Increasing Caffeine Clearance With Herbs/supps (Cyp1A2 Activity)

dazdaz today is a good day ✭✭✭

hi all,


I'm interested to know if we can speed up caffeine clearance from the blood by ingesting a 'pill' (or consuming a herb).


On the face of it ('google research'), one way to do this could possibly be to increase the activity of Cytochrome P450 1A2 (CYP1A2).


If we look at the CYP1A2 wiki page here, one candidate listed as an inducer is Echinacea,

but when you actually read the reference study on pubmed, it actually seems to do the opposite;

quote: "Echinacea dosing significantly reduced the oral clearance of caffeine" & "Echinacea (E purpurea root) reduced the oral clearance of substrates of CYP1A2"


Another potential candidate mentioned (google again) was Ginkgo Biloba, but the consensus (new studies i think?), seem to show G.Biloba has no effect on CYP1A2.


So that's as far as i've got at the moment.


Hopefully some of you good peeps will have more to offer.  Thanks All.


fake it till you make it


  • John BrissonJohn Brisson The Legend Formerly Known as Ron Swanson ✭✭✭
    edited November 2014

    Increasing liver function should in turn increase the metabolism of caffeine, so milk thistle, increasing glutathione, same ol song and dance should work.

    My book Fix Your Gut, is offered on Amazon for $9.99.


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  • dazdaz today is a good day ✭✭✭
    edited February 2016

    I've just started to look at L-Theanine...

    ...not related to my thread title; 'CYP1A2 Activity' , but may achieve my desired result...

    ie. offset or nullify any effects of caffeine that linger in to the evening/night and impair sleep  

    fake it till you make it

  • dazdaz today is a good day ✭✭✭
    edited February 2016

    When rutaecarpine (active indole in Evodia) is fed to rats, the AUC and Cmax values of Caffeine are significantly reduced; meaning rutaecarpine can reduce the exposure of caffeine to the body.[66][67] This also extends to the similar xanthine compound theophylline.[68] These effects extend to consumption of Evodia itself, and combination decoctions such as Wu Zhu Yu Tang.[67] 


    This effect is rather significant; pretreatment of 80mg/kg oral Rutaecarpine daily for 3 days (a high dose, but its bioavailability is unaugmented) in rats reduced the Cmax to 31% of the control group, the Tmax to 22%, the AUC to 5% of control, and reduced the half-life from 0.73+/-0.07 hours to 0.27+/-0.1 hours.[66] Similar trends were seen for all metabolites of caffeine (paraxanthine, theophylline, theobromine) 


    Rutaecarpine is able to induce (increase) activity of various hepatic enzymes such as CYP1A2, CYP2B, and CYP2E1;[28][69] CYP2E1 induction is seen at 80mg/kg oral ingestion in rats while only 20mg/kg is needed for CYP1A2.[67] As Caffeine is highly metabolized by CYP1A and CYP2E1, their increased activity causes greater metabolism of caffeine in a shorter time frame and thus limits systemic exposure.  

    Rutaecarpine appears to potently suppress the circulating levels of caffeine via increasing hepatic and intestinal degradation; a highly antagonistic compound

    fake it till you make it

  • dazdaz today is a good day ✭✭✭
    edited February 2017

    Dropping an activated charcoal capsule (or 'two') with your coffee could perhaps reduce the absorption of the caffeine.
    (may sound a bit pointless, but if it works, there could be situations for it).

    fake it till you make it

  • jcg3jcg3 ✭✭✭

    Why are you trying to increase the clearance of caffeine?

    I think exercise would work, or generally high activity, but not sure if that would be significant or timely.

    I know grapefruit will do the opposite - slow down clearance by slowing down liver phase 1 detox (I think it's phase 1). So avoid GSE...

    I haven't noticed theanine increasing caffeine clearance, but it can certainly calm down excitation. Theanine is an amino acid that promotes gaba, so it's mostly balancing the excitation with an inhibitory effect.

    Caffeine works by blocking adenosine receptors. Not sure what could counter that. Alternatively, you could consider melatonin or 5-htp or tryptophan to induce sleepiness via a different mechanism...

  • dazdaz today is a good day ✭✭✭

    @jcg3 said:
    Why are you trying to increase the clearance of caffeine?

    "offset or nullify any effects of caffeine that linger in to the evening/night and impair sleep"

    fake it till you make it

  • jcg3jcg3 ✭✭✭


    For extreme overdose an ER might use activated charcoal, stomach pumping.

    "Some home treatments for caffeine overdose include drinking water, mild exercise, and eating foods high in potassium or magnesium, such as bananas or dark leafy greens."

    I'm not sure (and curious) how the mg or k would help metabolize the caffeine.

    Rather than use activated charcoal with your coffee, why not drink decaf? I will also make coffee weaker if I'm making it later in the afternoon... less beans, less extraction time, water it down, etc.

  • jcg3jcg3 ✭✭✭

    Nevermind - dumb comment. I've had too much coffee and couldn't sleep before. We're not always proactive enough to avoid it... you're just asking what some options are when it happens...

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