Drugs and Chemicals of
Concern > Fentanyl
FENTANYL
(Trade Names: Actiq®, FentoraTM,
Duragesic®; Street Names: Apache, China girl, China white, Dance fever,
Friend, Goodfella, Jackpot, Murder 8, TNT, Perc-O-Pop, Lollipop, Tango and
Cash)
September 2007
DEA/OD/ODE
Introduction:
Fentanyl is a potent
synthetic opioid. It was introduced into medical practice as an
intravenous anesthetic under the trade name of Sublimaze in the
1960s.
Licit Uses:
The clinical use of
fentanyl has increased during the past decade. For example,
fentanyl prescriptions increased from about 0.5 million in 1994
to 7.04 million in 2006 (IMS Health). Fentanyl pharmaceuticals
are currently available in the dosage forms of oral transmucosal
lozenges, commonly referred to as the fentanyl
"lollipops" (Actiq®), effervescent buccal tablets (Fentora™),
transdermal patches (Duragesic®), and injectable formulations.
Oral transmucosal lozenges and effervescent buccal tablets are
used for the management of breakthrough cancer pain in patients
who are already receiving opioid medication for their underlying
persistent pain. Transdermal patches are used in the management
of chronic pain in patients who require continuous opioid
analgesia for pain. Fentanyl citrate injections are administered
intravenously, intramuscularly, spinally or epidurally for
potent analgesia and anesthesia. Fentanyl is frequently used in
anesthetic practice for patients undergoing heart surgery or for
patients with poor heart function. Because of a recent concern
about deaths and overdoses resulting from fentanyl transdermal
patches (Duragesic® and generic version), on July 15, 2005, the
Food and Drug Administration issued safety warnings and
reiterated the importance of strict adherence to the guidelines
for the proper use of these products.
Chemistry and
Pharmacology:
Fentanyl is 100 times more
potent than morphine as an analgesic. It is a µ opioid receptor
agonist with high lipid solubility and a rapid onset and short
duration of effects. Fentanyl rapidly crosses the blood-brain
barrier. It is similar to other µ opioid receptor
agonists (like morphine or oxycodone) in its pharmacological
effects and produces analgesia, sedation, respiratory
depression, nausea, and vomiting. Fentanyl appears to produce
muscle rigidity with greater frequency than other opioids.
Unlike some µ opioid receptor agonists,
fentanyl does not cause histamine release and has minimal
depressant effects on the heart.
Illicit Uses:
Fentanyl is abused for its
intense euphoric effects. Fentanyl can serve as a direct
substitute for heroin in opioid dependent individuals. However,
fentanyl is a very dangerous substitute for heroin because it is
much more potent than heroin which results in frequent overdoses
that can lead to respiratory depression and death.
Fentanyl patches are
abused by removing the liquid contents from the patches and then
injecting or ingesting these contents. Patches have also been
frozen, cut into pieces and placed under the tongue or in the
cheek cavity for drug absorption through the oral mucosa. Used
patches are attractive to abusers as a large percentage of
fentanyl remains in these patches even after a 3-day use.
Fentanyl oral transmucosal lozenges and fentanyl injectables are
also diverted and abused.
Abuse of fentanyl
initially appeared in mid-1970s and has increased in recent
years. There have been reports of deaths associated with abuse
of fentanyl products.
Illicit Distribution:
Fentanyl is diverted via
pharmacy theft, fraudulent prescriptions, and illicit
distribution by patients and registrants (physicians and
pharmacists). Theft has also been identified at nursing homes
and other long-term care facilities. Fentanyl oral transmucosal
lozenges (Actiq®) are typically sold illicitly (street names:
"Perc-O-Pop" or "Lollipop") at $20 to $25
per unit or $450 per carton (contains 24 units) while
transdermal patches (Duragesic®) are sold at prices ranging
from $10 to $100 per patch depending upon the dose of the unit
and geographical area. According to the National Forensic
Laboratory Information System, state and local cases involving
fentanyl expressed as a percent of the total of all drug cases
increased by 18-fold from 0.0078 percent in 2001 (37 cases) to
0.144 percent in 2006 (1,472 cases involving 1,643 drug items).
Clandestine Manufacture:
During the last year, the
distribution of clandestinely manufactured fentanyl has caused
an unprecedented outbreak of hundreds of suspected fentanyl-related
overdoses and over 972 confirmed and 162 suspected fentanyl-related
deaths among the heroin user population. Most of these deaths
have occurred in Delaware, Illinois, Maryland, Michigan,
Missouri, New Jersey, and Pennsylvania. DEA has immediately
undertaken the development of regulations to control the
precursor chemicals used by the clandestine laboratories to
illicitly manufacture fentanyl. Recently, one of the precursors
was designated as a List 1 chemical. DEA is now in the process
of designating a second chemical as a schedule II immediate
precursor.
Control Status:
Fentanyl is a schedule II
substance under the federal Controlled Substances Act of 1970.
Comments and additional information are welcomed by the
Drug and Chemical Evaluation Section, FAX 202-353-1263 or telephone
202-307-7183.
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