|Summary sheet: Pentedrone|
|Common names||Pentedrone, Drone|
|Routes of Administration|
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. Pentedrone acts as a norepinephrine-dopamine reuptake inhibitor (NDRI).
Pentedrone was first detected being sold online in 2010. It is an example of a contemporary designer drug specifically chosen to mimic and/or replace the effects of street drugs like cocaine, MDMA, or methamphetamine. Pentedrone and similar compounds are sometimes 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 abused.
Little data exists about the toxicity and abuse potential of pentedrone in humans. Due to its novelty and brief history of human usage, all information related to this compound should be treated with extreme caution. It is strongly recommended that one use harm reduction practices if using this substance.
Pentedrone is 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.
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 ☠.
- 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.
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.
- 25x-NBOMe & 25x-NBOH - 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.
- 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 - 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.
- Tramadol - Tramadol is known to lower the seizure threshold 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.
- MAOIs - 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.
- 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 controlled under Anlage II BtMG (Narcotics Act, Schedule II) as of July 17, 2013. It is illegal to manufacture, possess, import, export, buy, sell, procure or dispense it without a license.
- Switzerland: Pentedrone is a controlled substance specifically named under Verzeichnis D.
- United Kingdom: Pentedrone is a Class B drug in the United Kingdom as a result of the cathinone catch-all clause.
- 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.
- 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
- ↑ 1.0 1.1 Simmler, L. D., Rickli, A., Hoener, M. C., Liechti, M. E. (April 2014). "Monoamine transporter and receptor interaction profiles of a new series of designer cathinones". Neuropharmacology. 79: 152–160. doi:10.1016/j.neuropharm.2013.11.008. ISSN 0028-3908.
- ↑ 2010 Annual report on the state of the drugs problem in Europe
- ↑ Liu, C., Jia, W., Li, T., Hua, Z., Qian, Z. (August 2017). "Identification and analytical characterization of nine synthetic cathinone derivatives N -ethylhexedrone, 4-Cl-pentedrone, 4-Cl- α -EAPP, propylone, N -ethylnorpentylone, 6-MeO-bk-MDMA, α -PiHP, 4-Cl- α -PHP, and 4-F- α -PHP: Identification of nine synthetic cathinones". Drug Testing and Analysis. 9 (8): 1162–1171. doi:10.1002/dta.2136. ISSN 1942-7603.
- ↑ 4.0 4.1 4.2 Shoptaw, S. J., Kao, U., Ling, W. (21 January 2009). Cochrane Drugs and Alcohol Group, ed. "Treatment for amphetamine psychosis". Cochrane Database of Systematic Reviews. doi:10.1002/14651858.CD003026.pub3. ISSN 1465-1858.
- ↑ Hofmann, F. G. (1983). A handbook on drug and alcohol abuse: the biomedical aspects (2nd ed ed.). Oxford University Press. ISBN 9780195030563.
- ↑ 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.
- ↑ http://portal.anvisa.gov.br/documents/10181/3115436/%281%29RDC_130_2016_.pdf/fc7ea407-3ff5-4fc1-bcfe-2f37504d28b7
- ↑ "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.
- ↑ "Anlage II BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 18, 2019.
- ↑ "Siebenundzwanzigste Verordnung zur Änderung betäubungsmittelrechtlicher Vorschriften" (PDF) (in German). Bundesanzeiger Verlag. Retrieved December 18, 2019.
- ↑ "§ 29 BtMG" (in German). Bundesministerium der Justiz und für Verbraucherschutz. Retrieved December 18, 2019.
- ↑ "Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien" (in German). Bundeskanzlei [Federal Chancellery of Switzerland]. Retrieved January 1, 2020.
- ↑ The Misuse of Drugs Act 1971 (Amendment) Order 2010e
- ↑ "Temporary Placement of 10 Synthetic Cathinones into Schedule I". 28 January 2014.