Etizolam Composition
Etizolam is a thienodiazepine derivative that contains a thiophene ring replacing the benzene ring found in traditional benzodiazepines, with a triazole ring fused to the diazepine ring structure. 1
Chemical Structure and Classification
- Etizolam belongs to the thienodiazepine class, which is structurally different from classic benzodiazepines but has similar pharmacological effects 2
- The molecular structure features a thiophene ring (instead of benzene) and a triazole ring fused to the diazepine ring 1
- Despite structural differences, etizolam has high affinity for the benzodiazepine site of GABAA receptors, similar to traditional benzodiazepines 2
Pharmaceutical Formulations
- Etizolam is typically available in tablet form at various dosages (commonly 0.25 mg, 0.5 mg, and 1 mg) 3, 4
- It can also be found in powder form or administered on blotter paper for oral absorption 1
- In clinical studies, etizolam has been administered at dosages of 0.25 mg to 0.5 mg twice daily for anxiety disorders 5, 3
Pharmacological Properties
- Etizolam has anxiolytic properties similar to classic benzodiazepines but may have selectivity for specific GABAA receptor subtypes (alpha1, beta2, gamma2) associated with anxiety 3
- It metabolizes into two major metabolites: α-hydroxyetizolam and 8-hydroxyetizolam, which can be detected in biological specimens 1
- Etizolam has a higher potency as an anxiolytic but lower lethality compared to diazepam 2
Regulatory Status
- Etizolam is approved for medical use in some countries including Japan, South Korea, and Italy 1
- In many other countries, it is classified as a controlled substance or new psychoactive substance (NPS) 2
- The World Health Organization (WHO) listed etizolam as a new psychoactive substance since 2015 4
Safety Considerations
- At therapeutic doses (0.25-1.0 mg), studies suggest minimal effects on psychomotor performance, vigilance, short-term memory, and decision-making speed 4
- Like other benzodiazepines, common side effects may include drowsiness and sedation 5
- Higher doses or recreational use can lead to dependence, intoxication, and potentially fatal outcomes, especially when combined with other substances 2
- The risk of respiratory depression increases when combined with other central nervous system depressants, similar to traditional benzodiazepines 6
Clinical Comparison to Other Benzodiazepines
- Etizolam has a similar mechanism of action to benzodiazepines like midazolam, acting on GABAA receptors 6, 1
- Like midazolam, flumazenil can potentially reverse the effects of etizolam in cases of overdose 6
- Unlike some traditional benzodiazepines, etizolam may have less impact on cognitive function at therapeutic doses 3