Designer Benzodiazepines: A Review of Published Data and Public Health Significance

Greenblatt, H. Karl; Greenblatt, David J.

doi:10.1002/cpdd.667

Cited by 31 publications

(16 citation statements)

References 37 publications

(130 reference statements)

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“…They are usually ingested with other sedatives, primarily opioids, to potentiate their effects; promote ‘come down’ after stimulant use; or unintentionally, as counterfeits of prescription benzodiazepines [ 20 ]. Safety/toxicity profiles for most of the known DBZDs are not described yet, with limited knowledge of their pharmacodynamics and pharmacokinetics [ 15 , 25 , 26 ]. To date, the consumption of these new and unknown molecules is regarded as a serious threat to public health and society [ 20 , 27 , 28 ].…”

Section: Introductionmentioning

confidence: 99%

The Psychonauts’ Benzodiazepines; Quantitative Structure-Activity Relationship (QSAR) Analysis and Docking Prediction of Their Biological Activity

et al. 2021

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Designer benzodiazepines (DBZDs) represent a serious health concern and are increasingly reported in polydrug consumption-related fatalities. When new DBZDs are identified, very limited information is available on their pharmacodynamics. Here, computational models (i.e., quantitative structure-activity relationship/QSAR and Molecular Docking) were used to analyse DBZDs identified online by an automated web crawler (NPSfinder®) and to predict their possible activity/affinity on the gamma-aminobutyric acid A receptors (GABA-ARs). The computational software MOE was used to calculate 2D QSAR models, perform docking studies on crystallised GABA-A receptors (6HUO, 6HUP) and generate pharmacophore queries from the docking conformational results. 101 DBZDs were identified online by NPSfinder®. The validated QSAR model predicted high biological activity values for 41% of these DBDZs. These predictions were supported by the docking studies (good binding affinity) and the pharmacophore modelling confirmed the importance of the presence and location of hydrophobic and polar functions identified by QSAR. This study confirms once again the importance of web-based analysis in the assessment of drug scenarios (DBZDs), and how computational models could be used to acquire fast and reliable information on biological activity for index novel DBZDs, as preliminary data for further investigations.

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Section: Introductionmentioning

confidence: 99%

The Psychonauts’ Benzodiazepines; Quantitative Structure-Activity Relationship (QSAR) Analysis and Docking Prediction of Their Biological Activity

et al. 2021

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“…According to the literature data, clinical symptoms caused by taking designer benzodiazepines appear very quickly and are much more intense compared to classic medications. Despite the use of flumazenil with other medications, the resulting brain damage due to hypoxia contributed to the patient's death (73,102,103).…”

Section: Nps-related Fatalitiesmentioning

confidence: 99%

Pharmacotherapy of Patients Taking New Psychoactive Substances: A Systematic Review and Analysis of Case Reports

et al. 2021

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Background: In recent years, an increase in the frequency of hospitalizations of patients taking newer and newer psychoactive substances has been observed around the world. Each year, authors publish case reports of patients who consumed previously unknown NPS. Most publications of this type concern the period between 2014 and 2016. However, no publication systematically reviews the pharmacotherapy used in these cases. This study aims to review the case reports of patients taking NPS published between 2010 and 2019, as well as analyzing the pharmacotherapy used.Methods: We searched the Thomson (Web of Knowledge), PubMed/Medline, Science Direct, Scopus and Google Scholar databases. The search was performed using all possible combinations of the term “case report” describing the use of NPS, also referred to as designer medications, internet medications, research chemicals and herbal highs.Results: We analyzed 51 case reports on the intake of various types of NPS. Most of them (p < 0.001) concerned the use of synthetic cannabinoids (41.2%) and cathinones (31.4%). The pharmacotherapy applied primarily (p < 0.001) consisted of administering benzodiazepines to patients (62.7%), most of whom took only this group of medications (25.5%), followed by groups receiving benzodiazepines combined with neuroleptics (15.7%) and muscle relaxants (11.8%). Opioids were administered primarily to patients taking synthetic opioids (p < 0.001). Of the 5 cases of deaths from NPS reported in the literature, three relate specifically to the synthetic opioid MT-45. The later the time period, the more medications patients were administered (p = 0.02).Conclusion: In the pharmacotherapy for NPS poisoning, one should focus primarily on combating psychomotor agitation.

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“…“Novel Psychoactive Substances,” synonymous with “Designer Drugs,” generally describe psychotropic agents that are synthetic analogues, derivatives, or endogenous metabolic products of existing psychotropic drugs in clinical use . They may be manufactured illicitly—often outside the United States—for the purpose of bypassing regulatory requirements and law enforcement control.…”

Section: Binding Affinity Of Selected Fentanyl Analogues and Derivatimentioning

confidence: 99%

“…Designer drugs are of public health concern due to the risks of abuse, and the hazards of accidental or intentional overdosage. Cannabinoids, benzodiazepines, and opioids are among the psychotropic drug classes extensively represented in the designer drug realm . All pose a public health hazard, with designer opioids—in particular the >70 reported designer fentanyl derivatives—being of greatest contemporary concern …”

Section: Binding Affinity Of Selected Fentanyl Analogues and Derivatimentioning

confidence: 99%

Public Health Risk of Designer Psychotropic Drugs: Should PHASE Be Phased In?

Greenblatt

2019

Clin Pharma and Therapeutics

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Designer Benzodiazepines: A Review of Published Data and Public Health Significance

Cited by 31 publications

References 37 publications

The Psychonauts’ Benzodiazepines; Quantitative Structure-Activity Relationship (QSAR) Analysis and Docking Prediction of Their Biological Activity

The Psychonauts’ Benzodiazepines; Quantitative Structure-Activity Relationship (QSAR) Analysis and Docking Prediction of Their Biological Activity

Pharmacotherapy of Patients Taking New Psychoactive Substances: A Systematic Review and Analysis of Case Reports

Public Health Risk of Designer Psychotropic Drugs: Should PHASE Be Phased In?

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