• Clinical data 90%
  • Efficacy 80%
  • Security 70%
  • Toxicity 30%

Valeriana officinalis
Radix Valerianae

Synonyms

Valeriana alternifolia Ledeb., Valeriana excelsa Poir., Valeriana sylvestris Grosch.

General appearance

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.

Medicinal uses

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.

Pharmacology

Experimental pharmacology

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.

Clinical pharmacology

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.

Contraindications

Radix Valerianae should not be used during pregnancy or lactation.

Warnings

No information available.

News and Journals

References
1. African pharmacopoeia, 1st ed. Lagos, Organization of African Unity, Scientific, Technical
& Research Commission, 1985.
2. British pharmacopoeia. London, Her Majesty’s Stationery Office, 1988.
3. Deutsches Arzneibuch 1996. Stuttgart, Deutscher Apotheker Verlag, 1996.
4. European pharmacopoeia, 2nd ed. Strasbourg, Council of Europe, 1995.
5. Pharmacopée française. Paris, Adrapharm, 1996.
6. Pharmacopoea hungarica VII. Budapest, Medicina konyvkiado, 1986.
7. The Japanese pharmacopoeia XIII. Tokyo, Ministry of Health and Welfare, 1996.
8. Morazzoni P, Bombardelli E. Valeriana officinalis: traditional use and recent evaluation
of activity. Fitoterapia, 1995, 66:99–112.
9. Youngken HW. Textbook of pharmacognosy, 6th ed. Philadelphia, Blakiston, 1950.
10. Bisset NG. Max Wichtl’s herbal drugs & phytopharmaceuticals. Boca Raton, FL, CRC
Press, 1994.
11. Farnsworth, NR. ed. NAPRALERT database. Chicago, University of Illinois at Chicago,
IL, March 15, 1995 production (an on-line database available directly through
the University of Illinois at Chicago or through the Scientific and Technical Network
(STN) of Chemical Abstracts Services).
12. Bruneton J. Pharmacology, phytochemistry, medicinal plants. Paris, Lavoisier, 1995.
13. Jackson BP, Snowden DW. Atlas of microscopy of medicinal plants, culinary herbs and
spices. Boca Raton, FL, CRC Press, 1990.
14. Quality control methods for medicinal plant materials. Geneva, World Health Organization,
1998.
15. Deutsches Arzneibuch 1996. Vol. 2. Methoden der Biologie. Stuttgart, Deutscher
Apotheker Verlag, 1996.
16. European pharmacopoeia, 3rd ed. Strasbourg, Council of Europe, 1997.
17. Guidelines for predicting dietary intake of pesticide residues, 2nd rev. ed. Geneva,
World Health Organization, 1997 (unpublished document WHO/FSF/FOS/97.7;
available from Food Safety, WHO, 1211 Geneva 27, Switzerland).
18. Feytag WE. Bestimmung von Valerensäuren und Valerenal neben Valepotriaten in
Valeriana officinalis durch HPLC. Pharmazeutische Zeitung, 1983, 128:2869–2871.
19. van Meer JH, Labadie RP. Straight-phase and reverse phase high-performance liquid
chromatographic separations of valepotriate isomers and homologues. Journal of
chromatography, 1981, 205:206–212.
20. Graf E, Bornkessel B. Analytische und pharmazeutisch-technologische Versuche mit
Baldrian. Deutsche Apotheker Zeitung, 1978, 118:503–505.
21. Hänsel R, Schultz J. Valerensäuren und Valerenal als Leitstoffe des offizinellen
Baldrians. Bestimmung mittels HPLC-Technik. Deutsche Apotheker Zeitung, 1982,
122:333–340.
22. Leathwood PD, Chauffard F. Quantifying the effects of mild sedatives. Journal of
psychological research, 1982/1983, 17:115.
23. Leathwood PD, Chauffard F. Aqueous extract of valerian reduces latency to fall
asleep in man. Planta medica, 1985, 2:144–148.
24. Schultz H, Stolz C, Muller J. The effect of valerian extract on sleep polygraphy in
poor sleepers: a pilot study. Pharmacopsychiatry, 1994, 27:147–151.
25. Balderer G, Borbely A. Effect of valerian on human sleep. Psychopharmacology, 1985,
87:406–409.
26. Wagner H, Jurcic K, Schaette R. Comparative studies on the sedative action of
Valeriana extracts, valepotriates and their degradation products. Planta medica, 1980,
37:358–362.
27. Santos MS et al. Synaptosomal GABA release as influenced by valerian root extract,
involvement of the GABA carrier. Archives of international pharmacodynamics, 1994,
327:220–231.
28. Santos MS et al. An aqueous extract of valerian influences the transport of GABA in
synaptosomes. Planta medica, 1994, 60:278–279.
29. Santos MS et al. The amount of GABA present in the aqueous extracts of valerian is
sufficient to account for 3H-GABA release in synaptosomes. Planta medica, 1994,
60:475–476.
30. Wagner H, Jurcic K. On the spasmolytic activity of Valeriana extracts. Planta medica,
1979, 37:84–89.
31. Houghton P. Herbal products: valerian. Pharmacy journal, 1994, 253:95–96.
32. Hazelhoff B, Malingre TM, Meijer DKF. Antispasmodic effects of Valeriana compounds:
An in vivo and in vitro study on the guinea pig ileum. Archives of international
pharmacodynamics, 1982, 257:274–278.
33. Krieglstein J, Grusla D. Zentraldämpfende Inhaltsstoffe im Baldrian. Valepotriate,
Valerensäure, Valeranon und ätherisches Öl sind jedoch unwirksam. Deutsche
Apotheker Zeitung, 1988, 128:2041–2046.
34. German Commission E Monograph, Valerianae radix. Bundesanzeiger, 1985, 90:15
May.
35. Tortarolo M et al. In vitro effects of epoxide-bearing valepotriates on mouse early
hematopoietic progenitor cells and human T-lymphocytes. Archives of toxicology,
1982, 51:37–42.
36. Braun R. Valepotriates with an epoxide structure-oxygenating alkylating agents.
Planta medica, 1982, 41:21–28.
37. Tufik S. Effects of a prolonged administration of valepotriates in rats on the mothers
and their offspring. Journal of ethnopharmacology, 1985, 87:39–44.
38. Willey LB et al. Valerian overdose: a case report. Veterinary and human toxicology,
1995, 37:364–365.
39. MacGregor FB. Hepatotoxicity of herbal remedies. British medical journal, 1989,
299:1156–1157.