====== Esmolol (Brevibloc®) ======
^ Esmolol | {{ :cardio:beta_blockers:esmolol_structure.svg?200 |}} |
| Brand Name | Brevibloc® |
| Drug Class | [[cardio:beta_blockers:start|β-Blocker]] (β1-selective) |
| Primary Indication | Acute Rate Control |
| β1 Selectivity | High |
| Intrinsic Sympathomimetic Activity | No |
| Half-Life | ~9 minutes |
| Route | IV only |
| Metabolism | Plasma esterases |
| FDA Approval | 1986 |
===== Overview =====
Esmolol is a short-acting, β1-selective adrenergic receptor antagonist used for rapid, titratable heart rate control in acute settings.
Its ultra-short half-life (~9 minutes) allows for precise titration and rapid discontinuation if adverse effects occur.
It is commonly used in ICU and perioperative settings.
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===== Mechanism of Action =====
**Receptor Activity**
* Selective β1-adrenergic receptor antagonist
**Cardiac Effects**
* ↓ Heart rate
* ↓ Myocardial contractility
* ↓ AV nodal conduction
**Net Effect**
* Reduced cardiac output
* Rate control in tachyarrhythmias
Minimal β2 activity at therapeutic doses.
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===== Indications =====
* Acute atrial fibrillation with rapid ventricular response
* Supraventricular tachycardia
* Intraoperative or postoperative tachycardia
* Acute hypertension (short-term control)
* Thyroid storm (adjunct therapy)
Used when rapid onset and rapid offset are desired.
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===== Contraindications =====
Absolute:
* Severe bradycardia
* Second- or third-degree AV block (without pacemaker)
* Cardiogenic shock
* Decompensated heart failure
Relative / Caution:
* Asthma or severe COPD
* Hypotension
* Peripheral vascular disease
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===== Dosing =====
IV bolus:
* 500 mcg/kg over 1 minute
Continuous infusion:
* 50–200 mcg/kg/min
Titrated based on heart rate and blood pressure.
Effects dissipate within 10–20 minutes after discontinuation.
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===== Pharmacokinetics =====
Route:
* Intravenous only
Metabolism:
* Rapid hydrolysis by plasma esterases
Half-life:
* ~9 minutes
Elimination:
* Renal excretion of inactive metabolites
Short half-life allows rapid reversal of effect.
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===== Adverse Effects =====
Common:
* Hypotension
* Bradycardia
Serious:
* AV block
* Acute heart failure exacerbation
* Cardiogenic shock
Rapid offset reduces prolonged toxicity risk.
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===== Drug Interactions =====
Additive AV nodal suppression:
* [[cardio:ccb:non_dhp|Non-DHP Calcium Channel Blockers]] (verapamil, diltiazem)
* Digoxin
Other antihypertensives:
* Increased hypotension risk
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===== Monitoring =====
* Continuous cardiac monitoring
* Blood pressure
* Heart rate
Used in monitored settings (ICU, OR, ED).
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===== Clinical Pearls =====
* Ultra-short acting β1-selective blocker.
* Ideal for unstable or dynamic clinical situations.
* Effects disappear quickly after discontinuation.
* Metabolized by plasma esterases — not dependent on hepatic metabolism.
* Useful in thyroid storm for rapid rate control.
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===== Comparison Within Class =====
Compared to [[cardio:beta_blockers:metoprolol|Metoprolol]]:
* Much shorter half-life
* IV only
* More titratable
Compared to [[cardio:beta_blockers:propranolol|Propranolol]]:
* β1-selective
* Less bronchospasm risk
Compared to [[cardio:beta_blockers:sotalol|Sotalol]]:
* No potassium channel blockade
* Not used for rhythm control
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===== Related =====
* [[cardio:beta_blockers:start|Beta-Blockers]]
* [[cardio:arrhythmias:start|Arrhythmias]]
* [[cardio:beta_blockers:metoprolol|Metoprolol]]
* [[cardio:beta_blockers:propranolol|Propranolol]]