Entourage Effect - Part 2.....3?
Short one today, kava lovers. I’m squeezing in a little research here and there between phone calls.
Today’s fact of the day will be addressing kavain yet again. Kavain seems to be the kavalactone which is most focused on in studies. Kavain has been seen as a positive allosteric modulator of GABA-A, and a negative allosteric modulator of glycine [1]. In a study from 2005 researchers sought to understand the pharmacokinetics of kavain in relation to consumption of full spectrum extracts vs kavain on its own.
Kavain and full spectrum kava extract were fed to rats. Single dose oral administration of kavain combined with full spectrum kava extract caused the increase in peak concentration (C_Max) to DOUBLE compared with isolated kavain. Mean time to reach these peak plasma concentrations TRIPLED. Kavain AUC (Area under curve) was found 3 times higher following coadministration. It was also found that kavain was more slowly eliminated when combined with full spectrum extract, and researchers theorize that the modification of metabolism times from other kavalactones may be the culprit of this drug-drug interaction [2]. Essentially full spectrum application of kavalactones were seen to positively modulate the oral bioavailability and metabolization of kavain, further adding to the idea that an entourage effect is in play with kava.
[1] Volgin, Andrey, Longen Yang, Tamara Amstislavskaya, Konstantin Demin, Dongmei Wang, Dongni Yan, Jingtao Wang, et al. 2020. “DARK Classics in Chemical Neuroscience: Kava.” ACS Chemical Neuroscience, January.
(https://doi.org/10.1021/acschemneuro.9b00587)
[2] Mathews, James M., Amy S. Etheridge, John L. Valentine, Sherry R. Black, Donna P. Coleman, Purvi Patel, James So, and Leo T. Burka. 2005. “Pharmacokinetics and Disposition of the Kavalactone Kawain: Interaction with Kava Extract and Kavalactones in Vivo and in Vitro.” Drug Metabolism and Disposition: The Biological Fate of Chemicals 33 (10): 1555–63.
(https://doi.org/10.1124/dmd.105.004317)
Short one today, kava lovers. I’m squeezing in a little research here and there between phone calls.
Today’s fact of the day will be addressing kavain yet again. Kavain seems to be the kavalactone which is most focused on in studies. Kavain has been seen as a positive allosteric modulator of GABA-A, and a negative allosteric modulator of glycine [1]. In a study from 2005 researchers sought to understand the pharmacokinetics of kavain in relation to consumption of full spectrum extracts vs kavain on its own.
Kavain and full spectrum kava extract were fed to rats. Single dose oral administration of kavain combined with full spectrum kava extract caused the increase in peak concentration (C_Max) to DOUBLE compared with isolated kavain. Mean time to reach these peak plasma concentrations TRIPLED. Kavain AUC (Area under curve) was found 3 times higher following coadministration. It was also found that kavain was more slowly eliminated when combined with full spectrum extract, and researchers theorize that the modification of metabolism times from other kavalactones may be the culprit of this drug-drug interaction [2]. Essentially full spectrum application of kavalactones were seen to positively modulate the oral bioavailability and metabolization of kavain, further adding to the idea that an entourage effect is in play with kava.
[1] Volgin, Andrey, Longen Yang, Tamara Amstislavskaya, Konstantin Demin, Dongmei Wang, Dongni Yan, Jingtao Wang, et al. 2020. “DARK Classics in Chemical Neuroscience: Kava.” ACS Chemical Neuroscience, January.
(https://doi.org/10.1021/acschemneuro.9b00587)
[2] Mathews, James M., Amy S. Etheridge, John L. Valentine, Sherry R. Black, Donna P. Coleman, Purvi Patel, James So, and Leo T. Burka. 2005. “Pharmacokinetics and Disposition of the Kavalactone Kawain: Interaction with Kava Extract and Kavalactones in Vivo and in Vitro.” Drug Metabolism and Disposition: The Biological Fate of Chemicals 33 (10): 1555–63.
(https://doi.org/10.1124/dmd.105.004317)