Analogue drugs are here, and they are deadly. The United States of America is five percent of the entire world’s population, yet we consume seventy-five percent of the world’s pharmaceutical drugs. OxyContin reportedly lost eighty percent of its income when the manufacturer stopped making the pill in a crushable form, where substance abusers could shoot, snort, and smoke the drug.

Drugs that Lead to Overdoses

The heroin sold on the streets is unregulated; it may be cut with potent drugs such as fentanyl, W-18, or other powerful drugs causing many overdoses. Those who were using OxyContin rapidly lose their tolerance to the drug when they stop using it for any period of time, which also contributes to overdoses.

Analogues: Structural analogues of fentanyl include:

Alfentanil (trade name Alfenta), an ultra-short-acting (five- to 10-minute) analgesic.

Sufentanil (trade name Sufenta), a potent analgesic (five to 10 times more potent than fentanyl) for use in specific surgeries and surgery in heavily opioid-tolerant/opioid-dependent patients. Its binding affinity is high enough to theoretically break through a buprenorphine blockade to offer pain relief from acute trauma in patients taking high-dose buprenorphine.

Remifentanil (trade name Ultiva), currently the shortest-acting opioid, has the benefit of rapid offset, even after prolonged infusions.

Carfentanil (trade name Wildnil) is an analog of fentanyl with an analgesic potency 10,000 times that of morphine and is used in veterinary practice to immobilize certain large animals such as elephants.

W-15 and W-18 These are U-opioid agonist with a distinctive chemical structure that does not seem related to any other family of opioid. W-18 is by far the more powerful of the two with bioavailability, half-life, tolerance, 10,000x more powerful than morphine vs. W-15 is 5.4 x stronger.

MT-45, which is about 80%, as strong as morphine.

AH-7921 an opioid analgesic also about 80% the strength of morphine.

U-47700 an opioid analgesic selective for the U-opioid receptor 7.5 times the potency of morphine.

Butyr-fentanyl or butyrylfentanyl is a synthetic opioid analgesic, an analog of Fentanyl, approximately .25% of the strength of Fentanyl.

Acetylfentanyl an analogue of fentanyl 40 times stronger than heroin, 80 times more potent than morphine, and 15 times less potent than fentanyl.

Gray Death: A Combination of Heroin, Fentanyl, Carfentanil, and U-47700, looks like concrete powder, gray in color, causes fatality, absorbed through skin, not safe to the touch,

 

Analogue Drugs

The thinking has been that Fentanyl analogs have been increasing the overdose rate of heroin users for some time If heroin is mixed with an analog, heroin just becomes an easy cause of death for the ME to write down.  Who knows, maybe W-18 is responsible for more deaths in our Nation’s opioid epidemic already than we could ever imagine?  If law enforcement caught one shipment, how many shipments made it through onto our streets?  It’s a scary thought either way; think about it!

Analogue Drugs Are Here

The Drug Enforcement Administration and the Centers for Disease Control and Prevention have been diligently investigating all of the increases in Fentanyl-related non-suicide overdose fatalities across multiple states in the US.  Now these agencies will need to expand their efforts to include analog compounds. These analogue drugs must be stopped.

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