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Ingredient review

Valeriana officinalis

Description

What is it?

Valeriana officinalis, commonly referred to as Valerian root, is a medicinal herb found in North America, Asia, and Europe that has been traditionally used to treat sleep and anxiety disorders.  Valerian contains more than 150 phytochemicals, and valerian extracts are most often standardized by their valeric acid content. However, it is not fully known which constituents are primarily responsible for its effects. (26)(31)(54) Valerian’s mechanism of action is not completely understood but may be due to its stimulation of GABA transmission via positive modulation of GABA-A receptors, (7)(33) similarly to benzodiazepines (a class of sedatives). (31) However, valerian may possess certain advantages over benzodiazepines and other conventional sedatives, including lower rates of adverse events. (18)(27)(59) For example, valerian may not impair alertness, concentration, or reaction time upon awakening, (35) impair machine operation and driving ability, (22)(57) or exhibit the same extent of clinically relevant interactions with other pharmaceuticals. It is important to note, however, that valerian may theoretically have additive effects if administered in combination with other sedatives. (26)(31)

Main uses

Anxiety and stress
Behavioral and nervous system regulation
Insomnia and sleep disturbance
Premenstrual, menstrual, and postmenopausal symptoms

Formulations

Formulation
Characteristics
Dormeasan ®
Tincture containing 460 mg valerian root at a drug extract ratio (DER) of 1:10 and 460 mg of Humulus lupulus at a DER of 1:12, both of which are dissolved in 61% ethanol (15)
LI 156 (Sedonium®)
Contains 300 mg dry root extract of at a DER of 3-6:1 (14)
NSF-3
Contains 300 mg valerian standardized to 0.8% valerenic acid, 30 mg Humulus lupulus standardized to 0.35% rutin, and 80 mg Passiflora incarnata standardized to 4% isovitexin in a 410 mg tablet (38)
Songha Night™
Contains 120 mg of valerian extract at a DER of 4.5:1 and 80 mg of Melissa officinalis extract at a DER of 5:1 (32)
Valdispert ® forte
Contains 135 mg of aqueous alkaline dried valerian root extract with DER of 5-6:1 (52)
Ze 185 (Relaxane®)
Contains 90 mg of a 55% methanolic valerian root extract at a DER of 5-8:1, 90 mg of a 90% ethanolic Petasites hybridus root extract at a DER of 7-14:1, 90 mg of a 50% ethanolic Passiflora incarnata herbal extract at a DER of 3-6:1, and 60 mg of a 20% ethanolic Melissa officinalis leaf extract at a DER of 3.5-5.5:1 (40)
Ze 91019
Contains 250 mg of a 45% methanolic valerian root extract at a DER of 4-6:1 and 60 mg of Humulus lupulus extract at a DER of 5-7:1 (34)(58)

Dosing & administration

Adverse effects

Reported side effects may include headaches, gastrointestinal distress, nausea, diarrhea, sweating, dizziness, drowsiness, or other psychological effects such as feelings of isolation, brain fog, depression, or irritability. Valerian does not appear to have an increased risk of any severe side effects compared to other pharmaceutical treatments or placebo groups. (8)(56) However, the likelihood of experiencing multiple adverse events per patient may be greater than placebo. (36)

Pharmacokinetics

Absorption

  • Valerenic acid max serum concentration occurs between 1-2 hours in healthy adults with large interindividual variability (range 0.5-4 hours) (2)(3)
  • Similar absorption speed occurs with single- or multiple-doses (3)

Distribution

  • Valerenic acid in serum measurable for at least five hours in healthy adults (2)

Metabolism

  • Low doses (125 mg three times per day) did not inhibit CYP2D6, CYP1A2, CYP3A4/5, or CYP2E1 in humans (25)
  • High doses (500 mg twice per day) mildly inhibited CYP2D6, but not likely in a clinically relevant fashion and had no effect on CYP3A4 in humans (17)

Excretion

  • Valerenic acid’s half-life was approximately one hour in healthy adults (2)(3)
  • Similar elimination rate occurs with single- or multiple-doses, but elimination rate may be positively correlated with body weight indicating that higher range doses may be required for individuals with increased body weight (3)

 

Last updated: September 14th, 2020

References