Benzodiazepines: Uses, Dangers, and Clinical Considerations

Edinoff, Amber N.; Nix, Catherine A.; Hollier, Janice; Sagrera, Caroline E.; Delacroix, Blake M.; Abubakar, Tunde; Cornett, Elyse M.; Kaye, Adam M.; Kaye, Alan D.

doi:10.3390/neurolint13040059

Cited by 100 publications

(74 citation statements)

References 69 publications

(127 reference statements)

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“…A disadvantage of most current pharmacological and non-pharmacological treatment options is their rather slow onset of action, which usually takes several weeks until the occurrence of a clinically meaningful therapeutic effect [1]. Within the plethora of available antidepressants and anxiolytics, only benzodiazepines are fast acting anxiolytics already after acute treatment and have found their place even as emergency medication for many conditions [2,3]. However, their long-term use is hampered by side effects, such as tolerance development and abuse liability [2,3].…”

Section: Introductionmentioning

confidence: 99%

Translocator protein (18kDa) TSPO: a new diagnostic or therapeutic target for stress-related disorders?

et al. 2022

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Efficient treatment of stress-related disorders, such as depression, is still a major challenge. The onset of antidepressant drug action is generally quite slow, while the anxiolytic action of benzodiazepines is considerably faster. However, their long-term use is impaired by tolerance development, abuse liability and cognitive impairment. Benzodiazepines act as positive allosteric modulators of ɣ-aminobutyric acid type A (GABA A ) receptors. 3α-reduced neurosteroids such as allopregnanolone also are positive allosteric GABA A receptor modulators, however, through a site different from that targeted by benzodiazepines. Recently, the administration of neurosteroids such as brexanolone or zuranolone has been shown to rapidly ameliorate symptoms in post-partum depression or major depressive disorder. An attractive alternative to the administration of exogenous neurosteroids is promoting endogenous neurosteroidogenesis via the translocator protein 18k Da (TSPO). TSPO is a transmembrane protein located primarily in mitochondria, which mediates numerous biological functions, e.g., steroidogenesis and mitochondrial bioenergetics. TSPO ligands have been used in positron emission tomography (PET) studies as putative markers of microglia activation and neuroinflammation in stress-related disorders. Moreover, TSPO ligands have been shown to modulate neuroplasticity and to elicit antidepressant and anxiolytic therapeutic effects in animals and humans. As such, TSPO may open new avenues for understanding the pathophysiology of stress-related disorders and for the development of novel treatment options.

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Section: Introductionmentioning

confidence: 99%

Translocator protein (18kDa) TSPO: a new diagnostic or therapeutic target for stress-related disorders?

et al. 2022

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“…Prescription of temazepam became the most frequently given during pregnancy, and its acceptance rate increased over time. We assumed this trend might occur due to temazepam’s short half-life, no active metabolite, and no dose accumulated after repeated administration (Bellantuono et al 2019 ; Edinoff et al 2021 ).…”

Section: Discussionmentioning

confidence: 99%

Exposure to psychotropic drugs before and during pregnancy: what has changed over the last two decades?

Robiyanto

Schuiling-Veninga

Bos

et al. 2023

Arch Womens Ment Health

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Trends in prescribing psychotropic drugs before and during pregnancy may have changed over the years, but actual information is lacking. We therefore compared and assessed the exposure and acceptance rates of classes of antipsychotic (+ lithium), anxiolytic, sedative/hypnotic, antidepressant, and psychostimulant before and during pregnancy in the past two decades. All singleton pregnancies with ≥1 prescription of psychotropic drug from six months before pregnancy until child’s birthdate were identified in the pregnancy subset of the IADB.nl prescription database. The prescription patterns of psychotropics were distinguished as continuation rate (CR), initiation rate (IR), discontinuation rate (DR), total exposure rate (TER), and acceptance rate. Singleton pregnancies exposed to psychotropic drugs before and during pregnancy increased from 118.4 to 136.5 (per 1000 singleton pregnancies) between decades. Changing trends were observed in decade 2, including a high increase in the TER of antipsychotic class (3.3 to 6.8) and antidepressant class (23.0 to 40.6). A marked increase for individual drugs was seen for sertraline (TER: 0.6 to 6.6 and PAT: 35.3% to 82.5%), citalopram (TER: 2.3 to 10.0 and PAT: 51.1% to 74.6%), and quetiapine (TER: 0.4 to 3.1 and PAT: 57.1% to 66.0%). Although the total exposure rates of five classes of psychotropics in singleton pregnancies increased in decade 2, only antidepressant class had a higher acceptance rate during pregnancy. Certain SSRI antidepressants and atypical antipsychotics were more frequently prescribed in decade 2 than in decade 1, reflecting that treatment options were preferred for safer treatment choices.

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“…As tranquilizers, benzodiazepines have a wide range of clinical use, most commonly for treating insomnia (temazepam) [ 15 , 20 , 21 ] and panic disorder (alprazolam, lorazepam, or clonazepam) [ 15 , 20 , 22 , 23 , 24 , 25 ]. Benzodiazepines are the first choice of drug for treating status epilepticus [ 24 ], a neurologic emergency that requires prompt treatment [ 25 ].…”

Section: Introductionmentioning

confidence: 99%

“…Benzodiazepines are the first choice of drug for treating status epilepticus [ 24 ], a neurologic emergency that requires prompt treatment [ 25 ]. Long-acting benzodiazepines are used for treating alcohol withdrawal syndrome and associated seizures, administered immediately with a gradual reduction up to cessation [ 20 , 26 , 27 , 28 , 29 ]. Clobazam is approved for another epileptic syndrome known as Lennox–Gestaut Syndrome [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

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

Edinoff

Nix

Odisho

et al. 2022

Neurology International

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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-4H-[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.

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Benzodiazepines: Uses, Dangers, and Clinical Considerations

Cited by 100 publications

References 69 publications

Translocator protein (18kDa) TSPO: a new diagnostic or therapeutic target for stress-related disorders?

Translocator protein (18kDa) TSPO: a new diagnostic or therapeutic target for stress-related disorders?

Exposure to psychotropic drugs before and during pregnancy: what has changed over the last two decades?

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

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