The effect of beta blockers on the heart and hypertension - how it works

There are many different medications available to treat cardiovascular disease, but beta blockers are considered the most effective.

In most cases, they are used to treat hypertension, but they have the potential to treat other heart diseases. It is very important to take into account an individual approach to choosing a medicine, since these medicines are not universal.

Indications for use

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

• a chronic condition of high blood pressure in the body;
• increased blood pressure due to other pathologies;
• increased rhythm of contractions of the heart muscle;
• painful sensations in the heart with diagnosed coronary artery disease;
• rehabilitation period after a previous heart attack;
• pathological changes in heart rate;
• functional disorders in 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 of sudden death;
• high blood pressure due to surgery;
• migraine;
• alcohol and drug addiction.

List of drugs

Many people are interested in which medications belong to the group of beta blockers. Beta blockers are pills that block adrenaline receptors.

The most effective are selective drugs, and they have almost no side effects. In this case, these include “Bisoprolol”, “Propranolol”. Bisoprolol, Carvedilol, Propranolol are non-selective drugs that are used in the treatment of many cardiovascular diseases. All patients easily tolerate these drugs, but if the therapeutic dose is exceeded, side effects may occur.

Nebivolol is a non-cardioselective drug and is often used to treat coronary artery disease. When taking drugs from this group, you must strictly follow the dosage prescribed by your doctor.

Only a specialist can prescribe such medications to a patient after carrying out all the necessary diagnostic procedures!

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.

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This 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 is normalized, and cell membranes are stabilized.

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

• Anaprilin;
• 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.

The main advantage of this group is that they can be taken by people who have diabetes and a tendency to develop bronchospasms.

Representatives of the selective group are:

• Metoprolol;
• Tenormin;
• Lokren;
• Esmolol;
• Bisoprolol;
• 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.

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

• Metoprolol;
• Bisoprolol;
• 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 have the least number of contraindications and side effects.

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.

Indications

The reasons for use depend on the type of medication and the specific name. If we summarize several types of drugs, the following picture will emerge.

• Primary hypertension. It is caused by diseases of the heart and blood vessels and is accompanied by a persistent gradual increase in blood pressure. When chronic, the disorder is difficult to correct.
• Secondary or renovascular hypertension. Caused by hormonal imbalance and kidney function. It can proceed benignly, indistinguishable from the primary one, or malignantly with a rapid jump in blood pressure to critical levels and maintaining a crisis status for an indefinitely long time, up to the destruction of target organs and death.
• Arrhythmias of different types. Mainly supraventricular. To interrupt an acute condition and prevent the development of further repeated episodes, relapses of the disorder.
• Ischemic disease. The antianinal effect of the drugs is based on reducing the need of the heart and its structures for oxygen and nutrients. However, its use is associated with certain risks; it is worth assessing myocardial contractility and susceptibility to infarction.
• Chronic heart failure in the initial stages. The use is due to the same antianginal effect.

As part of additional use, as an auxiliary profile, beta blockers are prescribed for pheochromocytoma (tumor of the adrenal cortex that synthesizes norepinephrine).

It can be used during a current hypertensive crisis to normalize heart rhythm and dilate blood vessels (the vasodilatory effect is inherent mainly in mixed beta blockers, like Carvidelol, which also affect alpha receptors).

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 considered to be drugs under the trade name Nebivolol Sandoz, as well as Carvedilol.

Carvedilol is a selective drug. During the period of its use, 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.

Nebivolol – 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.

Beta blocker withdrawal syndrome

Abrupt refusal of therapy after long-term use of adrenergic blockers leads to withdrawal syndrome, which manifests itself:

• arrhythmia;
• increased heart rate;
• attacks of angina pectoris;
• heartbeat.

A group of beta-blockers reduces the sensitivity of receptors to adrenal hormones. The body tries to compensate for this by increasing the number of target cells for adrenaline and norepinephrine. Additionally, drugs in this group prevent the transformation of thyroxine into triiodothyronine. Therefore, stopping the pills leads to a sharp increase in thyroid hormones in the blood.

To prevent withdrawal syndrome, you must:

• gradually reduce the dose of adrenergic blockers over 1.5-2 weeks;
• temporarily limit the load;
• include antianginal drugs in therapy;
• limit your intake of medications that lower blood pressure.

Beta-blockers are drugs whose overdose can lead to cardiac complications and even cardiac arrest. Therefore, before taking pills and increasing the dosage, be sure to consult your doctor. Proper treatment reduces the risk of adverse reactions and undesirable consequences.

To prevent severe consequences of stopping these drugs, you must adhere to the following recommendations:

• stop using beta-adrenergic receptor blockers gradually, over 2 weeks, according to the following scheme: on the 1st day, the daily dose of propranolol is reduced by no more than 80 mg, on the 5th - by 40 mg, on the 9th - by 20 mg and on the 13th - by 10 mg;
• patients with coronary artery disease during and after discontinuation of beta-adrenergic blockers should limit physical activity and, if necessary, increase the dose of nitrates;
• for persons with coronary artery disease who are planning coronary artery bypass grafting, beta-adrenergic blockers are not canceled before surgery; 2 hours before surgery, 1/2 the daily dose is prescribed; beta-blockers are not administered during surgery, but for 2 days. after it it is prescribed intravenously.

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.

Mechanism of action of beta blockers

The beta blocker realizes its effect by blocking B1 and B2 adrenergic receptors, which are responsible for the structural and functional characteristics and distribution in the tissues of the body. Type B1 adrenergic receptors predominate in the heart, pancreas and renal apparatus.

Beta blockers, the mechanism of action of which is based on blocking certain receptors, bind to B1 adrenergic receptors and interfere with the action of adrenaline and norepinephrine. Beta 1.2 adrenergic blockers are responsible for:

1. Reducing heart rate.
2. Decreased strength of heart contractions.
3. Suppression of conductivity (dropotropic effect).
4. Automatism of the cardiovascular system (bathmotropic effect).

Due to the fact that beta blockers block adrenaline receptors, this reduces the myocardial oxygen demand. Due to their blocking ability, these drugs have antiarrhythmic properties.

In addition, they normalize blood pressure, so they are often used in the treatment of hypertension. Blocking B2 adrenergic blockers affects:

1. Increased smooth muscle tone in the bronchi.
2. Contraction of the uterus during pregnancy.
3. Contractile actions in the cells of the gastrointestinal tract (may be accompanied by nausea and diarrhea).

It is worth considering that the drugs in this group affect lipid and carbohydrate metabolism and increase the synthesis of glycogen in the liver.

Instructions for use

The duration of the course of treatment, dosage of drugs and the general treatment regimen are determined by the doctor. In order for therapy to be effective, the general condition of the patient’s body must be taken into account, and whether there are any contraindications is noted.

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.

Throughout treatment, blood pressure and heart rate readings should be monitored. Even with minor deviations from the norm, you should immediately consult a doctor to adjust the treatment.

Stopping beta blockers should occur gradually. Abrupt termination of a course often provokes a withdrawal effect and negative manifestations intensify.

conclusions

To prevent withdrawal syndrome, if the drug is taken for a long time, it is necessary to stop taking it gradually, gradually reducing the prescribed dosage. Adrenergic receptors reduce the risk of recurrent myocardial infarction, so they must be taken regularly, following all the doctor’s recommendations.

In the treatment of cardiovascular diseases with adrenergic blockers, it is very important to take into account the stage and type of pathology. This is what determines which adrenergic blocker group you need to take.

Only after making an accurate diagnosis can you choose a treatment package that will include adrenergic blockers. As a rule, therapy takes quite a long time.

Side effects

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

• feeling of 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 of the digestive system;
• decreased sexual desire;
• development of inflammatory processes on the mucous membrane of the eyes;
• allergic rashes over the entire area of ​​the 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.

Reception features

If your cardiologist prescribes adrenergic blockers, you should tell him or her about your regular use of prescription and over-the-counter medications. It is necessary to notify a specialist about serious concomitant pathologies - emphysema, sinus rhythm disorder, bronchial asthma.

To avoid adverse reactions and complications, adrenergic blockers are used in accordance with the instructions:

• tablets are taken after meals;
• During therapy, monitor heart rate;
• if your health worsens, consult a doctor;
• therapy is not stopped without the recommendation of a specialist.

The dosage and duration of treatment depend on the type of disease and are determined by the doctor. You cannot combine adrenergic blockers with other drugs or alcohol. Violation of the rules for the use of β-adrenolytics is fraught with worsening health conditions.

Before starting treatment, the patient should inform the doctor about the presence of diseases that may be grounds for discontinuation of adrenergic blockers.

Medicines from this group are taken during or after meals. This reduces the possible negative effects of drugs on the body. The duration of administration, dosage regimen and other nuances are determined by the doctor.

During use, you should constantly check your heart rate. If this indicator decreases noticeably, the dosage should be changed. You cannot stop taking the medication on your own or start using other means.

Contraindications

Beta blockers are strictly prohibited for the following concomitant conditions of the body:

• 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 blood pressure.

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

Contraindications for use

β1- and β2-adrenolytics have similar contraindications for use. Drugs are not prescribed for:

• atrioventricular block;
• bradycardia;
• orthostatic hypotension;
• sinoatrial block;
• left ventricular failure;
• terminal cirrhosis of the liver;
• obstructive pulmonary disease;
• decompensated kidney failure;
• chronic pathologies of the bronchi;
• vasospastic angina;
• acute myocardial failure.

Selective adrenergic blockers are not taken in case of peripheral circulation disorders, pregnancy and lactation.

All indications for the use of beta blockers depend on certain properties of the particular drug in the group. Non-selective blockers have narrower indications, while selective ones are safer and can be used more widely. In general, the indications are general, although they are limited by the inability to use the drug in some patients. For non-selective drugs, the indications are as follows:

• myocardial infarction in any period, angina pectoris, rest, unstable angina;
• atrial fibrillation normoform and tachyform;
• sinus tachyarrhythmia with or without conduction to the ventricles;
• heart failure (chronic);
• arterial hypertension;
• hyperthyroidism, thyrotoxicosis with or without crisis;
• pheochromocytoma with crisis or for basic treatment of the disease in the preoperative period;
• migraine;
• dissecting aortic aneurysm;
• alcohol or drug withdrawal syndrome.

Due to the safety of many drugs in the group, especially the second and third generations, the list of beta blocker drugs often appears in protocols for the treatment of diseases of the heart and blood vessels. In terms of frequency of use, they are almost the same as ACE inhibitors, which are used to treat CHF and hypertension with and without metabolic syndrome. Together with diuretics, these two groups of drugs can increase life expectancy in chronic cardiac failure.

Beta blockers, like other drugs, have some contraindications. Moreover, since the drugs act on receptors, they are safer than ACE inhibitors. General contraindications:

• bronchial asthma, COPD;
• bradyarrhythmia, sick sinus syndrome;
• atrioventricular blockade of the second degree;
• symptomatic hypotension;
• pregnancy, childhood;
• decompensation of heart failure – CHF II B-III.

An allergic reaction in response to taking a blocker is also a contraindication. If an allergy develops to any drug, then replacing the drug with another solves the problem.

These drugs are strictly prohibited for use in such pathologies and conditions as:

1. Pregnancy and breastfeeding period.
2. Allergic reaction to a medicinal component.
3. Severe disorders of the liver and kidneys.
4. Decreased blood pressure (hypotension).
5. Bradycardia is a decrease in heart rate.
6. Heart defects.

Persons suffering from diabetes mellitus should take adrenergic blockers with extreme caution. During the therapeutic course, you need to constantly monitor your blood glucose levels.

For asthma, the doctor should choose other medications. Some adrenergic blockers can be very dangerous for the patient due to the presence of contraindications.

Adrenergic blockers are the drugs of choice in the treatment of many diseases. In order for them to have the desired effect, they must be taken exactly according to the regimen prescribed by the doctor. Failure to comply with this rule may result in a sharp deterioration in your health.

• essential arterial hypertension;
• secondary arterial hypertension;
• signs of hypersympathicotonia (tachycardia, high pulse pressure, hyperkinetic type of hemodynamics);
• concomitant ischemic heart disease – angina pectoris (selective beta-blockers for smokers, non-selective beta-blockers for non-smokers);
• previous heart attack, regardless of the presence of angina;
• heart rhythm disturbances (atrial and ventricular extrasystole, tachycardia);
• subcompensated heart failure;
• hypertrophic cardiomyopathy, subaortic stenosis;
• mitral valve prolapse;
• risk of ventricular fibrillation and sudden death;
• arterial hypertension in the preoperative and postoperative period;
• Beta blockers are also prescribed for migraines, hyperthyroidism, alcohol and drug withdrawal.

• bradycardia;
• atrioventricular block 2-3 degrees;
• arterial hypotension;
• acute heart failure;
• cardiogenic shock;
• vasospastic angina.

• bronchial asthma;
• chronic obstructive pulmonary disease;
• stenosing peripheral vascular disease with limb ischemia at rest.

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;
• loss of consciousness;
• heart rhythm disturbances;
• a sharp decrease in heart rate;
• blue discoloration of the skin;
• convulsions;
• coma.

If drug poisoning occurs due to an overdose, it is necessary to provide first aid to the victim as soon as possible. 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.

If symptoms of heart failure occur, the victim is given to take diuretics and drugs from the group of glycosides.

Use for diseases of the cardiovascular system

Adrenergic blockers are used primarily in the treatment of various diseases of the cardiovascular system. There is no universal treatment regimen and duration of therapy.

For different pathologies, medications and dosage regimens will differ.

Chronic heart failure

Patients with chronic heart failure (CHF) are often treated with adrenergic blockers. These drugs improve the functioning of the entire system and reduce the load on the heart, and also protect it from toxic effects. Adrenergic blockers eliminate arrhythmic syndrome.

In the treatment of CHF, drugs from the group of metoprolol and bucindolol are mainly used, as they increase the density of the heart muscle. When treating with Metoprolol, the recommended initial dosage is 5 mg, for Bucindolol - 1.2 mg. Gradually the dose is increased.

Heart rhythm disturbances

Heart rhythm disturbances require mandatory treatment, and adrenergic blockers are often used for this. The universal drug in this case is Amiodarone. It can be used to relieve an acute attack, or can be taken continuously.

This drug is used for angina pectoris and heart rhythm disturbances (atrial flutter). In case of an acute attack of heart failure, you must urgently take 1 tablet of this drug. A regular course of treatment will help prevent future attacks.

Myocardial infarction

Adrenergic blockers are used after a myocardial infarction and sometimes to prevent it. In most cases, they are used to reduce the risk of another heart attack.

Adrenergic blockers after myocardial infarction help reduce pain and discomfort. After a heart attack, they normalize the patient’s physical and emotional state.

The dosage and duration of treatment are selected by the doctor individually.

Hypertonic disease

Adrenergic blockers are often used in the treatment of hypertension; their action is based on lowering blood pressure.

For hypertension, drugs from any group of adrenergic blockers can be prescribed. This is due to the fact that the choice of drug is influenced by concomitant diseases and the general condition of the patient.

Hydrophilic adrenergic blockers are mainly used. They can be either selective or non-selective.

Many patients prefer selective adrenergic blockers, but they are not suitable for every type of hypertension. If the blood pressure is too high, which rises frequently, they do not give the desired result.

Difference from Alpha blockers

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

• alpha blockers;
• 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. An additional effect when taking alpha blockers can be considered a decrease in cholesterol levels.

Beta group drugs block the functioning of the corresponding beta receptors. They reduce the intensity of contractions of the heart muscle and lower blood pressure. As an additional effect, auxiliary therapy for cardiac ischemia can be considered.

To whom and when are adrenergic blockers prescribed?

• cardioselective (Metaprolol, Atenolol, Betaxolol, Nebivolol);
• cardionon-selective (Propranolol, Nadolol, Timolol, Metoprolol).

Depending on their ability to dissolve in lipids or water, beta-blockers are pharmacokinetically divided into three groups.

1. Lipophilic beta-blockers (Oxprenolol, Propranolol, Alprenolol, Carvedilol, Metaprolol, Timolol). When administered orally, it is quickly and almost completely (70-90%) absorbed in the stomach and intestines. Drugs in this group penetrate well into various tissues and organs, as well as through the placenta and the blood-brain barrier. Typically, lipophilic beta-blockers are prescribed in low doses for severe hepatic failure and congestive heart failure.
2. Hydrophilic beta-blockers (Atenolol, Nadolol, Talinolol, Sotalol). Unlike lipophilic beta-blockers, when administered orally, they are absorbed only by 30-50%, are metabolized to a lesser extent in the liver, and have a long half-life. They are excreted primarily through the kidneys, and therefore hydrophilic beta-blockers are used in low doses in case of insufficient renal function.
3. Lipo- and hydrophilic beta-blockers, or amphiphilic blockers (Acebutolol, Bisoprolol, Betaxolol, Pindolol, Celiprolol), are soluble in both lipids and water, after oral administration 40-60% of the drug is absorbed. They occupy an intermediate position between lipo- and hydrophilic beta-blockers and are excreted equally by the kidneys and liver. The drugs are prescribed to patients with moderately severe renal and liver failure.

1. Cardiononselective (Propranolol, Nadolol, Timolol, Oxprenolol, Pindolol, Alprenolol, Penbutolol, Carteolol, Bopindolol).
2. Cardioselective (Atenolol, Metoprolol, Bisoprolol, Betaxolol, Nebivolol, Bevantolol, Esmolol, Acebutolol, Talinolol).
3. Beta-blockers with the properties of alpha-adrenergic receptor blockers (Carvedilol, Labetalol, Celiprolol) are drugs that share the mechanisms of hypotensive action of both groups of blockers.

Cardioselective and non-cardioselective beta-blockers, in turn, are divided into drugs with and without intrinsic sympathomimetic activity.

1. Cardioselective beta-blockers without internal sympathomimetic activity (Atenolol, Metoprolol, Betaxolol, Bisoprolol, Nebivolol), along with an antihypertensive effect, slow down the heart rate, provide an antiarrhythmic effect, and do not cause bronchospasm.
2. Cardioselective beta-blockers with internal sympathomimetic activity (Acebutolol, Talinolol, Celiprolol) reduce heart rate to a lesser extent, inhibit the automaticity of the sinus node and atrioventricular conduction, give a significant antianginal and antiarrhythmic effect in sinus tachycardia, supraventricular and ventricular arrhythmias, and have little effect on beta -2 adrenoreceptors of the bronchi of the pulmonary vessels.
3. Non-cardioselective beta-blockers without intrinsic sympathomimetic activity (Propranolol, Nadolol, Timolol) have the greatest antianginal effect, so they are more often prescribed to patients with concomitant angina.
4. Non-cardioselective beta-blockers with internal sympathomimetic activity (Oxprenolol, Trazikor, Pindolol, Visken) not only block, but also partially stimulate beta-adrenergic receptors. Drugs in this group reduce heart rate to a lesser extent, slow atrioventricular conduction and reduce myocardial contractility. They can be prescribed to patients with arterial hypertension with mild conduction disturbances, heart failure, and a slower pulse.

Other drugs for treating hypertension

In addition to medications from the beta-blocker group, the following medications with an excellent mechanism of action are selected for complex therapy:

1. Alpha blockers, temporarily blocking alpha1,2 adrenergic receptors. During the initial use of such medications, pressure may rapidly drop when changing position from horizontal to vertical. Certain drugs in this category do not have a significant effect on blood pressure. They are intended for smooth muscle receptors and are used in urology.
2. Antagonist or inhibitors - are a combination of ACE inhibitors and a calcium antagonist chosen by the doctor. The ranges of effects of medications complement each other well. The combined use of drugs can significantly reduce the dosage relative to their independent use.
3. Diuretics. By removing water and salt from the body, blood pressure is reduced. Such drugs are most often prescribed together with ACE inhibitors, etc. Diuretics do not bring long-term results - their effect on blood pressure is short-lived. In the form of diuretics, special medications or medicinal plants are used. It is impossible to take diuretics continuously due to the harmful effects on the entire body.
4. Sartans or angiotensin II receptor blockers have rare side effects. Drugs of this category contain a large number of medicinal properties and are successfully combined with other medications. The performance of sartans is quite high. Proper selection of the drug and its dosage allows the majority of patients to take one tablet per day.
5. Drugs for dilation of blood vessels. Medicines that relax vascular walls are ineffective in the treatment of hypertension and have a number of side effects. In some cases, it is necessary to use complex drugs against tachycardia. In addition, addiction to the drug and cessation of its effect are likely.
6. Calcium channel blockers. Their action is based on active substances blocking the entry of calcium ions into blood vessels and heart cells. A calcium antagonist significantly reduces the possibility of a stroke, however, it can cause the formation of cardiac pathology. This group of drugs includes substances with different chemical components. Calcium channel blockers belong to the 1st or 2nd generation. Among the disadvantages of such drugs is their rapid removal from the blood and a narrow range of therapeutic effects. III generation calcium channel blockers stay in the blood longer.

In addition, the use of an endothelial receptor antagonist is common.

Efficacy in hypertension

Taking ß-blockers allows you to:

1. lower blood pressure;
2. reduce the risks of developing myocardial infarction and cardiac ischemia;
3. reduce the likelihood of death after a heart attack;
4. reduce the frequency of cardiac arrhythmia.

With sufficiently high effectiveness, beta blockers are inexpensive.

The degree of pressure reduction is directly proportional to the initial values. Medicines in this series reduce it by approximately 20/15 mmHg. Compared to the effect of thiazide diuretics, these figures are somewhat lower. It is not without reason that the latter are used as first-line drugs in the treatment of arterial hypertension. They are also easier to tolerate by patients. However, in approximately 60% of patients, blood pressure returns to normal solely under the influence of beta blockers.

Types of adrenergic blockers

In 1949, scientists found that the walls of blood vessels and heart tissue contain several types of receptors that respond to adrenaline and norepinephrine:

• Alpha 1, alpha 2.
• Beta 1, beta 2.

Under the influence of adrenaline, receptors produce impulses that cause vasoconstriction, increased heart rate, increased blood pressure and glucose levels, and dilation of the bronchi. In people with arrhythmia and hypertension, this reaction increases the likelihood of a hypertensive crisis and heart attack.

The discovery of receptors and the study of the mechanism of their operation served as the basis for the creation of a new class of medications for the treatment of hypertension:

• alpha-blockers;
• beta blockers.

Beta-blockers play the main role in the treatment of arterial hypertension; alpha blockers have an auxiliary role.

Alpha blockers

All drugs of this type are divided into 3 subgroups. The classification is based on the mechanism of action on receptors: selective - blocking one type of receptor, non-selective - blocking both types of receptors (alpha 1, alpha 2).

In case of arterial hypertension, it is necessary to block alpha1 type receptors. Doctors prescribe alpha 1-blockers for this purpose:

• Doxazosin.
• Terazosin.
• Prazonin.

These medications have a small list of side effects, one significant drawback and several advantages:

• have a positive effect on cholesterol levels (total), thereby inhibiting the development of atherosclerosis;
• they are not dangerous to take for people suffering from diabetes; when consumed, the blood sugar level remains unchanged;
• blood pressure decreases, while the pulse rate increases slightly;
• male potency does not suffer.

Flaw

Under the influence of an alpha blocker, all types of blood vessels (large, small) expand, so the pressure decreases more when a person is in an upright position (standing). When using an alpha blocker, a person's natural mechanism for normalizing blood pressure when rising from a horizontal position is disrupted.

A person may faint if they abruptly assume a vertical position. When he gets up, his blood pressure drops sharply, and oxygen supply to the brain deteriorates. The person feels severe weakness, dizziness, and darkening of the eyes. In some cases, fainting is inevitable. It is only dangerous due to injuries from a fall, since after assuming a horizontal position, consciousness returns and the pressure returns to normal. This reaction occurs at the beginning of treatment, when the patient takes the first tablet.

Mechanism of action and contraindications

After taking a tablet (drops, injections), the following reactions occur in the human body:

• the load on the heart decreases due to the expansion of small veins;
• blood pressure levels decrease;
• blood circulates better;
• cholesterol levels decrease;
• pulmonary pressure is normalized;
• Sugar levels return to normal.

The practice of using alpha blockers has shown that for some patients there is a risk of heart attack. Contraindications to use are diseases: hypotension (arterial), renal (liver) failure, symptoms of atherosclerosis, myocardial infarction.

Side effects

Side effects are possible during alpha blocker therapy. The patient may get tired quickly, he may be bothered by dizziness, drowsiness, and fatigue. In addition, in some patients after taking the pills:

• nervousness increases;
• the functioning of the gastrointestinal tract is disrupted;
• allergic reactions occur.

You should talk to your doctor if the symptoms described above appear.

Doxazosin

The active substance is doxazosin mesylate. Additives: magnesium, MCC, sodium lauryl sulfate, starch, milk sugar. Release form: tablets. There are two types of packaging: cell from 1 to 5 in a pack, jar. The blister pack may contain 10 or 25 tablets. Number of tablets in a jar:

• 30;
• 50;
• 100.

After a single dose, the effect is observed after 2, maximum 6 hours. The action lasts for 24 hours. Food taken at the same time as Doxazosin slows down the effect of the drug. With prolonged use, left ventricular hypertrophy is possible. The drug is excreted by the kidneys and intestines.

Terazosin

The active ingredient is terazosin hydrochloride, tablets are available in two types - 2 and 5 mg. One pack contains 20 tablets, packaged in 2 blister-type packages. The drug is well absorbed (90% absorption). The effect occurs within an hour.

Most of the substance (60%) is excreted through the gastrointestinal tract, 40% through the kidneys. Terazosin is prescribed orally, starting with 1 mg for a hypertensive problem, the dose is gradually increased to 10-20 mg. It is recommended to take the entire dose before bedtime.

Prazonin

The active substance is prazonin. One tablet may contain 0.5 or 1 mg of prazonin. Medicine is prescribed for high blood pressure. The active substance promotes vasodilation:

• arteries;
• veins;
• venous vessels.

The maximum effect with a single dose should be expected from 1 to 4 hours, lasts 10 hours. A person may become accustomed to the medicine; if necessary, increase the dose.

Cautions and complications of beta blocker therapy

Before starting to take a beta blocker, the patient should be clearly informed that any independent change in the dose of the drug or discontinuation of its use can lead to the development of a pronounced withdrawal syndrome with the development of interruptions in heart function, increased blood pressure, and return of angina attacks (depending on the original indication for use). The most dangerous is abrupt withdrawal of beta blockers in patients with CHF.

Absolute contraindications to the use of any beta blockers include severe sinus bradycardia (less than 50 beats/min), grade II–III atrioventricular block, and sick sinus syndrome. The most serious limitation to the use of beta blockers is bronchial asthma, since even cardioselective beta blockers can partially increase bronchial tone.

Serious limitations may arise when using beta blockers in patients with chronic obstructive bronchitis. In all cases, when selecting a drug for patients with broncho-obstructive syndrome, the choice should fall on cardioselective beta blockers; therapy should be carried out under instrumental control of external respiration function.

In the presence of disturbances of peripheral blood flow (for example, with atherosclerotic lesions), preference is given to cardioselective beta blockers, since blockade of β2 receptors leads to a decrease in peripheral blood flow.

The presence of type 2 diabetes mellitus (DM) or dyslipidemia today is not a limitation to the use of beta blockers, especially cardioselective ones

Caution should be exercised only when prescribing beta blockers to patients with type 1 diabetes (risk of decreased sensitivity to hypoglycemia), as well as in cases of decompensation of diabetes

When using beta blockers and elderly people, the risk of developing constipation should be taken into account; in many patients, beta blocker increases the permeability of the vascular network of the nasal cavity, which is manifested by a feeling of nasal congestion and rhinorrhea (fluid flow from the nose) of a non-infectious nature.

Concerns about the possibility of developing impotence in young people when treating hypertension with beta blockers, which were expressed during the period of widespread introduction of these drugs into everyday practice, turned out to be exaggerated. It should be remembered that the root cause of impotence is often untreated hypertension, and antihypertensive drugs, including beta blockers, help restore libido and proper potency in parallel with achieving target blood pressure levels.

G.N. Kobylyanu, N.S. Manyakina, D.A. Maksimkin

2010

I generation – non-cardioselective

Non-cardioselective adrenergic blockers are the first representatives of this group of drugs. Due to the blocking of receptors of the first and second types, they can lead to side effects - bronchospasms.

With intrinsic sympathomimetic activity

Some drugs have the ability to partially stimulate beta-adrenergic receptors - this is sympathomimetic activity. The main advantage is that they practically do not slow down the heart rate and do not lead to possible withdrawal syndrome.

The list of drugs includes:

No intrinsic sympathomimetic activity

• Sotalol;
• Nadolol;
• Flestrolol;
• Nepradilol;
• Timolol.

What are adrenergic blockers

Beta blockers are popular drugs used in the treatment of cardiovascular pathologies.
Many people are interested in what they are and what their general principle of operation is. Adrenergic blockers from the alpha or beta group are aimed at neutralizing adrenaline receptors in the heart and blood vessels. In other words, these substances are ready to “turn off” those receptors that normally respond to a certain reaction to norepinephrine and adrenaline.

Therefore, the properties of adrenergic blockers are completely opposite to the properties of these hormones.

The most popular blockers

1. Professional calorie blocker PBK-20. The essence of a dietary supplement is that it absorbs harmful substances and components that enter the body with food. It is an assistant in burning fats, except for those that are immediately absorbed after eating, and fats that the body needs for full functioning. Helps speed up metabolic processes, allowing you to keep the same food in your diet, but at the same time lose pounds. A worthy advantage of PBK-20 is slow but steady weight loss (helps to avoid sudden surges in weight gain that cause global damage).

The work of the supplement comes down to the following phases: - Increase in volume when entering the digestive organ; — Absorption of dangerous elements, such as toxic substances (toxins), fats, heavy metals, excess ammonia; — Envelopment of these substances and removal from the body without a chance of absorption.

The special structure of PBK-20, consisting of fibers, retains body moisture, which facilitates the functioning of the bile ducts. Normalizes blood sugar levels and cholesterol levels. After a few doses, it adjusts the microorganisms contained in the gastrointestinal tract (beneficial intestinal microflora) to function properly.

Effective drugs

List: Effective beta-blockers in the treatment of arterial hypertension

Every year, new generation beta blockers appear. The main advantage of modern drugs is a smaller list of side effects.

Mechanism of action of drugs

These drugs can reduce the frequency along with the strength of heart contractions, thereby lowering blood pressure. As a result, oxygen consumption by the heart muscle decreases.

There is an extension of diastole - a period of rest and general relaxation of the heart, during which the vessels are filled with blood. A decrease in diastolic intracardiac pressure also contributes to improvement of coronary perfusion. There is a process of redistribution of blood flow from normally blood-supplied areas to ischemic areas, as a result of which a person’s tolerance to physical activity increases.

Beta blockers have antiarrhythmic effects. They are able to suppress the cardiotoxic and arrhythmogenic effects of catecholamines, and in addition, prevent the accumulation of calcium ions in heart cells, which worsen energy metabolism in the myocardial region.

The list of beta-blocker drugs is very extensive.

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1. Non-cardioselective beta blockers:

A. Without internal sympathomimetic activity:

• propranolol (anaprilin, obzidan);
• nadolol (korgard);
• sotalol (sotahexal, tenzol);
• timolol (blocarden);
• nipradilol;
• flestrolol.

B. With internal sympathomimetic activity:

• oxprenolol (Trazicor);
• pindolol (wisken);
• alprenolol (aptin);
• penbutolol (betapressin, levatol);
• bopindolol (Sandorm);
• bucindolol;
• dilevalol;
• carteolol;
• labetalol.

2. Cardioselective beta blockers:

A. Without internal sympathomimetic activity:

• metoprolol (betaloc, betaloc zok, corvitol, metozok, metocard, metocor, serdol, egilok);
• atenolol (betacard, tenormin);
• betaxolol (betak, lokren, kerlon);
• esmolol (breviblok);
• bisoprolol (aritel, bidop, biol, biprol, bisogamma, bisomore, concor, corbis, cordinorm, coronal, nipperten, tirez);
• carvedilol (acridilol, bagodilol, vedicardol, dilatrend, carvedigamma, carvenal, coriol, recardium, tallitone);
• nebivolol (binelol, nebivator, nebikor, nebilan, nebilet, nebilong, nevotenz, od-neb).

B. With internal sympathomimetic activity:

• acebutalol (acecor, sectral);
• talinolol (cordanum);
• celiprolol;
• epanolol (vasacor).

3. Beta blockers with vasodilating properties:

• amozulalol;
• bucindolol;
• dilevalol;
• labetolol;
• medroxalol;
• nipradilol;
• pindolol.

4. Long-acting beta blockers:

B. Cardioselective:

5. Ultra-short-acting beta blockers, cardioselective:

What drugs are beta blockers?

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

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

Attention! Selective and non-selective beta blockers lower blood pressure to the same extent. But there are fewer negative effects from taking 2nd generation cardioselective varieties, so they can be prescribed even in the presence of concomitant pathologies.

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

At the same time, although they do not cause vasospasm and a strong decrease in the pulse, they are still poorly able to stop attacks of angina pectoris, acute coronary syndrome, and also do not provide proper exercise tolerance after taking them. The list of such drugs includes Celiprolol, Pindolol, Oxprenolol, Acebutolol.

Advice. When starting to take the medicine, find in the instructions a mention of which type - lipophilic (fat-soluble) or hydrophilic (water-soluble) the tablets are. This determines when to take them, before or after eating.

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