Ana Gallegos

The pharmacology and toxicology of the synthetic cathinone mephedrone (4‐methylmethcathinone)

Mephedrone (4-methylmethcathinone) is a synthetic cathinone that is used as a recreational drug. It has been available since 2007 but its availability and use increased significantly during 2009 and 2010. In this review article we will summarize the available literature on the sources, availability, and prevalence of the use of mephedrone. We will also discuss the pharmacology of mephedrone, the patterns of acute toxicity associated with its use, the reports of fatalities associated with its use, and the potential for mephedrone dependence.

Khat use and monitoring drug use in Europe: the current situation and issues for the future.

AIM OF THE STUDY To review the information available on the use of khat (Catha edulis) in the EU, and to assess the future use of this drug and related substances. MATERIAL AND METHODS Khat is not controlled by international law and it has not been systematically included in the list of illicit drugs monitored in the EU. The current principal source of information on khat use in Europe is the early-warning system set up to monitor new and emerging drugs. Further information was obtained from official national reports to the EMCDDA and from the scientific literature. RESULTS Across Europe, the use of khat is low. Khat use is limited to countries with immigrant communities from countries where khat use is common (such as Ethiopia, Somalia and Kenya). Information on the prevalence of khat use in the general population is scarce. Data on seizures provide an insight on the situation, though these may be difficult to interpret. The most recent estimates suggest that Europe accounts for about 40% of the khat seized worldwide. CONCLUSION The shortage of data on the use and patterns of use of khat in Europe does not allow an evaluation of the needs for health and social interventions in communities in which the drug is used. But seizures of the plant are increasing in the EU, and more synthetic derivatives of the pharmacologically active ingredients of the plant (cathine and cathinone) are appearing on the market. Some of these, like mephedrone, have significant potential for future diffusion, and are likely to play a greater role on the European drug scene of the future.

Acryloylfentanyl, a recently emerged new psychoactive substance: a comprehensive review

N-(1-Phenethylpiperidin-4-yl)-N-phenylacrylamide, or acryloylfentanyl (acrylfentanyl), is a synthetic opioid and a close structural analogue of fentanyl, which is widely used in medicine as an adjunct to general anaesthesia during surgery and for pain management. Until recently, acryloylfentanyl was known only from the scientific literature, but in 2016 this non-controlled substance became available on the illicit drug market as a powder and nasal spray in Europe and the USA. By the end of 2016, detection of acryloylfentanyl in six European countries, including 47 deaths associated with the drug, had been reported to the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) through the European Union Early Warning System, which is a part of the system designed to identify and respond to the appearance of new psychoactive substances that may pose potential public health risks similar to drugs controlled under the United Nations drug control conventions. Herein we review what is known about this potent narcotic opioid. In addition to describing its chemical properties and the synthetic routes, analytical methodologies for the identification of the substance, as well as the limited information on the biological properties, including in vitro and in vivo pharmacological studies with the substance, are summarised. Analytically confirmed acute intoxications show that the signs and symptoms of acryloylfentanyl poisoning correspond to the opioid overdose triad of decreased consciousness, miosis and respiratory depression. Importantly, naloxone works as an antidote in life-threatening poisoning. The major human urinary metabolites identified in fatal overdose cases were nor-acryloylfentanyl, as well as mono- and dihydroxylated derivatives and their conjugates.

Monitoring Novel Psychoactive Substances: A Global Perspective

A globalised, networked world has led to novel psychoactive substances becoming widely available at an unprecedented pace. This development poses serious challenges to the current policies and procedures for detecting, identifying, monitoring and responding to their use. This chapter examines the key role that drug monitoring systems can play at the national, regional and international level in responding to this challenge. First we focus on the European Union early warning system on new psychoactive substances of the European Monitoring Centre for Drugs and Drug Addiction. In addition, national, regional and international drug monitoring systems are reviewed. The chapter also presents a number of the more promising new approaches that may be useful in monitoring novel substances in the face of a sophisticated, highly innovative and fast moving drug market. Finally, a review of findings from some of the first European studies on the prevalence of use of novel psychoactive substances is presented.

Computer-aided (in silico) approaches in the mode-of-action analysis and safety assessment of Ostarine and 4-methylamphetamine

This study exemplifies computer‐aided (in silico) approaches in assessing the risks of new psychoactive substances emerging in the European Union. In this work, we (i) consider the potential of Ostarine exhibiting psychoactivity and (ii) anticipate potential activities and toxicities of 4‐methylamphetamine.