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A Short Exploration of Selected Sensitive CYP3A4 Substrates (Probe Drug)
Sarvesh Sabarathinam1, Thangavel M Vijayakumar1
1Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, SRM Nagar, Kattankulathur, 603203, Kanchipuram, Chennai, TN, India.
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.
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