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A Short Exploration of Selected Sensitive CYP3A4 Substrates (Probe Drug)

[ Vol. 14 , Issue. 1 ]

Author(s):

Sarvesh Sabarathinam and Thangavel M. Vijayakumar*   Pages 2 - 4 ( 3 )

Abstract:


Background: CYP450 enzymes in the liver have a significant role in the metabolism of xenobiotics. Probe drug strategy is broadly used to evaluate the pharmacodynamic and pharmacokinetic drug/ herb-drug interactions/ food-drug interactions. Probe drugs reveal the exact pathway of drug metabolism in the liver by their targeted tractability property. The CYP3A4 isoenzyme metabolizes the majority of the drugs (65%).

Methods: The characteristics of targeted probe drugs were observed from the admetSAR (version2) online database.

Results: Midazolam is widely used as a probe drug because of its peculiar character. Midazolam affirms the accurate and consistent prediction of pharmacokinetic mediated drug interactions even in nanogram concentrations with or without a potent CYP3A inhibitor. Remarkably, midazolam is used as a CYP3A4 substrate in the majority of in vivo studies.

Conclusion: It is concluded that midazolam shows a good response in all clinical studies because of its lesser half-life and bioavailability when compared with other probe drugs.

Keywords:

Probe drug, CYP3A4, midazolam, drug interactions, substrates, inhibitor, CAM.

Affiliation:

Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, SRM Nagar, Kattankulathur, 603203, Kanchipuram, Chennai, TN, Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, SRM Nagar, Kattankulathur, 603203, Kanchipuram, Chennai, TN

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