Bidop

General characteristics. Structure:

Active agent: bisoprolola гемифумарат 5 mg or 10 mg.

Excipients: lactoses monohydrate, cellulose microcrystallic, magnesium stearate, кросповидон, a pigment of the PB 22812 brand yellow (lactoses monohydrate of 87%, iron oxide of yellow 13%) (for a dosage of 5 mg), a RV-27215 brand pigment beige (lactoses monohydrate of 87%, ferrous oxide red and yellow 13%) (for a dosage of 10 mg).

Pharmacological properties:

Pharmacodynamics. The selection a beta 1 adrenoblocker without own sympathomimetic activity, does not possess membrane stabilizing action. Reduces activity of a renin of a blood plasma, reduces the need of a myocardium for oxygen, urezhat the heart rate (HR) (at rest and at loading). Has hypotensive, anti-anginal and antiarrhytmic effect. Blocking in low doses beta1 - heart adrenoceptors, reduces stimulated catecholamines formation of cyclic adenosinemonophosphate (tsAMF) from adenosinetriphosphate (ATP), reduces intracellular current of calcium ions, renders negative hrono-, dromo-, batmo-and inotropic action, oppresses conductivity and excitability.
At exceeding of a therapeutic dose has beta2-adrenoceptor blocking effect.
The general peripheric vascular resistance at the beginning of drug use, in the first 24 h, increases (as a result of reciprocal increase of activity of alpha adrenoceptors and elimination of stimulation of beta2-adrenoceptors) which in 1-3 days is returned to initial, and at long appointment - decreases.
The hypotensive effect is connected with reduction of minute volume of blood, sympathetic stimulation of peripheral vessels, decrease of the activity a system renin-angiotenzinovoy (has bigger value for patients with initial hypersecretion of a renin), recovery of sensitivity 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 is noted 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 of a myocardium, 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 oxygen requirement, especially at patients with chronic heart failure can increase.
At use in average therapeutic doses, unlike non-selective beta adrenoblockers, exerts less expressed impact on the bodies containing beta2-adrenoceptors (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 (Na+) in an organism; expressiveness of atherogenous action does not differ from effect of propranolol.
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.

Pharmacokinetics. Absorption - 80-90%, meal does not influence absorption. The maximum concentration in a blood plasma is observed in 1-3 h, communication with proteins of a blood plasma - 26-33%. Permeability through a blood-brain barrier and a placental barrier - low. 50% of a dose are metabolized in a liver with formation of inactive metabolites, an elimination half-life - 10-12 h. About 98% are brought by kidneys, out of them 50% in not changed look, less than 2% through intestines (with bile).

Indications to use:

- Arterial hypertension;
- Coronary heart disease: prevention of attacks of stable stenocardia.

Route of administration and doses:

Inside, in the morning on an empty stomach, without chewing, once. The dose should be selected individually.
Arterial hypertension and coronary heart disease: prevention of attacks of stable stenocardia usually initial dose makes 5 mg of 1 times a day.
If necessary the dose is increased to 10 mg of 1 times a day. The maximum daily dose of-20 mg a day.

Patients with a renal failure at the clearance of creatinine (CC) have less than 20 ml/min. or with the expressed abnormal liver functions the maximum daily dose - 10 mg.
Increase in a dose at such patients needs to be carried out with extra care.
Dose adjustment is not required from elderly patients.

Features of use:

Control of the patients accepting Bidop® has to include measurement of ChSS and the ABP (in an initiation of treatment - daily, then 1 time in 3-4 months) carrying out an ECG, definition of concentration of glucose in blood of patients with a diabetes mellitus (1 time in 4-5 months). At elderly patients it is recommended to control function of kidneys (1 times in 4-5 months). It is necessary to train the patient in a technique of calculation of ChSS and to instruct about need of medical consultation at ChSS less than 50 уд. / min.
Before an initiation of treatment it is recommended to conduct a research of function of external respiration at patients with the burdened bronchopulmonary anamnesis.
Approximately at 20% of patients with stenocardia beta adrenoblockers are inefficient. The main reasons - the expressed coronary atherosclerosis with a low threshold of ischemia (ChSS less than 100 уд. / min.) and the increased final diastolic volume of a left ventricle breaking a subendocardial blood stream.
At "smokers" efficiency of beta adrenoblockers is lower.
The patients using contact lenses have to consider that against the background of treatment reduction of products of the lacrimal liquid is possible.

When using patients with a pheochromocytoma have a risk of development of paradoxical arterial hypertension (if it is previously not reached effective alpha адреноблокада).
At a thyrotoxicosis of Bidop® can mask certain clinical signs of a thyrotoxicosis (for example, tachycardia). Sharp cancellation at patients with a thyrotoxicosis is contraindicated as it is capable to strengthen symptomatology.
At a diabetes mellitus can mask the tachycardia caused by a hypoglycemia. Unlike non-selective beta adrenoblockers practically does not strengthen the hypoglycemia caused by insulin and recovery of concentration of glucose in blood to normal level does not detain.
At a concomitant use of a clonidine its reception can be stopped only in several days after drug withdrawal of Bidop®.
Strengthening of expressiveness of hypersensitivity reaction and lack of effect of usual doses of Epinephrinum (adrenaline) against the background of the burdened allergological anamnesis is possible.
In case of need performing planned surgical treatment carry out drug withdrawal for 48 h prior to the beginning of the general anesthesia. If the patient accepted drug before surgical intervention, it should pick up medicine for the general anesthesia with minimum negative inotropic effect.
Reciprocal activation of a vagus nerve can be eliminated with intravenous administration of atropine (1-2 mg).
The medicines reducing stocks of catecholamines (including, Reserpinum), can strengthen effect of beta adrenoblockers therefore the patients accepting such combinations of medicines have to be under constant observation of the doctor regarding identification of the expressed decrease in the ABP or bradycardia.
Patients with bronkhospastichesky diseases can appoint cardioselective adrenoblockers in case of intolerance and/or inefficiency of other antihypertensives. The overdose is dangerous by development of a bronchospasm.
In case of emergence in patients of advanced age of the accruing bradycardia (less than 50 уд. / min.), the expressed decrease in the ABP (systolic the ABP is lower than 100 mm hg), AV of blockade, a bronchospasm, ventricular arrhythmias, heavy abnormal liver functions and kidneys it is necessary to reduce a dose or to stop treatment. It is recommended to stop therapy at development of a depression.
It is impossible to interrupt sharply treatment because of danger of development of heavy arrhythmias and a myocardial infarction. Cancellation is carried out gradually, reducing a dose within 2 weeks and more (lower a dose by 25% in 3-4 days). It is necessary to cancel before a research of content in blood and urine of catecholamines, a normetanefrin and vanilinmindalny acid; credits of antinuclear antibodies.

Influence on ability of control of vehicles and to work with the equipment
During treatment dizziness, especially at the beginning of therapy in this connection it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions is possible.

Side effects:

The side effects observed at drug use are classified on category depending on the frequency of their emergence: very often> 1/10; often> 1/100, <1/10; infrequently> 1/1000, <1/100; seldom> 1/10000, <1/1000; very seldom <1/10000, including separate messages.
- From the central nervous system: infrequently - increased fatigue, weakness, an adynamy, dizziness, a headache, frustration of a dream, a depression, concern, confusion of consciousness or short-term loss of memory, it is rare - hallucinations, a myasthenia, "dreadful" dreams, spasms (including in gastrocnemius muscles), paresthesias in extremities (at patients with the "alternating" lameness and Reynaud's syndrome), a tremor.
- From an organ of sight: seldom - a vision disorder, reduction of secretion of the lacrimal liquid, dryness and morbidity of eyes; very seldom - conjunctivitis.
- From cardiovascular system: very often - a sinus bradycardia, heartbeat; often - the expressed decrease in the ABP, manifestation of a vasomotor spasm (strengthening of disturbance of peripheric circulation, a cold snap of the lower extremities, paresthesias, Reynaud's syndrome); infrequently - orthostatic hypotension, disturbance of conductivity of a myocardium, AV blockade (up to development of total cross block and a cardiac standstill), arrhythmias, easing of contractility of a myocardium, development of chronic heart failure (puffiness of anklebones, feet, an asthma), a stethalgia.
- From the alimentary system: often - dryness of a mucous membrane of an oral cavity, nausea, vomiting, an abdominal pain, a lock or diarrhea; seldom - abnormal liver functions (dark urine, yellowness of scleras or skin, a cholestasia), taste changes, hepatitis. From respiratory system: infrequently - difficulty of breath at appointment in high doses (selectivity loss) and/or at predisposed patients - laringo-and a bronchospasm; seldom - a nose congestion.
- From endocrine system: a hyperglycemia (at patients with a non-insulin-dependent diabetes mellitus), a hypoglycemia (at the patients receiving insulin), a hypothyroid state.
Allergic reactions: seldom - a skin itch, rash, a small tortoiseshell.
- From integuments: seldom - sweating strengthening, a dermahemia; very seldom - a dieback, psoriazopodobny skin reactions, an aggravation of symptoms of psoriasis, an alopecia.
- Laboratory indicators: seldom - increase in activity of "hepatic" transaminases (increase in alaninaminotranspherase, aspartate aminotransferase), a hyperbilirubinemia, a gipertriglitseridemiya; in some cases - thrombocytopenia (unusual bleedings and hemorrhages), an agranulocytosis, a leukopenia.
Influence on a fruit: pre-natal growth inhibition, hypoglycemia, bradycardia.
Others: infrequently - an arthralgia; seldom - weakening of a libido, decrease in a potentiality; dorsodynia, syndrome of "cancellation" (strengthening of attacks of stenocardia, increase in the ABP).

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 intravenous agents increase risk of development of anaphylactic reactions.
Phenytoinum at intravenous administration, means for inhalation anesthesia (derivatives of hydrocarbons) increase expressiveness of cardiodepressive action and probability of decrease in the ABP.
Changes efficiency of insulin and hypoglycemic means for intake, masks symptoms of the developing hypoglycemia (tachycardia, increase in the ABP).
Reduces clearance of lidocaine and xanthines (except theophylline) and increases their concentration in a blood plasma, especially at patients with initially increased clearance of theophylline under the influence of smoking.
Hypotensive effect non-steroidal anti-inflammatory drugs (a delay of ions of sodium (Na+) and blockade of synthesis of prostaglandin kidneys) weaken, glucocorticosteroids and estrogen (a delay of ions of Na+).

Cardiac glycosides, Methyldopum, Reserpinum and гуанфацин, blockers of "slow" calcium channels (verapamil, diltiazem), Amiodaronum and other antiarrhytmic means increase risk of development or aggravation of bradycardia, AV of blockade, a cardiac standstill and heart failure.
Nifedipine can lead to considerable decrease in the ABP.
Diuretics, clonidine, sympatholytics, гидралазин and other antihypertensives can lead to excessive decrease in the ABP.
Extends action of not depolarizing muscle relaxants and anticoagulating effect of coumarins.
Rub - and tetracyclic antidepressants, antipsychotic means (neuroleptics), ethanol, sedative and hypnagogues strengthen oppression of the central nervous system.
Simultaneous use with MAO inhibitors is not recommended (except for MAO-B, see the section "Contraindications"), owing to considerable strengthening of hypotensive action, having rummaged in treatment between reception of MAO inhibitors (except for MAO-B) 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; rifampicin shortens an elimination half-life.

Contraindications:

Hypersensitivity to a bisoprolol and other beta adrenoblockers; shock (including cardiogenic); collapse; fluid lungs; acute heart failure; the chronic heart failure in a decompensation stage demanding performing inotropic therapy; AV blockade of the II-III degree without electrocardiostimulator; sinuatrial blockade; sick sinus syndrome; the expressed bradycardia (ChSS less than 60 уд. / min.); a cardiomegaly (without symptoms of heart failure); the expressed arterial hypotension (systolic the ABP less than 100 mm hg, especially at a myocardial infarction); severe forms of bronchial asthma and the chronic obstructive pulmonary disease (COPD) in the anamnesis; a concomitant use of inhibitors of a monoaminooxidase (MAO) (except for MAO-B); late stages of disturbance of peripheric circulation; Reynaud's syndrome; a pheochromocytoma (without simultaneous use of alpha adrenoblockers): metabolic acidosis; age up to 18 years (efficiency and safety are not established); a lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption (since lactose is a part of drug).
With care
Liver failure; chronic renal failure (KK less than 20 ml/min.); myasthenia; thyrotoxicosis; diabetes mellitus; Printsmetal's stenocardia, AV blockade of the I degree; psoriasis; a depression (including in the anamnesis); allergic reactions in the anamnesis; observance of a rigid diet; advanced age.

Use at pregnancy and in the period of a lactation
Use of the drug Bidop® at pregnancy is possible only in that case when the estimated advantage of therapy for mother exceeds potential risk of development of side effects in a fruit and/or the child.
There are no data on whether gets бисопролол into maternal milk. In need of use of drug in the period of a lactation breastfeeding is recommended to be stopped.

Overdose:

Symptoms: arrhythmia, ventricular premature ventricular contraction, the expressed bradycardia, AV blockade, the expressed decrease in the ABP, development of chronic heart failure, cyanosis of nails and palms, breath difficulty, a bronchospasm, dizziness, unconscious states, spasms, a hypoglycemia.

Treatment: a gastric lavage and purpose of the adsorbing means; symptomatic therapy: at the developed AV to blockade - intravenous administration of 1-2 mg of atropine, Epinephrinum or temporary statement of a pacemaker; at ventricular premature ventricular contraction - lidocaine (the drugs IA of a class are not used); at the expressed decrease in the ABP - the patient has to be in the provision of Trendelenburga; if there are no fluid lungs signs - intravenous administration of plasma substituting solutions, at inefficiency - introduction of Epinephrinum, dopamine, Dobutaminum (for maintenance, chronotropic and inotropic action and elimination of the expressed decrease in the ABP); at heart failure - cardiac glycosides, diuretics, a glucagon; at spasms - intravenously diazepam; at a bronchospasm - beta2-adrenostimulyator it is inhalation.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets, 5 mg, 10 mg.
On 14 tablets in the blister of the PVC/PVDH/ave. On 1,2 or 4 blisters with the application instruction in a cardboard pack.