Health Care Professional Information

Scientific Name
Valeriana officinalis, Valeriana radix
Common Name

Garden valerian, Indian valerian, Pacific valerian, Mexican valerian, and garden heliotrope

Brand Name

Valerina Forte®

Clinical Summary

Derived from the root of the plant, this supplement is frequently used as a sedative to improve sleep. Although the active ingredients are not known, a mixture of constituents (e.g., valepotriates and volatile oils) is thought to be responsible for its biological activity. Valerian exhibits antioxidant (19) and cytoprotective (20) effects in vitro.

Studies show that the sleep-inducing properties of valerian extract are not superior compared to placebo (1) (2) (27); valerian also failed to improve sleep in a study of cancer patients (22). However, conclusions from meta-analyses indicate that modest improvements in sleep quality may be obtained with valerian (3) (21). It may also be effective against dysmenorrhea (24) and improve quality of sleep in postmenopausal women (25).

Valerian may have an additive effect when combined with barbiturates (e.g., pentobarbital) and benzodiazepines (e.g., alprazolam or triazolam) (18). Safety information regarding long-term use is not available, although cases of hepatotoxicity (4) and withdrawal syndrome have been reported.

Purported Uses
  • Colic
  • Insomnia
  • Menstrual cramps
  • Migraine treatment
  • Sedation
  • Spasms
  • Stomach and intestinal gas
Constituents
  • Alkaloids: Pyridine type, actinidine, chatinine, skyanthine, valerianine, valerine
  • Iridoids: Valepotriates, valtrate and didrovaltrate
  • Volatile Oils: Monoterpenes (borneol), sesquiterpenes (b-bisabolene)
  • Other constituents: Caffeic and chlorogenic acids, B-sitosterol, tannins, choline
    (7)
Mechanism of Action

Many researchers believe that the sedative effect of valerian is due to the valepotriates, and others believe it is due to the valepotriate decomposition products (baldrinal and homobaldrinal). In vitro, valerenic acid decreases degradation of Gamma-aminobutyric acid (GABA). Valerenic acid in animals appears to inhibit the enzyme system responsible for the central catabolism of GABA, increasing GABA concentration and decreasing CNS activity, and direct binding of valerenic acid to GABA-receptors has been demonstrated (8). Aqueous extracts of the roots contain appreciable amounts of GABA that could directly cause sedation, but some controversy surrounds the bioavailability of this compound.
(9)(10)(11)

Pharmacokinetics

One study demonstrated the onset of sleep-promoting effect within 30 minutes of oral administration.
(12)

Warnings

Long-term use has been associated with hepatotoxicity (4). Patients should be warned not to drive or operate dangerous machinery when taking valerian.
Valerian should be stopped about one week before surgery because it may interact with anesthesia.
(13)(14)

Adverse Reactions

Common: Headache, uneasiness, cardiac disturbances, morning drowsiness, impaired alertness (15).
Case Report: Long-term use of valerian has been reported to cause hepatotoxicity in a 27-year-old woman. Her symptoms improved following discontinuation of valerian use (4).
Administration of valerian to pregnant mice caused a significant reduction in zinc level in the fetal brain (26).

Herb-Drug Interactions
  • Barbiturates: Valerian increases the sedation time induced by barbiturates.
  • Benzodiazepines: Valerian may have synergistic effects (18).
  • Haloperidol: Valerian may have an additive effect causing hepatic damage (17).
  • UGT (Uridine 5'-diphospho-glucuronosyltransferase) substrates: Valerian modulates UGT enzymes in vitro and can increase the side effects of drugs metabolized by them (23).
  • Cytochrome P450 3A4 substrates: Valerian inhibits cytochrome P450 (CYP) 2D6 (5) and CYP3A4 (6), and can affect the intracellular concentration of drugs metabolized by these enzymes.
Literature Summary and Critique

Jacobs B, et al. An Internet-Based Randomized, Placebo-Controlled Trial of Kava and Valerian for Anxiety and Insomnia. Medicine 2005 Jul;84(4):197-207.
An Internet-based double-blind study found that kava is no more effective than an placebo for anxiety. 391 patients were recruited through e-mail or advertisements on web sites. The participants were randomly assigned to 1 of 3 treatment groups that were given capsules containing either kava, valerian, or a placebo for 4 weeks. At the end of the study, patients who received valerian had similar improvements in anxiety symptoms and in sleep as compared to the placebo group.

Oxman AD, et al. A televised, web-based randomised trial of an herbal remedy (valerian) for insomnia. PLoS ONE. 2007;2(10):e1040.
In this randomized, double-blind, placebo-controlled study, 405 participants with insomnia were recruited via television and the internet. Participants were mailed valerian (200 mg tablets) or placebo tablets and took 3 tablets 1 hour before bed-time for 2 weeks. Although no differences in self-reported sleep quality were detected, participants in the intervention group reported better outcomes on the global self-assessment question and a trend toward improved sleep duration and reduced night awakening was observed. The authors concluded that valerian had modest effects on sleep quality compared to placebo. Because the optimal dose of valerian is unknown, the potential benefit of larger dosages awaits further study.

Dosage (Inside MSKCC Only)
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References
  1. Diaper A, Hindmarch I. A double-blind, placebo-controlled investigation of the effects of two doses of a valerian preparation on the sleep, cognitive and psychomotor function of sleep-disturbed older adults. Phytother Res. Oct 2004;18(10):831-836.
  2. Jacobs BP, Bent S, Tice JA, et al. An internet-based randomized, placebo-controlled trial of kava and valerian for anxiety and insomnia. Medicine (Baltimore). Jul 2005;84(4):197-207.
  3. Bent S, Padula A, Moore D, et al. Valerian for sleep: a systematic review and meta-analysis. Am J Med. Dec 2006;119(12):1005-1012.
  4. Cohen DL, Del Toro Y. A case of valerian-associated hepatotoxicity. J Clin Gastroenterol. Sep 2008;42(8):961-962.
  5. Hellum BH, Nilsen OG. The in vitro inhibitory potential of trade herbal products on human CYP2D6-mediated metabolism and the influence of ethanol. Basic Clin Pharmacol Toxicol. Nov 2007;101(5):350-358.
  6. Hellum BH, Nilsen OG. In vitro inhibition of CYP3A4 metabolism and P-glycoprotein-mediated transport by trade herbal products. Basic Clin Pharmacol Toxicol. May 2008;102(5):466-475.
  7. Newall CA, Anderson LA, Phillipson JD. Herbal Medicines: A Guide for Health-Care Professionals. 1st ed. London: Pharmaceutical Press; 1996.
  8. 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. Jun 17 2008.
  9. De Smet PA. Adverse Effects of Herbal Drugs. New York: Springer; 1997.
  10. Houghton PJ. The scientific basis for the reputed activity of Valerian. J Pharm Pharmacol. May 1999;51(5):505-512.
  11. Schulz V, Rudolf H, Tyler V. Rational Phytotherapy: A Physician's Guide to the Use of Herbs and Related Remedies. 3rd ed. Berlin (Germany): Springer; 1998.
  12. Fachinformation: Sedalint® Baldrian, valerian extract. Muenchen (Germany): Sanofi Winthrop GmbH; 1996.
  13. Ang-Lee MK, Moss J, Yuan CS. Herbal medicines and perioperative care. JAMA. Jul 11 2001;286(2):208-216.
  14. Upton R. Valerian Root: Analytical, quality control, and therapeutic monograph. Soquel (CA): American Herbal Pharmacopoeia; 1999.
  15. Plushner SL. Valerian: Valeriana officinalis. Am J Health Syst Pharm. Feb 15 2000;57(4):328, 333, 335.
  16. Brinker F. Herb Contraindications and Drug Interactions. 3rd ed. Sandy (OR): Eclectic Medical Publications; 2001.
  17. Dalla Corte CL, Fachinetto R, Colle D, et al. Potentially adverse interactions between haloperidol and valerian. Food Chem Toxicol. 2008 Jul;46(7):2369-75.
  18. Carrasco MC, Vallejo JR, Pardo-de-Santayana M, et al. Interactions of Valeriana officinalis L. and Passiflora incarnata L. in a patient treated with lorazepam. Phytother Res. 2009 May 13. [Epub ahead of print].
  19. Sudati JH, Fachinetto R, Pereira RP, et al. In vitro antioxidant activity of Valeriana officinalis against different neurotoxic agents. Neurochem Res. 2009 Aug;34(8):1372-9.
  20. 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. 2009 Feb;34(2):215-20.
  21. Fernández-San-Martín MI, Masa-Font R, Palacios-Soler L, et al. Effectiveness of Valerian on insomnia: A meta-analysis of randomized placebo-controlled trials. Sleep Med. 2010 Mar 25. [Epub ahead of print]
  22. Barton DL, Atherton PJ, Bauer BA, et al. The use of Valeriana officinalis (Valerian) in improving sleep in patients who are undergoing treatment for cancer: a phase III randomized, placebo-controlled, double-blind study (NCCTG Trial, N01C5). J Support Oncol. 2011 Jan-Feb;9(1):24-31.
  23. Mohamed ME, Frye RF. Effects of herbal supplements on drug glucuronidation. Review of clinical, animal, and in vitro studies. Planta Med. 2011 Mar;77(4):311-21.
  24. Mirabi P, Dolatian M, Mojab F, Majd HA. Effects of valerian on the severity and systemic manifestations of dysmenorrhea. Int J Gynaecol Obstet. 2011 Dec;115(3):285-8. Epub 2011 Sep 28.
  25. Taavoni S, Ekbatani N, Kashaniyan M, Haghani H. Effect of valerian on sleep quality in postmenopausal women: a randomized placebo-controlled clinical trial. Menopause. 2011 Sep;18(9):951-5.
  26. Mahmoudian A, Rajaei Z, Haghir H, Banihashemian S, Hami J. Effects of valerian consumption during pregnancy on cortical volume and the levels of zinc and copper in the brain tissue of mouse fetus. Zhong Xi Yi Jie He Xue Bao. 2012 Apr;10(4):424-9.
  27. Oxman AD, Flottorp S, Håvelsrud K, et al. A televised, web-based randomised trial of an herbal remedy (valerian) for insomnia. PLoS ONE. 2007;2(10):e1040.

Consumer Information

How It Works

Bottom Line: Valerian has been shown in some studies to improve sleep.

Scientists are uncertain which compounds in valerian are responsible for its actions. In laboratory experiments, an extract of valerian prevented the breakdown of an important chemical in the nervous system called GABA. GABA is an inhibitory neurotransmitter, so increasing its availability will generally decrease the activity of the nervous system, causing a calming effect. The roots of valerian also contain considerable amounts of GABA.
Some studies have shown that valerian improves sleep and may help anxiety disorders. More research is needed.

Purported Uses
  • To calm muscle spasms
    Laboratory studies suggest positive effect, but human data are lacking.
  • To treat anxiety
    Large clinical trials found that valerian is no more effective than a placebo for anxiety.
  • To treat insomnia
    A review of clinical trials found small improvements in sleep with valerian, but further research is needed to determine the correct dose.
Research Evidence

Anxiety and Insomnia:
An Internet-based double-blind study recruited 391 patients through e-mail or advertisements on web sites. The participants were randomly assigned to 1 of 3 treatment groups that were given capsules containing either kava, valerian, or a placebo for 4 weeks. At the end of the study, patients who received valerian had similar improvements in anxiety symptoms and in sleep as compared to the placebo group.

In another randomized, double-blind, placebo-controlled study, 405 participants with insomnia were recruited via television and the internet. Participants were mailed valerian (200 mg tablets) or placebo tablets. Although no differences in self-reported sleep quality were detected, participants in the valerian group reported better sleep. The authors concluded that valerian had modest effects on sleep quality compared to placebo.

Patient Warnings
  • Valerian should be stopped about one week before surgery, because it can interfere with general anesthesia.
Do Not Take If
  • You are taking Barbiturates (Valerian lengthens the sedation time induced by barbiturates).
  • You are taking Benzodiazepines (Valerian may have additive effects).
  • You are taking Haloperidol (Valerian may have an additive effect causing hepatic damage).
  • You are taking drugs that are substrates of UGT (Uridine 5'-diphospho-glucuronosyltransferase) enzymes (Valerian may increase the risk of side effects of these drugs).
  • You are taking drugs that are substrates of Cytochrome P450 3A4 (Valerian may increase the risk of side effects of these drugs).
Side Effects
  • Headache
  • Uneasiness
  • Cardiac disturbances
  • Morning drowsiness when used at night to promote sleep
  • Impaired alertness
  • Liver toxicity and withdrawal syndrome have been reported after long-term use

Valerian fed to pregnant mice resulted in significant reduction in zinc level in the fetal brain.

E-mail your questions and comments to aboutherbs@mskcc.org.