Pharmacodynamics and pharmacokinetics
The drug has antiarrhythmic, antianginal and hypotensive effects. The drug does not have internal SMA and does not have a membrane-stabilizing effect.
The hypotensive effect is due to a decrease in the synthesis of renin, monooxygenase, inhibition of the activity of the renin-angiotensin system and the central nervous system. The drug can lower blood pressure during stress and physical exertion at rest.
The antianginal effect is ensured by a decrease in pulse rate, as well as a decrease in the need for oxygen in myocardial tissue. Long-term use of the medication increases exercise tolerance and reduces the severity of angina attacks and their frequency. As a result of eliminating arrhythmogenic factors (arterial hypertension, increased cAMP content, tachycardia, increased activity of the sympathetic nervous system), an antiarrhythmic effect is achieved.
For thyrotoxicosis, heart diseases of functional origin, sinus tachycardia , atrial fibrillation, supraventricular tachycardia, Metoprolol allows you to restore sinus rhythm and reduce heart rate. The drug prevents the formation of migraines.
Average therapeutic dosages of metoprolol, unlike other beta-blockers, have a less pronounced effect on the organs in which beta-2-blockers are located (uterus, bronchi, smooth muscle tissue of peripheral arteries, skeletal muscles, pancreas) and on carbohydrate metabolism.
Long-term use of the medication leads to a decrease in blood cholesterol levels.
Metoprolol 50 mg
Metoprolol
Registration number: LP-000950
Trade name of the drug: Metoprolol
International nonproprietary name: metoprolol
Dosage form: tablets
Composition per tablet: metoprolol tartrate 0.05 g or 0.1 g (calculated as 100% substance).
Excipients: lactose monohydrate (milk sugar) - 0.08949 g or
0.12778 g, potato starch - 0.04275 g or 0.06349 g, povidone (kollidon 30 or plasdon K-29/30) - 0.003 g or 0.0048 g, colloidal silicon dioxide (Aerosil 300) - 0.003 g or
0.0048 g, crospovidone (kollidon CL-M or polyplasdon XL-10) – 0.007 g or 0.0112 g, magnesium stearate – 0.002 g or 0.0032 g, stearic acid – 0.002 g or 0.0032 g.
Description: round tablets of a flat-cylindrical shape with a chamfer and a score, white or white with a yellowish tint. Slight marbling is allowed.
Pharmacotherapeutic group: selective beta1-blocker
ATX code: [С07АВ02]
Pharmacological properties
Pharmacodynamics Cardioselective beta1-blocker. It has a slight membrane-stabilizing effect and does not have internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects.
By blocking beta1-adrenergic receptors of the heart, it reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate, reduces the intracellular calcium current, has a negative chrono-, dromo-, batmo- and inotropic effect (reduces heart rate, inhibits conductivity and excitability, reduces myocardial contractility ).
The total peripheral vascular resistance at the beginning of the use of beta-adrenergic 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 returns to the original level after 1-3 days, and with long-term use it decreases.
The antihypertensive effect is due to a reflex decrease in minute blood volume 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 decrease in blood pressure) and ultimately a decrease in peripheral sympathetic influences. Reduces high blood pressure (BP) at rest, during physical exertion and stress. The antihypertensive 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 (prolongation of diastole and improvement of 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. By increasing the end-diastolic pressure in the left ventricle of the heart and increasing the stretching of the muscle fibers of the ventricles, it can increase the myocardial oxygen demand, especially in patients with chronic heart failure. 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 the retrograde directions through the AV node) and along additional paths.
In case of supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and thyrotoxicosis, it reduces the heart rate (HR) or can even lead to rhythm restoration.
Prevents the development of migraine.
In contrast to non-selective beta-blockers, when used in average therapeutic doses, 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 blocks beta1 and beta2 adrenergic receptors.
Pharmacokinetics Absorption in the gastrointestinal tract when taken orally is complete (95%). Solubility in fats is moderate. Subjected to intensive first-pass metabolism, bioavailability is 50% upon first administration and increases to 70% upon repeated use. Communication with blood plasma proteins - 10%. The time to reach the maximum concentration of metoprolol is 1.5-2 hours. During the course of treatment, bioavailability increases. Eating increases bioavailability by 20 - 40%.
It is quickly distributed in tissues, penetrates the blood-brain barrier, and the placental barrier. Penetrates into breast milk (concentration higher than in blood plasma).
Metabolized in the liver, two metabolites have beta-blocking activity. The CYP2D6 isoenzyme takes part in the metabolism of the drug. The half-life of metoprolol ranges from 3.5 to 7 hours when taken orally. It is not removed by hemodialysis.
A significant accumulation of metabolites is observed in patients with a creatinine clearance of 5 ml/min, while the beta-blocking activity of the drug does not increase.
Bioavailability increases in liver failure, while its overall clearance is reduced.
Indications for use
Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs); functional disorders of cardiac activity accompanied by tachycardia; coronary heart disease: myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks; heart rhythm disturbances (supraventricular tachycardia; ventricular extrasystole); hyperthyroidism (complex therapy); prevention of migraine attacks.
Contraindications
Hypersensitivity to metoprolol, other components of the drug and other beta-blockers, cardiogenic shock, grade II-III atrioventricular block, sinoatrial block, sick sinus syndrome, severe bradycardia (heart rate less than 50 beats/min), acute and chronic heart failure in stages of decompensation, Prinzmetal's angina, acute myocardial infarction (heart rate less than 45 beats/min, PQ interval more than 0.24 s, systolic blood pressure less than 100 mm Hg), pheochromocytoma (without simultaneous use of alpha-blockers), concomitant use of monoamine oxidase inhibitors or simultaneous intravenous administration of verapamil; lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome, severe peripheral circulatory disorders, severe forms of bronchial asthma and a history of bronchospasm; age up to 18 years, lactation period.
Directions for use and doses
Orally, during or immediately after a meal, the tablets can be divided in half (but not chewed) and washed down with liquid. For arterial hypertension (in monotherapy or in combination with other antihypertensive drugs), the initial dose is 50-100 mg 1-2 times a day (morning and evening); if the therapeutic effect is insufficient, the daily dose can be increased to 100-200 mg. The maximum daily dose is 200 mg.
For functional disorders of cardiac activity accompanied by tachycardia - 50 mg 2 times a day (morning and evening). Elderly patients are recommended to start treatment with 50 mg/day.
Coronary heart disease: myocardial infarction (secondary prevention) - 200 mg/day, divided into 2 doses (morning and evening).
Prevention of angina attacks, in case of heart rhythm disturbances - 100-200 mg 1-2 times a day (morning and evening).
For hyperthyroidism - 50 mg 2 times a day (morning and evening).
Prevention of migraine attacks - 100-200 mg 1-2 times a day (morning and evening).
Carefully
Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease, renal/liver failure, myasthenia gravis, pheochromocytoma (with simultaneous use with alpha-blockers), thyrotoxicosis, stage I atrioventricular block, depression (including in history) , psoriasis, peripheral circulatory disorders (“intermittent” claudication, Raynaud’s syndrome), aggravated allergic history, pregnancy, old age.
Overdose
Symptoms: severe sinus bradycardia, dizziness, atrioventricular block (up to the development of complete transverse block and cardiac arrest), marked decrease in blood pressure, fainting, arrhythmia, ventricular extrasystole, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma, nausea, vomiting, cyanosis, convulsions, hypoglycemia. The first signs of overdose appear 20 minutes - 2 hours after taking the drug. Treatment: gastric lavage and taking absorbent medications; 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 - intravenously (i.v.), with an interval of 2-5 minutes, beta-agonists - until the desired effect is achieved or i.v. 0.5-2 mg of atropine. If there is no positive effect, dopamine, dobutamine or norepinephrine. For hypoglycemia - administration of 1-10 mg of dextrose solution, installation of a transvenous intracardial pacemaker. For bronchospasm, beta2-adrenergic agonists are used. For convulsions - slow intravenous administration of diazepam. Hemodialysis is ineffective.
special instructions
Monitoring of patients taking beta-blockers includes monitoring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), blood glucose concentration in patients with diabetes (once every 4-5 months). 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.
It is possible that the severity of allergic reactions may increase (against the background of a burdened allergic history) and there will be no effect from the administration of usual doses of epinephrine (adrenaline). In elderly patients, it is recommended to monitor kidney function (once every 4-5 months).
May increase symptoms of peripheral arterial circulation disorders. For exertional angina, the selected dose of the drug should ensure the heart rate at rest within the range of 55-60 beats/min, and during exercise - no more than 110 beats/min. In smokers, the effectiveness of beta-blockers is lower.
Metoprolol may mask some clinical manifestations of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can intensify 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 values.
If necessary, use in patients with concomitant bronchial asthma requires additional use of beta2-adrenergic agonists; for pheochromocytoma - alpha-blockers.
If surgical intervention is necessary, it is necessary to warn the surgeon/anesthesiologist about taking metoprolol (the choice of drugs for general anesthesia with minimal negative inotropic effect); discontinuation of the drug is not recommended. In the event of increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg), AV block, bronchospasm, ventricular arrhythmias, severe impairment of liver and kidney function, it is necessary to reduce the dose or discontinue treatment. It is recommended to discontinue therapy if skin rashes appear and depression develops caused by taking beta-blockers. The drug is discontinued gradually, reducing the dose over 10 days. If treatment is abruptly stopped, nightmare dream syndrome may occur; very rarely - amnesia/memory impairment, depression, hallucinations, slowing of the speed of mental and motor reactions, muscle cramps, asthenia, myasthenia gravis. . From the senses: rarely - blurred vision, dry and sore eyes, conjunctivitis, decreased secretion of tear fluid; very rarely - ringing in the ears, disturbance of taste. . From the digestive system: often - nausea, abdominal pain, constipation or diarrhea; infrequently - vomiting; rarely - dryness of the oral mucosa, impaired liver function, hepatitis.
From the skin: infrequently - urticaria, increased sweating; rarely - alopecia; very rarely - photosensitivity, exacerbation of psoriasis, skin itching, rash, skin hyperemia, psoriasis-like skin reactions. . From the respiratory system: often - shortness of breath with physical effort; uncommon – bronchospasm in patients with bronchial asthma; rarely – rhinitis.
Other: infrequently - weight gain; very rarely - arthralgia, thrombocytopenia; Peyronie's disease, hypoglycemia, hyperglycemia, increased titer of antinuclear antibodies, decreased libido, potency.
Interaction with other drugs
Barbiturates increase the metabolism of metoprolol due to the induction of microsomal liver enzymes.
Propafenone increases the plasma concentration of metoprolol by 2-5 times (probably due to inhibition of the CYP2D6 isoenzyme by propafenone). Simultaneous intravenous administration of verapamil can cause bradycardia and a marked decrease in blood pressure.
Class I antiarrhythmic drugs can lead to additive negative inotropic effects with the development of severe hemodynamic side effects in patients with impaired left ventricular function (this combination should be avoided in patients with sick sinus syndrome or impaired AV conduction).
Amiodarone is a risk of developing severe sinus bradycardia (including long after discontinuation of amiodarone, due to its long half-life).
Diltiazem is a risk of developing severe bradycardia (mutually enhancing the inhibitory effect on AV conduction and sinus node function). The antihypertensive effect is weakened by glucocorticosteroids and estrogens (sodium ion retention).
Beta-adrenergic agonists, aminophylline, theophylline, indomethacin and other non-steroidal anti-inflammatory drugs weaken the antihypertensive effect.
Diphenhydramine reduces the clearance of metoprolol, enhancing its effect. Epinephrine - the risk of developing a pronounced decrease in blood pressure and bradycardia. Phenylpropanolamine in high doses causes a paradoxical increase in blood pressure (up to a hypertensive crisis).
Quinidine inhibits the metabolism of metoprolol in rapid metabolizers, leading to a significant increase in plasma concentrations of metoprolol and an increase in its beta-blocking effect.
Clonidine - there is a risk of a pronounced increase in blood pressure when clonidine is abruptly discontinued while taking beta-blockers simultaneously, therefore, if clonidine is discontinued, gradual cessation of beta-blockers should be started several days before its discontinuation.
Rifampicin - enhances the metabolism of metoprolol, reducing plasma concentrations (due to the induction of microsomal liver enzymes). Cimetidine and hydralazine increase the concentration of metoprolol in the blood. Medicines for inhalation anesthesia (halogenated hydrocarbons) enhance the cardiodepressive effect of metoprolol. Incompatible with monoamine oxidase type A inhibitor.
Cardiac glycosides, methyldopa, reserpine, guanfacine and clonidine increase the risk of bradycardia.
Nifedipine, in addition to enhancing the antihypertensive effect, can lead to the development
heart failure.
Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase depression of the central nervous system.
With the simultaneous use of metoprolol and sympatholytics, nitroglycerin, barbiturates, vasodilators (alprostadil) and other antihypertensive drugs (for example, prazosin), the antihypertensive effect may be enhanced, therefore patients taking such combinations of drugs should be under constant medical supervision to detect an excessive decrease in blood pressure or bradycardia.
Changes the effectiveness of insulin and oral hypoglycemic agents. Increases the risk of developing hypoglycemia, enhances its severity and duration, masks its symptoms (tachycardia, sweating, increased blood pressure).
When used together with ethanol, the risk of a pronounced decrease in blood pressure increases and an increased inhibitory effect on the central nervous system is noted.
Reduces the clearance of lidocaine and increases its concentration in the blood plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking.
Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Prolongs the effect of antidepolarizing muscle relaxants and the anticoagulant effect of coumarin derivatives.
Aldesleukin increases arterial hypotension.
Mefloquine increases inhibition of conduction and excitability of the heart muscle.
When used simultaneously with norepinephrine, epinephrine, other adrenergic and sympathomimetics (including in the form of eye drops or as part of antitussives), a slight increase in blood pressure is possible.
Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving metoprolol. Iodine-containing radiopaque drugs for intravenous administration increase the risk of anaphylactic reactions.
Use during pregnancy and breastfeeding
During pregnancy, it is prescribed only according to strict indications if the expected benefit to the mother outweighs the potential risk to the fetus (due to the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory depression in the newborn). Treatment must be interrupted 48-72 hours before delivery. In cases where this is not possible, it is necessary to ensure strict monitoring of newborns for 48 to 72 hours after delivery.
Since metoprolol passes into breast milk, the drug should not be taken during breastfeeding or the mother should stop breastfeeding during treatment.
Impact on the ability to drive vehicles and machinery
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form
Tablets of 50 mg and 100 mg.
10 or 20 tablets in a blister pack made of polyvinyl chloride film and aluminum foil.
30 tablets per jar made of polymer materials.
Each jar or 3 or 5 blister packs of 10 tablets or 2 blister packs of 20 tablets, together with instructions for use, are placed in a cardboard pack for consumer packaging.
Storage conditions:
In a dry place, protected from light, at a temperature not exceeding 25ºС.
Best before date:
2 years. Do not use after the expiration date.
Units:
pack
Indications for use of Metoprolol
The medicine is used for myocardial infarction , unstable angina , exertional angina , coronary , arterial hypertension arterial hypertension crisis .
The drug is used for rhythm disturbances: supraventricular arrhythmia , ventricular form of arrhythmia, sinus tachycardia , atrial tachycardia, atrial flutter, atrial fibrillation , ventricular extrasystole .
The drug is used for thyrotoxicosis (in complex therapy), for tremor (senile, essential forms), for migraines, withdrawal syndrome , akathisia when taking antipsychotics, and for anxiety.
Release form of Metoprolol
Metoprolol is available in tablet form for systemic treatment. The main substance is metoprolol tartrate, which can be contained in the amount of 25 mg, 50 mg or 100 mg in one tablet. Auxiliary components:
- magnesium stearate;
- silica;
- sodium carboxymethyl starch;
- microcrystalline cellulose.
The drug belongs to the cardioselective beta-blockers.
Contraindications
Metoprolol is not prescribed for 2-3 degree atrioventricular block, cardiogenic shock , intolerance to the active substance, acute form of heart failure , and arterial hypotension , Prinzmetal's angina , breastfeeding, in the acute period of myocardial infarction, simultaneous use of an MAO inhibitor, with intravenous infusion of Verapamil.
With metabolic acidosis , myasthenia gravis, diabetes mellitus, liver failure, pheochromocytoma, chronic renal failure, COPD (chronic obstructive bronchitis , emphysema ), with bronchial asthma, obliterating disease of peripheral vessels, during pregnancy, thyrotoxicosis, psoriasis, depression, in pediatric practice, persons In elderly patients, the medicine is prescribed with caution.
Drug interactions Metoprolol
When taking Metoprolol simultaneously with insulin or oral hypoglycemic agents, their effect may be enhanced or prolonged. In this case, the symptoms of hypoglycemia (especially tachycardia and tremor) may be masked. In such cases, it is necessary to regularly monitor blood glucose levels. With the simultaneous use of Metoprolol and tricyclic antidepressants, barbiturates, phenothiazines, nitroglycerin, diuretics, vasodilators and other antihypertensive drugs (for example, prazosin), oral contraceptives, ranitidine, cimetidine, the hypotensive effect may be enhanced; with the simultaneous use of calcium antagonists (such as nifedipine), in addition to enhancing the hypotensive effect, heart failure may develop; calcium antagonists (such as verapamil and diltiazem) or other antiarrhythmics (such as disopyramide) may cause hypotension, bradycardia and other cardiac arrhythmias; cardiac glycosides, reserpine, guanfacine and clonidine may develop severe bradycardia; norepinephrine, epinephrine or other sympathomimetic drugs, as well as MAO inhibitors, may increase blood pressure; indomethacin and rifampicin may reduce the hypotensive effect of metoprolol; lidocaine makes it difficult to remove the latter; alcohol - may increase the inhibitory effect on the central nervous system; peripheral muscle relaxants (for example, suxamethonium, tubocurarine) may enhance neuromuscular blockade. Narcotic drugs enhance the hypotensive effect of metoprolol, while the negative inotropic effect of these drugs is potentiated. Therefore, before surgery under general anesthesia, the anesthesiologist must be informed that the patient is taking Metoprolol. When clonidine and metoprolol are used simultaneously, treatment with the latter should be discontinued several days before clonidine is discontinued to prevent a hypertensive crisis.
Side effects
Nervous system: slower speed of motor and mental reactions, weakness, headaches, increased fatigue, paresthesia in the extremities, convulsions, tremors, drowsiness, attention disorders, anxiety, insomnia, myasthenia gravis, hallucinations, memory impairment, confusion, “nightmare” dreams, asthenia.
Sense organs: eye pain, decreased vision, conjunctivitis, dry eyes, decreased tear production.
Cardiovascular system: orthostatic hypotension , loss of consciousness, dizziness, drop in blood pressure, sinus bradycardia, swelling, decreased myocardial contractility, cardialgia , myocardial conduction disorders, manifestation of vasospasm, CHF, rarely worsening of impaired atrioventricular conduction is observed.
Digestive tract: changes in taste, disturbances in liver function (cholestasis, darkening of urine, yellowing of the skin and sclera).
Skin: photodermatosis , psoriasis-like skin reactions, exacerbation of psoriasis, skin rashes, exanthema, reversible form of alopecia, increased sweating.
Respiratory system: bronchospasm, nasal congestion, shortness of breath.
Endocrine system: hypoglycemia (in insulin-requiring diabetes mellitus), hyperglycemia (in persons with non-insulin-dependent diabetes mellitus), hypothyroid state. Possible development of rash, itching, allergies, thrombocytopenia, hyperbilirubinemia, agranulocytosis.
The effect of Metoprolol on the fetus: hypoglycemia, intrauterine growth retardation, bradycardia.
The drug can cause decreased potency, libido, weight gain, and joint pain. Abrupt cessation of taking the drug causes the development of “withdrawal syndrome”.
Side effects of Metoprolol
Taking Metoprolol in rare cases can cause a number of side effects:
- increased fatigue;
- drowsiness;
- decreased concentration;
- sleep disorders.
Less common are negative effects on the organ of vision: dry tear duct, dry eye syndrome and pain.
From the digestive tract - taste disturbance and decreased liver function. In addition, skin reactions in the form of photodermatosis also occur. If the patient has a manifestation of psoriasis on the skin, the affected area may increase or enter an acute stage. In some patients, the intensity of sweating increases.
From the respiratory system - nasal congestion, bronchospasm or shortness of breath appears.
Metoprolol tablets, instructions for use (Method and dosage)
The medicine is taken orally. Tablets should not be divided in half, chewed, or broken. The average dosage for arterial hypertension is 100-150 mg for 1-2 doses per day.
Angina: 2-3 times a day 50 mg.
Thyrotoxicosis, hyperkinetic cardiac syndrome, tachyarrhythmia: 1-2 times a day, 50 mg.
For secondary prevention of myocardial infarction, 200 mg of metoprolol is indicated.
For the prevention of migraine, 100-200 mg per day is prescribed for 2-4 doses.
In case of paroxysmal supraventricular tachycardia, in order to stop the attack, it is administered parenterally under inpatient observation.
In case of acute myocardial infarction, Metoprolol is administered immediately after hospitalization of the patient; it is necessary to monitor the level of blood pressure, pulse, ECG, and atrioventricular conduction.
For elderly people, therapy begins with 50 mg per day. In case of pathology of the hepatic system, dosage adjustment is not carried out (it is preferable to prescribe drugs that are not metabolized in the hepatic system).
Instructions for use of Metoprolol Ratiopharm and Metoprolol Acri are similar.
Overdose
Manifested by dizziness, drop in blood pressure, sinus bradycardia , arrhythmias, fainting, ventricular extrasystole , cardiogenic shock, heart failure, cardiac arrest, bronchospasm , nausea, vomiting, coma, loss of consciousness.
The first symptoms are observed 20 minutes after taking increased doses of the drug.
The administration of enterosorbents and timely gastric lavage are required. If there is a significant drop in blood pressure, the patient is placed in a Trendelenburg position and norepinephrine, Dobutamine , and Dopamine . Later glucagon , and an intracardial pacemaker is installed in a transvenous manner as needed.
Diazepam is administered slowly intravenously . When bronchospasm develops, beta-2 adrenergic stimulants are administered intravenously.
Hemodialysis has not proven effective.
Interaction
Extracts of allergens used for skin testing, the allergens themselves significantly increase the likelihood of developing anaphylaxis, severe systemic allergic reactions in patients who use Metoprolol.
The risk of developing anaphylactic reactions increases with intravenous administration of radiocontrast drugs based on iodine . Medicines for general inhalation anesthesia, phenytoin when administered intravenously increase the likelihood of a drop in blood pressure and increase the severity of the cardiodepressive effect.
Metoprolol can mask the symptoms of hypoglycemia (high blood pressure, tachycardia ) and change the effectiveness of oral forms of hypoglycemic agents, insulin.
The drug reduces the clearance of xanthines, lidocaine , increasing their concentration in the blood plasma, especially in patients with increased clearance of theophylline with concomitant smoking.
Estrogens, glucocorticosteroids, NSAIDs weaken the hypotensive effect of the drug.
Methyldopa , Reserpine , BMCC, cardiac glycosides, antiarrhythmic drugs, Amiodarone , Diltiazem , Verapamil , guanfacine - aggravate the course of bradycardia , heart failure , atrioventricular block .
When taking Nifedipine, a significant drop in blood pressure is observed. Hydralazine , sympatholytics, clonidine , diuretics, and other antihypertensive drugs can provoke a sharp and excessive drop in blood pressure.
Metoprolol prolongs the period of anticoagulant action of coumarins and increases the period of action of non-depolarizing muscle relaxants. Antipsychotic drugs, tetracyclic antidepressants, neuroleptics, tricyclic antidepressants, hypnotics and sedatives, ethanol - enhance the inhibitory effect of metoprolol on the central nervous system.
The simultaneous administration of MAO inhibitors is unacceptable due to the risk of a sharp drop in blood pressure.
Impaired peripheral circulation is observed when non-hydrogenated ergot alkaloids are prescribed.
Pharmacological properties of the drug Metoprolol
Metoprolol is a selective β-adrenergic receptor blocker. It acts predominantly on β1-receptors of the myocardium, to a lesser extent - on β2-receptors of peripheral vessels and bronchi. In contrast to non-selective β-adrenergic receptor blockers, metoprolol in average therapeutic doses has a lesser effect on the smooth muscles of the bronchi and peripheral arteries, insulin release, carbohydrate and lipid metabolism. In case of hypertension (arterial hypertension), it reduces blood pressure, the hypotensive effect stabilizes at the end of the 2nd week of regular use. In patients with coronary artery disease, it exhibits anti-ischemic and antianginal effects, reduces the number and severity of attacks, and reduces sensitivity to physical stress; helps normalize heart rhythm. After oral administration, it is quickly absorbed. The maximum concentration in blood plasma is reached after 1–2 hours. Bioavailability increases in patients with liver disease and in the elderly. Penetrates the placental barrier and is detected in breast milk. It is excreted primarily by the kidneys, mainly in the form of metabolites.
special instructions
Monitoring of patients using beta-blockers includes regular monitoring of blood pressure, pulse, and sugar levels. It is important to teach the patient to keep track of the pulse rate, and in case of bradycardia, he needs to seek the help of his attending physician.
Elderly people need to monitor the functioning of the renal system.
Metoprolol can cause peripheral arterial circulatory disorders.
Metoprolol is withdrawn gradually over at least 10 days.
Taking more than 200 mg per day leads to a decrease in cardioselectivity.
When taking the drug, it is possible to mask the clinical picture of thyrotoxicosis ( tachycardia ).
When planning a surgical intervention, it is necessary to notify the anesthesiologist about taking the drug Metoprolol, and do not stop taking the drug.
arterial hypotension , increasing bradycardia , ventricular arrhythmia , atrioventricular block, severe pathology of the liver and kidneys are registered in elderly people
Treatment is stopped if depression develops or skin rashes appear.
When taking the drug during pregnancy, it should be discontinued 48-72 hours before the expected birth.
Metoprolol has an effect on driving vehicles and performing complex work.
Recipe in Latin:
Rp: Metoprololi 0.05 D. td No. 100 in tab. S. 1 tablet. 2-3 times a day.
Metoprolol analogs
Level 4 ATC code matches:
Biol
Metocard
Metozok
Nebilet
Nebilong
Betaxolol
Bisogamma
Aritel
Cordinorm
Vasocardin
Corvitol
Bidop
Bisoprolol
Nebivolol
Biprol
Bisoprol
Concor Cor
Lokren
Concor
Niperten
Metoprolol-Acri, Metoprolol-Ratiopharm, Metoprolol-OBL, Metoprolol Organica, Metoprolol Zentiva are synonymous drugs.
The following analogues of Metoprolol are also distinguished:
- Egilok
- Betalok
- Metocard
- Metocore
- Serdol
- Anepro
- Vasocardin
- Corvitol
- Metobloc
- Metoprol
- Emzok
Metoprolol price, where to buy
The price of Metoprolol in tablets of 50 mg is on average 40 rubles per pack of 30 pieces.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Metoprolol tab.
50 mg No. 30Pranafarm LLC 31 rub. order - Metoprolol Retard-Akrikhin tablets p.p.o. prolonged action 25 mg 30 pcs. JSC Akrikhin
RUB 187 order
- Metoprolol-Akrikhin tablets 50 mg 30 pcs. JSC Akrikhin
61 rub. order
- Metoprolol Organica tablets 50mg 60pcsAO Organika
102 RUR order
- Metoprolol tablets p.o.p prolong. release 100 mg 30 pcs Vertex AO
RUB 293 order
Pharmacy Dialogue
- Metoprolol (25 mg tablet No. 60) Ozon LLC
62 RUR order
- Metoprolol retard-Akrikhin extended-release tablets 50 mg No. 30 Akrikhin OJSC
RUB 232 order
- Metoprolol retard-Akrikhin tablets 100 mg No. 30 Akrikhin OJSC
RUB 317 order
- Metoprolol (25 mg tablet No. 60) Organics (Novokuznetsk Autonomous Okrug)
74 RUR order
- Metoprolol (50 mg tablet No. 30) Ozon LLC
33 rub. order
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Pharmacy24
- Metoprolol tartrate 50 mg No. 20 tablets PAT "Farmak", Ukraine
13 UAH. order - Metoprolol-KMP 50 mg N30 tablets PAT "Kievmedpreparat", Ukraine
11 UAH order
- Metoprolol tartrate 100 mg No. 20 tablets PAT "Farmak", Ukraine
16 UAH order
- Metoprolol-KMP 100 mg N30 tablets PAT "Kievmedpreparat", Ukraine
20 UAH order
