Egilok - instructions for use, doses, side effects, contraindications

Excipients: cellulose microcrystalline 41.5 / 83/166 mg, sodium carboxymethyl starch (type A) 7.5 / 15/30 mg, silicon dioxide colloidal anhydrous 2/4/8 mg, povidone (K-90) 2/4/8 mg, magnesium stearate 2/4/8 mg.

Description:

Tablets 25 mg: White or almost white, round, biconvex tablets with a cross-shaped dividing line and double bevel ("double snap" form) on one side and with engraving E 435 - on the other side, odorless.

Tablets 50 mg: White or almost white, round, biconcave tablets, with a risk on one side and with engraving E 434 - on the other side, odorless.

Tablets 100 mg: White or almost white, round, biconvex tablets, with a facet, with a risk on one side and with engraving E 432 - on the other side, odorless.

Pharmacotherapeutic group:beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.02 Metoprolol

Pharmacodynamics:

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.

With arterial hypertension metoprolol reduces blood pressure in patients in the "standing" and "lying". The prolonged antihypertensive effect of the drug is associated with a gradual decrease in the total peripheral vascular resistance.

With arterial hypertension, prolonged use of the drug leads to a statistically significant decrease in left ventricular mass and an improvement in its diastolic function.

In men with mild to moderate hypertension metoprolol reduces mortality from cardiovascular causes (primarily, sudden death, a 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.

Reduction of the heart rate and corresponding diastole lengthening with metoprolol intake provide an improvement in blood supply and assimilation of oxygen by myocardium with disturbed blood flow. Therefore, with angina pectoris, the drug reduces the number, duration and severity of seizures, as well as asymptomatic manifestations of ischemia, and improves the patient's physical performance.

With myocardial infarction metoprolol reduces the death rate, reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A decrease in the death rate can also be observed with metoprolol in both 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 recurrent myocardial infarction.

With chronic heart failure in the background of idiopathic hypertrophic obstructive cardiomyopathy metoprolol tartrate, taken 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 extrasystole metoprolol reduces the incidence of ventricular contractions and the number of ventricular extrasystoles.

In therapeutic doses, peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than those of nonselective beta-blockers.

Compared with non-selective beta-blockers metoprolol less impact on insulin production and carbohydrate metabolism. It does not increase the duration of attacks of hypoglycemia.

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

Pharmacokinetics:

Metoprolol is rapidly and completely absorbed in the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic range of doses.

The maximum concentration in the blood plasma is achieved after 1.5-2 hours after ingestion. After suction metoprolol is largely exposed to the metabolism of the primary passage through the liver. The bioavailability of metoprolol is approximately 50% at a single dose and approximately 70% with regular admission.

Admission simultaneously with food can increase the bioavailability of metoprolol by 30-40%. Metoprolol insignificantly (~ 5-10%) binds to blood 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 (1 to 9 hours). The total ground 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 not found.

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

Impaired liver function slightly affects the pharmacokinetics of metoprolol. However, with severe cirrhosis of the liver and after applying the portocaval shunt bioavailability can increase, and the overall clearance from the body decreases. After portocaval 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 approximately 6-fold compared to that of healthy volunteers.

Indications:

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.

Contraindications:

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

Due to the lack of clinical data, Egiolok® is contraindicated in acute myocardial infarction, accompanied by a heart rate of less than 45 beats per minute, at intervals PQ more than 240 ms, and systolic blood pressure below 100 mm Hg.

Carefully:

Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (COPD), renal / hepatic insufficiency, myasthenia gravis, pheochromocytoma (with simultaneous use with alpha-blockers), thyrotoxicosis, AV blockade of the I degree, depression (including in the anamnesis), psoriasis, obliterating diseases of peripheral vessels ("intermittent" lameness, Raynaud's syndrome), pregnancy, lactation,old age, in patients with a history of allergic anamnesis (it is possible to reduce the response with adrenaline).

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 exceeds 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 childbirth, as it is possible to develop bradycardia, respiratory depression, lower blood pressure and hypoglycemia.

Despite the fact that when taking therapeutic doses of metoprolol only small amounts of the drug are excreted into breast milk, the newborn should be kept under observation (bradycardia is possible).

Application of the drug during lactation Not recommended. If it is necessary to use the drug during lactation it is recommended to stop breastfeeding.

Dosing and Administration:

Egilok® tablets are taken orally. Tablets can be taken with food or regardless of food intake. If necessary, the tablet can be broken in half.

The dose should be selected gradually and individually to avoid excessive bradycardia. The maximum daily dose is 200 mg.

Recommended doses:

Arterial hypertension

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

Angina pectoris

The initial dose of 25-50 mg from two to three times a day. Depending on the effect, this dose can be gradually increased to 200 mg per day or add another antianginal drug.

Supportive therapy after myocardial infarction

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

Heart rhythm disturbances

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 add another antiarrhythmic agent.

Hyperthyroidism

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

Functional disorders of the heart, accompanied by palpitation

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.

Preventing 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 changing the dosing regimen is not required.

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

In elderly patients correction of the dose is not required.

Side effects:

Egilok® is usually well tolerated by patients. Side effects are usually weak and reversible. The following are secondary. effects are recorded in clinical trials and in the therapeutic use of metoprolol. In some cases, the association of an undesirable phenomenon with the use of the drug is not reliably established.

The following parameters of the frequency of side effects are defined as follows: very often: ≥ 10%, often: 1-9.9%, infrequently: 0.1-0.9%, rarely: 0.01-0.09%, very rarely (including individual messages): <0.01%.

From the nervous system: very often - increased fatigue; often - dizziness, headache; rarely - increased excitability, anxiety, impotence / sexual dysfunction; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, "nightmarish" 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 limbs, a feeling of palpitations; infrequent - temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, atrioventricular blockade of the I degree; rarely - conduction disorders, 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, a violation of liver function.

From the skin: infrequently - hives, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis.

From the respiratory system: often - shortness of breath with physical effort; infrequently - bronchospasm in patients with bronchial asthma; rarely rhinitis.

From the sense organs: rarely - visual impairment, dryness and / or eye irritation, conjunctivitis; very rarely - ringing in the ears, a violation of taste.

Other: infrequent increase in body weight; very rarely - arthralgia, thrombocytopenia.

The use of Egiloc® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause can not be reliably established.

Overdose:

Symptoms: marked decrease in arterial pressure, sinus bradycardia, atrioventricular blockade, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The above symptoms may increase with the simultaneous use of ethanol, antihypertensive drugs, quinidine and barbiturates.

The first symptoms of an overdose appear after 20 minutes - 2 hours after taking the drug.

Treatment: careful monitoring of the patient (control of blood pressure, heart rate, respiration rate, kidney function, blood glucose concentration, blood serum electrolytes) in intensive care units is necessary.

If the drug has been taken recently, rinsing the stomach with activated charcoal may reduce further absorption of the drug (if washing is not possible, you can induce vomiting if the patient is conscious).

In case of excessive reduction of blood pressure, bradycardia and the threat of heart failure - in / with, with an interval of 2-5 minutes, beta-adrenomimetics - until the desired effect or iv in 0.5-2 mg of atropine. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine). When hypoglycemia - the introduction of 1-10 mg glucagon, the installation of a temporary pacemaker. When bronhospazme enter beta-adrenomimetiki. With convulsions - slow IV injection of diazepam.

Hemodialysis is ineffective.

Interaction:

The antihypertensive effects of the drug Egilok® and other antihypertensive drugs usually intensify. To avoid arterial hypotension, careful monitoring of patients receiving combinations of such drugs is necessary. However, the summation of the effects of antihypertensive drugs can, if necessary, be used 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. Avoid intravenous administration of calcium channel blockers like verapamil to patients receiving beta-blockers.

Caution should be exercised while taking the following products at the same time:

Oral antiarrhythmic drugs (such as quinidine and amiodarone) - the risk of bradycardia, atrioventricular blockade.

Cardiac glycosides - risk of bradycardia, conduction disorders; metoprolol does not affect the positive inotropic effect of cardiac glycosides.

Other antihypertensive drugs (especially the group of guanethidine, reserpine, alpha-methyldopha, clonidine and guanfacin) because of the risk of hypotension and / or bradycardia.

Termination of simultaneous reception of metoprolol and clonidine should be started, canceling metoprolol, and then (in a few days) clonidine; if you first cancel clonidine, the hypertensive crisis can develop.

Some drugs acting on the central nervous system, for example: hypnotics, tranquilizers, tri- and tetracyclic antidepressants, neuroleptics and ethanol increase the risk of hypotension.

Means for anesthesia - risk of oppression of cardiac activity.

Alpha- and beta-sympathomimetics - The risk of hypertension, a significant bradycardia; the possibility of cardiac arrest.

Ergotamine - increased vasoconstrictor effect.

Betha₂-sympathomimetics - functional antagonism.

Nonsteroidal anti-inflammatory drugs (eg, indomethacin) - can weaken the antihypertensive effect.

Estrogens - it is possible to reduce the antihypertensive effect of metoprolol.

Hypoglycemic agents for ingestion and insulin - metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia.

Curare like muscle relaxants - Increased neuromuscular blockade.

Enzyme Inhibitors (eg, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline) - increased effects of metoprolol due to an increase in its concentration in the blood plasma.

Inductors of enzymes (rifampicin and barbiturates): effects of metoprolol may be reduced due to an increase in "hepatic" metabolism.

Simultaneous application withwhich blocks sympathetic ganglia, or other beta-blockers (for example: eye drops) or monoamine oxidase inhibitors requires careful medical supervision.

Special instructions:

Control of patients taking beta-blockers includes regular measurement of heart rate (heart rate) 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.

It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at a heart rate of less than 50 beats per minute.

When taking a dose above 200 mg per day, cardioselectivity decreases.

With heart failure, treatment with Egilok® begins only after reaching the stage of compensation of cardiac function.

It is possible to increase the severity of the hypersensitivity reactions and the absence of the effect of the administration of usual doses of epinephrine (epinephrine) in patients withweighed allergic anamnesis.

Anaphylactic shock can be more severe in patients taking Egilok®.

It can intensify the symptoms of peripheral arterial circulation.

It should be avoided abrupt discontinuation of the drug Egilok®. The drug should be canceled gradually by lowering the doses for about 14 days. Abrupt cancellation can increase the symptoms of angina and increase the risk of coronary events. Particular attention should be paid to patients with coronary artery disease when drug is withdrawn.

With angina pectoris, the selected dose of Egilok® should provide a heart rate at rest within 55-60 beats / min, with a load of no more than 110 beats / minute.

Patients who use contact lenses should take into account that against the background of treatment with beta-adrenoblockers, tear production can be reduced.

Egilok® can mask some clinical manifestations of hyperthyroidism (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, as it can strengthen symptoms.

In diabetes mellitus can mask tachycardia caused by hypoglycemia.Unlike non-selective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels. If the drug Egilok® is administered to people 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 corrected (see section "Interaction with other medicinal products").

If it is necessary to prescribe to patients with bronchial asthma, beta-adrenostimulants are prescribed as concomitant therapy; when pheochromocytoma - alpha-adrenoblockers.

If surgical intervention is necessary, the surgeon / anesthesiologist should be warned about the therapy (choice of a means for general anesthesia with a minimum negative inotropic effect), drug discontinuation is not recommended.

Drugs that reduce catecholamine stocks (for example, reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs should be under constant observation of the doctor for the detection of excessive reduction in blood pressurepressure or bradycardia.

In elderly patients, it is recommended to regularly monitor liver function. Correction of the dosing regimen is required only if the patient develops an elderly bradycardia (less than 50 beats / min), a marked decrease in blood pressure (systolic blood pressure below 100 mmHg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction , sometimes it is necessary to stop treatment.

Patients with severe renal failure are advised to monitor kidney function.

Special monitoring should be carried out on the condition of patients with depressive disorders receiving metoprolol; In the case of depression, caused by the use of beta-blockers, it is recommended to stop therapy.

If progressive bradycardia occurs, reduce the dose or stop taking the drug.

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

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:Tablets, 25 mg, 50 mg and 100 mg.

Packaging:

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

Tablets 50 mg: for 60 tablets in a bottle of brown glass with a PE cap with a shock absorber, with the control of the first autopsy. 1 bottle with instructions for use packed in a cardboard box. Or 15 tablets in a blister of PVC / PVDC / / al. foil. 4 blisters together with instructions for use are packed in a cardboard box.

Tablets 100 mg: for 30 or 60 tablets in a bottle of brown glass with a PE cap with a shock absorber, with the control of the first autopsy. 1 bottle with instructions for use packed in a cardboard box.

Storage conditions:

Store at temperatures from 15 to 25 ° C, out of the reach of children.

Shelf life:5 years.

Do not use after the expiry date indicated on the package

Terms of leave from pharmacies:On prescription

Registration number:P N 015639/01

Date of registration:17.03.2009 / 08.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS PHARMACEUTICALS, Plc Hungary

SERDIK, LLC Russia

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp25.07.2016

Illustrated instructions

Instructions

Egilok® (Egilok®)