By Kurt W.G. Matthies
Recent reports of fentanyl appearing on North American streets are in the news. Counterfeit “Norco” (hydrocodone/APAP) tablets are appearing on California streets, but chemical analysis shows them to contain fentanyl. A large supply of counterfeit fentanyl pills have been seized by Canadian authorities.~~
This powerful opioid is not being diverted from controlled medical stores but is being manufactured in Asia and believed to be smuggled into America via Mexico. Powerless to stop the flow of counterfeit drugs with its multi-billion dollar budget the DEA has released a warning against these new entrants into American drug markets.
These pills bear a certain verisimilitude with heroin pills.
Fentanyl has long been a part of American street heroin culture. Called China White, this high-potency combination of Heroin, morphine, and fentanyl, began to appear on NYC streets during the Vietnam War, and is preferred by many Heroin connoisseurs over other forms of street dope. China White was made famous by the 1960’s French Connection case as told by the popular 1971 American movie starring Gene Hackman.
Because of medical abandonment related to CDC opioid guidelines/restrictions, many suffering Americans who live with chronic pain are turning to the street drug markets to self-medicate their under-treated pain and suffering. As predicted by pain advocates, the drug cartels are inventing new products to fill America’s needs for effective analgesia.
While I would never recommend self-medication with street drugs, I believe it’s important for those who are desperate for effective pain relief and considering this departure from conventional medical care to understand the risks involved with this choice. Remember that all medical treatment, whether or not that treatment is ordered by a licensed physician, is best managed under the principle of informed consent.
All people in pain considering the use of counterfeit fentanyl or street heroin should understand that the unknown dosing and purity of street drugs add an incalculable element of risk to the use of analgesics, even when those drugs are taken orally and not intravenously. You need also to realize that while fentanyl is a highly effective opioid against pain, it is poorly suited pharmacologically for chronic pain treatment. There can be no denial that there is a low probability for success when choosing self-medication with street drugs, especially fentanyl which can kill with the slip of a decimal point.
People who self-medicate with fentanyl can unintentionally “wake up dead.”^^
Fentanyl Use in American Medicine
The transdermal fentanyl patch (Duragesic, Mylan) is used to treat baseline chronic pain. These patches are worn on the skin and are constructed so that medication is slowly and regularly absorbed through the skin, delivering a steady-state dose of fentanyl to the system. This dose is measured in micrograms per hour, i.e., by absorption through the skin.
A microgram is 1/1000 of a milligram or in other words, 1000 micrograms equals one milligram.
A typical starting dose for transdermal fentanyl ranges from 25 to 50 micrograms/hour. Transdermal fentanyl patches come in fixed sizes delivering 12.5, 25, 50, 75, or 100 micrograms per hour. The fentanyl rate of absorption is controlled by the surface area of the patch, thus the 100 microgram patch has twice the surface area of the 50 microgram patch.
FDA warnings clearly state that the transdermal fentanyl patch should only be prescribed for the pain patient who is deemed opioid tolerant, meaning that he or she has used chronic opioid therapy (COT) for 6 months or more, and is requiring regular dose increases due to the effects of opioid tolerance.
When first prescribed the Duragesic transdermal fentanyl patch in 1997, I was using 40mg of oral oxycodone a day and needed yet another dose adjustment to control my pain. My starting dose was titrated to 50 micrograms / hour, but within 18 months, I required 150 micrograms / hour for an equal level of analgesia. Within two years the rapid tolerance caused by fentanyl boosted my opioid dose to unmanageable heights and I was rotated to an appropriate opioid medication.
Use of “the patch” was common during the Decade of Pain, as medical experts believed it to be an abuse-proof drug delivery system. However, resourceful Americans hell-bent on opioid misuse soon discovered that oral absorption of the gel contained within the Duragesic patch, or chewing portions of the Mylan patch quickly maximized a controlled dose of fentanyl to the brain, causing the euphoric rush that accelerates addictive craving.
Oral fentanyl is dosed, not like pills – that are swallowed and metabolized by the GI system — but to quickly dissolve in the mouth and absorbed by the oral mucosa – similar to the trick addicts discovered with that Duragesic goo (but probably more palatable.) Trans-mucosal delivery systems cause dumping of medication into the blood stream, not a new idea. The sublingual tablets used by my grandfather for his heart trouble 60 years ago are a simple transmucosal delivery system for nitroglycerin, which causes rapid vasodilation, relieving the pain of angina pectoris common with cardiac artery insufficiency.
Likewise, transmucosal fentanyl provides quick and effective pain relief for the breakthrough pain experienced by many with chronic pain syndromes maintained on COT. The Actiq fentanyl “lollipop” was an effective medication for the control of severe breakthrough pain in chronic pain patients during the Decade of Pain, but recent fears of misuse and unintentional death have limited transmucosal fentanyl to the realm of palliative care in recent years.
For me, this conservative pullback is a source of pain tantamount to the loss of methadone treatment for baseline chronic pain. My weekend would have benefited from a dose of Actiq after being overcome by an intense pain flare during dinner Friday night. Had I been prescribed Actiq for breakthrough pain, a standard of care for the quick and aggressive treatment of breakthrough pain, my flare would have ended in 10 minutes. Instead, 72 hours later I struggle to get this pain flare under control, and my family plans were again victimized due to the demands of my chronic pain condition.
Intravenous fentanyl (Sublimaze) is very strong medicine, indeed. 100 micrograms (0.1 mg) of Sublimaze is considered to be equivalent to 10 mg of intravenous morphine.
Intravenous fentanyl is considered to be 100 times stronger than morphine.
IV fentanyl is given in the medical procedure room or dentist’s chair in combination with an intravenous benzodiazepene, typically midazolam (Versed), to produce a state known as conscious sedation (or waking anesthesia.) These medications are given at levels to produce moderate anesthesia so that the patient can respond to verbal commands. A typical starting dose might be 35 micrograms fentanyl with 1 mg midazolam, but because of the relatively short half-life of fentanyl, the drug must be repeated every 15 minutes for extended medical procedures.
Fentanyl, like all opioids, depresses respiration, and its medical use against pain must be tapered to minimize this deadly side-effect. But here’s the rub — fentanyl’s half-life for respiratory depression is longer than its analgesic effect, increasing the risk of overdose with extended use against pain. IV fentanyl should never be used without proper medical supervision, and personally I’ve refused IV fentanyl unless administered by a trained anesthesiologist. In my thinking, dentists and surgeons don’t have the training or experience to deal with this powerful drug, especially in an opioid tolerant patient.
The Tragedy of Medical Abandonment
Medical abandonment of people who suffer from daily pain treated with COT is a cruel and dangerous practice in American medicine today. Tragically, many thousands of Americans on COT will be abandoned by their primary care physician this year. Unfortunately, this leaves too many American’s with little choice to stop the pain and suffering. So, they turn to street drugs which are ubiquitous, less expensive, and often easier to acquire than physician prescribed medications in today’s America.
This turn is indeed an act of desperation for the multitudes of abandoned and under treated pain patients caused by opiophobic pain treatment, has the potential to create a public health crisis of unprecedented proportions. An article in last year’s NEJM documents this trend.** The irony is that this crisis will be blamed on those physicians who continue the compassionate and medically sound treatment of chronic pain with opioids.
The hand of the nanny-state driven by the anti-opioid cartel is at the center of this pending public health crisis. Hopefully, strong leadership from the pain management community will help us navigate the National Pain Initiative toward sensible, safer, and compassionate shores. Until they do, all who suffer from chronic pain would benefit from a vigilant awareness of the situation, and I encourage every pain professional to speak out, without fear, regarding the fallacies in today’s current pain treatment paradigm that minimizes the effectiveness of COT. The facts, in unbiased medical research, are evident.
In the meantime, anyone using street drugs to self-medicate pain after medical abandonment needs to be aware of the terrible risk of unintentional overdose and death. If you are considering this route or have already set off down this road, denying the risk involved in using these counterfeit opioids will harm you. By all means, obtain an injectable or intranasal opioid antagonist like Narcan (naloxone) that can quickly reverse overdose, and train a family member to use it. (They must learn to recognize the signs of respiratory depression – you do not want them to inject you if you are only sleeping!)
Please take the time to educate yourself on the use of both opioid agonists and antagonists from a medical perspective. This knowledge may save your life.
^^ Wake up dead – death from an opioid overdose.
** Shifting Patterns of Prescription Opioid and Heroin Abuse in the United States, N Engl J Med 2015;
373:1789-179 DOI: 10.1056/NEJMc1505541
Photo Credit – Calgary Police Service