Esmolol Hydrochloride
Pronouncation: (ESS-moe-lahl HIGH-droe-KLOR-ide)Class: Beta-adrenergic blocking agent
Trade Names:
Brevibloc
- Injection 10 mg/mL
- Injection 250 mg/mL
Pharmacology
Feedback for Esmolol HCl
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Blocks beta-receptors primarily affecting CV system (eg, decreases heart rate, contractility, BP) and lungs (promoting bronchospasm).
Pharmacokinetics
Distribution
Distribution t ½ is approximately 2 min. 55% is protein bound.
Metabolism
Rapidly metabolized by the esterases in the cytosol of red blood cells to an acid metabolite and methanol.
Elimination
The t ½ is approximately 9 min. Less than 2% excreted unchanged in the urine.
Indications and Usage
Short-term management of supraventricular tachyarrhythmias and noncompensatory sinus tachycardia.
Unlabeled Uses
Treatment of caffeine toxicity; attenuation of CV responses to electroconvulsive therapy or induction of anesthesia; adjunct therapy for acute MI and unstable angina; treatment of thyroid storm.
Contraindications
Sinus bradycardia; second- or third-degree heart block; CHF unless secondary to tachyarrhythmia treatable with beta-blockers; overt cardiac failure; cardiogenic shock.
Dosage and Administration
AdultsUsual: IV 500 mcg/kg/min for 1 min; then infusion of 50 to 200 mcg/kg/min, which has been titrated to desired end point (eg, heart rate, BP) in 50 mcg/kg/min increments.
General Advice
- 10 mg/mL vial does not need further dilution.
- Do not administer through butterfly needles.
- For IV administration, use 250 mg/mL solution diluted in dextrose 5% injection and sodium chloride 0.9% or 0.45% injection, lactated Ringer's injection, and potassium chloride (40 mEq/L) in dextrose 5% injection or sodium chloride 0.9% or 0.45% injection. To prepare solution remove 20 mL from 500 mL bottle of suitable infusion fluid and add 2 amps of 250 mg/mL solution of esmolol. Final concentration is 10 mg/mL.
Storage/Stability
Store diluted solution at room temperature or under refrigeration. Discard after 24 h.
Drug Interactions
ClonidineMay enhance or reverse antihypertensive effect; potentially life-threatening increases in BP may occur, especially on withdrawal.
NSAIDsSome agents may impair antihypertensive effect.
PrazosinPotential for and degree of orthostatic hypotension may be increased.
VerapamilEffects of both drugs may be increased.
Incompatibility
Sodium bicarbonate 5% injection.
Laboratory Test Interactions
Antinuclear antibodies may develop; usually reversible on discontinuation. May interfere with glucose or insulin tolerance test results. May cause changes in serum lipid levels.
Adverse Reactions
Cardiovascular
Hypotension; bradycardia; CHF; cold extremities; pallor; second or third-degree heart block.
CNS
Insomnia; fatigue; dizziness; depression; lethargy; drowsiness; forgetfulness.
Dermatologic
Rash; hives; fever; alopecia.
EENT
Dry eyes; blurred vision; tinnitus; slurred speech; sore throat.
GI
Nausea; vomiting, diarrhea; dry mouth.
Genitourinary
Impotence; painful, difficult, or frequent urination.
Hematologic
Agranulocytosis; thrombocytopenia purpura.
Respiratory
Bronchospasm; shortness of breath; wheezing.
Miscellaneous
Weight changes; facial swelling; muscle weakness; inflammation at infusion site.
Precautions
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Renal Function
Reduced daily dose advised.
Hepatic Function
Reduced daily dose advised.
Anaphylaxis
Deaths have occurred; aggressive therapy may be required.
CHF
Administer drug in patients with CHF controlled by digitalis and diuretics. Notify health care provider at first sign or symptom of CHF or other unexplained respiratory symptoms.
Diabetes mellitus
May mask signs and symptoms of hypoglycemia (eg, tachycardia, BP changes). May potentiate insulin-induced hypoglycemia.
Nonallergic bronchospasm (eg, chronic bronchitis, emphysema)
Use caution in patients with bronchospastic diseases.
Peripheral vascular disease
May precipitate or aggravate symptoms of arterial insufficiency.
Thyrotoxicosis
May mask clinical signs (eg, tachycardia) of developing or continuing hyperthyroidism. Abrupt withdrawal may exacerbate symptoms of hyperthyroidism, including thyroid storm.
Overdosage
Symptoms
Hypotension, bradycardia, intraventricular conduction disturbances, shock.
Patient Information
- Caution patient to notify health care provider of any urticaria, shortness of breath, vertigo, syncope, or inability to void.
- Advise diabetic patient to notify health care provider of hypoglycemic reaction symptoms.
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Atrial Fibrillation, Supraventricular Tachycardia, Atrial Flutter, Intra- or Post-op SVT or Hypertension
