Esmolol Hydrochloride in Sodium Chloride

ESMOLOL HYDROCHLORIDE IN SODIUM CHLORIDE- esmolol hydrochloride injection
Mylan Institutional LLC

1 INDICATIONS AND USAGE

1.1 Supraventricular Tachycardia or Noncompensatory Sinus Tachycardia

Esmolol hydrochloride in sodium chloride injection is indicated for the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable. Esmolol hydrochloride in sodium chloride injection is also indicated in noncompensatory sinus tachycardia where, in the physician’s judgment, the rapid heart rate requires specific intervention. Esmolol hydrochloride in sodium chloride injection is intended for short- term use.

1.2 Intraoperative and Postoperative Tachycardia and Hypertension

Esmolol hydrochloride in sodium chloride injection is indicated for the short-term treatment of tachycardia and hypertension that occur during induction and tracheal intubation, during surgery, on emergence from anesthesia and in the postoperative period, when in the physician’s judgment such specific intervention is considered indicated.

Use of esmolol hydrochloride in sodium chloride injection to prevent such events is not recommended.

2 DOSAGE AND ADMINISTRATION

2.1 Dosing for the Treatment of Supraventricular Tachycardia or Noncompensatory Sinus Tachycardia

Esmolol hydrochloride in sodium chloride injection is administered by continuous intravenous infusion with or without a loading dose. Additional loading doses and/or titration of the maintenance infusion (step-wise dosing) may be necessary based on desired ventricular response.

Table 1 Step-Wise Dosing

Step	Action
1	Optional loading dose (500 mcg per kg over 1 minute), then 50 mcg per kg per min for 4 min
2	Optional loading dose if necessary, then 100 mcg per kg per min for 4 min
3	Optional loading dose if necessary, then 150 mcg per kg per min for 4 min
4	If necessary increase dose to 200 mcg per kg per min

The effective maintenance dose for continuous and step-wise dosing is 50 to 200 mcg per kg per minute, although doses as low as 25 mcg per kg per minute have been adequate. Dosages greater than 200 mcg per kg per minute provide little added heart-rate lowering effect, and the rate of adverse reactions increases.

Maintenance infusions may be continued for up to 48 hours.

2.2 Intraoperative and Postoperative Tachycardia and Hypertension

In this setting it is not always advisable to slowly titrate to a therapeutic effect. Therefore two dosing options are presented: immediate control and gradual control.

Immediate Control

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Administer 1 mg per kg as a bolus dose over 30 seconds followed by an infusion of 150 mcg per kg per min if necessary.

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Adjust the infusion rate as required to maintain desired heart rate and blood pressure. Refer to Maximum Recommended Doses below.

Gradual Control

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Administer 500 mcg per kg as a bolus dose over 1 minute followed by a maintenance infusion of 50 mcg per kg per min for 4 minutes.

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Depending on the response obtained, continue dosing as outlined for supraventricular tachycardia (refer to Figure 1). Refer to Maximum Recommended Doses below.

Maximum Recommended Doses

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For the treatment of tachycardia, maintenance infusion dosages greater than 200 mcg per kg per min are not recommended; dosages greater than 200 mcg per kg per min provide little additional heart rate-lowering effect, and the rate of adverse reactions increases.

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For the treatment of hypertension, higher maintenance infusion dosages (250 to 300 mcg per kg per min) may be required. The safety of doses above 300 mcg per kg per minute has not been studied.

2.3 Transition from Esmolol Hydrochloride in Sodium Chloride Injection Therapy to Alternative Drugs

After patients achieve adequate control of the heart rate and a stable clinical status, transition to alternative antiarrhythmic drugs may be accomplished.

When transitioning from esmolol hydrochloride in sodium chloride injection to alternative drugs, the physician should carefully consider the labeling instructions of the alternative drug selected and reduce the dosage of esmolol hydrochloride in sodium chloride injection as follows:

1.

Thirty minutes following the first dose of the alternative drug, reduce the esmolol hydrochloride in sodium chloride injection infusion rate by one-half (50%).

2.

After administration of the second dose of the alternative drug, monitor the patient’s response, and, if satisfactory control is maintained for the first hour, discontinue the esmolol hydrochloride in sodium chloride injection infusion.

2.4 Directions for Use

Esmolol hydrochloride in sodium chloride injection is available in a pre-mixed bag. Esmolol hydrochloride in sodium chloride injection is not compatible with Sodium Bicarbonate (5%) solution (limited stability) or furosemide (precipitation).

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Premixed Bag

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The medication port is to be used solely for withdrawing an initial bolus from the bag.

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Use aseptic technique when withdrawing the bolus dose.

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Do not add any additional medications to the bag.

Figure 2: Two-Port IntraVia Bag

3 DOSAGE FORMS AND STRENGTHS

All esmolol hydrochloride in sodium chloride injection dosage forms are iso-osmotic solutions of esmolol hydrochloride in sodium chloride.

Table 1 Esmolol Hydrochloride in Sodium Chloride Injection Presentations

Product Name	Esmolol Hydrochloride in Sodium Chloride Injection [10 mg/mL] [250 mL]	Esmolol Hydrochloride in Sodium Chloride Injection [20 mg/mL] [100 mL]
Total Dose	2500 mg / 250 mL	2000 mg / 100 mL
Esmolol Hydrochloride Concentration	10 mg/mL	20 mg/mL
Packaging	250 mL Bag	100 mL Bag

4 CONTRAINDICATIONS

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Esmolol hydrochloride in sodium chloride injection is contraindicated in patients with:

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Severe sinus bradycardia: May precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest [see Warnings and Precautions (5.2)].

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Heart block greater than first degree: Second- or third-degree atrioventricular block may precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest [see Warnings and Precautions (5.2)].

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Sick sinus syndrome: May precipitate or worsen bradycardia resulting in cardiogenic shock and cardiac arrest [see Warnings and Precautions (5.2)].

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Decompensated heart failure: May worsen heart failure.

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Cardiogenic shock: May precipitate further cardiovascular collapse and cause cardiac arrest.

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IV administration of cardiodepressant calcium-channel antagonists (e.g.,verapamil) and esmolol hydrochloride in sodium chloride injection in close proximity (i.e., while cardiac effects from the other are still present); fatal cardiac arrests have occurred in patients receiving esmolol hydrochloride in sodium chloride injection and intravenous verapamil.

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Pulmonary hypertension: May precipitate cardiorespiratory compromise.

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Hypersensitivity reactions, including anaphylaxis, to esmolol or any of the inactive ingredients of the product (cross-sensitivity between beta blockers is possible).