Fentanyl

Fentanyl

Trade names	Actiq, Duragesic, Sublimaze
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
Article quality
Editor rating	In development
User likes	0

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.

Pharmacology

Pharmacodynamics

Mechanism of action

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

Pharmacokinetics

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

References

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