Universal reference book for medicines
Product name: EHILOK ® (EGILOK ® )

Active substance: metoprolol

Type: Beta 1- blocker

Manufacturer: EGIS Pharmaceuticals (Hungary)
Composition, form of production and packaging
Tablets are
white or almost white, round, biconvex, with a cruciform dividing line and double bevel (double step shape) on one side and engraved "E435" on the other side, odorless.

1 tab.

metoprolol tartrate 25 mg

Excipients: microcrystalline cellulose - 41.5 mg, sodium carboxymethyl starch (type A) - 7.5 mg, silicon dioxide colloidal anhydrous - 2 mg, povidone K90 - 2 mg, magnesium stearate - 2 mg.

20 pcs.
- blisters (3) - packs of cardboard.
60 pcs.
- banks of dark glass (1) - packs of cardboard.
Tablets white or almost white, round, biconcave, with a risk on one side and engraved "E434" - on the other side, odorless.

1 tab.

metoprolol tartrate 50 mg

Excipients: cellulose microcrystalline - 83 mg, sodium carboxymethyl starch (type A) - 15 mg, silicon dioxide colloidal anhydrous - 4 mg, povidone K90 - 4 mg, magnesium stearate - 8 mg.

15 pcs.
- blisters (4) - packs of cardboard.
60 pcs.
- banks of dark glass (1) - packs of cardboard.
Tablets white or almost white, round, biconcave, with a facet, with a risk on one side and engraved "E432" - on the other side, odorless.

1 tab.

metoprolol tartrate 100 mg

Excipients: microcrystalline cellulose - 166 mg, sodium carboxymethyl starch (type A) - 30 mg, silicon dioxide colloidal anhydrous - 8 mg, povidone K90 - 8 mg, magnesium stearate - 8 mg.

30 pcs.
- banks of dark glass (1) - packs of cardboard.
60 pcs.
- banks of dark glass (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Cardioselective blocker of? -adrenoceptors.

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 lowers blood pressure in patients in a standing and lying position.
Long-term antihypertensive effect of the drug is associated with a gradual decrease in OPSS. 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, fatal and non-fatal heart attack and stroke).
Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic BP, heart rate and myocardial contractility.
The decrease in heart rate and the 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 lowers 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 against a background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken in low doses (2-5 mg / day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient.
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.

In comparison with nonselective beta-blockers, metoprolol less affects insulin production and carbohydrate metabolism, does not increase the duration of hypoglycemia attacks.

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 decrease in the total serum cholesterol concentration after the use of metoprolol for several years.
PHARMACOKINETICS

Suction

Metoprolol is rapidly and completely absorbed from the digestive tract.
The drug is characterized by linear pharmacokinetics in the therapeutic range of doses. C maxin the blood plasma is achieved after 1.5-2 hours after ingestion. Bioavailability is approximately 50% with a single dose and approximately 70% with regular application. Taking the drug at the same time as food can increase bioavailability by 30-40%.
Distribution

Metoprolol slightly (approximately 5-10%) binds to blood plasma proteins.
V d is 5.6 l / kg.
Metabolism

After absorption metoprolol is largely exposed to the effect of "first passage" through the liver.
Metabolised in the liver by cytochrome P450 isoenzymes. Metabolites do not have pharmacological activity.
Excretion

T 1/2 is 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%.
Pharmacokinetics in special clinical cases

There were no significant changes in the pharmacokinetics of metoprolol in elderly patients.

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 insufficiency (GFR <5 ml / min), a significant accumulation of metabolites is observed. However, such accumulation of metabolites does not enhance the degree of beta-adrenergic blockade.
Disturbance of liver function slightly affects the pharmacokinetics of metoprolol.
However, with severe cirrhosis of the liver and after applying the portocaval anastomosis, the bioavailability can increase, and the total clearance from the body is reduced. After portocaval shunting, the total clearance of the drug from the body is approximately 0.3 l / min, and the AUC increases approximately 6-fold compared to that of healthy volunteers.
INDICATIONS

- arterial hypertension (in monotherapy or in combination with other antihypertensive drugs);

- functional disorders of cardiac activity, accompanied by tachycardia;

- IHD (secondary prevention of myocardial infarction, prevention of angina attacks);

- heart rhythm disturbances (supraventricular arrhythmias, ventricular extrasystole);

- hyperthyroidism (as part of complex therapy);

- prevention of migraine attacks.

DOSING MODE

The drug should be taken orally during or regardless of food intake.
If necessary, the tablet can be broken in half.
The dose should be selected gradually and individually to avoid the development of excessive bradycardia.
The maximum daily dose is 200 mg.
With a mild or moderate degree of arterial hypertension, the initial dose is 25-50 mg 2 times / day (morning and evening).
If necessary, the dose can be gradually increased to 100-200 mg / day or add another antihypertensive agent.
With angina, the initial dose is 25-50 mg 2-3 times / day.
Depending on the effect, the dose can be gradually increased to 200 mg / day or add another antianginal drug.
The recommended dose of the drug for maintenance therapy after myocardial infarction is 100-200 mg / day, divided into 2 doses (morning and evening).

With heart rhythm disturbances, the initial dose is 25-50 mg 2-3 times / day.
If necessary, the daily dose can be gradually increased to 200 mg / day or add another antiarrhythmic agent.
In hyperthyroidism, the usual daily dose is 150-200 mg in 3-4 doses.

In functional heart disorders accompanied by palpitation, the usual dose is 50 mg 2 times / day (morning and evening);
If necessary, the dose can be increased to 200 mg in 2 divided doses.
For prevention of migraine attacks, the recommended dose is 100 mg / day in 2 divided doses (morning and evening);
If necessary, the dose can be increased to 200 mg / day in 2 divided doses.
Patients with impaired renal function do not need to change the dosage regimen.

In liver cirrhosis, dose changes are usually not required due to the low binding of metoprolol to blood plasma proteins.
In case of 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.

SIDE EFFECT

Egilok ® is usually well tolerated by patients.
Side effects, as a rule, are weak and reversible. The following side effects are documented 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; infrequently - paresthesia, convulsions, depression, decreased concentration, drowsiness, insomnia, nightmares; 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, palpitation;
infrequent - temporary enhancement of symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV-blockade of the I degree;rarely - conduction disorders, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders).
From the respiratory system: often - shortness of breath with physical effort;
infrequently - bronchospasm in patients with bronchial asthma; rarely rhinitis.
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: rarely - hives, increased sweating;
rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis.
From the senses: rarely - visual impairment, dryness and / or eye irritation, conjunctivitis;
very rarely - ringing in the ears, a violation of taste.
On the part of the reproductive system: rarely - impotence / sexual dysfunction.

Other: infrequently - weight gain;
very rarely - arthralgia, thrombocytopenia.
The use of Egilok ® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause can not be reliably established.

CONTRAINDICATIONS

- cardiogenic shock;

- AV blockade II and III degree;

- Sinoatrial blockade;

- SSSU;

- sinus bradycardia (heart rate <50 bpm);

- heart failure in the stage of decompensation;

- violations of peripheral blood circulation of severe degree;

- age to 18 years (due to lack of sufficient clinical data);

- simultaneous iv injection of verapamil;

- severe form of bronchial asthma;

- pheochromocytoma without simultaneous use of alpha-blockers;

- hypersensitivity to metoprolol or any other component of the drug;

- hypersensitivity to other beta-blockers.

Due to the lack of clinical data, Egiolok ® is contraindicated in acute myocardial infarction, accompanied by a heart rate <45 bpm, with a PQ interval of> 240 ms, and systolic blood pressure <100 mmHg.

With caution should prescribe the drug in diabetes mellitus;
metabolic acidosis; bronchial asthma; COPD; renal / hepatic insufficiency; myasthenia gravis;pheochromocytoma (with simultaneous use with alpha-blockers); thyrotoxicosis; AV-blockade of the 1st degree, depression (including in the anamnesis); psoriasis;obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pregnancy; during lactation; elderly patients; patients with a history of allergic anamnesis (there may be a decrease in response with the use of adrenaline).
PREGNANCY AND LACTATION

The use of the drug is not recommended for pregnancy.
The use of the drug is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.If it is necessary to prescribe the drug during pregnancy, careful monitoring of the fetus and newborn within 48-72 hours after delivery is necessary, since bradycardia, arterial hypotension, hypoglycemia and respiratory depression are possible.
Despite the fact that when using the drug in therapeutic doses only a small amount of metoprolol is excreted in breast milk, it is necessary to observe the state of the newborn (bradycardia is possible).
The use of the drug during lactation is not recommended. If you need to use Egilok ® during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with impaired renal function do not need to change the dosage regimen.

With caution should prescribe the drug for kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In liver cirrhosis, dose changes are usually not required due to the low binding of metoprolol to blood plasma proteins.
In case of severe hepatic insufficiency (for example, after portocaval bypass surgery), it may be necessary to reduce the dose of Egilok ® .
With caution should prescribe the drug in hepatic failure.

APPLICATION FOR CHILDREN

Due to the lack of sufficient clinical data, the drug is not recommended for use in children and adolescents under the age of 18 years .

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

When appointing the drug Egilok ® should regularly monitor heart rate and blood pressure.
It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate <50 bpm.
Patients with diabetes should regularly monitor blood glucose and, if necessary, adjust the dose of insulin or oral hypoglycemic drugs.

When using the drug at a dose exceeding 200 mg / day, cardioselectivity decreases.

The appointment of Egilok to patients with chronic heart failure is possible only after reaching the stage of compensation.

In patients taking Egilok ® , it is possible to intensify the severity of hypersensitivity reactions (against the background of a weighed allergic anamnesis) and the absence of the effect of the administration of usual doses of epinephrine (epinephrine).

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

Against the backdrop of the use of Egiloc, the symptoms of impaired peripheral circulation may worsen.

Egilok ® should be canceled gradually, consistently reducing its dose within 14 days.
With a sharp cessation of treatment, there may be an increase in angina attacks and a risk of developing coronary disorders. During the period of drug cancellation, patients with coronary artery disease should be under careful medical supervision.
With angina pectoris, the selected dose of Egilok ® should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats per 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 (for example, tachycardia).
Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, since it can strengthen symptoms.
With diabetes, taking Egiloc 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.
When appointing metoprolol, patients with bronchial asthma need the simultaneous use of beta 2 -adrenomimetics.

In patients with pheochromocytoma, Egilok ® should be used in combination with alpha-blockers.

Before conducting any surgical intervention, it is necessary to inform the surgeon / anesthesiologist about the ongoing therapy with Egiloc (selection of the drug for general anesthesia with minimal negative inotropic effect);
withdrawal of the drug is not required.
Drugs that reduce the supply of catecholamines (for example, reserpine) can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision for the detection of excessive reduction in blood pressure or bradycardia.

When prescribing the drug, elderly patients should be monitored regularly for liver function.
Correction of the dosing regimen is required only if elderly patients experience an increasing bradycardia (<50 bpm), a marked decrease in blood pressure (systolic blood pressure <100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmia, severe impairment of function liver. Sometimes it is necessary to stop treatment.
Patients with severe renal failure are advised to monitor kidney function.

It is necessary to conduct special monitoring of the condition of patients with depressive disorders.
In the case of depression caused by the use of beta-blockers should discontinue therapy.
In the event of progressive bradycardia should reduce the dose or stop the drug.
Use in Pediatrics

Due to the lack of sufficient clinical data product is not recommended for use in children and adolescents under the age of 18 years .
Impact on the ability to drive vehicles and manage mechanisms

Caution should be exercised when driving and when engaging in potentially hazardous activities that require high concentration (the risk of dizziness and fatigue).
OVERDOSE

Symptoms: marked reduction of blood pressure, sinus bradycardia, AV-block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The above symptoms may be amplified while the use of ethanol, antihypertensives, quinidine and barbiturates.
Overdose first symptoms appear after 20 min-2 hr after dosing.
Treatment:requires careful monitoring of the patient (control of blood pressure, heart rate, respiratory rate, kidney function, blood glucose, serum electrolytes) under intensive care. If the drug was passed recently, gastric lavage with activated charcoal may reduce further absorption of the drug (if washing is not possible, can cause vomiting, if the patient is conscious). In case of excessive reduction in blood pressure, bradycardia and heart failure threat - in / at intervals of 2-5 minutes, the introduction of beta-agonists (to achieve the desired effect) or on / in administering 0.5-2 mg atropine. If no positive effect - dopamine, dobutamine or norepinephrine (noradrenaline). When hypoglycemia - glucagon administration 1-10 mg, temporary pacemaker. When bronchospasm - administration of beta 2-adrenomimetikov. In convulsions - slow / w diazepam.
Hemodialysis is ineffective.
DRUG INTERACTION

Antihypertensive drug effects Egilok ® while the use of other agents usually increase. To avoid hypotension requires careful monitoring of the patients receiving the combination of such means. However, the beneficial effect of antihypertensive drugs can, if necessary, to use in order to achieve effective control of blood pressure.
Simultaneous metoprolol and calcium channel blockers slow diltiazem-type and verapamil may lead to increased negative inotropic and chronotropic effects. Avoid on / in the calcium channel blockers verapamil-type patients receiving beta-blockers.
Combinations requiring compliance with caution
Oral antiarrhythmic drugs (such as quinidine and amiodarone): risk of bradycardia, AV-blockade.
Cardiac glycosides: risk of bradycardia, disturbances of; metoprolol did not affect the positive inotropic effect of cardiac glycosides.
Other antihypertensive drugs (especially group guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine): the risk of hypotension and / or bradycardia.
Termination of the simultaneous application of clonidine and metoprolol should always start, canceling metoprolol, and then (after a few days) clonidine; if the first cancel clonidine may develop a hypertensive crisis.
Some drugs acting on the CNS (eg, sedatives, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol): the risk of hypotension.
Means of anesthesia: the risk of depression of cardiac activity.
Alpha- and beta-sympathomimetics: the risk of developing hypertension, significant bradycardia, the possibility of cardiac arrest.
Ergotamine: increased vasoconstrictor effect.
Beta 2 -simpatomimetiki: functional antagonism.
NSAIDs (eg, indomethacin) may weaken the antihypertensive effect.
Estrogens: may reduce the antihypertensive effect of metoprolol.
Hypoglycemic agents for oral and insulin metoprolol may enhance hypoglycemic effects and to mask the symptoms of hypoglycemia.
Curariform relaxants: increased neuromuscular blockade.
Enzyme inhibitors (e.g., cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, e.g., paroxetine, fluoxetine and sertraline) may increase due to increased effects of metoprolol in the blood plasma concentration.
Enzyme inducers (rifampicin and barbiturates): metoprolol effects may be reduced due to increased hepatic metabolism.
Simultaneous application means blocking the sympathetic ganglia, or other beta-blockers (e.g., eye drops) or MAO inhibitors requires close medical supervision.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of 15 ° to 25 ° C.
Shelf life - 5 years.
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