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

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



Oral
Dosage
Threshold
(These values are for immediate-release bupropion.)
75 mg
Light 75 - 100 mg
Common 100 - 175 mg
Strong 250 - 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









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.


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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Chemistry

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Bupropion is a cathinone (aminoketone).

Pharmacology

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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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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.

The effects listed below are based on the subjective effect index, which is based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated with a healthy amount of skepticism. It is worth noting that these effects will rarely (if ever) occur all at once but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Visual effects
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Cognitive effects
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Auditory effects
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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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We also recommend that you conduct independent research and use harm reduction practices when 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,[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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Although many psychoactive substances are reasonably safe to use on their own, they can quickly become dangerous or even life-threatening when taken with other substances. The following lists some known dangerous combinations, but cannot be guaranteed to include all of them. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed 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.

Legal status

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Internationally, bupropion is usually not controlled, but it is prescription-only.

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. 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. 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
  5. Lemke, Thomas L., Williams, David A. (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 611–613.
  6. 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
  7. 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/
  8. Cayman Chemicals. (2012, July 19). Retrieved from https://www.caymanchem.com/msdss/10488m.pdf


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