esmolol (es-moe-lol) Brevibloc

 Indications

Management of sinus tachycardia and supraventricular

arrhythmias.

Action

Blocks stimulation of beta1(myocardial)-adrenergic receptors.

Does not usually affect beta2(pulmonary, vascular,

or uterine)-receptor sites. Therapeutic Effects:

Decreased heart rate. Decreased AV conduction.

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Rapidly and widely distributed.

Metabolism and Excretion: Metabolized by enzymes

in RBCs and liver.

Half-life: 9 min.

TIME/ACTION PROFILE (antiarrhythmic effect)

ROUTE ONSET PEAK DURATION

IV within minutes unknown 1–20 min

Contraindications/Precautions

Contraindicated in: Uncompensated HF; Pulmonary

edema; Cardiogenic shock; Bradycardia or heart

block; Known alcohol intolerance.

Use Cautiously in: Geri:qsensitivity to the effects

of beta blockers; Thyrotoxicosis (may mask symptoms);

Diabetes mellitus (may mask symptoms of hypoglycemia);

Patients with a history of severe allergic reactions

(intensity of reactions may beq); OB, Lactation,

Pedi: Safety not established; neonatal bradycardia, hypotension,

hypoglycemia, and respiratory depression

may occur rarely.

Adverse Reactions/Side Effects

CNS: fatigue, agitation, confusion, dizziness, drowsiness,

weakness. CV: hypotension, peripheral ischemia.

GI: nausea, vomiting. Derm: sweating. Local: injection

site reactions.

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 maypeffectiveness. May alter the

effectiveness of insulins or oral hypoglycemic

agents (dose adjustments may be necessary). Mayp

effectiveness of theophylline. Maypbeneficial 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, thenqinfusion

to 100 mcg/kg/min for 4 min. If no response, repeat

loading dose of 500 mcg/kg over 1 min andqinfusion

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,

thenqinfusion to 100 mcg/kg/min for 4 min. If no response,

repeat loading dose of 250–500 mcg/kg over 1

min andqinfusion 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 beqevery 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.