Selective drugs. Adrenergic blockers: action, features of use. Lipo- and hydrophilic preparations

Beta blockers: pharmacological properties and clinical applications

S. Yu. Shtrygol, Dr. med. Sciences, Professor National Pharmaceutical University, Kharkov

β-adrenergic receptor blockers (antagonists) have been successfully used in cardiology and other areas of medicine for about 40 years. The first β-blocker was dichloroisopropylnorepinephrine, which has now lost its value. More than 80 drugs of similar action have been created, but not all of them have wide clinical use.

β-blockers are characterized by a combination of the following most important pharmacological effects: hypotensive, antianginal and antiarrhythmic. Along with this, β-blockers have other types of action, for example, psychotropic effects (in particular, tranquilizing), the ability to lower intraocular pressure. For arterial hypertension, β-blockers are among the first-line drugs, especially in young patients with a hyperkinetic type of circulation.

β-adrenergic receptors play an important role in the regulation of physiological functions. These receptors specifically recognize and bind molecules of the adrenal medulla hormone adrenaline and the neurotransmitter norepinephrine circulating in the blood and transmit the molecular signals received from them to effector cells. β-adrenergic receptors are coupled with G-proteins, and through them with the enzyme adenylate cyclase, which catalyzes the formation of cyclic adenosine monophosphate in effector cells.

Since 1967, two main types of β-receptors have been identified. β1-adrenergic receptors are localized mainly on the postsynaptic membrane in the myocardium and conduction system of the heart, in the kidneys and adipose tissue. Their excitation (provided mainly by the neurotransmitter norepinephrine) is accompanied by an increase in heart rate, increased heart automaticity, facilitation of atrioventricular conduction, and an increase in the heart's need for oxygen. In the kidneys they mediate the release of renin. Blockade of β1-adrenergic receptors leads to the opposite effects.

β2-adrenergic receptors are located on the presynaptic membrane of adrenergic synapses; when they are excited, the release of the mediator norepinephrine is stimulated. There are also extrasynaptic adrenergic receptors of this type, predominantly excited by circulating adrenaline. β2-adrenergic receptors predominate in the bronchi, in the vessels of most organs, in the uterus (when excited, the smooth muscles of these organs relax), in the liver (when excited, glycogenolysis and lipolysis increase), pancreas (control insulin release), in platelets (reduce the ability to aggregate ). Both types of receptors are present in the CNS. In addition, another subtype of β-adrenergic receptors (β3 -) was discovered relatively recently, localized primarily in adipose tissue, where their stimulation stimulates lipolysis and heat production. The clinical significance of agents that can block these receptors remains to be clarified.

Depending on the ability to block both main types of β-adrenergic receptors (β1 - and β2 -) or to block predominantly β1-receptors, which predominate in the heart, cardiononselective (i.e., non-selective) and cardioselective (selective for β1-adrenergic receptors of the heart) are distinguished. drugs.

The table shows the most important representatives of β-blockers.

Table. The main representatives of β-adrenergic receptor antagonists

Basic pharmacological properties
β-blockers

By blocking β-adrenergic receptors, drugs in this group prevent the influence of norepinephrine on them, a mediator released from sympathetic nerve endings, as well as adrenaline circulating in the blood. Thus, they weaken the sympathetic innervation and the effect of adrenaline on various organs.

Hypotensive effect. Drugs in this group reduce blood pressure due to:

1. Weakening the influence of the sympathetic nervous system and circulating adrenaline on the heart (decreasing the strength and frequency of heart contractions, and therefore the stroke and minute volume of the heart)
2. Reducing vascular tone due to relaxation of their smooth muscles, but this effect is secondary and occurs gradually (initially, vascular tone may even increase, since β-adrenergic receptors in the vessels, when excited, promote relaxation of smooth muscles, and when β-receptors are blocked, vascular tone increases due to the predominance influences on α-adrenergic receptors). Only gradually, due to a decrease in the release of norepinephrine from sympathetic nerve endings and due to a decrease in the secretion of renin in the kidneys, as well as due to the central action of β-blockers (reduction of sympathetic influences), the total peripheral resistance decreases.
3. Moderate diuretic effect due to inhibition of tubular reabsorption of sodium (Shtrygol S. Yu., Branchevsky L. L., 1995).

The hypotensive effect is practically independent of the presence or absence of selectivity of β-adrenergic receptor blockade.

Antiarrhythmic effect caused by inhibition of automatism in the sinus node and in heterotopic foci of excitation. Most β-blockers also have a moderate local anesthetic (membrane stabilizing) effect, which is important for their antiarrhythmic effect. However, β-blockers slow down atrioventricular conduction, which underlies their adverse effects of atrioventricular block.

Antianginal effect based primarily on a decrease in the heart's oxygen demand due to a decrease in the frequency and contractility of the myocardium, as well as a decrease in lipolysis activity and a decrease in the content of fatty acids in the myocardium. Consequently, with less cardiac work and lower levels of energy substrates, the myocardium requires less oxygen. In addition, β-blockers enhance the dissociation of oxyhemoglobin, which improves myocardial metabolism. β-blockers do not dilate coronary vessels. But due to bradycardia, lengthening diastole, during which intense coronary blood flow occurs, they can indirectly help improve blood supply to the heart.

Along with the listed types of action of β-blockers, which are of high relevance in cardiology, one cannot help but dwell on the antiglaucomatous effect of the drugs in question, which is important in ophthalmology. They reduce intraocular pressure by reducing the production of intraocular fluid; For this purpose, mainly the non-selective drug timolol (Ocumed, Okupres, arutimol) and the β1-adrenergic blocker betaxolol (Betoptik) in the form of eye drops are used.

In addition, β-blockers reduce insulin secretion in the pancreas, increase bronchial tone, and increase the content of atherogenic fractions of lipoproteins (low and very low density) in the blood. These properties underlie the side effects that will be discussed in detail below.

β-blockers are classified not only by their ability to selectively or non-selectively block β-adrenergic receptors, but also by the presence or absence of intrinsic sympathomimetic activity. It is found in pindolol (Wisken), oxprenolol (Trazicor), acebutolol (Sectral), talinolol (Cordanum). Due to their special interaction with β-adrenergic receptors (stimulation of their active centers to a physiological level), these drugs at rest practically do not reduce the frequency and strength of heart contractions, and their blocking effect appears only when the level of catecholamines increases during emotional or physical stress.

Adverse effects such as a decrease in insulin secretion, an increase in bronchial tone, and atherogenic effects are especially characteristic of non-selective drugs without internal sympathomimetic activity and almost do not appear in β1-selective drugs in small (medium therapeutic) doses. With increasing doses, the selectivity of action decreases and may even disappear.

β-blockers vary in their ability to dissolve in lipids. This is associated with such features as penetration into the central nervous system and the ability to be metabolized and excreted from the body in one way or another. Metoprolol (egilok), propranolol (anaprilin, inderal, obzidan), oxprenolol (trazicor) are lipophilic, therefore they penetrate the central nervous system and can cause drowsiness, lethargy, lethargy, and are metabolized by the liver, so they should not be prescribed to patients with impaired liver function. Atenolol (Tenormin) and acebutolol (Sectral) are hydrophilic, almost do not penetrate the brain and cause virtually no side effects from the central nervous system, but are excreted by the kidneys, so they should not be prescribed to patients with renal failure. Pindolol (wisken) occupies an intermediate position.

Drugs such as propranolol and oxprenolol act for a relatively short time (about 8 hours) and are prescribed 3 times a day. It is enough to take metoprolol 2 times a day, and atenolol once a day. The remaining drugs listed in the classification can be prescribed 2-3 times a day.

There is conflicting information on the effect of β-blockers on the life expectancy of patients. Some authors have established its increase (Olbinskaya L. I., Andrushchishina T. B., 2001), others indicate its decrease due to disorders of carbohydrate and lipid metabolism with long-term use (Mikhailov I. B., 1998).

Indications

β-blockers are used for hypertension and symptomatic arterial hypertension, especially with the hyperkinetic type of blood circulation (it is manifested clinically by excessively pronounced tachycardia and a significant increase in systolic blood pressure during physical activity).

They are also prescribed for coronary heart disease (angina at rest and variant, especially insensitive to nitrates). The antiarrhythmic effect is used for sinus tachycardia, atrial fibrillation, and ventricular extrasystole (for arrhythmias, doses are usually lower than for arterial hypertension and angina pectoris).

In addition, β-blockers are used for hypertrophic cardiomyopathy, thyrotoxicosis (especially with an allergy to Mercazolil), migraine, and parkinsonism. Non-selective drugs can be used to induce labor in women with high blood pressure. In the form of ophthalmic dosage forms, β-blockers, as already noted, are used for glaucoma.

Features of the destination,
dosage regimen

For arterial hypertension, coronary heart disease and cardiac arrhythmias, β-blockers are usually prescribed in the following dosages.

Propranolol (anaprilin) ​​is available in tablets of 0.01 and 0.04 g and in ampoules of 1 ml of 0.25% solution, 0.01-0.04 g is prescribed orally 3 times a day (daily dose 0. 03-0.12 g). Oxprenolol (Trazicor) is available in tablets of 0.02 g, prescribed 1-2 tablets 3 times a day. Pindolol (wisken) is available in tablets of 0.005; 0.01; 0.015 and 0.02 g, in the form of a 0.5% solution for oral administration and in ampoules of 2 ml of a 0.2% solution for injection. It is prescribed orally at 0.01-0.015 g per day in 2-3 doses, the daily dose can be increased to 0.045 g. 2 ml of 0.2% solution is administered intravenously slowly. Metoprolol (betaloc, metocard) is available in tablets of 0.05 and 0.1 g. It is prescribed orally at 0.05-0.1 g 2 times a day, the maximum daily dose is 0.4 g (400 mg). Metocard-retard is a long-acting drug of metoprolol, available in tablets of 0.2 g. Prescribed 1 tablet 1 time per day (in the morning). Atenolol (tenormin) is available in tablets of 0.05 and 0.1 g, administered orally in the morning (before meals) once a day, 0.05-0.1 g. Acebutolol (sectral) - available in tablets of 0.05-0.1 g. 2 g, administered orally 0.4 g (2 tablets) once in the morning or in two doses (1 tablet morning and evening). Talinolol (kordanum) - available in tablets of 0.05 g. Prescribed 1-2 tablets 1-2 times a day 1 hour before meals.

The hypotensive effect reaches its maximum gradually, over 1-2 weeks. The duration of treatment is usually at least 1-2 months, often several months. The withdrawal of β-blockers should be done gradually, with a dose reduction over 1-1.5 weeks to half the minimum therapeutic dose, otherwise withdrawal syndrome may develop. During treatment, it is necessary to control the heart rate (bradycardia at rest no more than 30% of the initial level; during physical activity, tachycardia no more than 100-120 beats/min), ECG (PQ interval should increase by no more than 25% ). It makes sense to determine the level of glucose in the blood and urine and low- and very low-density lipoproteins, especially with long-term use of beta-blockers.

In patients with concomitant arterial hypertension, obstructive pulmonary diseases and metabolic disorders, preference is given to cardioselective drugs (Egilok, Metocard, Tenormin, Sectral, Cordanum) in minimal effective doses or in combination with other antihypertensive drugs.

Side effects
and the possibilities of their correction

The following side effects are typical for beta-adrenergic blockers.

• Severe bradycardia, impaired atrioventricular conduction, development of heart failure (mainly for drugs that lack internal sympathomimetic activity).
• Bronchial obstruction (mainly for drugs that indiscriminately block β-adrenergic receptors). This effect is especially dangerous in patients with altered bronchial reactivity and suffering from bronchial asthma. Since β-blockers can be absorbed into the blood and cause bronchial obstruction even when used in the form of eye drops, ophthalmologists should take this ability into account when prescribing timolol or betaxolol to patients with glaucoma combined with bronchial asthma. After introducing eye drops into the conjunctival sac, it is recommended to press the inner corner of the eye for 2-3 minutes to avoid the solution getting into the nasolacrimal duct and nasal cavity, from where the drug can be absorbed into the blood.
• Central nervous system disorders: fatigue, decreased attention, headache, dizziness, sleep disturbances, agitation or, conversely, depression, impotence (especially for lipophilic drugs: metoprolol, propranolol, oxprenolol).
• Deterioration of lipid metabolism accumulation of cholesterol in low and very low density lipoproteins, increased atherogenic properties of blood serum, especially in conditions of increased dietary consumption of sodium chloride. This property certainly reduces the therapeutic value of β-blockers in cardiology, since it means an increase in atherosclerotic vascular damage. To correct this side effect, we have experimentally developed and tested in the clinic a method consisting in the use of potassium and magnesium salts, in particular, sanasol in a daily dose of 3 g for adding salt to ready-made dishes against the background of limiting dietary intake of table salt (Shtrygol S. Yu., 1995; Shtrygol S. Yu. et al., 1997). In addition, it was found that the atherogenic properties of β-blockers are weakened by the simultaneous administration of papaverine (Andrianova I. A., 1991).
• Hyperglycemia, impaired glucose tolerance.
• Increased level of uric acid in the blood.
• Vasospasm of the lower extremities (intermittent claudication, exacerbation of Raynaud's disease, obliterating endarteritis) mainly for drugs that can block β2-adrenergic receptors.
• Dyspeptic symptoms: nausea, heaviness in the epigastrium.
• Increased uterine tone and bradycardia in the fetus during pregnancy (especially for drugs that block β2-adrenergic receptors).
• Withdrawal syndrome (forms 1-2 days after sudden cessation of taking the drug, lasts up to 2 weeks); To prevent it, as already noted, it is necessary to reduce the dose of β-blockers gradually, over a period of at least 1 week.
• It is relatively uncommon for β-blockers to cause allergic reactions.
• A rare side effect is oculocutaneous syndrome (conjunctivitis, adhesive peritonitis).
• In isolated cases, talinolol can cause sweating, weight gain, decreased tear secretion, alopecia, and increased symptoms of psoriasis; the latter effect has also been described with the use of atenolol.

Contraindications

Severe heart failure, bradycardia, sick sinus syndrome, atrioventricular block, arterial hypotension, bronchial asthma, obstructive bronchitis, peripheral circulatory disorders (Raynaud's disease or syndrome, obliterating endarteritis, atherosclerosis of the lower extremity vessels), diabetes mellitus types I and II.

Interaction with other drugs

Rational combinations.β-blockers combine well with α-blockers (there are so-called “hybrid” α, β-blockers, for example labetalol, proxodolol). These combinations enhance the hypotensive effect, while simultaneously with a decrease in cardiac output, the total peripheral vascular resistance quickly and effectively decreases.

Combinations of β-blockers with nitrates are successful, especially when arterial hypertension is combined with coronary heart disease; at the same time, the hypotensive effect is enhanced, and the bradycardia caused by β-blockers is neutralized by the tachycardia caused by nitrates.

Combinations of β-blockers with diuretics are favorable, since the effect of the latter is enhanced and somewhat prolonged due to the inhibition of renin release in the kidneys by β-blockers.

The action of β-blockers and ACE inhibitors, angiotensin receptor blockers is very successfully combined. For drug-resistant arrhythmias, β-blockers can be combined with caution with procainamide and quinidine.

Valid combinations. Beta-blockers can be combined with caution in low doses with calcium channel blockers belonging to the dihydropyridine group (nifedipine, phenigidine, cordafen, nicardipine, etc.).

Irrational and dangerous combinations. It is unacceptable to combine β-adrenergic receptor antagonists with calcium channel blockers of the verapamil group (verapamil, isoptin, finoptin, gallopamil), since this potentiates a decrease in the frequency and strength of heart contractions, and deterioration of atrioventricular conduction; excessive bradycardia and hypotension, atrioventricular block, and acute left ventricular failure are possible.

β-blockers cannot be combined with sympatholytics reserpine and drugs containing it (raunatin, rauvazan, adelfan, cristepine, brinerdine, trirezide), octadine, since these combinations sharply weaken the sympathetic effects on the myocardium and can lead to similar complications.

Combinations of β-blockers with cardiac glycosides (increases the risk of bradyarrhythmias, blockades and even cardiac arrest), with direct M-cholinomimetics (aceclidine) and anticholinesterase drugs (prozerin, galantamine, amiridine), tricyclic antidepressants (imipramine) for the same reasons.

Cannot be combined with antidepressants MAO inhibitors (nialamide), as a hypertensive crisis is possible.

The effect of such drugs as typical and atypical β-adrenomimetics (isadrine, salbutamol, oxyphedrine, nonachlazine, etc.), antihistamines (diphenhydramine, diprazine, fenkarol, diazolin, etc.), glucocorticoids (prednisolone, hydrocortisone, budesonide, ingacort, etc. ) when combined with β-blockers is weakened.

It is irrational to combine β-blockers with theophylline and drugs containing it (aminophylline) due to slower metabolism and accumulation of theophylline.

When β-blockers are taken simultaneously with insulin and oral hypoglycemic agents, an excessive hypoglycemic effect develops.

β-blockers weaken the anti-inflammatory effect of salicylates, butadione, and the antithrombotic effect of indirect anticoagulants (neodicoumarin, phenylin).

In conclusion, it must be emphasized that in modern conditions, preference is given to β-blockers of cardioselective action (β1-blockers) as the safest in relation to broncho-obstruction, disorders of lipid and carbohydrate metabolism and peripheral circulation, having a longer duration of action and therefore taken in a more convenient mode for the patient (1-2 times a day).

Literature

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3. Gaevy M. D., Galenko-Yaroshevsky P. A., Petrov V. I., etc. Pharmacotherapy with the basics of clinical pharmacology / Ed. V. I. Petrova. Volgograd, 1998. 451 p.
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5. Lyusov V. A., Kharchenko V. I., Savenkov P. M. et al. Potentiation of the hypotensive effect of labetalol in patients with hypertension when affecting the sodium balance in the body // Cardiology. 1987. No. 2. P. 71 -77.
6. Mikhailov I. B. Clinical pharmacology. St. Petersburg: Foliant, 1998. 496 p.
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Beta-adrenergic receptor blockers, commonly known as beta blockers, are an important group of hypertension medications that act on the sympathetic nervous system. These drugs have been used in medicine for a long time, since the 1960s. The discovery of beta blockers has significantly increased the effectiveness of treating cardiovascular diseases, as well as hypertension. Therefore, the scientists who were the first to synthesize and test these drugs in clinical practice were awarded the Nobel Prize in Medicine in 1988.

In the practice of treating hypertension, beta blockers are still medications of primary importance, along with diuretics, i.e. diuretics. Although, since the 1990s, new groups of drugs have also appeared (calcium antagonists, ACE inhibitors), which are prescribed when beta blockers do not help or are contraindicated for the patient.

Popular medicines:

History of discovery

In the 1930s, scientists discovered that it was possible to stimulate the ability of the heart muscle (myocardium) to contract if it was exposed to special substances - beta-agonists. In 1948, the concept of the existence of alpha and beta adrenergic receptors in the mammalian body was put forward by R. P. Ahlquist. Later, in the mid-1950s, scientist J. Black theoretically developed a way to reduce the frequency of angina attacks. He suggested that it would be possible to invent a drug that would effectively “protect” the beta receptors of the heart muscle from the influence of adrenaline. After all, this hormone stimulates the muscle cells of the heart, causing them to contract too intensely and causing heart attacks.

In 1962, under the leadership of J. Black, the first beta blocker, protenalol, was synthesized. But it turned out to cause cancer in mice, so it was not tested on humans. The first medicine for humans was propranolol, which appeared in 1964. For the development of propranolol and the “theory” of beta blockers, J. Black received the Nobel Prize in Medicine in 1988. The most modern drug in this group, nebivolol, was launched on the market in 2001. It and other third-generation beta blockers have the additional important benefit of relaxing blood vessels. In total, more than 100 different beta blockers were synthesized in laboratories, but no more than 30 of them were or are still used by practicing physicians.

Mechanism of action of beta blockers

The hormone adrenaline and other catecholamines stimulate beta-1 and beta-2 adrenergic receptors, which are found in various organs. The mechanism of action of beta blockers is that they block beta-1 adrenergic receptors, “shielding” the heart from the effects of adrenaline and other “accelerating” hormones. As a result, the work of the heart becomes easier: it contracts less frequently and with less force. Thus, the frequency of angina attacks and heart rhythm disturbances is reduced. The likelihood of sudden cardiac death is reduced.

Beta blockers lower blood pressure through several different mechanisms simultaneously:

• Decreased heart rate and strength;
• Decreased cardiac output;
• Decreased secretion and decreased concentration of renin in the blood plasma;
• Restructuring of the baroreceptor mechanisms of the aortic arch and sinocarotid sinus;
• Depressant effect on the central nervous system;
• Effect on the vasomotor center - decreased central sympathetic tone;
• Decreased peripheral vascular tone due to alpha-1 receptor blockade or nitric oxide (NO) release.

Beta-1 and beta-2 adrenergic receptors in the human body

From the table we see that beta-1 adrenergic receptors are found, for the most part, in the tissues of the cardiovascular system, as well as skeletal muscles and kidneys. This means that stimulating hormones increase the rate and force of heart contractions.

Beta blockers serve as protection against atherosclerotic heart disease, relieving pain and preventing further development of the disease. The cardioprotective effect (protection of the heart) is associated with the ability of these drugs to reduce regression of the left ventricle of the heart and have an antiarrhythmic effect. They reduce pain in the heart area and reduce the frequency of angina attacks. But Beta blockers are not the best choice of drugs for treating hypertension unless the patient has complaints of chest pain and heart attacks.

Unfortunately, simultaneously with the blockade of beta-1 adrenergic receptors, beta-2 adrenergic receptors are also targeted, which there is no need to block. Because of this, negative side effects from taking medications occur. Beta blockers have serious side effects and contraindications. They are described in detail below in the article. The selectivity of a beta blocker is the extent to which a particular drug is able to block beta 1 adrenergic receptors without affecting beta 2 adrenergic receptors. All other things being equal, the higher the selectivity, the better, because there are fewer side effects.

Classification

Beta blockers are divided into:

• selective (cardioselective) and non-selective;
• lipophilic and hydrophilic, i.e. soluble in fats or water;
• There are beta blockers with and without intrinsic sympathomimetic activity.

We will consider all these characteristics in detail below. Now the main thing to understand is that There are 3 generations of beta blockers, and there will be more benefit if treated with a modern medicine, and not outdated. Because the effectiveness will be higher, and there will be much fewer harmful side effects.

Classification of beta blockers by generation (2008)

Third-generation beta blockers have additional vasodilating properties, i.e. the ability to relax blood vessels.

• When taking labetalol, this effect occurs because the drug blocks not only beta-adrenergic receptors, but also alpha-adrenergic receptors.
• Nebivolol increases the synthesis of nitric oxide (NO), a substance that regulates vascular relaxation.
• And carvedilol does both.

What are cardioselective beta blockers?

There are receptors in the tissues of the human body that respond to the hormones adrenaline and norepinephrine. Currently, alpha-1, alpha-2, beta-1 and beta-2 adrenergic receptors are distinguished. Recently, alpha-3 adrenergic receptors have also been described.

The location and significance of adrenergic receptors can be briefly presented as follows:

• alpha-1 - are localized in blood vessels, stimulation leads to their spasm and increased blood pressure.
• alpha-2 - are a “negative feedback loop” for the tissue regulation system. This means that their stimulation leads to a decrease in blood pressure.
• beta-1 - are localized in the heart, their stimulation leads to an increase in the frequency and strength of heart contractions, and also increases the myocardial oxygen demand and increases blood pressure. Also, beta-1 adrenergic receptors are present in large quantities in the kidneys.
• beta-2 - localized in the bronchi, stimulation causes relief of bronchospasm. These same receptors are located on liver cells; the effect of the hormone on them causes the conversion of glycogen into glucose and the release of glucose into the blood.

Cardioselective beta blockers are active primarily against beta-1 adrenergic receptors, rather than selective beta blockers, equally block both beta-1 and beta-2 adrenergic receptors. In the cardiac muscle, the ratio of beta-1 and beta-2 adrenergic receptors is 4:1, i.e., energetic stimulation of the heart is carried out mostly through beta-1 receptors. As the dosage of beta blockers increases, their specificity decreases, and then the selective drug blocks both receptors.

Selective and non-selective beta blockers reduce blood pressure approximately equally, but Cardioselective beta blockers have fewer side effects, they are easier to use for concomitant diseases. Thus, selective drugs are less likely to cause bronchospasm, since their activity will not affect beta-2 adrenergic receptors, which are located mostly in the lungs.

Cardio-selectivity of beta blockers: beta-1 and beta-2 adrenergic receptor blocking index

Selective beta-blockers are weaker than non-selective beta-blockers in increasing peripheral vascular resistance, so they are more often prescribed to patients with peripheral circulatory problems (for example, intermittent claudication). Please note that carvedilol (Coriol) is, although from the latest generation of beta blockers, not cardioselective. However, it is actively used by cardiologists, and the results are good. Carvedilol is rarely prescribed to lower blood pressure or treat arrhythmias. It is more often used to treat heart failure.

What is the intrinsic sympathomimetic activity of beta blockers?

Some beta blockers not only block beta adrenergic receptors, but also stimulate them. This is called the intrinsic sympathomimetic activity of some beta blockers. Drugs that have intrinsic sympathomimetic activity are characterized by the following properties:

• these beta blockers slow your heart rate to a lesser extent
• they do not significantly reduce the pumping function of the heart
• to a lesser extent increase total peripheral vascular resistance
• less likely to provoke atherosclerosis because they do not have a significant effect on blood cholesterol levels

You can find out which beta blockers have intrinsic sympathomimetic activity and which drugs do not.

If beta-blockers, which have intrinsic sympathomimetic activity, are taken for a long time, chronic stimulation of beta-adrenergic receptors occurs. This gradually leads to a decrease in their density in tissues. After this, suddenly stopping the medication does not cause withdrawal symptoms. At all, The dose of beta blockers should be reduced gradually: 2 times every 2-3 days for 10-14 days. Otherwise, serious withdrawal symptoms may appear: hypertensive crises, increased frequency of angina attacks, tachycardia, myocardial infarction or sudden death due to a heart attack.

Studies have shown that beta blockers, which have intrinsic sympathomimetic activity, are no different in their effectiveness in lowering blood pressure than drugs that do not have this activity. But in some cases, the use of drugs with internal sympathomimetic activity allows one to avoid unwanted side effects. Namely, bronchospasm with airway obstruction of various nature, as well as spasms in the cold with atherosclerosis of the vessels of the lower extremities. In recent years (July 2012), doctors have come to the conclusion that one should not attach much importance to whether a beta blocker has intrinsic sympathomimetic activity or not. Practice has shown that drugs with this property reduce the incidence of cardiovascular complications no more than those beta blockers that do not.

Lipophilic and hydrophilic beta blockers

Lipophilic beta blockers are soluble in fat, while hydrophilic beta blockers are soluble in water. Lipophilic drugs undergo significant “processing” during their initial passage through the liver. Hydrophilic beta-blockers are not metabolized in the liver. They are excreted from the body mainly in urine, unchanged. Hydrophilic beta blockers last longer because they are not eliminated as quickly as lipophilic beta blockers.

Lipophilic beta blockers penetrate the blood-brain barrier better. It is a physiological barrier between the circulatory system and the central nervous system. It protects nervous tissue from microorganisms, toxins and “agents” of the immune system circulating in the blood, which perceive brain tissue as foreign and attack it. Through the blood-brain barrier, nutrients enter the brain from the blood vessels, and waste products from the nervous tissue are removed back.

It turned out that lipophilic beta-blockers are more effective in reducing mortality in patients with coronary heart disease. At the same time, they cause more side effects from the central nervous system:

• depression;
• sleep disorders;
• headache.

In general, the activity of fat-soluble beta-blockers is not affected by food intake. It is advisable to take hydrophilic preparations before meals with plenty of water.

The drug bisoprolol is notable for its ability to dissolve in both water and lipids (fats). If the liver or kidneys are not working well, then the task of removing bisoprolol from the body is automatically taken over by the healthier system.

Modern beta blockers

• carvedilol (Ccoriol);
• bisoprolol (Concor, Biprol, Bisogamma);
• metoprolol succinate (Betaloc LOC);
• nebivolol (Nebilet, Binelol).

Other beta blockers can be used to treat hypertension. Doctors are recommended to prescribe second- or third-generation drugs to their patients. Above in the article you can find a table that describes which generation each drug belongs to.

Modern beta blockers reduce the likelihood of a patient dying from a stroke, and especially from a heart attack. At the same time, studies since 1998 have systematically shown that propranolol (anaprilin) ​​not only does not reduce, but even increases mortality compared to placebo. There is also conflicting data on the effectiveness of atenolol. Dozens of articles in medical journals claim that it reduces the likelihood of cardiovascular “events” much less than other beta blockers, while causing more side effects.

Patients should understand that all beta blockers reduce blood pressure approximately equally. Perhaps nebivolol does this a little more effectively than everyone else, but not by much. At the same time, they reduce the likelihood of developing cardiovascular disease in very different ways. The main goal of treating hypertension is precisely to prevent its complications. It is assumed that Modern beta blockers are more effective in preventing complications of hypertension than previous generation medications. They are also better tolerated because they are less likely to cause side effects.

Back in the early 2000s, many patients could not afford to be treated with quality drugs because patented drugs were too expensive. But now you can buy generic drugs at the pharmacy, which are very affordable and still work effectively. Therefore, financial considerations are no longer a reason to avoid using modern beta blockers. The main task is to overcome the ignorance and conservatism of doctors. Doctors who do not follow the news often continue to prescribe old medications that are less effective and have significant side effects.

Indications for use

The main indications for the use of beta blockers in cardiological practice:

• arterial hypertension, including secondary (due to kidney damage, increased thyroid function, pregnancy and other reasons);
• heart failure;
• cardiac ischemia;
• arrhythmias (extrasystole, atrial fibrillation, etc.);
• long QT syndrome.

In addition, beta blockers are sometimes prescribed for vegetative crises, mitral valve prolapse, withdrawal syndrome, hypertrophic cardiomyopathy, migraine, aortic aneurysm, and Marfan syndrome.

In 2011, the results of a study of women with breast cancer who took beta blockers were published. It turned out that while taking beta blockers, metastases occur less frequently. The American study involved 1,400 women who had undergone surgery for breast cancer and were prescribed chemotherapy. These women were taking beta blockers because of cardiovascular problems they had in addition to breast cancer. After 3 years, 87% of them were alive and without cancer “events.”

The control group for comparison consisted of breast cancer patients of the same age and with the same percentage of patients with diabetes mellitus. They did not receive beta blockers and had a 77% survival rate. It is too early to draw any practical conclusions, but perhaps in 5-10 years beta blockers will become a simple and inexpensive way to improve the effectiveness of breast cancer treatment.

Use of beta blockers to treat hypertension

Beta blockers lower blood pressure generally as well as other classes of drugs. It is especially recommended to prescribe them for the treatment of hypertension in the following situations:

• Concomitant coronary heart disease
• Tachycardia
• Heart failure
• Hyperthyroidism is hyperfunction of the thyroid gland.
• Migraine
• Glaucoma
• Arterial hypertension before or after surgery

Are these medications suitable for diabetes?

Treatment with “good old” beta blockers (propranolol, atenolol) can worsen tissue sensitivity to the effects of insulin, i.e. increase insulin resistance. If a patient is predisposed, his chances of developing diabetes increase. If the patient has already developed diabetes, its course will worsen. At the same time, when using cardioselective beta blockers, tissue sensitivity to insulin deteriorates to a lesser extent. And if you prescribe modern beta blockers, which relax blood vessels, then, as a rule, in moderate doses they do not disrupt carbohydrate metabolism and do not worsen the course of diabetes.

In 2005, the Kiev Institute of Cardiology named after Academician Strazhesko studied the effect of beta blockers on patients with metabolic syndrome and insulin resistance. It turned out that carvedilol, bisoprolol and nebivolol not only do not worsen, but even increase the sensitivity of tissues to the action of insulin. At the same time, atenolol significantly worsened insulin resistance. A 2010 study showed that carvedilol did not improve vascular insulin sensitivity, but metoprolol worsened it.

Patients may experience weight gain when taking beta blockers. This occurs due to increased insulin resistance, as well as other reasons. Beta blockers reduce metabolic rate and interfere with the process of breakdown of adipose tissue (inhibit lipolysis). In this sense, atenolol and metoprolol tartrate performed poorly. At the same time, according to research results, taking carvedilol, nebivolol and labetalol was not associated with a significant increase in body weight in patients.

Taking beta blockers may affect insulin secretion by the beta cells of the pancreas. These drugs can suppress the first phase of insulin secretion. As a result, the main tool for normalizing blood sugar is the second phase of insulin release by the pancreas.

Mechanisms of influence of beta blockers on glucose and lipid metabolism

Note to the table. It should be emphasized once again that modern beta blockers have a minimal negative effect on glucose and lipid metabolism.

In insulin-dependent diabetes mellitus, an important problem is that any beta blockers may mask symptoms of impending hypoglycemia- tachycardia, nervousness and trembling (tremor). At the same time, increased sweating continues. Also, diabetics who receive beta blockers have difficulty recovering from a hypoglycemic state. Because the main mechanisms of increasing blood glucose levels - glucagon secretion, glucogenolysis and gluconeogenesis - are blocked. However, in type 2 diabetes, hypoglycemia is rarely such a serious problem as to warrant treatment with beta blockers.

It is believed that if indicated (heart failure, arrhythmia and especially previous myocardial infarction) the use of modern beta blockers in patients with diabetes is advisable. In a 2003 study, beta blockers were prescribed to patients with heart failure and diabetes. The comparison group included patients with heart failure without diabetes. In the first group, mortality decreased by 16%, in the second - by 28%.

Diabetics are recommended to prescribe metoprolol succinate, bisoprolol, carvedilol, nebivolol - beta blockers with proven effectiveness. If the patient does not yet have diabetes, but is at increased risk of developing it, it is recommended to prescribe only selective beta blockers and not use them in combination with diuretics (water medications). It is advisable to use drugs that not only block beta-adrenergic receptors, but also have the properties of relaxing blood vessels.

Contraindications and side effects

Read the details in the article “”. Find out what contraindications exist for their use. Some clinical situations are not absolute contraindications for treatment with beta blockers, but require increased caution. You will find details in the article linked above.

Increased risk of impotence

Erectile dysfunction (complete or partial impotence in men) is what beta blockers are most often blamed for. It is believed that beta blockers and diuretics are groups of drugs for hypertension that most often lead to a deterioration in male potency. In reality, everything is not so simple. Research convincingly proves that new modern beta blockers do not affect potency. You will find a complete list of these drugs suitable for men in the article “”. Although old generation beta blockers (not cardioselective) can indeed worsen potency. Because they impair the blood supply to the penis and possibly interfere with the production of sex hormones. Nevertheless, Modern beta blockers help men control hypertension and heart problems while maintaining potency.

In 2003, the results of a study were published on the incidence of erectile dysfunction while taking beta blockers, depending on patient awareness. First, the men were divided into 3 groups. They were all taking a beta blocker. But the first group did not know what medicine they were being given. The men in the second group knew the name of the drug. For patients in the third group, doctors not only told them which beta blocker they were prescribed, but also informed them that decreased potency is a common side effect.

In the third group, the incidence of erectile dysfunction was the highest, as much as 30%. The less information patients received, the lower the frequency of potency weakening.

Then we carried out the second stage of the study. It involved men who complained of erectile dysfunction as a result of taking a beta blocker. They were all given another pill and told that it would improve their potency. Almost all participants noted an improvement in their erections, although only half of them were given real silendafil (Viagra), and the other half were given a placebo. The results of this study convincingly prove that the reasons for the weakening of potency while taking beta blockers are largely psychological.

In conclusion of the section “Beta blockers and increased risk of impotence”, I would like to once again urge men to study the article “”. It provides a list of modern beta blockers and other medications for hypertension that do not impair potency, and perhaps even improve it. After this, you will be much more comfortable taking blood pressure medications as prescribed by your doctor. It is foolish to refuse to be treated with beta blockers or other pills for hypertension for fear of worsening potency.

Why doctors are sometimes reluctant to prescribe beta blockers

Until recent years, doctors actively prescribed beta blockers to most patients who needed treatment for high blood pressure and prevention of cardiovascular complications. Beta blockers, together with the so-called old, or traditional, drugs for hypertension. This means that the effectiveness of new blood pressure-lowering tablets, which are constantly being developed and entering the pharmaceutical market, is compared with them. First of all, they are compared with beta blockers.

After 2008, publications appeared that beta blockers should not be the first choice drugs for the treatment of patients with hypertension. We will analyze the arguments that are given. Patients can study this material, but they should remember that the final decision on which medicine to choose remains with the doctor in any case. If you don't trust your doctor, just find another one. Make every effort to consult the most experienced doctor because your life depends on it.

So, opponents of the widespread therapeutic use of beta blockers argue that:

1. These drugs are less effective than other hypertension medications in reducing the likelihood of cardiovascular complications.
2. It is believed that beta blockers do not affect the stiffness of the arteries, that is, they do not stop, much less reverse, the development of atherosclerosis.
3. These medications do little to protect target organs from the damage caused by high blood pressure.

There are also concerns that under the influence of beta blockers the metabolism of carbohydrates and fats is disrupted. As a result, the likelihood of developing type 2 diabetes mellitus increases, and if diabetes already exists, its course worsens. And that beta blockers cause side effects that impair the quality of life of patients. This refers, first of all, to a weakening of sexual potency in men. We discussed the topics “Beta blockers and diabetes” and “Increased risk of impotence” in detail above in the relevant sections of this article.

There have been studies that show that beta blockers are worse than other hypertension medications at reducing the risk of cardiovascular complications. Relevant publications in medical journals began to appear after 1998. At the same time, there is evidence from an even larger number of reliable studies that have obtained opposite results. They confirm that all major classes of blood pressure-lowering drugs have approximately the same effectiveness. The generally accepted view today is that Beta blockers are very effective after a myocardial infarction to reduce the risk of recurrent infarction. As for prescribing beta blockers for hypertension to prevent cardiovascular complications, each doctor makes his own opinion based on the results of his practical work.

If the patient has severe atherosclerosis or a high risk of atherosclerosis (see what tests need to be taken to find out), then the doctor should pay attention to modern beta blockers, which have vasodilation properties, i.e., relax blood vessels. It is the blood vessels that are one of the most important target organs that are affected by hypertension. Among people who die from cardiovascular diseases, in 90% it is vascular damage that leads to death, while the heart remains absolutely healthy.

What indicator characterizes the degree and rate of development of atherosclerosis? This is an increase in the thickness of the intima-media complex (IMC) of the carotid arteries. Regular measurement of this value using ultrasound serves to diagnose vascular damage both as a result of atherosclerosis and due to hypertension. With age, the thickness of the inner and middle linings of the arteries increases; this is one of the markers of human aging. Under the influence of arterial hypertension, this process is much accelerated. But under the influence of medications that lower blood pressure, it can slow down and even reverse. In 2005, a small study was conducted on the effect of taking beta blockers on the progression of atherosclerosis. Its participants included 128 patients. After 12 months of taking the drug, a decrease in intima-media thickness was observed in 48% of patients treated with carvedilol and in 18% of those treated with metoprolol. Carvedilol is believed to be able to stabilize atherosclerotic plaques due to its antioxidant and anti-inflammatory effects.

Features of prescribing beta blockers to elderly people

Doctors are often wary of prescribing beta blockers to older people. Because this “complex” category of patients, in addition to heart and blood pressure problems, often have concomitant diseases. Beta blockers may worsen their course. Above we discussed how drugs from the beta blocker group affect the course of diabetes. We also recommend to your attention a separate article “”. The practical situation now is that beta blockers are prescribed 2 times less often to patients over 70 years of age than to younger ones.

With the advent of modern beta blockers, side effects from their use have become much less common. Therefore, “official” recommendations now indicate that beta blockers can be more safely prescribed to older patients. Studies from 2001 and 2004 showed that bisoprolol and metoprolol succinate reduced mortality equally in younger and older patients with heart failure. In 2006, a study of carvedilol was conducted, which confirmed its high effectiveness in heart failure and good tolerability in elderly patients.

Thus, if there is evidence, then beta blockers can and should be prescribed to elderly patients. In this case, it is recommended to start taking the medicine with small doses. If possible, it is advisable to continue treatment of elderly patients with low doses of beta blockers. If there is a need to increase the dose, this should be done slowly and carefully. We recommend to your attention the articles “” and “”.

Can hypertension be treated with beta blockers during pregnancy?

What is the best beta blocker?

There are a lot of beta blocker drugs. It seems that each drug manufacturer produces its own tablets. This can make it difficult to choose the right medication. All beta blockers have approximately the same effect on lowering blood pressure, but they differ significantly in their ability to prolong the life of patients and the severity of side effects.

The doctor always chooses which beta blocker to prescribe! If the patient does not trust his doctor, then he should consult another specialist. We strongly discourage self-medication with beta blockers. Re-read the article “” again and make sure that these are not harmless pills, and therefore self-medication can cause great harm. Make every effort to be treated by the best doctor. This is the most important thing you can do to prolong your life.

The following considerations will help you choose a medicine together with your doctor (!!!):

• For patients with underlying kidney problems, lipophilic beta blockers are preferred.
• If the patient has liver disease, most likely, in this situation the doctor will prescribe a hydrophilic beta blocker. Specify in the instructions how the drug you are going to take (prescribe to the patient) is eliminated from the body.
• Old beta blockers often impair potency in men, but modern drugs do not have this unpleasant side effect. In the article ““ you will find out all the necessary details.
• There are drugs that act quickly, but not for long. They are used for hypertensive crises (labetalol intravenously). Most beta blockers do not begin to act immediately, but lower blood pressure over a long period of time and more gradually.
• It is important how many times a day you need to take this or that drug. The less, the more convenient it is for the patient, and the less likely he is to quit treatment.
• It is preferable to prescribe new generation beta blockers. They are more expensive, but have significant advantages. Namely, it is enough to take them once a day, they cause a minimum of side effects, are well tolerated by patients, do not worsen glucose metabolism and lipid levels in the blood, as well as potency in men.

Doctors who continue to prescribe the beta blocker propranolol (Anaprilin) ​​deserve condemnation. This is an outdated drug. It has been proven that propranolol (anaprilin) ​​not only does not reduce, but even increases the mortality of patients. It is also controversial whether it is worth continuing to use atenolol. In 2004, the prestigious British medical journal Lancet published an article “Atenolol for hypertension: is it a wise choice?” It stated that the prescription of atenolol was not an appropriate medication for the treatment of hypertension. Because it reduces the risk of cardiovascular complications, but does it worse than other beta blockers, as well as blood pressure medications from other groups.

You can find out which specific beta blockers are recommended earlier in this article:

• to treat heart failure and reduce the risk of sudden death from heart attack;
• men who want to lower blood pressure, but are afraid of deterioration in potency;
• diabetics and those at increased risk of diabetes;

We remind you once again that the final choice of which beta blocker to prescribe is made only by the doctor. Don't self-medicate! The financial side of the issue should also be mentioned. A lot of pharmaceutical companies produce beta blockers. They compete with each other, so the prices for these drugs are quite affordable. Treatment with a modern beta blocker will most likely cost the patient no more than $8-10 per month. Thus, the price of a drug is no longer a reason to use an outdated beta blocker.

Beta blockers are medications that block natural processes in the body. In particular, stimulation of the heart muscle with adrenaline and other “accelerating” hormones. It has been proven that these drugs in many cases can extend the patient's life by several years. But they have no effect on the causes of hypertension and cardiovascular diseases. We recommend to your attention the article “”. Magnesium deficiency in the body is one of the common causes of hypertension, heart rhythm disturbances and blockage of blood vessels with blood clots. We recommend. They eliminate magnesium deficiency and, unlike “chemical” drugs, truly help lower blood pressure and improve heart function.

For hypertension, in second place after magnesium is hawthorn extract, followed by the amino acid taurine and good old fish oil. These are natural substances that are naturally present in the body. Therefore, you will experience “side effects” from , and they will all be beneficial. Your sleep will improve, your nervous system will become calmer, swelling will go away, and in women, PMS symptoms will become much easier.

For heart problems, it comes in second place after magnesium. This is a substance that is present in every cell of our body. Coenzyme Q10 is involved in energy production reactions. In the tissues of the heart muscle its concentration is twice as high as the average. This is a phenomenally useful remedy for any heart problems. To the point that taking coenzyme Q10 helps patients avoid a heart transplant and live normally without it. Official medicine has finally recognized coenzyme Q10 as a cure for cardiovascular diseases. Registered and . This could have been done 30 years ago, because progressive cardiologists have been prescribing Q10 to their patients since the 1970s. I would especially like to note that Coenzyme Q10 improves survival of patients after a heart attack, i.e., in the same situations where beta blockers are especially often prescribed.

We recommend that patients start taking a beta blocker as prescribed by their doctor along with natural health benefits for hypertension and heart disease. At the beginning of treatment, do not try to replace the beta blocker with any “folk” methods of treatment! You may be at high risk of having a first or second heart attack. In such a situation, the medicine truly saves you from sudden death due to a heart attack. Later, after a few weeks, when you feel better, you can carefully reduce the dosage of the medicine. This should be done under the supervision of a doctor. The ultimate goal is to stay completely on natural supplements, instead of “chemical” pills. With the help of the materials on our site, thousands of people have already been able to do this, and they are very pleased with the results of this treatment. Now you.

Articles in medical journals on the treatment of hypertension and cardiovascular disease with CoQ10 and magnesium

Any modern cardiologist knows how beneficial magnesium, fish oil and coenzyme Q10 are for the heart. Tell your doctor that you will be taking a beta blocker along with these supplements. If the doctor objects. - it means that he is behind the times, and it is better for you to turn to another specialist.

1. Olga

   Is it necessary to take blockers for neurosis?

2. Tamara

   I am 62 years old, height 158, weight 82. The pressure persists for the second week, tachycardia. I drink, lozap 2 times (50 and 25 mg), ogelok (25 mg), amlotop (2.5), but there is no stabilization of pressure. Is it possible to change medications?

3. Anton

   how Q10 can replace beta blockers
   after all, they take the load off the heart during angina, and Q10 is just a vitamin

4. Stas

   51 years old 186 cm. 127 kg-
   atrial fibrillation. dry mouth. nocturnal polyuria - more than 1 liter of urine. Diabetes is not diagnosed. Sugar levels are normal in the morning. I’m on a diet. If you eat something sweet after 6 or just eat something in the evening, you get excited. insomnia. From 12 at night to 4 in the morning there was an urge to go to the toilet, which led to a disruption of the rhythm. This has been going on for many years. I accept Valz and Egilok. During the day, the bladder does not bother The adrenal glands are normal Blood tests are normal No sexual infections have been detected Can Egilok reduce the production of antidiuretic hormone? Does it make sense to change it to Concor? (I tried it once, but migraines started) Thanks

5. Natalia

   45 years old, height 167, weight 105 kg. Bisoprolol 2.5 mg was prescribed for the first time. The pressure fluctuates, but not higher than 140/90. How long should I use it, my whole life?

6. Andrey

   51 years old, 189 cm, 117 kg.
   Six years ago, the doctor prescribed Noliprel blood pressure 200/100.
   At the moment, after coughing symptoms, I stopped taking medications; my blood pressure was 160/100.
   After the examination, the doctor prescribed Valsacor 160, biprol 5 mg, Arifon retard 1.5 mg, Atoris 20 mg.
   The pressure became 110/70.
   Is it worth taking this set of medications?

7. Vadim

   I am 48 years old, height 186, weight 90 kg. I was diagnosed with hypertension at the age of 16, for the last 5 years I have been taking Locrene 5 mg once a day, the upper pressure does not rise above 130, and the lower one is often 95-100, I have also become weather-sensitive, and lately I have had poor sleep, anxiety , deterioration in sex life (poor erection) I live in a village, the doctors are far from me, I have two questions: do I need to look for a replacement for Lokren and can I sometimes take Viagra or other drugs to improve erection, thank you

8. Galina

   58 years /168cm /75kg
   working pressure is 140/90, periodically jumps to 170/100, but the main thing is that the pulse is constantly 90 and higher, even after sleep it feels like I’ve run 100 meters; Sugar and cholesterol are normal, I smoke, my diet is average (I allow fatty foods), an ultrasound showed excess fat on the liver. I periodically take anaprilin (when my pulse goes through the roof). Now the doctor prescribed bisoprolol. Should I start taking it or try to do without chemicals first?

9. Igor

   26 years old, 192cm, weight 103. I went to the doctor with tachycardia 90-100 beats/min and he prescribed me bisoprolol 5 mg per day. I work out in the gym and cycle. Can I continue training?

   1. admin Post author

      > 26 years old, 192cm, weight 103. See a doctor
      > with tachycardia 90-100 beats/min

      I explain how to determine your normal heart rate. The theoretical maximum is 220 beats per minute minus age, i.e. for you 194 beats per minute. The resting pulse is about 50% of the maximum, i.e. for you 82 plus or minus 10 beats per minute. Even with light loads, the heart rate rises to 55-65% of the theoretical maximum.

      Conclusion: if you feel normal, then you have no trace of tachycardia. But if you feel bad, then this is the second question...

      > is it possible to continue training?

      Depends on how you feel.

      If I were you, I would now do the following:
      1. Read the list of references here -
      2. Books “Younger Every Year” and “Chi-Running. A revolutionary way to run" - you can easily find it if you want.
      3. From the book “Younger Every Year” you will learn a lot of interesting things about the pulse
      4. You are overweight - study our articles in the block “Cure from hypertension in 3 weeks - it’s real” and now switch to a low-carbohydrate diet. If you do this from a young age, then in adulthood you will not have the problems that your peers will have, and they will envy your health.
      5. Buy a heart rate monitor and train with it.

      > he prescribed me bisoprolol 5 mg per day

      If you feel normal, then you don’t need bisoprolol for nothing. And if there are complaints about the heart, then you need to be thoroughly examined, and not just “suppress” the symptoms with chemical tablets.

      1. Igor

         Thanks for the answer. The complaint about my heart is that I feel it beating and at the same time there are also arrhythmias that cause discomfort. The main problem is that I am easily excitable, at the slightest stress adrenaline is released and the pulse instantly rises to 110. I did a cardiogram, the doctor said that there is dystrophy myocardium, but this is not serious and many people have this. 7 years ago I had stage 1 fibrosis of the mitral valve. I’ll go do an ultrasound and see what’s there now. Today I took a biprolol tablet and I felt much better, my pulse is 70, like an astronaut's :-) though this is not an option and I understand that. We need to get examined. As for the pressure, it happens that it rises to 140, but I would not say that this is my problem. The pressure can only play out once a month or even less often.

10. Natalia

    Please tell me, is it possible to take Nebilet when planning a pregnancy, does it affect conception?
    My husband and I take this drug, the doctor thinks it is necessary...

11. yagut

    Hello, what antihypertensive medication would you recommend for a patient taking chemotherapy? A/D 190/100, P/s 102 min.

12. Tatiana

    Hello. Mom is 80 years old. Diagnosis: hypertension with predominant heart damage. With heart failure ||st. WHO, 3st. Dyslepidemia||A according to Fredrickson.NK ||f.k (NYHA). LVDD. relative mitral regurgitation. Episodes of sinus tachycardia. Dyscirculatory encephalopathy grade 2 of complex origin (hypertensive, atherosclerotic). Significant stenosis of the right vertebral artery. Parapervical cyst of the left kidney. Prescribed: ramipril 2.5-5.0 mg in the morning, betaloc zok 25 mg in the morning, amlodipine 5 mg in the evening. The problem is that mom feels very bad, pressure surges, night tremors and shudders and a sharp increase in pressure, feelings of anxiety and fear, severe cough and dry throat. Noise in the head and knocking. Tell me whether the treatment has been prescribed correctly, is it possible to replace Betaloc with another beta blocker (as it has a strong side effect in the form of coughing attacks and shortness of breath). Mom's height is 155, weight 58 kg.

    1. admin Post author

       Is it possible to replace Betaloc with another beta blocker?

       Discuss this issue with your doctor, but this is unlikely to make sense

       severe side effects in the form of coughing attacks and shortness of breath

       I suspect that taking other beta blockers will do the same. The patient is 80 years old, her body is worn out... nothing surprising. Perhaps the doctor will decide to stop the beta blocker altogether, since the patient tolerates them so poorly. But don’t cancel it yourself, it can lead to a sudden heart attack.

       If I were you, I would no longer expect a miracle from any treatment. Read the article ““. Try adding magnesium-B6 to your mother, as prescribed there, along with the medications prescribed by the doctor. In no case instead of medications, but in addition to them.

       pressure surges, night tremors and shudders, feelings of anxiety and fear

       There is a chance that these symptoms will improve as a result of taking magnesium.

       If finances allow, then try Coenzyme Q10.

       1. Tatiana

          I want to ask you, amlodipine, my mother was prescribed to take it in the evening, what time is the best time to take it in the evening? If she drinks it at 9 p.m., her blood pressure will definitely jump. And it turns out to be a vicious circle: the medicine seems to be helping, but a surge in pressure occurs. Thank you.

          1. admin Post author

             >it seems like the medicine should
             >help, but there is a pressure surge

             I would suggest skipping the medication once and seeing how your blood pressure behaves in response. But in your case, this risks a heart attack or stroke. So I don’t recommend taking risks.

13. Catherine

    Hello, I am 35 years old, height 173, weight 97 kg. I am 13 weeks pregnant, I had stage 2 hypertension before pregnancy and now my blood pressure is rising to 150/100 due to medications. Today my pulse was 150, I was afraid that I might have a stroke or my heart would break. Can pregnant women take beta blockers? Gynecologists disagree.

14. Tatyana Iosifovna

    Dear doctor! I am 73 years old. I have had hypertension since I was 50. I had a mastectomy of the mammary gland 2 years ago. I am being monitored. There are no special complaints from oncology. Problems with blood vessels. In the morning the pressure is either low or normal. There is no tachycardia. Emergency - 65-70.
    I was prescribed Betaloc, Cardiomagnyl and Lazap Plus.
    The beta blocker should be taken in the morning. But with a heart rate of 60, I hesitate to take it. The pressure rises (to 170) in the second half of the day. At the same time, it is not always relieved by taking antihypertensive drugs, tachycardia develops (up to 95-98). To reduce pressure, I take another 15-20 mg of Physitenza before bed. The pressure normalizes, but the heart rate does not. There are feelings of constriction in the heart area.
    ECG: SR not excluded. c/o changes in the basal parts of the left ventricle.
    ECHO:LVH of the basal part of the IVS, type DD2. Chambers and valves are normal.
    Question: when is the best time to take beta blockers? They also lower blood pressure. I have a hard time with hypotension; Shortness of breath appears both when walking and lying down. In the morning I feel normal.
    P.S. my height is 164, weight is 78 kg. Sincerely, T.I.

15. Dmitriy

    Dear doctor, help me figure it out so I can understand exactly what is happening to me. City of Kiev, height 193, weight 116 kg, waist circumference 102 cm. In August 2013, there was a reason to call an ambulance, it all happened on Monday at lunchtime on the street (heat), sudden weakness, dizziness, fear of falling, then I felt panic, palpitations . They called an ambulance, my blood pressure was 140/100, my pulse was 190. They injected me with something and gave me anaprilin under my tongue and Corvalol. After this, I went to the doctors, took blood tests, the blood showed glucose 7.26, liver tests of ALT and AST were significantly elevated. They attributed it to the fact that there had been alcoholic libations before and subsequent poisoning. They did an ultrasound of the heart, a cardiogram, then a gastroscopy at the Shalimov Institute, an MRI (they found glaucoma, all other organs were OK), in general, almost all the tests. They told me to drink bisoprolol 5 mg every day. A diagnosis of stage 1 hypertension was made. They recommended a lifestyle change, diet, walking, giving up alcohol. I took bisoprolol for 2 months, the pressure stabilized immediately - it was always normal, then somewhere after 1.5 months bisoprolol began to lower the pressure 105-115/65-75, the dose was reduced. Then I felt great and had a cardiogram done on a cardio machine under different loads. The doctor said based on the results that there is nothing to complain about the heart, everything is OK, we are canceling bisoprolol. Bisoprolol was abruptly stopped; I took 2.5 mg for the last 2 weeks. And then it began - in almost two weeks, three attacks, heart rate jumps to 100 and above, with subsequent pressure jumps to 150/95. Knocked down and calmed down with Corvalol. Fears began that this might happen again. I turned to the same cardiologist - again bisoprolol 2.5 mg for the winter and consult a neurologist. The latter prescribed the anti-depressant Triticco, which was supposed to relieve fears, panic, etc. When they were taken together, the pressure in the cold remained stable at 118-124/65-85, and then the pressure dropped again to 105/60. The neurologist again abruptly stopped bisoprolol. The situation appeared again, twice in 4 days - incomprehensible anxiety, rapid pulse above 100, and probably blood pressure. I already knocked it down with Corvalol and anaprilin. After this, the fears resumed, the cardiologist advised Nebilet, which lowers the blood pressure less and keeps the pulse better than bisoprolol. Don’t quit Tritiko and finish it, and also, to somehow knock bad thoughts out of your head, take gedozepam. I don’t understand what to do next, where to go? Your site is very informative, but it’s difficult to find doctors even in Kyiv. They say that the problem is in my head, I create my own fears. Please advise, sometimes it seems to me that my doctors have no time for me. Age 45 years.

    Treatment of hypertension without drugs."

    1. Dmitriy

       Thank you very much for your answer. I did not write (missed) that after I was tested for the first time (which showed glucose 7.26), and this was 08.20.13, I stopped drinking alcohol, began taking bisoprolol, taking walks, and eating selectively. A week later, namely 08/28/13, I donated blood again at Shalimov’s clinic and my glucose showed 4.26. With this, I calmed down regarding sugar (the doctors attributed the cause of the crisis and high blood glucose to the fact that a week before there was severe alcohol poisoning at a birthday party). As I understand it, we urgently need to take all the tests again in the order that you recommend, and follow the recommendations on the website - diet, exercise, that’s 100%. What about my pulse jumps, panic attacks? Or do you think they are closely related to glucose? As of today, I have stopped taking my own antidepressant and am again taking bisoprolol instead of Nebilet. It is much easier on bisoprolol, although panic attacks appear during the day. What do you recommend doing about this? Is it possible to cope with panic attacks and stop bisoprolol after some time if it turns out that my glucose levels are okay?

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How to cure hypertension on your own
in 3 weeks, without expensive harmful drugs,
"starvation" diet and heavy physical training:
free step-by-step instructions.

Adrenaline and norepinephrine (catecholamines) are responsible for regulating the basic functions of the human body. When released, they affect hypersensitive nerve endings - adrenergic receptors, which are divided into subtypes: alpha and beta (2 subtypes).

B1-adrenergic receptor, when released in large quantities, increases the heart rate, accelerates the breakdown of glycogen, and also dilates the coronary arteries.

B2-adrenergic receptors relax the walls of blood vessels, reduce the tone of the uterus in women, and lead to an acceleration of the process of insulin secretion. Activation of both types of catecholamines the human body mobilizes all its forces to support life. Beta blockers are a special group of drugs that interfere with the effects of catecholamines on vital organs.

Mechanism of action

As stated, the use of beta blockers leads to a decrease in blood pressure and a decrease in heart rate. Patients experience prolongation of diastole - the time of rest of the heart muscle, during which the coronary vessels fill with blood.

Improving the filling of the coronary vessels (blood supply to the myocardium) is the reason for the decrease in intracardiac pressure.

Blood begins to circulate and be redistributed between normal and ischemic areas, and the person is able to more easily endure physical activity. Another undeniable advantage of beta blockers is they have unique antiarrhythmic properties. Their intake leads to suppression of the action of catecholamines and reduces the rate of accumulation of calcium ions in the body, which seriously impair energy metabolic operations in the myocardium.

Classification of drugs

β-blockers are a group of drugs. They are classified according to specific characteristics. For example, cardioselectivity or the ability of the chosen drug block the effects of only β1-adrenergic receptors.

The higher the selectivity of beta-blockers, the safer they are for use by patients with respiratory tract diseases and diabetes.

However, the concept of selectivity is an abstract indicator, because when taking drugs in large quantities, the degree of the indicator decreases. There is a category of drugs with sympathomimetic activity: they additionally stimulate the effects of beta blockers and can lead to a slowdown in heart rate and can negatively affect lipid metabolism in the body.

The classification includes drugs with vasodilating properties to dilate blood vessels. The process can be controlled by direct action of α-blockers on the walls of blood vessels.

Indications and absolute contraindications for use

Indications for the use of beta-blockers depend entirely on their properties. Non-selective blockers have a limited range of uses, while selective drugs can be used in a wide range of patients. May be prescribed for:

1. Arterial hypertension;
2. Migraine;
3. Heart failure;
4. Marfan syndrome;
5. Migraine;
6. Glaucoma;
7. Aortic aneurysm;
8. at any stage;
9. Chronic heart failure;
10. Sinus tachyarrhythmia.

In the records of cardiologists and cardiac surgeons who prescribe appropriate treatment for their patients, you can often see second and third generation drugs that are ideal for treating blood vessels and the heart.

In the presence of the following diseases and abnormalities, there is an absolute prohibition (contraindication) for the use of β-blockers:

1. Pregnancy, childhood;
2. Bronchial asthma;
3. Second degree heart block;
4. Weakness of the sinus node;
5. Decompensation of heart failure.

I generation – non-cardioselective

Non-cardioselective adrenergic blockers are the first representatives of this group of drugs. Due to blocking of receptors of the first and second types may cause side effects– bronchospasms.

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

The list of drugs includes:

• Carteolol;
• Adprenolol;
• Labetalol;
• Pindolol;
• Dilevalol;
• Bucindolol.

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

II generation – cardioselective

Second generation drugs block type 1 receptors, which are located in the heart. Can be used by patients who have a high likelihood of developing side effects due to lung diseases ( this is due to the fact that they do not affectβ -2-adrenergic blockers in the lungs).

Cardioselective beta-blockers of the second generation are prescribed to patients with atrial fibrillation or.

With intrinsic sympathomimetic activity

• Celiprolol;
• Talinolol;
• Acekor;
• Epanolol.

No intrinsic sympathomimetic activity

• Betaxolol;
• Esmolol;
• Bisoprolol;
• Nebivolol;
• Atenolol.

III generation (with vasodilating features)

The features of third-generation drugs are their special pharmacological effects: they block both beta and alpha receptors in blood vessels. Let's take a closer look at existing groups.

Non-cardioselective

Promote relaxation of the walls of blood vessels due to the simultaneous effect on beta-1 and beta-2 adrenergic blockers. These include:

• Dilevalol;
• Amozulalol;
• Nipradilol;
• Labetalol.

Cardioselective

Serve to increase the volume of nitric oxide released to dilate the blood vessels of the heart and reduce the likelihood of blood vessel blockage(atherosclerotic plaques). The new generation of drugs includes:

• Nebivolol;
• Carvedilol;
• Celiprolol.

Duration of action

All β-blockers are divided into two main groups: long-acting and short-acting. The duration is affected by the biochemical composition of the drug.

Long-acting drugs

1. Amphiphilic– soluble in fats and water (for example, Acebutolol and Biseprolol). Excreted from the body by hepatic metabolism or renal excretion.
2. Hydrophilic (Atenolol)– they are processed in water, but are not absorbed in the liver.
3. Short-acting lipophilic– dissolves in fats, is well absorbed by the liver, and acts for a short period of time.
4. Long acting lipophilic.

Ultra-short-acting drugs

Most often, such beta blockers are given in the form of droppers. The duration of exposure to the body does not exceed 30 minutes, after which all biochemical substances begin to break down in the human blood.

They are actively used in patients with hypotension and heart failure, since they do not cause side effects. The main representative of this group of drugs is Esmolol.

Side effects

Please note that taking these medications must be strictly supervised by your doctor!

In a separate group of people side effects may occur, which are expressed in:

• hair loss;
• heart rhythm disturbance;
• sleep disturbance and depression;
• memory impairment;
• sexual dysfunction;
• allergic reactions.

The use of adrenergic blockers for prostatitis

Beta blockers are widely used in urology for the treatment of prostatitis. Contains terazosin and silodosin improve the urination process in people experiencing problems.

Prescribed for prostatitis or the following problems:

• weak bladder tone;
• low pressure in the urethra;
• BPH;
• relaxed state of the prostate muscles.

Positive results from taking adrenergic blockers in these cases are visible within a few weeks. The list of drugs includes: Glansin, Omsulosin and Focusin.

You should not self-medicate - we strongly advise you to consult your doctor so as not to aggravate the course of the disease.

Irina Zakharova

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

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

• Alpha 1, alpha 2.
• Beta 1, beta 2.

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

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

• alpha-blockers;
• beta blockers.

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

Alpha blockers

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

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

• Doxazosin.
• Terazosin.
• Prazonin.

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

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

Flaw

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

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

Mechanism of action and contraindications

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

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

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

Side effects

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

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

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

Doxazosin

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

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

Terazosin

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

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

Prazonin

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

• arteries;
• venous vessels.

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

Beta blockers

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

The substances included in the composition block the negative effect on the heart muscle:

• lower blood pressure;
• improve general condition.

By giving preference to such medications, you can not be afraid of hypertensive crises and stroke.

Kinds

The list of medications for hypertension is wide. It includes selective and non-selective drugs. Selectivity is a selective influence on only one type of receptor (beta 1 or beta 2). Non-selective agents affect both types of beta receptors simultaneously.

When taking beta blockers, patients experience the following symptoms:

• heart rate decreases;
• pressure decreases noticeably;
• the tone of blood vessels becomes better;
• the formation of blood clots slows down;
• body tissues are better supplied with oxygen.

In practice, beta-blockers are widely used to treat patients with arterial hypertension. Cardioselective and non-cardioselective blockers can be prescribed.

List of cardioselective beta blockers

Let's look at a description of several of the most popular medications. They can be purchased without a prescription at the pharmacy, but self-medication can lead to serious consequences. Taking beta blockers is possible only after consulting a doctor.

List of cardioselective drugs:

• Atenolol.
• Metoprolol.
• Acebutolol.
• Nebivolol.

Atenolol

Long-acting drug. At the initial stage, the dosage rate per day is 50 mg, after some time it can be increased, the maximum daily dose is 200 mg. An hour after taking the drug, the patient begins to feel the therapeutic effect.

The therapeutic effect lasts throughout the day (24 hours). After two weeks, you must visit a doctor to assess the effectiveness of drug treatment. The blood pressure should normalize by the end of this period. Atenolol is available in the form of 100 mg tablets, packaged in jars of 30 pieces or in blister packs of 10 pieces.

Metoprolol

When taking Metoprolol, a rapid decrease in blood pressure occurs, the effect occurs after 15 minutes. The duration of the therapeutic effect is short - 6 hours. The doctor prescribes a frequency of doses from 1 to 2 times a day, 50–100 mg at a time. You can consume no more than 400 mg of Metoprolol per day.

The product is available in the form of 100 mg tablets. In addition to the active ingredient metoprolol, they include auxiliary substances:

• lactose monohydrate;
• cellulose;
• magnesium stearate;
• povidone;
• potato starch.

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

Acebutolol

The daily dose of Acebutolol is 400 mg. Take it 2 times. During treatment, the doctor may increase the dosage per day to 1200 mg. The greatest therapeutic effect is felt by patients who, along with high blood pressure, are diagnosed with ventricular arrhythmia.

The medicine is available in two forms:

• 0.5% solution for injection in 5 ml ampoules;
• tablets weighing 200 or 400 mg.

Acebutolol is excreted from the body through the kidneys and gastrointestinal tract 12 hours after administration. The active substance may be contained in breast milk. This must be taken into account by breastfeeding women.

Nebivolol

You can evaluate the effect of the drug 2 weeks after starting treatment. In addition to lowering blood pressure, the medicine has an antiarrhythmic effect. By the end of the fourth week of treatment, the patient’s blood pressure should be established, and by the end of 2 months of the course of treatment it should become stable.

Nebivolol is produced in the form of tablets, packaged in cardboard boxes. The active substance is nebivolol hydrochloride. Its elimination from the body depends on the person’s metabolism; the higher the metabolism, the faster it is eliminated. Excretion occurs through the gastrointestinal tract and kidneys.

The daily norm for an adult is from 2 to 5 mg per day. After the patient adapts to the drug, the daily dose can be increased to 100 mg. The greatest effect is achieved by taking the drug at the same time.

Non-cardioselective drugs

The group of non-cardioselective blood pressure drugs includes the following beta-blockers:

• Pindolol.
• Timolol.
• Propranolol.

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

Timolol for the treatment of hypertension is prescribed at a dose of 10 mg twice a day. If there is a need for health reasons, the daily dose is increased to 40 mg.

Beta blockers should be discontinued under the supervision of a physician. The patient's blood pressure may rise sharply. If the patient refuses to take it, a gradual reduction in the daily dose is recommended over the course of a month.

The effect of adrenaline and norepinephrine on beta-adrenergic receptors in diseases of the heart and blood vessels can lead to fatal consequences. In this situation, medications grouped as beta-blockers (BABs) not only make life easier, but also prolong it. Studying the topic of BAB will teach you to better understand your body when getting rid of an illness.

What are beta blockers

Adrenergic blockers (adrenolytics) are understood as a group of drugs with a common pharmacological effect - neutralization of adrenaline receptors of blood vessels and the heart. Medicines “turn off” the receptors that respond to adrenaline and norepinephrine and block the following actions:

• sharp narrowing of the lumen of blood vessels;
• increased blood pressure;
• antiallergic effect;
• bronchodilator activity (expansion of the lumen of the bronchi);
• increased blood glucose levels (hypoglycemic effect).

The drugs affect β2-adrenergic receptors and β1-adrenergic receptors, causing the opposite effect of adrenaline and norepinephrine. They dilate blood vessels, lower blood pressure, narrow the lumen of the bronchi and reduce blood sugar levels. When beta1-adrenergic receptors are activated, the frequency and strength of heart contractions increase, and the coronary arteries dilate.

Due to the effect on β1-adrenergic receptors, cardiac conductivity improves, the breakdown of glycogen in the liver and energy production are enhanced. When beta2-adrenergic receptors are excited, the walls of blood vessels and the muscles of the bronchi relax, insulin synthesis and the breakdown of fat in the liver are accelerated. Stimulation of beta-adrenergic receptors with catecholamines mobilizes all the forces of the body.

Drugs from the group of beta-adrenergic receptor blockers reduce the frequency and strength of heart contractions, lower blood pressure, and reduce oxygen consumption by the heart. The mechanism of action of beta-blockers (BAB) is associated with the following functions:

1. Diastole lengthens - due to improved coronary perfusion, intracardiac diastolic pressure decreases.
2. Blood flow is redistributed from normally supplied areas to ischemic areas, which increases exercise tolerance.
3. The antiarrhythmic effect consists of suppressing arrhythmogenic and cardiotoxic effects, preventing the accumulation of calcium ions in the heart cells, which can worsen energy metabolism in the myocardium.

Medicinal properties

Non-selective and cardioselective beta-blockers are capable of inhibiting one or more receptors. They have opposite vasoconstrictor, hypertensive, antiallergic, bronchodilator and hyperglycemic effects. When adrenaline binds to adrenergic receptors under the influence of adrenergic blockers, stimulation occurs and sympathomimetic internal activity increases. Depending on the type of beta blockers, their properties are distinguished:

1. Non-selective beta-1,2-blockers: reduce peripheral vascular resistance and myocardial contractility. Due to the drugs of this group, arrhythmia is prevented, the production of renin by the kidneys and blood pressure are reduced. At the initial stages of treatment, vascular tone increases, but then it decreases to normal. Beta-1,2-adrenergic blockers inhibit the aggregation of platelets, the formation of blood clots, enhance the contraction of the myometrium, and activate the motility of the digestive tract. In case of coronary heart disease, adrenergic receptor blockers improve exercise tolerance. In women, non-selective beta blockers increase uterine contractility, reduce blood loss during childbirth or after surgery, and lower intraocular pressure, which allows them to be used for glaucoma.
2. Selective (cardioselective) beta1-blockers - reduce the automaticity of the sinus node, reduce the excitability and contractility of the heart muscle. They reduce myocardial oxygen demand and suppress the effects of norepinephrine and adrenaline under stress conditions. Due to this, orthostatic tachycardia is prevented and mortality in heart failure is reduced. This improves the quality of life of people with ischemia, dilated cardiomyopathy, after a stroke or heart attack. Beta1-blockers eliminate the narrowing of the lumen of the capillaries, in case of bronchial asthma they reduce the risk of developing bronchospasm, in case of diabetes mellitus they eliminate the risk of developing hypoglycemia.
3. Alpha and beta adrenergic blockers - reduce cholesterol and triglyceride levels, normalize lipid profile parameters. Due to this, blood vessels dilate, afterload on the heart decreases, and renal blood flow does not change. Alpha-beta blockers improve myocardial contractility and help blood not remain in the left ventricle after contraction, but completely pass into the aorta. This leads to a reduction in the size of the heart and a decrease in the degree of its deformation. In heart failure, drugs reduce attacks of ischemia, normalize cardiac index, and reduce mortality in ischemic disease or dilated cardiomyopathy.

Classification

To understand the principle of operation of drugs, the classification of beta-blockers is useful. They are divided into non-selective and selective. Each group is divided into two more subtypes - with or without internal sympathomimetic activity. Thanks to such a complex classification, doctors have no doubt about choosing the optimal medication for a particular patient.

Based on the predominant effect on beta-1 and beta-2 adrenergic receptors

Based on the type of effect on the types of receptors, selective beta-blockers and non-selective beta-blockers are distinguished. The former act only on cardiac receptors, which is why they are also called cardioselective. Non-selective drugs affect any receptors. Non-selective beta-1,2-blockers include Bopindolol, Methipranolol, Oxprenol, Sotalol, Timolol. Selective beta-1 blockers are Bisoprolol, Metoprolol, Atenolol, Tilinolol, Esmolol. Alpha-beta blockers include Proxodalol, Carvedilol, Labetalol.

According to its ability to dissolve in lipids or water

Beta-blockers are divided into lipophilic, hydrophilic, lipohydrophilic. Fat-soluble are Metoprolol, Propranolol, Pindolol, Oxprenol, hydrophilic are Atenolol, Nadolol. Lipophilic drugs are well absorbed from the gastrointestinal tract and metabolized by the liver. In case of renal failure, they do not accumulate and therefore undergo biotransformation. Lipohydrophilic or amphophilic drugs contain Acebutalol, Bisoprolol, Pindolol, Celiprolol.

Hydrophilic beta-adrenergic receptor blockers are less well absorbed in the digestive tract, have a long half-life, and are excreted by the kidneys. They are preferably used in patients with liver failure because they are eliminated by the kidneys.

By generation

Among beta-blockers, medications of the first, second and third generations are distinguished. There are more benefits from modern drugs, their effectiveness is higher, and there are fewer harmful side effects. First generation drugs include Propranolol (part of Anaprilin), Timolol, Pindolol, Sotalol, Alprenol. Second generation drugs - Atenolol, Bisoprolol (part of Concor), Metoprolol, Betaxolol (Locren tablets).

Third-generation beta blockers additionally have a vasodilating effect (relax blood vessels), these include Nebivolol, Carvedilol, Labetalol. The first increases the production of nitric oxide, which regulates vascular relaxation. Carvedilol additionally blocks alpha adrenergic receptors and increases the production of nitric oxide, while Labetalol acts on both alpha and beta adrenergic receptors.

List of beta blockers

Only a doctor can choose the right drug. He also prescribes the dosage and frequency of taking the medicine. List of known beta blockers:

1. Selective beta blockers

These drugs act selectively on receptors of the heart and blood vessels, therefore they are used only in cardiology.

1.1 Without intrinsic sympathomimetic activity

1.2 With intrinsic sympathomimetic activity

These medications do not have a selective effect; they lower blood and intraocular pressure.

2.1 Without intrinsic sympathomimetic activity

2.2 With intrinsic sympathomimetic activity

3. Beta blockers with vasodilating properties

To solve problems of high blood pressure, adrenergic receptor blockers with vasodilating properties are used. They constrict blood vessels and normalize heart function.

3.1 No intrinsic sympathomimetic activity

3.2 With intrinsic sympathomimetic activity

4. Long-acting beta blockers

Lipophilic beta-blockers - long-acting drugs last longer than their antihypertensive counterparts, and are therefore prescribed in lower dosages and with reduced frequency. These include metoprolol, which is contained in the tablets Egilok Retard, Corvitol, Emzok.

5. Ultra-short-acting adrenergic blockers

Cardioselective beta-blockers are ultra-short-acting drugs with a working time of up to half an hour. These include esmolol, which is contained in Breviblok, Esmolol.

Indications for use

There are a number of pathological conditions that can be treated with beta-blockers. The decision to prescribe is made by the attending physician based on the following diagnoses:

1. Angina pectoris and sinus tachycardia. Often, beta-blockers are the most effective treatment for preventing attacks and treating angina pectoris. The active substance accumulates in the tissues of the body, providing support to the heart muscle, which reduces the risk of recurrent myocardial infarction. The ability of the drug to accumulate allows you to temporarily reduce the dose. The feasibility of taking beta blockers for exertional angina increases with the simultaneous presence of sinus tachycardia.
2. Myocardial infarction. The use of beta blockers for myocardial infarction leads to limitation of the necrosis sector of the heart muscle. This leads to a reduction in mortality, and the risk of cardiac arrest and recurrent myocardial infarction is reduced. It is recommended to use cardioselective agents. It is permissible to begin use immediately upon the patient’s admission to the hospital. Duration – 1 year after myocardial infarction.
3. Heart failure. The prospects for using beta blockers for the treatment of heart failure are still under study. Currently, cardiologists allow the use of drugs if this diagnosis is combined with angina pectoris, arterial hypertension, arrhythmia, or a tachysystological form of atrial fibrillation.
4. Arterial hypertension. Young people leading an active lifestyle often experience arterial hypertension. In these cases, beta blockers may be prescribed as prescribed by a doctor. An additional indication for use is the combination of the main diagnosis (hypertension) with rhythm disturbances, angina pectoris and after myocardial infarction. The development of hypertension into hypertension with left ventricular hypertrophy is the basis for taking beta blockers.
5. Heart rhythm abnormalities include disorders such as supraventricular arrhythmias, atrial flutter and fibrillation, and sinus tachycardia. To treat these conditions, drugs from the group of beta blockers have been successfully used. A less pronounced effect is observed in the treatment of ventricular arrhythmias. In combination with potassium drugs, beta blockers are successfully used for the treatment of arrhythmias caused by glycoside intoxication.

Features of use and rules of administration

When a doctor decides to prescribe beta-blockers, the patient must inform the doctor about the presence of diagnoses such as emphysema, bradycardia, asthma and arrhythmia. An important circumstance is pregnancy or suspicion of it. BABs are taken simultaneously with food or immediately after the end of the meal, as food reduces the severity of the side effect. The dosage, regimen and duration of therapy are determined by the treating cardiologist.

During treatment, it is recommended to carefully monitor your pulse. If the frequency decreases below the established level (determined when prescribing a treatment regimen), you must inform your doctor about this. In addition, observation by a doctor during the course of taking medications is a condition for the effectiveness of therapy (a specialist, depending on individual indicators, can adjust the dosage). You cannot stop taking beta blockers on your own, otherwise the side effects will be aggravated.

The peculiarities of the impact of biologically active substances on the human body can lead to a number of side effects of varying severity. Patients may experience the following:

• insomnia;
• weakness;
• headache;
• breathing problems;
• exacerbation of ischemic heart disease;
• intestinal disorder;
• mitral valve prolapse;
• dizziness;
• depression;
• drowsiness;
• fatigue;
• hallucinations;
• nightmares;
• slower reaction;
• anxiety;
• conjunctivitis;
• noise in ears;
• convulsions;
• Raynaud's phenomenon (pathology);
• bradycardia;
• psychoemotional disorders;
• inhibition of bone marrow hematopoiesis;
• heart failure;
• heartbeat;
• hypotension;
• atrioventricular block;
• vasculitis;
• agranulocytosis;
• thrombocytopenia;
• muscle and joint pain
• chest pain;
• nausea and vomiting;
• liver dysfunction;
• abdominal pain;
• flatulence;
• spasm of the larynx or bronchi;
• dyspnea;
• skin allergies (itching, redness, rash);
• cold extremities;
• sweating;
• baldness;
• muscle weakness;
• decreased libido;
• decrease or increase in enzyme activity, blood glucose and bilirubin levels;
• Peyronie's disease.

Withdrawal syndrome and how to avoid it

With long-term treatment with high dosages of beta blockers, a sudden stop of therapy can cause withdrawal syndrome. Severe symptoms manifest themselves in the form of ventricular arrhythmias, angina attacks and myocardial infarction. Mild consequences are expressed in the form of increased blood pressure and tachycardia. Withdrawal syndrome develops several days after the course of therapy. To eliminate this outcome, you must follow the rules:

1. It is necessary to stop taking beta blockers slowly, for 2 weeks, gradually reducing the dose of the next dose.
2. During gradual withdrawal and after complete cessation of use, it is important to sharply reduce physical activity and increase the intake of nitrates (in consultation with the doctor) and other antianginal agents. During this period, it is important to limit the use of blood pressure lowering medications.

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