Pharmacognosy · Phytomedicine

Valerian

Valeriana officinalis L. — The pre-eminent botanical sedative of Western medicine, whose root exerts multivalent GABAergic activity through valerenic acid, valepotriates, and flavonoids to promote sleep and reduce anxiety.

51 Primary Refs
14+ Properties
Root Parts Used
✦ Researched
Last Updated
Primary Source Wikiphyto · NCBI PubMed
Family Caprifoliaceae
Evidence Grade B · Multiple RCTs & Meta-Analyses

Biological Overview

Valeriana officinalis is a robust herbaceous perennial whose underground parts — rhizome, roots and stolons — have been used medicinally since antiquity. Its unique bioactivity arises from a synergistic ensemble of valerenic acid sesquiterpenes, iridoid valepotriates, and flavonoids that converge on the GABAergic system through multiple complementary molecular mechanisms, producing sedative, anxiolytic, and spasmolytic effects.

Key ActivesValerenic Acid, Valepotriates, 6-Methylapigenin, Linarin
Primary TargetsGABA-A Receptors, GABA-T, Adenosine A1, 5-HT5a
Evidence Base51 refs · Meta-analysis, multiple RCTs
Traditional SystemWestern Herbalism, Homeopathy, EMA-Registered
Botanical Classification

Taxonomy & Identification

Latin Name
Valeriana officinalis L.
Family
Caprifoliaceae (APG IV); ex-Valerianaceae
Common Names
Valerian, Garden Valerian, All-Heal, Herb of Cats
French Name
Valériane, Herbe aux chats
Parts Used
Rhizome, roots and stolons (underground parts)
Origin
Temperate Europe; widely cultivated worldwide
Pharmacopoeia
French Pharmacopoeia, List A; EMA monograph
Morphology & Distribution

Description & Habitat

Valeriana officinalis is a robust herbaceous perennial of damp, shaded habitats — riverbanks, marshes, and moist meadows — widely distributed across temperate Europe. Stems are hollow, ribbed (cannelées), and can reach up to 2 metres in height, extensively branched at the summit. Basal and cauline leaves are pinnatisect with toothed lobes.

The inflorescence consists of terminal umbelliform cymes bearing small white or pink flowers. The underground parts — rhizome, roots and stolons — develop a characteristically pungent odour on drying, due to isovalerenic acid formation. This same compound attracts cats, explaining the common name "herb of cats." Temperate Europe is the natural range, though the plant is extensively cultivated globally to supply the pharmaceutical industry.

Name Etymology

The name "Valerian" derives from the Latin valere — "to be in good health" — the same root as "valid" and "convalescence." The species name officinalis signals its long-established place in the official pharmacopoeia. The plant's association with cats (herbe aux chats) arises because actinidine, an alkaloid trace-component, is also present in Nepeta cataria and acts as a feline attractant.

Morphological Profile
Growth HabitRobust herbaceous perennial, up to 2 m tall
StemsHollow, ribbed (cannelées), highly branched at apex
LeavesPinnatisect with toothed lobes; basal and cauline
FlowersSmall, white or pink; terminal umbelliform cymes
Underground PartsRhizome + roots + stolons; strongly aromatic when dried
HabitatDamp meadows, riverbanks, marshes; temperate Europe

Drying Note

The underground parts must be dried carefully at temperatures below 40 °C. Valepotriates are thermolabile and decompose above this threshold, and most commercial preparations have been shown chromatographically to be devoid of intact valepotriates — though their degradation products (baldrinals) remain pharmacologically active.

Ethnobotany & Traditional Use

History & Tradition

Before the advent of synthetic tranquillisers, valerian root was regarded as the most effective calming agent available to Western medicine. Its documented use stretches from ancient Greece to the World War trenches, spanning more than 2,000 years of continuous medicinal application across diverse cultural traditions. The genus encompasses some 200 species distributed worldwide.

Ancient Greece & Rome

Hippocrates & Dioscorides

Hippocrates and Dioscorides recommended valerian for insomnia. Roman physicians used it to combat palpitations and arrhythmia. The name derives from the Latin valere — to be in good health.

Middle Ages — Europe

Tranquilliser & Soporific

Medieval European physicians prescribed valerian as a tranquilliser and soporific. From the late 16th century it was employed for epilepsy across Europe. Native Americans used it in powder form to calm epileptic convulsions.

World War I — 1914–1918

Shell Shock & Nervous Trauma

Use of valerian expanded dramatically to treat the nervous shock caused by artillery bombardment. Soldiers suffering acute psychogenic stress were treated with valerian preparations — an indication that anticipated modern understanding of GABAergic anxiolysis.

Modern Era — EMA Recognition

Global Cultivation & Regulatory Status

Valerian is now cultivated in numerous countries to supply the pharmaceutical industry. It holds formal European Medicines Agency (EMA) monograph status for both the root and its essential oil, and is listed on the French Pharmacopoeia (List A). [1]

Traditional Indications

  • ▸ Insomnia & sleep onset difficulties
  • ▸ Nervous excitability & palpitations
  • ▸ Epilepsy (historical adjuvant)
  • ▸ Anxiety & nervous tension
  • ▸ Spasms & cramps
  • ▸ Homeopathic: hysteric neuropathy, myoclonus

Cat Attraction

The root odour mimics feline urine due to isovalerenic acid. The alkaloid actinidine — also present in Nepeta cataria — is a specific feline attractant. Interestingly, the tisane has an unpleasant taste, unlike catnip (Nepeta cataria) infusions.

Pharmaceutical Forms

Parts Used & Formulations

Dried underground parts (rhizome, roots, stolons) are the pharmacopoeial material. Multiple galenical preparations are available; valepotriate content varies significantly by preparation method.

Pharmacopoeial Material

Dried underground parts of Valeriana officinalis L. s.l., comprising the rhizome surrounded by roots and stolons. Must be dried carefully at temperatures below 40 °C to preserve thermolabile valepotriates.

Available Forms

  • ▸ Mother tincture (underground parts)
  • ▸ Dry extract (extrait sec)
  • ▸ Fluid extract (extrait fluide)
  • ▸ EPS (extrait de plantes standardisé)
  • ▸ Herbal tisane (infusion)
  • ▸ Essential oil (supercritical CO₂ or steam)

Valepotriate Note

Most commercial specialities have been shown by chromatography to be devoid of intact valepotriates, which are unstable and degrade above 40 °C and in gastric acid. Their degradation products — baldrinals and derivatives — are pharmacologically active and contribute to the antidepressant effect.

Clinical Dosimetry

Dosages

Dosages sourced from primary literature and the EMA monograph. All preparations should be used under the supervision of a qualified healthcare provider.

Indication Form Dose Notes
Mood support (thymoanaleptic) Dry extract 100 mg Lower dose — mood-lifting rather than soporific
Sleep induction Dry extract 400 mg Soporific dose; equivalent to ~2–2.5 g root powder
Nervousness (adult) Capsules 270 mg dry extract 2 capsules morning & evening 540 mg/day dry extract total
Maximum adult dose Dry extract 800 mg/day Corresponding to ~4–5 g root powder
Essential oil (EMA) Essential oil 15 mg × 2–3 per day (30–45 mg/day) Per EMA/HMPC/278053/2015 [2]
Phytochemistry

Composition

The bioactivity of valerian root arises from a complex interplay of structurally distinct compound classes that individually and synergistically modulate the GABAergic system.

Principal Root Compounds

Non-volatile SesquiterpenesValerenic acid, isovalerenic acid, hydroxy-valerenic acid, acetoxy-valerenic acid — principal anxiolytic & GABAergic agents
Principal
Sesquiterpene Ketones & AlcoholsValeranone (hypotensive at 5 mg/kg), valerianool, maaliol, kessyl alcohol, valerénal
Present
Iridoids — Valepotriates0.5–1.2%; valtrate (80%), isovaltrate, acevaltrate, dihydrovaltrate, isovaleroxyhydroxydihydrovaltrate — anxiolytic, antidepressant; thermolabile
0.5–1.2%
Alkaloids (traces)Valeramine, actinidine (feline attractant)
Trace
Lignans8-Hydroxypinorésinol — benzodiazepine receptor ligand, strongly neuroprotective
Present
Flavonoids6-Methylapigenin (GABA-A ligand, anxiolytic), 2-S-(-)-hesperidin, linarin (sedative & sleep-enhancing)
Present
GABAPresent in aqueous root extracts; direct sedation debated due to uncertain bioavailability
Debated

Essential Oil (>0.5%)

MonoterpenesBorneol — potentiates GABA sensitivity at GABA-A receptors
Present
Sesquiterpenesβ-caryophyllene, cadinene and derivatives
Present
EstersBornyl acetate, bornyl isovalerate
Present

Key Active — Valerenic Acid

GABA-A Receptor Modulation

Valerenic acid is a partial agonist at GABA-A receptors, enhancing benzodiazepine binding at low concentrations and inhibiting GABA-transaminase — the enzyme responsible for GABA catabolism

Glutamatergic Activity

Valerenic acid also interacts selectively with glutamatergic receptors, adding a second inhibitory neuronal mechanism beyond pure GABAergic action

Plant Properties — Pharmacodynamics

Whole-plant biological activities with primary literature citations

14+ Properties Meta-Analysis Validated Multi-Receptor Activity

Soporific / Sleep-Inducing

Multiple meta-analyses confirm sleep-inducing activity. [3][4] A 2020 systematic review and meta-analysis confirmed valerian as an effective sleep inducer. [5] Valerian improves sleep structure and quality. [6] A 2024 double-blind RCT with a 2% valerenic acid standardised extract demonstrated reduced sleep onset latency, improved sleep quality, efficiency and total sleep duration. [7]

Anxiolytic

Anxiolytic activity demonstrated in clinical and preclinical studies. [8][9] Valerenic acid is identified as the primary anxiolytic constituent. [10][11][12] Anxiolytic effect is accentuated in combination with lemon balm (Melissa officinalis). [13]

GABAergic — GABA Reuptake Inhibition

Valerian extracts inhibit GABA reuptake and stimulate GABA release at synaptic terminals. [14][15] Valerenic acid is a GABA-A receptor ligand and inhibits GABA-transaminase. [16] GABA catabolism is inhibited, prolonging GABAergic signalling. [17][18]

Benzodiazepine Receptor Binding

Sesquiterpenes and valepotriates bind benzodiazepine receptors. Flavonoids such as apigenin, hesperidin, and linarin bind central receptors. 6-Methylapigenin, an anxiolytic flavonoid, is a competitive ligand for the benzodiazepine binding site and for GABA-A receptors. [19]

Adenosine A1 Receptor Agonism

Valerian extracts show partial agonist activity at adenosine A receptors, which play a role in neurotransmitter release modulation. [20] A lignan fraction is an agonist of the adenosine A1 receptor, and hydroxypinorésinol binds benzodiazepine receptors and is strongly neuroprotective. [27][28][29]

Molecular Synergy (GABAergic)

Valerian exhibits GABAergic effects through diverse molecular synergies. [21][22] Low extract concentrations enhance benzodiazepine binding at GABA-A; valerenic acid inhibits enzymatic GABA degradation. [23][24] Valerenic acid also interacts with glutamatergic receptors. [25]

Borneol — GABA Sensitisation

Borneol (both (+) and (−) enantiomers) increases the sensitivity of GABA-A receptors to their natural ligand, acting as a positive modulator. [26] This EO monoterpene thus amplifies the overall GABAergic synergy unique to the whole-root extract.

Flavonoid Synergy

6-Methylapigenin and hesperidin act synergistically on CNS receptors. [30] Linarin, another flavonoid isolated from Valeriana officinalis, has documented sedative and sleep-enhancing properties in its own right.

Antistress — Monoaminergic

Valerian reduces induced stress by diminishing the ratio of monoaminergic neurotransmitters to their metabolites, demonstrating inhibitory effects on both physical (electric shock) and psychological (nociceptive) stress responses. [31]

Serotonergic — 5-HT5a Agonism

Valerian extract and valerenic acid are partial agonists of the 5-HT5a serotonin receptor, which plays a role in serotonergic regulation of the circadian cycle. [32] Valerian increases 5-hydroxytryptamine levels and promotes hippocampal cell proliferation in depressive rat models. [33]

Sedative & Anticonvulsant

Central nervous system depressant and anticonvulsant activity demonstrated. [34] Anti-epileptic effects shown on animal models — valerenic acid and extracts delay seizure onset in zebrafish PTZ models. [35]

Antidepressant (Valepotriates)

Valepotriates have antidepressant properties. While largely absent from commercial preparations due to instability, their degradation products — baldrinals and derivatives — retain pharmacological activity. This framing distinguishes valerian from simple sedatives with a potential mood-modulating dimension.

Hypotensive

Valeranone exerts hypotensive effects at 5 mg/kg in animal models — a minor but documented pharmacological activity attributable to the sesquiterpene ketone fraction of the root.

Neuroprotective

Hydroxypinorésinol (a lignan) is strongly neuroprotective against oxidative damage. [28][29] Flavonoids hesperidin and linarin interact with SUR1 receptors, suggesting potential in Parkinson's disease through mechanisms identified by in silico modelling. [43]

Aromatherapy

Essential Oil Properties

The essential oil (>0.5% of root dry weight) concentrates GABAergic-active esters and acids. Supercritical CO₂ extraction appears to concentrate active principles more effectively than hydrodistillation.

🧪

GABAergic Aroma Compounds

Isovaleric acid, valerenic acid, and bornyl acetate increase GABA activity by reducing GABA-transaminase activity — the catabolic enzyme — thereby raising synaptic GABA levels. These mechanisms are operative via inhalation as well as oral routes. [36]

💨

Inhalation & Sleep Extension

Inhalation of valerian's aromatic molecules significantly prolongs pentobarbital-induced sleep time in animal models, confirming that the volatile fraction exerts genuine CNS depressant activity via the olfactory pathway — independent of oral ingestion. [38]

🌿

Supercritical CO₂ Extraction

Comparative analysis between supercritical CO₂ extraction and conventional hydrodistillation shows that CO₂ extraction concentrates the pharmacologically active sesquiterpenic and ester fractions more effectively, yielding a more potent essential oil. [37]

😴

EO Clinical Indications

Specific aromatherapeutic indications for the essential oil include anxiety and insomnia. The EMA recommends 2–3 administrations of 15 mg per day (30–45 mg/day total) for the essential oil preparation. [2]

Clinical Applications

Clinical Indications

Indications of the whole plant (phytotherapy) and essential oil (aromatherapy), translated and organised from primary literature with supporting references.

🌙
Sleep Disorders
Primary Clinical Indication
  • Sleep onset insomnia: primary indication, particularly for difficulties falling asleep; efficacy documented in combination with hops (Humulus lupulus) [39] even after a single administration [40]
  • Menopausal insomnia: valerian improves sleep quality in postmenopausal women with insomnia [41]
  • Combined valerian + hops: a literature review of studies from 1950–2009 found improvement in sleep parameters with valerian alone or with hops, though further controlled trials were recommended [42]
  • Nervous excitability, palpitations of nervous origin
🧠
Anxiety & Nervous System
Anxiolytic & Adaptogenic
  • Anxiolytic & mildly antidepressant: ruminating anxiety, chronic stress exposure, postural contractures of stress
  • Neurotonic states & neuro-vegetative dystonias in adults and children; hyperactive alpha-sympathetic stress response
  • Memory preservation in depressive patients — avoids stress-related memory loss
  • Tension headaches: randomised placebo-controlled double-blind trial demonstrates efficacy [44]
  • Adjuvant in smoking cessation and epilepsy (petit mal in children)
🔬
Neuroprotection & Emerging
Research Applications
  • Neuroprotection: potential in Parkinson's disease via SUR1 receptor interactions of hesperidin and linarin [43]
  • Insufficient pituitary-adrenal response to chronic stress
  • Homeopathic indications: hysteric neuropathy, hyperaesthesia, emotional exacerbation, changeable mood, lowered pain threshold, spasms, myoclonus, cramps, spasmophilia [45]
🌸
Essential Oil Indications
Aromatherapy
  • Anxiety — inhalation of volatile compounds confirmed to modulate GABAergic tone [36]
  • Insomnia — sleep prolongation demonstrated in animal models via aromatherapeutic route [38]
Pharmacodynamics

Mode of Action

Valerian's activity results from convergent multi-compound, multi-receptor interactions — not a single active molecule — representing a paradigm of phytochemical synergy.

⚡

GABA Reuptake Inhibition & Release

Valerian inhibits the reuptake of GABA into synaptic terminals and stimulates presynaptic GABA release. Valerenic acid inhibits GABA-transaminase (GABA-T) — the primary enzyme of GABA catabolism — thereby elevating synaptic GABA concentrations and prolonging inhibitory neurotransmission. [14][15][16][17]

🔗

Benzodiazepine Receptor Binding

Sesquiterpenes, valepotriates, and flavonoids all bind benzodiazepine receptor sites — albeit with lower affinity than synthetic benzodiazepines. Valepotriates decompose into baldrinals and valerianic acid derivatives in the gastrointestinal tract; these metabolites retain pharmacological activity. This explains the efficacy of preparations from which intact valepotriates are absent.

🧬

Alpha-Sympatholytic Effect

Valerian acts as an alpha-sympatholytic agent, modulating the hyperactive sympathetic tone characteristic of chronic stress states — the physiological underpinning of its traditional use in neuro-vegetative dystonias and stress-related somatic symptoms.

🌊

Serotonergic & Glutamatergic Interactions

Valerenic acid is a partial agonist at 5-HT5a serotonin receptors, influencing circadian regulation. It additionally interacts with glutamatergic synaptic membranes, [25] while valeranol and maaliol contribute to overall inhibitory CNS tone through additional receptor pathways.

Legal & Regulatory Status

Regulation

French Pharmacopoeia — List A (Underground Parts)

The underground parts of Valeriana officinalis (rhizome, roots and stolons) are listed on the French Pharmacopoeia, List A — designating medicinal plants whose use in preparations intended for the public is reserved for pharmacy.

EMA / HMPC Herbal Monograph — Essential Oil

The European Medicines Agency Committee on Herbal Medicinal Products (HMPC) has issued a formal European Union herbal monograph for the valerian essential oil (EMA/HMPC/278053/2015), establishing its regulatory status and recommended dosages across the EU. [2]

Clinical Safety

Safety & Precautions

Valerian has a well-established safety profile in standard dosages. Rare hepatotoxic events have been reported in the context of polyherbal preparations. Drug interactions via CYP enzymes warrant attention.

⚠️

Adverse Effects & Toxicity

  • General safety review: a literature review concludes there is no evidence calling into question valerian's safety, even in cancer patients [46]
  • Overdose effects: supra-therapeutic dosing may produce asthenia, hypotension, heavy-headedness, mydriasis, and abdominal pain
  • Valepotriate toxicity: in vitro cytotoxicity reported at 400 mg/kg — not clinically relevant at standard doses
  • Rare hepatotoxicity: three cases of hepatomegaly with acute hepatitis and centrilobular necrosis reported following a polyherbal preparation containing valerian; liver function normalised within 3 months of discontinuation [50][51]
🚫

Contraindications & Drug Interactions

  • CYP450 interactions: documented interactions with cytochromes P450 1A2, 2D6, 2E1, and 3A4/5 — relevant for patients on drugs metabolised by these pathways [47][48]
  • Benzodiazepine interactions: possible pharmacodynamic interaction; a clinical case of interaction with lorazepam combined with Passiflora incarnata has been reported [49]
  • Children: avoid use in children without specialist supervision
  • Pregnancy: avoid during pregnancy
Clinical Disclaimer: This monograph is for educational and professional reference only. It does not constitute medical advice, diagnosis, or treatment guidance. Valeriana officinalis preparations should be used under the supervision of a qualified healthcare provider. The Health Reference reviews content against current primary literature.
Common Questions

Frequently Asked Questions

What is the main active compound in valerian root?
The principal bioactive compounds are valerenic acid and its derivatives (isovalerenic acid, hydroxy- and acetoxy-valerenic acid), iridoid valepotriates (valtrate, isovaltrate, acevaltrate), and flavonoids including 6-methylapigenin, linarin, and hesperidin. Valerenic acid is the most extensively characterised, acting as a GABA-A receptor ligand and inhibiting GABA-transaminase to sustain inhibitory neurotransmission. No single compound is responsible — valerian's effects are the product of polypharmacological synergy across all these molecular classes.
What does the clinical evidence say about valerian for sleep?
A 2020 systematic review and meta-analysis confirmed valerian as an effective sleep-inducing agent. Multiple randomised placebo-controlled trials have documented improvements in sleep quality, sleep latency, and total sleep time. A 2024 double-blind RCT using a standardised extract with 2% valerenic acid demonstrated significant reductions in sleep onset time and improvements in overall sleep quality, efficiency, and duration. Evidence for combined valerian + hops preparations is also positive, though some reviews call for larger controlled trials.
What is the recommended clinical dosage?
Primary literature cites 100 mg dry extract for mood support and 400 mg for sleep induction. For nervousness in adults, 2 capsules of 270 mg morning and evening is the cited regimen. The maximum dose is 800 mg dry extract per day, corresponding to approximately 4–5 g of root powder. For the essential oil, the EMA recommends 15 mg × 2–3 per day (30–45 mg total). All preparations should be used under the supervision of a qualified healthcare provider.
Can valerian be combined with hops or lemon balm?
Yes — both combinations have clinical support. Valerian + hops combinations have been studied in randomised controlled trials for insomnia, with positive outcomes even after a single dose. Valerian + lemon balm (Melissa officinalis) combinations demonstrate an accentuated anxiolytic effect compared to either plant alone, suggesting pharmacodynamic synergy. These are among the best-evidenced multi-herb combinations in European phytomedicine.
Is valerian safe to use alongside prescription sedatives or benzodiazepines?
Caution is required. Valerian has documented interactions with CYP450 enzymes (1A2, 2D6, 2E1, 3A4/5), and a clinical case of pharmacodynamic interaction with lorazepam has been published. Because valerian enhances GABAergic transmission through mechanisms overlapping with benzodiazepines, additive CNS depression is theoretically possible. Valerian should not be combined with benzodiazepines, sedative-hypnotics, or other CNS depressants without explicit medical supervision.
Why does valerian smell unpleasant after drying?
Fresh valerian root has little odour. On drying and storage, isovaleric acid (isovalérenic acid) is generated through enzymatic degradation — this is the compound responsible for the characteristic pungent, "sweaty socks" odour. The same compound also gives valerian its cat-attracting quality. Interestingly, the alkaloid actinidine — also present in catnip (Nepeta cataria) — contributes additionally to the feline-attractant property, whereas the tisane itself has an unpleasant taste quite unlike catnip infusions.
Primary Literature

Bibliography

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Additional Clinical & Reference Literature

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