Chapter: Modern Pharmacology with Clinical Applications: Pharmacological Management of Chronic Heart Failure

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Esmolol

Esmolol (Brevibloc) is a short-acting intravenously ad-ministered β1-selective adrenoceptor blocking agent.

Esmolol

Esmolol (Brevibloc) is a short-acting intravenously ad-ministered β1-selective adrenoceptor blocking agent. It does not possess membrane-stabilizing activity or sym-pathomimetic activity.

Electrophysiological Actions

Esmolol’s electrophysiological actions are similar to those of propranolol.

Hemodynamic Effects

Esmolol decreases arterial pressure, heart rate, ventric-ular contractility, and pulmonary vascular resistance.

Pharmacokinetics

The pharmacokinetic characteristics of esmolol:

Oral bioavailability : 100%

Onset of action : 15–30 minutes

Peak response : 2–5 minutes

Duration of action : 20–30 minutes

Plasma half-life : 3.7 hours

Primary route of metabolism : Hepatic

Primary route of excretion : Renal

Therapeutic serum concentration : 0.4–1.2  μg /mL

Clinical Uses

Esmolol is used in the treatment of supraventricular tachyarrhythmias for rapid control of ventricular rate and reduction of myocardial oxygen consumption. Discontinuation of administration is followed by a rapid reversal of its pharmacological effects because of es-molol’s rapid hydrolysis by plasma esterases.

Adverse Effects and Contraindications

The most frequently reported adverse effects are hy-potension, nausea, dizziness, headache, and dyspnea. As with many β-blocking drugs, esmolol is contraindicated in patients with overt heart failure and those in cardio-genic shock.

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