Fentanyl
Trade names

Actiq, Duragesic, Sublimaze

Fentanyl.svg
Clinical data
Drug class

Opioid

Uses

Analgesia

Routes of administration

Buccal, Epidural, Intrathecal, Intravenous, Transdermal

Dosage
Pharmacodynamics
Mechanism of action

μ-opioid agonism

Pharmacokinetics
Onset of action

5 minutes

Duration of action

30-60 minutes

Metabolism

Hepatic (CYP3A4)

Redistribution half-life

6 minutes (initial) 1 hour (slow)

Elimination half-life

16 hours

Protein binding

80-85%

Physical and chemical data
Formula

5 minutes

Molar mass

336.479 g/mol

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Fentanyl is a synthetic, lipophilic phenylpiperidine opioid agonist used for analgesia. It is highly lipophilic leading to fast passage across the blood-brain barrier with a 6.8 minute onset time. Fentanyl will also rapidly redistribute to adipose and fatty tissue leading to a short duration of action.

Uses

  • Administration
    • IV, IM, transdermal, intranasal, intrathecal, epidural, buccal.

Contraindications

Absolute contraindications

Precautions

Pharmacology

Pharmacodynamics

Mechanism of action

  • µ-selective opioid receptor
  • Low affinity: delta & kappa opioid receptors

Adverse effects

Pharmacokinetics

  • Context Sensitive Half Time
    • Infusion or repeated doses lead to prolong duration of action as drug redistributes back from tissue to plasma.

Chemistry and formulation

History

References

  1. Comer SD, Cahill CM. Fentanyl: Receptor pharmacology, abuse potential, and implications for treatment. Neurosci Biobehav Rev. 2019 Nov;106:49-57.