Ingredient review
Vitex agnus-castus
Description
What is it?
Vitex agnus-castus (VAC) is also commonly known as chaste tree or chasteberry. The plant’s main constituents include vitexin, casticin, agnuside, p-hydroxybenzoic acid, alkaloids, and diterpenoids. The fruit consists of flavonoids, terpenoids, neolignans, phenolic compounds, and glycerides. (20) Its main flavonoids include casticin, vitexin, and orientin. (8) Standardized extracts typically measure the iridoid or flavonoid content where aucubin (iridoid glycoside) or agnuside is used as the reference material. (9)
Download ingredient reviewMain uses
Premenstrual syndrome
Regulation of hormonal balance
Formulations
Form
Safety
Agnolyt ® (100 g of tincture provides 9 g of VAC with 1:5 ratio. A capsule contains dried extract of VAC fruit [9.58–11,5 : 1] 3.5–4.2mg) (5)
Considered as safe with no serious adverse events; 12 of 85 patients reported mild GI distress, skin manifestations or headaches, while 5 reported similarly in B6 group (13)
Agnucaston ® - BNO 1095 (70% ethanol, 30% H2O extract; 4 mg of extract equivalent to 40 mg of dry weight (10:1 ratio) VAC) (2) (25)
No adverse events over 3 menstrual cycles (12)
Agnugol ® (3.2-4.8 mg dried fruit extract ) (6)
Prefemin® - Ze 440 (60% ethanol m/m, fruit extract ratio 6-12:1 standardized for casticin; 20 mg of extract equivalent to 120-240 mg of dry weight VAC) (22)
Equal instances (~5%) of reported adverse events between VAC (20 mg per day) and placebo groups with good tolerability over 3 cycles (22)
No serious adverse events with VAC (20 mg per day) over 3 cycles
(18)
20/50 reported 37 adverse events, none serious in nature (20 mg per day) over 8 cycles (3)
Physicians suspected adverse events in 1% of patients with no serious effects. 94% of patients describe tolerance as good or very good (14)
Dosing & administration
Bone fractures
Dosing & administration
4 mg (as Agnugol® dried fruit extract) per day for 8 weeks
Outcomes
alkaline phosphatase, serum VEGF (6)
Class of evidence
b
Cyclical mastalgia
Dosing & administration
3.2–4.8 mg (as dried fruit extract) for two months
Outcomes
breast pain intensity and length (days) in VAC and placebo, but significantly greater extent in VAC (17)
Class of evidence
b
Hyperprolactinemia
Dosing & administration
20 mg (as Strontan®) per day for 3 months
Outcomes
prolactin release
luteal phase: to normal length, progesterone synthesis, 17 beta-estradiol (16)
Class of evidence
c
Polycystic ovarian syndrome (PCOS)
Dosing & administration
One capsule (as standardized fruit extract to 2, 1-3 and 3 mg of aucubin) per day for 3 months
Outcomes
serum DHEA-S; normalized 60% of participants’ (with oligomenorrhea or amenorrhea) menstrual cycle duration (7)
Class of evidence
b
Postmenopausal hot flashes
Dosing & administration
40 drops per day (as standardized extract - unspecified concentration) for 8 weeks
Outcomes
frequency of hot flashes (1)
Class of evidence
b
Premenstrual syndrome (PMS)
Dosing & administration
20 mg tablet (as ZE 440 fruit extract) per day for 3 cycles
Outcomes
visual analog scale (VAS) compared with placebo (22)
Class of evidence
b
Dosing & administration
8 mg, 20 mg or 30 mg (as ZE 440 fruit extract) per day for 3 cycles
Outcomes
total symptom score. 30 mg did not improve effects observed in 20 mg (23)
Class of evidence
b
Dosing & administration
40 mg (as BNO 1095 extract) per day for 3 cycles
Outcomes
PMSD score, PMTS score (12)
*note: 50% placebo effect
Class of evidence
b
Dosing & administration
40 mg (as BNO 1095 extract) per day for 3 cycles
Outcomes
PMSD score, negative affect score & water retention score (15)
Class of evidence
b
Dosing & administration
40 drops (extract added to fruit juice - unspecified concentration) per day for 6 days prior to menstruation for 6 cycles
Outcomes
mean VAS in VAC and placebo, but to a significantly greater extent by VAS (26)
Class of evidence
b
Adverse effects
Vitex agnus-castus does not pose serious health risks and is considered safe. However, it is recommended that pregnant and lactating women avoid its use due to limited safety data in these states. Commonly reported side effects include nausea, headache, gastrointestinal disturbances, menstrual disorders, acne, pruritus, and erythematous rash. However, these side effects are mild and reversible. (4)(5)
Pharmacokinetics
The pharmacokinetics of VAC have been scarcely studied.
Absorption
- In mice, the oral bioavailability of agnuside was 0.7% with peak plasma concentrations achieved within 30-45 minutes of administration. (21)
- In vitro, BNO 1095 (a VAC extract) solubility and permeability was improved once it was nano-emulsified, suggesting the possibility for improved bioavailability. (19)
Distribution
- In mice, agnuside was found in the highest amounts in the intestine, kidney, liver, spleen, brain, lungs and heart. (21)
Metabolism
- No data is currently available.
Excretion
- No data is currently available.