Esmolol


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV Supraventricular arrhythmias Loading dose (optional): 500 mcg/kg over 1 min. Maintenance: 50 mcg/kg/min for 4 min. If response is satisfactory, continue maintenance infusion. If satisfactory response is not achieved, titrate infusion in increments of 50 mcg/kg/min for 4 min to max 200 mcg/kg/min until desired response is achieved; may admin optional loading dose of 500 mcg/kg over 1 min prior to each infusion rate increase. Once response is satisfactory, maintain infusion for up to 48 hr, if necessary. Perioperative HTN and/or tachycardia During anaesth: Loading dose of 80 mg over 15-30 sec, followed by an infusion of 150 mcg/kg/min, may increase to 300 mcg/kg/min if necessary. After anaesth: 500 mcg/kg/min infused for 4 min followed by another infusion of 300 mcg/kg/min as needed. Post-op: Loading dose (optional): 500 mcg/kg over 1 min. Maintenance: 50 mcg/kg/min for 4 min. If response is satisfactory, continue maintenance infusion. If response is unsatisfactory, titrate infusion in increments of 50 mcg/kg/min for 4 min to max 300 mcg/kg/min until desired response is achieved; may admin optional loading dose of 500 mcg/kg over 1 min prior to each infusion rate increase.
Dosage Details
Intravenous
Rapid temporary control of ventricular rate in supraventricular arrhythmias
Adult: Loading dose (optional): 500 mcg/kg over 1 min followed by a maintenance infusion of 50 mcg/kg/min for 4 min. If response is satisfactory, continue maintenance infusion. If satisfactory response is not achieved, titrate infusion in increments of 50 mcg/kg/min for 4 min to max 200 mcg/kg/min until desired response is achieved; may admin optional loading dose of 500 mcg/kg over 1 min prior to each infusion rate increase. Once response is satisfactory, maintain infusion for up to 48 hr, if necessary.

Intravenous
Perioperative hypertension and/or tachycardia
Adult: During anaesth: Loading dose of 80 mg over 15-30 sec, followed by an infusion of 150 mcg/kg/min, may increase to 300 mcg/kg/min if necessary. After anaesth: 500 mcg/kg/min infused for 4 min followed by another infusion of 300 mcg/kg/min as needed. Post-op: Loading dose (optional): 500 mcg/kg over 1 min. Maintenance: 50 mcg/kg/minute for 4 min. If response is satisfactory, continue maintenance infusion. If response is unsatisfactory, titrate infusion in increments of 50 mcg/kg/min for 4 min to max 300 mcg/kg/min until desired response is achieved; may admin optional loading dose of 500 mcg/kg over 1 min prior to each infusion rate increase.
Incompatibility
Diazepam, furosemide, Na bicarbonate, or thiopental Na.
Contraindications
Sinus bradycardia, 2nd and 3rd degree AV block, sick sinus syndrome, cardiogenic shock, overt cardiac failure, pulmonary HTN, untreated phaeochromocytoma, metabolic acidosis, severe asthma. Concomitant admin w/ vasoconstrictive and inotropic agents (e.g. epinephrine, norepinephrine, dopamine), IV Ca channel blockers (e.g. verapamil).
Special Precautions
Patients w/ inadequate cardiac function, well-compensated heart failure, bronchospastic disease, myasthenia gravis, conduction disorder, peripheral vascular disease. May mask signs and symptoms of hypoglycaemia and hyperthyroidism. Avoid abrupt withdrawal as it may precipate thyroid storm or MI, and may exacerbate angina and ventricular arrhythmias. Renal impairment. Pregnancy and lactation.
Adverse Reactions
Hypotension, bradycardia, heart block, syncope, peripheral ischaemia, pallor, flushing, nausea, vomiting, anorexia, dizziness, somnolence, paraesthesia, diaphoresis, headache, agitation, fatigue, asthenia, confusion, depression, anxiety, agitation, bronchospasm, wheezing, dyspnoea, nasal congestion.
IV/Parenteral: C
MonitoringParameters
Monitor BP. Perform continuous ECG, monitor respiratory rate, serum K esp in patients w/ renal impairment.
Overdosage
Symptoms: Severe hypotension, bradycardia, AV block, cardiac insufficiency, cardiogenic shock, cardiac arrest, bronchospasm, respiratory depression, sleep and mood disturbances, fatigue, loss of consciousness to coma, convulsions, mesenteric ischemia, peripheral cyanosis, nausea, vomiting, hypoglycaemia and hyperkalaemia. Management: Symptomatic and supportive treatment. IV atropine sulfate may be given for symptomatic bradycardia. IV admin of a cardiac glycoside and/or a diuretic for the management of heart failure and admin of fluids or pressor agents for the management of symptomatic hypotension. IV glucagon for myocardial depression and hypotension. For the management of shock resulting from inadequate cardiac contractility, a vasopressor and/or a positive inotropic agent (e.g., dobutamine, dopamine, isoproterenol) may be given and for bronchospasm, a β2-adrenergic agonist and/or a theophylline derivative.
Drug Interactions
May increase serum digoxin levels. Additive effects w/ catecholamine-depleting drugs (e.g. reserpine). May prolong neuromuscular blockade of succinylcholine. May increase serum levels w/ morphine or warfarin. May decrease hypotensive effects w/ NSAIDs.
Potentially Fatal: May lead to fatal cardiac arrest w/ IV Ca channel blockers (e.g. verapamil). Increased risk of reducing cardiac contractility in presence of high systemic vascular resistance w/ vasoconstrictive or inotropic drugs (e.g. dopamine, norepinephrine, epinephrine).
Action
Description: Esmolol is a short-acting cardioselective agent, which competitively blocks β1-adrenergic receptor while having little effect on the β2-adrenergic receptors of bronchial and vascular smooth muscle. At high doses, selectivity usually diminishes, and the drug will competitively inhibit β1- and β2-adrenergic receptors.
Onset: 2-10 min.
Duration: 10-30 min.
Pharmacokinetics:
Distribution: Volume of distribution: Approx 3.4 L/kg (esmolol); approx 0.4 L/kg (acid metabolite). Plasma protein binding: Approx 55%.
Metabolism: Rapidly hydrolysed by esterases in the RBC.
Excretion: Via urine (approx 73-88% as acid metabolite; 2% as unchanged drug). Elimination half-life: Approx 9 min.
Storage
Store at 25°C. Protect from freezing. Avoid excessive heat.
MIMS Class
References
Anon. Esmolol: Drug Information. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/12/2013.

Brevibloc (Baxter). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 06/12/2013.

Buckingham R (ed). Esmolol HCl. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/12/2013.

McEvoy GK, Snow EK, Miller J et al (eds). Esmolol HCl. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/12/2013.

Wickersham RM. Esmolol. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed 06/12/2013.

Disclaimer: This information is independently developed by MIMS based on Esmolol from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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