Valerian Root: Non-Addictive Alternative for Insomnia and Anxiety

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Valerian Root: Non-Addictive Alternative for Insomnia and Anxiety

A major challenge facing healthcare practitioners today is safe and non-addictive medications for anxiety and insomnia. This category has largely been dominated in the last two decades by benzodiazepines like diazepam (Valium(R)) and alprazolam (Xanax(R)). While these drugs have been very useful in the management of more severe cases of anxiety, potential addiction and serious side effects secondary to withdrawal have cast a shadow over their long-term efficacy. Clearly, there is a need for gentler, non-addictive substances for the long-term management of insomnia and anxiety -- particularly for initial intervention in milder forms of these conditions.

Extracts of valerian root, usually in combination with other plant medicines, are often prescribed in Europe as a substitute for benzodiazepines in the management of insomnia and anxiety. Valerian root extracts are derived from the plant Valeriana officinalis, an upright perennial that grows wild in woodlands, along river banks, and in damp meadows all over Europe. Most of the plants used for medicinal preparations are cultivated.

The root of the plant is used medicinally. The root contains 0.4-1.4% volatile oils where the primary active constituents are found.( 1) These constituents include monoterpenes and sesquiterpenes with the primary focus on valerenic acid and valeranone. Current monographs on valerian require a minimum of 0.5% volatile oil content for medicinally used valerian root.( 2)

Mechanism of Action

While valerian root has been used for centuries in traditional herbal medicine preparations (and more recently in modern European extracts) for sleep disorders, nervousness, and even gastrointestinal pains of nervous origin, the mechanism of action for the active constituents has only recently been elucidated.

The breakthrough report on valerian's mechanism of action was published in 1989. Drs. J. Holzl and P. Godau of the Institute for Pharmaceutical Biology in Marburg, Germany, discovered that valerian binds benzodiazepine receptors in vitro.( 3) Valerian and its active constituents were shown to actually displace flurodiazepam off isolated benzodiazepine receptors from guinea pig brains.

Another in vitro study, completed in Milan, Italy, demonstrates the ability of valerian to bind GABA-A receptors.( 4) This deepens our understanding about the activity of valerian in the central nervous system. Sedation in the CNS is primarily mediated through GABA-A receptors. Important modulatory sites have been shown for the GABA-A chloride channel receptor complex, like central benzodiazepine receptors and barbiturate receptors.

Emphasis should be placed on the fact that the active constituents of valerian root appear to weakly bind benzodiazepine receptors when compared to drugs like diazepam or alprazolam. While exerting an effect on these receptors, valerian root is not associated with dependence and potential addiction.

Clinical Applications

INSOMNIA

Sleep disorders are rampant in our society. Epidemiological reports have shown that approximately one-third of the adult population suffers from initial and/or continued sleep disorders.( 5) Treatment is indicated in about 15% of these cases.

Clinical research has indicated the ability of valerian root to reduce sleep latency. Two placebo-controlled clinical studies examined the ability of an aqueous extract of valerian to both reduce sleep latency and improve sleep quality in humans suffering from insomnia. Using dosages of 400 to 900 mg of valerian root at bedtime, researchers found that valerian not only shortened sleep latency but also resulted in a reduction in night awakenings as well as an increase in dream recall. Perhaps most important was the observation that the morning "hangover" commonly associated with benzodiazepines was absent with use of valerian root.( 6, 7) The lower dosage range of 400 to 450 mg was shown to be as effective as the higher dosages recommended.

A more recent study in Germany compared a standardized valerian product, containing a concentrated extract of valerian root and an extract of lemon balm (Melissa officinalis), with triazolam (Halcion(R)) on sleep in twenty healthy volunteers ages 30 to 50 years.( 8) The median values of sleep efficiency of the volunteers established the criteria for the formation of two groups of "good" or "bad" sleepers. The valerian/lemon balm combination contains 160 mg of valerian root extract and 80 mg of lemon balm extract per tablet. Subjects were randomized to receive either one tablet of this combination or 0.125 mg of triazolam at bedtime. Sleep was monitored over nine nights.

Both groups showed a significant increase in sleep efficiency and in sleep stages 3 and 4 -- especially those in the category of "bad" sleepers. There was no rebound phenomena observed in either treatment group. In contrast to the triazolam group, daytime sedation and impairment of concentration or performance capabilities were not observed in the valerian/lemon balm group.

ANXIETY/AFFECTIVE DISORDERS

Based on the results with insomnia and sleep improvement in comparison with benzodiazepines, use of valerian combination products is growing among healthcare practitioners in the management of mild to moderate anxiety. Valerian, in combination with either lemon balm or passion flower (Passiflora incarnata), appears to offer a safe and efficacious tool in the early treatment of anxiety as well as the long-term management of those unable to use or attempting to withdraw from benzodiazepines.

Easing the withdrawal symptoms of patients attempting to discontinue the use of benzodiazepines is an intriguing area for future clinical work with valerian combination products. It has been my clinical observation that the more potent valerian combinations mentioned above are very useful in this process.

Another European study also indicates that valerian may be a useful tool in patients with affective disorders.( 9) The combination of a concentrated valerian and passion flower extract was compared with the European neuroleptic drug, Propaphenin(R), in 20 psychosomatic and affective disorder patients. Each tablet of the valerian/passion flower combination contained 100 mg. of valerian root and 45 mg of passion flower. The daily dose was two tablets three times daily. All patients were monitored by EEG as well as depression and anxiety clinical monitoring questionnaires.

EEG changes included selective alpha-and theta-wave increases in both groups. However, in the valerian/passion flower group, these were noted after only two weeks of use as compared to six weeks for the neuroleptic group. Depression and anxiety measures were decreased in both groups but side effects like reduced vigilance and orthostatic load were noted only in the neuroleptic group.

Safety of Long-Term Valerian Use

European monographs on valerian list no contraindications to its use in humans. It appears to be safe during pregnancy and lactation. Patients using valerian for anxiety should beware of using it concomitantly with alcohol. Caution should also be taken when driving or operating machinery after valerian use.

References
(1) British Herbal Compendium. British Herbal Medicine Association. 1992.

(2) Valerianae Radix, (Valerian Root). European Monograph. European Scientific Cooperative for Phytotheraphy, 1992.

(3) Holzl J & Godau P: Receptor bindings studies with Valeriana officianlis on the benzodiazepine receptor. Planta Med 55: 642, 1989.

(4) Mennini T, Bernasconi P, et al: In vitro study on the interaction of extracts and pure compounds from Valeriana officinalis roots with GABA, benzodiazepine and barbiturate receptors. Fitoterapia 64: 291-300, 1993.

(5) Bixler EO, Kales A, et al: Prevalence of sleep disorders in the Los Angeles metropolitan area. Am J Psychiatr 136: 1257-62, 1979.

(6) Leathwood PD & Chauffard F: Aqueous extract of valerian reduces latency to fall asleep in man. Planta Med 51: 144-8, 1985.

(7) Leathwood PD, Chauffard F, et al: Aqueous extract of valerian root (Valerian officinalis L.) improves sleep quality in man. Pharmacol Biochem Behav 17: 65-71, 1982.

(8) Dressing H, Riemann D, et al: Insomnia: Are valerian/balm combination of equal value to benzodiazepine? Therapiewoche 42: 726-36, 1992.

(9) Schellenberg V, Schellenberg R & Janig L: Quantitative EEG monitoring in phyto-and psychopharmacological treatment of psychosomatic and affective disorders. Schizophrenia Res 9 (2, 3): Abstract, 1993.

Natural Product Research Consultants, Inc.

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By Donald J. Brown

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