Betaloc Zoc, delayed-release pills 50mg 30pcs

Composition

Active ingredients:

metoprolol succinate – 47.5 mg, which corresponds to the content of: metoprolol tartrate-50 mg, metoprolol-39 mg.

Auxiliary substances:

ethylcellulose-23 mg,

hyprolose-7 mg,

hypromellose-6.2 mg,

microcrystalline cellulose-120 mg,

paraffin-100 mcg,

macrogol-1.6 mg,

silicon dioxide-12 mg,

sodium stearyl fumarate-300 mcg,

titanium dioxide-1.6 mg

Pharmacological action

Antianginal, antihypertensive, antiarrhythmic.

Betaloc ZOK selectively blocks beta-1-adrenergic receptors and interferes with the effects of catecholamines realized through them. Lowers blood pressure, has a membrane-stabilizing effect.

Reduces myocardial oxygen consumption, frequency of angina attacks, and increases exercise tolerance. The duration of beta-1-receptor blockade, which provides a stable clinical effect, is 24 hours.

Indications

• Hypertension, angina pectoris, cardiac arrhythmia, especially supraventricular tachycardia;
• post-infarction period (maintenance therapy), functional cardiac disorders accompanied by palpitations;
• migraine (prevention).

Use during pregnancy and lactation

As with most medications, Betalok ® ZOK should not be administered during pregnancy and lactation, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or child.

Like other antihypertensive drugs, beta-blockers can cause side effects, such as bradycardia in the fetus, newborns, or children who are breastfed.

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

Contraindications

Hypersensitivity, grade II or III AV block, severe sinus bradycardia, sinus node weakness syndrome, decompensated heart failure, cardiogenic shock, peripheral circulatory disorders.

Side effects

From the cardiovascular system:  often-bradycardia, orthostatic hypotension (very rarely accompanied by syncope), cold extremities, palpitation sensation; infrequently-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 disorders, arrhythmias; very rarely-gangrene (in patients with severe peripheral circulatory disorders).

From the central nervous system and peripheral nervous system:  very often-increased fatigue; often-dizziness, headache; infrequently-paresthesia, convulsions, depression, decreased ability to concentrate, drowsiness or insomnia, nightmares; rarely-increased nervous excitability, anxiety; very rarely-memory disorders, amnesia, depression, hallucinations.

From the digestive system:  often – nausea, abdominal pain, diarrhea, constipation; infrequently-vomiting; rarely-dryness of the oral mucosa, liver function disorders; very rarely-hepatitis.

From the hematopoietic system:  very rarely – thrombocytopenia.

Respiratory system disorders:  often-shortness of breath during exercise; infrequently-bronchospasm; rarely-rhinitis.

Musculoskeletal disorders:  very rarely – arthralgia.

From the side of the senses:  rarely – dryness and / or irritation of the eyes, conjunctivitis, visual impairment; very rarely-ringing in the ears, impaired taste sensations.

Dermatological reactions:  infrequently-skin rash (like psoriasis-like urticaria), increased sweating; rarely-hair loss; very rarely-photosensitization, exacerbation of psoriasis.

Other services:  sometimes-weight gain; rarely-impotence, sexual dysfunction.

Betalok ® ZOK is well-tolerated by patients, and side effects are generally mild and reversible.

Interaction

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

Combinations to avoid

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

Propafenone:  when propafenone was administered to 4 patients treated with metoprolol, there was a 2-5-fold increase in the concentration of metoprolol in blood plasma, while 2 patients had side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. Probably, the interaction is caused by propafenone inhibition, like quinidine, of metoprolol metabolism by the CYP2D6 isoenzyme. Taking into account the fact that propafenone has beta-blocker properties, co-use of metoprolol and propafenone is not advisable.

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

Combinations that may require dose adjustment of Betalok ® ZOK

Class I antiarrhythmic drugs:  when combined with beta-blockers, the negative inotropic effect can be summed up, as a result of which serious hemodynamic side effects develop in patients with impaired left ventricular function. This combination should also be avoided in patients with SSSU and impaired AV conduction. The interaction is described on the example of disopyramide.

Amiodarone:  concomitant use with metoprolol may result in severe sinus bradycardia. Taking into account the extremely long T1 / 2 of amiodarone (50 days), possible interactions should be considered long after the withdrawal 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, there were cases of severe bradycardia.

NSAIDs:  NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction has been reported in combination with Indometacin and probably will not be observed in combination with sulindac. Negative interactions have been reported in studies with diclofenac.

Diphenhydramine:  diphenhydramine reduces the biotransformation of metoprolol to alpha-hydroxymethoprolol by 2.5 times. At the same time, there is an increase in the effect of metoprolol.

Epinephrine (epinephrine):  10 cases of severe hypertension and bradycardia were reported in patients treated with non-selective beta-blockers (including pindolol and propranolol) and treated with epinephrine. Interaction was also observed in the group of healthy volunteers. It is assumed that similar reactions can be observed when using epinephrine together with local anesthetics in case of accidental contact with the vascular bed. Apparently, this risk is much lower when using 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 mainly prevents 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 while taking phenylpropanolamine.

Quinidine:  quinidine inhibits metoprolol metabolism in a special group of patients with rapid hydroxylation (approximately 90% of the population in Sweden), causing mainly a significant increase in the plasma concentration of metoprolol and increased beta-adrenergic blockade. It is believed that this interaction is also characteristic of other beta-blockers, in the metabolism of which the CYP2D6 isoenzyme is involved.

Clonidine:  hypertensive reactions with abrupt withdrawal of clonidine may increase with simultaneous use of beta-blockers. When used together, if clonidine withdrawal is necessary, discontinuation of beta-blockers should begin several days before clonidine withdrawal.

Rifampicin:  rifampicin may increase 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 carefully monitored.

While taking beta-blockers, inhaled anesthetics increase the cardiodepressive effect.

While taking beta-blockers, patients receiving oral hypoglycemic agents may need to adjust the dose of the latter.

The plasma concentration of metoprolol may increase when taking cimetidine or hydralazine.

Cardiac glycosides, when combined with beta-blockers, can increase the time of AV conduction and cause bradycardia.

How to take it, course of use and dosage

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

With 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 use Betalok ® ZOK in combination with other antihypertensive drugs (preferably a diuretic and a calcium channel blocker dihydropyridine derivative).

For 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 stable symptomatic chronic heart failure with impaired left ventricular systolic function: Betalok ® ZOK can be prescribed to patients who have not had any episodes of exacerbation in the last 6 weeks and have not changed the main therapy in 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, and in some cases, it may be necessary to cancel the drug.

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

With stable chronic heart failure of functional classes III and IV: The recommended starting 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, the symptoms of heart failure may worsen. After 1-2 weeks, the dose can be increased to 25 mg 1 time/day, then after another 2 weeks – to 50 mg 1 time/day. If well tolerated, the dose can be doubled every 2 weeks until a maximum dose of 200 mg once a day is reached.

In case of hypotension and / or bradycardia: it may be necessary to reduce concomitant therapy or reduce the dose of Betalok ® ZOK. Arterial hypotension at the beginning of therapy does not necessarily indicate that this dose of Betaloc ZOK will not be tolerated with further long-term treatment. However, the dose should not be increased until the condition stabilizes. You may also need to monitor your kidney function.

For cardiac arrhythmias: the drug is prescribed at 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.

With functional disorders of the heart, 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: assign a dose of 100-200 mg 1 time/day.

Betalok ® ZOK is intended for daily use 1 time/day (preferably in the morning). A tablet of Betalok ® ZOK should be swallowed with liquid. Tablets can be divided in half, but should not be chewed or crumbled. Food intake 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 of the drug is not required due to the low degree of binding of metoprolol to plasma proteins. However, in severe hepatic impairment (in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.

Overdose

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

Symptoms: the most serious are symptoms 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, weak peripheral perfusion, heart failure, cardiogenic shock, depression of lung function, apnea, increased fatigue, impaired and loss of consciousness, tremor, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, esophageal spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia; effects on the kidneys; transient myasthenic syndrome.

Concomitant use of alcohol, antihypertensive drugs, quinidine, or barbiturates may worsen the patient’s condition. The first signs of overdose may occur 20 minutes-2 hours after taking the drug.

Treatment: taking activated charcoal, if necessary – gastric lavage.

Atropine at a dose of 0.25-0.5 mg iv for adults and 10-20 mcg / kg for children should be administered before gastric lavage (due to the risk of vagus nerve stimulation).

If it is necessary to maintain airway patency, intubation and mechanical ventilation are performed.

To stop bronchospasm, terbutaline can be used by injection or inhalation.

It is necessary to fill the BCC, conduct a glucose infusion. Atropine 1.0-2.0 mg IV, if necessary, repeat the use (especially with vagal symptoms). ECG monitoring.

In the case of myocardial depression, infusion of dobutamine or dopamine is indicated. You can use glucagon 50-150 mcg / kg iv with an interval of 1 min. In some cases, the addition of epinephrine to therapy may be effective.

In case of arrhythmia and dilated ventricular (QRS) complex, sodium solutions (chloride or bicarbonate) are infused. An artificial pacemaker can be installed.

In case of cardiac arrest due to an overdose, resuscitation measures may be required for several hours.

Symptomatic treatment is performed.

Special instructions

Patients receiving beta-blockers should not be given intravenous slow calcium channel blockers (such as verapamil).

Patients with asthma or COPD should receive concomitant beta-2-adrenomimetic therapy. Betalok ® ZOK should be administered at the lowest effective dose. In this case, it may be necessary to increase the dose of beta-2-adrenomimetic.

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

When using beta-1-blockers, the risk of their influence on carbohydrate metabolism or the possibility of masking the symptoms of hypoglycemia is significantly lower than when using non-selective beta-blockers.

In patients with decompensated chronic heart failure, compensation should be achieved and maintained during treatment with Betalok® ZOK prior to prescribing.

Very rarely, during therapy with Betalok ® ZOK, patients with impaired conductivity may experience deterioration of the condition up to AV block. If bradycardia develops during treatment, the dose of the drug should be reduced or the drug should be gradually discontinued.

During the period of use of the drug, it is possible to increase the symptoms of peripheral arterial circulation disorders, mainly due to a decrease in blood pressure.

Caution should be exercised when prescribing the drug to patients with severe renal insufficiency, with metabolic acidosis, co-use with cardiac glycosides.

In patients taking beta-blockers, anaphylactic shock occurs in a more severe form. The use of epinephrine (epinephrine) in therapeutic doses does not always lead to the achievement of the desired clinical effect against the background of taking metoprolol.

Patients with pheochromocytoma should be treated with an alpha-blocker concomitantly with Betalok 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 carried out 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 is reached (1/2 tab. 25 mg), which should be taken at least 4 days before complete discontinuation of the drug. If symptoms appear (for example, increased angina symptoms, increased blood pressure), a slower withdrawal regimen is recommended. Abrupt withdrawal of a 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 surgical intervention, the anesthesiologist should be informed that the patient is taking Betalok ® ZOK. Discontinuation of beta-blocker therapy is not recommended for patients undergoing surgery. Avoid prescribing the drug in high doses without prior titration of doses of the drug to patients with cardiovascular risk factors undergoing non-cardiological operations, due to the increased risk of bradycardia, hypotension and stroke, including those with a fatal outcome.

Data from clinical trials on efficacy and safety in patients with severe stable symptomatic chronic heart failure (NYHA class IV) are limited. Treatment of such patients should be carried out by doctors with special knowledge and experience.

Patients with symptomatic heart failure in combination with acute myocardial infarction and unstable angina were excluded from studies based on which indications for use were determined. The efficacy and safety of the drug for this group of patients is not described.The use of the drug in unstable heart failure in the decompensation stage is contraindicated.

Use in pediatrics

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

Influence on the ability to drive motor vehicles and manage mechanisms

When driving vehicles and engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions, it should be borne in mind that dizziness and fatigue may occur when taking Betalok® ZOK.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Metoprolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Hypertension, Angina, Arrhythmia, Migraine