Metocard tablets 100mg №10×3

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Metocard tablets 100 mg in a blister. in pack. No. 10х3
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Tablets of white color, round, biconvex, with dividing risk. The main active ingredient of metoprolol tartrate Release form Tablets Dosage 100 mg If necessary, the dose of insulin or oral hypoglycemic drugs for patients with diabetes should be adjusted individually. The patient should be taught how to calculate heart rate and should be instructed to consult a doctor if the heart rate is less than 50 bpm. When taking a dose above 200 mg / day, cardioselectivity decreases. In heart failure, treatment with metoprolol is started only after reaching the stage of compensation. It is possible to increase the severity of hypersensitivity reactions (against the background of a burdened allergic history) and the lack of effect from the administration of conventional doses of epinephrine (adrenaline). Against the background of taking Metocard, symptoms of peripheral arterial circulation disorders may increase. Cancellation of the drug is carried out gradually, reducing the dose within 10 days. With a sharp cessation of treatment, a withdrawal syndrome may occur (increased angina attacks, increased blood pressure). Particular attention should be paid to patients with angina pectoris when discontinuing the drug. With angina pectoris, the selected dose of the drug should provide heart rate at rest within the range of 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. Metoprolol may mask some of the clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms. In diabetes mellitus, Metocard 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. If it is necessary to prescribe to patients with bronchial asthma, β2-adrenergic stimulants are used as concomitant therapy; with pheochromocytoma – alpha-blockers. If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being carried out (the choice of a general anesthesia agent with a minimal negative inotropic effect), drug withdrawal is not recommended. Drugs that reduce catecholamine stores (for example, reserpine) can enhance 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 and bradycardia. In elderly patients, regular monitoring of liver function is recommended. Correction of the dosing regimen is required only if an elderly patient develops increasing bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver dysfunction 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 taking metoprolol should be carried out; in case of development of depression caused by taking beta-blockers, it is recommended to stop therapy. Use in pediatrics The safety and efficacy of the drug in children and adolescents under the age of 18 years has not been established. Influence on the ability to drive vehicles and control mechanisms At the beginning of treatment with metoprolol, patients may experience dizziness, fatigue. In this case, they should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions. In the future, this issue should be resolved after assessing the patient’s individual response to therapy. Pharmacological action Cardioselective beta1-adrenergic blocker, which does not have internal sympathomimetic activity and membrane stabilizing properties. It has antihypertensive, antianginal, antiarrhythmic effect. By blocking β1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces intracellular Ca2+ current, has a negative chrono-, dromo-, batmo-, and inotropic effect (slows heart rate, inhibits conductivity and excitability, reduces myocardial contractility). OPSS at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) – increases (as a result of a reciprocal increase in the activity of α-adrenergic receptors and the elimination of stimulation of β2-adrenergic receptors), which after 1-3 days returns to the original, and with long-term administration – decreases. The acute antihypertensive effect is due to a decrease in cardiac output, a stable antihypertensive effect develops within 2-3 weeks and is due to a decrease in renin synthesis and accumulation of plasma renin, inhibition of the activity of the renin-angiotensin system (it is of great importance in patients with initial renin hypersecretion) and the central nervous system, restoration of sensitivity baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences. Reduces high blood pressure at rest, during physical exertion and stress. Blood pressure decreases after 15 minutes, maximum – after 2 hours and the decrease continues for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular intake. The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening of diastole and improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance. The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in atrioventricular conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through AV node) and additional pathways. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart disease and hyperthyroidism, the drug slows down the heart rate or may even lead to the restoration of sinus rhythm. Prevents the development of migraine. When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on organs containing β2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism. When used in high doses (more than 100 mg / day), it has a blocking effect on both subtypes of β-adrenergic receptors. Pharmacokinetics Absorption After oral administration, it is rapidly and almost completely (95%) absorbed from the gastrointestinal tract. Cmax metoprolol in blood plasma is achieved 1-2 hours after ingestion. Bioavailability is 50% at the first dose and increases to 70% with repeated use. Eating increases bioavailability by 20-40%. Distribution Plasma protein binding averages 10%. Penetrates through the BBB and the placental barrier. It is excreted in breast milk in small amounts. Metabolism Biotransformed in the liver. Metabolites do not have pharmacological activity. Withdrawal T1 / 2 averages 3.5 hours (from 1 to 9 hours). About 5% of the drug is excreted unchanged by the kidneys. Not removed by hemodialysis. Pharmacokinetics in special clinical situations The bioavailability of metoprolol increases with cirrhosis of the liver. Impaired liver function slows down the metabolism of the drug. Indications for use Arterial hypertension (including hyperkinetic type) as monotherapy or in combination with other antihypertensive agents; IHD: myocardial infarction (secondary prevention – complex therapy), prevention of angina attacks; heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole); hyperthyroidism (complex therapy); prevention of migraine attacks. Dosing and Administration The drug is taken orally simultaneously with meals or immediately after meals. Tablets can be divided in half, but not chewed, and washed down with liquid. With arterial hypertension, the initial dose is 50-100 mg / day in 1-2 doses. If necessary, the daily dose is gradually increased to 100-200 mg. In the absence of a satisfactory therapeutic effect, Metocard can be administered in combination with other antihypertensive agents. The maximum daily dose is 200 mg. With angina pectoris, arrhythmias, prevention of migraine attacks, 100-200 mg / day are prescribed in 2 divided doses (morning and evening). In secondary prevention of myocardial infarction, a dose of 200 mg / day is prescribed in 2 divided doses (morning and evening). With functional disorders of cardiac activity, accompanied by tachycardia, the drug is prescribed at a dose of 100 mg / day in 2 divided doses (morning and evening). In elderly patients, with impaired renal function, and if necessary, hemodialysis does not require dose adjustment of the drug. In case of impaired liver function, the dose of the drug should be reduced depending on the clinical condition. Use during pregnancy and lactation During pregnancy, Metocard should be used only if the intended benefit to the mother outweighs the potential risk to the fetus. Metoprolol crosses the placental barrier. If it is necessary to use the drug during pregnancy due to the possible development of bradycardia, arterial hypotension, hypoglycemia in the newborn, it is necessary to carefully monitor the development of the fetus. After delivery, it is necessary to ensure strict control over the condition of the newborn for 48-72 hours. Metoprolol is excreted in breast milk. The effect of metoprolol on the newborn has not been studied, therefore, if it is necessary to use Metocard during lactation, breastfeeding should be stopped. Interaction with other drugs Simultaneous use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. The interval between taking MAO inhibitors and metoprolol should be at least 14 days. Simultaneous / in the introduction of verapamil can provoke cardiac arrest. The simultaneous appointment of nifedipine leads to a significant decrease in blood pressure. Against the background of simultaneous use with Metokard, inhalation general anesthesia agents (hydrocarbon derivatives) increase the risk of myocardial function inhibition and the development of arterial hypotension. Beta-agonists, theophylline, cocaine, etrogens (sodium retention), indomethacin and other NSAIDs (sodium retention and blocking the synthesis of prostaglandin by the kidneys) weaken the hypotensive effect. There is an increase in the inhibitory effect on the central nervous system when used simultaneously with the standard; summation of the cardiodepressive effect – with means for general anesthesia; increased risk of peripheral circulatory disorders – with ergot alkaloids. When taken together with oral hypoglycemic agents, their effect may be reduced; with insulin – an increased risk of developing hypoglycemia, increasing its severity and duration, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure). When combined with antihypertensive agents, diuretics, nitroglycerin or slow calcium channel blockers, a sharp decrease in blood pressure may develop (special caution is necessary when combined with prazosin). When Metocard is used with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, alpha-methyldopa, clonidine, guanfacine, general anesthesia agents and cardiac glycosides, an increase in the severity of heart rate decrease and inhibition of AV conduction is observed. If metoprolol and clonidine are taken simultaneously, then when metoprolol is canceled, clonidine is canceled after a few days (due to the risk of withdrawal syndrome). Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in the metabolism of metoprolol, to a decrease in the concentration of metoprolol in the blood plasma and a decrease in the effect. Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) – increase the concentration of metoprolol in the blood plasma. Allergens used for immunotherapy or allergen extracts for skin tests when used together with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiopaque substances for intravenous administration – increase the risk of developing anaphylactic reactions. Metoprolol, with simultaneous use, reduces the clearance of xanthine (except diphylline), especially with initially increased clearance of theophylline under the influence of smoking; reduces the clearance of lidocaine, increases the concentration of lidocaine in the blood plasma. Metocard, with simultaneous use, enhances and prolongs the action of antidepolarizing muscle relaxants, prolongs the anticoagulant effect of coumarins. With the combined use of Metocard with ethanol, the risk of a pronounced decrease in blood pressure increases. Tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), sedatives and hypnotics, when used together with metoprolol, increase CNS depression. Contraindicationscardiogenic shock; AV block II or III degree; sinoatrial blockade; SSSU; severe bradycardia; chronic heart failure in the phase of decompensation; Prinzmetal’s angina; arterial hypotension (in the case of use in the secondary prevention of myocardial infarction – systolic blood pressure less than 100 mm Hg, heart rate less than 45 beats / min); lactation period; simultaneous reception with MAO inhibitors; simultaneous intravenous administration of verapamil; age up to 18 years; hypersensitivity to metoprolol or other components of the drug, other beta-blockers. With caution, the drug should be prescribed for diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), obliterating peripheral vascular diseases (intermittent claudication, Raynaud’s syndrome), chronic liver and / or kidney failure, myasthenia gravis, pheochromocytoma, AV blockade of the 1st degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, as well as elderly patients. Composition of metoprolol tartrate 50 mg Excipients: lactose, povidone, talc, magnesium stearate, microcrystalline cellulose, rice starch. OverdoseSymptoms: severe severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, syncope, in acute overdose – cardiogenic shock, loss of consciousness, coma, AV blockade (up to the development of complete transverse blockade and cardiac arrest), cardialgia. The first signs of an overdose appear 20 minutes to 2 hours after taking the drug. Treatment: gastric lavage and the appointment of adsorbing agents, symptomatic therapy: with a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position; in case of excessive decrease in blood pressure, bradycardia and heart failure – intravenous administration (with an interval of 2-5 minutes) of beta-agonists – until the desired effect is achieved or intravenous administration of 0.5-2 mg of atropine sulfate. In the absence of a positive effect, the introduction of dopamine, dobutamine or norepinephrine (norepinephrine). As a follow-up, perhaps the appointment of 1-10 mg of glucagon, the setting of a transvenous intracardiac pacemaker. With bronchospasm, intravenous β2-adrenergic stimulants should be administered. Metoprolol is poorly excreted by hemodialysis. Side effects From the side of the central nervous system and peripheral nervous system: increased fatigue, weakness, headache, slowing down the speed of mental and motor reactions; rarely – paresthesia in the limbs (in patients with intermittent claudication and Raynaud’s syndrome), depression, anxiety, decreased attention, drowsiness, insomnia, nightmares, confusion or short-term memory impairment, muscle weakness. From the sensory organs: rarely – decreased vision, decreased secretion of lacrimal fluid, dryness and soreness of the eyes, conjunctivitis, tinnitus. From the side of the cardiovascular system: sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension, dizziness, sometimes loss of consciousness; rarely – a decrease in myocardial contractility, a temporary aggravation of symptoms of chronic heart failure (edema, swelling of the feet and / or lower legs, shortness of breath), arrhythmias, manifestation of angiospasm (increased peripheral circulatory disorders, coldness of the lower extremities, Raynaud’s syndrome), myocardial conduction disturbance. From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, change in taste, impaired liver function, increased activity of liver enzymes; extremely rarely – hyperbilirubinemia. Dermatological reactions: urticaria, pruritus, rash, exacerbation of psoriasis, psoriasis-like skin reactions, skin flushing, exanthema, photodermatosis, increased sweating, reversible alopecia. On the part of the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when administered in high doses – loss of selectivity and / or in predisposed patients), shortness of breath. From the endocrine system: hyperglycemia in patients with non-insulin dependent diabetes mellitus, hypothyroidism. From the hemopoietic system: rarely – thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia. Impact on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia. Other: back or joint pain; in isolated cases – a slight increase in body weight, a decrease in libido and / or potency. Side effects depend on the individual sensitivity of the patient. Usually they are minor and disappear after the drug is discontinued. Storage conditions The drug should be stored in a dry, dark place out of the reach of children at a temperature not exceeding 25 ° C. Buy Metocard tablets 100 mg No. 10×3