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Comment · Thu, August 15, 2013 · Ceretropic

Will heat or acidity degrade noopept? (can I put noopept in my morning cup of coffee?)

What they were answering

Direct reply to the original post in this thread.

u/MisterYouAreSoDumb · Ceretropic

Noopept's melting point is 97*C (206*F). That is less than boiling, which is what most people use for coffee. So I would not suggest putting it in boiling water.

I'd be worried about stomach enzymes too. 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.

Full Text

> 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.

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