ESMOLOL HYDROCHLORIDE IN PLASTIC CONTAINER
Clinical safety rating: safe
Other drugs that lower heart rate or blood pressure can have additive effects Can cause profound hypotension and bradycardia.
Selective beta-1 adrenergic receptor antagonist with rapid onset and short duration of action; reduces heart rate, myocardial contractility, and blood pressure; no intrinsic sympathomimetic activity or membrane stabilizing activity.
| Metabolism | Rapidly metabolized by ester hydrolysis in erythrocytes; hydrolyzed by esterases in red blood cells to inactive metabolite (ASL-8123) and methanol; not metabolized by liver or kidney. |
| Excretion | Rapid hydrolysis by esterases in blood and tissues to inactive acid metabolite (ASL-8123) and methanol. Less than 2% excreted unchanged in urine. Renal elimination of metabolite accounts for >80% of dose; <5% fecal. |
| Half-life | Terminal elimination half-life is approximately 9 minutes (range 6–12 min) in healthy adults; prolonged to 15–20 min in hepatic impairment. Clinical context: rapid offset allows precise titration. |
| Protein binding | 55% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Volume of distribution: approximately 3.4 L/kg (range 1.4–5.6 L/kg). Clinical meaning: extensive distribution into extravascular tissues, reflecting rapid equilibrium. |
| Bioavailability | Intravenous: 100%. Oral: not administered orally due to extensive first-pass metabolism and short half-life (bioavailability negligible). |
| Onset of Action | Intravenous bolus: onset within 60 seconds (often within 30 sec). Continuous infusion: steady-state effect achieved within 30 minutes without loading dose; faster with loading dose (within 5 min). |
| Duration of Action | Duration of beta-blockade after discontinuation: 10–20 minutes for most hemodynamic effects; complete recovery by 30 minutes. Clinical note: titratability due to ultra-short duration allows rapid adjustment. |
Intravenous loading dose: 500 mcg/kg over 1 minute, followed by maintenance infusion: 50 mcg/kg/min for 4 minutes; if adequate response not achieved, repeat loading dose and increase maintenance infusion by 50 mcg/kg/min increments up to 200 mcg/kg/min.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. Metabolized by red blood cell esterases, not renally cleared. |
| Liver impairment | No dose adjustment required for hepatic impairment. Metabolized by esterases in blood, not hepatic CYP450 system. |
| Pediatric use | Children: Loading dose 100-500 mcg/kg over 1 minute; maintenance infusion 25-100 mcg/kg/min. Titrate by 25-50 mcg/kg/min every 5-10 minutes to effect. Maximum 200 mcg/kg/min. |
| Geriatric use | Elderly patients may have increased sensitivity; start at lower end of dosing range (e.g., 25 mcg/kg/min maintenance) and titrate cautiously. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other drugs that lower heart rate or blood pressure can have additive effects Can cause profound hypotension and bradycardia.
| FDA category | Animal |
| Breastfeeding | Esmolol is not detected in breast milk due to very short half-life and high protein binding; M/P ratio not calculated. Compatible with breastfeeding, but monitor infant for bradycardia and hypotension. |
| Teratogenic Risk | First trimester: Limited human data; animal studies show no major malformations, but beta-blockade may cause fetal bradycardia and hypoxia. Second and third trimesters: Risk of fetal bradycardia, intrauterine growth restriction, neonatal hypoglycemia, and respiratory depression at delivery. Overall, consider risk-benefit. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | supraventricular tachycardia |
| Serious Effects |
["Sinus bradycardia","Heart block greater than first degree","Cardiogenic shock","Decompensated heart failure","Pulmonary hypertension","Known hypersensitivity to esmolol or any component","Severe asthma or COPD with bronchospasm (relative contraindication)"]
| Precautions | ["Bradycardia and hypotension: may cause significant bradycardia, especially in patients with impaired left ventricular function","Heart failure: can precipitate or exacerbate heart failure; use with caution in patients with compensated heart failure","Bronchospasm: can cause bronchospasm in patients with reactive airway disease (asthma/COPD) due to selective beta-1 blockade at low doses, but risk increases with higher doses","Diabetes and hypoglycemia: may mask symptoms of hypoglycemia (tachycardia) and prolong hypoglycemic effect","Peripheral vascular disease: may precipitate or aggravate peripheral vascular insufficiency","Abrupt withdrawal: avoid abrupt discontinuation; taper to reduce risk of myocardial ischemia and angina exacerbation","Anaphylaxis: may blunt response to epinephrine used to treat anaphylaxis","Infusion site reactions: local irritation, phlebitis"] |
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| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and ECG for bradycardia/hypotension. Monitor fetal heart rate and uterine activity if used during labor. Neonatal monitoring for bradycardia, hypoglycemia, and respiratory depression postpartum. |
| Fertility Effects | No specific human studies; animal studies suggest no adverse effects on fertility at clinically relevant doses. Beta-blockers may rarely cause impotence or libido changes, but esmolol's ultra-short action minimizes impact. |