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All about: Esmolol HCl

Big Image Pronouncation: (ESS-moe-lahl HIGH-droe-KLOR-ide)
Class: Beta-adrenergic blocking agent

Trade Names:
Brevibloc
- Injection 10 mg/mL
- Injection 250 mg/mL

Mechanism of Action

Pharmacology

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

Adults

Usual: 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

Clonidine

May enhance or reverse antihypertensive effect; potentially life-threatening increases in BP may occur, especially on withdrawal.

NSAIDs

Some agents may impair antihypertensive effect.

Prazosin

Potential for and degree of orthostatic hypotension may be increased.

Verapamil

Effects 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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