Fentanyl And Its Analogues

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Fentanyl was introduced to the United States in 1968 by the Janssen Pharmaceutical Company and marketed under the trade name Sublimaze. Its primary purpose was for use as an intravenous anesthetic and analgesic. It is 100 times more potent than morphine in reducing pain, and its duration of action is only 30 minutes (compared to morphine, which lasts several hours). Over the years, fentanyl has proved to be an extremely useful drug, and to date, it is still widely used for surgeries, childbirth, pain associated with cancer and other diseases, and the treatment of trauma-related injuries. Although fentanyl solutions are often given intravenously, pill forms of the drug are also available.

Due to the success of fentanyl, Janssen and other pharmaceutical companies started to produce other legal fentanyl analogues with a wider range of potency and duration of action, including:

• Alfentanil—also known as Alfenta®, it is very short-acting (5-15 minutes), 20-30 times more potent than morphine, and used for dental, diagnostic, and other minor surgical procedures.

• Sufentanil—also known as Sufenta®, it is extremely potent (2,000-4,000 times more potent than morphine), and is used for heart surgery and childbirth.

• Carfentanil—also known as Wildnil®, it is 10,000 times more potent than morphine and is often used by veterinarians and wild animal researchers to immobilize large animals.

• Lofentanil—another extremely potent fentanyl derivative that is 6,000 times stronger than morphine and is very long-acting (i.e., hours), so it is used only for prolonged surgical procedures and treatment of multiple trauma-related injuries.

In 1979-1980, some illegal fentanyl analogues appeared that were being sold as substitutes for heroin on the street. Suddenly, a series of more than a dozen mysterious deaths occurred in southern California. Upon autopsy, the victims strongly looked as if they had overdosed on heroin; however, no traces of heroin could be found in their bodies. Later, forensic chemists identified a fentanyl analogue (alpha-methyl-fentanyl) that was present in all of the victims. As it turns out, alpha-methyl-fentanyl was being sold on the streets under the name "China White" (Figure 7.2), because it resembled (and contained) pure synthetic heroin that was produced in Southeast Asia.

Later in the 1980s, other fentanyl analogues started to be found in the tissues of heroin users and overdose victims. One such analogue was 3-methyl-fentanyl (see Figure 7.3), which is 6,000 times more potent than morphine. This drug was found in the tissue of 16 overdose victims in Pennsylvania in 1988. In all, more than 150 deaths have been attributed to overdoses of illegal fentanyl analogues. It is likely that victims overdose because they think they are injecting heroin and are ignorant to the potency of the fentanyl analogues that they are actually taking. Alpha-methyl-fentanyl became classified as a Schedule I controlled substance in 1982, and 3-methyl-fentanyl was similarly classified in 1985.

Fentanyl analogues often come as a fine or coarse powder that is either white or yellowish-white (when sold as "China White"), tan (when sold as "Synthetic Heroin"), or light brown (when sold as "Mexican Brown"). Other names for fentanyl or its analogues include "Goodfella" and "Tango and Cash." Drug dealers often cut (dilute) fentanyl analogues with large amounts of powdered sugar so that the actual drug content is very small (as low as 1%). When dealers "cook" the fentanyl analogues, the sugar content can become caramelized, giving it a brownish color. The drugs are mostly injected intravenously but can also be snorted or smoked.

Cut Heroin With Fentanyl
Figure 7.2 China White powder, shown here, is a synthetic form of heroin that is very pure. China White that was tainted with illegal fentanyl analogues, which are hundreds of times more potent than heroin, caused numerous overdoses in heroin addicts in the late 1970s and early 1980s.

Users of fentanyl analogues report that these drugs produce a rapid "rush" or euphoria that is similar to that felt with heroin, followed by a sedated, dream-like state. As analgesics, they also produce a profound loss of pain sensation and have common unwanted side effects such as sleepiness and constipation. However, because they are so potent, fentanyl analogues can

Fentanyl Synthesis

Figure 7.3 The chemical structure of fentanyl and its illegal analogues alpha-methyl-fentanyl and 3-methyl-fentanyl are shown here. Fentanyl was originally designed and marketed as an anesthetic, as it is 100 times stronger than morphine. It is still in use today as a pain reliever for certain surgeries, childbirth, and cancer.

Figure 7.3 The chemical structure of fentanyl and its illegal analogues alpha-methyl-fentanyl and 3-methyl-fentanyl are shown here. Fentanyl was originally designed and marketed as an anesthetic, as it is 100 times stronger than morphine. It is still in use today as a pain reliever for certain surgeries, childbirth, and cancer.

easily produce unexpected respiratory paralysis (stopped breathing) and subsequently death. Some law enforcement agents have reported that fentanyl analogue overdose victims often still have the needle in their arm when they are found, likely because the onset of death was so quick.

Opiate painkillers act on a neurotransmitter receptor called the mu (like the Greek letter m, pronounced "mew") opioid receptor. Mu opioid receptors are present on the surface of many neurons of the brain and spinal cord, and normally serve as receptors for the body's own painkillers such as endorphins. When a person takes fentanyl, meperidine, morphine, or other opiate drugs, the drug binds to the mu opioid receptors, causing neurons in the spinal cord to become inactive. When pain signals from nerve endings in the skin, muscle, or organs arrive at the spinal cord, these signals are not transmitted to the brain, and therefore pain is not experienced. There are also high concentrations of mu opioid receptors in regions of the brainstem that control breathing, so when a person takes an opiate drug, neurons that control breathing become less active and respiration is decreased. Mu opioid receptors are also present in the frontal cortex and limbic system, where opiate drugs act to produce both pleasurable and sedating effects. Finally, mu opioid receptors are present in the intestines, where opiate drugs act to inhibit bowel movements and produce constipation.

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Responses

  • marie
    How to cut fentanyl powder?
    3 years ago
  • SHISHAY
    Do dealers use sweetners to cut fentanyl analogs?
    2 years ago
  • christopher
    What color is fentanyl?
    1 year ago
  • Eglantine Lothran
    How to remove powder sugar from heroin fentanyl?
    6 months ago
  • Merigo
    What does street fentanyl powder look like?
    1 month ago

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