Comparative analysis of the effectiveness and safety of various dosage forms of metoprolol in the treatment of cardiovascular diseases

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.

pharmachologic effect

Manufacturer: Ozone (Russia)
Release form: tablets

Active ingredient: metoprolol

Analogs: Bisoprolol, Anaprilin, Betalok zok

Metoprolol belongs to the group of selective beta-blockers. Based on the chemical composition, there are 2 forms of the drug: Metoprolol tartrate and Metoprolol succinate. The medication reduces the frequency and severity of angina attacks, lowers blood pressure and restores the rhythm of heart contractions.

Under the influence of the drug, the need for oxygen in the cellular structures of the myocardium decreases, and the tolerance of the heart muscle to physical activity increases.

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.

Metoprolol or Betaloc ZOK – which is better?

Manufacturer: AstraZeneca AB (Sweden)
Release form: tablets

Active ingredient: metoprolol succinate

Betaloc ZOK is a selective beta1-blocker. Its characteristic feature is the prolonged release of the active substance. This effect of the medication tablets helps maintain a constant concentration of the drug in the blood for 24 hours or more. It is prescribed for the following pathologies:

• angina pectoris;
• heart rhythm disturbance;
• arterial hypertension.

The drug is used for myocardial infarction after the acute phase, as well as to prevent the development of a repeated acute ischemic state.

According to reviews from cardiologists, the best treatment for coronary heart disease, arrhythmia and high blood pressure is Betaloc ZOK. This is a long-acting drug, the concentration of which in the blood is maintained for a day or more.

It is well tolerated by patients, has a mild effect and rarely causes side effects. The Betaloc analogue is convenient to take, as it is taken once a day.

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.

Metoprolol or Concor - which is better for arrhythmia

Manufacturer: Merck KGaA (Germany)
Release form: tablets

Active ingredient: bisoprolol

Metoprolol and its analog Concor have the same indications, but a different mechanism of action due to different active components. Medicines are used for chronic heart failure, arterial hypertension, coronary heart disease complicated by angina pectoris.

For arrhythmia, the best substitute for Metoprolol is Concor, since the drug is fast-acting. The patient's condition improves within half an hour from taking the medicine.

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”.

Nebivolol

Manufacturer: Salutas Pharma GmbH (Germany)
Release form: tablets

Active ingredient: nebivolol

Nebivolol belongs to the group of beta-blockers and is a racemate consisting of 2 enantiomers - L-Nebivolol and D-Nebivolol. The drug reduces blood pressure and pulse with a single dose. A stable hypotensive effect is observed 1–2 weeks after regular use of the drug.

Nebivolol is prescribed 2.5-5 mg 1 time in 1 half day. According to indications, the dosage of the medicine can be increased to 10 mg per day.

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.

Metoprolol or Bisoprolol - which is better for arrhythmia and tachycardia, what is the difference

Manufacturer: VERTEX (Russia)
Release form: tablets

Active ingredient: bisoprolol

Metoprolol and Bisoprolol belong to the same pharmacological group, have equivalent indications for use, but have a different mechanism of action, which is due to different active substances.

The action of Bisoprolol is aimed at reducing the symptoms of myocardial ischemia, normalizing blood pressure and restoring the heart rate. Despite the similarity of medications, there are differences between them:

• Metoprolol begins to act within half an hour after taking the drug, and Bisoprolol - 1–1.5 hours after its use;
• the duration of activity of the Bisoprolol analogue reaches 12 hours, so the drug is taken once a day, while for Metoprolol it lasts only up to 4 hours and is taken several times a day;
• Metoprolol is excreted from the body only through the liver, which creates additional stress on the organ, and Bisoprolol is removed through the kidneys and liver.

According to doctors, Bisoprolol is well tolerated and is more often prescribed for arrhythmia or tachycardia, since it effectively copes with this cardiac pathology and is convenient to take once a day.

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.

Coronal

Manufacturer: AS Zenvita (Czech Republic)
Release form: tablets

Active ingredient: bisoprolol

Coronal is a selective beta-blocker. Under the influence of the medication, blood pressure is reduced, heart rhythm is restored, and angina attacks are prevented during myocardial ischemia.

The Coronal analogue, after oral administration, is well absorbed into the bloodstream and 90% of the medication enters the blood plasma, reaching its maximum after 2–3 hours. The drug is prescribed at a dose of 2.5-5 mg with possible adjustment according to indications.

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.

Metoprolol or Anaprilin - which is better?

Manufacturer: Sintez OJSC (Russia)
Release form: tablets

Active ingredient: propranolol

Anaprilin and Metoprolol are beta-blockers, the active substances of which are:

• reduce heart rate;
• reduce myocardial oxygen demand;
• reduce blood pressure;
• effectively reduce attacks of angina in coronary heart disease;
• restore heart rhythm.

In this case, Metoprolol will be the best, since it is more active due to the larger amount of active ingredient in the drug. Its concentration in the blood plasma remains for up to 12 hours, while its analog Anaprilin is eliminated from the body after 3-4 hours.

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 or Egilok – which is better?

Manufacturer: Egis (Hungary)
Release form: tablets

Active ingredient: metoprolol

Metoprolol and its analogue Egilok have the same active ingredient. Both drugs actively stop attacks of atrial fibrillation and tachycardia, reduce pulse and blood pressure to normal within 2 weeks of taking the drug. Egilok, with fewer side effects, is well tolerated by patients.

According to doctors, the best results are observed with treatment with Egilok. This is a “purer” drug, since higher quality raw materials are used in its production.

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

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 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

  185 rub. order

• Metoprolol-Akrikhin tablets 50 mg 30 pcs. JSC Akrikhin

  60 rub. order

• Metoprolol Organica tablets 50mg 60pcsAO Organika

  102 RUR order

• Metoprolol-Teva tablets 50 mg 30 pcs. Merkle GmbH

  29 RUR order

Pharmacy Dialogue

• Metoprolol-Akrikhin tablets 50 mg No. 30 Akrikhin OJSC

  56 RUR order

• Metoprolol retard-Akrikhin tablets 100 mg No. 30 Akrikhin OJSC

  RUB 271 order

• Metoprolol retard-Akrikhin extended-release tablets 25 mg No. 30 Akrikhin OJSC

  47 RUR order

• Metoprolol (25 mg tablet No. 60) Ozon LLC

  59 RUR order

• Metoprolol (25 mg tablet No. 60) Organics (Novokuznetsk Autonomous Okrug)

  62 RUR order

show more

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

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.

Analogues of the drug Metoprolol Succinate

Active analogues of the drug Metoprolol Succinate:

• Betalok;
• Vasocardin;
• Corvitol;
• Metozok;
• Metocard;
• Metolol;
• Serdol;
• Egilok;
• Emzok.

Diseases associated with disruption of the heart and blood vessels cannot be ignored. If your blood pressure regularly increases, you should consult a doctor who will conduct an examination to identify the reasons for the persistent increase. For hypertension, the doctor will prescribe medication.

If a doctor prescribes Metoprolol, you cannot decide on its own to discontinue it or replace it with analogues. You should consult your doctor before you start taking Metoprolol replacement.

Metoprolol tablets 25 mg No. 15x4

Name

Metoprolol.

Release form

Pills.

Dosage

25 mg. Quantity per package: 60 pcs.

Manufacturer

Lekpharm sooo.

INN

Metoprolol.

FTG

Beta1-adrenergic blocker selective.

Description

Tablets are white, flat-cylindrical in shape, with a bevel (dosages 25 mg and 50 mg). Tablets are white, flat-cylindrical in shape, beveled and scored (dosage 100 mg).

Compound

Each tablet contains: active substance: metoprolol tartrate – 25 mg, 50 mg or 100 mg; excipients: colloidal anhydrous silicon dioxide, microcrystalline cellulose, sodium starch glycolate (type A), talc, magnesium stearate, lactose monohydrate.

Pharmacotherapeutic group

Beta blockers. Selective beta blockers. Metoprolol. ATX code: C07A B02

Pharmacological properties

Pharmacodynamics Metoprolol is a beta-blocker. It does not have internal sympathomimetic activity. High blood pressure is reduced both in a standing and lying position. Does not cause orthostatic hypotension and does not affect the electrolyte composition of the blood. It has antianginal, antihypertensive and antiarrhythmic effects. Reduces the stimulating effect of catecholamines on the heart during physical and psychoemotional stress, leading to a decrease in heart rate, myocardial contractility, and cardiac output. In the first days of use, the drug increases peripheral vascular resistance, which normalizes or even decreases with long-term use. Reduces myocardial oxygen demand (due to a decrease in heart rate and reduced myocardial contractility), reduces the number and severity of angina attacks and increases exercise tolerance. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia, functional heart disease and hyperthyroidism, it reduces heart rate and can lead to restoration of sinus rhythm. The antiarrhythmic effect is due to a decrease in the rate of spontaneous excitation of the sinus and ectopic pacemaker and a slowdown in AV conduction. Prevents the development of headaches of vascular origin. To a lesser extent than non-selective beta-blockers, it affects the release of insulin and carbohydrate metabolism, masks the symptoms of hypoglycemia in patients with diabetes, increases the content of triglycerides in the blood, reduces the content of free fatty acids and high-density lipoproteins. Pharmacokinetics Absorption and distribution After taking the drug orally, metoprolol is almost completely (approximately 95%) absorbed from the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1.5–2 hours. The bioavailability of metoprolol is approximately 50% with a single dose and approximately 70% with multiple doses. Concomitant food intake can increase the bioavailability of metoprolol by 30–40%. Plasma protein binding – 10%. Penetrates through the BBB and placental barrier, excreted in breast milk. Metoprolol is widely distributed in tissues and has a large volume of distribution (5.6 l/kg). Metabolism and excretion Metoprolol is intensively biotransformed in the liver with the formation of inactive metabolites. The plasma half-life ranges from 1 to 9 hours (average 3.5 hours). The total clearance of the drug is about 1 l/min. It is excreted mainly by the kidneys (95%), about 5% - unchanged, the rest - in the form of metabolites. Separate groups of patients There were no significant differences in the pharmacokinetics of metoprolol in elderly patients. If renal function is impaired, the excretion of metabolites decreases and the excretion of unchanged metoprolol remains virtually unchanged. In severe renal failure (GFR 5 ml/min), a significant accumulation of metabolites is observed, but the degree of beta-adrenergic blockade does not increase. Impaired liver function has little effect on the pharmacokinetics of metoprolol. However, in severe liver cirrhosis and/or after a portacaval shunt, bioavailability may increase and total clearance may decrease. After portacaval shunting, the total clearance of the drug is approximately 0.3 L/min, and the area under the concentration-time curve increases approximately 6-fold compared with healthy individuals.

Indications for use

Arterial hypertension; Angina; stable symptomatic chronic heart failure with impaired left ventricular systolic function (as an adjuvant therapy to the main treatment of chronic heart failure); reduction in mortality and recurrent infarction after the acute phase of myocardial infarction; heart rhythm disturbances, including supraventricular tachycardia, decreased ventricular contraction frequency with atrial fibrillation and ventricular extrasystoles; functional disorders of cardiac activity accompanied by tachycardia; prevention of migraine attacks; as an adjuvant for hyperthyroidism.

Directions for use and doses

The dosage is selected individually according to the symptoms of the disease. The tablets are taken orally during or after meals, without chewing and with a sufficient amount of drinking water. During dose selection, heart rate should be monitored to prevent bradycardia. The duration of the course of therapy is determined by the doctor individually and depends on the characteristics of the disease. If, after long-term use of the drug, it is necessary to stop treatment, then this should be done gradually and slowly, since sudden discontinuation of the drug can lead to a sharp increase in blood pressure. Arterial hypertension. For moderate to moderate arterial hypertension, the initial dose is 25–50 mg twice a day (morning and evening). If necessary, the daily dose can be gradually increased to 200 mg (100 mg in the morning and evening) or another antihypertensive agent can be added. Angina pectoris. The initial dose is 25–50 mg two to three times a day. Depending on the effect, this dose can be gradually increased to 200 mg per day in two divided doses or another antianginal drug can be added. Secondary prevention of myocardial infarction. The usual dose is 50–100 mg twice daily (morning and evening). Arrhythmias. The initial dose is 25–50 mg two to three times a day. If necessary, the daily dose can be gradually increased to 200 mg or another antiarrhythmic agent can be added. Hyperthyroidism. The dose should be set individually. Recommendations for use: at the beginning of treatment, 50 mg 3-4 times a day; the dose can be increased to 100 mg 3–4 times a day if the heart rate is higher than 75 beats/min after 3–4 days of treatment with the initial dose of the drug. In hyperthyroidism, the biotransformation of metoprolol is increased, so it may be necessary to use a higher dose of the drug. The drug is usually used during the period of withdrawal from another drug. Functional heart disorders accompanied by tachycardia. The usual dose is 50 mg twice daily (morning and evening); if necessary, the single dose can be increased to 100 mg, maintaining the same dosage regimen. Prevention of migraine attacks. The usual dose is 50 mg twice daily (morning and evening); if necessary, it can be increased to 100 mg per day. Special groups of patients Renal dysfunction. There is no need to change the dosage of the drug in case of impaired renal function. Liver dysfunction. For patients suffering from liver disease, metoprolol is prescribed in the same doses as for patients whose liver function is not impaired. However, in cases of significant impairment of liver function (for example, after bypass surgery), it may be necessary to reduce the dose of metoprolol. Elderly patients. No dose adjustment is required. Children. Clinical experience with metoprolol in children is limited.

Side effect

The frequency of adverse reactions listed below was determined using the following notation: very common (> 1/10), common (> 1/100 - 1/1000 - 1/10,000 -

Contraindications

Hypersensitivity to metoprolol tartrate, other beta-adrenolytic agents or any other excipients. Second or third degree atrioventricular node block. Heart failure in the stage of decompensation (pulmonary edema, circulatory disorders or hypotension) and constant or periodic use of drugs that increase myocardial contractile function (beta-adrenergic receptor agonists). Symptomatic and clinical sinus bradycardia (heart rate 0.24 seconds or systolic pressure

Overdose

Symptoms: hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma. The symptoms listed above may increase with the simultaneous use of alcohol, antihypertensive drugs, quinidine and barbiturates. The first symptoms of an overdose appear 20 minutes to 2 hours after taking the drug. Treatment: intensive care and monitoring of the patient's vital functions (circulatory and respiratory, renal, glycemic, serum electrolytes) are necessary. If the drug was taken not too long ago, gastric lavage is mandatory; if lavage is not possible and the patient is conscious, vomiting can be induced (in the presence of medical personnel), followed by the administration of activated charcoal and an osmotic laxative. Atropine (0.25–0.5 mg IV for adults, 10–20 mcg/kg for children) should be given before gastric lavage (due to the risk of vagus nerve stimulation). For severe hypotension, bradycardia and risk of heart failure, beta1-agonists (dobutamine) should be administered intravenously at intervals of 2–5 minutes or by infusion until the desired effect is achieved. If selective beta1-agonists are not available, administer atropine or dopamine intravenously. In the absence of the desired effect, it is possible to use other adrenergic agonists (isoprenaline or norepinephrine). Administration of glucagon in doses of 1–10 mg is useful in achieving reversibility of the effects of beta-receptor blockade. In cases of severe bradycardia that are resistant to pharmacotherapy, implantation of a cardiac pacemaker may be required. Bronchospasm can be relieved by IV administration of a beta2-agonist (eg, salbutamol or terbutaline). These antidotes can be used in doses exceeding therapeutic ones. Hemodialysis is ineffective.

Use during pregnancy and lactation

Metoprolol should not be prescribed during pregnancy and breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and/or child. Pregnancy Beta-adrenolytic drugs may impair placental perfusion and cause fetal death and preterm birth. Intrauterine growth retardation has been observed after long-term use of metoprolol for pregnant women with mild to moderately elevated blood pressure. Beta-adrenolytic drugs can prolong labor and cause bradycardia in the fetus and newborn. There are also reports of hypoglycemia, hypotension, increased bilirubinemia, as well as a difficult response to tissue hypoxemia in the newborn. Treatment with the drug must be interrupted 48–72 hours before the planned date of birth. When this is not possible, the newborn should be monitored for 48 to 72 hours after birth for subjective and objective symptoms of beta-adrenergic blockade (eg, cardiac and pulmonary complications). Breastfeeding The concentration of metoprolol in milk is approximately three times higher than in blood plasma. Although the risk of harm to the nursing infant following therapeutic dosage is low (except in those with slow metabolisms), the breastfed infant should be monitored for signs of beta-adrenergic blockade.

Precautions and application features

If bradycardia increases, the dose of the drug must be reduced or the drug discontinued, gradually reducing the dose. Beta-adrenolytic drugs should be used cautiously in patients with bronchial asthma. If a patient with asthma is taking a beta2-agonist drug (in the form of tablets or inhalations), then, when starting treatment with metoprolol, the dose of the beta2-agonist should be monitored and increased if necessary. Metoprolol may interfere with glycemic control in the treatment of diabetes mellitus and mask signs of hypoglycemia. In patients with non-insulin-dependent diabetes mellitus, plasma glucose levels should be monitored. Disorders of atrioventricular conduction may sometimes intensify during treatment with metoprolol (possibility of atrioventricular node blockade). Metoprolol may lead to exacerbation of peripheral arterial disease such as intermittent claudication. In Prinzmetal's angina, beta blockers may increase the number and duration of attacks. In patients with psoriasis, an exacerbation of the disease may occur while taking metoprolol. Beta-adrenolytic drugs may worsen or cause the symptoms of lichen planus. In the case when metoprolol is prescribed to patients with tumors arising from chromaffin tissue (pheochromocytoma), it is necessary to first use an alpha-adrenolytic drug and continue its use simultaneously with metoprolol. Treatment with metoprolol may mask signs of thyroid hyperfunction. When performing general anesthesia while taking beta-blockers, the risk of developing arterial hypotension increases. If surgical intervention is necessary, the anesthesiologist should be informed about the therapy being carried out in order to select an anesthetic agent with minimal negative inotropic effect, however, discontinuation of the drug before surgery in patients with coronary artery disease is not recommended. Before conducting a radiological examination with iodinated contrast agents, treatment with metoprolol should be discontinued in advance. In cases where the use of metoprolol is absolutely necessary and cannot be discontinued, appropriate treatment must be prescribed. Avoid prescribing high doses of metoprolol immediately without prior titration to patients undergoing non-cardiac surgery, as it has been associated with bradycardia, hypotension and stroke, including death, in patients with cardiovascular risk factors. Just like other beta-adrenolytic drugs, metoprolol can increase both sensitivity to allergens and intensify anaphylactic reactions. Epinephrine does not always produce the desired therapeutic result in patients treated with beta-adrenolytic drugs. Patients with severe renal impairment, severe acute conditions involving metabolic acidosis, and patients receiving combination treatment with digitalis should be given special attention. For elderly people, the drug is prescribed with caution in low doses and under constant medical supervision with regular monitoring of kidney function indicators. Patients who use contact lenses should take into account that during treatment with beta-blockers, there may be a decrease in the production of tear fluid. The drug Metoprolol contains lactose monohydrate. It should not be used in patients with rare hereditary galactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome.

Impact on the ability to drive vehicles or potentially dangerous mechanisms

Use with caution while working for vehicle drivers and people whose profession involves increased concentration. Dizziness and fatigue may occur during treatment with metoprolol, so patients should assess their response to the medication before driving or operating mechanical devices while in motion. The described symptoms may intensify if you drink alcohol at the same time or after changing medications.

Interaction with other drugs

Metoprolol is a CYP2D6 substrate, and therefore drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) may affect the plasma concentrations of metoprolol tartrate. The combined use of Metoprolol with the following drugs should be avoided: barbituric acid derivatives. Barbiturates increase the metabolism of metoprolol due to enzyme induction. Propaphenone. When propafenone was prescribed to four patients treated with metoprolol, an increase in plasma concentrations of metoprolol was observed by 2-5 times, while two patients experienced side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. The interaction is likely due to propafenone's inhibition, like quinidine, of the metabolism of metoprolol via the cytochrome P4502D6 system. Taking into account the fact that propafenone has beta-blocker properties, the co-administration of metoprolol and propafenone does not seem appropriate. Verapamil. The combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function. The combination of Metoprolol with the following drugs may require dose adjustment of Amiodarone. The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia. Given the extremely long half-life of amiodarone (50 days), a possible interaction should be considered long after discontinuation of amiodarone. Class I antiarrhythmic drugs. Class I antiarrhythmics and beta-blockers may result in additive negative inotropic effects, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with sick sinus syndrome and impaired AV conduction. The interaction is described using disopyramide as an example. Nonsteroidal anti-inflammatory drugs (NSAIDs). NSAIDs weaken the antihypertensive effect of beta-blockers. Studies have focused primarily on indomethacin. This effect will not occur when interacting with sulindac. In studies with diclofenac, no such interaction was found. Diphenhydramine. Diphenhydramine reduces the clearance of metoprolol to α-hydroxymetoprolol by 2.5 times. At the same time, an increase in the effect of metoprolol is observed. Diltiazem: Diltiazem and beta-blockers mutually enhance the inhibitory effect on AV conduction and sinus node function. When metoprolol was combined with diltiazem, cases of severe bradycardia were observed. Epinephrine. Ten cases of severe hypertension and bradycardia have been reported in patients taking non-selective beta blockers (including pindolol and propranolol) and receiving epinephrine. The interaction was also observed in the group of healthy volunteers. It is assumed that similar reactions can be observed when epinephrine is used together with local anesthetics if it accidentally enters the vascular bed. It is assumed that this risk is much lower with the use of cardioselective beta-blockers. Phenylpropanolamine. Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values ​​in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, beta-blockers may cause paradoxical hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported while taking phenylpropanolamine. Quinidine. Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation, mainly causing a significant increase in plasma concentrations of metoprolol and increased beta blockade. It is believed that a similar interaction is typical for other beta-blockers, the metabolism of which involves cytochrome P4502D6. Clonidine. Hypertensive reactions during abrupt withdrawal of clonidine may be exacerbated by concomitant use of beta-blockers. When used together, if clonidine is discontinued, discontinuation of beta-blockers should begin several days before discontinuation of clonidine. Rifampicin. Rifampicin may increase the metabolism of metoprolol, reducing plasma concentrations of metoprolol. Patients concomitantly taking metoprolol and other beta-blockers (eye drops) or monoamine oxidase inhibitors should be closely monitored. While taking beta-blockers, inhalational anesthetics enhance the cardiodepressive effect. While taking beta-blockers, patients receiving oral hypoglycemic agents may require dose adjustment of the latter. Plasma concentrations of metoprolol may increase when taking cimetidine or hydralazine. Cardiac glycosides, when used together with beta-blockers, can increase atrioventricular conduction time and cause bradycardia. Metoprolol may cause a decrease in the elimination of other drugs (eg lidocaine).

Storage conditions

In a place protected from moisture and light at a temperature not exceeding 25 °C. Keep out of the reach of children.

Best before date

2 years. Do not use after the expiration date stated on the packaging.

Package

10 tablets with a dosage of 25 mg, 50 mg and 100 mg in a blister pack made of polyvinyl chloride film and aluminum foil. Three blister packs for dosages of 50 mg and 100 mg, six blister packs for dosages of 25 mg and 50 mg along with instructions for use in a cardboard pack.

Release from pharmacies

By doctor's prescription.

Buy Metoprolol tablet 25 mg in container pack No. 15x4 in the pharmacy

Price for Metoprolol tablet 25 mg in container pack No. 15x4

Instructions for use for Metoprolol tablet 25 mg in container pack No. 15x4