Metoprolol | Betalok Zok tablets coated with delayed exp. 25 mg 14 pcs.
Special Price
$16.49
Regular Price
$24.00
In stock
SKU
BID463369
Release form
Film-coated sustained-release tablets.
Film-coated sustained-release tablets.
Release form
Film-coated sustained-release tablets.
Packing
14 pcs. 25 mg each.
Pharmacological action
Selective beta1-blocker without internal sympathomimetic activity. It has a slight membrane stabilizing effect and does not show the activity of a partial agonist.
Metoprolol reduces or inhibits the agonistic effect that catecholamines, released during nervous and physical stresses, exert on the cardiac activity. This means that metoprolol has the ability to prevent an increase in heart rate, minute volume 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 the drug Betalok® ZOK is used, a constant concentration of the drug in the blood plasma is observed and a stable clinical effect is achieved (blockade of 1-adrenergic receptors) for more than 24 hours.
Due to the lack of apparent peak plasma concentrations, Betaloc® ZOK is clinically characterized by better selectivity for β 1 -adrenoreceptors compared to conventional tablet forms of beta1-address oblokatorov. In addition, the potential risk of side effects observed at peak plasma concentrations of the drug, such as bradycardia and weakness in the legs when walking, is significantly reduced.
Betalok® ZOK in combination with beta2-adrenergic agonists may be prescribed to patients with symptoms of obstructive pulmonary disease. When combined with beta2-adrenergic agonists, Betaloc® ZOK in therapeutic doses has a lesser effect on bronchodilation caused by beta2-adrenergic agonists than non-selective beta-blockers. Metoprolol to a lesser extent than non-selective beta-blockers affects insulin production and carbohydrate metabolism. The effect of the drug on the reaction of the cardiovascular system under hypoglycemia is significantly less pronounced compared with non-selective beta-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 position, and during exercise. At the beginning of metoprolol therapy, an increase in OPSS is noted. With prolonged use, a decrease in blood pressure is possible due to a decrease in OPSS with a constant cardiac output.
In a MERIT-HF study of survival in chronic heart failure (NYHA Class II-IV functional class) with a reduced ejection fraction ( 0.4), which included 3991 patients, Betalok® ZOK showed an increase in survival and a decrease in hospitalization rates. With prolonged 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 Betaloc® ZOK showed an increase in the ejection fraction of the left ventricle, a decrease in the final systolic and final diastolic volumes of the left ventricle.
The quality of life during the treatment with Betalok® ZOK does not deteriorate or improve. Improving the quality of life during treatment with Betaloc® ZOK was observed in patients after myocardial infarction.
Indications
Arterial hypertension.
Angina pectoris.
Stable symptomatic chronic heart failure with impaired systolic function of the left ventricle (as an adjunct therapy to the main treatment for heart failure).
To reduce mortality and recurrence of heart attack after the acute phase of myocardial infarction.
Heart rhythm disturbances, including supraventricular tachycardia, decreased ventricular contractions with atrial fibrillation and ventricular extrasystoles.
Functional disorders of the heart, accompanied by tachycardia.
Prevention of migraine attacks.
Contraindications
AV block II and III degree.
Chronic heart failure in the decompensation stage.
Continuous or intermittent therapy with inotropic drugs aimed at stimulating -adrenoreceptors.
Clinically significant sinus bradycardia.
SSSU.
Cardiogenic shock.
Severe severe disturbances in peripheral arterial circulation (including with the threat of gangrene).
Arterial hypotension.
Patients with suspected acute myocardial infarction with a heart rate of less than 45 beats / min, a PQ interval of more than 0.24 s, or a systolic blood pressure of less than 100 mmHg.
IV administration of slow calcium channel blockers (like verapamil).
Children and adolescents under 18 years of age (efficacy and safety not established).
Hypersensitivity to the drug.
Hypersensitivity to other beta-blockers.
Precautions: use the drug for grade I AV blockade, Prinzmetal angina, bronchial asthma, COPD, diabetes mellitus, severe renal failure, metabolic acidosis, together with cardiac glycosides.
Use during pregnancy and lactation
Like most Betalok® ZOK preparations should not be prescribed during pregnancy and during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or baby.
Like other antihypertensive drugs, beta-blockers can cause side effects, such as bradycardia in the fetus, newborns or breastfed babies.
The amount of metoprolol excreted in breast milk and the beta-blocking effect in a breast-fed baby (when the mother is taking metoprolol in therapeutic doses) are insignificant.
Special instructions
Patients receiving beta-blockers should not be given iv calcium channel blockers (like verapamil).
Patients with bronchial asthma or COPD should be prescribed concomitant therapy with beta2-adrenergic agonist. BetalokВ® ZOK should be prescribed in the minimum effective dose. In this case, an increase in the dose of beta2-adrenergic agonist may be required.
It is not recommended to prescribe non-selective beta-blockers to patients with Prinzmetal angina. Selective beta-blockers should be given with caution to this group of patients.
When using beta1-blockers, the risk of their effect on carbohydrate metabolism or the ability to mask the symptoms of hypoglycemia is significantly less than when using non-selective beta-blockers.
In patients with chronic heart failure in the decompensation stage, before the appointment of BetalokВ® ZOK, compensation must be achieved and maintained during treatment with the drug.
Very rarely, with BetalocВ® ZOK therapy, in patients with impaired conduction, a worsening of the condition can occur up to AV block. If bradycardia develops during treatment, the dose of the drug must be reduced or the drug should be gradually withdrawn.
During the period of use of the drug, intensification of symptoms of peripheral arterial circulation disorders is possible, mainly due to a decrease in blood pressure.
Caution should be exercised when administering the drug to patients with severe renal failure, with metabolic acidosis, co-administration with cardiac glycosides.
In patients taking beta-blockers, anaphylactic shock is more severe. The use of epinephrine (adrenaline) in therapeutic doses does not always lead to the achievement of the desired clinical effect while taking metoprolol.
Alpha-blocker should be given to patients with pheochromocytoma at the same time as BetalocВ® ZOK.
Abrupt withdrawal of beta-blockers is dangerous, especially in high-risk patients, and should therefore be avoided. If it is necessary to cancel the drug, it should be done gradually, for at least 2 weeks, with a two-fold reduction in the dose of the drug at each stage, until the final dose of 12.5 mg (1/2 tab. 25 mg) is reached, which should be take at least 4 days until the drug is completely discontinued. When symptoms appear (for example, increased symptoms of angina pectoris, increased blood pressure), a slower withdrawal regimen is recommended. Abrupt abolition of beta-blocker can lead to a worsening of the course of chronic heart failure and an increased risk of myocardial infarction and sudden death.
In case of surgery, inform the anesthetist that the patient is taking BetalocВ® ZOK. To patients who have surgery, it is not recommended to discontinue therapy with beta-blockers. Avoid prescribing the drug in high doses without prior titration of the dose to patients with cardiovascular risk factors undergoing non-cardiac surgery due to the increased risk of bradycardia, arterial hypotension and stroke, including fatal.
Clinical trial data on efficacy and safety in patients with severely stable symptomatic chronic heart failure (NYHA Class IV Grade) are limited. The treatment of such patients should be carried out by doctors with special knowledge and experience.
Patients with symptomatic heart failure combined with acute myocardial infarction and unstable angina were excluded from the studies, on the basis of which the indications for prescription were determined. The effectiveness and safety of the drug for this group of patients is not described. The use of the drug in unstable heart failure in the stage of decompensation is contraindicated.
Use in pediatrics
Experience with the use of BetalocВ® ZOK in children is limited.
Effect on the ability to drive vehicles and control mechanisms
When driving vehicles and engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions, it should be borne in mind that dizziness and fatigue can be observed when taking BetalokВ® ZOK.
Composition
1 tablet contains:
Active substances:
metoprolol succinate - 23.75 mg, which corresponds to the content of: metoprolol tartrate 25 mg, metoprolol 19.5 mg.
Excipients:
ethyl cellulose - 21.5 mg,
hyprolose - 6.13 mg,
hypromellose - 5.64 mg,
microcrystalline cellulose - 94.9 mg,
paraffin - 60 ?g,
macrogol - 1.41 mg ,
silicon dioxide - 14.6 mg,
sodium stearyl fumarate - 241 ?g,
titanium dioxide - 1.41 mg.
Dosage and administration of
Bradycardia should be avoided when selecting a dose.
For arterial hypertension: the dose is 50-100 mg 1 time / day. If necessary, the dose can be increased to 100 mg 1 time / day or Betalok® ZOK can be used in combination with other antihypertensive drugs (preferably a diuretic and a calcium channel blocker, a dihydropyridine derivative).
With angina pectoris: the dose is 100-200 mg 1 time / day. If necessary, Betalok® ZOK can be used in combination with another antianginal drug.
In case of stable symptomatic chronic heart failure with impaired systolic function of the left ventricle: Betalok® ZOK can be prescribed to patients who have not had exacerbation episodes during the last 6 weeks and have not had changes in the main therapy during the last 2 weeks. Therapy of heart failure with beta-blockers can sometimes lead to a temporary worsening of the symptomatic picture. In some cases, it is possible to continue therapy or reduce the dose, and in some cases, it may be necessary to discontinue the drug.
In stable chronic heart failure of the II functional class: the recommended initial dose for the first 2 weeks is 25 mg 1 time / day. After 2 weeks, the dose can be increased to 50 mg 1 time / day and then can be doubled every 2 weeks. The maintenance dose for long-term treatment is 200 mg 1 time / day.
With stable chronic heart failure of the III and IV functional classes: the recommended initial dose for the first 2 weeks is 12.5 mg 1 time / day. The dose is selected individually. During the period of increasing the dose, the patient should be monitored, as in some patients, heart failure symptoms may worsen. After 1-2 weeks, the dose can be increased to 25 mg 1 time / day, then after another 2 weeks - up to 50 mg 1 time / day. With good tolerance, you can double the dose every 2 weeks until a maximum dose of 200 mg is reached 1 time / day.
In case of arterial hypotension and / or bradycardia: a reduction in concomitant therapy or a reduction in the dose of Betalok® ZOK may be necessary. Arterial hypotension at the beginning of therapy does not necessarily indicate that this dose of Betalock ZOK will not be tolerated with further long-term treatment. However, the dose should not be increased until the condition is stabilized. Renal function monitoring may also be required.
In case of cardiac arrhythmias: the drug is prescribed in a dose of 100-200 mg 1 time / day.
For maintenance treatment after myocardial infarction: the drug is prescribed at a dose of 200 mg 1 time / day.
For functional disorders of cardiac activity accompanied by tachycardia: the dose is 100 mg 1 time / day, if necessary, the dose can be increased to 200 mg / day.
For the prevention of migraine attacks: prescribed in a dose of 100-200 mg 1 time / day.
Betalok® ZOK is intended for daily use 1 time / day (preferably in the morning). The Betalok® ZOK tablet should be swallowed with a liquid. Tablets can be divided in half, but should not be chewed or crumbled. Eating does not affect the bioavailability of the drug.
In patients with impaired renal function, as well as in elderly patients: there is no need to adjust the dose of the drug.
In patients with impaired liver function: usually dose adjustment is not required due to the low degree of binding of metoprolol to plasma proteins. However, in severely impaired liver function (in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.
Side effects of
The following criteria were used to assess the incidence of cases:
Very often (> 10%).
Often (1-9.9%).
Infrequently (0.1-0.9%).
Rarely (0.01-0.09%).
Very rare (<0.01%).
From the cardiovascular system: often - bradycardia, orthostatic arterial hypotension (very rarely accompanied by fainting), cold extremities, palpitations, infrequent - temporary increase in symptoms of heart failure, AV block I degree, cardiogenic shock in patients with acute myocardial infarction, edema, pain in the heart rarely — other conduction disturbances, arrhythmias very rarely — gangrene (in patients with severe peripheral circulatory disorders).
From the side of the central nervous system and peripheral nervous system: very often - increased fatigue often - dizziness, headache infrequently - paresthesias, cramps, depression, decreased ability to concentrate, drowsiness or insomnia, nightmares rarely - increased nervous irritability, anxiety very rarely - memory impairment, amnesia, depression, hallucinations.
From the digestive system: often - nausea, abdominal pain, diarrhea, constipation infrequently - vomiting rarely - dry mucous membrane of the oral cavity, impaired liver function very rarely - hepatitis.
From the hemopoietic system: very rarely - thrombocytopenia.
From the respiratory system: often - shortness of breath with physical exertion infrequently - bronchospasm rarely - rhinitis.
From the musculoskeletal system: very rarely - arthralgia.
On the part of the sensory organs: rarely - dryness and / or irritation of the eyes, conjunctivitis, visual impairment is very rare - ringing in the ears, disturbances in taste.
Dermatological reactions: infrequently - skin rash (like psoriasis-like urticaria), increased sweating rarely - hair loss is very rare - photosensitivity, exacerbation of psoriasis.
Other: sometimes - weight gain rarely - impotence, sexual dysfunction.
Betalok® ZOK is well tolerated by patients, side effects are mostly mild and reversible.
Drug interactions
Metoprolol is a substrate of CYP2D6, and therefore, drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) can affect plasma concentration.
Combinations to avoid
Derivatives of barbituric acid: barbiturates enhance the metabolism of metoprolol due to the induction of enzymes (the study was conducted with phenobarbital).
Propafenone: when prescribing propafenone to 4 patients receiving metoprolol, a 2-5-fold increase in the concentration of metoprolol in the blood plasma was noted, while in 2 patients, side effects characteristic of metoprolol were noted. This interaction was confirmed in a study of 8 volunteers. The interaction is probably due to the inhibition by propafenone, like quinidine, of the metabolism of metoprolol via the CYP2D6 isoenzyme. Taking into account the fact that propafenone has the properties of a beta-blocker, the combined administration of metoprolol and propafenone does not seem appropriate.
Verapamil: A combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on AV conduction and sinus node function.
Combinations, the use of which may require dose adjustment of Betaloc® ZOK
Class I antiarrhythmic drugs: when combined with beta-adrenergic blocking agents, a negative inotropic effect may be added, resulting in serious hemodynamic side effects in patients with impaired left ventricular function. A similar combination should also be avoided in patients with CVS and impaired AV conduction. The interaction is described by the example of a disopyramid.
Amiodarone: co-administration with metoprolol can lead to severe sinus bradycardia. Considering the extremely long T1 / 2 of amiodarone (50 days), the possible interaction should be considered long after the withdrawal of amiodarone.
Diltiazem: diltiazem and beta-blockers mutually reinforce the inhibitory effect on AV conduction and sinus node function. With a combination of metoprolol with diltiazem, cases of severe bradycardia were noted.
NSAIDs: NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction has been reported with a combination with indomethacin and probably will not be observed with a combination with sulindac. Negative interactions have been observed in studies with diclofenac.
Diphenhydramine: diphenhydramine reduces the biotransformation of metoprolol to -hydroxymethoprolol by 2.5 times. At the same time, an increase in the action of metoprolol is 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. The interaction was also noted in the group of healthy volunteers. It is assumed that similar reactions can be observed with the use of epinephrine in conjunction with local anesthetics in case of accidental entry into 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 can increase diastolic blood pressure to pathological values in healthy volunteers. Propranolol basically inhibits the increase in blood pressure caused by phenylpropanolamine. However, beta-blockers can cause paradoxical hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported with phenylpropanolamine.
Quinidine: quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (in Sweden, approximately 90% of the population), mainly causing a significant increase in the plasma concentration of metoprolol and increased blockade of β-adrenoreceptors. It is believed that such an interaction is also characteristic of other beta-blockers, in the metabolism of which the isoenzyme CYP2D6 is involved.
Clonidine: hypertensive reactions with abrupt cancellation of clonidine may be enhanced while taking beta-blockers. With joint use, if it is necessary to cancel clonidine, discontinuation of beta-blockers should begin a few days before the cancellation of clonidine.
rifampicin: rifampicin can enhance the metabolism of metoprolol, reducing its concentration in blood plasma. Patients taking metoprolol and other beta-blockers (eye drops) or MAO inhibitors at the same time should be closely monitored.
In patients with beta-blockers, inhaled anesthetics enhance the cardiac depressant effect.
While taking beta-blockers, patients receiving oral hypoglycemic agents may need a dose adjustment.
Plasma concentration of metoprolol may increase with cimetidine or hydralazine.
Cardiac glycosides when used together with beta-blockers can increase AV conduction time and cause bradycardia.
Overdose
Metoprolol at a dose of 7.5 g in an adult caused lethal intoxication. In a 5 year old child taking 100 mg of metoprolol, no signs of intoxication were observed after gastric lavage. Taking 450 mg of metoprolol by a teenager for 12 years resulted in moderate intoxication. The intake of 1.4 g and 2.5 g of metoprolol in adults caused moderate and severe intoxication, respectively. The intake of 7.5 g by adults resulted in extremely severe intoxication.
Symptoms: The most serious are the symptoms from the cardiovascular system, but sometimes, especially in children and adolescents, symptoms from the CNS and pulmonary function suppression, bradycardia, AV-blockade of I-III degree, asystole, severe decrease in blood pressure may prevail weak peripheral perfusion, heart failure, cardiogenic shock, pulmonary function depression, apnea, increased fatigue, impaired consciousness and loss, tremor, convulsions, sweating, paraesthesia, bronchospasm, nausea, vomiting, esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia transient effects.
Concomitant use of alcohol, antihypertensive agents, quinidine or barbiturates may worsen the patient's condition. The first signs of overdose can be observed 20 min-2 h after drug administration.
Treatment: Activation of activated charcoal, if necessary - gastric lavage.
Atropine at a dose of 0.25-0.5 mg / v for adults and 10-20 mcg / kg for children should be given before gastric lavage (due to the risk of vagus nerve stimulation).
Intubation and IVL are performed if necessary to maintain airway patency.
Terbutaline may be injected or inhaled for the treatment of bronchospasm.
Followsto replenish BCC, to carry out an infusion of glucose. Atropine 1.0-2.0 mg I / O, if necessary repeat the administration (especially with vaginal symptoms). ECG monitoring.
Infusion of dobutamine or dopamine is indicated in case of myocardial depression. You can use glucagon 50-150 mcg / kg I / O at intervals of 1 min. In some cases, it may be effective to add epinephrine to therapy.
Sodium (chloride or bicarbonate) solutions are infused with arrhythmia and enlarged ventricular (QRS) complex. Installation of an artificial rhythm driver is possible.
Resuscitation may require several hours for heart failure due to overdose.
Symptomatic treatment is performed.
Storage conditions
Keep out of the reach and sight of children at temperatures above 30 РC.
Shelf life
3 years.
Active ingredient
Metoprolol
Conditions of drug supply
d61 eptu
dosage form
tablets
Prescribed
Prescribed
For adults prescribed by a doctor
AstraZeneca, Britain
Film-coated sustained-release tablets.
Packing
14 pcs. 25 mg each.
Pharmacological action
Selective beta1-blocker without internal sympathomimetic activity. It has a slight membrane stabilizing effect and does not show the activity of a partial agonist.
Metoprolol reduces or inhibits the agonistic effect that catecholamines, released during nervous and physical stresses, exert on the cardiac activity. This means that metoprolol has the ability to prevent an increase in heart rate, minute volume 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 the drug Betalok® ZOK is used, a constant concentration of the drug in the blood plasma is observed and a stable clinical effect is achieved (blockade of 1-adrenergic receptors) for more than 24 hours.
Due to the lack of apparent peak plasma concentrations, Betaloc® ZOK is clinically characterized by better selectivity for β 1 -adrenoreceptors compared to conventional tablet forms of beta1-address oblokatorov. In addition, the potential risk of side effects observed at peak plasma concentrations of the drug, such as bradycardia and weakness in the legs when walking, is significantly reduced.
Betalok® ZOK in combination with beta2-adrenergic agonists may be prescribed to patients with symptoms of obstructive pulmonary disease. When combined with beta2-adrenergic agonists, Betaloc® ZOK in therapeutic doses has a lesser effect on bronchodilation caused by beta2-adrenergic agonists than non-selective beta-blockers. Metoprolol to a lesser extent than non-selective beta-blockers affects insulin production and carbohydrate metabolism. The effect of the drug on the reaction of the cardiovascular system under hypoglycemia is significantly less pronounced compared with non-selective beta-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 position, and during exercise. At the beginning of metoprolol therapy, an increase in OPSS is noted. With prolonged use, a decrease in blood pressure is possible due to a decrease in OPSS with a constant cardiac output.
In a MERIT-HF study of survival in chronic heart failure (NYHA Class II-IV functional class) with a reduced ejection fraction ( 0.4), which included 3991 patients, Betalok® ZOK showed an increase in survival and a decrease in hospitalization rates. With prolonged 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 Betaloc® ZOK showed an increase in the ejection fraction of the left ventricle, a decrease in the final systolic and final diastolic volumes of the left ventricle.
The quality of life during the treatment with Betalok® ZOK does not deteriorate or improve. Improving the quality of life during treatment with Betaloc® ZOK was observed in patients after myocardial infarction.
Indications
Arterial hypertension.
Angina pectoris.
Stable symptomatic chronic heart failure with impaired systolic function of the left ventricle (as an adjunct therapy to the main treatment for heart failure).
To reduce mortality and recurrence of heart attack after the acute phase of myocardial infarction.
Heart rhythm disturbances, including supraventricular tachycardia, decreased ventricular contractions with atrial fibrillation and ventricular extrasystoles.
Functional disorders of the heart, accompanied by tachycardia.
Prevention of migraine attacks.
Contraindications
AV block II and III degree.
Chronic heart failure in the decompensation stage.
Continuous or intermittent therapy with inotropic drugs aimed at stimulating -adrenoreceptors.
Clinically significant sinus bradycardia.
SSSU.
Cardiogenic shock.
Severe severe disturbances in peripheral arterial circulation (including with the threat of gangrene).
Arterial hypotension.
Patients with suspected acute myocardial infarction with a heart rate of less than 45 beats / min, a PQ interval of more than 0.24 s, or a systolic blood pressure of less than 100 mmHg.
IV administration of slow calcium channel blockers (like verapamil).
Children and adolescents under 18 years of age (efficacy and safety not established).
Hypersensitivity to the drug.
Hypersensitivity to other beta-blockers.
Precautions: use the drug for grade I AV blockade, Prinzmetal angina, bronchial asthma, COPD, diabetes mellitus, severe renal failure, metabolic acidosis, together with cardiac glycosides.
Use during pregnancy and lactation
Like most Betalok® ZOK preparations should not be prescribed during pregnancy and during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or baby.
Like other antihypertensive drugs, beta-blockers can cause side effects, such as bradycardia in the fetus, newborns or breastfed babies.
The amount of metoprolol excreted in breast milk and the beta-blocking effect in a breast-fed baby (when the mother is taking metoprolol in therapeutic doses) are insignificant.
Special instructions
Patients receiving beta-blockers should not be given iv calcium channel blockers (like verapamil).
Patients with bronchial asthma or COPD should be prescribed concomitant therapy with beta2-adrenergic agonist. BetalokВ® ZOK should be prescribed in the minimum effective dose. In this case, an increase in the dose of beta2-adrenergic agonist may be required.
It is not recommended to prescribe non-selective beta-blockers to patients with Prinzmetal angina. Selective beta-blockers should be given with caution to this group of patients.
When using beta1-blockers, the risk of their effect on carbohydrate metabolism or the ability to mask the symptoms of hypoglycemia is significantly less than when using non-selective beta-blockers.
In patients with chronic heart failure in the decompensation stage, before the appointment of BetalokВ® ZOK, compensation must be achieved and maintained during treatment with the drug.
Very rarely, with BetalocВ® ZOK therapy, in patients with impaired conduction, a worsening of the condition can occur up to AV block. If bradycardia develops during treatment, the dose of the drug must be reduced or the drug should be gradually withdrawn.
During the period of use of the drug, intensification of symptoms of peripheral arterial circulation disorders is possible, mainly due to a decrease in blood pressure.
Caution should be exercised when administering the drug to patients with severe renal failure, with metabolic acidosis, co-administration with cardiac glycosides.
In patients taking beta-blockers, anaphylactic shock is more severe. The use of epinephrine (adrenaline) in therapeutic doses does not always lead to the achievement of the desired clinical effect while taking metoprolol.
Alpha-blocker should be given to patients with pheochromocytoma at the same time as BetalocВ® ZOK.
Abrupt withdrawal of beta-blockers is dangerous, especially in high-risk patients, and should therefore be avoided. If it is necessary to cancel the drug, it should be done gradually, for at least 2 weeks, with a two-fold reduction in the dose of the drug at each stage, until the final dose of 12.5 mg (1/2 tab. 25 mg) is reached, which should be take at least 4 days until the drug is completely discontinued. When symptoms appear (for example, increased symptoms of angina pectoris, increased blood pressure), a slower withdrawal regimen is recommended. Abrupt abolition of beta-blocker can lead to a worsening of the course of chronic heart failure and an increased risk of myocardial infarction and sudden death.
In case of surgery, inform the anesthetist that the patient is taking BetalocВ® ZOK. To patients who have surgery, it is not recommended to discontinue therapy with beta-blockers. Avoid prescribing the drug in high doses without prior titration of the dose to patients with cardiovascular risk factors undergoing non-cardiac surgery due to the increased risk of bradycardia, arterial hypotension and stroke, including fatal.
Clinical trial data on efficacy and safety in patients with severely stable symptomatic chronic heart failure (NYHA Class IV Grade) are limited. The treatment of such patients should be carried out by doctors with special knowledge and experience.
Patients with symptomatic heart failure combined with acute myocardial infarction and unstable angina were excluded from the studies, on the basis of which the indications for prescription were determined. The effectiveness and safety of the drug for this group of patients is not described. The use of the drug in unstable heart failure in the stage of decompensation is contraindicated.
Use in pediatrics
Experience with the use of BetalocВ® ZOK in children is limited.
Effect on the ability to drive vehicles and control mechanisms
When driving vehicles and engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions, it should be borne in mind that dizziness and fatigue can be observed when taking BetalokВ® ZOK.
Composition
1 tablet contains:
Active substances:
metoprolol succinate - 23.75 mg, which corresponds to the content of: metoprolol tartrate 25 mg, metoprolol 19.5 mg.
Excipients:
ethyl cellulose - 21.5 mg,
hyprolose - 6.13 mg,
hypromellose - 5.64 mg,
microcrystalline cellulose - 94.9 mg,
paraffin - 60 ?g,
macrogol - 1.41 mg ,
silicon dioxide - 14.6 mg,
sodium stearyl fumarate - 241 ?g,
titanium dioxide - 1.41 mg.
Dosage and administration of
Bradycardia should be avoided when selecting a dose.
For arterial hypertension: the dose is 50-100 mg 1 time / day. If necessary, the dose can be increased to 100 mg 1 time / day or Betalok® ZOK can be used in combination with other antihypertensive drugs (preferably a diuretic and a calcium channel blocker, a dihydropyridine derivative).
With angina pectoris: the dose is 100-200 mg 1 time / day. If necessary, Betalok® ZOK can be used in combination with another antianginal drug.
In case of stable symptomatic chronic heart failure with impaired systolic function of the left ventricle: Betalok® ZOK can be prescribed to patients who have not had exacerbation episodes during the last 6 weeks and have not had changes in the main therapy during the last 2 weeks. Therapy of heart failure with beta-blockers can sometimes lead to a temporary worsening of the symptomatic picture. In some cases, it is possible to continue therapy or reduce the dose, and in some cases, it may be necessary to discontinue the drug.
In stable chronic heart failure of the II functional class: the recommended initial dose for the first 2 weeks is 25 mg 1 time / day. After 2 weeks, the dose can be increased to 50 mg 1 time / day and then can be doubled every 2 weeks. The maintenance dose for long-term treatment is 200 mg 1 time / day.
With stable chronic heart failure of the III and IV functional classes: the recommended initial dose for the first 2 weeks is 12.5 mg 1 time / day. The dose is selected individually. During the period of increasing the dose, the patient should be monitored, as in some patients, heart failure symptoms may worsen. After 1-2 weeks, the dose can be increased to 25 mg 1 time / day, then after another 2 weeks - up to 50 mg 1 time / day. With good tolerance, you can double the dose every 2 weeks until a maximum dose of 200 mg is reached 1 time / day.
In case of arterial hypotension and / or bradycardia: a reduction in concomitant therapy or a reduction in the dose of Betalok® ZOK may be necessary. Arterial hypotension at the beginning of therapy does not necessarily indicate that this dose of Betalock ZOK will not be tolerated with further long-term treatment. However, the dose should not be increased until the condition is stabilized. Renal function monitoring may also be required.
In case of cardiac arrhythmias: the drug is prescribed in a dose of 100-200 mg 1 time / day.
For maintenance treatment after myocardial infarction: the drug is prescribed at a dose of 200 mg 1 time / day.
For functional disorders of cardiac activity accompanied by tachycardia: the dose is 100 mg 1 time / day, if necessary, the dose can be increased to 200 mg / day.
For the prevention of migraine attacks: prescribed in a dose of 100-200 mg 1 time / day.
Betalok® ZOK is intended for daily use 1 time / day (preferably in the morning). The Betalok® ZOK tablet should be swallowed with a liquid. Tablets can be divided in half, but should not be chewed or crumbled. Eating does not affect the bioavailability of the drug.
In patients with impaired renal function, as well as in elderly patients: there is no need to adjust the dose of the drug.
In patients with impaired liver function: usually dose adjustment is not required due to the low degree of binding of metoprolol to plasma proteins. However, in severely impaired liver function (in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.
Side effects of
The following criteria were used to assess the incidence of cases:
Very often (> 10%).
Often (1-9.9%).
Infrequently (0.1-0.9%).
Rarely (0.01-0.09%).
Very rare (<0.01%).
From the cardiovascular system: often - bradycardia, orthostatic arterial hypotension (very rarely accompanied by fainting), cold extremities, palpitations, infrequent - temporary increase in symptoms of heart failure, AV block I degree, cardiogenic shock in patients with acute myocardial infarction, edema, pain in the heart rarely — other conduction disturbances, arrhythmias very rarely — gangrene (in patients with severe peripheral circulatory disorders).
From the side of the central nervous system and peripheral nervous system: very often - increased fatigue often - dizziness, headache infrequently - paresthesias, cramps, depression, decreased ability to concentrate, drowsiness or insomnia, nightmares rarely - increased nervous irritability, anxiety very rarely - memory impairment, amnesia, depression, hallucinations.
From the digestive system: often - nausea, abdominal pain, diarrhea, constipation infrequently - vomiting rarely - dry mucous membrane of the oral cavity, impaired liver function very rarely - hepatitis.
From the hemopoietic system: very rarely - thrombocytopenia.
From the respiratory system: often - shortness of breath with physical exertion infrequently - bronchospasm rarely - rhinitis.
From the musculoskeletal system: very rarely - arthralgia.
On the part of the sensory organs: rarely - dryness and / or irritation of the eyes, conjunctivitis, visual impairment is very rare - ringing in the ears, disturbances in taste.
Dermatological reactions: infrequently - skin rash (like psoriasis-like urticaria), increased sweating rarely - hair loss is very rare - photosensitivity, exacerbation of psoriasis.
Other: sometimes - weight gain rarely - impotence, sexual dysfunction.
Betalok® ZOK is well tolerated by patients, side effects are mostly mild and reversible.
Drug interactions
Metoprolol is a substrate of CYP2D6, and therefore, drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) can affect plasma concentration.
Combinations to avoid
Derivatives of barbituric acid: barbiturates enhance the metabolism of metoprolol due to the induction of enzymes (the study was conducted with phenobarbital).
Propafenone: when prescribing propafenone to 4 patients receiving metoprolol, a 2-5-fold increase in the concentration of metoprolol in the blood plasma was noted, while in 2 patients, side effects characteristic of metoprolol were noted. This interaction was confirmed in a study of 8 volunteers. The interaction is probably due to the inhibition by propafenone, like quinidine, of the metabolism of metoprolol via the CYP2D6 isoenzyme. Taking into account the fact that propafenone has the properties of a beta-blocker, the combined administration of metoprolol and propafenone does not seem appropriate.
Verapamil: A combination of beta-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure. Verapamil and beta-blockers have a complementary inhibitory effect on AV conduction and sinus node function.
Combinations, the use of which may require dose adjustment of Betaloc® ZOK
Class I antiarrhythmic drugs: when combined with beta-adrenergic blocking agents, a negative inotropic effect may be added, resulting in serious hemodynamic side effects in patients with impaired left ventricular function. A similar combination should also be avoided in patients with CVS and impaired AV conduction. The interaction is described by the example of a disopyramid.
Amiodarone: co-administration with metoprolol can lead to severe sinus bradycardia. Considering the extremely long T1 / 2 of amiodarone (50 days), the possible interaction should be considered long after the withdrawal of amiodarone.
Diltiazem: diltiazem and beta-blockers mutually reinforce the inhibitory effect on AV conduction and sinus node function. With a combination of metoprolol with diltiazem, cases of severe bradycardia were noted.
NSAIDs: NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction has been reported with a combination with indomethacin and probably will not be observed with a combination with sulindac. Negative interactions have been observed in studies with diclofenac.
Diphenhydramine: diphenhydramine reduces the biotransformation of metoprolol to -hydroxymethoprolol by 2.5 times. At the same time, an increase in the action of metoprolol is 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. The interaction was also noted in the group of healthy volunteers. It is assumed that similar reactions can be observed with the use of epinephrine in conjunction with local anesthetics in case of accidental entry into 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 can increase diastolic blood pressure to pathological values in healthy volunteers. Propranolol basically inhibits the increase in blood pressure caused by phenylpropanolamine. However, beta-blockers can cause paradoxical hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported with phenylpropanolamine.
Quinidine: quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (in Sweden, approximately 90% of the population), mainly causing a significant increase in the plasma concentration of metoprolol and increased blockade of β-adrenoreceptors. It is believed that such an interaction is also characteristic of other beta-blockers, in the metabolism of which the isoenzyme CYP2D6 is involved.
Clonidine: hypertensive reactions with abrupt cancellation of clonidine may be enhanced while taking beta-blockers. With joint use, if it is necessary to cancel clonidine, discontinuation of beta-blockers should begin a few days before the cancellation of clonidine.
rifampicin: rifampicin can enhance the metabolism of metoprolol, reducing its concentration in blood plasma. Patients taking metoprolol and other beta-blockers (eye drops) or MAO inhibitors at the same time should be closely monitored.
In patients with beta-blockers, inhaled anesthetics enhance the cardiac depressant effect.
While taking beta-blockers, patients receiving oral hypoglycemic agents may need a dose adjustment.
Plasma concentration of metoprolol may increase with cimetidine or hydralazine.
Cardiac glycosides when used together with beta-blockers can increase AV conduction time and cause bradycardia.
Overdose
Metoprolol at a dose of 7.5 g in an adult caused lethal intoxication. In a 5 year old child taking 100 mg of metoprolol, no signs of intoxication were observed after gastric lavage. Taking 450 mg of metoprolol by a teenager for 12 years resulted in moderate intoxication. The intake of 1.4 g and 2.5 g of metoprolol in adults caused moderate and severe intoxication, respectively. The intake of 7.5 g by adults resulted in extremely severe intoxication.
Symptoms: The most serious are the symptoms from the cardiovascular system, but sometimes, especially in children and adolescents, symptoms from the CNS and pulmonary function suppression, bradycardia, AV-blockade of I-III degree, asystole, severe decrease in blood pressure may prevail weak peripheral perfusion, heart failure, cardiogenic shock, pulmonary function depression, apnea, increased fatigue, impaired consciousness and loss, tremor, convulsions, sweating, paraesthesia, bronchospasm, nausea, vomiting, esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia transient effects.
Concomitant use of alcohol, antihypertensive agents, quinidine or barbiturates may worsen the patient's condition. The first signs of overdose can be observed 20 min-2 h after drug administration.
Treatment: Activation of activated charcoal, if necessary - gastric lavage.
Atropine at a dose of 0.25-0.5 mg / v for adults and 10-20 mcg / kg for children should be given before gastric lavage (due to the risk of vagus nerve stimulation).
Intubation and IVL are performed if necessary to maintain airway patency.
Terbutaline may be injected or inhaled for the treatment of bronchospasm.
Followsto replenish BCC, to carry out an infusion of glucose. Atropine 1.0-2.0 mg I / O, if necessary repeat the administration (especially with vaginal symptoms). ECG monitoring.
Infusion of dobutamine or dopamine is indicated in case of myocardial depression. You can use glucagon 50-150 mcg / kg I / O at intervals of 1 min. In some cases, it may be effective to add epinephrine to therapy.
Sodium (chloride or bicarbonate) solutions are infused with arrhythmia and enlarged ventricular (QRS) complex. Installation of an artificial rhythm driver is possible.
Resuscitation may require several hours for heart failure due to overdose.
Symptomatic treatment is performed.
Storage conditions
Keep out of the reach and sight of children at temperatures above 30 РC.
Shelf life
3 years.
Active ingredient
Metoprolol
Conditions of drug supply
d61 eptu
dosage form
tablets
Prescribed
Prescribed
For adults prescribed by a doctor
AstraZeneca, Britain
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