For healthcare professionals, the volume of literature available on herb-drug interactions often makes it
difficult to separate experimental/potential interactions from those deemed clinically relevant. There is a need for
concise and conclusive information to guide pharmacotherapy in HIV/AIDS. In this review, the bases for potential
interaction of medicinal herbs with specific antiretroviral drugs are presented, and several botanicals are discussed
for which clinically relevant interactions in humans are established. Such studies have provided, in most cases, sufficient
ground to warrant the avoidance of concurrent administration of antiretroviral (ARVs) drugs with St John’s
wort (Hypericum perforatum), black pepper (Piper species) and grapefruit juice. Other botanicals that require caution in the use with
antiretrovirals include African potato (Hypoxis hemerocallidea), ginkgo (Ginkgo biloba), ginseng (Panax species), garlic (Allium sativum),
goldenseal (Hydrastis canadensis) and kava kava (Piper methysticum). The knowledge of clinically significant herb-drug interaction
will be important in order to avoid herb-induced risk of sub-therapeutic exposure to ARVs (which can lead to viral resistance) or the
precipitation of toxicity (which may lead to poor compliance and/or discontinuation of antiretroviral therapy).
Keywords: Antiretroviral therapy, drug metabolism, enzyme inhibition, herb-drug interaction, HIV/AIDS, grapefruit juice, pharmacokinetics,
piperine, St John’s wort.
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