A-PVP

Not to be confused with A-PHP.
Summary sheet: A-PVP
A-PVP
Α-PVP.svg
Chemical Nomenclature
Common names α-PVP, alpha-PVP, Flakka, Flak, O-2387, β-ketone-prolintane, Prolintanone, Gravel
Substitutive name alpha-pyrrolidinovalerophenone
Systematic name (RS)-1-Phenyl-2-(1-pyrrolidinyl)-1-pentanone
Class Membership
Psychoactive class Stimulant
Chemical class Cathinone / Pyrrolidinophenone
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 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 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 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.

Interactions
Alcohol
MXE
Dissociatives
DXM
MDMA
Stimulants
25x-NBOMe
25x-NBOH
Tramadol
SNRIs
MAOIs
Serotonin releasers
SSRIs
5-HTP


alpha-Pyrrolidinovalerophenone (also known as α-PVP, A-PVP, alpha-PVP, and flakka) is a novel stimulant substance of the cathinone and pyrrolidinophenone classes. 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 to 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 IC50 (nM) NET IC50 (nM) SERT IC50 (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

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.


Physical effects
 

    • Stimulation - In terms of its effects on the user's physical energy levels, α-PVP can be considered to be extremely stimulating and energetic. This encourages activities such as running, climbing and dancing, although it can also encourage just sitting immobile engaged in repetitive tasks. The particular style of stimulation which α-PVP presents can be described as forced. This means that at higher dosages it becomes difficult or impossible to keep still as jaw clenching, involuntarily bodily shakes and vibrations become present, resulting in an extreme unsteadiness of the hands and a general loss of motor control.
    • Spontaneous bodily sensations - The "body high" of α-PVP can be described as a moderate to extreme euphoric tingling sensation that encompasses the entire body. It is capable of becoming overwhelming at higher dosages. This sensation maintains a consistent presence that steadily rises with the onset and hits its limit once the peak has been reached.
    • Tactile enhancement - α-PVP can enhance one's sense of touch to extreme degrees, often leading to states of sexual arousal.
    • Vibrating vision - α-PVP can cause the eyeballs to spontaneously wiggle back and forth in a rapid motion, causing vision to become blurry and temporarily out of focus. This condition is known as nystagmus.
    • Appetite suppression
    • Abnormal heartbeat - Due to the potency of its rush, α-PVP can cause various uncomfortable or painful sensations in the heart, especially when abused or used for extended periods. Those with genetic a family history of heart issues are discouraged from using this drug in its most potent methods of administration, if not avoid it entirely.
    • Increased blood pressure - α-PVP, especially when it is vaporized or injected, can lead to sudden spikes of blood pressure that may manifest in an extremely uncomfortable "exploding heart" sensation.
    • Increased heart rate
    • Dehydration - Dry mouth and dehydration are a universal experience with α-PVP and are a product of an increased heart rate, adrenergic activity and the motivation to engage in strenuous physical activities. While it is important to avoid becoming dehydrated, especially when out dancing in a hot environment, there is a potential possibility of suffering from water intoxication through over-drinking. Therefore it is advised that users simply sip at water and be mindful of their water in-take.
    • Dry mouth
    • Mouth numbing - In a similar fashion to that of cocaine, a-PVP numbs the areas of the body which it touches, these areas can include the nostrils, gums, mouth and urethra of the user.
    • Increased perspiration
    • Difficulty urinating - Higher doses of α-PVP result in an overall difficulty when it comes to urination, an effect that is temporary and typically harmless.
    • Headaches - This typically can occur towards the end of the experience, but can sometimes happen during one as well.
    • Muscle spasms
    • Restless legs
    • Vasoconstriction - α-PVP is reported to be very vasoconstricting at higher doses, and is on par with that of amphetamine and methamphetamine.[citation needed]
    • Teeth grinding - This component can be considered to be less intense when compared with that of MDMA, though becomes more present at high doses.
    • Seizure - α-PVP may lower the seizure threshold in some individuals, especially when it is abused.[citation needed]

Visual effects
 

Cognitive effects
 

  • The cognitive effects of α-PVP can be broken down into several components which progressively intensify proportional to dosage. The ample head space of α-PVP is described by many as one of extreme mental stimulation and a powerful rushing euphoria that dissipates quickly.
    • Anxiety & Paranoia - α-PVP can lead to states of extreme paranoia when abused or dosed too highly, which is why eyeballing this substance is strongly discouraged. The paranoia this compound produces shares many features of the paranoia that can be induced by methamphetamine or cocaine, and typically happens while during the come down.
    • Thought acceleration
    • Disinhibition
    • Cognitive euphoria - A euphoria very similar to amphetamine or cocaine is present as well as feelings of joy and happiness which are likely a direct result of marked norepinephrine and dopamine reuptake inhibition.
    • Immersion enhancement
    • Focus enhancement - α-PVP has been noted as enhancing focus, but in a way that leaves the user totally fixated on whatever task at hand, however trivial.
    • Ego inflation - Similar to the ego inflation of cocaine or methamphetamine, α-PVP can temporarily induce states of egomania at its peak.
    • Increased libido - Like its predecessors MDPV and pentedrone, α-PVP can induce states of extreme sexual arousal due to its powerful disinhibiting effects
    • Increased music appreciation
    • Analysis enhancement - Users report that this effect typically only occurs at low doses, and becomes increasingly more impairing as one increases their intake.
    • Motivation enhancement - This effect provides short-lived states of extreme motivation, but due to the cognitively narrowing aspects of its action, rarely ever translates into productive action.
    • Compulsive redosing - A high tendency to compulsive redose is a hallmark of this class of drug.
    • Feelings of impending doom - This typically is experienced when the substance is abused, but can happen at higher than needed doses, or the comedowns of binges. It can also happen spontaneously, although this tends to be rare.
    • Time distortion - Strong feelings of time compression are common within α-PVP and increase in the perception of perceived experience is greatly increased
    • Psychosis - This compound is known to readily induce psychosis if it is abused for prolonged periods of time.
    • Wakefulness

Auditory effects
 

After effects
 

Experience reports

There are currently 0 experience reports which describe the effects of this substance in our experience index. Additional experience reports can be found here:

Toxicity and harm potential

 

This toxicity and harm potential section is a stub.

As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it.
Note: Always conduct independent research and use harm reduction practices if using this substance.

Further information: Research chemicals § 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.

Dependence and abuse 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

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

  • 25x-NBOMe & 25x-NBOH - 25x compounds are highly stimulating and physically straining. Combinations with A-PVP should be strictly avoided due to the risk of excessive stimulation and heart strain. This can result in increased blood pressure, vasoconstriction, panic attacks, thought loops, seizures, and heart failure in extreme cases.
  • Alcohol - Combining alcohol with stimulants can be dangerous due to the risk of accidental over-intoxication. Stimulants mask alcohol's depressant effects, which is what most people use to assess their degree of intoxication. Once the stimulant wears off, the depressant effects will be left unopposed, which can result in blackouts and severe respiratory depression. If mixing, the user should strictly limit themselves to only drinking a certain amount of alcohol per hour.
  • DXM - Combinations with DXM should be avoided due to its inhibiting effects on serotonin and norepinephrine reuptake. There is an increased risk of panic attacks and hypertensive crisis, or serotonin syndrome with serotonin releasers (MDMA, methylone, mephedrone, etc.). Monitor blood pressure carefully and avoid strenuous physical activity.
  • MDMA - Any neurotoxic effects of MDMA are likely to be increased when other stimulants are present. There is also a risk of excessive blood pressure and heart strain (cardiotoxicity).
  • MXE - Some reports suggest combinations with MXE may dangerously increase blood pressure and increase the risk of mania and psychosis.
  • Dissociatives - Both classes carry a risk of delusions, mania and psychosis, and these risk may be multiplied when combined.
  • Stimulants - A-PVP may be dangerous to combine with other stimulants like cocaine as they can increase one's heart rate and blood pressure to dangerous levels.
  • Tramadol - Tramadol is known to lower the seizure threshold[12] and combinations with stimulants may further increase this risk.

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

In June 2016, the European Council decided that α-PVP shall be subjected by the Member States to control measures and criminal penalties by July 3, 2017.[14]

  • 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: Since June 26, 2019, α-PVP is illegal to possess, produce and sell under the SMG. (Suchtmittelgesetz Österreich)[15]
  • Belgium: α-PVP is a controlled substance.[16]
  • Brazil: Possession, production and sale is illegal as it is listed on Portaria SVS/MS nº 344.[17]
  • China: As of October 2015, α-PVP is a controlled substance in China.[18]
  • Cyprus: α-PVP is a controlled under the New Psychoactive Substances Legislation as of June 24, 2011.[2]
  • Czech Republic: α-PVP is a controlled substance.[19]
  • Estonia: α-PVP is listed in Regulation No. 73 as of June 2, 2014.[2]
  • Finland: α-PVP is listed in the Narcotics Act 373 as of December 30, 2013.[2]
  • France: α-PVP is a controlled substance as of August 2, 2012.[2]
  • Germany: α-PVP is controlled under Anlage II BtMG (Narcotics Act, Schedule II)[20] as of July 17, 2013.[21] It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.[22]
  • Greece: α-PVP is a controlled substance under law 3459/2006.[2]
  • Hungary: α-PVP is a Schedule A controlled substance.[2]
  • Ireland: α-PVP is a controlled substance as it is covered by the generic definition of controlled cathinones.[2]
  • Italy: α-PVP is a controlled substance as of December 29, 2011.[2]
  • Latvia: α-PVP is a controlled substance.[2]
  • Lithuania: α-PVP is a controlled substance since 2010.[2]
  • Norway: α-PVP is a controlled substance.[2]
  • Poland: α-PVP is a Schedule IV controlled substance as of July 1, 2015.[2]
  • Portugal: α-PVP is a controlled substance as of April 17, 2013.[2]
  • Romania: α-PVP is a controlled substance.[2]
  • Slovakia: α-PVP is a controlled substance as of October 1, 2013.[2]
  • Slovenia: α-PVP is a controlled substance since July 2014.[2]
  • Sweden: α-PVP is controlled under the Narcotic Drugs Control Act as of February 2013.[2]
  • Switzerland: α-PVP is a controlled substance specifically named under Verzeichnis D.[23]
  • Turkey: α-PVP is a controlled substance as of March 22, 2012.[2]
  • United Kingdom: α-PVP is a Class B drug in the United Kingdom as a result of the cathinone catch-all clause.[24]
  • 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.[25]

See also

External links

Literature

References

  1. ↑ Wander, A. (1963), ‘α-Pyrrolidino valerophenones’, patent specification 9274
  2. ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 2.11 2.12 2.13 2.14 2.15 2.16 2.17 2.18 2.19 2.20 "α-PVP: EMCDDA–Europol Joint Report on a new psychoactive substance: 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (α-PVP)" (PDF). European Monitoring Centre for Drugs and Drug Addiction. Retrieved December 25, 2019. 
  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. ↑ Marinetti, L. J., Antonides, H. M. (April 2013). "Analysis of synthetic cathinones commonly found in bath salts in human performance and postmortem toxicology: method development, drug distribution and interpretation of results". Journal of Analytical Toxicology. 37 (3): 135–146. doi:10.1093/jat/bks136. ISSN 1945-2403. 
  5. ↑ http://www.aafs.org/sites/default/files/pdf/ProceedingsWashingtonDC2013.pdf
  6. ↑ Cheap, synthetic “flakka” dethroning cocaine on Florida drug scene 
  7. ↑ Klavž, J., Gorenjak, M., Marinšek, M. (1 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: 121–124. doi:10.1016/j.forsciint.2016.01.018. ISSN 0379-0738. 
  8. ↑ Sykutera, M., Cychowska, M., Bloch-Boguslawska, E. (May 2015). "A Fatal Case of Pentedrone and α-Pyrrolidinovalerophenone Poisoning". Journal of Analytical Toxicology. 39 (4): 324–329. doi:10.1093/jat/bkv011. ISSN 1945-2403. 
  9. ↑ National Institute on Drug Abuse, Emerging Trends 
  10. ↑ 10.0 10.1 10.2 Shoptaw, S. J., Kao, U., Ling, W. W. (8 October 2008). "The Cochrane Database of Systematic Reviews (Complete Reviews)". In The Cochrane Collaboration. Treatment for amphetamine psychosis. John Wiley & Sons, Ltd. pp. CD003026.pub2. doi:10.1002/14651858.CD003026.pub2. 
  11. ↑ Hofmann, F. G. (1983). A handbook on drug and alcohol abuse: the biomedical aspects (2nd ed ed.). Oxford University Press. ISBN 9780195030563. 
  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. doi:10.1007/BF03161089. eISSN 1937-6995. ISSN 1556-9039. OCLC 163567183. 
  13. ↑ Gillman, P. K. (2005). "Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity". British Journal of Anaesthesia. 95 (4): 434–441. doi:10.1093/bja/aei210  . eISSN 1471-6771. ISSN 0007-0912. OCLC 01537271. PMID 16051647. 
  14. ↑ "Council Implementing (EU) 2016/1070". Official Journal of the European Union. Office for Official Publications of the European Communites (published July 2, 2016). June 27, 2016. pp. 18–20. OCLC 52224955. L 178. 
  15. ↑ https://www.ris.bka.gv.at/Dokumente/BgblAuth/BGBLA_2019_II_167/BGBLA_2019_II_167.pdfsig
  16. ↑ http://www.ejustice.just.fgov.be/cgi_loi/change_lg.pl?language=fr&la=N&cn=1998012251&table_name=wet
  17. ↑ http://portal.anvisa.gov.br/documents/10181/3115436/%281%29RDC_130_2016_.pdf/fc7ea407-3ff5-4fc1-bcfe-2f37504d28b7
  18. ↑ 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
  19. ↑ 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
  20. ↑ "Anlage II BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 18, 2019. 
  21. ↑ "Siebenundzwanzigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften" (in German). Bundesanzeiger Verlag. Retrieved December 18, 2019. 
  22. ↑ "§ 29 BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 18, 2019. 
  23. ↑ "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020. 
  24. ↑ The Misuse of Drugs Act 1971 (Amendment) Order 2010 
  25. ↑ http://www.deadiversion.usdoj.gov/fed_regs/rules/2014/fr0128.htm


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