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Assessment Form Date 8.1.2016 ANNEX 5 Register No 006122/06.08.04.01/2015 1. ------IND- 2016 0080 FIN EN- ------ 20160215 --- --- PROJET § 3(a) of the Narcotics Act (373/2008) SUBSTANCE Deschloroetizolam Deskloroetizolam 1. Name, synonyms, street name, CAS number IUPAC: 2-ethyl-9-methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine Other names: ETIZ-2, etizolam-2 Street names: Etiz-dechlorinate, Legal-Eti CAS: 40054-73-7 2. Molecular structure C17H16N4S Drug class: Benzodiazepines On the right, structure of etizolam (classified as a medicine) 3. Physical properties Physical state: The substance has been found as blue or pink tables and white powder ('6 mg buttons') Molecular weight: 308.40 g/mol Lääkealan turvallisuus- ja kehittämiskeskus | Säkerhets- och utvecklingscentret för läkemedelsområdet | Finnish Medicines Agency P.O. Box 55, 00034 FIMEA | Tel. 029 522 3341 Unique identifier 0921536-6 | [email protected] | www.fimea.fi | 2 (4) Assessment Form 4. Effects mechanism Structurally, deschloroetizolam is a benzodiazepine. It is an analogue of etizolam, which is classified as a medicine, in that it has one less chloroatom in its benzene ring structure. The pharmacological effect of benzodiazepine is based on the molecule binding to the gammaaminobutyric acid receptor (GABA) in the central nervous system. As a result of this binding, it will strengthen the effect of the GABA inhibitor. This will result in a nonspecific slowing down of the nerve paths, causing sedative, hypnotic, anxiolytic and anticonvulsant effects. The effect of benzodiazepine is targeted almost entirely at the central nervous system. On internet forums, the effect of deschloroetizolam has been described as similar to that of etizolam, albeit longer lasting; its effects have been described as lasting more than 8 hours. Thus it is comparable to medium-lasting benzodiazepines, such as alprazolam and oxazepram. 5. Manufacture The synthesis of deschloroetizolam has been described in a patent in 1988. 6. Effective dosage, abuse dosages According to internet forums, the abuse dose for beginners is 5-10 mg. Once tolerance has been built, the dosage can be up to ten times that amount. As is typical of the designer drug market place, even though designer benzodiazepines may be sold in pill form that might indicate their strength, these products do not have a marketing channel subject to supervision, and so there are no quality control requirements in place. Therefore, user reports do not provide a reliable account of the substance’s purity or strength. 7. Mixed use According to users' reports, diclazepam and other designer benzodiazepines are often used together with other sedatives or alcohol. 8. Health risks Health risks to the individual The known adverse effects of benzodiazepines include muscle weakness, motor skills impairment, nausea, memory impairment and sleepiness. The paralysing effect on the nervous system will increase if benzodiazepines are used together with alcohol other psychoactive drugs, such as sleep aids, sedatives or anti-psychotic drugs. The use of benzodiazepines will easily result in tolerance build-up, and long-term use may result in physical and psychological dependency on the substance. The dependency risk will grow along with dosage and use, and it will increase if the substance is used together with different benzodiazepines. Public health and social risks The public health and social risks of deschloroetizolam are comparable to at least the risks of other benzodiazepine use, such as the risks caused by loss of memory or fatigue at work or when driving. The development of tolerance and dependency and the resulting need to obtain more of the substance may, in the worst case, lead to criminal acts and the neglect of other obligations. 3 (4) Assessment Form 9. Connection with other criminality No data available 10. Documented observations on substance use Medical and industrial use There is no known medical or industrial use for deschloroetizolam. Reported appearance in Finland Deschloroetizolam has been discussed on internet forums during spring of 2015, also in Finnish, based on a comment dated 27.3.2015 stating that the substance is available in Finland. The substance has not been identified in confiscation databases of authorities. Reporting in the EU and the EMCDDA Early Warning System (EWS) Deschloroetizolam was first reported to the EWS system by the United Kingdom in September 2014 and after that, reports have been made by four countries, including in Scandinavia (Table 1). Table 1. Confiscations reported to the EMCDDA Country and date United Kingdom 01/09/2014 Sweden 08/09/2014 United Kingdom 18/12/2014 Germany 15/09/2015 Norway 24/09/2015 Norway 26/10/2015 Amount and form Official Other information blue tablet 0.07 g white powder Police light pink tablet 8.55 g blue tablets and 320 g pink tablets 102 blue tablets Police 74 blue tablets Police seizure Customs 11. Availability Deschloroetizolam can be ordered online. According to internet forums, deschloroetizolam was on the market in Finland in autumn of 2015, marked as 6 mg tablets (10 for €25, 20 for €40). 12. Usage profile Based on reports to the EMCDDA Early Warning System, national databases and scientific literature, the abuse of benzodiazepine derivatives has grown over the last few years. The abuse of these substances may be an attractive alternative to benzodiazepines subject to a prescription. Benzodiazepines are often used as a recreational drug together with other sedatives or alcohol. They have also been used to relieve the side effects of stimulant use. Based on reports from internet forums, users of designer benzodiazepine are often familiar with benzodiazepines. However, there are also instances of users who are unfamiliar with the drug. 4 (4) Assessment Form 13. Current status At this point, deschloroetizolam is not a controlled substance in Finland. In Russia, the substance was classified as a controlled substance in summer of 2015. 14. Other information With regard to their abuse, deschloroetizolam and other designer benzodiazepines are usually equivalent to benzodiazepines used for medicinal purposes. The effective duration of deschloroetizolam is comparable to those of benzodiazepines classified as medium-term narcotics. Benzodiazepines with a long-term effect, upon accumulation in the body, may affect driving ability or other motor or cognitive skills long after the last dose. There is no certainty regarding the quality of substances that are similar to medicinal substances but outside of the legal channels of production and distribution. Therefore there is no information on the purity of these substances and the products containing them, which makes their use more dangerous than the use of quality-controlled known medicines. 15. References 1. EMCDDA., European Monitoring Centre for Drugs and Drug Addiction, http://www.emcdda.europa.eu (password-protected file, viewed 15.12.2015) 2. Pubchem database. http://pubchem.ncbi.nlm.nih.gov/compound/827322#section=Top (viewed 15.12.2015) 3. Internet forums http://www.hollilla.com/reader.php?action=thread&thread=7041697&offset=60 (viewed 20.10.2015) https://tqn3fywqa5s2ojso.onion.cab/tori/res/233979.html (viewed 20.10.2015) https://www.flashback.org/t2378736 (viewed 20.10.2015) 4. Syvälahti E and Hietala J. Ahdistuneisuus- ja unihäiriöiden lääkeaineet [Medicines for anxiety and sleep disorders]. In book Koulu, Mervaala, Tuomisto (editor) Farmakologia ja toksikologia, Medicina, 2012. 5. Moriwaki M et al. Thieno-(triazolo)diazepine compound and medicinal application of the same. Patent. EP0315698A1. 6. Micromedex database; http://www.micromedexsolutions.com (viewed 10.12.2015) 7. Chemicals Register. Finnish Safety and Chemicals Agency (Tukes). (viewed 20.10.2015) 8. Internet shops https://www.brc-finechemicals.com/pellet-products/deschloroetizolam/6mg-deschloroetizolampellets.html (viewed 20.10.2015) 9. Forensic laboratory data, written communication, 31.8.2015 10. Forensic Medicine data, 7.12.2015 11. Customs laboratory data, written communication, 31.8.2015 12. Moosmann B, King LA, Auwärter V. Designer benzodiazepines: a new challenge. World Psychiatry. 2015;14:248 13. Förordning om kontroll av narkotika. Svensk författningssamling 1992:1554 http://www.riksdagen.se/sv/Dokument-Lagar/Lagar/Svenskforfattningssamling/Forordning19921554-om-kont_sfs-1992-1554/ (viewed 20.10.2015) 16. Alternatives to classification as an intoxicating substance and classification proposal resulting from evaluation Based on the reports obtained on the substance, the Finnish Medicines Agency recommends that the substance be added to Annex IV to Government Decree (543/2008) on substances, preparations and plants to be classified as narcotics.