Betak of the tab. of p/o of 20 mg No. 30

Pharmacological properties

Pharmacodynamics. betaksolol it is characterized by three pharmacological properties:

• cardioselective β-adrenoceptor blocking action;
• lack of partial agonistic activity (that is does not show own simpatomitichesky activity);
• weak membrane stabilizing effect (like quinidine or local anesthetics) in the concentration exceeding the recommended therapeutic doses.

Pharmacokinetics

Absorption. Drug is quickly and completely soaked up after intake at very small effect of the first passing through a liver and very high bioavailability — about 85% that provides low differences of its concentration in blood plasma at different patients or at one patient at prolonged use.

Betaksolol contacts proteins of blood plasma for 50%.

Metabolism. The volume of distribution is about 6 l/kg of body weight. In an organism betaksolol generally turns into inactive metabolites, and only 10–15% of a betaksolol define in urine in not changed look. The main way of elimination — through kidneys.

Removal. T _½ betaksolola makes 15–20 h of an organism

Indication

Ag. prevention of attacks of angina of exertion.

Use

Usual dose at ag and for prevention of attacks of angina of exertion — 1 tablet on 20 mg/days

Dosing for patients with a renal failure. At patients with a renal failure the clearance of a betaksolol decreases with decrease in kidney function.

Dose needs to be adapted to a condition of function of kidneys of the patient: at clearance of creatinine of ≥20 ml/min. of dose adjustment it is not required. However it is recommended to make clinical observation, since 1st week of treatment before achievement of equilibrium levels of medicine in blood (on average 4 days).

For patients with a heavy renal failure (clearance of creatinine of 20 ml/min.) the recommended initial dose makes 10 mg/days (irrespective of frequency and the schedule of procedures of dialysis at patients to whom the hemodialysis is carried out).

For patients with a liver failure need to adjust a dose; however at the beginning of therapy the clinical observation is desirable.

Children. Safety and efficiency of use of medicine for children are not established therefore its application for this category of patients is contraindicated.

Contraindication

Severe forms oh and hobl. the heart failure which is not controlled by treatment. cardiogenic shock. av-blockade of ii and iii of degree at the patients who do not have a pacemaker. stenocardia printsmetat (monotherapy by medicine is contraindicated at the isolated / standard form of this disease). dysfunction of sinus node (including sinuatrial blockade). bradycardia (chss 45–50 ud. / mines). severe forms of a syndrome of Reynaud and other violations of peripheric circulation. not treated pheochromocytoma. arterial hypotension. hypersensitivity to a betaksolol. anaphylactic reactions in the anamnesis. metabolic acidosis.

for application in a combination with floktafeniny and sultopridy (see INTERACTIONS).

in combination with Amiodaronum, bepridily, diltiazem and verapamil (see INTERACTIONS).

Due to the availability of lactose it is medicine it is contraindicated to patients with a congenital galactosemia, malabsorption of a glucose/galactose or a syndrome of deficiency of lactase.

Side effects

Disturbance from skin and hypodermic cellulose: skin reactions, including psoriazopodobny rashes or exacerbation of psoriasis (see special instructions), urticaria, an itch, a hyperhidrosis.

Disturbance from nervous system: dizziness, headache, distal paresthesias, lethargy.

Disturbance from an organ of sight: dryness of a mucous membrane of an eye, violation of visual acuity.

Mental disorders: adynamy, insomnia, fatigue, depression, nightmares, confusion of consciousness, hallucination.

Disturbance from digestive system: gastrointestinal frustration (abdominal pain, diarrhea, nausea and vomiting.)

Metabolic and nutritive frustration: a hypoglycemia, a hyperglycemia, bradycardia (perhaps, heavy), delay of AV conductivity or strengthening of the existing AV blockade, heart failure, decrease in the ABP.

Disturbance from vessels: cryesthesia in extremities, Reynaud's syndrome, deterioration in the alternating lameness.

Disturbance from a respiratory system, a thorax and mediastinum: bronchospasm, dispnoe.

Disturbance from a reproductive system: impotence.

Laboratory indicators. Emergence of antinuclear antibodies which only in exceptional cases was followed by clinical manifestations as a system lupus erythematosus, disappearing after the treatment termination is seldom observed.

Special instructions

Never should stop suddenly medicament treatment at patients with stenocardia: the sharp termination of administration of medicament can lead to serious violations of a warm rhythm, a myocardial infarction or sudden to a lethal outcome.

Due to the availability of lactose it is medicine it is contraindicated to patients with a congenital galactosemia, malabsorption of a glucose/galactose or a syndrome of deficiency of lactase.

Precautionary measure at application. Drug withdrawal. Treatment by medicines should not be stopped suddenly, especially at persons with an ischemic heart disease. The dose needs to be reduced gradually, during 1–2 weeks, and if necessary it is possible to begin at the same time replacement therapy to avoid progressing of stenocardia.

OH and HOBL. Patients can only appoint blockers of β-adrenoceptors with moderate severity of a disease, with the choice of a selection blocker of β-adrenoceptors in a low initial dose. Before an initiation of treatment it is recommended to carry out the assessment of respiratory function.

At development of attacks during treatment can apply bronchodilators (β ₂ - adrenomimetik).

Heart failure. For treatment of patients with not refractory heart failure the medicament Betak in case of need can be used under careful control in low doses which gradually raise.

Bradycardia. The dose needs to be lowered if ChSS at rest 50–55 ud. / mines and the patient has clinical manifestations of bradycardia.

AV blockade of the I degree. Considering negative dromotropic effect of blockers of β-adrenoceptors, Betak with care appoint to patients with AV blockade of the I degree.

Printsmetal's Stenocardia. The quantity and duration of attacks of stenocardia can increase at application of blockers of β-adrenoceptors for patients with Printsmetal's stenocardia. Use of medicine is possible at a disease of moderate severity and provided that treatment is carried out along with use of vasodilators.

Disturbance of peripheric circulation. Blockers of β-adrenoceptors can lead to aggravation of symptoms of patients with violations of peripheric circulation (Raynaud's disease or Reynaud's syndrome, arteritis or chronic obliterating diseases of arteries of the lower extremities). In such cases it is recommended to apply a cardioselective blocker of β-adrenoceptors with existence of properties of partial agonist of β-receptors; it is necessary to appoint it with care.

Pheochromocytoma. At application of blockers of β-adrenoceptors the treatment of AG caused by a pheochromocytoma requires careful monitoring of the ABP.

Sick advanced age. At patients of advanced age the strict compliance to contraindications is obligatory. It is necessary to be careful: treatment of patients of advanced age should be begun with a low dose and under careful observation (see USE).

Sick with a renal failure. For patients with a renal failure the dose of medicine needs to be adjusted depending on concentration of creatinine in blood or clearance of creatinine (see USE).

Patients with diabetes. It is necessary to warn the patient about need to strengthen self-checking of level of glucose of blood in an initiation of treatment. Prodromal symptoms of a hypoglycemia can be disguised, especially tachycardia, heartbeat and the increased sweating (see INTERACTIONS and SIDE EFFECTS).

Psoriasis. Prescribing of medicine demands careful assessment about need of its application as there are messages about aggravation of symptoms of patients with psoriasis at treatment by blockers of β-adrenoceptors (see. Side EFFECTS).

Allergic reactions. At the patients inclined to the heavy anaphylactic reactions which are especially connected with application of a floktafenin (see INTERACTIONS), or when performing desensitization the therapy by blockers of β-adrenoceptors can lead to further strengthening of reactions and decrease in efficiency of treatment of this state epinephrine in usual doses.

General anesthesia. Blockers of β-adrenoceptors cause easing of reflex tachycardia and increase risk of developing arterial hypotension. Treatment continuation by blockers of β-adrenoceptors reduces risk of developing arrhythmia, myocardial ischemia and hypertensive crises. It is necessary to inform the anesthesiologist that the patient undergoes treatment by blockers of β-adrenoceptors.

In need of the termination of treatment and medicament withdrawal enough 48 h for recovery of sensitivity to catecholamines are considered.

Therapy by blockers of β-adrenoceptors should not be stopped:

• sick with coronary insufficiency, it is desirable for them to take the medicament before operation, considering the risk connected with sudden cancellation of a blocker of β-adrenoceptors;
• in case of urgentny operations or when the termination of treatment is impossible. The patient needs to be protected from consequences of excitement of vagus nerve, applying premedication atropine, with repetition if necessary. It is necessary to apply means which suppress a myocardium least to anesthesia, and the loss of blood should be offset.

needs to consider risk of development of anaphylactic reactions.

Ophthalmology. Blockade of β-adrenoceptors leads to decrease in intraocular pressure and can cause change of results of screening assay of glaucoma. It is necessary to inform the ophthalmologist on what the patient accepts betaksolol. The patients applying blockers of β-adrenoceptors and it is system, and in the form of eye drops, demand control taking into account possible additive effect of these medicines.

Thyrotoxicosis. Blockers of β-adrenoceptors mask cardiovascular symptoms of a thyrotoxicosis.

Athletes. Athletes need to consider that medicine contains active substance which can give positive reaction when carrying out tests of anti-doping control.

Drug contains lactose therefore it should not be applied to patients with rare hereditary forms of intolerance of a galactose, insufficiency of lactase or a syndrome of a glyukozo-galaktozny malyadsorbtion.

during pregnancy and feeding by a breast

Pregnancy. Teratogenic aspect. Now messages about teratogenic effects of medicine at the person are not received. Neonatal aspect. Action of blockers of β-adrenoceptors remains within several days after the birth at newborns whose mothers applied this medicine. Though the specified residual effect can not have clinical consequences, nevertheless the possibility of development of heart failure remains. In that case the newborn should be placed in intensive care unit (see OVERDOSE). In such situation it is necessary to avoid use of plasma substitutes (because of risk of developing a sharp fluid lungs). Also there are messages about bradycardia, respiratory a distress syndrome and a hypoglycemia. Therefore careful observation of newborns in specialized conditions is recommended (control of ChSS and level of glucose of blood during the first 3–5 days of life).

, except for cases when the advantage of use of medicine exceeds possible risks.

Feeding by a breast. Blockers of β-adrenoceptors get into breast milk. Feeding by a breast during the Betak medicament treatment should be stopped as risk of development of a hypoglycemia or bradycardia at newborns did not study.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Researches of influence of a betaksolol on ability to steer vehicles or to work with mechanisms were not conducted. At control of vehicles or work with other mechanisms it is necessary to consider that against the background of intake of this medicine can sometimes arise dizziness, violation of visual acuity and other side reactions that can negatively affect ability to steer vehicles or to work with other mechanisms.

Interaction

Bradycardia can be caused by a number of medicines: blockers of β-adrenoceptors, antiarrhytmic medicines of the class ia (quinidine, Disopyramidum), the class iii (Amiodaronum and sotalol), the class iv (diltiazem and verapamil) and also foxglove glycosides, a clonidine, guafantsiny, meflokhiny and the cholinesterase inhibitors applied to treatment at Alzheimer's disease.

Contraindicated simultaneous application Betak with medicines stated below

Floktafenin. At shock or the arterial hypotension caused floktafeniny the blockers of β-adrenoceptors cause decrease in compensatory cardiovascular reactions.

Sultoprid. Disturbance of a warm rhythm (excessive bradycardia) caused by additive effect of decrease in ChSS.

is not recommended to use the medicament Betak with medicines stated below

Blockers of calcium channels (bepridit, diltiazem and verapamil). Disturbance of automatism (excessive bradycardia, stop of sinus node), AV conductivity and also heart failure (synergy action). Such combinations can be applied only at careful clinical control and ECG monitoring, especially at patients of advanced age or in an initiation of treatment.

Amiodaronum. Disturbance of contractility, automatism and conductivity (oppression of sympathetic compensatory mechanisms).

Should use with care the medicament Betak with medicines stated below

Inhalation anesthetics containing halogen. Blockers of β-adrenoceptors cause decrease in cardiovascular compensatory reactions (during operation the oppression of β-adrenoceptors can be eliminated with β-stimulators).

As a rule, therapy by blockers of β-adrenoceptors it is not necessary to stop, and sharp medicament withdrawal should be avoided anyway. It is necessary to report to the anesthesiologist about the carried-out treatment.

Drugs which can provoke Bouveret's ventricular disease like torsade de pointes (except a sultoprid). Antiarrhytmic medicines of the class Ia (quinidine, hydroquinidine and Disopyramidum) and class III (Amiodaronum, dofetilid, ibutilid, sotatol); some neuroleptics of group of a fenotiazin (Chlorpromazinum, tsiamemazin, levomepromazinum, thioridazine), benzamides (amisulprid, Sulpiridum, tiaprid), phenyl propyl ketones (Droperidolum, a haloperidol), other neuroleptics (Pimozidum) and other medicines (tsizaprid, difemanit, in/in erythromycin, galofantrin, mizolastin, moxifloxacin, pentamidine, in/in Spheromycinum and Vincaminum). Increase in risk of developing ventricular arrhythmia and especially Bouveret's disease as torsades de pointes (the hypopotassemia is a provocative factor). Also ECG control is necessary clinical.

Propafenon. Disturbance of contractility, automatism and conductivity (oppression of sympathetic compensatory mechanisms). Also ECG control is necessary clinical.

Baclofenum. Strengthening of antihypertensive action. Control of the ABP and dose adjustment of antihypertensive medicament is required.

Insulin and anti-diabetic streptocides. Some symptoms of a hypoglycemia, such as tachycardia, heartbeat can mask all blockers of β-adrenoceptors (see. Special INSTRUCTIONS). The patient needs to be warned about need of strengthening of self-checking of level of glucose of blood.

cholinesterase Inhibitors (ambenomium, donepezil, Galantaminum, neostigmin, pyridostigmine, rivastigmin, takrin). Risk of strengthening of bradycardia (additive action). Regular clinical control is necessary.

Antihypertensive medicaments of the central action (clonidine, apraklonidin, alpha Methyldopum, guanfantsin, moksonidin, rilmenidin). Substantial increase of the ABP at sharp cancellation of antihypertensive medicine of the central action. It is necessary to avoid sudden cancellation of antihypertensive medicament and to carry out clinical control.

Lidokain (in / c). Increase in concentration of lidocaine in blood plasma with possible strengthening of undesirable neurologic and warm effects (decrease in metabolism of lidocaine in a liver). It is recommended clinical and ECG control and, perhaps, definition of concentration of lidocaine in blood plasma both during treatment by blockers of β-adrenoceptors, and after its termination. If necessary — lidocaine dose adjustment.

Combination, requiring special attention

NPVP (system), including selection TsOG-2 inhibitors. Decrease in hypotensive effect (oppression of the NPVP vazodilatiruyushchy prostaglandins, delay of liquid and sodium pyrazolon derivatives).

Blockers of calcium channels (dihydropyridines). Arterial hypotension, a circulatory unefficiency at patients with latent or uncontrollable heart failure. Treatment by blockers of β-adrenoceptors can minimize reflex nice mechanisms which are started at excessive hemodynamic reactions.

Antidepressants, related to Imipraminum, neuroleptics. Strengthening of hypotensive effect and risk of developing of orthostatic hypotension (additive action).

Meflokhin. Risk of bradycardia (additive action concerning development of bradycardia).

Dipiridamolum (in / c). Strengthening of antihypertensive effect.

Blockers of α-adrenoceptors applied in urology (alfuzozin, docsazozin, Prazozinum, tamsulozin, terazozin). Strengthening of antihypertensive effect. The increased risk of orthostatic hypotension.

Amifostin. Strengthening of antihypertensive effect.

Cardiac glycosides. A combination which can prolong time of AV conductivity and to become the cause of bradycardia.

Fingolimod. Simultaneous application of a fingolimod with blockers of β-adrenoceptors can enhance bradikardichny effect and therefore this combination is not recommended. In case of need simultaneous application the corresponding monitoring is required from the moment of an initiation of treatment, it is recommended to carry out night monitoring.

Yodosoderzhashchy contrast agents. In case of shock or arterial hypotension on introduction of yodosoderzhashchy contrast agents, blockers of β-adrenoceptors cause reduction of expressiveness of cardiovascular compensatory reactions.

, treatment by blockers of β-adrenoceptors is required to be stopped before carrying out a radiographic research. If application is necessary, the doctor has to have possibilities of performing intensive care.

GKS and tetrakozaktid. Decrease in antihypertensive effect (a delay of water and sodium in a combination with GKS).

Overdose

medicine overdose Symptoms: bradycardia or excessive decrease hell.

In bradycardia or excessive decrease in the ABP needs to be entered: 1–2 mg of atropine in/in; 1 mg of a glucagon (to repeat introduction of medicine if necessary); if necessary to carry out slow infusion of 25 mkg of an izoprenalin or to enter 2.5-10 mkg/kg/min. of Dobutaminum.

At a warm decompensation at newborns whose mothers during pregnancy applied blockers of β-adrenoceptors: a glucagon at the rate of 0.3 mg/kg of body weight; hospitalization in intensive care unit; izoprenalin and Dobutaminum: usually in rather high doses and long time, under control of the expert.

Storage conditions

At a temperature not above 25 °C in original packing.