FENTANYL (pharmacokinetic profile)

Structure/Class
  1. Phenylpeperidine opioid (fentanyl/sufentanil/remifentanil/alfentanil)
Pharmacodynamics
  1. As above
Absorption/administration
  1. PO, IV, SC, Patch, intra-nasal, lozenges
Distribution
  1. Rapidly leaves the blood stream and accumulates in highly perfused tissues (brain/kidney/lung/heart)
  2. Importantly, fentanyl is lipophilic and tends to accumulate in fatty tissue, particularly after high dose/long term infusion.
  3. Overall high first pass metabolism.
Metabolism
  1. Hepatic (almost fully metabolised) by CYP3A4 system (c.f. codeine, which is by the CYP2D6 system)
    • No active metabolites
Excretion
  1. Renal
Special notes