A-PVP

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Summary sheet: A-PVP
A-PVP
Α-PVP.svg
Chemical Nomenclature
Common names α-PVP, alpha-PVP, Flakka, O-2387, β-ketone-prolintane, Prolintanone
Substitutive name alpha-pyrrolidinovalerophenone
Systematic name (RS)-1-Phenyl-2-(1-pyrrolidinyl)-1-pentanone
Class Membership
Psychoactive class Stimulant
Chemical class Cathinone / Pyrrolidine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.


Smoked
Dosage
Threshold 1 - 2 mg
Light 2 - 5 mg
Common 5 - 15 mg
Strong 15 - 25 mg
Heavy 25 mg +
Duration
Total 30 - 60 minutes
Onset 20 - 60 seconds
Peak 3 - 6 minutes
Offset 15 - 30 minutes
After effects 1 - 3 hours
Oral
Dosage
Threshold 1 - 5 mg
Light 5 - 10 mg
Common 10 - 25 mg
Strong 25 - 40 mg
Heavy 40 mg +
Duration
Total 2 - 6 hours
Onset 2 - 20 minutes
Peak 1 - 2.5 hours
Offset 1 - 5 hours
After effects 4 - 12 hours



Insufflated
Dosage
Threshold 0.5 - 1 mg
Light 1 - 5 mg
Common 5 - 15 mg
Strong 15 - 25 mg
Heavy 25 mg +
Duration
Total 2 - 5 hours
Onset 10 - 30 minutes
Peak 20 - 45 minutes
Offset 30 - 90 minutes
After effects 2 - 4 hours






DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

alpha-Pyrrolidinovalerophenone (also known as α-PVP, A-PVP, alpha-PVP, and flakka) is a novel stimulant substance of the cathinone class. α-PVP is chemically related to prolintane and belongs to a group called the substituted cathinones, which includes compounds like MDPV, hexen, and a-PHP. It acts as a norepinephrine-dopamine reuptake inhibitor.

α-PVP was patented in the 1960s by Boehringer Ingelheim,[1] although it was never marketed. Reports of its use began to appear in the early 2010s. α-PVP has been subject to much scrutiny by the media as one of the ingredients found in "bath salts" or "legal highs" products.[citation needed] It has been mass produced in China and sold online as a research chemical.[citation needed] It has been linked to numerous hospitalizations and overdose deaths.[2]

User reports indicate that α-PVP produces powerful but short-lived stimulant effects comparable to those of methamphetamine and cocaine when insufflated or vaporized. Commonly reported effects include stimulation, disinhibition, increased libido, compulsive redosing, and euphoria. Like other synthetic cathinones, α-PVP is associated with compulsive use and addiction.

Very little data exists about the pharmacological properties, metabolism, and toxicity of a-PVP. Due to its potent psychostimulant effects and unknown toxicity profile, it is highly advised to use harm reduction practices if using with this substance.

Chemistry

α-PVP, or alpha-Pyrrolidinovalerophenone, is a synthetic substance belonging to a group called the substituted cathinones. Substituted cathinones are derivatives of the naturally occurring substance cathinone, which is one of the psychoactive principles in khat (Catha edullis). Cathinone is composed of a phenethylamine core with an alkyl group attached to the alpha carbon, and a ketone group attached to the beta carbon. α-PVP's structure consists of a cathinone core with a propyl group substituted at the alpha carbon, and a pyrrolidine ring at the amino group.

The hydrochloride salt of α-PVP is described as a white or off-white, odourless crystalline powder, with a melting point of 161.3°C. It is reported to be soluble in PBS (~10mg/ml, pH7.2), in EtOH (~20mg/ml), in DMSO (~10mg/ml) and in DMF (~3mg/ml).[2]

Pharmacology

α-PVP is a potent and selective norepinephrine-dopamine reuptake inhibitor (NDRI), with a similar potency as MDPV.[3] α-PVP does not act as a transporter substrate, i.e. it does not cause neurotransmitter release. It is a more potent inhibitor of DAT and NET than the classical stimulants cocaine and amphetamine.

Effects of MDPV, α-PVP, cocaine, and amphetamine on inhibition of [3H] transmitter uptake at dopamine (DAT), norepinephrine (NET) and serotonin (SERT) transporters[2]
Compound DAT (nM) NET (nM) SERT (nM) DAT/SERT ratio
a-PVP 12.8 ± 1.2 14.2 ± 1.2 >10,000 >781
MDPV 4.1 ± 0.6 25.9 ± 5.6 3305 ± 485 806
Cocaine 211 ± 19 292 ± 34 313 ± 17 1.5
Amphetamine 93 ± 17 67 ± 16 3418 ± 314 37

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Visual effects
Eye.svg

Cognitive effects
User.svg

After effects
Aftereffects (3).svg

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Toxicity and harm potential

The toxicity and long-term health effects of recreational α-PVP use do not appear to have been studied in any scientific context and the exact toxic dosage is unknown. This is because α-PVP has very little history of human usage.

Anecdotal reports suggest that there do not seem to be any negative health effects attributed to simply trying this substance at low to moderate doses by itself and using it sparingly (but nothing can be guaranteed).

α-PVP has been reported to be the cause, or a significant contributory cause, of death in suicides and overdoses caused by combinations of drugs.[4][5][6][7] α-PVP has also been linked to at least one death where it was combined with pentedrone and caused heart failure.[8]

It is strongly recommended that one use harm reduction practices when using this substance.

Tolerance and addiction potential

As with other stimulants, the chronic use of α-PVP can be considered highly addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal effects may occur if a person suddenly stops their usage.

Tolerance to many of the effects of α-PVP develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). α-PVP produces cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of α-PVP all stimulants will have a reduced effect.

Psychosis

Main article: Stimulant psychosis

α-PVP, like other stimulants, can result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[9][10] A review on treatment for amphetamine, dextroamphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[10][11] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[10]

Dangerous interactions

Although many psychoactive substances are safe to use on their own, they can become dangerous or even life-threatening when taken with other substances. The list below contains some potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses but still increase the possibility of injury of death. Independent research should always be conducted to ensure that a combination of two or more substances is safe before consumption.

  • 25x-NBOMe/25x-NBOH - Members of the 25x family are highly stimulating and physically straining. Combinations with stimulants should be avoided due to the risk of excessive stimulation. This can result in panic attacks, thought loops, seizures, increased blood pressure, vasoconstriction, and heart failure in extreme cases.
  • Alcohol - Alcohol can be dangerous to combine with stimulants due to the risk of accidental over-intoxication. Stimulants mask the sedative effects of alcohol, which is the main factor people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects of alcohol are left unopposed, which can result in blackouts and respiratory depression. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
  • DXM - Combinations with DXM should be strictly avoided due to DXM's effects on serotonin and dopamine reuptake. This can lead to panic attacks, hypertensive crisis, or serotonin syndrome.
  • MXE - Combinations with MXE may dangerously elevate blood pressure and increase the risk of psychosis.
  • Tramadol - Tramadol lowers the seizure threshold.[12] Combinations with stimulants may further increase this risk.
  • MDMA - The neurotoxic effects of MDMA may be increased when combined with other stimulants.
  • Cocaine - This combination may increase strain on the heart.

Serotonin syndrome risk

Combinations with the following substances can cause dangerously high serotonin levels. Serotonin syndrome requires immediate medical attention and can be fatal if left untreated.

Legal status

  • Australia: α-PVP made illegal in New 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.[citation needed]
  • Austria: α-PVP is illegal to possess, produce and sell under the NPSG (Neue-Psychoaktive-Substanzen-Gesetz Österreich).[citation needed]
  • Brazil: Possession, production and sale is illegal as it is listed on Portaria SVS/MS nº 344.[14]
  • China: As of October 2015, α-PVP is a controlled substance in China.[15]
  • Europe: α-PVP is banned in Estonia, Finland, France, Germany, Greece, Hungary, Ireland, Italy, Latvia, Lithuania, Poland, Romania, Slovenia, Sweden, United Kingdom, Turkey, Belgium,[16] and Norway,[17] as well as the Czech Republic.[18]
  • United Kingdom: α-PVP is a Class B drug in the United Kingdom as a result of the cathinone catch-all clause.[19]
  • United States: On January 28, 2014, the U.S. DEA listed α-PVP, along with 9 other synthetic cathinones, on the Schedule 1 with a temporary ban, effective February 27, 2014.[20]

See also

External links

Literature

References

  1. Wander, A. (1963), ‘α-Pyrrolidino valerophenones’, patent specification 9274
  2. 2.0 2.1 2.2 http://www.emcdda.europa.eu/system/files/publications/1814/TDAS15001ENN.pdf EMCDDA. (2015). EMCDDA–Europol Joint Report on a new psychoactive substance: 1‐phenyl‐2‐(1‐pyrrolidinyl)‐1‐pentanone (α‐PVP).
  3. Marusich, Julie A.; Antonazzo, Kateland R.; Wiley, Jenny L.; Blough, Bruce E.; Partilla, John S.; Baumann, Michael H. (2014). "Pharmacology of novel synthetic stimulants structurally related to the "bath salts" constituent 3,4-methylenedioxypyrovalerone (MDPV)". Neuropharmacology. 87: 206–213. doi:10.1016/j.neuropharm.2014.02.016. ISSN 0028-3908. 
  4. Analysis of synthetic cathinones commonly found in bath salts in human performance and postmortem toxicology: method development, drug distribution and interpretation of results (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/23361867
  5. http://www.aafs.org/sites/default/files/pdf/ProceedingsWashingtonDC2013.pdf
  6. Cheap, synthetic 'flakka' dethroning cocaine on Florida drug scene | http://news.yahoo.com/cheap-synthetic-flakka-dethroning-cocaine-florida-drug-scene-140910992.html
  7. 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 (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0379073816000372
  8. https://www.ncbi.nlm.nih.gov/pubmed/25737339
  9. http://www.drugabuse.gov/drugs-abuse/emerging-trends
  10. 10.0 10.1 10.2 Shoptaw, S. J., Kao, U., & Ling, W. (2009). Treatment for amphetamine psychosis. The Cochrane Library.
  11. Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
  12. Talaie, H., Panahandeh, R., Fayaznouri, M. R., Asadi, Z., & Abdollahi, M. (2009). Dose-independent occurrence of seizure with tramadol. Journal of Medical Toxicology, 5(2), 63-67. https://doi.org/10.1007/BF03161089
  13. Gillman, P. K. (2005). Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity. British Journal of Anaesthesia, 95(4), 434-441. https://doi.org/10.1093/bja/aei210
  14. http://portal.anvisa.gov.br/documents/10181/3115436/%281%29RDC_130_2016_.pdf/fc7ea407-3ff5-4fc1-bcfe-2f37504d28b7
  15. 关于印发《非药用类麻醉药品和精神药品列管办法》的通知 | http://www.sfda.gov.cn/WS01/CL0056/130753.html
  16. http://www.ejustice.just.fgov.be/cgi_loi/change_lg.pl?language=fr&la=N&cn=1998012251&table_name=wet
  17. http://www.emcdda.europa.eu/publications/joint-reports/alpha-pvp
  18. Látky, o které byl doplněn seznam č. 4 psychotropních látek (příloha č. 4 k nařízení vlády č. 463/2013 Sb.) | http://www.mzcr.cz/Admin/_upload/files/3/Nov%C3%A9%20PL.pdf
  19. United Kingdom. (2010). Misuse of Drugs Act 1971 (S.I. 2010/1207). London: The Stationery Office Limited. Retrieved February 9, 2018, from https://www.legislation.gov.uk/uksi/2010/1207/made
  20. http://www.deadiversion.usdoj.gov/fed_regs/rules/2014/fr0128.htm