West Ward Pharmaceutical Corporation

West Ward Pharmaceutical Corporation Drugs

• Esmolol Hydrochloride
  

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  Esmolol Hydrochloride

  

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  Dosing Information:

  SUPRAVENTRICULAR TACHYCARDIA

  Dosage needs to be titrated, using ventricular rate as the guide.

  An initial loading dose of 0.5 milligrams/kg (500 micrograms/kg) infused over a minute duration followed by a maintenance infusion of 0.05 milligrams/kg/min (50 micrograms/kg/min) for the next 4 minutes is recommended. This should give a rough guide with respect to the responsiveness of ventricular rate.

  After the 4 minutes of initial maintenance infusion (total treatment duration being 5 minutes), depending upon the desired ventricular response, the maintenance infusion may be continued at 0.05 mg/kg/min or increased step-wise (e.g. 0.1 mg/kg/min, 0.15 mg/kg/min to a maximum of 0.2 mg/kg/min) with each step being maintained for 4 or more minutes.

  If more rapid slowing of ventricular response is imperative, the 0.5 mg/kg loading dose infused over a 1 minute period may be repeated, followed by a maintenance infusion of 0.1 mg/kg/min for 4 minutes. Then, depending upon ventricular rate, another (and final) loading dose of 0.5 mg/kg/min infused over a 1 minute period may be administered followed by a maintenance infusion of 0.15 mg/kg/min. If needed, after 4 minutes of the 0.15 mg/kg/min maintenance infusion, the maintenance infusion may be increased to a maximum of 0.2 mg/kg/min.

  In the absence of loading doses, constant infusion of a single concentration of esmolol reaches pharmacokinetic and pharmacodynamic steady-state in about 30 minutes. Maintenance infusions (with or without loading doses) may be continued for as long as 24 hours.

  The following table summarizes the above and assumes that 3 loading doses (the maximum recommended) are infused over 1 minute and incremental maintenance doses are required after each loading dose. There should be no 4th loading dose, but the maintenance dose may be incremented one more time.

  * As the desired heart rate or endpoint is approached, the loading infusion may be omitted and the maintenance infusion titrated to 300 mcg/kg/min (0.3 mg/kg/min) or downward as appropriate. Maintenance dosages above 200 mcg/kg/min (0.2 mg/kg/min) have not been shown to have significantly increased benefits. The interval between titration steps may be increased. Elapsed Time Loading Dose (over 1 minute) Maintenance Dose (over 4 minutes) (minutes) micrograms/kg/min milligrams/kg/min micrograms/kg/min milligrams/kg/min 0 – 1 500 0.5 1 – 5 50 0.05 5 – 6 500 0.5 6 – 10 100 0.1 10 – 11 500 0.5 11 – 15 150 0.15 15 – 16 · · 16 - 20 *200 *0.2 > 20 Maintenance dose titrated to heart rate or other clinical endpoint.

  In the treatment of supraventricular tachycardia, responses to esmolol hydrochloride usually (over 95%) occur within the range of 50 to 200 micrograms/kg/min (0.05 to 0.2 milligrams/kg/min). The average effective dosage is approximately 100 micrograms/kg/min (0.1 milligrams/kg/min) although dosages as low as 25 micrograms/kg/min (0.025 milligrams/kg/min) have been adequate in some patients. Dosages as high as 300 micrograms/kg/min (0.3 milligrams/kg/min) have been used, but these provide little added effect and increase the rate of adverse effects, so doses greater than 200 micrograms/kg/min are not recommended. Dosage of esmolol hydrochloride in supraventricular tachycardia must be individualized by titration in which each step consists of a loading dosage followed by a maintenance dosage.

  This specific dosage regimen has not been studied intraoperatively and, because of the time required for titration, may not be optimal for intraoperative use.

  The safety of dosages above 300 mcg/kg/min (0.3 mg/kg/min) has not been studied.

  In the event of an adverse reaction, the dosage of esmolol hydrochloride may be reduced or discontinued. If a local infusion site reaction develops, an alternate infusion site should be used and caution should be taken to prevent extravasation. The use of butterfly needles should be avoided.

  Abrupt cessation of esmolol hydrochloride in patients has not been reported to produce the withdrawal effects which may occur with abrupt withdrawal of beta blockers following chronic use in coronary artery disease (CAD) patients. However, caution should still be used in abruptly discontinuing infusions of esmolol hydrochloride in CAD patients.

  After achieving an adequate control of the heart rate and a stable clinical status in patients with supraventricular tachycardia, transition to alternative antiarrhythmic agents such as propranolol, digoxin, or verapamil, may be accomplished.

  A recommended guideline for such a transition is given below but the physician should carefully consider the labeling instructions for the alternative agent selected.

  Alternative Agent Dosage Propranolol hydrochloride 10-20 mg q 4-6 hrs Digoxin 0.125-0.5 mg q 6 hrs (p.o. or i.v.) Verapamil 80 mg q 6 hrs

  The dosage of esmolol hydrochloride should be reduced as follows:

  Thirty minutes following the first dose of the alternative agent, reduce the infusion rate of esmolol hydrochloride by one-half (50%). Following the second dose of the alternative agent, monitor the patient’s response and if satisfactory control is maintained for the first hour, discontinue esmolol hydrochloride.

  The use of infusions of esmolol hydrochloride up to 24 hours has been well documented; in addition, limited data from 24-48 hrs (N=48) indicate that esmolol hydrochloride is well tolerated up to 48 hours.

  INTRAOPERATIVE AND POSTOPERATIVE TACHYCARDIA AND/OR HYPERTENSION

  In the intraoperative and postoperative settings it is not always advisable to slowly titrate the dose of esmolol hydrochloride to a therapeutic effect. Therefore, two dosing options are presented: immediate control dosing and a gradual control when the physician has time to titrate.

  Immediate Control For intraoperative treatment of tachycardia and/or hypertension give an 80 mg (approximately 1 mg/kg) bolus dose over 30 seconds followed by a 150 mcg/kg/min infusion, if necessary. Adjust the infusion rate as required up to 300 mcg/kg/min to maintain desired heart rate and/or blood pressure. Gradual Control For postoperative tachycardia and hypertension, the dosing schedule is the same as that used in supraventricular tachycardia. To initiate treatment, administer a loading dosage infusion of 500 mcg/kg/min of esmolol hydrochloride for one minute followed by a four-minute maintenance infusion of 50 mcg/kg/min. If an adequate therapeutic effect is not observed within five minutes, repeat the same loading dosage and follow with a maintenance infusion increased to 100 mcg/kg/min (see above SUPRAVENTRICULAR TACHYCARDIA).

  Notes:

  1. Higher dosages (250-300 mcg/kg/min) may be required for adequate control of blood pressure than those required for the treatment of atrial fibrillation, flutter and sinus tachycardia. One third of the postoperative hypertensive patients required these higher doses.

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

  Directions for Use of the 10 mL Ready-to-use Vial (10 milligrams/mL)

  This dosage form is prediluted to provide a ready-to-use, iso-osmotic solution of 10 mg/mL esmolol hydrochloride in sodium chloride recommended for esmolol hydrochloride intravenous administration. It may be used to administer the appropriate esmolol hydrochloride loading dosage infusions by hand-held syringe while the maintenance infusion is being prepared.

  The 10 mL Ready-to-use Vial esmolol hydrochloride at a concentration of 10 milligrams/mL. When using a 10 milligrams/mL concentration, a loading dose of 0.5 mg/kg infused over 1 minute period of time, for a 70 kg patient is 3.5 mL.

  Compatibility with Commonly Used Intravenous Fluids

  Esmolol hydrochloride was tested for compatibility with ten commonly used intravenous fluids at a final concentration of 10 mg Esmolol Hydrochloride per mL. Esmolol hydrochloride was found to be compatible with the following solutions and was stable for at least 24 hours at controlled room temperature or under refrigeration:

  Dextrose (5%) Injection, USP Dextrose (5%) in Lactated Ringer’s Injection Dextrose (5%) in Ringer’s Injection Dextrose (5%) and Sodium Chloride (0.45%) Injection, USP Dextrose (5%) and Sodium Chloride (0.9%) Injection, USP Lactated Ringer’s Injection, USP Potassium Chloride (40 mEq/liter) in Dextrose (5%) Injection, USP Sodium Chloride (0.45%) Injection, USP Sodium Chloride (0.9%) Injection, USP

  Esmolol hydrochloride is NOT compatible with Sodium Bicarbonate (5%) Injection, USP.

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