Ingredient review —Tribulus terrestris
What is it?
Description
The plant Tribulus terrestris, commonly known as tribulus or goat’s head, has been used for thousands of years in traditional medicines. Its chemical constituents are said to have analgesic, anti-aging, anti-cancerous, anti-cariogenic, anti-inflammatory, anti-microbial, anti-oxidative, anti-spasmodic, anti-urolithic, diuretic, hepatoprotective, and immunomodulatory properties. Tribulus has known applications in sexual, cardiovascular, and anti-diabetic functions. (5)(22) A variety of tribulus products exist, containing various anatomical parts of the plant (e.g., whole plant, fruit, seeds, aerial parts, leaves, etc.). However, there is a wide discrepancy in the content of its most bioactive saponin components, particularly furostanol and spirostanol, based on the plant’s location of origin and the anatomical parts used. This may affect clinical efficacy, safety, and pharmacodynamic action. (19)
It is important to note that many tribulus products are marketed for their ability to increase testosterone, improve sexual function, and address other disorders related to male or female reproductive organs. However, a large proportion of clinical trials available to date include multi-ingredient formulations, making it unclear as to whether effects are attributable to tribulus, the other ingredients, or their combination. In this ingredient review, only single-ingredient tribulus formulations were considered.
Main uses
Raising testosterone (male and female)
Sexual dysfunction and hypoactive sexual desire
Formulations
Formulation
Comparison
Androsten®
Standardized extract containing 15% steroidal saponins (e.g., 250 mg tablet contains ~37.5 mg protodioscin) (14)
EFFEX®
Standardized extract containing 35-45% furostanol saponins
Provided similar efficacy on erectile dysfunction measures as Tribestan® (18)
Tribestan®
Trib Gold
Standardized extract containing 45% steroidal saponins (e.g., 250 mg contains ~112.5 mg protodioscin) (7)
Dosing & administration
Erectile dysfunction (ED) and hypoactive sexual desire (male)
General outcomes from A-level evidence
Inconsistent results in improvement in International Index of Erectile Function scores were reported (3)
Dosing & administration
500 mg (as Tribestan®) three times per day after meals for 12 weeks to adults with mild or moderate ED with or without hypoactive sexual desire
Outcomes
Improved International Index of Erectile Function score, with improvements in intercourse satisfaction, orgasmic function, sexual desire, overall satisfaction, & Global Efficacy Question scores compared with placebo (10)
Class of evidence
b
Dosing & administration
250 mg (as Trib Gold) three times per day for 12 weeks to adults with late-onset hypogonadism with ED
Outcomes
International Index of Erectile Function score (Arabic version), as well as total testosterone, prostate-specific antigen, & aspartate transaminase compared with baseline, while no changes occurred with placebo (7)
Class of evidence
c
Hypoactive sexual desire (female)
General outcomes from A-level evidence
No data currently available.
Dosing & administration
250 mg (as Androsten®) three times per day for 12-16 weeks to pre- or post-menopausal women with hypoactive sexual desire disorder
Outcomes
the Sexual Quotient Female Version (QS-F) scores for desire, sexual interest, foreplay, arousal, harmonious interaction with partner, lubrication, pain, anorgasmia, and intercourse comfort, the Female Sexual Function Index (FSFI) scores for lubrication and satisfaction, & the Female Intervention Efficacy Index scores for vaginal lubrication, genitalia sensation, sexual intercourse/sexual stimulation, and ability to reach orgasm; & free and bioavailable testosterone
Class of evidence
b
Dosing & administration
7.5 ml (as syrup containing 5.25 mg of ethanolic tribulus extract) twice per day for one month to women with hypoactive sexual desire disorder
Outcomes
FSFI total score and scores for desire, arousal, lubrication, satisfaction, & pain (2)
Class of evidence
b
Male infertility parameters
General outcomes from A-level evidence
Improves sperm motility and morphology parameters in idiopathic male infertility (16)
Dosing & administration
6,000 mg capsules with whole Tribulus terrestris twice per day (morning and night) before food and with warm water for eight weeks to males with oligospermia
Outcomes
abnormal spermatozoa forms and rapid-linear progressive sperm motility compared to baseline, & scores for Quality of Sexual Health including the global index, sexual life, and psychosexual scores
Overall, tribulus produced a 78.11% improvement in vitality and strength, quality of sexual health, semen parameters, & symptoms of oligospermia, though placebo improved by 70.95% (note: no statistically significant difference reported) (17)
Class of evidence
b
Dosing & administration
250 mg (as Tribestan®) three times per day for 12 weeks to men with oligospermia
Outcomes
Improved sperm concentration and morphology, & reduced luteinizing hormone compared to baseline (9)
Class of evidence
c
Testosterone promotion (male)
Dosing & administration
250 mg (as Trib Gold) three times per day for 12 weeks to adults with late-onset hypogonadism with ED
Outcomes
total testosterone, International Index of Erectile Function score (Arabic version), prostate-specific antigen, & aspartate transaminase compared with baseline, while no changes occurred with placebo (7)
Class of evidence
c
Type II diabetes
General outcomes from A-level evidence
No data currently available.
Dosing & administration
500 mg (as hydroalcoholic tribulus extract containing ~60% saponins) twice per day for 12 weeks to adult women
Outcomes
fasting blood glucose, two-hour postprandial glucose, HbA1C, total cholesterol, & LDL (15)
Class of evidence
b
Adverse effects
A higher frequency of side effects do not occur compared with placebo or are reported at similar rates. (2)(6)(10)(15)(20) In one prospective, randomized, double-blind, placebo-controlled clinical trial that included 60 postmenopausal women with sexual dysfunction, the incidence of diarrhea was greater following tribulus intake compared with a placebo. (12)
Pharmacokinetics
Currently, little is known about the pharmacokinetics of tribulus and there is no available data in humans.
Absorption
- Protodioscin, one of the main active components of tribulus, is slowly absorbed with low absolute bioavailability, as shown in rodents (21)
- Saponins possess membrane permeabilizing effects due to its amphiphilic properties that can improve the absorption of other hydrophilic and hydrophobic compounds (19)
Distribution
- Listed from highest to lowest concentrations, post-injection methyl-protodioscin was found in rodent womb, lung, kidney, liver, heart, spleen, small intestine, stomach, large intestine, ovary, skeletal muscle, fat and brain tissues (4)
Metabolism
Excretion
- Methyl-protodioscin possessed a post-injection half-life of 25 to 29 minutes, (4) and protodioscin possessed a post-oral administration half-life of approximately 12 hours in rodents (21)
- Methyl-protodioscin is excreted primarily in bile, as well as in the urine of rodents (4)
Last updated: July 28th, 2020
References
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