Storage
Store at room temperature
Synonyms
Esmolol HCL; Brevibloc; ASL-8052; DTXSID7049003; V05260LC8D
Molecular Formula
C16H26ClNO4
Smiles
CC(C)NCC(COC1=CC=C(C=C1)CCC(=O)OC)O.Cl
Appearance
White to off-white solid
Boiling Point
430.2°C at 760 mmHg
General Description
Esmolol hydrochloride is an ultra‑short‑acting beta‑1 selective adrenergic antagonist characterized by an ester linkage that is rapidly hydrolyzed by red blood cell esterases. The molecule is a derivative of metoprolol with a methyl‑3‑(4‑hydroxyphenyl)propionate group that facilitates rapid metabolism. Its chemical structure imparts a very short elimination half‑life (approximately 9 minutes), enabling precise titration of beta blockade.
Mechanism of Action
Esmolol competitively blocks beta‑1 adrenergic receptors in the heart, reducing cyclic AMP production and decreasing intracellular calcium influx in cardiomyocytes. This results in negative chronotropic, inotropic, and dromotropic effects, lowering heart rate, myocardial contractility, and blood pressure. At therapeutic doses, it has negligible beta‑2 receptor activity, thus avoiding bronchospasm or peripheral vasoconstriction. Its effect is rapidly reversible upon discontinuation.
Application
The drug is indicated for the acute management of supraventricular tachycardia (including atrial fibrillation and flutter) and for controlling ventricular rate during surgery. It is also used for non‑compensatory sinus tachycardia and as a short‑acting agent for perioperative hypertension. Because of its rapid offset, esmolol is preferred in critically ill patients or those undergoing procedures where immediate reversal of beta blockade might be needed.
In a phase II open‑label trial, 40 septic shock patients with tachycardia were randomized to esmolol infusion or standard care. The primary endpoint — difference in norepinephrine equivalent dose at 6 hours — was not met (0.30 vs. 0.21 mcg/kg/min, P=0.15). Shock‑free days also did not differ. However, esmolol significantly lowered C‑reactive protein levels at 12 and 24 hours and reduced oxygen consumption in a subset of patients. The authors conclude that while esmolol did not improve vasopressor requirements, it was associated with decreased inflammation.
Fig. 1 Hourly esmolol dose during the duration of the study. (Cocchi MN, et al., 2022)
References
- Cocchi MN, et al. Esmolol to Treat the Hemodynamic Effects of Septic Shock: A Randomized Controlled Trial. Shock. 2022;57(4):508-517.
In a phase 3, double‑blind, multicenter trial (176 patients with diabetic foot ulcers), topical esmolol 14% gel plus standard of care (SoC) significantly increased wound closure at 12 weeks (60.3% vs. 41.7% with SoC alone; OR 2.13, P=0.03). Benefits persisted at 24 weeks (77.2% vs. 55.6%; OR 2.71, P=0.01). Median closure time was 85 days in the esmolol group but not estimable in controls. Adverse events were mostly not drug‑related. Topical esmolol is an effective addition to SoC for healing diabetic foot ulcers.
Fig. 2 Enrollment and Flow Chart of the Study Participants. (Rastogi A, et al., 2023)
References
- Rastogi A, et al. Topical Esmolol Hydrochloride as a Novel Treatment Modality for Diabetic Foot Ulcers: A Phase 3 Randomized Clinical Trial. JAMA Netw Open. 2023;6(5):e2311509.
Does Esmolol Hydrochloride require protection from light during long-term storage?
Yes, it is photosensitive. UV light can cause photodegradation and discoloration. Store in light-resistant containers, preferably original packaging.
What is the recommended storage temperature for Esmolol Hydrochloride?
Store at controlled room temperature (15-25°C). Avoid excessive heat above 30°C, which accelerates hydrolysis of the methyl ester group.
Is Esmolol Hydrochloride stable in solution for intravenous administration?
Reconstituted solutions are stable for up to 24 hours at room temperature when protected from light.
How is the impurity esmolol acid (the hydrolyzed metabolite) monitored during stability?
This primary hydrolysis product is quantified using a stability-indicating HPLC method, ensuring it remains below pharmacopoeial limits.