Betalok ZOK
Betalok ZOK: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Betaloc ZOK
ATX code: C07AB02
Active ingredient: Metoprolol (Metoprolol)
Manufacturer: AstraZeneca AB (Sweden)
Description and photo update: 19.10.2018
Prices in pharmacies: from 117 rubles.
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Betaloc ZOK is a selective beta 1 -adrenergic blocker.
Release form and composition
Film-coated sustained-release tablets: almost white or white, biconvex; Betaloc ZOK 25 mg - oval, on each side with a notch, on one side engraving "A" over "β", Betaloc ZOK 50 mg - round, on one side a dividing line, on the other - engraving "A" over "mo", Betaloc ZOK 100 mg - round, with a dividing line on one side and engraving "A" above "ms" on the other side (25 mg - 14 pcs. In a blister, in a cardboard box 1 blister; 50 mg and 100 mg - each 30 pcs. In a plastic bottle, in a cardboard box 1 bottle).
1 tablet contains:
- active substance: metoprolol succinate - 23.75 mg, 47.5 mg or 95 mg, which is equivalent to the content of 25 mg, 50 mg or 100 mg (respectively) of metoprolol tartrate and 19.5 mg, 39 mg or 78 mg (respectively) of metoprolol;
- auxiliary components: sodium stearyl fumarate, hyprolose, ethyl cellulose, hypromellose, macrogol, silicon dioxide, microcrystalline cellulose, titanium dioxide, paraffin.
Pharmacological properties
Pharmacodynamics
Metoprolol belongs to the group of beta 1 -adrenergic blockers, its blocking effect on beta 1 -adrenergic receptors occurs in significantly lower doses than is required to block beta 2 -adrenergic receptors. It has a minor effect that stabilizes the membrane.
Metoprolol inhibits or reduces the agonistic effect of catecholamines, which they have on cardiac activity during exercise and stress. This confirms its ability to prevent an increase in blood pressure (BP), heart rate, increased heart contractility, and an increase in minute volume.
Betaloc ZOK provides a constant concentration of the drug in the blood plasma and a stable clinical effect for more than 24 hours.
Due to the absence of clear peak concentrations in blood plasma, the clinical effect of the drug is characterized by better selectivity for beta 1 -adrenergic receptors compared to conventional tablet forms of beta 1- blockers. This significantly reduces the potential risk of side effects, such as bradycardia and weakness in the legs when walking, that occur at peak plasma concentrations of the drug.
In obstructive pulmonary diseases, Betaloc ZOK can be prescribed in combination with beta 2 -adrenomimetics, this, if necessary, will reduce bronchodilation that occurs against the background of therapeutic doses of beta 2 -adrenomimetics.
When compared with nonselective beta-blockers, the drug has a lesser effect on insulin production and carbohydrate metabolism, in conditions of hypoglycemia it causes a much less pronounced reaction of the cardiovascular system.
With arterial hypertension, the use of metoprolol significantly lowers blood pressure and maintains it for 24 hours or more, both in the standing and lying position, and during exercise.
At the beginning of treatment, there is an increase in total peripheral vascular resistance (OPSS), but long-term use of the drug leads to a decrease in blood pressure against the background of a decrease in OPSS with stable cardiac output.
Studies have confirmed an increase in survival when using Betaloc ZOK in patients with chronic heart failure of II – IV functional classes according to the NYHA classification (New York Heart Association) with a reduced ejection fraction and a decrease in the frequency of their hospitalizations. After long-term therapy, a decrease in the severity of symptoms (according to NYHA functional classes) and an overall improvement in well-being were achieved. Studies have shown an increase in the left ventricular ejection fraction, a decrease in the end systolic and end diastolic volumes of the left ventricle.
During the period of treatment with the drug, the quality of life does not deteriorate, on the contrary, improvement is observed in patients who have had myocardial infarction.
Pharmacokinetics
The tablets quickly disintegrate upon contact with liquid, as a result of which the active substance is dispersed in the gastrointestinal tract. The release rate of metoprolol depends on the acidity of the medium. After taking the drug, the therapeutic effect continues for more than 24 hours, a constant release rate of the active substance is achieved within 20 hours. The half-life is 3.5 hours on average.
With blood plasma proteins, the connection of metoprolol is low, about 5-10%.
After oral administration, Betaloc ZOK is completely absorbed, systemic bioavailability is approximately 30-40% after taking a single dose.
The oxidative metabolism of the active substance occurs in the liver. At the same time, its three main metabolites did not show a clinically significant beta-blocking effect.
About 5% of the taken dose of the drug is excreted unchanged in the urine, the rest is excreted in the form of metabolites.
Indications for use
- arterial hypertension;
- adjunctive therapy to the main treatment in stable symptomatic chronic heart failure with impaired systolic function of the left ventricle;
- angina pectoris;
- the period after the acute phase of myocardial infarction in order to reduce the frequency of re-infarction and mortality;
- functional disorders of cardiac activity, accompanied by tachycardia;
- supraventricular tachycardia, a decrease in the frequency of ventricular contractions with ventricular extrasystoles and atrial fibrillation or other heart rhythm disturbances;
- prevention of migraine attacks.
Contraindications
- atrioventricular (AV) block II and III degree according to the NYHA classification;
- stage of decompensation of heart failure;
- continuous or intermittent therapy with inotropic agents that act on beta-adrenergic receptors;
- clinically significant sinus bradycardia;
- sick sinus syndrome (SSS);
- cardiogenic shock;
- severe form of peripheral circulatory disorders (including the threat of gangrene);
- arterial hypotension;
- patients with suspected acute myocardial infarction with a heart rate (HR) less than 45 beats per minute, systolic blood pressure less than 100 mm Hg or a PQ interval (the time it takes for excitation to travel through the atria and atrioventricular node to the ventricular myocardium) more than 0.24 seconds;
- simultaneous intravenous (iv) administration of verapamil and other slow calcium channel blockers;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to beta-blockers and drug components.
With caution, Betaloc ZOK should be prescribed for Prinzmetal's angina pectoris, I degree AV blockade, chronic obstructive pulmonary disease (COPD), bronchial asthma, diabetes mellitus, severe renal failure, metabolic acidosis, in combination with cardiac glycosides.
Instructions for use Betalok ZOK: method and dosage
According to the instructions, Betalok ZOK is taken orally without chewing (including pills divided in half), drinking plenty of liquid.
The prescribed dose should be taken once a day, in the morning.
Food intake does not affect the bioavailability of the drug.
The dose of the drug is determined individually, when it is selected, the development of bradycardia should not be allowed.
Recommended daily dosage of Betaloca ZOK:
- arterial hypertension: 50-100 mg, in the absence of a sufficient therapeutic effect against the background of a dose of less than 100 mg, the drug is indicated in combination with other antihypertensive drugs, preferably with a diuretic and a calcium channel blocker derived from dihydropyridine;
- angina pectoris: 100-200 mg, possibly a combination with another antianginal agent;
- stable chronic heart failure of functional class II: during the first 2 weeks, Betaloc ZOK 25 mg is prescribed (initial dose), then, if necessary, an increase of 25 mg is possible with an interval of 2 weeks. Maintenance dose - 200 mg;
- stable chronic heart failure of the III-IV functional class: the initial dose (first 2 weeks) - 12.5 mg, then the dose is selected individually, under the close supervision of a physician. in some patients, symptoms of heart failure may worsen during dose escalation. A step-by-step (once every 2 weeks) increase in the dose with good tolerance of the drug can be continued until the maximum dose of 200 mg is reached. With the development of arterial hypotension and / or bradycardia, a decrease in the dose of the drug or concomitant therapy is indicated. The possible appearance of arterial hypotension at the beginning of treatment does not necessarily indicate dose intolerance with further prolonged therapy, but the dose cannot be increased until the condition is stabilized. During this period, kidney function should be monitored;
- cardiac arrhythmias: 100-200 mg;
- maintenance therapy after myocardial infarction: 200 mg each;
- functional disorders of cardiac activity, accompanied by tachycardia: 100-200 mg;
- prevention of migraine attacks: 100-200 mg.
When prescribing Betaloc ZOK for the treatment of stable symptomatic chronic heart failure with impaired systolic function of the left ventricle, it is necessary that the patient has no exacerbation episodes for the last 6 weeks and changes in the main therapy for the next 2 weeks before starting the drug. If the symptomatic picture worsens while taking beta-blockers, treatment is continued, if the condition normalizes with a decrease in the dose, otherwise it is stopped.
In case of impaired renal function or an elderly patient, dose adjustment of Betaloc ZOK is not required.
With a pronounced degree of liver dysfunction, consideration should be given to lowering the dose.
Side effects
- on the part of the cardiovascular system: often - coldness of the extremities, bradycardia, palpitations, orthostatic arterial hypotension (including in very rare cases accompanied by fainting); infrequently - 1st degree AV block, transient worsening of symptoms of heart failure, edema, pain in the region of the heart, cardiogenic shock in acute myocardial infarction; rarely - arrhythmias, other conduction disorders; very rarely - gangrene (against the background of severe peripheral circulatory disorders);
- from the digestive system: often - pain in the abdomen, diarrhea, constipation, nausea; infrequently - vomiting; rarely - dryness of the oral mucosa;
- from the central nervous system: very often - severe fatigue; often - headache, dizziness; infrequently - drowsiness or insomnia, paresthesia, depression, convulsions, nightmares, decreased concentration; rarely - anxiety, increased nervous irritability; very rarely - depression, memory impairment, hallucinations, amnesia;
- from the liver: rarely - a functional disorder of the liver; very rarely - hepatitis;
- dermatological reactions: infrequently - increased sweating, skin rash (similar to psoriasis-like urticaria); rarely - hair loss; very rarely - exacerbation of psoriasis, photosensitivity;
- from the senses: rarely - visual impairment, conjunctivitis, irritation and / or dryness of the eyes; very rarely - disturbances in taste, ringing in the ears;
- from the respiratory system: often - shortness of breath against the background of physical activity; infrequently - bronchospasm; rarely - rhinitis;
- from the musculoskeletal system: very rarely - arthralgia;
- from the hematopoietic system: very rarely - thrombocytopenia;
- from the side of metabolism: infrequently - increased body weight;
- others: rarely - sexual dysfunction, impotence.
Overdose
Symptoms (within 2 hours after taking a large dose of the drug): intoxication (its degree depends on the dose taken and the person's age), bradycardia, asystole, AV blockade of I – III degrees, a strong decrease in blood pressure, heart failure, weak peripheral perfusion, cardiogenic shock, apnea, bronchospasm, suppression of lung function, impaired consciousness, increased fatigue, tremor, convulsions, loss of consciousness, increased sweating, paresthesia, nausea, vomiting, possible esophageal spasm, hyperkalemia, hypoglycemia (more often in children) or hyperglycemia, exposure on the kidneys, transient myasthenic syndrome. The simultaneous use of antihypertensive drugs, quinidine or barbiturates, alcohol consumption worsens the patient's condition.
Treatment: the appointment of activated carbon, intravenous (i / v) administration of atropine at a dose of 0.25-0.5 mg for adults, for children - at the rate of 0.01-0.02 mg per 1 kg of the child's weight (due to the risk of stimulating the vagus nerve, the administration of atropine is prescribed before gastric lavage!) Symptomatic therapy is carried out. If necessary, gastric lavage, electrocardiography, measures to maintain airway patency and adequate ventilation are performed. It is necessary to ensure the replenishment of the circulating blood volume, prescribe glucose infusion. In case of vagal symptoms, intravenous administration of atropine should be repeated at a dose of 1-2 mg. With depression of the myocardium, intravenous drip of dopamine or dobutamine is indicated. Shown in / in the use of glucagon at a dose of 0.05-0.15 mg per 1 kg with an interval of 1 minute. If necessary, adrenaline can be added to therapy. With an enlarged ventricular (QRS) complex and arrhythmias, infusion of sodium chloride or bicarbonate solution, installation of an artificial pacemaker is indicated, in case of cardiac arrest - resuscitation measures for several hours, with bronchospasm - injection or inhalation use of terbutaline.
special instructions
The use of the drug in patients with bronchial asthma or COPD should be carried out in the minimum effective dose and accompanied by the appointment of beta 2 -adrenomimetic. If necessary, the dose of beta 2 -adrenomimetic is increased.
Beta 1 -blockers have less effect on the disturbance of carbohydrate metabolism or masking the symptoms of hypoglycemia compared to nonselective beta-blockers.
Betaloc ZOK can be prescribed to patients with chronic heart failure in the stage of decompensation only after reaching the stage of compensation and maintaining it during treatment with the drug. In very rare cases, with a violation of AV conduction, the patient's condition may worsen. With the development of bradycardia against the background of treatment, it is necessary to reduce the dose of the drug or gradually cancel it.
The action of the drug can aggravate the existing violation of peripheral circulation, mainly due to a decrease in blood pressure.
While taking metoprolol, anaphylactic shock becomes more severe, and therapeutic doses of epinephrine (adrenaline) do not always achieve the desired clinical effect.
With pheochromocytoma, an alpha-blocker should be used in combination with the drug.
Avoid abrupt discontinuation of Betaloc ZOK, especially in high-risk patients, as this can aggravate the course of chronic heart failure, increase the risk of myocardial infarction and sudden death. Cancellation of the drug should be made by gradually lowering the dose taken (reducing it by half once every 2 weeks) until the final dose is reached - 12.5 mg. After 4 days of taking the final dose, the drug can be canceled. If during the period of lowering the dose there is an increase in the symptoms of angina pectoris, an increase in blood pressure, then the dose should be lowered more slowly.
When carrying out a planned surgical operation, it is not recommended to discontinue beta-blocker therapy; you should inform the anesthesiologist about taking Betaloc ZOK. When carrying out non-cardiological operations, it is impossible to prescribe high doses of the drug without first titrating them to patients with cardiovascular risk factors.
Patients with severe, stable symptomatic chronic heart failure should be treated by a physician with specialized knowledge and experience, as there are limited clinical trial data for such patients.
The use of Betaloc ZOK is contraindicated in unstable heart failure in the stage of decompensation.
Influence on the ability to drive vehicles and complex mechanisms
During the period of use of the drug, care should be taken when driving vehicles and mechanisms, since dizziness and other side effects may appear.
Application during pregnancy and lactation
The use of Betaloc ZOK during gestation and breastfeeding is contraindicated, except in exceptional cases that threaten the mother's life, when the expected therapeutic effect of taking the drug for the mother exceeds the potential threat to the fetus and / or child.
The drug may cause bradycardia and other side effects in the fetus, newborn, or breastfed babies, although the dose of metoprolol excreted in breast milk and its beta-blocking effect in a baby is believed to be negligible.
Pediatric use
Due to the lack of information on the efficacy and safety of the drug in children and adolescents under the age of 18, the use of Betaloc ZOK in this category of patients is contraindicated.
With impaired renal function
Care must be taken when using the drug in patients with severe renal failure.
For violations of liver function
In patients with severe hepatic impairment, such as severe cirrhosis, portocaval anastomosis, consideration may be given to reducing the dose of Betaloc ZOK.
Use in the elderly
Elderly patients should not adjust the dosage regimen.
Drug interactions
With the simultaneous use of Betalok ZOK:
- quinidine, paroxetine, fluoxetine, terbinafine, sertraline, diphenhydramine, celecoxib, propafenone (drugs that inhibit CYP2D6) may affect the plasma concentration of metoprolol;
- propafenone increases plasma concentration and the risk of developing undesirable effects of metoprolol;
- phenobarbital and other barbituric acid derivatives increase the metabolism of metoprolol;
- verapamil promotes the development of bradycardia and a decrease in blood pressure;
- amiodarone can cause severe sinus bradycardia, including for a long period after its withdrawal;
- disopyramide and other class I antiarrhythmic drugs can cause serious hemodynamic adverse events with impaired left ventricular function against the background of the summation of the negative inotropic effect of the two drugs;
- non-steroidal anti-inflammatory drugs (including indomethacin, diclofenac) reduce the antihypertensive effect of beta-blockers;
- diltiazem, against the background of mutual enhancement of the inhibitory effect on the AV conduction and the function of the sinus node, causes severe bradycardia;
- diphenhydramine enhances the effect of metoprolol;
- phenylpropanolamine (norephedrine) causes an increase in diastolic blood pressure to pathological values at a dose of 50 mg, and at a higher dose - reactions of paradoxical arterial hypertension up to the development of a hypertensive crisis;
- epinephrine (adrenaline) increases the risk of severe arterial hypertension and bradycardia;
- when clonidine is abruptly canceled, it contributes to the appearance of a hypertensive reaction, therefore, with combination therapy, the drug should be discontinued several days before clonidine is discontinued;
- quinidine inhibits the metabolism of metoprolol in patients with rapid hydroxylation, causes a significant increase in the plasma concentration of metoprolol and an increase in its effect;
- rifampicin may increase the metabolism of metoprolol;
- inhalation anesthetics enhance the cardiodepressant effect;
- oral hypoglycemic agents require dose adjustment;
- cardiac glycosides can cause bradycardia by prolonging AV conduction time;
- cimetidine, hydralazine can increase the plasma concentration of metoprolol.
With SSS and impaired AV conduction, combination with class I antiarrhythmic drugs should be avoided.
Analogs
Betalok ZOK analogs are: Azoprol Retard, Corvitol, Vasokardin, Metoprolol, Metoprolol Tartrate, Metoprolol Zentiva, Metokor, Egilok Retard.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Betaloca ZOK
According to reviews, Betalok ZOK is well tolerated, side effects are mostly mild and reversible.
Price for Betalok ZOK in pharmacies
The price of Betaloca ZOK on average for a package of tablets in a dose of 25 mg is 160 rubles, for 50 mg - 270 rubles, for 100 mg - 370 rubles.
Betalok ZOK: prices in online pharmacies
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Drug name Price Pharmacy |
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Betaloc ZOK 25 mg film-coated tablets with sustained release 14 pcs. 117 RUB Buy |
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Betaloc ZOK tablets p.o. with slow. release 25mg 14 pcs. 151 RUB Buy |
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Betaloc ZOK 50 mg film-coated tablets with sustained release 30 pcs. 229 r Buy |
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Betaloc ZOK 100 mg film-coated tablets with sustained release 30 pcs. 347 r Buy |
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Betaloc ZOK tablets p.o. with slow. release 100mg 30 pcs. 426 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
