Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects

As tranquilizers, benzodiazepines have a wide range of clinical uses. Recently, there has been a significant rise in the number of novel psychoactive substances, including designer benzodiazepines. Flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4<i>H</i>-[1,2,4]triazolo[4,3-a][1,4]ben...

Full description

Bibliographic Details
Main Authors: Amber N. Edinoff, Catherine A. Nix, Amira S. Odisho, Caroline P. Babin, Alyssa G. Derouen, Salim C. Lutfallah, Elyse M. Cornett, Kevin S. Murnane, Adam M. Kaye, Alan D. Kaye
Format: Article
Language:English
Published: MDPI AG 2022-08-01
Series:Neurology International
Subjects:
Online Access:https://www.mdpi.com/2035-8377/14/3/53
_version_ 1797484120669945856
author Amber N. Edinoff
Catherine A. Nix
Amira S. Odisho
Caroline P. Babin
Alyssa G. Derouen
Salim C. Lutfallah
Elyse M. Cornett
Kevin S. Murnane
Adam M. Kaye
Alan D. Kaye
author_facet Amber N. Edinoff
Catherine A. Nix
Amira S. Odisho
Caroline P. Babin
Alyssa G. Derouen
Salim C. Lutfallah
Elyse M. Cornett
Kevin S. Murnane
Adam M. Kaye
Alan D. Kaye
author_sort Amber N. Edinoff
collection DOAJ
description As tranquilizers, benzodiazepines have a wide range of clinical uses. Recently, there has been a significant rise in the number of novel psychoactive substances, including designer benzodiazepines. Flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4<i>H</i>-[1,2,4]triazolo[4,3-a][1,4]benzodiazeZpine) is a triazolo-analogue of flubromazepam. The most common effects noted by recreational users include heavy hypnosis and sedation, long-lasting amnesia, and rapid development of tolerance. Other effects included anxiolysis, muscle-relaxing effects, euphoria, loss of control, and severe withdrawals. Clonazolam, or 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-α]-[1,4]-benzodiazepine, is a triazolo-analog of clonazepam. It is reported to be over twice as potent as alprazolam. Deschloroetizolam (2-Ethyl-9-methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is part of the thienodiazepine drug class, which, like benzodiazepines, stimulates GABA-A receptors. Meclonazepam ((3S)-5-(2-chlorophenyl)-3-methyl-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one) is a designer benzodiazepine with additional anti-parasitic effects. Although it has proven to be an efficacious therapy for schistosomiasis, its sedative side effects have prevented it from being marketed as a therapeutic agent. The use of DBZs has been a subject of multiple recent clinical studies, likely related to increasing presence and availability on the internet drug market and lack of regulation. Many studies have aimed to identify the prevalence of DBZs and their effects on those using them. This review discussed these designer benzodiazepines and the dangers and adverse effects that the clinician should know.
first_indexed 2024-03-09T22:56:55Z
format Article
id doaj.art-3710db9aecf84b2698584a0b52b118ea
institution Directory Open Access Journal
issn 2035-8377
language English
last_indexed 2024-03-09T22:56:55Z
publishDate 2022-08-01
publisher MDPI AG
record_format Article
series Neurology International
spelling doaj.art-3710db9aecf84b2698584a0b52b118ea2023-11-23T18:08:35ZengMDPI AGNeurology International2035-83772022-08-0114364866310.3390/neurolint14030053Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse EffectsAmber N. Edinoff0Catherine A. Nix1Amira S. Odisho2Caroline P. Babin3Alyssa G. Derouen4Salim C. Lutfallah5Elyse M. Cornett6Kevin S. Murnane7Adam M. Kaye8Alan D. Kaye9Department of Psychiatry, Massachusetts General Hospital, Harvard School of Medicine, Boston, MA 02114, USADepartment of Psychiatry and Behavioral Medicine, Louisiana State University Health Shreveport, Shreveport, LA 71103, USADepartment of Psychiatry and Behavioral Medicine, Louisiana State University Health Shreveport, Shreveport, LA 71103, USASchool of Medicine, Louisiana State University Health Shreveport, Shreveport, LA 71103, USASchool of Medicine, Louisiana State University Health Shreveport, Shreveport, LA 71103, USASchool of Medicine, Louisiana State University New Orleans, New Orleans, LA 70112, USADepartment of Anesthesiology, Louisiana State University Shreveport, Shreveport, LA 71103, USADepartment of Psychiatry, Massachusetts General Hospital, Harvard School of Medicine, Boston, MA 02114, USAThomas J. Long School of Pharmacy and Health Sciences, Department of Pharmacy Practice, University of the Pacific, Stockton, CA 95211, USADepartment of Psychiatry and Behavioral Medicine, Louisiana State University Health Shreveport, Shreveport, LA 71103, USAAs tranquilizers, benzodiazepines have a wide range of clinical uses. Recently, there has been a significant rise in the number of novel psychoactive substances, including designer benzodiazepines. Flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4<i>H</i>-[1,2,4]triazolo[4,3-a][1,4]benzodiazeZpine) is a triazolo-analogue of flubromazepam. The most common effects noted by recreational users include heavy hypnosis and sedation, long-lasting amnesia, and rapid development of tolerance. Other effects included anxiolysis, muscle-relaxing effects, euphoria, loss of control, and severe withdrawals. Clonazolam, or 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-α]-[1,4]-benzodiazepine, is a triazolo-analog of clonazepam. It is reported to be over twice as potent as alprazolam. Deschloroetizolam (2-Ethyl-9-methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is part of the thienodiazepine drug class, which, like benzodiazepines, stimulates GABA-A receptors. Meclonazepam ((3S)-5-(2-chlorophenyl)-3-methyl-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one) is a designer benzodiazepine with additional anti-parasitic effects. Although it has proven to be an efficacious therapy for schistosomiasis, its sedative side effects have prevented it from being marketed as a therapeutic agent. The use of DBZs has been a subject of multiple recent clinical studies, likely related to increasing presence and availability on the internet drug market and lack of regulation. Many studies have aimed to identify the prevalence of DBZs and their effects on those using them. This review discussed these designer benzodiazepines and the dangers and adverse effects that the clinician should know.https://www.mdpi.com/2035-8377/14/3/53designer drugsbenzodiazepinesflubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4<i>H</i>-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine) clonazolamdeschloroetizolamwithdrawaladverse effects
spellingShingle Amber N. Edinoff
Catherine A. Nix
Amira S. Odisho
Caroline P. Babin
Alyssa G. Derouen
Salim C. Lutfallah
Elyse M. Cornett
Kevin S. Murnane
Adam M. Kaye
Alan D. Kaye
Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects
Neurology International
designer drugs
benzodiazepines
flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4<i>H</i>-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine) clonazolam
deschloroetizolam
withdrawal
adverse effects
title Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects
title_full Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects
title_fullStr Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects
title_full_unstemmed Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects
title_short Novel Designer Benzodiazepines: Comprehensive Review of Evolving Clinical and Adverse Effects
title_sort novel designer benzodiazepines comprehensive review of evolving clinical and adverse effects
topic designer drugs
benzodiazepines
flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4<i>H</i>-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine) clonazolam
deschloroetizolam
withdrawal
adverse effects
url https://www.mdpi.com/2035-8377/14/3/53
work_keys_str_mv AT ambernedinoff noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT catherineanix noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT amirasodisho noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT carolinepbabin noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT alyssagderouen noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT salimclutfallah noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT elysemcornett noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT kevinsmurnane noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT adammkaye noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects
AT alandkaye noveldesignerbenzodiazepinescomprehensivereviewofevolvingclinicalandadverseeffects