Betaloc, pills 100mg, 100pcs

Composition

1 tablet contains:

Active ingredient:

metoprolol tartrate 100 mg.

Auxiliary substances:

lactose monohydrate,

magnesium stearate,

microcrystalline cellulose,

sodium carboxymethyl starch,

colloidal anhydrous silicon dioxide,

povidone.

Pharmacological action

Metoprolol is a β1-adrenoblocker that blocks β1-receptors at doses significantly lower than the doses required to block β2-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 increased contractility of the heart, as well as an increase in blood pressure caused by a sharp release of catecholamines.

If necessary, patients with symptoms of obstructive pulmonary disease can be prescribed metoprolol in combination with beta_{– 2}-adrenomimetics. When combined with beta_{– 2}-adrenomimetics, Betaloc® in therapeutic doses has a lesser effect on the bronchodilation caused by beta_-2-adrenomimetics than non-selective beta-blockers. Metoprolol affects insulin production and carbohydrate metabolism to a lesser extent than non-selective beta-blockers. The effect of Betalok® on the response of the cardiovascular system under hypoglycemic conditions is significantly less pronounced compared to non-selective p-blockers.

Clinical studies have shown that Betaloc® can cause a slight increase in triglyceride levels and a decrease in the content of free fatty acids in the blood. In some cases, there was a slight decrease in the high-density lipoprotein (HDL) fraction, which is less pronounced than in the case of non-selective P-blockers. However, one clinical study showed a significant reduction in serum total cholesterol levels when treated with metoprolol for several years.

The quality of life during treatment with Betalok® does not worsen or improve. Improved quality of life during treatment with Betalok® was observed in patients after myocardial infarction.

Indications

• Arterial hypertension: lower blood pressure and reduce the risk of cardiovascular and coronary death (including sudden death).
• Angina pectoris.
• Cardiac arrhythmias, including supraventricular tachycardia.
• In complex therapy after myocardial infarction.
• Functional disorders of cardiac activity accompanied by tachycardia.
• Prevention of migraine attacks.
• Hyperthyroidism (complex therapy).

Use during pregnancy and lactation

As with most medications, Betaloc® should not be administered during pregnancy or during breast-feeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or child. Like other antihypertensive agents, 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

• Grade II and III atrioventricular block.
• Heart failure in the stage of decompensation.
• Patients receiving long-term or intermittent therapy with inotropic agents acting on beta-adrenergic receptors.
• Clinically significant sinus bradycardia.
• Sinus node weakness syndrome.
• Cardiogenic shock.
• Severe peripheral circulatory disorders.
• Arterial hypotension.
• Betalok is contraindicated in patients with acute myocardial infarction with a heart rate of less than 45 beats per minute, a PQ interval of more than 0.24 seconds, or a systolic blood pressure of less than 100 mm Hg.
• For serious peripheral vascular diseases with the threat of gangrene.
• Intravenous use of slow calcium channel blockers such as verapamil is contraindicated in patients receiving beta-blockers.
• Age up to 18 years (efficacy and safety have not been established).
• Known hypersensitivity to metoprolol and its components or to other beta-blockers.

With caution: atrioventricular block I degree, Prinzmetal angina pectoris, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis, bronchial asthma), diabetes mellitus, severe renal failure.

Side effects

Betalok is well tolerated by patients and the side effects are mostly mild and reversible.

As a result of clinical studies or when using the drug Betalok (metoprolol tartrate) in clinical practice, the following undesirable side effects have been described. In many cases, a causal relationship with treatment with Betalok has not been established.

The following criteria were used to assess the frequency of cases:

• Very often ( > 10%).
• Often (1-9.9%).
• Infrequently (0.1-0.9%).
• Rarely (0.01-0.09%).
• Very rare (

Cardiovascular system:  often-bradycardia, postural disturbances (very rarely accompanied by syncope), cold extremities, palpitations; infrequently-temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction; AV block I degree; rarely-other cardiac conduction disorders, arrhythmias; very rarely-gangrene in patients with previous severe peripheral circulatory disorders.

Central Nervous System:  very often-increased fatigue; often-dizziness, headache; rarely-increased nervous excitability, anxiety, impotence/sexual dysfunction; infrequently-paresthesia, convulsions, depression, decreased attention, drowsiness or insomnia, nightmares; very rarely-amnesia/memory disorders, depression, hallucinations.

GASTROINTESTINAL TRACT:  often – nausea, abdominal pain, diarrhea, constipation; infrequently-vomiting; rarely-dry mouth.

Liver:  rarely-liver function disorders.

Skin conditions:  infrequently-rash (in the form of urticaria), increased sweating; rarely-hair loss; very rarely-photosensitization, exacerbation of psoriasis.

Respiratory organs:  often-shortness of breath during physical exertion; infrequently-bronchospasm in patients with bronchial asthma; rarely-rhinitis.

Sensory organs:  rarely-visual disturbances, dryness and / or eye irritation, conjunctivitis; very rarely-ringing in the ears, impaired taste sensations.

Metabolism:  infrequently – weight gain.

Musculoskeletal disorders:  very rarely – arthralgia.

Blood:  very rarely – thrombocytopenia.

Interaction

Co-use of Betalok®should be avoided with the following medications:

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

Propafenone: when propafenone was administered to four patients treated with metoprolol, there was a 2-5-fold increase in the plasma concentration of metoprolol, while two patients had side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. The interaction is probably due to the inhibition of propafenone, like quinidine, of metoprolol metabolism by the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a beta-blocker, co-use of metoprolol and propafenone is not advisable.

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

Combination of Betalok® with the following medications, it may require dose adjustment:

Class I antiarrhythmics: Class I antiarrhythmics and beta-blockers can add up to a negative inotropic effect, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function. This combination should also be avoided in patients with sinus node weakness syndrome and impaired AV conduction. The interaction is described on the example of disopyramide.

Amiodarone: Concomitant use of amiodarone and metoprolol may result in severe sinus bradycardia. Taking into account the extremely long half-life 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.

Nonsteroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect of beta-blockers. This interaction is best documented for indomethacin. The described interaction was not observed for sulindaq. In studies with diclofenac, the described reaction was not observed.

Diphenhydramine: Diphenhydramine reduces the clearance 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 have been reported in patients receiving non-selective beta-blockers (including pindolol and propranolol) and epinephrine (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. It is assumed that this risk is much lower with the use of cardioselective beta-blockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure to pathological values in healthy volunteers. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, beta-blockers may cause periodoxic 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), mainly causing a significant increase in the plasma concentration of metoprolol and an increase in beta-blockade. It is believed that this interaction is also characteristic of other p-blockers in the metabolism of which cytochrome P4502D6 is involved.

Clonidine: Hypertensive reactions with abrupt withdrawal of clonidine may increase with the combined use of beta-blockers. When used together, if clonidine is discontinued, discontinuation of beta-blockers should begin several days before clonidine is discontinued.

Rifampicin: Rifampicin may enhance metoprolol metabolism by reducing the plasma concentration of metoprolol.

The concentration of metoprolol in blood plasma may increase when combined with cimetidine, hydralazine, selective serotonin inhibitors such as paroxetine, fluoxetine and sertraline. Patients taking metoprolol and other p-blockers (eye drops) or monoamine oxidase (MAO) inhibitors at the same time should be carefully monitored. While taking beta-blockers, inhaled anesthetics enhance the cardiodepressive effect. While taking beta-blockers, patients receiving oral hypoglycemic agents may need to adjust the dose of the latter.

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

How to take, course of use and dosage

Tablets can be taken both with food and on an empty stomach.

Arterial hypertension

100-200 mg of Betalok® once in the morning or in two doses; in the morning and in the evening. If necessary, you can increase the dose or add another antihypertensive agent.

Long-term antihypertensive therapy of 100-200 mg of Betalok per day reduces overall mortality, including sudden death, as well as the incidence of cerebral strokes and coronary circulatory disorders in patients with arterial hypertension.

Angina

pectoris 100-200 mg per day in two doses; morning and evening. If necessary, another antianginal drug may be added to the therapy.

Cardiac arrhythmias

100-200 mg per day in two doses; morning and evening. If necessary, another antiarrhythmic drug may be added to the therapy.

Maintenance therapy after myocardial infarction

The maintenance dose is 200 mg per day in two divided doses; morning and evening. The use of Betaloc at a dose of 200 mg per day can reduce mortality in patients who have had a myocardial infarction, and reduce the risk of developing a second myocardial infarction (including in patients with diabetes mellitus).

Functional disorders of cardiac activity, accompanied by tachycardia

100 mg of the drug Betalok once a day, it is recommended to take the tablet in the morning. If necessary, the dose can be increased.

Prevention of migraine

attacks 100-200 mg per day in two doses; morning and evening.

Hyperthyroidism

150-200 mg per day in 3-4 divided doses.

Impaired renal function

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

Impaired liver function

Usually, due to the low degree of binding to plasma proteins, no dose adjustment of metoprolol is required. However, in severe hepatic impairment (in patients with severe cirrhosis of the liver or portocaval anastomoses), a dose reduction may be required.

Advanced age

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

Children

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

Overdose

Symptoms: the consequences of an overdose of Betalok® may include a marked decrease in blood pressure, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impaired consciousness/coma, nausea, vomiting and cyanosis.

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

Treatment: take activated charcoal, gastric lavage if necessary. If there is a marked decrease in blood pressure, bradycardia, or a threat of heart failure, a beta_-1-adrenomimetic (for example, dobutamine) should be administered intravenously at intervals of 2-5 minutes or infused until a therapeutic effect is achieved. If a selective Pi agonist is unavailable, dopamine or atropine sulfate can be administered intravenously to block the vagus nerve.

If the therapeutic effect is not achieved, other sympathomimetics, such as dobutamine or norepinephrine, can be used.

You can enter glucagon in a dose of 1-10 mg. Sometimes it may be necessary to use a heart rate driver. To stop bronchospasm, a beta_-2-adrenomimetic should be administered intravenously.

It should be borne in mind that the doses of antidotes required to eliminate symptoms that occur with an overdose of beta-blockers are much higher than therapeutic ones, since beta-adrenergic receptors are in a bound state with a beta-blocker.

Special instructions

Patients taking beta-blockers should not be given intravenous “slow” calcium channel blockers such as verapamil. Patients with obstructive pulmonary disease should not be prescribed beta-blockers. If other antihypertensive agents are poorly tolerated or ineffective, metoprolol can be prescribed, since it is a selective drug. It is necessary to prescribe the minimum effective dose, if necessary, it is possible to prescribe a beta_-2-adrenomimetic.

When using beta_-1blockers, 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 chronic heart failure in the decompensation stage, it is necessary to achieve a compensation stage both before and during treatment with the drug.

Patients suffering from Prinzmetal angina should not be prescribed non-selective beta-blockers.

Very rarely, patients with impaired AV conduction may experience deterioration (possible outcome-AV blockade). If bradycardia develops during treatment, the dose of Betaloc should be reduced or the drug should be gradually discontinued.

Metoprolol may worsen the symptoms of peripheral circulatory disorders mainly due to a decrease in blood pressure. Caution should be exercised when prescribing the drug to patients suffering from severe renal insufficiency, with metabolic acidosis, co-use with cardiac glycosides. Patients suffering from pheochromocytoma should be prescribed an alpha-blocker in parallel with Betalok.

In patients with cirrhosis of the liver, the bioavailability of metoprolol increases. In case of surgical intervention, the anesthesiologist should be informed that the patient is taking a beta-blocker.

Abrupt discontinuation of the drug should be avoided. If it is necessary to cancel the drug, the cancellation should be carried out gradually. In most patients, the drug can be discontinued in 14 days. The dose of the drug is reduced gradually, in several doses, until the final dose of 25 mg is reached once a day. Patients with ischaemic heart disease should be closely monitored by a doctor during drug withdrawal. In patients taking beta-blockers, anaphylactic shock occurs in a more severe form.

Influence on the ability to drive motor vehicles and manage mechanisms

When using the drug, episodes of dizziness or general weakness are possible, and therefore it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Pills.

Storage conditions

At a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 5 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

Angina, Migraine, Hypertension, Arrhythmia