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What is it?

Description

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”)

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
  1. Al-Kuraishy, H. (2016). Central additive effect of Ginkgo biloba and rhodiola rosea on psychomotor vigilance task and short-term working memory accuracy. Journal of Intercultural Ethnopharmacology, 5(1), 7-13. ()
  2. Bystritsky, A., Kerwin, L., & Feusner, J. D. (2008). A pilot study of Rhodiola rosea (Rhodax®) for generalized anxiety disorder (GAD). The Journal of Alternative and Complementary Medicine, 14(2), 175-180. ()
  3. Chang, Y., Yao, H., Hsieh, S., Lu, T., & Yeh, T. (2007). Quantitative determination of salidroside in rat plasma by on-line solid-phase extraction integrated with high-performance liquid chromatography/electrospray ionization tandem mass spectrometry. Journal of Chromatography B, 857(1), 164-169. ()
  4. Chiang, H., Chen, H., Wu, C., Wu, P., & Wen, K. (2015). Rhodiola plants: Chemistry and biological activity. Journal of Food and Drug Analysis, 23(3), 359-369. ()
  5. Darbinyan, V., Aslanyan, G., Amroyan, E., Gabrielyan, E., Malmstrom, C., & Panossian, A. (2007). Clinical trial of Rhodiola rosea L. extract SHR-5 in the treatment of mild to moderate depression. Nordic Journal of Psychiatry, 61(5), 343-348. ()
  6. De Bock, K., Eijnde, B. O., Ramaekers, M., & Hespel, P. (2004). Acute Rhodiola rosea intake can improve endurance exercise performance. International Journal of Sport Nutrition and Exercise Metabolism, 14(3), 298-307. ()
  7. Guo, N., Hu, Z., Fan, X., Zheng, J., Zhang, D., Xu, T., . . . Li, H. (2012). Simultaneous determination of salidroside and its aglycone metabolite p-tyrosol in rat plasma by liquid chromatography-tandem mass spectrometry. Molecules, 17(4), 4733-4754. ()
  8. Guo, N., Zhu, M., Han, X., Sui, D., Wang, Y., & Yang, Q. (2014). The metabolism of salidroside to its aglycone p-tyrosol in rats following the administration of salidroside. PLoS ONE, 9(8), e103648. ()
  9. He, Y., Liu, X., Wang, X., Liu, X., Wang, G., & Xie, L. (2010). Sodium-dependent glucose transporter was involved in salidroside absorption in intestine of rats. Chinese Journal of Natural Medicines, 7(6), 444-448. ()
  10. Hellum, B., Tosse, A., Hoybakk, K., Thomsen, M., Rohloff, J., & Nilsen, O. G. (2009). Potent in vitro inhibition of CYP3A4 and p-glycoprotein by Rhodiola rosea. Planta Medica,76(4), 331-338. ()
  11. Ishaque, S., Shamseer, L., Bukutu, C., & Vohra, S. (2012). Rhodiola rosea for physical and mental fatigue: A systematic review. BMC Complementary and Alternative Medicine, 12(1), 70. ()
  12. Kasper, S., & Dienel, A. (2017). Multicenter, open-label, exploratory clinical trial with Rhodiola rosea extract in patients suffering from burnout symptoms. Neuropsychiatric Disease and Treatment, 13, 889-898. ()
  13. Lekomtseva, Y., Zhukova, I., & Wacker, A. (2017). Rhodiola rosea in subjects with prolonged or chronic fatigue symptoms: Results of an open-label clinical trial. Complementary Medicine Research, 24(1), 46-52. ()
  14. Mao, J. J., Xie, S. X., Zee, J., Soeller, I., Li, Q. S., Rockwell, K., & Amsterdam, J. D. (2015). Rhodiola rosea versus sertraline for major depressive disorder: A randomized placebo-controlled trial. Phytomedicine, 22(3), 394-399. ()
  15. Noreen, E. E., Buckley, J. G., Lewis, S. L., Brandauer, J., & Stuempfle, K. J. (2013). The effects of an acute dose of Rhodiola rosea on endurance exercise performance. Journal of Strength and Conditioning Research, 27(3), 839-847. ()
  16. Olsson, E., Schéele, B. V., & Panossian, A. (2009). A randomised, double-blind, placebo controlled, parallel group study of the standardised extract SHR-5 of the roots of Rhodiola rosea in the treatment of subjects with stress-related fatigue. Planta Medica, 75(09), 105-112. ()
  17. Panossian, A., Wikman, G., & Sarris, J. (2010). Rosenroot (Rhodiola rosea): Traditional use, chemical composition, pharmacology and clinical efficacy. Phytomedicine, 17(7), 481-493. ()
  18. Skarpanska-Stejnborn, A., Pilaczynska-Szczesniak, L., Basta, P., & Deskur-Smielecka, E. (2009). The influence of supplementation with Rhodiola rosea l. extract on selected redox parameters in professional rowers. International Journal of Sport Nutrition and Exercise Metabolism, 19(2), 186-199. ()
  19. Thu, O. K., Nilsen, O. G., & Hellum, B. (2016). In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products. Pharmaceutical Biology, 54(12), 3249-3256. ()
  20. Van Diermen, D., Marston, A., Bravo, J., Reist, M., Carrupt, P. A., & Hostettmann, K. (2009). Monoamine oxidase inhibition by Rhodiola rosea L. roots. Journal of Ethnopharmacology, 122(2), 397-401. ()
  21. Yu, S., Liu, L., Wen, T., Liu, Y., Wang, D., He, Y., . . . Wei, W. (2008). Development and validation of a liquid chromatographic/electrospray ionization mass spectrometric method for the determination of salidroside in rat plasma: Application to the pharmacokinetics study. Journal of Chromatography B, 861(1), 10-15. ()
  22. Zhang, Y., Li, L., Lin, L., Liu, J., Zhang, Z., Xu, D., & Xiang, F. (2013). Pharmacokinetics, tissue distribution, and excretion of salidroside in rats. Planta Medica, 79(15), 1429-1433. ()

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