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Not your father’s marijuana

 I guess it seemed like a good idea at the time. In 1985 Michael
Hovey, an organic chemist at du Pont in Wilmington cooked up a batch of 3-methylfentanyl
in his lab, thus ushering in the era of the so-called “designer drugs”. The
drug Hovey made is an analog (close chemical relative) of fentanyl, a very
powerful legal narcotic used during general anesthesia and for chronic pain management.
But 3-methylfentanyl, (sometimes called China White) is 1000-fold more potent,
and this makes it very dangerous. 3-Methylfentanyl is so potent that a dose the
size of a grain of salt will stop you from breathing.

Hovey easily prepared the drug in his lab, and by the time
he was done what he synthesized had a street value of $112 million. After that,
things started to go poorly. Getting rid of the proved to be challenging, as
evidenced by the fact that he tried to sell it to an undercover FBI agent. Later,
out on bail and determined not to go back to prison, Hovey committed “suicide
by police.”

The designer drug industry has grown and flourished, and the
chemists have gotten cleverer. Law enforcement and designer drug chemistry have
been playing tag for years, but the chemists are winning right now. It is trivial
to make small changes in the structure of a psychotropic drug and create a
different drug that will be an even better street drug. Or worse. And maybe
even legal.

Since there are hypothetically an infinite number of permutations
of any drug, some of these substances managed to skirt law enforcement by
virtue of being novel. Some of them haven’t even ever been made, existing only
in the mind of the chemist. This makes regulation of these drugs especially
challenging.

Over the last few years, something called “synthetic
marijuana,”“K2,” or “herbal incense” has rapidly penetratedThe chemical structure
of K2 isn’t even remotely close to that of tetrahydrocannibinol (THC), the active
chemical in pot, but it acts at the same receptor in the brain. In fact, it is
5-fold more potent than THC, with a number of side effects, including seizures,
vomiting, hallucinations and delusions, and heart attacks.

The speed with which these drugs are penetrating American society
is impressive. The American Association of Poison Control Centers estimates
that ER visits were about 15,000 in 2011, compared with fewer than 3,000 in
2010.

So, K2 is banned. Now what? That’s where the chemical innovation
comes into play. By systematically modifying various portions of the molecule,
it is possible to make hundreds of new analogs—some of which will be even
stronger, and possibly even legal. There are K2 analogs that are up to 50-fold
more potent than THC and very dangerous. Depending on how drug laws are
written, and the strategy of the chemist, the new drug may not fit the
definition of what is banned.  may be
different enough from those already on the banned list that they are perfectly
legal.

Using street drugs has its share of hazards, but using
designer street drugs adds another layer of risk. If one believes he is buying
fentanyl, but actually gets 3-methylfentanyl the possibility of a fatal
overdose is obvious. But there is another potential problem that is much less
obvious—the presence of impurities, typically arising from poor synthetic
techniques.

The classic case of this involved a narcotic called MPPP, an
analog of Demerol with properties similar to morphine. This drug was prepared
for recreational use in the 70s, but the first user got a very unpleasant
surprise. The major impurity formed when the chemist is not careful is called
MPTP. MPTP is converted in the body to a metabolite, MPP+ that gets into the
brain and selectively destroys the cells that normally use dopamine, a crucial
neurotransmitter. The result is that dopamine can no longer do one of its jobs—controlling
voluntary movement. This is precisely what happens when the dopamine-containing
cells in the brain die naturally, for reasons that are not
understood—Parkinson’s disease.

Parkinson’s Disease is a neurological degenerative condition
characterized by a progressive loss of control of voluntary motion, including
difficulty in walking, tremor, and rigidity of the body. If it progresses far
enough it can be fatal.

Within a few days of taking contaminated MPPP people started
to develop some of the Parkinson’s symptoms, in most cases irreversibly. And this could happen after a single exposure to the contaminated drug. The first person to
prepare the drug for recreational use was a graduate student in organic
chemistry. He developed severe Parkinson’s symptoms after three days, and
committed suicide two years later. An autopsy of his brain showed profile very
similar to those who had died of the disease “naturally.” The drug continued to
be made, and a bad batch in California in 1982 sent many young people to the
hospital, some with terminal Parkinson’s symptoms.

Designer drugs will continue to be made. There are
potentially thousands of new and different drugs that could be made simply by
starting the synthetic process with a slightly different chemical. This will
ultimately give a different, and possibly unknown designer drug. Some of them
will be perfectly legal, since it is difficult (although possible) to criminalize
something that doesn’t yet exist.

The U.S. now has thousands of permanently unemployed organic
chemists as a result of massive cuts in U.S. -based pharmaceutical research within
the past few years. They are part of the 300,000 pharmaceutical jobs that were
lost in the last decade. It is impossible to say whether any of them will be
desperate enough to take this path, however, the vast majority of them certainly
have the skills required to do so.

According to the DEA, most of these drugs come from China,
most likely synthesized by organic chemists there.