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Developing Education and Treatment Protocols for Substance Use Disorders That Are Socially Responsible, Accountable, and Integrated
Published in Sahar Swidan, Matthew Bennett, Advanced Therapeutics in Pain Medicine, 2020
The DSM-5 recognizes substance-related disorders resulting from the use of ten separate classes of drugs: alcohol; caffeine; cannabis; hallucinogens (phencyclidine or similarly acting arylcyclohexylamines, and other hallucinogens, such as LSD); inhalants; opioids; sedatives, hypnotics, or anxiolytics; stimulants (including amphetamine-type substances, cocaine, and other stimulants); tobacco; and other or unknown substances. While some major groupings of psychoactive substances are specifically identified, the use of other or unknown substances can also form the basis of a substance-related or addictive disorder.
‘In and Out of the Hole’
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Ephenidine, also known as N-Ethyl-1,2-diphenylethanamine (NEDPA), appeared on the NPS scene in 2013, when it was marketed as a replacement for MXE after the UK ban. Its effects are described as ‘smooth’ compared to other dissociative anaesthetics (Beharry & Gibbons, 2016). At regular doses, ephenidine showed lower potential to induce ‘out-of-body’ experiences. Diphenidine and methoxyphenidine (MXP or 2-MXP) appeared on the market after the arylcyclohexylamine ban in 2013 and had not been used previously among designer drugs, although diphenidine synthesis was first reported in 1924. Diphenidine and 2-methoxyphenidine have both been reported to have long-lasting dissociative effects (Kang et al., 2017), but diphenidine was shown to be more potent and particularly linked to transient anterograde amnesia (Wallach et al., 2016). Methoxyphenidine effects vary and include tactile disconnections, loss of motor control, perception of body lightness, and long-lasting dissociative effects; users report subjective physical effects similar to those of dextromethorphan (DXM) (Wallach et al., 2016).
Anesthetic agents: Intravenous
Published in Hemanshu Prabhakar, Charu Mahajan, Indu Kapoor, Manual of Neuroanesthesia, 2017
Ketamine is a phencyclidine derivative and its chemical formulation is arylcyclohexylamine. It produces the state called “dissociated anesthesia,” which is characterized by the presence of dissociation between thalamocortical and limbic systems.30 It is an anesthetic state in which the eyes remain open with slow nystagmus. Independent skeletal muscle movement often occurs after the administration of this drug. It also provides intense analgesia as well as amnesia. Because of the possibility of increased airway secretions and emergence delirium, it is advised to give antisialagogue (glycopyrrolate) and midazolam as a premedication in patients receiving ketamine.
The Domino Effect: Ed Domino’s early studies of Psychoactive Drugs
Published in Journal of Psychoactive Drugs, 2018
Dr. Victor Maddox was a Parke-Davis medicinal chemist trying to synthesize a new analgesic. He began to react α-aminonitriles with the Grignard reagent Phenylmagnesium bromide. Unknown to him at the time, Maddox had caused a Bruylants reaction, resulting in a new molecule (1-(1-ethylcyclohexyl)piperidine) (Maddox 1981). This sparked his curiosity, and he then reacted 1-piperidinocyclohexanecarbonitrile(PCC) with the Grignard. On March 26, 1956, PCP was born (Maddox, Godefroi, and Parcell 1965). Maddox then submitted the compounds for testing to Parke-Davis pharmacologist Dr. Graham Chen. Using pigeons and cats, Chen noticed that low doses of PCP caused what he called “a state of catalepsy” (Chen 1965; Chen et al. 1959). About a week after first receiving the compound, Chen called Maddox and told him that PCP was the “most unique compound he had ever examined” (Domino 1980). Once the anesthetic potential of PCP was realized, Parke-Davis began a persistent pursuit into the properties of PCP and related arylcyclohexylamines.
Pro-psychotic effects of synthetic cannabinoids: interactions with central dopamine, serotonin, and glutamate systems
Published in Drug Metabolism Reviews, 2018
William E. Fantegrossi, Catheryn D. Wilson, Michael D. Berquist
Glutamate (Glu) is the major excitatory neurotransmitter, and it binds to both ionotropic and metabotropic receptors. Metabotropic Glu receptors (mGluR) have at least eight subtypes classified into three groups based on sequence homology, signal transduction, and pharmacology. Maksymetz et al. (2017) have recently reviewed current strategies to target mGluR to treat schizophrenia, but there is scant data on interactions between mGluRs and CB receptors, so further discussion of this is largely outside the scope of this review. However, there are three currently recognized ionotropic Glu receptors (α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), kainate, and N-methyl-d-aspartate (NMDA) receptors), and the NMDA receptors are most closely associated with neurological disorders, including schizophrenia and psychosis (Maeng and Zarate 2007). Importantly, administration of the non-competitive NMDA antagonist phencyclidine (PCP) to healthy human subjects reliably induces psychosis-like effects (Davies and Beech 1960; Cohen et al. 1962), as does the structurally related arylcyclohexylamine ketamine (Krystal et al. 1994; Malhotra et al. 1996). Accordingly, the remainder of this section will focus on interactions between CB1R and NMDA receptors.
Overdoses and deaths related to the use of ketamine and its analogues: a systematic review
Published in The American Journal of Drug and Alcohol Abuse, 2023
Tharcila V. Chaves, Bob Wilffert, Zila M. Sanchez
This article includes drugs from the same chemical group: arylcyclohexylamines. Phencyclidine or phenylcyclohexyl piperidine (PCP) is believed to be the first arylcyclohexylamine with recognized anaesthetic properties. Clinical studies on humans showed a tendency toward emergent delirium, which was often quite prolonged. It led to the discovery of ketamine, which has a shorter half-life, so the emergence phenomena are short lived and can be easily controlled. Several other drugs were designed based on PCP and ketamine. In this article, they are referred to as ketamine analogues (13–15).