

When selecting a dose, it is necessary to avoid the development of bradycardia.

For arterial hypertension, the initial dose is 50-100 mg 1 time per day. In the absence of clinical effect, you can increase the dose to 100 mg 1 time per day or use Betaloc® ZOK in combination with other antihypertensive drugs (preferably a diuretic and a calcium channel blocker dihydropyridine derivative).

For angina pectoris, the average therapeutic dose is 100-200 mg once a day. If necessary, Betaloc® ZOK can be used in combination with other antianginal drugs.

In case of stable symptomatic chronic heart failure with impaired left ventricular systolic function, Betaloc® ZOK can be prescribed to patients who have not had episodes of exacerbation over the past 6 weeks and there have been no changes in the main therapy over the past 2 weeks. Treatment of heart failure with beta-blockers can sometimes lead to a temporary worsening of the symptomatic picture. In some cases, it is possible to continue therapy or reduce the dose, and in some cases it may be necessary to discontinue the drug.

For stable chronic heart failure of functional class II, the recommended initial dose for the first 2 weeks is 25 mg 1 time per day. After 2 weeks, the dose can be increased to 50 mg 1 time per day and then can be doubled every 2 weeks. The maintenance dose for long-term treatment is 200 mg once a day.

For stable chronic heart failure of functional classes III and IV, the recommended initial dose for the first 2 weeks is 12.5 mg 1 time per day. The dose is selected individually. During the period of increasing the dose, the patient should be monitored, because In some patients, heart failure symptoms may worsen. After 1-2 weeks, the dose can be increased to 25 mg 1 time per day, then after another 2 weeks - up to 50 mg 1 time per day. If well tolerated, the dose can be doubled every 2 weeks until maximum dose 200 mg 1 time per day.

In case of arterial hypotension and/or bradycardia, it may be necessary to reduce concomitant therapy or reduce the dose of Betaloc ZOK. Hypotension at the start of therapy does not necessarily indicate that given dose Betaloc ZOK will not be tolerated during further long-term treatment. However, doses should not be increased until the condition has stabilized. Monitoring of renal function may also be necessary.

For maintenance treatment after myocardial infarction, the drug is prescribed at a dose of 200 mg once a day.

For cardiac arrhythmias, the drug is prescribed 100-200 mg once a day.

For functional cardiac disorders accompanied by tachycardia, the dose is 100 mg once a day; if necessary, the dose can be increased to 200 mg per day.

To prevent migraine, 100-200 mg is prescribed once a day.

Betalok® ZOK is intended for daily intake 1 time per day (preferably in the morning). Betaloc ZOK tablet should be swallowed with liquid. The tablets can be divided in half, but should not be chewed or crushed.

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

Side effect

To assess the frequency of cases, the following criteria were used: very often (> 10%), often (1-9.9%), sometimes (0.1-0.9%), rarely (0.01-0.09%), very rarely (< 0.01%).

From the cardiovascular system: often - bradycardia, orthostatic arterial hypotension (very rarely accompanied by fainting), coldness of the extremities, palpitations; sometimes - temporary increase in symptoms of heart failure, AV blockade of the first degree, cardiogenic shock in patients with acute myocardial infarction; rarely - other conduction disorders, arrhythmias; very rarely - gangrene (in patients with severe peripheral circulatory disorders).

From the central nervous system and peripheral nervous system: very often - fatigue; often - dizziness, headache; sometimes - paresthesia, muscle cramps, depression, decreased ability to concentrate, drowsiness or insomnia, nightmares; rarely - nervousness, anxiety; very rarely - memory impairment, amnesia, depression, hallucinations.

From the digestive system: often - nausea, abdominal pain, diarrhea, constipation; sometimes - vomiting; rarely - dry mouth, liver dysfunction; very rarely - hepatitis.

From the hematopoietic system: very rarely - thrombocytopenia.

From the respiratory system: often - shortness of breath on exertion; sometimes - bronchospasm; rarely - rhinitis.

From the musculoskeletal system: very rarely - arthralgia.

From the senses: rarely - dryness and/or irritation of the eyes, conjunctivitis, blurred vision; very rarely - ringing in the ears, taste disturbances.

Dermatological reactions: sometimes - rash (in the form of urticaria), increased sweating; rarely - hair loss; very rarely - photosensitivity, exacerbation of psoriasis.

Other: sometimes - weight gain; rarely - impotence, sexual dysfunction.

Betaloc® ZOK is well tolerated by patients; side effects are mostly mild and reversible.

Contraindications to the use of BETALOK® ZOK

AV block II and III degrees;
chronic heart failure in the decompensation stage (pulmonary edema, hypoperfusion syndrome or hypotension);
long-term or intermittent therapy with inotropic agents aimed at stimulating β-adrenergic receptors;
clinically significant sinus bradycardia;
SSSU;
cardiogenic shock;
arterial hypotension;
severe peripheral disturbances arterial circulation(including with the threat of gangrene);
patients with suspected acute myocardial infarction with heart rate less than 45 beats/min, PQ interval more than 0.24 s or systolic blood pressure less than 100 mm Hg;
patients prescribed IV administration of slow calcium channel blockers (like verapamil);
children's and adolescence up to 18 years of age (the effectiveness and safety of the drug have not been established);
hypersensitivity to the components of the drug;
hypersensitivity to other beta-blockers.

Use the drug with caution in case of 1st degree AV block, Prinzmetal's angina, bronchial asthma, COPD, diabetes mellitus, severe renal failure, metabolic acidosis, co-administration with cardiac glycosides.

Use of BETALOK® ZOK during pregnancy and breastfeeding

Like most drugs, Betaloc® ZOK should not be prescribed during pregnancy and breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and/or child.

Like other antihypertensive agents, beta blockers may cause side effects such as bradycardia in the fetus, neonates, or breast-fed children. The amount of metoprolol released into breast milk, and the beta-blocking effect in a breastfed child (when the mother takes metoprolol in therapeutic doses) are insignificant.

Use for liver dysfunction

When prescribing the drug to patients with severe liver dysfunction (for example, in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.

Use for renal impairment

Caution should be exercised when prescribing the drug to patients with severe renal failure.

special instructions

Beta-blockers are not recommended for patients with obstructive pulmonary disease. At poor tolerance or the ineffectiveness of other antihypertensive drugs, metoprolol can be prescribed, since it is a selective drug. The minimum effective dose should be prescribed; if necessary, a beta2-agonist may be prescribed.

When using beta1-blockers, the risk of affecting carbohydrate metabolism or the possibility of masking symptoms of hypoglycemia is significantly less than when using non-selective beta-blockers.

In patients with chronic heart failure in the stage of decompensation, before prescribing Betaloc® ZOK, it is necessary to achieve compensation and maintain it during treatment with the drug.

Very rarely, during therapy with Betalok ZOK, patients with conduction disorders may experience a deterioration in their condition up to AV blockade. If bradycardia develops during treatment, the dose of the drug should be reduced or the drug should be gradually discontinued.

During the period of use of the drug, symptoms of peripheral arterial circulation disorders may increase, mainly due to a decrease in blood pressure.

If it is necessary to prescribe Betaloc ZOK to patients with pheochromocytoma, alpha-blockers should be prescribed simultaneously.

Caution should be exercised when prescribing the drug to patients with severe renal failure, metabolic acidosis, and co-administration with cardiac glycosides.

Data clinical trials The effectiveness and safety in patients with severe stable heart failure (NYHA functional class IV) are limited. Treatment of such patients should be carried out by doctors qualified special knowledge and experience.

Patients with heart failure combined with acute myocardial infarction and unstable angina were excluded from studies on the basis of which indications for use were determined. The effectiveness and safety of the drug for this group of patients has not been described. Use in unstable and decompensated heart failure is contraindicated.

Abrupt discontinuation of the drug should be avoided. The drug should be discontinued gradually over 2 weeks. The dose is reduced gradually, in several doses, until the final dose is reached - 25 mg 1 time per day.

If surgical intervention is necessary, the anesthesiologist should be informed about the therapy being carried out in order to select an anesthetic agent with minimal negative inotropic effect, however, discontinuation of the drug before surgery is not recommended.

It should be borne in mind that in patients taking beta-blockers, anaphylactic shock proceeds more severely.

Use in pediatrics

Experience with Betaloc ZOK in children is limited. Prescribing the drug to this category of patients is contraindicated.

Impact on the ability to drive vehicles and operate machinery

When driving vehicles and engaging in potentially hazardous activities that require increased attention and the speed of psychomotor reactions, it should be taken into account that when taking Betalok® ZOK, dizziness and fatigue may occur.

Overdose

Metoprolol at a dose of 7.5 g in an adult caused intoxication with a fatal outcome. A 5-year-old child who took 100 mg of metoprolol showed no signs of intoxication after gastric lavage. Taking 450 mg of metoprolol by a 12-year-old teenager resulted in moderate intoxication. Administration of 1.4 g and 2.5 g of metoprolol to adults caused moderate and severe intoxication, respectively. Taking 7.5 g by adults resulted in extremely severe intoxication.

Symptoms: the most serious are symptoms from the cardiovascular system, but sometimes, especially in children and adolescents, symptoms from the central nervous system and suppression of pulmonary function, bradycardia, AV block I-III degree, asystole, marked decrease in blood pressure, weak peripheral perfusion, heart failure, cardiogenic shock, depression of pulmonary function, apnea, increased fatigue, impairment and loss of consciousness, tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia; effects on the kidneys; transient myasthenic syndrome.

Concomitant use of alcohol, antihypertensive drugs, quinidine or barbiturates may worsen the patient's condition. The first signs of overdose can be observed 20 minutes to 2 hours after taking the drug.

Treatment: taking activated carbon, and, if necessary, gastric lavage.

Atropine at a dose of 0.25-0.5 mg IV for adults and 10-20 mcg/kg for children should be prescribed before gastric lavage (due to the risk of vagus nerve stimulation).

If necessary, maintain patency respiratory tract mechanical ventilation is performed. Terbutaline can be used by injection or inhalation to relieve bronchospasm.

It is necessary to replenish the blood volume and administer a glucose infusion. Atropine 1.0-2.0 mg IV, repeat administration if necessary (especially for vagal symptoms). ECG monitoring.

In case of myocardial depression it is indicated infusion administration dobutamine or dopamine. You can use glucagon 50-150 mcg/kg IV at intervals of 1 minute. In some cases, adding epinephrine to therapy may be effective.

For arrhythmia and a widened ventricular (QRS) complex, sodium solutions (chloride or bicarbonate) are infused. It is possible to install an artificial pacemaker.

Cardiac arrest due to an overdose may require resuscitation for several hours.

Symptomatic treatment is carried out.

Drug interactions

Metoprolol is a CYP2D6 substrate, and therefore drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) may affect the plasma concentrations of metoprolol.

Combinations to Avoid

Barbituric acid derivatives: Barbiturates increase the metabolism of metoprolol due to enzyme induction (study conducted with phenobarbital).

Propafenone: when propafenone was prescribed to 4 patients receiving metoprolol, there was an increase in the concentration of metoprolol in the blood plasma by 2-5 times, while 2 patients experienced side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. The interaction is likely due to propafenone's inhibition, like quinidine, of the metabolism of metoprolol via the CYP2D6 isoenzyme. Taking into account the fact that propafenone has beta-blocker properties, the co-administration of metoprolol and propafenone does not seem appropriate.

Verapamil: The combination of beta blockers (atenolol, propranolol and pindolol) and verapamil may cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta blockers have complementary inhibitory effects on AV conduction and function sinus node.

Combinations that may require dose adjustment of Betaloc® ZOK

Class I antiarrhythmic drugs: when combined with beta-blockers, the negative inotropic effect may be additive, resulting in serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with SSSS and impaired AV conduction. The interaction is described using disopyramide as an example.

Amiodarone: Concomitant use with metoprolol may lead to severe sinus bradycardia. Taking into account the extremely long T1/2 of amiodarone (50 days), it should be taken into account possible interaction long after discontinuation of amiodarone.

Diltiazem: Diltiazem and beta-blockers mutually enhance the inhibitory effect on AV conduction and sinus node function. When metoprolol was combined with diltiazem, cases of severe bradycardia were observed.

NSAIDs: NSAIDs reduce the antihypertensive effect of beta-blockers. This interaction has been reported in combination with indomethacin and is likely not to be observed in combination with sulindac. Negative interaction was noted in studies with diclofenac.

Diphenhydramine: Diphenhydramine reduces the biotransformation of metoprolol to β-hydroxymetoprolol by 2.5 times. At the same time, an increase in the effect of metoprolol is observed.

Epinephrine (adrenaline): Ten cases of severe hypertension and bradycardia have been reported in patients taking non-selective beta blockers (including pindolol and propranolol) and receiving epinephrine. The interaction was also observed in the group of healthy volunteers. It is assumed that similar reactions can be observed when epinephrine is used together with local anesthetics in case of accidental exposure to vascular bed. Apparently, this risk is much lower with the use of cardioselective beta-blockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg may increase diastolic blood pressure to pathological levels in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, beta blockers may cause paradoxical hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of development have been reported hypertensive crisis while taking phenylpropanolamine.

Quinidine: Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (in Sweden, approximately 90% of the population), causing mainly a significant increase in plasma concentrations of metoprolol and increased blockade of β-adrenergic receptors. It is believed that such an interaction is also typical for other beta-blockers, the metabolism of which involves the CYP2D6 isoenzyme.

Clonidine: Hypertensive reactions following abrupt withdrawal of clonidine may be exacerbated by concomitant use of beta-blockers. When used together, if it is necessary to discontinue clonidine, discontinuation of beta-blockers should begin several days before discontinuation of clonidine.

Rifampicin: Rifampicin may increase the metabolism of metoprolol, reducing its plasma concentration. Patients concomitantly taking metoprolol and other beta-blockers (eye drops) or MAO inhibitors should be closely monitored.

While taking beta-blockers, inhalational anesthetics enhance the cardiodepressive effect.

While taking beta-blockers, patients receiving oral hypoglycemic agents may require dose adjustment of the latter.

Plasma concentrations of metoprolol may increase when taking cimetidine or hydralazine.

Cardiac glycosides, when used in combination with beta-blockers, can increase AV conduction time and cause bradycardia.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children at temperatures above 30°C. Shelf life - 3 years.

Dosage regimen for Egilok with normal release rate:

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

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

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

For functional disorders of 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.

A selective β-adrenergic receptor blocker, has antianginal, antihypertensive and antiarrhythmic effects, reduces the automaticity of the sinus node, inhibits AV conduction, reduces the inotropic function of the myocardium and heart rate. The antihypertensive effect stabilizes at the end of the 2nd week of drug use. Reduces the number of angina attacks, reduces myocardial oxygen demand, and increases tolerance to physical activity. In case of myocardial infarction, it limits the ischemia zone of the heart muscle and prevents heart rhythm disturbances. The main advantage of Egilok Retard (extended-release tablets) is the prolonged release of metoprolol. Therapeutic effect noted at a significantly lower concentration of metoprolol in the blood than when taking metoprolol in usual forms tablets. Therefore, it is enough to prescribe 1 tablet per day of Egilok Retard to achieve a clinical effect.
The drug is quickly and completely absorbed into the gastrointestinal tract (95% of the dose). The absorption of metoprolol in retard form is significantly prolonged, which determines a uniform concentration of the drug Egilok Retard in the blood plasma and a relative bioavailability of 80% compared to the schedule of changes in the drug content in the blood after administration of immediate-release metoprolol. The maximum concentration in blood plasma is achieved 1.5 hours after oral administration and after 2-6 hours - the drug in the form of retard. Plasma protein binding - 12%. The volume of distribution is 5.6 l/kg body weight. Metoprolol is metabolized in the liver; its metabolites do not show activity. About 5% of the dose is excreted unchanged in the urine.

Indications for use of the drug Egilok

AH (arterial hypertension);
IHD: stable or unstable angina(except for Prinzmetal's angina);
heart failure;
heart rhythm disturbances (sinus, supraventricular tachycardia; ventricular extrasystole);
arrhythmia due to prolapse mitral valve;
secondary prevention after myocardial infarction;
functional disorders of cardiac activity, accompanied by tachycardia;
hyperthyroidism;
prevention of migraine attacks.

Use of the drug Egilok

For hypertension (arterial hypertension), the initial dose of Egilok Retard is 50 mg/day in 1 dose. Daily dose can be gradually increased to 100-200 mg in 1 dose. Egilok Retard can be used with other antihypertensive drugs to enhance the hypotensive effect.
For the treatment of angina pectoris, the dose is 50 mg 1 time per day with further dose titration to the clinically optimal dose. If necessary, the dose can be increased to 100-200 mg per dose. Egilok Retard can be used with other antianginal drugs.
For heart failure, the initial dose is 25 mg/day. If necessary, every 2 weeks the dose can be increased to 50 mg, after another 2 weeks - to 100 mg, if necessary, after 2 weeks to 200 mg.
For arrhythmia, the initial dose is 50-200 mg/day in 1 dose.
After myocardial infarction, for the purpose of secondary prevention, the dose is selected individually under the control of heart rate and blood pressure.
For the prevention of migraine attacks, the usual dose is 100-200 mg/day in 1 dose. The tablets are taken once a day (in the morning), without chewing and with a sufficient amount of liquid.
The drug can also be taken with food or on an empty stomach.

Contraindications to the use of the drug Egilok

G hypersensitivity to metoprolol or other components of the drug; AV block II-III degrees, severe sinus bradycardia (heart rate ≤50 beats/min), arterial hypotension, acute decompensated heart failure, severe peripheral circulatory disorders; cardiogenic shock, severe peripheral circulatory disorders, asthma, sick sinus syndrome.

Side effects of the drug Egilok

Decreased heart rate, blood pressure. AV conduction disturbances, symptoms of heart failure, and depression are also possible. There may be such side effects, such as fatigue, headache, dizziness, sleep disturbance. In many cases, these phenomena are temporary and disappear on their own when the dose of the drug is reduced.
Rarely, nonspecific skin reactions and coldness of the extremities, vomiting, diarrhea, constipation, bronchospasm, thrombocytopenia, and liver dysfunction occur.
If any other side effects occur that are not listed in the instructions, you must inform your doctor.

Special instructions for the use of the drug Egilok

The drug should be used with caution when treating patients with diabetes mellitus and diseases peripheral arteries, pheochromocytoma (it is possible to use the drug Egilok Retard only in combination with α-adrenergic receptor blockers), impaired renal and liver function. Before starting treatment, it is necessary to determine the function of the liver and kidneys. Treatment with Egilok Retard should be discontinued gradually. Sudden cessation of treatment, especially if cardiovascular pathology, may lead to worsening of the condition (withdrawal syndrome).
The use of Egilok Retard may cause fatigue or slight dizziness. Therefore, during the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
If a patient seeks medical help or needs surgical treatment, be sure to notify the doctor that the patient is taking the drug Egilok Retard.
Prescribing Egilok Retard during pregnancy and breastfeeding is possible if the potential benefit to the mother outweighs the risk to the child.

Interactions of the drug Egilok

Caution is necessary when using the drug simultaneously with:

verapamil and diltiazem - risk of hypotension, bradycardia, atrioventricular block, asystole;
clonidine - clonidine should be stopped a few days after the end of metoprolol to avoid the development of withdrawal syndrome;
narcotic drugs - the risk of developing a cardiodepressive effect;
ergotamine - increases the vasoconstrictor effect);
some drugs that affect the central nervous system: sleeping pills - bromazepam, lorazepam;
tranquilizers - chlordiazepoxide, trimethacin, tofisopam;
tri- and tetracyclic antidepressants - citalopram, moclobemide;
neuroleptics - chlorpromazine, triflupromazine - and alcohol - risk of arterial hypotension, effect on the central nervous system;
NSAIDs, such as indomethacin, may reduce the antihypertensive effect of metoprolol;
estrogens, for example norethindrone, norgestrel - the antihypertensive effect of metoprolol is reduced;
hypoglycemic by oral means, for example, chlorpropamide, glibenclamide, tolbutamide and insulin - enhancing their hypoglycemic effect, masking the symptoms of hypoglycemia;
curare-like muscle relaxants - increased neuromuscular blockade;
H2 receptor antagonists, for example cimetidine - may increase the bioavailability of the drug);
rifampicin, barbiturates, such as phenobarbital, secobarbital, pentobarbital - the antihypertensive effect of metoprolol may be reduced.

Particular caution is required when used with ganglion-blocking drugs and other β-adrenergic receptor blockers, sympathomimetics, antiarrhythmic drugs I class.

Overdose of the drug Egilok, symptoms and treatment

Symptoms: arterial hypotension, sinus bradycardia, AV block, heart failure, cardiogenic shock, asystole, nausea, vomiting, cyanosis, bronchospasm, loss of consciousness, coma.
Treatment: gastric lavage, taking activated charcoal, for severe hypotension - β-adrenergic receptor agonists (norepinephrine) or intravenous administration of atropine (for bradycardia). If there is no effect, dopamine or dobutamine should be prescribed. Glucagon (1-10 mg) may be effective. In severe cases, implantation of an artificial pacemaker may be necessary. Bronchospasm is eliminated by intravenous administration of β2-adrenergic agonists. Metoprolol is practically not excreted from the body by hemodialysis.

Storage conditions for the drug Egilok

At a temperature of 15-25 °C.

List of pharmacies where you can buy Egilok:

Saint Petersburg

International name

Metoprolol

Group affiliation

Beta1-adrenergic blocker selective

Dosage form

Tablets, extended-release tablets, enteric-coated tablets, extended-release film-coated tablets

pharmachologic effect

Cardioselective beta1-blocker. It does not have a membrane-stabilizing effect and does not have internal SMA. It has hypotensive, antiangial 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 the use of beta-adrenergic blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), which returns to the original level after 1-3 days, and decreases with long-term administration.

The hypotensive effect is due to a decrease in IOC and renin synthesis, inhibition of the activity of the renin-angiotensin system (of greater importance in patients with initial hypersecretion of renin) 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 peripheral sympathetic influences. Reduces high blood pressure at rest, during physical exertion and stress. The hypotensive effect develops quickly (systolic blood pressure decreases after 15 minutes, maximum after 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: 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 (extension 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 number and severity of angina attacks and increases exercise tolerance. Due to an increase in end-diastolic pressure in the LV and an increase in the stretch of ventricular muscle fibers, it can increase the need for oxygen, especially in patients with CHF.

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 AV conduction (mainly in the antegrade and to a lesser extent in the retrograde directions through the AV node) and along additional pathways.

With supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional diseases heart and thyrotoxicosis reduces heart rate or can even lead to the restoration of sinus rhythm.

Prevents the development of migraine.

In contrast to non-selective beta-blockers, when prescribed 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 and uterus) and on carbohydrate metabolism; the severity of the atherogenic effect does not differ from the effect of propranolol. When taken for many years, it reduces the concentration of cholesterol in the blood. When used in large doses(more than 100 mg/day) has a blocking effect on both subtypes of beta-adrenergic receptors.

With intravenous infusion of metoprolol tartrate for 10 minutes or more maximum action develops after 20 minutes, the decrease in heart rate at doses of 5 and 10 mg is 10 and 15%, respectively.

Indications

IHD, exertional angina, unstable angina, myocardial infarction (acute phase, as well as secondary prevention).

Arterial hypertension, hypertensive crisis.

CHF (compensated) in combination with diuretics, ACE inhibitors and cardiac glycosides.

Rhythm disturbances (including when general anesthesia) – sinus tachycardia, ventricular and supraventricular arrhythmias (including supraventricular tachycardia, atrial fibrillation, atrial flutter, atrial tachycardia, tachyarrhythmias caused by digitalis, catecholamines, ventricular extrasystole, arrhythmias due to mitral valve prolapse), congenital long QT syndrome .

Thyrotoxicosis ( complex therapy), withdrawal syndrome, migraine (prevention), tremor (essential, senile), anxiety (auxiliary treatment), akathisia against the background of antipsychotics.

Contraindications

Hypersensitivity, cardiogenic shock, AV block II-III stage, SA block, SSSU, sinus bradycardia (heart rate less than 50/min), acute HF or decompensated CHF, Prinzmetal's angina, arterial hypotension, acute myocardial infarction (P-Q more than 0.24 s or systolic blood pressure less than 100 mm Hg); lactation period, simultaneous use of MAO inhibitors or simultaneous intravenous administration of verapamil. Caution. Diabetes mellitus, metabolic acidosis, bronchial asthma, COPD (emphysema, chronic obstructive bronchitis), liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, thyrotoxicosis, depression (including a history), psoriasis, obliterating peripheral vascular diseases (intermittent claudication, Raynaud's syndrome), pregnancy, childhood (efficacy and safety have not been determined ), elderly age.

Side effects

From the nervous system: increased fatigue, weakness, headache, slower speed of mental and motor reactions. Rarely: paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremors, convulsions, depression, anxiety, decreased attention, drowsiness, insomnia, nightmares, confusion or momentary loss memory, hallucinations, asthenia, myasthenia.

From the senses: rarely - decreased vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis, tinnitus, decreased hearing.

From the cardiovascular system: sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely - decreased myocardial contractility, development (worsening) of CHF (edema, swelling of the feet and/or lower legs, shortness of breath), heart rhythm disturbances, manifestation of vasospasm (increased peripheral circulatory disorders, cold snap) lower limbs, Raynaud's syndrome), myocardial conduction disturbances, cardialgia. Very rarely - aggravation of pre-existing AV conduction disorders.

From the digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea, in some cases - impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), changes in taste.

From the outside skin: skin rashes (exacerbation of psoriasis), psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

From the respiratory system: nasal congestion, bronchospasm when prescribed in high doses (loss of selectivity and/or in predisposed patients), shortness of breath.

From the outside endocrine system: hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state.

Allergic reactions: urticaria, skin itching, rash.

Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes, hyperbilirubinemia.

Effect on the fetus: intrauterine retention growth, hypoglycemia, bradycardia.

Other: pain in the back or joints, weight gain, decreased libido and/or potency, with abrupt cessation of treatment - withdrawal syndrome (increased angina attacks, increased blood pressure).

Application and dosage

Inside, with food or immediately after a meal, the tablets can be divided in half, but not chewed and washed down with liquid, for dosage forms prolonged action - swallow whole, do not crush, do not break (except for metoprolol succinate and tartrate), do not chew.

For arterial hypertension average dose– 100-150 mg/day in 1-2 doses, if necessary – 200 mg/day.

For angina pectoris – 50 mg 2-3 times a day.

For hyperkinetic cardiac syndrome (including thyrotoxicosis) – 50 mg 1-2 times a day.

For tachyarrhythmia – 50 mg 2-3 times a day, if necessary – 200-300 mg/day.

Secondary prevention of myocardial infarction – 200 mg/day.

Prevention of migraine – 100-200 mg/day in 2-4 doses.

To relieve paroxysmal supraventricular tachycardia, it is administered parenterally in a hospital setting. Administer slowly, a dose of 2-5 mg (1-2 mg/min). If there is no effect, the administration can be repeated after 5 minutes. Increasing the dose above 15 mg usually does not lead to greater severity of action. After stopping the attack of arrhythmia, patients are transferred to oral administration at a dose of 50 mg 4 times a day, with the first dose taken 15 minutes after stopping the IV administration.

IN acute stage myocardial infarction immediately after hospitalization of the patient (with constant monitoring of hemodynamics: ECG, heart rate, AV conduction, blood pressure), a bolus of 5 mg should be administered intravenously, the administration should be repeated every 2 minutes until a total dose of 15 mg is reached. If well tolerated, after 15 minutes - orally, 25-50 mg every 6 hours, for 2 days. Patients who do not tolerate the full IV dose should be started on oral administration, starting with a half dose. Maintenance therapy continues at doses of 200 mg/day (in 2 doses) for 3 months to 3 years.

Renal failure does not require dose adjustment. In case of liver failure, it is advisable to prescribe other beta-blockers that are not metabolized in the liver.

special instructions

Monitoring of patients taking beta-blockers includes monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), the concentration of glucose in the blood in patients with diabetes (once every 4-5 months). The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50/min.

Possible increased severity of allergic reactions (against the background of aggravated allergy history) and lack of effect from administration usual doses epinephrine.

In elderly patients, it is recommended to monitor kidney function (once every 4-5 months). May increase symptoms of peripheral arterial circulation disorders. Patients with cardiac arrhythmias whose systolic blood pressure is below 100 mm Hg should be given IV only if special precautions are taken (there is a risk of a further decrease in blood pressure). The drug is discontinued gradually, reducing the dose over 10 days.

In case of arterial hypertension, the effect occurs after 2-5 days, a stable effect is observed after 1-2 months.

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. In smokers, the effectiveness of beta-blockers is lower.

At combination therapy with clonidine, the latter should be discontinued several days after metoprolol is discontinued in order to avoid a hypertensive crisis. At a dose above 200 mg/day, cardioselectivity decreases.

Metoprolol may mask some clinical manifestations thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because 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.

If necessary, beta2-adrenergic stimulants are used as concomitant therapy for patients with bronchial asthma; for pheochromocytoma - alpha-blockers.

If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a drug for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not recommended.

Reciprocal activation of the n.vagus can be eliminated by intravenous administration of atropine (1-2 mg).

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

In case of increasing bradycardia (less than 50/min), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias in elderly patients, severe violations liver and kidney function, it is necessary to reduce the dose or discontinue treatment. It is recommended to discontinue therapy if skin rashes appear and depression develops caused by taking beta-blockers.

The drug is discontinued gradually, reducing the dose over 10 days. If treatment is abruptly stopped, withdrawal syndrome may occur (increased angina attacks, increased blood pressure). Special attention When discontinuing the drug, it is necessary to pay attention to patients with angina pectoris.

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

During pregnancy, it is prescribed only for strict indications (due to possible development in the newborn bradycardia, hypotension, hypoglycemia and respiratory paralysis). Treatment must be interrupted 48-72 hours before delivery. In cases where this is not possible, it is necessary to ensure strict monitoring of newborns for 48-72 hours after delivery.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction

Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving metoprolol. Iodine-containing radiopaque drugs for intravenous administration increase the risk of developing anaphylactic reactions.

Phenytoin with intravenous administration, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure.

Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.

The hypotensive effect is weakened by NSAIDs (Na+ retention and blockade of Pg synthesis by the kidneys), corticosteroids and estrogens (Na+ retention).

Cardiac glycosides, methyldopa, reserpine and guanfacine, BMCC (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and HF. Nifedipine can lead to a significant decrease in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

Prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins.

Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedative and hypnotic drugs increase CNS depression.

Not recommended simultaneous use with MAO inhibitors due to a significant increase in the hypotensive effect, the break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days.

Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

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