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Valerian (valeriana officinalis)

James Meschino DC, MS, ROHP

General Features

There are more than 200 plant species belonging to the genus Valeriana, but the most common one, and the one used for medicinal purposes is Valeriana officinalis.  1,9 10   This plant grows wild all over Europe, but most of the Valerian used in consumer health products is cultivated.  10   The rootstock contains its active constituents, which are concentrated into health products used primarily for the treatment of insomnia and anxiety.  1,9,10      Scientific studies evaluating the effects of Valerian on humans began in the 1970’s, which subsequently lead to its approval as a sleep aid by the Germany’s Commission E Monograph in 1985.  9

Principle Active Constituents

  1. Valepotriates (iridoid molecules) and valerenic acid. These compounds are exclusive to Valerian.1  It now appears that valerenic acid is a possible active constituent, but not the valepotriates.  9
  2. Volatile Oils 12

Clinical Application and Mechanism of Action

  1. Insomnia

Valerian acts as a sedative in that its active constituents, which are not fully understood or known, are capable of binding to the same brain receptors as Valium and other benzodiazepine drugs.  Central nervous system sedation is regulated by receptors in the brain known as GABA-A receptors (gamma amino butyric acid).  Experimental test tube studies indicate that active constituents in Valerian may weakly bind to GABA-A receptors in the brain, producing a sedation effect.  Human trials suggest that Valerian tends not to impair mental function or produce a morning hangover, and dependency has not been reported with its use.  Studies have demonstrated improved sleep quality and insomnia relief.  1,2,3,9,11,12

        Overall, studies suggest that Valerian improves sleep quality (more restful sleep), and the transition into sleep.  However, it may not increase total sleep time.  These findings arise from several double-blind trials, that provide evidence for Valerian as an effective treatment for individuals with mild to moderately severe insomnia. 2,3,4,13,14,15,16     

A 28-day study, involving 121 subjects, showed that Valerian supplementation provided significant improvement in insomnia cases, compared to the placebo.  13

A 14-day trial, involving 78 elderly patients, also showed that Valerian supplementation provided significant improvement in insomnia cases, compared to placebo.  As shown in other studies, it often takes a number of days before the effects of Valerian appear.  As such, patients tend to report more consistent improvement in relief of insomnia after several days of Valerian supplementation (its effects are not immediate as would be the case for many drugs prescribed for this condition). 14       

There is also convincing evidence from animal studies that Valerian produces a calming effect, as well as enhanced sleepiness, and reduced activity patterns.  These studies provide important objective proof of Valerian’s natural sedative capabilities.  18,19,20,21

In head-to-head trials testing Valerian against the drug oxazepam (10 mg at bedtime) and bromazepam, Valerian supplementation demonstrated that it could provide equal relief for insomnia, as did these common sleep-aid medications. 15,16

  1. Anxiety

Several preliminary studies indicate that Valerian may be an effective treatment in cases of uncomplicated anxiety (not linked to major depression) and it has been used for this problem historically and clinically, although more research is needed to better understand its application in this regard.  1,2,3,17

Dosage and Standardized Grade

  1. Insomnia: As a mild sedative, Valerian may be taken 30-45 minutes before retiring at the following dosage and standardized grade: Valerian extract, 200 –400 mg (standardized to 0.8% valerenic acids content) 8,11
  2. Anxiety and Stress Reduction: 200 mg, twice per day (standardized to 0.8% valerenic acids content). 11

 

Adverse Side Effects, Toxicity and Contraindications

Animal studies show that it takes enormously large doses of Valerian to produce any serious side effects, and in one suicide attempt, a human subject experienced no life threatening effects (stomach cramps, fatigue, chest tightness, tremors and light-headedness), after taking 20 gms of valerin (20-40 times the recommended dose).  22,23   There have been approximately 50 reported cases of overdose when subjects took a product called Sleep-Qik, containing Valerian as well as conventional medications, but no liver damage was noted.  24,25

Generally speaking, Valerian is considered to be safe and usually causes only mild gastrointestinal upset on rare occasions. It is on the GRAS list (generally recognized as safe) of the FDA.

Some mild impairment to attention ability may occur for a couple of hours after intake, and thus, driving immediately after Valerian supplementation is not advised.  However, Valerian is not reported to cause morning drowsiness when taken the night before.  9,10,11 If morning sleepiness does occur, simply reduce the dosage.1

Drug-Nutrient Interactions

Valerian may potentiate the actions of the following medications and thus, it is considered to be prudent to not take Valerian concurrently with these drugs:

  • Barbituates or Sedatives 26
  • Antidepressants 27,28,29 
  • Anti-anxiety medications 30,31,32    
  • Hypnotic drugs 33,34,35

 

Pregnancy and Lactation

During pregnancy and lactation, the only supplements that are considered safe include standard prenatal vitamin and mineral supplements.  All other supplements or dose alterations may pose a threat to the developing fetus and there is generally insufficient evidence at this time to determine an absolute level of safety for most dietary supplements other than a prenatal supplement.  Any supplementation practices beyond a prenatal supplement should involve the cooperation of the attending physician (e.g., magnesium and the treatment of preeclampsia.)

References:  Pregnancy and Lactation
1.     Encyclopedia of Nutritional Supplements. Murray M. Prima Publishing 1998.

2.     Reavley NM. The New Encyclopedia of Vitamins, Minerals, Supplements, and Herbs. Evans and Company Inc. 1998.

3.     The Healing Power of Herbs (2nd edition). Murray M. Prima Publishing 1995.

4.     Boon H and Smith M. Health Care Professional Training Program in Complementary Medicine. Institute of Applied Complementary Medicine Inc. 1997.

 

  1. Houghton PJ. The biological activity of Valerian and related plants.  J Ethnopharmacol 1988;22(2):121-42.
  2. Leathwood P, et.al.. Aqueous extract of Valerian root (Valeriana Officinalis L.) Improves sleep quality in man.   Pharmacol Biochem Behav 1982;17:65-71.
  3. Bakderer G, Borbely AA. Effect of Valerian on human sleep.  Pharmacol 1985;87:406-9.
  4. Leathwood PD, Chauffard F. Aqueous extract of Valerian reduces latency to fall asleep in man.  Planta Medica  1985;54:144-8.
  5. Lindahl O, Lindwall L. Double blind study of a Velerian preparations.  Pharmacol Biochem Behav 1989;32(4):1065-6.
  6. Dressing H, et.al.. Insomnia:  are Valeriana/Melissa combinations of equal value to Benzodiazepine?   Therapiewoche 1992;42:726-36.
  7. Leung A. Encyclopedia of common natural ingredients used in food, drugs, and cosmetics.  New York,  New York.  John Wiley & Sons, 1980.
  8. Murray MT. The healing power of herbs.  2nd  Prima Publishing, 1995.
  9. Natural Products Encysclopedia www.consumerslab.com: Valerian
  10. Healthnotes, Inc. 2001 www.healthnotes.com: Valerian
  11. Dietary Supplement Information Bureau. www.content.intramedicine.com: Valerian
  12. Mennini 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 1993;64:291–300
  13. Vorbach EU, Gortelmeyer R, Bruning J. Therapy for insomniacs:effectiveness and tolerance of valerian preparations [translated from German]. Psychopharmakotherapie 1996;3:109-15
  14. Kamm-Kohl AV, Jansen W, Brockmann P. Modern valerian therapy for nervous disorders in old age [translated from German]. Med Welt 1984;35:1450-4
  15. Dorn M. Efficacy and tolerability of Baldrian versus oxazepam in non-organic and non-psychiatric insomniacs: a randomized, double-blind, clinical, comparative study [translated from German]. Forsch Komplementarmed Klass Naturkeilkd 2000;7:79-84
  16. Schmitz M, Jackel M. Comparative study for assessing quality of olife of patients with exogenous sleep disorders (temporary sleep onset and sleep interruption disorders)
  17. Kohnen R, Oswald WD. The effects of valerian, propranolol, and their combination on activation, performance and mood of healthy volunteers under social stress conditions. Pharmacopsychiatry 1988;21:447-8
  18. Hendriks H, Bos R, Woerdenbag HJ, et al. Central nervous depressant activity of valerenic acid in the mouse. Planta Med 1985;1:28-31
  19. Leuschner J, Muller J, Rudmann M. Characterisation of the central nervous depressant activity of a commercially available valerian root extract. Arzneimittelforschung 1993;43:638-41
  20. Krieglstein J, Grusla D. Centrally depressant components of valerian. However, valepotriates, valerenic acid, valeranone and the essential oil are ineffective [in German]. Dtsch Apoth Ztg 1988;128:2041-6
  21. European Scientific Cooperative on Phytotherapy. Valerianae radix. Exeter, UK: ESCOP 1996-1997:3-4 Monographs on the Medicinal uses of Plant Drugs, Fascicule 4
  22. Resecrans JA, Defeo JJ, youngken HW Jr. Pharmacological investigation of certain Valeriana officinalis L. extracts. J Pharm Sci 1961l50:240-4
  23. Willey LB, Mady SP, Cobaugh DJ, et al. Valerian overdose: a case report. Vet Hum Toxicol 1995;37:364-5
  24. Chan TY, Tang CH, Critchley JA. Poisoning due to an over-the-counter hypnotic, Sleep-Qik (hyoscine, cyproheptadine, valerian). Postgrad Med J 1995;71(834):227-8
  25. Chan TY. An assessment of the delayed effects associated with valerian overdose [letter]. Int J Clin Pharmacol Ther 1998;36:569
  26. Hendriks H, et al. Central nervous depressant activity of valerenic acid in the mouse. Planta Med Feb1985;1:28-31
  27. Houghton PJ. The biological activity of valerian and related plants. J Ethnopharmacol 1988;22(2):121-42
  28. Santos MS, et al. Synaptosomal GABA release as influenced by valerian root extract – involvment of the GABA carrier. Arch Int Pharmacodyn Ther 1994;327(2):220-31
  29. Houghton PJ. The scientific basis for the reputed activity of valerian. J Pharm Pharmacol May 1999;51(5):505-12
  30. Houghton PJ. The biological activity of valerian and related plants. J Ethnopharmacol 1988;22(2):121-42
  31. Santos MS, et al. Synaptosomal GABA release as influenced by valerian root extract – involvment of the GABA carrier. Arch Int Pharmacodyn Ther 1994;327(2):220-31
  32. Houghton PJ. The scientific basis for the reputed activity of valerian. J Pharm Pharmacol May1999;51(5):505-12
  33. Houghton PJ. The biological activity of valerian and related plants. J Ethnopharmacol 1988;22(2):121-42
  34. Santos MS, et al. Synaoptosomal GABA release as influenced by valerian root extract – involvment of the GABA carrier. Arch Int Pharmacodyn Ther 1994;327(2):220-31
  35. Houghton PJ. The scientific basis for the reputed activity of valerian. J Pharm Pharmacol May1999;51(5):505-12
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