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Valerian trials

by Jill Hoppe, Certified Herbalist

Medical Herbalism 12(1):16-18

A controlled and double-blind German study evaluated whether valerian root extract impaired reaction time, alertness and concentration the morning after administration, in 102 people. A computer-assisted application measured reaction time, alertness, two-handed coordination, sleep quality, and visual discrimination tasks. One group took 600 mg. valerian root extract (LI 156), another took 1 mg. of the benzodiazepine flunitrazepam (Rohypnol), and a third group took placebo. The next morning, valerian did not impair reaction abilities, concentration or coordination in any patient. After fourteen days of nightly administration, a second evaluation took place. Patients taking valerian or placebo did not experience significant negative impact. The researchers concluded that single or repeated use of 600 mg. valerian root extract does not have a negative effect on reaction time, alertness and concentration the morning after intake. (Kuhlmann).

In a recent Gallup survey, 36% of American respondents reported insomnia complaints. The benzodiazepine tranquilizers (valium, xanax, etc.) are the most widely used substances for the treatment of sleep disorders. Benzodiazepines effectively induce sleep, but they are addictive and have other side effects including impaired coordination, negative effects on memory, confusion, lethargy, weakness and rebound insomnia after withdrawal. Valerian may be a useful alternative for people with sleep problems or anxiety.

Traditional Use

Valerian has been traditionally employed as a nervine, carminative, and sedative. Galen (130–200 CE) prescribed valerian for insomnia and numerous ailments. Felter (1922) recorded the use of valerian for cerebral and spinal stimulating effects, hysteria, hypochondria, headache, hemicrania, chorea, mental depression, carminative effects, and nervine actions, particularly when “the brain circulation is feeble and there is mental depression and despondency.”

Recent Trials

Clinical research shows that valerian improves overall sleep quality, shortens the time it takes to fall asleep and decreases the number of perceived awakenings during sleep. One double-blind, placebo-controlled valerian study of 128 people measured subjective sleep parameters. Each person received 3 samples containing placebo, 3 samples containing 400 mg. valerian extract, and 3 samples containing an over-the-counter preparation with 400 mg. valerian and hops strobiles. The samples were administerd on non-consecutive nights. Compared to the placebo, valerian reduced the fall asleep time and increased sleep quality—particularly among those who considered themselves poor or irregular sleepers. The commercial preparation with valerian and hops was not as effective as the experimental valerian extract (Leatherwood).

In-vitro and in-vivo experiments have identified antispasmodic effects on smooth muscles, hypotensive effects, and dilating effects on coronary arteries. Anti-depressant activity has also been investigated. A randomized, investigator-blinded study with 39 fibromyalgia patients examined the effects on pain, disturbed sleep and tender point count using plain water, pine oil or valerian whirlpool baths. The baths were carried out 10 times, three times per week. General pain, daytime change of pain intensity, well-being and occurrence of disturbed sleep were recorded before and after therapy. The number of tender points were identified by digital palpitation. Pain threshold on the shinbone and middle part of the deltoid muscle, and pain threshold and pain tolerance of both trapezius muscles were measured by an instrument used to asses pain. After the valerian baths, well-being and sleep significantly improved and tender point count decreased significantly. Pine oil baths resulted in significant improvement in well-being, but a significant decrease of pain threshold in the shinbone and the right deltoid muscle. Plain water baths significantly reduced general pain intensity. (Ammer)

Mode of Action

Valerian contains an extensive array of active constituents. Most valerian studies, however, have focused upon the valepotriates, volatile oils and valerenic acid. Despite extensive investigation, the exact constituents responsible for valerian’s sedative effect, and the mode of action, remain unknown. Like many medicinal plants, the therapeutic effect depends upon the interaction of the plant’s constituents as a whole, rather than its isolated parts. Valerian contains amino acids, alkaloids, phenolic acids, flavonoids, caffeic acid, choline, B-sitosterol, fatty acids plus numerous additional constituents and minerals. A nutritional analysis identified valerian as the best herbal source of calcium examined (Pedersen). A root analysis identified 42,000 parts per million (Duke).

Valerian’s sedative effects may involve the inhibition of the breakdown of the amino acid gamma-aminobutyric acid (GABA). A study using aqueous valerian root and rhizome extract exhibited an increase in GABA at the synaptic cleft (space between the junction of two neurons) by inhibiting re-uptake and/or stimulation of GABA release from nerve terminals on isolated rat brain synaptosomes. The release was Na+ dependent and Ca2+ independent. GABA is a major inhibitory neurotransmitter that induces relaxation by blocking the arousal of brain centers (benzodiazepines are thought to potentiate the activity of GABA). Since GABA does not readily cross the blood-brain barrier, however, the authors of this study were not convinced that valerian binds to GABA receptor sites in the brain (Santos). The amino acids of valerian root and rhizome extracts were evaluated in another study to identify whether an exchange mechanism is involved in the GABA release, induced by valerian extract. Arginine and glutamine were the highest amino acid concentrations found, followed by alanine and GABA. The authors comment that the high glutamine concentration could contribute to valerian’s sedative effects since glutamine crosses the blood-brain barrier, where it can be taken up by the nerve terminals and metabolized to GABA. The actual GABA present in the valerian preparation may also contribute to valerian’s sedative properties (Santos).

Authors of a 1999 double-blind study with 16 insomniac patients theorized that slow distribution and slow increase in concentration of valerian to the effector site may produce the mild sedative effect, but only after prolonged use. No effect on sleep was noted by insomniacs with short-term valerian treatment, but after two weeks of treatment, sleep and subjective sleep perception improved. An unexpected outcome in this study was a significant reduction in headaches and gastrointestinal complaints while patients were taking valerian (Donath). This finding is consistent with the traditional use of valerian.

Indications

Like many medicinal plants, valerian has numerous medicinal uses but its main indications are for tension and anxiety. Valerian may be used during anxiety, nervous insomnia, tension-induced indigestion or muscle cramping. The eclectic specific indications of pale face and deficient cerebral circulation may help predict the patients most likely to benefit, and patient without those indications may be most likely to experience adverse effects of overstimulation and insomnia.

Dose

The fresh or recently dried root is believed to be the highest quality herb.

Tincture (fresh, whole plant 1:2; dry root 1:5, 70% alcohol): 30 – 90 drops, to 3 times daily

Capsules (root - #00): 2 – 3 daily

Hot Tea: Two teaspoons dried root per 1 cup boiling water, 2-3 times daily, one before bed

Cold Infusion: Pour a glass of water over 2 teaspoons dried root, let stand 8 hours

Plant juice: Adults = 1 tablespoon 3 times daily. Children = 1 teaspoon 3 times daily

External use: Brew a strong valerian tea, strain and add to bathwater

Standardized extract (1.0 to 1.5 valtrate or 0.8 valeric acid): 300 – 400 mg. daily

Cautions

Energetically, valerian is acrid, slightly bitter, and warm. Culpepper (1649) stated that valerian is “under the influence of mercury, and therefore hath a warming faculty.” Sauer (1777) wrote “Valerian possesses the virtues of warming and drying; of dissolving thick humors trapped in small glands; of strengthening the eyesight, head, and liver; of forcing urine and sweat; and of withstanding all poisons.” The warming effects of valerian may be why some people find valerian stimulating. Valerian may aggravate tiredness the morning following administration in some people. If this occurs, herbal traditions suggest reducing the dose in half.

The valepotriates have been found to be toxic in-vitro; however, this has not been demonstrated in-vivo. (Chan)

Empirical evidence suggests that valerian may alleviate symptoms when attempting to withdraw from benzodiazepine drugs (Andreatini). Valerian was implicated in a serious withdrawal effect, however, which included cardiac complications and delirium in a 58-year-old man with a history of coronary artery disease, hypertension, and congestive heart failure. The patient was admitted to a hospital for a lung biopsy and upon admission he was taking multiple medications (isosorbide, dinitrate, digoxin, furosemide, benazepril, aspirin, lovastatin, ibuprofen), potassium, zinc, vitamins and 530 mg. – 2 g. per dose of valerian extract daily. This dose is perhaps five times the dose used in traditional herbalism. Herbal remedies are usually discontinued in hospitalized patients and this patient began exhibiting symptoms within 24 hours after valerian discontinuation. Since the patient’s symptoms were reversed with administration of the benzodiazepine midazolam (1 mg every hour, total dose of 11 mg in 17 hours), the authors hypothesized that valerian withdrawal produced a benzodiazepine-like withdrawal syndrome. The authors considered that the medications increased the potential for a valerian withdrawal reaction. (Garges).

References

Ammer K, Melnizky P. Medicinal Baths for treatment of generalized fibromyalgia. Forsch Komplementarmed 1999;6(2):80-85 [Article in German]

Andreatini R, Leite JR. Effect of valepotriates on the behavior of rats in the elevated plus-maze during diazepam withdrawal. European Journal of Pharmacology 1994;260(2-3):233-5

Blumenthal M. Herbal Medicine Explanded Commission E Monographs. Boston, Massachusetts: Integrative Medicine Communications, 2000

Chan TYK, Tang CH, Critchely AJH. Poisoning Due to an Over-the-counter Hypnotic, Sleep-Qik (Hyoscine, Cyproheptadine, Valerian). Postgrad.Med. J. 1995;71:227-228

Culpepper’s Complete Herbal. Great Britain: Wordsworth Editions Limited, 1995

Donath F, Quispe S, Diefenbach K, Maurer A, Fietze I, Roots I. Critical Evaluation of the Effect of Valerian Extract on Sleep Structure and Sleep Quality. Pharmacopsychiatry 2000;33:47-53

Ellingwood F. American Materia Medica, therapeutics and Pharmacognosy. Portland, Oregon: Eclectic Medical Publications, 1983

Felter HW. The Eclectic Materia Medica, Phamacology and Therapeutics. Cincinnati, Ohio: 1922

Foster S, Tyler V. Tyler’s Honest Herbal. Binghamton, New York Haworth: Herbal Press, 1999

Garges HP, Varia I, Doraiswamy PM. Cardiac Complications and Delirium Associated with Valerian Root Withdrawal. JAMA. 1998;280(18):1566-1567

Grieve M. A Modern Herbal. Great Britain: Tiger Books International, 1998

Kuhlmann J, Berger W, Podzuweit H, Schmidt U. The influence of valerian treatment on “reaction time, alertness and concentration” in volunteers. Pharmacopsychiatry 1999;32(6):235-41

Leatherwood PD, Chauffard F, Heck E, Munoz-Box R. Aqueous extract of valerian root (Valeriana officinalis L.) improves sleep quality in man. Pharmacol Biochem Behavior 1982;7(1):65-71

McCaleb R, Leigh E, Morien K. The Encyclopedia of Popular Herbs. Rocklin, California: Prima Publishing, 2000

Pedersen M. Nutritional Herbology. Warsaw, Indiana: Wendell W. Whitman Company, 1994

Santos M, Ferreira F, Cunha A, Carvalho A, Macedo T. An Aqueous Extract of Valerian Influences Trasport of GABA in Synaptosomes. Planta Medica 1994;60:278-279

Santos M, Ferreira F, Faro C, Pires E, Carvalho A, Cunha A, Macedo T. The Amount of GABA Present in Aqueous Extracts of Valerian is Sufficient to Account for [3H]GABA Release in Synaptosomes. Planta Medica 1994;60:475-476

United States. Department of Agriculture. Dr. Duke’s Phytochemical and Ethnobotanical Databases. Agricultural Research Service – NGRL, Beltsville Agricultural Research Center, Beltsville, Maryland