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Re: How does Wellbutrin work ? » SLS

Posted by Sunnely on February 23, 2001, at 22:07:02

In reply to How does Wellbutrin work ?, posted by SLS on February 23, 2001, at 14:55:02

Stephen M. Stahl, MD (Essential Psychopharmacology, 2000, 2nd ed., Cambridge University Press, Cambridge, UK) explains it this way:

"Bupropion is the prototypical agent of the norepinephrine and dopamine reuptake inhibitors. For many years, its mechanism of action was unclear. Bupropion itself has weak reuptake properties for dopamine, and weaker yet reuptake properties for norepinephrine. The action of the drug on norepinephrine and dopamine neurotransmission, however, has always appeared to be more powerful than these properties could explain, which has led to proposals that bupropion acts rather vaguely as an adrenergic modulator of some type. Bupropion is metabolized to an active metabolite, which is not only a more powerful norepinephrine reuptake blocker than bupropion itself but is also concentrated in the brain. In some ways, therefore, bupropion is more of a pro-drug (i.e., precursor) than a drug itself. That is, it gives rise to the "real" drug, namely its hydroxylated active metabolite (hydroxybupropion), and it is this metabolite that is the actual mediator of antidepressant efficacy via norepinephrine and dopamine reuptake blockade."

===============================================

> How does Wellbutrin (bupropion) work?
>
>
> - Scott


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