Esmolol Hydrochloride

Esmolol Hydrochloride Manufacturers

• Baxter Healthcare Corporation
  

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  Esmolol Hydrochloride | Baxter Healthcare Corporation

  

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

  Esmolol hydrochloride 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

  In the absence of loading doses, continuous infusion of a single concentration of esmolol reaches pharmacokinetic and pharmacodynamic steady-state in about 30 minutes.

  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 • 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. • Adjust the infusion rate as required to maintain desired heart rate and blood pressure. Refer to Maximum Recommended Doses below. Gradual Control • 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. • Depending on the response obtained, continue dosing as outlined for supraventricular tachycardia. Refer to Maximum Recommended Doses below. Maximum Recommended Doses • 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. • For the treatment of hypertension, higher maintenance infusion dosages (250-300 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 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 to alternative drugs, the physician should carefully consider the labeling instructions of the alternative drug selected and reduce the dosage of esmolol hydrochloride as follows:

  1. Thirty minutes following the first dose of the alternative drug, reduce the esmolol hydrochloride 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 infusion. 2.4 Directions for Use

  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. The ready-to-use vial may be used to administer a loading dosage by hand-held syringe while the maintenance infusion is being prepared.When using a 10 mg/mL concentration, a loading dose of 0.5 mg/kg infused over 1 minute, for a 70 kg patient is 3.5 mL.

  Esmolol hydrochloride 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.

  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

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• General Injectables & Vaccines, Inc
  

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  Esmolol Hydrochloride | General Injectables & Vaccines, Inc

  

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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 mg/kg (500 mcg/kg) infused over a minute duration followed by a maintenance infusion of 0.05 mg/kg/ min (50 mcg/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.

  
  
  Loading Dose
  (over 1 minutes
  
  
  Maintenance Dose
  (over 4 minutes)
  
  Elapsed Time
  (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*
  greater than 20
  
  
  
  Maintenance dose titrated
  to heart rate or other clinical
  endpoint.
  
  
  *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.
  
  In the treatment of supraventricular tachycardia, responses to esmolol hydrochloride usually (over 95%) occur within the range of 50 to 200 mcg/kg/min (0.05 to 0.2 mg/kg/min). The average effective dosage is approximately 100 mcg/kg/min (0.1 mg/kg/min) although dosages as low as 25 mcg/kg/min (0.025 mg/kg/min) have been adequate in some patients. Dosages as high as 300 mcg/kg/min (0.3 mg/kg/min) have been used, but these provide little added effect and increase the rate of adverse effects, so doses greater than 200 mcg/kg/min are not recommended. Dosage of esmolol 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 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 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 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 to 20 mg q 4 to 6 hours
  Digoxin
  0.125 to 0.5 mg q 6 hours (p.o. or i.v.)
  Verapamil
  80 mg q 6 hrs
  
  The dosage of esmolol hydrochloride should be reduced as follows:
  
  1. Thirty minutes following the first dose of the alternative agent, reduce the infusion rate of esmolol by one-half (50%).
  2. 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. The use of infusions of esmolol up to 24 hours has been well documented; in addition, limited data from 24 to 48 hrs (N=48) indicate that esmolol 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.
  
  1. 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.
  
  2. 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 for one minute followed by a fourminute 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 ).
  
  Note:
  Higher dosages (250 to 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.
  
  Directions for Use of the 10 mL Ready-to-use Vial (10 mg/mL)
  This dosage form is prediluted to provide a ready-to-use 10 mg/mL concentration recommended for esmolol 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 contains Esmolol Hydrochloride at a concentration of 10 mg/mL. When using a 10 mg/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 was tested for compatibility with ten commonly used intravenous fluids at a final concentration of 10 mg Esmolol Hydrochloride per mL. Esmolol 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
  Dextrose (5%) in Lactated Ringer's Injection
  Dextrose (5%) in Ringer's Injection
  Dextrose (5%) and Sodium Chloride (0.45%) Injection
  Dextrose (5%) and Sodium Chloride (0.9%) Injection
  Lactated Ringer's Injection
  Potassium Chloride (40 mEq/Liter) in Dextrose (5%) Injection
  Sodium Chloride (0.45%) Injection
  Sodium Chloride (0.9%) Injection
  
  Esmolol is NOT compatible with Sodium Bicarbonate (5%) Injection.
  Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
  

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• General Injectables & Vaccines, Inc
  

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  Esmolol Hydrochloride | Western Family Foods Inc

  

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  • take only as directed – see Overdose warning • use dose cup • do not exceed 4 doses per 24 hrs

  adults & children 12 yrs & over

  30 mL (2 TBSP) every 4 hrs

  children 6 to under 12 yrs

  15 mL (1 TBSP) every 4 hrs

  children 4 to under 6 yrs

  ask a doctor

  children under 4 yrs

  do not use

  Other information • each 15 mL tablespoon contains: sodium 6 mg • store at 20-25 °C (68-77 °F). Do not refrigerate.

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• West Ward Pharmaceutical Corporation
  

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  Esmolol Hydrochloride | West Ward Pharmaceutical Corporation

  

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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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• Mylan Institutional Llc
  

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  Esmolol Hydrochloride | Mylan Institutional Llc

  

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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 a 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.

  Loading Dose

  Maintenance Dose

  Elapsed Time

  (over 1 minute)

  (over 4 minutes)

  (minutes)

  micrograms/

  milligrams/

  micrograms/

  milligrams/

  kg/min

  kg/min

  kg/min

  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 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 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 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 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 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 mg to 20 mg q 4 to 6 hrs 

  Digoxin 

  0.125 mg to 0.5 mg q 6 hrs (p.o. or i.v.) 

  Verapamil 

  80 mg q 6 hrs 

  The dosage of esmolol should be reduced as follows:

  1. Thirty minutes following the first dose of the alternative agent, reduce the infusion rate of esmolol by one-half (50%). 2. 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.                    

  The use of infusions of esmolol up to 24 hours has been well documented; in addition, limited data from 24 to 48 hrs (N=48) indicate that esmolol 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 to a therapeutic effect.  Therefore, two dosing options are presented:  immediate control dosing and a gradual control when the physician has time to titrate.

  1. 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.

  2. 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 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 to 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 10 mg/mL concentration recommended for esmolol intravenous administration.  It may be used to administer the appropriate esmolol loading dosage infusions by hand-held syringe while the maintenance infusion is being prepared.

  The 10 mL Ready-to-use Vial contains esmolol at a concentration of 10 milligram/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.
  

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• Fresenius Kabi Usa, Llc
  

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  Esmolol Hydrochloride | Fresenius Kabi Usa, Llc

  

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

  Esmolol hydrochloride 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

  In the absence of loading doses, continuous infusion of a single concentration of esmolol reaches pharmacokinetic and pharmacodynamic steady-state in about 30 minutes.

  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

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

  Gradual Control

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

  Maximum Recommended Doses

  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. 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 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 injection to alternative drugs, the physician should carefully consider the labeling instructions of the alternative drug selected and reduce the dosage of esmolol hydrochloride injection as follows:

  Thirty minutes following the first dose of the alternative drug, reduce the esmolol hydrochloride infusion rate by one-half (50%). After administration of the second dose of the alternative agent, monitor the patient’s response and if satisfactory control is maintained for the first hour, discontinue the esmolol hydrochloride infusion. 2.4 Directions for Use

  Esmolol hydrochloride 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.

  Esmolol hydrochloride injection is recommended for intravenous administration.  It may be used to administer the appropriate loading dosage infusions by hand-held syringe while the maintenance infusion is being prepared [see How Supplied/Storage and Handling (16.2)].

  Compatibility with Commonly Used Intravenous Fluids

  Esmolol hydrochloride injection was tested for compatibility with 10 commonly used intravenous fluids at a final concentration of 10 mg esmolol hydrochloride per mL.  Esmolol hydrochloride injection 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 2.1 Dosing for the Treatment of Supraventricular Tachycardia or Noncompensatory Sinus Tachycardia

  Esmolol hydrochloride 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

  In the absence of loading doses, continuous infusion of a single concentration of esmolol reaches pharmacokinetic and pharmacodynamic steady-state in about 30 minutes.

  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

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

  Gradual Control

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

  Maximum Recommended Doses

  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. 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 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 injection to alternative drugs, the physician should carefully consider the labeling instructions of the alternative drug selected and reduce the dosage of esmolol hydrochloride injection as follows:

  Thirty minutes following the first dose of the alternative drug, reduce the esmolol hydrochloride infusion rate by one-half (50%). After administration of the second dose of the alternative agent, monitor the patient’s response and if satisfactory control is maintained for the first hour, discontinue the esmolol hydrochloride infusion. 2.4 Directions for Use

  Esmolol hydrochloride 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.

  Esmolol hydrochloride injection is recommended for intravenous administration.  It may be used to administer the appropriate loading dosage infusions by hand-held syringe while the maintenance infusion is being prepared [see How Supplied/Storage and Handling (16.2)].

  Compatibility with Commonly Used Intravenous Fluids

  Esmolol hydrochloride injection was tested for compatibility with 10 commonly used intravenous fluids at a final concentration of 10 mg esmolol hydrochloride per mL.  Esmolol hydrochloride injection 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

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• Cardinal Health
  

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  Esmolol Hydrochloride | Mylan Institutional Inc.

  

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  2.1 Dosing Information

  Tizanidine tablets may be prescribed with or without food. Once the formulation has been selected and the decision to take with or without food has been made, this regimen should not be altered.

  Food has complex effects on tizanidine pharmacokinetics, which differ with the different formulations. Tizanidine capsules and tizanidine tablets are bioequivalent to each other under fasting conditions (more than 3 hours after a meal), but not under fed conditions (within 30 minutes of a meal). These pharmacokinetic differences may result in clinically significant differences when switching administration of tablet and capsules and when switching administration between the fed or fasted state. These changes may result in increased adverse events, or delayed or more rapid onset of activity, depending upon the nature of the switch. For this reason, the prescriber should be thoroughly familiar with the changes in kinetics associated with these different conditions [see Clinical Pharmacology (12.3)].

  The recommended starting dose is 2 mg. Because the effect of tizanidine peaks at approximately 1 to 2 hours post-dose and dissipates between 3 to 6 hours post-dose, treatment can be repeated at 6 to 8 hour intervals, as needed, to a maximum of three doses in 24 hours.

  Dosage can be gradually increased by 2 mg to 4 mg at each dose, with 1 to 4 days between dosage increases, until a satisfactory reduction of muscle tone is achieved. The total daily dose should not exceed 36 mg. Single doses greater than 16 mg have not been studied.

  2.2 Dosing in Patients with Renal Impairment

  Tizanidine tablets should be used with caution in patients with renal insufficiency (creatinine clearance < 25 mL/min), as clearance is reduced by more than 50%. In these patients, during titration, the individual doses should be reduced. If higher doses are required, individual doses rather than dosing frequency should be increased [see Warnings and Precautions (5.7)].

  2.3 Dosing in Patients with Hepatic Impairment

  Tizanidine tablets should be used with caution in patients with any hepatic impairment. In these patients, during titration, the individual doses should be reduced. If higher doses are required, individual doses rather than dosing frequency should be increased. Monitoring of aminotransferase levels is recommended for baseline and one month after maximum dose is achieved, or if hepatic injury is suspected [see Use in Specific Populations (8.7)].

  2.4 Drug Discontinuation

  If therapy needs to be discontinued, particularly in patients who have been receiving high doses (20 mg to 36 mg daily) for long periods (9 weeks or more) or who may be on concomitant treatment with narcotics, the dose should be decreased slowly (2 mg to 4 mg per day) to minimize the risk of withdrawal and rebound hypertension, tachycardia, and hypertonia [see Drug Abuse and Dependence (9.3)].

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• General Injectables And Vaccines, Inc.
  

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  Esmolol Hydrochloride | General Injectables And Vaccines, Inc.

  

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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 of 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.

  In the treatment of supraventricular tachycardia, responses to esmolol 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 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 may be reduced or discontinued. If a local infustion site ractions develops, and 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 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 in CAD patients.

  After achieving an adequate control of the heart rate and a stable colinical statues 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 carefull consider the labeling instructions for the alternative agent selected.

  The dosage of esmolol should be reduced as follows:

  1. Thirty minutes following the first dose of the alternative agent, reduce the infusion rate of esmolol by one-half (50%).

  2. 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.

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

  INTRAOPERATIVE AND POSTOPERATIVE TACHYCARDIA AND/OR HYPERTENSION

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

  1. 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.

  2. Gradual Control

  For postoperative tachycardia and hypertension, the dosing schedule is the same as that used in supravetnricular tachycardia. To initiate treatment, administer a loading dosage infusion of 500 mcg/kg/min of esmolol for one minute followed by a four-minute maintenance finsution of 50 mcg/kg/min. If an adequate therapeutic effect is not observed within five minutes, repoeat the same loading dosage and follow with a maintenance infusion increased to 100 mcg/kg/min (see above SUPRAVENTRICULAR TACHYCARDIA).

  Notes:

  1. Higher doses (250 to 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 10 mg/mL concentration recommended for esmolol intravenous administration. It may be used to administer the appropriate esmolol loading dosage infusions by hand-held syringe while the maintenance infusion is being prepared.

  The 10 mL Ready-to-use Vial contains esmolol at a concentration of 10 milligram/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.

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