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Serotonin releaser combined with reuptake enhancer danger?

Ham-milton

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Jul 20, 2007
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I was doing some looking around at some of the less common TCAs, and the one I'm most familiar with, amineptine, purportedly enhances the reuptake of serotonin. As far as I'm aware, it's pretty unique in that effect.

I assume that combining amineptine with a serotonin releaser like MDMA isn't going to cause serotonin syndrome because it's picking up the released serotonin, preventing a huge build up in the synapse.

That said, does this sort of combination present any unique dangers? Or will it, unlike reuptake inhibitors, actually enhance the entactogenic effects? I suppose that even if it does enhance the effect, it's likely possible to over-do it, and the cause new problems but via a different route.

I'm not considering this combo myself, or actually concerned about particular effects of combining these two particular drugs, but more in the potential dangers or plus' from an interaction of two different effects.
 
Did I mess that up? Which TCA is the serotonin reuptake enhancer? Mianserin maybe? there are so many of them.

Maybe my understanding of the cause of serotonin syndrome is wrong, but isn't it caused by a build up of free serotonin? Wouldn't a reuptake enhancer prevent that?
 
Ham-milton said:
Did I mess that up? Which TCA is the serotonin reuptake enhancer? Mianserin maybe? there are so many of them.

Maybe my understanding of the cause of serotonin syndrome is wrong, but isn't it caused by a build up of free serotonin? Wouldn't a reuptake enhancer prevent that?

tianeptine from the same company as amineptine is listed as a serotonin reuptake enhancer, I don't know about amineptine as an enhancer, certainly the long chain and the rings are similar
 
Oh, yep, I did mess it up. Tianeptine is Stablon, that's actually the one I meant.
 
In theory i suspect one would anticipate it to be antagonistic to the effect of MDMA (et al) and counter the effect to some partial degree

No one i believe knows why Tianeptine seems to work...there may be a dopamnergic component and its effects seem to suggest it being successful for ED and being clinically tried for ADHD

an interesting drug that some seem to respond well to
 
Really? I had thought since drugs that prevented reuptake antagonised the effects of MDMA, the reuptake of the released serotonin was crucial for the entactogenic effects to take place. I thought that something like tianeptine would increase the effects.

I suppose this means I have an incomplete understanding of what's needed.
 
LuxEtVeritas said:
In theory i suspect one would anticipate it to be antagonistic to the effect of MDMA (et al) and counter the effect to some partial degree

No one i believe knows why Tianeptine seems to work...there may be a dopamnergic component and its effects seem to suggest it being successful for ED and being clinically tried for ADHD

an interesting drug that some seem to respond well to

I could see how it could possibly counter the effect of MDMA, but then again MDMA is very effective at reversing the transporter as well as screwing with VMAT-2 where the effect of MDMA is the dumping the vesicle contents into the cytoplasm.
if Tianeptine is a serotonin reuptake enhancer even in the presence of MDMA, then it will reverse some of the extracellular efflux, but then dump that back into the cytoplasm, where it would be transported back out by the monoamine transporters in reverse mode. This combination is a way to get very high cytoplasmic concentrations of serotonin, which is probably not a good thing. and as the transporters require metal ions and energy to work this cycling will consume a lot of ions and energy.
I suspect that the alterations phosphorylations and conformal changes caused by MDMA to SERT and the other monoamine transporters would prevent Tianeptine from working very well.
 
Ham-milton said:
Really? I had thought since drugs that prevented reuptake antagonised the effects of MDMA, the reuptake of the released serotonin was crucial for the entactogenic effects to take place. I thought that something like tianeptine would increase the effects.

I suppose this means I have an incomplete understanding of what's needed.

Reuptake inhibitors do indeed antagonise MDMA but because they prevent the uptake of MDMA itself into the neuron.
 
Oh, it's not because they stop the released serotonin from being taken back up?

That's a slight variation on my understanding, I suppose.

I'd like to see animals tested with this sort of combination.
 
There is actually one report on here of someone who had been taking Tianeptine for a month and then took MDMA. She said that it seemed to potentiate it as it was strongest roll she'd ever had.

As far as how Tianeptine works there has been research into its effects on neurogenesis, which the SSRIs also do. I'm also uncertain as to how much its affects on the opiate receptors could contribute.
 
Actually, I think it is a matter of when each drug is taken.

SSRI before MDMA blocks the action of MDMA. If taken after, perhaps it could enhance the risk of SS. And if taken after with sufficient time, there seems to be evidence of nuroprotective properties.

As for Tianeptine, I don't know about taking before MDMA, but taking it after MDMA (about 12 hours) almost completely cancelled the comedown for me.
 
Jamshyd said:
Actually, I think it is a matter of when each drug is taken.

SSRI before MDMA blocks the action of MDMA. If taken after, perhaps it could enhance the risk of SS. And if taken after with sufficient time, there seems to be evidence of nuroprotective properties.

As for Tianeptine, I don't know about taking before MDMA, but taking it after MDMA (about 12 hours) almost completely cancelled the comedown for me.

What dosage was that?
 
25mg twice a day. (so a standard medical dose, basically).

I forgot to mention that taking Tianeptine (same dose) slightly earlier than taking dexamphetamine REALLY potentiated the amp. but also added a side effect of intense vertigo. Not something I'd ever do again.
 
It might not be stimulating, yes, but MDMA works (and certainly feels) just like other stim. amphetamines, except that it has a much higher affinity for SERT.

Please note that I have not predosed MDMA with tianeptine - I've only taken tianeptine after MDMA.
 
I've only had MDMA once now, but I didn't find the stimulation anywhere near the level of even amphetamine. Maybe as strong as phentermine, but not more.

It was a tested roll, btw- just MDMA with a little caffeine, no other MDXX compounds or any depressants.
 
Oh I actually agree - I find pure MDMA to be actually almost sedating, in the lethargic manner that AMT is the same.

However, I am talking on a pharmacological level, the way this drug interacts with receptors is similar to Amphetamine, just with some drastically different affinities.
 
amineptine mix

What does anyone think about mixing oxycontin ,valium, fentinyl, klonopin and amineptine?

I don't knkow much about the chemistry of drugs. Do yo think anything will potentiate the amineptine?
 
^^Um...I don't even know where to begin. First, I think you should go back and read that sentence out loud. Does it sound like a smart idea? No, it doesn't. If you decide to proceed, after mixing two strong opioids and two benzos, I think you will be too, um, what's the word? Oh yeah: dead, to notice the amineptine.
 
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