Beta-blockers zastosovuetsya when. List of drugs for beta-blockers and their zastosuvannya. Selective and non-selective features

The intake of beta-blockers can cause hypotension - an epidemiological decrease in blood pressure, as well as bradycardia - a change in the frequency of the heart rate. The patient should immediately turn around for medical assistance so the systolic pressure will be less than 100 mm Hg, and the pulse will be less than 50 beats per whilin. Do not take blockers beta pid hour of vaginess, shards of stench can lead to a constricted fetal growth.

Beta-blockers may have numerous side effects. The axis of the most serious of them.

  • It was suggested that: it may be the result of a change in blood flow to the brain with a decrease in blood pressure.
  • Upovilnennya heart rate: a sign of global weakness.
  • Heart blockade: if the heart conduction system is damaged, taking beta-blockers can lead to heart failure.
  • Intolerance to physical challenges: not shortest choice drug for the active athlete.
  • Acute asthma: preparations of this group can make the sick bronchial asthma.
  • Decrease in the level of LDL-cholesterol or lipid levels in the blood: beta-blockers reduce the level of "good" cholesterol.
  • Toxicity: in case of liver disease or deficiency of beta-blockers, beta-blockers can accumulate in the body, stinks are excreted from it through the liver, or else.
  • Imovirnіst podvischennya krov'yannya vise at times when taking the drug: just stop taking the drug, the bloody vise can go higher, lower to the cob of lukewarmness. Qi preparations should be drunk step by step by stretching kіlkoh tizhnіv.
  • Decreased blood glucose levels: in diabetics who take drugs from these groups, there may be a decreased reaction to low blood glucose levels, hormone levels that increase blood glucose levels, lie in nerves, and be blocked by beta-blockers.
  • The most safe side effect of taking beta-blockers: heart attack. Take beta-blockers as needed step by step to get rid of the pain in the heart and heart attacks.

Be especially careful when you get beta-blockers:

  • Blood diabetes (especially sickness, if you take insulin);
  • Chronic obstructive disease of the leg without bronchial obstruction;
  • Peripheral artery lesions with little or no culling that interspersed;
  • depression;
  • Dyslipidemia (problems with blood cholesterol and triglyceride levels);
  • Asymptomatic dysfunction of the sinus node, atrioventricular blockade of the 1st stage.

When these camps follow:

  • choose cardioselective beta-blockers;
  • start at an even lower dose;
  • move її smoothly, lower sound;
  • for patients with diabetes mellitus - strictly control the level of glucose in the blood.

Absolute contraindications to beta-blockers:

  • Individual hypersensitivity;
  • Bronchial asthma and chronic obstructive disease of the lungs with bronchial obstruction (otherwise, it may cause congestion of bronchodilators);
  • Atrioventricular blockade 2-3 degree due to the presence of piece water to the rhythm;
  • Bradycardia with clinical manifestations;
  • Syndrome of weakness of the sinus node;
  • cardiogenic shock;
  • Severe damage to peripheral arteries;
  • Decreased arterial pressure due to clinical manifestations.

Go to the introduction of beta-blockers

Незалежно від фармакологічних особливостей бета-блокаторів (наявність або відсутність кардіоселективності, внутрішньої симпатоміметичної активності та ін.), їх різке скасування після тривалого застосування (або значне зменшення дозування) підвищують ризик розвитку гострих серцево-судинних ускладнень, які називаються «синдром відміни» синдром рикошету ".

This syndrome of beta-blockers in the case of hypertension can be manifested by an increase in the numbers of arterial pressure right up to the development of a hypertensive crisis. In patients with angina pectoris - often and/or increased intensity of angina episodes and, more likely, - a development of acute coronary syndrome. For those who suffer from heart failure, it is a sign of decompensation, or an increasing sign.

Lowering the dose or externally applying beta-blockers in times of need should be carried out step by step (for a few days or more days), and more closely monitoring the patient's self-esteem and blood tests. Even though it is still necessary to apply a beta-blocker, it is necessary to organize and implement an offensive set of approaches to reduce the risk of crises:

  • the patient may be subject to medical control;
  • to the ailing person as soon as possible physical and emotional excitement;
  • start accepting supplements from other groups (or increase their dosing) to intimidate a possible injury.

In case of hypertension, slid vicoristovuvat іnshi class likіv, yakі reduce the pressure. At ischemic disease heart - nitrate okremo chi together with calcium antagonists. In heart failure patients, instead of beta-blockers, diuretics and ACE inhibitors are prescribed.

Headlines about beta-blockers and their power: ““.

The side effects of all beta-blockers are very similar, but in different drugs from the stink group they vary according to the level of virulence. Report div. articles about specific drugs and beta-blockers.

  1. Raisa

    I suffer from hypertension for about 6 years. I take deltiazem 2 times a day, concor evenings and nifedipine as needed. I would like to switch to the drug 24 years old. Suggest, which drug should be changed.

  2. Olga

    chi obov'yazkovo in case of neurosis take blockers

  3. GANNA

    Hello! Sinu 36 years, supra-world vaga, rise and diastolic 140/100 liquor, prescribing preparations: lozap, concor, enap, diraton. The drug did not give a clear result. Nirks are normal. Tell me, why is there a high diastolic pressure and what kind of analysis is required to build?

  4. Alina

    I have a neurosis of the heart due to the illness of a child with cerebral palsy. Meni 54 rocks. I'm also afraid of falling ill, even if I'm healthy forever. What year were the panic attacks from strong haircuts vise. Uzі heart of kindness, only broken diastol function. And so everything is harazd, yet another blockade in front of her of the left leg of the PG and NBPNPG. I took a course at the neurological department. I drank coronal for 2 months at 1.25. Mexidol and MagneB6. I want to switch to supplements. your thought

  5. Boris

    Dyakuyu for your work! May God bless you.
    Please be kind about my problem.
    Meni 45 years. Skinny, swedish, virile, never knowing health problems, wanting not to play sports for a long time. Vletka perezhdzhzhav on p'yaty over - pulling a lot of furniture in the corner and downstairs. Unexpectedly, an arrhythmia appeared. Lie down, calmed down. And in the autumn of one day she showed up early and to the point of insult - huffing. Medicines were corrected to medicine - tachycardia. Trohi strebnuv vise, hoch zavzhd buv at the norm. They pricked the potassium-magnesium urticaria and started giving carvedol. Ultrasound of the heart showed insufficiency of the mitral valve, a subsided stool.
    Carvediol, as if not worthy of me - I didn’t wake up sometimes before going to bed. The cardiologist prescribed calcium (blocker?) for 10 days and nothing more.
    I spent time with a private cardiologist. She got it on the computer, knew a bunch of other ailments, and said to her heart: if you don’t have a valve, you can live to old age.
    Prescribed BADI. Tsiliy complex of subsequent rejoicing. And if you become arrhythmia, then she prescribed: Coenzyme Q10 + a large number of minerals. Axis i has become nourishing in me.
    As if the weather “smikaetsya” heart, especially at night, then I sleep badly, boasting.
    Can you drink magnesium 6 at the same time with dietary supplements? I'm so aware that magnesium is to blame for helping a lot with arrhythmias and valve problems?
    Chi not zavazhayut stench alone alone?
    At once I drink 20 days of chlorophyll and a coloid for purification. Let's sweat for a month for another BADI. Be there and Q10 - for a long time. Bude there and Omega3 - for a long time. But while I reach them, the doctor said: the organism is deluded, and the stench cannot be repaired again, it is necessary to be cleansed by others.
    And I think, while I am being cleansed, will my heart suffer? From i guess, magnesium drink. Chi right? Chi can one hour? Nirki Garazd.

    1. admin Post author

      > Fleshed out on the computer,
      > the doctor said: the organism is deluded
      > p'yu 20 days
      > you need to cleanse yourself

      I respect what you have done to a charlatan

      > Can you drink magnesium-B6 together with dietary supplements?

      So, and start shvidshe. You can type the DEPARTMENT of a colloidal slab.
      Mite on the uvazi, scho it was rotten for the human body, read from Wikipedia. True, it’s better for everything, in additions, like they sold you, there’s not a single thing and it’s close :).

      > Ultrasound of the heart showed
      > mitral valve insufficiency

      It is vital for you to see this side and to know what is written there.

      Ale! If you think about doing more and more physical education - only after full-time consultations with a competent doctor. Hypertension people can be merciful without problems with the heart, but you can’t, because you are called infarction on the way.

      It is important to consider all of our stats in the block “Growing up in hypertension for 3 days – it’s real”. It is said there that it is necessary to have an analysis done and cooled down at an independent laboratory, as well as additives, magnesium cream, to take coris for heart nourishment. If you are thin, then a low-carbohydrate diet is not important for you.

  6. Tetyana

    Meni 30 years old, 164 cm, 65 kg at a time. In red 2013 rock (vaga bula 86 kg) I was more strong, tribal stressful situation, after I fell ill. Tachycardia up to 150 beats per quill with tension, often increased arterial pressure up to 180/105, severe confusion and severe weakness. Blood analysis is normal, blood density is less than 118% and cholesterol is 5.2. Physicians, cardiologists, have given advice, which is not cardiology, but psychosomatics. I was prescribed noofen, bisoprolol. I have already completed the entire course, I am now leading a healthy way of life. Charging, sports, regular walks, proper eating. I felt better, lost weight by 20 kg, blood pharynx was already 87% and cholesterol was 4. Arterial pressure was stable 112/70, pulse was 60-75 after the start. Now the hour has come for bisoprolol. Let me tell you, how to correctly take yoga, so that there is no withdrawal syndrome? I took yoga for 4 months at 2.5, and for 2 more days at 1.25, and then how much more do you drink? Thank you very much for help :).

  7. Hermann

    Meni 73 rocks. In conjunction with fluctuations in arrhythmias, which are more frequent, and indications of ultrasound of the heart, stress echocardiography is recommended. What is needed in advance of the next day to say veroshpiron, norvan, product, cardiomagnyl, crestor?

  8. Igor

    Good afternoon! Dyakuyu, scho you help people. May I ask. Size 177 cm, weight 109 kg, weight 40 years. Periodically, three times a month, the tick is 165/98/105 with tachycardia. Menі lіkar therapist 4 months ago admitting to drink bіsoprolol once a day, saying that it's for life. I drank right, there were no problems, the vice was renewed 117/70/75. I stopped taking Bisoprolol - by lowering the dose, and after 3 days tachycardia and vice 140/90/98 appeared. Turning back to shvidkoy - they gave me pills - after 20 quills it became warm in my hands, everything calmed down. The next day, having drunk a huge dose of Bisoprolol, everything was good. After a couple of days, I started drinking again half. 2 days have passed - I have a new vice and tachycardia. What should I do? Earlier, during the crisis, I drank Anaprilin and Valocordin. Now I don't know how to arrange everything for me. Razumіyu, scho my therapist don't give a shit, but I want to live! What should I do? Thank you!

  9. Lydia

    I live! Chi can but beta-blockers have such side effects, like the liver of the tongue, you can feel the sting in the throat and on the palate. Earlier it was blamed, then more often, but at the same time not to pass for a long month already. I went back to the gastroenterologist - the sign of exuberance does not help. I respected that the symptoms would improve in the first five years after taking beta-blockers, as well as in other cases.

    Meni 67 years, size 161 cm, weight 86 kg. I take a lot of beta-blockers. Started with Atenolol, then Coronal, then Binelol once a day. I take two Valz tablets a year. How long did Enap take. Diagnosis - hypertension stage 2. There is no diabetes. Bowel problems.

    What can be done with beta-blockers? What is it like hypertensive pills without such side effects?

  10. Karina

    I live! My size is 155 cm, the weight is 52 kg, for the last 29 years. After low stress situations (canopies 2.5 years ago, and then the funeral of the father 11 months after the birth of the child), problems began with the heart. Panic attacks came. The pulse of a calm stan is over it rises. She underwent a cardiogram - a tachycardia crimson, no daily respirations were detected. Additional ECG monitoring did not reveal any serious problems either. Ultrasound of the heart revealed even a small prolapse - the doctor said that with such a pathology one can become extremely alive and live to a deep old age. Everything would be nothing, that axis was only quickened, the heartbeat began to turbulate less. So is the ringing bіl near the region of the heart. Stverzhuvati, scho to the very heart, I do not undertake, but as long as they appear independently of the pressure and for an hour to wind up in a lying position. Likar prescribed nebivolol and adaptol. Later, adaptol was replaced with melissa and valerian in tablets. Kіlka once step by step took a beta-blocker - thank God, without naslіdkіv. Ninі p'yu їkh znovu, ale є problem. Tachycardia does not go away. Obviously, the pulse is no longer 120-150, but in an hour it reaches 100 in a calm physical state. My child is already active, declaring to God, but albeit leading to constant stress and insufficiency. What can be done to the sky to calm the rhythm and nerves? Maybe valocordin at the drops? Thank you in advance for help and ask for spelling and punctual pardons. I even boast about the frequent pulse and folding in typing on the phone. That same therapist made a diagnosis of VVD.

    I live! Meni 41 rec. 80kg, doing sports. 12 years later, a non-cardiologist recognized Coronal 5mg (because 12 years later, it was unbearable to sit at the PC, it became stuffy and scary, pidbіg until the end of the day, it was allowed to go to the doctor, they died) (if there might be a reaction to stress), they said that hypertension (150/100 was already bulo), it was injected lower (it was sick for two days sweat) and then cardiol. prescribed a blocker.
    During the beer, 12 years of discipline were disciplined, everything was normal, pressure was normal, And the rest of the drink began to hurt my head and showed apathy to physical challenges and even a lack of work and fire! The dose was magnified and reduced and increased (gradually natural), as a result, the pressure was 140/85, and such a cotton head. (Kava doesn't really help) While I'm lost, help plz. Can you tell me to take a BB (dose w min. bula)? Abo navpaki increase the dose (ale pressurize the same with a higher dose of BB !!!) Trying to remember the coronal for the concor (it didn’t work, the head began to get confused, turning back to the coronal) ....
    Once in 12 years, I went to the doctors for the drive to tell the BB. And all yak one vyslovluvalis negatively. (Ale, when they recognized their hour, there was really no volodinny!!! I am so understanding, all at once afraid of the consequences for their words: ((Explain and help plz!).

Didn't they know the information, did they joke around?
Submit your food here.

How to wriggle out of hypertension independently
for 3 days, without expensive shkіdlivih likіv,
"hungry" diet and important physical culture:
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Dyakuyu

The site provides additional information, including for information. It is necessary to go through the diagnosis of that likuvannya ill under the supervision of a fahіvtsya. Usі drugs and mayut contraindications. Consultation fahіvtsya є obov'yazkovaya!

Adrenoblockers¾ a group of drugs, combined with a global pharmacological action - to neutralize the adrenaline receptors of the blood vessels of the heart. That is, adrenoblockers "mimic" receptors, which in a great state react to adrenaline and norepinephrine. Obviously, the effects of adrenoblockers are similar to those of adrenaline and norepinephrine.

Zagalna characteristic

Adrenoblockers work on adrenergic receptors, they are roztashovuyutsya at the walls of the blood vessels and the heart. The name given to the group of preparations was taken away by itself in view of the fact that stinks block the activity of adrenoreceptors.

Normally, if the adrenoreceptors are strong, they can infuse adrenaline and norepinephrine, as in the bloodstream. Adrenaline in connection with adrenoreceptors provokes the following effects:

  • Vessel-sounding (sharply sounding lumen of blood-bearing vessels);
  • Hypertensive (moving arterial pressure);
  • Antiallergic;
  • Broncholitic (expansion of the lumen of the bronchi);
  • Hyperglycemic (increasing the level of glucose in the blood).
The preparations of the group of adrenoblockers act as a bi-mimics of adrenoreceptors, visibly, deviate, directly proliferating adrenaline, so that they expand blood vessels, reduce arterial pressure, sound the lumen of bronchial tubes and change the level of glucose in the blood. Obviously, the most severe effects of adrenoblockers, the power of all drugs of the pharmacological group.

Classification

In the walls of the blood-bearing vessels, there are several types of adrenergic receptors - ce alpha-1, alpha-2, beta-1 and beta-2, which are called in a similar way: alpha-1-adrenergic receptors, alpha-2-adrenergic receptors, beta-1-adrenoreceptors and beta -2-adrenergic receptors. Preparations of a group of adrenoblockers can be different types of receptors, for example, only beta-1-adrenoreceptors or alpha-1,2-adrenoreceptors, etc. Adrenoblockers are subdivided into sprat groups, depending on the fact that they themselves see adrenoreceptor stinks.

Also, adrenoblockers are classified into the following groups:

1. Alpha blockers:

  • alpha-1-blockers (alfuzosin, doxazosin, prazosin, silodosin, tamsulosin, terazosin, urapidil);
  • Alpha-2-blockers (yohimbine);
  • Alpha-1,2-adrenergic blockers (nitsergoline, phentolamine, proroxan, dihydroergotamine, dihydroergocristine, alpha-dihydroergocriptine, dihydroergotoxin).
2. Beta blockers:
  • Beta-1,2-blockers (also called non-selective) - bopindolol, metipranolol, nadolol, oxprenolol, pindolol, propranolol, sotalol, timolol;
  • Beta-1-blockers (also called cardioselective or simply selective) - atenolol, acebutolol, betaxolol, bisoprolol, metoprolol, nebivolol, talinolol, celiprolol, esatenolol, esmolol.
3. Alpha beta blockers (alpha-i beta-adrenergic receptors mimic one hour) - butylmethyloxadiazole (proxodolol), carvedilol, labetalol.

In this classification, international names of active speeches were given, which should be included in the warehouse of preparations, which should lie down to the dermal group of adrenoblockers.

The skin group of beta-blockers is also divided into two types - from internal sympathomimetic activity (ICA) or without ICA. However, the classification is given as additional and necessary only for doctors to choose the optimal drug.

Adrenoblockers - list

Let's bring up lists of drugs for the skin group of adrenoblockers (alpha and beta), okay, to avoid confusion. In all lists, the name of the active speech (MPN) is indicated first, and then below - the commercial names of the preparations, before the warehouse of which the names of the components are included.

Drugs alpha-blockers

Let's list the alpha-adrenergic blockers of different subgroups in different lists for the easiest and most structured search for the necessary information.

Before preparations of the alpha-1-adrenergic blocking group appear like this:

1. Alfuzosin (MPN):

  • Alfuprost MR;
  • alfuzosin;
  • Alfuzosin hydrochloride;
  • Dalphaz;
  • Dalphaz Retard;
  • Dalfaz SR.
2. Doxazosin (MPN):
  • Artezin;
  • Artezin Retard;
  • doxazosin;
  • Doxazosin Bylupo;
  • Doxazosin Zentiva;
  • Doxazosin Sandoz;
  • Doxazosin-ratiopharm;
  • Doxazosin Teva;
  • doxazosin mesylate;
  • Zokson;
  • Kamiren;
  • Kamiren HL;
  • Cardura;
  • Cardura Neo;
  • Tonocardin;
  • Urocard.
3. Prazosin (INN):
  • Polpresin;
  • Prazosin.
4. Silodosin (MPN):
  • Urorek.
5. Tamsulosin (MPN):
  • Hyperprost;
  • Glansin;
  • Myctosin;
  • Omnik Okas;
  • Omnic;
  • Omsulosin;
  • Proflosin;
  • Sonizin;
  • Tamselin;
  • Tamsulosin;
  • Tamsulosin Retard;
  • Tamsulosin Sandoz;
  • Tamsulosin-OBL;
  • Tamsulosin Teva;
  • Tamsulosin hydrochloride;
  • Tamsulon FS;
  • Taniz EPAC;
  • Taniz Do;
  • Tulosin;
  • Focusin.
6. Terazosin (MPN):
  • Koran;
  • Setegis;
  • Terazosin;
  • Terazosin Teva;
  • Khaitrin.
7. Urapidil (INN):
  • Urapidil Carino;
  • Ebrantil.
Before preparations of alpha-2-blockers Yohimbine and Yohimbine hydrochloride are seen.

Before preparations of the alpha-1,2-blockers group to have the following preparations:

1. Dihydroergotoxin (sumish dihydroergotamine, dihydroergocristine and alpha-dihydroergocriptin):

  • Redergin.
2. Dihydroergotamine:
  • Ditamin.
3. Nicergoline:
  • Nilogrin;
  • Nicergoline;
  • Nicergoline-Ferein;
  • Sermion.
4. Proroxan:
  • Pirroxan;
  • Proroxan.
5. Phentolamine:
  • Phentolamine.

Beta blockers - list

Some of the beta-adrenergic blockers in the skin group include a large number of drugs, we will list them for more easy administration and, if necessary, information.

Selective beta-blockers (beta-1-blockers, selective blockers, cardioselective blockers). Name the pharmacological group of adrenergic blockers in the arches of rehabilitated congestion.

Also, before selective beta-blockers, the following preparations should be applied:

1. Atenolol:

  • Atenobeny;
  • Atenova;
  • Atenol;
  • Athenolan;
  • Atenolol;
  • Atenolol-Agio;
  • Atenolol-AKOS;
  • Atenolol-Acre;
  • Atenolol Bylupo;
  • Atenolol Nycomed;
  • Atenolol-ratiopharm;
  • Atenolol Teva;
  • Atenolol UBF;
  • Atenolol FPP;
  • Atenolol Stada;
  • Atenosan;
  • Betacard;
  • Velorin 100;
  • Viro-Atenolol;
  • Ormidol;
  • Prinorm;
  • Sinar;
  • Tenormin.
2. Acebutolol:
  • Acecor;
  • Sektral.
3. Betaxolol:
  • Betak;
  • Betaxolol;
  • Betalmik EC;
  • Betoptik;
  • Betoptik C;
  • Betoftan;
  • Xonef;
  • Xonef BK;
  • Lokren;
  • Optibetol.
4. Bisoprolol:
  • Aritel;
  • Aritel Core;
  • Bidop;
  • Bidop Cor;
  • Biol;
  • Biprol;
  • Bisogama;
  • Biocard;
  • Bisomor;
  • bisoprolol;
  • Bisoprolol-OBL;
  • Bisoprolol LEXVM;
  • Bisoprolol Lugal;
  • Bisoprolol Prana;
  • Bisoprolol-ratiopharm;
  • Bisoprolol C3;
  • Bisoprolol Teva;
  • bisoprolol fumarate;
  • Concor Core;
  • Korbis;
  • Cordinorm;
  • Cordinorm Core;
  • Coronal;
  • Niperten;
  • Tirez.
5. Metoprolol:
  • Betaloc;
  • Betaloc ZOK;
  • Vasocordin;
  • Corvitol 50 and Corvitol 100;
  • Metozok;
  • Metocard;
  • Metocor Adifarm;
  • Metolol;
  • metoprolol;
  • Metoprolol Acre;
  • Metoprolol Akrikhin;
  • Metoprolol Zentiva;
  • Metoprolol Organic;
  • Metoprolol OBL;
  • Metoprolol-ratiopharm;
  • metoprolol succinate;
  • metoprolol tartrate;
  • Serdol;
  • Egilok Retard;
  • Egilok S;
  • Emzok.
6. Nebivolol:
  • Bivotens;
  • Benelol;
  • Nebivator;
  • Nebivolol;
  • Nebivolol NANOLIK;
  • Nebivolol Sandoz;
  • Nebivolol Teva;
  • Nebivolol Chaikapharma;
  • Nebivolol STADA;
  • Nebivolol hydrochloride;
  • Nebikor Adifarm;
  • Nebilan Lannacher;
  • Newcomer;
  • Nebilong;
  • OD-Neb.


7. Talinolol:

  • Kordanum.
8. Celiprolol:
  • Celiprol.
9. Yesatenolol:
  • Estekor.
10. Esmolol:
  • Breviblock.
Non-selective beta-blockers (beta-1,2-blockers). Before the whole group lie like this medical care:

1. Bopindolol:

  • Sandonorm.
2. Metipranolol:
  • trimepranol.
3. Nadolol:
  • Korgard.
4. Oxprenolol:
  • Trazikor.
5. Pindolol:
  • Wisken.
6. Propranolol:
  • Anaprilin;
  • Viro-Anaprilin;
  • Іnderal;
  • Іnderal LA;
  • obzidan;
  • propranobene;
  • propranolol;
  • Propranolol Nycomed.
7. Sotalol:
  • Darob;
  • SotaGEKSAL;
  • Sotalex;
  • Sotalol;
  • Sotalol Canon;
  • Sotalol hydrochloride.
8. Timolol:
  • Arutimol;
  • Glaumol;
  • Glautam;
  • Kuzimolol;
  • Niolol;
  • Okumed;
  • Okumol;
  • Okupres E;
  • Optimol;
  • Oftan Timogel;
  • Oftan Timolol;
  • Oftensin;
  • TimoGEKSAL;
  • Thymol;
  • Timolol;
  • Timolol AKOS;
  • Timolol Betalek;
  • Timolol Bufus;
  • Timolol DIA;
  • Timolol Lens;
  • Timolol MEZ;
  • Timolol PIS;
  • Timolol Teva;
  • Timolol maleate;
  • Timollong;
  • Timoptic;
  • Timoptic Depot.

Alpha-beta-blockers (drugs that mimic both alpha and beta-adrenergic receptors)

Before the preparations of this group, the following should be considered:

1. Butylmethyloxadiazole:

  • Albetor;
  • Albetor Long;
  • Butylmethyloxadiazole;
  • Proxodolol.
2. Carvedilol:
  • Acridilol;
  • Bagodilol;
  • Vedicardol;
  • Dilatrend;
  • Carvedigama;
  • Carvedilol;
  • Carvedilol Zentiva;
  • Carvedilol Canon;
  • Carvedilol Obolenske;
  • Carvedilol Sandoz;
  • Carvedilol Teva;
  • Carvedilol STADA;
  • Carvedilol-OBL;
  • Carvedilol Pharmaplant;
  • Carvenal;
  • Carvitend;
  • Carvidil;
  • Cardivas;
  • Coriol;
  • Credex;
  • Recardium;
  • Talliton.
3. Labetalol:
  • Abetol;
  • Amipres;
  • Labetol;
  • Trandol.

Beta-2 blockers

Pharmaceutical preparations, although isolated, only mimic beta-2-adrenergic receptors, none. Previously, the drug Butoxamine, which is a beta-2-adrenoblocker, has been released in recent years in medical practice and becomes of interest only to medical experimenters who specialize in pharmacology and organic synthesis.

Less than non-selective beta-adrenergic blockers; However, other selective blockers that mimic beta-1-adrenergic receptors exclusively are often non-selectively called beta-2-blockers. The similar name is not correct, but it is widened in a different way. So, if you say "beta-2-blockers", you need to know that there is a group of non-selective beta-1,2-blockers on the market.

Diya

Oskіlki exclusion of different types of adrenoreceptors to produce to the development of zagal zagalnyh, albeit in some aspects of effects, then we can look at the dermal type of adrenoblockers okremo.

Dia alpha-blockers

Alpha-1-adrenergic blockers and alpha-1,2-adrenergic blockers Pharmacological activity. And one type of one drug and these groups are considered to have side effects, which are more pronounced in alpha-1,2-adrenergic blockers, and the stench is more often blamed on alpha-1-adrenergic blockers.

So, the preparations of these groups expand the vessels of all organs, especially the skin, mucous membranes, intestines and nirok. For the rahunok of this, the peripheral peripheral pressure of the vessels changes, the blood flow and blood supply of the peripheral tissues improve, and the arterial pressure also decreases. For the decrease in the peripheral support of the vessels, the change in the amount of blood, which rotates to the atrium of the veins (venous rotation), actually changes the preta postnatalization on the heart, which significantly eases the work of the body and is positively indicated on the station of this organ. According to the foregoing, it is possible to increase the number of whiskers that alpha-1-adrenoblockers and alpha-1,2-adrenoblockers can do the following:

  • Reduce the arterial pressure, change the deep peripheral pressure of the vessel and postnatalization on the heart;
  • Expand the veins and change the predilection at the heart;
  • Polipshyut blood circulation as in the whole organism, so in the heart meat;
  • Polypshuyut camp of people who suffer from chronic heart failure, changing the severity of symptoms (buttocks, stribkiv vise, etc.);
  • Reduce the pressure on legenous coli krovoobіgu;
  • Reduce the level of total cholesterol and low-grade lipoproteins (LPNS), but increase instead of high-grade lipoproteins (LPSLs);
  • Increase the sensitivity of clitin to insulin, which makes glucose more effective, and the concentration in the blood decreases.
Zavdyaki assigned to the pharmacological effects of alpha-adrenergic blockers reduce arterial pressure without the development of reflex heartbeat, and also change the severity of hypertrophy of the left duct of the heart. The drug effectively reduces the isolated increase in systolic pressure (the first number), including the increase in obesity, hyperlipidemia and reduced tolerance to glucose.

In addition, alpha-adrenergic blockers reduce the severity of symptoms of inflammation and obstructive processes in the sechostatic organs, resulting in hyperplasia of the anterior fold. Tobto, the preparations can be used or change the manifestation of an inconsistent deformity of the sich mihur, nocturnal sechovipkanny, frequent sechovipchennya and liver during sichovipkannі.

Alpha-2-adrenergic blockers are slightly injected into the blood-bearing vessels of the internal organs, the heart, stinks are injected more importantly into the vascular system of the organs. For this very reason, alpha-2-adrenergic blockers may have a very narrow sphere of stagnation - the exaltation of impotence in people.

Diagnosis of non-selective beta-1,2-blockers

  • Change the heart rate;
  • Reduce the arterial pressure and calmly change the deep peripheral support of the vessels;
  • Change the speed of the myocardium;
  • Change the consumption of heart oil in sourness and increase the resistance of її clitin to sour hunger (ischemia);
  • Change the level of activity of the igniters in the conduction system of the heart and thereby prevent arrhythmias;
  • Change the vibration of the renina with nirks, which also leads to a decrease in the arterial pressure;
  • At the cob stages, the stagnation increases the tone of the blood-bearing vessels, and then it decreases to normal or lower;
  • Pereskodzhayut clumping of platelets and formation of thrombi;
  • Polypshuyut kisnyu vіd erythrocytes to cells of organs and tissues;
  • Pіdsilyuyut skorochennya miometrіyu (m'yazovy ball of the uterus);
  • Increase the tone of the bronchi and the sphincter of the stravokhod;
  • Strengthen the motility of the organs of the herbal tract;
  • Relax the detrusor of sich michur;
  • Increase the release of active forms of hormones in the thyroid gland in peripheral tissues (but only beta-1,2-adrenergic blockers).
Zavdyaky appointed pharmacological effects of non-selective beta-1,2-blockers reduce the risk of recurrent heart attack and heart death by 20 - 50% in people who suffer from IXC or heart failure. In addition, with IXC, drugs of this group change the frequency of attacks of angina pectoris and pain in the heart, improve the tolerance of physical, mental and emotional distress. In case of hypertensive ailment, the preparations of this group change the risk of development of IXC and stroke.

In women, non-selective beta-blockers increase uterine contractility and reduce blood loss at a lower hour or after surgery.

In addition, non-selective beta-blockers reduce intraocular pressure and change the production of water in the anterior chamber of the eye. Dana di preparations victorious in glaucoma and other ailments of the eyes.

Diagnosis of selective (cardioselective) beta-1-blockers

Preparations of this group may have such pharmacological effects:
  • Lower the heart rate (HR);
  • Change the automatism of the sinus node (guiding the rhythm);
  • Zagalmovuyut conduction of the impulse by the atrioventricular node;
  • Change the shortness of that zbudlivist heart meat;
  • Change the need of the heart in sourness;
  • Ignore the effects of adrenaline and norepinephrine on the heart in the minds of physical, mental and emotional pressure;
  • Reduce arterial pressure;
  • Normalize the heart rhythm in arrhythmias;
  • Surround that width of the zone of ushkodzhennya in case of myocardial infarction.
As a result of pharmacological effects, selective beta-blockers change the amount of blood that the heart pumps into the aorta in one shortness of time, reduce arterial pressure and prevent orthostatic tachycardia (early heartbeat when lying down in a sitting position). Also, the preparations increase the frequency of the heart rate and change its strength for the lowering of the heart rate in acidity. Zagalom, selective beta-1-adrenergic blockers reduce the frequency and severity of attacks from IXC, improve the tolerance of attacks (physical, mental and emotional) and significantly reduce mortality in people who suffer from heart failure. These effects of drugs lead to a significant increase in the life of people who suffer from IXC, dilated cardiomyopathy, and also suffered a myocardial infarction and stroke.

In addition, beta-1-adrenergic blockers cause arrhythmia and ringing of the lumen of other vessels. In people who suffer from bronchial asthma, the risk of bronchospasm is reduced, and in case of diabetes mellitus, the development of hypoglycemia is reduced (low blood sugar level).

Diya alpha-beta-adrenergic blockers

Preparations of this group may have such pharmacological effects:
  • Reduce the arterial pressure and change the deep peripheral support of the vessels;
  • Reduce intraocular pressure in acute glaucoma;
  • Normalize indications with lipidograms (reduce the level of total cholesterol, triglycerides and lipoproteins in low blood pressure, and also increase the concentration of lipoproteins in high blood pressure).
Zavdyaky assigned to pharmacological effects of alpha-beta-blockers may reduce hypotensive pressure (reduce pressure), expand blood vessels and change postnatal pressure on the heart. On the basis of beta-blockers, the drugs of this group reduce arterial pressure, without changing the circulatory blood flow and not increasing the peripheral peripheral pressure of the vessels.

In addition, alpha-beta-adrenergic blockers improve the shortness of the myocardium, for which the blood does not fill up in the left ventricle after the shortness of the blood, but in full obsyazatsya in the aorta. Tse spryaє zmenshennu rozmіrіv sertsya i nizhuє stupі yogo deformії. Zavdyaky polypshennuyu work and heart preparations of this group in case of congestive heart failure increase the severity of physical, mental and emotional tensions that can be tolerated, change the frequency of heart attacks and IXC, as well as normalize the hearts.

The use of alpha-beta-blockers reduces mortality and the risk of re-infarction in people who suffer from IXC or dilated cardiomyopathy.

Zastosuvannya

It is clearly shown that the sphere of stagnation of different groups of adrenoblockers is OKremo, so that the swindlers get away.

Indicated before the blocking of alpha-adrenergic blockers.

Several preparations and subgroups of alpha-adrenoblockers (alpha-1, alpha-2 and alpha-1,2) may have different mechanisms of action and sometimes they are one in the nuances of the injection on the judge, then the scope of their zastosuvannya, apparently, the indications are also different.

Alpha-1-blockers indications before zastosuvannya with advancing camps and illness:

  • hypertonic ailment (with the method of lowering the arterial pressure);
  • Dobryakіsna hyperplasia of the anterior ridge.
Alpha-1,2-blockers indications before zastosuvannya for nayavnosti in a person of advancing states or ill:
  • Peripheral circulatory disorders (for example, Raynaud's disease, endarteritis toshcho);
  • Dementia (bewilderment), maddened by the judicial component;
  • Vertigo and damage to the work of the vestibular apparatus, affected by the judgment factor;
  • Diabetic angiopathy;
  • Dystrophic disease of the horn of the eye;
  • Neuropathy of the zonal nerve, accompanied by yoga ischemia (sour starvation);
  • Hypertrophy of the anterior fold;
  • Decomposition of sieve production against the background of neurogenic sich michur.
Alpha-2-blockers to sing vinyatkovo for the exaltation of impotence in people.

Stopping beta-blockers (indication)

Selective and non-selective beta-adrenoblockers may be devastated by one type of one indication of that area of ​​zastosuvannya, which is influenced by the nuances of singing їх infusion on the heart of that judge.

Indication for zastosuvannya non-selective beta-1,2-adrenergic blockers. offensive:

  • Arterial hypertension;
  • Angina pectoris;
  • Sinus tachycardia;
  • Prevention of mucosal and supraventricular arrhythmias, as well as bigeminia, trigeminia;
  • mitral valve prolapse;
  • myocardial infarction;
  • Prevention of migraine;
  • Advance internal vice.
Indication for the use of selective beta-1-adrenergic blockers. This group of adrenergic blockers is also called cardioselective, shards, head rank, stench in the heart, and a significantly smaller world on the judge and the size of the arterial pressure.

Cardioselective beta-1-adrenergic blockers are indicated before stagnation for manifestations in people of advanced illness or becoming:

  • Arterial hypertension of moderate degree of severity;
  • ischemic heart disease;
  • Hyperkinetic cardiac syndrome;
  • Various types of arrhythmias (sinus, paroxysmal, supraventricular tachycardia, extrasystole, trembling or atrial fibrillation, atrial tachycardia);
  • Hypertrophic cardiomyopathy;
  • mitral valve prolapse;
  • Myocardial infarction (treatment of a heart attack, which has already become, and prevention of a relapse);
  • Prevention of migraine;
  • Neurocirculatory dystonia for hypertensive type;
  • In complex therapy of pheochromocytoma, thyrotoxicosis and tremor;
  • Akathisia provoked by the use of neuroleptics.

Indicated for alpha-beta-adrenergic blockers.

The preparations of this group are indicated for constipation for manifestations in people of advanced stages or illness:
  • Arterial hypertension;
  • Stable angina;
  • Chronic heart failure (at the warehouse of combined therapy);
  • arrhythmia;
  • Glaucoma (the drug is administered as eye drops).

Side effects

Let's take a look at the side effects of adrenoblockers of various groups of okremo, oscalls, unimportantly on similarities, between them there are a number of identities.

Usі alpha-adrenoblockers zdatnі provokuvat yak however, і different side effects, scho s peculiarities of their injection of chi іnshi types of adrenergic receptors.

Side effects of alpha-blockers

Otzhe, all alpha-blockers (alpha-1, alpha-2 and alpha-1,2) provoke the same side effects:
  • Head bіl;
  • orthostatic hypotension (slight decrease in the grip when moving to a standing position from a sitting or lying position);
  • Syncopal stands (short-hour insomnia);
  • Nudota or vomit;
  • Constipation or carrying.
Cream of that alpha-1-adrenergic blockers can cause such side effects, moreover characteristic for all groups of adrenoblockers:
  • hypotension (stronger decrease in arterial pressure);
  • Tachycardia (heartbeat);
  • arrhythmia;
  • Zadishka;
  • Unclear dawn (fog in front of the eye);
  • xerostomia;
  • Considering discomfort in the abdomen;
  • Damage to cerebral circulation;
  • Decreased libido;
  • priapism (trival painful erections);
  • Allergic reactions (hanging, sverbіzh shkіri, kropiv'yanka, Quincke's snag).
Alpha-1,2-adrenergic blockers, a cream for all adrenoblockers, can cause the following side effects:
  • excitement;
  • Cold weather;
  • angina attack;
  • Increased acidity of shell juice;
  • Impaired ejaculation;
  • Bіl at kіntsіvkah;
  • Allergic reactions (blackheads and redness of the upper half of the body, kropivyanka, erythema).
Side effects of alpha-2-adrenergic blockers, creamy for all adrenoblockers, such as:
  • Tremor;
  • arousal;
  • Drativity;
  • Advancement of arterial pressure;
  • Tachycardia;
  • Stronger rukhovoї activity;
  • Bіl in the stomach;
  • Priapism;
  • Change in the frequency and quantity of sechovi- sions.

Beta-blockers - side effects

Selective (beta-1) and non-selective (beta-1,2) adrenergic blockers may have both the same side effects and different ones, which is due to their peculiarities in different types of receptors.

So, however, for selective and non-selective beta-blockers, there are also side effects:

  • Zamorochennya;
  • Head bіl;
  • drowsiness;
  • sleeplessness;
  • Nightmare dream;
  • Stomlyuvanist;
  • Weakness;
  • Worried;
  • entanglement of information;
  • Short-hour episodes to waste your memory;
  • Upovilnennya reaction;
  • Paresthesia (obvious bіgannya "goosebumps", names of kіntsіvok);
  • Porushennya dawn and relish;
  • Dryness empty mouth that eyes;
  • bradycardia;
  • Heartbeat;
  • Atrioventricular block;
  • Damage to the conductivity of the heart meat;
  • arrhythmia;
  • Decreased speed of the myocardium;
  • hypotension (decreased arterial pressure);
  • Heart failure;
  • Raynaud's phenomenon;
  • Pain in the chest, m'yazah and swamps;
  • Thrombocytopenia (a change in the total number of platelets in the blood below the norm);
  • Agranulocytosis (the presence of neutrophils, eosinophils and basophils in the blood);
  • Nudota that vomit;
  • Bіl in the stomach;
  • Carrying chi constipation;
  • Damaged robotic liver;
  • Zadishka;
  • Spasm of bronchi and larynx;
  • Allergic reactions (sverbіzh shkіri, visip, reddish);
  • Drinkability;
  • Cold weather;
  • M'yazova weakness;
  • Loss of libido;
  • Increase or decrease in the activity of enzymes, blood bilirubin and glucose levels.
Non-selective beta-blockers (beta-1,2), dodatkovo to transfer more, can also cause such side effects:
  • Razdratuvannya eyes;
  • Diplopia (twin vision);
  • Nasal congestion;
  • Dyhal insufficiency;
  • collapse;
  • Zagostrennya kulgavostі, scho interspersed;
  • Timchasov damage to cerebral circulation;
  • Ischemia of the brain;
  • Neatness;
  • Decreased level of hemoglobin in the blood and hematocrit;
  • Nabryak Quincke;
  • Change of vag body;
  • Vovchakovy syndrome;
  • impotence;
  • Peyron's disease;
  • Thrombosis of the mesenteric artery of the intestine;
  • Colitis;
  • Increased level of potassium, sechoic acid and triglycerides in the blood;
  • Blurring that lowering of the dawn, liver, sverbіzh and vіdchuttya third party body in the eyes, tearing, fear of light, swelling of the horn, inflamed edges of the eyes, keratitis, blepharitis and keratopathy (scratches for the eyes).

Side effects of alpha-beta-blockers

Side effects of alpha-beta-adrenergic blockers include deacons. side activities both alpha and beta blockers. However, the stench is not identical to the side effects of alpha-blockers and beta-blockers, but the symptoms of side effects are similar. Otzhe, alpha-beta blockers may have the following side effects:
  • Zamorochennya;
  • Head bіl;
  • Asthenia (look at it, a fall of strength, baiduzhostі toshcho);
  • Syncopal stands (short-hour insomnia);
  • M'yazova weakness;
  • Scattered weakness and stubbornness;
  • sleep disorder;
  • depression;
  • Paresthesia (seemingly "goosebumps", names of kіntsіvok, etc.);
  • Xerophthalmia (dry eye);
  • Changes in the production of mucous membranes;
  • bradycardia;
  • Impaired atrioventricular conduction to blockade;
  • Hypotension is postural;
  • Pain in the chest, in the abdomen and in the kinks;
  • angina pectoris;
  • loss of peripheral blood flow;
  • Complicated heart failure;
  • Zagostrennya Raynaud's syndrome;
  • Nabryaki;
  • Thrombocytopenia (a decrease in the number of platelets in the blood below the norm);
  • Leukopenia (change in total number;
  • Cold weather;
  • Blockade of the lower bundle of Hiss.
With vicarious alpha-beta-adrenergic blockers, visual eye drops may develop side effects:
  • bradycardia;
  • Decreased arterial pressure;
  • Bronchospasm;
  • Zamorochennya;
  • Weakness;
  • Seeing the liver or a third-party body in the center;

Contraindication

Contraindication to zastosuvannya different groups of alpha-adrenergic blockers.

Contraindications before the stoppage of various groups of alpha-adrenoblockers are indicated in the table.
Contraindications before blocking alpha-1-adrenergic blockers Contraindications before blocking alpha-1,2-adrenergic blockers Contraindications before blocking alpha-2-adrenergic blockers
Stenosis (ringing) of the aortic and mitral valvesAtherosclerosis of the peripheral vessels of the severe stage
Orthostatic hypotensionArterial hypotensionClips of the arterial vice
Serious damage to the robotic liverIncreased sensitivity to drug componentsUncontrolled hypotension or hypertension
VagityAngina pectorisSevere damage to the robotic liver abo nirok
Anniversary of the breastBradycardia
Increased sensitivity to drug componentsOrganic damage to the heart
Heart failure that developed against the background of constrictive pericarditis and cardiac tamponadeMyocardial infarction, transfers less than 3 months ago
Heart defects that run on the background low vise filling of the left chickGostra bleeding
Severe nirkov deficiencyVagity
Anniversary of the breast

Beta-blockers - contraindications

Selective (beta-1) and non-selective (beta-1,2) adrenoblockers may be practically identical contraindications before congestion. However, the spectrum of contraindications before the ingestion of selective beta blockers is broader, lower for non-selective ones. Usі contraindications to zastosuvannya for beta-1- and beta-1,2-adrenoblockers in the table.
Contraindication to non-selective (beta-1,2) blockers Contraindications before stopping selective (beta-1) blockers
Individual sensitivity to drug components
Atrioventricular block II or III stage
Sinoatrial blockade
Severe bradycardia (pulse less than 55 beats per beat)
Weak sinus syndrome
Cardiogenic shock
Hypotension (systole pressure less than 100 mm Hg)
Gostra heart failure
Chronic heart failure at the stage of decompensation
Obliterating disease of vesselsPeripheral blood circulation disorder
Angina PrinzmetalVagity
Bronchial asthmaAnniversary of the breast

Contraindications before blocking alpha-beta-blockers

Contraindications before blocking alpha-beta-blockers in the onset:
  • Increased individual sensitivity to any components of the preparations;
  • Atrioventricular block II or III stage;
  • Sinoatrial blockade;
  • Syndrome of weakness of the sinus node;
  • Chronic heart failure at the stage of decompensation (IV functional class according to NYHA);
  • cardiogenic shock;
  • Sinus bradycardia (pulse less than 50 beats per beat);
  • arterial hypotension (systolic pressure lower than 85 mm Hg);
  • Chronic obstructive disease of the leg;
  • Bronchial asthma;
  • Virazkov's ailment of the slug or twelve-fingered intestine;
  • Blood type 1 diabetes;
  • The period of vaginess and breast growth;
  • Severe disease of the liver.

Hypotensive beta-blockers

Antihypertensive drug may be given by different groups of adrenergic blockers. Alpha-1-adrenergic blockers, such as active components of speech, such as doxazosin, prazosin, urapidil or terazosin, may have the most pronounced hypotensive effect. To this very same preparation, this group of vicorist is used for the trial therapy of hypertensive ailments, with the method of reducing the pressure and further support on the middle pleasant level. Preparations of the alpha-1-adrenoblocker group are optimal for congestion in people who suffer less from hypertensive disease, without concomitant cardiac pathology.

In addition, hypotensive and all beta-blockers are both selective and non-selective. Hypotensive non-selective beta-1,2-adrenergic blockers to counteract active speech bopindolol, metipranolol, nadolol, oxprenolol, pindolol, propranolol, sotalol, timolol. These preparations, the cream of the hypotensive effect, are also injected into the heart, so they are not only used in the treatment of hypertension, but also heart disease. The most "weak" hypotensive non-selective beta-blocker is sotalol, which may be more important for the heart. However, this drug zastosovuєtsya in the treatment of arterial hypertension, as it can be caused by diseases of the heart. All non-selective beta-blockers are optimal for congestion with hypertension, which is associated with ICS, angina pectoris and myocardial infarction.

Antihypertensive selective beta-1-adrenergic blockers are medicinal preparations that can be used as active speech agents such as: atenolol, acebutolol, betaxolol, bisoprolol, metoprolol, nebivolol, talinolol, celiprolol, esatenolol, esmolol. The healing features of di, qi preparations are best suited for the treatment of arterial hypertension, which is associated with obstructive pathologies of the leg, congestion of the peripheral arteries, circulatory diabetes, atherogenic dyslipidemia, and also for chickens.

Alpha-beta-adrenergic blockers, which can prevent the active speech of carvedilol or butylmethyloxadiazole, are also hypotensive. Ale, through a wide range of side effects and pronounced infusion on other judges, preparations of this group of vicarious are more closely related to alpha-1-adrenergic blockers and beta-blockers.

In this hour, the drugs of choice for the treatment of arterial hypertension are beta-blockers and alpha-1-blockers.

Alpha-1,2-adrenergic blockers vikoristovuyutsya mainly for the treatment of peripheral and cerebral circulatory disorders, the oscillators may be more pronounced on other blood-bearing vessels. Theoretically, the preparations of this group can be used to reduce arterial pressure, but it is not effective due to the large number of side effects, which are to blame for cioma.

Adrenoblockers for prostatitis

In case of prostatitis, alpha-1-adrenergic blockers are stagnant, which can prevent the active speech of alfuzosin, silodosin, tamsulosin or terazosin, with the method of improving and facilitating the process of sechoviprosy. Indications for the recognition of adrenergic blockers in prostatitis are a low pressure in the middle of the urethra, a weak tone of the sieve michur itself or that of the neck, as well as the mucosa of the front of the urethra. Preparations normalize the cross section, which will speed up the removal of decay products, as well as dead disease-causing bacteria, and, apparently, increase the effectiveness of antimicrobial and anti-spasm treatment, which should be carried out. The positive effect will begin to develop again after 2 more periods of exposure. It's a pity, normalization of the current of the section for the diagnosis of adrenoblockers is only observed in 60 - 70% of people who suffer from prostatitis.

The most popular and effective adrenergic blockers for prostatitis are drugs that can be used against tamsulosin (for example, Hyperprost, Glansin, Myktosin, Omsulosin, Tulosin, Fokusin toshcho).

Before zastosuvannyam, you should consult with a faculty member.

BAB is a group of pharmacological drugs when introduced into the body of a person, blocking of beta-adrenergic receptors occurs.

Beta-adrenergic receptors are subdivided into three subtypes:

    бета1-адренорецептори, які розташовані в серці і через які опосередковуються стимулюючі впливи катехоламінів на діяльність серця - насоса: почастішання синусового ритму, поліпшення внутрішньосерцевої провідності, підвищення збудливості міокарда, посилення скоротливості міокарда (позитивні хроно-, дромо-, бат) ;

    beta2-adrenergic receptors, which are most important in the bronchi, smooth lingual cells of the arterial wall, skeletal masses, in the subductal cavity; with their stimulation, bronchitis, vasodilatation effects, relaxation of smooth tissues and secretion of insulin are realized;

    beta3-adrenergic receptors, localized most importantly on adipocyte membranes, take part in thermogenesis and lipolysis.

The idea of ​​winning beta-blockers as cardioprotectors belongs to the English J. W. Black, who in 1988 was awarded the Nobel Prize in 1988 together with the scientists, the creators of beta-blockers. The Nobel Committee recognized the clinical significance of these drugs as "the biggest breakthrough in the fight against heart diseases since the recognition of digitalis 200 years ago."

Classification

Preparations from the group of beta-blockers are considered for the presence or absence of cardioselectivity, intrinsic sympathetic activity, membrane-stabilizing, vasodilatory powers, variability in lipids and water, influencing the aggregation of platelets, and also for platelets.

At this time, clinicians see three generations of drugs with a beta-blocking effect.

I generation- non-selective beta1- and beta2-adrenoblockers (propranolol, nadolol), which, in a series of negative ino-, chrono-dromotropic effects, may improve the tone of the smooth muscles of the bronchi, the vessel wall, myometrium, which is between the armor.

II generation- cardioselective beta1-blockers (metoprolol, bisoprolol), high selectivity for beta1-adrenergic receptors in the myocardium may be more tolerable in case of trivial congestion and reconciliation, proving the basis for a long-term prognosis of life with the treatment of AH and HS.

Preparations III generation- celiprolol, bucindolol, carvedilol may have additional vasodilating power for the control of blockade of alpha-adrenergic receptors, without internal sympathomimetic activity.

table. Classification of beta-blockers.

1. β 1 ,β 2 -AB (non-cardioselective)

В·anaprilin

(propranolol)

2. β 1 -AB (cardioselective)

V bisoprolol

metoprolol

3. AB with vasodilating powers

β 1 ,α 1 -AB

B labetalol

B carvediol

β 1 -AB (activation of NO production)

nebivolol

end of the blockade

α 2 -adrenergic receptors and stimulation

β 2 -adrenergic receptors

celiprolol

4. AB due to intrinsic sympathomimetic activity

non-selective (β 1,β 2)

pindalol

selective (β1)

acebutalol

Talinolol

epanolol

Effective

The effect of blocking the influx of mediators on the beta1-adrenergic receptors of the myocardium and the weakening of the infusion of catecholamines on the membrane adenylyl cyclase of cardiomyocytes due to changes in the concentration of cyclic adenosine monophosphate (cAMP) indicate the main cardiotherapeutic effects of beta-blockers.

Anti-ischemic effect of beta-blockers explained by the decrease in consumption of the myocardium in the heart, in the event of a change in the frequency of heart rates (HR) and the strength of the heart rates, which is due to blocking of beta-adrenergic receptors in the myocardium.

Beta-blocker is once to forget the painting of the perfusion of the miracard for the zhunky kinsevo di-tape in a long slate (LS) of the zbizhnnya of Gradiynta, the vicinity of the coronarna of the pyd dijoye.

Antiarrhythmic diya beta-blockers, foundations on their zdatnosti change adrenergic influx on the heart, produce up to:

    change in heart rate (negative chronotropic effect);

    decrease in automatism of the sinus node, AV-z'ednannya and the His-Purkin system (negative bathmotropic effect);

    shortness of trivality to the potential di and refractory period in the Hisa-Purkin system (the QT interval is shortened);

    an increase in conductivity in the AV-z'ednanny and an increase in the trivality of the effective refractory period of the AV-z'ednanny, a decrease in the PQ interval (negative dromotropic effect).

Beta-adrenergic blockers increase the threshold of tympanic fibrillation in patients with host IM and may be seen as a prevention of fatal arrhythmias in the acute period of IM.

Hypotensive diya beta-blockers

    changes in the frequency and strength of the heart rate (negative chrono- inotropic diya), which can lead to a decrease in the low heart rate (MOS);

    decreased secretion and changes in plasma renin concentration;

    perebudovoy baroreceptor mechanisms of the aortic arch and carotid sinus;

    central prinychennyam sympathetic tone;

    blockade of postsynaptic peripheral beta-adrenergic receptors in the venous vascular bed, decreased blood flow to the right heart valves and decreased MOS;

    competitive antagonism with catecholamines for receptor binding;

    increase in the level of prostaglandins in the blood.

Influx on beta2-adrenergic receptors signifies a significant part of side effects and contraindications up to their congestion (bronchospasm, ringing of peripheral vessels). The peculiarity of cardioselective beta-blockers in the case of non-selective ones is greater sporidity to beta1-receptors in the heart, lower to beta2-adrenergic receptors. Therefore, when vikoristannі in small and medium doses qі preparations may be less pronounced by injecting into the smooth muscles of the bronchi and peripheral arteries. It should be noted that the ratio of cardioselectivity is not the same in different drugs. Index ci/beta1 to ci/beta2, which characterizes the degree of cardioselectivity, becomes 1.8:1 for non-selective propranolol, 1:35 for atenolol and betaxolol, 1:20 for metoprolol, 1:75 for bisoprolol. However, remember that the selectivity is dose-dependent, it will decrease with increasing doses of the drug.

Depending on the clinically significant pharmacokinetic powers of beta-blockers in drugs and subdivided into 3 groups (div. Table)

table. Features of the metabolism of beta-blockers.

* lipophilicity promotes penetration through the blood-brain barrier; with blockade of central beta-1 receptors, vagal tone is increased, which may be significant in the mechanism of antifibrillatory activity. There is evidence (Kendall M.J. et al., 1995) that a reduced risk of rapt death is more pronounced with vicarious lipophilic beta-blockers.

Shown:

    IXC (IM, snocardia)

    Tachyarrhythmias

    Rozsharovuyucha aneurysm

    Bleeding from varicose veins of the stravokhod (prevention in liver cirrhosis - propranolol)

    Glaucoma (timolol)

    Hyperthyroidism (propranolol)

    Migraine (propranolol)

    Alcohol withdrawal (propranolol)

Rules for the recognition of β-AB:

    initiate therapy at low doses;

    increase the dose not more frequently at 2 intervals;

    carry out treatment at the maximum tolerated dose;

    after 1-2 days after the cob treatment and 1-2 days after the completion of the dose titration, the necessary control of biochemical indicators in the blood.

When a number of symptoms appear against the background of an adrenoblocker, the following recommendations are made:

    with increasing symptoms of heart failure, the dose of β-blocker should be changed twice;

    for the presence of auto and / or bradycardia - reduce the dose of β-adrenergic blocker;

    in case of a serious aggravation, change the dose of a β-adrenergic blocker twice or take a cure;

    with heart rate< 50 уд./мин следует снизить дозу β-адреноблокатора вдвое; при значительном снижении ЧСС лечение прекратить;

    with a reduced heart rate, it is soon necessary to reconsider the doses of other drugs to reduce the increase in heart rate;

    For the presence of bradycardia, it is necessary to conduct an ECG monitoring for early detection of heart blocks.

Side effects all β-blockers are divided into cardial (bradycardia, arterial hypotension, development of atrioventricular blockades) and extracardial (confusion, depression, nightmares, insomnia, memory loss, stomluvanity, hyperglycemia, hypothermia).

Stimulation of β2-adrenergic receptors to increase glycogenolysis in the liver and skeletal tissues, gluconeogenesis and insulin resistance. Therefore, the stagnation of non-selective β-ABs can be associated with an increase in glycemia and an increase in insulin resistance. At the same hour at the vipadkas cerebrodiabetes Type 1 non-selective β-AB promotes the risk of chronic hypoglycemia, and after the introduction of insulin, traces of glycemia return to normal. Still unsafe is the nature of these preparations, resulting in a paradoxical hypertensive reaction, as it can be accompanied by reflex bradycardia. Such changes in hemodynamics will be associated with a significant increase in the level of adrenaline on aphids of hypoglycemia.

Another problem, which can be blamed for the repeated accumulation of non-selective β-ABs, is the disruption of lipid metabolism, the increase in the concentration of lipoproteins in even low blood pressure, triglycerides and the change in the presence of antiatherogenic cholesterol in the pancreas. Incidentally, these changes are blamed on the weakening of the effects of lipoprotein lipase, which is indicative of the metabolism of endogenous triglycerides. Stimulation of non-blocking α-adrenergic receptors against the background of blockade of β1 and β2-adrenergic receptors can lead to inhibition of lipoprotein lipase, while the inhibition of selective β-blockers gives the possibility of preventing these disorders of lipid metabolism. It should be noted that the favorable injection of β-AB as a cardioprotective agent (for example, after acute myocardial infarction) is significantly more important and important, lower than the adverse effect of these drugs on lipid metabolism.

Contraindication

Absolute contraindications for β-AB - bradycardia (< 50–55 уд./мин), синдром слабости синусового узла, АВ-блокада II–III степени, гипотензия, острая сосудистая недостаточность, шок, тяжелая бронхиальная астма. Хронические обструктивные заболевания легких в стадии ремиссии, компенсированные заболевания периферических артерий в начальных стадиях, депрессия, гиперлипидемия, АГ у спортсменов и сексуально активных юношей могут быть относительными противопоказаниями для применения β-АБ. Если существует необходимость их назначения по показаниям, предпочтительно назначать малые дозы высокоселективных β-АБ.

Antagonistcalcium(AK) - a large group of people for the chemical structure of preparations, the total power of them - the ability to change the intake of ions calcium in the smooth tongue cells of the vessels and cardiomyocytes, in a way of interaction with the right calcium channels (L-type) of cellular membranes. As a result, the smooth mucosa of the arterioles is relaxed, the arterial pressure and deep peripheral support of the vessels are reduced, the strength and frequency of the heart rates change, and atrioventricular (AV) conduction improves.

AK classification:

generation

Pokhіdnі dihydropyridine

(atreria>heart)

Pokhіdnі phenylalkіlamіnu

(atreria<сердце)

Pokhіdnі benzothiazepine

(atreri = heart)

I generation

(Preparations short ї dії)

Nifedipine

(Pharmadipin, Korinfar)

Verapamil(Izoptin, Lekoptin, Finoptin)

Diltiazem

II generation(Retard forms)

lik. form)

NifedipineSR

NicardipinSR

felodipineSR

VerapamilSR

Diltiazem SR

IIb

active

speeches)

Isradipin

Nisoldipin

Nimodipin

Nivaldipin

Nitrendipine

IIIgeneration(only in a group similar to dihydropyridine)

Amlodipine(Norvask, Emlodin, Duaktin, Normodipin, Amlo, Stamlo, Amlovas, Amlovask, Amlodak, Amlong, Amlopin, Tenox and іn);

Left wrapping amlodipine - Azomex

Lacidipine(Lacipil),

Lercanidipin(Lerkamen)

Combination drugs:

Equator, Gipril A (amlodipine + lysinopril)

Tinochok(Amlodipine + atenolol)

Note: SR and ER - preparations for improved vivilennia

Main pharmacological effects of calcium antagonists:

    Hypotensive behavior (typical for similar dihydropyridine, phenylalkylamine, benzothiazepine)

    Antianginal (characteristic of similar dihydropyridine, phenylalkylamine, benzothiazepine)

    Antiarrhythmic effect (typical for verapamil and diltiazem preparations).

Preparations, which belong to different groups, are considered for the manifestation of their disease on the heart on the peripheral suture. So, dihydropyridine AK is more important on the judge, and therefore the stink may be more pronounced hypotensive diabetic, and practically do not add to the conduction of the heart and to its transient function. Verapamil may be very tropic to calcium channels of the heart, in connection with which veins change the strength and frequency of the heart rate, worse AV conduction and less blood pressure on the judge, therefore, the hypotensive effect of the expressions is less, lower in dihydropyridine AK. Diltiazem is on the heart of that judge of the equal world. The shards of verapamil and diltiazem are similar to each other, they are mentally united in a subgroup of non-dihydropyridine AKs. At the boundaries of the skin group AK, preparations and short doses are seen prolongation preparations.

In Denmark, AK is one of the main classes of medicinal preparations, which can be used for cob therapy of hypertension. Based on recent studies (ALLHAT, VALUE), prolongation of AK showed a hypotensive effect that enhances the antihypertensive activity of ACE inhibitors, angiotensin II receptor antagonists, diuretics and β-adrenergic blockers. The maximum decrease in arterial pressure with the use of AK is indicated for low-level, volume AH. AK in combination with other antihypertensive drugs (ACE inhibitors, diuretics and β-adrenergic blockers) does not only have a similar hypotensive effect, but it also reduces the frequency of "great cerebrovascular complications" - myocardial infarction, cerebral infarction. Hypertrophy of the myocardium of the left duct (LS) is an independent risk factor in arterial hypertension. AK reduces LSH hypertrophy, improves diastolic function, especially in patients with arterial hypertension and IXC. An important aspect of the organoprotective action of AK is the advancement or improvement of remodeling of the vessels (the thickness of the vessel wall decreases, the endothelial-deposit vasodilation improves due to the increase in NO production).

Particularly necessary in the treatment of hypertension in patients with cerebrovascular diabetes (CD), because they have a particularly great risk of cardiovascular complications. In case of increased AH and CD, the optimal antihypertensive drug is responsible not only for the achievement of healthy AT values, but also for the manifestation of organoprotective power and being metabolically neutral. Prolongation of dihydropyridine AKs (felodipine, amlodipine and others), in the order of ACE inhibitors and ARBs, drugs of choice in the treatment of hypertension in patients with CD, since stink does not only effectively reduce AT, but may be shown by the authorities in that organoprotective nephroprotective effect (changes in the severity of microalbuminuria, improves the progress of diabetic nephropathy), as well as metabolically neutral. In a large number of patients with arterial hypertension, the CD of the target level of AT can only be reached with a combination of antihypertensive drugs. The most rational in this clinical situation is the combination of AK with ACE inhibitors and ARBs. In Denmark, it has been repeatedly shown (ASCOT–BPLA) that the use of drugs for the treatment of hypertension with favorable metabolic effects or metabolically neutral ones reduces the risk of developing CD by 30% compared with other antihypertensive drugs (thiazide diuretics, β-adrenergic blockers). The results of these studies are known in the European Clinical Recommendations for the treatment of hypertension. So, when treating hypertension in patients with a high risk of development of CD (excessive family history of CD, obesity, impaired glucose tolerance), it is recommended to take vicorist preparations with a favorable metabolic profile (for example, prolongation of AC, ACE inhibitor or ARA).

Shown:

    IXC (angina pectoris)

    AH in summer ailments

    Sistolichna AG

    AH and damage to peripheral arteries

    AH and atherosclerosis of the carotid arteries

    AG on aphids COPD and BR.

  • AH in women

    AH and supraventricular tachycardia*

    AH and migraine*

Contraindication:

    AV block II-III stage*

* - only for non-hydropiridine AK

Prominent contraindications:

* - only for non-hydropiridine AK

Effective combinations

In the majority of BA patients, it was shown that in 70% of patients with AD, in order to achieve high levels of AT, a combination of two or three antihypertensive drugs is necessary. Among the combinations of two drugs, effective and safe are:

    ACE inhibitor + diuretic,

    BAB + diuretic,

    AK + diuretic,

    sartani + diuretic,

    sartani + ACE inhibitor + diuretic

    AK + ACE inhibitor,

Pid hypertensive crisis rozumіyut usі vypadki raptovoy and significant rise of AT, which are accompanied by the appearance or potentiation already іsnuyuchoї cerebroї, kardialі chi zagalnovegetativnoї symptomatology, rapid progression of disruption of the functions of the life of important organs.

Criteria for a hypertensive crisis:

    shodo raptovy cob;

    individually high pidyom AT;

    the appearance of a stronger skarg of a cardial, cerebral chi of a vegetative nature.

In the United States, that European wide-width nabula is easy to choose the tactics of managing a sick clinical classification, in such a hypertensive crisis, it is divided into complications and inconveniences.

    Aggravation of hypertensive crises are characterized by gostrim or progressive damage to target organs (POM), become a direct threat to the life of the ailing and the negative, stretching for 1 year, lowering the arterial pressure.

    Uncomplicated hypertensive crises there is no sign of a severe or progressive POM, to become a potential threat to the life of an ailing person, to increase the speed of a short period of time, a decrease in AT.

Celebration of hypertensive crises

In case of medical treatment of hypertensive crises, it is necessary to overcome the upcoming problems:

        Cupping of the rise of AT. When choosing the next step of terminology on the cob of glee, choose the drug and the method of its introduction, establish the necessary level of reduction in arterial pressure, determine the level of permissible reduction in arterial pressure.

        Ensuring adequate control over the camp of the patient for an hour of lowering AT. It is necessary to have a proper diagnosis due to the aggravation of an overworld decrease in the arterial pressure.

        Consolidation of the achieved effect. For whom you should prescribe the same drug, for the help of which the arterial pressure is lowered, in case of impossibility - other hypotensive symptoms. The hour is determined by the mechanism and terms of the selected preparations.

        Lіkuvannya uskladnen that accompanying illnesses.

        Optimum dosing of medicinal preparations for drug treatment.

        Carrying out preventive visits to avoid crises.

Antihypotensive drugs.

Antihypotensive drugs are a group of drugs that can be used to restore normal arterial pressure to normal. Severely falling arterial pressure (collapse, shock) can be caused by blood loss, trauma, trauma, infectious diseases, heart failure, and other. In addition, chronic hypotension may develop as an independent illness. For the elimination of arterial hypotension, the following drugs should be used:

    increase the volume of circulating blood - plasma pumps, salts;

    sudinozvuzhuvalnі zabob (caffeine, cordiamine, alpha-adrenomimetics, glucocorticoid, mineralcorticoid, angiotensinamide);

    to improve tissue microcirculation and reduce hypoxia - ganglion blockers, a-blockers;

    non-glycoside cardiotonics (dobutamine, dopamine);

    make sure that you give a tonic effect on the central nervous system - tinctures of lemongrass, ginseng, lure, aralia; extracts of eleutherococcus and rhodiola erysipelas.

Preparations, yakі zastosovuyt in uncomplicated hypertensive crises

Preparations

Dose and method

Introduction

dії

Side effects

Captopril

12.5-25 mg orally or sublingually

After 30 min.

Hypotension is orthostatic.

Clonidine

0.075-0.15 mg intravenously or 0.01% retail 0.5-2 ml intravenously or intravenously

After 10-60 min.

Dry mouth, drowsiness. Contraindications are ailing from AV blockade, bradycardia.

propranolol

20 - 80 mg orally

After 30-60 min.

Bradycardia, bronchoconstriction.

1% - 4-5 ml intravenously

0.5% - 8-10 ml intravenously

After 10-30 min.

More effective in combination with other antihypertensive drugs.

Nifedipine

5-10 mg orally or

sublingually

After 10-30 min.

Headache, tachycardia, redness, possible development of angina pectoris.

Droperidol

0.25% 1 ml intravenously or intravenously

After 10-20 min.

Extrapyramidal lesions.

Parenteral therapy for complicated hypertensive crises

Naming the drug

Method of administration, doses

Cob dії

Trivality dії

Note

Clonidine

intravenously 0.5-1.0 ml 0.01%

or internally 0.5-2.0 ml 0.01%

After 5-15 min.

Not recommended for brain stroke. Possible development of bradycardia.

Nitroglycerin

intravenously drip 50-200 mcg / min.

After 2-5 min.

Especially indications for acute heart failure, IM.

Enalapril

intravenously 1.25-5 mg

After 15-30 min.

Effective in acute insufficiency of LS.

Nimodipin

After 10-20 min.

With subarachnoid hemorrhages.

Furosemide

IV bolus 40-200 mg

After 5-30 min.

It is important for hypertensive crises due to severe heart failure.

propranolol

0.1% in 3-5 ml in 20 ml physiological order

After 5-20 min.

Bradycardia, AV block, bronchospasm.

Magnesium sulfate

IV bolus 25% solution

After 30-40 min.

With sudomas, eclampsia.

Name the drug, yoga synonyms, understand the safety and order of admission from pharmacies

Release form (warehouse), quantity of the drug in the package

Method of admission, average therapeutic dose

Clonidine (clonidine)

(List B)

Tablets 0.000075 and 0.00015 N.50

1 tablet 2-4 times per doba

Ampoules 0.01% retail 1 ml N.10

Pid shkir (in m'yaz) 0.5-1.5 ml

In a vein, 0.5-1.5 ml per 10-20 ml of 0.9% sodium chloride up to 3-4 times per day (in the minds of a hospital)

          Moxonidine (Physiotens)

(List B)

Walks by 0.001

1 tablet 1 time per dose

Methyldopa (additional)

(List B)

Walks of 0.25 and 0.5

1 tablet 2-3 times per doba

Reserpine (rosusidil)

Walks by 0.00025

1 tablet 2-4 times per day

(List B)

Ampoules 0.25% retail 1 ml N.10

In m'yaz (at the vein is povilno) 1 ml

Prazosin (minipres)

(List B)

Walks 0.001 and 0.005 N.50

½-5 tablets 2-3 times per doba

Atenolol (tenormin)

(List B)

Walks of 0.025; 0.05 and 0.1 N.50, 100

½-1 tablet 1 time per dose

Bisoprolol

(List B)

Walks by 0.005 and 0.001

1 tablet 1 time per dose

Nifedipine (Phenigidine, Korinfar)

(List B)

Tablets (capsules, dragees) 0.01 and 0.02 each

1-2 tablets (capsules, dragees) 3 times per doba

Sodium nitropruside

Natrii nitroprussidum

(List B)

Ampoules of 0.05 dry speech N.5

In a vein drip 500 ml of 5% glucose solution.

Captopril (capoten)

(List B)

Walks by 0.025 and 0.05

½-1 tablet 2-4 times a day

Magnesium sulfate

Magnesii sulfas

Ampoules 25% retail 5-10 ml N.10

In m'yaz (at the vein it is enough) 5-20 ml

"Adelfan"

(List B)

Official walks

½-1 tablet 1-3 times per doba (once later)

"Brinerdin"

(List B)

Official dragee

1 dragee 1 time per doba (vranci)

Preparations with important therapeutic effects are widely sought after by specialists. The stench zastosovuetsya for the treatment of cardial diseases, as the most common among other pathologies. Most of the illnesses lead to the death of patients. Lіkami, yakі need for likuvannya tsikh zahvoryuvan, є beta-blockers. The list of drugs by class, which consists of 4 divisions, and their classification is presented below.

Classification of beta-blockers

The chemical composition of the budova preparations in the class is heterogeneous and in the case of it there are no clinical effects. It is more important to see the specificity to the singing receptors and the sporidness to them. There is more specificity to beta-1 receptors, but less of a side effect of drug speeches. At the same time, it is rational to apply this way to the combination of cym.

First generation of drugs:

  • non-selective to beta-receptors of the 1st and 2nd types: "Propranolol" and "Sotalol", "Timolol" and "Oxprenolol", "Nadolol", "Penbutamol".

Another generation:

  • selectively to beta-receptors of the 1st type: "Bisoprolol" and "Metoprolol", "Acebutalol" and "Atenolol", "Esmolol".

Third generation:


These beta-blockers (the list of preparations is more amazing) in different hours were the main group of drugs, they were stagnant and contagious in case of ailments of the vessels and heart. Many of them, most importantly representatives of the other and the third generation, are standing up and today. Due to the effects of these pharmacological effects, it is possible to control the frequency of the heart rate and the conduction of an ectopic rhythm to the tunic, to change the frequency of angina attacks of angina pectoris.

Explanation before classification

The most early faces are representatives of the first generation, so non-selective beta-blockers. The list of drugs and preparations of representations is higher. These drugs can block receptors of the 1st and 2nd types, giving both a therapeutic effect and a side effect, which manifests itself as bronchospasm. Therefore, stench is contraindicated in COPD, bronchial asthma. The most important drugs of the first generation are: "Propranolol", "Sotalol", "Timolol".

Among the representatives of another generation, a list of drugs for beta-blockers has been compiled, the mechanisms of which are some of the effects of the most important blocking of receptors of the first type. The stench is characterized by a weak sporidity to type 2 receptors, which is rarely indicated by bronchospasm in patients with asthma and COPD. The most important drugs of the 2nd generation are "Bisoprolol" and "Metoprolol", "Atenolol".

Third generation of beta-blockers

Representatives of the third generation are the most important beta-blockers. The list of drugs is compiled from Nebivolol, Carvedilol, Labetalol, Bucindolol, Celiprolol and others (divine more). The most important from the clinical point of view are: “Nebivolol” and “Carvedilol”. The first is the most important blocking of the beta-1 receptor and stimulates the vision of NO. This is due to the expansion of the vessels and the decrease in the risk of the development of atherosclerotic plaques.

It is important that beta-blockers cause heart disease, but Nebivolol is a universal drug, which is good for both purposes. However, it’s a good thing, the lower price is to be decided. Let's follow the authorities, but the cheap ones, є "Carvedilol". In addition to the power of beta-1 and alpha-blocker, which allows you to reduce the frequency and strength of the heart, as well as expand the judges of the periphery.

Qi effects allow control of chronic and hypertension. Moreover, in times of CHF, "Carvedilol" is a drug of choice, moreover, it is an antioxidant. Therefore, it is necessary to change the development of atherosclerotic plaques.

Indications for ingestion of drugs in groups

Should be indicated before the beta-blockers are prescribed, they should be taken under the influence of the power of a particular group of drugs. In non-selective blockers, the indications are higher, but also selectively benign and may be more pronounced. Shown in a flash of smoke, wanting to stink around the impossibility of congestion of faces in some patients. For non-selective drugs, the following are indicated:


Current cardiology cannot be diagnosed without preparations of the group of beta-adrenoblockers, which are known to be more than 30 at a time. Необхідність включення бета-адреноблокаторів у програму лікування серцево-судинних захворювань (ССЗ) очевидна: за останні 50 років кардіологічної клінічної практики бета-адреноблокатори зайняли міцні позиції у профілактиці ускладнень та у фармакотерапії артеріальної гіпертонії (АГ), ішемічної серцевої недостатності (ХСН), метаболічному syndromes (MS), as well as for other forms of tachyarrhythmias. Traditionally, in uncomplicated cases, medical treatment of hypertension is started with beta-blockers and diuretics, which reduce the risk of developing myocardial infarction (IM), impaired cerebral blood flow and rapt cardiogenic death.

The concept of mediated drug use through tissue receptors in various organs was proponated by N. Langly in 1905, and in 1906 by N. Langly. H. Dale confirmed it in practice.

In 90 years, it was established that beta-adrenergic receptors are subdivided into three subtypes:

    Бета1-адренорецептори, які розташовані в серці і через які опосередковуються стимулюючі впливи катехоламінів на діяльність серця - насоса: почастішання синусового ритму, покращення внутрішньосерцевої провідності, підвищення збудливості міокарда, посилення скоротливості міокарда (позитивні хроно-, дромо-, бат- ;

    Beta2-adrenergic receptors, which are most important in the bronchi, smooth lingual cells of the arterial wall, skeletal masses, and in the submucosa; with their stimulation, bronchitis, vasodilatation effects, relaxation of smooth tissues and secretion of insulin are realized;

    Beta3-adrenergic receptors, localized most importantly on adipocyte membranes, take part in thermogenesis and lipolysis.
    The idea of ​​winning beta-blockers as cardioprotectors belongs to the English J.W. The Nobel Committee recognized the clinical significance of these drugs as "the biggest breakthrough in the fight against heart diseases since the recognition of digitalis 200 years ago."

The effect of blocking the influx of mediators on the beta1-adrenergic receptors of the myocardium and the weakening of the infusion of catecholamines on the membrane adenylyl cyclase of cardiomyocytes due to changes in the concentration of cyclic adenosine monophosphate (cAMP) indicate the main cardiotherapeutic effects of beta-blockers.

Anti-chemic effect of beta-blockers explained by the decrease in consumption of the myocardium in the heart, in the event of a change in the frequency of heart rates (HR) and the strength of the heart rates, which is due to blocking of beta-adrenergic receptors in the myocardium.

Beta-blocker is once to forget the painting of the perfusion of the miracard for the zhunky kinsevo di-tape in a long slate (LS) of the zbizhnnya of Gradiynta, the vicinity of the coronarna of the pyd dijoye.

Antiarrhythmic action of beta-blockers, foundations on their zdatnosti change adrenergic influx on the heart, produce up to:

    change in heart rate (negative chronotropic effect);

    Reduced automatism of the sinus node, AV-z'ednannya and the His-Purkin system (negative bathmotropic effect);

    Shortness of trivality to the potential di and refractory period in the Hisa-Purkin system (the QT interval is shortened);

    Increased conduction in the AV-Z'ednanny and increased frivolity of the effective refractory period of the AV-Z'Dnanny, lowering the PQ interval (negative dromotropic effect).

Beta-adrenergic blockers increase the threshold of tympanic fibrillation in patients with host IM and may be seen as a prevention of fatal arrhythmias in the acute period of IM.

Hypotensive diya beta-blockers

    Changes in the frequency and strength of the heart sooner (negative chrono- inotropic diya), which can lead to a decrease in mild heart failure (MOS);

    Decreased secretion and changes in plasma renin concentration;

    Perebudovoy baroreceptor mechanisms of the aortic arch and carotid sinus;

    Central prinychennyam sympathetic tone;

    Blockade of postsynaptic peripheral beta-adrenergic receptors in the venous vascular bed, changes in blood flow to the right heart valves and decreased MOS;

    Competitive antagonism to catecholamine for receptor binding;

    Increased level of prostaglandins in the blood.

Preparations from the group of beta-blockers are considered for the presence or absence of cardioselectivity, intrinsic sympathetic activity, membrane-stabilizing, vasodilatory powers, variability in lipids and water, influencing the aggregation of platelets, and also for platelets.

Influx on beta2-adrenergic receptors signifies a significant part of side effects and contraindications up to their congestion (bronchospasm, ringing of peripheral vessels). The peculiarity of cardioselective beta-blockers in the case of non-selective ones is greater sporidity to beta1-receptors in the heart, lower to beta2-adrenergic receptors. Therefore, when vikoristannі in small and medium doses qі preparations may be less pronounced by injecting into the smooth muscles of the bronchi and peripheral arteries. It should be noted that the ratio of cardioselectivity is not the same in different drugs. The index ci/beta1 to ci/beta2, which characterizes the degree of cardioselectivity, becomes 1.8:1 for non-selective propranolol, 1:35 for atenolol and betaxolol, 1:20 for metoprolol, 1:75 for bisoprolol (Bisogama). However, bearing in mind that the selectivity is dose-dependent, it decreases with increasing doses of the drug (Fig. 1).

At this time, clinicians see three generations of drugs with a beta-blocking effect.

I generation - non-selective beta1- and beta2-adrenergic blockers (propranolol, nadolol), which, in a series of negative ino-, chrono-dromotropic effects, can improve the tone of the smooth muscles of the bronchi, the vessel wall, myometrium, and so on.

II generation - cardioselective beta1-adrenergic blockers (metoprolol, bisoprolol), high selectivity for beta1-adrenergic receptors in the myocardium may be more tolerable in case of trivial congestion and proving the base of long-term prognosis of life with likuvanni AH.

In the mid-1980s, third-generation beta-adrenoblockers appeared on the world pharmaceutical market with low selectivity to beta1, 2-adrenergic receptors, but with a reduced blockade of alpha-adrenergic receptors.

III generation drugs - celiprolol, bucindolol, carvedilol (yogo generic analogue with the brand name Carvedigamma®) may have additional vasodilating power over the blockade of alpha-adrenergic receptors, without internal sympathomimetic activity.

In 1982-1983, the scientific medical literature published the first reports about the clinical record of carvedilol stagnation and CVD treatment.

A number of authors have shown a protective action of third-generation beta-blockers on cellular membranes. This is explained, first, by the inhibition of lipid peroxidation (LPO) processes of membranes and by the antioxidant effect of beta-blockers and, in other words, by the decrease in the intake of catecholamines on beta receptors. Deyakі authors pov'yazuyut membrane-stable action of beta-blockers with a change in the conductivity of sodium through them and inhibition of lipid peroxidation.

Зазначені додаткові властивості розширюють перспективи застосування цих лікарських засобів, оскільки нівелюють характерний для перших двох поколінь негативний вплив на скорочувальну функцію міокарда, вуглеводний та ліпідний обмін і водночас забезпечують покращення перфузії тканин, позитивний вплив на показники гемостазу та рівень оксидативних процесів.

Carvedilol is metabolized in the liver (glucuronidation and sulfation) for the support of the cytochrome P450 enzyme system, with the other enzyme families - CYP2D6 and CYP2C9. Antioxidant activity of carvedilol and its metabolites is present in the molecules of the carbazole group (Fig. 2).

Metabolisms of carvedilol - SB 211475, SB 209995 reduce LPO in 40-100 times more active, lower the drug itself, and vitamin E - approximately 1000 times more.

Injection of carvedilol (Carvedigami®) in the treatment of IXC

Based on the results of a number of completed bugatocentric studies, beta-adrenergic blockers may have an anti-chemic effect. It should be noted that the anti-chemic activity of beta-adrenergic blockers can be compared with the activity of calcium antagonists and nitrates, ale, for the administration of these groups, beta-blockers not only improve the quality, but also improve the vitality of life. Based on the results of a meta-analysis of 27 rich-centered studies, in which over 27 thousand took part. osib, selective beta-blockers without internal sympathomimetic activity in patients with a history of hostile coronary syndrome reduce the risk of developing recurrent MI and mortality in a heart attack by 20%.

However, not only selective beta-blockers positively affect the nature of the overshoot and the prognosis in patients with IXC. The non-selective beta-blocker carvedilol has also demonstrated good efficacy in patients with stable angina pectoris. The high anti-chemic efficacy of this drug is explained by the presence of additional alpha1-blocking activity, which causes dilatation of the coronary vessels and collaterals in the post-stenotic area, and therefore - a decrease in myocardial perfusion. In addition, carvedilol may cause an antioxidant effect, induces the ingestion of free radicals, which are viable during the period of ischemia, which may lead to an additional cardioprotective effect. At one hour, carvedilol blocks apoptosis (programmed death) of cardiomyocytes in the area of ​​ischemia, preserving the functioning of the myocardium. As shown, the carvedilol metabolite (BM 910228) has a lesser beta-blocking effect, but it is also an active antioxidant, blocking lipid peroxidation, and “enhancing” active free radicals OH-. This derivative preserves the inotropic effect of cardiomyocytes on Ca++, the intracellular concentration of such cardiomyocytes is regulated by the Ca++ pump of the sarcoplasmic reticulum. Therefore, carvedilol appears to be more effective in treating myocardial ischemia due to the inhibition of free radicals on lipid membranes of subcellular structures of cardiomyocytes.

Due to the unique pharmacological powers of carvedilol, it can override traditional beta1-selective blockers in terms of myocardial perfusion expansion and preservation of systolic function in patients on ICS. As shown by Das Gupta et al., in patients with LS dysfunction and heart failure, which developed after IXC, carvedilol monotherapy reduced the pressure on the side, and also increased the fraction of HF (LV) and improved the hemodynamic parameters of the bradycardia, with no development.

Based on the results of clinical studies in patients with chronic stable angina pectoris, carvedilol reduces heart rate at rest during physical exertion, and also increases EF in calm. Equal studies of carvedilol and verapamil, in which 313 patients took part, showed that, compared with verapamil, carvedilol significantly changed heart rate, systolic AT and increased HR ´ AT with maximally tolerated physical stress. Moreover, carvedilol has a more favorable tolerability profile.
It is important that carvedilol may be effective in the treatment of angina pectoris, lower than beta1-blockers. Thus, in the course of a 3-month randomized bagatocentric subvariant blind follow-up, carvedilol was directly compared with metoprolol in 364 patients with stable chronic angina pectoris. They took carvedilol 25-50 mg orally per doba or metoprolol 50-100 mg orally per doba. At that time, both drugs demonstrated good antianginal and protischemic effects, carvedilol significantly increased the hour to ST segment depression by 1 mm with physical stress, lower metoprolol. The tolerability of carvedilol was even worse, and, importantly, with an increase in the dose of carvedilol, no significant changes were observed in the types of non-negligible manifestations.

It is noteworthy that carvedilol, which is not a drug, has an effect on other beta-blockers, cardiodepressive disease, improving the quality of life and life expectancy of patients from hospital IM (CHAPS) and post-infarction ischemic dysfunction of LSH (CAPRICO). Rich data were collected during the Carvedilol Heart Attack Pilot Study (CHAPS), a pilot study of carvedilol injection into IM development. This was the first randomized study in which carvedilol was compared with placebo in 151 patients with acute IM. The treatment was started 24 years after the onset of pain in the chest, and the dose of the drug was increased to 25 mg of the drug per doba. The main endpoints of the study were the function of LSH and the safety of the drug. The ailments were guarded for 6 months from the cob of illness. Zgіdno z otrimanimi dannymi, the frequency of development of serious cardiac events has changed by 49%.

Withdrawal during the follow-up of CHAPS echographic data of 49 patients with decreased EF LS (< 45%) показали, что карведилол значительно улучшает восстановление функции ЛЖ после острого ИМ, как через 7 дней, так и через 3 месяца. При лечении карведилолом масса ЛЖ достоверно уменьшалась, в то время как у пациентов, принимавших плацебо, она увеличивалась (р = 0,02). Толщина стенки ЛЖ также значительно уменьшилась (р = 0,01). Карведилол способствовал сохранению геометрии ЛЖ, предупреждая изменение индекса сферичности, эхографического индекса глобального ремоделирования и размера ЛЖ. Следует подчеркнуть, что эти результаты были получены при монотерапии карведилолом. Кроме того, исследования с таллием-201 в этой же группе пациентов показали, что только карведилол значимо снижает частоту событий при наличии признаков обратимой ишемии. Собранные в ходе вышеописанных исследований данные убедительно доказывают наличие явных преимуществ карведилола перед традиционными бета-адреноблокаторами, что обусловлено его фармакологическими свойствами.

The good tolerance and anti-remodeling effect of carvedilol is indicated by those who have been able to reduce the risk of death in patients who have had IM. A large-scale study of CAPRICORN has been attributed to the use of carvedilol in the management of LSH dysfunction after IM. The CAPRICORN study has previously demonstrated that carvedilol in combination with ACE inhibitors has been shown to reduce global and cardiovascular mortality as well as the rate of recurrent non-fatal heart attacks in this group of patients. New evidence that carvedilol, although less so, is no more effective in remodeling in patients with CHF and ICS, supports the need for early recognition of carvedilol in myocardial ischemia. In addition, due to special respect, the drug is given to the “sleeping” (hibernating) myocardium.

Carvedilol in curative AG

The role of disrupted neurohumoral regulation in the pathogenesis of arterial hypertension is not evident today. Offending the main pathogenetic mechanisms of hypertension - an increase in the cardiac outlet and an increase in the peripheral vascular support - are controlled by the sympathetic nervous system. Therefore, beta-blockers and diuretics have long been the standard of antihypertensive therapy.

In the recommendations of JNC-VI, beta-blockers were considered as first-line drugs for uncomplicated forms of hypertensive disease, but in the control clinical studies, the bula was brought to a lesser level of beta-blockers and diuretics to reduce cardiovascular mortality and disease. Apparently, until the results of a meta-analysis of previous studies of BA-blockers, beta-blockers did not show the effectiveness of reducing the risk of stroke. The negative metabolic effects and peculiarities of the impact on hemodynamics did not allow them to also occupy an important place in the process of changing the remodeling of the myocardium and vessels. Only representatives of another generation of beta-blockers — atenolol, metoprolol — were included in the meta-analysis and did not include data on new drugs. With the appearance of new representatives in this group of a significant world, the insecurity of their congestion in ailments with impaired heart conduction, circulatory diabetes, impaired lipid metabolism, and nirk pathology was leveled. The zastosuvannya of the same drugs allows you to expand the scope of zastosuvannya beta-blockers in hypertension.

The most promising in the treatment of patients with arterial hypertension with other representatives of the class of beta-blockers - drugs and vasodilating powers, one of them is carvedilol.

Carvedilol may treat hypotensive effects. Based on the results of a meta-analysis of the hypotensive effect of carvedilol, more lower in 2.5 ths. ill for arterial hypertension, AT decreases after a single dose of the drug, the maximum hypotensive effect develops after 1-2 days. In this case, data on the effectiveness of the drug in different age groups have been obtained: no reliable results in the presence of AT against the background of a 4-year intake of carvedilol at a dose of 25 or 50 mg in patients with age up to 60 years have not been established.

It is important that the fact that in the presence of non-selective and other beta1-selective adrenoblockers, beta-blockers with vasodilating activity not only does not reduce the sensitivity of tissues to insulin, but also affects the trochi. Carvedilolu is a Zmenshuvati ilnsuli-resistance-an ethnicity, which is great with the gigor of the thumbnails of beta1-adrenal-bold active, and the vitality of Lipoprotean, the vibrants of the roller, the roller Comparison of the effects of various beta-blockers confirms this concept. Thus, a randomized follow-up was prescribed carvedilol and atenolol for type 2 diabetes and AH. It was shown that after 24 days of therapy, the levels of blood sugar and insulin levels decreased with treatment with carvedilol, and increased with treatment with atenolol. In addition, carvedilol had a greater positive effect on sensitivity to insulin (p = 0.02), high lipid levels (p = 0.04), triglycerides (p = 0.01), and lipid peroxidation (p = 0.04).

Apparently, dyslipidemia is one of the most important factors in the risk of developing CVD. Particularly unfriendly є poddnannya її s AG. However, taking certain beta-blockers can lead to significant changes in blood lipid levels. As it was guessed, carvedilol does not give a negative infusion of grayish rhubarb lipids. In a bagatocentric blind randomized patient, carvedilol was administered to the lipid profile in patients with mild AH and dyslipoproteinemia. The study included 250 patients who were randomly assigned to carvedilol at a dose of 25-50 mg per dose or ACE inhibitor captopril at a dose of 25-50 mg per dose. The choice of captopril for the improvement was indicated, because the wine either does not have an effect, or positively contributes to the exchange of lipids. The trivality of rejoicing became 6 months. In both groups, positive dynamics was noted: both drugs and equally improved the lipid profile. The favorable effect of carvedilol on lipid metabolism, more than anything else, associated with alpha-adrenergic blocking activity, it was shown that the blockade of beta1-adrenergic receptors induces vasodilation, resulting in improved hemodynamics, as well as changes.

Blockade of beta1-, beta2- and alpha1-receptors, carvedilol may also have additional antioxidant and antiproliferative powers, which is important to protect the risk factors of CVD and the safety of infection of target organs in patients with hypertension.

Thus, the metabolic neutrality of the drug allows for widespread use in patients with arterial hypertension and diabetes mellitus, as well as in patients with MS, which is especially important in cases of mild age.

Alpha-blocking and antioxidant dicarvedilol, which prevent peripheral and coronary vasodilation, administer the drug to the parameters of central and peripheral hemodynamics, showed a positive effect on the drug fraction and stroke volume of LS, which is especially important in treating AH patients.

As you can see, arterial hypertension often occurs with irritants, and when choosing antihypertensive therapy, it is necessary to protect the possibility of injecting a drug into the functional state of the drug. Stasis of beta-blockers in the majority of depressions may be associated with changes in nirk blood flow and glomerular filtration rate. The presence of beta-adrenergic blocking effect in carvedilol and the safety of vasodilation, as shown, positively affects the function of nirok.

In this way, carvedilol in its beta-blocking and vasodilatory power, which ensures its effectiveness in the treatment of arterial hypertension.

Beta-blockers in the treatment of CHF

CHF is one of the most unacceptable pathological conditions, which significantly worsen the quality and triviality of the life of ailments. The breadth of heart failure is even greater, the most common diagnosis in patients from 65 years of age. In this hour, there is a trend towards an increase in the number of patients with CHF, which leads to improved survival in other CVDs, which is similar to those in severe forms of IXC. According to WHO data, 5-day survival of patients with CHF does not exceed 30-50%. In a group of patients who have had IM, up to 50% die due to the first fate after circulatory insufficiency associated with coronary heart disease. Therefore, the most important task for optimizing therapy for CHF is the search for drugs, which will improve the life of patients with CHF.

One of the most promising classes of drugs, effective both for the prevention of development, and for the treatment of CHF, the recognition of beta-adrenergic blockers, and the activation of the sympathoadrenal system are one of the leading pathogenetic mechanisms for the development of CHF. Compensatory, at the cob stages of illness, hypersympathicotonia in the future is the main cause of myocardial remodeling, increased trigger activity of cardiomyocytes, increased peripheral vascular support and damage to perfusion of target organs.

The history of beta-blockers in the treatment of ailments for CHF is 25 years old. Large-scale international studies CIBIS-II, MERIT-HF, US Carvedilol Heart Failure Trials Program, COPERNICUS have validated as first-line beta-blockers for the treatment of CHF patients, confirming their safety and efficacy in the treatment of such ailments (Table). Метааналіз результатів основних досліджень з вивчення ефективності бета-адреноблокаторів у хворих з ХСН показав, що додаткове призначення до інгібіторів АПФ бета-адреноблокаторів, поряд з покращенням гемодинамічних показників та самопочуття пацієнтів, сприяє покращенню перебігу ХСН, показників якості життя1, знижує частоту % та ризик смерті ailments for CHF by 37%.

According to the European recommendations of 2005, the use of beta-blockers is recommended in all patients with CHF for addition to therapy with ACE inhibitors and symptomatic treatment. Moreover, according to the results of the COMET multicenter follow-up, it was the first direct trial of the injection of carvedilol and the second generation selective beta-blocker metoprolol at doses that provide an equivalent antiadrenergic effect, for survival in the middle term, 17%.

It ensured the average "winning" in the rozrahunkovyi carelessness of life by 1.4 years in the carvedilol group for the maximum carelessness of patients up to 7 years. Carvedilol was indicated for its cardioselectivity and apparent alpha-blocking effect, which caused a change in hypertrophic myocardial condition to norepinephrine, a decrease in peripheral vascular support, and an increase in renina sway. In addition, in clinical trials in patients with CHF, an antioxidant, protizapal (reduction in the level of FNP-alpha (swelling necrosis factor), interleukin 6-8, C-peptide), antiproliferative and antiapoptotic activity of the drug, as among the preparations in their own, and in the third groups.

On fig. Figure 3 shows a dose titration scheme for carvedilol in various pathologies of the cardiovascular system.

Thus, carvedilol, with its beta- and alpha-adrenergic blocking effect with antioxidant, protizapal, antipoptotic activity, is among the most effective drugs in the class of beta-adrenoblockers, and can be found in the early stages of treatment of CVD and MS.

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A. M. Shilov
M. V. Melnik*, Doctor of Medical Sciences, Professor
A. Sh. Avshalumov**

*MMA im. I. M. Sechenova, Moscow
**Clinic of the Moscow Institute of Cybernetic Medicine, Moscow