Betaloc ZOK, 25 mg, delayed-release, film-coated tablets, 14 pcs.

Pharmacodynamics and pharmacokinetics

The active ingredient Betaloc reduces or eliminates the stimulating effect of catecholamines during stress and exercise, reduces myocardial contractility and cardiac output, reduces high blood pressure and heart rate. In addition, metoprolol reduces myocardial oxygen demand and prolongs diastole.

The drug may slightly increase TG levels and also slightly reduce HDL fractions and free fatty acid levels in the blood plasma.

The tablets are characterized by a delayed release of the active substance, so the concentration of the drug in the blood plasma remains unchanged, which ensures a stable clinical effect for a day or more. The drug is better tolerated than its analogues, and the risk of developing unwanted side effects is significantly reduced.

Betaloc ZOK is completely absorbed. Absorption does not depend on the timing of meals. The degree of connection with blood plasma proteins is 5-10%. The active substance is metabolized in the liver to form three metabolites without beta-blocking activity.

About 95% of the drug is excreted in the urine, the remaining amount remains unchanged. The half-life averages 3-4 hours.

Comparison

Each of the drugs is effective in the treatment of diseases of the cardiovascular system. When taking medications based on metoprolol, it is possible to normalize blood pressure and significantly improve the patient’s condition.

If you conduct a comparative analysis of the drugs, you can note that the active ingredients are the same, but have a different chemical formula. There are differences in the degree of influence on the cardiovascular system. Betaloc is available in only one dosage, but Betaloc Zok is produced in three different dosages: 25 mg, 50 mg and 100 mg. Thanks to this, it is possible to select the optimal treatment regimen for the patient.

The list of indications for medications is the same; one drug or another is prescribed taking into account the patient’s medical history and the effectiveness of previous treatment.

It must be taken into account that Betaloc can provoke more adverse reactions, this is due to the specific properties of the active substance. The second drug is much better tolerated, since the active substance is not released immediately, but gradually, ensuring a constant plasma level. Although there is still a possibility of negative symptoms occurring.

Each of the medications is sold strictly according to your prescription.

If you choose which of these drugs is better, you should first determine the purpose of the treatment, only after that the doctor can recommend the use of the first or second drug.

Indications for use

What are Betaloc ZOK tablets for? First of all, they are prescribed to patients with:

• arterial hypertension;
• heart rhythm disturbances;
• angina pectoris;
• functional disorders of the heart, which are accompanied by tachycardia .

As an element of therapy, the drug is used for chronic heart failure . In addition, Betaloc ZOK is used to reduce mortality and the likelihood of recurrent infarction after the acute phase of myocardial infarction , as well as as a prophylactic against migraine .

The principle of action of the drugs

Both drugs have a fairly similar, even with careful comparison, principle of action. Only the former affects β1-type adrenergic receptors, while the latter acts on β2-type receptors. Both drugs significantly reduce myocardial oxygen demand, which leads to a decrease in heart rate and an expected decrease in blood pressure.

Action of Betalok ZOK

Immediately after taking these drugs, they help reduce SBP (formed during the contraction of the ventricles of the heart, also popularly called “upper”), and after a course of therapy for a period of two to three weeks, DBP levels also gradually return to normal (appearing after contraction of the atria, known also known as “lower”).

The maximum concentration of both drugs in the blood of patients is observed 1.5 hours after their oral administration. Therefore, you should not rush to take another pill immediately after the effect was not noted after taking the previous one, you need to wait so as not to provoke an overdose.

Both drugs reduce the degree of the body’s response to the action of catecholamines, which significantly contributes to a decrease in cardiac output, which is used in groups of patients who suffer from dilated cardiomyopathy, and also indirectly affects the reduction of blood pressure through the Kitaev reflex.

Comparison of the dynamics of concentrations of the active substance in blood serum

These drugs also affect the condition of the vascular wall and bronchi, relaxing them, which facilitates the passage of blood and air through them, thereby also helping to reduce pressure.

In the process of performing physical exercises in combination with the use of these medications, tests show a normal level of adrenal gland function and the body's response to the action of adrenaline, as well as a decrease in the likelihood of developing angina attacks in patients with angina pectoris, which confirms their vasodilating effect.

Contraindications

This drug is contraindicated in cases of atrioventricular block II-III degree, therapy with inotropic agents to activate beta-adrenergic receptors, sick sinus syndrome, peripheral arterial circulation disorders, heart failure in the decompensation phase, clinically significant sinus bradycardia , cardiogenic shock , as well as hypersensitivity to beta-adrenergic blockers and any component of the drug.

In addition, Betaloc ZOK is not suitable for patients with acute myocardial infarction with a heart rate less than 45 per minute, systolic blood pressure less than 100 mm Hg. Art. or the duration of the P-Q interval on the ECG is more than 0.24 s.

Compatibility

The drugs have the same composition, so taking two drugs will not lead to an increase in therapeutic effectiveness, but rather may harm the patient, aggravating the course of the disease. If necessary, another drug may be additionally prescribed, which will help relieve negative symptoms and stabilize the patient’s condition.

You should not self-medicate; before taking a medication that affects the functioning of the cardiovascular system, you should definitely consult a cardiologist. Take care of your own health; if you experience any side symptoms during treatment, you should inform your doctor.

This article was written by specialists with medical education from the team. You can read the original instructions on the manufacturer’s website: Betalok and Betalok Zok.

Side effects

As a rule, when used correctly, the medicine is well tolerated by patients to whom it is prescribed. Side effects are minor or easily reversible.

Cardiovascular system: bradycardia , coldness of the extremities, increased manifestations of heart failure , orthostatic hypotension , cardiogenic shock , edema, pain in the heart, fainting, palpitations, first degree atrioventricular block arrhythmia .

Gastrointestinal tract: nausea , diarrhea , vomiting , abdominal pain, constipation .

Skin: rash, increased sweating.

Metabolism: increased body fat.

CNS: increased fatigue, headache , convulsions, problems concentrating, insomnia , dizziness , paresthesia , depression , drowsiness , nightmares.

Respiratory organs: shortness of breath , bronchospasm .

In rare cases, when taking the drug, the following are possible:

• gangrene;
• increased nervous excitability;
• memory impairment;
• hallucinations;
• anxiety;
• depression;
• dryness of the oral mucosa;
• hepatitis;
• hair loss;
• exacerbation of psoriasis ;
• liver dysfunction;
• photosensitivity;
• rhinitis;
• visual impairment;
• conjunctivitis;
• taste disturbances;
• irritation and/or dry eyes;
• tinnitus;
• arthralgia;
• thrombocytopenia;
• impotence , sexual dysfunction .

Possible side effects

Before using this medicine, you should carefully study information about all possible side effects using the official instructions in the package. Since the drug directly affects the heart rate, in a short time it can significantly reduce the pulse and lower blood pressure, the side effects of taking it should be taken seriously.

"Betaloc ZOK" can affect various organs and systems of the body, for example:

• from the sensory organs, vision impairment, dry eyes, and tinnitus may occur;
• possible disorders in the functioning of the central nervous system, such as slow motor and mental reactions, headaches;
• when large doses of the drug are prescribed, respiratory dysfunction may occur - bronchospasm, shortness of breath, nasal congestion;
• from the dermatological side, various rashes, skin itching, urticaria, photodermatosis, psoriasis-like reactions are possible.

If any changes in well-being occur or if symptoms similar to those described above occur, cardiologists advise that you must notify your doctor.

Instructions for use of Betaloc ZOK (Method and dosage)

Instructions for use of Betaloc ZOK include taking the drug once daily, regardless of meals (preferably in the morning). Tablets should not be crushed or chewed. During dosage selection, heart rate should be monitored.

Arterial hypertension : 50 mg per day (if the therapeutic effect is not achieved, the dose can be gradually increased to 100-200 mg per day, while Betaloc ZOK tablets, instructions for use, can be combined with other antihypertensive drugs).

Stable chronic heart failure of functional class III-IV : to begin with, a dosage is prescribed - 12.5 mg per day (1/2 tablet of 25 mg). If necessary, the dose is gradually increased, but this must be done strictly under the supervision of a doctor. After 14 days, the initial dosage is increased to 25 mg per day; after another 2 weeks, 50 mg per day can be prescribed. Thus, every 14 days the dose can be doubled until a maximum dosage of 200 mg is reached. However, the dose should not be increased until there is clear evidence that the patient is stable. Kidney function needs to be monitored.

Stable chronic heart failure of functional class II : at the beginning, a dose of 25 mg is prescribed. After the first 2 weeks, it can be increased to 50 mg per day, and then doubled every 14 days until a therapeutic effect is achieved. The maximum dosage is 200 mg per day.

For migraine prevention, 100–200 mg per day is prescribed.

For angina pectoris, 100–200 mg per day is prescribed (can be combined with other drugs for the treatment of angina pectoris).

For arrhythmia, 100–200 mg per day is prescribed.

Cardiac disorders with palpitations: 100 mg per day (if necessary, the dosage can be increased to 200 mg).

Betaloc Zok tab prolong release 25mg No. 14

Compound

Active substance: metoprolol tartrate - 25 mg. 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.

Pharmacokinetics

Upon contact with liquid, the tablets quickly disintegrate, and the active substance is dispersed 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. T1/2 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

• arterial hypertension;
• angina pectoris;
• stable symptomatic chronic heart failure with impaired left ventricular systolic function (as an adjuvant therapy to the main treatment of heart failure);
• to reduce mortality and the incidence of re-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

• AV block II and III degrees;
• heart failure in the stage of decompensation;
• continuous or intermittent therapy with inotropic agents acting on β-adrenergic receptors;
• clinically significant sinus bradycardia;
• SSSU;
• cardiogenic shock;
• severe disturbances of peripheral circulation (including with the threat of gangrene);
• arterial hypotension;
• patients with suspected acute myocardial infarction with a heart rate less than 45 beats/min, a PQ interval of more than 0.24 seconds, or a systolic blood pressure of less than 100 mm Hg;
• hypersensitivity to metoprolol and other components of the drug or to other beta-blockers;
• intravenous administration of slow calcium channel blockers (like verapamil);
• age under 18 years (efficacy and safety have not been established).

Carefully

use the drug for AV blockade of the first degree, Prinzmetal's angina, bronchial asthma, COPD, diabetes mellitus, severe renal failure, metabolic acidosis, together with cardiac glycosides.

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 1 time/day. If necessary, the dose can be increased to 100 mg 1 time / day or Betaloc® ZOK can be used in combination with other antihypertensive agents, preferably a diuretic and a calcium channel blocker dihydropyridine derivative.

Angina pectoris

100-200 mg Betaloc® ZOK 1 time/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 1 time / day. After 2 weeks of therapy, the dose can be increased to 50 mg 1 time / day, and then can be doubled every 2 weeks.

Maintenance dose for long-term treatment: 200 mg Betaloc® ZOK 1 time/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) 1 time/day. The dose is selected individually. During the period of increasing the dose, the patient should be monitored, because In some patients, heart failure symptoms may worsen.

After 1-2 weeks, the dose can be increased to 25 mg Betaloc® ZOK 1 time / day. Then, after 2 weeks, the dose can be increased to 50 mg 1 time / day. 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 1 time / 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 1 time/day.

Maintenance treatment after myocardial infarction

200 mg Betaloc® ZOK 1 time/day.

Functional cardiac disorders accompanied by tachycardia

100 mg Betaloc® ZOK 1 time / day, if necessary, the dose can be increased to 200 mg / day.

Preventing migraine attacks

100-200 mg Betaloc® ZOK 1 time/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 cirrhosis or portocaval anastomosis), a dose reduction may be required.

Elderly age

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

Children

Experience with the use of Betaloc® ZOK in children is limited.

Storage conditions

The drug should be stored out of the reach of children at temperatures above 30°C.

Best before date

3 years. Do not use after the expiration date.

special instructions

Patients receiving beta-blockers should not receive IV calcium channel blockers (like verapamil).

Patients with bronchial asthma or COPD should be prescribed concomitant therapy with a beta2-agonist. It is necessary to prescribe the minimum effective dose of Betaloc® ZOK, and an increase in the dose of the beta2-adrenergic agonist may be required.

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

When using beta1-blockers, the risk of their effect on carbohydrate metabolism or the possibility of masking the symptoms of hypoglycemia is significantly 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.

Very rarely, patients with impaired AV conduction may worsen (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 beta-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 suffering from 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 the final dose of 12.5 mg (1/2 tablet 25 mg) is reached, which should be taken as at least 4 days before the drug is completely discontinued. If symptoms appear (eg, increased symptoms of angina, 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 beta-blocker therapy is not recommended. Prescribing the drug in high doses without prior titration of the drug doses should be avoided in patients with cardiovascular risk factors undergoing non-cardiac surgery, due to the increased risk of bradycardia, arterial hypotension and stroke, incl. with fatal outcome.

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.

Description

Beta1-adrenergic blocker selective.

Dosage form

White or off-white, oval, biconvex, film-coated tablets, sustained-release, scored on both sides and debossed with “A” over “β” on one side.

Use in children

The use of the drug is contraindicated in children and adolescents under the age of 18 (the effectiveness and safety of the drug have not been established).

Pharmacodynamics

Metoprolol is a beta1-adrenergic blocker that blocks β1-adrenergic receptors in doses significantly lower than the doses required to block β2-adrenergic 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 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.

Unlike conventional tablet dosage forms of selective beta1-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 (blockade of beta1-adrenergic receptors) is ensured for more than 24 hours.

Due to the absence of obvious peak plasma concentrations, clinically Betaloc® ZOK is characterized by better selectivity for β1-adrenergic receptors compared to conventional tablet forms of beta1-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 beta2-agonists. When used together with beta2-adrenergic agonists, Betaloc® ZOK in therapeutic doses has a lesser effect on the bronchodilation caused by beta2-adrenergic agonists than non-selective beta-blockers. Metoprolol affects insulin production and carbohydrate metabolism to a lesser extent than non-selective beta-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 beta-blockers.

The use of the drug 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 peripheral vascular resistance is observed. However, with long-term use, a decrease in blood pressure is possible due to a decrease in peripheral vascular resistance while cardiac output remains unchanged.

In the MERIT-HF study of survival in chronic heart failure (II-IV functional class according to the NYHA classification) with reduced ejection fraction (≤0.4), 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 a general improvement in well-being and a decrease in the severity of symptoms (according to NYHA functional classes). Also, therapy with the drug 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.

Side effects

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%), very rarely (<0.01%).

From the cardiovascular system: often - bradycardia, orthostatic arterial hypotension (very rarely accompanied by fainting), coldness of the extremities, palpitations; uncommon - temporary increase in symptoms of heart failure, AV block of the first degree, cardiogenic shock in patients with acute myocardial infarction, edema, pain in the heart area; rarely - other conduction disorders, arrhythmias; very rarely - 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, convulsions, depression, decreased concentration, drowsiness or insomnia, nightmares; rarely - increased nervous excitability, anxiety; very rarely - memory impairment, amnesia, depression, hallucinations.

From the digestive system: often - nausea, abdominal pain, diarrhea, constipation; infrequently - vomiting; rarely - dryness of the oral mucosa.

From the liver: rarely - liver dysfunction; very rarely - hepatitis.

Dermatological reactions: uncommon - skin rash (such as psoriasis-like urticaria), increased sweating; rarely - hair loss; very rarely - photosensitivity, exacerbation of psoriasis.

From the respiratory system: often - shortness of breath on exertion; uncommon - bronchospasm; rarely - rhinitis.

From the senses: rarely - blurred vision, dryness and/or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, disturbances of taste.

From the musculoskeletal system: very rarely - arthralgia.

From the side of metabolism: infrequently - weight gain.

From the hematopoietic system: very rarely - thrombocytopenia.

Other: rarely - impotence, sexual dysfunction.

Use during pregnancy and breastfeeding

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 beta-blocking effect in a breastfed baby (when the mother takes metoprolol in therapeutic doses) are negligible.

Interaction

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.

Combinations to Avoid

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

Propafenone: when propafenone was prescribed to 4 patients treated with metoprolol, an increase in the plasma concentration of metoprolol was observed by 2-5 times, while 2 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 CYP2D6 isoenzyme. Taking into account the fact that propafenone has beta-blocker properties, the co-administration of metoprolol and propafenone does not seem appropriate.

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

Combinations that may require dose adjustment of Betaloc® ZOK

Class I antiarrhythmic drugs: when combined with beta-blockers, the negative inotropic effect may be additive, resulting in serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with SSSS and impaired AV conduction. The interaction is described using disopyramide as an example.

Amiodarone: Concomitant use with metoprolol may lead to severe sinus bradycardia. Taking into account the extremely long T1/2 of amiodarone (50 days), the possible interaction should be considered long after discontinuation of amiodarone.

Diltiazem: Diltiazem and beta-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.

NSAIDs: NSAIDs reduce the antihypertensive effect of beta-blockers. This interaction has been reported in combination with indomethacin and is likely not to be observed in combination with sulindac. Negative interactions have been noted in studies with diclofenac.

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

Epinephrine (adrenaline): Ten cases of severe hypertension and bradycardia have been reported in patients taking non-selective beta blockers (including pindolol and propranolol) and receiving epinephrine. 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. Apparently, this risk is much lower with the use of cardioselective beta-blockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg may increase diastolic blood pressure to pathological levels in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, beta-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-adrenergic receptor blockade. It is believed that such an interaction is also typical for other beta-blockers, the metabolism of which involves the CYP2D6 isoenzyme.

Clonidine: Hypertensive reactions following abrupt withdrawal of clonidine may be exacerbated by concomitant use of beta-blockers. When used together, if it is necessary to discontinue clonidine, discontinuation of beta-blockers should begin several days before discontinuation of clonidine.

Rifampicin: Rifampicin may increase the metabolism of metoprolol, reducing its plasma concentration. Patients concomitantly taking metoprolol and other beta-blockers (eye drops) or MAO inhibitors should be closely monitored.

While taking beta-blockers, inhalational anesthetics enhance the cardiodepressive effect.

While taking beta-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 in combination with beta-blockers, can increase AV conduction time and cause bradycardia.

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; granzitory 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 myocardial depression, infusion of dobutamine or dopamine is indicated.

You can also use glucagon 50-150 mcg/kg IV at 1-minute intervals. 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.

Impact on the ability to drive vehicles and operate machinery

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

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 , weak 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 infusions. If necessary, Atropine (before gastric lavage) is administered intravenously 1-2 mg. For myocardial depression, Dobutamine or Dopamine . 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 ), as well as an artificial pacemaker, help. For arrhythmia and an extensive ventricular complex, a sodium solution is injected. Resuscitation measures may be necessary.

General description of the drug

"Betalok ZOK", the price of which differs depending on the dosage and number of tablets in the package, is classified as one of the types of cardioselective beta-blockers. Externally, these tablets are enteric-coated. "Betalok ZOK", reviews from cardiologists, whose effects are mostly positive, is a long-acting drug. Due to its shell, the medicine has a delayed release. However, it does not have sympathomimetic internal activity.

The main active ingredient of the drug is metoprolol, a substance that has the following effects on the body:

• antihypertensive;
• antianginal;
• antiarrhythmic.

Also, this drug quite effectively reduces the excitability of the myocardium, reducing its need for oxygen.

Interaction

When using the drug Betaloc ZOK and other beta-adrenergic receptor blockers, as well as MAO inhibitors and ganglion blockers, strict medical supervision is required.

The drug should not be combined with Propafenone , Verapamil . When taking Diltiazem and/or antiarrhythmic drugs, a negative ino- and chronotropic effect may develop. When using inhalational anesthetics, the cardiodepressive effect is enhanced.

It is possible that inducers or inhibitors of microsomal liver enzymes may influence the content of the active substance Betaloc ZOK in the blood plasma. Its concentration is reduced when combined with Rifampicin or increased when taken simultaneously with Cimetidine , hydralazine , phenytoin , and serotonin .

When discontinuing clonidine, Betaloc ZOK must be discontinued several days before.

In combination with COX inhibitors, the antihypertensive effect of the drug may be reduced. Dosage adjustments of oral antidiabetic agents may also be necessary when administered concomitantly.

Interaction with other drugs

Also, the doctor prescribing Betaloc ZOK should be informed about all the medications that the patient is using at the time of prescription. There are substances the use of which is strictly contraindicated when using Betalok ZOK. When taking it, it is strictly forbidden to inject Verapamil into a person. When using Betalok ZOK, you should be very careful when prescribing drugs similar to Reserpine (which, by their action, reduce the reserves of catecholamines). Such simultaneous administration can provoke an attack of bradycardia and a rapid drop in blood pressure in the patient.

Analogues of Betalok ZOK

Level 4 ATC code matches:
Biol

Metocard

Metozok

Nebilet

Nebilong

Betaxolol

Bisogamma

Aritel

Cordinorm

Vasocardin

Corvitol

Bidop

Bisoprolol

Nebivolol

Biprol

Bisoprol

Concor Cor

Lokren

Concor

Niperten

The following analogues of Betalok ZOK are sold in pharmacies:

• Betalok
• Egilok
• Metoprolol
• Metocard
• Metocore
• Serdol
• Azoprol Retard
• Vasocardin
• Corvitol

Reviews about analogues of Betalok ZOK are quite different. Some of them are almost as good as him, and some are of a fairly low level. So the price of analogs of this product, as well as their manufacturers, deserves special attention. To finally decide which medicine is best for each specific case, you should consult a doctor. In addition, before use, be sure to read the instructions.

Key differences and effectiveness

As mentioned above, the main way Metoprolol differs from Betaloc ZOK is that the first acts on β1-adrenergic receptors, and the second on β2-adrenergic receptors. The former are more localized in the vascular walls and the atrioventricular node, while the latter are also located in the bronchi. There are equally many receptors of both types in the heart muscle. This is where the differences in their action come from.

Indications and dosage regimen of Metoprolol

There is also a slight difference in the chemical structure of the main substances - the difference lies only in the basis of which salt the medicine was produced from. Metoprolol has tartrate salt, and Betalok ZOK has succinate.

This may play a minor role in selecting the optimal drug for therapy, since some people are more susceptible to the first substance, while others are more susceptible to the second. There is also a difference in the additional chemical compounds included in the tablets.

It is quite difficult to predict which particular remedy will be more effective for each specific patient. Therapy of essential arterial hypertension involves a long and painstaking selection of the appropriate drug or combinations thereof, and then the dosage of each of them.

It is important to consider the presence of concomitant diseases. If a patient suffers from migraines due to hypertension, then of course it is better to choose Metoprolol, and if, for example, he has bronchial asthma or COPD, then the second drug is better for him.

In addition, it is impossible to predict which particular salt (more on this above) the patient’s body will be more susceptible to. Therefore, when selecting appropriate therapy, you will need to be patient and prepare for the fact that the result may not come as quickly as you would like.

Side effects when taking the drugs discussed are extremely rare; according to a double-blind study with a placebo-controlled group, their frequency did not exceed 0.001%. Among the main side effects of these drugs are possible:

• bradycardia;
• 1st degree atrioventricular block;
• passing increase in symptoms of heart failure;

• 
  hypotension;

• weight gain;
• thrombocytopenia;
• agranulocytosis;
• leukopenia;
• drowsiness or, on the contrary, insomnia;
• impaired concentration;
• nervousness;
• slight and passing increase in shortness of breath;
• the appearance of skin rashes;
• hives;
• erythema;
• nausea;
• vomit;
• stomach ache;
• peripheral edema;
• impotence;
• muscle spasms.

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 unstable 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.

Reviews from doctors about this drug

On numerous forums, cardiologists speak quite well about this drug. One of its main advantages is the ability of the drug to effectively reduce blood pressure. Since this medication is much less expensive than its analogues, for many hypertensive patients this medicine truly becomes a panacea.

This drug also deserves good reviews from doctors because, according to the results of many studies, its main component, metaprolol, has the property of prolonging life. Despite the fact that this drug has a fairly good reputation among cardiologists, there is a certain category of people who are advised by doctors to take additional safety measures while taking these pills. Among these recommendations are:

1. Regularly checking blood glucose levels in people with diabetes. It is necessary to take into account the fact that, being a beta-blocker, “Betaloc ZOK can mask tachycardia that occurs due to hypoglycemia. At the beginning of taking the pills, cardiologists recommend that every patient measure their blood pressure and monitor their pulse daily. In cases where, when taking Betalok ZOK, the heart rate is less than 50 beats per minute, cardiologists strongly recommend seeking medical advice.
2. For elderly patients who take this medicine, doctors recommend monitoring kidney function at least once every 6 months.

Betaloka ZOK price, where to buy

The average price of Betaloc ZOK 50 mg is about 250 rubles, the price of 25 mg is about 150 rubles, and the average cost of 100 mg of the drug is about 400 rubles.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

ZdravCity

• Betaloc ZOK tablets p.p.o.
  with deceleration release 50 mg 30 pcs. Astra Zeneca AB/LLC Astra Zeneca Industries 284 rub. order
• Betaloc ZOK tablets p.p.o. with deceleration release 25 mg 14 pcs. AstraZeneca AB / ZiO-Zdorovye / Astra Zeneca Industries LLC

  146 RUR order

Pharmacy Dialogue

• Betalok Zok (tablet p/o 100 mg No. 30)Astra Zeneсa/AstraZeneca Industries

  RUB 383 order

• Betaloc Zok tablets 25 mg No. 14Astra Zenesa/AstraZeneca Industries

  135 rub. order

• Betaloc Zok tablets 50 mg No. 30Astra Zenesa/AstraZeneca Industries

  RUB 265 order

• Betalok Zok (tablet p/o 50 mg No. 30)Astra Zeneca/ZIO Health

  RUB 279 order

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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

Average cost of the drug

"Betalok ZOk", the price of which depends on the number of tablets in the package and on the markup of the final seller, costs on average from 130 to 460 rubles. The cheapest are 25 mg tablets, which are packaged in 14 pieces. in a pack. Their price is about 130-150 rubles.

The most expensive is Betalok ZOK with a dosage of 100 mg, which is packaged in 30 pieces. into bottles. It costs about 420–480 rubles.