# wellbutrin prn as a stimulant



## swim (Apr 4, 2011)

since stimulants are banned in Italy, I thought I could take WB 150 prn in place of them playing on WB's instant-activating and analeptic properties.
Actually my GP proposed me to augment my treatment (now prozac 20mg and amisulpride 50mg every other day) with WB 150 but I'm afraid it could worsen my sinus tachycardia (which was caused by long drawn GAD).
The other med I could use in place of a proper stim is Provigil and even though in this case therapeutic plan is requested (and I don't have one) I could easily get hold of it.
So what do you think of WB 150 taken as a stimulant as needed? Or is it Provigil a better choice in this case?


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## beaches09 (Feb 1, 2009)

I've tried this many times. You'll often get an effect from it even after a single dose, though it's mild and far better just taking it normally and letting it build up for a week or two.

I don't remember the exact but (I think) the half life for the XL is close to a day, so I would dose 1 day and then I would still feel good the next day, but if I didn't dose that day, I'd wake up the next day feeling a lot more depressed than before dosing at all. So I don't recommend it for PRN personally. Just take it everyday. Instead of PRN maybe just try introducing a very small daily dose and go from there. Start at 37.5 then maybe 75mg. Might be a lot more seamless and give you that little boost you're looking for, without the downfall of prn and possibly the anxiety of larger doses.


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## swim (Apr 4, 2011)

beaches09 said:


> I've tried this many times. You'll often get an effect from it even after a single dose, though it's mild and far better just taking it normally and letting it build up for a week or two.
> 
> I don't remember the exact but (I think) the half life for the XL is close to a day, so I would dose 1 day and then I would still feel good the next day, but if I didn't dose that day, I'd wake up the next day feeling a lot more depressed than before dosing at all. So I don't recommend it for PRN personally. Just take it everyday. Instead of PRN maybe just try introducing a very small daily dose and go from there. Start at 37.5 then maybe 75mg. Might be a lot more seamless and give you that little boost you're looking for, without the downfall of prn and possibly the anxiety of larger doses.


thanks, I do also think so. The problem is we have only two WB dosages which are 150 and 300 and the pills are small and hard. I think WB's great for depression as I felt a remarkable mood uplift when taking it (for only 3 days) but I'm afraid it won't help me reduce my BPM.
So basically I don't know whether to add WB to prozac or to increase prozac alone dosage.
Btw we have one stimulant which is Ritalin but it's off-limits.


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## metamorphosis (Dec 18, 2008)

I take Wellbutrin 300xl. Used on a regular basis, allowing it's blood serum levels to reach a therapeutic level, lt is a very strong antidepressant by itself and also used as an adjunct to SSRI's for its relatively few side effects- no sexual side effects, negative on the weight gain, and it's energizing quality as a NE antagonist. Which, can cause agitation to many people who have SAD unless used with a anxiolytic but many times negates the SSRI's side effects

As far as being used as a prn "pep" pill, it might help mildly but it's effects on norepinephrine will have a stronger effect over time.

If you want non-amp stimulants, than go for provigil or nuvigil med. wise IMHO. There also many supplements and herbs for increased energy and strengthening of the adrenal glands.


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## meedo (Oct 4, 2011)

metamorphosis said:


> I take Wellbutrin 300xl. Used on a regular basis, allowing it's blood serum levels to reach a therapeutic level, lt is a very strong antidepressant by itself and also used as an adjunct to SSRI's for its relatively few side effects- no sexual side effects, negative on the weight gain, and it's energizing quality as a NE antagonist. Which, can cause agitation to many people who have SAD unless used with a anxiolytic but many times negates the SSRI's side effects
> 
> As far as being used as a prn "pep" pill, it might help mildly but it's effects on norepinephrine will have a stronger effect over time.
> 
> If you want non-amp stimulants, than go for provigil or nuvigil med. wise IMHO. There also many supplements and herbs for increased energy and strengthening of the adrenal glands.


How can it be NE antagonist? i thought it was a norepinephrine reuptake inhibitor .

How do you maintain neuron health and sensitivity ? i hear wellbutrin loose effect after a while for many people. I am very interested in it .. i want to get it to increase dopamine and confidence and self esteem !!

By the way.. i always benefit from your post my man !!:clap


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## beaches09 (Feb 1, 2009)

You could get a pill splitter. It's got a razor blade and can cut pretty small pills into 4ths.


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## metamorphosis (Dec 18, 2008)

meedo said:


> How can it be NE antagonist? i thought it was a norepinephrine reuptake inhibitor .
> 
> How do you maintain neuron health and sensitivity ? i hear wellbutrin loose effect after a while for many people. I am very interested in it .. i want to get it to increase dopamine and confidence and self esteem !!
> 
> By the way.. i always benefit from your post my man !!:clap


 Wellbutrin's action as a reuptake inhibitor, blocks the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine and therefore an increase in adrenergic (adrenal) neurotransmission.

An antagonist is a drug that binds to a receptor (i.e., it has affinity for the receptor binding site) but does not activate the receptor. Antagonists are also called receptor reuptake inhibitors because they block the effect of agonists. It antagonizes the neuron and the ability of NT reuptake by the receptor sites. It is an antagonist, just as the word implies.

An agonist is a drug that binds to a receptor of a cell and triggers a response by the cell. An agonist often mimics the action of the naturally occurring NT.

Here's a long review of bupropion reuptake effects on NE and to a lesser extent DA.

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC514842/


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## jim_morrison (Aug 17, 2008)

metamorphosis said:


> An antagonist is a drug that binds to a receptor (i.e., it has affinity for the receptor binding site) but does not activate the receptor. Antagonists are also called receptor reuptake inhibitors because they block the effect of agonists.


It's true that all reuptake inhibitors are antagonists (of the reuptake pump for the relevant receptor). However, not all receptor antagonists are reuptake inhibitors ie; a direct dopamine receptor antagonist such as haldol displays no reuptake inhibition properties.


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## Endorphin (Dec 4, 2011)

Doesn't Wellbutrin affect the same receptors as nicotine? They give it to people to quit smoking. Ive tried it once and felt really good. Relaxed but at the same time stimulated sort of like nicotine. Nicotine doesnt give me the "stimulant anxiety" it relaxes me more but it can definately be different with you


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## jim_morrison (Aug 17, 2008)

It has the opposite effect, it blocks nicotine receptors rather than stimulating them as nicotine would. But it may give a subjective 'stimulating' feeling due to it's enhancement of norepinephrine and to a lesser extent dopamine.


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## Endorphin (Dec 4, 2011)

jim_morrison said:


> It has the opposite effect, it blocks nicotine receptors rather than stimulating them as nicotine would. But it may give a subjective 'stimulating' feeling due to it's enhancement of norepinephrine and to a lesser extent dopamine.


Oh alright. You seem to know your drugs


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## metamorphosis (Dec 18, 2008)

jim_morrison said:


> It's true that all reuptake inhibitors are antagonists (of the reuptake pump for the relevant receptor). However, not all receptor antagonists are reuptake inhibitors ie; a direct dopamine receptor antagonist such as haldol displays no reuptake inhibition properties.


 True, there are different characteristics of medication that fall under the antagonistic term. How about a general definition of antagonist medications general modes of action:

A basic definition, Antagonist:A drug that binds to a receptor on a cell surface to block activity at the receptor. The antagonist itself does not elicit a biological response, it prevents the activating substance from binding to the receptor and so nullifies its action

Antagonists produce a conformational change in the g-proein linked receptors. It causes no change in signal transduction ( pre or post synaptic NT releasers), which includes no change in the amount of activity that may be present in the abscence of an agonists. True antagonist are actually neutral without actions of their own. Terminology wise , they are sometimes called silent. Antagonists will block the actions of everything an agonist would do. It does nothing itself, whereas an agonist's methods is to stimulate an increased downstream effect of NTs. from neurons. Selective reuptake inhibitors are one type of antagonist by working by binding to SERT.

This study mentions two type of antagonists (competitive and non competitive):

*Drugs and receptors DG Lambert, BSc (Hons) PhD, Reader in Anaesthetic Pharmacology, Edmund*
Antagonists*

Antagonists
Neutral antagonists block the effect of an agonist. There are two types of antagonism: competitive (reversible, surmountable) and non-competitive (irreversible, insurmountable). For example, naloxone is a competitive antagonists at all opioid receptors and ketamine is a non-competitive antagonist at the NMDA-glutamate receptor.

The action of a competitive antagonist can be overcome by increasing the dose of the agonist (i.e. the block is surmountable). Both the agonist and antagonist bind to the same site on the receptor. The effect that this has on the dose-response curve of an agonist is to shift it to the right. As the response is surmountable, the maximum response remains unchanged (Fig. 3). The degree of rightward shift is related to the affinity of the antagonist and the dose used. The higher the dose, the more agonist needed to overcome the response. The higher the affinity of the antagonist, the greater the shift (remember affinity is the strength of antagonist-receptor interaction and more agonist is needed to interrupt this interaction). Conversely, if the degree of shift is known, then the affinity of the antagonist can be estimated.
The actions of a non-competitive antagonist cannot be overcome by increasing the dose of agonist (Fig. 3). This is because the agonist and antagonist binding sites are different; hence, the agonist will not displace the antagonist molecule (e.g. ketamine binds in the NMDA receptor channel pore but the agonist, glutamate, binds to the extracellular surface of the receptor). Graphically, the actions of an irreversible antagonist are the same as those for a non-competitive antagonist but the explanation is different; for the irreversible antagonist the binding site may be the same as the agonist but as it is irreversible (often chemically linked) it cannot be displaced and hence cannot be overcome.


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## metamorphosis (Dec 18, 2008)

Endorphin said:


> Oh alright. You seem to know your drugs


Wellbutrin's helps in reducing the cravings of smoking in two ways.Nicotinic receptors crave "their fix" of nicotine for release of the pleasurable effects it produces, especially in the nucleus accumbus region of the brain. One being the NDRI's release of some DA into that area . The second action bupropion contributes to help with smoking cessation is it's affinity of binding to nicotinic receptors (alpha 4 beta 2). Bupropion also exerts enegetic properties with it's effect on NE.

Here's a long but excellent full abstract on nicotine. It's effects on the brain's reward systems and medications ued for cessation, bupropion included. If you have the time and patience to read it.

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2946180/


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## Huk phin (Oct 30, 2011)

OP - I would recommended standard Wellbutrin and not the XL version.


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## meedo (Oct 4, 2011)

Huk phin said:


> OP - I would recommended standard Wellbutrin and not the XL version.


why?


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