Possible harm and precautions. Belonging to the ATX classification

Among the cardiac drugs that actively affect the functioning of the heart muscle, Metoprolol should be highlighted - a popular drug with high efficiency and an affordable price. The drug allows not only to prevent exacerbation of heart diseases associated with rhythm disturbances and ischemic lesions, but also to completely normalize the functioning of the heart and the whole body.

Metoprolol is not only the name of the drug - it is a substance with a selective effect, which is part of many effective cardiac drugs. Products based on it require caution in use - they not only support the functioning of the heart, but can also cause harm if taken uncontrolled, so before the first use, you need to find out how to take them correctly and what precautions to take.

Drug group

Metoprolol is a selective adrenergic blocker that acts on beta 1 receptors and does not have a membrane stabilizing or internal sympathomimetic effect. The main properties of the drug are antiarrhythmic, antianginal and hypotonic.

Since the name Metoprolol is similar to the active substance, the International generic name, under which the drug is known throughout the world - Metoprolol.

The drug is intended for the treatment of heart diseases of various nature: rhythm disturbances, angina pectoris, ischemia, prolapse mitral valve and others. It is also prescribed in neurology - to patients with migraines to prevent an attack, and by endocrinologists - as part of complex treatment thyrotoxicosis.

Release forms

The drug is available in three forms - tablets, extended-release tablets and solution for injection. On pharmacy shelves you can see various trade names: Metoprolol Teva, Metoprolol Organica, Metoprolol Acri and others. Patients have a question about how they differ from each other (Table 1).

The tablets contain excipients; they may differ slightly depending on the different manufacturers, but this does not affect pharmachologic effect drug. Injection solutions with metoprolol are rarely used and mainly in conditions inpatient treatment until the patient can take pills. In pharmacies you can buy a similar solution called Betalok.

Table 1 – Forms of release

Ingredients: tartrate or succinate?

The drug may be based on different active ingredients: metoprolol tartrate and metoprolol succinate, which have some differences, make it possible to create drugs with rapid and delayed action. Tartrate is intended to produce faster therapeutic effect, but its effect is short-term. Therefore, drugs based on it should be taken at least 2 times a day 4.

Succinate is used to create tablets with a delayed action, which allows you to maintain the therapeutic dose at the required concentration for 24 hours. In addition, succinate, compared to tartrate, is more effective in heart failure, improves the effect of statins and rarely causes adverse reactions.

Cost in pharmacies

The price of Metoprolol depends on the content of the active substance, the number of tablets in the package and the form of the active substance. On average, the price in pharmacies varies from 16 to 420 rubles. (Table 2).

Table 2 - Prices of Metoprolol from some manufacturers

As can be seen from the table, prolonged-release tablets have the highest price. But, taking into account the fact that they need to be taken only once a day, they are no more expensive than regular tablets.

Pharmacological properties

Metoprolol has a pronounced antiarrhythmic effect and is able to act on the sinus node, reducing its impulse conduction. This allows you to normalize its automaticity and eliminate sinus tachycardia and arrhythmia. Reducing the frequency of impulse transmission helps to slow down AV conduction.

The drug reduces the contractile activity of the myocardium and stabilizes the rhythm, which leads to less myocardial oxygen demand and prevents the development of hypoxia in conditions of ischemic damage.

In patients with ischemia and exertional angina, the drug has a pronounced anti-ischemic and antianginal effect. Metoprolol reduces the frequency and severity of angina attacks, and when regular use eliminates them completely. As a result of taking the drug, patients become more resistant to physical activity and may not be afraid of discomfort in the chest area.

Taking Metoprolol for myocardial infarction allows you to limit the necrotic zone and prevent it from becoming larger. The drug helps avoid relapses and prevent fatal arrhythmias and other complications after a heart attack.

On the first day after taking the drug, general vascular resistance increases, but after 24-72 hours it returns to its original state and when further treatment starts to decline.

Metoprolol can have a hypotonic effect by reducing renin synthesis, reducing cardiac output and central nervous system depression. The hypotonic effect is best achieved in stress- and exercise-induced hypertension, but does not last long.

Achieve pronounced effect possible only after 10-15 days of regular use.

Metropolol tartrate is very quickly absorbed into the bloodstream and the highest concentration in plasma is observed no later than after 120 minutes. When passing through the liver, it forms inactive metabolites, which are excreted in the urine.

Metropolol succinate has a more pronounced and long-lasting effect, together with statins it fights atherosclerosis and has positive influence on the muscles of the bronchi. Succinate provides therapeutic effect throughout the day. The rate of absorption depends on the acidity in the gastrointestinal tract.

Indications and contraindications

Metoprolol is most often prescribed as part of complex therapy for functional disorders of the heart, accompanied by increased load on the heart and hypertension.

Indications for use:

In neurology, the drug is used to treat akathisia caused by taking antipsychotics, neurocirculatory dystonia, hyperkinetic syndrome and neurocirculatory dystonia, together with other medicines.

Due to the pharmaceutical properties of the drug, it should not be taken by patients with low blood pressure, sinus node dysfunction, or those taking MAO inhibitors.

Other contraindications:

If the use is necessary for a woman who is breastfeeding, then it must be stopped for the duration of treatment. natural feeding child. During pregnancy, the drug is prescribed only when absolutely necessary. Treatment of pregnant women should take place in a hospital, where fetal development is regularly monitored.

Particular care should be taken in patients with diabetes mellitus and impaired carbohydrate metabolism, in this case, a reduced dosage may be prescribed.

It is not advisable to take Metoprolol if diseases associated with obstruction of the lungs and bronchi are diagnosed, including bronchial asthma.

Observation and regular examination is required if the patient has diseases peripheral vessels(including autoimmune nature), chronic diseases liver and kidneys, damage to nerves and muscle fibers, adrenal tumor, psoriasis and depressive conditions.

Instructions for use

You should consider how to properly take Metoprolol from different manufacturers and dosages.

Akrikhin

Akrikhin produces regular and extended-release tablets. Regular Metoprolol should be taken at full stomach without compromising the integrity of the tablet.

The dosage is selected taking into account the disease:

Long-acting tablets are taken only once a day, at the same hours after meals. How to use:

The duration of therapy is selected individually for each patient. Who is regularly examined by the attending physician and assesses his condition.

Ratiopharm

Metoprolol Ratiopharm has less detailed instructions. The manufacturer indicates that the recommended daily dose is 100 mg per day, divided into two doses. If there is no expected therapeutic effect, then the dose is increased to 200 mg per day.

In some cases, specialists prescribe up to 400 mg per day - this is the maximum dosage that can be taken in 24 hours.

Teva

Metoprolol Teva has similar instructions according to application, as tablets from the manufacturer Akrikhin. The only thing that differs is that the instructions indicate dosages for hyperthyroidism - 150-200 mg per day, divided into 3 or 4 doses. In any case, any dosage can be changed based on the individual health characteristics of the patient, so before using the drug, you must see your doctor.

Organic

Metoprolol Organic does not have any special features for use, and therefore the dosage of the drug does not differ from other manufacturers of tablets with normal action. Like other manufacturers, the instructions indicate that the dosage of the drug is reduced if the patient is diagnosed with severe liver dysfunction. Elderly people and those with mild liver problems do not change the dosage, but these patients need to undergo examinations more often.

Tartrate

Metoprolol Tartrate - tablets from the Ukrainian manufacturer Farmak are known by this name. As already mentioned, the effect of the drug is more active, but shorter lasting.

The instructions indicate the following dosages:

Akri

Instructions for use of Metoprolol Acri indicate the following dosages, which are practically no different from treatment regimens from other manufacturers:

1. Hypertension: 100-150 mg per day, if the effect is insufficient, increase the daily dose to 200 mg.
2. Tachyarrhythmia - 50 mg 2-3 times a day, in severe cases increase the daily dose to 300 mg.
3. Angina pectoris: 2-3 times a day, 50 mg.
4. Cardiac hyperkinetic syndrome, hyperthyroidism - 1-2 times a day, 50 mg.
5. Migraines – 100-200 mg per day.

The abstract states that in case of paroxysmal supraventricular tachycardia and acute myocardial infarction, intravenous administration of solutions with metoprolol is necessary until the condition stabilizes, after which the tablet form of the drug is prescribed. This method of treatment also applies to other types of Metoprolol.

The course of therapy can be continued long term– up to 3 years, provided that the drug is well tolerated. You must also comply minimum term treatment – ​​3 months to achieve a pronounced therapeutic effect.

At what pressure should I take it?

Pharmacological properties Metoprolol allows its use in the treatment of hypertension, both as monotherapy and in combination with other hypotonic drugs, except diuretics.

The drug is able to reduce blood pressure after the first dose, but to achieve lasting results, Metoprolol must be taken for at least 10-14 days. Regular taking of pills protects against increased blood pressure and development associated violations from the side of the heart.

Patients with severe arterial hypertension are recommended to take a long-acting drug. Metropolol succinate provides a more pronounced and prolonged hypotonic effect and reduces the load on the heart, without the development of adverse reactions.

Since Metoprolol is often used to quickly lower blood pressure, but does not have a long-term effect, many patients start taking one tablet after another. This is strictly unacceptable, as symptoms of overdose and a sharp deterioration in general health may occur.

When you first take the pills, you need to take the minimum dose to check the body’s reaction and prevent a sharp decline pressure, which can lead to hypotonic shock. The dosage can be gradually increased, but not more than 200 mg.

If Metoprolol needs to be taken by patients with low blood pressure or those who are prone to hypotension, they should regularly monitor blood pressure and heart rate. It is recommended to check the pulse rate and their severity daily - a sharp decrease in the number of beats per minute indicates that it is necessary to gradually reduce the dosage, and then completely abandon Metoprolol.

Abruptly stopping taking the pills is undesirable, as chest pain and other signs of angina may appear. Therefore, discontinuation of the drug is agreed in advance with the attending physician, who will tell you how to properly reduce the dosage.

Features of application

The treatment regimen does not always correspond to the instructions for use, since in some cases individual selection of the dosage and duration of treatment is necessary.

In pregnant women

The effect of Metoprolol on pregnant women has been little studied, so the drug is prescribed to them only for vital indications. Treatment should be coordinated not only with a cardiologist, but also with a gynecologist who has complete information about the condition of the mother and child, and knows how pregnancy proceeds from the earliest stages.

Usually the drug is prescribed for arterial hypertension, angina pectoris and pathological rhythm disturbances, which become more pronounced during pregnancy and not only interfere with the woman’s ability to normal image life, but can also cause death.

The use of Metoprolol is recommended in a hospital setting, since constant monitoring of the condition of the fetus is necessary due to the risk of developing disorders. of cardio-vascular system, for example, bradycardia, as well as pathological abnormalities.

If a woman took the drug during pregnancy, then her child should be under the constant supervision of specialists for the first 72 hours to make sure that there are no complications.

In bodybuilding

Metoprolol is popular among athletes due to its ability to increase myocardial resistance to physical stress and prevent the development of hypoxia. I take it especially often during intensive training before competitions, when not only physical fatigue, but also nervous overstrain leads to disruption of cardiac function.

Bodybuilders who use steroids and fat burners note that taking them simultaneously with Metoprolol helps normalize heart rate and reduce blood pressure, which leads to increased resistance to heavy physical activity.

But this drug is prohibited for professional athletes, so they can only be used during training, so that the active substance has time to be eliminated from the body before competitions. The dosage is selected individually after examining the athlete and diagnosing the functional activity of the heart.

Possible harm and precautions

Side effects from tartrate-based Metoprolol occur more often than from succinate, so most doctors recommend taking slow-release tablets.

Negative reactions from the body

The most common adverse reactions are observed in the central nervous system and cardiovascular system:

The following violations are less common:

1. Hypoglycemia or hyperglycemia.
2. Hypothyroidism.
3. Thrombocytopenia, agranulocytosis, increased bilirubin in the blood.
4. Allergic reactions.
5. Skin diseases: psoriasis, photodermatosis, rash, alopecia.
6. Increased sweating.
7. Bronchospasm, shortness of breath, nasal congestion.
8. Visual disturbances, pain in the eyes.
9. Taste disturbances.

It is extremely rare, but still Metoprolol can negatively affect libido, cause joint pain and lead to weight gain.

If the drug is abruptly discontinued, a “withdrawal syndrome” develops, especially after long-term treatment.

Overdose symptoms

Symptoms of overdose occur if you take the drug in a dosage that exceeds the maximum permissible limit. Most often, symptoms are expressed in the form of adverse reactions, accompanied by nausea and vomiting.

But sometimes more dangerous conditions are observed:

To eliminate the dangerous condition, it is necessary to rinse the stomach, drink enterosorbent and call ambulance. Emergency help in case of a sharp drop in pressure, it is carried out using drugs based on dopamine and glucagon.

Alcohol compatibility

Since the drug is metabolized in the liver, drinking alcohol simultaneously with Metoprolol leads to increased load to this organ. In addition, taking pills and alcoholic beverages increases the negative impact of the medication and leads to treatment failure.

The interaction of beta blockers and alcohol can lead to a critical decrease in blood pressure that will be difficult to raise by medicinal method. Therefore, doctors are against drinking alcohol at the same time as taking heart medications.

In addition, when combining Metoprolol and ethanol, the following may develop:

• delusional states;
• dyspeptic symptoms;
• allergic reactions.

Analogs

Metoprolol cannot always be taken, so it is often replaced with drugs based on another substance with similar action. There are also structural analogues that can replace the drug if it is not available in pharmacies.

Structural

Metoprolol is not the cheapest, but also not the most expensive drug among other drugs based on active ingredient metoprolol. Should be compared average cost other medicines (may vary depending on the dosage and number of units in one package):

Replace Metoprolol structural analogue should be used with caution, as the content of the active ingredient may vary significantly. It is best to consult a doctor so that he can describe in detail new scheme treatment.

Drugs based on other groups

If you are intolerant to Metoprolol or between its courses, medications with other active substances in the composition, but having a similar effect, are prescribed:

These drugs are inexpensive, so they can replace Metoprolol without much expense if the patient is allergic to the active substance or the time has come to change treatment tactics.

JSC "Farmak", Kyiv, Ukraine

Active ingredient: Metoprolol tartrate

1 tablet contains metoprolol tartrate 0.05 g or 0.1 g

Release form of Metoprolol tartrate

Tablets 0.05 g No. 10x2, No. 10x5
Tablets 0.1 g No. 10x2, No. 10x5

Who is Metoprolol tartrate indicated for?

Arterial hypertension, angina pectoris (including post-infarction), hyperkinetic syndrome, arrhythmias (supraventricular tachycardia), treatment acute heart attack myocardium and secondary prevention after a heart attack (as part of complex therapy). Prevention of migraine attacks.

How to use Metoprolol tartrate

The dose of Metoprolol tartrate is determined individually. For arterial hypertension, the initial dose is 50-100 mg per day in two doses (morning and evening). The dose is gradually increased at weekly intervals until a therapeutic effect is achieved. The maximum daily dose is 400 mg. The tablets are taken orally with a small amount of liquid, without chewing, after meals.

With angina pectoris, functional cardialgia Prescribe 1-2 tablets (50-100 mg) of Metoprolol tartrate 1-2 times a day. For maintenance therapy, 1-2 tablets (50-100 mg of metoprolol tartrate) are prescribed 2 times a day.

For tachyarrhythmias, for preventive treatment for migraines, take 100-200 mg of Metoprolol tartrate per day, in the form of 1-2 single doses (1/2 tablet 2 times a day). If it is necessary to discontinue treatment, the dose is reduced gradually (over 10 days or more), under the supervision of a physician. The duration of treatment is determined individually.

Features of application

Particularly careful medical supervision is necessary when treating patients with diabetes mellitus, with unstable blood sugar levels, while following a strict diet with fasting; patients with pheochromocytoma require preliminary therapy with α-adrenergic receptor blockers; patients undergoing desensitization treatment (risk of developing an anaphylactic reaction) patients with impaired liver function.

Occasionally, manifestation of latent diabetes or deterioration of the condition of patients with diabetes is possible. Anaphylactic shock in patients taking β-adrenergic blockers has severe course. Treatment of high blood pressure with Metoprolol tartrate requires regular medical supervision. During treatment, you should refrain from driving or working with other potentially dangerous technical means. This is even more true when starting a course of treatment and changing the drug, as well as its use in combination with alcohol. In patients with severe liver dysfunction, the dose of the drug is reduced. IN in some cases Metoprolol tartrate can provoke the onset or exacerbation of psoriasis or lead to psoriasiform exanthema, therefore, it is recommended to prescribe Metoprolol tartrate to patients with a personal or family history of psoriasis (squamosus) only after a careful assessment of the expected benefits and possible risks.

Children. Sufficient clinical experience Metoprolol tartrate is not used for children, so it is not recommended for this age category.

Use during pregnancy and lactation. During pregnancy (especially in the first trimester), Metoprolol tartrate should be used only when the expected therapeutic effect exceeds the potential risk to the fetus. Due to the possible development of bradycardia in the newborn, arterial hypotension, hypoglycemia and respiratory depression, the course of treatment must be interrupted 48-72 hours before delivery. In cases where this is not possible, close monitoring of newborns is necessary for 48-72 hours after birth. Metoprolol tartrate passes into breast milk, so it is contraindicated during lactation.

Side effects of Metoprolol tartrate

From the nervous system: fatigue, dizziness, depression, confusion, headache, sweating, sleep disturbance (nightmarish dreams), as well as changes in mood, short-term memory loss, a feeling of numbness of the skin and “crawling goosebumps”, a feeling of coldness in the extremities, rarely - muscle weakness, in some cases - sexual disorders. All these phenomena disappear on their own when doses are reduced and gradually increased.

From the outside gastrointestinal tract: dyspepsia, abdominal pain, stool disturbances, changes in liver function tests, hepatitis.

From the respiratory system: some patients may experience shortness of breath during exercise, bronchospasm, attacks of bronchial asthma (in patients with bronchial asthma).

From the cardiovascular system: orthostatic hypotension, sometimes accompanied by loss of consciousness, slowing of the pulse, functional disorders of the heart (atrioventricular conduction disorders), an increase in symptoms of heart failure, pain in the heart and increased heart rate, bradycardia, increased frequency of angina attacks, and possibly an increase in existing peripheral circulatory disorders (up to gangrene) .

From the senses: dry mouth, conjunctivitis, decreased secretion of the lacrimal gland (this circumstance should be taken into account in patients who wear contact lenses), weight gain, visual and hearing disorders (tinnitus) may rarely be observed.

Allergic reactions: itching, rash (in most cases psoriasiform or dystrophic skin lesions), hair loss, skin photosensitivity, allergic rhinitis.

From the outside endocrine system: Patients with diabetes may develop hypoglycemia.

From the hematopoietic system: thrombocytopenia, leukopenia.

To whom is Metoprolol tartrate contraindicated?

Sinoauricular block II and III degree, cardiogenic shock decompensated heart failure, bradycardia less than 50 beats per minute, severe arterial hypotension, metabolic acidosis, severe peripheral circulatory disorders, bronchial asthma, hypersensitivity to Metoprolol tartrate and its components.

Interactions of Metoprolol tartrate

When taking Metoprolol tartrate simultaneously with insulin or oral hypoglycemic agents, their effect may be enhanced or prolonged. In this case, the symptoms of hypoglycemia (especially tachycardia and tremor) may be masked. In such cases, it is necessary to regularly monitor blood glucose levels.

With simultaneous use of Metoprolol tartrate and

• Tricyclic antidepressants, barbiturates, phenothiazines, nitroglycerin, diuretics, vasodilators and other antihypertensive agents (eg, prazosin), oral contraception, ranitidine, cimetidine - the hypotensive effect may be enhanced;
• Calcium antagonists (such as nifedipine) - in addition to enhancing the hypotensive effect, heart failure may develop;
• Calcium antagonists (such as verapamil and diltiazem) or other antiarrhythmic drugs (for example, disopyramide) - arterial hypotension, bradycardia, other cardiac arrhythmias and heart failure may develop;
• Cardiac glycosides, reserpine, α-methyldopa, guanfacine and clonidine - severe bradycardia may develop, conduction disturbances clonidine can be canceled only a few days after stopping treatment with metoprolol tartrate;
• Norepinephrine, adrenaline or other sympathomimetic drugs, as well as monoamine oxidase inhibitors - may increase blood pressure and reduce the effect of Metoprolol tartrate;
• Indomethacin and rifampicin - the hypotensive effect of Metoprolol tartrate may decrease; lidocaine - it is difficult to remove the latter;
• Peripheral muscle relaxants (for example, suxamethonium, tubocurarine) - may enhance neuromuscular blockade. Narcotics enhance the hypotensive effect of Metoprolol tartrate. At the same time, the negative inotropic effect of these drugs is potentiated. Therefore, before surgery under general anesthesia, the anesthesiologist should be informed that the patient is taking Metoprolol tartrate.

Overdose of Metoprolol tartrate

In case of an overdose of the drug, the following is observed: arterial hypotension, bradycardia up to cardiac arrest, acute heart failure, cardiogenic shock, respiratory failure and bronchospasm, nausea and vomiting, headache, loss of consciousness and generalized convulsions. In this case, general detoxification measures are carried out (gastric lavage, taking activated carbon), symptomatic treatment.

Analogs of the drug metoprolol tartrate are presented, in accordance with medical terminology, called “synonyms” - drugs that are interchangeable in their effects on the body, containing one or more identical active ingredients. When selecting synonyms, consider not only their cost, but also the country of production and the reputation of the manufacturer.

Description of the drug

List of analogues

Note! The list contains synonyms of Metoprolol tartrate, having similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by your doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from Eastern Europe: KRKA, Gedeon Richter, Actavis, Egis, Lek, Hexal, Teva, Zentiva.

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Official instructions for use

METOKARD ®

Registration number:

Trade name of the drug:

International nonproprietary name:

Dosage form:

Compound:

Pharmacotherapeutic group:

Pharmacological properties

Indications for use

Contraindications

Pregnancy and lactation period.

Directions for use and doses

Side effect

Overdose

Interaction with other drugs

special instructions

Release form

Storage conditions

Best before date

Vacation conditions

Manufacturer

The information on the page was verified by physician-therapist E.I. Vasilyeva.

Metoprolol tartrate is a drug belonging to beta-blockers.

What is the composition and release form of the drug Metoprolol tartrate?

The drug contains the active compound - metoprolol tartrate in a dosage of 50 mg or 100 mg. The excipients of the medicine are: potato starch, added lactose monohydrate, in addition, magnesium stearate, colloidal silicon dioxide.

The drug Metoprolol tartrate can be stored for three years from the date of pharmaceutical release, after which you should refrain from using it, as the drug will lose its properties.

What is the effect of the drug Metoprolol tartrate?

The drug Metoprolol tartrate has a hypotensive effect, as well as antianginal and antiarrhythmic effects. Reduces heart rate, affects AV conduction, slowing it down somewhat, in addition, reduces myocardial contractility, reduces cardiac output and oxygen demand of the heart muscle.

The hypotensive effect stabilizes by the end of the 14th day of the course of use of the drug Metoprolol tartrate. With angina pectoris, the patient's frequency of heart attacks and their severity decreases. When arrhythmia normalizes heart rate. Under the influence of the drug during a heart attack, the ischemic area is limited.

What are the indications for use of Metoprolol tartrate?

I will list when Metoprolol tartrate is indicated for use:

Arterial hypertension;
IHD;
Hyperkinetic cardiac syndrome;
Rhythm disturbances (paroxysmal and extrasystole, ventricular arrhythmia, supraventricular tachycardia, atrial fibrillation);
Hypertrophic cardiomyopathy;
Mitral valve prolapse;
Migraine prevention;
With thyrotoxicosis.

In addition, the drug is prescribed for the prevention and treatment of heart attacks.

What are the contraindications for use of the drug Metoprolol tartrate?

The instructions for use prohibit the use of the drug Metoprolol tartrate in the following situations:

Hypersensitivity to the components of the drug;
For 2nd and 3rd degree AV block;
With sinoatrial block;
When breastfeeding;
Arterial hypotension;
For decompensated heart failure;
Sinus bradycardia;
Pregnancy;
Cardiogenic shock.

In addition, the drug Metoprolol tartrate is not prescribed for severe impairment of the so-called peripheral circulation.

What are the uses and dosage of Metoprolol tartrate?

The dose of Metoprolol tartrate is determined by the treating specialist. The tablets are not chewed; it is recommended to swallow them whole after a meal with a small amount of water. Maximum daily dosage means - 400 milligrams. The duration of the course can last for three years.

For arterial hypertension, 100 mg per day is usually prescribed once, or the dose is divided into two doses. The doctor may increase the dose of the medication to 200 milligrams. For angina pectoris, it is recommended to start therapy with Metoprolol tartrate with a dose of 50 or 100 mg.

What are the side effects of Metoprolol tartrate?

The drug Metoprolol tartrate can cause the following side effects: weakness, dizziness, bradycardia, headache, depressive state, decreased concentration of attention, hypotension is noted, drowsiness or insomnia is associated, nightmares, muscle cramps, cold extremities, paresthesia are characteristic, in addition, heart failure, nervousness, anxiety, as well as edema syndrome and weakened libido.

Other side effects include: blurred vision, conjunctivitis, lethargy, arrhythmia, increased fatigue, fainting, anxiety, possible confusion, and loss of body weight. momentary loss memory, hallucinations, bronchospasm and shortness of breath, tinnitus, as well as a disturbance in the sense of taste occur.

Except listed symptoms you can note: muscle weakness, thrombocytopenia, leukopenia, agranulocytosis, nausea are characteristic, abdominal pain is noted, constipation or diarrhea is possible, vomiting, dry mouth, arthralgia, myalgia, liver dysfunction, in addition, flatulence, heartburn, some changes in the skin, reversible alopecia, photosensitivity, as well as exacerbation of psoriasis and hyperhidrosis ( increased sweating).

Overdose from Metoprolol tartrate

special instructions

In case of increasing bradycardia, while using Metoprolol tartrate, it is recommended to reduce the dosage of the drug. Against the background of diabetes mellitus, doses of antidiabetic drugs should be adjusted, and glycemic levels will also need to be monitored.

How to replace Metoprolol tartrate, what analogues should I use?

Metozok, Corvitol 100, Lidalok, Emzok, Metoprolol Zentiva, Betalok, Egilok, Egilok Retard, Metoprolol succinate, in addition, Vasocardin retard, Betalok ZOK, Corvitol 50, Metoprolol-Acri, Metoprolol-OBL, Betalol, Egilok S, Metolol, Metoprolol -ratiopharm, Metoprolol, Metocard, Serdol, Vazocardin, Metocor Adifarm are analogues.

Conclusion

Metoprolol tartrate can only be prescribed by qualified specialist. If side effects occur, the patient should consult a doctor.

The patient must independently study the instructions for use of the prescribed drug. Be healthy!

Registration number:

Validity registration certificate:

30.06.2017

Title in English:

METOPROLOL TARTRATE

Compound

active substance: metoprolol;

1 tablet contains metoprolol tartrate 50 mg (0.05 g) or 100 mg (0.1 g) calculated as 100% dry substance;

Excipients: potato starch, lactose monohydrate, magnesium stearate, colloidal anhydrous silicon dioxide.

Dosage form

Basic physical and chemical properties: tablets are white, with a flat surface, scored and chamfered. Gray inclusions are allowed on the surface of the tablets.

Pharmacotherapeutic group. Selective beta-adrenergic receptor blockers.

ATX code C07A B02.

Pharmacological properties

Pharmacodynamics.

Metoprolol tartrate is a cardioselective β-blocker without intrinsic sympathomimetic activity and membrane stabilizing effect. It affects mainly β 1 -adrenergic receptors of the heart, has antianginal, hypotensive and antiarrhythmic effects. In patients who have had a myocardial infarction, it reduces the risk of recurrent myocardial infarction, and in patients with arterial hypertension, it reduces the risk of cardiovascular complications (stroke). Its anti-ischemic effect has been proven in the case of silent myocardial ischemia and reduction of left ventricular hypertrophy in patients with arterial hypertension.

The antianginal effect is due to a decrease in heart rate, myocardial contractility, and systemic blood pressure, which leads to a decrease in myocardial oxygen demand. Due to the lengthening of diastole (due to the negative chronotropic effect), myocardial perfusion improves.

In contrast to non-selective β-blockers, Metoprolol tartrate, when used in average therapeutic doses, has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries, insulin release, carbohydrate and lipid metabolism.

Pharmacokinetics. After oral administration, absorption of Metoprolol tartrate from the gastrointestinal tract is almost complete (90%) and does not depend on food intake, but bioavailability is about 50% due to intensive metabolism during the first pass through the liver (65–80%). With prolonged use, bioavailability increases due to decreased blood circulation in the liver and saturation of liver enzymes. The maximum concentration of the drug in the blood plasma is recorded after 1–2 hours, but the effect on blood pressure and heart rate is observed (after a single dose of 100 mg) for 12 hours.

The half-life is 3–7 hours. In case of renal failure, it increases to 27 hours or more. Excreted by the kidneys in the form of metabolites. In case of liver failure, the drug can accumulate in the body. It penetrates well through the blood-brain and placental barriers and into breast milk. Smoking, drinking alcohol, taking certain medicines changes the metabolism of Metoprolol tartrate (for example, barbiturates, difenin, rifampicin - increase, chlorpromazine - decrease). Biotransformation in the liver decreases in cirrhosis, so in such patients the dose is reduced and the concentration in the blood plasma is monitored.

Clinical characteristics

Indications

Metabolic acidosis.

Suspicion of acute myocardial infarction with heart rate 0.24 c, systolic blood pressure

Hypersensitivity to the components of the drug or to other beta blockers.

Interaction with other drugs and other types of interactions.

Metoprolol is a substrate of the CYP 2D6 enzyme. Plasma concentrations of metoprolol may be affected by drugs that inhibit CYP 2D6, for example: quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine. When starting treatment with these drugs, it may be necessary to reduce the dose of Metoprolol tartrate.
The simultaneous use of Metoprolol tartrate with the following drugs should be avoided:

Barbituric acid derivatives: Barbiturates (studied for pentobarbital) stimulate the metabolism of metoprolol by enzyme induction.

Propaphenone: In 4 patients treated with metoprolol, after taking propafenone, metoprolol plasma concentrations increased 2-5 times, and 2 patients experienced side effects typical of metoprolol. The interaction was confirmed in 8 healthy volunteers. This interaction may be explained by the fact that propafenone, like quinidine, inhibits the metabolism of metoprolol through the cytochrome P450 2D6 system. The result of this combination is unpredictable, since propafenone also has beta-blocking properties.

Verapamil: in combination with beta-blockers (described for atenolol, propranolol and pindolol), verapamil can cause the development of bradycardia and a decrease in blood pressure. Verapamil and beta blockers have additive inhibitory effects on atrioventricular conduction and sinus node function.

Concomitant use of Metoprolol tartrate with the following drugs may require dose adjustment

Amiodarone: Clinical case reports confirm that patients taking amiodarone may develop severe sinus bradycardia if the drug is co-administered with metoprolol. Amiodarone is extremely a long period half-life (approximately 50 days) – this means that the interaction may occur for a long time after discontinuation of this drug.

Antiarrhythmic drugs class I: Class I antiarrhythmics and beta blockers have additive negative inotropic effects, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. The use of this combination should also be avoided in patients with sick sinus syndrome and atrioventricular conduction disorders. This interaction is best described for disopyramide.

Non-steroidal anti-inflammatory/anti-rheumatic drugs (NSAIDs)): NSAIDs have been shown to antagonize the antihypertensive effects of beta blockers. Indomethacin was mainly studied. It is likely that this interaction does not occur with sulindac. Study negative interaction was carried out with diclofenac.

Digitalis glycosides: Concomitant use of digitalis glycosides and beta-receptor blockers may increase atrioventricular conduction time and cause bradycardia.
Diphenhydramine: Diphenhydramine reduces (2.5 times) the metabolism of metoprolol to alpha-hydroxymetoprolol through the CYP 2D6 system in individuals with rapid hydroxylation. The effects of metoprolol are enhanced.

Diltiazem: Diltiazem and beta-receptor blockers have additive inhibitory effects on antrioventricular conduction and sinus node function. Severe bradycardia has been observed during treatment with diltiazem.

Epinephrine: After administration of epinephrine (adrenaline) to patients who used non-selective beta-receptor blockers (including pindolol and propranolol), severe hypertension and bradycardia developed (approximately 10 cases). In addition, it has been suggested that epinephrine, which is found in local anesthetics, may provoke the development of these reactions in the case of intravascular administration of the drug. The risk is probably less when used with cardioselective beta blockers.
Phenylpropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg may lead to an abnormal increase in diastolic blood pressure in healthy volunteers. Propranolol generally counteracts the increase in blood pressure caused by phenylpropanolamine. However, beta-receptor blockers may provoke paradoxical hypertensive reactions in patients using high doses of phenylpropanolamine. 2 cases have been described hypertensive crisis during treatment with phenylpropanolamine only.

Quinidine: Quinidine inhibits the metabolism of metoprolol into so-called rapid metabolizers with a significant increase in plasma levels and a resulting increase in beta-receptor blockade. Similar interactions may occur with other beta blockers that are metabolized by the same enzyme (cytochrome P450 2D6).

Clonidine: Beta blockers may potentiate the hypertensive response when clonidine is suddenly discontinued. If concomitant clonidine therapy must be discontinued, the beta blocker should be discontinued several days before clonidine is discontinued.
Rifampicin: Rifampicin may stimulate the metabolism of metoprolol, resulting in a decrease in its plasma levels.

Patients receiving other beta-blockers (eg, eye drops) or monoamine oxidase inhibitors (MAOIs) concomitantly with metoprolol should be closely monitored. The administration of inhalational anesthetics to patients receiving treatment with beta-receptor blockers increases the cardiodepressive effect. In patients receiving beta blockers, repeated dosage adjustments of oral antidiabetic agents may be necessary. Metoprolol plasma concentrations may increase if cimetidine or hydralazine is coadministered.
The plasma concentration of metoprolol may increase if alcohol is consumed at the same time.

Patients receiving sympathetic ganglion blockers concomitantly with metoprolol should be closely monitored.

Metoprolol may interfere with the elimination of lidocaine.

It is necessary to prescribe metoprolol with caution to patients who use stimulants of β 2 receptors and β 1 receptors, as well as dihydropyridines.

Additional insulin dosage adjustments may be necessary in patients receiving beta blockers.

Caution should be exercised when metoprolol is used concomitantly with ergotamine.
Caution should be exercised when combining metoprolol with other drugs with antihypertensive effects.

Features of application.

Patients receiving treatment with beta blockers should not receive intravenous verapamil.
Metoprolol may cause peripheral arterial circulatory disorders such as intermittent claudication. Patients with severe renal impairment, with serious acute conditions and patients who receive combination treatment with digitalis preparations, special attention should be paid.

In patients with Prinzmetal's angina, the frequency and severity of angina may increase as a result of alpha receptor-mediated narrowing coronary vessels. Therefore, such patients should not be prescribed non-selective beta blockers. Selective β 1 blockers should be used with caution.

When treating patients with bronchial asthma or other obstructive pulmonary diseases, adequate bronchodilator therapy should be prescribed simultaneously. It may be necessary to increase the dose of beta 2 receptor stimulants.

During treatment with metoprolol, the risk of effects on carbohydrate metabolism or the risk of latent hypoglycemia is less than with the use of non-selective beta blockers.

Very rare condition of patients with impaired atrioventricular conduction medium degree severity may worsen (possibly to atrioventricular block).
Beta blocker therapy may reduce the effectiveness of treatment of anaphylactic reactions. Treatment with adrenaline in normal doses does not always lead to the expected therapeutic effect.

Patients with pheochromocytoma treated with metoprolol tartrate should be simultaneously prescribed an alpha blocker.

Data from controlled clinical studies on the effectiveness and safety of the drug in patients with severe stable symptomatic heart failure (NYHA (New York Heart Association) class IV) are limited. Treatment of such patients should only be carried out by doctors with special skills and experience (see section "Dosage and Administration").

Patients with symptomatic heart failure accompanied by acute myocardial infarction and unstable angina were excluded from the study, which established the possibility of using the drug in heart failure.

Thus, the effectiveness and safety of treatment of acute myocardial infarction accompanied by heart failure has no documented evidence. The use of Metoprolol tartrate is contraindicated in unstable, uncompensated heart failure.

Abrupt discontinuation of beta blockers is dangerous, especially in high-risk patients, and may worsen congestive heart failure and increase the risk of myocardial infarction and sudden death. Therefore, it is necessary to stop treatment with metoprolol for any reason, if possible gradually, over at least 2 weeks, when the dose at each stage is halved to the smallest dose of 12.5 mg (half a 25 mg tablet). The lowest dose should be taken for at least 4 days until the drug is completely discontinued. If symptoms return, it is recommended to slow down the dose reduction.

In case of surgery, it is necessary to warn the anesthesiologist that the patient is taking Metoprolol tartrate. It is not recommended that patients undergoing surgery discontinue treatment with beta blockers. If discontinuation of metoprolol is considered necessary, it should, if possible, occur at least 48 hours before general anesthesia. Urgent initiation of high-dose metoprolol in patients who have had non-cardiac events surgical interventions should be avoided as it is associated with bradycardia, hypotension and stroke, including death in patients with cardiovascular risk factors.

However, for some patients, the use of beta blockers as premedication is desirable. In such cases, it is necessary to choose an anesthetic with a slight negative inotropic effect in order to minimize the risk of myocardial depression.

Hemodynamic status should be carefully monitored in patients with suspected or known myocardial infarction.

The use of metoprolol may lead to an increase in less severe peripheral circulatory disorders.

In patients with a history of heart failure or poor cardiac reserve, the need for concomitant diuretic therapy should be considered.
The use of metoprolol may lead to the development of bradycardia in patients.

Metoprolol should be prescribed with caution to patients with first degree heart block.
Metoprolol may mask early symptoms of acute hypoglycemia during tachycardia, as well as symptoms of thyrotoxicosis.

Serious attention should be paid to patients with psoriasis.

When using metoprolol in patients with labile and type I diabetes mellitus, there may be a need to adjust the dose of the hypoglycemic drug.

The drug contains lactose, so it should not be prescribed to patients with hereditary lactase deficiency, galactose intolerance or disorders of glucose/galactose metabolism.

Use during pregnancy or breastfeeding.

Metoprolol tartrate should not be used during pregnancy and lactation unless the doctor considers that the benefit outweighs the possible harm to the fetus/child. Beta blockers reduce placental blood flow, which can lead to intrauterine fetal death, immaturity and premature birth.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Dizziness and fatigue may occur during treatment with Metoprolol tartrate. Patients whose activities require increased attention (driving a car, working with machinery) should be warned about the possibility of such effects.

Directions for use and doses

The dose of Metoprolol tartrate is determined individually. The maximum daily dose is 400 mg.

The tablets are taken orally, with a small amount of liquid, without chewing, after meals.

The duration of treatment is determined individually and can be 3 years.

At arterial hypertension The initial dose is 100 mg per day once or divided into two doses (morning and evening). If necessary, the daily dose can be increased to 200 mg.

At angina pectoris Prescribe 50–100 mg of Metoprolol tartrate 2–3 times a day.

At arrhythmias Prescribe 50 mg 2-3 times a day. If necessary, the daily dose is increased to 300 mg, divided into 2-3 doses.

At hyperthyroidism (thyrotoxicosis) prescribed 50 mg 4 times a day. When a therapeutic effect is achieved, the dose is gradually reduced.

For myocardial infarction(it is advisable to start treatment within the first 12 hours after the onset of chest pain): 50 mg every 6 hours for 48 hours, the recommended maintenance daily dose is 200 mg, divided into 2 doses. The course of treatment is at least 3 months.

Preventing migraine attacks: Metoprolol tartrate is prescribed at a dose of 100–200 mg per day, divided into 2 doses.

Correction of the dosage regimen is necessary for patients with impaired liver function.

Elderly patients and patients with renal failure do not need dose adjustment.

Children. The use of Metoprolol tartrate is contraindicated in children.

Overdose

Toxicity: In an adult, taking a dose of 7.5 g caused fatal intoxication. Taking 100 mg of the drug by a 5-year-old child was not accompanied by symptoms of intoxication after gastric lavage. A dose of 450 mg caused moderate intoxication in a 12-year-old child and a dose of 1.4 g in an adult; a dose of 2.5 g caused severe intoxication in an adult; and a dose of 7.5 g caused very serious intoxication.

Symptoms: the most important are cardiovascular symptoms However, in some cases, especially in children and young people, central nervous system symptoms and respiratory depression may predominate. Bradycardia, atrioventricular block I–III degree, prolongation of the QT interval (exceptional case), asystole, decreased blood pressure, insufficient peripheral perfusion, heart failure, cardiogenic shock. Respiratory depression, respiratory arrest. Others: fatigue, confusion, loss of consciousness, small-scale tremor, convulsions, sweating, paresthesia, bronchospasm, nausea, vomiting, esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia. Effect on the kidneys. Temporary myasthenic syndrome. Concomitant use of alcohol antihypertensive drugs, quinidine or barbiturates may worsen the patient's condition. The first signs of an overdose can be observed 20 minutes - 2 hours after taking the drug.

Treatment: if necessary, gastric lavage, taking activated charcoal. Atropine (0.25-0.5 mg intravenously in adults, 10-20 mcg/kg body weight in children) should be administered before gastric lavage (due to the risk of vagal stimulation). May require intubation and use of a machine artificial respiration; adequate volume restoration; glucose infusion; ECG monitoring; repeated intravenous administration of atropine 1–2 mg (mainly for vagal symptoms). In case of inhibition of myocardial function: infusion of dobutamine or dopamine and calcium glubionate 9 mg/ml, 10–20 ml. Glucagon 50–150 mcg/kg IV over 1 minute followed by infusion can be given, as can amrinone. Adding epinephrine (adrenaline) has been effective in some cases. Infusion of sodium (sodium chloride or bicarbonate) in case of prolongation of the QRS complex and arrhythmia. A pacemaker may be used. If circulatory arrest occurs, resuscitation measures may be required for several hours. For bronchospasm, prescribe terbutaline (injection or inhalation). Symptomatic therapy.

Adverse reactions

Adverse reactions occur in approximately 10% of patients and are usually dose-related. Adverse reactions associated with the use of metoprolol are listed below depending on the organ class and frequency. Frequency is defined as follows: very often (> 1/10); often (> 1/100 – 1/1000 – 1/10000 –

Also, when using metoprolol, insomnia, drowsiness, amnesia, first degree heart block, increased existing atrioventricular block, postural disorders (very rarely with syncope), Raynaud's phenomenon, increased symptoms of intermittent claudication, rash (in the form of psoriatiform urticaria and dystrophic skin lesions) may be observed. , impotence/sexual dysfunction, precordial pain, the appearance of antinuclear antibodies (not related to systemic lupus erythematosus).

Best before date

Do not use the drug after the expiration date indicated on the package.

Storage conditions

Store in original packaging at a temperature not exceeding 25 o C.

Keep out of the reach of children.

Package.

10 tablets in a blister. 2 or 5 blisters per pack.

On prescription.

Manufacturer

PJSC Farmak.

Manufacturer's location and address of place of business

Ukraine, 04080, Kyiv, st. Frunze, 74.

Date of last revision.

End of the official instructions

Additional Information

Pharmacotherapeutic group:

Selective beta-adrenergic receptor blockers.