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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 14 of 14. This is the beginning of the thread.
Posted by dondon on March 6, 2004, at 14:26:14
I've heard that zoloft has more potent da reuptake
properties than wellbutrin at higher doses. Is this
true? At what dose does zoloft begin to have a
meaningful effect on dopamine? 300 mgs, 400 mgs?
Posted by rvanson on March 6, 2004, at 16:58:14
In reply to zoloft and dopamine, posted by dondon on March 6, 2004, at 14:26:14
> I've heard that zoloft has more potent da reuptake
> properties than wellbutrin at higher doses. Is this
> true? At what dose does zoloft begin to have a
> meaningful effect on dopamine? 300 mgs, 400 mgs?I've never seen any medical studies showing that Zoloft has dopamine enhancing properties, though some people seem to think so.
Does anyone know of a site where there is proof of this link ?
Posted by T-rotten on March 6, 2004, at 19:13:56
In reply to Re: zoloft and dopamine » dondon, posted by rvanson on March 6, 2004, at 16:58:14
> > I've heard that zoloft has more potent da reuptake
> > properties than wellbutrin at higher doses. Is this
> > true? At what dose does zoloft begin to have a
> > meaningful effect on dopamine? 300 mgs, 400 mgs?
>
> I've never seen any medical studies showing that Zoloft has dopamine enhancing properties, though some people seem to think so.
>
> Does anyone know of a site where there is proof of this link ?What I heard is that fluoxetine is the most IRSS potent on dopamine function but not as bupropion. Now I got confused.
Posted by rvanson on March 6, 2004, at 23:11:07
In reply to Re: zoloft and dopamine, posted by T-rotten on March 6, 2004, at 19:13:56
> > > I've heard that zoloft has more potent da reuptake
> > > properties than wellbutrin at higher doses. Is this
> > > true? At what dose does zoloft begin to have a
> > > meaningful effect on dopamine? 300 mgs, 400 mgs?
> >
> > I've never seen any medical studies showing that Zoloft has dopamine enhancing properties, though some people seem to think so.
> >
> > Does anyone know of a site where there is proof of this link ?
>
> What I heard is that fluoxetine is the most IRSS potent on dopamine function but not as bupropion. Now I got confused.heres a link to the Prozac/Dopamine connection.
Posted by Shawn. T. on March 7, 2004, at 13:24:56
In reply to Re: zoloft and dopamine, posted by rvanson on March 6, 2004, at 23:11:07
Zoloft (sertraline) exhibits relatively weak dopamine reuptake inhibiting properties (see http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11543737&dopt=Abstract and http://www.preskorn.com/books/ssri_s3.html ). I don't believe that anyone has studied its dopaminergic effects in vivo with humans. A 30 mg/kg, i.p dose of the drug given to rats has been shown to decrease dopamine metabolites; one would expect this result if it were inhibiting dopamine reuptake (see http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9660102&dopt=Abstract ). Unfortunately, that result doesn't tell us anything about how typical oral doses of Zoloft affect humans. I very strongly doubt that Zoloft is a stronger dopamine reuptake inhibitor than Wellbutrin at normal therapeutic concentrations.
Prozac (fluoxetine) is a 5-HT2C receptor antagonist. As a result, it may increase dopamine and norepinephrine levels in some regions of the brain such as the prefrontal cortex while having no effects in other regions (see http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11919662&dopt=Abstract ). It's also interesting to note that norepinephrine reuptake inhibitors can inhibit dopamine reuptake in the prefrontal cortex because the region lacks dopamine transporters (see http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12716261&dopt=Abstract ). On a similar note, the finding by Bymaster et al. (2002) that sertraline does not inhibit the reuptake of dopamine in the prefrontal cortex does not imply that it lacks an effect on dopamine reuptake in other locations.
Shawn
Posted by dondon on March 7, 2004, at 16:48:20
In reply to Re: zoloft and dopamine, posted by Shawn. T. on March 7, 2004, at 13:24:56
It says zoloft has moderate affinity for dopamine reuptake.
I bet if one were to push the dose to 400 mgs it would
become a potent da reuptake inhibitor.
Posted by King Vultan on March 7, 2004, at 17:32:05
In reply to Re: zoloft and dopamine » dondon, posted by rvanson on March 6, 2004, at 16:58:14
> > I've heard that zoloft has more potent da reuptake
> > properties than wellbutrin at higher doses. Is this
> > true? At what dose does zoloft begin to have a
> > meaningful effect on dopamine? 300 mgs, 400 mgs?
>
> I've never seen any medical studies showing that Zoloft has dopamine enhancing properties, though some people seem to think so.
>
> Does anyone know of a site where there is proof of this link ?
The best info on this particular topic I've seen is at www.preskorn.com in a column that I think is entitled: Bupropion: What Mechanism of Action? Preskorn goes into some detail on the pharmacology of both bupropion (Wellbutrin) and sertraline (Zoloft), particularly in regard to their dopamine reuptake inhibiting capabilities.The bottom line is that Wellbutrin winds up being a much more powerful dopamine reuptake inhibitor in practice because of the activity of its metabolites, which build up in the body to enormous concentrations. The dopamine reuptake inhibition of the parent molecule is weak and is actually inferior to that of Zoloft, but Zoloft's dopamine reuptake inhibition winds up being limited because of tolerance issues related to its much more powerful blockade of serotonin reuptake. To approach Wellbutrin's ability to blockade dopamine reuptake, a very high dosage of Zoloft would be necessary, which would likely generate severe adverse effects related to saturation of the serotonin reuptake transporter.
Todd
Posted by Dave1 on March 7, 2004, at 17:49:34
In reply to Re: zoloft and dopamine » rvanson, posted by King Vultan on March 7, 2004, at 17:32:05
Hi,
I get hand tremor, and my tongue sticks out involuntarily sometimes. This started since I hbegan taking Prozac, 3 months ago, for OCD.
I am currently on 80mg/day.
My question: What does all this Prozac/Dopamine relation data suggest about the possibility of developing a tardive dyskinesia like disorder if I continue on the Prozac long-term.Any input welcome.
Dave
Posted by dondon on March 7, 2004, at 18:37:14
In reply to Re: zoloft and dopamine » rvanson, posted by King Vultan on March 7, 2004, at 17:32:05
Actually I just did some research and found out that zoloft
is far more potent than bupropion in terms of da
reuptake. It is also more potent than nomifensine(a drug
that is used for treating parkinsons when amantadine can't be used or tolerated)
If a patient with parkinson's disease had to depend on zoloft for symptom relief , they could use 200 mgs of zoloft with
30 mg of remeron (blocks 5ht2 and 5ht3) for treating parkinsons
Posted by Sad Panda on March 8, 2004, at 2:57:35
In reply to zoloft and dopamine, posted by dondon on March 6, 2004, at 14:26:14
I suspect Zoloft's weak DA reuptake ability may have something to do with it's reputation for being an above average SSRI. I think it should be the first choice for a depression med because of this & because it's the safest.
Cheers,
Panda.
Posted by jlbl2l on March 8, 2004, at 3:30:38
In reply to zoloft and dopamine, posted by dondon on March 6, 2004, at 14:26:14
if you know a bit about neurochemistry and neuropharmacology you may know that ALL anti depressants increase dopamine because dopamine is regarded as the final pleasure pathway in the brain. meaning, dopamine ultimately makes us happy. thats why DIRECT dopamine reuptake inhibitors (such as amniptine) were banned. too much happiness i guess, right? and thats why ADS will never acheive 100% perfection for anyone. oh well. Amineptine is still available btw. :-)
Posted by jlbl2l on March 8, 2004, at 3:33:06
In reply to Re: zoloft and dopamine, posted by jlbl2l on March 8, 2004, at 3:30:38
oh yeah and to follow up, zoloft at the higher end dosages DOES increase dopamine more so than other A-D's probably because its also more effective globally than other ads. Who knows tho? creful tho, max dose zoloft can lead to mania caused by to much dopamine. ive seen it in person!
Posted by King Vultan on March 8, 2004, at 8:06:09
In reply to Re: zoloft and dopamine, posted by Dave1 on March 7, 2004, at 17:49:34
> Hi,
>
> I get hand tremor, and my tongue sticks out involuntarily sometimes. This started since I hbegan taking Prozac, 3 months ago, for OCD.
> I am currently on 80mg/day.
>
>
> My question: What does all this Prozac/Dopamine relation data suggest about the possibility of developing a tardive dyskinesia like disorder if I continue on the Prozac long-term.
>
> Any input welcome.
>
> DaveTardive dyskinesia is caused by chronic blockade of dopamine receptors, as antipsychotic drugs do. This is the exact opposite of what is being discussed here, which is blockading dopamine reuptake, resulting in increasing dopamine transmission and consequent stimulation of those dopamine receptors. Your hand tremor is likely the result of stimulating serotonin 2A receptors from Prozac's blockade of serotonin reuptake.
Todd
Posted by King Vultan on March 8, 2004, at 8:16:47
In reply to Re: zoloft and dopamine, posted by dondon on March 7, 2004, at 18:37:14
> Actually I just did some research and found out that zoloft
> is far more potent than bupropion in terms of da
> reuptake. It is also more potent than nomifensine(a drug
> that is used for treating parkinsons when amantadine can't be used or tolerated)
> If a patient with parkinson's disease had to depend on zoloft for symptom relief , they could use 200 mgs of zoloft with
> 30 mg of remeron (blocks 5ht2 and 5ht3) for treating parkinsons
No, Zoloft appears superficially to have superior dopamine reuptake inhibition, but the reality is that its blockade of serotonin reuptake and related adverse effects limit its dosage and consequently its ability to affect dopamine reuptake. The issue of Wellbutrin's metabolites and their blockade of dopamine reuptake is also enormous. This is a link to the article I mentioned earlier.http://www.preskorn.com/columns/0001.html
Todd
This is the end of the thread.
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