Fentanyl: The Ebola Of Opioids

“This guy can make dope out of the dirt in your pockets,” a DEA agent said about George Marquardt in a 1993 interview with the Canberra Times. He was referring to a legendary kingpin known as the ‘Drug Wizard of Wichita’. He called Marquardt “the very best illicit chemist in the history of American drug making—and one of the deadliest.”

Marquardt, a self-taught chemist and gadgeteer from Kansas, ran the first major illegal fentanyl lab in the USA. He was known as the ‘Walter White of Wichita’. White, to the uninitiated, is a fictional character from the TV series Breaking Bad. He was a high school chemistry teacher who became a methamphetamine manufacturer and dealer. White was to meth as Marquardt was to fentanyl.

Marquardt was enticed by the (financial) “independence” and “working with highly potent and volatile chemicals.” Fentanyl is so deadly that it’s almost impossible to create safely in a covert setting. But he did just that. He cracked the recipe for fentanyl and made it himself in an illegal lab. He started by working with a friend to produce fentanyl “using basic lab equipment and old chemistry manuals.” He was about 15 years old. He then sold his secret to drug dealers and other manufacturers.

He went to prison for 22 years because people died from fentanyl use and this was traced back to him. When the feds caught him, the USA’s first fentanyl epidemic was seemingly resolved. But it made a comeback. Marquardt was released in 2015. He died recently—not due to fentanyl—but to old age.

What is it for?

Famous for being the drug that killed Prince, fentanyl is the most potent opioid pain reliever on the market. It is 50 to 100 times stronger than heroin and 100 times more potent than morphine. It is usually prescribed for people with chronic severe pain who do not respond to other opioids. Many users are cancer patients or the dying. Palliative care patients are often already taking opiates, like morphine, when fentanyl is prescribed to them.

Fentanyl is also used as an anaesthetic in surgery. Strict guidelines are imposed on which patients should use fentanyl and for what purpose.

Carfentanil, on the other hand, is 100 times stronger than fentanyl. It is used to tranquilize elephants.

What is it made of?

Fentanyl is a synthetic opioid. An opioid is an opium-like compound that binds to one or more of the three opioid receptors of the body [1]. It is made up of chemicals and synthesized from opium, which comes from the poppy plant. Its chemical name is N-phenyl-N propenamide [2].

Illegal versions are a mix of heroin, cocaine, Xanax, and other hazardous materials. These combinations are made to increase the euphoric effects of fentanyl. Xanax is a benzodiazepine used to treat anxiety, panic, and phobias.

When people buy black market drugs, they don’t know they are ingesting fentanyl because some pills look like legal prescription drugs. Others are tricked into thinking they bought heroin. This is why the risk of fatal overdose and death is astronomical.

What other names does it go by?

Slang terms include: Apache, China White, China Girl, China Town, Dance Fever, Friend, Goodfellas, Great Bear, He-Man, Jackpot, King Ivory, Murder 8, Poison, Tango & Cash, and TNT [2].

Brand names include: Abstral, Actiq (lollipop), Duragesic (patch), Fentora, Onsolis (buccal soluble film), and Sublimaze (intravenous anaesthetic).

Actiq was the first rapid-release version for treating cancer breakthrough pain. Onsolis, which comes in a small disc taken orally, cannot be abused by crushing and snorting it.

What does it look and taste like?

The Centre for Addiction and Mental Health (CAMH) says it is often impossible to tell if a powder or pill contains fentanyl. Illegal fentanyl usually doesn’t have a specific taste, colour, or odour.

Some claim that it is generally white when legal and off-white or brown when illicit. Heroin that is light brown may look lighter when it has fentanyl in it.

Fentanyl powder is sweet compared to heroin, which is bitter. Some users say fentanyl has a medicine-like smell.

In what formats is it available?

Fentanyl is administered via transdermal patch, pill form, powder, lozenge (aka ‘lollipop'), sublingual tablet or spray (placed or sprayed under the tongue), effervescent buccal tablet or spray (inserted or sprayed inside the cheek), buccal soluble film, injection, nasal spray, and inhaler.

The transdermal format is like a nicotine patch with gel in it. The fentanyl is released slowly over two to three days. The injectable form is normally used for anaesthetic purposes, usually combined with a benzodiazepine during surgical procedures. The lollipop format was originally meant for cancer patients who can’t swallow pills.

How did it originate?

Belgian chemist Dr. Paul Janssen first developed the drug in 1959. He founded Janssen Pharmaceutica in 1953 and introduced fentanyl as an injectable anaesthetic in the 1960s. Johnson & Johnson now owns Janssen Pharmaceutica, which has its headquarters in Beerse, Belgium.

The US Food and Drug Administration (FDA) approved the manufacture and distribution of fentanyl in 1968. Abuse of the drug became prominent in the 1980s, though people had already started using it illicitly in the 1970s. The first batch of fentanyl overdoses in the US was reported in the 1990s.

The effects of fentanyl

What are its beneficial effects?

Pain relief, relaxation, euphoria, sedation.

What are its side effects?

Seizures, low blood pressure, confusion, drowsiness, dizziness, nausea, vomiting, appetite loss, sweating, urinary retention, rigidity of the chest wall and abdominal muscles (associated with injected formulations), constipation, clammy skin, bluing of the skin (cyanosis), itchiness, abnormally slow and irregular heartbeat, constricted pupils, respiratory failure, and coma.

If the last three symptoms occur together, opioid poisoning may be present. Chest wall rigidity makes it difficult to perform CPR.

Overdose symptoms include excessive sleepiness (it is difficult to wake the patient), slow, shallow breathing, gurgling, weak pulse, pale face, sweaty skin, limpness, purpling/bluing of the lips, inner lips and fingertips, and passing out.

These effects are also found in people who use other opioids like heroin, morphine, hydromorphone, hydrocodone, methadone, and oxycodone.

What are its withdrawal symptoms?

Insomnia, anxiety, agitation, restlessness, chills, sweating.

Why is it such a dangerous drug?

Fentanyl is so powerful that just two milligrams, the equivalent of four grains of salt, is enough to kill an adult. Its potency is also a danger to emergency responders and law enforcement crew, who risk harm from exposure. That is why they wear epidemic-grade protective gear during rescues and raids.

“Fentanyl is one of the most dangerous opioid painkillers,” says Dr. Charles Reznikoff, an addiction specialist at the Hennepin County Medical Center in Minnesota. “Fentanyl is what I call the ‘ebola of opioids’ because it kills you quickly, as opposed to many of the other opioids that take a long time and are less apt to kill you in overdose.”

The Centers for Disease Control and Prevention (CDC) says that because fentanyl is so strong, the difference between a dose that will get a person high and one that can kill is very small. One can overdose even on a prescription patch where the dose is known. Everyone handles fentanyl differently. One person’s prescription can kill another. The risk of fatal overdose is even higher with simultaneous use with other drugs and alcohol.

Why did the FDA approve it if it’s so harmful?

When the FDA approved fentanyl, it was supposed to be an analogue for Demerol (synthetic opioid pain medication) and meant only for patients in end-of-life care. An analogue is a drug whose structure is related to that of another drug but whose chemical and biological properties may be different [3].

Fentanyl was meant to be an analgesic (narcotic painkiller) and anaesthetic, and not for recreational use. The United States Controlled Substances Act of 1970 classifies it as a Schedule II narcotic.

In 2005 and 2007, the FDA issued public health warnings on the high potential for abuse and dangers of the fentanyl patch, both generic and branded.

How is it absorbed into the body?

This depends on how it is administered. When it’s injected, the effects are localised. When taken sublingually, it reaches the bloodstream through the lower surface of the tongue and the floor of the mouth. In lozenge form, it’s absorbed through the mucous membrane lining the inside of the mouth.

Regardless of how it’s taken, it affects the respiratory centre and the central nervous system quickly by crossing the blood-brain barrier.

How does it affect the brain?

Fentanyl binds itself to opioid receptors located in the areas of the brain that control pain and emotions. When it does, dopamine levels in the brain’s reward centres increase. This produces euphoria and relaxation. Like all opioids, though, fentanyl is not selective when it connects to opioid receptors. It doesn’t just go to the reward centers of the brain, but also to the parts that control breathing.

How long does it stay in the body?

Fentanyl’s effects happen really quickly because it crosses the blood-brain barrier faster than other opioids, but these don’t last long.

Hamilton Morris, a journalist and chemist specialising in psychoactive drugs, says, “It’s a very short duration opportunity opioid, which necessitates compulsive, constant redosing. If you’re addicted to fentanyl, unless you’re doing a transdermal patch, you typically can’t make it through a single night with having to redose. It’s always done in these prolonged-release formulations, like a lollipop that you suck, or a patch. It’s not a drug well-suited to street use. It shouldn’t be used as a heroin replacement.”

Good intentions

Marquart thought he was doing the public a favour by manufacturing fentanyl. He thought that one of the major burdens of being addicted to heroin is its price. So he figured that by substituting inexpensive fentanyl, the price of heroin would go down, and the financial burden associated with opioid addiction would be reduced. It could be potentially safer. But that is not what happened and many people died.

How do users abuse it?

They snort, inject, smoke, chew, or swallow it. Some remove the gel from the transdermal patch and inject or eat it. Others freeze the patch and place it inside the cheek or under the tongue. Fentanyl is also put on blotter paper. Some fentanyl street drugs masquerade as legal pharmaceutical medication.

Why do people use it?

For rapid effects and euphoria, especially in large doses. Novalynn Tagata, a recovering fentanyl addict, explains that fentanyl can “achieve the best high, better than any opioid. If you got it, you hit gold.”

How does it feel to use it?

“Once it hits, it shuts everything off within seconds,” claims Tagata.

Kalama Colburn, who got addicted to fentanyl after using her grandma’s meds for a back injury, describes it as a “magic pill that numbs pain.” She said it relieved her depression by giving her physical and emotional comfort.

How does it feel to stop using it?

Storm Hultsman, an opiate addict in recovery, describes it: “It’s like you’re in a burning house and only breathing smoke. Then you finally step outside and get a breath of fresh air.”

Is there an antidote for it?

Naloxone, an opioid antagonist, can temporarily reverse opioid overdose effects within five minutes. It helps restore breathing. It is given via injection, a handheld auto-injector (Evzio), and a nasal spray (Narcan). It works, even when fentanyl has been taken with other opioid drugs or alcohol. It doesn’t work, however, on non-opioid drugs.

New York State has a Naloxone Initiative involving community members, prisons, law enforcement, schools, first responders, healthcare professionals, firefighters, and pharmacies in the stockpiling, distribution, and administration of naloxone.

Methadone was implemented as a medical treatment for opioid use disorder. The FDA established it in 1966 and approved it in 1972. Considered the gold standard in treating opioid use disorders, it is highly effective in reducing fentanyl use.

Dr. Joseph Turban, addiction specialist at Ku Aloha Ola Mau, an addiction treatment center in Hawaii, explains: “Methadone keeps people out of withdrawal. It takes away the physical and mental craving, the flu-like illness.”

The FDA approved buprenorphine in 2002. As effective as methadone, it is administered sublingually daily or every other day.

Doctors often have fentanyl addicts taper off the drug than stopping it completely because of withdrawal symptoms. This opioid maintenance, compared to diabetes treatment with insulin, is usually combined with psychosocial therapy to pinpoint triggers and determine root causes.

The National Institute on Drug Abuse (NIDA) also recommends naltrexone, which blocks opioid receptors and prevents fentanyl’s effects.

Where does fentanyl come from?

The DEA claims that China is the current source of most of the fentanyl in the US. It is manufactured very cheaply there. Mexican drug dealers mix it with more expensive heroin or cocaine to increase potency and lower the cost, then sell it across the border. Interestingly, China does not have a fentanyl abuse problem.

US President Trump admonished China in a Twitter thread where he insisted that all postal carriers “search for and refuse all deliveries of fentanyl from China (or anywhere else).”

Per the Associated Press, Liu Yuejin, the Vice Commissioner of China’s National Narcotics Control Commission, said China is not the source of the fentanyl that’s killing Americans. He said China is making extensive efforts to control fentanyl, and should not be labelled as the opioid’s main origin. “We began regulating all fentanyl-related drugs as a class of controlled substances with the aim of curbing illegal drug trafficking. No cases of fentanyl smuggling have been discovered between the US and China since the new measures were implemented,” Liu claimed. He also noted that fentanyl deaths in the US continue despite China’s strict controls, an indication that the drugs were not coming from China.

Solutions

As fentanyl abuse/dependence counts as a substance use disorder, detoxification is the first step towards recovery. Rehabilitation centres offer this in combination with residential treatment, medication, community support, and behavioural therapies.

The alcohol and drug abuse division of Hawaii’s Department of Health has implemented the Hawaii Opioid Action plan to stop opioid abuse by treating addiction more like a chronic illness and less like a crime. Police stations statewide have set up prescription drug drop boxes, so excess meds don’t wind up in the wrong hands.

They’re also investigating more drug treatment options as an alternative to incarceration. Law enforcement stands behind this. Gary Yabuta, Director of Hawaii HIDTA (high-intensity drug trafficking area), whose mission it is to stop the flow of fentanyl into Hawaii, says, “We cannot lock addicts up and think this is going to go away.”

A law passed in the last legislative session limits prescription opioids to just seven days because people can get hooked in a matter of weeks.

The CDC suggests to doctors that before giving out prescription fentanyl, they should assess if a patient is a good fit for the drug based on their history of potential opioid or alcohol abuse. If not, they should explore other options.

Is there hope for fentanyl addicts?

“You will suffer unimaginably, but the ones that love you also suffer with you,” says Hultsman. If addicts realize this, they will make an effort to recover.

Tagata got healed for her children. Her turning point was when she found herself sitting on a cardboard box by the road without shoes, not having showered for three weeks and talking to herself. Her family drove past her but didn’t stop. She testifies: “I lost everything, but gained it all back in a year. There is hope, success, and life after addiction.” She wants the same for others like her.

Fentanyl Statistics

• The CDC claims that every 11 minutes, someone in the US dies of an opioid overdose.
• A BBC News report stated that across the US, about 3,000 deaths occurred from opioids like fentanyl in 2013. In 2017, this increased to over 29,000 (but the CDC said it was 70,000). More Americans died of drug overdoses that year than in the Vietnam, Iraq, and Afghanistan wars combined.
• In New York City, since July 1, 2016, nearly half (47%) of confirmed drug overdose deaths involved fentanyl. New York State had a 20.4% increase in opioid overdose deaths from 2014 to 2015.
• Per the National Forensic Laboratory Information System, pharmaceutically and clandestinely produced fentanyl in the US increased from 5,400 in 2014 to over 14,600 in 2015.
• In Massachusetts, 75% of those who died from an unintentional overdose in 2016 had fentanyl in their system.