Recommendations for the use of Egilok. What helps Egilok? Instructions for use

Latin name: Egilok S

ATX Code: C07AB02

Active substance: metoprolol (Metoprolol)

Producer: Intas Pharmaceuticals, Ltd. (Intas Pharmaceuticals, Ltd.) (India)

Description and photo update: 30.11.2018

For people suffering high blood pressure, usually there is no question: "Egilok" - what are these pills from? The tool is in the first aid kit of most hypertensive patients, as it is effective, but it is inexpensive (one package is about a hundred rubles, specific figures depend on the characteristics of the release). The drug is made on the basis of metoprolol. "Egilok" is used for pressure in other diseases of the vessels, the heart, helping to alleviate the patient's condition. The drug is available in tablet form and is intended for oral administration. It can only be safe to use it in accordance with the instructions for use and in clear coordination of the therapeutic program with the attending physician. The medication is quite strong, so doctors strongly recommend to refrain from self-medication. The instruction to "Egilok" also reminds of this.

Caution is the key to effective therapy

As the saying goes folk wisdom, with the right dose, even poison becomes an indispensable medicine, and the most useful and harmless substance in excess threatens a person with death. When it comes to medical preparations, this wisdom is of particular importance, since excessive (as well as insufficient) intake of the drug into the body may either not improve the patient's condition, or aggravate it. Before use, it will not be superfluous to carefully read the instructions for "Egilok". Even if the attending doctor explained in detail how to use the drug.

"Egilok" is designed for people suffering from high blood pressure, which means that it has a rather strong effect on the functioning of blood vessels, the heart muscle. Not only the state of health of the patient, but also his very life often depends on the correct use of the medication.

How it works?

As can be seen from the instructions, "Egilok" reduces pressure, bringing it to normal levels. The drug fights arrhythmia, normalizes the heart rhythm, normalizes muscle contractions, and also stabilizes the sequence of contractions and excitations. Due to the slowing of the conduction of impulses, the excitability of the heart muscle decreases, which leads to a decrease in the frequency of contractions. Speaking about how much Egilok works, doctors usually mention an hour and a half - it is during this time period that the activity of the drug reaches its peak, after which it remains for some more time.

The predominant part of the substance that enters the body is completely processed in the liver. Here is the accumulation of metabolic products. Five percent leave the body through the urinary system.

What's on sale?

Reviews of "Egilok" contain references to three types of funds. People treat drugs differently. Medicines are on sale under the trade names "Egilok", "Egilok S", "Egilok Retard". Distinctive feature- composition, although basic active ingredient all three drugs are the same. "Egilok", "Egilok Retard" are made using metoprolol tartrate, but the third variety is based on a compound of the same metoprolol, but called succinate. In addition, each tablet contains auxiliary components that simplify absorption. medicinal product and increase its activity.

In the basic "Egilok" cellulose and silicon dioxide, several other compounds are used as additional compounds. "Egilok Retard" is made with inclusions of magnesium stearate and molasses, talc. Finally, the third option, that is, "Egilok C", contains, among others, stearic acid and several varieties of cellulose, glycerol. When choosing a specific drug, you need to be guided not only by the question "what are these pills from." "Egilok" effectively eliminates pressure, but individual intolerance to any component is possible, prohibiting the use of the agent in question. If, when studying the composition, the patient discovered a substance that his body does not tolerate, it is urgent to notify the doctor about this and select an effective replacement.

When to apply?

Indications "Egilok": arterial hypertension, also known as hypertension. Since regular use of the drug reduces and normalizes arterial pressure, he becomes a permanent inhabitant of the hypertensive first aid kit. The drug can be used as a prophylactic to prevent myocardial infarction. Such use is reasonable if the person belongs to a risk group for pathology.

In some cases, as can be seen from the reviews, "Egilok" is prescribed for migraine, as the remedy prevents headache attacks and reduces their frequency. All of the above indications apply to the three previously mentioned types of medication.

Features of use

"Egilok", "Egilok Retard" are effective in hyperthyroidism, with increased activity heart muscle. The tool is used as part of complex therapy to combat the disease. "Egilok", "Egilok S" are effective in supraventricular arrhythmias. Forms of release "C", "Retard" are relevant if there is a failure of the functioning of the heart muscle in a chronic form. The tool is also used as one of the elements in integrated approach to solving the problem.

Since it is necessary to use the described component together with other drugs to prevent complications, exacerbations, as well as eliminate the symptoms of chronic diseases of the heart and blood vessels, the issue of compatibility is especially acute. "Egilok" enhances the effectiveness of some groups of drugs and is not combined with others. In complex therapy, this group of drugs is usually used together with diuretics, while the pressure drug activates diuretics. PAF inhibitors can be used. A common approach is to combine the drug and glycosides to support the work of the cardiovascular system. But "Egilok" and alcohol categorically do not combine. Therefore, with problems with pressure, it is necessary to refrain from alcoholic beverages even in small doses. With diagnosed heart failure acute form, associated with problems in the functioning of the ventricle on the left, Egilok C gives the greatest efficiency in combination with the above groups of medicines.

Prevention is the best cure

Reviews of "Egilok" demonstrate that the drug is often used as a prophylactic. Known for its effectiveness in the program for the prevention of extrasystoles. In addition, "Egilok C" gives good results in myocardial infarction. The drug can be used even on late stage, thereby reducing the likelihood fatality. At correct application"Egilok S" allows you to leave in the past tachycardia, problems of the functioning of the heart muscle.

Release Features

The composition of "Egilok" can be found in the instructions for use. This information is always contained on the leaflet in the carton with blisters in which the tablets are packed. The main active components of all three forms of release are indicated earlier, the effectiveness of the agent is due to the presence of metoprolol in it in the form of derivatives.

Reviews of "Egilok" contain a mention that the tool usually has a convex shape on both sides. Only type "C" is usually oblong. The color is always white. One tablet contains the active ingredient in the amount of 25 mg, 50 mg, 100 mg. An indication of this is on the packaging of the drug. Also on sale is "Egilok Retard" with a content of the main active ingredient of 200 mg. The pack contains 30 tablets or twice as many.

When not?

Egilok's contraindications are a fairly extensive list, and all of them must be strictly observed, since the drug has strong influence to the heart muscle. First of all, a ban on the use establishes bradycardia, that is, a slow rhythm of contraction of the heart muscle. If the frequency of contractions decreases to 50-60 per minute, "Egilok" is not applicable.

"Egilok" can not be used with a weak sinus node, sinoatrial blockade. The drug is not applicable for problems with peripheral circulation. The drug should not be used with chronically low blood pressure. The use of Egilok is associated with a certain health hazard if there is a possibility of an allergic reaction. During pregnancy, the use of the described drug must be agreed with the attending physician. There is a possibility of a negative effect on the fetus, so the drug can be used only if the benefit from its use is significantly higher than the risk. If any contraindications are identified, the doctor decides to replace the drug or adjust the dosage of Egilok. You cannot change anything in the program on your own, you must urgently seek advice from a specialist.

How to be treated?

"Egilok" is intended for oral use. The drug is used for violations in the work of the heart and blood vessels on the recommendation of the attending doctor. The dosage, the scheme of application is also determined by the doctor, focusing on the diagnosis of the patient, accompanying illnesses and other drugs in the therapy program. Below are several options for using Egilok for common diseases. Please note: these are standard programs recommended by the manufacturer, but you cannot prescribe a medication for yourself according to these schemes, you must first undergo a doctor's examination to identify all significant factors.

With arterial hypertension, Egilok is used twice a day, usually in the evening, in the morning. The dosage of the drug is from 25 mg or more. With insufficient effectiveness, the dose is increased to 100 mg per 24 hours. Arrhythmia is treated similarly, the same program is used for angina pectoris. Sometimes the remedy is used three times a day, at a time taking from 25 mg or more. In the absence of a positive effect, the dose is increased to 100 mg, divided into two doses in 24 hours.

Drug programs: what else is there?

When using an agent for the prevention of a heart attack, Egilok is taken every day in an amount of 50 mg (if necessary, the dose is doubled).

If it was detected vegetovascular dystonia if panic attacks are diagnosed that provoked a violation of the rhythm of the heartbeat, "Egilok" is used in a standard amount, that is, 50 mg. In the absence of a pronounced effect, the amount of the drug is doubled. It is assumed that "Egilok" is drunk twice a day. In the prevention of migraine, the agent is used in the same way.

Overdose: what to do?

When exceeding allowable dose"Egilok" quite strongly affects the cardiovascular system. Bradycardia develops, dizziness, the patient feels sick. There is a high probability of hypotension, fainting, extrasystole. The rhythm of the heartbeat may be disturbed. In the most severe situations, cardiogenic shock develops, leading to loss of consciousness, up to coma. In rare cases, an overdose provokes cardialgia, atrioventricular blockade. In the absence of help, there is a chance of a complete stop of the heartbeat. Pronounced overdose symptoms appear half an hour or several hours (up to two) after the drug enters the patient's body.

In case of an overdose, it is urgent to wash the stomach, take activated charcoal and symptomatic therapy to eliminate the primary manifestations of the effect of the drug on the body. With a sharp decrease in pressure, the patient is placed in such a way that the level of the head is below the level of the hips. With bradycardia, acute hypotension, with insufficient functioning of the heart muscle, an urgent intake of beta-agonists and a number of specific medications is necessary. In the absence of a quick effect, they resort to drugs containing dopamine, dobutamine. In some cases, the effectiveness shows the use of from a gram to ten grams of glucagon. Depending on the symptoms, diazepam, beta-2-agonists, and an intracardiac electrical stimulator may help. As clinical studies have shown, it is impossible to remove excess drug from the body by hemodialysis.

"Egilok": side effects

And that's not it. Some patients (and this is confirmed by reviews on the World Wide Web) when taking Egilok more often feel tired, others complain of increased excitability. Sometimes there is a feeling of anxiety, a depressed state, there are difficulties with concentration. There is a possibility of headaches, the head may be spinning.

"Egilok" in rare cases provokes sleep disorders - nightmares, insomnia or drowsiness. Clinical studies have shown that taking the medication can adversely affect cognitive abilities (first of all, memory suffers), general state becomes depressed. With an extremely low probability (and yet it exists), hallucinations, paresthesia, convulsive states. The reviews on the Internet contain references to weight gain with the systematic treatment of Egilok. Laboratory tests may show an increase in the concentration of bilirubin in the blood. There may be problems with the gastrointestinal tract, stool, decreased visual acuity. As revealed during official drug trials, side effects accompany the drug is quite rare, most patients tolerate the drug well. This is also evidenced by the reviews of doctors and patients.

"Egilok": analogues

If an individual intolerance to the drug is detected, it can be replaced with another, similar medication. Be sure to coordinate the replacement with your doctor. Most often, the reason for adjusting the prescribed drug is allergic reaction. There are quite a lot of drugs for hypertension in pharmacies, so there is plenty to choose from. Most often prescribed:

• "Metoprolol";
• "Metocard";
• "Metozok".

When studying analogues of Egilok, it is necessary to be guided, first of all, by efficiency, health benefits, and only then evaluate the cost. The drug is relatively inexpensive (from a hundred rubles per pack), therefore, just for the sake of economy, it is categorically not recommended to replace it with cheaper drugs. Diseases of the heart and vascular system are dangerous not only for everyday activity, but also for life, which requires you to treat the issue very responsibly and coordinate all adjustments to the therapeutic program with your doctor.

Responsibility as an aspect of successful treatment

High blood pressure is always a danger, even if the disease is not chronic, but only manifests itself from time to time. Often, hypertension is accompanied by other health disorders, which in combination creates a danger to human life. This obliges you to take your health with the utmost responsibility. As a rule, the described drug is chosen by people to whom the attending doctor advised him. If you are going to take the remedy, you need to be prepared for the possible side effects indicated in the instructions (they are listed above). If we systematize the information collected from reviews of the drug, we can see that of the most unpleasant and strong phenomena that occur relatively often, people were bothered by problems with the stool.

Feedback on Egilok from experts is mostly positive, since the drug effectively fights the main problem, is inexpensive and accessible to most people. At correct use interruptions in the work of the heart muscle are a thing of the past, pressure is stabilizing. True, Egilok gives a good result only when it really suits the patient. You can’t experiment on yourself, and it won’t work: the drug is dispensed from pharmacies strictly with a prescription from the attending physician.

Hypertension: the first signs

The sooner the treatment of the disease is started, the less blood can be dispensed with, figuratively speaking. When should I go to the doctor, when is it reasonable to start taking Egilok? The first symptoms of hypertension are often ignored - people simply cannot appreciate the full significance of what is happening. As a rule, at the beginning, the disease marks itself with an increase in irritability, frequent dizziness and a state of fatigue. Over time, pressure provokes memory impairment, headaches and weakness.

Noticing such manifestations in yourself, it is necessary to introduce a clear control over the level of blood pressure as a rule. By conducting statistics over a relatively long time period (weeks or even months), you can identify how often the indicators go beyond the norm (120/80), how strong the deviations are. With this information, you can seek help from a doctor.

Egilok (active substance metoprolol) is a popular Hungarian selective beta-1-blocker without its own sympathomimetic activity. It has antihypertensive, antianginal (anti-ischemic) and antiarrhythmic effects. It suppresses the automatism of the pacemaker of the first order, reduces the heart rate, slows down atrioventricular conduction, reduces the excitability and contractility of the heart muscle, reduces cardiac output, reduces the heart's need for oxygen. Reduces the stimulating effect of catecholamine neurotransmitters on the heart during physical and psycho-emotional stress. The antihypertensive effect of Egilok stabilizes by the end of the second week. medication course. With angina pectoris, the drug reduces the frequency and severity of attacks. In case of myocardial infarction, Egilok limits the area of ​​ischemic damage, reduces the risk of developing life-threatening arrhythmias and the likelihood of recurrent myocardial infarction. When used in moderate doses, less than non-selective beta-blockers, affects smooth muscle bronchial tree and peripheral arteries. After oral administration, Egilok is rapidly and completely absorbed from the gastrointestinal tract. Maximum concentration active substance in the blood is noted after 1-2 hours. The plasma half-life is 3-4 hours.

Egilok is available in tablets. The recommended daily dose of the drug is 100 mg for 1-2 doses with the possibility of a gradual increase to 200 mg. The maximum daily dose should not exceed 400 mg. The drug is very well researched, incl. Russian scientists. So, in one of the studies, domestic cardiologists studied the effectiveness of egilok in the treatment of arterial hypertension in patients with diabetes mellitus. The relevance of this issue is due to the fact that about 70% of patients suffering from non-insulin-dependent diabetes mellitus die from certain cardiovascular complications, and strict control of blood pressure can significantly reduce mortality rates even to a greater extent than glycemic control.

The feasibility of using beta-blockers in such patients has been questioned for a long time. It was believed that they significantly increase the risk of hypoglycemia, hide its signs, slow down the rate of recovery of glucose concentration after a hypoglycemic episode and worsen the lipid profile. As it turned out, such fears were unfounded. Returning to the above study, it should be noted that systolic and diastolic blood pressure decreased in both groups, however, in the diabetic group, this decrease was more pronounced. In addition, therapy with Egilok led to a decrease in the level of total and "bad" cholesterol, triglycerides and had virtually no effect on carbohydrate metabolism. Another study examined the effectiveness of the drug in coronary heart disease. A number of clinicians have complained that some antianginal agents can effectively relieve pain, while providing only a slight anti-ischemic effect. This can mask the danger signal that the heart attacked by ischemia (so-called painless ischemia) gives. The study involved patients with angina pectoris. As a result of treatment with Egilok, the frequency of angina attacks decreased by half. Confirmation of the anti-ischemic activity of the drug is the improvement of exercise tolerance. Beta-blockers and, in particular, egilok are used not only with therapeutic, but also with preventive purpose, including the prevention of ischemic complications in postinfarction patients. The drug can also be used to treat patients suffering from ischemic heart disease in combination with broncho-obstructive syndrome, which in itself is a contraindication to the use of beta-blockers.

Pharmacology

Cardioselective beta 1 -blocker without internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects. Reduces the automatism of the sinus node, reduces heart rate, slows down AV conduction, reduces myocardial contractility and excitability, reduces cardiac output, reduces myocardial oxygen demand. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.

It causes a hypotensive effect, which stabilizes by the end of the 2nd week of course use. In angina pectoris, metoprolol reduces the frequency and severity of attacks. Normalizes the heart rhythm with supraventricular tachycardia and atrial fibrillation. In myocardial infarction, it helps to limit the zone of ischemia of the heart muscle and reduces the risk of developing fatal arrhythmias, reduces the possibility of recurrence of myocardial infarction. When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.

Pharmacokinetics

After oral administration, metoprolol is rapidly and almost completely absorbed from the gastrointestinal tract, Cmax of the active substance in the blood plasma is reached after 1-2 hours. After absorption, metoprolol is largely subjected to the "first pass" effect through the liver. It is intensively metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system with the formation of non-active metabolites. T 1/2 of metoprolol from plasma is 3-4 hours and does not change during the course of treatment. More than 95% of the dose taken is excreted by the kidneys, of which only 3% is unchanged.

Release form

Tablets white or almost white, round, biconvex, with a cross-shaped dividing line and a double bevel on one side and engraved "E435" on the other side, odorless.

Excipients: microcrystalline cellulose, sodium starch glycolate, anhydrous colloidal silicon dioxide, povidone K90, magnesium stearate.

30 pcs. - jars of dark glass (1) - packs of cardboard.
60 pcs. - jars of dark glass (1) - packs of cardboard.

Dosage

When taken orally, the average dose is 100 mg / day in 1-2 doses. If necessary, the daily dose is gradually increased to 200 mg. With a / in the introduction of a single dose - 2-5 mg; with no effect reintroduction maybe in 5 minutes.

Maximum doses: when taken orally, the daily dose is 400 mg; when administered intravenously, a single dose is 15-20 mg.

Interaction

With simultaneous use with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of developing severe arterial hypotension, bradycardia, AV blockade.

With simultaneous use with barbiturates, the metabolism of metoprolol is accelerated, which leads to a decrease in its effectiveness.

With simultaneous use with hypoglycemic agents, it is possible to enhance the effect of hypoglycemic agents.

With simultaneous use with NSAIDs, it is possible to reduce the hypotensive effect of metoprolol.

With simultaneous use with opioid analgesics, the cardiodepressive effect is mutually enhanced.

With simultaneous use with peripheral muscle relaxants, it is possible to increase the neuromuscular blockade.

With simultaneous use with means for inhalation anesthesia, the risk of inhibition of myocardial function and the development of arterial hypotension increases.

With simultaneous use with oral contraceptives, hydralazine, ranitidine, cimetidine, the concentration of metoprolol in the blood plasma increases.

With simultaneous use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.

With simultaneous use with verapamil, Cmax in blood plasma and AUC of metoprolol increase. The minute and stroke volume of the heart, pulse rate, and arterial hypotension decrease. Perhaps the development of heart failure, dyspnea and blockade of the sinus node.

With intravenous administration of verapamil while taking metoprolol, there is a risk of cardiac arrest.

With simultaneous use, it is possible to increase bradycardia caused by digitalis glycosides.

With simultaneous use with dextropropoxyphene, the bioavailability of metoprolol increases.

With simultaneous use with diazepam, a decrease in clearance and an increase in the AUC of diazepam are possible, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions.

With simultaneous use with diltiazem, the concentration of metoprolol in the blood plasma increases due to inhibition of its metabolism under the influence of diltiazem. The effect on the activity of the heart is additively suppressed due to the slowing down of the impulse through the AV node caused by diltiazem. There is a risk of developing severe bradycardia, a significant decrease in stroke and minute volume.

With simultaneous use with lidocaine, a violation of the excretion of lidocaine is possible.

With simultaneous use with mibefradil in patients with low activity of the CYP2D6 isoenzyme, an increase in the concentration of metoprolol in the blood plasma and an increase in the risk of developing toxic effects are possible.

With simultaneous use with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form eye drops or as part of antitussives), some increase in blood pressure is possible.

With simultaneous use with propafenone, the concentration of metoprolol in the blood plasma increases and develops toxic effect. It is believed that propafenone inhibits the metabolism of metoprolol in the liver, reducing its clearance and increasing serum concentrations.

With simultaneous use with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop.

With simultaneous use with rifampicin, the concentration of metoprolol in the blood plasma decreases.

Metoprolol may cause a slight decrease in the clearance of theophylline in smoking patients.

Fluoxetine inhibits the CYP2D6 isoenzyme, which leads to inhibition of the metabolism of metoprolol and its accumulation, which can enhance the cardiodepressive effect and cause bradycardia. A case of lethargy development is described.

Fluoxetine and mainly its metabolites are characterized by a long half-life, so the possibility of drug interaction persists even several days after fluoxetine is discontinued.

There are reports of a decrease in the clearance of metoprolol from the body when used simultaneously with ciprofloxacin.

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

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

With simultaneous use, metoprolol increases the concentration of ethanol in the blood and prolongs its excretion.

Side effects

From the side of the cardiovascular system: possible bradycardia, arterial hypotension, AV conduction disturbances, the appearance of symptoms of heart failure.

From the digestive system: at the beginning of therapy, dry mouth, nausea, vomiting, diarrhea, constipation are possible; in individual cases- Liver dysfunction.

From the side of the central nervous system and peripheral nervous system: at the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, a feeling of cold and paresthesia in the extremities are possible; possible decrease in the secretion of lacrimal fluid, conjunctivitis, rhinitis, depression, sleep disturbances, nightmares.

From the hemopoietic system: in some cases - thrombocytopenia.

From the endocrine system: hypoglycemic conditions in patients with diabetes mellitus.

From the respiratory system: in predisposed patients, symptoms of bronchial obstruction may appear.

Allergic reactions: skin rash, itching.

Indications

Arterial hypertension, prevention of angina attacks, cardiac arrhythmias (supraventricular tachycardia, extrasystole), secondary prevention after myocardial infarction, hyperkinetic cardiac syndrome (including with hyperthyroidism, NCD). Prevention of migraine attacks.

Contraindications

II and III degree AV blockade, sinoatrial blockade, bradycardia (heart rate less than 50 bpm), SSS, arterial hypotension, stage IIB-III chronic heart failure, acute heart failure, cardiogenic shock, metabolic acidosis, severe peripheral circulatory disorders, hypersensitivity to metoprolol.

Application features

Use during pregnancy and lactation

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. Metoprolol crosses the placental barrier. Due to the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory arrest in a newborn, metoprolol must be canceled 48-72 hours before the planned delivery date. After delivery, it is necessary to ensure strict control over the condition of the newborn for 48-72 hours.

Metoprolol is excreted in breast milk in small amounts. Use during lactation is not recommended.

Application for violations of liver function

Application for violations of kidney function

special instructions

Use with caution in patients with chronic obstructive airways disease, diabetes mellitus (especially with a labile course), Raynaud's disease and obliterating diseases of peripheral arteries, pheochromocytoma (should be used in combination with alpha-blockers), severe renal and hepatic dysfunction.

Against the background of treatment with metoprolol, a decrease in the production of lacrimal fluid is possible, which is important for patients using contact lenses.

Completion of a long course of treatment with metoprolol should be carried out gradually (at least within 10 days) under the supervision of a physician.

At combination therapy with clonidine, the latter should be discontinued a few days after the abolition of metoprolol, in order to avoid a hypertensive crisis. With simultaneous use with hypoglycemic agents, correction of their dosing regimen is required.

A few days before anesthesia, it is necessary to stop taking metoprolol or choose an anesthetic agent with a minimal negative inotropic effect.

Influence on the ability to drive vehicles and control mechanisms

In patients whose activities require increased attention, the question of the use of metoprolol on an outpatient basis should be decided only after an assessment of the patient's individual response.

Registration number: P No. 015639/01 03/17/2009

Trade name: Egilok ®

International generic name: metoprolol

PHARMACOLOGICAL PROPERTIES

Mechanism of action:

Metoprolol suppresses the effect of increased activity of the sympathetic system on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.

At arterial hypertension metoprolol lowers blood pressure in patients in the standing and lying positions. The long-term antihypertensive effect of the drug is associated with a gradual decrease in total peripheral vascular resistance. With arterial hypertension long-term use the drug leads to a statistically significant decrease in the mass of the left ventricle and improve its diastolic function. In men with mild to moderate hypertension, metoprolol reduces mortality from cardiovascular causes(primarily sudden death, fatal and non-fatal heart attack and stroke).

Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic arterial pressure, heart rate and myocardial contractility. A decrease in heart rate and a corresponding lengthening of diastole when taking metoprolol provide improved blood supply and oxygen uptake by the myocardium with impaired blood flow. Therefore, in angina pectoris, the drug reduces the number, duration and severity of attacks, as well as asymptomatic manifestations of ischemia, and improves the patient's physical performance. In myocardial infarction, metoprolol reduces the mortality rate, reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A decrease in mortality can also be observed with the use of metoprolol in both the early and late phases of myocardial infarction, as well as in high-risk patients and patients with diabetes mellitus. The use of the drug after myocardial infarction reduces the likelihood of non-fatal re-infarction. In chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken starting from low doses (2x5 mg / day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.

With supraventricular tachycardia, atrial fibrillation and ventricular premature beats, metoprolol reduces the frequency of ventricular contractions and the number of ventricular extrasystoles.

At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than the same effects of non-selective beta-blockers.

Compared with non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism. It does not increase the duration of hypoglycemic episodes.

Metoprolol causes a slight increase in the concentration of triglycerides and a slight decrease in the concentration of free fatty acids in blood serum. There is a significant decrease in the total concentration of serum cholesterol after several years of taking metoprolol.

Metoprolol is rapidly and completely absorbed into gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range. The maximum plasma concentration is reached 1.5-2 hours after ingestion. After absorption, metoprolol is largely metabolized by the primary passage through the liver. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with regular administration.

Reception simultaneously with food can increase the bioavailability of metoprolol by 30-40%. Metoprolol is slightly (~ 5-10%) bound to plasma proteins. The volume of distribution is 5.6 l/kg.

Metoprolol is metabolized in the liver by cytochrome P-450 isoenzymes. Metabolites do not have pharmacological activity.

Half-life (t 1/2) an average of 3.5 hours (from 1 to 9 hours). The total clearance is approximately 1 l / min.

Approximately 95% of the administered dose is excreted by the kidneys, 5% in the form of unchanged metoprolol. In some cases, this value can reach 30%.

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

Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases, there is a decrease in the excretion of metabolites. In severe renal failure (glomerular filtration rate less than 5 ml / min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade.

Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after a porto-caval shunt, bioavailability may increase and total clearance from the body may decrease. After porto-caval shunting, the total clearance of the drug from the body is approximately 0.3 l / min, and the area under the concentration-time curve increases by approximately 6 times compared with that in healthy volunteers.

Arterial hypertension (in monotherapy or (if necessary) in combination with other antihypertensive drugs); functional disorders of cardiac activity, accompanied by tachycardia.

Ischemic heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks.

Heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole). Hyperthyroidism (complex therapy). Prevention of migraine attacks.

Hypersensitivity to metoprolol or any other component of the drug, as well as other beta-blockers; atrioventricular block (AV) II or III degree; sinoatrial blockade; sinus bradycardia (heart rate less than 50/min), sick sinus syndrome; cardiogenic shock; severe disorders of peripheral circulation; heart failure in the stage of decompensation, age up to 18 years (due to the lack of sufficient clinical data), simultaneous intravenous administration of verapamil, severe bronchial asthma and pheochromocytoma without the simultaneous use of alpha-blockers.

Due to the lack of clinical data, Egioloc ® is contraindicated in acute infarction myocardium, accompanied by a heart rate below 45 beats / min, with a PQ interval of more than 240 ms, and systolic blood pressure below 100 mm Hg.

Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (COPD), renal / hepatic failure, myasthenia gravis, pheochromocytoma (when used simultaneously with alpha-blockers), thyrotoxicosis, AV blockade of the 1st degree, depression (including in history), psoriasis, obliterating peripheral vascular disease ("intermittent" claudication, Raynaud's syndrome), pregnancy, lactation, old age, in patients with aggravated allergic history(possibly decreased response with adrenaline).

USE IN PREGNANCY AND LACTATION

The use of the drug is not recommended during pregnancy. The use of the drug is possible only if the benefit to the mother outweighs the potential risk to the fetus. If the drug is necessary, you should carefully monitor the fetus, and then the newborn for several days (48 - 72 hours) after birth, as bradycardia, respiratory depression, lowering blood pressure and hypoglycemia may develop.

Despite the fact that when taking therapeutic doses of metoprolol, only small amounts of the drug are released into breast milk, the newborn should be kept under observation (possible bradycardia). The use of the drug during lactation is not recommended. If necessary, the use of the drug during lactation is recommended to stop breastfeeding.

METHOD OF APPLICATION AND DOSES

Egilok ® tablets are taken orally. Tablets can be taken with or without food. If necessary, the tablet can be broken in half. The dose should be adjusted gradually and individually to avoid excessive bradycardia. The maximum daily dose is 200 mg. Recommended doses:

Arterial hypertension

With mild or moderate arterial hypertension, the initial dose is 25-50 mg twice a day (morning and evening). If necessary, the daily dose can be gradually increased to 100-200 mg / day or another antihypertensive agent can be added.

angina pectoris

Initial dose of 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.

Supportive care after myocardial infarction

The usual daily dose - 100 - 200 mg / day, divided into two doses (morning and evening).

Heart rhythm disorders

The initial dose is 25 to 50 mg two or three times a day. If necessary, the daily dose can be gradually increased to 200 mg / day or another antiarrhythmic agent can be added. Hyperthyroidism

The usual daily dose is 150-200 mg per day for 3-4 doses.

Functional disorders of the heart, accompanied by a sensation of palpitations The usual daily dose is 50 mg 2 times a day (morning and evening); if necessary, it can be increased to 200 mg in two divided doses.

Prevention of migraine attacks

The usual daily dose is 100 mg/day in two divided doses (morning and evening); if necessary, it can be increased to 200 mg / day in 2 divided doses.

Special patient groups

In case of impaired renal function, a change in the dosing regimen is not required.

With cirrhosis of the liver, a dose change is usually not required due to the low binding of metoprolol to plasma proteins (5-10%). In severe hepatic insufficiency (for example, after portocaval bypass surgery), it may be necessary to reduce the dose of Egilok ® .

In elderly patients, dose adjustment is not required.

Egilok ® is usually well tolerated by patients. Side effects are usually mild and reversible. The side effects listed below have been reported in clinical trials and in the therapeutic use of metoprolol. In some cases, the relationship of an adverse event with the use of the drug has not been reliably established. The frequency parameters listed below are defined as follows: very often: > 10%), often: 1-9.9%, infrequently: 0.1-0.9%, rarely: 0.01-0.09%, very rarely (including isolated reports):< 0,01 %.

From the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - hyperexcitability, anxiety, impotence/sexual dysfunction; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, "nightmare" dreams; very rarely - amnesia / memory impairment, depression, hallucinations.

From the side of the cardiovascular system: often - bradycardia, orthostatic hypotension (in some cases, syncope is possible), coldness of the lower extremities, palpitations; infrequently - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, atrioventricular block I degree; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders). From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function.

On the part of the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of the course of psoriasis. From the respiratory system: often - shortness of breath during physical effort; infrequently - bronchospasm in patients with bronchial asthma; rarely - rhinitis.

From the sensory organs: rarely - blurred vision, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, a violation of taste sensations. Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia. Egilok ® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably established.

Symptoms: pronounced decrease in blood pressure, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase with the simultaneous use of ethanol, antihypertensive drugs, quinidine and barbiturates.
The first symptoms of an overdose appear 20 minutes -2 hours after taking the drug.

Treatment: it is necessary to carefully monitor the patient (control of blood pressure, heart rate, respiratory rate, kidney function, blood glucose concentration, blood serum electrolytes) in the conditions of the department intensive care. 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 - in / in, with an interval of 2-5 minutes, beta-agonists - until the desired effect is achieved or in / in 0.5-2 mg of atropine. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine). With hypoglycemia - the introduction of 1-10 mg of glucagon, the installation of a temporary pacemaker. With bronchospasm, beta2-agonists should be administered. With convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.

INTERACTIONS WITH OTHER DRUGS

The antihypertensive effects of the drug Egilok ® and other antihypertensive drugs are usually enhanced. In order to avoid arterial hypotension, careful monitoring of patients receiving combinations of such agents is necessary. However, the summation of the effects of antihypertensive drugs can be used if necessary to achieve effective control of blood pressure.

The simultaneous use of metoprolol and blockers of "slow" calcium channels such as diltiazem and verapamil can lead to an increase in negative inotropic and chronotropic effects. The intravenous administration of calcium channel blockers such as verapamil should be avoided in patients receiving beta-blockers.

Caution should be exercised when taken concomitantly with the following agents:

Oral antiarrhythmic drugs (such as quinidine and amiodarone) - the risk of bradycardia, atrioventricular 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 reception metoprolol and clonidine should always be started, canceling metoprolol, and then (after a few days) clonidine; if clonidine is discontinued first, a hypertensive crisis may develop.

Some drugs that act on the central nervous system, for example: sleeping pills, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol increase the risk of arterial hypotension. Means for anesthesia (risk of oppression of cardiac activity).

Alpha- and beta-sympathomimetics (risk of arterial hypertension, significant bradycardia; possibility of cardiac arrest). Ergotamine (increased vasoconstrictor effect). Beta-2 sympathomimetics (functional antagonism).

Non-steroidal anti-inflammatory drugs (eg, indomethacin) - may weaken the antihypertensive effect.

Estrogens (may reduce the antihypertensive effect of metoprolol). Oral hypoglycemic agents and insulin (metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia). Curare-like muscle relaxants (increased neuromuscular blockade). Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline) - an increase in the effects of metoprolol due to an increase in its concentration in blood plasma. Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to an increase in hepatic metabolism.

The simultaneous use of sympathetic ganglion blockers or other beta-blockers (for example: eye drops) or monoamine oxidase inhibitors requires careful medical supervision.

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 instruct about the need for medical advice if the heart rate is less than 50 beats / min. When taking a dose above 200 mg per day, cardioselectivity decreases.

In heart failure, treatment with Egilok ® is started only after reaching the stage of compensation of cardiac function.

Possible increased severity of reactions hypersensitivity and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline) in patients with a aggravated allergic history.

Anaphylactic shock may be more severe in patients taking Egilok ® . May exacerbate symptoms of peripheral arterial circulatory disorders. Avoid abrupt discontinuation of the drug Egilok ® . The drug should be discontinued gradually by reducing the dose over a period of approximately 14 days. Abrupt withdrawal may exacerbate angina symptoms and increase the risk of coronary disorders. Special attention when discontinuing the drug should be given to patients with coronary artery disease. In case of exertional angina, the selected dose of Egilok ® should provide heart rate at rest within 55-60 beats / min, with exercise - no more than 110 beats / min. Patients using contact lenses should take into account that against the background of treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible. Egilok may mask some of the clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal level. In the case of prescribing the drug Egilok ®, patients with diabetes mellitus should monitor the concentration of blood glucose and, if necessary, adjust the dose of insulin or hypoglycemic agents for oral administration (see section "Interaction with other drugs").

If it is necessary to prescribe to patients with bronchial asthma, beta2-agonists are prescribed as concomitant therapy; with pheochromocytoma - alpha-blockers.

If it is necessary to perform a surgical intervention, it is necessary to warn the surgeon / anesthesiologist about the therapy being carried out (the choice of a general anesthesia agent with a minimal negative inotropic effect), discontinuation of the drug is not recommended. Drugs that reduce catecholamine stores (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect excessive lowering of blood pressure or bradycardia.

In elderly patients, regular monitoring of liver function is recommended. Correction of the dosing regimen is required only if an elderly patient develops increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction sometimes it is necessary to stop treatment. Patients with severe renal insufficiency are advised to monitor renal function.

Special monitoring 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 stop therapy.

If progressive bradycardia occurs, the dose should be reduced or the drug should be discontinued.

Due to the lack of sufficient clinical data, the drug is not recommended for use in children.

Impact on ability to drive vehicles and sophisticated technology.

Care must be taken when driving and engaging in potentially dangerous species activities requiring increased concentration attention (risk of dizziness and increased fatigue).

Tablets 25 mg: 60 tablets in a brown glass bottle with a PE cap with an accordion shock absorber, with a first opening control. 1 bottle, together with instructions for use, is packed in a cardboard box. Or 20 tablets in a PVC/PVDC//al. foil. 3 blisters, together with instructions for use, are packed in a cardboard box.