Brand Name
Brevibloc
Generic Name
Esmolol
View Brand Information FDA approval date: December 31, 1986
Classification: beta-Adrenergic Blocker
Form: Injection
What is Brevibloc (Esmolol)?
Esmolol Hydrochloride is a beta-adrenergic blocker indicated for the short-term treatment of: Control of ventricular rate in supraventricular tachycardia including atrial fibrillation and atrial flutter and control of heart rate in noncompensatory sinus tachycardia.
Approved To Treat
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Brand Information
BREVIBLOC (esmolol hydrochloride)
1DOSAGE FORMS AND STRENGTHS
All BREVIBLOC injection dosage forms are iso-osmotic solutions of esmolol hydrochloride in sodium chloride.
2CONTRAINDICATIONS
BREVIBLOC (Esmolol Hydrochloride) injection is contraindicated in patients with:
- Severe sinus bradycardia: May precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest
- Heart block greater than first degree: Second- or third-degree atrioventricular block may precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest
- Sick sinus syndrome: May precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest
- Decompensated heart failure: May worsen heart failure.
- Cardiogenic shock: May precipitate further cardiovascular collapse and cause cardiac arrest.
- IV administration of cardiodepressant calcium-channel antagonists (e.g., verapamil) and BREVIBLOC injection in close proximity (i.e., while cardiac effects from the other are still present); fatal cardiac arrests have occurred in patients receiving BREVIBLOC injection and intravenous verapamil.
- Pulmonary hypertension: May precipitate cardiorespiratory compromise.
- Hypersensitivity reactions, including anaphylaxis, to esmolol or any of the inactive ingredients of the product (cross-sensitivity between beta blockers is possible).
3DRUG INTERACTIONS
Concomitant use of BREVIBLOC injection with other drugs that can lower blood pressure, reduce myocardial contractility, or interfere with sinus node function or electrical impulse propagation in the myocardium can exaggerate BREVIBLOC injection’s effects on blood pressure, contractility, and impulse propagation. Severe interactions with such drugs can result in, for example, severe hypotension, cardiac failure, severe bradycardia, sinus pause, sinoatrial block, atrioventricular block, and/or cardiac arrest. In addition, with some drugs, beta blockade may precipitate increased withdrawal effects. (See clonidine, guanfacine, and moxonidine below.) BREVIBLOC injection should therefore be used only after careful individual assessment of the risks and expected benefits in patients receiving drugs that can cause these types of pharmacodynamic interactions, including but not limited to:
- Digitalis glycosides: Concomitant administration of digoxin and BREVIBLOC injection leads to an approximate 10% to 20% increase of digoxin blood levels at some time points. Digoxin does not affect BREVIBLOC injection pharmacokinetics. Both digoxin and beta blockers slow atrioventricular conduction and decrease heart rate. Concomitant use increases the risk of bradycardia.
- Anticholinesterases: BREVIBLOC injection prolonged the duration of succinylcholine-induced neuromuscular blockade and moderately prolonged clinical duration and recovery index of mivacurium.
- Antihypertensive agents clonidine, guanfacine, or moxonidine: Beta blockers also increase the risk of clonidine-, guanfacine-, or moxonidine-withdrawal rebound hypertension. If, during concomitant use of a beta blocker, antihypertensive therapy needs to be interrupted or discontinued, discontinue the beta blocker first, and the discontinuation should be gradual.
- Calcium channel antagonists: In patients with depressed myocardial function, use of BREVIBLOC injection with cardiodepressant calcium channel antagonists (e.g., verapamil) can lead to fatal cardiac arrests.
- Sympathomimetic drugs: Sympathomimetic drugs having beta-adrenergic agonist activity will counteract effects of BREVIBLOC injection.
- Vasoconstrictive and positive inotropic agents: Because of the risk of reducing cardiac contractility in presence of high systemic vascular resistance, do not use BREVIBLOC injection to control tachycardia in patients receiving drugs that are vasoconstrictive and have positive inotropic effects, such as epinephrine, norepinephrine, and dopamine.
4DESCRIPTION
BREVIBLOC (Esmolol Hydrochloride) injection is a beta adrenergic receptor blocker with a very short duration of action (elimination half-life is approximately 9 minutes). Esmolol hydrochloride is:
- (±)-Methyl p-[2-hydroxy-3-(isopropylamino) propoxy] hydrocinnamate hydrochloride and has the following structure:
- Esmolol hydrochloride has the empirical formula C
- Esmolol hydrochloride is a white to off-white crystalline powder. It is a relatively hydrophilic compound which is very soluble in water and freely soluble in alcohol. Its partition coefficient (octanol/water) at pH 7.0 is 0.42 compared to 17.0 for propranolol.
4.1BREVIBLOC Injection Dosage Forms
All BREVIBLOC injection presentations are clear, colorless to light yellow, sterile, nonpyrogenic, iso‑osmotic solutions of esmolol hydrochloride in sodium chloride. The formulations for BREVIBLOC PREMIXED Injection, BREVIBLOC PREMIXED Double Strength Injection, and BREVIBLOC Injection are described in the table below:
The calculated osmolarity of BREVIBLOC PREMIXED Injection and BREVIBLOC PREMIXED Double Strength Injection is 312 mOsmol/L. The 250 mL and 100 mL bags are non-latex, non-PVC INTRAVIA bags with dual PVC ports. The INTRAVIA bags are manufactured from a specially designed multilayer plastic (PL 2408). Solutions in contact with the plastic container leach out certain chemical compounds from the plastic in very small amounts; however, biological testing was supportive of the safety of the plastic container materials.
5NONCLINICAL TOXICOLOGY
Because of its short-term usage, no carcinogenicity, mutagenicity, or reproductive performance studies have been conducted with esmolol.
6CLINICAL STUDIES
Supraventricular Tachycardia
In two multicenter, randomized, double-blind, controlled comparisons of BREVIBLOC injection with placebo and propranolol, maintenance doses of 50 to 300 mcg/kg/min of BREVIBLOC injection were found to be more effective than placebo and about as effective as propranolol, 3‑6 mg given by bolus injections, in the treatment of supraventricular tachycardia, principally atrial fibrillation and atrial flutter. The majority of these patients developed their arrhythmias postoperatively. About 60-70% of the patients treated with BREVIBLOC injection developed either a 20% reduction in heart rate, a decrease in heart rate to less than 100 bpm, or, rarely, conversion to normal sinus rhythm and about 95% of these patients did so at a dosage of 200 mcg/kg/min or less. The average effective dosage of BREVIBLOC injection was approximately 100 mcg/kg/min in the two studies. Other multicenter baseline-controlled studies gave similar results. In the comparison with propranolol, about 50% of patients in both the BREVIBLOC injection and propranolol groups were on concomitant digoxin. Response rates were slightly higher with both beta blockers in the digoxin-treated patients.
In all studies significant decreases of blood pressure occurred in 20-50% of patients, identified either as adverse reaction reports by investigators, or by observation of systolic pressure less than 90 mmHg or diastolic pressure less than 50 mmHg. The hypotension was symptomatic (mainly hyperhidrosis or dizziness) in about 12% of patients, and therapy was discontinued in about 11% of patients, about half of whom were symptomatic. Hypotension was more common with BREVIBLOC injection (53%) than with propranolol (17%). The hypotension was rapidly reversible with decreased infusion rate or after discontinuation of therapy with BREVIBLOC injection. For both BREVIBLOC injection and propranolol, hypotension was reported less frequently in patients receiving concomitant digoxin.
7PATIENT COUNSELING INFORMATION
Physicians should inform patients of the risks associated with BREVIBLOC injection:
- The most common adverse reactions are symptomatic hypotension (hyperhidrosis, dizziness) and asymptomatic hypotension.
- Inform patients or caregivers that there is a risk of hypoglycemia when esmolol is given to patients who are fasting or who are vomiting. Monitor for symptoms of hypoglycemia.
Manufactured for
Baxter Healthcare Corporation
Deerfield, IL 60015 USA
Baxter, Brevibloc, Brevibloc Premixed and Intravia are trademarks of Baxter International Inc.
Novaplus is a registered trademark of Vizient, Inc.
0719006353
8PACKAGE/LABEL PRINCIPAL DISPLAY PANEL
LOT EXP
NDC 10019-668-10
100 mL Single-Dose Container
Rx Only
For Intravenous Use Only
EACH ML CONTAINS 20 mg ESMOLOL
RECOMMENDED DOSAGE: SEE PRESCRIBING
INFORMATION
INFORMATION
CAUTIONS: CHECK FOR LEAKS BY SQUEEZING
CONTAINER FIRMLY IF LEAKS ARE FOUND DISCARD AS
STERILITY MAY BE IMPAIRED USE ONLY IF SOLUTION IS
CLEAR COLORLESS TO LIGHT YELLOW
CONTAINER FIRMLY IF LEAKS ARE FOUND DISCARD AS
STERILITY MAY BE IMPAIRED USE ONLY IF SOLUTION IS
CLEAR COLORLESS TO LIGHT YELLOW
DO NOT INTRODUCE ADDITIVES
MUST NOT BE USED IN SERIES CONNECTIONS
STORE AT 25°C (77°F) EXCURSIONS PERMITTED TO
NovaPlus Logo0725006216 2J1416
MANUFACTURED BY
LOT EXP
NDC 10019-672-10
250 mL
EACH mL CONTAINS 10 mg ESMOLOL
USUAL DOSAGE SEE PACKAGE INSERT
CAUTIONS CHECK FOR LE AKS BY SQUEEZING CONTAINER FIRMLY
IF LEAKS ARE FOUND DISCARD AS STERILITY MAY BE IMPAIRED USE
ONLY IF SOLUTION IS CLEAR COLORLESS TO LIGHT YELLOW DISCARD
UNUSED PORTION
DO NOT INTRODUCE ADDITIVESMUST NOT BE USED IN SERIES CONNECTIONS
STORE AT 25°C (77°F) EXCURSIONS PERMITTED TO 15°-30°C
CAUTIONS CHECK FOR LE AKS BY SQUEEZING CONTAINER FIRMLY
IF LEAKS ARE FOUND DISCARD AS STERILITY MAY BE IMPAIRED USE
ONLY IF SOLUTION IS CLEAR COLORLESS TO LIGHT YELLOW DISCARD
UNUSED PORTION
DO NOT INTRODUCE ADDITIVESMUST NOT BE USED IN SERIES CONNECTIONS
STORE AT 25°C (77°F) EXCURSIONS PERMITTED TO 15°-30°C
MANUFACTURED BY
INTRAVIA CONTAINER