α-PVP is used by a variety of differentroutes of administration, includingoral,insufflation,injection,vaporization,sublingual, andrectal.[6] The dose range of α-PVP for therapeutic purposes was originally defined as 10 to 50mg, with a most-suitable dose of 20mg, whereas the recreational dose range is typically between 10 and 300mg.[6] The effects of α-PVP onset after 10minutes, peak after 10 to 40minutes, and last 2 to 3hours.[6]
The drug is much more potent thanamphetamine as an NDRI inin vitro, with 46-fold greater potency in terms of dopamine reuptake inhibition and 7-fold greater potency in terms of norepinephrine reuptake inhibition in HEK293 cells.[22] It is one of the most potent dopamine reuptake inhibitorsin vitro known.[17]
Theabsorption of α-PVP is very rapid.[6] In humans, the effects of the drugonset after 10minutes, peak between 10 and 40minutes, and last 2 to 3hours.[6]
α-PVP may be quantified in blood, plasma, or urine byliquid chromatography-mass spectrometry to confirm a diagnosis of poisoning in hospitalized patients or to provide evidence in a medicolegal death investigation. Blood or plasma α-PVP concentrations are expected to be in a range of 10–50 μg/L in persons using the drug recreationally, >100 μg/L in intoxicated patients, and >300 μg/L in victims of acute overdosage.[27][28]
α-PVP is banned in Estonia, Finland, France, Germany, Hungary, Russia, Ireland, Latvia, Lithuania, Netherlands, Poland, Romania, Slovenia, Sweden, the United Kingdom, Turkey, Norway,[18] as well as the Czech Republic.[29]
α-PVP is aSchedule 9 prohibited substance under thePoisons Standard (July 2016).[30] A Schedule 9 substance is a substance which may be abused or misused, the manufacture, possession, sale or use of which should be prohibited by law except when required for medical or scientific research, or for analytical, teaching or training purposes with approval of Commonwealth and/or State or Territory Health Authorities.[30] The drug was explicitly made illegal inNew South Wales after it was illegally marketed with the imprimatur of erroneous legal advice that it was not encompassed by analog provisions of the relevant act. It is encompassed by those provisions, and therefore has been illegal for many years in New South Wales. The legislative action followed the death of two individuals from using it; one jumping off a balcony, another having a heart attack after a state ofdelirium.[31][32]
On January 28, 2014, the U.S.Drug Enforcement Agency (DEA) listed α-PVP, along with nine other syntheticcathinones, as aSchedule I controlled substance with a temporary ban, effective February 27, 2014.[36] The temporary ban was then extended.[37]
α-PVP is sometimes the active ingredient in recreational drugs sold as "bath salts".[31] It may also be distinguished from "bath salts" and sold under a different name: "flakka," a name used in Florida, or "gravel" in other parts of the U.S. It is reportedly available as cheaply as US$5 per dose.[38] A laboratory for one county in Florida reported a steady rise in α-PVP detections in seized drugs from none in January–February 2014 to 84 in September 2014.[39]
^abcdefghijklmnoKolesnikova TO, Khatsko SL, Demin KA, Shevyrin VA, Kalueff AV (January 2019). "DARK Classics in Chemical Neuroscience: α-Pyrrolidinovalerophenone ("Flakka")".ACS Chem Neurosci.10 (1):168–174.doi:10.1021/acschemneuro.8b00525.PMID30384587.
^GB 927475, "α-Pyrrolidinovalerophenones", published May 29, 1963
^Sauer C, Peters FT, Haas C, Meyer MR, Fritschi G, Maurer HH (June 2009). "New designer drug alpha-pyrrolidinovalerophenone (PVP): studies on its metabolism and toxicological detection in rat urine using gas chromatographic/mass spectrometric techniques".Journal of Mass Spectrometry.44 (6):952–64.Bibcode:2009JMSp...44..952S.doi:10.1002/jms.1571.PMID19241365.
^Klavž J, Gorenjak M, Marinšek M (August 2016). "Suicide attempt with a mix of synthetic cannabinoids and synthetic cathinones: Case report of non-fatal intoxication with AB-CHMINACA, AB-FUBINACA, alpha-PHP, alpha-PVP and 4-CMC".Forensic Science International.265:121–4.doi:10.1016/j.forsciint.2016.01.018.PMID26890319.
^Sykutera M, Cychowska M, Bloch-Boguslawska E (May 2015). "A Fatal Case of Pentedrone and α-Pyrrolidinovalerophenone Poisoning".Journal of Analytical Toxicology.39 (4):324–9.doi:10.1093/jat/bkv011.PMID25737339.
^Zwartsen A, Verboven AH, van Kleef RG, Wijnolts FM, Westerink RH, Hondebrink L (December 2017). "Measuring inhibition of monoamine reuptake transporters by new psychoactive substances (NPS) in real-time using a high-throughput, fluorescence-based assay".Toxicol in Vitro.45 (Pt 1):60–71.Bibcode:2017ToxVi..45...60Z.doi:10.1016/j.tiv.2017.05.010.PMID28506818.
^Eiden C, Mathieu O, Cathala P, Debruyne D, Baccino E, Petit P, Peyriere H (November 2013). "Toxicity and death following recreational use of 2-pyrrolidino valerophenone".Clinical Toxicology.51 (9):899–903.doi:10.3109/15563650.2013.847187.PMID24111554.S2CID22826544.
^Baselt RC (2014).Disposition of toxic drugs and chemicals in man. Seal Beach, Ca.: Biomedical Publications. p. 1751.ISBN978-0-9626523-9-4.
^关于印发《非药用类麻醉药品和精神药品列管办法》的通知.China Food and Drug Administration (in Chinese). 27 September 2015. Archived fromthe original on 1 October 2015. Retrieved1 October 2015.
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