What does Metoprolol help with? Instructions for use

Existing analogues of the drug

What to do if the patient was unable to purchase the medication Metoprolol prescribed by the doctor?
Its analogues are available in any pharmacy. Most of them contain a similar active ingredient, due to which they have the same properties as the mentioned drug. Among such medicines the following can be noted: “Metoprolol-Acri”, “Metolol”, “Metocor Adifarm” and others. After purchasing these products, the patient is recommended to read the attached instructions and also consult a doctor. This is due to the fact that the methods of administration may differ from the dosages of the above-mentioned drug.

What other analogues does this drug have? You can replace the medication prescribed by your doctor with the following medications: Bisoprolol, Metoprolol-ratiopharm, Metocard, Corvitol, Metozok, Lidalok, Serdol, Egilok, Emzok and others.

Indications for treatment with Metoprolol

Metoprolol is used as the only treatment for uncomplicated cardiovascular conditions. Indicated for use in the complex treatment of moderate to moderate heart disorders. Prescribed for:

• arterial hypertension (hypertension);
• coronary heart disease;
• angina pectoris;
• heart rhythm disturbances (tachycardia, extrasystoles, arrhythmias);
• cardiomyopathy;
• myocardial infarction;

Prescribed for myocardial infarction

• mitral valve prolapse;
• thyrotoxicosis;
• migraine headaches;
• akathisia (syndrome of constant motor restlessness, “restlessness”).

Metoprolol is quite effective for hypertension. It gradually and painlessly reduces blood pressure, bringing blood circulation back to normal. Acts as a prolonged agent in monotherapy or in combination with other antihypertensive drugs. Not suitable for emergency treatment of hypertensive crisis. Metoprolol is not used for low blood pressure (hypotension).

Active components and properties of the drug

Metoprolol is produced in the form of a solution for intravenous injection (ampoules of 5 ml, each containing 5 mg of active ingredient), as well as in the form of tablets with different dosages (100, 50, 25 mg of active ingredient).

Composition of the drug:

• Metoprolol tartrate (is a white crystalline powder, practically odorless, which is soluble in water, alcohol, chloroform, weakly interacts with acetone and is insoluble in ether).
• Metoprolol succinate (white, odorless crystals, easily soluble in water).

Metoprolol solution and tablets have pronounced antiarrhythmic, hypotensive, and antianginal properties. This drug reduces blood pressure, which “jumped” as a result of stress, severe emotional shock, and increased physical activity.

The hypotensive effect of Metoprolol is due to the fact that the main active ingredient of the drug reduces the force of heart contractions, suppresses the synthesis of renin, and inhibits the functions of the sympathetic part of the central nervous system.

The antianginal properties of the tablets (solution) are ensured by a decrease in the need of heart cells for oxygen and a decrease in heart rate.

The ability to eliminate the factors causing arrhythmia (those that lead to heart rhythm disturbances) - hypertension, increased activity of the sympathetic nervous system - allows Metoprolol to fight various heart rhythm disturbances.

Pharmacokinetics: absorption of Metoprolol (if we are talking about treatment with tablets) is almost complete and is in no way related to food intake, however, the bioavailability of the drug is about 50% (on the first pass through the liver) due to increased metabolism.

Over time, the bioavailability of Metoprolol (if taken on a regular basis) increases due to a decrease in hepatic circulation and gradual saturation of enzymes.

About 90% of the drug is absorbed in the gastrointestinal tract.

Indications for use of Metoprolol Ratiopharm:

• IHD;
• ;
• prevention of angina pectoris;
• hypertension (alone or in combination with other antihypertensive drugs), including the hyperkinetic type;
• supraventricular tachycardia, extrasystole and other heart rhythm disturbances;
• tachycardia caused by thyrotoxicosis (thyroid disease) or functional malfunctions of the myocardium.

Metoprolol solution (tablets) prevent migraines, help restore a “healthy” sinus rhythm and normalize heart rate.

Its advantages include:

• high bioavailability;
• ease of use;
• rapid clinical effect;
• possibility of long-term use;
• affordable price;
• wide range of medical indications.

The main disadvantage is the impressive number of side effects in case of overdose.

Pharmacological group

Metoprolol is a widely used representative of beta-blockers (BABs) throughout the world, the main area of ​​application of which is cardiology. This is explained by their high effectiveness in treating hypertension and coronary disease, chronic circulatory disorders and some arrhythmias.

BABs received their name for their ability to inactivate beta-adrenergic receptors located in the heart (beta1-adrenergic receptors) and in the smooth muscles of blood vessels, bronchi, digestive system, urinary and genital tracts (beta2-adrenergic receptors).

Metoprolol is a cardioselective (selective) β1-blocker. In other words, this drug has a higher affinity for β1-adrenergic receptors than for β2-adrenergic receptors, which allows its use to avoid some side effects. By acting on β1-adrenergic receptors, it causes a decrease in the strength and frequency of heart contractions (HR), which is mainly responsible for its pharmacological effect.

Metoprolol does not have internal sympathomimetic activity, since it is a pure beta blocker, that is, it does not activate β-adrenergic receptors, unlike some other representatives of this pharmaceutical group, which could negate the beta-blocking effect.

What is Metoprolol used for?

Indications for prescribing the medicine are:

• high levels of thyroxine and triiodothyronine;
• IHD (heart attack and angina);
• arrhythmia such as ventricular extrasystole;
• supraventricular tachycardia;
• recurrent migraine attacks;
• arterial hypertension of various origins (primary and secondary);
• functional disorders of the heart, accompanied by rapid heartbeat;
• chronic cardiovascular failure.

Tablets with a beta blocker increase exercise tolerance during ischemia of the heart muscle.

For thyrotoxicosis

Metoprolol is effective for thyrotoxicosis. This condition is characterized by tissue poisoning with thyroxine and triiodothyronine. The most common cause is hyperthyroidism. Thyrotoxicosis develops against the background of diffuse toxic and nodular goiter, as well as autoimmune thyroiditis.

Like other blood pressure-lowering medications (Bisoprolol-Teva, Nifedipine, Concor and Atenolol), Metoprolol lowers blood pressure against the background of high levels of thyroid hormones.

At what pressure

For moderate arterial hypertension, monotherapy with Metoprolol can be performed. Combination with other drugs that lower blood pressure (Amlodipine, Losartan) is possible. The indication for prescribing Metoprolol is blood pressure over 140/90 mmHg. and higher.

Metoprolol succinate in the treatment of chronic heart failure

β-blockers are the main drugs for the treatment of CHF, i.e. medications whose effect has been proven beyond doubt, and which are recommended specifically for the treatment of CHF (evidence level A). The Russian recommendations for the diagnosis and treatment of CHF (third revision) mention three β-blockers, including metoprolol succinate, which showed a reduction in the risk of death in patients with CHF, and in addition - the risk of sudden death, death from progression of CHF and reduced the frequency of hospitalization. In 2012, new European guidelines for the diagnosis and treatment of acute and chronic heart failure were adopted, which stated that β-blockers are recommended in addition to angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists (ARBs) in case of intolerance to the inhibitors ACE for all patients with systolic CHF II–IV class with ejection fraction (EF) ≤40%. The effectiveness of metoprolol succinate for the treatment of patients with CHF was revealed in the double-blind placebo-controlled study MERIT-HF (Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure), which was devoted to studying the effectiveness of metoprolol succinate CR/XL in patients with CHF II-IV class according to NYHA and EF less than 40%. The number of patients included was 3991, of whom 1926 were hospitalized for myocardial infarction (MI). The average EF was 28%. Most patients received concomitant therapy with diuretics, ACE inhibitors and digoxin. The observation period was 1 year. Patients were randomized to receive metoprolol succinate CR/XL or placebo. The starting dose of metoprolol succinate CR/XL was 12.5–25 mg/day. Within 6 weeks. the dose of the drug was increased to 100 mg/day, and subsequently to 200 mg/day. subject to compensated hemodynamics (by the end of the study, the dose of furosemide varied on average from 60 to 100 mg/day). The MERIT-HF study was stopped early when it became clear that mortality was significantly lower in the active treatment group than in the placebo group: in the metoprolol succinate CR/XL group, overall mortality decreased by 34% (p = 0.0062), and the incidence of sudden death – by 41% (p=0.002). Results of the study: reduction in overall mortality by 34%, sudden mortality by 41%, and from progression of CHF by 49%. The single endpoint of all-cause mortality/hospitalization for progression of heart failure decreased by 31% (p<0.001), and cardiac death/nonfatal myocardial infarction decreased by 39% (p<0.001). The effectiveness of metoprolol succinate CR/XL did not depend on the etiology of CHF (ischemic or non-ischemic), the age of patients, the presence of arterial hypertension (AH) or diabetes mellitus. A slightly greater effectiveness of metoprolol succinate CR/XL was noted in patients with FC III and IV CHF compared to patients with FC II CHF according to the NYHA classification. Previous population-based studies, and in particular the Framingham Study, have clearly demonstrated that there really are differences in the incidence and survival of patients in different groups. These include different survival rates between men and women, differences in age and severity of the underlying disease, and the severity of concomitant pathology. In addition, the dose of the drug achieved during treatment and the dependence of the treatment effect on the dose achieved are also of great importance. Thus, the question of the effectiveness of β-blockers in patients with CHF of different gender (especially women), age, with different severity of CHF, in the presence of concomitant pathology, and the use of different doses of the drug seems relevant. The effect of metoprolol succinate on the course of CHF in women. The prevalence of CHF among men is higher than among women in the age group under 60 years. However, due to longer life expectancy, the number of women with CHF is 2.6 times higher than the number of men (72 versus 28%). The MERIT-HF study (n=3093) included 898 women. Noteworthy is the fact that the women were older (65 years, p<0.001), with a more severe course of congestive heart failure (higher FC, hypertension, diabetes mellitus are more often observed, but slightly higher EF), but there were fewer smokers, patients with coronary heart disease (CHD) and atrial fibrillation. Treatment with metoprolol CR/XL compared with placebo in women reduced the risk of hospitalization by 19% (p=0.044); hospitalizations due to cardiovascular diseases - by 29% (p = 0.013); hospitalizations due to progression of CHF – by 42% (p=0.021). There was no significant difference in the effect on the primary endpoint of mortality. The main result is a reduction in the risk of developing the combined endpoint of death + hospitalization due to progression of CHF by 21% (p = 0.044). Treatment of women with severe CHF with metoprolol CR/XL also led to a reduction in the number of hospitalizations, but the greatest effect was achieved in influencing the combined endpoint - a risk reduction of 63% (p = 0.0008). Among men, treatment with metoprolol CR/XL resulted in a 10% reduction in the risk of hospitalization (p=0.044); cardiovascular hospitalization – by 14% (p=0.005), and hospitalization due to progression of CHF – by 18% (p=0.0001). The use of metoprolol CR/XL among men demonstrated a significant reduction in overall mortality - 7.3 versus 12% (p = 0.0001), cardiovascular mortality - 172 versus 101 (p < 0.0001), mortality due to progression of CHF - 48 versus 25 (p=0.006) and sudden death – 114 versus 62 (p=0.0001) people. In terms of the impact on the combined endpoint of death + hospitalization due to progression of CHF, the use of metoprolol CR/XL in men had a slightly smaller effect than in women - a reduction in the risk of development by 18% (p = 0.0011). Among men with severe CHF, the effect of metoprolol CR/XL therapy on study endpoints was also noted: a reduction in the risk of hospitalization by 20% (p = 0.04), hospitalization from cardiovascular causes by 25% (p = 0.01) ), due to progression of CHF – by 35% (p=0.01). The main difference is that, in comparison with placebo, the use of metoprolol CR/XL in men led to a significant reduction in overall mortality by 40% (p = 0.015), cardiovascular mortality - by 45% (p = 0.007), due to the progression of CHF - by 50% (p=0.056) and sudden death – by 48% (p=0.025) (Table 1). When comparing men and women who received placebo in the study, it turned out that being female leads to a 37% reduction in the risk of death during concomitant therapy with ACE inhibitors and diuretics (p = 0.015). A similar comparison among patients treated with metoprolol CR/XL did not produce significant differences. Consequently, therapy for CHF with metoprolol succinate is effective in both sexes. Effect of metoprolol succinate on the course of severe CHF (NYHA class III–IV) As part of the MERIT-HF study, an analysis was performed in a subgroup of patients with severe CHF. This subgroup included 795 patients with an EF of less than 25% and a clinical picture of NYHA class III–IV CHF. Among these patients, 399 were randomized to metoprolol CR/XL and 396 to placebo. All received adequate concomitant therapy with ACE inhibitors and diuretics. The baseline characteristics of the patients were almost identical. As a result of the analysis of the results obtained, a decrease in the risk of death by 39% (p = 0.0086), a decrease in the risk of sudden death by 45% (p = 0.024), a decrease in the risk of death due to progression of CHF by 55% (p = 0.015) was found (Fig. . 1). In addition, the reduction in the risk of the combined indicator of death + hospitalization was 29% (p = 0.0012), the reduction in the risk of death + hospitalization due to progression of CHF was 44% (p < 0.0001), as well as a decrease in the indicator of cardiac death or non-fatal MI by 46% (p=0.0014). Effect of dose of metoprolol succinate on the course of the disease In the MERIT-HF study, the number of patients was 3991, of whom 1845 received placebo, and 1806 were allocated to the metoprolol CR/XL treatment group. According to the protocol, after a two-week washout period, titration of metoprolol CR/XL began with doses of 12.5–25 mg, and patients with initially more severe CHF (NYHA class III–IV) began titration with a dose of 12.5 mg. The target dose of the drug was 200 mg once daily. The dose was increased every 2 weeks. As a result, by the 3rd month visit. patients reached the doses they received in the further study. The researchers interpreted the distribution of high doses/low doses as follows: • high doses – the dose of the drug in the study was more than 100 mg/day; • low doses – the dose of the drug in the study is less than or equal to 100 mg/day. During the study, 1202 patients received high doses of the drug, and 604 patients received low doses. It should be especially noted that the doses were achieved during titration and were the maximum for each patient individually, which was assessed by heart rate and blood pressure levels. Comparison of the initial characteristics of both observation groups gave the following results: the low-dose group included mainly patients with severe CHF - NYHA class III-IV (67 versus 53%), was significantly older in age (65.9 versus 62.5 years ), with initially lower blood pressure and a higher incidence of ischemic heart disease as a cause of heart failure. In addition, a history of MI was more common in the low-dose group. In terms of the effect on the primary endpoint, both comparison groups were identical - the reduction in the risk of death was 38% in both cases (p = 0.010 for low doses and p = 0.0022 for high doses), although in the low-dose group there was a tendency to higher mortality (8.2 vs. 6.2%). There were also no significant differences in the effect on the secondary combined endpoint of death + hospitalization: the risk reduction in the high-dose group was 29% (p < 0.0001), and in the low-dose group – 22% (p = 0.0056) . Consequently, dose titration and achieving an individual maximum tolerated and effective dose for each patient ensures that there are no differences in the effect of high and low doses of the drug on the course of CHF. The starting dose of metoprolol succinate for patients with CHF is 12.5 mg 1 time/day, the therapeutic dose is 100 mg, the maximum dose is 200 mg 1 time/day. For metoprolol succinate, the dose titration is: 12.5 – 25 – 50 – 75 – 100 – 200 mg. The titration period is 2 weeks, and in case of questionable tolerability - 4 weeks. The effect of metoprolol succinate on the course of CHF in patients with hypertension. Hypertension is one of the main causes of the development of CHF in Russia (88% of cases), as well as ischemic heart disease (59% of cases). The combination of hypertension and ischemic heart disease occurs in half of patients with CHF. The MERIT-HF study analyzed the effect of metoprolol CR/XL treatment on endpoints in a subgroup of patients with hypertension. A total of 1747 patients with hypertension were included in the study. Of these, 871 patients received metoprolol CR/XL, and 876 patients received placebo. The treatment results are shown in Table 2. From the data presented in Table 2, it is obvious that therapy with metoprolol CR/XL in the group of patients with a history of hypertension is no less effective than therapy with metoprolol CR/XL in the general study population. Therefore, metoprolol succinate is an effective drug for the treatment of patients with CHF and hypertension. The Russian recommendations for the diagnosis and treatment of hypertension (4th edition, 2010) have a corresponding section “HTN and CHF”. This section states that in patients with congestive CHF, predominantly systolic, hypertension is often found in the anamnesis, although an increase in blood pressure with a decrease in the contractile function of the LV myocardium is relatively rare. Loop and thiazide diuretics, ACE inhibitors, ARBs, β-blockers and aldosterone antagonists are recommended as initial therapy for hypertension in the presence of congestive CHF. Dihydropyridine antihypertensive agents may be prescribed in case of insufficient antihypertensive effect or in the presence of angina pectoris. Non-dihydropyridine ACs are not used due to the possibility of worsening myocardial contractility and increasing the symptoms of CHF. LV diastolic dysfunction is detected in almost all hypertensive patients with LVH, which is often accompanied by the development of heart failure and worsens the prognosis. There is currently no evidence of benefit of any class of antihypertensive drugs in these patients. The new European guidelines for the diagnosis and treatment of acute and chronic heart failure (2012) also contain an algorithm for the treatment of hypertension in patients with symptomatic heart failure (NYHA class II–IV) and systolic dysfunction. Step 1: ACE inhibitor (or ARB), beta blocker, and mineralocorticoid receptor antagonist as first, second, and third line therapy, respectively (Class I, A). Step 2. Thiazide diuretic (or adding a loop diuretic if the patient is already receiving a thiazide diuretic) if the increase in blood pressure persists despite the combination of an ACE inhibitor (or ARB) + β-blocker + mineralocorticoid receptor antagonist (Class I, C). Step 3. If elevated blood pressure still persists, amlodipine (Class I, A), hydralazine (Class I, A) or felodipine (Class IIa, B) is recommended. Moxonidine and α-blockers are not recommended (Class III, B and Class III, A, respectively). The effect of metoprolol succinate on the course of CHF in patients with concomitant diabetes mellitus Another important cause of the development of CHF, in addition to hypertension and/or coronary artery disease, in our country is diabetes mellitus - its contribution is 11.9%. For patients with CHF, the presence of diabetes mellitus determines a significantly worse prognosis for life. In the MERIT-HF study, the use of metoprolol succinate compared with placebo in patients with and without diabetes mellitus resulted in a reduction in the incidence of hospitalization (Fig. 2). It was found that the frequency of side effects associated with carbohydrate metabolism (hyper- and hypoglycemia), as well as the frequency of new cases of diabetes mellitus, did not differ in the metoprolol succinate group and in the placebo group (Fig. 3). The effect of metoprolol succinate on the course of CHF in elderly patients It is known that the prevalence of CHF increases significantly with age: for example, in the age group from 20 to 29 years old it is only 0.3% of cases, and in the age group over 90 years old, almost 70% have CHF. respondents. More than 65% of patients with CHF are in the age group of 60–80 years. The MERIT-HF study included 1982 elderly (65 years and older) patients with CHF. The results obtained suggest a positive effect of metoprolol succinate on mortality in elderly patients with CHF. Thus, their overall mortality decreased by 37%, the frequency of sudden death - by 43%, and mortality from CHF - by 61% compared to placebo (all of these results are reliable) (Fig. 4). Thus, the presented results of the analysis of the MERIT-HF study indicate that the use of metoprolol succinate is highly effective and safe in patients with both moderate and severe CHF, in patients of different sexes, ages, with a titrated dose of the drug and the presence of concomitant diseases (hypertension, diabetes mellitus). diabetes).

Currently, metoprolol tartrate (Egilok, Egilok Retard, pharmaceutical) is widely used in the pharmaceutical market. Metoprolol tartrate suppresses the effects of increased sympathetic system activity on the heart, and also causes a rapid decrease in heart rate, contractility, cardiac output and blood pressure. In case of CHF against the background of idiopathic hypertrophic obstructive cardiomyopathy, metoprolol tartrate, starting with low doses (2×5 mg/day) with a gradual increase in dose, significantly improves heart function, quality of life and physical endurance of the patient. T.V. Tyurina et al. in their study, they showed the high antianginal effectiveness of Egilok, its ability to increase exercise tolerance, reducing the clinical manifestations of heart failure, dyscirculatory encephalopathy, as well as a significant improvement in the quality of life when taking this drug. According to O.G. Smolenskaya et al., the use of Egilok is possible and rational for CHF both against the background of hypertension and with initially normal blood pressure. At the same time, the clinical condition of patients with CHF significantly improves, which is due to an increase in tolerance to physical activity and the positive effect of the drug on the altered diastolic function of the left ventricular myocardium. In addition, the administration of Egilok to patients with CHF significantly reduces its severity and reduces FC. In 2012, it expanded the line of metoprolol by registering Egilok S (metoprolol succinate) in the Russian Federation. Thus, Egilok S can be successfully used in the treatment of hypertension and CHF, which will significantly increase the effectiveness and safety of therapy for these diseases.

Literature 1. Diagnosis and treatment of chronic heart failure. Russian recommendations, third revision // Heart failure. – 2010. – T. 11 (No. 1). – P. 69–160. 2. ESC Guidelines for diagnosis and treatment of acute and chronic heart failure // Eur. Heart J. 2012. Vol. 33. P. 1787–1847. 3. MERIT–HF Study Group. Effect of metoprolol CR/XL in chronic heart failure: Metoprolol CR/XL Randomized Intervention Trial in Congestive Heart Failure (MERIT–HF) // Lancet. 1999. Vol. 353. P. 2001–2007. 4. Goldstein S. et al. // J. Amer. Coll. Cardiol. 2001. Vol. 38. P. 932–938. 5. Deedwania PC et al. //Eur. Heart J. 2004. Vol. 25. P. 1300–1309. 6. Wikstrand J., Hjalmarson A., Waagstein F. et al. MERIT–HF Study Group. Dose of metoprolol CR/XL and clinical outcomes in patients with heart failure: analysis of the experience in metoprolol CR/XL randomized intervention trial in chronic heart failure (MERIT–HF) // J. Amer. Coll. Cardiol. 2002. Vol. 40(3). P. 491–498. 7. Tyurina T.V., Grotova A.V., Krylova L.G., Bukhensky I.M. Efficacy and safety of Egilok retard in the treatment of arterial hypertension in the elderly // Arterial hypertension. – 2008. – T. 14, No. 1. – P. 143–146. 8. Smolenskaya O.G., Zhdanova I.V., Semyatnikova N.M., Silkina N.N. Egilok in the treatment of chronic heart failure in patients with normal and elevated blood pressure // Ros. cardiol. magazine. – 2002. – No. 4. – P. 48–52.

Analogues and prices

Metoprolol analogues (the instructions should always be read before using any drugs) can only be prescribed by a doctor.

Analogues of the drug are:

• "Betalok", made in Sweden. The cost of the medicine is from 122 to 973 rubles.
• Swedish Betalok Zok costs from 122 to 491 rubles.
• "Egilok", produced at a pharmaceutical plant in Hungary, costing from 67 to 343 rubles per pack.
• "Egilok Retard", price - from 81 to 230 rubles.
• "Metoprolol-Acri" produced in the Russian Federation, . The price varies from 39 to 853 rubles.
• "Metoprolol-Ratiopharm" (costs from 28 to 3150 rubles) from the German company "Ratiopharm".
• "Metoprolol Zentiva" Czech for 125 rubles.
• "Metoprolol-Teva" from the pharmaceutical company "Teva" from Israel. The cost of the drug ranges from 19 to 142 rubles.

Price fluctuations depend on the dosage of the drug (25, 50, 100 mg) and the number of tablets in the package.

Vasocardin

As for savings, Metoprolol can be purchased much cheaper. However, Vasocardin contains 20 more tablets. If long-term treatment is expected, it is more profitable to purchase this analogue. There are no significant differences in composition and, accordingly, contraindications.

According to research, Vasocardin begins to affect the body within 15 minutes after use. The effect lasts for six hours. After a month of therapy with Vasocardin, blood pressure becomes normal, chest pain and rapid painful heartbeat disappear, and shortness of breath ceases to torment.

A biochemical blood test done a month after starting to take the medicine shows a much better result than before. Vasocardin should be taken simultaneously with food, washed down with a large volume of water. The standard dosage is 500 to 100 mg every 24 hours. Sometimes it is allowed to increase it to 200 mg.

When taking Vasocardin, the following conditions should be taken into account:

• problems with the thyroid gland - you should drink 150-200 mg of Vasocardin per day. In this case, you need to divide this dosage into three or four times;
• cardiac arrhythmia, existing migraine or its threat, angina pectoris - 100-200 mg every day. In this case, it is worth dividing the reception into two times;
• arterial hypertension - 50-100 mg both morning and evening. It is not prohibited to increase the dose to 200 mg, but in this case it is necessary to obtain the approval of the attending physician;
• preventive measures regarding myocardial infarction - 100-200 mg twice a day.

It is recommended that if you have kidney or liver problems, consult your doctor about dosage.

special instructions

Special attention is required for patients suffering from:

• diabetes mellitus;
• metabolic acidosis (pathological increase in the amount of acid in the blood, leading to coma);
• bronchial asthma, chronic pulmonary obstruction, emphysema;
• peripheral vascular diseases - Raynaud's disease, intermittent claudication - the medicine is discontinued slowly to avoid withdrawal syndrome (worsening the severity of angina attacks);
• chronic failure of the liver and kidneys;
• myasthenia (pathologically rapid muscle fatigue);
• development of adrenal tumors;
• thyrotoxicosis;
• depressive states;
• psoriasis.

It's also important to remember:

• In case of heart failure, use is permitted after stabilization of the heart. For angina pectoris - with a stable heart rate at rest of at least 55 beats/min, and no more than 110 during exercise.
• Abrupt withdrawal of the drug in patients suffering from thyrotoxicosis is not allowed to avoid worsening symptoms.
• Before surgery, you must inform the anesthesiologist about Metoprolol therapy.
• In elderly patients, the dose is adjusted in case of increasing bradycardia (less than 50 beats/min), a sharp drop in pressure, AVB (atrioventricular block with cardiac arrhythmia), bronchospasm, and liver dysfunction. In case of severe pathologies, treatment is interrupted.
• In case of renal failure, constant monitoring of renal function is required.
• If neurological disorders or depression worsen, immediately discontinue Metoprolol.

At the beginning of treatment, patients are not recommended to drive vehicles or perform work that requires quick reactions.

Pathological types and causes of tachycardia

A pathological disturbance of heart rhythm can manifest itself in a state of complete rest on the part of the patient. The causes may be factors affecting the heart or other pathologies.

Common etiology:

• myocardial infarction;
• myocarditis;
• congenital or acquired heart defects;
• thyrotoxicosis;
• renal colic;
• blood loss in the acute phase (pre-shock).

The main types of pathological tachycardia are as follows:

• progressive;
• ciliary;

What is tachycardia in humans

• reciprocal;
• recurrent;
• sinoatrial;
• pacemaker

Composition of the drug and its release form

In what form is the drug Metoprolol sold? Reviews from patients say that you can find three types of this drug in the pharmacy. Let's look at the release forms and composition in more detail.

• Pills. They contain the active ingredient metoprolol tartrate (100, 50 and 25 milligrams). In addition, the medication also includes auxiliary components in the form of colloidal anhydrous silicon dioxide, microcrystalline cellulose, sodium carboxymethyl starch (type A) and magnesium stearate. The medicine is sold in 50, 10, 30, 20 or 40 tablets per package.
• Tablets with sustained release properties (“Metoprolol succinate”), coated. They contain similar active and excipients. In pharmacies this medicine can be found in 30, 20 or 10 tablets per package.
• Solution for intravenous injection in ampoules of 5 milliliters. The medicine goes on sale in cardboard packaging of 10 ampoules.

Features of pharmacokinetics

Metoprolol is a fat-soluble biologically active substance, and therefore is used in pharmaceuticals in the form of salts: tartrate, succinate and fumarate, which optimizes its rate of delivery to the bloodstream and solubility.

The standard release forms of metoprolol with immediate release (IR - Immediate Release) are represented by its rapidly soluble tartrate, the duration of the therapeutic effect of which is 12 hours. Thanks to the CR/XL ZOK (Controlled Release/Extended Release, Zero–Order–Kinetics) technology, a retard dosage form with a prolonged release of the active substance has been developed, which uses less soluble metoprolol succinate.

A tablet of such a drug consists of a multi-element system of compressed spherical granules of the active substance, enclosed in an ethylcellulose polymer membrane, which controls the release of the drug from them. In the stomach, the drug is broken down into granules that function as diffusion chambers, ensuring a stable absorption rate of metoprolol for 20 hours, resulting in its clinical effect lasting more than a day.

Special instructions for the use of the drug

Currently, you can purchase the drug Metoprolol at any pharmacy. No recipe is required. However, the patient taking the medication should be regularly monitored by the attending physician. This is especially true for those patients who have been diagnosed with diabetes or angina.

You should be aware that with increasing dosage (more than 200 mg per day), cardioselectivity decreases. In the presence of heart failure, therapy is started only after the compensation stage has been reached.

People who use contact lenses should take into account that during treatment with Metoprolol, the production of tear fluid decreases.

Sometimes this medication masks some manifestations of thyrotoxicosis. At the same time, abrupt withdrawal of the drug in patients with the mentioned disease is contraindicated, as this increases the symptoms.

If it is necessary to undergo surgery, the patient should be sure to notify the anesthesiologist about drug therapy.

During treatment with Metoprolol, you must wear appropriate clothing. This is due to the fact that the drug can cause allergic reactions on the skin due to exposure to sunlight.

It should also be said that the drug “Metoprolol” (including analogues of this drug) in elderly people can cause the appearance of increasing bradycardia, a pronounced decrease in blood pressure, and atrioventricular block. That is why such patients require special monitoring.

In addition, during treatment with this drug, you should refrain from driving vehicles and stop engaging in hazardous activities that require increased concentration and speed of psychomotor reactions. It is also recommended to avoid ethanol intake.

Application and dosage

• Hypertension: 0.05-0.1 g once a day.
• Angina pectoris: 0.1-0.2 g once a day.
• Compensated CHF II FC: start with 0.025 g once a day for the first 2 weeks and then double the dose every six months; maintenance dose - 0.2 g once a day.
• Compensated CHF III-IV FC: initial dose - 12.5 mg once a day for the first 2 weeks; in patients with satisfactory tolerability of the drug, the dose can be doubled every six months to the maximum of 0.2 g once a day.
• Arrhythmias: 0.1-0.2 g once a day.
• Secondary prevention in the post-infarction period: 0.2 g once a day.
• Functional tachycardia: 0.1-0.2 g once a day.
• Prevention of migraine paroxysms: 0.1-0.2 g once a day.

Metoprolol succinate is used daily, the dosage frequency is once a day. Eating does not affect its bioavailability. The doctor selects the dose of the medicine, as the heart rate should be monitored to avoid bradycardia.

Indications for use: what helps

Metoprolol - what is it prescribed for? Doctors recommend this medicine for various diseases of the cardiovascular system, for example, it is prescribed for:

• Neuroleptic akathesia.
• Hypertension.
• To prevent heart attack.
• For migraines.
• Angina pectoris.
• Various heart rhythm disturbances.
• In case of cardiovascular failure, to reduce the likelihood of death of the patient.
• With ischemia.
• Mitral valve prolapse.
• For thyrotoxicosis (used in combination with other medications).
• Idiopathic cardiomyopathy and other heart diseases.

What do Metoprolol tablets and ampoules help with?

Tablets and solution in ampoules Metoprolol helps to improve the health of patients with various cardiac disorders, for example:

• The medicine helps lower blood pressure.
• Helps normalize heart rate during tachycardia.
• Treats ischemic disease.
• Helps prevent a heart attack and reduce the likelihood of another heart attack.
• Helps fight migraines
• Treats unstable angina pectoris.

Positive effect on the body

Blood pressure levels will finally stabilize by the end of the second week of therapy with this medication.

It is important to note that Anaprilin can also prevent the appearance of severe headaches of so-called vascular origin. This is due to minimizing the severity of dilatation of the largest arteries due to beta-blockade of vascular receptors.

While taking the medication, there is a decrease in the likelihood of the occurrence of such a phenomenon as trembling of the upper and lower extremities. It also increases the atherogenic properties of blood.

Compound

The active component of this product is propranolol hydrochloride. One tablet contains 10 or 40 mg of this substance. But the auxiliary components are refined sugar, starch (potato), calcium stearate and talc.

Tablets Anaprilin 40 mg

Indications for use

It is prescribed for such ailments and conditions of the body as:

• cardiac ischemia;
• high blood pressure;
• pain in the sternum;
• heart rhythm disturbances;
• sinus tachycardia;
• supraventricular and atrial fibrillation;
• myocardial infarction;
• mitral valve prolapse;
• trembling of limbs;
• cardiopsychoneurosis;
• migraine.

As a rule, this drug is used as part of combination therapy.

Available analogues of this product

So, what can replace Anaprilin? The most popular substitutes for Anaprilin are the following: Vero-Anaprilin, Gemangiol, Inderal, Inderal LA, Obzidan, Propranobene, Propranolol, Propranolol Nycomed, and Propranolol hydrochloride.

Tablets Obzidan 40 mg

Some of these drugs are not only more affordable, but also extremely effective in treating high blood pressure and other diseases of the cardiovascular system.

The fact that they are cheaper does not mean their effectiveness is low. On the contrary, they have the best characteristics and are able to relieve the patient of any discomfort in the shortest possible time.

Russian analogues

Among the most popular domestically produced drug substitutes are the following:

1. Sotalol Canon

   . This drug is produced exclusively in tablets. Of course, this is a more expensive substitute from a Russian manufacturer. It is capable of exerting a strong antiarrhythmic effect, but, nevertheless, differs from the drug in question in the active component. In this remedy, sotalol acts as it. The approximate cost of this drug varies from 70 to 130 rubles;
2. Vero-Anaprilin . It contains a similar active ingredient and is available in the same dosage. As you know, it is not much different from Anaprilin. As for the indications for use and contraindications, they are also almost the same. Its cost is approximately 20 rubles.

Foreign analogues

Of course, there are much more of these drugs, since they have a more pronounced effect, a minimum number of contraindications and side effects.

The following can be considered foreign analogues:

1. Sotahexal

   . It is produced in tablets. The manufacturing country is Germany. Of course, this medicine is much more expensive than domestic Anaprilin, and besides, for the high cost you will receive fewer tablets. Only 20 instead of 50, as in the product under consideration. This means that with regular use you will have to spend large sums to constantly purchase new blisters. The main indications for use are: symptomatic and chronic heart rhythm disorders. The average price of this medication varies from 80 to 140 rubles;
2. Propranolol . The country that produces this drug is Germany. As the name suggests, its active substance is the component of the same name. It is prescribed for high blood pressure, angina pectoris and myocardial infarction. It has a high degree of effectiveness, for which cardiologists constantly prescribe it to their patients. The average cost is about 100 rubles;
3. Propranobene. Available in capsules. As you know, the manufacturer is Germany. It is also prescribed for high blood pressure, tachycardia, and other dangerous diseases of the cardiovascular system. The cost of this medication is also more than 100 rubles. However, it is worth noting that it is absolutely safe for the patient’s health, unlike cheaper analogues. This is due to the complete absence of undesirable impurities in its composition.

Comparison with Metoprolol

What is better - Anaprilin or Metoprolol? Metoprolol is the medicine most often prescribed for high blood pressure and other serious conditions caused by problems with the cardiovascular system.

Metoprolol tablets

According to its classification, it is classified as a beta blocker. This medication minimizes the effect of adrenaline and other stimulating hormones on the human heart. Thanks to this, the patient’s pulse becomes a little slower, blood pressure returns to normal, and the load on the heart muscle is significantly reduced.

Pharmacological action of Metoprolol Succinate

Cardioselective beta-blocker without intrinsic sympathomimetic activity. The drug has a hypotensive, antianginal and antiarrhythmic effect. Reduces the automaticity of the sinus node, lowers heart rate, leads to a slowdown of AV conduction and a decrease in contractility and excitability of the heart muscle. In addition, taking the drug reduces cardiac output, reduces myocardial oxygen demand, and also suppresses the effect of catecholamines on the heart during physical and emotional stress.

Causes a hypotensive effect, which normalizes by the end of 2 weeks of regular use. In case of exertional angina, the effect of metoprolol is manifested by a decrease in the frequency and severity of attacks. Restores heart rhythm during supraventricular tachycardia and atrial fibrillation.

In case of myocardial infarction, the drug helps limit the area of ​​cardiac ischemia.

In case of myocardial infarction, it helps limit the area of ​​cardiac ischemia and reduces the risk of fatal arrhythmias, and reduces the chance of relapses after myocardial infarction. When used in moderate therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries than non-selective drugs from this group.

Metocard

It is considered the best imported analogue, which is inexpensive. At the same time, it also helps with myocardial infarction and problems with heart rhythm.

Metocard tablets

It is listed as a means of providing effective prevention of migraines. Metocard is useful for use in complex therapy in the fight against thyroid hyperfunction.

You need to take the medicine with plenty of liquid at the same time as food or immediately after taking it. You should not chew the tablets. But dividing in half to measure the required dosage and ease of use is quite possible.

The nuances when determining the amount of medicine are as follows:

• for the prevention of migraine, angina pectoris, arrhythmia - you should drink 100-200 mg of Metocard in the morning and evening.
• Prevention of myocardial infarction involves taking the medicine twice a day, 200 mg.
• tachycardia - in the mornings and evenings you should drink about 100 mg of Metocard.
• for arterial hypertension, you need to take 50 or 100 mg of the medicine in one or two doses a day. This dose is called the initial dose. It can be increased to 200 mg if necessary. However, you cannot drink more at one time.

In the absence of the desired result, it is recommended to combine Metocard with other drugs to normalize blood pressure levels.

Release form, composition and packaging

The main active component of the drug is the chemical substance of the same name - metoprolol. 1 tablet can contain from 25 to 100 mg of metoprolol. The medicine also contains the following additional ingredients:

• methylcellulose;
• microcrystalline cellulose;
• magnesium stearate;
• hypromellose;
• glycerol;
• corn starch;
• titanium dioxide

The main active component of the drug is the chemical substance of the same name - metoprolol.

The drug is available in 3 forms:

1. Pills. Depending on the dosage, they may contain 25 mg, 50 or 100 mg of the active ingredient. Small tablets have a white-grayish color. 1 package can contain 10, 20, 30, 40 and 50 pieces.
2. Tablets coated with a special coating. The protective shell allows you to slow down the action of the medication, but this does not affect the effect of taking it. Such tablets are sold in 10, 20 and 30 pieces in a blister.
3. Solution for intravenous injection. Available in ampoules of 5 ml. The drug is sold in a cardboard package containing 10 ampoules.

Atenolol-AKOS

Another budget analogue of Metoprolol in tablet form. It copes quite effectively with lowering blood pressure, relieves chest pain, and brings the heart rate to normal levels.

Atenolol tablets

It has the same contraindications as in the case of Metoprolol. By the way, a similar list is also relevant in the case of other drug analogues. IN

Unlike the previous case, this drug should be taken before meals. You should prepare a large amount of water to wash down the medicine. It's not worth chewing.

The dosage should be prescribed depending on the following nuances:

• for arterial hypertension, heart rhythm disturbances, chest pain - 50 g once a day. If necessary, you can increase the amount of medication taken at a time to 100 mg. On average, to achieve an effect, it is worth treatment for at least a week or two. If even after this period Atenolol-AKOS does not produce results, it is better not to extend the period of use, but to use other drugs;
• with the same diagnosis, you can drink 25 mg of the medicine for each day of the course as support. Before each such appointment, it is advisable to find out your blood pressure readings in order to calculate the further course. Depending on it, it is worth adjusting the dosage, but the maximum daily volume of medication taken should not exceed 200 mg;
• if there are problems with the kidneys, the dosage should be set as follows - no more than 50 mg. The specialist must determine how often to carry out this dosage - every day or every other day. It all depends on the individual functioning of the kidneys.

If there is a need to stop using Atenolol-AKOS, it is recommended to do this gradually, taking 0.5 of the prescribed dose every three to four days.

Pharmacokinetics absorption, metabolism and excretion of the drug

We will talk about the indications for use of the drug and the analogs available for the drug “Metoprolol” below, and now let’s talk about the pharmacokinetic features.

This product is absorbed very quickly and almost completely (about 95%). Maximum plasma concentrations are usually achieved 50-110 minutes after oral administration.

When first used, the bioavailability of the drug is 50%. When repeated, it increases to 70%. By the way, eating food increases the bioavailability of the drug by 20-40%. It also increases if the patient has cirrhosis of the liver. The average binding to proteins is 10%.

The mentioned drug penetrates well through the placental and blood-brain barriers. It is also excreted in small quantities into breast milk.

The drug is metabolized in the liver. Moreover, the metabolites do not have pharmacological activity. About 5% of the drug is excreted unchanged by the kidneys. Therapy for a patient with reduced renal function does not require a reduction or other dose adjustment of the drug. However, abnormal liver function may slow down the metabolism of the drug. In this case, the dosage should be reduced.

Video on the topic

Metoprolol or Bisoprolol - which is better to take for pressure surges? About the pros and cons of these and other adrenergic blockers in the video:

It is extremely important to treat diseases related to the heart and blood vessels with special attention. Ignoring them can even lead to death. Therefore, you should always have Metoprolol and its analogues on hand, which can help at any moment.

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Dosage regimen

Doctors must use an individual approach to prescribing the drug, which depends on the disease. According to reviews of the instructions for Metoprolol, patients would like a more detailed dosage regimen for this drug.

For hypertension of the first and second degree (systolic pressure - up to 160 mm Hg), you should start with 25-50 mg of the drug twice a day with an interval of 12 hours. The dosage can be increased to 100 mg twice (total 200 mg) or use an additional agent to reduce blood pressure.

For the treatment of angina pectoris, take 25-50 mg up to three times a day under control of the frequency of ventricular contraction. The dose may be increased to 200 mg per day, or an additional drug may be added to treat angina.

To prevent a recurrent heart attack, up to one hundred milligrams are prescribed per day in two doses.

For arrhythmic pathologies, the drug is indicated in a dose of 25-50 mg up to three times a day. If there is insufficient effectiveness, it is possible to increase the dose to 200 mg per day or add another antiarrhythmic drug.

For functional tachycardia, take from 50 to 100 mg per day.

To prevent migraine attacks, take 50 mg twice a day. It is possible to increase the dose to 100 mg twice a day.

Patients suffering from tachycardia, with an increased level of thyroid hormones in the blood, are prescribed 50 mg up to four times a day under the control of the frequency of contractions of the heart muscle. Three days after treatment, the dosage can be increased to 100 mg 3-4 times a day, which will be equal to the maximum daily dose of Metoprolol (400 mg per day).

The instructions for Metoprolol stipulate that the medication should be taken during or after a meal with a sufficient amount of water. Patients should be taught to count the minute number of heartbeats, which should not be less than 60 beats. The duration of treatment is individual and should be monitored by a doctor. The withdrawal of the drug should be carried out very slowly to avoid a jump in blood pressure.

Medicine "Metoprolol": instructions for use

Oral form

The tablets are taken orally with water. The standard dosage is 100 mg per day. The medicine is used in several approaches. If necessary, the volume of the drug is doubled. The highest daily amount of medication is 400 mg.

Instructions for using injections

Metoprolol solution is injected into a vein at a dosage of 2-5 mg. The maximum single dose reaches 20 mg. If there is no therapeutic effect, the injections are performed again after 5 minutes. The withdrawal of medication is carried out gradually under medical supervision.

Dosage of the drug "Metoprolol Succinate" in the treatment of diseases

For the treatment of supraventricular tachycardia, angina pectoris, hypertension, extrasystole, 50-100 mg of the drug per day is prescribed in the initial stages. For myocardial infarction, 200 mg per day should be taken as maintenance treatment. In case of chronic heart failure, the dosage is set separately for each patient. The duration of taking Metoprolol Succinate takes about 3 months.

Precautionary measures

Contraindications to taking the drug:

• bradycardia (slow heart rate);
• acute heart failure,
• hypotension (low blood pressure);
• metabolic acidosis;
• cardiogenic shock;
• peripheral circulatory disorders;
• sick sinus syndrome.

Metoprolol should be avoided by patients under 18 years of age, as well as by patients with individual intolerance to the main or auxiliary active ingredients in the drug.

An overdose (incorrectly chosen dosage regimen) of the drug can cause the following side effects:

delayed reactions (motor, mental), headaches, general weakness, fatigue, decreased performance, insomnia, memory problems, inability to concentrate on a specific object, unreasonable anxiety, myalgia, convulsions, insomnia (from the nervous system); blurred vision, increased dryness of the eye mucosa, conjunctivitis, decreased amount of tear fluid produced; abnormal drop in blood pressure, dizziness, fainting, cardialgia, conduction disturbances, vasospasm, circulatory problems (from the cardiovascular system); changes in taste, liver dysfunction (“signals” of the gastrointestinal tract); photodermatosis, psoriatic skin rashes, alopecia (baldness), hyperhidrosis (increased sweating) - dermatological consequences of improper use of Metoprolol; swelling of the mucous membrane, nasal congestion, shortness of breath (problems associated with malfunction of the respiratory system); a sharp drop in blood sugar levels in insulin-dependent diabetics or, conversely, a jump in this indicator in patients with type 2 diabetes, symptoms of hypothyroidism (hormonal disorders); Long-term use of Metoprolol in rare cases leads to the appearance of an itchy allergic rash on the skin, an increase in the level of platelets in the blood, and agranulocytosis.

If an overdose of Metoprolol occurs, patients are given:

1. Gastric lavage.
2. Symptomatic drug therapy - atropine sulfate is administered intravenously, Dobutamine infusion (with a decrease in cardiac muscle contractility); adrenaline, norepinephrine (abnormal decrease in blood pressure), for convulsions - Diazepam, jet intravenous injection of Eufillin helps cope with bronchospasm.

Metoprolol should be treated with special caution in patients suffering from diabetes mellitus. So, in patients who take glucose-lowering drugs or inject insulin, this medicine can mask the symptoms of hypoglycemia (a pathological condition of the body associated with a sharp decrease in blood glucose levels)

The active components present in Metoprolol affect the level of glucose in the blood and also “imprint” on the synthesis of liver enzymes.

Renal and liver failure are indications for reducing the dose of Metoprolol (the bioavailability of the drug with these pathological changes in the patient’s body increases significantly).

Patients with coronary artery disease after discontinuation of the drug should be under the supervision of a cardiologist.

Side effects:

Increased fatigue, headache, dizziness, decreased concentration, paresthesia, convulsions, depression, decreased attention, drowsiness, insomnia, nightmares, confusion, memory impairment, hallucinations, sexual dysfunction, visual impairment, decreased secretion of the lacrimal gland, conjunctivitis, noise in ears, hearing loss. Sinus bradycardia, arterial hypotension, orthostatic hypotension, decreased myocardial contractility, increased symptoms of heart failure, first degree AV block, disturbances in cardiac conduction and rhythm, cardialgia. In patients with Raynaud's syndrome, increased peripheral circulatory disorders, nausea, vomiting, abdominal pain, dry mouth, constipation, diarrhea, impaired liver function, abnormal liver enzymes, changes in the sense of taste, rash, psoriasis-like skin reactions, skin hyperemia, photodermatosis, sweating, alopecia, exacerbation of psoriasis, nasal congestion, bronchospasm, shortness of breath. Endocrine system - hyperglycemia (in patients with non-insulin-dependent diabetes), hypoglycemia (in patients taking insulin), urticaria, itching, rash, thrombocytopenia, arthralgia, myalgia. Sexual dysfunction.

Use of medication during pregnancy and lactation

Pregnancy is not an absolute contraindication. Metoprolol can be prescribed when the positive effect of the drug prevails over the possible negative consequences for the unborn child. The drug can harm the fetus if it passes through the placenta, as it impairs its blood supply. This can lead to growth and development delays, premature birth or fetal death.

Three days before the date of birth, the use of the medication must be stopped, as there is a risk of bradycardia, a drop in blood pressure and sugar, an increase in bilirubin, as well as cessation of respiratory activity in the child. Newborns whose mothers took Metoprolol during pregnancy should be closely monitored for three days after birth.

The drug can pass into breast milk, so when using this drug you should refrain from feeding or replace the drug. If the mother continues to breastfeed while taking this medication, the baby should be monitored for the development of bradycardia, decreased blood pressure, and decreased blood sugar.

Membrane stabilizing agents

There is often a need to take Metoprolol together with other drugs, since the diseases for which these tablets are indicated are usually accompanied by other pathologies. Therefore, it is important for the patient to know which medications Metoprolol is compatible with.

• It is strictly not recommended to take it simultaneously with MAO inhibitors and antihypertensive drugs, otherwise the decrease in blood pressure may be too strong. There should be a break of at least 14 days between doses. For the same reason, it is dangerous to take the drug together with Nifepidin.
• The simultaneous use of Metoprolol and Verapamil can lead to cardiac arrest.
• Metoprolol reduces the effectiveness of hypoglycemic drugs. At the same time, it can cause the development of hypoglycemia when taking insulin and intensify its manifestations - tachycardia, increased sweating, increased blood pressure.
• Take with caution together with ethanol, as together they increase the inhibitory effect on the central nervous system.

In any case, it is necessary to study the instructions for use before starting to take the drug to make sure that there are no contraindications, and also that the patient is not taking medications that are incompatible with these tablets.

Membrane stabilizers are used relatively rarely. This group of drugs affects cellular pumps, namely the concentration of sodium ions and sodium-potassium channels. A group of drugs actively affects electrolytes and prolongs the repolarization phase. The drugs reduce the activity of Purkinje fibers, they cannot conduct impulses, and also return the sending of impulses back.

Treatment of tachycardia should be carried out in a complex manner. It is necessary to select drugs with better tolerability for the patient, as well as determine the etiological factor and, if possible, eliminate it. Treatment of arrhythmia can occur in courses or be taken for life, so constant consultation with a specialist and preventive examinations every two to three months are important.

We suggest you read: What will help with low blood pressure

Originally posted 2018-03-16 11:16:17.

Contraindications to the use of Metoprolol

The drug should not be prescribed in case of previously known cases of individual sensitivity to this group of substances, metoprolol tartrate itself or auxiliary components of the drug, including lactase deficiency.

Cardiac conduction disorders in the form of second and third degree atrioventricular block do not allow the use of Metoprolol in treatment. Sick sinus syndrome and bradycardia with a slow heart rate of less than 50 beats per minute are also contraindications.

Decompensated heart failure, accompanied by pulmonary edema, decreased blood pressure and impaired peripheral circulation, makes it impossible to take this medication.

Prinzmetal's angina is a contraindication to the use of Metoprolol due to the possible prolongation of its attacks.

It is undesirable to take the drug if you have a systolic blood pressure below 90 mmHg. Art.

Metabolic acidosis, accompanied by a decrease in blood pH, is a contraindication to taking the medication.

Severe bronchial asthma and obstructive bronchitis are conditions in which Metoprolol is contraindicated.

Do not take together with MAO inhibitors (except MAO-B).

Peripheral circulatory disorders complicated by gangrenous lesions or the threat of its development.

It has not been studied in persons under 18 years of age, so the medicine is not prescribed to children.

Contraindicated in cases of established or suspected acute stage of infarction with severe bradycardia (up to 45 beats per minute), low blood pressure and prolongation of the P-Q interval.

Cardioselective beta1-blockers are a serious group of drugs widely used in medical practice. Therefore, contraindications must be taken into account before prescribing the drug.

Contraindications:

2nd and 3rd degree AV block, unstable or decompensated HF (pulmonary edema, hypoperfusion or hypotension), as well as in patients with long-term or intermittent inotropic treatment with β-receptor agonists, clinically significant sinus bradycardia, CVS, cardiogenic shock, severe peripheral impairment arterial circulation in patients with suspected o. MI, if heart rate is below 55 beats/min, PQ interval> 0.24 sec. or systolic blood pressure less than 100 mm. Hg Art.; patients who have hypersensitivity to any of the components of the drug or to other beta-blockers.

The daily dose (DDD) was determined: orally - 0.15 g, parenterally - 0.15 g.

Pharmacological action of the drug

Metoprolol has the ability to act on beta1-adrenergic receptors, blocking them, which leads to a series of changes in the functioning of organs and blood vessels. The drug substance metoprolol tartrate helps lower blood pressure, dilates the blood vessels of the heart, providing an antianginal effect, and has an antiarrhythmic effect.

The drug slows the heart rate and the force of heart contraction, causing the heart muscle to need less oxygen. Consequently, in patients with angina, the ability to perform heavy workloads increases and the frequency of angina attacks decreases.

During stressful situations and physical activity, the amount of adrenal hormones in people’s blood increases, which leads to increased heart rate and increased blood pressure, and Metoprolol (contraindications are described below) reduces this effect on the cardiovascular system. In case of rhythm disturbances and tachycardia accompanying hyperthyroidism, the drug brings the frequency back to normal.

The effect on the sinus node leads to a restoration of rhythm and a slowdown in impulse conduction between the atria and ventricles. Acting on the blood vessels of the brain, it fights headaches.

The drug is able to some extent influence carbohydrate and fat metabolism, increasing the number of triglycerides in the bloodstream, reducing sugar, fatty acids and high-density lipoproteins.

Bisoprolol or Metoprolol: which is better, reviews, difference

What is better and more effective - Metoprolol or Bisoprolol? How are they different from each other? Bisoprolol and Metoprolol - the same thing or not? In this article we will try to compare and name the main difference between these representatives of the group of selective beta-1 adrenergic blockers. The action of the latter is aimed at selective blocking of β1-adrenergic receptors.

These receptors are localized in the heart. Stimulation leads to an increase in both the frequency and strength of contractions of the organ, increases the need for oxygen, and raises blood pressure. β1-adrenergic receptors are also localized in the kidneys, where they are part of the juxtaglomerular apparatus, which is part of the endocrine system of organs.

To find out which is better: Metoprolol or Bisoprolol, studies have been conducted repeatedly. Experts planned to understand which drug is more effective. A comparison of medications showed that there is a difference between the medications, but it is not considered significant.

Comparing Bisoprolol and Metoprolol, we note that the difference lies in the half-life. The first has an action time of up to 12 hours, while the second has only 4 hours. As a result, Metoprolol has to be taken up to 3 times a day, which cannot be called convenient.

Review of Metoprolol and Betaloc ZOK

Metoprolol is a drug classified as a selective β-adrenergic receptor blocker. The main active ingredient is metoprolol tartrate. Each tablet may contain 100, 50 or 25 mg of this medication.

The tablets are round with a flat surface, white or white with a cream tint, and also have two intersecting perpendicular stripes for dividing. Additional components included: lactose, cellulose, monohydrate, talc, calcium stearate, povidone and crospovidone.

pharmachologic effect

Betaloc ZOK is considered a selective β-adrenergic receptor blocker, the active component of which is metoprolol succinate, available in tablets, each of which can contain 95, 47.5 or 23.75 mg of the latter, which corresponds to 100, 50 and 25 mg of metoprolol tartrate.

Tablets are convex on both sides, white or almost white, coated, have a stripe on both sides and an engraving with the abbreviation of the name. Additional components: hypromellose, paraffin, macrogol, ethylcellulose, sodium stearyl fumarate, silicon dioxide, titanium dioxide.

Antiarrhythmic drugs

Treatment of tachycardia with normal blood pressure requires a combination of drugs. You cannot purchase them yourself in pharmacies. Some of the medications slightly reduce blood pressure, but the dosage to reduce blood pressure during arrhythmia is not critical. The combination is selected empirically and adjusted during treatment. The patient is also prescribed a gentle physical regimen.

Beta blockers: side effects and contraindications in the treatment of tachycardia

Most often used:

• beta blockers;
• calcium channel blockers;
• membrane stabilizers;
• potassium blockers;
• microelements to support the myocardium.

Effective drugs that normalize heart rate belong to such pharmacological groups as:

• Beta blockers. Beta blockers help slow the heart rate, they reduce the ejection fraction, as well as the myocardial oxygen demand. Medicines must be included in the treatment plan for tachyarrhythmia, and the effect on blood pressure at low dosages is insignificant. Cardioselective drugs include Nebivalol, Metoprolol, Carvedilol, Bisoprolol, Atenolol.
• Calcium channel inhibitors. Calcium channel antagonists have a good level of tropism for cardiac tissue. By unloading the heart from calcium ions, you can obtain the effect of a slight relaxation of the heart muscle, and then reduce the myocardial need for oxygen and stop an attack of tachycardia. The drugs include Verapamil, Nifedipine, Amlodipine, Diltiazem, Cinnarizine.
• Potassium blockers. During the blocking of potassium ions, a decrease in the activity of electromechanical processes is observed. Drugs from this group can be taken as treatment and prevention of attacks. During use, you need to monitor your thyroxine level. The drugs include Amiodarone and Cordarone.

Tags: pressure, metoprolol, normal, tachycardia

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Drug interactions

If you combine Metoprolol Ratiopharm with other types of blood pressure lowering drugs (for example, diuretics), you can get hypotension and bradycardia.
Metoprolol is absorbed faster if taken with barbiturates. Its combined use with NSAIDs may reduce the effectiveness of the active substance.

Metoprolol is a substance that can enhance the effect of hypoglycemic drugs. However, it is undesirable to take it simultaneously with opioid analgesics, as this may cause cardiac failure.

It is dangerous to administer verapamil during treatment with metoprolol, as the combination can cause cardiac arrest. In this case, the maximum concentration of active substances in the blood is achieved, which can provoke hypotension, heart failure and reduce the heart rate.

Inhalation anesthesia requires discontinuation of Metoprolol, since otherwise myocardial activity is dangerously inhibited. Arterial hypotension also develops due to the interaction of metoprolol and amiodarone. Dextropropoxyphene increases the bioavailability of the active substance.

Metoprolol Ratiopharm is a drug for normalizing blood pressure. Can also be used for the treatment of other diseases of the cardiovascular system according to indications. The drug has many contraindications; For its maximum effectiveness and safety, you need to choose the right dosage - only your doctor can do this correctly.

Reviews

When treating with the drug "Metoprolol", you can hear a wide variety of reviews, because doctors often prescribe this drug to their patients for the treatment of hypertension and various heart pathologies.

Since it is quite difficult to cope with such serious illnesses in one course of treatment, this medication, after choosing the right dose, is taken for the rest of your life. If a person sees positive dynamics in the stabilization of blood pressure and heart rate, he will continue to be treated with it. Doctors hear positive feedback from such patients.

But this doesn't always happen. The drug has a number of side effects, the manifestation of which may limit or even force you to stop taking it. For example, manifestations of insomnia or depression during treatment can be caused both by taking the drug and by the person’s psycho-emotional state and unhealthy environment.

Many patients ask their doctor questions about the compatibility of a particular medication they are already taking. Sometimes it turns out that combining drugs is undesirable or you need to reduce the dosage of one of the medications. For example, the dose of drugs containing alcohol should be reduced to prevent an increase in ethanol levels in the blood.

If these features are not taken into account, there will be many more undesirable consequences, which means that negative statements about its ineffectiveness simply cannot be avoided. For patients starting to take the drug Metoprolol, reviews, both positive and negative, will help them avoid mistakes, correctly understand the treatment regimen and set themselves up for a speedy recovery.

This drug, as a drug that lowers blood pressure, is applicable in complex therapy; alone it is less effective. Its disadvantage is a pronounced decrease in heart rate and the inability to take it for people suffering from respiratory diseases or high blood sugar levels. High doses of this drug are less selective for the heart muscle, which is also undesirable. In addition, the substance metoprolol cannot be used to treat heart disease if there is low blood pressure. This remedy should not be taken without the advice of a doctor; if it helps some people, this does not mean that it is suitable for everyone without restrictions.

Complications from taking

Side effects may occur at different stages of Metoprolol therapy. Thus, at the beginning of treatment the following undesirable reactions were observed:

• weakness,
• fast fatiguability,
• dizziness,
• headache,
• muscle cramps,
• chills.

Less common manifestations such as decreased heart rate, hypotension, and heart failure with swelling of the extremities were recorded.

From the organs of vision: conjunctivitis, smell - rhinitis.

Dyspeptic disorders were manifested by nausea, vomiting, and constipation.

From the nervous system: tendency to depression, sleep disturbances, dry mouth.

A decrease in sugar levels in diabetes mellitus as a manifestation of endocrine system disorders.

Rarely, patients with a predisposition to allergic reactions experienced bronchial asthma, dermatitis, and itching.

Pharmacology

It predominantly blocks beta1-adrenergic receptors of the heart and does not have internal sympathomimetic and membrane-stabilizing activity. Reduces cardiac output and SBP, slows heart rate, weakens the stimulating effect of catecholamines on the myocardium during physical activity 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, ultimately, a decrease in peripheral sympathetic influences. The hypotensive effect develops quickly (sBP decreases after 15 minutes, maximum after 2 hours) and lasts for 6 hours;

when taking metoprolol succinate, the clinical effect of beta1-adrenergic receptor blockade lasts 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.

Reduces the frequency and severity of attacks of coronary artery disease, the mortality rate in patients with diagnosed myocardial infarction, and increases exercise tolerance. Metoprolol succinate reduces the risk of death (including sudden death), recurrent infarction (including in patients with diabetes) 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, inhibiting automatism and lengthening the refractory period. Has a moderate negative inotropic effect.

Cardioselectivity is maintained when using daily doses not exceeding 200 mg. Due to the selective effect on beta1-adrenergic receptors, the risk of bronchospasm is theoretically reduced (in patients with bronchial asthma, pulmonary vital function is less reduced), hypoglycemia and peripheral vasoconstriction.

In experiments on dogs (up to 105 mg/kg/day, for 1 year), rats (up to 800 mg/kg/day, for 2 years) and mice (up to 750 mg/kg/day, for 21 months) No signs of carcinogenicity were found, but histological changes such as liver cell hyperplasia and induration of lung tissue by macrophages were detected.

When administered to albino mice in doses up to 750 mg/kg/day for 21 months, it increased the incidence of benign pulmonary adenomas in females, but when the experiment was repeated, an increase in the incidence of any tumors was not observed. Results of the test for dominant lethal mutations in mice, the study of chromosomes of somatic cells, the test for abnormalities of the nuclei of somatic cells in interphase, etc.

indicated the absence of mutagenic properties. In rats receiving doses 55.5 times higher than the maximum daily dose for humans (450 mg), there was no effect on fertility, increased rates of post-implantation death and decreased the survival of newborn animals (no signs of teratogenicity).

Metoprolol tartrate is quickly and almost completely (95%) absorbed when taken orally and undergoes intensive first-pass metabolism. Bioavailability is about 50% upon first use and increases to 70% upon repeated use. About 12% binds to blood plasma albumin. It is quickly distributed in tissues, penetrates the BBB (the level in the central nervous system is 78% of the plasma concentration), the placental barrier, and breast milk (concentrations exceed plasma concentrations).

Volume of distribution - 5.5 l/kg. Cmax is reached 1–2 hours after administration, blood levels vary significantly. T1/2 - from 3 to 7 hours. Biotransformed in the liver, with the formation of two active metabolites. Excreted primarily by the kidneys in the form of metabolites, Cl - 1 l/min. When taken orally, less than 5% is excreted unchanged in the urine, when administered intravenously - about 10%.

https://www.youtube.com/watch?v=rdyDoCe2LOY

If renal function is impaired, bioavailability does not change, but the rate of excretion of metabolites may decrease. In patients with liver cirrhosis, metabolism and overall clearance slow down (no dosage adjustment is required). It is not removed by hemodialysis. With intravenous infusion of metoprolol tartrate over 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, the Cmax of metoprolol succinate is 1/4–1/2 the Cmax of metoprolol tartrate, but lasts longer. Bioavailability in 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.

Is it possible for pregnant women to take Metoprolol?

The drug has the ability to be quickly absorbed into the body. Half of it is eliminated from the blood within three to five hours. The medication can affect the number of heartbeats and blood pressure for approximately 10-12 hours.

Metabolic processes take place in the liver and are excreted through the kidneys, usually as inactive metabolic products. The drug can cross the placental barrier and enter breast milk.

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According to reviews, “Metoprolol” affects the fetus during pregnancy, so it can only be prescribed in special situations when its pharmacological effect will be slightly higher than the likely risk to the child’s body.

In addition, if a woman is breastfeeding, she must stop breastfeeding and switch the baby to formula while using the medicine.

According to reviews, Metoprolol during pregnancy at 39 weeks should be stopped no later than 2 days before the expected birth. Using the medicine during lactation does not require stopping breastfeeding. It is only necessary to monitor the child’s condition to exclude the negative effects of the medicine on the baby.

Metoprolol: side effects

Everything is standard: weakness, lethargy, fainting, decreased blood pressure, reluctance to get out from under the blanket, etc. Plus, in people prone to depression, it can come out and make itself known loudly. So if you suddenly feel very sad while taking the drug, it is better to give it up.

Weakness and low blood pressure go away quite quickly - within a week. Then you don’t feel the drug at all. I did not have nausea or other digestive disorders; in this regard, I tolerate metoprolol well.

But in vain I hoped to get rid of sweating... Yes, it is less, it’s not on anapriline, well, now it’s generally winter, and therefore it’s difficult to judge what will happen in the summer heat. In general, when I move, I continue to sweat.

How does the drug work?

Once in the blood, the active substance metoprolol acts on beta-1 adrenergic receptors, which are located in the heart muscle, which indicates the selectivity of this compound. The receptors are blocked from the effects of the hormone adrenaline, which increases the frequency and strength of contractions of the heart muscle. It is this mechanism that “unloads” the myocardial muscle: heart contractions occur at large intervals and become less strong, and blood pressure normalizes.

It has been proven that selective blockers have fewer side effects than non-selective substances and are easier to treat concomitant diseases.

Under the influence of metoprolol, a reduction in automaticity in the sinus node is observed, atrioventricular conduction time slows down, the function of contractility and excitability of the myocardial muscle decreases, the volume of cardiac output and the oxygen needs of the heart decrease. When an infarction of the heart muscle develops, the drug limits the area with impaired blood supply, reducing the likelihood of developing an unpreventable arrhythmia and a recurrent infarction.

The average therapeutic dose affects to a lesser extent, compared with non-selective beta-blockers, the functioning of pancreatic cells, skeletal muscles, smooth muscles in the bronchi, uterus and peripheral arteries.

The drug "Metoprolol" is a hypotensive, antianginal and antiarrhythmic agent. It inhibits the stimulating effect of catecholamine substances on the heart muscle during physical activity and an excited psycho-emotional state.

Mechanism of action

The drug reduces the frequency of heart contractions, slows down the occurrence and conduction of electrical impulses, and the heart contracts less intensely. As a result, pressure and myocardial oxygen demand decrease, which plays a key role in the treatment of not only arterial hypertension, but also angina pectoris and coronary heart disease.

The use of metoprolol for myocardial infarction reduces the area of ​​necrosis and prevents the spread of the process . The risk of death and arrhythmias is significantly reduced.

Distribution in the body

The drug is taken orally and is absorbed in the gastrointestinal tract. The effect is achieved quickly; after 20 minutes, systolic pressure begins to decrease, diastolic pressure returns to normal a little later. Sufficient concentration in the body is maintained for 10-11 hours. The biologically active substances that are included in the composition are metabolized in the liver and excreted by the kidneys. Metoprolol ratiopharm penetrates the blood-brain barrier, exerting a central hypotensive effect. Also, the components of the drug are detected in breast milk, therefore, during breastfeeding, the drug should be discontinued or replaced with another.

Overdose

If the drug is abused, the following may occur:

• severe bradycardia;
• pronounced drop in blood pressure;
• peripheral circulatory disorders;
• dyspnea;
• atrioventricular conduction disorders;
• tremor and fine motor skills disorders;
• muscle cramps;
• depression of consciousness;
• bronchospasm;
• cardiogenic shock, coma;
• heart block and cardiac arrest;
• loss of glycemic control.

If the drug is abused, severe bradycardia may occur.

If the drug is abused, dyspnea may occur.

If the drug is abused, coma may occur.

If the drug is abused, cardiac arrest may occur.

If the drug is abused, seizures may occur.

If the drug is abused, tremor may occur.

https://www.youtube.com/watch?v=l9K8HXuW1c8

The first symptoms of an overdose begin to appear 20-120 minutes after taking a high dosage. If the patient has taken the drug within the last 4 hours, it is necessary to lavage the gastric cavity, induce vomiting and give an adsorbent. In case of severe bradycardia, intravenous administration of adrenaline or atropine at a dose of 1-2 mg is necessary.

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

Treatment: gastric lavage, symptomatic therapy: administration of atropine sulfate (0.5–2 mg intravenously quickly) for bradycardia and impaired AV conduction; glucagon (1–10 mg IV, then IV drip 2–2.5 mg/hour) and dobutamine - in case of decreased myocardial contractility; adrenomimetics (norepinephrine, adrenaline, etc.

What other contraindications does the medicine have?

According to the instructions, Metoprolol for pregnant women is prescribed with extreme caution in the following conditions:

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Before starting therapy, you must ensure that there are no restrictions.

Russian name

Metoprolol

Metoprololum (

https://www.youtube.com/watch?v=rmHXoEGFdzE

Metoprololi)

(±)-1-[4-(2-Methoxyethyl)phenoxy]-3-[(1-methylethyl)amino]-2-propanol (as tartrate or succinate)

Indications

There are quite a lot of indications for use, because the drug reduces blood pressure well, reduces tissue ischemia, and normalizes heart rhythm. The instructions for the drug clearly indicate the diseases for which taking metoprolol is simply necessary.

• Arterial hypertension. The drug can be used either alone or in combination with other medications. By reducing the release of blood into the systemic circulation, pressure decreases. The influence of aortic baroreceptors on the heart is also suppressed.
• Angina attack. Metoprolol ratiopharm relieves the heart, it contracts less quickly, the load on the organ decreases, and less oxygen is required. The drug is a mandatory element of treatment in case of chest pain, discomfort combined with shortness of breath, and fear of death.
• Prophylactic medication, for example, for hypertension, reduces the risk of myocardial ischemia.
• Arrhythmias. Rhythm disturbances are a common occurrence in older people. Metoprolol is indicated for tachycardia, extrasystole, and atrial fibrillation. Biologically active substances slow down the functioning of the sinus node, prevent the emergence of additional (ectopic) lesions, and slow down the conduction of impulses between the atria and ventricles.
• The drug has found use in hyperthyroidism as part of complex therapy, the main effect is a decrease in heart rate.
• Metoprolol ratiopharm helps prevent migraine attacks.
• During myocardial infarction, a focus of necrosis occurs and the tissue around it is damaged. The drug helps preserve living cells, reduces the affected area, increases blood flow, and relieves stress on the heart.

You can take metoprolol only as prescribed by a doctor; you can choose the dosage yourself; the frequency of administration is prohibited!

Pharmacological properties of the drug

What is the drug Metoprolol intended for? Indications for the use of this remedy will be presented below. Now I would like to tell you about what pharmacological properties this drug has.

The medicine mentioned is a cardioselective beta-adrenergic receptor blocker. It does not exhibit membrane stabilizing properties and does not have sympathomimetic intrinsic activity. However, this drug is a hypotensive, antiarrhythmic and antianginal agent.

The medication is able to reduce the patient’s heart rate, reduce myocardial excitability and contractility, slow down AV conduction, and also reduce myocardial oxygen demand.

As a rule, the hypotensive effect is observed in patients only after fourteen days after taking the drug. The drug reduces the frequency of attacks during supraventricular tachycardia, angina pectoris and atrial fibrillation. As a result, the patient's heart rate normalizes.

Slow-release tablets (Metoprolol succinate) have a significant advantage over regular ones. They allow you to maintain a constant concentration of the active element in the blood, which ensures a good therapeutic effect throughout the day. It should also be noted that the effect of Metoprolol succinate helps reduce the risk of bradycardia and weakness, and has a lesser effect on the smooth muscles of the bronchi.

Compound

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The main active component of the drug is metoprolol tartrate, its concentration in one tablet is 50 or 100 milligrams. In addition, the structure of the drug includes additional substances:

• Polysorbate 80.
• Titanium oxide.
• Talc.
• Hypromellose.

The tablets are packaged in blisters of 10 and 14 pieces. There are 2, 3 and 4 blisters in total in the package.

Analogs

If there is no therapeutic effect, the drug can be replaced with one of the analogues:

• Egilok;
• Betalok ZOK;
• Corvitol;
• Betalok;
• Vasocardin;

A quick word about medications. Metoprolol

The drug Corvitol for heart patients and hypertension

The peculiarity of Metoprolol retard-Akrikhin tablets is their prolonged action, which lasts for 24 hours. In contrast, classic Metoprolol contains tartrate salt, which has a rapid therapeutic effect within 30 minutes for a short period of time.