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Refresher - Kava does NOT act as a benzodiazepine.

Kapmcrunk

The Kaptain (40g)
KavaForums Founder
Kava is not a benzodiazepine.
When we say kava doesn't act as a benzodiazepine, this is what we reference when we say this. In this 2016 study authors Chua et al were working to elicit which subunits of the GABA-A complex that kavain was positively modulating. An interesting study, however we'll be focusing on just one specific part of it, and that is effects seen even in the presence of flumazenil (brand name Romazicon).

We should define what flumazenil is as a drug.

Standard prescription benzodiazepine brand names are Xanax, Valium, and Klonopin among others. Flumazenil is a benzodiazepine antagonist (reversal agent) that is used for the complete or partial reversal of the sedative effects caused by benzodiazepines. It’s the first line treatment in cases of benzodiazepine overdose and toxicity. This drug works by binding to, but not activating the site on GABA-A to which benzos attach. This site is known as the allosteric BZP site.

Chua et al went about testing normalized responses from the GABA-A receptor in the presence of a number of different combinations of compounds. These compounds were Kavain, Flumazenil, Diazepam (Valium), and the neurotransmitter GABA. You can see in the included figure that Flumazenil cancels out the effects of diazepam. This is clear when we look at GABA only normalized response vs. GABA, Diazepam, and Flumazenil. In the combination of all three we see the same response as if GABA alone had been administered, underscoring the cancellation of effects from diazepam.

Kavain was administered in combination with GABA, and again with GABA, and Flumazenil. The figure shows that the normalized response only varies slightly between GABA + Kavain and GABA, Kavain and Flumazenil. This indicates that kavain’s modulatory properties are unaffected by the presence of flumazenil. This also gives direct evidence that kavain does not function as a benzodiazepine, as effects at this allosteric site are required for downregulation of subunits and hence withdrawal and tolerance are absent. While kavain was shown in this study, other studies have been performed in the presence of full spectrum extract and flumazenil with identical results (Garrett et al 2003, Shinomiya et al 2005).

Chua, Han Chow, Emilie T. H. Christensen, Kirsten Hoestgaard-Jensen, Leonny Y. Hartiadi, Iqbal Ramzan, Anders A. Jensen, Nathan L. Absalom, and Mary Chebib. 2016. “Kavain, the Major Constituent of the Anxiolytic Kava Extract, Potentiates GABAA Receptors: Functional Characteristics and Molecular Mechanism.” PloS One 11 (6): e0157700. https://doi.org/10.1371/journal.pone.0157700.

Garrett, Kennon M., Garo Basmadjian, Ikhlas A. Khan, Brian T. Schaneberg, and Thomas W. Seale. 2003. “Extracts of Kava (Piper Methysticum) Induce Acute Anxiolytic-like Behavioral Changes in Mice.” Psychopharmacology 170 (1): 33–41. https://doi.org/10.1007/s00213-003-1520-0

Shinomiya, Kazuaki, Toshio Inoue, Yoshiaki Utsu, Shin Tokunaga, Takayoshi Masuoka, Asae Ohmori, and Chiaki Kamei. 2005. “Effects of Kava-Kava Extract on the Sleep-Wake Cycle in Sleep-Disturbed Rats.” Psychopharmacology 180 (3): 564–69. https://doi.org/10.1007/s00213-005-2196-4
 

Kapmcrunk

The Kaptain (40g)
KavaForums Founder
Perhaps in the future they investigate other major kavalactones, too.
This is actually further down in the line in research regarding flumazenil and kava's effects. Full spectrum extract also continued to exert its effects during and after Flumazenil administration.
 

Orz[EST]

Kava Enthusiast
This is great news! I wonder if there is a similar distinction in comparison to alcohol.
Alcohol has noradrenaline reuptake inhibitor properties that characterize moderate (or heavyish-moderate) blood alcohol concentration (energizing).

Kava may have a a stimulant component that is not at the forefront.
 

Hermes

Kava Curious
Thanks for this. I find it useful to read the science. As a layman who self-medicated with the tranquilizer clonazepam 18 years ago in a country with a candystore of pharmaceuticals, I can draw life experience comparisons. Although effective for eliminating chronic insomnia in the very short-term, my hangover from Klonapin was huge. Furthermore, my sleep, while unconscious, was not truly restful. In fact the 'sleep' on one occasion was so heavy that someone entered my home and removed a DVD player eight feet from my head looping the theme song from 'Sedotta e abbandonata', without my waking. So, clonazepam is like being hit over the head. Kava more like a shoulder massage. Is kava being considered as a harm reduction therapy anywhere in the world?
 
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