Cardioselective beta 1 adrenergic blockers. Beta-adrenergic blockers of the 3rd generation in the lykuvanny of the heart-vascular disease

In lіkuvanni ailments of the heart and sudin an important role is played by adrenergic blockers. Tse drugs that drive adrenergic receptors to the robot, so that they allow the pain of venous pains to be prevented, high vise and normalization of the heart rhythm.

For the elimination of the heart and the fever of the disease, the adrenergic blockers

What are the adrenergic blockers?

Adrenoblockers (adrenolytics)- group medications They infuse adrenergic impulses into the vertebral walls and tissues of the heart, which react to adrenaline and norepinephrine. The mechanism of the polyagus is that the stench blocks the adrenergic receptors themselves, the therapeutic effect required for heart pathologies can be reached:

• the grip decreases;
• expand enlightenment in ships;
• zukor change in blood;

Adrenolytics are viral against adrenaline and norepinephrine, so that they are antagonists. This will allow not to allow critical indicators in a vice in case of hypertension and improvement of heart pathologies (arrhythmia, atherosclerosis, hypertension, ischemia, infarction, deficiency, defects).

Classification of drugs in adrenolitics

Recipes, rosted in the vessels and smooth muscles of the heart, are subdivided into alpha-1, alpha-2, beta-1, beta-2.

Also, as adrenergic impulses need to block the development of 3 main groups of adrenocytes:

• alpha blockers;
• beta blockers;
• alpha beta blockers.

The skin group is driven as soon as it appears, as it detects robots and specific receptors (beta, alpha, or one hour alpha-beta).

Blockers alpha adrenergic blockers

Alpha adrenergic blockers can be of 3 types:

• leaks, scho block alpha-1 receptor;
• medications that are injected into alpha-2 impulses;
• Combined drugs, at the same time blocking alpha-1,2 pulses.

The main group of alpha-blockers

Pharmacology of drugs in a group (mainly alpha-1 blockers) - improvement of education in veins, arteries and capillaries.

Tse allow:

• lowering the definitions of the verdict;
• change the vice;
• minimizuvati on the heart and leave the robot;
• lowering the steps of stealing the walls of the livin 'louse;
• normal fatty;
• stabilizes carbohydrate metabolism (increases sensitivity to insulin, normalizes sugar in plasma).

Blockers of alpha-2 receptors are less effective in the treatment of pathologies of the heart, as they have a weak therapeutic effect. The stench is well recommended in urology. Such preparations are often used in cases of malfunctioning of statovykh functions in choloviks.

Table "Overflow of short alpha adrenergic blockers"

Sered alpha adrenergic blockers of the new generation of high efficiency Tamsulozin. Yogo vikoristovuyu with prostatitis, so as a good way to reduce the tone of soft tissues in front of the throat, normalize the symptoms and reduce the symptoms of good prostate problems.

Likki are well tolerated by the body, but there are fewer effects:

• blues, diarrhea;
• zapamorochennya, head b_l;
• accelerated sertsebitty, beating at the breasts;
• allergic visip, undead.

beta adrenoblockers

Pharmacology of the preparations in the group of beta blockers in polyaga is in the fact that the stench overwhelms the stimulation with adrenaline beta1 or beta1.2 impulses. This is the way to bring about a very fast heart and bring a great virus of blood, and also does not allow a rapid expansion of the bronchial education.

All beta adrenergic blockers are divided into 2 groups - selective (cardioselective, antagonism of beta-1 receptors) and nonselective (blocking adrenaline at once in two strands - beta-1 and beta-2 pulses).

Mechanism of beta-blockers

Victory of cardioselective drugs in the treatment of heart pathologies allows one to seek an offensive therapeutic effect:

• to decrease the level of the heart rhythm (decrease the risk of tachycardia);
• the frequency of attacks of angina pectoris will speed up, smoothen inappropriate symptoms ailments;
• The strength of the heart system is improved to emotional, mental and physical options.

The reception of beta blockers allows the normalization of the patient's zagalny camp, who suffers from heart damage, and also reduces the risk of hypoglycemia in diabetics, does not allow rapid bronchial spasm in asthmatics.

Nonselective adrenergic blockers to change the abdominal cavity of the peripheral blood stream and infuse on the tone of the walls, which is:

• decreased heart rate;
• normalization of the vice (with hypertension);
• a decrease in the speed of feeling activity of the myocardium and an increase in stiffness to hypoxia;
• for arrhythmia recovery for the reduction of malignancy in the provincial system of the heart;
• the uniqueness of the gross destruction of the bloody beast in the brain.

Stagnation of nonselective beta adrenergic blockers gives the possibility of a thrombus development in vessels and a decrease in the rate of an infarction, causing an organism's stiffness to a variety of conditions. Prior to that, such preparations will push the tone of the uterus, intestines, the drainage system and slowly infuse on sechovy mikhur(Relax the sphinkter).

Table "List of the most effective drugs for blocking adrenaline on beta impulses"

Krym synthetic beta-blockers, and natural substitutes. Naybilsh effective vvazayutsya Passionflower. The drug is a natural relaxant of oily tissues, a good noxious and tranquilizer for patients with a sleep and a sleepy toughness, and a pleasant feeling.

All those guilty are taken by the doctor for the reasons of individual peculiarities to the organism of the patient and the severity of the illness. Failure to control the reception of arenoblockers can destroy the camp of the sick, right up to the heart.

Alpha beta blockers

Lykarsky speeches of a group of groups live at once on all types of receptors in the walls of the sudins, hearts and soft tissues of their organs.

Victory of such drugs gives the ability to reach a high therapeutic effect in the treatment of important damages in the robot's heart and sudin:

• the vice (arterial and internal) decreases;
• normalize daily exchange;
• the speed of the heart grows faster (the size of the body changes, the rhythm improves, the patient's camp lays down with lack of heart or vices).

Hybrid alpha-beta adrenoblockers

Carvedilol, Labetalol and Methiloxadiazole are used by the new generation.

Їx priznachayut with such stuns, yak:

• hypertension;
• arrhythmia;
• glaucoma (open skin);
• vrodzheni and nabuti wadi sertsya;
• the deterioration of the functions of the heart is chronic in nature.

As a counter-indication, as all groups of adrenocytes may not be able to receive alpha-beta blockers, it is not possible to use an alpha-beta blocker for insulin-dependent diabetics, patients with obstructive illnesses, as well as people who are in danger of seeing two people.

mid side effects, Yak viklikayut medications pidgrupy, see:

• blockade of heart impulses or serioznі vіdhilennya in їkh provіdnostі;
• zboi in peripheral blood loss;
• changes in blood indicators in bik admission (increase bilirubin, glucose, cholesterol);
• reduction of large blood cells in plasma (leukocytes) and non-nuclear cells (thrombocytes);
• shedding bloody houses in the battle.

With vicious alpha-beta blockers, the number of leukocytes in the blood decreases

To prevent negative reactions, for the maximum change, it is necessary to take into account the dosage and triviality of therapy. Adrenoblokatory - serioznі medication, uncontrolled reception, which can lead to serious inheritance.

All adrenergic blockers are heart drugs, which are aimed at normalization, I will become people with serious ailments. The stench additionally helps to block adrenaline and norepinephrine adrenaline and norepinephrine into the heart receptor, which lays down the brain to the robot, stabilizes blood circulation and increases the rate of adrenal stimulation. To become stagnant in adrenalitis and in urology for the treatment of hyperplasia in front of myuroma, gynecology with the aim of preventing great blood loss, improving blood circulation in the pelvic organs.

The preparations of the group of beta-blockers are of great interest in connection with their hostile effectiveness. X stagnation with ischemic ailments of the heart meat, heart defect and singular damage to the heart.

It is not often the case that they recognize them when pathological changes the rhythm of the heart. Beta-adrenergic blockers are called lykarski zasobi, as they block developmental types (β1-, β2-, β3-) blockers for the hour of the day. The meaning of the number of words is collapsible to re-evaluate. The stench vvazhayutsya One class of medicines in cardiology, for the development of such a bullet, the Nobel Prize in Medicine was awarded.

Beta-blockers are seen selective and non-selective. You can find out about those who are selective - the function of blocking β1-adrenergic receptors. It is important to note that it doesn’t flow into the β2-adrenergic receptor. The basic information about these speeches is provided in the ts_y statty. Here you can get acquainted with the lecture classifications, as well as with preparations injected into the body. So how can you imagine selective and non-selective beta-blockers?

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

nonselective

Nonselective beta-adrenergic blockers - drugs that do not block beta-adrenergic receptors vibrating. Until then, the stink of a strong antianginal, hypotensive, antiarrhythmic and membrane stabilizing action.

Before a group of non-selective blockers, you can enter the following licenses:

• Propranolol (medicines with similar active speech :, Inderal, Obzidan);
• Bopindolol (Sandinorm);
• Levobunolol (Vistagen);
• Nadolol (korgard);
• Obunol;
• Oxprenolol (Coretal, trazikor);
• pindolol;
• sotalol;
• Thimozol (Arutimol).

The antianginal effect of this type of β-adrenergic blockers in the field is in the fact that the smell is normal and the frequency of the heart is very fast. Until then, the quickness of the myocardium will change, so step by step to reduce its consumption in pratsy. Such a rank, the blood of the heart is often held.

Such an effect of reassurance is in favor of sympathetic stimulation of peripheral vessels and associated activity of the renin-angiotensin system. Moreover, one hour sposterіgaєtsya minimizatsiya zagalny peripheral vascular support and lowering of the heart wikidu.

Non-selective blocker Inderal

And the axis of the antiarrhythmic action of these speeches is explained by the vivid arrhythmogenic factors. Deyak_ categories of cich drugs may be so called internal sympathetic activity. In other words, the stench I’ll push to stimulate the beta-adrenergic receptor.

Dani lykarski try not to alter or reduce the frequency of hearts very quickly in a calm state. Until then, the stench does not allow any increase in the amount of the rest when the physicists are victorious, for the adrenergic agonists are injected.

cardioselective drugs

See the advancing cardioselective beta blockers:

• Ormidol;
• Prinorm;
• Atenol;
• Betacard;
• Blokium;
• Catenol;
• Catenolol;
• hypotensive;
• Myocord;
• Normiten;
• Prenormin;
• Telvodin;
• Tenolol;
• Tenzikor;
• Velorin;
• Falitonsin.

As it seems, in the structures of the tissues of the human body there is a receptor, which reacts to the hormones adrenaline and norepinephrine. At the given moment, α1-, α2-, β1-, β2-adrenergic receptors are being developed. Not so long ago, boules described β3-adrenergic receptors.

The increase in the development of adrenergic receptors can be achieved by an offensive rank:

• α1- to be found in the body itself in the vessels (in the arteries, veins and capillaries), stimulation is active to produce spasm and quick advices blood grip;
• α2- vvazhayutsya "loop of a ringing negative ring" for the system of regulation of tissue tissue to the body - not talking about those who stimulate the body to lead to an instant reduction in the arterial grip;
• β1- roztashovani in the heart, and їkh stimulation to produce up to the frequency of the heart is very fast, before the need for myocardium in sour;
• β2- distribution in nirkas, stimulation of provoking bronchospasm.

Cardioselective β-blockers are active in β1-adrenergic receptors. And the axis of the non-selective, the stench is the same to block β1 and β2. At the heart of the relationship, the rest become 4: 1.

In other words, stimulation of the given organ heart-vascular system Energy is carried out mainly through β1. With quick adjustments, the dosage of beta-blockers is gradually made to a minimum of specificity. Only when used is a selective medication to block the offense of the receptor.

It is important to note that whether a beta-blocker is selective or non-selective, it will also lower the blood pressure.

However, at the same hour, cardioselective beta-blockers have less side effects... The very reason for this is a bit more stasis in case of adult maladies.

In such a rank, the stench of the smallest ymovirnistyu will provoke the manifestation of bronchospasm. It should be explained that the β2-adrenergic receptor does not interfere with the activity, and that the significant part of the organs of the body - the lungs - is displaced.

Varto respect, that selective adrenergic blockers are rather weak, not selective. Until then, the stench zbіlshuyt peripheral opіr sudin. The same zavdyak tsomu unique power These drugs are recognized for cardiology patients with severe impairment of peripheral blood circulation. In the main, there are ailments with a change in culture.

Obov'yazkovo slid respect for the fact that the medicine under the name Carvedilol does not belong to the category of cardioselective leaks.

Little is known, but it is not often the case for lowering the blood pressure and the weakening of arrhythmias. As a rule, he is victorious for the therapy of heart failure.

Beta blockers of the last generation

At present, there are three main generations of such lykarsky zasobіv. Naturally, bazhano koristuvatisya itself medicines of the rest (new) generation. It is recommended to live in three for doba.

Carvedilol 25 mg

Besides, it is not necessary to forget, but the stench is not tied to the smallest number of unnecessary side effects. Carvedilol and Celiprolol can be added to the innovated drugs. Yak said earlier young people heart meat.

Prior to non-selective trivialities, there are the following:

• Bopindolol;
• nadolol;
• Penbutolol;
• Sotalol.

And the axis to selective drugs of trivial diy is as follows:

• atenolol;
• betaxolol;
• Epanolol.

When sparing low efficacy of the opposite medication, it is important to look over the signs of the drug.

If necessary, turn to a special drug in order to win new lines. All on the right side is in the fact that it’s not easy to just don’t put on the necessary infusion on the patient’s body.

At the present moment, all the parts of the journey are seen by the likars' efforts, as the day itself has been prolonged. Smell to take revenge at your warehouse of active components, as they vivilnyayutsya step by step, extending a significant interval for an hour, smoothly pouring into the health of the patient of the cardiologist.

Faces can be even more divine, and even the least child is just not sleepy before them. In this context, everything is even more individual and lies in the singular features of the health of a sick person.

The very reason for the treatment must be carried out with accuracy and special pedantry. It is even more important to respect the beasts of honor for all the individual specialties of the organisms of the people.

Prototype

For the very reason that beta-blockers are built up so that they are injected into various organizations and systems (do not depend on a positive rank), it’s not preferable, and it’s prohibitively indicated in case of some other ailments.

Rise of unpleasant effects and fences until they are sucked without being tied with the presence of beta-adrenergic blockers in the organs and structures of the human body.

Prototype indications for medicinal products, є:

• asthma;
• symptomatic reduction of arterial vise;
• a decrease in the frequency of the heart is very fast (meaning that the heart rate of a sick person is more trustworthy);
• the important is decompensated heart failure.

Likarsky is not self-selected because of this category of preparations for the heart. It is important to remember that you can make a serious shkodi healthy for a sick person.

Prototype indications can be valid (if there is a lot of cinnamon for the process of therapy, I change the school code and if there is no need to have some defects):

• small ailments of the organs of the heart-vascular system;
• obstructively impaired organs of chronic nature;
• in individuals with a heart deficiency and confidence in the pulse, the consumption is not good, but it is not hardened;
• Diabetes mellitus;
• past the cultivation of the lower cuts.

Video by topic

Both non-selective and selective beta-blockers (preparations from these groups) are used for treatment and heart ailments:

When you get sick, if you receive beta-blockers of testimony, then you should be safe in the region. Especially females are especially prone to beating a baby and one-year-old breasts. Another important point є Raptova vіdmіna lykarsky zasobu: In any case, it is not recommended to take too much of this drug. In іnshomu vypadnu people and chekє is not supported by the phenomenon under the name "vidmini syndrome".

β-adrenergic blockers block β-adrenergic receptors in other organs and tissues, which intertwine the injection of catecholamines, producing organoprotective effects when heart-and-heart disease, Yes, the possibility of storing them in ophthalmology, gastroenterology. From the side, the systemicity is infused into the β-adrenergic receptors of the wicklica, a number of side effects. To reduce unnecessary side effects, synthesized selective β-adrenergic blockers, β-adrenergic blockers with additional vasodilating powers. The level of selectivity is to start the vibrancy of the action. Lipophilicity is a sign of overriding cardioprotective effect. best wider suckingβ-adrenergic blockers may occur in patients with ischemic ailments of the heart, arterial hypertension, chronic heart failure.

Key words:β-adrenergic blockers, selectivity, vasodilating power, cardioprotective.

TYPE I LOCALIZATION β-adrenergic receptors

β-adrenergic blockers, for which there are blocking effects on the β-adrenergic receptors of organs and tissues, stagnate in CLINIC PRACTICE From the ear of the 1960s, it may have hypotensive, antiaginal, antiischemic, antiarrhythmic and organoprotective effects.

Віdomі type 2 β-blockers - і β 2 adrenergic receptors; spіvvіdnoshennya їх is not the same in different organs and tissues. effective stimulation different typesβ-blockers are presented in table. 5.1.

PHARMACODYNAMIC DIA BLOKADI β-adrenergic receptors

Pharmacodynamic effects of the overwhelming blockade of β l adrenergic receptors є:

Change in the frequency of the heart is fast (negative chronotropic, bradycardiac effect);

Decrease in arterial grip (decrease in pislyanavantazhennya, hypotensive effect);

Control of atrioventricular (AV) conduction (negative dromotropic effect);

Decreased myocardial anxiety (negative batmotropic, antiarrhythmic);

Decrease in the speed of feeling of the myocardium (negative inotropic, antiarrhythmic);

Table 5.1

Localization and treatment of β-blockers in organs and tissues

Reducing the grip in the system of the voritnoy veni (for the reduction of the hepatic and mesenteric arterial blood flow);

Reduction of the approval of the internal work (lowering of the internal vice);

Psychotropic effects for beta-blockers that penetrate through the hematoencephalic bar (weakness, drowsiness, depression, sleeplessness, no nightmares, hallucinations, etc.);

Vidmini syndrome in the development of rapid admission of short-acting beta-blockers (hypertensive reaction, aggravated coronary insufficiency, including the development of unstable angina pectoris, gastric myocardial infarction and raptor death).

Pharmacodynamic effects of private recurrent blockade β 2 adrenergic receptors є:

Adjustment of bronchial smooth muscle tone, including extreme stepїї variability - bronchospasm;

Disruption of the mobilization of glucose from the liver into the roof of the house due to galvanization of glycogenolysis and gluconeogenesis, giving the potential for hypoglycemic activity in insulin and other hypoglycemic drugs;

Pіdvischennya gladkoї musculature tonus arterіy - arterіalna vazokonstriktsіya scho viklikaє zbіlshennya OPSS, koronarospazm, zmenshennya nirkovogo bloodstream, znizhennya krovoobіgu in kіntsіvkah, gіpertenzivnu reaktsіyu on gіperkateholamіnemіyu at gіpoglіkemії, feohromotsitomі, pіslya vіdmіni klonіdinu, pid hour operatsії abo in pіslyaoperatsіynomu perіodі.

STRUCTURE of β-adrenergic receptors І diya β-adrenergic blockade

The molecular structure of the β-blocker is characterized by the singing lasting of amino acids. Stimulation of β-blockers to the cascade of activity of G-protein, the enzyme - adenylate cyclase, the establishment of cyclic AMP with ATP for the duration of adenylate cyclase, activity of protein kinase. Pid dієyu proteїnkіnazi vіdbuvaєtsya pіdvischennya fosforilyatsії kaltsієvih kanalіv Zi zbіlshennyam Strum kaltsіyu vseredine klіtini in perіod voltage-іndukovanoї depolyarizatsії, kaltsіy-іndukovane vivіlnennya kaltsіyu of sarkoplazmotіcheskogo reticulum of pіdvischennyam rіvnya cytosolic kaltsіyu, zbіlshennya frequency now efektivnostі Venue of іmpulsu i, i sili skorochennya rozslablennya away.

Diabetics of β-blockers intertwine β-adrenergic receptors from the infusion of β-agonists, preventing negative chrono-, dromo- and batmo- and inotropes of efficacy.

power of selectivity

By the initial pharmacological parameters of β-blockers є β l-selective (cardioselective) and stages of selectivity, internal sympathomimetic activity (ICA), level of lipophilicity and membrane-stabilizing effect, additional vasodilating power, preparation.

For the development of cardioselectivity, assess the steps of the injection with the drug injected agonist β-adrenergic receptors on the frequency of heart rate, tremor of the fingers, arterial vise, Bronchial tone due to the effects of propranolol.

The stage of selectivity shows the intensity of the interaction with β-adrenergic receptors and the origin of the intensity of the force and the triviality of the β-blocker. Overblock β l adrenergic receptors by the beginning of the index of selectivity of β-blockers, reduction of β-blockers 2 blockade, by themselves, reducing the number of side effects (Table 5.2).

Trivial admission of β-blockers in the development of circulating β-receptors, especially in the course of the growth of β-adrenoceptor blockade and significantly more circulatory circulations,

β-blockers of the 1st generation, in the same world, they blockade and β 2 adrenergic receptors, referred to non-selective β-blockers - propranolol, nadolol. Singing perevagu may have nonselective β-blockers without ICA.

Until the II generation, selective β l adrenoblockers, called Cardioselective - atenolol, bisoprolol, betaxolol, metoprolol, nebivolol, talinolol, oxprenolol, acebutolol, celiprolol. At low doses, β l-selective drug little infusion on physiological reactions, mediated by peripheral β 2 -adrenergic receptors - bronchodilation, insulin secretion, glucose mobilization from the liver, vasodilatation and rapid uterine activity hour of vaginosti That is why they may be overwhelmed by the turn of the hypotensive action, the lesser frequency of side effects, which are sometimes nonselective.

High level of selectivity β l-adrenoblocks give the possibility of stagnation in patients with bronchial obstruction, for diabet I and II type, impaired peripheral blood circulation in some cases with non-selective and less selective β-blockers.

The level of selectivity of β-adrenergic blockers is injected into the posterior peripheral vertebral arthritis as one of the primary components of the hypotensive effect. selective β l adrenergic blockers do not throttle adrenergic blocking into OPSS, nonselective β-adrenergic blockers, for blockade β 2 receptor in sudin, can enhance vasoconstrictor effect and increase

The selectivity stays in the form of the first dose. The increase in the dose of the drug is superimposed on the decrease in the selectivity of the drug, the clinical manifestations of β blockade 2 adrenergic receptors, in high doses β l-selective beta-adrenergic blockers to consume β l-selective.

Seeing β-adrenergic blockers, which is a vasodilating effect, may combine the mechanism of action: labetalol (nonselective blocker і a1 - adrenergic receptors), car-

vedilol (non-selective β blocker 1 β 2- і a 1 -adrenergic receptors), dilevalol (non-selective β-adrenergic receptor blocker and partial agonist β 2 adrenergic receptors), nevolol (b 1-blocker with activation of endothelial nitrogen oxide). The drugs may have developed mechanisms of vasodilating activity, and can be transferred to β-adrenergic blockers of the third generation.

Most of the level of selectivity and manifestation of vasodilating powers M.R. Bristow, in 1998, the classification of beta-blockers was promoted (Table 5.3).

Table 5.3

Classification of beta-blockers (M. R. Bristow, 1998)

Deyaki β-adrenergic blockers may be building up to partial activation of adrenergic receptors, so that partial agonistic activity. Cy β-adrenergic blockers are called drugs with internal activity - alprenolol, acebutalol, oxprenolol, penbutalol, pindolol, talinolol, praktolol. Nybilsh is characterized by a strong sympathomimetic activity in pindolol.

The internal sympathomimetic activity of β-blockers is intertwined with a decrease in the frequency of the heart rate at a very low rate, which can be seen in patients with a low heart rate on the cob.

Nonselective (β 1- + β 2-) β-blockers without ICA: propranolol, nadolol, sotalol, timolol, і from ICA: alprenolol, bopindolol, oxprenolol, pindolol.

Preparations with membrane-stabilizing effect - propranolol, betaxolol, bisoprolol, oxprenolol, pindolol, talinolol.

Lipophilic, hydrophilic, AMPHOphilic

Evidence in the triviality of β-adrenergic blockers with a low selectivity index is due to the peculiarities of the chemistry budget, the style and the way of life. See hydrophilic, lipophilic and amphophilic preparations.

Lipophilic drugs, as a rule, are metabolized in the liver, and in the case of an occasionally short period of half-life (T 1/2). Lipophilicity is united with the pechinkovy path of elimination. Lipophilic drugs are quickly and easily (90%) soaked in shlunkovo-intestinal tract, Їх metabolism in the oven to become 80-100%, the bioavailability of more lipophilic β-blockers (propranolol, metoprolol, alprenolol, etc.) ).

The stage of liver blood flow is infused into the metabolic rate, at the value of single doses and the frequency of the drug taken. It is necessary to be rescued in case of lithuanian patients, ailments with heart failure, with liver cirrhosis. In case of severe inconveniences, the efficiency of elimination decreases

Table 5.4

Pharmacokinetic parameters of lipophilic β-blockers

proportionally lowering the function of the stove. Lipophilic drugs in case of trivial stasis may themselves change liver blood flow, increase their blood metabolism and metabolism of other lipophilic drugs. We will explain the increase in the period of half-change and the possibility of a change in a single (additional) dose and the multiplicity of the intake of lipophilic drugs, increasing the effect, contaminate the overdose.

Quite the injection of microsomal oxidation into the metabolism of lipophilic drugs. Preparations that induce microsomal oxidation of lipophilic β-blockers (malignant cure, alcohol, rifampicin, barbiturati, difenin), significantly accelerate their efficiency, reduce the appearance of blood pressure. Protolezhne infusion nadayut drugs, which increase liver blood flow, change the speed of microsomal oxidation in hepatocytes (cimetidine, chlorpromazine).

Among the lipophilic β-adrenergic blockers in the intake of betaxolol, it is not possible to correct the dosage in case of liver failure, but in the case of the inhibition of betaxolol, it is necessary to correct the dosage of the drug in the case of severe neurodevelopmental deficiencies. Correction of a dose of metoprolol is carried out in case of severe damage to the liver function.

Lipophilicity of β-blockers during penetration through hemato-encephalic, hysteroplacental barri in the eye chamber.

Hydrophilic drugs are not needed in a healthy way, and there may not be more hygrophilous drugs (30-70%) and irresistibly (0-20%) are wetted in a slurry-intestinal tract 70% metabolites, may have a longer period of time (6-24 years), lower lipophilic β-blockers (Table 5.5).

Reduced glomerular filtration rate (in lithians, with chronic nirkova lack) Changes in the rate of treatment of hydrophilic drugs, as well as changes in dosage and multiplicity of intake. Orієntuvatisya can be based on the concentration of creatine, the level of which grows with a decrease in the fluidity of the glomerular filtration below 50 ml / min. In general, the multiplicity of the sign of the hydrophilic β-blocker may be used every other day. With hydrophilic β-blockers penbutalol is not vimag

Table5.5

Pharmacokinetic parameters of hydrophilic β-blockers

Table5.6

Pharmacokinetic parameters of amphophilic β-blockers

korektsії dosi at impaired functions nirok. Nadolol does not reduce blood circulation and the speed of glomerular filtration;

The injection of microsomal oxidation into the metabolism of hydrophilic β-blockers is not present.

β-blockers of supra-short dyes run with blood esterases and vikoristovyuyutsya vklyuchno for internal infusions. β-blockers, which contain blood esterases, may take an even shorter period of half-elimination, and they will rise in 30 minutes after the infusion. Such preparations will be stagnant for drinking guest ischemia, Control over the slurry rhythm in case of paroxysm of supra-slurry tachycardia in the period of the operation or in the period of operation. The shortness of time to rob the more unhealthy їх stasis in ailments with hypotonia, with heart failure, and βl-selectivity to the drug (esmolol) - in case of bronchial obstruction.

Amphophilic β-blockers are expressed in fats and in water (acebutolol, bisoprolol, pindolol, celiprolol), but two paths of elimination - liver metabolism and nirkov excretion (Table 5.6).

Balancing the clearence of the drug in the form of a safety net for the ailments due to the lack of nirk and oven deficiency, low efficiency of the relationship with the others drugs... The rate of elimination of drugs is reduced only in case of severe neurotic and peptic deficiency. In general, the addition of a dose of β-adrenergic blockers with a balanced clearence should be changed by 1.5-2 times.

Amphophilic β-adrenoceptor blocker pindol in chronic nircovymic deficiency may cause nircoval blood circulation.

Doses of β-adrenergic blockers must be taken individually, depending on the clinical effect, equal heart rate, AT. The pochatkova dose of a β-blocker is responsible for becoming 1 / 8-1 / 4 of the average therapeutic single dose, with a lack of effect, the dose is increased through the skin for 3-7 days to the average therapeutic single dose. Heart rate at rest vertical position is guilty of buty in between 55-60 in khilina, systolic AT - not lower than 100 mm Hg. The maximum turnover of β-adrenergic blocking effect is observed after 4-6 months of regular intake of a β-blocker, special control in the center of the term, it is possible to detect lipophilic β-adrenergic blockers,

Sobnim_ spov_lnuvati sv_y power metabolism. The multiplicity of the drug taken depends on the frequency of angina attacks and triviality of the β-blocker.

Slid vrahovuvati, that the triviality of the bradycardiac and hypotensive action of β-adrenergic blockers signifi- cantly replaces the period of half-elimination, and the triviality of the antianginal action is less than the triviality of the negative chronotropic.

MECHANIZMI antianginal and anti-ischemic β-adrenergic blockers FOR LICUANIA OF STENOCARDIA

Improving the balance between the need for myocardium in acid and the delivery of it through the coronary arteries can be achieved by reducing the coronary blood flow and reducing the consumption of the myocardium in acid.

The basis of the antianginal and anti-ischemic action of β-adrenergic blockers is based on the health of the injection on the hemodynamic parameters - the reduction in the rate of myocardial recovery of heart rate, rapid health of the systemic myocardium. β-adrenergic blockers, decrease in heart rate, increase in triviality of diastoli. Delivery of sour to the myocardium of the lіvnogo shlunochka zdіysnyutsya in the main in the diastolu, so as in the systole of the coronary artery to squeeze navkolishnіm myocardium and the triviality of diastoli vnnacha the level of coronary blood flow. Decrease in the speed of myocardial health in the order of the increase in the hour of the distal relaxation with the decrease in the heart rate, the increase in the period of the diastolic perfusion of the myocardium. Decrease of the long-lasting grip in the lactose for the reduction of the fast-feeling health of the myocardium with the decrease in the systemic AT pressure

A decrease in the systemic arterial grip on the

15-20%, galvanized central adrenergic infusions (for drugs that penetrate through hematoencephalic barriers) and antireninovym (up to 60%) for β-adrenergic blockers, as well as reducing systolic and persistent thymus.

Znizhennya frequency now Sertsevy skorochen i zmenshennya skorotlivoї zdatnostі mіokarda in rezultatі β-blockade adrenoretseptorіv sericite generally produces up zbіlshennya obsyagu i kіntsevogo dіastolіchnogo vise in lіvomu shlunochku scho koreguyut poєdnannyam β-adrenoblokatorіv of drugs scho zmenshuyut venous Povernennya krovі to lіvogo shlunochka (nіrovazodіlatatori) ...

Β-blockers Lіpofіlnі adrenoretseptorіv scho not mayutsya vnutrіshnoї simpatomіmetichnoї aktivnostі, Square od selektivnostі, bіlshoyu mіroyu volodіyut kardіoprotektіvnim dієyu have moved GOSTR іnfarkt mіokarda Khvorov at trivalomu zastosuvannі, zmenshuyuchi rizik re іnfarktu mіokarda, raptovoї smertі that zagalnoї smertnostі tsієї groupies patsієntіv. Such power is specific to metoprolol, propranolol (pre-BHAT, 3837 ailments), timolol (Norwegian MSG, 1884 ailments). Lipophilic preparations with internal sympathetic activity may reduce prophylactic antianginal efficacy. Effectiveness of carvedilol and bisoprolol by cardioprotective powers can be attributed to the effects of retardated form of metoprolol. Hydrophilic β-adrenergic blockers - atenolol, sotalol were not infused into the lateral mortality and the frequency of raptor death in patients with ischemic ailments of the heart. The data for the meta-analysis of 25 control samples are presented in table. 5.8.

For vtorinnoї profіlaktiki β-blockers pokazanі vsіm patsієntam, SSMSC shifted Q-claw іnfarkt mіokarda protyagom, yak mіnіmum 3 rokіv at vіdsutnostі absolutely protipokazan to priznachennya preparatіv tsogo Klas, Especially patsієntam over 50 rokіv of іnfarktom perednoї stіnki lіvogo shlunochka, rannoї postіnfarktnoї stenokardієyu, TEMPLE the frequency of the heart is very fast, the lingering lesions of the rhythm of the heart, the manifestations of stable heart failure.

Table 5.7

Preparations of β-blockers in the treatment of angina pectoris

Note,- selective drug; # - in Russia, the original drug is not registered; the original preparation is shown in bold;

* - single dose.

Table 5.8

Cardioprotective efficacy of β-blockers in ailments who have had myocardial infarction

Efekti β-blockers in CHF

Therapeutic effect of β-blockers in CHF dressings with direct antiarrhythmic action, positive injections on the function of the adolescent slurry, changes in the chronic ischemia of the dilated slurry during the presence of β-myocardial infarction, asphyxiation

With CHF, there is an increase in the level of basal norepinephrine in the blood plasma, due to the additional production of adrenergic nerve deficiencies, the improvement in blood plasma and blood plasma reductions The concentration of the basal level of noradrenaline in blood plasma is an independent predictor of death in CHF. The first increase in the activity of the sympathoadrenal system in CHF is compensatory in nature and the increase in the development of the heart wikidum, overgrowth of the regional blood flow into the heart and skeletal muscles; nirkova vasoconstriction spri polypheny of perfusion of life of important organs. Nadal p_advishennya activity of sympathetic-adrenal

vitality of the system and to produce up to the advancement of consumption by myocardium, strengthening of ischemia, disruption of the rhythm of the heart, direct infusion on cardiomyocytes - remodeling, hypertrophy, apoptosis and necrosis.

With a trivial increase in catecholamines, the β-adrenergic receptors of the myocardium move to a decrease in responsiveness to a neurotransmitter (a decrease in the number of receptors on the adrenergic membrane) The strength of β-blockers of the myocardium is reduced by half, the steps of the decrease in receptors are proportional to the severity of CHF, the rapidity of the myocardium and the fraction of wikidu. Change rate β 2 adrenergic receptors in bik zbіlshennya β 2 adrenergic receptors. Disruption of the production of β-blockers fordenylate cyclase and lead to direct cardiotoxic effects of catecholamines, re-entanglement of mitochondrial cardiomyocytes with calcium ions, disruption of the processes of refhosphoric formation of blood pressure Activation of phospholipases and proteases during the destruction of the cell membrane and the collapse of the cardiomyocytes.

The decrease in the strength of adrenergic receptors in the myocardium is reduced by the loss of local reserves of norepinephrine, the deterioration of the adequate supply of adrenergic pressure of the myocardium, and the progress of illness.

Positive efekta β-adrenobloktaorov in CHF Je: znizhennya simpatichnoї aktivnostі, zmenshennya HR, antiaritmіchny efekt, polіpshennya dіastolіchnoї funktsії, zmenshennya gіpoksії mіokarda that regresіya gіpertrofії, zmenshennya necrosis i apoptosis kardіomіotsitіv, zmenshennya virazhenostі zastіynih yavisch for rakhunok blockade renіn-angіotenzin-aldosteronovoї system.

At the present time, USCP - American programs for carvedilol, CIBIS II with bisoprolol and MERIT HF with metoprolol succinate for hospitalization of the drug, COPERNICUS, CAPRICORN for serious deaths % in important categories of ailments with CHF, the value of β-blockers occupy one of the main positions of pharmacotherapy for ailments of CHF of all functional classes. β-adrenergic blockers order with ACE inhibitors

є the main problems in the treatment of CHF. The number of hospitalizations and the prognosis of decompensated ailments that are not victorious (level of proof A). β-adrenergic blockers are guilty of stagnation in all ailments of CHF, as there are no contraindications that are common for the whole group of people. The severity of decompensation, to become, to, the level of the vyhid vise (SBP not less than 85 mm Hg) and the vyhidnogo heart rate does not play an independent role in the established counter-indication until the appointment of β-adrenergic blockers. The purpose of β-blockers to be repaired 1 /8 therapeutic dosage for patients with an extended stabilization stanchion of CHF. β-adrenergic blockers in the treatment of CHF should not be found until the preparations of "high supplementation" and the illnesses cannot be evolved from the stage of decompensation and hyperhydration. Can the value β l-selective β-adrenergic blocker bisoprolol as a drug of cob therapy in patients over 65 years of age with CHF II - III FC NYHA<35% с последующим присоединением ингибитора АПФ (степень доказанности В). Начальная терапия βl-selective β-adrenergic blocking agent can be used in clinical situations of overturned tachycardia with low AT, with the help of an ACE engineer.

The tactics of the appointment of β-blockers in ailments with CHF are presented in table. 5.9.

In the first 2-3 months, low doses of β-blockers are used to induce changes in peripheral vascular support, decrease in the systolic function of the myocardium, so that in the titration of the dose, it is associated with the ailment of chronic heart failure of the β-adrenoceptor blocker, In cich vipads, it is recommended to increase the doses of diuretics, angibitoris ACE, the preservation of positive inotropic drugs (small doses of heart glucosides or calcium sensitizers - levosimendanu), a larger dose of β-adrenergic drugs.

Prototype indications for β-blockers in HF є:

Bronchial asthma is a very important pathology of bronchial tubes, which leads to increased symptoms of bronchial obstruction in case of β-blocker;

Symptom bradykadiya (<50 уд/мин);

Symptom hypotonia (<85 мм рт.ст.);

Table 5.9

Pochatkov, tsilovi doses and the scheme for the selection of doses of β-adrenergic blockers for heart failure following the results of large-scale placebo control

doslidzhen

A-V blockade of the II stage і vische;

Important regional designation.

We will absolutely show є the sign of β-blockers in patients with CHF and type 2 CD. All the positive power of drugs in a class will increase in the presence of diabetics. Stagnation of a noncardioselective і adrenergic blocker with additional powers 0 4 -adrenoblokatory carvedilol in such patients can be used as a choice for increasing the sensitivity of peripheral tissues to insulin (level of delivery A).

Results of SENIORS 'advances from the amount of β l-selective β-adrenergic blocker nebivolol, which demonstrated a small, altogether less significant decrease in the frequency of hospitalization and death in patients with CHF older than 75 years, allowed to recommend nonvolol for treating patients with chronic heart failure older than 70 years.

Doses of β-areneblockers for the treatment of CHF ailments, secured by the National Recommendations of the All-Russian Society of Scientific Organizations I OSSN, are presented in Table 5.10.

Table 5.10

Dozi of beta-blockers for the treatment of CHF ailments

lіvogo shlunochka<35%, была выявлена одинаковая эффективность и переносимость бетаксолола и карведилола.

Stagnation of the nonselective β-blocker bucindolol, which is associated with internal activity, additional vasodilating powers (before BEST), insufficiently lowered the mortality rate and frequency of the state; meaning a decrease in the prognosis and growth of the risk of death by 17% in the group of patients of the Black race.

It would be necessary to further clarify the effectiveness of drugs in the whole group in some demographic groups of patients, in lithuanian patients, who are ill with flashy arrhythmias.

BASIC Mechanism of hypotensive activity β -ADRENOB locator

β-adrenergic blockers є drugs of starting therapy in the treatment of arterial hypertension. β-adrenergic blockers are the first line of drugs in hypertension in patients with a history of acute myocardial infarction, who have stable angina pectoris, heart deficiency, in individuals with an intolerance of an

As a result of blockade of β-adrenergic receptors in the heart, the frequency of the heart rate decreases and the myocardial health becomes very fast, and the heart rate decreases. The blockade of β-adrenergic receptors in cells of the juxtaglomerular apparatus should be reduced to a decrease in the secretion of renin, a decrease in the confirmation of angiotensin, and a decrease in the systemic vascular resistance. Change in aldosterone production The sensitivity of the baroreceptors of the aortic arch and the carotid sinus changes, and the norepinephrine is induced by the end of postganglionic sympathetic nerve fibers. Galmuvannya of central adrenergic infusions (for β-adrenergic blockers, which penetrate through the hematoencephalic bar) is seen.

Stagnation of β-adrenergic blockers in systolic and diastolic arterial vices, control of arterial vices in the early ranks, normalization

dobovogo profile arterial vise. The hypertrophy of this season's louse is seen as one of the most significant officials in the development of heart-and-heart acceleration.

β-adrenergic blockers as a result of decreased activity of the sympathetic and renin-angiotesin system є by the optimal class of drugs for preventing and revitalizing the hypertrophy of the louse. The reduction of the level of aldosterone is interrupted by the simulation of fibrosis of the myocardium, which reduces the diastolic function of the louse.

The level of selectivity of β-adrenergic blockers is injected into the posterior peripheral vertebral arthritis as one of the primary components of the hypotensive effect. selective β l adrenergic blockers do not throttle the injection into OPSS, nonselective, for blockade β 2 receptors for sudin, may enhance vasoconstrictor effect and increase OPSS.

β-adrenergic blockers in combination with vasodilators and labetolol є with Vibor preparations for the threat of aortic aneurysm rosacea on aphids caused by arterial vise. Tse edina klinichna situation pidvishenny arterial vise, which vimagaє shvidny reduction of arterial vise stretching 5-10 min. The introduction of a β-adrenergic blocker can overwhelm the vasodilator for preventing the development of the heart wikid, which can destroy the situation.

Labetolol is a Vibor drug in the treatment of hypertensive crisis, accelerated by coronary insufficiency, parenteral administration of a nonselective β-adrenergic blocker is indicated for the development of tachycardia or disturbed rhythm.

Labetolol і esmolol є preparations for the treatment of ailments with craniocerebral injuries, accelerated hypertensive crises.

Labetolol і oxprenalol - Vibor preparations for the control of arterial vise in vaginal patients with methyldopi intolerance. The efficacy of pindolol is proportional to oxprenolol and labetolol. With trivial stasis of atenolol, a decrease in the mass of the neonatal and placenta is revealed, which is associated with a decrease in the fetal-placental blood flow.

Table. 5.11 shows the basic dose and frequency of intake of β-blockers for the treatment of hypertension.

Table 5.11

Add dose and frequency of intake of β-blockers for the treatment of hypertension

CONTROL OF THE EFFECTIVENESS OF THERAPY β-adrenergic blockers

An effective frequency of the heart is very fast at the maximum ochіkuvannoy dії Chergova dose of β-adrenergic blocker (call in 2 years after receiving the reception) to become 55-60 strokes in khilina. Stable hypotensive effect is infused after 3-4 months of regular intake of the drug. I will look at the possibility of increasing the atrioventricular conductivity, the necessary electrocardiographic control, especially in the case of a large decrease in heart rate. Vimagayuyu respect for the patient with the symptoms of a lack of blood circulation, such patients need more trivial titration of the dose of β-adrenergic blocker through the threat of development of symptoms of decompensation.

Due to the peculiarities of the pharmacodynamics of β-adrenergic blockers in conjunction with changes in the interaction between β-adrenergic receptors and stimulation of the production of alaninaminotransferase, receptor activation with adenylate cyclase. Change and twist the sensitivity of the β-blocker to the β-adrenergic blocker. The price is the origin of the directness and important predictions of the nature of the pharmacodynamic response to the lykarsky zasib.

Changes and pharmacokinetic parameters: changes in blood volume, water and myazova mass, increase in adipose tissue, change in tissue perfusion. The amount of liver blood flow decreases by 35-45%. Decrease in the number of hepatocytes, the level of enzymatic activity - the weight of the liver decreases by 18-25%. The number of functional glomeruli nirok, the fluidity of glomerular filtration (by 35-50%) and tubular secretion change.

OKREMI PREPARATIONS β-adrenergic blockers

nonselectiveβ adrenoblockers

propranolol- non-selective beta-blocker without vascular sympathomimetic activity with non-trivial day. Bioavailability of propranolol when received in the middle of the warehouse is less than 30%, T 1/2 - 2-3 hours. Due to the great speed of metabolism, the drug during the first passage through the liver of the concentration in the blood plasma for a single dose and the same dose may occur in children in 7-20 times. From the cross section, 90% of the dose taken is in vivid metabolites. A number of medications have been injected into the organisms for rosinitis, propranolol, mabut, and other β-adrenergic blockers. At the same hour, the β-adrenergic blockers themselves can change the metabolism and pharmacokinetics of their own lymphocytes. Propranolol should be used in the middle, repaired from small doses - 10-20 mg, step by step (especially in older people and in case of adolescence for heart failure) for 2-3 weeks to bring the dose to an effective dose (160-180-240 mg). I will look at the short T 1/2 of the drug, to achieve a post-therapeutic concentration, it is necessary to take propranolol 3-4 times as needed. Likuvannya can be trivial. Slid pam'yatati, scho visoki

Doses of propranolol can lead to frequent side effects. To vibrate the optimal dose, it is necessary to regularly change the heart rate and AT. The drug should be recommended on a step-by-step basis, especially when it is trivial to take, or when high doses are taken (change the dose by 50% in one period), so as to reduce the risk of admission syndrome, often - a sharp pidyom arterial grip.

nadolol- a non-selective β-blocker without internal sympatomimetic and membrane-stabilizing activity. It is easy to learn from one of the other drugs in a group of trivial and useful functions. Volodya Nadolol antianginal activity. It is possible to repair the lesser cardiodepressive effect through the visibility of the membrane-dependent activity. When you take it, almost 30% of the drug is absorbed in the middle. Only 18-21% are bound to plasma beads. The peak of concentration in the blood is reached internally in 3-4 hours, T 1/2

From 14 to 24 years old, it is allowed to prescribe the drug 1 time for dob with ailments such as angina pectoris and hypertension. Nadolol is not metabolized in organisms, vivod in nirkami and intestines in an insignificant viglyad. The new vision is only accessible after 4 days after a one-time dose taken. Nadolol priznachayut 40-160 mg 1 time per doba. A stable level of concentration in the blood is reached after 6-9 days of admission.

pindololє a non-selective blocker of β-adrenergic receptors with activity. It’s good to get wet when you take it all in the middle. Visible high availability, T 1/2

3-6 hours, the beta-blocking effect will last for 8 years. 57% of the dose taken is close to the bottle. From the cross section, 80% of the drug is seen (40% in an unmistakable viglyade). Metabolism of this is represented in the presence of glucuronides and sulfates. KhNN simply does not change the constant of elimination and the hour of the day. The rate of elimination of the drug is reduced only in case of severe neurotic and peptic deficiency The drug penetrates through the hematoencephalic bar and placenta. Sumіsny with diuretics, antiadrenergic drugs, methyldopa, reserpіn, barbіturata, foxglove. For β-adrenoceptor blocking 2 mg pindolol equivalent 40 mg propranolol. Pindolol should be consumed 5 mg 3-4 times a day, and in important cases - 10 mg 3 times a day.

If necessary, the drug can be injected vnutrishnovenno in drops of 0.4 mg; the maximum dose for intravenous injection is 1-2 mg. The drug viclikє mensh of bends negative inotropic effect in calm, low propranolol. Win weak, lower nonselective β-adrenergic blockers, infusion on β 2 adrenergic receptors, and in particular doses, it is more safe for bronchospasm and diabetic diabetes. In hypertension, the hypotensive effect of pindolol develops more often, less for propranolol: an ear of diya - after a day, and the maximum effect - after 4-6 months.

selectiveβ adrenoblockers

nebivolol- a high-grade β-blocker of the third generation. Active speech is nonvololu - racemate, it is stored in two enathioomers. D-nonvolol є competitive and leaseselective β l-blocker. L-nonvolol appears to be able to vasodilate for the development of modulation of the endothelium of sudin relaxing factor (NO), which leads to normal basal tone of sudin. Whenever you get it, you get wet all the way through the middle. Highly lipophilic drug. Nevolol is actively metabolized, often with the approval of active hydroxymetabolites. The hour of reaching a stable and equally important concentration, especially with a quick metabolism, can be reached for 24 years, for hydroxymetabolites - through a small amount of dib.

The level of hypothetical effect and the number of indications for the therapy of patients should be taken in proportion to 2.5-5 mg of an additional dose of the drug, for which the average effective dose of a non-volatile 5 mg is taken at the same time; with nirkovy deficiency, as well as in individuals over 65 years of age, the dose is not guilty of overhanging 2.5 mg.

Hypotensive dyu nonvololu develop during the first period of growth, growth up to the 4th stage of regular growth, with trivial treatment up to 12 msec, the effect is stably reduced. The arterial grip is forced to rotate the received nonvolol for 1 msec to the cob ryvnya;

The prescriptions for the manifestation of vasodilating powers do not infuse nonvolol into the indicators of nircovy hemodynamics (opirkovy arteries, nircovial blood circulation, glomerular filtration,

filtration fraction) as in ailments with a normal, as well as impaired nirk function on the basis of arterial hypertension.

Unimportant to the high lipophilicity, it is not practical to add side effects from the side of the central nervous system: it’s not vicious, powering lipophilic β-adrenergic blockers, sleep disturbance, nightmares. One neurological disorder - paresthesia - the frequency is 2-6%. Sexual issues were identified with frequency, as did not appear as a placebo (less than 2%).

carvedilol Volodin β- and a 1 -adrenergic blocking, as well as antioxidant power. Winning the heritage of arteriolar vasodilatation and neurohumoral vasoconstrictor activation of the heart. Carvedilol is poorly prolonged antihypertensive effect. Yomu power is an antianginal effect. Win is not volodya active. Carvedilol galmonic proliferation and migration of smooth oleaginous cells, apparently, acts on a specific mytogen receptor. Carvedilol has little lipophilic power. T 1/2 for 6 hours. When first passed through the oven, it is metabolized. In blood plasma, 95% of carvedilol is tied with beads. The drug is administered through the liver. Zastosovyut with hypertension - 25-20 mg once per doba; with angina pectoris and with chronic heart failure - 25-50 mg twice a day.

bisoprolol- a highly selective pre-active β-adrenergic blocker without internal sympathomimetic activity, not a membrane stabilizing effect. Volodya amphophilic powers. Prolonged performances can be awarded once for doba. The drink of bisoprolol was infused in 2-4 years after receiving the treatment, the antihypertensive effect is 3–24 years. Bioavailability becomes 65-75% for bisoprolol hydrochloride and 80% for bisoprolol fumarate. The bioavailability of the drug is improved in patients. Acceptance does not add to the bioavailability of bisoprolol. A small amount of blood plasmas (30%) will ensure safety in case of alcohol consumption with a large amount of drugs. 20% of bisoprolol is metabolized into 3 inactive metabolites. The lineage of pharmacokinetics is observed in the form of a dose in the range of 2.5-20 mg. T s becomes 7-15 years for bisoprolol fumarate and 4-10 years for bisoprolol hydrochloride. Bisoprolol fumarate is linked with blood cells by 30%,

bisoprolol hydrochloride - by 40-68%. Cumulation of bisoprolol in blood can be possible with damaged liver function and nirok. In the rivniy world, one is made with peppers and nirkas. The rate of elimination of the drug is reduced only in case of severe liver and liver deficiency, due to the possibility of accumulation of bisoprolol in the blood with damaged liver function and low liver function.

Penetration through the hematoencephalic bar. Stagnate with arterial hypertension, angina pectoris, heart failure. The pochatkova dose for hypertension should be 5-10 mg per dose, you can increase the dose up to 20 mg per day, with a lack of liver function and nirok dobova, the dose is not to blame for 10 mg. Bisoprolol is not infused into the level of glucose in the blood of patients with diabetes and the level of thyroid hormones, it is practically not infused into the potential of choloviks.

betaxolol- a cardioselective β-adrenergic blocker without sympathetic sympathetic activity and weak membrane changes. The power of blocking β-adrenergic receptors is 4 times more effective than propranolol. MA VISOK Lіpophilnіst. Good (more than 95%) get wet in the intestinal tract. For a one-time reception, the maximum concentration in blood plasma is reached in 2-4 years. Acceptance does not flow into the steps and the efficiency of absorption. On the basis of the type of lipophilic drugs in the bioavailability with oral administration of betaxolol to become 80-89%, which is explained on the basis of the "first pass" effect through the oven. The individuality of the specificity of metabolism is not infused with the variability of the concentration of the drug in the blood, which allows for a greater stable response to the drug in case of stagnation. The step of lowering the heart rate is proportional to the dose of betaxolol. The correlation of the antihypertensive effect with the increase in the concentration of betaxolol in the blood up to 3-4 hours after being taken and given for a period of 24 years, the accumulation of the effect as a dose. With regular intake of betaxolol, the antihypertensive effect reaches the maximum value after 1-2 times. Betaxolol is metabolized in the microsomal oxidation pathway, however, cimetidine does not change the concentration of the drug in case of alcohol consumption and should not be increased until T 1/2 is increased. T 1/2 becomes 14-22 years old, so you can take the drug 1 time for extra. The older person T 1/2 grows up to the age of 27.

It is linked with plasmas by 50-55%, of which with albumin by 42%. Poisoning of the stove and nirok does not pour on the steps of the ringing with bites, it does not change with the one-hour ingestion of digoxin, aspirin, diuretics. Betaxolol and its metabolism are administered from the cross section. The speed of elimination to the drug is reduced only in case of severe nircovy and liver deficiency. The peculiarities of the pharmacokinetics of betaxolol do not change the dosage regimen in case of severe hepatitis and non-invasive deficiencies. Correction of the dose to the drug is necessary only in the case of severe disability and in patients who are out of business on dialogue. We are sick with a significant nirkovy deficiency, as for vimaga hemodializu, the dose of betaxolol should be 5 mg per dose, the dose can be taken for 5 mg of skin for 14 days, the maximum dose is 20 mg. The pochatkova dose for hypertension and angina pectoris should be 10 mg once per dose, if necessary, the dose can be added in 7-14 days. To make the effect stronger, betaxalol can be combined with thiazide nimiduretics, vasodilators, aganistamy imdazoline receptors, about 1 -adrenergic blockers. Outperforming the other selective β 1 -adrenergic receptors є the overall decrease in the concentration of HDL. Betaxolol does not infuse on the process of glucose metabolism and compensatory mechanisms in case of hypoglycemia. Behind the stage of lowering heart rate, AT, adjusting tolerance to physical adaptation in patients with angina pectoris, betaxolol was not recognized as Nadolol.

metoprolol- selective blocker β 1 -adrenergic receptors. Bioavailability of metoprolol to become 50%, TS - 3-4 hours for lykarskoy form of sinus infection. With blood cells it is close to 12% to the drug. Metoprolol quickly collapses in tissues, penetrating through the hematoencephalic bar, ingesting milk in breast milk in higher concentrations, lower in plasma. The drug is susceptible to intensive hepatic metabolism in the cytochrome P4502D6 system, and there are two active metabolites - α-hydroxymetoprolol and o-dimethylmetoprolol. Vіk does not pour on the concentration of metoprolol, cirrhosis increases the bioavailability of up to 84% and T 1/2 up to 7.2 hours. In patients with hyperthyroidism, the level is reduced to reach the maximum concentration and area under the kinetic curve. The drug isnu in viglyadi metoprolol tartrate

nya), metoprolol succinate with trivially monitored vivilnenny. Forms of permissive vivilnenny may maximize the concentration of active speech in 2.5 times lower than the forms of vivilnenny, so I can get overwhelmed in patients with a lack of blood circulation. Pharmacokinetic parameters for metoprolol oral administration in doses of 100 mg are presented in table. 5.12.

Table 5.12

Pharmacokinetics of lykarsky forms of metoprolol

Metoprolol succinate in the form of a controllable vivilnenny can be persistently vividly active, so that it does not lie in the slurry when it is wet.

In case of arterial hypertension and angina pectoris, metoprolol is prescribed 2 times a day, 50-100-200 mg. The hypotensive effect is fast, the systolic arterial grip will decrease after 15 minutes, maximum - after 2 years. The diastolic grip is reduced by the deciliters of regular reception. Forms of up-to-date vivilnenny є with preparations of a vibor in case of lack of blood circulation. The clinical efficacy of ACE ingibitors in heart failure is significantly improved when a β-blocker is added to them (as a result of ATLAS, MERIT HF, PRECISE, MOCHA).

atenolol- selective β l- an adrenergic blocker, which is not volodya sympathomimetic and membrane-stabilizing activity. Absorbed from the intestinal tract by approximately 50%. Peak plasma concentration infusion after 2-4 years. Mayzhe does not metabolize in the liver and is more importantly metabolized. Closely 6-16% are linked to plasma beads. T 1/2 to become 6-7 hours a yak with a one-time, so i with a trivial

recognition. For oral intake, the decrease in the heart wikid is already in a year, the maximum effect is 2 or 4 hours and the triviality is not less than 24 years. The hypotensive effect, as in all β-adrenergic blockers, is not correlated with the plasma and growths for continuous reception with a stretch of decile tissue. In case of hypertension, the dose should be 25-50 mg, with 2-3 days the dose should be increased to 100-200 mg, divided by 2 doses. In lithuanians, with the manifestation of a chronic nirkovo deficiency, it is recommended to recommend a correction of the dose with a filtration lower than 35 ml / min.

Lykarski Vzaєmodia β-adrenergic blockers

Table 5.13

likarskі vzaєmodії

Pobіchna dіya and contraindication to the consumption of β-adrenergic blockers

The side effects of β-adrenergic blockers are, by the way, a more important blocking inflow on the same type of receptors; The level of lipophilicity is the beginning of the manifestation of side effects on the side of the central nervous system (Table 5.14).

The main side effects of β-adrenergic blockers are: sinus bradycardia, development of an increase in the degree of atrioventricular blockade, manifestation of congestive congestive heart failure, aggravated bronchial asthma and obstructive pulmonary disease

Table 5.14

Characteristics of side effects of β-blockers

vitality of function in choloviks, development of angiospasm, retinal weakness, drowsiness, depression, impairment, decreased speed of reaction, the possibility of development of the syndrome of vision (important for drugs in short) triviality.

The prototype is shown before the intake of β-blockers. Preparations cannot be stashed in case of bradycardia swelling (less than 48 beats / hv), arterial hypotonia (systolic arterial vise lower than 100 mm Hg), bronchial asthma, syndromes of weakness of sinus vascular disease, lesions Among other indications, there is a circulatory diabetes in the stage of decompensation, impairment of peripheral blood circulation, lack of blood circulation in the stage of decompensation, vaginitis (for β-adrenergic blockers, but not)

МІСЦЕ β-adrenoblockers

At KOMBINOVANO TERAPI

Monotherapy of β-blockers is effective for the prevention of angina attacks in angina pectoris of the I-III functional class and in 30-50% of patients with mellitus and small arterial hypertension for the appearance of the central digits of the arterial vise.

For the data of the HOT, for the extension of the central diastolic arterial vise lower than 85-80 mm Hg. 68-74% of patients need a combination of hypotensive therapy. Combined therapy for reaching the whole numbers of the arterial vise is shown to be overwhelmed by a large number of ailments on the CD and a chronic nircum deficiency.

Nezaperechnimi perevagami ratsіonalnih kombіnatsіy Je potentsіyuvannya gіpotenzivnogo efekta for rakhunok vplivu on rіznі Lanka pathogenesis arterіalnoї gіpertonії, polіpshennya perenosimostі preparatіv, zmenshennya number pobіchnih efektіv, obmezhennya kontrregulyatornih mehanіzmіv (bradikardії, pіdvischennya zagalnogo more peripheral support, arterіospazma, nadmіrnogo znizhennya skorochuvalnoї zdatnostі mіokarda that іnshih) scho are included on the cob stages of the sign of hypotensive drugs (Table 5.15). Combined hypotensive therapy is indicated for patients with arterial hypertension, with the manifestation of proteinuria, diabetics, nyrkovo deficiency.

Effective combination of β-adrenergic blocker and diuretic intake. Secoginny and vasodilating effect of diuretic intertwines the absorption of sodium and increases the tone of peripheral vasodins, powering β-adrenergic blockers. β-adrenergic blockers, in their turn, bring the activity of the sympathoadrenal and renin-angiotensin systems characteristic of a diuretic. You can stream a β-adrenergic blocker to develop diuretic hipokalii. The variability of such combinations is varied.

Use the combination of lycarsky form: tenorethic (50-100 mg atenolol and 25 mg chlorthalidone), HGT lopressor (50-100 mg metoprolol and 25-50 mg hydrochlorothiazide), basketoid (40-80 mg Nadolendoflumethydone) і 5 mg Clopamid), ziac (2.5-5-10 mg bisoprolol and 6, 25 mg hydrochlorothiazide).

With the addition of dihydropyridine antagonists of the major calcium channels, β-adrenergic blockers may have an additive effect, they prevent the development of tachycardia and activation of the sympathetic nervous system, the power of the pochatkovydinamydinamydinami. Such a combined therapy is indicated for hypertensive patients with ІHS, patients with important refractory arterial hypertension. Logimax is a combination of a trivial system of vivification of active components 50-100 mg metoprolol and 5-10 mg felodipin, vibirkovo for precapillary resistive judgment. 50 mg of atenolol and 5 mg of amlodipin enter the drug Tenochek before the warehouse.

The addition of β-blockers and calcium antagonists - verapamil or diltiazem - is certainly in the plan of significant hope for atrioventricular conductivity.

Conveniently receiving β-blockers and blockers of a 1 -adrenergic receptors. β-adrenergic blockers galvanize the development of tachycardia, which is characteristic for the appointment of α-blockers. Blockers of a 1 -adrenergic receptors change the effect of β-adrenergic blockers, such as moving the peripheral vascular support, pouring onto the lipid and carbohydrate exchange.

Drugs β-blockers and ACE, lowering the activity of the renin-angiotensin system, can cause a synergistic hypotensive effect. The assignment of the IAPF will not lead to an increase in the approval of angiotensin II, since it is an alternative way of education. Hyperreninemia, which is associated with the development of an ACE inhibitor, can be reduced due to the addition of a direct transfer of β-adrenergic blockers to the secretion of renin by the juxtaglomerular apparatus of nirok. Applying the secretion renin to reduce the production of angiotensin I and, in some cases, angiotensin II. The vasodilating power of ACE inhibitors can change the vasoconstrictor effects of β-blockers. The organoprotective effect of such a combination in patients due to congestive heart failure has been reported.

Kombіnatsіya β-blocker i agonіsta іmіdazolіnovih retseptorіv (preparation tsentralnoї dії) Mauger Buti ratsіonalna in kombіnovanoї terapії arterіalnoї gіpertonії for dosyagnennya tsіlovih digits arterіalnogo vise at patsієntіv of metabolіchnimi torn down (up to 80% patsієntіv arterіalnu gіpertonіyu strazhdaє metabolіchnimi torn down). additive

the hypotensive effect is to overcome the correction of insulin resistance, impaired tolerance to glucose, dyslipidemia, which govern the class of β-adrenergic blockers.

Table 5.15

Combined antihypertensive therapy with β-blockers

Adrenoreceptors, sensitive to catecholics of aminiv, grow in different organs and appear one from one of their functions and smoother. Also, the stench is caused by the variability of reactions, which can be detected when they are activated.

Before lykarskiy zasobіv, scho pouring on the sensitivity of the receptors, to deliver preparations of alpha-adrenergic blockers. Until the class is given nonselective values. Since 1980, the use of selective drugs for the therapy began.

What are the alpha adrenergic blockers?

The effect of obsession with the reception of the designated lykarskoy group, the zeros of the same name.

Alpha-adrenergic blocking drugs are known to "capture" adrenergic receptors, blocking their sensitivity to the infusion of mediators. Until the end, adrenaline, dopamine and norepinephrine are delivered.

Mechanism of Diya

The effect is that it is spontaneous in the reception, to lie down as a type of blocked alpha receptors. Їх accepted for two groups: a1 and a2. Suggest to the body on the injection of blockers into the hand within the framework of the table.

Table 1. Mechanism of alpha-adrenergic blocking agents, which is injected onto adrenergic receptors a1

The blocking of receptors of types A2 for the additional alpha-blockers give the result, but it is itself produced up to:

• sounding the education of the judges;
• lift the grip;
• wikid norepinephrine;
• promotion of rukhovoy activity;
• improvement of libido and normalization of statutory functions;
• I stimulate the central nervous system.

Mechanism of alpha-adrenergic blocking agents

Classification

For therapeutic purposes, a few types of preparations are used. The stench is seen in its vibrating or nonvibirkov injected into the receptor.

selective

Dani lіkarski dіyut dіyut on the receptor vibіrkovo, zokrem, stench pick up adrenergic receptors type A1. At the moment, the classification of selective alpha-adrenergic blockers includes a group of pidgroups, who are for their triviality. Before likarsky zasobіv, scho to be recognized as a nontrivial effect, to introduce prazosin. Prolonged diu is indicated for terazosin and doxazosin. Besides, in the vicinity of the group they see uroselective blockers, which are injected into the adrenergic receptors, rosted in the muscles of the sechostatus tract.

nonselective

On the basis of the previous preparations, given alpha-blockers, inject nevibirkov. Stink block peripheral alpha-receptor type a1 and type A2. It is not selective for alpha-adrenergic blockers to produce a nontrivial decrease in the arterial grip through the inflow on a1. However, the blocking of alpha-2-adrenergic receptors stimulates the development of norepinephrine, which leads to a hypotensive effect to the level of improvement.

Nonselective therapeutic options can be used only for short-hour emergency treatment, or not for trivial use.

list of drugs

Blockers of adrenergic receptors may have a wide range of peculiarities of stasosuvannya. Meaning you can only fachіvets. It is clear that the actions of the given class are within the framework of the table.

Table 2. List of alpha-blocker drugs, which can be injected onto the A1 and A2 receptors

showing

A wide range of drugs allows the drug class to be used for therapy in cases of sickness. Naybilsh is often useful for cardiological practice, as well as for the treatment of pathologies of the sechostatic system.

Good prostate hyperplasia

Earlier, it was a sickness, which is a good idea in front of a throat, adenoma of the prostate. In the middle, there is another type of skin, which is 40-45 years old, suffering from pathology.

Stagnation of alpha-adrenergic blockers allows the suppression of obstructions and teasing caused by an adenoma.

arterial hypertension

Regularly adjust the arterial vise up to mm Hg. more and more to be called arterial hypertension (hypertension). To reduce the grip of fahivts in the row of vipadks, blockers a1 are assigned. Alpha-adrenergic blockers for hypertension of the selective type suffer from a reduced vice without an increase in the number of hearts. Prepare the class to speed up before- and post-navantazhennya on the tissue of the heart. Make it easy to get a trivial effect - up to 24 years.

Інші heart-damned sickness

Alpha-adrenergic blockers a1 may be indicated and indicated before being consumed. Zokrema, which are recommended for therapy in case of heart failure. The preparations give a reversible effect of bends in case of hypertrophy of a lone slunk. It is recommended to use blockers of A2 receptors, which I recommend in case of impaired erectile function and impotence.

Prototype

Before the vicarious preparations the preparations were made to become familiar with the contiguous ones.

Table 3. Prototype indications before treatment with alpha-blockers a1

A2 blockers are not recommended for ruptured laryngeal blood, bleeding, hyperplasia of the anterior throat, diabetic diabetics, in case of an impaired hemorrhage, vaginosis, etc. More details can be found in the information in the instructions to a specific drug.

Arterial hypertension as a factor in the development of an insult

Possible results from the reception

Until the most obvious negative manifestations, a vicious reception of A1 blockers, a decrease in the arterial vise and orthostatic collapse. As a rule, some secondary effects are promoted by the first intake of an alpha-adrenergic blocker (the phenomenon of "first dose"). Also, the patients see:

• bile in the head, spoiled;
• svidka stomlivanst, drowsiness, decreased prasezdatnosti;
• sharpened;
• The improvement of postural manifestations is too thin.

Therapy with alpha-2-adrenergic blockers can cause arterial pressure, tremors, dyspepsia, often sevalence, etc.

Instructions for the administration of pills

Annotation to likarsky zasobіv includes reports about the mechanism of the action, the scheme of reception and special features of the victorian. Deyakі aspekti, wikkladenі in іnstruktsії to alpha-adrenergic blockers, guided dalі.

For zapobigannya vinnennya efect "pershoi dozi" lykarskiy is recommended to sign, repaired from the smallest amount - 0.5-1 mg. Besides, there is a special form of this alpha-adrenergic blocker, which is controlled by volodya's control over the development of diabetic speech.

ЇЇ In general, the decrease in the dose is not necessary for the first dose.

A drug based on doxazosin mesylate Alpha-adrenergic blocker to produce a vice to an absolute reduction. Navigate with trivial therapy in patients who did not appear to have a tolerance to this. Krim hypotensive effect, rob the beneficial infusion into the eccentric function.

prazosin

Carrying out pharmacological therapy is recommended to repair with a small amount - 0.5-1 mg, which will eliminate the excessive decrease in the arterial vise. Dostupovo dobova amount of alpha-adrenergic blocker to increase. The maximum denna dose is over 7.5 mg. As a rule, the drug is well tolerated.

It may be the reason for the decrease in pracezdatnost, pain in the head, ruined zoru, if there is a noise in the ears, the serpentine of the heart rhythm, dyspeptic disorders are too small. Cei alpha-adrenergic blockers produce calcium antagonists, angibitoris ACE, ACE, etc.

Setegis is an alpha-adrenergic blocker, vibrations in Ugorshchyna. Є an analogue of the peredny drug. Dobova dose of Setegis is taken individually, out of the arterial grip of a particular patient. It is recommended to fix the price with a minimum amount, step by step, increase the amount of mg.

Corisne video

From the upcoming video, you can learn more about the role of alpha-adrenergic blockers in the development of arterial hypertension:

visnovka

1. Alpha-adrenergic blockers are effective lykarski to work for normalization of arterial vise, therapy of prostate adenoma, improvement of libido and struggle with potential.
2. The preparations given to the class of varto are taken from protection through the digitized list of the number of secondary defects.
3. It is categorically hardened to accept alpha-adrenergic blockers without a doctor's recommendation.

Adrenergic blockers are called adrenergic receptors, which block adrenergic receptors. Depending on the different types of blockers, a group of words can be used for:

1) α-adrenergic blockers;

2) β-adrenergic blockers;

3) α-, β-adrenergic blockers.

α-adrenoblockers

α 1 -Adrenoblokatori

Up to α 1 -adrenergic blockers are introduced prazosin(Prazosin; minipress, polpressin), terazosin(Terazosin; root), doxazosin(Doxazosin; tonocardin, cardura). The preparation expands arterial and venous vessels; reduce arterial grip. Relax the smooth mucus of the cuticle of the cuticle, the prostate and the prostatic part of the urethra. Prazosin for 6 hours, terazosin and doxazosin for 18-24 years.

Stagnant preparation for arterial hypertension. In addition, the stench is effective in the case of a secular discoloration, tied with good hyperplasia in front of the throat.

Side effects of α 1 -adrenergic blockers:

- reflex tachycardia is gone;

- orthostatic potential;

- nasal congestion (enlargement of the mucous membrane of the nose);

- peripheral embankments;

- hastened sechovipuskannya.

Tamsulozin(Tamsulosin; omnik) block in the main α 1A -adrenoceptor and in the connection with the cym of the vibratory release of the smooth mucus of the cuticle, prostate and prostatic part of the urethra; arterial grip, however, does not change. Stagnate tamsulosin in the middle when the patient is prone to severe hyperplasia in front of the disease.

Alfuzosin(Alfuzosin; dalphas) ​​- α 1 -adrenergic receptors. I can turn my attention to the smooth muscles of the tricycle of the slash, urethra, before the throat. The drug is prescribed vseredinu 1-2 times for goodness in case of good hyperplasia in front of myuria.

α 2 -Adrenoblokatori

yohimbine(Yohimbine) - alkaloid of the measles tree, which grows in Western Africa (Corynanthe yohimbe). In connection with the blockade of presynaptic α 2 -adrenergic receptors in the central nervous system, yohimbine has a central stimulating effect, spriyas spriyas, podvischennyu statoval cravings. For the blockade of peripheral α 2 -adrenoreceptors widening the blood vessels, increasing the blood circulation of the cavernous til and shrinking the erections.

Yohimbine is used for antidiuretic action (it can stimulate the secretion of antidiuretic hormone).

Staste yohimbine yak with impotence. Mean 1-3 times a day.

Yohimbine side effects:

- zabudlivost;

- tremor;

- deyake reduction of arterial grip;

- tachycardia;

- zamorochennya;

- head b_l;

- diarrhea.

α 1 -, α 2 -Adrenoblokatori

phentolamine(Phentolamine) blocking postsynaptic α 1 -adrenoreceptor and extra-naptic α 2 -adrenoceptor. To that, phentolamine reduces the stimulating inflow of sympathetic energy and adrenaline circulating in the blood and norepinephrine to the blood vessels and circulatory expansion.

At the same hour, phentolamine blocking presynaptic α 2 -adrenergic receptors for noradrenergic end-to-end and recovery of norepinephrine. Tse intermingled with phentolamine (Fig. 32).

Small. 32. Infusion of phentolamine on adrenergic energy of blood vessels. Phentolamine blocking presynaptic α 2 -adrenoreceptors and increasing norepinephrine. Phentolamine blocks postsynaptic α 1 -adrenoreceptors and transcriptions of norepinephrine.

Phentolamine expands arterial and venous vessels, decreases arterial vise, reduces tachycardia. Tachycardia of the mediator is reflexively, and also because of the mediator's assimilation - norepinephrine - in the heart (tied to the blockade of presynaptic α 2 -adrenoreceptors) (Fig. 33).

Small. 33. Infusion of phentolamine on the vision of norepinephrine in the heart. Phentolamine blocking presynaptic α 2 -adrenoreceptors and increasing vivification of norepinephrine, which stimulates β 1 -adrenoceptors of sinusoidal vascular cells and increases the frequency of the heart.

Phentolamine is highly susceptible to hypotensive effects in pheochromocytoma (the fluff of the cerebral speech of the supra-nirkoval lobes, which is seen in the roof of the superfluous adrenal mass). On a blockade of α 1 - і α 2 -adrenergic receptors of adrenaline, it is seen as a chubby, even more lowering the arterial vise, stimulating β 2 -adrenoreceptors of sudin (Fig. 34).

The pheochromocytoma is inviting to see a surgical path. Phentolamine vicoristovuyu for the prevention of hypertensive crises before the operation, before the hour of the operation and in drops, if the operation is uncomfortable.

In addition, phentolamine stasis in case of spasms of peripheral sudins (Raynaud's syndrome, regional endarteritis).

Small. 34. Adjustment of hypotensive action of phentolamine in case of sensitization of hypertension and pheochromocytoma. In case of pheochromocytomy on the blockade of α 1 - and α 2 -adrenoreceptors, the β 2 -adrenoreceptors are stimulated and the arterial vise is reduced even more.

Side effects of phentolamine:

Tachycardia is rotated;

zamorochennya;

Nasal congestion (bulging of mucous membrane of the nose as a result of enlarged sudin);

Orthostatic Potency;

Adjustment of the secretion of silt worms and slunk worms;

Destruction of the ejaculation.

In case of pheochromocytomy, β-adrenergic blockers are consumed for the reduction of tachycardia by the introduction of phentolamine. It is not possible to prescribe β-adrenergic blockers to phentolamine, as in case of pheochromocytomy, β-adrenergic blockers produce an arterial vise.

Proproxan(Proroxan) block of central and peripheral postsynaptic α 1 -adrenoceptor and presynaptic α 2 -adrenoceptor. Nadaє hypotensive and sedative. Change in abstinence with stagnation to opioid, alcohol. Introduce propoxan to the shkiru or internally in case of hypertensive crises. Priznachayut all the middle for the prevention of hypertensive crises, with ailments.

β-blockers

β-adrenergic blockers are the first row in case of elimination:

1) tachyarrhythmias and extrasystoles;

2) angina pectoris;

3) arterial hypertension.

At the same hour, the stench is contraindicated in chronic obstructive diseases of the legends, obliterated diseases of the sudins, atrioventricular blots. To reduce physical activity, to reduce dyslipidemia. β-blockers for:

1) β 1 -, β 2-adrenergic blockers;

2) β 1 -adrenoblockers;

3) β-adrenergic blockers with internal activity.

β 1 -, β 2-adrenergic blockers

Up to β 1 -, β 2-blockers (non-selective β-blockers), propranolol, nadolol, Penbutolol, timolol are used.

propranolol(Propranolol; anaprilin, obsidan, inderal) in conjunction with blockade of β 1 -adrenergic receptors:

1) drive the heart's power:

a) I will relax my heart;

b) reduce the speed of the heart (lower the automatism of the sinus university);

c) lowering the automatism of the atrioventricular node and Purkin fibers (in the heart's slings);

d) accelerated atrioventricular conduction;

2) changes in the secretion of the renin of the juxtaglomerular cells of nirok.

Have a sound with blockade of β 2 -adrenergic receptors:

1) the sound of blood-bearing judgments (including coronary);

2) the tone of smooth bronchial mucosa;

3) advancing the rapidity of the myometrium;

4) change the hyperglycemic dyu adrenaline.

Propranolol lipofylene, easily penetrates into the central nervous system. The triviality of propranolol is close to 6 hours. The drug is prescribed in the middle 3 times a day; retard capsules - once a day. In extreme cases, propranolol should be administered intravenously.

Shown before zasosuvannya propranolol:

1) angina pectoris; in connection with weakening and a very fast heart rate propranolol decreases heart rate reduction in vasospastic stenocardia propranolol contraindications.

2) Prevention of myocardial infarction. For a gastrointestinal phase of myocardial infarction, with a stable stagnation of the sickly intake of propranolol, before the repeated infarction and lowering the mortality of ailments (mabut, the value of a decrease in the consumption of cinnamon in the sourness of the coronary artery disease)

3) Heart arrhythmias. Propranolol reduces the automatism of the sinus node, the automatism and performance of the atrioventricular node, the automatism of the Purkin fibers. Effective in supra-mucous tachyarrhythmias: sinus tachycardia, paroxysmal anterior tachycardia, moderate and triple anterior tachycardia (for normalization of the rhythm of fast mucus). It can be used to get stuck in case of extrasystoles that are tied with automatic adjustments.

4) Arterial hypertension. Propranolol reduces the heart wikid (it will weaken and reduce the speed of the heart) and in case of isolated systolic hypertension, the arterial grip may be reduced in case of first stagnation. However, most often, with a one-time intake of propranolol, the arterial grip decreases slightly, so as, blocking β 2 -adrenoreceptors of blood-bearing sudins, propranolol vicliks, the ulceration of the sudins and the movement of the posterior peripheral support of the sudins.

With a systematic use of propranolol for a stretch of 1-2 times, the sound of the sudin changes; the arterial grip is very low. Expanded Sudin Explain:

1) renewals of the baroreceptor depressor reflex (weakening in ailments for hypertensive ailments);

2) attaching nice central infusions to the heart and the judgment;

3) oppressive infusion of propranolol on the secretion of renin (block β 1 -adrenergic receptors);

4) blockade of presynaptic β 2 -adrenergic receptors (the appearance of norepinephrine changes with nice fibers).

Use propranolol as follows:

With hypertrophic cardiomyopathy;

With thyrotoxicosis (symptomatic therapy);

With essential (family) tremor (block of β 2 -adrenoreceptors of skeletal muscles);

For the prophylaxis of migraine (increasing the expansion and pulsation of the brain);

To weaken the abstinence from drinking alcohol;

With trivoses, napruzi (changes in tachycardia).

When pheochromocytomy is treated with α-adrenergic blockers, propranolol is used for lowering the arterial vise for usunenia tachycardia, as well as α-adrenergic blockers. It is not possible to take propranolol to α-adrenergic blockers, as in case of pheochromocytomy, propranolol causes an arterial vise (blocking β 2 -adrenoreceptors of sudin, absorbing sudinosilicidal adrenaline).

Possible effects of propranolol:

Overly weakened heart is fast (heart lack is possible);

Weakness with physical pressure, increased stomachability;

bradycardia;

Difficulty atrioventricular conductivity (contraindications for atrioventricular block II-III stages);

Dryness of the eyes (change in production of tears), xerophthalmia;

Seeing a cold chill (ringing of peripheral vessels);

Increased bronchial tone (bronchospasm may develop in patients with bronchial asthma);

Adjustment of tone and rapid activity of myometry;

Decreased tolerance to glucose, hypoglycemia (loss of hyperglycemic adrenaline associated with activation of β 2 -adrenergic receptors); propranolol according to the strength of hypoglycemic agents.

In addition, there may be nudity, bloating, diarrhea, spasmodic pain in the abdomen, drowsiness, no nightmares, depression, attack of disorientation, hallucination, impotency, alopecia, shkinny. Propranolol appears in the blood plasma at the level of LPDNShch and decreases the level of lipoproteins of high degree.

For the consumption of propranolol bending syndrome: In case of a sharp admitted use of the drug, it is possible to aggravate coronary insufficiency, arterial hypertension.

Protipokazany propranolol at sertsevіy nedostatnostі, sindromі slabkostі sinus vuzla, virazhenoї bradikardії, atrіoventrikulyarnіy blokadі II-III stupenіv, vasospastic stenokardії (stenokardіya Prinzmetal), spasms peripheral character sudin, bronhіalnіy astmі i hronіchnoї obstruktivnoї hvorobi legen (COPD), feohromotsitomі (at feohromotsitomі propranolol pіdvischuє arterіalny vice; to get stuck on aphids of α-adrenergic blockers), vaginosity. Propranolol undergoes hypoglycemic conditions, which can become stagnant in case of diabetic diabetes.

nadolol(Nadolol; corgard) to be considered as propranolol trivial for a day - up to 24 years. Assume all the middle 1 time a day for systematic treatment of hypertensive ailments, angina pectoris.

timolol(Timolol) stasis for arterial hypertension, angina pectoris, for prevention of migraine. The drug is priznachayut vseredinu 2 times for doba.

timolol maleate(Timolol maleate) stagnate in case of intracritical glaucoma in vigellas with intramural drops 1-2 times a day (timolol on the basis of propranolol does not affect muscle anesthesia).

Reducing the internal vice with timolol will bind to changes in the internal production. The internal medicine is to establish itself for the secretion of the cells of the blood vessels (ciliary) blood and the filtration of blood plasma through the endothelium of the blood-bearing vessels. timolol:

1) block of β 2 -adrenergic receptors in the epithelium of the vyykovy body and changes in the secretion of the internal lineage;

2) at the connection with the blockade of β 2 -adrenergic receptors of the blood-bearing vessels of the reaction and changes in the filtration (Table 6).

After putting timolol into the conjunctival microshock, the internal grip will start to decrease in 20 min, the maximum effect will be reached after 2 years; the triviality of the show is close to 24 years old.

Table 6. Preparations that can become stagnant in glaucoma