Metoprolol-Akrichin
Monitoring of patients taking beta-blockers includes regular monitoring of heart rate (HR) and blood pressure, blood glucose levels in patients with diabetes mellitus. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed orally should be selected individually.
The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. When taking a dose above 200 mg per day, cardioselectivity decreases.
In case of heart failure, treatment with metoprolol begins only after reaching the compensation stage.
It is possible that the severity of hypersensitivity reactions may increase (against the background of a burdened allergic history) and the lack of effect from the administration of usual doses of epinephrine (adrenaline).
May increase symptoms of peripheral arterial circulation disorders.
The drug is discontinued gradually, reducing the dose over 10 days. If treatment is abruptly stopped, withdrawal syndrome may occur (increased angina attacks, increased blood pressure).
When discontinuing the drug, special attention should be paid to patients with angina pectoris.
For exertional angina, the selected dose of the drug should ensure the heart rate at rest is within 55-60 beats/min, and during exercise - no more than 110 beats/min.
Patients who use contact lenses should take into account that during treatment with beta-blockers, the production of tear fluid may decrease.
Metoprolol may mask some clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels.
If it is necessary to prescribe to patients with bronchial asthma, beta2-adrenergic agonists are used as concomitant therapy; for pheochromocytoma - alpha-blockers.
If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a general anesthesia agent with minimal negative inotropic effect); discontinuation of the drug is not recommended.
Drugs that reduce the supply of catecholamines (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure and bradycardia.
In elderly patients, regular monitoring of liver function is recommended. Correction of the dosage 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), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver dysfunction , sometimes it is necessary to stop treatment.
In patients with severe renal failure, monitoring of renal function is recommended.
Special monitoring should be carried out for the condition of patients with depressive disorders taking metoprolol; in case of depression caused by taking beta-blockers, it is recommended to discontinue therapy.
Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Metoprolol-Akrikhin tablet 50 mg x30
Registration number: P N003213/01 Trade name of the drug: Metoprolol-Akrikhin
International nonproprietary name: metoprolol
Dosage form: tablets
Composition: One tablet contains: active substance: metoprolol tartrate in terms of 100% substance - 50 mg, excipients: lactose monohydrate, colloidal silicon dioxide, potato starch, povidone, sodium carboxymethyl starch, magnesium stearate.
Description: tablets are white with a grayish or yellowish tint, flat-cylindrical, with a chamfer.
Pharmacotherapeutic group: selective beta1-blocker ATC code: C07AB02
Pharmacological properties
Pharmacodynamics Metoprolol is a cardioselective beta-adrenergic receptor blocker that does not have intrinsic sympathomimetic activity and membrane-stabilizing properties. It has hypotensive, antianginal and antiarrhythmic effects. By blocking beta1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, bathmo- and inotropic effect (reduces the heart rate (HR), inhibits conductivity and excitability, reduces myocardial contractility). The total peripheral resistance 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 alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), which after 1-3 days returns to the original one, and with prolonged application - decreases.
The hypotensive effect is due to a reflex decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (of greater importance in patients with initial hypersecretion of renin) and the central nervous system, restoration of the sensitivity of the baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease blood pressure) and, ultimately, a decrease in peripheral sympathetic influences. Reduces high blood pressure (BP) at rest, during physical exertion and stress.
The hypotensive effect develops quickly (systolic blood pressure decreases after 15 minutes, maximum after 2 hours) and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular use.
The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening diastole and improving myocardial perfusion) and contractility, as well as a decrease in the sensitivity of the myocardium 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 (AV) conduction (mainly in the antegrade and, to a lesser extent, in retrograde directions) through the AV node and along additional pathways.
With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and hyperthyroidism, it reduces heart rate, or can even lead to the restoration of sinus rhythm.
Prevents the development of migraine. When used in average therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism. When used in large doses (more than 100 mg/day), it has a blocking effect on both subtypes of beta-adrenergic receptors.
Pharmacokinetics Absorption when taken orally is complete (95%). The maximum concentration in blood plasma is achieved 1-2 hours after oral administration. The half-life averages 3.5 hours (range 1 to 9 hours). Subjected to intensive first-pass metabolism, bioavailability is 50% upon first administration and increases to 70% upon repeated use. Eating increases bioavailability by 20-40%. The bioavailability of metoprolol increases in liver cirrhosis. Communication with blood plasma proteins - 10%. Penetrates through the blood-brain and placental barriers. Passes into breast milk in small quantities. Metabolized in the liver, 2 metabolites have beta-adrenergic blocking activity. The CYP2D6 isoenzyme takes part in the metabolism of the drug. About 5% is excreted unchanged by the kidneys. Treatment of patients with reduced renal function does not require dose adjustment of the drug. Impaired liver function slows down the metabolism of the drug, and in cases of insufficiency of liver function, the dose of the drug should be reduced. It is not removed by hemodialysis.
Indications for use: • arterial hypertension (as monotherapy or in combination with other antihypertensive drugs), • coronary heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks, • cardiac arrhythmias (supraventricular tachycardia, ventricular extrasystole), •hyperthyroidism (complex therapy), •prevention of migraine attacks.
Contraindications • hypersensitivity to metoprolol or other components of the drug, other beta-blockers, • cardiogenic shock, • atrioventricular block (AV) II-III degree, • sick sinus syndrome, • severe bradycardia, • chronic heart failure in the stage of decompensation, • Prinzmetal's angina, • arterial hypotension (if used for secondary prevention of myocardial infarction - systolic blood pressure less than 100 mm Hg, heart rate less than 45 beats/min), • lactation period (see “Pregnancy and lactation”), • simultaneous taking monoamine oxidase inhibitors (MAO) or simultaneous intravenous administration of verapamil (see “Interaction with other drugs”), • age under 18 years (efficacy and safety have not been established), • lactose intolerance, lactase deficiency or Glucose-galactose malabsorption.
With caution 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 renal failure, myasthenia gravis, pheochromocytoma ( with simultaneous use of alpha-blockers), AV blockade of the first degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, old age.
Pregnancy and lactation During pregnancy, it is prescribed taking into account the ratio of benefit to the mother and risk to the fetus (due to the development of bradycardia, arterial hypotension, hypoglycemia in the fetus). At the same time, careful monitoring is carried out, especially over the development of the fetus. It is necessary to monitor newborns for 48-72 hours after delivery. The effect of metoprolol on a newborn during breastfeeding has not been studied, therefore women taking Metoprolol-Akrikhin should stop breastfeeding.
Directions for use and dosage: The tablets are taken orally during or immediately after meals, do not chew, and are washed down with a small amount of liquid. Arterial hypertension. The initial daily dose is 50-100 mg in 1-2 doses (morning and evening). If the therapeutic effect is insufficient, the daily dose can be gradually increased to 100-200 mg and/or additional prescription of other antihypertensive drugs. The maximum daily dose is 200 mg. Angina pectoris, arrhythmias, prevention of migraine attacks. 100-200 mg per day in two doses (morning and evening).
Secondary prevention of myocardial infarction. 200 mg per day in two doses (morning and evening).
Hyperthyroidism. 50 mg 2 times a day (morning and evening).
In elderly patients, with impaired renal function, and also if hemodialysis is necessary, the dose is not changed. In case of liver dysfunction, the dose of the drug should be reduced depending on the clinical condition.
Side effects From the central nervous system: increased fatigue, weakness, headache, slowdown in 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 senses: rarely - decreased vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis, tinnitus.
From the cardiovascular system: sinus bradycardia, palpitations, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely - decreased myocardial contractility, temporary worsening of symptoms of chronic heart failure (edema, swelling of the feet and/or lower legs, shortness of breath), arrhythmias, manifestation of vasospasm (increased peripheral circulatory disorders, coldness of the lower extremities, Raynaud's syndrome), impaired myocardial conduction.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, diarrhea, constipation, change in taste.
From the skin: urticaria, skin itching, rash, exacerbation of psoriasis, psoriasis-like skin reactions, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.
From the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when prescribed in high doses - loss of selectivity and/or in predisposed patients), shortness of breath.
From the endocrine system: hypoglycemia (in patients receiving insulin), rarely - hyperglycemia (in patients with insulin-dependent diabetes mellitus).
Laboratory indicators: rarely - thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of liver enzymes, extremely rarely - hyperbilirubinemia.
Effect on the fetus: possible intrauterine growth retardation, hypoglycemia, bradycardia.
Other: back or joint pain, like all beta-blockers, in isolated cases can cause a slight increase in body weight, decreased libido and/or potency.
Overdose Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, in case of acute overdose - cardiogenic shock, loss of consciousness, coma, atrioventricular block (up to the development of complete transverse blockade and cardiac arrest), cardialgia. The first signs of overdose appear 20 minutes -2 hours after taking the drug. Treatment: gastric lavage and taking adsorbents, symptomatic therapy: in case of a pronounced decrease in blood pressure, the patient should be in the Trendelenburg position; in case of an excessive decrease in blood pressure, bradycardia and heart failure - intravenously, at intervals of 2-5 minutes, beta - adrenergic agonists - until the desired effect is achieved or 0.5-2 mg of atropine sulfate intravenously. If there is no positive effect, dopamine, dobutamine or norepinephrine (norepinephrine). As subsequent measures, it is possible to administer 1-10 mg of glucagon and install a transvenous intracardial pacemaker. For bronchospasm, beta2-agonists should be administered intravenously. Metoprolol is poorly excreted by hemodialysis.
Interaction with other drugs • Concomitant use with monoamine oxidase inhibitors (MAOIs) is not recommended due to a significant increase in the hypotensive effect. The treatment break between taking MAO inhibitors and metoprolol should be at least 14 days. • Simultaneous intravenous administration of verapamil can provoke cardiac arrest. • Simultaneous administration of nifedipine leads to a significant decrease in blood pressure. •Inhalation anesthetics (hydrocarbon derivatives) increase the risk of suppression of myocardial function and the development of arterial hypotension. •Beta-adrenergic agonists, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blocking renal prostaglandin synthesis) weaken the hypotensive effect. •There is an increased inhibitory effect on the central nervous system with ethanol, a summation of the cardiodepressive effect with anesthesia, and an increased risk of peripheral circulatory disorders with ergot alkaloids. •When taken together with hypoglycemic agents for oral administration, their effect may be reduced; with insulin, the risk of developing hypoglycemia may increase, its severity will increase and prolong, masking some symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure). • When combined with antihypertensive drugs, diuretics, nitroglycerin or blockers of “slow” calcium channels, a sharp decrease in blood pressure may develop (special caution is required when combined with prazosin), an increase in the severity of the decrease in heart rate and inhibition of atrioventricular conduction - when using metoprolol with verapamil, diltiazem, antiarrhythmic drugs (amiodarone), reserpine, methyldopa, clonidine, guanfacine, general anesthetics and cardiac glycosides. •If metoprolol and clonidine are taken simultaneously, then when metoprolol is discontinued, clonidine is discontinued after a few days (due to the risk of withdrawal syndrome). •Inducers of microsomal liver enzymes (rifampicin, barbiturates) lead to increased metabolism of metoprolol, a decrease in its concentration in the blood plasma and a decrease in effect. Inhibitors (cimetidine, oral contraceptives, phenothiazines) - increase the concentration of metoprolol in plasma. •Allergens used for immunotherapy or allergen extracts for skin testing when used in combination with metoprolol increase the risk of systemic allergic reactions or anaphylaxis; iodine-containing radiocontrast agents for intravenous administration increase the risk of anaphylactic reactions. •Reduces the clearance of xanthine (except for diphylline), especially with the initially increased clearance of theophylline under the influence of smoking. Reduces the clearance of lidocaine, increases the concentration of lidocaine in the blood plasma. •Enhances and prolongs the effect of antidepolarizing muscle relaxants, prolongs the anticoagulant effect of coumarins. •When used together with ethanol, the risk of a pronounced decrease in blood pressure increases.
Special instructions •Monitoring of patients taking beta-blockers includes regular monitoring of heart rate (HR) and blood pressure, blood glucose levels in patients with diabetes. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed orally should be selected individually. •The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. When taking a dose above 200 mg per day, cardioselectivity decreases. •In case of heart failure, treatment with metoprolol is started only after reaching the compensation stage. • Possible increased severity of hypersensitivity reactions (against the background of a burdened allergic history) and lack of effect from the administration of usual doses of epinephrine (adrenaline). •May increase symptoms of peripheral arterial circulatory disorders. •Discontinuation of the drug is carried out gradually, reducing the dose over 10 days. •If treatment is abruptly stopped, “withdrawal” syndrome may occur (increased attacks of angina, increased blood pressure). •When discontinuing the drug, special attention should be paid to patients with angina pectoris. •For exertional angina, the selected dose of the drug should ensure a heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min. •Patients who use contact lenses should take into account that during treatment with beta-blockers, the production of tear fluid may decrease. •Metoprolol may mask some clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms. •In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels. •If necessary, beta2-adrenergic agonists are used as concomitant therapy for patients with bronchial asthma; for pheochromocytoma, alpha-blockers are used. •If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a general anesthesia agent with minimal negative inotropic effect); discontinuation of the drug is not recommended. •Drugs that reduce catecholamine reserves (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure and bradycardia. •In elderly patients, regular monitoring of liver function is recommended. •Adjustment of the dosage 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), atrioventricular block, bronchospasm, ventricular arrhythmias, severe dysfunction liver, sometimes it is necessary to stop treatment. •In patients with severe renal impairment, monitoring of renal function is recommended. •Special monitoring of the condition of patients with depressive disorders taking metoprolol should be carried out; in case of depression caused by taking beta-blockers, it is recommended to discontinue therapy. •Due to the lack of sufficient clinical data, the drug is not recommended for use in children.
Effect on the ability to drive vehicles and complex equipment. At the beginning of treatment with metoprolol, patients may experience dizziness and fatigue. In this case, they should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. In the future, dose safety is determined individually.
Release form Tablets 50 mg. 10 tablets in a blister pack. 3 blister packs along with instructions for use in a cardboard pack.
Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.
Shelf life: 4 years. Do not use after the expiration date.
Conditions for dispensing from pharmacies By prescription.
Manufacturer/Organization accepting consumer complaints: Open Joint-Stock Company Chemical and Pharmaceutical Plant AKRIKHIN (JSC AKRIKHIN), Russia 142450, Moscow region, Noginsky district, Staraya Kupavna, st. Kirova, 29. Phone/fax: +
Metoprolol-Akrikhin tab 50mg N60 (Akrikhin)
Monitoring of patients taking beta-blockers includes regular monitoring of heart rate (HR) and blood pressure, blood glucose levels in patients with diabetes mellitus. If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents prescribed orally should be selected individually. The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. When taking a dose above 200 mg per day, cardioselectivity decreases. In case of heart failure, treatment with metoprolol begins only after reaching the compensation stage. It is possible that the severity of hypersensitivity reactions may increase (against the background of a burdened allergic history) and the lack of effect from the administration of usual doses of epinephrine (adrenaline). May increase symptoms of peripheral arterial circulation disorders. The drug is discontinued gradually, reducing the dose over 10 days. If treatment is abruptly stopped, withdrawal syndrome may occur (increased angina attacks, increased blood pressure). When discontinuing the drug, special attention should be paid to patients with angina pectoris. For exertional angina, the selected dose of the drug should ensure the heart rate at rest is within 55-60 beats/min, and during exercise - no more than 110 beats/min. Patients who use contact lenses should take into account that during treatment with beta-blockers, the production of tear fluid may decrease. Metoprolol may mask some clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels. If it is necessary to prescribe to patients with bronchial asthma, beta2-adrenergic agonists are used as concomitant therapy; for pheochromocytoma - alpha-blockers. If surgical intervention is necessary, it is necessary to warn the anesthesiologist about the therapy being performed (choosing a general anesthesia agent with minimal negative inotropic effect); discontinuation of the drug is not recommended. Drugs that reduce the supply of catecholamines (for example, reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure and bradycardia. In elderly patients, regular monitoring of liver function is recommended. Correction of the dosage 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), atrioventricular block, bronchospasm, ventricular arrhythmias, severe liver dysfunction , sometimes it is necessary to stop treatment. In patients with severe renal failure, monitoring of renal function is recommended. Special monitoring should be carried out for the condition of patients with depressive disorders taking metoprolol; in case of depression caused by taking beta-blockers, it is recommended to discontinue therapy. Due to the lack of sufficient clinical data, the drug is not recommended for use in children. Effect of the drug on the ability to drive vehicles and machines: At the beginning of treatment with metoprolol, patients may experience dizziness and fatigue. In this case, they should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. In the future, dose safety is determined individually.
Side effects
From the nervous system and sensory organs: weakness, fatigue, headache, dizziness, depression, sleep disorders, nightmares, convulsions, feeling of cold and paresthesia in the extremities, conjunctivitis, decreased secretion of tear fluid.
From the cardiovascular system and blood: bradycardia, arterial hypotension, impaired AV conduction, heart failure with peripheral edema, thrombocytopenia.
From the respiratory system: rhinitis, symptoms of bronchial obstruction (in predisposed patients).
From the gastrointestinal tract: dry mouth, vomiting, diarrhea or constipation, impaired liver function.
Allergic reactions: rash, itching.
Other: hypoglycemic conditions (in patients with diabetes mellitus).
Precautionary measures
Prescribed with caution for diabetes mellitus (especially with a labile course), Raynaud's disease, peripheral circulatory disorders, pheochromocytoma, severe impairment of liver and kidney function. Patients who use contact lenses should take into account a possible decrease in tear production. Long-term treatment should be discontinued gradually (at least 10 days).
When performing surgery during treatment, the anesthetic agent with the least negative inotropic effect should be the drug of choice. In the case of intended use of chloroform or ether for anesthesia, it is necessary to stop taking the drug several days in advance.
