Esatenolol Actions

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Actions of Esatenolol in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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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.

Esatenolol pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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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

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