About Fentanyl

WHAT IS FENTANYL?

Fentanyl is a powerful synthetic opioid drug which is approximately 100 times more powerful than morphine (source: Janssen Pharmaceuticals Canada).

It is commonly used legitimately as an anesthetic in hospitals or for long-term pain management in the form of prescription Fentanyl patches.

It is also used in veterinary applications for sedation and general anesthesia.

Fentanyl and its analogues are listed as a schedule I drug under the Controlled Drugs and Substances Act in Canada.

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Fentanyl has become very popular in the sales of illicit street drugs as either a cutting agent or direct substitution for heroin or in the manufacturing of counterfeit Oxycodone pills.

Other illicit drugs such as cocaine and methamphetamine have been found to contain Fentanyl or a Fentanyl analogue. This may be an intentional mix on the part of the drug trafficker or may be as a result of an accidental cross contamination as the drug trafficker may be selling Fentanyl and other illicit drugs.

FENTANYL DETECTED DEATHS (BC)

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© Calgary Police Service

The numbers above have been compiled by the BC Coroners Service for Fentanyl detected deaths in British Columbia up to January 31, 2019

 

Fentanyl detected deaths have dramatically increased over the past few years with the significant increase in illicit Fentanyl making its way to the street. These detected deaths have been most profoundly identified in western Canada such as British Columbia and Alberta but are now increasing substantially across the country as more and more illicit Fentanyl makes its way to the recreational drug market.

Median lethal dose – LD50

The “median lethal dose” (LD50) is a term used as a general indicator of a substance’s acute toxicity. LD50 refers to the dose required to kill half the subjects of a test population. The lethal dose of any substance can vary with the subject depending on size, weight, sex, tolerance for regular exposure. Many illicit drugs have LD50 rates that are based on studies conducted on laboratory animals.

TYPES OF FENTANYL

Fentanyl Patches

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  • Typically contain between 2.5 mg and 10 mg of Fentanyl per patch with the dosage being slowly released over a length of time as identified on the packaging.
  • Recreational drug users are able to open these patches and extract the Fentanyl inside.
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  • Fentanyl patches are not being seen as a source for significant volumes of illicit Fentanyl other than for personal users.
  • There have been occurrences of counterfeit Fentanyl patch production identified in eastern Canada where the abuses of Fentanyl patches are more common than in western Canada
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Fentanyl 72 Hour Transdermal Patch
© Calgary Police Service

CDN 80 Pills

If you encounter green pills with “CDN” stamped on one side and “80” on the other, these are very likely counterfeit OxyContin.

Oxycodone Tablet
Oxycodone Tablet
Counterfeit Oxycodone Tablet - Green Throughout
Counterfeit Oxycodone Tablet - Green Throughout
Counterfeit Oxycodone Tablet - White Center
CLICK TO READ MORE ABOUT CDN80

Oxycodone is a powerful semisynthetic opioid drug that has been used to treat moderate to severe acute or chronic pain under the name of OxyContin. One of the most common forms of Oxycodone in Canada has been the green “CDN 80” tablet which has the letters “CDN” stamped on one side and the “80” on the other side indicating the milligram size of the tablet. These tablets have been diverted or stolen and sold on the street for recreational drug users. Due to the issue of these pills being misused and abused by recreational drug users, the company producing them, Purdue Pharma, discontinued the production of this form Oxycontin in 2012.

Since the removal of the legitimate Oxycontin “CDN 80” tablet, illicit drug traffickers have begun to manufacture counterfeit “CDN 80” tablets using Fentanyl as the active ingredient inside these tablets. A number of Fentanyl analogues as well as other potent synthetic opioids have been found during analysis of these counterfeit tablets.

Originally these counterfeit tablets were found to be a solid color throughout similar to an MDMA tablet, that were easily identifiable to recreational drug users when the pill is split into two as the pharmaceutical version of the “CDN 80” tablet had a green coating but white inside. Over the past few years, illicit drug producers have increased the quality and counterfeit appearance of these counterfeit “CDN 80” tablets to exactly mimic the correct green color exterior and white interior to match that of the now discontinued “CDN 80” tablet.

Other Forms of Fentanyl

You might find illicit Fentanyl in other forms such as blotter paper or liquid.

Carfentanil Paper
© Winnipeg Police
Liquid Fentanyl
© Hamilton Police
Liquid Fentanyl
© Hamilton Police

PRODUCTION OF COUNTERFEIT OXYCODONE TABLETS

Pill press machines used in the production of counterfeit Oxycodone tablets are high quality and pharmaceutical-grade.

Pill press machines like the one in the photograph are capable of producing 10,000 to 18,000 tablets per hour.

© CBC

IMPROPER MIXING OF FENTANYL POWDER AS HEROIN/OXYCODONE

© CBC

As the pure Fentanyl used in counterfeit heroin or counterfeit Oxycodone pills is so potent, the improper mixing of Fentanyl by drug traffickers can easily lead to batches of pills with ‘hot spots’. These batches of counterfeit Oxycodone pills may then be distributed in a specific geographic area and result in an increased number of overdoses/deaths in that area.

SOURCE OF ILLICIT FENTANYL

Through the analysis of illicit drug samples containing Fentanyl, it has been identified that the vast majority of Fentanyl submissions are identified to have not originated from pharmaceutical grade Fentanyl sources. Given the slight reduction of purity levels of these samples, it has been identified that the source of the majority of the Fentanyl which is found in the illicit domestic drug trade is either sourced from drug laboratories overseas or through the production of Fentanyl in domestic clandestine drug laboratories within Canada.

The majority of Fentanyl presently being distributed in Canada in the illicit drug trade is believed to be produced in other countries such as China, and then smuggled into the country, most commonly through international mail and package distribution.

Domestic Fentanyl Production

There are a number of synthesis routes that may be used by an illicit clandestine drug producer to manufacture Fentanyl.

FENTANYL CLANDESTINE DRUG LABS

Unlike commercial methamphetamine and MDMA clandestine drug labs, those producing Fentanyl, given its extreme potency, are often significantly smaller in size. Many solvents used to produce Fentanyl are the same as other synthetic drug production; however their precursor materials are not ones that are used to manufacture methamphetamine or MDMA.

Any suspected Fentanyl clandestine drug lab requires a response by law enforcement members with appropriate training and proper personal protective equipment.

Given the extreme potency of Fentanyl, these clandestine drug labs represent the highest risk of exposure to first responders, trained law enforcement clandestine lab investigators, and the general public.

The clean up and remediation of the locations where these clandestine labs are located is imperative to ensure that contamination does not remain present that could injure or potentially kill people who may be exposed to these locations.

Over the past few years, there has been a noted increase in domestic Fentanyl clandestine drug labs.

 

Bulletin:
Fentanyl, its analogues, and other potent opioids high risk to first responders

Fentanyl Lab

FENTANYL ANALOGUES

A number of Fentanyl analogues have been identified by law enforcement across Canada. Analogues of Fentanyl can vary in potency / toxic properties depending on the chemical structure with some being less potent / toxic than Fentanyl and some being significantly more.

Definition of an analogue: a compound having a structure similar to that of another one, but differing from it in respect of a certain component (Wikipedia).

Fentanyl structure comparison versus 3-methylfentanyl:

The chemical structure of Fentanyl is extremely close to that of an analogue of Fentanyl, 3-methylfentanyl. However, 3-methylfentanyl is significantly more potent / toxic.

Fentanyl Structure
3-Methylfentanyl Structure

Analogues of Fentanyl such as Ohmefentanyl and Carfentanil are significantly more potent than Fentanyl. Carfentanil is approximately 10,000 times more powerful than a comparable dose of morphine versus Fentanyl at 100 times. (source: US Department of Justice Drug Enforcement Administration)

 

DEA Officer Safety Alert regarding Carfentanil

Due to the extreme potency of some analogues such as Carfentanil, these analogues have no legitimate medical use on humans. Carfentanil is only used legitimately as tranquilizer agent for large animals such as elephants.

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Acetyl Fentanyl is an analogue of Fentanyl but has no known approved medical or industrial applications (source World Health Organization – Acetylfentanyl Critical Review Report). As a designer analogue of Fentanyl and one that is not used in the medical community, limited amounts of information is available from testing that has been done on animals. As with any Fentanyl analogues, its pharmacological affects are similar to that of Fentanyl and other synthetic opioid drugs, with the major difference with Fentanyl analogues being the variance in their potency. Within the realm of analogue potency, Acetyl Fentanyl is noted to be less potent than Fentanyl. Fentanyl is approximately 80-100 times the potency of morphine with Acetyl Fentanyl being approximately 15 times the potency of morphine (United States Drug Enforcement Administration – Acetyl fentanyl).

 

Acetyl Fentanyl is one of the common Fentanyl analogues that are seized by law enforcement being smuggled into Canada, typically from China. It is also commonly encountered in street level drugs such as counterfeit heroin and counterfeit Oxycodone “CDN 80” tablets.

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Butyryl Fentanyl (also commonly referred to as Butyrfentanyl) is one of a number of analogues of Fentanyl that have been encountered by law enforcement in the illicit drug trade either with Fentanyl, or as a substitute for it, commonly used by drug traffickers in the manufacturing of counterfeit opioids such as heroin or Oxycodone tablets. Analogues of Fentanyl such as Carfentanil may be found from the creation of these analogues from pharmaceutical companies such as those created by Janssen Pharmaceuticals, which typically have a large amount of data associated to their creation and subsequent testing, or “designer analogues” that have been created outside of the legitimate pharmaceutical industry that typically lack any legitimate testing or studies. By this distinction, Butyryl Fentanyl is classified as a designer analogue of Fentanyl.

 

All analogues of Fentanyl similarly bind to the opioid receptors in the body and create similar symptomlogical affects to the body of that of an opioid, however, the potency and duration of affects can differ significantly between analogues of Fentanyl. Varying potencies for Fentanyl analogues are noted such as Alfentanyl (potency noted as approximately that of morphine) versus Carfentanil (with documented potency from Janssen Pharmaceuticals of 10,000 times that of morphine). Similar variations of duration of affects are noted for Fentanyl (approximately 1 hour) to Carfentanil (7.1 hours).

 

Studies of the potency of Butyryl Fentanyl indicate that the analogue has the approximate potency of ¼ that of Fentanyl or 25 times that of morphine

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Carfentanil is an analogue of Fentanyl that was originally created by Janssen Pharmaceuticals. Subsequent testing conducted on the analogue, identified that it had an extreme potency of approximately 10,000 times that of morphine, or 100 times that of Fentanyl (source Janssen Pharmaceuticals Canada). Due to this extreme toxicity, it was not found to have an application to be used on humans, even within the medical community in highly controlled environments.

 

Carfentanil has subsequently been used legitimately as a large animal tranquilizing agent. This is a drug that is legitimately used by highly trained veterinarians under extreme caution, to sedate animals such as elephants with only extremely small doses required. In discussions with an ex Calgary Zoo employee, they advised me that the Zoo kept Carfentanil on hand, but would only use it to incapacitate and kill any dangerous animal that may escape their enclosure.

 

Legitimately this drug is sold under the tradename Wildnil by a company named Wildpharm. I have personally spoken with representatives of this company who advised that only trained veterinarians under controlled environments are able to use their product. Further, they provide the antagonist Naltrexone directly with the Carfentanil as a reversal agent to be used by a person who may become inadvertently exposed to the Carfentanil for first aid protocols.

 

For reference for the legitimate use of Carfentanil, the United States Drug Enforcement Administration limits the production and importation of legitimate Carfentanil for the entire country to 19 grams in total per year.

 

Carfentanil was first identified in the illicit drug market in Canada during the interception of an extremely large shipment of 1.1 kg of highly pure Carfentanil intercepted by the Canada Border Service Agency in June of 2016. I was the hazardous materials technician that handled this shipment and due to its extreme toxicity, BC Ambulance paramedics who are required to assist during clandestine lab operations by RCMP policy, were originally ordered to leave during the operation by their head Provincial Doctor.

 

Carfentanil is now commonly observed in the illicit drug supply and is noted to be the number one analogue of Fentanyl that is encountered in the British Columbia submissions to Health Canada. Given its extreme potency and inability to be used on humans even within medicine, it is my opinion that the presence of Carfentanil has significantly increased the overdose deaths within the Province of British Columbia.

In addition to the extreme potency of Carfentanil, from literature I have reviewed, Carfentanil is shown to have a half-life of approximately 7.1 hours. This is significantly longer than Fentanyl.

 

Further, in relation to the extreme potency noted for Carfentanil, the use of it in weaponization is a true concern to law enforcement. During the Moscow Theatre Siege of 2002, the Russian Special Forces introduced an incapacitation agent into the Theatre for the purpose of incapacitating the terrorists inside. The introduction of this incapacitation agent resulted in the deaths of 129 hostages. From testing conducted on survivors, the analogues Carfentanil and Remifentanyl were identified and suspected to have been used as the incapacitation agent by the Russian Special Forces.

 

Carfentanil is and analogue of Fentanyl, and therefore listed as a Schedule I substance under the CDSA.

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Cyclopropyl Fentanyl is relatively new analogue of Fentanyl now being found in the illicit drug market commonly used by drug traffickers in the manufacturing of counterfeit opioids such as heroin or Oxycodone tablets. Analogues of Fentanyl such as Carfentanil may be found from the creation of these analogues from pharmaceutical companies such as those created by Janssen Pharmaceuticals, which typically have a large amount of data associated to their creation and subsequent testing. “Designer analogues” that have been created outside of the legitimate pharmaceutical industry typically lack any legitimate testing or studies. By this distinction, Cyclopropyl Fentanyl is classified as a designer analogue of Fentanyl.

 

All analogues of Fentanyl similarly bind to the opioid receptors in the body and create similar symptom logical affects to the body of that of an opioid, however, the potency and duration of affects can differ significantly between analogues of Fentanyl. Varying potencies for Fentanyl analogues are noted such as Alfentanyl (potency noted as approximately that of morphine) versus Carfentanil (with documented potency from Janssen Pharmaceuticals of 10,000 times that of morphine). Similar variations of duration of affects are noted for Fentanyl (approximately 1 hour) to Carfentanil (7.1 hours).

 

Unlike other analogues of Fentanyl that were produced by legitimate pharmaceutical companies with subsequent testing to determine potency and half-life, Cyclopropyl Fentanyl is a new analogue of Fentanyl which at the time of the authoring of this expert opinion, has no known half-life or potency from any form of testing that is known to me.

 

Cyclopropyl Fentanyl is an analogue of Fentanyl, and therefore listed as a Schedule I substance under the CDSA.

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Furanyl Fentanyl is one of a number of analogues of Fentanyl that have been encountered by law enforcement in the illicit drug trade either with Fentanyl, or as a substitute for it, commonly used by drug traffickers in the manufacturing of counterfeit opioids such as heroin or Oxycodone tablets. Analogues of Fentanyl such as Carfentanil may be found from the creation of these analogues from pharmaceutical companies such as those created by Janssen Pharmaceuticals, which typically have a large amount of data associated to their creation and subsequent testing. “Designer analogues” that have been created outside of the legitimate pharmaceutical industry typically lack any legitimate testing or studies. By this distinction, Furanyl Fentanyl is classified as a designer analogue of Fentanyl.

 

All analogues of Fentanyl similarly bind to the opioid receptors in the body and create similar symptomlogical affects to the body of that of an opioid, however, the potency and duration of affects can differ significantly between analogues of Fentanyl. Varying potencies for Fentanyl analogues are noted such as Alfentanyl (potency noted as approximately that of morphine) versus Carfentanil (with documented potency from Janssen Pharmaceuticals of 10,000 times that of morphine). Similar variations of duration of affects are noted for Fentanyl (approximately 1 hour) to Carfentanil (7.1 hours).

 

In 2015, Fentanyl and a number of Fentanyl analogs were restricted in China, which is a source for much of the Fentanyl that is found in the Canadian illicit drug market. Since the restriction of Fentanyl and a number of pharmaceutical created analogs of Fentanyl, Furanyl Fentanyl has now been found to be the most common Fentanyl analog now intercepted by the Canada Border Service Agency being smuggled into Canada. Furanyl Fentanyl had not been seen in the illicit drug trade prior to 2016.

 

Studies of the potency of Furanyl Fentanyl indicate that the analogue has the approximate potency of 1/5 that of Fentanyl or 20 times that of morphine in studies conducted on mice.

 

Furanyl Fentanyl is an analogue of Fentanyl, and therefore listed as a Schedule I substance under the CDSA.

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As the analogue 3-Methylfentanyl was never created by a pharmaceutical company such as Janssen Pharmaceuticals, limited information on the drug is known. Further, as it was not designed by the pharmaceutical industry, it is referred to as a designer analogue of Fentanyl.

 

Potency information available for 3-Methylfentanyl indicates that the drug is between 400 – 6000 times that of morphine, variable dependent on the isomer structure of the molecule. To date, I have not been able to locate any documents that list the half-life of this analogue.

 

3-Methylfentanyl has been a common analogue that has been seen in the illicit drug supply over the past few years, specifically in the British Columbia area.

 

During one fatal overdose that I am aware of in Abbotsford, 3-Methylfentanyl was colored pink when found in the residence of the deceased. In speaking with confidential informants and other police officers, I am aware that Fentanyl and analogues are commonly colored pink after being cut and intentionally sold as Fentanyl in some areas.

 

3-Methylfentanyl is and analogue of Fentanyl, and therefore listed as a Schedule I substance under the CDSA.

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W SERIES COMPOUNDS (i.e. W-18)

4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide (referred to as W-18) is one of a series of compounds including W #1 – 32 compounds that produce analgesic effects (pain killer) similar to other potent opioid agonists such as Fentanyl and analogues of Fentanyl.

W-18 along with W-1 through W-32 was originally developed in 1982 but was never used for pharmaceutical purposes. Drug traffickers in Canada have used W-18 as a substitution for Fentanyl both in powder form and counterfeit Oxycodone tablets.

Recent testing and further research of W-18 has found that it does not bind to the opioid receptor and is an analgesic (pain killer).