No

Antiarrhythmic Agent, Class II; Beta Blocker, Beta₁ Selective

Treatment of supraventricular tachycardia, atrial fibrillation/flutter (primarily to control ventricular rate), and hypertension (especially perioperatively)

C (per manufacturer); D (in 2nd or 3rd trimester, based on expert analysis)

Hypersensitivity to esmolol or any component; sinus bradycardia; heart block greater than first degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; bronchial asthma; uncompensated cardiac failure; hypotension; pregnancy (2nd and 3rd trimesters)

Hypotension is common; patients need close blood pressure monitoring. Administer cautiously in compensated heart failure and monitor for a worsening of the condition. Use caution in patients with PVD (can aggravate arterial insufficiency). Use caution with concurrent use of beta-blockers and either verapamil or diltiazem; bradycardia or heart block can occur. Avoid concurrent I.V. use of both agents. In general, beta-blockers should be avoided in patients with bronchospastic disease. Esmolol, a beta-1 selective beta-blocker, can be cautiously used in patients with bronchospastic disease. Monitor pulmonary status closely. Use cautiously in diabetics because it can mask prominent hypoglycemic symptoms. Can mask signs of thyrotoxicosis. Can cause fetal bradycardia when administered in the third trimester of pregnancy or at delivery. Use caution in patients with renal dysfunction (active metabolite retained). Do not use in the treatment of hypertension associated with vasoconstriction related to hypothermia. Concentrations >10 mcg/mL or infusion into small veins or through a butterfly catheter should be avoided (can cause thrombophlebitis). Extravasation can lead to skin necrosis and sloughing.

>10%:

Cardiovascular: Asymptomatic hypotension (25%), symptomatic hypotension (12%)

Miscellaneous: Diaphoresis (10%)

1% to 10%:

Cardiovascular: Peripheral ischemia (1%)

Central nervous system: Dizziness (3%), somnolence (3%), confusion (2%), headache (2%), agitation (2%), fatigue (1%)

Gastrointestinal: Nausea (7%), vomiting (1%)

Local: Pain on injection (8%)

<1% (Limited to important or life-threatening symptoms): Pallor, flushing, bradycardia, severe bradycardia/asystole (rare), chest pain, syncope, heart block, edema, depression, abnormal thinking, anxiety, fever, lightheadedness, seizures, erythema, skin discoloration, anorexia, dyspepsia, constipation, xerostomia, abdominal discomfort, urinary retention, thrombophlebitis, infusion site reactions, paresthesia, rigors, midcapsular pain, weakness, abnormal vision, bronchospasm, wheezing, dyspnea, nasal congestion, pulmonary edema, congestive heart failure, taste perversion, depression, acne, eczema, psoriasis, skin irritation, pruritus, flushing, alopecia, exfoliative dermatitis, skin necrosis (from extravasation)

Symptoms of intoxication include cardiac disturbances, CNS toxicity, bronchospasm, hypoglycemia and hyperkalemia. The most common cardiac symptoms include hypotension and bradycardia; atrioventricular block, intraventricular conduction disturbances, cardiogenic shock, and asystole may occur with severe overdose, especially with membrane-depressant drugs (eg, propranolol); CNS effects include convulsions, coma, and respiratory arrest (commonly seen with propranolol and other membrane-depressant and lipid-soluble drugs).

Treatment includes symptomatic treatment of seizures, hypotension, hyperkalemia, and hypoglycemia; bradycardia and hypotension resistant to atropine, isoproterenol, or pacing may respond to glucagon; wide QRS defects caused by the membrane-depressant poisoning may respond to hypertonic sodium bicarbonate; repeat-dose charcoal, hemoperfusion, or hemodialysis may be helpful in removal of only those beta-blockers with a small V_d, long half-life, or low intrinsic clearance (acebutolol, atenolol, nadolol, sotalol)

Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.

Clonidine: Hypertensive crisis after or during withdrawal of either agent.

Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.

Glucagon: Esmolol may blunt the hyperglycemic action of glucagon.

NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.

Sulfonylureas: beta-blockers may alter response to hypoglycemic agents.

Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers; avoid concurrent use, especially if I.V. verapamil/diltiazem is used.

Clear, colorless to light yellow solution which should be stored at room temperature and protected from temperatures >40°C

Standard diluent: 5 g/500 mL NS

Class II antiarrhythmic: Competitively blocks response to beta₁-adrenergic stimulation with little or no effect of beta₂-receptors except at high doses, no intrinsic sympathomimetic activity, no membrane stabilizing activity

Onset of beta-blockade: I.V.: Within 2-10 minutes (onset of effect is quickest when loading doses are administered)

Duration of activity: Short, 10-30 minutes; prolonged following higher cumulative doses, extended duration of use

Protein binding: 55%

Metabolism: In blood by esterases

Half-life: Adults: 9 minutes

Elimination: ~69% of dose excreted in urine as metabolites and 2% as unchanged drug

I.V. administration requires an infusion pump (must be adjusted to individual response and tolerance):

Some centers have utilized doses of 100-500 mcg/kg given over 1 minute for control of supraventricular tachycardias.

Loading doses of 500 mcg/kg/minute over 1 minute with maximal doses of 50-250 mcg/kg/minute (mean = 173) have been used in addition to nitroprusside to treat postoperative hypertension after coarctation of aorta repair.

Adults: Loading dose: 500 mcg/kg over 1 minute; follow with a 50 mcg/kg/minute infusion for 4 minutes; if response is inadequate, rebolus with another 500 mcg/kg loading dose over 1 minute, and increase the maintenance infusion to 100 mcg/kg/minute. Repeat this process until a therapeutic effect has been achieved or to a maximum recommended maintenance dose of 200 mcg/kg/minute. Usual dosage range: 50-200 mcg/kg/minute with average dose of 100 mcg/kg/minute.

Esmolol: Hemodynamic effects of beta-blockade return to baseline within 20-30 minutes after discontinuing esmolol infusions.

Guidelines for withdrawal of therapy:

Transfer to alternative antiarrhythmic drug (propranolol, digoxin, verapamil).

Infusion should be reduced by 50% 30 minutes following the first dose of the alternative agent.

Following the second dose of the alternative drug, patient's response should be monitored and if control is adequate for the first hours, esmolol may be discontinued.

Dialysis: Not removed by hemo- or peritoneal dialysis; supplemental dose is not necessary.

Avoid xanthine-containing foods or beverages

Blood pressure, heart rate, MAP, EKG, respiratory rate, I.V. site; cardiac monitor and blood pressure monitor required

Increases cholesterol (S), glucose

Esmolol provides an important mechanism for close titration of rate control in patients with atrial fibrillation. Esmolol may also be beneficial in allowing close blood pressure control. Esmolol should only be administered in intensive care or closely monitored situations. Potential adverse effects include hypotension and bradyarrhythmias. These are usually short-lived because of esmolol's short half-life (9 minutes).

May cause drowsiness, confusion, fatigue, or depression

Barbiturates may decease effects of esmolol

No information available to require special precautions

No effects or complications reported

Esmolol is administered in emergencies, patient education should be appropriate to the situation.

Decrease infusion or discontinue if hypotension, congestive heart failure, etc occur; The 250 mg/mL ampul is not for direct I.V. injection, but must first be diluted to a final concentration not to exceed 10 mg/mL (ie, 2.5 g in 250 mL or 5 g in 500 mL).

Injection, as hydrochloride: 10 mg/mL (10 mL); 250 mg/mL (10 mL)

Angaran DM, Schultz NJ, and Tschida VH, "Esmolol Hydrochloride: An Ultrashort-Acting, Beta-Adrenergic Blocking Agent," Clin Pharm, 1986, 5(4):288-303.

Brunette DD and Rothong C, "Emergency Department Management of Thyrotoxic Crisis With Esmolol," Am J Emerg Med, 1991, 9(3):232-4.

Cuneo BF, Zales VR, Blahunka PC, et al, "Pharmacodynamics and Pharmacokinetics of Esmolol, A Short-Acting Beta-Blocking Agent in Children," Pediatr Cardiol, 1994, 15(6):296-301.

Gorczynski RJ, "Basic Pharmacology of Esmolol," Am J Cardiol, 1985, 56(11):3F-13F.

Gray RJ, "Managing Critically Ill Patients With Esmolol: An Ultra-Short Acting Beta-Adrenergic Blocker," Chest, 1988, 93(2):398-403.

Lowenthal DT, Porter RS, Saris SD, et al, "Clinical Pharmacology, Pharmacodynamics and Interactions With Esmolol," Am J Cardiol, 1985, 56(11):14F-18F.

Luyt D, Dance M, Litmanovich H, et al, "Esmolol in the Treatment of Severe Tachycardia in Neonatal Tetanus," Anaesth Intensive Care, 1994, 22(3):303-4.

Trippel DL, Wiest DB, and Gillette PC, "Cardiovascular and Antiarrhythmic Effects of Esmolol in Children," J Pediatr, 1991, 119(1):142-7.

Vincent RN, Click LA, Williams HM, et al, "Esmolol As an Adjunct in the Treatment of Systemic Hypertension After Operative Repair of Coarctation of the Aorta," Am J Cardiol, 1990, 65(13):941-3.

Wiest DB, "Esmolol: A Review of Its Therapeutic Efficacy and Pharmacokinetic Characteristics," Clin Pharmacokinet, 1995, 28(3):190-202.

Wiest DB, Garner SS, and Childress LM, "Stability of Esmolol Hydrochloride in 5% Dextrose Injection," Am J Health Syst Pharm, 1995, 52(7):716-8.

Wiest DB, Trippel DL, Gillette PC, et al, "Pharmacokinetics of Esmolol in Children," Clin Pharmacol Ther, 1991, 49(6):618-23.