The effectiveness of beta blockers in the fight against hypertension and heart disease. Full overview of all types of adrenoblockers: selective, non-selective, alpha, beta in blockers classification

18.08.2020

Drugs from hypertension categories of beta-adrenobloclars can easily learn from the scientific name with the ending "Lol". If the doctor prescribes a beta blocker, tell him that he discharges the prolonged action medication. Such a medication can cost more, but the prolonged means is accepted only once a day. It has great importance For men and women of older age, which are prone to forgetfulness and may accidentally skip the time of reception of the tablets.

Pills

Beta-adrenoblastors did not show hypotensive properties to the first clinical experiments. Scientists and did not wait for them. However, as it turned out, the first beta-blocker was capable of reduced the pressure value in patients with arterial hypertension and angina. In the future, the hypotensive property was found in propranolol and other beta blockers.

Classification

Chemical composition Drugs of the category of beta-adrenoblockers are not ungeneged, and therapeutic effects do not depend on it. It is more important to consider the specifics of the interaction of drugs with specific receptors and how compatible they are. The more specificity to beta-1 receptors, the less negative concomitant actions. Therefore, beta-adrenobloclars - a list of drugs of a new generation - will be properly present:

First generation: non-selective preparations for the first and second receptors: Satolol, propranolol, ndolol, oxprenolol, thymolol;
Second generation: selective drugs to the first-type receptors: Acelebalol, metaprolol, atenolol, anaprilin, esmolol;
Third generation: Cardooselective blocking agents for beta-1 receptors with additional drug actions: Talinolol, betaxalol, nebivolol. This also includes non-selective blocking compounds of beta-1 and beta-2, having concomitant drug properties: bucindolol, carvedilol, labetalol. Carolol.

The listed beta-adrenoblasts in different periods were the main category of drugs used and used in the diseases of heart and vessels. Most of Appointed drugs refers to the last two generations. Thanks to them pharmacological actions There was an opportunity to keep under control the heart rate, to conduct an ectopic pulse to ventricular departments, reducing the risks of anginal angina attacks.

The most first medicines among beta adrenoblockers are tools from the first category indicated in the classification table - non-selective beta blockers. These drugs block the first and second type of receptors, providing, in addition to therapeutic effect, a negative effect in the form of bronchospasm. Therefore, they are not recommended for chronic pathologies of lungs and bronchi, asthma.

In the second generation, beta-adrenerboators are indicated, whose principle of operation is conjugate with the blockade only for the first type of receptors. They have a weak relationship with beta-2 receptors, so side effects In the form of a spasm of bronchi in patients suffering from pulmonary diseases, rarely occur.

Features of the mechanism of drugs

The effect of reducing blood pressure of this category is determined directly to their beta-adrenoblocking property. Blocking adrenoreceptors quickly acts on the heart - the number of abbreviations is reduced, and its efficiency increases.

The mechanism of operation of blockers

Beta adrenoblockers on people in healthy and calm state do not affect, that is, pressure remains normal. But in patients with hypertension, this effect is necessarily present. Beta blockers work with stressful situations and physical Loads. In addition, on the background of blocking beta receptors, the production of renin substance is reduced. Therefore, the intensity of the production of an angiotensine of the second type decreases. And this hormone affects hemodynamics and stimulates the production of aldosterone. Thus, the activity of the renin-angiotensin system decreases.

Medical properties

Beta-adrenobloclars of different generations differ from each other by selectivity, solubility in fats, the presence of internal sympathomimetic activity (the property is selectively activated by the suppressed adrenoreceptors, which reduces the number of side effects). But at the same time, all drugs have the same hypotensive effect.

Important! Almost all beta-blockers reduce the bloodstream in the kidneys, but this is not reflected in the functional ability of the organ even with long-term reception of drugs.

Reception rules

Adrenoblockers receptors give an excellent effect with hypertension of all degrees. Despite the substantial pharmacokinetic differences, they have a rather long hypotensive effect. Therefore, one or two drug receptions are enough per day. Beta blockers give a less pronounced effect in people with dark skin and patients of mature age, however there are exceptions.

Tablet reception

The reception of these drugs in hypertension does not lead to water delay and salt compounds in the body, so it does not have to prescribe diuretics to prevent hypertensive edema. It is worth noting that diuretic medicines and beta-adrenoblays enhance general effect Pressure drops.

Side effects

Beta-adrenoblockers doctors are not prescribed astmatics, patients with a weakness of a sinus node, patients with pathologies of atrioventricular conductivity. The reception of beta-blockers during pregnancy is prohibited, especially in the last months.

Adrenoblockers are not always prescribed to people suffering from simultaneously IBS, hypertension, hsn or cardiomyopathy, since these drugs reduce myocardial reductions and at this time increase the overall resistance of vascular walls. Beta blockers are not suitable for diabetics with insulin addiction. They cannot be used in conjunction with calcium channel blockers.

These drugs without ACC increase the content of triglycerides in the blood plasma. In this case, the concentration of HDL cholesterol decreases, but the total cholesterol in the blood remains unchanged. Beta-adrenoblockers from the BCA practically do not change the lipid picture and can even increase the value of HDL cholesterol. Further consequences of this action were not studied.

Side properties

If sharply cancel the use of β-adrenobloclars, this can cause a ricochetic syndrome, which manifests itself with such symptomatic signs:

Tachycardia;
A sharp increase in pressure;
Heart impairment, arrhythmias;
Ischemic attacks;
Tremble in body and chills limbs;
Acute attacks of angina;
The risk of infarction;
In rare cases, death.

Attention! Almost under strict control and with constant observation, slowly reducing the dose over two weeks, while the body is not accustomed to function without medication.

The hypotensive effect of the β-adrenoblocker can be weakened by the reception of non-steroidal anti-inflammatory agents, for example, indoentacin.

A significant increase in the pressure in the vessels in response to the use of adrenobloclockers can be observed in patients with hypoglycemia and a peochromocytoy. This side effect sometimes occurs when the adrenaline dose is introduced.

First generation adrenoblors

These non-selective drugs block adrenoreceptors β1 and β2. However, they have several side effects: a decrease in the lumen of the bronchi, cough stimulation, an increase in the tone of the muscle system of the uterus, hypoglycemia, etc. In the list of first-generation drugs are presented:

Propranolol. This medicine in a certain respect has become the standard with which the remaining adrenoblocators are compared. It does not have ACM and no selectivity with alpha-adrenoreceptors. It has good fat solventness, so quickly gets to the central nervous system, soothing and reducing pressure. Duration therapeutic effect It is 8 hours.
Pindolol. In the preparation there is an ACA. The tool has an average fat solventness, a weakly pronounced stabilizing effect.
Timolol. The adrenoblocator in which there is no WSA. It received widespread use in ophthalmological practice with glaucoma therapy, relieving eye and cilia inflammation. However, in the case of the use of thymolol for eye in the form of droplets, an acute systemic effect may be observed, accompanied by a chopping, decompensation of heart failure.

Timolol

Second generation of drugs

Adrenoblocators with cardiodelectivity to beta-1 receptors have much less side effects, but when taking increased doses The remaining adrenoreceptors can be blocked in indiscriminately, that is, they have relative selectivity. Consider briefly the properties of drugs:

Atenol - used earlier in demand in cardiological practice. This is a water-soluble medicine, therefore it is difficult for him to pass through the hemat andthelical wall. Does not have in the composition of the BCA. As a side effect, the ricochet syndrome may appear.
Metoperol is a highly selective adrenoblocator that has excellent fat solventness. Therefore, it is used in the form of saline compounds of succinate and tartrate. Due to this, its solubility is improved and the duration of transportation in the vessels is reduced. The production technique and the type of salt provide long-term therapeutic action. Metoprolol Tartrate is a classic form of metoprolol. The duration of its effect is 12 hours. It can be produced under such names: Methodogramard, Betalok, Egilov, etc.
Bisoprolol is the most popular beta adrenoblocator. It does not contain ACC. The medicine has a high cardo selectivity. The purpose of the bisoprolol is allowed with diabetes and thyroid diseases.

Third generation drugs

Adrenobloclars of this category have an additional vasodilator action. The most effective from the point of view of therapy with the preparations of the Third Group is considered:

Carvedilol is a non-selective type blocker that does not have ACC. Increases the lumens of peripheral vascular branches, blocking alpha-1 receptors. It has antioxidant properties.
Nebivolol - remedy with vasodilatory effect and high selectivity. Such properties ensures stimulation of nitrogen oxide. A steady hypotensive effect begins two weeks of treatment, in some cases four weeks later.

Carvedilol

Attention! It is impossible to assign beta adrenoblastors without a doctor. Before therapy necessarily need to get medical recommendations, explore the instructions for the medicine, read about it in Wikipedia.

Contraindications

Adrenoblockers, like many drugs, have certain contraindications. Since these tools affect adrenoreceptors, they are less dangerous compared to their antagonists - ACE inhibitors.

Common list of contraindications:

Asthma and chronic pulmonary diseases;
Any types of arrhythmias (rapid or slow heartbeat);
Sinus node weakness syndrome;
Ventricular atrial blockade in the second stage of development;
Hypotension with severe symptoms;
Tooling the fetus;
Childhood;
Decompensation XSN.

Allergies to the constituent drug becomes contraindication. If an allergic reaction begins for some kind of drug, it is replaced. In various sources of literature, analogs and substitutes of drugs are indicated.

Efficiency of adrenoblocators

Under angina, adrenoblockers significantly reduce the risks of systematic seizures and the severity of their flow, reduce the likelihood of progression of vascular pathologies.

In case of insufficiency, myocardial beta-blocking agents, inhibitors, adrenolics and diuretic medicines increase the lifetime. These medicines effectively regulate tachycardia and arrhythmia.

In general, these funds help keep control of any heart disease under control, keeping pressure at a normal level. In modern therapeutic practice, the blockers of the third group are predominantly used. The second category is prescribed, with selectivity to beta-1 receptors. The use of such drugs makes it possible to keep control of arterial hypertension and struggle with cardiovascular diseases.

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The mechanism of action of beta adrenoblockers

The effects of beta-adrenoblockers are implemented by the blockade of β1 and β2-adrenoreceptors. Two types of β-adrenoreceptors (β1 and β2-adrenoreceptors) are isolated, which are distinguished by structural and functional features and distribution in tissues. β1-adrenoreceptors dominated in the structures of the heart, the islet tissue of the pancreas, the YUCSTAGLOMERAILA device of the kidneys, adipocytes.

Preparations, binding to β1-adrenoreceptors of the heart, impede the effects of norepinephrine, adrenaline, reduce the activity of adenylate cyclase. The decrease in the activity of the enzyme leads to a decrease in the synthesis of the CAMF and the inhibition of CA2 + intake into cardiomyocytes. Thus, the main effects of β-adrenoblockers are implemented:

negative inotropic effect (reduced heart abbreviations);
negative chronotropic effect (reduced heart rate);
negative dromotropic effect (conductivity is suppressed);
negative bathemopic effect (automatism decreases).

The antianginal effect of drugs is manifested by a decrease in the forces of heart abbreviations and heart rate, which reduces the need of myocardium in oxygen.

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

Reducing the content of Ca2 + due to the blockade of β1-adrenoreceptors in the cells of the YuCstalomerular apparatus (south) of the kidneys is accompanied by the oppression of the secretion of renin, and, accordingly, decrease in the formation of angiotensin II, which leads to a decrease arterial pressure and determines the effectiveness of β-adrenoblockers as antihypertensive drugs.

Blockade β2-adrenoblocators Promotes improvement:

tone of smooth muscles of bronchi;
contractile activity of a pregnant uterus;
reduction of smooth muscle cells of the gastrointestinal tract (pain in the abdomen, vomiting, nausea, diarrhea, significantly less than constipation).

In addition, the narrowing of the arteriole and Vole causes an increase in the OPS and may worsen the blood supply to the limbs up to the development of Reynos syndrome.

β-adrenoblocators cause changes in lipid and carbohydrate metabolism. They slow down lipolysis, prevent the content of free fatty acids in the blood plasma, while the content of TG is increasing, and the concentration of total hs does not change, the content of HS HDL decreases, the XC LDL increases, which leads to an increase in the atherogenicity coefficient.

β-adrenobloclars cause activation of glycogen synthesis from glucose in the liver and suppress glycogenolysis, which can lead to hypoglycemia, especially against the background of the use of hypoglycemic medicinal preparations in patients diabetes. Due to the blockade of beta-adrnoblocatorial of the pancreas and the braking of physiological secretion of insulin, drugs can cause hyperglycemia, but healthy people They usually do not affect blood glucose concentration.

According to the effects on receptors, beta-adrenobloclochetors are divided into non-selective (affecting β1 and β2-adrenoreceptors) and cardioslelective (affect β1-adrenoreceptors), in addition, some of them have internal sympathomimetic activity (BCA).

Beta-adrenobloclars, which have ACSPRENOLOL, Bopindolol, oxprenolol) to a lesser extent reduce the heart rate and the reduction of myocardium, practically do not affect lipid exchange, they are weaker than the cancellation syndrome.

The vasodilator effect of beta-adrenobloclars is due to one of the following mechanisms or by their combination:

pronounced BCA in relation to β-adrenobloclockers of vessels (for example, pindolol, celiprolol);
a combination of β- and α-adrenoblocking activity (for example, carvedilol);
release from endothelial nitrogen oxide (nebivolol);
direct vasodilation effect.

Cardooselective beta-adrenoblockers in low doses, in contrast to non-selective, affect the tone of the bronchi and arteries, the secretion of insulin, the mobilization of glucose from the liver, the contractile activity of the pregnant uterus, so they can be prescribed with accompanying chronic obstructive diseases of the lungs, diabetes, peripheral circulatory disorders ( For example, with Riby, pregnancy syndrome). They practically do not cause the narrowing of the vessels of skeletal muscles, so when they are used less often, high fatigue and muscle weakness are noted.

Pharmacokinetics beta adrenoblockers

The pharmacokinetic effect of various beta-adrenoblastors is determined by the degree of solubility in fats and water. Three groups of beta adrenoblastors are distinguished:

fat soluble (lipophilic),
water soluble (hydrophilic),
grease and water soluble.

Lipophilic beta-adrenoblockers (metoprolol, alprenolol, oxprenolol, propranolol, thymolol) quickly absorbed into the gastrointestinal tract, easily penetrate the BC (often cause such side effects as insomnia, general weakness, drowsiness, depression, hallucinations, nightmarish dreams). Therefore, one-time doses and multiplicity of admission should be reduced in senior patients with diseases nervous system. Lipophilic beta-adrenoblays can slow down elimination from the blood of other drugs that are metabolized in the liver (for example, lidocaine, hydrolylazine, theophylline). Lipophilic β-adrenoblastors should be appointed at least 2-3 times a day.

Hydrophilic beta-adrenobloclars (atenolol, supolyol, sotalol) is not completely (by 30-70%) are absorbed into the gastrointestinal tract and slightly (0-20%) are metabolized in the liver. Excreted mainly by the kidneys. Have a long half-life (6-24 year). T1 / 2 hydrophilic drugs increases with a decrease in the glass filtration rate (for example, with renal failure, in elderly patients). The multiplicity of application varies from 1 to 4 times a day.

There are beta-adrenoblars, soluble in fats and in water (acebotolol, pindolol, celiprolol, bisoprolol). They have two ways to eliminate - liver (40-60%) and renal. Grease and water-soluble drugs can be prescribed 1 time per day, with the exception of pindolol: it takes 2-3 times. T1 / 2 is 3-12 hours. Most drugs (bisoprolol, pindolol, celiprolol) practically do not interact with drugs that are metabolized in the liver, so they can be prescribed in patients with moderate hepatic or renal failure (With severe violations of liver and kidney functions, the dose of the drug is recommended to be reduced by 1.5 times).

Pharmacokinetics parameters Beta-adrenerboators:

		metabolites
Atenolol
Betaxolol
Bisoprolol
Carvedilol
Metoprolol

Pindolol
Propranolol

Talinolol

Coleiprolol
	250-500 μg / kg

* Note :? - data not detected

Indications for the use of beta adrenoblockers

stress angina,
acute coronary syndrome
AG I. primary prophylaxis stroke and ibs in patients ag
prevention of ventricular and superstricular arrhythmias,
prevention of myocardial re-infarction,
prevention of sudden death in patients with the syndrome of the elongated interval Q-T,
chronic heart failure (Carvedilol, metoprolol, bisoprolol, nebivolol),
systemic diseases with increased influence of the sympathetic nervous system,
thyrotoxicosis
essential Tremor,
alcohol abstinence,
aortic aneurysm,
hypertrophic cardiomyopathy,
digitalization intoxication,
mitral stenosis (Tahisistolic form),
mitral valve prolapse,
tetrad Fallo.

Side effects and contraindications of beta adrenoblockers

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

The side effects of beta-adrenoblockers, contraindications for their use and states that require special caution when using beta adrenobloclars:

Side effects

Absolute contraindications

Conditions requiring special caution

Cardual:

severe sinus bradycardia,
stop sinus knot,
full atrio-ventricular blockade,
reducing the systolic function of the left ventricle.

Neurological:

depression,
insomnia,
nightmarket dreams.

Gastrointestinal:

nausea,
vomiting
flatulence,
constipation
diarrhea.

Bronchostriction (in persons with bronchial asthma, COPD).

Weakness.

Fatigue.

Drowsiness.

Sexy dysfunction.

Increased risk of developing insulin-induced hypoglycemia.

Masking symptoms of hypoglycemia.

Cooking limbs.

Reyno syndrome.

Pronounced hypotension.

Hypertriglyceridemia, decrease in high density lipoprotein levels.

Hepatotoxicity.

Individual hypersensitivity.

Bronchial asthma.

COPL with broncho-construction.

Atri-ventricular blockade I-II Art.

Bradycardia with clinical manifestation.

Sinus node weakness syndrome.

Cardial shock.

Heavy lesions of peripheral arteries.

Hypotension with clinical manifestations.

Diabetes.

COPD without broncho-processing.

Defeat of peripheral arteries.

Depression.

Dyslipidemia.

Asymptomatic sinus node dysfunction.

Atri-ventricular blockade I Art.

For β-adrenoblockers, the abolition syndrome is characterized.

The interaction of drugs

The combination of beta-adrenobloclars with other drugs, shows a negative in-and-chronotropic effect, can lead to severe by-road reactions. With a combination of β-adrenobloclockers with clonidine, a pronounced decrease in blood pressure and bradycardia is developing, especially with the horizontal position of patients.

The combination of the assignment of beta-adrenobloclockers with verapamil, amiodarone, heart glycosides can lead to a sharp bradycardia and violations of AV conduction.

The combination of beta-adrenobloclockers with nitrates or calcium channel blockers is reasonable, since the first reduce the need of myocardium in oxygen, while others, reducing the tone of peripheral and coronary vessels, provide hemodynamic discharge of myocardium and an increase in coronary blood flow.

Preparations of a group of beta-adrenoblockers are of great interest in connection with their striking efficiency. They are used in the ischemic disease of the heart muscle, heart failure and certain impairment of heart performance.

Often the Doctor prescribe them with pathological changes in the rhythm of the heart. Beta-adrenoblocators are called drugs that block various types (β1-, β2-, β3-) of adrenoreceptors for a certain time gap. The value of these substances is difficult to overestimate. They are considered the only one in their kind class of medicines in cardiology, for the development of which was awarded Nobel Prize According to medicine.

Beta-adrenobloclars are isolated. Selective and non-selective. From reference books you can learn that selectivity is the ability to block exclusively β1-adrenoreceptors. It is important to note that it does not affect β2-adrenoreceptors. This article contains basic information about these substances. Here you can familiarize yourself with their detailed classification, as well as drugs and their influence on the body. So are selective and non-selective beta blockers?

The classification of beta blockers is completely simple. As noted earlier, all drugs are divided into two main groups: non-selective and selective beta blockers.

Non-selective blockers

Non-selective beta-adrenoblays - preparations that do not selectively block β-adrenoreceptors. In addition, they have a strong antiagonal, hypotensive, antiarrhythmic and membrane-stabilizing actions.

The group of non-selective blockers includes such drugs:

Propranolol (medicines with a similar active substance:, Inderal, Obizant);
Bopindolol (Sandinorm);
Levobunolol (Vistagen);
Nadolol (Corgard);
Obanol;
Ospprenolol (Coretal, Trazikor);
Pindolol;
Satolol;
Tymimin (Aruthimol).

The anti-naiginal effect of this type of β-adrenoblastors is that they are able to normalize the frequency of heart abbreviations. In addition, the reduction of myocardium is reduced, which gradually leads to a decrease in its need for oxygen portions. Thus, the blood supply to the heart is significantly improved.

Such an effect is due to the slowdown in the sympathetic stimulation of peripheral vessels and the oppression of the activity of the renin-angiotensin system. Moreover, at the same time there is a minimization of general peripheral vascular resistance and a decrease in cardiac output.

Non-selective intederal blocker

But the antiarrhythmic action of these substances is due to the removal of arrhythmogenic factors. Some categories of these drugs have so-called internal sympathomimetic activity. In other words, they have a powerful stimulating effect on beta-adrenoreceptors.

Data drugs do not reduce or slightly reduce the heart rate at rest. In addition, they do not allow the increase in the latter when performing exercise Or under the influence of adrenomimetics.

Cardooselective drugs

The following cardioslelective beta blockers are distinguished:

Ormidol;
Prurry;
Atenol;
Betacard;
Blocium;
Katel;
Catenol;
Hypoten;
MiOgord;
Normed;
PRENORMIN;
Televodine;
Tenolol;
Tensoricor;
Welorin;
Falitonezine.

As is known, there are certain receptors in the structures of the tissues of the human body, which react to adrenaline and norepinephrine hormones. At the moment, α1-, α2-, β1-, β2-adrenoreceptors are distinguished. Not so long ago, β3-adrenoreceptors were described.

Present the location and value of adrenoreceptors as follows:

α1. - are located in the organism vessels (in arteries, veins and capillaries), active stimulation leads to their spasm and a sharp increase in blood pressure;
α2. - the "back negative communication loop" is considered for the system for regulating the health of the body tissue - this suggests that their stimulation can lead to an instant decrease in blood pressure;
β1. - located in the heart muscle, and their stimulation leads to an increase in the frequency of heart abbreviations, and also increases the need of myocardium in oxygen;
β2. - Placed in the kidneys, stimulation provokes the removal of bronchospasm.

Cardooselective β-blockers have an activity against β1-adrenoreceptors. But as for non-selective, they are equally blocking β1 and β2. In the heart, the ratio of the latter is 4: 1.

In other words, stimulation of this body of cardio-vascular system Energy is carried out mainly through β1. With a rapid increase in the dosage of beta blockers, their specificity is gradually reduced to a minimum. Only after that the selective medication blocks both receptors.

It is important to note that any beta-adrenobloclater is selective or non-selective equally lowers blood pressure.

However, at the same time, it is at cardioslelective beta-blockers a lot less side effects. It is for this reason that they are much more expedient to apply with various concomitant ailments.

Thus, they with the minimum probability will provoke the phenomena of bronchospasm. This is explained by the fact that their activity will not affect β2-adrenoreceptors placed in the impressive part of the respiratory organs - the lungs.

It is worth noting that selective adrenoblays are much weaker than non-selective. In addition, they increase the peripheral resistance of the vessels. It is due to this unique property that the drugs are prescribed by patients with cardiologists with serious peripheral circulatory disorders. It is mainly due to patients with a mixed chromota.

Be sure to pay attention to the fact that the medication called Carvedilol does not apply to the category of cardio selective drugs.

Few people know, but infrequently prescribed to lower blood pressure and eliminate arrhythmias. As a rule, it is used for heart failure therapy.

Last generation beta blockers

At the moment there are three basic generations of such medicines. Naturally, it is desirable to use precisely medicines of the last (new) generation. They are recommended to use three times a day.

Preparation Carvedilol 25 mg

In addition, it is not necessary to forget that they are directly connected only with the minimum number of unwanted side effects. Innovative preparations include Carvedilol and Coleiprolol. As mentioned earlier, they are quite successfully used for treatment. various diseases Cardiac muscle.

The non-selective long-term drugs include the following:

Bopindolol;
Supolyol;
Penbutolol;
Satolol.

But to selective drugs of longevity include such:

Atenolol;
Betaxolol;
Empapolol.

When observing the low efficiency of the chosen medication, it is important to revise the prescribed drug.

If necessary, contact your personal doctor so that it picked up a new medicine. The whole thing is that often the means simply do not have the necessary influence on the patient's body.

At the moment, more and more often, preference is given to those drugs that possess precisely prolonged action. They contain the active ingredients that are released gradually, during an impressive period of time, smoothly acting on the health of the patient's cardiologist.

Medicines can be very effective, but one or another patient is simply not susceptible to them. In this case, everything is very individual and depends on certain features of the patient's health.

For this reason, treatment must be carried out with accuracy and special scrupulousness. It is very important to pay attention to all individual characteristics of the human body.

Contraindications for use

It is for the reason that beta-blockers have the ability to influence various organs and systems (not always positive), their use is undesirable and even contraindicated with some concomitant illness of the body.

Various adverse effects and prohibitions for use are directly related to the presence of beta-adrenoreceptors in many organs and structures of the human body.

Contraindications to use drug addictsare:

asthma;
symptomatic decrease in blood pressure;
decrease in heart rate (significant deceleration of the pulse in the patient);
heavy decompensated heart failure.

Do not independently select a medicine from this category of drugs for the heart. It is important to remember that this can cause serious harm to the health of the patient.

Contraindications can relative (when significant benefits for the therapy process exceeds the harm and probability of adoptive effects):

various diseases of the cardiovascular system;
obstructive disease of the respiratory organs of a chronic nature;
in persons with heart failure and slowing down the pulse, use is undesirable, but not prohibited;
diabetes;
transient lameness of the lower extremities.

Video on the topic

What non-selective and selective beta-blockers (drugs from these groups) are used for treatment and heart disease:

For diseases, when receiving beta-adrenobloclars is shown, it should be extremely careful to use them. This is especially true for women who have babe and nursing breasts. Another important point is the sudden cancellation of the selected drug: In no case is not recommended to drastically stop drinking one or another. Otherwise, a person is waiting for an unexpected phenomenon called "Cancellation Syndrome".

Irina Zakharova

Beta -Dereblocators are preparations affecting the sympathetic system of the human body, which regulates the work of the heart and blood vessels. In hypertension, the substances included in the drugs are blocking the effect of adrenaline and norepinephrine on the receptors of the heart and blood vessels. The blockade contributes to the expansion of the vessels and a decrease in heartbeat.

In 1949, scientists found out that the walls blood vessels And heart fabrics contain several varieties of receptors that react to adrenaline and norepinephrine:

Alpha 1, Alpha 2.
Beta 1, beta 2.

The receptors under the influence of adrenaline produce impulses, under the action of which the vessels are narrowing, the increase in the pulse, the increase in pressure and the level of glucose, the expansion of the bronchi. In people with arrhythmia and hypertension, such a reaction increases the likelihood of a hypertensive crisis and a heart attack.

The opening of the receptors, the study of the mechanism of their work served as the basis for the creation of a new class of medicines for the treatment of hypertension:

alpha adrenoblocators;
beta adrenoblockers.

The main role for the treatment of arterial hypertension is played by beta-adrenobloclars, alpha blockers have an auxiliary value.
Alpha adrenoblocators
All drugs of this species are divided into 3 subgroups. At the heart of the classification, the mechanism of influence on receptors: selective - blocking of one type of receptors, non-selective - blocking both types of receptors (alpha 1, alpha 2).
In case of arterial hypertension, you need to block alpha1 receptors. Doctors for this purpose are prescribed alpha 1-adrenoblays:
Doxazozin.
Terasosin.
Prasonin.

These drugs have a small list of side effects, one essential drawback and several advantages:
have a positive effect on the level of cholesterol (general), which is constrained by the development of atherosclerosis;
they are not hazardous to take people suffering from diabetes, with the use of blood sugar remains unchanged;
the blood pressure is reduced, while the pulse rate increases slightly;
male potency does not suffer.

Disadvantage
Under the influence of the alpha blocker, there is an expansion of all types of blood vessels (large, small), so the pressure is reduced stronger when a person is in a vertical position (standing). When using an alpha-blocker, a person is disturbed by a natural mechanism for the normalization of blood pressure when lifting from a horizontal position.
In person it is possible to faint with a sharp adoption vertical position. When he gets up with a sharp reduction in pressure, the nutrition of the brain of oxygen deteriorates. A person feels a sharp weakness, dizziness, darkening in the eye. In some cases, fainting is inevitable. It is only dangerous by injuries when falling, since after making a horizontal position, consciousness is returned, the pressure is normalized. Such a reaction happens at the beginning of treatment, when the patient takes the first tablet.

Mechanism of action and contraindications
After receiving a tablet (droplets, injections), the following reactions occur in the human body:
the load on the heart is reduced due to the expansion of small veins;
reduced level of blood pressure;
blood circulates better;
reduced cholesterol levels;
normalized pulmonary pressure;
coming to normal level of sugar.

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

Side effects
During therapy with alpha-blockers, side effects are possible. The patient can be quickly tired, it can be disturbed by dizziness, drowsiness, fast fatigue. In addition, some patients after taking tablets:
rapid nervousness;
violates the work of the gastrointestinal tract;
allergic reactions occur.

You must talk with a doctor if the symptoms described above appeared.
Doxazozin
Active substance - Doxazozin Mesylate. Additional magnesium, MCC, sodium lauryl sulfate, starch, milk sugar. Release form - tablets. Packing is two types: cells from 1 to 5 in a bundle, bank. Cell packaging may contain 10 or 25 tablets. Number of tablets in the bank:

After one-time reception, the effect is observed after 2, a maximum after 6 hours. The action lasts for 24 hours. Food taken simultaneously with doxazosin slows the effect of the drug. For long use Possible hypertrophy of the left ventricle. Give the drug kidney and intestines.
Terasosin
Active substance The hydrochloride of Terazozin, tablets produce two species - 2 and 5 mg. One pack contains 20 tablets, packed in 2 contour packaging of cellular type. The drug is well absorbed (absorption of 90%). The effect occurs within an hour.

Most of the substance (60%) is excreted through the gastrointestinal tract, 40% by kidney. Therazozin is prescribed orally orally, begin with 1 mg with a hypertensive problem, the dose is smoothly increased to 10-20 mg. Recommend the entire dose to take before bedtime.
Prazonin
Active substance - Prasonin. One tablet may include 0.5 or 1 mg of prazonin. Prescribe medicine high pressure. The active substance contributes to the extension of the vessels:
arteries;
venous vessels.

The maximum effect in one-time reception should be expected from 1 to 4 hours, lasts 10 hours. A person may have addiction to the medicine, if necessary, increase the dose.
Beta blockers
Beta-adrenoblays with hypertension provide real help. They are included in the treatment regimens. With absence allergic reactions And the contraindications of the medicine fits most people. Receiving tablets-blockers reduces the accompanying hypertension symptoms, serves as good prevention.

The substances that are part of the composition block the negative effect on the heart muscle:
reduce pressure;
improve the general condition.

By preferring such medicines, you can not be afraid of hypertensive crises and stroke.
Views
The list of drugs from hypertension is wide. It includes drugs selective and non-selective. Selectivity is a selective influence only on one type of receptors (beta 1 or beta 2). Non-selective means affect both types of beta receptors simultaneously.

When taking beta blockers in patients, the following manifestations are observed:
frequency of heart rate;
the pressure is noticeably reduced;
the tone of blood vessels becomes better;
slows down the formation of blood clots;
the body fabric is better supplied with oxygen.

In practice, beta-adrenobloclars are widely used to treat patients with arterial hypertension. Blockers cardiacs can be assigned and non-magazine selective.
List of cardiolective beta blockers
Consider a description of several most popular drugs. They can be purchased without a recipe in the pharmacy, but self-medication can lead to serious consequences. Reception of beta-blockers is possible only after the consultation of the doctor.

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

Atenolol
Preparation of prolonged action. At the initial stage, the rate of reception per day is 50 mg, after some time it can be increased, the maximum daily dose of 200 mg. An hour after receiving the drug, the patient begins to feel the therapeutic effect.
Therapeutic effect lasts during the day (24 hours). After two weeks, you need to visit the doctor to assess the effectiveness of treatment with the drug. Pressure by the end of this period should normalize. Atenolol is produced in the form of 100 mg tablets, packed in banks for 30 pieces or in cellular packs of 10 pcs.

Metoprolol
When taking the metoprolol, a rapid pressure drop occurs, the effect occurs after 15 minutes. The duration of the therapeutic effect is small - 6 hours. The doctor assigns multiplicity of receptions from 1 to 2 times a day at 50-100 mg per reception. For a day, you can use no more than 400 mg of metoprolol.
Produce a tool in the form of 100 mg tablets. In addition to the active substance metoprolol, they include a subsidiary substance:
lactose monohydrate;
cellulose;
magnesium stearate;
povidone;
potato starch.

The substance is derived from the body through the kidneys. In addition to hypertension, the metropolol is effective as a prophylactic drug during angina, myocardial infarction, migraine.

Acebutolol.
Daily dose of acebutolol 400 mg. Take it 2 times. In the course of treatment, the doctor may increase the rate of reception per day to 1200 mg. Gallest therapeutic effect Feel the patients who, along with increased pressure Diagnosed ventricular arrhythmia.
The medicine is released in two types:
0.5% injection solution in 5 ml ampoules;
tablets weighing 200 or 400 mg.

From the body, the AceboTolol is excreted through the kidneys and gastrointestinal tract after 12 hours after the reception. The active substance may be contained in breast milk. It must be taken into account in lactating women.
Nebivol
You can estimate the result of the action of the drug 2 weeks after the start of reception. In addition to reducing pressure, the medicine has an antiarrhythmic effect. By the end of the fourth week of reception, the patient should establish pressure, by the end of 2 months of the course reception it should become stable.

Produce nebivolt in the form of tablets packed in carton boxes. The active ingredient hydrochloride of nonbivolol. Its removal from the body depends on human metabolism, the higher the metabolism, the one is displayed faster. The elimination occurs through the gastrointestinal tract.
The daily rate of an adult is from 2 to 5 mg per day. After adapting the patient for the drug, the daily dose can be increased to 100 mg. The greatest effect is achieved by taking a medicine at the same time.
Drugs are necardiodelective
The following beta adrenoblasts are included in the group of non-Archemic drugs:
Pindolol.
Timolol.
Propranolol.

Pindolol is prescribed according to the scheme: 5 mg 3-4 times a day. It is possible to increase the one-time dose to 10 mg at a 3-fold reception within the day. This drug in moderate doses is prescribed patients with diagnosis of diabetes mellitus.

Timolol in the treatment of hypertension is prescribed with a two-time reception at a dose of 10 mg. If a need for health arises, the daily dose is adjusted to 40 mg.
Cancel reception of beta-blockers needed under the control of the doctor. The patient can dramatically rise the pressure. Patient with refusal to receive a gradual decrease daily dose within a month.

From this article you will learn: what are adrenoblays, which groups they are divided into. The mechanism of their action, indications, a list of drugs-adrenoblastors.

Publication date Articles: 06/08/2017

Date of renewal of the article: 05/29/2019

Adrenolithics (adrenoblockers) are a group of drugs blocking nerve impulses that react to norepinephrine and adrenaline. Drug Effect They are opposite to the action of adrenaline and norepinephrine on the body. The name of this pharmaceutical group speaks of itself - drugs included in it, "interrupt" the effect of adrenoreceptors located in the heart and walls of blood vessels.

Such drugs are widely used in cardiological and therapeutic practice for the treatment of diseases of the vessels and hearts. Often, cardiologists prescribe their elderly people who are diagnosed with arterial hypertension, heart rhythm disorders and other cardiovascular pathologies.

Classification of adrenoblocrators

In the walls of the vessels there are 4 types of receptors: beta-1, beta-2, alpha-1, alpha-2-adrenoreceptors. The most common are alpha and beta-adrenoblays, "switching" corresponding adrenaline receptors. There are also alpha-beta-blockers that are simultaneously blocking all receptors.

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

Subgroups of adreenolithics:

General mechanism of action of adrenoblockers

When norepinephrine or adrenaline is thrown into the blood flow, adrenoreceptors react instantly, contacting him. As a result of this process, the following effects occur in the body:

vessels are narrowed;
pulse is expected;
blood pressure increases;
the level of glucose in the blood increases;
bronchi expands.

If there are certain diseases, for example, arrhythmias or hypertension, then such effects are undesirable, for they can provoke or relapse of the disease. Adrenoblays "turn off" these receptors, so they act directly opposite:

expand the vessels;
cordial frequency regenerate;
prevent blood sugar increases;
narrow lumen bronchi;
lower hell.

These are common actions characteristic of all types of means from the adreenolithic group. But drugs are divided into subgroups depending on the impact on certain receptors. Their actions are a bit different.

General side effects

For all adrenoblastors (alpha, beta) are:

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

Since drugs from different subgroups have some different therapeutic actions, then unwanted consequences of their reception are also varying.

Common contraindications for selective and non-selective beta blockers:

bradycardia;
syndrome of a weak sinus node;
acute heart failure;
atrioventricular and synoyatrial blockade;
hypotension;
decompensated heart failure;
allergy to drug components.

Non-selective blockers can not be taken when bronchial asthma and obliterating diseases of vessels, selective - with pathology of peripheral blood circulation.

Click on photo to enlarge

Such medicines must prescribe a cardiologist or therapist. An independent uncontrolled reception can lead to serious consequences up to death due to stopping heart, cardiogenic or anaphylactic shock.

Alpha adrenoblocators

Act

Alpha-1 adrenoblastors receptors expand the vessels in the body: peripherals - noticeably painting skin Pokrov and mucous membranes; internal organs - in particular intestines with kidneys. Due to this, peripheral blood flow increases, the microcirculation of tissues is improved. The resistance of the vessels along the periphery decreases, and the pressure decreases, and without reflex highlights.

By reducing the return of venous blood in the atrium and expansion of the "periphery", the load on the heart is significantly reduced. Because of the relief of his work, the degree characteristic of hypertensive and people of old age with heart problems is reduced.

Other effects:

Affect fat exchange. Alfa-AB reduce the level of triglycerides, "bad" cholesterol and increase high density lipoproteins. Such an additional effect is good for people suffering from hypertension, burdened with atherosclerosis.
Affect the exchange of carbohydrates. When taking drugs, the susceptibility of cells with insulin increases. Because of this glucose is absorbed faster and more efficient, it means that its level does not rise in blood. Such an action is important for diabetics, in which alpha-adrenoblockers reduce the level of sugar in the bloodstream.
Reduce the severity of signs of inflammation in organs gOOD SYSTEM. These funds are successfully used with prostate hyperplasia to eliminate some characteristic symptoms: Partial emptying of the bladder, burning in urethra, frequent and night urination.

Alpha-2 blockers adrenaline receptors have the opposite effect: the vessels narrow, increase hell. Therefore, in cardiological practice is not used. But they successfully treat impotence in men.

List of drugs

The table contains a list of international unpatient names Drugs from the group of alpha receptor blockers.

Indications for use

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

Indications for the appointment of alpha-1-adrenoblockers	Indications for alpha-1, -2-blockers
Arterial hypertension	Nutrition B. soft tissues Limbs - ulceration due to layers, frostbite, during thrombophlebitis, expressed atherosclerosis
Chronic heart failure with myocardial hypertrophy	Diseases accompanied by peripheral blood flow disorders - Diabetic microangiopathy, endarterite, Renault disease, Akricyanosis
Prostate hyperplasia	Migraine
	Saving consequences of stroke
	Street dementia
	Failure of the vestibular apparatus due to problems with vessels
	Dystrophy cornea eye
	Elimination of the manifestations of the neurogenic bladder
	Prostatitis
	Neuropathy of optic nerve

Indication for alpha-2-blockers One - erectile dysfunction in men.

Side Effects of Alpha Adrenolithics

In addition to the general side effects listed above in the article, these drugs possess the following side effects:

Side Effects of Alpha-1-Blockers	Unwanted effects when receiving alpha-2 receptor blockers	Side effects from alpha-1, -2-adrenoblockers
Eveny	Increased hell	Loss of appetite
Strong decline of hell	The emergence of anxiety, irritability, increased excitability, motor activity	Insomnia
Arrhythmia, tachycardia	Tremor (trembling in the body)	Sweating
The appearance of shortness of breath	Reducing the frequency of urination and volume of waste	Cooling limbs
Rubble		Heat in tele
Dry oral mucosa		Increased acidity (pH) of gastric juice
Chest pain
Reduced sexual attraction
Urinary incontinence
Painful erections

Contraindications

Pregnancy.
Lactation period.
Allergies or intolerance of active acting or auxiliary substances.
Heavy disorders (diseases) of the liver, kidneys.
Arterial hypotension - reduced pressure.
Bradycardia.
Heavy heart defects, including aortic stenosis.

Beta adrenoblocators

Cardooselective beta-1-adrenoblastors: action principle

Drugs from this subgroup are used to treat heart disease, since they are mainly a positive effect on this authority.

Received effects:

Antiarrhythmic effect by reducing the activity of the rhythm driver - sinus node.
Defend of heart abbreviations.
Reducing the excitability of myocardium under psycho-emotional and / or exercise.
Antihypoxic effect due to reduced oxygen needs with cardiac muscle.
Lower hell.
Preventing the expansion of the focus of necrosis with a heart attack.

A group of selective preparations of beta-adrenobloclars reduce the frequency and facilitate the attack of angina. Also improve the portability of physical and mental loads on the heart in patients with heart failure, which are prolonged by life. These funds significantly improve the quality of life to patients who have suffered a stroke or myocardial infarction suffering ischemic disease Hearts, angina, hypertension.

Diabeticov warns the level of sugar in the blood, reduce the risk of bronchial spasms in people with bronchial asthma.