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Comment · Thu, May 7, 2020

Dynamax works great but can't sleep

Original post in this thread

agatechno · 8 points

It seems that I'm a slow metabolizer of caffeine. I've been using dynamax and it's arguably the best caffeine based supplement I've used. But I only get a few hours of sleep when using it. Yesterday I took it at 7am and stayed awake in bed from 10pm-2am before finally falling asleep. I also took sleep support from ND but the Caffeine seems to render it useless. Someone recently linked to a product (evodia fruit extract) on the nootropics sub that supposedly increases caffeine metabolism. Would this work even though the caffeine from dynamax is extended release?

What they were answering

Direct reply to the original post — see the thread post above.

u/MisterYouAreSoDumb

So you are likely feeling the effects from the caffeine metabolite paraxanthine. That has even stronger locomotor stimulating effects than caffeine.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3562388/

In this study we show that in rats paraxanthine has a stronger locomotor activating effect than caffeine or the two other main metabolites of caffeine, theophylline and theobromine. As previously described for caffeine, the locomotor activating doses of paraxanthine more efficiently counteract the locomotor depressant effects of an adenosine A1 than an adenosine A2A receptor agonist. In drug discrimination experiments in rats trained to discriminate a maximal locomotor activating dose of caffeine, paraxanthine, unlike theophylline, generalized poorly to caffeine suggesting the existence of additional mechanisms other than adenosine antagonism in the behavioral effects of paraxanthine.

So what is happening is likely that you are metabolizing the caffeine later in the day into paraxanthine, and that is keeping you awake. You are correct to point to Evodia rutaecarpa. That contains a compound called rutaecarpine. Rutaecarpine not only speeds up the metabolism of caffeine, but also speeds up the metabolism of paraxanthine.

https://www.ncbi.nlm.nih.gov/pubmed/21468923

The areas under the curve of both caffeine and its three major metabolites (paraxanthine, theophylline, and theobromine) were significantly reduced by rutaecarpine, indicating that caffeine was rapidly converted into the desmethylated metabolites, and that those were also quickly transformed into further metabolites via the hydroxyl metabolites due to the remarkable induction of CYP1A2 and 2E1. The significant induction of ethoxyresorufin O-deethylase, pentoxyresorufin O-depentylase, and p-nitrophenol hydroxylase strongly supported the decrease in caffeine and its major metabolites in plasma, as well as in urine. These results clearly suggest that rutaecarpine increases the metabolism of caffeine, theophylline, theobromine, and paraxanthine by inducing CYP1A2 and CYP2E1 in rats.

So that might be a good idea for you. Taking rutaecarpine in the afternoon would speed up the breakdown, and give your body time to clear out the paraxanthine in your system before bed.

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