ESMOLOL

What it is

Esmolol Hydrochloride Medsurge is supplied as a 100 mg/10 mL vial containing 100 mg esmolol hydrochloride. The injection is a clear, colourless to light yellow, sterile, nonpyrogenic solution of esmolol hydrochloride for intravenous infusion. Esmolol hydrochloride is a beta 1-selective (cardioselective) adrenergic blocking agent with rapid onset and a short duration of action (elimination half-life is approximately 9 minutes).

Approved indications

— Rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. — Non-compensatory sinus tachycardia where, in the physician's judgement, the rapid heart rate requires specific intervention.

Dosing overview

In the treatment of supraventricular tachycardia, responses to esmolol hydrochloride usually occur within the range of 50 to 200 microgram/kg/min (0.05 to 0.2 mg/kg/min), with an average effective dosage of approximately 100 microgram/kg/min (0.1 mg/kg/min) although dosages as low as 25 microgram/kg/min (0.025 mg/kg/min) have been adequate in some patients. To initiate treatment, administer a loading infusion of 500 microgram/kg/min (0.5 mg/kg/min) over one minute followed by a 4 minute maintenance infusion of 50 microgram/kg/min (0.05 mg/kg/min). If an adequate therapeutic effect is not observed, repeat the loading dosage infusion over one minute and increase the maintenance infusion to 100 microgram/kg/min (0.1 mg/kg/min).

Key safety warnings

In clinical trials, 20–50% of patients treated with esmolol hydrochloride have had hypotension, generally defined as systolic pressure less than 90 mmHg and/or diastolic pressure less than 50 mmHg, with about 12% of patients being symptomatic (mainly sweating or dizziness). Decrease of dose or termination of infusion reverses hypotension, usually within 30 minutes. Sympathetic stimulation is necessary in supporting circulatory function in congestive heart failure and beta-blockade carries the potential hazard of further depressing myocardial contractility and precipitating more severe failure, and continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. At the first sign or symptom of impending cardiac failure esmolol hydrochloride should be withdrawn, although withdrawal may be sufficient because of the short elimination half-life of esmolol hydrochloride. Patients with bronchospastic diseases should, in general, not receive beta-blockers; however, because of its relative beta 1-selectivity and titratability, esmolol hydrochloride may be used with caution in patients with bronchospastic diseases, but since beta 1-selectivity is not absolute, esmolol hydrochloride should be carefully titrated to obtain the lowest possible effective dose. Infusion concentrations of 20 mg/mL were associated with more venous irritation, including thrombophlebitis, than concentrations of 10 mg/mL, and concentrations greater than 10 mg/mL or infusion into small veins or through a butterfly catheter should be avoided; extravasation may lead to a serious local reaction and possible skin necrosis.

Contraindications

Esmolol Hydrochloride Medsurge is contraindicated in patients with hypersensitivity to esmolol hydrochloride or any of the excipients. Esmolol hydrochloride is contraindicated in patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock or overt heart failure. Esmolol hydrochloride is also contraindicated in patients with severe bradycardia (less than 50 beats per minute), sick sinus syndrome, severe AV-nodal conductance disorders (without pacemaker), second and third degree AV-block, severe hypotension, non-treated phaeochromocytoma, pulmonary hypertension, acute asthma attack and metabolic acidosis. Esmolol hydrochloride should NOT be administered concomitantly with IV verapamil or within close proximity since fatal cardiac arrest has occurred in patients receiving both drugs.

Regulatory history

Esmolol Hydrochloride Medsurge (ARTG 393119) was first listed on 4 May 2023.