Talk:Bupropion
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Bupropion is known to cause extremely unpleasant if not dangerous experiences when used recreationally and especially at high doses.
Please use responsible use practices such as always having a trip sitter when trying this substance.
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This page has not been approved by the PsychonautWiki administrators. It may contain incorrect information, particularly with respect to dosage, duration, subjective effects, toxicity and other risks. |
| Bupropion | |||||||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||||||
| Common names | Wellbutrin, Zyban, Aplenzin, bupropion | ||||||||||||||||||||||||||||||
| Systematic name | (RS)-2-(tert-Butylamino)-1-(3-chlorophenyl)propan-1-one | ||||||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||||||
| Psychoactive class | Stimulant | ||||||||||||||||||||||||||||||
| Chemical class | Substituted cathinone | ||||||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||||||
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- Bupropion, sold as Wellbutrin (in sustained-release, immediate-release, or extended-release form), Zyban, and known also as amfebutamone, is a cathinone[1] medication used on-label for major depressive disorder and smoking cessation. Bupropion is also used off-label for seasonal affective disorder and ADHD. Bupropion is also taken recreationally for its deliriant-like and stimulant effects. It is a norepinephrine-dopamine reuptake inhibitor (NDRI) and nicotinic acetylcholine receptor antagonist. [2][3] It may exert its deliriant-like actions through antagonism of the nicotinic acetylcholine receptors.
History and culture
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This History and culture section is a stub. As a result, it may contain incomplete or wrong information. You can help by expanding it. |
Chemistry
Bupropion, is a molecule of the cathinone class with substituted a chlorine atom at R3 of its phenyl ring, and a tert-btylamine at the amino group. Cathinones are a sub-category of amphetamines, sharing the core amphetamine structure of a phenyl ring bound to an amino (NH2) group through an ethyl chain and an additional methyl substitution at Rα. Bupropion and other cathinones are differentiated by their ketone substitution on the beta carbon of the amphetamine skeleton, meaning they are β-keto-amphetamines
Pharmacology
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This pharmacology section is incomplete. You can help by adding to it. |
Bupropion binds to norepinephrine transporter (NET) and dopamine transporter (DAT), therefore inhibiting the reuptake of both monoamines. It also binds to nicotinic acetylcholine receptors as an antagonist. [4] Bupropion is extensively metabolized to hydroxybupropion, threohydrobupropion, and erythrohydrobupropion. It exerts its deliriant-like actions through antagonism of the nicotinic acetylcholine receptors, inhibiting the action of acetylcholine. The nAChRs it antagonizes are α3β2, α3β4, α4β2 nicotinic acetylcholine receptors. It also, very weakly, antagonizes the nicotinic acetylcholine receptor α7. [5][6] It is likely this antagonism of the nAChRs that causes bupropion to make users hallucinate and have vivid dreams.
Subjective effects
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This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it. |
Bupropion has an effects profile similar to diphenhydramine at high doses; in low doses, it acts as a mild and usually pleasant substance, but in high doses, delirium begins to take over and make for an extremely uncomfortable experience.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a research literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be regarded with a healthy degree of skepticism. It is 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 much more likely with higher doses and may include addiction, serious injury, or death.
Physical effects 
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- Stimulation - Bupropion's NDRI activity makes it a stimulating substance.
- Spontaneous physical sensations - This effect is usually weak. It can be described as a mild and pleasant soft or sharp tingling sensation with warmth radiating from the body, according to other substances with similar pharmacology.
- Seizures - This effect becomes more likely proportional to dose.
- Increased heart rate
- Increased blood pressure
- Pupil dilation
- Appetite suppression
- Nausea
- Tactile hallucinations - This effect is usually only present at high doses.
- Temperature regulation suppression
Visual effects 
- These effects are usually only present when taking high recreational doses, when it begins to act as a deliriant.
Cognitive effects 
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- Delirium - This occurs at high to very high and/or unreasonable doses and is a consequence of bupropion's antagonism of nicotinic acetylcholine receptors (nAChRs). Unlike other deliriants, this effect can be very painful and hard to get away from because of bupropion's ability to keep the user awake, unlike deliriants like diphenhydramine.
- Paranoia
- Delusions - This effect is usually only present at very high doses.
- Anxiety
- Mania - Bupropion increases the risk of manic episodes in individuals suffering from bipolar disorder.
- Motivation enhancement - This is commonly expressed in the form of being more talkative, fidgety, or having increased interest in tasks.
- Dream potentiation - Reports list that taking bupropion can lead to wild, vivid, and realistic dreams, usually feeling linear and very immersive, almost like a fun adventure. Time also seems to have passed much more than it actually has from sleep to wake. It is also easier to recall dreams. Consequently, bupropion can also inhibit sleep, but this can be countered with melatonin safely. This effect is likely exerted by its antagonistic action on nicotinic acetylcholine receptors.
- Time distortion - This is in the form of time expansion. A time period such as twenty minutes can feel as if it were up to eight hours. It happens at unreasonably high doses.
- Cognitive euphoria - The euphoria produced by bupropion is usually mild but in some people it has been reported to produce intense euphoria on par with that of amphetamine.
- Ego inflation
- Dysphoria - This effect is only present at high doses, usually due to its deliriant actions.
- Novelty enhancement
- Language suppression - This effect is only present at high doses, usually due to its deliriant actions.
- Increased sense of humor
- Increased libido - Bupropion is sometimes prescribed off-label for treatment of SSRI-induced sexual dysfunction.
- Craving suppression - Bupropion reduces the enjoyment and therefore the need for nicotine. Alone or with varenicline, bupropion SR and ER can be used for treatment of tobacco addiction and dependence. [7]
Auditory effects 
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- Auditory hallucinations - This effect is only present at high doses, usually due to its deliriant actions.
- Auditory enhancement - Sounds may be easier or more painful to hear. Usually, this isn't part of delirium necessarily, but it can be.
Experience reports
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
Toxicity and harm potential
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This toxicity and harm potential section is a stub. As such, it may contain incomplete or even dangerously wrong information. You can help by expanding or correcting it. |
It is strongly recommended that one use harm reduction practices when using bupropion; bupropion can cause seizures and therefore should not be combined with other substances that lower the seizure threshold such as tramadol or be used during GABAergic withdrawal.
Lethal dosage
Bupropion, despite having a relatively average LD50 for rats and mice,[8] is still very dangerous in overdose due to the risk of monoamine flood, seizures, and heart attacks or strokes.
Tolerance and addiction potential
Theoretically, bupropion is addictive because of its activity as an NDRI.
Dangerous interactions
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This dangerous interactions section is a stub. As such, it may contain incomplete or invalid information. You can help by expanding upon or correcting it. |
Although many psychoactive substances are reasonably safe to use on their own, they can suddenly become dangerous or even life-threatening when combined with other substances. The following list includes some known dangerous combinations (although it is not guaranteed to include all of them). Independent research (e.g. Google, DuckDuckGo) should always be conducted 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 (Amphetamine, lisdexamfetamine, methylphenidate, cocaine) - This combination can increase the chance of a heart attack, stroke, or adrenergic flood.
- Tramadol, tapentadol, or any other drug or substance that lowers the seizure threshold such as dextropropoxyphene or lithium. - This combination can increase the risk of seizures, death from seizures, or status epilepticus (seizure lasting longer than five minutes).
- Sedatives (Alprazolam, clonazolam, diazepam, opioids, phenobarbital, secobarbital, quetiapine) - Bupropion's effects are masked by sedatives such as benzodiazepines, barbiturates, alcohol, and antipsychotics. If the effects of sedatives wear off before bupropion's, bupropion's effects may seem or become more pronounced.
- Alcohol - This combination increases the risk of atypical and unpleasant or dangerous side effects such as seizures, paranoia, or depression.
- Depressive and/or manic disorders - Bupropion can increase the risk of suicide in depressed patients or users. It can also increase the risk of positive or negative mania.
- DXM - Bupropion is a potent inhibitor of CYP2D6, the enzyme primarily responsible for breaking down DXM. This can lead to prolonged effects and excessive accumulation of DXM in the bloodstream.[citation needed]
Legal status
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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. |
Internationally, bupropion is usually not controlled, but it is prescription-only.
See also
External links
Literature
References
- ↑ Iverson, of the ACMD, L. (2010, March 31). Consideration of the Cathinones. Retrieved from https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/119173/acmd-cathinodes-report-2010.pdf
- ↑ MedlinePlus. (2017, July 27). Retrieved from https://medlineplus.gov/druginfo/meds/a695033.html
- ↑ I, C. F., E, B. B., W, M. S., A, N. H., J, L. R., & I, D. M. (2014). Bupropion and bupropion analogs as treatments for CNS disorders. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24484978
- ↑ I, C. F., E, B. B., W, M. S., A, N. H., J, L. R., & I, D. M. (2014). Bupropion and bupropion analogs as treatments for CNS disorders. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24484978
- ↑ Lemke, Thomas L., Williams, David A. (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 611–613.
- ↑ I, C. F., E, B. B., W, M. S., A, N. H., J, L. R., & I, D. M. (2014). Bupropion and bupropion analogs as treatments for CNS disorders. Retrieved from https://www.ncbi.nlm.nih.gov/pubmed/24484978
- ↑ Ebbert, J. O., MD, MSc, Hatsukami, D. K., Ph.D., Croghan, I. T., Ph.D., Schroeder, D. R., MS, Allen, S. S., MD, Hays, T. J., MD, & Hurt, R. D., MD. (2014, January 8). Combination Varenicline and Bupropion SR for Tobacco Dependence Treatment in Cigarette Smokers: A Randomized Trial. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3959999/
- ↑ Cayman Chemicals. (2012, July 19). Retrieved from https://www.caymanchem.com/msdss/10488m.pdf