A fluorine turns a medicinal benzodiazepine into NPS: the case of flualprazolam

Ntoupa, Panagoula-Stamatina A.; Papoutsis, Ioannis; Dona, Artemisia; Spiliopoulou, Chara; Athanaselis, Sotiris

doi:10.1007/s11419-020-00565-4

Cited by 14 publications

(7 citation statements)

References 20 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Flualprazolam is a fluorinated analogue of alprazolam, but there is little information in the literature regarding its specific pharmacological effects because it was never legitimately marketed. Based on its structural similarity to traditional benzodiazepines, alprazolam and triazolam, and user reports, flualprazolam most likely has similar CNS depressant effects ( 189 , 190 ). Flualprazolam was reported to be in circulation by the EMCDDA and DEA in 2018; as of the third quarter in 2020, flualprazolam was the most reported novel benzodiazepine in the USA.…”

Section: Nps Benzodiazepinesmentioning

confidence: 99%

Reports of Adverse Events Associated with Use of Novel Psychoactive Substances, 2017–2020: A Review

Mohr

Logan

Fogarty

et al. 2022

Journal of Analytical Toxicology

View full text Add to dashboard Cite

An important role of modern forensic and clinical toxicologists is to monitor the adverse events of novel psychoactive substances (NPS). Following a prior review from 2013-2016, this critical literature review analyzes and evaluates published case reports for NPS from January 2017 through December 2020. The primary objective of this study is to assist in the assessment and interpretation of these cases as well as provide references for confirmation methods. Chemistry, pharmacology, adverse events, and user profiles (e.g., polypharmacy) for NPS are provided including case history, clinical symptoms, autopsy findings, and analytical results. Literature reviews were performed in PubMed and Google Scholar for publications using search terms such as NPS specific names, general terms (e.g., “designer drugs,” “novel psychoactive substances”), drug classes (e.g., “designer stimulants,”), and outcome-based terms (e.g., “overdose,” “death”). Government and website drug surveillance databases and abstracts published by professional forensic science organizations were also searched. Toxicological data and detailed case information were extracted, tabulated, analyzed, and organized by drug category. Case reports included overdose fatalities (378 cases), clinical treatment and hospitalization (771 cases), and driving under the influence of drugs (170 cases) for a total of 1,319 cases providing details of adverse events associated with NPS. Confirmed adverse events with associated toxidromes of more than 60 NPS were reported to include synthetic cannabinoid, NPS stimulant, NPS hallucinogen, NPS benzodiazepine, and NPS opioid cases. Fifty of these NPS were reported for the first time in January 2017 through December 2020 as compared to the previous four years surveyed. This study provides insight and context of case findings described in the literature and in digital government surveillance databases and websites during a recent four-year period. This review will increase awareness of adverse events associated with NPS use to better characterize international emerging drug threats.

show abstract

Section: Nps Benzodiazepinesmentioning

confidence: 99%

Reports of Adverse Events Associated with Use of Novel Psychoactive Substances, 2017–2020: A Review

Mohr

Logan

Fogarty

et al. 2022

Journal of Analytical Toxicology

View full text Add to dashboard Cite

show abstract

“…An analysis of user reports has indicated that fluclotizolam is reported to be a potent benzodiazepine, with a dose of more than 0.75 mg reported as having a 'heavy effect' [47]. Flualprazolam has been reported in a number of DUID incidences, an 'anaesthesia robbery' case, as well as being detected post-mortem in a number of intoxications [48][49][50][51].…”

Section: Binding Affinitymentioning

confidence: 99%

The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines

et al. 2022

View full text Add to dashboard Cite

Purpose The number of benzodiazepines appearing as new psychoactive substances (NPS) is continually increasing. Information about the pharmacological parameters of these compounds is required to fully understand their potential effects and harms. One parameter that has yet to be described is the blood-to-plasma ratio. Knowledge of the pharmacodynamics of designer benzodiazepines is also important, and the use of quantitative structure–activity relationship (QSAR) modelling provides a fast and inexpensive method of predicting binding affinity to the GABAA receptor. Methods In this work, the blood-to-plasma ratios for six designer benzodiazepines (deschloroetizolam, diclazepam, etizolam, meclonazepam, phenazepam, and pyrazolam) were determined. A previously developed QSAR model was used to predict the binding affinity of nine designer benzodiazepines that have recently appeared. Results Blood-to-plasma values ranged from 0.57 for phenazepam to 1.18 to pyrazolam. Four designer benzodiazepines appearing since 2017 (fluclotizolam, difludiazepam, flualprazolam, and clobromazolam) had predicted binding affinities to the GABAA receptor that were greater than previously predicted binding affinities for other designer benzodiazepines. Conclusions This work highlights the diverse nature of the designer benzodiazepines and adds to our understanding of their pharmacology. The greater predicted binding affinities are a potential indication of the increasing potency of designer benzodiazepines appearing on the illicit drugs market.

show abstract

“…[11][12][13] It is also found in many hypnotics and psychiatric drugs. [14,15] The excess of it causes fluorosis and also responsible in disruption of immune system, acute gastric and kidney problems. [16,17] Besides industrial applications, cyanide is well known for its high toxicity as inhalation or consumption can cause health concern or even fatality.…”

Section: Introductionmentioning

confidence: 99%

“…Fluoride is often added to drinking water and toothpaste to maintain dental health and treatment of osteoporosis [11–13] . It is also found in many hypnotics and psychiatric drugs [14,15] . The excess of it causes fluorosis and also responsible in disruption of immune system, acute gastric and kidney problems [16,17] .…”

Section: Introductionmentioning

confidence: 99%

Development of Solution‐ and Film‐Based Economical Sensors for Reversible Sensing of Fluoride and Cyanide Ions

et al. 2022

View full text Add to dashboard Cite

Three Bisphenol based economical sensors were developed from readily available reagents with single synthetic step. The bisphenols were obtained from reaction of 2,6-dimethylphenol with 4-hydroxybenzaldehyde (BP-1), 4-bromobenzaldehyde (BP-2) and 4-nitrobenzaldehyde (BP-3). The cyanide and fluoride ions induce visual colour changes which enabled their naked eye detection and distinguished them as well. All the three sensors were able to detect these anions upto a nano molar range. Selective detection of these two anions with paper strips experiments were demonstrate by taking the BP-1 as representative case. Again, among the sensors BP-1 was chosen to immobilize into the cellulose based hydrogel matrix.Resulting composite efficiently detect cyanide and fluoride ions in 100 % aqueous system which otherwise was not feasible owing to water insolubility of BP-1. The 1 cm 2 film containing 0.01 mmol of BP-1 can absorb 2 ppm of fluoride ion from standard aqueous solution of KF. The morphology study reveals a smooth and miscible distribution of BP-1 into the polymer matrix. Surface morphology of the composite changes upon treatment with cyanide solution. Both the solution and film based sensing of these anions were found to be reversible in nature. The substituent effect on anion binding ability of respective sensors were demonstrated experimentally and validated theoretically.

show abstract

A fluorine turns a medicinal benzodiazepine into NPS: the case of flualprazolam

Cited by 14 publications

References 20 publications

Reports of Adverse Events Associated with Use of Novel Psychoactive Substances, 2017–2020: A Review

Reports of Adverse Events Associated with Use of Novel Psychoactive Substances, 2017–2020: A Review

The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines

Development of Solution‐ and Film‐Based Economical Sensors for Reversible Sensing of Fluoride and Cyanide Ions

Contact Info

Product

Resources

About