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Beloc

Beloc
Beloc used for arterial hypertension, angina pectoris; stable symptomatic chronic heart failure systolic function of the left ventricle (as an adjunct therapy to the main treatment of heart failure);

Brand: Metoprolol

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: September 2023
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Beloc 40 mg
360 pills - 40 mg
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$291.81 $0.81 $320.07 Add to cart
270 pills - 40 mg
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180 pills - 40 mg
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120 pills - 40 mg
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$116.93 $1.30 $36.04 Add to cart
60 pills - 40 mg $86.95 $1.45 $15.03 Add to cart
30 pills - 40 mg $50.99 $1.70 No Add to cart
Beloc 20 mg
360 pills - 20 mg
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$161.91 $0.45 $137.97 Add to cart
270 pills - 20 mg
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Product description

Pharmacological action of Beloc

Buy Beloc in Canada

Metoprolol is a beta1blocker that blocks βreceptors1-adrenergic-adrenergicin doses significantly lower than the doses required for blocking 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, minute volume and an increase in cardiac contractility, as well as an increase in blood pressure caused by a sharp release of catecholamines.

Unlike conventional tablet dosage formsselective beta1adrenoblokatorov(including metoprolol tartrate), when using the drug Betalok® KRC observed constant drug concentration in blood plasma and ensures a stable clinical effect (βblockade)1-adrenoceptor  over 24 h.

Because no obvious peak plasma concentration clinically Betalok® KRChas a better selectivity to β1-adrenoceptors compared to conventional tablet formulations beta1adrenoblokatorov. In addition, the potential risk of side effects observed at peak plasma concentrations of the drug, for example, bradycardia and weakness in the legs when walking, is greatly reduced.

Patients with symptoms of obstructive pulmonary disease, if necessary, can be prescribed Beloc® ZOK in combination with beta2-adrenomimetics. When used together with beta2-adrenomimetics, Beloc® ZOK in therapeutic doses has a lesser effect on thecaused by beta2bronchodilation-adrenomimetics 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 conditions of hypoglycemia is much less pronounced in comparison with non-selective beta-blockers.

The use of Beloc® ZOK in arterial hypertension leads to a significant decrease in blood pressure for more than 24 hours, both in the lying and standing position, and during exercise. At the beginning of therapy with metoprolol, there is an increase in OPSS. However, with long-term use, a decrease in blood pressure is possible due to a decrease in OPSS with a constant cardiac output.

The survival MERIT-HF-study in chronic heart failure (II-IV functional class NYHA classification) with a reduced ejection fraction (≤0.4), which included 3991 patients, Betalok® KRCshowed improved survival and reduction in the incidence of hospitalization. With long-term treatment, patients achieved a general improvement in well-being, a decrease in the severity of symptoms (according to NYHA functional classes). Also with the use of drug therapy Betalok® KRCshowed an increase in left ventricular ejection fraction, reduced end-systolic and end-diastolic volume of the left ventricle.

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

Pharmacokinetics

Upon contact with liquid, the tablets rapidly disintegrate, while the active substance is dispersed in the gastrointestinal tract. The release rate of the active substance depends on the acidity of the medium. The duration of therapeutic effect after administration of the drug in the dosage form Betalok® KRC(sustained release tablets) is more than 24 hours, while achieving constant release rate of the active substance over 20 hours. T1/2 is on average 3.5 h.

Betalok® fully KRC 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 major metabolites of metoprolol showed no clinically significant β-blocking effect. About 5% of an oral dose of the drug is excreted in the urine unchanged, the rest of the drug is excreted in the form of metabolites. The connection with blood plasma proteins is low, about 5-10%.

Indications for Beloc® ZOK

Treatment of heart failure with Beloc

  • 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 of heart failure);
  • to reduce mortality and the frequency of re-infarction after the acute phase of myocardial infarction;
  • cardiac arrhythmias, including supraventricular tachycardia, decreased ventricular rate during atrial fibrillation and ventricular extrasystoles;
  • functional disorders of cardiac activity, accompanied by tachycardia;
  • prevention of migraine attacks.

The dosage regimen of Beloc

Beloc tablets packaging

Beloc® ZOK is intended for daily intake 1 time / day, it is recommended to take the drug in the morning.Beloc tablet® ZOKshould be swallowed with some liquid. Tablets (or tablets cut in half) should not be chewed or crumbled. Food intake does not affect the bioavailability of the drug.

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

Arterial hypertension

50-100 mg 1 time / day. If necessary, the dose may be increased up to a dose of 100 mg 1 time / day or apply Beloc® KRCin combination with other antihypertensive agent, preferably a diuretic and a calcium channel blocker dihydropyridine derivative.

Angina

100-200 mg Beloc® KRC 1 time / day. If necessary, another antianginal drug can be added to therapy.

Stable symptomatic chronic heart failure with impaired left ventricular systolic function

Patients should be in the stage of stable chronic heart failure without exacerbations during the last 6 weeks and without 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, in some cases it may be necessary to discontinue the drug.

Stable chronic heart failure, II functional class

The recommended initial dose of Beloc® 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 is 200 mg Beloc® 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 Beloc® 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, symptoms of heart failure may worsen.

After 1-2 weeks, the dose can be increased to 25 mg Beloc® ZOK 1 time / day. Then, after 2 weeks, the dose can be increased to 50 mg 1 time / day. Patients who tolerate the drug, it is possible to double the dose every 2 weeks until reaching a maximum dose of 200 mg Beloc® KRC 1 time / day.

In the case of hypotension and / or bradycardia may need to decrease concomitant therapy or dose reduction Beloc® KRC. Hypotension in early therapy does not necessarily indicate that the dose Beloc® KRC will not be carried during the future long-term treatment. However, the dose should not be increased until the condition has stabilized. Monitoring of kidney function may be required.

Cardiac arrhythmias

100-200 mg Beloc® KRC 1 time / day.

treatment after myocardial infarction

Maintenance200 mg Beloc® ZOK 1 time / day.

Functional disorders of cardiac activity, accompanied by tachycardia

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

Prevention of migraine attacks

100-200 mg Beloc® ZOK 1 time / day.

Renal dysfunction

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

Liver dysfunction

Usually, due to the low degree of binding to plasma proteins, dose adjustment of metoprolol is not required. However, in severely impaired liver function (in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.

Elderly

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

Children

The experience of using Beloc® ZOK in children is limited.


Contraindications to the use of

  • AV block II and III degree;
  • 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 peripheral circulatory disorders (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 sec, 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;
  • IV injection of slow calcium channel blockers (like verapamil);
  • age up to 18 years (efficacy and safety have not been established).

With care use in patients with AV-I blockade degree, Prinzmetal angina, asthma, COPD, diabetes, renal failure, severe, metabolic acidosis, together with cardiac glycosides.

Application of pregnancy and breastfeeding

Like most drugs Beloc® ZOKshould not be administered during pregnancy and lactation, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or the child.

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 breastfed baby (when the mother is taking metoprolol in therapeutic doses) are negligible.

Application for impaired liver function

When prescribing the drug to patients with severe impaired liver function (for example, in patients with severe cirrhosis or porto-caval anastomosis), a dose reduction may be required.

Application for impaired renal function

Use the drug with caution in patients with severe renal failure.

Use in children

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

Use in elderly patients

When prescribing the drug to the elderly, there is no need to adjust the dosage regimen.

Special instructions

Patients receiving beta-blockers should not be administered intravenous blockers of slow calcium channels (like verapamil).

Patients with bronchial asthma or COPD should be prescribed concomitant beta2-adrenomimetic therapy. It is necessary to assign the minimum effective dose Beloc® ZOK, in this case you may need to increase the dose of beta2-adrenomimetika.

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

With the use of beta1-blockers, the risk of their effect on carbohydrate metabolism or the possibility of masking the symptoms of hypoglycemia is much less than with the use of 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, in patients with impaired AV conduction, deterioration may occur (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 withdrawn.

Beloc® 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, simultaneous use 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.

Patients suffering pheochromocytoma, simultaneously with the preparation Beloc® KRCshould be administered alpha-blocker.

Abrupt withdrawal of beta-blockers is dangerous, especially in high-risk patients, and therefore should be avoided. If it is necessary to discontinue the drug, it should be done gradually, over at least 2 weeks, with a two-fold decrease 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 taken as at least 4 days before the complete withdrawal of the drug. When symptoms appear (eg, increased angina symptoms, increased blood pressure), a slower withdrawal regimen is recommended. Abrupt withdrawal of a beta-blocker can lead to an aggravation 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 Beloc® ZOK. Discontinuation of beta-blocker therapy is not recommended for patients who are to undergo surgery. Avoid prescribing the drug in high doses without preliminary titration of doses of the drug to patients with cardiovascular risk factors undergoing noncardiological operations, due to an increased risk of bradycardia, arterial hypotension and stroke, incl. with a lethal outcome.

Data from clinical studies 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 in combination with acute myocardial infarction and unstable angina pectoris were excluded from the studies, on the basis of which the indications for prescription were determined. The efficacy and safety of the drug for this group of patients has not been described. The use of unstable heart failure in the stage of decompensation is contraindicated.

Effects on ability to drive vehicles and management mechanisms

when driving and classes of potentially hazardous activities that require increased attention and psychomotor speed reactions, it should be noted that the application of Beloc® ZOK may experience dizziness, and fatigue.

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. The intake of 450 mg of metoprolol in a 12-year-old teenager resulted in moderate intoxication. The intake of 450 mg of metoprolol in a 12-year-old teenager resulted in moderate intoxication. Admission of 1.4 g and 2.5 g of metoprolol in adults caused moderate and severe intoxication, respectively. Admission of 7.5 g to adults led to extremely severe intoxication.

Symptoms: with an overdose of metoprolol, the most serious symptoms are from the cardiovascular system, however, sometimes, especially in children and adolescents, symptoms from the central nervous system and suppression of pulmonary function, bradycardia, AV blockade of I-III degrees, asystole, pronounced decrease Blood pressure, weak peripheral perfusion, heart failure, cardiogenic shock; suppression of lung function, apnea, as well as increased fatigue, impaired consciousness, loss of consciousness, tremors, convulsions, increased sweating, paresthesia, bronchospasm, nausea, vomiting, possible esophagial spasm, hypoglycemia (especially in children) or hyperglycemia, hyperkalemia; effects on the kidneys; transient myasthenic syndrome; concomitant use of alcohol, antihypertensive drugs, quinidine, or barbiturates may worsen the patient's condition. The first signs of an overdose can be observed 20 minutes to 2 hours after taking the drug.

Treatment: the appointment of activated carbon, if necessary, gastric lavage. 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 stimulation). If necessary, maintain airway patency (intubation) and adequate ventilation. Replenishment of circulating blood volume and glucose infusion. ECG monitoring. Atropine 1.0-2.0 mg IV, if necessary, repeat the introduction (especially in the case of vagal symptoms). In the case of (suppression) of myocardial depression, infusion of dobutamine or dopamine is indicated. You can also use glucagon 50-150 mcg / kg i.v. at intervals of 1 min. In some cases, adding adrenaline to therapy may be effective. For arrhythmias and an enlarged ventricular (QRS) complex, sodium solutions (chloride or bicarbonate) are infused. Installation of an artificial pacemaker is possible. In case of cardiac arrest due to overdose, resuscitation may be necessary for several hours. To stop bronchospasm, terbutaline can be used (by injection or by inhalation). Symptomatic treatment is carried out.

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 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 prescribed to 4 patients treated with metoprolol, there was an increase in the plasma concentration of metoprolol by 2-5 times, while in 2 patients there were side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. Probably, the interaction is due to inhibition by propafenone, like quinidine, of the metabolism of metoprolol by the isoenzyme CYP2D6. Taking into account the fact that propafenone has the properties of a beta-blocker, the joint appointment of metoprolol and propafenone does not seem appropriate.

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

The combinations of the application which may require correction dose Beloc® KRC

Antiarrhythmics class I: when combined with beta-blockers may summation of negative inotropic effect, thereby developing serious adverse hemodynamic effects in patients with impaired left ventricular function. This combination should also be avoided in patients with CVS and AV conduction disorders. The interaction is described using the example of disopyramide.

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

Diltiazem: Diltiazem and beta-blockers mutually enhance the inhibitory effect on AV conduction and sinus node function. With the combination of metoprolol with diltiazem, cases of severe bradycardia have been reported.

NSAIDs: NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction has been reported when combined with indomethacin and probably will not be observed when combined 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, there is an increase in the effect of metoprolol.

Epinephrine (adrenaline): 10 cases of severe arterial hypertension and bradycardia have been reported in patients taking non-selective beta-blockers (including pindolol and propranolol) and receiving epinephrine. Interaction was noted in a group of healthy volunteers. It is assumed that similar reactions can be observed when using epinephrine in conjunction with local anesthetics in case of accidental ingestion 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 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 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 an increase in the blockade of β-adrenergic receptors. It is believed that a similar interaction is characteristic of other beta-blockers, in the metabolism of which the isoenzyme CYP2D6 is involved.

Clonidine: hypertensive reactions with abrupt withdrawal of clonidine may increase with the simultaneous administration of beta-blockers. When used together, if it is necessary to cancel clonidine, the discontinuation of beta-blockers should be started several days before the withdrawal of clonidine.

Rifampicin: Rifampicin can increase the metabolism of metoprolol, decreasing its concentration in blood plasma. Patients simultaneously taking metoprolol and other beta-blockers (eye drops) or MAO inhibitors should be closely monitored.

While taking beta-blockers, inhalation anesthetics enhance the cardiodepressant 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 with cimetidine or hydralazine.

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

Storage conditions of the drug Beloc® ZOK

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


Side effects

Beloc® ZOK is well tolerated by patients, side effects are generally 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 side of the cardiovascular system: often - bradycardia, orthostatic arterial hypotension (very rarely accompanied by fainting), cold extremities, palpitations; infrequently - a temporary increase in the symptoms of heart failure, AV block of the 1st degree, cardiogenic shock in patients with acute myocardial infarction, edema, pain in the region of the heart; 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; infrequently - paresthesia, convulsions, depression, decreased concentration, 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 - dryness of the oral mucosa.

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

Dermatological reactions: infrequently - 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 during exercise; infrequently - bronchospasm; rarely - rhinitis.

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

From the musculoskeletal system: very rarely - arthralgia.

From the side of metabolism: infrequently - an increase in body weight.

From the hematopoietic system: very rarely - thrombocytopenia.

Others: rarely - impotence, sexual dysfunction.