J Forensic Sci. 1988 Mar;33(2):569-75.
Abstract
Historically, drugs of abuse have come from two sources: plant products and diverted pharmaceuticals. Today, new, totally synthetic drugs produced by clandestine laboratories have become an increasingly important source of abused substances. Of particular concern are the fentanyls, a family of very potent narcotic analgesics, which first appeared on the streets in California in 1979 under the name "China White". At least 10 different analogs have been identified to date and are thought to be responsible for over 100 overdose deaths. The fentanyls are not used by any particular ethic or age group, but rather by the general heroin using population. Their use, however, does seem to be restricted to suburban, rather than urban areas, and almost exclusively to the state of California. The most potent analogs, the 3-methyl- and beta-hydroxy-fentanyls, may be up to 1000 times as potent as heroin, but are not chemically related to the opiates and therefore not detected by conventional narcotic screening tests. However, using a sensitive radioimmunoassay highly specific for the fentanyls they can be measured at the very low concentrations observed in body fluids, generally less than 10 ng/mL. It is likely that, as efforts to restrict the importation of natural products and prevent diversion of pharmaceuticals become more effective, the fentanyls and other synthetics will become increasingly important drugs of abuse.
see also
In the mid-1980s, it wasn’t clear whether these types of “synthetic heroin” would become a plague or simply fade away. A University of California at Davis pharmacology professor named Gary Henderson studied the chemical impurities in China White and concluded that a single chemist was responsible for all of it. “Most likely he made a few grams of the drug—millions of doses—and then shut up his shop,” he told journalist Jack Shafer in 1985.
Henderson became the scientist doctors turned to when their overdose patients had strange blood samples, and the DEA consulted when it turned up inscrutable chemicals. He had already been researching fentanyl for years; his lab focused on how it was used to dope racehorses, whose urine turned up traces of it. He worked to develop a technique to identify fentanyl and began to understand the nature of the drug, including its potential for chemical manipulation. “Perhaps hundreds,” he said, when asked how many fentanyl analogues would be possible. “Maybe thousands.”
Henderson was way ahead of his time when it came to predicting the horrors not just of fentanyl but of NPS generally. “It seems we are still watching reruns of The French Connection while there is someone out there using a computer to search the chemical literature looking for new drugs to synthesize,” he told the US Senate’s Budget Committee in July 1985, a statement that was remarkably prescient. He coined the phrase designer drugs, defining them as “substances where the psychoactive properties of a drug are retained, but the molecular structure has been altered to avoid prosecution.” Often synthesized from common chemicals, they were skillfully marketed under attractive, exotic names, he added. His 1988 paper “Designer Drugs: Past History and Future Prospects” is nothing less than prophecy, speculating accurately not just on the future of NPS chemistry but on the implications for law enforcement. “In the view of this author,” he wrote, “it is likely that the future drugs of abuse will be synthetics rather than plant products. A single gram of any very potent drug could be synthesized at one location, transported to distribution sites worldwide, and then formulated (cut) into many thousand, perhaps a million, doses…. Preventing the distribution of such small amounts of the pure drug will be exceedingly difficult…. In fact, any success we may have in curtailing the distribution of natural products such as opium, coca, and marijuana and preventing the diversion of pharmaceuticals will only stimulate the development of potent synthetic substitutes.”
Westhoff, Ben. Fentanyl, Inc. (Kindle location 654-674/6750). Grove Atlantic. 2019, Kindle edition.