Esatenolol (Esatenololum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Beta-blockers

Included in the formulation
  • Estecor
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    AKTAVIS GROUP, AO     Iceland
    • АТХ:

    C.07.A.B   Selective beta-blockers

    C.07.A.B.03   Atenolol

    Pharmacodynamics:

    S (-) enantiomer of atenolol, selective β1-adrenoceptor without internal sympathomimetic activity. Has antihypertensive, antiarrhythmic, anti-anginal action.

    Due to the blockade of β1-adrenoceptor has a negative foreign, chrono-, butmotropic effect for 24 hours.

    Antianginal effect is due to a decrease in myocardial oxygen demand with prolonged diastole.

    In therapeutic doses does not affect the tone of peripheral arteries.

    Pharmacokinetics:

    After oral administration, an empty stomach is absorbed in the gastrointestinal tract up to 50%. The maximum concentration in the blood plasma is reached after 3 hours. The connection with plasma proteins is up to 16%.

    The half-life is 4 hours.

    Poorly penetrates the blood-brain barrier, penetrates the placenta. Partially metabolized in the liver, eliminated by the kidneys. When hemodialysis is removed from the blood plasma.

    Indications:

    Arterial hypertension, hypertensive crisis, neurocirculatory dystonia according to the hypertonic type; ischemic heart disease, angina pectoris (with the exception of Prinzmetal angina), arrhythmias.

    ICD-10

    IX.I10-I15.I10   Essential [primary] hypertension

    IX.I20-I25.I20   Angina pectoris [angina pectoris]

    IX.I30-I52.I47   Paroxysmal tachycardia

    IX.I30-I52.I48   Atrial fibrillation and flutter

    IX.I30-I52.I49   Other disorders of the heart rhythm

    Contraindications:

    Cardiogenic shock, atrioventricular blockade of II-III degree, bradycardia, chronic heart failure in decompensation stage, bronchial asthma, peripheral arterial circulation disorders, renal and hepatic insufficiency, individual intolerance.

    Carefully:

    Chronic bronchitis with an asthmatic component, obliterating arterial diseases, atrioventricular blockade of the 1st degree, disturbance of the water-electrolyte balance.

    Pregnancy and lactation:

    Recommendations for FDA - Category D. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside once a day for 30-40 minutes before meals for 12.5 mg, if necessary, increase the dose to 50 mg.

    Side effects:

    Central nervous system: dizziness, insomnia, asthenia.

    Respiratory system: shortness of breath, rarely - bronchospasm

    The cardiovascular system: bradycardia, atrioventricular blockage, cold extremities.

    Blood System: neutropenia, thrombocytopenia.

    Sense organs: "dry eye syndrome", transient visual impairment.

    Gastrointestinal tract: dyspepsia, diarrhea, or constipation.

    Reproductive system: lowering the potency.

    Leather: hyperhidrosis.

    Allergic reactions.

    Overdose:

    Symptoms: pronounced bradycardia, arterial hypotension.

    Treatment: intravenously 1-2 mg atropine, 2.5 μg / kg dobutamine, intravenously bolus 10 mg glucagon, intravenously drop 10-20 μg isoprenaline at a rate of not more than 5 μg / min.

    Interaction:

    Potentiates the effect of lidocaine in systemic application.

    Strengthens the negative dromo-, ino-, chromotropic action of amiodarone, anesthetics, antiarrhythmics, diltiazem, verapamil.

    Cimetidine increases the bioavailability of esatenolol.

    Special instructions:

    During the treatment it is necessary to control the heart rate and blood pressure, blood glucose.

    For general anesthesia in patients taking esatenolol, should be used with minimal inotropic action. Before surgery, it is recommended to cancel the drug 48 hours prior to surgery.

    In the treatment of esatenolol, it is recommended to refrain from driving a car and working with moving mechanisms.

    Instructions
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