Echinacea alkamide disposition and pharmacokinetics in humans after tablet ingestion

Matthias, A.; Addison, R. S.; Penman, Kerry G.; Dickinson, R. G.; Bone, Kerry; Lehmann, R.

doi:10.1016/j.lfs.2005.04.009

Cited by 68 publications

(71 citation statements)

References 8 publications

(9 reference statements)

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“…This study and that by Matthias et al [5] reported that alkamides from echinacea are orally available. By contrast, Matthias et al found that phenols were not detected in blood samples after oral administration of tablets formulated from either E. purpurea or E. angustifolia [5]. In this study we were also able to quantitate the alkamide constituents of echinacea (prepared from roots of E. angustifolia and E. purpurea) during multiple dosing.…”

Section: Discussionsupporting

confidence: 69%

“…Similarities between the E. purpurea root and E. angustifolia root in terms of alkylamide content were reported. Furthermore pharmacokinetic parameters of alkamides of combination product of E. purpurea and E. angustifolia root and of E. angustifolia root alone were reported to be similar [5,6,21] and hence the results from the study Gorski et al [9] can be compared with the present study with respect to alkylamide pharmacokinetics.…”

Section: Discussionsupporting

confidence: 52%

“…Echinacea alkamide content in the echinacea tablets used in this study and in the plasma of subjects after oral administration of multiple doses of echinacea tablets were determined using a previously reported and validated LCMS method [5]. Echinacea alkamide content in plasma was determined from blood samples collected over a dosing interval after 2 weeks of regular echinacea intake.…”

Section: Determination Of Echinacea Alkamides In Tablets and In Plasmamentioning

confidence: 99%

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Pharmacokinetic and pharmacodynamic interactions of echinacea and policosanol with warfarin in healthy subjects

Abdul

Jiang

Williams

et al. 2010

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Echinacea and policosanol are commonly used herbal medicines which may be ingested by patients receiving warfarin. Echinacea has been implicated in interacting with drug metabolizing enzymes and policosanol has been shown to decrease platelet aggregation. The potential interaction of echinacea and policosanol with warfarin has not previously been investigated. WHAT THIS STUDY ADDS • Concomitant treatments with echinacea increased the apparent clearance of S‐warfarin but did not have a clinically significant effect on warfarin pharmacodynamics in healthy subjects. Policosanol did not significantly affect warfarin pharmacokinetics or pharmacodynamics. AIMS This study investigated the pharmacokinetic and pharmacodynamic interactions of echinacea and policosanol with warfarin in healthy subjects. METHODS This was an open‐label, randomized, three‐treatment, cross‐over, clinical trial in healthy male subjects (n= 12) of known CYP2C9 and VKORC1 genotype who received a single oral dose of warfarin alone or after 2 weeks of pre‐treatment with each herbal medicine at recommended doses. Pharmacodynamic (INR, platelet activity) and pharmacokinetic (warfarin enantiomer concentrations) end points were evaluated. RESULTS The apparent clearance of (S)‐warfarin (90% CI of ratio; 1.01, 1.18) was significantly higher during concomitant treatment with echinacea but this did not lead to a clinically significant change in INR (90% CI of AUC of INR; 0.91, 1.31). Policosanol did not significantly affect warfarin enantiomer pharmacokinetics or warfarin response. Neither echinacea nor policosanol had a significant effect on platelet aggregation after 2 weeks of pre‐treatment with the respective herbal medicines. CONCLUSION Echinacea significantly reduced plasma concentrations of S‐warfarin. However, neither echinacea nor policosanol significantly affected warfarin pharmacodynamics, platelet aggregation or baseline clotting status in healthy subjects.

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Section: Discussionsupporting

confidence: 69%

Section: Discussionsupporting

confidence: 52%

Section: Determination Of Echinacea Alkamides In Tablets and In Plasmamentioning

confidence: 99%

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Pharmacokinetic and pharmacodynamic interactions of echinacea and policosanol with warfarin in healthy subjects

Abdul

Jiang

Williams

et al. 2010

Brit J Clinical Pharma

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“…It was recently shown that alkylamides from Echinacea are resorbed in vivo and can be detected in nanomolar concentrations (0.5-50 nM) in human blood plasma upon ingestion (26,27).…”

Section: Discussionmentioning

confidence: 99%

“…Immunomodulatory actions of endogenous and exogenous cannabinoids have been investigated in numerous studies (18), mostly performed with isolated cells or transformed cell lines, but only sparse data exist for ex vivo studies or studies with whole blood. Recent reports have shown that plasma levels of alkylamides in the lower nanomolar range can be achieved in humans after oral administration of commercial alkylamide-containing Echinacea preparations (26,27). So far, however, it is not known whether alkylamides can exert immunomodulatory effects via the CB 2 receptor at such low concentrations.…”

mentioning

confidence: 99%

Alkylamides from Echinacea Are a New Class of Cannabinomimetics

Raduner

Majewska

Chen

et al. 2006

Journal of Biological Chemistry

227

119

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Alkylamides (alkamides) from Echinacea modulate tumor necrosis factor ␣ mRNA expression in human monocytes/macrophages via the cannabinoid type 2 (CB 2 ) receptor (Gertsch, J., Schoop, R., Kuenzle, U., and Suter, A. (2004) FEBS Lett. 577, 563-569). Here we show that the alkylamides dodeca-2E,4E,8Z,10Z-tetraenoic acid isobutylamide (A1) and dodeca-2E,4E-dienoic acid isobutylamide (A2) bind to the CB 2 receptor more strongly than the endogenous cannabinoids. The K i values of A1 and A2 (CB 2 ϳ60 nM; CB 1 >1500 nM) were determined by displacement of the synthetic high affinity cannabinoid ligand [ 3 H]CP-55,940. Molecular modeling suggests that alkylamides bind in the solvent-accessible cavity in CB 2 , directed by H-bonding and -interactions. In a screen with 49 other pharmacologically relevant receptors, it could be shown that A1 and A2 specifically bind to CB 2 and CB 1 . A1 and A2 elevated total intracellular Ca 2؉ in CB 2 -positive but not in CB 2 -negative promyelocytic HL60 cells, an effect that was inhibited by the CB 2 antagonist SR144528. At 50 nM, A1, A2, and the endogenous cannabinoid anandamide (CB 2 K i >200 nM) up-regulated constitutive interleukin (IL)-6 expression in human whole blood in a seemingly CB 2 -dependent manner. A1, A2, anandamide, the CB 2 antagonist SR144528 (K i <10 nM), and also the non-CB 2 -binding alkylamide undeca-2E-ene,8,10-diynoic acid isobutylamide all significantly inhibited lipopolysaccharide-induced tumor necrosis factor ␣, IL-1␤, and IL-12p70 expression (5-500 nM) in a CB 2 -independent manner. Alkylamides and anandamide also showed weak differential effects on anti-CD3-versus anti-CD28-stimulated cytokine expression in human whole blood. Overall, alkylamides, anandamide, and SR144528 potently inhibited lipopolysaccharide-induced inflammation in human whole blood and exerted modulatory effects on cytokine expression, but these effects are not exclusively related to CB 2 binding.

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Echinacea for preventing and treating the common cold

Karsch‐Völk

Barrett

Kiefer

et al. 2014

Cochrane Database of Systematic Reviews

196

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BackgroundEchinacea plant preparations (family Asteraceae) are widely used in Europe and North America for common colds. Most consumers and physicians are not aware that products available under the term Echinacea differ appreciably in their composition, mainly due to the use of variable plant material, extraction methods and the addition of other components. ObjectivesTo assess whether there is evidence that Echinacea preparations are effective and safe compared to placebo in the prevention and treatment of the common cold.

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Echinacea alkamide disposition and pharmacokinetics in humans after tablet ingestion

Cited by 68 publications

References 8 publications

Pharmacokinetic and pharmacodynamic interactions of echinacea and policosanol with warfarin in healthy subjects

Pharmacokinetic and pharmacodynamic interactions of echinacea and policosanol with warfarin in healthy subjects

Alkylamides from Echinacea Are a New Class of Cannabinomimetics

Echinacea for preventing and treating the common cold

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