Egilok tablets 50mg №60

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Egilok tabl 50mg in vial No. 60 in a pack. No. 1
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Tablets are white or almost white, round, biconvex, scored on one side and engraved “E434” on the other side, odorless. The main active ingredient Metoprolol Release form Tablets are white or almost white, round, biconvex, with a score on one side and engraved “E434” on the other side, odorless. Dosage 50mg per vial No. 60 Special instructions When prescribing the drug Egilok®, heart rate and blood pressure should be regularly monitored. The patient should be taught how to calculate the heart rate and should be instructed to consult a doctor if the heart rate is <50 bpm. In patients with diabetes mellitus, blood glucose levels should be regularly monitored and, if necessary, dose adjustment of insulin or oral hypoglycemic drugs should be carried out. 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 increase the severity of hypersensitivity reactions (against the background of a aggravated allergic history) and the lack of effect from the administration of conventional doses of epinephrine (adrenaline). Anaphylactic shock may be more severe in patients taking Egilok®. Against the background of the use of Egilok, the symptoms of peripheral circulatory disorders may worsen. Egilok® should be canceled gradually, consistently reducing its dose within 14 days. With a sharp cessation of treatment, it is possible to increase angina attacks and the risk of developing coronary disorders. During the period of drug withdrawal, patients with coronary artery disease should be under close medical supervision. With angina pectoris, the selected dose of Egilok® should provide heart rate at rest within 55-60 beats / min, with exercise - no more than 110 beats / min. Patients using contact lenses should take into account that against the background of treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible. Egilok® may mask some clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt discontinuation of the drug in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms. In diabetes mellitus, taking Egilok may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels. When prescribing metoprolol to patients with bronchial asthma, the simultaneous use of beta2-agonists is necessary. In patients with pheochromocytoma, Egilok® should be used in combination with alpha-blockers. Before carrying out any surgical intervention, it is necessary to inform the surgeon / anesthesiologist about the ongoing therapy with Egilok (the choice of a drug for general anesthesia with a minimal negative inotropic effect); discontinuation of the drug is not required. Drugs that reduce catecholamine stores (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect excessive reduction in blood pressure or bradycardia. When prescribing the drug to elderly patients, liver function should be regularly monitored. Correction of the dosing regimen is required only in the case of the appearance in elderly patients of increasing bradycardia (<50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure <100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe dysfunction liver. Sometimes it is necessary to stop treatment. Patients with severe renal insufficiency are advised to monitor renal function. Special monitoring of the condition of patients with depressive disorders should be carried out. In case of development of depression caused by the use of beta-blockers, therapy should be discontinued. If progressive bradycardia occurs, the dose should be reduced or the drug discontinued. Use in pediatrics 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. Influence on the ability to drive vehicles and control mechanisms Care must be taken when driving vehicles and when engaging in potentially hazardous activities that require increased concentration of attention (risk of dizziness and increased fatigue). Pharmacological action Cardioselective blocker of α-adrenergic receptors. 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 a standing and lying position. The long-term antihypertensive effect of the drug is associated with a gradual decrease in OPSS. In arterial hypertension, long-term use of the drug leads to a statistically significant decrease in the mass of the left ventricle and an improvement in its diastolic function. In men with mild or 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 blood pressure, heart rate and myocardial contractility. The decrease in heart rate and the corresponding lengthening of diastole when taking metoprolol provide improved blood supply and oxygen uptake by the myocardium with impaired blood flow. Therefore, in angina pectoris, the drug reduces the number, duration and severity of attacks, as well as asymptomatic manifestations of ischemia, and improves the patient's physical performance. In myocardial infarction, metoprolol reduces the mortality rate, reducing the risk of sudden death. This effect is primarily associated with the prevention of episodes of ventricular fibrillation. A decrease in mortality can also be observed with the use of metoprolol in both the 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 re-infarction. In chronic heart failure against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, taken at 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 premature beats, metoprolol reduces the frequency of ventricular contractions and the number of ventricular extrasystoles. At therapeutic doses, the peripheral vasoconstrictor and bronchoconstrictor effects of metoprolol are less pronounced than the same effects of non-selective beta-blockers. Compared with non-selective beta-blockers, metoprolol has less effect on insulin production and carbohydrate metabolism, and 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 blood serum. There is a significant decrease in the total concentration of serum cholesterol after the use of metoprolol for several years. Pharmacokinetics Absorption Metoprolol is rapidly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in the therapeutic dose range. Cmax in plasma is achieved 1.5-2 hours after ingestion. Bioavailability is approximately 50% with a single dose and approximately 70% with regular use. Taking the drug simultaneously with food can increase bioavailability by 30-40%. Distribution Metoprolol is slightly (approximately 5-10%) bound to plasma proteins. Vd is 5.6 l / kg. Metabolism After absorption, metoprolol is largely subjected to the effect of "first pass" through the liver. It is metabolized in the liver by cytochrome P450 isoenzymes. Metabolites do not have pharmacological activity. Withdrawal T1 / 2 averages 3.5 hours (from 1 to 9 hours). The total 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 situations Significant changes in the pharmacokinetics of metoprolol in elderly patients have not been identified. Impaired renal function does not affect the systemic bioavailability or excretion of metoprolol. However, in these cases, there is a decrease in the excretion of metabolites. In severe renal failure (GFR <5 ml / min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade. Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and after portocaval anastomosis, bioavailability may increase and total clearance from the body may decrease. After porto-caval shunting, the total clearance of the drug from the body is approximately 0.3 l / min, and the AUC increases by approximately 6 times compared with that in healthy volunteers. Indications for use - 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 extrasystoles); - hyperthyroidism (as part of complex therapy); - prevention of migraine attacks. Dosage and administration The drug should be taken orally during or regardless of the meal. 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 mild or moderate 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 another antihypertensive agent can be added. With angina pectoris, 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 another antianginal drug can be added. The recommended dose of the drug for maintenance therapy after myocardial infarction is 100-200 mg / day, divided into 2 doses (morning and evening). For 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 another antiarrhythmic agent can be added. In hyperthyroidism, the usual daily dose is 150-200 mg in 3-4 doses. With functional disorders of the heart, accompanied by a sensation of palpitations, 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 the 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. In patients with impaired renal function, no change in dosing regimen is required. With cirrhosis of the liver, a dose change is usually not required due to the low binding of metoprolol to plasma proteins. In severe liver failure (for example, after a portocaval bypass), it may be necessary to reduce the dose of Egilok®. In elderly patients, dose adjustment is not required. Use during pregnancy and lactation The use of the drug is not recommended during pregnancy. The use of the drug is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If it is necessary to prescribe the drug during pregnancy, careful monitoring of the condition of the fetus and newborn within 48-72 hours after delivery is necessary, since bradycardia, arterial hypotension, hypoglycemia and respiratory depression may develop. Despite the fact that when using the drug in therapeutic doses, only a small amount of metoprolol is excreted in breast milk, the condition of the newborn should be monitored (possible bradycardia). The use of the drug during lactation is not recommended. If necessary, the use of the drug Egilok® during lactation should stop breastfeeding. Precautions With caution, the drug should be prescribed for diabetes mellitus; metabolic acidosis; bronchial asthma; COPD; renal/liver failure; myasthenia gravis; pheochromocytoma (when used simultaneously with alpha-blockers); thyrotoxicosis; AV blockade of the 1st degree, depression (including history); psoriasis; obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); pregnancy; during lactation; elderly patients; patients with a burdened allergic history (possible decrease in response to the use of adrenaline). Interaction with other drugs Antihypertensive effects of the drug Egilok® with simultaneous use with other antihypertensive drugs are usually enhanced. In order to avoid arterial hypotension, careful monitoring of patients receiving combinations of such agents 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 slow calcium channel blockers such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. The intravenous administration of calcium channel blockers such as verapamil should be avoided in patients receiving beta-blockers. Combinations requiring caution Oral antiarrhythmic drugs (such as quinidine and amiodarone): risk of developing bradycardia, AV blockade. Cardiac glycosides: risk of developing bradycardia, conduction disturbances; metoprolol does not affect the positive inotropic effect of cardiac glycosides. Other antihypertensive drugs (especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacine groups): risk of developing arterial hypotension and / or bradycardia. Termination of the simultaneous use of metoprolol and clonidine should be started by canceling metoprolol, and then (after a few days) clonidine; if clonidine is discontinued first, a hypertensive crisis may develop. Some drugs that act on the central nervous system (for example, hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol): risk of developing arterial hypotension. Means for anesthesia: the risk of oppression of cardiac activity. Alpha- and beta-sympathomimetics: the risk of developing arterial hypertension, significant bradycardia, the possibility of cardiac arrest. Ergotamine: increased vasoconstrictor effect. Beta2-sympathomimetics: functional antagonism. NSAIDs (eg, indomethacin): possible weakening of the antihypertensive effect. Estrogens: possible decrease in the antihypertensive effect of metoprolol. Oral hypoglycemic agents and insulin: metoprolol may enhance their hypoglycemic effects and mask the symptoms of hypoglycemia. Curare-like muscle relaxants: increased neuromuscular blockade. Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; selective serotonin reuptake inhibitors, for example, paroxetine, fluoxetine and sertraline): it is possible to increase the effects of metoprolol due to an increase in its concentration in blood plasma. Enzyme inducers (rifampicin and barbiturates): the effects of metoprolol may be reduced due to increased hepatic metabolism. The simultaneous use of drugs that block the sympathetic ganglia, or other beta-blockers (for example, eye drops) or MAO inhibitors requires careful medical supervision. Contraindications - cardiogenic shock; - AV block II and III degree; - sinoatrial blockade; - SSSU; - sinus bradycardia (HR<50 bpm); - heart failure in the stage of decompensation; - severe peripheral circulatory disorders; - age up to 18 years (due to lack of sufficient clinical data); - simultaneous intravenous administration of verapamil; - severe form of bronchial asthma; - pheochromocytoma without the 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, Egioloc® is contraindicated in acute myocardial infarction, accompanied by heart rate <45 beats / min, with a PQ interval > 240 ms, and systolic blood pressure <100 mm Hg. Composition In 1 tab. metoprolol tartrate 50 mg Excipients: microcrystalline cellulose - 83 mg, sodium carboxymethyl starch (type A) - 15 mg, colloidal anhydrous silicon dioxide - 4 mg, povidone K90 - 4 mg, magnesium stearate - 8 mg. Overdose Symptoms: marked decrease in blood pressure, sinus bradycardia, AV blockade, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase with simultaneous use with ethanol, antihypertensive drugs, quinidine and barbiturates. The first symptoms of an overdose appear 20 minutes to 2 hours after taking the drug. Treatment: it is necessary to carefully monitor the patient (control of blood pressure, heart rate, respiratory rate, kidney function, blood glucose concentration, blood serum electrolytes) in an intensive care unit. If the drug has been taken recently, gastric lavage with activated charcoal may reduce further absorption of the drug (if lavage is not possible, vomiting can be induced if the patient is conscious). In case of excessive reduction in blood pressure, bradycardia and the threat of heart failure - in / in, with an interval of 2-5 minutes, the introduction of beta-agonists (until the desired effect is achieved) or / in the introduction of 0.5-2 mg of atropine. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine). With hypoglycemia - the introduction of 1-10 mg of glucagon, the installation of a temporary pacemaker. With bronchospasm - the introduction of beta2-agonists. With convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective. Side effects Egilok® is usually well tolerated by patients. Side effects are usually mild and reversible. The side effects listed below have been reported in clinical trials and in the therapeutic use of metoprolol. In some cases, the relationship of an adverse event with the use of the drug has not been reliably established. The side effect frequency parameters listed below 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, palpitations; infrequently - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with myocardial infarction, AV blockade of the first degree; rarely - conduction disturbances, arrhythmia; very rarely - gangrene (in patients with peripheral circulatory disorders). From the respiratory system: often - shortness of breath during 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, impaired liver function. On the part of the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of the course of psoriasis. From the sensory organs: rarely - blurred vision, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, a violation of taste sensations. From the reproductive system: rarely - impotence / sexual dysfunction. Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia. The use of the drug Egilok® should be discontinued if any of the above effects reaches a clinically significant intensity, and its cause cannot be reliably established. Storage conditions Keep out of the reach of children at a temperature of 15 ° to 25 ° C. Buy Egilok tablets 50mg No. 60 Price for Egilok tablets 50mg No. 60