|Summary sheet: Pentedrone|
|Molecular structure of Pentedrone|
|Common names||Pentedrone, Drone|
|Routes of Administration|
Pentedrone (also known as Drone) is a synthetic stimulant substance of the substituted cathinone chemical class that produces typical cathinone-type stimulating and euphoric effects when administered. Its stimulant effects are believed to be caused by its activity as an NDRI (norepinephrine-dopamine reuptake inhibitor), with modest effects on serotonin reuptake.
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".
Pentedrone is known to come in the form of either a white powder or crystallized shards 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. 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.
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.
- 1 Chemistry
- 2 Pharmacology
- 3 Subjective effects
- 4 Toxicity and harm potential
- 5 Legality
- 6 See also
- 7 External links
- 8 Literature
- 9 References
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.
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 releasersThis enables the endogenous neurotransmitters dopamine and norepinephrine to accumulate within various synaptic regions in the brain, resulting in stimulating and euphoric effects.
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.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed 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 and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.
- Stimulation - In terms of its effects on the user's physical energy levels, pentedrone can be considered to be very stimulating and energetic.
- Spontaneous physical 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 a pleasant tingling sensation, which persists for a short period after administration before quickly falling off, which can lead users to redose more than they initially intended.
- Physical euphoria - This effect usually occurs at the peak of the experience, which can be short-lived compared to its total duration.
- 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 validated.
- Tactile enhancement
- Abnormal heartbeat
- Increased heart rate
- Increased blood pressure
- Increased perspiration
- Appetite suppression
- Focus enhancement
- Temporary erectile dysfunction
- 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.
- Thought acceleration
- Cognitive euphoria
- Immersion enhancement
- Motivation enhancement
- Increased music appreciation
- Ego inflation
- 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.
- Compulsive redosing
- Time distortion
- 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:
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.
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). A review on treatment for (dextro)amphetamine, and methamphetamine abuse-induced psychosis states that about 5–15% of users fail to recover completely. The same review asserts that, based upon at least one trial, antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis.
Although many psychoactive substances are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.
- 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.
- 25x-NBOMe - Both the NBOMe series and this compound induce powerful stimulation and their interaction may cause severe side effects. These can include thought loops, seizures, increased blood pressure, vasoconstriction, increased heart rate, and heart failure (in extreme cases).
- Alcohol - It is dangerous to combine alcohol, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of alcohol which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of alcohol will be significantly increased, leading to intensified disinhibition as well as respiratory depression. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM - This combination may cause increased heart rate and panic attacks.
- MXE - Increased heart rate and blood pressure may occur.
- Tramadol - This combination can increase the risk of seizures.
- 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.
- Cocaine - This combination may increase strain on the heart to dangerous levels.
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.
- China - As of October 2015, pentedrone is a controlled substance in China.
- Czech Republic - Pentedrone is banned in the Czech Republic.
- 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.
- 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.
- Responsible use
- Designer drug
- Psychoactive substance index
- Substituted cathinone
- N-Ethylpentedrone (NEP)
- 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
- 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
- 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
- Treatment for amphetamine psychosis | 
- Treatment for amphetamine psychosis | 
- 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 | 
- 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
- "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.