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Kava Fact of the Day Kava, Caffeine, and CYP1A2

Kapmcrunk

The Kaptain (40g)
KavaForums Founder
56e9c8ecdd08955e538b47db.jpg

(Icey, Public domain, via Wikimedia Commons)

Recently we covered CYP450 enzymes and how kava may inhibit the activity at some of these areas. Today we’re going to focus specifically on the enzyme CYP1A2, and how inhibiting it effects caffeine metabolism.

We’ve seen quite a number of kava drinkers over the years remark about how their morning coffee began to be somewhat more of a stimulating experience. Some kava drinkers find this extra boost a side benefit of drinking kava. Other people experiencing this marked increase in stimulation may find it overpowering.

Caffeine metabolism occurs primarily in the liver, with a half-life of 5 hours, and requires about 8-10 hours to clear entirely. First pass metabolism accounts for 75-80% of caffeine’s metabolism in the body. The enzyme responsible for this is CYP1A2 [1].

Kava has been shown in its different forms to inhibit the enzyme CYP1A2 to varying degrees. In 2005 a study was carried out on kava drinking volunteers. They had the subjects stop drinking kava for 30 days, and measured the metabolic rate of caffeine both prior to and after the break. The caffeine metabolism ratio was shown to increase by 200% after 30 days. This indicated, when consuming kava on a regular basis, that some users can see what feels like DOUBLE the amount of caffeine they’ve ingested. This study also suggested these values return back to normal once kava drinking is stopped [2].

So, kava lovers, if you’ve been drinking your morning coffee and are seeing a definite increase in the stimulatory properties, this could be the culprit as to why.


[1] Institute of Medicine (US) Committee on Military Nutrition Research. Caffeine for the Sustainment of Mental Task Performance: Formulations for Military Operations. Washington (DC): National Academies Press (US); 2001. 2, Pharmacology of Caffeine. Available from: https://www.ncbi.nlm.nih.gov/books/NBK223808/

[2] Cabalion, P., Barguil, Y., Duhet, D., Mandeau, A., Warter, S., Russmann, S., Tarbah, F., & Daldrup, T. (2005). Kava in modern therapeutic uses: To a better evaluation of the benefit/risk relation: researches in New Caledonia and in Futuna. Revista de Fitoterapia, 5(special issue), 53–70.
 

AvaCat

Kava Curious
Thats neat i must be different in though i can still drink a cup or shot of espresso and fall asleep haha.
 

Kapmcrunk

The Kaptain (40g)
KavaForums Founder
Thats neat i must be different in though i can still drink a cup or shot of espresso and fall asleep haha.
Totally normal :)

CYP1A2 is a highly variable enzyme and can be expressed in varying concentrations. This means the kava/coffee combo may be benign to one person while way be overstimulating to the next.

"There is approximately 40% variability in liver expression of the CYP1A2 gene and 60% variability in caffeine metabolism"

Thorn, Caroline F et al. “PharmGKB summary: very important pharmacogene information for CYP1A2.” Pharmacogenetics and genomics vol. 22,1 (2012): 73-7
 

Orz[EST]

Kava Enthusiast
I almost knew it! I posted something like 'coffee is not a potentiator of kava, it seems to be the other way around'.

Now I know it and thanks.
 

Aceofwands9

Kava Enthusiast
This helps explain why i gave up drinking rockstar energy drinks when i started drinking kava and went back to just coffee. I just felt overstimulated and that i didn't need them anymore.
 

Alia

'Awa Grower/Collector
View attachment 11795
(Icey, Public domain, via Wikimedia Commons)

Recently we covered CYP450 enzymes and how kava may inhibit the activity at some of these areas. Today we’re going to focus specifically on the enzyme CYP1A2, and how inhibiting it effects caffeine metabolism.

We’ve seen quite a number of kava drinkers over the years remark about how their morning coffee began to be somewhat more of a stimulating experience. Some kava drinkers find this extra boost a side benefit of drinking kava. Other people experiencing this marked increase in stimulation may find it overpowering.

Caffeine metabolism occurs primarily in the liver, with a half-life of 5 hours, and requires about 8-10 hours to clear entirely. First pass metabolism accounts for 75-80% of caffeine’s metabolism in the body. The enzyme responsible for this is CYP1A2 [1].

Kava has been shown in its different forms to inhibit the enzyme CYP1A2 to varying degrees. In 2005 a study was carried out on kava drinking volunteers. They had the subjects stop drinking kava for 30 days, and measured the metabolic rate of caffeine both prior to and after the break. The caffeine metabolism ratio was shown to increase by 200% after 30 days. This indicated, when consuming kava on a regular basis, that some users can see what feels like DOUBLE the amount of caffeine they’ve ingested. This study also suggested these values return back to normal once kava drinking is stopped [2].

So, kava lovers, if you’ve been drinking your morning coffee and are seeing a definite increase in the stimulatory properties, this could be the culprit as to why.


[1] Institute of Medicine (US) Committee on Military Nutrition Research. Caffeine for the Sustainment of Mental Task Performance: Formulations for Military Operations. Washington (DC): National Academies Press (US); 2001. 2, Pharmacology of Caffeine. Available from: https://www.ncbi.nlm.nih.gov/books/NBK223808/

[2] Cabalion, P., Barguil, Y., Duhet, D., Mandeau, A., Warter, S., Russmann, S., Tarbah, F., & Daldrup, T. (2005). Kava in modern therapeutic uses: To a better evaluation of the benefit/risk relation: researches in New Caledonia and in Futuna. Revista de Fitoterapia, 5(special issue), 53–70.
This is also interesting- from Dec. 2014. Coffee and Liver Health Clinical Gastroenterol: "Over the past 20 years, an increasing number of epidemiological and experimental studies have demonstrated the positive effects of coffee on chronic liver diseases. Coffee consumption has been inversely associated with the activity of liver enzymes in subjects at risk, including heavy drinkers. Coffee favours an improvement in hepatic steatosis and fibrosis, and a reduction in cirrhosis and the risk of hepatocellular carcinoma."
 

faldho

Newbie
This affects caffeine tolerance right? So if you quit Kava for 30 days you would need twice as much caffeine to feel the same?
 

Jacob Bula

Nobody
This is also interesting- from Dec. 2014. Coffee and Liver Health Clinical Gastroenterol: "Over the past 20 years, an increasing number of epidemiological and experimental studies have demonstrated the positive effects of coffee on chronic liver diseases. Coffee consumption has been inversely associated with the activity of liver enzymes in subjects at risk, including heavy drinkers. Coffee favours an improvement in hepatic steatosis and fibrosis, and a reduction in cirrhosis and the risk of hepatocellular carcinoma."
I believe my coffee habits saved my liver during my 20s.
 

Kapmcrunk

The Kaptain (40g)
KavaForums Founder
This affects caffeine tolerance right? So if you quit Kava for 30 days you would need twice as much caffeine to feel the same?
Essentially if you were to get accustomed to the feeling of caffeine and kava together, and you suddenly quit kava, the caffeine would appear to have a higher tolerance value as the enzymatic pathway that kava was suppressing is now available to more quickly metabolize caffeine.
 
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