What is Fentanyl Made of?
Though it is a tightly controlled, scheduled substance, pharmaceutical fentanyl is a common target for diversion and abuse. Because of its potency, both diverted and illicitly manufactured fentanyl have inherently high abuse liability as well as dangerous overdose risks.1,2
What Is Fentanyl?
Fentanyl (brand names include Abstral, Actiq, Duragesic, and Subsys) is a synthetically manufactured opioid drug.1,2 In its various formulations, fentanyl is indicated for use in treating chronic and/or severe pain, such as breakthrough cancer pain.1,2
It is also sometimes used for procedural analgesia or sedation, as well as for managing acute post-operative pain.
One of fentanyl’s prescription formulations is an extended-release transdermal patch, which allows the medication to be absorbed through the skin.1,2 Fentanyl is an extremely potent opioid drug; it is commonly reported as being between 50 and 100 times more potent than morphine.
The United States Drug Enforcement Administration (DEA) ) places fentanyl products in the Schedule II controlled substance category.3 This means that the medication has a high potential for abuse as well as severe physical or psychological dependence, but there is an acceptable medical use for it, such as for severe physical pain.3
Because the drug is extremely potent, it can be a very effective analgesic (pain-controlling) medication when used under the supervision of a physician. Unfortunately, the drug’s extreme potency is a double-edged sword since, outside of therapeutic uses, it has also made it attractive to those who abuse drugs for an intense high.7
What Is a Synthetic Opioid?
Naturally occurring opiate alkaloids, such as those contained in the raw plant materials once used to produce opium, are derived from the poppy plant, and have pain-relieving properties.4
Some of these alkaloid substances (e.g., morphine and codeine) are used as building blocks in the manufacturing of pharmaceutical opioid drugs (i.e., semi-synthetic opioids).
Fully synthetic opioids like fentanyl similarly interact with human opioid receptors to elicit their effects, but are made in a laboratory, and require access to specific, regulated chemical components for their production.2,4
Most medications also contain other substances; some may be inert and used to bind the drug into forms that allow it to be taken orally or injected.
Other substances may be added to help the delivery of the drug. For example, the transdermal fentanyl patch includes ethanol (alcohol) to speed up the rate of absorption through the skin.5 Pharmaceutical fentanyl is also available in a sublingual tablet form (Abstral), a troche or lollipop form (Actiq), and as an injectable solution (Sublimaze).3
The Effects of Fentanyl
As an opioid analgesic, fentanyl use is associated with significant physical and psychological effects that include the reduction of pain, feelings of relaxation, and feelings of sedation.2
Recreational users may be drawn to its ability to elicit a reinforcing, euphoric rush, while others may misuse the drug essentially as a means of achieving temporary emotional numbness and dissociation (being removed from potential stressful emotions).2
Over time, a person may become increasingly desensitized to the opioid, thus requiring higher doses to achieve the same effects—this is known as tolerance.
While the neurochemical details of how opiate drugs produce euphoria are somewhat complicated, such rewarding feelings are most likely due in part to increased activity within the dopamine neurotransmitter system, as they are with many other drugs of abuse.6
Increased dopamine release is thought to accompany feelings of reinforcement or reward, and it is suggested that the release of dopamine accounts for the psychologically reinforcing effects of opiate drugs. The pain-reducing effects of opiate drugs are related to their similarity to natural painkilling substances in the brain, such as endorphins and enkephalins.6
These substances may also play a role in feelings of euphoria and wellbeing.
How Is Fentanyl Cut on the Street?
Illicit sources of fentanyl have been known to go by various street names, such as China girl, China white, Tango & Cash, and poison.7When recreational users refer to a drug being “cut,” it could mean that the drug is diluted or combined with some substance that may or may not be inert in order to produce a larger volume of the drug.
However, in some cases where dealers are attempting to increase the potency of low-grade drugs, fentanyl can be used as an additive to heroin. Fentanyl is often passed off as heroin on the street, and because it is far more potent than heroin, it can increase the risk for a fatal overdose.7
Illegally manufactured forms of fentanyl are thought to be a major factor in the increasing prevalence of overdoses on heroin and other opiate drugs.9 It is difficult to estimate the number of people who use fentanyl each year, as many people may not know that they are using products that have been cut with fentanyl.
In 2017, there were more than 70,200 deaths estimated to be due to drug overdoses.10 Overdoses attributed to fentanyl or similar drugs (fentanyl analogs) rose the most steeply, with approximately 28,400 deaths in 2017.10 59% of deaths related to opioid use involved fentanyl in 2017, compared to 14.3% in 2010.11
- Illegally manufactured fentanyl is more potent and less expensive than heroin, and this allows illicit dealers to get more money for a smaller amount of the drug.11 Cutting opioid drugs like heroin with fentanyl or substituting fentanyl for opioid drugs increases profits for illicit drug dealers and also results in an increased risk to users.11
- Small amounts of fentanyl can be extremely dangerous, even in individuals who have developed tolerance to less potent opioid drugs.11
- Illicit fentanyl can be sold by pressing it into counterfeit pills, dropping it onto blotter paper, placing it into a solution in eye droppers or nasal sprays, or as a powder.11 The powder can be snorted, smoked, or injected.
- Some users extract the drug from the gel matrix of the transdermal patches in an effort to inject it, or chew the patches to obtain the extended-release dose immediately rather than over time.2,5 The lozenges or lollipop forms can be abused by chewing them rather than sucking on them to similarly bypass the intended controlled release mechanism.
The Risks of Fentanyl Use and Abuse
Medical use of fentanyl can be safe when under the supervision of a physician. There are numerous potential side effects of fentanyl that can be monitored in clinical situations, such as in instances of fentanyl being used for postoperative pain or other short-term periods.
Some of the side effects associated with fentanyl use include:11,12
- Diminished appetite.
- Nausea and vomiting.
- Dry mouth.
- Trouble urinating.
- Feeling weak or dizzy.
- Loss of consciousness.
- Respiratory depression.
Like all opioid products, the risk to develop significant physiological dependence on fentanyl is extremely high, particularly for people who misuse the drug.12 The development of physical dependence is coupled with a high likelihood of unpleasant opioid withdrawal. Withdrawal symptoms associated with abrupt fentanyl discontinuation are not likely to be fatal, but can be very painful, can compel immediate relapse, and may potentially be associated with certain medical complications such as excessive vomiting, diarrhea and increased risks of dehydration, electrolyte disturbances, and potential aspiration/choking hazards.12,13
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