May 11, 2012
UPDATES: The makers of the product commented below and also emailed me some of their studies. They say: “Regarding the dose, our target was to be safe as well as effective. We did an internal review of all the available studies and combined them with our own studies on human liver cells in our lab. We chose a dose that was still effective for CYP1A2 induction (for caffeine metabolism) but under the effective doses for other physiological effects such as antiplatelet effects and vasorelaxant effects to avoid adverse reactions popping up. Rutaecarpine’s most potent effect (lucky for us) is Cyp1a2 induction.” So, there may be something in this, even if at first glance it looks like they’re offering way below the effective dose compared to the rat studies. They offered to send me a sample to try, but my mother always told me not to accept sweets from strangers, so I’ll give that a miss.
Have any Sciencebase readers tried this stuff? Do you think it works? It’s difficult to know what effect it might have given that part of the stimulant effect of coffee and other caffeine-containing drinks is partially psychosomatic (people report feeling pepped up only to discover they were drinking decaff all along). Plasma analysis would definitely demonstrate raised caffeine metabolism regardless though.
Red Ferret and others have been talking about a “herbal” treatment – Rutaesomn – that is supposed to deactivate any caffeine you have had and so help you sleep. Aside from the fact that the marketing says it’s “drug free”, which if it’s physiologically active it cannot be except as a matter of semantics, the research would also suggest that the average person would need far more than is in a single bottle of 30 tablets of the product for it to have any effect.
The active component in Rutaesomn seems to be an alkaloid called rutaecarpine. There is a paper from 2011 in Arch Pharm Res that studied its effects on rats. Apparently, 80 milligrams of the stuff per kilogram of body mass in the lab rats (given each day for three days before administering with caffeine) is enough to raise two liver enzymes sufficiently to promote caffeine metabolism and subsequent excretion of the metabolite. So, there may very well be a mechanism for efficacy.
However, the product contains just 100 milligrams of rutaecarpine per tablet and there are 30 in a bottle. An average adult male human weighing 80 kg and hoping to see an effect would based have to ingest 6400 milligrams of the active ingredient for three days to experience the same relative activity as was observed in the rats. That’s a couple of bottles of the stuff every day for three days before you could have a coffee.
There is the issue of translating from a rat model to humans, however, and ratio of body surface area rather than weight is often used as conversion factor, which would mean that you’d need rather less than my suggested 6400 mg to be taking the equivalent of the rats in the study.
It would be so much easier, if you fancied a good night’s sleep, simply to avoid the double espresso after your evening meal or cut back on the caffeinated “energy drinks”. Surely…