SPL Set ID: 595cc3d5-1306-4828-aefa-5595219ffd62

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 16 H 26 NO 4 Cl and a molecular weight of 331.8. It has one asymmetric center and exists as an enantiomeric pair. • 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. 11.1 BREVIBLOC 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: Table 4 BREVIBLOC Injection Formulations BREVIBLOC PREMIXED Injection (Esmolol Hydrochloride) BREVIBLOC PREMIXED Double Strength Injection (Esmolol Hydrochloride) BREVIBLOC Injection (Esmolol Hydrochloride) Esmolol Hydrochloride, USP 10 mg/mL 20 mg/mL 10 mg/mL Sodium Chloride, USP 5.9 mg/mL 4.1 mg/mL 5.9 mg/mL Water for Injection, USP Q.S. to volume of 250 mL Q.S. to volume of 100 mL Q.S. to volume of 10 mL Sodium Acetate Trihydrate, USP 2.8 mg/mL 2.8 mg/mL 2.8 mg/mL Glacial Acetic Acid, USP 0.546 mg/mL 0.546 mg/mL 0.546 mg/mL Sodium Hydroxide Q.S. to adjust pH to 4.5-5.5 Hydrochloric Acid Q.S. to adjust pH to 4.5-5.5 Q.S. = Quantity sufficient 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. BREVIBLOC Structural Formula