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Actions of Esatenolol in details
Esatenolol is a cardioselective beta1-blocker without intrinsic sympathomimetic activity. This medication has antihypertensive, antianginal and antiarrhythmic action. Atenolol reduces the stimulatory effect on the heart sympathetic innervation and circulating catecholamines.
The hypotensive effect of this drug is associated with a decrease in minute volume of blood, decreased activity of the renin-angiotensin system (has a greater significance for patients with initial hypersecretion of renin), sensitivity of baroreceptors of the aortic arch (not going to enhance their activity in response to decreased blood pressure) and the effect on the CNS; manifested lower both systolic and diastolic blood pressure, decreasing stroke volume and cardiac output. In the medium therapeutic doses it has no effect on the tone of peripheral arteries.
The antianginal effect of Esatenolol is associated with decreased myocardial oxygen demand by decreasing heart rate (lengthening of diastole and improved myocardial perfusion) and contractility, as well as reduced sensitivity to the effects of myocardial sympathetic innervation. Decrease in heart rate occurs at rest and during exercise.
The antiarrhythmic effect of this medicine is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increase of cAMP, hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of AV conduction.
The hypotensive effect lasts 24 hours, with regular admission is stabilized by the end of 2 weeks of treatment. The negative chronotropic effect is manifested by 1 h after administration, reaches a maximum after in 2-4 hours and lasts up to 24 hours.
After oral administration the absorption of Esatenolol from the gastrointestinal tract is 50-60%, its bioavailability is 40-50%. This drug is practically not metabolized in the body; poorly penetrates the BBB. The plasma protein binding is 6-16%. T1/2 is 6-9 h. Atenolol is primarily excreted by the kidneys in unchanged form. Renal dysfunction accompanied mainly to the increase of T1/2 and cumulation. This medication is excreted during hemodialysis. For elderly patients T1/2 of atenolol is increased.
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Information checked by Dr. Sachin Kumar, MD Pharmacology