ESMOLOL HYDROCHLORIDE DOUBLE STRENGTH 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 no intrinsic sympathomimetic activity or membrane stabilizing activity. Reduces heart rate, myocardial contractility, and blood pressure by blocking catecholamine effects at beta-1 receptors predominantly in cardiac tissue.
| Metabolism | Rapid hydrolysis by esterases in erythrocyte cytosol to inactive metabolite, 3-[4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl]propionic acid (ASL-8123) and methanol; minimal hepatic metabolism (CYP450). |
| Excretion | Rapid metabolism by red blood cell esterases; metabolites are inactive. Less than 2% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life is approximately 9 minutes. Clinical context: ultra-short acting beta-blocker, steady state achieved within 30 minutes. |
| Protein binding | Approximately 55% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is 3.5 L/kg. Clinical meaning: extensive distribution, suggesting high tissue penetration. |
| Bioavailability | Intravenous: 100% bioavailability. Not administered orally. |
| Onset of Action | Intravenous: onset within 60 seconds, peak effect at 5 minutes. |
| Duration of Action | Duration of action is 10-20 minutes after infusion discontinuation. Clinical notes: rapid offset allows precise titration. |
Loading dose: 500 mcg/kg IV over 1 minute, followed by maintenance infusion of 50 mcg/kg/min IV for 4 minutes. Titrate by 50 mcg/kg/min increments every 4 minutes as needed to maximum of 200 mcg/kg/min. For double-strength (20 mg/mL) formulation, adjust infusion rate accordingly.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required based on GFR. However, caution in severe renal impairment (CrCl <30 mL/min) due to potential accumulation of acid metabolite; monitor heart rate and blood pressure closely. |
| Liver impairment | No specific dose adjustment per Child-Pugh class. Use with caution in hepatic impairment due to potential reduced clearance; monitor for excessive bradycardia or hypotension. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: loading dose of 100-500 mcg/kg IV over 1 minute, then infusion starting at 50 mcg/kg/min, titrated up to 200-1000 mcg/kg/min based on response. Monitor closely. |
| Geriatric use | Lower initial doses recommended due to age-related decreased clearance: loading dose 250-500 mcg/kg IV over 1 minute, maintenance infusion start at 25-50 mcg/kg/min; titrate cautiously. Increased sensitivity to beta-blockade effects. |
| 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 excreted into breast milk in low amounts; M/P ratio is not well established. Due to short half-life (9 minutes), exposure is minimal. However, monitor infant for bradycardia and hypotension. Consider alternatives with more safety data. |
| Teratogenic Risk | Esmolol is a class C drug in pregnancy. First trimester: Limited data, but beta-blockers are generally associated with fetal bradycardia, growth restriction, and hypoglycemia. Second and third trimesters: Risk of fetal bradycardia, hypotension, and hypoglycemia; use only if benefit outweighs risk. Near term: May cause neonatal bradycardia, respiratory depression, and hypoglycemia. |
■ FDA Black Box Warning
None
| Common Effects | supraventricular tachycardia |
| Serious Effects |
["Sinus bradycardia","Heart block greater than first degree","Cardiogenic shock","Overt heart failure","Hypersensitivity to esmolol or any component","Severe bronchial asthma or chronic obstructive pulmonary disease with bronchospasm","Pulmonary hypertension","Patients receiving verapamil or diltiazem IV (risk of profound bradycardia, hypotension)"]
| Precautions | ["Hypotension: dose-related, may require dose reduction or discontinuation","Bradycardia: may be severe; monitor heart rate","Heart failure: may worsen; caution in compensated heart failure","Bronchospastic disease: risk of bronchospasm in asthma/COPD; avoid if possible","Diabetes mellitus: may mask hypoglycemic symptoms (tachycardia)","Renal impairment: elimination half-life prolonged; use with caution","Extravasation: causes local necrosis; ensure IV access","Abrupt withdrawal: may exacerbate angina or increase risk of MI in coronary artery disease"] |
Loading safety data…
| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and ECG continuously during infusion. Assess fetal heart rate and uterine activity if used for tachyarrhythmia in pregnancy. Monitor neonatal heart rate, blood pressure, and glucose after delivery. |
| Fertility Effects | No human data on fertility effects. Animal studies have not shown impaired fertility. Beta-blockers may affect sperm motility in men, but clinical significance is unclear. |