- Clinical data 90%
- Efficacy 80%
- Security 70%
- Toxicity 30%
Valeriana alternifolia Ledeb., Valeriana excelsa Poir., Valeriana sylvestris Grosch.
Rhizome, erect, entire or usually cut into 2–4 longitudinal pieces, 2–5cm long, 1–3cm thick; externally, dull yellowish brown or dark brown, sometimes crowned by the remains of stem bases and scale leaves, and bears occasional, short, horizontal branches (stolons), and numerous rootlets or their circular scars; fracture, short and horny. Internally, whitish, with an irregular outline, occasionally hollow and exhibiting a comparatively narrow ark traversed, here and there, by root-traces, and separated by a dark line, the cambium, from a ring, small xylem bundles surrounding a central pith. Roots, numerous, slender, cylindrical, usually plump; 2–12cm but mostly 8–10cm long, 0.5–2mm in diameter; externally, greyish brown to brownish yellow, longitudinally striated, with fibrous lateral rootlets; brittle; internally, showing a wide bark and a narrow central stele.
Major chemical constituents of Valeriana officinalis
The chemical composition of Radix Valerianae varies greatly depending on the subspecies, variety, age of the plant, growing conditions, and type and age of the extract. The volatile oil (ranges 0.2–2.8%) contains bornyl acetate and bornyl isovalerate as the principal components. Other significant constituents include -caryophyllene, valeranone, valerenal, valerenic acid, and other sesquiterpenoids and monoterpenes. The co-occurrence of three cyclopentane-sesquiterpenoids (valerenic acid, acetoxyvalerenic acid, and valerenal) is confined to V. officinalis and permits its distinction from V. edulis and V. wallichii. The various subspecies of V. officinalis have different compositions of volatile oil and, for example, average bornyl acetate content varies from 35% in V. officinalis ssp. pratensis to 0.45% in V. officinalis ssp. illyrica.
A second important group of constituents (0.05–0.67% range) is a series of non-glycosidic bicyclic iridoid monoterpene epoxy-esters known as the valepotriates. The major valepotriates are valtrate and isovaltrate (which usually represent more than 90% of the valepotriate content). Smaller amounts of dihydrovaltrate, isovaleroxy-hydroxydihydrovaltrate, 1-acevaltrate or others are present. The valepotriates are rather unstable owing to their epoxide structure, and losses occur fairly rapidly on storage or processing, especially if the drug is not carefully dried. Principal degradation products are baldrinal, homobaldrinal, and valtroxal.
Uses supported by clinical data
As a mild sedative and sleep-promoting agent. The drug is often used as a milder alternative or a possible substitute for stronger synthetic sedatives, such as the benzodiazepines, in the treatment of states of nervous excitation and anxiety-induced sleep disturbances.
Uses described in pharmacopoeias and in traditional systems of medicine
As a digestive aid, and an adjuvant in spasmolytic states of smooth muscle and gastrointestinal pains of nervous origin. When associated with papaverine, belladonna, and other spasmolytics, Radix Valerianae has been shown to be useful as an adjuvant in spastic states of smooth muscle such as spastic colitis.
Uses described in folk medicine, not supported by experimental or clinical data
To treat epilepsy, gum sores, headaches, nausea, sluggish liver, urinary tract disorders, vaginal yeast infections, and throat inflammations; and as an emmenagogue, antiperspirant, antidote to poisons, diuretic, anodyne, and a decoction for colds.
The sedative activity of V. officinalis has been demonstrated both in vitro and in vivo. In vitro studies have demonstrated the binding of valerian extracts to GABA (γ-aminobutyric acid) receptors, adenosine receptors and the barbiturate and benzodiazepine receptors. Both hydroalcoholic and aqueous total extracts show affinity for the GABA-A receptors, but there is no clear correlation between any of the known chemical components isolated from Radix Valerianae and GABA-A binding activity. Aqueous extracts of the roots of V. officinalis inhibit re-uptake and stimulate the release of radiolabelled GABA in the synaptosomes isolated from rat brain cortex. This activity may increase the extracellular concentration of GABA in the synaptic cleft, and thereby enhance the biochemical and behavioural effects of GABA. Interestingly, GABA has been found in extracts of V. officinalis and appears to be responsible for this activity. The valtrates, and in particular dihydrovaltrate, also show some affinity for both the barbiturate receptors and the peripheral benzodiazepine receptors.
In vivo studies suggest that the sedative properties of the drug may be due to high concentrations of glutamine in the extracts. Glutamine is able to cross the blood–brain barrier, where it is taken up by nerve terminals and subse quently metabolized to GABA. The addition of exogenous glutamine stimulates GABA synthesis in synaptosomes and rat brain slices.
The spasmolytic activity of the valepotriates is principally due to valtrate or dihydrovaltrate. These agents act on centres of the central nervous system and through direct relaxation of smooth muscle, apparently by modulating Ca2 entry into the cells or by binding to smooth muscle.
A number of clinical investigations have demonstrated the effectiveness of Radix Valerianae as a sleep aid and minor sedative. In a double-blind study, valerian (450mg or 900mg of an aqueous root extract) significantly decreased sleep latency as compared with a placebo. The higher dose of valerian did not further decrease sleep latency. Additional clinical studies have demonstrated that an aqueous extract of valerian root significantly increased sleep quality, in poor and irregular sleepers, but it had no effect on night awakenings or dream recall. The use of Radix Valerianae appears to increase slow-wave sleep in patients with low baseline values, without altering rapid eye movement (REM) sleep.
While extracts of the drug have been clearly shown to depress central nervous system activity, the identity of the active constituents still remains controversial. Neither the valepotriates, nor the sesquiterpenes valerenic acid and valeranone, nor the volatile oil alone can account for the overall sedative activity of the plant. It has been suggested that the baldrinals, degradation products of the valepotriates, may be responsible. Currently, it is still not known whether the activity of Valeriana officinalis extracts resides in one compound, a group of compounds, or some unknown compound, or is due to a synergistic effect.
Radix Valerianae should not be used during pregnancy or lactation.
No information available.
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