Ingredient review

Rhodiola rosea

Description

What is it?

The Rhodiola plant consists of over 200 species originating from the Himalayan belt, Tibet, China, and Mongolia. (4) It is one of the most commonly used plants in Chinese traditional medicine for healthy aging, endocrine activity, cardiovascular health, nervous and immune system stimulation, mental and physical performance, and as an adaptogen to fight stress, depression, and anxiety. (17) The two major constituents used to evaluate the quality of Rhodiola rosea-derived compounds are salidroside and tyrosol. (4)

Not be confused with: 

  • Other species of Rhodiola
  • Rosa damascena
  • Rosell
  • Rosmarinic acid
  • Scutellaria baicalensis (also called “golden root”)
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Main uses

Exercise performance
Neurological conditions

Formulations

Proprietary extract
Safety
SHR-5 standardized extract (ethanolic (70%) extract with drug/extract ratio of 4:1; standardized to contain 3.07% rosavin and 1.95% salidroside) (14)(16)
Up to 1360 mg per day over 12 weeks reported safe (14)
WS® 1375 (Rosalin®) (ethanolic (60%) extract with drug/extract ratio of 1.5–5:1) (12)
200 mg, 2x per day over 8 weeks reported safe (12)(13)

Dosing & administration

Adverse effects

Reported adverse effects, typically rare and described as mild in nature, may include headaches at doses of 200 mg per day over 4 weeks. Reports of adverse effects are rare between doses of 50 mg to 1500 mg per day, suggesting a wide profile of safety. (11) Other reported mild or moderate adverse effects include dizziness and dry-mouth. (2)

Pharmacokinetics

Absorption

  • Salidroside is shown to be absorbed in the intestine via the Sodium-dependent Glucose Transporter (SGLT1) in rats. (9)
  • Oral bioavailability of salidroside has shown wide variances between doses.
  • In rats was shown that 12 mg/kg was ~32% bioavailable, (21) 25 mg/kg was ~98%  bioavailable, (3) and 100 mg/kg was ~52%  bioavailable for both salidroside and p-tyrosol. (7)

Distribution

  • Salidroside was found in the liver, kidney, and heart tissues following IV administration, but only in the liver following oral administration in rats. (8)
  • Salidroside was also found in skeletal muscle, fat, ovaries and testis in rats. (22)
  • Salidroside’s deglycosylated metabolite, p-Tyrosol, was found in the heart, spleen, kidney, liver, and lungs, following IV administration of salidroside, and in most tissues other than the brain and kidney following oral administration in rats. (8)

Metabolism

  • Salidroside’s elimination may be highly determined by its metabolism, as only 54% of an administered intravenous dose was recovered from excretion routes. (22
  • In vitro studies show particular inhibition of CYP3A4, though CYP2D6, and CYP1A2 inhibition has also been demonstrated. (10)(19)
  • In vitro studies also show inhibition of MAO and P-gp mediated metabolism. (10)(20)

Excretion

  • In rats, large proportions of Salidroside and small fractions of p-tyrosol are excreted in the urine. (8)(22)

References