Beta-blockers - list of drugs, destination, contraindications

Beta-blockers - a class of drugs used in diseases of the cardiovascular system( hypertension, angina pectoris, myocardial infarction, cardiac rhythm disturbance and chronic heart failure) and others. At present, beta-blockers are accepted by millions of people around the world. The developer of this group of pharmacological agents has revolutionized the therapy of heart disease. In modern practical medicine beta-blockers have been used for several decades.

• Purpose
• Indications
• I Generation - a non-cardioselective
• With intrinsic sympathomimetic
• activity without intrinsic sympathomimetic activity
• II Generation - cardioselective
• With intrinsic sympathomimetic
• activity without intrinsic sympathomimetic activity
• III generation - with vasodilating properties
• non-cardioselective
• cardioselective
• Byduration of action
• Prolonged action
• NecardiosLecture
• Cardioselective
• Ultra-short action
• Contraindications
• Adverse effects

Intended

Adrenaline and other catecholamines play an indispensable role in the vital activity of the human body. They are secreted into the bloodstream and affect the sensitive nerve endings - adrenoreceptors located in tissues and organs. And they, in turn, are divided into 2 types: beta-1 and beta-2-adrenergic receptors.

Beta-blockers block beta-1-adrenergic receptors, establishing the protection of the heart muscle from the effects of catecholamines. As a result, the frequency of contractions of the heart muscle decreases, the risk of an attack of angina and violations of the heart rhythm decreases.

Beta-blockers reduce blood pressure by using several mechanisms of action:

• blockade of beta-1 receptors;
• central nervous system depression;
• decreased sympathetic tone;
• a decrease in renin level in the blood and a decrease in its secretion;
• decrease in heart rate and rate;
• decreased cardiac output.

Beta-2-adrenoceptors are blocked together with beta-1, which leads to negative side effects from the use of beta-blockers. Therefore, each drug of this group is given the so-called selectivity - the ability to block beta-1-adrenergic receptors, without interfering in any way with beta-2-adrenergic receptors. The higher the selectivity of the drug, the more effective its therapeutic effect.

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Indications

The list of indications of beta-blockers includes:

• infarction and post-infarction;
• angina;
• heart failure;
• high blood pressure;
• hypertrophic cardiomyopathy;
• problems with heart rhythm;
• essential tremor;
• Marfan syndrome;
• migraine, glaucoma, anxiety and other diseases that are not cardiac in nature.

Beta-blockers are very easy to recognize among other drugs by name with a characteristic ending "lol".All preparations of this group have differences in the mechanisms of action on receptors and adverse events. According to the basic classification, beta-blockers are divided into 3 main groups.

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Generation I - noncardioselective

First generation drugs - noncardioselective adrenoblockers - are among the earliest representatives of such a group of medicines. They block the receptors of the first and second types, thus providing both a therapeutic and side effect( can lead to bronchospasm).

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With internal sympathomimetic activity

Some beta-blockers have the ability to partially stimulate beta-adrenergic receptors. This property is called internal sympathomimetic activity. Such beta-blockers to a lesser extent slow down the rhythm of the heart and the strength of its contractions, have a less negative effect on lipid metabolism and do not often lead to the development of withdrawal syndrome.

For first-generation drugs with intrinsic sympathomimetic activity are:

• Alprenolol ( Aptin);
• Bucindolol ;
• Labetalol ;
• Oxprenolol ( Trazicore);
• Penbutolol ( Betasprin, Levatol);
• Dilevalol ;
• Pindolol ( Vicin);
• Bopindolol ( Sandonorm);
• Carotenol.

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Without internal sympathomimetic activity

• Nadolol ( Korgard);
• Timolol ( Blokarden);
• Propranolol ( Obsidan, Anaprilin);
• Sotalol ( Sotagexal, Tenzol);
• Flestrolol ;
• NEPRADILOL .
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Generation II - cardioselective

Second generation drugs block predominantly the first type of receptors, the bulk of which are localized in the heart. Therefore, cardioselective beta-blockers have fewer side effects and are safe in the occurrence of concomitant pulmonary diseases. Their activity does not affect beta-2-adrenergic receptors located in the lungs.

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With internal sympathomimetic activity of

• Talinolol ( Cordanum);
• Acebutalol ( Sectral, Acecor);
• Epanolol ( Vasacor);
• Celiprolol .

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No internal sympathomimetic activity of

• Atenolol ( Betacard, Tenormin);
• Esmolol ( Brevibrok);
• Metoprolol ( Serdol, Methocol, Metocard, Egilok, Metozok, Corvitol, Betalococcus, Betaloc);
• Bisoprolol ( Coronale, Cordinorm, Tyrez, Niperten, Corbis, Concor, Bisomor, Bisogamma, Biprol, Biol, Bidop, Aritel);
• Betaxolol ( Kerlon, Lokren, Betak);
• Nebivolol ( Nebilong, Nebilet, Nebilan, Nebikor, Nebivator, Binelol, Od-neb, Nevotenz);
• Carvedilol ( Talliton, Recardium, Coriol, Carvenal, Carvedigamma, Dilatrend, Vedicardol, Bagodolol, Acridilol);
• Betaxolol ( Keerlon, Lokren, Betak).

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Generation III - with vasodilating properties of

Beta-blockers of the third generation have additional pharmacological properties, as they block not only the beta receptors, but also the alpha receptors found in the blood vessels.

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Non-cardioselective

Non-selective beta blockers of the new generation are drugs that equally affect beta-1 and beta-2-adrenergic receptors and promote the relaxation of blood vessels.

• Pindolol;
• Nipradilol;
• Medrosalol;
• Labetalol;
• Dilevalol;
• Bucindolol;
• Amozulalol.

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Cardioselective

Cardioselective drugs of the third generation contribute to increased nitric oxide excretion, which causes vasodilation and a reduced risk of atherosclerotic plaques. To a new generation of cardioselective adrenoblockers are:

• Carvedilol;
• Celiprolol;
• Nebivolol.

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For the duration of the action of

In addition, beta-blockers are classified by duration of action on long-acting and ultra-short-acting drugs. Most often, the duration of the therapeutic effect depends on the biochemical composition of beta-blockers.

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Long-acting

Long-acting drugs are divided into:

• Lipophilic short-acting - wellare dissolved in fats, the liver actively participates in their processing, they act for several hours. They better overcome the barrier between the circulatory and nervous system( Propranolol );
• Lipophilic long-acting( Retard, Metoprolol ).
• Hydrophilic - soluble in water and not processed in the liver( Atenolol ).
• Amphiphilic - have the ability to dissolve in water and in fats( Bisoprolol, Celiprolol, Acebutolol ), has two ways of excretion from the body( renal excretion and hepatic metabolism).

Long-acting drugs differ in the mechanisms of action on adrenergic receptors and are divided into cardioselective and noncardioselective.

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Non-cardioselective

• Sotalol;
• Penbutolol;
• Nadolol;
• BOPINDOLOL.

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Cardioselective

• Epanolol;
• Bisoprolol;
• Betaxolol;
• Atenolol.

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Ultra-short action

Beta-blockers of ultrashort action are used only for droppers. The beneficial substances of the drug are destroyed by the action of blood enzymes and stop after 30 minutes after the end of the procedure.

Short-term action makes the drug less dangerous with concomitant diseases - hypotension and heart failure, and cardioselectivity - with bronchoobstructive syndrome. Representative of this group is substance Esmolol .

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Contraindications

Beta-blockers are absolutely contraindicated for:

• pulmonary edema;
• cardiogenic shock;
• severe form of heart failure;
• bradycardia;
• of chronic obstructive pulmonary disease;
• bronchial asthma;
• 2 degrees of atrioventricular blockade of the heart;
• hypotension( lowering blood pressure by more than 20% of normal performance);
• by uncontrolled insulin-dependent diabetes mellitus;
• Reynaud syndrome;
• atherosclerosis of peripheral arteries;
• manifestations of allergies to the drug;
• pregnancy, as well as in childhood.

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Side effects of

The use of such drugs should be treated very seriously and carefully, because in addition to the therapeutic effect, they have the following side effects.

• Overwork, sleep disorders, depression;
• Headache, dizziness;
• Memory impairment;
• Rash, itching, psoriasis symptoms;
• Hair loss;
• Stomatitis;
• Poor physical tolerance, rapid fatigue;
• Deterioration of the course of allergic reactions;
• Heart rate imbalance - decreased heart rate;
• Cardiac blockade, provoked by a violation of the conduction function of the heart;
• Reducing blood sugar;
• Reducing cholesterol in the blood;
• Exacerbation of respiratory system diseases and bronchospasm;
• The onset of a heart attack;
• Risk of sudden increase in pressure after discontinuation of medication;
• Appearance of sexual dysfunction.