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The effects of ketoconazole and rifampin on the single-dose pharmacokinetics of crizotinib in healthy subjects.
Author: BelloAkintunde, BregaNicoletta, O'GormanMelissa, TanWeiwei, XuHuiping
Original Abstract of the Article :
PURPOSE: To investigate the potential effects of strong CYP3A inhibitor ketoconazole and strong CYP3A inducer rifampin on the pharmacokinetics of crizotinib in human. METHODS: Two separate open-label, 2-period, 2-treatment, 1-sequence, crossover, single-dose studies were conducted in healthy subjec...See full text at original site
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引用元:
https://doi.org/10.1007/s00228-015-1945-5
データ提供:米国国立医学図書館(NLM)
Crizotinib and Its Metabolite: A Pharmacokinetic Dance in the Desert
Crizotinib, a medication used to treat certain types of cancer, is metabolized by the CYP3A enzyme, a crucial player in drug metabolism. This study investigates the impact of strong CYP3A inhibitors and inducers on the pharmacokinetics of crizotinib. The researchers conducted two separate single-dose studies in healthy subjects, administering crizotinib alone and in combination with either ketoconazole (a strong CYP3A inhibitor) or rifampin (a strong CYP3A inducer). The results reveal that ketoconazole significantly increased the systemic exposure to crizotinib, while rifampin drastically reduced it, highlighting the crucial role of CYP3A in the drug's metabolism. The study also found that the effects of ketoconazole and rifampin on the metabolite of crizotinib, PF-06260182, were even more pronounced than those on crizotinib itself. These findings provide valuable insights into the pharmacokinetic interactions of crizotinib with other drugs, suggesting the need for careful consideration of potential drug interactions when prescribing this medication.
Navigating the Desert of Drug Interactions
This study reveals the complex dance between crizotinib and CYP3A, emphasizing the need for careful consideration of potential drug interactions. The findings show that strong CYP3A inhibitors can significantly increase crizotinib's exposure, while inducers can dramatically reduce it. These interactions can impact the effectiveness and safety of the drug, highlighting the importance of monitoring patients closely and adjusting dosages as needed. It's like navigating a desert where the landscape can shift unexpectedly due to the influence of other factors. You need to be aware of these potential shifts to avoid getting lost or worse.
Managing Drug Interactions: A Desert Survival Guide
This study provides a vital reminder of the importance of understanding drug interactions, especially when prescribing medications like crizotinib. By carefully considering potential interactions and monitoring patients closely, clinicians can help ensure the safe and effective use of this important drug. Remember, just like a camel needs to be aware of its surroundings in the desert, so too should a doctor be aware of potential drug interactions to ensure the well-being of their patients.
Dr.Camel's Conclusion
This study highlights the complex interplay between crizotinib and CYP3A, emphasizing the importance of understanding drug interactions to ensure safe and effective treatment.
Date :
- Date Completed 2016-09-06
- Date Revised 2018-12-02
Further Info :
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