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First synthesized in Belgium in the late 1950s, fentanyl, (Schedule II controlled substance) 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 in the present. 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 similar to those of heroin, with the exception that there is less of a euphoric 'high' associated with the drug and a stronger analgesic effect. Additionally, fentanyl may be hundreds of times more potent — though in some places, it is sold as heroin, often leading to overdoses. Fentanyl also has a shorter half-life than that of heroin, and is most commonly used orally, but like heroin, can also be smoked, snorted or injected.

Actiq has appeared on the streets under the street name of "percopop". The pharmacy retail price ranges from US$16 to US$50 per unit (based on strength of lozenge), with the black market cost anywhere from US$20 to US$60 per unit, depending on the strength.

Some heroin dealers mix fentanyl powder with larger amounts of heroin in order to increase potency or compensate for low-quality heroin, and to increase the volume of their product. As of late May 2006, a mix of fentanyl and either cocaine or heroin has caused an outbreak in overdose deaths in the United States, heavily concentrated in the cities of Detroit, Philadelphia, Milwaukee, Camden, Chicago,, and Little Rock. The mixture of fentanyl and heroin is known as "magic", among other names, on the street.

Both Actiq and Duragesic are becoming as popular as OxyContin in pharmacy burglaries and robberies. In the U.S., law enforcement agencies are being instructed in how to tell the difference between Actiq and other medications so they are better able to notice abuse of the drug.

Several large quantities of illicitly-produced fentanyl have been seized by U.S. law enforcement agencies. In June 2006, 945 grams of 83%-pure fentanyl powder were seized by Border Patrol agents in California from a vehicle which had entered from Mexico. Mexico is the source of much of the illicit fentanyl for sale in the U.S. However, there has been one domestic fentanyl lab discovered by law enforcement, in April 2006 in Azusa, CA. The lab was a source of counterfeit 80 mg OxyContin tablets containing fentanyl instead of oxycodone, as well as bulk fentanyl and other drugs.

The "china white" form of fentanyl refers to the clandestinely produced alpha-methyl strain (AMF) . This has been reported in the literature to be twice the strength of regular fentanyl. The main bonus of the alpha-methyl is it provides a site of resistance to metabolic degradation resulting in a drug with an increased duration .

Fentanyl has been diverted by pharmacy theft, fraudulent prescriptions and illicit distribution by patients, 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 at $20-25 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. There is evidence of large illegal distribution rings selling fentanyl products along with other opioid pharmaceuticals.

Source: DEA Diversion Control Program

Symptoms of an overdose from Fentenyl are:

  • low breathing
  • seizures
  • dizziness
  • confusion
  • dry mouth
  • weakness
  • loss of consciousness
  • coma
  • confusion
  • tiredness
  • cold and clammy skin
  • small pupils

Typical side effects of Duragesic therapy include abdominal pain, anxiety, confusion, constipation, depression, diarrhea, dizziness, dry mouth, euphoria, hallucinations, headache, impaired or interrupted breathing, indigestion, itching, anorexia, nausea, agitation, shortness of breath, sleepiness, sweating, urinary retention, vomiting, and weakness.

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