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Selective adrenergic blockers list of drugs. Adrenergic blockers: action, application features

Irina Zakharova

Beta blockers are drugs that affect the sympathoadrenal system of the human body, which regulates the functioning of the heart and blood vessels. In case of hypertension, substances included in medications block the effect of adrenaline and norepinephrine on the receptors of the heart and blood vessels. The blockade helps to dilate blood vessels and reduce heartbeat.

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.

Receptors, under the influence of adrenaline, 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 a person uses an alpha blocker, the 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:

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;
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.
Beta blockers
Beta-blockers for hypertension provide real help to patients. They are included in patient treatment regimens. In the absence of allergic reactions and contraindications, the medicine is suitable for most people. Taking blocker tablets reduces the symptoms associated with hypertension and serves as a good prevention for it.

The substances included in the composition block the negative effect on the heart muscle:
lower blood pressure;
improve general condition.

By giving preference to such medications, you can not be afraid of hypertensive crises and stroke.
Species
The list of medications for hypertension is wide. It includes selective and non-selective drugs. Selectivity is a selective influence on only one type of receptor (beta 1 or beta 2). Non-selective agents affect both types of beta receptors simultaneously.

When taking beta blockers, patients experience the following symptoms:
heart rate decreases;
pressure decreases noticeably;
the tone of blood vessels becomes better;
the formation of blood clots slows down;
body tissues are better supplied with oxygen.

In practice, beta-blockers are widely used to treat patients with arterial hypertension. Cardioselective and non-cardioselective blockers can be prescribed.
List of cardioselective beta blockers
Let's look at a description of several of the most popular medications. They can be purchased without a prescription at the pharmacy, but self-medication can lead to serious consequences. Taking beta blockers is possible only after consulting a doctor.

List of cardioselective drugs:
Atenolol.
Metoprolol.
Acebutolol.
Nebivolol.

Atenolol
Long-acting drug. At the initial stage, the dosage rate per day is 50 mg, after some time it can be increased, the maximum daily dose is 200 mg. An hour after taking the drug, the patient begins to feel the therapeutic effect.
The therapeutic effect lasts throughout the day (24 hours). After two weeks, you must visit a doctor to assess the effectiveness of drug treatment. The blood pressure should normalize by the end of this period. Atenolol is available in the form of 100 mg tablets, packaged in jars of 30 pieces or in blister packs of 10 pieces.

Metoprolol
When taking Metoprolol, a rapid decrease in blood pressure occurs, the effect occurs after 15 minutes. The duration of the therapeutic effect is short - 6 hours. The doctor prescribes a frequency of doses from 1 to 2 times a day, 50–100 mg at a time. You can take no more than 400 mg of Metoprolol per day.
The product is available in the form of 100 mg tablets. In addition to the active ingredient metoprolol, they include auxiliary substances:
lactose monohydrate;
cellulose;
magnesium stearate;
povidone;
potato starch.

The substance is excreted from the body through the kidneys. In addition to hypertension, Metropolol is effective as a prophylactic agent for angina, myocardial infarction, and migraine.

Acebutolol
The daily dose of Acebutolol is 400 mg. Take it 2 times. During treatment, the doctor may increase the dosage per day to 1200 mg. The greatest therapeutic effect is felt by patients who, along with high blood pressure, are diagnosed with ventricular arrhythmia.
The medicine is available in two forms:
0.5% solution for injection in 5 ml ampoules;
tablets weighing 200 or 400 mg.

Acebutolol is excreted from the body through the kidneys and gastrointestinal tract 12 hours after administration. The active substance may be contained in breast milk. This must be taken into account by breastfeeding women.
Nebivolol
You can evaluate the effect of the drug 2 weeks after starting treatment. In addition to lowering blood pressure, the medicine has an antiarrhythmic effect. By the end of the fourth week of treatment, the patient’s blood pressure should be established, and by the end of 2 months of the course of treatment it should become stable.

Nebivolol is produced in the form of tablets, packaged in cardboard boxes. The active substance is nebivolol hydrochloride. Its elimination from the body depends on the person’s metabolism; the higher the metabolism, the faster it is eliminated. Excretion occurs through the gastrointestinal tract and kidneys.
The daily norm for an adult is from 2 to 5 mg per day. After the patient adapts to the drug, the daily dose can be increased to 100 mg. The greatest effect is achieved by taking the drug at the same time.
Non-cardioselective drugs
The group of non-cardioselective blood pressure drugs includes the following beta-blockers:
Pindolol.
Timolol.
Propranolol.

Pindolol is prescribed according to the following regimen: 5 mg 3–4 times a day. It is possible to increase the single dose to 10 mg when taken 3 times during the day. This drug is prescribed in moderate doses to patients diagnosed with diabetes mellitus.

Timolol for the treatment of hypertension is prescribed at a dose of 10 mg twice a day. If there is a need for health reasons, the daily dose is increased to 40 mg.
Beta blockers should be discontinued under the supervision of a physician. The patient's blood pressure may rise sharply. If the patient refuses to take it, a gradual reduction in the daily dose is recommended over the course of a month.

The group of adrenergic blockers includes drugs that can block the nerve impulses responsible for the reaction to adrenaline and norepinephrine. These drugs are used to treat pathologies of the heart and blood vessels.

Most patients with relevant pathologies are interested in what adrenergic blockers are, when they are used, and what side effects they can cause. This will be discussed further below.

Classification

The walls of blood vessels have 4 types of receptors: α-1, α-2, β-1, β-2. Accordingly, alpha and beta blockers are used in clinical practice. Their action is aimed at blocking a specific type of receptor. A-β blockers turn off all adrenaline and norepinephrine receptors.

Tablets of each group come in two types: selective ones block only one type of receptor, non-selective ones interrupt communication with all of them.

There is a certain classification of drugs in the group under consideration.

Among alpha-blockers:

α-1 blockers;
α-1 and α-2.

Among β-blockers:

cardioselective;
non-selective.

Features of the action

When adrenaline or norepinephrine enters the blood, adrenergic receptors react to these substances. In response, the following processes develop in the body:

the lumen of blood vessels narrows;
myocardial contractions become more frequent;
blood pressure rises;
glycemic levels increase;
the bronchial lumen increases.

In case of pathologies of the heart and blood vessels, these consequences are dangerous to human health and life. Therefore, in order to stop such phenomena, it is necessary to take drugs that block the release of adrenal hormones into the blood.

Adrenergic blockers have the opposite mechanism of action. The way alpha and beta blockers work differs depending on what type of receptor is blocked. For various pathologies, adrenergic blockers of a certain type are prescribed, and their replacement is strictly unacceptable.

Action of alpha-blockers

They dilate peripheral and internal vessels. This allows you to increase blood flow and improve tissue microcirculation. A person’s blood pressure drops, and this can be achieved without an increase in heart rate.

These drugs significantly reduce the load on the heart by reducing the volume of venous blood entering the atrium.

Other effects of α-blockers:

reduction of triglycerides and bad cholesterol;
increase in the level of “good” cholesterol;
activation of cell sensitivity to insulin;
improved glucose absorption;
reducing the intensity of signs of inflammation in the urinary and reproductive systems.

Alpha-2 blockers constrict blood vessels and increase pressure in the arteries. They are practically not used in cardiology.

Action of beta blockers

The difference between selective β-1 blockers is that they have a positive effect on heart function. Their use allows you to achieve the following effects:

reducing the activity of the heart rate driver and eliminating arrhythmia;
decrease in heart rate;
regulation of myocardial excitability against the background of increased emotional stress;
decreased oxygen demand of the heart muscles;
decrease in blood pressure indicators;
relief of angina attack;
reducing the load on the heart during cardiac failure;
decrease in glycemic levels.

Non-selective β-blocker drugs have the following effects:

prevention of blood elements clumping;
increased contraction of smooth muscles;
relaxation of the bladder sphincter;
increased bronchial tone;
decrease in intraocular pressure;
reducing the likelihood of acute heart attack.

Action of alpha-beta blockers

These drugs reduce blood pressure inside the eyes. Helps normalize triglycerides and LDL levels. They give a noticeable hypotensive effect without disturbing blood flow in the kidneys.

Taking these drugs improves the mechanism of adaptation of the heart to physical and nervous stress. This allows you to normalize the rhythm of its contractions and alleviate the patient’s condition with heart defects.

When is medication indicated?

Alpha1-blockers are prescribed in the following cases:

arterial hypertension;
enlargement of the heart muscle;
prostate enlargement in men.

Indications for use of α-1 and 2 blockers:

trophic disorders of soft tissues of various origins;
severe atherosclerosis;
diabetic disorders of the peripheral circulatory system;
endarteritis;
acrocyanosis;
migraines;
post-stroke condition;
decrease in intellectual activity;
disorders of the vestibular apparatus;
bladder neurogenicity;
inflammation of the prostate.

Alpha2-blockers are prescribed for erectile disorders in men.

Highly selective β-blockers are used in the treatment of diseases such as:

arterial hypertension;
hypertrophic type cardiomyopathy;
arrhythmias;
migraine;
mitral valve defects;
heart attack;
with VSD (with hypertensive type of neurocirculatory dystonia);
motor agitation when taking antipsychotics;
increased thyroid activity (complex treatment).

Non-selective beta blockers are used for:

arterial hypertension;
enlargement of the left ventricle;
angina pectoris with exertion;
dysfunction of the mitral valve;
increased heart rate;
glaucoma;
Minor's syndrome - a rare nervous genetic disease in which tremor of the hand muscles is observed;
for the purpose of preventing hemorrhage during childbirth and operations on the female genital organs.

Finally, α-β blockers are indicated for the following diseases:

for hypertension (including to prevent the development of hypertensive crisis);
open-angle glaucoma;
stable type angina;
heart defects;
heart failure.

Use for pathologies of the cardiovascular system

β-blockers occupy a leading place in the treatment of these diseases.

The most selective are Bisoprolol and Nebivolol. Blocking adrenergic receptors helps reduce the degree of contractility of the heart muscle and slow down the speed of nerve impulses.

The use of modern beta blockers gives the following positive effects:

decreased heart rate;
improvement of myocardial metabolism;
normalization of the vascular system;
improvement of left ventricular function, increase in its ejection fraction;
normalization of heart rate;
drop in blood pressure;
reducing the risk of platelet aggregation.

Side effects

The list of side effects depends on the drugs.

A1 blockers can cause:

swelling;
a sharp drop in blood pressure due to a pronounced hypotensive effect;
arrhythmia;
runny nose;
decreased libido;
enuresis;
pain during erection.

A2 blockers cause:

increased blood pressure;
anxiety, irritability, increased excitability;
muscle tremors;
urinary disorders.

Non-selective drugs in this group can cause:

appetite disorders;
sleep disorders;
increased sweating;
feeling of coldness in the extremities;
feeling of heat in the body;
hyperacidity of gastric juice.

Selective beta blockers may cause:

general weakness;
slowing down nervous and mental reactions;
severe drowsiness and depression;
decreased visual acuity and impaired taste perception;
numbness of the feet;
drop in heart rate;
dyspeptic symptoms;
arrhythmic phenomena.

Non-selective β-blockers can exhibit the following side effects:

visual disturbances of various types: “fog” in the eyes, the feeling of a foreign body in them, increased production of tears, diplopia (“double vision” in the visual field);
rhinitis;
suffocation;
pronounced drop in pressure;
syncope;
erectile dysfunction in men;
inflammation of the colon mucosa;
hyperkalemia;
increased levels of triglycerides and urates.

Taking alpha-beta blockers can cause the following side effects in the patient:

thrombocytopenia and leukopenia;
a sharp disturbance in the conduction of impulses emanating from the heart;
dysfunction of peripheral circulation;
hematuria;
hyperglycemia;
hypercholesterolemia and hyperbilirubinemia.

List of drugs

Selective (α-1) adrenergic blockers include:

Eupressil;
Tamsulon;
Doxazosin;
Alfuzosin.

Non-selective (α1-2 blockers):

Sermion;
Redergin (Klavor, Ergoxil, Optamine);
Pyrroxane;
Dibazin.

The most famous representative of α-2 adrenergic blockers is Yohimbine.

List of drugs from the β-1 adrenergic blocking group:

Atenol (Tenolol);
Lokren;
Bisoprolol;
Breviblock;
Celiprol;
Cordanum.

Non-selective β-blockers include:

Sandorm;
Betalok;
Anaprilin (Obzidan, Poloten, Propral);
Timolol (Arutimol);
Slowtrazicore.

New generation medicines

New generation adrenergic blockers have many advantages over “old” drugs. The advantage is that they are taken once a day. The latest generation of products cause much fewer side effects.

These medications include Celiprolol, Bucindolol, Carvedilol. These drugs have additional vasodilating properties.

Reception features

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 for use

Pregnancy and breastfeeding period.
Allergic reaction to a medicinal component.
Severe disorders of the liver and kidneys.
Decreased blood pressure (hypotension).
Bradycardia is a decrease in heart rate.

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β-adrenergic receptor blockers, or β-blockers, are a group of drugs that can reversibly block β-adrenergic receptors. They have been used in clinical practice since the early 60s of the 20th century for the treatment of coronary artery disease and cardiac arrhythmias; later they began to be used for the treatment of hypertension, and subsequently for the treatment of heart failure. The importance of β-blockers for the secondary prevention of diseases of the cardiovascular system turned out to be so high that in 1988 the scientists who took part in the creation of this group of drugs were awarded the Nobel Prize. In recent years, after obtaining the results of several large controlled clinical trials and meta-analyses, the range of use of β-blockers has narrowed somewhat, primarily due to their less active use as drugs for primary prevention in patients with hypertension.

Mechanism of action

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

Pharmacokinetics

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

Table 1

Main properties of β-blockers used in the clinic

Preparation	Presence of β1-selectivity	Presence of intrinsic sympathomimetic activity	Presence of vasodilating properties	T1/2
Atenolol Betaxolol Bisoprolol Carvedilol Metoprolol Nadolol Nebivolol Pindolol Proxodolol Propranolol Sotalol Talinolol Timolol Esmolol	Yes Yes Yes No Yes No Yes No No data No No Yes No Yes	No No No No No No No Yes No No Yes Yes No No	No No No Yes No No Yes No Yes No No No No No	6-9 hours 16-22 h 7-15 h 6 hours 3-7 hours 10-24 h 10 o'clock 2-4 hours No data 2-5 hours 7-15 h 6 hours 2-4 hours 9 min

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

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

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

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

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

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

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

Groups of β-blockers depending on fat solubility

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

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

Groups of β-blockers depending on metabolism in the liver

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

These properties of the drugs have virtually no clinically significant effect.

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

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

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

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

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

β-blockers of medium duration of action. The effect of regular metoprolol tartrate tablets lasts from 8 to 10 hours, so they must be prescribed 2 or even 3 times a day.
Short-acting β-blockers. The shortest-acting drugs include esmolol. Its antianginal and antihypertensive effect lasts only 10-20 minutes after stopping the infusion.

Martsevich S.Yu., Tolpygina S.N.

Beta blockers

High blood pressure is a cardiovascular risk parameter. Therefore, according to the latest recommendations, the goals of drug therapy for hypertension are not only to achieve its reduction and sustainable control, but also to prevent heart attack, stroke and death.

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

Some studies indicate that long-term treatment with beta-blockers (BABs) cause negative metabolic effects, which significantly increases the risk of complications, especially in patients with coronary heart disease. Others indicate their high effectiveness for recent heart attacks due to heart failure. Nevertheless, beta blockers continue to confidently occupy third place in the list of antihypertensive drugs.

Let's try to figure out in what cases their use will be safe, and, perhaps, will bring additional benefits, and for whom it is not recommended to drink beta-blockers, even if they are of the latest generation.

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

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

Since the topic of our article is BAB, let’s consider how stimulation of β-receptors affects the functioning of body systems. Under the influence of the adrenal hormone and similar substances, they, in addition to increasing the release of renin in the kidneys, perform various functions.

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

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

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

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

In addition, the resulting side effects significantly narrowed the number of patients who needed such drugs. However, today there are already 3 generations of BAB.

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

What drugs are beta blockers?

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

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

List of BAB generations - name, synonyms and analogues	Characteristics, depending on the effect on adrenergic receptors
	This is a subgroup of non-selective beta blockers. They inhibit adrenergic receptors of both alpha and beta types with equal force. Suppression of the latter causes negative side effects that limit their use
	This category of beta blockers is selective for β-2 receptors. It received the general name “Cardioselective drugs”. 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.
	These modern drugs have not only cardioselective effects. They have a vasodilating effect. They know how to relax the vessels of the circulatory system. Labetalol does this by blocking alpha-adrenergic receptors, Nebivolol enhances vascular relaxation in the periphery, and Carvedilol does both at the same time.

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.

Indications for use and warnings

Detailed comparative characteristics of beta blockers are understandable only to highly specialized cardiologists. Based on it, taking into account the real results in the achieved indicators of lowering blood pressure and improving (worsening) the well-being of a particular patient, individual doses are selected, and possibly combined forms of beta-blockers with other blood pressure medications. You should be patient, as this may take considerable time, sometimes about a year.

In general, β-blocker drugs can be prescribed for:

, primary hypertension, stable chronic heart failure, ischemic heart disease, arrhythmias, previous heart attack, UI-QT syndrome, ventricular hypertrophy, protrusion of the mitral valve leaflets, hereditary Morphan's disease;
secondary hypertension caused by pregnancy, thyrotoxicosis, kidney damage;
increased blood pressure before and after surgery;
vegetative-vascular crises;
glaucoma;
persistent migraines;
drug, alcohol or drug withdrawal.

FYI. Just recently, the cost of some new beta blockers was exorbitant. Today there are many synonyms, analogues and generics, which are not inferior in their effectiveness to the promoted patented BAB drugs, and their price is quite affordable even for low-income pensioners.

Contraindications

The administration of any type of beta-blockers to patients with II-III degree atrioventricular block is absolutely prohibited.

Relative ones include the presence of:

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

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

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

Side effects

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

The most common among them are:

development of general weakness;
decreased performance;
increased fatigue;
dry cough, asthma attacks;
cold hands and feet;
bowel disorders;
drug-induced psoriasis;
sleep disturbances accompanied by nightmares.

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

Withdrawal syndrome

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

However, patients suffering from angina should not be surprised. They will have to take the long-acting form of the beta-blocker twice - both in the morning and in the evening. For them, there is also a warning about observing a gradual withdrawal from treatment with beta blockers, since their sudden withdrawal can cause a significant worsening of the disease.

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

And at the end of this article, we suggest watching a video that talks about medications that are prohibited for simultaneous use with beta-blockers.

Frequently asked questions to the doctor

My husband's anniversary is approaching. He was recently prescribed Carvedilol. Can he drink alcoholic beverages?

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

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

There are also paradoxical cases when beta blockers do not reduce, but rather enhance the effect of the drug - the pressure drops sharply, the heart slows down. Even cases of death have been recorded.

What can replace beta blockers?

Based on the principles of the mechanism of action, beta blockers can only be replaced with them, and switch from one type of medication to another. However, not all patients with problems in the cardiovascular system achieve the desired result, and some experience severe side effects that interfere with a normal lifestyle.

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

Nowadays, drug therapy is effectively carried out using all kinds of drugs, including completely new ones. Beta blockers are good for hypertension and heart disease. It is the drugs from this category that are most often used to restore normal functioning of the cardiac and vascular system and lower blood pressure.

It is extremely important to choose the right drugs, taking into account the distinctive features of beta blockers from different groups. In addition, possible side effects must be taken into account. If you provide an individual approach to the treatment of each patient, you can achieve excellent results. Today we will look at the main differences, features, principles of action and advantages of various beta blockers.

The key task of these drugs is to prevent the negative effects of adrenaline on the heart. The fact is that due to the influence of adrenaline, the heart muscle suffers, pressure rises and the overall load on the cardiovascular system increases significantly.

Beta blockers are actively used in modern practice for the drug treatment of tachycardia, heart failure and metabolic syndrome, and coronary heart disease.

Let's consider the basic principles of treatment using drugs in this category.

Experts note that high blood pressure does not always require treatment throughout the patient’s life. In some cases, the problem can be resolved. This is due to the fact that the pressure increased due to a specific pathology. If you manage to get rid of it, stop it completely, then the pressure also returns to normal, without requiring further therapy.

Treatment with one drug

There is one important principle in drug therapy using beta blockers. Doctors use only one drug at the initial stage of treatment. This minimizes the risk of side effects. This also has a positive effect on the psychological state of the patient.

When a medicine is selected, its dosage is gradually increased to the maximum level.

Selection of medicine

If low efficiency is observed, positive dynamics are completely absent, it is necessary to add new drugs or replace the drug with another.

The fact is that sometimes drugs simply do not have the desired effect on the patient’s body. They may be effective, but a particular patient is not receptive to them. Everything here is strictly individual, depending on the numerous characteristics of the body.

Therefore, therapy must be carried out with special care, taking into account all the individual characteristics of the patient.

Nowadays, preference is increasingly given to long-acting drugs. In them, active substances are released gradually, over a long period of time, having a gentle effect on the body.

Professional treatment

It is very important to remember: if you have hypertension or high blood pressure, you should never take medications or prescribe beta blockers to yourself. It is strictly not recommended to self-medicate or limit yourself only to the use of folk remedies.

For hypertension, it is necessary to carry out comprehensive treatment under the supervision of a doctor and carefully monitor your health. Sometimes measures have to be taken throughout life. This is the only way to maintain normal health and remove the threat to life.

Classification of beta blockers

There is a whole range of types of beta blockers. All these remedies have a positive effect on the heart and blood vessels. The level of effectiveness in each specific case will depend on many factors.

Read what a hypertonic solution is. We will look at the main categories of drugs, talk about their advantages and features. However, when prescribing drug therapy, the last word remains with the doctor, since an individual approach to each patient is required.

There are hydrophilic beta blockers. They are used when an effective effect on the body in an aquatic environment is necessary. Such drugs are practically not transformed in the liver, leaving the body in a slightly changed form. First of all, such drugs are used if there is a need for prolonged action. The substances in them remain practically unchanged, are released for a long time and have a long-lasting effect on the body. This group included esmolol,.
Beta blockers from the lipophilic group dissolve faster and more efficiently in fat-like substances. Such drugs are most in demand if it is necessary to cross the barrier between the nervous system and blood vessels. The liver is where the main processing of the active substances of drugs takes place. This category of medications includes propranolol,.
There is also a group of non-selective beta blockers. These drugs act on two beta receptors: beta 1 and beta 2. Among non-selective drugs, carvedilol and nadolol are known.
Selective drugs only affect beta-1 receptors. Their influence is selective. Most often, such medications are called cardioselective, since many beta-1 receptors are found in the heart muscle. If you gradually increase the dose of drugs from this group, they begin to have a positive effect on both types of receptors: beta-2 and beta-1. Cardioselective drugs include metaprolol,.
The drug is also widely known, which experts consider separately. The key active ingredient in the medicine is bisoprolol. The product is neutral and has a mild effect on the body. There are practically no side effects observed, the metabolic processes of carbohydrates and lipids are maintained without disturbances. Most often, Concor is recommended for those who already have diabetes or are suspected of being predisposed to developing this disease. The thing is that Concor does not affect the level of glucose in the blood at all, so hypoglycemia will not develop because of it.
In general drug therapy, alpha blockers can also be used as auxiliary drugs. They are designed to stop the effect of beta-adrenergic receptors on the body. Beta blockers have a similar effect. Such drugs help to normalize the functioning of the genitourinary system; they are also prescribed in the treatment of prostate adenoma. This group includes terazosin and doxazosin.
have minimal side effects, ensure safety for the body, while the medicinal properties of the drugs are significantly improved. The most modern, safe, effective beta blockers are celiprolol,.

It is important to remember: it is unacceptable to choose medications for the treatment of hypertension in person, without a prescription.

Almost all drugs have serious contraindications and can cause unpredictable side effects. Just reading the instructions is not enough. However, these drugs have quite a serious effect on the body. You should take medications only as prescribed by a doctor, under supervision.

Let's find out how to properly take beta blockers for hypertension. First of all, you need to check with your doctor what concomitant diseases you have. This plays a big role, since the drugs have quite a lot of contraindications.

You also need to tell whether you are pregnant, whether you are planning to have a child, or conceive in the near future. All this is very important when treating with beta blockers. Hormonal levels are of great importance.

Doctors often give the following recommendation: you need to regularly monitor your blood pressure levels and record readings several times a day. Such data is very useful during the treatment process, it will allow you to create a clearer clinical picture of the course of the disease and find out how well the drugs affect the body.

Constant monitoring by a doctor while taking beta blockers is necessary, since only a specialist can competently monitor drug therapy, monitor the likely occurrence of side effects, and evaluate the effectiveness of treatment and the effects of drugs on the body. Only a doctor, having carefully studied all the individual characteristics of the patient’s body, can correctly determine the frequency of use and dose of beta blockers.

If any surgical intervention is planned, or the use of anesthesia, even for tooth extraction, the doctor must be informed that the person is taking beta blockers.