Comment · Thu, August 29, 2013 · Ceretropic
Noopept- 1 Week Check-In
Original post in this thread
brocasta · 17 points
Experiencing great focus, feeling gregarious, experiencing greater verbal fluidity, coherence and clarity in formulating concepts, better time visualizing concepts, stellar sex performance/drive/experiences, and the apparent option to toggle "bullet time."
I've gone from 80th to 100th %ile in a number of brain training games.
I have a history of abuse of psychedelics, cannabis, dissociatives, alcohol, and benzos, though that's 9 months and counting behind me :)
How's everyone else responding?
I should add I started on my smoking quit date, slamming Hup A, lobelia, and theanine as well. Also aware that the Hup is not a viable long term option.
Peace and good vibes to all y'all!
EDIT: I don't wanna be misunderstood here. I'm pretty burnt at the end of every day. I work and play in two bands; if I don't study in the morning before work, I'm in no condition to do it in the evening. These effects are part pharmacological, part positive thinking/manifestation. Noots (for me anyway) don't compel me to be a better or produtive person; I often forget I'm on them, but when I compare where I'm at in terms of working on myself a week after starting this regimen, as well as a change…
What they were answering
GetsEclectic · 1 points
First problem was, not taking it under the tongue, won't work at all unless you do.
This is not true, noopept has high oral bioavailability.
u/MisterYouAreSoDumb · Ceretropic
Noopept has low oral bioavailablity. Around 10% to be exact. Don't cite Wikipedia. I just changed the entry.
Oral administration of noopept reaches much lower plasma concentrations than IV and sublingual. A lot of people quote a Russian study as saying that it's oral bioavailability is 97%, but that is incorrect.
The study showing that is in Russian and was done on rats and chinchilla rabbits. Their finding was actually 98.67% bioaccessibility of oral tablets in comparison to the oral parent compound via a feeding tube. The actual finding of peroral in comparison to IV was 9.33%. That means that only roughly 10% of the oral dose makes it to your bloodstream. Those quoting the 97% number have not read the actual study. I'll link the full text for you below.
> The absolute bioaccessibility was on the average
AUC
p.o./
AUC
i.v.
= 9.33 +-1.30%, which is evidence of a pronounced effect of the “first passage” via the gastrointestinal
tract and the liver. In comparison with rats, rabbits are characterized by slower absorption of the parent substance,
which is manifested by an almost twofold increase in MRT
and by decrease in the C
max
AUC
0
ratio in the latter case.
Peptides are easily ripped apart by digestive enzymes, and noopept is not immune to these effects. It's only saving grace is that it is a very small dipeptide. This means that it has a higher likelihood of being absorbed before being ripped apart than larger peptides that are almost 0% bioavailable. The longer it takes to get to your bloodstream, the more it will be broken apart. It will be ripped into it's 3 parts, the glycine, proline, and phenylacetyl esters. If this happens peripherally, the molecules are useless to the brain. They must pass the BBB before being metabolized. This is much less likely if you allow it to undergo first pass metabolism. The only thing noopept has going for it is size, which as you can see from the study doesn't help much.
Noopept is active orally, but much less than sublingual. Even the Russian pharmaceutical instructions state that it should be taken sublingually. The study I linked used 10mg/kg IV, and 50mg/kg peroral, and still the oral was unable to get close to the Cmax of IV.
>Thus, the results of our investigation showed that the absolute (peroral) bioaccessibility of noopept is 7.09% in rats and
9.33% +-1.30% in rabbits.
Here is another Russian study on the matter:
Similar plasma level of GVS- 111 was observed after 5 mg/kg parenteral and 50 mg/kg oral administration.
So it took 50mg/kg peroral to reach the plasma concentration of 5mg/kg paenteral. A very substantial difference.
Considerable differences related to the administration route were revealed in GVS-111 metabolism. After parenteral administration, apart from the unchanged GVS-111 molecule, the plasma contained 2 phenylacetyl metabolites phenylacetylproline and phenylacetic acid, which were not detected after oral administration. At the same time, plasma chromatograms after oral administration showed a peak which was eluted before GVS-111 and differed from the known phenylacetyl-derivatives by the elution time. It could be either hydroxylated or methylated GVS-111 metabolite. This difference in GVS-111 metabolism in different administration routes seems to be due to the fact that parenterally administered peptide is hydrolyzed preferentially by plasma peptidases, while metabolic transformations after oral administration occur during its first passage through the liver.
Given the evidence, noopept should be taken sublingually to be most effective.