Esmolol
Brevibloc
The beta-blocker to choose when reversibility matters. With a half-life of 9 minutes and the effect gone 20–30 minutes after the infusion ends, it is useful in patients where beta-blockade is desirable but risky — impending heart failure, obstructive lung disease, uncertain haemodynamics.
Avoid in acute heart failure, AV block II–III without a pacemaker, and cardiogenic shock. Bolus doses can cause marked hypotension.
Dosing in adults
| Indication | Regimen | Comment |
|---|---|---|
| Hypertensive crisis | Loading dose 500 μg/kg iv over 1 minute, then infusion 25–50 μg/kg/min | titrated every 4 minutes |
| Aortic dissection | Same loading dose, titrate to heart rate below 60/min and systolic below 120 mmHg | beta-blockade before vasodilators |
| Perioperative tachycardia and hypertension | Infusion 25–300 μg/kg/min | bolus 300 μg/kg may be repeated during infusion |
| Rate control in supraventricular tachycardia | 500 μg/kg bolus, then 50–200 μg/kg/min | maximum dose 300 μg/kg/min |
No dose adjustment of esmolol. The acidic metabolite accumulates in severe renal failure but is clinically inactive.
No dose adjustment — hydrolysed by esterases in erythrocytes.
Loading dose 500 μg/kg iv over 1 minute, then 50–300 μg/kg/min.
Do not give as sole treatment in phaeochromocytoma or cocaine- or amphetamine-induced hypertension — uninhibited alpha-stimulation raises the blood pressure further. Establish alpha-blockade first.
Pharmacokinetics
- ONSET
- 1 minute
- PEAK EFFECT
- 5 minutes
- DURATION
- 20–30 minutes
- t½
- 9 minutes
- Vd
- 3,4 l/kg
- PROTEIN BINDING
- 55 %
- METABOLISM
- Esterases in erythrocytes
- EXCRETION
- Renal (inactive metabolite)