From what "metoprolol" helps. Instructions for use

Gross formula

C 15 H 25 NO 3

Pharmacological group of metoprolol substance

Nonological Classification (ICD-10)

CAS code

37350-58-6

Characteristics of metoprolol substance

Metoprolol Tartrate: White, almost odorless crystalline powder, well-soluble in water, methylene chloride, chloroform and alcohol, weakly soluble in acetone, insoluble on the air.

Metoprolol Sukcinate: White crystalline powder, easily soluble in water, soluble in methanol, moderately soluble in ethanol, weakly soluble in dichloromethane and 2-propanol, practically insoluble in ethyl acetate, acetone, diethyl ether and heptane.

Pharmacology

pharmachologic effect - Antianginal, hypotensive, antiarrhythmic.

Blocks predominantly beta 1 -adrenoreceptors of the heart, does not have internal sympathomimetic and membrane-stabilizing activity. Reduces the heart rate and the garden, slows down the heart rate, weakens the stimulating effect of catecholamines on myocardials during exercise and mental overvoltage, prevents reflex orthostatic tachycardia. The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, the inhibition of the activity of the renin-angiotensin system and the central nervous system, the restoration of the sensitivity of baroreceptors and, as a result, a decrease in peripheral sympathetic influences. The hypotensive effect develops quickly (the garden decreases after 15 minutes, the maximum - after 2 hours) and continues for 6 hours; When administering the metoprolol of succinate - the clinical effect of the Beta Beta block 1 -adrenoreceptors is preserved 24 hours. Dad varies slower: a stable decrease is observed after several weeks of regular reception. The antianginal effect is a consequence of the reduction of the frequency and force of heart rate, the energy costs and the needs of myocardium in oxygen. Reduces the frequency and severity of IBS seizures, the mortality rate in patients with diagnosed myocardial infarction increases the portability of the loads. Metoprollane succinate reduces the risk of death (including sudden death), the occurrence of repeated heart attack (including patients with diabetes mellitus) and improves the quality of life of patients with acute myocardial infarction and idiopathic dilatation cardiomyopathy. An antiarrhythmic effect manifests itself in the elimination of arrhythmogenic sympathetic effects on the conductive heart system, slowing the sinus rhythm and the speed of excitation of excitation via AV node, braking of automatism and lengthening the refractory period. It has a moderate negative inotropic effect. Cardooselectivity is preserved when using daily doses, not exceeding 200 mg. Due to the electoral action on beta 1 -adrenororeceptors, the risk of bronchospasm is theoretically decreases (patients with bronchial asthma less decreases the life function of the lungs), hypoglycemia and narrowing peripheral vessels.

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) Signs of carcinogenicity were not found, but histological changes in the type of hyperplasia of hepatic cells and induction by macrophages of the pulmonary fabric are revealed. With the introduction of albino mice in doses up to 750 mg / kg / day for 21 months, increased the frequency of the development of benign adenomes in the females, but when re-conducting experience, an increase in the incidence of any tumors was not noted. The results of the test of dominant lethal mutations in mice, studies of chromosome of somatic cells, dough on the anomalies of the nuclei of somatic cells in interfase, etc. indicated the absence of mutagenic properties. In rats received doses, 55.5 times higher than the maximum daily dose for a person (450 mg) did not affect fertility, increased the parameters of the postpact death and reduced the survival rate of newborn animals (there was no signs of teratogenicity).

Metoprolol Tartrate quickly and almost completely (95%) is absorbed when taking inside, subjected to intense preyed metabolism. Bioavailability is about 50% at the first reception and increases to 70% when re-use. About 12% binds to albumin plasma blood. It is quickly distributed in the tissues, penetrates through the GEB (the level in the CNS is 78% of the plasma concentration), the placental barrier, breast milk (concentration exceeds plasma). Distribution volume - 5.5 l / kg. C Max is achieved after 1-2 hours after taking, blood level varies significantly. T 1/2 - from 3 to 7 hours. Biotransformed in the liver, with the formation of two active metabolites. It is removed mainly by the kidneys in the form of metabolites, CL - 1 l / min. When taking inside, less than 5% is excreted with urine unchanged, with in / in infusion - about 10%. If the kidney function is violated, bioavailability does not change, but the rate of excretion of metabolites can decrease. In patients with cirrhosis of the liver, metabolism and general clearance slows down (no dosing mode correction is required). Not removed during hemodialysis. When in / in the infusion of the metoprolol of the tartrate for 10 minutes and the more maximum action is developing after 20 minutes, the demolition of the heart rhythm with doses of 5 and 10 mg is 10 and 15%, respectively. After taking inside in the same doses of C Max, the subcinate metoprolol is 1 / 4-1 / 2 c max metoprolol of the tartrate, but continuously saved. Bioavailability in doses of 50-400 mg (1 time per day) by 23% less from such after the reception of a similar dose of tartrate. Pharmacokinetic parameters do not depend on the age of patients.

The use of metoprolol substance

Arterial hypertension of moderate and moderate gravity (monotherapy or in combination with other hypotensive drugs), IBS, hyperkinetic cardiac syndrome, heart rate impaired (sinus tachycardia, ventricular and sufficientar-centuric arrhythmia, including paroxysmal tachycardia, sucanementaricular tachycardia, extrasistol, fluttering and flickering atrial, atrial Tachycardia), hypertrophic cardiomyopathy, mitral valve prolapse, myocardial infarction (prevention and treatment), migraine (prevention), thyrotoxicosis (complex therapy); Treatment of acatus caused by neuroleptics.

Contraindications

Hypersensitivity, AV blockade II and III degree, synoatrial blockade, acute or chronic (in the decompensation stage) heart failure, sine node weak syndrome, expressed sinus bradycardia (heart rate less than 60 q / min), cardiogenic shock, arterial hypotension (garden less 100 mm Hg. Art.), Pronounced disorders of peripheral blood circulation, pregnancy, breastfeeding.

Restrictions on application

Sugar diabetes, hypoglycemia, burded allergic history, metabolic acidosis, bronchial asthma, emphysema, non-allergic bronchitis, hyperthyroidism, psoriasis, feuhromocytoma, violation of the liver function and / or kidney, myasthenia, depression, carrying out general anesthesia, elderly and children's age.

Application in pregnancy and breastfeeding

Perhaps if the expected effect of therapy exceeds the potential risk to the fetus. At the time of treatment, breastfeeding should be stopped.

Side effects methoprolol substance

From the nervous system and sense organs: at least 10% - weakness; 1-9.9% - dizziness and headache; 0.1-0.9% - Reducing attention concentration, drowsiness / insomnia, nightmares, depression, muscle cramps, paresthesia; 0.01-0.09% - nervousness, anxiety, weakening of libido, visual impairment, xerofthalmia, conjunctivitis; Less than 0.01% - lethargy, increased fatigue, anxiety, confusion of consciousness, amnesia / short-term loss of memory, hallucinations, noise in ears, violation of taste sensations.

From the side of the cardiovascular system and blood (blood formation, hemostasis): 1-9.9% - bradycardia, heartbeat, hypotension, cooling limbs; 0.1-0.9% - heart failure, AV blockade, edema syndrome, chest pain; 0.01-0.09% is a decrease in the reduction of myocardium, arrhythmia, less than 0.01% - gangrene (in patients with severe peripheral circulation); Violation of the conductivity of myocardium, syncope, thrombocytopenia, leukopenia, agranulocytosis.

From the head of the gastrointestinal authorities: 1-9.9% - nausea, abdominal pain, diarrhea or constipation; 0.1-0.9% - vomiting; 0.01-0.09% - dryness in the oral cavity, liver function disorders; Meteorism, dyspepsia, heartburn, hepatitis.

From the respiratory system: Dyspnea (1-9.9%), bronchospasm (0.1-0.9%), vasomotor rhinitis (0.01-0.09%), dysnae.

From the side of the skin: 0.1-0.9% - rash, dystrophic skin changes; 0.01-0.09% - reversible alopecia; less than 0.01% - photosensibilization, exacerbation of psoriasis; Itching, erythema, urticaria, hyperhydrosis.

Others: Reducing body weight (0.1-0.9%), arthritium, arthritis, Malgia, muscle weakness, Peyroni disease.

Interaction

The hypotension potentiate sympatholytolitis, nifedipine, nitroglycerin, diuretics, hydralazine and other hypotensive drugs. Antiarrhythmic and anesthesia rates increase the risk of developing bradycardia, arrhythmias, hypotension. Preparations of vintage potentiate the deceleration of AV conductivity. Simultaneous in / in the introduction of verapamil and diltiazem can provoke a stop of the heart. Beta adreminimetics, aminoophyllin, cocaine, estrogens, indomethacin and other NSAIDs weaken antihypertensive effect. Enhances and prolong the effect of antide -olarizing muscle relaxants. The combination with alcohol leads to a mutual strengthening of the oppressive effect on the CNS. Allergens increase the risk of severe systemic allergic reactions or anaphylaxis. Changes the effectiveness of insulin and oral antidiabetic agents and increases the risk of hypoglycemia. Oral contraceptives, cimetidine, ranitidine, phenothiazines - increase the level of metoprolol in the blood, rifampicin - reduces. Lidocaine clearance, Beta 2 -adrenomimetics, the effectiveness of the dose of the latter). Incompatible with Inhibitors of Mao Type A.

Overdose

Symptoms: Arterial hypotension, sharp heart failure, bradycardia, heart stop, AV blockade, cardiogenic shock, bronchospasm, respiratory impairment and consciousness / coma, nausea, vomiting, generalized cramps, cyanosis (manifest after 20 minutes - 2 hours after reception).

Treatment: Stomaching, symptomatic therapy: administration of atropine sulfate (in / in fast 0.5-2 mg) - in bradycardia and violation of AV conduction; glucagon (1-10 mg V / B, then in / in drip 2-2.5 mg / h) and dobutamine - in the event of a decrease in myocardial reduction; adreminimetics (noraderenalin, adrenaline, etc.) - with arterial hypotension; diazepam (in / in slow) - to eliminate seizures; Inhalation of beta adrenomimetics or in / in inkjet administration of Euphillin to relieve bronchospast reactions; Cardiosulation.

Ways of administration

Inside, in / c.

Precautions Substance metoprolol

In patients with chronic heart failure, it is possible to deteriorate the contractile ability of myocardium, which causes the need to apply heart glycosides and / or diuretics with careful monitoring of hemodynamic status. In the event of an increasing bradycardia or AV blockade, it is necessary to reduce the dose or in / in entering atropine. Against the background of sugar diabetes and hyperfunction of the thyroid gland, metoprolol can mask tachycardia caused by hypoglycemia or thyrotoxicosis. In patients with diabetes, the dose correction of antidiabetic drugs and thorough control of the level of glycemia is needed. During the treatment of surgical intervention, a anesthetic agent with the smallest negative inotropic effect should become a means of choice. Perhaps the more pronounced development of the reaction of hypersensitivity and the absence of the therapeutic effect of conventional doses of adrenaline on the background of an exempted allergological history. With the termination of the simultaneous treatment with clonidine, the metoprolol is canceled gradually, a few days before the cancellation of the clonidine, due to the danger of the development of severe hypertensive crisis. In patients with feochromocyte, use is possible only with alpha-adreenolithics. The metoprolol reception is stopped in 2-3 days before delivery (the risk of bradycardia, hypotension and hypoglycemia in a newborn), in exceptional cases, newborns after delivery should be under medical control within 48-72 hours. It should be refracted from use in pediatric practice, since the safety and efficiency of its use in children is not defined. When canceling treatment, reduce the dose must be gradually within 10-14 days. Patients with IBS should be under the careful observation of the doctor during this period. With caution to apply during operation to drivers of vehicles and people whose profession is associated with increased concentration of attention.

special instructions

During treatment, it is possible to change the results of tests during laboratory studies (increase of urea level, transamamine, phosphatase, LDH).

Interactions with other active substances

Trade names

Name	Validation of the Vyshkovsky index ®
	0.2301

25.11.2018

Metoprolol was first released in 1969 for the first time, and from 1980s widely applied worldwide.

Medicine metoprolol It is necessary to use with various diseases of the cardiovascular system, andwith what pressure This drug will be effective?

Properties of the impact on the body

Metoprolol belongs to drugs capable of blocking beta-adrenoreceptors. Such receptors are available in different tissues of the body: smooth muscles, muscle cardiac, kidney, arteries.

They respond to the reaction to stress, in particular, the effect of adrenaline. Finding into the human body, substances that block the effect of beta-adrenoreceptors prevent the action of hormones on receptors and weaken the stressful state.

Beta adrenoblasts have a cardiac effect - reduce the strength and frequency of abbreviations of the heart muscle, reduce its need for oxygen, reduce cardiac conductivity, prevent heart stimulation during physical and emotional loads.

Metoprolol has these qualities. It has an antihypertensive, antiarrhythmic effect and eliminates the symptoms of ischemia.

The antihypertensive result comes gradually and is achieved after a two-week medication. Metoprolol leads to the norm of heart rhythm during tachycardia and atrial flications, reduces the risk of developing arrhythmias than limits the infarct zone and the possibility of his repeat. When used in small doses, less affects the muscles of the bronchi and remote arteries.

Medicinal forms

Metoprolol is produced in two medicinal species: Tartrate and Sukcinate.Both tartrate, and succinate has the form of a white crystalline powder. Both types are well soluble in water. Tartrate is well dissolved in alcohol, trichloromethane and methylene chloride, worse - in acetone, not dissolved at all. Succinate dissolves in methyl alcohol, worse - in ethyl, dissolutely soluble in isopropol and dichloromethane, does not dissolve in ether and acetone.

The substance of metoprolol succinate in the body is poorly released from the microgranuins and is valid long than a tartrate.

The healing effect of succinate lasts about a day, and the tartrate acts not more than 12 hours. Metoprolol Tartrate is less effective, has many side effects.

Metoprolol is metabolized in the liver and is excreted through the urinary system.

Form of manufacture and shelf life

Release tablets 25, 50, 100 and 200 mg, packed by 14, 30, 50, 60, 100, and 200 pcs. For intravenous use - 1% solution in ampoules of 0.05 g, packed by 10 pcs.

Trade names: Betalok, Botok Zok, Egilos, Egilov C, Egilot Retard, Metoprolol Ratiopharm, Metoprolol Acry, Corvitol, Vazocardin and others.

Stored at temperatures up +25 ° C for 3 years.

When do you need to use metoprolol?

Metoprolol can be prescribed by a doctor with pathologies:

• arterial hypertension;
• heart Ischemia;
• hyperkinetic cardiac syndrome;
• heart rate disorders;
• heart attacks;
• matral valve prolapse;
• hypertrophic cardiomyopathy;
• akatysia provoked by neuroleptics.

At the same time, metoprolol is effective with different types of arrhythmias: sinus, ventricular, atrial, perventicular, paroxysmal tachycardia, atrial flicker.

For the treatment of hypertension can be used both in solitary and complex form. Metoprolol can be used to prevent migraine and in overall therapy of hyperthyroidism.

The procedure for the use of metoprolol

Pills Metoprolol can be drunk immediately after meals. But the use of them directly during the meal, enhances the bioavailability of the active substance by 35-40%.Pills Swallow without chewing, and drinking water. A long-term drug is not desirable to smoke in half, such a medicine must be purchased the desired dosage. Dosing the drug is selected by a doctor according to the patient's testimony.

Adults and children over 18 years old metoprolol is recommended to use in doses:

• with hypertension - 100 - 150 mg per day in 1 or 2 reception, a maximum of 200 mg;
• for the prevention of re-infarction - 0.2 g per day in 2 receptions;
• for the prevention of migraines - 0.1-0.2 g per day, separated by 2-4 times;
• with hyperkinetic cardiac syndrome, including the treatment of hyperthyroidism - 50 mg 1-2 times per day;
• when arrhythmia - 0.05 g 2-3 times for 24 hours.

For localization of perventicular tachycardia and in the acute stage of infarction, the drug is administered intravenously in a hospital. With tachycardia, metoprolol is introduced by one-time doses of 2-5 mg at 5 minutes interval before the desired effect is on the onset, but not more than 15 mg. The drug is introduced at a speed of 1-2 mg per minute. The dose of 15 mg does not exceed, because it does not lead to the result. After the localization of the arrhythmic attack, the patient takes the medicine orally to 0.05 g 4 times a day. The first dose of tablet medication should arrive after 15 minutes after administration intravenously.

With a heart attack, metoprolol is introduced three times of 5mg every 2min. Next, patients receive a drug orally at 25-50 mg every 6 hours.Pills Begin to take 15 minutes after administration intravenously.

In the case when a person is poorly transferred to the introduction of intravenously, at the first time the dose of intake is reduced by half. Patients aged better to start taking this medicine with the smallest dose - 0.05 g per day.

Treatment of metoprololol

The therapeutic effect occurs with long-term reception of this fund. For the prevention of recurrence, metoprolol infarction is taken for up to 3 years.Metoprolol is not suitable in order to immediately remove the attack of hypertension.

When treating this tool, it is necessary to strictly adhere to the dosage and reception time specified by the doctor.It is impossible to cancel the medicine yourself or make longer breaks between receptions.

Thirdish

In addition to an effective positive effect, metoprolol has many side effects that can be expressed at the beginning of the reception period like this:

• dizziness;
• weakness;
• fatigue;
• headaches;
• muscle cramps;
• feeling of cold in feet and arms;
• dry mouth;
• constipation or diarrhea;
• conjunctivitis;
• rhinitis;
• skin rash or itching.

On the appearance of such testimony, it is necessary to inform the doctor to appoint otherpills . The long-term effect of this medicine, in the event of a negative reaction, can lead to development:

• hypotension;
• bradycardia;
• sleep disorders;
• depression;
• hypoglycemia (in sugar diabetes);
• reducing the allocation of a tear secret;
• bronchial obstruction (among people predisposed to it).

When is it dangerous to use it?

This beta-adrenoblocator is contraindicated with a sinus node weak syndrome, a stable sinus bradycardia, when the pulse is below 60 blows / min, arterial hypotension (with systolic pressure below 100 mm R.St.), hypersensitivity, synutrial blockade, heart failure in decompensation stage, An atrioventicular blockade of the II and III degree, cardiogenic shock, pronounced violations of the blood flow process in the circulatory system.

When pregnancy and breastfeeding, the attending physician may appoint this medication only when the risk of a woman's disease is higher than the danger of influencing the fruit or child of possible side effects.

In renal failure, metoprolol can be used.

With liver pathologies, thismedicine It is better to replace with another beta adrenoblocator that is metabolized outside the liver.For people with diabetes and Reino disease, a medicine is prescribed with caution.People who use contact lenses should be borne in mind that metoprolol can reduce the development of a tear secret.

Interaction with other substances

In the treatment of metoprolol and simultaneoususage Other drugs should be remembered that its action can increase or weaken, even the opposite effect will occur.

Allergy substances are intensified in action and can cause an allergic reaction. The contraceptives taken inside, antacids - enhance the concentration of metoprolol in the blood, and rifampicin - reduces.

Heart-based heartbreaks in combination with metoprolol reduce atrioventicular conductivity. Nonteroidal anti-inflammatory drugs reduce the antihypertensive effect. The possibility of hypotension and bradycardia can cause painkillers and antiarrhythmic agents.

Other drugs from pressure Can cause hypotension. The use of alcohol during treatment with metoprolol will increase the inhibition of the central nervous system.

Metoprolol reduces the effect of lidocaine, changes the effectiveness of insulin-containing drugs and increases the possibility of the development of hypoglycemia.

Overdose

With a simultaneous reception of the metoprolol dose, exceeding the daily rate, for 2 hours, nausea appears, vomiting, breathing is disturbed, consciousness is confused. Bronchospasm, convulsions, cardiogenic shock, an atrioventicular blockade may occur. Acute heart failure, hypotension, bradycardia is developing, a heart stop may occur.

To avoid heavy consequences, after receiving a large dose of metoprolol, it is necessary to rinse the stomach with a large number of pure water and call ambulance. Then, in the hospital, symptomatic treatment is carried out:

• in bradycardia and reducing atrioventicular conductivity - atropine intravenously introduced;
• when decreasing the heart muscle reduction - glucagon and dobutamine are used;
• in arterial hypotension - use adrenomimetics;
• to eliminate seizures - slowly intravenously introduced diazepams;
• to curb the bronchial spasms, there are inhalations with beta-adreminimetics or intravenously introduced eufillin;
• to avoid stopping the heart, the cardiosuulators are used.

For the resistant effect of metoprolol, apply for a long time. The termination of his reception should occur gradually, for 10 days, under medical control.

If there is a surgery, the patient needs to stop taking metoprolol a few days before applying an anesthetic. The anesthetic drug in this case should have the smallest impact on the strength of heart abbreviations.

Take metoprolol only to appoint a doctor and clearly follow its recommendations. Before receiving, be sure to get acquainted with the annotation to the medicine. Reception of medicines with a healthy lifestyle - the key to the treatment of hypertension.

Metoprolol - This is a drug having a selective type of action. It affects the Beta-adrenoreceptors of the heart muscle. This medicine has a fairly wide range of actions: stops or prevents angina, reduces pressure and leads the heart rhythm to normal. The drug oppresses the automation of the sinus node, it also has a depressive effect on the heart rate, reduces the atrioventricular conductivity, suspends the function of the heart to shrink and carry out the excitation pulse throughout myocardium, reduces blood pressure with cardiac emission and the amount of oxygen required by myocardium. It has the property of stimulation of the inhibition of catecholamines in the heart muscle in physical and emotional-substitution load. With the walls of the voltage, the metoprolol cuts the frequency and strength of the attacks, leads heart rhythm to the norm in the rigging tachycardia and the flickering of the atria. Metoprolol in people with myocarad infarction causes a decrease in the necrosis site, the subsequent risk of the start of fatal arrhythmia is reduced, mortality and risk of recurrences of repeated heart attacks decreases. When receiving an average of therapeutic doses of higher-selective, acts on the smooth muscles of bronchial wood and peripherally lying blood flowing vessels than non-selective beta-adrenoblays.

Indications for use

A drug Metoprololit is used to treat diseases: arterial hypertension of moderate and moderate gravity (monotherapy or in combination with other hypotensive drugs), IBS, hyperkinetic cardiac syndrome, heart rate impaired (sinus tachycardia, ventricular and sucavative warrior arrhythmia, including paroxysmal tachycardia, prevernavicular tachycardia, extrasistol, tremitation and atrial flickering, atrial tachycardia), hypertrophic cardiomyopathy, mitral valve prolapse, myocardial infarction (prevention and treatment), migraine (prevention), thyrotoxicosis (integrated therapy); Treatment of acatus caused by neuroleptics.

Mode of application

Metoprololtake inside, with food or immediately after eating, tablets can be divided by half, but not to cheat and drink with a liquid, for dosage forms of prolonged action - to swallow, not to crush, not to break (except for metoprolol succinate and tartrate), not chew. With arterial hypertension, the average dose is 100-150 mg / day in 1-2 receptions, if necessary - 200 mg / day. Under angina - 50 mg 2-3 times a day. With hyperkinetic cardiac syndrome (including with thyrotoxicosis) - 50 mg 1-2 times per day. With tachiaritimia - 50 mg 2-3 times a day, if necessary - 200-300 mg / day. Secondary prevention of myocardial infarction - 200 mg / day. Migraine prevention - 100-200 mg / day in 2-4 reception. For the relief of paroxysmal hydrodynricular tachycardia, parenterally is administered in a hospital. Enter slowly, dose 2-5 mg (1-2 mg / min). In the absence of effect, the introduction can be repeated after 5 minutes. Increasing the dose of more than 15 mg usually does not lead to greater severity of action. After reliving, the attack arrhythmia of patients is transferred to oral administration at a dose of 50 mg 4 times a day, and the first dose is taken 15 minutes after the termination of the introduction. In the acute stage of the myocardial infarction immediately after the patient's hospitalization (with constant hemodynamic control: ECG, CSS, AV conductivity, blood pressure) should be introduced Bolus to / in 5 mg, the introduction of every 2 min to reach a total dose of 15 mg should be reached. With good tolerability after 15 minutes - inside, 25-50 mg every 6 hours, for 2 days. Patients who poorly transferred the introduction of a full-dose dose should begin to begin oral administration, starting with a half-dose. Supporting therapy continues in doses of 200 mg / day (for 2 receptions), for 3 months-3 years. Elderly patients are recommended to begin treatment with 50 mg / day. Renal failure does not require a dose correction. With liver failure, it is advisable to assign other beta-adrenoblays that are not subjected to metabolism in the liver.

Side effects

At the beginning of therapy from side effects from the use of the drug Metoprololweakness, fatigue, dizziness, headache, muscle cramps, the feeling of cold and paresthesia in the limbs are possible. Bradycardia, arterial hypotension, imparation of atrioventricular conductivity, the appearance of heart failure symptoms with peripheral edema, reduction of the secretion of tear fluid, conjunctivitis, rhinitis, depression, sleep disorder, nightmare, dry mouth, hypoglycemic states in patients with diabetes, vomiting, diarrhea , constipation. In predisposed patients, the symptoms of bronchial obstruction is possible. Separate cases of violations of liver functions, thrombocytopenia, allergic reactions are leather rash, itching.

Contraindications

A drug Metoprololcontraindicated in hypersensitivity, AV blockade of II and III degree, synoyatrial blockade, acute or chronic (in the decompensation stage) of heart failure, a sine node weak syndrome, pronounced sinus bradycardia (Heat less than 60 q / min), cardiogenic shock, arterial hypotension (garden Less than 100 mm Hg.

art.), severe disorders of peripheral blood circulation, pregnancy, breastfeeding.

Interaction with other medicines

The hypotension potentiate sympatholytolitis, nifedipine, nitroglycerin, diuretics, hydralazine and other hypotensive drugs. Antiarrhythmic and anesthesia rates increase the risk of developing bradycardia, arrhythmias, hypotension. Preparations of vintage potentiate the deceleration of AV conductivity. Simultaneous in / in the introduction of verapamil and diltiazem can provoke a stop of the heart. Beta adreminimetics, aminoophyllin, cocaine, estrogens, indomethacin and other NSAIDs weaken antihypertensive effect. Enhances and prolong the effect of antide -olarizing muscle relaxants. The combination with alcohol leads to a mutual strengthening of the oppressive effect on the CNS. Allergens increase the risk of severe systemic allergic reactions or anaphylaxis. Changes the effectiveness of insulin and oral antidiabetic agents and increases the risk of hypoglycemia. Antacids, oral contraceptives, cimetidine, ranitidine, phenothiazines - increase the level of metoprolol in the blood, rifampicin - reduces. Lower Lidocaine clearance, beta2-adrenomimetics efficiency (a dose increase in the latter). Incompatible with Inhibitors of Mao Type A.

Overdose

Symptoms of overdose of the drug Metoprolol: Arterial hypotension, acute heart failure, bradycardia, heart stop, AV blockade, cardiogenic shock, bronchospasm, respiratory impairment and consciousness / coma, nausea, vomiting, generalized convulsions, cyanosis (manifest after 20 minutes - 2 hours after reception).
Treatment: stomach wash, symptomatic therapy: administration of atropine sulfate (V / in fast 0.5-2 mg) - in bradycardia and violation of AV conduction; glucagon (1-10 mg V / B, then in / in drip 2-2.5 mg / h) and dobutamine - in the event of a decrease in myocardial reduction; adreminimetics (noraderenalin, adrenaline, etc.) - with arterial hypotension; diazepam (in / in slow) - to eliminate seizures; Inhalation of beta adrenomimetics or in / in inkjet administration of Euphillin to relieve bronchospast reactions; Cardiosulation.

Storage conditions

List B. at a temperature not higher than + 25 ° C.

Form release

Tablets at 50 and 100 mg per pack of 30; 100 and 200 pieces; Tablets retard 200 mg per pack of 14 pieces; 1% solution in 5 ml ampoules per pack of 10 pieces.

Composition

(±) -1--3 - [(1-methyl ethyl) amino] -2-propanol (in the form of tartrate or succinate).
Metoprolol Tartrate: White, almost odorless crystalline powder, well-soluble in water, methylene chloride, chloroform and alcohol, weakly soluble in acetone, insoluble on the air. Metoprolol Sukcinate: White crystalline powder, easily soluble in water, soluble in methanol, moderately soluble in ethanol, weakly soluble in dichloromethane and 2-propanol, practically insoluble in ethyl acetate, acetone, diethyl ether and heptane.

Synonyms

Betalok (Vetaloc), Blanks (Specikor), Specikor, Squirrel (LOC), Lopressor (Lopressor), Nonclock, Operovol (Orresol), Selopral (Selopral), Vazocardin, Corvitol, Methuxal, Metolol

Additionally

Caution is prescribed with diabetes (especially under the labilence), Rayno disease and patients with impaired peripheral blood circulation, feochromocetoma, pronounced disorders of the kidney and liver function (when prescribing metoprolol-acry of this category of patients, constant control over the dynamics of the functional state of the liver and / or kidney). Patients enjoy contact lenses should take into account that against the background of the treatment of metoprolol-acry perhaps, a decrease in the production of tear fluid. The cessation of the duration of the course should occur gradually (minimum within 10 days) under the supervision of the doctor. A few days before the anesthesia, chloroform or ether must stop taking the drug. In the case of drug intake before surgery, the patient should choose a narcotic agent with a minimal negative inotropic effect.

Main settings

Name:	Metoprolol
ATH code:	C07AB02. -

At elevated pressure, it is necessary to maintain its level in the normal state of the drug. Combination therapy is prescribed to the patient, which most often includes beta adrenoblays.

Metoprolol - What kind of medicine?

In pharmacies you can meet a variety of variations of the same drug - Metoprolol. These are Tablets Metoprolol-retard Akrichin, Teva, Organizer, Ratiopharm, Zentiv - differences consist in the manufacturer. Also, the difference between these drugs exists in the subtype of the active substance: some means include metoprolol succinate, the other - metoprolol tartrates that have the same action and do not differ in efficiency.

The auxiliary substances of drugs can be:

• povidone;
• silicon dioxide;
• lactose monohydrate;
• magnesium stearate;
• starch;
• cellulose.

Outward tablets metoprolol white, convex on both sides, have risk for dividing and engraving "M" on the reverse side. The price for 30 tablets varies greatly depending on the manufacturer and dosage (25, 50,100 mg) and can be from 30 to 350 rubles. In Latin, the doctor indicates in the recipe for the drug Metoprolol».

Action and testimony of the drug

The medicine is prescribed to take with different pathologies of the cardiovascular system. By type of action, it refers to cardiodelective beta-adrenoblockers. When taking inside, the tablets give the following effects:

• antiarrhythmic;
• antianginal;
• antihimensive;
• the membrane-stabilizing (poorly pronounced action).

The medicine blocks special cardiac receptors than reduces the production of CAMF from ATP. This inhibits the movement of calcium ions, makes a rarely heartbeat frequency and the excitability of the heart muscle. With long-term reception, the vascular resistance of the peripheral arteries is reduced (in the first days of treatment it may increase).

Due to the reduction of blood flow and suppressing products of renin (component regulating pressure), antihypertensive effect of the drug is observed.

Metoprolol leads to a norm of blood pressure in a state of rest, stress, with loads, while maintaining its work during the day. As the need for the heart muscle in oxygen falls, the sensitivity of the heart to the influence of sympathetic nerves is reduced. This leads to a decrease in the attacks of angina, which develop on the background of the IBS.

As the drug adopts, the effects of arrhythmogenic factors decrease, therefore, the manifestations of arrhythmia are ceased. Two more important properties of the drug - the ability to prevent migraine attacks and reduced cholesterol levels (the latter is achievable, if you take it for a long time - for several months or years).

Metoprolol is prescribed to treat such pathologies:

• IBS, attacks of angina;
• preinfarction state;
• moored myocardial infarction.

The main indication for the use of the drug can be called the presence of arterial hypertension. Metoprolol is prescribed as a monopreparation or associated with other medicines with a different mechanism of action. Other readings - thyrotoxicosis, tachycardia, extrasystole, migraine.

Instructions for use

The medicine is better to drink while eating, or do it immediately after the end of food intake. Chewing tablets can not be chewed, but the division by 2.4 parts is allowed. Water picking should be abundant.

Procedure for treatment with metoprolol Next:

Elderly people should begin therapy no more than with 50 mg (one-time dose), with a positive result, the dose can be enhanced.

How fast metoprolol reduces pressure?

Arterial hypertension is a severe chronic disease and requires continuous therapy. Despite the fact that the metoprolol is able to quickly reduce pressure indicators, it is necessary to drink it regularly at the same time, not missing a single reception. This is especially important for patients who suffer from stable hypertension. That is, with conservative methods of treatment in the form of weight loss, salt limitations, eliminating harmful habits The pressure remains high.

The effect of the medication begins approximately 15 minutes after use and continues up to 4-6 hours. Metal reception of metoprolol, of course, let's say, but such pills are not suitable if the patient has hypertensive crisis. A sharp decline in pressure is due to a decrease in cardiac output, while a stable antihypertensive effect develops only after 2-3 weeks from the beginning of the reception. During this time, a special substance is accumulated in blood plasma - renin, which monitors pressure indicators.

A variety of different factors can affect the rate of occurrence of the therapeutic effect:

• combined use of metoprolol with other drugs from pressure;
• dosage and multiplicity of use;
• dosage form of medication (tablets, injections, droppers);
• age and other individual characteristics of the body;
• anamnesis of chronic diseases of various organs.

The pressure reduction rate also depends on the initial indicators. What they are less, the more pronounced and rapid will be the effect of reception.

One of the most frequent mistakes in the treatment of metoprolol is the pass of the recommended dose. Against the backdrop of course treatment, patients feel very well and just forget about the need for timely reception of the drug. As a result, the action of the latter decreases, and pressure can dramatically jump. It is because of the passing of the recommended dose often arise hypertensive crises.

The effectiveness of the medication can affect the change in reception time. According to the instructions, metoprolol take once a day. And it is always necessary to do this at the same time. With severe hypertension, even 1-2 hours matter. Therefore, medication is recommended to receive daily at 12 o'clock in the afternoon.

The effect of the drug is minimized with the improper selection of drugs in the scheme of complex treatment. It is strictly forbidden to take ACE inhibitors (metoprolol) with preparations from the Sartan group (Lozartan). Despite the fact that both groups of medicines are used to reduce pressure, their combined reception can lead to unpredictable consequences. Taking even several tablets instead of the expected pressure reduction often leads to the development of a hypertensive crisis. Keep such an attack is very difficult.

The effect of diet on the velocity of the drug

Arterial hypertension is one of the diseases in which it is recommended to adhere to a balanced diet. From the diet you need to exclude pickled, fatty and smoked dishes, as well as limit salt intake. If not to comply with medical recommendations, the action of metoprolol can be slowed or not observed at all.

Therefore, it is important for the efficient and timely effects of the drug to comply with the principles of proper nutrition. Excessive use of salt, alcoholic beverages, even against the background of treatment, can lead to a slowdown of the drug or to a sharp increase in pressure.

Contraindications and "Side"

The medicine has a number of contraindications that need to be strictly observed:

The drug is prohibited to use in children under 18 - it can be prescribed only to adults. Lactation is also a contraindication to therapy by metoprolol. With caution, they give a means to patients with diabetes mellitus, liver pathologies, severe allergic conditions, psoriasis.

During pregnancy, the medicine is prescribed only on life indications - if the risk is higher than the possible danger to the fetus.

Side effects vary by types and severity, in comparison with " by chairs"From the reception of other beta blockers they are similar. It is a blood composition impairment, allergies, aggravation of diabetes mellitus, headaches, asthenia, muscle weakness, sleep disorders, shortness of breath.

Analogs and other information

Among the analogues can be called a number of drugs with the same active substance, as well as other components related to the beta-blockers class.

A drug	Composition	Price, ruble
	Atenolol

Metoprolol refer to cardiolective β1-adrenoblockers, when using the stability of the heart to stress loads with intensive emission into the blood of adrenaline. Today we will tell you in more detail about the testimony for the use of the drug metoprolol, its instructions, analogues, prices and reviews of it cardiologists and patients.

Features of the drug

Has an action:

• hypotensive (reduces pressure);
• antianginal (increases heart endurance);
• antiarrhythmic (normalizes heart rhythm).

Composition

The active substance is Tartrath metoprolol. The auxiliary components include silicon dioxide in anhydrous colloidal form, magnesium stearate, sodium carboxymethyl starch, crystalline cellulose.

Medicinal forms

It is produced in the form of tablets, round convex with risk:

• in the soluble shell of white, beige color - 100 mg. The pack is located 3 blisters of 10 pieces;
• in the shell of a pale pink color - 50 mg. In one pack of 2 or 4 blisters of 14 tablets.

Average prices in Russia from 55 to 140 rubles.

pharmachologic effect

The medication is most effective in the treatment of patients with angina. It reduces the duration and severity of pain attacks, increases the portability of the loads - physical and psycho-emotional.

Pharmacodynamics

When taking metoprolol, it is observed:

• reduction of frequency and severity of angina attacks;
• blood pressure stabilization;
• removing attacks;
• decrease in heart rate;
• suppression of excitability of the heart muscle;
• reducing the severity of ischemia (cessation of blood supply) with, reducing the probability of development, infarction relapses.

Reducing blood pressure occurs within 15 - 20 minutes. Therapeutic action - approximately 6 hours. Stabilization of pressure - after continuous use of about 3 weeks.

Pharmacokinetics

The medicine quite quickly is 95% absorbed into the blood through the gastric and intestine mucosa. The maximum of the metoprolol tartrate in the blood is detected after 1 to 2 hours. The half-life of metoprolol is about 4 hours.

Bioavailability (ability to absorb) increases from 50% to 70 during re-admission. More than 95% of the drug stands out with urine.

Indications

Metoprolol is prescribed with the following states:

1. Regular blood pressure lifts.
2. Violation of heart rhythm - arrhythmia.
3. Ischemia, myocardial infarction, attacks of angina (especially with diabetes, chronic lung obstruction).
4. Hyperthyroidism (in complex treatment).
5. Prevention of migraine attacks.

Therapy of patients with kidney disease does not require a dose change. In hemodialysis, the drug from blood plasma is not deleted.

Instructions for the use of metoprolol tablets

The medicine is accepted together with food, without chewing, drinking water.

• With arterial hypertension. The initial dose per day is 50 mg, then 100 mg - once or 2 times. If the therapeutic effect is absent, the daily dose for 3 to 4 days is raised to the maximum 200 mg.
• Under the attacks of arrhythmia, angina - from 100 to 200 mg for 2 receptions.
• Prevent repeated heart attack - Two-time reception per day at 100 mg (morning, evening).
• To stabilize heart rate - 50 mg twice a day.
• With tachycardiacaused by hyperthyroidism, 50 mg to 4 times a day.
• With panic attacks, neurosis with tachycardia - 50 mg twice a day.

Contraindications

Metoprolol is not allowed for use in the following states:

1. Stage of decompensation with (dangerous condition in disruption of the myocardial function).
2. Reducing the heart rate less than 45 ° C / min.
3. AV (atrioventricular) blockade (violation of cardiac pulses).
4. (Rhythm, frequency, excitation, myocardial reduction).
5. (view of cardiac arrhythmia).
6. (spontaneous angina).
7. Reduced blood pressure (systolic - less than 100 mm.rt.st.).
8. Children and adolescents (up to 18 years).
9. The period of tooling the child (growth delay, fetal hypoxia).
10. Pronounced sensitivity to medication components.
11. Breast milk breastfeeding period.

During pregnancy, medicine is prescribed according to the fact that the medicinal effect for the mother exceeds the risks for the health of the baby.

Side effects

Unwanted effects are rare. May manifest:

1. Fatigue, weakness in muscles, migraine, inhibition, insomnia, confusion of perception.
2. Violation of vision, hearing, conjunctivitis.
3. , arrhythmia, dizziness.
4. Angiospasm (Violation of blood flow in the vessels of legs and arms, the formation of fingertips).
5. Nausea, diarrhea or constipation.
6. Urban, rash, itching, pigmentation, reversible hair loss.
7. Construction of the nasal sinuses, spasm of bronchi, shortness of breath.
8. Fall or increase blood sugar.
9. Thrombocytopenia (bleeding), leukocytopenia (decrease in immunity).
10. A slight weight increase, a temporary decrease in sexual entry and potency.

When canceling the drug - all negative manifestations subsided.

special instructions

Special attention is necessary for patients suffering from:

• diabetes;
• metabolic acidosis (pathological increase in the amount of acid in the blood, leading to coma);
• bronchial asthma, chronic lung obstruction, emphysema;
• diseases of peripheral vessels - Reino disease, chromoty mixed, - the medicine is abolished slowly to avoid cancellation syndrome (agility of the severity of angina attacks);
• chronic insufficiency of liver and kidney functions;
• miastenia (pathologically fast muscle fatigue);
• development of adrenal tumors;
• thyrotoxicosis;
• depressive states;
• psoriasis.

It is also important to remember:

• In heart failure, the application is allowed after stabilizing the heart of the heart. With the angina of the voltage - with a stable pulse frequency at a time of at least 55 beats / min, and not more than 110 during load.
• A sharp cancellation of the means in patients suffering from thyroxicosis is not allowed to avoid gaining symptoms.
• Before the surgical operation, you must inform the anesthesia about therapy with metoprolol.
• In patients in solid age, the dose is adjusted with increasing bradycardia (less than 50 ides / min), a sharp pressure drop, ABB (atrioventricular blockade with a heart rhythm impaired), bronchial spasme, liver disorders. In severe pathologies, treatment is interrupted.
• With renal failure, constant monitoring of the kidney function is required.
• With the strengthening of neurological disorders, depressed is the immediate cancellation of metoprolol.

Interaction with other medicines

The medicine relaxes or enhances the influence of some medicines. For instance:

1. Enhances the effect of funds for blood liquefaction (warfarin).
2. Beta-adrenostimulants, oral contraceptives, theophylline, cocaine, indomethacin, ibuprofen, diclofenac, paracetamol, nimesulide reduce the hypotensive metoprolol effect.

1. , Diltiazem, Amiodaron, Resern, Klonidin (deep bradycardia, heart stop risk).
2. (sharp reduction in pressure).
3. Beta-adrenoblocators (anaprine, pindolol, atenolol).
4. Means of surgical anesthesia, heart glycosides (stanfantine) - inhibition of heart function.
5. Mao inhibitors (antidepressant type) - the threat of a significant pressure drop.
6. Antidepressants (tri- and tetracyclic), neuroleptics, sleeping pills, tranquilizers (inhibition of the nervous system).
7. Ethanol, narcotic substances (inhibition of cardiac activity).
8. Hypoglycemic drugs (reduction of action).
9. Insulin (threat of long hypoglycemia).
10. Preparations for reducing pressure, diuretic, (sharp drop of blood pressure), prazosin requires special caution.
11. Allergens for skin samples and immunotherapy (risk of anaphylactic shock).
12. The substances for X-ray with the content of iodine with intravenous injection (anaphylaxis threat).