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Anesthetics /Sedatives

dexmedetomidine (Precedex ®) etomidate (Amidate ®)
fospropofol disodium -LUSEDRA™ ketamine (Ketalar ®)
methohexital (Brevital ®) pentobarbital (Nembutal ®)
propofol (Diprivan ®) thiopental (Pentothal ®)
   
Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.    [  Read the disclaimer    |   <<Back     ]

dexmedetomidine  (Precedex ®)  top of page

Alpha2-adrenergic agonist sedative.

INDICATIONS AND USAGE
Precedex is a relatively selective alpha2-adrenergic agonist indicated for:
  • Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting. Administer Precedex by continuous infusion not to exceed 24 hours. [Note:  various studies have listed infusions for up to 5 days]
  • Sedation of non-intubated patients prior to and/or during surgical and other procedures.

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DOSAGE AND ADMINISTRATION
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  • Individualize and titrate Precedex dosing to desired clinical effect.
  • Administer Precedex using a controlled infusion device.
  • Dilute the 200 mcg/2 mL (100 mcg/mL) vial contents in 0.9% sodium chloride solution to achieve required concentration (4 mcg/mL) prior to administration.
  • The 200 mcg/50mL and 400 mcg/100 mL single-use bottles do not require further dilution prior to administration.
 For Adult Intensive Care Unit Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion of 0.2 to 0.7 mcg/kg/hour.

For Adult Procedural Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion initiated at 0.6 mcg/kg/hour and titrated to achieve desired clinical effect with doses ranging from 0.2 to 1 mcg/kg/hour.

Alternative Doses: Recommended for patients over 65 years of age and awake fiberoptic intubation patients.
INDICATION

DOSAGE AND ADMINISTRATION 

Initiation of Intensive Care Unit Sedation

For adult patients: a loading infusion of one mcg/kg over 10 minutes.

For adult patients being converted from alternate sedative therapy: a loading dose may not be required

For patients over 65 years of age: a dose reduction should be considered

For adult patients with impaired hepatic-function: a dose reduction should be considered

Maintenance of Intensive Care Unit Sedation

For adult patients: a maintenance infusion of 0.2 to 0.7 mcg/kg/hour. The rate of the maintenance infusion should be adjusted to achieve the desired level of sedation.

For patients over 65 years of age: a dose reduction should be considered

For adult patients with impaired hepatic function: a dose reduction should be considered

Initiation of Procedural Sedation

For adult patients: a loading infusion of one mcg/kg over 10 minutes. For less invasive procedures such as ophthalmic surgery, a loading infusion of 0.5 mcg/kg given over 10 minutes may be suitable.

For awake fiberoptic intubation in adult patients: a loading infusion of one mcg/kg over 10 minutes.

For patients over 65 years of age: a loading infusion of 0.5 mcg/kg over 10 minutes

For adult patients with impaired hepatic function: a dose reduction should be considered

Maintenance of Procedural Sedation

For adult patients: the maintenance infusion is generally initiated at 0.6 mcg/kg/hour and titrated to achieve desired clinical effect with doses ranging from 0.2 to 1 mcg/kg/hour. The rate of the maintenance infusion should be adjusted to achieve the targeted level of sedation.

For awake fiberoptic intubation in adult patients: a maintenance infusion of 0.7 mcg/kg/hour is recommended until the endotracheal tube is secured.

For patients over 65 years of age: a dose reduction should be considered

For adult patients with impaired hepatic function: a dose reduction should be considered


Dosage Adjustment
Due to possible pharmacodynamic interactions, a reduction in dosage of Precedex or other concomitant anesthetics, sedatives, hypnotics or opioids may be required when co-administered

Dosage reductions may need to be considered for adult patients with hepatic impairment, and geriatric patients [see package insert]

WARNINGS AND PRECAUTIONS:
  • Monitoring: Continuously monitor patients while receiving Precedex. 
  • Bradycardia and Sinus Arrest: Have occurred in young healthy volunteers with high vagal tone or with different routes of administration, e.g., rapid intravenous or bolus administration.
  • Hypotension and Bradycardia: May necessitate medical intervention. May be more pronounced in patients with hypovolemia, diabetes mellitus, or chronic hypertension, and in the elderly. Use with caution in patients with advanced heart block or severe ventricular dysfunction.
  • Co-administration with Other Vasodilators or Negative Chronotropic Agents: Use with caution due to additive pharmacodynamic effects.
  • Transient Hypertension: Observed primarily during the loading dose. Consider reduction in loading infusion rate.
  • Arousability: Patients can become aroused/alert with stimulation; this alone should not be considered as lack of efficacy.
  • Prolonged exposure to dexmedetomidine beyond 24 hours may be associated with tolerance and tachyphylaxis and a dose-related increase in adverse events
USE IN SPECIFIC POPULATIONS:
  • Geriatric Patients: Dose reduction should be considered.
  • Hepatic Impairment: Dose reduction should be considered.
  • Pregnancy: Based on animal data, may cause fetal harm.
  • Nursing Mothers: Caution should be exercised when administered to a nursing woman.
DOSAGE FORMS AND STRENGTHS:
1] Precedex Injection, 200 mcg/2 mL (100 mcg/mL) in a glass vial. To be used after dilution.
2] Precedex in 0.9% Sodium Chloride Injection 200 mcg/50 mL (4 mcg/mL) in a 50 mL glass bottle. Ready to use.
3] Precedex in 0.9% Sodium Chloride Injection 400 mcg/100 mL (4 mcg/mL) in a 100 mL glass bottle. Ready to use.

etomidate  (Amidate ®)  top of page

Ultrashort-acting nonbarbiturate hypnotic.
Dosing (adults):
Anesthesia: Initial: 0.2 to 0.6 mg/kg IV over 30-60 seconds for induction of anesthesia; maintenance: 5-20 mcg/kg/minute. Produces rapid induction of anesthesia with minimal cardiovascular effects.

Procedural sedation (usual): 0.1 to 0.2 mg/kg IV over 30-60 seconds

Onset of action: 30-60 seconds.
Peak effect: 1 minute.
Duration: 3-5 minutes ( terminated by redistribution).

DOSAGE AND ADMINISTRATION (package insert)
Etomidate Injection, USP is intended for administration only by the intravenous route. The dose for induction of anesthesia in adult patients and in pediatric patients above the age of ten (10) years will vary between 0.2 and 0.6 mg/kg of body weight, and it must be individualized in each case. The usual dose for induction in these patients is 0.3 mg/kg, injected over a period of 30 to 60 seconds. There are inadequate data to make dosage recommendations for induction of anesthesia in patients below the age of ten (10) years; therefore, such use is not recommended. Geriatric patients may require reduced doses of etomidate.

Smaller increments of intravenous etomidate may be administered to adult patients during short operative procedures to supplement subpotent anesthetic agents, such as nitrous oxide. The dosage employed under these circumstances, although usually smaller than the original induction dose, must be individualized. There are insufficient data to support this use of etomidate for longer adult procedures or for any procedures in pediatric patients; therefore, such use is not recommended. The use of intravenous fentanyl and other neuroactive drugs employed during the conduct of anesthesia may alter the etomidate dosage requirements. Consult the prescribing information for all other such drugs before using.

Supplied: 2 mg/ml (10 ml, 20 ml) injection.

fospropofol disodium -LUSEDRA™: top of page

fospropofol disodium -LUSEDRA™ Injection CIV

Mechanism of Action
:
Fospropofol disodium is a prodrug of propofol. Following intravenous injection, fospropofol is metabolized by alkaline phosphatases. For every millimole of fospropofol disodium administered, one millimole of propofol is produced (1.86 mg of fospropofol disodium is the molar equivalent of 1 mg propofol).

INDICATIONS AND USAGE:
LUSEDRA is a sedative-hypnotic agent indicated for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures.

USE IN SPECIFIC POPULATIONS
Patients geq65 years of age should receive the modified dosing regimen.
Patients with severe systemic disease (ASA P3 or P4) should receive the modified dosing regimen.

DOSAGE AND ADMINISTRATION:
Use supplemental oxygen in all patients undergoing sedation with LUSEDRA.  Continuously monitor with pulse oximetry, electrocardiogram, and frequent blood pressure measurements.

Standard dosing regimen: initial intravenous bolus dose of 6.5 mg/kg followed by supplemental doses of 1.6 mg/kg as needed. No initial dose should exceed 16.5 mL; no supplemental dose should exceed 4 mL.

Modified dosing regimen [for patients who are geq65 years of age or who have severe systemic disease (ASA P3 or P4)]: 75% of the standard dosing regimen.

AAdminister supplemental doses only when patients can demonstrate purposeful movement in response to verbal or light tactile stimulation and no more frequently than every 4 minutes.

Adults who weigh >90 kg should be dosed as if they are 90 kg; adults who weigh <60 kg should be dosed as if they are 60 kg.

Intended for single-use administration only.

DOSAGE FORMS AND STRENGTHS::
Injection, solution containing 1,050 mg fospropofol disodium per 30 mL.

CONTRAINDICATIONS::
None

WARNINGS AND PRECAUTIONS
-A person trained in the administration of general anesthesia and not involved in the conduct of the diagnostic/therapeutic procedure should manage treatment of patients with LUSEDRA.
-Respiratory depression
-Hypoxemia
--Hypotension

ADVERSE REACTIONS
Most common adverse reactions (> 20%) are paresthesia and pruritus. (6)

To report SUSPECTED ADVERSE REACTIONS, contact Eisai Inc. at 1-888-422-4743 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS
As with other sedative-hypnotic agents, LUSEDRA may produce additive cardiorespiratory effects when administered with other cardiorespiratory depressants such as benzodiazepines and narcotic analgesics.

ketamine  (Ketalar ®)  top of page

Ketalar is a rapid-acting general anesthetic producing an anesthetic state characterized by profound analgesia, normal pharyngeal-laryngeal reflexes, normal or slightly enhanced skeletal muscle tone, cardiovascular and respiratory stimulation, and occasionally a transient and minimal respiratory depression.

Dosing
(adults): Anesthesia (sedation, analgesia): IM: 3-8 mg/kg. IV: Range: 1-4.5 mg/kg; usual induction dosage: 1-2 mg/kg.
Maintenance
: Supplemental doses of 1/3 to 1/2 of initial dose.
Onset of action: (IV): General anesthesia: 1-2 minutes; Sedation: 1-2 minutes. (IM): General anesthesia: 3-8 minutes.
Duration: 5-15 minutes IV; 12-25 minutes IM.
Supplied: Injection, solution: 50 mg/ml (10 ml); 100 mg/ml (5 ml). Ketalar®: 10 mg/ml (20 ml); 50 mg/ml (10 ml); 100 mg/ml (5 ml).

methohexital  (Brevital ®)  top of page

Ultra short-acting IV barbiturate anesthetic.

Dosing (adults): Anesthesia: IV: Induction: 50-120 mg to start; 20-40 mg every 4-7 minutes. (doses must be titrated to effect).
Onset: IV: Immediately
Duration: Single dose: 10-20 minutes
Supplied: 500 mg, 2.5 g, 5 gram (powder for reconstitution)

pentobarbital (Nembutal ®)   top of page

Short-acting barbiturate with sedative, hypnotic, and anticonvulsant properties.

Dosing (adults): Hypnotic: IM: 150-200 mg. IV: Initial: 100 mg, may repeat every 1-3 minutes up to 200-500 mg total dose. Preoperative sedation: IM: 150-200 mg.

Barbiturate coma in head injury patients or status epilepticus: IV: Loading dose: 5-10 mg/kg given slowly over 1-2 hours; monitor blood pressure and respiratory rate; maintenance infusion: initial: 1 mg/kg/hour; may increase to 2-3 mg/kg/hour; maintain burst suppression on EEG. Status epilepticus: IV: Loading dose: 2-15 mg/kg given slowly over 1-2 hours; maintenance infusion: 0.5-3 mg/kg/hour.
Onset: IM: 10-15 minutes. IV: ~ 1 minute.
Duration: IV: 15 minutes

Supplied
: Injection: 50 mg/ml (20 ml, 50 ml).

propofol (Diprivan ®)  top of page

Dosing (adults):
Induction: General anesthesia: ASA I or II, <55 years: 2-2.5 mg/kg IV (~40 mg every 10 seconds until onset of induction). Cardiac anesthesia: 0.5-1.5 mg/kg IV (~20 mg every 10 seconds until onset of induction). Neurosurgical patients: 1-2 mg/kg IV (~20 mg every 10 seconds until onset of induction).

Maintenance
: ASA I or II, <55 years: IV infusion: Initial: 150-200 mcg/kg/minute for 10-15 minutes; decrease by 30% to 50% during first 30 minutes of maintenance; usual infusion rate: 100-200 mcg/kg/minute (6-12 mg/kg/hour). IV intermittent bolus: 20-50 mg increments as needed.

 ICU sedation in intubated mechanically-ventilated patients: Avoid rapid bolus injection; individualize dose and titrate to response. Continuous infusion: Initial: 0.3 mg/kg/hour (5 mcg/kg/min); increase by 0.3-0.6 mg/kg/hour (5-10 mcg/kg/min) every 5-10 minutes until desired sedation level is achieved; usual maintenance: 0.3-4.8 mg/kg/hour (5-80 mcg/kg/min) or higher.

Onset: Anesthetic: Bolus infusion (dose dependent): 9-51 seconds (average 30 seconds).
Duration
(dose and rate dependent): 3-10 minutes.
Supplied: Injection: 10 mg/ml (20 ml, 50 ml, 100 ml).

thiopental (Pentothal ®)   top of page

Dosing (adults):
Anesthesia: IV: Induction: 3-5 mg/kg.
Maintenance: 25-100 mg as needed. Increased intracranial pressure: IV: Children and Adults: 1.5-5 mg/kg/dose; repeat as needed to control intracranial pressure.

Seizures: I.V.: 75 to 250 mg/dose, repeat as needed.

Renal dosing: crcl <10 ml/minute: Administer 75% of normal dose.
Onset: Anesthetic: IV: 30-60 seconds.
Duration: 5-30 minutes.

Supplied: Powder for reconstitution: 250 mg, 400 mg, 500 mg, 1 g.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
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