Drugs that pose a deadlier threat

Press, 25 January 1986, Page 19

Drugs that pose a deadlier threat

ROGER HIGHFIELD

in London reports on

the spreading manufacture of drugs cooked up from basic materials to make substitutes for addictive “controlled” drugs, like heroin.

They can be a thousand times more potent than heroin, yet still be as legal as sugar. They are socalled “designer drugs," cooked up from basic chemicals to make substitutes for additive "controlled” drugs, like heroin. They pose a novel challenge to scientists and legislators. Yet, ironically, they may give new insights into neurological diseases. Designer drugs are not new, such as XTC, a hallucinogenic. Others, notably some of the new wave of potent heroin analogues, mostly being manufactured in California, are far more sophisticated and deadly. The fear is that they may soon arrive on the world drug scene. Qualified chemists, rather than amateurs, are now turning their hand to making designer drugs. Last month, Michael Hovey, a Du Pont chemist, was arrested In Delaware for such an offence. It is signficant because it is the first time a professional chemist has been arrested for manufacturing heroin substitutes, and because it means the practice is spreading from California to the east coast of the United States. F

In Britain, the Government is considering whether it needs legislation similar to that being considered by the United States House of Representatives. This aims at eliminating the manufacture and distribution of substances which are chemically related to a controlled drug. They hope to outlaw drugs that have not yet been made. In most countries, heroin, LSD, and cocaine are under the strict-. est control and are designated class A drugs. However, what if an underground chemist soups up a derivative of a class A drug? It may be thousands of times more potent than the original. In the United States, emergency legislation has been introduced that can outlaw a designer drug in six weeks. Even so, in that time the underground chemist can come up with a new — and legal — variation. f

The chemists who make these drugs must be skilful. At the very least, they will be unsuccessful. Worst, they may kill people. Designer drugs may only have a few extra atoms. But they, and as important, their impurities, may be much more powerful than the original. Until recently two major European chemical companies were unknowingly selling a speciality chemical that was “a trivial step, one that you could perform on your kitchen stove” away from fentanyl, a widely used anaesthetic, the grand-daddy of the most notorious family of heroin substitutes. Take 3-methyl fentanyl, for example, a derivative of fentanyl and a powerful narcotic. It produces a “high” similar to heroin but it is 1000 times more potent. A couple of milligrames are lethal. These potent heroin, analogues

present a new challenge to scientists, who must design a test capable of detecting around one thousandth of a million of a gram of the material in body fluids. The best United States assay, based on antibodies, can only detect certain fentanyl derivatives, and even then it is pushed to its limits. It is likely many fentanyl-related deaths in United States go undetected. Detacting fentanyls is one thing; finding out exactly which derivative requires an expensive chunk of equipment called a mass spectrometer, which in effect weighs molecules. Then r

complications still arise: fentanyl derivatives tend to fall apart in the spectrometer and it takes a computer to work out the structure of the original compound. Is there the technology available for an inexpensive assay? According to Dr Gary Henderson, of the University of California, who developed the antibody assay: “Nothing comes to mind.” Underground chemists can reap staggering rewards. Frank Sapienza, a United States Drug Enforcement Administration chemist, estimates that for an outlay of around $3OOO on equipment and chemicals, it is pos-

sible to produce a billion dollars worth of 3-methyl fentanyl. As a bonus, the chemist does not have to bother with Turkish poppy fields or running the gauntlet at customs. The underground chemists make the same approach used by major drug companies to disover new pharmaceuticals. Using the published literature, databases containing details of the latest synthetic chemicals, and the tens of thousands of commercially available speciality chemicals, they can make a number of molecules similar to one that is known to have some pharmacological activity. The respectable idea is to make a product with enhanced activity, fewer side effects, or sidestep another company’s patents. Unlike the drug companies, the “biker .labs” and “bucket chemists” are trying to make a legal version of an illegal sub-

stance, with little concern for drug trials, quality control, or side effects. The underground chemists recently turned their hand to make derivates of Sufentanyl, a recently released drug used in long surgical procedures, such as open heart surgery. Next, according to Dr Gray Henderson, they will move to on to "recreational drugs” such as ampheta-mine-mescalin hybrids: “There is a lot of interesting chemistry when you start mixing the psychedelics with amphetamines,” he says. Dr Henderson believes that some of the fentanyl derivatives are the work of a world class chemist, citing the following evidence: the approach used to find the more powerful derivatives has been systematic; they have been made by using original recipes which are constantly change - in order not to give the

game away by the starting materials; quality control is high; and, in the case of 3-methyl fentanyl, it is so potent that sophisticated handling techniques are required to make and formulate it. This world class chemist is unlikely to be caught One gram of 3-methyl fentanyl is enough to produce one million doses. A single session in his laboratory will set him up for life. Heroin users in California pay up to $75 for each dose of fentanyl derivative. Another disaster, associated with a different class of designer drug, Ironically, could benefit sufferers of Parkinsonism. The drug in question was MPPP, a narcotic about three times as potent as morphine. It appears simple to synthesise but one slip with the acidity or temperature and a different substance emerges, known as MPTP. A mixture of MPPP and MPTP — marketed as “synthetic heroin” — led to the first disaster in 1982. Several people who used it began to “freeze.” They could neither move nor talk. ,- ; » f