Metoprolol from what they. Metoprolol - stamina and peace of mind, as well as an active life of a person. Application restrictions

A cardiological drug with a pronounced hypotensive effect. Used to treat hypertension, heart failure and other similar problems. It is prescribed for adult patients only. Use during pregnancy is prohibited. Long-term and regular use of metoprolol is recommended to achieve a stable clinical result.

Dosage form

The antihypertensive drug Metoprolol is available in the form of white, yellowish-white and pink biconvex round film-coated tablets with an active element content of 25, 50 and 100 mg.

The primary package (blister) contains 10 and 14 units of medication. The product is packaged in cardboard boxes (secondary packaging) of 2, 3 or 4 blisters.

Description and composition

The active ingredient in Metoprolol is metoprolol tartrate. The substance is a selective beta-adrenergic blocker with a pronounced hypotensive effect.

Auxiliary components in the composition of tablets are:

anhydrous silicon dioxide (colloidal);
microcrystalline cellulose;
magnesium stearate;
sodium carboxymethyl starch.

The composition of the film shell:

dyes (for pink tablets);
talc;
hypromellose;
titanium dioxide;
polysorbate 80.

Pharmacological group

The drug Metoprolol belongs to the pharmacological group of selective beta1-adrenergic blockers. It does not have an internal sympathomimetic effect. It has a pronounced antianginal, antiarrhythmic and hypotensive effect. Metoprolol tartrate significantly reduces the stimulation of cardiac activity caused by adrenaline and other hormonal catecholamines. Under the action of the drug, the heart rate decreases, the load on the heart muscle, the automatism of the sinus node, and the level of blood pressure, peripheral vascular resistance and myocardial oxygen demand decreases.

The development of the hypotensive effect occurs gradually. The maximum therapeutic effect is observed after 2-3 weeks of continuous use. In patients with an increased risk of getting a second myocardial infarction, the likelihood of relapse is significantly reduced. While taking the drug, there is a decrease in the frequency of angina attacks and an improvement in their tolerability.

Unlike non-selective beta-adrenergic blockers, Metoprolol, used in medium therapeutic dosages, does not have a pronounced effect on the smooth muscles of the peripheral arteries and bronchi.

The bioavailability of the active substance is on average 35%. The concentration of metoprolol tartrate in the blood serum reaches a maximum after 1.5-2 hours after the initial dose. In the liver, the substance is metabolized to form inactive metabolites. The duration of the half-life can be from 3 to 5 hours. The drug is excreted by the kidneys.

Indications for use

Metoprolol is prescribed for the prevention and treatment of a number of disorders in the functioning of the cardiovascular system.

for adults

arterial hypertension;
chronic form of heart failure;
angina;
heart rhythm disturbances;
migraine prevention;
cardiac syndrome of hyperkinetic type;
prevention of recurrence of myocardial infarction.

for kids

The use of Metoprolol by children under 18 years of age is strictly prohibited.

During pregnancy or breastfeeding, the use of metoprolol for the treatment or prevention of diseases of the cardiovascular system is possible only when the benefit to the woman is much higher than the possible risks to the development of the child or fetus. The main danger lies in provoking metoprolol tartrate bradycardia, hypoglycemia and arterial hypotension in the fetus / child. Patients during lactation should immediately stop breastfeeding.

Contraindications

atrioventricular blockade of the 2nd and 3rd degree;
stage of decompensation of heart failure;
pregnancy and HB;
weakness of the sinus node;
bradycardia;
children's age up to 18 years;
pathologically high sensitivity to metoprolol tartrate;
arterial hypotension;
SA blockade;
variant (spontaneous) angina pectoris.

Carefully:

bronchial asthma;
renal and / or liver failure in a chronic form;
depressive states;
elderly age;
Raynaud's syndrome;
thyrotoxicosis;
myasthenic fatigue;
psoriasis.

Applications and doses

Metoprolol tablets should be taken after meals or directly during meals with plenty of clean water.

for adults

With arterial hypertension, the average daily dosage can be from 50 mg to 100 mg of the drug. This amount of funds must be divided into two doses (preferably in the morning and evening). The maximum dosage is 200 mg per day.

For the prevention of migraines, as well as the treatment of angina pectoris and arrhythmias, it is recommended to use from 100 mg to 200 mg of the drug.

In the prevention of recurrence of myocardial infarction, it is necessary to take 100 mg of metoprolol twice a day.

for kids

Children under 18 years of age taking the drug is strictly contraindicated due to insufficient information about the safety of use.

for pregnant women and during lactation

For pregnant patients, an individual dosage calculation is necessary to minimize the negative impact on fetal development. During lactation, it is necessary to abandon breastfeeding. Correction of the scheme of reception and dosages is not required.

Side effects

headache;
nausea and;
loss of consciousness (rare);
pain in the abdomen;
blurred vision and dry eyes;
feeling of weakness and increased fatigue;
insomnia;
arrhythmia;
violation of taste perception;
rash and itching of the skin;
exacerbation of psoriasis;
deterioration of the liver;
decrease in contractile function of the myocardium;
hypotension;
hypoglycemia in patients with;
leukopenia;
thrombocytopenia;
joint pain;
decreased libido;
hypothyroidism;
shortness of breath and / or a feeling of congestion in the nasal cavity.

Interaction with other drugs

Taking NSAIDs provokes a decrease in the antihypertensive effectiveness of the drug. Antiarrhythmic drugs in combination with metoprolol increase the risk of bradycardia, hypotension and cardiac arrhythmias. The simultaneous use of diltiazem and is contraindicated. The reason is the high probability of cardiac arrest. Antihypertensive drugs enhance the effect of metoprolol. The simultaneous therapeutic use of antidiabetic drugs can cause the development of hypoglycemia. When combined with alcohol, the mutual inhibitory effect on the central nervous system increases.

special instructions

During the course of treatment with Metoprolol, it is necessary to monitor heart rate, blood pressure and blood glucose levels in patients with. Abrupt withdrawal of the use of the drug can provoke a withdrawal syndrome (a sharp increase in blood pressure and increased angina pectoris). Therapy for heart failure should be started exclusively at the stage of compensation. Increase or absence of susceptibility to adrenaline (epinephrine) is possible. Beta-blockers can reduce tear production. The drug can provoke depression in patients with a predisposition. In this case, the drug should be stopped. Due to the high likelihood of developing disorders of psychomotor reactions, patients should refrain from working with dangerous or high-precision mechanisms, driving vehicles and practicing extreme sports.

Overdose

With drug intoxication with metoprolol tartrate, the following symptoms are observed:

arrhythmia;
a sharp drop in blood pressure;
feeling of nausea and urge to;
dizziness;
sinus bradycardia in severe form;
bronchospasm;
blue coloration of the skin and mucous membranes (cyanosis);
headache;
ventricular extrasystole.

In the event of an extreme degree of poisoning, the following conditions are possible:

fainting;
atrioventricular blockade (up to cardiac arrest);
cardiogenic shock;
coma;
cardiac syndrome.

Therapy activities:

reception of a large number of sorbents;
gastric lavage;
symptomatic treatment.

Analogues

Instead of metoprolol, the following medicines can be used:

ZOK is a Swiss original drug containing metoprolol, which is produced in tablets with a delayed release of the active substance. They are not allowed for minors. When the benefit to the mother outweighs the risk to the fetus, the drug can be prescribed to pregnant and lactating women.
Hypotef is a combined drug that, in addition to metoprolol, contains,. It is produced in tablets, which are used to treat arterial hypertension in people over 45 years of age.
Logimax is a combination drug containing, in addition to metoprolol, felodipine. It is produced in tablets of prolonged action. They have antianginal, antiarrhythmic and hypotensive effects. The drug is used for arterial hypertension in adults, except for pregnant and lactating patients.
contains as an active component . The drug is produced in tablets that can be used in adults suffering from high blood pressure, stable angina, chronic heart failure. With caution, the medicine can be given to women in position. At the time of therapy, the child should be transferred to the mixture.

Storage conditions

It is necessary to store Metoprolol in a dark place, as far as possible from children, at a temperature of at least 15 and no more than 25 degrees.

Shelf life - 5 years.

The price of the drug

The cost of the drug is an average of 177 rubles. Prices range from 16 to 431 rubles.

Metoprolol: instructions for use and reviews

Latin name: Metoprolol

ATX Code: C07AB02

Active substance: metoprolol

Manufacturer: Ozone (Russia), Moscow Endocrine Plant (Russia), Hemopharm (Serbia), Adipharm (Bulgaria), Biochemist (Russia), Marbiopharm (Russia), Zentiva (Slovakia), Organica (Russia), Ratiopharm (Germany)

Description and photo update: 07.08.2019

Metoprolol is a selective beta-1 blocker.

Release form and composition

Dosage forms:

Tablets: white with a gray tint or white, with a chamfer on both sides and a dividing line on one side, have a round flat shape, 100 mg each (10 or 30 pieces in a blister pack, in a carton box from 1 to 10 packs ; 10, 20, 30, 40, 50, 60, 70, 80, 90 or 100 pieces in polymer containers, in a cardboard bundle 1 container; 10 pieces in blisters, in a cardboard bundle 3 or 5 blisters), 50 mg (in blisters: 10 pcs., in a carton pack 1, 2, 3, 5 or 10 packs, 15 or 20 pcs., in a carton pack 2 packs, 30 pcs., in a carton pack 1 or 2 packs; in polymer containers of 20, 30, 40 or 50 pcs., in a carton pack 1 container), 25 mg each (in blisters: 10 pcs., in a carton pack 1 package, 30 pcs., in 1 or 2 packs in a carton pack; 20, 40 or 50 pieces in polymer containers, 1 container in a carton pack);
Film-coated tablets: round, biconvex, with a dividing line on one side, may be pinkish or white to yellowish-white in color, 50 mg each (14 pieces in blisters, in a carton pack of 2 or 4 blisters), 100 mg each (10 pieces in blisters, 3 blisters in a carton box).

Active ingredient - metoprolol tartrate:

1 tablet - 25 mg, 50 mg or 100 mg;
1 film-coated tablet - 50 mg (pink) or 100 mg.

Auxiliary components:

Tablets: microcrystalline cellulose, lactose monohydrate, potato starch, povidone, sodium carboxymethyl starch, magnesium stearate;
Film-coated tablets: sodium carboxymethyl starch (type A), microcrystalline cellulose, anhydrous colloidal silicon dioxide, magnesium stearate.

Additionally, as part of the shell: polysorbate 80, hypromellose, titanium dioxide (E171), talc; in the pink shell there is a dye crimson (Ponceau 4R).

Pharmacological properties

Pharmacodynamics

Metoprolol is a cardioselective beta1-blocker. It has antiarrhythmic, antianginal, antihypertensive and insignificant membrane stabilizing effects.

By blocking beta1-adrenergic receptors of the heart, the formation of cAMP (cyclic adenosine monophosphate) stimulated by catecholamines from ATP (adenosine triphosphate) decreases, intracellular calcium current decreases, heart rate slows down, myocardial contractility decreases, excitability and conductivity are inhibited.

In the first 24 hours after taking beta-blockers, the total peripheral vascular resistance increases, after 1-3 days it returns to its original value, and with prolonged use of the drug it decreases.

The antihypertensive effect of metoprolol is due to the following effects:

decrease in minute volume of blood;
decreased renin synthesis;
inhibition of the activity of the renin-angiotensin-aldosterone system;
suppression of the activity of the central nervous system;
restoration of the sensitivity of baroreceptors of the aortic arch;
decrease in peripheral sympathetic influences.

The drug reduces high blood pressure during stress, physical exertion and at rest. The antihypertensive effect of metoprolol develops quite quickly: it takes from 15 minutes to 2 hours to lower systolic blood pressure (the effect persists for 6 hours); for a stable decrease in diastolic blood pressure, regular administration of the drug for several weeks is necessary.

The antianginal effect of metoprolol is determined by a decrease in the oxygen demand of the heart muscle due to a decrease in contractility and heart rate, as well as a decrease in the sensitivity of the myocardium to the influence of sympathetic innervation. Metoprolol reduces the number and severity of angina attacks and increases exercise tolerance. In some patients, especially those suffering from chronic heart failure, an increase in myocardial oxygen demand is possible due to an increase in the end-diastolic pressure in the left ventricle and a stronger stretching of the muscle fibers of the ventricles.

The antiarrhythmic effect of metoprolol is due to the following effects:

elimination of arrhythmogenic factors (arterial hypertension, tachycardia, increased cAMP content, increased activity of the sympathetic nervous system);
slowing atrioventricular conduction;
decrease in the rate of spontaneous excitation of ectopic and sinus pacemakers.

The drug slows down the heart rate and can restore the rhythm in patients with atrial fibrillation, supraventricular and sinus tachycardia with thyrotoxicosis and functional heart diseases.

Metoprolol helps prevent the development of migraine attacks.

It differs from non-selective beta-blockers in that, when used in average therapeutic doses, it has less effect on carbohydrate metabolism and organs containing beta2-adrenergic receptors (smooth muscles of the bronchi, peripheral arteries and uterus, skeletal muscles, pancreas). When taking high doses of the drug (more than 100 mg per day), beta1- and beta2-adrenergic receptors are blocked.

Pharmacokinetics

Metoprolol is 95% absorbed in the gastrointestinal tract. It has moderate solubility in fats. At the first dose, bioavailability is 50%, with repeated use it increases to 70%. The drug is 10% bound to plasma proteins. The maximum concentration is reached in 1.5-2 hours. With course treatment with metoprolol, its bioavailability increases. Simultaneous intake with food increases bioavailability by 20-40%.

Metoprolol quickly penetrates into all tissues, as well as through the blood-brain and placental barriers. It is excreted in breast milk (the concentration in breast milk exceeds the concentration in plasma).

Metabolism of the drug occurs in the liver with the participation of the CYP2D6 isoenzyme. Two metabolites have a beta-adrenergic blocking effect. The elimination half-life when taken orally is 3.5–7 hours. It is not removed by hemodialysis.

With a creatinine clearance of 5 ml / min, a significant accumulation of metabolites is observed, but the activity of the drug does not increase.

In hepatic insufficiency, the bioavailability of metoprolol increases, and its total clearance is reduced.

Indications for use

Ischemic heart disease: myocardial infarction (as part of the complex therapy of secondary prevention), prevention of angina attacks;
Monotherapy or as part of combination treatment (with other antihypertensive agents) of arterial hypertension, including hyperkinetic type, tachycardia;
Hyperthyroidism (as part of complex therapy);
Heart rhythm disturbances, including ventricular extrasystole, supraventricular tachycardia;
Prevention of migraine attacks.

Contraindications

Cardiogenic shock;
Sinoatrial (SA) block;
Atrioventricular (AV) block II-III degree;
Severe bradycardia;
Sick sinus syndrome;
Prinzmetal's angina;
Heart failure in the stage of decompensation;
Arterial hypotension (for secondary prevention of myocardial infarction - with systolic blood pressure (BP) below 100 mm Hg and heart rate (HR) less than 45 beats per minute);
Simultaneous therapy with monoamine oxidase inhibitors (MAO) or verapamil;
Age up to 18 years;
The period of breastfeeding;
Hypersensitivity to the components of the drug or other beta-blockers.

With caution, it is recommended to prescribe metoprolol to patients with AV blockade of the 1st degree, metabolic acidosis, diabetes mellitus, chronic obstructive pulmonary disease (chronic obstructive bronchitis, pulmonary emphysema), bronchial asthma, obliterating peripheral vascular disease (Raynaud's syndrome, intermittent claudication), myasthenia gravis, chronic renal and / or liver failure, pheochromocytoma, thyrotoxicosis, psoriasis, depression (including history), in old age and during pregnancy.

Instructions for use Metoprolol: method and dosage

The tablets are taken whole orally, during or immediately after a meal, with a sufficient amount of liquid.

The dosage regimen is prescribed by the doctor based on clinical indications.

Secondary prevention of myocardial infarction: 200 mg in 2 doses (morning and evening);
Arterial hypertension: initial dose of 50-100 mg in 1 or 2 doses. To achieve a therapeutic effect, a gradual increase in dose to 100-200 mg and / or the simultaneous administration of other antihypertensive drugs is indicated. The daily dose should not exceed 200 mg;
Tachycardia against the background of functional disorders of cardiac activity: 100 mg in 2 divided doses;
Angina pectoris, arrhythmias, prevention of migraine attacks: 100-200 mg in 2 divided doses.

Dose adjustment is not required for impaired renal function, the need for hemodialysis, and the treatment of elderly patients.

Appointment of metoprolol to patients with functional disorders of the liver should be made in accordance with their clinical condition.

Side effects

Cardiovascular system: palpitations, sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, loss of consciousness); rarely - a decrease in myocardial contractility, arrhythmias, a temporary increase in symptoms of chronic heart failure (shortness of breath, swelling, including the feet and / or lower legs), manifestation of angiospasm (coldness of the lower extremities, increased peripheral circulatory disorders, Raynaud's syndrome), cardialgia, impaired myocardial conduction;
Nervous system: weakness, increased fatigue, slowing down of the speed of psychomotor reactions, headache; rarely - anxiety, muscle weakness, paresthesia in the limbs (against the background of intermittent claudication and Raynaud's syndrome), drowsiness, depression, insomnia, decreased attention, confusion, nightmares, short-term memory impairment;
Digestive system: dry mouth, nausea, vomiting, taste changes, abdominal pain, diarrhea or constipation, liver dysfunction;
Sense organs: rarely - tinnitus, decreased secretion of lacrimal fluid, decreased vision, conjunctivitis, dryness and soreness of the eyes;
Skin: itching, rash, urticaria, increased sweating, exacerbation of psoriasis, psoriasis-like reactions, exanthema, hyperemia, photodermatosis, reversible alopecia;
Endocrine system: hypoglycemia (with insulin-dependent diabetes mellitus); rarely - hypothyroidism, hyperglycemia (in diabetes mellitus);
Respiratory system: nasal congestion, shortness of breath, difficulty exhaling (bronchospasm at high doses);
Laboratory indicators: rarely - agranulocytosis, thrombocytopenia (unusual hemorrhages and bleeding), leukopenia, increased activity of hepatic transaminases; very rarely - hyperbilirubinemia;
Impact on the fetus: possible intrauterine bradycardia, growth retardation, hypoglycemia;
Other: back or joint pain; in isolated cases - a slight increase in body weight, a decrease in potency and libido.

The likelihood and severity of side effects depend on the individual sensitivity of the patient, as a rule, they are minor and transient.

Overdose

In case of overdose, the following symptoms occur: dizziness, cyanosis, vomiting, nausea, bronchospasm, severe severe sinus bradycardia, arrhythmia, fainting, marked decrease in blood pressure, ventricular extrasystole. In acute overdose, atrioventricular blockade, cardiogenic shock, cardialgia, coma, loss of consciousness may occur.

The first signs of an overdose occur 20 minutes - 2 hours after taking the drug.

The patient should be given a gastric lavage and an adsorbent administered. Symptomatic therapy is carried out: with a decrease in blood pressure, the patient is placed in a prone position with a slightly raised pelvis and legs; with an excessive decrease in blood pressure, heart failure and bradycardia, beta-agonists are administered intravenously at intervals of 2–5 minutes (until the desired effect is achieved) or atropine sulfate intravenously at a dose of 0.5–2 mg.

If there is no positive effect, dopamine, norepinephrine or dobutamine is administered.

In the future, it is possible to prescribe glucagon at a dose of 1–10 mg and install an electrical stimulator. In the case of bronchospasm, beta2-adrenergic stimulants are administered intravenously. Hemodialysis is ineffective.

special instructions

Treatment with beta-blockers must be accompanied by regular monitoring of heart rate and blood pressure, in patients with diabetes - the level of glucose in the blood (the dose of hypoglycemic agents or insulin is selected individually).

When prescribing the drug, the patient should be taught the method of self-calculation of heart rate and instructed to immediately consult a doctor if the heart rate is below 50 beats per minute.

The cardioselectivity of metoprolol at a dose of more than 200 mg per day is reduced.

The use of the drug in the treatment of heart failure should be started only in the stage of compensation.

In patients with a burdened allergic history, it is possible to increase the severity and lack of effect from the usual doses of epinephrine (adrenaline) in hypersensitivity reactions.

The drug may increase the symptoms of pathology of the peripheral arterial circulation.

Cancellation of the drug should be carried out by gradually reducing the dose within 10 days. Abrupt discontinuation of treatment can cause the patient to withdraw from the syndrome (increased blood pressure, increased angina attacks).

An individual dose of the drug for angina pectoris should provide the patient with a resting heart rate of 55-60 beats per minute, with a load - no higher than 110.

When using contact lenses, it is necessary to take into account the decrease in the production of lacrimal fluid while taking beta-blockers.

The drug may mask tachycardia and other symptoms of hyperthyroidism.

In patients with diabetes mellitus, taking metoprolol may mask tachycardia caused by hypoglycemia. With insulin-induced glycemia, the drug has practically no effect on the process of restoring the concentration of glucose in the blood to a normal level.

In bronchial asthma, the use of the drug is indicated with the simultaneous appointment of beta 2-adrenergic stimulants, with pheochromocytoma - alpha-blockers.

Before performing a surgical operation, it is necessary to inform the anesthesiologist about taking metoprolol so that general anesthesia is carried out with a minimum negative inotropic effect without discontinuation of the drug.

It should be borne in mind that with the simultaneous use of reserpine and other drugs that reduce the reserves of catecholamines and enhance the action of beta-blockers, an excessive decrease in blood pressure and the development of bradycardia are possible.

In elderly patients, it is necessary to monitor liver function, and with a strong decrease in blood pressure, AV blockade, the appearance of bronchospasm, ventricular arrhythmias, increasing bradycardia, severe liver dysfunction, dose adjustment or drug withdrawal is required.

In severe renal failure, regular monitoring of kidney function is required.

It is necessary to monitor the condition of patients with depressive disorders, if signs of depression appear, treatment should be discontinued.

At the beginning of the use of the drug, patients should be careful or refuse to drive vehicles and mechanisms, since during this period they may experience fatigue and dizziness. During treatment, dose safety is determined individually.

Use during pregnancy and lactation

For pregnant women, the drug is prescribed only according to strict indications, taking into account the benefit / risk ratio, since under the influence of Metoprolol, the development of bradycardia, hypoglycemia and arterial hypotension in the fetus is possible. It requires careful monitoring of the development of the fetus, as well as the newborn in the first 48-72 hours after delivery.

If necessary, the use of the drug during breastfeeding, breastfeeding should be discontinued.

Application in childhood

According to the instructions, metoprolol is contraindicated in children and adolescents under 18 years of age, since its efficacy and safety when used in childhood have not been established.

For impaired renal function

The drug is used with caution in patients with chronic renal failure.

For impaired liver function

The drug is used with caution in patients with chronic liver failure.

Use in the elderly

The drug is prescribed with caution to the elderly.

drug interaction

It is impossible to prescribe Metoprolol simultaneously with MAO inhibitors due to increased hypotensive effect, it is necessary to observe a break between taking the drugs for at least 14 days.

Intravenous (IV) administration of verapamil while taking metoprolol can cause cardiac arrest.

When used simultaneously with Metoprolol:

Nifedipine, ethanol - significantly reduce blood pressure;
Derivatives of hydrocarbons for inhalation anesthesia - increase the likelihood of developing arterial hypotension against the background of depression of myocardial function;
Theophylline, beta-agonists, cocaine, estrogens, indomethacin and other non-steroidal anti-inflammatory drugs - weaken the hypotensive effect;
Antipsychotics, tetra- and tricyclic antidepressants, hypnotics and sedatives and ethanol - increase the depression of the nervous system;
Ergot alkaloids - increase the risk of peripheral circulatory disorders;
Antihypertensive drugs, diuretics, slow calcium channel blockers or nitroglycerin - potentiate a sharp decrease in blood pressure (especially prazosin);
Diltiazem, verapamil, antiarrhythmic drugs (amiodarone), methyldopa, reserpine, clonidine, general anesthesia, guanfacine, cardiac glycosides - lead to a strong decrease in heart rate and inhibition of AV conduction;
Rifampicin, barbiturates (inducers of microsomal liver enzymes) - accelerate the metabolism of metoprolol, reducing its concentration in blood plasma and reducing the clinical effect;
Hypoglycemic agents for oral administration and insulin - reduce their effectiveness, the risk of developing hypoglycemia increases;
Oral contraceptives, cimetidine, phenothiazines (inhibitors) - increase the level of metoprolol concentration in blood plasma.

Metoprolol reduces the clearance of xanthine (except for difillin), especially in patients with increased clearance of theophylline due to smoking, increases the level of plasma lidocaine concentration, prolongs the anticoagulant effect of coumarins, prolongs and enhances the effect of antidepolarizing muscle relaxants.

The combination with allergen extracts used for skin tests and allergens for immunotherapy increases the likelihood of systemic allergic reactions (including anaphylaxis). When taken simultaneously with radiopaque iodine-containing agents for intravenous administration, the risk of anaphylactic reactions increases.

With the simultaneous use of metoprolol and clonidine, if it is necessary to stop treatment, clonidine should be canceled only a few days after metoprolol.

Analogues

Metoprolol's analogues are: Betaloc, Metocard, Metoprolol Retard-Akrikhin, Metoprolol-Akri, Metoprolol-Ratiopharm, Metoprolol-OBL, Metoprolol Organic, Metoprolol Zentiva, Anepro, Vasocardin, Corvitol, Metoblock, Metokor, Metoprol, Egilok, Emzok.

Terms and conditions of storage

Keep away from children.

Store in a dry, dark place at a temperature of 15-25°C.

Shelf life - 5 years.

Name:

Metoprolol (Metoprolol)

Pharmacological
action:

Cardioselective beta1-blocker without internal sympathomimetic activity. It has antihypertensive, antianginal and antiarrhythmic effects.
Reduces the automatism of the sinus node, reduces heart rate, slows down AV conduction, reduces myocardial contractility and excitability, reduces cardiac output, reduces myocardial oxygen demand. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.
Causes hypotensive effect, which stabilizes by the end of the 2nd week of course use.
In angina pectoris, metoprolol reduces the frequency and severity of attacks. Normalizes the heart rhythm with supraventricular tachycardia and atrial fibrillation.
In myocardial infarction, it helps to limit the zone of ischemia of the heart muscle and reduces the risk of developing fatal arrhythmias, reduces the possibility of recurrence of myocardial infarction.
When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.

Pharmacokinetics
After oral administration, metoprolol is rapidly and almost completely absorbed from the gastrointestinal tract, Cmax of the active substance in the blood plasma is reached after 1-2 hours.
Intensively metabolized in the liver with the formation of inactive metabolites.
T1 / 2 of metoprolol from plasma is 3-4 hours and does not change during the course of treatment. More than 95% of the dose taken is excreted by the kidneys, of which only 3% is unchanged.

Indications for
application:

Arterial hypertension;
- prevention of angina attacks;
- heart rhythm disorders (supraventricular tachycardia, extrasystole);
- secondary prevention after myocardial infarction;
- hyperkinetic cardiac syndrome (including with hyperthyroidism, NCD);
- prevention of migraine attacks.

Mode of application:

Inside, with food or immediately after a meal, tablets can be divided in half, but not chewed and washed down with liquid, for prolonged-release dosage forms - swallow whole, do not crush, do not break (except for metoprolol succinate and tartrate), do not chew.
With arterial hypertension the average dose is 100-150 mg / day in 1-2 doses, if necessary - 200 mg / day.
With angina - 50 mg 2-3 times a day.
With hyperkinetic cardiac syndrome (including thyrotoxicosis) - 50 mg 1-2 times a day. With tachyarrhythmia - 50 mg 2-3 times a day, if necessary - 200-300 mg / day.
Secondary prevention of myocardial infarction- 200 mg / day. Prevention of migraine - 100-200 mg / day in 2-4 doses.
For the relief of paroxysmal supraventricular tachycardia, it is administered parenterally, in a hospital setting. Enter slowly, a dose of 2-5 mg (1-2 mg / min).

If there is no effect, the administration can be repeated after 5 minutes. Increasing the dose above 15 mg usually does not lead to a greater severity of action.
After stopping the attack of arrhythmia, patients are transferred to oral administration at a dose of 50 mg 4 times a day, with the first dose being taken 15 minutes after the cessation of intravenous administration.

In the acute stage of myocardial infarction immediately after the patient's hospitalization (with constant monitoring of hemodynamics: ECG, heart rate, AV conduction, blood pressure), a 5 mg intravenous bolus should be administered, repeating the administration every 2 minutes until a total dose of 15 mg is reached.
With good tolerance after 15 minutes - inside, 25-50 mg every 6 hours, for 2 days.
In patients who have not tolerated the full intravenous dose, oral administration should be initiated starting with half the dose.
Supportive care continues at doses of 200 mg / day (for 2 doses), for 3 months-3 years. Elderly patients are recommended to start treatment with 50 mg / day. Renal failure does not require dose adjustment. In liver failure, it is advisable to prescribe other beta-blockers that are not metabolized in the liver.

Side effects:

From the side of the cardiovascular system: possible bradycardia, arterial hypotension, AV conduction disturbances, the appearance of symptoms of heart failure.
From the digestive system: at the beginning of therapy, dry mouth, nausea, vomiting, diarrhea, constipation are possible; in some cases - violations of the liver.
From the side of the central nervous system and peripheral nervous system: at the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, a feeling of cold and paresthesia in the extremities are possible; possible decrease in the secretion of lacrimal fluid, conjunctivitis, rhinitis, depression, sleep disturbances, nightmares.
From the hematopoietic system: in some cases - thrombocytopenia.
From the endocrine system: hypoglycemic conditions in patients with diabetes mellitus.
From the respiratory system: in predisposed patients, symptoms of bronchial obstruction may appear.
allergic reactions: skin rash, itching.

Contraindications:

Hypersensitivity;
- AV block II and III degree;
- sinoatrial blockade;
- acute or chronic (in the stage of decompensation) heart failure;
- sinus node weakness syndrome, severe sinus bradycardia (heart rate less than 60 bpm);
- cardiogenic shock;
- arterial hypotension (SBP less than 100 mm Hg);
- severe disorders of peripheral circulation;
- pregnancy, breastfeeding.

Carefully used in patients with chronic obstructive airways disease, diabetes mellitus (especially with a labile course), Raynaud's disease and obliterating diseases of peripheral arteries, pheochromocytoma (should be used in combination with alpha-blockers), severe renal and hepatic dysfunction.
Against the background of treatment with metoprolol, a decrease in the production of lacrimal fluid is possible, which is important for patients using contact lenses.
Completion of a long course of treatment with metoprolol should be carried out gradually (at least within 10 days) under the supervision of a physician.

The simultaneous use of metoprolol with MAO inhibitors is not recommended.
In combination therapy with clonidine, the latter should be discontinued a few days after the abolition of metoprolol, in order to avoid a hypertensive crisis. With simultaneous use with hypoglycemic agents, correction of their dosing regimen is required.
A few days before anesthesia, it is necessary to stop taking metoprolol or choose an anesthetic agent with a minimal negative inotropic effect.

Influence on the ability to drive vehicles and control mechanisms
In patients whose activities require increased attention, the question of the use of metoprolol on an outpatient basis should be decided only after an assessment of the individual patient's response.

Interaction
other medicinal
by other means:

When used simultaneously and:
- with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of developing severe arterial hypotension, bradycardia, AV blockade;
- with barbiturates, the metabolism of metoprolol is accelerated, which leads to a decrease in its effectiveness;
- with hypoglycemic agents, it is possible to increase the effect of hypoglycemic agents;
- with NSAIDs, it is possible to reduce the hypotensive effect of metoprolol;
- with opioid analgesics mutually increased cardiodepressive effect;
- with peripheral muscle relaxants, it is possible to increase the neuromuscular blockade;
- with means for inhalation anesthesia, the risk of inhibition of myocardial function and the development of arterial hypotension increases;
- with oral contraceptives, hydralazine, ranitidine, cimetidine, the concentration of metoprolol in the blood plasma increases;
- with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible;
- with verapamil, Cmax in blood plasma and AUC of metoprolol increase. The minute and stroke volume of the heart, pulse rate, and arterial hypotension decrease. Possible development of heart failure, dyspnea and blockade of the sinus node.
With intravenous administration of verapamil while taking metoprolol, there is a risk of cardiac arrest.
With simultaneous use, it is possible to increase bradycardia caused by digitalis glycosides.
- with dextropropoxyphene, the bioavailability of metoprolol increases;
- with diazepam, a decrease in clearance and an increase in the AUC of diazepam are possible, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions;
- with diltiazem, the concentration of metoprolol in the blood plasma increases due to the inhibition of its metabolism under the influence of diltiazem. The effect on the activity of the heart is additively suppressed due to the slowing down of the impulse through the AV node caused by diltiazem.
There is a risk of developing severe bradycardia, a significant decrease in stroke and minute volume;
- with lidocaine, a violation of the excretion of lidocaine is possible;
- with mibefradil in patients with low activity of the CYP2D6 isoenzyme, an increase in the concentration of metoprolol in the blood plasma and an increase in the risk of developing toxic effects are possible;
- with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form of eye drops or as part of antitussives), some increase in blood pressure is possible;
- with propafenone increases the concentration of metoprolol in the blood plasma and develops a toxic effect. It is believed that propafenone inhibits the metabolism of metoprolol in the liver, reducing its clearance and increasing serum concentrations;
- with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop;
- with rifampicin, the concentration of metoprolol in the blood plasma decreases.
Metoprolol may cause a slight decrease in the clearance of theophylline in smoking patients.
Fluoxetine inhibits the CYP2D6 isoenzyme, which leads to inhibition of the metabolism of metoprolol and its accumulation, which can enhance the cardiodepressive effect and cause bradycardia. A case of lethargy is described.
Fluoxetine and mainly its metabolites are characterized by a long T1 / 2, so the possibility of drug interaction remains even several days after fluoxetine is discontinued.
There are reports of a decrease in the clearance of metoprolol from the body when used simultaneously with ciprofloxacin;
- with ergotamine, it is possible to increase peripheral circulatory disorders;
- with estrogens, the antihypertensive effect of metoprolol decreases;
With simultaneous use, metoprolol increases the concentration of ethanol in the blood and prolongs its excretion.

Pregnancy:

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.
Metoprolol crosses the placental barrier.
Due to the possible development of bradycardia, arterial hypotension, hypoglycemia and respiratory arrest in a newborn, metoprolol must be canceled 48-72 hours before the planned delivery date.
After delivery, it is necessary to ensure strict control over the condition of the newborn for 48-72 hours.
Metoprolol is excreted in breast milk in small amounts.
Use during lactation is not recommended.

Overdose:

Symptoms: arterial hypotension, acute heart failure, bradycardia, cardiac arrest, AV blockade, cardiogenic shock, bronchospasm, impaired breathing and consciousness / coma, nausea, vomiting, generalized convulsions, cyanosis (manifested 20 minutes - 2 hours after ingestion).

Treatment: gastric lavage, symptomatic therapy: the introduction of atropine sulfate (in / in quickly 0.5-2 mg) - with bradycardia and impaired AV conduction; glucagon (1-10 mg IV, then IV drip 2-2.5 mg / h) and dobutamine - in case of a decrease in myocardial contractility; adrenomimetics (norepinephrine, adrenaline, etc.) - with arterial hypotension; diazepam (in / in slowly) - to eliminate seizures; inhalation of beta-adrenergic agonists or intravenous jet administration of aminophylline for the relief of bronchospastic reactions; pacing.

Release form:

Metoprolol tablets 50 mg and 100 mg in a package of 10 to 300 pieces.
Metoprolol-Acre tablets 50 mg per pack of 30 pieces.
Tablets Metoprolol-Ratiopharm 50 mg and 100 mg in a package of 30 to 100 pieces.
Metoprolol Organic tablets 25 mg and 50 mg in a package of 20 to 60 pieces.
Metoprolol-OBL tablets prolonged action of 25 mg, 50 mg, 100 mg in a package of 10 to 42 pieces.
1% Metoprolol solution in ampoules 5 ml in a pack of 10 pieces.

Storage conditions:

In a dry place, at a temperature not exceeding 30 °C. In closed packaging.
Keep out of the reach of children.
Shelf life - 5 years.

1 tablet Metoprolol 100 mg contains:
- active substance: metoprolol - 100 mg;
- Excipients: lactose monohydrate 180 mg, microcrystalline cellulose 72 mg, potato starch 12 mg, sodium carboxymethyl starch 16 mg, povidone 16 mg, magnesium stearate 4 mg.

Indications for use:
Arterial hypertension of moderate and moderate severity (monotherapy or in combination with other antihypertensive drugs), ischemic heart disease, hyperkinetic cardiac syndrome, cardiac arrhythmias (sinus tachycardia, ventricular and supraventricular arrhythmia, including paroxysmal tachycardia, supraventricular tachycardia, extrasystole, atrial flutter and fibrillation, atrial tachycardia), hypertrophic cardiomyopathy, mitral valve prolapse, myocardial infarction (prevention and treatment), migraine (prevention), thyrotoxicosis (complex therapy); treatment of akathisia caused by antipsychotics.

Pharmachologic effect:
Metoprolol acts predominantly on the beta1-adrenergic receptors of the heart. It has antianginal, antihypertensive and antiarrhythmic action. Reduces the automatism of the sinus node, slows down the heart rate, slows down atrioventricular conduction, reduces myocardial contractility and excitability, cardiac output, myocardial oxygen demand. Suppresses the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress.

The antihypertensive effect develops gradually and stabilizes by the end of the 2nd week of the course administration of the product. With exertional angina, metoprolol reduces the frequency and severity of attacks. Normalizes the heart rhythm with supraventricular tachycardia and atrial fibrillation. Against the background of taking Metoprolol in patients with myocardial infarction, due to the limitation of the infarction zone and the reduction in the risk of developing fatal arrhythmias, mortality and the possibility of recurrence of myocardial infarction are reduced. When used in medium therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective beta-blockers.

Metoprolol route of administration and dosage:
Inside, with food or immediately after eating, the tablets can be divided in half, but not chewed and washed down with liquid, for prolonged-release dosage forms - swallow whole, do not crush, do not break (except for metoprolol succinate and tartrate), do not chew. With arterial hypertension, the average dose is 100-150 mg / day in 1-2 doses, if necessary - 200 mg / day. With angina - 50 mg 2-3 times a day. With hyperkinetic cardiac syndrome (including thyrotoxicosis) - 50 mg 1-2 times a day. With tachyarrhythmia - 50 mg 2-3 times a day, if necessary - 200-300 mg / day. Secondary prevention of myocardial infarction - 200 mg / day. Prevention of migraine - 100-200 mg / day in 2-4 doses. For the relief of paroxysmal supraventricular tachycardia, it is administered parenterally, in a hospital setting. Enter slowly, a dose of 2-5 mg (1-2 mg / min). If there is no effect, the administration can be repeated after 5 minutes. Increasing the dose above 15 mg usually does not lead to a greater severity of action. After stopping the attack of arrhythmia, the patients are transferred to oral administration at a dose of 50 mg 4 times a day, with the first dose being taken 15 minutes after the cessation of intravenous administration. In the acute stage of myocardial infarction, immediately after the patient's hospitalization (with constant monitoring of hemodynamics: ECG, heart rate, AV conduction, blood pressure), a 5 mg intravenous bolus should be administered, repeat the administration after 2 minutes until a total dose of 15 mg is reached. With good tolerance after 15 minutes - inside, 25-50 mg after 6 hours, for 2 days. Patients who have not tolerated the full intravenous dose should begin oral administration starting with half the dose. Maintenance therapy continues at doses of 200 mg / day (for 2 doses), for 3 months-3 years. Elderly patients are recommended to start treatment with 50 mg / day. Renal failure does not require dose adjustment. In liver failure, it is advisable to prescribe other beta-blockers that are not metabolized in the liver.

Metoprolol contraindications:
Hypersensitivity, AV blockade II and III degree, sinoatrial blockade, acute or chronic (in the stage of decompensation) heart failure, sick sinus syndrome, severe sinus bradycardia (heart rate less than 60 bpm), cardiogenic shock, arterial hypotension (systolic blood pressure less than 100 mm Hg), severe peripheral circulatory disorders, pregnancy, breastfeeding.

Metoprolol side effects:
At the beginning of therapy, weakness, fatigue, dizziness, headache, muscle cramps, a feeling of cold and paresthesia in the extremities are possible. Bradycardia, arterial hypotension, impaired atrioventricular conduction, the appearance of symptoms of heart failure with peripheral edema, a decrease in the secretion of lacrimal fluid, conjunctivitis, rhinitis, depression, sleep disturbance, nightmares, dry mouth, hypoglycemic conditions in patients with diabetes mellitus, vomiting, diarrhea are also possible. , constipation. Predisposed patients may develop symptoms of bronchial obstruction. There have been isolated cases of liver dysfunction, thrombocytopenia, allergic reactions - skin rash, itching.

Use with other medicinal products:
Hypotension is potentiated by sympatholytics, nifedipine, nitroglycerin, diuretics, hydralazine and other antihypertensive products. Antiarrhythmic and anesthetic drugs increase the risk of developing bradycardia, arrhythmias, and hypotension. Digitalis preparations potentiate the slowing of AV conduction. Simultaneous intravenous administration of verapamil and diltiazem may cause cardiac arrest. Beta-agonists, aminophylline, cocaine, estrogens, indomethacin and other NSAIDs weaken the antihypertensive effect. Enhances and prolongs the action of antidepolarizing muscle relaxants. The combination with alcohol leads to a mutual strengthening of the inhibitory effect on the central nervous system. Allergens increase the risk of severe systemic allergic reactions or anaphylaxis. Changes the effectiveness of insulin and oral antidiabetic agents and increases the risk of hypoglycemia. Antacids, oral contraceptives, cimetidine, ranitidine, phenothiazines - increase the level of metoprolol in the blood, rifampicin - reduces. Reduces the clearance of lidocaine, the effectiveness of beta2-adrenergic agonists (it is necessary to increase the dose later). Incompatible with MAO inhibitors type A.

Release form:
Tablets of 50 and 100 mg in a pack of 30; 100 and 200 pieces; retard tablets 200 mg in a pack of 14; 1% solution in 5 ml ampoules in a pack of 10 pcs.

Overdose:
Symptoms: arterial hypotension, acute heart failure, bradycardia, cardiac arrest, AV blockade, cardiogenic shock, bronchospasm, impaired breathing and consciousness / coma, nausea, vomiting, generalized convulsions, cyanosis (appear after 20 minutes - 2 hours after administration).
Treatment: gastric lavage, symptomatic therapy: the introduction of atropine sulfate (in / in quickly 0.5-2 mg) - with bradycardia and impaired AV conduction; glucagon (1-10 mg IV, then IV drip 2-2.5 mg / h) and dobutamine - in case of a decrease in myocardial contractility; adrenomimetics (norepinephrine, adrenaline, etc.) - with arterial hypotension; diazepam (in / in slowly) - to eliminate seizures; inhalation of beta-adrenergic agonists or intravenous jet administration of aminophylline for the relief of bronchospastic reactions; pacing.

Storage conditions:
List B. At a temperature not higher than +25°C.

Synonyms:
Betaloc (Betaloc), Bloxan (Blocksan), Specicor (Specikor), Protein (Veloc), Lopresor (Lopressor), Neoblock, Opresol (Orresol), Selopral (Selopral), Vasocardin, Corvitol, Methohexal, Metolol

Metoprolol composition:
(±)-1--3-[(1-methylethyl)amino]-2-propanol (as tartrate or succinate).
Metoprolol tartrate: white, practically odorless crystalline powder, highly soluble in water, methylene chloride, chloroform and alcohol, slightly soluble in acetone, insoluble in ether. Metoprolol succinate: white crystalline powder, freely soluble in water, soluble in methanol, sparingly soluble in ethanol, slightly soluble in dichloromethane and 2-propanol, practically insoluble in ethyl acetate, acetone, diethyl ether and heptane.

Additionally:
It is prescribed with caution in diabetes mellitus (especially with a labile course), Raynaud's disease and patients with impaired peripheral circulation, pheochromocetoma, severe impairment of kidney and liver function (when prescribing Metoprolol-Acre in this category of patients, constant monitoring of the dynamics of the functional state of the liver and / or kidneys). Patients using contact lenses should take into account that during treatment with Metoprolol-Acre, a decrease in the production of lacrimal fluid is possible. The termination of the duration of the course should occur gradually (at least 10 days) under the supervision of a physician. A few days before anesthesia with chloroform or ether, it is necessary to stop taking the product. In the case of taking the drug before surgery, the patient should choose a narcotic drug with a minimal negative inotropic effect.

Attention!
Before using the medication "Metoprolol" you need to consult a doctor.
The instructions are provided solely for familiarization with " metoprolol».

Tablets

- Concentrate for solution for infusion 250 mg/ml

- Solution for infusion

- Solution for intravenous administration 10 mg/ml

- Tablets 5 mg, 10 mg

- Tablets 50 mg

- Tablets 5 mg, 10 mg

- Tablets 20 mg

- Tablets 5 mg

- Tablets

- Tablets 5 mg

- Tablets 5 mg, 10 mg

- Tablets 12.5 mg, 25 mg, 50 mg

Indications for the use of the drug Metoprolol

Arterial hypertension of moderate and moderate severity (monotherapy or in combination with other antihypertensive drugs), ischemic heart disease, hyperkinetic cardiac syndrome, cardiac arrhythmia (sinus tachycardia, ventricular and supraventricular arrhythmia, including paroxysmal tachycardia, supraventricular tachycardia, extrasystole, atrial flutter and fibrillation, atrial tachycardia), hypertrophic cardiomyopathy, mitral valve prolapse, myocardial infarction (prevention and treatment), migraine (prevention), thyrotoxicosis (complex therapy); treatment of akathisia caused by antipsychotics.

Metoprolol release form

Film-coated tablets 1 tab.
metoprolol tartrate 50 mg
100 mg
excipients: silicon dioxide colloidal anhydrous; MCC; sodium carboxymethyl starch (type A); magnesium stearate
shell: : hypromellose; polysorbate 80; talc; titanium dioxide E 171
in table. 50 mg each (optional): crimson dye (Ponceau 4R)

There are 14 pieces in a blister; in a cardboard pack 2 or 4 blisters (tablet 50 mg) or in a blister 10 pcs.; in a cardboard pack 3 blisters (Table 100 mg).

Pharmacodynamics of the drug Metoprolol

Blocks predominantly beta1-adrenergic receptors of the heart, does not have internal sympathomimetic and membrane stabilizing activity. It reduces cardiac output and SAD, slows down the heart rate, weakens the stimulating effect of catecholamines on the myocardium during physical exertion and mental stress, and prevents reflex orthostatic tachycardia. The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin system and the central nervous system, restoration of baroreceptor sensitivity and, as a result, a decrease in peripheral sympathetic influences. The hypotensive effect develops rapidly (SBP decreases after 15 minutes, maximum - after 2 hours) and lasts for 6 hours; when taking metoprolol succinate, the clinical effect of blockade of beta1-adrenergic receptors persists for 24 hours. DBP changes more slowly: a stable decrease is observed after several weeks of regular use. The antianginal effect is a consequence of a decrease in the frequency and strength of heart contractions, energy costs and myocardial oxygen demand. It reduces the frequency and severity of IHD attacks, the mortality rate in patients with diagnosed myocardial infarction, and increases exercise tolerance. Metoprolol succinate reduces the risk of death (including sudden death), re-infarction (including in patients with diabetes mellitus) and improves the quality of life of patients with acute myocardial infarction and idiopathic dilated cardiomyopathy. The antiarrhythmic effect is manifested in the elimination of arrhythmogenic sympathetic influences on the conduction system of the heart, slowing down the sinus rhythm and the rate of propagation of excitation through the AV node, inhibition of automatism and lengthening the refractory period. It has a moderate negative inotropic effect. Cardioselectivity is maintained when using daily doses not exceeding 200 mg. Due to the selective action on beta1-adrenergic receptors, the risk of bronchospasm is theoretically reduced (in patients with bronchial asthma, the vital function of the lungs decreases less), hypoglycemia and peripheral vasoconstriction.

Pharmacokinetics of Metoprolol

Metoprolol tartrate is rapidly and almost completely (95%) absorbed when taken orally and undergoes intensive first pass metabolism. Bioavailability is about 50% at the first dose and increases to 70% with repeated use. About 12% binds to plasma albumin. It is rapidly distributed in tissues, penetrates the BBB (the level in the central nervous system is 78% of plasma concentration), the placental barrier, breast milk (concentrations exceed plasma concentrations). The volume of distribution is 5.5 l/kg. Cmax is achieved within 1-2 hours after administration, the level in the blood varies significantly. T1 / 2 - from 3 to 7 hours. Biotransformed in the liver, with the formation of two active metabolites. It is excreted mainly by the kidneys in the form of metabolites, Cl - 1 l / min. When ingested, less than 5% is excreted in the urine unchanged, with intravenous infusion - about 10%. In case of impaired renal function, bioavailability does not change, but the rate of excretion of metabolites may decrease. In patients with cirrhosis of the liver, metabolism and total clearance slow down (no dosage adjustment is required). Not removed by hemodialysis. With intravenous infusion of metoprolol tartrate for 10 minutes or more, the maximum effect develops after 20 minutes, the decrease in heart rate at doses of 5 and 10 mg is 10 and 15%, respectively. After oral administration in equal doses, Cmax of metoprolol succinate is 1/4–1/2 Cmax of metoprolol tartrate, but it persists for a longer time. Bioavailability at doses of 50-400 mg (1 time per day) is 23% less than that after taking a similar dose of tartrate. Pharmacokinetic parameters do not depend on the age of patients.

Use of Metoprolol during pregnancy

Perhaps if the expected effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications to the use of the drug Metoprolol

Hypersensitivity, AV blockade II and III degree, sinoatrial blockade, acute or chronic (in the stage of decompensation) heart failure, sick sinus syndrome, severe sinus bradycardia (heart rate less than 60 bpm), cardiogenic shock, arterial hypotension (systolic blood pressure less than 100 mm Hg), severe peripheral circulatory disorders, pregnancy, breastfeeding.

Side effects of the drug Metoprolol

From the nervous system and sensory organs: at least 10% - weakness; 1–9.9% - dizziness and headache; 0.1-0.9% - decreased concentration, drowsiness / insomnia, nightmares, depression, muscle cramps, paresthesia; 0.01–0.09% - nervousness, anxiety, weakening of libido, visual impairment, xerophthalmia, conjunctivitis; less than 0.01% - lethargy, fatigue, anxiety, confusion, amnesia / short-term memory loss, hallucinations, tinnitus, taste disturbance.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): 1–9.9% - bradycardia, palpitations, hypotension, cold extremities; in 0.1-0.9% - heart failure, AV blockade, edematous syndrome, chest pain; in 0.01–0.09% - a decrease in myocardial contractility, arrhythmias, less than 0.01% - gangrene (in patients with severe impairment of peripheral circulation); violation of myocardial conduction, syncope, thrombocytopenia, leukopenia, agranulocytosis.

From the digestive tract: 1-9.9% - nausea, abdominal pain, diarrhea or constipation; 0.1–0.9% - vomiting; 0.01-0.09% - dryness in the mouth, abnormal liver function; flatulence, dyspepsia, heartburn, hepatitis.

From the respiratory system: shortness of breath (1–9.9%), bronchospasm (0.1–0.9%), vasomotor rhinitis (0.01–0.09%), dyspnea.

From the side of the skin: 0.1–0.9% - rash, degenerative skin changes; 0.01–0.09% - reversible alopecia; less than 0.01% - photosensitivity, exacerbation of psoriasis; itching, erythema, urticaria, hyperhidrosis.

Others: weight loss (0.1-0.9%), arthralgia, arthritis, myalgia, muscle weakness, Peyronie's disease.

Dosing and Administration of Metoprolol

As an antianginal, antihypertensive and antiarrhythmic agent, with hyperkinetic syndrome, metoprolol tartrate is administered orally at a dose of 100-200 mg in 2-3 doses, if necessary, the dose is increased at weekly intervals up to 450 mg / day. In the acute period of myocardial infarction, under the monitoring of blood pressure, heart rate and ECG, 3 bolus intravenous injections of 5 mg are performed with two-minute breaks (total dose of 15 mg), with good tolerance, 15 minutes after the last injection, 25–50 mg are administered orally every 6 hours for 48 hours, and then - 50-100 mg 2 times a day (morning and evening) for 3 months - 3 years. When switching to the use of metoprolol succinate, the dose remains the same. For the prevention of migraine attacks - inside 50-100 mg 2-4 times a day.

Overdose of metoprolol

Symptoms: arterial hypotension, acute heart failure, bradycardia, cardiac arrest, AV blockade, cardiogenic shock, bronchospasm, impaired breathing and consciousness / coma, nausea, vomiting, generalized convulsions, cyanosis (manifested 20 minutes - 2 hours after ingestion).

Treatment: gastric lavage, symptomatic therapy: the introduction of atropine sulfate (in / in quickly 0.5-2 mg) - with bradycardia and impaired AV conduction; glucagon (1-10 mg IV, then IV drip 2-2.5 mg / h) and dobutamine - in case of a decrease in myocardial contractility; adrenomimetics (norepinephrine, adrenaline, etc.) - with arterial hypotension; diazepam (in / in slowly) - to eliminate seizures; inhalation of beta-adrenergic agonists or intravenous jet administration of aminophylline for the relief of bronchospastic reactions; pacing.

Interactions of the drug Metoprolol with other drugs

Hypotension is potentiated by sympatholytics, nifedipine, nitroglycerin, diuretics, hydralazine and other antihypertensive drugs. Antiarrhythmic and anesthetic drugs increase the risk of developing bradycardia, arrhythmias, and hypotension. Digitalis preparations potentiate the slowing of AV conduction. Simultaneous intravenous administration of verapamil and diltiazem may cause cardiac arrest. Beta-agonists, aminophylline, cocaine, estrogens, indomethacin and other NSAIDs weaken the antihypertensive effect. Enhances and prolongs the action of antidepolarizing muscle relaxants. The combination with alcohol leads to a mutual strengthening of the inhibitory effect on the central nervous system. Allergens increase the risk of severe systemic allergic reactions or anaphylaxis. Changes the effectiveness of insulin and oral antidiabetic agents and increases the risk of hypoglycemia. Oral contraceptives, cimetidine, ranitidine, phenothiazines - increase the level of metoprolol in the blood, rifampicin - reduces. Reduces the clearance of lidocaine, the effectiveness of beta2-agonists (it is necessary to increase the dose of the latter). Incompatible with MAO inhibitors type A.

Precautions while using metoprolol

In patients with chronic heart failure, myocardial contractility may deteriorate, necessitating the use of cardiac glycosides and / or diuretics with careful monitoring of the hemodynamic status. In case of increasing bradycardia or AV blockade, it is necessary to reduce the dose or inject atropine intravenously. Against the background of diabetes mellitus and hyperthyroidism, metoprolol can mask tachycardia caused by hypoglycemia or thyrotoxicosis. In patients with diabetes, dose adjustment of antidiabetic drugs and careful monitoring of glycemic levels are necessary. When performing surgery against the background of treatment, the anesthetic with the least negative inotropic effect should become the means of choice. Perhaps a more pronounced development of a hypersensitivity reaction and the absence of a therapeutic effect of conventional doses of adrenaline against the background of an aggravated allergic history. When concomitant treatment with clonidine is stopped, metoprolol is discontinued gradually, a few days before clonidine is discontinued, due to the risk of developing a severe hypertensive crisis. In patients with pheochromocytoma, the use is possible only in conjunction with alpha-adrenolytics. Reception of metoprolol is stopped 2-3 days before delivery (the risk of developing bradycardia, hypotension and hypoglycemia in the newborn), in exceptional cases, newborns after childbirth should be under medical supervision for 48-72 hours. Pediatric use should be avoided as the safety and efficacy of its use in children have not been determined. When canceling treatment, the dose should be reduced gradually over 10-14 days. Patients with coronary artery disease should be under close medical supervision during this period. Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention.