Bisoprolol - instructions for use, analogs, reviews and release forms (tablets of 2.5 mg, 5 mg and 10 mg) of the drug for the treatment of angina and depression in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Bisoprolol. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Bisoprolol in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Bisoprolol in the presence of existing structural analogues. Use to treat angina and reduce pressure in adults, children,as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Bisoprolol - selective beta-blocker without its own sympathomimetic activity; has antihypertensive, antiarrhythmic and anti-anginal action. Blocking at low doses beta1-adrenoreceptors of the heart, reduces catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions (Ca2 +), has a negative chrono-, dromo-, batmo- and inotropic effect (it calms the frequency of cardiac contractions, inhibits conduction and excitability, reduces myocardial contractility).

When the dose is increased, beta2-adrenergic blocking action exerts.

The total peripheral vascular resistance at the beginning of beta-adrenoblockers in the first 24 hours increases (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta2-adrenoreceptors), which returns to the initial one after 1-3 days, and decreases with long-term administration.

Antihypertensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels,a decrease in the activity of the renin-angiotensin-aldosterone system (is more important for patients with initial renin hypersecretion), restoration of the sensitivity of the aortic arch baroreceptors (no increase in their activity in response to a decrease in blood pressure), and influence on the CNS. With arterial hypertension, the effect occurs after 2-5 days, stable effect - after 1-2 months.

The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in the heart rate and a decrease in contractility, diastole lengthening, and improvement in myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the ventricular fibers, myocardial oxygen demand may increase, especially in patients with chronic heart failure (CHF).

In contrast to nonselective beta-blockers, when administered at moderate therapeutic doses, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause retention of sodium ions (Na +) in the body.When used in large doses has a blocking effect on both subtypes of beta-adrenergic receptors.

Composition

Bisoprolol fumarate + excipients.

Pharmacokinetics

Bisoprolol is almost completely absorbed from the digestive tract (80-90%). Eating does not affect the absorption of the drug. Permeability through the blood-brain barrier and the placental barrier is low, the secretion with breast milk is low. Metabolised in the liver. It is excreted by the kidneys - 50% unchanged, less than 2% - through the intestine.

Indications

• arterial hypertension;
• ischemic heart disease (IHD): prevention of attacks of stable angina pectoris.

Forms of release

Tablets 2.5 mg, 5 mg and 10 mg.

Instructions for use and dosage

Inside, in the morning on an empty stomach, not liquid, with a small amount of liquid.

With arterial hypertension and coronary heart disease (prevention of attacks of stable angina) it is recommended to take 5 mg once. If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg.

In patients with impaired renal function (creatinine clearance less than 20 ml / min) or with severe impairment of liver function, the maximum daily dose is 10 mg.

Dose adjustments in elderly patients are not required.

Side effect

• headache;
• dizziness;
• insomnia;
• asthenia;
• depression;
• drowsiness;
• increased fatigue;
• loss of consciousness;
• hallucinations;
• "nightmarish" dreams;
• convulsions;
• confusion or short-term memory loss;
• impaired vision;
• decrease in secretion of tear fluid;
• dryness and soreness of the eyes;
• hearing impairment;
• conjunctivitis;
• sinus bradycardia;
• marked decrease in blood pressure;
• violation of AV-conduction;
• orthostatic hypotension;
• decompensation of CHF;
• peripheral edema;
• manifestation of angiospasm (increased peripheral circulatory disturbance, coldness of the lower limbs, Raynaud's syndrome, paresthesia);
• chest pain;
• diarrhea;
• nausea, vomiting;
• dryness of the oral mucosa;
• constipation;
• nasal congestion;
• difficulty breathing when given in high doses (loss of selectivity);
• in predisposed patients - laryngo- and bronchospasm;
• Hyperglycemia (type 2 diabetes mellitus);
• hypoglycemia (type 1 diabetes mellitus);
• itching;
• rash;
• hives;
• allergic rhinitis;
• increased sweating;
• hyperemia of the skin;
• exacerbation of psoriasis symptoms;
• alopecia;
• muscle weakness;
• cramps in the calf muscles;
• arthralgia;
• thrombocytopenia, agranulocytosis;
• violation of potency;
• withdrawal syndrome (increased angina attacks, increased blood pressure).

Contraindications

• acute heart failure or chronic heart failure in the stage of decompensation (requiring inotropic therapy);
• cardiogenic shock;
• atrioventricular blockade of 2 and 3 degrees, without an electrocardiostimulator;
• sinoatrial blockade;
• syndrome of weakness of the sinus node;
• bradycardia (heart rate less than 60 beats per minute);
• cardiomegaly (no signs of heart failure);
• arterial hypotension (systolic pressure less than 100 mm Hg);
• severe forms of bronchial asthma and obstructive pulmonary disease;
• severe violations of peripheral circulation, Raynaud's syndrome;
• lactation period;
• simultaneous administration of MAO inhibitors with the exception of MAO-B;
• hereditary lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
• pheochromocytoma (without simultaneous use of alpha-blockers);
• metabolic acidosis;
• simultaneous administration of floktaphenin, sultopride;
• simultaneous intravenous administration of verapamil, diltiazem;
• age under 18 years (effectiveness and safety not established);
• hypersensitivity to bisoprolol, the components of the drug and to other beta-blockers.

Application in pregnancy and lactation

Use during pregnancy is possible if the benefit to the mother exceeds the risk of side effects in the fetus.

Influence on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia, respiratory distress (neonatal asphyxia) in neonates is also possible.

If bisoprolol should be used during lactation, breastfeeding should be discontinued, as bisoprolol is excreted in breast milk.

Use in children

Contraindicated for children under the age of 18 (efficacy and safety not established).

special instructions

Control of patients taking bisoprolol should include monitoring heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), an electrocardiogram (ECG), a blood glucose concentration in patients with diabetes mellitus (1 to 4-5 month). In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 months).

Patients should be taught how to count heart rate and instructed about the need for medical consultation at a heart rate of less than 50 beats per minute.

Before the start of treatment, it is recommended to perform an external respiration function in patients with a history of bronchopulmonary anamnesis.

Approximately in 20% of patients with angina pectoris, beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increase in the end diastolic volume of the left ventricle, which disrupts the subendocardial, blood flow. In "smokers" the effectiveness of beta-blockers is lower.

Patients who use contact lenses should take into account that a reduction in tear fluid production is possible against the background of treatment.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (unless an effective alpha-adrenoblockade has been previously achieved).

In thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, as it can strengthen symptoms.

In diabetes mellitus can mask tachycardia caused by hypoglycemia.In contrast to non-selective beta-blockers, it does not substantially increase insulin-induced hypoglycemia and does not delay the restoration of glucose concentration in the blood to a normal value.

With the simultaneous administration of clonidine, his reception may be terminated only a few days after the cancellation of Bisoprolol.

It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from the usual doses of epinephrine (adrenaline) against the background of a weighed allergic anamnesis.

If it is necessary to conduct routine surgical treatment, the drug can be withdrawn 48 hours before the start of the general anesthesia. If the patient has taken the drug before the operation, he should choose a drug for general anesthesia with a minimum negative inotropic effect.

Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).

Drugs that reduce the reserves of catecholamines (for example, reserpine), can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision for the diagnosis of arterial hypotension or bradycardia.

Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs, but strict monitoring of dosage should be carried out. Overdosing is dangerous by the development of bronchospasm.

If elderly patients develop an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic BP below 100 mmHg), AV blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney dysfunction, reduce the dose or stop treatment. It is recommended to stop therapy with the development of depression caused by the use of beta-blockers.

Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).

It should be canceled before the study of blood and urine content of catecholamines, normetanephrine and vanillylmandelic acid, antinuclear antibody titers.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities; requiring increased concentration of attention and speed of psychomotor reactions.

Drug Interactions

Allergens used for immunotherapy, or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.

Phenytoin with intravenous administration, drugs for inhalation of general anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressive action and the likelihood of lowering blood pressure.

Iodine-containing radiopaque diagnostic tools for intravenous administration increase the risk of anaphylactic reactions.

Bisoprolol changes the effectiveness of insulin and hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).

Antihypertensive effect weaken non-steroidal anti-inflammatory drugs (sodium ion delay and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium ion delay).

Cardiac glycosides, methyldopa, reserpine and guanfacine increase the risk of developing or worsening bradycardia, atrioventricular blockade, cardiac arrest and heart failure.

Combinations of bisoprolol with calcium antagonists (verapamil, diltiazem, bepridil) are not recommended, with their intravenous administration, due to the increase in the negative effect on the inotropic function of the myocardium, AV-conduction and blood pressure.

The combined use of Nifedipine and bisoprolol can lead to a significant reduction in blood pressure.

With the simultaneous use of bisoprolol and antiarrhythmic drugs of class 1 (disopyramide, quinidine, hydroquinidine), atrial-ventricular conduction may worsen and negative inotropic action (clinical monitoring and monitoring of electrocardiography is necessary).

With simultaneous use of bisoprolol and antiarrhythmic drugs of class 3 (for example, amiodarone), atrial dilatation may worsen.

With the simultaneous use of the drug Bisoprolol and other beta-blockers, including those contained in eye drops, synergy is possible.

Simultaneous use of the drug Bisoprolol with beta-adrenomimetics (for example, isoprenaline, dobutamine) can lead to a decrease in the effect of both drugs.

The combination of bisoprolol with beta and alpha-adrenomimetics (eg, iorepinephrine, epinephrine) can enhance the vasoconstrictor effects of these agents that occur with alpha-adrenergic receptors, leading to an increase in blood pressure.

Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.

With the simultaneous use of bisoprolol and mefloquine, the risk of bradycardia increases.

The simultaneous administration of bisoprolol with floktaphenin and sultopride is contraindicated.

The effect of nondepolarizing muscle relaxants and the anticoagulant effect of coumarins during treatment with bisoprolol may be prolonged.

Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics), ethanol (alcohol), sedative and hypnotic drugs increase the inhibition of the central nervous system. It is not recommended simultaneous use of bisoprolol with MAO inhibitors (except MAO-B) due to a significant increase in hypotensive effect. A break in treatment between taking MAO inhibitors and Bisoprolol should be at least 14 days.

Reduces the clearance of Lidocaine and xanthines (except diprofilina) and increases their concentration in blood plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.

Sulfasalazine increases the concentration of bisoprolol in the blood plasma.

Rifampicin shortens the half-life of bisoprolol.

Analogues of the drug Bisoprolol

Structural analogs for the active substance:

• Aritel;
• Aritel Cor;
• Bidop;
• Biol;
• Biprol;
• Bisogamma;
• Bisocardium;
• Bisomore;
• Bisoprolol OBL;
• Bisoprolol Lugal;
• Bisoprolol Prana;
• Bisoprolol ratopharm;
• Bisoprolol Sandoz
• Bisoprolol Teva;
• Bisoprolol hemifumarate;
• Bisoprolol fumarate;
• Bisoprolol fumarate Pharmaplant;
• Concor;
• Concor Cor;
• Corbis;
• Cordinorm;
• Coronale;
• Niperten;
• Thyrez.

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