Can Rutaesomn decaf your body? #herbal

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…

via Rutaesomn.

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5 thoughts on “Can Rutaesomn decaf your body? #herbal

  1. Thanks for the additional, detailed response. On a point of semantics. Caffeine is a toxin*. It is an alkaloid present in certain plants as an evolutionary response to attack from pests, it can be lethal to such pests or simply act as a deterrent. Caffeine is toxic at sufficiently high doses in humans. The LD50 is ~150-200 mg/kg (which would mean 100 cups of coffee for the average adult, but still toxic).

    *http://goldbook.iupac.org/T06418.html – Poisonous substance produced by a biological organism such as a microbe, animal or plant.

    As to the artificial stimulation of pilots and truckers…caffeine just happens to be a legal drug, but it is a drug nevertheless, why not let them use cocaine or speed and get them properly alert? Or, better still ensure that labour laws give them adequate rest time in between flights and drives (oh, and make sure they’re not drinking alcohol or smoking dope on or before a journey).

    Regarding healthcare providers, they can often be as ill-informed as the next person. I have had to explain to different GPs on at least two occasions I can recall right now, issues surrounding certain medications and their interaction with another medication of which those GPs were unaware.

    Have you addressed the point about having to take the product prior to drinking the coffee and therefore not benefit from the stimulant effect of the drug in the first place though. At the doses you mention, I still strongly suspect that the product will have minimal effects anyway.

    On a broader note, I am all for consumers being made aware of the facts, however, the profession doesn’t have all the facts, good information on interactions, metabolites and side effects is limited, science is an ongoing process. It also always strikes me as odd that people are quite willing to fill their bodies with countless unproven substances with unknown long-term effects and yet on the other hand will complain about air pollution, for instance. Consumers tend to cherrypick the data to fit with their preconceptions and beliefs. If someone tells them such and such a herb is of benefit, they will seek out the papers that support that view if they’re inclined to take it…I suppose the same might be said of GPs and real pharmaceuticals…

  2. Mathew,

    Thank you for your questions and concerns! We have been continually revamping our FAQ page http://www.rutaesomn.com/facts-about-sleep-aids.html as our primary goal is to provide a safe and effective product. Over the last few weeks due to a multitude of comments and posts we have added more needed information answering people’s questions. A few of your questions are answered there.

    It is important to note that herbal supplements generally do not have every single desired study available especially when compared to the studies birthed from the billions spent on actual prescription drugs. The premise of herbal supplements is as follows:
    “Under the law, manufacturers of dietary supplements are responsible for making sure their products are safe before they go to market. They are also responsible for determining that the claims on their labels are accurate and truthful.” http://www.fda.gov/food/dietarysupplements/consumerinformation/ucm110567.htm

    I encourage you to continue to be an educated consumer as it is important that we are all aware of what we consume. Thank you for your diligence, please feel free to submit any additional concerns or questions to our contact page: http://www.rutaesomn.com/learn-more.html

    This was a great question of yours (One we’ve been asked before, I’ll also add this information to our FAQ):
    “What research has been done on the effect upon the subject of having caffeine rapidly processed? Is it similar to suddenly drinking a few espresso shots, but with the effects compressed into a shorter time frame? Does this increase the risk of heart arrhythmia?”

    When caffeine is metabolized it is broken down into three main compounds: Paraxanthine (84%), Theobromine (12%), and Theophylline (4%). These compounds are then further metabolized and then excreted in the urine. None of these compounds show the strong stimulant effects that caffeine does. Increasing the body’s speed in breaking down caffeine would therefore not increase the potential arrhythmic effects of caffeine and would in fact reduce the stimulant effects of caffeine.

    The other inquiry you had: “Check it out. Note the role of cytokine production in the immune suppressing effects of rutaecarpine.”
    Thanks for bringing this article to our attention. You’ll see that Jeon TW et al conclude that rutaecarpine may decrease antibody forming cells in a dose-dependent matter. The immunosuppressive effects begun slightly at 20mg/kg but were more significant at the 40-80mg/kg. If using the first dose conversion calculation method these doses are all much higher than the rutaecarpine dose in Rutaesomn. If using the second dose conversion calculation that I presented earlier, the low dose (20mg/kg) in mice comes closer to the rutaecarpine dose in Rutaesomn in humans. It is also important to take into account the different routes of administration. This study presents the dose as an IV bolus. Although rutaecarpine shows a chemical structure suggesting good oral bioavailability the IV dose is most likely more potent than an oral dose. It appears that rutaecarpine may cause immunosuppressive effects at higher doses in humans. Our FAQ recommends the max dose of 1 capsule or 100mg of rutaecarpine. As I previously mentioned our target dose is below the pharmacological effects found in the available studies. In the concluding pharagraph of the article you directed me to cited that “the dose (of rutaecarpine) required to show toxicological adverse effects was higher than the range of doses required to show pharmacological effects.”

    As a pharmacist I think it is also important to say that anyone taking any herbal supplement should contact their healthcare provider and inquire how a specific herbal supplement may interact with any current medications or disease states.

    The source we generally like to refer to is Natural Medicines Comprehensive Database. This source is created by Pharmacist’s Letter. Pharmacists letter is an unbiased and unequivocally trusted source for every Doctor of Pharmacy in the nation. Rutaecarpine has appeared in hundreds of products and does not have any reported adverse effects in humans per NMCD. As recommended by the FDA report any adverse effect: http://www.fda.gov/Food/DietarySupplements/Alerts/ucm111110.htm

    **David,
    I’ll first state that I have a bias as I am one of the pharmacists that created Rutaesomn, and I absolutely love my morning cup of coffee :) However, I very much appreciate and understand your view on caffeine. I would disagree that it is a toxin but do agree that consumers should be aware of what they consume and how it effects them, so they can make an informed decision. After excluding those such as myself that enjoy coffee and other caffeinated beverages because we like the taste, we have found Rutaesomn to be helpful in those professionals that require high alertness and attention at any hour such as pilots, night shift doctors, truck drivers, and others. These populations may need the caffeine to be productive, alert, and therefore safe while others rely on their performance. We are excited that we are able to help a potential of millions of people that haven’t had a solution to their restless sleep because of their caffeine intake.

    For our previous conversation I found that it is interesting that your initial dosing calculations are supported by the FDA’s dosing calculator here (This dose does not account for the metabolic rate or BSA conversion ratio’s)http://www.accessdata.fda.gov/scripts/cder/onctools/animalresults.cfm

    Here is an additional article discussing the dosing conversions I initially referred to http://www.fasebj.org/content/22/3/659.full.pdf
    This conflict in dosing supports the importance of the Phase I-III human trials required for FDA approval. The finances required for these studies are unfortunately cost-inhibited for herbal supplement companies.

    As always I respectfully thank you for your time, and appreciate the hard questions that come from your site. Please feel free to contact me anytime.

    -Tim Linnet, Doctor of Pharmacy
    Chief Operational Officer
    Linnet Biopharmaceuticals Inc.
    http://www.rutaesomn.com, http://www.linnetpharm.com

  3. Thanks for pulling up that research Matthew. From the off it never struck me as a good idea to ingest a toxin and then ingest something else to try and accelerate the metabolism of the toxin. Much better to simply avoid the toxin in the first place. No one *needs* to ingest caffeine. It’s not an essential nutrient. Far from it.

  4. None of the marketing copy I’ve seen for this product deals with this study:

    Toxicol Lett. 2006 Jul 1;164(2):155-66. Epub 2006 Jan 18.
    Immunosuppressive effects of rutaecarpine in female BALB/c mice.
    Jeon TW, Jin CH, Lee SK, Jun IH, Kim GH, Lee DJ, Jeong HG, Lee KB, Jahng Y, Jeong TC.
    Source

    College of Pharmacy, Yeungnam University, 214-1, Dae-dong, Gyeongsan 712-749, South Korea. taecheon@yumail.ac.kr

    Check it out. Note the role of cytokine production in the immune suppressing effects of rutaecarpine. Note how other studies mention the role of cytokine in metabolizing caffeine. No one has done any research or tests on this, but it’s possible that caffeine enhances the immune suppressive effects of rutaecarpine. Good news for transplant patients, bad news for everyone else.

    What research has been done on the effect upon the subject of having caffeine rapidly processed? Is it similar to suddenly drinking a few espresso shots, but with the effects compressed into a shorter time frame? Does this increase the risk of heart arrhythmia?

  5. Mr. Bradley,

    I am happy to see your post on Rutaesomn. I would like to take a minute to introduce myself and respond to your comments and questions.

    My name is Tim Linnet, Doctor of Pharmacy and Chief Operational Officer at Linnet Biopharmaceuticals Inc. the creators of Rutaesomn.

    As a pharmacist I very much appreciate your view and skepticism of herbal products as pharmacists come from the same objective perspective.

    In deciding on a dose for Rutaesomn we scoured the available research and did our own studies in the University of the Pacific TJLSF Lab. (http://linnetbiopharmaceuticals.com/academic.html) Our dose target was one that would still be efficacious as well as safe (primarily). Although rutaecarpine has no reported side effects per Pharmacist Letter’s Natural Medicines Comprehensive Database there are quite a few studies showing physiological effects. Primarily we wanted to keep Rutaesomn safe, thus we targeted a dose under the doses used in those studies. After two years of research we are very pleased with how well Rutaesomn works. We have had positive responses from Physicians, Pharmacists, and many others.

    It is also important to note that our dosing conversion calculations differ from those you cited.
    http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm078932.pdf Is a great reference to use. In short when testing in animals an HED or Human Equivalent Dose should be based on BSA or body surface area conversions. After doing these calculations you’ll see that our dose is very near (albeit under) the doses showing efficacy in animal models.
    I enjoyed looking around your blog. It looks like you have excellent qualifications as well as notoriety in the press field.
    We are working hard on improving our Rutaesomn FAQ to include all of the recent press we are getting. This post influenced me to add pertinent information for online researchers on our FAQ which should be updated shortly.

    Tim Linnet, Doctor of Pharmacy
    Linnet Biopharmacetuicals Inc.

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