esmolol

Absorption: IV administration results in complete bioavailability.

Distribution: Rapidly and widely distributed.

Metabolism/Excretion: Metabolized by enzymes in RBCs and liver.

Half-Life: 9 min.

Time/Action Profile ⬆ ⬇

(antiarrhythmic effect)

ROUTE	ONSET	PEAK	DURATION
IV	within min	unknown	1–20 min

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Uncompensated HF;
Pulmonary edema;
Cardiogenic shock;
Bradycardia or heart block;
Known alcohol intolerance;
Lactation: Lactation.

Use Cautiously in:

Thyrotoxicosis (may mask symptoms);
Diabetes mellitus (may mask symptoms of hypoglycemia);
Patients with a history of severe allergic reactions (intensity of reactions may be ↑);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; may cause fetal bradycardia, uterine blood flow, and fetal hypoxia if used during the last trimester;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may have sensitivity to the effects of beta blockers.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, peripheral ischemia

Derm: sweating

Endo: hypoglycemia

F and E: hyperkalemia

GI: nausea, vomiting

Local: injection site reactions

Neuro: fatigue, agitation, confusion, dizziness, drowsiness, weakness

Interactions ⬆ ⬇

Drug-drug:

General anesthesia, IV phenytoin, and verapamil may cause additive myocardial depression.
Additive bradycardia may occur with digoxin.
Additive hypotension may occur with other antihypertensives, acute ingestion of alcohol, or nitrates.
Concurrent use with amphetamine, cocaine, ephedrine, epinephrine, norepinephrine, phenylephrine, or pseudoephedrine may result in unopposed alpha-adrenergic stimulation (excessive hypertension, bradycardia).
Concurrent thyroid hormone administration may ↓ effectiveness.
May alter the effectiveness of insulins or oral hypoglycemic agents (dose adjustments may be necessary).
May ↓ effectiveness of theophylline.
May ↓ beneficial beta cardiovascular effects of dopamine or dobutamine.
Use cautiously within 14 days of MAO inhibitor therapy (may result in hypertension).

Route/Dosage ⬆ ⬇

IV (Adults ): Antiarrhythmic: 500-mcg/kg loading dose over 1 min initially, followed by 50-mcg/kg/min infusion for 4 min; if no response within 5 min, give 2nd loading dose of 500 mcg/kg over 1 min; then ↑ infusion to 100 mcg/kg/min for 4 min. If no response, repeat loading dose of 500 mcg/kg over 1 min and ↑ infusion rate by 50-mcg/kg/min increments (not to exceed 200 mcg/kg/min for 48 hr). As therapeutic end point is achieved, eliminate loading doses and decrease dose increments to 25 mg/kg/min. Intraoperative antihypertensive/antiarrhythmic: 250–500-mcg/kg loading dose over 1 min initially, followed by 50-mcg/kg/min infusion for 4 min; if no response within 5 min, give 2nd loading dose of 250–500 mcg/kg over 1 min;, then ↑ infusion to 100 mcg/kg/min for 4 min. If no response, repeat loading dose of 250–500 mcg/kg over 1 min and ↑ infusion rate by 50-mcg/kg/min increments (not to exceed 200 mcg/kg/min for 48 hr).
IV (Children ): Antiarrhythmic: 50 mcg/kg/min, may be ↑ every 10 min up to 300 mcg/kg/min.

Availability ⬆ ⬇

(Generic available)

Solution for injection (for use as loading dose): 10 mg/mL
Premixed infusion: 2000 mg/100 mL; 2500 mg/250 mL

Assessment ⬆ ⬇

Monitor BP, ECG, and pulse frequently during dose adjustment period and regularly during therapy. The risk of hypotension is greatest within the first 30 min of starting esmolol infusion. Hold therapy for severe bradycardia or 2nd/3rd degree heart block.
Monitor for bronchospasm in patients with asthma or COPD.
Monitor intake and output ratios and daily weights. Assess routinely for signs and symptoms of HF (dyspnea, rales/crackles, weight gain, peripheral edema, jugular venous distention). Hold therapy if cardiogenic shock or decompensated HF develops.
Assess infusion site frequently during therapy. Concentrations >10 mg/mL may cause injection site reaction (redness, swelling, skin discoloration, and burning at the injection site). Do not use small veins or butterfly needles for administration. If venous irritation occurs, stop the infusion and resume at another site.
Monitor for signs and symptoms of hypoglycemia (sweating, nausea, tachycardia). Tachycardia may be prevented by esmolol. If hypoglycemia occurs, seek emergency treatment.
Assess electrolytes regularly during therapy; may cause life-threatening hyperkalemia (↑ risk if renal impairment).

Toxicity and Overdose:

Monitor patients receiving esmolol for signs of overdose (bradycardia, severe hypotension, severe dizziness or fainting, severe drowsiness, dyspnea, bluish fingernails or palms, seizures).
- IV glucagon and symptomatic care are used in the treatment of esmolol overdose. Because of the short action of esmolol, discontinuation of therapy may relieve acute toxicity.

Implementation ⬆ ⬇

IV vasoactive medications are inherently dangerous. Esmolol is available in different concentrations; fatalities have occurred when loading dose vial is confused with concentrated solution for injection, which contains 2500 mg in 10 mL (250 mg/mL) and must be diluted. Before administering, have second practitioner independently check original order, dose calculations, and infusion pump settings.
Do not confuse Brevibloc with Brevital. If both are available as floor stock, store in separate areas.

IV Administration:

Diluent: The 10-mg/mL vial should be used for the loading dose. These vials are already diluted. No further dilution is needed..
Diluent: Premixed infusions are already diluted and ready to use. Solution is clear, colorless to light yellow; do not administer solutions that are discolored or contain particulate matter. Do not remove overwrap until ready to use. Use within 24 hr once opened.Concentration: Premixed 10 mg/mL and 20 mg/mL.
Rate: Based on patient's weight (see Route/Dosage section). Titration of dose is based on desired heart rate or undesired decrease in BP. Esmolol infusions should not be abruptly discontinued; the infusion rate should be tapered.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of esmolol to patient.
May cause drowsiness. Caution patients receiving esmolol to call for assistance during ambulation or transfer.
Advise patients to change positions slowly to minimize orthostatic hypotension.
Patients with diabetes should closely monitor blood glucose, especially if weakness, malaise, irritability, or fatigue occurs. Medication does not block dizziness or sweating as signs of hypoglycemia.
Advise patient to call right away for chest pain, trouble breathing, nausea, unusual sweating, light-headedness, feeling faint, itchiness, numbness in hands or feet, warmth/redness in upper body (face, neck, arms, chest).
Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnant. Avoid breastfeeding during therapy. May cause fetal bradycardia.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇