This article is Part II of my recent syndicated article on the use of Heroin in hospice patients. I think you will find it informative and historically interesting. If you haven’t read the first article, it is entitled “Heroin, Why It’s Here, And Where It Stands”. Read on.
In as far as the treatment of hospice patients, certainly, an argument could be made for fentanyl, the most potent opiate pain killer ever synthesized by man, and available in the United States. Also known as Duragesic®, and Sublimaze®, the drug’s ability as a pain palliator is legend, but much like morphine, it is more specifically designed for pain and questionable in delivering the euphoric side effect available from Heroin.
Keep in mind that fentanyl is a highly selective opiate mµ receptor agonist. Binding the receptor tightly, fentanyl is built perfectly for pain control. As the synthesis of opiate compounds has evolved, the reach for better pain control with fewer side effects has been the goal in pharmaceutical science.
The “dirtier” or less refined the opioid, the more of accompanying side effects, including euphoria, tend to be present. For instance, opium, codeine, and hydrocodone are considered “more dirty” by practicing physicians. As a drug is refined and we move toward better pain control, one finds drugs like oxycodone, hydromorphone, meperidine, and morphine, ultimately reaching the pristine fentanyl. Interestingly, the dirtier the opioid, the lower on the controlled substance list we find the drug. Go figure.
Fentanyl is what we in Medicine call a “designer drug”. Born in the streets of California, it found its way into the U.S. Pharmacopeia in a circuitous fashion. In 1973, when the Bureau of Narcotics and Dangerous Drugs (BNDD) was disbanded and the Department of Justice reformed it as the Drug Enforcement Administration (DEA), the well known list of controlled substances and the scheduling system for control types was published and made into law.
This list included all known opiate compounds at the time. What resulted from this was a group of black market chemists beginning a campaign to outwit the DEA by modifying opiate drugs, bending their molecular structure so as not to appear on the DEA’s list. A modification would occur and appear on the streets, illegal profits would be made, and with time the DEA would catch up. The DEA would then add the new street drug to their list, but the chemists would move on to a different modification not on the list. This went on for years.
The products of this “make and chase” routine, were “designer drugs”, made by black market chemists to escape the controlled substance list and prosecution by the federal government.
One of these designer drugs ended up on the street as a “new Heroin”, dubbed “China White”. When it first showed up, many Heroin addicts who first tried it at doses to which they were accustomed, died from overdoses. The drug was extremely potent and much lower dosages were required. The Ld50, what we refer to as the lethal dose which will kill at least 50% of those who consume the drug, was tiny when compared to Heroin’s Ld50. Although China White has been the center of much fiction in literature and film lore, the real China White was a designer drug from the black market now known as fentanyl. That’s right!
A pharmaceutical firm eagerly observing and following this war between the DEA and criminal street chemists, isolated the compound, patented it, got FDA approval in the U.S., and reintroduced it as a legal controlled intravenous pain killer under the name Sublimaze®, and later, the transdermal form, Duragesic®.
To this day, Janssen Pharmaceuticals plays this down; vehemently assuring the medical world that Dr. Paul Janssen synthesized the drug in 1960. However, those of us in the medical profession know that they garnished the drug from the streets of Los Angeles and didn’t invent it on their own. Not surprisingly, the profits made from this “legal form” of the drug were in the billions of dollars.
So yes, we have excellent pain nullifying drugs available, they even have a colorful history, but what Medicine seeks is a comfortable place for our patients who are dying with malignant pain. Many in the profession would say, “All we seek for our patients is a peaceful and comfortable calling back to Elysium”.
We have come full circle, and here we are, back at Heroin. We can only wait to see what the future of opiate and even cannabinoid “receptor binding” research brings. Hopefully a drug that is safe, a drug which is perfect for our hospice patients, and with no stigma attached to it.