Beta-adrenoblocators They are called drugs that reversible (temporarily) blocked different kinds (β 1 -, β 2 -, β 3 -) of adrenoreceptors.

The value of beta adrenoblockers It is difficult to overestimate. They are the only class of drugs in Cardiology, for the development of which is presented. Awarding the Prize in 1988, the Nobel Committee called the clinical significance of beta-adrenobloclars " the greatest breakthrough in the fight against heart disease after the opening of Digitalisa 200 years ago».

DiGitalis preparations (plants of fluttering, lat. Digitalis) call a group cardiac glycosides (digoxin, Stroofantin et al.), which are used to treat chronic heart failure from about 1785.

Brief classification of beta adrenoblockers

All beta-adrenoblocators are divided into non-selective and selective.

Selectivity (cardooselectivity) - The ability to block only beta1-adrenoreceptors and not affect beta2 receptors, since the useful effect of beta-adrenoblockers is due to the mainly blockade of beta1 receptors, and the main side effects are beta2 receptors.

In other words, selectivity is selectivity, selectivity of the action (from the English. selective - selective). However, this cardooselectivity is only relative - in large doses, even selective beta-adrenoblastors can partially block both beta2-adrenoreceptors. Please note that cardiolective preparations are stronger reduce diastolic (lower) pressurethan non-selective.

Still some beta adrenobloclars have the so-called Vs. (internal sympathomimetic activity). Less often call it SSA (own sympathomimetic activity). BCA is the ability of beta adrenoblor partially stimulate The beta-adrenoreceptors suppressed by them, which reduces the side effects ("softens" the effect of the drug).

For example, beta adrenoblockers from the BCA to a lesser extent reduce heart rateAnd if the heart rate is source low, then sometimes they can increase it.

Beta adrenoblays with mixed action:

• Carvedilol - Mixed α 1 -, β 1 -, β 2 -adrenoblocator without BCA.
• Labetalol - α-, β 1 -, β 2 -adrenoblocator and partial agonist (stimulator) β 2 receptors.

Useful effects of beta adrenoblockers

To understand what we can achieve from the use of beta-adrenerboators, we must understand the effects that occur at.

Cardiac Regulation Scheme.

Adrenoreceptors and Catecholamins acting on them [ ], as well as adrenal devices that allocate adrenaline and norepinephrine directly into the bloodstream, are combined into sympatoadrenal system (CAC). Activation of the sympathoadrenal system occurs:

• w. healthy people with stress,
• in patients with a number of diseases:
  • myocardial infarction,
  • acute and chronic heart failure (the heart does not cope to pump blood. At CXN, shortness of breath arise (in 98% of patients), fatigue (93%), heartbeat (80%), swelling, cough),
  • arterial hypertension and etc.

Beta1 adrenoblastors limit the effects of adrenaline and norepinephrine in the body, thereby leading to 4 Effects:

1. reduction of heart cutness
2. reducing heart rate (heart rate),
3. decrease in conductivity in the conductive heart system,
4. reducing the risk of arrhythmias.

Now more for each item.

Reducing heart rate

The decrease in heart rate leads to the fact that the heart pushes the blood in the aorta with a smaller force and creates a smaller level of systolic (upper) pressure. Reducing the reduction of abbreviations reduces the work of the heart And, accordingly, the need of myocardium in oxygen.

Reduced heart rate

The decrease in the heart rate allows the heart more rest. This is perhaps the most important thing about which I wrote before. During the abbreviation (systole), the muscle tissue of the heart is not heavily, as the coronary vessels in the thickness of myocardium are shifted. Blood supply myocardium Perhaps only during his relaxation (diastole). The higher the heart rate, the smaller the overall duration of the heart relaxation periods. The heart does not have time to relax fully and may experience ischemia (lack of oxygen).

So, beta-adrenoblays reduce the power of heart abbreviations and the need of myocardium in oxygen, and also lengthen the period of rest and blood supply to the heart muscle. That is why beta blockers are pronounced anti -cehetic action and often used for treating anginawhich is one of the forms of IBS (ischemic heart disease). Old name angina - angina pectorisLatin angina Pectoris., therefore, the opponentical action is also called antianginal. Now you will know what is the antichangal effect of beta-adrenobloclars.

Please note that among all Cardiology Classes beta adrenoblocators without It is better to reduce the heart rate ( frequency of heart abbreviations). For this reason, heartbeat and tachycardia (CSS above 90 per minute) First of all, they are prescribed.

Since beta blockers reduce the work of the heart and blood pressure, they contraindicated In situations where the heart does not cope with its work:

• heavy arterial hypotension (Hell is less than 90-100 mm Hg. Art.),
• acute heart failure (Cardiogenic shock, pulmonary edema, etc.),
• Hsn ( chronic heart failure) In the Stage decompensation.

It is curious that beta blockers must be used (in parallel with three other classes of lek. Drugs - aPF inhibitors, heart glycosides, diuretic) in treatment initial stages chronic heart failure. Beta blockers protect the heart from excessive activation of the sympathetic system and increase the life expectancy patients. I'll tell you more about modern principles The treatment of HSN in the topic about heart glycosides.

Conduct reduction

Conduct reduction ( reducing the velocity of electrical impulses by ) as one of the effects of beta blockers also has great importance. Under some conditions, beta blockers may disrupt preservative conductivity (slow down impulses from atria to ventricles in AV-node) what causes an atrioventricular blockade (AV blockade) various degrees (from i to III).

AV-block diagnosis Various degrees of gravity is put on ECG and manifests itself in one or more signs:

1. constant or cyclic interval lengthening P-Q View More 0.21 s,
2. losing individual ventricular cuts,
3. reduced heart rate (usually from 30 to 60).

Stably increased duration interval P-Q from 0.21 s and above.

a) periods of gradual elongation of the P-Q interval with the fallout of the QRS complex;
b) loss of separate QRS complexes without gradually elongation of the P-Q interval.

At least half of the ventricular QRS complexes falls.

The impulses from the atria to the ventricles are not conducted at all.

From here council: If the patient has a pulse less often 45 blows per minute or an unusual uneven rhythm appeared, it is most likely to adjust the dose of the drug.

In what cases are elevated risk of conducting conductivity disorders?

1. If the beta adrenoblocator is prescribed to the patient with bradycardia (Heart rate below 60 per minute)
2. if it is originally available violation of atrioventricular conduction (increased the time of the electric. pulses in AV node more than 0.21 C),
3. if the patient is individually high sensitivity to beta blockers
4. if a exceeded (incorrectly selected) dose of beta adrenoblocker.

To prevent conduction disorders, you need to start with small doses of beta blocker And raise the dosage gradually. If the side effects occur, the beta-adrenobloclater cannot be canceled sharply due to the risk of tachycardia (heartbeat). Need to reduce the dosage and cancel the drug gradually, within a few days.

Beta adrenoblastors are contraindicated if the patient has hazardous deviations on the ECG, for example:

• violations of conductivity (Atrioventricular blockade II or III degree, synoatrial blockade, etc.),
• too rare rhythm (CSS less than 50 per minute, i.e. sharp bradycardia),
• sinus node weakness syndrome (SCC).

Reducing the risk of arrhythmia

Reception of beta adrenoblockers leads to reducing the excitability of myocardium. In the heart muscle, there are fewer excitation foci, each of which is capable of leading to cardiac arrhythmia. For this reason, beta blockers are effective in treating, as well as for prevention and treatment and stomacle Rhythm disorders. Clinical studies have shown that beta blockers significantly reduce the risk of fatal (deadly) arrhythmias (for example, ventricular fibrillation) and therefore are actively used for prevention sudden death , Including with the pathological elongation of the Q-T interval on the ECG.

Any myocardial infarction due to pain and necrosis (dieting) of the heart muscle site is accompanied by pronounced activation of the sympathetic system. The purpose of beta-blockers with myocardial infarction (if there is no indicated above contraindications) significantly reduces the risk of sudden death.

Indications for the use of beta blockers:

• IBS (angina, myocardial infarction, chronic heart failure),
• prevention of arrhythmias and sudden death,
• arterial hypertension (treatment of increased blood pressure),
• other diseases with an increase in the activity of catecholamines [ adrenaline, Noradrenalin, Dopamine] in organism:
  1. tyredoxicosis (hyperfunction thyroid gland),
  2. alcohol abstinence (), etc.

Side Effects of Beta Adrenoblockers

Part of side effects due to excessive action of beta adrenoblockers on the cardiovascular system:

• sharp bradycardia (Heart rate below 45 per minute),
• atrioventricular blocada,
• arterial hypotension (systolic blood pressure below 90-100 mm Hg. Art.) - more often with intravenous introduction of beta-adrenobloclars,
• strengthening heart failure up to the edema of the lungs and stop the heart,
• worsening blood circulation in the legs With a decrease in cardiac emissions - more often in older people with atherosclerosis of peripheral vessels or endarterity.

If the patient has feochromocytoma (a benign tumor of the brain layer of the adrenal glands or nodes of the sympathetic vegetative nervous system that emitting catecholamines; occurs in 1 for 10 thousand people and up to 1% of patients with hypertension), T. beta blockers may even increase blood pressure Due to the stimulation of α 1 -adrenororeceptors and spasm arterioles. To normalize hell, beta blockers need to be combined with.

In 85-90% of cases of pheochromocytoma is a tumor of adrenal glands.

Beta blockers by themselves show antiarrhythmic effectbut in combination with other anti-anhythmic drugs possible provocation attacks of ventricular tachycardia or ventricular bigemia (constant alternate change of normal reduction and ventricular extrasystole, from lat. bI - two).

Bigemia.

The rest of the side effects of beta blockers are easy-smart.

The narrowing of bronchi and bronchospasm

Beta2-adrenoreceptors expand bronchi. Accordingly, beta-blockers acting on beta2-adrenoreceptors are narrowing the bronchi and can provoke bronchospasm. This is especially dangerous to patients with bronchial asthma , smokers and other people with lung diseases. They have cough and shortness of breath increases. To prevent this bronchospasm, you need to take into account the risk factors and be sure to apply only cardio selective beta blockerswhich in ordinary doses do not act on beta2-adrenoreceptors.

Reducing sugar levels and lipid profile deterioration

Since the stimulation of beta2-adrenoreceptor causes the splitting of glycogen and the growth of glucose levels, the beta blockers can reduce the level of sugar in blood with development moderate hypoglycemia. People with normal carbohydrate exchange There is nothing to fear, and patients with, should be careful. Moreover, beta blockers mask such symptoms of hypoglycemia like tremor (jitter) I. heartbeat (tachycardia), due to excessive activation of the sympathetic nervous system due to the emission of contrincing hormones during hypoglycemia. note that sweet glands They are controlled by the sympathetic nervous system, but they are m-cholinoreceptors that are not blocked by adrenoblockers. Therefore, hypoglycemia during the reception of beta blockers is characterized especially strong sweating.

Patients S. diabetesInsuline, it is necessary to inform about the increased risk of development when using beta adrenoblockers. For such patients are preferred selective beta blockersnot acting on beta2-adrenoreceptors. Patients with diabetes mellitus in an unstable condition ( poorly predictable blood glucose levels) Beta blockers are not recommended, in other cases, please.

Sexual violations

Perhaps development impotence (Modern name - erectile dysfunction), for example, when taking propranolola For 1 year it develops in 14% of cases. Also noted development fibrous plaques In the body of the penis with its deformation and the difficulty of erection when taking propranolola and metoprolol. Sexual violations are more often in persons with (that is, problems with potency when taking beta blockers usually arise from those who are possible without drugs).

Fear impotence and for this reason do not take medicine when arterial hypertension - error decision. Scientists find out that long increased blood pressure leads to erectile dysfunction Regardless of the availability of accompanying atherosclerosis. With high hell walls of vessels thicken, become denser and can not supply internal organs the right amount of blood.

Other side effects of beta adrenoblockers

Other side effects When taking beta blockers:

• from side gastrointestinal tract (in 5-15% of cases): constipation, less often diarrhea and nausea.
• from side nervous system: Depression, sleep disorders.
• from side skin and mucous membranes: rash, urticaria, eye redness, reducing the secretion of tear fluid (relevant for useful contact lenses) and etc.
• when receiving propranolola Occasionally happens laryingospasm (Difficult noisy, whistling inhale) as a manifestation of an allergic reaction. Laringostasm arises as a reaction to an artificial yellow dye tartrazine In a tablet approximately after 45 minutes After taking the drug inside.

Cancellation syndrome

If you take beta-blockers for a long time (several months or even weeks), and then suddenly stop receiving, arises cancellation syndrome. In the coming days after the cancellation occurs heartbeat, anxiety, angina attacks, ECG worsens, maybe the development of myocardial infarction and even a sudden death.

Development of cancellation syndrome is due to the fact that during the reception of beta-blockers the body adapts to the reduced influence (NOR) of adrenaline and increases the number of adrenoreceptors in organs and tissues. In addition, since propranolol slows down the transformation of the hormone of the thyroid gland tyroxina (T 4) in hormone triiodthththinine (T 3), then some signs of cancellation syndrome (anxiety, trembling, heartbeat), especially expressed after the abolition of propranolol, can be caused by excess thyroid hormones.

For the prevention of cancellation syndrome recommended gradual cancellation of the drug for 14 days. If necessary, surgical manipulations on the heart exist other diagrams of the discharge of the drug, but in any case the patient must know your medicine: What, in which dosage, how many times a day and how long he takes. Or at least write them on the leaf of paper and wear with you.

Features of the most significant beta blockers

Propranolol (Anaprilin) - non-selective beta blocker without BCA. it the most famous drug from beta blockers. Act briefly - 6-8 hours. Characterized by the abolition syndrome. Fat solvent, so penetrates the brain and possesses soothing action. Non-selective, therefore, has a large number of due beta2-blockade of side effects ( sensing bronchi and enhances cough, hypoglycemia, cooling limbs).

It is recommended for receiving under stress situations (for example, before the exam, see). Since there is sometimes increased individual sensitivity to beta-blocator with a rapid and significant decrease in blood pressure, its first purpose is recommended to be conducted under the control of the doctor with a very low dose (for example, 5-10 mg anaprilin). To increase blood pressure should be introduced atropine (and not glucocorticoid hormones). For permanent reception propranolol It is not suitable, in this case another beta blocker is recommended - bisoprolol (below).

Atenolol is a cardioslelective beta blocker without BCA. Previously was a popular drug (as well as metoprolol). Applied 1-2 times a day. Water soluble, so does not penetrate the brain. Honor cancellation syndrome.

Metoprolol - cardioslelective beta blocker without BCA, similar to atenolol. Accepted 2 times a day. Atenolol and metoprolol have now lost their importance due to the distribution bisoprolol.

Betaxolol (Locase) - Cardooselective beta blocker without BCA. Mainly used for treatment arterial hypertension. Accepted 1 time per day.

Bisoprolol (Concorp) - Cardooselective beta blocker without BCA. Perhaps the most important drug today from beta blockers. Convenient form of reception (1 time per day) and reliable smooth 24-hour antihypertensive effect. Reduces blood pressure by 15-20%. Does not affect the level of thyroid hormones and blood glucose, so allowed in diabetes mellitus. Bisoprolol is weaker than the cancellation syndrome. There are many on the market bisoprolol Different manufacturers, so you can choose inexpensive. In Belarus, the cheapest generic today - Bisoprolol-Lugal (Ukraine).

ESMOLOL - is available only in solution for intravenous administration as antiarrhythmic drug. Duration of 20-30 minutes.

Nebivolol (root) - Cardooselective beta blocker without BCA. Also an excellent drug. Causes a smooth decrease in blood pressure. Expressed antihypertensive effect It comes after 1-2 weeks of reception, the maximum - after 4 weeks. Nebivolt enhances production azota oxide (NO) in the endothelium of blood vessels. The most important function of nitrogen oxide - expansion of vessels. In 1998 was awarded Nobel Medicine Prize with wording " For the opening of the role of nitrogen oxide as a signal molecule in regulation of cardio-vascular system " Nebivolol has a number additional useful effects:

• vasteransior [Vasodilative] (from Lat. vAS. - vessel dilatatio. - expansion),
• antiagregant (inhibits platelet aggregation and thrombosis),
• angioprotective (Protects the vessels from the development of atherosclerosis).

Carvedilol - α 1 -, β-adrenoblocator without BCA. Thanks to the blockade of α 1 -receptors, has vasodilative action And additionally reduces blood pressure. Less atenolol reduces heart rate. Does not impair the tolerance of physical exertion. Unlike other blockers, reduces blood glucose levels, therefore it is recommended for type 2 diabetes mellitus. Possessed antioxidant properties, slows down atherosclerosis processes. Accepted 1-2 times a day. Especially recommended for treatment of chronic heart failure (CHF).

Labetalol - α-, β-adrenoblocator and partially stimulates β 2-receptors. Well reduces blood pressure with a minor increase in heart rate. It has an antiagonal effect. It is capable of raising blood sugar. In large doses, bronchospasm can cause cardioslelective beta blockers. Used intravenous with hypertensive cries and (less often) inside 2 times a day for the treatment of arterial hypertension.

Medicinal interactions

As I already indicated above, combination of beta blockers with other antiarrhythmic drugs Potentially dangerous. However, this is the problem of all groups of antiarrhythmic drugs.

Among antihypertensive (hypotensive) drugs prohibited Only a combination of beta blockers and calcium channel blockers from the group verapamila and diltiazem. This is associated with an increased risk of cardiac complications, since all these drugs act on the heart, reduce the power of abbreviations, heart rate and conductivity.

Overdose of beta adrenoblockers

Symptoms overdose Beta blockers:

• sharp bradycardia (heart rate below 45 per minute)
• dizziness up to the loss of consciousness,
• arrhythmia,
• akricyanosis ( scorn in fingertips),
• if the beta-blocker is fat soluble and penetrates the brain (for example, propranolol), then a coma and cramps can develop.

Assistance in overdose Beta blockers depends on the symptoms:

• for bradycardia - atropine (parasimpatic effect blocker), β 1 -stimulators ( dobutamine, Isoproterenol, Dopamine),
• for heart failure - cardiac glycosides and diuretic,
• for low hell (hypotension below 100 mm Hg. Art.) - adrenaline, Meston and etc.
• for bronchospaisme - aminoophyllin (efufillin), isoproterenol.

For local application (instillation in the eyes) beta blockers reduce the education and secretion of waterthat reduces intraocular pressure. Local beta blockers ( timolol, Proksodolol, Betaxolol et al.) Used for treating glaucoma (eye disease with gradual due to elevated intraocular pressure ). Perhaps development system side effects, caused by the hit of anti-chloroous beta-blockers on the tears and nose channel and from there in the stomach, followed by suction in the gastrointestinal tract.

Beta blockers are taken into account as possible doping and athletes should be used with serious restrictions.

Supplement about Koraxan

In connection with frequent issues in the comments about the drug Koraxan (Ivabradin) Highlight its similarities and differences with beta blockers. Koraxan blocks i f -Channels of the sinus node and therefore does not apply to beta adrenoblockers.

In this way, koracan Used to gear sinus rhythm with normal (slightly reduced) hell and the absence of arrhythmias. If a Hell elevated or there are cardiac arrhythmias, you need to use beta blockers. A combination of shoquacan with beta blockers is allowed.

More about Coraxan: http://www.rlsnet.ru/tn_index_id_34171.htm

Beta blockers in the treatment of hsn

(update from 19.07.2014)

A group of beta blockers refers to the basic (mandatory) for treatment Xsn (chronic heart failure). According to the results of clinical studies now for the treatment of HSN recommended 4 drugs:

• carvedilol,
• bisoprolol,
• extended form metoprolol Sukcinate,
• people over 70 years old are also allowed nebivol.

These 4 drugs proved in clinical studies Its ability to improve the condition and increase the survival of patients with HSN.

• atenolol,
• metoprolol Tartrate.

The aim of treating beta-blockers with CHSN is a decrease in the heart rate at least 15% of the initial level below 70 ° C. per minute (50-60). It has been established that the decrease in the heart rate for every 5 blows reduces mortality by 18%.

The initial dose of CXN is 1/8 from therapeutic And slowly rises every 2-4 weeks. In case of intolerance and the inefficiency of beta-blockers, they are combined or completely replaced by a blocker I f -Channels of a sinus node - ivabradin (see above Supplement about Koraxan).

Read more about the use of beta blockers in the treatment of HSN, read in national recommendations on the diagnosis and treatment of HSN of the 4th revision, approved in 2012-2013. (PDF, 1 MB, in Russian).

Beta-blockers are an extensive group of drugs, which are used to treat hypertension, heart disease, as a component of thyrotoxicosis therapy, migraine. Preparations are capable of changing the sensitivity of adrenoreceptors - the structural components of all organism cells that react to catecholamines: adrenaline, norepinephrine.

Consider the principle of operation of drugs, their classification, basic representatives, a list of indications, contraindications, possible side effects.

History opening

The first drug group was synthesized in 1962. It was a protonalol, which as it turned out in the experiments on mice, caused cancer, so he did not receive a clinical tolerance. The debut beta blocker, admitted to practical application, became propranolol (1968). For the development of this medication and studying beta receptors, his creator James Black later received the Nobel Prize.

Since the creation of propranolol and to this day, scientists have developed more than 100 representatives of women, about 30 of which began to be used by doctors in everyday practice. This breakthrough was the synthesis of a representative. last generation Nebivolol. He was distinguished from his relatives to relax blood vessels, optimal portability, convenient reception mode.

pharmachologic effect

There are cardiospecific drugs that interact mainly with beta-1 receptors and nonspecific reactions with receptors of any structure. The mechanism of action of cardiolective, non-selective drugs is the same.

Clinical effects of specific drugs:

• reduce the frequency, heart strength. Exception - Acebotolol, Coleiprolol, capable of accelerating the rhythm of the heart;
• reduce myocardial needs in oxygen;
• reduce blood pressure;
• slightly increase the plasma concentration of "good" cholesterol.

Non-specific medicines additionally:

• cause a narrowing of bronchi;
• warn thrombocyte sticking and blood clots;
• increase the tone of the uterus;
• suspend the splitting of adipose tissue;
• lower intraocular pressure.

The reaction of patients to the reception of Bab is unequal depends on many indicators. Factors affecting the sensitivity to beta adrenoblockers:

• age - the sensitivity of the adrenoreceptors of the vascular wall to drugs is reduced in newborns, premature children, people of old age;
• thyrotoxicosis is accompanied by a two-time increase in the number of beta-adrenoreceptors in the heart muscle;
• the exhaustion of the reserves of norepinephrine, adrenaline - the use of some Bab (reserpine) is accompanied by the deficiency of catecholamines, which leads to the hyper-sensitive receptors;
• reducing the sympathetic activity - the reaction of cells on catecholamines is amplified after temporary sympathetic denervation;
• reducing the sensitivity of adrenoreceptors - develops with prolonged use of drugs.

Classification of beta blockers, generation of drugs

There are several approaches to the separation of drugs into groups. The most common method takes into account the ability of medicines to interact mainly with beta-1-adrenoreceptors, which are especially much in the heart. This feature distinguish:

• 1 generation - non-selective medicines (propranolol) - block the operation of receptors of both types. Their use except the expected effect is accompanied by undesirable, primarily the bronchi spasm.
• 2 generation Cardooselective (Atenolol, Bisoprolol, metoprolol) - little affect beta-2-adrenoreceptors. Their action is more specific;
• 3 generation (Carvedilol, Nebivolol) - have the ability to expand the clearance of vessels. There may be cardioslelective (nebivolol), non-selective (carvedilol).

Other classification options take into account:

• the ability to dissolve in fats (lipophilic), water (water-soluble);
• the duration of the action: ultrashort (is used to quickly appear, termination), short (take 2-4 times / day), prolonged (take 1-2 times / day);
• the presence / absence of internal sympathomimetic activity is a special effect of some selective, non-selective beta-adrenobloclars, which can not only block, but also to excite beta-adrenoreceptors. Such drugs do not reduce / reduce the slightly heart rate and can be assigned to patients with bradycardia. These include pindolol, oxprenolol, cardiolol, alprenolol, dilellol, acebutolol.

Different class representatives differ from their relatives pharmacological properties. Even the recent generation medicines are not universal. Therefore, the concept of "best" is purely individual. The optimal drug is selected by a doctor who takes into account the age of the patient, the features of the course of the disease, the history of the disease, the presence of concomitant pathologies.

Beta blockers: appointment testimony

Beta-adrenoblocators are one of the main classes of drugs used in the treatment of arterial hypertension. Popularity is explained by the ability of drugs to normalize heart rate frequency, as well as some other performance of the heart (shock volume, heart index, the total peripheral resistance of the vessels), which other hypotensive means do not apply. Such disorders accompany the flow of hypertension in third patients.

A complete list of readings includes:

• chronic heart failure - prolonged action preparations (metoprolol, bisoprolol, carvedilol);
• unstable angina;
• myocardial infarction;
• violation heart Rhythm;
• thyrotoxicosis;
• migraine Prevention.

I appoint drugs, the doctor must remember the peculiarities of their application:

• the initial dose of medication must be minimal;
• the increase in dosage is very smooth, no more than 1 time / 2 weeks;
• if it is necessary to carry out long-term treatment, the smallest effective dose is used;
• taking women, it is necessary to constantly monitor the heart rate, blood pressure indicators, weight;
• 1-2 weeks after the start of reception, 1-2 weeks after determining the optimal dosage it is necessary to check the biochemical blood biochemical indicators.

Beta-adrenoblocators and diabetes

According to European recommendations, beta-blockers with diabetes mellitus are prescribed as additional drugs, exclusively in small doses. This rule does not apply to two representatives of the group with vasodilatory properties - Nebivolol, Carvedilol.

Pediatric practice

Babs are used to treat children's hypertension, which is accompanied by an accelerated heartbeat. It is allowed to prescribe beta-adrenobloclars with patients with chronic heart failure subject to the following rules:

• before the start of receiving women, children must pass;
• medicines are prescribed only to patients with a stable state of health;
• the initial dosage should not exceed ¼ from the maximum one.

List of drugs with hypertension

In the treatment of hypertension, both selective and non-selective beta-blockers are used. Below is a list of drugs that includes the most popular medicines and their trade names.

To achieve a better effect, hypotensive tools of different groups are often combined with each other. The best combination is considered sharing Bab with. Sharing with medicines of other groups is also possible, but less studied.

List of comprehensive drugs

Most. best medicine To combat high pressure, the selective beta adrenoblor of the third generation of prolonged action is nebivolol. Application of this medicine:

• allows you to achieve a more significant reduction in the indicators of hell;
• it has fewer side effects, does not violate the erection;
• does not increase the level of bad cholesterol, glucose;
• protects cell membranes from the impact of some damaging factors;
• safe for patients with diabetes mellitus, metabolic syndrome;
• improves blood supply to fabrics;
• does not cause bronchospasm;
• convenient reception mode (1 time / day).

Contraindications

The list of contraindications is determined by the type of medication. For most tablets are:

• atrioventricular blockade of 2-3 degrees;
• reduced blood pressure;
• acute vascular failure;
• sinus node weakness syndrome;
• heavy cases of bronchial asthma.

Medications are prescribed with caution:

• sexually active young people who suffer from arterial hypertension;
• athletes;
• with chronic instructive pulmonary disease;
• depression;
• elevated plasma lipid concentration;
• diabetes;
• defeat peripheral arteries.

During pregnancy, beta blockers try not to use. They reduce blood flow to the placenta, the uterus, can cause disorders of the fetus. However, if there is no alternative treatment, the possible benefit for the mother's body exceeds the risk of side effects of the fetus, the use of women maybe.

Side effects

There are cardiac, extraordinary unwanted reactions. The larger selectivity the medicine is possessed, the less extracardional side effects it has.

With a joint admission of beta-adrenobloclars and drugs that depress heart function, cardiac complications are especially bright. Therefore, they are trying not to appoint them together with clonidine, verapamil, amiodar.

Cancellation syndrome drugs

Cancellation syndrome call the body response in response to a sharp cessation of receiving any medication. It is manifested by the exacerbation of all the symptoms that were eliminated by the use of medication. The patient's health will deteriorate quickly, there are no previously symptoms characteristic of the disease. If the medicine has a short duration of action, cancellation syndrome can develop between tablet receptions.

Clinically manifests:

• an increase in the number, frequency of angina attacks;
• acceleration of the heart;
• violation of the rhythm of heart abbreviations;
• an increase in blood pressure;
• myocardial infarction;
• sudden death.

To prevent the development of cancellation syndrome for each drug, algorithms of gradual discontinuation were developed. For example, the removal of propranolol should take 5-9 days. Throughout this period, the dosage of the drug is gradually reduced.

Literature

1. S. Yu. Madsevich. Cancellation syndrome antianginal drugs. Clinical significance and measures of warning, 1999
2. D. Levi. Adrenoreceptors, their stimulants and blockers, 1999
3. I. Zaitseva. Some aspects pharmacological properties Beta Adrenoblocators, 2009
4. A. M. Shilov, M. B. Melnik, A. Sh. Avshalumov. Beta-adrenoblockers III generation in the treatment of cardiovascular diseases, 2010

Last updated: January 24, 2020

Alpha - adrenoblocators belong to the group of substances capable of suppressing nerve impulsescaused by adrenaline and norerange. They help stabilize the sympathetic nervous system, lead the pulse and reduce the pressure. The mechanism of action is based on the oppression of the action of adrenoreceptors, which are in the heart and vessels.

Alpha and expand vessels, improving blood flow. These medicines unload the heart, eliminating the harmful cholesterol. The drug helps it easier to absorb glucose, which helps in combating diabetes. Due to the blockade of receptors, arrhythmia and pain in the heart disappear. Some blockers act on alpha - 2 - adrenoreceptors, it contributes to the treatment of prostate hyperplasia.

Classification

Alpha Adrenoblocators are divided into two groups: selective and non-selective. The first to affect one type of receptors - alpha - 1, the second - on alpha - 1 and alpha - 2.

Selective

Can eliminate the action of arteriole receptors. These funds reduce pressure without such side effects as arrhythmia, sugar jumps. Against the background of drug intake, the body is inactivating the allocation of norepinephrine. This is exactly what prevents the rhythm violation and difficulty breathing. Indications for the use of selective blockers is hypertension against the background of diabetes mellitus, cardiovascular diseases, as well as inflammation of the prostate gland, including prostate adenoma. Selective alpha - 1 - adrenoblockers include doxazozin, prazosin, therazozin.

Non-selective

This type of blockers are used to eliminate symptoms and crises. They also block the adrenoreceptors, but at the same time increase the pulse. They are prescribed with acute circulatory impairment, stroke, atherosclerosis, endarteritis and some types of benign tumors. They are treated and rare diseases - pheochromocyti, Reino disease, abstineent syndrome. Compared to selective blockers, they have a less long action. The most famous drugs of this group are: nicergoline, fantolamine, tropodiffen, Pirroxane, Butyroxane.

Important!

The use of non-selective drugs is possible only in emergency cases. They are not suitable for permanent reception.

Table "List of the best alpha - adrenoblockers"

Among all the adrenoblockers there are the most common, which almost 100% of cases give the result in the treatment. Below is a list of drugs that have similar treatment properties:

Instructions for use

All adrenoblastors have a similar mechanism of action, side effects and contraindications. Many of them are of great popularity, and some are prescribed with caution, due to the unpredictable effect in the treatment.

Features Alfa - Adrenoblockers

The effect of this pharmacological group is aimed at removing the spasm of the vessels and reduce the secretion of renin in the kidneys. After the preparation is taken, an antiagonal effect appears, which is due to a decrease in the frequency and strength of heart cuts. The antidiuretic effect is observed in connection with the relaxation of the muscles of a smooth muscles. In this regard, the resistance of urine outflow is reduced. Thanks to the blocking of alpha - receptors, a persistent hypotensive effect occurs, which lasts about a day.

When the reception of drugs is shown

Indications for the use of alpha - adrenoblockers are the following diseases:

• benign prostate hyperplasia. In this case, Tamsulosin is prescribed, doxazozin, Nethegis. These same drugs are used with prostatitis when squeezing the lumen of the urethra of the prostate gland is observed;
• arterial hypertension. In this case, drugs are prescribed to relieve acute attacks to increase pressure. Since the drugs have a persistent antispasmodic effect, the actions of the drug grabs for a day. This ensures the removal of the load on the vessels and the heart for a long time;
• cardiovascular diseases such as arrhythmia, heart failure, ischemic disease Hearts, extrasystoles. In this case, there is a thorough selection of drugs. The most frequently appointed ones are: Prazozin, Alfuzosin, Ureradil.

It's important to know!

Some symptoms are similar to heart disease, however, are caused by the disorder of the vegetative nervous system.

Contraindications for reception

There are a number of contraindications that cannot be ignored, otherwise unwanted symptoms or lesions of some organs and systems arise:

1. Children's age up to 18 years.
2. Pregnancy and breastfeeding.
3. Predisposition to hypotension.
4. Hemophilia.
5. Individual intolerance to the components.

The remaining contraindications are indicated in the instructions of the drugs. They may include additional items. Before use, read the instructions.

Application for cardiovascular pathologies

Cardiologists prescribe adrenoblays with left ventricle hypertrophy. In this case, they have a reversible action. The use of drugs of this pharmacological group helps the patient to cope with critically high pressure And he saves it from the stroke. The main effect of alpha - blockers is aimed at expanding the ducts of coronary vessels. Improved blood circulation Against the background of taking these drugs is a good prevention of ischemic lesions of the heart and myocardial infarction.

Features of reception in urology

In the tissues of the prostate gland and bladder Alpha - 1 are adrenoreceptors, whose action is depressed when receiving blockers. Such drugs are accepted daily once a day. The initial dose is established by the doctor separately for each patient, depending on the defeat of the organs of the urogenital system. The drug is beginning to take with a minimum dose. Thanks to the vasodilator properties of alpha - adrenoblays help to fight poor urination, reduce pressure in the urinary channel. However, the effect does not occur immediately, but after a couple of weeks after the start of reception. Among the drugs used in urology are prescribed Tamsulosin, doxazosin, alfuzosin.

Features of admission in cardiology

Before using the drug, it is necessary to carry out a test for sensitivity and individual tolerance of funds. The course of treatment is beginning with a low dose, increasing it daily. To avoid sharp deterioration well-being after receiving alpha - adrenoblockers is recommended in horizontal position In one hour. When appointing a new product from this pharmacological group, it is necessary to monitor the level of sugar in the body. In cases of overdose or independent cancellation of the drug may occur side effects, Up to stroke.

Attention!

Never throw away Alpha - adrenobloclars without consulting a doctor. It can provoke acute circulatory disorders and hypertensive crises.

Side Effects and Overdose

Like all medicines, adrenoreceptor blockers sometimes cause unwanted effects, such as:

• dizziness;
• sharp decline in pressure;
• collapse;
• headache;
• nausea or vomiting;
• rapid pulse;
• lack of air;
• allergic reactions;
• student urination.

Side effects Not always manifest. Often they arise against the background of improper reception or overdose of medicine. Any response to the drug should not be ignored. Refer to the doctor, finding one or another symptom, worsening your well-being.

Since this pharmacological group Includes many different drugs, the symptoms of overdose are different. Often, intoxication occurs, which manifests the headache, vomiting, trembling limbs, inhibition of breathing, strong decrease in pressure. Treatment includes washing the stomach, the reception of sorbents and antagonists. Do not hesitate and call emergency help To restore health status.

conclusions

You can make several alpha approvals - adrenoblocators:

• all these funds are allowed to receive only after the doctor's appointment;
• alpha - adrenoblocators improve blood flow throughout the body, providing blood flow to the heart muscle and organs of the urogenital system.
• preparations show the effect after two weeks of continuous reception;
• it is impossible to cancel the drug independently, due to the occurrence of the opposite effect;
• before applying any means, it is necessary to familiarize yourself with contraindications and side effects.

Catecholamines are important in the regulation of the functions of the organism: adrenaline and norepinephrine. They stand out in blood and act on special sensitive nerve endings - adrenoreceptors. The latter are divided into two large groups: alpha and beta-adrenoreceptors. Beta-adrenoreceptors are located in many organs and tissues and are divided into two subgroups.

When the β1-adrenoreceptors are activated, the frequency and power of heart abbreviations increase, expand coronary arteryThe conductivity and automaticism of the heart improves, the decay of glycogen in the liver and energy formation increases.

When the β2-adrenoreceptors are excited by the walls of the vessels, the muscles of the bronchi, the tone of the uterus is reduced during pregnancy, insulin and disintegration of fat increases. Thus, the stimulation of beta-adrenoreceptors using catecholamines leads to the mobilization of all the body for active livelihoods.

Beta adrenoblays (Bab) - group medicinal substancesbinding beta-adrenoreceptors and impede the action of catecholamines on them. These drugs are widely used in cardiology.

Babs reduce the frequency and strength of heart abbreviations, reduce blood pressure. As a result, oxygen consumption with cardiac muscle decreases.

Diastola is lengthened - the rest period, relaxation of the heart muscle, during which there is a filling of coronary blood vessels. Improving the coronary perfusion (myocardial blood supply) contributes to the decrease in intracardiac diastolic pressure.

The redistribution of blood flow occurs from normal blood ducts to the ushised, as a result, the portability of physical exertion is improved.

Bab has an antiarrhythmic action. They suppress the cardiotoxic and arrhythmogenic effect of catecholamines, and also prevent the accumulation of calcium ions in the heart cells, worsening energy exchange in myocardium.

Classification

Bab is an extensive group of medicines. They can be classified for many signs.
Cardooselectivity - the ability of the drug to block only β1-adrenoreceptors, without affecting β2-adrenoreceptors, which are in the wall of the bronchi, vessels, uterus. The higher the selectivity of Bab, the safer to apply it in concomitant diseases respiratory tract and peripheral vessels, as well as diabetes mellitus. However, selectivity is the concept of relative. When prescribing a drug in large doses, selectivity decreases.

Some women inherent internal sympathomimetic activity: the ability to some degree to stimulate beta-adrenoreceptors. Compared to ordinary women, such drugs slow down the heart rhythm and the strength of its abbreviations, less often lead to the development of cancellation syndrome, less adversely affect lipid exchange.

Some women are able to additionally expand the vessels, that is, there are vazodilative properties. This mechanism is implemented using pronounced internal sympathomimetic activity, alpha-adrenoreceptor blockades or direct action on vascular walls.

The duration of action most often depends on the peculiarities of the chemical structure of Bab. Lipophilic facilities (propranolol) act several hours and quickly derived from the body. Hydrophilic preparations (atenolol) are effective for a longer time, can be assigned less frequently. Currently created lipophilic substances long action (Metoprolol Retard). In addition, there are women with a very small duration of action - up to 30 minutes (esmolol).

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1. Noncardiodelective Bab:

BUT. Without internal sympathomimetic activity:

• propranolol (Anaprilin, Obizant);
• nadolol (Corgard);
• satolol (Sotagexal, Tensol);
• timolol (blocarden);
• nipradilol;
• flestrolol.

• oplespolol (trazicor);
• pindolol (wqquen);
• alprenolol (APTIN);
• penbutolol (Betapressin, Levatol);
• bopindolol (Sandonorm);
• bucindolol;
• dilealol;
• carolol;
• labetalol.

2. Cardooselective women:

A. Without internal sympathomimetic activity:

B. With internal sympathomimetic activity:

• acelebalol (acecor, sectal);
• talinolol (Cordanum);
• coleiprolol;
• emolol (Vasakor).

3. BB with vazodilative properties:

A. Narkdiodelective:

B. Cardooselective:

• carvedilol;
• nebivolol;
• coleiprolol.

4. Long-term women:

A. Narkdiodelective:

• bopindolol;
• supolyol;
• penbutolol;
• satolol.

B.
Cardooselective:

• atenolol;
• betaxolol;
• bisoprolol;
• empapolol.

5. Babs of ultrashort action, cardiolective:

• eSMOLOL.

Application for diseases of the cardiovascular system

Threw stress

In many cases, women are one of the leading means to treat and prevent attacks. Unlike nitrates, these funds do not cause tolerance (drug sustainability) with long use. Babs are capable of cumulating (accumulating) in the body, which allows you to reduce the dosage of the drug after a while. In addition, these funds protect the heart muscle itself, improving the forecast by reducing the risk of myocardial repeated infarction.

Antianginal activity of all women is about the same.
Their choice is based on the duration of the effect, the severity of side effects, costs and other factors.

We begin treatment with a small dose, gradually increasing it to effective. The dosage is selected in such a way that the frequency of the heart abbreviations at rest was not lower than 50 per minute, and the level of systolic blood pressure is at least 100 mm RT. Art. After the onset therapeutic effect (The cessation of angina seizures, improving the tolerance of physical exertion) The dose is gradually reduced to the minimum efficient.

Prolonged use of high doses of women is inappropriate, as it significantly increases the risk of side effects. With insufficient effectiveness of these funds, it is better to combine them with other groups of drugs.

Babs can not be abruptly canceled, as it may occur with cancellation syndrome.

Babs are especially shown if the stroke angina is combined with sinus tachycardia, glaucoma, constipation and gastroofine reflux.

Myocardial infarction

Early use of women when it helps to limit the cordial muscle necrosis area. At the same time, mortality decreases, the risk of myocardial infarction and the heart stop decreases.

Such an effect is provided by women without internal sympathomimetic activity, it is preferable to use cardio selective tools. They are especially useful in combining myocardial infarction with arterial hypertension, sinus tachycardia, post-infarction angina and a tachiisistolic form.

Bab can be prescribed immediately when the patient is admitted to the hospital with all patients in the absence of contraindications. In the absence of side effects, the treatment of them continues at least a year after the myocardial infarction.

Chronic heart failure

The use of women in heart failure is studied. It is believed that they can be used when combined with heart failure (especially diastolic) and angina stress. Rhythm disorders, arterial hypertension, a tachiisistolic form of atrial fibrillation in combination with also the grounds for the appointment of this group of drugs.

Hypertonic disease

Babs are shown in the treatment hypertensive diseasecomplicated. They are also widely used in young patients leading an active lifestyle. This group of drugs is prescribed by combining arterial hypertension with stress angina or violations of the heart rhythm, as well as after the myocardial infarction.

Disturbance of cardiac rhythm

Babs are used with such heart rate disorders such as fibrillation and fluttering atrial, sucanementaricular arrhythmias, poorly transferred sinus tachycardia. They can also be appointed during rhythm violations, but their effectiveness in this case is usually less expressed. Bab in combination with potassium preparations are used for the treatment caused by glycoside intoxication.

Side effects

The cardiovascular system

Bab depress the ability of a sinus node to produce pulses that cause heart cuts and cause sinusovoy bradycardia - Slowing the pulse to the values \u200b\u200bless than 50 per minute. This side effect is significantly less pronounced in women with internal sympathomimetic activity.

Preparations of this group can cause an atrioventricular blockade of varying degrees. They reduce the strength of heart abbreviations. The last side effect is less pronounced in women with vazodilative properties. Babs reduce blood pressure.

Medicines of this group cause spasm of peripheral vessels. A cooling limbs may appear, the Raino syndrome is worse. These side effects are almost deprived of preparations with vazodilative properties.

Babs reduce the renal blood flow (except for the supolyol). Due to the deterioration of peripheral blood circulation in the treatment with these means, there is sometimes a pronounced general weakness.

Respiratory system

Bab causes the spasm of the bronchi due to the concomitant blockade of β2-adrenoreceptors. This side effect is less pronounced in cardiodelective funds. However, their doses, effective in relation to angina or hypertension, are often sufficiently high, while cardioselitivity is significantly reduced.
The use of high doses of women can provoke apnea, or a temporary stop of breathing.

Bab worsen the current allergic reactions On the bites of insects, medicinal and food allergens.

Nervous system

Propranolol, metoprolol and other lipophilic women penetrate blood into the cerebral cells through the hematorencephalic barrier. So they can cause headache, sleep disorders, dizziness, memory deterioration and depression. In severe cases, hallucinations arise, convulsions, coma. These side effects are significantly less pronounced in hydrophilic women, in particular, Atenolol.

Treatment of women can be accompanied by a violation of neuromuscular conductivity. This leads to the emergence of muscle weakness, decrease in endurance and fast fatigue.

Metabolism

Non-selective women suppress insulin production in the pancreas. On the other hand, these drugs brake mobilization of glucose from the liver, contributing to the development of prolonged hypoglycemia in patients with diabetes. Hypoglycemia contributes to the heating into the blood of adrenaline acting on alpha-adrenoreceptors. This leads to a significant rise in blood pressure.

Therefore, if necessary, the appointment of women patients with accompanying diabetes mellitus, it is necessary to prefer with cardiolalective drugs or replace them with calcium antagonists or other groups.

Many women, especially non-selective, reduce the content of "good" cholesterol (high density alpha-lipoproteins) and increase the level of "bad" (triglycerides and lipoproteins of very low density). This disadvantage is deprived of drugs with β1-internal sympathomimetic and α-blocking activity (carvedilol, labetolol, pindolol, dilellol, celiprolol).

Other side effects

Treatment of women in some cases is accompanied by sexual dysfunction: violation of the erection and loss of sexual entry. The mechanism of such an effect is unclear.

Bab can cause skin changes: rash, itching, erythema, symptoms of psoriasis. In rare cases, hair loss and stomatitis is recorded.

One of the serious side effects is the oppression of blood formation with the development of agranulocytosis and thrombocytopenic purpura.

Cancellation syndrome

If women are used for a long time in high dosage, the sudden cessation of treatment can provoke the so-called cancellation syndrome. It is manifested by the participation of angina attacks, the emergence of ventricular rhythm disorders, the development of myocardial infarction. In easier cases, the abolition syndrome is accompanied by tachycardia and an increase in blood pressure. Cancellation syndrome is usually manifested several days after the cease of reception of women.

To avoid the development of cancellation syndrome, you need to follow the following rules:

• cancel Babe slowly, for two weeks, gradually reducing the dosage for one reception;
• during and after the abolition of women, it is necessary to limit physical exercise, if necessary, increase the dosage of nitrates and other antichangative funds, as well as drugs that reduce blood pressure.

Contraindications

Bab is absolutely contraindicated in the following situations:

• swelling of lungs and cardiogenic shock;
• severe heart failure;
• bronchial asthma;
• atrioventricular blockade II - III degree;
• the level of systolic blood pressure is 100 mm Hg. Art. and below;
• cardiac frequency less than 50 per minute;
• poorly controlled insulin-dependent diabetes mellitus.

Relative contraindications to the appointment of women - Riino and atherosclerosis of peripheral arteries with the development of interspersed chromium.