What are beta- and alpha-blocker drugs, their classification. To whom and why are beta blockers prescribed? The most common side effect of beta blockers

Treatment of cardiac diseases in modern times medical practice It 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 levels and heart rate.

However, like any medical supplies, beta blockers require caution and care during therapy.

Beta blocker drugs are used in the treatment of the following diseases:

• chronic condition high blood pressure in the body;
• increased level pressure against the background of other pathologies;
• increased rhythm of contractions of the heart muscle;
• painful sensations in the heart when diagnosed coronary 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;
• abnormal increase in the size of the ventricle and septum;
• a condition in which the 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 pressure due to previous surgical intervention;
• migraine;
• alcohol and drug addiction.

Classification

Drugs in this group have several classifications, which divide drugs according to various criteria.

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

• non-selective drugs;
• selective drugs.

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

This effect on the body manifests itself in the form of a decrease in blood clotting and a decrease in the number of plaques, and the level of pressure in the bloodstream also decreases. blood vessels, the rhythm of myocardial contractions is normalized, cell membranes are stabilized.

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

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

The cost of these drugs is very diverse and varies from 50 rubles. up to 1000 rub. per package.

Selective beta blockers work specifically at a specific type of receptor. The second name of this group is cardioselective. Blocked receptors are located in the cells of the myocardium, lipoid tissue, and also in the intestines.

Representatives of the selective group are:

• Metoprolol;
• Tenormin;
• Esmolol;
• Coriol;
• Nebikor;
• Cordanum;
• Vazacor;
• Acekor.

The cost of drugs in pharmacies varies. It depends on the manufacturer, the concentration of the active ingredient, and the number of tablets in the package.

Domestic drugs are much cheaper than foreign analogues. 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 in the group of beta blockers, 3 generations are distinguished.

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

• Propranolol;
• Sotalol;
• Timolol.

2nd generation medicines The group of beta blockers includes selective drugs:

• Metoprolol;
• Esmolol.

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

• Talinolol;
• Celiprolol;
• Carteolol.

Currently, it is 3rd generation drugs that are most often used. They are distinguished by the smallest number of contraindications and.

However, you cannot 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 leading position in terms of effectiveness is occupied by a group of 3rd generation beta blockers. This is the most modern and progressive type of drugs that act on adrenergic receptors.

The best among them are drugs under trade name, and .

Carvedilol is a selective drug. During the period of its administration it is noted effective reduction the level of pressure in the blood vessels due to the expansion of the lumen, and the number of plaques decreases.

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

How do beta blockers affect blood pressure?

Beta blockers block the work of special adrenergic receptors in the body, which are located in the cells of cardiac muscle tissue, liver, fatty tissue, etc. As a result of a decrease in receptor activity, the following changes occur in the body:

• the heart rate 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 normalizing heart rate and myocardial function is noted.

Instructions for use

Duration of the course of treatment, dosage of drugs and general scheme treatment is determined. In order for therapy to be effective, it must be taken into account general state the patient’s body, it is noted whether there are any contraindications.

In addition, regular monitoring of the patient’s condition is carried out. If side effects are detected, the doctor will replace the medications with similar ones.

During the entire treatment it is necessary to monitor the indications 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;
• disturbance of the rhythm of heart contractions in the direction of slowing down;
• increased asthmatic symptoms;
• intoxication of the body, which is manifested by nausea and accompanying vomiting;
• decrease in blood glucose concentration;
• excessive drop in blood pressure levels;
• pathological changes in metabolic processes;
• increased symptoms of lung diseases;
• impaired concentration;
• dyspeptic disorders digestive system;
• decreased sexual desire;
• development inflammatory processes on the mucous membrane of the eyes;
• allergic rashes over the entire area skin;
• circulatory disorders in the extremities.

If side effects occur during therapy with these medications, stop taking the drug. The doctor selects more suitable analogues.

Contraindications

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

In addition, beta blockers should not be taken during pregnancy or during pregnancy planning.

Overdose

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

• severe dizziness;
• heart rhythm disturbances;
• a sharp decline heart rate;
• blue discoloration of the skin;
• convulsions;
• coma.

If drug poisoning occurs due to an overdose, 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 medical call.

Depending on the symptoms, the patient may be prescribed different drugs to normalize the condition. In case of heart rhythm disturbances, 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 adrenergic receptors are divided into the following groups:

• beta blockers.

Alpha group drugs 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. Additional effect When taking alpha blockers, cholesterol levels can be reduced.

• How do beta blockers work?
• Modern beta blockers: list

Modern beta-blockers are drugs that are prescribed for therapy cardiovascular diseases, in particular hypertension. There is a wide range of drugs in this group. It is extremely important that treatment is prescribed exclusively by a doctor. Self-medication is strictly prohibited!

Beta blockers: purpose

Beta blockers are a very important group of drugs that are prescribed to patients with hypertension and heart disease. The mechanism of action of drugs is to act on the sympathetic nervous system. Medicines in this group are among the most important drugs in the treatment of diseases such as:

Also, the prescription of this group of drugs is justified in the treatment of patients with Marfan syndrome, migraine, withdrawal syndrome, mitral valve prolapse, aortic aneurysm and in the case of vegetative crises. Drugs should be prescribed exclusively by a doctor after a detailed examination, diagnosis of the patient and collection of complaints. Despite the free access to medicines in pharmacies, you should never choose your own medicines. Therapy with beta blockers is a complex and serious undertaking that can either make the patient’s life easier or significantly harm it if administered incorrectly.

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Beta blockers: types

The list of drugs in this group is very extensive.

It is customary to distinguish the following groups of beta-adrenaline receptor blockers:

• The heart rate slows down less;
• the pumping function of the heart does not decrease as much;
• Peripheral vascular resistance increases less;
• the risk of developing atherosclerosis is not so great, since the effect on blood cholesterol levels is minimal.

However, both types of medications are equally effective in reducing blood pressure. There are also fewer side effects from taking these medications.

List of drugs that have sympathomimetic activity: Sectral, Cordanum, Celiprolol (from the cardioselective group), Alprenol, Trazicor (from the non-selective group).

The following medications do not have this property: cardioselective drugs Betaxolol (Lokren), Bisoprolol, Concor, Metoprolol (Vazocordin, Engilok), Nebivolol (Nebvet) and non-selective Nadolol (Korgard), Anaprilin (Inderal).

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Lipo- and hydrophilic preparations

Another type of blockers. Lipophilic drugs are fat soluble. When these drugs enter the body, they are largely processed by the liver. The effect of drugs of this type is quite short-term, since they are quickly eliminated from the body. At the same time, they are distinguished by better penetration through the blood-brain barrier, through which they pass into the brain. nutrients and waste products are removed nerve tissue. In addition, a lower mortality rate has been proven among patients with ischemia who took lipophilic blockers. However, these drugs have side effects on the central nervous system, causing insomnia and depression.

Hydrophilic drugs dissolve well in water. They do not undergo the process of metabolism in the liver, but are excreted in to a greater extent through the kidneys, that is, with urine. In this case, the type of medication does not change. Hydrophilic drugs have a prolonged effect because they are not eliminated from the body very quickly.

Some drugs have both lipo- and hydrophilic properties, that is, they dissolve equally successfully in both fats and water. Bisoprolol has this property. This is especially important in cases where the patient has problems with the kidneys or liver: the body itself “selects” the system that is in a healthier state to remove the medicine.

Typically, lipophilic blockers are taken regardless of meals, and hydrophilic blockers are taken before meals and with a large volume of water.

Selecting a beta blocker is an extremely important and very difficult task, since the choice of a specific medication depends on many factors. All these factors can only be taken into account by a qualified specialist. Modern pharmacology has a wide range of truly effective drugs Therefore, the patient’s most important priority task is to find a good doctor who will competently select the appropriate treatment for a particular patient and determine which medications will be best for him. Only in this case drug therapy will bring results and literally prolong the life of the patient.

Today it is difficult to imagine cardiology without the use of drugs that belong to the category of beta blockers. These medications have proven themselves in the treatment of complex diseases such as hypertension, tachycardia, and heart failure. They have proven their effectiveness in the practice of treating coronary heart disease and metabolic syndrome.

What are beta blockers

This term refers to drugs that can be used to reversibly block β-adrenergic receptors. These drugs are effective in the treatment of hypertension because they affect the functioning of the sympathetic system. nervous system.

These drugs have been widely used in medicine since the sixties of the last century. It must be said that thanks to their discovery, the effectiveness of the treatment of cardiac pathologies has increased significantly.

Classification of beta blockers

Despite the fact that all the drugs included in this group differ in their ability to block adrenergic receptors, they are divided into different categories.

Classification is carried out depending on the subtypes of receptors and other characteristics.

Selective and non-selective agents

There are two types of receptors - beta1 and beta2. Drugs from the group of beta blockers that have the same effect on both types are called non-selective.

Those drugs whose action is directed at beta1 receptors are called selective. The second name is cardioselective.

Such means include bisoprolol, metoprolol.

It is worth noting that as the dosage increases, the specificity of the drug decreases. This means that it begins to block two receptors at once.

Lipophilic and hydrophilic drugs

Lipophilic agents are included in the group of fat-soluble agents. They more easily penetrate the barrier located between the circulatory and central nervous systems. The liver is actively involved in the processing of such drugs. This group includes metoprolol, propranolol.

Hydrophilic agents are easily soluble in water. They are not processed by the liver in the same way and are excreted almost in their original form. Such drugs have a longer lasting effect because they stay in the body longer. These should include atenolol And esmolol.

Alpha and beta blockers

The name alpha blockers are given to those drugs that temporarily stop the functioning of α-adrenergic receptors. They are widely used as adjuncts in the treatment of hypertension.

They are also used in the case of prostate adenoma as a means of improving urination. This category includes doxazosin, terazosin.

Beta blockers block β-adrenergic receptors. This category includes metoprolol, propranolol.

Concor

This drug contains an active substance called bisoprolol. It should be classified as a metabolically neutral beta blocker, since it does not cause disturbances in lipid or carbohydrate metabolism.

When using this drug, the glucose level does not change and hypoglycemia is not observed.

New generation beta blockers

Today there are three generations of such drugs. Of course, it is preferable to use new generation products. They need to be consumed only once a day.

In addition, they are associated with few side effects. New beta blockers include carvedilol, celiprolol.

Areas of application of beta blockers

These tools have been used quite successfully in various violations in the work of the heart.

For hypertension

With the help of beta blockers, it is possible to prevent the negative effect of the sympathetic nervous system on the heart. Thanks to this, it is possible to facilitate its functioning and reduce the need for oxygen.

Due to this, the load is significantly reduced and, as a result, the pressure is reduced. In case of hypertension, indicated carvedilol, bisoprolol.

With tachycardia

The drugs perfectly reduce the heart rate. That is why in case of tachycardia with an indicator of more than 90 beats per minute, beta blockers are prescribed. The most effective means in this case include bisoprolol, propranolol.

For myocardial infarction

With the help of beta blockers, it is possible to limit the area of ​​necrosis, reduce the risk of relapse, and protect the myocardium from the toxic effects of hypercatecholaminemia.

Also, these drugs reduce the risk of sudden death, help increase endurance during physical activity, reduce the likelihood of arrhythmia and have a pronounced antianginal effect.

On the first day after a heart attack it is used anaprilin, the use of which is shown two next year provided there are no side effects. If there are contraindications, cardioselective drugs are prescribed - for example, cordanum.

For diabetes

Patients with diabetes mellitus and heart disease should definitely use these drugs. It should be borne in mind that non-selective agents lead to an increased metabolic response to insulin. That is why their use is not recommended.

Highly selective beta blockers do not have any negative effects. Moreover, drugs such as carvedilol And nebivolol, can improve lipid and carbohydrate metabolism. They also make tissues more responsive to insulin.

For heart failure

These drugs are indicated for the treatment of patients with heart failure. Initially, a small dose of medication is prescribed, which will gradually increase. The most effective means is carvedilol.

Instructions for use

Compound

As active substance in such preparations, as a rule, atenolol, propranolol, metoprolol, timolol, bisoprolol, etc. are used.

Excipients may be different and depend on the manufacturer and form of release of the drug. Starch, magnesium stearate, calcium hydrogen phosphate, dyes, etc. can be used.

Mechanism of action

These drugs may have various mechanisms. The difference lies in the active ingredient used.

The primary role of beta blockers is to prevent the cardiotoxic effects of catecholamines.

The following mechanisms are also important:

• Antihypertensive effect. Associated with stopping the formation of renin and the production of angiotensin II. As a result, it is possible to release norepinephrine and reduce central vasomotor activity.
• Anti-ischemic effect. By reducing the number of heartbeats, the need for oxygen can be reduced.
• Antiarrhythmic action. As a result of a direct electrophysiological effect on the heart, it is possible to reduce sympathetic influences and myocardial ischemia. Also, with the help of such substances, it is possible to prevent hypokalemia induced by catecholamines.

Some drugs may have antioxidant characteristics and suppress the proliferation of vascular smooth muscle cells.

Indications for use

Such drugs are usually prescribed for:

• arrhythmias;
• hypertension;
• heart failure;
• long QT syndrome.

Mode of application

Before taking the drug, be sure to tell your doctor if you are pregnant. The fact of planning a pregnancy is also important.

The specialist should also be aware of the presence of pathologies such as arrhythmia, emphysema, asthma, and bradycardia.

Beta blockers are taken with or immediately after meals. Thanks to this, it is possible to minimize possible side effects. The duration and frequency of taking the medication should be determined exclusively by a specialist.

During use, it is sometimes necessary to monitor your pulse. If you note that its frequency is below the required level, you should immediately notify your doctor.

It is also very important to regularly see a specialist who can assess the effectiveness of the prescribed treatment and its side effects.

Side effects

The drugs have quite a lot of side effects:

• Constant fatigue.
• Decreased heart rate.
• Exacerbation of asthma.
• Heart blockades.
• Toxic effects.
• Reducing LDL cholesterol.
• Reducing blood sugar.
• Threat of increased blood pressure after discontinuation of the drug.
• Heart attacks.

There are conditions in which taking such drugs is quite dangerous:

• diabetes;
• depression;
• obstructive pulmonary pathologies;
• peripheral arterial disorders;
• dyslipidemia;
• sinus node dysfunction without symptoms.

Contraindications

There are also contraindications to the use of such drugs:

• Bronchial asthma.
• Individual sensitivity.
• Second or third degree atrioventricular block.
• Bradycardia.
• Cardiogenic shock.
• Sick sinus syndrome.
• Pathologies of peripheral arteries.
• Low pressure.

Interaction with other drugs

Some medications may interact with beta blockers and increase their effect.

You should tell your doctor if you are taking:

• Remedies for ARVI.
• Medicines for the treatment of hypertension.
• Medicines for the treatment of diabetes mellitus, including insulin.
• MAO inhibitors.

Release form

Such drugs can be produced in the form of tablets or injection solution.

Storage conditions

These drugs should be stored at a temperature not exceeding twenty-five degrees. This should be done in a dark place, out of reach of children.

Do not use medications after their expiration date has expired.

Drug overdose

There are distinctive signs of an overdose:

• , loss of consciousness;
• arrhythmia;
• sudden bradycardia;
• acrocyanosis;
• coma, convulsive state.

Depending on the symptoms, the following drugs are prescribed as first aid:

• In case of heart failure, diuretics and cardiac glycosides are prescribed.
• In case of low blood pressure, adrenaline and mesaton are prescribed.
• For bradycardia, atropine, dopamine, and dobutamine are indicated.
• For bronchospasm, isoproterenol and aminophylline are used.

Beta blockers and alcohol

Alcoholic drinks can reduce positive effect from the use of beta blockers. Therefore, it is not recommended to drink alcohol during the course of treatment.

Beta blockers and pregnancy

Atenolol and metoprolol are considered the safest during this period. Moreover, these drugs are prescribed, as a rule, only during the third trimester of pregnancy.

It should be borne in mind that such drugs can cause fetal growth retardation, especially if taken in the first and second trimester of pregnancy.

Stopping beta blockers

Abrupt withdrawal of any drug is extremely undesirable. This is associated with an increased threat of acute cardiac conditions. This phenomenon is called “withdrawal syndrome”.

As a result of abrupt withdrawal, blood pressure may increase significantly and even develop.

In people with angina, the intensity of angina episodes may increase.

Patients with heart failure may complain of symptoms of decompensation. Therefore, the dose reduction should be carried out gradually - this is done over several weeks. It is very important to monitor the patient's health status.

List of drugs used

The best beta blockers today are:

• bisoprolol;
• carvedilol;
• metoprolol succinate;
• nebivolol

However, only a doctor should prescribe a beta blocker. Moreover, it is recommended to choose drugs of a new generation.

According to patient reviews, it is modern new generation beta blocker drugs that cause minimal side effects and help cope with the problem without leading to a deterioration in the quality of life.

Where can you buy beta blockers?

You can buy beta blockers at the pharmacy, but some drugs are sold only with a doctor's prescription. average price beta blocker tablets cost about 200-300 rubles.

What can replace beta blockers?

At the initial stage of treatment, doctors do not advise replacing beta blockers with other medications. If you do this yourself, there is a serious risk of myocardial infarction.

When the patient feels better, the dosage can be reduced little by little. However, this should be done under constant medical supervision. Adequate replacement Only a specialist can choose a beta blocker.

Beta blockers have proven effective in treating many heart pathologies. However, in order for the therapy to give the desired results, it is recommended to use new generation products and strictly adhere to all the specialist’s instructions.

This will allow you not only to cope with the symptoms of the pathology, but also not to harm your own health.

The video will allow you to more accurately understand the place of beta blockers in the treatment of cardiovascular diseases:

Arterial hypertension requires mandatory treatment with medications. New drugs are constantly being developed to normalize blood pressure and prevent dangerous consequences such as stroke and heart attack. Let's take a closer look at what alpha and beta blockers are - a list of drugs, indications and contraindications for use.

Adrenolytics are drugs that have one pharmacological effect - the ability to neutralize adrenaline receptors of the heart and blood vessels. They turn off the receptors that normally respond to norepinephrine and adrenaline. The effects of adrenolytics are opposite to those of norepinephrine and adrenaline and are characterized by a decrease in pressure, dilation of blood vessels and narrowing of the lumen of the bronchi, and a decrease in glucose in the blood. The drugs act on receptors located in the heart and walls of blood vessels.

Alpha-blocker drugs have a dilating effect on the blood vessels of organs, especially the skin, mucous membranes, kidneys and intestines. Due to this, an antihypertensive effect occurs, a decrease in peripheral vascular resistance, an improvement in blood flow and blood supply to peripheral tissues.

Let's look at what beta blockers are. This is a group of drugs that bind to beta-adrenergic receptors and block the effect of catecholamines (norepinephrine and adrenaline) on them. They are considered the main drugs in the treatment of essential arterial hypertension and increased pressure. They have been used for this purpose since the 60s of the 20th century.

The mechanism of action is expressed in the ability to block beta adrenergic receptors of the heart and other tissues. The following effects arise:

Beta blockers have not only a hypotensive effect, but also a number of other properties:

• Antiarrhythmic activity due to inhibition of the effects of catecholamines, a decrease in the speed of impulses in the area of ​​the atrioventricular septum and a slowdown in sinus rhythm;
• Antianginal activity. Beta-1 adrenergic receptors of blood vessels and myocardium are blocked. Because of this, heart rate, myocardial contractility, and blood pressure decrease, the duration of diastole increases, and coronary blood flow improves. In general, the heart's need for oxygen decreases, tolerance to physical stress increases, periods of ischemia decrease, and the frequency of anginal attacks decreases in patients with post-infarction angina and exertional angina;
• Antiplatelet ability. Platelet aggregation slows down, prostacyclin synthesis is stimulated, blood viscosity decreases;
• Antioxidant activity. There is an inhibition of free fatty acids that are caused by catecholamines. The need for oxygen for further metabolism is reduced;
• Venous blood flow to the heart and the volume of circulating plasma decrease;
• Insulin secretion decreases due to inhibition of glycogenolysis;
• There is a sedative effect, the contractility of the uterus increases during pregnancy.

Indications for use

Alpha-1 blockers are prescribed for the following pathologies:

Alpha 1,2 blockers are used for the following conditions:

• pathology of cerebral circulation;
• migraine;
• dementia, which is caused by a vascular component;
• pathology of peripheral circulation;
• problems with urination due to a neurogenic bladder;
• diabetic angiopathy;
• dystrophic diseases of the cornea;
• vertigo and pathologies of the functioning of the vestibular apparatus associated with the vascular factor;
• neuropathy optic nerve associated with ischemia;
• prostatic hypertrophy.

Important: Alpha-2 blockers are prescribed only for the treatment of impotence in males.

Non-selective beta-1,2 blockers are used in the treatment of the following pathologies:

• arterial;
• increased intraocular pressure;
• migraine (preventive purposes);
• hypertrophic cardiomyopathy;
• heart attack;
• sinus tachycardia;
• tremor;
• bigeminy, supraventricular and ventricular arrhythmia, trigeminy (preventive purposes);
• angina pectoris;
• mitral valve prolapse.

Selective beta-1 blockers are also called cardioselective because of their effect on the heart and less on blood pressure and blood vessels. They are prescribed in the following conditions:

Alpha-beta blockers are prescribed in the following cases:

• arrhythmia;
• stable angina;
• CHF (combined treatment);
• high blood pressure;
• glaucoma (eye drops);
• hypertensive crisis.

Classification of drugs

There are four types of adrenergic receptors in the walls of blood vessels (alpha 1 and 2, beta 1 and 2). Medicines from the group of adrenergic blockers can block different types receptors (for example, only beta-1 adrenergic receptors). Drugs are divided into groups depending on the shutdown of certain types of these receptors:

Alpha blockers:

• alpha-1 blockers (silodosin, terazosin, prazosin, alfuzosin, urapidil, tamsulosin, doxazosin);
• alpha-2 blockers (yohimbine);
• alpha-1, 2-blockers (dihydroergotamine, dihydroergotoxin, phentolamine, nicergoline, dihydroergocristine, proroxan, alpha-dihydroergocriptine).

Beta blockers are divided into the following groups:

• non-selective adrenergic blockers (timolol, metypranolol, sotalol, pindolol, nadolol, bopindolol, oxprenolol, propranolol);
• selective (cardioselective) adrenergic blockers (acebutolol, esmolol, nebivolol, bisoprolol, betaxolol, atenolol, talinolol, esatenolol, celiprolol, metoprolol).

List of alpha-beta adrenergic blockers (they include alpha and beta adrenergic receptors at the same time):

• labetalol;
• proxodolol;
• carvedilol.

Please note: The classification shows the names active substances, which are part of drugs in a certain group of blockers.

Beta blockers also come with or without intrinsic sympathomimetic activity. This classification is considered auxiliary, since it is used by specialists to select the necessary medicine.

List of drugs

Common names for alpha-1 blockers:

• Alfuzosin;
• Dalfaz;
• Artesin;
• Zoxon;
• Urocard;
• Prazosin;
• Urorek;
• Miktosin;
• Tamsulosin;
• Cornam;
• Ebrantil.

Alpha-2 blockers:

• Yohimbine;
• Yohimbine hydrochloride.

Alpha-1,2-blockers:

• Redergin;
• Ditamine;
• Nicergoline;
• Pyrroxane;
• Phentolamine.

• Atenol;
• Atenova;
• Atenolan;
• Betacard;
• Tenormin;
• Sectral;
• Betoftan;
• Xonephus;
• Optibetol;
• Bisogamma;
• Bisoprolol;
• Concor;
• Tirez;
• Betalok;
• Serdol;
• Binelol;
• Cordanum;
• Breviblock.

Non-selective beta blockers:

• Sandorm;
• Trimepranol;
• Visken;
• Inderal;
• Obzidan;
• Darob;
• Sotalol;
• Glaumol;
• Thymol;
• Timoptic.

Alpha-beta blockers:

• Proxodolol;
• Albetor;
• Bagodilol;
• Carvenal;
• Credex;
• Labetol;
• Abetol.

Side effects

Common side effects from taking adrenergic blockers:

Side effects from taking alpha-1 blockers:

• swelling;
• severe decrease in pressure;
• arrhythmia and tachycardia;
• dyspnea;
• runny nose;
• dry mouth;
• pain in the chest area;
• decreased libido;
• pain during erection;
• urinary incontinence.

Side effects when using alpha-2 receptor blockers:

• increase in pressure;
• anxiety, excessive excitability, irritability and physical activity;
• tremor;
• decreased frequency of urination and volume of fluid.

Side effects from alpha-1 and -2 blockers:

• decreased appetite;
• sleep problems;
• excessive sweating;
• coldness of hands and feet;
• increased acidity in the stomach.

Common side effects of beta blockers:

Non-selective beta blockers may cause the following conditions:

• pathologies of vision (fogginess, feeling that there is something in the eye foreign body, tearfulness, duality, burning);
• cardiac ischemia;
• colitis;
• cough with possible attacks of suffocation;
• a sharp decrease in pressure;
• impotence;
• fainting;
• runny nose;
• an increase in blood uric acid, potassium and triglycerides.

Alpha-beta blockers have the following side effects:

• decrease in blood platelets and leukocytes;
• formation of blood in the urine;
• increased cholesterol, sugar and bilirubin;
• pathologies of the conduction of heart impulses, sometimes leading to blockade;
• worsened peripheral circulation.

Interaction with other drugs

The following drugs have favorable compatibility with alpha blockers:

Favorable combination of beta blockers with other drugs:

1. The combination with nitrates is successful, especially if the patient suffers not only from hypertension, but also from coronary heart disease. The hypotensive effect is enhanced, bradycardia is leveled by tachycardia, which is caused by nitrates.
2. Combination with diuretics. The effects of diuretics are increased and prolonged due to the inhibition of the release of renin from the kidney by beta blockers.
3. ACE inhibitors and angiotensin receptor blockers. If there are drug-resistant arrhythmias, you can carefully combine use with quinidine and procainamide.
4. Calcium channel blockers of the dihydropyridine group (cordafen, nikirdipine, phenigidine). You can combine it with caution and in small dosages.

Dangerous combinations:

1. Calcium channel blockers that belong to the verapamil group (isoptin, gallopamil, finoptin). The frequency and strength of heart contractions decreases, atrioventricular conduction becomes worse, hypotension, bradycardia, acute left ventricular failure and atrioventricular block increase.
2. Sympatholytics - octadine, reserpine and drugs containing it (rauvazan, brinerdine, adelfan, raunatin, cristepine, trirezide). There is a sharp weakening of sympathetic influences on the myocardium, and associated complications may arise.
3. Cardiac glycosides, direct M-cholinomimetics, anticholinesterase drugs and tricyclic antidepressants. The likelihood of blockade, bradyarrhythmia and cardiac arrest increases.
4. Antidepressants-MAO inhibitors. There is a possibility of hypertensive crisis.
5. Typical and atypical beta-agonists and antihistamines. These drugs are weakened when used together with beta blockers.
6. Insulin and sugar-lowering medications. The hypoglycemic effect increases.
7. Salicylates and butadione. There is a weakening of the anti-inflammatory effect;
8. Indirect anticoagulants. The antithrombotic effect is weakened.

Contraindications to taking alpha-1 blockers:

Contraindications to taking alpha-1,2 blockers:

• arterial hypotension;
• acute bleeding;
• lactation;
• pregnancy;
• myocardial infarction that occurred less than three months ago;
• organic heart lesions;
• atherosclerosis of peripheral vessels in severe form.

Contraindications for alpha-2 blockers:

• excessive sensitivity to the components of the drug;
• severe pathologies of kidney or liver functioning;
• blood pressure surges;
• uncontrolled hypertension or hypotension.

General contraindications to taking non-selective and selective beta-blockers:

• excessive sensitivity to the components of the drug;
• cardiogenic shock;
• sinoatrial block;
• weakness of the sinus node;
• hypotension (blood pressure less than 100 mm);
• acute heart failure;
• atrioventricular block of the second or third degree;
• bradycardia (pulse less than 55 beats/min.);
• CHF in the stage of decompensation;

Contraindications to taking non-selective beta blockers:

• bronchial asthma;
• obliterating vascular diseases;
• Prinzmetal's angina.

Selective beta blockers:

• lactation;
• pregnancy;
• pathology of peripheral circulation.

Hypertensive patients should use the medications discussed strictly according to the instructions and in the dose prescribed by the doctor. Self-medication can be dangerous. At the first appearance of side effects, you should immediately contact a medical facility.

Still have questions? Ask them in the comments! A cardiologist will answer them.

Mechanism of action of beta blockers

The effects of beta-blockers are realized by blockade of β1 and β2-adrenergic receptors. There are two types of β-adrenergic receptors (β1- and β2-adrenergic receptors), which differ in structural and functional characteristics and distribution in tissues. β1-adrenergic receptors dominate in the structures of the heart, islet tissue of the pancreas, juxtaglomerular apparatus of the kidneys, and adipocytes.

The drugs, by binding to β1-adrenergic receptors of the heart, prevent the action of norepinephrine and adrenaline on them, and reduce the activity of adenylate cyclase. A decrease in enzyme activity leads to a decrease in cAMP synthesis and inhibition of Ca2+ entry into cardiomyocytes. This is how the main effects of β-blockers are realized:

• negative inotropic effect(the strength of heart contractions decreases);
• negative chronotropic effect (heart rate decreases);
• negative dromotropic effect (conductivity is suppressed);
• negative bathmotropic effect(automaticity decreases).

The antianginal effect of the drugs is manifested by a decrease in the force of heart contractions and heart rate, which reduces the myocardial oxygen demand.

Due to inhibition of conductivity and automatism, the drugs have an antiarrhythmic effect.

A decrease in Ca2+ content due to blockade of β1-adrenergic receptors in the cells of the juxtalomerular apparatus (JA) of the kidneys is accompanied by inhibition of renin secretion and, accordingly, a decrease in the formation of angiotensin II, which leads to a decrease in blood pressure and determines the effectiveness of β-blockers as antihypertensive drugs.

Blockade β2-blockers helps to increase:

• bronchial smooth muscle tone;
• contractile activity of the pregnant uterus;
• contraction of smooth muscle cells gastrointestinal tract(manifested by abdominal pain, vomiting, nausea, diarrhea, and much less constipation).

In addition, narrowing of arterioles and venules causes an increase in peripheral vascular resistance and can impair blood supply to the extremities, leading to the development of Raynaud's syndrome.

β-blockers cause changes in lipid and carbohydrate metabolism. They inhibit lipolysis, prevent an increase in the content of free fatty acids in the blood plasma, while the TG content increases, and the concentration of total cholesterol does not change, the HDL cholesterol content decreases, and LDL cholesterol increases, which leads to an increase in the atherogenic coefficient.

β-blockers cause activation of glycogen synthesis from glucose in the liver and suppress glycogenolysis, which can lead to hypoglycemia, especially when using hypoglycemic drugs in patients with diabetes mellitus. Due to the blockade of beta-blockers in the pancreas and inhibition of physiological insulin secretion, the drugs can cause hyperglycemia, but in healthy people they usually do not affect blood glucose concentrations.

Based on their effect on receptors, beta-blockers are divided into non-selective (affecting β1- and β2-adrenergic receptors) and cardioselective (affecting β1-adrenergic receptors), in addition, some of them have intrinsic sympathomimetic activity (ICA).

Beta-blockers with BSA (pindolol, bopindolol, oxprenolol) reduce heart rate and myocardial contractility to a lesser extent, have virtually no effect on lipid metabolism, and have a less pronounced withdrawal syndrome.

The vasodilatory effect of beta blockers is due to one of the following mechanisms or a combination of them:

• pronounced ICA in relation to vascular β-blockers (for example, pindolol, celiprolol);
• a combination of β- and α-adrenergic blocking activity (for example, carvedilol);
• release of nitric oxide (nebivolol) from endothelial cells;
• direct vasodilatory effect.

Cardioselective beta-blockers in low doses, unlike non-selective ones, have little effect on the tone of the bronchi and arteries, insulin secretion, mobilization of glucose from the liver, contractile activity of the pregnant uterus, so they can be prescribed for concomitant chronic obstructive pulmonary diseases, diabetes mellitus, peripheral circulatory disorders (for example, Raynaud's syndrome, pregnancy). They practically do not cause vasoconstriction of skeletal muscles, therefore, when using them, they are less likely to cause increased fatigue and muscle weakness.

Pharmacokinetics of beta-blockers

The pharmacokinetic effect of various beta-blockers is determined by the degree of their solubility in fats and water. There are three groups of beta blockers:

• fat-soluble (lipophilic),
• water-soluble (hydrophilic),
• fat and water soluble.

Lipophilic beta-blockers (metoprolol, alprenolol, oxprenolol, propranolol, timolol) are quickly absorbed from the gastrointestinal tract and easily penetrate the blood-brain barrier (often causing side effects such as insomnia, general weakness, drowsiness, depression, hallucinations, nightmares). Therefore, single doses and frequency of administration should be reduced in elderly patients and with diseases of the nervous system. Lipophilic beta-blockers may slow the elimination from the blood of other drugs that are metabolized in the liver (for example, lidocaine, hydrolasine, theophylline). Lipophilic β-blockers should be prescribed at least 2-3 times a day.

Hydrophilic beta-blockers (atenolol, nadolol, sotalol) are not completely (30-70%) absorbed into the gastrointestinal tract and slightly (0-20%) metabolized in the liver. Excreted mainly by the kidneys. They have a long half-life (6-24 years). T1/2 of hydrophilic drugs increases with a decrease in glomerular filtration rate (for example, with renal failure, in elderly patients). The frequency of use varies from 1 to 4 times a day.

There are beta-blockers that are fat- and water-soluble (acebutolol, pindolol, celiprolol, bisoprolol). They have two elimination routes - hepatic (40-60%) and renal. Fat and water-soluble drugs can be prescribed once a day, with the exception of Pindolol: it is taken 2-3 times. T1/2 is 3-12 hours. Most drugs (bisoprolol, pindolol, celiprolol) have virtually no interaction with drugs that are metabolized in the liver, so they can be prescribed to patients with moderate hepatic or renal failure(in case of severe dysfunction of the liver and kidneys, the dose of the drug is recommended to be reduced by 1.5 times).

Pharmacokinetic parameters of beta-blockers:

*Note: ? - data not found

Indications for the use of beta-blockers

• angina pectoris,
• acute coronary syndrome,
• Hypertension and primary prevention of stroke and ischemic heart disease in patients with hypertension,
• prevention of ventricular and supraventricular arrhythmias,
• prevention re-infarction myocardium,
• prevention of sudden death in patients with long QT interval syndrome,
• chronic heart failure (carvedilol, metoprolol, bisoprolol, nebivolol),
• systemic diseases with increased influence of the sympathetic nervous system,
• thyrotoxicosis,
• essential tremor,
• alcohol withdrawal,
• dissecting aortic aneurysm,
• hypertrophic cardiomyopathy,
• digitalis intoxication,
• mitral stenosis (tachysystolic form),
• mitral valve prolapse,
• tetralogy of Fallot.

Side effects and contraindications of beta-blockers

The main side effects and contraindications of beta-blockers are presented in the table.

Side effects of beta blockers, contraindications to their use and conditions requiring special caution when using beta blockers:

β-blockers are characterized by withdrawal syndrome.

Drug interactions

Combination of beta blockers with others medicines, exhibits a negative foreign and chronotropic effect, can lead to severe adverse reactions. When beta-blockers are combined with clonidine, a pronounced decrease in blood pressure and bradycardia develops, especially when patients are in a horizontal position.

The combination of beta-blockers with verapamil, amiodarone, and cardiac glycosides can lead to severe bradycardia and impaired AV conduction.

The combination of beta-blockers with nitrates or calcium channel blockers is justified, since the former reduce the myocardial oxygen demand, while the others, by reducing the tone of peripheral and coronary vessels, provide hemodynamic unloading of the myocardium and an increase in coronary blood flow.