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Introduction

Controlled Substance Analogs

The clandestine production, distribution and of "designer drugs," hereafter termed "controlled substance analogs", pose potentially serious threats to the public health and safety as well as unique challenges to the law enforcement, legal and medical communities. Currently the problem of controlled substance analogs appears relatively small when compared to that of other abused substances such as heroin, cocaine or marijuana, in terms of geographic distribution and number of users. Nevertheless, in those areas where controlled substance analogs are available, substantial numbers of people use them and suffer serious adverse consequences. It has been estimated that up to 20 per cent of the narcotic addicts in California use controlled substance analogs. The potential spread of this phenomenon across the country is a very real possibility and a cause for serious concern. The federal government has used its available resources to effectively control and eliminate the eliminate the sources of supply of several of these analogs.. However, new controlled substance analogs continue to surface. Moreover in the past year

they have become increasingly available in and found in areas outside of California. Despite some government successes, this unique facet of the drug abuse problem persists and requires continued attention.

Nature of the Problem

Controlled

substance

analogs

are produced in an effort to

circumvent the provisions of the Controlled Substances Act (CSA). They differ from controlled substances only in slight modifications of chemical structure. Hence, these analogs frequently produce effects indistinguishable from those of the controlled substances which they mimic. The structural changes, however, produce different and distinct chemical entities which unless specifically listed under the CSA, are not controlled under that statute. Because the CSA, for the most part, ties proscribed activities to precisely defined chemical entities, individuals manufacturing or distributing these analogs are not violating the CSA. Only after a substance is scheduled under the CSA can law enforcement take actions take actions against those illegally handling such a substance.

The general phenomenon of controlled substance analogs is not new. Chemical variants of mescaline, phencyclidine (PCP), methaqualone and amphetamine were produced in the 1960's and

. 1970's.

One by one each substance was placed under the CSA or its predecessor laws. The novel aspect of the recent wave of analogs is that extremely potent narcotic substances, capable of replacing heroin, are being produced domestically. The first of these potent synthetic narcotics appeared in California in 1979-1980 under the name`. "China "China White." It was subsequently identified as alpha-methylfentanyl, an analog of the Schedule II

narcotic analgesic, fentanyl (Sublimaze, Innovar).

Analogs of the Schedule II synthetic, narcotic analgesic, meperidine (Demerol) have also been identified in the past several years. To date, eleven fentanyl analogs and two meperidine analogs have been identified in the illicit drug traffic since 1980. These substances are clandestinely manufactured, produce a spectrum of heroin-like activity and range up to 1500 times the analgesic potency of morphine. They can be and are substituted for heroin. Availability of the narcotic analogs has been confined predominantly to California with isolated confirmed occurrences in Delaware, New York, Texas, Oregon and Arizona.

In addition to the narcotic analogs, there are a number of analogs of hallucinogenic amphetamines available. One of these, MDMA, known as Ecstasy or Adam, as Ecstasy or Adam, has been distributed in most sections of the country. Since the emergency scheduling of MDMA in Schedule I of the CSA in July 1985, another analog known as MDE or Eve, has been encountered in a few areas. The attached paper entitled "Controlled Substances Analogs" describes the specific analogs in more detail.

Health Hazards of Controlled Substance Analogs

The health hazards associated with the production and use of controlled substance analogs are a function of their clandestine laboratory origin, unknown pharmacology and toxicology and high potency. Several examples will highlight these hazards.

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The clandestine manufacture of MPPP, a meperidine analog, results in the production of a by-product, MPTP, unless the synthesis is carefully controlled. MPTP produces a parkinsonian syndrome in humans. Several individuals in California who used "synthetic heroin" (MPPP/MPTP) subsequently developed an irreversible, degenerative syndrome indistinguishable from Parkinson's Disease. Forensic samples of MPPP produced in clandestine laboratories contained varying amounts of the neurotoxin, MPTP. This link between MPTP, MPPP and Parkinson's disease was not established until after several lives were ruined.

MDMA, an analog of MDA, has been abused for several years. It is described by advocates of its use, including some psychiatrists, as a safe and mild psychedelic. Until recently very little was known about its pharmacology or toxicology. Animal experiments conducted in 1985, however, have shown that MDMA and MDA destroy serotonergic nerve terminals in the brains of rats. It is believed that the same thing can occur in humans at doses which are ingested by abusers. These serotonergic nerve terminals affect mood, sleep, sexual sexual activity, aggressive behavior and `perception of aversive stimuli.

The fentanyl analogs identified by forensic laboratories may be up to 1500 or more times as potent as morphine. It is extremely difficult to accurately and uniformly mix such potent substances

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with cutting agents.

Additionally, active by-products are formed during the synthesis of fentanyl analogs and they add to the amount of active ingredient present. Several of the fentanyl analogs identified have not been described in the literature; their activities can be estimated but they are not known with certainty. These circumstances all contribute to the likelihood of overdoses. Indeed, there have been over 100 reported overdose deaths associated with the use of fentanyl analogs since 1980.

The

production of these new and untested analogs by chemists using new and untested methods of synthesis leads to impure drugs of unpredictable activity, toxicity and potency which may produce serious injury or death. The hazards associated with the use of these substances must also be considered by others, such as law enforcement personnel or forensic chemists and toxicologists who involuntarily are exposed to these compounds. More information regarding the dangers of incidental exposure to controlled substance analogs must be generated and disseminated to the appropriate people.

various

Non-medical Problems

The controlled substance analog phenomenon has exposed inherent weaknesses in several areas of the government's drug abuse. control program. The first of these is a legal problem and involves the mechanism by which abusable substances are placed under the Controlled Substances Act (CSA).

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