Valeriana officinalis.Valerian and Medical Attributes.Valerian Root Extract.

Valerian:Pharmacology,Mechanisms of Action.

Valerian Root Extract INCI Name Valeriana Officinalis Extract EINECS ELINCS No.232-501-7 CAS 8057-49-6 Valerienic acid 109-52-4 photo picture image Pharmacology and Mechanisms of Action:

This plant is well known as a CNS-depressant. The active ingredient is a matter of some debate. This group of chemicals is not usually present in significant amounts in the crude herb or tincture, which clinically also shows a sedative effect. It might be the volatile oils and valeric acid that have the sedating effect, depressant effect on the autonomic system. It can be said that this herb is antispasmodic and equalizing (sedative in state of agitation and stimulant in fatigue). Valerian is also hypotensive, antibacterial, especially Gram positive bacteria (due to its alkaloids), antidiuretic, and hepatic (protecting the liver from necrosis). The iridoid compound is very attractive to cats. They obtain a euphoric "high" from it.

Valerian has an affinity for GABAA receptors, likely due to the relatively high GABA content in valerian itself. The amount of GABA present in valerian extract is sufficient to induce release of GABA in synaptosomes and may also inhibit GABA reuptake.

Other believed mechanisms of action in valerian include inhibition of the catabolism of GABA by valerenolic acid and acetylvalerenolic acid and affinity for the 5-HTA receptor by another constituent of valerian, called hydroxypinoresinal.

Due to the herb's historical use as an anti-convulsant, sedative, migraine treatment and pain reliever, most basic research has been focused on the interaction of valerian constituents with the GABA neurotransmitter. The findings of these studies remain inconclusive.

Scientists have isolated over 150 phytochemical [plant-based] components from the rootstock of Valerian since the early 1900s. There are at least two (2) primary compounds as well as other amino acid constituents that are thought to exhibit a sedative effect in Central Nervous System (CNS) . These include:

Valerenic Acids (valerenic acid, hydroxy valerenic acid, acethoxy valerenic acid and valerenal)
Valepotriates (valtrate, isovaltrate, acevaltrate, didrovaltrate)
GABA (Gamma-Aminobutyric Acid)
Tyrosine, Arginine, and Glutamine

Pharmacological research suggests that together, these components naturally inhibit enzyme-induced GABA (Gamma-Aminobutyric Acid) breakdown in the brain, although, the precise mechanism of action has yet to be defined.

In human clinical trials Valerian Root has been shown to reduce restlessness, nervous tension, occasional anxiety and panic, and sleep difficulties. Results of further analysis indicate that Valerian Root can also help to stabilize mild mood changes and support a positive mood balance. Research has demonstrated that neither single nor repeated evening administrations of Valerian Root have a negative impact on reaction time, alertness or concentration the day after use.
Valerian Root Extract INCI Name Valeriana Officinalis Extract EINECS ELINCS No.232-501-7 CAS 8057-49-6 Valerienic acid 109-52-4 photo picture image

Clinical Research:

Clinical study indicates that the combination of phytochemical components derived from Valerian Root (i.e., flavonoids such as valepotriates, valerenic acid, and free amino acids like Glutamine and Gamma-AminoButyric Acid) act to effectively relax the Central Nervous System (CNS) when administered in moderate to high dosage ranges. Research results demonstrate an increased release of GABA, decreased GABA reuptake [reabsorption], and decreased GABA degradation in laboratory settings.

The review of all available clinical trials, observations and empirical data based on traditional and contemporary use reveals overwhelming evidence to support the effectiveness of Valerian Root as a natural sedative as well as in its ability to potentiate relaxation of the Central Nervous System (CNS). Studies confirm that Valerian Root is well-tolerated. Side effects were rare or mild and no adverse events related to withdrawal, dependence or addiction were observed.

A randomized, controlled, double-blind trial was recently completed to determine whether Valerian Root extracts adversely affected alertness, reaction time and concentration. During a period of 14 days, participants were measured using the primary criterion, the Vienna Determination Test, to assess reactive stress tolerance. Evaluation of secondary criteria, which included further [VDT] parameters and safety standards were found to be consistent with the results of the primary criterion. Researchers concluded that Valerian Root extracts administered in either a single dose [of 600mg] or repeated high doses [of up to 600mg] did not have a negative impact on participants' alertness, reaction time or concentration the morning after intake.

Remedies:

Macerations, infusions, and tinctures are used to treat insomnia and anxiety.
Compresses soaked in the tincture can ease muscle cramps.
Washes from the infusion or maceration are used for chronic ulcers and wounds and for drawing out splinters.

Valerian root is used primarily as a mild sedative to calm restlessness and anxiety and overcome mild insomnia. At least two double-blind studies have demonstrated that valerian extract can significantly reduce the amount of time it takes people to fall asleep without changing the normal stages of sleep. Valerian is used in Europe as an antispasmodic, particularly for abdominal cramps due to nervousness and for uterine cramps and menstrual agitation. Valerian is also used as a mild tranquilizer for people experiencing emotional stress, much as antianxiety drugs are prescribed, and has been prescribed for exhaustion. Some herbalists have also recommended it for tension headaches, bronchial spasms, and lingering coughs. Valerian has occasionally been tried as part of a program to take a patient off antidepressants or benzodiazepines, and valerian is sometimes used as a muscle relaxant to treat pain.

The dried roots of valerian smell unmistakably of 3-methylbutanoic acid (isovaleric acid, 'sour toes'), but more pleasantly smelling elements may also be perceived, e.g. myrtenyl isovalerate. Small amounts of various sesquiterpenes are present too, e.g. valerianol. Extracts from valerian roots are available in pharmacies as a mild sedative. Earlier, when the pharmacies made their own extracts and discarded the roots in the backyards, one could see cats from the town roll upon them. Male cats are mad with some pyridine alcaloids in valerian root, e.g. the iridoid monoterpene actinidine, resembling the active ingredient nepetalactone in catnip (or catmint), Nepeta cataria (Labiatae)

isovaleric acid and myrtenyl isovalerate: Valerian Root Extract INCI Name Valeriana Officinalis Extract EINECS ELINCS No.232-501-7 CAS 8057-49-6 Valerienic acid 109-52-4 photo picture image actinidine and nepetalactone:

Scientific Proofs of Valerian's Effectiveness:Valerian Trials

A human body is far from being a "perpetum mobile". It needs much rest and good care to function well. Nature has reserved the time for rest ,it is a night, when all we can restore our strength and give a break to out nervous system after the hard work and psychological stresses of the day-time.

However, many people cannot have healing rest at night, because their bodies are tortured by insomnia. Others cannot get rid of the anxiety even spending a quiet and soothing evening with friends and relatives. Doctors would prescribe them very effective pills (but the latter always have side effects); traditional herbalists would unambiguously recommend to try Valerian, the herb, which people all around the world have been using for centuries to fight sleeping disorders and to sooth the nervous system.

Indeed, Valerian is a powerful sedative; and an anxiolytic. Although it was said to be effective against many different diseases, its main function is to cause the relaxation of the whole body and provoke sleep.

Nowadays scientists carry out multiple trials to discover and make official conclusions concerning the power and effect of Valerian on human bodies.

Actually, the work that has already been done proves that Valerian plant (herbalists and scientists usually employ only one sort, V. officinalis) can really help fight insomnia (usually improving the ability to fall asleep, increasing total sleep time, reducing sleep latency, and making the quality of all sleep stages better), lessen the stress (decreasing systolic blood pressure and heart rate reaction), and reduce anxiety (especially GAD-generalized anxiety disorder).
Valerian Root Extract INCI Name Valeriana Officinalis Extract EINECS ELINCS No.232-501-7 CAS 8057-49-6 Valerienic acid 109-52-4 photo picture image

Many people, who considered themselves to be poor sleepers, reported about the positive effect of Valerian extract after the clinical trials. Researchers concluded that the herb worked best in older male patients, female poor sleepers, younger people, smokers and those who had lengthy sleep latencies.

A great advantage of Valerian treatment was that patients noticed no side effects in response to the doses of the extract used in the trials (400 to 600 mg of a standardized commercial preparation of dried Valerian root). Still, overdose in anything is dangerous. The known symptoms of Valerian overdose are dizziness, blurry vision, nausea, restlessness, excitability, and grogginess upon awakening.

As for the anxiety disorders, clinical trials proved the improvement of patient's state, significantly decreased subjective feelings of somatic arousal, and reduction in the psychic factor of the Hamilton Anxiety Scale in response to either valerian,propranolol tincture (100mg Valerian, 20mg propranolol), or Valerian extract (50 mg~ 3 times daily in one trial and 600 mg of Valerian in comparison to 120mg of Kava Kava and placebo daily in another study).

The results of the trials made are quite promising. Nevertheless, many questions still remain: why do some people not respond to Valerian extract; who cannot take it; what are the consequences of the long-term Valerian usage...? There is no data on all these issues. To be on the safe side, pregnant and breastfeeding women, as well as children under 3 are not recommended to take this sedative. High doses are also forbidden.

To study all these aspects, scientists must understand the mechanism of Valerian activity and its components better. For the time being, they defined such constituents in Valerian extract: volatile oil (including valeric acid), iridoids (valepotriates), alkaloids, furanofuran lignans, and free amino acids such as g-aminobutyric acid (GABA), tyrosine, arginine, and glutamine. What ingredient is responsible for the sedative and hypnotic effect is not known exactly. There are two versions, however: either volatile oil or the whole bouquet (which is more likely) may produce such effect.

Scientists suggest that Valerian extract increases the amount of gamma aminobutyric acid (GABA, an inhibitory neurotransmitter) and blocks an enzyme that destroys it. This may cause the sleep-provoking effect of Valerian.

Hopefully, scientists will find the answers to all their and our questions. For the time being, it is possible to confirm that Valerian helped and still helps many people at least lessen, if not solve, their sleeping and anxiety disorders.
Valerian Root Extract INCI Name Valeriana Officinalis Extract EINECS ELINCS No.232-501-7 CAS 8057-49-6 Valerienic acid 109-52-4 photo picture image

Valerian and Insomnia,Sedative Action:All-Heal Effect

Valerian, a tall, wispy perennial plant from Valerianaceae family, grows in Europe and Northern Asia and is cultivated in North America. Its popularity in many cultures from ancient times produced a few tens of names:

Amantilla, All-Heal, Baldrian, Baldrianwurzel, Belgium Valerian, Common Valerian, Fragrant Valerian, Garden Heliotrope, Garden Valerian, Indian Valerian, Mexican Valerian, Pacific Valerian, Valeriana, Valeriana officinalis, Valeriana rhizome, Valerianae radix, Valeriane; Valeriana edulis; Valeriana jatamansii, Valeriana wallichii; Valeriana sitchensis; Capon's Tail, Cat's Love, Garden Heliotrope, Setwall, Spikenard, Vandal root.

From 250 Valerian spices Valerian Officinalis is most frequently used.

Beginning from ancient Greek physicians of all times recommended Valerian as calming, sleep-promoting, soothing, quieting, relaxing and antispasmodic mean. It was believed a remedy for cholera, carminative, anxiolytic, anti-convulsant in epilepsy and pain killer. Different parts of herb were used in soap perfumery and cookery.

Numerous investigations also proved Valerian efficient for mood disorders, attention deficit hyperactivity disorder (ADHD), muscle and joint pain, restlessness, alcoholism, nervous asthma, migraine, stomach upset, menstrual cramps and symptoms associated with menopause.

Almost all mentioned Valerian actions could be explained by its sedative effect on central nervous system. Volatile oil, derived from herb root with pungent odour, appears to contribute to the sedating properties. It contains monoterpenes, sesquiterpenes, valerenic acids, valerenal and valeranone.

The way by which Valerian extract may cause sedation is increase of GABA (gamma aminobutyric acid) production; exactly GABA receptors regulate CNS sedation. In addition, valerenic acid inhibits an enzyme that destroys GABA. Another constituent ,pyruvate,enhances the transport of glucose into the muscle cells.

Today Valerian is widely used for insomnia and various conditions caused by nervous disorders. Comparing to other sleep-promoting medicines Valerian is safe and gentle, not toxic and not produces dependency. It reduces the time it takes to fall asleep and improves the quality of sleep itself. Valerian best woks in case of its rotation with other sleep-inducing herbs like melissa, hops or chamomile.

In case of proper use in recommended doses Valerian herb produce no side effects. Failing overdose it may cause vivid dreams, blurred vision, changes in heart rhythm, stomach upset, itching, fatigue, abdominal cramping, chest tightness, foot and hand tremor or liver damage. Inasmuch as Spikenard may have mutating effects on cells, pregnant and lactating women should avoid use of this herb. It also is not recommended for children under 3 and persons with liver dysfunction.

To avoid dangerous interactions don't take Setwall with other muscle relaxants; narcotic pain relievers; prescription sleep medications; cancer, allergy and antifungal drugs; and alcohol.
Daily dose of All-Heal herb varies for each form medicine sold in (tincture, tablet, liquid, capsule and dried herb/tea), age and condition of the patient.

Reference:

1.Valeriana officinalis.Valerian and Medical Attributes.Valerian Root Extract.

last edit date:1st,Mar.2010.

Available Product

Name:Valerian Root Extract
Serie No:S-029.
Specifications:4:1 TLC,Valerienic acid 0.3%0.4%0.6%0.8%HPLC.
INCI Name:VALERIANA OFFICINALIS EXTRACT
EINECS/ELINCS No.:232-501-7
CAS:8057-49-6.Valerienic acid.109-52-4.
Chem/IUPAC Name:Valeriana Officinalis Extract is an extract of the rhizome and roots of the valerian,Valeriana officinalis,Valerianaceae

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