Bisoprolol drug names. Beta1-selective adrenergic blocker Bisoprolol: pharmacological characteristics and recommended dosage. Interaction with other drugs

For 1 tablet:

dosage 2.5 mg :

active substance: bisoprolol fumarate 2.5 mg;

Excipients: microcrystalline cellulose 93.5 mg, corn starch 43.7 mg, croscarmellose sodium 2.9 mg, magnesium stearate 1.5 mg, colloidal silicon dioxide 1.4 mg;

shell:film coating (polyvinyl alcohol 1.80 mg, titanium dioxide 1.03 mg, macrogol 0.91 mg, talc 0.67 mg, iron dye yellow oxide 0.09 mg) 4.5 mg;

dosage 5 mg:

active substance: bisoprolol fumarate 5.0 mg;

helpedaTspruce substances: microcrystalline cellulose 91.0 mg, corn starch 43.7 mg, croscarmellose sodium 2.9 mg, magnesium stearate 1.5 mg, colloidal silicon dioxide 1.4 mg;

shell:film coating (polyvinyl alcohol 1.8000 mg, macrogol 0.9090 mg, titanium dioxide 0.8770 mg, talc 0.6660 mg, yellow iron oxide dye 0.2475 mg, black iron oxide dye 0.0005 mg) 4.5 mg;

dosage 10 mg:

active substance: bisoprolol fumarate 10.0 mg;

Excipients: microcrystalline cellulose 150.4 mg, corn starch 73.0 mg, croscarmellose sodium 4.9 mg, magnesium stearate 2.4 mg, colloidal silicon dioxide 2.3 mg;

shell:film coating (polyvinyl alcohol 2.80 mg, titanium dioxide 1.75 mg, macrogol 1.41 mg, talc 1.04 mg) 7.0 mg.

Dosage 2.5 mg: Round biconvex tablets with a score and a chamfer, film-coated from light yellow to yellow. In cross section, the kernel is white to yellowish-white.

Dosage 5 mg: Round biconvex tablets with a score and a chamfer, film-coated from yellow to dark yellow. In cross section, the kernel is white to yellowish-white.

Dosage 10 mg: Round, biconvex, white film-coated tablets. In cross section, the kernel is white to yellowish-white.

Bisoprolol is a selective beta 1-blocker, without its own sympathomimetic activity, and does not have a membrane-stabilizing effect. As with other beta 1-blockers, the mechanism of action in arterial hypertension is unclear. At the same time, it is known that it reduces the activity of renin in the blood plasma, reduces the myocardial oxygen demand, and reduces the heart rate (HR). It has antihypertensive, 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 (Ca 2+), has a negative chrono-, dromo-, bathmo- and inotropic effect, inhibits conductivity and excitability, reduces atrioventricular (AV) conduction.

When the therapeutic dose is exceeded, it has a beta 2-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 beta 2-adrenergic receptors), after 1-3 days it returns to its original value, and with prolonged 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 a decrease in heart rate, a slight decrease in contractility, prolongation of diastole, and improved myocardial perfusion.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through AV node) and along additional paths.

When used in average therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta 2 - 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; the severity of the atherogenic effect does not differ from the effect of propranolol.

Suction . almost completely (> 90%) is absorbed from the gastrointestinal tract. Its bioavailability due to minor metabolism during the “first pass” through the liver (at a level of approximately 10-15%) is approximately 85-90% after oral administration. Food intake does not affect the bioavailability of bisoprolol. exhibits linear kinetics, with its plasma concentrations being proportional to the administered dose over a dose range of 5 to 20 mg. The maximum concentration in blood plasma is achieved after 2-3 hours.

Distribution. distributed quite widely. The volume of distribution is 3.5 l/kg. The binding to plasma proteins reaches approximately 35%; uptake of bisoprolol by blood cells is not observed.

Metabolism. 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 experiments with human liver microsomes in vitro, show that it is metabolized primarily by the CYP 3A 4 isoenzyme (about 95%), and the CYP 2D 6 isoenzyme plays only a small role.

Excretion. The clearance of bisoprolol is determined by the balance between its excretion through the kidneys as unchanged substance (about 50%) and oxidation in the liver (about 50%) to metabolites, which are then also excreted by the kidneys. The total clearance of bisoprolol is 15.6 ± 3.2 l/h, with renal clearance being 9.6 ± 1.6 l/h. The half-life of bisoprolol is 10-12 hours.

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 chronic heart failure (CHF), plasma concentrations of bisoprolol are higher and the half-life is longer compared to healthy volunteers.

Arterial hypertension;

Coronary heart disease: prevention of attacks of stable angina;

Chronic heart failure.

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;

AV blockade II-III degree, without pacemaker;

Sinoatrial block;

Sick sinus syndrome;

Bradycardia (heart rate before treatment less than 60 beats/min);

Severe hypotension (systolic blood pressure less than 100 mmHg)

Cardiomegaly (without signs of heart failure);

Severe forms of bronchial asthma and chronic obstructive pulmonary disease (COPD) in history;

Severe peripheral circulatory disorders;

Raynaud's syndrome;

Metabolic acidosis;

Pheochromocytoma (without simultaneous use of alpha-blockers);

Concomitant use of monoamine oxidase inhibitors (MAO) (except for MAO type B inhibitors);

Age up to 18 years (efficacy and safety have not been established).

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; hyperthyroidism, old age, restrictive cardiomyopathy, congenital heart defects or heart valve disease with severe hemodynamic disturbances, CHF with myocardial infarction within the last 3 months, strict diet.

Pregnancy

Bisoprolol does not have direct cytotoxic, mutagenic or teratogenic effects, but has pharmacological effects that can 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 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 the drug is considered necessary, blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child, and in the event of adverse events in relation to pregnancy and/or the fetus, alternative methods of therapy should be taken. 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 excretion of bisoprolol into breast milk. Therefore, taking the drug is not recommended for women during breastfeeding.

If it is necessary to use the drug during breastfeeding, breastfeeding should be stopped.

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 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.

Monitoring the condition of patients taking the drug should include measuring heart rate and blood pressure, conducting an ECG, and determining the concentration of glucose in the blood 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 60 beats/min.

Patients who use contact lenses should take into account that during treatment with the drug, the production of tear fluid may decrease.

It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from the usual doses of epinephrine (adrenaline) against the background of a burdened allergological 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 effect.

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

Medicines that deplete catecholamine stores (including) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a significant 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 the drug 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 mm Hg), or AV block is detected in patients, it is necessary to reduce the dose or stop treatment.

It is recommended to discontinue drug therapy 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.

The use of the drug 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.

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

10 tablets each in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

100 tablets per polymer blow molded jar made of polypropylene and sealed with a polypropylene lid or polymer jar made of low-density polyethylene and sealed with a lid made from a mixture of high-density polyethylene and low-density polyethylene.

3, 5 or 10 blister packs or 1 polymer jar together with instructions for use are placed in a cardboard pack.

In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

With high blood pressure, the patient must be prescribed medications to lower it. One of the most inexpensive and accessible remedies is Bisoprolol.

Bisoprolol - description and action

Bisoprolol tablets are an antihypertensive drug, widely used in the treatment of hypertension and a number of other diseases of the heart and blood vessels. The drug belongs to the group of selective beta blockers and is available in two dosages:

• 0.005 g (5 mg);
• 0.01 g (10 mg).

The product is produced by various pharmaceutical companies - Teva, Pranapharm, Vertex, Atoll, Severnaya Zvezda and many others. The tablets are very inexpensive - in pharmacies you can find a pack of 30 pieces of 10 mg each for 40-50 rubles.

The composition of the drug is represented by the active substance - bisoprolol fumarate, a number of auxiliary components (magnesium stearate, cellulose, starch, colloidal dioxide).

It is not advisable to split the tablets, as they are film-coated.

Like other beta blockers, the drug has a positive effect on blood vessels in arterial hypertension. Its purpose is to relieve signs of high blood pressure, but the exact mechanism of operation has not yet been established. When taken, bisoprolol reduces the amount and activity of renin in the blood, and this leads to a decrease in the oxygen demand of the heart muscle. The pills also help slow down the heart rate. Thus, three main effects of the drug are achieved:

At the very beginning of taking the medicine, it causes an increase in general vascular resistance. After 1-3 days of use, the indicator returns to the original level, and then decreases even later. When taken regularly, Bisoprolol tablets help against hypertension in 2-5 days, and complete stabilization of blood pressure occurs in 30-60 days.

Indications of the drug and contraindications

The main purpose of the drug is the treatment of arterial hypertension. Since it helps improve the functional state of the heart, it is most often recommended for a combination of hypertension and coronary heart disease (CHD). In complex therapy, the medicine is indicated for:

When taken regularly, the drug serves as a prophylactic against angina attacks; they may not occur for months or years. The medicine is used in monotherapy for primary hypertension, at the initial stage of the disease with a slight to moderate increase in pressure. At more complex stages it is usually recommended in complex therapy. Contraindications to taking the drug are as follows:

Use the drug with caution if you have a history of abnormal reactions to other beta blockers.

Instructions for use

The medication should be taken strictly according to indications. The method is this: take the tablets in the dosage prescribed by the doctor in the morning, before meals (15-30 minutes).

It is also possible to take the drug during breakfast, after breakfast. Take the tablet with a small amount of water. Reception is carried out once a day.

It is forbidden to bite, chew, or grind Bisoprolol tablets into powder.

The dosage is always selected individually; it depends on the severity of the disease, the duration of the disease, the presence of additional pathologies and the cause of hypertension. Heart rate is also taken into account. Typically the order of therapy is as follows:

If kidney function is impaired in a patient with glomerular filtration rate below 20 ml/minute, the maximum amount of Bisoprolol is 10 mg. Increasing the dosage is extremely undesirable, since the elimination of metabolites occurs with the participation of the kidneys.

If the dosage regimen is violated, there is a high probability of overdose. It is manifested by heart rhythm disturbances (blockades, extrasystole). The patient may experience a sharp drop in blood pressure and blood sugar, and there is a risk of seizures, fainting, and bronchospasm. In severe cases, acute heart failure is possible. Treatment is gastric lavage, administration of symptomatic drugs (epinephrine, etc.).

How to stop taking Bisoprolol correctly

The drug Bisoprolol has a specific dosage regimen:

• the first 7 days - 1/4 tablet 5 mg;
• For the next 7 days, the dosage is doubled - 1/2 tablet (2.5 mg of bisoprolol fumarate);
• after 14 days the dosage will be 3/4 tablet;
• then the dose is increased to 1 tablet, which contains 5 mg of the active substance;
• for 5 weeks, take 7.5 mg;
• at week 6, the maximum dosage is prescribed - 10 mg.

This treatment regimen can only be followed if the medication is well tolerated. But in any case, the regimen and dosage should only be determined by a doctor. No matter how long Bisoprolol therapy lasts, you cannot stop taking the medication suddenly. They complete it gradually, just as they started. To do this, you need to reduce the dosage from 10 mg to 1.25 mg. Only during the therapeutic course can you not allow your health to deteriorate. It is necessary to reduce the dosage of the drug within 10-14 days.

If it is necessary to prevent critical conditions involving disturbances in the functioning of the heart, as well as control blood pressure, then take Bisoprolol 1 tablet per day, regardless of meals.

Compared to cheap artificial analogues, the medication does not adversely affect men's health, metabolic processes in the body are not disrupted and rarely leads to the development of side effects. But the following symptoms may still develop: headache, depression, ECG changes, drowsiness or insomnia, dizziness, blurred vision or hearing, dry conjunctiva. If it was not possible to avoid them, then you need to urgently call an ambulance. While the doctors arrive, you need to rinse your stomach and drink activated charcoal to cleanse your internal organs.

Side effects - what to worry about?

The most common side effects relate to changes in heart rate and are observed at the initial stage of therapy. Subsequently, the condition stabilizes. People with heart failure experience bradycardia - a slow heartbeat. This same category of patients often experiences a strong decrease in pressure, vasospasm, atrioventricular conduction disturbances, and edema.

In severe cases, transverse blockade with asystole was recorded.

During treatment, sensations of “goosebumps” and coldness may appear in the legs and hands. Sometimes there is chest pain and shortness of breath. Side effects from the nervous system are dizziness, sleep disturbances, depression, drowsiness, tremor.

Almost all of these symptoms disappear on their own within 14 days from the start of treatment. Visual impairment, dry eyes, conjunctivitis, and hearing loss were recorded less frequently.

Bisoprolol analogues and substitutes

Analogues of Bisoprolol include drugs - beta-blockers. Their action is based on the neutralization of receptors of the heart and blood vessels that are sensitive to adrenaline and norepinephrine. The first of this pharmaceutical group was an original patented medicine containing the active substance bisoprolol (manufactured by Merc, Germany). Generics of Concor are Bidop, Niperten, Bisoprolol Teva, Aritel, Bisogamma, Biol, Cordinorm Cor and other drugs containing bisoprolol.

Other beta blockers - analogues of Bisoprolol:

Bisoprolol substitutes - calcium antagonists

Substitutes are drugs that give a similar result, but have a different principle of action. These include slow calcium channel blockers (SCBCs), or calcium antagonists. The principle of action is to block the channels through which calcium ions pass into the cells, causing spasm of the vascular wall. By dilating coronary vessels, calcium antagonists improve nutrition of the heart muscle. The result of using BMCC is a decrease in blood pressure, a decrease in cardiac output and myocardial oxygen demand.

The most popular BMCC preparations:

ACE inhibitor drugs

Another group of antihypertensive drugs - substitutes for Bisoprolol - angiotensin-converting enzyme inhibitors. The hypotensive effect is achieved by suppressing the synthesis of the enzyme angiotensin II, which causes vasospasm. ACE inhibitors have the same cumulative effect as beta blockers and are prescribed for continuous use.

A special group of ACE inhibitors are sartans. These are improved modern drugs that have a minimum of contraindications and side effects compared to other antihypertensive drugs. Sartans do not have a negative effect on cardiac activity.

The most popular drugs in this group:

It is important to know

During therapy, it is important to regularly measure blood pressure. At the beginning of the course, it is important to conduct an ECG at least once every 3 months. Patients with diabetes need to measure the concentration of sugar in peripheral blood daily and take urine tests every 3-4 months to monitor kidney function. You should also regularly measure your heart rate; if it drops below 50 beats per minute, consult a doctor immediately.

In patients with bronchial asthma, dynamic monitoring of the respiratory system is performed. During therapy, there may be a decrease in the production of tear fluid, which must be taken into account when wearing contact lenses.

Bisoprolol acts specifically against conditions such as tachycardia and cardiac muscle contraction disorders. If these ailments are accompanied by hypertension, then the drug actively lowers blood pressure, influencing the normalization of the patient’s well-being.

The drug is part of the spectrum of selective beta blockers. Such components have a very good effect on the cardiovascular and circulatory systems. The medicine is produced using high-tech equipment that meets all quality standards. The drug itself has long established itself in the best positions. The medication has contraindications. It is worth considering them carefully, taking into account the optimal dosage and recommendations of the treating doctor.

Release form

The heart medicine is produced in the form of coated tablets. Each pill is placed in blisters. There are 10 pills in a strip. There are 5, 3 or 2 blisters in a cardboard box. The dragees are round and yellowish in color. The inside of the tablets is cream-colored.

Each tablet contains 2.5; 5 or 10 mg of active substance. Bisoprolol manufacturers use corn starch, specialized cellulose, macrogol 3350, etc. as additional ingredients. The shell of each pill contains talc, dyes, and polyvinyl alcohol.

pharmachologic effect

Blockade of beta1-adrenergic receptors, and of a selective type, leads to an improvement in the patient’s condition. So the drug affects the functioning of the cardiovascular system as a whole.

According to the laws of physiology, beta1-adrenergic receptors receive impulses from the central nervous system. If there are disturbances in this process, the heart begins to work unstably, heartbeat disturbances appear, proper blood pumping becomes difficult, and blood pressure rises. When the drug acts on the impulses of the central nervous system, the heart rate decreases, blood pressure drops and, as a result, a person’s well-being improves.

Bisoprolol is an antihypertensive agent. Doctors classify its effect as one that confidently lowers blood pressure. Tablets are prescribed for the complex treatment of a huge range of ailments.

The action of the drug is aimed at eliminating the causes of ischemia and alleviating its symptoms. At the same time, the heart rhythm returns to normal. The obvious anti-ischemic effect is explained by the ability of the drug to reduce the heart rate and, as a consequence, myocardial contractility. Improving blood flow contributes to the delivery of more oxygen to the heart tissue and this, in turn, has a very beneficial effect on the functioning of the vascular and cardiac systems.

In addition, under the influence of Bisoprolol, cardiac output decreases. Tachycardia is stopped, which is due to the antiarrhythmic effect.

Beta blockers

Once in the body, the drug begins to act actively after complete absorption in the gastrointestinal tract. In this case, it takes from 1 to 3 hours. It is during this period that the greatest clinical effect occurs. It lasts quite a long time.

Instructions for use

Among the indications that cause the use of medicine are pathologies and hereditary diseases, as well as ailments acquired during life under the influence of harmful environmental factors. Doctors prescribe Bisoprolol Prana and Bisoprolol Teva in the following cases:

1. Acute ischemia.
2. Arrhythmia.
3. Tachycardia.
4. Hypertension.

Cardiologists often prescribe the drug to heart patients diagnosed with CHF (chronic heart failure). The drug becomes the main one among other drugs that specifically act on the causes and consequences of diseases of the heart and blood vessels.

Contraindications

Doctors and manufacturers of the drug have identified conditions for which the use of the medicine is strictly prohibited. However, doctors recommend taking the drug, but under the strict supervision of cardiologists. However, if the prescription of this medication leads to a sharp deterioration in the functioning of organs and systems, the prescription of the medication is not justified. Cardiologists' approach is individual. And yet, the following ailments are among the contraindications:

1. Lung diseases.
2. Severe asthma.
3. Hypotension or severe changes in blood pressure.
4. Circulatory disorders.
5. Raynaud's syndrome.
6. Bradycardia.
7. Deficiency at a stage requiring inotropic therapy.
8. A pathology in which the heart increases in size.
9. Complication of myocardial infarction.
10. Disruption of atrioventricular conduction of electrical impulses from the atria to the ventricles, which often leads to severe arrhythmia and hemodynamics.
11. Impaired formation or strength of impulse in the sinus node.

Bisoprolol cannot be taken with such drugs, like Sultopride and Floctafenine. Doctors do not recommend simultaneous administration of this medication.

Effective and safe use in heart patients under the age of 10-15 years has not been proven. No studies of the drug have been conducted on minors.

You should not take MAO inhibitors with this medication. If the patient has lactose rejection or has genetic disturbances in the absorption of monosaccharides in the gastrointestinal tract, Bisoprolol is contraindicated. It should also not be used when the patient has severe sensitivity to the active substance or auxiliary components.

Regarding the use of this medicine, you should additionally consult with a specialist. Among them are an allergist and a nutritionist. This should be done if the patient is prescribed antihistamines or is on a strict diet.

Bisoprolol Alkaloid are not prescribed to patients diagnosed with a hormonally active tumor located in the adrenal glands, even though the tumor is benign.

Another condition in which the drug is contraindicated is a slow process of removing acids or an increased level of bicarbonates in the body.

During pregnancy and lactation

Doctors do not recommend the use of medication for women carrying or breastfeeding children. But there are cases when prescribing the drug is justified. The doctor may prescribe Bisoprolol during pregnancy in situations where the benefit for the expectant or existing mother outweighs the possible harm or the likelihood of adverse reactions.

In addition, if there is a need for urgent treatment with Bisoprolol for nursing mothers, doctors consider the possibility of transferring newborns to artificial nutrition and abandoning breastfeeding in favor of women's health.

Alcohol compatibility

Since the effect of the drug is associated with an effect on the central nervous system, the use of alcohol, even weak and in small quantities, is prohibited during the treatment period. This will lead to depression of the nervous system. Mental disorders, depressive states, and psychoses are also likely. That's why Bisoprolol and alcohol are incompatible.

Dosage

More often, at the beginning of the use of therapeutic measures, doctors prescribe small doses of the drug. This is up to 5 mg. Later, the patient can use 10 mg. The total amount of the drug should not exceed 20 mg per 24 hours.

Most desirable take Bisoprolol in the morning. You can take the tablet on an empty stomach. It is not contraindicated to do this while eating. The pill is swallowed whole. It's important to wash it down. It is strictly forbidden to take the tablet with juice, mineral water, milk, kefir, tea, coffee. This inactivates the active substance and can affect the occurrence of adverse reactions.

The cardiologist prescribes the dosage individually. Dosage regimens for certain heart diseases vary. So, for CHF, heart patients are recommended to take up to 1.25 mg. Increase the dose by another 1 mg in the second week of treatment. The same amount occurs in the 3rd week of taking the drug. From the 4th to the 8th seven days, doctors prescribe up to 5 mg and 10 mg from the 8th to 12th weeks.

For heart patients who have just started taking the drug, it is important to constantly measure blood pressure and pulse. It is advisable to undergo an ECG again. An increase in the amount of mg of the drug per day can only take place when all health indicators are normal.

In case of deviations in the functioning of systems and organs, use should be canceled immediately. If a patient suffers from ailments of the urinary system, he is recommended to drink at least 10 mg per day.

The treatment regimen outlined above is established. However, regarding the dosage, it is worth consulting with the treating cardiologist on an individual basis. Doctors often do not adhere to the dosages accepted and recommended by the scientific medical world, and in their prescriptions they are guided only by important indicators of the patient’s health status.

Exceeding doses is undesirable. This is allowed in extreme cases and only if such a measure is justified. Medication treatment is long-term. It is not advisable to use it in large doses.

Overdose

If the patient intentionally or accidentally exceeds the recommended doses of Bisoprolol, arrhythmia and a sharp decrease in heart rate may occur. These conditions are caused by the appearance of difficulty breathing and the development of heart failure.

When an overdose of Bisoprolol occurs, urgent gastric lavage is necessary. The patient should be given a drip for intoxication effects on the body. Symptoms characteristic of exceeding doses of Bisoprolol:

1. Slowing heart rate.
2. Heart rhythm disturbance, characterized by the appearance of new impulses.
3. Simple arrhythmia.
4. Disturbance in the conduction of electrical impulses from the atria to the ventricles.
5. A sharp drop in pressure.
6. Blueness of fingers on all extremities.
7. Labored breathing.
8. Dizziness.

An overdose of Bisoprolol requires hospitalization of the patient in the cardiology department for a number of procedures. In cases where pulmonary edema is not diagnosed, several droppers are given until the desired effect occurs and the condition is alleviated. For seizures, doctors prescribe Diazepam.

Analogs and prices

There are many remedies identical in the type of action of Bisoprolol. Among the main ones: Biprol, Niperten and Coronal. They contain the same active substance as the main component of Bisoprolol.

Pharmacists have also created other analogues: Cor, Tirez, Aritel, Corbis, Bidop, as well as Betak, Lidalok, Metozok, Vero-Atenolol, Vazocardin, Lokren, Egilok, Serdol.

Cost of Bisoprolol in different cities of Russia varies within 40-70 rub. for a monthly course with a dosage of 10 mg. The highest price is in the capital. There, pharmacists will ask for up to 20-25 rubles for 10 tablets. This is about a hundred rubles for 50 pieces.

Table of current prices for the drug Bisoprolol in online pharmacies. The last data update was 10/21/2019 00:00.

Name:

Bisoprolol

Pharmacological
action:

Selective beta1-blocker without intrinsic sympathomimetic activity, does not have membrane stabilizing activity.
Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise) and cardiac output, while stroke volume does not decrease significantly. Inhibits AV conduction. Has antianginal and hypotensive effects.
In high doses (200 mg or more) it can cause blockade of β2-adrenergic receptors, mainly in the bronchi and vascular smooth muscles.

Hypotensive effect of connection n with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (more important for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and an effect on the central nervous system.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and decreased contractility, prolongation of diastole, and improved myocardial perfusion.
Antiarrhythmic effect caused by the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the AV -node) and along additional paths.

Pharmacokinetics
Absorption - 80-90%, food intake does not affect absorption.
Cmax in blood plasma is achieved after 2-4 hours. Plasma protein binding is 26-33%. Bisoprolol penetrates to a small extent through the BBB and the placental barrier; excreted in breast milk.
Metabolized in the liver.
T1/2 - 9-12 hours. Excreted by the kidneys - 50% unchanged, less than 2% - with bile.

Indications for
application:

Arterial hypertension;
- prevention of angina attacks;
- chronic heart failure.

Mode of application:

The dose is selected individually.
The average dose of the drug is 0.005-0.01 g.
The drug is taken once a day, usually in the morning on an empty stomach or during breakfast. The tablet should be swallowed whole with liquid.
With a slight increase in blood pressure, the initial dose of the drug may be 0.0025 g/day.
Exceeding the average daily dose of the drug is allowed only in exceptional cases.
The drug is usually prescribed for a long time.
In patients with impaired renal function and severe liver dysfunction, the daily dose of the drug should not exceed 0.01 g.

Side effects:

From the central nervous system and peripheral nervous system: weakness, fatigue, dizziness, headache, sleep disorders, mental disorders (depression, rarely hallucinations), feeling of cold and paresthesia in the extremities.
From the cardiovascular system: orthostatic hypotension, bradycardia, impaired AV conduction, the appearance of symptoms of heart failure, worsening intermittent claudication and the main clinical symptoms of Raynaud's syndrome.
From the side of the organ of vision: decreased secretion of tear fluid, conjunctivitis.
From the digestive system: diarrhea, constipation, nausea, abdominal pain.
From the musculoskeletal system: muscle weakness, muscle cramps.
Dermatological reactions: skin itching; in some cases - increased manifestations of psoriasis, the appearance of psoriasis-like rashes.
From the respiratory system: Predisposed patients may experience symptoms of bronchial obstruction.
Others: sweating, hot flashes, impaired potency, decreased glucose tolerance in patients with diabetes, allergic reactions.

Contraindications:

Acute heart failure;
- chronic heart failure in the stage of decompensation, cardiogenic shock, collapse, AV blockade of II and III degrees (without a pacemaker), CVS;
- sinoatrial blockade, severe bradycardia (HR<50 уд./мин);
- Prinzmetal's angina;
- pronounced decrease in blood pressure (systolic blood pressure<90 мм рт.ст.);
- history of severe forms of bronchial asthma and COPD;
- late stages of peripheral circulatory disorders;
- Raynaud's disease;
- pheochromocytoma (without simultaneous use of alpha-blockers);
- metabolic acidosis;
- simultaneous use of MAO inhibitors (except for MAO type B inhibitors);
- children and adolescents up to 18 years of age;
- increased sensitivity to bisoprolol and other beta-blockers.

Use during pregnancy and lactation is not recommended

Use with caution with psoriasis and with indications of psoriasis in a family history, diabetes mellitus in the decompensation phase, with a predisposition to allergic reactions.
In case of pheochromocytoma, the use of bisoprolol is possible only after taking alpha-blockers.
Avoid sudden withdrawal of bisoprolol, the course of treatment should be completed slowly with a gradual reduction in dose.
Before surgery, the anesthesiologist should be informed about treatment with bisoprolol.
Bisoprolol at a dose of more than 10 mg/day should be used only in exceptional cases.
This dose should not be exceeded in case of renal failure (creatinine clearance less than 20 ml/min) and severe liver dysfunction.
During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery
Use with caution in patients whose activities require concentration and high speed of psychomotor reactions.

Interaction
other medicinal
by other means:

Bisoprolol should not be used concomitantly with floctafenine, since beta-adrenergic blockers may interfere with the compensatory cardiovascular responses associated with floctafenine-induced hypotension or shock.
Bisoprolol should not be used simultaneously with sultopride, since it may the risk of ventricular arrhythmia increases.

With the simultaneous use of nifedipine and other calcium channel blockers (dihydropyridine derivatives), the hypotensive effect of bisoprolol may be enhanced.
When used simultaneously with antiarrhythmic drugs (phenytoin, disopyramide, lidocaine, flecainide, amiodarone), conduction disturbances and a negative inotropic effect may occur.
When used concomitantly with parasympathomimetic drugs, AV conduction time may increase and the risk of bradycardia may increase.
With the simultaneous use of bisoprolol and local β-adrenergic receptor blockers (for example, those contained in eye drops for the treatment of glaucoma), the effect of bisoprolol may be enhanced.
When used concomitantly with insulin and oral antidiabetic drugs A hypoglycemic effect may occur.
When used simultaneously with beta-adrenergic blockers, symptoms of hypoglycemia may be hidden.

When used simultaneously with drugs for anesthesia, the risk of arrhythmias and myocardial ischemia may increase.
Simultaneous use with cardiac glycosides (digitalis preparations) can lead to a decrease in heart rate and impaired AV conduction.
When used simultaneously with NSAIDs, the hypotensive effect of bisoprolol is reduced.
When used simultaneously with β-sympathomimetics (dobutamine, orciprenaline), the effect of both drugs is reduced.
Sympathomimetics that activate α- and β-adrenergic receptors (epinephrine, norepinephrine), increase blood pressure and intensify the symptoms of intermittent claudication.
Tricyclic antidepressants, barbiturates, and phenothiazines enhance the hypotensive effect.
When used simultaneously with MAO inhibitors (except for MAO type B inhibitors), the hypotensive effect of β-adrenergic receptor blockers increases.

Calcium channel blockers (verapamil, diltiazem) and antihypertensive drugs (clonidine, methyldopa, moxonidine, reserpine) should not be used simultaneously during bisoprolol therapy. This can lead to the development or worsening of bradycardia, AV block, heart failure, and decreased blood pressure.
When combined with mefloquine, the risk of developing bradycardia increases.
When used simultaneously with ergotamine derivatives peripheral perfusion disturbances increase.
When combined with rifampicin, a slight decrease in the half-life of bisoprolol is possible. There is usually no need for dose adjustment.

Pregnancy:

Use during pregnancy and lactation Not recommended and perhaps in the case where the expected benefit to the mother outweighs the potential risk of side effects in the fetus and child.
In exceptional cases of use during pregnancy, bisoprolol should be discontinued 72 hours before the expected due date due to the possibility of bradycardia, arterial hypotension, hypoglycemia and respiratory depression in the newborn. If discontinuation is not possible, then the condition of the newborn must be carefully monitored for 72 hours after birth.
If it is necessary to use bisoprolol during lactation, breastfeeding should be stopped.

Overdose:

Symptoms: bradycardia, arterial hypotension, bronchospasm, acute heart failure, hypoglycemia.
Treatment: Stop taking the drug and consult a doctor. Depending on the degree of overdose, supportive and symptomatic therapy is carried out. There is evidence that bisoprolol is difficult to dialyze.
For bradycardia: intravenous administration of atropine. In case of bradycardia that does not respond to treatment, isoprenaline or other drugs with a positive chronotropic effect can be used with caution, and, if necessary, cardiac pacing.
For arterial hypotension: taking vasoconstrictor drugs, intravenous administration of glucagon.
For II and III degree AV block: careful monitoring of patients is required during isoprenaline infusion; If necessary, pacemaker is used.
For exacerbation of CHF: intravenous administration of diuretics, vasodilators and vasoconstrictors.
For bronchospasm: bronchodilators (eg isoprenaline), β2-adrenergic blockers and/or aminophylline.
For hypoglycemia: intravenous administration of glucose.

Release form:

Bisoprolol tablets, coated, 2.5 mg, 5 mg and 10 mg in packages of 10-10,000 pieces.
Bisoprolol-OVL tablets, coated, 2.5 mg, 5 mg and 10 mg in packages of 10-300 pieces.
Bisoprolol-LEKSVM tablets, coated, 5 mg and 10 mg in packages of 20-100 pieces.

Bisoprolol-Lugal tablets, coated, 5 mg and 10 mg in packages of 10-50 pieces.
Bisoprolol-Prana tablets, coated, 5 mg and 10 mg in packages of 10-100 pieces.
Bisoprolol-Ratiopharm tablets, coated, 5 mg and 10 mg in packages of 30-100 pieces.
Bisoprolol-Teva tablets, coated, 5 mg and 10 mg in packages of 30-50 pieces.

Storage conditions:

Store in a dry place, protected from light, out of reach of children, at a temperature not exceeding 20 °C.

1 tablet of Bisoprolol contains:
- active substance: bisoprolol fumarate - 5 mg;
- Excipients: croscarmellose sodium (primellose), povidone (medium molecular weight polyvinylpyrrolidone), pregelatinized starch (starch 1500), colloidal silicon dioxide (aerosil), talc, microcrystalline cellulose, lactose (milk sugar), magnesium stearate.

Instructions for use will tell you about the drug Bisoprolol. But the official annotation does not always provide answers. for all questions that occur in hypertensive patients. In this article we will consider not only the key points, but also those that concern the buyer: price, reviews, analogues.

pharmachologic effect

Antihypertensive tablets Bisoprolol, in Latin Bisoprolol, are a beta1-blocker, which determines their pharmacology.

The drug is aimed at eliminating the symptoms of myocardial ischemia and lowering blood pressure levels. Also, the medicine Bisoprolol normalizes the heart rate.

Pharmacodynamics and pharmacokinetics

The drug Bisoprolol not characterized sympathomimetic and membrane-stabilizing properties. Its pharmacokinetics and pharmacodynamics depends on active substance.

Small doses of the main element help weaken renin activity, which responsible for regulation Blood pressure and water-salt ratio. The myocardium uses less oxygen, and its conductivity and excitability decrease.

Antihypertensive tablets Bisoprolol have a positive effect on heart rate, reducing the amount contractions both during physical activity and at rest.

Under their influence, the stimulation of catecholamine decreases, as does the formation of adenosine monophosphate based on adenosine triphosphate cyclical nature.

The influence of the drug Bisoprolol extends to to calcium ions inside cells, reducing their current. There is a decrease in blood pressure, and the symptoms of myocardial ischemia blocked. Use of antihypertensive tablets Bisoprolol ensures oppression atrioventicular conduction and cardiac output.

High dose drug manifests itself, as a beta blocker. For this reason he can cause blockingβ2-adrenergic receptors, which are located in the bronchi and smooth vascular muscles. For achievement such an effect you need a dose of antihypertensive tablets Bisoprolol from 0.2 g.

Absorption of the drug occurs no more than 90%. The absorption process has nothing to do with whether the antihypertensive pill was taken: before or after meals. For the maximum amount of active substance in the blood, it takes from 1 hour to 3 hours.

Bisoprolol fumarate binds to plasma proteins only 30%. This substance crosses the placenta and may fall into breast milk.

Basal Metabolism occurs in the liver and is excreted through urination.

Composition and release form

The drug Bisoprolol is produced in tablets that are coated with a yellow coating.

The accumulation of the active substance has three options: 2.5 mg, 5 mg and 10 mg.

Photos of the drug depending on the dosage:

These tablets contain a number of inactive components in the form:

1. Magnesium stearate.
2. Colloidal silicon dioxide.
3. Crospovidone.
4. Alcohol-Polyvinyl.
5. Titanium dioxide.
6. Talc.
7. Macrogol.
8. Corn starch.
9. Dye.

The drug Bisoprolol is packaged in 2, 3, 5 strips of 10 tablets in cardboard packages.

Their release does several pharmaceutical companies domestic and foreign:

• "Lugansk Chemical Plant", "Health" (Ukraine).
• "Teva" (Israel).
• "PranaPharm", "Northern Star", "Rompharma", "Biocom", "Vertex", "Atoll" (RF).
• Sandoz, Merkle GmbH for Ratiopharm GmbH (Germany).

Indications for use

What are antihypertensive tablets Bisoprolol used for? They are most effective against:

1. Hypertension, when increased blood pressure has systematic nature.
2. Angina pectoris.
3. Chronic heart failure as part of complex therapy.

Photo gallery of states:

Angina pectoris

Heart failure

Hypertension

Useful video:

At what pressure should I take the medicine?

Very often, hypertensive patients themselves prescribe the drug Bisoprolol, but at what pressure they do not know to take it, but there may be consequences the most unpleasant.

It is recommended to start drinking antihypertensive medications based on bisoprolol when the tonometer readings are 140 or higher.

So after the Bisoprolol tablet, blood pressure will not drop sharply and hypotension will not begin, which also has an unpleasant symptoms.

During pregnancy and breastfeeding

The abstract for the drug Bisoprolol states that it contraindicated for women who are pregnant or breastfeeding. This is due to the fact that the active substance penetrates both through the placenta and into breast milk.

In some, especially difficult situations, when antihypertensive tablets Bisoprolol are vital for the mother, they are prescribed.

If the woman is pregnant, therapy should be stopped three days before giving birth.

If this is not done, the baby may be born with diseases:

• Hypotension.
• Bradycardia.
• Hypoglycemia.
• Hypoxia.

Photos of diseases:

When such a scheme is not possible, the born child must be under constant supervision 7 days of life.

Breastfeeding woman should stop feeding if necessary to use the drug Bisoprolol.

Contraindications

• Intolerance.
• Aggravation heart failure and at the stage of decompensation.
• Shock.
• Disturbed functioning of the sinus node.
• Pulmonary swelling.
• Sinoatrial blockades.
• Bronchial asthma.
• Metabolic acidosis.
• Bradycardia.
• Pheochromocytomas.
• AV block.
• Hypolactasia.
• Arterial hypotension.
• Violation peripheral blood circulation.
• History of COPD.
• a lack of potassium and sodium.
• Overabundance calcium.
• Lactose intolerance.

Contraindications include psoriasis.

Almost all diabetics suffer from hypertension, which is why many patients are interested in whether the drug can be taken for diabetes mellitus.

Severe diabetes with complications and inability to control is an absolute limitation.

Antihypertensive tablets Bisoprolol should not be taken during pregnancy.

Adverse reactions

Indications for the drug Bisoprolol allow it to be used by all hypertensive patients. However, from the development of side effects no one is insured.

special instructions

Official description of the drug Bisoprolol warns that patients under 18 years of age should not use it.

Carefully Should people take Bisoprolol blood pressure pills? with possible allergies to components.

The mechanism of action of the drug Bisoprolol is such that it does not involve abrupt cessation of administration. This needs to be done gradually.

Impact on the ability to drive vehicles

Effect of antihypertensive tablets Bisoprolol on the body negative in that case if a hypertensive person drives a vehicle or engages in activities that requires an adequate response psychomotor skills.

Instructions for use

Why the drug Bisoprolol is prescribed was mentioned earlier. Experienced hypertensive patients usually know how to take antihypertensive pills, so as not to harm.

Overdose

Bisoprolol poisoning is a dangerous condition. It manifests itself with symptoms as:

• Ventricular extrasystole.
• Convulsive syndrome.
• Bradycardia.
• Blueness of fingers and palms.
• AV block.
• Bronchospasm.
• Arrhythmias.
• Syncope.
• Difficulty breathing.
• Severe decrease in blood pressure.
• Dizziness.

Withdraw from an overdose Antihypertensive tablets Bisoprolol are helped by the following drugs:

1. Adsorbents.
2. Atropine/epinephrine into a vein.
3. Lidocaine into a vein.
4. Plasma replacement solutions intravenously.
5. Dopamine.
6. Dobutamine.
7. Cardiac glycosides.
8. Diuretics.
9. Glucagon.
10. Diazepam.
11. Beta-agonists.

The choice of medications depends on the symptoms and complications that arise from bisoprolol poisoning.

Drug interactions

Taking the drug Bisoprolol with other medications may cause serious harm, if you don't know the rules their compatibility.

Bisoprolol and alcohol

The drug Bisoprolol and alcohol, the compatibility of which is zero, cannot be used simultaneously. The point is that they can develop serious adverse reactions or poisoning.

Price for the drug

How much the drug Bisoprolol costs depends on the number of antihypertensive tablets in the pack and the dosage.

The cheapest option is domestic manufacturers. Usually the cost of their products does not exceed 70 rubles. Imported medicine will cost more than 120 rubles.

Conditions for dispensing from pharmacies

In order to buy the drug Bisoprolol, a doctor must write a prescription.

It includes items about who prescribes to whom, as well as “Rp.: Tab. Bisoprololi 0.005 No. 20 D.S. 1 tab. per day (AH, IHD).”

Analogues substitutes

The drug Bisoprolol helps against hypertension well, but no worse analogues cope with high blood pressure:

• Lokren is created on the basis of betaxolol in the form of tablets. Manufacturer: Sanofi-Winthrop Industrie (France).
• Concor Available in tablet form with bisoprolol. Manufacturer: Merck KGaA (Germany).
• Niperten is produced in tablets based on bisoprolol. Manufacturer: KRKA-Rus (RF).
• Bidop produced with bisoprolol in tablet form. Manufacturer: Gedeon Richter (Hungary).
• Egilok is created on the basis of metoprolol tartrate in tablets. Manufacturer: Egis (Hungary).
• Indapamide is made on the basis of indapamide in the form of tablets. Manufacturer: Valenta Pharmaceuticals and PRANAFARM (Russian Federation), Hemofarm (Serbia and Chornogro), Stada Arzneimittel (Germany), Teva (Israel), Tianjin Pacific Chemical & Pharmaceutical Co. Ltd (China).

Photos of analogues:

Lokren

Concor

Niperten

Bidop

Egilok

Indapamide

There are many other substitutes based on bisoprolol and other active ingredients that have a reliable hypotensive effect.