Bisoprolol-Mick

General characteristics. Structure:

Active ingredient: 2,5 mg, 5 mg or 10 mg of a bisoprolol of a fumarat.

Antihypertensive.

Pharmacological properties:

Pharmacodynamics. The selection β-adrenoblocker without own sympathomimetic activity; has hypotensive, antiarrhytmic and anti-anginal effect. Blocking in low doses β 1 adrenoceptors of heart, reduces stimulated catecholamines formation of cyclo-adenosinemonophosphate (tsAMF) from adenosinetriphosphate (ATP), reduces intracellular current of calcium ions, renders negative hrono-, dromo-, batmo-and inotropic action, urezhat the heart rate (HR), conductivity and excitability oppresses, reduces contractility of a myocardium.

At increase in a dose has β2-адреноблокирующее effect. The General Peripheric Vascular Resistance (GPVR) at the beginning of use of β-adrenoblockers, in the first 24 h, increases (as a result of reciprocal increase of activity of α-adrenoceptors and elimination of stimulation β2-адренорецепторов) which in 1-3 days is returned to initial, and at long appointment decreases.

The hypotensive effect is connected with reduction of the minute volume of blood (MVB), sympathetic stimulation of peripheral vessels, decrease of the activity system renin-angiotensin-aldosteronovoy (has bigger value for patients with initial hypersecretion of a renin), recovery of sensitivity of baroreceptors of an aortic arch (there is no strengthening of their activity in response to a lowering of arterial pressure (ABP) and influence on the central nervous system (CNS). At arterial hypertension the effect occurs in 2-5 days, stable action - in 1-2 months.

The anti-anginal effect is caused by reduction of need of a myocardium for oxygen as a result of an urezheniye of ChSS and decrease in contractility, lengthening of a diastole, improvement of perfusion of a myocardium. Due to increase in end diastolic pressure in a left ventricle and increases in stretching of muscle fibers of ventricles can increase oxygen requirement, especially at patients with the chronic heart failure (CHF).

The antiarrhytmic effect is caused by elimination of aritmogenny factors (tachycardia, a superactivity of a sympathetic nervous system, the increased maintenance of tsAMF, arterial hypertension), reduction of speed of spontaneous excitement of sinus and ectopic pacemakers and delay of atrioventricular (AV) carrying out (it is preferential in antegrade and to a lesser extent in retrograde the directions through an AV node) and on additional ways.

Unlike non-selective β-adrenoblockers at appointment in average therapeutic doses exerts less expressed impact on the bodies containing β2-адренорецепторы (a pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchial tubes and a uterus) and on carbohydrate metabolism, does not cause a delay of ions of sodium in an organism; expressiveness of atherogenous action does not differ from effect of propranolol.

Pharmacokinetics: Absorption - 80-90%, meal does not influence absorption, TCmax - 2-4 h, communication with proteins of plasma - 26-33%. Permeability through a blood-brain barrier (GEB) and a placental barrier - low, secretion with breast milk - low. It is metabolized in a liver, T1/2 is 9-12 h. It is removed by kidneys - 50% in not changed look, less than 2% with bile.

Indications to use:

- Arterial Hypertension (AH),
- coronary heart disease: stable stenocardia.

Route of administration and doses:

Bisoprolol-Mick it is necessary to accept in the morning to, in time or after food. The capsule should be swallowed entirely with a small amount of water. Treatment should be begun with small doses and to increase a dose slowly. Anyway, the dose should be defined individually depending on pulse rate and success of treatment.

Duration of treatment is not limited. It depends on type and disease severity. Treatment Bisoprololom-Mick cannot be stopped sharply, especially at patients with coronary heart disease, t. to as it can lead to an aggravation of a condition of the patient. If the termination of treatment is necessary, the dose should be reduced gradually (for example, reduction twice of a dose at an interval of a week).

Arterial hypertension. The recommended dose makes 5 mg of a bisoprolol once a day. At easy forms of arterial hypertension (diastolic arterial pressure is up to 105 mm of mercury.) treatment can be to 2,5 mg once a day that it is quite enough.

If necessary the dose can be increased to 10 mg once a day. Further increase in a dose is justified only in exceptional cases.

The maximum recommended dose makes 20 mg once a day.

Coronary heart disease (stenocardia). The recommended dose makes 5 mg of a bisoprolol once a day. If necessary the dose can be increased to 10 mg once a day. Further increase in a dose is justified only in exceptional cases.

The maximum recommended dose makes 20 mg once a day.

Dosage at a liver and/or renal failure. With hepatic or renal dysfunction easy or moderate severity of dose adjustment usually is not required from patients. At patients with a heavy renal failure (clearance of creatinine <20 ml/min.) and at patients with heavy abnormal liver functions the daily dose of a bisoprolol should not exceed 10 mg.

Experience of use of a bisoprolol for dialysis patients is limited and there are no proofs about need of change of a dose.

Elderly people. It is not required from elderly patients of dose adjustment.

Children. There is no therapeutic experience of use of a bisoprolol for children. For this reason this means cannot be recommended for children.

Features of use:

During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of the side reactions given below was defined according to the following:
- very often ≥1/10;
- often ≥1/100, <1/10;
- infrequently ≥1/1000, <1/100;
- seldom ≥1/10 000, <1/1000;
- very seldom <1/10 000.

Central nervous system. Often: dizziness *, head боль*. Seldom: loss of consciousness.

General disturbances. Often: the adynamy (at patients with HSN) raised утомляемость*. Infrequently: an adynamy (at patients with arterial hypertension or stenocardia).

Mental disturbances. Infrequently: depression, sleeplessness. Seldom: hallucinations, nightmares.

From an organ of sight. Seldom: reduction of dacryagogue (it is necessary to consider when carrying contact lenses). Very seldom: conjunctivitis.

From an acoustic organ. Seldom: hearing disorder.

From cardiovascular system. Very often: bradycardia (at patients with HSN). Often: aggravation of symptoms of a current of HSN (at patients with HSN), feeling of a cold snap or numbness in extremities, the expressed decrease in the ABP especially at patients with HSN. Infrequently: disturbance of AV of conductivity, bradycardia (at patients with arterial hypertension or stenocardia); aggravation of symptoms of a current of HSN (at patients with arterial hypertension or stenocardia), orthostatic hypotension.

From respiratory system. Infrequently: a bronchospasm at patients with bronchial asthma or obstruction of respiratory tracts in the anamnesis. Seldom: allergic rhinitis.

From the alimentary system. Often: nausea, vomiting, diarrhea, lock.
Seldom: hepatitis.

From a musculoskeletal system. Infrequently: muscular weakness, myotonia.

From integuments. Seldom: hypersensitivity reactions, such as skin itch, rash, hyperemia of integuments. Very seldom: alopecia. Beta adrenoblockers can promote an aggravation of symptoms of a course of psoriasis or cause psoriazopodobny rash.

From reproductive system. Seldom: disturbance of a potentiality.

Laboratory indicators. Seldom: increase in concentration of triglycerides and activity of "hepatic" transaminases in blood (aspartate aminotransferases (ASF), alaninaminotranspherases (ALT)).

* At patients with arterial hypertension or stenocardia especially often these symptoms appear at the beginning of a course of treatment. Usually these phenomena have easy temper and pass, as a rule, within 1-2 weeks after an initiation of treatment.

Interaction with other medicines:

The allergens used for an immunotherapy or extracts of allergens for skin tests increase risk of emergence of heavy system allergic reactions or an anaphylaxis at the patients receiving бисопролол.

Iodinated X-ray contrast diagnostic means for in / венного introductions increase risk of development of anaphylactic reactions.

Phenytoinum at in / венном introduction, HP for inhalation general anesthesia (derivatives of hydrocarbons) is raised by expressiveness of cardiodepressive action and probability of decrease in the ABP.

Changes efficiency of insulin and peroral hypoglycemic HP, masks symptoms of the developing hypoglycemia (tachycardia, increase in the ABP).

The clearance of lidocaine and xanthines (except Diphyllinum) can decrease in connection with possible increase in their concentration in a blood plasma, especially at patients with initially increased clearance of theophylline under the influence of smoking.

Non-steroidal anti-inflammatory drugs (NPVP), glucocorticoid means (GKS) and estrogen weaken hypotensive effect of a bisoprolol (a delay of ions of sodium, blockade of synthesis of prostaglandins kidneys).

Cardiac glycosides, Methyldopum, Reserpinum and гуанфацин, blockers of "slow" calcium channels (BMKK) (verapamil, diltiazem), Amiodaronum, etc. antiarrhytmic means increase risk of development or aggravation of bradycardia, AV blockade, a cardiac standstill and the heart failure (HF). Nifedipine can lead to considerable decrease in the ABP.

Diuretics, clonidine, sympatholytics, гидралазин, etc. can lead hypotensive drugs to excessive decrease in the ABP.

Action of not depolarizing muscle relaxants and anticoagulating effect of coumarins during treatment bisoprololy can be extended.

Rub - and tetracyclic antidepressants, antipsychotic HP (neuroleptics), ethanol, sedative and HP hypnotic drugs strengthen oppression of TsNS.

Simultaneous use with monoamine oxidase inhibitors (MAO) owing to considerable strengthening of hypotensive action is not recommended. Having rummaged in treatment between reception of MAO inhibitors and a bisoprolola has to make not less than 14 days.

Not hydrogenated alkaloids of an ergot increase risk of development of disturbances of peripheric circulation.

Ergotamine increases risk of development of disturbance of peripheric circulation; Sulfasalazinum increases concentration of a bisoprolol in a blood plasma; rifampicin shortens T1/2 of a bisoprolol.

Contraindications:

Bisoprolol-Mick it is not necessary to apply at patients with:
- heart failure or with an acute decompensation of cordial function.

Therapy by means of inotropic drugs is required;
- cardiogenic shock;
- The degree AV block II or III (without pacemaker);
- disease of a sinus node (sick sinus syndrome);
- sinuatrial block;
- bradycardia from less than 60 beats/min prior to treatment;
- arterial hypotension (systolic the ABP is lower than 100 mm hg);
- heavy bronchial asthma or heavy chronic obstructive frustration;
- at late stages of diseases of peripheral arteries, an obliterating endarteritis and Reynaud's syndrome;
- uncured pheochromocytoma;
- metabolic acidosis;
- hypersensitivity to a bisoprolol or any of excipients;
- age up to 18 years;

Pregnancy and period of a lactation.

Storage conditions:

List B. In the dry, protected from light place. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in blister strip packagings, on 3 planimetric cells in a cardboard box.