• N&PD Moderators: Skorpio

Bupropion above 300 mg, counteract activation and induce fatigue - mechanism?

Bupropion itself is a legit NDRI in vitro, but if taken orally almost all of it gets metabolized before reaching systemic circulation, producing metabolites that are NRI and lack any noticable effects on dopamine. But if Bupropion is administered IV/IM/nasal/rectal the "first pass effect" is bypassed, allowing Bupropion to reach systemic circulation unchanged and deliver its NDRI activities to the subject.


This just has me thinking.


What I'd like to do is determine the effect dopamine has on myself.
Whether it's positive and stimulating, or sedating/faituge inducing.


I have bupropion tablets - SR version.


If I wanted to by pass the metabolism process - how exactly do I do that?
I mean, fuck injecting - I hate needles.


Crush it up and snort it, some shit like that?
 
Ritalin has potent effects on dopamine like cocaine and unlike wellbutrin ritalin can occupy 50 percent of the dopamine transporters in pet scan studies
 
The synergistic effect of releasing agents and reuptake inhibitors happens at certain doses where the releasing agents dump out a lot of neurotransmitters into the synapse and then the reuptake inhibitors prevent the clearance of said neurotransmitters. There will be a point though where the reuptake inhibitor interferes with the releasing agent's ability to reverse the transporter however.

Also Cocaine/Methylphenidate are kinda weird, could be DAT inverse agonists. Meaning they could be stabilizing the DAT in a reverse facing conformation that could cause neurotransmitter efflux, rather than just plugging it up in its normal forward facing conformation.
 
This just has me thinking.


What I'd like to do is determine the effect dopamine has on myself.
Whether it's positive and stimulating, or sedating/faituge inducing.


I have bupropion tablets - SR version.


If I wanted to by pass the metabolism process - how exactly do I do that?
I mean, fuck injecting - I hate needles.


Crush it up and snort it, some shit like that?
Injecting is serious business,
ONLY inject INJECTABLES.
NEVER inject pills or any other drug form not intended for injection.

Now back on point about your question:
Snorting bupropion burns so bad.
Some people attribute it to the excipients present in SR pills, but trust me, I've snorted pure crystal bupropion, it still burns like hell.

Best method is enema.
Crush your pill, mix it well with 2ml of water, let the slur to settle down, suck out the top clear solution using a syringe, remove the needle (obviously...), insert the syringe into your backdoor as deep as you can, empty it.
 
I would be careful my sister had a seizure from using wellbutrin orally and she does no other drugs or drink. I dont know how if you took it In a enema how that would influence its ability to cause seizures in some. Also another possibility is stimulation causing reduced activity.often after taking adderall ill just be perfectly still rather than running around once it reaches a certain intensity.
 
Good thread; but yeah, combination of Wellbutrin and other N/D reuptake inhibitors or releasers is potentially dangerous in terms of both seizures and psychosis. Medically it would be considered (on the lighter side of) "heroic" treatments for depression. I have (clinically/anecdotally) seen people who do report sedation from Wellbutrin, to the point where they prefer to take it at night (not so much that it's a sedative, but that the sedation is significant enough that they don't want to take it in the morning as usually prescribed, which isn't a problem but does testify to the fact that this is a real phenomenon.) I do not, however, buy into the idea that people with AD(H)D find amphetamines/NDRIs "sedating," they certainly do help them concentrate (do that for us too) and in that sense I guess could be called "calmative," but sedating, no. We still generally find problems with sleeplessness and anxiety if they're not dosed properly, although you will come across patients who reply that amphetamines are anxiolytic rather than anxiogenic, which is another interesting question perhaps not totally related to the OP's. (I even knew at least one guy who would do cocaine right before bed saying that he found it to be relaxing and not to be a problem with insomnia and so on. Brains are pretty diverse.)
 
Im surprised desipramine isnt available in the UK. Its an old-school TCA NRI. What about protriptyline?
 
Injecting is serious business,
ONLY inject INJECTABLES.
NEVER inject pills or any other drug form not intended for injection.

Now back on point about your question:
Snorting bupropion burns so bad.
Some people attribute it to the excipients present in SR pills, but trust me, I've snorted pure crystal bupropion, it still burns like hell.

Best method is enema.
Crush your pill, mix it well with 2ml of water, let the slur to settle down, suck out the top clear solution using a syringe, remove the needle (obviously...), insert the syringe into your backdoor as deep as you can, empty it.

Now I've plugged bupe and I've plugged prop but I've never plugged buprop. lol ;-j (I have some now though)
 
Im surprised desipramine isnt available in the UK. Its an old-school TCA NRI. What about protriptyline?

Also
Also not

Nortriptyline is, amitriptyline, amoxapine, prothiadien (almost solely a serotonergic), anafranil.
A lot of serotonergics, but not noradrenergics.

Nortriptyline was licensed only about 6 months ago.

Though, there is reboxetine, for which I found an online article delineating its functional values - apparently similar to desipramine on NET.
So maybe I'll chance that.
 
Also
Also not

Nortriptyline is, amitriptyline, amoxapine, prothiadien (almost solely a serotonergic), anafranil.
A lot of serotonergics, but not noradrenergics.

Nortriptyline was licensed only about 6 months ago.

Though, there is reboxetine, for which I found an online article delineating its functional values - apparently similar to desipramine on NET.
So maybe I'll chance that.

what, for pain?
TCAs are really old school drugs
and underrated ones, too
does the NHS just have a hate on for them or what
 
what, for pain?
TCAs are really old school drugs
and underrated ones, too
does the NHS just have a hate on for them or what

Umm
Quite possibly - the licensed doses are.... yeah, not depressive theraputic doses.

Also bupropion is only available here as a smoking cessation aid, only some GP's script it off license - like mine did.

I think it was due to their toxicity in overdose is the main reason for their non-inclusion.

Though the health system in the US have refuted reboxetine...
I don't know if they still allow mianserin and, milnicipran - tetracyclics.
They're not licensed under the NHS but, can import them from sweden and netherlands.
 
Not everyone finds amphetamine relaxing. I find it rewarding so urs relaxing like if u like playing basketball its stimulating but if u enjoy its relaxing
 
TCAs are very useful drugs. And I dont mean in any recreational sense at all. Hard to believe the NRIs are so disliked in the UK. What about obtaining a prescription and getting the medication shipped from outside the country?
 
TCAs are very useful drugs. And I dont mean in any recreational sense at all. Hard to believe the NRIs are so disliked in the UK. What about obtaining a prescription and getting the medication shipped from outside the country?

Good
question.

Meeting my doc next monday so, I'm gonna find out, but I'm not holding my breath.

The NHS, or NHS doctors, don't normally script off license medications.

I'll either then try and convince my GP to script a med he never has before, and has no experience with, going solely on what I tell him.

Or pay 250 units of currency for a private consultation, a private doctor - and see what happens with that.
 
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