Abstract
Etizolam is an agonist at the GABA-A receptor and possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative, and skeletal muscle relaxant properties. The compound binds at the benzodiazepine binding site of the GABA-benzodiazepine receptor complex. Etizolam is licensed only in a few countries for the treatment of anxiety, panic, and insomnia. Also, there are only few clinical studies investigating clinically effects in the indications mentioned above. Regarding side effects, the risk of tolerance and dependency is comparable to other benzodiazepines. However, regarding the illicit non-prescribed use of etizolam, there are several reports on withdrawal, craving, and other related symptoms.
References
Altamura AC, Moliterno D, Paletta S, Maffini M, et al. Understanding the pharmacokinetics of anxiolytic drugs. Expert Opin Drug Metab Toxicol. 2013;9:423–40. https://doi.org/10.1517/17425255.2013.759209.
Araki K, Yasui-Furukori N, Fukasawa T, Aoshima T, et al. Inhibition of the metabolism of etizolam by itraconazole in humans: evidence for the involvement of CYP3A4 in etizolam metabolism. Eur J Clin Pharmacol. 2004;60:427–30. https://doi.org/10.1007/s00228-004-0789-1.
Bertolino A, Mastucci E, Porro V, Corfiati L, et al. Etizolam in the treatment of generalized anxiety disorder: a controlled clinical trial. J Int Med Res. 1989;17:455–60. https://doi.org/10.1177/030006058901700507.
Brunetti P, Giorgetti R, Tagliabracci A, Huestis MA, Busardò FP. Designer benzodiazepines: a review of toxicology and public health risks. Pharmaceuticals (Basel). 2021;14(6):560. https://doi.org/10.3390/ph14060560.
Casacchia M, Bolino F, Ecari U. Etizolam in the treatment of generalized anxiety disorder: a double-blind study versus placebo. Curr Med Res Opin. 1990;12:215–23. https://doi.org/10.1185/03007999009111650.
De Candia MP, Di Sciascio G, Durbano F, Mencacci C, et al. Effects of treatment with etizolam 0.5 mg BID on cognitive performance: a 3-week, multicenter, randomized, double-blind, placebo-controlled, two-treatment, three-period, noninferiority crossover study in patients with anxiety disorder. Clin Ther. 2009;31:2851–9. https://doi.org/10.1016/j.clinthera.2009.12.010.
Fracasso C, Confalonieri S, Garattini S, Caccia S. Single and multiple dose pharmacokinetics of etizolam in healthy subjects. Eur J Clin Pharmacol. 1991;40:181–5. https://doi.org/10.1007/BF00280074.
Fukasawa T, Yasui-Furukori N, Suzuki A, Inoue Y, et al. Pharmacokinetics and pharmacodynamics of etizolam are influenced by polymorphic CYP2C19 activity. Eur J Clin Pharmacol. 2005;61:791–5. https://doi.org/10.1007/s00228-005-0032-8.
Fukasawa T, Suzuki A, Otani K. Effects of genetic polymorphism of cytochrome P450 enzymes on the pharmacokinetics of benzodiazepines. J Clin Pharm Ther. 2007;32:333–41. https://doi.org/10.1111/j.1365-2710.2007.00829.x.
Gupta S, Garg B. A case of etizolam dependence. Indian J Pharmacol. 2014;46:655–6. https://doi.org/10.4103/0253-7613.144943.
Kondo S, Fukasawa T, Yasui-Furukori N, Aoshima T, et al. Induction of the metabolism of etizolam by carbamazepine in humans. Eur J Clin Pharmacol. 2005;61:185–8. https://doi.org/10.1007/s00228-005-0904-y.
Moosmann B, Auwärter V. Designer benzodiazepines: another class of new psychoactive substances. Handb Exp Pharmacol. 2018;252:383–410. https://doi.org/10.1007/164_2018_154.
National Records of Scotland. Drug-related deaths in Scotland in 2019. 2019. https://www.nrscotland.gov.uk/files//statistics/drug-related-deaths/2019/drug-related-deaths-19-pub.pdf
Nielsen S, McAuley A. Etizolam: a rapid review on pharmacology, non-medical use and harms. Drug Alcohol Rev. 2020;39:330–6. https://doi.org/10.1111/dar.13052.
Pariante F, Caddeo S, Ecari U. Etizolam in the treatment of generalized anxiety disorder associated with depressive symptoms. Curr Med Res Opin. 1989;11:543–9. https://doi.org/10.1185/03007998909112670.
Sanna E, Pau D, Tuveri F, Massa FC, et al. Molecular and neurochemical evaluation of the effects of etizolam on GABAA receptors under normal and stress conditions. Arzneimittelforschung. 1999;49:88–95.
Sanna E, Busonero F, Talani G, Mostallino MC, et al. Low tolerance and dependence liabilities of etizolam: molecular, functional, and pharmacological correlates. Eur J Pharmacol. 2005;519:31–42. https://doi.org/10.1016/j.ejphar.2005.06.047.
Savoldi F, Somenzini G, Ecari U. Etizolam versus placebo in the treatment of panic disorder with agoraphobia: a double-blind study. Curr Med Res Opin. 1990;12:185–90. https://doi.org/10.1185/03007999009111500.
Scottish Drug Forum. Etizolam information sheet. 2014. https://www.nhsaaa.net/media/4654/etizolam_infosheet_sdf_drugwatch1_1-2.pdf; https://www.nhsaaa.net/media/4654/etizolam_infosheet_sdf_drugwatch1_1-2.pdf
Suzuki Y, Kawashima Y, Shioiri T, Someya T. Effects of concomitant fluvoxamine on the plasma concentration of etizolam in Japanese psychiatric patients: wide interindividual variation in the drug interaction. Ther Drug Monit. 2004;26:638–42. https://doi.org/10.1097/00007691-200412000-00009.
Wakakura M, Tsubouchi T, Inouye J. Etizolam and benzodiazepine induced blepharospasm. J Neurol Neurosurg Psychiatry. 2004;75:506–7.
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Zwanzger, P. (2022). Tranquilizer/Anxiolytics: Benzodiazepines (Short-Acting) – Etizolam. In: Riederer, P., Laux, G., Nagatsu, T., Le, W., Riederer, C. (eds) NeuroPsychopharmacotherapy. Springer, Cham. https://doi.org/10.1007/978-3-319-56015-1_408-1
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