Although Heroin is a highly addictive opiate narcotic, it is an extremely effective painkiller and anxiolytic. In fact, in the United Kingdom, it is used the same way in which we physicians in the United States use Morphine.
That's right. In the UK, Heroin is manufactured and prescribed as the drug, Dimorphine. We U.S. physicians feel this is unnecessary, and potentially risky, as Dimorphine is quickly metabolized by the liver into Morphine, the so-called, "warm blanket" of the opiate world.
It seems, however, that the side effects to Heroin make it an "electric warm blanket" when talking about it with IV Heroin users. Having interviewed many former intravenous Heroin users, they consistently inform me that they feel the euphoria from Heroin is much more intense and more pleasant than the euphoric effects of Morphine. Interestingly, because of this more intense effect, many physicians have started thinking outside the box regarding this medication's ability to treat the hospice patient. Certainly, Europe is leaning in this direction concerning palliative therapy in terminally ill patients with malignant pain. Germany, Switzerland, Denmark and the Netherlands have legalized its use in this regard, and currently Norway and other European Union nations are considering a move in this direction.
It seems that of the first world nations, the Union of Europe always leads with the Caduceus first. In a humanitarian effort to make a more dignified and comfortable place for the dying patient, one should not be surprised that Europe made the first move, moreover, Germany, the worlds engineering guru, would be the first nation to endorse it in this way. It is very interesting that Germany advances this particular type of therapy. As you may have guessed, Heroin is a German Invention.
Historically, Heroin had an interesting birth. After Dr. Bayer of Bayer Laboratories (a German company to this day) isolated acetylsalicylic acid from willow bark, he was able to move forward with other work. Aspirin, the very first in an important class of medications now known as Non Steroidal Anti-Inflammatory Drugs, is what he isolated from willow bark. After this great discovery, his now wealthy laboratory went to work isolating isomers of the central nervous system's mµ receptor agonists we call opiate compounds.
What Bayer Labs isolated was diacetylmorphine. You guessed it, Heroin. The company went to work immediately, packaged the drug in liquid form, and began selling it over the counter in the United States as a non-addictive cough medicine patented with the brand name, Heroin, meaning "hero within." That's right. Heroin is a registered trademark of Bayer Laboratories. I know. Wouldn’t you like to have that trademark?
This marketing campaign went on from 1895 to 1910. Then, reports from the U.S. began to mount from a concerned American public, undermining Bayer's marketing efforts, warning of the morphine metabolite and addiction. You must remember that at that time, most Americans were already aware of the severe problem with morphine and its evil hold, as we were taking care of hundreds of thousands of Civil War Veterans wounded in combat who had become addicted to it. Bayer soon capitulated with embarrassment and removed the product from the marketplace.
Of interest, is that the U.S. Congress would install the Harrison Narcotics and Tax Act, making Heroin illegal, 4 years later. By 1924, it was a felony to even possess the drug, and has been ever since.
Chances are, Americans in general, will never accept this drug for any therapy, no matter what argument is laid on the table. Americans, the first industrialized people to have dealt with this dragon on a gigantic scale, at war with cartels who push it through our southern borders, and dealing with a monster which runs wild in our streets to this day, will probably never accept or tolerate its presence in our pharmacopeia.
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 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, many opiate addicts associate the dirtier side effects with potency, however, 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 suddenly from overdoses. The drug was unknowingly, 100 times more potent than Heroin. The Ld50, what we refer to as the lethal dose which will kill at least 50% of those who consume a 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 terminal patients who suffer, is a peaceful and comfortable calling back to Elysium”. Understand, we are looking for more than just pain control. We are looking for comfort and dignity for those who suffer. As a Healer, I not only endorse it, I make it my mission!
We have come full circle, and here we are, back at Heroin, the first true synthetic opiate. A German invention for pain. And why not? German scientists, it seems, have always lead the way in modern medicine. Since The Age of Enlightenment, there they were and here they are, with ideas that have withstood the test of time. The Fathers of Microbiology, Aspirin, Psychiatry, The X-Ray, The EKG, Cancer Chemo-Therapy, and now, trying to find for humans who suffer, a way to leave with dignity and without fear. We can only wait to see what the future of opiate and even cannabinoid “receptor binding” research brings, especially in regard for the suffering hospice patient.
Hopefully a drug that is safe, a drug which is suited for the effects our hospice patients need without obtunding their ability to think clearly, or their ability to enjoy a good laugh and a beautiful sunset.
Dr. Counce
Author Resource:-
Founded by Dr. Charles Counce, The Conservatory of Medical Arts and Sciences is a higher education consulting firm and private charitable teaching resource based in the mountains of Lake George, Colorado. The Conservatory is the flagship of The Venture 17 Division of Education, a nonprofit collegiate consulting firm and professorate specializing in higher academics in the medical arts and sciences.
The Doctor is a professor of Human Anatomy and Physiology, as well as Cardiopulmonary Medicine, Molecular Biology, Clinical Biochemistry, and Hematology. In addition, he teaches American History.
Dr. Counce's blog, "The Searchlight Messenger", can be seen and commented on at http://www.venture17.com