Insights into the Pharmacology, Toxicology, and Clinical Applications of Hallucinogens

A special issue of Journal of Clinical Medicine (ISSN 2077-0383). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: closed (1 May 2022) | Viewed by 23010

Special Issue Editors


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Guest Editor
1. TOXRUN – Toxicology Research Unit, University Institute of Health Sciences, Advanced Polytechnic and University Cooperative (CESPU), CRL, 4585-116 Gandra, Portugal
2. Department of Public Health and Forensic Sciences, and Medical Education, Faculty of Medicine, University of Porto, 4200-319 Porto, Portugal
3. UCIBIO-REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
4. MTG Research and Development Lab, 4200-604 Porto, Portugal
Interests: real-world evidence; implementation science; toxicology; forensic sciences; psychoactive substances; drugs; biomedical research; scientometrics; scientific medical writing; pedagogical Innovation
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
1. IINFACTS - Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences, University Institute of Health Sciences (IUCS), CESPU, CRL, Gandra, Portugal
2. UCIBIO-REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Porto, Portugal
Interests: psychoactive substances; pharmacokinetics; pharmacodynamics; pharmacology; clinical, analytical and forensic toxicology; drug discovery

Special Issue Information

Dear Colleagues,

This Special Issue aims to cover, in a broad spectrum, the physicochemical characteristics, structure versus activity relationship, pharmacokinetics, pharmacodynamics, pharmacogenetics, psychological and physiological effects, and toxicity of hallucinogens to provide comprehensive and systematic knowledge on their biological risks and potential medicinal benefits. Special emphasis will be put on the toxicological perils associated with drug–drug pharmacokinetic interactions. Furthermore, the impact of interindividual pharmacogenetic variability on toxicity and therapeutic efficacy of hallucinogens, especially concerning polymorphisms in gene-encoding enzymes involved in metabolism (e.g., CYP450 isoforms) and/or in target receptors will be thoroughly scrutinized. The identification of additional metabolites, which may be pharmacologically/toxicologically active and responsible for enhanced therapeutic properties or toxicity, will be also highlighted, these being of further relevance as alternative biomarkers for drug exposure confirmation and treatment monitoring.

Prof. Dr. Ricardo Jorge Dinis-Oliveira
Prof. Dr. Diana Dias da Silva
Guest Editors

Manuscript Submission Information

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Keywords

  • Hallucinogens
  • Psilocybin
  • Psilocin
  • Therapeutic potential
  • Pharmacology
  • Toxicology
  • Pharmacogenomics

Published Papers (4 papers)

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Research

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17 pages, 2161 KiB  
Article
Rapid Targeted Method of Detecting Abused Piperazine Designer Drugs
by Anna Welz, Marcin Koba, Piotr Kośliński and Joanna Siódmiak
J. Clin. Med. 2021, 10(24), 5813; https://doi.org/10.3390/jcm10245813 - 12 Dec 2021
Cited by 3 | Viewed by 2527
Abstract
Piperazine derivatives belong to the popular psychostimulating compounds from the group of designer drugs. They are an alternative to illegal drugs such as ecstasy and amphetamines. They are being searched by consumers for recreational use due to their stimulating and hallucinogenic effects. Many [...] Read more.
Piperazine derivatives belong to the popular psychostimulating compounds from the group of designer drugs. They are an alternative to illegal drugs such as ecstasy and amphetamines. They are being searched by consumers for recreational use due to their stimulating and hallucinogenic effects. Many NPS-related poisonings and deaths have been reported where piperazines have been found. However, a major problem is the potential lack of laboratory confirmation of the involvement of piperazine derivatives in the occurrence of poisoning. Although many methods have been published, piperazine derivatives are not always included in a routine analytical approach or targeted toxicological analysis. There is an increasing need to provide qualitative evidence for the presence of piperazine derivatives and to ensure reproducible quantification. This article describes a new rapid method of detecting piperazine derivatives in biological material, using LC-MS. All target analytes were separated in a 15 min run time and identified based on the precursor ion, at least two product ions, and the retention time. Stable isotopically labeled (SIL) internal standards: BZP-D7, mCPP-D8 and TFMPP-D4 were used for analysis, obtaining the highest level of confidence in the results. The proposed detection method provides the analytical confirmation of poisoning with piperazine designer drugs. Full article
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Review

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23 pages, 1182 KiB  
Review
An Updated Review on the Psychoactive, Toxic and Anticancer Properties of Kava
by Rita B. Soares, Ricardo Jorge Dinis-Oliveira and Nuno G. Oliveira
J. Clin. Med. 2022, 11(14), 4039; https://doi.org/10.3390/jcm11144039 - 12 Jul 2022
Cited by 5 | Viewed by 5880
Abstract
Kava (Piper methysticum) has been widely consumed for many years in the South Pacific Islands and displays psychoactive properties, especially soothing and calming effects. This plant has been used in Western countries as a natural anxiolytic in recent decades. Kava has [...] Read more.
Kava (Piper methysticum) has been widely consumed for many years in the South Pacific Islands and displays psychoactive properties, especially soothing and calming effects. This plant has been used in Western countries as a natural anxiolytic in recent decades. Kava has also been used to treat symptoms associated with depression, menopause, insomnia, and convulsions, among others. Along with its putative beneficial health effects, kava has been associated with liver injury and other toxic effects, including skin toxicity in heavy consumers, possibly related to its metabolic profile or interference in the metabolism of other xenobiotics. Kava extracts and kavalactones generally displayed negative results in genetic toxicology assays although there is sufficient evidence for carcinogenicity in experimental animals, most likely through a non-genotoxic mode of action. Nevertheless, the chemotherapeutic/chemopreventive potential of kava against cancer has also been suggested. Both in vitro and in vivo studies have evaluated the effects of flavokavains, kavalactones and/or kava extracts in different cancer models, showing the induction of apoptosis, cell cycle arrest and other antiproliferative effects in several types of cancer, including breast, prostate, bladder, and lung. Overall, in this scoping review, several aspects of kava efficacy and safety are discussed and some pertinent issues related to kava consumption are identified. Full article
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19 pages, 1094 KiB  
Review
MDMA for the Treatment of Negative Symptoms in Schizophrenia
by Mitchell D. Arnovitz, Andrew J. Spitzberg, Ashkhan J. Davani, Nehal P. Vadhan, Julie Holland, John M. Kane and Timothy I. Michaels
J. Clin. Med. 2022, 11(12), 3255; https://doi.org/10.3390/jcm11123255 - 07 Jun 2022
Cited by 2 | Viewed by 9490
Abstract
The profound economic burden of schizophrenia is due, in part, to the negative symptoms of the disease, which can severely limit daily functioning. There is much debate in the field regarding their measurement and classification and there are no FDA-approved treatments for negative [...] Read more.
The profound economic burden of schizophrenia is due, in part, to the negative symptoms of the disease, which can severely limit daily functioning. There is much debate in the field regarding their measurement and classification and there are no FDA-approved treatments for negative symptoms despite an abundance of research. 3,4-Methylenedioxy methamphetamine (MDMA) is a schedule I substance that has emerged as a novel therapeutic given its ability to enhance social interactions, generate empathy, and induce a state of metaplasticity in the brain. This review provides a rationale for the use of MDMA in the treatment of negative symptoms by reviewing the literature on negative symptoms, their treatment, MDMA, and MDMA-assisted therapy. It reviews recent evidence that supports the safe and potentially effective use of MDMA to treat negative symptoms and concludes with considerations regarding safety and possible mechanisms of action. Full article
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21 pages, 856 KiB  
Review
Ayahuasca as a Decoction Applied to Human: Analytical Methods, Pharmacology and Potential Toxic Effects
by Ľuboš Nižnanský, Žofia Nižnanská, Roman Kuruc, Andrea Szórádová, Ján Šikuta and Anežka Zummerová
J. Clin. Med. 2022, 11(4), 1147; https://doi.org/10.3390/jcm11041147 - 21 Feb 2022
Cited by 8 | Viewed by 4062
Abstract
Ahyahuasca is a term commonly used to describe a decoction prepared by cooking the bark or crushed stems of the liana Banisteriopsis caapi (contains β-carbolines) alone or in combination with other plants, most commonly leaves of the shrub Psychotria viridis (contains N,N-dimethyltryptamine-DMT). [...] Read more.
Ahyahuasca is a term commonly used to describe a decoction prepared by cooking the bark or crushed stems of the liana Banisteriopsis caapi (contains β-carbolines) alone or in combination with other plants, most commonly leaves of the shrub Psychotria viridis (contains N,N-dimethyltryptamine-DMT). More than 100 different plants can serve as sources of β-carbolines and DMT, which are the active alkaloids of this decoction, and therefore it is important to know the most accurate composition of the decoction, especially when studying the pharmacology of this plant. The aim was to summarize the latest sensitive methods used in the analysis of the composition of the beverage itself and the analysis of various biological matrices. We compared pharmacokinetic parameters in all of the studies where decoction of ayahuasca was administered and where its composition was known, whereby minimal adverse effects were observed. The therapeutic benefit of this plant is still unclear in the scientific literature, and side effects occur probably on the basis of pre-existing psychiatric disorder. We also described toxicological risks and clinical benefits of ayahuasca intake, which meant that the concentrations of active alkaloids in the decoction or in the organism, often not determined in publications, were required for sufficient evaluation of its effect on the organism. We did not find any post-mortem study, in which the toxicological examination of biological materials together with the autopsy findings would suggest potential lethality of this plant. Full article
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