====== 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. ---- ===== 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. ---- ===== 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. ---- ===== 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 ---- ===== 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. ---- ===== 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. ---- ===== Adverse Effects ===== Common: * Hypotension * Bradycardia Serious: * AV block * Acute heart failure exacerbation * Cardiogenic shock Rapid offset reduces prolonged toxicity risk. ---- ===== Drug Interactions ===== Additive AV nodal suppression: * [[cardio:ccb:non_dhp|Non-DHP Calcium Channel Blockers]] (verapamil, diltiazem) * Digoxin Other antihypertensives: * Increased hypotension risk ---- ===== Monitoring ===== * Continuous cardiac monitoring * Blood pressure * Heart rate Used in monitored settings (ICU, OR, ED). ---- ===== 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. ---- ===== 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 ---- ===== Related ===== * [[cardio:beta_blockers:start|Beta-Blockers]] * [[cardio:arrhythmias:start|Arrhythmias]] * [[cardio:beta_blockers:metoprolol|Metoprolol]] * [[cardio:beta_blockers:propranolol|Propranolol]]