Talk:Bupropion - PsychonautWiki

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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Bupropion
Bupropion.svg
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

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.


⇣ Smoked
Dosage
Bioavailability {{{SmokedROA_Bioavailability}}}
Threshold < 75 mg
Light 75 - 150 mg
Common 150 - 225 mg
Strong 300 - 375 mg
Heavy 375 > mg
Duration
Total x - x hours
Onset 0.5 minutes
Come up x minutes
Peak x hours
Offset x hours
⇣ Oral
Dosage
Threshold
(These values are for immediate-release bupropion.)
75 mg
Light 75 - 125 mg
Common 125 - 225 mg
Strong 225 - 325 mg
Heavy 325 mg + Warning: Heavy risk of death by seizures
Duration
Total (These values are for immediate-release bupropion.) 8 - 12 hours
Onset 40 - 60 minutes
Peak 90 minutes
Offset 5 - 8 hours
After effects 1 - 2 days



⇣ Insufflated
Dosage
Threshold 50 mg
Light 50 - 150 mg
Common 150 - 300 mg
Strong 300 - 900 mg Warning: Heavy risk of death by seizures
Heavy 900 mg + Warning: Heavy risk of death by seizures
Duration
Total 20 - 180 minutes
Onset 30 - 120 seconds
Come up 1 - 5 minutes
Peak 5 - 20 minutes
Offset 10 - 60 minutes
After effects 1 - 6 hours






DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Interactions


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

 

This History and culture section is a stub.

As a result, it may contain incomplete or wrong information. You can help by expanding it.

Bupropion was invented by Nariman Mehta of Burroughs Wellcome (now GlaxoSmithKline) in 1969, and the US patent for it was granted in 1974. It was approved by the U.S. Food and Drug Administration as an antidepressant on 30 December 1985, and marketed under the name Wellbutrin. However, a significant incidence of seizures at the originally recommended dosage (400–600 mg/day) caused the withdrawal of the drug in 1986. Subsequently, the risk of seizures was found to be highly dose-dependent, and bupropion was re-introduced to the market in 1989 with a lower maximum recommended daily dose of 450 mg/day.

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

 

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. [3] 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. [4][5] It is likely this antagonism of the nAChRs that causes bupropion to make users hallucinate and have vivid dreams.

Subjective effects

 
 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), 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
 

Visual effects
 

Cognitive effects
 

    • 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
    • Disinhibition - This occurs mainly at recreational doses.
    • Delusions - This effect is usually only present at very high doses.
    • Anxiety - Bupropion causes more anxiety than other stimulants.
    • 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. This effect is mild when compared to amphetamines or methylphenidates.
    • 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 bupropion's high action on norepinephrine.
    • 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.
    • Increased music appreciation
    • Immersion enhancement
    • 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. [6]

Auditory effects
 

    • 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

 

This toxicity and harm potential section is a stub.

As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it.
Note: Always conduct independent research and use harm reduction practices if using this substance.

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,[7] is still very dangerous in overdose due to the risk of monoamine flood, seizures, and heart attacks or strokes.

Tolerance and addiction potential

Bupropion has potential for addiction because of its activity as an NDRI. The potential for addiction is greatly raised by insuffalation as an ROA. Bupropion can be addictive in both theraputic and recreational doses.

Dangerous interactions

 

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.

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 (Amphetamine, lisdexamfetamine, methylphenidate, cocaine) - This combination can increase the chance of a heart attack, stroke, or adrenergic flood. These agents often individually lowers the seizure threshold and may have additive effects when combined with Bupropion.
  • 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.
  • 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.[8] In extreme cases, panic attacks caused by these substances have led to more serious heart issues. Both DXM and Bupropion also lower the seizure threshold.
    • On the other hand, dextromethorphan/bupropion is an approved combination drug; each extended-release tablet contains 45 mg DXM and 105 mg bupropion. The maximum dose for depression is set at 2 tablets per day, spaced at least 8 hours apart.[9] Although this combination drug is safe enough to be approved, the safety of an instant-release combination and of higher doses remains a concern.
  • Cannabis - Bupropion causes anxiety, thought loops and paranoia more often than other stimulants.
  • 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.
  • 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.[10]
  • PCP - Increases risk of tachycardia, hypertension, and manic states.
  • Methoxetamine - Increases risk of tachycardia, hypertension, and manic states.
  • Psychedelics (e.g. LSD, mescaline, psilocybin) - Bupropion significantly 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

 

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.

  • Australia: Bupropion is a Schedule 4 controlled substance.[11]
  • Brazil: Bupropion is a Class C1 controlled substance.[12]

See also

External links

Literature

References

  1. ↑ 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
  2. ↑ MedlinePlus. (2017, July 27). Retrieved from https://medlineplus.gov/druginfo/meds/a695033.html
  3. ↑ 3.0 3.1 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
  4. ↑ Lemke, Thomas L., Williams, David A. (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 611–613.
  5. ↑ 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
  6. ↑ 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/
  7. ↑ Cayman Chemicals. (2012, July 19). Retrieved from https://www.caymanchem.com/msdss/10488m.pdf
  8. ↑ Journal of Clinical Psychopharmacology (June 2005). Inhibition of CYP2D6 activity by bupropion; Retrieved from https://pubmed.ncbi.nlm.nih.gov/15876900/
  9. ↑ McCarthy, B; Bunn, H; Santalucia, M; Wilmouth, C; Muzyk, A; Smith, CM (30 November 2023). "Dextromethorphan-bupropion (Auvelity) for the Treatment of Major Depressive Disorder". Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology. 21 (4): 609–616. doi:10.9758/cpn.23.1081. PMID 37859435. PMC 10591164. Retrieved via PMC.
  10. ↑ 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. 
  11. ↑ https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2013-PI-01138-1
  12. ↑ https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992


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