Beta-blockers (β-adrenergic receptors). Adrenoblockers - what is it? Cardioselective adrenoblockers modern drugs

High blood pressure is one of the cardiovascular risk parameters. Therefore, according to the latest recommendations, the tasks drug therapy hypertension it is considered not only to achieve its reduction and sustainable control, but also to prevent heart attack, stroke and lethal outcome.

Today, a subgroup of antihypertensive drugs consists of drugs that affect the occurrence of complications in different ways. It includes: diuretic pharmaceutical drugs, ACE inhibitors, beta-blockers, calcium antagonists and angiotensin receptor blockers.

Some studies indicate that long-term treatment beta-blockers (BAB) cause negative metabolic effects, which significantly increase the risk of complications, especially in patients with ischemic disease hearts. Others testify to their high efficiency for recent heart attacks on the background of heart failure. Nevertheless, BAB continues to confidently occupy the third place in the list of antihypertensive drugs.

Let's try to figure out in which cases their intake will be safe, and, possibly, will bring additional benefits, and who should drink BAB, albeit latest generation, Not recommended.

In the outer membrane of cells human body there are special proteins that recognize and respond appropriately to hormonal substances - adrenaline and norepinephrine. That is why they are called adrenergic receptors.

In total, two alpha and three varieties of beta (β) adrenergic receptors have been identified. The division is based on their different sensitivity to medicinal substances- adreno-stimulants and adreno-blockers.

Since the topic of our article is BAB, we will consider how the functioning of body systems is affected by stimulation of β-receptors. Under the influence of the adrenaline hormone and substances similar to it, they, in addition to increasing the release of renin in the kidneys, perform different functions.

The mechanism of action of beta blockers fully justifies their name.

By blocking the action of β-adrenergic receptors, and protecting the heart from the adrenaline hormone, they contribute to:

improving the performance of the myocardium - it contracts and unclenches less often, the force of contractions becomes less, and the rhythm is more uniform;
braking pathological changes in the tissues of the left ventricle.

The main cardioprotective (protecting the heart) effects of the first BBs for which they were valued were a reduction in the frequency of attacks of "angina pectoris" and a decrease in pain syndrome in heart. But they simultaneously suppressed the work of β2 receptors, which, as can be seen from the table, do not need to be suppressed.

In addition, the resulting side effects significantly narrowed the contingent of patients who needed such drugs. However, today there are already as many as 3 generations of BABs.

On a note. In the absence of pain in the region of the heart and attacks of "angina pectoris", the treatment of pathologies of the cardiovascular system with the help of β-blockers of any, even a new generation, is not recommended.

What drugs are beta blockers?

Until now, about 100 drugs have been created that have a depressing effect on β-adrenergic receptors. Today, there are about 30 active ingredients in use, which are the basis for the production of beta blockers.

We present the classification of beta blockers based on the list of drugs that have passed certification and are most often prescribed by our cardiologists:

List of BAB generations - name, synonyms and analogues	Characteristics, depending on the effect on adrenoreceptors
	This is a subgroup of non-selective BBs. They depress adrenergic receptors and alpha and beta types with equal force. Suppression of the latter causes negative side effects that limit their use.
	This category of BAB is selective for β-2 type receptors. It has received the general name "Cardioselective drugs". Attention! Selective and non-selective BB lower blood pressure to the same extent. But from taking cardioselective varieties of the 2nd generation, there are fewer negative effects, so they can be prescribed even in the presence of concomitant pathologies.
	These modern drugs have not only cardioselective effects. They have a vasodilating effect. They know how to relax blood vessels circulatory system. Labetalol does this by blocking alpha-adrenergic receptors, Nebivolol enhances peripheral vascular relaxation, and Carvedilol does both at the same time.

BAB drugs with internal sympathomimetic activity, in the vast majority of cases. are used in the drug therapy of uncomplicated heart failure, including during pregnancy.

At the same time, although they do not cause vasospasm and a strong slowing of the pulse, they still fail to stop attacks of angina pectoris, acute coronary syndrome, and also not to give after taking proper exercise tolerance. The list of such drugs includes - Celiprolol, Pindolol, Oxprenolol, Acebutolol.

Advice. Starting to drink the medicine, find in the instructions a mention of which type - lipophilic (fat-soluble) or hydrophilic (water-soluble) tablets are. It depends on when they should be taken, before or after eating.

In addition, it was noted that treatment with water-soluble forms does not cause nightmares. However, they, alas, are not suitable for lowering blood pressure in the presence of renal failure.

Indications for use and warnings

A detailed comparative characteristic of beta blockers is understandable only to narrow-profile cardiologists. Based on it, taking into account the real results in the achieved indicators of lowering blood pressure and improving (deteriorating) the well-being of a particular patient, individual doses are selected, and possibly combined forms of beta-blockers with other drugs for pressure. Be patient, as this can take a significant amount of time, sometimes up to a year.

In general, β-adrenergic blocking drugs can be prescribed for:

, primary hypertension, chronic stable heart failure, ischemic heart disease, arrhythmias, myocardial infarction, VQT syndrome, ventricular hypertrophy, leaflet protrusion mitral valve, hereditary disease Morfan;
secondary hypertension caused by pregnancy, thyrotoxicosis, kidney damage;
increase in blood pressure before planned and after surgical intervention;
vegetovascular crises;
glaucoma;
persistent migraines;
drug, alcohol or drug withdrawal.

For your information. Until recently, the cost of some new beta blockers was exorbitant. Today, there are many synonyms, analogues and generics that are not inferior in their effectiveness to the popular patented BAB drugs, and their price is quite affordable even for low-income pensioners.

Contraindications

Under an absolute ban is the appointment of any type of beta-blockers to patients with atrioventricular block II-III degree.

Relative include:

bronchial asthma;
chronic pulmonary obstruction;
diabetic disease, accompanied by frequent bouts of hypoglycemia.

However, it should be clarified that, under the supervision of a doctor and subject to precautions in finding and adjusting a safe dose, patients with these diseases can choose one of the many drugs of the 2nd or 3rd generation.

If there is a history of diabetic disease without episodes of hypoglycemia or metabolic syndrome, doctors are not forbidden, and even recommended to prescribe Carvedilol, Bisoprolol, Nebivolol and metoprolol succinate to such patients. They don't violate carbohydrate metabolism, do not reduce, but rather increase sensitivity to the insulin hormone, and also do not inhibit the breakdown of fats that increase body weight.

Side effects

Each of the BAB drugs has a small list of its own unique side effects.

The most common among them are:

development of general weakness;
decrease in working capacity;
increased fatigue;
dry cough, asthma attacks;
cold hands and feet;
stool disorders;
drug-induced psoriasis;
sleep disturbances accompanied by nightmares.

Important. Many men categorically refuse treatment with beta-blockers because of the side effect that is possible when taking first-generation drugs - complete or partial impotence (erectile dysfunction). Please note that the drugs of the new, 2nd and 3rd generation, help to control blood pressure and at the same time allow you to maintain potency.

withdrawal syndrome

When selecting the correct dose and type of beta-blocker, the doctor takes into account what pathology will be treated. There are BAB drugs that you can (should) drink 2 to 4 times a day. However, in the treatment of hypertension, prolonged forms are mainly used, which are drunk 1 time (in the morning) in 24 hours.

Nevertheless, one should not be surprised at patients suffering from angina pectoris. They will have to drink a prolonged form of a beta-blocker twice - both in the morning and in the evening. For them, there is also a warning about observing the gradual withdrawal of treatment with beta-blockers, since their sudden withdrawal can cause a significant aggravation of the course of the disease.

To do this, you need to strike a balance. Weekly, slightly reducing the dose of the beta-blocker, they begin to take another drug that reduces blood pressure and heart rate, also gradually increasing its dosage.

And in conclusion of this article, we suggest watching a video in which we are talking about drugs that are prohibited for simultaneous use with BAB drugs.

Frequently asked questions to the doctor

Husband's birthday is coming up. He was recently put on Carvedilol. Can he drink alcoholic beverages?

To drink or not to drink alcohol - the choice always remains with the patient. All drinks containing ethanol alcohol repeatedly neutralize the effect of beta-blocker drugs.

Plus, after a while, for everyone it is individual, and depends on many indicators, blood pressure slightly lowered by alcohol libation rises sharply, causing an attack of hypertension or angina pectoris. The combination of a beta-blocker and alcohol can result in ventricular fibrillation.

There are also paradoxical cases when BAB does not reduce, but rather enhances the effect of the drug - the pressure drops sharply, the heart slows down. Even deaths have been recorded.

What can replace beta blockers?

Based on the principles of the mechanism of action, it is possible to replace beta-blockers only with them, and switch from one type of drug to another. However, not all patients with problems in the cardiovascular system can achieve the desired result, and some have severe side effects that interfere with a normal lifestyle.

For such people, to reduce and control blood pressure, the doctor will select a diuretic and / or ACE inhibitor, and to combat tachycardia - one of the calcium channel antagonists.

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β-adrenergic receptor blockers, or β-blockers, are a group of drugs that can reversibly block β-adrenergic receptors. They are used in clinical practice since the beginning of the 60s of the XX century for the treatment of coronary artery disease and heart rhythm disturbances; later they began to be used for the treatment of hypertension, and later - for the treatment of heart failure. The importance of β-blockers in the secondary prevention of diseases of the cardiovascular system was so high that in 1988 the scientists who took part in the creation of this group of drugs were awarded the Nobel Prize. In recent years, after receiving the results of several large controlled clinical research and meta-analyzes, the range of use of β-blockers narrowed somewhat, primarily due to their less active use as drugs for primary prevention in patients with hypertension.

Mechanism of action

The mechanism of action of β-blockers is quite complex, not fully understood, differs significantly for different drugs and consists in preventing the cardiotoxic effect of catecholamines, reducing heart rate, myocardial contractility and blood pressure, which leads to a decrease in myocardial oxygen demand. Improvement in perfusion of ischemic myocardial regions with the use of β-blockers is also due to diastole lengthening and "reverse coronary steal" due to an increase in vascular resistance in non-ischemic areas of the myocardium.

Pharmacokinetics

All β-blockers are capable of blocking β-adrenergic receptors. However, these drugs have differences (Table 1). They are subdivided depending on the selectivity of action on β-adrenergic receptors. different types, the presence of internal sympathomimetic activity, solubility in fats, the ability to be metabolized in the liver, duration of action.

Table 1

The main properties of β-blockers used in the clinic

A drug	Presence of β1 -selectivity	Presence of intrinsic sympathomimetic activity	Presence of vasodilating properties	Т1/2
Atenolol Betaxolol bisoprolol Carvedilol metoprolol Nadolol Nebivolol Pindolol Proxodolol propranolol Sotalol Talinolol Timolol Esmolol	Yes Yes Yes Not Yes Not Yes Not There is no data Not Not Yes Not Yes	Not Not Not Not Not Not Not Yes Not Not Yes Yes Not Not	Not Not Not Yes Not Not Yes Not Yes Not Not Not Not Not	6-9 h 16-22 h 7-15 h 6 h 3-7 h 10-24 hours 10 h 2-4 h There is no data 2-5 h 7-15 h 6 h 2-4 h 9 min

Groups of β-blockers depending on the selectivity of action. There are two main types of β-adrenergic receptors: β1- and β2-adrenergic receptors.

Non-selective. They act equally on both types of β-adrenergic receptors (propranolol).
selective . They act to a greater extent on β1-adrenergic receptors (metoprolol, atenolol, etc.).

The selectivity of the action of β-blockers can be expressed to varying degrees, it almost always decreases or even disappears with increasing dose.

Groups of β-blockers depending on the presence of internal sympathomimetic activity and blockade of other types of receptors. Allocate β-blockers with internal sympathomimetic activity and without it, with α1 -adrenergic blocking activity and the ability to form nitric oxide.

β-blockers with intrinsic sympathomimetic activity. They are able to simultaneously have a stimulating effect on the sympathetic nervous system. Previously, this property was considered as useful by reducing the inhibitory effect of drugs on cardiovascular system. However, the presence of internal sympathomimetic activity worsens the prognosis of the disease.
β-blockers without internal sympathomimetic activity. It is the severity of the blockade of β1-adrenergic receptors that underlies the favorable effect of drugs on the prognosis of the disease.

The results of clinical studies have confirmed that β1-blockers with intrinsic sympathomimetic activity are much less effective than β-blockers without it, and currently drugs of the first group are rarely used.

β-blockers with α1-blocking activity. Due to this new effect, the drugs have an additional vasodilating effect (carvedilol).
β-blockers capable of forming nitric oxide (nebivolol).

Groups of β-blockers depending on fat solubility

Lipophilic (metoprolol, propranolol, bisoprolol, carvedilol).
hydrophilic (timolol, sotalol, atenolol).

Previously, parallels were drawn between these properties of β-adrenergic locators and their effectiveness, as well as the ability to have side effects primarily on the central nervous system. However, according to the results of recent studies, in particular a meta-analysis of observational data on 35,000 patients who received β-blockers after myocardial infarction, no relationship was found between the ability of a particular drug to dissolve in fats and have side effects.

Groups of β-blockers depending on metabolism in the liver

β-blockers metabolized in the liver. They are characterized by the so-called first pass effect.
β-blockers that are not metabolized in the liver. They are excreted from the body by the kidneys unchanged.

These properties of drugs have practically no clinically significant effect.

Groups of β-blockers depending on the duration of action. It can be indirectly judged by the half-life (in no case should the half-life be considered equal to the duration of the drug!). In accordance with this, drugs of prolonged action, medium and short duration of action are isolated.

β-blockers of prolonged action. Such drugs can be taken once a day (nadolol, bisoprolol, betaxolol). For some β-blockers (primarily for metoprolol), special dosage forms have been created that can significantly prolong their action and provide a more uniform effect.

Initially, a long-acting form of metoprolol tartrate (the so-called metoprolol SA) was proposed with a duration of effects of about 24 hours. Such dosage forms contain metoprolol tartrate in the form of an insoluble matrix (METO-IM) or in the form of a hydrophilic matrix (METO-HM). These extended release metoprolol tartrate formulations are available in Russia (eg Egilok retard).

In order to make the effect of metoprolol even more uniform, a special sustained release dosage form was proposed (metoprolol CR / ZOK; English controlled release / zero order kinetics, that is, a controlled release drug with zero order kinetics), in which metoprolol was used in the form of succinate .

Pharmacokinetic studies have shown that after taking 1 tablet of metoprolol CR / ZOK at 100 mg, a uniform concentration of metoprolol in the blood was maintained at a level of 100 nmol / l for at least 24 hours, which is significantly less than the peak concentration of the drug after taking conventional tablets (after taking a conventional metoprolol tablet the peak concentration reaches 600 nmol / l), but enough to create the maximum effect of the blockade of β-adrenergic receptors. However, the absence of sharp peaks in the increase in the concentration of metoprolol after taking dosage form slow release leads to better tolerability of the drug and prevents a number of undesirable effects.

β-Adrenoblockers of medium duration of action. The effect of regular metoprolol tartrate tablets lasts from 8 to 10 hours, so they must be administered 2 or even 3 times a day.
β-Adrenoblockers of short action. Esmolol is one of the shortest acting drugs. Its antianginal and antihypertensive effect lasts only 10-20 minutes after the infusion is stopped.

Martsevich S.Yu., Tolpygina S.N.

Beta blockers

Content

One of the Nobel Prizes in 1988 belongs to D. Black, a scientist who developed and conducted clinical trials of the first beta-blocker - propranolol. This substance began to be used in medical practice in the 60s of the 20th century. Modern cardiology practice is impossible without the use of beta-blockers for hypertension and heart disease, tachycardia and stroke, arterial disease and other dangerous pathologies of the circulatory system. Of the 100 stimulants developed, 30 are used for therapeutic purposes.

What are beta blockers

large group pharmaceuticals, which protect the beta receptors of the heart from the effects of adrenaline, are called beta-blockers (BBs). The names of medicines containing these active substances end in "lol". They can easily be chosen among medicines for the treatment of cardiovascular diseases. Atenolol, bisoprolol, propranolol, timolol and others are used as the active substance.

Mechanism of action

In the human body there is a large group of catecholamines - biologically active substances that have a stimulating effect on internal organs and systems, triggering adaptive mechanisms. The action of one of the representatives of this group - adrenaline is well known, it is also called a stress substance, the hormone of fear. The action of the active substance is carried out through special structures - β-1, β-2 adrenoreceptors.

The mechanism of action of beta-blockers is based on the inhibition of the activity of β-1-adrenergic receptors in the heart muscle. The organs of the circulatory system respond to this effect as follows:

the heart rate changes in the direction of decreasing the frequency of contractions;
the force of heart contractions decreases;
decreased vascular tone.

In parallel, beta-blockers inhibit the action nervous system. So it is possible to restore the normal functioning of the heart, blood vessels, which reduces the frequency of angina attacks, arterial hypertension, atherosclerosis, coronary disease. Reduces the risk of sudden death from a heart attack, heart failure. Advances have been made in the treatment of hypertension and conditions associated with high blood pressure.

Indications for use

Beta-blockers are prescribed for hypertension and heart disease. This general characteristics their therapeutic effect. The most common diseases for which they are used are:

Hypertension. Beta-blockers for hypertension reduce the load on the heart, its oxygen demand decreases and blood pressure normalizes.
Tachycardia. With a heart rate of 90 beats per minute or more, beta-blockers are the most effective.
Myocardial infarction. The action of the substances is aimed at reducing the affected area of the heart, preventing relapse, and protecting the muscle tissue of the heart. In addition, drugs reduce the risk of sudden death, increase physical endurance, reduce the development of arrhythmias, and contribute to myocardial oxygen saturation.
Diabetes mellitus with cardiac pathologies. Highly selective beta-blockers improve metabolic processes enhance tissue sensitivity to insulin.
Heart failure. Drugs are prescribed according to a scheme that involves a gradual increase in dosage.

The list of diseases for which beta-blockers are prescribed includes glaucoma, various types of arrhythmia, mitral valve prolapse, tremor, cardiomyopathy, acute aortic dissection, hyperhidrosis, complications of hypertension. The drugs are prescribed for the prevention of migraine, varicose bleeding, for the treatment of arterial pathologies, depression. Therapy of these diseases involves the use of only some BBs, since their pharmacological properties are different.

Classification of drugs

The classification of beta-blockers is based on the specific properties of these active substances:

Adrenaline receptor blockers are able to simultaneously act on both β-1 and β-2 structures, which causes side effects. Based on this feature, two groups of drugs are distinguished: selective (acting only on β-1 structures) and non-selective (acting on both β-1 and β-2 receptors). Selective BBs have a peculiarity: with increasing dosage, the specificity of their action is gradually lost, and they begin to block β-2 receptors as well.
Solubility in certain substances distinguishes groups: lipophilic (soluble in fat) and hydrophilic (soluble in water).
BB, which are able to partially stimulate adrenoreceptors, are combined into a group of drugs with internal sympathomimetic activity.
Adrenaline receptor blockers are divided into short-acting and long-acting drugs.
Pharmacologists have developed three generations of beta-blockers. All of them are still used in medical practice. The drugs of the last (third) generation have the least number of contraindications and side effects.

Cardioselective beta-blockers

The higher the selectivity of the drug, the stronger the therapeutic effect it has. Selective beta-blockers of the first generation are called non-cardioselective, these are the earliest representatives of this group of drugs. In addition to therapeutic, they have strong side effects (for example, bronchospasm). II generation BBs are cardioselective drugs, they have a directed effect only on type 1 cardiac receptors and have no contraindications for people with diseases of the respiratory system.

Talinolol, Acebutanol, Celiprolol have internal sympathomimetic activity, Atenolol, Bisoprolol, Carvedilol do not have this property. These medicines have proven themselves in the treatment of atrial fibrillation, sinus tachycardia. Talinolol is effective in hypertensive crisis, angina attacks, heart attack, in high concentrations it blocks type 2 receptors. Bisoprolol can be taken continuously for hypertension, ischemia, heart failure, and is well tolerated. It has a pronounced withdrawal syndrome.

Internal sympathomimetic activity

Alprenolol, Karteolol, Labetalol - the 1st generation of beta-blockers with internal sympathomimetic activity, Epanolol, Acebutanol, Celiprolol - the 2nd generation of drugs with such an effect. Alprenolol is used in cardiology for the treatment of coronary heart disease, hypertension, a non-selective beta-blocker with a large number of side effects and contraindications. Celiprolol has proven itself in the treatment of hypertension, is the prevention of angina attacks, but the interaction of the drug with a lot of medicines has been revealed.

Lipophilic drugs

Lipophilic adrenaline receptor blockers include Propranolol, Metoprolol, Retard. These drugs are actively processed by the liver. In hepatic pathologies or in elderly patients, an overdose may occur. Lipophilicity determines the side effects that manifest themselves through the nervous system, such as depression. Propranolol is effective in thyrotoxicosis, cardiomyalgia, myocardial dystrophy. Metoprolol inhibits the action of catecholamines in the heart during physical and emotional stress, is indicated for use in cardiac pathologies.

Hydrophilic drugs

Beta-blockers for hypertension and heart disease, which are hydrophilic drugs, are not processed by the liver, they are excreted through the kidneys. In patients with kidney failure accumulate in the body. They have a prolonged action. It is better to take medicines before meals and drink plenty of water. Atenolol belongs to this group. It is effective in the treatment of hypertension, the hypotensive effect lasts for about a day, while the peripheral vessels remain in good shape.

Latest generation beta blockers

The latest generation of beta-blockers include Carvedilol, Celiprolol. They have a minimum number of side effects, and you need to use them once a day. Carvedilol is prescribed in complex therapy for chronic heart failure, as a prophylactic against angina attacks, with hypertension. Celiprolol has similar prescriptions, this drug is canceled gradually, for at least 2 weeks.

Unfortunately, with age or for a number of other reasons, the heart muscle stops contracting properly, however, modern medications effectively help to stimulate contractions of the heart muscle. Beta-blockers formed the basis of many drugs for angina and lowering blood pressure, in their composition they contain special substances that are a barrier from the negative effects of adrenaline on the heart. To facilitate the search for these drugs, they are usually called with an ending in "lol", consider the most effective and popular beta-blockers list of drugs for hypertension, get acquainted with the indications and contraindications of these medications.

Purpose of use

Medical statistics puts mortality from cardiovascular diseases in the first place, respectively, the fight against these diseases has become a global scale, every year the best specialists develop more and more effective medicines for the treatment of hypertension and other diseases in this category. Most of them contain beta-blockers. As mentioned above, the main goal of these funds is to reduce the effect of adrenaline on the heart muscle, the secretion of this hormone increases the work of the heart at times, resulting in an increase in blood pressure, which negatively affects the work of the whole organism as a whole.

Basically, these drugs affect:

normalization of blood pressure;
reducing the risk of complications in the course of hypertension;
reducing the risk of heart attack, stroke and other cardiovascular diseases.

But whatever the purpose of these funds, their intake without the supervision of a doctor is prohibited, you do not need to self-medicate, the dosage and calculation of the time of admission should be prescribed by a specialist.

Classification

V modern medicine there are a huge number of adrenoblockers, all of them are aimed at slowing down the nerve impulse, but each of the drugs depends on its effect on receptors, and also other features:

lipophilic - used to pass substances between the vessel and the nerve fiber, easily disintegrate in a fat-like environment, lipophilic drugs are processed by the liver. The most common are Metoprolol;
hydrophilic beta-blockers are used to act mainly in the aquatic environment, this type undergoes a change in the liver more slowly, they are practically not processed by it, respectively, their duration of action is longer. One of these drugs is Atenolol;
All beta blockers act on two types of beta receptors called beta-1 and beta-2. If drugs simultaneously act on both types of receptors, then it is called non-selective, if only one, then it is called selective. Non-selective beta-blockers for hypertension include nadolol. Selective substances have an effect on beta-1, which are concentrated in the heart muscle, so these substances have a second name - Cardioselective, these include Bisoprolol;
there is a group of beta-blockers that are used to stop the negative action of beta-adrenergic receptors, most often these drugs are prescribed as auxiliary drugs for the treatment of prostate adenoma. The function of the drug in this case is to facilitate the process of urination in men, the most prescribed is Dexazonin;
a separate group of drugs include Concor, active substance is Bisoprolol, the drug is neutral, does not change the level of sugar in the blood, as other active substances of this series do.

Modern medicine does not stand still, every year pharmaceutical scientists develop new beta-blockers, so one generation of drugs is replaced by another. If these medicinal substances are classified into groups according to the release date, then all beta-blockers are divided into three generations, the most modern - the third, scientists are trying to reduce the risks of side effects, increase the effectiveness of active substances, etc.

The first generation of beta-blockers for hypertension - Propranolol, Nadolol.
Second generation - Atenolol, Bisoprolol;
The most modern in medicine include Celiprolol and Carvedilol.

The latest generation drugs have an increased duration of action in the body, so the patient should take them only once a day, all third-generation drugs are aimed at relaxing blood vessels.

Concor

One of the most modern and effective drugs is Concor. The drug belongs to beta-1-blockers, the main active ingredient is Kisoprolol. The active substance does not affect respiratory system, but still there are a number of contraindications.

Concor takes once a day, does not require grinding.

While taking Concor, the coronary vessels expand, the pressure decreases, and the pulse rate decreases.

This medicine has an analogue - Coronal.

Indications

Beta-blockers for hypertension are also applicable to a number of other diseases, their list is very wide. Patients with the following diseases shown beta blockers:

ischemia of the heart;
as mentioned above, hypertension;
heart failure;
tachycardia;
myocardial infarction;
various complications of diabetes.

Also, these drugs are used in combination with other medicines in the treatment of vegetative diseases, migraines, withdrawal symptoms. Which of the beta-blockers to use in a particular case is decided by the attending physician after a detailed examination of the patient, only he can recommend the dosage and frequency of taking the medication.

Application

Hypertension implies treatment with these drugs, in this case there is a long course of therapy, and it is necessary to strictly follow the recommendations of the attending physician:

it is not allowed to prescribe inhibitors on your own, because. they have many side effects and a number of contraindications;
also, the doctor must be told about all past and current diseases, chronic diseases;
because these drugs can affect the hormonal background of a woman, it is necessary to talk about pregnancy or pregnancy planning during a medical consultation, but this does not mean that beta-blockers are prohibited during the period of bearing a child, some categories of drugs are prescribed in the third trimester under the supervision of a doctor;
in order to adjust the dosage and duration of the use of medications, it is necessary to keep a blood pressure diary, where you need to record all indications of pressure changes during the day;
because beta-blockers have a number of side effects, their use is allowed only under the strict supervision of the attending physician, and the patient himself must carefully observe and listen to the reaction of his body;
to reduce the risk of side effects, these drugs should be taken with or immediately after meals;
if the patient is to undergo anesthesia, then it is necessary to say in advance about taking beta-blockers, even anesthesia during tooth extraction on people taking these medications has a special effect.

Side effect

As mentioned above, beta-blockers have many side effects, so the appointment of these drugs is under the strict supervision of the attending physician. The main side effects include:

chronic feeling of fatigue;
bradycardia;
asthma attacks;
blockade;
development of shortness of breath with any physical exertion;
hypoglycemia;
with a sharp withdrawal of the drug, there may be jumps in blood pressure;
increased risk of heart attacks.

There are a number of conditions for which beta-blockers may pose a risk of complicating current conditions:

diabetes;
chronic depression;
obstructive diseases of the respiratory system;
pathologies in the blood supply system;
dyslipidemia.

Contraindications

For some diseases, these drugs are strictly prohibited, the doctor must find another method of treatment. These diseases include:

bronchial asthma;
allergy, flesh to Quincke's edema;
bradycardia in severe forms;
blockades;
pathology of the sinus node;
vascular pathology;
hypotension.

Cancel

It is worth noting that it is not recommended to cancel beta-blockers abruptly, the so-called withdrawal syndrome often occurs, as mentioned above, sharp jumps in blood pressure can be observed. V rare cases with a sharp abolition of these drugs, a hypertensive crisis develops. During what time the medicine will be canceled, the attending physician decides, sometimes the cancellation takes several weeks.

We remind you once again that beta-blockers, the list of these drugs for hypertension was given above - substances that have many side effects and contraindications, so it is not recommended to take them without a doctor's prescription, uncontrolled use of drugs can lead to serious consequences for the patient's health.

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From this article you will learn: what are adrenoblockers, what groups they are divided into. Mechanism of their action, indications, list of adrenoblockers.

Article publication date: 06/08/2017

Article last updated: 05/29/2019

Adrenolytics (blockers) are a group of drugs that block nerve impulses that respond to norepinephrine and adrenaline. medicinal effect they are opposite to the action of adrenaline and norepinephrine on the body. The name of this pharmaceutical group speaks for itself - the drugs included in it "interrupt" the action of adrenoreceptors located in the heart and the walls of blood vessels.

Such drugs are widely used in cardiology and therapeutic practice for the treatment of vascular and heart diseases. Often cardiologists prescribe them to older people who are diagnosed with arterial hypertension, cardiac arrhythmias and other cardiovascular pathologies.

Classification of blockers

There are 4 types of receptors in the walls of blood vessels: beta-1, beta-2, alpha-1, alpha-2-adrenergic receptors. The most common are alpha- and beta-blockers, which “turn off” the corresponding adrenaline receptors. There are also alpha-beta blockers that simultaneously block all receptors.

The means of each of the groups can be selective, interrupting selectively only one type of receptor, for example, alpha-1. And non-selective with simultaneous blocking of both types: beta-1 and -2 or alpha-1 and alpha-2. For example, selective beta-blockers can only affect beta-1.

Subgroups of adrenolytics:

General mechanism of action of adrenergic blockers

When norepinephrine or epinephrine is released into the bloodstream, adrenoceptors instantly react by binding to it. As a result of this process, the following effects occur in the body:

narrowing of the vessels;
pulse quickens;
blood pressure rises;
increases the level of glucose in the blood;
bronchi expand.

If there are certain diseases, for example, arrhythmia or hypertension, then such effects are undesirable for a person, because they can provoke or relapse the disease. Adrenoblockers "turn off" these receptors, so they act in the opposite way:

dilate blood vessels;
slow down the heart rate;
prevent an increase in blood sugar;
narrow the lumen of the bronchi;
lower BP.

These are common actions characteristic of all types of drugs from the group of adrenolytics. But drugs are divided into subgroups depending on the effect on certain receptors. Their actions are slightly different.

Common side effects

Common to all blockers (alpha, beta) are:

Headache.
Fast fatiguability.
Drowsiness.
Dizziness.
Increased nervousness.
Short-term fainting is possible.
Violations of the normal activity of the stomach and digestion.
Allergic reactions.

Since drugs from different subgroups have slightly different therapeutic actions, then the undesirable consequences of their reception also differ.

General contraindications for selective and non-selective beta-blockers:

bradycardia;
weak sinus syndrome;
acute heart failure;
atrioventricular and sinoatrial blockade;
hypotension;
decompensated heart failure;
allergy to drug components.

Non-selective blockers should not be taken with bronchial asthma and obliterating vascular disease, selective - in the pathology of the peripheral circulation.

Click on photo to enlarge

Such medications should be prescribed by a cardiologist or therapist. Independent uncontrolled intake can lead to serious consequences up to death due to cardiac arrest, cardiogenic or anaphylactic shock.

Alpha blockers

Action

Alpha-1 receptor blockers dilate blood vessels in the body: peripheral - noticeable by redness skin and mucous; internal organs- in particular the intestines with the kidneys. Due to this, peripheral blood flow increases, microcirculation of tissues improves. The resistance of the vessels along the periphery decreases, and the pressure decreases, and without a reflex increase in heart rate.

By reducing returns venous blood into the atria and the expansion of the "periphery" significantly reduces the load on the heart. Due to the facilitation of his work, the degree characteristic of hypertensive patients and elderly people with heart problems decreases.

Other effects:

affect fat metabolism. Alpha-ABs lower triglycerides, "bad" cholesterol and increase high-density lipoproteins. Such an additional effect is good for people suffering from hypertension aggravated by atherosclerosis.
Influence the metabolism of carbohydrates. When taking drugs, the susceptibility of cells to insulin increases. Because of this, glucose is absorbed faster and more efficiently, which means that its level does not increase in the blood. This action is important for diabetics, in whom alpha-blockers reduce blood sugar levels.
Reduce the severity of signs of inflammation in the organs of the genitourinary system. These drugs are successfully used in prostatic hyperplasia to eliminate some of the characteristic symptoms: partial emptying Bladder, burning in the urethra, frequent and nocturnal urination.

Blockers of alpha-2 adrenaline receptors have the opposite effect: constrict blood vessels, increase blood pressure. Therefore, they are not used in cardiology practice. But they successfully treat impotence in men.

List of drugs

The table provides a list of international generic names of drugs from the group of alpha receptor blockers.

Indications for use

Since the effect of drugs from this subgroup on the vessels is somewhat different, their scope is also different.

Indications for the appointment of alpha-1-blockers	Indications for alpha-1, -2 blockers
Arterial hypertension	Eating disorders in soft tissues limbs - ulceration due to bedsores, frostbite, thrombophlebitis, severe atherosclerosis
Chronic heart failure with myocardial hypertrophy	Diseases accompanied by a disorder of peripheral blood flow - diabetic microangiopathy, endarteritis, Renaud's disease, acrocyanosis
prostate hyperplasia	Migraine
	Relief of the consequences of a stroke
	Senile dementia
	Job failure vestibular apparatus due to vascular problems
	Corneal dystrophy
	Elimination of manifestations of neurogenic bladder
	Prostatitis
	Optic neuropathy

There is only one indication for alpha-2 blockers - erectile dysfunction in men.

Side effects of alpha-adrenolytics

In addition to the common side effects listed above in the article, these drugs have the following side effects:

Side effects of alpha-1 blockers	Undesirable effects when taking alpha-2 receptor blockers	Side effects from alpha-1, -2-blockers
Edema	Increase in blood pressure	Loss of appetite
A strong decrease in blood pressure	The appearance of anxiety, irritability, increased excitability, motor activity	Insomnia
Arrhythmia, tachycardia	Tremor (shaking in the body)	sweating
The appearance of shortness of breath	Decreased frequency of urination and volume of urine produced	Cold extremities
Runny nose		Heat in the body
Dryness of the oral mucosa		Increased acidity (pH) of gastric juice
Chest pain
Decreased sex drive
Urinary incontinence
painful erections

Contraindications

Pregnancy.
lactation period.
Allergy or intolerance to the active ingredient or excipients.
Severe disorders (diseases) of the liver, kidneys.
Arterial hypotension is low blood pressure.
Bradycardia.
Severe heart defects, including aortic stenosis.

Beta blockers

Cardioselective beta-1-blockers: principle of action

Medicines from this subgroup are used to treat heart disease, because they mainly have a positive effect on this organ.

Received effects:

Antiarrhythmic action by reducing the activity of the pacemaker - the sinus node.
Decreased heart rate.
Decreased excitability of the myocardium under conditions of psycho-emotional and / or physical activity.
Antihypoxic effect due to a decrease in the oxygen demand of the heart muscle.
Lowering blood pressure.
Prevention of the expansion of the focus of necrosis in a heart attack.

A group of selective drugs, beta-blockers, reduce the frequency and alleviate an attack of angina pectoris. They also improve the tolerance of physical and mental stress on the heart in patients with heart failure, who prolong life. These funds significantly improve the quality of life for patients who have had a stroke or myocardial infarction, suffering from coronary heart disease, angina pectoris, and hypertension.

In diabetics, they prevent an increase in blood sugar levels, reduce the risk of bronchospasm in people with bronchial asthma.

Non-selective beta-1, -2-blockers: action

In addition to antiarrhythmic, hypotensive, antihypoxic effects, such drugs have other actions:

The antithrombotic effect is possible due to the prevention of platelet aggregation.
Strengthen the contraction of the muscular layer of the uterus, intestines, esophageal sphincter, at the same time relaxing the sphincter of the bladder.
During childbirth, blood loss is reduced in the woman in labor.
Increase the tone of the bronchi.
Reduce intraocular pressure by reducing fluid in the anterior chamber of the eye.
Reduce risk acute infarction, stroke, development of coronary artery disease.
Reduce mortality from heart failure.

List of drugs

There are currently no drugs belonging to the pharmacological subgroup of beta-2-adrenergic receptors.

Indications for use

Indications for prescribing selective beta-blockers	Indications for the appointment of non-selective beta-blockers
ischemic heart disease	Arterial hypertension
Hypertension	Left ventricular myocardial hypertrophy
Hypertrophic cardiomyopathy	angina pectoris
Most types of arrhythmias	heart attack
Prevention of migraine attacks	Mitral valve prolapse
Mitral valve prolapse	Sinus tachycardia
Treating an existing heart attack and preventing a recurrence	Glaucoma
Neurocirculatory dystonia (hypertonic type)	Prevention of massive bleeding during childbirth or gynecological operations
Removal of motor excitation - akathisia - against the background of taking antipsychotics	Minor's disease is a disease of the nervous system of a hereditary nature, manifested by the only symptom - trembling of the hands.
At complex treatment thyrotoxicosis

Side effects

Common side effects of this group of drugs	Non-selective beta-blockers can also cause
Weakness	Vision problems: hazy, double vision, burning sensation, sensation of being hit foreign body, lacrimation
Reaction slowdown	Runny nose
Drowsiness	Cough, possible asthma attacks
Depression	A sharp drop in blood pressure
Temporary loss of vision and loss of taste	Fainting
Coldness and numbness of feet and hands	Ischemia of the heart
Bradycardia	Impotence
Conjunctivitis	Colitis
Dyspepsia	Increase in blood potassium, triglycerides, uric acid
Increased or slow heart rate

Alpha beta blockers

Action

Drugs from this subgroup lower arterial and intraocular pressure, normalize lipid metabolism, i.e. reduce the level of triglycerides, cholesterol, low density lipoproteins, while increasing high density. The hypotensive effect is achieved without changes in renal blood flow and an increase in total peripheral vascular resistance.

When they are taken, the adaptation of the heart to physical and psycho-emotional stress increases, contractile function heart muscle. This leads to a decrease in the size of the heart, normalization of the rhythm, relief from heart disease or congestive insufficiency. If IHD is diagnosed, then the frequency of its attacks against the background of taking alpha-beta-blockers decreases.

List of medicines

Carvedilol.
Butylmethyloxadiazole.
Labetalol.

Open angle glaucoma

Contraindications

You can not take adrenoblockers from this subgroup for the same pathologies as described above, supplementing them with obstructive pulmonary disease, diabetes(I type), peptic ulcer of the stomach and 12 duodenal ulcer.