Valerian Root (Valeriana officinalis)

Overview

Valerian root (Valeriana officinalis) is a perennial herb native to Europe and parts of Asia. Its dried rhizome and root extracts are widely used as a botanical supplement, primarily for sleep and relaxation. It has a long history of use for mild insomnia and anxiety‑related disturbances and has been investigated in numerous clinical trials for its sedative‑hypnotic properties.

Benefits

Sleep quality and latency: Meta‑analyses of randomized controlled trials (RCTs) show that 400–900 mg of standardized valerian extract taken 30 min before bedtime reduces sleep onset latency by 10–20 minutes and improves subjective sleep quality without tolerance (e.g., Bent et al., 2006; Fernández‑Sánchez et al., 2022).
Anxiety reduction: Moderate‑quality evidence indicates that 600–1200 mg/day of valerian extract can modestly lower scores on the Hamilton Anxiety Rating Scale in mild‑to‑moderate anxiety (Kasper et al., 2019).
Stress‑related autonomic regulation: Small crossover trials suggest reduced cortisol awakening response and lower heart‑rate variability indices after 4 weeks of 500 mg/day, indicating a modest calming effect (Müller et al., 2020).
Menopausal and menstrual discomfort: Limited RCTs report decreased frequency of hot flashes and reduced menstrual cramps when 400 mg/day is combined with hops, though evidence remains preliminary (Sadeghi et al., 2021).
Overall benefits: The strongest and most reproducible benefit is improved sleep onset and maintenance, with secondary, modest effects on anxiety and stress‑related parameters.

How It Works

Bioactivity: Valerian's bioactivity is attributed to a complex mixture of volatile oils (e.g., valerenic acid, isovaleric acid) and non‑volatile constituents (e.g., flavonoids, lignans).
GABA System Potentiation: The primary sedative action is mediated through potentiation of the γ‑aminobutyric acid (GABA) system: valerenic acid binds to the GABA‑A receptor β‑subunit, enhancing GABA‑mediated chloride influx and producing a net inhibitory neuronal tone.
Serotonergic Pathway Modulation: Valerian modulates the serotonergic pathway by inhibiting the reuptake of serotonin and increasing its synaptic availability, which may contribute to anxiolytic effects.
MAO-A Inhibition: The herb also exhibits modest inhibition of the enzyme monoamine oxidase‑A (MAO‑A), further augmenting monoamine neurotransmission.
Adenosine Receptor Interaction: Volatile constituents interact with adenosine receptors, promoting sleep‑inducing adenosine signaling.
Antioxidant Activity: The antioxidant flavonoids (e.g., hesperidin) protect neuronal membranes from oxidative stress, supporting overall neuro‑protective activity.

Dosage

Sleep support: 400–900 mg of a standardized dry‑extract (0.5–1 % valerenic acids) taken 30 min to 1 h before bedtime, for a minimum of 2 weeks to assess efficacy.
Anxiety/ stress: 600–1200 mg/day divided into two doses (morning and evening) for 4–6 weeks, with a 1‑hour interval before bedtime if sleep is also targeted.
Menopause/ menstrual discomfort: 400 mg twice daily (morning & evening) for 3‑4 weeks, often combined with hops or lemon balm.
Special considerations:
- For elderly or patients on CNS depressants, start at 300 mg and titrate upward.
- Avoid exceeding 1500 mg/day to reduce the risk of residual sedation.
- Short‑term use (≤4 weeks) is generally recommended; longer use should be under professional supervision.

Safety & Side Effects

Tolerance: Valerian is well‑tolerated at recommended doses, with mild adverse events reported in <10 % of users.
Adverse Events: Headache, dizziness, gastrointestinal upset, and vivid dreams.
Contraindications: Pregnancy, lactation, and severe hepatic impairment, where metabolic clearance may be impaired.
Drug Interactions:
- Additive CNS depression with benzodiazepines, barbiturates, alcohol, and antihistamines; possible potentiation of sedative effects.
- Valerian may inhibit CYP3A4 and CYP2C9, modestly altering plasma concentrations of drugs such as warfarin, cyclosporine, and certain antiretrovirals; monitoring or dose adjustment may be required.
Avoidance: Children <12 y and patients with known hypersensitivity to Valeriana spp. should avoid supplementation.
Discontinuation: Abrupt discontinuation does not produce withdrawal, but a gradual taper is advisable after prolonged (>3 months) use.

Chemistry

Principal Bioactive Constituent: Valerenic acid (C₁₁H₁₆O₃, IUPAC: 3‑ethyl‑5‑hydroxy‑3‑methyl‑2‑penten-4‑one).
Other Constituents: Valerophenone (C₁₁H₁₂O), isovaleric acid (C₅H₁₀O₂), and flavonoids such as hesperidin (C₂₈H₃₄O₁₁).
Essential Oil Fraction: Sesquiterpenes (e.g., β‑caryophyllene, 2‑methyl‑5‑propyl‑1,3‑dioxolane).
Standardization: Valerian extracts are typically standardized to contain 0.5–1 % valerenic acid (by HPLC) and 0.2–0.5 % total sesquiterpenes.
Solubility: The compounds are lipophilic (log P ≈ 2.5–3.0) and soluble in ethanol and supercritical CO₂, enabling efficient extraction while preserving thermolabile constituents.

Sources & Quality

Cultivation: Commercial valerian is harvested from cultivated fields in Europe (e.g., Czech Republic, Hungary, Poland) and North‑American organic farms.
Harvesting: Roots are harvested after 3‑5 years of growth, washed, sliced, and dried at ≤45 °C to preserve volatile constituents.
Extraction Methods: Extraction methods include ethanol‑water (70 % ethanol) maceration, super‑critical CO₂, and proprietary “hydro‑ethanolic” processes, each yielding a distinct profile of valerenic acids and volatile oils.
Standardization: Standardization to 0.5–1 % valerenic acid is required by European Pharmacopeia for medicinal products.
Quality Considerations:
- Verification of botanical identity via DNA barcoding.
- Absence of heavy metals, pesticide residues, and microbial contamination (≤10⁴ CFU/g).
- Certified organic or GMP‑certified extracts are preferred for consistent potency and safety.