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Remifentanil
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Administration
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Dosage Forms
References

Pronunciation
(rem i FEN ta nil)

U.S. Brand Names
Ultiva™

Generic Available

No


Synonyms
GI87084B

Pharmacological Index

Analgesic, Narcotic


Use

Analgesic for use during general anesthesia for continued analgesia


Pregnancy Risk Factor

C


Contraindications

Not for intrathecal or epidural administration, due to the presence of glycine in the formulation, it is also contraindicated in patients with a known hypersensitivity to remifentanil, fentanyl or fentanyl analogs; interruption of an infusion will result in offset of effects within 5-10 minutes; the discontinuation of remifentanil infusion should be preceded by the establishment of adequate postoperative analgesia orders, especially for patients in whom postoperative pain is anticipated


Warnings/Precautions

Remifentanil is not recommended as the sole agent in general anesthesia, because the loss of consciousness cannot be assured and due to the high incidence of apnea, hypotension, tachycardia and muscle rigidity; it should be administered by individuals specifically trained in the use of anesthetic agents and should not be used in diagnostic or therapeutic procedures outside the monitored anesthesia setting; resuscitative and intubation equipment should be readily available


Adverse Reactions

>10%: Gastrointestinal: Nausea, vomiting

1% to 10%:

Cardiovascular: Hypotension, bradycardia, tachycardia, hypertension

Central nervous system: Dizziness, headache, agitation, fever

Dermatologic: Pruritus

Ocular: Visual disturbances

Respiratory: Respiratory depression, apnea, hypoxia

Miscellaneous: Shivering, postoperative pain


Overdosage/Toxicology

Symptoms of overdose include apnea, chest wall rigidity, seizures, hypoxemia, hypotension and bradycardia

Support of patient's airway, establish an I.V. line, administer intravenous fluids and administer naloxone 2 mg I.V. (0.01 mg/kg for children) with repeat administration as needed up to a total of 10 mg; glycopyrrolate or atropine may be useful for the treatment of bradycardia or hypotension


Drug Interactions

Increased effect with CNS depressants


Stability

Stable for 24 hours at room temperature after reconstitution and further dilution to concentrations of 20-250 mcg/mL


Mechanism of Action

Binds with stereospecific mu-opioid receptors at many sites within the CNS, increases pain threshold, alters pain reception, inhibits ascending pain pathways


Pharmacodynamics/Kinetics

Onset of effect: I.V.: 1-3 minutes

Protein binding: 92%

Metabolism: Rapid by blood and tissue esterases

Half-life: 10 minutes (dose-dependent)

Elimination: Renal


Usual Dosage

Adults: I.V. continuous infusion:

During maintenance:

With nitrous oxide (66%): 0.4 mcg/kg/minute (range: 0.1-2 mcg/kg/min)

With isoflurane: 0.25 mcg/kg/minute (range: 0.05-2 mcg/kg/min)

With propofol: 0.25 mcg/kg/minute (range: 0.05-2 mcg/kg/min)

Continuation as an analgesic in immediate postoperative period: 0.1 mcg/kg/minute (range: 0.025-0.2 mcg/kg/min)


Administration

Inject slowly over 3-5 minutes


Monitoring Parameters

Respiratory and cardiovascular status, blood pressure, heart rate


Mental Health: Effects on Mental Status

May cause dizziness or agitation


Mental Health: Effects on Psychiatric Treatment

None reported


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Dosage Forms

Powder for injection, lyophilized: 1 mg/3 mL vial, 2 mg/5 mL vial, 5 mg/10 mL vial


References

Hogue CW, Bowdle TA, O'Leary C, et al, "A Multicenter Evaluation of Total Intravenous Anesthesia With Remifentanil and Propofol for Elective Inpatient Surgery," Anesth Analg, 1996, 83(2):279-285.

Kapila A, Glass PS, Jacobs JR, et al, "Measured Context-Sensitive Half-Times of Remifentanil and Alfentanil," Anesthesiology, 1995, 83(5):968-75.

Rosow C, "Remifentanil: A Unique Opioid Analgesic," Anesthesiology, 1993, 79(5):875-6.

Warner DS, Hindman BJ, Todd MM, et al, "Intracranial Pressure and Hemodynamic Effects of Remifentanil Versus Alfentanil in Patients Undergoing Supratentorial Craniotomy," Anesth Analg, 1996, 83:348-353.

Westmoreland CL, Hoke JF, Sebel PS, et al, "Pharmacokinetics of Remifentanil (GI87084B) and Its Major Metabolite (GI90291) in Patients Undergoing Elective Inpatient Surgery," Anesthesiology, 1993, 79(5):893-903.


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