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FURANYL FENTANYL Review Report Agenda Item 4.6

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FURANYL FENTANYL Review Report Agenda Item 4.6 FURANYL FENTANYL Review Report Agenda Item 4.6 Expert Committee on Drug Dependence Thirty-ninth Meeting Geneva, 6-10 November 2017 39th ECDD (2017) Agenda item 4.6 Furanyl fentanyl Page 2 of 16 39th ECDD (2017) Agenda item 4.6 Furanyl fentanyl Contents Acknowledgements.................................................................................................................................. 5 Summary...................................................................................................................................................... 6 1. Substance identification ....................................................................................................................... 7 A. International Nonproprietary Name (INN).......................................................................................................... 7 B. Chemical Abstract Service (CAS) Registry Number .......................................................................................... 7 C. Other Chemical Names ................................................................................................................................................... 7 D. Trade Names ....................................................................................................................................................................... 7 E. Street Names ....................................................................................................................................................................... 7 F. Physical Appearance ....................................................................................................................................................... 7 G. WHO Review History ....................................................................................................................................................... 7 2. Chemistry ................................................................................................................................................... 8 A. Chemical Name .................................................................................................................................................................. 8 B. Chemical Structure ........................................................................................................................................................... 8 C. Stereoisomers ...................................................................................................................................................................... 8 D. Methods and Ease of Illicit Manufacturing ........................................................................................................... 8 E. Chemical Properties ......................................................................................................................................................... 8 F. Identification and Analysis ........................................................................................................................................... 8 3. Ease of Convertibility Into Controlled Substances ........................................................................ 9 4. General Pharmacology .......................................................................................................................... 9 A. Routes of administration and dosage ...................................................................................................................... 9 B. Pharmacokinetics ............................................................................................................................................................. 9 C. Pharmacodynamics .......................................................................................................................................................... 9 5. Toxicology ................................................................................................................................................ 10 6. Adverse Reactions in Humans ........................................................................................................... 11 7. Dependence Potential .......................................................................................................................... 11 A. Animal Studies ................................................................................................................................................................. 11 B. Human Studies................................................................................................................................................................. 11 8. Abuse Potential ...................................................................................................................................... 11 A. Animal Studies ................................................................................................................................................................. 11 B. Human Studies................................................................................................................................................................. 11 9. Therapeutic Applications and Extent of Therapeutic Use and Epidemiology of Medical Use .............................................................................................................................................................. 11 10. Listing on the WHO Model List of Essential Medicines .............................................................. 12 11. Marketing Authorizations (as a Medicinal Product) ................................................................. 12 12. Industrial Use ......................................................................................................................................... 12 13. Non-Medical Use, Abuse and Dependence ..................................................................................... 12 Page 3 of 16 39th ECDD (2017) Agenda item 4.6 Furanyl fentanyl 14. Nature and Magnitude of Public Health Problems Related to Misuse, Abuse and Dependence ............................................................................................................................................. 12 15. Licit Production, Consumption and International Trade ......................................................... 13 16. Illicit Manufacture and Traffic and Related Information ........................................................ 13 17. Current International Controls and Their Impact ...................................................................... 13 18. Current and Past National Controls ................................................................................................ 13 19. Other Medical and Scientific Matters Relevant for a Recommendation on the Scheduling of the Substance ..................................................................................................................................... 13 References ................................................................................................................................................ 14 Annex 1: Report on WHO Questionnaire for Review of Psychoactive Substances for the 39th ECDD: Evaluation of Furanyl Fentanyl ................................................................................. 16 Page 4 of 16 39th ECDD (2017) Agenda item 4.6 Furanyl fentanyl Acknowledgements This report has been drafted under the responsibility of the WHO Secretariat, Department of Essential Medicines and Health Products, Teams of Innovation, Access and Use and Policy, Governance and Knowledge. The WHO Secretariat would like to thank the following people for their contribution in producing this review report: Dr. Katia Gysling, Chile (literature search, review and drafting), Dr. Dilkushi Poovendran, Geneva, Switzerland (questionnaire analysis and report drafting) and Dr. Stephanie Kershaw, Adelaide, Australia (review report editing, questionnaire analysis and report drafting). WHO would like to thank the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) for providing information on Furanyl Fentanyl from the European Union Early Warning System, which includes data reported by the Reitox National Focal Points in the EU Member States, Turkey, and Norway. Page 5 of 16 39th ECDD (2017) Agenda item 4.6 Furanyl fentanyl Summary Furanyl Fentanyl is a new designer opioid drug. It is a derivative of fentanyl with two distinctive characteristics: 1) higher liposolubility that allows its rapid absorption into general circulation 2) It binds to µ-opioid receptors with significant higher affinity than morphine. These characteristics give furanyl fentanyl a highly risky pharmacological profile. In the last several years there has been an increase in deaths due to the use of this designer opioid. Furthermore, it has been reported that it might be present in cocaine crack and other illicit drugs sold on the black market. Page 6 of 16 39th ECDD (2017) Agenda item 4.6 Furanyl fentanyl 1. Substance identification A. International Nonproprietary Name (INN) N/A B. Chemical Abstract Service (CAS) Registry Number 101345-66-8 furanyl fentanyl base 101365-56-4 furanyl fentanyl hydrochloride C. Other Chemical Names N-(1-phenethylpiperidin-4-yl)-N-phenylfuran-2-carboxamide N-phenyl-N-[1-(2-phenylethyl)-4-piperidinyl]-2-furancarboxamide N-phenyl-N-[1-(2-phenylethyl)piperidin-4-yl]furan-2-carboxamide 2-furanoylfentanyl, FU-F,
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