Instruction for use: Egilok

Trade name of the drug – Egilok

Dosage Form: tablets

Active substance:Metoprololum

ATX

C07AB02 Metoprolol

Pharmacotherapeutic group: Beta1-selective blocker [Beta-blockers]

The nosological classification (ICD-10)

E05 Thyrotoxicosis [hyperthyroidism]: Von Basedow's disease; Basedow's disease; hyperthyroidism; Goitre diffuse toxic; Increased thyroid function; tireotoksicski reaction; Toxic diffuse goiter; goiter; Enlargement of the thyroid gland with symptoms of hyperthyroidism; The phenomenon of iodine Basedow

G43 Migraine: The pain of migraine; Migraine; hemiplegic migraine; Migraine headache; A migraine attack; Continuous headache; hemicrania

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

I20 Angina [angina]: Heberden disease; Angina pectoris; The attack of angina pectoris; recurrent angina; Spontaneous angina; Stable angina pectoris; Angina rest; Angina progressing; Angina mixed; Angina spontaneous; stable angina; Chronic stable angina; Angina Syndrome X

I25.2 Transferred last myocardial infarction: Cardiac syndrome; Myocardial infarction; post-MI; Rehabilitation after myocardial infarction; Reocclusion of the operated vessel; Angina postinfarctnaya; Status after myocardial infarction; Status after myocardial infarction; myocardial infarction

I25.9 Chronic ischemic heart disease, unspecified: CHD; Insufficiency of coronary circulation; Coronary atherosclerosis in patients with coronary artery disease

I47.1 Supraventricular tachycardia: Supraventricular paroxysmal tachycardia; supraventricular tachyarrhythmia; supraventricular tachycardia; Supraventricular arrhythmias; Supraventricular paroxysmal tachycardia; supraventricular tachyarrhythmias; supraventricular tachycardia; Neurogenic sinus tachycardia; orthodromic tachycardia; Paroxysmal supraventricular tachycardia; Paroxysm of supraventricular tachycardia; Paroxysm of supraventricular tachycardia with WPW-syndrome; Paroxysm of atrial tachycardia; Paroxysmal supraventricular tachyarrhythmia; Paroxysmal supraventricular tachycardia; Politopnye atrial tachycardia; Atrial fibrillation; Atrial tachycardia is true; Atrial tachycardia; Atrial tachycardia with AV block; reperfusion arrhythmias; Reflex Bertsolda-Jarisch; Recurrent sustained supraventricular paroxysmal tachycardia; Symptomatic ventricular tachycardia; Sinus tachycardia; Supraventricular paroxysmal tachycardia; supraventricular tachyarrhythmia; supraventricular tachycardia; supraventricular arrhythmia; supraventricular arrhythmias; Tachycardia of AV connections; supraventricular tachycardia; Tachycardia orthodromic; sinus tachycardia; The nodal tachycardia; Chaotic atrial tachycardia politopnye; Wolff-Parkinson-White

I49.3 Premature ventricular depolarization: Asynergia left ventricle; ventricular Arrhythmia; Pronounced PVCs; fibrillation; ventricular beat; ventricular beat; Ventricular arrhythmias; ventricular beat; Paroxysmal ventricular arrythmia; Recurrent ventricular arrhythmias; ventricular premature beats; Asynergia ventricular

R00.0 Unspecified Tachycardia: Tachycardia

Composition (per tablet): active substance: metoprolol tartrate 25 mg, 50 mg, 100 mg

Other ingredients: MCC - 41.5 / 83/166 mg; sodium carboxymethylstarch (type A) - 7.5 / 15/30 mg; Colloidal anhydrous silica - 2/4/8 mg; povidone (K90) - 2/4/8 mg; magnesium stearate - 2/4/8 mg

Description

Tablets 25 mg: white or almost white, round, biconcave, with cross a dividing line and double-bevel (a form of "double SNEP") on one side and engraved "E 435" - on the other, odorless.

Tablets 50 mg: white or almost white, round, biconcave, with Valium on one party and chasing "E 434" - on the other, odorless.

Tablets 100 mg: white or almost white, round, biconvex, with a facet, with Valium on one party and chasing "E 432" - on the other, odorless.

Pharmacological Properties of Egilok

Pharmachologic effect - antianginal, hypotensive, antiarrhythmic, beta1-adrenoceptor blocking.

Pharmacodynamics

Mechanism of action

Metoprolol inhibits the hyperactivity of the sympathetic system effect on the heart and causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure.

standing and lying When hypertension metoprolol reduces blood pressure in patients in the state. Long antihypertensive effect of the drug is associated with a gradual decrease in systemic vascular resistance.

When hypertension long-term use of the drug leads to a statistically significant reduction in left ventricular mass and improve diastolic function. Men with mild to moderate hypertension metoprolol reduced mortality from cardiovascular causes (especially sudden death, fatal and non-fatal heart attack and stroke).

Like other beta-blockers, metoprolol reduces myocardial oxygen demand by reducing the systemic blood pressure, heart rate and myocardial contractility. Reduced heart rate and corresponding lengthening of diastole when taking metoprolol provide improved blood flow and myocardial oxygen uptake with impaired blood flow. Therefore, drug for angina reduces the number, duration and severity of attacks, but also displays asymptomatic ischemia and improves the patient's physical performance.

In myocardial infarction, metoprolol lowers mortality, reducing the risk of sudden death. This effect is primarily related to the prevention of ventricular fibrillation episodes. Reducing the mortality rate can also be observed in the application of metoprolol in the early and in the late phase of myocardial infarction, as well as in high-risk patients and patients with diabetes mellitus. Use of the drug after myocardial infarction reduces the likelihood of nonfatal reinfarction.

In CHF, against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, starting with a low dose (2 × 5 mg / day) with gradual dose escalation, improves heart function, quality of life and physical endurance of the patient.

If supraventricular tachycardia, atrial fibrillation and ventricular arrhythmias, metoprolol reduces the incidence of ventricular rate and the number of PVCs.

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

Compared with non-selective beta-blockers, metoprolol 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 small decrease in the concentration of serum free fatty acids. There is a significant decrease in total cholesterol concentration of the blood serum after several years of metoprolol.

Pharmacokinetics

Metoprolol is rapidly and completely absorbed in the digestive tract. For the drug is characterized by linear pharmacokinetics in the therapeutic dose range.

Cmax plasma levels achieved in 1.5-2 hours after oral administration. After absorption metoprolol largely metabolized first pass through the liver. The bioavailability of metoprolol is approximately 50% with single and approximately 70% when taken regularly.

Receiving simultaneously with food can increase the bioavailability of metoprolol is 30-40%. Metoprolol slightly (~ 5-10%) bound to plasma proteins. Vd is 5.6 L / kg. Metoprolol is metabolised in the liver by cytochrome P450 isoenzymes. Metabolites not possess pharmacological activity. T1 / 2 on average - 3.5 hours (from 1 to 9 hours). The total clearance is approximately 1 l / min. Approximately 95% of the administered dose excreted by the kidneys, 5% - metoprolol as unchanged. In some cases, this value can reach 30%.

There were no significant changes in the pharmacokinetics have been identified in older patients.

Renal impairment does not affect the systemic bioavailability and elimination of metoprolol. However, in these cases, a decrease in the excretion of metabolites. In severe renal insufficiency (glomerular filtration rate of less than 5 ml / min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the level of beta-adrenergic blockade.

Abnormal liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after the imposition of portocaval shunt the bioavailability may increase and the total clearance from the body down. After grafting portocaval total clearance of the drug from the body is approximately 0.3 liters / min, and AUC increased about six times compared with that in healthy volunteers.

Indications for Egilok

hypertension (in monotherapy or (if required) in combination with other antihypertensive drugs);

Coronary heart disease: heart attack (secondary prevention - complex therapy), prevention of angina attacks;

cardiac arrhythmias (supraventricular tachycardia, ventricular premature beats);

functional cardiac abnormalities, accompanied by tachycardia;

Hyperthyroidism (complex therapy);

prevention of migraine attacks.

Contraindications for Egilok

Hypersensitivity to metoprolol or any other component of the drug, as well as other beta-blockers;

atrioventricular (AV) block II or III degree;

sinoatrial block;

sinus bradycardia (heart rate less than 50 beats / min.);

syndrome sick sinus;

cardiogenic shock;

severe peripheral circulatory disorders;

heart failure in the stage of decompensation;

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

simultaneous in / with the introduction of verapamil;

severe bronchial asthma;

pheochromocytoma without simultaneous use of alpha-blockers.

Due to the lack of clinical data Egilok® contraindicated in acute myocardial infarction accompanied by heart rate below 45 beats. / Min, with the PQ interval of 240 ms and a garden below 100 mm Hg. Art.

Precautions: diabetes mellitus; metabolic acidosis; bronchial asthma; COPD; renal / hepatic impairment; myasthenia gravis; pheochromocytoma (while the use of alpha-blockers); hyperthyroidism; AV block of I degree; depression (including history); psoriasis; obliterating peripheral vascular disease (intermittent claudication, Raynaud's syndrome); pregnancy; lactation; elderly age; Patients with allergic history (may decrease the response in the application of adrenaline).

Pregnancy and breast-feeding

Use of the drug is not recommended during pregnancy. Use of the drug is possible only when the benefit to the mother outweighs the potential risk to the fetus. If the drug is required, should be monitored closely for the fruit, and then the newborn for a few days (48-72 hours) after birth, because Perhaps the development of bradycardia, respiratory depression, decreased blood pressure and hypoglycemia.

Despite the fact that the therapeutic dose of metoprolol only small quantities of the drug are allocated in breast milk, newborn should be kept under surveillance (available bradycardia). Use of the drug during lactation is not recommended. If necessary, use during lactation should stop breastfeeding.

Side effect of Egilok

Egilok® generally well tolerated by patients. Side effects are usually mild and reversible. The following side effects reported in clinical trials and therapeutic use of metoprolol. In some cases, the connection adverse event with use of the drug did not significantly set. The following parameters of the frequency of side effects are defined as follows: very common (≥10%); often (1-9,9%); rare (0.1-0.9%); rare (0,01-0,09%); very rare, including isolated reports (≤0,01%).

From the nervous system: very often - fatigue; often - dizziness, headache; rarely - increased irritability, anxiety, impotence / sexual dysfunction; rarely - paresthesia, convulsions, depression, poor concentration, drowsiness, insomnia, nightmares; very rarely - Amnesia / memory impairment, depression, hallucinations.

From the CCC: often - bradycardia, orthostatic hypotension (in some cases, possible syncope), cooling of the lower extremities, palpitations; infrequently - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV block of I degree; rarely - conduction disorders, arrhythmias; very rarely - gangrene (in patients with impaired peripheral circulation).

From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; rarely - vomiting; rare - dryness of the oral mucosa, the liver.

For the skin: rarely - urticaria, increased sweating; rare - alopecia; very rarely - photosensitivity, exacerbation of psoriasis flow.

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

From the sensory organs: rarely - blurred vision, dry and / or irritated eyes, conjunctivitis; very rarely - ringing in the ears, impaired sense of taste.

Other: rarely - weight gain; very rarely - arthralgia, thrombocytopenia.

Receiving Egilok® drug should be terminated if any of the above effects, clinically significant intensity reaches and its cause cannot be determined reliably.

Interaction

Antihypertensive effects Egilok® preparation and other antihypertensive drugs when used together usually amplified. To avoid hypotension, careful monitoring of patients receiving the combination of such agents. However, summation of the effects of antihypertensive drugs can, if necessary, to use in order to achieve effective control of blood pressure.

The simultaneous use of metoprolol and BCCI type diltiazem and verapamil may lead to increased negative inotropic and chronotropic effects. Avoid on / in the BCCI type of verapamil in patients receiving beta-blockers.

Care should be taken while taking the following means

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

Cardiac glycosides (risk of bradycardia, conduction disturbances, metoprolol does not affect the positive inotropic effect of cardiac glycosides).

Other antihypertensives (especially guanethidine group, reserpine, alpha-methyldopa, clonidine and guanfatsina) - because of the risk of hypotension and / or bradycardia.

Termination of simultaneously receiving metoprolol and clonidine should always start by canceling metoprolol, and then (a few days) clonidine; if the first cancel clonidine may develop a hypertensive crisis.

Some drugs acting on the CNS, such as hypnotics, anxiolytics, tri- and tetracyclic antidepressants, antipsychotics and ethanol, increase the risk of hypotension.

Means for anesthesia (risk of cardiac depression).

Alpha and beta sympathomimetics (risk of hypertension, significant bradycardia; the possibility of cardiac arrest).

Ergotamine (increased vasoconstrictor effect).

Beta1-sympathomimetic (functional antagonism).

NSAIDs (eg, indomethacin) - may reduce the antihypertensive effect.

Estrogens (may reduce the antihypertensive effect of metoprolol).

Hypoglycemic agents and oral insulin (metoprolol may enhance hypoglycemic effects and masked symptoms of hypoglycemia).

Curariform muscle relaxants (increased neuromuscular blockade).

Enzyme inhibitors (eg cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, such as paroxetine, fluoxetine and sertraline) - metoprolol strengthening effects due to the increase of its concentration in blood plasma.

Enzyme inducers (rifampicin and barbiturates): Effects of metoprolol may be reduced due to increased hepatic metabolism.

Concomitant use of agents that block the sympathetic ganglia, or other beta-blockers (eg eye drops) or MAO inhibitors requires careful medical supervision.

Dosage and Administration

Inside, Egilok® tablets can be taken with food or without regard to food. If necessary, the tablet can break in half.

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

Recommended dose

Arterial hypertension. In mild to moderate hypertension initial dose - 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. Starting dose - 25-50 mg two to three times per day. Depending on the effect, the dose can be gradually increased up to 200 mg per day, or add other antianginal drug.

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

Cardiac arrhythmias. Initial dose - from 25 to 50 mg twice or three times a day. If necessary, the daily dose can be gradually increased up to 200 mg / day, or add another antiarrhythmic agent.

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

Functional disorders of the heart, accompanied by 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.

Prophylaxis of migraine attacks. A typical 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

If the kidney function change the dosing regimen is required.

In cirrhosis of the liver usually does not require dose changes due to low binding of metoprolol plasma proteins (5-10%). In severe hepatic failure (e.g. portocaval bypass surgery) it may be necessary to reduce the dose of the drug Egilok®.

In elderly patients a dose adjustment is required.

Overdose

Symptoms: marked reduction of blood pressure, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma.

The above symptoms may worsen while taking ethanol, antihypertensive agents, quinidine and barbiturates.

The first signs appear overdose 20 min - 2 h after dosing.

Treatment: careful observation of the patient (control of blood pressure, heart rate, respiratory rate, renal function, blood glucose, electrolytes, serum) under conditions of 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 of blood pressure, bradycardia, and the threat of heart failure - I / O, with an interval of 2-5 minutes are appointed by beta-agonists - to achieve the desired effect or / injected 0.5-2 mg atropine. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (noradrenaline). When hypoglycemia - the introduction of 1-10 mg of glucagon; installing a temporary pacemaker. When bronchospasm enter beta2-agonists. In convulsions - slow in / diazepam. Hemodialysis is ineffective.

Special instructions

Control patients taking beta-blockers, includes regular measurement of heart rate and blood pressure, blood glucose in diabetic patients. If necessary, the dose of insulin for patients with diabetes or hypoglycemic agents for oral administration should be adjusted individually. It is necessary to train the patient's heart rate calculation method and instruct on the need of medical advice in heart rate less than 50 bpm. / Min. When receiving doses greater than 200 mg per day cardioselective decreases.

In heart failure, treatment with Egilok® begin only after the compensation stage of heart function.

Perhaps the increased severity of hypersensitivity reactions and the lack of effect of the introduction of the usual doses of epinephrine (adrenaline) in patients with allergic history.

Anaphylaxis may be more severe in patients taking Egilok®.

May exacerbate symptoms of peripheral arterial circulation.

Avoid abrupt discontinuation of the drug Egilok®. The drug should be lifted gradually by reducing the dose within about 14 days. Abrupt withdrawal may intensify symptoms of angina and increase the risk of coronary events. Particular attention should be paid to drug discontinuation in patients with coronary artery disease.

When angina selected dose Egilok® should provide resting heart rate in the range of 55-60 beats / min under load -. Not more than 110 beats / min..

Patients who use contact lenses should bear in mind that during treatment with beta-blockers may reduce the production of tear fluid.

Egilok® can mask some of the clinical manifestations of hyperthyroidism (eg tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because the symptoms can increase.

In diabetes may mask tachycardia caused by hypoglycemia. In contrast, nonselective beta-blockers, almost no increase insulin-induced hypoglycemia and delay recovery of blood glucose to normal levels. In the case of the appointment of the drug Egilok® diabetics should control the concentration of blood glucose and, if necessary, correct the dose of insulin or hypoglycemic agents for oral administration ( "Interaction" cm.).

The appointment to patients with bronchial asthma as a concomitant therapy using beta2-adrenostimulyatorov; in pheochromocytoma - alpha-blockers.

When the need for surgical intervention must notify the surgeon / anesthetist on therapy (means choice for general anesthesia with minimal negative inotropic effects), removal of the drug is not recommended.

Drugs that reduce the reserves of catecholamines (eg reserpine), may enhance the effect of beta-blockers, so patients taking these combinations of drugs should be under constant supervision of a physician to identify excessive reduction of blood pressure or bradycardia.

Elderly patients are advised to regularly monitor liver function. Correction of dosage regimen is required only in the case of elderly patients increasing bradycardia (less than 50 beats / min.), Expressed reduce blood pressure (SBP below 100 mm Hg..), The AV blockade bronchospasm, ventricular arrhythmias, severe liver dysfunction; it is sometimes necessary to discontinue treatment. Patients with severe renal impairment is recommended to monitor renal function.

It is necessary to carry out special monitoring of patients with depressive disorders taking metoprolol; in the case of depression, caused by the intake of beta-blockers, it is recommended to discontinue therapy.

In the event of progressive bradycardia should reduce the dose or stop taking the drug.

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

Effects on ability to drive and use machines. Be careful when driving and occupations potentially hazardous activities that require high concentration (the risk of dizziness and fatigue).

Release Form

Tablets, 25 mg. According to Table 60. brown glass vial with PE-cap with a cushion-like an accordion, with the control of the first opening. 1 fl. in a cardboard bundle. Or at Table 20. in a blister made of PVC / PVDC // Aluminum Foil. 3 blisters in a carton box.

Tablets, 50 mg. According to Table 60. brown glass vial with PE-cap with a cushion-like an accordion, with the control of the first opening. 1 fl. in a cardboard bundle. Or at Table 15. in a blister made of PVC / PVDC // Aluminum Foil. 4 blisters in a carton box.

Tablets, 100 mg. 30 or Table 60. brown glass vial with PE-cap with a cushion-like an accordion, with the control of the first opening. 1 fl. in a cardboard bundle.

Manufacturer

CJSC "Pharmaceutical plant EGIS." 1106 Budapest, ul. Keresturi, 30-38, Hungary.

Representative office of JSC "Pharmaceutical plant EGIS" (Hungary) in Moscow. 121108, Moscow, ul. Ivan Franko, 8.

In the case of packaging and packing of the drug in Russia further stated:

Pre-packaged, packed: SERDIKS LLC. 142150, Russia, Moscow region., Podolsky district, d. Sofyino, p. 1/1.

Conditions of supply of pharmacies

On prescription.

Storage conditions of Egilok

At a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life

5 years.

Do not use beyond the expiration date printed on the package.