BETALOK ZOK TABLE 25 MG No. 14

Pharmacological properties of the drug Betaloc zok

Metoprolol is a competitive cardioselective β1-adrenergic receptor blocker. It has a slightly pronounced membrane-stabilizing effect and does not have partial agonist activity. Metoprolol eliminates or reduces the stimulating effect of catecholamines on the heart during physical and psychoemotional stress, reduces heart rate, moderately reduces myocardial contractility and cardiac output, and also reduces high blood pressure. Reduces myocardial oxygen demand and increases diastole. At high concentrations of endogenous adrenaline, metoprolol affects blood pressure to a much lesser extent than non-selective beta-adrenergic receptor blockers. Unlike traditional tablet dosage forms, when using Betaloc ZOK tablets with a delayed release of the active substance, a constant concentration of the drug in the blood plasma is observed and a stable clinical effect is ensured (blockade of β1-adrenergic receptors) for more than 24 hours. Due to the absence of concentration peaks in the blood plasma Betaloc ZOK is characterized by better clinical tolerability than conventional tablet forms of β1-adrenergic receptor blockers - the potential risk of side effects that are observed at peak plasma concentrations of the drug, such as bradycardia and weakness in the lower extremities when walking, is significantly reduced. If necessary, Betaloc ZOK can be prescribed in combination with β2-adrenergic receptor agonists to patients with COPD. In therapeutic doses, metoprolol in combination with β2-adrenergic receptor agonists has a lesser effect on bronchial tone compared to non-selective β-adrenergic receptor blockers. Betaloc ZOK has a lesser effect on insulin release and carbohydrate metabolism than non-selective beta-adrenergic receptor blockers. The effect of Betaloc ZOK on the response of the cardiovascular system in conditions of hypoglycemia is much less pronounced than that of non-selective beta-adrenergic receptor blockers. Clinical studies have shown that Betaloc ZOK may cause a slight increase in TG levels and a decrease in plasma free fatty acid levels. In some cases, a slight decrease in the HDL fraction was noted, but it was less significant compared to taking non-selective β1-adrenergic receptor blockers. However, one long-term clinical study showed a significant reduction in total cholesterol levels after treatment with metoprolol for several years. In the MERIT-HF study (Effect of Metoprolol Therapy on Survival in NYHA Class II–IV Heart Failure with Reduced Ejection Fraction (≤40%)), which included 3991 patients, metoprolol therapy resulted in a reduction in mortality and hospitalization. With long-term treatment, patients showed an improvement in their condition and a decrease in the functional class of heart failure according to NYHA. Metoprolol therapy led to an increase in left ventricular ejection fraction and a decrease in left ventricular end-systolic and diastolic volumes. Betaloc ZOK is completely absorbed after oral administration. Absorption of the drug does not depend on food intake. Due to active metabolism during first pass through the liver, the systemic bioavailability of metoprolol after oral administration is approximately 50%. When the sustained-release formulation of metoprolol is used, its bioavailability is reduced by approximately 20–30% compared to conventional tablets, but this is not clinically significant because the sustained-release formulation has the same AUC as the conventional tablet. Metoprolol is characterized by a low degree of binding to plasma proteins (approximately 5–10%). Metoprolol is metabolized in the liver, producing three metabolites that do not have β-adrenergic blocking activity. More than 95% of the drug dose taken orally is excreted in the urine, 5% is excreted unchanged. In some cases, the amount of the drug that is excreted unchanged in the urine can reach 30%. The mean half-life is 3.5 hours (1–9 hours). The total plasma clearance is approximately 1 l/min. In elderly patients, significant changes in the pharmacokinetics of metoprolol are not observed. Systemic bioavailability and excretion of metoprolol do not change in patients with renal failure, but the excretion of metabolites in such patients is reduced. Significant accumulation of metabolites was observed in patients with a glomerular filtration rate of less than 5 ml/min. Such accumulation of metabolites does not have a β-adrenergic blocking effect. In patients with reduced liver function, the pharmacokinetics of metoprolol (due to low protein binding) changes slightly, however, in patients with severe liver cirrhosis or portacaval shunts, the bioavailability of metoprolol may be increased and overall clearance may be decreased. In patients with a portacaval shunt, the total clearance of metoprolol is approximately 0.3 l/min, and the AUC value is approximately 6 times higher than that in healthy individuals.

Betaloc zok 25 mg 14 pcs. sustained release coated tablets

pharmachologic effect

Beta1-adrenergic blocker selective.

Composition and release form Betaloc zok 25 mg 14 pcs. sustained release coated tablets

Tablets - 1 tablet:

Active substance: 23.75 mg of metoprolol succinate, which corresponds to 19.5 mg of metoprolol and 25 mg of metoprolol tartrate;
Excipients: ethylcellulose 21.5 mg, hyprolose 6.13 mg, hypromellose 5.64 mg, microcrystalline cellulose 94.9 mg, paraffin 0.06 mg, macrogol 1.41 mg, silicon dioxide 14.6 mg, sodium stearyl fumarate 0.241 mg, titanium dioxide 1.41 mg.

14 tablets in an aluminum/PVC blister, in a cardboard box with instructions for use.

Description of the dosage form

Oval, biconvex, white or almost white, film-coated tablets; with a notch on both sides and an A β engraving on one side.

Characteristic

Tablets are white to off-white, round, scored on one side and engraved on the other side.

Directions for use and doses

Betaloc® ZOK is intended for daily use once a day; it is recommended to take the drug in the morning. The Betaloc® ZOK tablet should be swallowed with liquid. Tablets (or halved tablets) should not be chewed or crushed. Food intake does not affect the bioavailability of the drug.

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

Arterial hypertension

50-100 mg once a day. If necessary, the dose can be increased to 100 mg per day or another antihypertensive agent can be added, preferably a diuretic and a calcium antagonist of the dihydropyridine series.

Angina pectoris

100-200 mg Betaloc® ZOK once a day. If necessary, another antianginal drug may be added to therapy.

Stable symptomatic chronic heart failure with impaired left ventricular systolic function

Patients must be in stable chronic heart failure without episodes of exacerbation during the last 6 weeks and without changes in primary therapy during the last 2 weeks.

Treatment 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; in some cases, it may be necessary to discontinue the drug.

Stable chronic heart failure, functional class II

The recommended initial dose of Betaloc® ZOK for the first 2 weeks is 25 mg once a day. After 2 weeks of therapy, the dose can be increased to 50 mg once daily, and then can be doubled every 2 weeks.

The maintenance dose for long-term treatment is 200 mg Betaloc® ZOK once a day.

Stable chronic heart failure, III-IV functional class

The recommended initial dose for the first 2 weeks is 12.5 mg Betaloc® ZOK (half a 25 mg tablet) once a day. The dose is selected individually. During the dosage increase period, the patient should be monitored as symptoms of heart failure may worsen in some patients.

After 1-2 weeks, the dose can be increased to 25 mg Betaloc® ZOK once a day. Then, after 2 weeks, the dose can be increased to 50 mg once daily. For patients who tolerate the drug well, the dose can be doubled every 2 weeks until a maximum dose of 200 mg Betaloc® ZOK is reached once a day.

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, the dose should not be increased until the condition has stabilized. Monitoring of renal function may be required.

Heart rhythm disturbances

100-200 mg Betaloc® ZOK once a day.

Maintenance treatment after myocardial infarction

200 mg Betaloc® ZOK once a day.

Functional cardiac disorders accompanied by tachycardia

100 mg Betaloc® ZOK once a day. If necessary, the dose can be increased to 200 mg per day.

Preventing migraine attacks

100-200 mg Betaloc® ZOK once a day.

Renal dysfunction

There is no need to adjust the dose in patients with impaired renal function.

Liver dysfunction

Usually, due to the low degree of binding to plasma proteins, no dose adjustment of metoprolol is required. However, in severely impaired liver function (in patients with severe liver cirrhosis or portacaval anastomosis), a dose reduction may be required.

Elderly age

Pharmacodynamics

Metoprolol is a β1-blocker that blocks β1 receptors in doses significantly lower than the doses required to block β2 receptors.

Metoprolol has a slight membrane-stabilizing effect and does not exhibit partial agonist activity.

Metoprolol reduces or inhibits the agonistic effect that catecholamines, released during nervous and physical stress, have on cardiac activity. This means that metoprolol has the ability to prevent the increase in heart rate (HR), cardiac output and contractility, as well as the increase in blood pressure (BP), caused by a sharp release of catecholamines.

Unlike conventional tablet dosage forms of selective β1-blockers (including metoprolol tartrate), when using the drug Betaloc® ZOK, a constant concentration of the drug in the blood plasma is observed and a stable clinical effect (β1-blockade) is ensured for more than 24 hours.

Due to the absence of obvious peak plasma concentrations, clinically Betaloc® ZOK is characterized by better β1-selectivity compared to conventional tablet forms of β1-blockers. In addition, the potential risk of side effects observed at peak plasma concentrations, such as bradycardia and weakness in the legs when walking, is significantly reduced.

Patients with symptoms of obstructive pulmonary diseases, if necessary, can be prescribed Betaloc® ZOK in combination with β2-adrenergic agonists. When used together with β2-adrenergic agonists, Betaloc® ZOK in therapeutic doses has a lesser effect on bronchodilation caused by β2-adrenergic agonists than non-selective β-blockers. Metoprolol affects insulin production and carbohydrate metabolism to a lesser extent than non-selective β-blockers. The effect of the drug on the response of the cardiovascular system in conditions of hypoglycemia is much less pronounced compared to non-selective β-blockers.

The use of Betaloc® ZOK for arterial hypertension leads to a significant decrease in blood pressure for more than 24 hours both in the supine and standing positions, and during exercise. At the beginning of metoprolol therapy, an increase in vascular resistance is observed. However, with long-term use, a decrease in blood pressure is possible due to a decrease in vascular resistance while cardiac output remains unchanged.

In MERIT-HF (a survival study in chronic heart failure (NYHA class II-IV) and reduced cardiac ejection fraction (≤ 0.40), which included 3991 patients), Betaloc® ZOK showed an increase in survival and a decrease in the frequency of hospitalizations. With long-term treatment, patients achieved overall improvement in symptoms (according to NYHA classes). Also, therapy with Betaloc® ZOK showed an increase in left ventricular ejection fraction, a decrease in end-systolic and end-diastolic volumes of the left ventricle.

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

Pharmacokinetics

Upon contact with liquid, the tablets quickly disintegrate, dispersing the active substance in the gastrointestinal tract. The rate of release of the active substance depends on the acidity of the medium. The duration of the therapeutic effect after taking the drug in the dosage form of Betaloc® ZOK (slow-release tablets) is more than 24 hours, while a constant rate of release of the active substance is achieved within 20 hours. The half-life averages 3.5 hours.

Betaloc® ZOK is completely absorbed after oral administration. Systemic bioavailability after oral administration of a single dose is approximately 30-40%.

Metoprolol undergoes oxidative metabolism in the liver. The three main metabolites of metoprolol did not exhibit a clinically significant β-blocking effect. About 5% of the oral dose of the drug is excreted unchanged in the urine, the rest of the drug is excreted in the form of metabolites. The binding to plasma proteins is low, approximately 5-10%.

Indications for use Betaloc zok 25 mg 14 pcs. sustained release coated tablets

Arterial hypertension;
angina pectoris;
stable symptomatic chronic heart failure with impaired left ventricular systolic function (as an adjuvant therapy to the main treatment of chronic heart failure);
reduction in mortality and recurrent infarction after the acute phase of myocardial infarction;
heart rhythm disturbances, including supraventricular tachycardia, decreased ventricular contraction frequency with atrial fibrillation and ventricular extrasystoles;
functional disorders of cardiac activity accompanied by tachycardia;
prevention of migraine attacks.

Contraindications

Atrioventricular block II and III degrees, heart failure in the stage of decompensation, continuous or intermittent therapy with inotropic drugs acting on beta-adrenergic receptors, clinically significant sinus bradycardia, sick sinus syndrome, cardiogenic shock, severe peripheral circulatory disorders, including those at risk gangrene, arterial hypotension.

Betaloc® ZOK is contraindicated in patients with suspected 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 mmHg.

Known hypersensitivity to metoprolol and its components or to other beta-blockers.

In patients receiving β-blockers, intravenous administration of slow calcium channel blockers such as verapamil is contraindicated.

Age up to 18 years (efficacy and safety have not been established).

With caution: first degree atrioventricular block, Prinzmetal's angina, bronchial asthma, chronic obstructive pulmonary disease, diabetes mellitus, severe liver failure, severe renal failure, metabolic acidosis, co-administration with cardiac glycosides.

Application of Betaloc zok 25 mg 14 pcs. slow-release tablets, coated during pregnancy and lactation

Like most drugs, Betaloc® ZOK should not be prescribed during pregnancy and breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and/or child. Like other antihypertensive agents, beta-blockers may cause side effects such as bradycardia in the fetus, neonates, or breast-fed children.

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 negligible.

special instructions

Patients taking β-blockers should not receive intravenous calcium channel blockers such as verapamil.

Patients with bronchial asthma or chronic obstructive pulmonary disease should be prescribed concomitant therapy with a β2-agonist. It is necessary to prescribe the minimum effective dose of Betaloc® ZOK, and an increase in the dose of the β2-adrenergic agonist may be required.

It is not recommended to prescribe non-selective beta-blockers to patients with Prinzmetal's angina. In this group of patients, beta-selective blockers should be prescribed with caution.

When using β1-blockers, the risk of their influence on carbohydrate metabolism or the possibility of masking the symptoms of hypoglycemia is significantly 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.

Very rarely, patients with impaired AV conduction may experience deterioration (a possible outcome is AV block).

If bradycardia develops during treatment, the dose of the drug should be reduced or the drug should be gradually discontinued.

Betaloc® ZOK can aggravate the course of existing peripheral circulatory disorders, mainly due to a decrease in blood pressure.

Caution should be exercised when prescribing the drug to patients with severe renal failure, metabolic acidosis, and simultaneous use with cardiac glycosides.

In patients taking β-blockers, anaphylactic shock occurs in a more severe form.

The use of epinephrine (adrenaline) in therapeutic doses does not always lead to the achievement of the desired clinical effect while taking metoprolol.

Patients with pheochromocytoma should be prescribed an alpha-blocker simultaneously with Betaloc® ZOK.

Abrupt withdrawal of beta-blockers is dangerous, especially in high-risk patients, and should therefore be avoided. If it is necessary to discontinue the drug, it should be done gradually over at least 2 weeks, with a twofold reduction in the dose of the drug at each stage, until a final dose of 12.5 mg (1/2 tablet of 25 mg) is reached, which should be taken at least 4 days until the drug is completely discontinued. If symptoms occur (eg, worsening angina symptoms, increased blood pressure), a slower withdrawal regimen is recommended.

Abrupt withdrawal of a beta-blocker may worsen the course of chronic heart failure and increase the risk of myocardial infarction and sudden death.

In case of surgery, the anesthesiologist should be informed that the patient is taking Betaloc® ZOK. In patients undergoing surgery, discontinuation of β-blocker therapy is not recommended. Prescribing high doses without prior titration of the drug should be avoided in patients with cardiovascular risk factors undergoing non-cardiac surgery due to the increased risk of bradycardia, arterial hypotension and stroke, including death.

Clinical trial data on efficacy and safety in patients with severe stable symptomatic chronic heart failure (NYHA class IV) are limited.

Such patients should be treated by physicians with specialized knowledge and experience.

Patients with symptomatic heart failure combined with acute myocardial infarction and unstable angina were excluded from studies based on which indications for use were determined. The effectiveness and safety of the drug for this group of patients has not been described.

Use in unstable heart failure in the decompensation stage is contraindicated.

Impact on the ability to drive vehicles and operate machinery

When driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, it should be taken into account that dizziness and fatigue may occur when using Betalok® ZOK.

Overdose

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. Administration of 1.4 g and 2.5 g of metoprolol to adults caused moderate and severe intoxication, respectively. Taking 7.5 g by adults resulted in extremely severe intoxication.

Symptoms: in case of an overdose of metoprolol, the most serious symptoms are those from the cardiovascular system, but sometimes, especially in children and adolescents, symptoms from the central nervous system and suppression of pulmonary function, bradycardia, AV block I-III degree, asystole, marked decrease in blood pressure may predominate. , poor peripheral perfusion, heart failure, cardiogenic shock; depression of pulmonary function, apnea, as well as increased fatigue, impaired consciousness, loss of consciousness, tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, possible esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia; 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: administration of activated carbon, gastric lavage if necessary. IMPORTANT! Atropine (0.25-0.5 mg IV for adults, 10-20 mcg/kg for children) should be given before gastric lavage (due to the risk of vagus nerve stimulation). If necessary, maintain a patent airway (intubation) and provide adequate ventilation. Replenishment of circulating blood volume and glucose infusion. ECG monitoring. Atropine 1.0-2.0 mg IV, repeat administration if necessary (especially in case of vagal symptoms). In case of (suppression of) myocardial depression, infusion of dobutamine or dopamine is indicated. Glucagon 50-150 mcg/kg IV can also be used at intervals of 1 minute. In some cases, adding epinephrine to therapy may be effective. For arrhythmia and a wide ventricular (QRS) complex, 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 (injected or inhaled) can be used to relieve bronchospasm. Symptomatic treatment is carried out.

Side effects Betaloc zok 25 mg 14 pcs. sustained release coated tablets

Betaloc® ZOK is well tolerated by patients, side effects are mostly mild and reversible.

To assess the frequency of cases, the following criteria were used: very often (>10%), often (1-9.9%), infrequently (0.1-0.9%), rarely (0.01-0.09%) and very rarely (

Cardiovascular system - Often: bradycardia, orthostatic hypotension (very rarely accompanied by fainting), cold extremities, palpitations; Uncommon: temporary increase in symptoms of heart failure, 1st degree AV block; cardiogenic shock in patients with acute myocardial infarction, swelling, pain in the heart area; Rarely: other conduction disorders, arrhythmias; Very rare: gangrene in patients with previous severe peripheral circulatory disorders.

Central nervous system - Very common: increased fatigue; Common: dizziness, headache; Uncommon: paresthesia, convulsions, depression, decreased concentration, drowsiness or insomnia, nightmares; Rarely: increased nervous excitability, anxiety; Very rare: amnesia/memory impairment, depression, hallucinations.

Gastrointestinal tract - Often: nausea, abdominal pain, diarrhea, constipation; Uncommon: vomiting; Rarely: dryness of the oral mucosa.

Liver - Rarely: liver dysfunction; Very rare: hepatitis.

Skin - Uncommon: skin rash (like psoriasis-like urticaria), increased sweating; Rarely: hair loss; Very rare: photosensitivity, exacerbation of psoriasis.

Respiratory organs - Often: shortness of breath on exertion; Uncommon: bronchospasm; Rarely: rhinitis.

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

From the musculoskeletal system - Very rarely: arthralgia.

Metabolism - Uncommon: weight gain.

Blood - Very rare: thrombocytopenia.

Other - Rare: impotence/sexual dysfunction.

Drug interactions

Metoprolol is a CYP2D6 substrate, and therefore drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) may affect the plasma concentrations of metoprolol.

The combined use of Betaloc® ZOK with the following drugs should be avoided:

Barbituric acid derivatives: barbiturates (study conducted with pentobarbital) increase the metabolism of metoprolol due to enzyme induction.

Propafenone: When propafenone was prescribed to four patients treated with metoprolol, an increase in plasma concentrations of metoprolol was observed by 2-5 times, while two patients experienced side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. The interaction is likely due to propafenone's inhibition, like quinidine, of the metabolism of metoprolol via the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a beta-blocker, the joint 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 β-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function.

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

Amiodarone: Concomitant use of amiodarone and metoprolol may result in severe sinus bradycardia. Given the extremely long half-life of amiodarone (50 days), a possible interaction should be considered long after discontinuation of amiodarone.

Class I Antiarrhythmics: Class I antiarrhythmics and β-blockers may result in additive negative inotropic effects, 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 AV conduction. The interaction is described using disopyramide as an example.

Nonsteroidal anti-inflammatory drugs (NSAIDs): NSAIDs reduce the antihypertensive effect of beta-blockers. This interaction has been documented for indomethacin. It is likely that the described interaction will not be observed with sulindac. Negative interactions have been noted in studies with diclofenac.

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

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

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 observed in the group of healthy volunteers. It is assumed that similar reactions can be observed when epinephrine is used together with local anesthetics if it accidentally enters the vascular bed. It is assumed that this risk is much lower with the use of cardioselective beta-blockers.

Phenylpropanolamine: 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 paradoxical hypertension reactions 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 (in Sweden, approximately 90% of the population), causing mainly a significant increase in plasma concentrations of metoprolol and increased beta-blockade. It is believed that a similar interaction is typical for other β-blockers, the metabolism of which involves cytochrome P4502D6.

Clonidine: Hypertensive reactions during abrupt withdrawal of clonidine may be exacerbated by concomitant use of beta-blockers. When used together, if clonidine is discontinued, discontinuation of β-blockers should begin several days before discontinuation of clonidine.

Rifampicin: Rifampicin may increase the metabolism of metoprolol, reducing plasma concentrations of metoprolol.

Patients concomitantly taking metoprolol and other β-blockers (eye drops) or monoamine oxidase inhibitors (MAOIs) should be closely monitored.

When taking β-blockers, inhalational anesthetics enhance the cardiodepressive effect.

While taking β-blockers, patients receiving oral hypoglycemic agents may require dose adjustment of the latter.

Plasma concentrations of metoprolol may increase when taking cimetidine or hydralazine.

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

Indications for use of the drug Betaloc zok

arterial hypertension (AH) (to reduce blood pressure and the risk of developing coronary and other cardiovascular complications, as well as cardiovascular and coronary death, including sudden death);
angina pectoris;
compensated chronic heart failure with impaired left ventricular systolic function (as an addition to the basic treatment of heart failure);
in order to reduce mortality and the incidence of recurrent infarction after the acute phase of myocardial infarction;
heart rhythm disturbances, including supraventricular tachycardia, as well as to reduce the frequency of ventricular contractions during atrial fibrillation and ventricular extrasystoles;
functional disorders of cardiac activity;
migraine prevention.

Use of the drug Betaloc zok

Betaloc ZOK is intended for daily use once a day, preferably in the morning. Tablets (or tablets split in half) should not be chewed or crushed. Food intake does not affect the bioavailability of the drug. During dose selection, heart rate should be monitored to prevent bradycardia. Hypertension (arterial hypertension) The recommended dose of Betaloc ZOK for patients with mild or moderate hypertension (arterial hypertension) is 50 mg 1 time per day. If the therapeutic effect is not achieved, the dose should be increased to 100–200 mg once a day or combined with other antihypertensive drugs. Angina pectoris The recommended dose is 100–200 mg Betaloc ZOK 1 time per day. If necessary, Betaloc ZOK can be combined with other drugs for the treatment of angina. Stable chronic heart failure with impaired left ventricular systolic function (as an addition to basic therapy) Patients must be in the stage of compensated chronic heart failure for at least 6 weeks; basic therapy should not change during the last 2 weeks. Treatment of heart failure with β-adrenergic blockers may lead to transient clinical deterioration. Further continuation of therapy or dose reduction is possible; in some cases, discontinuation of the drug may be necessary. Initiation of therapy with Betaloc ZOK in patients with severe heart failure (NYHA IV) should be carried out by an experienced physician experienced in treating patients with heart failure. Stable chronic heart failure, functional class II The recommended initial dose of Betaloc ZOK for the first 2 weeks is 25 mg (1 tablet of 25 mg or tablets of 50 mg) 1 time per day. After 2 weeks, the dose can be increased to 50 mg once a day and then can be doubled every 2 weeks. The optimal dose for long-term treatment is 200 mg Betaloc ZOK 1 time per day. Stable chronic heart failure, functional class III-IV The dose is selected individually. The recommended initial dose for the first 2 weeks is 12.5 mg Betaloc ZOK (1/2 tablet of 25 mg) 1 time per day. During the period of increasing the dose, the patient should be under the supervision of a physician, as in some cases the symptoms of heart failure may intensify. After 2 weeks of taking Betaloc ZOK at a dose of 12.5 mg, the dose can be increased to 25 mg (1 tablet of 25 mg or tablets of 50 mg) once a day. After 2 weeks, the dose can be increased to 50 mg once a day. For patients who tolerate higher doses well, the dose can be doubled every 2 weeks until a maximum dose of 200 mg Betaloc ZOK is reached once a day. In case of hypotension and/or bradycardia, it is necessary to reduce the dose of Betaloc ZOK or concomitant medications. Hypotension at the beginning of therapy does not necessarily indicate that such a dose of Betaloc ZOK will not be tolerated in the future. However, the dose should not be increased until the patient's condition has stabilized. Monitoring of kidney function is necessary. Cardiac arrhythmias The recommended dose is 100–200 mg Betaloc ZOK 1 time per day. Maintenance therapy after myocardial infarction It has been shown that as a result of long-term treatment with Betalok ZOK at a dose of 200 mg per day, the risk of death (including sudden death) is reduced, and the risk of recurrent myocardial infarction is reduced (including in patients with diabetes mellitus). Functional cardiac disorders accompanied by palpitations The recommended dose is 100 mg Betaloc ZOK 1 time per day. If necessary, the dose can be increased to 200 mg. Prevention of migraine The recommended dose is 100–200 mg Betaloc ZOK 1 time per day. Patients with impaired renal function No dose adjustment is required in patients with impaired renal function. Patients with impaired liver function Betaloc ZOK is usually prescribed to patients with liver cirrhosis at the same dose as patients with normal liver function. Only in case of severe liver failure is it possible to reduce the dose. Elderly patients No dose adjustment is required. Children Experience with the use of Betaloc ZOK in children is limited.

Reviews of Betaloka ZOK

Reviews of Betalok ZOK indicate that quite often after its use undesirable symptoms occur. Thus, patients often report cases of rhinitis . Some also complain of irregular pulse and instability of blood pressure . Because of this, specialists prescribe additional medications that are designed to eliminate these side effects. However, it should be noted that most people still tolerate this medication easily.

In addition, reviews of Betalok ZOK draw attention to the fact that the selection of dosages should be approached with particular care. The patient’s condition must be constantly monitored and the danger of deterioration must be eliminated in a timely manner.

Contraindications for Betaloc zok

AV blockade II–III degree; heart failure in the decompensation phase (pulmonary edema, hypoperfusion syndrome or arterial hypotension), simultaneous (long-term or periodic) therapy with inotropic agents aimed at stimulating β-adrenergic receptors; clinically significant sinus bradycardia, sick sinus syndrome, cardiogenic shock, severe peripheral arterial circulation disorders. Metoprolol should not be prescribed to patients with suspected acute myocardial infarction with a heart rate less than 45 per minute, a P-Q on the ECG of more than 0.24 s, or a systolic blood pressure level of less than 100 mmHg. Art. Hypersensitivity to any component of the drug or to other beta-adrenergic receptor blockers.

Side effects of the drug Betaloc zok

Well tolerated, side effects are usually mild and reversible. Side effects according to the frequency of occurrence are distributed as follows: very often - at least 10%, often - 1-9%, infrequently - 0.1%, rarely - 0.01-0.09%, very rarely - less than 0.01% . From the cardiovascular system Often: bradycardia, postural disturbances (extremely with dizziness), coldness of the extremities; uncommon: temporary worsening of symptoms of heart failure, 1st degree AV block, edema, pain in the heart area; rarely: sinoatrial conduction disturbance, arrhythmia; very rare: gangrene in patients with severe peripheral circulatory disorders. From the side of the central nervous system Very often: increased fatigue; often: dizziness, headache; uncommon: paresthesia, muscle cramps. From the gastrointestinal tract Often: nausea, abdominal pain, diarrhea, constipation; uncommon: vomiting; rarely: dry mouth. From the blood system : Very rare: thrombocytopenia. From the hepatobiliary system Rarely: changes in functional liver parameters; very rare: hepatitis. From the musculoskeletal system Very rare: arthralgia. Metabolic disorders : Uncommon: weight gain. Mental status: Uncommon: depression, decreased concentration, drowsiness or insomnia, nightmares; rarely: increased excitability, anxiety; very rarely: amnesia and other memory impairments, confusion, hallucinations. From the respiratory system Often: shortness of breath with physical effort; not often: bronchospasm; rarely: rhinitis. From the senses : Rarely: visual disturbances, dryness and/or irritation of the eyes, conjunctivitis; very rarely: taste disturbances, tinnitus. Skin disorders Uncommon: rash (urticaria, areas of skin dystrophy), increased sweating; rarely: hair loss; very rarely: photosensitivity, exacerbation of psoriasis. Other Impotence, sexual dysfunction.

Special instructions for the use of the drug Betaloc zok

Patients taking beta-blockers should not receive intravenous verapamil-type calcium antagonists. As a rule, when treating patients with asthma, β2-adrenergic receptor agonists (in tablets or aerosol) are prescribed as concomitant therapy. In cases where these patients begin to take Betaloc ZOK, an increase in the dose of β2-adrenergic receptor agonists may be necessary. The risk that Betaloc ZOK will affect β2-adrenergic receptors is lower than in the case of the use of conventional non-selective β1-adrenergic receptor blockers in tablets. Betaloc ZOK has a lesser effect on insulin release and carbohydrate metabolism than non-selective beta-adrenergic receptor blockers. In patients with chronic heart failure, compensation for the disease should be achieved before starting the use of Betaloc ZOK, and during its use they should be under medical supervision. In extremely rare cases, the condition of patients with moderate AV conduction disorders may worsen (possible development of complete AV block). If bradycardia develops during treatment, the dose of Betaloc ZOK should be reduced or the use of the drug should be gradually discontinued. Betaloc ZOK may increase the severity of peripheral arterial circulatory disorders by reducing blood pressure. Patients with pheochromocytoma should be prescribed an α-adrenergic receptor blocker simultaneously with Betaloc ZOK. When performing surgery, it is necessary to warn the anesthesiologist that the patient is taking Betaloc ZOK. However, it is not recommended to discontinue treatment with beta-adrenergic blockers in patients scheduled for surgery. Data on the effectiveness and safety of the drug in patients with severe stable heart failure (NYHA functional class IV) are limited. These patients must be treated by physicians with specialized skills and experience. Abrupt discontinuation of β-adrenergic blockers should be avoided, as this may worsen heart failure and also increase the risk of myocardial infarction and sudden cardiac death. If treatment must be stopped, this should be done as gradually as possible, over a period of at least 2 weeks under medical supervision. The dose is reduced by half at each stage. The last dose (12.5 mg) should be taken for at least 4 days until the drug is completely discontinued. If symptoms return, it is recommended to slow down the dose reduction. Anaphylactic shock in patients taking metoprolol is more severe. Pregnancy and lactation Betaloc ZOK can be prescribed during pregnancy only if the expected therapeutic effect for the mother outweighs the potential risk to the fetus. β-adrenergic receptor blockers can cause the development of bradycardia in the fetus and newborn, which should be taken into account when prescribing the drug in the third trimester of pregnancy, as well as during childbirth. It is unlikely that metoprolol prescribed to the mother in therapeutic doses will have a negative effect on the infant. Effect on the ability to drive vehicles and work with potentially dangerous mechanisms Since dizziness and weakness may develop when using the drug, caution should be exercised when driving vehicles and working with potentially dangerous mechanisms.

Betaloka ZOK price, where to buy

The average price of Betaloc ZOK 50 mg is 270 rubles, the price of 25 mg is 160 rubles, and the average cost of 100 mg of the drug is 370 rubles.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine

ZdravCity

Betaloc ZOK tablets p.p.o.
with deceleration release 100 mg 30 pcs. AstraZeneca AB / Astra Zeneca Industries LLC 431 rub. order
Betaloc ZOK tablets p.p.o. with deceleration release 50 mg 30 pcs. Astra Zeneca AB/LLC Astra Zeneca Industries
RUB 286 order
Betaloc ZOK tablets p.p.o. with deceleration release 25 mg 14 pcs. AstraZeneca AB / ZiO-Zdorovye / Astra Zeneca Industries LLC
RUB 153 order

Pharmacy Dialogue

Betalok Zok (tablet p/o 100 mg No. 30)Astra Zeneсa/AstraZeneca Industries
RUB 385 order
Betaloc Zok tablets 25 mg No. 14Astra Zenesa/AstraZeneca Industries
RUB 139 order
Betaloc Zok tablets 50 mg No. 30Astra Zenesa/AstraZeneca Industries
RUB 272 order
Betalok Zok (tablet p/o 50 mg No. 30)Astra Zeneca/ZIO Health
RUB 279 order

Pharmacy24

Betaloc Zok 100 mg N30 Astra Zeneca AB, Sweden
199 UAH order
Betaloc Zok 50 mg N30 tablets Astra Zeneca AB, Sweden
142 UAH order
Betaloc Zok 25 mg No. 14 tablets Astra Zeneca AB, Sweden
80 UAH order

Interactions of the drug Betaloc zok

Patients should be under medical supervision if other beta-adrenergic receptor blockers (for example, in the form of eye drops), ganglion blockers, or MAO inhibitors are simultaneously prescribed with Betaloc ZOK. Concomitant use with propafenone should be avoided. Propafenone inhibits the metabolism of metoprolol via cytochrome P450 2D6. The result of using this combination is unpredictable, since propafenone also has a β-adrenergic blocking effect. If clonidine is suddenly discontinued during treatment with beta-adrenergic blockers, blood pressure may increase. If it is necessary to discontinue concomitant therapy with clonidine, the β-adrenergic blocker should be discontinued several days before discontinuing clonidine. In patients taking calcium antagonists such as verapamil or diltiazem and/or antiarrhythmic drugs simultaneously with Betaloc ZOK, a negative ino- and chronotropic effect may develop. In patients taking β-adrenergic blockers, intravenous administration of verapamil is contraindicated (risk of cardiac arrest). β-adrenergic receptor blockers can enhance the negative ino- and chronotropic effects of antiarrhythmic drugs (quinidine analogues, amiodarone). In patients receiving treatment with beta-adrenergic blockers, the use of inhalational anesthetics increases the severity of the cardiodepressive effect. Inducers or inhibitors of microsomal liver enzymes may affect the concentration of metoprolol in blood plasma. Metoprolol plasma concentrations are reduced by concomitant use of rifampicin or may be increased by concomitant use of cimetidine, phenytoin, alcohol, hydralazine and serotonin reuptake inhibitors (paroxetine, fluoxetine and sertraline). With simultaneous use of indomethacin or other COX inhibitors, the antihypertensive effect of beta-adrenergic blockers may be reduced. Cardioselective beta-adrenergic blockers have a significantly lesser effect on blood pressure when patients are given epinephrine than non-selective beta-adrenergic blockers. When taking beta-adrenergic blockers concomitantly, dose adjustment of oral antidiabetic agents may be necessary.

Overdose of the drug Betaloc zok

Symptoms: severe arterial hypotension, sinus bradycardia, AV block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, disturbances of consciousness up to coma, nausea, vomiting, cyanosis of the extremities. Concomitant use of alcohol, antihypertensive drugs, quinidine or barbiturates may worsen the patient's condition. The first symptoms develop 20 minutes to 2 hours after an overdose. Treatment: gastric lavage, taking activated carbon. In cases of severe arterial hypotension, bradycardia, or the threat of developing heart failure, administration of a β1-adrenergic receptor agonist (for example, prenalterol) intravenously at intervals of 2–5 minutes or as an infusion is indicated until a therapeutic effect is achieved. In the absence of a selective β1-adrenergic receptor agonist, it can be replaced by intravenous dopamine or atropine sulfate to block the vagus nerve. If a therapeutic effect cannot be achieved, other sympathomimetics (dobutamine or norepinephrine) can be used. Administration of glucagon at a dose of 1–10 mg is indicated. It may be necessary to use a pacemaker. To relieve bronchospasm, a β2-adrenergic receptor agonist is administered intravenously. It should be borne in mind that the doses of antidotes that are necessary to eliminate the symptoms of an overdose of a β-adrenergic receptor blocker are much higher than therapeutic doses, since β-adrenergic receptors are bound by their blockers.

Overdose

There are cases where, at a dosage of 7.5 g, the drug caused severe intoxication with a fatal outcome in an adult. At doses of 1.4 and 2.5 g, respectively, there was moderate and severe intoxication.

An overdose of this drug can lead to respiratory depression, atrioventricular block I–III degrees, decreased blood pressure , heart failure, bradycardia , asystole , poor peripheral perfusion , cardiogenic shock , apnea . In addition, Betaloc ZOK in increased doses can cause impairment of consciousness, tremor , excessive sweating and fatigue, bronchospasm , vomiting, hypoglycemia or hyperglycemia , renal impairment, loss of consciousness, convulsions, paresthesia , nausea, as well as esophageal spasm and hyperkalemia .

Initial signs of a drug overdose will be noticeable 20-120 minutes after administration.

Activated carbon is prescribed as treatment, as well as gastric lavage if necessary.

Depending on the manifestations of overdose, symptomatic treatment is carried out. So, you may need intubation and adequate ventilation , ECG monitoring , blood volume replenishment and glucose infusion . If necessary, atropine intravenously (before gastric lavage) 1-2 mg. For myocardial dobutamine or dopamine is administered . It is possible to use glucagon intravenously at a dosage of 50–150 mcg per 1 kg of weight. In some cases, adrenaline , terbutaline (to relieve bronchospasm ), and an artificial pacemaker help. For arrhythmia and an extensive ventricular complex, a sodium solution is injected. Resuscitation measures may be necessary.