BREVIBLOC IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BREVIBLOC IN PLASTIC CONTAINER (BREVIBLOC IN PLASTIC CONTAINER).
Esmolol is a cardioselective beta-1 adrenergic receptor antagonist with minimal intrinsic sympathomimetic activity and membrane-stabilizing properties. At therapeutic doses, it blocks beta-1 receptors in the myocardium, decreasing heart rate, myocardial contractility, and AV conduction velocity, leading to reduced cardiac output and myocardial oxygen demand.
| Metabolism | Emesis: rapamycin. Metabolized rapidly by esterases in red blood cells and plasma to an inactive acid metabolite and methanol. Not metabolized by cytochrome P450 enzymes. |
| Excretion | Elimination primarily via red blood cell esterases; renal excretion of unchanged drug is less than 1% of dose. Metabolite ASL-8123 is inactive and renally excreted. |
| Half-life | Terminal elimination half-life is approximately 9 minutes (range 4–15 minutes) for the parent drug, leading to rapid offset of effect. The half-life of the metabolite ASL-8123 is about 3.7 hours. |
| Protein binding | Approximately 65% bound to plasma proteins (primarily albumin); the metabolite ASL-8123 is about 55% protein bound. |
| Volume of Distribution | Volume of distribution at steady state is 4.5 L/kg (range 2–6 L/kg), indicating extensive distribution into tissues, including red blood cells, where hydrolysis occurs. |
| Bioavailability | Not applicable; esmolol is administered intravenously only. Oral bioavailability is negligible due to extensive first-pass metabolism. |
| Onset of Action | Intravenous bolus: Onset of beta-blockade occurs within 2–5 minutes. Continuous infusion: Steady-state effect achieved within 5–10 minutes (30 minutes if no loading dose). |
| Duration of Action | Duration of action is short-lived; following bolus, clinical effects dissipate within 10–30 minutes after discontinuation of infusion due to rapid hydrolysis. Heart rate and blood pressure return to baseline within 15–30 minutes. |
Initial loading dose: 500 mcg/kg IV over 1 minute, followed by continuous IV infusion of 50 mcg/kg/min for 4 minutes; if inadequate response, repeat loading dose and increase infusion by 50 mcg/kg/min increments up to 200 mcg/kg/min. Maintenance: 25-200 mcg/kg/min continuous IV infusion.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment for GFR > 30 mL/min. For GFR 10-30 mL/min: reduce maintenance infusion by 50%. For GFR < 10 mL/min (dialysis): reduce maintenance infusion by 75%. Monitor closely. |
| Liver impairment | No specific Child-Pugh based adjustments. Esmolol is hepatically metabolized via ester hydrolysis; in severe hepatic impairment (Child-Pugh class C), consider dose reduction due to potential accumulation and prolonged effect. Use with caution. |
| Pediatric use | Children: Loading dose of 100-500 mcg/kg IV over 1 minute, followed by continuous infusion of 25-200 mcg/kg/min. Maximum infusion rate 1000 mcg/kg/min. Dosage adjusted to heart rate and blood pressure response. |
| Geriatric use | Elderly patients may have reduced renal function; start at lower end of dosing range (e.g., 25 mcg/kg/min). Consider reduced loading dose (250 mcg/kg) due to increased sensitivity. Monitor for bradycardia and hypotension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BREVIBLOC IN PLASTIC CONTAINER (BREVIBLOC IN PLASTIC CONTAINER).
| Breastfeeding | It is not known whether esmolol is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Brevibloc is administered to a nursing woman. No M/P ratio is available. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal studies, esmolol hydrochloride has been shown to produce increased post-implantation loss and decreased fetal body weights at maternally toxic doses. Use during pregnancy only if potential benefit justifies potential risk to fetus. Beta-blockers may cause fetal bradycardia, hypoglycemia, and respiratory depression, especially when administered during the second and third trimesters. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Sinus bradycardia","Heart block greater than first degree (unless a pacemaker is present)","Cardiogenic shock","Decompensated heart failure","Hypotension (systolic blood pressure <90 mmHg)","Severe pulmonary hypertension","Known hypersensitivity to esmolol or any component","Intravenous administration of calcium channel blockers (e.g., verapamil) within 48 hours","Uncorrected hypovolemia","Severe asthma (relative contraindication)"]
| Precautions | ["Hypotension: may cause significant hypotension, especially at high doses or in volume-depleted patients; dose reduction or temporary discontinuation may be necessary.","Bradycardia: may lead to severe bradycardia, including sinus arrest; monitor heart rate and decrease dose if heart rate <50-55 bpm.","Heart failure: may exacerbate congestive heart failure; use with caution in patients with compensated heart failure.","Bronchospasm: may cause bronchospasm in patients with asthma or COPD due to beta-1 selectivity loss at high doses.","Diabetes/hypoglycemia: beta-blockers may mask signs of hypoglycemia (e.g., tachycardia).","Hyperthyroidism: abrupt withdrawal may exacerbate thyroid storm.","Peripheral vascular disease: may worsen symptoms due to unopposed alpha-mediated vasoconstriction.","Prinzmetal angina: may increase frequency and duration of angina attacks.","Renal impairment: risk of accumulation of the acid metabolite; use with caution in severe renal impairment.","Local reactions: extravasation may cause skin necrosis; use intravenous line carefully."] |
Loading safety data…
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and ECG continuously. Monitor fetal heart rate and uterine activity via electronic fetal monitoring. Assess for signs of maternal hypotension, bradycardia, or heart failure. Monitor neonatal heart rate and blood glucose after delivery if administered near term. |
| Fertility Effects | Animal reproduction studies have not been conducted with esmolol. It is not known whether esmolol can affect reproduction capacity. |
| Food/Dietary | No clinically significant food interactions. Maintain normal dietary habits unless instructed otherwise. |
| Clinical Pearls | Brevibloc (esmolol) is an ultra-short-acting cardioselective beta-blocker with rapid onset (2-10 min) and offset (half-life ~9 min). It is administered via continuous IV infusion and requires titration based on heart rate and blood pressure. Use with caution in bronchospastic disease; cardioselectivity is dose-dependent. Monitor for hypotension, bradycardia, and signs of heart failure. For intraoperative tachycardia/hypertension, a loading dose is often followed by maintenance infusion. |
| Patient Advice | This medication is given intravenously and will be closely monitored by healthcare professionals. · Report dizziness, fainting, slow heartbeat, or difficulty breathing immediately. · Avoid sudden discontinuation; the medication is short-acting and will wear off quickly after stopping. · Inform your doctor if you have asthma, COPD, diabetes, or thyroid disease. · You may experience dizziness upon standing; avoid sudden position changes. |