Antianginal, antiarrhythmic, uterotonic, hypotensive effects .
Blocks beta1 and beta2-adrenergic receptors, exhibits a membrane stabilizing effect . Suppresses the automaticity of the sinoatrial area , inhibits the appearance of ectopic sources in the atria, AV combination , ventricles (at the lowest level ). Reduces the pace of execution of excitement in the AV combination according to the Kent beam, to a greater extentin anterograde orientation .
After the process a one-time dose hypotensive result uninterrupted in extent TWENTIETH -24 hours. Hypotension stabilizes to end 2nd week cure .
Propranolol medicine Mechanisms of the hypotensive effect :
Propranolol medicine, by blocking the heart ‘s 1-adrenoreceptors, reduces the sensitive outburst ( decreases the power and frequency of decreases in the heart);
By blocking 1-adrenoreceptors in juxtaglomerular cells of the kidneys,reduces accentuation of renin, as a result decreases the combination of angiotensin II, which has manifested vasoconstrictive properties (the enzyme generates the conversion of angiotensinogen to hormone I, which is further converted to hypertensive II).
Propranolol medicine resumes the susceptibility of a weakened or confused baroreceptor depressor reflex (the presence of a hypertensive disease is given the reaction is suppressed due to a decrease in the susceptibility of aortic arch baroreceptors).
Reducing the separation norepinephrine closes adrenergic fibers ( due to war presynaptic adrenoceptor).
Propranolol medicine The oppression of the main links of the sympathetic regulation of the vascular tone.
The mechanism of antianginal effects : reduces heart rate, reduces the power of mental decreases , in consequence reduces the need for myocardium in oxygen. Reduces kidneybleeding , and rate of glomerular filtration. The one-time adoption of prolonged configurations is equivalent to the administration of certain doses of Propranolol medicine hydrochloride. The presence of prolonged use reduces vascular return , exerts a cardioprotective effect ( accurately reduces the risk of secondary myocardial infarction and sudden death in twentieth -50%). In patients with moderateconfiguration of hypertension – reduces the possibility of the formation of coronary artery disease and medullary strokes. The presence of coronary artery disease reduces the frequency of seizures , increases the transportability of physiological loads, reduces the need for nitroglycerin. More rezultativen in patients of young of the year ( up to FORTY years ) with hyperdynamic view blood flow and the presence of an enlargedrenin content. Increases the activity of bronchial and uterine contractility ( sokraschayaet bloodstream presence families and in the postoperative stage ) increases secretory and slide dynamic TRACT . Delays platelet aggregation and activates fibrinolysis. It inhibits lipolysis in fatty matter , preventing an increase in degree of independent plump acids ( the presence of a given concentration ofplasma triglycerides and atherogenic index increase . It inhibits glycogenolysis, the secretion of glucagon and insulin, the conversion of thyroxin to triiodothyronine. Reduces intraocular influence , reduces the secretion of liquid moisture .
Reduction of tremor is caused more by a block of – adrenoreceptors of the structural muscles .
Anxiolytic ( decrease in anxiety , fear , anxiety) is associated with a weakening of somaticsigns of anxiety . Prophylaxis -governmental main unwell ( pain ) – due to obstruction of the arteries expand, increasing the concentration conditions of coagulation ( insulation -adrenoceptor), reducing aggregation and platelet adhesion suppressing release of renin. Pharmacokinetics:
With the way inside, instantly and almost completely absorbs with TRACT (90%). Bioavailability is THIRTY-40% (the result of the ” 1st passage”) depends on the nature of the food and the saturation of the hepatic blood flow and increases the presence of a long- term method ( metabolites that inhibit liver enzymes appear ). Cmax in plasma is seen by 1-1.5 h or 6 h ( with the goal of a prolonged figure ). Binds with plasma proteins in 90-95%; the elimination half-life is 2-5 h ( TENh with the goal of a prolonged figure ). The size of the distribution – 3-5 l / kg. Accumulates in the lung substance , leading the brain, the kidneys, the soul , flows through viviparous obstacle , it falls into a deep milk . It is subject to glucose gluing in the liver (99%). Injected with bile into the intestinal tract , deglyukuroniruetsya and reabsorbed ( period of half-life in the background of course implementation is capable of stretch up to 12 hours). Excreted by the kidneys in the form of metabolites.
Hypertension, disease , sinus acceleration (including the presence of hyperthyroidism), supraventricular acceleration , tachysystolic model radiance atrial, supraventricular and ventricular arrhythmia , hypertrophic disease , heart attack of the myocardium, loss clamshell valve subaortalny stricture , simpatikoadrenalovy exacerbation ypatients with diencephalic syndrome, neurocirculatory dystonia, portal hypertension, essential tremor , involuntary attacks, hostile actions , pain ( prevention ), additional therapy, the presence of pheochromocytoma ( only in combination with a plant- adrenoblocker), thyrotoxicosis (including preoperative organization ),