Valerian Root

• Sleep quality improvement
• Stress reduction
• Anxiety relief

• Muscle relaxation
• Menstrual cramp relief
• Digestive comfort
• Headache relief
• Cognitive support during stress

Valerian root (Valeriana officinalis) exerts its primary effects through multiple mechanisms centered on the GABAergic system, the main inhibitory neurotransmitter network in the central nervous system. The herb contains over 150 chemical constituents, with valerenic acid and its derivatives being the most well-studied active compounds.

These compounds work synergistically to promote relaxation, reduce anxiety, and improve sleep quality through direct and indirect modulation of GABA receptors, inhibition of GABA breakdown, and effects on other neurotransmitter systems. Unlike benzodiazepines, valerian appears to work through multiple subtle mechanisms rather than potent action at a single target, which may explain its generally milder effects and favorable safety profile.

The optimal dosage of valerian root varies based on the preparation method, standardization, and individual factors. For sleep and anxiety, research typically uses 300-900 mg of dried root extract taken 30-60 minutes before bedtime. Standardized extracts are often calibrated to contain 0.3-0.8% valerenic acid, which serves as a marker compound for quality and potency. There is no established Recommended Dietary Allowance (RDA) for valerian as it is not considered an essential nutrient.

Individual response varies significantly, with some people requiring higher doses for effect while others may be sensitive to lower doses.

Valerian root contains numerous bioactive compounds with varying pharmacokinetic profiles, making its overall bioavailability complex to characterize. The key marker compounds, including valerenic acid and its derivatives, have relatively low oral bioavailability due to poor water solubility, extensive first-pass metabolism, and potential efflux transport. The bioavailability of valerian’s active compounds is influenced by extraction method, formulation, and individual factors such as gastrointestinal function and genetic variations in metabolizing enzymes.

Different preparation methods can significantly affect which compounds are extracted and their subsequent bioavailability.

General Characteristics: Absorption of valerian’s active compounds occurs primarily in the small intestine, with limited absorption in the stomach. The rate and extent of absorption vary significantly by compound class and are influenced by their physicochemical properties.

Compound Specific Absorption:

General Characteristics: After absorption, valerian’s active compounds are distributed throughout the body via the bloodstream, with varying degrees of tissue penetration based on their physicochemical properties.

Blood-brain Barrier Penetration: Valerenic acid and its derivatives can cross the blood-brain barrier due to their lipophilic nature and relatively small molecular size, which is crucial for their central nervous system effects. Some water-soluble components like GABA have limited BBB penetration, suggesting their effects may be indirect or peripheral.

Protein Binding: Valerenic acid demonstrates moderate to high plasma protein binding (approximately 70-90%), primarily to albumin. This protein binding affects its free concentration and tissue distribution but may also protect it from rapid metabolism and elimination.

Tissue Distribution: Lipophilic compounds like valerenic acid and essential oil components show preferential distribution to lipid-rich tissues including the brain, liver, and adipose tissue. Limited studies suggest accumulation in the liver, which is also the primary site of metabolism.

General Characteristics: Valerian’s active compounds undergo extensive metabolism, primarily in the liver through Phase I and II reactions, with some compounds also metabolized by the gut microbiota.

Hepatic Metabolism: Cytochrome P450 enzymes (particularly CYP3A4, CYP2D6) catalyze oxidation, reduction, and hydroxylation reactions of valerenic acid and other lipophilic compounds., Conjugation reactions, including glucuronidation (via UDP-glucuronosyltransferases) and sulfation (via sulfotransferases), are common for valerenic acid and its phase I metabolites.

Gut Microbial Metabolism: The gut microbiota plays a significant role in metabolizing certain valerian compounds, particularly valepotriates which may be hydrolyzed to produce baldrinals and other metabolites. These microbial metabolites may contribute to the bioactivity of valerian.

Metabolic Pathways:

General Characteristics: Valerian’s active compounds and their metabolites are primarily eliminated via biliary excretion followed by fecal elimination, with some renal excretion of water-soluble metabolites.

Half Life: The elimination half-life varies among compounds: valerenic acid typically has a half-life of 1-2 hours in humans. Some metabolites may have longer half-lives.

Excretion Routes: Conjugated metabolites are excreted in bile and appear in feces after potential deconjugation by gut bacteria. Water-soluble metabolites are excreted in urine.

Enterohepatic Circulation: Some evidence suggests that valerenic acid and its metabolites may undergo enterohepatic circulation, where they are excreted in bile, deconjugated by gut bacteria, reabsorbed, and recirculated. This process can extend their presence in the body and contribute to prolonged effects.

Pharmacokinetic Studies: Limited human pharmacokinetic studies with small sample sizes; most detailed studies conducted in animals

Analytical Challenges: Complex mixture of compounds makes comprehensive pharmacokinetic characterization difficult; focus on marker compounds may not capture full activity profile

Standardization Issues: Variable standardization approaches between products and studies complicates comparison of results

Knowledge Gaps: Limited understanding of active metabolites, enterohepatic circulation, and long-term pharmacokinetics with regular use

Valerian root has a generally favorable safety profile based on both traditional use spanning thousands of years and modern clinical research. It is well-tolerated by most individuals at recommended doses, with infrequent and typically mild adverse effects. Unlike many conventional sedatives, valerian does not appear to cause significant tolerance, dependence, or withdrawal symptoms with long-term use. However, certain populations should exercise caution, and potential interactions with medications should be considered.

The safety profile is best established for short to medium-term use (up to 4-8 weeks), with more limited data on very long-term consumption.

Common Mild:

Rare Serious:

Pediatric:

• Limited data on safety in children. Some clinical studies have used valerian in children over 3 years for sleep disorders and attention issues with good tolerability, but long-term safety not established.
• Reduced dosing based on age and weight; typically 1/3 to 1/2 adult dose for children 3-12 years.
• Potential for increased sensitivity to neurological effects; limited safety data in this population.

Geriatric:

• Generally safe in older adults, with potential benefits for age-related sleep disturbances. May be more sensitive to effects due to age-related changes in metabolism.
• Start with lower doses (300 mg) and titrate slowly. May be more sensitive to sedative effects.
• Increased risk of drug interactions due to polypharmacy common in older adults; potential for enhanced sedation or dizziness that could increase fall risk; monitor for morning drowsiness.

Pregnant And Lactating:

• Not recommended during pregnancy and lactation due to insufficient safety data and traditional cautions about potential uterine stimulant effects.
• Avoid use during pregnancy and lactation.
• No adequate studies in pregnant or lactating women; animal studies insufficient to establish safety profile for pregnancy.

Hepatic Impairment:

• Caution advised due to metabolism of key compounds in the liver and rare case reports of hepatotoxicity. Severe liver disease is a contraindication.
• Avoid use in severe liver impairment; consider reduced doses (50% of standard) in mild to moderate impairment if used.
• Monitor liver function tests if used regularly in patients with pre-existing liver disease.

Renal Impairment:

• Limited data, but likely safe in mild to moderate renal impairment as most active compounds undergo hepatic metabolism with limited renal elimination.
• No specific adjustments needed for mild to moderate impairment; use caution in severe renal disease.
• No specific monitoring required beyond standard care for renal disease.

Psychiatric Conditions:

• Generally safe for anxiety and stress-related conditions, but caution advised in severe depression or bipolar disorder.
• Theoretical risk of worsening depression due to sedative effects; potential for interaction with psychiatric medications.
• Use under healthcare provider supervision in individuals with significant psychiatric conditions.

Acute Toxicity:

• No established LD50 in humans; animal studies show very low toxicity with LD50 > 5000 mg/kg for extracts in rodents
• No formal maximum tolerated dose established; doses up to 20 g of dried root have been used in traditional medicine without serious adverse effects
• Theoretical symptoms might include excessive sedation, headache, gastrointestinal distress, and dizziness, though documented cases are extremely rare
• Supportive care; symptoms expected to resolve within 24-48 hours due to relatively short half-life of active compounds

Chronic Toxicity:

• Clinical studies up to 28 days show favorable safety profile; traditional use suggests safety with long-term consumption, though modern controlled studies of very long-term use are limited
• No evidence of carcinogenic potential in available studies
• No mutagenic effects observed in standard assays
• Insufficient data in humans; some traditional sources suggest avoiding during pregnancy due to potential uterine stimulant effects
• Rare case reports of hepatotoxicity, but causal relationship not established; no other specific organ toxicity identified in clinical studies or post-marketing surveillance at recommended doses

Adulteration:

• Substitution of Valeriana officinalis with other Valeriana species; adulteration with other plant materials; synthetic additives to enhance sedative effects
• HPLC analysis of valerenic acid content; microscopic analysis; DNA barcoding
• Purchase from reputable sources; look for products with third-party testing certification; standardized extracts with specified valerenic acid content offer more reliable quality

Contamination:

• Heavy metals, pesticide residues, microbial contamination, mycotoxins
• Should meet USP, EP, or equivalent pharmacopeial standards for herbal preparations
• Third-party testing, Good Manufacturing Practices (GMP) certification, organic cultivation when possible

Standardization Issues:

• Variability in active compound content between products; degradation of unstable compounds during processing and storage
• Valerenic acid content is the primary quality marker; should be standardized to 0.3-0.8% in high-quality extracts
• Look for products that specify standardization parameters; check for expiration dates and proper storage conditions

Us Fda: Sold as dietary supplement under DSHEA regulations; not approved as a drug

European Medicines Agency: Approved as a traditional herbal medicinal product for sleep disturbances and mild anxiety in several EU countries

Health Canada: Approved as a Natural Health Product (NHP) with monograph for sleep aid and anxiolytic

Australia Tga: Listed complementary medicine with approved indications for sleep disorders and anxiety

International Status: Recognized in many pharmacopoeias including European Pharmacopoeia, British Pharmacopoeia, and German Commission E monographs

Reported Adverse Events: Very few serious adverse events reported despite widespread use; most common reports involve mild gastrointestinal symptoms, headache, and morning drowsiness

Pharmacovigilance Data: Consistent with favorable safety profile established in clinical studies

Case Reports: Isolated case reports of hepatotoxicity, but causal relationship not definitively established; rare reports of allergic reactions

Longest Duration Studies: Clinical studies up to 8 weeks show continued favorable safety profile; longer-term safety based primarily on traditional use and post-marketing surveillance

Theoretical Concerns: Potential for rare idiosyncratic reactions with long-term use; theoretical concern for hepatotoxicity based on rare case reports

Monitoring Recommendations: No specific monitoring required for long-term use in healthy individuals; periodic liver function testing may be considered in those with pre-existing liver conditions or taking multiple medications

Morning After Effects:

• Morning drowsiness reported in approximately 5-10% of users, typically mild and transient
• Higher doses (>900 mg); taking late at night; individual sensitivity; concurrent use of other sedatives
• Significantly less morning impairment than benzodiazepines or Z-drugs in comparative studies

Cognitive Performance:

• Mild impairment of complex cognitive tasks and reaction time for 2-4 hours after ingestion in some individuals
• No significant impairment of cognitive function or psychomotor performance the morning after evening administration at standard doses in most studies
• Limited data; theoretical concern for impairment immediately after ingestion; no significant evidence for next-day driving impairment with evening use

Recommendations:

• Take at least 2 hours before bedtime and at least 8-10 hours before activities requiring full alertness
• Start with lower doses and increase gradually to minimize risk of morning drowsiness
• Evaluate personal response before engaging in potentially dangerous activities; effects vary significantly between individuals

Prevalence: Rare; estimated at less than 1% of users

Risk Factors: Known allergies to plants in the Valerianaceae family; multiple plant allergies; atopic conditions

Manifestations: Typical allergic reactions including skin rash, itching, hives; rarely more severe reactions including difficulty breathing

Cross Reactivity: Potential cross-reactivity with related plants in the Valerianaceae family; limited data on cross-reactivity with other plant families

Physical Dependence:

• No significant evidence of physical dependence in clinical studies or post-marketing surveillance
• Unlike benzodiazepines and Z-drugs, valerian does not appear to cause dependence even with long-term use

Psychological Dependence:

• Limited evidence of mild psychological dependence in some long-term users
• Primarily concerns about ability to sleep without supplement rather than craving or drug-seeking behavior

Withdrawal Symptoms:

• No significant withdrawal syndrome documented in clinical studies
• Some anecdotal reports of mild and transient symptoms including sleep disturbance for 1-3 days after discontinuing long-term use
• Gradual tapering not generally necessary but may be prudent after very long-term use

Classification: Dietary supplement ingredient under DSHEA (Dietary Supplement Health and Education Act of 1994)

Approved Uses: No approved drug uses; marketed as dietary supplement only

Supplement Status: Legal for sale as dietary supplement; not approved as a food additive

Labeling Restrictions: Cannot make disease claims; structure/function claims must include disclaimer that FDA has not evaluated the claim

Adverse Event Reporting: Serious adverse events must be reported by manufacturers to FDA within 15 days

Manufacturing Requirements: Must comply with dietary supplement cGMP (current Good Manufacturing Practices) under 21 CFR Part 111

United States Pharmacopeia: Monographed in USP-NF (United States Pharmacopeia-National Formulary)

European Pharmacopoeia: Official monograph for Valeriana officinalis L., radix (valerian root)

British Pharmacopoeia: Official monograph for Valerian Root and Valerian Root Dry Extract

German Commission E: Positive monograph for sleep disorders and nervous conditions

Chinese Pharmacopoeia: Monographs for Chinese Valeriana species (not V. officinalis specifically)

Japanese Pharmacopoeia: Not officially monographed

Low to moderate, depending on form and quality

$0.10-$0.75 per day for standard valerian root (300-600mg daily); $0.25-$1.00 per day for premium standardized extracts; $0.05-$0.30 per day for bulk dried root or tea

Overview: Valerian root offers excellent value for its sleep-promoting and anxiolytic effects compared to both conventional pharmaceuticals and many alternative supplements. The cost-benefit ratio is particularly favorable for mild to moderate insomnia and anxiety, where its efficacy approaches that of some prescription medications but at a fraction of the cost and with fewer side effects. Generic and store-brand products provide adequate quality for most users, though standardized extracts with guaranteed valerenic acid content may offer more consistent results and better value despite higher initial cost.

Cost Comparison To Alternatives:

Cost Effectiveness By Form:

Conventional Insurance: Generally not covered by health insurance in the United States and most Western countries

Health Savings Accounts: May be eligible for HSA/FSA reimbursement with a Letter of Medical Necessity in the US

Integrative Medicine Plans: Some specialized integrative medicine insurance plans may provide partial coverage

International Variations: Covered by some national health insurance systems in countries where approved as a traditional herbal medicinal product (parts of Europe); typically requires prescription in these cases

Dried Root: 1-2 years when stored properly in airtight containers away from light, heat, and moisture

Powdered Root: 6-12 months due to increased surface area and exposure to oxidation

Standardized Extracts: 2-3 years when stored in original container at room temperature away from moisture

Tinctures: 3-5 years due to preservative effect of alcohol content

Capsules Tablets: 2-3 years when stored in original container with desiccant if provided

Synthesis Methods

Natural Sources

Quality Considerations

Common Adulterants

Sustainability Considerations

Geographical Considerations

Commercial Forms

Extraction Methods

Supply Chain Considerations

Authentication Methods

Valerian root (Valeriana officinalis) has a rich history of medicinal use spanning over 2,000 years across multiple civilizations. Its name derives from the Latin ‘valere’ meaning ‘to be strong’ or ‘to be healthy,’ reflecting its traditional reputation as a healing herb. Throughout history, valerian has been primarily valued for its calming, sedative, and anxiolytic properties, though its applications have evolved and expanded over time.

From ancient Greek and Roman physicians to medieval European herbalists, and from traditional folk medicine to modern clinical research, valerian has maintained a consistent presence in the therapeutic arsenal for sleep disorders, anxiety, and nervous conditions.

Documented Adverse Effects: Occasional mentions of headache in historical texts, Some reports of morning drowsiness, Rare mentions of digestive upset with large doses, Occasional reports of vivid dreams

Historical Contraindications: Few specific contraindications in historical literature, Some 19th century sources advised caution in ‘bilious temperaments’, Occasionally contraindicated in pregnancy in some traditional sources, Some sources advised caution with very large doses due to potential for headache

Poisoning Cases: Remarkably few documented cases of serious poisoning throughout history, despite widespread use

Safety Reputation: Generally regarded as one of the safer herbal remedies across most historical periods; often specifically recommended as a safer alternative to opium and later to barbiturates

Valerian root (Valeriana officinalis) has been the subject of scientific investigation for its effects on sleep, anxiety, and related conditions for several decades. The evidence base includes in vitro studies, animal models, and human clinical trials, with the strongest evidence supporting its use for insomnia and anxiety. While the quality of studies varies and results are not uniformly positive, meta-analyses generally support modest benefits for sleep quality and anxiety with minimal adverse effects. Research on the individual active compounds, particularly valerenic acid and its derivatives, provides supporting evidence for valerian’s mechanisms of action.

The overall body of evidence suggests that valerian is a mild to moderate sedative and anxiolytic with a favorable safety profile, though its effects may be less potent and consistent than conventional pharmaceutical options.

Investigation of specific valerian compounds for targeted drug development, Exploration of potential applications in neurodegenerative conditions, Research on effects on gut microbiome and gut-brain axis signaling, Studies on genetic factors affecting individual response to valerian, Development of enhanced delivery systems to improve bioavailability, Investigation of potential applications in pain management, Research on long-term effects on stress resilience and neuroplasticity, Exploration of synergistic effects with other herbs and nutrients

Strength Of Evidence: Moderate overall; stronger for subjective sleep quality and mild anxiety; weaker for specific sleep parameters and other conditions

Consistency Of Findings: Mixed results across studies, but meta-analyses generally support modest benefits

Applicability To General Population: Most studies conducted in adults with mild to moderate sleep or anxiety issues; limited evidence in specific clinical populations

Risk Of Bias: Variable quality of studies; many older studies with methodological limitations

Overall Assessment: Sufficient evidence to support use for mild to moderate sleep and anxiety issues in generally healthy adults; promising but not definitive evidence for other applications

Traditional Use Validation: Modern research generally supports traditional applications for sleep, anxiety, and muscle tension

Discrepancies: Traditional use for digestive complaints has limited modern research support; traditional use in higher doses than typically studied in clinical trials

Evolving Understanding: Traditional attribution of effects to essential oil components has shifted to focus on valerenic acid and other non-volatile compounds

Significance: Demonstrates value of traditional knowledge in guiding modern research while refining understanding through scientific methods