Etizolam
[CAS# 40054-69-1]

Identification

• Classification: Analytical chemistry >> Standard >> Standard material
• Name: Etizolam
• Synonyms: 4-(2-Chlorophenyl)-2-ethyl-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine; AHR 3219; Depas; Y 7131
• Molecular Formula: C₁₇H₁₅ClN₄S
• Molecular Weight: 342.85
• CAS Registry Number: 40054-69-1
• EC Number: 662-368-4
• SMILES: CCC1=CC2=C(S1)N3C(=NN=C3CN=C2C4=CC=CC=C4Cl)C

Properties

• Density: 1.43
• Melting point: 147-148 ºC

Safety Data

• Hazard Symbols: GHS07;GHS08 Danger
• Hazard Statements: H315-H319-H360
• Precautionary Statements: P203-P264-P264+P265-P280-P302+P352-P305+P351+P338-P318-P321-P332+P317-P337+P317-P362+P364-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Skin irritation	Skin Irrit.	2	H315
Eye irritation	Eye Irrit.	2	H319
Reproductive toxicity	Repr.	1B	H360
Reproductive toxicity	Repr.	2	H361
Specific target organ toxicity - single exposure	STOT SE	3	H336
Reproductive toxicity	Lact.	-	H362

Discovory and Applicatios

Etizolam is a thienodiazepine derivative discovered in the 1980s by Japanese pharmaceutical researchers. It was developed as an alternative to traditional benzodiazepines, aiming to provide similar anxiolytic, sedative, and hypnotic effects with potentially fewer side effects and lower dependence risk. The discovery of Etizolam involved the modification of the benzodiazepine structure, incorporating a thiophene ring, which distinguished it from classical benzodiazepines and contributed to its unique pharmacological profile. Since its introduction, Etizolam has been utilized primarily in Japan, India, and Italy for treating anxiety disorders and insomnia.

Etizolam is primarily used in the medical field for its anxiolytic, sedative, and hypnotic properties. It is prescribed for treating anxiety, panic disorders, and insomnia. Etizolam's mechanism of action is similar to that of benzodiazepines, as it enhances the effect of gamma-aminobutyric acid (GABA) at the GABA-A receptor, leading to increased neuronal inhibition and a calming effect on the central nervous system. Patients benefit from its rapid onset of action and effectiveness in relieving symptoms of anxiety and sleep disturbances.

One of the significant advantages of Etizolam over traditional benzodiazepines is its lower risk of tolerance and dependence when used appropriately. Studies have shown that Etizolam has a reduced potential for abuse compared to conventional benzodiazepines, making it a safer option for long-term treatment of anxiety and insomnia. Additionally, Etizolam has muscle relaxant and anticonvulsant properties, which can be beneficial in certain clinical situations.

Etizolam has also found applications in research and development. Scientists study its pharmacological properties to develop new anxiolytic and hypnotic medications with improved safety profiles. Research into Etizolam's structure-activity relationship has provided valuable insights into designing thienodiazepine derivatives and understanding the mechanisms underlying their therapeutic effects. This research contributes to the broader field of psychopharmacology and aids in the development of innovative treatments for anxiety and sleep disorders.

Due to its psychoactive effects, Etizolam is regulated in many countries. While it is legally prescribed in some regions, it is classified as a controlled substance in others, reflecting concerns about potential misuse. Regulatory bodies monitor its distribution and usage to prevent abuse while ensuring it remains accessible for legitimate medical use. The regulatory landscape surrounding Etizolam underscores the need for careful management and ongoing evaluation of its risk-benefit profile.

Despite its medical benefits, Etizolam has seen non-medical use and recreational abuse. Users seeking its sedative and anxiolytic effects sometimes misuse it, leading to potential health risks, including dependence, withdrawal symptoms, and overdose. Public health efforts focus on educating about these risks and promoting safe, supervised use under medical guidance.

References

2024. A Pharmacovigilance Study on Psychotropic Agent-Induced Urinary Retention Using the Japanese Adverse Drug Event Report Database. Drugs - Real World Outcomes, 11(4).
DOI: 10.1007/s40801-024-00465-8

2024. Systematic review: The relationship between gabapentinoids, etizolam, and drug related deaths in Scotland. PLOS ONE, 19(10).
DOI: 10.1371/journal.pone.0310655

1987. An antagonistic activity of etizolam on platelet-activating factor (PAF). In vitro effects on platelet aggregation and PAF receptor binding. The Japanese Journal of Pharmacology, 44(4).
DOI: 10.1016/s0021-5198(19)43446-x