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

Active substance: metoprolol

Type: Beta 1- blocker

Manufacturer: EGIS Pharmaceuticals (Hungary) manufactured by ACINO PHARMA (Switzerland)
Composition, form of production and packaging
Long-acting tablets coated with a film coat of
white or almost white color, oblong, biconvex, with a risk on both sides.

1 tab.

metoprolol tartrate 50 mg

- "- 100 mg

Excipients: silicon dioxide colloidal anhydrous, magnesium stearate, microcrystalline cellulose;
in the composition of pellets: macrogol 6000, sugar grits (sucrose, molasses starch), talc; in the composition of the pellet shell: giprolose, magnesium stearate, triethyl citrate, ethyl cellulose.
Composition of the film coat:
hypromellose, macrogol 6000, talc, titanium dioxide (E171).

10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2013.

PHARMACHOLOGIC EFFECT

The cardioselective blocker of β-adrenoreceptors does not possess internal sympathomimetic and membrane-stabilizing activity.
It has antihypertensive, anti-anginal and antiarrhythmic effects.
Metoprolol suppresses the effect of increased activity of the sympathetic system on the heart, and also causes a rapid decrease in heart rate and cardiac output.

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 a single and short-term repeated intake of metoprolol reduces the activity of renin plasma, which is due to the suppression of renal?
1- adrenoreceptors, which leads to a decrease in the production of renin and, accordingly, the reduction of angiotensin mediated angiotensin-dependent vasoconstriction.
With arterial hypertension, prolonged use of metoprolol leads to a statistically significant decrease in the mass of the left ventricle.

Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing systemic BP, heart rate and heart contractility.
By reducing heart rate and corresponding diastole lengthening, metoprolol improves blood supply and oxygenation of myocardial regions with disturbed blood flow. Therefore, the drug reduces the frequency of angina attacks and improves physical performance.
When taken after myocardial infarction, metoprolol reduces the risk of repeated myocardial infarction.

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.
It does not significantly change cardiovascular reactions to hypoglycemia and does not increase the duration of hypoglycemic episodes.
PHARMACOKINETICS

Suction

After intake of metoprolol almost completely (approximately 95%) is absorbed from the digestive tract.
However, after absorption, metoprolol is largely metabolized by "first passage" through the liver. Bioavailability is approximately 35%. With repeated admission, the AUC increases by approximately 20%.
The curve of the dependence of the concentration in the blood plasma on time has the features characteristic for the sustained-release formulations.

The pharmacokinetics of metoprolol are linear up to a dose of 800 mg.

Distribution

Binding to plasma proteins is 10%.

Metoprolol is well distributed in tissues and has a large V d of 5.5 l / kg.

During 4-6 hours after taking the slow-absorption phase passes into a roughly 6-hour plateau (C max = 37.4 ng / ml after the administration of a single dose, C ss maxis
54.7 ng / ml), followed by a slow-release phase.
Metabolism

Metoprolol is metabolized in the liver with the participation of cytochrome P450 isoenzymes.
Metabolites (O-desmethylmethoprolol and? -hydroximethoprolol) do not possess beta-adrenoblocking activity. Since the metabolism of the drug is carried out by polymorphic enzymes, its level in the blood plasma has significant (up to 17-fold) differences in different patients.
Excretion

T 1/2 metoprolol in the form of a retard tablet is 6-12 hours, which is much more than T 1/2 metoprolol in a conventional dosage form (about 3 hours).
A longer half-life can be explained by delayed absorption.
Metoprolol is excreted mainly by the kidneys (approximately 95%).
About 10% of the administered dose of metoprolol is excreted unchanged. Metabolites are excreted with bile.
Pharmacokinetics in special clinical cases

Metoprolol is not removed from the body during hemodialysis.
Treatment of patients with reduced renal function does not require dose adjustment.
Violation of the liver function slows the metabolism of metoprolol, and in cases of insufficient liver function, the dose of the drug should be reduced.

INDICATIONS

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

- Chronic heart failure in the stage of compensation (in combination with standard therapy with diuretics, ACE inhibitors, cardiac glycosides);

- IHD (secondary prevention of myocardial infarction - as part of complex therapy, prevention of angina attacks);

- Prevention of cardiac arrhythmias, especially supraventricular tachycardia and ventricular tachycardia caused by adrenergic-dependent lengthening of the QT interval;

hyperkinetic cardiac syndrome;

- hyperthyroidism (as part of complex therapy);

- prevention of migraine attacks.

DOSING MODE

The drug is taken 1 time / day, in the morning, regardless of food intake.

In order to prevent bradycardia, the dose should be selected individually and increased gradually.

With arterial hypertension, the recommended initial dose is 50 mg 1 time / day.
If the therapeutic effect is insufficient, the daily dose can be increased to 100 mg or 200 mg, or additionally, another antihypertensive agent should be prescribed. The maximum daily dose is 200 mg.
With angina, the recommended initial dose is 50 mg 1 time / day.
If the therapeutic effect is insufficient, the daily dose can be increased to 100 mg or 200 mg, or additionally, another antihypertensive agent should be prescribed.
For secondary prevention of myocardial infarction the usual maintenance dose is 200 mg 1 time / day.

With heart failure in the compensation stage, the recommended initial dose is 25 mg 1 time / day.
After 2 weeks, the daily dose can be increased to 50 mg, then two weeks to 100 mg and finally, after 2 weeks - up to 200 mg.
If heart rhythm disturbances are prescribed, 50-200 mg 1 time / day.

With hyperthyroidism, the usual dose is 50-200 mg 1 time / day.

With hyperkinetic cardiac syndrome, the drug is prescribed in a dose of 50-200 mg 1 time / day.

For prevention of migraine attacks, the drug is prescribed in a dose of 100-200 mg 1 time / day.

In elderly patients and patients with renal insufficiency , as well as in patients on hemodialysis, dose adjustment is not required.

In severe hepatic insufficiency, the dose of the drug should be reduced in accordance with the clinical condition of the patient.

Tablets should be taken whole, not liquid, squeezed with liquid.
Tablets can be broken in half.
SIDE EFFECT

Determination of the frequency of adverse reactions: very often (> 1/10);
often (> 1/100, <1/10); sometimes (> 1/1000, <1/100); rarely (> 1/10 000, <1/1000); very rarely (<1/10 000), including individual messages.
From the side of the central nervous system and peripheral nervous system: very often (especially at the beginning of the course of treatment) - increased fatigue, weakness, dizziness and headache;
sometimes - reduced concentration of attention, slowing of the speed of mental and motor reactions, sleep disturbances, drowsiness, insomnia, nightmares, depression, tremors, convulsions, anxiety; rarely - excitability, anxiety, paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome); very rarely - short-term memory loss, confusion and hallucinations, muscle weakness, asthenia, myasthenia gravis.
From the senses: rarely - reduced vision, reduced secretion of tear fluid, dry and painful eyes, conjunctivitis, tinnitus, hearing loss.

From the side of the cardiovascular system: often - excessive reduction in blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness), increased heart rate, sinus bradycardia;
rarely - decreased myocardial contractility, the development of heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), heart rhythm disturbances, manifestation of angiospasm (increased peripheral circulatory disturbance, coldness of the lower limbs, Raynaud's syndrome), impaired myocardial conductivity , cardialgia; very rarely - aggravation of pre-existing violations of AV-conduction.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea;
very rarely - increased activity of hepatic enzymes, hyperbilirubinemia; in some cases - a violation of the liver (dark urine, icteric sclera or skin, cholestasis), changes in taste.
Dermatological reactions: increased sweating;
rarely - rashes on the skin (exacerbation of psoriasis), skin hyperemia, exanthema, reversible alopecia; very rarely - photodermatosis, psoriasis-like skin reactions.
Allergic reactions: urticaria, skin itching, rash.

On the part of the respiratory system: nasal congestion, bronchospasm in high doses (loss of selectivity and / or in predisposed patients), dyspnea.

From the hemopoietic system: very rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.

On the part of metabolism: lowering the level of HDL cholesterol and increasing the level of triglycerides (along with the normal level of total cholesterol), weight gain.

On the part of the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid status.

Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Other: pain in the back or joints, decreased libido and / or potency, with a sharp cessation of treatment - withdrawal syndrome (increased angina attacks, increased blood pressure).

CONTRAINDICATIONS

- cardiogenic shock;

- AV blockade II and III degree;

- Sinoatrial blockade;

- SSSU;

- heart failure in the stage of decompensation;

angiospastic angina (Prinzmetal angina);

- pronounced bradycardia (heart rate <50 bpm);

- arterial hypotension;

- severe violations of peripheral arterial blood circulation;

- lactation period;

- simultaneous administration of MAO inhibitors;

- simultaneous iv injection of verapamil;

- age under 18 years (effectiveness and safety not established);

- Hypersensitivity to metoprolol and other ingredients of the drug.

Due to the limited clinical data, the use of the drug is contraindicated in myocardial infarction under the following conditions: heart rate less than 45 beats per minute, PQ interval exceeds 0.24 seconds, systolic blood pressure less than 100 mmHg, severe heart failure and AV blockade of II or III degree .

With caution should prescribe the drug in diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), obliterating peripheral vascular diseases (intermittent claudication, Raynaud's syndrome), chronic renal and / or hepatic insufficiency, myasthenia gravis, pheochromocytoma, AV-blockade of the first degree, thyrotoxicosis, depression (including in the anamnesis), psoriasis, pregnancy, elderly patients, fructose intolerance, violation of sun
glucose / galactose intake, sugarase / isomaltase insufficiency.
PREGNANCY AND LACTATION

The use of the drug Egilok ® Retard in pregnancy is possible only on strict indications in the event that the intended use for the mother exceeds the potential risk to the fetus.
If it is necessary to prescribe the drug during pregnancy, careful monitoring, especially for the fetus, is necessary, since bradycardia, arterial hypotension, fetal hypoglycemia are possible. Treatment should be interrupted for 48-72 hours before childbirth. In cases where this is not possible, it is necessary to ensure observation of the newborn within 48-72 hours after delivery.
Influence of metoprolol on a newborn during breastfeeding has not been studied, therefore, women taking Egilok® Retard should stop breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution should prescribe the drug for chronic kidney failure.

In elderly patients, patients with impaired renal function , and if hemodialysis is necessary, a change in the dosage regimen is not required.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should prescribe the drug for liver failure.

In patients with impaired liver function, the dose of the drug should be selected individually depending on the clinical condition.

APPLICATION FOR CHILDREN

Contraindicated: age under 18 years (efficacy and safety not established).

APPLICATION IN ELDERLY PATIENTS

Caution should be given to elderly patients.

SPECIAL INSTRUCTIONS

Control of patients taking beta-blockers includes regular monitoring of heart rate and blood pressure, glucose content in patients with diabetes mellitus.
It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at heart rate less than 50 beats per minute. When taking the drug at a dose of more than 200 mg / day decreases the cardioselectivity of metoprolol.
Before the start of treatment, chronic heart failure should be compensated, and the state of compensation should be maintained throughout the treatment process.

It is possible to increase the severity of reactions of hypersensitivity (against a background of an allergic anamnesis) and the absence of the effect of the introduction of medium doses of epinephrine (adrenaline).
In patients taking the drug, anaphylactic shock can occur particularly hard.
The drug can strengthen the existing bradycardia.
In patients receiving beta-adrenoblockers, epinephrine (adrenaline) can raise blood pressure and cause (reflex) bradycardia; this reaction is less likely in the case of selective beta-blockers.
The drug may increase the symptoms of peripheral circulatory disorders.

If it is necessary to prescribe a preparation for a patient with bronchial asthma, simultaneous use of beta 2 -adrenostimulants (changing the dose of previously used beta 2 -adrenostimulants) may be required.

If it is necessary to prescribe the drug to a patient with pheochromocytoma, alpha-adrenoblockers should be used.

Reception of the drug may mask some clinical manifestations of hyperthyroidism (for example, tachycardia).
Sharp abolition in patients with thyrotoxicosis is contraindicated, since it is possible to increase its symptoms.
With angina pectoris, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load - no more than 110 beats per minute.
In smokers, the effectiveness of the drug may be lower.
When prescribing a patient with diabetes mellitus, it should be more often monitored the parameters of carbohydrate metabolism and, if necessary, adjust the dose of insulin and oral hypoglycemic agents.
With diabetes, the drug can mask tachycardia caused by hypoglycemia. Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.
Drugs that reduce the supply of catecholamines (eg, reserpine) may increase the effect of the drug Egilok® Retard, so patients taking such combinations of drugs should be under constant monitoring by the doctor for the detection of excessive lowering of blood pressure and bradycardia.

Patients with severe renal failure are advised to monitor kidney function (1 every 4-5 months).

Bioavailability of metoprolol may increase with cirrhosis of the liver.

In elderly patients it is recommended to regularly monitor liver function.
Correction of the dosing regimen is required only if older bradycardia (less than 50 bpm) appears in patients of advanced age, a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmia, severe impairment of function sometimes it may be necessary to stop treatment.
It is necessary to carry out special monitoring of the condition of patients with depressive disorders in the anamnesis.
In the case of development of depression, Egilok® Retard should be discontinued.
Before any surgical operation, an anesthesiologist should be warned that the patient is taking Egiloc® Retard.
Cancellation of the drug should be carried out at least 48 hours before surgery, except in special cases, such as thyrotoxicosis or pheochromocytoma. In cases where withdrawal of the drug before surgery is not possible, you should choose a means for general anesthesia with a minimum negative inotropic effect.
With the simultaneous use of the drug Egilok ® Retard with clonidine in the case of abolition of Egiloka Retard clonidine should be discontinued after a few days in order to avoid the development of hypertensive crisis.

With a sharp cessation of treatment, withdrawal can occur (increased angina attacks, increased blood pressure), so the drug is canceled gradually, reducing the dose within 10 days.
Particular attention should be given to patients with angina when discontinuing the drug.
Patients who use contact lenses should take into account that against the background of treatment with beta-adrenoblockers, tear production can be reduced.

Taking into account that the preparation contains sucrose, it is not recommended to appoint it to patients with intolerance to fructose, impaired glucose / galactose absorption, as well as insufficiency of sugarase / isomaltase.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

OVERDOSE

Symptoms: marked reduction of blood pressure, expressed severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, arrhythmia, ventricular premature beats, bronchospasm, fainting; in acute overdose - cardiogenic shock, loss of consciousness, coma, AV-block (up to the full development of cross-blockade and heart failure), kardialgiya.
Overdose first symptoms appear after 20 min-2 hr after dosing.
The above symptoms may worsen while taking alcohol, antihypertensive agents, quinidine and barbiturates.
Treatment:Intensive therapy and careful monitoring of the patient (circulatory and respiratory parameters, renal function, blood glucose, serum electrolytes). If the drug has recently adopted, its absorption can be further reduced by washing the stomach, vomiting, stimulation and administration of activated charcoal.
In marked decrease in blood pressure: the patient must be in the Trendelenburg position; in the event of excessive reduction in blood pressure, bradycardia and heart failure should threat in / enter beta adrenostimulyatorov at intervals of 2-5 minutes, to achieve the desired effect or / enter 0.5-2 mg atropine sulfate.
If no sufficient effect should apply dopamine, dobutamine or norepinephrine (noradrenaline).
As a follow-up appointment may glucagon in a dose of 1-10 mg glucagon, setting an artificial pacemaker.
Bronchospasm is possible to stop in / at the introduction of stimulants? 2 -adrenoceptor (e.g., terbutaline).
Metoprolol poorly displayed by hemodialysis


DRUG INTERACTION

With simultaneous use of egilok Retard with MAO inhibitors may be a significant enhancement of the hypotensive action. The interval between administration of MAO inhibitors and egilok Retard should be at least 14 days.
Simultaneous in / with the introduction of verapamil can cause heart failure, co-administration of nifedipine results in significant reduction in blood pressure.
When combined with antihypertensives, diuretics, nitroglycerin or calcium channel blockers may slow develop sharp decrease in blood pressure (special caution is required in combination with prazosin); verapamil, diltiazem, antiarrhythmics (amiodarone), reserpine, methyldopa, clonidine, guanfacine, means for general anesthesia and cardiac glycosides - increasing expression of heart rate deceleration and inhibition of AV-conduction.
Means for inhalation anesthesia (derivatives of hydrocarbons) increase the risk of depression of the myocardium and development of arterial hypotension.
Beta adrenostimulyatorov, theophylline, cocaine, estrogens (sodium retention), indomethacin, and other NSAIDs (cause sodium retention and blockage of prostaglandin synthesis by the kidneys) weaken the hypotensive effect of the drug.
When applied simultaneously with the drug Egilok ® Retard tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), sedatives and hypnotics drugs increase inhibitory effect on the CNS.
When co-administered with the hypoglycemic agents for oral administration may reduce its effect; insulin - increasing the risk of hypoglycemia, increased its intensity and duration, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
Inductors of microsomal liver enzymes (rifampicin, barbiturates) accelerate metabolism of metoprolol, which reduces the concentration of metoprolol in the blood plasma and the reduction effect egilok Retard.
Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) increase the concentration of metoprolol in the blood plasma.
The allergens used for immunotherapy or allergen extracts for skin samples when combined with metoprolol, increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing contrast media for the on / in the increase the risk of anaphylactic reactions.
Metoprolol reduces the clearance of xanthine derivatives, especially with the initially increased clearance of theophylline under the influence of smoking.
Metoprolol reduces the clearance of lidocaine, increases the concentration of lidocaine in the blood plasma.
It strengthens and prolongs the effect of muscle relaxants antidepolyarizuyuschih; It extends the anticoagulant effect of coumarin.
In a joint application with ethanol increases the risk of significant decrease in blood pressure and there is a growing inhibitory action on the central nervous system.
In a joint application with ergot alkaloids is increased risk of peripheral circulatory disorders.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored out of reach of children at a temperature of no higher than 30 ° C.
Shelf life - 5 years. Do not use after the expiration date printed on the package.
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