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Pronunciation |
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(rem
i FEN ta
nil) |
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U.S. Brand
Names |
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Ultiva™ |
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Generic
Available |
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No |
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Synonyms |
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GI87084B |
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Pharmacological Index |
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Analgesic, Narcotic |
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Use |
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Analgesic for use during general anesthesia for continued
analgesia |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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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 |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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 |
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Drug
Interactions |
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Increased effect with CNS depressants |
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Stability |
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Stable for 24 hours at room temperature after reconstitution and further
dilution to concentrations of 20-250 mcg/mL |
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Mechanism of
Action |
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Binds with stereospecific mu-opioid receptors at many sites within the CNS,
increases pain threshold, alters pain reception, inhibits ascending pain
pathways |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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) |
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Administration |
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Inject slowly over 3-5 minutes |
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Monitoring
Parameters |
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Respiratory and cardiovascular status, blood pressure, heart
rate |
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Mental Health: Effects
on Mental Status |
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May cause dizziness or agitation |
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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Dosage Forms |
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Powder for injection, lyophilized: 1 mg/3 mL vial, 2 mg/5 mL vial, 5 mg/10 mL
vial |
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References |
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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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