Betaloc, tablets 100 mg 100 pcs

Metoprolol is a β₁-adrenoblocker that blocks β₁-receptors at doses significantly lower than those required to block β2-receptors. Metoprolol has little membrane-stabilizing effect and no partial agonist activity. Metoprololol reduces or inhibits the agonist effect that catecholamines released during nervous and physical stress have on cardiac activity. This means that metoprolol has the ability to inhibit the increase in HR, minute volume, and increased cardiac contractility and BP caused by the sudden release of catecholamines.

Patients with symptoms of obstructive pulmonary disease may be prescribed metoprolol in combination with β₂-adrenomimetics if necessary. When used together with β₂-adrenomimetics, Betaloc® in therapeutic doses has less effect on the bronchodilation induced by β₂-adrenomimetics than nonselective β-adrenoblockers. Metoprolol affects insulin production and carbohydrate metabolism to a lesser extent than non-selective β-adrenoblockers. The effect of Betaloc® on cardiovascular response in hypoglycemia is significantly less than that of non-selective p-adrenoblockers.

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

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

Indications

Active ingredient

Composition

1 tablet contains:

Active ingredient:

metoprolol tartrate 100 mg.

Associates:

Lactose monohydrate,

Magnesium stearate,

Microcrystalline cellulose,
.

sodium carboxymethyl starch,

silicon dioxide colloidal anhydrous,

povidone.

How to take, the dosage

The tablets may be taken with food or on an empty stomach.

Arterial hypertension

100-200 mg of Betaloc® once in the morning or in two doses; in the morning and in the evening. If necessary, the dose may be increased or another antihypertensive may be added.

Long-term antihypertensive therapy with 100-200 mg of Betaloc® per day may decrease overall mortality, including sudden death, and the incidence of brain stroke and coronary artery disease in patients with arterial hypertension.

Estension

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

Heart rhythm disorders

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

Supportive therapy after myocardial infarction

The maintenance dose is 200 mg daily in two doses; morning and evening. Administration of Betaloc at a dose of 200 mg daily may decrease mortality in patients who have had a myocardial infarction and decrease the risk of recurrent myocardial infarction (including in patients with diabetes).

Functional cardiac disorders with tachycardia

100 mg of Betaloc once daily, tablet taken in the morning is recommended. The dose can be increased if necessary.

Prevention of migraine attacks

100-200 mg daily in two doses; in the morning and in the evening.

Hyperthyroidism

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

Renal dysfunction

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

Hepatic impairment

In general, 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 or portocaval anastomosis), dose reduction may be required.

Elderly age

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

Children

The experience with Betaloc® in children is limited.

Interaction

Co-prescription of Betaloc® with the following drugs should be avoided:

Barbituric acid derivatives: barbiturates (the study was conducted with phenofarbital) slightly enhance metabolism of metoprolol, due to enzyme induction.

Propafenone: When propafenone was administered to four patients treated with metoprolol, a 2-5-fold increase in plasma concentrations of metoprolol was observed, with two patients experiencing side effects characteristic of metoprolol. This interaction was confirmed in a study on 8 volunteers. The interaction is probably due to the inhibition of metoprolol metabolism by the cytochrome P4502D6 system with propafenone, similar to quinidine. Given that propafenone has the properties of a β-adrenoblocker, the combined administration of metoprolol and propafenone is not advisable.

Verapamil: A combination of β-adrenoblockers (atenololol, propranolol, and pindolol) and verapamil may cause bradycardia and lead to a decrease in BP. Verapamil and β-adrenoblockers have a complementary inhibitory effect on atrio-ventricular conduction and sinus node function.

The combination of Betaloc® with the following drugs may require dose adjustments:

Class I antiarrhythmic agents: Class I antiarrhythmic agents and β-adrenoblockers may result in a summation of negative inotropic effects that may lead to serious hemodynamic side effects in patients with impaired left ventricular function. Such combination should also be avoided in patients with sinus node weakness syndrome and AV conduction abnormality. Interactions are described using disopyramide as an example.

Amiodarone: Concomitant use of amiodarone and metoprolol may result in marked sinus bradycardia. Given the extremely long half-life of amiodarone (50 days), the possible interaction long after amiodarone withdrawal should be considered.

Diltiazem: Diltiazem and β-adrenoblockers mutually enhance the inhibitory effect on AV conduction and sinus node function. When combining metoprolol with diltiazem, there have been cases of marked bradycardia.

Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect of β-adrenoblockers. This interaction is most documented for indomethacin. No described interaction has been noted for sulindac. In studies with diclofenac, no described reaction has been noted.

Diphenhydramine: Diphenhydramine decreases the clearance of metoprolol to α-hydroxymetoprolol by 2.5 times. At the same time there is an increase in the action of metoprolol.

Epinephrine (adrenaline): 10 cases of severe arterial hypertension and bradycardia have been reported in patients taking non-selective β-adrenoblockers (including pindolol and propranolol) and receiving epinephrine (adrenaline). Interaction was also observed in the group of healthy volunteers. It is assumed that similar reactions may also be observed when epinephrine is used together with local anesthetics in case of accidental ingestion into the vascular bed. This risk is thought to be much lower with cardioselective β-adrenoblockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) at a single dose of 50 mg may cause elevation of diastolic BP to abnormal values in healthy volunteers. Propranolol generally interferes with the BP elevation induced by phenylpropanolamine. However, β-adrenoblockers may cause paradoxical arterial hypertension reactions in patients receiving high doses of phenylpropanolamine. Several cases of hypertensive crisis have been reported with phenylpropanolamine.

Hinidine: Quinidine inhibits metabolism of metoprolol 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 an increase in β-blockade. This interaction is believed to be characteristic of other p-adrenoblockers whose metabolism involves cytochrome P4502D6.

Clonidine: Hypertensive reactions when clonidine is abruptly withdrawn may worsen if β-adrenoblockers are coadministered. When used together, if clonidine is withdrawn, discontinuation of β-adrenoblockers should be started several days before clonidine withdrawal.

Rifampicin: Rifampicin may increase metabolism of metoprolol, decreasing the plasma concentration of metoprolol.

Plasma concentrations of metoprololol may increase when combined with cimetidine, hydralazine, and selective serotonin inhibitors such as paroxetine, fluoxetine and sertraline. Patients taking metoprolol and other p-adrenoblockers (eye drops) or monoamine oxidase inhibitors (MAOIs) simultaneously should be closely monitored. Against the background of β-adrenoblockers, inhaled anesthetics increase the cardiodepressant effect. Patients receiving oral hypoglycemic agents may require adjustment of the dose of the latter while taking β-adrenoblockers.

The cardiac glycosides in concomitant use with β-adrenoblockers may increase atrioventricular conduction time and cause bradycardia.

Special Instructions

Patients taking β-adrenoblockers should not receive intravenous calcium channel blockers such as verapamil. Patients with obstructive pulmonary disease should not be prescribed β-adrenoblockers. If other antihypertensive agents are poorly tolerated or ineffective, metoprolol may be prescribed, since it is a selective drug. The lowest effective dose should be prescribed; if necessary, a β2-adrenomimetic may be prescribed.

When using β1-adrenoblockers, the risk of their effect on carbohydrate metabolism or possibility of masking hypoglycemic symptoms is significantly less than when using non-selective β-adrenoblockers.

In patients with decompensated chronic heart failure, a stage of compensation should be achieved both before and during treatment with the drug.

Patients with Prinzmetal angina are not recommended to be treated with nonselective β-adrenoblockers.

Very rarely, patients with impaired AV conduction may worsen (possible outcome is AV blockade). If bradycardia develops with treatment, the dose of Betaloc should be reduced or the drug should be gradually withdrawn.

Methoprolol may worsen symptoms of peripheral circulatory disorders mainly due to decreased blood pressure. Caution should be exercised when prescribing the drug in patients with severe renal insufficiency, in metabolic acidosis, co-administration with cardiac glycosides. In patients with pheochromocytoma, an alpha-adrenoblocker should be prescribed concomitantly with Betaloc.

In patients with cirrhosis, the bioavailability of metoprolol increases. In case of surgery, the anesthesiologist should be informed that the patient is taking a β-adrenoblocker.

Abrupt withdrawal of the drug should be avoided. If withdrawal is necessary, it should be done gradually. In most patients the drug can be withdrawn within 14 days. The dose of the drug is reduced gradually, in several doses, until a final dose of 25 mg once daily is reached. Patients with coronary heart disease should be under close medical supervision during drug withdrawal. In patients taking β-adrenoblockers anaphylactic shock is more severe.

Impact on driving and operating machinery

When using the drug, episodes of dizziness or general weakness may occur, therefore, it is necessary to refrain from driving and engaging in potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Side effects

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

The following undesirable side effects have been described in clinical trials or in the use of Betaloc (metoprolol tartrate) in clinical practice. In many cases, a causal relationship to treatment with Betaloc has not been established.

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

Cardiovascular system: frequent – bradycardia, postural disturbances (very rarely accompanied by syncope), limb cooling, palpitations; infrequent – temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction; Grade I AV blockade; rare – other cardiac conduction disorders, arrhythmias; very rare – gangrene in patients with previous severe peripheral circulatory disturbances.

CNS: very common – fatigue; common – dizziness, headache; rare – increased nervous excitability, anxiety, impotence/sexual dysfunction; infrequent – paresthesias, seizures, depression, impaired attention, drowsiness or insomnia, nightmares; very rare – amnesia/memory disturbances, depression, hallucinations.

Gastrointestinal tract: frequently – nausea, abdominal pain, diarrhea, constipation; infrequently – vomiting; rarely – dry mouth.

Liver: rarely – liver function disorders.

The skin: infrequent – rash (as urticaria), increased sweating, rarely – hair loss, very rare – photosensitization, exacerbation of psoriasis.

Respiratory organs: often – shortness of breath with physical effort; infrequent – bronchospasm in patients with bronchial asthma; rarely – rhinitis.

Sensory organs: rare – visual disturbances, dry and/or irritated eyes, conjunctivitis; very rare – ringing in the ears, impaired sense of taste.

Metabolism: infrequent – increase in body weight.

Skeletal and muscular system: very rare – arthralgia.

Blood: very rarely – thrombocytopenia.

Overdose

Symptoms: Symptoms of Betaloc® overdose may include marked BP decrease, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impaired consciousness/coma, nausea, vomiting and cyanosis.

The concomitant use of alcohol, taking antihypertensives, quinidine, or barbiturates may worsen the patient’s condition. The first signs of overdose may appear within 20 minutes to 2 hours after taking the drug.

Treatment: take activated charcoal, if necessary, gastric lavage. In case of marked BP decrease, bradycardia or threat of heart failure, β1-adrenomimetic (e.g. dobutamine) should be administered intravenously at 2-5 minute intervals or by infusion until therapeutic effect is achieved. If no selective Pi-agonist is available, intravenous dopamine or atropine sulfate may be given to block the vagus nerve.

If therapeutic effect is not achieved, other sympathomimetics such as dobutamine or noradrenaline may be used.

Glucagon may be administered in a dose of 1-10 mg. Occasionally it may be necessary to use a pacemaker. An intravenous β2-adrenomimetic should be given to relieve bronchospasm.

It should be borne in mind that the doses of antidotes required to relieve symptoms arising from β-adrenoblocker overdose are much higher than the therapeutic doses because the β-adrenoreceptors are in a bound state with the β-adrenoblocker.

Pregnancy use

Like most drugs, Betaloc® should not be administered during pregnancy and while breastfeeding unless the expected benefit to the mother outweighs the potential risk to the fetus and/or baby. As other antihypertensive agents, β-adrenoblockers may cause side effects such as bradycardia in the fetus, newborns or breastfed children.

The amount of metoprolol excreted into breast milk and the β-blocking effects in the breastfed baby (when the mother takes metoprolol at therapeutic doses) are minor.

Similarities