Self-medication can be harmful to your health.
You should consult your doctor and read the instructions before use.

Egilok sr: instructions for use

Compound

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 sustained release film-coated tablets 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.

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; - cardiac ischemia; - 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.

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 heart side - vascular 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 changes skin, 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.

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 using Egilok 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.

Precautionary measures

In patients with severe heart failure, the dose should be individually selected, starting with the lowest concentration.
During the use of Egilok, worsening of peripheral circulatory disorders was observed.

Even in therapeutic doses, Egilok can cause broncho-obstructive complications, especially if the patient has a predisposition in the form of a disease of the bronchopulmonary system.
In patients with diabetes mellitus and in other patients taking hypoglycemic drugs, blood sugar levels are regularly monitored.
When conducting surgical interventions and so on. , you should inform the anesthesiologist about taking Egilok.
When prescribing Egilok simultaneously with drugs that cause depression of the nervous system (hypnotics, tranquilizers, antipsychotics, tranquilizers), the effect may be enhanced; monitoring by a neurologist or psychiatrist is necessary.

In patients whose work and lifestyle require increased concentration (including driving), the question of prescribing the drug should be decided only after a thorough examination of the patient. Start driving a car, etc. after assessing the patient’s individual response to the drug for at least several days.

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

Instructions for use

The name "egilok" - trademark, given medicine manufacturer (Hungary). There is also Indian egilok.

Egilok's INN is metoprolol. This is the main active ingredient, supplemented by auxiliary ingredients: anhydrous colloidal silicon dioxide, microcrystalline cellulose, magnesium stearate, sodium carboxymethyl starch and povidone. Dosage form: tablets.

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

In Latin Egilok is Egilok, and in current beginning designated: Metoprolol tartat, if it is a fast-acting form. Extended-release egilok retard contains another metoprolol compound – succinate. Accordingly: Metoprolol succinate.

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

Large dosage tablets have risks that help them break neatly. The tableted drug has no odor.

Pharmacological group, mechanism of action

Pharmacotherapeutic group of Egilok: beta1-blockers. Egilok is a cardioselective drug that targets the myocardium and the coronary vessels that supply it.

Selective beta1-blockers at a reasonable dosage work only with beta1-adrenergic receptors, blocking only them. Another type, responsible for breathing, gestation of the fetus, peripheral vessels - β2-adrenergic receptors - calmly continues to work, the egilok is not directed at them. The medicine purposefully moves towards its intended target, finding the receptors for which it was created. By binding to them, egilok does not allow catecholamines to produce a strong shake-up in the body under provoking factors:

1. Emotional stress;
2. Increased physical activity;
3. Sudden changes in weather (almost 100% of “vascular” patients react to this by worsening their condition).

The sympathetic system, under the influence of egilok, reduces activity towards the myocardium. Egilok, by blocking β1-adrenergic receptors, slows down the pulse, reduces four important values ​​at once: heart rate, volume cardiac output, contractility force and blood pressure numbers.

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

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

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

Normalizing the size and function of the left ventricle and restoring the time needed for rest (diastole) has a direct impact on patient survival. Mortality from vascular accidents, especially in men, is significantly reduced. Why egilok tablets are taken: to prevent such misfortunes as heart attacks, strokes, cases sudden death. If hypertension is moderate, “mild”, then healing effect more clearly expressed.

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

The selectivity of Egilok is an advantage over non-selective drugs of the same group. It has almost no spasmodic effect (with adequate doses) on the respiratory muscles (bronchi), as well as on the smooth muscles of the walls of peripheral vessels. It also does not affect tissues of muscles not included in the myocardial zone. It works only cardiologically, with a positive effect.

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

Pharmacokinetics

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

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

The drug is eliminated by the kidneys. It may slow down if you have kidney failure, but this does not cause significant harm.

Indications for use

For egilok, the indications for its use are similar to the use of other beta-blockers. What these tablets are prescribed for can be understood by studying the mechanism of action of egilok. The drug is used for:

• Hypertension of all stages (arterial hypertension) - monotherapy or as a component in a complex of drugs;
• Tachyarrhythmias (tachycardias) of inorganic origin are functional reversible malfunctions of the myocardium;
• Arrhythmias with organic causes: supraventricular, paroxysmal tachycardia, atrial, ventricular, supraventricular extrasystole;
• Angina pectoris, stable course;
• Prevention of exacerbation of migraine, prevention of painful attacks;
• Hyperthyroidism (symptom relief, addition of specific therapeutic methods);
• Angina pectoris complicated by a heart attack is included in the complex of basic therapeutic measures. Treatment of the post-infarction state, simultaneous prevention of recurrence, prevention of a new heart attack.

The instructions for use indicate at what pressure Egilok is effective. It is prescribed for any stage of this disease. If blood pressure levels are slightly higher than normal, one drug may help (monotherapy). Then the instructions for use provide a minimum - 25 mg of egilok per dose may already be enough.

Ischemia – narrowing, infringement. In fact, there is no infringement, there is a strong narrowing of the feeding arteries. In acute cases, and - their blockage, closure of the lumen with atherosclerosis (plaques come off), thrombosis (blockage of a vessel with a blood clot). When the lumen of the vessels is narrowed, the nutrition of the myocardium is inevitably disrupted. Egilok relaxes blood vessels, facilitating the passage of blood through them to the myocardium. IHD is a form of angina “with experience”, its dangerous phase. By improving the blood supply and nutrition of the heart, egilok helps it survive.

Used after heart attacks, protects against recurrences, increases survival

This happens with neuroses, in those suffering from dystonia, other disorders of the nervous system or cardiovascular system. Among the whole range of symptoms, tachycardia often comes out ahead of the rest. It worries more, creates fear, intensifies itself and intensifies the rest of the symptoms. There is no better remedy than beta blockers. Egilok will calm down rapid pulse and, having some anxiolytic, anti-anxiety effect, will calm a person. The other one will leave at the same time unpleasant symptoms: fear, sweating, tremors. Even a heart that does not have organic changes anxiety no good. The drug will help return everything to normal.

Arithymia of organic origin

Complex, severe rhythm disturbances. Caused by various reasons: atherosclerosis, impaired conduction of myocardial impulses, pathology of the sinus node. Beta blockers regulate the rhythm during tachycardia (reduce heart rate). Some types of ecstasystole are amenable to egilok, the rhythm is evened out. Or the extrasystoles at least become less frequent and acquire a sinus rhythm instead of an erratic one. The medicine egilok is sometimes used even for implicit bradycardia - for health reasons. Special caution is needed here, but the patient’s life must be saved. Even Egilok 25 may turn out to be an excess, it is divided, and initially dosed with a quarter of such a tablet. And this small dose will still have the desired impact. Almost without slowing down the pulse contractions.

The instructions for use list bradycardia as a contraindication for Egilok, but reviews from practicing cardiologists indicate: sometimes, in the smallest doses, it is necessary. Grind (again contrary to the instructions), directly under the tongue - for speed of action. This will save lives in an acute situation, and the selection of other drugs will come later.

If the heart rate allows (not too low), beta blockers help with this diagnosis. Attacks of angina pectoris, it is not for nothing that it is named with the addition of the word “stress,” occur during physical or mental stress. Egilok, taken constantly, relieves stress. Attacks become rare and mild.

Migraine, attack prevention

The disease is common, but little studied. Dilatation (expansion) is considered to be the culprit of pain today. cerebral vessels from overflowing with blood and high blood pressure.

By lowering blood pressure, egilok warns and blocks dilatation.

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

The disease cannot be treated with beta blockers. But they are used for an auxiliary purpose. Egilok will help reduce the rapid pulse characteristic of the disease. At the same time, the intensity of sweating, tremor, and blood pressure decrease. The symptoms of hyperthyroidism are smoothed out, this is important for the patient’s well-being.

Prevention of recurrent heart attacks

The drug, in combination with others, helps protect a person from the risk of a recurrence of a heart attack. A weakened heart may not be able to withstand a second heart attack. Here the role of medications and the doctor’s ability to navigate their selection and development of treatment tactics are vitally important.

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

Use with caution

• Pheochromocytoma – combination with alpha-blockers is necessary; without them, Egilok is not used.
• Diabetes mellitus has a dose-dependent effect, with large doses Stimulation of hypoglycemia cannot be ruled out.
• Metabolic acidosis – interference with failure may occur metabolic processes beta blocker with unpredictable results.
• Bronchial asthma - low impact on the second type of receptors that control the respiratory system - β2-adrenergic receptors - occurs occasionally in sensitive, asthmatic patients.
• Obliterating endarteritis, pathology of peripheral vessels.
• Failure - renal, hepatic: possible clearance problems, delayed elimination, increased concentration of the drug above the recommended level in the body.
• Depression is a stage of exacerbation or remission.
• Tendency to allergies - if it is necessary to administer anti-shock drugs (adrenaline), the body may not respond to them under the influence of egilok.
• Hyperthyroidism (thyrotoxicosis) – increased hormonal activity of the affected person thyroid gland requires careful selection of drugs and doses, even for symptomatic treatment.
• COPD – serious illnesses lungs make the respiratory system sensitive even to almost neutral selective beta blockers. The cardioselectivity of Egilok does not exclude micro-influences on other systems. If they are impaired by disease, special control is required.

Pregnancy, lactation

If both are at risk: the mother from stopping Egilok, the fetus from using it, doctors compare the risks. If possible, a drug that is gentle on the baby is selected for the pregnant woman. If such a possibility is excluded, and it is egilok that is needed (for health reasons), they try to save both. The effect of the drug on the developing organism is carefully monitored.

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

If there are any, intensive therapy is carried out and attempts are made to correct Negative influence drug received in utero.

The child may be under observation for a long time.

Directions for use, dosage

Take the drug without strictly linking the time of administration with food. There is no need to wait minutes before or after eating. You can - right along with food, it will be absorbed even better. The daily dose of egilok is divided according to the instructions in the instructions into two doses - morning and evening. The minimum is set based on the condition and concomitant diseases. Start with small doses. Through gradual selection they reach the optimal one. At each such increasing “step” they stay for up to two weeks to check the effectiveness.

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

The dosage of Egilok can and should vary depending on the type of disease. There may be the same doses for some diagnoses.

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

Start with 25 or 50 mg, depending on the patient’s condition and overall tolerance to the medication. For ischemic heart disease, this dosage is taken twice or three times a day. The daily dose can be increased to 200 mg. If such an amount is poorly tolerated, and a smaller amount does not give the desired effect, leave it in a normally tolerated amount. The treatment is adjusted by adding another medicine that complements Egilok, which alleviates the patient’s condition.

Functional tachyarrhythmia

Prescription: morning and evening – 50 mg each. If the effect is insufficient - 100 mg. Monotherapy usually works well.

Extrasystole, tachycardia

Start with 25 or 50 mg. Frequency of administration: three times a day. If it is well tolerated but has little effectiveness, the dose is increased. Do not exceed the maximum level - 200 mg. Can be practiced combination treatment arrhythmias. It’s better to start – stationary.

Stable exertional angina

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

Preventing migraine attacks

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

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

For frequently annoying migraines, Egilok is indicated for use - constantly

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

Side effects

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

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

• Drying of the mucous membranes of the mouth;
• Insomnia or drowsiness;
• Symptomatic exacerbation of heart failure;
• Orthostatic hypotension;
• Hallucinations;
• Painful heartbeat;
• Cardiogenic shock;
• Liver failure;
• Abdominal pain,
• Cardiac conduction disturbances;
• Constipation;

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

Blockade of myocardial sections (atrioventricular);

Bronchospasm;

Hypoglycemia;

Blueness (cyanosis) of the skin;

Unconscious state;

Falling into a coma.

An overdose of Egilok during therapy with blood pressure-lowering drugs, taking barbiurates, or in the presence of ethanol in the body is more dangerous. Symptoms intensify, the prognosis worsens.

Emergency assistance is needed, hospitalization and a set of rehabilitation measures are required.

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

Drug interactions

Concomitant use with antihypertensive drugs causes an additive effect. Combination therapy prescribed, started and monitored by a doctor. The overall effect is the goal of such treatment, but it should not be excessive. Excessive doses are dangerous due to hypotension, which can cause a number of complications. Some of them are more dangerous than high blood pressure.

It is risky to combine Egilok and other beta blockers with calcium channel blockers (slow). Particularly dangerous intravenous use verapamil, there is a risk of asystole (cardiac arrest).

Antiarrhythmics taken orally (cordarone, quinine) can provoke atrioventricular block. Not excluded severe bradycardia.

Do not combine Egilok with cardiac glycosides: the conductive function of the heart may be affected and severe bradycardia may develop.

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

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

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

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

Ergotamine has a vasoconstrictor effect; a beta blocker cannot resist it in this combination.

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

Antihyperglycemic agents and insulin increase their activity when paired with Egilok (risk of hypoglycemia).

Estrogens prevent beta blockers from lowering blood pressure

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

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

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

special instructions

Analogues

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

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

The most famous analogues are:

• Metoprolol: Russia, Poland;
• Lidalok: Russia;
• Metoprolol Teva: Israel;
• Metolol: Russia;
• Metoprolol ratiopharm: Germany;
• Emzok: Germany;
• Metoprolol organic: Russia;
• Metoprolol zentiva: Slovenia;
• Egilok Retard (extended): Switzerland, Hungary;
• Metoprolol-Obl: Russia;
• Metoprolol succinate: India;
• Metozok: Russia;
• Metokor adifarm: Bulgaria;
• Metoprolol tartrate: Ukraine;
• Corvitol 50: Germany;
• Betaloc, Betaloc ZOK (extended): Sweden, France;
• Metocard: Russia, Poland;
• Metoprolol-acri: Russia;
• Vasocardin: Slovenia;
• Betalok: Sweden;
• Egilok S (extended): Hungary;
• Serdol: Romania;
• Egilok: Hungary.

Dispensation by prescription.

"Egilok" is a synthetic drug used, in particular, for the treatment of arterial hypertension and the prevention of migraines. The main active ingredient of this drug is metoprolol tartrate. "Egilok" is available in dosages of 0.025 g, 0.05 g and 0.1 g in packs of 20, 30, 60,100 tablets. The drug "Egilok Retard" is also available in tablet form - with the same active and excipients. A pack contains 30 tablets with a dosage of 0.05 g and 0.1 g.

The drug is very quickly and almost completely (95 percent) absorbed from gastrointestinal tract. Its bioavailability is 50 percent. During treatment, the level of bioavailability is 70 percent. Eating 20-40 percent helps increase the bioavailability of the drug. The active substance of Egilok - metoprolol - is biotransformed in the liver. Metabolites of the drug are not pharmacologically active. 95 percent of the active substance of the drug is excreted from the body within 72 hours, in the urine. Approximately 5 percent of metoprolol remains unchanged. In this form they are excreted from the body.

Indications for use

"Egilok" is prescribed to patients with arterial hypertension (especially people over 60 years old), using this drug independently or in complex therapy with other antihypertensive drugs. It is necessary to take "Egilok" for secondary prevention of myocardial infarction, for the prevention of angina attacks, in case of violations heart rate– ventricular extrasystole, supraventricular arrhythmia, with hyperthyroidism. The drug is also prescribed for the prevention of migraines. "Egilok" is also used for coronary heart disease,

pharmachologic effect

"Egilok" is a cardioselective beta blocker that has a hypotensive effect, reduces the heart rate, reduces the severity of angina pectoris and the frequency of its attacks, helps improve physical condition patient. Also, thanks to the action of Egilok, the risk of recurrent myocardial infarction can be significantly reduced. Prevents the occurrence of migraines. If the doses indicated in the instructions are observed, it has no effect on peripheral arteries and bronchial smooth muscles.

The maximum effect of the drug appears within an hour and a half after administration. Approximately 5 percent of the active substance is excreted unchanged from the body in urine. The remaining amount of the drug is biotransformed in the liver. Therefore, people with liver pathology and disorders of its functions need medical supervision and dosage adjustment.

Directions for use and doses

The dosage of "Egilok" is prescribed to each patient at individually taking into account his state of health and the presence of accompanying factors. For example, for arterial hypertension, the initial dose of the drug is 50 mg per day in one or two doses. If there is no effect or insignificant results, it is recommended to increase the dosage, but not more than 200 mg per day. For patients suffering from angina pectoris, the recommended dose of the drug is 100-200 mg per day 1 or 2 times a day. A similar dose is prescribed for supraventricular arrhythmias, as well as for extrasystole. The drug should be taken twice a day (morning and evening). 100-200 mg per day twice a day is the drug prescribed for the prevention of secondary myocardial infarction and migraine attacks. It is not recommended to increase the dose indicated in the annotation.

In patients with diabetes, it is necessary to constantly monitor blood sugar levels.

When prescribing Egilok to patients with impaired liver and kidney function, medical supervision is required. This is necessary due to the ability of the drug to accumulate in the excretory organs.

Contraindications to the use of the drug

"Egilok" should not be prescribed to patients with sinus bradycardia with a heart rate less than 60 beats per minute; AV block of the second or third degree; sinoatrial block; peripheral circulatory disorders; arterial hypotension (low blood pressure below 90-100 mm Hg); high susceptibility of the drug components. In this case, any other means with similar action.

Side effects

While taking Egilok, you may experience high fatigue, drowsiness, dizziness, depression, insomnia, decreased concentration, nausea, vomiting, constipation, dry mouth, abdominal pain, heart failure. IN in rare cases visual disturbances, ringing in the ears, conjunctivitis may occur, allergic reactions, redness of the skin, baldness, increased sweating, weight gain. But in most cases the drug is well tolerated.

"Egilok" can cause absent-mindedness and drowsiness, so it should be prescribed with caution to people whose profession requires special attention.

A drug Egilok- it is beta1-adrenergic blocking, antiarrhythmic, hypotensive, antianginal.
Metoprolol suppresses the effects increased activity sympathetic system on the heart, and also causes rapid decline 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 physical performance patient.
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 with 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 free fatty acids in blood serum. 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 (glomerular filtration rate less than 5 ml/min), a significant accumulation of metabolites is observed. 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 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%). For 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 lower limbs, feeling of heartbeat; infrequently - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, 1st degree AV block; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders).
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 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 taste sensations.
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 heart attack myocardium, accompanied by a heart rate below 45 beats/min, with a PQ interval of more than 240 ms and SBP below 100 mm Hg.

Art.
With caution: diabetes mellitus; metabolic acidosis; bronchial asthma; COPD; renal/liver failure; myasthenia gravis; pheochromocytoma (when used simultaneously with alpha-blockers); thyrotoxicosis; AV block 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.
Despite the fact that when taking therapeutic doses of metoprolol, only small amounts of the drug are released into the breast milk, 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.
Termination simultaneous administration metoprolol and clonidine should definitely be started by stopping metoprolol, and then (after a few days) clonidine; if clonidine is first discontinued, it may develop hypertensive crisis.
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 increase with the simultaneous 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. With absence 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 lack of effect from administration usual doses 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 risk coronary disorders. Special attention when discontinuing the drug, care must be taken in patients with disease coronary arteries.
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 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 (eg 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 recovery of blood glucose concentrations to normal level. 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 notify the surgeon/anesthesiologist about the therapy being performed (choice of drug for general anesthesia with minimal negative inotropic effects), 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, severe liver dysfunction; sometimes it is necessary to stop treatment. Patients with severe renal failure It is recommended to monitor renal function.
Special monitoring of the condition of patients with depressive disorders taking metoprolol; 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 -

Beta1 blocker

Release forms

• 30 - dark glass jars (1) - cardboard packs. 60 - dark glass jars (1) - cardboard packs 60 - dark glass jars (1) - cardboard packs. 100 mg tablets - 30 pcs per pack. tablets 25 mg - 30 pcs per pack. tablets 50 mg - 30 pcs per pack. Extended-release tablets, film-coated, white or almost white, oblong in shape, biconvex, with a notch on both sides. pack of 10 tablets pack of 30 tablets pack of 30 tablets

Description of the dosage form

• 10 - blisters (1) - cardboard packs. 10 - blisters (2) - cardboard packs. 10 - blisters (3) - cardboard packs. tablets tablets Extended-release film-coated tablets Extended-release film-coated tablets are white, oval, biconvex, scored on both sides. Extended-release tablets, white, oval, biconvex, film-coated, scored on both sides. Extended-release tablets, film-coated tablets

pharmachologic effect

Mechanism of action: Metoprolol suppresses the effects 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 the standing and lying position. The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance. In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its 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 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 chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken starting from low doses (2-5 mg/day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient. 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. It does not increase the duration of hypoglycemic attacks. Metoprolol causes a slight increase in 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

Absorption After oral administration, metoprolol is almost completely (approximately 95%) absorbed from the gastrointestinal tract. However, after absorption, metoprolol is largely metabolized during the first pass through the liver. Bioavailability is approximately 35%. With repeated doses, AUC increases by approximately 20%. The plasma concentration versus time curve has features characteristic of sustained-release drugs. The pharmacokinetics of metoprolol is linear up to a dose of 800 mg. Distribution: Plasma protein binding is 10%. Metoprolol is well distributed in tissues and has a large Vd of 5.5 l/kg. Over the course of 4-6 hours after administration, the slow absorption phase enters an approximately 6-hour plateau (Cmax = 37.4 ng/ml after a single dose, Cssmax is 54.7 ng/ml), followed by a slow elimination phase. Metabolism Metoprolol is metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system. Metabolites (O-desmethylmetoprolol and β-hydroxymetoprolol) do not have beta-blocking activity. Since the drug is metabolized by polymorphic enzymes, its level in the blood plasma has significant (up to 17-fold) differences in different patients. The elimination T1/2 of metoprolol in the form of retard tablets is 6-12 hours, which is much longer than the T1/2 of metoprolol in the usual dosage form (approximately 3 hours). The longer half-life may be explained by delayed absorption. Metoprolol is excreted primarily by the kidneys (approximately 95%). About 10% of the administered dose of metoprolol is excreted unchanged. Metabolites are excreted in bile. Pharmacokinetics in special clinical cases Metoprolol is not removed from the body by hemodialysis. Treatment of patients with reduced renal function does not require dose adjustment of the drug. Impaired liver function slows down the metabolism of metoprolol, and in cases of insufficiency of liver function, the dose of the drug should be reduced.

Special conditions

Monitoring of patients taking beta-blockers includes regular measurement of heart rate (HR) and blood pressure, blood glucose concentration in patients with diabetes mellitus. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents for oral administration should be selected individually. The patient should be taught how to calculate heart rate and 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. There may be an increase in the severity of hypersensitivity reactions and a lack of effect from the administration of usual doses of epinephrine (adrenaline) in patients with a burdened allergic history. 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 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, the concentration of blood glucose should be monitored and, if necessary, the dose of insulin or hypoglycemic agents for oral administration should be adjusted (see section "Interaction with other medicines "). If it is necessary to prescribe to patients with bronchial asthma, beta2-adrenergic stimulants are prescribed as concomitant therapy; for pheochromocytoma, alpha-adrenergic 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 action), discontinuation of the drug is not recommended. 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 medical supervision to detect an excessive decrease in blood pressure or bradycardia. In elderly patients, it is recommended to regularly monitor liver function.Adjustment of the dosage regimen is required only if an elderly patient develops increasing bradycardia (less than 50 beats/min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), or atrioventricular block. , bronchospasm, ventricular arrhythmias, severe liver dysfunction, sometimes it is necessary to stop treatment. In patients with severe renal failure, monitoring of renal function is recommended. Special monitoring should be carried out for the condition of patients with depressive disorders taking metoprolol; in case of development 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 complex equipment. Caution must be exercised when driving vehicles and when engaging in potentially hazardous activities that require increased concentration (risk of dizziness and fatigue). OVERDOSE Symptoms: 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 increase with the simultaneous use of ethanol, antihypertensive drugs, quinidine and barbiturates. The first symptoms 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 the threat of heart failure - intravenously, at intervals of 2-5 minutes, beta-adrenergic agonists - until the desired effect is achieved or intravenously 0.5-2 mg of atropine. 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.

Compound

• metoprolol succinate 100 mg, which corresponds to the content of metoprolol 95 mg Excipients: microcrystalline cellulose - 295.6 mg, methylcellulose - 47.5 mg, glycerol - 0.95 mg, corn starch - 7.75 mg, ethylcellulose - 45.7 mg, magnesium stearate - 7.5 mg. Film shell composition: sepifilm LP 770 white - 15 mg (microcrystalline cellulose 5-15%, hypromellose 60-70%, stearic acid 8-12%, titanium dioxide (E171) 10-20%). metoprolol succinate 25 mg, which corresponds to the content of metoprolol 23.75 mg Excipients: microcrystalline cellulose - 73.9 mg, methylcellulose - 11.87 mg, glycerol - 0.24 mg, corn starch - 1.94 mg, ethylcellulose - 11.43 mg, magnesium stearate - 1.87 mg. Film shell composition: sepifilm LP 770 white - 3.75 mg (microcrystalline cellulose 5-15%, hypromellose 60-70%, stearic acid 8-12%, titanium dioxide (E171) 10-20%). metoprolol succinate 50 mg, which corresponds to the content of metoprolol 47.5 mg Excipients: microcrystalline cellulose - 147.8 mg, methylcellulose - 23.75 mg, glycerol - 0.48 mg, corn starch - 3.87 mg, ethylcellulose - 22.85 mg, magnesium stearate - 3.75 mg. Film shell composition: sepifilm LP 770 white - 7.5 mg (microcrystalline cellulose 5-15%, hypromellose 60-70%, stearic acid 8-12%, titanium dioxide (E171) 10-20%). Metoprolol tartrate 100 mg Excipients: colloidal anhydrous silicon dioxide, magnesium stearate, microcrystalline cellulose; pellets contain: macrogol 6000, granulated sugar (sucrose, starch syrup), talc; The pellet shell contains: hyprolose, magnesium stearate, triethyl citrate, ethylcellulose. Film shell composition: hypromellose, macrogol 6000, talc, titanium dioxide (E171). Metoprolol tartrate 100 mg Excipients: colloidal anhydrous silicon dioxide, magnesium stearate, microcrystalline cellulose; pellets contain: macrogol 6000, granulated sugar (sucrose, starch syrup), talc; The pellet shell contains: hyprolose, magnesium stearate, triethyl citrate, ethylcellulose. Film shell composition: hypromellose, macrogol 6000, talc, titanium dioxide (E171). Metoprolol tartrate 100 mg Excipients: microcrystalline cellulose, sodium carboxymethyl starch, colloidal anhydrous silicon dioxide, povidone, magnesium stearate. Metoprolol tartrate 100 mg Excipients: microcrystalline cellulose, sodium carboxymethyl starch, colloidal anhydrous silicon dioxide, povidone, magnesium stearate. Metoprolol tartrate 25 mg Excipients: microcrystalline cellulose, sodium carboxymethyl starch, colloidal anhydrous silicon dioxide, povidone, magnesium stearate. Metoprolol tartrate 50 mg Excipients: colloidal anhydrous silicon dioxide, magnesium stearate, microcrystalline cellulose; pellets contain: macrogol 6000, granulated sugar (sucrose, starch syrup), talc; The pellet shell contains: hyprolose, magnesium stearate, triethyl citrate, ethylcellulose. Film shell composition: hypromellose, macrogol 6000, talc, titanium dioxide (E171). Metoprolol tartrate 50 mg Excipients: microcrystalline cellulose, sodium carboxymethyl starch, colloidal anhydrous silicon dioxide, povidone, magnesium stearate.

Egilok indications for use

• - arterial hypertension (in monotherapy or, if necessary, in combination with other antihypertensive drugs); - chronic heart failure in the compensation stage (in combination with standard diuretic therapy, ACE inhibitors, cardiac glycosides); - IHD (secondary prevention of myocardial infarction - as part of complex therapy; prevention of angina attacks); - prevention of cardiac arrhythmias, especially supraventricular tachycardia and ventricular tachycardia caused by adrenergic-dependent prolongation of the QT interval; - hyperkinetic cardiac syndrome; - hyperthyroidism (as part of complex therapy); - prevention of migraine attacks.

Egilok contraindications

• - cardiogenic shock; - AV block of II and III degrees; - sinoatrial block; - SSSU; - severe bradycardia (HR

Egilok dosage

• 100 mg 100 mg 25 mg 25 mg, 50 mg, 100 mg 50 mg 50 mg, 100 mg

Egilok side effects

• 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 at therapeutic use metoprolol. In some cases, the connection between an adverse event and the use of the drug has not been reliably established. Frequency parameters listed below side effects defined as follows: very often: 10%, often: 1-9.9%, infrequently: 0.1-0.9%, rarely: 0.01-0.09%, very rarely (including individual reports): 0 .01%. 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 outside of cardio-vascular 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, first degree atrioventricular block; 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.

Drug interactions

The antihypertensive effects of Egilok® and 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 blockers of “slow” calcium channels such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. Should be avoided intravenous administration calcium channel blockers such as verapamil in patients receiving beta-blockers. Caution should be exercised when taken simultaneously with the following drugs: Oral antiarrhythmic drugs (such as quinidine and amiodarone) - risk of bradycardia, atrioventricular block. Cardiac glycosides (risk of 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) 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 acting on the central nervous system, for example: sleeping pills, 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). Beta2-sympathomimetics (functional antagonism). Nonsteroidal anti-inflammatory drugs (for example, 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 (for example: eye drops) or monoamine oxidase inhibitors requires close medical supervision.

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, arterial hypotension, arrhythmia, ventricular extrasystole, bronchospasm, fainting; in case of acute overdose - cardiogenic shock, loss of consciousness, coma, cardiac arrest. cardialgia.

Storage conditions

• store at room temperature 15-25 degrees
• keep away from children

Information provided by the State Register of Medicines.

Synonyms

• Betaloc, Vasocardin, Corvitol, Metocard, Metolol, Metoprolol, Emzok