Chemistry:7-Aminoflunitrazepam
7-Aminoflunitrazepam is a benzodiazepine and a major metabolite of the drug flunitrazepam.[1]
Pharmacology
While it possesses the core benzodiazepine structure like its parent drug flunitrazepam, it is generally regarded as being inactive,[2] with an assay determining it to have an IC50 value of 15381.5 µM at GABAA receptors.[3] As a reference, its, more potent, parent drug flunitrazepam displaces diazepam binding with an IC50 quantified as 0.001700 µM.[4]
Pharmacokinetics
The presence of 7-aminoflunitrazepam can be detected for up to 4 weeks in urine.[5] Detection in oral fluid is also possible, but for considerably less time than in urine.[6]
Usage
Due to being relatively inactive and a metabolite of flunitrazepam, it is usually instead used as a biomarker to confirm flunitrazepam poisoning/intoxication.[7] Due to benzodiazepines, notably flunitrazepam, being frequently used as drugs to facilitate sexual assault, testing for the presence of flunitrazepam metabolites can be important steps in sexual assault investigations, where it is suspected that a drug has been used to facilitate the crime.[8][9][10]
References
- ↑ Feely, J.; Kavanagh, P. V.; McNamara, S. M. (1999). "The detection and quantitation of 7-aminoflunitrazepam, the major urinary metabolite of flunitrazepam, by gas chromatography/mass spectrometry". Irish Journal of Medical Science 168 (3): 189–192. doi:10.1007/BF02945851. PMID 10540786.
- ↑ Bylund, David B. (2017). "Flunitrazepam". Reference Module in Biomedical Sciences. doi:10.1016/B978-0-12-801238-3.98271-0. ISBN 978-0-12-801238-3.
- ↑ "AID 40995 - Binding affinity towards benzodiazepine/GABA A receptor. - PubChem". https://pubchem.ncbi.nlm.nih.gov/bioassay/40995.
- ↑ "AID 40826 - Inhibition of [3Hdiazepam binding to GABA-A benzodiazepine receptor of rat brain - PubChem"]. https://pubchem.ncbi.nlm.nih.gov/bioassay/40826.
- ↑ Verstraete, Alain G. (April 2004). "Detection times of drugs of abuse in blood, urine, and oral fluid". Therapeutic Drug Monitoring 26 (2): 200–205. doi:10.1097/00007691-200404000-00020. PMID 15228165.
- ↑ Samyn, Nele; De Boeck, Gert; Cirimele, Vincent; Verstraete, Alain; Kintz, Pascal (2002). "Detection of flunitrazepam and 7-aminoflunitrazepam in oral fluid after controlled administration of rohypnol". Journal of Analytical Toxicology 26 (4): 211–215. doi:10.1093/jat/26.4.211. PMID 12054361.
- ↑ "LOINC 105950-0 7-Aminoflunitrazepam [Presence in Urine by Confirmatory method"] (in en-US). https://loinc.org/105950-0.
- ↑ Negrusz, A.; Moore, C. M.; Hinkel, K. B.; Stockham, T. L.; Verma, M.; Strong, M. J.; Janicak, P. G. (September 2001). "Deposition of 7-aminoflunitrazepam and flunitrazepam in hair after a single dose of Rohypnol". Journal of Forensic Sciences 46 (5): 1143–1151. doi:10.1520/JFS15113J. PMID 11569557.
- ↑ Ohshima, T. (2006). "A case of drug-facilitated sexual assault by the use of flunitrazepam". Journal of Clinical Forensic Medicine 13 (1): 44–45. doi:10.1016/j.jcfm.2005.05.006. PMID 16087387.
- ↑ "Detection of "Date-Rape" Drugs in Hair and Urine, Final Report | National Institute of Justice" (in en). https://nij.ojp.gov/library/publications/detection-date-rape-drugs-hair-and-urine-final-report.
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