(Valeriana officinalis) extract comes from a flowering plant native to
Europe and Asia, but is also found in North America.1-3 It is most
commonly used for the treatment of insomnia and anxiety disorders and its use
dates back to the times of ancient Greece and Rome.1,2,4-7 It is also
permitted or considered an acceptable option for sleep related disorders in the
U.K. (Medicines Control Agency), Canada (Health Canada), Australia (Therapeutic
Goods Administration), Germany (Commission E) and France.3,8,9 Valerian
comes in a number of dosage forms (dried root, tincture, and fluid extract) and
contains bornyl acetate, sesquiterpenoids (valerenic acid, acetoxyvalerenolic
acid) and some lipophilic iridoids called valepotriates.10 While the
specific ingredient responsible for the activity of valerian has not been
identified, it is thought that a combination of sesquiterpenoids and
valepotriates may be involved in its mechanism of action.8,10 According
to the National Sleep Foundation, over 50% of American adults experience one or
more symptoms of insomnia at least a few nights a week.11 In addition,
self-treatment of various problems by patients (especially with the use of
natural or herbal medicines) is on the rise across the world.12-14
Therefore, there is a good chance patients will consider the use of valerian to
treat their sleep related problems.
How does valerian work to
improve sleep problems or insomnia?
of the oldest and most commonly prescribed treatments for insomnia are the
benzodiazepines (e.g., diazepam, alprazolam).15 Simply stated, the
mechanism of action of valerian is similar to that of benzodiazepines.16,17
As it relates to insomnia, benzodiazepines are known to hasten sleep onset,
decrease nocturnal awakenings, and increase total sleep time.15 Benzodiazepines
do this by increasing, or potentiating, the binding of the major inhibitory
neurotransmitter, gamma-aminobutyric acid (GABA) to the GABA-A receptor.18
GABA-A receptors, found in the CNS, are most commonly made up of a combination
of 5 protein subunits (2-alpha, 2-beta, and 1-gamma).18 In the absence of
a benzodiazepine, GABA will weakly bind to the alpha subunit on the GABA-A
receptor and allow the negatively charged chloride to diffuse into the neuron.
However, in the presence of a benzodiazepine, the benzodiazepine will
allosterically bind to the gamma subunit on the GABA-A receptor, which causes
GABA to bind to the alpha subunit more effectively than before.18 This
causes a greater movement of chloride into the neuron, thereby causing the
neuron to be hyperpolarized (more negatively charged inside the cell as
compared to outside the neuron; from -70 mV to about -80 mV). This now
makes the neuron less responsive to stimulation by excitatory postsynaptic
potentials (EPSPs), thus suppressing the CNS. As stated before, the
mechanism of action of valerian is similar to that of a benzodiazepine;
however, instead of binding to the gamma subunit like a benzodiazepine, it
appears to bind to the beta subunit on the GABA-A receptor.17 Regardless,
it has the same effect on chloride movement into the neuron resulting in a
hyperpolarized state. In addition, valerian has also been shown to
decrease the removal or metabolism of GABA thereby increasing the likelihood
that GABA will bind to its receptor and elicit the effects described above.19
the clinical trial evidence suggests that valerian may be useful for treating
insomnia; however, there is a lack of well designed clinical trials that
support this claim or provide evidence of its long-term efficacy and safety
(i.e., beyond 4 to 6 weeks).1,2,4-7 Regardless, the side effect profile
of valerian seems to be tolerable with headaches, dizziness, and GI
disturbances being the most common complaints, though not significant.1-7
There is insufficient data to accurately determine if the physical dependency
commonly seen with benzodiazepines or the effects of alcohol are potentiated
with valerian use. However, due to its known mechanism of action and the
lack of long-term data, caution is warranted until proven otherwise.
Common doses of 300 to 400 mg of standardized extract (containing at least 0.5%
essential oil) at bedtime may be seen for the treatment of insomnia.20
- National Center for Complementary and Alternative Medicine:
National Institutes of Health. Herbs at a glance: Valerian. Last
accessed on 2-14-2009.
- National Institutes of Health: Office of Dietary Supplements. Valerian.
Bethesda, Maryland. Version: 1/16/2008. Last accessed on 2/14/09.
- Health Canada. Natural Health Products. Valerian. March 30, 2007. Last accessed on 2-14-2009.
F, Quispe S, Diefenbach K et al. Critical evaluation of the effect of
valerian extract on sleep structure and sleep quality.
- Stevinson C, Ernst E. Valerian for insomnia: a systematic review of randomized clinical trials. Sleep Med 2000;1:91-9.
G, Ploch M, Miettinen-Baumann A et al. Efficacy and tolerability of
valerian extract LI 156 compared with oxazepam in the treatment of
non-organic insomnia - a randomized, double-blind, comparative clinical
study. Eur J Med Res 2002;7:480-6.
- Miyasaka LS, Atallah AN, Soares BG. Valerian for anxiety disorders. Cochrane Database Syst Rev 2006;18:CD004515.
- Ebadi M. Valerian. In: Pharmacodynamic basis of herbal medicine. 2nd Ed. Taylor & Francis Group. Boca Raton, FL. 2007:599-609.
Goods Administration. Department of Health and Ageing: Australian
Government. Substances that may be used in listed medicines in
Australia. Version 12/2007. Last accessed on 2/14/2009.
M, Franz G. Stability control of valerian ground material and
extracts: a new HPLC-method for the routine quantification of valerenic
acids and lignans. Pharmazie 2004;59(6):446-52.
- National Sleep Foundation. Sleep-related problems: Insomnia and sleep. Last accessed on 2/14/2009.
- World Health Organization. Traditional medicine fact sheet. Revised last on December 2008. Last accessed on 2/14/2009.
Center for Complementary and Alternative Medicine: National Institutes
of Health. The Use of complementary and alternative medicine in the
United States: 2007 National Health Interview Survey Report. Last
accessed on 2/14/2009.
Canada. Natural Health Products. Baseline natural health products
survey among consumers, March 2005. Last accessed on 2-14-2009.
A, Sloan R. Benzodiazepines and related drugs for insomnia in
palliative care. Cochrane Database Syst Rev 2002;4:CD003346.
T, Bernasconi P, Bombardelli E et al. In vitro study on the
interaction of extracts and pure compounds from Valeriana officinalis
roots with GABA, benzodiazepine and barbiturate receptors. Fitoterapia
- Benke D, Barberis A, Kopp S et
al. GABA(A) receptors as in vivo substrate for the anxiolytic action
of valerenic acid, a major constituent of valerian root extracts.
- Raffa RB, Rawls SM, Beyzarov EP. Chapter 3: Drugs Used in Disorders of the Central Nervous System and Treatment of Pain. In: Netter's Illustrated Pharmacology. Elsevier Inc. Philadelphia, PA. 2005:57-67.
- Gabel TG. Chapter 11: Herbal Medications, Neutraceuticals, and Anxiety and Depression. In: Herbal Medicinals: A Clinicians Guide. Miller LG, Murray WJ eds. Pharmaceutical Products Press. New York, NY. 1998:209-10.
- Inhibition of gamma-aminobutyric acid catabolism by valerenic acid derivatives. Planta Med 1982;46:219-20.