Fentanyl
First synthesized in Belgium in the late 1950s, fentanyl, with
an analgesic potency of about 80 times that of morphine, was
introduced into medical practice in the 1960s as an intravenous
anesthetic under the trade name of Sublimaze®. Thereafter; two
other fentanyl analogues were introduced; alfentanil (Alfenta®),
an ultra-short (5-10 minutes) acting analgesic, and sufentanil
(Sufenta®), an exceptionally potent analgesic (5 to 10 times
more potent than fentanyl) for use in heart surgery. Today,
fentanyls are extensively used for anesthesia and analgesia.
Duragesic®, for example, is a fentanyl transdermal patch used in
chronic pain management, and Actiq® is a solid formulation of
fentanyl citrate on a stick that dissolves slowly in the mouth
for transmucosal absorption. Actiq® is intended for
opiate-tolerant individuals and is effective in treating
breakthrough pain in cancer patients. Carfentanil (Wildnil®) is
an analogue of fentanyl with an analgesic potency 10,000 times
that of morphine and is used in veterinary practice to
immobilize certain large animals.
Illicit use of pharmaceutical fentanyls first appeared in the
mid-1970s in the medical community and continues to be a problem
in the United States. To date, over 12 different analogues of
fentanyl have been produced clandestinely and identified in the
U.S. drug traffic. The biological effects of the fentanyls are
indistinguishable from those of heroin, with the exception that
the fentanyls may be hundreds of times more potent. Fentanyls
are most commonly used by intravenous administration, but like
heroin, they may also be smoked or snorted.
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