ESMOLOL HYDROCHLORIDE
| ESMOLOL HYDROCHLORIDE (ess'moe-lol) Brevibloc Classifications: beta-adrenergic antagonist; antiarrhythmic; Therapeutic:antiarrhythmic Prototype: Propranolol Pregnancy Category: C |
Availability
10 mg/mL, 250 mg/mL injection
Action
Ultrashort-acting beta1-adrenergic blocking agent with cardioselective properties. Hemodynamic effects are mild, with potency as a beta blocker about 1/100 that of propranolol. Inhibits the agonist effect of catecholamines by competitive binding at beta-adrenergic receptors. Antiarrhythmic properties occur at the AV node.
Therapeutic Effect
Effective as an antiarrhythmic agent on the AV-nodal conduction system. Blocks sympathetically mediated increases in cardiac rate and BP since it binds predominantly to beta1-receptors in cardiac tissue.
Uses
Supraventricular tachyarrhythmias (SVT) in perioperative and postoperative periods or in other critical situations. Also short-term treatment of noncompensating sinus tachycardia and in the control of heart rate for patients with MI.
Unlabeled Uses
Moderate postoperative hypertension; treatment of intense transient adrenergic response to surgical stress in cardiac as well as noncardiac surgery.
Contraindications
Hypersensitivity to esmolol; cardiac failure, heart block greater than first degree, sinus bradycardia, cardiogenic shock; decompensated CHF; pulmonary disease such as bronchial asthma, acute bronchospasm, COPD, pulmonary edema; pregnancy (category C). Safety in children is not established.
Cautious Use
History of allergy; CHF; diabetes mellitus; kidney function impairment; lactation.
Route & Dosage
| Supraventricular Tachyarrhythmias Adult: IV 500 mcg/kg loading dose followed by 50 mcg/kg/min, may increase dose q5–10min prn if response inadequate, may repeat loading dose followed by 100 mcg/kg/min 4 x min; may continue repeating loading dose and increasing 4-min dose by 50 mcg/kg/min prn (max: 200 mcg/kg/min) Intraoperative/Postoperative Tachycardia Adult: IV 80 mg bolus followed by 150 mcg/kg/min; increase if needed (max: 300 mcg/kg/min) |
Administration
- Note: Do not use the 2500 mg ampule for direct IV injection.
| Intravenous PREPARE: Direct: Use the 10 mg/mL vial undiluted for the loading dose. IV Infusion: Use the concentrate for injection (250 mg/mL). Prepare maintenance infusion by adding 2.5 g to 250 mL or 5 g to 500 mL of IV solution to yield 10 mg/mL. Compatible diluents include D5W, D5/RL, D5/NS, D5/.45NS, RL. ADMINISTER: Direct: Give loading dose over 1 min. IV Infusion: Give maintenance infusion over 4 min. If adequate response is noted, continue maintenance infusion with periodic adjustments as needed. If an adequate response has not occurred, repeat loading dose and follow with an increased maintenance infusion of 100 mcg/kg/min. May continue titration cycle with same loading dose while increasing maintenance infusion by 50 mcg/kg/min until desired end point is near. Then omit loading dose and titrate maintenance dose up or down by 25 to 50 mcg/kg/min until desired heart rate is reached. INCOMPATIBILITIES Solution/Additive: Diazepam, procainamide, thiopental. Y-site: Amphotericin B cholesteryl, furosemide, warfarin. |
- Diluted infusion solution is stable for at least 24 h at room temperature.
Adverse Effects (≥1%)
CNS: Headache, dizziness, somnolence, confusion, agitation. CV: Hypotension (dose related), cold hands and feet, bradyarrhythmias, flushing, myocardial depression. GI: Nausea, vomiting. Respiratory: Dyspnea, chest pain, rhonchi, bronchospasm. Skin: Infusion site inflammation (redness, swelling, induration).Interactions
Drug: May increase digoxin IV levels 10–20%; morphine IV may increase esmolol levels by 45%; succinylcholine may prolong neuromuscular blockade.Pharmacokinetics
Onset: <5 min. Peak: 10–20 min. Duration: 10–30 min. Metabolism: Hydrolyzed by RBC esterases. Elimination: In urine. Half-Life: 9 min.Nursing Implications
Assessment & Drug Effects
- Monitor BP, pulse, ECG, during esmolol infusion. Hypotension may have its onset during the initial titration phase; thereafter the risk increases with increasing doses. Usually the hypotension experienced during esmolol infusion is resolved within 30 min after infusion is reduced or discontinued.
- Change injection site if local reaction occurs. IV site reactions (burning, erythema) or diaphoresis may develop during infusion. Both reactions are temporary. Blood chemistry abnormalities have not been reported.
- Overdose symptoms: Discontinue administration if the following symptoms occur: bradycardia, severe dizziness or drowsiness, dyspnea, bluish-colored fingernails or palms of hands, seizures.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug