Egilok S

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Latin name: Egilok S

ATX code: C07AB02

Active ingredient: metoprolol (Metoprolol)

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

Description and photo updated: 30.11.2018

Sustained-release tablets, film-coated, Egilok S

Egilok S is a beta ₁ -adrenergic blocker of selective action.

Release form and composition

Dosage form - tablets of prolonged action, film-coated: biconvex, oval, white, with a risk on both sides (10 pcs. In a blister, in a cardboard box of 3 or 10 blisters and instructions for use of Egilok C).

Composition of 1 tablet:

active substance: metoprolol succinate - 25, 50, 100 or 200 mg;
auxiliary components: ethylcellulose, methylcellulose, microcrystalline cellulose, glycerol, magnesium stearate, corn starch;
film casing: Sepifilm LP 770 white (hypromellose, titanium dioxide E171, stearic acid, microcrystalline cellulose).

Pharmacological properties

Pharmacodynamics

The active substance of Egilok C - metoprolol succinate, is a beta ₁ -adrenergic blocker, which is capable of blocking β ₁ -adrenergic receptors when used in significantly smaller doses than are required to block β ₂ -adrenergic receptors.

Egilok S has a slight membrane stabilizing activity, is not a partial agonist.

Metoprolol is able to reduce or suppress the agonistic effect exerted on cardiac activity by catecholamines, which are released during physical and nervous stress. This means that the drug can prevent an increase in the minute volume and heart rate (HR), an increase in heart contractility and an increase in blood pressure (BP) due to a sharp release of catecholamines.

Unlike conventional tableted selective beta ₁ -adrenoceptor blockers (including metoprolol tartrate), prolonged-release metoprolol succinate provides a constant plasma concentration of the drug and a stable clinical effect (beta _1- adrenergic blockade) for at least 24 hours. Due to the absence of significant maximum plasma concentrations of metoprolol succinate has a higher β ₁ -selectivity than conventional metoprolol tablet forms. In addition, Egilok S significantly reduces the potential risk of developing side effects that often occur at maximum plasma concentrations, for example, weakness in the legs when walking or bradycardia.

With concomitant obstructive pulmonary diseases, Egilok C can be prescribed in addition to beta ₂ -adrenomimetics. Metoprolol succinate has less effect on the bronchodilation caused by them compared to non-selective beta-blockers.

Metoprolol succinate less than non-selective beta-blockers, affects carbohydrate metabolism and insulin production, as well as the cardiovascular system in hypoglycemic conditions.

In case of arterial hypertension, Egilok S significantly reduces blood pressure, this effect persists for at least 24 hours, both in the supine and standing position, and during physical activity. At the beginning of the use of the drug, an increase in vascular resistance is observed. However, with prolonged use of metoprolol succinate, a decrease in blood pressure is possible due to a decrease in vascular resistance, while cardiac output does not change.

Pharmacokinetics

Each Egilok S tablet contains a large number of microgranules (pellets) coated with a polymer shell, due to which a controlled release of the active substance is carried out.

The effect of the drug comes on quickly. Once in the gastrointestinal tract (GIT), the tablets disintegrate into separate pellets, each of which acts separately, and together they provide a uniform release of metoprolol succinate for more than 20 hours. The release rate depends on the acidity of the gastric environment. Thus, the duration of action of Egilok C is more than 24 hours.

Metoprolol succinate is completely absorbed in the gastrointestinal tract. After taking a single dose, the systemic bioavailability is approximately 30-40%.

The substance is characterized by low binding to plasma proteins - 5-10%.

The drug is metabolized in the liver by oxidation to form three main metabolites, which do not have clinically significant activity. It is excreted mainly in the form of metabolites, only about 5% of the dose is eliminated unchanged by the kidneys.

The half-life of free metoprolol is ~ 3.5-7 hours.

Indications for use

stable chronic heart failure, accompanied by clinical manifestations (II – IV functional class according to NYHA classification) and impaired systolic function of the left ventricle (as an additional drug in the main therapy of chronic heart failure);
arterial hypertension;
cardiac arrhythmias, including supraventricular tachycardia, a decrease in the rate of ventricular contraction during ventricular extrasystoles and atrial fibrillation;
angina pectoris;
functional disorders of cardiac activity, accompanied by tachycardia;
reduction in the frequency of re-infarction and mortality after the acute phase of myocardial infarction;
prevention of migraine attacks.

Contraindications

Absolute:

arterial hypotension with systolic blood pressure <90 mm Hg. Art.;
sick sinus syndrome (SSS);
atrioventricular block II and III degree;
clinically significant sinus bradycardia with heart rate <50 beats / min;
decompensated heart failure;
PQ interval> 0.24 sec;
suspicion of acute myocardial infarction with heart rate <45 beats / min;
cardiogenic shock;
severe peripheral circulatory disorders with the threat of gangrene development;
pheochromocytoma (if alpha-blockers are not used at the same time);
age up to 18 years;
intravenous (iv) administration of slow calcium channel blockers such as verapamil;
simultaneous use of monoamine oxidase (MAO) inhibitors (with the exception of type B);
long-term or course use of inotropic drugs and drugs acting on β-adrenergic receptors;
hypersensitivity to any component of the drug or other beta-blockers.

Egilok C tablets should be used with caution in the following cases (a careful assessment of the balance of benefits and risks is required):

Prinzmetal's angina;
atrioventricular block I degree;
obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome);
metabolic acidosis;
severe renal / hepatic impairment;
chronic obstructive pulmonary disease;
bronchial asthma;
diabetes;
thyrotoxicosis;
psoriasis;
myasthenia gravis;
depression;
pheochromocytoma (while taking alpha-blockers);
simultaneous use of cardiac glycosides;
elderly age.

Egilok S, instructions for use: method and dosage

Egilok S is taken orally, once a day (regardless of the prescribed dose), preferably in the morning. The tablets must be swallowed whole, without chewing or crumbling, and washed down with a sufficient amount of liquid. Meal time does not matter.

The optimal dose is selected by the doctor individually, with caution - in order to avoid the development of bradycardia.

Treatment of stable chronic heart failure (CHF) with clinical manifestations and impaired left ventricular systolic function is started only if the patient has been in a stable condition without exacerbation episodes for the last 6 weeks. At the same time, during the last 2 weeks, it is impossible to change the scheme of the main therapy.

In some cases, beta-blockers (including Egilok C) can cause a temporary worsening of the course of chronic heart failure. Sometimes it is possible to prolong therapy or reduce the dose, but some patients require metoprolol to be discontinued.

With CHF functional class II, at the beginning of therapy, 25 mg is prescribed, after 2 weeks, if necessary, the dose is increased to 50 mg. If, in this case, the effect is insufficient, further doubling of the dose is possible at intervals of 2 weeks. With long-term treatment, the maintenance dose is usually 200 mg.

With CHF III and IV functional classes in the first two weeks, Egilok C is prescribed in a daily dose of 12.5 mg (½ tablet at a dosage of 25 mg). The optimal maintenance dose is selected individually under close medical supervision, since symptoms of heart failure may progress. After 1-2 weeks, if necessary, increase the daily dose to 25 mg, after another 2 weeks - to 50 mg. If the therapeutic effect is insufficient, but provided that the drug is well tolerated, it is possible to double the dose at intervals of 2 weeks until the maximum is reached - 200 mg.

In the case of arterial hypotension and / or bradycardia, it may be necessary to correct the scheme of the main therapy, or to reduce the dose of Egilok C. The development of arterial hypotension during the dose selection period does not always indicate intolerance to the drug at this dose with continued treatment. However, the dose can be further increased only after the patient's condition has stabilized. Sometimes monitoring of the functional state of the kidneys is required.

Recommended daily doses (in 1 dose) of Egilok S for other indications:

arterial hypertension: 50-100 mg. If the effect is not enough, the daily dose is increased to a maximum of 200 mg or another antihypertensive agent is added to therapy (diuretics and slow calcium channel blockers are preferred);
heart rhythm disturbances: 100-200 mg;
angina pectoris: 100-200 mg. If the therapeutic effect is insufficient, another antianginal agent is added to the therapy;
functional disorders of cardiac activity, accompanied by tachycardia: 100 mg, if necessary, the daily dose is increased to 200 mg;
maintenance therapy after myocardial infarction: 100-200 mg (in this case, the daily dose can be divided into 2 doses);
prevention of migraine attacks: 100-200 mg.

The elderly, patients with impaired renal function and patients with moderate impairment of liver function do not need to adjust the dose.

In severe functional disorders of the liver (severe form of cirrhosis, portocaval anastomosis), it may be necessary to reduce the dose of Egilok S.

Side effects

Egilok S is generally well tolerated. If adverse reactions occur, they are usually mild and reversible.

Possible side effects (classified as follows: very often -> 10% of cases; often - 1-9.9%; infrequently - 0.1-0.9%; rarely - 0.01-0.09%; very rarely - <0.01%):

on the part of the cardiovascular system: often - a feeling of palpitations, orthostatic hypotension (very rarely accompanied by fainting), bradycardia, cold extremities; infrequently - a temporary increase in symptoms of heart failure, pain in the heart area, peripheral edema, atrioventricular block of the 1st degree, cardiogenic shock in patients with acute myocardial infarction; rarely - other disorders of cardiac conduction, arrhythmias; very rarely in patients with previous severe peripheral circulatory disorders - gangrene;
from the digestive system: often - abdominal pain, constipation, diarrhea, nausea; infrequently - vomiting; rarely - dryness of the oral mucosa, liver dysfunction; very rarely - hepatitis;
from the central nervous system: very often - increased fatigue; often - headache, dizziness; infrequently - insomnia / drowsiness, nightmares, decreased attention, paresthesia, depression, convulsions; rarely - anxiety, increased nervous excitability, sexual dysfunction / impotence; very rarely - depression, memory impairment / amnesia, hallucinations;
from the senses: rarely - dryness and / or irritation of the eyes, visual impairment, conjunctivitis; very rarely - disturbances in taste, ringing in the ears;
from the respiratory system: often - shortness of breath with physical exertion; infrequently - bronchospasm; rarely - rhinitis;
from the musculoskeletal system: very rarely - arthralgia;
on the part of the skin: infrequently - urticaria, increased sweating; rarely - hair loss; very rarely - exacerbation of the course of psoriasis, photosensitivity;
others: infrequently - an increase in body weight; very rarely - thrombocytopenia.

Overdose

The most serious symptoms of an overdose of metoprolol succinate are disorders of the cardiovascular system, but sometimes suppression of pulmonary function and a predominance of symptoms from the central nervous system are possible.

Possible symptoms: a marked decrease in blood pressure, AV blockade of I – III degrees, bradycardia, weak peripheral perfusion, asystole, cardiogenic shock, heart failure, apnea, suppression of lung function, bronchospasm, impairment or loss of consciousness, increased fatigue, increased sweating, tremor, paresthesia, convulsions, esophageal spasm, nausea, vomiting, impaired renal function, hyperkalemia, hyperglycemia, hypoglycemia (especially in children), transient myasthenic syndrome. With the concomitant intake of alcohol, barbiturates, antihypertensive drugs or quinidine, the patient's condition may worsen. The first symptoms of an overdose may occur 20–120 minutes after taking high doses of Egilok S.

First aid measures: intake of activated charcoal, if necessary - gastric lavage. Before gastric lavage, atropine (0.25–0.5 mg for adults) is prescribed due to the risk of stimulating the vagus nerve. If necessary, provide airway patency (by intubation) and adequate ventilation. It is necessary to administer glucose, replenish the circulating blood volume, and control the electrocardiogram. Also, atropine is administered at a dose of 1–2 mg intravenously; if necessary, the administration is repeated (especially in the presence of vagal symptoms). For depression (suppression) of the myocardium, an infusion of dopamine or dobutamine is given. In addition, it is possible to administer glucagon intravenously at 50–150 mcg / kg at intervals of 1 min. In some cases, it is advisable to add epinephrine (adrenaline) to therapy. With arrhythmias and an enlarged ventricular complex, an infusion of a solution of sodium chloride 0.9% or sodium bicarbonate is indicated. If necessary, install an artificial pacemaker. To stop bronchospasm, terbutaline is used (by injection or inhalation). In case of cardiac arrest, appropriate resuscitation measures are taken.

special instructions

Beta-blockers are not recommended for patients with obstructive pulmonary disease. If other antihypertensive drugs are poorly tolerated or do not provide the desired therapeutic effect, it is possible to use Egilok C, but the minimum effective dose should be prescribed. If necessary, use beta ₂ -adrenomimetics.

Compared to non-selective beta-blockers, selective beta ₁ -blockers have a lesser effect on carbohydrate metabolism and mask the symptoms of hypoglycemia, but the risk of such an effect cannot be completely excluded.

In decompensated chronic heart failure, the stage of compensation should be achieved before starting treatment, and it should be maintained during therapy.

Data from clinical studies on the safety and efficacy of Egilok S in severe stable heart failure (NYHA class IV) are limited.

Metoprolol succinate may worsen symptoms of peripheral circulatory disorders (usually due to a decrease in blood pressure).

For patients with concomitant pheochromocytoma, Egilok C is prescribed simultaneously with an alpha-blocker.

In rare cases, in violation of atrioventricular conduction, deterioration (up to AV block) is possible. With the development of bradycardia, you need to reduce the dose of metoprolol succinate or gradually cancel it.

Patients who are to undergo surgery should warn the anesthesiologist about taking the drug Egilok S. It is not recommended to cancel beta-blockers.

Anaphylactic shock that develops during therapy with beta-blockers is more severe. At the same time, the use of adrenaline in standard therapeutic doses does not always cause the desired effect.

The efficacy and safety of Egilok S in patients with symptoms of heart failure in combination with acute myocardial infarction and unstable angina pectoris has not been established.

In case of abrupt withdrawal of the drug, it is possible to increase the symptoms of chronic heart failure, increase the risk of myocardial infarction and sudden death, especially in high-risk patients. For this reason, it is not recommended to suddenly stop taking Egilok C. This should be done gradually, for at least 2 weeks, reducing the dose by 2 times at each stage until the final dose of 12.5 mg is reached - it should be taken at least for 4 days before the complete withdrawal of the drug. If unwanted symptoms appear with this scheme, a slower cancellation of therapy is recommended.

Influence on the ability to drive vehicles and complex mechanisms

Egilok S can cause dizziness and fatigue, therefore, patients receiving the drug should be careful when driving and performing potentially hazardous types of work.

Application during pregnancy and lactation

Adequate controlled studies on the use of metoprolol succinate in pregnant women have not been conducted. As a result, Egilok S can only be used in women for whom the expected benefits of therapy outweigh the possible risks.

Beta-blockers can cause some side effects in the fetus, newborns, and infants, such as bradycardia.

Metoprolol passes into mother's milk in small quantities, so the risk of developing adverse reactions is low. Nevertheless, infants whose mothers receive Egilok C during lactation should be under close medical supervision for possible signs of β-adrenergic receptor blockade.

Pediatric use

Egilok S is contraindicated under 18 years of age, since its efficacy and safety in pediatric patients have not been established.

With impaired renal function

Egilok S is prescribed with caution in patients with chronic renal failure.

Correction of the dosage regimen for functional impairment of the kidneys and hemodialysis is not required.

For violations of liver function

Egilok C is prescribed with caution to patients with hepatic insufficiency. The doctor selects the dose individually, based on the data of the clinical condition.

Use in the elderly

For the treatment of elderly patients, Egilok C tablets are used with precautions.

Drug interactions

Combinations not recommended:

verapamil: high risk of developing bradycardia and lowering blood pressure, there is a complementary inhibitory effect on AV conduction and sinus node function;
derivatives of barbituric acid: the metabolism of metoprolol is enhanced;
propafenone: the plasma concentration of metoprolol increases significantly (2–5 times), the development of side effects is possible.

Combinations requiring caution and may require dose adjustment:

class I antiarrhythmics: it is possible to add up a negative inotropic effect, which is fraught with the development of serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in cases of AV conduction disorder and sick sinus syndrome;
non-steroidal anti-inflammatory drugs (with the possible exception of sulindac): the antihypertensive effect of metoprolol is weakened;
cardiac glycosides: AV conduction time increases, bradycardia develops;
clonidine: after its abrupt withdrawal, hypertensive reactions may increase (it is recommended to start withdrawing beta-blockers several days before stopping the use of clonidine);
quinidine: in patients with rapid hydroxylation, the metabolism of metoprolol is inhibited, which causes a significant increase in its plasma concentration and an increase in beta-blockade (similar reactions are possible when using other beta-blockers, in the metabolism of which the isoenzyme CYP2D6 is involved);
rifampicin: it is possible to increase the metabolism of metoprolol and decrease its plasma concentration;
oral hypoglycemic agents: there is a possibility of a change in their effect, which may require dose adjustment;
inhalation anesthetics: increased cardiodepressant effect;
amiodarone: the development of severe sinus bradycardia is possible. Amiodarone has a long half-life, so the interaction may appear long after its withdrawal;
epinephrine: there is a risk of bradycardia and severe arterial hypertension;
diltiazem: there is a mutual strengthening of the inhibitory effect on the conductivity and function of the sinus node, cases of severe bradycardia are known;
phenylpropanolamine (norephedrine): it is possible to increase diastolic blood pressure to pathological values and develop a hypertensive crisis (even after using a single dose of 50 mg);
diphenhydramine: the metabolism of metoprolol to α-hydroxymetoprolol decreases 2.5 times, the effect of the drug Egilok C is enhanced;
cimetidine, hydralazine: the plasma concentration of metoprolol may increase.

Special care should be taken with the simultaneous use of other beta-blockers (including in the form of eye drops) and MAO inhibitors.

Analogs

The analogues of Egilok S are Aritel, Atenolol, Betacard, Bisoprolol, Concor, Coronal, Metocard, Niperten, Serdol, Tirez, Egilok, Estekor and many others.

Terms and conditions of storage

Store at a temperature not exceeding 30 ° C out of reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Egilok S

Reviews about Egilok S are positive: the drug effectively reduces high blood pressure, is well tolerated and is relatively inexpensive.

As disadvantages indicate the development of side effects in some patients.

Price for Egilok S in pharmacies

Average prices for Egilok S for a pack of 30 tablets are:

dosage 25 mg - 170 rubles;
dosage of 50 mg - 257 rubles;
dosage 100 mg - 330 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!