What is the use of Esmolol (a beta-1 selective adrenergic receptor blocker)?

From the Guidelines

Esmolol is a short-acting, intravenous beta-1 selective adrenergic receptor blocker used primarily for rapid control of heart rate in various clinical situations, including acute management of supraventricular tachycardias, perioperative control of heart rate and blood pressure, rate control in atrial fibrillation or flutter, and management of sympathetic overstimulation. The typical starting dose is 500 mcg/kg IV over 1 minute, followed by an infusion of 50-300 mcg/kg/min, titrated to desired effect, as recommended by the 2017 European Heart Rhythm Association (EHRA) and ESC Council on Hypertension guidelines 1. For most indications, the target heart rate is usually 60-80 beats per minute. Esmolol is commonly used for:

• Acute management of supraventricular tachycardias
• Perioperative control of heart rate and blood pressure
• Rate control in atrial fibrillation or flutter
• Management of sympathetic overstimulation (e.g., thyroid storm) Its ultra-short half-life (about 9 minutes) allows for rapid titration and quick offset of action when discontinued, making it ideal for situations requiring precise control, as noted in the 2016 ACC/AHA/HRS guideline for the management of adult patients with supraventricular tachycardia 1. This characteristic also makes it safer in patients with relative contraindications to beta-blockers, such as those with reactive airway disease. When using esmolol, closely monitor heart rate, blood pressure, and ECG, and be prepared to adjust the dose or discontinue the drug if bradycardia or hypotension occurs, as advised in the 2013 ACCF/AHA focused update incorporated into the ACCF/AHA 2007 guidelines for the management of patients with unstable angina/non-ST-elevation myocardial infarction 1. Have atropine and other resuscitation equipment readily available. Esmolol's rapid action is due to its quick hydrolysis by red blood cell esterases, resulting in inactive metabolites, which contributes to its short duration of action and makes it a valuable tool for acute cardiovascular management, as described in the 2011 ACCF/AHA focused update incorporated into the ACC/aha 2007 guidelines for the management of patients with unstable angina/non-ST-elevation myocardial infarction 1.

From the FDA Drug Label

ESMOLOL HYDROCHLORIDE injection, for intravenous use Initial U. S. Approval: 1986 INDICATIONS AND USAGE Esmolol hydrochloride injection is a beta adrenergic blocker indicated for the short-term treatment of: Control of ventricular rate in supraventricular tachycardia including atrial fibrillation and atrial flutter and control of heart rate in noncompensatory sinus tachycardia Control of perioperative tachycardia and hypertension

The use of Esmolol is for the short-term treatment of:

• Control of ventricular rate in supraventricular tachycardia, including atrial fibrillation and atrial flutter
• Control of heart rate in noncompensatory sinus tachycardia
• Control of perioperative tachycardia and hypertension 2

From the Research

Clinical Use of Esmolol

Esmolol is a beta-1 selective adrenergic receptor blocker used in various clinical settings, including:

• Unstable angina and myocardial infarction 3, 4, 5, 6
• Atrial fibrillation or flutter and supraventricular tachycardia 3, 4, 6
• Peri- and postoperative tachycardia and hypertension 3, 4, 5, 6, 7
• Electroconvulsive therapy 4
• Emergency management of hypertension, tachycardia, or arrhythmia in critical care units, emergency rooms, and surgery 3, 6

Dosage and Administration

The dosage of esmolol varies depending on the clinical setting and diagnosis, with typical doses ranging from 25-300 micrograms/kg/min, often administered with a loading dose or bolus 3, 4, 5, 6. The drug is usually infused intravenously, and its effects can be rapidly reversed by discontinuing the infusion 3, 4, 5, 6, 7.

Adverse Effects

The most frequently reported adverse effect associated with esmolol infusion is hypotension, which can be minimized by careful dosage titration and patient monitoring 3, 4, 5, 6, 7. Other potential adverse effects include diaphoresis and bradycardia 5, 7.

Pharmacokinetic Characteristics

Esmolol has a rapid onset of action, with a distribution half-life of approximately 2 minutes, and a short duration of action due to rapid clearance, with a clearance half-life of approximately 9 minutes 3, 4, 5, 7. The drug is metabolized by red blood cell cytosol esterases, resulting in a rapid return to pretreatment levels within 30 minutes after discontinuation of the infusion 5, 6.