From the Guidelines
Esmolol has a duration of effect of 10–30 min when administered intravenously. This is based on the most recent and highest quality study available, which is the 2019 European Heart Journal article on the management of hypertensive emergencies 1. The study provides a comprehensive overview of intravenous drugs for the treatment of hypertensive emergencies, including esmolol, and lists its duration of action as 10–30 min.
Key Characteristics of Esmolol
- Onset of action: 1–2 min
- Duration of action: 10–30 min
- Dose: 0.5–1 mg/kg i.v. bolus; 50–300 mg/kg/min as continuous i.v. infusion
- Contraindications: History of 2nd or 3rd degree AV block (and in the absence of rhythm support), systolic heart failure, asthma, and bradycardia
- Adverse effects: Bradycardia
Clinical Use of Esmolol
Esmolol is a valuable agent in critical care settings due to its rapid onset and short duration of action, allowing for tight control of heart rate and quick reversal of effects if adverse reactions occur 1. It is particularly useful in situations requiring short-term beta blockade, such as perioperative tachyarrhythmias, hypertensive emergencies, or testing a patient's tolerance to beta blockade before initiating longer-acting agents.
Transition to Oral Beta-Blockers
If beta blockade needs to be continued beyond the acute setting, transition to an oral beta-blocker should be planned as the effects of esmolol dissipate rapidly once the infusion is stopped 1. This ensures continuous beta blockade and minimizes the risk of rebound hypertension or other adverse effects.
From the FDA Drug Label
Esmolol hydrochloride is a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes After termination of infusion, substantial recovery from beta blockade is observed in 10 to 20 minutes. At 30 minutes after the discontinuation of esmolol hydrochloride infusion, all of the hemodynamic parameters had returned to pretreatment levels.
The duration of effect of Esmolol (esmolol hydrochloride) intravenous (IV) administration is approximately 9 minutes for its elimination half-life, with substantial recovery from beta blockade in 10 to 20 minutes and full recovery of hemodynamic parameters within 30 minutes after discontinuation of infusion 2.
From the Research
Duration of Effect of Esmolol
The duration of effect of esmolol, an ultra-short-acting intravenous cardioselective beta-antagonist, is characterized by its rapid onset and offset of action. Key aspects of its duration of effect include:
- Onset of activity: occurs within 2 minutes 3
- Achievement of 90% of steady-state beta-blockade: within 5 minutes 3
- Full recovery from beta-blockade: observed 18 to 30 minutes after terminating the infusion 3
- Undetectable esmolol blood concentrations: 20 to 30 minutes postinfusion 3
- Recovery from beta blockade: achieved within ten minutes after discontinuation of infusion 4
- Reversal of hypotension: readily reversed within 10 to 30 minutes of discontinuing the infusion of esmolol 5
Factors Influencing Duration of Effect
The duration of effect of esmolol is influenced by its pharmacokinetic properties, including:
- Elimination half-life: approximately 9 minutes 3, 6, 7, 4, 5
- Total body clearance: approaching 3 times cardiac output and 14 times hepatic blood flow 3
- Metabolism: metabolised by red blood cell cytosol esterases to an acid metabolite and methanol 3
Clinical Implications
The short duration of effect of esmolol makes it a useful agent in clinical settings where rapid control and reversibility of beta-blockade are desired, such as: