Esmolol Injection

Table 2: Esmolol Hydrochloride Injection Presentation

Product Name	Esmolol Hydrochloride Injection
Total Dose	100 mg/10 mL
Esmolol Hydrochloride Concentration	10 mg/mL
Packaging	10 mL Vial

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 molecular formula C16H26NO4Cl and a molecular weight of 331.8. It has one asymmetric center and exists as an enantiomeric pair. • Esmolol hydrochloride, USP 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.

Esmolol Hydrochloride Injection Dosage Forms

Esmolol hydrochloride injection is a clear, colorless to light yellow, sterile, nonpyrogenic solution of esmolol hydrochloride. The formulation is described in the table below:

Table 4: Esmolol Hydrochloride Injection Formulation

Q.S. = Quantity sufficient
	Esmolol Hydrochloride Injection
Esmolol Hydrochloride, USP	10 mg/mL
Water for Injection, USP	Q.S. to volume of 10 mL
Sodium Acetate Anhydrous, USP	1.688 mg/mL (equivalent to 2.8 mg/mL Sodium Acetate Trihydrate)
Glacial Acetic Acid, USP	0.546 mg/mL
Sodium Hydroxide	Q.S. to adjust pH to 4.5 to 5.5
Hydrochloric Acid	Q.S. to adjust pH to 4.5 to 5.5

Supraventricular Tachycardia: In two multicenter, randomized, double-blind, controlled comparisons of esmolol hydrochloride with placebo and propranolol, maintenance doses of 50 to 300 mcg/kg/min of esmolol hydrochloride were found to be more effective than placebo and about as effective as propranolol, 3 mg to 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% to 70% of the patients treated with esmolol hydrochloride 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 esmolol hydrochloride 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 esmolol hydrochloride 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% to 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 esmolol hydrochloride (53%) than with propranolol (17%). The hypotension was rapidly reversible with decreased infusion rate or after discontinuation of therapy with esmolol hydrochloride. For both esmolol hydrochloride and propranolol, hypotension was reported less frequently in patients receiving concomitant digoxin.

NDC 67457-182-10

Esmolol
Hydrochloride
Injection
100 mg/10 mL
(10 mg/mL)

For Intravenous Use

Rx only     10 x 10 mL Single-Dose Vials  

Contains no preservatives.
Discard unused portion.

Each mL contains: 10 mg Esmolol Hydrochloride, USP and Water for Injection. Buffered with 1.688 mg Sodium
Acetate Anhydrous (equivalent to 2.8 mg Sodium Acetate Trihydrate) and 0.546 mg Glacial Acetic Acid.
Sodium Hydroxide and/or Hydrochloric Acid added for pH adjustment. pH range is 4.5 to 5.5.

Usual Dosage: See accompanying prescribing information.

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]

Protect from freezing.

Avoid excessive heat.

Avoid contact with alkalies. Do not use if discolored or if a precipitate is present.

Manufactured for:
Mylan Institutional LLC
Rockford, IL 61103 U.S.A.

Manufactured by:
Mylan Institutional
Galway, Ireland

MI:182:10C:R3

Mylan.com

ESMOLOL HYDROCHLORIDE  esmolol hydrochloride injection, solution

Product Information Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:67457-182 Route of Administration INTRAVENOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength ESMOLOL HYDROCHLORIDE (ESMOLOL) ESMOLOL HYDROCHLORIDE 10 mg  in 1 mL

Inactive Ingredients Ingredient Name Strength SODIUM ACETATE ANHYDROUS   ACETIC ACID   SODIUM HYDROXIDE   HYDROCHLORIC ACID   WATER

Packaging # Item Code Package Description 1 NDC:67457-182-10 10 VIAL in 1 CARTON 1 NDC:67457-182-00 10 mL in 1 VIAL

Marketing Information Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date ANDA ANDA076474 05/29/2007

Labeler - Mylan Institutional LLC (790384502)

Revised: 04/2017   Mylan Institutional LLC