Molecular and Neurochemical Evaluation of the Effects of Etizolam on GABAA Receptors under Normal and Stress Conditions

Sanna, Enrico; Pau, Davide; Tuveri, Francesca; Massa, Federico; Maciocco, Elisabetta; Acquas, C; Floris, C.; Fontana, Simona; Maira, G.; Biggio, Giovanni

doi:10.1055/s-0031-1300366

Cited by 8 publications

(8 citation statements)

References 13 publications

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“…Preclinical studies suggest that etizolam may have a lower ability to induce tolerance compared to benzodiazepines such as lorazepam . Etizolam is considered to possess mainly anxiolytic rather than sedative effects, which is thought to be due to a lower intrinsic activity at α1 subunit‐containing GABA A receptors when compared to diazepam and alprazolam . Etizolam has also been described to have some imipramine‐like effects in preclinical studies .…”

Section: Resultsmentioning

confidence: 99%

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Etizolam: A rapid review on pharmacology, non‐medical use and harms

Nielsen

McAuley

2020

Drug and Alcohol Review

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Issues. Etizolam is a thienodiazepine derivative, with high affinity for the benzodiazepine site of GABA A receptors. It is often referred to as a new (or novel) psychoactive substance, a 'designer' benzodiazepine or a 'street benzodiazepine'. Increasing reports of non-medical use, identification of etizolam as an ingredient in counterfeit medications and the common identification of etizolam in drug-related deaths, highlight the need for a greater understanding of etizolam. Approach. A rapid narrative review was conducted using PubMed and Google Scholar to synthesise what is known about etizolam to answer two research questions: (i) Does the pharmacological or toxicological profile of etizolam differ from other benzodiazepines?; and (ii) What is the nature and context of non-medical use and harms related to etizolam? Key Findings. Etizolam has a higher potency as an anxiolytic but lower lethality compared with diazepam. Few harms are documented with the therapeutic use of pharmaceutical products. Harms appear to be predominantly related to the use of etizolam in illicitly manufactured pills and occur almost exclusively in the context of mixed-drug toxicity. Conclusion. In therapeutic doses, there is little to suggest that etizolam is more harmful than other benzodiazepines. Most harms with etizolam appear to be related to the wide availability of illicitly manufactured pills, which are taken in unknown doses and combined with other substances. Current harm reduction advice, including avoiding combining opioids and benzodiazepines, remains relevant and increasingly important within an emerging culture of non-medical use. [Nielsen S, McAuley A. Etizolam: A rapid review on pharmacology, non-medical use and harms. Drug Alcohol Rev 2020;39: [330][331][332][333][334][335][336]

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Section: Resultsmentioning

confidence: 99%

“…Etizolam is a thienodiazepine derivative, with high affinity for the benzodiazepine site of GABA A receptors . It differs from classic benzodiazepines by having a benzene ring replaced with a thiophene ring.…”

Section: Introductionmentioning

confidence: 99%

Etizolam: A rapid review on pharmacology, non‐medical use and harms

Nielsen

McAuley

2020

Drug and Alcohol Review

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“…The highest concentrations of etizolam that have been reported in the literature in femoral blood are 270 22 and 300 ng/mL, 23 and in this study, the highest concentration was 172 ng/mL. It is possible that etizolam may even be safer than other benzodiazepines, as it possesses fewer sedative properties due to its lower intrinsic activity at GABA-A receptors containing an alpha-1 subunit, 7 the alpha-1 subunit being thought to result in the sedative effects of benzodiazepines. 24…”

Section: Resultsmentioning

confidence: 51%

“…5 Etizolam is mainly taken orally, but there have been reports of users smoking, insufflating, injecting and rectally administering etizolam. 6 As with other benzodiazepines, etizolam acts as a positive allosteric modulator of the γ-aminobutyric acid type A (GABA-A) receptor, 7 and is abused mainly for its anxiolytic effects and also for its ability to modulate intoxication and withdrawal of other substances such as heroin. 8 Benzodiazepines are commonly abused alongside other substances, with high levels of use in opioid abusers.…”

Section: Introductionmentioning

confidence: 99%

Femoral blood concentrations of the designer benzodiazepine etizolam in post-mortem cases

et al. 2020

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Etizolam is a thienodiazepine that although licensed for clinical usage in Japan, India and South Korea is commonly abused and detected in post-mortem cases around the world. To date, there are limited data in the literature to allow for the interpretation of blood concentrations of etizolam in post-mortem cases. A liquid chromatography with tandem mass spectrometry method was used to quantitate etizolam concentrations in 28 post-mortem cases where etizolam was detected. The median concentration of etizolam in femoral blood was 8.5 ng/mL (range 1.0–172.0 ng/mL; n = 24); in antemortem plasma, the etizolam concentration range was 4–44 ng/mL ( n = 4). The mean age of the individuals abusing etizolam was 38.5 ± 8.4 years (median 39 years), with the majority being male (86%). In all of the cases, multiple drugs were detected, with the most common being pregabalin (61%) followed by morphine/heroin (54%), diazepam (54%) and benzoylecgonine (21%), illustrating the increasing problem of poly-substance use in drug abusers. The cause of death in the cases in which etizolam was detected was multi-drug toxicity in 87.5% of the cases, with 12.5% unrelated to drug use (hangings and blunt-force trauma). These data will further help forensic practitioners with the interpretation of post-mortem etizolam concentrations.

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“…Any small wrinkles left in the membrane at this stage can be ignored, as they tend to disappear shortly after the preparation has been returned to the incubator and the membrane then forms a perfectly smooth Rings of internal diameter 28 mm and external diameter 33 mm are a useful size. Larger rings can be used, but freeing correspondingly greater areas of vitelline membrane from the yolk introduces extra technical difficulties 12,13 . The edge of the membrane can now be trimmed with scissors.…”

Section: Methodsmentioning

confidence: 99%

Untitled

2012

IJPSR

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There are various drugs used in daily life. Some of them show hazardous effect on various organs and some of them shows even lethal effect. Such drugs are required to banned. One of them is Etizolam (marketed under the brand name Sedekopan, Pasaden or Depas) is a drug which is a thiebenzothiodiazepines analog. The aim of this work is done to compare the effect of administration of the etizolam drug at (Zero-day) before incubation and at the (5-day) first week of incubation, to get an idea about the extent of the teratogenic effect of this drug on the development of chick embryo. So that morphological and biochemical studies were done on the chick embryo of 8-and 16-days old chick embryos treated with (0.5mg/ml egg) of etizolam on the (zero and 5-th days) of incubation. Etizolam caused abnormality in concentration dependent manner. Enlarged remains of primitive streak was seen at 0.1mg/ml and o.3mg/ml concentration of Etizolam embryo dies. Etizolam inhibit development of somites of the development of 5-day at of incubation also it does not allow the development of notochord. The toxic effects of the drug was seen also more at 16-days treated chick embryos and the drug induced death of chick embryo at both 8-and 16-days treated with 0.1mg/ml and o.3mg/ml. The conclusion from this study was the etizolam drug has dangerous effects on tissues and with powerful toxicity on the cells, because the drug absorbed rapidly with peak plasma levels achieved between 30 minutes and 2 hours and has a mean elimination half life of about 3 and a half hours.

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Molecular and Neurochemical Evaluation of the Effects of Etizolam on GABAA Receptors under Normal and Stress Conditions

Cited by 8 publications

References 13 publications

Etizolam: A rapid review on pharmacology, non‐medical use and harms

Etizolam: A rapid review on pharmacology, non‐medical use and harms

Femoral blood concentrations of the designer benzodiazepine etizolam in post-mortem cases

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