Drug Status Report

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Drug Status Report Drug: Fluperlapine Drug Name Status: Fluperlapine is the proper name (INN). Chemical Name: 3-Fluoro-6-(4-methyl-1-piperazinyl)morphanthridine Chemical structure: Molecular Formula: C19H20FN3 Pharmacological class / Application: Antipsychotic International status: US: The substance is not currently listed on the US Controlled Substances Act and is not mentioned on the DEA website. United Nations: The substance is not listed on the Yellow List - List of Narcotic Drugs under International Control nor the Green List - List of Psychotropic Substances under International Control. Canadian Status: Fluperlapine is a structural analog of the antipsychotic drug clozapine and was developed in the search for new antipsychotic drugs that would not cause agranulocytosis in the treatment of schizophrenia1. Clonazepin is excluded specifically from the heading “Benzodiazepines, their salts and derivatives, including”of item 18 of Schedule IV to the CDSA and listed as sub-item 32.1. While fluperlapine bears some structural similarity to the benzodiazepines, the substance belongs to a class of compounds known as the dibenzazepines2, which do not contain the essential structural elements of the benzodiazepines shown below: Characteristic structural features of benzodiazepines 1Lai, WG. et al. (1999) Bioactivation and covalent binding of hydroxyfluperlapine in human neutrophils: implications for fluperlapine-induced agranulocytosis, Drug Met. Disp. 28:255-263. 2Liegeois J-F F. et al. (1994) Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential nervous system agents: Synthesis and neurochemical study, J. Med. Chem 37:519-525.. 2 In addition, the substance is not a salt or derivative of a benzodiazepine and therefore is not included under the heading “Benzodiazepines, their salts and derivatives, including” of Item18 of Schedule IV to the CDSA. Recommendation: Fluperlapine is not included in the Schedules to the CDSA and is not a controlled substance. June 19th 2010.

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