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4-Fluoroamphetamine (4-FA) Critical Review Report Agenda Item 5.4

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4-Fluoroamphetamine (4-FA) Critical Review Report Agenda Item 5.4 4-Fluoroamphetamine (4-FA) Critical Review Report Agenda item 5.4 Expert Committee on Drug Dependence Thirty-seventh Meeting Geneva, 16-20 November 2015 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine Page 2 of 35 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine Page 3 of 35 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine Contents Acknowledgements .......................................................................................................................... 6 Summary .......................................................................................................................................... 7 1. Substance identification ................................................................................................................ 8 A. International Nonproprietary Name (INN) .................................................................................... 8 B. Chemical Abstract Service (CAS) Registry Number ...................................................................... 8 C. Other Names .................................................................................................................................. 8 D. Trade Names .................................................................................................................................. 8 E. Street Names .................................................................................................................................. 8 F. Physical properties ........................................................................................................................ 8 G. WHO Review History ..................................................................................................................... 9 2. Chemistry ....................................................................................................................................... 9 A. Chemical Name .............................................................................................................................. 9 B. Chemical Structure ........................................................................................................................ 9 C. Stereoisomers ................................................................................................................................. 9 D. Synthesis ......................................................................................................................................... 9 E. Chemical description. .................................................................................................................. 10 F. Chemical properties ..................................................................................................................... 10 G. Chemical identification ................................................................................................................ 10 3. Ease of convertibility into controlled substances ....................................................................... 12 4. General pharmacology ................................................................................................................ 12 A. Pharmacodynamics ...................................................................................................................... 12 B. Routes of administration and dosage ........................................................................................... 17 C. Pharmacokinetics ......................................................................................................................... 17 5. Toxicology ................................................................................................................................... 17 6. Adverse reactions in humans ...................................................................................................... 18 7. Dependence potential .................................................................................................................. 20 A. Animal Studies .............................................................................................................................. 20 B. Human Studies ............................................................................................................................. 21 8. Abuse potential ............................................................................................................................ 21 A. Animal Studies .............................................................................................................................. 21 B. Human Studies ............................................................................................................................. 21 9. Therapeutic applications and extent of therapeutic use and epidemiology of medical use ...... 21 10. Listing on the WHO Model List of Essential Medicines ........................................................... 21 11. Marketing authorizations (as a medicinal product) ................................................................... 21 12. Industrial use ............................................................................................................................... 21 13. Non-medical use, abuse and dependence ................................................................................... 21 14. Nature and magnitude of public health problems related to misuse, abuse and dependence .. 22 Page 4 of 35 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine 15. Licit production, consumption and international trade ............................................................. 22 16. Illicit manufacture and traffic and related information ............................................................ 22 17. Current international controls and their impact ........................................................................ 24 18. Current and past national controls ............................................................................................. 24 19. Other medical and scientific matters relevant for a recommendation on the scheduling of the substance ..................................................................................................................................... 25 References ....................................................................................................................................... 26 Page 5 of 35 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine Acknowledgements This report has been drafted under the responsibility of the WHO Secretariat, Essential Medicines and Health Products, Policy Access and Use team. The WHO Secretariat would like to thank the following people for their contribution in producing this critical review report: Dr. Simon Brandt, United Kingdom (literature search, review and drafting), Dr. Michael H. Baumann, United States (helpful comments) and Dr. Stephanie Kershaw, Switzerland (editing). The WHO Secretariat would also like to thank the European Monitoring Centre for Drugs and Drug Addiction (EMCCDA) for providing data on 4-fluoroamphetamine collected through the European Union Early Warning System, which includes data provided by Reitox National Focal Points in the EU Member States, Turkey and Norway as well as the Europol National Units. Page 6 of 35 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine Summary 1-(4-Fluorophenyl)propan-2-amine (4-fluoroamphetamine, 4-FA) is a psychomotor stimulant that was first synthesized in the early 1940s. The European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) received the first formal notification of the detection of 4-FA in Europe in December 2008 although its presence has been noted since at least 2007. In Europe, it has been found in tablets sold as ‘ecstasy’/MDMA, paste or powder sold as amphetamine. In addition, it can be obtained from Internet retailers as a ‘research chemical’ and it has also been detected as an adulterant present in other illicit controlled substances. 4-FA appears to be most commonly administered orally or by nasal insufflation (snorting). The EMCDDA has been notified of seizures from various locations in Europe since 2008. Data indicate that 4-FA may be able to inhibit monoamine oxidase and that it functions as a substrate-type releasing agent of dopamine, norepinephrine and serotonin. It has been shown to display amphetamine-like features in vivo and in vitro and further research is warranted to investigate the extent to which 4-FA displays a potential for abuse and dependence in both animals in humans that is comparable to substances such as amphetamine, cocaine or related psychostimulants. Case report data in the scientific literature that unambiguously confirm a causal relationship between adverse effects of 4-FA and its presence in biofluids are limited to only a relatively small number of cases. In cases where this information is available, reported clinical features were associated with those of a sympathomimetic toxidrome. The EMCDDA has received reports from positive identifications in biofluids samples from 2009 onward. It has been reported that 4-FA might have established itself as a drug of choice in a surveyed convenience sample of 249 life-time users of 4-FA in one European country. Surveys that systematically assess the prevalence of use 4-FA within the general population are not available. Page 7 of 35 37th ECDD (2015) Agenda item 5.4 4-Fluoroamphetamine 1. Substance identification A. International Nonproprietary Name (INN)
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