Talk:Clobenzorex
Summary sheet: Clobenzorex |
Clobenzorex | |||||||||||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||||||||||
Common names | Clobenzorex, Greenies, Asenlix, Itravil, Finedal, Rexigen | ||||||||||||||||||||||||||||||||||
Substitutive name | N-(2-Chlorobenzyl)amphetamine | ||||||||||||||||||||||||||||||||||
Systematic name | (+)-N-[(2-Chlorophenyl)methyl]-α-methylbenzeneethanamine | ||||||||||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||||||||||
Psychoactive class | Stimulant | ||||||||||||||||||||||||||||||||||
Chemical class | Amphetamine | ||||||||||||||||||||||||||||||||||
Routes of Administration | |||||||||||||||||||||||||||||||||||
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Interactions | |||||||||||||||||||||||||||||||||||
Clobenzorex (Asenlix, Finedal, or Rexigen; or the US slang "greenies") is a stimulant substance of the amphetamine class. It is a N-alkyl amphetamine prodrug for d-amphetamine (dextroamphetamine) used as an anorectic (a medication that suppresses appetite) that is legally distributed in Mexico.[1] Like amphetamine, clobenzorex produces its effects by promoting the release of neurotransmitters dopamine and norepinephrine in the brain.
Subjective effects are essentially identical to that of lisdexamfetamine except with half the potency by weight and a slightly longer duration. These include stimulation (in a small percent of the population paradoxal sedation), focus enhancement, motivation enhancement, euphoria, and in a smaller population . Likewise, clobenzorex was designed exclusively for oral administration. This means that insufflation, smoking or injection do not provide faster absorption or onset. It has been used by US baseball players to reduce fatigue, increase attention and improve reaction times during athletic activities.
Despite the (?), many users report that clobenzorex is capable of producing dependence and addiction like other euphoric stimulants, particularly when it is taken above the recommended dosage. As a result, it is highly advised to use harm reduction practices if using this substance.
History and culture
This History and culture section is a stub. As a result, it may contain incomplete or wrong information. You can help by expanding it. |
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Chemistry
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Pharmacology
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Pharmacokinetics
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Pharmacodynamics
Amphetamine is a full agonist of the trace amine-associated receptor 1 (TAAR1), which is a key regulator of common and trace brain monoamines such as dopamine, serotonin and noradrenaline.[2][3][4] The agonism of this set of receptors results in the release of increased concentrations of dopamine, serotonin and noradrenaline in the synaptic cleft. This leads to cognitive and physical stimulation within the user.
d-amphetamine's affinity for the TAAR1 receptor is twice that of l-amphetamine.[5] As a result, d-amphetamine produces three to four times as much central nervous system (CNS) stimulation as l-amphetamine. l-amphetamine, on the other hand, has stronger cardiovascular and peripheral effects.
Conversion rate
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Subjective effects
While the subjective effects are almost identical to that of amphetamine, clobenzorex is significantly in its duration and more consistent in its intensity due to the slow release metabolism to d-amphetamine. Unlike lisdexamfetamine, this drug is not rate-limited in its metabolism[6].
Peripheral effects (such as increased heart rate and higher body temperature) are reported to be less prominent than formulations that partly contain l-amphetamine, such as Adderall or the racemic amphetamine sulphate sold illicitly.
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
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- Stimulation - Clobenzorex is reported to be very energetic and stimulating in a manner similar to lisdexamfetamine. It can encourage physical activities such as dancing, socializing, running, or cleaning. The particular style of stimulation which clobenzorex produces can be described as forced. This means that, at higher dosages, it becomes difficult or impossible to keep still as jaw clenching, involuntary bodily shakes and vibrations become present, resulting in extreme shaking of the entire body, unsteadiness of the hands, and a general loss of fine motor control. This effect is replaced with mild fatigue and general exhaustion during the offset of the experience.
- Spontaneous bodily sensations - The "body high" of clobenzorex can be described as a moderate euphoric tingling sensation that encompasses the entire body. This sensation maintains a consistent presence that steadily rises with the onset and hits its limit once the peak has been reached.
- Abnormal heartbeat
- Increased heart rate
- Increased blood pressure
- Appetite suppression - This effect is more pronounced compared to amphetamine, sometimes causing people to not eat for the entire duration of action. Clobenzorex is commonly prescribed to treat ? due to its strong appetite suppressing effect.
- Bronchodilation
- Muscle tension
- Dehydration
- Dry mouth
- Frequent urination
- Increased bodily temperature
- Increased perspiration
- Nausea - This effect usually only occurs at heavy doses.
- Pupil dilation - This effect is more prominent on the offset of the experience and usually only occurs at common to heavy doses.
- Stamina enhancement
- Teeth grinding - This component can be considered to be less intense when compared with that of MDMA.
- Temporary erectile dysfunction
- Vasoconstriction
Visual effects
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The visual effects of clobenzorex are usually less consistent and only mildly noticeable at higher dosages. They are somewhat comparable to the visual effects of deliriants and occur more readily in darker areas.
Enhancements
- Visual acuity enhancement
- Double vision - Amphetamines can cause double vision at high doses.
Distortions
- Drifting (breathing and morphing) - This effect is usually subtle and only occurs at higher doses, after long periods of being awake, or when combined with cannabis. Commonly this consists of level 1-2 drifting.
- Brightness alteration - Clobenzorex can make spaces seem brighter as a result of its pupil dilating effects.
Hallucinatory states
- Transformations - This effect occurs very rarely, and typically only when the user has taken high doses, is coming down, or has been awake for unusually long periods. They are usually very mild when they do occur.
Cognitive effects
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Clobenzorex shares most of its cognitive effects with other amphetamines, although it is less forceful in its come up due to the slower metabolism. It produces a variety of cognitive enhancements associated with stimulants. However, during the latter part of the duration, these cognitive enhancements may compete with or be nullified by the accumulated dopamine depletion and its effects.
The most prominent of these cognitive effects generally include:
- Analysis enhancement
- Anxiety - This effect occurs more frequently on the offset phase of the experience.
- Creativity enhancement
- Compulsive redosing - Due to the slow come up of clobenzorex, the full effects may not be felt for up to ? hours after consumption, causing some to redose during the come up. Compulsive redosing is more common if heavy doses are taken.
- Ego inflation
- Emotion suppression - This effect is more commonly reported with clobenzorex, in comparison to other amphetamines such as dextroamphetamine and methamphetamine. It is usually most intense at low and common doses.
- Focus enhancement
- Irritability - This effect occurs more frequently on the offset phase of the experience.
- Immersion enhancement
- Increased music appreciation
- Memory enhancement
- Motivation enhancement
- Increased libido or Decreased libido
- Novelty enhancement
- Time distortion - This can be described as the experience of time speeding up and passing much quicker than it usually would when sober.
- Thought acceleration
- Thought organization
- Wakefulness
- Cognitive euphoria
Auditory effects
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- Enhancements
- Hallucinations - Use of clobenzorex and other amphetamines, at a strong or heavy dose, can occasionally cause mild auditory hallucinations. These hallucinations most commonly occur amongst a source of white noise, such as a fan, and typically consist of quiet phantom music or voices. Clobenzorex may also cause auditory hallucinations in the form of stimulant psychosis.
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. The comedown produced by clobenzorex is often reported to be much less intense than its metabolite, dextroamphetamine, due to its increased duration of action. Its effects commonly include: Making sure to eat well and to hydrate are recommended to decrease the severity of comedown effects. Using mild sedatives is also a common strategy for stimulant comedowns.
Experience reports
There are currently 0 experience reports which describe the effects of this substance in our experience index.
Toxicity and harm potential
In rodents and primates, sufficiently high doses of amphetamine cause dopaminergic neurotoxicity, or damage to dopamine neurons, which is characterized by reduced transporter and receptor function. There is no evidence that amphetamine is directly neurotoxic in humans. However, large doses of amphetamine may cause indirect neurotoxicity as a result of increased oxidative stress from reactive oxygen species and autoxidation of dopamine.
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
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Overdose
A severe amphetamine overdose can result in a stimulant psychosis that may involve a variety of symptoms, such as paranoia, delusions, and hallucinations, including the infamous Shadow people. A Cochrane Collaboration review on treatment for amphetamine, dextroamphetamine, and methamphetamine psychosis states that about 5–15% of users fail to recover completely. According to the same review, there is at least one trial that shows antipsychotic medications effectively resolve the symptoms of acute amphetamine psychosis. Psychosis very rarely arises from therapeutic use. The combination of prolonged use of high doses combined with sleep deprivation significantly increases the risk of stimulant psychosis.
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.
- Alcohol - Drinking alcohol on stimulants is considered risky because it reduces the sedative effects of the alcohol that the body uses to gauge drunkenness. This often leads to excessive drinking with greatly reduced inhibitions, increasing the risk of liver damage and increased dehydration. The effects of stimulants will also allow one to drink past a point where they might normally pass out, increasing the risk. If you do decide to do this then you should set a limit of how much you will drink each hour and stick to it, bearing in mind that you will feel the alcohol and the stimulant less.
- GHB/GBL - Stimulants increase respiration rate allowing a higher dose of sedatives. If the stimulant wears off first then the depressant effects of the GHB/GBL may overcome the user and cause respiratory arrest.
- Opioids - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
- Cocaine - The rewarding effects of cocaine are mediated by DAT inhibition, and an increase of exocytosis of dopamine through the cell membrane. Amphetamine reverses the direction of DAT and the direction vesicular transports within the cell by a pH mediated mechanism of displacement, thus excludes the regular mechanism of dopamine release through means of exocytosis because the effects Na+/K+ ATPase are inhibited. You will find cardiac effects with the combination of cocaine and amphetamine due to a SERT mediated mechanism from the subsequent activation of 5-HT2B, which is an effect of serotonin-related valvulopathy. Amphetamines generally cause hypertension in models of abuse, and this combination can increase the chances of syncope due to turbulent blood flow during valve operation. The rewarding mechanisms of cocaine are reversed by administration of amphetamine.[7][8]
- Cannabis - Stimulants increase anxiety levels and the risk of thought loops and paranoia which can lead to negative experiences.
- Caffeine - This combination of stimulants is generally considered unnecessary and may increase strain on the heart, as well as potentially causing anxiety and physical discomfort.
- Tramadol - Tramadol and stimulants both increase the risk of seizures.
- DXM - Both substances raise heart rate, in extreme cases, panic attacks caused by these substances have led to more serious heart issues.
- Ketamine - Combining amphetamine and ketamine may result in psychoses that resemble schizophrenia, but not worse than the psychoses produced by either substance alone, but this is debatable. This is due to amphetamines ability to attenuated the disruption of working memory caused by ketamine. Amphetamine alone may result in grandiosity, paranoia, or somatic delusions with little to no effect on negative symptoms. Ketamine, however, will result in thought disorders, disruption of executive functioning, and delusions due to a modification of conception. These mechanisms are due to an increase of dopaminergic activity in the mesolimbic pathway caused by amphetamine due to its pharmacology effecting dopamine, and due to a disruption of dopaminergic functioning in the mesocortical pathways via NMDA antagonism effects of ketamine. Combining the two, you may expect mainly thought disorder along with positive symptoms.[9]
- PCP - Increases risk of tachycardia, hypertension, and manic states.
- Methoxetamine - Increases risk of tachycardia, hypertension, and manic states.
- Psychedelics (e.g. LSD, mescaline, psilocybin) - Increases risk of anxiety, paranoia, and thought loops.
- 25x-NBOMe - Amphetamines and NBOMes both provide considerable stimulation that when combined they can result in tachycardia, hypertension, vasoconstriction and, in extreme cases, heart failure. The anxiogenic and focusing effects of stimulants are also not good in combination with psychedelics as they can lead to unpleasant thought loops. NBOMes are known to cause seizures and stimulants can increase this risk.
- 2C-T-x - Suspected of mild MAOI properties. May increase the risk of hypertensive crisis.
- 5-MeO-xxT - Suspected of mild MAOI properties. May increase the risk of hypertensive crisis.
- DOx
- aMT - aMT has MAOI properties which may interact unfavorably with amphetamines.
- MAOIs - MAO-B inhibitors can increase the potency and duration of phenethylamines unpredictably. MAO-A inhibitors with amphetamine can lead to hypertensive crises.
Legal status
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- Brazil: Clobenzorex is a Class A3 controlled prohibited psychotropic.[10]
- Canada: Clobenzorex is not specifically listed in the CDSA, however due to structural similarities with norbenzphetamine, it is a Schedule I under item 19(17).[citation needed]
- United Kingdom: Clobenzorex is a Class B controlled drug.[11]
- United States: Clobenzorex is not scheduled and is unaffected by the Federal Analogue Act as a derivative of Benzphetamine.[12] Importation for personal use is lawful provided that is for use to treat a condition with no approved medications, unlawful marketing is not occurring in the U.S, not deemed hazardous to health for the treating the condition, and is verified as a continuation of a treatment plan that began in a foreign country.[13]
See also
External links
- Clobenzorex (Wikipedia)
- Clobenzorex (Isomer Design)
- Clobenzorex (DrugBank)
- SUBSTANCE (N/A)
Literature
- Young, R., Darmani, N. A., Elder, E. L., Dumas, D., & Glennon, R. A. (1997). Clobenzorex: Evidence for amphetamine-like behavioral actions. Pharmacology, Biochemistry, and Behavior, 56(2), 311–316. https://doi.org/10.1016/S0091-3057(96)00329-2
- Cody, J. T. & Valtier, S. (2001). Amphetamine, clobenzorex, and 4-hydroxyclobenzorex levels following multidose administration of clobenzorex. Journal of Analytical Toxicology, 25(3), 158–165. https://doi.org/10.1093/jat/25.3.158
References
- ↑ Young R, Darmani NA, Elder EL, Dumas D, Glennon RA (February 1997). "Clobenzorex: evidence for amphetamine-like behavioral actions". Pharmacology, Biochemistry, and Behavior. 56 (2): 311–316. doi:10.1016/s0091-3057(96)00329-2. PMID 9050090.
- ↑ Miller, G. M. (January 2011). "The Emerging Role of Trace Amine Associated Receptor 1 in the Functional Regulation of Monoamine Transporters and Dopaminergic Activity". Journal of neurochemistry. 116 (2): 164–176. doi:10.1111/j.1471-4159.2010.07109.x. ISSN 0022-3042.
- ↑ Drug banks amphetamine targets
- ↑ TA1 receptor | http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=364
- ↑ Lewin, A. H., Miller, G. M., Gilmour, B. (1 December 2011). "Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class". Bioorganic & medicinal chemistry. 19 (23): 7044–7048. doi:10.1016/j.bmc.2011.10.007. ISSN 0968-0896.
- ↑ ?
- ↑ Greenwald, M. K., Lundahl, L. H., Steinmiller, C. L. (December 2010). "Sustained Release d-Amphetamine Reduces Cocaine but not 'Speedball'-Seeking in Buprenorphine-Maintained Volunteers: A Test of Dual-Agonist Pharmacotherapy for Cocaine/Heroin Polydrug Abusers". Neuropsychopharmacology. 35 (13): 2624–2637. doi:10.1038/npp.2010.175. ISSN 0893-133X.
- ↑ Siciliano, C. A., Saha, K., Calipari, E. S., Fordahl, S. C., Chen, R., Khoshbouei, H., Jones, S. R. (10 January 2018). "Amphetamine Reverses Escalated Cocaine Intake via Restoration of Dopamine Transporter Conformation". The Journal of Neuroscience. 38 (2): 484–497. doi:10.1523/JNEUROSCI.2604-17.2017. ISSN 0270-6474.
- ↑ Krystal, J. H., Perry, E. B., Gueorguieva, R., Belger, A., Madonick, S. H., Abi-Dargham, A., Cooper, T. B., MacDougall, L., Abi-Saab, W., D’Souza, D. C. (1 September 2005). "Comparative and Interactive Human Psychopharmacologic Effects of Ketamine and Amphetamine: Implications for Glutamatergic and Dopaminergic Model Psychoses and Cognitive Function". Archives of General Psychiatry. 62 (9): 985. doi:10.1001/archpsyc.62.9.985. ISSN 0003-990X.
- ↑ Anvisa (2023-07-24). "RDC Nº 804 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 804 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Portuguese). Diário Oficial da União (published 2023-07-25). Archived from the original on 2023-08-27. Retrieved 2023-09-28.
- ↑ "Misuse of Drugs Act 1971 (c. 38): SCHEDULE 2: Controlled Drugs". Office of Public Sector Information. Retrieved 2009-06-15.
- ↑ Boos, Terrence (2023-04-06). "Clobenzorex Letter". Imgur. Archived from the original on 2023-07-11. Retrieved 2023-07-11.
- ↑ "Is it legal for me to personally import drugs?". FDA.gov. Food and Drug Administration. 2021-06-28. Retrieved 2021-07-22.