Who and why are beta-blockers prescribed? What are beta- and alpha-blockers, their classification Without internal sympathomimetic activity

Adrenoblockers make up a large group of drugs that cause blockade of receptors for adrenaline and norepinephrine. They are widely used in therapeutic and cardiological practice, they are prescribed everywhere for patients of different ages, but mainly for the elderly, who are most likely to have vascular and heart damage.

The functioning of organs and systems is subject to the action of a variety of biologically active substances, which affect certain receptors and cause certain changes - vasodilation or constriction, a decrease or increase in the strength of heart contractions, bronchospasm, etc. In certain situations, the action of these hormones is excessive or it becomes necessary to neutralize their effects due to emerging disease.

Epinephrine and norepinephrine are secreted by the adrenal medulla and have a wide range of biological effects.- vasoconstriction, increased pressure, increased blood sugar, bronchial dilation, relaxation of the intestinal muscles, dilated pupils. These phenomena are possible due to the release of hormones in peripheral nerve endings, from which the necessary impulses go to organs and tissues.

At various diseases there is a need for blockade of adrenergic impulses to eliminate the effects of adrenaline and norepinephrine. For this purpose, adrenoblockers are used, the mechanism of action of which is the blockade of adrenoreceptors, protein molecules to adrenaline and norepinephrine, while the formation and release of the hormones themselves are not disturbed.

Classification of adrenoblocking substances

There are alpha-1, alpha-2, beta-1 and beta-2 receptors located in the vascular walls and the heart. Depending on the variety of inactivated receptors, alpha- and beta-blockers are isolated.

Alpha-blockers include phentolamine, tropafen, pyrroxane, and agents that inhibit the activity of beta receptors include anaprilin, labetalol, atenolol and others. The drugs of the first group turn off only those effects of adrenaline and noradrenaline that are mediated by alpha receptors, the second - respectively, by beta-adrenergic receptors.

To increase the effectiveness of treatment and eliminate some side effects, selective adrenoblocking substances have been developed that act strictly on a certain type of receptor (α1,2, β1,2).

Groups of adrenoblockers

  1. Alpha blockers:
    • α-1-blockers - prazosin, doxazosin;
    • α-2-blockers - yohimbine;
    • α-1,2-blockers - phentolamine, pyrroxane, nicergoline.
  1. Beta blockers:
    • cardioselective (β-1) blockers - atenolol, bisoprolol;
    • non-selective β-1,2-blockers - propranolol, sotalol, timolol.
  1. Blockers of both alpha and beta adrenoreceptors - labetalol, carvedilol.

Alpha blockers

Alpha-blockers (alpha-AB), blocking different types alpha receptors act in the same way, realizing the same pharmacological effects, and the difference in their use is in the number of adverse reactions, which, for obvious reasons, are more in alpha 1,2 blockers, because they are directed to all adrenaline receptors at once.

Drugs in this group contribute to the expansion of the lumen of blood vessels, which is especially noticeable in the skin, mucous membranes, intestinal wall, kidneys. With an increase in the capacity of the peripheral bloodstream, the resistance of the vascular walls and systemic arterial pressure decrease, therefore microcirculation and blood flow in the periphery circulatory system is greatly facilitated.

A decrease in venous return due to the expansion and relaxation of the "periphery" contributes to reducing the load on the heart, due to which its work becomes easier, and the condition of the organ improves. Alpha-blockers help to reduce the degree by facilitating the work of the organ, do not cause tachycardia, which often occurs when using a number.

In addition to the vasodilating and hypotensive effect, alpha-blockers change the indicators of fat metabolism for the better, contributing to a decrease in the total and increasing the concentration of anti-atherogenic fat fractions, so their appointment is possible with obesity and dyslipoproteinemias of various origins.

With the use of α-blockers, carbohydrate metabolism also changes. Cells become more sensitive to insulin, so sugar is better and faster absorbed by them, which prevents hyperglycemia and normalizes the indicator. This effect is very important for patients.

A special scope of alpha-blockers is urological pathology. So, α-adrenergic blocking drugs are actively used in prostate hyperplasia due to the ability to eliminate some of its symptoms (night urination, partial emptying Bladder, burning sensation in the urethra).

Alpha-2-blockers have a weak effect on the vascular walls and heart, so they are not popular in cardiology, however, in the course of clinical trials, a striking effect on the genital area was noticed. This fact became the reason for their appointment for sexual dysfunction in men.

Indications for the use of alpha-AB are:

  • Peripheral blood flow disorders - acrocyanosis, diabetic microangiopathy);
  • Pheochromocytoma;
  • Trophic lesions of the soft tissues of the extremities, in particular, with atherosclerosis, frostbite, bedsores;
  • Consequences of transferred, vascular dementia;
  • BPH;
  • Anesthesia and surgical operations - for the prevention of hypertensive crises.

Prazosin, doxazosin actively used in the treatment of hypertension, tamsulosin, terazosin effective in prostatic hyperplasia. Pyrroxane has a sedative effect, improves sleep, relieves itching in allergic dermatitis. In addition, due to the ability to inhibit the activity of the vestibular apparatus, pyrroxane can be prescribed for sea and air sickness. In narcological practice, it is used to reduce the manifestations of morphine withdrawal syndrome and alcohol withdrawal.

Nicergoline used by neurologists in the treatment of the brain, is indicated for acute and chronic disorders of cerebral blood flow, transient ischemic attacks, can be prescribed for head injuries, for the prevention of migraine attacks. It has an excellent vasodilating effect, improves blood circulation in the limbs, therefore it is used in the pathology of the peripheral bed (Raynaud's disease, atherosclerosis, diabetes, etc.).

Beta blockers

Beta-blockers (beta-blockers), used in medicine, are directed either to both types of beta receptors (1,2), or to beta-1. The first is called non-selective, the second - selective. Selective beta-2-ABs are not used for therapeutic purposes, since they do not have significant pharmacological effects, the rest are widespread.

basic action of beta-blockers

Beta-blockers have a wide range of effects associated with the inactivation of beta-receptors in blood vessels and the heart. Some of them are able not only to block, but also to some extent activate receptor molecules - the so-called internal symatomimetic activity. This property is noted for non-selective drugs, while selective beta-1-blockers are deprived of it.

Beta-blockers are widely used in the treatment of diseases of the cardiovascular system.- , . They reduce the heart rate, reduce pressure, and have an analgesic effect when. Depression of the central nervous system by certain drugs is associated with a decrease in concentration, which is important for drivers of vehicles and people engaged in strenuous physical and mental work. At the same time, this effect can be used in anxiety disorders.

Non-selective beta blockers

Means of non-selective action contribute to a decrease in heart rate, somewhat reduce the total vascular peripheral resistance, and have a hypotensive effect. The contractile activity of the myocardium decreases, therefore, the amount of oxygen required for the work of the heart also becomes less, which means that resistance to hypoxia increases (at, for example).

By reducing vascular tone, reducing the release of renin into the bloodstream, the hypotensive effect of beta-AB in hypertension is achieved. They have an antihypoxic and antithrombotic effect, reduce the activity of excitation centers in the conduction system of the heart, preventing arrhythmias.

Beta blockers tone up smooth muscle bronchi, uterus, gastrointestinal tract and, at the same time, relax the sphincter of the bladder.

The effects allow beta-blockers to reduce the likelihood of occurrence and sudden coronary death, according to some reports, by half. Patients with ischemia of the heart during their use note that pain attacks become more rare, resistance to physical and mental stress increases. In hypertensive patients, when taking non-selective beta-blockers, the risk of myocardial ischemia becomes less.

The ability to increase the tone of the myometrium allows the use of this group of drugs in obstetric practice to prevent and treat atonic bleeding during childbirth, blood loss during operations.

Selective beta-blockers

location of β-adrenergic receptors

Selective beta-blockers act primarily on the heart. Their influence is:

  1. Decrease in heart rate;
  2. Decrease in activity sinus node, conductive tracts and myocardium, due to which an antiarrhythmic effect is achieved;
  3. Reducing the oxygen required by the myocardium - antihypoxic effect;
  4. Decreased systemic pressure;
  5. Limiting the focus of necrosis in a heart attack.

With the appointment of beta-blockers, the load on the heart muscle and the volume of blood entering the aorta from the left ventricle at the time of systole are reduced. In patients taking selective drugs, reduces the risk of tachycardia when changing position from supine to vertical.

The clinical effect of cardioselective beta-blockers is a decrease in the frequency and severity of angina attacks, increased resistance to physical and psycho-emotional stress. In addition to improving the quality of life, they reduce mortality from heart disease, the likelihood of hypoglycemia in diabetes, and bronchospasm in asthmatics.

The list of selective beta-ABs includes many names, including atenolol, acebutolol, bisoprolol, metoprolol (egilok), nebivolol. Non-selective blockers of adrenergic activity include nadolol, pindolol (visken), propranolol (anaprilin, obzidan), timolol (eye drops).

Indications for the appointment of beta-blockers are:

  • Increased systemic and intraocular (glaucoma) pressure;
  • Ischemic heart disease (angina pectoris, myocardial infarction);
  • Migraine prevention;
  • Pheochromocytoma, thyrotoxicosis.

Beta-blockers are a serious group of drugs that can only be prescribed by a doctor, but even in this case, adverse reactions are possible. Patients may experience headache and dizziness, complain of poor sleep, weakness, reduced emotional background. A side effect may be hypotension, slowing of the heart rate or its violation, allergic reactions, shortness of breath.

Non-selective beta-blockers, among the side effects, have a risk of cardiac arrest, visual impairment, fainting, signs of respiratory failure. Eye drops can cause irritation of the mucous membrane, burning sensation, lacrimation, inflammation in the tissues of the eye. All these symptoms require consultation with a specialist.

When prescribing beta-blockers, the doctor will always take into account the presence of contraindications, which are more in the case of selective drugs. It is impossible to prescribe substances that block adrenoreceptors to patients with pathology of conduction in the heart in the form of blockades, bradycardia, they are prohibited in cardiogenic shock, individual hypersensitivity to drug components, acute or chronic decompensated heart failure, bronchial asthma.

Selective beta-blockers are not prescribed for pregnant women and nursing mothers, as well as for patients with distal blood flow pathology.

The use of alpha-beta-blockers

Drugs from the group of α,β-blockers help to lower systemic and intraocular pressure, improve fat metabolism (reduce the concentration of cholesterol and its derivatives, increase the proportion of anti-atherogenic lipoproteins in blood plasma). Expanding blood vessels, reducing pressure and load on the myocardium, they do not affect the blood flow in the kidneys and the total peripheral vascular resistance.

Drugs acting on two types of adrenaline receptors increase myocardial contractility, due to which the left ventricle completely ejects the entire volume of blood into the aorta at the time of its contraction. This effect is important when the heart is enlarged, its cavities expand, which often happens with heart failure, heart defects.

When administered to patients with heart failure, α,β-blockers improve heart function, making patients more resistant to physical and emotional stress, prevent tachycardia, and angina attacks with pain in the heart become more rare.

Having a positive effect, primarily on the heart muscle, α,β-blockers reduce mortality and the risk of complications in acute myocardial infarction, dilated cardiomyopathy. The reasons for their appointment are:

  1. Hypertension, including at the time of the crisis;
  2. Congestive heart failure - in combination with other groups of drugs according to the scheme;
  3. Chronic ischemia of the heart in the form of stable angina pectoris;
  4. Some types of heart rhythm disturbances;
  5. Increased intraocular pressure - applied topically in drops.

While taking this group of drugs, it is possible side effects, which reflect the effect of the drug on both types of receptors - both alpha and beta:

  • dizziness and headache associated with a decrease blood pressure, fainting is possible;
  • Weakness, feeling tired;
  • Decrease in the frequency of contractions of the heart, deterioration in the conduction of impulses through the myocardium up to blockades;
  • Depressive states;
  • Changes in blood counts - a decrease in leukocytes and platelets, which is fraught with bleeding;
  • Edema and weight gain;
  • Shortness of breath and bronchospasm;
  • Allergic reactions.

This is an incomplete list of possible effects, about which the patient can read all the information in the instructions for use for a particular drug. Do not panic if you find such an impressive list of possible adverse reactions, because the frequency of their occurrence is low and usually the treatment is well tolerated. If there are contraindications to specific substances, the doctor will be able to choose another remedy with the same mechanism of action, but safe for the patient.

Alpha-beta-blockers can be used as drops to treat raised intraocular pressure (glaucoma). The probability of systemic action is small, but still it is worth bearing in mind some possible manifestations of treatment: hypotension and slowing of the heartbeat, bronchospasm, shortness of breath, palpitations and weakness, nausea, allergic reactions. When these symptoms appear, it is urgent to go to an ophthalmologist to correct therapy.

Like any other group of drugs, α,β-blockers have contraindications for use, which are known to therapists, cardiologists and other doctors who use them in their practice.

These drugs should not be prescribed to patients with impaired conduction of impulses in the heart.(sinoatrial block, AV block 2-3 degree, sinus bradycardia with a pulse rate of less than 50 per minute), as they will further aggravate the disease. Due to the effect of lowering pressure, these drugs are not used in hypotensive patients, with cardiogenic shock, decompensated heart failure.

Individual intolerance, allergies, severe liver damage, diseases with bronchial obstruction (asthma, obstructive bronchitis) are also an obstacle to the use of adreno-blocking agents.

Alpha-beta-blockers are not prescribed for expectant mothers and lactating women due to the possible negative effect on the fetus and the body of the infant.

The list of drugs with beta-adrenergic blocking effects is very wide, they are taken by a large number of patients with cardiovascular pathology around the world. With high efficacy, they are usually well tolerated, rarely give adverse reactions and can be prescribed for a long time.

Like any other medicine, a beta-blocker cannot be used alone, without the supervision of a doctor, even if it helps to reduce pressure or eliminate tachycardia in a close relative or neighbor. Before using such drugs, a thorough examination is necessary to establish an accurate diagnosis in order to exclude the risk of adverse reactions and complications, as well as consultation with a therapist, cardiologist, ophthalmologist.

Unfortunately, with age or for a number of other reasons, the heart muscle stops contracting properly, but modern medications effectively help stimulate contractions of the heart muscle. Beta-blockers formed the basis of many drugs for angina pectoris and lowering blood pressure, in their composition they contain special substances that are a barrier against 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 disease in the first place, respectively, the fight against these diseases has acquired 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, there is no need to self-medicate, the dosage and calculation of the time of admission should be prescribed by a specialist.

Classification

IN 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.

  1. The first generation of beta-blockers for hypertension - Propranolol, Nadolol.
  2. Second generation - Atenolol, Bisoprolol;
  3. 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 conditions are indicated for 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;
  • to adjust the dosage and duration of the use of medications, it is necessary to keep a diary of blood pressure, 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. In rare cases, with the abrupt abolition of these drugs develops hypertensive crisis. 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.

In contact with

Treatment of cardiac diseases in modern medical practice is almost impossible to imagine without the use of a special group of drugs - beta-blockers.

The list of diseases for which therapy using these drugs is used is extensive. They effectively normalize blood pressure and heart rate.

However, like any medication, beta-blockers require caution and care during therapy.

Beta-blockers are used in the treatment of the following diseases:

  • a chronic condition of high blood pressure in the body;
  • increased pressure against the background of other pathologies;
  • rapid rhythm of contractions of the heart muscle;
  • pain in the heart with a diagnosed ischemic disease;
  • rehabilitation period after a previous heart attack;
  • pathological changes in the rhythm of heart contractions;
  • functional disorders in the work of the myocardium;
  • thickening of the ventricular wall;
  • an abnormal increase in the size of the ventricle and septum;
  • the state in which mitral valve protrudes into the cavity of one atrium at the time of contraction of the other;
  • asynchronous contraction of ventricular myocardial cells or risk sudden death;
  • high level of pressure against the background of the transferred surgical intervention;
  • migraine;
  • alcohol and drug addiction.

Classification

The drugs in this group have several classifications that divide drugs according to various criteria.

All beta-blockers are divided depending on the characteristics of their effects on receptors:

  • non-selective drugs;
  • selective drugs.

A group of non-selective agents do not have the ability to select adrenergic receptors for blocking. They affect all structures.

Such an effect on the body manifests itself in the form of a decrease in blood clotting and a decrease in the number of plaques, the level of pressure in the blood vessels also decreases, the rhythm of myocardial contractions normalizes, and cell membranes stabilize.

The most popular drugs among non-selective beta-blockers are:

  • Sandinorm;
  • Vistagen;
  • Korgard;
  • Vistagan;
  • Trazikor;
  • Whisken;
  • Sotalex;
  • Okumol;
  • Obzidan.

The cost of these drugs is very diverse and varies from 50r. up to 1000r. for packing.

Selective beta-blockers work purposefully on a certain type of receptor. The second name of this group is cardioselective. Blocked receptors are located in myocardial cells, lipoid tissue, and also in the intestine.

The representatives of the selective group are:

  • metoprolol;
  • Tenormin;
  • Esmolol;
  • Coriol;
  • Nebicor;
  • Cordanum;
  • Vasacor;
  • Acecor.

The cost of drugs in pharmacies is varied. It depends on the manufacturer, the concentration of the active ingredient, as well as the number of tablets in the package.

Domestic drugs are much cheaper than foreign counterparts. Their cost, as a rule, does not exceed 250 rubles. Foreign funds have a price above 500 rubles.

In addition to selectivity, the classification can be based on the progressiveness and novelty of the drug. Thus, among the drugs of the beta-blocker group, 3 generations are distinguished.

The 1st generation of drugs is characterized by non-selectivity of action. These include:

  • propranolol;
  • Sotalol;
  • Timolol.

The 2nd generation of drugs of the beta-blocker group includes selective drugs:

  • metoprolol;
  • Esmolol.

The 3rd generation of drugs combines the means of selective and non-selective effects:

  • Talinolol;
  • Celiprolol;
  • Karteolol.

Currently, it is the 3rd generation drugs that are most often used. They differ in the least number of contraindications and.

However, you can not choose your own medicine. This can only be done by the attending physician based on the results of a general examination of the body.

The highest quality and most effective beta blocker

The group of beta-blockers of the 3rd generation occupies a leading position in terms of the effectiveness of action. This is the most modern and progressive type of drugs that act on adrenoreceptors.

The best among them are drugs under the trade name, as well.

Carvedilol is a selective drug. During its administration, there is an effective decrease in the level of pressure in the blood vessels due to the expansion of the lumen, and the number of plaques also decreases.

- combines 2 types of action. It effectively reduces blood pressure and also helps in the fight against heart disease. Nebivolol is more expensive than Carvediol.

How Beta Blockers Affect Blood Pressure

Beta-blockers block the work of special adrenoreceptors in the body, which are located in the cells of the heart muscle tissue, liver, adipose tissue, etc. As a result of a decrease in the activity of receptors, the following changes occur in the body:

  • the rhythm of heart contractions slows down somewhat and myocardial cells require less oxygen;
  • the process of blood flow in the coronary region is normalized and high-quality nutrition of the heart muscle occurs;
  • the substance renin is produced, which reduces peripheral resistance;
  • special active biological substances are produced that expand the vascular lumen;
  • cell membranes become less permeable to sodium and potassium ions.

All of these processes occur almost simultaneously, due to this, a decrease in blood pressure occurs. Additionally, the effect of normalization of the heart rate and myocardial function is noted.

Instructions for use

The duration of the course of administration, dosage of drugs and the general treatment regimen is determined. In order for therapy to be effective, it must be taken into account general state the patient's body, whether there are any contraindications.

In addition, regular monitoring of the patient's condition is carried out. If side effects are detected, the doctor replaces the medication with similar ones.

During the entire treatment, it is necessary to monitor the readings of blood pressure and heart rate. Even with minor deviations from the norm, you should immediately consult a doctor to adjust the treatment.

Side effects

In some cases, beta-blocker therapy is accompanied by negative side effects:

  • feeling chronic fatigue and increased fatigue;
  • violation of the rhythm of heart contractions in the direction of slowing down;
  • increased asthmatic manifestations;
  • intoxication of the body, which is manifested by nausea and concomitant vomiting;
  • decrease in the concentration of glucose in the blood;
  • excessive pressure drop in the vessels;
  • pathological changes in metabolic processes;
  • increased symptoms of lung disease;
  • impaired concentration;
  • dyspeptic disorders of the digestive system;
  • decreased sexual desire;
  • the development of inflammatory processes on the mucous membrane of the eyes;
  • allergic rashes over the entire area of ​​​​the skin;
  • circulatory disorders in the limbs.

If side effects appear during therapy with these drugs, then the drug is stopped taking. The doctor selects more suitable analogues.

Contraindications

  • asthma;
  • individual intolerance to the components of a particular medicinal product;
  • pathology of the heart rhythm in the form of a decrease in the number of contractions;
  • violation of the impulse from the atrium to the ventricle;
  • insufficient work of the left ventricle;
  • vascular diseases;
  • low blood pressure.

In addition, beta-blockers should not be taken during pregnancy and during its planning period.

Overdose

If beta-blockers are taken incorrectly, the recommended dosages and duration of treatment are exceeded, an overdose phenomenon may occur. It is accompanied by the following symptomatic manifestations:

  • severe dizziness;
  • heart rhythm disturbances;
  • a sharp decrease in heart rate;
  • blueing of the skin;
  • convulsions;
  • coma.

If drug poisoning occurs against the background of an overdose, then it is necessary to provide first aid as soon as possible. medical care to the victim. It includes:

  1. washing the patient's stomach;
  2. taking absorbent drugs;
  3. emergency call.

Depending on the symptoms, the patient may be prescribed different drugs to normalize the condition. If the heart rhythm is disturbed, the victim is given atropine, adrenaline or dopamine, depending on the characteristics of the pathology.

Difference from alpha blockers

All drugs that inhibit and block the activity of adrenoreceptors are divided into the following groups:

  • beta blockers.

Drugs of the alpha group act on the corresponding receptors. Their influence is aimed at simplifying the process of blood flow, which in turn reduces the level of pressure in the vessels. An additional effect when taking alpha-blockers can be considered a decrease in cholesterol levels.

Drugs that have the effect of stimulating beta-adrenergic systems are a group of drugs called.

Adrenoblockers were officially recognized and introduced into medical practice in the middle of the twentieth century.

Since then, this class of antiadrenergic substances has been widely and successfully used as antihypertensive, antianginal and other drugs.

However, the features of the pharmacological activity of beta-blockers cause a number of restrictions in their appointment due to the presence of contraindications and the possibility of side effects.

Adrenolytics block the process of nerve impulse transmission by binding to adrenoreceptors instead of catecholamines.

Beta-blockers specifically inhibit the effects of sympathetic nerve impulses and sympathomimetic substances on beta-adrenergic receptors.

Due to the chemical structure, the binding of beta-blockers to receptors causes not a stimulating, but an inhibitory effect.

The combination of physicochemical properties of different drugs from this group provides various features influence. Beta-blockers are antagonists, when interacting with receptors, they produce an inhibitory effect.

A number of substances combine an antagonistic action with an agonistic one, additionally exerting some stimulating effect. Antagonists slow down heart rate, weaken the force of heart contractions, inhibit automatism and slow down conduction due to the blockade of nerve transmission.

Cardioselective beta-blocker Atenolol

A drug with a joint effect will not affect or even slightly increase it. These drugs differ in the selectivity of their effects on beta 1- or beta 2-adrenergic receptors.

Drugs that specifically bind beta 1 receptors of the heart muscle are considered cardioselective (,).

Others simultaneously act on both types of receptors - cardiac beta 1-adrenergic receptors and beta 2-adrenergic receptors of the bronchi, pancreas, small vessels (Propranolol), due to which the development of bronchospasm may be a concomitant result of exposure to non-selective blockers.

There are drugs with a combined effect on both types of adrenergic receptors - alpha and beta ().

Depending on the solubility in media, adrenolytics are lipophilic (Nebivolol), hydrophilic (Atenolol) and with combined solubility in water and lipids (Bisoprolol).

Beta-blockers have local anesthetic and antiarrhythmic effects on the heart. Due to the antianginal effect of the heart muscle, it needs less oxygen. The mechanism of antiarrhythmic effect is due to the elimination of arrhythmogenic sympathetic action on the conduction system of the heart.

The hypotensive effect is associated with a number of mechanisms: the volume of cardiac output is reduced, the sensitivity of baroreceptors decreases, and the work of the renin-angiotensin system is inhibited to some extent.

Beta-blockers also have a number of other effects:

  • inhibit the work of the central nervous system;
  • stimulate the contractility of the uterus;
  • reduce intraocular pressure;
  • interfere with the formation of glucose in the body;
  • cause vasoconstriction;
  • contribute to the development of insulin resistance, etc.

The variety of effects explains the side effects of beta-blockers and contraindications to their use, which must be considered when using them. In the treatment of cardiac diseases, highly selective drugs should be preferred.

It is necessary to take into account the fact that the selectivity of the effect is not one hundred percent, in high doses and cardioselective blockers can block beta 2-adrenergic receptors, causing serious undesirable effects.

Contraindications for the use of beta-blockers

In the following diseases and conditions, beta-blockers are contraindicated:

  • sinus;
  • intraventricular block incomplete or complete;
  • severe heart failure;
  • bronchial asthma and other pulmonary diseases with obstructive syndrome;
  • significant violations of peripheral arterial blood flow;
  • individual intolerance.

Careful prescription of drugs in this group is required for moderate disorders of peripheral arterial blood flow, COPD without bronchial obstruction, and depressive states.

Side effects of beta blockers

Taking medications may be accompanied by the development of unwanted reactions.

The main side effects when using beta-blockers are directly related to their adrenolytic action:

  • increased fatigue, sleep disturbances, depressive states due to the effect on the central nervous system;
  • bradycardia, blockade of intracardiac conduction are explained by the blockade of adrenergic receptors of the heart;
  • bronchospasm due to blocking of bronchial adrenoreceptors;
  • , vomiting, diarrhea, and due to intoxication of the body from the accumulation of the drug (with impaired liver function);
  • hypoglycemia due to the suppression of glucose synthesis and the formation of insulin resistance;
  • , Raynaud's syndrome, allergic reactions, etc.

It is possible to minimize the side effects of beta-blockers by carefully selecting the appropriate drug at the optimal dosage, because the sensitivity to treatment in patients is extremely individual.

So, to avoid unwanted effects on the central nervous system, it is possible to prefer water-soluble beta-blockers instead of fat-soluble ones that are not able to penetrate into the central nervous system.

It is possible to prevent the development of bronchial obstruction by prescribing the minimum initial dose of the drug with a slow increase until the optimal amount of the drug is reached.

Application during pregnancy

Beta-blockers should not be taken during pregnancy.

These drugs can adversely affect the fetus through indirect and direct effects.

It is directly related to the entry of the drug into the bloodstream of the fetus and the implementation of a toxic effect on it: there is a high probability of slowing the heart rate, developing hypoglycemia, and inhibiting the functions of the central nervous system.

The use of beta-blockers during pregnancy is justified only in case of severe cardiac pathology in small doses and under the constant supervision of doctors in a hospital setting.

Indirectly, beta-blockers act on the fetus through a decrease in uteroplacental blood flow, which can manifest as a delay in fetal development, especially when taking drugs in the 1st and 2nd trimester of pregnancy. They also have the property to increase the tone of the uterus and lead to the development of vasoconstriction.

Use in diabetes

The basis of the treatment of chronic heart failure, along with other drugs, is the use of beta-blockers.

Limiting the use of beta-blockers works if the patient has diabetes mellitus due to the potential risk of developing a hypoglycemic state.

This effect is especially characteristic of non-selective beta-blockers.

The drugs inhibit the formation of glucose in the body, contribute to a decrease in insulin sensitivity and mask the clinic of a hypoglycemic state.

The use of beta-blockers against the background of diabetes mellitus should take place with a preference for highly selective, regular monitoring of the amount of blood glucose and, if necessary, with dose adjustment of the hypoglycemic agent.

Beta blockers and erectile dysfunction

When taking beta-blockers, an adverse effect on potency is observed - sexual function is inhibited, up to impotence in 1% of cases.

The exact mechanism of this effect has not been elucidated. The presumptive cause is the inhibitory effect of beta-blockers on the central nervous system, on the hormonal background and on the cavernous bodies.

However, not every drug from this group is accompanied by the appearance of this unwanted effect, which creates the possibility of choosing beta-blockers instead of not using them.

Related videos

About the mechanism of action and the use of beta-blockers in the video:

Beta-blockers have a wide range of contraindications and adverse reactions, the fear of which reduces the scope of their use. As a result, patients who have direct indications for the appointment of blockers do not receive these drugs.

Careful and gentle selection of the optimal beta-blocker in the optimal dose, taking into account concomitant disorders, will increase the frequency of their use in cardiac diseases and minimize adverse reactions.

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The site provides background information for informational purposes only. Diagnosis and treatment of diseases should be carried out under the supervision of a specialist. All drugs have contraindications. Expert advice is required!

Adrenoblockers are a group of drugs united by a common pharmacological action - the ability to neutralize the adrenaline receptors of blood vessels and the heart. That is, adrenoblockers "turn off" receptors that normally respond to adrenaline and norepinephrine. Accordingly, the effects of blockers are completely opposite to those of adrenaline and norepinephrine.

general characteristics

Adrenoblockers act on adrenoreceptors, which are located in the walls of blood vessels and in the heart. Actually, this group of drugs got its name precisely from the fact that they block the action of adrenoreceptors.

Normally, when adrenergic receptors are free, they can be affected by adrenaline or noradrenaline that appears in the bloodstream. Adrenaline, when bound to adrenoreceptors, provokes the following effects:

  • Vasoconstrictor (dramatically narrows the lumen of the blood vessels);
  • Hypertensive (increased blood pressure);
  • Antiallergic;
  • Bronchodilator (expands the lumen of the bronchi);
  • Hyperglycemic (increases blood glucose levels).
Drugs of the group of adrenergic blockers, as it were, turn off adrenoreceptors and, accordingly, have an effect that is directly opposite to adrenaline, that is, they dilate blood vessels, lower blood pressure, narrow the lumen of the bronchi and reduce the level of glucose in the blood. Naturally, these are the most common effects of adrenergic blockers, inherent in all drugs of this type without exception. pharmacological group.

Classification

There are four types of adrenergic receptors in the walls of blood vessels - alpha-1, alpha-2, beta-1 and beta-2, which are usually called respectively: alpha-1 adrenoreceptors, alpha-2 adrenoreceptors, beta-1 adrenergic receptors and beta -2-adrenergic receptors. Adrenoblocker drugs can turn off different kinds receptors, for example, only beta-1-adrenergic receptors or alpha-1,2-adrenergic receptors, etc. Adrenoblockers are divided into several groups depending on which types of adrenergic receptors they turn off.

So, adrenoblockers are classified into the following groups:

1. Alpha blockers:

  • Alpha-1-blockers (alfuzosin, doxazosin, prazosin, silodosin, tamsulosin, terazosin, urapidil);
  • Alpha-2 blockers (yohimbine);
  • Alpha-1,2-blockers (nicergoline, phentolamine, proroxan, dihydroergotamine, dihydroergocristine, alpha-dihydroergocriptine, dihydroergotoxin).
2. Beta blockers:
  • Beta-1,2-blockers (also called non-selective) - bopindolol, metipranolol, nadolol, oxprenolol, pindolol, propranolol, sotalol, timolol;
  • Beta-1-blockers (also called cardioselective or simply selective) - atenolol, acebutolol, betaxolol, bisoprolol, metoprolol, nebivolol, talinolol, celiprolol, esatenolol, esmolol.
3. Alpha beta blockers (both alpha and beta adrenoreceptors are turned off at the same time) - butylmethyloxadiazole (proxodolol), carvedilol, labetalol.

This classification contains international titles active substances included in the composition of drugs belonging to each group of adrenoblockers.

Each group of beta-blockers is also divided into two types - with internal sympathomimetic activity (ISA) or without ICA. However, this classification is auxiliary, and is necessary only for doctors to select the optimal drug.

Adrenoblockers - list

We give lists of drugs for each group of adrenergic blockers (alpha and beta) separately in order to avoid confusion. In all lists, first indicate the name of the active substance (INN), and then below - the commercial names of the drugs that include this active ingredient.

Alpha-adrenergic blockers

Here are the lists of alpha-blockers of various subgroups in different lists for the most easy and structured search for the necessary information.

To the drugs of the group of alpha-1-adrenergic blockers include the following:

1. Alfuzosin (INN):

  • Alfuprost MR;
  • Alfuzosin;
  • Alfuzosin hydrochloride;
  • Dalphaz;
  • Dalphaz Retard;
  • Dalfaz SR.
2. Doxazosin (INN):
  • Artezin;
  • Artezin Retard;
  • doxazosin;
  • Doxazosin Belupo;
  • Doxazosin Zentiva;
  • Doxazosin Sandoz;
  • Doxazosin-ratiopharm;
  • Doxazosin Teva;
  • doxazosin mesylate;
  • Zokson;
  • Kamiren;
  • Kamiren HL;
  • Cardura;
  • Cardura Neo;
  • Tonocardin;
  • Urocard.
3. Prazosin (INN):
  • Polpressin;
  • Prazosin.
4. Silodosin (INN):
  • Urorek.
5. Tamsulosin (INN):
  • Hyperprost;
  • Glansin;
  • Miktosin;
  • Omnic Okas;
  • Omnic;
  • Omsulosin;
  • Proflosin;
  • Sonizin;
  • Tamzelin;
  • Tamsulosin;
  • Tamsulosin Retard;
  • Tamsulosin Sandoz;
  • Tamsulosin-OBL;
  • Tamsulosin Teva;
  • Tamsulosin hydrochloride;
  • Tamsulon FS;
  • Taniz ERAS;
  • Taniz K;
  • Tulosin;
  • Focusin.
6. Terazosin (INN):
  • Cornam;
  • Setegis;
  • Terazosin;
  • Terazosin Teva;
  • Khaitrin.
7. Urapidil (INN):
  • Urapidil Carino;
  • Ebrantil.
To the drugs of the group of alpha-2-adrenergic blockers include Yohimbine and Yohimbine hydrochloride.

To the drugs of the group of alpha-1,2-adrenergic blockers include the following drugs:

1. Dihydroergotoxin (mixture of dihydroergotamine, dihydroergocristine and alpha-dihydroergocriptine):

  • Redergin.
2. Dihydroergotamine:
  • Ditamine.
3. Nicergoline:
  • Nilogrin;
  • Nicergoline;
  • Nicergolin-Ferein;
  • Sermion.
4. Proroxan:
  • Pyrroxane;
  • Proroxan.
5. Phentolamine:
  • Phentolamine.

Beta blockers - list

Since each group of beta-blockers includes a fairly large number of drugs, we will list them separately for easier perception and searching for the necessary information.

Selective beta-blockers (beta-1-blockers, selective blockers, cardioselective blockers). The generally accepted names of this pharmacological group of adrenergic blockers are listed in brackets.

So, selective beta-blockers include the following drugs:

1. Atenolol:

  • Atenobene;
  • Atenova;
  • Atenol;
  • Athenolan;
  • Atenolol;
  • Atenolol-Agio;
  • Atenolol-AKOS;
  • Atenolol-Acre;
  • Atenolol Belupo;
  • Atenolol Nycomed;
  • Atenolol-ratiopharm;
  • Atenolol Teva;
  • Atenolol UBF;
  • Atenolol FPO;
  • Atenolol Stada;
  • Atenosan;
  • Betacard;
  • Velorin 100;
  • Vero-Atenolol;
  • Ormidol;
  • Prinorm;
  • Sinar;
  • Tenormin.
2. Acebutolol:
  • Acecor;
  • Sektral.
3. Betaxolol:
  • Betak;
  • Betaxolol;
  • Betalmic EU;
  • Betoptik;
  • Betoptik C;
  • Betoftan;
  • Xonef;
  • Xonef BK;
  • Lokren;
  • Optibetol.
4. Bisoprolol:
  • Aritel;
  • Aritel Core;
  • Bidop;
  • Bidop Kor;
  • Biol;
  • Biprol;
  • Bisogamma;
  • Bisocard;
  • Bisomore;
  • bisoprolol;
  • Bisoprolol-OBL;
  • Bisoprolol LEXVM;
  • Bisoprolol Lugal;
  • Bisoprolol Prana;
  • Bisoprolol-ratiopharm;
  • Bisoprolol C3;
  • Bisoprolol Teva;
  • bisoprolol fumarate;
  • Concor Core;
  • Corbis;
  • Cordinorm;
  • Cordinorm Core;
  • Coronal;
  • Niperten;
  • Tirez.
5. Metoprolol:
  • Betaloc;
  • Betaloc ZOK;
  • Vasocordin;
  • Corvitol 50 and Corvitol 100;
  • Metozok;
  • Metocard;
  • Metokor Adifarm;
  • Metolol;
  • metoprolol;
  • Metoprolol Acry;
  • Metoprolol Akrikhin;
  • Metoprolol Zentiva;
  • Metoprolol Organic;
  • Metoprolol OBL;
  • Metoprolol-ratiopharm;
  • metoprolol succinate;
  • metoprolol tartrate;
  • Serdol;
  • Egilok Retard;
  • Egilok C;
  • Emzok.
6. Nebivolol:
  • Bivotens;
  • Binelol;
  • Nebivator;
  • Nebivolol;
  • Nebivolol NANOLEK;
  • Nebivolol Sandoz;
  • Nebivolol Teva;
  • Nebivolol Chaikapharma;
  • Nebivolol STADA;
  • Nebivolol hydrochloride;
  • Nebicor Adifarm;
  • Nebilan Lannacher;
  • non-ticket;
  • Nebilong;
  • OD-Neb.


7. Talinolol:

  • Kordanum.
8. Celiprolol:
  • Celiprol.
9. Esatenolol:
  • Estekor.
10. Esmolol:
  • Breviblock.
Non-selective beta-blockers (beta-1,2-blockers). This group includes the following medications:

1. Bopindolol:

  • Sandonorm.
2. Metipranolol:
  • trimepranol.
3. Nadolol:
  • Korgard.
4. Oxprenolol:
  • Trazikor.
5. Pindolol:
  • Whisken.
6. Propranolol:
  • Anaprilin;
  • Vero-Anaprilin;
  • Inderal;
  • Inderal LA;
  • obzidan;
  • propranobene;
  • propranolol;
  • Propranolol Nycomed.
7. Sotalol:
  • Darob;
  • SotaGEKSAL;
  • Sotalex;
  • Sotalol;
  • Sotalol Canon;
  • Sotalol hydrochloride.
8. Timolol:
  • Arutimol;
  • Glaumol;
  • Glautam;
  • Cusimolol;
  • Niolol;
  • Okumed;
  • Okumol;
  • Okupres E;
  • Optimol;
  • Oftan Timogel;
  • Oftan Timolol;
  • Oftensin;
  • TimoGEKSAL;
  • Thymol;
  • Timolol;
  • Timolol AKOS;
  • Timolol Betalek;
  • Timolol Bufus;
  • Timolol DIA;
  • Timolol LENS;
  • Timolol MEZ;
  • Timolol POS;
  • Timolol Teva;
  • Timolol maleate;
  • Timollong;
  • Timoptic;
  • Timoptic Depot.

Alpha-beta-blockers (drugs that turn off both alpha and beta adrenoceptors)

The drugs in this group include the following:

1. Butylmethyloxadiazole:

  • Albetor;
  • Albetor Long;
  • Butylmethyloxadiazole;
  • Proxodolol.
2. Carvedilol:
  • Acridilol;
  • Bagodilol;
  • Vedicardol;
  • Dilatrend;
  • Karvedigamma;
  • Carvedilol;
  • Carvedilol Zentiva;
  • Carvedilol Canon;
  • Carvedilol Obolensky;
  • Carvedilol Sandoz;
  • Carvedilol Teva;
  • Carvedilol STADA;
  • Carvedilol-OBL;
  • Carvedilol Pharmaplant;
  • Carvenal;
  • Carvetrend;
  • Carvidil;
  • Cardivas;
  • Coriol;
  • Credex;
  • Recardium;
  • Talliton.
3. Labetalol:
  • Abetol;
  • Amipress;
  • Labetol;
  • Trandol.

Beta-2 blockers

There are currently no drugs that turn off only beta-2-adrenergic receptors in isolation. Previously, the drug Butoxamine, which is a beta-2-blocker, was produced, but today it is not used in medical practice and is of interest exclusively to experimental scientists specializing in pharmacology, organic synthesis, etc.

There are only non-selective beta-blockers that simultaneously turn off both beta-1 and beta-2 adrenergic receptors. However, since there are also selective blockers that turn off exclusively beta-1-adrenergic receptors, non-selective ones are often called beta-2-blockers. This name is incorrect, but quite widespread in everyday life. Therefore, when they say "beta-2-blockers", you need to know what is meant by the group of non-selective beta-1,2-blockers.

Action

Since the shutdown of various types of adrenergic receptors leads to the development of generally common, but different in some aspects, effects, we will consider the effect of each type of adrenergic blockers separately.

The action of alpha-blockers

Alpha-1-blockers and alpha-1,2-blockers have the same pharmachologic effect. And the drugs of these groups differ from each other in side effects, which are usually greater in alpha-1,2-blockers, and they occur more often compared to alpha-1-blockers.

So, drugs of these groups dilate the vessels of all organs, and especially strongly skin, mucous membranes, intestines and kidneys. Due to this, the total peripheral vascular resistance decreases, blood flow and blood supply to peripheral tissues improves, and blood pressure decreases. By reducing peripheral vascular resistance and reducing the amount of blood that returns to the atria from the veins (venous return), the pre- and afterload on the heart is significantly reduced, which greatly facilitates its work and positively affects the state of this organ. Summarizing the above, we can conclude that alpha-1-blockers and alpha-1,2-blockers have the following effect:

  • Reduce blood pressure, reduce total peripheral vascular resistance and afterload on the heart;
  • Expand small veins and reduce the preload on the heart;
  • Improve blood circulation both throughout the body and in the heart muscle;
  • Improve the condition of people suffering from chronic heart failure, reducing the severity of symptoms (shortness of breath, pressure surges, etc.);
  • Reduce pressure in the pulmonary circulation;
  • Reduce the level of total cholesterol and low-density lipoprotein (LDL), but increase the content of high-density lipoprotein (HDL);
  • They increase the sensitivity of cells to insulin, so that glucose is used faster and more efficiently, and its concentration in the blood decreases.
Due to these pharmacological effects, alpha-blockers reduce blood pressure without the development of a reflex heartbeat, and also reduce the severity of left ventricular hypertrophy. The drugs effectively lower isolated elevated systolic pressure (first digit), including those associated with obesity, hyperlipidemia, and reduced glucose tolerance.

In addition, alpha-blockers reduce the severity of symptoms of inflammatory and obstructive processes in the genitourinary organs caused by prostatic hyperplasia. That is, the drugs eliminate or reduce the severity of incomplete emptying of the bladder, nighttime urination, frequent urination, and burning during urination.

Alpha-2 blockers have little effect on blood vessels internal organs, including the heart, they affect mainly the vascular system of the genital organs. That is why alpha-2-blockers have a very narrow scope - the treatment of impotence in men.

The action of non-selective beta-1,2-blockers

  • Reduce heart rate;
  • Reduce blood pressure and moderately reduce the total peripheral vascular resistance;
  • Reduce myocardial contractility;
  • Reduce the need of the heart muscle for oxygen and increase the resistance of its cells to oxygen starvation (ischemia);
  • Reduce the degree of activity of foci of excitation in the conduction system of the heart and, thereby, prevent arrhythmias;
  • Reduce the production of renin by the kidneys, which also leads to a decrease in blood pressure;
  • On the early stages applications increase the tone of blood vessels, but then it decreases to normal or even lower;
  • Prevent platelets from sticking together and forming blood clots;
  • Improve the return of oxygen from red blood cells to the cells of organs and tissues;
  • Strengthen the contraction of the myometrium (the muscle layer of the uterus);
  • Increase the tone of the bronchi and esophageal sphincter;
  • Strengthen the motility of the digestive tract;
  • Relax the bladder detrusor;
  • Slow down the formation of active forms of thyroid hormones in peripheral tissues (only some beta-1,2-blockers).
Due to these pharmacological effects, non-selective beta-1,2-blockers reduce the risk of re-infarction and sudden cardiac death by 20-50% in people with coronary artery disease or heart failure. In addition, with coronary artery disease, drugs of this group reduce the frequency of angina attacks and pain in the heart, improve the tolerance of physical, mental and emotional stress. In hypertension, drugs in this group reduce the risk of coronary artery disease and stroke.

In women, non-selective beta-blockers increase uterine contractility and reduce blood loss during childbirth or after surgery.

In addition, due to the effect on the vessels of peripheral organs, non-selective beta-blockers reduce intraocular pressure and reduce the production of moisture in the anterior chamber of the eye. This action of drugs is used in the treatment of glaucoma and other eye diseases.

The action of selective (cardioselective) beta-1-blockers

The drugs of this group have the following pharmacological effects:
  • Reduce the heart rate (HR);
  • Reduce the automatism of the sinus node (pacemaker);
  • Inhibit impulse conduction through the atrioventricular node;
  • Reduce contractility and excitability of the heart muscle;
  • Reduce the heart's need for oxygen;
  • Suppress the effects of adrenaline and norepinephrine on the heart under conditions of physical, mental or emotional stress;
  • Reduce blood pressure;
  • Normalize heartbeat with arrhythmias;
  • Limit and counteract the spread of the damage zone in myocardial infarction.
Due to these pharmacological effects, selective beta-blockers reduce the amount of blood ejected by the heart into the aorta per contraction, reduce blood pressure and prevent orthostatic tachycardia (rapid heartbeat in response to a sudden transition from sitting or lying to standing). Also, drugs slow down the heart rate and reduce their strength by reducing the heart's need for oxygen. In general, selective beta-1-blockers reduce the frequency and severity of CAD attacks, improve exercise tolerance (physical, mental, and emotional), and significantly reduce mortality in people with heart failure. These effects of drugs lead to a significant improvement in the quality of life of people suffering from coronary artery disease, dilated cardiomyopathy, as well as those who have had myocardial infarction and stroke.

In addition, beta-1-blockers eliminate arrhythmia and narrowing of the lumen of small vessels. In people suffering from bronchial asthma, they reduce the risk of bronchospasm, and in diabetes mellitus, they reduce the likelihood of developing hypoglycemia (low blood sugar).

The action of alpha-beta-blockers

The drugs of this group have the following pharmacological effects:
  • Reduce blood pressure and reduce total peripheral vascular resistance;
  • Reduce intraocular pressure in open-angle glaucoma;
  • Normalize lipid profile indicators (reduce the level of total cholesterol, triglycerides and low density lipoproteins, but increase the concentration of high density lipoproteins).
Due to these pharmacological effects, alpha-beta-blockers have a powerful hypotensive effect (reduce blood pressure), dilate blood vessels and reduce afterload on the heart. Unlike beta-blockers, drugs of this group reduce blood pressure without changing renal blood flow and without increasing the total peripheral vascular resistance.

In addition, alpha-beta-blockers improve myocardial contractility, due to which blood does not remain in the left ventricle after contraction, but is ejected in full into the aorta. This helps to reduce the size of the heart and reduces the degree of its deformation. By improving the work of the heart, the drugs of this group in congestive heart failure increase the severity and volume of endured physical, mental and emotional stress, reduce the frequency of heart contractions and IHD attacks, and also normalize the cardiac index.

The use of alpha-beta-blockers reduces mortality and the risk of re-infarction in people with coronary artery disease or dilated cardiomyopathy.

Application

Consider the indications and scope of various groups of adrenergic blockers separately in order to avoid confusion.

Indications for the use of alpha-blockers

Since the drugs of subgroups of alpha-blockers (alpha-1, alpha-2 and alpha-1.2) have different mechanisms of action and differ somewhat from each other in the nuances of the effect on the vessels, their scope and, accordingly, the indications are also different.

Alpha-1-adrenergic blockers indicated for use in the following conditions and diseases:

  • Hypertension (to lower blood pressure);
  • Benign prostatic hyperplasia.
Alpha-1,2-blockers are indicated for use if a person has the following conditions or diseases:
  • Peripheral circulatory disorders (for example, Raynaud's disease, endarteritis, etc.);
  • Dementia (dementia) due to the vascular component;
  • Vertigo and disorders of the vestibular apparatus due to the vascular factor;
  • Diabetic angiopathy;
  • Dystrophic diseases of the cornea of ​​the eye;
  • Optic neuropathy due to its ischemia (oxygen starvation);
  • prostatic hypertrophy;
  • Disorders of urination against the background of a neurogenic bladder.
Alpha-2 blockers used exclusively for the treatment of impotence in men.

The use of beta-blockers (indications)

Selective and non-selective beta-blockers have slightly different indications and applications, due to differences in certain nuances of their effect on the heart and blood vessels.

Indications for the use of non-selective beta-1,2-blockers the following:

  • Arterial hypertension ;
  • Angina pectoris;
  • Sinus tachycardia;
  • Prevention of ventricular and supraventricular arrhythmias, as well as bigeminy, trigeminy;
  • Mitral valve prolapse;
  • myocardial infarction;
  • Prevention of migraine;
  • Increased intraocular pressure.
Indications for the use of selective beta-1-blockers. This group blockers are also called cardioselective, because they mainly affect the heart, and to a much lesser extent on the vessels and blood pressure.

Cardioselective beta-1-blockers are indicated for use if a person has the following diseases or conditions:

  • Arterial hypertension of moderate or low severity;
  • Coronary artery disease;
  • Hyperkinetic cardiac syndrome;
  • Various types of arrhythmias (sinus, paroxysmal, supraventricular tachycardia, extrasystole, flutter or atrial fibrillation, atrial tachycardia);
  • Hypertrophic cardiomyopathy;
  • Mitral valve prolapse;
  • Myocardial infarction (treatment of a heart attack that has already occurred and prevention of a second one);
  • Prevention of migraine;
  • Neurocirculatory dystonia of hypertonic type;
  • IN complex therapy pheochromocytoma, thyrotoxicosis and tremor;
  • Akathisia provoked by the use of neuroleptics.

Indications for the use of alpha-beta-blockers

Preparations of this group are indicated for use if a person has the following conditions or diseases:
  • Arterial hypertension;
  • stable angina;
  • Chronic heart failure (as part of combination therapy);
  • Arrhythmia;
  • Glaucoma (the drug is administered in the form of eye drops).

Side effects

Let us consider the side effects of adrenoblockers of different groups separately, since, despite the similarities, there are a number of differences between them.

All alpha-blockers are capable of provoking both the same and different side effects, which is due to the peculiarities of their effect on certain types of adrenergic receptors.

Side effects of alpha blockers

So, all alpha blockers (alpha-1, alpha-2 and alpha-1.2) provoke the following side effects:
  • Headache;
  • Orthostatic hypotension (a sharp decrease in pressure when moving to a standing position from a sitting or lying position);
  • Syncope (short-term fainting);
  • nausea or vomiting;
  • Constipation or diarrhea.
Besides, alpha-1-blockers may cause the following side effects in addition to those listed above characteristic for all groups of adrenoblockers:
  • Hypotension (severe decrease in blood pressure);
  • Tachycardia (palpitations);
  • Arrhythmia;
  • Dyspnea;
  • Blurred vision (fog before the eyes);
  • xerostomia;
  • Feeling of discomfort in the abdomen;
  • Violations cerebral circulation;
  • Decreased libido;
  • Priapism (prolonged painful erections);
  • Allergic reactions (rash, skin itching, urticaria, Quincke's edema).
Alpha-1,2-blockers, in addition to those common to all blockers, can provoke the following side effects:
  • arousal;
  • Cold extremities;
  • An attack of angina pectoris;
  • Increased acidity of gastric juice;
  • ejaculation disorder;
  • Pain in limbs;
  • Allergic reactions (redness and itching of the upper half of the body, urticaria, erythema).
Side effects of alpha-2 blockers, in addition to those common to all blockers, are as follows:
  • Tremor;
  • Excitation;
  • Irritability;
  • Increased blood pressure;
  • Tachycardia;
  • Increased motor activity;
  • Abdominal pain;
  • Priapism;
  • Decreased frequency and amount of urination.

Beta-blockers - side effects

Selective (beta-1) and non-selective (beta-1,2) blockers have both the same side effects and different ones, due to the peculiarities of their effect on different types of receptors.

So, the same for selective and non-selective beta-blockers are the following side effects:

  • Dizziness;
  • Headache;
  • Drowsiness;
  • Insomnia;
  • Nightmares;
  • fatigue;
  • Weakness;
  • Anxiety;
  • confusion;
  • Brief episodes of memory loss;
  • Reaction slowdown;
  • Paresthesia (feeling of running "goosebumps", numbness of the limbs);
  • Violation of vision and taste;
  • Dryness oral cavity and eye;
  • bradycardia;
  • palpitations;
  • atrioventricular block;
  • Violation of conduction in the heart muscle;
  • Arrhythmia;
  • Deterioration of myocardial contractility;
  • Hypotension (lowering blood pressure);
  • Heart failure;
  • Raynaud's phenomenon;
  • Pain in the chest, muscles and joints;
  • Thrombocytopenia (a decrease in the total number of platelets in the blood below normal);
  • Agranulocytosis (lack of neutrophils, eosinophils and basophils in the blood);
  • Nausea and vomiting;
  • Abdominal pain;
  • diarrhea or constipation;
  • Liver disorders;
  • Dyspnea;
  • Spasm of the bronchi or larynx;
  • Allergic reactions (skin itching, rash, redness);
  • sweating;
  • Cold extremities;
  • muscle weakness;
  • Deterioration of libido;
  • Increase or decrease in the activity of enzymes, the level of bilirubin and glucose in the blood.
Non-selective beta-blockers (beta-1,2), in addition to the above, can also provoke the following side effects:
  • eye irritation;
  • Diplopia (double vision);
  • Nasal congestion;
  • respiratory failure;
  • Collapse;
  • Exacerbation of intermittent claudication;
  • Temporary disorders of cerebral circulation;
  • cerebral ischemia;
  • fainting;
  • Decrease in the level of hemoglobin in the blood and hematocrit;
  • Quincke's edema;
  • Change in body weight;
  • lupus syndrome;
  • Impotence;
  • Peyronie's disease;
  • Thrombosis of the mesenteric artery of the intestine;
  • Colitis;
  • Increased levels of potassium, uric acid and triglycerides in the blood;
  • Blurred and decreased visual acuity, burning, itching and foreign body sensation in the eyes, lacrimation, photophobia, corneal edema, eyelid margin inflammation, keratitis, blepharitis and keratopathy (eye drops only).

Side effects of alpha-beta blockers

Side effects of alpha-beta blockers include some of the side effects of both alpha and beta blockers. However, they are not identical to the side effects of alpha-blockers and beta-blockers, since the set of symptoms of side effects is completely different. So, alpha-beta blockers have the following side effects:
  • Dizziness;
  • Headache;
  • Asthenia (feeling of fatigue, loss of strength, indifference, etc.);
  • Syncope (short-term fainting);
  • muscle weakness;
  • General weakness and fatigue;
  • sleep disorders;
  • Depression;
  • Paresthesia (feeling of running "goosebumps", numbness of the limbs, etc.);
  • xerophthalmia (dry eye);
  • Decreased production of tear fluid;
  • bradycardia;
  • Violation of atrioventricular conduction up to blockade;
  • Hypotension is postural;
  • Pain in the chest, abdomen and limbs;
  • angina;
  • Deterioration of peripheral circulation;
  • Aggravation of the course of heart failure;
  • Exacerbation of Raynaud's syndrome;
  • swelling;
  • Thrombocytopenia (decrease in the number of platelets in the blood below normal);
  • Leukopenia (decrease in total;
  • Cold extremities;
  • Blockade of the legs of the bundle of Hiss.
When using alpha-beta-blockers in the form of eye drops, the following side effects may develop:
  • bradycardia;
  • Decreased blood pressure;
  • Bronchospasm;
  • Dizziness;
  • Weakness;
  • Burning sensation or foreign body in the eye;

Contraindications

Contraindications to the use of various groups of alpha-blockers

Contraindications to the use of various groups of alpha-blockers are given in the table.
Contraindications to the use of alpha-1-blockers Contraindications to the use of alpha-1,2-blockers Contraindications to the use of alpha-2-blockers
Stenosis (narrowing) of the aortic or mitral valvessevere peripheral vascular atherosclerosis
orthostatic hypotensionArterial hypotensionJumps in blood pressure
Severe liver dysfunctionHypersensitivity to drug componentsUncontrolled hypotension or hypertension
Pregnancyangina pectorisSevere liver or kidney problems
LactationBradycardia
Hypersensitivity to drug componentsOrganic heart disease
Heart failure secondary to constrictive pericarditis or cardiac tamponadeMyocardial infarction less than 3 months ago
Heart defects occurring against the background of low filling pressure of the left ventricleAcute bleeding
severe kidney failurePregnancy
Lactation

Beta-blockers - contraindications

Selective (beta-1) and non-selective (beta-1.2) blockers have almost identical contraindications for use. However, the range of contraindications to the use of selective beta-blockers is somewhat wider than for non-selective ones. All contraindications for use for beta-1- and beta-1,2-blockers are shown in the table.
Contraindications to the use of non-selective (beta-1,2) blockers Contraindications to the use of selective (beta-1) blockers
Individual hypersensitivity to drug components
Atrioventricular block II or III degree
Sinoatrial blockade
Severe bradycardia (heart rate less than 55 beats per minute)
Sick sinus syndrome
Cardiogenic shock
Hypotension (systolic pressure less than 100 mmHg)
Acute heart failure
Chronic heart failure in the stage of decompensation
Obliterating vascular diseasesPeripheral circulation disorders
Prinzmetal's anginaPregnancy
Bronchial asthmaLactation

Contraindications to the use of alpha-beta blockers

Contraindications to the use of alpha-beta blockers are as follows:
  • Increased individual sensitivity to any components of the drugs;
  • Atrioventricular block II or III degree;
  • Sinoatrial blockade;
  • Sick sinus syndrome;
  • Chronic heart failure in the stage of decompensation (IV functional class according to NYHA);
  • Cardiogenic shock;
  • Sinus bradycardia (pulse less than 50 beats per minute);
  • Arterial hypotension (systolic pressure below 85 mm Hg);
  • Chronic obstructive pulmonary disease;
  • Bronchial asthma;
  • peptic ulcer of the stomach or duodenum;
  • Type 1 diabetes;
  • The period of pregnancy and breastfeeding;
  • Severe liver disease.

Hypotensive beta-blockers

Hypotensive action have drugs of various groups of adrenoblockers. The most pronounced hypotensive effect is exerted by alpha-1-blockers containing as active ingredients substances such as doxazosin, prazosin, urapidil or terazosin. Therefore, it is the drugs of this group that are used for long-term therapy of hypertension in order to reduce pressure and subsequently maintain it at an average acceptable level. Drugs of the alpha-1-blocker group are optimal for use in people suffering from only hypertension without concomitant cardiac pathology.

In addition, all beta-blockers are hypotensive, both selective and non-selective. Hypotensive non-selective beta-1,2-blockers containing bopindolol, metipranolol, nadolol, oxprenolol, pindolol, propranolol, sotalol, timolol as active substances. These drugs, in addition to the hypotensive effect, also affect the heart, so they are used not only in therapy arterial hypertension but also heart disease. The most "weak" antihypertensive non-selective beta-blocker is sotalol, which has a predominant effect on the heart. However, this drug is used in the treatment of arterial hypertension, which is combined with heart disease. All non-selective beta-blockers are optimal for use in hypertension associated with coronary heart disease, exertional angina and myocardial infarction.

Hypotensive selective beta-1-blockers are drugs containing the following as active substances: atenolol, acebutolol, betaxolol, bisoprolol, metoprolol, nebivolol, talinolol, celiprolol, esatenolol, esmolol. Given the peculiarities of action, these drugs are best suited for the treatment of arterial hypertension, combined with obstructive pulmonary pathologies, peripheral arterial diseases, diabetes, atherogenic dyslipidemia, as well as for heavy smokers.

Alpha-beta-blockers containing carvedilol or butylmethyloxadiazole as active substances are also hypotensive. But due to a wide range of side effects and a pronounced effect on small vessels, drugs in this group are used less frequently compared to alpha-1-blockers and beta-blockers.

Currently, the drugs of choice for the treatment of arterial hypertension are beta-blockers and alpha-1-blockers.

Alpha-1,2-blockers are used mainly for the treatment of peripheral and cerebral circulation disorders, since they have a more pronounced effect on small blood vessels. Theoretically, drugs of this group can be used to lower blood pressure, but this is ineffective due to the large number of side effects that will occur in this case.

Adrenoblockers for prostatitis

For prostatitis, alpha-1-blockers are used, containing alfuzosin, silodosin, tamsulosin or terazosin as active substances, in order to improve and facilitate the process of urination. Indications for the appointment of adrenergic blockers for prostatitis are low pressure inside the urethra, weak tone of the bladder itself or its neck, as well as the muscles of the prostate gland. The drugs normalize the outflow of urine, which accelerates the excretion of decay products, as well as dead pathogenic bacteria, and, accordingly, increases the effectiveness of antimicrobial and anti-inflammatory treatment. The positive effect is usually fully developed after 2 weeks of use. Unfortunately, the normalization of urine outflow under the action of adrenergic blockers is observed only in 60-70% of men suffering from prostatitis.

The most popular and effective adrenoblockers for prostatitis are drugs containing tamsulosin (for example, Hyperprost, Glansin, Miktosin, Omsulosin, Tulosin, Fokusin, etc.).

Before use, you should consult with a specialist.