Bisoprolol: instructions for use. Which is better - Bisoprolol or Concor? Release forms and analogues

Gross formula

C 18 H 31 NO 4

Pharmacological group of the substance Bisoprolol

Nosological classification (ICD-10)

CAS Code

66722-44-9

Characteristics of the substance Bisoprolol

Cardioselective β 1-blocker, has no internal sympathomimetic and membrane-stabilizing activity. Bisoprolol fumarate is a white crystalline powder. Soluble in water, methanol, ethanol, chloroform. Molecular weight - 766.97.

Pharmacology

Pharmacological action- antianginal, hypotensive, antiarrhythmic.

Pharmacodynamics

A selective β 1 -blocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. It has only slight affinity for β 2 -adrenergic receptors smooth muscle bronchi and blood vessels, as well as to β 2 -adrenergic receptors involved in the regulation of metabolism. Therefore, bisoprolol generally does not affect resistance respiratory tract and metabolic processes in which β 2 -adrenergic receptors are involved.

The selective effect of bisoprolol on β 1 -adrenergic receptors persists beyond the therapeutic range.

Bisoprolol does not have a pronounced negative inotropic effect. His maximum effect achieved 3-4 hours after oral administration. Even when using bisoprolol once a day, it therapeutic effect persists for 24 hours thanks to a 10-12 hour T1/2 from blood plasma. As a rule, the maximum reduction in blood pressure is achieved 2 weeks after the start of treatment.

Bisoprolol reduces the activity of the sympathoadrenal system by blocking β 1 -adrenergic receptors of the heart.

When administered once orally in patients with coronary artery disease without signs of CHF, bisoprolol reduces heart rate, reduces the stroke volume of the heart and, as a result, reduces the ejection fraction and myocardial oxygen demand. With long-term therapy, the initially elevated TPR decreases. A decrease in renin activity in blood plasma is considered as one of the components of the antihypertensive effect of β-blockers.

Pharmacokinetics

Suction

Bisoprolol is almost completely (>90%) absorbed from the gastrointestinal tract. Its bioavailability due to insignificant metabolization during the initial passage through the liver (>10%) is about 90% after oral administration. Food intake does not affect bioavailability. Bisoprolol exhibits linear kinetics, with its plasma concentration being proportional to the dose taken in the range from 5 to 20 mg. Tmax in blood plasma is 2-3 hours.

Distribution

Bisoprolol is distributed quite widely. Vd is 3.5 l/kg. The binding to plasma proteins reaches approximately 30%.

Metabolism

Metabolized via the oxidative pathway without subsequent conjugation. All metabolites are polar (water-soluble) and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not show pharmacological activity. Data obtained from experiments with human liver microsomes under conditions in vitro, show that bisoprolol is metabolized primarily by the CYP3A4 isoenzyme (about 95%), and the isoenzyme CYP2D6 plays only a minor role.

Removal

The clearance of bisoprolol is determined by the balance between excretion by the kidneys unchanged (>50%) and metabolism in the liver (>50%) to metabolites, which are also excreted by the kidneys. The total clearance is 15 l/hour. T 1/2 - 10-12 hours.

Pharmacokinetics various groups patients

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and concurrent impairment of liver or kidney function.

Application of the substance Bisoprolol

Arterial hypertension; ischemic disease hearts: stable angina; chronic heart failure.

Contraindications

Hypersensitivity to bisoprolol; acute heart failure; chronic heart failure in the stage of decompensation, requiring inotropic therapy; cardiogenic shock; AV block II and III degrees without a pacemaker; sick sinus syndrome; sinoatrial block; severe bradycardia (HR<60 уд./мин); тяжелая артериальная гипотензия (сАД <100 мм рт.ст. ); тяжелые формы бронхиальной астмы или хронической обструктивной болезни легких; выраженные нарушения периферического артериального кровообращения или синдром Рейно; феохромоцитома (без одновременного применения α-адреноблокаторов); метаболический ацидоз; возраст до 18 лет (недостаточно данных по эффективности и безопасности у данной возрастной группы).

Restrictions on use

Carrying out desensitizing therapy; Prinzmetal's angina; hyperthyroidism; type 1 diabetes mellitus and diabetes mellitus with significant fluctuations in blood glucose concentrations; AV block of the first degree; severe renal failure (Cl creatinine<20 мл/мин); тяжелые нарушения функции печени; псориаз; рестриктивная кардиомиопатия; врожденные пороки сердца или порок клапана сердца с выраженными гемодинамическими нарушениями; хроническая сердечная недостаточность с инфарктом миокарда в течение последних 3 мес; строгая диета.

Use during pregnancy and breastfeeding

In general, beta-blockers reduce blood flow to the placenta and may affect fetal development. Blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child should be monitored and, in the event of adverse events in pregnancy and/or the fetus, alternative therapies with a proven safety profile for use during pregnancy should be taken. The newborn should be carefully examined: symptoms of bradycardia and hypoglycemia may occur in the first 3 days of life.

There is no data on the excretion of bisoprolol into breast milk. Therefore, taking this drug is not recommended for women during breastfeeding. If its use during lactation is necessary, breastfeeding should be discontinued.

Side effects of the substance Bisoprolol

The frequency of adverse reactions listed below was determined according to the following criteria recommended by WHO: very often (≥1/10); often (≥1/100,<1/10); нечасто (≥1/1000, <1/100); редко (≥1/10000, <1/1000); очень редко (<1/10000).

From the nervous system: often - dizziness 1, headache 1; rarely - loss of consciousness.

From the mental side: infrequently - depression, insomnia; rarely - hallucinations, nightmares.

From the side of the organ of vision: rarely - decreased tear production (should be taken into account when wearing contact lenses); very rarely - conjunctivitis.

Hearing and labyrinth disorders: rarely - hearing loss.

From the SSS side: very often - bradycardia (in patients with CHF); often - worsening symptoms of CHF (in patients with CHF), a feeling of coldness or numbness in the extremities, a marked decrease in blood pressure, especially in patients with CHF; uncommon - AV conduction disturbance, bradycardia (in patients with arterial hypertension or angina pectoris), worsening of symptoms of CHF (in patients with arterial hypertension or angina pectoris), orthostatic hypotension.

From the respiratory system, chest and mediastinal organs: uncommon - bronchospasm in patients with bronchial asthma or a history of airway obstruction; rarely - allergic rhinitis.

From the gastrointestinal tract: often - nausea, vomiting, diarrhea, constipation.

From the liver and biliary tract: rarely - hepatitis.

From the musculoskeletal and connective tissue side: Uncommon: muscle weakness, muscle cramps.

For the skin and subcutaneous tissues: rarely - hypersensitivity reactions, such as itching, skin rash, hyperemia of the skin; very rarely - alopecia.

β-blockers can contribute to the exacerbation of psoriasis symptoms or cause a psoriasis-like rash.

From the genital organs and breast: rarely - impaired potency.

General disorders and disorders at the injection site: often - asthenia (in patients with CHF), increased fatigue 1; infrequently - asthenia (in patients with arterial hypertension or angina pectoris).

Laboratory and instrumental data: rarely - an increase in the concentration of triglycerides and the activity of AST and ALT in the blood plasma.

1 In patients with arterial hypertension or angina, these symptoms especially often appear at the beginning of treatment. Typically, these phenomena are mild in nature and usually disappear within 1-2 weeks after the start of treatment.

Interaction

The effectiveness and tolerability of bisoprolol may be affected by the simultaneous use of other drugs. Such interaction can also occur in cases where two drugs are taken after a short period of time.

Treatment of CHF. Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.

CCBs such as verapamil and, to a lesser extent, diltiazem, when used simultaneously with bisoprolol, can lead to a decrease in myocardial contractility and impaired AV conduction. In particular, intravenous administration of verapamil to patients taking beta-blockers can lead to severe arterial hypotension and AV block. Centrally acting antihypertensive drugs (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to a decrease in heart rate and a decrease in cardiac output, as well as vasodilation due to a decrease in central sympathetic tone. Abrupt withdrawal, especially before discontinuation of beta-blockers, may increase the risk of rebound hypertension.

Combinations requiring special caution

Treatment of arterial hypertension and angina pectoris. Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.

All indications for the use of bisoprolol. CCBs - dihydropyridine derivatives (for example, nifedipine, felodipine, amlodipine) - when used simultaneously with bisoprolol, may increase the risk of developing arterial hypotension. In patients with CHF, the risk of subsequent deterioration in cardiac contractility cannot be excluded.

Class III antiarrhythmic drugs (eg amiodarone) may worsen AV conduction disturbances.

The effect of topical β-blockers (for example, eye drops for the treatment of glaucoma) may enhance the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate).

Parasympathomimetics, when used simultaneously with bisoprolol, may increase AV conduction disturbances and increase the risk of developing bradycardia.

The hypoglycemic effect of insulin or hypoglycemic drugs for oral administration may be enhanced. Signs of hypoglycemia, in particular tachycardia, may be masked or suppressed. Such an interaction is more likely when using non-selective beta-blockers.

Drugs for general anesthesia may increase the risk of cardiodepressive effects, leading to arterial hypotension (see “Precautions”).

Cardiac glycosides, when used simultaneously with bisoprolol, can lead to an increase in impulse conduction time and thus to the development of bradycardia. NSAIDs may reduce the antihypertensive effect of bisoprolol.

The simultaneous use of bisoprolol with β-adrenergic agonists (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs. The use of bisoprolol with adrenergic agonists that affect α- and β-adrenergic receptors (for example, norepinephrine, epinephrine) may enhance the vasoconstrictor effects of these drugs that occur with the participation of α-adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers.

Antihypertensive drugs, as well as other drugs with a possible antihypertensive effect (for example, tricyclic antidepressants, barbiturates, phenothiazines), can enhance the antihypertensive effect of bisoprolol.

Mefloquine, when used simultaneously with bisoprolol, may increase the risk of bradycardia.

MAO inhibitors (except MAO B inhibitors) may enhance the antihypertensive effect of β-blockers. Concomitant use may also lead to the development of a hypertensive crisis.

Overdose

Symptoms: the most common symptoms of overdose are AV block, severe bradycardia, marked decrease in blood pressure, bronchospasm, acute heart failure and hypoglycemia.

Sensitivity to a single high dose of bisoprolol varies widely among individual patients, and patients with CHF are likely to be highly sensitive.

Treatment: First of all, it is necessary to stop taking bisoprolol and begin supportive symptomatic therapy.

For severe bradycardia: intravenous administration of atropine. If the effect is insufficient, drugs with a positive chronotropic effect can be administered with caution. Sometimes temporary placement of an artificial pacemaker may be necessary.

With a pronounced decrease in blood pressure: intravenous administration of plasma-substituting solutions and vasopressor drugs.

For AV block: Patients should be closely monitored and treated with α- and β-agonists such as epinephrine. If necessary, install an artificial pacemaker.

In case of exacerbation of CHF: intravenous administration of diuretics, drugs with a positive inotropic effect, as well as vasodilators.

For bronchospasm: use of bronchodilators, incl. β 2 -adrenergic agonists and/or aminophylline.

For hypoglycemia: intravenous administration of dextrose.

Routes of administration

Inside.

Precautions for the substance Bisoprolol

Treatment with bisoprolol should not be interrupted suddenly, especially in patients with coronary artery disease. If discontinuation of treatment is necessary, the dose should be reduced gradually.

If clonidine is used simultaneously, it can be discontinued only a few days after bisoprolol is discontinued.

At the initial stages of treatment with bisoprolol, patients require constant monitoring.

Monitoring the condition of patients taking bisoprolol should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then - once every 3-4 months), conducting an ECG, determining the concentration of glucose in the blood in patients with diabetes mellitus (once every 4 months). -5 months). In elderly patients, it is recommended to monitor renal function (once every 4-5 months).

The patient should be trained in the method of calculating heart rate and instructed about the need to consult a doctor for heart rate<60 уд./мин .

Bisoprolol should be used with caution in the following cases: diabetes mellitus with significant fluctuations in plasma glucose concentrations - symptoms of severe hypoglycemia, such as tachycardia, palpitations or increased sweating, may be masked; strict diet; carrying out desensitizing therapy; AV block of the first degree; Prinzmetal's angina; mild to moderate peripheral arterial circulatory disorders (increased symptoms may occur at the beginning of therapy); psoriasis (including history).

If increasing bradycardia (HR) is detected in elderly patients<60 уд./мин), выраженного снижения АД (сАД <100 мм рт.ст. ), AV-блокады, бронхоспазма, желудочковых аритмий, тяжелых нарушений функции печени и/или почек необходимо уменьшить дозу бисопролола или прекратить лечение.

Respiratory system

For bronchial asthma or COPD, simultaneous use of bronchodilating drugs is indicated. In patients with bronchial asthma, increased resistance of the respiratory tract may occur, which requires a higher dose of β 2 -adrenergic agonists. In smokers, the effectiveness of β-blockers is lower.

Allergic reactions

β-blockers, including bisoprolol, may increase sensitivity to allergens and the severity of anaphylactic reactions due to the weakening of adrenergic compensatory regulation under the influence of β-blockers. Epinephrine therapy does not always produce the expected therapeutic effect.

General anesthesia

When performing general anesthesia, the risk of β-adrenergic receptor blockade should be taken into account. If it is necessary to discontinue bisoprolol therapy before surgery, this should be done gradually and completed 48 hours before general anesthesia.

Pheochromocytoma

In patients with an adrenal tumor (pheochromocytoma), bisoprolol can only be used against the background of simultaneous use of α-blockers.

Hyperthyroidism

When treated with bisoprolol, the symptoms of hyperthyroidism (hyperthyroidism) may be masked.

Patients who use contact lenses should be informed that during treatment there may be a decrease in tear production.

Special patient groups

Impaired kidney or liver function. In case of mild or moderate hepatic or renal dysfunction, dosage adjustment is usually not required.

In case of severe renal impairment (Cl creatinine<20 мл/мин) и у пациентов с тяжелыми заболеваниями печени максимальная суточная доза составляет 10 мг. Увеличение дозы у таких пациентов должно осуществляться с особой осторожностью.

Old age. No dose adjustment is required.

Children. Since there is not enough data on the use of bisoprolol in children, it is not recommended for use in children under 18 years of age.

Currently, there is insufficient data regarding the use of bisoprolol in patients with CHF in combination with type 1 diabetes mellitus, severe renal and/or liver dysfunction, restrictive cardiomyopathy, congenital heart defects or heart valve disease with severe hemodynamic impairment. Also, until now, sufficient data have not been obtained regarding patients with CHF with myocardial infarction within the last 3 months.

Influence or ability to perform potentially hazardous activities that require special attention and quick reactions (for example, driving, working with moving mechanisms). Bisoprolol does not affect the ability to drive vehicles, according to the results of a study in patients with coronary artery disease. However, due to individual reactions, the ability to drive vehicles or operate technically complex mechanisms may be impaired. Particular attention should be paid to this at the beginning of treatment, after changing the dose, and also when consuming alcohol at the same time.

Interactions with other active ingredients

Trade names

Name	The value of the Vyshkowski Index ®

LSR-007326/10-290710

Trade name: Bisoprolol -Teva

International nonproprietary name (INN): bisoprolol

Dosage form:

film-coated tablets

Compound
1 film-coated tablet contains:
active substance: bisoprolol fumarate 5.00 or 10.00 mg;
excipients: microcrystalline cellulose, mannitol, croscarmellose sodium, magnesium stearate;
shell: hypromellose, titanium dioxide, macrogol-6000.

Round, biconvex, film-coated tablets, white or almost white, with engraving on one side: “BISOPROLOL 5” (dosage 5 mg) or “BISOPROLOL 10” (dosage 10 mg).

Pharmacotherapeutic group:

Beta1-adrenergic blocker selective

ATX Code:С07АВ07

Pharmacological properties
Pharmacodynamics
Bisoprolol is a selective beta 1-blocker, without its own sympathomimetic activity, and does not have a membrane-stabilizing effect. As with other beta1-blockers, the mechanism of action in hypertension is unclear. At the same time, it is known that bisoprolol reduces the activity of renin in the blood plasma, reduces the myocardial oxygen demand, and reduces the heart rate (HR). It has hypotensive, antiarrhythmic and antianginal effects.
By blocking beta 1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, inhibits all cardiac functions, reduces atrioventricular (AV) conductivity and excitability. When the therapeutic dose is exceeded, it has a beta2-adrenergic blocking effect. Total peripheral vascular resistance at the beginning of drug use, in the first 24 hours, increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta2-adrenergic receptors), after 1-3 days it returns to its original value, and with long-term use it decreases.
The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the sympathoadrenal system (SAS) (of great importance for patients with initial renin hypersecretion), restoration of sensitivity in response to a decrease in blood pressure (BP) and an effect on the central nervous system (CNS). In case of arterial hypertension, the effect develops after 2-5 days, a stable effect is observed after 1-2 months.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of decreased contractility and other myocardial functions, prolongation of diastole, and improved myocardial perfusion. Due to increased end-diastolic pressure in the left ventricle and increased stretch of ventricular muscle fibers, oxygen demand may increase, especially in patients with chronic heart failure (CHF).
When used in average therapeutic doses, in contrast to non-selective beta-blockers, 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 sodium ion retention in the body; the severity of the atherogenic effect does not differ from the effect of propranolol.
Pharmacokinetics
Bisoprolol is almost completely absorbed from the gastrointestinal tract; food intake does not affect absorption. The first pass effect through the liver is negligible, resulting in high bioavailability (90%).
Bisoprolol is metabolized via the oxidative pathway without subsequent conjugation. All metabolites have strong polarity and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not exhibit pharmacological activity. Data obtained from in vitro experiments with human liver microsomes indicate that bisoprolol is metabolized primarily by the CYP3A4 isoenzyme (about 95%), with the CYP2D6 isoenzyme playing only a minor role.
Communication with blood plasma proteins is about 30%. Volume of distribution - 3.5 l/kg. Total ground clearance is approximately 15 l/h. The maximum concentration in blood plasma is determined after 2-3 hours. Permeability through the blood-brain barrier and placental barrier is low.
The plasma half-life (10-12 hours) ensures effectiveness for up to 24 hours after a single daily dose.
Bisoprolol is excreted from the body in two ways; 50% of the dose is metabolized in the liver with the formation of inactive metabolites. About 98% is excreted by the kidneys, of which 50% is excreted unchanged; less than 2% - through the intestines (with bile).
Since elimination occurs equally in the kidneys and liver, no dosage adjustment is required in patients with impaired liver function or renal failure. The pharmacokinetics of bisoprolol is linear and does not depend on age.
In patients with CHF, plasma concentrations of bisoprolol are higher and the half-life is longer compared to healthy volunteers.

Indications for use

• Arterial hypertension;
• coronary heart disease: prevention of attacks of stable angina.

Contraindications

• Hypersensitivity to the components of the drug and other beta-blockers;
• acute heart failure and CHF in the stage of decompensation, requiring inotropic therapy;
• cardiogenic shock;
• collapse;
• atrioventricular (AV) block II-III degree, without a pacemaker;
• sinoatrial block;
• sick sinus syndrome;
• bradycardia (heart rate before treatment less than 60 beats/min);
• severe arterial hypotension (systolic blood pressure less than 100 mmHg)
• cardiomegaly (without signs of heart failure);
• severe forms of bronchial asthma and a history of chronic obstructive pulmonary disease (COPD);
• severe peripheral circulatory disorders;
• Raynaud's syndrome;
• metabolic acidosis;
• pheochromocytoma (without simultaneous use of alpha-blockers);
• simultaneous use of monoamine oxidase inhibitors (MAO) (with the exception of MAO type B inhibitors);
• concomitant use of floctafenine and sultopride.
• age under 18 years (efficacy and safety have not been established).

With caution
Psoriasis, depression (including history), diabetes mellitus (may mask symptoms of hypoglycemia), allergic reactions (history), bronchospasm (history), desensitization therapy, Prinzmetal's angina, 1st degree AV block, severe renal dysfunction (creatinine clearance (CC) less than 20 ml/min); severe liver dysfunction; thyrotoxicosis, old age.

Use during pregnancy and breastfeeding
Pregnancy
Bisoprolol does not have direct cytotoxic, mutagenic or teratogenic effects, but has pharmacological effects that may have a harmful effect on pregnancy and/or the fetus or newborn. Typically, beta blockers reduce placental perfusion, leading to reduced fetal growth, intrauterine fetal death, miscarriage, or premature birth. The fetus and newborn child may experience pathological reactions, such as intrauterine growth retardation, hypoglycemia, and bradycardia.
Bisoprolol-Teva should not be used during pregnancy; use is possible if the benefit to the mother outweighs the risk of side effects in the fetus and/or child. In the event that treatment with Bisoprolol-Teva is considered necessary, blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child should be monitored, and in the event of adverse events in relation to pregnancy and/or the fetus, alternative methods should be taken therapy. The newborn should be carefully examined after birth. Symptoms of hypoglycemia and bradycardia usually occur during the first 3 days of life.
Breastfeeding period
There is no data on the penetration of bisoprolol into breast milk. Therefore, taking the drug Bisoprolol-Teva is not recommended for women during breastfeeding.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Directions for use and doses
The drug Bisoprolol-Teva is taken orally, in the morning on an empty stomach, 1 time per day with a small amount of liquid, in the morning before, during or after breakfast. The tablets should not be chewed or crushed into powder.
In all cases, the doctor selects the dosage regimen and dose individually for each patient, in particular, taking into account the heart rate and condition of the patient. For arterial hypertension and coronary heart disease, the drug is prescribed 5 mg 1 time per day. If necessary, the dose is increased to 10 mg 1 time per day. In the treatment of arterial hypertension and angina pectoris, the maximum daily dose is 20 mg 1 time / day.
For patients with severely impaired renal function (creatinine clearance less than 20 ml/min.) or with severely impaired liver function, the maximum daily dose is 10 mg 1 time per day. Increasing the dose in such patients must be carried out with extreme caution. No dose adjustment is required in elderly patients.

Side effect
The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification): very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual messages.
From the heart and blood vessels: very often - a decrease in heart rate (bradycardia, especially in patients with CHF); sensation of heartbeat, often - a pronounced decrease in blood pressure (especially in patients with CHF), manifestation of vasospasm (increased peripheral circulatory disorders, a feeling of cold in the extremities (paresthesia); infrequently - impaired AV conduction (up to the development of complete transverse block and cardiac arrest), arrhythmias , orthostatic hypotension, worsening CHF with the development of peripheral edema (swelling of the ankles, feet; shortness of breath), chest pain.
From the nervous system: often - dizziness, headache, asthenia, fatigue, sleep disturbances, depression, anxiety; rarely - confusion or short-term memory loss, nightmares, hallucinations, myasthenia gravis, tremors, muscle cramps. Typically, these phenomena are mild in nature and usually disappear within 1-2 weeks after the start of treatment.
From the senses: rarely - blurred vision, decreased tear production (should be taken into account when wearing contact lenses), tinnitus, hearing loss, ear pain; very rarely - dry and sore eyes, conjunctivitis, taste disturbances.
From the respiratory system: uncommon - bronchospasm in patients with bronchial asthma or obstructive airway diseases; rarely - allergic rhinitis; nasal congestion.
From the digestive system: often - nausea, vomiting, diarrhea, constipation, dry oral mucosa, abdominal pain; rarely - hepatitis, increased activity of liver enzymes (alanine aminotransferase, aspartate aminotransferase), increased bilirubin concentration, change in taste.
From the musculoskeletal system: infrequently - arthralgia, back pain.
From the genitourinary system: very rarely - impaired potency, weakened libido.
Laboratory indicators: rarely - increased concentration of triglycerides in the blood; in some cases - thrombocytopenia, agranulocytosis, leukopenia.
Allergic reactions: rarely - skin itching, rash, urticaria
From the skin: rarely - increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions; very rarely - alopecia; beta-blockers can aggravate the course of psoriasis.
Others:“withdrawal” syndrome (increased frequency of angina attacks, increased blood pressure).

Overdose
Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.
Treatment: If an overdose occurs, first of all you need to stop taking the drug, perform gastric lavage, prescribe adsorbents, and carry out symptomatic therapy.
For severe bradycardia, intravenous atropine is administered. If the effect is insufficient, a drug with a positive chronotropic effect can be administered with caution. Sometimes temporary placement of an artificial pacemaker may be necessary.
With a pronounced decrease in blood pressure - intravenous administration of plasma-substituting solutions and vasopressors.
For hypoglycemia, intravenous glucagon or intravenous dextrose (glucose) may be indicated.
With AV block: patients should be closely monitored and treated with beta-agonists such as epinephrine. If necessary, install an artificial pacemaker.
In case of exacerbation of CHF, intravenous administration of diuretics, drugs with positive inotropic effects, as well as vasodilators. For bronchospasm, prescribe bronchodilators, including beta2-adrenergic agonists and/or aminophylline.

Interaction with other drugs
The effectiveness and tolerability of drugs may be affected by concomitant use of other drugs. This interaction can also occur when two drugs are taken within a short period of time. The doctor must be informed about the use of other medications, even if used without a prescription.
Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.
Class III antiarrhythmic drugs (eg, amiodarone) may worsen AV conduction disturbances.
The effect of beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) may enhance the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate).
Parasympathomimetics, when used simultaneously with bisoprolol, may increase AV conduction disturbances and increase the risk of developing bradycardia. The simultaneous use of Bisoprolol-Teva with beta-agonists (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs.
The combination of bisoprolol with adrenergic agonists that affect beta and alpha adrenergic receptors (for example, norepinephrine, epinephrine) may enhance the vasoconstrictor effects of these drugs that occur with the participation of alpha adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers. Mefloquine, when used simultaneously with bisoprolol, may increase the risk of bradycardia.
Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol. Iodine-containing radiopaque diagnostic agents for intravenous administration increase the risk of developing anaphylactic reactions. Phenytoin, when administered intravenously, and agents for inhalation anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure.
The effectiveness of insulin and hypoglycemic agents for oral administration may change during treatment with bisoprolol (masks the symptoms of developing hypoglycemia: tachycardia, increased blood pressure).
The clearance of lidocaine and xanthines (except theophylline) may be reduced due to a possible increase in their concentration in the blood plasma, especially in patients with an initially increased clearance of theophylline under the influence of smoking. The hypotensive effect is weakened by non-steroidal anti-inflammatory drugs (NSAIDs) (sodium ion retention and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium ion retention). Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of “slow” calcium channels (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol. Tricyclic and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase depression of the central nervous system.
Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. The treatment break between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Ergotamine increases the risk of developing peripheral circulatory disorders. Sulfasalazine increases the concentration of bisoprolol in the blood plasma. Rifampin shortens the half-life of bisoprolol.

Special instructions
Monitoring the condition of patients taking the drug Bisoprolol-Teva should include measuring heart rate and blood pressure, conducting an ECG, and determining blood glucose concentrations in patients with diabetes mellitus (once every 4-5 months). In elderly patients, it is recommended to monitor renal function (once every 4-5 months).
The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.
Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a burdened bronchopulmonary history.
Patients who use contact lenses should take into account that during treatment with the drug, the production of tear fluid may decrease.
When using the drug Bisoprolol-Teva in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if effective blockade of alpha-adrenergic receptors is not previously achieved).
In thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal values.
With simultaneous use of clonidine, its use can be discontinued only a few days after discontinuation of the drug Bisoprolol-Teva. It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history.
If planned surgical treatment is necessary, the drug should be discontinued 48 hours before general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effects.
Reciprocal activation of the vagus nerve can be eliminated by intravenous atropine (1-2 mg).
Drugs that deplete catecholamine stores (including reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia.
Patients with bronchospastic diseases may be prescribed cardioselective beta-blockers with caution in case of intolerance and/or ineffectiveness of other antihypertensive drugs. While taking beta-blockers in patients with concomitant bronchial asthma, airway resistance may increase. If the dose of Bisoprolol-Teva is exceeded in such patients, there is a risk of developing bronchospasm. If increasing bradycardia (heart rate less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure less than 100 mmHg), or AV blockade is detected in patients, it is necessary to reduce the dose or stop treatment. It is recommended to discontinue therapy with Bisoprolol-Teva if depression develops.
Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. The drug is discontinued gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days).
The drug should be discontinued before testing the concentrations of catecholamines, normetanephrine, vanillinmandelic acid, and antinuclear antibody titers in the blood and urine.
Beta blockers are less effective in smokers.
Impact on the ability to drive vehicles and work with equipment that requires increased concentration
The use of the drug Bisoprolol-Teva does not affect the ability to drive vehicles according to the results of a study in patients with coronary artery disease. However, due to individual reactions, the ability to drive vehicles or operate technically complex mechanisms may be impaired. Particular attention should be paid to this at the beginning of treatment, after changing the dose, and also when consuming alcohol at the same time.

Release form
Film-coated tablets 5 mg and 10 mg 10 tablets in a PVC / aluminum blister. 3 or 5 blisters along with instructions for use in a cardboard box.

Storage conditions
At a temperature not exceeding 25° C. Keep out of the reach of children.

Best before date
2 years.
Do not use after the expiration date stated on the package.

Conditions for dispensing from pharmacies
According to the recipe.

Owner ru:
Teva Pharmaceutical Enterprises Ltd., Israel
Manufacturer
Pharmaceutical plant Teva Private Co. Ltd., N-4042, Debrecen, st. Pallagi 13, Hungary
Address for receiving complaints: Russia, Moscow, 119049, st. Shabolovka, 10, Business Center "Concord"

From this medical article you can familiarize yourself with the drug Bisoprolol. The instructions for use will explain at what pressure the medicine can be taken, what it helps with, what are the indications for use, contraindications and side effects. The annotation presents the forms of release of the drug and its composition.

In the article, doctors and consumers can only leave real reviews about Bisoprolol, from which you can find out whether the medicine helped in the treatment of angina pectoris and lowering blood pressure in children and adults. The instructions list analogues of Bisoprolol, prices of the drug in pharmacies, as well as its use during pregnancy.

Bisoprolol is a selective alpha 1-adrenergic receptor blocker that is widely used in cardiological practice. Why do doctors prescribe it? According to the instructions for Bisoprolol, indications for its use are arterial hypertension, heart failure, coronary heart disease, and cardiac arrhythmias.

Release form and composition

Bisoprolol is available in the form of film-coated tablets (10 pieces in blister packs, 1 package in a cardboard box; 30 pieces in polymer or glass jars, 1 jar in a cardboard box). The active substance is bisoprolol fumarate, in 1 tablet - 2.5 mg, 5 mg or 10 mg.

Pharmacological properties

The drug has antiarrhythmic, hypotensive and antianginal (anti-ischemic) effects. It blocks beta1-adrenergic receptors of the heart, reduces heart rate and cardiac output. Bisoprolol reduces the conduction of electrical excitation through the heart, i.e. atrioventricular conduction.

In large doses (more than 0.02 g), the drug has a blocking effect on beta2-adrenergic receptors, mainly in the smooth muscles of blood vessels and bronchi. The maximum effect of the drug develops 1-3 hours after administration and continues throughout the day.

What does Bisoprolol help with?

Indications for use include pathologies such as:

• angina pectoris (coronary heart disease);
• arterial hypertension (persistent increase in blood pressure);
• arrhythmia due to mitral valve prolapse;
• ventricular and supraventricular extrasystole;
• sinus tachycardia (heart rhythm disturbances).

In addition, Bisoprolol is prescribed to patients for the treatment of chronic heart failure as part of complex therapy (together with inhibitors, ACE inhibitors, diuretics, cardiac glycosides).

Instructions for use

Bisoprolol is recommended to be taken in the morning, regardless of meals. The tablets should be swallowed whole, without chewing, with water. The dosage regimen is determined by the attending physician individually for each patient. Use for stable angina and arterial hypertension should begin with 2.5-5 mg per day, followed by an increase to 5-10 mg, not exceeding a daily dose of 20 mg.

In case of chronic heart failure, prescription is possible only for patients who have been in a state of stabilization over the past 6 weeks. During the first week, such patients take 1.25 mg of the drug once a day. For the second week, the drug is prescribed at 2.5 mg per day, for the third week - 3.75 mg, from the fourth to the eighth week - 5 mg, from the eighth to the twelfth week - 7.5 mg, after the twelfth week the daily dose of Bisoprolol is increased up to 10 mg.

In patients with chronic heart failure, after starting to take the drug, blood pressure, conductivity, and heart rate should be checked for normality within the first few hours.

If all indicators are in order, a further increase in the dose is possible; if there are deviations, discontinuation of the drug is necessary. The maximum daily dose of the drug is 20 mg, but patients with severe liver dysfunction and severe renal failure should not take more than 10 mg per day. The drug should be discontinued slowly, reducing the dose gradually.

Side effect

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

Contraindications

According to the instructions, the use of Bisoprolol is contraindicated for diseases such as:

• pronounced sinoatrial block;
• sick sinus syndrome;
• in the later stages of peripheral circulatory disorders;
• with cardiogenic shock;
• severe hypotension;
• atrioventricular block II and III degrees;
• bradycardia with a pulse less than 50 beats/min;
• hypersensitivity to the composition of the drug Bisoprolol, which can cause these tablets to cause adverse reactions;
• tendency to bronchospasms.

In case of drug overdose, bradycardia, arterial hypotension, heart failure, bronchospasm, and slow heart rate may occur.

For children, during pregnancy and lactation

Contraindicated in children under 18 years of age (efficacy and safety have not been established). Use during pregnancy is possible if the benefit to the mother outweighs the risk of side effects in the fetus.

Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia, and possible respiratory distress (neonatal asphyxia) in newborns. If it is necessary to take it during lactation, breastfeeding must be stopped, since Bisoprolol is excreted in breast milk.

Special instructions

Bisoprolol should be taken with caution if you have psoriasis (including indications of a family history of psoriasis), diabetes mellitus in the decompensation phase, or a predisposition to the development of allergic reactions. For pheochromocytoma, taking the drug is possible only after using alpha-blockers.

Before performing operations, the anesthesiologist must be informed about taking the medication. The drug should be taken with caution by patients whose work requires a high concentration of attention and speed of psychomotor reactions.

Interaction

Inadmissible combinations with Bisoprolol:

• Floctafenine;
• Sultopride.

• with antihypertensive drugs that are characterized by a central mechanism of action;
• with calcium antagonists;
• with MAO inhibitors (except for MAO-B inhibitors).
• The drug is prescribed with caution with:
• sympathomimetics;
• Amifostine;
• cardiac glycosides (digitalis preparations);
• anticholinesterase drugs;
• non-steroidal anti-inflammatory drugs;
• antihypertensive drugs that increase the risk of hypotension (for example, tricyclic antidepressants, phenothiazines or barbiturates);
• sympathomimetics, which are characterized by the ability to activate β-adrenergic receptors;
• ergotamine derivatives;
• calcium antagonists, which belong to the group of dihydropyridine derivatives;
• Baclofen;
• anesthetics;
• insulin preparations and oral antidiabetic agents;
• parasympathomimetics;
• local blockers;
• antiarrhythmic drugs of class I and III.

Analogues of the drug Bisoprolol

The same active substance contains analogues:

1. Biol.
2. Corbis.
3. Concor Cor.
4. Tirez.
5. Concor.
6. Biprol.
7. Bisoprolol-Prana (-Lugal, -Ratiopharm, -Teva).
8. Cordinorm.
9. Aritel.
10. Bisomore.
11. Bidop.
12. Niperten.
13. Bioscard.
14. Bisocard.
15. Bisogamma.
16. Aritel Cor.

Analogs have a similar effect:

1. Betak.
2. Nebilet.
3. Betalok.
4. Nebivolol.
5. Breviblock.
6. Lidalok.
7. Atenolol.
8. Serdol.
9. Metoprolol-Acri.
10. Metocard.
11. Nebivator.
12. Vero-Atenolol.
13. Vasocardin.
14. Metozok.
15. Betacard.
16. Cordanum.
17. Lokren.
18. Egilok.
19. Nevotens.

Which is better - Bisoprolol or Concor?

Concor is the brand name under which the original bisoprolol is produced. The manufacturer of the drug is the German pharmaceutical company Merck KGaA. However, the patent for this medicine has long expired, so there are currently a large number of more affordable generic bisoprolol on the market.

It is believed that all of them are not inferior in quality to the original drug, however, there is not enough official data to confirm this today.

Price

In pharmacies, the price of BISOPROLOL, 10 mg tablets (Moscow), is 65 rubles per pack of 30 pieces.

In the fight against the consequences of arterial hypertension, tachycardia, arrhythmia, β-blockers occupy a permanent place among the active “fighters”, this is how the drug is described in the Bisoprolol instructions for use.

An advantageous feature of the drug is its ability to selectively influence β-1-blockers. How is this good for the patient? What are the main advantages of the drug, what is Bisoprolol in more detail: instructions for use, price, reviews, analogues - we will consider all this within the framework of this article.

What forms of release does Bisoprosol have?

The drug is not rich in various forms of release. You can only find Bisoprolol tablets on pharmacy shelves. These are round, white tablets convex on both sides, coated with a thin beige coating. You can purchase 20 tablets or packs of 30 or 50 pieces. The tablets are placed in cellular (blister) packaging.

General characteristics of the drug

A drug that can reduce the myocardium’s need for oxygen, make its rhythm less frequent, and neutralize renin, which is “free floating” in the patient’s bloodstream, this is exactly how the instructions describe Bisoprolol. This is a selective or, as experts also call it, a cardioselective β-adrenergic blocker that temporarily (reversibly) blocks β-1-adrenergic receptors. Selective blockade of these receptors forces the tonometer needle to descend to normal values. This is the answer to the question of what Bisoprolol can be recommended for.

After the discovery of digitalis, the synthesis of β-blocking drugs was considered the greatest discovery in the history of cardiology. This discovery was even awarded a Nobel Prize. Bisoprolol tablets belong to the group of essential drugs for life according to the WHO list.

Understanding what effect can be expected from the medication, it becomes clear why Bisoprolol is prescribed. The main effects that should be expected from the drug are as follows:

• decreased blood pressure;
• normalization of heart rate;
• elimination of signs of cardiac ischemia.

The instructions for use describe bisoprolol as a drug that does not have membrane-stabilizing properties and is not a sympathomimetic (a substance that affects the release of norepinephrine).

In its group of drugs, Bisoprolol is considered the most selective and most effective drug. It is distinguished by high bioavailability and a long elimination period. These undoubtedly positive qualities are inherent in the drug in minimal concentrations, which makes it possible to reduce the frequency of administration to 1 time per day. At least, that’s what the instructions for use for Bisoprolol Prana say.

Contraindications and side effects

Despite the selectivity due to which Bisoprolol Prana or any of its structural analogues can be prescribed to patients with chronic bronchial obstruction, which is not severe, suffering from liver and kidney pathology, atherosclerosis, it cannot be taken by all categories of patients. Bisoprolol instructions for use of the tablet categorically do not recommend that patients:

• with intolerance to bisoprolol or other β-blockers;
• severe asthma and obstruction;
• low blood pressure and a pronounced decrease in heart rate;
• with shock, collapse and pulmonary edema;
• with severe myocardial pathologies (decompensated or acute heart failure, AV block, cardiomegaly, Prinzmetal's angina, cardiac muscle defects, etc.);
• Raynaud's disease;
• metabolic acidosis;
• pheochromocytoma.

Bisoprolol tablets instructions for use do not recommend combined use with MAO inhibitors and class I antiarrhythmic drugs. It is not usually prescribed before the age of 18, because there are no significant studies confirming the safety/danger of this drug. It is very important to understand Bisoprolol instructions for use at what pressure it is prohibited to take. If systolic pressure drops to 100 units or less, this drug should not be taken. It is also important to remember that if the heart rate slows to 60 beats per minute or less, this drug is prohibited.

Bisoprolol tablets instructions for use are described as a medicine that should not be taken without a prescription from a cardiologist, as it can negatively affect the human body. And the list of negative effects expected from taking the medication is quite long:

• sleep disorder, depression, short-term disturbance of consciousness;
• bradycardia, arrhythmia, hypotension, worsening heart failure;
• indigestion, dry mouth, vomiting;
• nasal congestion;
• disturbances in blood sugar and thyroid function;
• violation of the blood formula;
• joint pain;
• decreased libido and potency.

This is not a complete list of possible side effects of the drug, described in Bisoprolol instructions for use of Pran (or any analogue). In addition, its use during pregnancy is extremely undesirable, as it can lead to disruption of the fetal heart, a lack of sugar in its blood and slower growth in the womb. Bradycardia and hypoglycemia can make themselves felt in the first 3 days of the baby’s life after birth. With prolonged use of the drug, there may be a withdrawal syndrome after stopping its use.

The minimum daily dose of the drug is 5 mg, the maximum is 20 mg. The product is taken once a day. The medical niceties that inspire specialists are usually not needed by their patients. Potential buyers of the medicine would like to receive an answer to a simple and short question: What are these tablets for? Bisoprolol? For the drug Bisoprolol, the indications for use are:

1. (stable angina);
2. persistent increase in blood pressure;
3. chronic

No matter in what form this medication Bisoprolol Teva/Lugal/Ratiopharm/Prana is offered in the pharmacy chain, the annotation for it will contain the same data.

Cost of the drug

The original bisoprolol, called Concor, is not the cheapest drug, although its price is not that high. For Concor, the price ranges from 200 to 500 rubles, depending on the dosage of the medication and the number of tablets in the package. The price for Bisoprolol is much lower, it varies from 30 to 160 rubles, depending on the packaging and dosage. For example, for 30 tablets containing 10 mg of active substance, the cost ranges from 35 to 45 rubles. In the range from 30 to 40 rubles for 30 tablets the price for Bisoprolol 5 mg will be about 70 rubles for 50 such tablets.

Having figured out what Bisoprolol helps with, having examined in detail what Bisoprolol is: instructions for use, price of the drug, it remains to understand how this drug can be replaced and how doctors and their patients feel about it.

Bisoprolol - official instructions for use (tablets)

Drugs with similar effects

We can say that for the medication Bisoprologl is an analogue of Concor. But in fact, the opposite is true. That is, Concor is a trademark for a product containing the original bisoprolol. The instructions for Concor are described in the same way as any of the Bisoprolol products on the market are described. There is no documented experimental data confirming the identity of these drugs or the difference between them.

However, if you do not refer to the instructions for use of Bisoprolol, reviews from cardiologists indicate that the original drug or high-quality generics are significantly more effective than cheap analogues. In the case of this drug, the question does not seem so curious: Bisoprolol or Bisoprolol, which is better? The best is the original version or synonyms, which cost from 150 rubles.

This β-blocker has many analogues, both structural and group. Structural analogues for the drug Bisoprolol are:

• Coronar, Corbis, Niperten,
• Bisomor, Bidop, Aritel Kor,
• Bioscard, Bisogamma.

Such drugs as Nebivator, Betalok, Betacard, Egilok, Metoprolol, Estekor and others have a similar mechanism of action.

Video: Arterial hypertension (recommendations of the European Society of Cardiology)

Reviews at a Glance

Many cardiologists highly value this β-blocker; in its group it is considered one of the best drugs that can improve the patient’s quality of life and prolong this very life. Patient reviews of Bisoprolol are mostly positive, but many note side effects from taking this medication. Some patients are even forced to abandon it, despite the pronounced therapeutic effect.

Instructions for medical use

medicine

Bisoprolol

Trade name

Bisoprolol

International nonproprietary name

Bisoprolol

Dosage form

Film-coated tablets 2.5 mg; 5 mg and 10 mg.

Compound

Each tablet contains:

active substance- bisoprolol fumarate - 2.5 mg; 5 mg or 10 mg;

excipients- microcrystalline cellulose, calcium hydrogen phosphate dihydrate, corn starch, colloidal anhydrous silicon dioxide, magnesium stearate, sodium starch glycolate (type A), opadry II (including polyvinyl alcohol, partially hydrolyzed, talc, macrogol 3350, white coloring pigment ( contains titanium dioxide, E 171), pink coloring pigment (contains titanium dioxide, E 171, carmine, E 120, indigo carmine-based aluminum varnish, E 132, black iron oxide, E 172) or blue coloring pigment (contains titanium dioxide , E 171, aluminum varnish based on indigo carmine, E 132, aluminum varnish based on quinoline yellow, E 104).

Description

Film-coated tablets, white - dosage 2.5 mg, blue - dosage 5 mg, pink - dosage 10 mg, with a biconvex surface, scored. On the cross section, two layers are visible - for dosages of 5 mg and 10 mg.

Farmacotherapy group

Beta blockers. Beta-blockers are selective. Bisoprolol.

ATX code C07AB07

Pharmacological properties

Pharmacokinetics

Absorption and distribution. Absorption - 80-90%, food intake does not affect absorption. Cmax in blood plasma is observed after 1-3 hours.

Communication with blood plasma proteins is about 30%. Passes through the BBB and the placental barrier to an insignificant extent, and is excreted in breast milk in small quantities.

Metabolism and excretion. 50% of the dose is metabolized in the liver to form inactive metabolites. T ½ - 10-12 hours. About 98% is excreted in the urine - 50% unchanged, less than 2% - with bile.

Pharmacodynamics

Selective β 1 -blocker. Reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise). It has hypotensive, antiarrhythmic and antianginal effects. Inhibits the conductivity and excitability of the myocardium, reduces atrioventricular conductivity.

In case of arterial hypertension, the effect occurs after 2-5 days, stable effect - after 1-2 months.

Indications for use

• arterial hypertension
• coronary heart disease (angina)

Directions for use and doses

The tablets should be taken with a small amount of liquid, without chewing, in the morning before, during or after breakfast.

Arterial hypertension, coronary heart disease (angina)

The recommended dose is 5 mg (1 tablet of Bisoprolol 5 mg) per day. If necessary, the daily dose can be increased to 10 mg (1 tablet of Bisoprolol 10 mg) per day. Increasing the dose is allowed only in individual cases. The maximum daily dose is 20 mg.

Titration. Treatment with bisoprolol should be started with a gradual increase in dose as follows:

1st week 1.25 mg once daily. If well tolerated, week 2 2.5 mg once daily. If well tolerated, week 3 3.75 mg once daily. If well tolerated, the dose is increased to 5 mg once a day over 4-7 weeks. If well tolerated, the dose is increased to 7.5 mg once daily for the next 4 weeks. If well tolerated, the dose is increased to 10 mg once daily as a continuous maintenance dose.

During the titration phase, careful monitoring of pulse, blood pressure, and signs of worsening cardiac therapy is necessary.

Dose adjustment. If the maximum recommended dose is not well tolerated, a gradual dose reduction should be carried out.

If there is temporary worsening of heart failure, hypotension, or bradycardia, temporary reduction or discontinuation of bisoprololol treatment may be considered. When the patient's condition is stabilized, titration of the dose of bisoprololol is necessary in each case to resume treatment.

Stopping treatment

The dose should be reduced gradually, since sudden withdrawal can lead to a sharp exacerbation of the disease. The dose should be reduced gradually (by 25% per week).

Patients with impaired renal or liver function. For patients with arterial hypertension or coronary heart disease and mild to moderate hepatic or renal dysfunction, dosage adjustment is usually not necessary. For patients with severe renal failure (creatinine clearance less than 20 ml/min) and patients with severe liver failure, the daily dose should not exceed 10 mg of bisoprolol.

Elderly patients. No dose adjustment is required.

Side effects

Often:

Dizziness*, headache*

Nausea, vomiting, diarrhea, constipation

Feeling of cold or numbness in the extremities

Fatigue*

Uncommon:

Bradycardia, atrioventricular conduction disturbances, worsening of existing heart failure

Bronchospasm in patients with bronchial asthma or a history of obstructive respiratory disease

Muscle weakness, muscle spasms

Hypotension

Asthenia

Depression, sleep disorders

Rarely:

Increased triglyceride levels, increased liver enzymes (ALT, AST)

Fainting

Reduced lacrimation (should be considered when the patient wears contact lenses)

Hearing impairment

Allergic rhinitis

Hypersensitivity reactions such as itching, redness, rash

Hepatitis

Potency disorders

Nightmares, hallucinations

Very rarely:

Conjunctivitis

Hair loss. Beta blockers may trigger or worsen psoriasis or cause a psoriasis-type rash.

*These symptoms occur more often at the beginning of treatment. They are usually mild in nature and usually disappear within 1-2 weeks.

Contraindications

• hypersensitivity to bisoprolol or to any of the components of the drug

• acute heart failure or decompensated heart failure that requires intravenous inotropic therapy
• cardiogenic shock
• atrioventricular block II and III degrees (without pacemaker)
• sick sinus syndrome
• sinoatrial block
• symptomatic bradycardia

Symptomatic hypotension

• history of severe forms of bronchial asthma and chronic obstructive pulmonary disease
• late stages of peripheral arterial occlusive disease or Raynaud's disease

Untreated pheochromocytoma

• metabolic acidosis
• children under 18 years of age (efficacy and safety have not been established)
• pregnancy and lactation

With caution

Hypertension or angina with concomitant heart failure

Diabetes with significant fluctuations in blood glucose levels; symptoms of hypoglycemia (eg, tachycardia, rapid heartbeat, or sweating) that may be masked

Strict diet

Ongoing desensitization therapy

First degree AV block

Pritsmetal's angina

Peripheral arterial occlusive disease (complaints may increase, especially at the beginning of therapy)

In patients with a history of psoriasis, beta blockers (eg, bisoprolol) should be prescribed only after a careful benefit/risk assessment.

Drug interactions

Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone). There may be an increased effect on AV conduction time and an increase in negative inotropic effect.

Calcium channel blockers from the verapamil group and, to a lesser extent, from the diltiazem group. Negative effect on contractility and AV conduction. Administration of verapamil to patients receiving beta-blocker therapy may be accompanied by the development of severe arterial hypotension and AV block.

Centrally acting antihypertensives (eg clonidine, methyldopa, moxonidine, rilmenidine). Concomitant use of centrally acting antihypertensive drugs may further reduce the sympathetic tone of the central nervous system and, as a result, reduce heart rate and cardiac output, as well as cause vasodilation. Abrupt cessation of therapy, especially in conditions of prior withdrawal of beta-blockers, may increase the risk of developing a rebound effect (arterial hypertension).

Combinations to use with caution

Dihydropyridine-type calcium channel blockers (eg felodipine and amlodipine). It cannot be excluded that combined use may increase the risk of arterial hypotension and decreased ventricular pumping function in patients with heart failure.

Class III antiarrhythmic drugs (eg amiodarone). There may be an increased effect on AV conduction time.

Parasylpathomimetics. Concomitant use may prolong AV conduction time and increase the risk of bradycardia.

Beta blockers intended for topical use (for example, eye drops for the treatment of glaucoma). Potentiation of the systemic effects of bisoprolol is possible.

Insulin and oral sugar-lowering drugs. Strengthening the hypoglycemic effect. Beta-adrenergic receptor blockade may mask symptoms of hypoglycemia.

Anesthetics. Suppression of reflex tachycardia and increased risk of arterial hypotension.

Foxglove preparations. Increased atrioventricular conduction time, decreased heart rate.

Nonsteroidal anti-inflammatory drugs (NSAIDs). May suppress the hypotensive effects of bisoprolol.

Beta sympathomimetics (eg isoprenaline, dobutamine). Combination with bisoprolol may suppress the effects of both drugs.

Sympathomimetics acting on both beta and alpha adrenergic receptors (for example, norepinephrine, adrenaline). Combination with bisoprolol may enhance the alpha-adrenergic receptor-mediated vasoconstrictor effect of these drugs, which leads to an increase in blood pressure and exacerbation of intermittent claudication. Such an interaction is more likely when using non-selective beta-blockers.

Concomitant use of antihypertensive drugs or other drugs that lower blood pressure (for example, tricyclic antidepressants, barbiturates, phenothiazines) may increase the risk of developing arterial hypotension.

Special instructions

Allergic reactions: As with other beta blockers, bisoprolol may increase both sensitivity to allergens and the severity of anaphylactic reactions. In these cases, adrenaline may not always provide the desired therapeutic effect.

Respiratory system: For bronchial asthma or other chronic obstructive dysfunctions, which may be accompanied by symptoms, concomitant bronchodilator therapy is indicated. In rare cases, airway resistance may increase in patients with asthma, requiring increased doses of β2-sympathomimetics.

General anesthesia: In patients who have received general anesthesia, beta blockers reduce the risk of arrhythmia and myocardial ischemia during induction of anesthesia, intubation and after surgery. It is currently recommended that beta blockers be continued perioperatively. The anesthesiologist should be informed that the patient is taking beta-blockers, since there is a possibility of interaction with other drugs, which can lead to bradyarrhythmia, weakened reflex tachycardia, and a reduced reflex ability to prevent blood loss. If it is necessary to discontinue beta-blocker therapy before surgery, it should be done gradually and be completed approximately 48 hours before anesthesia.

Pheochromocytoma: In patients with pheochromocytoma, bisoprolol should be administered only after blockade of alpha receptors.

Thyrotoxicosis: When treated with bisoprolol, symptoms of thyrotoxicosis may not be detected.

The use of bisoprolol may lead to positive doping test results.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Bisoprolol did not affect the ability to drive a car in a study of patients suffering from coronary artery disease. However, due to individual reactions, the ability to drive a car or work with technically complex mechanisms may be impaired. Particular attention should be paid to this at the beginning of treatment, after changing the dose, and also when consuming alcohol at the same time.

Overdose

Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.

Treatment: gastric lavage and administration of adsorbents; symptomatic therapy: in case of developed AV block - intravenous administration of 1-2 mg of atropine, epinephrine or installation of a temporary pacemaker; for ventricular extrasystole - lidocaine (class IA drugs are not used); when blood pressure decreases, the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema - intravenous plasma-substituting solutions, if ineffective - administration of epinephrine, dopamine, dobutamine; for heart failure - cardiac glycosides, diuretics, glucagon; for convulsions - intravenous diazepam; for bronchospasm, beta-agonists by inhalation . Hypoglycemia: intravenous administration of glucose. Bisoprolol is poorly excreted from the body during dialysis.