Betaloc solution: instructions for use. Betaloc, solution for intravenous administration (ampoules) Betaloc in ampoules instructions for use

In this article, you can read the instructions for using the drug betaloc. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Betaloc in their practice are presented. A big request to actively add your reviews about the drug: did the medicine help or not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Analogues of Betalok in the presence of existing structural analogues. Use to treat heart rhythm disorders (arrhythmias) in adults, children, and during pregnancy and lactation. Interaction of the drug with alcohol.

betaloc- a beta1-blocker that blocks beta1 receptors at doses significantly lower than the doses required to block beta2 receptors. Metoprolol has a slight membrane-stabilizing effect and does not show partial agonist activity. Metoprolol reduces or inhibits the agonistic effect that catecholamines, which are released during nervous and physical stress, have on cardiac activity. This means that metoprolol has the ability to prevent an increase in heart rate, cardiac output and increased contractility of the heart, as well as an increase in blood pressure caused by a sharp release of catecholamines.

Patients with symptoms of obstructive pulmonary disease, if necessary, can be prescribed metoprolol in combination with beta2-agonists. When used together with beta2-agonists, Betaloc in therapeutic doses has less effect on bronchodilation caused by beta2-adrenomimetics than non-selective beta-blockers. Metoprolol to a lesser extent than non-selective beta-blockers affects insulin production and carbohydrate metabolism. The effect of Betaloc on the response of the cardiovascular system under conditions of hypoglycemia is much less pronounced compared to non-selective β-blockers.

Clinical studies have shown that Betaloc may cause a slight increase in triglyceride levels and a decrease in free fatty acids in the blood. In some cases, there was a slight decrease in the high-density lipoprotein (HDL) fraction, which is less pronounced than in the case of the use of non-selective P-blockers. However, in one of the clinical studies, a significant decrease in the level of total cholesterol in the blood serum was shown during the treatment with metoprolol for several years.

The quality of life during treatment with Betaloc does not deteriorate or improves. An improvement in the quality of life during treatment with Betaloc was observed in patients after myocardial infarction.

Compound

Metoprolol tartrate + excipients.

Pharmacokinetics

Betaloc is almost completely absorbed after oral administration. When taking the drug within therapeutic doses, the concentration of the drug in the blood plasma is linearly dependent on the dose taken.

After ingestion of the first dose of metoprolol, systemic circulation reaches about 50% of the dose. With repeated doses, the systemic bioavailability index increases to 70%. Taking the drug with food can increase systemic bioavailability by 30-40%. Communication with blood plasma proteins is low, about 5-10%.

Metoprolol undergoes oxidative metabolism in the liver with the formation of 3 main metabolites, none of which has a clinically significant beta-blocking effect.

About 5% of the dose taken is excreted in the urine unchanged, in some cases this figure can reach 30%.

Indications

arterial hypertension: lowering blood pressure and reducing the risk of cardiovascular and coronary death (including sudden death);
angina;
cardiac arrhythmias, including supraventricular tachycardia;
in complex therapy after myocardial infarction;
functional disorders of cardiac activity, accompanied by tachycardia;
prevention of migraine attacks;
hyperthyroidism (complex therapy);
supraventricular tachycardia (for injections).

Release forms

Tablets 100 mg.

Solution for intravenous administration (injections in ampoules for injection).

25 mg, 50 mg and 100 mg film-coated tablets (Betaloc ZOK).

Instructions for use and dosing regimen

Tablets

Tablets can be taken both with food and on an empty stomach.

Arterial hypertension

100-200 mg of Betaloc once in the morning or in two divided doses; morning and evening. If necessary, the dose can be increased or another antihypertensive agent added.

Long-term antihypertensive therapy of 100-200 mg of Betaloc per day can reduce overall mortality, including sudden death, as well as the incidence of cerebral strokes and coronary circulation disorders in patients with arterial hypertension.

angina pectoris

100-200 mg per day in two doses; morning and evening. If necessary, another antianginal drug may be added to therapy.

Heart rhythm disorders

100-200 mg per day in two doses; morning and evening. If necessary, another antiarrhythmic drug may be added to therapy.

Maintenance therapy after myocardial infarction.

The maintenance dose is 200 mg per day in two divided doses; morning and evening. The appointment of Betaloc at a dose of 200 mg per day can reduce mortality in patients who have had a myocardial infarction and reduce the risk of developing a recurrent myocardial infarction (including in patients with diabetes mellitus).

Functional disorders of cardiac activity, accompanied by tachycardia

100 mg of Betaloc once a day, it is recommended to take a tablet in the morning. If necessary, the dose may be increased.

Prevention of migraine attacks

100-200 mg per day in two doses; morning and evening.

Hyperthyroidism

150-200 mg per day in 3-4 doses.

Ampoules

Supraventricular tachycardia.

Begin administration with 5 mg (5 ml) of Betaloc at a rate of 1-2 mg/min. You can repeat the introduction with a 5-minute interval until a therapeutic effect is achieved. Usually the total dose is 10-15 mg (10-15 ml). The recommended maximum dose for intravenous administration is 20 mg (20 ml).

Prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarction or suspected of it.

Intravenously 5 mg (5 ml) of the drug. You can repeat the introduction with a 2-minute interval, the maximum dose is 15 mg (15 ml). 15 minutes after the last injection, oral metoprolol is prescribed at a dose of 50 mg (Betaloc) every 6 hours for 48 hours.

Betaloc ZOK

When selecting a dose, it is necessary to avoid the development of bradycardia.

With arterial hypertension, the dose is 50-100 mg 1 time per day. If necessary, the dose can be increased to 100 mg 1 time per day or Betaloc ZOK can be used in combination with other antihypertensive drugs (preferably a diuretic and a calcium channel blocker, a derivative of dihydropyridine).

With angina pectoris, the dose is 100-200 mg 1 time per day. If necessary, Betaloc ZOK can be used in combination with another antianginal drug.

With stable symptomatic chronic heart failure with impaired left ventricular systolic function, Betaloc ZOK can be prescribed to patients who have not experienced exacerbation episodes in the last 6 weeks and have not changed their main therapy in the last 2 weeks. Therapy of heart failure with beta-blockers can sometimes lead to a temporary worsening of the symptomatic picture. In some cases, it is possible to continue therapy or reduce the dose, and in some cases it may be necessary to discontinue the drug.

With stable chronic heart failure of the 2 functional class, the recommended initial dose for the first 2 weeks is 25 mg 1 time per day. After 2 weeks, the dose may be increased to 50 mg once daily and then doubled every 2 weeks. The maintenance dose for long-term treatment is 200 mg once a day.

With stable chronic heart failure of 3 and 4 functional classes, the recommended initial dose for the first 2 weeks is 12.5 mg 1 time per day. The dose is selected individually. During the period of increasing the dose, the patient should be monitored, because. in some patients, symptoms of heart failure may worsen. After 1-2 weeks, the dose can be increased to 25 mg 1 time per day, then after another 2 weeks - up to 50 mg 1 time per day. If well tolerated, the dose can be doubled every 2 weeks until a maximum dose of 200 mg once daily is reached.

In case of arterial hypotension and / or bradycardia, it may be necessary to reduce concomitant therapy or reduce the dose of Betaloc ZOK. Arterial hypotension at the beginning of therapy does not necessarily indicate that a given dose of Betaloc ZOK will not be tolerated during further long-term treatment. However, doses should not be increased until the condition has stabilized. Monitoring of kidney function may also be required.

In case of heart rhythm disturbances, the drug is prescribed at a dose of 100-200 mg 1 time per day.

For maintenance treatment after myocardial infarction, the drug is prescribed at a dose of 200 mg 1 time per day.

With functional disorders of cardiac activity, accompanied by tachycardia, the dose is 100 mg 1 time per day, if necessary, the dose can be increased to 200 mg per day.

For the prevention of migraine attacks, it is prescribed in a dose of 100-200 mg 1 time per day.

Betaloc ZOK is intended for daily use 1 time per day (preferably in the morning). Betaloc ZOK tablet should be swallowed with liquid. Tablets can be divided in half, but should not be chewed or crushed. Eating does not affect the bioavailability of the drug.

In patients with impaired renal function, as well as in elderly patients, there is no need to adjust the dose of the drug.

In patients with impaired liver function, dose adjustment of the drug is usually not required due to the low degree of binding of metoprolol to plasma proteins. However, in severe hepatic impairment (in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.

Side effect

bradycardia;
postural disorders (very rarely accompanied by syncope);
cold extremities;
heartbeat;
temporary increase in symptoms of heart failure;
AV blockade 1 degree;
cardiogenic shock in patients with acute myocardial infarction;
other disorders of cardiac conduction;
arrhythmias;
gangrene in patients with previous severe peripheral circulatory disorders;
increased fatigue;
dizziness;
headache;
increased nervous excitability;
anxiety;
impotence/sexual dysfunction;
paresthesia;
convulsions;
depression;
weakening of attention;
drowsiness or insomnia;
nightmares;
amnesia / memory impairment;
depression;
hallucinations;
nausea, vomiting;
pain in the abdomen;
diarrhea;
constipation;
dry mouth;
liver dysfunction;
rash (in the form of urticaria);
increased sweating;
hair loss;
photosensitivity;
exacerbation of psoriasis;
shortness of breath with physical effort;
bronchospasm;
rhinitis;
visual impairment;
dryness and/or irritation of the eyes;
conjunctivitis;
tinnitus;
taste disturbances;
arthralgia;
weight gain;
thrombocytopenia.

Contraindications

atrioventricular blockade of 2 and 3 degrees;
heart failure in the stage of decompensation;
patients receiving long-term or intermittent therapy with inotropic agents and acting on beta-adrenergic receptors;
clinically significant sinus bradycardia;
sick sinus syndrome;
cardiogenic shock;
severe disorders of peripheral circulation;
arterial hypotension;
betaloc is contraindicated in patients with acute myocardial infarction with a heart rate of less than 45 beats per minute, a PQ interval of more than 0.24 seconds, or a systolic blood pressure of less than 100 mm Hg;
with serious peripheral vascular diseases with the threat of gangrene;
patients receiving beta-blockers, intravenous administration of blockers of "slow" calcium channels such as verapamil is contraindicated;
age up to 18 years (efficacy and safety have not been established);
known hypersensitivity to metoprolol and its components or to other beta-blockers.

Use during pregnancy and lactation

The amount of metoprolol excreted in breast milk and the beta-blocking effect in a breastfed child (when the mother takes metoprolol in therapeutic doses) are insignificant.

Use in elderly patients

There is no need to adjust the dose in elderly patients.

Use in children

Contraindicated in children under 18 years of age.

special instructions

Patients taking beta-blockers should not be given intravenous "slow" calcium channel blockers such as verapamil. Patients suffering from obstructive pulmonary disease are not recommended to prescribe beta-blockers. In case of poor tolerance of other antihypertensive agents or their ineffectiveness, metoprolol can be prescribed, since it is a selective drug. It is necessary to prescribe the minimum effective dose, if necessary, it is possible to prescribe a beta2-agonist.

When using beta1-blockers, the risk of their effect on carbohydrate metabolism or the possibility of masking the symptoms of hypoglycemia is much less than when using non-selective beta-blockers.

In patients with chronic heart failure in the stage of decompensation, it is necessary to achieve a stage of compensation both before and during treatment with the drug.

Patients suffering from Prinzmetal's angina are not recommended to prescribe non-selective beta-blockers.

Very rarely, patients with impaired AV conduction may worsen (possible outcome - AV blockade). If bradycardia develops during treatment, the dose of Betaloc should be reduced or the drug should be gradually discontinued.

Metoprolol may worsen the symptoms of peripheral circulatory disorders, mainly due to a decrease in blood pressure. Caution should be exercised when prescribing the drug to patients suffering from severe renal insufficiency, with metabolic acidosis, co-administration with cardiac glycosides. Patients suffering from pheochromocytoma should be given an alpha-blocker in parallel with Betaloc.

In patients with cirrhosis of the liver, the bioavailability of metoprolol is increased. In the case of surgery, the anesthesiologist should be informed that the patient is taking a beta-blocker.

Abrupt discontinuation of the drug should be avoided. If it is necessary to cancel the drug, the cancellation should be carried out gradually. In most patients, the drug can be discontinued within 14 days. The dose of the drug is reduced gradually, in several doses, until the final dose of 25 mg is reached once a day. Patients with ischemic heart disease should be under close medical supervision during drug withdrawal. In patients taking beta-blockers, anaphylactic shock is more severe.

Influence on the ability to drive vehicles and control mechanisms

When using the drug, episodes of dizziness or general weakness are possible, and therefore it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

drug interaction

Co-administration of Betaloc with the following drugs should be avoided:

Barbituric acid derivatives: barbiturates (the study was conducted with phenobarbital) slightly increase the metabolism of metoprolol, due to the induction of enzymes.

Propafenone: When propafenone was administered to four patients treated with metoprolol, there was an increase in the plasma concentration of metoprolol by 2-5 times, while two patients had side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. Probably, the interaction is due to inhibition by propafenone, like quinidine, of the metabolism of metoprolol through the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a beta-blocker, the co-administration of metoprolol and propafenone does not seem appropriate.

Verapamil: The combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function.

The combination of Betaloc with the following drugs may require dose adjustment:

Class 1 antiarrhythmics: Class 1 antiarrhythmics and beta-blockers may result in a pooling negative inotropic effect, which may lead to serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with sick sinus syndrome and impaired AV conduction. The interaction is described on the example of disopyramide.

Amiodarone: The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia. Given the extremely long half-life of amiodarone (50 days), the potential for interactions long after amiodarone withdrawal should be taken into account.

Diltiazem: Diltiazem and beta-blockers mutually reinforce the inhibitory effect on AV conduction and sinus node function. When metoprolol was combined with diltiazem, there were cases of severe bradycardia.

Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction is best documented for indomethacin. There was no reported interaction for sulindac. In studies with diclofenac, the described reaction was not noted.

Diphenhydramine: Diphenhydramine reduces the clearance of metoprolol to alpha-hydroxymetoprolol by 2.5 times. At the same time, there is an increase in the action of metoprolol.

Epinephrine (adrenaline): 10 cases of severe hypertension and bradycardia have been reported in patients taking non-selective beta-blockers (including pindolol and propranolol) and receiving epinephrine (adrenaline). The interaction was also noted in the group of healthy volunteers. It is assumed that similar reactions can be observed when epinephrine is used in conjunction with local anesthetics in case of accidental entry into the vascular bed. This risk is expected to be much lower with cardioselective beta-blockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) at a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, beta-blockers can cause reactions of paradoxical arterial hypertension in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported while taking phenylpropanolamine.

Quinidine: Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (approximately 90% of the population in Sweden), causing mainly a significant increase in the plasma concentration of metoprolol and an increase in beta-blockade. It is believed that such an interaction is also characteristic of other p-blockers in the metabolism of which cytochrome P4502D6 is involved.

Concomitant use of alcohol, antihypertensive drugs, quinidine or barbiturates may worsen the patient's condition.

Clonidine: Hypertensive reactions with abrupt withdrawal of clonidine may be exacerbated by co-administration of beta-blockers. When used together, if clonidine is discontinued, discontinuation of beta-blockers should begin a few days before clonidine is discontinued.

Rifampicin: Rifampicin may increase the metabolism of metoprolol, decreasing the plasma concentration of metoprolol.

Plasma concentrations of metoprolol may increase when used in combination with cimetidine, hydralazine, selective serotonin inhibitors such as paroxetine, fluoxetine and sertraline. Patients simultaneously taking metoprolol and other β-blockers (eye drops) or monoamine oxidase inhibitors (MAOIs) should be closely monitored. Against the background of taking beta-blockers, inhalation anesthetics increase the cardiodepressive effect. Against the background of taking beta-blockers, patients receiving oral hypoglycemic agents may require dose adjustment of the latter.

Cardiac glycosides, when used together with beta-blockers, can increase the time of atrioventricular conduction and cause bradycardia.

Analogues of the drug Betaloc

Structural analogues for the active substance:

Betalok ZOK;
Vasocardin;
Corvitol 100;
Corvitol 50;
Metozok;
Metocard;
Metokor Adifarm;
Metolol;
metoprolol;
Egilok;
Egilok Retard;
Egilok C;
Emzok.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.

In addition to the main active ingredient ( metoprolol tartrate ) the medicine contains the following auxiliary components:

: sodium chloride , water.
Tablets: lactose monohydrate , sodium carboxymethyl starch , povidone , magnesium stearate , anhydrous colloidal silicon dioxide .

Release form

Solution for internal administration is a clear, colorless liquid.
white tablets are in a plastic bottle (100 pcs.), Placed in a cardboard box.

pharmachologic effect

Renders antiarrhythmic , antianginal and hypotensive action .

Pharmacodynamics and pharmacokinetics

Metoprolol significantly reduces or completely eliminates the effect catecholamines at mental , physical and emotional tension . In addition, it moderately reduces the heart rate and myocardial contractility . Has a hypotensive effect.

Betaloc may slightly increase the level of TG and reduce the concentration of free fatty acids in the blood serum. In some cases, there is a slight decrease in lipoproteins high density.

Betaloc solution spreads quickly, within a few minutes. At a dose of up to 20 mg, the pharmacokinetics are linear. The half-life is on average 3-4 hours. Absorbed by 95%, the remaining substances are excreted unchanged.

Indications for use

Indications for the use of tablets:

arterial hypertension ;
violation of the heart rhythm;
problems with the work of the heart, accompanied by;

As an element of complex therapy, they are prescribed during and after. Can be used to prevent seizures.

Indications for the use of the solution:

myocardium ;
pain sensations when myocardial infarction or suspicion of it.

Can also be used for prevention tachycardia and myocardial ischemia .

Contraindications

Betaloc tablets and solution should not be taken if you are hypersensitive to this drug and other beta blockers , and also when:

II and III degree;
clinically significant sinus bradycardia ;
sick sinus syndrome;
arterial hypotension ;
heart failure in the decompensation stage;
cardiogenic shock ;
pronounced violation peripheral circulation ;
sharp myocardial infarction with a heart rate of 45 beats / min or less, systolic blood pressure less than 100 millimeters of mercury. Art., as well as with an interval of PQ greater than 0.24 seconds;
severe peripheral vascular diseases (in case of a threat).

In addition, this remedy cannot be taken by those who receive inotropic drugs and stimulants beta-adrenergic receptors periodically or constantly.

Betaloc should be used with caution when atrioventricular block I degree , COPD , heavy , Princemetal , . For children, the effectiveness and safety of this drug have not been established.

In addition, the solution for injection should not be used in the treatment supraventricular , if blood pressure is less than 110 mm Hg, and tablets - to patients receiving intermittent long-term therapy inotropic drugs that affect beta-adrenergic receptors .

Side effects

When using Betaloc, side effects are usually mild or reversible.

As a result of the studies, the following possible side effects were identified:

from the side of cardio-vascular system: cold extremities, bradycardia fainting, palpitations, cardiogenic shock (occurs in those treated with acute), degree I and all kinds of other violations of the conduction of the heart;
from the side gastrointestinal tract: nausea , abdominal pain, vomit ;
from the side skin: rash, increased sweating;
from the side metabolism: increased body fat;
from the side CNS: increased fatigue, I am , convulsions , , impaired attention, or nightmares;
from the side respiratory organs: appearance during physical exertion, bronchospasm .

In rare cases, there is increased nervous excitability, / sexual dysfunction , anxiety, memory impairment, depression, dry mouth.

Some patients also experienced liver dysfunction, hepatitis , hair loss, photosensitivity , exacerbation , blurred vision, conjunctivitis eye irritation, tinnitus, taste disturbance, arthralgia , thrombocytopenia .

Instructions for use Betalok

Instructions for the use of Betaloc in the form of a solution provide for its introduction only by medical workers with the appropriate skills and the obligatory observance of the conditions for resuscitation.

At supraventricular tachycardia initial dose - 5 mg (5 ml). The rate of administration is 1-2 mg / min. Apply every 5 minutes until the desired effect is achieved (as a rule, it takes 10-15 mg of the solution). But you should not enter more than 20 mg.

At myocardial infarction , prevention and treatment myocardial ischemia , tachycardia begin to inject 5 mg (5 ml) of the solution every 2 minutes until the onset of effect, but the dose of 15 mg (15 ml) should not be exceeded. A quarter of an hour after the last injection, therapy should be continued using metoprolol for oral administration (50 mg every 6 hours for two days).

If you are prescribed to take Betaloc tablets, the instructions for use provide for different dosages for different cases:

arterial hypertension: appoint 100-200 mg 1 time in the morning or in two doses (in the morning and evening), if necessary, the dose can be increased or another dose can be added antihypertensive a drug;
cardiac arrhythmias: it is necessary to prescribe 100-200 mg per day in 2 doses (in the morning and evening), if necessary, you can add another antiarrhythmic a drug;
heart failure with tachycardia: appoint 100 mg 1 time per day (preferably in the morning), if necessary, the dose can be increased;
hyperthyroidism: appoint 150-200 mg per day in 3-4 doses;
angina pectoris: appoint 100-200 mg daily in 2 doses (in the morning and evening), if necessary, you can add another antianginal a drug;
supportive care after myocardial infarction: it is necessary to prescribe 200 mg daily, two doses in the morning and evening;
prevention migraine: appoint 100-200 mg per day in 2 doses (in the morning and evening).

Tablets are taken orally during a meal or on an empty stomach.

Overdose

The use of Betaloc solution at a dose of 7.5 g can lead to intoxication with a fatal outcome. Doses of 1.4 g and 2.5 g caused, respectively, moderate and severe intoxication.

Possible in case of overdose bradycardia , asystole , perfusion weak peripheral, atrioventricular block I-III degree, a pronounced decrease in blood pressure, cardiogenic shock , heart failure. On the part of the lungs, there is difficulty in breathing,. From the side of the central nervous system, there is increased fatigue, loss and impaired consciousness. In addition, there may be tremor , increased sweating, spasms , vomiting , hypo- or hyperglycemia , transient myasthenic syndrome , convulsions , paresthesia , nausea , hyperkalemia .

The first signs of drug overdose are observed 20-120 minutes after ingestion.

Treatment is with activated charcoal and/or gastric lavage. In addition, symptomatic treatment is carried out. So, if necessary, adequate ventilation of the lungs, ECG monitoring, replenishment of the bcc and glucose infusions are administered. When suppressed myocardium introduced or . It is also possible to use 50-150 mcg / kg intravenously every minute until the effect occurs. In some cases, they use . With the appearance and increase of the ventricular complex, a sodium solution is used. It is possible to use an artificial pacemaker. To prevent bronchospasm use terbutaline . And when the heart stops, resuscitation is carried out.

With an overdose of Betaloc tablets, there may be such consequences: sinus bradycardia , vomit or nausea , atrioventricular block , bronchospasm , heavy hypotension , cardiogenic shock , heart failure, cardiac arrest, impaired consciousness, .

Treatment is symptomatic. As a rule, gastric lavage is also prescribed.

With a significant decrease in blood pressure, bradycardia and heart failure, stimulants are administered beta1-adrenergic receptors (every 3-5 minutes until the result). Also appointed dopamine and , sympatholytics (norepinephrine , dobutamine ) and at a dosage of 1-10 mg. It is possible to use a pacemaker.

With spasm of the bronchi, intravenous beta2-adrenergic stimulants are used.

Interaction

When used together with Betalok ganglion blockers , blockers beta receptors and MAO inhibitors the patient's condition must be carefully monitored.

On cancellation , taken against the background of Betaloc, the latter is canceled a few days before.

In addition, this drug cannot be combined with other antiarrhythmic drugs, as well as calcium antagonists, barbiturates , . inhalation anesthetics in combination with Betalok give potentiation of cardiodepressive action .

Inductors and inhibitors metabolism affect the concentration of plasma Betaloc. And his hypotensive action decreases when combined with

Betaloc ZOK belongs to the same manufacturer and, as a rule, Betaloc itself is compared with it.

What is the difference between Betaloc ZOK and Betaloc?

The forums often ask the question: what is the difference Betaloc ZOK from Betalok. Experts explain that in the first case, the medicine does not act immediately. Active substances are released gradually, and therefore the drug is better tolerated. Its side effects are less pronounced. Both drugs, however, Betaloc and Betaloc ZOK - dispensed in pharmacies strictly by prescription.

Compound

1 ml 1 amp. Metoprolol tartrate 1 mg 5 mg. Excipients: sodium chloride, water for injection.

Pharmacological effect

In patients with myocardial infarction, intravenous administration of metoprolol reduces chest pain and reduces the risk of developing atrial fibrillation and flutter. Intravenous administration of metoprolol at the first symptoms (within 24 hours after the onset of the first symptoms) reduces the risk of myocardial infarction. Early initiation of treatment with metoprolol leads to an improvement in the further prognosis of the treatment of myocardial infarction. A decrease in heart rate (HR) is achieved with paroxysmal tachycardia and atrial fibrillation (flutter). Metoprolol is a β.1-adrenergic blocker that blocks β.1 receptors at doses significantly lower than those required to block β.2 receptors. Metoprolol has a slight membrane-stabilizing effect and does not show partial agonist activity. Metoprolol reduces or inhibits the agonistic effect that catecholamines, which are formed during nervous and physical stress, have on cardiac activity. This means that metoprolol has the ability to prevent an increase in heart rate, cardiac output and an increase in myocardial contractility, as well as an increase in blood pressure, caused by the release of catecholamines. Patients with symptoms of obstructive pulmonary disease, if necessary, can be prescribed metoprolol in combination with β.2-agonists. When used together with β .2-adrenergic agonists, Betaloc in therapeutic doses has a lesser effect on bronchodilation caused by β .2-agonists than non-selective β .-blockers. Metoprolol to a lesser extent than non-selective β.-blockers. affect insulin production and carbohydrate metabolism. The effect of Betaloc on the response of the cardiovascular system under conditions of hypoglycemia is much less pronounced compared to non-selective β-blockers. An improvement in the quality of life during treatment with Betaloc was observed in patients after myocardial infarction.

Indications

Supraventricular tachycardia - prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarction or suspicion of it.

Contraindications

Atrioventricular block II and III degree - heart failure in the stage of decompensation - clinically significant sinus bradycardia - sick sinus syndrome, - cardiogenic shock - severe peripheral circulatory disorders - arterial hypotension - patients with acute myocardial infarction with a heart rate of less than 45 beats per minute, PQ interval more than 0.24 seconds or systolic blood pressure less than 100 mm Hg - in case of serious peripheral vascular diseases with the threat of gangrene - patients receiving β. safety not established) - known hypersensitivity to metoprolol and its components or to other β.-blockers. With caution: atrioventricular block I degree, Prinzmetal's angina, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis, bronchial asthma), diabetes mellitus, severe renal failure.

Use during pregnancy and lactation

Like most drugs, Betaloc should not be prescribed during pregnancy and during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus. Like other antihypertensive agents, β.-blockers can cause side effects, such as bradycardia in the fetus, newborn or breastfeeding children, and therefore, special care should be taken when prescribing β.-blockers in the last trimester of pregnancy and directly. before childbirth. Lactation period: The amount of metoprolol excreted in breast milk and β.- blocking effect in a breastfed child (when the mother takes metoprolol in therapeutic doses) are insignificant.

Dosage and administration

Supraventricular tachycardia. Begin administration with 5 mg (5 ml) of Betaloc at a rate of 1-2 mg/min. You can repeat the introduction with a 5-minute interval until a therapeutic effect is achieved. Usually the total dose is 10-15 mg (10-15 ml). The recommended maximum dose for intravenous administration is 20 mg (20 ml). Prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarction or suspected of it. Intravenously 5 mg (5 ml) of the drug. You can repeat the introduction with a 2-minute interval, the maximum dose is 15 mg (15 ml). 15 minutes after the last injection, oral metoprolol is prescribed at a dose of 50 mg (Betaloc) every 6 hours for 48 hours. Impaired renal function There is no need to adjust the dose in patients with impaired renal function. Impaired liver function Usually, due to the low degree of binding to plasma proteins, dose adjustment is not required. However, in severe hepatic impairment (in patients with porto-caval anastomosis), a dose reduction may be required. Elderly There is no need to adjust the dose in elderly patients. Children There is limited experience with Betaloc in children.

Side effects

special instructions

Betaloc is well tolerated by patients and side effects are generally mild and reversible. As a result of clinical studies or the use of Betaloc (metoprolol tartrate) in clinical practice, the following undesirable side effects have been described. In many cases, a causal relationship with Betaloc treatment has not been established. The following criteria were used to assess the incidence of cases: very often (> 10%), often (1-9.9%), infrequently (0.1-0.9%), rarely (0.01-0.09%) and very rarely (less than 0.01%). Cardiovascular system Often: bradycardia, postural disturbances (very rarely accompanied by syncope), cold extremities, palpitations. Infrequently: temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction. AV block I degree. Rare: other cardiac conduction disorders, arrhythmias. Very rare: gangrene in patients with previous severe peripheral circulatory disorders. CNS Very common: fatigue. Often: dizziness, headache. Rare: irritability, anxiety, impotence/sexual dysfunction. Infrequently: paresthesia, convulsions, depression, impaired attention, drowsiness or insomnia, nightmares. Very rare: amnesia/memory impairment, depression, hallucinations of the gastrointestinal tract Common: nausea, abdominal pain, diarrhea, constipation. Uncommon: vomiting. Rare: dry mouth. Liver Rarely: abnormal liver function. Integuments Infrequently: rash (in the form of urticaria), increased sweating. Rare: hair loss. Very rare: photosensitivity, exacerbation of psoriasis. Respiratory organs Often: shortness of breath with physical effort. Uncommon: bronchospasm in patients with bronchial asthma. Rare: rhinitis. Sense Organs Rare: visual disturbances, dry and/or irritated eyes, conjunctivitis. Very rare: ringing in the ears, taste disturbances. Metabolism Uncommon: weight gain. From the musculoskeletal system: Very rarely: arthralgia Blood Very rarely: thrombocytopenia.

Betaloc Betaloc

Release form Betaloc

Solution for intravenous administration.

Composition of Betalok

1 ml of solution contains:

Active substances: metoprolol tartrate for injection - 1 mg.

Excipients: sodium chloride for injection - 9 mg; water for injection - up to 1 ml.

Packing Betalok

5 pieces. 5 ml.

Pharmacological action of Betalok

A decrease in heart rate (HR) is achieved with paroxysmal tachycardia and atrial fibrillation (flutter).

Metoprolol is a β 1 -blocker that blocks β 1 receptors at doses significantly lower than those required to block β 2 receptors. Metoprolol has a slight membrane-stabilizing effect and does not show partial agonist activity. Metoprolol reduces or inhibits the agonistic effect that catecholamines, which are formed during nervous and physical stress, have on cardiac activity. This means that metoprolol has the ability to prevent an increase in heart rate, cardiac output and an increase in myocardial contractility, as well as an increase in blood pressure, caused by the release of catecholamines. Patients with symptoms of obstructive pulmonary disease, if necessary, can be prescribed metoprolol in combination with β 2 -agonists. When used together with β 2 - adrenomimetics, Betaloc® in therapeutic doses has a lesser effect on bronchodilation caused by β 2 - adrenomimetics than non-selective β-blockers.

Metoprolol to a lesser extent than non-selective β-blockers. affect insulin production and carbohydrate metabolism. The effect of Betaloc® on the response of the cardiovascular system under conditions of hypoglycemia is much less pronounced compared to non-selective β-blockers. An improvement in the quality of life during treatment with Betaloc was observed in patients after myocardial infarction.

Indications and usage of Betaloc

Supraventricular tachycardia.
Prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarction or suspected of it.

Contraindications

Atrioventricular block II and III degree.
Heart failure in the stage of decompensation.
Clinically significant sinus bradycardia.
Sick sinus syndrome.
Cardiogenic shock.
Severe disorders of the peripheral circulation.
Arterial hypotension.
Patients with acute myocardial infarction with a heart rate of less than 45 beats per minute, a PQ interval of more than 0.24 seconds, or a systolic blood pressure of less than 100 mm Hg.
With serious peripheral vascular diseases with the threat of gangrene.
Patients receiving β-blockers are contraindicated for intravenous administration of "slow" calcium channel blockers such as verapamil.
Age up to 18 years (efficacy and safety not established).
Known hypersensitivity to metoprolol and its components or to other β-blockers.

Carefully: atrioventricular block I degree, Prinzmetal's angina, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis, bronchial asthma), diabetes mellitus, severe renal failure.

Use during pregnancy and lactation Betaloc

Pregnancy: to Like most drugs, Betaloc® should not be prescribed during pregnancy and during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus. Like other antihypertensive agents, β-blockers can cause side effects, such as bradycardia in the fetus, newborn or breastfeeding children, and therefore special care should be taken when prescribing β-blockers in the last trimester of pregnancy and immediately before delivery. .

lactation period: the amount of metoprolol excreted in breast milk and the β-blocking effect in a breastfed child (when the mother takes metoprolol in therapeutic doses) are insignificant.

Dosing and Administration of Betaloc

Supraventricular tachycardia: begin administration with 5 mg (5 ml) of Betaloc at a rate of 1-2 mg/min. You can repeat the introduction with a 5-minute interval until a therapeutic effect is achieved. Usually the total dose is 10-15 mg (10-15 ml). The recommended maximum dose for intravenous administration is 20 mg (20 ml).

Prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarction or suspected of it: intravenously 5 mg (5 ml) of the drug. You can repeat the introduction with a 2-minute interval, the maximum dose is 15 mg (15 ml). 15 minutes after the last injection, oral metoprolol is prescribed at a dose of 50 mg (Betaloc) every 6 hours for 48 hours.

Impaired kidney function: there is no need to adjust the dose in patients with impaired renal function.

Impaired liver function: usually due to the low degree of binding to plasma proteins, dose adjustment is not required. However, in severe hepatic impairment (in patients with porto-caval anastomosis), a dose reduction may be required.

Elderly age: there is no need to adjust the dose in elderly patients.

Children: experience with Betaloc in children is limited.

Side effects of Betalok

Betaloc is well tolerated by patients and side effects are generally mild and reversible.

As a result of clinical studies or the use of Betaloc (metoprolol tartrate) in clinical practice, the following undesirable side effects have been described. In many cases, a causal relationship with Betaloc treatment has not been established.

The following criteria were used to evaluate the incidence of cases:

Very often (> 10%).
Often (1-9.9%).
Infrequently (0.1-0.9%).
Rarely (0.01-0.09%).
Rarely (< 0,01%).

The cardiovascular system: often - bradycardia, postural disorders (very rarely accompanied by fainting), cold extremities, palpitations; infrequently - a temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction; AV block I degree; rarely - other cardiac conduction disorders, arrhythmias; very rarely - gangrene in patients with previous severe disorders of the peripheral circulation.

CNS: very often - increased fatigue; often - dizziness, headache; rarely - increased nervous excitability, anxiety, impotence / sexual dysfunction; infrequently - paresthesia, convulsions, depression, weakening of attention, drowsiness or insomnia, nightmares; very rarely - amnesia / memory impairment, depression, hallucinations.

GIT: often - nausea, pain in the abdomen, diarrhea, constipation; infrequently - vomiting; rarely - dry mouth.

Liver: rarely - abnormal liver function.

Skin covers: infrequently - rash (in the form of urticaria), excessive sweating; rarely - hair loss; very rarely - photosensitivity, exacerbation of psoriasis.

Respiratory system: often - shortness of breath with physical effort; infrequently - bronchospasm in patients with bronchial asthma; rarely - rhinitis.

Sense organs: rarely - visual disturbances, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, taste disturbances.

Metabolism: infrequently - an increase in body weight.

From the musculoskeletal system: very rarely - arthralgia.

Blood: very rarely - thrombocytopenia.

Special instructions Betalok

Patients taking β-blockers should not be given intravenous calcium channel blockers such as verapamil. Patients with asthma or obstructive pulmonary disease should be given concomitant bronchodilator therapy. If necessary, the dose of β 2 -agonist should be increased. When using β1-blockers, the risk of their effect on carbohydrate metabolism or the possibility of masking hypoglycemia is much less than when using non-selective β-blockers.

In patients with chronic heart failure in the stage of decompensation, it is necessary to achieve a stage of compensation both before and during treatment with the drug.

Patients suffering from Prinzmetal's angina are not recommended to prescribe non-selective β-blockers.

Very rarely, patients with impaired atrioventricular conduction may worsen (possible outcome - atrioventricular block). If bradycarlia develops during treatment, the dose of Betaloc should be reduced. Metoprolol may worsen the symptoms of peripheral arterial circulation disorders due to a decrease in blood pressure. Caution should be exercised when prescribing the drug to patients suffering from severe renal insufficiency, with metabolic acidosis, co-administration with cardiac glycosides. In patients taking β-blockers, anaphylactic shock is more severe. Patients suffering from pheochromocytoma should be given an alpha-alrenoblocker in parallel with Betaloc. In the case of surgery, the anesthesiologist should be informed that the patient is taking a β-blocker. You should not prescribe a second dose - the second or third at a heart rate of less than 40 beats per minute, a PQ interval of more than 0.26 seconds and a systolic blood pressure of less than 90 mm Hg.

Drug Interactions Betalok

Co-administration of Betaloc® with the following drugs should be avoided:

Barbituric acid derivatives: barbiturates (the study was conducted with phenobarbital) slightly increase the metabolism of metoprolol, due to the induction of enzymes.

Propafenone: when prescribing propafenone to four patients treated with metoprolol, there is an increase in the plasma concentration of metoprolol by 2-5 times. while two patients had side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. Probably, the interaction is due to inhibition by propafenone, like quinidium, of the metabolism of metoprolol through the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a β-blocker, the joint appointment of metoprolol and propafenone does not seem appropriate.

Verapamil: the combination of β-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and β-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function.

Combination of Betaloc with the following drugs, which may require dose adjustment:

Class I antiarrhythmic drugs: Class I antiarrhythmics and β-blockers can lead to a summation of negative inotropic effect, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with sick sinus syndrome and impaired atrioventricular conduction. The interaction is described on the example of disopyramide.

Amiodarone: The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia. Given the extremely long half-life of amiodarone (50 days), the potential for interactions long after amiodarone withdrawal should be taken into account.

Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect of β-blockers. This interaction is best documented for indomethacin. There was no reported interaction for sulindac. In studies with diclofenac, the described reaction was not noted.

Diphenhydramine: Diphenhydramine reduces the clearance of metoprolol to α-hydroxymetoprolol by 2.5 times. At the same time, there is an increase in the action of metoprolol.

Epinephrine (adrenaline): 10 cases of severe arterial hypertension and bradycardia have been reported in patients taking non-selective β-blockers (including pindolol and proprapolol) and receiving epinephrine (adrenaline). The interaction was also noted in the group of healthy volunteers. It is assumed that similar reactions can be observed when epinephrine is used in conjunction with local anesthetics in case of accidental entry into the vascular bed. It is assumed that this risk is much lower with the use of cardioselective β-blockers.

Phenytropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, β-blockers may cause naroloxal arterial hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported while taking phenylpropanolamine.

Quinidine: Quinine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (approximately 90% of the population in Sweden), causing mainly a significant increase in the plasma concentration of metoprolol and an increase in β-blockade. It is believed that such an interaction is also characteristic of other β-blockers in the metabolism of which cytochrome P4502D6 is involved.

Clonidine: Hypertensive reactions with abrupt withdrawal of clonidine may be aggravated by the combined use of β-blockers. When used together, in case of cancellation of clonidine. discontinuation of β-blockers should begin a few days before clonidine is discontinued.

Rifampicin: Rifampicin may increase the metabolism of metoprolol, decreasing the plasma concentration of metoprolol.

Plasma concentrations of metoprolol may increase when used in combination with cimegidine, hydratazip, selective serotonin inhibitors such as paroxetine, fluoxetine and sertratine. Patients simultaneously taking metoprolol and other β-blockers (eye drops) or monoamine oxidase inhibitors (MAOIs) should be closely monitored. Against the background of taking β-blockers, inhalation anesthetics increase the cardiodepressive effect. Against the background of taking β-blockers, patients receiving oral hypoglycemic agents may require dose adjustment of the latter. Cardiac glycosides, when used together with β-blockers, can increase the time of atrioventricular conduction and cause bradycardia.

Overdose of Betaloc

Toxicity: metoprolol at a dose of 7.5 g in an adult caused intoxication with a fatal outcome. A 5-year-old child who took 100 mg of metoprolol showed no signs of intoxication after gastric lavage. Taking 450 mg of metoprolol by a 12-year-old teenager resulted in moderate intoxication. Ingestion of 1.4 g and 2.5 g of metoprolol by adults caused moderate and severe intoxication, respectively. Reception of 7.5 g for adults led to extremely severe intoxication.

Symptoms: with an overdose of metoprolol, the most serious symptoms are from the cardiovascular system, but sometimes, especially in children and adolescents, symptoms from the central nervous system and suppression of pulmonary function may predominate. Bradycardia, atrioventricular block I-lII degree, asystole, pronounced decrease in blood pressure, poor peripheral perfusion, heart failure, cardiogenic shock, lung function depression, apnea, increased fatigue, impaired consciousness, loss of consciousness, tremor, convulsions, increased sweating, paresthesia, bronchospasm , nausea, vomiting, possible esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hypercalcemia, effects on the kidneys, transient myasthenic syndrome. Concomitant use of alcohol, antihypertensive drugs, quinidine or barbiturates may worsen the patient's condition. The first signs of an overdose can be observed 20 minutes - 2 hours after taking the drug.

Treatment: the appointment of activated charcoal, if necessary, gastric lavage. IMPORTANT! Atropine (0.25–0.5 mg IV for adults, 10–20 mcg/kg for children) should be given before gastric lavage (because of the risk of vagus nerve stimulation). If necessary, maintain airway patency (intubation) and adequate ventilation of the lungs. Replenishment of circulating blood volume and infusion of glucose. ECG control. Atropine 1.0-2.0 mg IV, if necessary, repeat the introduction (especially in the case of vagal symptoms). In the case of (suppression) myocardial depression, intravenous administration of dobutamine or dopamia is indicated. Glucagon 50-150 mcg/kg IV with an interval of 1 minute can also be used. In some cases, the addition of adrenaline to therapy may be effective. With arrhythmia and an increase in the ventricular complex (QRS), sodium solutions (chloride or bicarbonate) are infused. It is possible to install an artificial pacemaker. Cardiac arrest due to an overdose may require resuscitation for several hours. Terbutaline can be used to relieve bronchospasm (by injection or by inhalation). Symptomatic treatment is carried out.

Storage conditions for Betalok

In a place protected from light, at a temperature below 25 ° C.

Keep out of the reach of children.

In an online pharmacy betaloc can be purchased with home delivery. The quality of all products in our online pharmacy, including Betaloc, undergo quality control of goods by our trusted suppliers. You can buy Betaloc on our website by clicking on the "Buy" button. We will be happy to deliver Betalok to you absolutely free of charge to any address within our delivery area.

metoprolol is a cardioselective β1-adrenergic blocker. It has a slightly pronounced membrane-stabilizing effect and does not show partial antagonist activity. Metoprolol eliminates or reduces the stimulating effect of catecholamines on the heart during physical and psycho-emotional stress, moderately reduces heart rate, myocardial contractility and cardiac output, and also reduces elevated blood pressure. At a high concentration of endogenous adrenaline, metoprolol affects the level of blood pressure to a much lesser extent than non-selective β-adrenergic blockers.

Betaloc can be given in combination with β2-agonists in patients with COPD. At therapeutic doses, Betaloc in combination with β2-agonists has a lesser effect on bronchial tone compared to non-selective β-adrenergic blockers.

Betaloc has less effect on insulin release and carbohydrate metabolism than non-selective β-blockers.

The effect of Betaloc on the response of the cardiovascular system under conditions of hypoglycemia is much less pronounced than that of non-selective β-adrenergic blockers.

Betaloc may cause a slight increase in TG levels and a decrease in serum free fatty acids. In some cases, a slight decrease in HDL levels was noted.

In / in the introduction of metoprolol in myocardial infarction can reduce the severity of pain, reduce the incidence of fibrillation and atrial fibrillation. Early initiation of therapy (within 24 hours after the onset of the first symptoms) can prevent the spread of necrosis and limit the area of infarction.

After intravenous infusion, metoprolol is rapidly distributed (within 5-10 minutes). When used at a dose of 5–20 mg, the pharmacokinetics are linear. Metoprolol is metabolized in the liver, with the formation of three metabolites without a single clinically significant effect of β-adrenergic blockers. The half-life is about 3.5 hours (1-9 hours). Only 5% of metoprolol is excreted in the urine unchanged, the rest is in the form of metabolites.

In elderly patients, the pharmacokinetics of metoprolol does not change. The systemic bioavailability and excretion rate of metoprolol does not change in patients with kidney pathology, but the rate of excretion of metabolites decreases, which has no clinical significance.

Given the low degree of binding to plasma proteins, impaired liver function does not affect the pharmacokinetics of metoprolol. But in patients with severe liver cirrhosis or portal vein bypass, the excretion of metoprolol is reduced.

Betaloc IV - indications for use

supraventricular tachyarrhythmia; myocardial ischemia, tachyarrhythmia and pain syndrome due to myocardial infarction.

Contraindications

AV block II or III degree; acute or chronic heart failure in the stage of decompensation (pulmonary edema, hypoperfusion syndrome or hypotension); inotropic therapy (long-term or intermittent), therapy aimed at stimulating β-adrenergic receptors; sinus bradycardia, sick sinus syndrome, cardiogenic shock, severe disorders of the peripheral arterial circulation. Metoprolol should not be given to patients with suspected acute myocardial infarction if heart rate is below 45 bpm, P-Q interval is more than 0.24 s, and systolic blood pressure

Usage Precautions

patients receiving beta-adrenergic blockers should not be given intravenous calcium antagonists such as verapamil. As a rule, β2-adrenergic agonists (tablets and/or aerosol) are prescribed for patients with AD as concomitant therapy. In such cases, at the beginning of treatment with Betaloc, it may be necessary to increase the dose of the β2-adrenergic agonist.

During treatment with Betaloc, the risk of impaired carbohydrate metabolism or masking symptoms of hypoglycemia is lower than with non-selective β-adrenergic blockers.

In patients with chronic heart failure, compensation of the disease should be achieved before the start of therapy with Betalok, and during the period of its use, basic therapy should be continued.

Very rarely, in patients with moderate AV conduction impairment, a complication (AV blockade) may be noted. If bradycardia occurs during treatment, the dose of Betaloc should be reduced or the drug should be gradually discontinued.

Betaloc may increase the symptoms of peripheral arterial circulation disorders, mainly due to a decrease in blood pressure.

Patients with pheochromocytoma should be prescribed α-adrenergic blockers simultaneously with Betaloc.

In the case of surgery, it is necessary to warn the anesthesiologist that the patient is taking Betaloc, but it is not recommended to stop treatment with β-adrenergic blockers.

Cancellation of the drug is carried out gradually for at least 2 weeks; abrupt cancellation is unacceptable. The dose should be halved at each stage until a daily dose of 25 mg is reached. During this period, patients, especially those with coronary artery disease, should be under constant medical supervision. During drug withdrawal, the risk of coronary disorders, including sudden death, increases.

In patients receiving β-blockers, anaphylactic shock is more severe.

Patients with BP
When treating patients with suspected or confirmed myocardial infarction, hemodynamic parameters should be carefully monitored after each intravenous administration of 5 mg Betaloc. The second or third administration of Betaloc should not be given if the heart rate
During pregnancy and breastfeeding

Like other drugs, Betaloc should not be prescribed during pregnancy and lactation, except in cases where the use of Betaloc is vital. Like all antihypertensive drugs, β-blockers can cause adverse effects such as bradycardia in the fetus, newborn or breastfeeding child. The amount of metoprolol entering breast milk does not affect the child's β-adrenergic blockers.

Influence on the ability to drive vehicles and work with potentially dangerous mechanisms

The patient should be aware of his reaction to treatment with Betalok, as phenomena such as dizziness and weakness are possible.

Interaction with drugs

patients should be under medical supervision if they receive ganglioblockers, other β-adrenergic receptor blockers (eg eye drops) or monoamine oxidase inhibitors (i-MAO) simultaneously with Betaloc.

If it is necessary to cancel concomitant treatment with clonidine, the β-adrenergic blocker should be discontinued a few days before clonidine is discontinued.

In patients receiving verapamil-type calcium antagonists and / or drugs for the treatment of arrhythmias simultaneously with Betalok, negative ino- and chronotropic effects are possible, and the appointment of intravenous verapamil in such patients is contraindicated due to the risk of cardiac arrest. β-adrenergic blockers can enhance the negative ino- and chronotropic effects of drugs for the treatment of arrhythmias (quinidine analogues or amiodarone).

In patients receiving β-adrenergic blockers, inhalation anesthetics increase the cardiodepressive effect. Inducers or inhibitors of metabolism can affect the plasma concentration of metoprolol, which decreases with rifampicin and may increase with cimetidine, alcohol, hydralazine and serotonin reuptake inhibitors (paroxetine, fluoxetine and sertraline).

With concomitant treatment with indomethacin or other drugs that inhibit prostaglandin synthetase, the antihypertensive effect of β-adrenergic blockers may decrease. Cardioselective β-adrenergic blockers have a much lesser effect on blood pressure when adrenaline is administered to patients than non-selective β-adrenergic receptor blockers.

With the concomitant use of β-adrenergic blockers, dose adjustment of oral antidiabetic agents may be necessary.

Betaloc IV - method of administration and dosage

parenteral administration of Betaloc should be carried out by specially trained personnel in the presence of cardiorespiratory monitoring and the possibility of resuscitation.

Supraventricular tachyarrhythmia

The initial dose of the drug is 5 mg (5 ml of solution), the infusion rate is 1–2 mg / min. At this dose, the drug can be administered every 5 minutes until the desired effect is achieved. As a rule, 10–15 mg (10–15 ml of solution) is sufficient to achieve the desired effect. The maximum dose for intravenous administration is 20 mg (20 ml of solution).

Treatment of myocardial ischemia and pain syndrome due to myocardial infarction

In uncomplicated conditions, the initial dose is 5 mg (5 ml of solution) IV. The introduction of the drug can be repeated every 2 minutes, the maximum dose is 15 mg (15 ml of solution). 15 minutes after the last intravenous injection, 50 mg of metoprolol tartrate should be administered orally every 6 hours for 2 days. For long-term treatment, metoprolol tablets (eg Betaloc ZOK, sustained release tablets) should be prescribed.

Use in patients with renal insufficiency

In kidney disease, there is no need for dose adjustment.

Use in patients with hepatic insufficiency

Usually, patients with cirrhosis of the liver do not need to adjust the dose; in case of severe hepatic impairment, it may be necessary to reduce the dose.

Use in elderly patients

There is no need to reduce the dose.

Use in children

There is limited experience with Betaloc injection in children.

Side effects

Usually Betaloc is well tolerated. Side effects are minor and reversible. When using Betaloc, the following side effects were reported:

From the side of the cardiovascular system: often - bradycardia, postural disorders (very rarely - loss of consciousness), cold extremities, a feeling of increased heart rate, increased symptoms of heart failure, AV blockade, edema, pain in the heart area; rarely - cardiac disorders, arrhythmia, edema; very rarely - gangrene in patients with existing severe peripheral circulatory disorders.

From the side of the central nervous system: fatigue, dizziness, headache; sometimes - paresthesia, convulsions.

From the digestive tract: nausea, abdominal pain, diarrhea, constipation; rarely - vomiting, dry mouth.

On the part of the blood system: very rarely - thrombocytopenia.

Liver: rarely - deviations of liver parameters; very rarely - hepatitis.

From the musculoskeletal system: very rarely - arthralgia.

On the part of metabolism: weight gain.

Mental status: sometimes depression, decreased concentration, drowsiness or insomnia, nightmares; rarely - nervousness, anxiety, very rarely - amnesia / memory impairment, confusion, hallucinations.

On the part of the respiratory system: shortness of breath during physical exertion; sometimes - bronchospasm; rarely - rhinitis.

From the sensory organs: rarely - visual disturbances, dryness and / or irritation of the eyes, conjunctivitis; very rarely - tinnitus, taste disturbances.

From the skin: rashes, excessive sweating, hair loss; very rarely - photosensitivity, exacerbation of psoriasis.

Others: impotence/sexual dysfunction.

Overdose

Symptoms: severe hypotension, sinus bradycardia, AV block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impaired consciousness, coma, nausea, vomiting, and cyanosis. The simultaneous use of alcohol, drugs to lower blood pressure, quinidine or barbiturates can complicate the patient's condition.

Treatment: symptomatic therapy. In severe hypotension, bradycardia, and heart failure, β1-adrenergic stimulants (eg, prenalterone) are given intravenously at intervals of 2–5 minutes or as an infusion until the desired effect is achieved. In the absence of β1-adrenergic stimulants, dopamine can be used; for blockade of the vagus nerve, intravenous atropine sulfate is used. If the desired effect is not achieved, other sympathomimetics such as dobutamine or norepinephrine are used, glucagon is prescribed at a dose of 1–10 mg. It may be necessary to use a pacemaker. When bronchospasm occurs, β2-adrenergic stimulants are administered intravenously. It should be remembered that the doses of drugs (antidotes) required to treat an overdose of β-adrenergic blockers should be higher than therapeutic ones, since β-adrenergic receptors are occupied by their blocker.