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Gabapentin Prodrug: XP13512

Ham-milton

Bluelighter
Joined
Jul 20, 2007
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I was looking for any new information about how gabapentin works, and I came across this article about XP12512.

As I'm sure many are aware, Gabapentin itself is poorly absorbed, and as you take more and more, the percentage absorbed is less and less.

The researchers got around that by creating a prodrug designed for optimal absorption and named it XP13512. I've decided that whoever sells it is gonna name it Pronrontin, so that's what I'm gonna call it here.

Anyway, Gabapentin itself is virtually impossible to overdose on- a 32 gram overdoser managed to live and tell the tale with (fairly) minimal support from the ER. I don't think he was even put on a ventilator.

Will Pronrontin maintain this, or do you suppose the inability to die from it is directly related to the inability of the body to absorb it?

Will Pronrontin have a quicker method of action? I mean, neurontin takes about 2 hours to kick in at all, do you suppose that'll be the same or not?

It's pretty interesting, I think most of the problems with gabapentin itself are due to it's pharmacokinetic properties, but this should eliminate many of them, hopefully.

Here's the link: Pronrontin

It does talk about the synthesis at the very begining, though, so I hope I'm not violating policy. The information about the pharmacokinetics are towards the end (maybe halfway through?).

The synthesis, starting from gabapentin is pretty simple, I think. I'm no chemist, but it sounds like the sort of thing anyone with a bottom of neurontin and a handful of chemicals could handle.
 
If it has gigantic bioavailability (in comparison at least) then it would be a pretty bad idea to try dosing a lot of it. In other words, yeah it would prob cause an OD in a stupid user.
 
Yes, we know that. That's why I was telling him to be cautious because a much higher bioavailability can mean greater risk of OD.
 
I don't have a pile of this available, unfortunately (though from gabapentin, it seems pretty simple to obtain). I don't know if dosing with it will have an actual increased danger of OD- without seeing some data that's hard to say. With the increased bioavailability it's probably more likely. Is gabapentin as benign as it seems? It's hard to say. It's possible, though I think a bit unlikely.

Rather large doses are still going to be needed, probably between 1 and 2 grams. I don't think that this'll magically make it tons more potent.

Sorry, I'm a little buzzed. I'm having a hard time getting this to make sense. I'll postpone it.
 
Start with half of what you think you should take then slowly up it. Thats a good philosophy for drugs in general if you're uncertain.
 
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