IntravenousRapid temporary control of ventricular rate in supraventricular arrhythmiasAdult: 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.
IntravenousPerioperative hypertension and/or tachycardiaAdult: 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.
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Diazepam, furosemide, Na bicarbonate, or thiopental Na.
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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).
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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.
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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.
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Monitor BP. Perform continuous ECG, monitor respiratory rate, serum K esp in patients w/ renal impairment.
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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.
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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).
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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.
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Store at 25°C. Protect from freezing. Avoid excessive heat.
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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.
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