Directory → Wegetotropona funds → Adrainoliticaskie funds → Beta-adrenoblokatora
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The groupBeta-adrenoblokatora (beta-adrainolitiki) is a group of drugs that are specific blocking effects Stimulation бета-адренореактивны�� of the body's systems. Since beta-adrainoretseptora mostly in the heart of (their excessive initiation leads to the witness in the face of sokratimosti and oxygen consumption), bronchitis (stimulation, relaxation bronchi), and pressure (Activation - vazodilatation), easily projected effects of drugs in this group (antiaritmicski, antianginalny, gipotenzivny, bronhaakonstrictornyi etc.), and testify to their application.
Miscellaneous beta-adrenoblokatora vary in the range of beta-retseptora. Preparations selective blocker beta_1-adrainoretseptora, predominantly localized in the heart (cardiomiotita, cells carrying systems), as cardioselektivei (nebivolol, metoprolol, atenolol, talinolol, etc.). They also have an impact on бета_1-адренорецептор�� ukstaglomerulyarnogo apparatus kidneys and adipose tissue. Others (propranolol, oxprenolol, pindolol, timolol, etc.) operate simultaneously in the бета_1-адренорецептор�� and �ета_2-адренорецепторы �ronhov, peripheral vessels, pancreas, liver, skeletal muscles), and they are known neselektivei (blind). It is important to recognize that cardioseleguosti is not absolute : in high doses or long-term use "selective" " бета_1-адреноблокатор�� block �ета_2-адренорецепторы . It has been observed that cardioselektivee beta-adrenoblokatora more effective in the prevention of cardiovascular complications in the face of hypertensive disease and ischemic heart disease than selective.
Some beta-adrenoblokatora (propranolol, timolol, atenolol, etc.), in collaboration with beta-adrainoretseptorami only affect the their mediator (norarenalina). Others, in addition, the slightly stimulated receptors, ie imitate effect (albeit weak) mediator. These medicines (oxprenolol, talinolol, pindolol, etc.) of the so-called internal simpatomimeticescoy activity. Beta-adrenoblokatora deprived of this property, urejaut and weakened heart reduction, and with them, expressed impact on the variation is not.
Beta-adrenoblokatora also show differences in the availability of мембраностабилизирую щих properties ( местноанестезирующий �hinidinopodobnyy effects). Thus, propranolol, oxprenolol, pindolol, talinolol etc., as opposed to atenolola etc. have mestnoanesteziruta and hinidinopodobna activity. Some of these drugs block potassium (offer unique products protiwaritmicakih Class III), and sodium (properties preparations Class I) channels cardiomyocytes. The clinical significance and physico-chemical properties beta-adrenoblokatorov, incl. solubility in fats and water. Thus, lipofile beta-adrenoblokatora (metoprolol, nebivolol, betaxolol, oxprenolol, timolol, propranolol, etc.) quickly and almost completely imbibed from the blood, well pass through gistogematicalkie barriers metabolised in the liver. Features metabolism should be considered in violation of liver function in elderly patients with joint application with drugs, Lack mikrosomaionah activity of liver enzymes. Hydrophilic beta-adrenoblokatora (atenolol, nadolol, sotalol, etc.) are not fully and variabelno imbibed with the ingestion, little metabolised in the liver and normally excretiruyutza kidney in an unmodified form, either in the form of metabolites. They even penetrate GEB, and the least of the side effects of the central nervous system (weakness, insomnia, nightmares, depression, etc.). Amfofile (lipogidrofile) compounds (nebivolol, bisoprolol) are two main ways out from the body, liver metabolism and renal excretion, that allows you to use them in patients with concomitant human liver and kidneys. A lipofile beta-adrenoblokatora have cardioproteguoe effect and the long-term use after myocardial infarction reliably (by 20-50%) reduce mortality.
Negative chrono, and dromo- batmotroponoe effect underlies antiaritmicski effect. Antiaritmicescoe the better was the drugs with a strong мембраностабилизирую щим effect and without internal simpatomimeticescoy activity (propranolol). Beta-adrenoblokatora effective mainly in najeludockovh aritmiah and ekstrasistoliah. Antihypertensive effect of a decrease in heart emission curves, round, braking secreta renin, baroreflectornah change the arc rivers and karotidnyi elevation, the influence of the sosudodwigatelny oblong brain, increase vazodilatiruth release substances (PGE_2 and PGI_2, nitrogen oxide, predserdnyi natriyureticski factor, etc.). Beta-adrenoblokatora reduce suffering left heart impede free-radical processes, and the peroxide oxidation of lipids. A particular range of activity has nebivolol, which, together with the blockade vsokoizbiratelna бета_1-адренорецептор��в (affinity for him 293 times higher than beta_2-adrainoretseptoram), modulating the release endotelialnogo vazodilatirutego factor-nitric oxide (NO). Typically, antigipertenzivny effect reaches its maximum by the end of 2-3-i week. An exception is esmolol (beta_1-seleguy blokator ultrakorotki action), which is used in the treatment of PNDS krizov and acute coronary syndromes. Prolongirovanne forms cardioselektiveh бета-адреноблокаторо�� make it possible to control predutrenny recovery and daily fluctuations AD editing zircadnosti rhythms in patients with arterial disease.
Antianginalnoe Effects бета-адреноблокаторо�� to the needs of low heart of oxygen (at the expense of work and the energy cost of the heart), and the redistribution of coronary blood flow in favour ishemizirovannah pockets.
Beta-adrenoblokatora widely applied for the treatment of cardiovascular diseases. They appoint the heart, human heart rhythm, arterial disease spread in the face of giperkateholaminemii and gipersimpatikotonia. They have been used in tireotoxicose because not only weaken tachycardia, and gipertermiu giperkineziu but also violate tiroksina move in a more proactive triyodtironin; feohromotsytome (only in conjunction with the �льфа-адреноблокатора ми) , and some other functional states involving palpitations caused by excessive stimulation �ета-адренорецепторов . Some evidence, such as anxiety and panic disorders due to the ability бета-адреноблокаторо�� CNS oppress and to anxiolytic effect. Effectiveness of drugs of this group in the prevention of migraines, treatment essencialnogo tremora schizophrenia, parkinsonizma, tarditivna psoriasis, gastrointestinal bleeding in patients with cirrhosis of the liver, withdrawal syndrome, including drink, etc.
A local software in the form of eye drops beta-adrenoblokatora (timolol, etc.) reduce production watery moisture, and probably increase its capital to reduce inner pressure. This effect makes it possible to use for the treatment of glaucoma.
Various side effects and contraindications to the use of бета-адреноблокаторо�� connected with the �ета-адренорецепторов �Many organs and tissues of the body. For example, running бета_2-адренорецептор�� beta-kletok pancreas, to reduce insulin secretion and increase bazalny glucose level. Some observations beta-adrenoblokatora may increase the risk of developing diabetes in predisposed patients which limits their use (especially selective drugs) in this category of patients. Particular caution and control fast required at the time of appointment бета-адреноблокаторо�� against the backdrop of the admission of insulin or oral protivodiabeticakih funds. They can mask the symptoms gipoglikemii, incl. tachycardia.
Selective drugs as a result of the embargo бета_2-адренорецептор��в cause suffering receptacles limbs, the vitality and bronchus cancer (during pregnancy).
Therapy бета-адреноблокатора��и should not be terminated abruptly because Evolution syndrome "lifting". " It occurs in 1-2 days after an abrupt interruption reception is the greatest extent with the four on the 8th day and end on the half hour. It gradually lowering the dose бета-адреноблокаторо�� and to increase the interval between meals. Cancel possible if appointed dose is half or less than the minimum therapeutic.