Designer Drugs: Chemistry, Analysis, Regulation, Toxicology, Epidemiology & Legislation of New Psychoactive Substances

By Roy Gerona

A title in the Emerging Issues in Analytical Chemistry series, Designer Drugs: Chemistry, Analysis, Regulation, Toxicology, Epidemiology & Legislation of New Psychoactive Substances presents both an overview and a guide to techniques for designer drug analysis. Proliferation of the synthesis and use of designer drugs is a serious public health problem with social, economic, and legal implications. Whether abuse is studied at the population level or the individual level, researchers need both background and highly detailed technical information on specific drugs and drug classes in order to combat the proliferation and highly damaging consequences of these substances. Author Roy Gerona provides a comprehensive discussion that emphasizes the potential threat to society, presents the ongoing challenges confronting the various laboratory approaches to detection and identification of new chemical entities, and informs the development of improved analytical solutions for use in legislation, law enforcement, and treatment.

Designer Drugs: Chemistry, Analysis, Regulation, Toxicology, Epidemiology & Legislation of New Psychoactive Substances offers an introduction to the field and a source of information on specific drugs, drug effects, and analytical tools to a wide audience for anyone studying or engaging in designer drug analysis. Analytical and medical chemists, pharmacologist, toxicologists, and students, researchers, and policy makers in the fields of drug abuse, medicine, public health, and forensics will greatly benefit from this essential text.

• Summarizes available literature and evaluates the strengths and weaknesses of analytical methods for detecting and identifying designer drugs
• Directs the reader to sources of further reading at the conclusion of each chapter
• Emphasizes the potential threat to society
• Presents ongoing challenges confronting various laboratory approaches to detection and identification of new chemical entities

• Language: English
• Publisher: Elsevier Science
• Release date: Jan 17, 2024
• ISBN: 9780128118153

Roy Gerona

Assistant Adjunct Professor Roy Gerona works at the University of California San Francisco in the USA.

Book preview

Chapter 1: NPS origins and use

Abstract

The first decade of this century witnessed an unprecedented resurgence of designer drugs across a wide variety of classes. The convergence of Internet marketing, availability of information and user experiences in online drug forums and social media, ease of global distribution, novel ways of large scale production, unavailability of laboratory methods to detect their use, and inability of drug laws and policies to keep up with control and regulation contributed to their explosive spread and public health threat. Designer drugs' history started at the turn of the 20th century. The current resurgence is a culmination of developments in organic chemistry, technology, manufacturing, distribution, and social connectivity, along with a more open and daring approach to substance use. Because their pharmacological actions are similar to traditional recreational drugs but potencies and toxicities are inadequately known, they are a significant health threat. Rapid evolution of molecular identity is designed to skirt laws, challenge analysis, and foil control.

Keywords

Designer benzodiazepines; Designer drugs; Legal highs; New psychoactive substances; New synthetic opioids; Research chemicals; Synthetic cannabinoids; Synthetic cathinones; Synthetic drugs

Definition

Change is the only constant in the universe. This is true for recreational drugs as for our evolving lifestyles. Designer drugs in the 1980s has morphed into multiple terms: new psychoactive substances, novel psychoactive substances, legal highs, and research chemicals are currently in use, but even experts cannot agree on a formal collective name. In this book, we will call them new psychoactive substances (NPS).

These come in many forms. Depending on their chemical or pharmacological class, they are sold as pills, powders, blotters, injectables, joints, herbs, inhalants, vaping fluids, and edibles (Fig. 1.1). The more common classes are synthetic cannabinoids, synthetic cathinones, new synthetic opioids (NSO, opioid analogs), designer benzodiazepines, amphetamines, phenethylamines, piperazines, and tryptamines. There is usually a popular form associated with an NPS class. Synthetic cannabinoids are available as herbs and joints and are sometimes incorporated in vaping fluids and edibles, while NSO are typically powders, pills, or injectables.

What are NPS? The United Nations Office on Drugs and Crime (UNODC) defines them as substances of abuse, either in a pure form or a preparation, that are not controlled by the 1961 Single Convention on Narcotic Drugs or the 1971 Convention on Psychotropic Substances, but which may pose as a public health threat (see the last section of this chapter for more information on these conventions) (UNODC, 2021a). New does not necessarily refer to newly created drugs, but rather to substances that have recently become available in the recreational drug market. Hence, some NPS were synthesized and studied by academic and pharmaceutical laboratories decades ago. For example, methcathinone, an analog of methamphetamine, was first synthesized in the 1920s but became a popular NPS in the United States in the 1990s (Gonçalves et al., 2019).

Figure 1.1  Common forms of new psychoactive substances (designer drugs).

An NPS can pose a health threat because it exerts pharmacologic effects such as those of traditional recreational drugs (TRD, common drugs of abuse) such as cocaine, methamphetamine, heroin, and cannabis. It does this because it is either a structural or a functional analog of the drug it mimics. Structural analogs have chemical structures very similar to traditional recreational drugs (Fig. 1.2). Acetyl fentanyl, for example, differs from fentanyl only by having one less methyl group. The similarity in structure allows the NPS to bind to the same receptors with which the TRD interacts to facilitate its psychoactive effect. Some receptors can tolerate structural diversity in the molecules they interact with. Hence, an NPS can be a functional analog; i.e., despite its structure not being very similar to that of the TRD, it still binds to the same receptors and facilitates the same functional effect. A lot of synthetic cannabinoids are structurally different from delta-9-tetrahydrocannabinol (THC), the psychoactive component of cannabis, and yet they bind both cannabinoid receptors 1 and 2, sometimes even with stronger affinity than THC. Because of their structural difference, NPS that are functional analogs evade detection by drug screening and legislative control (Banister and Connor, 2018a).

The initial impetus for producing and manufacturing NPS is to provide alternative recreational drugs while evading legislative measures and drug screening. Ultimately, most NPS become controlled (Banister and Connor, 2018b). Placing an NPS under schedule triggers clandestine laboratories to hop on other new targets to produce and distribute, thereby creating a vicious cycle of cat and mouse chase between clandestine laboratories and drug regulatory agencies. Not all scheduled NPS disappear from circulation. The synthetic cannabinoid XLR 11 was temporarily scheduled in the United States in July 2012 following its association with several cases of acute kidney injury in the Pacific Northwest (Murphy et al., 2013; Buser et al., 2014). Surveillance studies continued to detect it as late as 2015. In extreme cases, an NPS might transition to becoming a mainstream recreational drug despite being scheduled, as happened with 3,4-methylenedioxymethamphetamine (MDMA), the active ingredient in the party drug Ecstasy. It was originally developed by a pharmaceutical company in 1912 and became popular as a designer street drug in the 1980s (Bernschneider-Reif et al., 2006; DEA, 1988). Even after it was placed under Schedule I by the United States Drug Enforcement Administration (DEA) in 1985, it continued to be one of the most sought-after party drugs. Now it is considered a traditional recreational