04/30/2026
About one in ten people who take valerian to sleep get wired instead and I have seen this clinically and may herbalists report seeing the same thing … I have a friend that becomes full of rage and super irritable. This is most likely why when you look at studies on valerian and it’s effects on sleep you get a lot of “inconclusive” or contradictory results and I want to talk about why that happens, because the mechanism is pretty cool and it connects a common physiological response to a whole class of drugs and herbs. But can also help us to utilize valerian more effectively.
King's American Dispensatory in 1905 talk about valerian as a "stimulant-tonic" but it’s dose dependent - we will get to that in a minute!
Valerian's main active compound, valerenic acid, is a positive modulator of GABA-A receptors — GABA being your nervous system's main calming neurotransmitter system. But GABA-A receptors aren't built the same in everybody and in people with a specific GABA A receptor configuration valerian won’t necessarily be calming… especially in larger doses…
This is a common effect of many GABA-A receptor positive allosteric modulators like progesterone, alcohol and benzodiazepines which also have a recognized "paradoxical agitation" phenomenon. It's a U-shaped (biphasic) dose-response curve.
So the paradoxical response isn't a freak occurrence it's a feature of this whole class of compounds, and it's tied to which subunits an individual's GABA-A receptors are made of.
If valerian wires you up there are a lot of beautiful nervines that work through different mechanisms passionflower (it’s has a broader action on the GABA system as a whole), hops, California poppy, skullcap, kava. You don't have to force a relationship with a plant whose chemistry doesn't match yours.
If you want to learn this kind of cool stuff about herbalism all the time check out the Herbal Medicine Monthly Subscription where I deep dive into one plant per month. Link's in the bio if you want to come learn with us
Shinjyo, N., Waddell, G., & Green, J. (2020). Valerian Root in Treating Sleep Problems and Associated Disorders—A Systematic Review and Meta-Analysis. Journal of Evidence-Based Integrative Medicine. (60 studies, n=6,894. Cites the 1905 King's American Dispensatory description of valerian as a "stimulant-tonic.")
Benke, D., et al. (2009). GABA-A receptors as in vivo substrate for the anxiolytic action of valerenic acid, a major constituent of valerian root extracts. Neuropharmacology. (Demonstrated that β3-containing GABA-A receptors are the major substrate for valerian's anxiolytic action.)
Khom, S., et al. (2007). Valerenic acid potentiates and inhibits GABA-A receptors: Molecular mechanism and subunit specificity. Neuropharmacology. (Valerenic acid is β2/β3 subunit-selective and biphasic — potentiates at low concentrations, inhibits at high concentrations.)
Bäckström, T., et al. (2014). Allopregnanolone and mood disorders. Progress in Neurobiology. (PMDD patients show altered GABA-A receptor sensitivity; α4 and δ subunit changes drive paradoxical anxiogenic effects of allopregnanolone.)
Taibi, D. M., et al. (2009). A randomized clinical trial of valerian fails to improve self-report, polysomnographic, and actigraphic sleep in older women with insomnia. Sleep Medicine. (Peer-reviewed acknowledgment of paradoxical stimulation as a recognized clinical effect.)
For educational purposes only—this content is not medical or clinical advice and is not intended to diagnose, treat, cure, or prevent any disease. I do not provide individualized recommendations or advise stopping or replacing medications, and no practitioner–client relationship is formed.
I am an herbalist, not a medical doctor—always consult a licensed healthcare provider before making health decisions or using herbs. Herbal use carries risks, including side effects, allergic reactions, and interactions, and plant identification is for educational purposes only—always verify before use. To the fullest extent permitted by law, I disclaim liability for any loss, injury, or damage resulting from the use or reliance on this content.