Index of drugs

Treatment of hypertension in adult patients. Prophylactic treatment of exercise-induced angina pectoris stable in adult patients.

1 tabl contains 20 mg of betaxolol hydrochloride.

Long-acting, cardioselective β₁-adrenolityk. Sympathomimetic does not work. The receptor blocking effect occurs within 24 h after administration of 20 mg betaxolol. After administration of therapeutic doses of betaxolol, a significant reduction in blood pressure, heart rate and stroke volume was observed. It exhibits poor stabilization of cell membranes without intrinsic sympathomimetic activity. It does not reduce the excretion of sodium through the kidneys. It reduces plasma renin activity. After oral administration it is completely and quickly absorbed. Bioavailability is about 85%. It is 50% bound to plasma proteins. 85-90% of the administered dose is metabolised in the liver. Only one metabolite (2-3% of the administered dose), resulting from aliphatic hydroxylation, has beta-adrenergic blocking activity. The metabolite has selective properties, its potency is 50% of the potency of betaxolol. 10 to 15% of the administered dose is excreted unchanged by the kidneys. Metabolites are mainly excreted by the kidneys. T_0,5 is 16-20 h.

Hypersensitivity to betaxolol hydrochloride or any of the excipients. Severe forms of bronchial asthma or chronic obstructive pulmonary disease. Uncompensated heart failure. Cardiogenic shock. Atrio-ventricular block IIst. and III. (with the exception of people with an implanted pacemaker). Prinzmetal angina (in pure form and as a monotherapy). The syndrome of a sick sinus-atrial node, including the sinoatrial block. Severe bradycardia (<45-50 beats per minute). Severe forms of Raynaud's disease and peripheral artery disorders. Untreated phaeochromocytoma. Hypotension. Anaphylactic reactions in an interview. Metabolic acidosis. Simultaneous use with floctafenine or with sultopride. Concomitant use with MAO inhibitors (except MAO-B inhibitors). Intravenous administration of Calcium channel blockers such as Verapamil or diltiazem and other antiarrhythmics (such as disopyramide or amiodarone) in patients being treated with betaxolol is contraindicated; the exception is treatment in an intensive care unit, where careful and constant monitoring of the patient is guaranteed.

The use of betaxolol should not be discontinued, particularly in patients with angina pectoris, as this may result in severe arrhythmia, myocardial infarction or sudden death. The dose should be gradually reduced, i.e. for 1 to 2 weeks; if necessary, treatment with another medicine should be started at the same time as decreasing the dose of betaxolol to avoid aggravation of angina. It is necessary to reduce the dose of betaxolol if the heart rate at rest is <50-55 beats per minute and if symptoms of bradycardia occur. Betaxolol should be used with caution in patients with bronchial asthma or COPD (betaxolol can only be used for mild forms of these diseases, treatment should be started at the lowest doses, pulmonary function tests are recommended prior to initiation of therapy, if an asthma attack occurs during treatment, drugs stimulating β receptors₂bronchodilator); with heart failure (betaxolol used under constant medical observation, start treatment with very small doses gradually increasing it); with atrio-ventricular block Ist. (due to the negative dromotropic effect of β-blockers); with Prinzmetal angina (risk of increased number and duration of angina attacks; betaxolol can only be used for milder disease and in a mixed form of angina, provided that vasodilator is used simultaneously); with peripheral arterial disease, e.g.Raynaud's syndrome or disease, inflammation of the arteries or chronic lower limb ischemia (symptoms may worsen); with pheochromocytoma (in the treatment of secondary hypertension caused by treatment of phaeochromocytoma of the adrenal gland, blood pressure should be closely monitored); with diabetes (regular glycemic control, because betaxolol may mask the symptoms of hypoglycaemia, such as tachycardia, palpitations or sweating); in the elderly (treatment under medical supervision and start with the lowest effective dose); with renal failure (modify the dosage depending on the creatinine clearance value); with hepatic insufficiency (careful clinical monitoring is indicated at the beginning of treatment); with glaucoma (patients to be treated with general beta blocker and eye drops should be monitored because of the possibility of adding treatment effects). Β-adrenergic block reduces intraocular pressure and may affect the wrong result of the glaucoma detection test; an ophthalmologist should be informed that the patient is being treated with betaxolol. The benefits of β-blockers should be carefully weighed in patients with a family history of psoriasis or psoriasis (risk of worsening of symptoms). Treatment with betaxolol may mask the cardiovascular symptoms of hyperthyroidism. In patients prone to severe anaphylactic reactions, irrespective of the underlying cause, particularly those caused by contrast agents containing Iodine or floctafenines and patients undergoing desensitisation therapy, betaxolol may lead to exacerbation of the sensitization and adrenaline-resistant reactions administered at the usual doses. Susceptibility to hypoglycaemia is increased, e.g. during prolonged fasting or severe physical exertion. Blockade of β receptors in the perioperative period reduces the incidence of arrhythmias and myocardial ischemia during induction and intubation, as well as in the postoperative period; the anesthesiologist should be informed about the β-blocker, because potential interactions with other drugs can cause bradyarrhythmia, weakness of reflex tachycardia and reduction of reflex ability to compensate for blood loss. If it is necessary to discontinue treatment, then 48 h is a sufficient period of time to regain sensitivity to catecholamines. In some cases, the β-blocker should not be discontinued: in patients with ischemic heart disease (continuation of treatment is recommended until surgery); in an emergency and if interruption of treatment is impossible, patients should be protected from excessive parasympathetic reactions by means of appropriate premedication with atropine; if necessary, atropine may be repeated. The use of betaxolol in children and adolescents is not recommended (no data on safety and efficacy).

The use of a drug in pregnancy is not recommended, unless the therapeutic benefits for the mother outweigh the possible risks to the fetus or newborn. Β-blockers reduce the flow through the placenta, which may cause intrauterine fetal death, premature and premature labor; the fetus may have side effects (especially hypoglycaemia and bradycardia). In newborns of mothers treated with beta-blockers, the effects of these drugs are maintained for several days after giving birth. There is an increased risk of cardiac and pulmonary complications in newborns during the post-natal period. If heart failure occurs, the newborn should be transferred to the ICU. Avoid administration of plasma volume enhancers (risk of acute pulmonary edema). There have also been reports of bradycardia, impaired breathing and hypoglycaemia in the newborn. Close supervision of the newborn in a specialized center (monitoring of heart rate and blood glucose) is recommended for the first 3 to 5 days after delivery. Betaxolol passes into breast milk. The risk of hypoglycaemia and bradycardia has not been evaluated, therefore breast-feeding is not recommended during treatment with betaxolol.

Common: allergic skin reactions (redness, itching, rash), baldness, fatigue, headache, dizziness, excessive sweating, weakness, insomnia, stomach pain, diarrhea, nausea and vomiting, bradycardia (including severe bradycardia), coldness of the limbs, impotence .Uncommon: symptoms similar to myasthenia gravis, muscle weakness, decreased tear production. Rare: psoriasis, exacerbation of existing psoriasis or occurrence of a psoriasis-like rash, depression, heart failure, lower blood pressure, slow conduction or worsening of the existing atrio-ventricular block, Raynaud's syndrome, exacerbation of existing claudication, bronchospasm. Very rarely: exacerbation of existing myasthenia gravis, peripheral paresthesia, visual impairment, hallucinations, confusion, nightmares, hypoglycaemia, hyperglycemia, revealing clinically occult diabetes, worsening of existing diabetes. In patients with hyperthyroidism, clinical signs of thyrotoxicosis may be masked. Hypoglycaemia may occur during long-term fasting or severe physical activity. The warning signs of hypoglycaemia (especially tachycardia and tremor) may be reduced. In rare cases, the appearance of antinuclear antibodies was observed, which in exceptional cases were accompanied by clinical symptoms, such as systemic lupus erythematosus, which subsided after the end of treatment. In addition, there may be a reduction in HDL-cholesterol and increased triglycerides.

Orally. Adults.Hypertension: for the treatment of mild hypertension, the starting dose is 10 mg once a day, if the effect is insufficient, the dose may be increased to 20 mg per day; in the treatment of severe hypertension, the usual dose is 20 mg once a day.Strenuous angina pectoris stable: individually, the starting dose is 10 mg per day, the dose can be increased to the usual 20 mg once a day, in some cases it may be necessary to increase the daily dose to 40 mg.Special groups of patients. Renal failure: CCr> 20 ml / min, no dose adjustment is required, however, clinical monitoring is recommended at the beginning of treatment until steady-state plasma concentrations of betaxolol are obtained (on average 4 days); CCr <20 ml / min and in patients undergoing hemodialysis or peritoneal dialysis the maximum daily dose is 10 mg. Hepatic insufficiency: no dosage adjustment is required, careful monitoring is recommended at the beginning of treatment. Elderly patients: treatment should be started with caution at low doses and the clinical condition of the patient should be closely monitored. The tablets are taken at the same time each day, preferably in the morning.