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ARCHIVE:  December 11, 2003

Oxycontin, Oxycodone, Heroin

Dear Dr. Shulgin:

I would like to know what Oxycottons are and what they are used for. And what is in them. Thank you for your time. -- Phyllis

Dear Phyllis:

I suspect that your question refers to one drug, Oxycontin, which has received a great deal of notoriety recently. It is a special preparation of the drug Oxycodone, a Schedule II narcotic analgesic that has been in the pharmacopoeia for many years. Let me lay out a bit of background.

In the listing of the Scheduled drugs, the explicit wording of the names of the classes of narcotics depends on just which Schedule is involved. In both Schedules I and II, compounds that are narcotics and are totally synthetic laboratory inventions are called Opiates. But if the compounds are actual Opium alkaloids, or chemical modifications of these alkaloids, then two names are employed. As Schedule I drugs they are called Opium derivatives, and if they are Schedule II drugs they are called Opium and Opiate. I must presume that Opium is meant to be the poppy plant Papaver somniferum. Then it seems inescapable that the singular word "opiate" means a material synthesized from an opium alkaloid and the plural word "opiates" represents only the narcotics that are laboratory creations.

Within this interpretation, Oxycodone should be called an opiate (singular), since it is a material that is made from codeine or thebaine, both natural Opium alkaloids. It was first prepared maybe a hundred years ago and, as with all the derivatives of these morphine-related treasures, explored in animals for its potential narcotic activity. This specific derivative, codeine with a couple of small molecular changes here and there, was an effective morphine substitute and became commercially available as a prescription narcotic. Modest pills, doses of 5 or 10 milligrams, were well accepted for pain control, either as Oxycodone or under the name of Percodan. It was obvious quite early that the dependence-developing potential of this heroin-like substitute was quite real, but in reality its role in the treatment of pain was excellent. Addiction to narcotics used for legitimate medical use was extremely rare.

This stable prescription situation was disrupted somewhere around 1998 with the introduction of an alternative form known as Oxycontin. This was the same compound embedded in a time-release capsule that would allow a larger dose to be used less frequently. Instead of ten milligrams every three hours, there could be forty milligrams every twelve hours. But the time-release factor was invalid if the pill was chewed up, or dissolved in water and injected. Suddenly there was a new "heroin-substitute" available, and the diversion from clinically valid use to street sales was rapid.

Efforts were made to block the Oxycontin availability, and yet this was a medically approved modification of the original Oxycodone pill. I don't know where this problem stands at the present moment, but the legal scene was rapidly becoming very complex. Efforts have been made to block this, but to allow that, and I suspect that the picture is still rather complex.

Let me accept this unspoken offer to repeat a simple solution that I feel would resolve all this pharmacological chaos. Make heroin legally available to those who have a dependence upon it. There should be neither a negative stigma nor a crime associated with its use, and there should be no disruption of one's social image with a daily fix. We all have our weaknesses. And we are all humans. Let us be who we are.

-- Dr. Shulgin

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