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Metoprolol refers to cardioselective blockers of β-adrenergic receptors, which do not possess internal sympathomimetic activity and membrane-stabilizing properties. Has antihypertensive, antianginal and antiarrhythmic action.
Blocking at low doses β-adrenoreceptors of the heart, reduces catecholamine-stimulated cAMP formation from ATP, reduces intracellular current of Ca2 +, has a negative chrono-, dromo-, batmo- and inotropic action (tends to decrease heart rate, inhibits conduction and excitability, reduces myocardial contractility) .
The total peripheral resistance at the beginning of the use of β-blockers (in the first 24 hours after oral administration) increases (as a result of the reciprocal increase in α-adrenergic receptor activity and elimination of β-adrenergic receptor stimulation), which returns to the initial one after 1-3 days, appointment - is reduced.
An acute antihypertensive effect is due to a decrease in cardiac output, a stable antihypertensive effect develops within 2-3 weeks and is due to a decrease in renin synthesis, and plasma renin accumulation, inhibition of renin-angiotensin system activity (important in patients with initial hypersecretion of renin) and CNS restoration of sensitivity baroreceptors of the aortic arch (there is no increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic Lying. Reduces elevated blood pressure at rest, with physical stress and stress.
The antianginal effect is determined by the reduction in myocardial oxygen demand as a result of a decrease in the heart rate (diastolic elongation and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to sympathetic innervation. Reduces the number and severity of angina attacks and increases the tolerance of exercise. BP decreases after 15 minutes, maximum - after 2 hours and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular intake.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and slowing AV conduction (mainly in the antegrade and, to a lesser extent, retrograde directions via the AV node) and by additional paths. With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart diseases and hyperthyroidism, it decreases the heart rate, or even can lead to the restoration of sinus rhythm. Prevents the development of migraine.
When used at average therapeutic doses, in contrast to nonselective beta-blockers, it exerts a less pronounced effect on organs containing β-adrenergic receptors (pancreas, skeletal muscles, smooth musculature of peripheral arteries, bronchi and uterus) and carbohydrate metabolism. When used in large doses (more than 100 mg / day) has a blocking effect on both subtypes of β-adrenoreceptors.
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Buy Metoprolol
-Arterial hypertension (as a monotherapy or in combination with other antihypertensive agents), including hyperkinetic type, tachycardia;
- ischemic heart disease: myocardial infarction (secondary prevention-complex therapy), prevention of angina attacks;
- heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole);
- hyperthyroidism (complex therapy);
- prevention of migraine attacks.