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De-caffeinating pills? Say it ain’t so, Think Geek

Let me state unequivocally at the outset: I LOVE Think Geek.

Love.

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?

Evodia rutaecarpa (Boymia rutacarpa when this was drawn in 1870.) Credit/Philipp Franz von Siebold and Joseph Gerhard Zuccarini, Public domain, via Wikimedia Commons.

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.

9 Comments

  • May 18th 201208:05
    by Scicurious

    Reply

    Walkin’ around inhibiting liver enzymes?!?! This sounds like a completely horrible idea. I am sad that the makers of my beloved caffeinated gum are selling this.

    Also, it seems like a bit of a round about way to de-caffeinate, having to wait several days to increase liver enzyme production, if that even has the desired effect…why not sell a competitive adenosine 1A agonist? I don’t think it’d be 100 percent effective, but it’s be better.

  • May 18th 201208:05
    by Brandon the Engineer

    Reply

    This sounds like all types of bad. Just as well start hooking up buttons to our bodies to turn us on, off, overclocked, and sleep. Drugs are turning us into living computers.

  • May 18th 201208:05
    by David Bradley

    Reply

    I was just about to post a comment to say I’d had some info from the manufacturers when I spotted your flattering footnote, you meke me blush…

  • May 19th 201210:05
    by stan linnet

    Reply

    Effects of Rutaecarpine on the Metabolism and Urinary Excretion of
    Caffeine in Rats
    Keumhan Noh
    1
    , Young Min Seo
    1
    , Sang Kyu Lee
    1
    , Sudeep R. Bista
    1
    , Mi Jeong Kang
    1
    , Yurngdong Jahng
    1
    ,
    Eunyoung Kim2
    , Wonku Kang
    1
    , and Tae Cheon Jeong
    1
    1
    College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Korea and
    2
    College of Pharmacy, Chungnam National
    University, Daejeon 305-764, Korea
    (Received May 14, 2010/Revised August 2, 2010/Accepted September 5, 2010)
    Although rutaecarpine, an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa, has been reported to reduce the systemic exposure of caffeine, the mechanism of this
    phenomenon is unclear. We investigated the microsomal enzyme activity using hepatic S-9
    fraction and the plasma concentration-time profiles and urinary excretion of caffeine and its
    major metabolites after an oral administration of caffeine in the presence and absence of
    rutaecarpine in rats. Following oral administration of 80 mg/kg rutaecarpine for three consecutive days, caffeine (20 mg/kg) was given orally. Plasma and urine were collected serially for
    up to 24 h and the plasma and urine concentrations of caffeine and its metabolites were measured, and compared with those in control rats. 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.
    Key words: Caffeine, Metabolites, Rutaecarpine, Cytochrome P450, Rat
    here is an independent source confirming rutaecarpine is a cyp1a2 inducer.(which is what david bradley reported)
    the studies we did with university of pacific showed the half life of rutaecarpine was around 4 hours.
    as a skeptical pharmacist myself i am continually amazed with rutaesomn positive efficacy. it really works.
    safety concern with fruit derived ingredient? people taking other medications should not take rutaesomn without first consulting their health care provider.

    • Aug 16th 201220:08
      by worlebird

      Reply

      Re: the study posted by stan linnet
      Doesn’t the study you posted say exactly what David is saying in this blog? The rats were not fed caffeine all day, and then fed some rutaecarpine and then tested. Rather, to quote your post, “Following oral administration of 80 mg/kg rutaecarpine for three consecutive days, caffeine (20 mg/kg) was given orally.” So the rats were fed rutaecarpine for 3 days first, then given caffeine and tested. That’s exactly the kind of effect David is writing that one might expect. It is NOT, however, the effect that the pills are being advertised with. The study emphatically does NOT demonstrate efficacy for the action being advertised, and the actual efficacy demonstrated by the study is probably undesirable to most consumers. In summary, it is likely that the effects being experienced by consumers who give testimonials (“It really works!”) are placebo effects, something that can (and should) be tested.

  • May 19th 201210:05
    by stan linnet

    Reply

    terra sigillata and david bradley are more than welcome to request samples of rutaesomn from our website and try our product. i love talking to brilliant scientists about our product (but still a little intimidated).still enjoying the wow moment when they find out that rutaesomn really works.

  • May 30th 201211:05
    by Jon

    Reply

    Gotta love ThinkGeek. I’ve bought numerous Christmas and birthday gifts for other people. Every year they get more fun and useless toys for my desk and others.

  • Jun 8th 201218:06
    by Julie

    Reply

    I just ordered a father’s day gift from that web site. Thanks

  • Sep 26th 201221:09
    by fitness guy

    Reply

    Funny how we see things that are supposed to fix a problem can actually do the opposite when looked at in real life situations.

    I am very sensitive to caffeine and do not drink any after noon at all or it does in fact keep me up. I would have in retrospect tried this and gotten myself in big sleep problems

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