Betalok

Betaloc has antianginal, antiarrhythmic and antihypertensive effects.

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Indications Betaloka

The tablets are used for the following pathologies:

• elevated blood pressure;
• heart rhythm disorders;
• cardiac dysfunction, against the background of which tachycardia is observed;
• angina pectoris.

As a component of combination therapy, it is used after myocardial infarction, as well as in thyrotoxicosis. In addition, it can be used to prevent migraine attacks.

The use of the solution is prescribed:

• in case of tachycardia;
• in case of ischemic myocardial damage;
• for pain that occurs during myocardial infarction or when there is a suspicion of its development.

In addition, the solution can be prescribed to prevent ischemic myocardial damage or tachycardia.

Release form

It is produced in the form of an injection liquid and in tablets, which contain 100 pieces in a bottle.

Pharmacodynamics

The component metoprolol significantly reduces or completely eliminates the effects of catecholamines that occur as a result of strong physical, mental or emotional stress. At the same time, it moderately weakens myocardial contractility and heart rate indicators. The substance also has an antihypertensive effect.

Betaloc can slightly increase TG values and reduce the level of free fatty acids in the blood serum. Sometimes, a slight decrease in high-density lipoproteins is also noted.

The use of the solution in the treatment of myocardial infarction helps to reduce the intensity of pain, and in addition helps to reduce the likelihood of ventricular fibrillation and atrial fibrillation. At the early stage of infarction, it helps to limit the area of damage and prevents the spread of necrosis.

Pharmacokinetics

The solution is distributed within the body at high speed – within just a few minutes. The use of doses not exceeding 20 mg leaves the pharmacokinetic parameters of the drug linear. The half-life is about 3-4 hours on average. The degree of absorption is 95%; the remainder of the drug is excreted unchanged.

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Dosing and administration

Schemes for application of the solution.

The injection fluid may only be administered by a medical professional with the necessary experience and skills, and in the presence of all the required conditions for performing resuscitation procedures, if necessary.

When treating paroxysmal tachycardia, the initial dose is 5 mg (or 5 ml), administered at a rate of 1-2 mg/minute. The drug should be administered at intervals of 5 minutes until the desired effect is achieved (usually this requires approximately 10-15 mg of the substance). It is prohibited to use more than 20 mg of the drug.

To prevent or treat ischemic myocardial damage, as well as in the treatment of myocardial infarction and tachycardia, first administer 5 mg (or 5 ml) of the drug at intervals of 2 minutes until the desired effect is achieved. Exceeding the dose of 15 mg is prohibited. 15 minutes after the end of the final injection, continue the treatment with oral administration of metoprolol (50 mg at intervals of 6 hours for 2 days).

Schemes for using the tablet form of the drug.

The tablets should be taken orally, with food or on an empty stomach. When prescribing tablets, the following dosage portions are usually used:

• elevated blood pressure: take 0.1-0.2 g of the medicine once in the morning (or divide the dose into 2 doses - in the morning and then in the evening). If necessary, the dose can be increased or another antihypertensive drug can be taken additionally;
• problems with heart rhythm: it is necessary to use 0.1-0.2 g of the drug per day, which is taken in 2 doses (in the morning and then in the evening). If necessary, it is allowed to add another antiarrhythmic drug;
• problems with cardiac function due to tachycardia: single dose of 0.1 g per day (recommended in the morning). If necessary, it is allowed to increase the portion;
• thyrotoxicosis: take 0.15-0.2 g per day, in 3-4 doses;
• angina: daily use of 0.1-0.2 g, twice a day (morning and evening). If necessary, sometimes another antianginal substance is added;
• supportive measures for people who have had a myocardial infarction: daily use of 0.2 g of the drug, twice a day, in the morning and then in the evening;
• prevention of migraine development: take 0.1-0.2 g of the drug per day, in 2 doses (in the morning and in the evening).

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Use Betaloka during pregnancy

Use in pregnant women.

The drug should not be prescribed to pregnant women if the doctor evaluates the benefit-risk ratio of the drug in favor of the second factor. Since β-blockers weaken placental blood circulation, this can cause fetal death in the womb, and also cause immaturity of development and premature labor.

Like other β-blockers, the injectable substance Betaloc may have a negative effect on the fetus, infant or newborn (the most likely option is the development of hypoglycemia or bradycardia). There is also a high probability of the newborn developing complications affecting the lungs.

The injection fluid was administered under careful control after the 20th week of pregnancy - when it caused an increase in blood pressure. But in this case, despite the fact that the drug passes through the placenta and is found in the umbilical cord blood, no signs of negative effects on the fetus could be detected.

Use during lactation.

Breastfeeding is prohibited when using the drug. Although the volumes of metoprolol penetrating into breast milk do not lead to a significant β-blocking effect on the infant if the woman uses Betaloc in standard doses.

Contraindications

Main contraindications:

• presence of hypersensitivity to the drug and other β-blockers;
• AV block of 2-3 degree severity;
• sinus bradycardia of clinical significance;
• cardiogenic shock;
• Short's syndrome;
• decreased blood pressure values;
• decompensated heart failure;
• severe disorder of peripheral blood flow processes;
• acute myocardial infarction, against the background of which there is a heart rate of 45 beats/minute or lower, systolic blood pressure of less than 100 mm Hg, and in addition a PQ interval of more than 0.24 seconds;
• severe peripheral vascular disease (if there is a risk of developing gangrene).

However, this medicine should not be used by people who occasionally or regularly use inotropic drugs and β-adrenergic receptor stimulants.

Caution is required when prescribing to individuals with grade 1 AV block, COPD, diabetes mellitus, severe renal failure and spontaneous angina.

In addition, the injectable substance cannot be used to treat supraventricular tachycardia if blood pressure values are less than 110 mm Hg; tablets are prohibited for use in individuals who have been using inotropic drugs for a long time during intermittent treatment (because they affect the activity of β-adrenergic receptors).

Side effects Betaloka

Negative symptoms that appear when using drugs are usually curable and have a mild degree of severity.

The following side effects were identified during testing:

• problems with the function of the cardiovascular system: cold extremities, cardiogenic shock (in people with acute myocardial infarction), fainting, grade 1 AV block and other various cardiac conduction disorders, as well as increased heart rate;
• gastrointestinal disorders: the appearance of diarrhea, abdominal pain, nausea, vomiting or constipation;
• disorders affecting the epidermis: hyperhidrosis and rashes;
• symptoms from metabolic processes: increase in the volume of fat deposits;
• lesions affecting the central nervous system: headaches, impaired attention, increased fatigue, drowsiness. In addition, paresthesia, dizziness, depression, insomnia or nightmares, as well as convulsions;
• problems with breathing: bronchial spasms and development of dyspnea during physical exertion.

Occasionally, increased nervous excitability, arrhythmia, a feeling of depression or anxiety, gangrene, memory impairment, dry mouth, impotence and hallucinations are observed.

In some individuals, problems with liver function, photosensitivity, alopecia, rhinitis, hepatitis, and exacerbation of psoriasis have been reported. In addition, problems such as conjunctivitis, visual disturbances, tinnitus, eye irritation, taste bud dysfunction, thrombocytopenia, and arthralgia have been reported.

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Overdose

Use of a 7.5 g portion of the solution may cause fatal poisoning. Use of 1.4 and 2.5 g portions resulted in moderate to severe poisoning.

Intoxication may cause asystole, grade 1-3 AV block, poor peripheral perfusion, bradycardia, heart failure, significant decrease in blood pressure, and cardiogenic shock. In addition, respiratory problems and apnea may occur. Disorder and loss of consciousness are also noted, as well as severe fatigue. Vomiting, hyperhidrosis, tremor, spasms, hyper- or hypoglycemia, seizures, nausea, temporary myasthenic syndrome, hyperkalemia, and paresthesia may develop.

The first signs of intoxication are observed 20-120 minutes after taking the drug.

To eliminate the disorders, gastric lavage or the use of activated carbon are used. Symptomatic measures are also taken. If necessary, appropriate pulmonary ventilation and intubation, replenishment of the BCC level, monitoring of ECG indicators, administration of atropine and glucose infusion can be performed.

In case of myocardial depression, dopamine or dobutamine are used. Glucagon may also be prescribed in a dose of 50-150 mcg/kg (IV method with administration every 60 seconds until the desired effect occurs). Sometimes adrenaline is also administered.

In case of increased ventricular complex and arrhythmia, a sodium solution is used. A pacemaker can also be used.

Terbutaline is used to prevent the development of bronchial spasm. In case of cardiac arrest, resuscitation procedures are performed.

In case of poisoning with tablets, complications such as vomiting, sinus bradycardia, AV block, nausea, coma, bronchospasm, cardiogenic shock, severe hypotension, cardiac failure or cardiac arrest, cyanosis and impaired consciousness occur.

Symptomatic measures are taken during therapy. Mainly gastric lavage is performed and activated carbon is prescribed.

In case of significant decrease in blood pressure, heart failure and bradycardia, β1-adrenoreceptor stimulants are used (at intervals of 3-5 minutes until the effect is achieved). In addition, atropine sulfate, dopamine, sympatholytics (such as dobutamine with norepinephrine), and glucagon in a dose of 1-10 mg are used. A pacemaker may be used.

To eliminate bronchial spasm, the patient is administered β2-adrenergic receptor stimulants intravenously.

Interactions with other drugs

When combining the drug with MAOIs, ganglionic blockers, and also agents that block the activity of β-receptors, it is necessary to carefully monitor the patient's condition.

If clonidine is used together with Betaloc during treatment, the former should be discontinued several days earlier than the latter.

In addition, the medication is prohibited to be combined with verapamil and other antiarrhythmic drugs, as well as with barbiturates, calcium antagonists and propafenone.

Inhalation anesthetics, when combined with Betaloc, increase the severity of the cardiodepressant effect.

Medicines that slow or induce metabolism affect the plasma parameters of the drug. Its antihypertensive effect is weakened when combined with drugs that slow down the binding of PG.

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Storage conditions

Betaloc must be kept in a dark place at temperatures not exceeding 25°C.

Shelf life

Betaloc is allowed to be used within 5 years from the date of manufacture of the therapeutic drug.

Application for children

There is no data on the possibility of safe and effective use of the drug in children.

Analogues

Analogues of the drug are Azoprol Retard, Betaloc ZOK, Metocor with Vasocardin, and in addition Metoprolol, Egilok Retard, Metoprolol Tartrate with Corvitol and Metoprolol Zentiva.

Reviews

Betaloc usually receives positive reviews - patients note quite high efficiency and good tolerability. But it should also be borne in mind that some people experienced negative symptoms such as irritability and weakness, as well as a general deterioration in health.