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alfentanil (Alfenta, ALF)
Tradename: Alfenta. DEA-controlled substance: class 2.
Indications:
1) analgesia, treatment of pain
2) anesthesia
3) sedation
4) endotracheal intubation
Contraindications:
1) increased intracranial pressure
2) severe respiratory depression
Dosage:
1) 8-20 ug/kg IV bolus
2) then 3-5 ug/kg/dose or infusion 1.5 ug/kg/min
3) total dose 8-40 ug/kg
4) higher doses used by longer procedures requiring endotracheal intubation
Injection: 500 ug/mL (2, 5, 10, 20 mL)
Pharmacokinetics:
1) onset of action: within 5 minutes
2) duration of action:
a) single dose up to 500 ug: 5-10 minutes
b) time to awakenening: 10 minutes following end of surgery
3) metabolized in the liver by cyt P450 3A4
Adverse effects:
1) common (> 10%)
- bradycardia
- peripheral vasodilation
- drowsiness
- sedation
- increased intracranial pressure
- nausea/vomiting
- constipation
- release of antidiuretic hormone (ADH, vasopressin)
- miosis
2) less common (1-10%)
- cardiac arrhythmias, orthostatic hypotension, confusion, CNS depression, blurred vision
3) uncommon (< 1%)
- convulsions, mental depression, paradoxical CNS excitement or delirium, dizziness, dysesthesia, rash, hives, itching, biliary tract spasm, urinary tract spasm, respiratory depression, bronchospasm, laryngospasm, physical & psychological dependence with prolonged use, cold & clammy skin
Toxicity: reversal of toxicity:
1) naloxone 2 mg IV (children 0.1 mg/kg)
2) may repeat as necessary up to 10 mg of naloxone
Drug interactions:
1) CNS depressants
2) phenothiazines
3) tricyclic antidepressants (TCA) may potentiate adverse effects of opiate agonists
4) any drug that inhibits cyt P450 3A4 may increase levels of alfentanil
5) any drug that induces cyt P450 3A4 may diminish levels of alfentanil
Interactions
drug interactions
drug adverse effects (more general classes)
Related
cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
General
opiate
opioid receptor agonist (narcotic)
Properties
MISC-INFO: elimination route LIVER
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Prescriber's Letter 13(3): 2006
Cytochrome P450 drug interactions
Detail-Document#: 220233
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference
- Department of Veterans Affairs, VA National Formulary