Given the severity of the Fentanyl poisoning epidemic in every part of our country, I wanted to summarize the pharmacology information for you. Fentanyl is a member of the opiate class of medications. These are derived from the opium poppy. Morphine would be one such medication and is the starting point of where everything else comes from. What I mean by that is mankind has learned to create synthetic opiates such as oxycodone (Percocet, oxycontin), hydrocodone (Vicodin), hydromorphone (Dilaudid), fentanyl, and heroin. Except for heroin, most were designed as analgesics or pain medications. I wanted to clarify again an error that keeps perpetuating itself in the media. Fentanyl is pronounced “fenta-nil” not “fenta-nol.” Also, opioids, the natural analgesics our bodies synthesize, are mistakenly replacing the correct term, which is opiates. All those drugs and medications that are synthesized are called opiates. I wanted to clarify that as people are getting confused, and I hope that clarifies things.
If you have ever had morphine for pain, you notice a euphoric feeling and the mitigation or disappearance of pain. Most people respond that way, but others may get nauseated or agitated. The euphoria in 1 mg of morphine is significant in someone who is “opiate naïve” or never had opiates before. That results from the opiate morphine acting on the mu-opioid receptor in our brains, which are present to bind with the body’s natural opioids. Morphine is many times more powerful than the opioids our body makes. Hence the euphoria. Because of the euphoria and because the body develops a tolerance to opiates, it is addicting, and one will soon require larger doses of the opiate.
Then, the chemists came along and made things like heroin, which is 50 times more potent than morphine, and fentanyl, which is 100 times more potent than morphine, so it has to be used in tiny doses. Instead of milligrams, it has to be used in micrograms. I’ve witnessed that miscalculating the dosage of fentanyl will stop the patient’s breathing, as at higher doses, opiates suppress respiration.
That brings us to our current epidemic, where synthetic fentanyl has become so powerful that contact with the skin or accidentally inhaling it (such as the police officers who check cars or handle drug money without gloves) will stop breathing. Naloxone, or Narcan, is the main antidote for overdose and can be given by injection, IV, or, now, most commonly, intranasally. That’s why groups such as paramedics and police carry it on them. Timing is important because the brain can only survive without oxygen for so long. In training, we would wait for the ambulance to bring the unconscious, non-breathing patient into the ER, and then Narcan was given. Now paramedics and police in the field can treat and revive the patient before they get to the hospital. So Narcan has saved countless lives.
Here are some facts about Narcan. It works by competing with the opiates at that mu-opioid receptor to revive the patient. Suppose you are ever stuck in a situation where you suspect someone has overdosed, and you have access to Narcan. In that case, first, make sure someone dials 911, then the protocol is to give 4 mg (1 spray) every 2-3 minutes up to 10 mg or until the patient revives or medical assistance arrives. Be advised that Narcan works extremely quickly, bringing someone from a state of deep euphoria to wide awake immediately (sometimes within less than a minute). That makes for an unpleasant experience for the patient, and they typically come out of it extremely grumpy at best or fiercely combative at worst. In my experience, using it is like lighting fireworks. You light the fuse and then step back. It is a good idea to have people on hand as the patient may need to be restrained for their safety and the safety of others. The other thing to know is that Narcan only lasts for so long, and if the patient still has the longer-acting opiate in their system, they can stop breathing again and require another dose. Thus, they need to get to the hospital as soon as possible.
Given that naloxone does not have severe side effects, if you give it and the person has not overdosed, they will not respond, and the medication will be metabolized and excreted from the body. I ran into a situation decades ago where a teen patient came in only with a diagnosis of being found unresponsive and not breathing. I was the physician on call, and I immediately ordered Narcan. The providers around me started saying we should not give it as we really don’t know what the issue is. My gut told me we had an unresponsive teen on the weekend, and the most likely culprit was an illicit substance. So, while all the other medical interventions were going on, I gave the Narcan, and in about 30 seconds, the patient sprung awake and was confused and very agitated. The patient was trying to pull out the breathing tube and all the IVs and was thrashing about. Restraints were necessary.
After medical emergencies called “codes” in a hospital, there is a debriefing where we review what went right and what could be improved. My main point to the group was that I had a high index of suspicion of substance abuse (this was way before fentanyl came on the market), and if we gave it and it was not an opiate, nothing would happen, and the patient would not be harmed. Thus, there was no time for deliberation, so I just gave it. I’m not one to hem and haw and discuss theoretical scenarios (called paralysis by analysis). When a patient comes in and is placed on life support, you act and keep acting until you stabilize the patient. Fortunately, it was the right call. The patient had taken so much heroin that they started to react to the opiate again, and I had to put the patient on an IV drip of Narcan until all the heroin was out of the body. The patient fully recovered and left the hospital a few days later. This patient was fortunate to have lived as well as not having any neurologic deficits from the brain being deprived of oxygen. Youth, and the physical resiliency associated with it, helped save this patient and prevent permanent brain damage. Not everyone else is so fortunate.
Some additional information on fentanyl is that it was created by a Belgian physician named Paul Janssen in the 1960s for medical purposes. It first entered the US market around 1976, and there was much debate over its approval by the FDA because it was so powerful.
What is currently happening is that the precursor chemicals used to make the pills are made in China and India. India became a player during a rare Chinese crackdown on synthesizing the precursors. India helped pick up the slack. So, the typical route is that the precursors mainly go to Mexico, where they are combined into a pill and then smuggled into the United States.
The problem is that fentanyl is added to other illicit drugs, such as oxycodone or even Adderall (a medication used for ADD or Attention Deficit Disorder), to give the user a better high. Unfortunately, the fentanyl doses are too high, and the person purchasing what they think is black market Percocet or Adderall will end up overdosing on fentanyl. It is actually a poisoning, not an overdose, as the person ingested fentanyl, and the dose was so high that survival became near impossible. Some statistics to illustrate that this is an epidemic are that there were approximately 9,000 deaths from fentanyl in 2015 and 70,601 deaths in 2021. Additionally, there were 14,699.88 pounds of fentanyl were seized on the southern borderline in the fiscal year 2022.
Please note fentanyl is everywhere, and if someone suddenly becomes confused, sleepy, or loses consciousness and stops breathing, first call or have someone else present call 911 and initiate CPR if indicated. If someone has Narcan on hand, follow the intranasal protocol and keep track of the number of doses they get until medical assistance arrives.
