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Active ingredients
Metoprolol
Release form
Pills
Composition
Active ingredient: Metoprolol tartrate Concentration of active ingredient (mg): 50
Pharmacological effect
Cardio selective blocker β-adrenoreceptors. 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 BP. In arterial hypertension, metoprolol lowers blood pressure in patients in a standing or lying position. The long-lasting antihypertensive effect of the drug is associated with a gradual decrease in OPSS. In hypertension, prolonged use of the drug leads to a statistically significant reduction in the mass of the left ventricle and an improvement in its diastolic function. In men with mild or moderate arterial hypertension, metoprolol reduces cardiovascular mortality (especially 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. A decrease in heart rate and a corresponding lengthening of diastole while taking metoprolol provide improved blood supply and oxygen absorption by the myocardium with impaired blood flow. Therefore, with 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 ventricular fibrillation episodes. A decrease in the mortality rate 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-lethal re-infarction. In chronic heart failure on the 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 extrasystoles metoprolol reduces the incidence of ventricular contractions and the number of ventricular peeches carbohydrate metabolism does not increase the duration of bouts of hypoglycemia. Metoprolol causes a slight increase in the concentration of triglycerides and a slight decrease in the concentration of serum free fatty acids. There is a significant decrease in the total serum cholesterol concentration after the use of metoprolol for several years.
Pharmacokinetics
AbsorptionMetoprolol is rapidly and completely absorbed from the gastrointestinal tract. The drug is characterized by linear pharmacokinetics in a therapeutic dose range. Cmax in plasma is reached within 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 the bioavailability by 30-40%. DistributionMethoprolol slightly (about 5-10%) binds to plasma proteins. Vd is 5.6 l / kg. Metabolism After absorption, metoprolol is largely exposed to the effect of first passing through the liver. Metabolized in the liver by cytochrome P450 isoenzymes. Metabolites do not possess pharmacological activity. Withdrawal of T1 / 2 averages 3.5 hours (from 1 to 9 hours). Total clearance is approximately 1 l / min. Approximately 95% of the administered dose is excreted by the kidneys, 5% as unchanged metoprolol. In some cases, this value can reach 30%. Pharmacokinetics in special clinical situations No significant changes in the pharmacokinetics of metoprolol in elderly patients have been identified. Disruption of renal function does not affect systemic bioavailability or excretion of metoprolol. However, in these cases, there is a decrease in metabolite excretion. In severe renal failure (GFR <5 ml / min), a significant accumulation of metabolites is observed. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade. Violation of liver function does not significantly affect the pharmacokinetics of metoprolol. However, in severe cirrhosis of the liver and after applying a portocaval anastomosis, bioavailability may increase, and the total clearance from the body may decrease.After portocaval shunting, the total clearance of the drug from the body is about 0.3 l / min, and the AUC increases by about 6 times compared with that in healthy volunteers.
Indications
- arterial hypertension (in monotherapy or in combination with other antihypertensive drugs) - chronic heart failure in the compensation stage (in addition to standard therapy with diuretics, ACE inhibitors, cardiac glycosides); - IHD (secondary prevention of myocardial infarction, prevention of angina attacks); - cardiac arrhythmias (supraventricular arrhythmias, ventricular extrasystoles); - hyperkinetic cardiac syndrome; - hyperthyroidism (as part of complex therapy); - prevention of seizure attacks moment reni.
Contraindications
- cardiogenic shock; - AV blockade of grade II and III; - sinoatrial blockade; - SSS; severe bradycardia (heart rate less than 50 beats / min); heart failure in the stage of decompensation; angiospastic angina (Prinzmetal angina); - severe arterial hypotension (systolic blood pressure below 100 mm Hg); - lactation period; - simultaneous administration of MAO inhibitors; - simultaneous intravenous administration of verapamil; - hypersensitivity to metoprolol and other ingredients of the drug. ibete, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), peripheral vascular disease obliterans (intermittent claudication, Raynaud's syndrome), hepatic failure, chronic renal failure, myasthenia, pheochromocytoma, AV-block, pheochromocytoma, AV-block failure, chronic renal failure, myasthenia, pheochromocytoma, AV-block, pheochromocytoma, AV-block failure, chronic renal failure, myasthenia, pheochromocytoma, AV-block failure, chronic renal failure thyrotoxicosis, depression (including history), psoriasis, as well as in children and adolescents under the age of 18 years and in elderly patients.
Precautionary measures
Precautions should be prescribed the drug for diabetes; metabolic acidosis; bronchial asthma; COPD; renal / hepatic failure; myasthenia; pheochromocytoma (with simultaneous use with alpha-blockers); thyrotoxicosis; AV-blockade of I degree, depression (including in history); psoriasis; peripheral vascular disease obliterans (intermittent claudication, Raynaud's syndrome); pregnancy; during lactation; elderly patients; patients with a history of allergic history (a decrease in response is possible when using adrenaline).
Use during pregnancy and lactation
The use of the drug is not recommended during pregnancy.The use of the drug is possible only in the case when the intended benefit to the mother outweighs the potential risk to the fetus. If necessary, the appointment of the drug during pregnancy requires careful monitoring of the condition of the fetus and newborn for 48-72 hours after delivery, since bradycardia, hypotension, hypoglycemia and respiratory depression are possible. Despite the fact that when using the drug in therapeutic doses, only a small amount Metoprolol is excreted in breast milk; the condition of the newborn should be monitored (bradycardia is possible). The use of the drug during lactation is not recommended. If necessary, the use of the drug Egilok during lactation should stop breastfeeding.
Dosage and administration
Egilok is prescribed for arterial hypertension in a daily dose of 50-100 mg / day in 1 or 2 doses. With insufficient therapeutic effect, it is possible to gradually increase the daily dose to 100-200 mg. For angina, supraventricular arrhythmias, for the prevention of migraine attacks, it is prescribed in a dose of 100-200 mg / day in 2 doses (in the morning and in the evening). For secondary prevention of myocardial infarction, The average daily dose of 200 mg in 2 doses (morning and evening). For functional disorders of cardiac activity, accompanied by tachycardia, a daily dose of 100 mg is prescribed in 2 doses (in the morning and evening). Tablets should be taken orally during or immediately after a meal. Tablets can be divided in half, but not chewed.
Side effects
On the part of the central nervous system and peripheral nervous system: fatigue, weakness, headache, slowing down the speed of mental and motor reactions; rarely - paresthesias in the limbs, depression, anxiety, decreased ability to concentrate, drowsiness, insomnia, nightmares, confusion or short-term memory impairment, asthenic syndrome, muscular weakness. On the part of the senses: rarely - decreased vision, reduced secretion of the lacrimal fluid , xerophthalmos, conjunctivitis, tinnitus. On the side of the cardiovascular system: sinus bradycardia, palpitations, lowering blood pressure, orthostatic hypotension; rarely - a decrease in myocardial contractility,temporary exacerbation of symptoms of chronic heart failure, arrhythmias, increased disorders of the peripheral circulation (cooling of the lower extremities, Raynaud's syndrome), myocardial conduction disorders; in rare cases - AV-blockade, cardialgia. On the part of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, dry mouth, change in taste; increased activity of hepatic transaminases; rarely - hyperbilirubinemia. Dermatological reactions: urticaria, pruritus, rash, exacerbation of psoriasis, psoriasis-like skin changes, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia. On the respiratory system: nasal obstruction, exhalation, reversible alopecia. doses or in predisposed patients), shortness of breath. From the endocrine system: hypoglycemia (in patients receiving insulin); rarely - hyperglycemia. From the hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia. Others: back or joint pain, slight increase in body weight, decreased libido and / or potency.
Overdose
Symptoms: pronounced 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 worsen with simultaneous use with ethanol, antihypertensive drugs, quinidine and barbiturates. The first symptoms of overdose appear 20 minutes to 2 hours after taking the drug. Treatment: careful monitoring of the patient is necessary (control of blood pressure, heart rate, respiratory rate, kidney function , the concentration of glucose in the blood, serum electrolytes) in the conditions of the intensive care unit. If the drug has been taken recently, gastric lavage with activated carbon may reduce further absorption of the drug (if washing is not possible, vomiting can be caused if the patient is conscious). In case of excessive reduction of blood pressure, bradycardia and the threat of heart failure - in / in, with an interval of 2-5 minutes, the introduction of beta-adrenomimetics (to achieve the desired effect) or in / in the introduction of 0.5-2 mg of atropine. In the absence of a positive effect - dopamine, dobutamine or norepinephrine (norepinephrine).In hypoglycemia - the introduction of 1-10 mg of glucagon, the installation of a temporary pacemaker. In case of bronchospasm - administration of beta2-adrenomimetics. For convulsions, slow i.v. administration of diazepam. Hemodialysis is ineffective.
Interaction with other drugs
The antihypertensive effects of Egilok with simultaneous use with other antihypertensive drugs usually increase. In order to avoid arterial hypotension, careful monitoring of patients receiving combinations of such agents is necessary. However, summing up the effects of antihypertensive drugs can, if necessary, be used to achieve effective BP control. Simultaneous use of metoprolol and slow calcium channel blockers such as diltiazem and verapamil can lead to increased negative inotropic and chronotropic effects. Injections 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, disorders of; Metoprolol does not affect the positive inotropic effect of cardiac glycosides. Other antihypertensive drugs (especially the guanethidine, reserpine, alpha-methyldopa, clonidine and guanfacin groups): the risk of arterial hypotension and / or bradycardia. and then (after a few days) clonidine; if you first cancel clonidine, a hypertensive crisis may develop. Some drugs acting on the CNS (for example, hypnotics, tranquilizers, tri- and tetracyclic antidepressants, antipsychotics and ethanol): the risk of arterial hypotension. Anesthesia: anesthesia risk, cardiac activity. and beta sympathomimetics: the risk of arterial hypertension, significant bradycardia, the possibility of cardiac arrest. Ergotamine: increased vasoconstrictor effect. Beta 2 sympathomimetics: functional antagonism. H The sun (eg, indomethacin) may weaken the antihypertensive effekta.Estrogeny: may reduce the antihypertensive effectMetoprolol. Hypoglycemic agents for ingestion and insulin: Metoprolol can enhance their hypoglycemic effects and mask the symptoms of hypoglycemia. Kurarepodobirovye muscle relaxants: increased neuromuscular blockade. Enzyme inhibitors (for example, cimetidine, ethanol, hydralazine; , fluoxetine and sertraline): possible enhancement of the effects of metoprolol due to an increase in its concentration in the blood plasma. Enzyme inducers (rifampicin and barbiturates): the effects of me Toprolol may decrease due to increased hepatic metabolism. Simultaneous use of agents blocking the sympathetic ganglia, or other beta-blockers (eg, eye drops) or MAO inhibitors requires careful medical observation.
special instructions
In the appointment of the drug Egilok should regularly monitor heart rate and blood pressure. Patients should be trained in how to calculate heart rate and instruct on the need for medical consultation with heart rate <50 beats / min. Patients with diabetes should regularly monitor their blood glucose levels and, if necessary, adjust the dose of insulin or oral hypoglycemic drugs. cardioselectivity decreases in excess of 200 mg / day. The appointment of Egilok to patients with chronic heart failure is possible only after reaching the stage of compensation. In patients who have Egilok, may increase the severity of hypersensitivity reactions (on the background of burdened allergological history) and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline). Anaphylactic shock may be more difficult in patients taking Egilok. should be abolished gradually, consistently reducing its dose within 14 days. With a sharp cessation of treatment may increase angina attacks and the risk of developing coronary disorders. During the period of discontinuation of the drug in patients with coronary artery disease, it is necessary to be under close medical supervision. When exertional angina, the selected dose of Egilok should provide heart rate at rest within 55-60 beats / min, with a load not more than 110 beats / min. Patients contact lenses should considerthat during treatment with beta-adrenergic blockers, there may be a decrease in the production of tear fluid. Egilok may mask some clinical manifestations of hyperthyroidism (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, because it can enhance the symptoms. In diabetes mellitus, Egilok may mask tachycardia caused by hypoglycemia. Unlike non-selective beta-adrenergic blockers, insulin-induced hypoglycemia practically does not increase and does not delay recovery of blood glucose concentration to normal levels. When metoprolol is prescribed to patients with bronchial asthma, simultaneous use of beta2-adrenomimetic is necessary. Patients with pheochromocytoma Egilok should be used in combination with alpha adrenergic blockers. Before performing any surgical intervention, it is necessary to inform the surgeon / anesthesiologist about the therapy Egilok m (the choice of drug for general anesthesia with minimal negative inotropic action); drug withdrawal is not required. Drugs that reduce catecholamine reserves (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 blood pressure or bradycardia. When prescribing the drug to elderly patients age should regularly monitor liver function. Correction of the dosing regimen is required only in case of an increase in bradycardia (<50 beats / min) in elderly patients, a pronounced decrease in blood pressure (systolic blood pressure <100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe dysfunction the liver. Sometimes it is necessary to discontinue treatment. Patients with severe renal failure are advised to monitor their renal function. Special monitoring of patients with depressive disorders should be carried out. In the case of the development of depression caused by the use of beta-blockers, therapy should be discontinued. If progressive bradycardia occurs, reduce the dose or discontinue the drug.