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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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