Betacor

Betacor is a drug that selectively blocks the activity of β-adrenergic receptors.

Indications Betacore

It is used to reduce high blood pressure. It is also used to prevent attacks of angina pectoris.

Release form

The drug is released in tablets. A blister pack contains 10 tablets of the drug; there are 3 such packs inside the box.

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Pharmacodynamics

Among the medicinal properties that are noted in Betaxolol:

• β-adrenergic blocking effect of cardioselective nature;
• lack of its own sympathomimetic effect (does not have a partial agonistic effect);
• weak membrane-stabilizing effect (similar to quinidine or local anesthetics) when used in concentrations that exceed the sizes of standard medicinal doses.

Pharmacokinetics

Suction.

The drug is completely and rapidly absorbed after oral administration. The effect of the first liver passage is extremely weak, and the bioavailability index of the substance is about 85%, due to which its values in the blood plasma of different people or in one patient with prolonged use of the drug differ insignificantly. The element betaxolol is synthesized with blood protein in the plasma by about 50%.

Exchange processes.

The distribution volume is approximately 6 l/kg. In the body, most of the betaxolol is transformed into inactive decay products, and only 10-15% of this element is determined in the urine in an unchanged state. Elimination occurs mainly through the kidneys.

Excretion.

The half-life of the active element is approximately 15-20 hours.

Dosing and administration

The standard dosage for reducing high blood pressure or preventing the development of angina is 1 tablet (20 mg) per day.

Serving sizes for people with renal impairment.

Along with the weakening of renal activity, the clearance rate of betaxolol also decreases. Therefore, the dose of the drug must be adapted to the renal activity of the patient: at a CC level of 20 ml/minute, there is no need to adjust the dosage.

However, it is necessary to perform a clinical examination, starting from the 1st week of therapy, until the equilibrium level of the drug in the blood is reached (this takes an average of 4 days).

In people with severe renal impairment (CrCl values <20 ml/min), therapy should be initiated with 10 mg/day (dialysis schedule and frequency are not important in people undergoing hemodialysis).

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Use Betacore during pregnancy

Teratogenic effect.

At present, there is no information about the development of teratogenic symptoms in humans or the occurrence of congenital anomalies in the fetus.

Neonatal influence.

If a pregnant woman took Betacor, the effect of the β-blocker will continue to persist in the newborn for several days after birth. Although this residual symptom may not be the cause of clinical complications, the likelihood of heart failure still remains. If such a disorder occurs, it is necessary to send the newborn to intensive care, and in addition to this, to refuse the use of plasma substitutes (because there is a possibility of acute pulmonary edema).

In addition, there are data on cases of hypoglycemia, bradycardia and RDSN. Because of this, it is necessary to carefully monitor the condition of the newborn, while keeping it in specialized conditions (during the first 3-5 days of life, it is necessary to monitor blood glucose levels and heart rate).

Due to all the above factors, betaxolol is prohibited during pregnancy. The only exceptions are those cases when the probable benefit from taking the drug is higher than the risk of complications in the fetus.

Lactation period.

It has been found that β-blockers can be excreted in breast milk. Breastfeeding should be discontinued during therapy with Betacor, because the likelihood of bradycardia or hypoglycemia in newborns has not yet been studied.

Contraindications

Main contraindications:

• severe bronchial asthma, as well as chronic pulmonary pathologies of an obstructive nature;
• cardiogenic shock;
• heart failure not controlled by therapy;
• having 2-3 degree of severity of AV block;
• bradycardia (heart rate is <45-50 beats/minute);
• spontaneous angina (monotherapy cannot be used if the patient has a typical or isolated form of this disease);
• problems with the functioning of the sinus node (this includes sinoatrial block);
• Raynaud's disease, which has a severe degree of expression (or other disorders of peripheral blood flow function);
• pheochromocytoma that is not amenable to treatment;
• decreased blood pressure values;
• intolerance to betaxolol;
• history of anaphylactic symptoms;
• metabolic form of acidosis.

Betacor should not be combined with such drugs as sultopride and floctafenine. It is also prohibited to combine the drug with diltiazem, verapamil, and also amiodarone and bepridil.

Since the drug contains lactose, it is not prescribed to people with congenital galactosemia, hypolactasia or glucose-galactose malabsorption.

Side effects Betacore

Taking the medication may cause the occurrence of certain side effects:

• disorders affecting the subcutaneous layer and epidermis: skin manifestations, including exacerbation of psoriasis or the appearance of psoriasis-like rashes. Itching, urticaria or hyperhidrosis may also occur;
• disorders of the nervous system: headaches or dizziness, lethargy and distal paresthesia;
• problems affecting the function of the visual organs: dry mucous membranes of the eyes, impaired visual acuity;
• mental disorders: the appearance of a feeling of fatigue, the development of insomnia or asthenia. The appearance of nightmares, depression, hallucinations, a feeling of confusion;
• gastrointestinal disorders: disorders in the gastrointestinal tract (such as diarrhea, abdominal pain and vomiting with nausea);
• nutritional and metabolic disorders: development of hyper- or hypoglycemia, as well as bradycardia (possibly to a severe degree). Inhibition of AV conduction or potentiation of existing AV block may be observed, as well as a decrease in blood pressure and heart failure;
• symptoms affecting the vascular system: increased intermittent claudication or Raynaud's disease. Cold extremities may also be observed;
• problems with the function of the respiratory organs and the sternum with the mediastinum: the appearance of dyspnea or bronchial spasms;
• reproductive disorders: development of impotence;
• changes in laboratory data: rarely, the occurrence of antinuclear antibodies is noted, occasionally accompanied by clinical symptoms similar to SLE, which disappear after discontinuation of therapy.

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Overdose

Signs of Betacor poisoning: bradycardia or a very strong decrease in blood pressure. With such symptoms, the patient should be given several drugs:

• intravenous injection of 1-2 mg of atropine;
• administration of 1 mg glucagon (repeat this injection if necessary);
• if necessary, perform an infusion (at a slow rate) of 25 mcg of isoprenaline or administer a dose of dobutamine equal to 2.5-10 mcg/kg/minute.

If a newborn whose mother used beta-blockers during pregnancy develops cardiac decompensation, the following procedures are required:

• administration of 0.3 mg/kg of glucagon;
• referral to intensive care;
• use of dobutamine with isoprenaline: often in fairly large doses and for a long time. Procedures are performed under the supervision of a physician.

Interactions with other drugs

The drug potentiates the effect of other antihypertensive drugs. When combined with antihypertensive drugs that have a central type of therapeutic effect (such as methyldopa and clonidine with moxonidine, etc.), one should avoid abruptly stopping the use of the latter, because this can lead to a significant increase in blood pressure.

When combined with diltiazem, reserpine, SG, amiodarone, and also quinidine, verapamil and methyldopa, the risk of developing disorders of cardiac automatism, contractility, and conduction increases.

Combination with calcium antagonists of the dihydropyridine series (especially in people with latent heart failure) increases the likelihood of a decrease in blood pressure and the development of cardiac decompensation, which is why it is recommended to avoid intravenous injections of antiarrhythmic drugs and calcium antagonists during therapy with Betacor.

Estrogens, antacids, NSAIDs, enveloping drugs and GCS reduce the antihypertensive effect of the drug, while tricyclics, on the contrary, enhance it (orthostatic collapse may develop).

The drug enhances the medicinal properties of non-depolarizing muscle relaxants and, in addition, slows down the liver metabolism of the substance lidocaine.

Phenothiazines with cimetidine increase the levels of the element betaxolol in blood plasma.

With a decrease in blood pressure and the development of anaphylactic symptoms caused by the use of contrast agents containing iodine, medications that block the activity of β-adrenergic receptors reduce the severity of compensatory symptoms from the cardiovascular system.

It is prohibited to combine Betacor with MAOIs, because this leads to a significant increase in the antihypertensive effect.

Allergens or their extracts used for skin testing increase the likelihood of severe systemic symptoms or anaphylaxis in people using Betacor.

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Storage conditions

Betacor must be kept in a place closed to children. Temperature values are no more than 25°C.

Shelf life

Betacor can be used for up to 4 years from the date of manufacture of the therapeutic agent.

Application for children

There is no data on the therapeutic efficacy and safety of the drug in children, which is why it cannot be prescribed to them.

Analogues

The analogs of the drug are Enzix Duo, Atenolol and Captopril with Panavital and Metoprolol, as well as Corvitol with Bisoprolol and Cordaflex with Biprol.

Reviews

Betacor receives mostly positive reviews from patients. After completing the course of medication prescribed by the doctor, many patients note stabilization of blood pressure indicators.