Background: In healthy volunteers, the probe drug method is widely practised to assess the pharmacokinetic
mediated herb-drug interactions (HDI). We analyzed the clinical evidence of CYP3A4 probe drug, Midazolam.
Methods: Literatures where Midazolam was used as a probe drug for prediction of herb-drug interaction was survey
through an online database such as google scholar, Scopus, Cochrane, PubMed and clinicaltrials.gov.
Results: Midazolam was considered as a sensitive probe for CYP3A4 substrates due to its bioavailability. We observed
that not all the herbs are causing drug interaction. However, significant changes of the Midazolam pharmacokinetics were
found after high-dose and long-term intake of some herbs and food supplements, Suggesting the induction and/or
inhibition of CYP activities.
Conclusion: Probe drug technique is one of the easiest ways for predicting CYP enzyme-mediated herb-drug interactions.
Midazolam shows a good response in clinical studies because of short half-life and low harmfulness compared with other