BREVIBLOC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BREVIBLOC (BREVIBLOC).
Selective beta-1 adrenergic receptor antagonist (cardioselective) that reduces heart rate, myocardial contractility, and blood pressure by blocking catecholamine effects on cardiac beta-1 receptors.
| Metabolism | Rapidly metabolized by red blood cell esterases via hydrolysis of ester linkage to acid metabolite (ASL-8123) and methanol; independent of hepatic or renal function. |
| Excretion | Rapid hydrolysis by red blood cell esterases to ASL-8123 (acid metabolite) and methanol; ~1% excreted unchanged in urine; renal elimination of metabolite accounts for >95% of dose; no significant biliary/fecal excretion. |
| Half-life | 9 minutes (terminal elimination half-life in adults); due to rapid esterase metabolism, context: requires continuous infusion for sustained effect; prolonged to 20-30 minutes in hepatic impairment. |
| Protein binding | ~60% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | 2.2 L/kg; indicates extensive distribution into tissues (higher than total body water). |
| Bioavailability | Intravenous only; not administered orally due to extensive first-pass metabolism. |
| Onset of Action | Intravenous bolus: <2 minutes; continuous infusion: 2-5 minutes. |
| Duration of Action | 10-20 minutes after cessation of infusion; offset rapid due to short half-life; may be prolonged in severe hepatic impairment. |
IV loading dose: 500 mcg/kg over 1 minute, followed by continuous infusion starting at 50 mcg/kg/min, titrated by 50 mcg/kg/min every 5 minutes up to 200 mcg/kg/min as needed.
| Dosage form | INJECTABLE |
| Renal impairment | No dosage adjustment required for GFR > 30 mL/min. For GFR ≤ 30 mL/min, reduce infusion rate by 50% and monitor closely. |
| Liver impairment | No specific Child-Pugh based adjustments; however, reduce initial infusion rate to 25 mcg/kg/min in severe hepatic impairment and titrate cautiously. |
| Pediatric use | Weight-based: IV loading dose of 500 mcg/kg over 1 minute; continuous infusion starting at 50 mcg/kg/min, titrated by 25-50 mcg/kg/min every 5-10 minutes; maximum 200 mcg/kg/min. |
| Geriatric use | Lower initial infusion rates starting at 25 mcg/kg/min; titrate cautiously due to increased sensitivity and reduced renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BREVIBLOC (BREVIBLOC).
| Breastfeeding | Present in breast milk in low amounts. M/P ratio unknown. Consider risk of infant bradycardia and hypoglycemia. Use with caution, monitor infant for signs of beta-blockade. |
| Teratogenic Risk | First trimester: Limited data, increased risk of fetal bradycardia and hypotension if used near term. Second and third trimesters: May cause fetal bradycardia, growth restriction, and neonatal hypoglycemia. Avoid use near delivery due to risk of persistent fetal bradycardia. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Sinus bradycardia, greater than first-degree heart block, cardiogenic shock, overt cardiac failure, hypersensitivity to esmolol or any component.
| Precautions | Beta-blocker withdrawal may exacerbate angina or precipitate myocardial infarction; avoid abrupt discontinuation. May cause hypotension, bradycardia, and heart failure exacerbation. Use with caution in patients with bronchospastic disease, diabetes (masks hypoglycemia), thyrotoxicosis, or impaired renal function. Infusion site reactions (extravasation, necrosis). |
| Food/Dietary | No specific food interactions are reported for intravenous esmolol. Maintain normal diet unless directed otherwise by the healthcare provider. Avoid excessive alcohol intake as it may enhance hypotensive effects. |
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| Monitor maternal heart rate, blood pressure, and signs of heart failure. Fetal monitoring: heart rate, growth, and amniotic fluid volume. Assess for neonatal bradycardia and hypoglycemia postpartum. |
| Fertility Effects | No known adverse effects on human fertility. In animal studies, no impairment of fertility observed. |
| Clinical Pearls | Brevibloc (esmolol) is an ultra-short-acting cardioselective beta-1 blocker with rapid onset (2-10 min) and offset (elimination half-life ~9 min). It is ideal for acute rate control in supraventricular tachyarrhythmias (e.g., atrial fibrillation/flutter) and perioperative tachycardia/hypertension. Administer as a loading dose (500 mcg/kg over 1 min) followed by maintenance infusion (50-300 mcg/kg/min). Monitor for hypotension and bradycardia; effects resolve quickly upon discontinuation. In heart failure, use with extreme caution and only if compensated. Contraindicated in sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt heart failure. |
| Patient Advice | This medication is given intravenously to rapidly control your heart rate and blood pressure. · You may experience dizziness, lightheadedness, or low blood pressure; report these symptoms immediately. · Notify your healthcare provider if you have a history of asthma, diabetes, or thyroid problems. · Do not abruptly stop this medication; it is discontinued under medical supervision due to rapid offset of action. · Inform all healthcare providers that you are receiving esmolol. |