BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER (BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER).
Selective beta-1 adrenergic receptor antagonist; reduces heart rate, myocardial contractility, and blood pressure by blocking catecholamine effects at beta-1 receptors.
| Metabolism | Rapidly metabolized by esterases in blood and liver to inactive acid metabolite and methanol. |
| Excretion | Primarily metabolized by red blood cell esterases; <1% excreted unchanged in urine. Elimination is not dependent on renal or hepatic function. |
| Half-life | Terminal elimination half-life is approximately 9 minutes (range 8–10 minutes). Clinically, the half-life is consistent with rapid offset of effect upon discontinuation; steady state is achieved within 30 minutes of continuous infusion. |
| Protein binding | Approximately 87% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | Vd is approximately 3.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Intravenous: 100% (IV administration only; oral not available). |
| Onset of Action | IV bolus: 2–5 minutes. Continuous infusion: 5–10 minutes. Onset is rapid due to absence of significant distribution delay. |
| Duration of Action | After IV bolus, effect diminishes within 10–20 minutes. After continuous infusion, hemodynamic effects resolve within 30 minutes of stopping. Duration is short due to rapid esterase metabolism. |
Intravenous: For stable patients, an initial loading dose of 500 mcg/kg/min over 1 minute followed by a maintenance infusion of 50 mcg/kg/min for 4 minutes; if response is inadequate, increase maintenance infusion to 100 mcg/kg/min and repeat loading dose after 10 minutes. Titrate in 50 mcg/kg/min increments up to 200 mcg/kg/min. For intraoperative and postoperative use, see full prescribing information.
| Dosage form | INJECTABLE |
| Renal impairment | No specific GFR-based dose adjustments are recommended; however, use with caution in renal impairment due to potential accumulation of metabolite (ASL-8123) with prolonged infusion. Monitor heart rate and blood pressure closely. |
| Liver impairment | No specific Child-Pugh based adjustments are provided; esmolol is hepatically metabolized via ester hydrolysis, but hepatic impairment may affect metabolism. Use with caution and titrate to effect. |
| Pediatric use | A loading dose of 500-1000 mcg/kg over 1 minute followed by a maintenance infusion of 50-250 mcg/kg/min, titrated to desired effect. In neonates and infants, use lower initial infusion rates (e.g., 50-100 mcg/kg/min) and titrate carefully due to limited data. |
| Geriatric use | Start at the low end of the dosing range (e.g., 25-50 mcg/kg/min maintenance infusion after loading) and titrate carefully due to increased sensitivity and age-related decline in organ function. Monitor for hypotension and bradycardia. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER (BREVIBLOC DOUBLE STRENGTH IN PLASTIC CONTAINER).
| Breastfeeding | Excreted in breast milk in low concentrations; M/P ratio = 0.25. Use with caution in nursing mothers; monitor infant for bradycardia and hypotension. |
| Teratogenic Risk | Inadequate human data; animal studies show no teratogenic risk at clinically relevant doses. First trimester: unknown risk; second and third trimesters: potential for fetal bradycardia and hypoglycemia due to beta-blockade; avoid use in preeclampsia due to risk of fetal growth restriction. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Severe bradycardia (<50 bpm)","Cardiogenic shock","Decompensated heart failure","Second- or third-degree AV block (without pacemaker)","Sick sinus syndrome","Hypersensitivity to esmolol or any component","Severe hypotension"]
| Precautions | ["Hypotension (most common adverse effect)","Bradycardia and heart block","Bronchospasm in patients with asthma/COPD","Heart failure exacerbation in patients with compensated HF","Abrupt withdrawal may precipitate myocardial ischemia or arrhythmias","May mask signs of hypoglycemia or hyperthyroidism"] |
| Food/Dietary | No significant food interactions; administer intravenously, so dietary restrictions are not applicable. |
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| Fetal Monitoring |
| Continuous fetal heart rate monitoring; maternal heart rate and blood pressure monitoring; assess for signs of maternal hypotension and bradycardia; periodic assessment of fetal growth in long-term use. |
| Fertility Effects | No specific data on human fertility; animal studies showed no adverse effects on fertility at therapeutic doses. |
| Clinical Pearls | Brevibloc Double Strength (esmolol HCl) is a cardioselective beta-blocker with an extremely short half-life (~9 minutes), allowing rapid titration and quick offset. It is contraindicated in patients with severe bradycardia, heart block greater than first degree, cardiogenic shock, or decompensated heart failure. Administer via IV infusion; avoid extravasation as it causes severe tissue necrosis. Monitor heart rate and blood pressure closely; hypotension is common. Use with caution in patients with reactive airway disease due to relative beta-1 selectivity. Have resuscitation equipment available. |
| Patient Advice | This medication is given through a vein to control heart rate and blood pressure during procedures or emergencies. · You may experience dizziness or lightheadedness; report these symptoms immediately. · Do not stop taking this medication abruptly without medical supervision. · Notify your healthcare provider if you have a history of asthma, slow heart rate, or heart failure. · Tell your provider about all medications you are taking, especially other heart medications. |