Active substanceBetaxololBetaxolol
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  • Dosage form: & nbspfilm-coated tablets
    Composition:

    Each tablet contains:

    active substance: betaxolol hydrochloride 20 mg;

    Excipients: Microcrystalline cellulose, lactose monohydrate, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, titanium dioxide E171, lecithin, xanthan gum, purified talc.

    Description:

    White or almost white, round biconvex, film-coated tablets with a line on one side.

    Pharmacotherapeutic group:Beta1-blocker selective
    ATX: & nbsp

    S.01.E.D.02   Betaxolol

    Pharmacodynamics:

    Betak - cardioselective beta1-adrenoceptor without internal sympathomimetic activity. Has a weak membrane-stabilizing activity. Has hypotensive effect, associated with a decrease in the minute volume of the heart and a decrease in sympathetic stimulation of peripheral vessels. When used in therapeutic doses betaxolol does not have a pronounced cardiodepressive effect, does not affect glucose metabolism, does not reduce the bronchodilating action of beta-adrenomimetics, does not cause delay in sodium and water in the body. The effect of the drug begins in 1-2 hours, the duration of action - 24 h.

    Pharmacokinetics:

    Absorption from the gastrointestinal tract is 100%. Bioavailability - 78-90%, food does not affect the speed and volume of absorption. After oral administration, the maximum concentration of betaxolol in the blood is reached in 2-4 hours. Stable concentration is observed after 5-7 days of taking the drug. The therapeutic concentration is 0.005-0.05 μg / ml. The connection with plasma proteins is 50-60%.The volume of distribution is from 4.0 to 13.01 l / kg.

    It is actively metabolized in the liver, metabolites are not active.

    Permeability through blood-brain and placental barriers is low. Betaxolol penetrates into breast milk, which should be considered in the case of prescribing during lactation.

    The half-life is 14-22 hours. It is excreted by the kidneys to 80% (15% unchanged). Kidney clearance is 0.2-0.34 l / kg / hour. Half-life with a violation of the liver is extended by 33%, but the clearance does not change; if the renal function is impaired, the half-life period increases on average by half, which requires a dose reduction.

    Indications:

    - Arterial hypertension;

    - prevention of attacks of stable angina pectoris.

    Contraindications:

    - Hypersensitivity to betaxolol and other components of the drug;

    - chronic heart failure of II-III degree;

    - acute heart failure;

    - cardiogenic shock;

    - atrioventricular blockade of II-III degree;

    - sinoatrial blockade;

    - syndrome of weakness of the sinus node;

    - pronounced bradycardia (heart rate (heart rate) less than 40 beats / min.);

    - angina of Prinzmetal;

    - cardiomegaly (no signs of heart failure);

    - arterial hypotension (in case of use with myocardial infarction);

    - simultaneous administration of monoamine oxidase inhibitors (MAO);

    - combined therapy with sultopride and floktaphenin;

    - age under 18 years (effectiveness and safety not established);

    - congenital galactosemia, malabsorption syndrome glucose / galactose or lactase deficiency (lactose formulation contains).

    Carefully:

    Patients with allergic history, chronic obstructive pulmonary disease, bronchial asthma, emphysema (including lung), diabetes, metabolic acidosis, chronic heart failure, peripheral vascular disease obliterans ( "intermittent" claudication, Raynaud's syndrome), hepatic insufficiency , chronic renal failure, myasthenia gravis, thyrotoxicosis, depression (including history), psoriasis degree atrioventricular block I, pheochromocytoma, pregnancy and pozhi th age.

    Pregnancy and lactation:

    During pregnancy, use the drug with caution and only in the event that,if the benefit to the mother exceeds the risk of side effects in the fetus and / or the child.

    Beta-blockers penetrate into breast milk. The risk of hypoglycemia or bradycardia has not been investigated, so breastfeeding during treatment should be discontinued.

    Dosing and Administration:

    The use of arterial hypertension and the prevention of attacks of stable angina: Betak taken once a day, regardless of food intake, washed down with water.

    The initial dose is 10 mg (1/2 tablets) per day. If necessary, increase the dose to 20 mg per day after 1-2 weeks. The drug is used under the control of heart rate (heart rate). With the development of bradycardia, the dose is reduced or abolished. The hypotensive effect occurs after 2-5 days, the stable effect develops after 1-2 months.

    In patients with impaired renal function (creatinine clearance less than 20 ml / min), with chronic hemodialysis, the initial dose of the drug is 5 mg / day. If necessary, increase the dose every 2 weeks by 5 mg to the maximum recommended daily dose of 20 mg.

    In patients with hepatic insufficiency a dose change is usually not required.However, at the beginning of therapy, a more thorough clinical observation of the patient is recommended.

    In elderly patients the initial dose of Betac is 5 mg per day.

    Side effects:

    From the side of the cardiovascular system: sinus bradycardia, palpitations, orthostatic hypotension, disturbance of myocardial conductivity, atrioventricular block (up to cardiac arrest), arrhythmias, weakening of myocardial contractility, development (or aggravation) of symptoms of heart failure (swelling of the ankles, feet, shins), pronounced decrease in arterial pressure, manifestation angiospasm (reduction of peripheral circulation, coldness of the lower limbs, Raynaud's syndrome), chest pain.

    From the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), a hypothyroid condition.

    From the respiratory system: obstruction of the nose, difficulty breathing when taken in high doses, in predisposed patients - laryngo- and bronchospasm.

    Allergic reactions: itching, rash, urticaria

    From the skin: hyperemia of the skin, exanthema, exacerbation of psoriasis symptoms, increased sweating.

    From the central nervous system: increased fatigue, weakness, dizziness, headache, drowsiness, insomnia, nightmares, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenic syndrome, muscle weakness, paresthesia in the extremities (with intermittent claudication, Raynaud's syndrome), tremor.

    From the digestive system: nausea, rarely vomiting, diarrhea or constipation, abdominal pain, impaired liver function (dark urine, icteric sclera or skin, cholestasis), taste change, dryness of the oral mucosa.

    From the sense organ: impaired vision, decreased lacrimal gland secretion, dry and painful eyes, conjunctivitis.

    On the part of the organs of hematopoiesis: leukopenia, thrombocytopenia, agranulocytosis.

    Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

    Other: back pain, arthralgia, weakening of libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure).

    Laboratory indicators: change in hepatic enzyme activity (aspartate aminotransferase and alanine aminotransferase), bilirubin level. In rare cases, the appearance of antinuclear antibodies is observed, which only in exceptional cases is accompanied by clinical manifestations of the type of systemic lupus erythematosus that occur when the treatment is discontinued.

    Overdose:

    Symptoms: severe bradycardia, dizziness, atrioventricular block, marked decrease in arterial pressure, fainting, arrhythmias, ventricular extrasystole, heart failure, bronchospasm, convulsions, cyanosis of finger nails or palms.

    Treatment: gastric lavage and administration of absorbent drugs; symptomatic therapy: with atrioventricular blockade, intravenous injection of 1-2 mg of atropine, epinephrine or temporary cardiac pacemaker is indicated; with arterial hypotension, if there is no evidence of pulmonary edema, intravenous drip infusion of plasma substitutes is recommended, with inefficiency - the introduction of epinephrine, dopamine, dobutamine; In bronchospasm inhalation beta is used1-adrenomimetics; with convulsions - intravenously injected diazepam; with ventricular extrasystole - lidocaine (preparations of Class 1A do not apply); with heart failure - cardiac glycosides, diuretics, glucagon.

    Interaction:

    Betaxolol slows down excretion lidocaine and xanthines (Besides diphylline) and increases their concentration in blood plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

    Nonsteroidal anti-inflammatory drugs weaken the hypotensive effect by delaying sodium and water and inhibiting the synthesis of prostaglandins in the kidneys.

    Glucocorticosteroids and estrogens reduce the hypotensive effect due to sodium retention.

    Simultaneous application phenothiazines from Betaxolol leads to an increase in the concentration of each drug in the blood plasma.

    Cardiac glycosides, methyldopa, reserpine and guanfacine, amiodarone, blockers of "slow", calcium channels (verapamil, diltiazem) and other antiarrhythmic drugs increase the risk of developing or aggravate bradycardia, the likelihood of developing atrioventricular blockade, cardiac arrest and heart failure.

    The simultaneous use of betaxolol, insulin and oral hypoglycemic drugs masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure) and changes the effectiveness of the latter.

    Betaxolol is not recommended at the same time as MAO inhibitors due to a significant increase in hypotensive effect. A break in the treatment between the methods of these drugs should be at least 14 days.

    Phenytoin when administered intravenously, means for inhalation of general anesthesia (hydrocarbon derivatives) increase the severity of cardiodepressive action and the likelihood of developing arterial hypotension.

    Betaxolol extends the action of nondepolarizing muscle relaxants and anticoagulant effect coumarins.

    Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensives can cause excessive blood pressure lowering.

    Tri- and tetracyclic antidepressants, antipsychotics, ethanol, sedative and hypnotic drugs increase the CNS depression.

    Unhydrated alkaloids of ergot increase the risk of peripheral circulatory disorders.

    Allergens, used for immunotherapy, or allergen extracts for skin tests increase the risk of severe allergic reactions or anaphylaxis in patients receiving betaxolol.

    Nifedipine can lead to a significant decrease in blood pressure.

    Iodine-containing radiopaque medicines for intravenous administration increase the risk of developing anaphylactic reactions.

    Special instructions:

    Since studies on the efficacy and tolerability of betaxolol in children not conducted, its use in pediatrics is not recommended.

    When taking the drug should be monitored heart rate and blood pressure - at the beginning of treatment daily and then 1 time in 3 - 4 months, blood glucose in patients with diabetes mellitus (1 time in 4-5 months.) In elderly patients should be monitored kidney function (1 every 4-5 months).

    It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at a heart rate of less than 50 beats per minute.

    In elderly patients, if there is an increasing bradycardia (less than 50 beats / min), arterial hypotension (BP below 100 mmHg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney function, it is necessary to lower the dose or stop treatment.

    Treatment should not be stopped abruptly, especially in patients with ischemic heart disease. The dose should be reduced gradually, that is, within 1-2 weeks and, if necessary, it is possible to simultaneously start substitution therapy to avoid the progression of angina pectoris.

    When used simultaneously with insulin and oral hypoglycemic agents betaxolol can mask symptoms of hypoglycemia (eg, tachycardia).

    Drugs that reduce catecholamine stocks (eg, reserpine), can enhance the action of beta-blockers. Patients taking such drugs should be under constant medical supervision for arterial hypotension or bradycardia.

    Patients with bronchopulmonary diseases can be prescribed cardioselective beta-blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but you should strictly follow the dosage, because Overdose is dangerous by the development of bronchospasm.

    Bronchial asthma and chronic obstructive pulmonary disease: beta-blockers may be prescribed only to patients with moderate disease severity, with the choice of a selective beta-adrenoblocker in a low initial dose.Before the start of treatment it is recommended to perform an evaluation of the function of breathing. When developing seizures during treatment, bronchodilators - β2-adrenomimetics.

    Patients using contact lenses, should take into account that against the background of treatment may reduce the production of tear fluid.

    With the development of depression, caused by the use of beta-blockers, it is recommended to stop therapy. When discontinuing therapy, the dose of the drug is recommended to be reduced gradually (by 1/4 every 3-4 days) for 1-2 weeks to avoid the occurrence of the "withdrawal" syndrome.

    In case of need for planned surgical treatment the drug is withdrawn 48 hours before the start of the general anesthesia. An anesthesiologist should be informed that the patient was receiving beta-blocker therapy. If the patient has taken the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.

    With thyrotoxicosis betaxolol can mask certain clinical signs of the disease (for example, tachycardia). Abrupt withdrawal of the drug in such patients can lead to increased symptoms.

    With diabetes mellitus admission betaxolol and can mask tachycardia caused by hypoglycemia. In contrast to non-selective beta-blockers, betaxolol practically does not increase insulin-induced hypoglycemia and does not delay the restoration of the glucose concentration in the blood to a normal level.

    When taken concomitantly with clonidine The abolition of clonidine should be carried out a few days after Betak's withdrawal.

    With a weighed allergic anamnesis it is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usually recommended doses of epinephrine.

    It is necessary to cancel Betak before the study of the blood and urine content of catecholamines, normetanephrine and vanillin-mandelic acid, antinuclear antibody titers.

    For the duration of treatment, exclude the use of ethanol.

    In "smokers" the effectiveness of beta-blockers is lower.

    In newborns, whose mothers were treated with beta-blockers, the effect of the latter persists for several days after birth. Although this residual effect may not have clinical consequences, nevertheless, it is possible to develop a heart defect requiring intensive care for a newborn (see section "Overdose").In such a situation, the introduction of blood volume-increasing solutions (the risk of developing pulmonary edema) should be avoided.

    There are also reports of bradycardia, respiratory distress syndrome and hypoglycemia, therefore careful monitoring of newborns under specialized conditions (HR control, blood glucose levels during the first 3-5 days of life) is recommended.

    Athletes must take into account that the drug contains an active substance, which can give a positive reaction when conducting tests of doping control.

    Effect on the ability to drive transp. cf. and fur:

    With caution apply Betak in patients, whose activities require increased concentration and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, film-coated, 20 mg.

    Packaging:

    For 10 tablets in a blister of PVC / aluminum foil.

    For 3 blisters with instructions for use are placed in a cardboard box.

    Storage conditions:

    Store in a dry, dark place at a temperature of up to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014124 / 01
    Date of registration:10.09.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:Medocemi Co., Ltd.Medocemi Co., Ltd. Cyprus
    Manufacturer: & nbsp
    Representation: & nbspMEDOKEMI LTD. MEDOKEMI LTD. Cyprus
    Information update date: & nbsp24.01.2017
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