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The Large and Nifty Not-quite-advanced Drug Chemistry, Pharmacology and More Thread

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No, but my wife says snorted gabapentin (neurontin) is not as effective as oral.

She snorted 2400 mgs.

She is fucking retarded.
 
Swerlz said:
I believe it has something to do with having to go through first-pass metabolization (through the liver)
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Yes, I believe that correct.

Sorry, at a point in my life where calling the wife a retard is a higher prority than passing on information. I have issues.
 
Mr valium man, read again. I said i can, and not i have or will.
damn about the b blockers. Having been on the brink of od my self i thought they wil only prevent that last line from making your heart feel like it is exploding.
 
I was thinking the same thing but it showed up in this this test.

A erowid crew member asked me to look into it but I can't seem to find anything. It's either very very new or a misprint. My gut says the latter; perhaps it's this?

Thanks for the help Murph :)
 
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chrisl21 said:
Mr valium man, read again. I said i can, and not i have or will.
damn about the b blockers. Having been on the brink of od my self i thought they wil only prevent that last line from making your heart feel like it is exploding.
Click to expand...

That's exactly the problem man. It won't FEEL like it is about to explode but in reality it still IS under excessive pressure and one should be aware of these sensations so they stop what is causing them, they shouldn't be unaware of them. Ignorance is bliss until it kills you.
 
naginnudej said:
I was thinking the same thing but it showed up in this this test.

A erowid crew member asked me to look into it but I can't seem to find anything. It's either very very new or a misprint. My gut says the latter; perhaps it's this?
Click to expand...
I must emphasize that the name "1-(3,4-Methylenedioxyphenyl)-2-methyl-2-pyrrolidinyl-1-propanone" is not 100% unambiguous. The following structure could also fit (although it is highly unlikely):



My vote still goes to the molecule shown in my last post.


Peace! - Murphy
 
My vote still goes to the molecule shown in my last post.
Click to expand...

Me too. The first one would be like a pyropropiophenone analogue of phentermine. I've actually wondered if that chemical would be active, and seems it is if it's showing up on some powder.

btw, anyone notice that powder also contains ethylamphetamine? neat.
 
iirc studies show that almost 100% of the drug is excreted (via renal pathways) unchanged.

A quick read shows that it exerts action on glutamic acid decarboxylase so maybe it passing through the liver anyway is required for its action? I don't know anything about enzymes really.
 
This is, once again, OD or BDD material.

And the reason it is effective is because pregabalin, like gabapentin, is taken up actively (like amino acids), not absorbed, in the gut. This means there is a limit to how much actually gets to your blood. When you IV, you bypass that barrier. That said, IVing capsules is a horrendous idea and can lead to things like infected abscesses and gangrene. If you think it is worth it, go nuts.
 
i still dont understand why IV does not work. bypassing first pass metabolization would be good for most drugs. this drug isnt metabolized at all, so sending it straight across the BBB seenms as if it would more effective than oral use. the BA is alrady 90% so really it would just be a quicker onset, but it doesnt seem to last at all.


when you take pregabalin orally it takes 1.5 hrs to Cmax, and that is VERY accurate. IV, you can feel it within 1 minute but it just dissapears. there is no plateau at all. im totally stumped. ive never used a drug where iv use was not far superior to oral.

there are some drugs, like tramadol, where the metabolite is the active drug and bypassing metabolization with IV renders it useless. however, pregab is not metabolized at all. does this make sense to anyone else or is it just me?
 
I'm pretty certain that pregabalin and gabapentin are both actively taken into the brain, not just through the gut. They're unable to cross the blood brain barrier and instead are taken up by an amino acid transporter (I forget which one- lysine springs to mind for some reason).

IIRC, that is.
 
I agree with Hammilton. Active transport happens from the guts into the blood stream (which can be bypassed by injection) AND from the blood stream into the brain (which can't be bypassed by any means).

- Murphy
 
I'm pretty certain that pregabalin and gabapentin are both actively taken into the brain, not just through the gut
[I
]AND from the blood stream into the brain (which can't be bypassed by any means).[/I]


so how would this exempt IV use of a drug that is not even metabolized? its not that there are no effects at all, it is just that they effects are greatly diminished.
 
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