Non-selective betta – substance . It has an antianginal, hypotensive and antiarrhythmic effect . Selectivity blocking the Betka -adrenoceptors (75% beta1 and 25% beta2-adrenoceptor), sokraschayaet stimulated by catecholamines formation of cAMP from ATP , in consequence of which also reduces the intracellular influx of calcium exhibits a Propranolol cost negative chronotropic, dromo-, BATM and inotropic effect (urezhaet frequency of soul decreases , suppresses electrical conductivity and emotionality , reduces myocardial contractility).
The source of the use Betka adrenoblokatorov single peripheral vennoe resistance in the initial 24 hours increases (in consequence reciprocal increase in active plant -adrenoceptor and elimination of the stimulation of beta2-adrenoceptor blood vessel structural muscle), but by1-3 days back to the initial , and the presence of a continuous direction decreases .
The hypotensive result is associated with a reduction in the short size of the heart, sympathetic stimulation of the peripheral blood vessel , a decrease in the active enzyme — an angiotensin concept ( contains significance in patients with initial renin hypersecretion), sensitivity of the baroreceptors of the aortic arch ( not performed an increase in their activity in the result in a reduction of the best ) and exposure to the main nervous concept . The hypotensive Propranolol cost result stabilizes by the end of 2 months of the course direction .
The antianginal effect is caused by a decrease in the need for myocardium in oxygen ( due to the result of a negative chronotropic and inotropic result ). Decrease in the frequency of mental decreases leads to diastole lengthening and improvement of myocardial perfusion. Due to the result of an increase in the final relaxation pressure in the left ventricle and an increase in the stretching of the muscle fibers of the ventricles can increase the need for oxygen, especially in patients with persistent mental illness.
Antiarrhythmic outcome is determined by the elimination of arrhythmogenic conditions (tachycardia, high active sympathetic nervous concept , increased location of cAMP, arterial hypertension), a reduction in the speed of unexpected excitement of sinus and ectopic rhythm drivers and a slower atrioventricular performance . The suppression of the fulfillment of impulses is noticed to a greater extent in the antegrade and at the lowest level in the reaction flows by means of the atrioventricular segment and according to the auxiliary routes Propranolol cost . According to the systematization of antiarrhythmic pharmaceutical money belongs to the category II substances . Reduced severity of myocardial ischemia – due to the result of reducing the need for myocardium in oxygen, post-infarction mortality can also be reduced due to antiarrhythmic effects . The ability to prevent the formation of primary unwell venous origin determined reduction in the severity of the expansion of the cerebral arteries due Betka -adrenoblokady governmental receptor inhibition generated catecholamines platelet aggregation and lipolysis, decrease in platelet adhesiveness, warning activation conditions clotting monthly in the period of the release of adrenaline stimulation of income of air in the matter and the reduction of renin secretion.
Reducing tremor in the background using propranolol is able to be caused by the war of beta2-adrenoreceptors. Increases atherogenic quality monthly . Increases the reduction of the uterus ( unexpected and initiated by pharmaceutical instruments , stimulating myometrium). Increases the activity of the bronchi.
Pharmacokinetics. Immediately and in sufficient detail (90%) , the presence of the method is absorbed inside and is relatively instantly introduced withorganism. Bioavailability after oral method is THIRTY -40% ( the result of ” first pass” through the liver , microsomal oxidation ), the presence of continuous process – increasing ( having metabolites which inhibit liver enzymes), its size is dependent on a disposition of food and saturation hepatic blood flow Propranolol cost. Metabolized by glucuronidation in the liver.The greatest concentration in the monthly plasma is achieved through 1-1.5 hours. It has significant lipophilicity, accumulates in the simple matter , the leading brain, the kidneys, the soul . It falls through the blood-brain and viviparous obstacles into deep milk . The relationship with plasma proteins monthly – 90-95%. The size of the distribution – 3-5 liters / kg. It enters the bile into the intestinal tract. is degraded and reabsorbed. The half-life interval is 3-5 minutes , in the background of course implementation it can stretch up to 12 times . Injected by the kidneys – 90%, in the unmodified version – less than 1%. The presence of hemodialysis is not removed .