Medically reviewed by Jessica Pyhtila, PharmD, BCGP, BCPS.
Nutritionally reviewed by Diana Lee, RD.
Do you ever consume caffeine from coffee or a pre-workout supplement in the evening and then regret it later when you’re trying to fall asleep? Rutaecarpine can help. Here we examine its properties, benefits, and effects.
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In a hurry? Here are the highlights:
- Rutaecarpine is an ingredient of the plant evodia rutaecarpa.
- Rutaecarpine effectively negates caffeine, limits its exposure, and expedites its excretion, thus eliminating it from the body faster.
- Rutaecarpine supplementation is safe and useful.
Rutaecarpine Supplement Suggestion: Daily De-CaffeinateTM
What is Rutaecarpine?
Rutaecarpine is one of the main bioactive ingredients of the plant evodia rutaecarpa, the berries of which have a history of usage in Traditional Chinese Medicine for warming, pain reduction, and alleviating GI distress1,2. We’re interested in rutaecarpine primarily for its effects on caffeine – effectively reducing and partially negating its effects – to improve sleep quality and reducing the time it takes to fall asleep3. This effect also applies to the fruit itself (though it only contains a tiny amount of rutaecarpine), but rutaecarpine specifically can be taken in capsule form as a supplement4,5.
- Faster elimination of caffeine.
- Better sleep.
- Useful for those who accidentally consume too much caffeine.
Why not just stop caffeine consumption earlier in the day? Or stop completely?
Let’s address the most obvious question here. Why not just stop caffeine consumption earlier in the day? Or why not stop caffeine consumption completely? Here are some interesting stats:
- The average caffeine intake in 2017 was 190mg per day6.
- 85% of Americans over the age of 2 consume at least 1 caffeinated drink per day7.
- The top 10% of caffeine consumers take in an average 380mg per day7.
It’s also easy to forget that caffeine adds up in popular drinks – and chocolate – that some people consume daily. I’ve included a few caffeine-heavy products like Bizzy Cold Brew Coffee and Red Bull for comparison:
|Product||Volume (fl. oz.)||Caffeine (mg)|
|Bizzy Cold Brew Coffee||8||375|
|Starbucks Cold Brew Coffee||8||100|
|Starbucks Decaf Coffee||8||13|
|Monster Energy Drink||16||160|
|Chick-Fil-A Iced Tea||16||62|
|Dark Chocolate (80% cacao)||1 oz.||23|
|Milk Chocolate||1 oz.||6|
|Chocolate chips, semisweet||1 oz.||14|
Caffeine metabolism varies among different people, but caffeine’s half-life for most people is in the range of 3-7 hours, so evening or even afternoon caffeine can very easily affect the restfulness of your sleep8. This can be particularly problematic for caffeine-naive (non-consumers), caffeine-sensitive (lower dosage threshold), and slow-caffeine-metabolizer (less enzyme activity) populations, for whom rutaecarpine can be a solution.
The benefits of drinking coffee notwithstanding, we can reliably expect that many people rely on caffeine consumption as part of their livelihood. Caffeine consumption is particularly prevalent in and important for populations who work in the evening – shift workers, pilots, truckers, nurses, doctors, etc. Rutaecarpine may be especially useful in these situations.
Mechanisms of Rutaecarpine – How it eliminates caffeine from the body faster
Rutaecarpine’s primary mechanism of action is inducing the activity of the CYP1A2 and CYP2E1 enzymes that break down caffeine.9 Note that any other substance metabolized by these enzymes will also be broken down faster. If you are currently on a medication that interacts with these enzymes, consult your doctor or healthcare practitioner before supplementing with rutaecarpine.
In studies, rutaecarpine’s inhibitory effects on caffeine were seen for all its metabolites as well – paraxanthine, theophylline, and theobromine.3 While there are no studies specifically on humans yet, we know rodents and humans metabolize caffeine similarly, so we would expect the effects on rodents to be the same for humans in this case.
I’ll be anxiously awaiting human trials, but for now, anecdotal evidence abounds from people successfully utilizing rutaecarpine as an anti-caffeine measure. With rutaecarpine, you can now freely reach for that dark chocolate, soda, or coffee in the afternoon and evening without worrying about it disrupting your sleep.
Is Rutaecarpine Safe?
Rutaecarpine supplementation is considered safe. The median lethal dose (LD50) of rutaecarpine in mice is 65mg/kg bodyweight10.
Rutaecarpine Dosage and Timing
Most rutaecarpine supplements use a 100mg dose to be taken about 2-4 hours before bedtime.
Rutaecarpine has a half-life of about 1 hour3.
The main supplement out there right now for rutaecarpine is called Daily De-CaffeinateTM. It was created by a team of pharmacists. Their research team’s lab findings indicated that the requisite CYP1A2 induction for caffeine breakdown was sufficient if taken 2-4 hours before bedtime, which was significantly reduced 12 hours after initial ingestion, so it shouldn’t affect your next-morning coffee fix11.
Rutaecarpine Side Effects
Adverse side effects from rutaecarpine aren’t common, but some people have reported slight dizziness and nausea.
Some things to note:
- The evodia fruit may cause allergic reactions for some people.
- Rutaecarpine negates, limits the systemic exposure of, and expedites the excretion of caffeine; it will not and is not intended to help caffeine withdrawal symptoms.
- Consuming rutaecarpine does not necessarily allow for higher caffeine consumption.
Medical Disclaimer: While I love diving into and extracting useful information from clinical research related to health, fitness, supplements, and more, I am in no way a medical expert. The content on this website is for informational purposes only; it is not professional medical advice, nor is it a substitute for professional medical advice. None of the statements on this website have been evaluated by the FDA. Products mentioned are not intended to diagnose, treat, cure, or prevent any disease. Read my lengthier medical disclaimer here.
- 1.Moon T, Murakami M, Kudo I, et al. A new class of COX-2 inhibitor, rutaecarpine from Evodia rutaecarpa. Inflamm Res. 1999;48(12):621-625. https://www.ncbi.nlm.nih.gov/pubmed/10669112.
- 2.Liao J, Chiou W, Shen Y, Wang G, Chen C. Anti-inflammatory and anti-infectious effects of Evodia rutaecarpa (Wuzhuyu) and its major bioactive components. Chin Med. 2011;6(1):6. https://www.ncbi.nlm.nih.gov/pubmed/21320305.
- 3.Noh K, Seo Y, Lee S, et al. Effects of rutaecarpine on the metabolism and urinary excretion of caffeine in rats. Arch Pharm Res. 2011;34(1):119-125. https://www.ncbi.nlm.nih.gov/pubmed/21468923.
- 4.Tsai T, Chang C, Lin L. Effects of Evodia rutaecarpa and rutaecarpine on the pharmacokinetics of caffeine in rats. Planta Med. 2005;71(7):640-645. https://www.ncbi.nlm.nih.gov/pubmed/16041650.
- 5.Zhou Y, Li S, Jiang R, et al. Quantitative analyses of indoloquinazoline alkaloids in Fructus Evodiae by high-performance liquid chromatography with atmospheric pressure chemical ionization tandem mass spectrometry. Rapid Commun Mass Spectrom. 2006;20(20):3111-3118. https://www.ncbi.nlm.nih.gov/pubmed/16986209.
- 6.U.S. consumers’ reasons for drinking coffee 2017 | Statistic. Statista. https://www.statista.com/statistics/320363/us-consumers–reasons-for-drinking-coffee/.
- 7.Mitchell DC, Knight CA, Hockenberry J, Teplansky R, Hartman TJ. Beverage caffeine intakes in the U.S. Food and Chemical Toxicology. January 2014:136-142. doi:10.1016/j.fct.2013.10.042
- 8.Temple J, Bernard C, Lipshultz S, Czachor J, Westphal J, Mestre M. The Safety of Ingested Caffeine: A Comprehensive Review. Front Psychiatry. 2017;8:80. https://www.ncbi.nlm.nih.gov/pubmed/28603504.
- 9.Ueng Y, Wang J, Lin L, Park S, Chen C. Induction of cytochrome P450-dependent monooxygenase in mouse liver and kidney by rutaecarpine, an alkaloid of the herbal drug Evodia rutaecarpa. Life Sci. 2001;70(2):207-217. https://www.ncbi.nlm.nih.gov/pubmed/11787945.
- 10.Yang X, Zhang H, Li M, Du L, Yang Z, Xiao S. Studies on the alkaloid constituents of Evodia rutaecarpa (Juss) Benth var. bodinaieri (Dode) Huang and their acute toxicity in mice. J Asian Nat Prod Res. 2006;8(8):697-703. https://www.ncbi.nlm.nih.gov/pubmed/17145657.
- 11.Daily De-CaffeinateTM. Daily De-CaffeinateTM. https://dailydecaffeinate.com/.