Fentanyl is a narcotic analgesic, first synthesized in Belgium in the late 1950s, with an analgesic potency of about 80 times that of morphine. It 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.
In 1979, fentanyl was at the center of a major scandal in the sport of horse racing, as tests of urine samples revealed the presence of the drug in hundreds of thoroughbred race horses, most of whom had raced at East Coast racetracks (in addition to its analgesic effects, fentanyl has a powerful stimulant effect on horses). The scandal resulted in the horses in question being disqualified from races in which they had either won or had earned a share of the purse, and the purse money was redistributed.
The incapacitating agent used by Russian security forces in the October 2002 Moscow theatre siege incident was a fentanyl derivative, according to a statement issued by the Russian Health Minister Yuri Shevchenko.