Bisoprolol сандоз

General characteristics. Structure:

Active ingredient: бисопролол; 1 tablet contains a bisoprolol of a fumarat of 2,5 mg or 5 mg, or 10 mg;

excipients: lactoses, monohydrate; starch corn; cellulose microcrystallic; methylparaben (Е 218); propylparaben (Е 216); talc; magnesium stearate; silicon dioxide colloid anhydrous; gipromelloza; titanium dioxide (E171); wax of karnaubskiya; dye: for tablets of 2,5 mg – quinolinic yellow (E104); for tablets of 5 mg – iron oxide (ІІІ) yellow (E172); for tablets of 10 mg – erythrosine (E127).

Main physical and chemical properties: tablets, coated, round form, biconvex; on 2,5 mg – yellow color, on 5 mg – brownish-yellow color, on 10 mg – pink color.

Pharmacological properties:

Pharmacodynamics. Active ingredient of drug Bisoprolol SANDOZ — бисопролол — the selection blocker β1-адренорецепторов. In therapeutic doses has no internal sympathomimetic activity and clinically expressed membranostabilizuyushchy properties. Bisoprolol SANDOZ has anti-hypertensive and anti-anginal effect. At treatment of patients with an ischemic heart disease without chronic heart failure Bisoprolol SANDOZ reduces the need of a myocardium for oxygen due to decrease in ChSS, reduction of cordial emission and decrease in the ABP. Normalizes perfusion of a myocardium due to decrease in end diastolic pressure and lengthening of a diastole. Drug has very low affinity to β2-адренорецепторам unstriated muscles of bronchial tubes and vessels, and also to β2-адренорецепторам endocrine system. Drug only in some cases can influence unstriated muscles of bronchial tubes and peripheral arteries, and also glucose metabolism.
Bisoprolol does not possess the expressed negative inotropic effect. The maximum effect of a bisoprolol is reached in 3–4 h later in/in uses. At one-time reception action Bisoprolola SANDOZ proceeds during 24 h. The maximum anti-hypertensive effect of a bisoprolol is, as a rule, reached in 2 weeks.

Pharmacokinetics. After reception бисопролол it is almost completely soaked up in a GIT. Bioavailability makes about 90% and does not depend on meal. Linkng with proteins of a blood plasma makes 30%, distribution volume — 3,1 l/kg, and the general clearance — about 15 l/kg. T½ makes 10–12 h of a blood plasma Bisoprolol is brought from an organism thus: 50% of active agent turn in a liver into inactive metabolites and are allocated with kidneys, 50% are removed with urine in not changed look. Dose adjustment for patients with an abnormal liver function or kidneys easy and moderately severe is not required. The pharmacokinetics of a bisoprolol linear also does not depend on age of the patient.

Indications to use:

AG, ischemic heart disease (stenocardia); chronic heart failure.

Route of administration and doses:

The dose of drug is selected individually, taking into account efficiency of treatment and ChSS. Treatment should be begun with low doses, gradually raising them.
The recommended dose makes 5 mg of 1 times a day.
AG ІІ degrees (diastolic the ABP to 105 mm of mercury.) in an initiation of treatment the dose of 2,5 mg of 1 times a day can be appointed (1/2 tablets on 5 mg). In case of need the dose can be raised to 10 mg of 1 times a day. Increase in a dose is allowed only in some cases.
The maximum daily dose — 20 mg.
Patients with a liver and renal failure
For patients with disturbance of functions of a liver or kidneys easy and moderately severe usually selection of a dose should not be done.
For patients with the expressed depression of function of kidneys (clearance of creatinine <20 ml/min.) and patients with a severe form of abnormal liver functions a daily dose 10 mg should not exceed.
Patients of advanced age do not need dose adjustment.
Drug should be accepted in the morning, without chewing, irrespective of meal, washing down with a small amount of liquid. Tablets can be divided.
The course of treatment is long. Duration of treatment depends on character and the course of a disease.
It is impossible to stop treatment suddenly, it is necessary to graduate slowly, gradually reducing a dose.

Features of use:

Treatment of HSN bisoprololy should be begun with titration of a dose. Therapy cannot be rummaged suddenly, it is necessary to graduate slowly, with a gradual dose decline.
Extra care is necessary during treatment bisoprololy patients with AG or stenocardia which are followed by heart failure.
With extra care it is necessary to accept Bisoprolol SANDOZ in such cases:
AV blockade І degrees;
diabetes mellitus with sharp fluctuations of indicators of level of glucose in blood; symptoms of a hypoglycemia can be hidden (for example tachycardia, a heart consciousness, the increased sweating);
rigid diet;
Printsmetal's stenocardia;
bronchospasm (OH and other obstructive diseases of moderately severe lungs);
long desensibilizatsionny therapy;
disturbance of peripheric circulation (increase in expressiveness of symptoms, especially at the beginning of therapy is possible).
Before an initiation of treatment it is recommended to conduct a research of functions of external respiration at patients with OH in the anamnesis.
It is necessary to warn the anesthesiologist about reception of blockers of β-adrenoceptors surely.......... It is not recommended to apply blockers of β-adrenoceptors during surgical interventions. It can increase risk of developing of arrhythmias and ischemia of a myocardium. A dose it is necessary to lower and stop gradually administration of drug approximately for 48 h to the general anesthesia.
At present patients have no sufficient therapeutic experience of treatment of HSN with the following diseases and morbid conditions: a diabetes mellitus of the I type, heavy renal failures and/or a liver, a restrictive cardiomyopathy, inborn heart disease, hemodynamically significant acquired valve heart diseases, a myocardial infarction for the last 3 months.
Sick psoriasis (including in the family anamnesis) blockers of β-adrenoceptors appoint advantage/risk after careful assessment.
To patients with a pheochromocytoma бисопролол appoint only against the background of the previous therapy blockers of α-adrenoceptors..........
During therapy bisoprololy thyrotoxicosis symptoms can mask.
At OH or other chronic obstructive diseases of moderately severe lungs the accompanying therapy is shown by bronchodilators. In certain cases against the background of administration of drug patients with OH, in connection with increase in a tone of respiratory tracts, can need higher doses β2-симпатомиметиков.
Drug use Bisoprolol SANDOZ can give positive reaction at a doping test.
Drug contains lactose therefore patients should not appoint it with the most rare hereditary forms of intolerance of a galactose, deficit of lactase or a syndrome malabsorption glucose-galaktoznoy.
Use during pregnancy and feeding by a breast
Do not apply. During therapy by drug breastfeeding should be stopped.
Children. Do not apply.
Ability to influence speed of response at control of vehicles or work with other mechanisms
In some cases drug can affect ability to manage vehicles or to work with difficult mechanisms therefore it should be considered especially in an initiation of treatment and at drug dose adjustment.

Side effects:

Undesirable effects are classified by the frequency of manifestations: very often (≥1/10), it is frequent (≥1/100, <1/10), sometimes (≥1/1000, <1/100), is rare (≥1/10 000, <1/1000), is very rare (<1/10 000), unknown (frequency cannot be estimated due to the lack of data).
From mentality: sometimes — a depression, a sleep disorder; seldom — nightmares, hallucinations.
From TsNS: very often — dizziness, a headache; seldom — a syncope.
From an organ of sight: seldom — decrease in a slezootdeleniye (it is necessary to consider when carrying contact lenses); very seldom — conjunctivitis.
From an acoustic organ: seldom — deterioration in hearing.
From cardiovascular system: very often — bradycardia (at patients with HSN); often — signs of an exacerbation of already existing heart failure (at sick HSN), a cryesthesia or numbness of extremities, arterial hypotension; sometimes — disturbance of atrioventricular conductivity, especially at patients with heart failure, orthostatic hypotension.
From respiratory system: sometimes — a bronchospasm at patients with OH in the anamnesis and chronic obstructive respiratory diseases; seldom — allergic rhinitis.
From a GIT: often — nausea, vomiting, diarrhea, a lock.
From gepatobiliarny system: seldom — hepatitis.
From skin: seldom — allergic reactions (an itch, reddening, a dieback); very seldom — at treatment by blockers of β-adrenoceptors can note an aggravation of symptoms of patients with psoriasis in the form of psoriasis rash, an alopecia.
From skeletal and muscular system: sometimes — a myasthenia, a spasm of muscles, spasms.
From reproductive system: seldom — disturbance of a potentiality.
General frustration: often — an adynamy (at patients with HSN), fatigue (especially in an initiation of treatment) is usually poorly expressed and passes for 1–2 weeks; sometimes — an adynamy (at patients with hypertensia and an ischemic heart disease).
Laboratory indicators: seldom — increase in the TG level in blood, increase in activity of liver enzymes in a blood plasma (ASAT, ALAT).

Interaction with other medicines:

Bisoprolol it is not necessary to apply along with floktafeniny as blockers of β-adrenoceptors can interfere with the compensatory cardiovascular reactions connected with arterial hypotension or the shock caused floktafeniny.
Bisoprolol it is not necessary to apply along with sultopridy as at the same time the risk of ventricular arrhythmia increases.
At simultaneous use of nifedipine and other blockers of calcium channels (dihydropyridine derivatives) hypotensive action of a bisoprolol can amplify.
At simultaneous use with antiarrhytmic medicines (Phenytoinum, Disopyramidum, lidocaine, флекаинид, Amiodaronum) there can be a disturbance of conductivity and a negative inotropic effect.
At simultaneous use with parasympathomimetic drugs time of AV conductivity can increase and raise risk of bradycardia.
At simultaneous use of a bisoprolol and blockers of β-adrenoceptors of local action (for example contained in eye drops for treatment of glaucoma) action of a bisoprolol can amplify.
At simultaneous use with insulin and anti-diabetic drugs for oral administration there can be a hypoglycemic effect.
At simultaneous use with blockers of β-adrenoceptors symptoms of a hypoglycemia can be hidden.
At simultaneous use with medicines for anesthesia the risk of developing of arrhythmias and ischemia of a myocardium can increase.
Simultaneous use with cardiac glycosides (foxglove drugs) can lead to decrease in ChSS, AV conductivity disturbance.
At simultaneous use with NPVP the hypotensive effect of a bisoprolol decreases.
At simultaneous use with β-sympathomimetics ((((((((((Dobutaminum, орципреналин) the effect of both medicines decreases.
Sympathomimetics which activate α-and β-adrenoceptors ((((((((((Epinephrinum, Norepinephrinum) raise the ABP and strengthen the phenomena of the alternating lameness.
Tricyclic antidepressants, barbiturates, фенотиазин strengthen hypotensive effect.
At simultaneous use with MAO inhibitors (except for MAO inhibitors of V type) the hypotensive effect of blockers of β-adrenoceptors increases..........
It is not necessary to apply at the same time blockers of calcium channels (verapamil, diltiazem), anti-hypertensive means (a clonidine, Methyldopum, моксонидин, Reserpinum) against the background of therapy bisoprololy. It can lead to development or deterioration in bradycardia, AV blockade, heart failure, decrease in the ABP.
At combined use with meflokhiny the risk of development of bradycardia increases.
At simultaneous use with derivatives of ergotamine disturbances of peripheral perfusion amplify.
At the combined use with rifampicin perhaps insignificant reduction of T½ of a bisoprolol. Usually there is no need for dose adjustment.

Contraindications:

Individual hypersensitivity to a bisoprolol or any other component of drug; heart failure in a decompensation phase; cardiogenic shock; atrioventricular blockade of II and III degrees; syndrome of weakness of a sinus node; the expressed sinuatrial blockade; symptomatic bradycardia (ChSS <60 уд. / mines); symptomatic arterial hypotension (systolic pressure <100 mm of mercury.); serious chronic obstructive illness of lungs; heavy OH; late stages of disturbance of peripheric circulation, Raynaud's disease; a pheochromocytoma which was not treated; metabolic acidosis; simultaneous use with floktafeniny and sultopridy; period of pregnancy and feeding by a breast; children's age.

Overdose:

Symptoms: bradycardia, arterial hypotension, bronchospasm, acute heart failure, hypoglycemia.
Treatment: to stop administration of drug and to see a doctor. Depending on extent of overdose carry out the supporting and symptomatic therapy. There are data according to which бисопролол hard is exposed to dialysis.
At bradycardia: in/in administration of atropine. In case of bradycardia which will not respond to treatment with care it is possible to apply изопреналин or other means with positive chronotropic effect, if necessary — cardiostimulation.
At arterial hypotension: reception of vasoconstrictive drugs, in/in introduction of a glucagon.
At AV blockade of II and III degrees: careful monitoring of patients is necessary during infusional introduction of an izoprenalin; in case of need apply cardiostimulation.
At HSN aggravation: in/in introduction of diuretic means, vazodilatator and vasoconstrictors.
At a bronchospasm: broncholitic drugs (for example изопреналин), blockers β2-адреномиметиков and/or Aminophyllinum.
At a hypoglycemia: in/in administration of glucose.

Storage conditions:

Period of validity 3 years from date of production of drug in packaging of "in bulk". To store in original packaging at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, on 5 mg / 12,5 mg No. 30
Tablets, film coated, on 10 mg / 25 mg No. 30