Let me state unequivocally at the outset: I LOVE Think Geek.
This purveyor of hip nerdgear – “Stuff for Smart Masses” – has saved me every Christmas, the occasional birthday, and brought me great personal pleasure with their clever offerings. But most important to me about Think Geek is that I know when giving a gift from them, I am giving someone solid science. A mini Van de Graaff generator. A USB plasma ball. And when my office visitors encounter my LED binary clock, I’m asked, “What the heck is that?”
My next two purchases are likely to be the Pet’s Eye View Digital Camera for the PharmBeagle and the DIY Guitar Pick Punch for me (even though you could buy 80 top-quality guitar picks for the same price).
But I will not be buying Rutaesomn® Sleep Aid – De-caffeinating Chill Pills.
The product is billed as being a pill that speeds metabolism of caffeine from your day-long coffee and energy drink binges. Take it 2-4 hours before you want to go to sleep, “helps get rid of caffeine in your body keeping you awake.”
Well, what is it exactly?
Rutaesomn® is an herbal extract from Evodia rutaecarpa that is also known in Chinese traditional medicine as Wu Zhu Yu where it’s used for alleged weight-loss activity. The biologically-active chemical in the herb is called rutaecarpine.
So, what does this have to do with caffeine?
Well, rutacarpine influences the activity of our major caffeine-metabolizing enzyme called CYP1A2. This is one of a family of over 50 such enzymes that allow us to handle drugs and chemicals we’ve encountered throughout our evolution, including even chemicals that haven’t yet been made.
These CYPs, or cytochrome P450 enzymes, could be thought of as the catalytic converters of the body. You’ll find them mostly in the liver and kidney but almost every cell of your body has some small amount. Most of the time they change chemicals into their less active forms (though there are important exceptions where they make drugs more active or even carcinogenic). Usually, the CYP clips off or modifies a part of the chemical to make it more water-soluble and, therefore, more easily excreted in the urine.
This is how CYP1A2 works to metabolize and inactivate the stimulant activity of caffeine.
But if you do a little reading, you’ll learn that rutaecarpine is an inhibitor of CYP1A2.
Wait a minute.
Doesn’t that mean that rutaecarpine would increase the length of caffeine action in the body?
Wouldn’t taking rutacarpine keep you awake longer after a caffeine binge?
Well, yes, if it’s taken in a high enough dose.
But here’s what I think the makers of Rutaesomn intended: when the body is faced with chemicals that inhibit CYP enzymes in the short-term, it compensates by making more of that very same enzyme after prolonged exposure to that inhibitor. Pretty amazing but it makes sense.
So, if one were to take a high enough dose of rutaecarpine for a few days, one’s CYP1A2 would be “induced.” That means that you’d have a greater capacity for metabolizing caffeine. But again, only if you took enough of it for 3, 4, or 5 days.
But wait. Doesn’t that mean that you’d be metabolizing the caffeine faster all the time, not just at bedtime? Yup.
Let’s recap, with the assumption that the dose of rutaecarpine selected by the manufacturer is actually high enough to have these known biological effects:
1. Taking a single dose of rutaecarpine at bedtime would inhibit the action of CYP1A2. That would cause your day’s worth of caffeine to be metabolized more slowly than normal.
2. Taking several daily doses of rutaecarpine would cause your liver and other organs to make more CYP1A2, increasing the rate at which you metabolize caffeine. This effect doesn’t go away overnight so, over time, you’d be metabolizing caffeine more quickly and requiring greater daily caffeine intake to reach your level of optimum brain stimulation.
My concerns about rutaecarpine inducing CYP1A2 over the long-term don’t even get to the point that this could increase metabolism of other drugs you might be taking, thereby decreasing their effect. Some antidepressants are normally metabolized by CYP1A2. Rutaecarpine is also reported to influence the effectiveness of platelets in blood-clotting, a major issue if one is taking drugs to prevent clots.
So, no offense to our dear geniuses at Think Geek, but I think that this particular product doesn’t hold up to their usual standard of scientific awesomeness.
Nowhere near the catnip-laced blowing bubbles.
Note: The superb British science writer David Bradley had a post on this topic last week at his Sciencebase blog where he drew some commentary by the maker of Rutaesomn.
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