Clinical Information

Fentanyl is an extremely fast acting synthetic opioid related to the phenylpiperidines.(1,2) It is available in injectable as well as transdermal formulations.(1) The analgesic effects of fentanyl is similar to those of morphine and other opioids(1): it interacts predominantly with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues.(1,3)

Fentanyl is approximately 80% to 85% protein bound.(1) Fentanyl plasma protein binding capacity decreases with increasing ionization of the drug. Alterations in pH may affect its distribution between plasma and the central nervous system (CNS). The average volume of distribution for fentanyl is 6 L/kg (range 3-8).(3,4)

In humans, the drug appears to be metabolized primarily by oxidative N-dealkylation to norfentanyl and other inactive metabolites that do not contribute materially to the observed activity of the drug. Within 72 hours of intravenous (IV) administration, approximately 75% of the dose is excreted in urine, mostly as metabolites with less than 10% representing unchanged drug.(3,4)

The mean elimination half-life is:(1-3)

-IV: 2 to 4 hours

-Iontophoretic transdermal system (Ionsys), terminal half-life: 16 hours

-Transdermal patch: 17 hours (range 13-22 hours, half-life is influenced by absorption rate)

-Transmucosal:

-Lozenge: 7 hours

-Buccal tablet

-100 to 200 mcg: 3 to 4 hours

-400 to 800 mcg: 11 to 12 hours

In clinical settings, fentanyl exerts its principal pharmacologic effects on the CNS. In addition to analgesia, alterations in mood (euphoria, dysphoria) and drowsiness commonly occur.(1,3) Because the biological effects of fentanyl are similar to those of heroin and other opioids, fentanyl has become a popular drug of abuse.