Fentanyl Guide, Meaning , Facts, Information and Description
Fentanyl is an opioid 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. Fentanyl has an LD50 of 3.1 mg/kg.
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2 Therapeutic use 3 Illicit use 4 Notoriety 5 External links |
Analogues
The pharmaceutical industry has developed several fentanyl analogues of fentanyl:
Therapeutic use
Today, fentanyls are extensively used for anesthesia and analgesia. Duragesic is a fentanyl transdermal patch used in chronic pain management. Actiq is a recently-developed 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 cancer pain. The unit is a raspberry-flavored lozenge on a stick which is sucked to release the fentanyl quickly into the system.
Fentanyl is frequently given intrathecally as part of spinal anesthesia or epidurally for epidural anesthesia and analgesia.
Illicit use
Illicit use of pharmaceutical fentanyls (known as MPPP or China White) first appeared in the mid-1970s in the medical community and continues to be a problem in the United States. United States authorities classify fentanyl as a narcotic. 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.
ACTIQ has begun to appear on the streets under the street name of "percopop".
Mistakes in the manufacture of fentanyls can lead to the creation of MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine), which has lead to Parkinson's disease in some users of these illicit fentanyls. MPTP, which is metabolized to the neurotoxin MPP+ by the MAO-B enzyme, makes its way to the brain where it kills dopamine-producing brain cells in the substantia nigra. This results in symptoms mostly identical to those of Parkinson's disease in the unfortunate individual. It should be noted that the difference between true idiopathic Parkinson's disease and MPTP-induced Parkinson's Disease is that idiopathic Parkinson's disease affects brain areas other than the substantia nigra, while MPTP-induced Parkinson's Disease is selective to the substantia nigra, as noted.
In the late 1970s and early 1980s, some cases of MPTP-induced parkinsonism appeared in California, Maryland, and Vancouver, British Columbia. Media reports of the time may have confused MPTP with MDMA, leading to the persisting rumor that MDMA may lead to Parkinson's disease. Media and law enforcement hysteria from these problems with designer drugs were key to the creation of the United States' Analogue Drug Laws.
Notoriety
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; some owners and trainers of the drugged horses were also fined and/or suspended.
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.
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