Instructions Betac film-coated tablets 20 mg blister No. 30
Composition
active ingredient: betaxolol;
1 tablet contains betaxolol hydrochloride 10 mg or 20 mg;
Excipients: microcrystalline cellulose, lactose monohydrate, sodium starch glycolate, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, titanium dioxide (E 171), purified talc, lecithin, xanthan gum.
Dosage form
Film-coated tablets.
Main physicochemical properties:
10 mg tablets - round biconvex tablets of white or almost white color, film-coated, with a core diameter of approximately 7.0 mm;
20 mg tablets - round biconvex tablets of white or almost white color with a dividing groove with a diameter of approximately 9.5 mm, film-coated.
Pharmacotherapeutic group
Selective beta-adrenergic blockers.
ATX code C07A B05.
Pharmacological properties
Pharmacodynamics
Betaxolol is characterized by three pharmacological properties:
- cardioselective beta-adrenergic blocking action;
- lack of partial agonist activity (i.e. does not exhibit its own sympathomimetic activity);
- weak membrane-stabilizing effect (similar to quinidine or local anesthetics) in concentrations exceeding recommended therapeutic doses.
Pharmacokinetics
Absorption. The drug is rapidly and completely absorbed after oral administration with a very small effect of the "first pass" through the liver and a very high bioavailability of approximately 85%, which ensures low differences in its concentration in the blood plasma in different patients or in the same patient during prolonged use.
Betaxolol is approximately 50% bound to plasma proteins.
Metabolism. The volume of distribution is approximately 6 l/kg. In the body, betaxolol is mainly converted to inactive metabolites, and only 10-15% of betaxolol is found in the urine unchanged. The main route of elimination is through the kidneys.
Elimination: The half-life of betaxolol from the body is 15-20 hours.
Indication
Arterial hypertension.
Prevention of angina attacks.
Contraindication
Severe forms of bronchial asthma and chronic obstructive pulmonary diseases.
Heart failure that is not controlled by treatment.
Cardiogenic shock.
Atrioventricular block of the second and third degree in patients without a pacemaker.
Prinzmetal's angina (monotherapy with the drug is contraindicated in isolated/typical form of this disease).
Sinus node dysfunction (including sinoatrial block).
Bradycardia (heart rate <45-50 beats/min).
Severe forms of Raynaud's syndrome and other peripheral circulatory disorders.
Untreated pheochromocytoma.
Arterial hypotension.
Hypersensitivity to betaxolol.
History of anaphylactic reactions.
Metabolic acidosis.
The drug is contraindicated for use in combination with floctafenine and sultopride (see section "Interaction with other medicinal products and other types of interactions").
The use of the drug is not recommended in combination with amiodarone, bepridil, diltiazem and verapamil (see section "Interaction with other medicinal products and other types of interactions").
Due to the presence of lactose, this medicinal product is contraindicated in patients with congenital galactosemia, glucose/galactose malabsorption or lactase deficiency syndrome.
Interaction with other medicinal products and other types of interactions
Bradycardia can be caused by a number of drugs: beta-blockers, antiarrhythmic drugs of class Ia (quinidine, disopyramide), class III (amiodarone and sotalol), class IY (diltiazem and verapamil), as well as digitalis glycosides, clonidine, guaifenesin, mefloquine, and cholinesterase inhibitors used to treat Alzheimer's disease.
The simultaneous use of Betac with the following drugs is contraindicated.
Floctafenine: In case of shock or hypotension caused by floctafenine, beta-blockers cause a decrease in compensatory cardiovascular reactions.
Sultopride. Violation of cardiac automaticity (excessive bradycardia) caused by the additive effect of reducing the rate of contractions.
It is not recommended to use Betac with the following drugs.
Calcium channel blockers (bepridil, diltiazem and verapamil). Violations of automaticity (excessive bradycardia, sinus node arrest), sinoatrial and atrioventricular conduction, heart failure (synergistic effect). Such combinations can be used only with careful clinical control and electrocardiographic monitoring, especially for elderly patients or at the beginning of treatment.
Amiodarone. Violations of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms).
Halogen-containing inhalation anesthetics. Beta-blockers cause a decrease in cardiovascular compensatory reactions (during surgery, beta-adrenergic receptor inhibition can be reversed with beta-stimulants). As a rule, beta-blocker therapy should not be discontinued, and abrupt withdrawal of the drug should be avoided in any case. The anesthesiologist should be informed of the treatment being administered.
Drugs that can provoke paroxysmal ventricular tachycardia of the torsades de pointes type (except sultopride). Class Ia (quinidine, hydroquinidine and disopyramide) and class III (amiodarone, dofetilide, ibutilide, sotatol) antiarrhythmic drugs; some phenothiazine neuroleptics (chlorpromazine, cyamemazine, levomepromazine, thioridazine), benzamides (amisulpride, sulpiride, tiapride), butyrophenones (droperidol, haloperidol), other neuroleptics (pimozide) and other drugs (cisapride, diphemanil, intravenous erythromycin, halofantrine, mizolastine, moxifloxacin, pentamidine, intravenous spiramycin and vincamine). Increased risk of ventricular arrhythmias and especially paroxysmal tachycardia of the torsades de pointes type (hypokalemia is a precipitating factor). Clinical and electrocardiographic monitoring is required.
Propafenone. Impaired contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms). Clinical and electrocardiographic monitoring is necessary.
Baclofen. Increased antihypertensive effect. Blood pressure monitoring and dose adjustment of the antihypertensive agent are required.
Insulin and antidiabetic sulfonamides. All beta-blockers may mask some of the symptoms of hypoglycemia, such as tachycardia, palpitations (see section "Special warnings and precautions for use"). The patient should be warned about the need to increase self-monitoring of blood sugar levels.
Cholinesterase inhibitors (ambenomium, donepezil, galantamine, neostigmine, pyridostigmine, rivastigmine, tacrine). Risk of increased bradycardia (additive effect). Regular clinical monitoring is required.
Centrally acting antihypertensives (clonidine, apraclonidine, alpha-methyldopa, guanfancine, moxonidine, rilmenidine). Significant increase in blood pressure with abrupt withdrawal of a centrally acting antihypertensive. Abrupt withdrawal of the antihypertensive should be avoided and clinical monitoring should be performed.
Lidocaine (intravenously). Increased plasma lidocaine concentrations with possible increased adverse neurological and cardiac effects (reduced hepatic metabolism of lidocaine). Clinical and electrocardiographic monitoring and possibly determination of plasma lidocaine concentrations are recommended both during and after treatment with beta-blockers. If necessary, lidocaine dose adjustment.
Combinations that require special attention.
Nonsteroidal anti-inflammatory drugs (systemic), including selective inhibitors
COX-2. Reduction of the hypotensive effect (suppression of vasodilating prostaglandins by nonsteroidal anti-inflammatory drugs and fluid and sodium retention by pyrazolone derivatives).
Calcium channel blockers (dihydropyridines). Arterial hypotension, circulatory failure in patients with latent or uncontrolled heart failure. Treatment with beta-blockers can minimize reflex sympathetic mechanisms that are triggered by excessive hemodynamic reactions.
Antidepressants related to imipramine, neuroleptics. Increased hypotensive effect and risk of orthostatic hypotension (additive effect).
Mefloquine: Risk of bradycardia (additive effect on the development of bradycardia).
Dipyridamole (intravenously). Enhancement of the antihypertensive effect.
Alpha-blockers used in urology (alfuzosin, doxazosin, prazosin, tamsulosin, terazosin). Increased antihypertensive effect. Increased risk of orthostatic hypotension.
Amifostine. Enhancement of the antihypertensive effect.
Cardiac glycosides. A combination that may prolong atrioventricular conduction time and cause bradycardia.
Fingolimod. Concomitant use of fingolimod with beta-blockers may potentiate the bradycardic effect and is therefore not recommended. If concomitant use is necessary, appropriate monitoring is required from the start of treatment, at least overnight monitoring is recommended.
Iodinated contrast media. In the event of shock or hypotension following the administration of aqueous contrast media, beta-blockers reduce cardiovascular compensatory responses.
Whenever possible, beta-blocker treatment should be discontinued prior to radiographic examination. If use is necessary, the physician should have access to intensive care.
Corticosteroids and tetracosactide: Decreased antihypertensive effect (water and sodium retention in combination with corticosteroids).
Application features
Treatment with the drug should never be abruptly discontinued in patients with angina: abrupt discontinuation of the drug may lead to serious heart rhythm disturbances, myocardial infarction, or sudden death.
Precautions for use. Drug withdrawal. Treatment with the drug should not be stopped abruptly, especially for patients with ischemic heart disease. The dose should be reduced gradually, over 1-2 weeks, and if necessary, replacement therapy can be started at the same time to avoid progression of angina.
Bronchial asthma and chronic obstructive pulmonary disease. Beta-blockers should only be prescribed to patients with moderate disease severity, with the choice of a selective beta-blocker at a low initial dose. It is recommended to assess respiratory function before starting treatment.
If attacks develop during treatment, bronchodilators can be used.
(beta2-adrenomimetics).
Heart failure. For the treatment of patients with non-refractory heart failure, Betac can be used, if necessary, under close medical supervision in low doses, which are gradually increased.
Bradycardia. The dose should be reduced if the resting heart rate is below 50-55 beats per minute and the patient has clinical manifestations of bradycardia.
First-degree atrioventricular block. Given the negative dromotropic effect of beta-blockers, Betax should be administered with caution to patients with atrioventricular block.
First degree.
Prinzmetal's angina. The number and duration of angina attacks may increase with the use of beta-blockers in patients with Prinzmetal's angina. The drug can be used in patients with moderate severity of the disease and provided that the treatment is carried out simultaneously with the use of vasodilators.
Peripheral circulatory disorders: Beta-blockers may worsen the condition of patients with peripheral circulatory disorders (Raynaud's disease or syndrome, arteritis or chronic obliterating diseases of the arteries of the lower extremities). In such cases, a cardioselective beta-blocker with partial beta-agonist properties is recommended; it should be prescribed with caution.
Pheochromocytoma: When beta-blockers are used to treat hypertension caused by pheochromocytoma, careful monitoring of blood pressure is required.
Elderly patients
. In elderly patients, strict compliance with contraindications is mandatory. Caution should be exercised: treatment of elderly patients should be initiated with a low dose and under close supervision (see section "Method of administration and dosage").
Patients with renal failure
For patients with renal insufficiency, the dosage should be adjusted depending on the concentration of creatinine in the blood or creatinine clearance (see section "Method of administration and dosage").
Patients with diabetes
The patient should be advised to increase self-monitoring of blood glucose levels at the beginning of treatment. Prodromal symptoms of hypoglycemia may be masked, especially tachycardia, palpitations and increased sweating (see sections "Interaction with other drugs" and "Adverse reactions").
Psoriasis.
The prescription of the drug requires a careful assessment of the need for its use, as there have been reports of worsening of the condition of patients with psoriasis during treatment with beta-blockers (see section "Adverse reactions").
Allergic reactions: In patients prone to severe anaphylactic reactions, especially those associated with the use of floctafenine (see section "Interaction with other drugs"), or during desensitization, beta-blocker therapy may lead to a further increase in the reaction and reduce the effectiveness of treating this condition with usual doses of adrenaline.
General anesthesia. Beta-blockers cause attenuation of reflex tachycardia and increase the risk of arterial hypotension. Continued treatment with beta-blockers reduces the risk of arrhythmia, myocardial ischemia and hypertensive crises. The anesthesiologist should be informed that the patient is being treated with a beta-blocker.
If it is necessary to discontinue treatment and discontinue the drug, 48 hours is considered sufficient to restore sensitivity to catecholamines.
Beta-blocker therapy should not be discontinued:
- in patients with coronary insufficiency, in whom it is desirable to take the drug before surgery, taking into account the risk associated with the sudden withdrawal of beta-blockers;
- in case of urgent operations or in cases where discontinuation of treatment is impossible. The patient should be protected from the effects of vagal excitation by prescribing premedication with atropine, with repetition if necessary. For anesthesia, it is necessary to use agents that suppress the myocardium to the least extent, and blood loss should be compensated.
The risk of anaphylactic reactions must be taken into account.
Ophthalmology: Beta-blockade reduces intraocular pressure and may alter the results of glaucoma screening tests. The ophthalmologist should be informed that the patient is taking betaxolol. Patients receiving
Beta-blockers, both systemically and in the form of eye drops, should be monitored, taking into account the possible additive effect of these drugs.
Athletes. Athletes should be aware that the product contains an active substance that may give a positive reaction in anti-doping control tests.
The drug contains lactose, therefore it is contraindicated for use in patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
Use during pregnancy or breastfeeding
Pregnancy.
Teratogenicity: To date, there have been no reports of teratogenic effects in humans.
Neonatal aspect.
The effect of beta-blockers persists for several days after birth in newborns whose mothers have been treated with this drug. Although this residual effect may not have clinical consequences, the possibility of developing heart failure remains. In such cases, the newborn should be placed in the intensive care unit (see section "Overdose"), and the use of plasma substitutes should be avoided (due to the risk of developing acute pulmonary edema). There are also reports of cases of bradycardia, respiratory distress syndrome and hypoglycemia. In this regard, careful monitoring of the newborn in specialized conditions is recommended (monitoring of heart rate and blood glucose levels during the first 3-5 days of life).
In this regard, the use of betaxolol during pregnancy is not recommended, except in cases where the benefits of using the drug outweigh the possible risks.
Breast-feeding.
Beta-blockers are excreted in breast milk. Breastfeeding should be discontinued during treatment with Betac, as the risk of hypoglycemia or bradycardia in newborns has not been studied.
Ability to influence reaction speed when driving vehicles or other mechanisms
Studies on the effect of betaxolol on the ability to drive have not been conducted. When driving or operating other mechanisms, it should be taken into account that dizziness, visual impairment and other adverse reactions may sometimes occur while taking this drug, which may adversely affect the speed of reactions when driving or operating other mechanisms.
Method of administration and doses
The usual dose for arterial hypertension and for the prevention of angina attacks is 1 tablet of 20 mg per day.
Dosage for patients with renal insufficiency. In patients with renal insufficiency, the clearance of betaxolol decreases with decreasing renal function.
The dose should be adapted to the patient's renal function: no dose adjustment is required for creatinine clearance ≥ 20 ml/min. However, clinical monitoring is recommended starting from the 1st week of treatment until steady-state levels of the drug are reached in the blood (average 4 days).
For patients with severe renal impairment (creatinine clearance < 20 ml/min), the recommended starting dose is 10 mg per day (regardless of the frequency and schedule of dialysis procedures in patients undergoing hemodialysis).
No dose adjustment is necessary for patients with hepatic impairment; however, clinical monitoring is desirable at the beginning of therapy.
Children
The safety and efficacy of the drug in children have not been established, therefore its use in this category of patients is contraindicated.
Overdose
Symptoms of drug overdose: bradycardia or excessive decrease in blood pressure.
In case of bradycardia or excessive decrease in blood pressure, it is necessary to administer
- 1-2 mg of atropine intravenously;
- 1 mg of glucagon (repeat the administration of the drug if necessary);
- if necessary, perform a slow infusion of 25 mcg of isoprenaline or administer
2.5-10 mcg/kg/min dobutamine.
In case of cardiac decompensation in newborns whose mothers used beta-blockers during pregnancy:
- glucagon at a dose of 0.3 mg/kg body weight;
- hospitalization in the intensive care unit;
- isoprenaline and dobutamine: usually in fairly high doses and for a long time, under the supervision of a specialist.
Adverse reactions
Skin and subcutaneous tissue disorders:
skin reactions, including psoriasis-like rashes or exacerbation of psoriasis (see section "Special warnings and precautions for use"), urticaria, itching, hyperhidrosis.
Nervous system disorders: dizziness, headache, distal paresthesia, lethargy.
Visual disorders: dry eyes, visual acuity reduced.
Mental disorders: asthenia, insomnia, fatigue, depression, nightmares, confusion, hallucinations.
Digestive system disorders: gastrointestinal disorders (abdominal pain, diarrhea, nausea and vomiting.)
Metabolic and nutritional disorders: hypoglycemia, hyperglycemia, bradycardia (possibly severe), slowing of atrioventricular conduction or worsening of existing atrioventricular block, heart failure, decreased blood pressure.
Vascular disorders: cold extremities, Raynaud's syndrome, worsening of intermittent claudication.
Respiratory, thoracic and mediastinal disorders: bronchospasm, dyspnea.
Laboratory parameters: The appearance of antinuclear antibodies has been observed rarely, which was only in exceptional cases accompanied by clinical manifestations of systemic lupus erythematosus type, which resolved after discontinuation of treatment.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging, out of the reach of children.
Packaging
10 tablets of 10 mg, 20 mg in a blister. 3 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Medochemie LTD (Central Factory).
Location of the manufacturer and its business address
1-10, Constantinoupoleos Street, Limassol, 3011, Cyprus.
