Herb-drug pharmacokinetic interactions: transport and metabolism of indinavir in the presence of selected herbal products

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Date
2015Author
Calitz, Carlemi
Gouws, Chrisna
Viljoen, Joe
Steenekamp, Jan
Hamman, Josias
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Show full item recordAbstract
Patients receiving anti-retroviral drug treatment are sometimes simultaneously taking
herbal remedies, which may result in pharmacokinetic herb-drug interactions. This study aimed
to determine if pharmacokinetic interactions exist between selected commercially available herbal
products (i.e., Linctagon Forte®, Viral Choice® and Canova®) and indinavir in terms of in vitro
transport and metabolism. Bi-directional transport of indinavir was evaluated across Caco-2 cell
monolayers in the presence and absence of the selected herbal products and verapamil (positive
control). Metabolism of indinavir was determined in LS180 cells in the presence and absence of
the selected herbal products as well as ketoconazole (positive control). The secretory transport of
indinavir increased in a concentration dependent way in the presence of Linctagon Forte® and Viral
Choice® when compared to that of indinavir alone. Canova® only slightly affected the efflux of
indinavir compared to that of the control group. There was a pronounced inhibition of the metabolism
of indinavir in LS180 cells over the entire concentration range for all the herbal products investigated
in this study. These in vitro pharmacokinetic interactions indicate the selected herbal products may
affect indinavir’s bioavailability, but the clinical significance needs to be confirmed with in vivo
studies before final conclusions can be made
URI
http://hdl.handle.net/10394/18031http://www.mdpi.com/1420-3049/20/12/19838/pdf
https://doi.org/10.3390/molecules201219838
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- Faculty of Health Sciences [2376]