New psychoactive substances—Designer benzodiazepines

Abstract

Designer benzodiazepines are a rather new class of new psychoactive substances counting 26 compounds by the end of 2019. However, due to their high habit‐forming potential, the easy availability of these drugs in online shops is rather alarming. While the risk of acute health effects or intoxications after the sole consumption of benzodiazepines is low, combined consumption with other central nervous system depressant drugs such as opioids or alcohol can lead to life‐threating conditions. Furthermore, long term use can lead to tolerance and addiction. In this review article the emergence of this drug class is described and the literature on pharmacokinetics and the various methods of detection is discussed. Furthermore, the structure activity relationships of benzodiazepines are summarized in order to predict the potency of newly emerging compounds. This article is categorized under: Toxicology > New Psychoactive Substances

Designer Benzodiazepines: Effects, Toxicity, and Interactions

“…For DBZDs, most of the available molecules are already described in scientific and patent literature. 11,12 The history of BZD development helps us to understand these strategies. The basic structure of BZDs involves the fusion of a benzene and diazepine ring.…”

“…6 With dozens of licensed BZDs worldwide, NPS vendors started by offering compounds licensed in a few countries, but neither were scheduled in the targeted countries nor covered under the United Nations Convention on Psychotropic Substances of 1971. 11 Phenazepam and etizolam were the first DBZDs to be proposed on NPS vendors' web sites in Europe in 2006, whereas they were prescription BZDs in Russia and Japan. These 2 molecules mark the starting point of this phenomenon.…”

Changing trends in novel benzodiazepine use within Scottish prisons: detection, quantitation, prevalence, and modes of use

“…10 Novel benzodiazepines are used illicitly for a variety of reasons including self-medication for anxiety or sleeping disorders. 11 It is common for individuals to partake in polydrug use with novel benzodiazepines often consumed alongside opiates, alcohol, or other psychoactive substances either to enhance their effects; alleviate withdrawal symptoms; 3,6,12 or reduce insomnia due to the use of stimulants. 6,12,13 Unintentional polydrug use can also occur due to the long half-lives and slow metabolic clearance of some benzodiazepinetype drugs, and the use of multiple central nervous system (CNS) depressants can greatly increase the risk of overdose leading to respiratory depression and death.…”

“…It is assumed that their effects closely resemble those of prescription benzodiazepines, including sedation, amnesia, muscle relaxation, and anticonvulsive activity. 11 Novel benzodiazepines are reported anecdotally to vary greatly in their potency, onset times, and pharmacological half-lives making consistent dosing challenging for individuals and their effects unpredictable, especially when the individual drug present, the mass present per dosage unit, and the number of dosage units consumed may be inconsistent. 2,3 Problematic benzodiazepine use in prisons has been reported globally.…”

Cross reactivity of the CEDIA and HEIA benzodiazepine kits for 29 designer benzodiazepines and tofisopam

“…However, data on newly emerging compounds such as flualprazolam, phenazolam, and fluclotizolam are missing. Additionally, tofisopam (e.g., Grandaxin®), a 2,3‐benzodiazepine, is offered via the Internet due to its anxiolytic properties 11 . Given the structural differences of tofisopam with the primary targets of benzodiazepine immunoassays (mostly 1,4‐benzodiazepines), detection via such assays seems questionable.…”