Articles

Valerian

Plant Part Used

Root

Active Constituents

Volatile oils (including isovalerenic and valerenic acid), iridoids (valerenic acid).(1),(2),(15)

[span class=alert]This section is a list of chemical entities identified in this dietary supplement to possess pharmacological activity. This list does not imply that other, yet unidentified, constituents do not influence the pharmacological activity of this dietary supplement nor does it imply that any one constituent possesses greater influence on the overall pharmacological effect of this dietary supplement.[/span]

Introduction

Valerian has been used for centuries as an agent to soothe the nervous system in response to stress. It has been reported that valerian helps improve sleep quality.(3),(4),(5) Although other agents have been introduced in recent years which offer similar benefits, valerian is still one of the most popular herbal preparations on the market and is widely used throughout Europe.

Interactions and Depletions

Interactions

  • Barbiturates
  • Antidepressants
  • Anti-anxiety medications;a case report described an interaction between a patient using lorazepam in conjunction with a valerian/passionflower combination.(16) Handshaking, dizziness, throbbing and muscular fatigue were reported, possibly through increased GABA leading to secondary effects.
  • Sedative and hypnotic medications
  • Haloperidol; A laboratory animal study found increased hepatic oxidative stress when using valerian and haloperidol concomitantly.(17) An earlier animal study found no effect when using haloperidol and valerian.(18)

Dosage Info

Dosage Range

200mg (standardized extract), 1-4 times a day

-OR- total daily dose not to exceed 800mg (standardized extract) daily.

Tea: Use 3-5 grams dried root and steep for 10-15 minutes in 240ml (one cup) hot water, 2 times daily and before bedtime.(6)

Liquid Extract (1:4w/v): 15 to 20 drops in water 2-3 times daily.(6)

Most Common Dosage

200mg (standardized extract), 2 times a day.

Stress: 200mg (standardized extract), 3 times a day.

Insomnia: 200-400mg (standardized extract) at bedtime.

Tea: Use 3 grams dried root and steep for 10-15 minutes in 240ml (one cup) hot water, 2 times daily and before bedtime.

Liquid extract (1:4w/v): Use 15 drops in water 2-3 times a day.

Standardization

[span class=doc]Standardization represents the complete body of information and controls that serve to enhance the batch to batch consistency of a botanical product, including but not limited to the presence of a marker compound at a defined level or within a defined range.[/span]

The most current available medical and scientific literature indicates that this dietary supplement should be standardized to 0.8% valerenic acids.

Uses

Frequently Reported Uses

  • Insomnia
  • Anxiety/Stress/Relaxation

Other Reported Uses

  • Nervous Symptoms Associated With Menopause And PMS
  • Hyperexcitability
  • Restless Leg Syndrome
  • Motor Agitation
  • Nighttime Cough
  • Anticonvulsant

Toxicities & Precautions

General

No known toxicities in recommended doses.

Avoid large doses and extended use.

Use with caution when drinking alcohol, driving a car or operate machinery while taking valerian.(7),(8)

If morning sleepiness occurs, the dose should be reduced.

Pregnancy/ Breast Feeding

If pregnant or nursing, consult a physician before use.

Age Limitations

Do not use in children under 3 years of age unless recommended by a physician.

NOTE - only use valepotriate and baldrinal free valerian in children under 12 years of age due to potential mutagenic properties.

Pharmacology

The usefulness of valerian is reported to be due to several principal components, including valepotriates, valerenic acid, and pungent oils which have a sedative effect on the central nervous system, as well as a relaxing effect on the smooth muscles of the GI tract.(9),(10) It is felt that both valepotriates and valeric acid bind to receptor sites similar to the benzodiazepines.(11) Valerian’s constituents reportedly influence gamma-aminobutyric acid (GABA-A) activity through affinity for receptors in the brain.(12),(19) It has been reported that the content of valerenic acid is related to GABAA receptor modulation.(20) Valerian does not have the same morning drug hangover effect as seen with some benzodiazepines.(4) Laboratory animal studies support the anxiolytic and sedative effects of valerian.(21)

Systematic reviews of valerian for sleep have found inconsistent and inconclusive results.(22) A small human study in 16 women (av. Age 69.4) found that valerian extract (300mg) did not improve insomnia after 2 weeks when compared to placebo.(23) A televised, web-based randomized trial followed 405 people aged 18-75 years while taking valerian extract for a 2 week period.(24) The authors concluded that valerian appears to be safe, but with modest beneficial effects at most on insomnia compared to placebo.

Valerian is commonly combined with other relaxing herbs (such as hops, passionflower, lemon balm, chamomile) in formulas for increased results in sleep and stress. A single dose of a combination of valerian and hops (Humulus lupulus) was reported in a small, double blind, randomized, placebo-controlled sleep study to improve sleep latency.(25) Another 4 week, randomized, double blind, placebo-controlled, prospective clinical study found a valerian/hops combination improved sleep latency superior to placebo and valerian alone.(26) Valerian and lemon balm (Melissa officinalis) are reported in human studies effective in promoting rest and sleep and decreasing anxiety when used in combination.(27),(28)

A small human study found valerian improved the symptoms of restless leg syndrome (RLS) and decreased daytime sleepiness in patients that report an Epworth Sleepiness Scale (ESS) score of 10 or greater.(29)

Studies have found that valerian extract when administered to healthy volunteers was not mood-altering or did not have psychomotor/cognitive effects. Because of fewer side effects, valerian could prove to be a less troublesome alternative to drugs in the treatment of insomnia.(13),(14)

Anticonvulsant activity has been reported In laboratory animal studies when using valerian, in part mediated through activation of the adenosine system.(30) Valerian has also been reported in a laboratory study to have a cytoprotective effect using a Parkinson’s disease model.(31)

References

  1. View Abstract: Tittel G, et al. High-performance Liquid Chromatographic Separation and Quantitative Determination of Valepotriates in Valeriana Drugs and Preparations. J Chromatogr. 1978;148(2):459-68.
  2. View Abstract: Leuschner J, et al. Characterisation of the Central Nervous Depressant Activity of A Commercially Available Valerian Root Extract. Arzneim-Forsch/Drug Res. 1993;43(6):638-41.
  3. View Abstract: Lindahl O, Lindwall L. Double Blind Study of Valerian Preparations. Pharmacol. Biochem. Behav. 1989;32(4):1065-66.
  4. View Abstract: Leathwood PD, et al. Aqueous Extract of Valerian Root (Valeriana officinalis L.) Improves Sleep Quality in Man. Pharmacol Biochem Behav. 1982;17:65-71.
  5. View Abstract: Balderer G, et al. Effect of Valerian on Human Sleep. Psvchopharmacology. 1985;87:406-09.
  6. PDR for Herbal Medicines, 2nd edition. Montvale, NJ: Medical Economics Company; 2000:784.
  7. Newall CA, et al. Herbal Medicines: A Guide for Health Care Professionals. London: The Pharmaceutical Press; 1996.
  8. Upton R. Valerian Root: Analytical, Quality Conrtol, and Therapeutic Monograph. Santa Cruz, CA: American Herbal Pharmacopoeia; 1999.
  9. Wagner H, et al. On the Spasmolytic Activity of Valeriana Extracts. Planta Med. 1979;37(1):84-86.
  10. Hendriks H, et al. Pharmacological Screening of Valerenal and Some Other Components of Essential Oil of Valeriana officinalis. Planta Medica. 1985;51:28-31.
  11. View Abstract: Houghton PJ. The Biological Activity of Valerian and Related Plants. J Ethnopharmacol. 1988;22(2):121-42.
  12. View Abstract: Santos MS, et al. Synaptosomal GABA Release as Influenced by Valerian Root Extract--Involvement of the GABA Carrier. Arch Int Pharmacodyn Ther. 1994;327(2):220-31.
  13. View Abstract: Gutierrez S, Ang-Lee MK, Walker DJ, Zacny JP. Assessing subjective and psychomotor effects of the herbal medication valerian in healthy volunteers. Pharmacol Biochem Behav. May2004;78(1):57-64.
  14. View Abstract: Hallam KT, Olver JS, McGrath C, Norman TR. Comparative cognitive and psychomotor effects of single doses of Valeriana officianalis and triazolam in healthy volunteers. Hum Psychopharmacol. Dec2003;18(8):619-25.
  15. Wang PC, Hu JM, Ran XH, et al. Iridoids and sesquiterpenoids from the roots of Valeriana officinalis. J Nat Prod. Sep 2009;72(9):1682-1685.
  16. Carrasco MC, Vallejo JR, Pardo-de-Santayana M, Peral D, Martín MA, Altimiras J. Interactions of Valeriana officinalis L. and Passiflora incarnata L. in a patient treated with lorazepam. Phytother Res. Dec 2009;23(12):1795-1796.
  17. Dalla Corte CL, Fachinetto R, Colle D, et al. Potentially adverse interactions between haloperidol and valerian. Food Chem Toxicol. Jul 2008;46(7):2369-2375. Epub 2008 Mar 28.
  18. Fachinetto R, Villarinho JG, Wagner C, et al. Valeriana officinalis does not alter the orofacial dyskinesia induced by haloperidol in rats: role of dopamine transporter. Prog Neuropsychopharmacol Biol Psychiatry. 1 Oct 2007;31(7):1478-1486. Epub 2007 Jul 4.
  19. 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. Neuropharmacology. Jan 2009;56(1):174-181. Epub 2008 Jun 17.
  20. Trauner G, Khom S, Baburin I, Benedek B, Hering S, Kopp B. Modulation of GABAA receptors by valerian extracts is related to the content of valerenic acid. Planta Med. Jan 2008;74(1):19-24. Epub 2007 Dec 19.
  21. Murphy K, Kubin ZJ, Shepherd JN, Ettinger RH. Valeriana officinalis root extracts have potent anxiolytic effects in laboratory rats. Phytomedicine. 28 Dec 2009. [Epub ahead of print]
  22. Bent S, Padula A, Moore D, Patterson M, Mehling W. Valerian for sleep: a systematic review and meta-analysis. Am J Med. Dec 2006;119(12):1005-1012. Review.
  23. Taibi DM, Vitiello MV, Barsness S, Elmer GW, Anderson GD, Landis CA. A randomized clinical trial of valerian fails to improve self-reported, polysomnographic, and actigraphic sleep in older women with insomnia. Sleep Med. Mar 2009;10(3):319-328. Epub 2008 May 14.
  24. Oxman AD, Flottorp S, Håvelsrud K, et al. A televised, web-based randomised trial of an herbal remedy (valerian) for insomnia. PLoS One. 17 Oct 2007;2(10):e1040.
  25. Dimpfel W, Suter A. Sleep improving effects of a single dose administration of a valerian/hops fluid extract - a double blind, randomized, placebo-controlled sleep-EEG study in a parallel design using electrohypnograms. Eur J Med Res. 26 May 2008;13(5):200-204.
  26. Alkharfy KM, Frye RF. Effect of valerian, valerian/hops extracts, and valerenic acid on glucuronidation in vitro. Xenobiotica. Feb 2007;37(2):113-123.
  27. Müller SF, Klement S. A combination of valerian and lemon balm is effective in the treatment of restlessness and dyssomnia in children. Phytomedicine. Jun 2006;13(6):383-387. Epub 2006 Feb 17.
  28. Kennedy DO, Little W, Haskell CF, Scholey AB. Anxiolytic effects of a combination of Melissa officinalis and Valeriana officinalis during laboratory induced stress. Phytother Res. Feb 2006;20(2):96-102.
  29. Cuellar NG, Ratcliffe SJ. Does valerian improve sleepiness and symptom severity in people with restless legs syndrome? Altern Ther Health Med. Mar-Apr 2009;15(2):22-28.
  30. Rezvani ME, Roohbakhsh A, Allahtavakoli M, Shamsizadeh A. Anticonvulsant effect of aqueous extract of Valeriana officinalis in amygdala-kindled rats: possible involvement of adenosine. J Ethnopharmacol. 3 Feb 2010;127(2):313-318. Epub 2009 Nov 10.
  31. De Oliveria DM, Barreto G, De Andrade DV, et al. Cytoprotective effect of Valeriana officinalis extract on an in vitro experimental model of Parkinson disease. Neurochem Res. Feb 2009;34(2):215-220. Epub 2008 May 30.