
Pentedrone
Pentedrone | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Summary sheet: Pentedrone |
Pentedrone (also known as Drone) is an uncommon synthetic stimulant belonging to the substituted cathinone class. Its stimulant effects are believed to be caused by its activity as an NDRI (norepinephrine-dopamine reuptake inhibitor).
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 abused or taken in excess.[citation needed]
Pentedrone was first detected being sold on the research chemical market during 2010 by the European Monitoring Centre for Drugs and Drug Addiction (i.e. EMCDDA). 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".[1] Little research exists about both pentedrone particularly with regards to its toxicity, addiction and abuse potential. Due to its novelty and short history of human usage, all information related to the use of this compound should be treated with caution. It is strongly recommended that one use harm reduction practices when using this substance.
Chemistry

Pentedrone is a substituted cathinone. 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.[2]
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 releaser 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[3] 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
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
- Spontaneous tactile sensations - Much like related cathninones, it is commonly reported that medium to high doses of pentedrone can result in a pleasurable body high characterized by pleasant tingling.
- Stimulation - In terms of its effects on the user's physical energy levels, pentedrone can be considered to be extremely stimulating and energetic.
- Dehydration - Dry mouth and increased sweating can occur after consuming pentedrone.
- Vasoconstriction - A number of reports indicate that pentedrone can produce slight vasoconstriction, though this has yet to be scientifically documented.[citation needed]
- Tactile enhancement
- Increased heart rate[citation needed]
- Increased perspiration[citation needed]
- Appetite suppression
- Focus enhancement
- Temporary erectile dysfunction
- Increased blood pressure[citation needed]
- Teeth grinding - At common doses, this component has been reported considerably to less intense when compared with that of MDMA or other cathinones like a-PHP or NEP.
Cognitive effects
- Euphoria
- Thought acceleration
- Analysis enhancement - This effect is mostly present in lower doses and is considered weak compared to other stimulant compounds. At high doses, it becomes overshadowed by euphoric stimulation.
- Immersion enhancement
- Time distortion
- Ego inflation
- Disinhibition
- Motivation enhancement
- Compulsive redosing
- Increased music appreciation
After effects
The effects which occur during the offset of a stimulant experience generally feel negative and uncomfortable in comparison to the effects which occurred during its peak. This is often referred to as a "comedown" and occurs because of neurotransmitter depletion. Its effects commonly include:
- Anxiety
- Cognitive fatigue
- Depression
- Irritability
- Motivation suppression
- Thought deceleration
- Wakefulness
Experience reports
Anecdotal reports which describe the effects of this compound within our experience index include: {{#ask: [[Category:Pentedrone]|format=ul|Columns}} 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 drug.
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 [[Cross-tolerance::all dopaminergic stimulants]], meaning that after the consumption of Pentedrone all stimulants will have a reduced effect.
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
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.
- Stimulants - Pentedrone can be potentially dangerous in combination with other stimulants as it can increase one's heart rate and blood pressure to dangerous levels.
- "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] & "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 25x compounds are highly stimulating and physically straining. Combinations with Pentedrone 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.
- "[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 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.
- "[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 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.
- "[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - 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).
- "[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Some reports suggest combinations with MXE may dangerously increase blood pressure and increase the risk of mania and psychosis.
- "[[UncertainInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Both classes carry a risk of delusions, mania and psychosis, and these risk may be multiplied when combined.
- "[[UnsafeInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Pentedrone may be dangerous to combine with other stimulants like cocaine as they can increase one's heart rate and blood pressure to dangerous levels.
- "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - Tramadol is known to lower the seizure threshold[8] and 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.
- "[[DangerousInteraction" contains a listed "[" character as part of the property label and has therefore been classified as invalid.]] - This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, and some antidepressants.[9]
- Cocaine - This combination may increase strain on the heart to dangerous levels.
Legal issues
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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. |
- China - As of October 2015, pentedrone is a controlled substance in China.[10]
- Czech Republic - Pentedrone is banned in the Czech Republic.[11]
- Germany - Pentedrone is a Anlage II controlled drug in Germany.
- United Kingdom - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[12]
- 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.[13]
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
- ↑ http://www.emcdda.europa.eu/publications/annual-report/2010 | 2010 Annual report on the state of the drugs problem in Europe
- ↑ 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
- ↑ 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
- ↑ Treatment for amphetamine psychosis | [1]
- ↑ Treatment for amphetamine psychosis | [2]
- ↑ Hofmann FG (1983). A Handbook on Drug and Alcohol Abuse: The Biomedical Aspects (2nd ed.). New York: Oxford University Press. p. 329. ISBN 9780195030570.
- ↑ Treatment for amphetamine psychosis | [3]
- ↑ 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.
- ↑ 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.
- ↑ "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.
- ↑ "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.
- ↑ Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted
- ↑ "Temporary Placement of 10 Synthetic Cathinones into Schedule I". 28 January 2014.