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.
Esmolol’s electrophysiological actions are similar to those of propranolol.
Esmolol decreases arterial pressure, heart rate, ventric-ular contractility, and pulmonary vascular resistance.
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
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.
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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