Pentedrone

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Summary sheet: Pentedrone
Pentedrone
Pentedrone.svg
Chemical Nomenclature
Common names Pentedrone, Drone
Substitutive name Alpha-methylamino-valerophenone
Systematic name 2-(Methylamino)-1-phenylpentan-1-one
Class Membership
Psychoactive class Stimulant
Chemical class Cathinone
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.



Oral
Dosage
Threshold Common Heavy
2 - 5 - 10 - 15 - 25 mg
Light Strong
Threshold 2 - 5 mg
Light 5 - 10 mg
Common 10 - 15 mg
Strong 15 - 25 mg
Heavy 25 mg +
Duration
Total 2 - 6 hours
Onset 15 - 30 minutes
Peak 1 - 2 hours
Offset 1 - 2 hours
After effects 1 - 10 hours



Insufflated
Dosage
Threshold Common Heavy
1 - 2 - 5 - 10 - 20 mg
Light Strong
Threshold 1 - 2 mg
Light 2 - 5 mg
Common 5 - 10 mg
Strong 10 - 20 mg
Heavy 20 mg +
Duration
Total 1 - 4 hours
Onset 5 - 10 minutes
Peak 30 - 90 minutes
Offset 30 - 90 minutes
After effects 1 - 8 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.

Pentedrone (also known as drone) is a lesser-known novel stimulant substance of the cathinone class. Pentedrone belongs to a group of compounds known as substituted cathinones which are sold online as research chemicals. Pharmacologically, it is a norepinephrine-dopamine reuptake inhibitor (NDRI).[1]

Pentedrone was first detected being sold online in 2010 by the European Monitoring Centre for Drugs and Drug Addiction. It is an example of a contemporary designer drug specifically chosen to mimic and/or replace the functional and structural features of popular street drugs like cocaine, MDMA, or methamphetamine, which are sometimes imprecisely referred to as "bath salts".[2]

Pentedrone is known to come in the form of either a white powder or crystallized shards[citation needed] which users can ingest to produce a powerful, fast-acting but short-lived euphoric stimulant effects which are comparable to those of crack-cocaine, N-ethylpentedrone and a-PVP-type compounds, particularly when they are insufflated, vaporized or injected.[citation needed] Starting with the advent of MDPV, research chemical stimulants like pentedrone have gained notoriety for its tendency to induce compulsive redosing and addictive behaviors in a seemingly significant percentage of its users as well the ability to readily induce paranoid, delusional states and stimulant psychosis when misused or taken in excess.[citation needed]

Little research exists about both pentedrone particularly with regards to its toxicity, addiction and abuse potential in humans. Due to its novelty and brief history of human usage, all information related to the use of this compound should be treated with extreme caution. It is strongly recommended that one use harm reduction practices if choosing to use this substance.

Chemistry

Pentedrone is a a molecule of the substituted cathinone chemical class. Substituted cathinones refer to a class of molecules which are principally constituted of a phenethylamine core with an alkyl group attached to the alpha carbon and an oxygen group attached to the beta carbon. They are also known as the beta-ketone (double-bonded oxygen to the β-carbon) analogs of amphetamines. Pentedrone is the a-pentyl beta-keto analog of methamphetamine.

Of general note, the cathinone backbone can be modified in three different places to create hundreds of possible compounds, which include substituents on the aromatic ring, the alpha carbon, and the amine group.[3]

Pharmacology

Due to the lack of research regarding the substance, all proceeding discussion regarding the pharmacology of this compound derives from speculation based upon its structure and subjective effect similarities to other cathinones and related molecules, such as prolintane, a-PVP, a-PHP and analogs like N-ethyl-(nor)-pentedrone (i.e. NEP).

Unlike many other substituted cathinones, which display both reuptake-inhibition and releasing agent properties, pentedrone has been shown to act as a pure reuptake inhibitor for the major catecholamine neurotransmitters dopamine and norepinephrine, with very modest activity on serotonin. This renders its pharmacological activity similar to that of methylphenidate, cocaine or MDPV (although the latter two possess heavy additional serotonergic activity. These pure uptake inhibitors likely do not enter the intracellular space of the synapse via the transporter, which may be associated with less intracellular pharmacological effects and toxicity compared with substrate-type releasers[1]This enables the endogenous neurotransmitters dopamine and norepinephrine to accumulate within various synaptic regions in the brain, resulting in stimulating and euphoric effects.[citation needed]

Notably, the addition of an ethyl group to the terminal amine (-NH2) group of the pentedrone molecule seems to increase its potency significantly, as is observed with its successor analog N-ethyl-(nor)-pentedrone (i.e. NEP) which is viewed as having preferential recreational properties.

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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Cognitive effects
User.svg

After effects
Aftereffects (3).svg

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

Additional experience reports can be found here:

Toxicity and harm potential

The toxicity and long-term health effects of recreational pentedrone use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown. This is because pentedrone has a very short history of human usage. Early anecdotal evidence from people who have tried pentedrone within the community suggests 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 in a sparing and controlled fashion (but nothing can be completely guaranteed).

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 pentedrone can be considered moderately addictive with a high potential for abuse and seems to be readily liable 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 pentedrone 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 total absence of further consumption). Pentedrone presents cross-tolerance with all dopaminergic stimulants, meaning that after the consumption of pentedrone all stimulants will have a reduced effect.

Psychosis

Main article: Stimulant psychosis

Abuse of compounds within the stimulant class at high dosages for prolonged periods of time can potentially result in a stimulant psychosis that may present with a variety of symptoms (e.g., paranoia, hallucinations, or delusions).[4] A review on treatment for (dextro)amphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely.[5][6] The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.[7]

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.[8] Combinations with stimulants may further increase this risk.
  • MDMA - The neurotoxic effects of MDMA are generally believed to be increased when combined with amphetamine and other stimulants.
  • MAOIs - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, 2C-T-2, 2C-T-7, αMT, and some antidepressants.[9]
  • Cocaine - This combination may increase strain on the heart to dangerous levels.

Legality

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This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding it.

  • Brazil - Possession, production and sale is illegal as it is listed on Portaria SVS/MS nº 344.[10]
  • China - As of October 2015, pentedrone is a controlled substance in China.[11]
  • Czech Republic - Pentedrone is banned in the Czech Republic.[12]
  • Germany - Pentedrone is a Anlage II controlled drug in Germany.
  • United Kingdom - Pentedrone is a Class B drug in the United Kingdom as a result of the cathinone catch-all clause.[13]
  • United States - On January 28, 2014, the DEA listed it, along with 9 other synthetic cathinones, on the Schedule 1 with a temporary ban, effective February 27, 2014.[14]

See also

External links

Literature

  • Simmler, L. D., Rickli, A., Hoener, M. C., & Liechti, M. E. (2014). Neuropharmacology Monoamine transporter and receptor interaction profiles of a new series of designer cathinones. Neuropharmacology, 79, 152–160. https://doi.org/10.1016/j.neuropharm.2013.11.008
  • Hwang, J., Kim, J., Oh, J., Hong, S., Ma, S., Jung, Y., … Jang, C. (2014). The new stimulant designer compound pentedrone exhibits rewarding properties and affects dopaminergic activity, 117–128. https://doi.org/10.1111/adb.12299

References

  1. 1.0 1.1 Simmler, L. D., Rickli, A., Hoener, M. C., & Liechti, M. E. (2014). Monoamine transporter and receptor interaction profiles of a new series of designer cathinones. Neuropharmacology, 79, 152–160. https://doi.org/10.1016/j.neuropharm.2013.11.008
  2. http://www.emcdda.europa.eu/publications/annual-report/2010 | 2010 Annual report on the state of the drugs problem in Europe
  3. Liu, C., Jia, W., Li, T., Hua, Z., & Qian, Z. (n.d.). Identification and analytical characterization of nine synthetic cathinone derivatives Pentedrone, 4-Cl-pentedrone, 4-Cl--EAPP, propylone, N-ethylnorpentylone, 6-MeO-bk-MDMA, -PiHP, 4-Cl--PHP, and 4-F--PHP. https://doi.org/10.1002/dta.2136
  4. Treatment for amphetamine psychosis | [1]
  5. Treatment for amphetamine psychosis | [2]
  6. Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
  7. Treatment for amphetamine psychosis | [3]
  8. 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
  9. 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
  10. http://portal.anvisa.gov.br/documents/10181/3115436/%281%29RDC_130_2016_.pdf/fc7ea407-3ff5-4fc1-bcfe-2f37504d28b7
  11. "关于印发《非药用类麻醉药品和精神药品列管办法》的通知" (in Chinese). China Food and Drug Administration. 27 September 2015. Retrieved 1 October 2015. 
  12. "Látky, o které byl doplněn seznam č. 4 psychotropních látek (příloha č. 4 k nařízení vlády č. 463/2013 Sb.)" (PDF) (in Czech). Ministerstvo zdravotnictví. 
  13. 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
  14. "Temporary Placement of 10 Synthetic Cathinones into Schedule I". 28 January 2014.