Zebeta
Zebeta
Zebeta (Bisoprolol)Pharmacological action
Reduces activity of a renin of plasma, reduces requirement of a myocardium for oxygen, reduces the CARDIAC CONTRACTIONS RATE (in rest and at a load). Hypotensive, antiarrhytmic and antianginal an effect has. Blocking in low doses heart b1-adrenoreceptors, reduces an intracellular current of ions of calcium, renders negative hrono - dromo - batmo - and inotropic action, oppresses conductivity and excitability, reduces contractility of a myocardium.
The hypotensive effect is bound to reduction of minute volume of blood, sympathetic stimulation of peripheric vessels, depression of activity a system renin-angiotenzinovoj (has larger value for patients with an initial hypersecretion of a renin), restoration of sensitivity of baroreceptors of an aortic arch. At an arterial hypertensia the effect comes in 2-5 days, stable action develops in 1-2 months
The antianginal effect is caused by reduction of requirement of a myocardium in oxygen as a result contractility depressions, diastole elongation, improvement of perfusion of a myocardium. At the expense of rising of final diastolic pressure in a left ventricle and augmentations of a stretching of muscular fibers of ventricles can raise requirement of a myocardium for oxygen, especially at patients with a chronic heart failure.
At application in average therapeutic doses, unlike not selective beta adrenoblockers, makes less expressed impact on the organs containing b2-adrenoreceptors (a pancreas, sceletal muscles, smooth muscles of peripheric arteries, bronchuses and a uterus) and on carbohydrate metabolism, does not cause a delay of ions of sodium in an organism; expression of atherogenous action does not differ from propranolol action. At application in the big doses (200 mg and more) the blocking effect on both subtypes of b-adrenoreceptors, mainly, in bronchuses and in unstriated muscles of vessels renders.
Indications
- An arterial hypertensia;
- Preventive maintenance of attacks of a stenocardia.
Dosage regimen
Preparation of 2 mg If necessary prescribe inside in a dose of 1 times/days a dose enlarge to 10 mg of 1 times/days the Maximum daily dose - 20 mg/days
At patients with disturbance of function of kidneys at a clearance of a creatinine less than 20 ml/mines or with the expressed disturbances of function of a liver the maximum daily dose - 10 mg.
Tablets should be accepted in the morning on an empty stomach, not chewing, washing down with liquid enough.
Side effect
From party TSNS: undue fatigability, delicacy, giddiness, a headache, dream disorders, depression, anxiety, confusion of consciousness or short-term loss of memory, hallucination, an asthenia, a myasthenia, paresthesias in extremities, a tremor.
From sense organs: sight disturbance, reduction of secretion of a plaintive liquid, dryness and morbidity of eyes, a conjunctivitis.
From cardiovascular system: a sinus bradycardia, palpitation, disturbance of conductivity of a myocardium, AV-blockade (up to development of full cross-section blockade and a cardiac standstill), arrhythmias, weakening of contractility of a myocardium, development (aggravation) of a chronic heart failure (puffiness of malleoluses, feet, a dyspnea), BP depression, an orthostatic hypotension, vasomotor spasm implication (intensifying of disturbance of a peripheric circulation, a cold snap of the bottom extremities), a stethalgia.
From the alimentary system: taste changes, dryness of a mucosa of an oral cavity, a nausea, vomiting, an abdominal pain, a constipation or a diarrhoeia, a hepatitis, disturbances of function of a liver (dark urine, yellowness of scleras or a skin, a cholestasia), change of activity of enzymes of a liver, level of bilirubin, triglycerides.
From endocrine system: a hyperglycaemia, a hypoglycaemia (at the patients receiving insulin), a hypothyroid condition.
From hemopoiesis system: a thrombocytopenia (unusual bleedings and hemorrhages), an agranulocytosis, a leukopenia.
Dermatological reactions: diaphoresis intensifying, a dermahemia, an exanthema, psoriasiform dermal reactions, an exacerbation of symptoms of a psoriasis.
Allergic reactions: a dermal itch, an eruption, an urticaria.
The other: a dorsodynia, an arthralgia, potency depression, a withdrawal (intensifying of attacks of a stenocardia, BP rising).
Contraindications
- A shock;
- A collapse;
- A fluid lungs;
- An acute heart failure;
- A chronic heart failure in a decompensation stage (including a cardiogenic shock);
- AV-blockade II and III degrees;
- Sinuatrial blockade;
- The expressed bradycardia;
- A cardiomegaly (without heart failure signs);
- An arterial hypotension (systolic arterial pressure less than 90 mm hg, especially at a myocardial infarction);
- A bronchial asthma;
- Chronic obstructive illness of lungs in the anamnesis;
- Simultaneous reception of inhibitors MAO (except for inhibitors MAO of type);
- Late stages of disturbance of a peripheric circulation;
- A Raynaud's disease;
- A pheochromocytoma (without simultaneous use of alpha adrenoblockers);
- A metabolic acidosis;
- The lactemia period;
- Age till 18 years (efficiency and safety are not established);
With care it is necessary to prescribe a preparation at hepatic insufficiency, chronic renal insufficiency, a myasthenia, a thyrotoxicosis, a diabetes, AV - blockade of I degree, a psoriasis, depression (including in the anamnesis), to patients of advanced age.
Pregnancy and lactemia
Application of Zebeta preparation at pregnancy and in a lactemia is possible in that case when the potential advantage for mother exceeds risk of development of by-effects at a foetus and the child.
It is established, that at Zebeta reception at pregnancy at a foetus the pre-natal growth inhibition, a hypoglycaemia, a bradycardia becomes perceptible.
Special indicatings
At Zebeta appointment is necessary to measure regularly the CARDIAC CONTRACTIONS RATE and a BP (in the treatment beginning - daily, then - 1 time in 3-4 months), to spend electrocardiogram, to define glucose level in blood at sick of a diabetes (1 time in 4-5 months). At elderly patients it is recommended to supervise function of kidneys (1 times in 4-5 months).
It is necessary to train the patient in a technique of calculation of the CARDIAC CONTRACTIONS RATE and to instruct about necessity of medical consultation at the CARDIAC CONTRACTIONS RATE less than 50 ud./minutes
Before the treatment beginning it is recommended to carry out research of function of external breath at patients with the burdened bronho-pulmonary anamnesis.
It is necessary to consider, that approximately at 20 % sick of a stenocardia beta adrenoblockers are noneffective because of a serious coronary atherosclerosis with a low threshold of an ischemia (the CARDIAC CONTRACTIONS RATE less than 100 ud./mines) and the raised final diastolic volume of the left ventricle breaking a subendocardial blood flow.
At smoking patients efficiency of beta adrenoblockers decreases.
The patients using contact lenses, should consider, that against treatment reduction of production of a plaintive liquid is possible.
At Zebeta use patients with a pheochromocytoma have a risk of development of a paradoxical arterial hypertensia (if the effective alpha-adrenoblokada preliminary is not reached).
At a Zebeta thyrotoxicosis can mask certain clinical signs of a thyrotoxicosis (for example, a tachycardia). Sharp Zebeta cancellation at patients with a thyrotoxicosis is contraindicative, as is capable to strengthen disease semiology.
At a Zebeta diabetes can mask a tachycardia caused by a hypoglycaemia. Unlike not selective beta adrenoblockers practically does not strengthen the hypoglycaemia caused by insulin and does not detain restoration of concentration of a glucose in blood to normal level.
At simultaneous reception of Clonidinum its reception can be stopped only in some days after Zebeta cancellation.
Intensifying of expression of reaction of a hypersensibility and absence of effect from usual doses of Epinephrinum against the burdened allergological anamnesis is possible.
In case of need carrying out of planned surgical treatment spend preparation cancellation for 48 h prior to the beginning of the general anaesthesia. If the patient has accepted a preparation before operation, it should pick up a medical product for the general anaesthesia with the minimum negative inotropic action.
The medical products reducing stocks of catecholamins (including Reserpinum), can strengthen action of beta adrenoblockers, therefore the patients accepting such combinations of medical products, should be under constant observation of the doctor about revealing of the expressed depression of a BP or a bradycardia.
In case of occurrence in patients of advanced age of an accruing bradycardia (less than 50 ud./mines), the expressed depression of a BP (a systolic BP below 100 mm hg), AV-blockade, a bronchospasm, ventricular arrhythmias, serious disturbances of function of a liver and kidneys it is necessary to reduce a dose of a preparation or to stop treatment. It is recommended to stop therapy at depression development.
It is impossible to interrupt sharply treatment because of danger of development of serious arrhythmias and a myocardial infarction. Cancellation spend gradually, reducing a dose within 2 weeks and more (reduce a dose on 25 % in 3-4 days).
Influence on ability to driving of motor transport and to management of mechanisms
In treatment it is necessary to be careful at driving of motor transport and employment by other potentially dangerous kinds of the activity demanding raised concentration of attention and speed of psychomotor reactions.
Overdosage
Symptoms: an arrhythmia, the expressed bradycardia, AV-blockade, BP depression, a chronic heart failure, a cyanosis of fingernails of fingers or palms, difficulty of breath, a bronchospasm, giddiness, syncopal conditions, cramps.
Treatment: a gastric lavage and appointment of adsorbing medical products. Spend symptomatic therapy. At the developed AV-blockade - i.v. introduction of atropine of 1-2 mg, Epinephrinum or statement of a time cardiostimulator; if there are no fluid lungs signs - i.v. enter plasma substituting solutions, at an inefficiency - introduction of Epinephrinum, Dopaminum, Dobutaminum (for maintenance of chronotropic and inotropic action and elimination of the expressed depression of a BP); at a heart failure - warm glycosides, diuretics, a glucagon; at cramps - i.v. Diazepamum; at a bronchospasm - beta2-adrenomimetiki it is inhalation.
Medicinal interaction
Simultaneous Zebeta application with inhibitors MAO owing to appreciable intensifying of hypotensive action is not recommended. Having rummaged in treatment between reception of inhibitors MAO should make not less than 14 days.
The allergens used for an immunotherapy, or extracts of allergens for dermal assays raise risk of occurrence of serious system allergic reactions or an anaphylaxis at the patients Zebeta receiving.
At simultaneous Zebeta application reduces a clearance of lidocaine and xanthines (except Diphyllinum) and raises their concentration in plasma, especially at patients with initially raised clearance of Theophyllinum under the influence of smoking.
Conditions and periods of storage
The list. In dry, protected from light, a place inaccessible to children, at a room temperature from 15 to 25 C. The Period of validity - 3 years.
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