Fentanyl – A Primer

Fentanyl is an extremely potent drug, whose legitimate uses include pain relief for cancer patients. It is one of the most potent drugs in the pharmacopeia. A usual dose of 100 micrograms or less does the trick; it would take about 10 milligrams of morphine to achieve the same result. For those who are metric challenged, a milligram is equal to 1,000 micrograms. If you do the math, fentanyl is about 100 times more powerful than morphine.

Fentanyl was first synthesized in 1960, and made its way into legitimate medicine a few years later. It is listed in Schedule 2 of the Controlled Substances Act (CSA), owing to its extreme potency, making it highly prone to abuse. During my career with DEA, I never encountered the stuff until I had been “off the bench” for several years.

The CSA, along with state drug laws, has been on the books since 1970. Most of the listed drugs were “grandfathered” into it from earlier statutes. Obviously, there needs to be a mechanism for adding new substances. To do so, one needs to elucidate the correct chemical structure (not always easy), demonstrate that it has been “abused”, and then, DEA (part of the Department of Justice) can propose it for addition to the Act. The law, however, requires concurrence of the Department of Health and Human Services. Once this has been achieved, the drug can be added to the list. This can easily take months.

Unfortunately, fentanyl is relatively easy to make. Moreover, fentanyl “analogues” are also easily synthesized. As a consequence, there are numerous clandestine “laboratories” making these substances. The Internet describes several “one pot” procedures. There are at least a dozen or so of these analogues out there in the traffic. They are closely related structurally to fentanyl, and have the same effects. Only fentanyl, itself, was illegal. If someone was busted for trafficking in an analogue which was not on the list, no prosecution was possible under the CSA. What is a narc to do? Even back in the day, in my early career in the 1960’s, there were clever chemists who made analogues which were not listed (as the saying went they were staying “one carbon atom” ahead of the feds).

By now, you might be wondering what an “analogue” is. If a molecule such as fentanyl is represented by a Christmas tree, each ornament might be likened to an organic functional group. For example, a methyl functional group consists of a single carbon atom bonded to three hydrogen atoms. If the fentanyl tree is decorated with a methyl group, an analogue is formed. This is a different organic compound from fentanyl. Its effect on the human body may be the same as fentanyl, be totally different, or, in many instances, much more potent. The position where the group is bonded to the fentanyl molecule is indicated by a number, or a greek letter. Thus, an additional methyl group may be 3-methyl fentanyl or alpha-methyl fentanyl, each of which are compounds distinct from fentanyl itself.

This issue came to a head in the late 1970’s when a new, more powerful “synthetic heroin” appeared on the West Coast, sold as “China White”. The stuff, however, caused some fatalities, always bad for business. Some of the material was submitted to the DEA Special Testing and Research lab. At first, the sample was found to contain nothing but lactose, a harmless cutting agent. When the chemists concentrated the mixture, however, they were able to detect miniscule amounts of a new (to us, anyway) substance which appeared to be similar to fentanyl. It was later found to be alpha-methyl fentanyl. (“Later” took several weeks during which many more might have overdosed).

Clearly, a speeded-up process to add stuff like this to the CSA had to be devised. Congress did pass a law, the Controlled Substances Analogue Act, in 1986. This pretty much said that if a substance was “chemically similar” to a controlled drug (if it looked like a duck…) it was illegal. This helped somewhat, but with the plethora of illegal substances flooding the market during the 2010’s, it was not adequate. In 2018, Congress passed legislation to permit DOJ to list substances by class, rather than specific name. Fentanyl analogues could be regarded as a “class” of drugs, and included in the CSA. Unfortunately, the legislation was to specified expire in two years. Congress has passed legislation to extend this provision when the current law expires on February 8th of 2020. Stay tuned…….

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