Bupropion and dopamine?

[MDPVagrant]

Bupropion is a dopamine and norepinephrine reuptake inhibitor. It is about twice as potent an inhibitor of dopamine uptake than norepinephrine uptake. As bupropion is rapidly converted in the body into several metabolites with differing activity, its action cannot be understood without understanding its metabolism. Occupancy of dopamine transporter (DAT) by bupropion and its metabolites in human brain measured by positron emission tomography was 6–22% according to an independent study[39] and 12–35% according to GSK researchers.[40]

The article goes on to note the supposedly "incredibly low" abuse potential, and I've read articles by doctors/scientists (people who should know better) who talk about "the good kind" of dopamine reuptake inhibitor e.g. bupropion, and the "bad" / addictive kind.

WTF? I felt the need to experiment a bit with this whole thing this morning, given a crapload of legally prescribed bupropion tablets sitting up in my cabinet. I do not take the stuff for depression currently.

Anyway, I took a single 100mg tablet (ground up to make it immediate-release), and prepared another via first boiling and then cold water extraction (CWE) techniques. In the meantime, I drank 32 ounces of 5.9 per cent alcohol beer. I noticed right away that the beer was feeling much more euphoric than usual, and that my mood was greatly enhanced.

Then, I rectally administered ~30mg extracted bupropion HCL to my chimpanzee, who weighs about what I do. The 'rush' was immediate, and felt quite a lot like any other SDRI. Sexual enhancement and all. It was much like MDPV, diphenyl prolinol or what have you.

So what's going on, and what's this with "6 to 22 percent" and "12 to 35 percent" DAT occupancy measured at different times? Could rapidity of absorption really be this important, or was it the concomitant administration of alcohol?

P.S. total intake by monkey was ~150mg in 4.5 hours, within therapeutic limits (barely). Anyone else who tries this, be careful of compulsive tendencies (as with any SDRI) and keep the seizure risk in mind. Trileptal on standby.

 

[hussness]

The reason why it doesn't have much abuse potential is because at doses barely above the therapeutic range it causes seizures. The drug originally went through trials at a higher therapeutic range, but too many patients were having seizures, so they scaled down the doses and got it to pass FDA approval.

 

[Reminisant B]

^Good point.

Bupropion is like the Dopamine reuptake equivalent of what Tramadol is to Opiates.

Tramadol can be potent with ZERO tolerance but it is self limiting in its nature because one can't really continue to increase the dose past a certain level without risking seizures & side effects.

Bupropion also stimulates α3β4 nicotinic receptoprs which is thought to add to its anti-addictive/anti-smoking properties so its more complicated than just DA re-uptake.

Non the less I agree with the original point, drugs tend to be branded into GOOD or BAD with no middle ground. Even more so their use, dexedrine is correcting a natural imbalance in ADHD but a student (with a more stable, developed brain) using the same dose to study for an exam - would by most people be labelled as abuse.

 

[Smyth]

Bupropion is a weak DARI, if a DARI at all, certainly not clear-cut vs. something like pyrovalerone. I think it is also a norepinephrine releaser, so certainly whatever the exact mechanism may be, which is of some importance, enhanced catecholamine levels ensue.

I def. wanna try some but that shit is expensive versus the selegiline that I recently procured. Although selegiline is nothing like 'weak speed', its actually a little drowsy, in my opinion having actually taken some.

 

[MDPVagrant]

Bupropion is a weak DARI, if a DARI at all, certainly not clear-cut vs. something like pyrovalerone.

I can tell you by the way it makes me feel that it is a dopamine reuptake inhibitor... after decades it's easy to recognize that feeling.

However, I gotta say one thing... my lab monkey (sorry if that reference is annoying, but I feel more comfortable with it) is no longer a typical or representative specimen. I dosed the monkey orally with a normal dose of bupropion the next day, and the reaction was "euphoria."

That had never happened before, but at this point the euphoric reaction is probably similar to the euphoria that anxious people get when dosing benzos. In other words, the monkey's dopamine receptors are chronically down-regulated, so a little extra dopamine seems to go a long way (in terms of a subjectively positive response).

P.S. it may be interesting to note that I'm completely fine mood-wise, no depression or anything else out of the ordinary. The usual lack of motivation, that's it (perhaps that's reason enough to consider talking to a doc & getting on bupropion again, I don't know).

 

[Will01996]

I have been taking Wellbutrin for 7 years to help with concentration, ADD and daytime sleepiness from opiate pain meds. I also take Ritalin.

Wellbutrin is very subtle. As others stated, it is self regulating becuase just a small increase in the dose makes me dizzy. (I am prescribed 150 mg. x 3 per day). If I take more than 2 pills, sometimes I am dizzy.

Prior to taking Wellbutrin, Ritalin was a weaker stimulant than coffee for me. I have never heard anyone else mention it, but the combo of Wellbutrin and Ritalin increases the effect of Ritalin a lot.

Also I felt nothing the first day and half on Wellbutrin. It took about a week of daily use to feel the benefit.

I forgot to take my Wellbutrin one day this week and I could tell a huge difference in my energy level by the end of the day.

Anyone else find that regular Wellbutrin use makes Ritalin work better?

I have often thought that someone would discover another drug, that taken in combo with Wellbutrin, would give the drug new potential. Kind of like Doriden (spelling?) did with Codeine.

 

[MDPVagrant]

I have been taking Wellbutrin for 7 years to help with concentration, ADD and daytime sleepiness from opiate pain meds. I also take Ritalin.

Wellbutrin is very subtle.

Not when dosed the way the OP suggests, i.e. extracted and then administered using one of the faster methods (insufflation, rectal, IV). It's capable of a powerful rush actually, which I suspect most people don't have a clue about thanks to XR and ER tablets.

Not that I'd recommend anyone use it recreationally BTW - the seizure risk is pretty high, and (although I suspect cocaine is higher) it's still not worth it IMO. Particularly if use becomes compulsive, because it can build to dangerously high blood levels. Also, it's just not anything special, and can be dowright jittery/unpleasant - IME diphenyl prolinol is more recreational and messes with NE less.

P.S. it's interesting how this thread has gone - I start it by posting direct personal experience + resulting thoughts, then most responses come back with vague theory (half of which sounds memorized from the PI sheet, or some ancient study). What?

 

[kamashankara]

I dosed 150 mg bupropion ER in the morning and found my afternoon to be highly creative and productive, got lots of writing done. I am very familiar with the classic dopamine surge of DRIs and finds bupropion to provide a comfortable lift when used occasionally in moderation.

on another note, I do recall back in the high school days taking 100 or so mg bupropion with about beers and feeling extremely euphoric and stimulated. I have read that bupropion can decrease alcohol tolerance, so there may be some sort of synergy there.

 

[AlphaMethylPhenyl]

Bupropion occupies D at levels sub ~45%, which is the level generally needed for euphoria. I also suspect it inhibits dopamine release since its a good antidepressant for those with mania (bi-polar).

 

[TCMVegas]

A year or two ago I looked up bupropion's affinities for NAT and DAT, as well as the affinities for its main metabolites and their concentrations.

Conclusion: I think I remember that it had about 10x the affinity for NE as DA. Which is easy to relate to its seizure risk as well as low abuse potential.

 

[Sherminator]

I've seen clinical studies on bupropion that used doses up to 450mg therapeutically, are you guys certain about it having such a narrow therapeutic range? When used in conjunction with SSRIs to combat the sexual side effects SSRIs are notorious for the effective dose is 225-450mg if my memory serves me right. Actually I just found the study I was thinking of: "Pharmacologic modification of psychosexual dysfunction." <http://www.ncbi.nlm.nih.gov/pubmed/3121861> This article doesn't deal specifically with SSRI induced sexual problems, but the doses for treating sexual dysfunction are definitely higher than you guys are talking about in this thread.

"Sixty female and male outpatients with psychosexual dysfunction (sexual aversion/inhibited sexual desire, inhibited sexual excitement, and/or inhibited orgasm) participated in a comparison of the efficacy of bupropion hydrochloride vs placebo....[After 8 week placebo test] Patients were then assigned randomly to 12 weeks of double-blind treatment with bupropion, 225-450 mg/day, or matching placebo."

 

[scarlet--o]

Chimpanzee SRSLY?

Do you srsly have a chimpanzee? And you actually test drugs on him? WTF IS WRONG W U?

The article goes on to note the supposedly "incredibly low" abuse potential, and I've read articles by doctors/scientists (people who should know better) who talk about "the good kind" of dopamine reuptake inhibitor e.g. bupropion, and the "bad" / addictive kind.

WTF? I felt the need to experiment a bit with this whole thing this morning, given a crapload of legally prescribed bupropion tablets sitting up in my cabinet. I do not take the stuff for depression currently.

Anyway, I took a single 100mg tablet (ground up to make it immediate-release), and prepared another via first boiling and then cold water extraction (CWE) techniques. In the meantime, I drank 32 ounces of 5.9 per cent alcohol beer. I noticed right away that the beer was feeling much more euphoric than usual, and that my mood was greatly enhanced.

Then, I rectally administered ~30mg extracted bupropion HCL to my chimpanzee, who weighs about what I do. The 'rush' was immediate, and felt quite a lot like any other SDRI. Sexual enhancement and all. It was much like MDPV, diphenyl prolinol or what have you.

So what's going on, and what's this with "6 to 22 percent" and "12 to 35 percent" DAT occupancy measured at different times? Could rapidity of absorption really be this important, or was it the concomitant administration of alcohol?

P.S. total intake by monkey was ~150mg in 4.5 hours, within therapeutic limits (barely). Anyone else who tries this, be careful of compulsive tendencies (as with any SDRI) and keep the seizure risk in mind. Trileptal on standby.

 

[immad]

Do you srsly have a chimpanzee? And you actually test drugs on him? WTF IS WRONG W U?

What is wrong with you to react to a three year old thread to ask whether someone actually has a chimp? (Hint: probably not)

What is wrong with me to respond to this, thereby keeping this going?

 

[Nagelfar]

"CHIMP" is the new "S.W.I.M." (i.e. someone who isn't me); which is Certainly haven't individually made purchase (or "property"/"possession") (of the illicit substances, or chemistry wares, in question), and the fightin' words in response to CHIMP is *C.H.U.M.P" (well Certainly Haven't U Made Purchase/Possession, of such a thing before?)